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Results for "

Oral

" in MCE Product Catalog:

3767

Inhibitors & Agonists

3

Screening Libraries

3

Dye Reagents

19

Peptides

1

Inhibitory Antibodies

141

Natural
Products

380

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-111755
    Oral antiplatelet agent 1

    P2Y Receptor Cardiovascular Disease
    Oral antiplatelet agent 1 is a potent antiplatelet agent with an IC50 of 2.94 μM in vitro as well as antithrombotic efficacy in a rat model. P2Y receptor antagonist.
  • HY-12422B
    (2S,3R)-Voruciclib hydrochloride

    CDK Cancer
    (2S,3R)-Voruciclib hydrochloride is the enantiomer of Voruciclib hydrochloride. (2S,3R)-Voruciclib is an orally active CDK inhibitor.
  • HY-76511
    Verlukast

    MK-679; L 668019

    Leukotriene Receptor Inflammation/Immunology
    Verlukast is a potent, selective, and orally active antagonist of leukotriene receptor. Verlukast has the potential for the research of asthma.
  • HY-107787
    Dioxopromethazine

    Prothanon; 9,9-Dioxopromethazine; 9,9-Dioxypromethazin

    Histamine Receptor Inflammation/Immunology
    Dioxopromethazine is an orally active antihistamine. Dioxopromethazine inhibits asthmatic symptoms.
  • HY-77591
    Cysteamine hydrochloride

    2-Aminoethanethiol hydrochloride; 2-Mercaptoethylamine hydrochloride

    Autophagy Reactive Oxygen Species Apoptosis Endogenous Metabolite Metabolic Disease Cancer
    Cysteamine hydrochloride (2-Aminoethanethiol hydrochloride) is an orally active agent for the treatment of nephropathic cystinosis and an antioxidant.
  • HY-124419
    RO0711401

    mGluR Neurological Disease
    RO0711401 is a selective and orally active positive allosteric modulator of mGlu1 receptor with an EC50 of 56 nM.
  • HY-132824
    Ledaborbactam etzadroxil

    VNRX-7145

    Bacterial Infection
    Ledaborbactam etzadroxil (VNRX-7145) is an orally active Ambler class A, C, and D β-lactamase enzymes inhibitor.
  • HY-A0165
    Tofisopam

    Others Neurological Disease
    Tofisopam, a 2,3-benzodiazepine compound, is an orally active anxiolytic agent.
  • HY-106499
    Sulfinalol

    Adrenergic Receptor Cardiovascular Disease
    Sulfinalol is an orally active β-adrenoceptor antagonist with direct vasodilator activity.
  • HY-15531
    Venetoclax

    ABT-199; GDC-0199

    Bcl-2 Family Autophagy Cancer
    Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy.
  • HY-W173220
    Clopirac

    PGE synthase Inflammation/Immunology
    Clopirac is a potent and orally active inhibitor of prostaglandin synthetase. Clopirac is an anti-inflammatory agent.
  • HY-137442
    Inupadenant

    EOS-850

    Adenosine Receptor Cancer
    Inupadenant is an orally active, highly selective A2A receptor antagonist. Inupadenant is not brain-penetrant. Inupadenant has potent anti-tumor activity.
  • HY-106571
    Cefteram pivoxil

    Ro 19-5248; T-2588

    Bacterial Infection
    Cefteram pivoxil (Ro 19-5248), an orally active cephalosporin antibiotic, is used for bacterial infections.
  • HY-76511S
    Verlukast-d6

    MK-679-d6; L 668019-d6

    Leukotriene Receptor Inflammation/Immunology
    Verlukast-d6 is a deuterium labeled Verlukast. Verlukast is a potent, selective, and orally active antagonist of leukotriene receptor. Verlukast has the potential for the research of asthma.
  • HY-10913
    Danegaptide

    GAP-134; ZP 1609

    Gap Junction Protein Cardiovascular Disease
    Danegaptide (GAP-134) is a potent, selective and orally active gap-junction modifier with an antiarrhythmic effect.
  • HY-10913A
    Danegaptide Hydrochloride

    GAP-134 Hydrochloride; ZP 1609 Hydrochloride

    Gap Junction Protein Cardiovascular Disease
    Danegaptide Hydrochloride (GAP-134 Hydrochloride) is a potent, selective and orally active gap-junction modifier with an antiarrhythmic effect.
  • HY-129683
    AM3102

    PPAR Metabolic Disease
    AM3102 is an oleoylethanolamide (OEA) analog. AM3102 is an endogenous high-affinity PPAR-alpha agonist. AM3102 resists enzymatic hydrolysis, activates PPAR-alpha with high potency in vitro, and persistently reduces feeding when administered in vivo either parenterally or orally.
  • HY-139346
    VX-150

    Sodium Channel Neurological Disease
    VX-150 is an orally active, highly selective NaV1.8 inhibitor. VX-150 has the potential for various pain indications research.
  • HY-100411
    MLi-2

    LRRK2 Neurological Disease
    MLi-2 is an orally active and highly selective LRRK2 inhibitor with an IC50 of 0.76 nM. MLi-2 has the potential for Parkinson’s disease.
  • HY-107533
    T-98475

    Others Endocrinology
    T-98475 (Compound 26d) is a potent, orally active, non-peptide luteinizing hormone-releasing hormone (LHRH) receptor antagonist with an IC50 of 0.2 nM.
  • HY-16735
    Avoralstat

    BCX4161

    Ser/Thr Protease Others
    Avoralstat (BCX4161), a potent and orally active plasma kallikrein (PKK) inhibitor, is used for hereditary angioedema research.
  • HY-145704
    Antimalarial agent 8

    Others Infection
    Antimalarial agent 8 (Compound 7e) is a novel orally active class of antimalarials. Antimalarial agent 8 is potent in vitro against P. falciparum and is orally efficacious (40 mg/kg) in an in vivo mouse model of malaria.
  • HY-110274
    IP7e

    Others Inflammation/Immunology
    IP7e is a potent, brain-penetrant and orally active Nurr1 activator with an EC50 value of 3.9 nM.
  • HY-106538
    Cadralazine

    ISF 2469

    Others Cardiovascular Disease
    Cadralazine (ISF 2469) is an orally active antihypertensive agent. Cadralazine is a peripheral arteriolar vasodilator.
  • HY-W011651
    Carbutamide

    BZ-55

    Others Metabolic Disease
    Carbutamide (BZ-55) is an orally active and first-generation sulfonylurea with hypoglycemic activity.
  • HY-13728B
    (Rac)-Plevitrexed

    (Rac)-ZD 9331; (Rac)-BGC9331

    Thymidylate Synthase Cancer
    (Rac)-Plevitrexed ((Rac)-ZD 9331; (Rac)-BGC9331) is a racemate of Plevitrexed. Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor.
  • HY-107318
    Alacepril

    Cetapril; DU-1219

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Alacepril (Cetapril) is an orally active angiotensin converting enzyme (ACE) inhibitor with long lasting antihypertensive effect.
  • HY-131914A
    EST64454 hydrochloride

    Sigma Receptor Neurological Disease
    EST64454 hydrochloride is a selective and orally active sigma-1 receptor antagonist with a Ki of 22 nM. EST64454 hydrochloride has the potential for the research of the pain.
  • HY-10162
    Olaparib

    AZD2281; KU0059436

    PARP Autophagy Mitophagy Cancer
    Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator.
  • HY-131705
    BTK inhibitor 17

    Btk Inflammation/Immunology
    BTK inhibitor 17 is a potent and orally active irreversible BTK inhibitor with an IC50 of 2.1 nM. BTK inhibitor 17 can be used for rheumatoid arthritis research.
  • HY-106506
    Desciclovir

    BW A515U

    Others Infection
    Desciclovir is a potent and orally active prodrug of the antiherpetic agent Acyclovir (ACV). Desciclovir is converted to acyclovir in vivo by xanthine oxidase.
  • HY-124073
    Dihydrocapsiate

    TRP Channel Metabolic Disease
    Dihydrocapsiate, as a compound of capsinoid family, is an orally active TRPV1 agonist. Dihydrocapsiate can be used for the research of metabolism disease.
  • HY-B1682
    Loracarbef

    Antibiotic Bacterial Infection
    Loracarbef, a cephalosporin antibiotic, is an orally active second-generation synthetic beta-lactam antibiotic of the carbacephem class.
  • HY-B1682A
    Loracarbef hydrate

    Antibiotic Bacterial Infection
    Loracarbef hydrate, a cephalosporin antibiotic, is an orally active second-generation synthetic beta-lactam antibiotic of the carbacephem class.
  • HY-137463
    AG-636

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Cancer
    AG-636 is a potent, reversible, selective and orally active dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 17 nM. AG-636 has strong anticancer effects.
  • HY-135655A
    Fobrepodacin

    SPR720; pVXc-486

    Bacterial Infection
    Fobrepodacin (SPR720) is an orally active and potent phosphate prodrug of SPR719 (VXc-486; HY-12930). Fobrepodacin has potent bactericidal activities in vivo.
  • HY-109155
    Paltusotine

    CRN00808

    Somatostatin Receptor Endocrinology
    Paltusotine (CRN00808) is an orally active, nonpeptide selective somatostatin type 2 (SST2) receptor agonist. Paltusotine has the potential for maintaining GH and IGF-1 levels after depot somatostatin receptor ligand therapy.
  • HY-13728A
    (R)-Plevitrexed

    (R)-ZD 9331; (R)-BGC9331

    Others Cancer
    (R)-Plevitrexed ((R)-ZD 9331; (R)-BGC9331) is a less active enantiomer of Plevitrexed. Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor.
  • HY-125856
    Milvexian

    BMS-986177; JNJ-70033093

    Factor Xa Cardiovascular Disease
    Milvexian (BMS-986177), an effective antithrombotic agent, is an orally-bioavailable, reversible and direct inhibitor of human and rabbit factor XIa (FXIa) with Ki of 0.11, and 0.38 nM, respectively.
  • HY-132815
    Fostroxacitabine bralpamide

    MIV-818

    Nucleoside Antimetabolite/Analog Cancer
    Fostroxacitabine bralpamide (MIV-818) is an orally active Troxacitabine-based nucleotide prodrug. Fostroxacitabine bralpamide has anticancer effects.
  • HY-108685
    Alendronate sodium

    Alendronic acid monosodium salt

    Others Metabolic Disease
    Alendronate sodium is an orally active nitrogen-containing bisphosphonate. Alendronate sodium potently inhibits bone resorption. Alendronate sodium is used for the research of postmenopausal osteoporosis.
  • HY-14383
    Vosilasarm

    RAD140

    Androgen Receptor Endocrinology Neurological Disease
    Vosilasarm (RAD140) is a potent, orally active, nonsteroidal selective androgen receptor modulator (SARM) with a Ki of 7 nM. Vosilasarm shows good selectivity over other steroid hormone nuclear receptors.
  • HY-133013
    GLPG-3221

    CFTR Inflammation/Immunology
    GLPG-3221 is a potent, orally active corrector of CFTR (cystic fibrosis transmembrane conductance regulator), with an EC50 of 105 nM. GLPG-3221 can be uesd for the treatment of cystic fibrosis.
  • HY-B1656
    Fomocaine

    P 652

    Others Neurological Disease Cardiovascular Disease
    Fomocaine (P 652) is an orally active local anaesthetic. Fomocaine shows antiarrhythmic activity.
  • HY-109099
    Pemigatinib

    INCB054828

    FGFR Cancer
    Pemigatinib (INCB054828) is an orally active, selective FGFR inhibitor with IC50s of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma.
  • HY-117507
    U92016A hydrochloride

    5-HT Receptor Neurological Disease
    U92016A hydrochloride is a potent, metabolically stable, orally acitive 5-HT1A receptor agonist with an exceptionally high degree of intrinsic activity. U92016A hydrochloride binds with high affinity to human 5-HT1A receptors expressed in Chinese hamster ovary cells (Ki=0.2 nM).
  • HY-144110
    HCV-IN-37

    HCV Infection
    HCV-IN-37 (Compound 3d) is a potent inhibitor of HCV. HCV-IN-37 is orally available and long-lasting in rat plasma after oral administration to rats by a single dose of 15 mg/kg. The high potency of active derivative HCV-IN-37 is primarily driven by the inhibitory effect on the virus entry stage.
  • HY-106578
    Quinupramine

    LM 208

    Neurological Disease
    Quinupramine is an orally active antidepressant. Quinupramine can penetrate into the CNS and affect some of the processes of neurotransmission. The antidepressant activity of quinupramine is associated with the central serotonin system, but not with the β-adrenergic system.
  • HY-144393
    P-gp/BCRP-IN-1

    BCRP Cancer
    P-gp/BCRP-IN-1 (compound 19) is a potential, relatively safe, orally active and efficient efflux transporter (P-gp and BCRP) inhibitor. P-gp/BCRP-IN-1 exerts resistance reversal by inhibiting the efflux function of P-gp and BCRP. P-gp/BCRP-IN-1 can overcome the resistance and improve the oral bioavailability of PTX (Paclitaxel).
  • HY-B1800
    Tolonidine

    Others Cardiovascular Disease
    Tolonidine is a derivative of imidazoline. Tolonidine is orally active and has been shown to possess hypotensive and antihypertensive properties.
  • HY-13236
    LUF6000

    Adenosine Receptor Cardiovascular Disease
    LUF6000 is an orally active allosteric modulator of the A3 adenosine receptor. LUF6000 has potent anti-inflammatory effect.
  • HY-108504
    Co 102862

    V 102862

    Sodium Channel Neurological Disease
    Co 102862 (V 102862) is a potent, broad-spectrum, state-dependent Na + channel blocker. Co 102862 is also an orally active anticonvulsant.
  • HY-12177S
    Aliskiren-d6 hemifumarate

    CGP 60536 D6 hemifumarate; CGP60536B D6 hemifumarate; SPP 100 D6 hemifumarate

    Renin Autophagy Cancer Cardiovascular Disease
    Aliskiren D6 hemifumarate (CGP 60536 D6 hemifumarate) is a deuterium labeled Aliskiren hemifumarate. Aliskiren hemifumarate is a direct and orally active renin inhibitor with an IC50 of 1.5 nM.
  • HY-132196
    BTK inhibitor 18

    Btk Inflammation/Immunology
    BTK inhibitor 18 is a potent, selective,orally active and covalent Btk inhibitor with a IC50 of 142 nM. BTK inhibitor 18 has anti-inflammatory activities.
  • HY-B0467S
    Amoxicillin D4

    Amoxycillin D4

    Bacterial Infection
    Amoxicillin D4 (Amoxycillin D4) is a deuterium labeled Amoxicillin. Amoxicillin is an antibiotic with good oral absorption and broad spectrum antimicrobial activity.
  • HY-N7225
    Yuanhuacine

    Gnidilatidin

    Others Cancer
    Yuanhuacine (Gnidilatidin), a daphnane diterpenoid from the flowers of Daphne genkwa with extensive anti-tumor activity. Yuanhuacine is a DNA-damaging agent with orally active.
  • HY-17359
    Deferasirox

    ICL 670

    Bacterial Ferroptosis Cancer
    Deferasirox (ICL 670) is an orally available iron chelator used for the management of transfusional iron overload.
  • HY-A0252
    Bupranolol

    Adrenergic Receptor Cancer Inflammation/Immunology
    Bupranolol is an orally active, competitive and non-selective β-adrenoceptor antagonist without intrinsic sympathomimetic activity.
  • HY-101820A
    Simotinib hydrochloride

    EGFR Cancer
    Simotinib hydrochloride is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities.
  • HY-B1363
    Bendroflumethiazide

    Bendrofluazide

    Others Cardiovascular Disease
    Bendroflumethiazide is an orally active diuretic. Bendroflumethiazide is an antihypertensive agent. Bendroflumethiazide has the potential for the research of arterial hypertensive disease.
  • HY-101820
    Simotinib

    EGFR Cancer
    Simotinib is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities.
  • HY-B1651
    Iron(II) fumarate

    Ferrous fumarate

    Others Metabolic Disease
    Iron(II) fumarate (Ferrous fumarate) is the iron(II) salt of fumaric acid. Iron(II) fumarate is an orally active dietary supplement and has the potential for iron deficiency anemia treatment.
  • HY-116437
    Selatinib

    EGFR Cancer
    Selatinib is a reversible and orally active dual EGFR and ErbB2 inhibitor with IC50s of 13 nM and 22.5 nM, respectively. Selatinib has anticancer effects.
  • HY-W020183
    γ-Terpinene

    Others Neurological Disease
    γ-Terpinene, a monoterpene, is an orally active antioxidant compound which can scavenge radicals directly. γ-Terpinene has potent antinociception activity.
  • HY-146075
    β-Lactamase-IN-8

    Bacterial Infection
    β-Lactamase-IN-8 (compound 20) is a potent and oral bioavailable broad-spectrum cyclic boronate β-lactamase inhibitor. β-Lactamase-IN-8 can be used for researching antibacteria.
  • HY-19947
    PF-06291874

    Glucagon receptor antagonists-4

    Glucagon Receptor Metabolic Disease
    PF-06291874 is a highly potent, non-peptide and orally active glucagon receptor antagonist. PF-06291874 is under the study for type 2 diabetes mellitus (T2DM).
  • HY-17463
    Prednisolone

    Glucocorticoid Receptor Endogenous Metabolite Endocrinology
    Prednisolone is a potent, orally active corticosteroid and a glucocorticoid. Prednisolone possesses about four times the anti-inflammatory activity of hydrocortisone while causing less salt and water retention. Prednisolone can be used for ocular, anti-inflammatory research.
  • HY-139585
    Tigulixostat

    LC350189

    Xanthine Oxidase Metabolic Disease
    Tigulixostat (LC350189) is an orally active, non-purine selective xanthine oxidase inhibitor. Tigulixostat lowers the production of uric acid. Tigulixostat can be used for gout and hyperuricemia study.
  • HY-B0255
    Adefovir dipivoxil

    GS 0840

    HBV Reverse Transcriptase Infection Cancer
    Adefovir dipivoxil, an adenosine analogue, is an oral prodrug of the nucleoside reverse transcriptase inhibitor Adefovir. Adefovir dipivoxil inhibits both the wild type and HBV Lamivudine-resistant strains.
  • HY-W105835
    Magnesium citrate

    Others Neurological Disease
    Magnesium citrate is a magnesium salt form that provides efficient penetration into brain and muscle tissue. Magnesium citrate increases pain threshold and reduces TLR4 concentration in the brain. Orally active.
  • HY-18345
    SR 49059

    Vasopressin Receptor Cardiovascular Disease Endocrinology
    SR 49059 (SR-49059) is a potent, orally active, selective vasopressin V1a antagonist with a Ki vaule of 1.4 nM.
  • HY-143200
    OSBPL7-IN-1

    Others Metabolic Disease
    OSBPL7-IN-1 is an orally active oxysterol binding protein like 7 (OSBPL7) inhibitor. OSBPL7-IN-1 promotes an increase of ABCA1 at the plasma membrane without affecting mRNA expression.
  • HY-122661
    Mefuparib hydrochloride

    MPH

    PARP Apoptosis Cancer
    Mefuparib hydrochloride (MPH) is an orally active, substrate-competitive and selective PARP1/2 inhibitor with IC50s of 3.2 nM and 1.9 nM, respectively. Mefuparib hydrochloride induces apoptosis and possesses prominent anticancer activity in vitro and in vivo.
  • HY-N7557
    (E)-2'-Hydroxy-3,4-dimethoxychalcone

    Others Cancer
    (E)-2'-Hydroxy-3,4-dimethoxychalcone (compound 7) is a Chalcone derivative with orally active. (E)-2'-Hydroxy-3,4-dimethoxychalcone has anti-tumour activities.
  • HY-142687
    SGK1-IN-4

    SGK Inflammation/Immunology
    SGK1-IN-4 (compound 17a) is a highly selective, orally active SGK1 inhibitor. SGK1-IN-4 can be used for osteoarthritis research.
  • HY-121776
    Nicomol

    Others Cardiovascular Disease
    Nicomol is an orally active hypolipidemic agent that can increase the high density lipoprotein cholesterol (HDL-C) level. Nicomol inhibits the rapid rise of plasma free fatty acids.
  • HY-145272
    ELOVL1-IN-3

    Others Neurological Disease
    ELOVL1-IN-3 (Compound 22) is a potent and orally active inhibitor of elongation of very long chain fatty acid 1 (ELOVL1) enzyme. ELOVL1-IN-3 serves as a useful tool for researching adrenoleukodystrophy (ALD)[1].
  • HY-A0287
    Clomifene

    Clomiphene

    Others Endocrinology
    Clomifene is an orally active compound used for infertility. Clomifene is a simple, relatively safe, easily administered and well-tolerated efficacious compound to induce ovulation.
  • HY-12697
    NGB 2904

    Dopamine Receptor Neurological Disease
    NGB 2904 is an orally active and selective dopamine (DA) D3 receptor antagonist. NGB 2904 can be used for the research of cocaine addiction.
  • HY-14568
    DCCCyB

    GlyT Neurological Disease
    DCCCyB is an orally bioavailable, potent, and selective inhibitor of GlyT1. DCCCyB demonstrates excellent in vivo occupancy of GlyT1 transporters in rhesus monkey.
  • HY-A0287A
    Clomifene hydrochloride

    Clomiphene hydrochloride

    Others Endocrinology
    Clomifene hydrochloride is an orally active compound used for infertility. Clomifene hydrochloride is a simple, relatively safe, easily administered and well-tolerated efficacious compound to induce ovulation.
  • HY-139398
    TBI-223

    Bacterial Infection
    TBI-223 is an orally bioavailable oxazolidinone antibiotic and an antimicrobial. TBI-223 shows activity against Mycobacterium tuberculosis (Mtb).
  • HY-112318A
    GSK-2793660

    Cathepsin Inflammation/Immunology
    GSK-2793660 is an orally active and irreversible inhibitor of Cathepsin C (CTSC). GSK-2793660 can be used for the research of bronchiectasis.
  • HY-143793
    RBP4 inhibitor 1

    Others Metabolic Disease
    RBP4 inhibitor 1 (compound 43b) is a potent and orally active retinol-binding protein 4 (RBP4) inhibitor with IC50s of 28 nM and 110 nM for human and mouse RBP4. RBP4 inhibitor 1 has a potent and long-lasting blood RBP4-level-reducing effect in mice.
  • HY-144073
    HPK1-IN-21

    MAP4K Cancer
    HPK1-IN-21 is a potent inhibitor of HPK1 kinase inhibitor (Ki=0.8 nM), HPK1-IN-21 also has orally active.
  • HY-141482
    WSB1 Degrader 1

    E1/E2/E3 Enzyme Cancer
    WSB1 Degrader 1 is a poten and orally active WSB1 (WD repeat and SOCS box-containing 1) degrader. WSB1 Degrader 1 has anticancer metastatic effects.
  • HY-141525
    SCD1 inhibitor-4

    Stearoyl-CoA Desaturase (SCD) Metabolic Disease
    SCD1 inhibitor-4 is a potent, orally active stearoylCoA desaturase-1 (SCD1) inhibitor. SCD1 inhibitor-4 can be used for the research of diabetes.
  • HY-120494
    sEH inhibitor-1

    Epoxide Hydrolase Inflammation/Immunology
    sEH inhibitor-1 (compound TCPU ) is a potent and oral active inhibitor of sEH (soluble epoxide hydrolase) with IC50s of 0.4 and 5.3 nM in human and murine, respectively.
  • HY-12222
    Obeticholic acid

    INT-747; 6-ECDCA; 6-Ethylchenodeoxycholic acid

    FXR Autophagy Others
    Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy.
  • HY-105860
    Selurampanel

    BGG 492

    iGluR Neurological Disease
    Selurampanel (BGG 492) is an orally active and competitive AMPA receptor antagonist with an IC50 of 190 nM. Selurampanel has reasonable blood-brain barrier penetration. Selurampanel can be used for epilepsy research.
  • HY-32345
    Elocalcitol

    BXL-628; Ro-26-9228

    VD/VDR Cancer Inflammation/Immunology
    Elocalcitol (BXL-628) is a selective, orally active vitamin D receptor (VDR) agonist. Elocalcitol shows anti-inflammatory activity. Elocalcitol inhibits growth of prostate cancer cells.
  • HY-B1390B
    Saccharin sodium hydrate

    Bacterial Inflammation/Immunology
    Saccharin sodium hydrate is an orally active, non-caloric artificial sweeteners (NAS). Saccharin sodium hydrate has bacteriostatic and microbiome-modulating properties.
  • HY-N0465
    Olaquindox

    Antibiotic Bacterial Infection
    Olaquindox, a quinoxalin derivative, is an orally active antibiotic. Olaquindox stimulates growth and decreases intestinal mucosal immunity of piglets.
  • HY-Y0272
    Saccharin

    Bacterial Inflammation/Immunology
    Saccharin is an orally active, non-caloric artificial sweeteners (NAS). Saccharin has bacteriostatic and microbiome-modulating properties.
  • HY-B0317
    Amlodipine

    Calcium Channel Cancer Cardiovascular Disease
    Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer.
  • HY-144770
    SARS-CoV-2-IN-13

    SARS-CoV Infection
    SARS-CoV-2-IN-13 (compound 5) is a potent inhibitor of SARS-CoV-2 with an IC50 of 0.057 μM. SARS-CoV-2-IN-13 is a niclosamide analogue. SARS-CoV-2-IN-13 contains higher stability in human plasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally.
  • HY-144771
    SARS-CoV-2-IN-14

    SARS-CoV Infection
    SARS-CoV-2-IN-14 (compound 6) is a potent inhibitor of SARS-CoV-2 with an IC50 of 0.39 μM. SARS-CoV-2-IN-14 is a niclosamide analogue. SARS-CoV-2-IN-14 contains higher stability in human plasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally.
  • HY-144772
    SARS-CoV-2-IN-15

    SARS-CoV Infection
    SARS-CoV-2-IN-15 (compound 11) is a potent inhibitor of SARS-CoV-2 with an IC50 of 0.49 μM. SARS-CoV-2-IN-15 is a niclosamide analogue. SARS-CoV-2-IN-15 contains higher stability in human plasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally.
  • HY-B0265
    Nimodipine

    BAY-e 9736

    Autophagy Calcium Channel Cardiovascular Disease Cancer
    Nimodipine (BAY-e 9736) is an orally active, well-tolerated and light-sensitive dihydropyridine calcium antagonist. Nimodipine can be used for the research of cerebrovascular disorders.
  • HY-143439
    LX-039

    Estrogen Receptor/ERR Cancer
    LX-039 is a highly potent, selective and orally active estrogen receptor degrader with EC50 value of 2.29 nM. LX-039 has indole C-3 chlorine atom. LX-039 exhibits excellent mouse pharmacokinetics, low clearance, high Cmax and oral exposure. LX-039 has anti-tumor activity.
  • HY-137892
    GSK620

    Epigenetic Reader Domain Inflammation/Immunology
    GSK620 is a potent and orally active pan-BD2 inhibitor with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood.
  • HY-124593
    PTC299

    VEGFR Dihydroorotate Dehydrogenase DNA/RNA Synthesis Cancer
    PTC299 is an orally active inhibitor of VEGFA mRNA translation that selectively inhibits VEGF protein synthesis at the post-transcriptional level. PTC299 is also a potent inhibitor of dihydroorotate dehydrogenase (DHODH). PTC299 shows good oral bioavailability and lack of off-target kinase inhibition and myelosuppression. PTC299 can be useful for the research of hematologic malignancies.
  • HY-B0561
    Spironolactone

    SC9420

    Mineralocorticoid Receptor Androgen Receptor Autophagy Metabolic Disease Cancer
    Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes.
  • HY-B0089
    Acarbose

    BAY g 5421

    Glucosidase Metabolic Disease
    Acarbose (BAY g 5421), antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose can potentiate the hypoglycemic effects of sulfonylureas or insulin.
  • HY-143216A
    Ensitrelvir fumarate

    S-217622 fumarate

    SARS-CoV Virus Protease Infection
    Ensitrelvir (S-217622) fumarate is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor (IC50=13 nM).
  • HY-143216
    Ensitrelvir

    S-217622

    SARS-CoV Virus Protease Infection
    Ensitrelvir (S-217622) is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor (IC50=13 nM).
  • HY-144878
    VPC-70619

    c-Myc Cancer
    VPC-70619 is a potent, orally active N-Myc inhibitor. VPC-70619 blocks the N-Myc-Max heterocomplex from binding to DNA E-boxes and demonstrated strong inhibition activity against N-Myc-dependent cell lines as well as high bioavailability in both oral and intraperitoneal administration.
  • HY-138639
    PW0787

    Others Neurological Disease
    PW0787 is a potent, selective, orally active, and brain-penetrant GPR52 agonist (EC50=135 nM). PW0787 suppresses psychostimulant behavior.
  • HY-121565
    SaRI 59-801

    Others Endocrinology Metabolic Disease
    SaRI 59-801 is an orally effective hypoglycemic compound. SaRI 59-801 decreases blood glucose in several species and to elevate plasma insulin in rats and mice.
  • HY-122168
    AAT-008

    Prostaglandin Receptor Inflammation/Immunology
    AAT-008 is a potent, selective, and orally active prostaglandin EP4 receptor antagonist with Kis of 0.97 and 6.1 nM for recombinant human EP4 and recombinant rat EP4, respectively.
  • HY-139784
    Idroxioleic acid

    (R)-2-Hydroxyoleic acid; (R)-2-OHOA

    Others Cancer
    Idroxioleic acid ((R)-2-Hydroxyoleic acid; (R)-2-OHOA), the R enantiomer of (Rac)-Idroxioleic acid, is an orally active fatty acid that modulates the lipid composition and structure of the membranes. Idroxioleic acid has antitumor activities.
  • HY-131973
    PDE10A-IN-2 hydrochloride

    Phosphodiesterase (PDE) Metabolic Disease Cardiovascular Disease
    PDE10A-IN-2 hydrochloride is a potent, highly selective and orally active phosphodiesterase 10A (PDE10A) inhibitor with an IC50 of 2.8 nM. PDE10A-IN-2 hydrochloride shows selectivity of >3500-fold against other PDE subtypes. PDE10A-IN-2 hydrochloride can be used for pulmonary arterial hypertension (PAH) research.
  • HY-141795
    Posovolone

    Co 134444

    Others Neurological Disease
    Posovolone (Co 134444) is an orally active, neuroactive steroid. Posovolone has anticonvulsant and anxiolytic-like activity as well as ataxic effects.
  • HY-B0317B
    Amlodipine besylate

    Amlodipine benzenesulfonate

    Calcium Channel Cancer Cardiovascular Disease
    Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer.
  • HY-W013172
    Norgestimate

    Progesterone Receptor Endocrinology
    Norgestimate, a synthetic progesterone analog, is an orally active progestin with highly selective progestational activity and minimal androgenicity. Norgestimate is used for an oral contraceptive.
  • HY-121341
    Brodimoprim

    Ro 10-5970

    Bacterial Infection
    Brodimoprim (Ro 10-5970), a trimethoprim analogue, is an orally active dihydrofolate reductase inhibitor. Brodimoprim is highly active against a broad spectrum of gram-negative and gram-positive bacteria.
  • HY-12713
    Lisuride

    Dopamine Receptor Neurological Disease
    Lisuride is an orally active dopamine D2 receptors agonist. Lisuride, as an ergot derivative, can be used for the research of Parkinson's disease, migraine, and high prolactin levels.
  • HY-15651A
    Alvelestat tosylate

    AZD9668 tosylate

    Elastase Inflammation/Immunology
    Alvelestat (tosylate) is an orally bioavailable, affinity and selective inhibitor of neutrophil elastase (NE) with a pIC50 value of 7.9 nM, a Ki value of 9.4 nM and a Kd value of 9.5 nM.
  • HY-119104
    AZD1940

    Cannabinoid Receptor Neurological Disease
    AZD1940 is an orally active, high affinity cannabinoid CB1/CB2 receptor agonist with pKi values of 7.93 and 9.06 for human CB1R and CB2R, respectively. AZD1940 shows a robust analgesia action.
  • HY-131336
    MGS0274

    mGluR Neurological Disease
    MGS0274, an ester-based lipophilic prodrug of a metabotropic glutamate (mGlu)2 and mGlu3 receptor agonist MGS0008, shows improved oral bioavailability. MGS0274 has the potential for the research of schizophrenia.
  • HY-108620
    CDP-840

    GR259653X

    Phosphodiesterase (PDE) Inflammation/Immunology
    CDP-840 (GR259653X) is a potent, selective and orally active phosphodiesterase IV (PDE IV) inhibitor. CDP-840 inhibits antigen-induced early and late phase bronchoconstriction in conscious squirrel monkeys.
  • HY-16346
    Netupitant

    CID 6451149

    Neurokinin Receptor Neurological Disease Endocrinology
    Netupitant (CID-6451149) is a highly potent, selective and orally active neurokinin-1 (NK1) receptor antagonist with a Ki of 0.95 nM for hNK1 in CHO cells. Netupitant has antiemetic affect.
  • HY-19522
    Seladelpar

    MBX-8025

    PPAR Metabolic Disease
    Seladelpar (MBX-8025) is an orally active, potent (50% effect concentration EC50 2 nM), and specific PPAR-δ agonist.
  • HY-19687
    Zopolrestat

    CP73850

    Aldose Reductase Metabolic Disease
    Zopolrestat (CP73850) is a potent, orally active aldose reductase (AR) inhibitor with an IC50 of 3.1 nM. Zopolrestat is used for the research of diabetic complications.
  • HY-B0698A
    Ceftibuten dihydrate

    Sch-39720 dihydrate

    Bacterial Antibiotic Infection
    Ceftibuten (Sch39720) dihydrate, an antibiotic, is an orally active cephalosporin, possesses potent activity in vitro against a wide range of gram-negative and certain gram-positive pathogens.
  • HY-137432A
    Avotaciclib trihydrochloride

    BEY1107 trihydrochloride

    CDK Cancer
    Avotaciclib (BEY1107) trihydrochloride is a potent and orally active inhibitor of cyclin dependent kinase 1 (CDK1). Avotaciclib trihydrochloride can be used for the research of locally advanced or metastatic pancreatic cancer.
  • HY-137432
    Avotaciclib

    BEY1107

    CDK Cancer
    Avotaciclib (BEY1107) is a potent and orally active inhibitor of cyclin dependent kinase 1 (CDK1). Avotaciclib can be used for the research of locally advanced or metastatic pancreatic cancer.
  • HY-144303
    Xanthine oxidase-IN-4

    Xanthine Oxidase Metabolic Disease
    Xanthine oxidase-IN-4 (compound 19a) is an orally active and potent xanthine oxidase (XO) inhibitor, with an IC50 of 0.039 μM. Xanthine oxidase-IN-4 exhibits hypouricemic potency in potassium oxonate induced hyperuricemia rats. Xanthine oxidase-IN-4 can be used for hyperuricemia and gout research.
  • HY-10443A
    Balapiravir hydrochloride

    Ro 4588161 hydrochloride; R1626 hydrochloride

    HCV DNA/RNA Synthesis Infection
    Balapiravir hydrochloride (Ro 4588161 hydrochloride; R1626 hydrochloride) is an orally active prodrug of a nucleoside analogue inhibitor of the RNA-dependent RNA polymerase (RdRp) of HCV (R1479; 4'-Azidocytidine). Balapiravir hydrochloride has anti-HCV activity.
  • HY-16747
    Maralixibat chloride

    SHP625 chloride; LUM001 chloride; Lopixibat chloride

    Others Metabolic Disease
    Maralixibat (SHP625) chloride is an orally active ileal bile acid transporter (IBAT) inhibitor. Maralixibat chloride can be used for the treatment of rare cholestatic liver diseases including Alagille syndrome (ALGS), progressive familial intrahepatic cholestasis (PFIC) and biliary atresia.
  • HY-10443
    Balapiravir

    Ro 4588161; R1626

    HCV DNA/RNA Synthesis Infection
    Balapiravir (Ro 4588161; R1626) is an orally active prodrug of a nucleoside analogue inhibitor of the RNA-dependent RNA polymerase (RdRp) of HCV (R1479; 4'-Azidocytidine). Balapiravir has anti-HCV activity.
  • HY-145887
    BCR-ABL1-IN-1

    Others Neurological Disease
    BCR-ABL1-IN-1 is a potent, orally active, and specific inhibitor of ABL kinase. BCR-ABL1-IN-1 has potential for elucidating the role of ABL kinases in the brain in non-clinical studies.
  • HY-13672
    LY2334737

    Nucleoside Antimetabolite/Analog Enterovirus Cancer Infection
    LY2334737 is an nucleoside analog and is an orally active prodrug of Gemcitabine. LY2334737 exhibits inhibitory activity against enterovirus A71 (EV-A71) infection. LY2334737 has antiviral and anticancer effects.
  • HY-131723
    Pregnenolone 16α-carbonitrile

    Cytochrome P450 Metabolic Disease
    Pregnenolone 16α-carbonitrile is an orally active prototypical and effective rodent-PXR activator. Pregnenolone 16α-carbonitrile, a synthetic steroid, induces cytochrome P450 3A expression. Pregnenolone 16α-carbonitrile exhibits increased resistance to subsequent stressful insults.
  • HY-112102
    (22S,23S)-Homobrassinolide

