AHAS inhibitor is a novel acetohydroxyacid synthase(AHAS) inhibitor, a promising drug target against Mycobacterium tuberculosis (MTB).

AGI-6780 is the first highly potent and selective small molecule inhibitor of isocitrate dehydrogenases, which binds in an allosteric manner at the dimer interface of mutant IDH2-R140Q (IC50=23 nM).

AG-881 is a potent and selective orally available inhibitor of mutated forms of both isocitrate dehydrogenase type 1 (IDH1) in the cytoplasm and type 2 (IDH2).

AG-490 (Tyrphostin B42) is an inhibitor of EGFR, ErbB2 and JAK2 with IC50 of 0.1 μM, 13.5 μM, and ~10 μM, respectively.

AG-18(RG-50810; Tyrphostin A23) inhibits EGFR with IC50 of 40 μM.

AG-1478 (Tyrphostin AG-1478) is a selective EGFR inhibitor with IC50 of 3 nM.

AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM. It is at least 1000-fold more potent than the benzamides.

Afuresertib (GSK2110183) is a potent pan-AKT inhibitor that demonstrated synergy with bortezomib in preclinical models of multiple myeloma (MM).

AFN-1252(Debio 1452) is a potent inhibitor of enoyl-acyl carrier protein reductase (FabI), inhibited all clinical isolates of Staphylococcus aureus and Staphylococcus epidermidis at concentrations of ≤0.12 μg/ml.

Afatinib is an irreversible EGFR/HER2 inhibitor with an IC50 of 14 nM for in vitro potency against HER2.

AF-353 is a novel, orally bioavailable, highly potent and selective P2X3/P2X2/3 receptor antagonist.

ADX-88178 is a novel potent, selective, and brain-penetrant positive allosteric modulator of the mGlu4 receptor.

ADX-47273 is a novel, potent and selective metabotropic glutamate receptor 5 allosteric modulator with an EC50 of 170 nM.

ADL5859 agonizes δ-opioid receptor with a 1000-fold selectivity than µ- or κ-opioid receptor with Ki of 32 nM and 37 nM, respectively.ADL5859 displays weak inhibitory activity at the hERG channel with an IC50 of 78 μM. The EC50 of ADL5859 against δ opioid

Adavivint (SM-04690, SM 04690, SM04690) is a novel small molecule Wnt pathway inhibitor with EC50 of 3 nM in vitro

AD80, a multikinase inhibitor, shows strong activity against human RET, BRAF, S6K, and SRC but were much less active than either AD57 or AD58 against mTOR. The IC50 value for RET is 4 nM.

Aclidinium Bromide(LAS 34273; LAS-W 330) is a long-acting, inhaled muscarinic antagonist as a maintenance treatment for chronic obstructive pulmonary disease (COPD).

Acetaminophen is a COX inhibitor for COX-1 and COX-2 with IC50 of 113.7 μM and 25.8 μM, respectively.

Acalisib (GS-9820) is a potent and selective inhibitor of PI3Kδ with IC50 value of 12.7 nM.

Acalabrutinib (ACP-196) is a second-generation, selective, irreversible inhibitor of BTK.

AC 55541 is a potent and selective protease-activated receptor 2 (PAR2) agonist (pEC50 = 6.7) that displays no activity at other PAR subtypes or at over 30 other receptors involved in nociception and inflammation.

ABX464 (ABX-464, ABX 464) is a novel class of anti-HIV small molecule targeting Rev-mediated viral RNA biogenesis, shows dose dependent inhibition of HIV-1 replication in stimulated PBMCs with IC50 of 0.1-0.5 uM.

ABT-751(E 7010) is a novel bioavailable tubulin-binding and antimitotic sulfonamide agent with IC50 of about 1.5 and 3.4 μM in neuroblastoma and non-neuroblastoma cell lines, respectively.

ABT-639 is a novel, peripherally acting, selective T-type Ca2+ channel blocker. ABT-639 blocks recombinant human T-type (Cav3.2) Ca2+ channels in a voltage-dependent fashion (IC50 = 2 μM) and attenuates LVA currents in rat DRG neurons (IC50 = 8 μM).

ABC1183 is a potent, selective, orally active GSK3α/β and CDK9 inhibitor with IC50 of 327/657 nM and 321 nM (CDK9/cyclin T1), shows growth inhibitory activity against a broad panel of cancer cell lines; decreases cell survival through G2/M arrest and modu

AB680 (AB-680) is a highly potent, selective, reversible inhibitor of CD73 with Ki/IC50 of 4.9/70 pM (hCD73), displays > 10,000-fold selectivity against related ecto-nucleotidases (CD39, NTPDases 2/3/8) and a large panel of unrelated enzymes, receptors, a

A83-01 is a selective inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 (IC50 values are 12, 45 and 7.5 nM respectively).

A-804598 is a novel, competitive, and selective P2X7 receptor antagonist with IC50 of 10 nM, 9 nM and 11 nM in rat, mouse and human P2X7 receptors respectively.

A-803467 is a selective NaV1.8 channel blocker with IC50 of 8 nM.

A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM, little effect on GPPase/FBPase activity.