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Results for "

oral

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2864

Inhibitors & Agonists

1

Screening Libraries

3

Dye Reagents

14

Peptides

133

Natural
Products

113

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-77591
    Cysteamine hydrochloride

    β-Mercaptoethylamine Hydrochloride; 2-Aminoethanethiol Hydrochloride; 2-Mercaptoethylamine Hydrochloride; Thioethanolamine Hydrochloride

    Autophagy Reactive Oxygen Species Apoptosis Endogenous Metabolite Metabolic Disease Cancer
    Cysteamine hydrochloride (β-Mercaptoethylamine Hydrochloride) is an orally active agent for the treatment of nephropathic cystinosis and an antioxidant.
  • HY-77591A
    Cysteamine

    β-Mercaptoethylamine; 2-Aminoethanethiol; 2-Mercaptoethylamine

    Autophagy Reactive Oxygen Species Apoptosis Endogenous Metabolite Cancer Metabolic Disease
    Cysteamine (β-Mercaptoethylamine) 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-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-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-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-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-16735
    Avoralstat

    BCX4161

    Others Others
    Avoralstat (BCX4161), a potent and orally active plasma kallikrein (PKK) inhibitor, is used for hereditary angioedema research.
  • 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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-123623
    Tinlarebant

    LBS-008; BPN-14967

    Others Others
    Tinlarebant (LBS-008) is an orally active non-retinoid RBP4 (retinol-binding protein 4) antagonist. Tinlarebant can be used for the research of the Stargardt disease.
  • 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-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-137432
    Avotaciclib

    BEY1107

    CDK Cancer
    Avotaciclib (BEY1107) is an orally active cyclin dependent kinase 1 (CDK1) inhibitor. Avotaciclib can be used for the research of cancer.
  • 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-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-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-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-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-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-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-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-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-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-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-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-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-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-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 P4503A expression. Pregnenolone 16α-carbonitrile exhibits increased resistance to subsequent stressful insults.
  • 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-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-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-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-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-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-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-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-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-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-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-109150
    Mesdopetam

    IRL790

    Dopamine Receptor Neurological Disease
    Mesdopetam (IRL790) is an orally active and low toxicity dopamine D3 receptor antagonist. Mesdopetam can be used for the research of Parkinson's disease (PD).
  • 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-132295
    ZN-c3

    Wee1 Cancer
    ZN-c3 is an orally active, highly potent and selective Wee1 inhibitor (IC50=3.9 nM). ZN-c3 can be used for the research of cancer.
  • 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-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-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-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-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-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-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-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-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-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-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-141411A
    (S)-MRI-1867

    Cannabinoid Receptor NO Synthase Metabolic Disease
    (S)-MRI-1867 is a peripherally restricted, orally bioavailable dual cannabinoid CB1 receptor and inducible NOS (iNOS) antagonist. (S)-MRI-1867 ameliorates obesity-induced chronic kidney disease (CKD).
  • 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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-138684
    MRTX9768

    Histone Methyltransferase Cancer
    MRTX9768 is a potent, orally active PRMT5 inhibitor. MRTX9768 is a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors.
  • 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-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-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-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-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-126290
    Ropsacitinib

    PF-06826647

    JAK Inflammation/Immunology
    PF-06826647 is an orally active and selective TYK2 inhibitor (IC50=17 nM), which binds to TYK2 catalytically active JH1 domain. PF-06826647 displays selectivity for TYK2 over JAK1 (IC50=383 nM) and JAK2 (74 nM). PF-06826647 can be used for the research of psoriasis, ulcerative colitis, and hidradenitis suppurativa.
  • 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-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-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-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-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-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-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-139142
    Simufilam

    PTI-125

    Others Neurological Disease
    Simufilam (PTI-125) is a low toxicity, orally active filamin A (FLNA) activator. Simufilam preferentially binds altered FLNA and restores its native conformation, restores receptor and synaptic activities, reduces its a7nAChR/TLR4 associations and downstream pathologies. Simufilam can be used for the research of Alzheimer's disease.
  • HY-139142A
    Simufilam dihydrochloride

    PTI-125 dihydrochloride

    Others Neurological Disease
    Simufilam (PTI-125) dihydrochloride is a low toxicity, orally active filamin A (FLNA) activator. Simufilam dihydrochloride preferentially binds altered FLNA and restores its native conformation, restores receptor and synaptic activities, reduces its a7nAChR/TLR4 associations and downstream pathologies. Simufilam dihydrochloride can be used for the research of Alzheimer's disease.
  • 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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-10274
    Dabigatran etexilate

    BIBR 1048

    Others Cardiovascular Disease
    Dabigatran etexilate (BIBR 1048) is an orally active prodrug of Dabigatran. Dabigatran etexilate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation.
  • 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-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-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-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-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-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-141521
    NX-13

    NOD-like Receptor (NLR) Inflammation/Immunology
    NX-13 is a first-in-class, orally active and gut-restricted agent that selectively targets and activates the NLRX1 pathway to induce immunometabolic changes. NX-13 results in lower inflammation and responses in inflammatory bowel disease. NX-13 can be used for the research of crohn's disease and ulcerative colitis.
  • HY-130120
    HWL-088

    GPR40 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-109127
    Berotralstat

    Others 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-10274A
    Dabigatran etexilate mesylate

    BIBR 1048MS; Dabigatran etexilate methanesulfonate

    Others Cardiovascular Disease
    Dabigatran etexilate mesylate (BIBR 1048MS) is an orally active prodrug of Dabigatran. Dabigatran etexilate mesylate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation.
  • 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-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-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-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-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-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-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-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-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-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-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-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-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-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-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 range 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-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-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-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-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-124631
    NLX-204

    5-HT Receptor Neurological Disease
    NLX-204 is an orally active, potent, highly affinity and selective 5-HT1A receptor-biased agonist (pKi=10.19). NLX-204 shows relatively higher affinity for α1 and D2 receptors than for other off-targets. NLX-204 can be used for the research of antidepressant.
  • 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-124631A
    NLX-204 hydrochloride

    5-HT Receptor Neurological Disease
    NLX-204 (hydrochloride) is an orally active, potent, highly affinity and selective 5-HT1A receptor-biased agonist (pKi=10.19). NLX-204 (hydrochloride) shows relatively higher affinity for α1 and D2 receptors than for other off-targets. NLX-204 (hydrochloride) can be used for the research of antidepressant.
  • 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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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 suppresses glucose metabolism and may yield favorable therapeutic indices suffering with advanced solid cancers.
  • 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-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-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-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-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-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-111784
    Inobrodib

    CCS1477

    Epigenetic Reader Domain Cancer
    Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain inhibitor. 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-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-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-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-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-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-13001
    Quizartinib

    AC220

    FLT3 Ligand 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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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 induces apoptosis. Y-27632 dihydrochloride primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation.
  • 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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-137141
    16-Keto Aspergillimide

    SB202327

    Parasite Infection
    16-Keto Aspergillimide (SB202327) is an anthelmintic agent isolated from Aspergillus strain IMI 337664.
  • HY-123033A
    Nicotinamide riboside chloride

    Sirtuin 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 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-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-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-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-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-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-101291
    Iberdomide

    CC-220

    Ligand 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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-B1045
    Chlorazanil hydrochloride

    Others Metabolic Disease
    Chlorazanil hydrochloride is a orally effective diuretic agent.
  • 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-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-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-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-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-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-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-16950
    4-Hydroxytamoxifen

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

    Estrogen Receptor/ERR Cancer
    4-Hydroxytamoxifen is an orally active, selective estrogen receptor modulator (SERM).
  • 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-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-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-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-110095
    (±)-CPSI-1306

    Others Metabolic Disease Inflammation/Immunology
    (±)-CPSI-1306 is an orally available antagonist of macrophage migration inhibitory factor (MIF).
  • 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-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-11077
    SR 146131

    Cholecystokinin Receptor Metabolic Disease Endocrinology
    SR 146131 is a potent, orally available, and selective nonpeptide (cholecystokinin 1) receptor agonist.
  • 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-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-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-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-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-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-100408
    GNF-6231

    Porcupine Cancer
    GNF-6231 is a potent, selective, and orally bioavailable Porcupine inhibitor that blocks Wnt signaling.
  • 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-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-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-10480
    Fasiglifam

    TAK-875

    GPR40 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-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-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-10014
    R547

    CDK GSK-3 Apoptosis Cancer
    R547 is a potent, selective and oral orally bioavailable ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively.
  • HY-N0565B
    Doxycycline (hyclate)

    Doxycycline hydrochloride hemiethanolate hemihydrate; WC2031

    Antibiotic MMP Bacterial Infection
    Doxycycline (hyclate) (Doxycycline hydrochloride hemiethanolate hemihydrate), an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor.
  • HY-102020
    RG3039

    PF-06687859

    Others Neurological Disease
    RG3039 (PF-06687859) is an orally bioavailable and brain-penetrant DcpS inhibitor with an IC50 of 0.069 nM.
  • HY-100388
    SHP099

    Phosphatase Cancer
    SHP099 is a potent, selective, orally available SHP2 inhibitor with an IC50 of 70 nM.
  • HY-101611
    MSC2530818

    CDK Cancer
    MSC2530818 is a potent, selective and orally available CDK8 inhibitor with an IC50 of 2.6 nM for CDK8.
  • HY-14832
    Ataluren

    PTC124

    CFTR Autophagy Metabolic Disease
    Ataluren (PTC124) is an orally available CFTR-G542X nonsense allele inhibitor.
  • HY-70037
    Cinacalcet

    AMG 073

    CaSR Cardiovascular Disease
    Cinacalcet (AMG 073) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
  • HY-100318
    NGD-4715

    MCHR1 (GPR24) Metabolic Disease Endocrinology
    NGD-4715 is a selective and orally active melanin-concentrating hormone receptor 1 (MCHR1) antagonist .
  • HY-U00148
    KY-556

    N556

    Others Inflammation/Immunology
    KY-556 is a promising and orally-active pro-drug of disodium cromoglycate (DSCG) against allergic diseases.
  • HY-107980
    DS28120313

    Others Inflammation/Immunology
    DS28120313 (compound 32) is an orally hepcidin production inhibitor with an IC50 of 0.093 μM.
  • HY-13059B
    SDZ 220-581 hydrochloride

    iGluR Neurological Disease
    SDZ 220-581 hydrochloride is an orally active, potent, competitive NMDA receptor antagonist with pKi value of 7.7.
  • HY-15526
    PSI-697

    P-Selectin Inhibitor

    Others Cancer
    PSI-697 is an oral P-selectin inhibitor with an IC50 of 125 μM.
  • HY-13059
    SDZ 220-581

    iGluR Neurological Disease
    SDZ 220-581 is an orally active, potent, competitive NMDA receptor antagonist with pKi value of 7.7.
  • HY-14870
    Selexipag

    NS-304; ACT-293987

    Prostaglandin Receptor Cardiovascular Disease Endocrinology
    Selexipag (NS-304) is an orally available and potent agonist for the Prostacyclin (PGI2) receptor (IP receptor).
  • HY-15599
    SSR128129E

    SSR

    FGFR Cancer
    SSR128129E is an orally available and allosteric FGFR inhibitor with an IC50 of 1.9 μM for FGFR1.
  • HY-13055
    Telotristat etiprate

    LX1606 Hippurate

    Tryptophan Hydroxylase Neurological Disease Cancer
    Telotristat etiprate (LX1606 Hippurate) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.
  • HY-18966
    PF-04418948

    Prostaglandin Receptor Cancer Endocrinology
    PF-04418948 is an orally active, potent and selective prostaglandin EP2 receptor antagonist with an IC50 of 16 nM.
  • HY-15411
    MK-0557

    Neuropeptide Y Receptor Metabolic Disease Endocrinology
    MK-0557 is a highly selective, orally available neuropeptide Y5 receptor antagonist with a Ki of 1.6 nM.
  • HY-A0285
    Norethisterone enanthate

    Norigest

    Progesterone Receptor Endocrinology
    Norethisterone enanthate is a long-acting parenteral progestogen. Norethisterone enanthate is orally active.
  • HY-12886
    Docebenone

    AA 861

    Lipoxygenase Ferroptosis Inflammation/Immunology
    Docebenone (AA 861) is a potent, selective and orally active 5-LO (5-lipoxygenase) inhibitor.
  • HY-15291
    MBX-2982

    GPR119 Metabolic Disease
    MBX-2982 is a selective, orally-available G protein-coupled receptor 119 (GPR119) agonist.
  • HY-14174
    MRK-560

    γ-secretase Neurological Disease
    MRK-560 is a potent, orally bioavailable and brain-penetrant γ-secretase inhibitor.
  • HY-A0128A
    Buclizine dihydrochloride

    Histamine Receptor Cancer Inflammation/Immunology
    Buclizine dihydrochloride is an orally active antihistamine antiallergic compound. Buclizine dihydrochloride is a potent teratogen in the rat.
  • HY-100347A
    SRI-011381 hydrochloride

    TGF-beta/Smad Neurological Disease
    SRI-011381 hydrochloride is an oral bioavailabile TGF-beta signaling agonist, exhibits neuroprotective effect.
  • HY-B0967
    Phthalylsulfacetamide

    Bacterial Infection
    Phthalylsulfacetamide is a sulfa drug, after oral administration, slowly decompose in the intestine,and release sulfacetamide ,generating antibacterial effect.
  • HY-U00084
    SUN 1334H

    Histamine Receptor Inflammation/Immunology Endocrinology
    SUN 1334H is a potent, orally active, highly selective H1 receptor antagonist, with Ki of 9.7 nM.
  • HY-19274
    ZD-1611

    Endothelin Receptor Cardiovascular Disease Endocrinology
    ZD-1611 is a potent, orally active, selective ETA receptor antagonist, used for the research of ischemic stroke.
  • HY-10064
    Ticagrelor

    AZD6140; AR-C 126532XX

    P2Y Receptor Cardiovascular Disease Cancer
    Ticagrelor (AZD6140) is a reversible oral P2Y12 receptor antagonist for the treatment of platelet aggregation.
  • HY-114397
    SHP394

