A potent, selective, orally active S1P1 antagonist with IC50 of 2.5 nM Ca2+ mobilization assays, without activity on S1P2, S1P3 and S1P4 (IC50>10 uM).

A potent, selective, orally active somatostatin receptor SSTR3 antagonist with binding Ki of 0.66 nM, >500-fold selectivity over SSTR1/2/4/5.

A potent, selective, orally active somatostatin receptor SSTR3 antagonist with binding Ki of 2.3 nM, >2,500-fold selectivity over SSTR1/2/4/5 (IC50>5 uM).

A potent, selective, orally active TAAR1 partial agonist with Ki of 6 nM, EC50 of 23 nM (hTAAR1), 140-fold selectivity over β2 adrenergic receptors.

A potent, selective, orally active TRPM8 channel antaognist with IC50 of 0.8 nM, .

A potent, selective, orally active γ-secretase modulator with Aβ42 IC50 of 39 nM.

A potent, selective, orally active, small-molecule antagonist of human glucagon receptor with Ki of 6.66 nM.

A potent, selective, orally available CX3C chemokine receptor 1 (CX3CR1) modulator that inhibits the fractalkine-induced chemotaxis of human peripheral blood NK cells with IC50 of 4.9 nM.

A potent, selective, orally available GlyT1 inhibitor with IC50 of 1.6 nM, weakly inhibits rat GlyT2 (IC50=138 nM).

A potent, selective, orally available GlyT1 inhibitor with IC50 of 29 nM, demonstrates excellent in vivo occupancy of GlyT1 transporters in vivo..

PF-0346275 is a potent, selective, orally available GlyT1 inhibitor with Ki of 11.6 nM, without activity against GlyT2 (IC50>10 uM).

A potent, selective, orally available GPR40 agonist with EC50 of 3.7 nM.

A potent, selective, orally available GPR40 agonist with EC50 of 8 nM.

A potent, selective, orally available GPR40 agonist with EC50 of 9 nM.

A potent, selective, orally available GPR40 agonist with Ki of 15 nM, β-arrestin EC50 of 108 nM.

A potent, selective, orally available IAP antagonist with IC50 of 1.3, 2.2 and 200 nM for cIAP-1, cIAP-2 and XIAP, respectively.

A potent, selective, orally available inhibitor of both native and mutant Bcr-Abl with IC50 of 20-80 nM.

A potent, selective, orally available inhibitor of HCV NS3/4A protease with Ki of 0.05 and 0.9 nM for GT1b and 2a protease, respectively.

A potent, selective, orally available RIPK2 inhibitor with IC50 of 3 nM.

Avacopan is a potent, selective, orally availale C5aR (CD88) inhibitor with IC50 of 0.1 nM.

A potent, selective, orally bioavailable BET bromodomain inhibitor with IC50 of 7.2 and 28.2 nM for BRD4 BD2 and BRD4 BD1, respectively.

A potent, selective, orally bioavailable GPR120 agonist with EC50 of 42 nM in calcium flux assays.