A potent, specific P-gp inhibitor with Kd of 5.1 nM.

A potent, specific mechanism-based human NAD(P)H: quinone oxidoreductase 1 (NQO1) inhibitor that demonstrates efficient inactivation of NQO1 at 100 nM in in cellular systems.

A potent, specific inhibitor of the SGK1 kinase activity, induces autophagy, apoptosis and ER stress in cancer cells.

A potent, specific immunoproteasome β5 subunit inhibitor..

A potent, specific immunoproteasome β5 subunit inhibitor with IC50 of 44 nM, 105 and 225-fold selectivity over β2i and β1i subunit, respecitvely.

A potent, specific immunoproteasome β5 subunit inhibitor with IC50 of 17 nM, 21-fold and 13-fold selectivity for β5 over LMP7 and LMP2 subunits, respecitvely..

A potent, specific immunoproteasome β1i (LMP2) subunit inhibitor with IC50 of 104 nM, 144- and 10-fold selectivity over β1c and β5 subunit respectivey.

A potent, specific immunoproteasome LMP7 subunit inhibitor with IC50 of 25 nM, >100-fold selectivity over β5c, β1i, β1c, β2i and β2c subunits (IC50>3 uM).

A potent, specific CDC-like kinase (CLK) inhibitor with IC50 of 78, 16 and 86 nM for CLK1, 2 and4, respectively.

A potent, specific BMP receptor activin receptor-like kinase 3 (ALK3) antaognist with Ki of 5.4 nM.

A potent, specific and orally bioavailable soluble epoxide hydrolase (sEH) inhibitor with IC50 of 1.3 nM.

A potent, specific and competitive inhibitor of human neutrophil elastase with IC50 of 44 nM.

A potent, specific and allosteric mGluR1 antagonist with IC50 of 6 nM and 1.4 nM for human and mouse mGluR1, respectively..

A potent, small molecule inhibitor of the proteasome subunit Rpn11 with IC50 of 2.5 uM..

A potent, small molecule fetal hemoglobin (HbF) inducer with EC50 of 100 nM.

A potent, selectove δ-opioid receptor agonist with Ki of 0.16 nM, dispalys 133.5-fold and 960.5-fold selectivity over μOR and κOR respectively.

A potent, selective, reversible rhomboid proteases inhibitor with Ki of 45 nM for GlpG .

A potent, selective, reversible inhibitor of PTP SHP2 with IC50 of 5.5 uM, exhibits >3-fold selectivity for SHP2 over other PTPs.

A potent, selective, reversible and competitive antagonist of glucagon receptor with high binding affinity (IC(=50=6.6 nM) and functional cAMP activity (IC50=15.7 nM).

A potent, selective, reversible and ATP-competitive inhibitor of Tpl2 kinase with IC50 of 50 nM.

A potent, selective, peripherally active and orally available FAAH inhibitor for treatment of chronic prostatitis/chronic pelvic pain syndrome..

A potent, selective, peptide-mimetic PAR-1 antagonist with binding IC50 of 0.44 uM, with no effect on PAR-2, PAR-3, or PAR-4.

A potent, selective, orally bioavailable P2X7 receptor antagonist.

A potent, selective, orally bioavailable inhibitor of CXCR4 that efficiently inhibits SDF-1α binding to CXCR4 with IC50 of 0.61 nM.

A potent, selective, orally bioavailable BET bromodomain inhibitor with IC50 of 7.2 and 28.2 nM for BRD4 BD2 and BRD4 BD1, respectively.

A potent, selective, orally available inhibitor of HCV NS3/4A protease with Ki of 0.05 and 0.9 nM for GT1b and 2a protease, respectively.

A potent, selective, orally available IAP antagonist with IC50 of 1.3, 2.2 and 200 nM for cIAP-1, cIAP-2 and XIAP, respectively.

A potent, selective, orally available GPR40 agonist with EC50 of 3.7 nM.

A potent, selective, orally available GlyT1 inhibitor with IC50 of 29 nM, demonstrates excellent in vivo occupancy of GlyT1 transporters in vivo..

A potent, selective, orally available GlyT1 inhibitor with IC50 of 1.6 nM, weakly inhibits rat GlyT2 (IC50=138 nM).