Search Result
Results for "
orally
" in MedChemExpress (MCE) Product Catalog:
5856
Inhibitors & Agonists
13
Biochemical Assay Reagents
461
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-147136
-
|
|
Others
|
Cancer
|
|
MYF-03-176 is an orally active and potent anticancer agent. MYF-03-176 shows strong antitumor efficacy in MPM mouse xenograft model via oral administration.
|
-
- HY-12422B
-
|
|
CDK
|
Cancer
|
|
rel-(2S,3R)-Voruciclib hydrochloride is the enantiomer of Voruciclib hydrochloride. Voruciclib is an orally active CDK inhibitor.
|
-
- HY-141711
-
|
|
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-16259
-
|
LY 135837
|
Others
|
Cardiovascular Disease
|
|
Indecainide hydrochloride is a potent and orally active class I local anesthetic antiarrhythmic agent.
|
-
- HY-119169
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulozole is an orally active synthetic microtubule inhibitor. Tubulozole can be used for the research of tumor.
|
-
- HY-76511
-
-
- HY-B0224
-
-
- HY-B0224A
-
-
- HY-107787
-
-
- HY-124419
-
|
|
mGluR
|
Neurological Disease
|
|
RO0711401 is a selective and orally active positive allosteric modulator of mGlu1 receptor with an EC50 of 56 nM.
|
-
- HY-18966
-
-
- HY-77591
-
-
- HY-15531
-
|
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-132824
-
|
VNRX-7145
|
Bacterial
|
Infection
|
|
Ledaborbactam etzadroxil (VNRX-7145) is an orally active Ambler class A, C, and D β-lactamase enzymes inhibitor.
|
-
- HY-13723A
-
|
SDZ-ASM 981 hydrate
|
Phosphatase
|
Inflammation/Immunology
|
|
Pimecrolimus hydrate (SDZ-ASM 981 hydrate) is a potent, nonsteroid and orally active calcineurin inhibitor. Pimecrolimus hydrate shows anti-inflammatory activity. Pimecrolimus hydrate has the potential for the research of atopic dermatitis and oral erosive lichen planus.
|
-
- HY-A0165
-
-
- HY-106499
-
-
- HY-136842
-
-
- HY-W173220
-
-
- HY-137442
-
|
EOS-850
|
Adenosine Receptor
|
Cancer
|
|
Inupadenant is an orally active, highly selective A2A receptor antagonist. Inupadenant is not brain-penetrant. Inupadenant has potent anti-tumor activity.
|
-
- HY-145483
-
|
KYM-001; PROTAC IRAK4 degrader-7
|
PROTACs
IRAK
|
Cancer
|
|
KT-474 (KYM-001; Compound I-417) is an orally active PROTAC IRAK4 degrader with antitumor activities.
|
-
- HY-106571
-
|
Ro 19-5248; T-2588
|
Bacterial
Antibiotic
|
Infection
|
|
Cefteram pivoxil (Ro 19-5248), an orally active cephalosporin antibiotic, is used for bacterial infections.
|
-
- HY-147041
-
|
GB1211
|
Galectin
|
Cancer
|
|
Selvigaltin (GB1211) is an orally available galectin-3 (Gal-3) inhibitor.
|
-
- HY-109022
-
|
MK-8031; AGN-241689
|
CGRP Receptor
|
Neurological Disease
|
|
Atogepant (MK-8031) is an orally active and selective calcitonin gene–related peptide receptor (CGRP) antagonist. Atogepant can be used for researching migraine.
|
-
- HY-A0175
-
-
- HY-155652
-
|
|
BCRP
|
Cancer
|
|
ABCG2-IN-1 (compound K2), a Ko143 analog, is an orally active ABCG2 inhibitor with an IC50 of 0.13 μM. ABCG2-IN-1 has favorable oral pharmacokinetic profiles in mice.
|
-
- HY-76511S
-
|
MK-679-d6; L 668019-d6
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
Verlukast-d6 is a deuterium labeled Verlukast. Verlukast is a potent, selective, and orally active antagonist of leukotriene receptor. Verlukast has the potential for the research of asthma[1].
|
-
- HY-107647A
-
-
- HY-129683
-
|
|
PPAR
|
Metabolic Disease
|
|
AM3102 is an oleoylethanolamide (OEA) analog. AM3102 is an endogenous high-affinity PPAR-alpha agonist. AM3102 resists enzymatic hydrolysis, activates PPAR-alpha with high potency in vitro, and persistently reduces feeding when administered in vivo either parenterally or orally.
|
-
- HY-139346
-
-
- HY-100411
-
MLi-2
4 Publications Verification
|
LRRK2
|
Neurological Disease
|
|
MLi-2 is an orally active and highly selective LRRK2 inhibitor with an IC50 of 0.76 nM. MLi-2 has the potential for Parkinson’s disease.
|
-
- HY-10913
-
-
- HY-10913A
-
|
GAP-134 Hydrochloride; ZP 1609 Hydrochloride
|
Gap Junction Protein
|
Cardiovascular Disease
|
|
Danegaptide Hydrochloride (GAP-134 Hydrochloride) is a potent, selective and orally active gap-junction modifier with an antiarrhythmic effect.
|
-
- HY-15383
-
|
|
Others
|
Others
|
|
Glyparamide is an orally active chlorophenyl-containing sulfonylurea. Glyparamide shows hypoglycemic activity and rarely causes hepatic injury.
|
-
- HY-154436
-
|
|
Others
|
Neurological Disease
|
|
Anticonvulsant agent 2 is a potent and orally active anticonvulsant agent. Anticonvulsant agent 2 shows antiepileptic activity.
|
-
- HY-107533
-
|
|
Others
|
Endocrinology
|
|
T-98475 (Compound 26d) is a potent, orally active, non-peptide luteinizing hormone-releasing hormone (LHRH) receptor antagonist with an IC50 of 0.2 nM.
|
-
- HY-145704
-
|
|
Parasite
|
Infection
|
|
Antimalarial agent 8 (Compound 7e) is a novel orally active class of antimalarials. Antimalarial agent 8 is potent in vitro against P. falciparum and is orally efficacious (40 mg/kg) in an in vivo mouse model of malaria.
|
-
- HY-16735
-
|
BCX4161
|
Ser/Thr Protease
|
Others
|
|
Avoralstat (BCX4161), a potent and orally active plasma kallikrein (PKK) inhibitor, is used for hereditary angioedema research.
|
-
- HY-B1343
-
-
- HY-B1316
-
|
|
Others
|
Neurological Disease
|
|
Trimetozine is an orally active sedative. Trimetozine has mild tranquilizing effects. Trimetozine can be used for the research of anxiety.
|
-
- HY-155299
-
-
- HY-110274
-
-
- HY-B0714
-
|
Dexketoprofen tromethamine salt
|
COX
|
Neurological Disease
|
|
Dexketoprofen trometamol (Dexketoprofen tromethamine salt) is an orally active non-selective COX inhibitor. Dexketoprofen trometamol has a pain-relieving effect.
|
-
- HY-106538
-
|
ISF 2469
|
Others
|
Cardiovascular Disease
|
|
Cadralazine (ISF 2469) is an orally active antihypertensive agent. Cadralazine is a peripheral arteriolar vasodilator.
|
-
- HY-W011651
-
|
BZ-55
|
Others
|
Metabolic Disease
|
|
Carbutamide (BZ-55) is an orally active and first-generation sulfonylurea with hypoglycemic activity.
|
-
- HY-101566S
-
|
BAY 1895344-d3
|
ATM/ATR
|
Cancer
|
|
Elimusertib-d3 (BAY 1895344-d3) is the deuterium labeled Elimusertib (BAY 1895344). Elimusertib is a potent, orally active and selective ATR inhibitor and has anti-tumor activity.
|
-
- HY-118635
-
-
- HY-112736
-
-
- HY-101234
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
ICI 162846 is an orally active antagonist of H2 receptor. ICI 162846 inhibits acid production accompanied by an increase in the secretion of histamine in chronic duodenal ulcer (CDU) models. ICI 162846 is effective in preventing CDU.
|
-
- HY-10162
-
|
AZD2281; KU0059436
|
PARP
Autophagy
Mitophagy
|
Cancer
|
|
Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator.
|
-
- HY-151141
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-17 (Compound 12B) is a potent, orally active α-glucosidase inhibitor with an IC50 of 3.79 μM. α-Glucosidase-IN-17 shows antidiabetic activity.
|
-
- HY-131914A
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
EST64454 hydrochloride is a selective and orally active sigma-1 receptor antagonist with a Ki of 22 nM. EST64454 hydrochloride has the potential for the research of the pain.
|
-
- HY-101245
-
|
SUN-1165; Pilzicainide(hydrochloride)
|
Sodium Channel
|
Cardiovascular Disease
|
|
Pilsicainide hydrochloride (SUN-1165) is an orally active sodium channel blocker and potent class Ic antiarrhythmic agent.
|
-
- HY-W010593
-
|
|
Others
|
Cancer
|
|
Ethylenethiourea is a degradation product of the ethylenebisthiocarbamate group of fungicides. Ethylenethiourea is tumorigenic and teratogenic. Ethylenethiourea is orally active.
|
-
- HY-107318
-
-
- HY-14560
-
|
|
Others
|
Neurological Disease
|
|
Reboxetine is an orally active, potent and selective noradrenaline uptake blocker. Reboxetine can be used for antidepressant research.
|
-
- HY-148684
-
|
|
AMPK
|
Metabolic Disease
|
|
AMPK activator 10 is an orally active, potent AMPK activator with EC150 of 44.3 nM by cell-ELISA. AMPK activator 10 increases the phosphorylation levels of ACC. AMPK activator 10 exhibits a glucose lowering effect.
|
-
- HY-120634
-
|
|
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-131705
-
|
|
Btk
|
Inflammation/Immunology
|
|
BTK inhibitor 17 is a potent and orally active irreversible BTK inhibitor with an IC50 of 2.1 nM. BTK inhibitor 17 can be used for rheumatoid arthritis research.
|
-
- HY-137463
-
-
- HY-135655A
-
|
SPR720; pVXc-486
|
Bacterial
|
Infection
|
|
Fobrepodacin (SPR720) is an orally active and potent phosphate proagent of SPR719 (VXc-486; HY-12930). Fobrepodacin has potent bactericidal activities in vivo.
|
-
- HY-12177S
-
|
CGP 60536 d6 (hemifumarate); CGP60536B d6 (hemifumarate); SPP 100 d6 (hemifumarate)
|
Renin
Autophagy
|
Cancer
Cardiovascular Disease
|
|
Aliskiren-d6 (hemifumarate) is a deuterium labeled Aliskiren hemifumarate. Aliskiren hemifumarate is a direct and orally active renin inhibitor with an IC50 of 1.5 nM[1][2].
|
-
- HY-153113
-
|
DJT1116PG
|
SGLT
|
Endocrinology
|
|
Rongliflozin (DJT1116PG) is a selective and orally active inhibitor of sodium-glucose co-transporter-2 (SGLT-2). Rongliflozin can be used for the research of type 2 diabetes mellitus (T2DM).
|
-
- HY-109155
-
|
CRN00808
|
Somatostatin Receptor
|
Endocrinology
|
|
Paltusotine (CRN00808) is an orally active, nonpeptide selective somatostatin type 2 (SST2) receptor agonist. Paltusotine has the potential for maintaining GH and IGF-1 levels after depot somatostatin receptor ligand therapy.
|
-
- HY-106506
-
|
BW A515U
|
Others
|
Infection
|
|
Desciclovir is a potent and orally active proagent of the antiherpetic agent Acyclovir (ACV). Desciclovir is converted to acyclovir in vivo by xanthine oxidase.
|
-
- HY-106325
-
|
|
Others
|
Inflammation/Immunology
|
|
AA 2379 is an orally active antirheumatic agent. AA 2379 has antiinflammatory, antipyretic activities and reduces pain sensation.
|
-
- HY-124073
-
|
|
TRP Channel
|
Metabolic Disease
|
|
Dihydrocapsiate, as a compound of capsinoid family, is an orally active TRPV1 agonist. Dihydrocapsiate can be used for the research of metabolism disease.
|
-
- HY-B1682
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Loracarbef, a cephalosporin antibiotic, is an orally active second-generation synthetic beta-lactam antibiotic of the carbacephem class.
|
-
- HY-B1682A
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Loracarbef hydrate, a cephalosporin antibiotic, is an orally active second-generation synthetic beta-lactam antibiotic of the carbacephem class.
|
-
- HY-W013378
-
-
- HY-132815
-
|
MIV-818
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
Fostroxacitabine bralpamide (MIV-818) is an orally active Troxacitabine-based nucleotide proagent. Fostroxacitabine bralpamide has anticancer effects.
|
-
- HY-108685
-
|
Alendronic acid monosodium salt
|
Others
|
Metabolic Disease
|
|
Alendronate sodium is an orally active nitrogen-containing bisphosphonate. Alendronate sodium potently inhibits bone resorption. Alendronate sodium is used for the research of postmenopausal osteoporosis.
|
-
- HY-109099
-
|
INCB054828
|
FGFR
|
Cancer
|
|
Pemigatinib (INCB054828) is an orally active, selective FGFR inhibitor with IC50s of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma.
|
-
- HY-132894
-
|
|
Influenza Virus
|
Infection
|
|
Cap-dependent endonuclease-IN-1 is an orally active cap-dependent endonuclease inhibitor with high potency. Cap-dependent endonuclease-IN-1 can be used for the research of influenza.
|
-
- HY-14383
-
|
RAD140
|
Androgen Receptor
|
Endocrinology
Neurological Disease
|
|
Vosilasarm (RAD140) is a potent, orally active, nonsteroidal selective androgen receptor modulator (SARM) with a Ki of 7 nM. Vosilasarm shows good selectivity over other steroid hormone nuclear receptors.
|
-
- HY-133013
-
|
|
CFTR
|
Inflammation/Immunology
|
|
GLPG-3221 is a potent, orally active corrector of CFTR (cystic fibrosis transmembrane conductance regulator), with an EC50 of 105 nM. GLPG-3221 can be uesd for the treatment of cystic fibrosis.
|
-
- HY-147993
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora kinase inhibitor-10 (Compound 6c) is an orally active Aurora B inhibitor with an IC50 of 8 nM. Aurora kinase inhibitor-10 shows antitumor activity.
|
-
- HY-117507
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
U92016A hydrochloride is a potent, metabolically stable, orally acitive 5-HT1A receptor agonist with an exceptionally high degree of intrinsic activity. U92016A hydrochloride binds with high affinity to human 5-HT1A receptors expressed in Chinese hamster ovary cells (Ki=0.2 nM).
|
-
- HY-144110
-
|
|
HCV
|
Infection
|
|
HCV-IN-37 (Compound 3d) is a potent inhibitor of HCV. HCV-IN-37 is orally available and long-lasting in rat plasma after oral administration to rats by a single dose of 15 mg/kg. The high potency of active derivative HCV-IN-37 is primarily driven by the inhibitory effect on the virus entry stage.
|
-
- HY-B0467S
-
|
Amoxycillin d4
|
Bacterial
|
Infection
|
|
Amoxicillin-d4 is a deuterium labeled Amoxicillin. Amoxicillin is an antibiotic with good oral absorption and broad spectrum antimicrobial activity[1][2].
|
-
- HY-B1656
-
-
- HY-144393
-
|
|
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-106578
-
|
LM 208
|
Others
|
Neurological Disease
|
|
Quinupramine is an orally active antidepressant. Quinupramine can penetrate into the CNS and affect some of the processes of neurotransmission. The antidepressant activity of quinupramine is associated with the central serotonin system, but not with the β-adrenergic system[1][2].
|
-
- HY-13236
-
-
- HY-148348
-
|
|
HBV
|
Infection
|
|
AB-836 is an orally active HBV capsid inhibitor. AB-836 inhibits viral replication by interacting with HBV core protein.
|
-
- HY-108504
-
|
V 102862
|
Sodium Channel
|
Neurological Disease
|
|
Co 102862 (V 102862) is a potent, broad-spectrum, state-dependent Na + channel blocker. Co 102862 is also an orally active anticonvulsant.
|
-
- HY-B1800
-
|
|
Others
|
Cardiovascular Disease
|
|
Tolonidine is a derivative of imidazoline. Tolonidine is orally active and has been shown to possess hypotensive and antihypertensive properties.
|
-
- HY-107730
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
NPY5RA-972 is an orally active, central nervous system (CNS) penetrating, potent and selective NPY Y5 receptor antagonist that prevents feeding driven by activation of this receptor.
|
-
- HY-132196
-
|
|
Btk
|
Inflammation/Immunology
|
|
BTK inhibitor 18 is a potent, selective,orally active and covalent Btk inhibitor with a IC50 of 142 nM. BTK inhibitor 18 has anti-inflammatory activities.
|
-
- HY-N7225
-
|
Gnidilatidin
|
Others
|
Cancer
|
|
Yuanhuacine (Gnidilatidin), a daphnane diterpenoid from the flowers of Daphne genkwa with extensive anti-tumor activity. Yuanhuacine is a DNA-damaging agent with orally active.
|
-
- HY-17359
-
|
ICL 670
|
Bacterial
Ferroptosis
|
Cancer
|
|
Deferasirox (ICL 670) is an orally available iron chelator used for the management of transfusional iron overload.
|
-
- HY-W013331
-
|
|
Others
|
Inflammation/Immunology
|
|
Deoxy artemisinin, a orally bioavailable compound separated from Artemisinin annua L., shows anti-inflammatory and antiulcer activities.
|
-
- HY-106816
-
-
- HY-W392925
-
|
d-Aminoglutethimide
|
Cytochrome P450
|
Cancer
|
|
(R)-(+)-Aminoglutethimide is a potent and orally active aromatase inhibitor. (R)-(+)-Aminoglutethimide has the potential for the research of breast cancer.
|
-
- HY-A0252
-
-
- HY-101820A
-
|
|
EGFR
|
Cancer
|
|
Simotinib hydrochloride is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities.
|
-
- HY-B1363
-
|
Bendrofluazide
|
Others
|
Cardiovascular Disease
|
|
Bendroflumethiazide is an orally active diuretic. Bendroflumethiazide is an antihypertensive agent. Bendroflumethiazide has the potential for the research of arterial hypertensive disease.
|
-
- HY-101820
-
|
|
EGFR
|
Cancer
|
|
Simotinib is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities.
|
-
- HY-153711
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
TRPA1-IN-2 (compound 1) is a potent and orally active TRPA1 inhibitor with an IC50 value of 0.04 µM. TRPA1-IN-2 shows anti-inflammation activity.
|
-
- HY-A0107
-
|
|
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Tetracycline is a broad-spectrum antibiotic with oral activity. Tetracycline exhibits activity against a wide range of bacteria including gram-positive, gram-negative bacteria, chlamydiae, mycoplasmas and rickettsiae. Tetracycline can be used for the research of infections.
|
-
- HY-151135
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-15 (Compound 14B) is a potent, orally active α-glucosidase inhibitor with an IC50 of 3.34 μM. α-Glucosidase-IN-15 shows antidiabetic activity.
|
-
- HY-146075
-
|
|
Bacterial
|
Infection
|
|
β-Lactamase-IN-8 (compound 20) is a potent and oral bioavailable broad-spectrum cyclic boronate β-lactamase inhibitor. β-Lactamase-IN-8 can be used for researching antibacteria.
|
-
- HY-19947
-
|
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-B1651
-
|
Ferrous fumarate
|
Others
|
Metabolic Disease
Cancer
|
|
Iron(II) fumarate (Ferrous fumarate) is the iron(II) salt of fumaric acid. Iron(II) fumarate is an orally active dietary supplement and has the potential for iron deficiency anemia treatment.
|
-
- HY-116437
-
|
|
EGFR
|
Cancer
|
|
Selatinib is a reversible and orally active dual EGFR and ErbB2 inhibitor with IC50s of 13 nM and 22.5 nM, respectively. Selatinib has anticancer effects.
|
-
- HY-W020183
-
|
|
Others
|
Neurological Disease
|
|
γ-Terpinene, a monoterpene, is an orally active antioxidant compound which can scavenge radicals directly. γ-Terpinene has potent antinociception activity.
|
-
- HY-103459
-
|
PD156707
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
CI-1020 (PD156707) is an orally active and selective antagonist targeting endothelin (ETA) with an IC50 value of 0.3 nM. CI-1020 blocks intimal hyperplasia in human saphenous veins completely in organ culture. CI 1020 inhibits hypoxic pulmonary hypertension and blocks ET-1-induced pressor responses following oral administration.
|
-
- HY-139585
-
|
LC350189
|
Xanthine Oxidase
|
Metabolic Disease
|
|
Tigulixostat (LC350189) is an orally active, non-purine selective xanthine oxidase inhibitor. Tigulixostat lowers the production of uric acid. Tigulixostat can be used for gout and hyperuricemia study.
|
-
- HY-119245
-
|
BMS-986166
|
LPL Receptor
|
Inflammation/Immunology
|
|
Udifitimod (BMS-986166) is a potent, selective and orally active S1P1R modulator. Udifitimod has the potential for the research of autoimmune diseases.
|
-
- HY-42990
-
|
|
Others
|
Others
|
|
Hydrogenated soya phosphatidylcholines is a natural product. Hydrogenated soya phosphatidylcholines can extend drug release in regard to drug loading and solubility for oral drug delivery of watersoluble drugs.
|
-
- HY-B1481B
-
|
Isoetarine hydrochloride
|
Others
|
Infection
|
|
Isoetharine hydrochloride is selective, short-acting and orally active β-agonist which is widely used as a bronchodilator in the research of inhalation research.
|
-
- HY-155787
-
|
|
CDK
|
Cancer
|
|
SHR5428 is a potent, orally active, selective and noncovalent inhibitor of CDK7 with highly potent CDK7 enzymatic activity (IC50=2.3 nM). SHR5428 inhibits triple negative breast cancer cellular activity on MDA-MB-468 cell (IC50=6.6 nM).
|
-
- HY-146223
-
|
|
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-147411
-
|
MK-8507
|
Reverse Transcriptase
HIV
|
Infection
|
|
Ulonivirine (MK-8507) is an orally active non-nucleoside reverse transcriptase inhibitor with high antiviral activity. Ulonivirine can be used for the research of HIV-1 infection.
|
-
- HY-W105835
-
|
Trimagnesium dicitrate
|
Toll-like Receptor (TLR)
|
Neurological Disease
|
|
Magnesium citrate is a magnesium salt form that provides efficient penetration into brain and muscle tissue. Magnesium citrate increases pain threshold and reduces TLR4 concentration in the brain. Orally active.
|
-
- HY-143200
-
|
|
Others
|
Metabolic Disease
|
|
OSBPL7-IN-1 is an orally active oxysterol binding protein like 7 (OSBPL7) inhibitor. OSBPL7-IN-1 promotes an increase of ABCA1 at the plasma membrane without affecting mRNA expression.
|
-
- HY-122661
-
|
MPH
|
PARP
Apoptosis
|
Cancer
|
|
Mefuparib hydrochloride (MPH) is an orally active, substrate-competitive and selective PARP1/2 inhibitor with IC50s of 3.2 nM and 1.9 nM, respectively. Mefuparib hydrochloride induces apoptosis and possesses prominent anticancer activity in vitro and in vivo.
|
-
- HY-N7557
-
|
|
Others
|
Cancer
|
|
(E)-2'-Hydroxy-3,4-dimethoxychalcone (compound 7) is a Chalcone derivative with orally active. (E)-2'-Hydroxy-3,4-dimethoxychalcone has anti-tumour activities.
|
-
- HY-103179
-
|
WAG-994; N6-Cyclohexy-2'-0-methyladenosine
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
SDZ-WAG994 (WAG-994) is a stable, long-acting, selective and orally active A1-adenosine receptor agonist with a KD of 23 nM. SDZ-WAG994 can be used for the research of atrial fibrillation.
|
-
- HY-155457
-
|
|
STING
Phosphodiesterase (PDE)
|
Cancer
|
|
Enpp-1-IN-19 (compound 29f) is an orally active ENPP1 inhibitor that inhibits cGAMP hydrolysis by ENPP1 (IC50=68 nM). Enpp-1-IN-19 increases anti-PD-L1 responses and inhibits tumor growth in CT26 syngeneic models. Enpp-1-IN-19 also enhances STING-mediated type I interferon responses, induces immune memory, and prevents tumor recurrence.
|
-
- HY-18345
-
-
- HY-N10379
-
-
- HY-119605
-
|
|
Others
|
Neurological Disease
|
|
DAA-1097 is an orally active and selective agonist for the peripheral benzodiazepine receptor (PBR). DAA-1097 has anxiolytic effects.
|
-
- HY-151568
-
|
|
Parasite
|
Infection
|
|
UCB7362 is an orally active and potent antimalarial plasmepsin X (PMX) inhibitor, with an IC50 of 7 nM. UCB7362 inhibits parasite growth.
|
-
- HY-142687
-
|
|
SGK
|
Inflammation/Immunology
|
|
SGK1-IN-4 (compound 17a) is a highly selective, orally active SGK1 inhibitor. SGK1-IN-4 can be used for osteoarthritis research.
|
-
- HY-121776
-
|
|
Others
|
Cardiovascular Disease
|
|
Nicomol is an orally active hypolipidemic agent that can increase the high density lipoprotein cholesterol (HDL-C) level. Nicomol inhibits the rapid rise of plasma free fatty acids.
|
-
- HY-N12353
-
|
|
Phosphatase
|
Metabolic Disease
|
|
Stevisalioside A (Compound 2) can be isolated from Stevia serrata roots. Stevisalioside A is an orally active antidiabetic agent. Stevisaliosides A inhibits PTP1B (IC50: 526.8 μM). Stevisalioside A reduces blood glucose levels and the postprandial peak in oral glucose and insulin tolerance tests in Streptozotocin (HY-13753) induced hyperglycemic mice.
|
-
- HY-143793
-
|
|
Others
|
Metabolic Disease
|
|
RBP4 inhibitor 1 (compound 43b) is a potent and orally active retinol-binding protein 4 (RBP4) inhibitor with IC50s of 28 nM and 110 nM for human and mouse RBP4. RBP4 inhibitor 1 has a potent and long-lasting blood RBP4-level-reducing effect in mice.
|
-
- HY-145272
-
|
|
Others
|
Neurological Disease
|
|
ELOVL1-IN-3 (Compound 22) is a potent and orally active inhibitor of elongation of very long chain fatty acid 1 (ELOVL1) enzyme. ELOVL1-IN-3 serves as a useful tool for researching adrenoleukodystrophy (ALD)[1].
|
-
- HY-144770
-
|
|
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
|
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
|
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-A0287
-
|
Clomiphene
|
Others
|
Endocrinology
|
|
Clomifene is an orally active compound used for infertility. Clomifene is a simple, relatively safe, easily administered and well-tolerated efficacious compound to induce ovulation.
|
-
- HY-14568
-
|
|
GlyT
|
Neurological Disease
|
|
DCCCyB is an orally bioavailable, potent, and selective inhibitor of GlyT1. DCCCyB demonstrates excellent in vivo occupancy of GlyT1 transporters in rhesus monkey.
|
-
- HY-A0287A
-
|
Clomiphene hydrochloride
|
Others
|
Endocrinology
|
|
Clomifene hydrochloride is an orally active compound used for infertility. Clomifene hydrochloride is a simple, relatively safe, easily administered and well-tolerated efficacious compound to induce ovulation.
|
-
- HY-139398
-
TBI-223
1 Publications Verification
|
Bacterial
|
Infection
|
|
TBI-223 is an orally bioavailable oxazolidinone antibiotic and an antimicrobial. TBI-223 shows activity against Mycobacterium tuberculosis (Mtb).
|
-
- HY-112318A
-
|
|
Cathepsin
|
Inflammation/Immunology
|
|
GSK-2793660 is an orally active and irreversible inhibitor of Cathepsin C (CTSC). GSK-2793660 can be used for the research of bronchiectasis.
|
-
- HY-144073
-
|
|
MAP4K
|
Cancer
|
|
HPK1-IN-21 is a potent inhibitor of HPK1 kinase inhibitor (Ki=0.8 nM). HPK1-IN-21 also has orally active.
|
-
- HY-141482
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
WSB1 Degrader 1 is a poten and orally active WSB1 (WD repeat and SOCS box-containing 1) degrader. WSB1 Degrader 1 has anticancer metastatic effects.
|
-
- HY-141525
-
-
- HY-120494
-
|
|
Epoxide Hydrolase
|
Inflammation/Immunology
|
|
sEH inhibitor-1 (compound TCPU ) is a potent and oral active inhibitor of sEH (soluble epoxide hydrolase) with IC50s of 0.4 and 5.3 nM in human and murine, respectively.
|
-
- HY-12222
-
|
INT-747; 6-ECDCA; 6-Ethylchenodeoxycholic acid
|
FXR
Autophagy
|
Others
|
|
Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy.
|
-
- HY-105860
-
|
BGG 492
|
iGluR
|
Neurological Disease
|
|
Selurampanel (BGG 492) is an orally active and competitive AMPA receptor antagonist with an IC50 of 190 nM. Selurampanel has reasonable blood-brain barrier penetration. Selurampanel can be used for epilepsy research.
|
-
- HY-32345
-
|
BXL-628; Ro-26-9228
|
VD/VDR
|
Cancer
Inflammation/Immunology
|
|
Elocalcitol (BXL-628) is a selective, orally active vitamin D receptor (VDR) agonist. Elocalcitol shows anti-inflammatory activity. Elocalcitol inhibits growth of prostate cancer cells.
|
-
- HY-B0317
-
|
|
Calcium Channel
|
Cancer
Cardiovascular Disease
|
|
Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer.
|
-
- HY-B0317C
-
|
|
Calcium Channel
|
Cancer
Cardiovascular Disease
|
|
Amlodipine mesylate, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine mesylate can be used for the research of high blood pressure and cancer.
|
-
- HY-143439
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
LX-039 is a highly potent, selective and orally active estrogen receptor degrader with EC50 value of 2.29 nM. LX-039 has indole C-3 chlorine atom. LX-039 exhibits excellent mouse pharmacokinetics, low clearance, high Cmax and oral exposure. LX-039 has anti-tumor activity.
