A potent, selective agonist of the orphan GPR88 receptor with EC50 of 877 nM.

A potent, selective agonist of the human and rat CCK1 receptor with Ki of 36 nM.

A potent, selective agonist of PBR/TSPO that inhibits [3H]PK 11195 binding to crude mitochondrial preparations of rat whole brain with IC50 of 0.92 nM..

A potent, selective adenylyl cyclase AC5/6 inhibitor with IC50 of 7.7/17 uM, respectively.

A potent, selective A2A adenosine receptor antagonist with Ki of 6.6 nM.

A potent, selective 5-HT2C receptor agonist with IC50 of 20 nM in HEK293 cells-exppressed 5-HT2C, shows weakly activity for 5-HT2A.

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, 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.