A potent and selective dopamine reuptake inhibitor with IC50 of 3.7 nM.

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.

AG-1024 (Tyrphostin) inhibits IGF-1R autophosphorylation with IC50 of 7 μM, less potent to IR with IC50 of 57 μM.

A PPARα agonist and an irreversible CPT-1 inhibitor.

AI-10-49 selectively binds to CBFβ-SMMHC and disrupts its binding to RUNX1.

Amifostine (WR2721) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer.

Acotiamide monohydrochloride trihydrate is an orally active and first-in-class gastroprokinetic agent for the treatment of functional dyspepsia. Acotiamide monohydrochloride trihydrate enhances acetylcholine released by enteric neurons through muscarinic

AMBMP hydrochloride is a Wnt canonical signaling activator. Also inhibits tubulin polymerization. Suppresses TLR2/4/5-induced inflammatory response in human monocytes. Inhibits cell proliferation and induces cell cycle arrest in MDA-MB-231 breast cancer c

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.

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 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.

Ampalex (Ampakine CX516) is an ampakine and nootropic that acts as an AMPA receptor positive allosteric modulator as a treatment for Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI).

Ammonium pyrrolidine dithiocarbamate (PDTC) is a potent nuclear factor-κB (NF-κB) inhibitor that inhibits IκB phosphorylation, blocks NF-κB translocation to the nucleus and reduces the expression of downstream cytokines.

AMG-548 is a potent and selective inhibitor of p38α with Ki of 0.5 nM, dispalys weak inhibition for p38β (Ki=3.6 nM), and >5,000-fold selectivity over p38γ and p38δ; shows >1,000-fold selectivity over other 36 kinases, and is efficacious in acute and chro

AMG-47a is a potent inhibitor of Lck and T cell proliferation; exhibits anti-inflammatory activity (ED50 = 11 mg/kg) in the anti-CD3 induced production of IL-2 in mice.

AMG-208 is a potent small molecular c-Met inhibitor with an IC50 of 9.3 nM.