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Results for "

bioavailable

" in MCE Product Catalog:

559

Inhibitors & Agonists

16

Screening Libraries

2

Biochemical Assay Reagents

6

Peptides

1

Inhibitory Antibodies

11

Natural
Products

30

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-141711
    VU6028418

    		mAChR Neurological Disease
    VU6028418 is a potent, highly selective and orally bioavailable M4 mAChR antagonist with an IC50 of 4.1 nM against hM4.
  • HY-15531
    Venetoclax

    ABT-199; GDC-0199; RG7601

    		 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-151196
    FXIa-IN-10

    		Others Cardiovascular Disease
    FXIa-IN-10 (Compound 3f) is a potent activated factor XI (FXIa) inhibitor with an Ki of 0.17 nM. FXIa-IN-10 has good oral bioavailability.
  • HY-W013331
    Deoxy artemisinin

    		Others Inflammation/Immunology
    Deoxy artemisinin, a orally bioavailable compound separated from Artemisinin annua L., shows anti-inflammatory and antiulcer activities.
  • 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-14568
    DCCCyB

    		GlyT Neurological Disease
    DCCCyB is an orally bioavailable, potent, and selective inhibitor of GlyT1. DCCCyB demonstrates excellent in vivo occupancy of GlyT1 transporters in rhesus monkey.
  • HY-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-12839
    p38 MAPK-IN-1

    		p38 MAPK Autophagy Inflammation/Immunology
    p38 MAPK-IN-1 (Compound 4) is a novel potent and selective inhibitor of p38 MAPK with IC50 of 68 nM. p38 MAPK-IN-1 shows sustained levels, low clearance and good bioavailability.
  • HY-15651A
    Alvelestat tosylate

    AZD9668 tosylate

    		 Elastase Inflammation/Immunology
    Alvelestat (tosylate) is an orally bioavailable, affinity and selective inhibitor of neutrophil elastase (NE) with a pIC50 value of 7.9 nM, a Ki value of 9.4 nM and a Kd value of 9.5 nM.
  • HY-119696
    MTIC

    		Drug Metabolite Cancer Neurological Disease
    MTIC is the active metabolite of Temozolomide (TMZ). MITC has lower bioavailability in the brain compared with TMZ, because the agent’s permeability through biological barriers and tumor cell membranes affects bioavailability. MITC exhibits low affinity to biological membrane.
  • HY-16247
    Apoptone

    HE3235

    		 Others Cancer
    Apoptone, synthetic analogue of 3β-androstanediol, is an orally bioavailable anticancer agent. Apoptone is active in rodent models of prostate and breast cancer.
  • 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-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-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-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-103061
    Dehydro-ZINC39395747

    		Others Cardiovascular Disease
    Dehydro-ZINC39395747 is a derivative of ZINC39395747. ZINC39395747 is a potent cytochrome b5 reductase 3 (CYB5R3) inhibitor with an IC50 of 9.14 μM and a Kd of 1.11 μM. ZINC39395747 can increase NO bioavailability in vascular cells.
  • 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-146267
    ERα degrader 5

    		Estrogen Receptor/ERR Cancer
    ERα degrader 5 (Compound 40) is a selective, orally bioavailable estrogen receptor (ER) degrader (SERD) with an EC50 of 1.1 nM against ERα. ERα degrader 5 shows antitumor effect in vivo.
  • HY-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-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-15043
    ELN-441958

    		Bradykinin Receptor Endocrinology Inflammation/Immunology
    ELN-441958 is a potent, neutral, competitive and selective bradykinin B1 receptor antagonist with a Ki of 0.26 nM against native human bradykinin B1 receptor. ELN-441958 has high oral bioavailability, and has low CNS exposure in the mouse.
  • HY-145695
    Dual AChE-MAO B-IN-1

    		Cholinesterase (ChE) Monoamine Oxidase Neurological Disease
    Dual AChE-MAO B-IN-1 (compound 15) is an orally bioavailable CNS-permeant potent inhibitor of both human AChE (IC50=550 nM) and MAO B (IC50=8.2 nM). Dual AChE-MAO B-IN-1 behaves as a safe and metabolically stable neuroprotective agent, devoid of cytochrome liability.
  • HY-122011
    PF-4950834

    		ROCK SGK PKA PKC Inflammation/Immunology
    PF-4950834 is a potent, selective, orally bioavailable, ATP-competitive rho kinase inhibitor with IC50 values of 8.35 nM and 33.12 nM against ROCK2 and ROCK1, respectively. PF-4950834 inhibits neutrophil migration.
  • HY-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-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-118301
    ADX71441

    		GABA Receptor Neurological Disease
    ADX71441 is a potent and selective positive allosteric modulator of the GABAB receptor. ADX71441 is bioavailable after oral administration and is brain penetrant. ADX71441 has the potential for research of anxiety, pain and spasticity.
  • HY-116804
    ZLD1039

    		Histone Methyltransferase Cancer
    ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC50 values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis.
  • HY-12113
    Oprozomib

    ONX 0912; PR-047

    		 Proteasome Autophagy Apoptosis 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-144770
    SARS-CoV-2-IN-13

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

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

    		SARS-CoV Infection
    SARS-CoV-2-IN-15 (compound 11) is a potent inhibitor of SARS-CoV-2 with an IC50 of 0.49 μM. SARS-CoV-2-IN-15 is a niclosamide analogue. SARS-CoV-2-IN-15 contains higher stability in human plasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally.
  • HY-145311
    Bis-Pro-5FU

    		Nucleoside Antimetabolite/Analog Cancer
    Bis-Pro-5FU (Compound 4) is a 5-FU precursor that confers oral bioavailability and increase the safety profile of 5-Fluorouracil (5-FU) chemotherapy regimens. 5-FU is an antineoplastic antimetabolite that is widely used for the research of colorectal and pancreatic cancer.
  • HY-144878
    VPC-70619

    		c-Myc Cancer
    VPC-70619 is a potent, orally active N-Myc inhibitor. VPC-70619 blocks the N-Myc-Max heterocomplex from binding to DNA E-boxes and demonstrated strong inhibition activity against N-Myc-dependent cell lines as well as high bioavailability in both oral and intraperitoneal administration.
  • HY-146789
    PI3Kδ/γ-IN-2

    		PI3K Cancer
    PI3Kδ/γ-IN-2 is a potent PI3Kδ and PI3Kγ dual inhibitor with IC50s of 1 nM and 4.3 nM, respectively. PI3Kδ/γ-IN-2 has favorable oral bioavailability. PI3Kδ/γ-IN-2 has potential for battling B-cell malignancies.
  • HY-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-10619E
    Niraparib tosylate hydrate

    MK-4827 tosylate hydrate

    		 PARP Apoptosis Cancer
    Niraparib (MK-4827) tosylate hydrate is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib tosylate hydrate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
  • 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-139981
    Microtubule destabilizing agent-1

    		Microtubule/Tubulin Cancer
    Microtubule destabilizing agent-1 (Compound 12b) acts as a microtubule destabilizing agent (MDA) based on hydroxamic acid, could serve as a potential MDA for further investigation. Microtubule destabilizing agent-1 shows favorable metabolism stability, high bioavailability, and potent antitumor activity.
  • HY-145835
    PERK-IN-5

    		PERK Cancer
    PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC50s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model.
  • HY-102074
    ERDRP-0519

    		Others Infection
    ERDRP-0519, an orally bioavailable small-molecule Measles virus (MeV) polymerase inhibitor, prevents measles disease in squirrel monkeys (Saimiri sciureus). ERDRP-0519 inhibits morbilliviruses with nanomolar potency..
  • HY-144660
    AChE-IN-7

    		Cholinesterase (ChE) Neurological Disease
    AChE-IN-7 (Compound 16) is a selective and potent inhibitor of acetylcholinesterase (eeAChE IC50 = 0.045 μM; eeBuChE IC50 = 19.68 μM). AChE-IN-7 is safe in vivo and in vitro, and shows good overall pharmacokinetic performance and high bioavailability (F = 55.5%). AChE-IN-7 also has high BBB permeability.
  • HY-120124
    Samelisant

    SUVN-G3031

    		 Histamine Receptor Neurological Disease
    Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders.
  • HY-116000
    Glumetinib

    Gumarontinib; 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-122608
    Samelisant free base

    SUVN-G3031 free base

    		 Histamine Receptor Neurological Disease
    Samelisant (SUVN-G3031) free base is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant free base has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant free base can be used for the research of sleep-related disorders.
  • HY-10096
    TCS2002

    		GSK-3 Neurological Disease
    TCS2002 (Compound 9b) is a highly selective, orally bioavailable and potent GSK-3β inhibitor with the IC50 of 35 nM. TCS2002 shows good pharmacokinetic profiles including favorable BBB penetration. TCS2002 can be used for the research of Alzheimer’s disease.
  • HY-145594
    Safusidenib

    AB-291; DS-1001

    		 Isocitrate Dehydrogenase (IDH) Cancer
    Safusidenib (AB-291; DS-1001) is an orally bioavailable, selective mutant IDH1 inhibitor. Safusidenib strongly inhibits mutant IDH1 but not wild-type IDH1. Safusidenib impairs tumor activity in chondrosarcoma. Safusidenib exhibits activity against IDH1R132H, and IDH1R132C with IC50s of 15, and 130 nM in assays without any preincubation, respectively.
  • HY-151360
    NHE3-IN-3

    		Sodium Channel Metabolic Disease
    NHE3-IN-3 (Compound 1) is a Na +/H + exchanger isoform 3 (NHE3) inhibitor with pIC50 of 6.2 and 6.6 against human and rat NHE3, respectively. NHE3-IN-3 shows high (98%) oral bioavailability in Sprague–Dawley rats.
  • HY-109142
    Ziresovir

    AK0529; RO-0529

    		 RSV Infection
    Ziresovir (AK0529;RO-0529) is a potent, selective, and orally bioavailable respiratory syncytial virus (RSV) fusion (F) protein (RSV F) protein inhibitor. Ziresovir shows anti-RSV activity (EC50=3 nM) and highlights pharmacokinetics in animal species.
  • HY-145559
    Cemdomespib

    KU-596

    		 HSP Metabolic Disease
    Cemdomespib (KU-596) is a highly bioavailable second-generation Hsp90 modulator. Cemdomespib has shown efficacy in improving sensory deficits in models of diabetic peripheral neuropathy. Cemdomespib induces Hsp70 levels and manifest neuroprotective activity through induction of the heat shock response.
  • 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-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-148825
    NP10679

    		iGluR Histamine Receptor Potassium Channel Cytochrome P450 Adrenergic Receptor Cancer Metabolic Disease Inflammation/Immunology
    NP10679 is a selective, pH dependent GluN2B subunit-specific N-methyl-D-aspartate (NMDA) receptor inhibitor with high oral bioavailability and good brain penetration. NP10679 inhibits GluN2B with IC50s of 23 and 142 nM at pH 6.9 and 7.6, respectively. NP10679 is a histamine H1 antagonist and a hERG channel inhibitor with IC50s of 73 and 620 nM, respectively. NP10679 is a reversible inhibitor of human liver CYP enzymes.
  • HY-144393
    P-gp/BCRP-IN-1

    		BCRP Cancer
    P-gp/BCRP-IN-1 (compound 19) is a potential, relatively safe, orally active and efficient efflux transporter (P-gp and BCRP) inhibitor. P-gp/BCRP-IN-1 exerts resistance reversal by inhibiting the efflux function of P-gp and BCRP. P-gp/BCRP-IN-1 can overcome the resistance and improve the oral bioavailability of PTX (Paclitaxel).
  • HY-100709
    ZPCK

    SL-01

    		 Nucleoside Antimetabolite/Analog DNA/RNA Synthesis Autophagy Apoptosis Cancer
    ZPCK is an oral active proagent of gemcitabine that was designed for improved oral bioavailability.
  • HY-141431
    Cbl-b-IN-2

    		E3 Ligase Ligand-Linker Conjugates Cancer Inflammation/Immunology
    Cbl-b-IN-2 (Example 8) is an orally bioavailable compound, can inhibit the E3 enzyme Casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) in the ubiquitin proteasome pathway. Cbl-b-IN-2 can be used to modulate the immune system and diseases amenable to immune system modulation. Cbl-b-IN-2 (Example 8) also may be administered to an individual with cancer, either alone or as part of a combination, with one or more of an immune checkpoint inhibitor, an anti-neoplastic agent, and radiation agent.
  • 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-151260
    AChE/BACE1/GSK3β-IN-1

    		Beta-secretase Cholinesterase (ChE) GSK-3 Neurological Disease
    AChE/BACE1/GSK3β-IN-1 is an orally active triple inhibitor of AChE/BACE1/GSK3β. AChE/BACE1/GSK3β-IN-1 has effective inhibitory activity against AChE, BACE1 and GSK3β with IC50 values of 1.0 μM, 20 μM and 15 μM, respectively. AChE/BACE1/GSK3β-IN-1 has good blood-brain barrier penetrability, suitable bioavailability. AChE/BACE1/GSK3β-IN-1 can be used for the research of Alzheimer's disease (AD).
  • 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-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-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-146223
    AZD4625

    		Ras Cancer
    AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS G12C. AZD4625 has high oral bioavailability.
  • HY-19324
    EPZ031686

    		Histone Methyltransferase Cancer
    EPZ031686 is an potent and orally active SMYD3 inhibitor and with an IC50 value of 3 nM. EPZ031686 can be used for cancer research.
  • HY-B1149A
    Bacampicillin hydrochloride

    		Bacterial Antibiotic Infection
    Bacampicillin hydrochloride is a penicillin antibiotic, is a prodrug of ampicillin with improved oral bioavailability.
  • 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-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-114530
    LY2452473

    		Androgen Receptor Cancer Metabolic Disease
    LY2452473 is an orally bioavailable, selective androgen receptor modulator (SARM).
  • HY-115874
    BMS-753426

    		CCR Others
    BMS-753426 is a potent and orally bioavailable antagonist of CCR2.
  • HY-145356
    HbF inducer-1

    		Others Others
    HbF inducer-1 is an orally bioavailable fetal hemoglobin inducer.
  • HY-17630
    Edasalonexent

    CAT-1004

    		 NF-κB Metabolic Disease
    Edasalonexent (CAT-1004) is an orally bioavailable NF-κB inhibitor.
  • HY-151535
    SARS-CoV-2 3CLpro-IN-5

    		SARS-CoV Infection Inflammation/Immunology
    SARS-CoV-2 3CLpro-IN-5 is a covalent inhibitor of 3C-like protease (3CL pro). SARS-CoV-2 3CLpro-IN-5 has inhibitory activity for 3CL pro with an IC50 value of 3.8 nM. SARS-CoV-2 3CLpro-IN-5 has 9.0% oral bioavailability (BA). SARS-CoV-2 3CLpro-IN-5 can be used for the research of coronavirus disease 2019 (COVID-19).
  • HY-12802
    AF38469

    		Neurotensin Receptor Neurological Disease
    AF38469 is a selective, orally bioavailable Sortilin inhibitor with an IC50 value of 330 nM.
  • HY-19947
    PF-06291874

    Glucagon receptor antagonists-4

    		 GCGR 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-15604
    AZD1208

    		Pim Autophagy Apoptosis Cancer
    AZD1208 is an orally bioavailable, highly selective PIM kinases inhibitor.
  • HY-107986
    GNE-6776

    		Deubiquitinase Cancer
    GNE-6776 is a selective and orally bioavailable USP7 inhibitor.
  • HY-76260
    Faropenem sodium

    		Bacterial Antibiotic Infection
    Faropenem sodium is an orally bioavailable penem antibiotic which can efficiently kill Mycobacterium tuberculosis.
  • HY-15604A
    AZD1208 hydrochloride

    		Pim Autophagy Apoptosis Cancer
    AZD1208 hydrochloride is an orally bioavailable, highly selective PIM kinases inhibitor.
  • HY-112298
    DS88790512