    Phosphatase Cancer
    SHP394 is an orally active, selective and allosteric inhibitor of SHP2, with an IC50 of 23 nM.
  • HY-14751
    Rolapitant

    SCH619734

    Neurokinin Receptor Cancer Endocrinology
    Rolapitant (SCH619734) is a potent, selective and orally active neurokinin NK1 receptor antagonist with a Ki of 0.66 nM.
  • HY-125879
    DS08210767

    Thyroid Hormone Receptor Metabolic Disease Endocrinology
    DS08210767 is a highly potent, orally bioavailable PTHR1 antagonist with IC50 of 90 nM.
  • HY-100388A
    SHP099 hydrochloride

    Phosphatase Cancer
    SHP099 hydrochloride is a potent, selective and orally available SHP2 inhibitor with an IC50 of 70 nM.
  • HY-111493
    LRRK2 inhibitor 1

    LRRK2 Neurological Disease
    LRRK2 inhibitor 1 is a potent, selective and oral LRRK2 inhibitor with an pIC50 of 6.8.
  • HY-103407A
    PD 168568 dihydrochloride

    Dopamine Receptor Neurological Disease
    PD 168568 dihydrochloride is an orally active and selective D4 dopamine receptor antagonist, with a Ki of 8.8 nM.
  • HY-102053
    Apimostinel

    NRX-1074; AGN-241660

    iGluR Neurological Disease
    Apimostinel (NRX-1074; AGN-241660) is an orally active NMDA receptor partial agonist.
  • HY-B0084
    Dienogest

    STS 557

    Progesterone Receptor Autophagy Apoptosis Endocrinology Cancer
    Dienogest(STS-557) is a specific progesterone receptor agonist with potent oral endometrial activity and is used in the treatment of endometriosis.
  • HY-U00359
    LTD4 antagonist 1

    Leukotriene Receptor Inflammation/Immunology
    LTD4 antagonist 1 is a potent, orally active antagonist of leukotriene D4 (LTD4) with a Ki of 0.57 nM.
  • HY-15343
    CEP-33779

    JAK Cancer
    CEP-33779 is a novel, selective, and orally bioavailable inhibitor of JAK2 with an IC50 of 1.8±0.6 nM.
  • HY-B1583
    (Z)-Capsaicin

    Zucapsaicin; Civamide; cis-Capsaicin

    TRP Channel HSV Neurological Disease
    (Z)-Capsaicin is the cis isomer of capsaicin, acts as an orally active TRPV1 agonist, and is used in the research of neuropathic pain.
  • HY-100304A
    KW-8232

    Prostaglandin Receptor SARS-CoV Metabolic Disease Endocrinology
    KW-8232, an orally active anti-osteoporotic agent, and can reduces the biosynthesis of PGE2.
  • HY-18698
    L-701324

    iGluR Neurological Disease
    L-701324 is an orally active and long acting anticonvulsant with high affinity and selectivity for the glycine site on the NMDA receptor.
  • HY-13986
    Merimepodib

    VX-497; MMPD

    HBV HCV Infection
    Merimepodib (VX-497) is a noncompetitive and oral inhibitor of inosine monophosphate dehydrogenase (IMPDH) with broad spectrum antiviral activities.
  • HY-B1080
    Tilorone dihydrochloride

    HIF/HIF Prolyl-Hydroxylase Influenza Virus Infection Cancer
    Tilorone dihydrochloride is the first recognized synthetic, small molecular weight compound that is an orally active interferon inducer, used as an antiviral drug.
  • HY-101790
    ZM223

    NEDD8-activating Enzyme Cancer
    ZM223 is a potent non-covalent NEDD8 activating enzyme (NAE) inhibitor, orally active.
  • HY-135399
    Tauro-Obeticholic acid

    FXR Inflammation/Immunology
    Tauro-Obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist.
  • HY-13059A
    SDZ 220-581 Ammonium salt

    iGluR Neurological Disease
    SDZ 220-581 Ammonium salt is an orally active, potent, competitive NMDA receptor antagonist with pKi value of 7.7.
  • HY-119517
    Seclazone

    Others Inflammation/Immunology
    Seclazone, a heterocyclic compound, possesses anti-inflammatory, analgesic, antipyretic and diuretic properties. Seclazone is orally active.
  • HY-70037A
    Cinacalcet hydrochloride

    AMG-073 hydrochloride

    CaSR Cardiovascular Disease
    Cinacalcet hydrochloride (AMG-073 hydrochloride) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
  • HY-104048
    QC6352

    Histone Demethylase Cancer
    QC6352 is an orally available, selective and potent KDM4C inhibitor with an IC50 of 35 nM.
  • HY-18012
    Spebrutinib

    AVL-292; CC-292

    Btk Cancer
    Spebrutinib (AVL-292; CC-292) is a covalent, orally active, and highly selective with an IC50 of 0.5 nM.
  • HY-109046
    Tulrampator

    CX-1632

    iGluR Neurological Disease
    Tulrampator (CX-1632) is an orally bioavailable positive AMPAR (allosteric modulator of AMPA receptor). Antidepressant.
  • HY-101474
    (±)-Zanubrutinib

    (±)-BGB-3111

    Btk Cancer
    (±)-Zanubrutinib ((±)-BGB-3111) is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.
  • HY-15599A
    SSR128129E free acid

    SSR free acid

    FGFR Cancer
    SSR128129E free acid is an orally available and allosteric FGFR inhibitor with an IC50 of 1.9 μM for FGFR1.
  • HY-105018
    Epelsiban

    GSK 557296

    Oxytocin Receptor Endocrinology
    Epelsiban (GSK 557296) is a potent, selective and orally bioavailable oxytocin receptor antagonist, with a pKi of 9.9 for human oxytocin receptor.
  • HY-108339
    PF-06471553

    Acyltransferase Metabolic Disease
    PF-06471553 is a potent, selective and orally available monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC50 of 92 nM.
  • HY-N0864
    Macranthoidin B

    Macranthoiside I

    Others Cancer
    Macranthoidin B is a major bioactive saponin in rat plasma after oral administration of extraction of saponins from Flos Lonicerae.
  • HY-100148
    ICI 211965

    ZM-211965

    Lipoxygenase Inflammation/Immunology
    ICI 211965 (ZM-211965) is a selective and orally potent 5-Lipoxygenase (5-LPO) inhibitor.
  • HY-12428
    A-1165442

    TRP Channel Neurological Disease
    A-1165442 is a potent, competitive and orally available TRPV1 antagonist with an IC50 of 9 nM for human TRPV1.
  • HY-15592
    Cabotegravir

    GSK-1265744; S/GSK1265744

    HIV HIV Integrase Infection
    Cabotegravir is a potent HIV integrase inhibitor as an oral lead-in tablet and long-acting injectable for the treatment and prevention of HIV infection.
  • HY-121235
    Clonixin

    SCH-10304

    Others Inflammation/Immunology
    Clonixin (SCH-10304) is an orally active analgesic and a non-steroidal anti-inflammatory agent in rodents.
  • HY-15659
    Wnt-C59

    C59

    Porcupine Wnt Cancer
    Wnt-C59 (C59) is a highly potent and oral porcupine (PORCN) inhibitor with an IC50 of 74 pM.
  • HY-100269
    Chymase-IN-1

    Others Inflammation/Immunology
    Chymase-IN-1 is a potent, selective, orally active, nonpeptide inhibitor of human mast cell chymase with an IC50 of 29 nM.
  • HY-101803
    CP671305

    Phosphodiesterase (PDE) Others
    CP671305 is a potent, orally active, selective inhibitor of phosphodiesterase-4-D, and possesses high activities.
  • HY-19191
    L-159282

    MK 996

    Angiotensin Receptor Cardiovascular Disease Endocrinology
    L-159282 is a highly potent, orally active, nonpeptide angiotensin II receptor antagonist, with anti-hypertensive activity.
  • HY-101726
    DuP 105

    Bacterial Infection
    DuP 105 is an orally active oxazolidinone, a new class of synthetic antimicrobial agent with activity against gram-positive bacteria.
  • HY-14938
    Tipelukast

    KCA 757; MN 001

    Leukotriene Receptor Inflammation/Immunology
    Tipelukast (KCA 757) is a sulfidopeptide leukotriene receptor antagonist, an orally bioavailable anti-inflammatory agent and used for the treatment of asthma.
  • HY-18954
    NMS-P118

    PARP Cancer
    NMS-P118 is a potent, orally available, and highly selective PARP-1 Inhibitor for cancer therapy.
  • HY-100422
    KDM5-IN-1

    Histone Demethylase Cancer
    KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.
  • HY-112148
    AKT-IN-2

    Akt Cancer
    AKT-IN-2 is a potent, selective and orally bioavailable AKT inhibitor with an IC50 of 5 nM for AKT1.
  • HY-70073
    Zaurategrast

    CT7758

    Integrin Inflammation/Immunology
    Zaurategrast (CT7758) is a potent and oral-effective α4-integrin inhibitor.
  • HY-134886
    PD-1-IN-24

    PD-1/PD-L1 Cancer
    PD-1-IN-24 (compound 1) is an orally active PD-1 inhibitor.
  • HY-109059
    Fulacimstat

    BAY1142524

    Others Cardiovascular Disease
    Fulacimstat is an orally available chymase inhibitor, with IC50s of 4, 3 nM for human and hamster chymase enzyme, respectively.
  • HY-76938
    Actarit

    4-Acetylaminophenylacetic acid; MS-932

    Others Inflammation/Immunology
    Actarit, an orally active antirheumatic compound, has the potential to treat type II collagen-induced arthritis.
  • HY-17629
    Dapansutrile

    NOD-like Receptor (NLR) Inflammation/Immunology
    Dapansutrile is a potent, selective and orally active inhibitor of NLRP3 inflammasome. Anti-inflammatory, analgesic activity.
  • HY-139464
    Q134R

    Others Neurological Disease
    Q134R, a neuroprotective hydroxyquinoline derivative that suppresses nuclear factor of activated T cell (NFAT) signaling. Q134R can across blood-brain barrier. Q134R has the potential for Alzheimer's disease (AD) and aging-related disorders research.
  • HY-N4019
    Maohuoside A

    Others Metabolic Disease
    Maohuoside A, a single compound isolated from the E. koreanum that potently promotes osteogenesis. Maohuoside A enhances the osteogenesis of bone marrow-derived mesenchymal stem cells via bone morphogenetic protein (BMP) and MAPK signaling pathways.
  • HY-120874
    PF-06372865

    GABA Receptor Neurological Disease
    PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy.
  • HY-13038A
    Fostamatinib

    R788

    Syk FLT3 Inflammation/Immunology Cancer
    Fostamatinib (R788) is the oral prodrug of the active compound R406. R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).
  • HY-111069
    Nifeviroc

    CCR HIV Infection Inflammation/Immunology
    Nifeviroc is an orally active CCR5 antagonist. Nifeviroc is used for the study of HIV type-1 infection.
  • HY-B0177
    Tinidazole

    Bacterial Infection
    Tinidazole, an orally available antibacterial agent, is a 5-nitroimidazole with selective activity against anaerobic bacteria and protozoa.
  • HY-111418
    EBI-2511

    Histone Methyltransferase Cancer
    EBI-2511 is a highly potent and orally active EZH2 inhibitor, with an IC50 of 6 nM in Pfeffiera cell lines, respectively.
  • HY-15009
    Fuscoside

    OPC-21268

    Vasopressin Receptor Cardiovascular Disease Endocrinology
    Fuscoside (OPC-21268) is an orally effective, nonpeptide, vasopressin V1 receptor antagonist with an IC50 of 0.4 μM.
  • HY-10109
    AS-605240

    PI3K Autophagy Cancer
    AS-605240 is a specific and orally active inhibitor of the PI3Kγ, with an IC50 of 8 nM, and a Ki of 7.8 nM.
  • HY-100946
    CEP-40783

    RXDX-106

    TAM Receptor c-Met/HGFR Cancer
    CEP-40783 is a potent, selective and orally available inhibitor of AXL and c-Met with IC50 values of 7 nM and 12 nM, respectively.
  • HY-137181
    9-Carboxymethoxymethylguanine

    HSV Infection
    9-Carboxymethoxymethylguanine is the main metabolite of Aciclovir. Acyclovir (Aciclovir) is a guanosine analogue and an orally active antiviral agent.
  • HY-100754
    Ritlecitinib

    PF-06651600

    JAK Inflammation/Immunology
    Ritlecitinib (PF-06651600) is an orally active and selective JAK3 inhibitor with an IC50 of 33.1 nM.
  • HY-104059
    AMG2850

    TRP Channel Inflammation/Immunology
    AMG2850 is a potent, orally bioavailable and selective transient receptor potential melastatin 8 (TRPM8) antagonist.
  • HY-132167
    AZD5305

    PARP Cancer
    AZD5305 is a potent, selective and oral active PARP inhibitor. AZD5305 is potent and efficacious in animal xenografts and PDX models.
  • HY-114307
    Ly93

    Others Inflammation/Immunology
    Ly93 is a selective and orally active sphingomyelin synthase 2 (SMS2) inhibitor, with an IC50 of 91 nM.
  • HY-N2549
    (±)-Abscisic acid

    (±)-ABA

    Others Metabolic Disease
    (±)-Abscisic acid is an orally active plant hormone that is present also in animals. (±)-Abscisic acid (ABA) contributes to the regulation of glycemia in mammals.
  • HY-17602
    Amcasertib

    BBI503

    Others Cancer
    Amcasertib is an orally administered investigational agent designed to inhibit cancer stem cell pathways, including Nanog, by targeting stemness kinases.
  • HY-16079
    AZD3514

    Androgen Receptor Cancer
    AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.
  • HY-B0063
    Gimatecan

    ST1481

    Topoisomerase Cancer
    Gimatecan (ST1481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity.
  • HY-16162A
    D-3263 hydrochloride

    TRP Channel Cancer
    D-3263 hydrochloride is an enteric-coated, orally bioavailable (transient receptor potential melastatin member 8) TRPM8 agonist.
  • HY-109004
    Enzaplatovir