|
-
- HY-137892
-
|
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
|
GSK620 is a potent and orally active pan-BD2 inhibitor with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood.
|
-
- HY-124593
-
PTC299
1 Publications Verification
|
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-B1390B
-
|
|
Bacterial
|
Inflammation/Immunology
|
|
Saccharin sodium hydrate is an orally active, non-caloric artificial sweeteners (NAS). Saccharin sodium hydrate has bacteriostatic and microbiome-modulating properties.
|
-
- HY-B0925
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Oxacillin sodium salt is an orally active synthetic penicillin with good bactericidal activity against staphylococci and other gram-positive pathogens.
|
-
- HY-N0465
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Olaquindox, a quinoxalin derivative, is an orally active antibiotic. Olaquindox stimulates growth and decreases intestinal mucosal immunity of piglets.
|
-
- HY-B0925A
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Oxacillin is an orally active synthetic penicillin with good bactericidal activity against staphylococci and other gram-positive pathogens.
|
-
- HY-Y0272
-
|
|
Bacterial
|
Inflammation/Immunology
|
|
Saccharin is an orally active, non-caloric artificial sweeteners (NAS). Saccharin has bacteriostatic and microbiome-modulating properties.
|
-
- HY-B1390A
-
|
|
Bacterial
|
Infection
|
|
Saccharin sodium is an orally active, non-caloric artificial sweeteners (NAS). Saccharin sodium has bacteriostatic and microbiome-modulating properties.
|
-
- HY-149409
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-31 (compound R1) is an orally active, potent α-Glucosidase inhibitor with an IC50 value of 10.1 μM. α-Glucosidase-IN-31 significantly reduces the blood glucose level and has antidiabetic activity.
|
-
- HY-B0250A
-
|
BCH-189 salicylate
|
HIV
Reverse Transcriptase
HBV
|
Infection
|
|
Lamivudine (BCH-189) salicylate is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine salicylate can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS.
|
-
- HY-B0561
-
-
- HY-15975
-
|
|
Parasite
|
Infection
|
|
GNF179 is an optimized 8,8-dimethyl imidazolopiperazine analog that exhibits antimalarial potency (IC50 of 4.8 nM against the multidrug resistant strain W2). GNF179 is orally active.
|
-
- HY-B0089
-
|
BAY g 5421
|
Glucosidase
|
Metabolic Disease
|
|
Acarbose (BAY g 5421), antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose can potentiate the hypoglycemic effects of sulfonylureas or insulin.
|
-
- HY-143216A
-
|
S-217622 fumarate
|
SARS-CoV
Virus Protease
|
Infection
|
|
Ensitrelvir (S-217622) fumarate is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor (IC50=13 nM).
|
-
- HY-143216
-
|
S-217622
|
SARS-CoV
Virus Protease
|
Infection
|
|
Ensitrelvir (S-217622) is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor (IC50=13 nM).
|
-
- HY-B0265
-
-
- HY-149290
-
|
|
Prostaglandin Receptor
|
Cancer
|
|
AMX12006 is a potent, selective and orally active EP4 antagonist with an IC50 value of 4.3 nM. AMX12006 shows cytotoxic and antitumor activity.
|
-
- HY-150721
-
-
- HY-144878
-
|
|
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-13723
-
|
SDZ-ASM 981
|
Phosphatase
|
Inflammation/Immunology
|
|
Pimecrolimus (SDZ-ASM 981) is a potent, nonsteroid and orally active calcineurin inhibitor with a Ki of 117 nM. Pimecrolimus shows anti-inflammatory activity.
|
-
- HY-131973
-
|
|
Phosphodiesterase (PDE)
|
Metabolic Disease
Cardiovascular Disease
|
|
PDE10A-IN-2 hydrochloride is a potent, highly selective and orally active phosphodiesterase 10A (PDE10A) inhibitor with an IC50 of 2.8 nM. PDE10A-IN-2 hydrochloride shows selectivity of >3500-fold against other PDE subtypes. PDE10A-IN-2 hydrochloride can be used for pulmonary arterial hypertension (PAH) research.
|
-
- HY-148159
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
Safrazine is an irreversible, non-specific and orally active monoamine oxidase (MAO) inhibitor. Safrazine can be used for the research of depression.
|
-
- HY-122168
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
AAT-008 is a potent, selective, and orally active prostaglandin EP4 receptor antagonist with Kis of 0.97 and 6.1 nM for recombinant human EP4 and recombinant rat EP4, respectively.
|
-
- HY-139784
-
|
NFX88; (R)-2-Hydroxyoleic acid; (R)-2-OHOA
|
Others
|
Cancer
|
|
Idroxioleic acid ((R)-2-Hydroxyoleic acid; (R)-2-OHOA), the R enantiomer of (Rac)-Idroxioleic acid, is an orally active fatty acid that modulates the lipid composition and structure of the membranes. Idroxioleic acid has antitumor activities.
|
-
- HY-138639
-
|
|
GPR52
|
Neurological Disease
|
|
PW0787 is a potent, selective, orally active, and brain-penetrant GPR52 agonist (EC50=135 nM). PW0787 suppresses psychostimulant behavior.
|
-
- HY-121565
-
|
|
Others
|
Endocrinology
Metabolic Disease
|
|
SaRI 59-801 is an orally effective hypoglycemic compound. SaRI 59-801 decreases blood glucose in several species and to elevate plasma insulin in rats and mice.
|
-
- HY-19415
-
|
|
Phospholipase
|
Metabolic Disease
|
|
SB-435495 is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM.
|
-
- HY-B0317B
-
|
Amlodipine benzenesulfonate
|
Calcium Channel
|
Cancer
Cardiovascular Disease
|
|
Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer.
|
-
- HY-50898C
-
|
GW572016 tosylate; GW2016 tosylate
|
EGFR
Ferroptosis
Autophagy
|
Cancer
|
|
Lapatinib (GW572016) tosylate is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.
|
-
- HY-10158A
-
|
SKI-606 hydrate
|
Src
Bcr-Abl
|
|
|
Bosutinib (hydrate) is an oral Src/Abl tyrosine kinase inhibito with IC50 of 1.2 nM and 1 nM, respectively.
|
-
- HY-13705
-
-
- HY-B1711
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
Norfenefrine is an orally active, endogenously found α-adrenergic agonist and can be used for the research of female stress incontinence.
|
-
- HY-141795
-
|
Co 134444
|
Others
|
Neurological Disease
|
|
Posovolone (Co 134444) is an orally active, neuroactive steroid. Posovolone has anticonvulsant and anxiolytic-like activity as well as ataxic effects.
|
-
- HY-153392
-
|
|
HDAC
|
Cardiovascular Disease
|
|
TYA-018 is an orally active, potent and highly selective HDAC6 inhibitor. TYA-018 can protect heart function in mice. TYA-018 also enhances energetics in mice by increasing expression of targets associated with fatty acid metabolism, protein metabolism, and oxidative phosphorylation.
|
-
- HY-119104
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
AZD1940 is an orally active, high affinity cannabinoid CB1/CB2 receptor agonist with pKi values of 7.93 and 9.06 for human CB1R and CB2R, respectively. AZD1940 shows a robust analgesia action.
|
-
- HY-120608
-
|
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
BMS-814580 is an orally active, highly efficacious MCHR1 inhibitor with a Ki of 16.9 nM against hMCHR1. BMS-814580 shows antiobesity activities.
|
-
- HY-121341
-
|
Ro 10-5970
|
Bacterial
|
Infection
|
|
Brodimoprim (Ro 10-5970), a trimethoprim analogue, is an orally active dihydrofolate reductase inhibitor. Brodimoprim is highly active against a broad spectrum of gram-negative and gram-positive bacteria.
|
-
- HY-15386
-
|
MD 780515
|
Monoamine Oxidase
|
Metabolic Disease
|
|
Cimoxatone (MD 780515) is a reversible, selectively and orally active type A monoamine oxidase (MAO-A) inhibitor. Cimoxatone enhances the anorectic action of Serotonin (HY-B1473A).
|
-
- HY-B0698
-
|
Sch 39720
|
Bacterial
Antibiotic
|
Infection
|
|
Ceftibuten (Sch39720), an antibiotic, is an orally active cephalosporin, possesses potent activity in vitro against a wide range of gram-negative and certain gram-positive pathogens.
|
-
- HY-12713
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Lisuride is an orally active dopamine D2 receptors agonist. Lisuride, as an ergot derivative, can be used for the research of Parkinson's disease, migraine, and high prolactin levels.
|
-
- HY-122230
-
|
|
Integrin
|
Cardiovascular Disease
|
|
UR-3216 is a selective, and orally active platelet surface glycoprotein (GPIIb/IIIa) receptor antagonist. UR-3216 has the potential for cardiovascular diseases research.
|
-
- HY-107611
-
-
- HY-B0698B
-
|
Sch 39720 hydrate
|
Bacterial
Antibiotic
|
Infection
|
|
Ceftibuten (Sch39720) hydrate, an antibiotic, is an orally active cephalosporin, possesses potent activity in vitro against a wide range of gram-negative and certain gram-positive pathogens.
|
-
- HY-15796
-
GNE0877
2 Publications Verification
|
LRRK2
|
Neurological Disease
|
|
GNE0877 is a highly selective, orally active and brain-penetrant LRRK2 inhibitor with an IC50 of 3 nM and a Ki of 0.7 nM. GNE0877 can be used for the research of neuroscience.
|
-
- HY-15651A
-
|
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-131336
-
|
|
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-108620
-
|
GR259653X
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
CDP-840 (GR259653X) is a potent, selective and orally active phosphodiesterase IV (PDE IV) inhibitor. CDP-840 inhibits antigen-induced early and late phase bronchoconstriction in conscious squirrel monkeys.
|
-
- HY-14950
-
|
JTT-705; RO4607381
|
CETP
|
Cardiovascular Disease
Cancer
|
|
Dalcetrapib (JTT-705) is an orally active cholesteryl ester transfer protein (CETP) inhibitor with IC50s of 204.6 nM and 6 μM against recombinant human (rh) CETP and human plasma CETP, respectively.
|
-
- HY-16346
-
-
- HY-B0255
-
-
- HY-17463
-
-
- HY-13728B
-
|
(Rac)-ZD 9331; (Rac)-BGC9331
|
Thymidylate Synthase
|
Cancer
|
|
(Rac)-Plevitrexed ((Rac)-ZD 9331; (Rac)-BGC9331)?is a racemate of Plevitrexed. Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor. (Rac)-Plevitrexed is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-144303
-
|
|
Xanthine Oxidase
|
Metabolic Disease
|
|
Xanthine oxidase-IN-4 (compound 19a) is an orally active and potent xanthine oxidase (XO) inhibitor, with an IC50 of 0.039 μM. Xanthine oxidase-IN-4 exhibits hypouricemic potency in potassium oxonate induced hyperuricemia rats. Xanthine oxidase-IN-4 can be used for hyperuricemia and gout research.
|
-
- HY-153700
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Estrogen receptor modulator 8 (compound 4) is an orally active inhibitor of Estrogen Receptor/ERR α (IC50=0.437 nM, MCF-7 cells). Estrogen receptor modulator 8 inhibits MCF-7 cells proliferation with an IC50 value of 0.1 nM.
|
-
- HY-B0592S
-
-
- HY-157149
-
|
|
MAP4K
|
Cancer
|
|
DS21150768 is a potent, orally active HPK1 inhibitor. DS21150768 shows potent activity to enhance T-cell function. DS21150768 has anticancer effects.
|
-
- HY-137432A
-
|
BEY1107 trihydrochloride
|
CDK
|
Cancer
|
|
Avotaciclib (BEY1107) trihydrochloride is a potent and orally active inhibitor of cyclin dependent kinase 1 (CDK1). Avotaciclib trihydrochloride can be used for the research of locally advanced or metastatic pancreatic cancer.
|
-
- HY-117668
-
|
|
Elastase
|
Infection
Inflammation/Immunology
|
|
MDL 101146 is an orally active neutrophil elastase inhibitor. MDL 101146 inhibits neutrophil elastase for human with a Ki value of 25 nM. MDL 101146 can be used for the research of arthritis.
|
-
- HY-137432
-
|
BEY1107
|
CDK
|
Cancer
|
|
Avotaciclib (BEY1107) is a potent and orally active inhibitor of cyclin dependent kinase 1 (CDK1). Avotaciclib can be used for the research of locally advanced or metastatic pancreatic cancer.
|
-
- HY-10158
-
|
SKI-606
|
Src
Bcr-Abl
Autophagy
|
Cancer
|
|
Bosutinib is an orally active Src/Abl tyrosine kinase inhibitor with IC50 of 1.2 nM and 1 nM, respectively.
|
-
- HY-17020A
-
|
N-Butyldeoxynojirimycin hydrochloride; NB-DNJ hydrochloride; OGT 918 hydrochloride
|
Glucosylceramide Synthase (GCS)
|
Neurological Disease
|
|
Miglustat (N-Butyldeoxynojirimycin) hydrochloride is an orally active ceramide glucosyltransferase inhibitor. Miglustat hydrochloride can be used for the research of type I gaucher disease.
|
-
- HY-17020
-
|
N-Butyldeoxynojirimycin; NB-DNJ; OGT 918
|
Glucosylceramide Synthase (GCS)
|
Neurological Disease
|
|
Miglustat (N-Butyldeoxynojirimycin) is an orally active ceramide glucosyltransferase inhibitor. Miglustat can be used for the research of type I gaucher disease.
|
-
- HY-19522
-
|
MBX-8025
|
PPAR
|
Metabolic Disease
|
|
Seladelpar (MBX-8025) is an orally active, potent (50% effect concentration EC50 2 nM), and specific PPAR-δ agonist.
|
-
- HY-19687
-
|
CP73850
|
Aldose Reductase
|
Metabolic Disease
|
|
Zopolrestat (CP73850) is a potent, orally active aldose reductase (AR) inhibitor with an IC50 of 3.1 nM. Zopolrestat is used for the research of diabetic complications.
|
-
- HY-155731
-
|
|
Influenza Virus
|
Infection
|
|
Antiviral agent 35 (compound 4d) is an orally active and potent influenza virus inhibitor, acting function in the early stage of virus replication. Antiviral agent 35 inhibits ROS accumulation, autophagy and apoptosis induced by influenza virus, and also inhibits inflammatory response mediated by RIG-1 pathway in mouse model with pulmonary infection. Antiviral agent 35 shows little cytotoxicity with CC50 >800 μM in MDCK cells, and anti-H1N1 (A/Weiss/43) activity with EC50 of 2.28 μM.
|
-
- HY-134956B
-
|
|
YAP
|
Cancer
|
|
(R)-VT104 is the R-enantiomer of VT104. (R)-VT104 shows an IC50 value of 0.1-1 μΜ for firefly luciferase. VT104 is an orally active and pan-TEAD auto-palmitoylation inhibitor.
|
-
- HY-145887
-
|
|
Bcr-Abl
|
Neurological Disease
|
|
BCR-ABL1-IN-1 is a potent, orally active, and specific inhibitor of ABL kinase. BCR-ABL1-IN-1 has potential for elucidating the role of ABL kinases in the brain in non-clinical studies.
|
-
- HY-13672
-
-
- HY-131723
-
|
|
Cytochrome P450
|
Metabolic Disease
|
|
Pregnenolone 16α-carbonitrile is an orally active prototypical and effective rodent-PXR activator. Pregnenolone 16α-carbonitrile, a synthetic steroid, induces cytochrome P450 3A expression. Pregnenolone 16α-carbonitrile exhibits increased resistance to subsequent stressful insults.
|
-
- HY-44132
-
|
RS 42358-197
|
5-HT Receptor
|
Neurological Disease
|
|
Dehydro Palonosetron (RS 42358-197) is a potent, seslective and orally active 5-HT3 receptor antagonist. Dehydro Palonosetron has no effect on the activities of 5-HT1 receptors, 5-HT2 receptors or 5-HT4 receptors.
|
-
- HY-112102
-
|
SSHB
|
Others
|
Metabolic Disease
|
|
(22S,23S)-Homobrassinolide is one of the most active brassinosteroids in inducing plant growth in various plant bioassay systems. (22S,23S)-Homobrassinolide shows Akt-dependent anabolic activity in rat skeletal muscle cells. Orally active.
|
-
- HY-145598
-
|
HMPL-523
|
Syk
|
Cancer
|
|
Sovleplenib (HMPL-523) is a highly potent, orally available and selective SYK inhibitor with an IC50 of 25 nM. Anti-tumor activity. Sovleplenib can be used for the research of immune thrombocytopenia (ITP).
|
-
- HY-135655
-
|
SPR720 disodium; pVXc-486 disodium
|
Bacterial
|
Infection
|
|
Fobrepodacin (SPR720) disodium is an orally active and potent phosphate proagent of SPR719 (VXc-486; HY-12930). Fobrepodacin disodium has potent bactericidal activities in vivo.
|
-
- HY-136447
-
ASP4132
1 Publications Verification
|
AMPK
|
Cancer
|
|
ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models.
|
-
- HY-B0698A
-
|
Sch-39720 dihydrate
|
Bacterial
Antibiotic
|
Infection
|
|
Ceftibuten (Sch-39720) dihydrate, an antibiotic, is an orally active cephalosporin, possesses potent activity in vitro against a wide range of gram-negative and certain gram-positive pathogens.
|
-
- HY-134661A
-
CVN424
1 Publications Verification
|
GPR6
|
Neurological Disease
|
|
CVN424 is an orally active and selective GPR6 inverse agonist with a Ki of 9.4 nM and an EC50 of 38 nM. CVN424 is brain-penetrant and has the potential for Parkinson disease research.
|
-
- HY-12717
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
Phentolamine is a potent, selective and orally active α1 adrenergic and α2 adrenergic receptor antagonist. Phentolamine can be used for the research of erectile dysfunction.
|
-
- HY-139399
-
|
JNJ-67856633
|
MALT1
|
Cancer
|
|
Safimaltib (JNJ-67856633) is an orally active, first-in-class, potent, selective and allosteric MALT1 protease inhibitor. Safimaltib in some cases lead to tumor stasis.
|
-
- HY-148617
-
-
- HY-W133967
-
-
- HY-15454
-
|
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-119868
-
|
Butoxamin
|
Adrenergic Receptor
|
Metabolic Disease
|
|
Butaxamine (Butoxamin) is a potent, selective and orally active β2-adrenoceptor antagonist. Butaxamine shows antiosteoporotic activity.
|
-
- HY-133937
-
|
|
Bacterial
HIV
|
Infection
|
|
Sulfametrole is an orally active and potent antibacterial. Sulfametrole can be used for infections research, such as HIV, severe pneumonia and UTIs (urinary tract infections).
|
-
- HY-132294
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
GNE-502 is an orally active and potent degrader for estrogen receptor (ER). GNE-502 can be used for the research of breast cancer.
|
-
- HY-16747
-
|
SHP625 chloride; LUM001 chloride; Lopixibat chloride
|
Apical Sodium-Dependent Bile Acid Transporter
|
Metabolic Disease
|
|
Maralixibat (SHP625) chloride is an orally active ileal bile acid transporter (IBAT) inhibitor. Maralixibat chloride can be used for the research of rare cholestatic liver diseases including Alagille syndrome (ALGS), progressive familial intrahepatic cholestasis (PFIC) and biliary atresia.
|
-
- HY-148238
-
|
|
IRAK
|
Inflammation/Immunology
|
|
GNE-2256 (molecule 19) is an orally active IRAK4 (Interleukin 1 receptor associated kinase 4) inhibitor (IRAK4 Ki=1.4 nM; IL-6 IC50=190 nM).
|
-
- HY-105303
-
|
|
PARP
|
Cancer
|
|
CEP-9722, the proagent of CEP-8983, is a selective and orally active PARP-1 and PARP-2 inhibitor with IC50s of 20 nM and 6 nM, respectively. CEP-9722 has anticancer effects.
|
-
- HY-130628
-
|
|
PAK
|
Cancer
|
|
PAK4-IN-1 (Compound 19) is a potent, selective, orally active PAK4 inhibitor with robust anti-tumor efficacy in vivo. PAK4-IN-1 is stable under both acidic and neutral conditions.
|
-
- HY-151899
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
A3AR modulator 1 (MRS8054) is an orally active A3 adenosine receptor (A3AR) (Adenosine Receptor) positive allosteric modulator (PAM). A3AR modulator 1 greatly enhances Cl-IB-MECA-stimulated [ 35S]GTPγS binding Emax.
|
-
- HY-109189
-
|
BPI-7711
|
EGFR
|
Cancer
|
|
Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity.
|
-
- HY-10439
-
|
|
PGE synthase
|
Inflammation/Immunology
|
|
HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX.
|
-
- HY-12661A
-
|
|
PERK
Autophagy
|
Cancer
|
|
AMG PERK 44 is an orally active and highly selective PERK inhibitor with an IC50 of 6 nM. AMG PERK 44 has 1000-fold and 160-fold selectivity over GCN2 (IC50=7300 nM) and B-Raf (IC50 >1000 nM), respectively. AMG PERK 44 induces autophagy.
|
-
- HY-N7560
-
|
|
Keap1-Nrf2
|
Inflammation/Immunology
Neurological Disease
|
|
Safranal is an orally active main component of Saffron (Crocus sativus) and is responsible for the unique aroma of this spice. Safranal has neuroprotective and anti-inflammatory effects and has the potential for Parkinson’s disease research.
|
-
- HY-105124A
-
-
- HY-105040C
-
|
LY2140023 hydrochloride
|
mGluR
|
Neurological Disease
|
|
Pomaglumetad methionil hydrochloride (LY2140023 hydrochloride) is an orally active, methionine prodrug of the selective mGlu2/3 receptor agonist LY404039. Pomaglumetad methionil hydrochloride has the potential for schizophrenia research.
|
-
- HY-N0420
-
|
Wormwood acid
|
Endogenous Metabolite
|
Neurological Disease
|
|
Succinic acid is a potent and orally active anxiolytic agent. Succinic acid is an intermediate product of the tricarboxylic acid cycle. Succinic acid can be used as a precursor of many industrially important chemicals in food, chemical and pharmaceutical industries.
|
-
- HY-149278
-
-
- HY-120643
-
|
|
11β-HSD
|
Metabolic Disease
|
|
BMS-823778 hydrochloride is a potent, selective and orally active 11β-HSD1 inhibitor with an IC50 of 2.3 nM against human 11β-HSD1.
|
-
- HY-153007
-
|
|
Dihydrofolate reductase (DHFR)
|
Infection
|
|
DHFR-IN-5 is a potent and orally active dihydrofolate reductase (DHFR) inhibitor with a Ki value of 0.54 nM for quadruple mutant Plasmodium falciparum DHFR. DHFR-IN-5 shows anti-malaria activity.
|
-
- HY-B0249
-
|
2',3'-Dideoxyinosine; ddI
|
HIV
Reverse Transcriptase
|
Infection
|
|
Didanosine (2',3'-Dideoxyinosine; ddI) is a a potent and orally active dideoxynucleoside analogue, and also is a potent nucleoside reverse transcriptase inhibitor. Didanosine shows antiretroviral activity for HIV.
|
-
- HY-139204
-
-
- HY-103706
-
|
|
Autophagy
Apoptosis
|
Cancer
|
|
ROC-325 is a potent and orally active autophagy inhibitor with a strong anticancer activity. ROC-325 induces the deacidification of lysosomes, accumulation of autophagosomes, and disrupted autophagic flux. ROC-325 also induces renal cell carcinoma apoptosis.
|
-
- HY-147066
-
|
|
DYRK
|
Cancer
|
|
Dyrk1A-IN-4 (compound 48) is a potent and orally active DYRK1A and DYRK2 inhibitor with IC50s of 2 nM and 6 nM, respectively. Dyrk1A-IN-4 has anticancer effects.
|
-
- HY-151591
-
|
|
Phosphatase
|
Metabolic Disease
|
|
SPAA-52 is an orally active, competitive and reversible low-molecular-weight protein tyrosine phosphatase (LMW-PTP) inhibitor (IC50=4 nM, Ki=1.2 nM). SPAA-52 can be used in diabete research.
|
-
- HY-144606
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Mu opioid receptor antagonist 1 (compound 19) is a selective and orally active μ opioid receptor (MOR) ligand with an Ki value of 0.58 nM and an EC50 of 1.15 nM. Orally administrating with Mu opioid receptor antagonist 1 increases intestinal motility during morphine-induced constipation. Mu opioid receptor antagonist 1 can be used for researching opioid-induced constipation (OIC).
|
-
- HY-139590A
-
|
BOS-172738 hemiadipate; DS-5010 hemiadipate
|
RET
PDGFR
|
Cancer
|
|
Zeteletinib (BOS-172738; DS-5010) hemiadipate is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib hemiadipate shows exquisite potency for the wild type RET, RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib hemiadipate has potent antitumor activity.
|
-
- HY-156078
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-32 (compound f26) is a reversible, noncompetitive and orally active α-glucosidase inhibitor with an IC50 value of 3.07 μM. α-Glucosidase-IN-32 complex with α-glucosidase through hydrogen bonds and hydrophobic interactions, led to changes in the conformation and secondary strictures of α-glucosidase and further the inhibition of the enzymatic activity. α-Glucosidase-IN-32 can be used for diabetic disease research.
|
-
- HY-139590
-
|
BOS-172738; DS-5010
|
RET
PDGFR
|
Cancer
|
|
Zeteletinib (BOS-172738; DS-5010) is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib shows exquisite potency for the wild type RET, RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib has potent antitumor activity.
|
-
- HY-10777
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
EMD 495235 is a potent and orally active coagulation factor Xa inhibitor with an IC50 of 5.5 nM and a Ki of 6.8 nM. EMD 495235 shows anticoagulant activities.
|
-
- HY-107013
-
|
|
MMP
|
Inflammation/Immunology
|
|
CP-544439 is a potent and orally active matrix metalloproteinase-13 (MMP-13) inhibitor with an IC50 of 0.75 nM.
|
-
- HY-16158
-
|
Wy-4508; Aminocyclohexylpenicillin; Ciclacillin
|
Bacterial
Antibiotic
|
Infection
|
|
Cyclacillin (Wy-4508) is an orally active aminopenicillin antibiotic, shows antibacterial activity against a wide range of gram-positive and gram-negative pathogens.
|
-
- HY-108287
-
|
|
Others
|
Endocrinology
|
|
Trithiozine is an orally active antisecretory and antiulcer agent. Trithiozine can be used for the research of peptic ulcer disease and hypersecretory disorders.
|
-
- HY-107355
-
|
|
Others
|
Inflammation/Immunology
|
|
Letosteine is an orally active, potent and safe expectorant. Letosteine dissolves bronchial mucus and reduces respiratory inflammation symptoms, and restores gas exchanges and natural defense mechanisms in the lung. Letosteine can be used for acute or chronic respiratory diseases (such as bronchopneumopathies) research[1][2][3].
|
-
- HY-137978
-
|
GNS561
|
Others
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
|
Ezurpimtrostat (compound 2-2) is a potent and orally active anti-fibrotic agent. Ezurpimtrostat can be used for the research of fibrosis, cancer, autophagy and cathepsins B (CTSB), L (CTSL) and D (CTSD) related diseases (extracted from patent WO2020048694 A1).
|
-
- HY-144064
-
|
|
Adenosine Receptor
|
Cancer
|
|
Adenosine receptor antagonist 2 is an orally active A2a/A2b adenosine receptor antagonist with IC50s of 1 nM and 3 nM, respectively. Adenosine receptor antagonist 2 has anti-tumor activity.
|
-
- HY-106584
-
|
Clospipramine
|
Dopamine Receptor
|
Neurological Disease
|
|
Mosapramine (Clospipramine) is an orally active and potent dopamine receptor antagonist with high affinity to dopamine receptor subtypes 2, 3 and 4, and with moderate affinity for the 5-HT 2 receptor. Mosapramine shows antipsychotic activity and can be used in schizophrenia research.
|
-
- HY-130126
-
|
SCO-792
|
Others
|
Others
|
|
Sucunamostat hydrate (SCO-792) is an orally active and reversible enteropeptidase inhibitor with IC50s of 4.6 nM and 5.4 nM for rat enteropeptidase and human enteropeptidase, respectively. Sucunamostat hydrate can slowly dissociate from enteropeptidase in vitro and inhibit protein digestion in vivo.
|
-
- HY-10449
-
|
TS 071
|
SGLT
|
Metabolic Disease
|
|
Luseogliflozin (TS 071) is a potent, selective, orally active sodium-dependent glucose cotransporter (SGLT) 2 inhibitor, with an IC50 of 2.26 nM, about 1765-fold selectivity over SGLT1 (IC50, 3990 nM). Luseogliflozin has the protential for researching type 2 diabetes.
|
-
- HY-A0287S
-
|
Clomiphene-d5 (hydrochloride)
|
Isotope-Labeled Compounds
|
Others
|
|
Clomifene-d5 (hydrochloride) is a deuterium labeled Clomifene. Clomifene is an orally active compound used for infertility. Clomifene is a simple, relatively safe, easily administered and well-tolerated efficacious compound to induce ovulation[1].
|
-
- HY-141411A
-
|
(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-120160
-
|
CP-86325
|
PPAR
|
Metabolic Disease
Neurological Disease
|
|
Darglitazone (CP-86325), a thiazolidinedione, is a potent, selective, and orally active PPAR-γ agonist. Darglitazone is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research.
|
-
- HY-B1355
-
|
|
Bacterial
COX
|
Infection
Inflammation/Immunology
|
|
Oxyphenbutazone monohydrate is a Phenylbutazone (HY-B0230) metabolite, with anti-inflammatory effect. Oxyphenbutazone monohydrate is an orally active non-selective COX inhibitor. Oxyphenbutazone monohydrate selectively kills non-replicating Mycobaterium tuberculosis.
|
-
- HY-14554
-
|
LY2140023
|
mGluR
|
Neurological Disease
|
|
Pomaglumetad methionil anhydrous (LY2140023) is an orally active, methionine prodrug of the selective mGlu2/3 receptor agonist LY404039. LY2140023 has the potential for schizophrenia research.
