A potent, long acting, orally active, selective ETA receptor antagonist that binds competitively to human ETA receptor with Ki of 0.43 nM, IC50 of 1.4 nM.

A potent, long acting, reversible and competitive DPP-4 inhibitor with IC50 of 0.9 nM.

A potent, mixed sigma2 agonist and sigma1 antagonist with Ki of 0.28 and 13.0 nM, respectively.

A potent, mixed sigma2 agonist and sigma1 antagonist with Ki of 0.28 and 13.0 nM, respectively.

CEP-11981 is a potent, multi-targeted, orally active, pan-VEGFR, TIE-2 and FGFR1 inhibitor with IC50 of 3-100 nM.

A potent, mutant-selective PfDHODH inhibitor with IC50 of 210 nM for 3D7 E182D PfDHODH.

A potent, noncompetitive TRPV1 antagonist that abrogates capsaicin and pH-evoked TRPV1 channel activity with submicromolar activity.

A potent, noncovalent SARS-CoV papain-like protease (PLpro) inhibitor with IC50 of 2.6 uM.

A potent, non-prostanoid prostacyclin partial agonist that potently inhibits human (IC50=35 nM), rabbit (IC50=136 nM) and rat (IC50=1.3 uM) platelet aggregation.

A potent, non-selective tyrosine protein kinase inhibitor for Trk family, CaMK and other phosphorylase kinases.

A potent, nonselective, brain penetrant, full agonist at both the central CB1 and peripheral CB2 receptors with Ki of 4.6 and 0.31 nM, respectively.

A potent, oral active glucagon receptor antagonist blocking the glucagon effect for the treatment of T2DM.

A potent, orally active dual modulator of FXR and soluble epoxide hydrolase (sEH) that exertss partial FXR agonism (pEC50=7.7) and sEH inhibitory activity (pIC50=8.4).

A potent, orally active gap-junction modifier.

A potent, orally active gap-junction modifier.

A potent, orally active hepcidin production inhibitor with IC50 of 39 nM, with low kinase inhibitory activity.

A potent, orally active iNOS inhibitor (IC50=10 nM, NO release DLD-1 cells) that prevents dimerization of iNOS, but has no effect on the expression or enzyme activity of iNOS.

A potent, orally active microsomal triglyceride transfer protein (MTP) inhibitor that inhibits both human and rodent MTP with IC50 of 2 nM.

A potent, orally active p38 MAPK inhibitor with IC50 of 50 nM, significantly decreases incidence of arthritis in mouse collagen-induced arthritis..

A potent, orally active PfDHODH inhibitor (IC50=0.3 uM) with antimalarial activity.

A potent, orally active sigma receptor antaognist with Ki of 27 and 7 nM for σ1 and σ2, respectively.

A potent, orally active γ-secretase inhibitor with cell IC50 of 0.3 nM.