    		TRP Channel Cardiovascular Disease
    DS88790512 is a potent, selective, and orally bioavailable TRPC6 inhibitor with an IC50 of 11 nM.
  • HY-19323
    Ceralasertib

    AZD6738

    		 ATM/ATR Cancer
    Ceralasertib (AZD6738) is an orally active and bioavailable inhibitor of ATR kinase with an IC50 of 1 nM.
  • HY-139885
    c-Myc inhibitor 4

    		c-Myc Cancer
    c-Myc inhibitor 4 is a potent, orally bioavailable c-MYC-reducing compound.
  • HY-114147
    Tuberculosis inhibitor 3

    		Bacterial Infection Inflammation/Immunology
    Tuberculosis inhibitor 3 (compound 2i) displays potent anti-TB activity (MIC < 0.016 μg/mL) against agent-sensitive/resistant MTB strains. Tuberculosis inhibitor 3 (compound 2i) shows acceptable PK profiles with oral bioavailability.
  • 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-132901
    IACS-15414

    		SHP2 Phosphatase Cancer
    IACS-15414 is a potent and orally bioavailable SHP2 inhibitor with an IC50 value of 122 nM.
  • 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-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-14178
    VX-11e

    		ERK Cancer
    VX-11e is a potent, selective, and orally bioavailable inhibitor of ERK with Ki < 2 nM.
  • HY-100026
    PQR620

    		mTOR Cancer
    PQR620 is an orally bioavailable and selective brain penetrant inhibitor of mTORC1/2.
  • HY-16925
    MI-503

    		Epigenetic Reader Domain Cancer
    MI-503 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.
  • HY-16902
    RO9021

    		Syk Inflammation/Immunology
    RO9021 is an orally bioavailable, novel ATP-competitive inhibitor of SYK, with an average IC50 of 5.6 nM.
  • HY-145354
    FXIa-IN-7

    		Factor Xa Cardiovascular Disease
    FXIa-IN-7 is a selective and orally bioavailable factor XIa inhibitor with an IC50 value of 0.4 nM.
  • HY-101103
    (2-Hydroxypropyl)-β-cyclodextrin

    Hydroxypropyl betadex; Hydroxypropyl-β-cyclodextrin; HP-β-CD

    		 Biochemical Assay Reagents Cancer
    (2-Hydroxypropyl)-β-cyclodextrin is a widely used drug delivery vehicle to improve the stability and bioavailability.
  • 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-141895
    Vps34-IN-3

    		PI3K Cancer
    Vps34-IN-3 is a potent, selective, and orally bioavailable VPS34 kinase inhibitor.
  • HY-10480
    Fasiglifam

    TAK-875

    		 Free Fatty Acid Receptor Metabolic Disease
    Fasiglifam (TAK-875) is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 72 nM.
  • HY-19809
    MI-463

    		Epigenetic Reader Domain Cancer
    MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.
  • HY-139901
    Chk1-IN-6

    		Checkpoint Kinase (Chk) Cancer
    Chk1-IN-6 is a potent, selective, and orally bioavailable CHK1 inhibitor candidate.
  • HY-151805
    RGT-068A

    		MALT1 Cancer
    RGT-068A is a potent, selective and oral bioavailable MALT1 inhibitor.
  • 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-119696S
    MTIC-d3

    		Isotope-Labeled Compounds Drug Metabolite Cancer Neurological Disease
    MTIC-d3 is deuterium labeled MTIC. MTIC is the active metabolite of Temozolomide (TMZ). MITC has lower bioavailability in the brain compared with TMZ, because the agent’s permeability through biological barriers and tumor cell membranes affects bioavailability. MITC exhibits low affinity to biological membrane[1].
  • HY-151625
    PARP-2-IN-3

    		PARP Apoptosis Cancer
    PARP-2-IN-3 (Compound 12) is a potent PARP-2 inhibitor with an IC50 of 0.07 μM. PARP-2-IN-3 induces apoptosis and necrosis in cancer cells. PARP-2-IN-3 shows appropriate predicted pharmacokinetic parameters and oral bioavailability.
  • 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-122616
    PF-06273340

    		Trk Receptor Inflammation/Immunology
    PF-06273340 is a potent, selective, orally bioavailable and peripherally restricted pan Trk inhibitor.
  • HY-132900
    RORγ agonist 1

    		ROR Cancer
    RORγ agonist 1 is a potent and orally bioavailable RORγ agonist (EC50 = 21 nM) with antitumor activity.
  • HY-142214
    TRPA1-IN-1

    		TRP Channel Others
    TRPA1-IN-1 is a potent, selective, and orally bioavailable TRPA1 small molecule antagonist.
  • HY-125879
    DS08210767

    		Thyroid Hormone Receptor Metabolic Disease Endocrinology
    DS08210767 is a highly potent, orally bioavailable PTHR1 antagonist with IC50 of 90 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-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-109046
    Tulrampator

    CX-1632; S-47445

    		 iGluR Neurological Disease
    Tulrampator (CX-1632) is an orally bioavailable positive AMPAR (allosteric modulator of AMPA receptor). Antidepressant.
  • HY-109004
    Enzaplatovir

    BTA-C585

    		 RSV Infection
    Enzaplatovir (BTA-C585) is an orally bioavailable Inhibitor for respiratory syncytial virus (RSV) infection.
  • 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-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-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-132189
    Laniquidar

    R101933

    		 P-glycoprotein Cancer
    Laniquidar (R101933) is a noncompetitive, third generation P-glycoprotein (P-gp) inhibitor with an IC50 of 0.51 μM. Laniquidar can be used for modulating multidrug resistance transporters. Laniquidar can also be used for studying acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS). Laniquidar has limited oral bioavailability.
  • HY-144073
    HPK1-IN-21

    		MAP4K Cancer
    HPK1-IN-21 is a potent inhibitor of HPK1 kinase inhibitor (Ki=0.8 nM). HPK1-IN-21 also has orally active.
  • HY-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-146391
    P-gp inhibitor 4

    		P-glycoprotein Cancer
    P-gp inhibitor 4 (Compound 8b) is a selective P-glycoprotein modulator with an EC50 of 94 nM. P-gp inhibitor 4 increases agent transport across gastro-intestinal barrier and recovers doxorubicin toxicity in multidrug resistant cancer cells.
  • HY-104059
    AMG2850

    		TRP Channel Inflammation/Immunology
    AMG2850 is a potent, orally bioavailable and selective transient receptor potential melastatin 8 (TRPM8) antagonist.
  • 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-111500A
    NMDAR antagonist 1

    		iGluR Neurological Disease
    NMDAR antagonist 1 is a potent and orally bioavailable NR2B-selective NMDAR antagonist.
  • 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-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-14419
    TCN238

    		mGluR Neurological Disease
    TCN238 is an orally bioavailable mGlu4 receptor positive allosteric modulator (PAM) with an EC50 of 1 μM.
  • HY-112386
    OXSI-2

    		Syk Inflammation/Immunology
    OXSI-2 is a bioavailable, cell-permeable Syk inhibitor with an EC50 of 313 nM and an IC50 of 14 nM.
  • 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-141845
    S1P2 antagonist 1

    		LPL Receptor Others
    S1P2 antagonist 1 is an orally bioavailable S1P2 antagonist against fibrotic diseases.
  • 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-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 Apoptosis Cancer
    ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
  • 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-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-139998
    PCSK9-IN-3

    		Ser/Thr Protease Cardiovascular Disease
    PCSK9-IN-3 is a novel, highly potent, and orally bioavailable next-generation tricyclic peptide PCSK9 inhibitor.
  • HY-132880
    GSK251

    		PI3K Cancer
    GSK251 is a highly potent, highly selective, orally bioavailable inhibitor of PI3Kδ with a novel binding mode.
  • 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-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-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-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-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-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-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-13301
    MPC-3100

    		HSP Cancer
    MPC-3100 is an orally bioavailable, synthetic, second-generation small-molecule inhibitor of Hsp90 with potential antineoplastic activity.
  • 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-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-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-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-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[1].
  • 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

    		Drug Metabolite Others
    Ivabradine impurity 1 is an Ivabradine impurity. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker.
  • 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-131282
    Ivabradine impurity 2

    		Drug Metabolite Others
    Ivabradine impurity 2 is an Ivabradine impurity. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker.
  • HY-150080
    GSK3739936

    BMS-986180

    		 HIV HIV Integrase Infection
    GSK3739936 (BMS-986180) is a potent HIV-1 allosteric integrase inhibitor with an IC50 value of 11.1 nM and an EC50 value of 1.7 nM. GSK3739936 is also a weak CYP inhibitor (IC50>24.3 μM). GSK3739936 shows favorable pharmacokinetic property in preclinical species with rapid absorption, low to moderate clearance and excellent oral bioavailability.
  • HY-12045
    HMN-214

    IVX-214

    		 Polo-like Kinase (PLK) Cancer
    HMN-214, an orally bioavailable proagent of HMN-176, is an inhibitor of polo-like kinase-1 (plk1), with antitumor activity.
  • HY-15656S
    Ceritinib D7

    LDK378 d7

    		 Anaplastic lymphoma kinase (ALK) Insulin Receptor IGF-1R Cancer Endocrinology
    Ceritinib-d7 is a deuterium labeled Ceritinib. Ceritinib is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor[1].
  • HY-114535
    Jaceidin

    		EGFR Cancer
    Jaceidin is a promising lead molecule for potent VEGFR inhibitor with excellent membrane permeability and oral bioavailability. Jaceidin exhibits anti-tumor activities.
  • HY-145119
    GS-621763

    		SARS-CoV Infection
    GS-621763, an orally bioavailable proagent of GS-441524, shows antiviral activity against SARS-CoV-2 pathogenesis in mice.
  • HY-19883S
    Lusutrombopag-d13

    S-888711-d13

    		 Thrombopoietin Receptor Inflammation/Immunology
    Lusutrombopag-d13 is deuterium labeled Lusutrombopag. Lusutrombopag is an orally bioavailable thrombopoietin (TPO) receptor agonist, used for treatment of chronic liver disease.
  • 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-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-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-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-13467
    AM-1638

    		Free Fatty Acid Receptor Metabolic Disease
    AM-1638 is a potent and orally bioavailable GPR40/FFA1 full agonist with an EC50 of 0.16 μM.
  • 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-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

    		 FBPase Metabolic Disease
    Managlinat dialanetil (MB06322) is an orally bioavailable inhibitor of fructose 1,6-bisphosphatase (FBPase) for the treatment of type 2 diabetes .
  • 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-136197
    StRIP16

    		Ras Cancer
    StRIP16, bioavailable StRIP3 analogue, is a double-stapled peptide which can bind to Rab8a GTPase, with a Kd of 12.7 μM.
  • 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 IC50 of 2.3 nM for rSCD1.
  • 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-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-139573
    Etavopivat

    FT-4202

    		 Pyruvate Kinase Inflammation/Immunology
    Etavopivat is a potent, selective, orally bioavailable red blood cell (RBC) pyruvate kinase (PKR) activator. Etavopivat has potent antisickling effects.
  • 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-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-12410
    GNE-9822

    		Itk Inflammation/Immunology
    GNE-9822 is a potent, orally active and selective ITK inhibitor with a Ki value of 0.7 nM. GNE-9822 has good ADME properties. GNE-9822 can be used in research of asthma.
  • HY-N10648
    PTP1B-IN-20

    		Phosphatase Metabolic Disease
    PTP1B-IN-20 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B; IC50=1.05 μM) over the highly homologous T-cell protein tyrosine phosphatase (TCPTP; IC50=78.0 μM), which is a key target for type 2 diabetes inhibition.
  • HY-147654
    PROTAC Hemagglutinin Degrader-1

    		PROTACs Influenza Virus Infection
    PROTAC Hemagglutinin Degrader-1 (Compound V3) is a potent PROTAC influenza hemagglutinin (HA) degrader with a median degradation concentration of 1.44 μM. PROTAC Hemagglutinin Degrader-1 shows broad-spectrum anti-influenza virus activity.
  • HY-N10649
    PTP1B-IN-21

    		Phosphatase Metabolic Disease
    PTP1B-IN-21 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B; IC50=1.56 μM) over the highly homologous T-cell protein tyrosine phosphatase (TCPTP; IC50>100 μM), which is a key target for type 2 diabetes inhibition.
  • HY-139485
    BMS-986224

    		Others Cardiovascular Disease
    BMS-986224 is a potent, selective and orally active 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-134494
    MS48107

    		GPR68 Neurological Disease
    MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). MS48107 is selective for GPR68 over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS48107 can readily cross the blood-brain barrier (BBB) in mice.
  • 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-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-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-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-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-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-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-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-111498A
    RGX-104

    Abequolixron

    		 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-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-114245
    Se-Methylselenocysteine

    Methylselenocysteine; Se-Methylseleno-L-cysteine

    		 Apoptosis Endogenous Metabolite 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-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-146057
    Antituberculosis agent-2

    		Bacterial Infection
    Antituberculosis agent-2 (Compound 8d) is an antituberculosis agent against agent-sensitive and multidrug-resistant tuberculosis. Antituberculosis agent-2 shows anti-tuberculosis activity with MIC values of 0.454, 1.757 and 1.644 μg/mL against M. tuberculosis H37Rv, 13946 and 14862, respectively. Antituberculosis agent-2 displays favorable mouse and human microsomal stability, low cytotoxicity, and acceptable oral bioavailability.
  • 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-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-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-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-103088
    Palupiprant

    E7046

    		 Prostaglandin Receptor Cancer Endocrinology
    Palupiprant (E7046) is an orally bioavailable and specific EP4 antagonist, with IC50 of 13.5 nM and Ki of 23.14 nM. Palupiprant exhibits anti-tumor activities.
  • 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-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-N2253
    Neoruscogenin

    		ROR Infection Neurological Disease
    Neoruscogenin, a member of the steroidal sapogenin family, is a bioavailable, potent, and high-affinity agonist of the nuclear receptor RORα (NR1F1).
  • 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-144300
    Rifasutenizol

    TNP-2198

    		 Bacterial Infection
    Rifasutenizol (TNP-2198) is a potent and orally bioavailable dual-targeted antibacterial agent. Rifasutenizol has potent activity against microaerophilic and anaerobic bacterial pathogens.
  • 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-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-145344
    ONO-8430506

    		Phosphodiesterase (PDE) Cancer
    ONO-8430506 is an orally bioavailable and potent autotaxin (ATX)/ENPP2 inhibitor with the IC90 of 100 nM for ATX activity in mouse plasma.
  • 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-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-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-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-B0689S
    Indinavir-d6

    MK-639-d6 (free base); L-735524-d6 (free base)

    		 HIV HIV Protease Inflammation/Immunology
    Indinavir-d6 is the deuterium labeled Indinavir. Indinavir (MK-639; L735524) is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability.
  • 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-15891A
    GW311616 hydrochloride

    GW311616A

    		 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-139624
    JNK3 inhibitor-1

    		JNK Others
    JNK3 inhibitor-1 is a potent and selective JNK3 inhibitor (IC50 = 0.005 μM). JNK3 inhibitor-1 is orally bioavailable and brain penetrant.
  • 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-101842
    ND-646

    		Acetyl-CoA Carboxylase Cancer
    ND-646 is an orally bioavailable and steric inhibitor of acetyl-CoA carboxylase (ACC) with IC50s of 3.5 nM and 4.1 nM for recombinant hACC1 and hACC2, respectively.
  • HY-12599
    URMC-099

    		Mixed Lineage Kinase Autophagy Neurological Disease Cancer
    URMC-099 is an orally bioavailable and potent mixed lineage kinase type 3 (MLK3) (IC50=14 nM) inhibitor with with excellent blood-brain barrier penetration properties.
  • HY-10758
    FXa-IN-1

    		Factor Xa Cardiovascular Disease
    FXa-IN-1 is a FXa inhibitor (IC50: 3 nM, Ki: 0.7 nM) with respectable oral bioavailability and half-life in vivo. FXa-IN-1 can be used for thromboembolic disorders.
  • HY-128593
    TPN171