    BTA-C585

    RSV Infection
    Enzaplatovir (BTA-C585) is an orally bioavailable fusion inhibitor for respiratory syncytial virus (RSV) infection.
  • HY-12075
    LY2109761

    TGF-β Receptor Autophagy Cancer
    LY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with Kis of 38 nM and 300 nM, respectively.
  • HY-109096
    Nidufexor

    LMB763

    FXR Autophagy Inflammation/Immunology
    Nidufexor (LMB763) is an orally-available farnesoid X receptor (FXR) agonist for the research of nonalcoholic steatohepatitis (NASH).
  • HY-111500A
    NMDAR antagonist 1

    iGluR Neurological Disease
    NMDAR antagonist 1 is a potent and orally bioavailable NR2B-selective NMDAR antagonist.
  • HY-103713
    Seclidemstat

    SP-2577

    Histone Demethylase Cancer
    Seclidemstat (SP-2577) is a potent and orally bioavailable LSD1 inhibitor, with a mean IC50 of 127 nM.
  • HY-109082
    Cevidoplenib

    Syk Inflammation/Immunology
    Cevidoplenib is an orally available inhibitor of spleen tyrosine kinase (Syk), with potential anti-inflammatory and immunomodulating activities.
  • HY-103126
    DR4485 hydrochloride

    5-HT Receptor Neurological Disease
    DR4485 (hydrochloride) is an orally active and selective 5-HT7 antagonist (pKi=8.14).
  • HY-15601
    Vesatolimod

    GS-9620

    Toll-like Receptor (TLR) Apoptosis HBV HCV HIV Inflammation/Immunology
    Vesatolimod (GS-9620) is a potent, selective and orally active agonist of Toll-Like Receptor (TLR7) with an EC50 of 291 nM.
  • HY-15778
    AVE 0991

    Angiotensin Receptor Cardiovascular Disease Endocrinology
    AVE 0991 is a nonpeptide and orally active angiotensin-(1-7) receptor agonist with an IC50 of 21 nM.
  • HY-101773
    c-Met-IN-2

    c-Met/HGFR Cancer
    c-Met-IN-2 is a potent, selective and orally available c-Met inhibitor, with an IC50 of 0.6 nM, with antitumor activity.
  • HY-117632
    ABX-1431

    MAGL Neurological Disease
    ABX-1431 is a highly potent, selective, and orally available, CNS-penetrant monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 14 nM.
  • HY-B0689
    Indinavir

    MK-639; L-735524

    HIV HIV Protease Inflammation/Immunology
    Indinavir(MK-639; L735524) is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability.
  • HY-13226
    Galunisertib

    LY2157299

    TGF-β Receptor Cancer
    Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.
  • HY-101580
    Paliroden

    SR 57667

    Others Neurological Disease
    Paliroden is an orally bioactive neurotrophic, non-peptidic compound that activates synthesis of endogenous neurotrophines, used for treatment of Alzheimer's Disease and Parkinson's.
  • HY-U00022
    RWJ 63556

    COX Lipoxygenase Inflammation/Immunology
    RWJ 63556 is an orally active COX-2 selective/5-lipoxygenase inhibitor, with anti-inflammatory activities.
  • HY-U00063
    Tiopinac

    RS 40974

    Others Inflammation/Immunology Neurological Disease
    Tiopinac (RS 40974), a dibenzthiepin, is an orally active and highly potent anti-inflammatory, analgesic and anti-pyretic agent.
  • HY-12353A
    Pimodivir

    VX-787

    Influenza Virus Infection
    Pimodivir (VX-787) is an orally bioavailable inhibitor of influenza A virus polymerases through interaction with the viral PB2 subunit.
  • HY-103020
    BAY-1816032

    Others Cancer
    BAY-1816032 is a potent and oral available BUB1 (budding uninhibited by benzimidazoles 1) kinase inhibitor with an IC50 of 7 nM.
  • HY-14419
    TCN238

    mGluR Neurological Disease
    TCN238 is an orally bioavailable mGlu4 receptor positive allosteric modulator (PAM) with an EC50 of 1 μM.
  • HY-121577
    Sonlicromanol

    KH176

    Reactive Oxygen Species Metabolic Disease
    Sonlicromanol (KH176) is an orally active reactive oxygen species (ROS) modulator for the study in mitochondrial disease.
  • HY-50911
    Turofexorate isopropyl

    FXR-450; XL335; WAY-362450

    FXR Autophagy Metabolic Disease Cancer
    Turofexorate isopropyl (FXR-450) is a potent, selective, and orally bioavailable FXR agonist with EC50 of 4 nM.
  • HY-17545
    LGK974

    WNT974

    Porcupine Cancer
    LGK974 (WNT974) is an orally bioavailable and specific Porcupine (PORCN) inhibitor with an IC50 of 0.1 nM.
  • HY-100239
    ICI 153110

    Phosphodiesterase (PDE) Cardiovascular Disease
    ICI 153110 is an orally active phosphodiesterase inhibitor with both vasodilating and inotropic properties which is designed for the treatment of congestive cardiac failure.
  • HY-40354
    Tofacitinib

    Tasocitinib; CP-690550

    JAK Apoptosis Inflammation/Immunology Cancer
    Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
  • HY-13038B
    Fostamatinib disodium hexahydrate

    R788 disodium hexahydrate

    Syk FLT3 Cancer Inflammation/Immunology
    Fostamatinib (R788) disodium hexahydrate is the oral prodrug of the active compound R406. R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).
  • HY-13038
    Fostamatinib Disodium

    R788(Disodium)

    Syk FLT3 Inflammation/Immunology Cancer
    Fostamatinib Disodium (R788 Disodium) is the oral prodrug of the active compound R406. R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).
  • HY-14249
    Bicalutamide

    Androgen Receptor Autophagy Cancer
    Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer.
  • HY-A0020S
    Eldecalcitol-d6

    VD/VDR Metabolic Disease
    Eldecalcitol-d6 is the deuterium labeled Eldecalcitol. Eldecalcitol is an orally active analogue of active vitamin D used in the treatment of osteoporosis.
  • HY-112633
    SMN-C3

    DNA/RNA Synthesis Others
    SMN-C3 is an orally active SMN2 splicing modulator and has the potential to treat spinal muscular atrophy (SMA).
  • HY-110328
    PKI-166 hydrochloride

    EGFR Cancer
    PKI-166 hydrochloride is a potent, selective and orally active EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM.
  • HY-N6675
    Gardenia yellow

    Sirtuin Neurological Disease Cancer
    Gardenia yellow is an active member of crocin, increases mRNA expression of SIRT3, and acts as an orally active antidepressant agent.
  • HY-17603
    Belizatinib

    TSR-011

    ALK Trk Receptor Cancer
    Belizatinib is an oral, dual, potent inhibitor of ALK and TRKA, TRKB, and TRKC, with IC50 of 0.7 nM for wild-type recombinant ALK kinase.
  • HY-16785A
    Veledimex racemate

    INXN-1001 racemate; RG-115932 racemate

    Interleukin Related Cytochrome P450 Cancer Inflammation/Immunology
    Veledimex racemate (INXN-1001 racemate) is the racemate of veledimex. Veledimex is an orally available, small-molecule activator ligand for the RheoSwitch Therapeutic System.
  • HY-109566
    AZD1390

    ATM/ATR Cancer Inflammation/Immunology
    AZD1390 is a potent, highly selective, orally bioavailable, brain-penetrant ATM inhibitor with an IC50 of 0.78 nM in cell.
  • HY-128576
    DS21360717

    Others Cancer
    DS21360717 is a potent and orally active FER tyrosine kinase inhibitor, with an IC50 of 0.49 nM. Anti-cancer activity.
  • HY-117155
    PKI-166

    EGFR Cancer
    PKI-166 is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM.
  • HY-109565
    ASTX660

    IAP Cancer
    ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
  • HY-15446
    Basimglurant

    RG7090; CTEP Derivative

    mGluR Neurological Disease
    Basimglurant (RG7090) is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM.
  • HY-B1050
    Gemifloxacin mesylate

    SB-265805S; LB-20304a

    Bacterial Infection
    Gemifloxacin mesylate is an oral broad-spectrum quinolone antibacterial agent, used in the treatment of acute bacterial exacerbation of chronic bronchitis, and mild-to-moderate pneumonia.
  • HY-111748
    RORγt Inverse agonist 2

    ROR Inflammation/Immunology
    RORγt Inverse agonist 2 is a selective, orally active RORγt inverse agonist with an EC50 of 119 nM.
  • HY-107363
    FT-1518

    mTOR Cancer
    FT-1518 is a new generation selective, potent and oral bioavailable mTORC1 and mTORC2 inhibitor, and exhibits antitumor activity.
  • HY-100304
    KW-8232 free base

    Prostaglandin Receptor SARS-CoV Metabolic Disease Endocrinology
    KW-8232 free base, an orally active anti-osteoporotic agent, and can reduces the biosynthesis of PGE2.
  • HY-10162S
    Olaparib D5

    AZD2281 D5; KU0059436 D5

    PARP Autophagy Mitophagy Cancer
    Olaparib D5 (AZD2281 D5) is a deuterium labeled Olaparib. Olaparib is a potent and oral PARP inhibitor.
  • HY-112167A
    GDC-0575 dihydrochloride

    ARRY-575 dihydrochloride; RG7741 dihydrochloride

    Checkpoint Kinase (Chk) Cancer
    GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) is an orally bioavailable CHK1 inhibitor, with an IC50 of 1.2 nM, and has antitumor activity.
  • HY-106873
    Nepinalone

    Others Others
    Nepinalone, an alchilaminate derivative of β-tetralone and an orally active cough suppressant, possesses a non-opioid antitussive activity.
  • HY-14272
    Ravuconazole

    BMS-207147; ER-30346

    Fungal Infection
    Ravuconazole (BMS-207147;ER-30346) is an orally available triazoleantifungle agent that potently inhibits a wide range of fungi.
  • HY-B0017
    Telbivudine

    Epavudine; L-Thymidine; NV 02B

    HBV Infection
    Telbivudine (Epavudine), an orally active thymidine nucleoside analog, is a potent antiviral inhibitor of hepatitis B virus (HBV) replication.
  • HY-41344
    Ganciclovir mono-O-acetate

    Others Infection
    Ganciclovir mono-O-acetate is a derivative of Ganciclovir. Ganciclovir, a nucleoside analogue, is an orally active antiviral agent with activity against CMV.
  • HY-111484
    GDC-0927

    SRN-927

    Estrogen Receptor/ERR Cancer
    GDC-0927 (SRN-927) is a potent, non-steroidal, orally bioavailable, selective estrogen receptor antagonist.
  • HY-107456
    E6130

    Others Inflammation/Immunology Endocrinology
    E6130 is an orally active and highly selective CX3CR1 modulator, that may be effective for treatment of inflammatory bowel disease.
  • HY-100493
    BP-1-102

    STAT Cancer
    BP-1-102 is an orally available, small-molecule inhibitor of transcription factor Stat3, with an IC50 of 6.8 μM.
  • HY-128977
    CD235

    Epigenetic Reader Domain Cancer
    CD235 is a structurally similar analogue of CD161. CD161 is a potent and orally bioavailable BET bromodomain inhibitor.
  • HY-101782
    HSK0935

    SGLT Metabolic Disease
    HSK0935 is a potent, highly selective and orally available SGLT2 inhibitor with an IC50 of 1.3 nM. Antihyperglycemic activities.
  • HY-112166
    Rilzabrutinib

    PRN1008

    Btk Cancer Metabolic Disease
    Rilzabrutinib (PRN1008) is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM.
  • HY-110255
    AZD 2066

    mGluR Neurological Disease
    AZD 2066 is a selective, orally active and brain-penetrant antagonist of mGluR5. AZD 2066 has antinociception effects.
  • HY-15200
    Agerafenib

    CEP-32496; RXDX-105

    Raf Cancer
    Agerafenib (CEP-32496; RXDX-105) is a highly potent and orally efficacious inhibitor of BRAF V600E with a Kd of 14 nM.
  • HY-112096
    eCF506

    Src Cancer
    eCF506 is a highly potent and orally bioavailable inhibitor of the non-receptor tyrosine kinase Src with an IC50 of less than 0.5 nM.
  • HY-116239
    Zenarestat

    Aldose Reductase Metabolic Disease Neurological Disease
    Zenarestat is a potent and orally active aldose reductase inhibitor. Zenarestat improves diabetic peripheral neuropathy in Zucker diabetic fatty rats.
  • HY-15232
    Tenofovir alafenamide

    GS-7340

    HIV Reverse Transcriptase Infection
    Tenofovir alafenamide (GS-7340) is an investigational oral prodrug of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
  • HY-13026S
    Idelalisib D5

    CAL-101 D5; GS-1101 D5

    PI3K Autophagy Cancer
    Idelalisib D5 is a deuterium labeled Idelalisib. Idelalisib is a highly selective and orally bioavailable p110δ inhibitor.
  • HY-100856
    PCO371

    Thyroid Hormone Receptor Endocrinology
    PCO371 is an orally active full agonist of parathyroid hormone receptor 1 (PTHR1), with no effect on PTH type 2 receptor.
  • HY-15232A
    Tenofovir alafenamide fumarate

    GS-7340 (fumarate)

    HIV Reverse Transcriptase Infection
    Tenofovir alafenamide fumarate (GS-7340 fumarate) is an investigational oral prodrug of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
  • HY-50295
    CI-1040

    PD 184352

    MEK Apoptosis Cancer
    CI-1040 (PD 184352) is an orally active, highly specific, small-molecule inhibitor of MEK with an IC50 of 17 nM for MEK1.
  • HY-B0729
    Polaprezinc

    Zinc L-carnosine

    Others Inflammation/Immunology
    Polaprezinc is an orally bioavailable chelate composed of zinc and L-carnosine, with potential gastroprotective, anti-oxidant, anti-ulcer and anti-inflammatory activities.
  • HY-N0661
    Alliin