    SSHB

    Others Metabolic Disease
    (22S,23S)-Homobrassinolide is one of the most active brassinosteroids in inducing plant growth in various plant bioassay systems. (22S,23S)-Homobrassinolide shows Akt-dependent anabolic activity in rat skeletal muscle cells. Orally active.
  • HY-143430
    LY3143921

    CDK Cancer
    LY3143921 ((S)-Example 2) is an orally active CDC7 kinase inhibitor. LY3143921 shows broad in vitro anticancer activity.
  • HY-133937
    Sulfametrole

    Bacterial HIV Infection
    Sulfametrole is an orally active and potent antibacterial. Sulfametrole can be used for infections research, such as HIV, severe pneumonia and UTIs (urinary tract infections).
  • HY-132294
    GNE-502

    Estrogen Receptor/ERR Cancer
    GNE-502 is an orally active and potent degrader for estrogen receptor (ER). GNE-502 can be used for the research of breast cancer.
  • HY-143430A
    LY3143921 hydrate

    CDK Cancer
    LY3143921 ((S)-Example 2) hydrate is an orally active CDC7 kinase inhibitor. LY3143921 hydrate shows broad in vitro anticancer activity.
  • HY-145598
    Sovleplenib

    HMPL-523

    Syk Cancer
    Sovleplenib (HMPL-523) is a highly potent, orally available and selective SYK inhibitor with an IC50 of 25 nM. Anti-tumor activity. Sovleplenib can be used for the research of immune thrombocytopenia (ITP).
  • HY-135655
    Fobrepodacin disodium

    SPR720 disodium; pVXc-486 disodium

    Bacterial Infection
    Fobrepodacin (SPR720) disodium is an orally active and potent phosphate prodrug of SPR719 (VXc-486; HY-12930). Fobrepodacin disodium has potent bactericidal activities in vivo.
  • HY-136447
    ASP4132

    AMPK Cancer
    ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models.
  • HY-W133967
    Calcium alginate

    Others Inflammation/Immunology
    Calcium alginate is a biopolymer that can be used for developing oral drug-delivery systems. Calcium alginate is a pH sensitive hydrogel stable in acidic media and soluble in basic media.
  • HY-15454
    Xevinapant

    AT-406; Debio 1143; SM-406

    IAP Cancer
    Xevinapant (AT-406) is a potent and orally bioavailable Smac mimetic and an antagonist of IAPs, and it binds to XIAP, cIAP1, and cIAP2 proteins with Ki of 66.4, 1.9, and 5.1 nM, respectively.
  • HY-105303
    CEP-9722

    PARP Cancer
    CEP-9722, the prodrug of CEP-8983, is a selective and orally active PARP-1 and PARP-2 inhibitor with IC50s of 20 nM and 6 nM, respectively. CEP-9722 has anticancer effects.
  • HY-130628
    PAK4-IN-1

    PAK Cancer
    PAK4-IN-1 (Compound 19) is a potent, selective, orally active PAK4 inhibitor with robust anti-tumor efficacy in vivo. PAK4-IN-1 is stable under both acidic and neutral conditions.
  • HY-N7560
    Safranal

    Others Inflammation/Immunology Neurological Disease
    Safranal is an orally active main component of Saffron (Crocus sativus) and is responsible for the unique aroma of this spice. Safranal has neuroprotective and anti-inflammatory effects and has the potential for Parkinson’s disease research.
  • HY-105124A
    Bufuralol hydrochloride

    Ro 3-4787 hydrochloride

    Adrenergic Receptor Endocrinology Cardiovascular Disease
    Bufuralol hydrochloride (Ro 3-4787 hydrochloride) is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a CYP2D6 probe substrate.
  • HY-105040C
    Pomaglumetad methionil hydrochloride

    LY2140023 hydrochloride

    mGluR Neurological Disease
    Pomaglumetad methionil hydrochloride (LY2140023 hydrochloride) is an orally active, methionine prodrug of the selective mGlu2/3 receptor agonist LY404039. Pomaglumetad methionil hydrochloride has the potential for schizophrenia research.
  • HY-134661A
    CVN424

    Others Neurological Disease
    CVN424 is an orally active and selective GPR6 inverse agonist with a EC50 of 9.4 nM and an EC50 of 38 nM. CVN424 is brain-penetrant and has the potential for Parkinson disease research.
  • HY-139204
    BMS-986242

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    BMS-986242 is an orally active, potent and selective indoleamine-2,3-dioxygenase 1 (IDO1) inhibitor. BMS-986242 can be used for the research of cancer.
  • HY-139399
    JNJ-67856633

    MALT1 Cancer
    JNJ-67856633 is an orally active, first-in-class, potent, selective and allosteric MALT1 protease inhibitor. JNJ-67856633 in some cases lead to tumor stasis.
  • HY-107013
    CP-544439

    MMP Inflammation/Immunology
    CP-544439 is a potent and orally active matrix metalloproteinase-13 (MMP-13) inhibitor with an IC50 of 0.75 nM.
  • HY-119980
    Fluphenazine

    Dopamine Receptor Sodium Channel Neurological Disease
    Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine is used for the research of schizophrenia. Fluphenazine blocks neuronal voltage-gated sodium channels.
  • HY-109189
    Rezivertinib

    BPI-7711

    EGFR Cancer
    Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity.
  • HY-10439
    HPGDS inhibitor 1

    PGE synthase Inflammation/Immunology
    HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX.
  • HY-12661A
    AMG PERK 44

    PERK Autophagy Cancer
    AMG PERK 44 is an orally active and highly selective PERK inhibitor with an IC50 of 6 nM. AMG PERK 44 has 1000-fold and 160-fold selectivity over GCN2 (IC50=7300 nM) and B-Raf (IC50 >1000 nM), respectively. AMG PERK 44 induces autophagy.
  • HY-103706
    ROC-325

    Autophagy Apoptosis Cancer
    ROC-325 is a potent and orally active autophagy inhibitor with a strong anticancer activity. ROC-325 induces the deacidification of lysosomes, accumulation of autophagosomes, and disrupted autophagic flux. ROC-325 also induces renal cell carcinoma apoptosis.
  • HY-147066
    Dyrk1A-IN-4

    DYRK Cancer
    Dyrk1A-IN-4 (compound 48) is a potent and orally active DYRK1A and DYRK2 inhibitor with IC50s of 2 nM and 6 nM, respectively. Dyrk1A-IN-4 has anticancer effects.
  • HY-139590A
    Zeteletinib hemiadipate

    BOS-172738 hemiadipate; DS-5010 hemiadipate

    RET PDGFR Cancer
    Zeteletinib (BOS-172738; DS-5010) hemiadipate is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib hemiadipate shows exquisite potency for the wild type RET, RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib hemiadipate has potent antitumor activity.
  • HY-139590
    Zeteletinib

    BOS-172738; DS-5010

    RET PDGFR Cancer
    Zeteletinib (BOS-172738; DS-5010) is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib shows exquisite potency for the wild type RET, RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib has potent antitumor activity.
  • HY-144606
    Mu opioid receptor antagonist 1

    Opioid Receptor Neurological Disease
    Mu opioid receptor antagonist 1 (compound 19) is a selective and orally active μ opioid receptor (MOR) ligand with an Ki value of 0.58 nM and an EC50 of 1.15 nM. Orally administrating with Mu opioid receptor antagonist 1 increases intestinal motility during morphine-induced constipation. Mu opioid receptor antagonist 1 can be used for researching opioid-induced constipation (OIC).
  • HY-B0592S
    Trandolapril D5

    RU44570 D5

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Trandolapril D5 (RU44570 D5) is a deuterium labeled Trandolapril (RU44570). Trandolapril is an orally active angiotensin converting enzyme (ACE) inhibitor for hypertension and congestive heart failure (CHF).
  • HY-120160
    Darglitazone

    CP-86325

    PPAR Metabolic Disease Neurological Disease
    Darglitazone (CP-86325), a thiazolidinedione, is a potent, selective, and orally active PPAR-γ agonist. Darglitazone is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research.
  • HY-14554
    Pomaglumetad methionil anhydrous

    LY2140023

    mGluR Neurological Disease
    Pomaglumetad methionil anhydrous (LY2140023) is an orally active, methionine prodrug of the selective mGlu2/3 receptor agonist LY404039. LY2140023 has the potential for schizophrenia research.
  • HY-123863
    SSR411298

    FAAH Neurological Disease
    SSR411298 is an orally active, selective and reversible fatty acid amide hydrolase (FAAH) inhibitor. SSR411298 has the potential for post-traumatic stress disorder research.
  • HY-B1271
    Sulfinpyrazone

    G-28315

    Others Inflammation/Immunology
    Sulfinpyrazone (G-28315) is an orally active and potent uricosuric agent for chronic and intermittent gouty arthritis. Sulfinpyrazone has antithrombotic and platelet inhibitory effects.
  • HY-107355
    Letosteine

    Inflammation/Immunology
    Letosteine is an orally active, potent and safe expectorant. Letosteine dissolves bronchial mucus and reduces respiratory inflammation symptoms, and restores gas exchanges and natural defense mechanisms in the lung. Letosteine can be used for acute or chronic respiratory diseases (such as bronchopneumopathies) research.
  • HY-144064
    Adenosine receptor antagonist 2

    Adenosine Receptor Cancer
    Adenosine receptor antagonist 2 is an orally active A2a/A2b adenosine receptor antagonist with IC50s of 1 nM and 3 nM, respectively. Adenosine receptor antagonist 2 has anti-tumor activity.
  • HY-108492
    TC-SP 14

    LPL Receptor Inflammation/Immunology
    TC-SP 14 (compound 14) is an orally active and potent S1P1 agonist (EC50 = 0.042 μM) with minimal activity at S1P3 (EC50 = 3.47 μM). TC-SP 14 significantly reduces blood lymphocyte counts and attenuates a delayed type hypersensitivity (DTH) response to antigen challenge.
  • HY-W013989
    1,3-Dicyclohexylurea

    Epoxide Hydrolase Cardiovascular Disease
    1,3-Dicyclohexylurea (DCU) is an orally active and potent sEH (soluble epoxide hydrolase) inhibitor. Oral Delivery of 1,3-Dicyclohexylurea nanosuspension enhances exposure and lowers blood pressure in hypertensive Rats.
  • HY-141411A
    Zevaquenabant

    (S)-MRI-1867

    Cannabinoid Receptor NO Synthase Metabolic Disease
    Zevaquenabant ((S)-MRI-1867) is a peripherally restricted, orally bioavailable dual cannabinoid CB1 receptor and inducible NOS (iNOS) antagonist. Zevaquenabant ameliorates obesity-induced chronic kidney disease (CKD).
  • HY-12146
    ELOVL6-IN-2

    Others Metabolic Disease
    ELOVL6-IN-2 is a potent, orally active and selective ELOVL6 inhibitor. ELOVL6-IN-2 inhibits mouse ELOVL6 activities, with an IC50 value of 34 nM.
  • HY-106158
    T-1095

    SGLT Metabolic Disease
    T-1095 is a selective and orally active Na +-glucose cotransporter (SGLT) inhibitor with IC50s of 22.8 µM and 2.3 µM for human SGLT1 and SGLT2, respectively. T-1095 can be used for diabetes research.
  • HY-16748
    Nelonicline

    ABT-126

    nAChR Neurological Disease
    Nelonicline (ABT-126) is an orally active and selective α7 nicotinic receptor agonist with high affinity to α7 nAChRs in human brain (Ki=12.3 nM). Nelonicline is used for the research of shizophrenia and Alzheimer's disease.
  • HY-118134
    Hepln-13

    Others Cancer
    Hepln-13 is a potent and orally active Hepsin inhibitor with an IC50 of 0.33 µM. Hepln-13 can be used for the research of metastatic prostate cancer.
  • HY-144300
    TNP-2198

    Bacterial Infection
    TNP-2198 is a potent and orally bioavailable dual-targeted antibacterial agent. TNP-2198 has potent activity against microaerophilic and anaerobic bacterial pathogens.
  • HY-144706
    Axl-IN-3

    TAM Receptor Cancer
    Axl-IN-3 is a potent, selective and orally active AXL kinase inhibitor with an IC50 of 41.5 nM. Axl-IN-3 has lower inhibition of other kinases.
  • HY-131065
    MET kinase-IN-2

    c-Met/HGFR Cancer
    MET kinase-IN-2 is a potent, selective, orally bioavailable MET kinase inhibitor with an IC50 of 7.4 nM. MET kinase-IN-2 has antitumor activity.
  • HY-109027
    Cavosonstat

    N91115

    GSNOR CFTR Inflammation/Immunology
    Cavosonstat (N91115) is an orally active S-nitrosoglutathione reductase (GSNOR) inhibitor. Cavosonstat is a CFTR stabilizer, and can be used for cystic fibrosis research.
  • HY-107703
    CGP 39551

    iGluR Neurological Disease
    CGP 39551 is a potent, orally active, competitive N-methyl-D-aspartate (NMDA) receptor antagonist with potent anticonvulsant activity. CGP 39551 shows measurable inhibitory activity at both L-[ 3H]-glutamate (Ki=8.4 μM).
  • HY-19672
    Lirimilast

    BAY 19-8004

    Phosphodiesterase (PDE) Inflammation/Immunology
    Lirimilast (BAY 19-8004) is a potent, selective and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 value of 49 nM. Lirimilast can be used for the treatment of asthma or chronic obstructive pulmonary disease (COPD). Lirimilast has potently anti-inflammatory properties.
  • HY-144870
    STAT3-IN-7

    STAT Cancer
    STAT3-IN-7, an aryl sulfonamido azetidine compound, is an orally active STAT3 inhibitor. STAT3-IN-7 has anticancer activities (WO2021016333A1, H182).
  • HY-135891
    AZD2423

    CCR Neurological Disease
    AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC50 of 1.2 nM for CCR2 Ca 2+ flux .
  • HY-115936
    COX-2-IN-9

    COX Inflammation/Immunology
    COX-2-IN-9 (compound 7a) is a potent, selective, and orally active inhibitor of COX-2 with an IC50 of 10.17 uM. COX-2-IN-9 has higher COX-2 selectivity than Celecoxib. COX-2-IN-9 shows good in vivo anti-inflammatory and low ulcerogenic activity.
  • HY-115934
    COX-2-IN-7

    COX Inflammation/Immunology
    COX-2-IN-7 (compound 4a) is a potent, selective, and orally active inhibitor of COX-2 with an IC50 of 6.585 uM. COX-2-IN-7 has higher COX-2 selectivity than Celecoxib. COX-2-IN-7 shows good in vivo anti-inflammatory and low ulcerogenic activity.
  • HY-117833
    PXS-4681A

    Monoamine Oxidase Inflammation/Immunology
    PXS-4681A is a potent, selective, irreversible and orally active semicarbazide-sensitive amine oxidase (SSAO; VAP-1) inhibitor with a Ki of 37 nM. PXS-4681A shows highly selectivity over related amine oxidases, ion channels, and seven-transmembrane domain receptors. PXS-4681A has anti-inflammatory effects.
  • HY-115935
    COX-2-IN-8

    COX Inflammation/Immunology
    COX-2-IN-8 (compound 6a) is a potent, selective, and orally active inhibitor of COX-2 with an IC50 of 6.585 uM. COX-2-IN-8 has higher COX-2 selectivity than Celecoxib. COX-2-IN-8 shows good in vivo anti-inflammatory and low ulcerogenic activity.
  • HY-109144
    Enavogliflozin

    DWP-16001

    SGLT Metabolic Disease
    Enavogliflozin (DWP-16001), an antidiabetic agent, is an orally active, best-in-class and selective sodium-glucose cotransporter-2 (SGLT-2) inhibitor.
  • HY-16748A
    Nelonicline citrate

    ABT-126 citrate

    nAChR Neurological Disease
    Nelonicline (ABT-126) citrate is an orally active and selective α7 nicotinic receptor agonist with high affinity to α7 nAChRs in human brain (Ki=12.3 nM). Nelonicline citrate is used for the research of shizophrenia and Alzheimer's disease.
  • HY-B0024
    Prulifloxacin

    NM441

    Bacterial Antibiotic Infection
    Prulifloxacin (NM441) is an orally active fluoroquinolone antibiotic with a broad spectrum of activity against Gram-positive and -negative bacteria. Prulifloxacin is a prodrug of a thiazeto-quinoline carboxylic acid derivative Ulifloxacin (NM394). Prulifloxacin has the potential for lower urinary tract infections and exacerbations of chronic bronchitis.
  • HY-118189
    Misoprostol acid

    Prostaglandin Receptor Inflammation/Immunology
    Misoprostol acid is an active metabolite of Misoprostol. Misoprostol is a synthetic analogue of prostaglandin E1 (PGE1), extensively absorbed, and undergoes rapid de-esterification to Misoprostol acid in the gastrointestinal tract after oral administration. Misoprostol can be used for non-steroidal anti-inflammatory drug-induced (NSAID) gastric ulcers. Misoprostol is an oral agent used to induce labor.
  • HY-138564
    NOS-IN-1

    NO Synthase Inflammation/Immunology
    NOS-IN-1 is a potent and orally active NO synthase (NOS) isoforms inhibitor with IC50s of 0.1 μM, 1.1 μM, and 0.2 μM for human iNOS (hiNOS), heNOS and hnNOS, respectively.
  • HY-A0213
    Tiludronate

    Tiludronic acid

    Proton Pump Inflammation/Immunology
    Tiludronate (Tiludronic Acid), an orally active bisphosphonate, can act an osteoregulator. Tiludronate is used for the research of the metabolic bone disorders. Tiludronate is a potent inhibitor of the osteoclast vacuolar H(+)-ATPase. Antiresorptive and anti-inflammatory properties.
  • HY-W027951
    N,N'-Dimethylthiourea

    DMTU

    Others Inflammation/Immunology
    N,N'-Dimethylthiourea (DMTU), isolated from Allii Sativi Bulbus, is an orally active scavenger of hydroxyl radical (•OH) and blocks •OH production by activated neutrophils in vitro. N,N'-Dimethylthiourea protects against water-immersion restraint stress (WIRS)-induced gastric mucosal lesions in rats by exerting its antioxidant action including •OH scavenging and anti-inflammatory action.
  • HY-112094S
    WNK-IN-11-d3

    Ser/Thr Protease Cardiovascular Disease
    WNK-IN-11 D3 is an orally active, selective and potent With-No-Lysine (WNK) kinase inhibitor. WNK-IN-11 D3 is effective at regulating cardiovascular homeostasis.
  • HY-145653
    GSK2647544

    Phospholipase Inflammation/Immunology Neurological Disease Cardiovascular Disease
    GSK2647544 is an orally available, selective inhibitor of Lp-PLA2. Lipoprotein-associated phospholipase (Lp-PLA2) is a calcium-independent phospholipase A2 with proinflammatory activities that is primarily secreted by monocyte-derived macrophages.
  • HY-113926
    BAY 60-2770

    Guanylate Cyclase Cardiovascular Disease
    BAY 60-2770 is a potent, selective, and orally active soluble guanylyl cyclase (sGC) activator. BAY 60-2770 increases the activity of sGC in a nitric oxide-independent manner. BAY 60-2770 shows antifibrotic effect.
  • HY-16759
    Verubecestat

    MK-8931

    Beta-secretase Neurological Disease
    Verubecestat (MK-8931) is an orally active, high-affinity BACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM. Verubecestat effectively reduces Aβ40 and has the potential for Alzheimer's Disease.
  • HY-A0213A
    Tiludronate disodium

    Tiludronic acid disodium

    Proton Pump Inflammation/Immunology
    Tiludronate (Tiludronic Acid) disodium, an orally active bisphosphonate, can act an osteoregulator. Tiludronate is used for the research of the metabolic bone disorders. Tiludronate is a potent inhibitor of the osteoclast vacuolar H(+)-ATPase. Antiresorptive and anti-inflammatory properties.
  • HY-107923
    Sulfisoxazole acetyl

    N1-Acetylsulfisoxazole

    Bacterial Infection
    Sulfisoxazole acetyl (N1-Acetylsulfisoxazole), a Sulfisoxazole derivative, is an orally active dihydropteroate synthase inhibitor. Sulfisoxazole acetyl has an antibacterial action.
  • HY-115989
    HCV-IN-38

    HCV Infection
    HCV-IN-38 is a potent, selective and orally active HCV inhibitor (EC50=15 nM, SI=431). HCV-IN-38 has high anti-HCV activity and low cytotoxicity. HCV-IN-38 has a good safety and oral pharmacokinetic profile.
  • HY-131349
    CCR4 antagonist 3

    CCR Cancer
    CCR4 antagonist 3 is an orally active, potent and selective CCR4 antagonist. CCR4 antagonist 3, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4 antagonist 3 has antitumor activity.
  • HY-131349A
    CCR4 antagonist 3 hydrochloride

    CCR Cancer Metabolic Disease
    CCR4 antagonist 3 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4 antagonist 3, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4 antagonist 3 has antitumor activity.
  • HY-139970
    VPC-13789

    Androgen Receptor Cancer Endocrinology
    VPC-13789 is a potent, selective, and orally bioavailable antiandrogen. VPC-13789 can be used for the research of castration-resistant prostate cancer (CRPC) therapeutics. VPC-13789 inhibits androgen receptor (AR) transcriptional activity in LNCaP cells (IC50=0.19 μM).
  • HY-115923
    Nur77 modulator 2

    Others Inflammation/Immunology
    Nur77 modulator 2, a Nur77 modulator (Kd of 0.35 μM), is a potent and orally active inflammation inhibitor. Nur77 modulator 2 modulates the colocalization of Nur77 at mitochondria.
  • HY-144444
    NSC381467

    EGFR Cancer
    NSC381467 is a potent and orally active inhibitor of EGFR tyrosine kinase (EGFR-TK). NSC381467 has strong antiproliferative activities. NSC381467 has the potential for the research of cancer diseases.
  • HY-144445
    NSC114126

    EGFR Cancer
    NSC114126 is a potent and orally active inhibitor of EGFR tyrosine kinase (EGFR-TK). NSC114126 has strong antiproliferative activities. NSC114126 has the potential for the research of cancer diseases.
  • HY-19926
    GDC-0425

    RG-7602

    Checkpoint Kinase (Chk) Cancer
    GDC-0425 (RG-7602) is an orally available, highly selective small molecule ChK1 inhibitor. GDC-0425 can be used for the research of various malignancies.
  • HY-145574
    Iruplinalkib

    WX-0593

    ALK ROS Cancer
    Iruplinalkib (WX-0593) is a potent, selective, and orally active inhibitor of ALK and ROS1 tyrosine kinase. Iruplinalkib (WX-0593) shows favorable safety and promising antitumor activity in advanced NSCLC with ALK or ROS1 rearrangement.
  • HY-120438
    TASP0415914

    PI3K Akt Inflammation/Immunology
    TASP0415914 is a potent and orally active PI3Kγ inhibitor with an IC50 of 29 nM. TASP0415914 also shows potent Akt inhibitory activities with an IC50 of 294 nM. TASP0415914 can be used for inflammatory diseases research.
  • HY-107725
    BIBO3304 TFA

    Neuropeptide Y Receptor Metabolic Disease
    BIBO3304 TFA is a potent, orally active, and selective neuropeptide Y (NPY) Y1 receptor antagonist, with subnanomolar affinity for both the human and the rat Y1 receptor (IC50=0.38 and 0.72 nM, respectively).
  • HY-11059
    sPLA2 inhibitor 1

    Phospholipase Inflammation/Immunology
    sPLA2 inhibitor 1, a D-tyrosine derivative, is an orally active, potent secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 29 nM for human nonpancreatic secretory PLA2 isoform IIa (hnpsPLA2-IIa). sPLA2 inhibitor 1 has anti-inflammatory activity.
  • HY-15010
    L-371,257

    Oxytocin Receptor Vasopressin Receptor Endocrinology
    L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (Ki=19 nM) and vasopressin V1a receptor (Ki=3.7 nM).
  • HY-11091
    Razaxaban hydrochloride

    BMS 561389 hydrochloride; DPC 906 hydrochloride

    Factor Xa Thrombin Cardiovascular Disease
    Razaxaban hydrochloride (BMS 561389 hydrochloride) is a highly potent, selective and orally active factor Xa inhibitor with a Ki of 0.19 nM. Razaxaban hydrochloride exhibits excellent selectivity (>5000-fold) for factor Xa over other related serine proteases. Razaxaban hydrochloride is also a potent thrombin inhibitor with a Ki of 540 nM. Razaxaban hydrochloride has strongly antithrombotic activity.
  • HY-B0232
    Dofetilide

    UK 68789

    Potassium Channel Cardiovascular Disease
    Dofetilide (UK 68789), as a class III antiarrhythmic agent, is an orally active, potent and specific IKr blocker. Dofetilide can be used for the research of cardiovascular disease.
  • HY-100888
    Simurosertib

    TAK-931

    CDK Cancer
    Simurosertib (TAK-931) is an orally active, selective and ATP-competitive cell division cycle 7 (CDC7) kinase inhibitor, with an IC50 of <0.3 nM. Simurosertib has anti-cancer activity.
  • HY-B0758
    Troxipide

    Others Inflammation/Immunology
    Troxipide is an orally active defensive factor-enhancing therapeutic agent for gastritis and gastric ulcer (GU). Troxipide is a non-antisecretory gastro protective agent with antiulcer, anti-inflammatory and mucus-secreting properties.
  • HY-14691
    Refametinib

    BAY 869766; RDEA119

    MEK Cancer
    Refametinib (BAY 869766; RDEA119) is an orally available, potent, non-ATP-competitive, selective, allosteric MEK1/MEK2 inhibitor with IC50s of 19 nM and 47 nM, respectively.
  • HY-132293
    BAY-8400

    DNA-PK Cancer
    BAY-8400 is an orally active, potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (IC50=81 nM). BAY-8400 can be used for the research of cancer.
  • HY-A0213B
    Tiludronate disodium hemihydrate

    Tiludronic acid disodium hemihydrate

    Proton Pump Metabolic Disease
    Tiludronate (Tiludronic Acid) disodium hemihydrate, an orally active bisphosphonate, can act an osteoregulator. Tiludronate disodium hemihydrate is used for the research of the metabolic bone disorders. Tiludronate disodium hemihydrate is a potent inhibitor of the osteoclast vacuolar H +-ATPase. Antiresorptive and anti-inflammatory properties.
  • HY-102057
    Felcisetrag

    TD-8954

    5-HT Receptor Others
    Felcisetrag (TD-8954) is an orally active, potent and selective 5-HT4 receptor agonist with gastrointestinal prokinetic properties. Felcisetrag has high affinity (pKi =9.4) for human 5-HT4(c) receptors.
  • HY-123058
    Vps34-IN-4

    PI3K Autophagy Cancer
    Vps34-IN-4 (compound 19) is a potent, selective, and orally active inhibitor of VPS34. Vps34-IN-4 inhibits the autophagy in vivo. Autophagy is a dynamic process that regulates lysosomal-dependent degradation of cellular components.
  • HY-103226
    SC-57461A

    Aminopeptidase Inflammation/Immunology
    SC-57461A is a potent, orally active, nonpeptide, and selective inhibitor of Leukotriene A4 (LTA4) hydrolase with IC50s of 2.5 nM, 3 nM, and 23 nM for recombinant human, mouse, and rat LTA4 hydrolase, respectively.
  • HY-145924
    BAY 2666605

    Phosphodiesterase (PDE) Cancer
    BAY 2666605 is an orally active PDE3A and PDE3B inhibitor with IC50s of 87 nM and 50 nM, respectively. BAY 2666605 is a PDE3A-SLFN12 complex inducer (WO2019025562A1; example 135).
  • HY-115922
    Anti-inflammatory agent 10

    COX Inflammation/Immunology
    Anti-inflammatory agent 10 (compound 30) is a tilomisole-based benzimidazothiazole derivative. Anti-inflammatory agent 10 expresses activity on COX-2 enzyme more than COX-1. Anti-inflammatory agent 10 is orally active.
  • HY-115921
    Anti-inflammatory agent 9

    COX Inflammation/Immunology
    Anti-inflammatory agent 9 (compound 28) is a tilomisole-based benzimidazothiazole derivative. Anti-inflammatory agent 9 expresses activity on COX-2 enzyme more than COX-1. Anti-inflammatory agent 9 is orally active.
  • HY-133127
    AR453588

    Glucokinase Metabolic Disease
    AR453588 is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 shows anti-hyperglycemic activity.
  • HY-133127A
    AR453588 hydrochloride

    Glucokinase Metabolic Disease
    AR453588 hydrochloride is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 hydrochloride shows anti-hyperglycemic activity.
  • HY-109149
    Lomardexamfetamine

    KP 106

    Others Neurological Disease
    Lomardexamfetamine (KP 106) is an orally active central nervous system stimulant composed of d-amphetamine and a ligand. Lomardexamfetamine can be used for the research of attention-deficit hyperactivity disorder.
  • HY-107722
    SCH 221510

    Opioid Receptor Neurological Disease
    SCH 221510 is a potent, orally active and selective NOP (nociceptin opioid receptor) agonist, with an EC50 of 12 nM and Ki of 0.3 nM. SCH 221510 shows an anxiolytic-like effect.
  • HY-14771A
    Imeglimin hydrochloride

    EMD 387008 hydrochloride

    Mitochondrial Metabolism Reactive Oxygen Species Metabolic Disease
    Imeglimin hydrochloride (EMD 387008) is an oral glucose-lowering agent. Imeglimin also reduces reactive oxygen species (ROS) production, increases mitochondrial DNA and improves mitochondrial function.
  • HY-106968
    ZD-9379

    iGluR Neurological Disease
    ZD-9379 is a potent, orally active, and brain penetrant full antagonist at the glycine site of the NMDA receptor. ZD-9379 has neuroprotective effect.
  • HY-123812
    PF-03654764

    Histamine Receptor Inflammation/Immunology Neurological Disease
    PF-03654764 is an orally active, selective histamine H3 receptor antagonist with Ki values of 1.2 nM and 7.9 nM for human H3 and rat H3 in whole cell assay, respectively. The combination of PF-03654764 and Fexofenadine (HY-B0801A) has the potential for allergic rhinitis research.
  • HY-132987
    ARX-1796

    AV-006

    Bacterial Infection
    ARX-1796 (AV-006), an Avibactam prodrug, is an orally bioavailable β-lactamase inhibitor. Avibactam has a spectrum of inhibition of class A and C β-lactamases, including ESBLs, AmpC and Klebsiella pneumoniae carbapenemase (KPC) enzymes.
  • HY-B1526
    Thiacetazone

    Thioacetazone; Amithiozone

    Bacterial Antibiotic Infection
    Thiacetazone (Thioacetazone) is a thiourea-containing antitubercular agent and is an orally active antibiotic. Thiacetazone has antibacterial action, which inhibits growth of Mycobacterium tuberculosis H37Rv with a MIC value of 0.1 μg/mL.
  • HY-146615
    Axl-IN-6

    TAM Receptor Cancer
    Axl-IN-6 (compound 14) is an orally active and potent AXL inhibitor. Axl-IN-6 is well tolerated and significantly inhibits the tumor growth in MV-4-11 subcutaneous xenograft model.
  • HY-133141
    DI-87

    Others Cancer
    DI-87 is an orally active and selective deoxycytidine kinase (dCK) inhibitor with an EC50 of 10.2 nM. DI-87 has antitumor activity and is used in combination therapy against tumors expressing dCK.
  • HY-136977
    EEDi-5285

    Histone Methyltransferase Cancer
    EEDi-5285 is an exceptionally potent and orally active embryonic ectoderm development (EED) inhibitor with an IC50 value of 0.2 nM for binds to the EED protein. EEDi-5285 has anti-cancer activity.
  • HY-138684
    MRTX9768

    Histone Methyltransferase Cancer
    MRTX9768 is a potent, selective, orally active, first-in-class PRMT5-MTA complex inhibitor.
  • HY-138684A
    MRTX9768 hydrochloride

    Histone Methyltransferase Cancer
    MRTX9768 hydrochloride is a potent, selective, orally active, first-in-class PRMT5-MTA complex inhibitor.
  • HY-B0281A
    Ranitidine hydrochloride

    Histamine Receptor Cytochrome P450 Bacterial Infection Endocrinology Metabolic Disease
    Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion. Ranitidine hydrochloride is a weak inhibitor of CYP2C19 and CYP2C9.
  • HY-14900
    Tedalinab

    GRC-10693

    Cannabinoid Receptor Inflammation/Immunology
    Tedalinab (GRC-10693) is a potent, orally active, and selective cannabinoid receptor 2 (CB2) agonist. Tedalinab has >4700-fold functional selectivity for CB2 over CB1. Tedalinab has potential for neuropathic pain and osteoarthritis treatment.
  • HY-19631B
    Ilginatinib hydrochloride

    NS-018 hydrochloride

    JAK Cancer
    Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
  • HY-19631A
    Ilginatinib

    NS-018

    JAK Cancer
    Ilginatinib (NS-018) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
  • HY-122856
    AZ12601011

    TGF-β Receptor Cancer
    AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth .
  • HY-103266
    TC-A 2317 hydrochloride

    Aurora Kinase Cancer
    TC-A 2317 hydrochloride is an orally active Aurora A kinase inhibitor (Ki=1.2 nM). TC-A 2317 hydrochloride exhibits excellent selectivity to Aurora B kinase (Ki=101 nM) and other 60 kinases, good cell permeability and good PK profile. Antitumor activity.
  • HY-14853
    Darexaban

    YM150

    Factor Xa Ser/Thr Protease Cardiovascular Disease
    Darexaban (YM150) is a potent, selective and orally active factor Xa (FXa) inhibitor with an IC50 of 54.6 nM. Darexaban shows high selectivity against other related serine proteases, such as trypsin, thrombin, and kallikrein. Darexaban has anticoagulant and antithrombotic effects.
  • HY-19631
    Ilginatinib maleate

    NS-018 maleate

    JAK Cancer
    Ilginatinib maleate (NS-018 maleate) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
  • HY-141513
    NH-3

    Thyroid Hormone Receptor Neurological Disease
    NH-3 is an orally active, reversible thyroid hormone receptor (THR) antagonist with an IC50 of 55 nM. NH-3, a derivative of the selective thyromi-metic GC-1, inhibits binding of thyroid hormones to their receptor and that inhibits cofactor recruitment.
  • HY-B0693
    Ranitidine

    Histamine Receptor Bacterial Cytochrome P450 Infection Endocrinology Metabolic Disease
    Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion. Ranitidine is a weak inhibitor of CYP2C19 and CYP2C9.
  • HY-132297
    PARP1-IN-5

    PARP Cancer
    PARP1-IN-5 is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 can be used for the research of cancer.
  • HY-132297A
    PARP1-IN-5 dihydrochloride

    PARP Cancer
    PARP1-IN-5 dihydrochloride is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer.
  • HY-10716A
    PF-03463275

    GlyT Neurological Disease
    PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research.
  • HY-100641
    4-Hydroxytolbutamide

    Hydroxytolbutamide

    Potassium Channel Autophagy Cancer Metabolic Disease
    4-Hydroxytolbutamide (Hydroxytolbutamide) is a metabolite of Tolbutamide. 4-Hydroxytolbutamide is metabolized by CYP2C8 and CYP2C9. Tolbutamide is a first generation potassium channel blocker and a sulfonylurea oral antidiabetic.
  • HY-13611
    Diflomotecan

    BN 80915

    Topoisomerase Cancer
    Diflomotecan (BN 80915) is a potent and orally active inhibitor of topoisomerase I. Diflomotecan (BN 80915) causes enhanced plasma stability and has the superior preclinical anti-tumour activity compared with other established compounds.
  • HY-106608
    Glutaurine

    LitOralon

    Thyroid Hormone Receptor Neurological Disease
    Glutaurine containing glutamine and taurine residues is an orally active hormone of the parathyroid. Glutaurine, as a hormone, is isolated from parathyroid gland oxyphil cells. Glutaurine can be used for the research of antiepileptic and anti-amnesia.
  • HY-119816
    Piretanide

    Others Cardiovascular Disease
    Piretanide is an oral active, relatively safe and effective diuretic. Piretanide has the potential for the research of congestive heart failure with a potential advantage of having potassium-sparing properties. Piretanide can also be used for the research of hypertension[1][2].
  • HY-126248
    Tankyrase-IN-2

    PARP Cancer
    Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model.
  • HY-14904A
    Umifenovir hydrochloride

    Influenza Virus SARS-CoV Infection
    Umifenovir hydrochloride is a potent, orally active broad-spectrum antiviral with activity against a number of enveloped and non-enveloped viruses. Umifenovir hydrochloride is used as an anti-influenza virus agent. Umifenovir hydrochloride could effectively inhibit the fusion of virus with host cells. Umifenovir hydrochloride is an efficient inhibitor of SARS-CoV-2 in vitro. Anti-inflammatory activity.
  • HY-122058A
    KRH-3955 hydrochloride

