ARN726 is a potent, selective, orally bioavailable N-acylethanolamine acid amidase (NAAA) inhibitor with IC50 of 63 nM (r-NAAA) and 27 nM (h-NAAA).

ARN-3261 is a potent, selective, orally available salt inducible kinase SIK2 and SIK3 inhibitor with IC50 of 11 nM and 19 nM, respectively.

ARN19874 (ARN-19874) is the first selective, cell-active inhibitor of N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD) with IC50 of 33.7 uM.

ARN14494 (ARN-14494) is a potent, small molecule serine palmitoyltransferase (SPT) inhibitor with IC50 of 27.3 nM.

ARN077 is the first potent, selective N-acylethanolamine acid amidase (NAAA) inhibitor with IC50 of 7 nM on both rat NAAA and human NAAA.

AR-HO47108 is a potent, selective acid pump antagonist (potassium-competitive acid blocker or P-CAB) that reversiblely inhibits gastric H+/K+-ATPase with pIC50 of 7.0.

Arg-AMS is a potent nanomolar inhibitor of arginyl tRNA synthetase, which displays tightly bound inhibitory characteristics for the A-domains in non-ribosomal peptide synthetases (NRPS) enzymes.

AR-C155858 is a potent monocarboxylate transporter MCT1 and MCT2 with Ki of 2.3 nM and <10 nM, displays no activity at MCT4.

AR-C102222 is a potent, selective iNOS inhibitor with IC50 of 35 nM, dislapys 3,000-fold and 20-fold selectivity over eNOS and nNOS respectively.

AR03 (AR-03, AR 03, Ape1 repair inhibitor 03) is a novel small molecule inhibitor of DNA repair protein apurinic/apyrimidinic endonuclease 1 (APE1) endonuclease activity with IC50 of 5 uM.

AQW-051 is a novel, potent and selective, orally bioavailable, brain-penetrant α7 nAChR partial agonist with pKd of 7.56.

AQ-13 dihydrochloride is an aminoquinoline antimalarial drug that is effective against chloroquine-resistant strains of Plasmodium falciparum.

AQ-101 is a novel small-molecule anthraquinone analog that induces MDM2 protein degradation (Kd=0.37 uM) through a self-ubiquitination and proteasome-mediated mechanism, leading to activation of p53.

APX2014 (APX-2014) is a novel potent inhibitor of reduction-oxidation factor 1-apurinic/apyrimidinic endonuclease 1 (Ref-1/APE1) with IC50 of 0.2 uM for redox EMSA inhibition.

APX2009 (APX-2009) is a novel potent inhibitor of reduction-oxidation factor 1-apurinic/apyrimidinic endonuclease 1 (Ref-1/APE1) with IC50 of 0.45 uM for redox EMSA inhibition.

APTO-253 is a small molecule inducer of KLF4, stabilizes G-quadruplex DNA and reduces MYC mRNA expression and protein levels.

APTO-253 is a novel small molecule with potent anti-tumor activity in cancer cells via induction of the gene that expresses the Krüppel-like factor 4 (KLF4) master transcription factor, leading to cell cycle inhibition and programmed cell death.

Aprotinin is a serine protease inhibitor isolated from bovine lung which inhibits trypsin and chymotrypsin with Ki values of 0.06 pM and 9 nM, respectively.

Apricitabine is a novel nucleoside reverse transcriptase inhibitor for the treatment of HIV infection that is refractory to existing drugs

Apogossypol (NSC 736630) is a Bcl-2 family antagonist that binds to Bcl-XL, Bcl-2 and Bcl-xL with IC50 of 2.6, 2.8 and 3.69 uM, respectively.

Aplaviroc (GSK-873140.

apelin receptor.

APD916 is a potent and selective antagonist of the H3 receptor with Ki of 0.7 nM for rH3R.

APD-371 (APD371, Olorinab) is a potent, selective and orally available CB2 agonist with EC50 of 6.2 nM; displays no activity against CB1 receptors (EC50>10 uM); exhibits activity in rat model of osteoarthritis pain.

APA modulator T5 is a small modulator of alternative polyadenylation (APA), modulates endogenous APA via nonkinase-mediated pathways and promotes distal-to-proximal (DtoP) APA usage in multiple transcripts.

APA modulator T4 is a small modulator of alternative polyadenylation (APA) with IC50 of 2.1 uM in reporter assays, modulates endogenous APA via nonkinase-mediated pathways and promotes distal-to-proximal (DtoP) APA usage in multiple transcripts.

AP219 is a control compound for AP39, containing the triphenylphosphonium scaffold but lacking the H2S-releasing portion.

AP14145 (AP-14145) is a potent, selective negative allosteric modulator of KCa2.2 and KCa2.3 with equal potency (IC50=1.1±0.3 uM).

AOH1160 is a potent, first-in-class, orally available small molecule inhibitor of Proliferating cell nuclear antigen (PCNA).

ANY1 (FosA inhibitor ANY1) is a small molecule active site inhibitor of FosA (metal-dependent glutathione S-transferase) with IC50 of 5.1 uM (K. pneumoniae FosA).