RC-3095 is a gastrin-releasing peptide receptor antagonist, synergizes with gemcitabine to inhibit the growth of human pancreatic cancer CFPAC-1 in vitro and in vivo. RC-3095 inhibit the growth of human glioblastomas in vitro and in vivo. RC3095 inhibits tumor growth and decrease the levels and mRNA expression of epidermal growth factor receptors in H-69 small cell lung carcinoma.R,BRS-1) antagonist.

A pyrimidine analog reverse transcriptase inhibitor (NRTI) for the treatment of HIV/AIDS.

GW1929 is a synthetic peroxisome proliferator-activated receptor-γ (PPARγ) agonist with IC50 of 6.2 nM and 13 nM for human and mouse, respectively.

A thienopyridine-class antiplatelet agent that works by irreversibly inhibiting P2Y12 receptor on platelets.

A-1210477 is a potent and selective MCL-1 inhibitor.

A-381393 is a potent and selective agonist of the dopamine D4 receptor.

A-420983 is a potent, orally active inhibitor of lck with efficacy in a model of transplant rejection.

Abametapir is the active ingredient of Xeglyze Lotion.

Abiraterone (D4A) is an active metabolite of the CYP17A1 inhibitor abiraterone.

ABT-333 is an NS5B non-nucleoside polymerase inhibitor.

ABT-594 represents a novel class of broad-spectrum analgesics whose primary mechanism of action is activation of the neuronal nicotinic acetylcholine receptors.

ABT-719 is a potent bacterial DNA gyrase inhibitor.

ABT-719 is a potent bacterial DNA gyrase inhibitor.

ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM, respectively.

ABX-1431 (ABX1431) is a highly potent, selective, orally available, CNS-penetrant monoacylglycerol lipase (MGLL) with IC50 of 14 nM (hMGLL).

AC-263093 (AC263093) is a potent, functionally selective neuropeptide FF receptor type 2 (NPFFR2) agonist with pKi of 6.9.

ACA is a cell permeable inhibitor of PLA2,reported to inhibit α-ketoisocaproic acid and glyceraldehyde-induced insulin secretion, as well as glucose-induced insulin secretion.

Acacetin is an O-methylated flavone found in Robinia pseudoacacia (black locust), Turnera diffusa (damiana),Betula pendula (silver birch),and in the fern Asplenium normale.

Acarbose is the first identified α-glucosidase inhibitor.

Acebilustat(ZK322) is a potent and selective leukotriene A4 hydrolase inhibitor.

Acecainide, also known as N-acetylprocainamide and ASL 601, is the N-acetylated metabolite of procainamide.

Acotiamide acts as an acetylcholinesterase inhibitor

Acrizanib（LHA510） is a potent and selective angiogenesis inhibitor and VEGFR‑2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration.

ACSS2 inhibitor is a novel ACSS2 inhibitor.

ACTB-1003 is a potent inhibitor of FGFR1 with IC50 <10 nM in FGFR-1 biochemical assay; more information can be find in Patent WO/2007/064883A2, Example 12.

ACY-738 demonstrates inhibitory activity against recombinant HDAC6 with IC50 values of 1.7 nM, with respective average selectivity over class I HDACs being 100-fold.

Adelmidrol is an anti-inflammatory ethanolamide derivative of azelaic acid.

AF-2364, an analogue of Lonidamine (LND), had a contraceptive effect when orally administered to adult Sprague–Dawley rats.

Afuresertib (GSK2110183) is a potent, orally bioavailable Akt inhibitor with Ki of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2.

AG 1406 is a selective inhibitor of the receptor tyrosine kinase VEGF receptor 2 .