    		Phosphodiesterase (PDE) Cardiovascular Disease
    TPN171 is a potent, selective and oral bioavailable inhibitor of phosphodiesterase type 5 (PDE5) with an IC50 of 0.62 nM, being developed for the treatment of pulmonary arterial hypertension (PAH).
  • HY-B1486
    Oxprenolol hydrochloride

    Ba 39089

    		 Adrenergic Receptor Cardiovascular Disease
    Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle.
  • 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-114277A
    Sotorasib racemate

    AMG-510 racemate

    		 Ras Cancer
    Sotorasib (AMG-510) racemate is the racemate of Sotorasib (AMG-510). AMG-510 is a potent, orally bioavailable, and selective KRAS G12C covalent inhibitor with anti-tumor activity.
  • HY-114411
    ERRγ Inverse Agonist 1

    		Estrogen Receptor/ERR Cancer
    ERRγ Inverse Agonist 1 (Compound 12) is a potent, selective and orally bioavailable Estrogen-related Receptor grammar (ERRγ) inverse agonist, with an IC50 of 40 nM.
  • HY-107145A
    Ningetinib

    		TAM Receptor VEGFR c-Met/HGFR Cancer
    Ningetinib is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.
  • HY-10191
    Linsitinib

    OSI-906

    		 IGF-1R Insulin Receptor Cancer Endocrinology
    Linsitinib (OSI-906) is a potent, selective and orally bioavailable dual inhibitor of the IGF-1 receptor and insulin receptor (IR) with IC50s of 35 and 75 nM, respectively.
  • HY-15651
    Alvelestat

    AZD9668

    		 Elastase Inflammation/Immunology
    Alvelestat (AZD9668) is an orally bioavailable, affinity and selective inhibitor of neutrophil elastase (NE) with a pIC50 value of 7.9 nM, a Ki value of 9.4 nM and a Kd value of 9.5 nM.
  • HY-16391
    Glasdegib

    PF-04449913

    		 Smo Cancer
    Glasdegib (PF-04449913) is a potent and orally bioavailable smoothened inhibitor. Glasdegib (PF-04449913) binds to human SMO (amino acids 181-787) with an IC50 of 4 nM.
  • HY-112286
    PI3Kγ inhibitor 2

    		PI3K Inflammation/Immunology
    PI3Kγ inhibitor 2 (Compound 16) is an orally bioavailable, CNS-penetrant, isoform selective PI3Kγ inhibitor with a Ki of 4 nM.
  • HY-13592
    HDAC-IN-7

    Chidamide impurity

    		 HDAC Cancer
    HDAC-IN-7 (Chidamide impurity) is an impurity of Chidamide. Chidamide is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor.
  • HY-13809
    BMS-833923

    XL-139

    		 Smo Apoptosis Cancer
    BMS-833923 (XL-139) is an orally bioavailable small-molecule inhibitor of Smoothened with potential antineoplastic activity; inhibits BODIPY cyclopamine binding to SMO in a dose-dependent manner with an IC50 of 21 nM.
  • HY-107145
    Ningetinib Tosylate

    		TAM Receptor VEGFR c-Met/HGFR Cancer
    Ningetinib Tosylate is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.
  • HY-19483
    ABT-670

    		Dopamine Receptor Neurological Disease
    ABT-670 is a selective, oral bioavailable agonist of dopamine D4 receptor, with EC50 of 89 nM, 160 nM, and 93 nM for human D4, ferret D4, and rat D4, respectively.
  • HY-135399S
    Tauro-Obeticholic acid-d5 sodium

    		FXR Inflammation/Immunology
    Tauro-Obeticholic acid-d5 (sodium) is deuterium labeled Tauro-Obeticholic acid. Tauro-Obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist[1].
  • HY-111505
    NAcM-OPT

    		E1/E2/E3 Enzyme NEDD8-activating Enzyme Cancer
    NAcM-OPT is an orally bioavailable cullin neddylation 1 (DCN1) inhibitor, which potently inhibits the DCN1-UBE2M interaction.
  • HY-10244
    MK-0608

    		HCV Infection
    MK-0608 is a potent and orally bioavailable inhibitor of HCV replication in vitro with an EC50 of 0.3 μM (EC90=1.3 μM) in the subgenomic-replicon assay.
  • HY-10302
    MK-3207 Hydrochloride

    		CGRP Receptor Neurological Disease
    MK-3207 (Hydrochloride) is a potent and orally bioavailable CGRP receptor antagonist with IC50 of 0.12 nM and Ki of 0.024 nM, and is highly selective versus human AM1, AM2, CTR, and AMY3.
  • HY-15454
    Xevinapant

    AT-406; Debio 1143; SM-406

    		 IAP Apoptosis Cancer
    Xevinapant (AT-406) is a potent and orally bioavailable Smac mimetic and an antagonist of IAPs, and it binds to XIAP, cIAP1, and cIAP2 proteins with Ki of 66.4, 1.9, and 5.1 nM, respectively.
  • HY-146460
    Antimicrobial agent-2

    		Reactive Oxygen Species Infection
    Antimicrobial agent-2 (compound V-a) is a broad-spectrum antimicrobial agent, possessing inhibitory activity against various Gram-positive and -negative bacteria. Antimicrobial agent-2 has excellent inhibitory effect on Methicillin-resistant Staphylococcus aureus (MRSA) with a MIC of 1 μg/mL. Antimicrobial agent-2 can effectively damage the membrane and lead to the leakage of protein, also can induce the generation of ROS. Antimicrobial agent-2 exhibits low toxicity, no obvious resistance and good bioavailability.
  • HY-112335
    Lck Inhibitor III

    		Src Interleukin Related Cancer
    Lck Inhibitor III (compound 12h) is a potent Lck inhibitor, with an IC50 of 867 nM. Lck Inhibitor III inhibits IL-2 synthesis in Jurkat cells, with an IC50 of 1.270 μM.
  • HY-12282
    GNE-9605

    		LRRK2 Neurological Disease
    GNE-9605 is a potent, orally active, selective Leucine-rich repeat kinase 2 (LRRK2) inhibitor with an IC50 value of 18.7 nM. GNE-9605 inhibits LRRK2 Ser1292 autophosphorylation. GNE-9605 can be used in research of Parkinson's disease (PD) .
  • HY-135336A
    (S)-Verapamil hydrochloride

    (S)-(-)-Verapamil hydrochloride

    		 Leukotriene Receptor Calcium Channel Apoptosis Cancer
    (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells.
  • 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-113906A
    (αR,8aS)-GSK1614343

    		GHSR Inflammation/Immunology
    (αR,8aS)-GSK1614343 (compound 18a, d2) is a cyclized ghrelin antagonist with an pIC50 value of 8.4. (αR,8aS)-GSK1614343 shows a competitive antagonism of hGHSR1a with a mean pKb value of 8.06.
  • HY-147653
    Integrase-LEDGF/p75 allosteric inhibitor 1

    		HIV Integrase Infection
    Integrase-LEDGF/p75 allosteric inhibitor 1 (Compound 31h) is an orally active integrase-LEDGF/p75 (IN-LEDGF/p75) allosteric inhibitor. Integrase-LEDGF/p75 allosteric inhibitor 1 inhibits HIV-1 DNA integration and shows antiviral activity with an EC50 of 3.9 nM against HIV-1 recombinant molecular clone NL432.
  • HY-17001
    Flupirtine Maleate

    		Potassium Channel iGluR Neurological Disease
    Flupirtine Maleate is a brain penetrant, and orally bioavailable, non-opioid and centrally acting analgesic agent. Flupirtine Maleate is an indirect N-methyl-D-aspartate receptor (NMDAR) antagonist. Neuroprotective properties.
  • HY-16751
    Ralinepag

    APD811

    		 Prostaglandin Receptor Cardiovascular Disease Endocrinology
    Ralinepag is a potent, orally bioavailable and non-prostanoid prostacyclin (IP) receptor agonist, with EC50s of 8.5 nM, 530 nM and 850 nM for human and rat IP receptor and human DP1 receptor, respectively.
  • HY-131952
    TLR7/8/9-IN-1

    		Toll-like Receptor (TLR) Inflammation/Immunology
    TLR7/8/9-IN-1 is a potent and orally bioavailable small molecule antagonist (IC50 = 43 nM) of Toll-like receptors 7/8/9 (TLR7/8/9).
  • HY-122682
    SBI-993

    		Others Metabolic Disease
    SBI-993 is a SBI-477 analog with improved potency and suitable pharmacokinetic properties for in vivo bioavailability. SBI-993 stimulates insulin signaling by deactivating the transcription factor MondoA.
  • HY-B1486A
    Oxprenolol

    Ba 39089 free base

    		 Adrenergic Receptor Cardiovascular Disease
    Oxprenolol (Ba 39089 free base) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle.
  • HY-13270
    ABT-751

    E7010

    		 Microtubule/Tubulin Autophagy Cancer
    ABT-751(E 7010) is a novel bioavailable tubulin-binding and antimitotic sulfonamide agent with IC50 of about 1.5 and 3.4 μM in neuroblastoma and non-neuroblastoma cell lines, respectively.
  • HY-10422
    AZD-8055

    		mTOR Autophagy Apoptosis Cancer
    AZD-8055 is a potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM. AZD-8055 inhibits both mTORC1 and mTORC2.
  • HY-101789
    Nav1.7-IN-3

    		Sodium Channel Neurological Disease
    Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration.
  • HY-15287
    Nelfinavir

    AG1341

    		 HIV Protease HIV Infection Cancer
    Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir is a broad-spectrum, anticancer agent.
  • HY-139798
    Iboxamycin

    		Bacterial Infection
    Iboxamycin is a potent antibiotic candidate bearing a fused bicyclic amino acid residue. Iboxamycin is orally bioavailable, safe and effective in researching both Gram-positive and Gram-negative bacterial infections in mice.
  • HY-135230
    LY2444296

    FP3FBZ

    		 Opioid Receptor Neurological Disease
    LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ∼1 nM. LY2444296 exhibits anti-anxiety like effects.
  • HY-13914
    Roniciclib

    BAY 1000394

    		 CDK Cancer
    Roniciclib is an orally bioavailable pan-cyclin dependent kinase (CDK) inhibitor, with IC50s of 5-25 nM for CDK1, CDK2, CDK3, CDK4, CDK7 and CDK9.
  • HY-N2593
    Isorhapontigenin

    		Autophagy Cancer Inflammation/Immunology
    Isorhapontigenin, an orally bioavailable dietary polyphenol isolated from the Chinese herb Gnetum cleistostachyum, displays anti-inflammatory effects. Isorhapontigenin induces autophagy and inhibits invasive bladder cancer formation.
  • HY-106441A
    Rislenemdaz

    MK-0657; CERC-301

    		 iGluR Neurological Disease
    Rislenemdaz (CERC-301) is an orally bioavailable and selective N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B) antagonist with Ki and IC 50 of 8.1 nM and 3.6 nM, respectively.
  • HY-15287A
    Nelfinavir Mesylate

    AG 1343 Mesylate

    		 HIV Protease HIV Cancer Infection
    Nelfinavir Mesylate (AG 1343 Mesylate) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir Mesylate (AG 1343 Mesylate) is a broad-spectrum, anticancer agent.
  • HY-13735A
    Quinacrine dihydrochloride

    Mepacrine dihydrochloride; SN-390 dihydrochloride

    		 Parasite Apoptosis Autophagy Mitophagy Cancer Infection
    Quinacrine (Mepacrine) dihydrochloride is an orally bioavailable antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine dihydrochloride suppresses NF-κB and activate p53 signaling, which results in the induction of the apoptosis.
  • HY-141411A
    Zevaquenabant

    (S)-MRI-1867

    		 Cannabinoid Receptor NO Synthase Metabolic Disease
    Zevaquenabant ((S)-MRI-1867) is a peripherally restricted, orally bioavailable dual cannabinoid CB1 receptor and inducible NOS antagonist. Zevaquenabant ameliorates obesity-induced chronic kidney disease (CKD).
  • HY-30237
    (R)-Roscovitine

    Seliciclib; CYC202

    		 CDK Cancer
    (R)-Roscovitine (Seliciclib) is an orally bioavailable and selective CDKs inhibitor with IC50s of 0.2 μM, 0.65 μM, and 0.7 μM for CDK5, Cdc2, and CDK2, respectively.
  • HY-13318
    Oseltamivir acid

    GS 4071; Ro 64-0802; Oseltamivir carboxylate

    		 Influenza Virus Drug Metabolite Infection
    Oseltamivir acid (GS 4071), the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC50=2 nM) with activity against both influenza A and B viruses.
  • HY-144122
    HIV-1 inhibitor-15

    		HIV Infection
    HIV-1 inhibitor-15 (compound 9d) is a highly potent and broad-spectrum HIV-1 inhibitor. HIV-1 inhibitor-15 has inhibitory activity against HIV-1 WT, L100I, K103N, Y181C, E138K with EC50s of 1.7 nM, 4 nM, 2 nM, 6 nM and 9 nM, respectively. HIV-1 inhibitor-15 has good solubility, safety profiles and favorable oral bioavailability.
  • HY-13017
    Ivacaftor

    VX-770

    		 CFTR Autophagy Endocrinology
    Ivacaftor (VX-770) is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively.
  • HY-100626
    WNK463

    		Ser/Thr Protease Cancer
    WNK463 is an orally bioavailable pan-With-No-Lysine (K) (WNK)-kinase inhibitor with IC50s of 5 nM, 1 nM, 6 nM, and 9 nM for WNK1, WNK2, WNK3, and WNK4, respectively.
  • HY-100080
    A-887826

    		Sodium Channel Neurological Disease
    A-887826 is a potent, selective, oral bioavailable and voltage-dependent Na(v)1.8 sodium channel blocker with an IC50 of 11 nM . A-887826 attenuates neuropathic tactile allodynia in vivo.
  • HY-133772
    Venetoclax N-oxide

    		Drug Metabolite Others
    Venetoclax N-oxide is an impurity of Venetoclax. 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.
  • HY-10900
    TCS 1102

    		Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    TCS 1102 is a potent, dual orexin receptor antagonist, with Ki values of 0.2 nM and 3 nM for OX2 and OX1 receptors, respectively. TCS 1102 demonstrates excellent brain peneration and moderate bioavailability in rats.
  • HY-117900A
    (Rac)-PF-06250112

    		Btk Inflammation/Immunology
    (Rac)-PF-0625011 is a racemate of PF-06250112. PF-06250112 is a potent, highly selective, orally bioavailable BTK inhibitor and shows inhibitory effect toward BMX nonreceptor tyrosine kinase and TEC.
  • HY-18938
    Selonsertib

    GS-4997

    		 MAP3K Apoptosis Cancer
    Selonsertib (GS-4997), an orally bioavailable, selective apoptosis signal-regulating kinase 1 (ASK1) inhibitor with a pIC50 of 8.3, has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis.
  • HY-19558
    IDX184

    		HCV HCV Protease Infection
    IDX184 is a potent and orally bioavailable inhibitor of HCV replication. IDX184 potently inhibits HCV polymerase (IC50=0.31 μM, Ki=52.3 nM).
  • HY-A0203
    Pentosan Polysulfate

    		HIV Infection Inflammation/Immunology
    Pentosan Polysulfate is an orally bioavailable medication with anti-inflammatory and pro-chondrogenic properties. Pentosan Polysulfate also displays a potent and selective anti-HIV activity. Pentosan Polysulfatecan be used for the research of interstitial cystitis.
  • HY-15315S
    Baricitinib-d5

    LY3009104-d5; INCB028050-d5

    		 JAK Inflammation/Immunology
    Baricitinib-d5 is the deuterium labeled Baricitinib. 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-15315S1
    Baricitinib-d3

