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.

ATN-224 is a choline salt of tetrathiomolybdate and an inhibitor of superoxide dismutase 1 (SOD1; IC50s = 2.91 and 3.51 µM in human and mouse blood cells, respectively, in vitro).

ATF6 agonist compound A147 is a specific, small molecule agonist of transcription factor ATF6, activates ATF6 and influences differentiation of stem cells.147 has broad antiviral activity against multiple DENV strains and serotypes and that the compound i

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.

Aripiprazole lauroxil, an N-acyloxymethyl prodrug of aripiprazole, is a Long-acting injectable (LAI) typical antipsychotic for schizophrenia.

Argatroban

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

APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119 respectively.

Apatinib is an orally bioavailable, small-molecule receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities.

Apararenone (MT-3995) is a novel potent, selective non-steroidal mineralocorticoid receptor antagonist for the treatment of diabetic nephropathies and non-alcoholic steatohepatitis..

AP1867 is a synthetic FKBP12F36V-directed ligand.

Anastrozole is known to inhibit the CYP19 enzyme (aromatase, IC50 = 15 nM) that converts androgens to estrogens. Anastrozole has been seen to reversibly bind to the CYP19 enzyme through competitive inhibition.

An irreversible, dual EGFR/HER2 inhibitor with IC50 of 0.5/0.4/10/14 nM for wt EGFR/EGFR L858R/EGFR L858R+T790M/HER2 respectively.

An irreversible inhibitor of carnitine palmitoyltransferase-1 (CPT-1) that inhibits fatty acid β-oxidation in rat liver with IC50 of 5-20 nM.

An ionophore antibiotic derived from S. hygroscopicus that acts as a potassium ionophore promoting K+/H+ exchange across mitochondrial membranes.