|
-
- HY-116524
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
PF-04781340 is a potent and selective 5-HT2C receptor agonist. PF-04781340 is orally available and have central nervous system penetrant profile.
|
-
- HY-120049
-
|
|
Others
|
Inflammation/Immunology
|
|
TAK-603 is a potent and orally active antirheumatic agent. TAK-603 inhibits Thl-type cytokine production. TAK-603 has the potential for the research of adjuvant arthritis.
|
-
- HY-148456
-
-
- HY-110132
-
-
- HY-124240
-
-
- HY-108492
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
TC-SP 14 (compound 14) is an orally active and potent S1P1 agonist (EC50 = 0.042 μM) with minimal activity at S1P3 (EC50 = 3.47 μM). TC-SP 14 significantly reduces blood lymphocyte counts and attenuates a delayed type hypersensitivity (DTH) response to antigen challenge.
|
-
- HY-B0317S1
-
|
|
Isotope-Labeled Compounds
|
Cancer
|
|
Amlodipine-d4 is a deuterium labeled Amlodipine (HY-B0317). Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer.
|
-
- HY-19415A
-
|
|
Phospholipase
|
Metabolic Disease
|
|
SB-435495 hydrochloride is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM.
|
-
- HY-103692
-
|
|
STAT
|
Cancer
|
|
STX-0119 is a selective, orally active STAT3 dimerization inhibitor. STX-0119 inhibits STAT3 transcription with an IC50 of 74 μM.
|
-
- HY-15127
-
|
13-cis-Retinoic acid
|
RAR/RXR
Endogenous Metabolite
Autophagy
|
Cancer
|
|
Isotretinoin (13-cis-Retinoic acid) is an orally active vitamin A derivative and is often be used for the research of severe acne. Isotretinoin also shows anticancer activity.
|
-
- HY-106084
-
|
T-2525; RO 19-5247; Cefterame
|
Bacterial
|
Infection
|
|
Cefteram (T-2525) is the free acid of Cefteram pivoxil (HY-106571), which is an orally active cephalosporin ester. Cefteram potently targets to the enteropathogenic Enterobacteriaceae and Vibrionaceae.
|
-
- HY-144300
-
|
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-123863
-
|
|
FAAH
|
Neurological Disease
|
|
SSR411298 is an orally active, selective and reversible fatty acid amide hydrolase (FAAH) inhibitor. SSR411298 has the potential for post-traumatic stress disorder research.
|
-
- HY-19415B
-
|
|
Phospholipase
|
Metabolic Disease
|
|
SB-435495 ditartrate is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM.
|
-
- HY-B1271
-
|
G-28315
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Sulfinpyrazone (G-28315) is an orally active and potent uricosuric agent for chronic and intermittent gouty arthritis. Sulfinpyrazone has antithrombotic and platelet inhibitory effects.
|
-
- HY-155130
-
|
|
Parasite
|
Infection
|
|
Antimalarial agent 31 (compound 7k) is an orally active Plasmodium falciparum aspartic protease plasmepsin X (PMX) inhibitor.
|
-
- HY-W013989
-
|
|
Epoxide Hydrolase
|
Cardiovascular Disease
|
|
1,3-Dicyclohexylurea (DCU) is an orally active and potent sEH (soluble epoxide hydrolase) inhibitor. Oral Delivery of 1,3-Dicyclohexylurea nanosuspension enhances exposure and lowers blood pressure in hypertensive Rats.
|
-
- HY-B1751F
-
-
- HY-106158
-
|
|
SGLT
|
Metabolic Disease
|
|
T-1095 is a selective and orally active Na +-glucose cotransporter (SGLT) inhibitor with IC50s of 22.8 µM and 2.3 µM for human SGLT1 and SGLT2, respectively. T-1095 can be used for diabetes research.
|
-
- HY-16748
-
|
ABT-126
|
nAChR
|
Neurological Disease
|
|
Nelonicline (ABT-126) is an orally active and selective α7 nicotinic receptor agonist with high affinity to α7 nAChRs in human brain (Ki=12.3 nM). Nelonicline is used for the research of shizophrenia and Alzheimer's disease.
|
-
- HY-105003
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
ST 1535 is a potent and orally active A2A adenosine receptor antagonist. ST 1535 shows antiparkinsonian activity and antitremorigenic effects. ST 1535 has the potential for the research of Parkinson’s disease.
|
-
- HY-12146
-
|
|
Others
|
Metabolic Disease
|
|
ELOVL6-IN-2 is a potent, orally active and selective ELOVL6 inhibitor. ELOVL6-IN-2 inhibits mouse ELOVL6 activities, with an IC50 value of 34 nM.
|
-
- HY-148570
-
|
|
Phosphoglycerate Dehydrogenase (PHGDH)
|
Cancer
|
|
PHGDH-IN-3 is an orally active phosphoglycerate dehydrogenase (PHGDH) inhibitor. PHGDH-IN-3 inhibits PHGDH with an IC50 value of 2.8 μM. PHGDH-IN-3 can be used for the research of cancer.
|
-
- HY-105124
-
-
- HY-118134
-
|
|
Others
|
Cancer
|
|
Hepln-13 is a potent and orally active Hepsin inhibitor with an IC50 of 0.33 µM. Hepln-13 can be used for the research of metastatic prostate cancer.
|
-
- HY-147367
-
-
- HY-144706
-
|
|
TAM Receptor
|
Cancer
|
|
Axl-IN-3 is a potent, selective and orally active AXL kinase inhibitor with an IC50 of 41.5 nM. Axl-IN-3 has lower inhibition of other kinases.
|
-
- HY-131065
-
|
|
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-107703
-
|
|
iGluR
|
Neurological Disease
|
|
CGP 39551 is a potent, orally active, competitive N-methyl-D-aspartate (NMDA) receptor antagonist with potent anticonvulsant activity. CGP 39551 shows measurable inhibitory activity at both L-[ 3H]-glutamate (Ki=8.4 μM).
|
-
- HY-19672
-
|
BAY 19-8004
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Lirimilast (BAY 19-8004) is a potent, selective and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 value of 49 nM. Lirimilast can be used for the treatment of asthma or chronic obstructive pulmonary disease (COPD). Lirimilast has potently anti-inflammatory properties.
|
-
- HY-115936
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-9 (compound 7a) is a potent, selective, and orally active inhibitor of COX-2 with an IC50 of 10.17 uM. COX-2-IN-9 has higher COX-2 selectivity than Celecoxib. COX-2-IN-9 shows good in vivo anti-inflammatory and low ulcerogenic activity.
|
-
- HY-115934
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-7 (compound 4a) is a potent, selective, and orally active inhibitor of COX-2 with an IC50 of 6.585 uM. COX-2-IN-7 has higher COX-2 selectivity than Celecoxib. COX-2-IN-7 shows good in vivo anti-inflammatory and low ulcerogenic activity.
|
-
- HY-117833
-
|
|
Monoamine Oxidase
|
Inflammation/Immunology
|
|
PXS-4681A is a potent, selective, irreversible and orally active semicarbazide-sensitive amine oxidase (SSAO; VAP-1) inhibitor with a Ki of 37 nM. PXS-4681A shows highly selectivity over related amine oxidases, ion channels, and seven-transmembrane domain receptors. PXS-4681A has anti-inflammatory effects.
|
-
- HY-115935
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-8 (compound 6a) is a potent, selective, and orally active inhibitor of COX-2 with an IC50 of 6.585 uM. COX-2-IN-8 has higher COX-2 selectivity than Celecoxib. COX-2-IN-8 shows good in vivo anti-inflammatory and low ulcerogenic activity.
|
-
- HY-144870
-
|
|
STAT
|
Cancer
|
|
STAT3-IN-7, an aryl sulfonamido azetidine compound, is an orally active STAT3 inhibitor. STAT3-IN-7 has anticancer activities (WO2021016333A1, H182).
|
-
- HY-13768C
-
|
SKF 104864A hydrochloride hydrate; NSC 609669 hydrochloride hydrate
|
Topoisomerase
Apoptosis
Autophagy
|
Cancer
|
|
Topotecan hydrochloride hydrate is an orally active and potent Topoisomerase I inhibitor. Topotecan hydrochloride hydrate induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan hydrochloride hydrate shows anticancer activity.
|
-
- HY-135891
-
|
|
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-156290
-
-
- HY-109027
-
|
N91115
|
GSNOR
CFTR
|
Inflammation/Immunology
|
|
Cavosonstat (N91115) is an orally active S-nitrosoglutathione reductase (GSNOR) inhibitor. Cavosonstat is a CFTR stabilizer, and can be used for cystic fibrosis research.
|
-
- HY-118189
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
Misoprostol acid is an active metabolite of Misoprostol. Misoprostol is a synthetic analogue of prostaglandin E1 (PGE1), extensively absorbed, and undergoes rapid de-esterification to Misoprostol acid in the gastrointestinal tract after oral administration. Misoprostol can be used for non-steroidal anti-inflammatory drug-induced (NSAID) gastric ulcers. Misoprostol is an oral agent used to induce labor.
|
-
- HY-137978A
-
|
GNS561 hydrochloride
|
Others
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
|
Ezurpimtrostat hydrochloride (compound 2-3) is a potent and orally active anti-fibrotic agent. Ezurpimtrostat hydrochloride reduces significantly the liver fibrosis in DEN (diethyl nitrosamine) cirrhotic rat model. Ezurpimtrostat hydrochloride can be used for the research of fibrosis, cancer, autophagy and cathepsins B (CTSB), L (CTSL) and D (CTSD) related diseases .
|
-
- HY-B1751
-
-
- HY-19985
-
|
|
EGFR
|
Cancer
|
|
PF-06459988 is an orally activity, irreversible and mutant-selective inhibitor of EGFR mutant forms. PF-06459988 demonstrates high potency and specificity to the T790M-containing double mutant EGFRs. PF-06459988 can be used for the research of cancer.
|
-
- HY-16748A
-
|
ABT-126 citrate
|
nAChR
|
Neurological Disease
|
|
Nelonicline (ABT-126) citrate is an orally active and selective α7 nicotinic receptor agonist with high affinity to α7 nAChRs in human brain (Ki=12.3 nM). Nelonicline citrate is used for the research of shizophrenia and Alzheimer's disease.
|
-
- HY-B0024
-
|
NM441
|
Bacterial
Antibiotic
|
Infection
|
|
Prulifloxacin (NM441) is an orally active fluoroquinolone antibiotic with a broad spectrum of activity against Gram-positive and -negative bacteria. Prulifloxacin is a proagent of a thiazeto-quinoline carboxylic acid derivative Ulifloxacin (NM394). Prulifloxacin has the potential for lower urinary tract infections and exacerbations of chronic bronchitis.
|
-
- HY-143430
-
|
|
CDK
|
Cancer
|
|
(S)-LY3177833 ((S)-Example 2) is an orally active CDC7 kinase inhibitor. (S)-LY3177833 shows broad in vitro anticancer activity.
|
-
- HY-109144
-
|
DWP-16001
|
SGLT
|
Metabolic Disease
|
|
Enavogliflozin (DWP-16001), an antidiabetic agent, is an orally active, best-in-class and selective sodium-glucose cotransporter-2 (SGLT-2) inhibitor.
|
-
- HY-143430A
-
|
|
CDK
|
Cancer
|
|
(S)-LY3177833 ((S)-Example 2) hydrate is an orally active CDC7 kinase inhibitor. (S)-LY3177833 hydrate shows broad in vitro anticancer activity.
|
-
- HY-138564
-
|
|
NO Synthase
|
Inflammation/Immunology
|
|
NOS-IN-1 is a potent and orally active NO synthase (NOS) isoforms inhibitor with IC50s of 0.1 μM, 1.1 μM, and 0.2 μM for human iNOS (hiNOS), heNOS and hnNOS, respectively.
|
-
- HY-A0213
-
|
Tiludronic acid
|
Proton Pump
|
Inflammation/Immunology
|
|
Tiludronate (Tiludronic Acid), an orally active bisphosphonate, can act an osteoregulator. Tiludronate is used for the research of the metabolic bone disorders. Tiludronate is a potent inhibitor of the osteoclast vacuolar H(+)-ATPase. Antiresorptive and anti-inflammatory properties.
|
-
- HY-B1196
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Tiapride hydrochloride is a selective and orally active D2 and D3 dopamine receptors antagonist with IC50 values of 110-320 nM and 180 nM, respectively. Tiapride hydrochloride shows anti-dyskinetic activity and anxiolytic activity. Tiapride hydrochloride is a neuroleptic agent.
|
-
- HY-N0420A
-
|
Wormwood acid tromethamine
|
Endogenous Metabolite
|
Neurological Disease
|
|
Succinic acid tromethamine is a potent and orally active anxiolytic agent. Succinic acid tromethamine is an intermediate product of the tricarboxylic acid cycle. Succinic acid tromethamine can be used as a precursor of many industrially important chemicals in food, chemical and pharmaceutical industries.
|
-
- HY-W027951
-
|
DMTU
|
Reactive Oxygen Species
|
Inflammation/Immunology
|
|
N,N'-Dimethylthiourea (DMTU), isolated from Allium sativum, is an orally active scavenger of hydroxyl radical (•OH) and blocks •OH production by activated neutrophils in vitro. N,N'-Dimethylthiourea protects against water-immersion restraint stress (WIRS)-induced gastric mucosal lesions in rats by exerting its antioxidant action including •OH scavenging and anti-inflammatory action.
|
-
- HY-155463
-
|
|
Interleukin Related
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NLRP3-IN-25 (compound 32) is an orally available NLRP3 inhibitor with anti-inflammatory activity. NLRP3-IN-25 attenuates renal injury in doxorubicin-induced glomerulonephritis in mice. NLRP3-IN-25 inhibits IL-1β secretion in THP-1 cells with an IC50 of 21 nM.
|
-
- HY-153704
-
|
|
CDK
|
Cancer
|
|
CDK4/6-IN-17 (compound 12) is an orally active CDK4/6 inhibitor with IC50 ranging of 10-100 nM in BE(2) cells. CDK4/6-IN-17 inhibits tumor growth in COLO205 xenograft model.
|
-
- HY-115989
-
|
|
HCV
|
Infection
|
|
HCV-IN-38 is a potent, selective and orally active HCV inhibitor (EC50=15 nM, SI=431). HCV-IN-38 has high anti-HCV activity and low cytotoxicity. HCV-IN-38 has a good safety and oral pharmacokinetic profile.
|
-
- HY-145653
-
-
- HY-113926
-
|
|
Guanylate Cyclase
|
Cardiovascular Disease
|
|
BAY 60-2770 is a potent, selective, and orally active soluble guanylyl cyclase (sGC) activator. BAY 60-2770 increases the activity of sGC in a nitric oxide-independent manner. BAY 60-2770 shows antifibrotic effect.
|
-
- HY-16759
-
|
MK-8931
|
Beta-secretase
|
Neurological Disease
|
|
Verubecestat (MK-8931) is an orally active, high-affinity BACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM. Verubecestat effectively reduces Aβ40 and has the potential for Alzheimer's Disease.
|
-
- HY-A0213A
-
|
Tiludronic acid disodium
|
Proton Pump
|
Inflammation/Immunology
|
|
Tiludronate (Tiludronic Acid) disodium, an orally active bisphosphonate, can act an osteoregulator. Tiludronate is used for the research of the metabolic bone disorders. Tiludronate is a potent inhibitor of the osteoclast vacuolar H(+)-ATPase. Antiresorptive and anti-inflammatory properties.
|
-
- HY-16730
-
|
PF-6450567
|
Parasite
|
Infection
|
|
Sarolaner (PF-6450567) is an orally active and broad-spectrum ectoparasiticide. Sarolaner is an isoxazoline compound which shows efficacy against fleas and ticks on dogs, with a LC80 value of 0.3 μg/mL against C. felis and a LC100 value of 0.003 μg/mL against O. turicata.
|
-
- HY-B1751A
-
-
- HY-B1751E
-
-
- HY-131349
-
|
|
CCR
|
Cancer
|
|
CCR4-351 is an orally active, potent and selective CCR4 antagonist. CCR4-351, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 has antitumor activity.
|
-
- HY-131349A
-
|
|
CCR
|
Cancer
Metabolic Disease
|
|
CCR4-351 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4-351 hydrochloride, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 hydrochloride has antitumor activity.
|
-
- HY-139970
-
|
|
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-P0217
-
-
- HY-107923
-
|
N1-Acetylsulfisoxazole
|
Bacterial
|
Infection
|
|
Sulfisoxazole acetyl (N1-Acetylsulfisoxazole), a Sulfisoxazole derivative, is an orally active dihydropteroate synthase inhibitor. Sulfisoxazole acetyl has an antibacterial action.
|
-
- HY-152947
-
|
|
Others
|
Metabolic Disease
|
|
ELOVL6-IN-4 is a potent, selective, and orally active long chain fatty acid elongase 6 (ELOVL6) inhibitor with IC50s of 79 nM and 94 nM for human and mouse ELOVL6, respectively. ELOVL6-IN-4 shows excellent selectivity over the other human ELOVL subtypes (ELOVL1, -2, -3, and -5) and mouse ELOVL3.
|
-
- HY-115923
-
|
|
Others
|
Inflammation/Immunology
|
|
Nur77 modulator 2, a Nur77 modulator (Kd of 0.35 μM), is a potent and orally active inflammation inhibitor. Nur77 modulator 2 modulates the colocalization of Nur77 at mitochondria.
|
-
- HY-144444
-
|
|
EGFR
|
Cancer
|
|
NSC381467 is a potent and orally active inhibitor of EGFR tyrosine kinase (EGFR-TK). NSC381467 has strong antiproliferative activities. NSC381467 has the potential for the research of cancer diseases.
|
-
- HY-144445
-
|
|
EGFR
|
Cancer
|
|
NSC114126 is a potent and orally active inhibitor of EGFR tyrosine kinase (EGFR-TK). NSC114126 has strong antiproliferative activities. NSC114126 has the potential for the research of cancer diseases.
|
-
- HY-19926
-
|
RG-7602
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
GDC-0425 (RG-7602) is an orally available, highly selective small molecule ChK1 inhibitor. GDC-0425 can be used for the research of various malignancies.
|
-
- HY-145574
-
|
WX-0593
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
|
Cancer
|
|
Iruplinalkib (WX-0593) is a potent, selective, and orally active inhibitor of ALK and ROS1 tyrosine kinase. Iruplinalkib (WX-0593) shows favorable safety and promising antitumor activity in advanced NSCLC with ALK or ROS1 rearrangement.
|
-
- HY-120438
-
|
|
PI3K
Akt
|
Inflammation/Immunology
|
|
TASP0415914 is a potent and orally active PI3Kγ inhibitor with an IC50 of 29 nM. TASP0415914 also shows potent Akt inhibitory activities with an IC50 of 294 nM. TASP0415914 can be used for inflammatory diseases research.
|
-
- HY-15991A
-
|
AZD1722 hydrochloride; RDX5791 hydrochloride
|
Na+/H+ Exchanger (NHE)
|
Metabolic Disease
|
|
Tenapanor (AZD1722) hydrochloride is a potent and orally active sodium/hydrogen exchanger isoform 3 (NHE3) inhibitor. Tenapanor hydrochloride reduces intestinal phosphate absorption predominantly through reduction of passive paracellular phosphate flux. Tenapanor hydrochloride has the potential for the research of hyperphosphatemia.
|
-
- HY-107725
-
|
|
Neuropeptide Y Receptor
|
Metabolic Disease
|
|
BIBO3304 TFA is a potent, orally active, and selective neuropeptide Y (NPY) Y1 receptor antagonist, with subnanomolar affinity for both the human and the rat Y1 receptor (IC50=0.38 and 0.72 nM, respectively).
|
-
- HY-15991
-
|
AZD1722; RDX5791
|
Na+/H+ Exchanger (NHE)
|
Metabolic Disease
|
|
Tenapanor (AZD1722) is a potent and orally active sodium/hydrogen exchanger isoform 3 (NHE3) inhibitor. Tenapanor reduces intestinal phosphate absorption predominantly through reduction of passive paracellular phosphate flux. Tenapanor has the potential for the research of hyperphosphatemia.
|
-
- HY-11059
-
|
|
Phospholipase
|
Inflammation/Immunology
|
|
sPLA2 inhibitor 1, a D-tyrosine derivative, is an orally active, potent secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 29 nM for human nonpancreatic secretory PLA2 isoform IIa (hnpsPLA2-IIa). sPLA2 inhibitor 1 has anti-inflammatory activity.
|
-
- HY-15010
-
|
|
Oxytocin Receptor
Vasopressin Receptor
|
Endocrinology
|
|
L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (Ki=19 nM) and vasopressin V1a receptor (Ki=3.7 nM).
|
-
- HY-11091
-
|
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-116278
-
|
|
STAT
|
Cancer
|
|
HJC0149 is a potent and orally active inhibitor of signal transducer and activator of transcription 3 (STAT3).
|
-
- HY-B0232
-
|
UK 68789
|
Potassium Channel
|
Cardiovascular Disease
|
|
Dofetilide (UK 68789), as a class III antiarrhythmic agent, is an orally active, potent and specific IKr blocker. Dofetilide can be used for the research of cardiovascular disease.
|
-
- HY-A0161A
-
|
Clofedanol hydrochloride; Calmotusin hydrochloride; NSC 113595 hydrochloride
|
Others
|
Infection
|
|
Chlophedianol (Clofedanol) hydrochloride is an orally active and potent antitussive agent. Chlophedianol hydrochloride can be used for the research of acute cough due to upper respiratory tract infections (URIs).
|
-
- HY-153702
-
|
|
JAK
|
Cancer
|
|
JAK-IN-27 (compound 1) is an orally active and potent JAKS family kinase inhibitor with IC50s of 3.0 nM (TYK2), 7.7 nM (JAK1), 629.6 nM (JAK3), respectively. JAK-IN-27 inhibits IFN-α2B-induced phosphorylation of STAT3 in Jurkat cells (IC50=23.7 nM).
|
-
- HY-19569
-
|
ABT-494
|
JAK
|
Inflammation/Immunology
|
|
Upadacitinib (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib (ABT-494) can be used for several autoimmune disorders research.
|
-
- HY-A0213B
-
|
Tiludronic acid disodium hemihydrate
|
Proton Pump
|
Metabolic Disease
|
|
Tiludronate (Tiludronic Acid) disodium hemihydrate, an orally active bisphosphonate, can act an osteoregulator. Tiludronate disodium hemihydrate is used for the research of the metabolic bone disorders. Tiludronate disodium hemihydrate is a potent inhibitor of the osteoclast vacuolar H +-ATPase. Antiresorptive and anti-inflammatory properties.
|
-
- HY-12410
-
|
|
Itk
|
Inflammation/Immunology
|
|
GNE-9822 is a potent, orally active and selective ITK inhibitor with a Ki value of 0.7 nM, and an EC50 value of 354.5 nM. GNE-9822 has good ADME properties. GNE-9822 can be used in research of asthma.
|
-
- HY-102057
-
|
TD-8954
|
5-HT Receptor
|
Others
|
|
Felcisetrag (TD-8954) is an orally active, potent and selective 5-HT4 receptor agonist with gastrointestinal prokinetic properties. Felcisetrag has high affinity (pKi =9.4) for human 5-HT4(c) receptors.
|
-
- HY-123058
-
|
|
PI3K
Autophagy
|
Cancer
|
|
Vps34-IN-4 (compound 19) is a potent, selective, and orally active inhibitor of VPS34. Vps34-IN-4 inhibits the autophagy in vivo. Autophagy is a dynamic process that regulates lysosomal-dependent degradation of cellular components.
|
-
- HY-103226
-
|
|
Aminopeptidase
|
Inflammation/Immunology
|
|
SC-57461A is a potent, orally active, nonpeptide, and selective inhibitor of Leukotriene A4 (LTA4) hydrolase with IC50s of 2.5 nM, 3 nM, and 23 nM for recombinant human, mouse, and rat LTA4 hydrolase, respectively.
|
-
- HY-16759A
-
|
MK-8931 TFA
|
Beta-secretase
|
Neurological Disease
|
|
Verubecestat (MK-8931) TFA is an orally active, high-affinity BACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM. Verubecestat TFA effectively reduces Aβ40 and has the potential for Alzheimer's Disease.
|
-
- HY-145924
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
BAY 2666605 is an orally active PDE3A and PDE3B inhibitor with IC50s of 87 nM and 50 nM, respectively. BAY 2666605 is a PDE3A-SLFN12 complex inducer (WO2019025562A1; example 135).
|
-
- HY-115922
-
|
|
COX
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 10 (compound 30) is a tilomisole-based benzimidazothiazole derivative. Anti-inflammatory agent 10 expresses activity on COX-2 enzyme more than COX-1. Anti-inflammatory agent 10 is orally active.
|
-
- HY-147987
-
|
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
FFA1 agonist-1 (Compound 17a) is an orally active fatty acid receptor 1 (FFA1) agonist with an EC50 of 0.75 μM. FFA1 agonist-1 can be used for type 2 diabetes mellitus research.
|
-
- HY-13768
-
|
SKF 104864A; NSC 609669
|
Topoisomerase
Autophagy
Apoptosis
|
Cancer
|
|
Topotecan (SKF 104864A; NSC 609669) is an orally active and potent Topoisomerase I inhibitor. Topotecan induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan shows anticancer activity.
|
-
- HY-115921
-
|
|
COX
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 9 (compound 28) is a tilomisole-based benzimidazothiazole derivative. Anti-inflammatory agent 9 expresses activity on COX-2 enzyme more than COX-1. Anti-inflammatory agent 9 is orally active.
|
-
- HY-100888
-
|
TAK-931
|
CDK
|
Cancer
|
|
Simurosertib (TAK-931) is an orally active, selective and ATP-competitive cell division cycle 7 (CDC7) kinase inhibitor, with an IC50 of <0.3 nM. Simurosertib has anti-cancer activity.
|
-
- HY-147402
-
|
D-0502
|
Estrogen Receptor/ERR
|
Cancer
|
|
Taragarestrant (D-0502) is a potent, orally active and selective estrogen receptor degrader (SERD). Taragarestrant shows potent activity in various ER+ breast cancer cell lines and xenograft models.
|
-
- HY-B0758
-
|
|
Others
|
Inflammation/Immunology
|
|
Troxipide is an orally active defensive factor-enhancing therapeutic agent for gastritis and gastric ulcer (GU). Troxipide is a non-antisecretory gastro protective agent with antiulcer, anti-inflammatory and mucus-secreting properties.
|
-
- HY-14691
-
|
BAY 869766; RDEA119
|
MEK
|
Cancer
|
|
Refametinib (BAY 869766; RDEA119) is an orally available, potent, non-ATP-competitive, selective, allosteric MEK1/MEK2 inhibitor with IC50s of 19 nM and 47 nM, respectively.
|
-
- HY-132293
-
|
|
DNA-PK
|
Cancer
|
|
BAY-8400 is an orally active, potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (IC50=81 nM). BAY-8400 can be used for the research of cancer.
|
-
- HY-121778
-
|
Melitracene; N 7001; Trausabun
|
Others
|
Neurological Disease
|
|
Melitracen (Melitracene) is an orally active tricyclic antidepressant and it is also a bipolar thymoleptic with activating properties. Melitracen inhibits 3H-5-HT and 14H-5-HT with IC50s of 670 nM and 5500 nM, respectively. Melitracen can be used for the research of depression and anxiety.
|
-
- HY-B1751D
-
-
- HY-123812
-
|
|
Histamine Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
PF-03654764 is an orally active, selective histamine H3 receptor antagonist with Ki values of 1.2 nM and 7.9 nM for human H3 and rat H3 in whole cell assay, respectively. The combination of PF-03654764 and Fexofenadine (HY-B0801A) has the potential for allergic rhinitis research.
|
-
- HY-123840
-
|
|
GABA Receptor
|
Neurological Disease
|
|
MRK-623 (Compound 14k) is an orally active, high-affinity GABAA receptor agonist, with the Ki values of 0.85 nM, 3.7 nM, 4.0 nM, and 0.53 nM for α1, α2, α3, and α5, respectively. MRK-623 shows anxiolytic effect.
|
-
- HY-133127
-
|
|
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
-
|
|
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-A0276
-
|
|
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Gentamicin sulfate, an orally active aminoglycoside antibiotic, inhibits the growth of both gram-positive and gram-negative bacteria and to inhibit several strains of mycoplasma in tissue culture. Gentamicin sulfate inhibits DNase I with an IC50 of 0.57 mM.
|
-
- HY-109149
-
|
KP 106
|
Others
|
Neurological Disease
|
|
Lomardexamfetamine (KP 106) is an orally active central nervous system stimulant composed of d-amphetamine and a ligand. Lomardexamfetamine can be used for the research of attention-deficit hyperactivity disorder.
|
-
- HY-107722
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
SCH 221510 is a potent, orally active and selective NOP (nociceptin opioid receptor) agonist, with an EC50 of 12 nM and Ki of 0.3 nM. SCH 221510 shows an anxiolytic-like effect.
|
-
- HY-14771A
-
-
- HY-106968
-
|
|
iGluR
|
Neurological Disease
|
|
ZD-9379 is a potent, orally active, and brain penetrant full antagonist at the glycine site of the NMDA receptor. ZD-9379 has neuroprotective effect.
|
-
- HY-B1526
-
|
Thioacetazone; Amithiozone
|
Bacterial
Antibiotic
|
Infection
|
|
Thiacetazone (Thioacetazone) is a thiourea-containing antitubercular agent and is an orally active antibiotic. Thiacetazone has antibacterial action, which inhibits growth of Mycobacterium tuberculosis H37Rv with a MIC value of 0.1 μg/mL.
|
-
- HY-146615
-
|
|
TAM Receptor
|
Cancer
|
|
Axl-IN-6 (compound 14) is an orally active and potent AXL inhibitor. Axl-IN-6 is well tolerated and significantly inhibits the tumor growth in MV-4-11 subcutaneous xenograft model.
