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 .

AG-1557 is an ultra-potent inhibitor of epidermal growth factor receptor tyrosine kinase (EGFRK).

AG-17 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 460 µM in the human epidermoid carcinoma cell line A431.

AG-494 is an inhibitor of epidermal growth factor receptor kinase with an IC50 value of 1 µM in HT-22 cells.

AG-99 is an inhibitor of EGF receptor kinase with an IC50 value of 10 µM in the human epidermoid carcinoma cell line A431.

AGI-5198 is the first highly potent and selective inhibitor of IDH1 R132H/R132C mutants with IC50 of 0.07 μM/0.16 μM.

USP25 and 28 inhibitor AZ-1 (AZ1) is a potent, selective, dual USP25/28 inhibitor with IC50 of 0.7/0.6 uM, respectively; shows a high degree of selectivity over other deubiquitinases (USP4,7 etc.); demonstrates target engagement against both USP25 and USP28 in cells, elicits modulation of both the total levels and the half-life of the c-Myc oncoprotein in cells, and also induces apoptosis and inhibits cell viability in a range of cancer cell lines.

ALK inhibitor 1 is a novel and selective inhibitor for the ALK kinase.

ALK inhibitor 2 is a novel and selective inhibitor for the ALK kinase.

ALKS-8700 also known as diroximel fumarate, is a prodrug of monomethyl fumarate in a controlled-release formulation that rapidly and efficiently converts to MMF in the body.

Alogliptin is an orally administered, anti-diabetic drug in the DPP-4 inhibitor class. A randomized clinical trial reporting in 2011 aimed to determine the efficacy and safety of alogliptin versus placebo and voglibose among newly diagnosed Type 2 diabete

Alovudine is a DNA polymerase subunit gamma-1 (POLG) inhibitor, shows promise for treating AML.

alpha-hederin is a water-soluble pentacyclic triterpenoid saponin, possessing several biological properties such as antispasmodic, moliscicidic, anthelmithic and inhibiting cell proliferation.

Alpha-Mangostin has neuroprotective, anti-cancer, antifungal, neuroprotective, renoprotective, antioxidant and anti-inflammatory activities.

Alprenolol is a non-selective beta blocker as well as 5-HT1A receptor antagonist.

Alrestatin is an AKR (aldose reductase) inhibitor, which attaches molecules to the active site of the NADP+/enzyme complex in a stacked formation.

Altiratinib is a MET/TIE2/VEGFR2/TRK (A,B,C) kinase inhibitor in Phase 1 clinical development for the treatment of invasive solid tumors including glioblastoma.

AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist

AM630 is a selective CB2 receptor antagonist that binds to CB1 and CB2 receptors with Ki values of 5.2 µM and 31.2 nM, respectively.

MRL-871 (MRL871) is a potent, selective inhibitor of RORγt via allosteric inverse agonism, inhibits coactivator binding with IC50 of 7 nM; significantly reduces the IL17a mRNA levels in EL4 murine lymphoblast cell line at 10 uM.

AMG 319 is an investigational, highly selective, small molecule inhibitor of PI3Kδ that blocks B cell proliferation following BCR stimulation both in vitro and in vivo, inhibits basal AKT phosphorylation, and inhibits proliferation in lymphoid tumor cells