BLU-782 (BLU782) is a novel potent, selective inhibitor of Activin receptor-like kinase (ALK2) mutant R206H with binding IC50 of <10 Nm.

BIBW2992 (Afatinib, Tomtovok, Tovok) irreversibly inhibits EGFR/HER2 including EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively.

Beta-guanidinopropionic acid is a novel creatine kinase inhibitor.

BC-1215 (BC1215) is a highly unique, selective E3 ligase F box component Fbxo3 inhibitor with IL1β IC50 of 0.9 ug/mL.

BAY 87-2243 is a highly potent and selective inhibitor of hypoxia-induced HIF-1 activation.

BAY 57-1293 represents a new class of potent inhibitors of herpes simplex virus (HSV) that target the virus helicase primase complex.

BAY 2402234 (BAY2402234) is a novel potent, selective, orally bioavailable DHODH inhibitor with IC50 of 1.2 nM (human full-length DHODH).

BAR502 is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.

Azeliragon is an oral, small-molecule inhibitor of RAGE.

AZD-7624 a potent, selective, inhaled p38α MAPK inhibitor for the treatment of chronic obstructive pulmonary disease.

AZD7545 is a novel, selective small-molecule inhibitor of PDHK2 (PDH kinase2) with an IC50 of 36.8 nM and 6.4 nM for PDHK1 and PDHK2 respectively.

AZD5363, a novel pyrrolopyrimidine-derived compound, inhibits all AKT isoforms (IC50 <10 nM).

AZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, activating Wnt signaling, increases bone mass in rats.

AZ-33 is a inhibitor of LDH-A with an IC50 of 0.5 μM.

AZ20 is a novel potent and selective inhibitor of ATR kinase with IC50 of 5 nM, 8-fold selectivity over mTOR.

AWD 131-138(Imepitoin) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.

AVN-944(VX-944) is a selective, noncompetitive inhibitor of the enzyme directed against human IMPDH with Ki of 6-10 nM for IMPDH1/IMPDH2.

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.

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

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.

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.

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

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

Argatroban

APS-3-77 is the negative binder of KSR2.