all-trans-4-Oxoretinoic acid, an active metabolite of vitamin A, induces gene transcription via binding to nuclear retinoic acid receptors (RARs).

Alloxazine is an A2 receptor antagonist, which is approximately 10-fold more selective for the A2B receptor than for the A2A receptor.

Allopurinol riboside, a metabolite of allopurinol, shows potent activities against parasites.

Alloepipregnanolone, a pregnane with anesthetic, hypnotic, and sedative properties, interferes with the development of rapid tolerance to the anxiolytic effect of ethanol.

Alizapride (MS 5080) is a dopamine D2 antagonist with prokinetic and antiemetic effects used in the treatment of nausea and vomiting..

Alizapride (MS 5080) is a dopamine D2 antagonist with prokinetic and antiemetic effects used in the treatment of nausea and vomiting..

Alfuzosin is an α1 adrenergic receptor antagonist used to treat benign prostatic hyperplasia (BPH).

ALDH3A1 inhibitor EN40 is a potent and selective, covalent, in vivo-active inhibitor of ALDH3A1 with IC50 of 2 uM, demonstrates no activity against ALDH1A3 and ALDH6A1 at 30 uM.

ALDH1A inhibitor 673A (ALDH1Ai 673A) is a potent, selective, pan-ALDH1A inhibitor with IC50 of 246, 230 and 348 nM for ALDH1A1, ALDH1A2 and ALDH1A3, respectively.

ALB-127158 is a potent (IC50=7 nM), selective, non-peptide antagonist of MCHR1 (Melanin-concentrating hormone receptor 1) for treatment of obesity..

AL-9 is a small molecule HCV replication inhibitor with EC50 of 0.29 and 0.75 uM for genotype 1b and 2a, inhibits purified PI4KIIIα with IC50 of 0.57 uM.

Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50 = 3.5 nM) and Akt2 (IC50 = 42 nM), with potent and balanced activity.

AKR1C3 inhibitor KV-37 is a potent, isoform selective and metabolically stable inhibitor of Aldo-keto reductase 1C3 (AKR1C3) with IC50 of 66 nM, displays 109-fold selectivity over AKR1C2.

AK306 is a small molecule clathrin heavy chain (CLTC/CHC) binding compound that induces arrest and apoptosis of the HCT116 colon cancer cell line with EC50 of 50 nM.

AK106-001616 (AK 106-001616) is a potent and selective inhibitor of cytosolic phospholipase A2 (cPLA2) with IC50 of 3.8 nM (human cPLA2 enzyme).

AJM300 (AJM 300, AJM-300) is a novel potent, selective, oraaly available alpha 4 integrin antagonist fortreatment of active ulcerative colitis..

AHU-377 is an inhibitor of neprilysin with IC50 value of 5 nM.

AgrA inhibitor F19 is a small-molecule AgrA inhibitor that act as antivirulence agent against Gram-positive pathogens, blocks staphylococcal transcription factor AgrA from binding to its promoter and inhibits toxin and virulence factor transcription.

AGPS-IN-1a is a potent inhibitor of the ether lipid-generating enzyme alkyl-glycerone phosphate synthase (AGPS), selectively lowers ether lipid levels in several types of human cancer cells and impairs their cellular survival and migration..

Agomelatine is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor.

AGN192836 (AGN 192836) is a potent, selective α2 adrenergic (alpha 2-adrenoceptor) agonist with EC50 of 8.7, 41 and 6.6 nM for α2A, α2B and α2C receptor, respectively.

AGN 210676 is a selective prostaglandin EP2 agonist extracted from patent US20070203222A1, Compound example 23, has an EC50 of 5 nM.

AGN 194310(VTP-194310) is a potent and selective pan-RARs agonist with Kd values of 3/2/5 nM for RARα/β/γ respectively.

AGL-2263 is an insulin receptor (IR) blocker.

AGI-14100 (AGI14100) is a novel potent and selective, orally available IDH1 mutant inhibitor.

Aganepag is a potent Prostanoid EP2 receptor agonist, with an EC50 of 0.19 nM, and shows no activity at EP4 receptor. Aganepag can be used in the research of wound healing, scar reduction, scar prevention and wrinkle treatment and prevention.

AG-24322 is a second generation CDK inhibitor. AG-024322 is a potent inhibitor of CDK1, CDK2, and CDK4 that produces cell-cycle arrest and antitumor activity in preclinical models. The no-adverse-effect dose of AG-024322 was 2 mg/kg and associated with ov

AG13958 is a VEGF inhibitor that was clinical development by Pfizer in 2006-07 for treatment of age-related macular degeneration (AMD).

Afegostat D-Tartrate is a pharmacological chaperone, which specifically and reversibly binds acid-β-glucosidase (GCase) in the endoplasmic reticulum (ER) with high affinity.

AF-792 (RO-5) is a novel selective P2X3 and P2X2/3 antagonist with pIC50 of 8.2 and 7.9 respectively, with no inhibition at other P2X receptors.