    Others Inflammation/Immunology Cardiovascular Disease
    Alliin, an orally active sulfoxide compound derived from garlic, exhibits hypoglycemic, antioxidant and anti-inflammatory activities.
  • HY-101729
    Anti-Heart Failure Agent 1

    Others Cardiovascular Disease
    Anti-Heart Failure Agent 1 an orally available compound suitable for the treatment of heart failure without inducing nausea, vomiting and restlessness.
  • HY-13064
    Cobimetinib

    GDC-0973; XL518

    MEK Apoptosis Cancer
    Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK1 inhibitor with an IC50 of 4.2 nM for MEK1.
  • HY-12864
    Brilanestrant

    ARN-810; GDC-0810

    Estrogen Receptor/ERR Cancer
    Brilanestrant (ARN-810; GDC-0810) is an orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM.
  • HY-A0076
    Tebipenem

    LJC 11036

    Bacterial Antibiotic Infection
    Tebipenem is an orally available carbapenem antibiotic, shows broad-spectrum activity against Gram-positive and -negative bacteria, except for Pseudomonas aeruginosa.
  • HY-16727
    Presatovir

    GS-5806

    RSV Infection
    Presatovir (GS-5806) is an orally bioavailable RSV fusion inhibitor with a mean EC50 value of 0.43 nM.
  • HY-U00122
    Antiulcer Agent 1

    Others Inflammation/Immunology
    Antiulcer Agent 1 is a 2-(3,4-dimethoxyphenyl)ethylamine derivative for oral administration at an exploratory stage of new drug development.
  • HY-15243
    Capromorelin Tartrate

    CP 424391-18

    GHSR Neurological Disease Endocrinology
    Capromorelin Tartrate is an orally active, potent growth hormone secretagogue receptor (GHSR) agonist, with Ki of 7 nM for hGHS-R1a.
  • HY-15202
    Binimetinib

    MEK162; ARRY-162; ARRY-438162

    MEK Autophagy Cancer
    Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM.
  • HY-110255A
    AZD 2066 hydrate

    mGluR Neurological Disease
    AZD 2066 hydrate is a selective, orally active and brain-penetrant antagonist of mGluR5. AZD 2066 hydrate has antinociception effects.
  • HY-10888
    Istradefylline

    KW-6002

    Adenosine Receptor Neurological Disease
    Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.
  • HY-106873A
    Nepinalone hydrochloride

    Others Others
    Nepinalone hydrochloride, an alchilaminate derivative of β-tetralone and an orally active cough suppressant, possesses a non-opioid antitussive activity.
  • HY-107978
    RIPK-IN-4

    RIP kinase Inflammation/Immunology
    RIPK-IN-4 is a potent and selective RIPK2 inhibitor with excellent oral bioavailability, and has an IC50 of 3 nM.
  • HY-119824S
    Trofosfamide-d4

    Bacterial Cancer
    Trofosfamide-d4 is the deuterium labeled Trofosfamide. Trofosfamide is an orally bioavailable oxazaphosphorine derivative with antineoplastic activity.
  • HY-131060
    CN128 hydrochloride

    CN328

    Others Others
    CN128 hydrochloride (CN328) is an orally active and selective iron chelator. CN128 is used for the research of β-thalassemia.
  • HY-15837
    SAR-260301

    PI3K Cancer
    SAR-260301 is an orally available and selective PI3Kβ inhibitor with an IC50 of 23 nM.
  • HY-N7111
    Sultamicillin tosylate

    Bacterial Infection
    Sultamicillin (tosylate) is a potent and orally active beta-lactamase inhibitor, an antibiotic with antibacterial activity. Sultamicillin (tosylate) is the tosylate salt of the double ester of sulbactam plus ampicillin.
  • HY-16715
    Acumapimod

    p38 MAPK Autophagy Inflammation/Immunology
    Acumapimod (BCT197) is an orally active p38 MAP kinase inhibitor, with an IC50 of less than 1 μM for p38α.
  • HY-10804
    CCT 137690

    Aurora Kinase Apoptosis Cancer
    CCT 137690 is a potent and orally available aurora kinase inhibitor with IC50s of 15, 25, and 19 nM for aurora A, B and C, respectively.
  • HY-132234
    M-1211

    Epigenetic Reader Domain Cancer
    M‑1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression.
  • HY-114926
    KT185

    MAGL Neurological Disease
    KT185 is an orally-bioavailable, brain-penetrant and selective ABHD6 inhibitor, with an IC50 0.21 nM in Neuro2A cells.
  • HY-19427A
    AZD9056 hydrochloride

    P2X Receptor Inflammation/Immunology
    AZD9056 hydrochloride is a selective orally active inhibitor of P2X7 which plays a significant role in inflammation and pain-causing diseases.
  • HY-133794
    Dasatinib N-oxide

    Drug Metabolite Cancer
    Dasatinib N-oxide is a minor metabolite of Dasatinib. Dasatinib is a potent and orally active dual Src/Bcr-Abl inhibitor.
  • HY-B0378A
    Moexipril hydrochloride

    RS-10085

    Angiotensin-converting Enzyme (ACE) Apoptosis Cardiovascular Disease
    Moexipril hydrochloride is a potent orally active non-sulfhydryl angiotensin converting enzyme(ACE) inhibitor, which is used for the treatment of hypertension and congestive heart failure.
  • HY-110164
    AdipoRon hydrochloride

    Adiponectin Receptor Metabolic Disease
    AdipoRon hydrochloride is an orally active and specific AdipoR agonist, binding to AdipoR1 and AdipoR2, with Kds of 1.8 and 3.1 μM, respectively.
  • HY-109754
    PF 03709270

    ulopenem etzadroxil

    Bacterial Infection
    PF 03709270 is an orally available ester prodrug form of sulopenem, with broad-spectrum antibacterial activity against most gram-positive and gram-negative bacteria.
  • HY-112278
    NCT-506

    Aldehyde Dehydrogenase (ALDH) Cancer
    NCT-506 is an orally bioavailable aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors with an IC50 of 7 nM.
  • HY-119217
    AZ084

    CCR Inflammation/Immunology Endocrinology
    AZ084 is a potent, selective, allosteric and oral active CCR8 antagonist, with a Ki of 0.9 nM. Has potential to treat asthma.
  • HY-128604
    XY101

    ROR Cancer
    XY101 is a potent, selective, metabolically stable and orally available RORγ inverse agonist with an IC50 of 30 nM and a Kd of 380 nM.
  • HY-10268
    Betrixaban

    PRT054021

    Factor Xa Cardiovascular Disease
    Betrixaban (PRT054021) is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with IC50 of 1.5 nM.
  • HY-10212
    BIIB021

    CNF2024

    HSP Autophagy Cancer
    BIIB021 (CNF2024) is an orally active, fully synthetic inhibitor of HSP90 with a Ki and an EC50 of 1.7 nM and 38 nM, respectively.
  • HY-111802
    3,4'-Dihydroxyflavone

    3,4'-DHF

    Influenza Virus Infection
    3,4'-Dihydroxyflavone (3,4'-DHF) is an oral active flavonoid with antiviral activity against Influenza A virus.
  • HY-100209
    Sufugolix

    TAK-013

    Others Endocrinology
    Sufugolix (TAK-013) is a highly potent and orally available luteinizing hormone-releasing hormone (LHRH) receptor antagonist with an IC50 of 0.1 nM.
  • HY-16997A
    Itacitinib adipate

    JAK Cancer
    Itacitinib adipate is an orally bioavailable and selective JAK1 inhibitor which has been tested for efficacy and safety in a phase II trial in myelofibrosis.
  • HY-B1096
    Etamivan

    Ethamivan; N,N-Diethylvanillamide

    Others Neurological Disease
    Etamivan (Ethamivan), an orally active respiratory stimulant, is mainly used in the research of barbiturate overdose and chronic obstructive pulmonary disease.
  • HY-15653
    Filorexant

    MK-6096

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    Filorexant (MK-6096) is an orally bioavailable potent and selective reversible antagonist of OX1 and OX2 receptor(<3 nM in binding).
  • HY-U00049
    Mioflazine

    Others Neurological Disease Cardiovascular Disease
    Mioflazine is an orally active nucleoside transport inhibitor, has the potential for sleep disorders treatment. Mioflazine inhibits nucleoside uptake.
  • HY-108413
    Talazoparib tosylate

    BMN 673ts

    PARP Cancer
    Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available PARP1/2 inhibitor with an IC50 of 0.57 nM for PARP1.
  • HY-109105
    Tepilamide fumarate

    XP-23829

    Others Inflammation/Immunology
    Tepilamide fumarate (XP-23829) is an oral fumaric acid ester, acts as a prodrug of monomethyl fumarate, and is used in the research of moderate to severe chronic plaque psoriasis.
  • HY-16265
    JI-101

    Ephrin Receptor PDGFR VEGFR Cardiovascular Disease Cancer
    JI-101 is an orally available multi-kinase inhibitor of VEGFR2, PDGFRβ and EphB4 with potent anti-cancer activity.
  • HY-101565
    Tapotoclax

    AMG-176

    Bcl-2 Family Cancer
    Tapotoclax (AMG-176) is a potent, selective and orally active MCL-1 inhibitor, with a Ki of 0.13 nM.
  • HY-108881
    Troleandomycin

    Triacetyloleandomycin

    Cytochrome P450 Infection Inflammation/Immunology
    Troleandomycin (Triacetyloleandomycin), a macrolide acrolide antibiotic, is a selective CYP3A inhibitor. Troleandomycin is an oral corticosteroid for asthma study.
  • HY-109037
    Mavacamten

    MYK461; SAR439152

    Myosin Cardiovascular Disease
    Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
  • HY-107987
    CXCR7 modulator 1

    CXCR Endocrinology
    CXCR7 modulator 1 (compound 25) is a potent and orally bioavailable peptoid hybrid CXCR7 modulator, with a Ki of 9 nM.
  • HY-131281
    Ivabradine impurity 1

    Others Others
    Ivabradine impurity 1 is an Ivabradine impurity. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker.
  • HY-133813A
    Apovincaminic acid hydrochloride salt

    Drug Metabolite Neurological Disease
    Apovincaminic acid hydrochloride salt is an orally active and brain-penetrant main active metabolite of Vinpocetine (VP). Apovincaminic acid hydrochloride salt exerts a neuroprotective type of action.
  • HY-137434
    Cedirogant

    ABBV-157

    ROR Inflammation/Immunology
    Cedirogant (ABBV-157) is an orally active RORγt inverse agonist. Cedirogant can be used for psoriasis research.
  • HY-101833
    YM-264

    Others Inflammation/Immunology
    YM-264 is a selective, potent and orally active platelet-activating factor (PAF) antagonist with a pKi value of 8.85 for rabbit platelet membranes.
  • HY-12528
    DBPR108

    Dipeptidyl Peptidase Metabolic Disease
    DBPR108 is a potent, selective, and orally bioavailable dipeptide-derived inhibitor of DPP4 with IC50 of 15 nM; no inhibition on DDP8 and DPP9.
  • HY-109001
    Alicapistat

    ABT-957

    Proteasome Neurological Disease
    Alicapistat (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential use in the treatment of Alzheimer's disease (AD).
  • HY-17646
    Verdiperstat

    AZD3241

    Glutathione Peroxidase Neurological Disease
    Verdiperstat (AZD3241) is a selective, irreversible and orally active myeloperoxidase (MPO) inhibitor, with an IC50 of 630 nM, and can be used in the research of neurodegenerative brain disorders.
  • HY-109057
    Enarodustat

    JTZ-951

    HIF/HIF Prolyl-Hydroxylase Metabolic Disease
    Enarodustat is a potent and orally active factor prolyl hydroxylase inhibitor, with an EC50 of 0.22 μM. Enarodustat has the potential for renal anemia treatment.
  • HY-10268S
    Betrixaban D6

    Factor Xa Cardiovascular Disease
    Betrixaban D6 is a deuterium labeled Betrixaban. Betrixaban is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor.
  • HY-131282
    Ivabradine impurity 2

    Others Others
    Ivabradine impurity 2 is an Ivabradine impurity. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker.
  • HY-121567
    Metipranolol

    Adrenergic Receptor Cardiovascular Disease
    Metipranolol is a nonselective and orally active β-adrenergic receptor antagonist. Metipranolol can be used for hypertension and glaucoma research.
  • HY-101790A
    ZM223 hydrochloride

    NEDD8-activating Enzyme Cancer
    ZM223 hydrochloride is an orally active, potent non-covalent NEDD8 activating enzyme (NAE) inhibitor with excellent anticancer activity.
  • HY-138630
    AG-270

    Others Cancer
    AG-270 is an allosteric, noncompetitive, first-in-class, reversible and orally active MAT2A inhibitor, with an IC50 of 14 nM.
  • HY-14789
    (R)-Elagolix

    NBI-56418

    GnRH Receptor Cancer Endocrinology
    Elagolix is a highly potent, selective, orally-active, short-duration, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (KD = 54 pM).
  • HY-121467S
    Acotiamide D6

    AChE Metabolic Disease
    Acotiamide D6 is a deuterium labeled Acotiamide. Acotiamide is an orally active and first-in-class gastroprokinetic agent for the treatment of functional dyspepsia.
  • HY-139058
    23-epi-26-Deoxyactein

    27-Deoxyactein

    Others Cancer Metabolic Disease
    23-epi-26-Deoxyactein is a natural and orally active anti-obesity and anti-cancer compound.
  • HY-32721
    Neratinib

    HKI-272

    EGFR Cancer
    Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor with IC50s of 59 nM and 92 nM for HER2 and EGFR, respectively.
  • HY-112167
    GDC-0575

    ARRY-575; RG7741

    Checkpoint Kinase (Chk) Cancer
    GDC-0575 (ARRY-575, RG7741) is a highly-selective oral small-molecule Chk1 inhibitor with an IC50 of 1.2 nM.
  • HY-15848
    AdipoRon

    Adiponectin Receptor Metabolic Disease
    AdipoRon is an orally active adiponectin receptor (AdipoR) agonist, binding to AdipoR1 and AdipoR2 with Kds of 1.8 and 3.1 μM, respectively.
  • HY-15947
    Ravoxertinib