|
-
- HY-133141
-
|
|
Others
|
Cancer
|
|
DI-87 is an orally active and selective deoxycytidine kinase (dCK) inhibitor with an EC50 of 10.2 nM. DI-87 has antitumor activity and is used in combination therapy against tumors expressing dCK.
|
-
- HY-136977
-
|
|
Histone Methyltransferase
|
Cancer
|
|
EEDi-5285 is an exceptionally potent and orally active embryonic ectoderm development (EED) inhibitor with an IC50 value of 0.2 nM for binds to the EED protein. EEDi-5285 has anti-cancer activity.
|
-
- HY-B0281A
-
-
- HY-151484
-
|
|
Parasite
|
Infection
|
|
Anti-infective agent 4 (compound 73) is an orally active inhibitor of Trypanosoma cruzi with an IC50 value of 0.016 μM. Anti-infective agent 4 effectively reduces parasite burden in vivo. Anti-infective agent 4 can be used for the research of infection.
|
-
- HY-14900
-
|
GRC-10693
|
Cannabinoid Receptor
|
Inflammation/Immunology
|
|
Tedalinab (GRC-10693) is a potent, orally active, and selective cannabinoid receptor 2 (CB2) agonist. Tedalinab has >4700-fold functional selectivity for CB2 over CB1. Tedalinab has potential for neuropathic pain and osteoarthritis treatment.
|
-
- HY-19631B
-
|
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
-
|
NS-018
|
JAK
|
Cancer
|
|
Ilginatinib (NS-018) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
|
-
- HY-122856
-
|
|
TGF-β Receptor
|
Cancer
|
|
AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth .
|
-
- HY-103266
-
|
|
Aurora Kinase
|
Cancer
|
|
TC-A 2317 hydrochloride is an orally active Aurora A kinase inhibitor (Ki=1.2 nM). TC-A 2317 hydrochloride exhibits excellent selectivity to Aurora B kinase (Ki=101 nM) and other 60 kinases, good cell permeability and good PK profile. Antitumor activity.
|
-
- HY-14853
-
|
YM150
|
Factor Xa
Ser/Thr Protease
|
Cardiovascular Disease
|
|
Darexaban (YM150) is a potent, selective and orally active factor Xa (FXa) inhibitor with an IC50 of 54.6 nM. Darexaban shows high selectivity against other related serine proteases, such as trypsin, thrombin, and kallikrein. Darexaban has anticoagulant and antithrombotic effects.
|
-
- HY-19631
-
|
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-106268A
-
|
|
Gap Junction Protein
|
Inflammation/Immunology
|
|
Larazotide acetate is a peptide which is an orally active zonulin antagonist. Larazotide acetate shows antiviral activity to varicella-zoster virus (VZV) with EC50s of 44.14 and 59.06 μM for strain OKA and 07-1, respectively. Larazotide acetate can be used for the research of celiac disease and infection.
|
-
- HY-141513
-
|
|
Thyroid Hormone Receptor
|
Neurological Disease
|
|
NH-3 is an orally active, reversible thyroid hormone receptor (THR) antagonist with an IC50 of 55 nM. NH-3, a derivative of the selective thyromi-metic GC-1, inhibits binding of thyroid hormones to their receptor and that inhibits cofactor recruitment.
|
-
- HY-106316
-
|
|
GABA Receptor
|
Neurological Disease
|
|
CGS 20625 is a potent, selective and orally active partial agonist for the central benzodiazepine receptor. CGS 20625 inhibits [3H]-flunitrazepam binding to central benzodiazepine receptors with an IC50 of 1.3 nM. CGS 20625 can be used for the research of pentylenetetrazol-induced seizures.
|
-
- HY-B0693
-
-
- HY-P5971
-
|
|
Melanocortin Receptor
|
Metabolic Disease
|
|
TCMCB07, a cyclic nonapeptide peptide, is an orally active and brain-penetrant melanocortin receptor 4 (MC4R) antagonist. TCMCB07 plays an important role in cachexia.
|
-
- HY-147402A
-
|
D-0502 meglumine
|
Estrogen Receptor/ERR
|
Cancer
|
|
Taragarestrant (D-0502) meglumine is a potent, orally active and selective estrogen receptor degrader (SERD). Taragarestrant meglumine shows potent activity in various ER+ breast cancer cell lines and xenograft models.
|
-
- HY-132297
-
|
|
PARP
|
Cancer
|
|
PARP1-IN-5 is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 can be used for the research of cancer.
|
-
- HY-132297A
-
|
|
PARP
|
Cancer
|
|
PARP1-IN-5 dihydrochloride is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer.
|
-
- HY-10716A
-
|
|
GlyT
|
Neurological Disease
|
|
PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research.
|
-
- HY-100641
-
|
Hydroxytolbutamide
|
Potassium Channel
Autophagy
|
Cancer
Metabolic Disease
|
|
4-Hydroxytolbutamide (Hydroxytolbutamide) is a metabolite of Tolbutamide. 4-Hydroxytolbutamide is metabolized by CYP2C8 and CYP2C9. Tolbutamide is a first generation potassium channel blocker and a sulfonylurea oral antidiabetic.
|
-
- HY-13611
-
|
BN 80915
|
Topoisomerase
|
Cancer
|
|
Diflomotecan (BN 80915) is a potent and orally active inhibitor of topoisomerase I. Diflomotecan (BN 80915) causes enhanced plasma stability and has the superior preclinical anti-tumour activity compared with other established compounds.
|
-
- HY-106608
-
|
Litoralon
|
Thyroid Hormone Receptor
|
Neurological Disease
|
|
Glutaurine containing glutamine and taurine residues is an orally active hormone of the parathyroid. Glutaurine, as a hormone, is isolated from parathyroid gland oxyphil cells. Glutaurine can be used for the research of antiepileptic and anti-amnesia.
|
-
- HY-141638
-
|
Methyl-IQ
|
Others
|
Cancer
|
|
Me-IQ (Methyl-IQ), an orally active heterocyclic amine, is carcinogenic and mutagenic. Me-IQ is several hundred-fold more mutagenic in liver than in lung microsomal preparations from uninduced mice and rabbits.
|
-
- HY-112094S
-
|
|
Ser/Thr Protease
|
Cardiovascular Disease
|
|
WNK-IN-11-d3 is an orally active, selective and potent With-No-Lysine (WNK) kinase inhibitor. WNK-IN-11-d3 is effective at regulating cardiovascular homeostasis[1].
|
-
- HY-119816
-
|
|
Others
|
Cardiovascular Disease
|
|
Piretanide is an oral active, relatively safe and effective diuretic. Piretanide has the potential for the research of congestive heart failure with a potential advantage of having potassium-sparing properties. Piretanide can also be used for the research of hypertension[1][2].
|
-
- HY-126248
-
|
|
PARP
|
Cancer
|
|
Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model.
|
-
- HY-14904A
-
|
|
Influenza Virus
SARS-CoV
|
Infection
|
|
Umifenovir hydrochloride is a potent, orally active broad-spectrum antiviral with activity against a number of enveloped and non-enveloped viruses. Umifenovir hydrochloride is used as an anti-influenza virus agent. Umifenovir hydrochloride could effectively inhibit the fusion of virus with host cells. Umifenovir hydrochloride is an efficient inhibitor of SARS-CoV-2 in vitro. Anti-inflammatory activity.
|
-
- HY-141496
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
A-77636 is an orally active, potent, selective and long-acting dopamine D1 receptor agonist (pEC50 = 8.13; EC50 = 1.1 nM). A-77636 shows the highest affinity (pKi = 7.40 ± 0.09; Ki = 39.8 nM) for the dopamine D1 receptor. A-77636 shows antiparkinsonian activity.
|
-
- HY-122058A
-
|
|
CXCR
HIV
|
Infection
Inflammation/Immunology
|
|
KRH-3955 hydrochloride is an orally bioavailable CXCR4 antagonist. KRH-3955 hydrochloride inhibits SDF-1α binding to CXCR4 with an IC50 of 0.61 nM. KRH-3955 hydrochloride is also a highly potent and selective inhibitor of X4 HIV-1, with an EC50 of 0.3 to 1.0 nM.
|
-
- HY-110129
-
|
SR-46349 hemifumarate; SR 46349B
|
5-HT Receptor
|
Neurological Disease
|
|
Eplivanserin (SR-46349) hemifumarate is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin hemifumarate displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C.
|
-
- HY-152074
-
|
|
CD73
|
Cancer
|
|
D73-IN-14 is a potent, selective and orally active CD73 inhibitor with an IC50 value of 0.17 nM. CD73-IN-14 increases the number of tumor-infiltrating CD8 + cells and shows anti-tumor activity. CD73-IN-14 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-10792
-
|
SR-46349
|
5-HT Receptor
|
Neurological Disease
|
|
Eplivanserin (SR-46349) is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C.
|
-
- HY-138684
-
-
- HY-138684A
-
-
- HY-A0171
-
|
Ba-30803 free base
|
Others
|
Neurological Disease
|
|
Benzoctamine is an orally active and potent psychoactive agent which possesses tranquillizing properties. Benzoctamine increases the turnover rate of catecholamines. Benzoctamine enhances the [3H]noradrenaline uptake in the rat heart. Benzoctamine also accelerated the disappearance of intracisternally injected [3H]noradrenaline.
|
-
- HY-108024A
-
|
KAF156 hydrochloride; GNF156 hydrochloride
|
Parasite
|
Infection
|
|
Ganaplacide (KAF156) hydrochloride is a first-in-class, orally active imidazolopiperazine antimalarial agent. Ganaplacide hydrochloride is active against a broad range of Plasmodium species, including drug-resistant parasites. Ganaplacide hydrochloride is parasiticidal against both asexual and sexual blood stages as well as the liver stages of the parasite.
|
-
- HY-113603
-
|
|
CRFR
|
Cancer
|
|
Tildacerfont is a potent and orally active corticotrophin-releasing factor type 1 (CRF1) receptort antagonis. Tildacerfont effectively reduces adrenocorticotropic hormone (ACTH) and adrenal androgen levels. Tildacerfont has favourable safety profile. Tildacerfont can be used for researching congenital adrenal hyperplasia.
|
-
- HY-115920
-
|
|
COX
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 8 (compound 13) is a tilomisole-based benzimidazothiazole derivative. Anti-inflammatory agent 8 expresses activity on COX-2 enzyme more than COX-1 with an IC50 of 0.09 nM. Anti-inflammatory agent 8 is orally active.
|
-
- HY-132987
-
|
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-139485
-
|
|
Apelin Receptor (APJ)
|
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-135825
-
|
|
Autophagy
|
Neurological Disease
|
|
TFEB activator 1 is an orally effective, mTOR-independent activator of TFEB. TFEB activator 1 significantly promotes the nuclear translocation of Flag-TFEB with an EC50 of 2167 nM. TFEB activator 1 enhances autophagy without inhibiting the mTOR pathway and has the potential for neurodegenerative diseases treatment.
|
-
- HY-146267
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERα degrader 5 (Compound 40) is a selective, orally bioavailable estrogen receptor (ER) degrader (SERD) with an EC50 of 1.1 nM against ERα. ERα degrader 5 shows antitumor effect in vivo.
|
-
- HY-N2059
-
|
|
Others
|
Cancer
|
|
Santalol is a mixture of α and β-isomer santalol. α-santalol is isolated from sandalwood oil. α-santalol is a promising anti-cancer agent against cancers such as oral, breast, prostate and skin cancer.
|
-
- HY-106050
-
|
Wy 18251
|
Others
|
Cancer
Inflammation/Immunology
|
|
Tilomisole (Wy 18251) is a benzimidazothiazole experimental agent with anti-inflammatory activity. Tilomisole causes less agranulocytosis than levamisole, but retains immunomodulating capabilities. Tilomisole is orally active. Tilomisole has the potential for the research of cancer and inflammation.
|
-
- HY-111145
-
|
|
Androgen Receptor
|
Cancer
|
|
RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer.
|
-
- HY-145919
-
-
- HY-147642
-
|
|
Others
|
Inflammation/Immunology
|
|
ChemR23-IN-4 (Compound 13) is a potent and orally efficacious ChemR23 inhibitor with an IC50 of 17 nM against human ChemR23.
|
-
- HY-147567
-
|
|
ATM/ATR
DNA-PK
PI3K
|
Cancer
|
|
ATR-IN-15 (compound 1) is an orally active and potent ATR kinase inhibitor, with an IC50 of 8 nM. ATR-IN-15 also inhibits human colon tumor cells LoVo, DNA-PK and PI3K, with IC50 values of 47, 663 and 5131 nM, respectively.
|
-
- HY-B0464
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cardiovascular Disease
|
|
Hydralazine hydrochloride is a orally active antihypertensive agent, reduces peripheral resistance directly by relaxing the smooth muscle cell layer in arterial vessel. Hydralazine hydrochloride has antioxidant activity, as well as inhibits ROS release and O2 ·- generation with an IC50 value of 9.53 mM and 1.19 mM, respectively.
|
-
- HY-146662
-
|
|
PGE synthase
|
Inflammation/Immunology
|
|
HPGDS inhibitor 3 is an orally active and highly potent peripherally restricted hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with IC50 value of 9.4 nM and EC50 of 42 nM, respectively. HPGDS inhibitor 3 exhibits good selectivity, good pharmacokinetic parameters in mouse, rat, and dog, and no CNS toxicity. HPGDS inhibitor 3 has anti-inflammatory activity.
|
-
- HY-110117
-
|
|
Integrin
Interleukin Related
|
Inflammation/Immunology
|
|
BIRT 377 is a potent amd orally bioavailable inhibitor of the interaction between intercellular adhesion molecule-1 (ICAM-1) and lymphocyte function-associated antigen-1 (LFA-1), with a Ki of 25.8 nM. BIRT 377 also inhibits the production of IL-2 in vivo. BIRT 377 can be used for researching inflammatory and immune disorders.
|
-
- HY-105286
-
|
|
11β-HSD
|
Metabolic Disease
|
|
BI-135585 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor with an IC50 of 13 nM. BI-135585 exhibits >1000-fold selectivity over other hydroxysteroid dehydrogenases. BI-135585 can be used for type 2 diabetes research.
|
-
- HY-125415
-
|
|
PGE synthase
|
Inflammation/Immunology
|
|
PF-4693627 is a potent, selective and orally bioavailable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor (IC50=3 nM) for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA).
|
-
- HY-134885
-
|
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-128442
-
|
Phenyl hydrogen sulfate
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Phenyl sulfate is an orally active gut microbiota-derived metabolite. Phenyl sulfate induces albuminuria and podocyte damage in experimental models of diabetes. Phenyl sulfate can be used as a disease marker and future therapeutic target in diabetic kidney disease.
|
-
- HY-147263
-
|
CC-11050
|
Phosphodiesterase (PDE)
|
Infection
Inflammation/Immunology
|
|
Dovramilast (CC-11050) is an orally active phosphodiesterase 4 (PDE4) inhibitor and can reduce the inflammatory response and improves Isoniazid (INH)-mediated bacillary clearance from the lungs. Dovramilast, as an adjunct, is used for the research of tuberculosis (TB).
|
-
- HY-W010144
-
|
|
COX
Lipoxygenase
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Phenidone, an orally active dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), ameliorates rat paralysis in experimental autoimmune encephalomyelitis. Phenidone is a potent hypotensive agent in the spontaneously hypertensive rat. Phenidone is used as a photographic developer.
|
-
- HY-19263
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
BMS-193884 is a selective, orally active, and competitive ETA antagonist with 10000-fold greater affinity for the human ETA receptor (Ki=1.4 nM) than for the ETB receptor.
|
-
- HY-10527C
-
|
Bay 57-9352 mesylate
|
VEGFR
PDGFR
c-Kit
|
Cancer
|
|
Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active VEGFR2, VEGFR3, PDGFα, and c-Kit inhibitor with IC50s of 6 nM, 4 nM, 15 nM and 1 nM, respectively.
|
-
- HY-10309
-
|
RO 48-3657
|
Integrin
|
Cardiovascular Disease
|
|
Sibrafiban (RO 48-3657) is the orally active, nonpeptide, double-proagent of Ro 44-3888 and a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban inhibits platelet aggregation.
|
-
- HY-P5971A
-
|
|
Melanocortin Receptor
|
Metabolic Disease
|
|
TCMCB07 TFA, a cyclic nonapeptide peptide, is an orally active and brain-penetrant melanocortin receptor 4 (MC4R) antagonist. TCMCB07 TFA plays an important role in cachexia.
|
-
- HY-112939
-
|
MCI-196; Colestimide
|
Others
|
Metabolic Disease
|
|
Colestilan (MCI-196) is a non-absorbed, non-calcium-based phosphate binder and is also a non-metallic, anion exchange resin. Colestilan is orally active and can be used for hypercholesterolaemia research.
|
-
- HY-150545
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE-IN-21 (Compound I-8) is a potent, selective and orally active AChE inhibitor with an IC50 of 2.66 nM. AChE-IN-21 displays excellent BBB permeability in vitro.
|
-
- HY-107798
-
|
|
Bacterial
|
Infection
|
|
Potassium guaiacolsulfonate hemihydrate is an orally active expectorant used for acute respiratory tract infections. Potassium guaiacolsulfonate hemihydrate helps loosen mucus and used for a cough caused by the common cold, infections or allergies in combination with other agents.
|
-
- HY-10262
-
|
|
IGF-1R
Insulin Receptor
Apoptosis
|
Cancer
Endocrinology
|
|
BMS-536924 is an orally active, competitive and selective insulin-like growth factor receptor (IGF-1R) kinase and insulin receptor (IR) inhibitor with IC50s of 100 nM and 73 nM, respectively. BMS-536924 has anti-cancer activity.
|
-
- HY-106268
-
|
|
Gap Junction Protein
|
Infection
Inflammation/Immunology
|
|
Larazotideis a peptide which is an orally active zonulin antagonist. Larazotide shows antiviral activity to varicella-zoster virus (VZV) with EC50s of 44.14 and 59.06 μM for strain OKA and 07-1, respectively. Larazotide can be used for the research of celiac disease and infection.
|
-
- HY-100413
-
|
|
Proton Pump
|
Inflammation/Immunology
|
|
CS-526 is a potent, selective, reversible and orally active acid pump antagonist. CS-526 inhibits H +,K +-ATPase activity. CS-526 inhibits gastric acid secretion and prevents esophageal lesions. CS-526 has the potential for the research of gastroesophageal reflux disease.
|
-
- HY-145925C
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
(S,R)-CFT8634 is a selective and orally active BRD9 protein degrader. (S,R)-CFT8634 has the potential for the research of disorders mediated by BRD9, including but not limited to abnormal cellular proliferation (extracted from patent WO2021178920A1, compound 176).
|
-
- HY-103595
-
|
Mepirizole; DA-398
|
Others
|
Inflammation/Immunology
|
|
Epirizole (Mepirizole) is an orally active NSAID (nonsteroidal anti-inflammatory agent). Epirizole shows anti-inflammatory activity, and can be used in chronic rheumatoid arthritis research.
|
-
- HY-149695
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-91 (compound 9) is an orally available EGFR inhibitor with blood-brain permeability. EGFR-IN-91 inhibits EGFR L858R/C797S and EGFR exon 19del/C797S, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants.
|
-
- HY-101918
-
|
|
Others
|
Cardiovascular Disease
|
|
DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
|
-
- HY-108060A
-
|
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-108060
-
-
- HY-15155
-
MLN0905
4 Publications Verification
|
Polo-like Kinase (PLK)
|
Cancer
|
|
MLN0905 is a potent, orally active Polo-like kinase 1 (PLK1) inhibitor. MLN0905 has inhibitory potency against PLK1 with an IC50 value of 2 nM. MLN0905 can be used for the research of cancer.
|
-
- HY-103250
-
|
|
Antibiotic
|
Infection
|
|
PF-945863 is an orally active macrolide antibiotic that can be used for the research of multidrug resistant respiratory tract bacterial strains.
|
-
- HY-121097
-
-
- HY-132981
-
|
|
P2X Receptor
|
Neurological Disease
|
|
Lu AF27139 is a potent, selective, and orally active antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 has rodent-active and CNS-penetrant character. Lu AF27139 has the potential for the research of CNS diseases.
|
-
- HY-122028
-
|
|
11β-HSD
|
Metabolic Disease
|
|
HSD-016 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with IC50 values of 11, 1 and 8 nM against human, mouse and rat 11β-HSD1, respectively. HSD-016 can be used for type 2 diabetes research.
|
-
- HY-A0279
-
|
Pristinamycine
|
Bacterial
Antibiotic
|
Infection
|
|
Pristinamycin, produced by Streptomyces pristinaespiralis, is an orally active streptogramin-like antibiotic consisting of two chemically unrelated components: Pristinamycin I (PI) and Pristinamycin II (PII). Pristinamycin is highly active against many antibiotic-resistant pathogens, particularly Gram-positive bacteria, including Methicillin-resistant Staphylococcus aureus (MRSA), Vancomycin-resistant S. aureus (VRSA) and Enterococcus faecium (VREF).
|
-
- HY-14904
-
|
|
SARS-CoV
Influenza Virus
|
Infection
|
|
Umifenovir is a potent, orally active broad-spectrum antiviral agent with activity against a number of enveloped and non-enveloped viruses. Umifenovir is used as an anti-influenza virus agent. Umifenovir could effectively inhibit the fusion of virus with host cells. Umifenovir is an efficient inhibitor of SARS-CoV-2 in vitro. Umifenovir shows anti-inflammatory activity.
|
-
- HY-146223A
-
|
|
Others
|
Cancer
|
|
(3R,10R,14aS)-AZD4625 is the inactive isomer of AZD4625 (HY-146223), and can be used as an experimental control. AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS G12C. AZD4625 has high oral bioavailability.
|
-
- HY-10322
-
|
BIBX 1382
|
EGFR
|
Cancer
|
|
Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50=3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity.
|
-
- HY-18010
-
|
|
Btk
BCRP
|
Inflammation/Immunology
|
|
PCI 29732 is a potent, orally active, reversible BTK inhibitor with Ki app values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase. PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2.
|
-
- HY-152104
-
|
|
FGFR
|
Cancer
|
|
FGFR-IN-9 (Compound 19) is a potent, reversible and orally active FGFR inhibitor with an IC50 of 17.1, 29.6, 30.7, 46.7 and 64.3 nM against FGFR4 WT, FGFR3, FGFR4 V550L, FGFR2 and FGFR1, respectively.
|
-
- HY-16950
-
|
(Z)-4-Hydroxytamoxifen; trans-4-Hydroxytamoxifen; (Z)-Afimoxifene
|
Estrogen Receptor/ERR
|
Cancer
|
|
4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) is an orally active, selective estrogen receptor modulator (SERM). 4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) induces CRISPR/Cas9 systems based on ER mediated nucleus translocation.
|
-
- HY-19490A
-
|
(S)-AQW-051
|
nAChR
|
Neurological Disease
|
|
(S)-VQW-765 ((S)-AQW-051) is an orally active, selective and effective α7 nicotinic ACh receptor (nAChR) partial agonist. (S)-VQW-765 has potential applications in cognitive disorders related to neurological diseases, such as Alzheimer's disease or schizophrenia.
|
-
- HY-14240
-
|
PG 530742; PGE 530742; PGE 7113313
|
MMP
|
Inflammation/Immunology
|
|
PG 116800 (PG 530742) is an orally avtive MMP inhibitor. PG 116800 has high affinity for MMP-2, -3, -8, -9, -13, and -14, while having substantially lower affinity for MMP-1 and -7. PG 116800 can be used for knee osteoarthritis research.
|
-
- HY-15658
-
GSK2801
2 Publications Verification
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
GSK2801 is a potent, selective, orally active and cell active acetyl-lysine competitive BAZ2A and BAZ2B bromodomains inhibitor with Kd values of 136 nM and 257 nM, respectively. GSK2801 shows >50-fold selectivity for BAZ2A/B over BRD4.
|
-
- HY-105033
-
|
Pirfloxacin
|
Bacterial
|
Infection
|
|
Irloxacin (Pirfloxacin) is a quinolone antibacterial agent. Irloxacin shows greater activity with an acid pH. Irloxacin has a good in vitro antimicrobial spectrum against both gram-positive and gram-negative bacteria. Orally active.
|
-
- HY-14771
-
-
- HY-151196
-
|
|
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-118189S
-
|
|
Isotope-Labeled Compounds
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
Misoprostol acid-d5 is deuterium labeled Misoprostol acid. Misoprostol acid is an active metabolite of Misoprostol. Misoprostol is a synthetic analogue of prostaglandin E1 (PGE1), extensively absorbed, and undergoes rapid de-esterification to Misoprostol acid in the gastrointestinal tract after oral administration. Misoprostol can be used for non-steroidal anti-inflammatory drug-induced (NSAID) gastric ulcers[1]. Misoprostol is an oral agent used to induce labor[2].
|
-
- HY-101699A
-
|
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
AMG-076 is an orally bioavailable and selective MCHR1 antagonist. AMG-076 results in significant reduction in body weight gain in nonobese mice fed a high-fat diet and in high-fat diet-induced obese (DIO) mice.
|
-
- HY-109083
-
|
GS-9674
|
FXR
Autophagy
|
Inflammation/Immunology
|
|
Cilofexor (GS-9674) is a potent, selective and orally active nonsteroidal FXR agonist with an EC50 of 43 nM. Cilofexor has anti-inflammatory and antifibrotic effects. Cilofexor has the potential for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research.
|
-
- HY-146237
-
|
CC-99282
|
Ligands for E3 Ligase
Molecular Glues
|
Cancer
|
|
Golcadomide (CC-99282) is a potent and orally active cereblon (CRBN) E3 ligase modulator (CELMoD). Golcadomide co-opts CRBN to induce potent and targeted degradation of Ikaros and Aiolos. Golcadomide can be used for researching non-Hodgkin lymphomas.
|
-
- HY-117610A
-
|
Ro 32-0432; Ro 31-8830 hydrochloride
|
PKC
|
Inflammation/Immunology
|
|
Bisindolylmaleimide XI hydrochloride (Ro 32-0432) is a potent, selective and orally active PKC inhibitor with IC50s of 9 nM, 28 nM, 31 nM, 37 nM, and 108 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCε, respectively.
|
-
- HY-B0298
-
|
HS-592; Meclastine
|
Histamine Receptor
|
Neurological Disease
|
|
Clemastine (HS-592) is a potent and orally active histamine receptor H1 antagonist. Clemastine is an antihistamine mainly used for relieving symptoms of allergic reactions primarily by competing with histamine to bind H1 receptors. Anti-inflammatory effects.
|
-
- HY-117623
-
|
PF-249
|
AMPK
|
Metabolic Disease
|
|
PF-06685249 (PF-249) is a potent and orally active allosteric AMPK activator with an EC50 of 12 nM for recombinant AMPK α1β1γ1. PF-06685249 can be used for diabetic nephropathy research.
|
-
- HY-B0464A
-
|
|
Reactive Oxygen Species
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Hydralazine is a orally active antihypertensive agent, reduces peripheral resistance directly by relaxing the smooth muscle cell layer in arterial vessel. Hydralazine has antioxidant activity, as well as inhibits reactive oxygen species (ROS) release and O2 ·- generation with an IC50 value of 9.53 mM and 1.19 mM, respectively.
|
-
- HY-12776
-
GSK805
2 Publications Verification
|
ROR
|
Inflammation/Immunology
|
|
GSK805 is an orally active and CNS penetrant RORγt inhibitor. GSK805 inhibits RORγ and Th17 cells differentiation with pIC50 values of 8.4 and >8.2. GSK805 inhibits the function of Th17 cells. GSK805 can be used for the research of immunity.
|
-
- HY-132292
-
|
|
PROTACs
Androgen Receptor
|
Cancer
|
|
ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer.
|
-
- HY-13215
-
|
CI-1011; PD-148515
|
Acyltransferase
|
Cancer
|
|
Avasimibe (CI-1011; PD-148515) is an orally active acyl coenzyme A-cholesterol acyltransferase (ACAT; also called SOAT)) inhibitor with IC50s of 24 and 9.2 µM for ACAT1 and ACAT2, respectively. Avasimibe can be used for the research of prostate cancer.
|
-
- HY-151111
-
|
|
Renin
|
Cardiovascular Disease
|
|
SPH3127 (DRI 18) is a novel, highly potent, and orally active direct renin inhibitor (recombinant human-renin IC50=0.4 nM, human plasma renin activity IC50=0.45 nM). SPH3127 shows antihypertensive effect and can be used in essential hypertension research.
|
-
- HY-W013172
-
|
|
Progesterone Receptor
|
Endocrinology
|
|
Norgestimate, a synthetic progesterone analog, is an orally active progestin with highly selective progestational activity and minimal androgenicity. Norgestimate is used for an oral contraceptive. Norgestimate is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-100087
-
-
- HY-151881
-
|
|
Ras
|
Cancer
|
|
SOS1-IN-15 (Compound 37) is an orally active SOS1 inhibitor with an IC50 of 5 nM. SOS1-IN-15 is a promising agent candidate for the research of KRAS-driven cancer.
|
-
- HY-144676
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
pan-HER-IN-1 (Compound C5) is an irreversible, orally active pan-HER inhibitor with IC50 values of 0.38, 1.6, 2.2 and 3.5 nM against EGFR, HER4, EGFR T790M/L858R and HER2, respectively. pan-HER-IN-1 induces apoptosis and shows antitumor activities.
|
-
- HY-106993B
-
|
GT-2331 (enantiomer)
|
Histamine Receptor
|
Neurological Disease
|
|
Cipralisant (GT-2331) enantiomer is the enantiomer of Cipralisant (HY-106993), Cipralisant is an orally active, potent, selective, and high affinity histamine H3 receptor antagonist (rat Ki=0.47 nM). Cipralisant (enantiomer) is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-144677
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
pan-HER-IN-2 (Compound C6) is a reversible, orally active pan-HER inhibitor with IC50 values of 0.72, 2.0, 8.2 and 75.1 nM against EGFR, HER4, EGFR T790M/L858R and HER2, respectively. pan-HER-IN-2 induces apoptosis and shows antitumor activities.
