A potent, selective, orally active 5-HT3 receptor agonist with high affinity for canine intestinal smooth muscle 5-HT3 receptors.

A potent, selective, orally acitve SGLT2 inhibitor with IC50 of 2.26 nM, 1650-fold selectivity over SGLT1.

A potent, selective, non-peptidic integrin α4β1 (VLA-4) antagonist with IC50 of 9 nM, displays 200-fold selectivity over α4β7 (IC50=2.1 uM).

A potent, selective, nonpeptide vasopressin V1A and V2 receptor antagonist with Ki of 0.48 nM and 3.04 nM respectively.

A potent, selective, non-peptide NK1 receptor antagonist with Ki of 0.74 nM, IC50 of 1.6 nM.

A potent, selective, noncovalent FAAH inhibitor with IC50 of 28 nM toward human FAAH and 100 nM toward rat FAAH.

A potent, selective, non-competitve inhibitor of 15-lipoxygenase (15-LOX) with Ki of 197 nM.

A potent, selective, noncompetitive, orally active CCR2 antagonist with IC50 of 172 nM.

A potent, selective, noncompetitive human α4β2 nAChRs negative allosteric modulator with IC50 of 13.5 uM, displays no inhibitory activity on Hα3β4 nAChRs at 100 uM..

A potent, selective, non-ATP-competitive inhibitor of p38α-mediated MK2a phosphorylation with apparent Ki of 330 nM.

A potent, selective, low glutamate fold shift (2.4) mGluR5 positive allosteric modulator with EC50 of 2.6 nM, without inherent mGluR5 agonist activity (EC50>30 uM).

A potent, selective, irreversible sigma-2 receptor partial agonist with Ki of 14.6 nM, >700-fold selectivity over sigma-1 receptors.

A potent, selective, irreversible EGFR mutants with IC50 of 12, 3, 4 and 5 nM for EGFR L858R-T790M, Del-T790M, L858R, and EGFR Del, respectively.

A potent, selective, highly CNS-penetrant mGluR5 antagonist.

A potent, selective, highly CNS-penetrant and orally available mGluR5 negative allosteric modulator Kd of 2.8 nM.

A potent, selective, full agonist of human and murine MC1R with EC50 of 16.8 and 11.6 nM, respectively.

A potent, selective, dual CysLT1 and CysLT2 antagonist with IC50 of 17 and 0.87 nM, respectively..

A potent, selective, covalent KRAS G12C inhibitor that selectively inhibit KRAS G12C-dependent signaling and cancer cell growth at sub-micromolar concentrations..

A potent, selective, competitive, orally active dipeptidyl peptidase-4 (DPP-4) inhibitor with IC50 of 13 nM.

A potent, selective, competitive, orally active dipeptidyl peptidase-4 (DPP-4) inhibitor with IC50 of 13 nM.

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.