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.

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

Argatroban

AR-A014418 is a selective and effective GSK3β inhibitor with an IC 50 value of 104 +/- 27 nM; no significant inhibition on 26 other kinases.

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

APY0201 is a potent, highly selective PIKfyve kinase inhibitor.

APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity.

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

APS-2-79 is a novel modulator of KSR-dependent MAPK signalling,KSR2,IC50=120 nM

Apoptosis Activator 2 activates caspases in a cytochrome c-dependent manner and induces apoptosis in tumor cells.

APO866 effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase) with IC50 of 0.09 nM.

Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively.

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.

Apatinib (YN968D1) is an orally bioavailable, selective VEGFR2 inhibitor with IC50 of 1 nM.

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.

Anle138b is a novel oligomer modulator.

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.

Anacetrapib (MK0859) is a potent, selective, reversible rhCETP and mutant CETP(C13S) inhibitor with IC50 of 7.9 nM and 11.8 nM, increases HDL-C and decreases LDL-C, does not increase aldosterone or blood pressure. Phase 3.

Anacardic acid inhibits the histone acetyltransferase (HAT) activity of the transcription co-activators p300 and p300/CREB-binding protein-associated factor (pCAF) with IC50 values of 8.5 and 5 µM, respectively.

AN3365 is a first-in-class antibiotic that demonstrates potent activity across a wide spectrum of Gram-negative bacteria, including those resistant to many other antibiotics.

AN-2728 is a topically administered, boron-containing, anti-inflammatory compound that inhibits PDE4 activity and thereby suppresses the release of TNFalpha, IL-12, IL-23 and other cytokines.

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.

An antibiotic that inhibits eukaryotic protein synthesis by inhibiting peptidyl transferase or the 80S ribosome system.

AMPPD, 1,2-dioxo-cyclohexane derivatives, is a new biochemistry ultrasensitive alkaline phosphatase substrate.