|
-
- HY-145564A
-
|
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-121450
-
|
Loxtidine; AH-234844
|
Histamine Receptor
|
Cancer
|
|
Lavoltidine (Loxtidine) is an an orally active, irreversible and highly potent histamine H2-receptor antagonist. Lavoltidine strongly inhibits gastric acid secretion and also induces hypergastrinemia.
|
-
- HY-15879
-
-
- HY-141700
-
|
|
FATP
|
Metabolic Disease
|
|
FATP1-IN-2 (compound 12a), an arylpiperazine derivative, is an orally active fatty acid transport protein 1 (FATP1) inhibitor (human IC50=0.43 μM, mouse IC50=0.39 μM).
|
-
- HY-109177
-
|
QBW251
|
CFTR
|
Inflammation/Immunology
|
|
Icenticaftor (QBW251) is an orally active CFTR channel potentiator, with EC50s of 79 nM and 497 nM for F508del and G551D CFTR, respectively. Icenticaftor can be used for chronic obstructive pulmonary disease (COPD) and cystic fibrosis research.
|
-
- HY-13512
-
|
Camostat mesilate; FOY305; FOY-S980
|
Ser/Thr Protease
SARS-CoV
|
Infection
Inflammation/Immunology
|
|
Camostat mesylate (Camostat mesilate) is an orally active, synthetic serine protease inhibitor for chronic pancreatitis. Camostat mesylate, an inhibitor of TMPRSS2, shows antiviral activity against SARS-CoV-2. Camostat mesylate also inhibits the activity of prostasin, trypsin, and matriptase.
|
-
- HY-106647
-
|
|
Others
|
Inflammation/Immunology
|
|
Abacavir hydroxyacetate is an orally active inhibitor of IL-20 and PRINS. Abacavir hydroxyacetate reduces proliferation rate of skin in psoriasis as an immune modulator. Abacavir hydroxyacetate can be used for the research of inflammatory skin problems.
|
-
- HY-153168
-
|
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
Bemoradan (compound 10a) is an orally active and selective canine Phosphodiesterase (PDE) fraction III inhibitor. Bemoradan is a long-acting, potent, inotropic vasodilator and a novel cardiotonic agent, and can be used in congestive heart
failure research.
|
-
- HY-115506
-
|
|
TRP Channel
|
Neurological Disease
|
|
PF-05105679 is an orally active and selective TRPM8 antagonist with an IC50 of 103 nM. PF-05105679 has the potential for cold-related pain.
|
-
- HY-102051
-
|
|
IAP
|
Cancer
|
|
XIAP/cIAP1 antagonist-1 is a potent and orally active XIAP/cIAP1 antagonist with EC50s of 5.1 nM and 0.32 nM for XIAP and cIAP1, respectively. XIAP/cIAP1 antagonist-1 inhibits the tumor growth in dose-dependent manner in vivo.
|
-
- HY-19838
-
|
|
GPR139
|
Neurological Disease
|
|
JNJ-63533054 is a potent, selective and orally active GPR139 agonist with an EC50 of 16 nM for human GPR139 (hGPR139). JNJ-63533054 shows selective for GPR139 over other GPCRs, ion channels, and transporters. JNJ-63533054 can cross the blood-brain barrier (BBB).
|
-
- HY-18204A
-
|
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-150963
-
|
|
Renin
|
Cardiovascular Disease
|
|
Renin inhibitor-1 (compound 26) is a potent and orally active renin inhibitor with IC50s of 0.9, 1.8 nM for rh-renin and hPRA, respectively. Renin inhibitor-1 shows antihypertensive efficacy. Renin inhibitor-1 has the potential for the research of hypertension and cardiovascular/renal diseases.
|
-
- HY-14578
-
-
- HY-107354
-
|
|
Others
|
Cardiovascular Disease
|
|
Gepefrine is an orally active pressor agent and sympathomimetic agent. Gepefrine improves the early orthostatic disregulation of the arterial pressure.
|
-
- HY-147260B
-
|
(Rac)-SAGE-718
|
TRP Channel
|
Neurological Disease
|
|
(Rac)-Dalzanemdor ((Rac)-SAGE-718) is an isomer of Dalzanemdor (HY-147260). Dalzanemdor is an orally active and highly intrinsically active N-methyl-d-aspartate receptor (NMDAR)-positive allosteric modulator (PAM). Dalzanemdor can be used in the research of Huntington's disease.
|
-
- HY-15546
-
|
|
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-151485
-
|
|
Parasite
|
Infection
|
|
Anti-infective agent 5 (compound 74) is an orally active inhibitor of Trypanosoma cruzi with an IC50 value of 0.10 μM. Anti-infective agent 5 effectively reduces parasite burden in vivo. Anti-infective agent 5 can be used for the research of infection.
|
-
- HY-100606
-
|
(-)-Pindolol; (S)-(-)-Pindolol; S-Pindolol
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
l-Pindolol ((-)-pindolol) is a reversible, competitive and orally active 5-HT1A/1B antagonist. l-Pindolol is a partial β-adrenoceptor agonist. l-Pindolol can be used for the research of neurological disease.
|
-
- HY-145721
-
|
GED-0301
|
TGF-beta/Smad
|
Inflammation/Immunology
|
|
Mongersen (GED-0301) is a specific and orally active SMAD7 antisense oligonucleotide. Mongersen restores TGF-β1 activity leading to inhibition of inflammatory signals. Mongersen can attenuate Crohn's disease-like experimental colitis in mice.
|
-
- HY-15043
-
|
|
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-106608A
-
|
Litoralon TFA
|
Thyroid Hormone Receptor
|
Neurological Disease
|
|
Glutaurine (Litoralon) TFA containing glutamine and taurine residues is an orally active hormone of the parathyroid. Glutaurine (Litoralon) TFA, as a hormone, is isolated from parathyroid gland oxyphil cells. Glutaurine (Litoralon) TFA can be used for the research of antiepileptic and anti-amnesia.
|
-
- HY-109176
-
|
GDC-9545; RG6171
|
Estrogen Receptor/ERR
|
Cancer
|
|
Giredestrant (GDC-9545), a non-steroidal estrogen receptor (ER) ligand, is an orally active and selective ER antagonist. Giredestrant potently competes with Estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity.
|
-
- HY-N7697F
-
|
|
Others
|
Others
|
|
Chitobiose, a chitosan oligosaccharide, is a dimer of β-1,4-linked glucosamine units. Chitobiose has orally activity and high antioxidant activity.
|
-
- HY-152156
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 11 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 11 targets the Colchicine binding site on tubulin, inhibits tubulin polymerization, promotes mitotic blockade and apoptosis.
|
-
- HY-N8435
-
-
- HY-10563
-
|
MCI-9042 free acid
|
5-HT Receptor
|
Infection
|
|
Sarpogrelate (MCI-9042) is a new, specific orally active 5-HT2 receptor antagonist, Sarpogrelate increases platelet aggregation and has hemostasis effect, and can be used for the research of Buerger’s disease.
|
-
- HY-115494
-
|
Neladenoson bialanate hydrochloride; BAY-1067197 hydrochloride
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
Neladenoson dalanate (Neladenoson bialanate; BAY-1067197) hydrochloride is a orally active agonist precursor of partial Adenosine A1 Receptor. Neladenoson dalanate hydrochloride has a good pharmacokinetic and safety profile, can be used for the chronic heart diseases.
|
-
- HY-148074
-
|
RPT193
|
CCR
|
Inflammation/Immunology
|
|
Zelnecirnon (RPT193) is an orally active inhibitor of CCR4, blocks the recruitment of Th2 inflammatory immune cells into inflamed tissues. Zelnecirnon can be used for allergic inflammation in atopic dermatitis, asthma, and other diseases research.
|
-
- HY-123353
-
|
Neladenoson bialanate; BAY-1067197
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
Neladenoson dalanate (Neladenoson bialanate; BAY-1067197) is a orally active agonist precursor of partial Adenosine A1 Receptor. Neladenoson dalanate has a good pharmacokinetic and safety profile, can be used for the chronic heart diseases.
|
-
- HY-119402
-
|
BCL6-IN-8c
|
Bcl-2 Family
|
Cancer
|
|
TP-021 (BCL6-IN-8c) is a potent and orally active B-cell lymphoma 6 (BCL6)-corepressor interaction inhibitor with an IC50 of 0.10 µM in cell-free enzyme-linked immunosorbent assay.
|
-
- HY-103416
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
A-77636 hydrochloride is a potent, orally active, selective and long acting dopamine D1 receptor agonist (pKi=7.40; Ki=39.8 nM) with antiparkinsonian activity. A-77636 hydrochloride is functionally inactive at dopamine D2 receptor.
|
-
- HY-12413A
-
|
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
BMS-986118 is a potent, orally active, and selective GPR40 agonist with an EC50 of 0.07 µM. BMS-986118 has dual insulinotropic and GLP-1 secretory effects, resulting in robust plasma glucose lowering effects in acute animal models.
|
-
- HY-134772
-
|
|
STAT
Cytochrome P450
|
Inflammation/Immunology
|
|
AS1810722 is an orally active and potent STAT6 inhibitor with an IC50 of 1.9 nM. AS1810722 shows a good profile of CYP3A4 inhibition. AS1810722, a derivative of fused bicyclic pyrimidine, has the potential for allergic diseases such as asthma and atopic diseases research.
|
-
- HY-103689
-
|
|
Others
|
Others
|
|
Cucurbit[8]uril is a potent, low toxicity and orally active supramolecular inducer of protein heterodimerization. Cucurbit[8]uril induces heterodimerization of methylviologen and naphthalene functionalized proteins. Cucurbit[8]uril can induce energy transfer .
|
-
- HY-103345
-
-
- HY-121132
-
|
|
Others
|
Inflammation/Immunology
|
|
Butibufen is an orally active non-steroidal compound. Butibufen shows analgesic and antipyretic properties. Butibufen can be used for the research of inflammation.
|
-
- HY-N0586A
-
|
(+)-Laurelliptine hydrochloride
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
Norisoboldine hydrochloride is an orally active natural aryl hydrocarbon receptor (AhR) agonist. Norisoboldine hydrochloride, as a major isoquinoline alkaloid present in Radix Linderae, can be used for the research of Rheumatoid arthritis and Ulcerative colitis.
|
-
- HY-N0586
-
|
(+)-Laurelliptine
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
Norisoboldine is an orally active natural aryl hydrocarbon receptor (AhR) agonist. Norisoboldine, as a major isoquinoline alkaloid present in Radix Linderae, can be used for the research of Rheumatoid arthritis and Ulcerative colitis.
|
-
- HY-151140
-
|
|
Cytochrome P450
|
Others
|
|
CYP11B1-IN-2 (compound 7aa) is an orally active, potent and selective CYP11B1 inhibitor, with IC50 values of 9 nM and 25 nM for human CYP11B1 and rat CYP11B1, respectively. CYP11B1-IN-2 can be used for the research of diseases caused by excessive cortisol.
|
-
- HY-19934
-
|
TAS-117
|
Akt
Apoptosis
Autophagy
|
Cancer
|
|
Pifusertib (TAS-117) is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). Pifusertib triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. Pifusertib induces apoptosis and autophagy.
|
-
- HY-19934A
-
|
TAS-117 hydrochloride
|
Akt
Apoptosis
Autophagy
|
Cancer
|
|
Pifusertib (TAS-117) hydrochloride is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). Pifusertib hydrochloride triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. Pifusertib hydrochloride induces apoptosis and autophagy.
|
-
- HY-145695
-
|
|
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-18662
-
|
|
TRP Channel
|
Cancer
Neurological Disease
|
|
RQ-00203078 is a highly selective, potent and orally active TRPM8 antagonist with IC50s of 5.3 nM and 8.3 nM for rat and human TRPM8 channels, respectively. RQ-00203078 shows little inhibitory action against TRPV1, TRPA1, TRPV4, or TRPM2 channels.
|
-
- HY-14336
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB 271046 is a potent, selective and orally active 5-HT6 receptor antagonist with a pKi of 8.92-9.09. SB 271046 show >200-fold selective for the 5-HT6 receptor over other receptors, binding sites and ion channels. SB 271046 has anticonvulsant activity.
|
-
- HY-17610
-
|
TS-091
|
Histamine Receptor
|
Neurological Disease
|
|
Enerisant is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively.
|
-
- HY-P5558
-
|
|
VEGFR
|
Inflammation/Immunology
|
|
KLTWQELYQLKYKGI (QK) is a VEGF mimicking peptide, binds to the VEGF receptors and competes with VEGF. KLTWQELYQLKYKGI is active in gastric ulcer healing in rodents when administered either orally or systemically. KLTWQELYQLKYKGI shows the ability to induce capillary formation and organization in vitro.
|
-
- HY-153701
-
|
|
JAK
|
Cancer
|
|
JAK-IN-26 (compound 2) is an orally active JAK inhibitor with good pharmacokinetic characteristics. JAK-IN-26 inhibits IFN-α2B-induced phosphorylation of STAT3 in Jurkat cells (IC50=17.2 nM).
|
-
- HY-120669
-
|
|
Sodium Channel
|
Metabolic Disease
|
|
PF-06761281 (Compound 4a) is a potent, orally active, partial selective sodium-coupled citrate transporter (NaCT or SLC13A5) inhibitor with IC50 values of 0.51, 13.2 and 14.1 µM against HEKNaCT, HEKNaDC1 and HEKNaDC3, respectively.
|
-
- HY-141535A
-
|
|
Interleukin Related
|
Infection
Inflammation/Immunology
|
|
IL-17 modulator 1 (disodium) is an orally active, highly efficacious IL-17 modulator extracted from patent WO 2020127685. IL-17 modulator 1 (disodium) can be used for the research of diseases including psoriasis, ankylosing spondylitis and psoriatic arthritis.
|
-
- HY-141514
-
|
|
STING
|
Cancer
Inflammation/Immunology
|
|
MSA-2 dimer is a selective, orally active non-nucleotide STING agonist (Kd=145 μM) with long-term antitumor and immunogenic activity. MSA-2 dimer is bound to STING as a non-covalent dimer exhibiting higher permeability than cyclic dinucleotide.
|
-
- HY-149989
-
|
|
Ack1
Akt
|
Cancer
|
|
Ack1 inhibitor 1 is a potent, selective, and orally active inhibitor of ACK1 kinase with an IC50 value of 2.1 nM. Ack1 inhibitor 1 inhibits the phosphorylation of ACK1 and activation of downstream AKT. Ack1 inhibitor 1 has anti-tumor activity.
|
-
- HY-19464
-
|
|
Others
|
Endocrinology
|
|
Org 43553 is an orally active and low molecular weight (LMW) luteinizing hormone receptor (LH-R) agonist. Org 43553 shows agonistic activity to human LH and FSH receptors with EC50 values of 3.7 and 110 nM, respectively. Org 43553 can be used for the research of endocrine.
|
-
- HY-100919
-
|
WIN 8077 chloride
|
Cholinesterase (ChE)
|
Others
|
|
Ambenonium (WIN 8077) chloride is an orally active and reversible inhibitor of Acetyicholinesterase (AChE) with high affinity. Ambenonium chloride inhibits human AChE with an IC50 value of 0.7 nM (hAChE).
|
-
- HY-134217
-
|
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
KYN-101 is a potent, selective and orally active AHR inhibitor. KYN-101 decreases the CYP1A1 mRNA expression. KYN-101 shows anti-cancer activity.
|
-
- HY-136185
-
|
|
Drug Metabolite
|
Others
|
|
Atorvastatin Epoxy Tetrahydrofuran Impurity is an impurity isolated oxidative degradation products of Atorvastatin (HY-B0589). Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids.
|
-
- HY-12697
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
NGB 2904 is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a Ki of 1.4 nM. NGB 2904 shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (Kis=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 antagonizes Quinpirole-stimulated mitogenesis.
|
-
- HY-108288
-
|
CP 47904
|
Antibiotic
Bacterial
|
Infection
|
|
Sulbactam pivoxil is a proagent of sulbactam. Sulbactam is a β-lactamase inhibitor which poorly adsorbed from gastrointestinal tract. Sulbactam pivoxil has a better absorption than the parent agent and provides high serum levels after oral administration.
|
-
- HY-147088
-
|
|
YAP
|
Cancer
|
|
TEAD-IN-2 is a novel, orally active inhibitor of transcriptional enhancer associate domain (TEAD) and modulates TEAD by ubiquitination and/or degradation by compounds. TEAD-IN-2 can be used for the research of a variety of diseases, disorders or conditions associated with TEAD.
|
-
- HY-108411
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis.
|
-
- HY-N0304
-
|
Levodopa; 3,4-Dihydroxyphenylalanine
|
Dopamine Receptor
Endogenous Metabolite
|
Neurological Disease
Cancer
|
|
L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease.
|
-
- HY-122011
-
|
|
ROCK
SGK
PKA
PKC
|
Inflammation/Immunology
|
|
PF-4950834 is a potent, selective, orally bioavailable, ATP-competitive rho kinase inhibitor with IC50 values of 8.35 nM and 33.12 nM against ROCK2 and ROCK1, respectively. PF-4950834 inhibits neutrophil migration.
|
-
- HY-116565
-
|
SUVN-D4010
|
5-HT Receptor
|
Neurological Disease
|
|
Usmarapride (SUVN-D4010) is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) can be used for the research of cognitive deficits associated with Alzheimer's disease.
|
-
- HY-100748
-
|
CXD101
|
HDAC
|
Cancer
|
|
Zabadinostat (CXD101) is a potent, selective and orally active class I HDAC inhibitor with IC50s of 63 nM, 570 nM and 550 nM for HDAC1, HDAC2 and HDAC3, respectively. Zabadinostat has no activity against HDAC class II. Zabadinostat has antitumor activity.
|
-
- HY-12282
-
|
|
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-146268
-
|
|
CaMK
|
Neurological Disease
|
|
CaMKIIα-IN-1 (Compound 4d) is an orally active Ca 2+/calmodulin-dependent protein kinase II α (CaMKIIα) inhibitor with a KD of 219 nM for CaMKIIα WT hub. CaMKIIα-IN-1 has good metabolic stability.
|
-
- HY-103433
-
|
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
K579 is a potent and orally active dipeptidyl peptidase IV inhibitor. K579 inhibits the blood glucose elevation. K579 increases the plasma insulin and active forms of glucagon-like peptide-1 (GLP-1). K579 has the potential for the research of diabetic.
|
-
- HY-151941
-
|
|
Bacterial
|
Infection
|
|
MtInhA-IN-1 is a selective and orally active Mycobacterium tuberculosis NADH-dependent enoyl-acyl carrier protein reductase (MtInhA) inhibitor with an IC50 of 0.23 μM. MtInhA-IN-1 potently against M. tuberculosis H37Rv strain with a MIC value of 0.4 μM.
|
-
- HY-B2145
-
|
IY-81149 sodium
|
Proton Pump
TOPK
|
Cancer
Inflammation/Immunology
|
|
Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
|
-
- HY-14325A
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
L-745870 trihydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 trihydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors.
|
-
- HY-142686
-
|
|
SGK
|
Inflammation/Immunology
|
|
SGK1-IN-3 (compound 3a) is a potent and orally active inhibitor of SGK1. The serine/threonine kinase SGK1 is an activator of the β-catenin pathway and a powerful stimulator of cartilage degradation that is found to be upregulated under genomic control in diseased osteoarthritic cartilage. SGK1-IN-3 has the potential for the research of osteoarthritis.
|
-
- HY-122643
-
|
|
Bacterial
|
Infection
|
|
NITD-916, a 4-hydroxy-2-pyridone derivative, is an orally active and highly lipophilic mycobacterial enoyl reductase InhA inhibitor with an IC50 of 570 nM. NITD-916 forms a ternary complex with InhA and NADH to block access to the fatty acyl substrate binding pocket. NITD-916 has potent anti-tuberculosis effects.
|
-
- HY-160019
-
|
|
Mitophagy
Deubiquitinase
|
Neurological Disease
|
|
MTX115325 (Example 1) is an orally active, brain-penetrating USP30 inhibitor (IC50=12 nM) with neuroprotective activity. MTX115325 increases ubiquitination (EC50=32 nM) of the mitochondrial outer membrane protein TOM20 (a USP30 substrate), increasing mitophagy. MTX115325 prevents dopaminergic neuron loss and preserves striatal dopamine.
|
-
- HY-10999
-
|
GSK1120212; JTP-74057
|
MEK
Autophagy
Apoptosis
|
Cancer
|
|
Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis.
|
-
- HY-10515
-
|
|
PDK-1
|
Cancer
|
|
BX-320 is a selective, ATP-competitive, orally acitive, and direct PDK1 inhibitor with an IC50 of 30 nM in a direct kinase assay format. BX-320 also induces apoptosis. Anticancer effect.
|
-
- HY-15197
-
|
|
Acyltransferase
|
Metabolic Disease
|
|
ABT-046 is a potent, selective, and orally active acyl CoA:diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC50s of both 8 nM against human and mouse DGAT-1.
|
-
- HY-B0162
-
|
|
HCN Channel
|
Cardiovascular Disease
|
|
Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity.
|
-
- HY-14670
-
|
ML 1785713
|
COX
|
Inflammation/Immunology
|
|
Firocoxib (ML 1785713) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 0.13 μM. Firocoxib shows 58-fold more selective for COX-2 than COX-1 (IC50 of 7.5 μM). Firocoxib has anti-inflammatory effects.
|
-
- HY-149960
-
|
|
Parasite
|
Infection
|
|
Antiparasitic agent-17 (compound 5u) is an orally active antiparasitic agent. Antiparasitic agent-17 inhibits Chloroquine sensitive (Pf3D7) and Chloroquine resistant (PfK1) strain with IC50s of 0.96 μM and 1.67 μM, respectively.
|
-
- HY-135401
-
|
|
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-B0162A
-
|
|
HCN Channel
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Ivabradine hydrochloride is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine hydrochloride reduces dose-dependently heart rate without modification of blood pressure. Ivabradine hydrochloride shows anticonvulsant, anti-ischaemic and anti-anginal activity.
|
-
- HY-100516
-
|
UR-8880
|
COX
|
Inflammation/Immunology
|
|
Cimicoxib (CX) is an orally active potent and selective COX-2 (cyclo-oxygenase-2) inhibitor. Cimicoxib exhibits promising anti-inflammatory and analgesic activity. The PK parameters of Cimicoxib in dogs given precise (2 mg/kg) and approximate doses (1.95-2.5 mg/kg) are similar.
|
-
- HY-147297
-
|
BCX9930
|
Complement System
|
Inflammation/Immunology
|
|
Pelecopan (BCX9930) is a potent, selective, orally active inhibitor of complement factor D with an IC50 value of 14.3 nM. Pelecopan can target factor D to prevent both intravascular and extravascular hemolysis in PNH. Pelecopan also be used for other alternative pathway (AP) mediated diseases.
|
-
- HY-151460
-
|
|
Others
|
Cancer
|
|
GCN2-IN-7 (compound 39) is an orally active and selective general control nonderepressible 2 (GCN2) inhibitor (IC50=5 nM). GCN2-IN-7 shows anti-tumor activity in vivo.
|
-
- HY-B1617A
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
Metabolic Disease
|
|
Zuclomiphene citrate is a cis isomer of Clomiphene citrate. Zuclomiphene citrate has an antiestrogenic effect and can inhibit the secretion of luteinizing hormone (LH) more than the trans isomer. Zuclomiphene citrate is also an orally active hypocholesterolemic agent.
|
-
- HY-15550
-
-
- HY-126383
-
|
|
Others
|
Cancer
Infection
Inflammation/Immunology
Others
|
|
Spilanthol is an orally active analgesic, neuroprotective, antioxidant, antimutagenic, anti-cancer, anti-inflammatory, antimicrobial and insecticidal compound.pilanthol can induce cAMP to inhibit negative regulation of urinary concentration mechanism. Spilanthol can be use as diuretic research.
|
-
- HY-156280
-
|
|
RAR/RXR
|
Endocrinology
|
|
RARα antagonist 1 (compound 21) is an orally active and selective retinoic acid receptor α(RARα) antagonist, with the IC50 of 4.6nM.
|
-
- HY-114245B
-
|
Methylselenocysteine hydrochloride; Se-Methylseleno-L-cysteine hydrochloride
|
Beta-secretase
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
Se-Methylselenocysteine hydrochloride, a precursor of Methylselenol, has potent cancer chemopreventive activity and anti-oxidant activity. Se-Methylselenocysteine hydrochloride is orally bioavailable, and induces apoptosis.
|
-
- HY-114245
-
|
Methylselenocysteine; Se-Methylseleno-L-cysteine
|
Apoptosis
Endogenous Metabolite
Beta-secretase
|
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-143880
-
|
|
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-101664
-
|
IY-81149
|
Proton Pump
TOPK
|
Cancer
Inflammation/Immunology
|
|
Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
|
-
- HY-146435
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 22 (compound 14a) is an orally active anti-inflammatory agent. Anti-inflammatory agent 22 inhibits LPS-induced TNF-α production with an IC50 value of 14.6 μM. Anti-inflammatory agent 22 has preventive effects on lymphedematous tissue via suppression of adipogenesis. Anti-inflammatory agent 22 suppresses limb lymphedema volume in mice.
|
-
- HY-124754
-
|
BTRX-335140; CYM-53093
|
Opioid Receptor
|
Metabolic Disease
Neurological Disease
|
|
Navacaprant (BTRX-335140) is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively.
Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. Navacaprant distributes well into the CNS and can be used for the research of neuropathy.
|
-
- HY-123689
-
|
ALKS-33; RDC-0313
|
Opioid Receptor
|
Neurological Disease
|
|
Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo.
|
-
- HY-124290
-
|
AJM300
|
Integrin
|
Inflammation/Immunology
|
Carotegrast methyl (AJM300) is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of Carotegrast methyl, is a specific and dual α4β1/α4β7 integrin antagonist. Carotegrast methyl prevents the development of colitis in mice.
|
-
- HY-138696
-
|
XL092
|
TAM Receptor
c-Met/HGFR
VEGFR
|
Cancer
|
|
Zanzalintinib (XL092) is an orally active, ATP-competitive inhibitor of multiple receptor tyrosine kinases (RTKs) including MET, VEGFR2, AXL and MER, with IC50s in cell-based assays of 15 nM, 1.6 nM, 3.4 nM, 7.2 nM respectively. Zanzalintinib exhibits anti-tumor activity. Zanzalintinib has the potential for kinase-dependent diseases and conditions research.
|
-
- HY-F0001
-
|
Disodium NADH
|
Endogenous Metabolite
|
Metabolic Disease
|
|
NADH disodium salt (Disodium NADH) is an orally active reduced coenzyme. NADH disodium salt is a donor of ADP-ribose units in ADP-ribosylaton reactions and a precursor of cyclic ADP-ribose. NADH disodium salt plays a role as a regenerative electron donor in cellular energy metabolism, including glycolysis, β-oxidation and the tricarboxylic acid (TCA) cycle.
|
-
- HY-124729
-
|
|
ULK
Autophagy
|
Neurological Disease
|
|
BL-918 is an orally active UNC-51-like kinase 1 (ULK1) activator with an EC50 of 24.14 nM. BL-918 exerts its cytoprotective autophagic effect by targeting ULK complex. BL-918 has the potential for Parkinson’s disease (PD) treatment.
|
-
- HY-10864
-
URB-597
3 Publications Verification
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-150061
-
|
|
PI3K
mTOR
|
Cancer
|
|
NVP-BBD130 is a potent, stable, ATP-competitive and orally active dual PI3K and mTOR inhibitor. NVP-BBD130 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-B0425
-
|
Albamycin; Cathomycin
|
Antibiotic
DNA/RNA Synthesis
HSP
Apoptosis
Bacterial
Orthopoxvirus
|
Cancer
Infection
|
|
Novobiocin (Albamycin) is a potent and orally active antibiotic. Novobiocin also is a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. Novobiocin has the potential for the research of highly beta-lactam-resistant pneumococcal infections. Novobiocin shows anti-orthopoxvirus activity.
|
-
- HY-109127A
-
|
BCX7353 dihydrochloride
|
Ser/Thr Protease
|
Others
|
|
Berotralstat dihydrochloride is a low toxicity, effective, highly specific, second-generation, synthetic and orally active plasma kallikrein inhibitor used for the research of hereditary angioedema (HAE) attacks. Berotralstat dihydrochloride works by blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE.
|
-
- HY-141535
-
|
|
Interleukin Related
|
Infection
Inflammation/Immunology
|
|
IL-17 modulator 1 is an orally active, highly efficacious small molecule IL-17 modulators extracted from patent WO 2020127685. IL-17 modulator 1 can be used for the research of preventing, researching or ameliorating a variety of diseases including psoriasis, ankylosing spondylitis and psoriatic arthritis.
|
-
- HY-132298
-
|
|
Adenylate Cyclase
|
Others
|
|
TDI-10229 is a potent and orally bioavailable inhibitor of soluble adenylyl cyclase (sAC, ADCY10). TDI-10229 displays nanomolar inhibition of sAC in both biochemical and cellular assays (IC50 of 195 nM) and exhibits mouse pharmacokinetic properties sufficient to warrant its use as an in vivo tool compound.
|
-
- HY-110198
-
|
|
Prostaglandin Receptor
PERK
|
Inflammation/Immunology
|
|
ONO-8130 is an orally active and selective prostanoid EP1 receptor antagonist. ONO-8130 blocks phosphorylation of ERK in the L6 spinal cord. ONO-8130 relieves bladder pain in mice with cyclophosphamide-induced cystitis. ONO-8130 can be used for interstitial cystitis research.
|
-
- HY-A0115
-
-
- HY-148246
-
|
|
TGF-β Receptor
|
Cancer
|
|
MU1700 is an orally active and potent ALK1/2 inhibitor with IC50s of 13 nM and 6 nM, respectively. MU1700 shows cell membrane permeability and high brain permeability.
|
-
- HY-A0231
-
|
Gondafon; Glycodiazine
|
Others
|
Metabolic Disease
|
|
Glymidine sodium is an oral active antidiabetic. Glymidine sodium is the inhibitor of hepatic lipolysis. Glymidine sodium inhibits the glucose formation and supresses the elevated pyruvate oxidation which results from the inhibition of endogenous lipid mobilization.
