Antineoplastic DNA alkylating agent

Specific inhibitor of the cellular inosine-5-monophosphate dehydrogenase (IMPDH); Immunosuppressive agent

Potent and selective PDE4 inhibitor

Novel potent, orally active and selective agonist of the melanocortin receptor 4 (MC4R)

The class III antiarrhythmic agent, blocking HERG, a human cardiac delayed rectifier K+ channel

Novel Dipeptidyl peptidase IV (DPP-4) inhibitor, improving neovascularization by increasing both the number of circulating endothelial progenitor cells and endothelial nitric oxide synthetase expression

Potent and Selective 5-Lipoxygenase Inhibitor

Selective 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor

Selective 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor

Novel Macrocyclic Inhibitor of Hepatitis C Virus NS3/4A Protease with Improved Preclinical Plasma Exposure

Novel renin inhibitor

Potent TRPV1 antagonist

Potent and selective human type-1 5alpha-reductase inhibitor

Novel Selective Androgen Receptor Modulator (SARM)

Novel nonpeptide bombesin receptor subtype-3 agonist

Novel potent muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM)

Novel bombesin receptor subtype-3 (BRS-3) modulator

Novel liver-targeting inhibitor of stearoyl-CoA desaturase (SCD)

Novel agonist of G-protein coupled receptor 40 (GPR40)

Prodrug of raltegravir with enhanced colonic absorption

Novel potent and selective MKK3/6 inhibitor

Novel highly specific, potent, orally bioavailable MKP5 inhibitor