    CXCR HIV Infection Inflammation/Immunology
    KRH-3955 hydrochloride is an orally bioavailable CXCR4 antagonist. KRH-3955 hydrochloride inhibits SDF-1α binding to CXCR4 with an IC50 of 0.61 nM. KRH-3955 hydrochloride is also a highly potent and selective inhibitor of X4 HIV-1, with an EC50 of 0.3 to 1.0 nM.
  • HY-110129
    Eplivanserin hemifumarate

    SR-46349 hemifumarate; SR 46349B

    5-HT Receptor Neurological Disease
    Eplivanserin (SR-46349) hemifumarate is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin hemifumarate displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C.
  • HY-10792
    Eplivanserin

    SR-46349

    5-HT Receptor Neurological Disease
    Eplivanserin (SR-46349) is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C.
  • HY-108024A
    Ganaplacide hydrochloride

    KAF156 hydrochloride; GNF156 hydrochloride

    Parasite Infection
    Ganaplacide (KAF156) hydrochloride is a first-in-class, orally active imidazolopiperazine antimalarial agent. Ganaplacide hydrochloride is active against a broad range of Plasmodium species, including drug-resistant parasites. Ganaplacide hydrochloride is parasiticidal against both asexual and sexual blood stages as well as the liver stages of the parasite.
  • HY-115920
    Anti-inflammatory agent 8

    COX Inflammation/Immunology
    Anti-inflammatory agent 8 (compound 13) is a tilomisole-based benzimidazothiazole derivative. Anti-inflammatory agent 8 expresses activity on COX-2 enzyme more than COX-1 with an IC50 of 0.09 nM. Anti-inflammatory agent 8 is orally active.
  • HY-139485
    BMS-986224

    HIV Cardiovascular Disease
    BMS-986224 is a potent, selective and orally bioavailable APJ receptor agonist (Kd = 0.3 nM). BMS-986224 exhibits similar receptor binding and signaling profile to (Pyr 1) apelin-13. BMS-986224 has the potential for the research of heart failure.
  • HY-135825
    TFEB activator 1

    Autophagy Neurological Disease
    TFEB activator 1 is an orally effective, mTOR-independent activator of TFEB. TFEB activator 1 significantly promotes the nuclear translocation of Flag-TFEB with an EC50 of 2167 nM. TFEB activator 1 enhances autophagy without inhibiting the mTOR pathway and has the potential for neurodegenerative diseases treatment.
  • HY-147642
    ChemR23-IN-4

    Others Inflammation/Immunology
    ChemR23-IN-4 (Compound 13) is a potent and orally efficacious ChemR23 inhibitor with an IC50 of 17 nM against human ChemR23.
  • HY-139300
    Epitinib

    HMPL-813

    EGFR Cancer
    Epitinib is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib can be used for the research of cancer.
  • HY-146267
    ERα degrader 5

    Estrogen Receptor/ERR Cancer
    ERα degrader 5 (Compound 40) is a selective, orally bioavailable estrogen receptor (ER) degrader (SERD) with an EC50 of 1.1 nM against ERα. ERα degrader 5 shows antitumor effect in vivo.
  • HY-N2059
    Santalol

    Others Cancer
    Santalol is a mixture of α and β-isomer santalol. α-santalol is isolated from sandalwood oil. α-santalol is a promising anti-cancer agent against cancers such as oral, breast, prostate and skin cancer.
  • HY-106050
    Tilomisole

    Wy 18251

    Others Cancer Inflammation/Immunology
    Tilomisole (Wy 18251) is a benzimidazothiazole experimental drug with anti-inflammatory activity. Tilomisole causes less agranulocytosis than levamisole, but retains immunomodulating capabilities. Tilomisole is orally active. Tilomisole has the potential for the research of cancer and inflammation.
  • HY-132817
    Gunagratinib

    ICP-192

    FGFR Cancer
    Gunagratinib (ICP-192) is a low toxicity and orally active pan-FGFR (fibroblast growth factor receptors) inhibitor that potently and selectively inhibits FGFR activities irreversibly by covalent binding. Gunagratinib can be used for the research of cancer.
  • HY-111145
    RD162

    Androgen Receptor Cancer
    RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer.
  • HY-147567
    ATR-IN-15

    ATM/ATR DNA-PK PI3K Cancer
    ATR-IN-15 (compound 1) is an orally active and potent ATR kinase inhibitor, with an IC50 of 8 nM. ATR-IN-15 also inhibits human colon tumor cells LoVo, DNA-PK and PI3K, with IC50 values of 47, 663 and 5131 nM, respectively.
  • HY-146662
    HPGDS inhibitor 3

    PGE synthase Inflammation/Immunology
    HPGDS inhibitor 3 is an orally active and highly potent peripherally restricted hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with IC50 value of 9.4 nM and EC50 of 42 nM, respectively. HPGDS inhibitor 3 exhibits good selectivity, good pharmacokinetic parameters in mouse, rat, and dog, and no CNS toxicity. HPGDS inhibitor 3 has anti-inflammatory activity.
  • HY-110117
    BIRT 377

    Integrin Interleukin Related Inflammation/Immunology
    BIRT 377 is a potent amd orally bioavailable inhibitor of the interaction between intercellular adhesion molecule-1 (ICAM-1) and lymphocyte function-associated antigen-1 (LFA-1), with a Ki of 25.8 nM. BIRT 377 also inhibits the production of IL-2 in vivo. BIRT 377 can be used for researching inflammatory and immune disorders.
  • HY-105286
    BI-135585

    Others Metabolic Disease
    BI-135585 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor with an IC50 of 13 nM. BI-135585 exhibits >1000-fold selectivity over other hydroxysteroid dehydrogenases. BI-135585 can be used for type 2 diabetes research.
  • HY-125415
    PF-4693627

    PGE synthase Inflammation/Immunology
    PF-4693627 is a potent, selective and orally bioavailable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor (IC50=3 nM) for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA).
  • HY-134885
    RMC-0331

    RM-023

    Ras Cancer
    RMC-0331 (RM-023) is a potent, selective and orally bioavailable SOS1 inhibitor. RMC-0331 is an in vivo tool compound that blocks RAS activation via disruption of the RAS-SOS1 interaction.
  • HY-W010144
    Phenidone

    COX Lipoxygenase Inflammation/Immunology Cardiovascular Disease
    Phenidone, an orally active dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), ameliorates rat paralysis in experimental autoimmune encephalomyelitis. Phenidone is a potent hypotensive agent in the spontaneously hypertensive rat. Phenidone is used as a photographic developer.
  • HY-19263
    BMS-193884

    Endothelin Receptor Cardiovascular Disease
    BMS-193884 is a selective, orally active, and competitive ETA antagonist with 10000-fold greater affinity for the human ETA receptor (Ki=1.4 nM) than for the ETB receptor.
  • HY-10527C
    Telatinib mesylate

    Bay 57-9352 mesylate

    VEGFR PDGFR c-Kit Cancer
    Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active VEGFR2, VEGFR3, PDGFα, and c-Kit inhibitor with IC50s of 6 nM, 4 nM, 15 nM and 1 nM, respectively.
  • HY-10309
    Sibrafiban

    RO 48-3657

    Integrin Cardiovascular Disease
    Sibrafiban (RO 48-3657) is the orally active, nonpeptide, double-prodrug of Ro 44-3888 and a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban inhibits platelet aggregation.
  • HY-107798
    Potassium guaiacolsulfonate hemihydrate

    Bacterial Infection
    Potassium guaiacolsulfonate hemihydrate is an orally active expectorant used for acute respiratory tract infections. Potassium guaiacolsulfonate hemihydrate helps loosen mucus and used for a cough caused by the common cold, infections or allergies in combination with other drugs.
  • HY-10262
    BMS-536924

    IGF-1R Insulin Receptor Apoptosis Cancer Endocrinology
    BMS-536924 is an orally active, competitive and selective insulin-like growth factor receptor (IGF-1R) kinase and insulin receptor (IR) inhibitor with IC50s of 100 nM and 73 nM, respectively. BMS-536924 has anti-cancer activity.
  • HY-103250
    PF-945863

    Antibiotic Infection
    PF-945863 is an orally active macrolide antibiotic that can be used for the research of multidrug resistant respiratory tract bacterial strains.
  • HY-101918
    DS-1040 Tosylate

    Others Cardiovascular Disease
    DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
  • HY-108060A
    Valopicitabine dihydrochloride

    NM283 dihydrochloride

    HCV HCV Protease Nucleoside Antimetabolite/Analog Infection
    Valopicitabine (NM283) dihydrochloride is a nucleoside analog and the orally bioavailable prodrug of the potent anti-HCV agent 2'-C-methylcytidine (NM107). NM107competitively inhibits NS5B polymerase, causing chain termination.
  • HY-141700
    FATP1-IN-2

    Others Metabolic Disease
    FATP1-IN-2, as an arylpiperazine derivative, is an orally active fatty acid transport protein 1 (FATP1) inhibitor (human IC50=0.43 μM, mouse IC50=0.39 μM).
  • HY-108060
    Valopicitabine

    NM283

    HCV HCV Protease Nucleoside Antimetabolite/Analog Infection
    Valopicitabine (NM283) is a nucleoside analog and the orally bioavailable prodrug of the potent anti-HCV agent 2'-C-methylcytidine (NM107). NM107competitively inhibits NS5B polymerase, causing chain termination.
  • HY-105033
    Irloxacin

    Pirfloxacin

    Bacterial Infection
    Irloxacin (Pirfloxacin) is a quinolone antibacterial agent. Irloxacin shows greater activity with an acid pH. Irloxacin has a good in vitro antimicrobial spectrum against both gram-positive and gram-negative bacteria. Orally active.
  • HY-139300A
    Epitinib succinate

    HMPL-813 succinate

    EGFR Cancer
    Epitinib succinate is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib succinate can be used for the research of cancer.
  • HY-14771
    Imeglimin

    EMD 387008

    Mitochondrial Metabolism Reactive Oxygen Species Metabolic Disease
    Imeglimin (EMD 387008) is an oral glucose-lowering agent. Imeglimin improves insulin sensitivity. Imeglimin also reduces reactive oxygen species (ROS) production, increases mitochondrial DNA and improves mitochondrial function.
  • HY-16950
    4-Hydroxytamoxifen

    (Z)-4-Hydroxytamoxifen; trans-4-Hydroxytamoxifen; (Z)-Afimoxifene

    Estrogen Receptor/ERR Cancer
    4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) is an orally active, selective estrogen receptor modulator (SERM). 4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) induces CRISPR/Cas9 systems based on ER mediated nucleus translocation.
  • HY-15658
    GSK2801

    Epigenetic Reader Domain Apoptosis Cancer
    GSK2801 is a potent, selective, orally active and cell active acetyl-lysine competitive BAZ2A and BAZ2B bromodomains inhibitor with Kd values of 136 nM and 257 nM, respectively. GSK2801 shows >50-fold selectivity for BAZ2A/B over BRD4.
  • HY-132981
    Lu AF27139

    P2X Receptor Neurological Disease
    Lu AF27139 is a potent, selective, and orally active antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 has rodent-active and CNS-penetrant character. Lu AF27139 has the potential for the research of CNS diseases.
  • HY-A0279
    Pristinamycin

    Pristinamycine

    Bacterial Infection
    Pristinamycin, produced by Streptomyces pristinaespiralis, is an orally active streptogramin-like antibiotic consisting of two chemically unrelated components: Pristinamycin I (PI) and Pristinamycin II (PII). Pristinamycin is highly active against many antibiotic-resistant pathogens, particularly Gram-positive bacteria, including Methicillin-resistant Staphylococcus aureus (MRSA), Vancomycin-resistant S. aureus (VRSA) and Enterococcus faecium (VREF).
  • HY-14904
    Umifenovir

    SARS-CoV Influenza Virus Infection
    Umifenovir is a potent, orally active broad-spectrum antiviral agent with activity against a number of enveloped and non-enveloped viruses. Umifenovir is used as an anti-influenza virus agent. Umifenovir could effectively inhibit the fusion of virus with host cells. Umifenovir is an efficient inhibitor of SARS-CoV-2 in vitro. Umifenovir shows anti-inflammatory activity.
  • HY-10322
    Falnidamol

    BIBX 1382

    EGFR Cancer
    Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50=3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity.
  • HY-18010
    PCI 29732

    Btk BCRP Inflammation/Immunology
    PCI 29732 is a potent, orally active, reversible BTK inhibitor with Ki app values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase. PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2.
  • HY-118189S
    Misoprostol acid-d5

    Prostaglandin Receptor Inflammation/Immunology
    Misoprostol acid D5 is deuterium labeled Misoprostol acid. Misoprostol acid is an active metabolite of Misoprostol. Misoprostol is a synthetic analogue of prostaglandin E1 (PGE1), extensively absorbed, and undergoes rapid de-esterification to Misoprostol acid in the gastrointestinal tract after oral administration. Misoprostol can be used for non-steroidal anti-inflammatory drug-induced (NSAID) gastric ulcers. Misoprostol is an oral agent used to induce labor.
  • HY-100087
    Budesonide impurity C

    Glucocorticoid Receptor Cancer Inflammation/Immunology
    Budesonide impurity C is an impurity of Budesonide. Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist.
  • HY-109083
    Cilofexor

    GS-9674

    FXR Autophagy Inflammation/Immunology
    Cilofexor (GS-9674) is a potent, selective and orally active nonsteroidal FXR agonist with an EC50 of 43 nM. Cilofexor has anti-inflammatory and antifibrotic effects. Cilofexor has the potential for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research.
  • HY-119402
    BCL6-IN-8c

    Bcl-2 Family Cancer
    BCL6-IN-8c is a potent and orally active B-cell lymphoma 6 (BCL6)-corepressor interaction inhibitor with an IC50 of 0.10 µM in cell-free enzyme-linked immunosorbent assay.
  • HY-117610A
    Bisindolylmaleimide XI hydrochloride

    Ro 32-0432; Ro 31-8830 hydrochloride

    PKC Inflammation/Immunology
    Bisindolylmaleimide XI hydrochloride (Ro 32-0432) is a potent, selective and orally active PKC inhibitor with IC50s of 9 nM, 28 nM, 31 nM, 37 nM, and 108 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCε, respectively.
  • HY-B0298
    Clemastine

    HS-592; Meclastine

    Histamine Receptor Neurological Disease
    Clemastine (HS-592) is a potent and orally active histamine receptor H1 antagonist. Clemastine is an antihistamine mainly used for relieving symptoms of allergic reactions primarily by competing with histamine to bind H1 receptors. Anti-inflammatory effects.
  • HY-117623
    PF-06685249

    PF-249

    AMPK Metabolic Disease
    PF-06685249 (PF-249) is a potent and orally active allosteric AMPK activator with an EC50 of 12 nM for recombinant AMPK α1β1γ1. PF-06685249 can be used for diabetic nephropathy research.
  • HY-132292
    ARD-2128

    PROTACs Androgen Receptor Cancer
    ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer.
  • HY-13215
    Avasimibe

    CI-1011; PD-148515

    Acyltransferase Cancer
    Avasimibe (CI-1011; PD-148515) is an orally active acyl coenzyme A-cholesterol acyltransferase (ACAT; also called SOAT)) inhibitor with IC50s of 24 and 9.2 µM for ACAT1 and ACAT2, respectively. Avasimibe can be used for the research of prostate cancer.
  • HY-121450
    Lavoltidine

    Loxtidine; AH-234844

    Histamine Receptor Cancer
    Lavoltidine (Loxtidine) is an an orally active, irreversible and highly potent histamine H2-receptor antagonist. Lavoltidine strongly inhibits gastric acid secretion and also induces hypergastrinemia.
  • HY-144676
    pan-HER-IN-1

    EGFR Apoptosis Cancer
    pan-HER-IN-1 (Compound C5) is an irreversible, orally active pan-HER inhibitor with IC50 values of 0.38, 1.6, 2.2 and 3.5 nM against EGFR, HER4, EGFR T790M/L858R and HER2, respectively. pan-HER-IN-1 induces apoptosis and shows antitumor activities.
  • HY-144677
    pan-HER-IN-2

    EGFR Apoptosis Cancer
    pan-HER-IN-2 (Compound C6) is a reversible, orally active pan-HER inhibitor with IC50 values of 0.72, 2.0, 8.2 and 75.1 nM against EGFR, HER4, EGFR T790M/L858R and HER2, respectively. pan-HER-IN-2 induces apoptosis and shows antitumor activities.
  • HY-15879
    LB42708

    Farnesyl Transferase Apoptosis Inflammation/Immunology
    LB42708 is a potent, selective and orally active farnesyltransferase inhibitor. LB42708 inhibits farnesylation of H-Ras, N-Ras and K-Ras4B with IC50s of 0.8 nM, 1.2 nM and 2.0 nM, respectively.
  • HY-109177
    Icenticaftor

    QBW251

    CFTR Inflammation/Immunology
    Icenticaftor (QBW251) is an orally active CFTR channel potentiator, with EC50s of 79 nM and 497 nM for F508del and G551D CFTR, respectively. Icenticaftor can be used for chronic obstructive pulmonary disease (COPD) and cystic fibrosis research.
  • HY-13512
    Camostat mesylate

    Camostat mesilate; FOY305; FOY-S980

    Ser/Thr Protease SARS-CoV Infection Inflammation/Immunology
    Camostat mesylate (Camostat mesilate) is an orally active, synthetic serine protease inhibitor for chronic pancreatitis. Camostat mesylate, an inhibitor of TMPRSS2, shows antiviral activity against SARS-CoV-2. Camostat mesylate also inhibits the activity of prostasin, trypsin, and matriptase.
  • HY-107354
    Gepefrine

    Others Cardiovascular Disease
    Gepefrine is an orally active pressor agent and sympathomimetic agent. Gepefrine improves the early orthostatic disregulation of the arterial pressure.
  • HY-115506
    PF-05105679

    TRP Channel Neurological Disease
    PF-05105679 is an orally active and selective TRPM8 antagonist with an IC50 of 103 nM. PF-05105679 has the potential for cold-related pain.
  • HY-B1395
    Mecamylamine hydrochloride

    nAChR Neurological Disease
    Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist that can treat various neuropsychiatric disorders. Mecamylamine hydrochloride is originally used as a ganglionic blocker in treating hypertension. Mecamylamine hydrochloride can easily crosses the blood-brain barrier.
  • HY-102051
    XIAP/cIAP1 antagonist-1

    IAP Cancer
    XIAP/cIAP1 antagonist-1 is a potent and orally active XIAP/cIAP1 antagonist with EC50s of 5.1 nM and 0.32 nM for XIAP and cIAP1, respectively. XIAP/cIAP1 antagonist-1 inhibits the tumor growth in dose-dependent manner in vivo.
  • HY-19838
    JNJ-63533054

    GPR139 Neurological Disease
    JNJ-63533054 is a potent, selective and orally active GPR139 agonist with an EC50 of 16 nM for human GPR139 (hGPR139). JNJ-63533054 shows selective for GPR139 over other GPCRs, ion channels, and transporters. JNJ-63533054 can cross the blood-brain barrier (BBB).
  • HY-18204A
    Sacubitril/Valsartan

    LCZ696

    Angiotensin Receptor Neprilysin Apoptosis Cardiovascular Disease Endocrinology
    Sacubitril/Valsartan (LCZ696), comprised Valsartan and Sacubitril (AHU377) in 1:1 molar ratio, is a first-in-class, orally bioavailable, and dual-acting angiotensin receptor-neprilysin (ARN) inhibitor for hypertension and heart failure. Sacubitril/Valsartan ameliorates diabetic cardiomyopathy by inhibiting inflammation, oxidative stress and apoptosis.
  • HY-N7697F
    Chitobiose

    Others Others
    Chitobiose, a chitosan oligosaccharide, is a dimer of β-1,4-linked glucosamine units. Chitobiose has orally activity and high antioxidant activity.
  • HY-115931
    ABAI-30

    NO Synthase Inflammation/Immunology
    ABAI-30 is a potent and orally active anti-inflammatory agent. ABAI-30 effectively inhibits NO production in lipopolysaccharide (LPS) induced RAW264.7 cells.
  • HY-15546
    BMS-817399

    CCR Inflammation/Immunology
    BMS-817399 is a potent, selective, and orally bioavailable CCR1 antagonist. BMS-817399 exhibits CCR1 binding affinity and chemotaxis inhibition potencies of 1 and 6 nM (IC50), respectively. BMS-817399 can be used for the research of rheumatoid arthritis.
  • HY-109176
    Giredestrant

    GDC-9545

    Estrogen Receptor/ERR Cancer
    Giredestrant (GDC-9545), a non-steroidal estrogen receptor (ER) ligand, is an orally active and selective ER antagonist. Giredestrant potently competes with Estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity.
  • HY-N8435
    Desoxo-narchinol A

    TNF Receptor COX NO Synthase PGE synthase Infection Inflammation/Immunology
    Desoxo-narchinol A is an orally active and potent anti-inflammatory agent. Desoxo-narchinol A can be isolated from the roots and rhizomes of Nardostachys jatamansi. Desoxo-narchinol A can be used for septic shock and inflammatory diseases research.
  • HY-145919
    hGPR91 antagonist 3

    Others Inflammation/Immunology Cardiovascular Disease
    hGPR91 antagonist 3 (Compound 5g) is a potent, selective, and orally active antagonist of hGPR91 (%F: 26). hGPR91 antagonist 3 has the potential for the research of hypertension, autoimmune disease and retinal angiogenesis.
  • HY-103416
    A-77636 hydrochloride

    Dopamine Receptor Neurological Disease
    A-77636 hydrochloride is a potent, orally active, selective and long acting dopamine D1 receptor agonist (pKi=7.40; Ki=39.8 nM) with antiparkinsonian activity. A-77636 hydrochloride is functionally inactive at dopamine D2 receptor.
  • HY-12413A
    BMS-986118

    Free Fatty Acid Receptor Metabolic Disease
    BMS-986118 is a potent, orally active, and selective GPR40 agonist with an EC50 of 0.07 µM. BMS-986118 has dual insulinotropic and GLP-1 secretory effects, resulting in robust plasma glucose lowering effects in acute animal models.
  • HY-134772
    AS1810722

    STAT Cytochrome P450 Inflammation/Immunology
    AS1810722 is an orally active and potent STAT6 inhibitor with an IC50 of 1.9 nM. AS1810722 shows a good profile of CYP3A4 inhibition. AS1810722, a derivative of fused bicyclic pyrimidine, has the potential for allergic diseases such as asthma and atopic diseases research.
  • HY-103689
    Cucurbit[8]uril

    Others Others
    Cucurbit[8]uril is a potent, low toxicity and orally active supramolecular inducer of protein heterodimerization. Cucurbit[8]uril induces heterodimerization of methylviologen and naphthalene functionalized proteins. Cucurbit[8]uril can induce energy transfer .
  • HY-N0586A
    Norisoboldine hydrochloride

    (+)-Laurelliptine hydrochloride

    Adenosine Receptor Inflammation/Immunology
    Norisoboldine hydrochloride is an orally active natural aryl hydrocarbon receptor (AhR) agonist. Norisoboldine hydrochloride, as a major isoquinoline alkaloid present in Radix Linderae, can be used for the research of Rheumatoid arthritis and Ulcerative colitis.
  • HY-N0586
    Norisoboldine

    (+)-Laurelliptine

    Adenosine Receptor Inflammation/Immunology
    Norisoboldine is an orally active natural aryl hydrocarbon receptor (AhR) agonist. Norisoboldine, as a major isoquinoline alkaloid present in Radix Linderae, can be used for the research of Rheumatoid arthritis and Ulcerative colitis.
  • HY-145695
    Dual AChE-MAO B-IN-1

    AChE Monoamine Oxidase Neurological Disease
    Dual AChE-MAO B-IN-1 (compound 15) is an orally bioavailable CNS-permeant potent inhibitor of both human AChE (IC50=550 nM) and MAO B (IC50=8.2 nM). Dual AChE-MAO B-IN-1 behaves as a safe and metabolically stable neuroprotective agent, devoid of cytochrome liability.
  • HY-18662
    RQ-00203078

    TRP Channel Cancer Neurological Disease
    RQ-00203078 is a highly selective, potent and orally active TRPM8 antagonist with IC50s of 5.3 nM and 8.3 nM for rat and human TRPM8 channels, respectively. RQ-00203078 shows little inhibitory action against TRPV1, TRPA1, TRPV4, or TRPM2 channels.
  • HY-120669
    PF-06761281

    Sodium Channel Metabolic Disease
    PF-06761281 (Compound 4a) is a potent, orally active, partial selective sodium-coupled citrate transporter (NaCT or SLC13A5) inhibitor with IC50 values of 0.51, 13.2 and 14.1 µM against HEKNaCT, HEKNaDC1 and HEKNaDC3, respectively.
  • HY-141535A
    IL-17 modulator 1 disodium

    Interleukin Related Infection Inflammation/Immunology
    IL-17 modulator 1 (disodium) is an orally active, highly efficacious IL-17 modulator extracted from patent WO 2020127685. IL-17 modulator 1 (disodium) can be used for the research of diseases including psoriasis, ankylosing spondylitis and psoriatic arthritis.
  • HY-141514
    MSA-2 dimer

    STING Cancer Inflammation/Immunology
    MSA-2 dimer is a selective, orally active non-nucleotide STING agonist (Kd=145 μM) with long-term antitumor and immunogenic activity. MSA-2 dimer is bound to STING as a non-covalent dimer exhibiting higher permeability than cyclic dinucleotide.
  • HY-136185
    Atorvastatin Epoxy Tetrahydrofuran Impurity

    Others Others
    Atorvastatin Epoxy Tetrahydrofuran Impurity is an impurity isolated oxidative degradation products of Atorvastatin (HY-B0589). Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids.
  • HY-108288
    Sulbactam pivoxil

    CP 47904

    Antibiotic Bacterial Infection
    Sulbactam pivoxil is a prodrug of sulbactam. Sulbactam is a β-lactamase inhibitor which poorly adsorbed from gastrointestinal tract. Sulbactam pivoxil has a better absorption than the parent drug and provides high serum levels after oral administration.
  • HY-108411
    Emedastine

    Histamine Receptor Inflammation/Immunology
    Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis.
  • HY-N0304
    L-DOPA

    Levodopa; 3,4-Dihydroxyphenylalanine

    Dopamine Receptor Endogenous Metabolite Neurological Disease
    L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease.
  • HY-122011
    PF-4950834

    ROCK SGK PKA PKC Inflammation/Immunology
    PF-4950834 is a potent, selective, orally bioavailable, ATP-competitive rho kinase inhibitor with IC50 values of 8.35 nM and 33.12 nM against ROCK2 and ROCK1, respectively. PF-4950834 inhibits neutrophil migration.
  • HY-116565
    Usmarapride

    SUVN-D4010

    5-HT Receptor Neurological Disease
    Usmarapride (SUVN-D4010) is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) can be used for the research of cognitive deficits associated with Alzheimer's disease.
  • HY-146268
    CaMKIIα-IN-1

    CaMK Neurological Disease
    CaMKIIα-IN-1 (Compound 4d) is an orally active Ca 2+/calmodulin-dependent protein kinase II α (CaMKIIα) inhibitor with a KD of 219 nM for CaMKIIα WT hub. CaMKIIα-IN-1 has good metabolic stability.
  • HY-103433
    K579

    Dipeptidyl Peptidase Metabolic Disease
    K579 is a potent and orally active dipeptidyl peptidase IV inhibitor. K579 inhibits the blood glucose elevation. K579 increases the plasma insulin and active forms of glucagon-like peptide-1 (GLP-1). K579 has the potential for the research of diabetic.
  • HY-19934
    TAS-117

    Akt Apoptosis Autophagy Cancer
    TAS-117 is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). TAS-117 triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. TAS-117 induces apoptosis and autophagy.
  • HY-19934A
    TAS-117 hydrochloride

    Akt Apoptosis Autophagy Cancer
    TAS-117 hydrochloride is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). TAS-117 hydrochloride triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. TAS-117 hydrochloride induces apoptosis and autophagy.
  • HY-B2145
    Ilaprazole sodium

    IY-81149 sodium

    Proton Pump TOPK Cancer Inflammation/Immunology
    Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
  • HY-14325A
    L-745870 trihydrochloride

    Dopamine Receptor Neurological Disease
    L-745870 trihydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 trihydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors.
  • HY-142686
    SGK1-IN-3

    SGK Inflammation/Immunology
    SGK1-IN-3 (compound 3a) is a potent and orally active inhibitor of SGK1. The serine/threonine kinase SGK1 is an activator of the β-catenin pathway and a powerful stimulator of cartilage degradation that is found to be upregulated under genomic control in diseased osteoarthritic cartilage. SGK1-IN-3 has the potential for the research of osteoarthritis.
  • HY-122643
    NITD-916

    Bacterial Infection
    NITD-916, a 4-hydroxy-2-pyridone derivative, is an orally active and highly lipophilic mycobacterial enoyl reductase InhA inhibitor with an IC50 of 570 nM. NITD-916 forms a ternary complex with InhA and NADH to block access to the fatty acyl substrate binding pocket. NITD-916 has potent anti-tuberculosis effects.
  • HY-124290
    Carotegrast methyl

    AJM300

    Integrin Inflammation/Immunology
    Carotegrast methyl (AJM300) is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of Carotegrast methyl, is a specific and dual α4β1/α4β7 integrin antagonist. Carotegrast methyl prevents the development of colitis in mice.
  • HY-114245
    Se-Methylselenocysteine

    Methylselenocysteine; Se-Methylseleno-L-cysteine

    Apoptosis Cancer
    Se-Methylselenocysteine, a precursor of Methylselenol, has potent cancer chemopreventive activity and anti-oxidant activity. Se-Methylselenocysteine is orally bioavailable, and induces apoptosis.
  • HY-10999
    Trametinib

    GSK1120212; JTP-74057

    MEK Autophagy Apoptosis Cancer
    Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis.
  • HY-10515
    BX-320

    PDK-1 Cancer
    BX-320 is a selective, ATP-competitive, orally acitive, and direct PDK1 inhibitor with an IC50 of 30 nM in a direct kinase assay format. BX-320 also induces apoptosis. Anticancer effect.
  • HY-B1617A
    Zuclomiphene citrate

    Estrogen Receptor/ERR Endocrinology Metabolic Disease
    Zuclomiphene citrate is a cis isomer of Clomiphene citrate. Zuclomiphene citrate has an antiestrogenic effect and can inhibit the secretion of luteinizing hormone (LH) more than the trans isomer. Zuclomiphene citrate is also an orally active hypocholesterolemic agent.
  • HY-15550
    4'-Hydroxy diclofenac

    Drug Metabolite Inflammation/Immunology Neurological Disease
    4'-Hydroxy diclofenac is an orally active metabolite of Diclofenac (HY-15036) by cytochrome P450 2C9 (CYP2C9). 4'-Hydroxy diclofenac has anti-inflammatory and analgesic properties.
  • HY-14670
    Firocoxib

    ML 1785713

    COX Inflammation/Immunology
    Firocoxib (ML 1785713) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 0.13 μM. Firocoxib shows 58-fold more selective for COX-2 than COX-1 (IC50 of 7.5 μM). Firocoxib has anti-inflammatory effects.
  • HY-100748
    CXD101

    HDAC Cancer
    CXD101 is a potent, selective and orally active class I HDAC inhibitor with IC50s of 63 nM, 570 nM and 550 nM for HDAC1, HDAC2 and HDAC3, respectively. CXD101 has no activity against HDAC class II. CXD101 has antitumor activity.
  • HY-135401
    VU6015929

    Discoidin Domain Receptor Inflammation/Immunology
    VU6015929 is a potent, selective and orally active dual discoidin domain receptor 1/2 (DDR1/2) inhibitor with IC50s of 4.67 nM and 7.39 nM, respectively. VU6015929 potently blocks collagen-induced DDR1 activation and collagen-IV production.
  • HY-100516
    Cimicoxib

    UR-8880

    COX Inflammation/Immunology
    Cimicoxib (CX) is an orally active potent and selective COX-2 (cyclo-oxygenase-2) inhibitor. Cimicoxib exhibits promising anti-inflammatory and analgesic activity. The PK parameters of Cimicoxib in dogs given precise (2 mg/kg) and approximate doses (1.95-2.5 mg/kg) are similar.
  • HY-A0231
    Glymidine sodium

    Gondafon; Glycodiazine

    Others Metabolic Disease
    Glymidine sodium is an oral active antidiabetic. Glymidine sodium is the inhibitor of hepatic lipolysis. Glymidine sodium inhibits the glucose formation and supresses the elevated pyruvate oxidation which results from the inhibition of endogenous lipid mobilization.
  • HY-A0115
    Ramiprilat

    HOE 498 diacid; Ramipril diacid

    Angiotensin-converting Enzyme (ACE) Endogenous Metabolite Cardiovascular Disease
    Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a Ki value of 7 pM. Ramiprilat can be used for high blood pressure and heart failure research.
  • HY-124729
    BL-918

    ULK Autophagy Neurological Disease
    BL-918 is an orally active UNC-51-like kinase 1 (ULK1) activator with an EC50 of 24.14 nM. BL-918 exerts its cytoprotective autophagic effect by targeting ULK complex. BL-918 has the potential for Parkinson’s disease (PD) treatment.
  • HY-10864
    URB-597

    KDS-4103

    FAAH Autophagy Mitophagy Neurological Disease
    URB-597 (KDS-4103) is an orally bioavailable and selective FAAH inhibitor. URB-597 inhibits FAAH activity with an IC50s of approximately 5 nM in rat brain membranes, 0.5 nM in intact rat neurons, 3 nM in human liver microsomes. Antidepressant-like effects. Analgesic activity.
  • HY-141535
    IL-17 modulator 1

    Interleukin Related Infection Inflammation/Immunology
    IL-17 modulator 1 is an orally active, highly efficacious small molecule IL-17 modulators extracted from patent WO 2020127685. IL-17 modulator 1 can be used for the research of preventing, treating or ameliorating a variety of diseases including psoriasis, ankylosing spondylitis and psoriatic arthritis.
  • HY-132298
    TDI-10229

    Adenylate Cyclase Others
    TDI-10229 is a potent and orally bioavailable inhibitor of soluble adenylyl cyclase (sAC, ADCY10). TDI-10229 displays nanomolar inhibition of sAC in both biochemical and cellular assays (IC50 of 195 nM) and exhibits mouse pharmacokinetic properties sufficient to warrant its use as an in vivo tool compound.
  • HY-110198
    ONO-8130

    Prostaglandin Receptor PERK Inflammation/Immunology
    ONO-8130 is an orally active and selective prostanoid EP1 receptor antagonist. ONO-8130 blocks phosphorylation of ERK in the L6 spinal cord. ONO-8130 relieves bladder pain in mice with cyclophosphamide-induced cystitis. ONO-8130 can be used for interstitial cystitis research.
  • HY-101664
    Ilaprazole

    IY-81149

    Proton Pump TOPK Cancer Inflammation/Immunology
    Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
  • HY-146435
    Anti-inflammatory agent 22

    TNF Receptor Inflammation/Immunology
    Anti-inflammatory agent 22 (compound 14a) is an orally active anti-inflammatory agent. Anti-inflammatory agent 22 inhibits LPS-induced TNF-α production with an IC50 value of 14.6 μM. Anti-inflammatory agent 22 has preventive effects on lymphedematous tissue via suppression of adipogenesis. Anti-inflammatory agent 22 suppresses limb lymphedema volume in mice.
  • HY-138768
    ELOVL6-IN-1

    Others Metabolic Disease
    ELOVL6-IN-1 is a potent, orally active and selective ELOVL6 inhibitor. ELOVL6-IN-1 dose-dependently inhibits mouse ELOVL6 activities, with an IC50 value of 0.350 μM. ELOVL6-IN-1 inhibits ELOVL6 in a noncompetitive manner for malonyl-CoA (Ki=994 nM) and palmitoyl-CoA.
  • HY-121149
    Droloxifene

    3-Hydroxytamoxifen

    Estrogen Receptor/ERR Apoptosis Cancer
    Droloxifene, a Tamoxifen derivative, is an orally active and selective estrogen receptor modulator. Droloxifene shows antiestrogenic and anti-implantation effects. Droloxifene induces p53 expression and apoptosis in MCF-7 cells. Droloxifene prevents bone loss in ovariectomized rats .
  • HY-147570
    ATR-IN-18

    ATM/ATR Cancer
    ATR-IN-18 (compound 2) is an orally active and potent ATR kinase inhibitor, with an IC50 of 0.69 nM. ATR-IN-18 shows antiproliferative activity in LoVo cells, with an IC50 of 37.34 nM. ATR-IN-18 has anti-tumor activity.
  • HY-B2178
    Emedastine difumarate

    Histamine Receptor Inflammation/Immunology
    Emedastine difumarate is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine difumarate is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis.
  • HY-144270
    Glucosylceramide synthase-IN-3

    Others Metabolic Disease Neurological Disease
    Glucosylceramide synthase-IN-3 (compound BZ1) is a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 16 nM for human GCS.Glucosylceramide synthase-IN-3 can be used for Gaucher's disease research.
  • HY-139077
    SCD1 inhibitor-3