|
-
- HY-121149
-
|
3-Hydroxytamoxifen
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
Droloxifene, a Tamoxifen derivative, is an orally active and selective estrogen receptor modulator. Droloxifene shows antiestrogenic and anti-implantation effects. Droloxifene induces p53 expression and apoptosis in MCF-7 cells. Droloxifene prevents bone loss in ovariectomized rats .
|
-
- HY-122592
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
Zifaxaban is an orally active, competitively and selective Factor Xa (FXa) inhibitor with an IC50 of 11.1 nM for human FXa. Zifaxaban shows >10000-fold greater selectivity than other serine proteases. Zifaxaban can be used for the arterial and venous thrombosis research.
|
-
- HY-147570
-
|
|
ATM/ATR
|
Cancer
|
|
ATR-IN-18 (compound 2) is an orally active and potent ATR kinase inhibitor, with an IC50 of 0.69 nM. ATR-IN-18 shows antiproliferative activity in LoVo cells, with an IC50 of 37.34 nM. ATR-IN-18 has anti-tumor activity.
|
-
- HY-B2178
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Emedastine difumarate is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine difumarate is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis.
|
-
- HY-144270
-
-
- HY-N0304A
-
|
Levodopa sodium; 3,4-Dihydroxyphenylalanine sodium
|
Dopamine Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
L-DOPA (Levodopa) sodium is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA sodium can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA sodium has anti-allodynic effects, and can be used for Parkinson's disease research.
|
-
- HY-139077
-
|
|
Stearoyl-CoA Desaturase (SCD)
|
Cancer
Metabolic Disease
|
|
SCD1 inhibitor-3 is a safe, potent and orally active SCD1 inhibitor. SCD1 inhibitor-3 can be used for the research of metabolic diseases such as obesity, type II diabetes and dyslipidemia, as well as skin diseases, acne and cancer.
|
-
- HY-150652
-
|
|
FGFR
Apoptosis
|
Cancer
|
|
FGFR-IN-8 (Compound 17a) is a highly potent and orally active panFGFR inhibitor against wild-type and mutant FGFRs. FGFR-IN-8 shows inhibition with IC50 values of <0.5, 189.1, <0.5, 22.6, <0.5 and 7.30 nM against FGFR1, V564F-FGFR2, N549H-FGFR2, V555M-FGFR3, FGFR3 and FGFR4, respectively. GFR-IN-8 induces cancer cell apoptosis and shows anticancer activities.
|
-
- HY-14180
-
|
|
IKK
|
Inflammation/Immunology
|
|
PHA 408 (PHA-408) is a potent, selective and orally active IκB kinase-2 (IKK-2) inhibitor. PHA 408 is a powerful anti-inflammatory agent against lipopolysaccharide (LPS)- and cigarette smoke (CS)-mediated lung inflammation.
|
-
- HY-147226
-
|
|
Prostaglandin Receptor
|
Endocrinology
Neurological Disease
|
|
EP3 antagonist 3 (compound 2) is an orally active, potent and selective EP3 antagonist, with a pKi of 8.3. EP3 antagonist 3 shows excellent pharmacokinetic properties. EP3 antagonist 3 can be used for overactive bladder (OAB) research.
|
-
- HY-12938
-
|
|
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-113974
-
|
t-AUCB
|
Epoxide Hydrolase
|
Cancer
|
|
trans-AUCB (t-AUCB) is a potent, orally active and selective soluble epoxide hydrolase (sEH) inhibitor with IC50s of 1.3 nM, 8 nM, 8 nM for hsEH, mouse sEH and rat sEH, respectively. trans-AUCB has anti-glioma activity.
|
-
- HY-100399
-
|
PD-132301; ATR-101
|
Acyltransferase
Apoptosis
|
Cancer
|
|
Nevanimibe (PD-132301) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe induces cell apoptosis and has the potential for adrenocortical cancer.
|
-
- HY-144841
-
|
CFT7455
|
Ligands for E3 Ligase
|
Cancer
|
|
Cemsidomide (CFT7455) is an orally active zinc finger transcription factors Ikaros (IKZF1), Aiolos (IKZF3) degrader. Cemsidomide is an anti-cancer agent that binds with high affinity to the cereblon E3 ligase (Kd of 0.9 nM) (WO2022032132A1; Compound 1).
|
-
- HY-147573
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BRD4 Inhibitor-23 is a potent and orally active BRD4 inhibitor with IC50s of 6.21 nM and 1.44 nM for BRD4 BD-1 and BRD4 BD-2, respectively (WO2022033542A1; Example 1).
|
-
- HY-100399A
-
|
PD-132301 hydrochloride; ATR101 hydrochloride
|
Acyltransferase
Apoptosis
|
Cancer
|
|
Nevanimibe hydrochloride (PD-132301 hydrochloride) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe hydrochloride inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe hydrochloride induces cell apoptosis and has the potential for adrenocortical cancer.
|
-
- HY-147772
-
-
- HY-114191B
-
|
|
Somatostatin Receptor
|
Endocrinology
Metabolic Disease
|
|
SSTR5 antagonist 2 hydrochloride is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of type 2 diabetes mellitus (T2DM).
|
-
- HY-109500
-
|
meso-Nordihydroguaiaretic acid; meso-NDGA
|
Lipoxygenase
|
Metabolic Disease
|
|
Masoprocol (meso-Nordihydroguaiaretic acid) is a potent and orally active lipoxygenase inhibitor. Masoprocol shows antihyperglycemic activity. Masoprocol decreases the glucose concentration and hepatic triglyceride in vivo. Masoprocol has the potential for the research of type II diabetes.
|
-
- HY-147416
-
|
BI 1029539; GS-248; OX-MPI
|
PGE synthase
|
Infection
|
|
Vipoglanstat (BI 1029539), a carboxamide, is a potent and selective, non-peptide and orally active small molecular inhibitor of human prostaglandin E synthase 1 (mPGES-1). Vipoglanstat also has anti-inflammatory activity.
|
-
- HY-148189
-
|
LXY-05-029
|
AMPK
|
Metabolic Disease
|
|
Aldometanib (LXY-05-029) is an orally active aldolase inhibitor. Aldometanib can activate lysosomal adenosine monophosphate-activated protein kinase (AMPK) and decreases blood glucose. Aldometanib can be used for the research of metabolic homeostasis.
|
-
- HY-144117
-
|
|
CDK
|
Metabolic Disease
|
|
GFB-12811 is a high selective and orally active CDK5 inhibitor with an IC50 of 2.3 nM. GFB-12811 is highly selective over the other tested kinases (CDK1/2/6/7/9).
|
-
- HY-109143
-
|
ABBV-105
|
Btk
|
Inflammation/Immunology
|
|
Elsubrutinib (ABBV-105) is an orally active, potent, selective and irreversible Bruton's tyrosine kinase (BTK) inhibitor。The IC50 of Elsubrutinib for BTK catalytic domain is 0.18 μM. Elsubrutinib can be used for the research of inflammatory disease.
|
-
- HY-146334
-
|
|
Chloride Channel
|
Inflammation/Immunology
|
|
DFBTA is an orally active, potent and little brain penetrated ANO1 (Calcium-activated chloride channel anoctamin-1) inhibitor, with an IC50 of 24 nM. DFBTA shows analgesic efficacy for inflammatory pain.
|
-
- HY-143872
-
|
|
Bcl-2 Family
|
Cancer
|
|
Bcl-2-IN-4 is a potent, orally active and selective Bcl-2 inhibitor with an IC50 of 1.5 nM. Bcl-2-IN-4 displays >200-fold selectivity over Bcl-xL (IC50 of 411 nM). Bcl-2-IN-4 inhibits RS4; 11 cell proliferation with an IC50 of 2.7 nM (WO2021180040A1; compound 2).
|
-
- HY-B0368A
-
|
SQ 14225 hydrochloride
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Captopril (SQ 14225) hydrochloride, antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril hydrochloride is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM.
|
-
- HY-12072
-
|
|
Src
|
Inflammation/Immunology
|
|
Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis.
|
-
- HY-B0368
-
|
SQ 14225
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
Cancer
|
|
Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM.
|
-
- HY-134188
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
JNJ-54717793, as a brain penetrant, is an orally active, selective and high affinity orexin-1 receptor (OX1R) antagonist (plasma EC50=85 ng/mL). The Ki values of JNJ-54717793 for hOX1R (human OX1R) and hOX2R are 16 nM and 700 nM, respectively. JNJ-54717793 is a potent compound of anxiety disorders.
|
-
- HY-107623
-
|
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
TC-MCH 7c, a phenylpyridone derivative, is an orally available, selective and brain-penetrable MCH1R antagonist with an IC50 of 5.6 nM for hMCH1R. TC-MCH 7c has Kis of 3.4 nM and 3.0 nM of human and mouse MCH1R, respectively.
|
-
- HY-130120
-
|
|
Free Fatty Acid Receptor
PPAR
|
Metabolic Disease
|
|
HWL-088 is a highly potent and orally active free fatty acid receptor 1 (FFA1/GPR40) agonist (EC50 of 18.9 nM) with moderate PPARδ activity (EC50 of 570.9 nM) . HWL-088 improves glucose and lipid metabolism, and has anti-diabetic effects.
|
-
- HY-13044
-
-
- HY-151807
-
|
|
15-PGDH
|
Metabolic Disease
|
|
15-PGDH-IN-1 is a potent and orally active 15-PGDH inhibitior. 15-PGDH-IN-1 has inhibition activity against recombinant human 15-PGDH with an IC50 value of 3 nM. 15-PGDH-IN-1 can be used for the research of tissue repair and regeneration.
|
-
- HY-19888
-
|
|
P2X Receptor
|
Inflammation/Immunology
|
|
GSK-1482160 is an orally available negative allosteric modulator of the P2X7 receptor. P2X7 receptors are involved in the production of pro-inflammatory cytokines, such as Il-1β, by central and peripheral immune cells. GSK-1482160 has the potential for the research of inflammation diseases.
|
-
- HY-109127
-
|
BCX7353
|
Ser/Thr Protease
|
Others
|
|
Berotralstat (BCX7353) is a low toxicity, effective, highly specific, second-generation, synthetic and orally active plasma kallikrein inhibitor used for the research of hereditary angioedema (HAE) attacks. Berotralstat works by blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE.
|
-
- HY-15011
-
|
|
Oxytocin Receptor
|
Others
|
|
L-372662 is a potent and orally active non-peptide oxytocin antagonist with a Ki value of 4.8. The Kd value of L-372662 for wild-type hOTR and [A318G]OTR is 5.8 nM and 73 nM. L-372662 shows selectivity to OTR:V1aR.
|
-
- HY-132935
-
|
|
c-Fms
|
Cancer
Inflammation/Immunology
|
|
BPR1R024 is an orally active and selective colony-stimulating factor-1 receptor (CSF1R) inhibitor. BPR1R024 has potent CSF1R inhibition activity with an IC50 value of 0.53 nM. BPR1R024 can be used for the research of immuno-oncology.
|
-
- HY-116565A
-
|
SUVN-D4010 free base
|
5-HT Receptor
|
Neurological Disease
|
|
Usmarapride (SUVN-D4010) free base is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) free base can be used for the research of cognitive deficits associated with Alzheimer's disease.
|
-
- HY-144448
-
|
|
FAK
Apoptosis
|
Cancer
|
|
FAK-IN-2 is a potent and orally active focal adhesion kinase (FAK) inhibitor, with anticancer activity (FAK IC50= 35 nM). FAK-IN-2 covalently inhibits the autophosphorylation of FAK in a dose-dependent manner, and inhibits the clone formation and migration of tumor cells, inducing apoptosis.
|
-
- HY-100886
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth.
|
-
- HY-144285
-
|
|
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-B0411A
-
|
R33812 monomaleate
|
Dopamine Receptor
|
Neurological Disease
|
|
Domperidone (R33812) monomaleate is an orally active and selective dopamine-2 receptor antagonist. Domperidone monomaleate acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine.
|
-
- HY-139486
-
|
|
Apelin Receptor (APJ)
|
Cardiovascular Disease
|
|
AM-8123 is an orally active and potent APJ agonist. AM-8123 inhibits Forskolin-stimulated cAMP production and promotes Gα protein activation. AM-8123 can be used for the research of cardiovascular disease.
|
-
- HY-118301
-
|
|
GABA Receptor
|
Neurological Disease
|
|
ADX71441 is a potent and selective positive allosteric modulator of the GABAB receptor. ADX71441 is bioavailable after oral administration and is brain penetrant. ADX71441 has the potential for research of anxiety, pain and spasticity.
|
-
- HY-130247
-
|
|
JAK
FLT3
Apoptosis
|
Cancer
|
|
JAK2/FLT3-IN-1 is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 has anti-cancer activity.
|
-
- HY-116804
-
|
|
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-149726
-
|
|
Histone Methyltransferase
|
Cancer
|
|
EZH2-IN-17 (compound 28) is a potent and orally active EZH2 inhibitor with an IC50 value of 0.95 nM. EZH2-IN-17 exhibits high anti-proliferation activity against different lymphoma cell lines including WSU-DLCL2, Pfeiffer and Karpas-422 (IC50 values of 2.36 nM, 1.73 nM, and 1.82 nM, respectively).
|
-
- HY-B1156
-
|
Cefradine; SQ-11436
|
Bacterial
Antibiotic
TOPK
|
Infection
Inflammation/Immunology
|
|
Cephradine (Cefradine) is a broad-spectrum and orally active cephalosporin. Cephradine is active against both gram-positive and gram-negative pathogens. Cephradine is effective in eradicating most penicillinase-producing organisms. Cephradine has been used in the research of genitourinary, gastrointestinal and respiratory tract infections, and in infections of the skin and soft tissues. Cephradine blocks solar-ultraviolet induced skin inflammation through direct inhibition of TOPK.
|
-
- HY-144256
-
|
|
Others
|
Cancer
|
|
CHD1Li 6.11 is a potent oncogenic CHD1L inhibitor (IC50=3.3 µM for cat-CHD1L recombinant protein). CHD1Li 6.11 is an orally bioavailable antitumor agent, significantly reducing the tumor volume of CRC xenografts generated from isolated quasi mesenchymal cells (M-phenotype), which possess enhanced tumorigenic properties.
|
-
- HY-50905
-
|
CHIR-258; TKI258
|
FLT3
c-Kit
FGFR
VEGFR
PDGFR
c-Fms
|
Cancer
|
|
Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC50s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity.
|
-
- HY-10443A
-
|
Ro 4588161 hydrochloride; R1626 hydrochloride
|
HCV
DNA/RNA Synthesis
|
Infection
|
|
Balapiravir hydrochloride (Ro 4588161 hydrochloride; R1626 hydrochloride) is an orally active proagent of a nucleoside analogue inhibitor of the RNA-dependent RNA polymerase (RdRp) of HCV (R1479; 4'-Azidocytidine). Balapiravir hydrochloride has anti-HCV activity. Balapiravir (hydrochloride) is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-10443
-
|
Ro 4588161; R1626
|
HCV
DNA/RNA Synthesis
|
Infection
|
|
Balapiravir (Ro 4588161; R1626) is an orally active proagent of a nucleoside analogue inhibitor of the RNA-dependent RNA polymerase (RdRp) of HCV (R1479; 4'-Azidocytidine). Balapiravir has anti-HCV activity. Balapiravir is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-137849
-
|
|
PARP
|
Cancer
|
|
RK-582 is an orally active, spiroindoline-based selective inhibitor of tankyrase. The IC50s of RK-582 against TNKS1/PARP5A and PARP1 are 36.1 nM and 18.168 nM, respectively. RK-582 inhibits rectal cancer COLO-320DM cells (GI50=0.23 μM) and significantly inhibits tumor growth in a COLO-320DM mouse xenograft model.
|
-
- HY-136207
-
|
|
nAChR
|
Neurological Disease
|
|
TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect.
|
-
- HY-12501A
-
ITI-214
1 Publications Verification
|
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-124758
-
|
|
Mitochondrial Metabolism
|
Cancer
Metabolic Disease
|
|
SH-BC-893 is an orally active anti-neoplastic sphingolipid analog. SH-BC-893 also protects from ceramide-induced mitochondrial dysfunction and corrects diet-induced obesity. SH-BC-893 can be used for the research of cancer and obesity.
|
-
- HY-147719
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-16 (compound 2b) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 102 µM. COX-2-IN-16 inhibits the NO production. COX-2-IN-16 shows anti-inflammatory activity.
|
-
- HY-114154
-
|
|
Glucocorticoid Receptor
|
Inflammation/Immunology
|
|
AL-438 is a potent, selective and orally active glucocorticoid receptor modulator with Kis of 2.5, 1786, 53, 1440, >1000 nM for glucocorticoid receptor, progesterone receptor, mineralocorticoid receptor, androgen receptor, estrogen receptor, respectively. AL-438 shows antiinflammatory activity.
|
-
- HY-144266
-
|
|
Glucosylceramide Synthase (GCS)
|
Metabolic Disease
Neurological Disease
|
|
Glucosylceramide synthase-IN-1 (T-036) a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 31 nM and 51 nM for human GCS and mouse GCS, respectively. Glucosylceramide synthase-IN-1 can be used for Gaucher's disease research.
|
-
- HY-111432
-
|
|
Ras
|
Others
|
|
CCG-232601 (compound 8f) is a potent and orally active Rho/MRTF/SRF transcriptional pathway inhibitor. CCG-232601 inhibits the development of Bleomycin-induced dermal fibrosis in mice. CCG-232601 has the potential for the research of antifibrotic for systemic scleroderma.
|
-
- HY-12113
-
|
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-118837
-
|
|
ROCK
|
Cancer
|
|
WF-536 is an orally active inhibitor of Rho-associated coiled-coil-containing protein kinase (ROCK). WF-536 has tumor anti-metastatic activity. WF-536 can be used for the research of cancer.
|
-
- HY-123797
-
|
|
SGLT
|
Metabolic Disease
|
|
KGA-2727 is a first selective, high-affinity and orally active SGLT1 inhibitor with Kis of 97.4 nM and 43.5 nM for human and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 has antidiabetic efficacy.
|
-
- HY-142283AS
-
|
|
EGFR
|
Cancer
|
|
Dosimertinib-d5 (mesylate) is a potent and orally active EGFR inhibitor. Dosimertinib-d5 (mesylate) decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d5 (mesylate) shows antiproliferative and anti-tumor activity. Dosimertinib-d5 (mesylate) has the potential for the research of non-small-cell lung cancer (NSCLC)[1].
|
-
- HY-13801
-
|
HOE 239
|
Parasite
|
Infection
|
|
Fexinidazole (HOE 239) is an orally active, potent nitroimidazole antitrypanosomal agent. Fexinidazole shows trypanocidal activity against T. brucei subspecies and strains with IC50s of 0.7-3.3 μM (0.2-0.9 μg/ml). Fexinidazol has the potential for human sleeping sickness (HAT) caused by infection with T. brucei.
|
-
- HY-114234A
-
|
|
Beta-secretase
|
Neurological Disease
|
|
TAK-070 Free base is a noncompetitive and orally active BACE1 inhibitor (IC50: 3.15 μM). TAK-070 Free base can be used for research of Alzheimer’s disease (AD). TAK-070 Free base inhibits brain levels of soluble Aβ, and improves cognitive impairments in AD model.
|
-
- HY-14674
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
CP-724714 is a potent, selective and orally active ErbB2 (HER2) tyrosine kinase inhibitor, with an IC50 of 10 nM. CP-724714 displays a marked selectivity against EGFR kinase (IC50=6400 nM). CP-724714 potently inhibits ErbB2 receptor autophosphorylation in intact cells. Antitumor activities.
|
-
- HY-14186
-
|
WYE-160020
|
Potassium Channel
|
Cardiovascular Disease
|
|
KVI-020 is an orally active, potent and selective blocker of the atrial potassium channel Kv1.5, with an IC50 of 480 nM. KVI-020 can inhibits hERG, with an IC50 of 15100 nM. KVI-020 is a potent antiarrhythmic agent, and can be used for atrial fibrillation (AF) research.
|
-
- HY-105896
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB399885 is a potent, selective, brain penetrant and orally active 5-HT6 receptor antagonist with pKi values 9.11 and 9.02 for human recombinant and native 5-HT6 receptors, respectively. SB399885 has cognitive enhancing properties.
|
-
- HY-114452
-
|
BTRX-246040
|
Opioid Receptor
|
Neurological Disease
|
|
LY2940094 (BTRX-246040) is a potent, selective and orally available nociceptin receptor (NOP receptor) antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 reduces ethanol self-administration in animal models.
|
-
- HY-W015828
-
|
RGX-202; 3-Guanidinopropionic acid
|
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
Ompenaclid (RGX-202) is an oral small-molecule SLC6A8 transporter inhibitor. Ompenaclid robustly inhibits creatine import in vitro and in vivo, reduces intracellular phosphocreatine and ATP levels, and induces tumor apoptosis. Ompenaclid can be used for the research of cancer and duchenne muscular dystrophy.
|
-
- HY-132193
-
|
|
RET
|
Cancer
|
|
RET-IN-4 is a potent, selective and orally active RET inhibitor with IC50s of 1.29 nM, 1.97 nM, and 0.99 nM for RET (WT), RET (V804M), and RET (M918T), respectively. RET-IN-4 exhibits better kinases selectivity against JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). RET-IN-4 has anticancer effects.
|
-
- HY-14336A
-
|
SB 271046A
|
5-HT Receptor
|
Neurological Disease
|
|
SB 271046 Hydrochloride (SB 271046A) is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 9.02, 8.55, and 8.81 for rat, pig and human, respectively. SB 271046 Hydrochloride is over 200 fold selective for the 5-HT6 receptor vs 55 other receptors, binding sites and ion channels. Anticonvulsant activity (EC50=0.16 μM).
|
-
- HY-130247A
-
|
|
JAK
FLT3
Apoptosis
|
Cancer
|
|
JAK2/FLT3-IN-1 (TFA) is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 (TFA) has anti-cancer activity.
|
-
- HY-145828
-
|
|
Microtubule/Tubulin
Ferroptosis
|
Cancer
|
|
Microtubule inhibitor 2 is a potent and selective, orally active microtubule inhibitor. Microtubule inhibitor 2 triggers cell death through ferroptosis . Microtubule inhibitor 2 shows antitumor activity.
|
-
- HY-10274
-
|
BIBR 1048
|
Thrombin
|
Cardiovascular Disease
|
|
Dabigatran etexilate (BIBR 1048) is an orally active proagent of Dabigatran (a direct inhibitor of thrombin). Dabigatran etexilate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation.
|
-
- HY-145872
-
|
|
HBV
|
Infection
|
|
HBV-IN-20 is a potent and oral active HBV inhibitor with an EC50 of 0.46 µM. HBV-IN-20 is a typical type II CpAM (core protein assembly modulators).
|
-
- HY-114191
-
|
|
Somatostatin Receptor
|
Metabolic Disease
Endocrinology
|
|
SSTR5 antagonist 2 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of treat type 2 diabetes mellitus (T2DM).
|
-
- HY-12047
-
|
AP24534
|
Bcr-Abl
PDGFR
VEGFR
FGFR
Src
Autophagy
|
Cancer
|
|
Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
|
-
- HY-114191A
-
|
|
Somatostatin Receptor
|
Metabolic Disease
Endocrinology
|
|
SSTR5 Antagonist 1 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of treat type 2 diabetes mellitus (T2DM).
|
-
- HY-116800
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
FR194921 is a potent, selective and orally active and cross the blood-brain barrier Adenosine A1 antagonist with Ki value of 6.6, 5400 nM for A1, A2A, respectively. FR194921 shows cognitive-enhancing and anxiolytic activity.
|
-
- HY-10358
-
|
MK-2206 (2HCl)
|
Akt
Autophagy
Apoptosis
|
Cancer
|
|
MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active allosteric AKT inhibitor with IC50s of 5 nM, 12 nM, and 65 nM for AKT1, AKT2, and AKT3, respectively. MK-2206 dihydrochloride induces autophagy.
|
-
- HY-D0873
-
|
EPPS
|
Amyloid-β
|
Neurological Disease
|
|
HEPPS (EPPS) is a buffering agent with the useful pH range from 7.3 ~ 8.7. HEPPS reduces Aβ-aggregate-induced memory deficits and rescues cognitive deficits in mice. EPPS is orally active and penetrates the blood-brain barrier.
|
-
- HY-136270
-
|
VX-803; M4344; ATR inhibitor 2
|
ATM/ATR
|
Cancer
|
|
Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity.
|
-
- HY-B0250
-
|
BCH-189
|
HIV
Reverse Transcriptase
HBV
|
Infection
Cancer
|
|
Lamivudine (BCH-189) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS.
|
-
- HY-101528
-
|
|
iGluR
|
Neurological Disease
|
|
IDRA 21 is a positive and orally active modulator of the AMPA receptor. IDRA 21 facilitates excitatory neurotransmission via GluR1/2 receptors. IDRA 21 has the potential for the research of cognitive/memory disorders, including those associated with aging.
|
-
- HY-13027G
-
-
- HY-15381
-
|
FTY720 phosphate
|
LPL Receptor
|
Infection
Inflammation/Immunology
Neurological Disease
|
|
Fingolimod phosphate (FTY720 phosphate) is an orally active sphingosine 1-phosphate (S1P) receptor agonist. Fingolimod phosphate can promote the neuroprotective effects of microglia. Fingolimod phosphate can be used for the research of multiple sclerosis and neurologic diseases.
|
-
- HY-145311
-
|
|
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-13458A
-
|
L-DOPS hydrochloride; DOPS hydrochloride; SM5688 hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
|
Droxidopa (L-DOPS) hydrochloride is a potent, orally active norepinephrine precursor. Droxidopa hydrochloride increases standing blood pressure, ameliorates symptoms of orthostatic hypotension and improves standing ability. Droxidopa hydrochloride has the potential for the research of neurogenic orthostatic hypotension (nOH) and alternative ADHD (attention deficit hyperactivity disorder).
|
-
- HY-15798
-
|
|
VSV
TAM Receptor
|
Cardiovascular Disease
|
|
UNC2881 is an orally active and specific Mer kinase inhibitor, inhibits steady-state Mer kinase phosphorylation with an IC50 value of 22 nM. UNC2881 shows additional inhibition against Axl and Tyro with IC50s of 360 nM and 250 nM, respectively. UNC2881 potently inhibits collagen-induced platelet aggregation, can be used for pathologic thrombosis research.
|
-
- HY-14803
-
|
BMS-214778; VEC-162
|
Melatonin Receptor
|
Neurological Disease
Endocrinology
|
|
Tasimelteon (BMS-214778) is an orally active and selective dual melatonin receptor agonist (DMRA). Tasimelteon has 2.1-4.4 times greater affinity for the MT2 receptor than for the MT1 receptor. Tasimelteon is a circadian regulator and has the potential for Non-24-Hour Sleep-Wake Disorder (Non-24).
|
-
- HY-14653
-
|
TAC-101; Am 555S
|
RAR/RXR
Apoptosis
|
Cancer
|
|
Amsilarotene (TAC-101; Am 555S), an orally active synthetic retinoid, has selective affinity for retinoic acid receptor α (RAR-α) binding with Ki of 2.4, 400 nM for RAR-α and RAR-β. Amsilarotene induces the apoptotic of human gastric cancer, hepatocellular carcinoma and ovarian carcinoma cells. Amsilarotene can be used for the research of cancer.
|
-
- HY-107670
-
|
DHβE hydrobromide
|
nAChR
|
Neurological Disease
|
|
Dihydro-β-erythroidine (DHβE) hydrobromide is a potent, orally active, and competitive antagonist of neuronal nAChRs. Dihydro-β-erythroidine hydrobromide shows selectivity for α4β4 and α4β2 nAChRs, with IC50s of 0.19 and 0.37 μM, respectively. Antidepressant-like activities.
|
-
- HY-139094
-
|
|
LPL Receptor
|
Metabolic Disease
|
|
A6770 is an orally active, potent sphingosine 1-phosphate (S1P) lyase (S1PL) inhibitor. A6770 is phosphorylated and the phosphorylated form directly inhibits S1P lyased.A6770, a potential key metabolite of THI, induces a [ 3H]dhS1P increase.
|
-
- HY-144863
-
|
|
GnRH Receptor
|
Cancer
|
|
BAY 1214784 is a potent, selective, and orally active antagonist of the human gonadotropin-releasing hormone receptor (hGnRH-R). BAY 1214784 is a spiroindoline derivative compound. BAY 1214784 effectively lowers plasma luteinizing hormone levels by up to 49%, at the same time being associated with low pharmacokinetic variability and good tolerability. BAY 1214784 has the potential for the research of uterine fibroids.
|
-
- HY-115553
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
DETQ is a selective, allosteric and orally active dopamine D1 receptor (Dopamine Receptor) potentiator. In HEK293 cells expressing the human D1 receptor, DETQ increases cAMP with an EC50 of 5.8 nM and a Kb of 26 nM. DETQ shows ~30-fold less potent at rat and mouse D1 receptors and is inactive at the human D5 receptor.
|
-
- HY-106420
-
|
16,16-dimethyl PGE2
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
16,16-Dimethyl prostaglandin E2 (16,16-dimethyl PGE2) is an orally active vertebrate Hematopoietic stem cells (HSCs) homeostasis critical regulator. 16,16-Dimethyl prostaglandin E2 can act through EP2/EP4 and has an interaction with the Wnt pathway.
|
-
- HY-11051
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
JNJ-20788560 is a selective and orally active delta opioid receptor agonist with an affinity of 2.0 nM for DOR (rat brain cortex binding assay). JNJ-20788560 also is a potent and efficacious antihyperalgesic agent that does not produce respiratory depression, pharmacologic tolerance, or physical dependence. JNJ-20788560 can be used for the research of the relief of inflammatory hyperalgesia.
|
-
- HY-112090
-
|
|
Epigenetic Reader Domain
HIV
|
Cancer
Infection
Inflammation/Immunology
|
|
ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC50 values ranging from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with agent-like properties enable the investigation of its antitumor efficacy and tolerability.
