A potent, selective and orally active SGLT2 inhibitor with IC50 of 8.9 nM, 280-fold selectivity over SGLT1.

A potent, selective and orally active cytosolic phospholipase A2α (cPLA2α) inhibitor with IC50 of 20 nM.

A potent, selective and orally active CRF1 receptor antagonist with Ki of 12 nM, shows no affinity for CRF2 receptor (Ki>10 uM).

A potent, selective and orally active CRF1 receptor antagonist with IC50 of 6.1 nM, >1,000-fold selectivity over CRF-binding protein and biogenic amine receptors.

A potent, selective and orally active COX-2 inhibitor with IC50 of 26 nM for inhibition of the COX-2-dependent production of PGE2 in human osteosarcoma cells.

A potent, selective and orally active adenosine A1 receptor antagonist with Ki of 1.3 nM.

A potent, selective and oral lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with IC50 of 0.23 nM, for the treatment of Alzheimer's disease and atherosclerosis..

A potent, selective and cell permeable inhibitor of mitotic kinesin Eg5 with IC50 of 0.8 uM, does not interact with other microtubule motor proteins.

A potent, selective and cell active Hedgehog acyltransferase (Hhat) inhibitor with IC50 of 0.87 uM.

A potent, selective and ATP-competitive inhibitor of IKK2 with IC50 of 60 nM and Ki of 20 nM, also interfers directly with FLT3 kinase activation.

A potent, selective ALK5 inhibitor with IC50 of 4.8 nM, >100-fold selectivity over 95 different kinases.

A potent, selective agonist of the rat (EC50=97 nM) and human (EC50=23 nM) TRPA1 channel.

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 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, 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, 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.