    Stearoyl-CoA Desaturase (SCD) Cancer Metabolic Disease
    SCD1 inhibitor-3 is a safe, potent and orally active SCD1 inhibitor. SCD1 inhibitor-3 can be used for the research of metabolic diseases such as obesity, type II diabetes and dyslipidemia, as well as skin diseases, acne and cancer.
  • HY-143880
    MRGPRX1 agonist 4

    Others Neurological Disease
    MRGPRX1 agonist 4 (compound 1t) is a potent and orally active Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC50 value of 0.1 μM. MRGPRX1 agonist 4 has good metabolic stability and oral bioavailability. MRGPRX1 agonist 4 can reduce behavioral heat hypersensitivity in a neuropathic pain model humanized MRGPRX1 mice. MRGPRX1 agonist 4 can be used for researching neuropathic pain.
  • HY-147772
    ZC0101

    Indoleamine 2,3-Dioxygenase (IDO) Apoptosis ROS Cancer
    ZC0101 is a potent, orally active IDO1 and TrxR dual inhibitor with IC50 values of 0.084 μM and 7.98 μM, respectively. ZC0101 effectively induces apoptosis and ROS accumulation in cancer cells.
  • HY-114191B
    SSTR5 antagonist 2 hydrochloride

    Somatostatin Receptor Endocrinology Metabolic Disease
    SSTR5 antagonist 2 hydrochloride is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of type 2 diabetes mellitus (T2DM).
  • HY-144117
    GFB-12811

    CDK Metabolic Disease
    GFB-12811 is a high selective and orally active CDK5 inhibitor with an IC50 of 2.3 nM. GFB-12811 is highly selective over the other tested kinases (CDK1/2/6/7/9).
  • HY-109143
    Elsubrutinib

    ABBV-105

    Btk Inflammation/Immunology
    Elsubrutinib (ABBV-105) is an orally active, potent, selective and irreversible Bruton's tyrosine kinase (BTK) inhibitor。The IC50 of Elsubrutinib for BTK catalytic domain is 0.18 μM. Elsubrutinib can be used for the research of inflammatory disease.
  • HY-146334
    DFBTA

    Chloride Channel Inflammation/Immunology
    DFBTA is an orally active, potent and little brain penetrated ANO1 (Calcium-activated chloride channel anoctamin-1) inhibitor, with an IC50 of 24 nM. DFBTA shows analgesic efficacy for inflammatory pain.
  • HY-14180
    PHA 408

    IKK Inflammation/Immunology
    PHA 408 (PHA-408) is a potent, selective and orally active IκB kinase-2 (IKK-2) inhibitor. PHA 408 is a powerful anti-inflammatory agent against lipopolysaccharide (LPS)- and cigarette smoke (CS)-mediated lung inflammation.
  • HY-113974
    trans-AUCB

    t-AUCB

    Epoxide Hydrolase Cancer
    trans-AUCB (t-AUCB) is a potent, orally active and selective soluble epoxide hydrolase (sEH) inhibitor with IC50s of 1.3 nM, 8 nM, 8 nM for hsEH, mouse sEH and rat sEH, respectively. trans-AUCB has anti-glioma activity.
  • HY-100399
    Nevanimibe

    PD-132301; ATR-101

    Acyltransferase Apoptosis Cancer
    Nevanimibe (PD-132301) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe induces cell apoptosis and has the potential for adrenocortical cancer.
  • HY-144841
    CFT7455

    Ligands for E3 Ligase Cancer
    CFT7455 is an orally active zinc finger transcription factors Ikaros (IKZF1), Aiolos (IKZF3) degrader. CFT7455 is an anti-cancer agent that binds with high affinity to the cereblon E3 ligase (Kd of 0.9 nM) (WO2022032132A1; Compound 1).
  • HY-147573
    BRD4 Inhibitor-23

    Epigenetic Reader Domain Cancer
    BRD4 Inhibitor-23 is a potent and orally active BRD4 inhibitor with IC50s of 6.21 nM and 1.44 nM for BRD4 BD-1 and BRD4 BD-2, respectively (WO2022033542A1; Example 1).
  • HY-100399A
    Nevanimibe hydrochloride

    PD-132301 hydrochloride; ATR101 hydrochloride

    Acyltransferase Apoptosis Cancer
    Nevanimibe hydrochloride (PD-132301 hydrochloride) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe hydrochloride inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe hydrochloride induces cell apoptosis and has the potential for adrenocortical cancer.
  • HY-143872
    Bcl-2-IN-4

    Bcl-2 Family Cancer
    Bcl-2-IN-4 is a potent, orally active and selective Bcl-2 inhibitor with an IC50 of 1.5 nM. Bcl-2-IN-4 displays >200-fold selectivity over Bcl-xL (IC50 of 411 nM). Bcl-2-IN-4 inhibits RS4; 11 cell proliferation with an IC50 of 2.7 nM (WO2021180040A1; compound 2).
  • HY-12072
    Lck Inhibitor

    Src Inflammation/Immunology
    Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis.
  • HY-138696
    XL092

    TAM Receptor c-Met/HGFR VEGFR Cancer
    XL092 is an orally active, ATP-competitive inhibitor of multiple receptor tyrosine kinases (RTKs) including MET, VEGFR2, AXL and MER, with IC50s in cell-based assays of 15 nM, 1.6 nM, 3.4 nM, 7.2 nM respectively. XL092 exhibits anti-tumor activity. XL092 has the potential for kinase-dependent diseases and conditions research.
  • HY-B0368
    Captopril

    SQ 14225

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM.
  • HY-134188
    JNJ-54717793

    Orexin Receptor (OX Receptor) Neurological Disease
    JNJ-54717793, as a brain penetrant, is an orally active, selective and high affinity orexin-1 receptor (OX1R) antagonist (plasma EC50=85 ng/mL). The Ki values of JNJ-54717793 for hOX1R (human OX1R) and hOX2R are 16 nM and 700 nM, respectively. JNJ-54717793 is a potent compound of anxiety disorders.
  • HY-107623
    TC-MCH 7c

    MCHR1 (GPR24) Metabolic Disease
    TC-MCH 7c, a phenylpyridone derivative, is an orally available, selective and brain-penetrable MCH1R antagonist with an IC50 of 5.6 nM for hMCH1R. TC-MCH 7c has Kis of 3.4 nM and 3.0 nM of human and mouse MCH1R, respectively.
  • HY-130120
    HWL-088

    Free Fatty Acid Receptor PPAR Metabolic Disease
    HWL-088 is a highly potent and orally active free fatty acid receptor 1 (FFA1/GPR40) agonist (EC50 of 18.9 nM) with moderate PPARδ activity (EC50 of 570.9 nM) . HWL-088 improves glucose and lipid metabolism, and has anti-diabetic effects.
  • HY-19888
    GSK-1482160

    P2X Receptor Inflammation/Immunology
    GSK-1482160 is an orally available negative allosteric modulator of the P2X7 receptor. P2X7 receptors are involved in the production of pro-inflammatory cytokines, such as Il-1β, by central and peripheral immune cells. GSK-1482160 has the potential for the research of inflammation diseases.
  • HY-109127
    Berotralstat

    Ser/Thr Protease Others
    Berotralstat (BCX7353) is a low toxicity, effective, highly specific, second-generation, synthetic and orally active plasma kallikrein inhibitor used for the research of hereditary angioedema (HAE) attacks. Berotralstat works by blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE.
  • HY-15011
    L-372662

    Oxytocin Receptor Others
    L-372662 is a potent and orally active non-peptide oxytocin antagonist with a Ki value of 4.8. The Kd value of L-372662 for wild-type hOTR and [A318G]OTR is 5.8 nM and 73 nM. L-372662 shows selectivity to OTR:V1aR.
  • HY-116565A
    Usmarapride free base

    SUVN-D4010 free base

    5-HT Receptor Neurological Disease
    Usmarapride (SUVN-D4010) free base is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) free base can be used for the research of cognitive deficits associated with Alzheimer's disease.
  • HY-144448
    FAK-IN-2

    FAK Apoptosis Cancer
    FAK-IN-2 is a potent and orally active focal adhesion kinase (FAK) inhibitor, with anticancer activity (FAK IC50= 35 nM). FAK-IN-2 covalently inhibits the autophosphorylation of FAK in a dose-dependent manner, and inhibits the clone formation and migration of tumor cells, inducing apoptosis.
  • HY-100886
    BAY1082439

    PI3K Apoptosis Cancer
    BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth.
  • HY-144285
    CXCR4 antagonist 4

    CXCR HIV Inflammation/Immunology
    CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM).
  • HY-139486
    AM-8123

    Others Cardiovascular Disease
    AM-8123 is an orally active and potent APJ agonist. AM-8123 inhibits Forskolin-stimulated cAMP production and promotes Gα protein activation. AM-8123 can be used for the research of cardiovascular disease.
  • HY-118301
    ADX71441

    GABA Receptor Neurological Disease
    ADX71441 is a potent and selective positive allosteric modulator of the GABAB receptor. ADX71441 is bioavailable after oral administration and is brain penetrant. ADX71441 has the potential for research of anxiety, pain and spasticity.
  • HY-130247
    JAK2/FLT3-IN-1

    JAK FLT3 Apoptosis Cancer
    JAK2/FLT3-IN-1 is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 has anti-cancer activity.
  • HY-116804
    ZLD1039

    Histone Methyltransferase Cancer
    ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC50 values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis.
  • HY-B1156
    Cephradine

    Cefradine; SQ-11436

    Bacterial Antibiotic TOPK Infection Inflammation/Immunology
    Cephradine (Cefradine) is a broad-spectrum and orally active cephalosporin. Cephradine is active against both gram-positive and gram-negative pathogens. Cephradine is effective in eradicating most penicillinase-producing organisms. Cephradine has been used in the research of genitourinary, gastrointestinal and respiratory tract infections, and in infections of the skin and soft tissues. Cephradine blocks solar-ultraviolet induced skin inflammation through direct inhibition of TOPK.
  • HY-144256
    CHD1Li 6.11

    Others Cancer
    CHD1Li 6.11 is a potent oncogenic CHD1L inhibitor (IC50=3.3 µM for cat-CHD1L recombinant protein). CHD1Li 6.11 is an orally bioavailable antitumor agent, significantly reducing the tumor volume of CRC xenografts generated from isolated quasi mesenchymal cells (M-phenotype), which possess enhanced tumorigenic properties.
  • HY-50905
    Dovitinib

    CHIR-258; TKI258

    FLT3 c-Kit FGFR VEGFR PDGFR c-Fms Cancer
    Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC50s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity.
  • HY-136207
    TC-2559 difumarate

    nAChR Neurological Disease
    TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect.
  • HY-12501A
    ITI-214

    Phosphodiesterase (PDE) Neurological Disease
    ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions.
  • HY-147719
    COX-2-IN-16

    COX Inflammation/Immunology
    COX-2-IN-16 (compound 2b) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 102 µM. COX-2-IN-16 inhibits the NO production. COX-2-IN-16 shows anti-inflammatory activity.
  • HY-W015828
    RGX-202

    Endogenous Metabolite Cancer
    RGX-202 is an oral small-molecule SLC6A8 transporter inhibitor. RGX-202 robustly inhibits creatine import in vitro and in vivo, reduces intracellular phosphocreatine and ATP levels, and induces tumor apoptosis. RGX-202 can be used for the research of cancer.
  • HY-144266
    Glucosylceramide synthase-IN-1

    Others Metabolic Disease Neurological Disease
    Glucosylceramide synthase-IN-1 (T-036) a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 31 nM and 51 nM for human GCS and mouse GCS, respectively. Glucosylceramide synthase-IN-1 can be used for Gaucher's disease research.
  • HY-111432
    CCG-232601

    Ras Others
    CCG-232601 (compound 8f) is a potent and orally active Rho/MRTF/SRF transcriptional pathway inhibitor. CCG-232601 inhibits the development of Bleomycin-induced dermal fibrosis in mice. CCG-232601 has the potential for the research of antifibrotic for systemic scleroderma.
  • HY-12113
    Oprozomib

    ONX 0912; PR-047

    Proteasome Autophagy Cancer
    Oprozomib (PR-047) is an orally bioavailable and selective peptide epoxyketone proteasome inhibitor with IC50s of 36 and 82 nM for proteasome (β5) and immunoproteasome (LMP7), respectively. Oprozomib (ONX 0912) induces apoptosis in MM cells.
  • HY-123797
    KGA-2727

    SGLT Metabolic Disease
    KGA-2727 is a first selective, high-affinity and orally active SGLT1 inhibitor with Kis of 97.4 nM and 43.5 nM for human and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 has antidiabetic efficacy.
  • HY-13801
    Fexinidazole

    HOE 239

    Parasite Infection
    Fexinidazole (HOE 239) is an orally active, potent nitroimidazole antitrypanosomal drug. Fexinidazole shows trypanocidal activity against T. brucei subspecies and strains with IC50s of 0.7-3.3 μM (0.2-0.9 μg/ml). Fexinidazol has the potential for human sleeping sickness (HAT) caused by infection with T. brucei.
  • HY-14674
    CP-724714

    EGFR Apoptosis Cancer
    CP-724714 is a potent, selective and orally active ErbB2 (HER2) tyrosine kinase inhibitor, with an IC50 of 10 nM. CP-724714 displays a marked selectivity against EGFR kinase (IC50=6400 nM). CP-724714 potently inhibits ErbB2 receptor autophosphorylation in intact cells. Antitumor activities.
  • HY-114452
    LY2940094

    BTRX-246040

    Opioid Receptor Neurological Disease
    LY2940094 (BTRX-246040) is a potent, selective and orally available nociceptin receptor (NOP receptor) antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 reduces ethanol self-administration in animal models.
  • HY-145828
    Microtubule inhibitor 2

    Microtubule/Tubulin Ferroptosis Cancer
    Microtubule inhibitor 2 is a potent and selective, orally active microtubule inhibitor. Microtubule inhibitor 2 triggers cell death through ferroptosis . Microtubule inhibitor 2 shows antitumor activity.
  • HY-10274
    Dabigatran etexilate

    BIBR 1048

    Thrombin Cardiovascular Disease
    Dabigatran etexilate (BIBR 1048) is an orally active prodrug of Dabigatran (a direct inhibitor of thrombin). Dabigatran etexilate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation.
  • HY-145872
    HBV-IN-20

    HBV Infection
    HBV-IN-20 is a potent and oral active HBV inhibitor with an EC50 of 0.46 µM. HBV-IN-20 is a typical type II CpAM (core protein assembly modulators).
  • HY-114191
    SSTR5 antagonist 2

    Somatostatin Receptor Metabolic Disease Endocrinology
    SSTR5 antagonist 2 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of treat type 2 diabetes mellitus (T2DM).
  • HY-12047
    Ponatinib

    AP24534

    Bcr-Abl PDGFR VEGFR FGFR Src Autophagy Cancer
    Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
  • HY-114191A
    SSTR5 antagonist 2 TFA

    Somatostatin Receptor Metabolic Disease Endocrinology
    SSTR5 Antagonist 1 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of treat type 2 diabetes mellitus (T2DM).
  • HY-10358
    MK-2206 dihydrochloride

    MK-2206 (2HCl)

    Akt Autophagy Apoptosis Cancer
    MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active allosteric AKT inhibitor with IC50s of 5 nM, 12 nM, and 65 nM for AKT1, AKT2, and AKT3, respectively. MK-2206 dihydrochloride induces autophagy.
  • HY-136270
    Gartisertib

    VX-803; M4344; ATR inhibitor 2

    ATM/ATR Cancer
    Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity.
  • HY-101528
    IDRA 21

    iGluR Neurological Disease
    IDRA 21 is a positive and orally active modulator of the AMPA receptor. IDRA 21 facilitates excitatory neurotransmission via GluR1/2 receptors. IDRA 21 has the potential for the research of cognitive/memory disorders, including those associated with aging.
  • HY-132193
    RET-IN-4

    RET Cancer
    RET-IN-4 is a potent, selective and orally active RET inhibitor with IC50s of 1.29 nM, 1.97 nM, and 0.99 nM for RET (WT), RET (V804M), and RET (M918T), respectively. RET-IN-4 exhibits better kinases selectivity against JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). RET-IN-4 has anticancer effects.
  • HY-14336A
    SB 271046 Hydrochloride

    SB 271046A

    5-HT Receptor Neurological Disease
    SB 271046 Hydrochloride (SB 271046A) is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 9.02, 8.55, and 8.81 for rat, pig and human, respectively. SB 271046 Hydrochloride is over 200 fold selective for the 5-HT6 receptor vs 55 other receptors, binding sites and ion channels. Anticonvulsant activity (EC50=0.16 μM).
  • HY-130247A
    JAK2/FLT3-IN-1 TFA

    JAK FLT3 Apoptosis Cancer
    JAK2/FLT3-IN-1 (TFA) is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 (TFA) has anti-cancer activity.
  • HY-145311
    Bis-Pro-5FU

    Nucleoside Antimetabolite/Analog Cancer
    Bis-Pro-5FU (Compound 4) is a 5-FU precursor that confers oral bioavailability and increase the safety profile of 5-Fluorouracil (5-FU) chemotherapy regimens. 5-FU is an antineoplastic antimetabolite that is widely used for the research of colorectal and pancreatic cancer.
  • HY-14803
    Tasimelteon

    BMS-214778; VEC-162

    Melatonin Receptor Neurological Disease Endocrinology
    Tasimelteon (BMS-214778) is an orally active and selective dual melatonin receptor agonist (DMRA). Tasimelteon has 2.1-4.4 times greater affinity for the MT2 receptor than for the MT1 receptor. Tasimelteon is a circadian regulator and has the potential for Non-24-Hour Sleep-Wake Disorder (Non-24).
  • HY-14653
    Amsilarotene

    TAC-101; Am 555S

    RAR/RXR Apoptosis Cancer
    Amsilarotene (TAC-101; Am 555S), an orally active synthetic retinoid, has selective affinity for retinoic acid receptor α (RAR-α) binding with Ki of 2.4, 400 nM for RAR-α and RAR-β. Amsilarotene induces the apoptotic of human gastric cancer, hepatocellular carcinoma and ovarian carcinoma cells. Amsilarotene can be used for the research of cancer.
  • HY-107670
    Dihydro-β-erythroidine hydrobromide

    DHβE hydrobromide

    nAChR Neurological Disease
    Dihydro-β-erythroidine (DHβE) hydrobromide is a potent, orally active, and competitive antagonist of neuronal nAChRs. Dihydro-β-erythroidine hydrobromide shows selectivity for α4β4 and α4β2 nAChRs, with IC50s of 0.19 and 0.37 μM, respectively. Antidepressant-like activities.
  • HY-139094
    A6770

    LPL Receptor Metabolic Disease
    A6770 is an orally active, potent sphingosine 1-phosphate (S1P) lyase (S1PL) inhibitor. A6770 is phosphorylated and the phosphorylated form directly inhibits S1P lyased.A6770, a potential key metabolite of THI, induces a [ 3H]dhS1P increase.
  • HY-144863
    BAY 1214784

    GnRH Receptor Cancer
    BAY 1214784 is a potent, selective, and orally active antagonist of the human gonadotropin-releasing hormone receptor (hGnRH-R). BAY 1214784 is a spiroindoline derivative compound. BAY 1214784 effectively lowers plasma luteinizing hormone levels by up to 49%, at the same time being associated with low pharmacokinetic variability and good tolerability. BAY 1214784 has the potential for the research of uterine fibroids.
  • HY-106420
    16,16-Dimethyl prostaglandin E2

    16,16-dimethyl PGE2

    Prostaglandin Receptor Inflammation/Immunology
    16,16-Dimethyl prostaglandin E2 (16,16-dimethyl PGE2) is an orally active vertebrate Hematopoietic stem cells (HSCs) homeostasis critical regulator. 16,16-Dimethyl prostaglandin E2 can act through EP2/EP4 and has an interaction with the Wnt pathway.
  • HY-112090
    ABBV-744

    Epigenetic Reader Domain HIV Cancer Infection Inflammation/Immunology
    ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC50 values ranging from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with drug-like properties enable the investigation of its antitumor efficacy and tolerability.
  • HY-105189
    Meclinertant

    SR 48692

    Neurotensin Receptor Neurological Disease
    Meclinertant (SR 48692) is a potent, selective, nonpeptide and orally active neurotensin receptor 1 (NTS1) antagonist. In human colon carcinoma (HT-29) cells, Meclinertant competitively antagonizes neurotensin-induced intracellular Ca 2+ mobilization with a pA2 values of 8.13. Meclinertant has anxiolytic, anti-addictive and memory-impairing effects.
  • HY-12501
    ITI-214 free base

    Phosphodiesterase (PDE) Neurological Disease
    ITI-214 free base is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 free base inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 free base shows efficacy in various animal models of motor and cognitive functions.
  • HY-10274A
    Dabigatran etexilate mesylate

    BIBR 1048MS; Dabigatran etexilate methanesulfonate

    Thrombin Cardiovascular Disease
    Dabigatran etexilate mesylate (BIBR 1048MS) is an orally active prodrug of Dabigatran (a direct inhibitor of thrombin). Dabigatran etexilate mesylate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation.
  • HY-142772
    Y08284

    Epigenetic Reader Domain Cancer
    Y08284 is a potent, selective, oral active CBP bromodomain inhibitor with an IC50 of 4.21 nM. Y08284 suppresses the proliferation of prostate cancer cell lines LNCaP, C4-2B, and 22Rv1. Antitumor activity.
  • HY-100560
    Abscisic acid

    (S)​-​(+)​-​Abscisic acid; ABA

    Endogenous Metabolite Proton Pump Metabolic Disease
    Abscisic acid ((S)-(+)-Abscisic acid), an orally active phytohormone in fruits and vegetables, is an endogenously produced mammalian hormone. Abscisic acid is a growth inhibitor and can regulate many aspects of plant growth and development. Abscisic acid inhibits proton pump (H +-ATPase) and leads to the plasma membrane depolarization in a Ca 2+-dependent manner. Abscisic acid, a LANCL2 natural ligand, is a potent insulin-sensitizing compound and has the potential for pre-diabetes, type 2 diabetes and metabolic syndrome.
  • HY-128449
    Cephradine monohydrate

    Cefradine monohydrate

    Bacterial Antibiotic TOPK Infection Inflammation/Immunology
    Cephradine (Cefradine) monohydrate is a broad-spectrum and orally active cephalosporin. Cephradine monohydrate is active against both grampositive and gram-negative pathogens and effective in eradicating most penicillinase-producing organisms known to be resistant to penicillin G, penicillin V, and ampicillin. Cephradine monohydrate has been used in the research of genitourinary, gastrointestinal and respiratory tract infections, and in infections of the skin and soft tissues. Cephradine monohydrate blocks solar-ultraviolet induced skin inflammation through direct inhibition of TOPK.
  • HY-146789
    PI3Kδ/γ-IN-2

    PI3K Cancer
    PI3Kδ/γ-IN-2 is a potent PI3Kδ and PI3Kγ dual inhibitor with IC50s of 1 nM and 4.3 nM, respectively. PI3Kδ/γ-IN-2 has favorable oral bioavailability. PI3Kδ/γ-IN-2 has potential for battling B-cell malignancies.
  • HY-13540
    E7016

    GPI 21016

    PARP Cancer
    E7016 (GPI 21016) is an orally available PARP inhibitor. E7016 can enhance tumor cell radiosensitivity in vitro and in vivo through the inhibition of DNA repair. E7016 acts as a potential anticancer agent.
  • HY-135747
    Gut restricted-7

    GR-7

    Bacterial Infection
    Gut restricted-7 (GR-7) is a potent, covalent and orally active pan-bile salt hydrolase (BSH) inhibitor. Gut restricted-7 has a tissue-selective and is restricted to the gut. Gut restricted-7 decreases gut bacterial BSHs and decreases deconjugated bile acid levels in feces of mice.
  • HY-145427
    NU5455

    DNA-PK Cancer
    NU5455 is a potent, selective, and orally active inhibitor of DNA-PKcs. NU5455 administration increases both the efficacy and the toxicity of a parenterally administered topoisomerase inhibitor. NU5455 enhances the activity of Doxorubicin released locally in liver tumor xenografts without inducing any adverse effect.
  • HY-19544
    JAK3-IN-1

    JAK Cancer
    JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC50 of 896 nM) and JAK2 (IC50 of 1050 nM).
  • HY-103258
    TC ASK 10

    MAP3K Apoptosis Cancer
    TC ASK 10 (Compound 10) is a potent, selective and orally active apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC50 of 14 nM. The inhibitory activities of TC ASK 10 towards other representative panel of kinases are less than 50%, except for ASK2 (IC50 of 0.51 μM).
  • HY-131034
    LP-922056

    Wnt Others
    LP-922056 is an orally active, highly potent Notum Pectinacetylesterase inhibitor with EC50s of 21 nM, 55 nM in human and mouse cellular assay, respectively. LP-922056 significantly increases midshaft femur cortical bone thickness in mice and rats.
  • HY-13556
    Arzoxifene

    LY353381; SERM III

    Estrogen Receptor/ERR Metabolic Disease
    Arzoxifene (LY353381) is an orally active selective estrogen receptor modulator with a fixed ring structure similar to raloxifene. Arzoxifene has minimal side effects with powerful antiestrogenic effects on breast cancer and endometrium, with equally strong favorable estrogenic effects on bone and lipid profile.
  • HY-136657
    SC-43

    Phosphatase STAT Apoptosis Cancer
    SC-43, a Sorafenib derivative, is a potent and orally active SHP-1 (PTPN6) agonist. SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis. SC-43 has anti-fibrotic and anticancer effects.
  • HY-101634
    ABT-072

    HCV Infection
    ABT-072 is an orally active and potent non-nucleoside HCV NS5B polymerase inhibitor (HCV GT1a EC50=1 nM; HCV GT1b EC50=0.3 nM).
  • HY-108766
    Ponatinib hydrochloride

    AP24534 hydrochloride

    Bcr-Abl FGFR PDGFR VEGFR Src Autophagy Cancer
    Ponatinib (AP24534) hydrochloride is a hydrochloride of ponatinib. Ponatinib is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
  • HY-10619B
    Niraparib tosylate

    MK-4827 tosylate

    PARP Apoptosis Cancer
    Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
  • HY-N2109
    Macranthoidin A

    Others Metabolic Disease
    Macranthoidin A is an orally active saponin from Flos Lonicerae. Macranthoidin A possess protection effects on hepatic injury caused by Acetaminophen, Cd, and CCl4, and conspicuous depressant effects on swelling of ear croton oil.
  • HY-14184
    Macitentan

    ACT-064992

    Endothelin Receptor Apoptosis Cardiovascular Disease Endocrinology Cancer
    Macitentan (ACT-064992) is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
  • HY-136527
    BMS-986251

    ROR Interleukin Related Inflammation/Immunology
    BMS-986251 is an orally active and selective RORγt inverse agonist with an EC50 of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC50 of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced (HY-B0180) models (preclinical models of psoriasis).
  • HY-144619
    TLR7/8 antagonist 2

    Toll-like Receptor (TLR) Inflammation/Immunology
    TLR7/8 antagonist 2 (Compound 15) is a potent and orally active agonist of TLR7/8 with IC50s of 4.9 and 0.6 nM, respectively. Inappropriate activation of TLR7 and TLR8 is linked to several autoimmune diseases, such as lupus erythematosus. TLR7/8 antagonist 2 has the potential for the research of autoimmune diseases.
  • HY-15670
    BMS-906024

    γ-secretase Notch Cancer
    BMS-906024 is an orally active and selective γ-secretase (gamma secretase) inhibitor. BMS-906024 is a potent pan-Notch receptors inhibitor with IC50s of 1.6 nM, 0.7 nM, 3.4 nM, and 2.9 nM for Notch1, -2, -3, and -4 receptors, respectively. BMS-906024 demonstrates broad-spectrum antineoplastic activity.
  • HY-137742
    SBP-7455

    ULK Autophagy Cancer
    SBP-7455 is a potent, high affinity and orally active dual ULK1/ULK2 autophagy inhibitor with IC50s of 13 nM and 476 nM in the ADP-Glo assays, respectively. SBP-7455 potently inhibits ULK1/2 enzymatic activity and can be used for triple-negative breast cancer (TNBC) research.
  • HY-17421
    Tenatoprazole

    TU-199

    Proton Pump Infection Inflammation/Immunology
    Tenatoprazole (TU-199) is an orally active imidazopyridine-based proton pump inhibitor with a prolonged plasma half-life. Tenatoprazole inhibits hog gastric H +/K +-ATPase activity with an IC50 of 6.2 μM. Tenatoprazole blocks the interaction of ubiquitin with the ESCRT-1 factor Tsg101, inhibits production of several enveloped viruses, including EBV.
  • HY-145953
    VY-3-135

    Others Cancer
    VY-3-135 is a potent, orally active, and stable ACSS2 inhibitor with an IC50 value of 44 nM. VY-3-135 is specific to ACSS2 among the AcCoA synthetase family of enzymes. VY-3-135 does not inhibit ACSS1 or ACSS3 enzymatic activity. VY-3-135 can be used for the research of breast cancer.
  • HY-145153
    S-777469

    Cannabinoid Receptor Neurological Disease
    S-777469 is a selective and orally available cannabinoid type 2 receptor (CB2) agonist with a Ki of 36 nM. S-777469 significantly suppresses compound 48/80-induced scratching behavior in mice in a dose-dependent manner. S-777469 produces its antipruritic effects by inhibiting itch signal transmission through CB2 agonism.
  • HY-16743
    Ibiglustat

    Venglustat; SAR402671; GZ402671

    Others Metabolic Disease
    Ibiglustat (Venglustat) is an orally active, brain-penetrant glucosylceramide synthase (GCS) inhibitor. Ibiglustat can be used for the research of Gaucher disease type 3, Parkinson's disease associated with GBA mutations, Fabry disease, GM2 gangliosidosis, and autosomal dominant polycystic kidney disease.
  • HY-15701B
    ADH-503

    (Z)-Leukadherin-1 choline

    Complement System Cancer
    ADH-503 ((Z)-Leukadherin-1 choline) is an orally active and allosteric CD11b agonist. ADH-503 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.
  • HY-101634A
    ABT-072 potassium trihydrate

    HCV Infection
    ABT-072 (potassium trihydrate) is an orally active and potent non-nucleoside HCV NS5B polymerase inhibitor (HCV GT1a EC50=1 nM; HCV GT1b EC50=0.3 nM).
  • HY-144656
    Steroid sulfatase-IN-1

    Others Cancer
    Steroid sulfatase-IN-1 is a potent and orally active Steroid sulfatase inhibitor with an IC50 of 1.71 µM. Steroid sulfatase-IN-1 shows antitumor activity (TGI=51%) in vivo. Steroid sulfatase-IN-1 has the potential for the research of breast cancer.
  • HY-135903
    Giredestrant tartrate

    GDC-9545 tartrate

    Estrogen Receptor/ERR Cancer
    Giredestrant tartrate (GDC-9545 tartrate), a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist. Giredestrant tartrate potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Anti-tumor activity.
  • HY-138563
    GSK973

    Epigenetic Reader Domain Cancer
    GSK973 is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5).
  • HY-144260
    3CPLro-IN-1

    SARS-CoV Infection
    3CPLro-IN-1 (compound A17) is a potent and orally active inhibitor of SARS-CoV-2 3CLpro with an IC50 of 5.65 μM. 3-Chymotrypsin-like cysteine protease (3CLpro) is an indispensable protein in viral replication and represents an attractive drug target for fighting COVID-19.
  • HY-133018
    HCV-IN-7

    HCV Infection
    HCV-IN-7 is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 has anti-viral activity.
  • HY-146684
    HDAC-IN-36

    HDAC Autophagy Apoptosis Cancer
    HDAC-IN-36 (compound 23 g) is an orally active and potent HDAC (histone deacetylase) inhibitor, with an IC50 of 11.68 nM (HDAC6). HDAC-IN-36 promotes apoptosis, autophagy and suppresses migration. HDAC-IN-36 shows anti-tumor and anti-metastatic activity, and can be used for breast cancer research.
  • HY-130208
    Thiodigalactoside

    TDG

    Galectin Cancer Metabolic Disease Inflammation/Immunology
    Thiodigalactoside (TDG) is an orally active and potent galectin (GAL) inhibitor with Kd values of 24 μM, 49 μM for GAL1 and GAL3, respectively. Thiodigalactoside, a non-metabolizable disaccharide, has anti-inflammatory and anti-cancer activity. Thiodigalactoside dramatically reduces body weight gain in diet-induced obese rats.
  • HY-133018A
    HCV-IN-7 hydrochloride

    HCV Cancer
    HCV-IN-7 hydrochloride is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 hydrochloride shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 hydrochloride has anti-viral activity.
  • HY-112852A
    TL02-59 dihydrochloride

    Src Apoptosis Cancer
    TL02-59 dihydrochloride is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM. TL02-59 dihydrochloride inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 dihydrochloride potently suppresses acute myelogenous leukemia (AML) cell growth.
  • HY-103493
    TAK-915

    Phosphodiesterase (PDE) Neurological Disease
    TAK-915 is a potent, selective, brain-penetrant and orally active phosphodiesterase 2A (PDE2A) inhibitor with an IC50 of 0.61 nM. TAK-915 is >4100-fold more selectivity for PDE2A than PDE1A. TAK-915 has the potential for neuropsychiatric and neurodegenerative disorders treatment.
  • HY-100851A
    LY-272015 hydrochloride

    5-HT Receptor Cardiovascular Disease
    LY-272015 hydrochloride is an orally active, specific 5-HT2B receptor antagonist. LY-272015 hydrochloride completely inhibits the phosphorylation of ERK2 induced by 5-HT or BW723C86. LY-272015 hydrochloride is antihypertensive in Deoxycorticosterone Acetate (DOCA)-salt-hypertensive rats.
  • HY-145280A
    IDO1/2-IN-1 hydrochloride

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO1/2-IN-1 hydrochloride (compound 4t) is the first potent IDO1/IDO2 dual inhibitor with IC50s of 28 nM and 144 nM for IDO1 and IDO2, respectively. IDO1/2-IN-1 hydrochloride exhibits antitumor activies. Orally active.
  • HY-145280
    IDO1/2-IN-1

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO1/2-IN-1 (compound 4t) is the first potent IDO1/IDO2 dual inhibitor with IC50s of 28 nM and 144 nM for IDO1 and IDO2, respectively. IDO1/2-IN-1 exhibits antitumor activies. Orally active.
  • HY-112852
    TL02-59

    Src Apoptosis Cancer
    TL02-59 is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM. TL02-59 inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 potently suppresses acute myelogenous leukemia (AML) cell growth.
  • HY-144309
    Cholesterol 24-hydroxylase-IN-1

    Cytochrome P450 Neurological Disease
    Cholesterol 24-hydroxylase-IN-1 (compound 17) is a potent, orally active, and highly selective cholesterol 24-hydroxylase (CH24H or CYP46A1) inhibitor (IC50=8.5 nM). Cholesterol 24-hydroxylase-IN-1 can cross blood-brain barrier.
  • HY-A0060
    Malotilate

    NKK 105

    Lipoxygenase Cancer
    Malotilate (NKK 105), an orally active hepatotropic agent and an anti-fibrotic substance, selectively inhibits the 5-lipoxygenase (5-LOX) (IC50=4.7 μM). Malotilate prevents the development of hepatocytic injury in alcohol-pyrazole hepatitis by decreasing hepatic acetaldehyde levels and preventing the retention of transferrin in the hepatocytes.
  • HY-139915
    MPO-IN-1

    Glutathione Peroxidase Inflammation/Immunology
    MPO-IN-1 is a potent, orally active, and irreversible indole-containing inhibitor of myeloperoxidase (MPO). MPO-IN-1 has IC50s of 2.6 μM and 5.3 μM for MPO and thyroid peroxidase (TPO), respectively. MPO-IN-1 inhibits MPO activity in an acute mouse model of inflammation.
  • HY-117658
    GSK-114

    Others Cardiovascular Disease
    GSK-114 is a highly selective, orally active TNNI3K inhibitor (IC50= 25 nM). GSK-114 shows a 40-fold selectivity for TNNI3K over B-Raf kinase (IC50= 1 µM). Cardiac troponin I-interacting kinase (TNNI3K or CARK) is a member of the tyrosine-like kinase family that is selectively expressed in heart tissue.
  • HY-134463
    NHWD-870

    Epigenetic Reader Domain Apoptosis Cancer
    NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation.
  • HY-A0027
    Fenspiride hydrochloride

    Histamine Receptor Phosphodiesterase (PDE) Inflammation/Immunology Endocrinology
    Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases.
  • HY-A0027A
    Fenspiride

    Histamine Receptor Phosphodiesterase (PDE) Inflammation/Immunology
    Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases.
  • HY-101903A
    BMS-309403 sodium

    FABP Metabolic Disease Cardiovascular Disease
    BMS-309403 sodium is a potent, orally active, and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor, with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 sodium interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 sodium improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells.
  • HY-101903
    BMS-309403

