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

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).

AGK2 is a potent, and selective SIRT2 inhibitor with IC50 of 3.5 μM.

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

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

AI-10-104 is a small molecule inhibitor that interferes with CBFβ binding to RUNX proteins with IC50 of 1.25 uM in FRET assays.

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

AICAR phosphate (Acadesine, AICA Riboside, NSC 105823) is a selective AMPK activator in both hepatocytes and adipocytes.

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

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

AK778 (Col001) is a small-molecule compound that inhibits the interaction of Hsp47 with collagen, competitively inhibits the interaction and causes the inhibition of collagen secretion by destabilizing the collagen triple helix. .

AKB-9778 is a potent, selective inhibitor of vascular endothelial protein tyrosine phosphatase (VE-PTP) with IC50 of 17 pM.

AKOS B018304 is an arylalkylidene derivative, with polar substitution at para-position.

Akt Inhibitor VIII is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity (IC50 = 58 nM, 210 nM, and 2.12 μM; respectively).

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).

AL-335 is a potent inhibitor of hepatitis C virus (HCV) NS5B polymerase with IE50 values as low as 70 nM. AL-335 is potentially useful for the Treatment of Hepatitis C Infection. AL-335 demonstrated high levels of the nucleoside triphosphate in vitro in primary human hepatocytes and Huh-7 cells as well as in dog liver following a single oral dose. AL-335 was selected for the clinical development where it showed promising results in phase 1 and 2 trials.

ALB-127158A, also known as ALB-127158(a), is a MCH1 antagonist for the treatment of obesity.

Albiglutide is a glucagon-like peptide-1 agonist (GLP-1 agonist).

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).

ALE-0540 is a nerve growth factor (NGF) antagonist that inhibits the binding of NGF to TrkA or both p75 and TrkA with IC50 of 5.88 and 3.72 uM, respectively.

Alexamorelin is a synthetic growth hormone (GH) secretagogue.

Alflutinib (AST-2818, ASK120067) is a third generation EGFR mutation selective tyrosine kinase inhibitor, inhibits EGFR active mutations as well as T790M acquired resistant mutation.The Alflutinib free base form is not stable, so we make it the mesylate s