ARM390 is a non-peptidic, low-internalizing δ-selective opioid receptor agonist.

ARN-509 is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM, useful for prostate cancer treatment.

ARS-853 is a selective, covalent inhibitor of KRAS-G12C that inhibits mutant KRAS driven signaling by binding to the GDP bound oncoprotein and preventing activation.

AS 8351 induces reprogramming of human fetal lung fibroblasts into functional cardiomyocytes, in combination with CHIR 99021, A83-01, BIX 01294, SC1, Y-27632, OAC2, SU 16f and JNJ 10198409.

AS-604850 is a selective, ATP-competitive PI3Kγ inhibitor with IC50 of 250 nM, over 80-fold selectivity for PI3Kγ than PI3Kδ/β, and 18-fold more selective for PI3Kγ than PI3Kα.

ASK1-IN-1 is an apoptosis signal regulating kinase 1 (ASK1) inhibitor extracted from patent WO2016025474A1, Compound 4.

ASP5878 is a selective FGFR inhibitor, to treat FGFR3-dependent urothelial cancer with or without chemoresistance.

ASP-9521 is a potent, selective and orally available AKR1C3 inhibitor with an IC50 of 11 nM for human AKR1C3.

Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells.

AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM; less potent to CDK3 and little active to CDK7.

Atractylenolide II has antiinflammatory activity, it can inhibit platelets activities and thrombus formation. Atractylenolide II has cytotoxic/apoptotic effects may via p38 activation ,ERK and Akt inactivation, p53 dependent, it also has antimelanoma effe

Atractylenolide III, a potential house dust mite control agent, has neuroprotection, gastroprotective, anti-cancer, and anti-inflammatory activities, it also may control immunological reactions by regulating the cellular functions of IL-6 in mast cells.

Atractylone has inhibitory effects on mast cell-mediated allergic reactions, it regulates the degranulation of mast cell, proves its potential in the treatment of mast cell-mediated allergic reactions.

Atrasentan Hcl(A-147627) is an endothelin antagonist receptor (IC50=0.0551 nM, ETA) being developed for the treatment of prostate cancer.

AU1235 is an adamantyl urea inhibitor of Mycobacterium tuberculosis.

Avanafil(TA-1790) is a potent and highly selective phosphodiesterase-5(PDE-5) inhibitor(IC50=5.2 nM) for erectile dysfunction; lower selectivity against PDE1, PDE6, and PDE11.

FB23 is a potent and selective FTO demethylase inhibitor with an IC50 of 60 nM. FB23 directly binds to FTO and selectively inhibits FTO's mRNA N6-methyladenosine (m6A) demethylase activity.

WYE-354 is a potent cell-permeable inhibitor of mTOR (IC50 = 4.3 nM) which blocks signaling through both mTOR complex 1 (mTORC1) and mTORC2.1,2 It is a much weaker inhibitor of phosphatidylinositol 3-kinase α (IC50 = 1026 nM) and other kinases.3 WYE-354 i

N-desmethyl Enzalutamide(N-desmethyl MDV3100) is a major metabolite of Enzalutamide, Enzalutamide(MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM.

AVex-73 is a muscarinic M1 agonist potentially for the treatment of Alzheimer's disease

Avitinib is an orally available, irreversible, epidermal growth factor receptor (EGFR) mutant-selective inhibitor, with potential antineoplastic activity.

Avitinib is an orally available, irreversible, epidermal growth factor receptor (EGFR) mutant-selective inhibitor, with potential antineoplastic activity.

NIK SMI1 is a potent, selective small molecule inhibitor of NF-κB inducing kinase (NIK) with Ki of 230±170 pM; only inhibits 3 out of 222 off-target kinases (KHS1, LRRK2, and PKD1) with >75% inhibition at 1 uM; potently inhibits anti-LTβR-induced nuclear p52 levels in anti-LTβR-stimulated HeLa cells, with no effect on canonical signaling; inhibits BAFF and CD40 signaling, suppresses immune responses in vivo; suppresses disease biomarkers and improves survival and renal function in NZB/W F1 mice.

ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor.

AZ191 is a potent and selective DYRK1B inhibitor with IC50 of 17 nM, about 5- and 110-fold selectivity over DYRK1A and DYRK2, respectively.

AZ304 is a novel potent, dual BRAF inhibitor targeting the kinase domains of wild type BRAF, V600E mutant BRAF and wild type CRAF with IC50 of 79 nM, 38 nM and 68 nM, respectively.

AZ31 is a novel ATM inhibitor.

CYM50308 is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC50 of 56 nM. CYM50308 displays 37-fold more selective for S1P4-R than S1P5-R. CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM.

Unique F-box/LRR-repeat protein 2 (FBXL2) activator

AZ505 ditrifluoroacetate is a potent and selective SMYD2 inhibitor with IC50 of 0.12 μM.