Potent and selective competitive inhibitor of human epithelial 15-lipoxygenase-2 (15-LOX-2)

Novel selective and potent inhibitor of recombinant h12/15-LOX and cellular mouse 12/15-LOX (m12/15-LOX)

Second generation 5-LO inhibitor, blocking the production of leukotrienes

Novel potent DNA binding agent, stabilizing topoisomerase-dependent cleavage, demonstrating exceptional efficacy against a number of murine and human tumor models

Novel IKK2 inhibitor, decreasing NF-κB activation and down-regulating the expression of a number of inflammatory proteins

Selective inhibitor of Myosin Light Chain Kinase (MLCK)

Novel Inhibitor of Scavenger Receptor BI-mediated Lipid Uptake

Novel endoplasmic reticulum proteostasis modulator, enhancing insulin production in pancreatic β cells, inhibiting the UPR, alleviating ER stress and protein aggregation, improving intracellular insulin levels and insulin secretion

Novel highly specific, potent, orally bioavailable MKP5 inhibitor

Novel potent and selective MKK3/6 inhibitor

Prodrug of raltegravir with enhanced colonic absorption

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

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

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

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

Novel nonpeptide bombesin receptor subtype-3 agonist

Novel Selective Androgen Receptor Modulator (SARM)

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

Potent TRPV1 antagonist

Novel renin inhibitor

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

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

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

Potent and Selective 5-Lipoxygenase Inhibitor

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

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

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

Potent and selective PDE4 inhibitor

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

Antineoplastic DNA alkylating agent