    FABP Metabolic Disease Cardiovascular Disease
    BMS-309403 is a potent, orally active and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells.
  • HY-123857
    JNJ-55308942

    P2X Receptor Inflammation/Immunology Neurological Disease
    JNJ-55308942 is a high-affinity, selective, brain-penetrant P2X7 functional antagonist (hP2X7: IC50=10 nM, Ki=7.1 nM; rP2X7: IC50=15 nM, Ki=2.9 nM). JNJ-55308942 is orally bioavailable, binds to brain P2X7 and blocks IL-1β release from adult rodent brain.
  • HY-138742
    HPK1-IN-7

    MAP4K Cancer
    HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1.
  • HY-132307
    Mcl-1 inhibitor 6

    Bcl-2 Family Apoptosis Cancer
    Mcl-1 inhibitor 6 is an orally active, selective myeloid cell leukemia 1 (Mcl-1) protein inhibitor with a Kd of 0.23 nM and a Ki of 0.02 μM. Mcl-1 inhibitor 6 possesses superior selectivity over other Bcl-2 family members (Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w, Kd>10 μM). Mcl-1 inhibitor 6 is a potent antitumor agent.
  • HY-10619
    Niraparib

    MK-4827

    PARP Apoptosis Cancer
    Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
  • HY-10619A
    Niraparib hydrochloride

    MK-4827 hydrochloride

    PARP Apoptosis Cancer
    Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
  • HY-117281
    Moexipril

    Angiotensin-converting Enzyme (ACE) Neurological Disease Cardiovascular Disease
    Moexipril is an orally active and potent angiotensin-converting enzyme (ACE) inhibitor. Moexipril can readily penetrate lipid membranes and thus target plasma and tissue ACE. Moexipril may improve endothelial dysfunction and exert neuroprotective effects. Moexipril can used for cardiovascular disease research.
  • HY-120536
    HPi1

    Bacterial Infection
    HPi1 is a potent, selective and orally active antimicrobial against Helicobacter pylori with an IC50 of 0.24 μM and an MIC of 0.08-0.16 μg/mL. HPi1 is inactive against other bacteria, including the gut commensals Lactobacillus casei, Lactobacillus reuteri, and Bifidobacterium longum.
  • HY-10999A
    Trametinib (DMSO solvate)

    GSK-1120212 (DMSO solvate); JTP-74057 (DMSO solvate)

    MEK Apoptosis Cancer
    Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib (DMSO solvate) activates autophagy and induces apoptosis.
  • HY-131343
    HBV-IN-4

    HBV DNA/RNA Synthesis Infection
    HBV-IN-4, a phthalazinone derivative, is a potent and orally active HBV DNA replication inhibitor with an IC50 of 14 nM. HBV-IN-4 induces the formation of genome-free capsids and has potent anti-HBV potencies.
  • HY-N10225
    Thielavin A

    Prostaglandin Receptor Endocrinology Cardiovascular Disease
    Thielavin A is an inhibitor of prostaglandin biosynthesis produced by Thielavia terricola. Thielavin A specifically inhibits the conversion of arachidonic acid into prostaglandin H2. Thielavin A has no anti-inflammatory activity on intravenous injection or on oral administration.
  • HY-144318
    CREB-IN-1 TFA

    Epigenetic Reader Domain Cancer
    CREB-IN-1 TFA is a potent, orally active CREB inhibitor (IC50=0.18 µM). CREB-IN-1 TFA inhibits breast cancer cell growth.
  • HY-15701A
    (Z)-Leukadherin-1

    ADH-503 free base

    Complement System Cancer
    (Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (Z)-Leukadherin-1 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.
  • HY-16743B
    Ibiglustat succinate

    Venglustat succinate; SAR402671 succinate; GZ402671 succinate

    Others Neurological Disease
    Ibiglustat (Venglustat) succinate is an orally active, brain-penetrant glucosylceramide synthase (GCS) inhibitor. Ibiglustat succinate can be used for the research of Gaucher disease type 3, Parkinson's disease associated with GBA mutations, Fabry disease, GM2 gangliosidosis, and autosomal dominant polycystic kidney disease.
  • HY-100459
    GSK3179106

    RET Metabolic Disease Inflammation/Immunology
    GSK3179106 is an orally active and selective RET kinase inhibitor with IC50s of 0.4 nM, 0.2 nM for human RET and rat RET, respectively. GSK3179106 has the potential for irritable bowel syndrome (IBS) through the attenuation of post-inflammatory and stress-induced visceral hypersensitivity.
  • HY-114153
    PLX5622

    c-Fms Neurological Disease
    PLX5622 is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 µM; Ki=5.9 nM). PLX5622 allows for extended and specific microglial elimination, preceding and during pathology development. PLX5622 demonstrates desirable PK properties in varies animals.
  • HY-114452A
    LY2940094 tartrate

    BTRX-246040 tartrate

    Opioid Receptor Neurological Disease
    LY2940094 (BTRX-246040) tartrate is a potent, brain penetrant, selective and orally available N/OFQ peptide (NOP) receptor antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 tartrate reduces Ethanol self-administration and Ethanol seeking in animal models.
  • HY-130187
    Sapienic acid

    Bacterial Infection
    Sapienic acid is a fatty acid commonly found on the skin and in mucosa. Sapienic acid has variable antimicrobial activities against Gram-positive and Gram-negative bacteria found on the skin and in the oral cavity. Sapienic acid is active against Streptococcus sanguinis, Streptococcus mitis and Fusobacterium nucleatum with MBC values of 31.3 μg/mL, 375.0 μg/mL and 93.8 μg/mL, respectively.
  • HY-146886
    FLT3-IN-15

    FLT3 Cancer
    FLT3-IN-15 is a highly potent and orally active FLT3 inhibitor with IC50s of 0.87 nM and 0.32 nM for FLT3 and FLT3/D835Y, respectively. FLT3-IN-15 can be used for researching acute myeloid leukemia.
  • HY-116830
    BRD0705

    GSK-3 Cancer
    BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) research.
  • HY-104066
    Theliatinib

    Xiliertinib; HMPL-309

    EGFR Cancer
    Theliatinib (Xiliertinib) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases. Anti-tumor activity.
  • HY-145685
    RECQL5-IN-1

    Others Cancer
    RECQL5-IN-1 (Compound 4a) acts as an orally effective RECQL5 inhibitor (targeting both enzymatic and nonenzymatic domain). RECQL5-IN-1 is a potent inhibitor of RECQL5 helicase activity (IC50=46.3 nM). RECQL5-IN-1 inhibits RECQL5-WT cells and RECQL5-KO2 cells with IC50s of 4.8 μM and 19.6 μM, respectively. RECQL5-IN-1 can be used for the research of breast cancer.
  • HY-145259
    HDAC6-IN-3

    HDAC Histone Demethylase Cancer
    HDAC6-IN-3 (Compound 14), an antiprostate cancer agent, is a potent, orally active HDAC6 inhibitor with IC50s ranging from 0.02-1.54 μM for HDAC1/2/3/6/8/10. HDAC6-IN-3 is also an effective MAO-A (IC50=0.79 μM) and LSD1 inhibitor.
  • HY-130609
    Aβ42-IN-1

    γ-secretase Neurological Disease
    Aβ42-IN-1, compound 1v, is a novel, potent and orally active γ-secretase modulator (GSM). Aβ42-IN-1 potently reduced Aβ42 levels with an IC50 value of 0.091 µM without CYP3A4 inhibition. Aβ42-IN-1 shows a sustained pharmacokinetic profile.
  • HY-12085
    Apremilast

    CC-10004

    Phosphodiesterase (PDE) Apoptosis TNF Receptor Inflammation/Immunology
    Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM.
  • HY-139605
    GLUT inhibitor-1

    GLUT Cancer Inflammation/Immunology
    GLUT inhibitor-1 is a potent and orally active inhibitor of glucose transporters, targeting both GLUT1 and GLUT3, with IC50s of 242 nM and 179 nM, respectively. GLUT inhibitor-1 has the potential for the reaesrch of cancers and autoimmune diseases.
  • HY-144107
    HCV-IN-34

    HCV Infection
    HCV-IN-34 (compound 3i) is an orally active and potent HCV entry inhibitor. HCV-IN-35 shows excellent antiviral activity, with an EC50 of 0.010 μM and a CC50 (half-maximal cytotoxic concentration) of 8.23 μM.
  • HY-122700
    Factor D inhibitor 6

    Complement System Inflammation/Immunology
    Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC50 of 30 nM and a Kd of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases.
  • HY-142520
    I-BET567

    Epigenetic Reader Domain Cancer Inflammation/Immunology
    I-BET567 is a potent and orally active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation.
  • HY-15178
    Oglemilast

    GRC 3886

    Phosphodiesterase (PDE) Inflammation/Immunology
    Oglemilast (GRC 3886) is a potent and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 of 0.5 nM for PDE4D3. Oglemilast inhibits pulmonary cell infiltration, including eosinophilia and neutrophilia in vitro and in vivo. Oglemilast has the potential for inflammatory airway diseases.
  • HY-106697
    Ponalrestat

    ICI 128436

    Aldose Reductase Metabolic Disease
    Ponalrestat (ICI 128436) is an orally active, selective and noncompetitive aldose reductase (AKR1B1; ALR) inhibitor. Ponalrestat selectively inhibits ALR2 (Ki=7.7 nM) over ALR1 (Ki=60 μM). Ponalrestat inhibits the conversion of glucose to sorbitol.
  • HY-145829
    Tofacitinib Prodrug-1

    JAK Apoptosis Inflammation/Immunology
    Tofacitinib Prodrug-1 is an effective and oral active prodrug to mitigate the systemic adverse effects of Tofacitinib. Tofacitinib Prodrug-1 can effectively attenuate the oxazolone-induced colitis in mice model with low toxicity. Tofacitinib Prodrug-1 is a potential drug candidate for the treatment of ulcerative colitis.
  • HY-137371
    Lactonic sophorolipid

    Bacterial Apoptosis Antibiotic Cancer Infection
    Lactonic sophorolipid is a natural antimicrobial surfactant for oral hygiene. Lactonic sophorolipid, a potential anticancer agent, induces apoptosis in human HepG2 cells through the caspase-3 pathway.
  • HY-115986
    MAO-B-IN-5

    Monoamine Oxidase Neurological Disease
    MAO-B-IN-5 is a potent, selective and orally active MAO-B inhibitor with an IC50 of 0.204 µM. MAO-B-IN-5 has the potential for the research of Parkinson's disease (PD).
  • HY-14806S
    Teneligliptin D8

    MP-513 D8

    Dipeptidyl Peptidase Cardiovascular Disease
    Teneligliptin D8 (MP-513 D8) a deuterium labeled Teneligliptin (MP-513). Teneligliptin is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor.
  • HY-15196
    TAK-285

    EGFR Cancer
    TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity. TAK-285 can cross the blood-brain barrier (BBB).
  • HY-13208
    Xevinapant hydrochloride

    AT-406 hydrochloride; Debio 1143 hydrochloride; SM-406 hydrochloride

    IAP Cancer
    Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with Kis of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors.
  • HY-108425A
    AMG8380

    Sodium Channel Neurological Disease
    AMG8380, an orally active and less active enantiomer of AMG8379, can serves as a negative control. AMG8380 inhibits human and mouse voltage-gated sodium channel NaV1.7 with IC50s of 0.907 and 0.387 μM, respectively. AMG8380 blocks Tetrodotoxin (TTX)-sensitive native channels with an IC50 of 2560 nM.
  • HY-106993A
    Cipralisant maleate

    GT-2331 maleate

    Histamine Receptor Neurological Disease
    Cipralisant (GT-2331) (maleate) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor. Cipralisant (maleate) has the potential for attention-deficit hyperactivity disorder research.
  • HY-144263
    3CPLro-IN-2

    SARS-CoV Infection
    3CPLro-IN-2 (compound C1) is a potent and orally active inhibitor of SARS-CoV-2 3CLpro with an IC50 and Ki of 1.55 and 6.09 μM, respectively. 3-Chymotrypsin-like cysteine protease (3CLpro) is an indispensable protein in viral replication and represents an attractive drug target for fighting COVID-19.
  • HY-114153A
    PLX5622 hemifumarate

    c-Fms Neurological Disease
    PLX5622 hemifumarate is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 µM; Ki=5.9 nM). PLX5622 hemifumarate allows for extended and specific microglial elimination, preceding and during pathology development. PLX5622 hemifumarate demonstrates desirable PK properties in varies animals.
  • HY-100017
    BAY-876

    GLUT Cancer
    BAY-876 is an orally active and selective glucose transporter 1 (GLUT1) inhibitor with an IC50 of 2 nM. BAY-876 is >130-fold more selective for GLUT1 than GLUT2, GLUT3, and GLUT4. BAY-876 is also a potent blocker of glycolytic metabolism and ovarian cancer growth.
  • HY-106993
    Cipralisant

    GT-2331

    Histamine Receptor Neurological Disease Endocrinology
    Cipralisant (GT-2331) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor. Cipralisant has the potential for attention-deficit hyperactivity disorder research.
  • HY-15652
    Freselestat

    ONO-6818; ONO-PO-736

    Elastase Inflammation/Immunology
    Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat has a potent anti-inflammatory activity.
  • HY-111817
    ACT-451840

    Parasite Infection
    ACT-451840 is an orally active, potent and low-toxicity compound, showing activity against sensitive and resistant plasmodium falciparum strains. ACT-451840 targets all asexual blood stages of the parasite, has a rapid onset of action. ACT-451840 behaves in a way similar to artemisinin derivatives, with very rapid onset of action and elimination of parasite. ACT-451840 can be used for the research of malarial.
  • HY-B0731A
    Perospirone

    SM-9018 free base

    5-HT Receptor Dopamine Receptor Neurological Disease
    Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT2A receptor (Ki=0.6 nM) and dopamine D2 receptor (Ki=1.4 nM), and also a partial agonist of 5-HT1A receptor (Ki=2.9 nM). Perospirone is an atypical antipsychotic agent and has the potential for schizophrenic disease research.
  • HY-146012
    HIV-1 protease-IN-4

    HIV Infection
    HIV-1 protease-IN-4 (Compound II-22) is a potent HIV-1 protease inhibitor. HIV-1 protease-IN-4 is a prodrug of atazanavir. HIV-1 protease-IN-4 as a prodrug that delivers the parent 1 to rat plasma with a 5-fold higher AUC and 67-fold higher C24 when compared to oral administration of the parent drug.
  • HY-115885
    XP5

    HDAC Cancer Inflammation/Immunology
    XP5 is a potent, orally active HDAC6 inhibitor with an IC50 of 31 nM. XP5 displays high antiproliferative activity against various cancer cell lines including the HDACi-resistant YCC3/7 gastric cancer cells (IC50=0.16-2.31 μM). XP5 enhances antitumor immunity when combined with a PD-L1 inhibitor in melanoma.
  • HY-143444
    JAK-IN-20

    JAK Inflammation/Immunology
    JAK-IN-20 is a potent, pan and orally active JAK inhibitor with an IC50s of 7 nM, 5 nM, 14 nM for JAK1, JAK2, JAK3, respectively. JAK-IN-20 shows excellent pharmacokinetics and displays anti-inflammatory efficacy in vivo.
  • HY-135299
    CH6953755

    Src Cancer
    CH6953755 is a potent, orally active and selective YES1 kinase (a member of the SRC family) inhibitor with an IC50 of 1.8 nM. CH6953755 inhibits YES1 kinase, leading to antitumor activity against YES1 Gene -amplified cancers in vitro and in vivo.
  • HY-144254
    PI3Kδ-IN-10

    PI3K Akt Apoptosis Cancer
    PI3Kδ-IN-10 is a highly potent and orally active PI3Kδ inhibitor with IC50 of 2 nM. PI3Kδ-IN-10 robustly suppresses the downstream AKT pathway to induce subsequent apoptosis in hepatocellular carcinoma models.
  • HY-16743A
    Ibiglustat (L-Malic acid)

    Venglustat (L-Malic acid); SAR402671 (L-Malic acid); GZ402671 (L-Malic acid)

    Others Metabolic Disease
    Ibiglustat (Venglustat) L-Malic acid is an orally active, brain-penetrant glucosylceramide synthase (GCS) inhibitor. Ibiglustat L-Malic acid can be used for the research of Gaucher disease type 3, Parkinson's disease associated with GBA mutations, Fabry disease, GM2 gangliosidosis, and autosomal dominant polycystic kidney disease.
  • HY-132300
    ZW4864

    β-catenin Cancer
    ZW4864 is an orally active and selective β catenin/B-Cell lymphoma 9 protein−protein interaction (β catenin/BCL9 PPI) inhibitor. ZW4864 inhibits β catenin/BCL9 PPI with a Ki value of 0.76 μM and an IC50 value of 0.87 μM.
  • HY-145564
    Emprumapimod

    PF-07265803

    p38 MAPK Inflammation/Immunology Cardiovascular Disease
    Emprumapimod is a potent, orally bioavailable and selective inhibitor of p38α MAPK directly inhibits LPS-induced IL-6 production from RPMI-8226 cell (IC50=100 pM). Emprumapimod can be used for the research of dilated cardiomyopathy and acute inflammatory pain.
  • HY-100433
    PACMA 31

    Others Cancer
    PACMA 31 is an irreversible, orally active protein disulfide isomerase (PDI) inhibitor with an IC50 of 10 μM. PACMA 31 forms a covalent bond with the active site cysteines of PDI. PACMA 31 shows tumor targeting ability and significantly suppresses ovarian tumor growth without causing toxicity to normal tissues.
  • HY-12047S
    Ponatinib-d8

    AP24534-d8

    Bcr-Abl PDGFR VEGFR FGFR Src Autophagy Cancer
    Ponatinib D8 (AP24534 D8) is a deuterium labeled Ponatinib. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
  • HY-108260
    Deferitrin

    GT-56-252

    Others Cardiovascular Disease
    Deferitrin (GT-56-252), a desferrithiocin (DFT) analogue, is an orally active trident iron chelator. Deferitrin is used for chronic iron overload due to transfusional therapy. Deferitrin has the potential for beta-thalassemia major.
  • HY-13580
    Budesonide

    Glucocorticoid Receptor Cancer Inflammation/Immunology
    Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma.
  • HY-19599
    Vorozole

    (+)-Vorozole; R83842

    Aromatase Cancer
    Vorozole is a potent and selective, orally active non-steroidal aromatase inhibitor. Vorozole shows antitumor activity in vivo. Vorozole has the potential for the research of mammary cancer.
  • HY-121383
    Labetalol

    AH5158; Sch-15719W free base

    Adrenergic Receptor Inflammation/Immunology Cardiovascular Disease
    Labetalol (AH5158) is an orally active selective α1- and non-selective β-adrenergic receptors competitive antagonist. Labetalol, an anti-hypertensive agent, can be used for the research of cardiovascular disease, such as hypertension in pregnancy.
  • HY-139609
    RP-3500

    ATR inhibitor 4

    ATM/ATR mTOR Cancer
    RP-3500 (ATR inhibitor 4) is an orally active, selective ATR kinase inhibitor (ATRi) with an IC50 of 1.00 nM in biochemical assays. RP-3500 shows 30-fold selectivity for ATR over mTOR (IC50=120 nM) and >2,000-fold selectivity over ATM, DNA-PK, and PI3Kα kinases. RP-3500 has potent antitumor activity.
  • HY-145284
    APJ receptor agonist 4

    Others Cardiovascular Disease
    APJ receptor agonist 4 is a potent and orally active agonist of apelin receptor (APJ) with EC50 and Ki of 0.06 nM and 0.07 nM respectively. APJ receptor agonist 4 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 4 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 4 leads to improved cardiac function and can be used for researching the HF disease.
  • HY-125390
    SM-360320

    CL-087

    Toll-like Receptor (TLR) Inflammation/Immunology
    SM-360320 (CL-087) is a potent, oral actively TLR7 agonist. SM-360320 is a mmuno-modulator and exerts an antitumor effect. SM-360320 can act in synergy with DNA vaccines leading to an enhanced Th1 antibody response. SM-360320 can inhibit HCV replication in hepatocytes via a type I IFN-independent mechanism in addition to its IFN-mediated activity.
  • HY-116594A
    OPC-14523 hydrochloride

    Sigma Receptor 5-HT Receptor Neurological Disease
    OPC-14523 hydrochloride is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 hydrochloride shows antidepressant-like activity.
  • HY-B0121B
    Sumatriptan

    GR 43175 free base

    5-HT Receptor Neurological Disease
    Sumatriptan (GR 43175 free base) is an orally active 5-HT1 receptor agonist with Kis of 17 nM, 27 nM and 100 nM for 5-HT1D, 5-HT1B and 5-HT1A receptors, respectively. Sumatriptan can be used for migraine headache research.
  • HY-136895
    AZ12672857

    Prostaglandin Receptor Cancer
    AZ12672857 is an orally active inhibitor of EphB4 (IC50=1.3 nM) and Src kinases. AZ12672857 shows good inhibition of proliferation of c-Src transfected 3T3 cells (IC50=2 nM) as well as autophosphorylation of EphB4 in transfected CHO-K1 cells (IC50=9 nM).
  • HY-129388A
    Pulrodemstat

    CC-90011; LSD1-IN-7

    Histone Demethylase Cancer
    Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
  • HY-145697
    GPR84 antagonist 2

    GPR84 Inflammation/Immunology
    GPR84 antagonist 2 (compound 33) is a potent, selective, and orally active GPR84 antagonist (IC50=8.95 nM). GPR84 antagonist 2 shows improved potency in the calcium mobilization assay and the ability to inhibit the chemotaxis of neutrophils and macrophages upon GPR84 activation. GPR84 antagonist 2 has the potential for the research of ulcerative colitis.
  • HY-B0121
    Sumatriptan succinate

    GR 43175

    5-HT Receptor Neurological Disease
    Sumatriptan succinate (GR 43175) is an orally active 5-HT1 receptor agonist with Kis of 17 nM, 27 nM and 100 nM for 5-HT1D, 5-HT1B and 5-HT1A receptors, respectively. Sumatriptan succinate can be used for migraine headache research.
  • HY-14165
    Veliflapon

    BAY X 1005; DG-031

    FLAP Leukotriene Receptor Inflammation/Immunology Cardiovascular Disease
    Veliflapon (BAY X 1005; DG-031) is an orally active and selective 5-lipoxygenase activating protein (FLAP) inhibitor. Veliflapon inhibits the synthesis of the leukotrienes B4 and C4.
  • HY-145835
    PERK-IN-5

    PERK Cancer
    PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC50s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model.
  • HY-116218
    Amelparib

    JPI-289

    PARP Neurological Disease Cardiovascular Disease
    Amelparib is a potent, orally active, and water-soluble inhibitor of PARP-1. Amelparib inhibits PARP-1 activity (IC50 =18.5 nmol/L) and cellular PAR formation (IC50 =10.7 nmol/L) in the nanomolar range. Amelparib is a potential neuroprotective agent. Amelparib has the potential for the research of acute ischaemic stroke.
  • HY-112037
    IACS-010759

    IACS-10759

    Mitochondrial Metabolism Apoptosis Cancer
    IACS-010759 is an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 inhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 has the potential for relapsed/refractory AML and solid tumors research.
  • HY-145702
    MAP855

    MEK ERK Cancer
    MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC50=3 nM, pERK EC50=5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2.
  • HY-15779
    K145

    SphK Apoptosis Cancer
    K145 is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. K145 is inactive against SphK1 and other protein kinases. K145 induces cell apoptosis and has potently antitumor activity.
  • HY-15779A
    K145 hydrochloride

    SphK Apoptosis Cancer
    K145 hydrochloride is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. K145 hydrochloride is inactive against SphK1 and other protein kinases. K145 hydrochloride induces cell apoptosis and has potently antitumor activity.
  • HY-144109
    HCV-IN-36

    HCV Infection
    HCV-IN-36 (compound (S)-3h) is an orally active and potent HCV entry inhibitor. HCV-IN-36 shows excellent antiviral activity, with an EC50 of 0.016 μM and a CC50 (half-maximal cytotoxic concentration) of 8.78 μM.
  • HY-106080A
    Furegrelate sodium

    U-63557A

    Others Cardiovascular Disease
    Furegrelate Sodium (U-63557A) is a potent, orally available, and selective thromboxane synthase inhibitor. Furegrelate Sodium inhibits human platelet microsomal thromboxane A2 (TxA2) synthase with an IC50 of 15 nM. Furegrelate Sodium is being developed as an antiplatelet agent.
  • HY-100507
    Avadomide

    CC 122

    E1/E2/E3 Enzyme Apoptosis Cancer Inflammation/Immunology
    Avadomide (CC 122) is an orally active cereblon modulator. Avadomide modulates cereblon E3 ligase activity and induces apoptosis of diffuse large B-cell lymphoma (DLBCL) cell lines. Avadomide exhibits potent antitumor and immunomodulatory activities.
  • HY-125351
    SPT-IN-1

    Others Metabolic Disease
    SPT-IN-1 (compound 1) is an orally active and potent SPT (serine palmitoyl transferase) inhibitor, with an IC50 of 5.19 nM for hSPT1. SPT-IN-1 can be used for type 2 diabetes and dyslipidemia research.
  • HY-102074
    ERDRP-0519

    Others Infection
    ERDRP-0519, an orally bioavailable small-molecule Measles virus (MeV) polymerase inhibitor, prevents measles disease in squirrel monkeys (Saimiri sciureus). ERDRP-0519 inhibits morbilliviruses with nanomolar potency..
  • HY-101246
    RPI-1

    RET Cancer
    RPI-1 is a specific, orally available 2-indolinone Ret tyrosine kinase inhibitor. RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT in human medullary thyroid carcinoma TT cells. Antitumor activity.
  • HY-121852
    SCH 336

    SCH-225336

    Cannabinoid Receptor Inflammation/Immunology
    SCH 336 is a potent, selective, inverse and orally active CB2 agonist. SCH 336 inhibits BaF3/CB2 migration. SCH 336 significantly inhibits the migration of leukocytes in vivo. SCH 336 blocks ovalbumin-induced lung eosinophilia in mice.
  • HY-N6967
    Levomenol

    (-)-α-Bisabolol

    Apoptosis Inflammation/Immunology Neurological Disease
    Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active.
  • HY-15652A
    Freselestat quarterhydrate

    ONO-6818 quarterhydrate; ONO-PO-736 quarterhydrate

    Elastase Inflammation/Immunology
    Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat quarterhydrate is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat quarterhydrate has a potent anti-inflammatory activity.
  • HY-145594
    Safusidenib

    Isocitrate Dehydrogenase (IDH) Cancer
    Safusidenib is an orally bioavailable, selective mutant IDH1 inhibitor. Safusidenib strongly inhibits mutant IDH1 but not wild-type IDH1. Safusidenib impairs tumor activity in chondrosarcoma. Safusidenib exhibits activity against IDH1R132H, and IDH1R132C with IC50s of 15, and 130 nM in assays without any preincubation, respectively.
  • HY-144743
    ATX inhibitor 12

    Phosphodiesterase (PDE) Others
    ATX inhibitor 12 (compound 20) is an orally active and potent ATX (autotaxin) inhibitor, with an IC50 of 1.72 nM. ATX inhibitor 12 effectively alleviates lung structural damage with fewer fibrotic lesions at an oral dose of 60 mg/kg in C57Bl/6J mice. ATX inhibitor 12 can be uesd for idiopathic pulmonary fibrosis (IPF) research.
  • HY-132300A
    ZW4864 free base

    β-catenin Cancer
    ZW4864 (free base) is an orally active and selective β catenin/B-Cell lymphoma 9 protein−protein interaction (β catenin/BCL9 PPI) inhibitor. ZW4864 (free base) inhibits β catenin/BCL9 PPI with a Ki value of 0.76 μM and an IC50 value of 0.87 μM.
  • HY-122218
    JHU-083

    Glutaminase Neurological Disease
    JHU-083, a prodrug of 6-diazo-5-oxo-L-norleucine (DON; HY-108357), is an orally active and selective glutaminase antagonist. JHU-083 blocks glutaminase activity in brain CD11b + cells and experimental cerebral malaria (ECM) resulting in a net decrease of glutamate levels in the animals.
  • HY-136789
    Tuxobertinib

    BDTX-189

    EGFR Cancer
    Tuxobertinib (BDTX-189) is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, including EGFR/HER2 exon 20 insertion mutants. Tuxobertinib shows KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity.
  • HY-130187A
    Sapienic acid sodium

    Bacterial Infection
    Sapienic acid sodium is a fatty acid commonly found on the skin and in mucosa. Sapienic acid sodium has variable antimicrobial activities against Gram-positive and Gram-negative bacteria found on the skin and in the oral cavity. Sapienic acid sodium is active against Streptococcus sanguinis, Streptococcus mitis and Fusobacterium nucleatum with MBC values of 31.3 μg/mL, 375.0 μg/mL and 93.8 μg/mL, respectively.
  • HY-112037A
    IACS-010759 hydrochloride

    IACS-10759 hydrochloride

    Mitochondrial Metabolism Apoptosis Cancer
    IACS-010759 hydrochlorideis an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 hydrochlorideinhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 hydrochloride has the potential for relapsed/refractory AML and solid tumors research.
  • HY-144893
    OKI-006

    HDAC Cancer
    OKI-006 is a potent and orally active inhibitor of histone deacetylase (HDAC). OKI-006 is a unique congener of the natural product HDAC inhibitor largazole. Histone deacetylases (HDACs) play critical roles in epigenomic regulation, and histone acetylation is dysregulated in many human cancers. OKI-006 has the potential for the research of cancer disease.
  • HY-103442
    CGP52411

    DAPH

    EGFR Amyloid-β Cancer Neurological Disease
    CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC50 of 0.3 μM. CGP52411 blocks the toxic influx of Ca 2+ ions into neuronal cells, and dramatic inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates associated with Alzheimer's disease.
  • HY-116399
    MMP-2/MMP-9-IN-1

    MMP Cancer
    MMP-2/MMP-9-IN-1 is a highly selective, orally active and potent type IV collagenase (MMP-9 and MMP-2) inhibitor with IC50s of 0.24 and 0.31 μM for MMP-9 and MMP-2, respectively. MMP-2/MMP-9-IN-1 is orally active in animal models of tumor growth and metastasis. MMP-2/MMP-9-IN-1 can be used for the research of cancer.
  • HY-145628
    CM398

    Sigma Receptor Inflammation/Immunology Neurological Disease
    CM398 is a highly selective, orally active sigma-2 receptor ligand (Ki=0.43 nM), with high sigma-1/sigma-2 selectivity rato (1000-fold). CM398 shows notable affinity for dopamine (Ki=32.90 nM) and serotonin transporters (Ki=244.2 nM). CM398 shows promising anti-inflammatory analgesic effects in the formalin model of inflammatory pain in mice.
  • HY-132291
    HIV-1 inhibitor-8

    HIV Infection
    HIV-1 inhibitor-8 is an orally active, low-toxicity and potent HIV‑1 non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV-1 inhibitor-8 yields exceptionally potent antiviral activities (EC50=4.44~54.5 nM) against various HIV‑1 strains. The IC50 of HIV-1 inhibitor-8 against WT HIV-1 reverse transcriptase is 0.081 μM.
  • HY-130609A
    Aβ42-IN-1 free base

    γ-secretase Neurological Disease
    Aβ42-IN-1 free base (compound 1v) is an orally active, high brain exposure γ-secretase modulator. Aβ42-IN-1 free base potently reduces Aβ42 levels with an IC50 value of 0.091 µM, and significantly reduces brain Aβ42 levels in mice. Aβ42-IN-1 free base is a promising compound for the treatment of Alzheimer’s disease.
  • HY-120124
    Samelisant

    SUVN-G3031

    Histamine Receptor Neurological Disease
    Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders.
  • HY-108482
    CP-96,345

    Neurokinin Receptor Inflammation/Immunology Neurological Disease
    CP-96,345 is a specific, highly potent, and orally active tachykinin and substance P receptor non-peptide inhibitor. CP-96,345 prevents the drop in blood pressure evoked by substance P and neurokinin A. CP-96,345 can be used for researching neurogenic inflammation.
  • HY-143264
    FAAH/MAGL-IN-2

    FAAH MAGL Neurological Disease
    FAAH/MAGL-IN-2 is a potent, reversible, orally active, and cross the blood-brain barrier FAAH and MAGL inhibitor with IC50s of 11 nM and 36 nM (Kis of 28 nM and 60 nM), respectively . FAAH/MAGL-IN-2 has the potential to treat neuropathic pain without causing locomotion impairment.
  • HY-14973
    Vidupiprant

    AMG 853

    Prostaglandin Receptor Inflammation/Immunology
    Vidupiprant (AMG 853) is a phenylacetic acid derivative. Vidupiprant is a potent and orally active CRTH2 (DP2) and prostanoid D receptor (DP or DP1) dual antagonist with IC50s of 3 nM and 4 nM in buffer, and 8 nM and 35 nM in human plasma, respectively. Vidupiprant has the potential for asthma treatment.
  • HY-14184S
    Macitentan-d4

    ACT-064992-d4

    Endothelin Receptor Apoptosis Cardiovascular Disease
    Macitentan D4 (ACT-064992 D4) is a deuterium labeled Sulfamethoxazole. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin) receptor antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
  • HY-14806
    Teneligliptin

    MP-513

    Dipeptidyl Peptidase Metabolic Disease
    Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM.
  • HY-139439
    SBI-581

    Others Cancer
    SBI-581 is an orally active and potent selective serine-threonine kinase TAO3 inhibitor, with an IC50 of 42 nM. SBI-581 promotes TKS5α accumulation at RAB11-positive vesicles. SBI-581 inhibits invadopodia formation. SBI-581 shows reasonable pharmacokinetics in mice using IP injection. SBI-581 shows antitumor activity.
  • HY-129388B
    Pulrodemstat benzenesulfonate

    CC-90011 benzenesulfonate; LSD1-IN-7 benzenesulfonate

    Histone Demethylase Cancer
    CC-90011 benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 benzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
  • HY-146121
    Antitubercular agent-26

    Bacterial Infection
    Antitubercular agent-26 (Compound 32) is an orally active anti-tubercular agent with an extracellular IC50 of 0.50 μM and an intracellular IC50 of 0.51 μM against M. tuberculosis H37Rv. Antitubercular agent-26 shows good metabolic stability, low risk of cardiotoxicity and no genotoxicity.
  • HY-144614
    JH-XVII-10

    DYRK Apoptosis Cancer Neurological Disease
    JH-XVII-10 is a potent, selective and orally active DYRK1A and DYRK1B inhibitor with IC50s of 3 nM and 5 nM for DYRK1A and DYRK1B, respectively. JH-XVII-10 shows antitumor efficacy in neck squamous cell carcinoma (HNSCC) cell lines.
  • HY-101870B
    Uzansertib phosphate

    INCB053914 phosphate

    Pim Cancer
    Uzansertib (INCB053914) phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines.
  • HY-101870
    Uzansertib

    INCB053914

    Pim Cancer
    Uzansertib (INCB053914) is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib has broad anti-proliferative activity against a variety of hematologic tumor cell lines.
  • HY-101402
    Cyclo(his-pro)

    Cyclo(histidyl-proline); Histidylproline diketopiperazine

    NF-κB Endogenous Metabolite Inflammation/Immunology Neurological Disease
    Cyclo(his-pro) (Cyclo(histidyl-proline)) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) could inhibit NF-κB nuclear accumulation. Cyclo(his-pro) can cross the brain-blood-barrier and affect diverse inflammatory and stress responses.
  • HY-144766
    ATX inhibitor 13

    Apoptosis Others Cancer
    ATX inhibitor 13 (10c) is an orally active and potent ATX inhibitor, with an IC50 of 3.4 nM. ATX inhibitor 13 inhibits proliferation and migration, and induces apoptosis and G2 phase arrest in RAW264.7 cells. ATX inhibitor 13 suppresses tumor cell colony formation.
  • HY-132303
    MK-8262

    CETP Metabolic Disease Cardiovascular Disease
    MK-8262 is an orally active and potent cholesteryl ester transfer protein (CETP) inhibitor with an IC50 of 53 nM and a log D of 5.3. MK-8262, a bistrifluoromethyl analogue, has the potential for coronary heart disease (CHD) correlated high-density lipoprotein (HDL) and low-density lipoprotein (LDL) research.
  • HY-116000
    Glumetinib

    SCC244

    c-Met/HGFR Cancer
    Glumetinib (SCC244) is a highly selective, orally bioavailable, ATP-competitive c-Met inhibitor with an IC50 of 0.42 nM. Glumetinib has greater than 2400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, TyrO3. Antitumor activity.
  • HY-146466
    Anticancer agent 61

    Others Cancer
    Anticancer agent 61 (compound 3v) is an orally active and potent anticancer agent. Anticancer agent 61 shows antiproliferative activity in HepG2, Bel-7402 and MCF-7 cancer cells, with IC50 values of 1.12, 1.97 and 1.08 μM, respectively. Anticancer agent 61 shows effective tumor growth inhibition.
  • HY-B0731
    Perospirone hydrochloride