    LY3009104-d3; INCB028050-d3

    		 JAK Inflammation/Immunology
    Baricitinib-d3 is the deuterium labeled Baricitinib. 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-15463S1
    Imatinib D4

    STI571 d4; CGP-57148B d4

    		 Bcr-Abl PDGFR c-Kit SARS-CoV Autophagy Cancer
    Imatinib-d4 is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity[1][2].
  • HY-136146
    SUVN-911

    		nAChR Neurological Disease
    SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a Ki of 1.5 nM. SUVN-911 has antidepressant activity.
  • HY-108472
    Loxoribine

    7-Allyl-8-oxoguanosine; RWJ 21757

    		 Toll-like Receptor (TLR) Influenza Virus Cancer Infection
    Loxoribine (7-Allyl-8-oxoguanosine) is a guanosine analog with anti-viral and anti-tumor activities. Loxoribine is an orally bioavailable and selective Toll-like receptor (TLR) 7 agonist.
  • HY-141866
    Acid Ceramidase-IN-1

    		Others Neurological Disease
    Acid Ceramidase-IN-1 is a potent and oral bioavailable acid ceramidase (AC, ASAH-1) inhibitor (hAC IC50=0.166 μM). Acid Ceramidase-IN-1 has excellent brain penetration in mice.
  • HY-120634
    BMS-929075

    		HCV Infection
    BMS-929075 is a potent and orally active HCV NS5B replicase palm site allosteric inhibitor. BMS-929075 shows high oral bioavailability. BMS-929075 shows cytotoxicity.
  • HY-15463S
    Imatinib-d8

    STI571-d8; CGP-57148B-d8

    		 Bcr-Abl PDGFR c-Kit SARS-CoV Autophagy Cancer
    Imatinib-d8 is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity[1][2].
  • HY-10038
    A 922500

    DGAT-1 Inhibitor 4a

    		 Acyltransferase Metabolic Disease
    A 922500 (DGAT-1 Inhibitor 4a) is a potent, selective, and orally bioavailable diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC50s of 9 and 22 nM against human and mouse DGAT-1, respectively.
  • HY-N0269
    Echinatin

    		Others Inflammation/Immunology
    Echinatin is a chalcone isolated from the Chinese herbal medicine Gancao with hepatoprotective and anti-inflammatory effects. Echinatin can be quickly absorbed and eliminated and extensively distributed with an absolute bioavailability of approximately 6.81% in Rat.
  • 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-115996
    Antitumor agent-51

    		Others Cancer
    Antitumor agent-51 possesses potent and selective inhibitory for osteosarcoma cell growth and migration with IC50 of 21.9 nM in MNNG/HOS cells. Antitumor agent-51 has a considerable bioavailability and a low toxicity.
  • HY-112287
    ERK1/2 inhibitor 1

    		ERK Cancer
    ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC50 of 3.0 nM against ERK1 and ERK2, respectively.
  • HY-146075
    β-Lactamase-IN-8

    		Bacterial Infection
    β-Lactamase-IN-8 (compound 20) is a potent and oral bioavailable broad-spectrum cyclic boronate β-lactamase inhibitor. β-Lactamase-IN-8 can be used for researching antibacteria.
  • HY-117853
    Atreleuton

    ABT-761; VIA-2291

    		 Lipoxygenase Cardiovascular Disease
    Atreleuton (ABT-761) is a selective, reversible, and orally bioavailable 5-Lipoxygenase (5-LO) inhibitor. Atreleuton (ABT-761) exhibits potent and selective inhibition of leukotriene formation.
  • HY-111457A
    BAY-678

    		Elastase Inflammation/Immunology
    BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).
  • HY-101930
    BMS-816336

    		11β-HSD Metabolic Disease
    BMS-816336 is a novel, potent and orally bioavailable inhibitor against human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with an IC50 of 3.0 nM.
  • HY-15874A
    Fiboflapon sodium

    GSK2190915 sodium salt; AM-803 sodium

    		 FLAP Leukotriene Receptor Inflammation/Immunology
    Fiboflapon sodium (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.
  • HY-144372
    TRPV1 antagonist 3

    		TRP Channel Neurological Disease
    TRPV1 antagonist 3 (Compound 7q) is a potent TRPV1 antagonist with an IC50 of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant.
  • HY-15450A
    INCB 3284

    		CCR Endocrinology
    INCB 3284 is a potent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM. INCB 3284 can be used in the research of acute liver failure.
  • HY-147528
    mGluR2 modulator 2

    		mGluR Neurological Disease
    mGluR2 modulator 2 (compound 2) is a potent, selective and orally bioavailable mGluR2 positive allosteric modulator with an EC50 value of 0.13 μM. mGluR2 modulator 2 can be used for researching antipsychotic.
  • HY-A0203A
    Pentosan Polysulfate Sodium (W/W 43%)

    		HIV Infection Inflammation/Immunology
    Pentosan Polysulfate Sodium is an orally bioavailable, semi-synthetic medication with anti-inflammatory and pro-chondrogenic properties. Pentosan Polysulfate Sodium also is a potent and selective anti-HIV agent. Pentosan Polysulfate Sodium is used for the treatment of interstitial cystitis.
  • HY-110176
    ASP2535

    		GlyT Neurological Disease
    ASP2535 is a potent, orally bioavailable, selective, brain permeable and centrally-active glycine transporter-1 (GlyT1) inhibitor. ASP2535 can improve cognitive impairment in animal models of schizophrenia and Alzheimer's disease.
  • HY-P0025
    NIM811

    (Melle-4)cyclosporin; SDZ NIM811

    		 Mitochondrial Metabolism HCV Infection Inflammation/Immunology
    NIM811 ((Melle-4)cyclosporin; SDZ NIM811) is an orally bioavailable mitochondrial permeability transition and cyclophilin dual inhibitor, which exhibits potent in vitro activity against hepatitis C virus (HCV) .
  • HY-19981
    Derazantinib

    ARQ-087

    		 FGFR Cancer
    Derazantinib (ARQ-087) is an orally bioavailable, ATP competitive tyrosine kinase inhibitor; exhibits potent activity against FGFR1-3 chondrocytes with IC50s of 4.5, 1.8, and 4.5 nM, respectively.
  • HY-14291
    Vildagliptin

    LAF237; NVP-LAF 237

    		 Dipeptidyl Peptidase Ferroptosis Apoptosis Metabolic Disease
    Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity.
  • HY-131336
    MGS0274

    		mGluR Neurological Disease
    MGS0274, an ester-based lipophilic proagent 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-120469
    2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide

    		JAK Inflammation/Immunology
    GDC-046 is a potent, selective, and orally bioavailable TYK2 inhibitor with Kis of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively.
  • HY-19327
    ACY-738

    		HDAC Cancer
    ACY-738 is a potent, selective and orally-bioavailable HDAC6 inhibitor, with an IC50 of 1.7 nM; ACY-738 also inhibits HDAC1, HDAC2, and HDAC3, with IC50s of 94, 128, and 218 nM.
  • HY-15445
    CTEP

    RO 4956371; mGluR5 inhibitor

    		 mGluR Neurological Disease
    CTEP (RO 4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, and shows > 1000-fold selectivity over other mGlu receptors.
  • HY-10290
    MK-0674

    		Cathepsin Metabolic Disease
    MK-0674 is a potent, orally bioavailable and selective cathepsin K inhibitor, with an IC50 of 0.4 nM, shows 1156, 1465, 11857 and 243 fold selectivity over Cat B, Cat F, Cat L and Cat S.
  • HY-102031
    Linperlisib

    YY-20394

    		 PI3K Cancer Inflammation/Immunology
    Linperlisib (YY-20394) is a potent, orally bioavailable and selective inhibitor of PI3Kδ extracted from patent WO 2015055071 A1, compound 10; has an IC50 of 6.4 nM.
  • HY-15874
    Fiboflapon

    GSK2190915; AM-803

    		 FLAP Leukotriene Receptor Inflammation/Immunology
    Fiboflapon (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.
  • HY-15976
    P7C3

    		Others Neurological Disease
    P7C3 is an orally bioavailable and blood-brain barrier penetrant aminopropyl carbazole, with neuroprotective effects. P7C3 can be used for the research of neurodegenerative diseases, including Parkinson's disease.
  • HY-100761
    SS28

    		Microtubule/Tubulin Apoptosis Cancer
    SS28, a SRT501 analog with oral bioavailability, inhibits tubulin polymerization to cause cell cycle arrest at G2/M phase. SS28 results in apoptosis rather than necrosis tubulin.
  • HY-12938
    AMG-8718

    		Beta-secretase Neurological Disease
    AMG-8718 is a potent, selective and orally active BACE1 inhibitor with IC50 values of 0.0007, 0.005 µM for BACE1 and BACE2, respectively. AMG-8718 significantly decreases Aβ40 levels in the CSF and brain.
  • HY-151903S
    FGFR2/3-IN-1

    		FGFR Cancer
    FGFR2/3-IN-1 is a potent and selective FGFR2 and FGFR3 (FGFR) inhibitor with IC50s of 1 nM and 0.5 nM, respectively. FGFR2/3-IN-1 displays >40-fold selectivity over FGFR1/FGFR4 and other kinome. FGFR2/3-IN-1 also inhibits FGFR3 V555L and V555M mutants with IC50s of 2.7 nM and 6.1 nM, respectively[1].
  • HY-144285
    CXCR4 antagonist 4

    		CXCR HIV Inflammation/Immunology
    CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM).
  • HY-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-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-123039
    CP-532623

    		CETP Metabolic Disease
    CP-532623 is a CETP inhibitor and elevates high-density lipoprotein cholesterolion. CP-532623 is a close structural analogue of Torcetrapib. CP-532623 has highly lipophilic properties.
  • HY-133149
    Lp-PLA2-IN-3

    		Phospholipase Cardiovascular Disease
    Lp-PLA2-IN-3 is a potent and orally bioavailable lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 of 14 nM for recombinant human Lp-PLA2 (rhLpPLA2).
  • HY-134885
    RMC-0331

    RM-023

    		 SHP2 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-111427
    CDK8/19-IN-1

    		CDK Cancer
    CDK8/19-IN-1 is a potent, selective and oral bioavailable CDK8/19 dual inhibitor, with IC50s of 0.46 nM, 0.99 nM and 270 nM for CDK8, CDK19 and CDK9, respectively.
  • HY-12947
    GNE-3511

    		MAP3K Neurological Disease
    GNE-3511 is an orally active bioavailable and brain-penetrant dual leucine zipper kinase (DLK) inhibitor with a Ki of 0.5 nM. GNE-3511 can cross the blood-brain-barrier and can be used for the research of neurodegenerative diseases.
  • HY-107981
    LSN 3213128

    		Antifolate Cancer
    LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT), with IC50 of 16 nM for AICARFT enzyme inhibiton and 19 nM in cells. Anti-tumor activity.
  • HY-12681
    CCT251545

    		Wnt Cancer
    CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with an IC50 of 5 nM in 7dF3 cells. CCT251545 is a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
  • HY-15980
    GNF179 (Metabolite)

    		Parasite Infection
    GNF179 metabolite is the metabolite of GNF179, which is an optimized 8,8-dimethyl IP analog that exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability.
  • HY-128596
    ALK-IN-6

    		Anaplastic lymphoma kinase (ALK) Cancer
    ALK-IN-6 (compound 11) is an orally bioavailable inhibitor of anaplastic lymphoma kinase (ALK), with IC50 values of 71 nM, 18.72 nM and 36.81 nM for ALK wild, ALK F1196M and ALK F1174L, respectively.
  • HY-124603
    AT791

    		Toll-like Receptor (TLR) Inflammation/Immunology
    AT791 is a potent and orally bioavailable TLR7 and TLR9 inhibitor. AT791 inhibits TLR7 and 9 signaling in a variety of human and mouse cell types and inhibits DNA-TLR9 interaction in vitro.
  • HY-10222
    Ixabepilone

    BMS-247550; Aza-epothilone B

    		 Microtubule/Tubulin Apoptosis Bacterial Cancer
    Ixabepilone (BMS-247550) is an orally bioavailable microtubule inhibitor, which binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arrests cells in the G2-M phase of the cell cycle and induces tumor cell apoptosis.
  • HY-B1486S
    Oxprenolol-d7 hydrochloride

    Ba 39089-d7

    		 Adrenergic Receptor Cardiovascular Disease
    Oxprenolol-d7 (hydrochloride) is the deuterium labeled Oxprenolol hydrochloride. Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle[1].
  • HY-Y0319G
    Acetic acid magnesium tetrahydrate

    		Endogenous Metabolite Bacterial Cancer
    Acetic acid magnesium tetrahydrate is a hydrated form of anhydrous magnesium acetate salt. As a salt form of Magnesium, Magnesium acetate is one of the bioavailable forms of magnesium and forms a very water soluble compound. Acetic acid magnesium tetrahydrate can be used as an electrolyte supplementation or a reagent in molecular biology experiments.
  • HY-19981A
    Derazantinib Racemate

    ARQ-087 Racemate

    		 FGFR Cancer
    Derazantinib Racemate (ARQ-087 Racemate) is the racemate of Derazantinib. Derazantinib is an orally bioavailable, ATP competitive tyrosine kinase inhibitor; exhibits potent activity against FGFR1-3 chondrocytes with IC50s of 4.5, 1.8, and 4.5 nM, respectively.
  • HY-107457
    AZD-8529

    		mGluR Neurological Disease
    AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
  • HY-12861
    CB-5083

    		p97 Cancer
    CB-5083 is a first-in-class, potent, selective, and orally bioavailable inhibitor of the p97 AAA ATPase/VCP. CB-5083 selectively inhibits p97 through its D2 site with the IC50 of 11 nM。
  • HY-108060A
    Valopicitabine dihydrochloride

    NM283 dihydrochloride

    		 HCV HCV Protease Nucleoside Antimetabolite/Analog Infection
    Valopicitabine (NM283) dihydrochloride is a nucleoside analog and the orally bioavailable proagent of the potent anti-HCV agent 2'-C-methylcytidine (NM107). NM107competitively inhibits NS5B polymerase, causing chain termination.
  • HY-19614
    BMS-795311

    		CETP Cardiovascular Disease
    BMS-795311 is a potent and orally bioavailable inhibitor of cholesteryl ester transfer protein (CETP), with IC50s of 4 nM in an enzyme-based scintillation proximity assay (SPA) and 0.22 μM in a human whole plasma assay (hWPA), respectively.
  • HY-N0447
    8-Gingerol

    		TRP Channel Bacterial Infection Inflammation/Immunology Cancer
    8-Gingerol, found in the rhizomes of ginger (Z. officinale) with oral bioavailability, activates TRPV1, with an EC50 of 5.0 µM. 8-Gingerol inhibits COX-2, and inhibits the growth of H. pylori in vitro.
  • HY-108060
    Valopicitabine

    NM283

    		 HCV HCV Protease Nucleoside Antimetabolite/Analog Infection
    Valopicitabine (NM283) is a nucleoside analog and the orally bioavailable proagent of the potent anti-HCV agent 2'-C-methylcytidine (NM107). NM107competitively inhibits NS5B polymerase, causing chain termination.
  • HY-119339
    SX-682

    		CXCR Cancer Inflammation/Immunology Endocrinology
    SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2. SX-682 can block tumor myeloid-derived suppressor cells (MDSCs) recruitment and enhance T cell activation and antitumor immunity.
  • HY-50674
    INCB3344

    		CCR Inflammation/Immunology Endocrinology
    INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
  • HY-15450
    INCB 3284 dimesylate

    		CCR Endocrinology
    INCB 3284 dimesylate is a potent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM. INCB 3284 dimesylate can be used in the research of acute liver failure.
  • HY-100279
    RMI 10874

    		Antibiotic Cancer Infection
    RMI 10874 is a tilorone analogue. Tilorone is a small-molecule, orally bioavailable antiviral agent. RMI 10874 completely abolishes lung colonization of an H-2 negative (GR9.B9) MCA-induced fibrosarcoma clone.
  • HY-117900
    PF-06250112

