CYM-5541 (ML249) is an selective and allosteric S1P3 receptor agonist with an EC50 between 72 and 132 nM. 了解更多

YH249是第一个高度特异性的直接p300 /β-catenin拮抗剂。 了解更多

mPGES1-IN-3 (Compound 17d) is a potent and selective microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor, which exhibits excellent mPGES-1 enzyme (IC50: 8 nM), cell (A549 IC50: 16.24 nM) and human whole blood potency (IC50: 249.9 nM). 了解更多

L-APB is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively. 了解更多

HS-243 is an inhibitor of transforming growth factor-?beta kinase. HS-243 can be used in treatment of cancer, malaria, inflammatory and other TAK1-?mediated diseases. 了解更多

A-784168 is a potent and selective antagonist of Vanilloid receptor type 1 (TRPV1). 了解更多

GMB-475 is a degrader of BCR-ABL1 tyrosine kinase based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. 了解更多

BpV(HOpic) is a potent and selective inhibitor of PTEN with an IC50 of 14 nM. Nanocarrier-BpV(HOpic) has neuroprotective activity. 了解更多

Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor. 了解更多

DD1 is a proteasome inhibitor that induces human myeloid tumor-selective apoptosis. 了解更多

RO6889678 is an inhibitor of HBV with a complex ADME profile. RO6889678 showed an intracellular enrichment of 78-fold in hepatocytes, with an apparent intrinsic clearance of 5.2 ?l/min per mg protein and uptake and biliary clearances of 2.6 and 1.6 ?l/min per mg protein, respectively. 了解更多

PF-06882961 is a potent, orally bioavailable agonist of the glucagon-like peptide-1 receptor agonist (GLP-1R) 了解更多

Eleclazine, also known as GS-6615, is a selective late sodium current inhibitor. Eleclazine is potentially useful for treatment of coronary vasodilators, antiarrhythmics and vasodilators. 了解更多

Beclamide is a chlorinated benzylpropanamide used as an anticonvulsant drug. It is used in the treatment of tonic-clonic seizyres and has sedative properties. 了解更多

Caroverine hydrochloride is a potent, competitive and reversible antagonist of NMDA and AMPA glutamate receptor. Caroverine hydrochloride is also an antioxidant and calcium-blocking agent that exhibits vasorelaxant action. Caroverine hydrochloride can be used for the research of inner ear tinnitus. 了解更多

NV-5138 is an active small-molecule drug for the treatment of major depressive disorder (MDD). 了解更多

PF-04995274 is a partial agonist of the serotonin (5-HT) receptor subtypes 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E (Kis = 0.36, 0.46, 0.15, and 0.32 nM, respectively, in a radioligand binding assay).1 It increases cAMP levels in HEK293 cells expressing 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E receptors (EC50s = 0.47, 0.36, 0.37, and 0.26 nM, respectively, for the human recombinant receptors). PF-04995274 decreases scopolamine-induced increases in the distance traveled in the Morris water maze in rats when administered at a dose of 0.032 mg/kg. 了解更多

AVN-101 is a very potent 5-HT7 receptor antagonist, with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors. It is a milti-target drug candidate for the treatment of CNS disorders. 了解更多

BI-187004, also known as VTP-34072, is an 11β-hydroxysteroid dehydrogenase 1 inhibitor. 了解更多

Zanubrutinib (BGB-3111) is a selective Bruton tyrosine kinase (BTK) inhibitor. 了解更多

XL-784 is a selective matrix metalloproteinases (MMP) inhibitor, with IC50s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for MMP-1??MMP-2??MMP-3??MMP-8??MMP-9??MMP-13??respectively. 了解更多

Setmelanotide (RM-493; BIM-22493; IRC-022493) is a selective melanocortin 4 receptor (MC4R) agonist with EC50s of 0.27 nM and 0.28 nM for human and rat MC4R, respectively. 了解更多

CRAC intermediate 1 is a key intermediate in the chemical synthesis of a series of CRAC channel inhibitors, detailed information can be found in Patent WO 2010122089 A1, intermediate 9. 了解更多

α-2,3-sialyltransferase-IN-1 (Lith-O-Asp analog) is a noncompetitive α-2,3-sialyltransferase inhibitor with an IC50 of 6 μM. 了解更多

YM17E is an inhibitor of acyl CoA:cholesterol acyltransferase (ACAT), with IC50 of 44 nM in rabbit liver microsomes in vitro. 了解更多

P-gp modulator 1 is a high affinity, orally available modulator of P-glycoprotein (Pgp), can reverse the Pgp-mediated multidrug resistance ((MDR). 了解更多

TRAF-STOP inhibitor 6877002, is a selective inhibitor of CD40-TRAF6 interaction, compound VII, shows inhibition of NF-κB activation in RAW cells, extracted from patent WO2014033122A1. 了解更多

PI3Kdelta inhibitor 1 (Compound 5d) is a potent, selective and orally available PI3Kδ inhibitor with an IC50 of 1.3 nM. 了解更多

(S)-b-aminoisobutyric acid is a non-protein amino acid originating from the catabolism of thymine and valine. 了解更多

(3-Carboxypropyl)trimethylammonium chloride is angiopathic substance produced as an intermediary metabolite by gut microbiota that feed on carnitine in dietary red meat. 了解更多

Indotecan (LMP-400) is a potent topoisomerase 1(Top1) inhibitor with IC50 values of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. 了解更多

ZLN024 is an AMPK allosteric activator. 了解更多

Methoxy-PEPy is a potent and highly selective mGlu5 receptor antagonist with IC50 of 1 nM. 了解更多

Cyantraniliprole D3 is the deuterium labeled Cyantraniliprole, which is an insecticide of the ryanoid class. 了解更多

3-AP (PAN-811) is a novel inhibitor of the M2 subunit of ribonucleotide reductase (RR), and is a potent radiosensitizer. 了解更多

Sch-42495 racemate is the racemate of Sch-42495. Sch-42495 is a novel neutral metalloendopeptidase (NEP) inhibitor. Sch-42495 is the orally active ethylester prodrug of SCH 42354. 了解更多

(R)-Zanubrutinib is the R enantiomer of Zanubrutinib. Zanubrutinib is a selective Bruton tyrosine kinase (BTK) inhibitor. 了解更多

Tipelukast (KCA 757) is a sulfidopeptide leukotriene receptor antagonist, an orally bioavailable anti-inflammatory agent and used for the treatment of asthma. 了解更多

Toreforant is a potent and selective histamine H4 receptor (H4R) antagonist, with a Ki at the human receptor of 8.4 nM. 了解更多

RU 24969 is a selective agonist at the 5-HT1A and 5-HT1B receptors. 了解更多

Avibactam sodium (NXL-104) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively. 了解更多

Apatinib (YN968D1) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 with an IC50 of 1 nM. 了解更多

Prifuroline is an antiarrhythmic agent. 了解更多

MBP146-78 is a potent and selective inhibitor of cGMP dependent protein kinases. 了解更多

DprE1-IN-2 (compound 18) is a potent DprE1 inhibitor with an IC50 of 28 nM. DprE1-IN-2 has antituberculosis effect. 了解更多

BCR-ABL-IN-1 is an inhibitor of BCR-ABL tyrosine kinase, with a pIC50 of 6.46, and may be used in the research of chronic myelogenous leukemia. 了解更多

STING agonist-1 (G10) is a novel human-specific STING agonist that elicits antiviral activity against emerging Alphaviruses. 了解更多

MBM-17 (compound 42c) is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 3 nM. 了解更多

Norverapamil hydrochloride ((??)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor. 了解更多