|
-
- HY-19644
-
|
GSK 2256294
|
Epoxide Hydrolase
|
Cardiovascular Disease
|
|
GSK2256294A (GSK 2256294) is a selective and orally active inhibitor of soluble epoxide hydrolase (sEH). GSK2256294A inhibits recombinant human sEH, rat sEH orthologs and murine sEH orthologs with IC50s of 27, 61 and 189 pM, respectively. GSK2256294A can be used for the research of chronic obstructive pulmonary disease (COPD) and cardiovascular disease.
|
-
- HY-12501
-
|
|
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-142772
-
|
|
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-10274A
-
|
BIBR 1048MS; Dabigatran etexilate methanesulfonate
|
Thrombin
|
Cardiovascular Disease
|
|
Dabigatran etexilate mesylate (BIBR 1048MS) is an orally active proagent of Dabigatran (a direct inhibitor of thrombin). Dabigatran etexilate mesylate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation.
|
-
- HY-124007
-
|
ISAHA
|
HDAC
|
Cancer
|
|
4-Iodo-SAHA (1k) is an orally active class I and class II histone deacetylase (HDAC) inhibitor with EC50s of 1.1, 0.95, 0.12, 0.24, 0.85 and 1.3 μM for Skbr3, HT29, U937, JA16 and HL60 cell lines, respectively. 4-Iodo-SAHA (1k) can be used for the research of cancer.
|
-
- HY-100560
-
|
(S)-(+)-Abscisic acid; ABA
|
Endogenous Metabolite
Proton Pump
|
Metabolic Disease
|
|
Abscisic acid ((S)-(+)-Abscisic acid), an orally active phytohormone in fruits and vegetables, is an endogenously produced mammalian hormone. Abscisic acid is a growth inhibitor and can regulate many aspects of plant growth and development. Abscisic acid inhibits proton pump (H +-ATPase) and leads to the plasma membrane depolarization in a Ca 2+-dependent manner. Abscisic acid, a LANCL2 natural ligand, is a potent insulin-sensitizing compound and has the potential for pre-diabetes, type 2 diabetes and metabolic syndrome.
|
-
- HY-128449
-
|
Cefradine monohydrate
|
Bacterial
Antibiotic
TOPK
|
Infection
Inflammation/Immunology
|
|
Cephradine (Cefradine) monohydrate is a broad-spectrum and orally active cephalosporin. Cephradine monohydrate is active against both grampositive and gram-negative pathogens and effective in eradicating most penicillinase-producing organisms known to be resistant to penicillin G, penicillin V, and ampicillin. Cephradine monohydrate has been used in the research of genitourinary, gastrointestinal and respiratory tract infections, and in infections of the skin and soft tissues. Cephradine monohydrate blocks solar-ultraviolet induced skin inflammation through direct inhibition of TOPK.
|
-
- HY-146789
-
|
|
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-14806S
-
|
MP-513 d8
|
Dipeptidyl Peptidase
|
Cardiovascular Disease
|
|
Teneligliptin-d8 is a deuterium labeled Teneligliptin (MP-513). Teneligliptin is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor[1].
|
-
- HY-122844
-
|
BI-853520; IN-10018
|
FAK
|
Cancer
|
|
Ifebemtinib (BI 853520) is an orally active and potent focal adhesion kinase (FAK) inhibitor (recombinant FAK IC50=1 nM). Ifebemtinib shows anti-proliferative activity against cancer cells. Ifebemtinib inhibits FER Kinase and FES Kinase with IC50s of 900 nM and 1040 nM, respectively.
|
-
- HY-13458
-
|
L-DOPS; DOPS; SM5688
|
Adrenergic Receptor
|
Neurological Disease
|
|
Droxidopa (L-DOPS; SM5688) is a potent, orally active norepinephrine precursor. Droxidopa increases standing blood pressure, ameliorates symptoms of orthostatic hypotension and improves standing ability. Droxidopa has the potential for the research of neurogenic orthostatic hypotension (nOH) and alternative ADHD (attention deficit hyperactivity disorder).
|
-
- HY-135747
-
|
GR-7
|
Bacterial
|
Infection
|
|
Gut restricted-7 (GR-7) is a potent, covalent and orally active pan-bile salt hydrolase (BSH) inhibitor. Gut restricted-7 has a tissue-selective and is restricted to the gut. Gut restricted-7 decreases gut bacterial BSHs and decreases deconjugated bile acid levels in feces of mice.
|
-
- HY-149120
-
|
|
Phospholipase
|
Inflammation/Immunology
Cardiovascular Disease
|
|
ASM-IN-1 is a potent and orally active acid sphingomyelinase (ASM) inhibitor with an IC50 value of 1.5 µM. ASM-IN-1 reduces lipid plaques in the aortic arch and aorta and reduces plasma ceramide concentration and Ox-LDL levels. ASM-IN-1 shows antiatherosclerotic and anti-inflammatory activity.
|
-
- HY-149252
-
|
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 32 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 32 shows anti-proliferative activity and inhibits microtubule polymerization. Tubulin inhibitor 32 induces Apoptosis and cell cycle arrest at G2/M phase. Tubulin inhibitor 32 shows anti-tumor activity.
|
-
- HY-131417
-
|
|
MMP
|
Cancer
Infection
Inflammation/Immunology
Cardiovascular Disease
|
|
cis-ACCP is an orally active antimetastatic matrix metalloproteinase-2 (MMP-2) selective inhibitor. cis-ACCP can inhibit MMP-2 and MMP-9 with IC50 values of 4 μM and 20 μM, respectively. cis-ACCP can be used for the research of a variety of chronic diseases.
|
-
- HY-148740
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Werner syndrome RecQ helicase-IN-3 is a potent and orally active werner syndrome recQ helicase (WRN) inhibitor with an IC50 value of 0.06 µM. Werner syndrome RecQ helicase-IN-3 shows antiproliferative activity. Werner syndrome RecQ helicase-IN-3 shows anticancer activity.
|
-
- HY-19151A
-
|
IS-741 sodium
|
Integrin
Phospholipase
|
Inflammation/Immunology
|
|
Fuzapladib (IS-741) sodium, an orally active leukocyte-function-associated antigen type 1 (LFA-1) activation inhibitor, is a leukocyte adhesion molecule. Fuzapladib sodium is also a phospholipase A2 (PLA2) inhibitor. Fuzapladib sodium exerts anti-inflammatory effects by inhibiting leukocyte migration into the inflammatory site.
|
-
- HY-145427
-
|
|
DNA-PK
|
Cancer
|
|
NU5455 is a potent, selective, and orally active inhibitor of DNA-PKcs. NU5455 administration increases both the efficacy and the toxicity of a parenterally administered topoisomerase inhibitor. NU5455 enhances the activity of Doxorubicin released locally in liver tumor xenografts without inducing any adverse effect.
|
-
- HY-19544
-
|
|
JAK
|
Cancer
|
|
JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC50 of 896 nM) and JAK2 (IC50 of 1050 nM).
|
-
- HY-103258
-
|
|
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-148741
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Werner syndrome RecQ helicase-IN-4 is a potent and orally active werner syndrome recQ helicase (WRN) inhibitor with an IC50 value of 0.06 µM. Werner syndrome RecQ helicase-IN-4 shows antiproliferative activity. Werner syndrome RecQ helicase-IN-4 shows anticancer activity.
|
-
- HY-13540
-
|
GPI 21016
|
PARP
|
Cancer
|
|
E7016 (GPI 21016) is an orally available PARP inhibitor. E7016 can enhance tumor cell radiosensitivity in vitro and in vivo through the inhibition of DNA repair. E7016 acts as a potential anticancer agent.
|
-
- HY-119524
-
|
|
Others
|
Metabolic Disease
|
|
Clofibride is an orally active hypolipaemic agent of pchlorophenoxyisobutyric type. Clofibride has weak toxicity and marked hypocholesterolaemic and hypotriglyceridaemic activity. Clofibride is converted into 4-chlorophenoxyisobutyric acid (CPIB) and 4-hydroxy-N-dimethylbutyramide (HMB) in vivo.
|
-
- HY-W727879
-
|
ABT-494-15N,d2
|
Isotope-Labeled Compounds
|
Others
|
|
Upadacitinib- 15N,d2 (ABT-494- 15N,d2) is the deuterium-labeled Upadacitinib (HY-19569). Upadacitinib- 15N,d2 (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib- 15N,d2 (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib- 15N,d2 (ABT-494) can be used for several autoimmune disorders research.
|
-
- HY-19447
-
|
LB80331
|
HBV
|
Infection
|
|
Besifovir (LB80331), a parent agent converted by LB80380 (HY-19447A), further metabolizes to its active form, LB80317 (HY-106235). Besifovir is an orally active, novel antiviral agent against hepatitis B virus (HBV).
|
-
- HY-131034
-
|
|
Wnt
|
Others
|
|
LP-922056 is an orally active, highly potent Notum Pectinacetylesterase inhibitor with EC50s of 21 nM, 55 nM in human and mouse cellular assay, respectively. LP-922056 significantly increases midshaft femur cortical bone thickness in mice and rats.
|
-
- HY-13556
-
|
LY353381; SERM III
|
Estrogen Receptor/ERR
|
Metabolic Disease
|
|
Arzoxifene (LY353381) is an orally active selective estrogen receptor modulator with a fixed ring structure similar to raloxifene. Arzoxifene has minimal side effects with powerful antiestrogenic effects on breast cancer and endometrium, with equally strong favorable estrogenic effects on bone and lipid profile.
|
-
- HY-136657
-
SC-43
1 Publications Verification
|
Phosphatase
STAT
Apoptosis
|
Cancer
|
|
SC-43, a Sorafenib derivative, is a potent and orally active SHP-1 (PTPN6) agonist. SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis. SC-43 has anti-fibrotic and anticancer effects.
|
-
- HY-101634
-
|
|
HCV
|
Infection
|
|
ABT-072 is an orally active and potent non-nucleoside HCV NS5B polymerase inhibitor (HCV GT1a EC50=1 nM; HCV GT1b EC50=0.3 nM).
|
-
- HY-10619B
-
|
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-136527
-
|
|
ROR
Interleukin Related
|
Inflammation/Immunology
|
|
BMS-986251 is an orally active and selective RORγt inverse agonist with an EC50 of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC50 of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced (HY-B0180) models (preclinical models of psoriasis).
|
-
- HY-144619
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
TLR7/8 antagonist 2 (Compound 15) is a potent and orally active agonist of TLR7/8 with IC50s of 4.9 and 0.6 nM, respectively. Inappropriate activation of TLR7 and TLR8 is linked to several autoimmune diseases, such as lupus erythematosus. TLR7/8 antagonist 2 has the potential for the research of autoimmune diseases.
|
-
- HY-15670
-
|
|
γ-secretase
Notch
|
Cancer
|
|
BMS-906024 is an orally active and selective γ-secretase (gamma secretase) inhibitor. BMS-906024 is a potent pan-Notch receptors inhibitor with IC50s of 1.6 nM, 0.7 nM, 3.4 nM, and 2.9 nM for Notch1, -2, -3, and -4 receptors, respectively. BMS-906024 demonstrates broad-spectrum antineoplastic activity.
|
-
- HY-137742
-
|
|
ULK
Autophagy
|
Cancer
|
|
SBP-7455 is a potent, high affinity and orally active dual ULK1/ULK2 autophagy inhibitor with IC50s of 13 nM and 476 nM in the ADP-Glo assays, respectively. SBP-7455 potently inhibits ULK1/2 enzymatic activity and can be used for triple-negative breast cancer (TNBC) research.
|
-
- HY-17421
-
|
TU-199
|
Proton Pump
|
Infection
Inflammation/Immunology
|
|
Tenatoprazole (TU-199) is an orally active imidazopyridine-based proton pump inhibitor with a prolonged plasma half-life. Tenatoprazole inhibits hog gastric H +/K +-ATPase activity with an IC50 of 6.2 μM. Tenatoprazole blocks the interaction of ubiquitin with the ESCRT-1 factor Tsg101, inhibits production of several enveloped viruses, including EBV.
|
-
- HY-145953
-
|
|
Others
|
Cancer
|
|
VY-3-135 is a potent, orally active, and stable ACSS2 inhibitor with an IC50 value of 44 nM. VY-3-135 is specific to ACSS2 among the AcCoA synthetase family of enzymes. VY-3-135 does not inhibit ACSS1 or ACSS3 enzymatic activity. VY-3-135 can be used for the research of breast cancer.
|
-
- HY-145153
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
S-777469 is a selective and orally available cannabinoid type 2 receptor (CB2) agonist with a Ki of 36 nM. S-777469 significantly suppresses compound 48/80-induced scratching behavior in mice in a dose-dependent manner. S-777469 produces its antipruritic effects by inhibiting itch signal transmission through CB2 agonism.
|
-
- HY-149099
-
|
|
RET
|
Cancer
|
|
RET-IN-22 (compound 17b) is a potent, selective and orally active RET inhibitor with an IC50 of 20.9 nM and 18.3 nM for wild-type RET and RET-V804M, respectively. RET-IN-22 shows highly selective profile to most kinases, especially to EGFR and VEGFR2. RET-IN-22 has anticancer effects.
|
-
- HY-132817
-
|
ICP-192
|
FGFR
|
Cancer
|
|
Gunagratinib (ICP-192) is a low toxicity and orally active pan-FGFR (fibroblast growth factor receptors) inhibitor that potently and selectively inhibits FGFR activities irreversibly by covalent binding. Gunagratinib can be used for the research of cancer. Gunagratinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-100555
-
|
|
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-13731
-
|
|
Others
|
Cancer
Inflammation/Immunology
|
|
PPI-2458 is a potent, orally active, selective and irreversible inhibitor of methionine aminopeptidase-2 (MetAP-2). PPI-2458 can be used for arthritis and lymphoma research.
|
-
- HY-N2109
-
|
|
Others
|
Metabolic Disease
|
|
Macranthoidin A is an orally active saponin from Flos Lonicerae. Macranthoidin A possess protection effects on hepatic injury caused by Acetaminophen, Cd, and CCl4, and conspicuous depressant effects on swelling of ear croton oil.
|
-
- HY-14184
-
-
- HY-139801
-
|
CI-907
|
Angiotensin-converting Enzyme (ACE)
|
Metabolic Disease
|
|
Indolapril hydrochloride (CI-907) is an orally active nonsulfhydryl angiotensin converting enzyme (ACE) inhibitor. Indolapril hydrochloride is highly specific in suppressing the contractile or pressor responses to Angiotensin I. Indolapril hydrochloride is a potent antihypertensive agent.
|
-
- HY-10715
-
|
|
GlyT
|
Neurological Disease
|
|
SSR504734 is an orally active, selective and reversible inhibitor of human, rat, and mouse GlyT1 (IC50=18, 15, and 38 nM, respectively). SSR504734 shows anti-schizophrenia, anti-anxiety and anti-depression activities.
|
-
- HY-12947
-
|
|
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-16743
-
|
Venglustat; SAR402671; GZ402671
|
Glucosylceramide Synthase (GCS)
|
Metabolic Disease
|
|
Ibiglustat (Venglustat) is an orally active, brain-penetrant glucosylceramide synthase (GCS) inhibitor. Ibiglustat can be used for the research of Gaucher disease type 3, Parkinson's disease associated with GBA mutations, Fabry disease, GM2 gangliosidosis, and autosomal dominant polycystic kidney disease.
|
-
- HY-15701B
-
|
(Z)-Leukadherin-1 choline
|
Complement System
|
Cancer
|
|
ADH-503 ((Z)-Leukadherin-1 choline) is an orally active and allosteric CD11b agonist. ADH-503 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.
|
-
- HY-155785
-
|
|
Reactive Oxygen Species
Autophagy
Apoptosis
JAK
|
Cancer
|
|
MTP is a PKM2 inhibitor. MTP induces cancer cell apoptosis by modulating caspase-3 activation. MTP induces autophagy and increases ROS generation. MTP also inhibits JAK2 signaling. MTP can be used for research of oral squamous cell carcinoma.
|
-
- HY-101634A
-
|
|
HCV
|
Infection
|
|
ABT-072 (potassium trihydrate) is an orally active and potent non-nucleoside HCV NS5B polymerase inhibitor (HCV GT1a EC50=1 nM; HCV GT1b EC50=0.3 nM).
|
-
- HY-144656
-
|
|
Others
|
Cancer
|
|
Steroid sulfatase-IN-1 is a potent and orally active Steroid sulfatase inhibitor with an IC50 of 1.71 µM. Steroid sulfatase-IN-1 shows antitumor activity (TGI=51%) in vivo. Steroid sulfatase-IN-1 has the potential for the research of breast cancer.
|
-
- HY-152149
-
|
|
DNA/RNA Synthesis
|
Inflammation/Immunology
|
|
CTP Synthetase-IN-1 is a potent, orally active cytidine 5'-triphosphate synthetase (CTPS) inhibitor with IC50s of 32 nM and 18 nM for human CTPS1 and human CTPS2, respectively. CTP Synthetase-IN-1 has anti-inflammatory effects.
|
-
- HY-135903
-
|
GDC-9545 tartrate; RG6171 tartrate
|
Estrogen Receptor/ERR
|
Cancer
|
|
Giredestrant tartrate (GDC-9545 tartrate), a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist. Giredestrant tartrate potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Anti-tumor activity.
|
-
- HY-138563
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
GSK973 is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5).
|
-
- HY-144260
-
|
|
SARS-CoV
|
Infection
|
|
3CPLro-IN-1 (compound A17) is a potent and orally active inhibitor of SARS-CoV-2 3CLpro with an IC50 of 5.65 μM. 3-Chymotrypsin-like cysteine protease (3CLpro) is an indispensable protein in viral replication and represents an attractive agent target for fighting COVID-19.
|
-
- HY-133018
-
|
|
HCV
|
Infection
|
|
HCV-IN-7 is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 has anti-viral activity.
|
-
- HY-146684
-
|
|
HDAC
Autophagy
Apoptosis
|
Cancer
|
|
HDAC-IN-36 (compound 23 g) is an orally active and potent HDAC (histone deacetylase) inhibitor, with an IC50 of 11.68 nM (HDAC6). HDAC-IN-36 promotes apoptosis, autophagy and suppresses migration. HDAC-IN-36 shows anti-tumor and anti-metastatic activity, and can be used for breast cancer research.
|
-
- HY-15228
-
RX-3117
1 Publications Verification
TV-1360; Fluorocyclopentenylcytosine
|
Nucleoside Antimetabolite/Analog
Apoptosis
|
Cancer
|
|
RX-3117 (TV-1360) is a potent and orally active anticancer and antimetaboliteagent. RX-3117 inhibits DNA methyltransferase 1 (DNMT1). RX-3117 shows antiproliferative and anti-tumour activity. RX-3117 induces cell cycle arrest at S phase and apoptosis.
|
-
- HY-130208
-
|
TDG
|
Galectin
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
|
Thiodigalactoside (TDG) is an orally active and potent galectin (GAL) inhibitor with Kd values of 24 μM, 49 μM for GAL1 and GAL3, respectively. Thiodigalactoside, a non-metabolizable disaccharide, has anti-inflammatory and anti-cancer activity. Thiodigalactoside dramatically reduces body weight gain in diet-induced obese rats.
|
-
- HY-133018A
-
|
|
HCV
|
Cancer
|
|
HCV-IN-7 hydrochloride is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 hydrochloride shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 hydrochloride has anti-viral activity.
|
-
- HY-112852A
-
|
|
Src
Apoptosis
|
Cancer
|
|
TL02-59 dihydrochloride is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM. TL02-59 dihydrochloride inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 dihydrochloride potently suppresses acute myelogenous leukemia (AML) cell growth.
|
-
- HY-103493
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
TAK-915 is a potent, selective, brain-penetrant and orally active phosphodiesterase 2A (PDE2A) inhibitor with an IC50 of 0.61 nM. TAK-915 is >4100-fold more selectivity for PDE2A than PDE1A. TAK-915 has the potential for neuropsychiatric and neurodegenerative disorders treatment.
|
-
- HY-100851A
-
|
|
5-HT Receptor
|
Cardiovascular Disease
|
|
LY-272015 hydrochloride is an orally active, specific 5-HT2B receptor antagonist. LY-272015 hydrochloride completely inhibits the phosphorylation of ERK2 induced by 5-HT or BW723C86. LY-272015 hydrochloride is antihypertensive in Deoxycorticosterone Acetate (DOCA)-salt-hypertensive rats.
|
-
- HY-145280A
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
IDO1/2-IN-1 hydrochloride (compound 4t) is the first potent IDO1/IDO2 dual inhibitor with IC50s of 28 nM and 144 nM for IDO1 and IDO2, respectively. IDO1/2-IN-1 hydrochloride exhibits antitumor activies. Orally active.
|
-
- HY-145280
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
IDO1/2-IN-1 (compound 4t) is the first potent IDO1/IDO2 dual inhibitor with IC50s of 28 nM and 144 nM for IDO1 and IDO2, respectively. IDO1/2-IN-1 exhibits antitumor activies. Orally active.
|
-
- HY-112852
-
TL02-59
4 Publications Verification
|
Src
Apoptosis
|
Cancer
|
|
TL02-59 is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM. TL02-59 inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 potently suppresses acute myelogenous leukemia (AML) cell growth.
|
-
- HY-144309
-
|
|
Cytochrome P450
|
Neurological Disease
|
|
Cholesterol 24-hydroxylase-IN-1 (compound 17) is a potent, orally active, and highly selective cholesterol 24-hydroxylase (CH24H or CYP46A1) inhibitor (IC50=8.5 nM). Cholesterol 24-hydroxylase-IN-1 can cross blood-brain barrier.
|
-
- HY-A0060
-
|
NKK 105
|
Lipoxygenase
|
Cancer
|
|
Malotilate (NKK 105), an orally active hepatotropic agent and an anti-fibrotic substance, selectively inhibits the 5-lipoxygenase (5-LOX) (IC50=4.7 μM). Malotilate prevents the development of hepatocytic injury in alcohol-pyrazole hepatitis by decreasing hepatic acetaldehyde levels and preventing the retention of transferrin in the hepatocytes.
|
-
- HY-139915
-
|
|
Glutathione Peroxidase
|
Inflammation/Immunology
|
|
MPO-IN-1 is a potent, orally active, and irreversible indole-containing inhibitor of myeloperoxidase (MPO). MPO-IN-1 has IC50s of 2.6 μM and 5.3 μM for MPO and thyroid peroxidase (TPO), respectively. MPO-IN-1 inhibits MPO activity in an acute mouse model of inflammation.
|
-
- HY-N9587
-
|
|
Apoptosis
|
Neurological Disease
|
|
Tricin 7-O-β-D-glucopyranoside is a potent and orally active neuroprotective agent. Tricin 7-O-β-D-glucopyranoside induces Apoptosis. Tricin 7-O-β-D-glucopyranoside decreases the expression of TNF-α induced phosphor-κB-α, phosphor-NF-κB, HMGB1.
|
-
- HY-16768
-
|
QAW039; NVP-QAW039
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
Fevipiprant (QAW039, NVP-QAW039) is s an orally active, selective, reversible prostaglandin D2 (DP2) receptor antagonist with an Kd value of 1.14 nM. Fevipiprant has the potential for the research of bronchial asthma.
|
-
- HY-117658
-
|
|
Others
|
Cardiovascular Disease
|
|
GSK-114 is a highly selective, orally active TNNI3K inhibitor (IC50= 25 nM). GSK-114 shows a 40-fold selectivity for TNNI3K over B-Raf kinase (IC50= 1 µM). Cardiac troponin I-interacting kinase (TNNI3K or CARK) is a member of the tyrosine-like kinase family that is selectively expressed in heart tissue.
|
-
- HY-139609
-
|
RP-3500; ATR inhibitor 4
|
ATM/ATR
mTOR
|
Cancer
|
|
Camonsertib (RP-3500) is an orally active, selective ATR kinase inhibitor (ATRi) with an IC50 of 1.00 nM in biochemical assays. Camonsertib shows 30-fold selectivity for ATR over mTOR (IC50=120 nM) and >2,000-fold selectivity over ATM, DNA-PK, and PI3Kα kinases. Camonsertib has potent antitumor activity.
|
-
- HY-134463
-
|
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation.
|
-
- HY-A0027
-
|
|
Histamine Receptor
Phosphodiesterase (PDE)
|
Inflammation/Immunology
Endocrinology
|
|
Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases.
|
-
- HY-A0027A
-
|
|
Histamine Receptor
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases.
|
-
- HY-120350
-
BI-1347
1 Publications Verification
|
CDK
|
Cancer
|
|
BI-1347 is an orally active, selective and potent CDK8 inhibitor (IC50=1.1 nM). BI-1347 shows anti-tumoral activity.
|
-
- HY-101903A
-
|
|
FABP
|
Metabolic Disease
Cardiovascular Disease
|
|
BMS-309403 sodium is a potent, orally active, and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor, with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 sodium interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 sodium improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells.
|
-
- HY-101903
-
|
|
FABP
|
Metabolic Disease
Cardiovascular Disease
|
|
BMS-309403 is a potent, orally active and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells.
|
-
- HY-123857
-
|
|
P2X Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
JNJ-55308942 is a high-affinity, selective, brain-penetrant P2X7 functional antagonist (hP2X7: IC50=10 nM, Ki=7.1 nM; rP2X7: IC50=15 nM, Ki=2.9 nM). JNJ-55308942 is orally bioavailable, binds to brain P2X7 and blocks IL-1β release from adult rodent brain.
|
-
- HY-138742
-
|
|
MAP4K
|
Cancer
|
|
HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1.
|
-
- HY-132307
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
Mcl-1 inhibitor 6 is an orally active, selective myeloid cell leukemia 1 (Mcl-1) protein inhibitor with a Kd of 0.23 nM and a Ki of 0.02 μM. Mcl-1 inhibitor 6 possesses superior selectivity over other Bcl-2 family members (Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w, Kd>10 μM). Mcl-1 inhibitor 6 is a potent antitumor agent.
|
-
- HY-10619E
-
|
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
-
|
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-15981
-
|
MK-3102
|
Dipeptidyl Peptidase
|
Metabolic Disease
Neurological Disease
|
|
Omarigliptin (MK-3102) is a potent, selective, orally active and cross the blood-brain barrier dipeptidyl peptidase 4 (DPP-4) inhibitor. Omarigliptin shows anti-parkinsonian activity. Omarigliptin has the neuroprotective effect to improve diabetes-associated cognitive dysfunction.
|
-
- HY-10619A
-
|
MK-4827 hydrochloride
|
PARP
Apoptosis
|
Cancer
|
|
Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
|
-
- HY-120536
-
|
|
Bacterial
|
Infection
|
|
HPi1 is a potent, selective and orally active antimicrobial against Helicobacter pylori with an IC50 of 0.24 μM and an MIC of 0.08-0.16 μg/mL. HPi1 is inactive against other bacteria, including the gut commensals Lactobacillus casei, Lactobacillus reuteri, and Bifidobacterium longum.
|
-
- HY-111232
-
|
|
GHSR
|
Metabolic Disease
|
|
GSK894281 is an orally active and highly potent ghrelin receptor full agonist with a pEC50 of <4.9 at the human motilin receptor. GSK894281 effectively enters the CNS. GSK894281 has the potential for constipation or to assist in emptying the colon prior to colonoscopy or colon surgery research.
|
-
- HY-10999A
-
|
GSK-1120212 (DMSO solvate); JTP-74057 (DMSO solvate)
|
MEK
Apoptosis
|
Cancer
|
|
Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib (DMSO solvate) activates autophagy and induces apoptosis.
|
-
- HY-147015
-
|
|
Orthopoxvirus
|
Infection
|
|
HOE961, the diacetate ester proagent of S2242, is active against respiratory cowpox virus infections, is orally active in infection models. Anti-orthopoxvirus activity.
|
-
- HY-B0411
-
|
R33812
|
Dopamine Receptor
|
Neurological Disease
|
|
Domperidone (R33812) is an orally active and selective dopamine-2 receptor antagonist. Domperidone acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine.
|
-
- HY-131343
-
|
|
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-124476
-
|
|
Caspase
Glutaminase
Apoptosis
|
Cancer
|
|
Cystamine is the disulfide form of the free thiol, cysteamine. Cystamine is an orally active transglutaminase (Tgase) inhibitor. Cystamine also has inhibition activity for caspase-3 with an IC50 value of 23.6 μM. Cystamine can be used for the research of severals diseases including Huntington's disease (HD) .
|
-
- HY-15701A
-
|
ADH-503 free base
|
Complement System
|
Cancer
|
|
(Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (Z)-Leukadherin-1 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.
|
-
- HY-W020050
-
|
|
Caspase
Glutaminase
Apoptosis
|
Cancer
Neurological Disease
|
|
Cystamine (dihydrochloride) is the disulfide form of the free thiol, cysteamine. Cystamine is an orally active transglutaminase (Tgase) inhibitor. Cystamine also has inhibition activity for caspase-3 with an IC50 value of 23.6 μM. Cystamine can be used for the research of severals diseases including Huntington's disease (HD) .
|
-
- HY-16743B
-
|
Venglustat succinate; SAR402671 succinate; GZ402671 succinate
|
Glucosylceramide Synthase (GCS)
|
Neurological Disease
|
|
Ibiglustat (Venglustat) succinate is an orally active, brain-penetrant glucosylceramide synthase (GCS) inhibitor. Ibiglustat succinate can be used for the research of Gaucher disease type 3, Parkinson's disease associated with GBA mutations, Fabry disease, GM2 gangliosidosis, and autosomal dominant polycystic kidney disease.
|
-
- HY-100459
-
|
|
RET
|
Metabolic Disease
Inflammation/Immunology
|
|
GSK3179106 is an orally active and selective RET kinase inhibitor with IC50s of 0.4 nM, 0.2 nM for human RET and rat RET, respectively. GSK3179106 has the potential for irritable bowel syndrome (IBS) through the attenuation of post-inflammatory and stress-induced visceral hypersensitivity.