    		Btk Inflammation/Immunology
    PF-06250112 is a potent, highly selective, orally bioavailable BTK inhibitor with an IC50 of 0.5 nM, shows inhibitory effect toward BMX nonreceptor tyrosine kinase and TEC with IC50s of 0.9 nM and 1.2 nM, respectively.
  • HY-B1486AS
    Oxprenolol-d7

    		Adrenergic Receptor
    Oxprenolol-d7 is the deuterium labeled Oxprenolol. Oxprenolol (Ba 39089 free base) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle[1].
  • HY-117650A
    RG7834

    RO 7020322

    		 HBV Infection
    RG7834 (RO 7020322) is a highly selective and orally bioavailable HBV inhibitor, potently inhibits HBV antigens (both HBsAg and HBeAg) and HBV DNA, with IC50s of 2.8, 2.6, and 3.2 nM, respectively, in dHepaRG Cells.
  • HY-148290
    KTX-951

    		PROTACs IRAK Cancer
    KTX-951 is a PROTAC targeting IRAK4 degradation (DC50=18 nM). KTX-951 (10 mg/kg) shows the oral bioavailability (F%) of 22% in a rat model. KTX-951 has good anticancer potential.
  • HY-15590
    AZ-23

    AZ23; AZ 23

    		 Trk Receptor Cancer
    AZ-23 is an ATP-competitive and orally bioavailable Trk kinase A/B/C inhibitor with IC50s of 2 nM (TrkA), 8 nM (TrkB), 24 nM (FGFR1), 52 nM (Flt3), 55 nM (Ret), 84 nM (MuSk), 99 nM (Lck), respectively.
  • HY-14291A
    Vildagliptin dihydrate

    LAF237 dihydrate; NVP-LAF 237 dihydrate

    		 Dipeptidyl Peptidase Ferroptosis Apoptosis Metabolic Disease
    Vildagliptin dihydrate (LAF237 dihydrate) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin dihydrate possesses excellent oral bioavailability and potent antihyperglycemic activity.
  • HY-13318S
    Oseltamivir acid-d3

    GS 4071-d3; Ro 64-0802-d3; Oseltamivir carboxylate-d3

    		 Influenza Virus Infection
    Oseltamivir acid-d3 is a deuterium labeled Oseltamivir acid. Oseltamivir acid, the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC50=2 nM) with activity against both influenza A and B viruses[1][2].
  • HY-14364
    A-987306

    		Histamine Receptor Inflammation/Immunology
    A-987306 is a potent and oral bioavailable histamine H4 antagonist, with Kis of 3.4 nM and 5.8 nM for rat H4, and human H4. A-987306 shows anti-inflammatory activity in mice peritonitis model.
  • HY-131964
    Imidacloprid-urea

    		Drug Metabolite Others
    Imidacloprid-urea is a metabolite of Imidacloprid. Imidacloprid is an effective and widely used neonicotinoid pesticide to control pests of cereals, vegetables, tea and cotton. Imidacloprid-urea can occupy or block adsorption sites of imidacloprid on soil, potentially affecting the fate, transport, and bioavailability of imidacloprid in the environment.
  • HY-17374
    Benfotiamine

    S-Benzoylthiamine O-monophosphate

    		 Others Neurological Disease
    Benfotiamine (S-Benzoylthiamine O-monophosphate) is an analog of vitamin B1 with higher absorption and bioavailability than vitamin B1, and is commonly used as a food supplement for diabetic complications. Benfotiamine exhibits direct antioxidative capacity and prevents induction of DNA damage.
  • HY-129393
    Etrumadenant

    AB928

    		 Adenosine Receptor Inflammation/Immunology Cancer
    Etrumadenant (AB928) is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. Etrumadenant relieves adenosine-mediated immune suppression. Etrumadenant has immunomodulatory and antitumor activities.
  • HY-117604
    THPP-1

    		Phosphodiesterase (PDE) Neurological Disease
    THPP-1, a SGC chemical probe, is a potent and orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 1 nM and 1.3 nM for human and rat PDE10A, respectively. THPP-1 has excellent pharmacokinetic properties in preclinical species.
  • HY-15185
    Nirogacestat

    PF-3084014; PF-03084014

    		 γ-secretase Apoptosis Cancer
    Nirogacestat (PF-3084014) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC50 of 6.2 nM. Inhibition of Notch signaling by Nirogacestat while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers.
  • HY-100678
    CGS 15943

    		Adenosine Receptor PI3K Cancer Inflammation/Immunology
    CGS 15943 is an orally bioavailable non-xanthine Adenosine Receptor antagonist. Its Ki for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM in transfected CHO cells, respectively. .
  • HY-105296
    Blarcamesine

    Anavex 2-73 free base

    		 Sigma Receptor mAChR Cancer
    Blarcamesine (Anavex 2-73 free base) is an orally bioavailable Sigma-1 receptor agonist and muscarinic receptor modulator, with anticonvulsant, anti-amnesic, neuroprotective and antidepressant properties. Blarcamesine ameliorates neurologic impairments in a mouse model of Rett syndrome.
  • HY-148565
    SERT-IN-2

    		Serotonin Transporter Neurological Disease
    SERT-IN-2 is a potent SERT inhibitor (IC50=0.58 nM) with promising anti-depression efficacy. SERT-IN-2 shows good bioavailability of 83.28% in rats. SERT-IN-2 can cross the blood-brain barrier.
  • HY-15531S
    Venetoclax-d8

    ABT-199-d8; GDC-0199-d8; RG7601-d8

    		 Bcl-2 Family Autophagy Cancer
    Venetoclax-d8 is deuterium labeled Venetoclax. 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[1][2][3].
  • HY-15727
    Afuresertib

    GSK2110183

    		 Akt PKC ROCK Cancer
    Afuresertib (GSK2110183) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3, respectively.
  • HY-15727A
    Afuresertib hydrochloride

    GSK2110183 hydrochloride

    		 Akt PKC ROCK Cancer
    Afuresertib hydrochloride (GSK 2110183 hydrochloride) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively.
  • HY-15532
    SCH900776

    MK-8776

    		 Checkpoint Kinase (Chk) Cancer
    SCH900776 (MK-8776) is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with an IC50 of 3 nM. SCH900776 shows 50- and 500-fold selectivity over CDK2 and Chk2, respectively.
  • HY-107457A
    AZD-8529 mesylate

    		mGluR Neurological Disease
    AZD-8529 mesylate is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
  • HY-145341
    GNE-149

    		Estrogen Receptor/ERR Cancer
    GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC50=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer.
  • HY-15546
    BMS-817399

    		CCR Inflammation/Immunology
    BMS-817399 is a potent, selective, and orally bioavailable CCR1 antagonist. BMS-817399 exhibits CCR1 binding affinity and chemotaxis inhibition potencies of 1 and 6 nM (IC50), respectively. BMS-817399 can be used for the research of rheumatoid arthritis.
  • HY-109015S
    Tucidinostat-d4

    Chidamide-d4; HBI-8000-d4; CS 055-d4

    		 HDAC Cancer
    Tucidinostat-d4 is the deuterium labeled Tucidinostat. Tucidinostat is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, respectively[1].
  • HY-100226
    A-205804

    		Integrin Inflammation/Immunology
    A-205804 is an orally bioavailable, potent and selective lead inhibitor of E-selectin and ICAM-1 expression, with an IC50 of 20 nM and 25 nM for E-selectin and ICAM-1, respectively. A-205804 can be used in the research of chronic inflammatory diseases.
  • HY-141623
    SRI-37330 hydrochloride

    		Others Metabolic Disease
    SRI-37330 hydrochloride is an orally bioavailable thioredoxin-interacting protein (TXNIP) inhibitor. SRI-37330 hydrochloride inhibits glucagon secretion and function, reduces hepatic glucose production and reverses hepatic steatosis. SRI-37330 hydrochloride can be used for type 2 diabetes research.
  • HY-108677
    L-368,899 hydrochloride

    		Oxytocin Receptor Endocrinology
    L-368,899 hydrochloride is a potent, selective, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC50s of 8.9 nM and 26 nM for rat uterus and human uterus oxytocin receptor, respectively. L-368,899 hydrochloride used as a tocolytic agent.
  • HY-128353
    ROR agonist-1

    		ROR Inflammation/Immunology
    ROR agonist-1 is a potent and orally bioavailable inverse agonist of the retinoic acid receptor-related orphan receptor C2 (RORC2), inhibition of IL-17A production from human primary TH 17 cells with a pIC50 of 7.5.
  • HY-145564
    Emprumapimod

    PF-07265803

    		 p38 MAPK Inflammation/Immunology Cardiovascular Disease
    Emprumapimod (PF-07265803) is a potent, orally active and selective inhibitor of p38α MAPK directly inhibits LPS-induced IL-6 production from RPMI-8226 cell (IC50=100 pM). Emprumapimod can be used for the research of dilated cardiomyopathy and acute inflammatory pain.
  • HY-145564A
    Emprumapimod hydrochloride

    PF-07265803 hydrochloride

    		 p38 MAPK Inflammation/Immunology Cardiovascular Disease
    Emprumapimod (PF-07265803) hydrochloride is an orally active and selective inhibitor of p38α MAPK. Emprumapimod hydrochloride can be used for the research of dilated cardiomyopathy and acute inflammatory pain.
  • 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-142772
    Y08284

    		Epigenetic Reader Domain Cancer
    Y08284 is a potent, selective, oral active CBP bromodomain inhibitor with an IC50 of 4.21 nM. Y08284 suppresses the proliferation of prostate cancer cell lines LNCaP, C4-2B, and 22Rv1. Antitumor activity.
  • HY-13213
    AM211

    AM211 free acid

    		 Prostaglandin Receptor Inflammation/Immunology Endocrinology
    AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC50s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively.
  • HY-13026
    Idelalisib

    CAL-101; GS-1101

    		 PI3K Autophagy Cancer
    Idelalisib (CAL-101; GS-1101) is a highly selective and orally bioavailable p110δ inhibitor with an IC50 of 2.5 nM, showing 40- to 300-fold selectivity for p110δ over other PI3K class I enzymes.
  • 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-127105A
    Iptacopan hydrochloride

    LNP023 hydrochloride

    		 Complement System Metabolic Disease Inflammation/Immunology
    LNP023 hydrochloride is an orally bioavailable, highly potent and highly selective factor B inhibitor. LNP023 shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. LNP023 inhibits factor B with an IC50 value of 10 nM.
  • HY-14560A
    (R,R)-Reboxetine mesylate

    (R,R)-FCE20124 mesylate; (R,R)-PNU155950E mesylate

    		 Adrenergic Receptor mAChR Neurological Disease
    (R,R)-Reboxetine mesylate is an antidepressant agent with great bioavailability. (R,R)-Reboxetine is the enantiomer of Reboxetine, which is a selective noradrenaline reuptake inhibitor. Reboxetine consists of (R,R) and (S,S) enantiomer, has low affinity for alpha-adrenergic and muscarinic receptors and low toxicity in animals.
  • HY-132987
    Avibactam tomilopil

    ARX-1796; AV-006

    		 Bacterial Infection
    Avibactam tomilopil (ARX-1796, AV-006), an Avibactam proagent, is an orally bioavailable β-lactamase inhibitor. Avibactam has a spectrum of inhibition of class A and C β-lactamases, including ESBLs, AmpC and Klebsiella pneumoniae carbapenemase (KPC) enzymes.
  • HY-120062
    TVB-3664

    		Fatty Acid Synthase (FASN) Cancer
    TVB-3664 is an orally available, reversible, potent, selective and highly bioavailable fatty acid synthase (FASN) inhibitor, with IC50 values of 18 nM and 12 nM for human and mouse cell palmitate synthesis, respectively. TVB-3664 significantly reduces tubulin palmitoylation and mRNA expression.
  • HY-13323A
    CX-5461 dihydrochloride

    		DNA/RNA Synthesis Cancer
    CX-5461 dihydrochloride is a potent and orally bioavailable inhibitor of Pol I-mediated rRNA synthesis, with IC50s of 142 nM in HCT-116, 113 nM in A375, and 54 nM in MIA PaCa-2 cells, and shows little or no effect on Pol II (IC50 ≥25 μM).
  • HY-111515
    BAY-678 racemate

    		Elastase Inflammation/Immunology
    BAY-678 racemate is a racemate of BAY-678. BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).
  • HY-145928
    Divarasib

    GDC-6036

    		 Ras Cancer
    Divarasib (GDC-6036) is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state.
  • HY-50682
    Azeliragon

    TTP488; PF-04494700

    		 Amyloid-β Neurological Disease
    Azeliragon (TTP488) is an orally bioavailable inhibitor of the receptor for advanced glycation end products (RAGE) in development as a potential treatment to slow disease progression in patients with mild Alzheimer’s disease (AD). Azeliragon also can cross the blood-brain barrier (BBB).
  • HY-109587B
    BM635 mesylate

    		Bacterial Infection
    BM635 mesylate is a MmpL3 inhibitor with outstanding anti-mycobacterial activity. BM635 mesylate has a MIC50 of 0.6 μM against M. tuberculosis  H37Rv. BM635 mesylate significantly improves the bioavailability compared to free-base BM635.
  • HY-119375
    Syncytial Virus Inhibitor-1

    		Bacterial Infection
    Syncytial Virus Inhibitor-1 is a potent, orally bioavailable respiratory syncytial virus (RSV) fusion inhibitor with EC50s of 0.002 μM, 0.004 μM, and 0.002 μM for RSV Long, RSV A2, and RSV B strains, respectively.
  • HY-15419
    RS-127445 hydrochloride

    		5-HT Receptor Neurological Disease
    RS-127445 hydrochloride is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 hydrochloride shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.
  • HY-128775
    JHU395

    		Others Cancer
    JHU395 is an orally-bioavailable and a plasma stable lipophilic glutamine antagonists (GA) proagent. JHU395 delivers 6-diazo-5-oxo-L-norleucine (DON) to malignant peripheral nerve sheath tumor (MPNST) in vitro and in vivo, and has antitumor activity in MPNST.
  • HY-14434
    Asunaprevir

    BMS-650032

    		 HCV HCV Protease SARS-CoV Infection
    Asunaprevir (BMS-650032) is a potent and orally bioavailable hepatitis C virus (HCV) NS3 protease inhibitor, with IC50 of 0.2 nM-3.5 nM. Asunaprevir inhibits SARS-CoV-2 3CL pro activity.
  • HY-14291S1
    Vildagliptin-d7

    LAF237-d7; NVP-LAF 237-d7

    		 Dipeptidyl Peptidase Ferroptosis Apoptosis Metabolic Disease
    Vildagliptin-d7 is deuterium labeled Vildagliptin. Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity[1].
  • HY-14567
    Ciproxifan

    FUB-359

    		 Histamine Receptor Neurological Disease Endocrinology
    Ciproxifan (FUB 359) is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan displays low apparent affinity at other receptor subtypes. Ciproxifan can be used for the research of aging disorders and Alzheimer's disease.
  • HY-10917
    GW2580

    		c-Fms Inflammation/Immunology Cancer
    GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling.
  • HY-145119S
    GS-621763-d1

    		Isotope-Labeled Compounds Others
    GS-621763-d1 is the deuterium labeled GS-621763 (HY-145119). GS-621763, an orally bioavailable proagent of GS-441524, shows antiviral activity against SARS-CoV-2 pathogenesis in mice.
  • HY-15185B
    Nirogacestat dihydrobromide

    PF-3084014 dihydrobromide; PF-03084014 dihydrobromide

    		 γ-secretase Apoptosis Cancer
    Nirogacestat dihydrobromide (PF-3084014 dihydrobromide) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC50 of 6.2 nM. Inhibition of Notch signaling by Nirogacestat dihydrobromide while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers.
  • HY-15419A
    RS-127445

