Alda-1 is an ALDH2 agonist, cell-permeable activator of both the wild-type ALDH2*1 and the asian E487K mutant ALDH2*2 forms of mitochondrial aldehyde dehydrogenase 2 (mtALDH2).

AL 082D06(D-06) is the first selective, nonsteroidal glucocorticoid receptor (GR) antagonist with Ki of 210 nM, exhibits excellent selectivity against AR, PR, MR and ER(Ki > 10 uM).

AK-7 is a cell- and brain-permeable inhibitor of SIRT2 (IC50 = 15.5 μM).

AIM-100 is a small molecule inhibitor of Ack1 with an IC50 of 24 nM IC50 value: 24 nM [3] Target: Ack1 Ack1 inhibitor AIM-100 not only inhibited Ack1 activation but also suppressed AKT tyrosine phosphorylation, leading to cell cycle arrest in the G1 ph

AIC246 is a novel anti-CMV compound which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.

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

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).