    SM-9018

    5-HT Receptor Dopamine Receptor Neurological Disease
    Perospirone hydrochloride (SM-9018) is an orally active antagonist of 5-HT2A receptor (Ki of 0.6 nM) and dopamine D2 receptor (Ki of 1.4 nM). Perospirone hydrochloride is also a partial agonist of 5-HT1A receptor (Ki of 2.9 nM). Perospirone hydrochloride is an atypical antipsychotic agent and has the potential for schizophrenic disease research.
  • HY-109016
    Valnivudine

    FV-100 free base

    Antibiotic Bacterial Infection
    Valnivudine (FV-100 free base), a prodrug of CF-1743, is an orally active anti-herpes zoster (HZ) nucleoside analogue. CF-1743, a bicyclic nucleoside analog (BCNA), has highly specific antiviral activity against varicella-zoster virus (VZV). Valnivudine is rapidly and extensively converted to CF-1743 in vivo.
  • HY-136300
    PHD-1-IN-1

    HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology Cardiovascular Disease
    PHD-1-IN-1 is an orally active and potent HIF prolylhydroxylase domain-1 (PHD-1) inhibitor with an IC50 of 0.034 μM. PHD-1-IN-1 has a unique monodentate binding interaction with the active site Fe 2+ ion and induces the formation of an “Arg367-out” pocket.
  • HY-101189
    JNJ-39758979

    Histamine Receptor Neurological Disease Endocrinology
    JNJ-39758979 is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity.
  • HY-101189B
    JNJ-39758979 dihydrochloride

    Histamine Receptor Inflammation/Immunology
    JNJ-39758979 dihydrochloride is a selective, orally active, and high-affinity histamine H4 receptor antagonist, with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 dihydrochloride functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 dihydrochloride shows good anti-inflammatory and antipruritic activity.
  • HY-129388
    Pulrodemstat Methylbenzenesulfonate

    CC-90011 Methylbenzenesulfonate; LSD1-IN-7 Methylbenzenesulfonate

    Histone Demethylase Cancer
    CC-90011 Methylbenzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 Methylbenzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 Methylbenzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
  • HY-137478A
    KB-0742 dihydrochloride

    CDK Cancer
    KB-0742 dihydrochloride is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 dihydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 dihydrochloride has potent anti-tumor activity.
  • HY-143894
    FLT3-IN-11

    FLT3 Cancer
    FLT3-IN-11 (compound 30) is a potent, selective and orally active FLT3 kinase inhibitor with IC50s of 7.22 nM and 4.95 nM for wild-type FLT3 and FLT3-D835Y, respectively. FLT3-IN-11 high selectivity for FLT3 over c-KIT (>1000-fold). FLT3-IN-11has excellent anti-acute myeloid leukemia (AML) activity (MV4-11 cells, IC50 of 3.2 nM).
  • HY-145774
    PD-1/PD-L1-IN-23

    PD-1/PD-L1 Cancer
    PD-1/PD-L1-IN-23 is a potent and orally active inhibitor of PD-1/PD-L1. PD-1/PD-L1-IN-23 is an ester prodrug of L7. L7 is a benzo[c][1,2,5]oxadiazole derivative and biologically evaluated as inhibitors of PD-L1. PD-1/PD-L1-IN-23 displays significant antitumor effects in tumor models of syngeneic and PD-L1 humanized mice.
  • HY-Y1620
    3-(3,4-Dimethoxyphenyl)propanoic acid

    Others Cardiovascular Disease
    3-(3,4-Dimethoxyphenyl)propanoic acid is an orally active short-chain fatty acids (SCFAs). 3-(3,4-Dimethoxyphenyl)propanoic acid stimulates γ globin gene expression, erythropoiesis in vivo and is used for the β hemoglobinopathies and other anemias.
  • HY-122608
    Samelisant free base

    SUVN-G3031 free base

    Histamine Receptor Neurological Disease
    Samelisant (SUVN-G3031) free base is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant free base has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant free base can be used for the research of sleep-related disorders.
  • HY-105670
    PHA-543613

    nAChR Neurological Disease
    PHA-543613 is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki of 8.8 nM. PHA-543613 displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors. PHA-543613 can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research.
  • HY-144654
    HDAC/Top-IN-1

    HDAC Topoisomerase Cancer
    HDAC/Top-IN-1 is an orally active and pan HDAC/Top dual inhibitor with IC50s of 0.036 μM, 0.14 μM, 0.059 μM, 0.089 μM and 9.8 μM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8. HDAC/Top-IN-1 efficiently induces apoptosis with S cell-cycle arrest in HEL cells. HDAC/Top-IN-1 has exhibits excellent in vivo antitumor efficacy.
  • HY-123981
    5MPN

    Others Cancer
    5MPN is a first-in-class, potent, orally active and selective 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4) inhibitor. 5MPN appears to be a competitive inhibitor of the F6P binding site (Ki=8.6 μM). 5MPN does not inhibit PFK-1 or PFKFB3. 5MPN targets the sugar metabolism of tumors and suppresses proliferation of multiple human cancer cell lines.
  • HY-120270
    PF-06679142

    AMPK Metabolic Disease
    PF-06679142 (Compound 10) is a potent, orally active AMPK activator with an EC50 of 22 nM against α1β1γ1-AMPK. PF-06679142 can be used for diabetic nephropathy research.
  • HY-145741
    MptpB-IN-1

    Antibiotic Infection
    MptpB-IN-1 (Compound 13) is a potent and orally active inhibitor of MptpB. Mycobacterium tuberculosis protein-tyrosine-phosphatase B (MptpB) is a secreted virulence factor that subverts antimicrobial activity in the host. MptpB-IN-1 reduces multidrug-resistant mycobacterium tuberculosis survival and infection burden.
  • HY-146884
    MET kinase-IN-3

    c-Met/HGFR VEGFR Cancer
    MET kinase-IN-3 (compound 8) is an orally active and potent MET inhibitor, with an IC50 of 9.8 nM. MET kinase-IN-3 shows good and broad-spectrum antiproliferative activity against cancer cell lines.
  • HY-W011117
    Danofloxacin

    Bacterial DNA/RNA Synthesis Antibiotic Infection
    Danofloxacin is a third generation fluoroquinolone and orally active antimicrobial agent. Danofloxacin shows a broad spectrum of activity against most Gram-negative and Gram-positive bacteria, mycoplasma and chlamydia species, and plays an antimicrobial role by inhibition of bacterial DNA-gyrase. Danofloxacinh has the potential for respiratory diseases in cattle, swine, and chickens treatment.
  • HY-100501
    M2698

    MSC2363318A

    Ribosomal S6 Kinase (RSK) Akt Cancer
    M2698 (MSC2363318A) is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with IC50s of 1 nM for p70S6K, Akt1 and Akt3. M2698 can cross the blood-brain barrier and has anti-cancer activity.
  • HY-146780
    TGFβRI-IN-4

    TGF-β Receptor Cancer
    TGFβRI-IN-4 is a highly potent and orally active TGFβ receptor type I (TGFβRI) inhibitor, with IC50s of 44 nM and 42.5 nM for ALK5 and NIH3T3. TGFβRI-IN-4 can suppress tumor growth and tumor weight in tumor xenograft model.
  • HY-146691
    hMAO-B-IN-2

    Monoamine Oxidase Neurological Disease
    hMAO-B-IN-2 (compound 6j) is an orally active, potent, selective and BBB penetrated and competitive reversible hMAO-B inhibitor, with an IC50 of 4 nM. hMAO-B-IN-2 shows low toxicity and good neuroprotective effects in SH-SY5Y cell. hMAO-B-IN-2 can be used for alzheimer’s disease research.
  • HY-12168
    Tanomastat

    BAY 12-9566

    MMP Cancer
    Tanomastat (BAY 12-9566) is an orally bioavailable, non-peptidic biphenyl matrix metalloproteinases (MMPs) inhibitor with a Zn-binding carboxyl group. The Ki values are 11, 143, 301, and 1470 nM for MMP-2, MMP-3, MMP-9, MMP-13 respectively. Tanomastat shows anti-invasive and antimetastatic activity in several experimental tumor models.
  • HY-145838
    AAK1-IN-4

    Others Neurological Disease
    AAK1-IN-4 is a highly selective, CNS-penetrable, and orally active adaptor protein-2-associated kinase 1 (AAK1) inhibitor (AAK1 IC50 of 4.6 nM, Filt Ki of 0.9 nM, and cell IC50 of 8.6 nM). AAK1-IN-4 has the potential for the research for neuropathic pain.
  • HY-108232
    MK-2206

    Akt Autophagy Apoptosis Cancer
    MK-2206 is an orally active, highly potent and selective allosteric Akt inhibitor, with IC50s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206. Anticancer activities.
  • HY-125858
    MI-1061

    MDM-2/p53 E1/E2/E3 Enzyme Apoptosis Cancer
    MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity.
  • HY-145839
    AAK1-IN-5

    Others Neurological Disease
    AAK1-IN-5 is a highly selective, CNS-penetrable, and orally active adaptor protein-2-associated kinase 1 (AAK1) inhibitor (AAK1 IC50 of 1.2 nM, Filt Ki of 0.05 nM, and cell IC50 of 0.5 nM). AAK1-IN-4 has the potential for the research for neuropathic pain.
  • HY-B0352
    Mirtazapine

    Org3770; 6-Azamianserin

    5-HT Receptor Histamine Receptor Adrenergic Receptor Inflammation/Immunology Neurological Disease
    Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively.
  • HY-144763
    XPO1-IN-1

    Apoptosis Others Cancer
    XPO1-IN-1 (compound D4) is an orally active and potent XPO1 inhibitor, with an IC50 of 24 nM in MM.1S cell. XPO1-IN-1 can efficiently induce cell apoptosis and cell cycle arrest. XPO1-IN-1 displays favorable metabolic stability and pharmacokinetic properties. XPO1-IN-1 can be used for multiple myeloma (MM) research.
  • HY-103565
    AMN082

    mGluR Neurological Disease
    AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects.
  • HY-16478
    Trifluridine/tipiracil hydrochloride mixture

    TAS-102

    Nucleoside Antimetabolite/Analog Thymidylate Synthase Cancer
    Trifluridine/tipiracil hydrochloride mixture (TAS-102) is a potent and orally active nucleoside antitumor agent. The composition of Trifluridine/tipiracil hydrochloride mixture (TAS-102) is a 1:0.5 mixture (on a molar basis) of alpha,alpha,alpha-tri-fluorothymidine (FTD) and thymidine phosphorylase inhibitor (TPI). Trifluridine/tipiracil hydrochloride mixture (TAS-102) shows the antitumor activity mainly via the inhibition of thymidylate synthase (TS) and incorporation into DNA.
  • HY-145285
    APJ receptor agonist 5

    Others Cardiovascular Disease
    APJ receptor agonist 5 (compound 3) is a potent and orally active agonist of apelin receptor (APJ) with an EC50 of 0.4 nM. APJ receptor agonist 5 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 5 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 5 leads to improved cardiac function and can be used for researching the HF disease.
  • HY-111784
    Inobrodib

    CCS1477

    Epigenetic Reader Domain Cancer
    Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. Inobrodib binds to p300 and CBP with Kd values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a Kd of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression.
  • HY-12085S
    Apremilast-d5

    CC-10004-d5

    Phosphodiesterase (PDE) TNF Receptor Apoptosis Inflammation/Immunology
    Apremilast D5 (CC-10004 D5) is a deuterium labeled Apremilast. Apremilast is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM.
  • HY-139612
    JDQ-443

    NVP-JDQ443

    Ras Cancer
    JDQ-443 is an orally active, potent, selective, and covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). JDQ-443 shows antitumor activity.
  • HY-122487
    Troriluzole

    BHV-4157

    Others Neurological Disease
    Troriluzole, a third-generation, tripeptide prodrug of Riluzole (HY-B0211), is an orally active glutamate modulator. Troriluzole reduces synaptic glutamate level and increases the synaptic glutamate absorption. Troriluzole has the potential for Alzheimer disease and generalized anxiety disorder (GAD).
  • HY-125858A
    MI-1061 TFA

    MDM-2/p53 E1/E2/E3 Enzyme Apoptosis Cancer
    MI-1061 TFA is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 TFA potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity.
  • HY-N4115
    Syrosingopine

    Su 3118

    Monocarboxylate Transporter Cancer Cardiovascular Disease
    Syrosingopine (Su 3118) is a potent and dual inhibitor of MCT1 and MCT4 with 60-fold higher potency on MCT4. Syrosingopine (Su 3118) prevents lactate and H+ efflux. Syrosingopine (Su 3118) is an anti-hypertensive drug with oral activity. Syrosingopine (Su 3118) combined with metformin has the potential for research cancer diseases.
  • HY-N2573A
    Corydalmine hydrochloride

    L-Corydalmine hydrochloride; TLZ-16-CL

    Fungal CXCR Infection Neurological Disease
    Corydalmine hydrochloride inhibits spore germination of some plant pathogenic as well as saprophytic fungi. Corydalmine hydrochloride acts as an oral analgesic agent, exhibiting potent analgesic activity. Corydalmine hydrochloride alleviates Vincristine-induced neuropathic pain in mice by inhibiting an NF-κB-dependent CXCL1/CXCR2 signaling pathway.
  • HY-133017
    Amcenestrant

    SAR439859

    Estrogen Receptor/ERR Cancer
    SAR439859 (compound 43d) is an orally active, nonsteroidal and selective estrogen receptor degrader (SERD). SAR439859 is a potent ER antagonist and has ER degrading activity with an EC50 of 0.2 nM for ERα degradation. SAR439859 demonstrates robust antitumor efficacy and limited cross-resistance in ER + breast cancer.
  • HY-101402A
    Cyclo(his-pro) TFA

    Cyclo(histidyl-proline) TFA; Histidylproline diketopiperazine TFA

    NF-κB Endogenous Metabolite Inflammation/Immunology Neurological Disease
    Cyclo(his-pro) TFA (Cyclo(histidyl-proline) TFA) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) TFA could inhibit NF-κB nuclear accumulation. Cyclo(his-pro) TFA can cross the brain-blood-barrier and affect diverse inflammatory and stress responses.
  • HY-125817
    BI-3406

    Ras p38 MAPK Cancer
    BI-3406 (compound I-6) is an orally active, highly potent and selective inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with an IC50 of 6 nM. BI-3406 potently reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 has anticancer activity.
  • HY-12908
    Bcl-xL antagonist 2

    Bcl-2 Family Cancer
    Bcl-xL antagonist 2 is a potent, selective, and orally active antagonist of BCL-XL with an IC50 and Ki of 0.091 μM and 65 nM, respectively. Bcl-xL antagonist 2 promotes the apoptosis of cancer cells. Bcl-xL antagonist 2 has the potential for the research of the chronic lymphocytic leukemia (CLL) and non-Hodgkin’s lymphoma (NHL).
  • HY-108460
    A-784168

    TRP Channel Neurological Disease
    A-784168 is a potent and orally active inhibitor of vanilloid receptor type 1 (TRPV1). Vanilloid receptor type 1 (TRPV1) is a ligand-gated nonselective cation channel that is considered to be an important integrator of various pain stimuli such as endogenous lipids, capsaicin, heat, and low pH. A-784168 has good CNS penetration.
  • HY-146138
    EGFR-IN-57

    EGFR VEGFR Casein Kinase Topoisomerase Microtubule/Tubulin Apoptosis Cancer
    EGFR-IN-57 (Compound 25a) is a potent, orally active EGFR-TK inhibitor with an IC50 of 0.054 µM. EGFR-IN-57 also inhibits VEGFR-2, CK2α, topoisomerase IIβ and tubulin polymerization with IC50 values of 0.087, 0.171, 0.13 and 3.61 µM, respectively. EGFR-IN-57 induces cell cycle arrest at G2/M and pre-G1 phases. EGFR-IN-57 induces cancer cell apoptosis.
  • HY-111790
    M3258

    Proteasome Apoptosis Cancer
    M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC50=3.6 nM) and cellular (IC50=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells.
  • HY-119257
    ABT-100

    Farnesyl Transferase Apoptosis Cancer
    ABT-100 is a potent, highly selective and orally active farnesyltransferase inhibitor. ABT-100 inhibits cell proliferation (IC50s of 2.2 nM, 3.8 nM, 5.9 nM, 6.9 nM, 9.2 nM, 70 nM and 818 nM for EJ-1, DLD-1, MDA-MB-231, HCT-116, MiaPaCa-2, PC-3, and DU-145 cells, respectively), increases apoptosis and decreases angiogenesis. ABT-100 possesses broad-spectrum antitumor activity.
  • HY-109019
    Vorolanib

    CM082; X-82

    VEGFR PDGFR Cancer Cardiovascular Disease
    Vorolanib (CM082) is an orally active, potent multikinase VEGFR/PDGFR inhibitor. Vorolanib is a potent ATP-binding cassette (ABC) transporter inhibitor. Vorolanib is an angiogenesis inhibitor and has antitumor activity combined with ZD1839 (HY-50895).
  • HY-143412
    MIR002

    HDAC DNA/RNA Synthesis Apoptosis Cancer
    MIR002 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. MIR002 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. MIR002 shows significant antitumor activity in vivo.
  • HY-136459
    NMDA receptor antagonist 2

    iGluR Neurological Disease
    NMDA receptor antagonist 2 is a potent and orally active NR2B subtype-selective NMDA antagonist with an IC50 and a Ki of 1.0 nM and 0.88 nM, respectively. NMDA receptor antagonist 2 is used for the study of neuropathic pain and Parkinson’s disease.
  • HY-17452
    Cefditoren sodium

    ME 1206

    Bacterial Infection Inflammation/Immunology
    Cefditoren sodium (ME 1206) is a broad-spectrum, third-generation, oral cephalosporin antibacterial with enhanced stability against many common β lactamases. Cefditoren sodium has activity against Gram-negative organisms and Gram-positive organisms. Cefditoren sodium can be used in the research of infection diseases such as acute exacerbations of chronic bronchitis, community-acquired pneumonia (CAP), streptococcal pharyngitis/tonsillitis, or uncomplicated skin and skin structure infections.
  • HY-W011220
    Ciglitazone

    ADD-3878; U-63287

    PPAR Cancer Cardiovascular Disease
    Ciglitazone is a potent and selective PPARγ agonist (EC50=3 μM). Ciglitazone inhibits proliferation and differentiation of th17 cells. Ciglitazone is a hypoglycemic agent orally active in the obese-hyperglycemic animal models. Ciglitazone induces apoptosis accompanied by activation of p38 MAPK and nuclear translocation of apoptosis inducing factor (AIF) in opossum kidney (OK) renal epithelial cells.
  • HY-13001
    Quizartinib

    AC220

    FLT3 Ligands for Target Protein for PROTAC Apoptosis Autophagy Cancer
    Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis.
  • HY-146619
    RAGE/SERT-IN-1

    Amyloid-β Serotonin Transporter Neurological Disease
    RAGE/SERT-IN-1 is a potent and orally active advanced glycation end products (RAGE) and serotonin transporter (SERT) inhibitor with IC50s of 8.26 μM and 31.09 nM, respectively. RAGE/SERT-IN-1 exhibits significant neuroprotective effect against Aβ25-35-induced neuronal damage and alleviates depressive behavior of mice. RAGE/SERT-IN-1 can be used for researching the comorbidity of Alzheimer's disease and depression.
  • HY-103565A
    AMN082 free base

    mGluR Neurological Disease
    AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects.
  • HY-143656
    SH379

    Autophagy Endocrinology
    SH379 is the derivative of 2-methylpyrimidine-fused tricyclic diterpene. SH379 is a potent and orally active anti-late-onset hypogonadism agent. SH379 significantly promotes the expression of the key testosterone synthesis-related enzymes StAR and 3β-HSD. SH379 stimulates autophagy through regulating AMPK/mTOR signaling pathway.
  • HY-108519
    AS1892802

    ROCK Neurological Disease
    AS1892802 is a potent, orally active, and highly selective inhibitor of ROCK. The onset of antinociceptive effect of AS1892802 is as fast as those of Tramadol and Diclofenac. AS1892802 did not induce gastric irritation or abnormal behavior. AS1892802 is an attractive analgesic profile for the research of severe osteoarthritis pain.
  • HY-19896
    COTI-2

    MDM-2/p53 Apoptosis Cancer
    COTI-2, an anti-cancer drug with low toxicity, is an orally available third generation activator of p53 mutant forms. COTI-2 acts both by reactivating mutant p53 and inhibiting the PI3K/AKT/mTOR pathway. COTI-2 induces apoptosis in multiple human tumor cell lines. COTI-2 exhibits antitumor activity in HNSCC through p53-dependent and -independent mechanisms. COTI-2 converts mutant p53 to wild-type conformation.
  • HY-143895
    FLT3-IN-12

    FLT3 Cancer
    FLT3-IN-12 is a potent, selective and orally active FLT3 kinase inhibitor with IC50s of 1.48 nM and 2.87 nM for FLT3-WT and FLT3-D835Y, respectively. FLT3-IN-12 possesses high selectivity over c-KIT (>1000-fold). FLT3-IN-12 has an excellent anti-AML (acute myeloid leukemia) activity (MV4-11, IC50 of 0.75 nM).
  • HY-13775
    XL019

    JAK Apoptosis Cancer
    XL019 is a potent, orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2.
  • HY-131909
    CJ-2360

    ALK Cancer
    CJ-2360 is a potent and orally active ALK inhibitor with IC50s of 2.2, 4.0, 8.8, 6.3, and 8.9 nM against wild-type ALK and F1197M, G1269A, L1196M, and S1206Y ALK mutants, respectively. CJ-2360 displays potent inhibitory activity against two clinically reported ALK mutants (C1156Y and L1196M) and a few other kinases (LTK, MERTK, CLK1, DAPK1, and DAPK2) among the 468 kinases evaluated.
  • HY-17600S
    Acalabrutinib-d4

    ACP-196-d4

    Btk Cancer
    Acalabrutinib D4 (ACP-196 D4) is a deuterium labeled Acalabrutinib. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor.
  • HY-128575
    BNC375

    nAChR Neurological Disease
    BNC375 is a potent, selective, and orally available type I positive allosteric modulator of α7 nAChRs with an EC50 of 1.9 μM. BNC375 exhibits good CNS-drug like properties and clinical candidate potential. .
  • HY-B1599
    Chloramphenicol palmitate

    Bacterial Infection
    Chloramphenicol palmitate is an orally active broad spectrum antibiotic and has a broad spectrum of activity against gram positive and gram negative bacteria. Chloramphenicol palmitate inhibits bacterial protein synthesis by blocking the peptidyl transferase step. Chloramphenicol palmitate can be used as bacterial selection agent in transformed cells containing chloramphenicol resistance genes.
  • HY-13302
    CP-547632

    VEGFR FGFR Cancer
    CP-547632 is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 has antitumor efficacy.
  • HY-13302B
    CP-547632 hydrochloride

    VEGFR FGFR Cancer
    CP-547632 hydrochloride is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 hydrochloride is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 hydrochloride has antitumor efficacy.
  • HY-126781
    Fozivudine tidoxil

    BM-211290

    HIV DNA/RNA Synthesis Infection
    Fozivudine tidoxil (BM-211290) is an orally active thioether lipid-zidovudine (ZDV) conjugate with anti-HIV activity. Fozivudine tidoxil, a member of the NRTI family of drug, is incorporated into the newly synthesized strand of DNA during intracellular viral replication and irreversibly binds viral RT which disrupts viral reverse-transcription.
  • HY-142946
    KRAS G12C inhibitor 44

    Ras Cancer
    KRAS G12C inhibitor 44 (compound 54) is a potent and orally active KRAS G12C inhibitor. KRAS G12C inhibitor 44 shows anti-proliferation activities with IC50s of 0.016, 0.028 µM in MIA PaCA-2, H358 cells, respectively. KRAS G12C inhibitor 44 shows antitumor effects in vivo.
  • HY-17452A
    Cefditoren (Pivoxil)

    Cefditoren pivoxyl; Cefditoren pivaloyloxymethyl ester; ME 1207

    Bacterial Antibiotic Infection Inflammation/Immunology
    Cefditoren Pivoxil (ME 1207) is a broad-spectrum, third-generation, oral cephalosporin antibacterial with enhanced stability against many common β lactamases. Cefditoren Pivoxil has activity against Gram-negative organisms and Gram-positive organisms. Cefditoren Pivoxil can be used in the research of infection diseases such as acute exacerbations of chronic bronchitis, community-acquired pneumonia (CAP), streptococcal pharyngitis/tonsillitis, or uncomplicated skin and skin structure infections.
  • HY-146112
    IRAK4-IN-14

    IRAK Cancer
    IRAK4-IN-14 (compound 28) is a potent, selective and orally active IRAK4 inhibitor with an IC50 of 0.003 µM. IRAK4-IN-14 shows good PK parameters in rats and mouse. IRAK4-IN-14 shows synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with Acalabrutinib.
  • HY-114338
    Dalpiciclib

    SHR-6390

    CDK Cancer
    Dalpiciclib (SHR-6390) is a highly selective, orally bioavailable CDK4/6 inhibitor with comparable potencies against CDK4 (IC50=12.4 nM) and CDK6 (IC50=9.9 nM). Dalpiciclib exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated tumor-suppressor retinoblastoma protein (Rb) and inducing G1 cell cycle arrest.
  • HY-146421
    Anti-inflammatory agent 21

    NO Synthase ROS NF-κB Inflammation/Immunology
    Anti-inflammatory agent 21 (compound 9o) is an orally active and low cytotoxic anti-inflammatory agent, with an IC50 value of 0.76 μM for NO. Anti-inflammatory agent 21 acts via accumulation ROS and blocks the NF-κB/MAPK signaling pathway. Anti-inflammatory agent 21 can ameliorate cartilage destruction and inflammatory cell infiltration in arthritis rats model.
  • HY-122560A
    VU0134992 hydrochloride

    Potassium Channel Cardiovascular Disease
    VU0134992 hydrochloride is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 µM. VU0134992 hydrochloride is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 µM) at -120 mV.
  • HY-122560
    VU0134992

    Potassium Channel Cardiovascular Disease
    VU0134992 is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 µM. VU0134992 is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 µM) at -120 mV.
  • HY-123032
    Sorivudine

    BV-araU

    DNA/RNA Synthesis Infection
    Sorivudine (BV-araU) is an orally active synthetic pyrimidine nucleoside antimetabolite drug. Sorivudine derives its antiviral activity from selective conversion by a specific thymidine kinase present in certain DNA viruses to nucleotides, which can in turn interfere with viral DNA synthesis.
  • HY-12422
    Voruciclib

    CDK Cancer
    Voruciclib is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL).
  • HY-12422A
    Voruciclib hydrochloride

    CDK Cancer
    Voruciclib hydrochloride is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib hydrochloride potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib hydrochloride represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL).
  • HY-W020468
    Linopirdine

    DuP 996

    Potassium Channel TRP Channel Neurological Disease
    Linopirdine (DuP 996) is an orally active, selective M-type K + current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing drug, increases acetylcholine release in rat brain tissue.
  • HY-144858
    EZM0414

    Histone Methyltransferase Cancer
    EZM0414 is a potent, selective, orally bioavailable inhibitor of SETD2 (IC50=18 nM in SETD2 biochemical assay; IC50=34 nM in cellular assay). EZM0414 can be used for the research of relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma.
  • HY-133807
    Benpyrine

    TNF Receptor Inflammation/Immunology
    Benpyrine is a highly specific and orally active TNF-α inhibitor with a KD value of 82.1 μM. Benpyrine tightly binds to TNF-α and blocks its interaction with TNFR1, with an IC50 value of 0.109 µM. Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research.
  • HY-146755
    TIY-7

    Trk Receptor Cancer
    TIY-7 is a selective and orally active tropomyosin receptor kinase (TRK) inhibitor. TIY-7 shows enzyme inhibitory activity with IC50s of 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM for TRKA, TRKA G595R, TRKA G667C, TRKA F589L, TRKC G623R, TRKC G696A, respectively. TIY-7 shows anti-tumor potency in mouse xenograft model.
  • HY-133011
    nAChR agonist 1

    nAChR Neurological Disease
    nAChR agonist 1 is a potent, brain-permeable, and orally efficacious positive allosteric modulator of α7 nicotinic acetylcholine receptor (α7 nAChR). nAChR agonist 1 has the EC50 of 0.32 µM in a Ca 2+ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease.
  • HY-107572
    PD 128042

    CI 976

    Acyltransferase Metabolic Disease
    PD 128042 (CI 976) is a potent, orally active, and selective inhibitor of ACAT (acyl coenzyme A:cholesterol acyltransferase) with an IC50s of 73 nM. PD 128042 is also a potent LPAT (lysophospholipid acyltransferase) inhibitor. PD 128042 inhibits Golgi-associated LPAT activity (IC50=15 μM). PD 128042 inhibits multiple membrane trafficking steps, including ones found in the endocytic and secretory pathway.
  • HY-15614A
    SC144 hydrochloride

    Interleukin Related Apoptosis Cancer
    SC144 hydrochloride is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 hydrochloride binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 hydrochloride shows potent inhibition of gp130 ligand-triggered signaling. SC144 hydrochloride induces apoptosis in human ovarian cancer cells.
  • HY-15614
    SC144

    Interleukin Related Apoptosis Cancer
    SC144 is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 shows potent inhibition of gp130 ligand-triggered signaling. SC144 induces apoptosis in human ovarian cancer cells.
  • HY-16992A
    W-54011

    Complement System Reactive Oxygen Species Inflammation/Immunology
    W-54011 is a potent and orally active non-peptide C5a receptor antagonist. W-54011 inhibits the binding of 125I-labeled C5a to human neutrophils with a Ki value of 2.2 nM. W-54011 also inhibits C5a-induced intracellular Ca 2+ mobilization, chemotaxis, and generation of ROS in human neutrophils with IC50s of 3.1 nM, 2.7 nM, and 1.6 nM, respectively.
  • HY-143337
    EGFR-IN-47

    Apoptosis EGFR Cancer
    EGFR-IN-47 is a potent and orally active EGFR L858R/T790M/C797S inhibitor with an IC50 of 0.01 µM. EGFR-IN-47 induces cell cycle attest and cell apoptosis. EGFR-IN-47 has the potential for the research of NSCLC.
  • HY-135853
    Molnupiravir

    EIDD-2801; MK-4482

    SARS-CoV Influenza Virus Infection
    Molnupiravir (EIDD-2801) is an orally bioavailable prodrug of the ribonucleoside analog EIDD-1931. Molnupiravir has broad spectrum antiviral activity against influenza virus and multiple coronaviruses, such as SARS-CoV-2, MERS-CoV, SARS-CoV. Molnupiravir has the potential for the research of COVID-19, and seasonal and pandemic influenza.
  • HY-12995A
    (S)-BI 665915

    FLAP Inflammation/Immunology
    (S)-BI 665915 is an orally active oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.7 nM for FLAP binding. (S)-BI 665915 inhibits FLAP functional in human whole blood with an IC50 of 45 nM. (S)-BI 665915 demonstrates an excellent cross-species drug metabolism and pharmacokinetics (DMPK) profile and a dose-dependent inhibition of LTB4 production.
  • HY-146723
    IKKβ-IN-1

    IKK Inflammation/Immunology
    IKKβ-IN-1 is a potent and orally active IkappaB (IKK-β) inhibitor with IC50 of 0.20 μM. IKKβ-IN-1 can reduce PGE2 and TNF-α production in mouse macrophage cells. IKKβ-IN-1 has the ability to protect mice against septic shock induced mortality.
  • HY-33009
    AS057278

    Others Neurological Disease
    AS057278 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant non-peptidic D-amino acid oxidase (DAAO) inhibitor with an IC50 value of 0.91 μM and EC50 of 2.2-3.95 μM. AS057278 can normalize phencyclidine (PCP)-induced prepulse inhibition in mice. AS057278 can be used for researching schizophrenia.
  • HY-144132
    αβ-Tubulin-IN-1

    Apoptosis Microtubule/Tubulin Cancer
    αβ-Tubulin-IN-1 is a potent and orally active αβ-Tubulin inhibitor. αβ-Tubulin-IN-1 induces cell cycle arrest at G2/M and efficient apoptosis. αβ-Tubulin-IN-1 inhibits tumor cell migration and Metastasis. αβ-Tubulin-IN-1 shows significant antitumor efficacy in a dose dependent manner.
  • HY-147531
    Antibacterial agent 106

    Bacterial Infection
    Antibacterial agent 106 (compound 8) is an orally active and potent antibacterial agent with antibiofilm activity. Antibacterial agent 106 shows potent antibacterial effect against multi-drug resistant (MDR)-Gram positive pathogens. Antibacterial agent 106 is highly effective in clearing 99.7% of the intracellular methicillin-resistant S. aureus (MRSA) harbored inside macrophages.
  • HY-13499
    CCR2 antagonist 5

    CCR Inflammation/Immunology
    CCR2 antagonist 5 is a selective, orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM). CCR2 antagonist 5 displays a Ki of 9.6 µM for mCCR2 binding. CCR2 antagonist 5 can be used in the research of inflammatory disease.
  • HY-13302C
    CP-547632 TFA

    VEGFR FGFR Cancer
    CP-547632 TFA is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 TFA is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 TFA has antitumor efficacy.
  • HY-146584
    Cathepsin C-IN-5

    Cathepsin Inflammation/Immunology
    Cathepsin C-IN-5 (compound SF38) is a potent, selective and orally active Cathepsin C inhibitor with IC50s of 59.9 nM, 4.26 µM, >5 µM, >5 µM, >5 µM for Cat C, Cat L, Cat S, Cat B, Cat K, respectively. Cathepsin C-IN-5 inhibits the Cat C activity in bone marrow and blood. Cathepsin C-IN-5 decreases the activation of NSPs (neutrophil serine proteases). Cathepsin C-IN-5 shows anti-inflammatory activity.
  • HY-14362
    GSK-25

    ROCK Ribosomal S6 Kinase (RSK) Cardiovascular Disease
    GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively).
  • HY-107427
    PF-3644022

    MAPKAPK2 (MK2) p38 MAPK Inflammation/Immunology
    PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect.
  • HY-108425
    AMG8379

    Sodium Channel Neurological Disease
    AMG8379 is a potent, orally active and selective sulfonamide antagonist of the voltage-gated sodium channel NaV1.7, with IC50s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively. AMG8379 potently and reversibly blocks endogenous Tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglia (DRG) neurons with an IC50 of 3.1 nM.
  • HY-144267
    Glucosylceramide synthase-IN-2

    Others Metabolic Disease Neurological Disease
    Glucosylceramide synthase-IN-2 (compound T-690) is a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 15 nM and 190 nM for human GCS and mouse GCS, respectively.Glucosylceramide synthase-IN-2 exhibits noncompetitive type inhibition with C8-ceramide and UDP-glucose.Glucosylceramide synthase-IN-2 can be used for Gaucher's disease research.
  • HY-10409
    Fedratinib

    TG-101348; SAR 302503

    JAK Apoptosis Cancer
    Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research.
  • HY-10409A
    Fedratinib hydrochloride hydrate

    TG-101348 hydrochloride hydrate; SAR 302503 hydrochloride hydrate

    JAK Apoptosis Cancer
    Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research.
  • HY-W062836
    BAY 41-8543

    Guanylate Cyclase Cardiovascular Disease
    BAY 41-8543 is an orally active, nitric oxide (NO)-independent stimulator of soluble guanylyl cyclase (sGC). BAY 41-8543 has vasodilator activity in the pulmonary and systemic vascular beds in the rat. BAY 41-8543 has antiplatelet effects and has the potential for cardiovascular diseases research.
  • HY-144653
    PDGFR-IN-1

    PDGFR Apoptosis Cancer
    PDGFR-IN-1 (compound 7m) is a potent and orally active PDGFR (platelet-derived growth factor receptor) inhibitor, with IC50 values of 2.4 and 0.9 nM for PDGFRα and PDGFRβ, respectively. PDGFR-IN-1 displays robust antitumor effects and low toxicity, and can be used to study osteosarcoma.
  • HY-19642
    Glesatinib

    MGCD265

    TAM Receptor c-Met/HGFR Cancer
    Glesatinib (MGCD265) is an orally active, potent MET/SMO dual inhibitor. Glesatinib, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC).
  • HY-124628
    IPI-9119

    Fatty Acid Synthase (FASN) Cancer
    IPI-9119 is an orally active, selective and irreversible FASN inhibitor with an IC50 of 0.3 nM in vitro biochemical assay. IPI-9119 inhibits tumor growth of castration-resistant prostate cancer (CRPC) xenografts mouse models.
  • HY-19642A
    Glesatinib hydrochloride

    MGCD265 hydrochloride

    TAM Receptor c-Met/HGFR Cancer
    Glesatinib hydrochloride (MGCD265 hydrochloride) is an orally active, potent MET/SMO dual inhibitor. Glesatinib hydrochloride, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC).
  • HY-144074
    LRRK2-IN-4

    LRRK2 Neurological Disease
    LRRK2-IN-4 is a potent, selective, CNS-penetran and orally active leucine-rich repeat kinase 2 (LRRK2) inhobitor with an IC50 of 2.6 nM. LRRK2-IN-4 has the potential for the research of Parkinson’s disease.
  • HY-119101
    AZD-5672

