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 c-MET inhibitor with IC50 of 0.93 nM.

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

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 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 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 AKT inhibitor with IC50 of 2.3 uM for Akt1.

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

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 bioavailable factor Xa (FXa) inhibitor for prevention and treatment of thromboembolic diseases..

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

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

A potent, selective, and oral renal outer medullary potassium channel (ROMK) inhibitor with IC50 of 68 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 irreversible BTK inhibitor with IC50 of 7 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 bioavailable OX2 receptor antagonist with Kb of 4.5 nM.

A potent, selective, allosteric LMPTP inhibitor with IC50 of 1.68 uM, displays good selective against other phosphatases.

A potent, selective, allosteric CCR2 antagonist with IC50 of 103 nM..

A potent, selective, allosteric CCR2 antagonist with binding IC50 of 5.1 nM.

A potent, selective α2B adrenoceptor antagonist with pKd of 8.8, 200-fold selectivity over α2A, and α2D receptors.

A potent, selective α2A-adrenoceptor antagonist with Ki of 1.7 nM, 80-fold selectivity over α2B-adrenergic receptors.

A potent, selective ubiquitin-specific protease USP8 inhibitor with IC50 of 0.85 uM.

A potent, selective ubiquitin-specific protease USP8 inhibitor with IC50 of 0.56 uM.

A potent, selective TRPM8 agonist with EC50 of 12 uM, a cooling agent.

A potent, selective TRPC6 channel inhibitor with IC50 of 0.1-0.6 uM, 12- and 5-fold selectivity over related TRPC3 and TRPC7.

A potent, selective translocator protein 18 kDa (TSPO/PBR) agonist with IC50 of 2.59 and 1.03 nM in competing with [3H]-PK11195 for binding to membrane preparations from rat cerebral cortex and ovary, respectively.

A potent, selective transcriptional CDK inhibitor with Ki of 2.3 and 0.38 nM for CDK7 and CDK9, respectively.

A potent, selective TLR9 antagonist with IC50 of 13 nM (human TLR9), displays 75-fold selectivity over TLR7 and no activity against TLR8 (IC50>10 uM).