    GDC-0994

    ERK Cancer
    Ravoxertinib (GDC-0994) is an orally active ERK kinase inhibitor with an IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.
  • HY-N2909
    Aurantiamide

    Others Inflammation/Immunology
    Aurantiamide is an orally active constituent of Portulaca oleracea L and has various biological activities, including antioxidant, antiplatelet, anti-inflammatory, and antitumor activities.
  • HY-50909
    Perifosine

    KRX-0401; NSC 639966; D21266

    Akt Autophagy Apoptosis Cancer
    Perifosine is an oral Akt inhibitor which inhibits proliferation of different tumor cell lines with IC50s of 0.6-8.9 μM.
  • HY-12045
    HMN-214

    IVX-214

    Polo-like Kinase (PLK) Cancer
    HMN-214, an orally bioavailable prodrug of HMN-176, is an inhibitor of polo-like kinase-1 (plk1), with antitumor activity.
  • HY-112318
    GSK-2793660

    Cathepsin Inflammation/Immunology
    GSK-2793660 is an oral, irreversible inhibitor of Cathepsin C (CTSC). GSK-2793660 can be used for the research of bronchiectasis.
  • HY-14936
    Sofigatran

    MCC-977

    Thrombin Cardiovascular Disease
    Sofigatran (MCC-977) is an orally active factor IIa (thrombin) inhibitor, acts as an anticoagulant. Sofigatran is used for the research of cardiovascular disease.
  • HY-U00168
    KP136

    AL136

    Histamine Receptor Inflammation/Immunology Endocrinology
    KP136 (AL136) is an orally effective antiallergic agent. The IC50 is 76.1 μg/mL for histamine release and 63 ug/mL for degranulation.
  • HY-B1784
    Sulfisomidin

    Sulfaisodimidine

    Bacterial Antibiotic Infection
    Sulfisomidin (Sulfaisodimidine) is an orally active short-acting sulfonamide antibacterial. Sulfisomidin can be used for the research of lower urinary tract infections.
  • HY-B0196A
    Venlafaxine hydrochloride

    Wy 45030 hydrochloride

    Serotonin Transporter Neurological Disease
    Venlafaxine hydrochloride (Wy 45030 hydrochloride) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant.
  • HY-W000838
    1-Hydroxyanthraquinone

    DNA/RNA Synthesis Cancer
    1-Hydroxyanthraquinone, a naturally occurring compound with oral activity from some plants like Tabebuia avellanedae, exhibits carcinogenic effect.
  • HY-14719
    RO4987655

    CH4987655

    MEK Cancer
    RO4987655 is an orally active and highly selective MEK inhibitor with an IC50 of 5.2 nM for inhibition of MEK1/MEK2.
  • HY-A0110A
    Cefotiam hexetil hydrochloride

    CTM-HE hydrochloride; SCE-2174 hydrochloride

    Bacterial Antibiotic Infection
    Cefotiam hexetil hydrochloride (CTM-HE) is an oral third-generation cephalosporin, which is a prodrug of cefotiam, but has no anti-bacterial property. Cefotiam is an antibiotic.
  • HY-19778
    (R)-BPO-27

    CFTR Autophagy Inflammation/Immunology
    (R)-BPO-27, the R enantiomer of BPO-27, is a potent, orally active and ATP-competitive CFTR inhibitor with an IC50 of 4 nM.
  • HY-122078
    FR-190809

    Acyltransferase Metabolic Disease
    FR-190809 is a potent, nonadrenotoxic, orally efficacious acyl-CoA:cholesterol O-acyltransferase (ACAT) inhibitor, with an IC50 of 45 nM.
  • HY-13041
    LX-1031

    Tryptophan Hydroxylase Neurological Disease
    LX-1031 is a potent, orally available tryptophan 5-hydroxylase (TPH) inhibitor that reduces serotonin (5-HT) synthesis peripherally.
  • HY-18072
    GSK2606414

    PERK Autophagy Apoptosis Cancer
    GSK2606414 is a cell-permeable and orally available protein kinase R-like endoplasmic reticulum (ER) kinase (PERK) inhibitor with an IC50 of 0.4 nM.
  • HY-18030
    CEP-28122

    ALK Cancer
    CEP-28122 is a highly potent and selective orally active ALK inhibitor with IC50 of 1.9 ± 0.5 nM in an enzyme-based TRF assay.
  • HY-12366
    Ubrogepant

    MK-1602

    CGRP Receptor Neurological Disease Cardiovascular Disease
    Ubrogepant (MK-1602) is a novel oral calcitonin gene-related peptide receptor (CGRP) antagonist in development for acute treatment of migraine.
  • HY-B1267
    Sulfaguanidine

    Bacterial Antibiotic Infection
    Sulfaguanidine is an orally active antimicrobial agent/antibiotic of sulfonamide class. Sulfaguanidine can be used for the research of enteric infections such as bacillary dysentery.
  • HY-106392
    Lucerastat

    NB-DGJ; N-(n-Butyl)deoxygalactonojirimycin

    Others Metabolic Disease
    Lucerastat, the galactose form of Miglustat, is an orally-available inhibitor of glucosylceramide synthase (GCS). Lucerastat has the potential for Fabry disease study.
  • HY-15253
    Tiplaxtinin

    PAI-039; Tiplasinin

    PAI-1 Apoptosis Metabolic Disease Cancer
    Tiplaxtinin is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 μM.
  • HY-114177A
    (S)-PF-06873600

    Others Cancer
    (S)-PF-06873600 it the S enantiomer of PF-06873600. PF-06873600 is a selective and orally bioavailable inhibitor of cyclin-dependent kinase (CDK).
  • HY-B0196
    Venlafaxine

    Wy 45030

    Serotonin Transporter Neurological Disease
    Venlafaxine (Wy 45030) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant.
  • HY-131283
    8-Demethyl Ivabradine

    Drug Metabolite Endocrinology
    8-Demethyl Ivabradine is a metabolite of Ivabradine. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker.
  • HY-50855B
    Silmitasertib sodium salt

    CX-4945 sodium salt

    Casein Kinase Autophagy Cancer
    Silmitasertib sodium salt is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC50 values of 1 nM against CK2α and CK2α'.
  • HY-13432
    Nanatinostat

    CHR-3996

    HDAC Cancer
    Nanatinostat (CHR-3996) is a potent, class I selective and orally active histone deacetylase (HDAC) inhibitor with an IC50 of 8 nM.
  • HY-18658
    Siremadlin

    NVP-HDM201; HDM201

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    Siremadlin (NVP-HDM201) is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
  • HY-75054
    Abiraterone acetate

    CB7630

    Cytochrome P450 Cancer
    Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity. Abiraterone acetate is a prodrug form of Abiraterone (CB7598).
  • HY-101749
    WAY127093B racemate

    Phosphodiesterase (PDE) Inflammation/Immunology
    WAY127093B racemate is the racemate of WAY127093B. WAY127093B is an orally active phosphodiesterase IV inhibitor in guinea pigs and rats.
  • HY-19477
    SB-616234-A

    5-HT Receptor Neurological Disease
    SB-616234-A is a selective and orally bioavailable 5-HT1B receptor antagonist, with anxiolytic and antidepressant activity.
  • HY-19189
    Terbogrel

    BIBV 308SE

    Prostaglandin Receptor Cardiovascular Disease Endocrinology
    Terbogrel is an orally available thromboxane A2 receptor antagonist and a thromboxane A2 synthase inhibitor, with both IC50s of about 10 nM.
  • HY-N0856
    Alisol C 23-acetate

    23-O-Acetylalisol C; Alisol C monoacetate

    Others Cardiovascular Disease
    Alisol C 23-acetate, a natural product extracted from Alisma orientale, can significantly and strongly inhibit DTH response after oral administration.
  • HY-112065
    PF-06869206

    Sodium Channel Metabolic Disease
    PF-06869206 is an orally bioavailable selective inhibitor of the sodium-phosphate cotransporter NaPi2a (SLC34A1) with an IC50 of 380 nM.
  • HY-A0176
    Glisoxepide

    Potassium Channel Metabolic Disease Cardiovascular Disease
    Glisoxepide, a sulphonamide derivative, is an orally available nonselective K(ATP) channel blocker, with antihyperglycemic activity and cardiovascular regulation effect.
  • HY-13467
    AM-1638

    GPR40 Metabolic Disease
    AM-1638 is a potent and orally bioavailable GPR40/FFA1 full agonist with an EC50 of 0.16 μM.
  • HY-14603
    Clioquinol

    Iodochlorhydroxyquin

    Fungal Autophagy Mitophagy Antibiotic Infection Cancer
    Clioquinol (Iodochlorhydroxyquin) is a topical antifungal agent with anticancer activity. Clioquinol acts as an oral antimicrobial agent for the research of diarrhea and skin infections. Antibiotic.
  • HY-19903
    ASP-9521

    Others Cancer
    ASP-9521 is a potent, selective and orally available AKR1C3 inhibitor with an IC50 of 11 nM for human AKR1C3.
  • HY-15232B
    Tenofovir alafenamide hemifumarate

    GS-7340 (hemifumarate)

    HIV Reverse Transcriptase Infection
    Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) is an investigational oral prodrug of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
  • HY-18071A
    BI-9627 hydrochloride

    Sodium Channel Cardiovascular Disease
    BI-9627 hydrochloride is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 hydrochloride displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 hydrochloride shows low DDI (drug-drug interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury.
  • HY-18071
    BI-9627

    Sodium Channel Cardiovascular Disease
    BI-9627 is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 shows low DDI (drug-drug interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury.
  • HY-136658
    1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(4-(4-cyanophenoxy)phenyl)urea

    STAT Apoptosis Cancer
    STAT3-IN-7 is a Sorafenib analogue and potently inhibits the phosphorylation of STAT3. STAT3-IN-7 induces cell apoptosis through SHP-1 dependent STAT3 inactivation. STAT3-IN-7 does not inhibit kinase activity and has anticancer effects.
  • HY-N0923
    Corydaline

    (+)-Corydaline; Corydalin

    AChE Enterovirus Opioid Receptor Neurological Disease
    Corydaline ((+)-Corydaline), an isoquinoline alkaloid isolated from Corydalis yanhusuo, is an AChE inhibitor with an IC50 of 226 µM. Corydaline is a μ-opioid receptor (Ki of 1.23 µM) agonist and inhibits enterovirus 71 (EV71) replication (IC50 of 25.23 µM). Corydaline has anti-angiogenic, anti-allergic and gastric-emptying and antinociceptive activities.
  • HY-A0035
    Faropenem

    Antibiotic Infection
    Faropenem is a potent and orally active beta-lactam antibiotic. Faropenem demonstrates broad-spectrum in vitro antimicrobial activity against many gram-positive and -negative aerobes and anaerobes. Faropenem is resistant to hydrolysis by nearly all beta-lactamases, including extended-spectrum beta-lactamases and AmpC beta-lactamases. Faropenem is developed as an oral prodrug, faropenem medoxomil, for the research of respiratory tract infections.
  • HY-B0559
    Nabumetone

    BRL14777

    COX Inflammation/Immunology Cancer
    Nabumetone is an orally active non-acidic anti-inflammatory agent, acts as a potent and selective COX-2 inhibitor, and is the prodrug of the active metabolite 6MNA.
  • HY-N4109
    Decursinol

    Others Cancer Inflammation/Immunology
    Decursinol, isolated from the roots of Angelica gigas, possesses antinociceptive effect with orally bioavailability. Decursinol possesses anti-tumor and anti-metastasis activity.
  • HY-19822
    Elacestrant

    RAD1901

    Estrogen Receptor/ERR Cancer
    Elacestrant (RAD1901) is an orally available selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.
  • HY-100419
    BFH772

    VEGFR Cancer
    BFH772 is a potent oral VEGFR2 inhibitor, which is highly effective at targeting VEGFR2 kinase with an IC50 value of 3 nM.
  • HY-100720
    GSK2193874

    TRP Channel Cardiovascular Disease
    GSK2193874 is an orally active, potent, and selective TRPV4 antagonist with IC50s of 2 nM and 40 nM for rTRPV4 and hTRPV4.
  • HY-17460A
    Garenoxacin Mesylate hydrate

    BMS284756 Mesylate hydrate

    Bacterial Infection
    Garenoxacin Mesylate hydrate (BMS284756 Mesylate hydrate) is a novel oral des-fluoro(6) quinolone with potent antimicrobial activity, against common respiratory pathogens, including resistant strains.
  • HY-112202
    GSK3395879

    TRP Channel Cardiovascular Disease
    GSK3395879 is a selective and orally bioavailable transient receptor potential vanilloid-4 (TRPV4) antagonist with an IC50 of 1 nM for hTRPV4.
  • HY-14955
    Managlinat dialanetil

    MB06322; CS-917

    Phosphatase Metabolic Disease
    Managlinat dialanetil (MB06322) is an orally bioavailable inhibitor of fructose 1,6-bisphosphatase (FBPase) for the treatment of type 2 diabetes .
  • HY-12525
    LGD-6972

    Glucagon Receptor Metabolic Disease
    LGD-6972 is a selective and orally active glucagon receptor antagonist. LGD-6972 has the potential for type 2 diabetes research.
  • HY-120272
    SMAP-2

    DT-1154

    Phosphatase Cancer
    SMAP-2 (DT-1154) is an orally active protein phosphatase 2A (PP2A) activator, with anti-cancer activity.
  • HY-101437
    Ralfinamide

    FCE-26742A

    Sodium Channel Neurological Disease
    Ralfinamide (FCE-26742A) is an orally available Na + blocker derived from α-aminoamide, with function of suppressing pain.
  • HY-19803
    Naquotinib mesylate

    ASP8273 (mesylate)

    EGFR Cancer
    Naquotinib mesylate (ASP8273 mesylate) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
  • HY-114258
    LY3295668