    CCR Potassium Channel P-glycoprotein Inflammation/Immunology
    AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM). AZD-5672 shows moderate activity against the hERG ion channel (binding IC50=7.3 μM). AZD5672 is a substrate of human P-gp, and inhibits P-gp-mediated digoxin transport (IC50=32 μM). AZD-5672 can be used for the research of rheumatoid arthritis.
  • HY-146468
    DPP-4/GPR119 modulator 1

    Dipeptidyl Peptidase GPR119 Potassium Channel Metabolic Disease
    DPP-4/GPR119 modulator 1 (Compound 22) is an orally active dipeptidyl peptidase IV (DPP-IV) inhibitor and GPR119 agonist. DPP-4/GPR119 modulator 1 shows blood glucose-lowering effect and moderate inhibition on hERG channel with an IC50 of 4.9 µM. DPP-4/GPR119 modulator 1 can be used for diabetes research.
  • HY-124623
    DNDI-8219

    Parasite Infection
    DNDI-8219 (compound 58) is a potent selective and orally active trypanocidal agent, possessing inhibitory activity against Trypanosoma cruzi (T. cruzi) with an IC50 of 0.4 μM. DNDI-8219 has low cytotoxicity (L6 cells IC50 > 100 μM). DNDI-8219 can effectively cure chronic T. cruzi infection and markedly reduce parasite burdens in mouse model. DNDI-8219 has good solubility, metabolic stability and safety.
  • HY-136360
    MI-3454

    Epigenetic Reader Domain Cancer
    MI-3454 is an orally active, highly potent and selective menin-MLL1 interaction inhibitor with an IC50 of 0.51 nM. MI-3454 inhibits proliferation, induces differentiation and complete remission or regression of leukemia in mouse models of MLL1-rearranged or NPM1-mutated leukemia through downregulation of key genes involved in leukemogenesis.
  • HY-10252
    NVP-ADW742

    ADW742; GSK 552602A; ADW

    IGF-1R Insulin Receptor Apoptosis Cancer Endocrinology
    NVP-ADW742 (ADW742) is an orally active, selective IGF-1R tyrosine kinase inhibitor with an IC50 of 0.17 μM. NVP-ADW742 inhibits insulin receptor (InsR) with an IC50 of 2.8 μM. NVP-ADW742 induces pleiotropic antiproliferative/proapoptotic biologic sequelae in tumor cells.
  • HY-106560
    Proglumetacin

    Inflammation/Immunology
    Proglumetacin is an orally active and potent cyclo-oxygenase inhibitor. Proglumetacin can inhibits SARS-CoV M pro (main protease of the SARS-CoV-2), with an AC50 of 8.9 μM (activity concentration at half maximal activity). Proglumetacin has anti-inflammatory activity, can be used for inflammation (such as Rheumatoid arthritis, and Allergic air pouch inflammation) research.
  • HY-145734A
    AMXI-5001 hydrochloride

    Microtubule/Tubulin Cancer
    AMXI-5001 hydrochloride is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 hydrochloride exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 hydrochloride induces complete regression of established tumors, including exceedingly large tumors.
  • HY-145734
    AMXI-5001

    Microtubule/Tubulin Cancer
    AMXI-5001 is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 induces complete regression of established tumors, including exceedingly large tumors.
  • HY-15724A
    Vercirnon sodium

    GSK-1605786 sodium; CCX282-B sodium; Traficet-EN sodium

    CCR Inflammation/Immunology Endocrinology
    Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon sodium inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon sodium is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively.
  • HY-15724
    Vercirnon

    GSK-1605786; CCX282-B; Traficet-EN

    CCR Inflammation/Immunology Endocrinology
    Vercirnon (GSK1605786A) is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively.
  • HY-12689
    Mitapivat

    AG-348

    Pyruvate Kinase Cancer
    Mitapivat (AG-348) is a potent, orally active, and allosteric activator of pyruvate kinase with an AC50 of 20 nM. Mitapivat (AG-348) increases enzymatic activity, protein stability, and ATP levels over a broad range of PKLR genotypes. Mitapivat (AG-348) has the potential for restoring the glycolytic pathway activity with PK deficiency.
  • HY-144675
    LSD1-IN-13

    Histone Demethylase Cancer
    LSD1-IN-13 (compound 7e) is an orally active and potent LSD1 inhibitor, with an IC50 of 24.43 nM. LSD1-IN-13 can activate CD86 expression, with an EC50 of 470 nM. LSD1-IN-13 induces differentiation of AML (acute myeloid leukemia) cell lines.
  • HY-144341
    DprE1-IN-1

    Bacterial Infection
    DprE1-IN-1 is a potent, orally active DprE1 inhibitor with favorable hepatocyte stability, low cytotoxicity and low hERG channel inhibition. DprE1-IN-1 displays potent activity against both drug-susceptible and clinically isolated drug-resistant Tuberculosis strains with MICs<0.1 μg/mL, as well as good intracellular antimycobacterial activity with a 1.29 log10 CFU reduction in macrophages.
  • HY-14327
    FAUC 213

    Dopamine Receptor Neurological Disease
    FAUC 213 is an orally active and highly selective dopamine D4 receptor complete antagonist with a Ki of 2.2 nM for hD4.4. FAUC 213 has less activity on D2 and D3 receptors (Kis of 3.4 μM, 5.3 μM for hD2, hD3, respectively). FAUC 213 can cross the blood-brain barrier (BBB). FAUC 213 exhibits atypical antipsychotic characteristic.
  • HY-143881
    FGFR4-IN-6

    FGFR Cancer
    FGFR4-IN-6 (Compound 9ka) is a covalently reversible FGFR4 inhibitor with an IC50 value of 5.4 nM. FGFR4-IN-6 also exhibits good oral pharmacokinetic properties. FGFR4-IN-6 induces significant tumor regressions in a xenograft mouse model of Hep3B2.1-7 HCC cell line without an obvious sign of toxicity.
  • HY-19336
    BAZ2-ICR

    Epigenetic Reader Domain Cancer
    BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR is an epigenetic chemical probe.
  • HY-132301
    MCT4-IN-1

    Monocarboxylate Transporter Cancer
    MCT4-IN-1 is an orally active and selective monocarboxylate transporter 4 (MCT4/SLC16A3) inhibitor with an IC50 of 77 nM and a Ki of 11 nM. MCT4-IN-1 targets to the cytosolic domain of MCT4. MCT4-IN-1 results in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. MCT4-IN-1 has the potential for MCT4 transporter inhibition research.
  • HY-10181B
    Dasatinib monohydrate

    BMS-354825 monohydrate

    Bcr-Abl Src Autophagy Apoptosis Cancer
    Dasatinib (BMS-354825) monohydrate is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib monohydrate inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib monohydrate also induces apoptosis and autophagy.
  • HY-17507
    Pantoprazole

    BY1023; SKF96022

    Proton Pump Autophagy Apoptosis Cancer Inflammation/Immunology
    Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole, a substituted benzimidazole, is a potent H +/K +-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142).
  • HY-18324
    CRS3123

    REP-3123

    Antibiotic Inflammation/Immunology
    CRS3123 is a potent and orally active narrow-spectrum antibiotic. CRS3123 inhibits bacterial methionyl-tRNA synthetase. CRS3123 has potent activity against Clostridium difficile (C. difficile) and aerobic Gram-positive bacteria but little activity against Gram-negative bacteria, including anaerobes. CRS3123 has the potential for the research of C. difficile infections.
  • HY-17507B
    Pantoprazole sodium hydrate

    BY1023 sodium hydrate; SKF96022 sodium hydrate

    Proton Pump Autophagy Apoptosis Cancer Inflammation/Immunology
    Pantoprazole sodium hydrate (BY10232 sodium hydrate) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole sodium hydrate, a substituted benzimidazole, is a potent H +/K +-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole sodium hydrate improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole sodium hydrate significantly increased tumor growth delay combined with Doxorubicin (HY-15142).
  • HY-A0014
    Ramelteon

    TAK-375

    Melatonin Receptor Neurological Disease Endocrinology Cancer
    Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation.
  • HY-124179
    IT-901

    NF-κB Cancer
    IT-901 is an orally active and potent NF-κB subunit c-Rel inhibitor with an IC50 of 0.1 µM, 3 μM for NF-κB DNA binding and c-Rel DNA binding, respectively. IT-901, a bioactive naphthalenethiobarbiturate derivative, has the potential for human lymphoid tumors and ameliorate graft-versus-host disease (GVHD).
  • HY-17507A
    Pantoprazole sodium

    BY1023 sodium; SKF96022 sodium

    Proton Pump Autophagy Apoptosis Cancer Inflammation/Immunology
    Pantoprazole sodium (BY10232 sodium) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole sodium, a substituted benzimidazole, is a potent H +/K +-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole sodium improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole sodium significantly increased tumor growth delay combined with Doxorubicin (HY-15142).
  • HY-10181A
    Dasatinib hydrochloride

    BMS-354825 hydrochloride

    Bcr-Abl Src Autophagy Apoptosis Cancer
    Dasatinib (BMS-354825) hydrochloride is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib hydrochloride also induces apoptosis and autophagy.
  • HY-10181
    Dasatinib

    BMS-354825

    Bcr-Abl Src Autophagy Apoptosis Cancer
    Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy.
  • HY-144126
    S1P1 agonist 5

    LPL Receptor Inflammation/Immunology
    S1P1 agonist 5 is a selective and orally active S1P1 agonist. S1P1 agonist 5 inhibits the lymphocyte egress from the lymphoid tissue to the peripheral blood. S1P1 agonist 5 has the potential for the research of multiple sclerosis (MS).
  • HY-146403
    Antibacterial agent 98

    Bacterial Infection
    Antibacterial agent 98 (compound g37) is a potent and orally active antibacterial agent. Antibacterial agent 98 inhibits the ATPase activity of Gyrase B and impairs Staphylococcus aureus (S. aureus ) DNA supercoiling. Antibacterial agent 98 shows antibacterial activity and not induce resistance development of MRSA (methicillin-resistant S. aureus).
  • HY-120118
    Metarrestin

    ML246

    DNA/RNA Synthesis Cancer
    Metarrestin (ML246) is an orally active, first-in-class and specific perinucleolar compartment inhibitor. Metarrestin disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription, at least in part by interacting with the translation elongation factor eEF1A2. Metarrestin blocks metastatic development and extends survival in mouse cancer models.
  • HY-15256
    Faldaprevir

    BI 201335

    HCV Protease Infection
    Faldaprevir (BI 201335) is a potent, orally active and selective noncovalent inhibitor of NS3/4A protease of HCV (hepatitis C virus) genotypes 1a and 1b, with Ki values of 2.6 and 2.0 nM, respectively. Faldaprevir inhibits HCV RNA replication, with EC50 values of 6.5 and 3.1 nM, respectively. Faldaprevir has potent antiviral activity against chronic HCV infection.
  • HY-132866
    YS-370

    P-glycoprotein Cancer
    YS-370 (compound 44) is a potent, high selective, and orally active inhibitor of P-glycoprotein (P-gp). YS-370 stimulates the P-gp ATPase activity and has moderate inhibition against CYP3A4. YS-370 effectively reverses multidrug resistance (MDR) to paclitaxel and colchicine in SW620/AD300 and HEK293T-ABCB1 cells. YS-370 in combination with paclitaxel achieves much stronger antitumor activity.
  • HY-137315
    TML-6

    Amyloid-β NF-κB mTOR Keap1-Nrf2 Neurological Disease
    TML-6, an orally active curcumin derivative, inhibits the synthesis of the β-amyloid precursor protein and β-amyloid (Aβ). TML-6 can upregulate Apo E, suppress NF-κB and mTOR, and increase the activity of the anti-oxidative Nrf2 gene. TML-6 has the potential for Alzheimer’s disease (AD) research.
  • HY-146516
    Anticancer agent 42

    MDM-2/p53 Apoptosis ROS Cancer
    Anticancer agent 42 (compound 10d) is an orally active anticancer agent, and shows a potent antitumor activity against MDA-MB-231 cell with an IC50 of 0.07 μM. Anticancer agent 42 can exert its anticancer activity by activating apoptotic pathway and p53 expression. Anticancer agent 42 can be used to study metastatic breast cancer.
  • HY-17368
    Rivastigmine

    S-Rivastigmine

    AChE Neurological Disease
    Rivastigmine (S-Rivastigmine) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease.
  • HY-18944
    FIT-039

    CDK HSV CMV DNA/RNA Synthesis Infection
    FIT-039 is a selective, ATP-competitive and orally active CDK9 inhibitor with an IC50 of 5.8 μM for CKD9/cyclin T1. FIT-039 does not inhibit other CDKs and other kinases. FIT-039 inhibits replication of HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human CMV. FIT-039 is a promising antiviral agent for inhibiting drug-resistant HSVs and other DNA viruses.
  • HY-19617A
    EGFR-IN-1 hydrochloride

    EGFR Cancer
    EGFR-IN-1 hydrochloride is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
  • HY-139920A
    Oritinib mesylate

    SH-1028 mesylate

    EGFR Cancer
    Oritinib (SH-1028) mesylate is a selective, orally active, and pyrimidine-based irreversible inhibitor of EGFR with an IC50 of 18 nM. Oritinib (SH-1028) mesylate exhibits potent activity against EGFR sensitive and resistant (T790 M) mutations. Oritinib (SH-1028) mesylate significantly inhibits proliferation of tumor cells with EGFR sensitive and resistant mutation.
  • HY-142295
    GNF2133

    DYRK Metabolic Disease
    GNF2133 is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 µM for DYRK1A and GSK3β, respectively. GNF2133 shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 has the potential for the research of type 1 diabetes.
  • HY-142295A
    GNF2133 hydrochloride

    DYRK Metabolic Disease
    GNF2133 hydrochloride is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 µM for DYRK1A and GSK3β, respectively. GNF2133 hydrochloride shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 hydrochloride significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 hydrochloride has the potential for the research of type 1 diabetes.
  • HY-117015
    Purfalcamine

    Parasite Infection
    Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM. Purfalcamine has antimalarial activity and causes malaria parasites developmental arrest at the schizont stage.
  • HY-111372
    Finerenone

    BAY 94-8862

    Mineralocorticoid Receptor Cardiovascular Disease
    Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease.
  • HY-144456
    Xanthine oxidase-IN-5

    Xanthine Oxidase Metabolic Disease
    Xanthine oxidase-IN-5 is an effective and orally active xanthine oxidase (XO) inhibitor with IC50 value of 0.70 μM. Xanthine oxidase-IN-5 displays favorable drug-like properties with ligand efficiency (LE) and lipophilic ligand efficiency (LLE) values of 0.33 and 3.41, respectively. Xanthine oxidase-IN-5 shows potent hypouricemic effects in hyperuricemic rat model.
  • HY-123319A
    Antofloxacin

    Bacterial Infection
    Antofloxacin is a well tolerate, orally active and broad-spectrum 8-amino-fluoroquinolone with potent antibacterial activities. Antofloxacin shows superior antibacterial activity against gyrA mutation-positive H. pylori strains, especially in Asn87- mutated strains, compared to levofloxacin. Antofloxacin is a weak, reversible inhibitor of CYP1A2 for the treatment of infections caused by a diverse group of bacterial species.
  • HY-121750
    CCG-222740

    Ras ROCK Cancer
    CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor. CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis.
  • HY-146079
    Antifungal agent 31

    Fungal Infection
    Antifungal agent 31 (compound 12) is a potent and orally active triazole antifungal agents with a pyrrolotriazinone scaffold. Antifungal agent 31 shows antifungal activity against Candida spp. and filamentous fungi. Antifungal agent 31 significantly reduced mortality rates and kidney fungal burden in two murine models of lethal systemic infections.
  • HY-14951
    Firategrast

    SB 683699

    Integrin Neurological Disease
    Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist. Firategrast reduces trafficking of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity.
  • HY-146361
    Influenza A virus-IN-7

    Influenza Virus Inflammation/Immunology
    Influenza A virus-IN-7 (compound 16r) is a potent and orally active influenza A virus inhibitor with an IC50 of 3.43 µM and CC50 of >100 µM. Influenza A virus-IN-7 shows anti-IAV activity with low cytotoxicity. Influenza A virus-IN-7 inhibits the transcription and replication of viral RNA.
  • HY-112041
    Unesbulin

    PTC596

    Apoptosis Cancer
    Unesbulin (PTC596) is an orally active and selective B-cell-specific Moloney murine leukemia virus integration site 1 (BMI-1) inhibitor. Unesbulin downregulates MCL-1 and induces p53-independent mitochondrial apoptosis in acute myeloid leukemia (AML) cells. Unesbulin has anti-leukemic activity.
  • HY-127102
    GSK3494245

    DDD01305143​

    Parasite Proteasome Infection
    GSK3494245 (DDD01305143) is a potent, orally active, and selective inhibitor of the chymotrypsin-like activity of the parasite proteasome binding in a site sandwiched between the β4 and β5 subunits (IC50=0.16 μM for WT L. donovani proteasomes). GSK3494245 moderately inhibits chymotrypsin-like activity of human proteasome (IC50: purified 26S=13 µM; enriched THP-1 extracts IC50=40µM). GSK3494245 exhibits attractive biological and biosafety properties.
  • HY-101343
    RS 39604

    5-HT Receptor Neurological Disease
    RS 39604 is a potent, selective, and orally active 5-HT4 receptor antagonist with a pKi of 9.1 in guinea pig striatal membranes. RS 39604 displays a low affinity (pKi<6.5) for 5-HT1A, 5-HT2C, 5-HT3, α1c, D1, D2, M1, M2, AT1, B1 and opioid mu receptors and moderate affinity for δ1, (pKi=6.8) and δ2 (pKi=7.8) sites.
  • HY-19978
    RO-3

    P2X Receptor Neurological Disease
    RO-3 is a potent, CNS-penetrant, and orally active P2X3 and P2X2/3 antagonist with pIC50s of 5.9 and 7.0 for human homomultimeric P2X3 and heteromultimeric P2X2/3 receptors, respectively. RO-3 shows selectivity for P2X3 and P2X2/3 over all other functional homomultimeric P2X receptors (IC50 >10 μM at P2X1,2,4,5,7).
  • HY-19617B
    EGFR-IN-1 TFA

    EGFR Cancer
    EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
  • HY-19617
    EGFR-IN-1

    EGFR Cancer
    EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
  • HY-132302
    Hu7691

    Akt PKA PKC ROCK Ribosomal S6 Kinase (RSK) SGK Cancer
    Hu7691 is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 inhibits tumor growth and enables decrease of cutaneous toxicity in mice.
  • HY-A0030
    Fesoterodine fumarate

    mAChR Metabolic Disease Neurological Disease
    Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB).
  • HY-70053
    Fesoterodine

    mAChR Metabolic Disease Neurological Disease
    Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB).
  • HY-12137A
    Volasertib trihydrochloride

    BI 6727 trihydrochloride

    Polo-like Kinase (PLK) Apoptosis Cancer
    Volasertib (BI 6727) trihydrochloride is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib trihydrochloride inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib trihydrochloride induces mitotic arrest and apoptosis. Volasertib trihydrochloride, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models.
  • HY-12137
    Volasertib

    BI 6727

    Polo-like Kinase (PLK) Apoptosis Cancer
    Volasertib (BI 6727) is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib induces mitotic arrest and apoptosis. Volasertib, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models.
  • HY-17600
    Acalabrutinib

    ACP-196

    Btk Cancer
    Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL).
  • HY-11017
    Rivastigmine tartrate

    ENA 713; SDZ-ENA 713

    AChE Neurological Disease
    Rivastigmine tartrate (ENA 713; SDZ-ENA 713) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM, 4.15 μM, respectively. Rivastigmine tartrate can pass the blood brain barrier (BBB). Rivastigmine tartrate is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease.
  • HY-19357
    E3330

    APX-3330

    DNA/RNA Synthesis Cancer
    E3330 (APX-3330) is a direct, orally active and selective AP endonuclease 1 (APE1; REF-1) inhibitor, which suppresses NF-κB DNA-binding activity. E3330 (APX-3330) blocks TNF-α-induced activation of IL-8 production in liver cancer cell lines. E3330 (APX-3330) shows anticancer properties, such as inhibition of cancer cell growth and migration.
  • HY-138642
    ARV-471

    Estrogen Receptor/ERR PROTACs Cancer
    ARV-471 is an oral estrogen receptor PROTAC protein degrader for breast cancer. ARV-471 is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. ARV-471 leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. ARV-471 robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of ~2 nM.
  • HY-124569
    NAB-14

    iGluR Neurological Disease
    NAB-14 is a potent, selective, orally active and non-competitive GluN2C/2D antagonists with an IC50 of 580 nM for GluN1/GluN2D. NAB-14 shows >800-fold selective for recombinant GluN2C and GluN2D over GluN2A and GluN2B. NAB-14 can cross the blood-brain-barrier.
  • HY-146260
    NVP-CLR457

    PI3K Cancer
    NVP-CLR457 (compound 40) is an orally active, potent and balanced pan-class I PI3K inhibitor. NVP-CLR457 shows a clear dose-dependent PK/PD/efficacy relationship. NVP-CLR457 has antitumor activity.
  • HY-123033A
    Nicotinamide riboside chloride

    Sirtuin Endogenous Metabolite Metabolic Disease Neurological Disease
    Nicotinamide riboside Chloride, an orally active NAD + precursor, increases NAD + levels and activates SIRT1 and SIRT3. Nicotinamide riboside Chloride is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities. Nicotinamide riboside Chloride reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease.
  • HY-123033
    Nicotinamide riboside

    Sirtuin Endogenous Metabolite Metabolic Disease Neurological Disease
    Nicotinamide riboside, an orally active NAD + precursor, increases NAD + levels and activates SIRT1 and SIRT3. Nicotinamide riboside is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities. Nicotinamide riboside reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease.
  • HY-13771A
    Ursodeoxycholic acid sodium

    Ursodeoxycholate sodium; Ursodiol sodium; UCDA sodium

    GPCR19 FXR Endogenous Metabolite Cancer Metabolic Disease Inflammation/Immunology
    Ursodeoxycholic acid (Ursodeoxycholate) sodium is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid sodium acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid sodium can be used for the research of a variety of hepatic and gastrointestinal diseases. Orally active.
  • HY-105685
    SRX246

    Vasopressin Receptor Neurological Disease
    SRX246 is a potent, CNS-penetrant, highly selective, orally bioavailable vasopressin 1a (V1a) receptor antagonist (Ki=0.3 nM for human V1a). SRX246 has no interaction at V1b and V2 receptors. SRX246 also displays negligible binding at 64 others receptors classes, including 35 G-proteincoupled receptors. SRX246 can be used for treatment of stress-related disorders.
  • HY-13771
    Ursodeoxycholic acid

    Ursodeoxycholate; Ursodiol; UDCA

    GPCR19 FXR Endogenous Metabolite Metabolic Disease Cancer
    Ursodeoxycholic acid (Ursodeoxycholate) is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Orally active.
  • HY-12736
    GSK143

    Syk PERK Cancer Inflammation/Immunology
    GSK143 is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 inhibits phosphorylated Erk (pErk: pIC50=7.1). GSK143 reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice.
  • HY-12736A
    GSK143 dihydrochloride

    Syk PERK Cancer Inflammation/Immunology
    GSK143 dihydrochloride is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 dihydrochloride inhibits phosphorylated Erk (pErk: pIC50=7.1). GSK143 dihydrochloride reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice.
  • HY-109014
    Tenofovir exalidex

    CMX-157

    HIV HBV Nucleoside Antimetabolite/Analog Infection
    Tenofovir exalidex (CMX157) is a lipid conjugate of the acyclic nucleotide analog Tenofovir with activity against both wild-type and antiretroviral drug-resistant HIV strains, including multidrug nucleoside/nucleotide analog-resistant viruses. Tenofovir exalidex is active against all major subtypes of HIV-1 and HIV-2 in fresh human PBMCs and against all HIV-1 strains evaluated in monocyte-derived macrophages, with EC50s ranging between 0.2 and 7.2 nM. CMX157 is orally available and has no apparent toxicity. Tenofovir exalidex also shows antiviral activity against HBV.
  • HY-144112
    HIV-1 inhibitor-13

    HIV Infection
    HIV-1 inhibitor-13 (compound 16c) is a orally active and potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI), with IC50 of 0.14 μM (HIV-1 RT). HIV-1 inhibitor-13 shows activity against a panel of HIV-1 resistant strains, with EC50 values of 2.85-18.0 nM.
  • HY-W062904
    Laquinimod sodium

    ABR-215062 sodium

    NF-κB Apoptosis Inflammation/Immunology Neurological Disease
    Laquinimod (ABR-215062) sodium, an orally available carboxamide derivative, is a potent immunomodulator which prevents neurodegeneration and inflammation in the central nervous system. Laquinimod sodium reduces astrocytic NF-κB activation to protect from Cuprizone-induced demyelination. Laquinimod sodium has the potential for relapsing remitting (RR) and chronic progressive (CP) forms of multiple sclerosis (MS; RRMS or CPMS) as well as neurodegenerative diseases research.
  • HY-144632
    Antifungal agent 22

    Fungal Infection
    Antifungal agent 22 (compound D16) is a potential and orally active antifungal agent for CM (cryptococcal meningitis), with an IC50 of 0.5 μg/mL. Antifungal agent 22 can penetrate the blood-brain barrier and kill the C. neoformans H99 cells by destroying the integrity of fungal cell membranes. Antifungal agent 22 shows selective anti-Cryptococcus activity with good metabolic stability and low cytotoxicity.
  • HY-13010
    Laquinimod

    ABR-215062

    NF-κB Apoptosis Inflammation/Immunology
    Laquinimod (ABR-215062), an orally available carboxamide derivative, is a potent immunomodulator which prevents neurodegeneration and inflammation in the central nervous system. Laquinimod reduces astrocytic NF-κB activation to protect from Cuprizone-induced demyelination. Laquinimod has the potential for relapsing remitting (RR) and chronic progressive (CP) forms of multiple sclerosis (MS; RRMS or CPMS) as well as neurodegenerative diseases research.
  • HY-132302A
    Hu7691 free base

    Akt PKA PKC ROCK Ribosomal S6 Kinase (RSK) SGK Cancer
    Hu7691 free base is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 free base inhibits tumor growth and enables decrease of cutaneous toxicity in mice.
  • HY-70053A
    Fesoterodine L-mandelate

    mAChR Metabolic Disease Neurological Disease
    Fesoterodine L-mandelate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine L-mandelate is used for the overactive bladder (OAB).
  • HY-108713
    Famitinib

    SHR1020

    VEGFR PDGFR Apoptosis Cancer
    Famitinib (SHR1020), an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively. Famitinib exerts powerful antitumor activity in human gastric cancer cells and xenografts. Famitinib triggers apoptosis.
  • HY-115993
    CDK4/6-IN-10

    CDK Apoptosis Cancer
    CDK4/6-IN-10 is a potent, selective and orally active CDK4 and CDK6 inhibitor with IC50s of 22 nM and 10 nM, respectively. CDK4/6-IN-10 shows antitumor activity. CDK4/6-IN-10 has the potential for the research of Multiple myeloma (MM).
  • HY-115620
    AQX-016A

    Phosphatase PI3K TNF Receptor Inflammation/Immunology
    AQX-016A is an orally active and potent SHIP1 agonist. AQX-016A can activate recombinant SHIP1 enzyme in vitro and stimulate SHIP1 activity. AQX-016A also can inhibit the PI3K pathway and TNFa production, can be useful for various inflammatory diseases research.
  • HY-120878
    CXCR2-IN-2

    CXCR Inflammation/Immunology
    CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM.
  • HY-101291
    Iberdomide

    CC-220

    Ligands for E3 Ligase Apoptosis Inflammation/Immunology Cancer
    Iberdomide (CC-220) is an orally active and potent cereblon (CRBN) E3 ligase modulator (CELMoD) with an IC50 of ~150 nM for cereblon-binding affinity. Iberdomide, a derivative of Thalidomide (HY-14658), has antitumor and immunostimulatory activities.
  • HY-10456
    TAK-715

    p38 MAPK Casein Kinase Inflammation/Immunology
    TAK-715 is an orally active and potent p38 MAPK inhibitor with IC50s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model.
  • HY-103112A
    SB 243213 dihydrochloride

    5-HT Receptor Neurological Disease
    SB 243213 dihydrochloride is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 dihydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 dihydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.
  • HY-116749
    Ethaselen

    BBSKE

    Others Cancer
    Ethaselen (BBSKE) is an orally active, selective thioredoxin reductase (TrxR) inhibitor with IC50s of 0.5 and 0.35 μM for the wild-type human TrxR1 and rat TrxR1, respectively. Ethaselen specifically binds to the unique selenocysteine-cysteine redox pair in the C-terminal active site of mammalian TrxR1. Ethaselen, an organoselenium compound, is a potent antitumor candidate that exerts potent inhibition on non-small cell lung cancer (NSCLC) by targeting TrxR.
  • HY-103112B
    SB 243213

    5-HT Receptor Neurological Disease
    SB 243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.
  • HY-103112
    SB 243213 hydrochloride

    5-HT Receptor Neurological Disease
    SB 243213 hydrochloride is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 hydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 hydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.
  • HY-144293
    HDAC-IN-31

    Apoptosis HDAC Cancer
    HDAC-IN-31 is a potent, selective and orally active HDAC inhibitor with IC50s of 84.90, 168.0, 442.7, >10000 nM for HDAC1, HDAC2, HDAC3, HDAC8, respectively. HDAC-IN-31 induces apoptosis and cell cycle arrests at G2/M phase. HDAC-IN-31 shows good antitumor efficacy. HDAC-IN-31 has the potential for the research of diffuse large B-cell lymphoma.
  • HY-123033B
    Nicotinamide riboside tartrate

    Sirtuin Metabolic Disease Neurological Disease
    Nicotinamide riboside tartrate, an orally active NAD + precursor, increases NAD + levels and activates SIRT1 and SIRT3. Nicotinamide riboside tartrate is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities. Nicotinamide riboside tartrate reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease.
  • HY-123033C
    Nicotinamide riboside malate

    Sirtuin Metabolic Disease Neurological Disease
    Nicotinamide riboside malate, an orally active NAD + precursor, increases NAD + levels and activates SIRT1 and SIRT3. Nicotinamide riboside malate is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities. Nicotinamide riboside malate reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease.
  • HY-120184
    VU0467485

    AZ13713945

    mAChR Neurological Disease
    VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity.
  • HY-100709
    ZPCK

    SL-01

    Nucleoside Antimetabolite/Analog DNA/RNA Synthesis Autophagy Apoptosis Cancer
    ZPCK is an oral active prodrug of gemcitabine that was designed for improved oral bioavailability.
  • HY-103309A
    ML218 hydrochloride

    Calcium Channel Neurological Disease
    ML218 hydrochloride is a potent, selective and orally active T-type Ca 2+ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC50s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 hydrochloride inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 hydrochloride has no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. ML218 hydrochloride can penetrate the blood-brain barrier.
  • HY-103309
    ML218

    Calcium Channel Neurological Disease
    ML218 is a potent, selective and orally active T-type Ca 2+ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC50s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 has no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. ML218 can penetrate the blood-brain barrier.
  • HY-143885
    JAK1/TYK2-IN-3

    JAK Inflammation/Immunology
    JAK1/TYK2-IN-3 is a potent, selective and orally active dual TYK2/JAK1 inhibitor with IC50 values of 6 and 37 nM, respectively. JAK1/TYK2-IN-3 also shows selectively relative to JAK2 (IC50=140 nM) and JAK3 (IC50=362 nM). JAK1/TYK2-IN-3 shows anti-inflammatory effect by regulating the expression of related TYK2/JAK1-regulated genes, as well as the formation of Th1, Th2, and Th17 cells.
  • HY-111360
    SPL-707

    γ-secretase Inflammation/Immunology
    SPL-707 is an orally active, selective signal peptide peptidase-like 2a (SPPL2a) inhibitor with an IC50 of 77 nM for hSPPL2a. SPL-707 inhibits γ-secretase (IC50=6.1 μM) and SPP (IC50=3.7 μM). SPL-707 has the potential for autoimmune diseases research by targeting B cells and dendritic cells.
  • HY-W107024
    BMS-986260

    TGF-β Receptor Cancer Inflammation/Immunology
    BMS-986260, an immuno-oncology agent, is a potent, selective, and orally active TGFβR1 inhibitor (IC50=1.6 nM). BMS-986260 displays exquisite selectivity for TGFβR1 over its isozyme TGFβR2, as well as in a panel of more than 200 kinases examined. BMS-986260 inhibits TGFβ mediated nuclear translocation of pSMAD2/3 in MINK and NHLF cells lines with an IC50 of 350 nM and 190 nM, respectively.
  • HY-W063968
    RO8191

    CDM-3008; RO4948191

    IFNAR JAK STAT HCV HBV Infection
    RO8191 (CDM-3008), an imidazonaphthyridine compound, is an orally active and potent interferon (IFN) receptor agonist. RO8191 directly binds to IFNα/β receptor 2 (IFNAR2) and activates IFN-stimulated genes (ISGs) expression and JAK/STAT phosphorylation. RO8191 shows antiviral activity against both HCV and EMCV with an IC50 of 200 nM for HCV replicon. RO8191 is a cccDNA modulator (CDM) through interferon-like activity and has anti-HBV activity.
  • HY-137141
    16-Keto Aspergillimide

    SB202327

    Parasite Infection
    16-Keto Aspergillimide (SB202327) is an anthelmintic agent isolated from Aspergillus strain IMI 337664.
  • HY-12564
    Phthalazinone pyrazole

    Aurora Kinase Cancer
    Phthalazinone pyrazole is a potent, selective, and orally active inhibitor of Aurora-A kinase with an IC50 of 0.031 μM. Phthalazinone pyrazole can arrests mitosis and subsequently inhibit tumor growth via apoptosis of proliferating cells. Phthalazinone pyrazole suppresses the epithelial-mesenchymal transition (EMT) during the differentiation of hepatocyte-like cells (HLCs) from human embryonic stem cells.
  • HY-B1367
    Carbenoxolone disodium

    Gap Junction Protein Infection Inflammation/Immunology
    Carbenoxolone disodium is the active metabolite of Glycyrrhizic acid (HY-N0184) and the inhibitor of human 11β-HSD and bacterial 3α, 20β-HSD. Carbenoxolone disodium is an uncoupling agent for gap junctions and a potent inhibitor of Vaccinia virus replication. Carbenoxolone disodium is used for the study of peptic, esophageal and oral ulceration and inflammation.
  • HY-136208
    TAN-452

    Opioid Receptor Neurological Disease
    TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioid receptor (KOR; Ki=5.31 nM and Kb=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control.
  • HY-19620A
    Branaplam hydrochloride

    LMI070 hydrochloride; NVS-SM1 hydrochloride

    DNA/RNA Synthesis Potassium Channel Cancer
    Branaplam (LMI070; NVS-SM1) hydrochloride is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC50 of 20 nM for SMN. Branaplam hydrochloride inhibits human-ether-a-go-go-related gene (hERG) with an IC50 of 6.3 μM. Branaplam hydrochloride elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model.
  • HY-19620
    Branaplam

    LMI070; NVS-SM1

    DNA/RNA Synthesis Potassium Channel Cancer
    Branaplam (LMI070; NVS-SM1) is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC50 of 20 nM for SMN. Branaplam inhibits human-ether-a-go-go-related gene (hERG) with an IC50 of 6.3 μM. Branaplam elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model.
  • HY-123938
    CYH33

    PI3K Cancer
    CYH33 is an orally active, highly selective PI3Kα inhibitor with IC50s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. CYH33 inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. CYH33 has potent activity against solid tumors.
  • HY-10583
    Y-27632 dihydrochloride

    ROCK Apoptosis Cancer
    Y-27632 dihydrochloride is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively. Y-27632 dihydrochloride attenuates Doxorubicin-induced apoptosis of human cardiac stem cells. Y-27632 also suppresses dissociation-induced apoptosis of murine prostate stem/progenitor cells. Y-27632 dihydrochloride primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation.
  • HY-129239
    Farudodstat

    ASLAN003

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Apoptosis Cancer
    Farudodstat (ASLAN003) is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 35 nM for human DHODH enzyme. Farudodstat inhibits protein synthesis via activation of AP-1 transcription factors. Farudodstat induces apoptosis and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice.
  • HY-103441
    JNJ28871063 hydrochloride

    EGFR Cancer
    JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2.
  • HY-139990
    CSF1R-IN-3

    c-Fms Cancer
    CSF1R-IN-3 (compound 21) is a potent and orally active CSF-1R inhibitor (IC50=2.1 nM). CSF1R-IN-3 is a potent antiproliferative activity against colorectal cancer cells. CSF1R-IN-3 inhibits the progression of colorectal cancer by suppressing the migration of macrophages, reprograming M2-like macrophages to the M1 phenotype, and enhancing the antitumor immunity.
  • HY-123938A
    CYH33 methanesulfonate

