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

A potent, specfic CXCR2 antagonist that inhibits IL8 down-regulation of forskolin-induced cAMP with IC50 of 7.79 uM.

A potent, specfic casein kinase 1δ (CK1δ) inhibitor with IC50 of 40 nM.

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. covalent protein lysine methyltransferase SETD8 inhibitor with IC50 of 804 nM.

A potent, selective, reversible, ATP-competitive Chk2 inhibitor with IC50 of 0.2 uM.

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 PI3Kδ inhibitor with IC50 of 2.6 nM.

A potent, selective, orally bioavailable P2X7 receptor antagonist.

A potent, selective, orally bioavailable Mps1 kinase inhibitor with IC50 of 11 nM.

A potent, selective, orally bioavailable MDM2-p53 interaction inhibitor with HTRF IC50 of 1.1 nM, SJSA-1 EdU IC50 of 68 nM.

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 GPR120 agonist with EC50 of 42 nM in calcium flux assays.