    AK-01

    Aurora Kinase Cancer
    LY3295668 (AK-01) is a potent, orally active and highly specific Aurora-A kinase inhibitor, with Ki values of 0.8 nM and 1038 nM for AurA and AurB, respectively.
  • HY-112712
    Cyclophilin inhibitor 1

    HCV Infection
    Cyclophilin inhibitor 1 is a potent and orally bioavailable cyclophilin A inhibitor, with a Kd of 5 nM, shows effective anti-HCV activity, with an EC50 of 98 nM for HCV 2a.
  • HY-N4173
    8-Oxoepiberberine

    Others Metabolic Disease
    8-Oxoepiberberine is an alkaloid metabolite in the plasma after oral administration of Zuojin formula, a traditional chinese medicine used to treat gastrointestinal disease.
  • HY-19822A
    Elacestrant dihydrochloride

    RAD1901 dihydrochloride

    Estrogen Receptor/ERR Cancer
    Elacestrant dihydrochloride (RAD1901 dihydrochloride) is an orally available selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.
  • HY-B0304A
    Dapoxetine hydrochloride

    LY-210448 hydrochloride

    Serotonin Transporter Neurological Disease
    Dapoxetine (LY-210448) hydrochloride is an orally active and selective serotonin reuptake inhibitor (SSRI). Dapoxetine hydrochloride can be used for the research of premature ejaculation (PE).
  • HY-100032
    PD 117519

    CI947

    Adenosine Receptor Neurological Disease
    PD 117519 (CI947) is an A2A adenosine agonist which has shown oral antihypertensive activity in pharmacological animal models.
  • HY-50844
    Ibutamoren Mesylate

    MK-677; MK-0677

    GHSR Endocrinology
    Ibutamoren Mesylate (MK-677) is a potent, non-peptide Growth hormone secretagogue receptor (GHSR) agonist. Ibutamoren Mesylate is an orally active growth hormone (GH) secretagogue.
  • HY-15822
    MF-438

    Stearoyl-CoA Desaturase (SCD) Metabolic Disease
    MF-438 is a potent and orally bioavailable stearoyl-CoA desaturase 1 (SCD1) inhibitor with an EC50 of 2.3 nM for rSCD1.
  • HY-125465
    SLLN-15

    Autophagy Cancer
    SLLN-15 is an oral active, selective and potent enhancer of autophagy that activates cytostatic macroautophagy/autophagy in triple-negative breast cancer (TNBC).
  • HY-12163
    Entinostat

    MS-275; SNDX-275

    HDAC Autophagy Apoptosis Cancer
    Entinostat is an oral and selective class I HDAC inhibitor, with IC50s of 243 nM, 453 nM, and 248 nM for HDAC1, HDAC2, and HDAC3, respectively.
  • HY-14817
    Indeglitazar

    PPM 204

    PPAR Metabolic Disease
    Indeglitazar (PPM 204) is an orally available PPAR pan-agonist for all three PPARα, PPARδ and PPARγ.
  • HY-19214
    Elisartan

    HN 65021

    Angiotensin Receptor Cardiovascular Disease Endocrinology
    Elisartan is an orally active non-peptide pro-drug of angiotensin II AT1 receptor antagonist HN-12206, and shows anti-hypertension activities.
  • HY-14934
    Rosabulin

    STA 5312

    Microtubule/Tubulin Cancer
    Rosabulin (STA 5312) is a potent and orally active microtubule inhibitor that inhibits microtubule assembly. Rosabulin has broad-spectrum anti-tumor activity.
  • HY-135601
    Cinacalcet metabolite M4

    Drug Metabolite Cardiovascular Disease
    Cinacalcet metabolite M4 is a metabolite of Cinacalcet. Cinacalcet is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease.
  • HY-135500
    ACT-373898

    Others Endocrinology
    ACT-373898 is an inactive carboxylic acid metabolite of Macitentan. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist.
  • HY-B1442
    Acetylleucine

    N-Acetyl-DL-leucine

    Others Others
    Acetylleucine (N-Acetyl-DL-leucine), orally active compound, can be used for the research of acute vestibular vertigo, cerebellar ataxia and nystagmus.
  • HY-124557
    Mahanimbine

    Others Metabolic Disease Inflammation/Immunology
    Mahanimbine is an orally active alkaloid from curry leaves. Mahanimbine inhibits progression of high-fat diet (HFD)-induced metabolic complications in mice.
  • HY-17458
    Azilsartan medoxomil monopotassium

    Azilsartan kamedoxomil; TAK 491 monopotassium

    Angiotensin Receptor Cardiovascular Disease Endocrinology
    Azilsartan medoxomil monopotassium is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension.
  • HY-U00133
    HSR6071

    Others Inflammation/Immunology
    HSR6071, a pyrazinecarboxamide derivative, is an orally active and potent antiallergic agent. HSR6071 potently inhibits the experimental asthma in rat models.
  • HY-101869
    MK-0343

    MRK-409

    GABA Receptor Neurological Disease
    MK0343 (MRK-409) is an orally bioavailable GABAA receptor subtype-selective partial agonist. MK0343 is a non-sedating anxiolytic.
  • HY-130078
    Ferrous bisglycinate

    Others Metabolic Disease Inflammation/Immunology
    Ferrous bisglycinate is an orally active iron fortificants and therapeutic iron supplements. Ferrous bisglycinate can be used for the research of iron deficiency anemia.
  • HY-19729
    Naquotinib

    ASP8273

    EGFR Cancer
    Naquotinib (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
  • HY-13009
    PF-04620110

    Acyltransferase Metabolic Disease
    PF-04620110 is a potent, selective and orally bioavailable diglyceride acyltransferase-1 (DGAT-1) inhibitor with an IC50 of 19 nM.
  • HY-128379
    Labetalone hydrochloride

    Others Others
    Labetalone hydrochloride is an impurity of Labetalol. Labetalol is an orally active adrenoceptor blocking drug which is a competitive antagonist at both alpha- and beta-adrenoceptor sites.
  • HY-10633
    SB-705498

    TRP Channel Neurological Disease
    SB-705498 is a potent, selective and orally bioavailable transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with a pIC50 of 7.1.
  • HY-14503
    MDR-1339

    DWK-1339

    Amyloid-β Neurological Disease
    MDR-1339 (DWK-1339) is an orally active and blood-brain-barrier-permeable Aβ-aggregation inhibitor, used in the research of Alzheimer's disease.
  • HY-16511
    Upamostat

    WX-671

    Ser/Thr Protease PAI-1 Cancer
    Upamostat (WX-671) is a serine protease inhibitor. Upamostat is the orally available prodrug of the WX-UK1, which is a urokinase plasminogen activator (uPA) inhibitor.
  • HY-14736
    Azilsartan medoxomil

    TAK-491

    Angiotensin Receptor Cardiovascular Disease Endocrinology
    Azilsartan medoxomil(TAK 491) is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension.
  • HY-19989A
    MK-571 sodium salt

    L-660711 sodium salt

    Leukotriene Receptor Inflammation/Immunology
    MK-571 sodium salt is a selective, orally active leukotriene D4 receptor antagonist, with Kis of 0.22 and 2.1 nM in guinea pig and human lung membranes.
  • HY-12870A
    AZD9496 maleate

    Estrogen Receptor/ERR Cancer
    AZD9496 maleate is a potent and selective estrogen receptor (ERα) antagonist with IC50 of 0.28 nM. AZD9496 maleate is an orally bioavailable selective oestrogen receptor degrader (SERD).
  • HY-112305
    AZ32

    ATM/ATR Cancer
    AZ32 is an orally bioavailable and blood-brain barrier-penetrating ATM inhibitor with an IC50 of <6.2 nM for ATM enzyme, and an IC50 of 0.31 μM for ATM in cell.
  • HY-101873
    Atorvastatin lactone

    HMG-CoA Reductase (HMGCR) Metabolic Disease Inflammation/Immunology
    Atorvastatin lactone is a prodrug form of atorvastatin. Atorvastatin is an orally active 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor.
  • HY-15947A
    Ravoxertinib hydrochloride

    GDC-0994 hydrochloride

    ERK Cancer
    Ravoxertinib hydrochloride (GDC-0994 hydrochloride) is an orally bioavailable inhibitor selective for ERK kinase activity with IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.
  • HY-15315
    Baricitinib

    LY3009104; INCB028050

    JAK Inflammation/Immunology
    Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
  • HY-50709
    A939572

    Stearoyl-CoA Desaturase (SCD) Cancer
    A939572 is a potent, and orally bioavailable stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50 values of <4 nM and 37 nM for mSCD1 and hSCD1, respectively.
  • HY-124669
    RTC-30

    Others Cancer
    RTC-30 is an optimized phenothiazine with anti-cancer potency. RTC-30 contains a hydroxylated linker (N) that confers increased oral bioavailability.
  • HY-16025
    EOC317

    ACTB-1003

    FGFR VEGFR Cancer
    EOC317 (ACTB-1003) is an oral kinase inhibitor with IC50s of 6, 2 and 4 nM for FGFR1, VEGFR2 and Tie-2.
  • HY-101437A
    Ralfinamide mesylate

    FCE-26742A mesylate

    Sodium Channel Neurological Disease
    Ralfinamide mesylate (FCE-26742A mesylate) is an orally available Na + channel blocker derived from α-aminoamide, with function of suppressing pain.
  • HY-50714
    Quiflapon sodium

    MK-591 sodium

    FLAP Apoptosis Inflammation/Immunology
    Quiflapon sodium (MK-591 sodium) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor. Quiflapon sodium is an orally active Leukotriene biosynthesis inhibitor. Induces apoptosis.
  • HY-112623
    Vafidemstat

    ORY-2001

    Histone Demethylase Monoamine Oxidase Neurological Disease
    Vafidemstat (ORY-2001) is an oral, brain penetrant, dual lysine-specific histone demethylase (LSD1)/MAO-B inhibitor.
  • HY-19562
    PF-06260933

    MAP4K Inflammation/Immunology
    PF-06260933 is an orally active and highly selective inhibitor of MAP4K4 with IC50s of 3.7 and 160 nM for kinase and cell, respectively.
  • HY-114403
    VU6012962

    mGluR Neurological Disease
    VU6012962 is an orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM) with an IC50 of 347 nM.
  • HY-B1141
    Eprodisate disodium

    NC-503

    Others Others
    Eprodisate disodium (NC-503) is the orally available disodium salt form of Eprodisate, a negatively charged sulfonated inhibitor of fibrillogenesis, that can be used in the treatment of amyloid A (AA) amyloidosis.
  • HY-10011
    SCH 563705

    CXCR Inflammation/Immunology Endocrinology
    SCH 563705 is a potent and orally available CXCR2 and CXCR1 antagonist, with IC50s of 1.3 nM, 7.3 nM and Kis of 1 and 3 nM, respectively.
  • HY-120274
    AZD9977

    Mineralocorticoid Receptor Metabolic Disease Cardiovascular Disease
    AZD9977 is a potent, selective, and orally active mineralocorticoid receptor (MR) modulator. AZD9977 is used for heart failure, and chronic kidney disease research.
  • HY-101907
    ASP7663

    TRP Channel Neurological Disease
    ASP7663 is an orally active and selective TRPA1 agonist. ASP7663 exerts both anti-constipation and anti-abdominal pain actions.
  • HY-15277
    AM966

    LPL Receptor Inflammation/Immunology
    AM966 is a high affinity, selective, oral LPA1-antagonist, inhibits LPA-stimulated intracellular calcium release (IC50=17 nM).
  • HY-118930
    MK-0493

    Melanocortin Receptor Endocrinology Metabolic Disease
    MK-0493 is a potent, orally active and selective agonist of the melanocortin receptor 4 (MC4R), demonstrating significant reductions in energy intake.
  • HY-14574
    PF-03814735

    Aurora Kinase VEGFR Cancer
    PF-03814735 is a potent, orally available, ATP-competitive and reversible aurora A and aurora B inhibitor with IC50s of 0.8 and 0.5 nM, respectively.
  • HY-19612B
    DDP-38003 trihydrochloride

    Histone Demethylase Cancer
    DDP-38003 trihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.
  • HY-122903B
    (+)-TK216

    DNA/RNA Synthesis Others
    (+)-TK216 is an enantiomer of TK216 (HY-122903). TK216 is an orally active and potent E26 transformation specific (ETS) inhibitor.
  • HY-101114
    LAS191954

    PI3K Inflammation/Immunology
    LAS191954 is a potent, selective and orally active PI3Kδ inhibitor for inflammatory diseases treatment, with an IC50 of 2.6 nM.
  • HY-17469
    Gimeracil

    Gimestat

    Others Cancer
    Gimeracil, a component of an oral fluoropyrimidine derivative S-1, inhibits DNA DSB repair and is a potent inhibitor of DPYD (dihydropyrimidine dehydrogenase, DPD).
  • HY-13233B
    Talabostat isomer mesylate

    Others Others
    Talabostat isomer mesylate is an isomer of talabostat mesylate. Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM.
  • HY-14844
    Lagociclovir

    MIV-210

    HBV Infection
    Lagociclovir(MIV-210) is a prodrug of 3'-fluoro-2',3'-dideoxyguanosine with high oral bioavailability in humans and potent activity against HBV.
  • HY-112929
    DT-061

    Phosphatase Cancer
    DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis.
  • HY-19612A
    DDP-38003 dihydrochloride

    Histone Demethylase Cancer
    DDP-38003 dihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.
  • HY-101383
    PF-01247324

    Sodium Channel Neurological Disease
    PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker with an IC50 of 196 nM for recombinant human Nav1.8 channel.
  • HY-18632
    GSK2879552

    Histone Demethylase Cancer
    GSK2879552 an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/ KDM1A), with potential antineoplastic activity.
  • HY-111050
    JNJ-38877618

    c-Met/HGFR Cancer
    JNJ-38877618 is a potent, highly selective, orally bioavailable Met kinase inhibitor with IC50s of 2 and 3 nM for wild type and mutant Met, respectively.
  • HY-10286A
    Dutogliptin tartrate