    		5-HT Receptor Neurological Disease
    RS-127445 is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.
  • HY-105309
    GSK-626616

    		DYRK Cardiovascular Disease
    GSK-626616 is a potent, orally bioavailable inhibitor of DYRK3 (IC50=0.7 nM). GSK-626616 inhibits other members of the DYRK family (e.g., DYRK1A and DYRK2) with similar potency, which is a potential therapy for the treatment of anemia.
  • HY-15289
    Ciproxifan maleate

    FUB 359 maleate

    		 Histamine Receptor Neurological Disease Endocrinology
    Ciproxifan maleate (FUB 359 maleate) is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan maleate displays low apparent affinity at other receptor subtypes. Ciproxifan maleate can be used for the research of aging disorders and Alzheimer's disease.
  • HY-16976
    GDC-0339

    		Pim Cancer
    GDC-0339 is a potent, orally bioavailable and well tolerated pan-Pim kinase inhibitor, with Kis of 0.03 nM, 0.1 nM and 0.02 nM for Pim1, Pim2 and Pim3, respectively. GDC-0339 is discovered as a potential treatment of multiple myeloma.
  • HY-15245
    GSK2636771

    		PI3K Cancer
    GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with a Ki of 0.89 nM and an IC50 of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.
  • HY-128781
    Glucagon receptor antagonists-5

    		GCGR Metabolic Disease
    Glucagon receptor antagonists-5 (compound 13K) is a potent and orally bioavailable indazole-based glucagon receptor antagonist (Ki=32 nM). Glucagon receptor antagonists-5 has potential for the treatment of type 2 diabetes mellitus (T2DM).
  • HY-14291S
    Vildagliptin-d3

    LAF237-d3; NVP-LAF 237-d3

    		 Dipeptidyl Peptidase Ferroptosis Apoptosis Metabolic Disease
    Vildagliptin-d3 is the deuterium labeled Vildagliptin. Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity[1][2].
  • HY-144858
    EZM0414

    		Histone Methyltransferase Cancer
    EZM0414 is a potent, selective, orally bioavailable inhibitor of SETD2 (IC50=18 nM in SETD2 biochemical assay; IC50=34 nM in cellular assay). EZM0414 can be used for the research of relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma.
  • HY-119272
    EF24

    		ERK Caspase Cancer
    EF24 is a curcumin analogue with greater anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK.
  • HY-13017S2
    Ivacaftor-d18

    VX-770-d18

    		 Autophagy CFTR Endocrinology
    Ivacaftor-d18 is the deuterium labeled Ivacaftor[1]. Ivacaftor (VX-770) is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively[2].
  • HY-101111
    PF-06840003

    EOS200271

    		 Indoleamine 2,3-Dioxygenase (IDO) Cancer
    PF-06840003 (EOS200271) is a highly selective orally bioavailable IDO-1 inhibitor with IC50s of 0.41 μM, 0.59 μM, and 1.5 μM for hIDO-1, dIDO-1, and mIDO-1, respectively.
  • HY-103696
    PTC-028

    		Apoptosis Cancer
    PTC-028 is an orally bioavailable inhibitor of stem cell factor BMI-1 in ovarian cancer. PTC-028 selectively inhibits cancer cells whereas normal cells remain unaffected. PTC-028 downregulates BMI-1, inducing caspase-mediated apoptosis.
  • HY-145844
    EGFR-IN-44

    		EGFR Apoptosis Cancer
    EGFR-IN-44 (Compound 6a) is a potent, orally active EGFR tyrosine kinase inhibitor with an IC50 of 4.11 nM. EGFR-IN-44 induces cell apoptosis and shows an oral bioavailability value of 33.57%. EGFR-IN-44 can be studied for non-small-cell lung cancers.
  • HY-139970
    VPC-13789

    		Androgen Receptor Cancer Endocrinology
    VPC-13789 is a potent, selective, and orally bioavailable antiandrogen. VPC-13789 can be used for the research of castration-resistant prostate cancer (CRPC) therapeutics. VPC-13789 inhibits androgen receptor (AR) transcriptional activity in LNCaP cells (IC50=0.19 μM).
  • HY-16434
    DGAT1-IN-3

    		Acyltransferase Metabolic Disease
    DGAT1-IN-3 is a potent, selective and orally bioavailable inhibitor of DGAT-1, with IC50s of 38 nM for human DGAT-1 and 120 nM for rat DGAT-1. DGAT1-IN-3 could be used to research of obesity, dyslipidemia, and metabolic syndrome.
  • HY-124283A
    LEI-101

    		Cannabinoid Receptor Neurological Disease
    LEI-101 is a potent, selective, and orally bioavailable cannabinoid CB2 receptor agonist, with a pEC50 of 8 for hCB2, and a pKi of less than 4 for hERG. LEI-101 is ~100-fold more potent in binding to CB2 receptors than to CB1 receptors.
  • HY-18030A
    CEP-28122 mesylate salt

    		Anaplastic lymphoma kinase (ALK) Cancer
    CEP-28122 mesylate salt, a diaminopyrimidine derivative, is a potent, selective, and orally bioavailable ALK inhibitor, with an IC50 value of 1.9 nM for recombinant ALK kinase activity. CEP-28122 has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 mesylate salt has good pharmacodynamic and pharmacokinetic activity.
  • HY-112151A
    EG01377 dihydrochloride

    		Complement System Cancer
    EG01377 dihydrochloride is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1), with a Kd of 1.32 μM, and IC50s of 609 nM for both NRP1-a1 and NRP1-b1. EG01377 dihydrochloride has antiangiogenic, antimigratory, and antitumor effects.
  • HY-107365
    PQR530

    		PI3K mTOR Cancer
    PQR530 is a potent, ATP-competitive, orally bioavailable and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, with a subnanomolar Kd toward PI3Kα and mTOR (0.84 and 0.33 nM, respectively). Antitumor activity.
  • HY-B0497S1
    Niclosamide-13C6

    BAY2353-13C6

    		 Isotope-Labeled Compounds STAT Parasite Antibiotic Infection Cancer
    Niclosamide- 13C6 is the 13C6 labeled Niclosamide. Niclosamide (BAY2353) is an orally bioavailable chlorinated salicylanilide, with anthelmintic and potential antineoplastic activity. Niclosamide (BAY2353) inhibits STAT3 with IC50 of 0.25 μM in HeLa cells and inhibits DNA replication in a cell-free assay.
  • HY-112151
    EG01377

    		Complement System Cancer
    EG01377 is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1), with a Kd of 1.32 μM, and IC50s of both 609 nM for NRP1-a1 and NRP1-b1. EG01377 has antiangiogenic, antimigratory, and antitumor effects.
  • HY-15287S
    Nelfinavir-d3

    		HIV Protease HIV Infection Cancer
    Nelfinavir-d3 (AG1341-d3) is the deuterium labeled Nelfinavir. Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir is a broad-spectrum, anticancer agent[1][2][3].
  • HY-124596
    CD161

    NKR-P1A

    		 Epigenetic Reader Domain Cancer
    CD161 (NKR-P1A) is a potent, selective and orally bioavailable bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50s of 28.2 nM and 7.2 nM for BRD4 BD1 and BRD4 BD2, respectively. CD161 has good anticancer activity.
  • HY-13491
    GNF-5837

    		Trk Receptor Cancer
    GNF-5837 is a potent, selective, and orally bioavailable pan-tropomyosin receptor kinase (TRK) inhibitor which display antiproliferative effects in cellular Ba/F3 assays ( IC50 values of 7 nM, 9 nM and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively) .
  • HY-16125
    Carboxyamidotriazole Orotate

    L-651582 Orotate; CAI Orotate

    		 Calcium Channel Cancer Inflammation/Immunology
    Carboxyamidotriazole Orotate (L-651582 Orotate) is the orotate salt form of Carboxyamidotriazole (CAI), an orally bioavailable signal transduction inhibitor. Carboxyamidotriazole Orotate is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole Orotate shows anti-tumor, anti-inflammatory and antiangiogenic effects.
  • HY-145835A
    (S)-PERK-IN-5

    		PERK Cancer Infection
    (S)-PERK-IN-5 is the S-enantiomer of PERK-IN-5. (S)-PERK-IN-5 (example 39) is a PERK inhibitor, with an IC50 of 0.101-0.250 μM.
  • HY-122559
    BMS-984923

    		mGluR Neurological Disease
    BMS-984923, a potent mGluR5 silent allosteric modulator (SAM), with exquisite binding affinity (Ki = 0.6 nM), exhibits good oral bioavailability and BBB penetration. BMS-984923 potently inhibits the PrPC-mGluR5 interaction and prevents pathological Aβo signaling without affecting physiological glutamate signaling.
  • HY-146025
    Antitumor agent-F10

    		Others Cancer
    Antitumor agent-F10 (Compound F10) is a camptothecin derivative. Antitumor agent-F10 is an orally–bioavailable and potent antitumor agent. Antitumor agent-F10 displays lower acute toxicity than SN-38 does and the solubility of F10 reached 9.86 μg/mL.
  • HY-50674A
    INCB3344 R-isomer

    		CCR Inflammation/Immunology
    INCB3344 R-isomer is the R-isomer of INCB3344. INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
  • HY-111457
    BAY-677

    		Others Inflammation/Immunology
    BAY-677 is an inactive control for BAY-678. BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).
  • HY-120028
    GNE-207

    		Epigenetic Reader Domain Histone Acetyltransferase Cancer
    GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells.
  • HY-104037
    Cintirorgon

    LYC-55716

    		 ROR Cancer
    Cintirorgon (LYC-55716) is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival.
  • HY-18204A
    Sacubitril/Valsartan

    LCZ696

    		 Angiotensin Receptor Neprilysin Apoptosis Cardiovascular Disease Endocrinology Cancer
    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-17552
    sn-Glycero-3-phosphocholine

    Choline Alfoscerate; Alpha-GPC; L-α-GPC

    		 Cholinesterase (ChE) Endogenous Metabolite Neurological Disease
    sn-Glycero-3-phosphocholine (Choline Alfoscerate) is a precursor in the biosynthesis of brain phospholipids and increases the bioavailability of choline in nervous tissue. sn-Glycero-3-phosphocholine (Choline Alfoscerate) has significant effects on cognitive function with a good safety profile and tolerability, and is effective in the treatment of Alzheimer's disease and dementia.
  • HY-10237
    Boceprevir

    EBP 520; SCH 503034

    		 HCV Protease HCV SARS-CoV Infection
    Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay. Boceprevir inhibits SARS-CoV-2 3CL pro activity.
  • HY-10533
    Eniluracil

    5-Ethynyluracil; GW776C85

    		 Others Cancer
    Eniluracil (5-Ethynyluracil) is an orally active dihydropyrimidine dehydrogenase (DPD) inhibitor. Eniluracil irreversibly inhibits DPD, increases the oral bioavailability of 5-fluorouracil to 100%, and facilitates the uniform absorption and toxicity of 5-fluorouracil. Eniluracil can be used in cancer research of combination with fluoropyrimidines (including 5-fluorouracil).
  • HY-106003
    GSK356278

    		Phosphodiesterase (PDE) Inflammation/Immunology Neurological Disease
    GSK356278 is a potent, selective, orally bioavailable and brain-penetrant inhibitor of phosphodiesterase 4 (PDE4), with pIC50s of 8.6, 8.8, and 8.7 for human PDE4A, PDE4B, and PDE4D, respectively. GSK356278 has anti-inflammatory activity, and exhibits anxiolytic and cognition-enhancing effects.
  • HY-126321
    RORγt agonist 1

    		ROR Cancer
    RORγt agonist 1 (compound 14) is a potent, orally bioavailable RORγt agonist with an EC50 of 20.8 nM. RORγt agonist 1 showes high metabolic stability, improved aqueous solubility and excellent mouse PK profile. RORγt agonist 1 is a potential candidate of RORγt agonist for cancer immunotherapy.
  • HY-17593
    Solithromycin

    CEM-101; OP-1068

    		 Bacterial Antibiotic Infection
    Solithromycin (CEM-101) is an orally bioavailable, effective antimicrobial agent, with IC50s for inhibition of cell viability, protein synthesis, and growth rate are 7.5 ng/mL, 40 ng/mL, and 125 ng/mL for Streptococcus pneumonia, Staphylococcus aureus, and Haemophilus influenzae, respectively. Solithromycin binds to the large 50S subunit of the ribosome and inhibits protein biosynthesis.
  • HY-133552
    RORγt Inverse agonist 10

    		ROR Inflammation/Immunology
    RORγt Inverse agonist 10 is a potent and orally bioavailable RORγt (retinoic acid receptor-related orphan nuclear receptor gamma t) inverse agonist, with an IC50 of 51 nM. RORγt is a major transcription factor of genes related to psoriasis pathogenesis such as IL-17A, IL-22, and IL-23R
  • HY-15656A
    Ceritinib dihydrochloride

    LDK378 dihydrochloride

    		 Anaplastic lymphoma kinase (ALK) Insulin Receptor IGF-1R Cancer Endocrinology
    Ceritinib dihydrochloride (LDK378 dihydrochloride) is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib dihydrochloride (LDK378 dihydrochloride) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib dihydrochloride (LDK378 dihydrochloride) shows great antitumor potency.
  • HY-10300
    Narlaprevir

    SCH 900518

    		 HCV HCV Protease SARS-CoV Infection
    Narlaprevir (SCH 900518) is a selective and orally bioavailable NS3 protease inhibitor with a Ki value of 6 nM and an EC90 value of 40 nM. Narlaprevir also inhibits the HCV nonstructural protein 3 serine protease. Narlaprevir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 2.3 μM.
  • HY-19867A
    Burixafor hydrobromide

    TG-0054 hydrobromide

    		 CXCR Inflammation/Immunology Cardiovascular Disease Endocrinology Cancer
    Burixafor hydrobromide (TG-0054 hydrobromide) is an orally bioavailable and potent antagonist of CXCR4 and a well anti-angiogenic drug that is of potential value in treating choroid neovascularization. Burixafor hydrobromide (TG-0054 hydrobromide) mobilizes mesenchymal stem cells, attenuates inflammation, and preserves cardiac systolic function in a porcine model of myocardial infarction.
  • HY-127105
    Iptacopan

    LNP023

    		 Complement System Metabolic Disease Inflammation/Immunology
    Iptacopan (LNP023) is a first-in-class, orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 value of 10 nM. Iptacopan shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. Iptacopan targets the underlying cause of complement 3 glomerulopathy (C3G).
  • HY-17377
    Vicriviroc maleate

    SCH-417690 maleate; SCH-D maleate

    		 CCR HIV Infection Endocrinology
    Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate) is a potent, selective, oral bioavailable and CNS penetrated antagonist of CCR5, with a Ki of 2.5 nM, and also inhibits HIV-1 in PBMC cells, with IC90s of 3.3 nM (JrFL), 2.8 nM (ADA-M), 1.8 nM (301657), 4.9 nM (JV1083) and 10 nM (RU 570).
  • HY-15785
    Pimitespib

    TAS-116

    		 HSP Cancer
    Pimitespib (TAS-116) is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94. Pimitespib demonstrates less ocular toxicity.
  • HY-133129
    MS1943

    		Histone Methyltransferase Apoptosis Cancer
    MS1943 is a first-in-class, orally bioavailable EZH2 selective degrader, with an IC50 of 120 nM. MS1943 significantly reduces EZH2 protein levels in numerous triple-negative breast cancer (TNBC) and other cancer and noncancerous cell lines. MS1943 effectively blocks proliferation of multiple TNBC and other cancer cell lines.
  • HY-15959
    Savolitinib

    Volitinib; HMPL-504; AZD-6094

    		 c-Met/HGFR Cancer
    Savolitinib (AZD-6094) is a potent, highly selective, and orally bioavailable c-Met inhibitor with IC50 s of 5 nM and 3 nM for c-Met and p-Met, respectively. Savolitinib (AZD-6094) selectively binds to and inhibits the activation of c-Met in an ATP-competitive manner, and disrupts c-Met signal transduction pathways. Antineoplastic activity.
  • HY-135853
    Molnupiravir

