Apicidin (OSI 2040) is a fungal metabolite that exhibits potent, broad spectrum antiprotozoal activity in vitro, potently inhibits HDAC with IC50 of 0.7 nM in an enzyme activity assay.

Apilimod(STA 5326) mesylate is a potent IL-12/IL-23 inhibitor, IL-12 production in cultures of IFN-r/LPS–stimulated human PBMCs is strongly inhibited by STA-5326 with an IC50 of 10 nM.

Aplaviroc (GSK-873140.

Aplaviroc, also known as AK-602; GW-873140; GW873140A; ONO-4128, is a CCR5 entry inhibitor for the potential treatment of HIV infection. Aplaviroc (GW873140) binds specifically to human cellular CC chemokine receptor 5 (CCR5) and demonstrates potent anti-human immunodeficiency virus activity in vitro in the subnanomolar range. In vitro studies show that aplaviroc selectively inhibits the binding of a particular monoclonal antibody, 45531, to CCR5.

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.

Apomorphine hydrochloride hemihydrate is a non-selective dopamine agonist which activates both D1-likeand D2-like receptors, with some preference for the latter subtypes..

Apoptozole is an inhibitor of heat shock protein 70 (Hsp70; 65% inhibition at 200 μM) that acts by blocking its ATPase activity.

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

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.

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

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

APX001 (APX 001A;E1210) is a novel broad-spectrum antifungal agent that inhibits the fungal protein Gwt1, demonstrates significantly acitive MIC50 and MIC90 values of 0.004 and 0.031 ug/ml (16 strains of C. auris).

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.

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.

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.

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

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

AQX 1125 (Rosiptor) is a specific, orally bioavailable SHIP1 activator.

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.

AR231453 is a potent and selective small molecule agonist of GPR119 that enhances glucose-dependent insulin secretion and glucagon-like peptide 1 (GLP-1) release; Antidiabetic agent.

ARA-290 (Cibinetide) is a non-erythropoietic erythropoietin (EPO) derivative.

Ara-G (9-β-D-Arabinofuranosyl guanine) is an inducer of apoptosis, inhibitor of DNA synthesis, an antimetabolite, and antineoplastic.