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 bioavailable histamine H4 receptor antagonist with Ki of 12.5 nM, >80-fold selectivity over other histamine receptors.

A potent, selective, orally bioavailable inhibitor of class I PI3K isoforms with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/β/δ/γ, respectively.

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 inhibitor of EZH2 with Ki of < 3 nM.

A potent, selective, orally bioavailable IRAK-4 inhibitor that potently inhibits human and rat IRAK-4 activity with subnanomolar order, >30-fold selectivity over IRAK-1.

A potent, selective, orally bioavailable P2X7 receptor antagonist.

SB-649868 is a potent and selective orally active orexin (OX) 1 and OX2 receptor antagonist (pKi =9.4 and 9.5 at the OX1 and OX2 receptor, respectively).

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

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

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

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

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

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

A potent, specific acyl protein thioesterase 2 (APT-2, LYPLA2) inhibitor with IC50 of 144 nM and Ki of 120 nM, >20-fold selectivity over APT-1 and serine hydrolase enzyme family.

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

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

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

A potent, specific and nonlipid agonist of LPA2 receptor with EC50 of 3.3 uM, does not activate any of the other LPA GPCRs (>10 uM).