    EIDD-2801; MK-4482

    		 SARS-CoV Influenza Virus Infection
    Molnupiravir (EIDD-2801) is an orally bioavailable proagent 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-15656
    Ceritinib

    LDK378

    		 Anaplastic lymphoma kinase (ALK) Insulin Receptor IGF-1R Cancer Endocrinology
    Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib (LDK378) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib (LDK378) shows great antitumor potency.
  • 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-107676
    SIB-1553A

    		nAChR Neurological Disease
    SIB-1553A is an orally bioavailable nicotinic acetylcholine receptors (nAChRs) agonist, with selectivity for β4 subunit-containing nAChRs. SIB-1553A is also a selective neuronal nAChR ligand. SIB-1553A is a cognitive enhancer, and has therapeutic potential for the symptomatic treatment of Alzheimer’s disease and other cognitive disorders.
  • HY-112601
    IDH1 Inhibitor 1

    		Isocitrate Dehydrogenase (IDH) Cancer
    IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1 R132H, IDH1 R132C, and IDH1 WT, respectively. Anticancer activity.
  • HY-103104
    Fananserin

    RP 62203

    		 5-HT Receptor Dopamine Receptor Neurological Disease
    Fananserin (RP 62203) is an orally bioavailable, potent and selective 5-hydroxytryptamine2 (5-HT2) receptor antagonist, with a Ki of 0.37 nM for the rat 5-HT2A receptor. Fananserin also is a selective dopamine D4 receptor antagonist, with a Ki of 2.93 nM for the human dopamine D4 receptor.
  • HY-111925
    BI-749327

    		TRP Channel Cardiovascular Disease
    BI-749327 is a potent, high selectivity and orally bioavailable TRPC6 antagonist, with IC50s of 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6, respectively. BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7.
  • HY-114277
    Sotorasib

    AMG-510

    		 Ras Cancer
    Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors.
  • HY-110117
    BIRT 377

    		Integrin Interleukin Related Inflammation/Immunology
    BIRT 377 is a potent amd orally bioavailable inhibitor of the interaction between intercellular adhesion molecule-1 (ICAM-1) and lymphocyte function-associated antigen-1 (LFA-1), with a Ki of 25.8 nM. BIRT 377 also inhibits the production of IL-2 in vivo. BIRT 377 can be used for researching inflammatory and immune disorders.
  • HY-133119
    PK150

    		Bacterial Infection
    PK150, an analogue of Sorafenib, shows oral bioavailability and antibacterial activity against several pathogenic strains at submicromolar concentrations. PK150 inhibits Gram-positive Methicillin-sensitive S. aureus (MSSA), Methicillin-resistant S. aureus (MRSA), Vancomycin intermediate S. aureus (VISA) with MICs of 0.3, 0.3-1, 0.3 µM, respectively.
  • HY-128345
    UDM-001651

    		Protease Activated Receptor (PAR) Cardiovascular Disease
    UDM-001651 is a potent, selective, and orally bioavailable protease-activated receptor 4 (PAR4) antagonist (IC50=4 nM; Kd=1.4 nM). UDM-001651 shows antiplatelet potency (IC50=25 nM) in a γ-thrombin-induced platelet-rich plasma aggregation assay (γ-Thr PRP).
  • HY-W007524
    2-Aminoquinoline

    2-Quinolinamine

    		 NO Synthase Orthopoxvirus Infection Neurological Disease
    2-Aminoquinoline (2-Quinolinamine) is a promising compound as bioavailable nNOS inhibitor but suffers from low human nNOS inhibition, low selectivity versus human eNOS, and significant binding to other CNS targets. 2-Aminoquinoline exhibits antiviral activity against the vaccinia virus. 2-Aminoquinoline has the potential for the research of antineurodegenerative agents.
  • 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-16361A
    Omigapil maleate

    CGP3466B; CGP3446 maleate; TCH346 maleate

    		 Apoptosis Metabolic Disease Neurological Disease
    Omigapil maleate, an orally bioavailable GAPDH nitrosylation inhibitor, abrogates Aβ1-42-induced tau acetylation, memory impairment, and locomotor dysfunction in mice. Omigapil maleate has the potential for the research of Alzheimer's disease. Omigapil maleate (CGP3446B maleate) is a apoptosis inhibitor. Omigapil maleate can be used for the research of congenital muscular dystrophy (CMD).
  • HY-10847A
    SB-277011 dihydrochloride

    SB-277011A dihydrochloride

    		 Dopamine Receptor Neurological Disease
    SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, with pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
  • HY-129707
    AMG 837 hemicalcium

    		Free Fatty Acid Receptor Metabolic Disease
    AMG 837 hemicalcium is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 hemicalcium inhibits specific [ 3H]AMG 837 binding at the human FFA1 receptor with a pIC50 of 8.13. AMG 837 hemicalcium could enhance insulin secretion and lower glucose levels in rodents.
  • HY-130119
    Integrin-IN-2

    		Integrin Cancer
    Integrin-IN-2 (compound 39) is an orally bioavailable pan αv integrin inhibitor. Integrin-IN-2 can increases the αvβ6, αvβ3, αvβ5 and αvβ8 binding affinities with pIC50 values of 7.8, 8.4, 8.4 and 7.4, respectively.
  • HY-18161
    CCT241736

    		FLT3 Aurora Kinase Cancer
    CCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor, which inhibits Aurora kinases (Aurora-A Kd, 7.5 nM, IC50, 38 nM; Aurora-B Kd, 48 nM), FLT3 kinase (Kd, 6.2 nM), and FLT3 mutants including FLT3-ITD (Kd, 38 nM) and FLT3(D835Y) (Kd, 14 nM).
  • 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-10237S
    Boceprevir-d9

    EBP 520-d9; SCH 503034-d9

    		 HCV Protease HCV SARS-CoV Infection
    Boceprevir-d9 is the deuterium labeled Boceprevir. Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay[1][2][3][4][5]. Boceprevir inhibits SARS-CoV-2 3CLpro activity[6].
  • HY-109015
    Tucidinostat

    Chidamide; HBI-8000; CS 055

    		 HDAC Cancer
    Tucidinostat (Chidamide) is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, less active on HDAC8 and HDAC11 (IC50s, 733 nM, 432 nM, respectively), and shows no effect on HDAC4/5/6/7/9.
  • HY-13967B
    AMG 837 calcium hydrate

    		Free Fatty Acid Receptor Metabolic Disease
    AMG 837 calcium hydrate is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 calcium hydrate inhibits specific [ 3H]AMG 837 binding at the human FFA1 receptor with a pIC50 of 8.13. AMG 837 calcium hydrate could enhance insulin secretion and lower glucose levels in rodents.
  • HY-101761
    TM5441

    		PAI-1 Apoptosis Cancer
    TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM and induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence.
  • 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-B0717
    Tocofersolan

    TPGS; D-α-Tocopherol polyethylene glycol 1000 succinate; Vitamin E-TPGS

    		 Others Metabolic Disease Neurological Disease
    Tocofersolan is synthetic polyethylene glycol derivative of α-tocopherol. Tocofersolan is an orally active and water-soluble analog of vitamin E. Tocofersolan can reduce neurobehavioral deficits in zebrafish embryos exposed to moderate and high concentrations of BaP during early development. Tocofersolan shows antioxidant activity. Tocofersolan can be used to provide an orally bioavailable source of vitamin E.
  • HY-125836
    CCR4 antagonist 2

    		CCR Cancer Endocrinology
    CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues. CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca 2+flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively.
  • HY-135853S
    Molnupiravir-d7

    EIDD-2801-d7; MK-4482-d7

    		 SARS-CoV Influenza Virus Inflammation/Immunology
    Molnupiravir-d7 is the deuterium labeled Molnupiravir. 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[1][2].
  • HY-151813
    NNMT-IN-4

    		Others Cancer
    NNMT-IN-4 (compound 38) is a selective, uncompetitive and membrane permeability nicotinamide N-methyltransferase (NNMT) inhibitor with IC50 values of 42 and 38 nM in vitro biochemical and cell-based assays, respectively. NNMT-IN-4 shows favorable PK/PD and safety profiles as well as excellent oral bioavailability and pharmaceutical properties. NNMT-IN-4 can be used as a vivo chemical probe of NNMT.
  • HY-124634
    PZ-2891

    		Others Neurological Disease
    PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC50s of 40.2 nM, 0.7 nM and 1.3 nM, respectively.
  • HY-142160
    GNE-9815

    		Raf Cancer
    GNE-9815 (compound 7) is a highly selective, pan-RAF inhibitor with good oral bioavailability. GNE-9815 exhibits Ki values of 0.062 and 0.19 nM for CRAF and BRAF, respectively. GNE-9815 combines with MEK inhibitor Cobimetinib (HY-13064) shows synergistic modulation of MAPK pathway. GNE-9815 can be used in studies of KRAS mutant cancers.
  • 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-10206
    Amuvatinib

    MP470; HPK 56

    		 c-Kit PDGFR RAD51 FLT3 c-Met/HGFR RET Apoptosis Cancer
    Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.
  • HY-10206A
    Amuvatinib hydrochloride

    MP470 hydrochloride; HPK 56 hydrochloride

    		 c-Kit PDGFR RAD51 FLT3 c-Met/HGFR RET Cancer
    Amuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib hydrochloride (MP470 hydrochloride) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.
  • HY-151424
    Vimentin-IN-1

    		Proteasome Cancer
    Vimentin-IN-1 is a FiVe1 derivative, an orally active and selective anticancer agent. FiVe1 binds type III intermediate filament protein vimentin (VIM), to induce hyperphosphorylation of Ser56, resulting selective disruption of mitosis and multinucleation in transformed VIM-expressing mesenchymal cancer cells. Vimentin-IN-1 shows better oral bioavailability and pharmacokinetic profiles than FiVe1.
  • HY-136026
    Camlipixant

    BLU-5937

    		 P2X Receptor Inflammation/Immunology
    Camlipixant (BLU-5937) a potent, selective, non-competitive and orally active P2X3 homotrimeric receptor antagonist with an IC50 of 25 nM against hP2X3 homotrimeric. Camlipixant shows potent anti-tussive effect and no taste alteration. Camlipixant can be used for the research of unexplained, refractory chronic cough.
  • HY-144653
    PDGFR-IN-1

    		PDGFR Apoptosis Cancer
    PDGFR-IN-1 (compound 7m) is a potent and orally active PDGFR (platelet-derived growth factor receptor) inhibitor, with IC50 values of 2.4 and 0.9 nM for PDGFRα and PDGFRβ, respectively. PDGFR-IN-1 displays robust antitumor effects and low toxicity, and can be used to study osteosarcoma.
  • HY-109118A
    Masupirdine mesylate

    SUVN-502 mesylate

    		 5-HT Receptor Neurological Disease
    Masupirdine mesylate (SUVN-502 mesylate) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine mesylate (SUVN-502 mesylate) shows high selectivity over 5-HT2A receptor and other 100 target sites, and has potential for treatment of Alzheimer's disease.
  • HY-15463
    Imatinib

    STI571; CGP-57148B

    		 Bcr-Abl PDGFR c-Kit SARS-CoV Autophagy Cancer
    Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
  • HY-133747
    JAK3-IN-9

    		JAK Inflammation/Immunology
    JAK3-IN-9 is an orally active JAK3 inhibitor with IC50 value of 1.7 nM. JAK3-IN-9 is highly selective to the JAK3 signal path. JAK3-IN-9 is lowly toxic with high oral bioavailability, shows good anti-arthritis activity. JAK3-IN-9 can be used in autoimmune disease research.
  • HY-50878
    Crizotinib

    PF-02341066

    		 Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy Cancer
    Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition.
  • HY-146388
    Mtb ATP synthase-IN-1

    		Bacterial ATP Synthase Infection
    Mtb ATP synthase-IN-1 (compound 6ab) is a potent Mycobacterium tuberculosis (Mtb) ATP synthase inhibitor, with MIC of 0.452-0.499 μg/mL against Mtb. Mtb ATP synthase-IN-1 has good metabolic stability, low cytotoxicity (Vero IC50 > 64 μg/mL), and acceptable oral bioavailability. Mtb ATP synthase-IN-1 can be used for researching anti-mycobacterium.
  • HY-50887
    L-873724

    		Cathepsin Metabolic Disease
    L-873724 is a potent, orally bioavailable, selective and reversible non-basic cathepsin K inhibitor, with IC50s of 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsin B, respectively. L-873724 also exhibits an IC50 of 0.5 nM for rabbit cathepsin K. L-873724 inhibits bone resorption.
  • HY-15463S2
    Imatinib-d3 hydrochloride

    STI571-d3 (hydrochloride); CGP-57148B-d3 (hydrochloride)

    		 PDGFR SARS-CoV c-Kit Bcr-Abl Autophagy Cancer
    Imatinib-d3 (hydrochloride) is the deuterium labeled Imatinib. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
  • HY-144256
    CHD1Li 6.11

    		Others Cancer
    CHD1Li 6.11 is a potent oncogenic CHD1L inhibitor (IC50=3.3 µM for cat-CHD1L recombinant protein). CHD1Li 6.11 is an orally bioavailable antitumor agent, significantly reducing the tumor volume of CRC xenografts generated from isolated quasi mesenchymal cells (M-phenotype), which possess enhanced tumorigenic properties.
  • HY-P99340
    Sotrovimab

    VIR 7831

    		 SARS-CoV Infection
    Sotrovimab (VIR 7831) is a human IgG1κ pan-sarbecovirus monoclonal antibody (mAb), neutralizes SARS-CoV-2, SARS-CoV-1, and multiple other sarbecoviruses. Sotrovimab is developed based on S309, exhibits a long half-life and great bioavailability in the respiratory mucosa. Sotrovimab could result in immune-mediated viral clearance and prevent progression of Covid-19 early in the course of disease.
  • HY-128570
    FD-IN-1

    		Complement System Inflammation/Immunology
    FD-IN-1 (Compound 12) is an orally bioavailable and selective factor D (FD) inhibitor with an IC50 of 12 nM. Complement FD, a highly specific S1 serine protease, plays a central role in the alternative complement pathway of the innate immune system. FD-IN-1 also inhibits factor XIa (FXIa) and Tryptase β2 with IC50s of 7.7 and 6.5 µM, respectively.
  • HY-110160
    Pozanicline dihydrochloride

    ABT-089 dihydrochloride

    		 nAChR Neurological Disease
    Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a Ki of 16.7 nM for binding to [ 3H]cytisine sites. Pozanicline is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a Ki of 17 nM while binding to α7 nAChR is insignificant.
  • HY-101855
    Emrusolmin

    Anle138b

    		 Amyloid-β Neurological Disease
    Emrusolmin (Anle138b), an oligomeric aggregation inhibitor, blocks the formation of pathological aggregates of prion protein (PrPSc) and of α-synuclein (α-syn). Emrusolmin strongly inhibits oligomer accumulation, neuronal degeneration, and disease progression in vivo. Emrusolmin has low toxicity and an excellent oral bioavailability and blood-brain-barrier penetration. Emrusolmin blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology.
  • HY-14483
    AF-353

    Ro-4

    		 P2X Receptor Cancer
    AF-353 (Ro-4) is a potent, selective and orally bioavailable P2X3/P2X2/3 receptor antagonist, with a pIC50 of 8.0 for both human and rat P2X3, and with a pIC50 of 7.3 for human P2X2/3.
  • 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-10251
    BMS-599626

    AC480

    		 EGFR Cancer
    BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy.
  • HY-12868
    Bimiralisib

    PQR309

    		 PI3K mTOR Cancer
    Bimiralisib (PQR309) is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively. Bimiralisib is an mTORC1 and mTORC2 inhibitor.
  • HY-15823
    CAY10566

