A potent, selectiive inhibitor of WNK1 kinase with IC50 of 95 nM, shows IC50 of 1.39 uM in the cellular OSR1 phosphorylation assay with reasonable aqueous solubility..

A potent, second-generation BET protein degrader that exhibits superior selectivity, potency and antitumor activity.

A potent, second generation HCV NS3 serine protease inhibitor with Ki of 6 nM.

A potent, reversible type III inhibitor of SAHH (S-adenosyl-L-homocysteine hydrolase) with Ki of 17.9 nM.

A potent, reasonably selective cannabinoid CB2 agonist with Ki of 0.4 nM, 25-fold selectivity over CB1 receptor..

A potent, reasonably selective agonist of peripheral cannabinoid receptor with Ki of 11 nM for CB2, 22-fold selectivity over the psychoactive CB1 receptors (Ki=245 nM)..

A potent, picomolar, dual inhibitor of Aurora A and B with IC50 of 0.02 and 0.03 nM, respectively.

A potent, orally bioavailable, small-molecule inhibitor of HDM2/p53 protein-protein interaction.

A potent, orally bioavailable P-selectin inhibitor with improved pharmacokinetic properties and oral efficacy in models of vascular injury..

A potent, orally bioavailable brain‐penetrant, NR2B-selective NMDA receptor (GluN2B) antagonist with Ki and IC 50 of 8.1 nM and 3.6 nM respectively, with no off-target activity.

A potent, orally available, dual ACE-neutral endopeptidase (vasopeptidase) inhibitor with IC50 of 12 and 63 nM, respectively.

A potent, orally active, and irreversible pan-Caspase protease inhibitor with IC50 of <0.08 to 7 nM for inhibition of activated caspase 3, 6 and 8.

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, 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.