    PHX-1149

    Dipeptidyl Peptidase Metabolic Disease
    Dutogliptin tartrate (PHX-1149) is an orally available, potent, and selective dipeptidyl peptidase-4 (DPP4) inhibitor for the treatment of type 2 diabetes mellitus.
  • HY-124600
    NVR 3-778

    HBV Infection
    NVR 3-778 is a first-in-Class and oral bioavailable HBV CAM (capsid assembly modulator) belonging to the SBA (sulfamoylbenzamide) class, with anti-HBV activity.
  • HY-138642
    ARV-471

    Estrogen Receptor/ERR PROTACs Cancer
    ARV-471 is a best-in-class, orally active estrogen receptor (ER) PROTAC degrader. ARV-471 is developed for the research of breast cancer.
  • HY-N8377
    Capsiate

    TRP Channel Inflammation/Immunology
    Capsiate, as a capsaicin analogue extracted from a non-pungent cultivar of CH-19 sweet red pepper, is an orally active agonist of TRPV1.
  • HY-112912
    P-gp modulator 1

    P-glycoprotein Cancer
    P-gp modulator 1 is a high affinity, orally available modulator of P-glycoprotein (Pgp), can reverse the Pgp-mediated multidrug resistance ((MDR).
  • HY-137573
    Trotabresib

    CC-90010

    Epigenetic Reader Domain Cancer
    CC-90010 (compound 1) is a reversible and orally active BET inhibitor. CC-90010 is applied in the study for advanced solid tumors.
  • HY-138625A
    LOX-IN-3 dihydrochloride

    Monoamine Oxidase Cancer
    LOX-IN-3 dihydrochloride is an orally active lysyl oxidase (LOX) inhibitor. LOX-IN-3 dihydrochloride can be used for fibrosis, cancer and/or angiogenesis research.
  • HY-B0262S
    Methocarbamol D5

    Sodium Channel Metabolic Disease
    Methocarbamol D5 is deuterium labeled Methocarbamol. Methocarbamol is an orally active central muscle relaxant and blocks muscular Nav1.4 channel.
  • HY-12870
    AZD9496

    Estrogen Receptor/ERR Cancer
    AZD9496 is a potent and selective estrogen receptor (ERα) antagonist with an IC50 of 0.28 nM. AZD9496 is an orally bioavailable selective oestrogen receptor degrader (SERD).
  • HY-132199
    SJ6986

    Others Cancer
    SJ6986 is a potent, selective and orally active GSPT1/2 degrader, with a DC50 of 2.1 nM (Dmax 99%) for GSPT1.
  • HY-111498A
    RGX-104

    LXR Cancer Inflammation/Immunology
    RGX-104 is an orally bioavailable and potent liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
  • HY-17608
    Daprodustat

    GSK1278863

    HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease
    Daprodustat (GSK1278863) is an orally active hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor being developed for the treatment of anemia associated with chronic kidney disease.
  • HY-111390
    Dot1L-IN-2

    Histone Methyltransferase Cancer
    Dot1L-IN-2 is a potent, selective and orally bioavailable inhibitor of Dot1L (a histone methyltransferase), with an IC50 and Ki of 0.4 nM and 0.08 nM, respectively.
  • HY-138625
    LOX-IN-3

    Monoamine Oxidase Cancer
    LOX-IN-3 is an orally active lysyl oxidase (LOX) inhibitor. LOX-IN-3 can be used for fibrosis, cancer and/or angiogenesis research.
  • HY-108532
    AC-261066

    RAR/RXR Cancer
    AC-261066 is a potent, orally available and isoform-selective retinoic acid beta2 (RARbeta2) receptor agonist, with a pEC50 of 8.0.
  • HY-122737
    RORγt Inverse agonist 8

    ROR Inflammation/Immunology
    RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist, with an IC50 of 19 nM for human RORγt-LBD.
  • HY-12835
    S1P1 Agonist III

    LPL Receptor Inflammation/Immunology
    S1P1 Agonist III is a potent and orally active S1P1 agonist with EC50 of 18 nM; no activity on S1P3.
  • HY-15197
    ABT-046

    Acyltransferase Metabolic Disease
    ABT-046 is a potent, selective, and orally efficacious acyl CoA:diacylglycerol acyltransferase 1 (DGAT-1) inhibitor (IC50= 8 nM).
  • HY-14807
    Tosedostat

    CHR-2797

    Aminopeptidase Cancer
    Tosedostat (CHR-2797) is an orally active aminopeptidase inhibitor. CHR-2797 exerts antiproliferative effects against a range of tumor cell lines.
  • HY-131341
    Syk-IN-4

    Syk Cancer Inflammation/Immunology
    Syk-IN-4 is a potent, selective and orally bioavailable SYK inhibitor with an IC50 of 0.31 nM. SYK has emerged as a potential target for autoimmunity and hematological cancers.
  • HY-114392
    Gly-β-MCA

    FXR Autophagy Metabolic Disease
    Gly-β-MCA, a bile acid, is a potent, sable, intestine-selective and oral bioactive farnesoid X receptor (FXR) inhibitor that may be a candidate for the treatment of metabolic disorders.
  • HY-100740
    Lanabecestat

    AZD3293; LY3314814

    Beta-secretase Neurological Disease
    Lanabecestat (AZD3293) is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM. Lanabecestat is used for the research of Alzheimer's disease.
  • HY-13660
    Mocravimod hydrochloride

    KRP-203

    LPL Receptor Inflammation/Immunology
    Mocravimod hydrochloride (KRP-203), an immunosuppressant, is a potent and orally active S1PR1 (sphingosine 1-phosphate receptor type 1) agonist.
  • HY-B1789A
    Telenzepine dihydrochloride

    mAChR Neurological Disease
    Telenzepine dihydrochloride is a selective and orally active muscarinic M1 receptor antagonist with a Ki of 0.94 nM. Telenzepine dihydrochloride inhibits gastric acid secretion and has antiulcer effects.
  • HY-14880A
    Bavisant dihydrochloride

    Histamine Receptor Neurological Disease Endocrinology
    Bavisant Hcl (JNJ-31001074) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD.
  • HY-123046
    AS1708727

    Autophagy Cancer Metabolic Disease
    AS1708727 is an orally active Foxo1 inhibitor, with EC50 values of 0.33 μM and 0.59 μM for G6Pase and PEPCK, respectively.
  • HY-109055
    Elenbecestat

    E2609

    Beta-secretase Neurological Disease
    Elenbecestat (E2609) is a potent, orally bioavailable and CNS-penetrant BACE-1 inhibitor. Elenbecestat has the potential for Alzheimer's disease (AD) research.
  • HY-13328
    Sapanisertib

    INK-128; MLN0128; TAK-228

    mTOR Autophagy Cancer
    Sapanisertib (INK-128; MLN0128; TAK-228) is an orally available, ATP-dependent mTOR1/2 inhibitor with an IC50 of 1 nM for mTOR kinase.
  • HY-122908
    Atuliflapon

    AZD5718

    FLAP Cardiovascular Disease
    Atuliflapon (AZD5718) is an orally active inhibitor of FLAP (5‑Lipoxygenase activating protein), with an IC50 of 2 nM. Atuliflapon is used in the study for coronary artery disease.
  • HY-17036
    Naphthoquine phosphate

    Parasite Infection
    Naphthoquine phosphate is a potent and orally active antimalarial agent. Naphthoquine phosphate has thorough killing function for various schizonts of plasmodia, including resistance of P. falciparum to Chloroquine.
  • HY-17492
    Zafirlukast

    ICI 204219

    Leukotriene Receptor Inflammation/Immunology Cancer
    Zafirlukast (ICI 204219) is a potent orally active leukotriene D4 (LTD4) receptor antagonist. Zafirlukast shows anti-asthmatic, anti-inflammatory and anti-bacterial effects.
  • HY-18175
    CCT244747

    Checkpoint Kinase (Chk) Cancer
    CCT244747 is a potent, orally bioavailable and highly selective CHK1 inhibitor, with an IC50 of 7.7 nM; CCT244747 also abrogates G2 checkpoint with an IC50 of 29 nM.
  • HY-111409
    RIP1 kinase inhibitor 1

    RIP kinase Inflammation/Immunology
    RIP1 kinase inhibitor 1 (compound 22) is a highly potent, orally available, and brain-penetrating RIP1 kinase inhibitor (pKi=9.04).
  • HY-128354
    CWHM-1552

    Parasite Infection
    CWHM-1552 is an orally efficacious inhibitor of P. falciparum with IC50s of 51 nM and 53 nM for 3D7 and Dd2 strain, respectively.
  • HY-15315A
    Baricitinib phosphate

    LY3009104 phosphate; INCB028050 phosphate

    JAK Inflammation/Immunology
    Baricitinib phosphate (LY3009104 phosphate; INCB028050 phosphate) is a selective orally bioavailable JAK1/JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, respectively.
  • HY-100757
    CPUY074020

    Histone Methyltransferase Cancer
    CPUY074020 is a potent and oral bioavailable inhibitor of histone methyltransferase G9a, with an IC50 of 2.18 μM. CPUY074020 possesses anti-proliferative activity.
  • HY-50855
    Silmitasertib

    CX-4945

    Casein Kinase Autophagy Cancer
    Silmitasertib (CX-4945) is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC50 values of 1 nM against CK2α and CK2α'.
  • HY-126137
    PDE9-IN-1

    Phosphodiesterase (PDE) Neurological Disease
    PDE9-IN-1 is a potent, selective, and orally bioavailable phosphodiesterase-9A (PDE9A) Inhibitor with an IC50 of 8.7 nM.
  • HY-109136
    Runcaciguat

    Guanylate Cyclase Cardiovascular Disease
    Runcaciguat is an orally active stimulator of soluble guanylate cyclase, and is used in the research of cardiovascular and renal diseases combined with selective partial adenosine A1 receptor agonists.
  • HY-15656S
    Ceritinib D7

    LDK378 D7

    ALK Insulin Receptor IGF-1R Cancer Endocrinology
    Ceritinib D7 (LDK378 D7) is a deuterium labeled Ceritinib. Ceritinib is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor.
  • HY-103088
    E7046

    Prostaglandin Receptor Cancer Endocrinology
    E7046 is an orally bioavailable and specific EP4 antagonist, with IC50 of 13.5 nM and Ki of 23.14 nM. E7046 exhibits anti-tumor activities.
  • HY-10159S
    Nilotinib D6

    AMN107 D6

    Bcr-Abl Autophagy Cancer
    Nilotinib D6 (AMN107 D6) is a deuterium labeled Nilotinib. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
  • HY-B0016S
    Capecitabine-d11

    DNA/RNA Synthesis Nucleoside Antimetabolite/Analog Apoptosis Cancer
    Capecitabine-d11 is the deuterium labeled Capecitabine. Capecitabine is an oral prodrug that is converted to its active metabolite, 5-FU, by thymidine phosphorylase.
  • HY-114388
    QM385

    Others Inflammation/Immunology
    QM385 is a potent sepiapterin reductase (SPR) inhibitor with an IC50 of 1.49 nM, which blocks T-cell proliferation and autoimmunity at nanomolar potency and with good oral bioavailability.
  • HY-100694
    GS-9901

    PI3K Inflammation/Immunology
    GS-9901 is a highly selective and orally active PI3Kδ inhibitor, with an IC50 of 1 nM. Has potential to treat rheumatoid arthritis.
  • HY-101760
    GSK2982772

    RIP kinase Inflammation/Immunology
    GSK2982772 is a potent, orally active and ATP competitive RIP1 kinase inhibitor with IC50 values of 16 nM and 20 nM for human and monkey RIP1, respectively.
  • HY-14723
    AMG-458

    c-Met/HGFR Cancer
    AMG-458 is a potent, selective and orally bioavailable c-Met inhibitor, with Ki values of 1.2 nM and 2.0 nM for human and mouse c-Met, respectively.
  • HY-126131
    anti-TB agent 1

    Bacterial Infection
    anti-TB agent 1 is a potent and orally active anti-tuberculosis agent, with MICs of < 2 nM against the Mtb strains H37Rv, rRMP and rINH.
  • HY-14880B
    Bavisant dihydrochloride hydrate

    JNJ31001074AAC

    Histamine Receptor Neurological Disease Endocrinology
    Bavisant dihydrochloride hydrate (JNJ31001074AAC) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD.
  • HY-B0524A
    Betahistine dihydrochloride

    Histamine Receptor Endocrinology Inflammation/Immunology Neurological Disease
    Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA).
  • HY-13836
    ELQ-300

    Parasite Infection
    ELQ-300 is a potent and orally bioavailable antimalarial agent, acts as an inhibitor of the reductive (Qi) site of the cytochrome bc1 complex (cyt bc1).
  • HY-18233
    E1210

    APX001A

    Fungal Infection
    E1210 is a first-in-class, broad-spectrum and orally active antifungal. E1210 has a mechanism of action-inhibition of fungal glycosylphosphatidylinositol (GPI) biosynthesis.
  • HY-15532B
    SCH900776 (S-isomer)

    MK-8776 S-isomer

    Others Cancer
    SCH900776 S-isomer is the S-isomer of SCH900776. SCH900776 is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with IC50 of 3 nM.
  • HY-138626
    ACH-000143

    Melatonin Receptor Metabolic Disease
    ACH-000143 is a potent and orally active melatonin receptor agonist, with EC50 values of 0.06 nM and 0.32 nM for MT1 and MT2, respectively.
  • HY-120261
    GB-88

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    GB-88 is an oral, selective non-peptide antagonist of PAR2, inhibits PAR2 activated Ca 2+ release with an IC50 of 2 µM.
  • HY-100015
    Mivebresib

    ABBV-075

    Epigenetic Reader Domain Apoptosis Cancer
    Mivebresib (ABBV-075) is a potent and orally active bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib binds to BRD4 with a Ki of 1.5 nM.
  • HY-13245
    PF-4136309

    INCB8761

    CCR Inflammation/Immunology Endocrinology
    PF-4136309 is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50s of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2.
  • HY-107575
    TLR4-IN-C34

    Toll-like Receptor (TLR) Inflammation/Immunology
    TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis.
  • HY-15675
    AZD1656

