A potent, selective, CNS-penetrant P2X7 antagonist with pKi of 9.1 and 7.9 for rat and huamn P2X7 channel, respectively.

A potent, selective, CNS penetrant, orally bioavailable RORγt with pIC50 of 8.3 in FRET assays.

A potent, selective, CNS penetrant dual leucine zipper kinase (DLK, MAP3K12) inhibitor with Ki of 3 nM.

A potent, selective, CNS penetrant and orally bioavailable mGlu5 positive allosteric modulator that potentiates human mGlu5 with EC50 of 130 nM.

A potent, selective, CNS penetrant and competitive orthosteric antagonist of M1 mAChR with IC50 of 132 nM, >75-fold selectivity over M2-M5.

A potent, selective, CNS penetrant 5-HT2C receptor agonist with Ki of 3 nM and EC50 of 9 nM, without significant P-gp efflux liability.

A potent, selective, cell-permeable I338G v-Src inhibitor with IC50 of 430 nM, shows no inhibition of wild-type v-Src at 300 uM.

A potent, selective, cell-active CBP/EP300 bromodomain inhibitor with IC50 of 0.47 uM for CBP.

A potent, selective, cell permeab anti-apoptotic protein kinase CK2 with Ki of 5 nM.

A potent, selective, cell active SHP2 inhibitor with IC50 of 200 nM, displays >5-fold selectivity against 20 other mammalian PTPs.

A potent, selective, brain-penetrant and orally bioavailable mGluR4 positive allosteric modulator with EC50 of 79 nM.

A potent, selective, brain-penetrant and orally bioavailable mGluR4 positive allosteric modulator with EC50 of 79 nM.

A potent, selective, brain permeable, orally available glycine transporter-1 (GlyT1) inhibitor with IC50 of 92 nM (rat GlyT1), 50-fold selectivity over GlyT2.

A potent, selective, brain penetrant, orally acitve mGluR7 allosteric agonist that inhibits forskolin-stimulated cAMP accumulation in mGluR7b CHO cells with EC50 of 64±32 nM.

A potent, selective, brain penetrant phosphodiesterase 2A (PDE2A) inhibitor with IC50 of 2 nM, >4,000-fold selectivity over PDE1 and PDE3-11.

A potent, selective, brain penetrant PDE9A inhibitor with IC50 of 1.8 nM.

A potent, selective, brain penetrant partial negative allosteric modulator of mGlu5 receptor with Ki of 14 nM, Ca assay IC50 of 32 nM.

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