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

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

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

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 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 hepcidin production inhibitor with IC50 of 39 nM, with low kinase inhibitory activity.

A potent, orally active gap-junction modifier.

A potent, orally active gap-junction modifier.

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

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

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

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

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

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

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, ligand-efficient, and cell-active inhibitor menin-MLL interaction with IC50 of 56 nM, Kd of 85 nM.

A potent, irreversible, and orally active inhibitor of steroid sulfatase (STS) with IC50 of 65 pM in intact MCF-7 cells.

A potent, irreversible inhibitor of human tissue transglutaminase (hTG2)..

A potent, irreversible inhibitor of human tissue transglutaminase (hTG2)..

A potent, irreversible and cell permeable inhibitor of tissue transglutaminase with IC50 of 20 nM..

A potent, highly specific JAK3 inhibitor with IC50 of 4 nM.

A potent, highly selective, orally active MDM2-p53 interaction inhibitor with IC50 of 4 nM.

A potent, highly selective, CNS penetrant mGlu7 negative allosteric modulator with IC50 of 0.76 uM.

A potent, highly selective, brain-penetrant NOP-R (Nociceptin/orphanin FQ receptor) agonist with EC50 of 8.8 nM.

A potent, highly selective α4β1 integrin antagonist with Kd of <10 pM.

A potent, highly selective renin inhibitor with IC50 of 0.47 nM.

A potent, highly selective renin inhibitor with IC50 of 0.47 nM.

A potent, highly selective PI3Kβ/δ inhibitor with IC50 of 7.8/5.3 nM respectively, with liitle to no activity on PI3Kα/γ (IC50=850/>10,000 nM).