AUY922 (NVP-AUY922) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Phase 1/2.

Autophinib is a novel potent autophagy inhibitor, inhibiting autophagy induced by starvation or Rapamycin by targeting the lipid kinase VPS34.

Auten-99 is a novel inhibitor of the myotubularin phosphatase Jumpy (also called MTMR14), acrossing the blood-brain barrier and exerting potent neuroprotective effects.

Aurora A inhibitor I is a selective Aurora A inhibitor (Aurora A: IC50=0.0034 μM; Aurora B IC50=3.4 μM), (B/A ratio=1000).

Auristatin E is a cytotoxic tubulin modifier with potent and selective antitumor activity; MMAE analog and cytotoxin in Antibody-drug conjugates.

Atovaquone is a medication used to treat or prevent for pneumocystis pneumonia, toxoplasmosis, malaria, and babesia.

Atipamezole(MPV1248) is an alpha-adrenoceptor antagonist with high affinity and selectivity for the alpha 2-receptor.

ATB-346 is a novel hydrogen sulphide-releasing derivative of naproxen with markedly reduced toxicity.

Atazanavir is a HIV protease inhibitor with Ki of 2.66 nM.

AT9283 is a small molecule a multi-targeted inhibitor with of 4, 1.2, 1.1 and approximate 3 nM for Bcr-Abl(T3151), Jak2 and Jak3, aurora A and B, respectively.

AT7867 is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively; little activity outside the AGC kinase family.

AT7519 is a novel multi-CDK inhibitor for CDK1/cyclin B, CDK2/Cyclin A, CDK3/Cyclin E, CDK4/Cyclin D1, CDK5/p35 and CDK6/Cyclin D3 with IC50 of 210 nM, 47 nM, 360 nM, 100 nM, 13 nM and 170 nM, respectively.

AT13387 is a selective potent Hsp90 inhibitor with IC50 of 18 nM in A375 cells, displays a long duration of anti-tumor activity.

AT13148 is a novel, oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity; AKT, p70S6K, PKA, ROCK, and SGK inhibitor.

Asunaprevir (BMS-650032) is a potent hepatitis C virus (HCV) NS3 protease inhibitor.

ASTX660 is a novel potent IAP antagonist that targets the BIR3 domain of cIAP1/2 and XIAP with IC50 of 12 nM and <40 nM.

ASP 7663 is a selective TRPA1 activator (EC50 values are ~0.5 μM in human, mouse and rat).

Ascomycin is an analog of tacrolimus with immunosuppressive, neurotrophic and antifungal activities.

Asapiprant (BGE-175) is a potent and specific antagonist of human PGD2/PTGDR signaling with Ki of 0.44 nM. BGE-175 is currently in a Phase 2 clinical trial to test whether it can prevent disease progression and mortality in older patients hospitalized wit

AS-252424 is a novel, potent and selective inhibitor of PI3Kγ with IC50 of 33 nM.

AS1517499 is a potent STAT6 inhibitor with IC50 of 21 nM.

ARV-771 is a potent bromodomain and extra-terminal (BET) proteins degrader with Kd values of 4.7, 7.6, 7.6 nM against bromodomain 2, 3 and 4, respectively.

ARS-1620 is a covalent compound with high potency and selectivity for KRAS-G12C.

ARRY-520 is a synthetic, small molecule kinesin spindle protein (KSP) inhibitor with IC50 of 6 nM.

ARQ-531 is a potent, reversible, orally available inhibitor of both wild type and C481S-mutant BTK kinase with IC50 of 0.85 and 0.39 nM,

ARQ 092 is an oral activie, potent and selective AKT inhibitor with IC50 values: 5.0 nM (AKT1); 4.5 nM (AKT2); 16 nM (AKT3).

ARN-3236 is potent, orally active and selective SIK2 inhibitor. ARN-3236 inhibited the growth of 10 ovarian cancer cell lines at an IC50 of 0.8 to 2.6 μmol/L.

ARN2966 is a potent post-transcriptional modulator of APP expression; reduces expression of APP with resultant lower production of Aβ.

Argatroban

AR7 is a retinoic acid receptor α (RARα) antagonist.