|
-
- HY-12047S
-
|
AP24534-d8
|
Bcr-Abl
PDGFR
VEGFR
FGFR
Src
Autophagy
|
Cancer
|
|
Ponatinib-d8 is a deuterium labeled Ponatinib. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
|
-
- HY-151248
-
|
|
HDAC
|
Neurological Disease
|
|
HDAC2-IN-1 (Compound 17) is a brain penetrant, orally active, competitive HDAC2 inhibitor with an IC50 of 0.5 μM. HDAC2-IN-1 also inhibits HDAC1 and HDAC8 with IC50s of 1.61 μM and 0.98 μM, respectively.
|
-
- HY-114452A
-
|
BTRX-246040 tartrate
|
Opioid Receptor
|
Neurological Disease
|
|
LY2940094 (BTRX-246040) tartrate is a potent, brain penetrant, selective and orally available N/OFQ peptide (NOP) receptor antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 tartrate reduces Ethanol self-administration and Ethanol seeking in animal models.
|
-
- HY-139300
-
|
HMPL-813
|
EGFR
|
Cancer
|
|
Epitinib is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib can be used for the research of cancer. Epitinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-130187
-
|
|
Bacterial
|
Infection
|
|
Sapienic acid is a fatty acid commonly found on the skin and in mucosa. Sapienic acid has variable antimicrobial activities against Gram-positive and Gram-negative bacteria found on the skin and in the oral cavity. Sapienic acid is active against Streptococcus sanguinis, Streptococcus mitis and Fusobacterium nucleatum with MBC values of 31.3 μg/mL, 375.0 μg/mL and 93.8 μg/mL, respectively.
|
-
- HY-146886
-
|
|
FLT3
|
Cancer
|
|
FLT3-IN-15 is a highly potent and orally active FLT3 inhibitor with IC50s of 0.87 nM and 0.32 nM for FLT3 and FLT3/D835Y, respectively. FLT3-IN-15 can be used for researching acute myeloid leukemia.
|
-
- HY-116830
-
BRD0705
1 Publications Verification
|
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-152075
-
|
|
TAM Receptor
|
Cancer
|
|
AXL-IN-14 is a potent and orally active AXL inhibitor with an IC50 value of 0.8 nM. AXL-IN-14 inhibits Gas6/AXL-mediated cell migration and invasion. AXL-IN-14 decreases the expression of p-AXL and p-AKT proteins. AXL-IN-14 shows anti-tumor activity.
|
-
- HY-152506
-
|
|
Amyloid-β
|
Neurological Disease
|
|
Antioxidant agent-8 is an orally active inhibitor of Aβ1-42 deposition. Antioxidant agent-8 inhibits fibril aggregation (IC50=11.15 µM) and promotes fibril disaggregation (IC50=6.87 µM). Antioxidant agent-8 also inhibits Cu 2+-induced Aβ1-42 fibril aggregation (IC50=3.69 µM) and promotes Cu 2+-induced Aβ1-42 fibril disaggregation (IC50=3.35 µM). Antioxidant agent-8 has antioxidant activity, anti-inflammatory activity, biosafety, blood-brain barrier permeability and neuroprotective effect.
|
-
- HY-N10225
-
|
|
Prostaglandin Receptor
|
Endocrinology
Cardiovascular Disease
|
|
Thielavin A is an inhibitor of prostaglandin biosynthesis produced by Thielavia terricola. Thielavin A specifically inhibits the conversion of arachidonic acid into prostaglandin H2. Thielavin A has no anti-inflammatory activity on intravenous injection or on oral administration.
|
-
- HY-144318
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
CREB-IN-1 TFA is a potent, orally active CREB inhibitor (IC50=0.18 µM). CREB-IN-1 TFA inhibits breast cancer cell growth.
|
-
- HY-145685
-
|
|
Others
|
Cancer
|
|
RECQL5-IN-1 (Compound 4a) acts as an orally effective RECQL5 inhibitor (targeting both enzymatic and nonenzymatic domain). RECQL5-IN-1 is a potent inhibitor of RECQL5 helicase activity (IC50=46.3 nM). RECQL5-IN-1 inhibits RECQL5-WT cells and RECQL5-KO2 cells with IC50s of 4.8 μM and 19.6 μM, respectively. RECQL5-IN-1 can be used for the research of breast cancer.
|
-
- HY-145259
-
|
|
HDAC
Histone Demethylase
|
Cancer
|
|
HDAC6-IN-3 (Compound 14), an antiprostate cancer agent, is a potent, orally active HDAC6 inhibitor with IC50s ranging from 0.02-1.54 μM for HDAC1/2/3/6/8/10. HDAC6-IN-3 is also an effective MAO-A (IC50=0.79 μM) and LSD1 inhibitor.
|
-
- HY-111313
-
|
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
JNJ-26070109 is a high-affinity, competitive, orally bioactive, and selective cholecystokinin 2 (CCK2) receptor antagonist with good pharmacokinetic properties, with pKis of 8.49, 7.99, and 7.70 for human, rat, and dog CCK2 receptors, respectively. The dual function of CCK2 receptors in regulating gastric acid secretion and growth of the gastrointestinal mucosa make this an attractive and novel target for the research of gastroesophageal reflux disease.
|
-
- HY-147841
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
HIV-1 inhibitor-41 (Compound B23) is an orally active non-nucleoside HIV-1 reverse transcriptase inhibitor with EC50 values of 20.8 nM and 50 nM against HIV-1 WT and mutant E138K strain, respectively. HIV-1 inhibitor-41 shows low hERG, no apparent CYP enzymatic inhibition and no acute toxicity.
|
-
- HY-147322
-
|
|
YAP
|
Cancer
|
|
YAP/TAZ inhibitor-2 is a potent and orally active TEAD-YAP/TAZ inhibitor with an EC50 value of 3 nM. YAP/TAZ inhibitor-2 shows anti-proliferative activity. YAP/TAZ inhibitor-2 shows antitumor activity.
|
-
- HY-139605
-
|
|
GLUT
|
Cancer
Inflammation/Immunology
|
|
GLUT inhibitor-1 is a potent and orally active inhibitor of glucose transporters, targeting both GLUT1 and GLUT3, with IC50s of 242 nM and 179 nM, respectively. GLUT inhibitor-1 has the potential for the reaesrch of cancers and autoimmune diseases.
|
-
- HY-16957
-
|
|
HCV
HIV
|
Infection
|
|
LJ001 is a broad-spectrum and orally active antiviral agent. LJ001 exerts antiviral activities by binding to viral membranes. LJ001 inhibits TGEV and PDCoV infection. LJ001 decreases TGEV N and PDCoV N-protein expression.
|
-
- HY-144107
-
|
|
HCV
|
Infection
|
|
HCV-IN-34 (compound 3i) is an orally active and potent HCV entry inhibitor. HCV-IN-35 shows excellent antiviral activity, with an EC50 of 0.010 μM and a CC50 (half-maximal cytotoxic concentration) of 8.23 μM.
|
-
- HY-12085
-
-
- HY-122700
-
|
|
Complement System
|
Inflammation/Immunology
|
|
Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC50 of 30 nM and a Kd of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases.
|
-
- HY-142520
-
|
|
Epigenetic Reader Domain
|
Cancer
Inflammation/Immunology
|
|
I-BET567 is a potent and orally active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation.
|
-
- HY-151920
-
|
|
Btk
|
Inflammation/Immunology
|
|
BTK-IN-17 (compound 36R) is a selective and orally activeBTK inhibitor with an IC50 value of 13.7 nM. BTK-IN-17 decreases the expression of p-BTK Y223 and p-PLCγ2 Y1217. BTK-IN-17 shows anti-inflammatory effects.
|
-
- HY-15178
-
|
GRC 3886
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Oglemilast (GRC 3886) is a potent and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 of 0.5 nM for PDE4D3. Oglemilast inhibits pulmonary cell infiltration, including eosinophilia and neutrophilia in vitro and in vivo. Oglemilast has the potential for inflammatory airway diseases.
|
-
- HY-106697
-
|
ICI 128436
|
Aldose Reductase
|
Metabolic Disease
|
|
Ponalrestat (ICI 128436) is an orally active, selective and noncompetitive aldose reductase (AKR1B1; ALR) inhibitor. Ponalrestat selectively inhibits ALR2 (Ki=7.7 nM) over ALR1 (Ki=60 μM). Ponalrestat inhibits the conversion of glucose to sorbitol.
|
-
- HY-145829
-
|
|
JAK
Apoptosis
|
Inflammation/Immunology
|
|
Tofacitinib precursor-1 is an effective and oral active precursor to mitigate the systemic adverse effects of Tofacitinib. Tofacitinib precursor-1 can effectively attenuate the oxazolone-induced colitis in mice model with low toxicity. Tofacitinib precursor-1 is a potential drug candidate for the research of ulcerative colitis.
|
-
- HY-137371
-
|
|
Bacterial
Apoptosis
Antibiotic
|
Cancer
Infection
|
|
Lactonic sophorolipid is a natural antimicrobial surfactant for oral hygiene. Lactonic sophorolipid, a potential anticancer agent, induces apoptosis in human HepG2 cells through the caspase-3 pathway.
|
-
- HY-115986
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-5 is a potent, selective and orally active MAO-B inhibitor with an IC50 of 0.204 µM. MAO-B-IN-5 has the potential for the research of Parkinson's disease (PD).
|
-
- HY-P3499
-
|
|
Guanylate Cyclase
|
Inflammation/Immunology
|
|
Dolcanatide is an orally active GC-C (guanylate cyclase-C) agonist. Dolcanatide shows laxative, anti-nociceptive and anti-inflammatory activity. Dolcanatide can be used in inflammatory bowel disease research.
|
-
- HY-15196
-
TAK-285
2 Publications Verification
|
EGFR
|
Cancer
|
|
TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity. TAK-285 can cross the blood-brain barrier (BBB).
|
-
- HY-13208
-
|
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-108425A
-
|
|
Sodium Channel
|
Neurological Disease
|
|
AMG8380, an orally active and less active enantiomer of AMG8379, can serves as a negative control. AMG8380 inhibits human and mouse voltage-gated sodium channel NaV1.7 with IC50s of 0.907 and 0.387 μM, respectively. AMG8380 blocks Tetrodotoxin (TTX)-sensitive native channels with an IC50 of 2560 nM.
|
-
- HY-144263
-
|
|
SARS-CoV
|
Infection
|
|
3CPLro-IN-2 (compound C1) is a potent and orally active inhibitor of SARS-CoV-2 3CLpro with an IC50 and Ki of 1.55 and 6.09 μM, respectively. 3-Chymotrypsin-like cysteine protease (3CLpro) is an indispensable protein in viral replication and represents an attractive agent target for fighting COVID-19.
|
-
- HY-149843
-
|
|
FGFR
PROTACs
|
Cancer
|
|
LC-MB12 is an orally active PROTAC compound targets FGFR2 degradation with a DC50 of 11.8 nM. LC-MB12 contains BGJ398 (a FGFR2 inhibitor), PROTAC linker and CRBN.LC-MB12 inhibits FGFR2 signaling in gastric cancer cells and has anti-tumor activity.
|
-
- HY-114153A
-
|
|
c-Fms
|
Neurological Disease
|
|
PLX5622 hemifumarate is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 µM; Ki=5.9 nM). PLX5622 hemifumarate allows for extended and specific microglial elimination, preceding and during pathology development. PLX5622 hemifumarate demonstrates desirable PK properties in varies animals.
|
-
- HY-13691
-
|
Ro-31-7453
|
Akt
mTOR
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
MKC-1 (Ro-31-7453) is an orally active and potent cell cycle inhibitor with broad antitumor activity. MKC-1 inhibits the Akt/mTOR pathway. MKC-1 arrests cellular mitosis and induces cell apoptosis by binding to a number of different cellular proteins including tubulin and members of the importin β family.
|
-
- HY-139300A
-
|
HMPL-813 succinate
|
EGFR
|
Cancer
|
|
Epitinib succinate is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib succinate can be used for the research of cancer. Epitinib (succinate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-100017
-
|
|
GLUT
|
Cancer
|
|
BAY-876 is an orally active and selective glucose transporter 1 (GLUT1) inhibitor with an IC50 of 2 nM. BAY-876 is >130-fold more selective for GLUT1 than GLUT2, GLUT3, and GLUT4. BAY-876 is also a potent blocker of glycolytic metabolism and ovarian cancer growth.
|
-
- HY-147927
-
|
|
Others
|
Metabolic Disease
|
|
Human enteropeptidase-IN-1 (compound 6b) is a highly potent, orally active and low systemic exposure enteropeptidase inhibitor. Human enteropeptidase-IN-1 boosts the increase in fecal protein output, and exhibits potent body weight loss in diet-induced obese (DIO) rat model. Human enteropeptidase-IN-1 can be used for anti-obesity research.
|
-
- HY-B0121A
-
|
GR 43175 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Sumatriptan (GR 43175) hydrochloride is an orally active 5-HT1 receptor agonist with Kis of 17 nM, 27 nM and 100 nM for 5-HT1D, 5-HT1B and 5-HT1A receptors, respectively. Sumatriptan hydrochloride can be used for migraine headache research.
|
-
- HY-12959A
-
|
BAY x 3702
|
5-HT Receptor
|
Neurological Disease
|
|
Repinotan hydrochloride (BAY x 3702) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus Repinotan hydrochloride has a weak affinity for other related receptors. Repinotan hydrochloride has pronounced neuroprotective effects.
|
-
- HY-15652
-
|
ONO-6818; ONO-PO-736
|
Elastase
|
Inflammation/Immunology
|
|
Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat has a potent anti-inflammatory activity.
|
-
- HY-111817
-
|
|
Parasite
|
Infection
|
|
ACT-451840 is an orally active, potent and low-toxicity compound, showing activity against sensitive and resistant plasmodium falciparum strains. ACT-451840 targets all asexual blood stages of the parasite, has a rapid onset of action. ACT-451840 behaves in a way similar to artemisinin derivatives, with very rapid onset of action and elimination of parasite. ACT-451840 can be used for the research of malarial.
|
-
- HY-B0731A
-
|
SM-9018 free base
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT2A receptor (Ki=0.6 nM) and dopamine D2 receptor (Ki=1.4 nM), and also a partial agonist of 5-HT1A receptor (Ki=2.9 nM). Perospirone is an atypical antipsychotic agent and has the potential for schizophrenic disease research.
|
-
- HY-132935A
-
|
|
c-Fms
|
Cancer
Inflammation/Immunology
|
|
BPR1R024 mesylate is an orally active and selective colony-stimulating factor-1 receptor (CSF1R) inhibitor.
BPR1R024 mesylate is the equivalent of BPR1R024 (HY-132935). BPR1R024 has potent CSF1R inhibition activity with an IC50 value of 0.53 nM. BPR1R024 can be used for the research of immuno-oncology.
|
-
- HY-146012
-
|
|
HIV
|
Infection
|
|
HIV-1 protease-IN-4 (Compound II-22) is a potent HIV-1 protease inhibitor. HIV-1 protease-IN-4 is a proagent of atazanavir. HIV-1 protease-IN-4 as a proagent that delivers the parent 1 to rat plasma with a 5-fold higher AUC and 67-fold higher C24 when compared to oral administration of the parent agent.
|
-
- HY-115885
-
|
|
HDAC
|
Cancer
Inflammation/Immunology
|
|
XP5 is a potent, orally active HDAC6 inhibitor with an IC50 of 31 nM. XP5 displays high antiproliferative activity against various cancer cell lines including the HDACi-resistant YCC3/7 gastric cancer cells (IC50=0.16-2.31 μM). XP5 enhances antitumor immunity when combined with a PD-L1 inhibitor in melanoma.
|
-
- HY-144254
-
|
|
PI3K
Akt
Apoptosis
|
Cancer
|
|
PI3Kδ-IN-10 is a highly potent and orally active PI3Kδ inhibitor with IC50 of 2 nM. PI3Kδ-IN-10 robustly suppresses the downstream AKT pathway to induce subsequent apoptosis in hepatocellular carcinoma models.
|
-
- HY-16743A
-
|
Venglustat (L-Malic acid); SAR402671 (L-Malic acid); GZ402671 (L-Malic acid)
|
Glucosylceramide Synthase (GCS)
|
Metabolic Disease
|
|
Ibiglustat (Venglustat) L-Malic acid is an orally active, brain-penetrant glucosylceramide synthase (GCS) inhibitor. Ibiglustat L-Malic acid can be used for the research of Gaucher disease type 3, Parkinson's disease associated with GBA mutations, Fabry disease, GM2 gangliosidosis, and autosomal dominant polycystic kidney disease.
|
-
- HY-132300
-
|
|
β-catenin
|
Cancer
|
|
ZW4864 is an orally active and selective β catenin/B-Cell lymphoma 9 protein−protein interaction (β catenin/BCL9 PPI) inhibitor. ZW4864 inhibits β catenin/BCL9 PPI with a Ki value of 0.76 μM and an IC50 value of 0.87 μM.
|
-
- HY-145655
-
|
|
CDK
|
Cancer
|
|
CDK7-IN-11 is an orally active CDK7 inhibitor. CDK7-IN-11 exhibits high CDK7 inhibitory activity with IC50 value of 4.2 nM. CDK7-IN-11 can be effectively used for the research of diseases associated with CDK7.
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- HY-155693
-
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Topoisomerase
Parasite
|
Infection
|
|
Topoisomerase II inhibitor 16 (compound CT3) is a selective, orally active, brain-penetrant and irreversible trypanosomal topoisomerase II inhibitor by stabilizing double-stranded DNA:enzyme cleavage complexes. Topoisomerase II inhibitor 16 has the potential for Chagas disease research.
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- HY-W062109
-
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|
Endogenous Metabolite
Histamine Receptor
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Inflammation/Immunology
|
|
Olopatadine is an orally active and selective histamine 1 (H1) receptor antagonist and a mast cell stabilizer. Olopatadine prevents immunologically stimulated pro-inflammatory mediator release from human conjunctival mast cells. Olopatadine can be used for researching allergic conjunctivitis.
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-
- HY-143444
-
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JAK
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Inflammation/Immunology
|
|
JAK-IN-20 is a potent, pan and orally active JAK inhibitor with an IC50s of 7 nM, 5 nM, 14 nM for JAK1, JAK2, JAK3, respectively. JAK-IN-20 shows excellent pharmacokinetics and displays anti-inflammatory efficacy in vivo.
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- HY-135299
-
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Src
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Cancer
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CH6953755 is a potent, orally active and selective YES1 kinase (a member of the SRC family) inhibitor with an IC50 of 1.8 nM. CH6953755 inhibits YES1 kinase, leading to antitumor activity against YES1 Gene -amplified cancers in vitro and in vivo.
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- HY-108260
-
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GT-56-252
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Others
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Cardiovascular Disease
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Deferitrin (GT-56-252), a desferrithiocin (DFT) analogue, is an orally active trident iron chelator. Deferitrin is used for chronic iron overload due to transfusional therapy. Deferitrin has the potential for beta-thalassemia major.
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- HY-14184S
-
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ACT-064992-d4
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Endothelin Receptor
Apoptosis
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Cardiovascular Disease
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|
Macitentan-d4 is a deuterium labeled Sulfamethoxazole. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin) receptor antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH)[1].
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- HY-13580
-
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Glucocorticoid Receptor
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Cancer
Inflammation/Immunology
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Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma.
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- HY-155141
-
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Cytochrome P450
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Cancer
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hCYP3A4-IN-1 (compound C6) is a potent, orally active hCYP3A4 inhibitor. hCYP3A4-IN-1 shows the IC50 values of 43.93 nM and 153.00 nM against hCYP3A4 in human liver microsomes (HLMs) and CHO-3A4 stably transfected cell line, respectively. hCYP3A4-IN-1 potently inhibits CYP3A4-catalyzed N-ethyl-1,8-naphthalimide (NEN) hydroxylation in a competitive manner (Ki = 30.00 nM).
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- HY-19599
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(+)-Vorozole; R83842
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Cytochrome P450
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Cancer
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|
Vorozole is a potent and selective, orally active non-steroidal aromatase inhibitor. Vorozole shows antitumor activity in vivo. Vorozole has the potential for the research of mammary cancer.
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- HY-107064
-
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CGP 9000; Oraspor
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Bacterial
Antibiotic
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Infection
|
|
Cefroxadine (CGP 9000) is an orally active cephalosporin antibiotic. Cefroxadine is more effective than cephalexin against Escherichia coli and Klebsiella pneumoniae with MIC values of 3.13 and 1.56 μg/mL respectively with a concentration of 10 6 μg/mL. Cefroxadine can be used for the research of infection.
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- HY-P2229
-
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SDZ CO 611
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Somatostatin Receptor
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Cancer
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|
Ilatreotide (SDZ CO61), glycated somatostatin derivative, is a highly potent glycated analog of somatostatin with improved oral activity. Ilatreotide can suppress the fasting level and postprandial release of several gastrointestinal and pancreatic hormones. Ilatreotide can be used for the research of gastroenteropancreatic tumors.
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- HY-14305
-
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p38 MAPK
|
Inflammation/Immunology
|
|
BMS-582949 (compound 7k) is an orally active and highly selective p38α MAP kinase inhibitor, with IC50 values of 13 nM for p38α, and 50 nM for cellular TNFα. BMS-582949 can be used for research on rheumatoid arthritis.
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- HY-121383
-
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AH5158; Sch-15719W free base
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Adrenergic Receptor
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Inflammation/Immunology
Cardiovascular Disease
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Labetalol (AH5158) is an orally active selective α1- and non-selective β-adrenergic receptors competitive antagonist. Labetalol, an anti-hypertensive agent, can be used for the research of cardiovascular disease, such as hypertension in pregnancy.
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- HY-N12240
-
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Bacterial
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Infection
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Oleanolic aldehyde is an antimicrobial compound used to inhibit oral bacteria. Oleanolic aldehyde inhibits Streptococcus mutans and Porphyromonas gingivalis, which are associated with dental caries and periodontal disease, with minimum inhibitory concentrations (MICs) of 488 μg/mL and 250 μg/mL, respectively.
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- HY-147208
-
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YAP
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Cancer
|
|
MSC-4106 is an orally active and potent inhibitor of YAP/TAZ-TEAD. MSC-4106 inhibits TEAD1 or TEAD3 auto-palmitoylation and shows inhibitory effect on NCI-H226 tumor xenograft model.
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-
- HY-14743B
-
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SCV 07 hydrochloride; Gamma-D-glutamyl-L-tryptophan hydrochloride
|
Bacterial
STAT
|
Infection
Inflammation/Immunology
Cancer
|
|
Golotimod hydrochloride (SCV 07 hydrochloride), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod hydrochloride (SCV 07 hydrochloride) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod hydrochloride (SCV 07 hydrochloride) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
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- HY-145284
-
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|
Apelin Receptor (APJ)
|
Cardiovascular Disease
|
|
APJ receptor agonist 4 is a potent and orally active agonist of apelin receptor (APJ) with EC50 and Ki of 0.06 nM and 0.07 nM respectively. APJ receptor agonist 4 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 4 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 4 leads to improved cardiac function and can be used for researching the HF disease.
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-
- HY-125390
-
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CL-087
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
SM-360320 (CL-087) is a potent, orally active TLR7 agonist. SM-360320 is a immuno-modulator and exerts an antitumor effect. SM-360320 can act in synergy with DNA vaccines leading to an enhanced Th1 antibody response. SM-360320 can inhibit HCV replication in hepatocytes via a type I IFN-independent mechanism in addition to its IFN-mediated activity.
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- HY-13699
-
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GnRH Receptor
PERK
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Others
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NBI-42902 is an orally active, potent functional and competitive antagonist of GnRH receptor with an IC50 value of 0.79 nM, a Ki value of 0.56 nM, respectively. NBI-42902 inhibits GnRH-stimulated inositol phosphate (IP) accumulation, Ca 2+ flux, and ERK1/2 activation. NBI-42902 inhibits serum luteinizing hormone (LH) in castrated male macaques. NBI-42902 can be used for research on sex-hormone-related diseases.
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- HY-116594A
-
|
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Sigma Receptor
5-HT Receptor
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Neurological Disease
|
|
OPC-14523 hydrochloride is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 hydrochloride shows antidepressant-like activity.
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- HY-130609
-
|
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γ-secretase
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Neurological Disease
|
|
Aβ42-IN-1, compound 1v, is a novel, potent and orally active γ-secretase modulator (GSM). Aβ42-IN-1 potently reduced Aβ42 levels with an IC50 value of 0.091 µM without CYP3A4 inhibition. Aβ42-IN-1 shows a sustained pharmacokinetic profile.
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- HY-148250
-
|
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iGluR
|
Neurological Disease
|
|
TP-050 is a potent, orally active and selective NMDAR agonist with an EC50 value of 0.51 µM and 9.6 µM for GluN2A and GluN2D, respecticely. TP-050 can cross the blood-brain barrier (BBB). TP-050 induces hippocampal long-term (LPT) potentiation enhancemen and enhances neuronal signal transmission.
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-
- HY-B0121B
-
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GR 43175 free base
|
5-HT Receptor
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Neurological Disease
|
|
Sumatriptan (GR 43175 free base) is an orally active 5-HT1 receptor agonist with Kis of 17 nM, 27 nM and 100 nM for 5-HT1D, 5-HT1B and 5-HT1A receptors, respectively. Sumatriptan can be used for migraine headache research.
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-
- HY-136895
-
|
|
Prostaglandin Receptor
|
Cancer
|
|
AZ12672857 is an orally active inhibitor of EphB4 (IC50=1.3 nM) and Src kinases. AZ12672857 shows good inhibition of proliferation of c-Src transfected 3T3 cells (IC50=2 nM) as well as autophosphorylation of EphB4 in transfected CHO-K1 cells (IC50=9 nM).
|
-
- HY-129388A
-
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CC-90011; LSD1-IN-7
|
Histone Demethylase
|
Cancer
|
|
Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
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-
- HY-145697
-
|
|
GPR84
|
Inflammation/Immunology
|
|
GPR84 antagonist 2 (compound 33) is a potent, selective, and orally active GPR84 antagonist (IC50=8.95 nM). GPR84 antagonist 2 shows improved potency in the calcium mobilization assay and the ability to inhibit the chemotaxis of neutrophils and macrophages upon GPR84 activation. GPR84 antagonist 2 has the potential for the research of ulcerative colitis.
|
-
- HY-B0121
-
|
GR 43175
|
5-HT Receptor
|
Neurological Disease
|
|
Sumatriptan succinate (GR 43175) is an orally active 5-HT1 receptor agonist with Kis of 17 nM, 27 nM and 100 nM for 5-HT1D, 5-HT1B and 5-HT1A receptors, respectively. Sumatriptan succinate can be used for migraine headache research.
|
-
- HY-114785
-
|
|
MMP
|
Cancer
|
|
BPHA is a potent and orally active MMP-2, MMP-9 and MMP-14 inhibitor with IC50s of 12 nM, 16 nM and 17 nM, respectively. BPHA does not inhibit MMP-1, -3, and -7 (the IC50s are 974, >1000, and 795 nM, respectively). BPHA has antiangiogenic and antitumor effects.
|
-
- HY-145564
-
|
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-145835
-
|
|
PERK
|
Cancer
|
|
PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC50s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model.
|
-
- HY-116218
-
|
JPI-289
|
PARP
|
Neurological Disease
Cardiovascular Disease
|
|
Amelparib is a potent, orally active, and water-soluble inhibitor of PARP-1. Amelparib inhibits PARP-1 activity (IC50 =18.5 nmol/L) and cellular PAR formation (IC50 =10.7 nmol/L) in the nanomolar range. Amelparib is a potential neuroprotective agent. Amelparib has the potential for the research of acute ischaemic stroke.
|
-
- HY-112037
-
|
IACS-10759
|
Mitochondrial Metabolism
Apoptosis
|
Cancer
|
|
IACS-010759 is an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 inhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 has the potential for relapsed/refractory AML and solid tumors research.
|
-
- HY-145702
-
|
|
MEK
ERK
|
Cancer
|
|
MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC50=3 nM, pERK EC50=5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2.
|
-
- HY-120160A
-
|
CP 86325 Sodium
|
PPAR
|
Metabolic Disease
Neurological Disease
|
|
Darglitazone Sodium, a thiazolidinedione, is an orally active, potent, and selective PPAR-γ (peroxisome proliferator-activated receptor) agonist. Darglitazone Sodium is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research.
|
-
- HY-14165
-
-
- HY-15779
-
|
|
SphK
Apoptosis
|
Cancer
|
|
K145 is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. K145 is inactive against SphK1 and other protein kinases. K145 induces cell apoptosis and has potently antitumor activity.
|
-
- HY-15779A
-
|
|
SphK
Apoptosis
|
Cancer
|
|
K145 hydrochloride is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. K145 hydrochloride is inactive against SphK1 and other protein kinases. K145 hydrochloride induces cell apoptosis and has potently antitumor activity.
|
-
- HY-144109
-
|
|
HCV
|
Infection
|
|
HCV-IN-36 (compound (S)-3h) is an orally active and potent HCV entry inhibitor. HCV-IN-36 shows excellent antiviral activity, with an EC50 of 0.016 μM and a CC50 (half-maximal cytotoxic concentration) of 8.78 μM.
|
-
- HY-144743
-
|
|
Phosphodiesterase (PDE)
|
Others
|
|
ATX inhibitor 12 (compound 20) is an orally active and potent ATX (autotaxin) inhibitor, with an IC50 of 1.72 nM. ATX inhibitor 12 effectively alleviates lung structural damage with fewer fibrotic lesions at an oral dose of 60 mg/kg in C57Bl/6J mice. ATX inhibitor 12 can be uesd for idiopathic pulmonary fibrosis (IPF) research.
|
-
- HY-106080A
-
|
U-63557A
|
Others
|
Cardiovascular Disease
|
|
Furegrelate Sodium (U-63557A) is a potent, orally available, and selective thromboxane synthase inhibitor. Furegrelate Sodium inhibits human platelet microsomal thromboxane A2 (TxA2) synthase with an IC50 of 15 nM. Furegrelate Sodium is being developed as an antiplatelet agent.
|
-
- HY-150076
-
