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

A potent, relatively selective G protein-coupled receptor kinase GRK2 inhibitor with IC50 of 66 nM.

A potent, relatively selective G protein-coupled receptor kinase GRK2 inhibitor with IC50 of 280 nM.

A potent, relatively selective and orally active adenylyl cyclase 1 (AC1) inhibitor with IC50 of 10 uM (cAMP production inhibition).

A potent, reasonably selective Chk1 inhibitor with cell IC50 of 5 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, pan-genotype HCV NS5A inhibitor with replicon EC90 of 0.003, 0.016, 0.067, 0.036, 0.007, and 0.007 nM for GT1a, GT1a L31V, GT1a Y93H, GT2b, GT3a, and Gt4a, respectively..

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

A potent, orally bioavailable, irreversible proteasome inhibitor with potent antimyeloma activity (IC50<60 nM).

A potent, orally bioavailable, full agonist of GPR40/FFA1 with EC50 of 0.16 uM.

A potent, orally bioavailable, dual XIAP/cIAP1 inhibitor with EC50 of 5.1/0.32 nM, respectively.

A potent, orally bioavailable, dual Src/Abl kinase inhibitor with IC50 of 0.5, 0.4, 0.5 and <1 nM for Src, Lck, Yes and Bcr-Abl, respectively.

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 available hydrophobic aminopeptidase inhibitor that structurally mimics the aminopeptidase inhibitor Tostedostat..

A potent, orally active, dual NK1 receptor antagonist (IC50=0.5 nM) and SERT inhibitor (IC50=5.2 nM).

A potent, orally active, centrally acting aminopeptidase inhibitor, the prodrug of the specific and selective aminopeptidase A inhibitor EC33.

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).