    Glucokinase Metabolic Disease
    AZD1656 is a potent, selective and orally active glucokinase activator with an EC50 of 60 nM. AZD1656 has the potential for type 2 diabetes research.
  • HY-128599
    NMS-P515

    PARP Cancer
    NMS-P515 is a potent, orally active and stereospecific PARP-1 inhibitor, with a Kd of 16 nM and an IC50 of 27 nM (in Hela cells). Anti-tumor activity.
  • HY-12469
    Decernotinib

    VX-509; VRT-831509

    JAK Inflammation/Immunology
    Decernotinib is a potent, orally active JAK3 inhibitor, with Kis of 2.5, 11, 13 and 11 nM for JAK3, JAK1, JAK2, and TYK2, respectively.
  • HY-13990
    NVP-TNKS656

    TNKS656

    PARP Apoptosis Cancer
    NVP-TNKS656 is a highly potent, selective, and orally active TNKS2 inhibitor with IC50 of 6 nM, and is > 300 fold selectivity against PARP1 and PARP2.
  • HY-131449
    Terazosin dimer impurity dihydrochloride

    Adrenergic Receptor Others
    Terazosin dimer impurity dihydrochloride, a dimer of Terazosin, is an impurity of Terazosin. Terazosin is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist.
  • HY-19519A
    Ladarixin sodium

    DF 2156A

    CXCR Infection Inflammation/Immunology
    Ladarixin sodium (DF 2156A) is an orally active, allosteric non-competitive and dual CXCR1 and CXCR2 antagonist. Ladarixin sodium can be used for the research of COPD and asthma.
  • HY-133807A
    (Rac)-Benpyrine

    TNF Receptor Inflammation/Immunology
    (Rac)-Benpyrine, a racemate of Benpyrine, is a potent and orally active TNF-α inhibitor. (Rac)-Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research.
  • HY-10286
    Dutogliptin

    PHX-1149 free base

    Dipeptidyl Peptidase Metabolic Disease
    Dutogliptin (PHX-1149 free base) is an orally available, potent, and selective dipeptidyl peptidase-4 (DPP4) inhibitor for the treatment of type 2 diabetes mellitus.
  • HY-D0237
    Betahistine mesylate

    Histamine Receptor Inflammation/Immunology
    Betahistine mesylate is an orally active histamine H1 receptor agonist and a H3 receptor antagonist. Betahistine mesylate is used for the study of rheumatoid arthritis (RA).
  • HY-112284
    Ebopiprant

    OBE022

    Prostaglandin Receptor Endocrinology
    Ebopiprant (OBE022) is an oral and selective prostaglandin F (PGF) receptor antagonist, with Kis of 1 nM, 26 nM for human and rat FP receptors, respectively.
  • HY-12472
    Balipodect

    TAK-063

    Phosphodiesterase (PDE) Neurological Disease
    Balipodect (TAK-063) is a highly potent, selective and orally active PDE10A inhibitor with IC50 of 0.30 nM; >15000-fold selectivity over other PDEs.
  • HY-14880
    Bavisant

    JNJ-31001074

    Histamine Receptor Neurological Disease Endocrinology
    Bavisant (JNJ-31001074) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD.
  • HY-136346
    2-Hydroxy atorvastatin lactone

    Drug Metabolite Others
    2-Hydroxy atorvastatin lactone is a metabolite of Atorvastatin. Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids.
  • HY-B0524
    Betahistine

    Histamine Receptor Cancer Inflammation/Immunology
    Betahistine is an orally active histamine H1 receptor agonist and a H3 receptor antagonist. Betahistine is used for the study of rheumatoid arthritis (RA).
  • HY-16640
    TCJL37

    JAK Inflammation/Immunology
    TCJL37 is a potent, selective, and orally bioavailable TYK2 inhibitor with a Ki of 1.6 nM. TCJL37 can be used for the research of inflammatory bowel diseases (IBD).
  • HY-11029
    SNT-207707

    Melanocortin Receptor Cancer Metabolic Disease Endocrinology
    SNT-207707 is a selective, potent and orally active melanocortin MC-4 receptor antagonist with an IC50 of 8 nM (binding) and 5 nM (function) on the MC-4 receptor.
  • HY-101857
    MGAT2-IN-1

    Acyltransferase Metabolic Disease
    MGAT2-IN-1 is an orally active inhibitor of monoacylglycerol acyltransferase (MGAT2) with IC50 of 7.8 and 2.4 nM for human and mouse MGAT2, respectively.
  • HY-133555
    mGluR2 antagonist 1

    mGluR Neurological Disease
    mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 nM) with excellent brain permeability.
  • HY-12449
    Crenigacestat

    LY3039478

    Notch γ-secretase Cancer
    Crenigacestat (LY3039478) is an orally active Notch and γ-secretase inhibitor, with an IC50 of 1 nM in most of the tumor cell lines tested.
  • HY-10333
    BMS-690514

    EGFR VEGFR Cardiovascular Disease Cancer
    BMS-690514 is a potent and orally active inhibitor of EGFR and VEGFR; has IC50s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively.
  • HY-B0804S
    Nadolol D9

    SQ-11725 D9

    Adrenergic Receptor Endocrinology Cardiovascular Disease
    Nadolol D9 (SQ-11725 D9) is the deuterium labeled Nadolol. Nadolol is a non-selective and orally active β-adrenergic receptors blocker.
  • HY-101023
    MK-8617

    HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology
    MK-8617 is an orally active pan-inhibitor of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) with an IC50 of 1 nM for PHD2.
  • HY-107781
    PAT-505

    Phosphodiesterase (PDE) Inflammation/Immunology
    PAT-505 is a potent, selective, noncompetitive and orally available autotaxin inhibitor, with an IC50 of 2 nM in Hep3B cells, 9.7 nM in human blood and 62 nM in mouse plasma.
  • HY-B0790
    TAI-1

    Apoptosis Cancer
    TAI-1, an orally active anticancer agent, is a highly potent first-in-class Hec1 inhibitor, with a GI50 of 13.48 nM in K562 cells.
  • HY-16779
    Fosravuconazole

    BMS-379224; E-1224

    Fungal Parasite Infection
    Fosravuconazole (BMS-379224), a prodrug of Ravuconazole, is an orally active broad spectrum antifungal agent. Fosravuconazole can be used for candidiasis, onychomycosis and parasitemia research.
  • HY-B0568S
    Deferiprone-d3

    HCV Ferroptosis Cardiovascular Disease Cancer
    Deferiprone-d3 is the deuterium labeled Deferiprone. Deferiprone is the only orally active iron-chelating drug to be used therapeutically in conditions of transfusional iron overload.
  • HY-109066
    Olinciguat

    IW-1701

    Guanylate Cyclase Cardiovascular Disease
    Olinciguat (IW-1701) is an oral guanylate cyclase (sGC) stimulator with concentration-dependent stimulation of sGC in purified rat and human enzyme assays and a whole cell assay.
  • HY-66011A
    Moxifloxacin

    Bacterial Antibiotic Infection
    Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia.
  • HY-14841
    Gisadenafil

    UK-369003

    Phosphodiesterase (PDE) Neurological Disease
    Gisadenafil (UK-369003) is a specific, orally active phosphodiesterase 5 (PDE5) inhibitor with an IC50 of 3.6 nM and prevents degradation of cyclic guanosine monophosphate (cGMP).
  • HY-114162A
    VTP50469 fumarate

    Epigenetic Reader Domain Apoptosis Cancer
    VTP50469 fumarate is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 fumarate has potently anti-leukemia activity.
  • HY-11034
    CVT-12012

    Stearoyl-CoA Desaturase (SCD) Metabolic Disease
    CVT-12012 is a potent and orally bioavailable stearoyl-coA desaturase (SCD) inhibitor, with IC50s of 38 nM, 6.1 nM for rat microsomal and human HEPG2, respectively.
  • HY-100373
    Isavuconazonium sulfate

    BAL8557-002

    Fungal Infection
    Isavuconazonium sulfate (BAL8557-002), the prodrug of the active triazole Isavuconazole, is an orally active antifungal agent. Isavuconazonium sulfate is used for invasive aspergillosis and mucormycosis.
  • HY-17598
    Rafoxanide

    Parasite Infection
    Rafoxanide is an orally active salicylanilide anthelmintic agent. Rafoxanide is an antiparasitic agent and can be used for the control of infestation with Hemonchus species and Fasciola species in sheep and cattle.
  • HY-111356
    IIIM-290

    CDK Cancer
    IIIM-290 is a potent and oral CDK inhibitor with IC50s of 90 and 94 nM for CDK2/A and CDK9/T1.
  • HY-32709
    Telcagepant

    MK-0974

    CGRP Receptor Neurological Disease
    Telcagepant (MK-0974) is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist with Kis of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively.
  • HY-16956
    Onatasertib

    CC-223; ATG-008

    mTOR Apoptosis Cancer
    Onatasertib (CC-223) is a potent, selective, and orally bioavailable inhibitor of mTOR kinase, with an IC50 value for mTOR kinase of 16 nM. Onatasertib inhibits both mTORC1 and mTORC2.
  • HY-135381
    3-Oxo Atorvastatin

    Others Cardiovascular Disease
    3-Oxo Atorvastatin is an impurity of 3-Oxo Atorvastatin. Atorvastatin is an orally active HMG-CoA reductase inhibitor and has the ability to effectively decrease blood lipids.
  • HY-111500
    (Rac)-NMDAR antagonist 1

    iGluR Neurological Disease
    (Rac)-NMDAR antagonist 1 is the racemate of NMDAR antagonist 1. NMDAR antagonist 1 is a potent and orally bioavailable NR2B-selective NMDAR antagonist.
  • HY-112723
    ACT-709478

    Calcium Channel Neurological Disease
    ACT-709478 is a potent, selective, orally active, and brain penetrating T-type calcium channel blocker. ACT-709478 is used in the research of generalized epilepsies.
  • HY-B0972
    Cinchophen

    Others Inflammation/Immunology
    Cinchophen is a potent and orally active non-steroidal anti-inflammatory agent, has analgesic and antimicrobial effects. Cinchophen can be used for the research of arthritis and some liver diseases.
  • HY-15889A
    AMG 925 HCl

    FLT3 CDK Cancer
    AMG 925 HCl is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with IC50s of 2±1 nM and 3±1 nM, respectively.
  • HY-128356
    SPL-410

    Others Inflammation/Immunology
    SPL-410 is an orally active, highly potent and selective hydroxyethylamine based SPPL2a (Signal Peptide Peptidase Like 2a) inhibitor, with an IC50 of 9 nM.
  • HY-109148
    Izencitinib

    TD-1473; JNJ-8398

    JAK Inflammation/Immunology
    Izencitinib (TD-1473) is an orally active, non-selective and gut-restricted JAK inhibitor. Izencitinib (TD-1473) can be used in the study for ulcerative colitis.
  • HY-13234S
    Rifaximin-d6

    Bacterial Antibiotic Infection
    Rifaximin-d6 is the deuterium labeled Rifaximin. Rifaximin is an orally administered, semi-synthetic, nonsystemic antibiotic derived from rifamycin SV with antibacterial activity.
  • HY-114162
    VTP50469

    Epigenetic Reader Domain Apoptosis Cancer
    VTP50469 is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 has potently anti-leukemia activity.
  • HY-15891
    GW311616

    Elastase Inflammation/Immunology
    GW-311616 is a potent, orally bioavailable, long duration and selective human neutrophil elastase (HNE) inhibitor with IC50 value of 22 nM and Ki value of 0.31 nM.
  • HY-112542
    Nemadectin

    CL-287088; LL-F28249 α

    Parasite Antibiotic Infection
    Nemadectin (CL-287088), an orally active broad-spectrum endectocide, is highly efficacious against natural infections of all the major canine gastrointestinal helminthes. Anthelmintic activity.
  • HY-108045
    Lodenafil carbonate

    Phosphodiesterase (PDE) Endocrinology
    Lodenafil carbonate, a dimer that acts as a prodrug delivering Lodenafil in vivo, is an orally active phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED).
  • HY-B0196B
    (S)-Venlafaxine

    Serotonin Transporter Cancer
    (S)-Venlafaxine is the (S)-configuration of Venlafaxine. Venlafaxine is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant agent.
  • HY-15889
    AMG 925

    FLT3 CDK Cancer
    AMG 925 is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with IC50s of 2±1 nM and 3±1 nM, respectively.
  • HY-15498
    Rimegepant

    BMS-927711

    CGRP Receptor Neurological Disease
    Rimegepant (BMS-927711) is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki of 0.027 nM and an IC50 of 0.14 nM for hCGRP receptor.
  • HY-101978
    CPI-444

    V81444; ciforadenant

    Adenosine Receptor Cancer
    CPI-444 (V81444) is a potent, orally active and selective adenosine A2A receptor (A2AR) antagonist, which induces antitumor responses.
  • HY-14316A
    Tebanicline dihydrochloride

    Ebanicline dihydrochloride; ABT-594 dihydrochloride

    nAChR Neurological Disease
    Tebanicline dihydrochloride (Ebanicline dihydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM.
  • HY-12294A
    PEAQX tetrasodium hydrate

    NVP-AAM077 tetrasodium hydrate

    iGluR Apoptosis Neurological Disease
    PEAQX (NVP-AAM077) tetrasodium hydrate is a potent, selective and orally active NMDA antagonist, with IC50 values of 270 nM and 29600 nM for hNMDAR 1A and hNMDAR 2A, respectively.
  • HY-12340
    ETP-46321

    PI3K Cancer
    ETP-46321 is a potent and orally bioavailable PI3Kα and PI3Kδ inhibitor with Kiapps of 2.3 and 14.2 nM, respectively.
  • HY-B1069
    Molsidomine

    SIN-10; Morsydomine

    Others Cardiovascular Disease
    Molsidomine is an orally active, long acting vasodilating drug, metabolized in the liver to the active metabolite linsidomine, which is an unstable compound that releases nitric oxide (NO) upon decay as the actual vasodilating compound.
  • HY-141677
    INCB059872