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 MDM2-p53 interaction inhibitor with HTRF IC50 of 1.1 nM, SJSA-1 EdU IC50 of 68 nM.

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

A potent, selective, orally bioavailable P2X7 receptor antagonist.

A potent, selective, orally bioavailable PI3Kδ inhibitor with IC50 of 2.6 nM.

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..

LY2033298 is a robust allosteric potentiator that is highly selective for the human M4 muscarinic acetylcholine receptor subtype. LY2033298 enhances inhibition by oxotremorine of light-induced phase shifts in hamster circadian activity rhythms.

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 Cdc25 dual specificity phosphatase inhibitor with Ki of 32/96/40 nM for Cdc25A/B/C, respectively.

SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist.

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

A potent, selective. covalent protein lysine methyltransferase SETD8 inhibitor with IC50 of 804 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.