A potent, selective, and bioavailable OX2 receptor antagonist with Kb of 4.5 nM.

A potent, selective, and centrally active positive allosteric modulator of AMPAR-mediated neurotransmission, which increase ion channel flux in the presence of agonist by suppressing desensitization and/or deactivation of the receptors..

A potent, selective, and centrally active positive allosteric modulator of AMPAR-mediated neurotransmission, which increase ion channel flux in the presence of agonist by suppressing desensitization and/or deactivation of the receptors..

A potent, selective, and irreversible BTK inhibitor with IC50 of 7 nM.

A potent, selective, and irreversible inhibitor of SSAO/VAP-1 (AOC3) with Ki of 37 nM, IC50 of <10 nM.

A potent, selective, and oral renal outer medullary potassium channel (ROMK) inhibitor with IC50 of 68 nM.

A potent, selective, and orally active p53-MDM2 antagonist with IC50 of 6 nM.

A potent, selective, and orally active p53-MDM2 antagonist with IC50 of 7 nM.

A potent, selective, and orally bioavailable factor Xa (FXa) inhibitor for prevention and treatment of thromboembolic diseases..

A potent, selective, and orally bioavailable ghrelin receptor (GHSR) inverse agonist with binding pKi of 8.36.

A potent, selective, and orally bioavailable inhibitor of interleukin-1 receptor-associate kinase-4 (IRAK4) with IC50 of 2.8 nM, 217- and 892-fold selectivity over IRAK-1 and TAK1, respectively.

A potent, selective, and orally efficacious pan-Pim inhibitor with IC50 of 5/25/16 nM for Pim1/2/3, respectively.

A potent, selective, ATP competitive AKT inhibitor with IC50 of 2.3 uM for Akt1.

A potent, selective, ATP-competitive and orally acitve Rho kinase inhibitor with IC50 of 33.1 and 8.5 nM for ROCK1 and ROCK2, respectively.

A potent, selective, ATP-competitive and orally bioavailable inhibitor of VEGFR-2 with Ki of 0.7 and 8.8 nM for unactivated and fully phosphorylated VEGFR-2, respectively.

A potent, selective, ATP-competitive Chk1 and Chk2 inhibitor with IC50 of 4.4 nM and 4.5 nM, respectively.

A potent, selective, ATP-competitive Chk1 inhibitor with IC50 of 13.3 nM.

A potent, selective, ATP-competitive c-MET inhibitor with IC50 of 0.93 nM.

A potent, selective, ATP-competitive inhibitor of IKKβ kinase with Ki of 2 nM.

A potent, selective, ATP-competitive inhibitor of IKKβ kinase with Ki of 2 nM.

A potent, selective, ATP-competitive inhibitor of MAP4K4 with IC50 of 1.9 uM, without effect on other stress pathway related kinases.

A potent, selective, ATP-competitive ITK inhibitor with IC50 of 19 nM.