    		Stearoyl-CoA Desaturase (SCD) Cancer
    CAY10566 is a potent, orally bioavailable and selective stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50s of 4.5 and 26 nM in mouse and human enzymatic assays, respectively. CAY10566 also shows excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells (IC50=7.9 nM or 6.8 nM).
  • 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-10209A
    Masitinib mesylate

    AB-1010 mesylate

    		 c-Kit PDGFR Src FGFR Apoptosis Cancer
    Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib mesylate (AB-1010 mesylate) has anti-proliferative, pro-apoptotic activity and low toxicity.
  • 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). ELQ-300 inhibits growth of P. falciparum Dd2, Tm90-C2B, and D1 with IC50 values of 6.6, 4.6 and 160 nM, respectively. ELQ-300 can be used for the research of antimalarial.
  • HY-12168B
    (Rac)-Tanomastat

    (Rac)-BAY 12-9566

    		 MMP Cancer
    (Rac)-Tanomastat ((Rac)-BAY 12-9566) is the racemate of Tanomastat. 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-131275
    Imatinib Impurity E

    		Drug Metabolite Others
    Imatinib Impurity E is the impurity of Imatinib. Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
  • HY-50878S
    Crizotinib-d5

    PF-02341066-d5

    		 Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy Cancer
    Crizotinib-d5 is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition[1][2][3].
  • HY-128879
    VP3.15

    		Phosphodiesterase (PDE) GSK-3 Neurological Disease
    VP3.15 is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS).
  • HY-128879A
    VP3.15 dihydrobromide

    		Phosphodiesterase (PDE) GSK-3 Neurological Disease
    VP3.15 dihydrobromide is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 dihydrobromide has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS).
  • HY-17552S
    sn-Glycero-3-phosphocholine-d9

    Choline Alfoscerate-d9; Alpha-GPC-d9; L-α-GPC-d9

    		 Cholinesterase (ChE) Endogenous Metabolite Neurological Disease
    sn-Glycero-3-phosphocholine-d9 is the deuterium labeled sn-Glycero-3-phosphocholine. sn-Glycero-3-phosphocholine (Choline Alfoscerate) is a precursor in the biosynthesis of brain phospholipids and increases the bioavailability of choline in nervous tissue. sn-Glycero-3-phosphocholine (Choline Alfoscerate) has significant effects on cognitive function with a good safety profile and tolerability, and is effective in the treatment of Alzheimer's disease and dementia[1][2].
  • HY-12010
    BMS-599626 Hydrochloride

    AC480 Hydrochloride

    		 EGFR Cancer
    BMS-599626 Hydrochloride (AC480 Hydrochloride) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 Hydrochloride displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 Hydrochloride inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy.
  • HY-10209
    Masitinib

    AB1010

    		 c-Kit PDGFR Src FGFR FAK Apoptosis Cancer
    Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity.
  • HY-50878A
    Crizotinib hydrochloride

    PF-02341066 hydrochloride

    		 Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy Cancer
    Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition.
  • HY-14979A
    ML786 dihydrochloride

    		Raf Bcr-Abl Discoidin Domain Receptor VEGFR RET Ephrin Receptor Cancer
    ML786 dihydrochloride is a potent and orally bioavailable Raf inhibitor, with IC50s of 2.1, 4.2, and 2.5 nM for V600EΔB-Raf, wt B-Raf, and C-Raf, respectively. ML786 dihydrochloride also inhibits Abl-1, DDR2, EPHA2, KDR, and RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 dihydrochloride can be used for the research of cancers.
  • 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-109035
    Inarigivir soproxil

    SB9200; GS-9992

    		 HCV HBV Infection
    Inarigivir soproxil (SB9200) is an agonist of innate immunity and shows potent antiviral activity against resistant HCV variants, with EC50s of 2.2 and 1.0 μM for HCV 1a/1b in cells of genotype 1 HCV replicon systems. Inarigivir soproxil, an orally bioavailable proagent of SB 9000, has broad-spectrum antiviral activity against RNA viruses including HCV, norovirus, respiratory syncytial virus and influenza and HBV.
  • HY-117482
    BPN-15606

    		γ-secretase Neurological Disease
    BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 has acceptable PK/PD properties, including bioavailability, half-life, and clearance.
  • HY-109118
    Masupirdine free base

    SUVN-502 free base

    		 5-HT Receptor Neurological Disease
    Masupirdine free base (SUVN-502 free base) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine free base (SUVN-502 free base) shows high selectivity over 5-HT2A receptor and other 100 target sites, and has potential for treatment of Alzheimer's disease.
  • HY-16961
    Sitravatinib

    MGCD516; MG-516

    		 VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor Cancer Inflammation/Immunology
    Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively. Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
  • HY-100408
    GNF-6231

    		Porcupine Cancer
    GNF-6231 is a potent, selective, and orally bioavailable Porcupine inhibitor that blocks Wnt signaling. 1) GNF-6231 shows IC50s of greater than 10 μM on all CYP isoforms tested 2) GNF-6231 have favorable potency and a PK profile across preclinical species upon oral administration. 3) The reference for orally in MMTV-Wnt1 tumor bearing mice is dosed at 3 mg/kg. 4) GNF-6231 showed very robust dose-related antitumor efficacy.
  • HY-143880
    MRGPRX1 agonist 4

    		Others Neurological Disease
    MRGPRX1 agonist 4 (compound 1t) is a potent and orally active Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC50 value of 0.1 μM. MRGPRX1 agonist 4 has good metabolic stability and oral bioavailability. MRGPRX1 agonist 4 can reduce behavioral heat hypersensitivity in a neuropathic pain model humanized MRGPRX1 mice. MRGPRX1 agonist 4 can be used for researching neuropathic pain.
  • HY-13208
    Xevinapant hydrochloride

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

    		 IAP Apoptosis Cancer
    Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with Kis of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors.
  • HY-117482A
    BPN-15606 besylate

    		γ-secretase Neurological Disease
    BPN-15606 besylate is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 besylate lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 besylate has acceptable PK/PD properties, including bioavailability, half-life, and clearance.
  • HY-101117
    EED226

    		Histone Methyltransferase Cancer
    EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model. EED226 is a potent, selective, and orally bioavailable EED inhibitor. EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays.
  • HY-117287
    Deucravacitinib

    BMS-986165

    		 JAK Interleukin Related IFNAR Inflammation/Immunology
    Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. Deucravacitinib inhibits IL-12/23 and type I IFN pathways. Deucravacitinib, the FDA's world first de novo deuterium, is available for study in moderate to severe plaque psoriasis.
  • 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-126750
    GNF362

    		Phosphatase Inflammation/Immunology
    GNF362 is a selective, potent, and orally bioavailable inhibitor of inositol trisphosphate 3’ kinase B (Itpkb) with an IC50 of 9 nM. GNF362 also inhibits Itpka and Itpkc with IC50 values of 20 nM and 19 nM, respectively. Inositol trisphosphate 3’ kinase B (Itpkb) is a Ca 2+-dependent kinase, which phosphorylates the 3’ position of Ins (1,4,5) P3 to generate inositol 1,3,4,5-tetrakisphosphate [Ins (1,3,4,5) P4].
  • HY-112306
    Ripretinib

    DCC-2618

    		 c-Kit PDGFR FLT3 VEGFR Apoptosis Cancer
    Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2). DCC-2618 exerts antineoplastic effect and induces apoptosis.
  • HY-16961A
    Sitravatinib malate

    MGCD516 malate; MG-516 malate

    		 VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor Cancer Inflammation/Immunology
    Sitravatinib malate (MGCD516 malate) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively. Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
  • HY-100370
    MRK-016

    		GABA Receptor Cancer
    MRK-016 is a selective, orally bioavailable inverse agonist of GABAA α5 receptor, with an EC50 of 3 nM for GABAA α5, and Kis of 0.83, 0.85, 0.77 and 1.4 nM for human GABAA α1β3γ2, GABAA α2β3γ2, GABAA α3β3γ2, and GABAA α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.
  • HY-145479
    PROTAC AR-V7 degrader-1

    		PROTACs Androgen Receptor Cancer
    PROTAC AR-V7 degrader-1 (Compound 6) is a potent, orally bioavailable and selective AR-V7 degrader with the DC50 of 0.32 µM by recruiting VHL E3 ligase to Androgen receptor (AR) DNA binding domain (DBD) binder. PROTAC AR-V7 degrader-1 exhibits activity against 22Rv1 cell-line expressing AR-V7 with the EC50 of 0.88 µM.
  • HY-13246
    Apitolisib

    GDC-0980; GNE 390; RG 7422

    		 PI3K mTOR Apoptosis Cancer
    Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC50s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with a Ki of 17 nM for mTOR.
  • HY-N1445
    Isoquercetin

    Quercetin 3-glucoside

    		 NF-κB NO Synthase Inflammation/Immunology Cancer
    Isoquercetin (Quercetin 3-glucoside) is a naturally occurring polyphenol that has antioxidant, anti-proliferative, and anti-inflammatory properties. Isoquercetin alleviates ethanol-induced hepatotoxicity, oxidative stress, and inflammatory responses via the Nrf2/ARE antioxidant signaling pathway. Isoquercetin regulates the expression of nitric oxide synthase 2 (NO2) via modulating the nuclear factor-κB (NF-κB) transcription regulation system. Isoquercetin has high bioavailability and low toxicity, is a promising candidate agent to prevent birth defects in diabetic pregnancies.
  • 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-100014
    KDM5A-IN-1

    		Histone Demethylase Cancer
    KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B).
  • 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-100818
    Futibatinib

    TAS-120

    		 FGFR Cancer
    Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor, with IC50s of 3.9, 1.3, 1.6, and 8.3 nM for FGFR 1-4, respectively. Futibatinib inhibits mutant and wild-type FGFR2 with similar IC50s (wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM).
  • HY-112602
    PI3K/mTOR Inhibitor-1

    		PI3K mTOR Cancer
    PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual PI3K/mTOR inhibitor with IC50s of 20/376/204/46 nM and 186 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ and mTOR, respectively. Antitumor activity.
  • 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-15514A
    Merestinib dihydrochloride

    LY2801653 dihydrochloride

    		 c-Met/HGFR FLT3 ROS Kinase Discoidin Domain Receptor Cancer
    Merestinib dihydrochloride (LY2801653 dihydrochloride) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib dihydrochloride also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM).
  • HY-126291
    GNE-616

    		Sodium Channel Neurological Disease
    GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype selective Nav1.7 inhibitor (Ki of 0.79 nM and Kd of 0.38 nM for hNav1.7) for the treatment of chronic pain. GNE-616 shows >1000 nM Kd and >2500-fold selectivity over hNav1.1, hNav1.3, hNav1.4, and hNav1.5. Selectivity over hNav1.2 and hNav1.6 is more modest at 31- and 73-fold, respectively.
  • 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-15514
    Merestinib

    LY2801653

    		 c-Met/HGFR FLT3 ROS Kinase Discoidin Domain Receptor Cancer
    Merestinib (LY2801653) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib (LY2801653) also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM).
  • HY-12169
    Marimastat

    BB2516; TA2516

    		 MMP Cancer
    Marimastat (BB2516) is a broad spectrum and orally bioavailable inhibitor of MMPs, with potent activity against MMP-9 (IC50=3 nM), MMP-1 (IC50=5 nM), MMP-2 (IC50=6 nM), MMP-14 (IC50=9 nM) and MMP-7 (IC50=13 nM), used in the treatment of cancer. Marimastat (BB2516) is an angiogenesis and metastasis inhibitor, which limits the growth and production of blood vessels. As an antimetatstatic agent it prevents malignant cells from breaching the basement membranes.
  • HY-135985
    DCLK1-IN-1

    		Others Cancer
    DCLK1-IN-1 is a selective, oral bioavailability in vivo-compatible chemical probe of the doublecortin like kinase 1 (DCLK1 kinase) domain. DCLK1-IN-1 inhibits DCLK1 and DCLK2 kinases (IC50: DCLK1=9.5/57.2 nM and DCLK2=31/103 nM in binding and kinase assay, respectively). DCLK1-IN-1 shows low toxicity, and can investigate DCLK1 biology and establish its role in cancer, like DCLK1 + pancreatic ductal adenocarcinoma (PDAC).
  • HY-124322
    NB-360

    		Beta-secretase Inflammation/Immunology Neurological Disease
    NB-360 is a potent, brain penetrable, and orally bioavailable dual BACE1/BACE2 inhibitor (IC50: mouse and human BACE1=5 nM; BACE2=6 nM). NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in amyloid precursor protein(APP) transgenic mice. NB-360 can completely block the progression of Aβ deposition in the brains of APP transgenic mice. NB-360 shows excellent selectivity over the related aspartyl proteases pepsin, cathepsin D and cathepsin E.
  • HY-123960
    Raphin1

    		Phosphatase Neurological Disease
    Raphin1 is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease.
  • HY-13238
    Dolutegravir

    S/GSK1349572

    		 HIV Integrase HIV Infection
    Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM).
  • HY-123960A
    Raphin1 acetate

    		Phosphatase Neurological Disease
    Raphin1 acetate is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 acetate binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 acetate crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease.
  • HY-100555
    CH5138303

    		HSP Cancer Infection
    CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model.
  • HY-13238A
    Dolutegravir sodium

    S/GSK1349572 sodium

    		 HIV Integrase HIV Infection
    Dolutegravir sodium (S/GSK1349572 sodium) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir sodium (S/GSK1349572 sodium) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir sodium (S/GSK1349572 sodium) retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM).
  • HY-13238S2
    Dolutegravir-d5

    S/GSK1349572-d5

    		 HIV Integrase HIV Infection
    Dolutegravir-d5 is deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
  • HY-13238S1
    Dolutegravir-d3

    S/GSK1349572-d3

    		 HIV Integrase HIV Infection
    Dolutegravir-d3 is the deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
  • HY-13342AS
    Apatinib-d8 free base

    YN968D1-d8 free base

    		 Src VEGFR Autophagy c-Kit RET Cancer
    Apatinib-d8 (free base) is the deuterium labeled Apatinib free base[1]. Apatinib free base (YN968D1 free base) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 (IC50=1 nM). Apatinib free base (YN968D1 free base) is an anti-angiogenic drug for the research of advanced or metastatic gastric cancer. Apatinib free base (YN968D1 free base) potently inhibits Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. It also inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ[2][3][4].
  • HY-10847B
    SB-277011 hydrochloride

    SB-277011A hydrochloride

    		 Dopamine Receptor 5-HT Receptor Neurological Disease
    SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor (D3R) antagonist with Ki values of 10.7 nM and 11.2 nM at rodent and human D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
  • HY-144392
    AChE/BuChE-IN-1

    		Cholinesterase (ChE) Neurological Disease
    AChE/BuChE-IN-1 (Compound 1), a chrysin derivative, is a selective butyrylcholinesterase (BuChE) inhibitor with an IC50 of 0.48 μM. AChE/BuChE-IN-1 inhibits acetylcholinesterase (AChE) with an IC50 of 7.16 μM. AChE/BuChE-IN-1 shows strong scavenging ·OH activities with a IC50 of 0.1674 μM. AChE/BuChE-IN-1 inhibits reactive oxygen species (ROS), Aβ1-42 aggregation (self-, Cu2+-induced, AChE-induced). AChE/BuChE-IN-1 has high BBB permeability and bioavailability and low cell toxicity. AChE/BuChE-IN-1 has the potential for Alzheimer' disease (AD) research.
  • HY-19974
    TAK-220

    		CCR HIV Infection Endocrinology
    TAK-220 is a selective and orally bioavailable CCR5 antagonist, with IC50s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7; TAK-220 also selectively inhibits HIV-1, with EC50s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA), and EC90s of 12 nM (HIV-1 KK), 5 nM (HIV-1 CTV), 12 nM (HIV-1 HKW), 28 nM (HIV-1 HNK), 15 nM (HIV-1 HTN), and 4 nM (HIV-1 HHA) in PBMCs.