    PI3K Cancer
    CYH33 methanesulfonate is an orally active, highly selective PI3Kα inhibitor with IC50s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. CYH33 methanesulfonate inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. CYH33 methanesulfonate has potent activity against solid tumors.
  • HY-112823A
    Almonertinib mesylate

    HS-10296 mesylate

    EGFR Cancer
    Almonertinib (HS-10296) mesylate is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib mesylate is used for the research of the non-small cell lung cancer.
  • HY-112823
    Almonertinib

    HS-10296

    EGFR Cancer
    Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer.
  • HY-112823B
    Almonertinib hydrochloride

    HS-10296 hydrochloride

    EGFR Cancer
    Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib hydrochloride is used for the research of the non-small cell lung cancer.
  • HY-10626
    T0901317

    LXR FXR ROR Apoptosis Cancer Metabolic Disease Cardiovascular Disease
    T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα. T0901317 activates FXR with an EC50 of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice.
  • HY-114657A
    Benproperine phosphate

    Arp2/3 Complex Cancer Inflammation/Immunology
    Benproperine phosphate is an orally active, potent actin-related protein 2/3 complex subunit 2 (ARPC2) inhibitor. Benproperine phosphate attenuates the actin polymerization rate of action polymerization nucleation by impairing Arp2/3 function. Benproperine phosphate has the potential for a cough suppressant and suppresses cancer cell migration and tumor metastasis.
  • HY-B0996
    Hexetidine

    NSC-17764

    Bacterial Fungal Infection
    Hexetidine is an orally active antiseptic with broad antibacterial and antifungal activity. Hexetidine give important potential for treatment of oral infections.
  • HY-19411
    SSR180711 hydrochloride

    nAChR Neurological Disease
    SSR180711 hydrochloride is an orally active, selective and reversible α7 acetylcholine nicotinic receptor (n-AChRs) partial agonist. SSR180711 hydrochloride can act on rat α7 n-AChR (Ki=22 nM; IC50=30 nM) and human α7 n-AChR (Ki=14 nM; IC50=18 nM). SSR180711 hydrochloride increases glutamatergic neurotransmission, ACh release and long-term potentiation (LTP) in the hippocampus.
  • HY-147660
    IMMH001

    LPL Receptor Inflammation/Immunology
    IMMH001, also called SYL930, is an orally active, potent and selective S1P1 (sphingosine-1-phosphate receptor 1) agonist. IMMH001 decreased levels of both chemokines and proinflammatory cytokines, including IL-1β, IL-5, IL-18, IP10, CCL3, and CCL5. IMMH001 can be used for rheumatoid arthritis (RA) research.
  • HY-14945
    Remogliflozin etabonate

    GSK189075

    SGLT Metabolic Disease
    Remogliflozin etabonate (GSK189075) is an orally active, selective and low-affinity sodium glucose cotransporter (SGLT2) inhibitor with Ki values of 1.95 μM, 2.14 μM, 43.1 μM, 8.57 μM for hSGLT2, rSGLT2, hSGLT1, rSGLT1, respectively. Remogliflozin etabonate is a prodrug based on benzylpyrazole glucoside and is metabolized to its active form, Remogliflozin, in the body. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models.
  • HY-124858
    SC99

    STAT JAK Apoptosis Cancer Cardiovascular Disease
    SC99 is an orally active, selective STAT3 inhibitor targeting JAK2-STAT3 pathway. SC99 docks into the ATP-binding pocket of JAK2. SC99 inhibits phosphorylation of JAK2 and STAT3 with no effects on the other kinases associated with STAT3 signaling. SC99 inhibits platelet activation, aggregation and displays potent anti-myeloma, anti-thrombotic activities.
  • HY-101682
    SCH 42495

    Neprilysin Cardiovascular Disease
    SCH 42495 is an orally active neutral metalloendopeptidase (NEP) inhibitor with antihypertensive effect. SCH 42495 is the orally active ethylester prodrug of SCH 42354.
  • HY-135699
    TD52

    Apoptosis Phosphatase Akt Cancer
    TD52, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 has less p-EGFR inhibition and has potent anti-cancer activity.
  • HY-B0216
    Ethynyl Estradiol

    17α-Ethynylestradiol; Ethynylestradiol

    Estrogen Receptor/ERR Endogenous Metabolite Endocrinology Cancer
    Ethynyl Estradiol (17α-Ethynylestradiol;Ethynylestradiol) is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills.
  • HY-128861A
    ACT001

    PAI-1 STAT PI3K Akt Apoptosis Cancer Inflammation/Immunology
    ACT001 is an orally active PAI-1 inhibitor by inhibiting the phosphorylation of PI3K and AKT. ACT001 inhibits the phosphorylation of STAT3 and PD-L1 expression by directly binding to STAT3. ACT001, a fumarate salt form of DMAMCL (a prodrug of Micheliolide), can cross the blood-brain barrier. ACT001 exerts synergistic effects in combination with Cisplatin (HY-17394) by inhibiting PI3K/AKT pathway in glioma. ACT001 has potent anti-glioblastoma (GBM) activity and immunomodulatory effects.
  • HY-120944
    BAY-7598

    MMP Inflammation/Immunology
    BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.
  • HY-B1045
    Chlorazanil hydrochloride

    Others Metabolic Disease
    Chlorazanil hydrochloride is a orally effective diuretic agent.
  • HY-B1469
    Isosorbide

    D-Isosorbide; Dianhydro-D-glucitol

    Others Metabolic Disease Cardiovascular Disease
    Isosorbide (D-Isosorbide), an orally active vasodilating agent that can be used for the research of heart failure and angina (chest pain). Isosorbide is also an oral hyperosmotic diuretic.
  • HY-101682A
    SCH 42495 racemate

    Neprilysin Cardiovascular Disease
    SCH 42495 racemate is the racemate of SCH 42495. SCH 42495 is an orally active neutral metalloendopeptidase (NEP) inhibitor with antihypertensive effect. SCH 42495 is the orally active ethylester prodrug of SCH 42354.
  • HY-B1658A
    Frovatriptan succinate hydrate

    (R)-Frovatriptan succinate hydrate; SB 209509 succinate hydrate; VML 251 succinate hydrate

    5-HT Receptor Neurological Disease
    Frovatriptan succinate hydrate ((R)-Frovatriptan succinate hydrate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate hydrate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate hydrate has the potential for migraine research.
  • HY-B1658B
    Frovatriptan succinate

    (R)-Frovatriptan succinate; SB 209509 succinate; VML 251 succinate

    5-HT Receptor Neurological Disease
    Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research.
  • HY-131061
    BET bromodomain inhibitor 1

    Epigenetic Reader Domain Cancer
    BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity.
  • HY-B0396
    Tebipenem pivoxil

    L084

    Bacterial Antibiotic Infection
    Tebipenem Pivoxil is a novel oral carbapenem antibiotic.
  • HY-101758
    BM-131246

    Others Metabolic Disease
    BM-131246 is an oral antidiabetic agent.
  • HY-139244S
    Norgestimate D6

    Progesterone Receptor Endocrinology
    Norgestimate D6 is the deuterium labeled Norgestimate. Norgestimate, a synthetic progesterone analog, is an orally active progestin with highly selective progestational activity and minimal androgenicity. Norgestimate is used for an oral contraceptive.
  • HY-B1894A
    Cefetamet pivoxil hydrochloride

    Ro 15-8075

    Bacterial Antibiotic Infection
    Cefetamet pivoxil hydrochloride is an oral third generation cephalosporin antibiotic.
  • HY-16635
    Setipiprant

    ACT-129968; KYTH-105

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Setipiprant is an orally available, selective CRTH2 antagonist.
  • HY-U00011
    Temarotene

    Ro 15-0778

    Others Inflammation/Immunology
    Temarotene is an orally administered, particular arotinoid.
  • HY-101682B
    (R)-SCH 42495

    Others Others
    (R)-SCH 42495 is the less active enantiomer of SCH 42495. SCH 42495 is an orally active neutral metalloendopeptidase (NEP) inhibitor with antihypertensive effect. SCH 42495 is the orally active ethylester prodrug of SCH 42354.
  • HY-143445
    EGFR-IN-48

    EGFR Cancer
    EGFR-IN-48 is a potent and orally active EGFR inhibitor with IC50s of 0.193 nM, 0.251 nM, 10.4 nM for EGFR d19/TM/CS, EGFR LR/TM/CS, EGFR WT, respectively. EGFR-IN-48 inhibits the proliferation of BaF3 EGFR del19/T790M/C797S and PC-9 EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively.
  • HY-B1149A
    Bacampicillin hydrochloride

    Bacterial Antibiotic Infection
    Bacampicillin hydrochloride is a penicillin antibiotic, is a prodrug of ampicillin with improved oral bioavailability.
  • HY-U00389
    WQ3810

    KPI-10 free base

    Bacterial Infection
    WQ3810 is an orally active fluoroquinolone, with potent antibacterial activities.
  • HY-16500
    Tolrestat

    AY-27773

    Aldose Reductase Cancer
    Tolrestat is a potent, orally active aldose reductase inhibitor with IC50 of 35 nM.
  • HY-B1382
    Pempidine

    1,2,2,6,6-Pentamethylpiperidine

    Others Neurological Disease
    Pempidine is a ganglion-blocking drug, introduced as an oral treatment for hypertension.
  • HY-16445A
    CNDAC

    Nucleoside Antimetabolite/Analog Cancer
    CNDAC is a major metabolite of oral drug sapacitabine, and a nucleoside analog.
  • HY-142663
    OI338

    Insulin Receptor Metabolic Disease
    OI338 is an orally available, ultralong-acting insulin analogue.
  • HY-B1149
    Bacampicillin

    Bacterial Antibiotic Infection
    Bacampicillin is a penicillin antibiotic, is a prodrug of ampicillin with improved oral bioavailability.
  • HY-111485
    INCB-057643

    Epigenetic Reader Domain Apoptosis Cancer
    INCB-057643 is a novel, orally bioavailable BET inhibitor.
  • HY-114703
    Eslicarbazepine

    BIA 2-194

    Others Neurological Disease
    Eslicarbazepine is an oral anticonvulsant indicated for the adjunctive treatment of partial seizures.
  • HY-119824
    Trofosfamide

    Bacterial Cancer
    Trofosfamide is an orally bioavailable oxazaphosphorine derivative with antineoplastic activity.
  • HY-13017A
    Ivacaftor benzenesulfonate

    VX-770 benzenesulfonate

    CFTR Autophagy Endocrinology
    Ivacaftor benzenesulfonate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment.
  • HY-111386
    E-7386

    Epigenetic Reader Domain Cancer
    E-7386 is an orally active CBP/beta-catenin modulator.
  • HY-142644
    ATX inhibitor 7

    Phosphodiesterase (PDE) Inflammation/Immunology
    ATX inhibitor 7 is a autotaxin inhibitor and shows good oral exposure.
  • HY-114530
    LY2452473

    Androgen Receptor Cancer Metabolic Disease
    LY2452473 is an orally bioavailable, selective androgen receptor modulator (SARM).
  • HY-B0401
    Tolbutamide

    Potassium Channel Autophagy Metabolic Disease Cancer
    Tolbutamide is a first generation potassium channel blocker, sulfonylurea oral hypoglycemic drug.
  • HY-115874
    BMS-753426

    CCR Others
    BMS-753426 is a potent and orally bioavailable antagonist of CCR2.
  • HY-145356
    HbF inducer-1

    Others Others
    HbF inducer-1 is an orally bioavailable fetal hemoglobin inducer.
  • HY-B0917
    Bromindione

    Fluidane; Halinone

    Others Cardiovascular Disease
    Bromindione is a potent, long-acting, inandione-derived, oral anticoagulant compound.
  • HY-106349
    Fosteabine

    Cytarabine ocfosfate; YNK 01

    Nucleoside Antimetabolite/Analog Cancer
    Fosteabine is an oral and prodrug analogue of cytarabine which is resistant to deoxycytidine deaminase.
  • HY-100830
    NCB-0846

    Wnt MAP4K Cancer
    NCB-0846 is an orally available TNIK inhibitor with an IC50 of 21 nM.
  • HY-U00041
    Pivalopril

    Pivopril; RHC 3659(S)

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Pivalopril is a new orally active angiotensin converting enzyme (ACE) inhibitor.
  • HY-16445
    Sapacitabine

    CS682; CYC682

    Nucleoside Antimetabolite/Analog Cancer
    Sapacitabine is an orally available nucleoside analog prodrug that is structurally related to cytarabine.
  • HY-17630
    Edasalonexent

    CAT-1004

    NF-κB Metabolic Disease
    Edasalonexent (CAT-1004) is an orally bioavailable NF-κB inhibitor.
  • HY-12507
    GSK-7975A

    Calcium Channel Inflammation/Immunology
    GSK-7975A is a potent and orally available CRAC channel inhibitor.
  • HY-16774
    Vericiguat

    BAY1021189

    Guanylate Cyclase Cardiovascular Disease
    Vericiguat (BAY1021189) is a potent, orally available and soluble guanylate cyclase stimulator.
  • HY-10159
    Nilotinib

    AMN107

    Bcr-Abl Autophagy Cancer
    Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
  • HY-10304
    Orbofiban

    Others Cardiovascular Disease
    Orbofiban is an orally active platelet GPIIb/IIIa antagonist that inhibits platelet aggregation.
  • HY-13254
    A-674563

    Akt Cancer
    A-674563 is an orally active and selective Akt1 inhibitor with a Ki of 11 nM.
  • HY-16445B
    CNDAC hydrochloride

    Nucleoside Antimetabolite/Analog Drug Metabolite Cancer
    CNDAC hydrochloride is a metabolite of the orally active agent sapacitabine, and a nucleoside analog.
  • HY-17378
    Dabigatran (ethyl ester)

    Thrombin Cardiovascular Disease
    Dabigatran ethyl ester is an emerging oral anticoagulant which is a direct inhibitor of thrombin activity.
  • HY-19887
    Tilapertin

    AMG747

    GlyT Neurological Disease
    Tilapertin is an oral inhibitor of glycine transporter type-1 (GlyT1).
  • HY-111068
    KD-3010

    PPAR Metabolic Disease
    KD-3010 is a potent, orally active, and selective PPARδ agonist.
  • HY-106570
    Tripamide

    Potassium Channel Metabolic Disease
    Tripamide is an orally active sulfonamide-derived diuretic antihypertensive agent.
  • HY-100329
    CGP 65015

    Others Others
    CGP 65015 is an oral iron chelator, which can mobilize iron deposits.
  • HY-142661
    BAY 1217224

    Thrombin Neurological Disease
    BAY 1217224 is a neutral, non-prodrug Thrombin inhibitor with good oral pharmacokinetics.
  • HY-12802
    AF38469

    Neurotensin Receptor Neurological Disease
    AF38469 is a selective, orally bioavailable Sortilin inhibitor with an IC50 value of 330 nM.
  • HY-19163
    SC-52012

    Others Cardiovascular Disease
    HY-19163 is an orally active fibrinogen receptor antagonist, with antiplatelet activities.
  • HY-106067A
    Dazoxiben

    Others Inflammation/Immunology
    Dazoxiben is a potent and orally active thromboxane (TX) synthase inhibitor.
  • HY-N8117
    Bisabolol oxide A

    Others Inflammation/Immunology
    Bisabolol oxide A possesses antihyperalgesic and antiedematous effects with oral activity.
  • HY-14885
    Eliglustat

    Genz 99067

    Others Metabolic Disease
    Eliglustat is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC50 of 24 nM.
  • HY-145119AS
    VV116

    JT001; GS-621763-d1 hydrobromide

    SARS-CoV RSV Influenza Virus Infection
    VV116 (JT001) is an orally active nucleoside antiviral agent against SARS-CoV-2 and respiratory syncytial virus (RSV) infection. VV116 has favorable oral bioavailability, excellent in vitro antiviral activity and selectivity.
  • HY-15604
    AZD1208

    Pim Autophagy Apoptosis Cancer
    AZD1208 is an orally bioavailable, highly selective PIM kinases inhibitor.
  • HY-N0565
    Doxycycline

    MMP Bacterial Parasite Antibiotic Infection
    Doxycycline, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor.
  • HY-107986
    GNE-6776

    Deubiquitinase Cancer
    GNE-6776 is a selective and orally bioavailable USP7 inhibitor.
  • HY-16069
    Tucatinib

    Irbinitinib; ARRY-380; ONT-380

    EGFR Cancer
    Tucatinib (Irbinitinib) is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.
  • HY-10314
    Lotrafiban

    SB-214857

    Others Cardiovascular Disease
    Lotrafiban is an orally-active platelet GPIIb/IIIa blocker for treatment of coronary and cerebrovascular disease.
  • HY-110095
    (±)-CPSI-1306

    Others Metabolic Disease Inflammation/Immunology
    (±)-CPSI-1306 is an orally available antagonist of macrophage migration inhibitory factor (MIF).
  • HY-145369
    DS34942424

    Opioid Receptor Neurological Disease
    DS34942424 is an orally potent analgesic without mu opioid receptor agonist activity.
  • HY-76260
    Faropenem sodium

    Bacterial Antibiotic Infection
    Faropenem sodium is an orally bioavailable penem antibiotic which can efficiently kill Mycobacterium tuberculosis.
  • HY-N0565A
    Doxycycline hydrochloride

    MMP Bacterial Antibiotic Infection
    Doxycycline hydrochloride, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor.
  • HY-139588
    Vemircopan

    ALXN2050; ACH 0145228; ACH-5228

    Complement System Inflammation/Immunology
    Vemircopan (ALXN2050) is an orally active complement factor D inhibitor.
  • HY-15199
    Agerafenib hydrochloride

    CEP-32496 hydrochloride; RXDX-105 hydrochloride

    Raf Cancer
    Agerafenib hydrochloride is a highly potent and orally efficacious inhibitor of BRAF V600E with a Kd of 14 nM.
  • HY-103519
    rac-BHFF

    GABA Receptor Neurological Disease
    rac-BHFF is a potent and orally active allosteric enhancer of GABAB receptor.
  • HY-11077
    SR 146131

    Cholecystokinin Receptor Metabolic Disease Endocrinology
    SR 146131 is a potent, orally available, and selective nonpeptide (cholecystokinin 1) receptor agonist.
  • HY-109074
    Seliforant

    SENS-111

    Histamine Receptor Inflammation/Immunology
    Seliforant (SENS-111) is a selective and orally histamine H4 receptor antagonist.
  • HY-18958
    CCT245737

    Checkpoint Kinase (Chk) Cancer
    CCT245737 is an orally active and seletive Chk1 inhibitor, with an IC50 of 1.3 nM.
  • HY-12419
    BMS-983970

    Notch Cancer
    BMS-983970 is an oral pan-Notch inhibitor for the treatment of multiplecancers.
  • HY-75957
    DMP 777

    L-694458

    Elastase Inflammation/Immunology
    DMP 777 is a potent, selective, and orally active human leukocyte elastase (HLE) inhibitor.
  • HY-U00363
    CHEMBL333994

    FK-480

    Cholecystokinin Receptor Endocrinology
    CHEMBL333994 is a potent and orally effective Cholecystokinin A (CCK-A) antagonist, with an IC50 of 0.67 nM.
  • HY-10180
    MLN8054

    Aurora Kinase Cancer
    MLN8054 is a potent, selective and orally available aurora A kinase inhibitor with an IC50 of 4 nM.
  • HY-A0145
    Phenprocoumon

    Others Others
    Phenprocoumon is a coumarin derivative that acts as a long acting oral anticoagulant and an antagonist of vitamin K.
  • HY-145355
    IDO1-IN-12

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO1-IN-12 is a potent and orally available IDO1 inhibitor.
  • HY-15604A
    AZD1208 hydrochloride

    Pim Autophagy Apoptosis Cancer
    AZD1208 hydrochloride is an orally bioavailable, highly selective PIM kinases inhibitor.
  • HY-14390
    LAS101057

    Adenosine Receptor Inflammation/Immunology
    LAS101057 is a potent, selective, and orally efficacious A2B receptor antagonist.
  • HY-101830
    Wy 49051

    Histamine Receptor Inflammation/Immunology Endocrinology
    Wy 49051 is a potent, orally active H1 receptor antagonist, with IC50 of 44 nM.
  • HY-112298
    DS88790512

    TRP Channel Cardiovascular Disease
    DS88790512 is a potent, selective, and orally bioavailable TRPC6 inhibitor with an IC50 of 11 nM.
  • HY-12727
    EPZ015666

    GSK3235025

    Histone Methyltransferase Cancer
    EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 with an IC50 of 22 nM.
  • HY-B0920
    Tolazamide

    U-17835

    Others Endocrinology
    Tolazamide is an oral blood glucose lowering drug used for people with Type 2 diabetes.
  • HY-14779
    Riociguat

    BAY 632521

    Guanylate Cyclase Cardiovascular Disease
    Riociguat is an oral stimulator of soluble guanylate cyclase (sGC) used in the treatment of pulmonary hypertension.
  • HY-106547
    Rilmazafone

    GABA Receptor Neurological Disease
    Rilmazafone is a benzodiazepine ω ligand and an orally active sleep inducer.
  • HY-10004
    Faropenem daloxate

    Faropenem medoxil

    Bacterial Antibiotic Infection
    Faropenem daloxate is the first oral penem in a new class of beta-lactam antibiotics.
  • HY-14885A
    Eliglustat hemitartrate

    Genz-112638; Eliglustat tartrate

    Others Metabolic Disease
    Eliglustat hemitartrate is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC50 of 24 nM.
  • HY-19323
    Ceralasertib

    AZD6738

    ATM/ATR Cancer
    Ceralasertib (AZD6738) is an orally active and bioavailable inhibitor of ATR kinase with an IC50 of 1 nM.
  • HY-139885
    c-Myc inhibitor 4

    c-Myc Cancer
    c-Myc inhibitor 4 is a potent, orally bioavailable c-MYC-reducing compound.
  • HY-U00207
    MEN11467

    Neurokinin Receptor Neurological Disease Endocrinology
    MEN11467 is a selective and orally- effective peptidomimetic tachykinin NK1 receptor antagonist.
  • HY-114299
    Salcaprozate sodium

    SNAC

    Others Others
    Salcaprozate sodium (SNAC), an oral absorption promoter, and has the potential as a delivery agent for oral forms of heparin and insulin. Salcaprozate sodium could increase passive transcellular permeation across small intestinal epithelia based on increased lipophilicity arising from non-covalent macromolecule complexation.
  • HY-B0216S1
    Ethynyl Estradiol-d7

    17α-Ethynylestradiol-d7; Ethynylestradiol-d7

    Estrogen Receptor/ERR Endogenous Metabolite Endocrinology Cancer
    Ethynyl Estradiol-d7 (17α-Ethynylestradiol-d7) is the deuterium labeled Ethynyl Estradiol. Ethynyl Estradiol (17α-Ethynylestradiol;Ethynylestradiol) is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills.
  • HY-B0216S
    Ethynyl Estradiol-d4

    17α-Ethynylestradiol-d4; Ethynylestradiol-d4

    Estrogen Receptor/ERR Endogenous Metabolite Endocrinology Cancer
    Ethynyl Estradiol-d4 (17α-Ethynylestradiol-d4) is the deuterium labeled Ethynyl Estradiol. Ethynyl Estradiol (17α-Ethynylestradiol;Ethynylestradiol) is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills.
  • HY-144668
    RdRP-IN-4

    Influenza Virus Infection
    RdRP-IN-4 (compound 11q), an aryl benzoyl hydrazide analog, is an orally active influenza A virus RNA-dependent RNA polymerase (RdRp) inhibitor by interacting with the PB1 subunit. RdRP-IN-4 exhibits potent inhibitory activity against the avian H5N1 flu strain with an EC50 of 18 nM in MDCK cells. RdRP-IN-4 displays excellent potency against the the H1N1 (A/PR/8/34) Flu A strain and Flu B strain (B/Lee/1940) with EC50 values of 53 nM and 20 nM, respectively. RdRP-IN-4 significantly inhibits the expression level of viral nucleoprotein (NP) in a dose-dependent manner. RdRP-IN-4 exhibits significant antiviral activity in infected mice.
  • HY-B0810
    Pivmecillinam

    FL-1039

    Bacterial Antibiotic Infection
    Pivmecillinam (FL-1039) is an orally active prodrug of mecillinam, an extended-spectrum penicillin antibiotic.
  • HY-15246
    TAK-580

    MLN 2480; BIIB-024

    Raf Cancer
    TAK-580 (MLN 2480) is an orally active and selective inhibitor of pan-Raf kinase.
  • HY-15828
    Onvansertib

    NMS-1286937; NMS-P937

    Polo-like Kinase (PLK) Apoptosis Cancer
    NMS-1286937 is a potent, selective and orally available PLK1 inhibitor, with an IC50 of 2 nM.
  • HY-19324
    EPZ031686

    Histone Methyltransferase Cancer
    EPZ031686 is an orally available SMYD3 inhibitor with an IC50 of 3 nM in cell-free assay.
  • HY-145561
    Cudetaxestat

    BLD-0409

    Phosphodiesterase (PDE) Inflammation/Immunology
    Cudetaxestat (BLD-0409) is a potent and orally active autotaxin (ATX) inhibitor.
  • HY-142618
    TNF-α-IN-6

    TNF Receptor Inflammation/Immunology
    TNF-α-IN-6 is an orally efficacious allosteric inhibitor of TNFα (KD = 6.8 nM).
  • HY-13017B
    Ivacaftor hydrate

    VX-770 hydrate

    CFTR Autophagy Endocrinology
    Ivacaftor hydrate (VX-770 hydrate) is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment.
  • HY-B0810A
    Pivmecillinam hydrochloride

    FL-1039 hydrochloride

    Bacterial Antibiotic Infection
    Pivmecillinam hydrochloride (FL-1039 hydrochloride) is an orally active prodrug of mecillinam, an extended-spectrum penicillin antibiotic.
  • HY-17478A
    Magnesium salicylate

    Inflammation/Immunology
    Magnesium salicylate is an orally active analgesic that temporarily relieves minor aches and pains.
  • HY-100408
    GNF-6231

    Porcupine Cancer
    GNF-6231 is a potent, selective, and orally bioavailable Porcupine inhibitor that blocks Wnt signaling.
  • HY-Y0569C
    Potassium Gluconate

    Potassium D-gluconate

    Endogenous Metabolite Fungal Infection
    Potassium Gluconate (Potassium D-gluconate) is an orally active carboxylic acid by the oxidation with antiseptic and chelating properties.
  • HY-132901
    IACS-15414

    Phosphatase Cancer
    IACS-15414 is a potent and orally bioavailable SHP2 inhibitor with an IC50 value of 122 nM.
  • HY-115721
    Antimalarial agent 2

    Parasite Infection
    Antimalarial agent 2 is a novel orally efficacious antimalarials that suggests a fast in vitro killing profile.
  • HY-111358
    TLR7 agonist 1

    Toll-like Receptor (TLR) Infection
    TLR7 agonist 1 is a potent, selective and oral TLR7 agonist with an IC50 of 90 nM.
  • HY-109032
    Firuglipel

    GPR119 Metabolic Disease
    Firuglipel (DS-8500a) is an orally available, potent and selective GPR119 agonist.
  • HY-15968
    Entospletinib

    GS-9973

    Syk Cancer
    Entospletinib (GS-9973) is an orally bioavailable, selective Syk inhibitor with an IC50 of 7.7 nM.
  • HY-11103
    Sitaxsentan sodium

    IPI 1040 sodium; TBC11251 sodium

    Endothelin Receptor Cardiovascular Disease Endocrinology
    Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) is an orally active, highly selective antagonist of endothelin A receptors.
  • HY-14857
    Carotegrast

    Integrin Inflammation/Immunology
    Carotegrast is an orally available α4 integrin receptor inhibitor with anti-inflammatories activities.
  • HY-19883
    Lusutrombopag

    S-888711

    Thrombopoietin Receptor Inflammation/Immunology
    Lusutrombopag is an orally bioavailable thrombopoietin (TPO) receptor agonist, used for treatment of chronic liver disease.
  • HY-B0162A
    Ivabradine hydrochloride

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Ivabradine hydrochloride is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker.
  • HY-B0016
    Capecitabine

    DNA/RNA Synthesis Nucleoside Antimetabolite/Analog Apoptosis Cancer
    Capecitabine is an oral prodrug that is converted to its active metabolite, 5-FU, by thymidine phosphorylase.
  • HY-115777
    ARN-6039

    ROR Neurological Disease
    ARN-6039 is an orally available inverse agonist of RORγ for autoimmune demyelinating disease.
  • HY-145121
    DS96432529

    CDK Metabolic Disease
    DS96432529 is a potent and orally active bone anabolic agent through CDK8 inhibition.
  • HY-14916
    Camobucol

    AGIX 4207

    Others Inflammation/Immunology
    Camobucol (AGIX 4207) is an orally active, phenolic antioxidant and anti-inflammatory compound with antirheumatic properties.
  • HY-B0467A
    Amoxicillin

    Amoxycillin

    Bacterial Antibiotic Infection
    Amoxicillin is an antibiotic with good oral absorption and broad spectrum antimicrobial activity.
  • HY-14178
    VX-11e

    ERK Cancer
    VX-11e is a potent, selective, and orally bioavailable inhibitor of ERK with Ki < 2 nM.
  • HY-16069A
    Tucatinib hemiethanolate

    Irbinitinib hemiethanolate; ARRY-380 hemiethanolate; ONT-380 hemiethanolate

    EGFR Cancer
    Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.
  • HY-13796
    IPSU

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85.
  • HY-118861A
    Enclomiphene citrate

    (E)-Clomiphene citrate; trans-Clomiphene citrate; Enclomifene citrate

    Estrogen Receptor/ERR Inflammation/Immunology
    Enclomiphene citrate is a potent and orally active oestrogen receptor antagonist, with antioestrogenic property.
  • HY-111368
    EBI-1051

    MEK Cancer
    EBI-1051 is a highly potent and orally efficacious MEK inhibitor with an IC50 of 3.9 nM.
  • HY-18690A
    Enasidenib mesylate

    AG-221 mesylate

    Isocitrate Dehydrogenase (IDH) Cancer
    Enasidenib mesylate is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes.
  • HY-B1429
    Chlorpropamide

    Na+/K+ ATPase Endocrinology
    Chlorpropamide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM).
  • HY-117244
    AZD7507

    c-Fms Cancer
    AZD7507 is a potent and orally active CSF-1R inhibitor, with antitumor activity.
  • HY-15412
    HhAntag

    Smo Cancer
    HhAntag is a specific, potent and orally active small molecule SMO antagonist of the Hh pathway.
  • HY-B0576
    Sulfacetamide Sodium

    Bacterial Antibiotic Infection
    Sulfacetamide Sodium is an anti-infective agent that is used topically to treat skin infections and orally for urinary tract infections.
  • HY-13055A
    Telotristat ethyl

    LX1032; LX1606

    Tryptophan Hydroxylase Cancer Neurological Disease
    Telotristat ethyl (LX1032) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.
  • HY-17625
    Acebilustat

    CTX-4430

    Aminopeptidase Inflammation/Immunology
    Acebilustat (CTX-4430) is a leukotriene A4 hydrolase inhibitor, used for an oral antiinflammatory drug.
  • HY-114332
    GNE-8505

    MAP3K Neurological Disease
    GNE-8505 is an orally available inhibitor of Dual leucine zipper kinase (DLK).
  • HY-100026
    PQR620

    mTOR Cancer
    PQR620 is an orally bioavailable and selective brain penetrant inhibitor of mTORC1/2.
  • HY-B0257A
    Dydrogesterone

    Progesterone Receptor Endocrinology
    Dydrogesterone is a potent, orally active progestogen indicated in a wide variety of gynaecological conditions related to progesterone deficiency.
  • HY-16925
    MI-503

    Epigenetic Reader Domain Cancer
    MI-503 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.
  • HY-16902
    RO9021

    Syk Inflammation/Immunology
    RO9021 is an orally bioavailable, novel ATP-competitive inhibitor of SYK, with an average IC50 of 5.6 nM.
  • HY-145354
    FXIa-IN-7

    Factor Xa Cardiovascular Disease
    FXIa-IN-7 is a selective and orally bioavailable factor XIa inhibitor with an IC50 value of 0.4 nM.
  • HY-I0447
    4-Aminosalicylic acid

    Bacterial Antibiotic Infection Inflammation/Immunology
    4-Aminosalicylic acid (ASA) is an orally active antibiotic and has the potential to treat tuberculosis.
  • HY-19741
    A-1331852

    Bcl-2 Family Cancer
    A-1331852 is an orally available BCL-XL selective inhibitor with a Ki of less than 10 pM.
  • HY-107792
    Benurestat

    Bacterial Infection
    Benurestat is an orally active urease inhibitor. Benurestat can be used for infected ureolysis research.
  • HY-111486
    LSZ-102

    Estrogen Receptor/ERR Cancer
    LSZ-102 is a potent, orally bioavailable selective estrogen receptor degrader with an IC50 of 0.2 nM.
  • HY-106446
    Rentiapril

    SA-446

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Rentiapril is an orally active angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity.
  • HY-B0481
    Miglitol

    BAY1099; BAY-m1099

    Others Metabolic Disease
    Miglitol is an oral anti-diabetic drug that acts by inhibiting the ability of the patient to breakdown complex carbohydrates into glucose.
  • HY-109018
    Velagliflozin

    SGLT Metabolic Disease
    Velagliflozin is an orally available sodium-glucose cotransporter 2 (SGLT2) inhibitor, with anti-diabetic activity.
  • HY-100600
    BGG463

    K03859

    CDK Others
    BGG463 (K03859) is an orally active type II CDK2 inhibitor.
  • HY-13742
    Ropidoxuridine

    IPdR

    Others Cancer
    Ropidoxuridine (IPdR) is a novel orally available, halogenated thymidine analog and is a potential radiosensitizer for use in human tumors.
  • HY-145346
    NLG802

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    NLG802 is a prodrug of indoximod, an orally active indoleamine 2,3-dioxygenase (IDO) inhibitor.
  • HY-141895
    Vps34-IN-3

    PI3K Cancer
    Vps34-IN-3 is a potent, selective, and orally bioavailable VPS34 kinase inhibitor.
  • HY-10480
    Fasiglifam

    TAK-875

    Free Fatty Acid Receptor Metabolic Disease
    Fasiglifam (TAK-875) is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 72 nM.
  • HY-19809
    MI-463

    Epigenetic Reader Domain Cancer
    MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.
  • HY-139901
    Chk1-IN-6

    Checkpoint Kinase (Chk) Cancer
    Chk1-IN-6 is a potent, selective, and orally bioavailable CHK1 inhibitor candidate.
  • HY-15333
    ZK-261991

    VEGFR Inflammation/Immunology
    ZK-261991 is an orally active VEGFR tyrosine kinase inhibitor with an IC50 of 5 nM for VEGFR2.
  • HY-139436
    ARD-2585

    PROTACs Androgen Receptor Cancer
    ARD-2585 is an exceptionally potent and orally active PROTAC degrader of androgen receptor.
  • HY-14932
    Pafuramidine

    DB289

    Parasite Antibiotic Infection
    Pafuramidine (DB289) is an orally bioavailable prodrug of furamidine, which has activity against Pneumocystis pneumonia.
  • HY-B0568
    Deferiprone

    HCV Ferroptosis Cardiovascular Disease Cancer
    Deferiprone is the only orally active iron-chelating drug to be used therapeutically in conditions of transfusional iron overload.
  • HY-19984
    CCT-251921

    CDK Cancer
    CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor with an IC50 of 2.3 nM.
  • HY-108527
    CD1530

    RAR/RXR Cancer
    CD1530 is a selective RARγ agonist with an Kd of 150 nM. CD1530 has been used in combination with bexarotene to inhibit oral carcinogenesis induced by the carcinogen 4-nitroquinoline 1-oxide in a mouse model of human oral-cavity and esophageal squamous-cell carcinoma.
  • HY-119272
    EF24

    ERK Caspase Cancer
    EF24 is a curcumin analogue with greater anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK.
  • HY-145844
    EGFR-IN-44

    EGFR Apoptosis Cancer
    EGFR-IN-44 (Compound 6a) is a potent, orally active EGFR tyrosine kinase inhibitor with an IC50 of 4.11 nM. EGFR-IN-44 induces cell apoptosis and shows an oral bioavailability value of 33.57%. EGFR-IN-44 can be studied for non-small-cell lung cancers.
  • HY-12904
    TCA1

    Bacterial Infection
    TCA1 is a small molecule with activity against drug-susceptible and -resistant Mycobacterium tuberculosis (Mtb). TCA1 inhibits enzymes involved in cell wall and molybdenum cofactor biosynthesis, such as DprE1 and MoeW.
  • HY-115772
    4′-Bromoflavone

    Others Cancer
    4′-Bromoflavone, a cancer chemopreventive agent, is a potent phase II detoxification enzymes inducer.
  • HY-N0565B
    Doxycycline (hyclate)

    Doxycycline hydrochloride hemiethanolate hemihydrate; WC2031