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

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

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

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, allosteric CCR2 antagonist with IC50 of 103 nM..

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

A potent, selective S1P3 antagonist with Ki of 0.25 nM.

A potent, selective S1P3 antagonist with Ki of 0.25 nM.

A potent, selective inhibitor of CXCL12 binding to CXCR4 and CXCR7 with IC50 of 200 nM.

A potent, selective dopamine D4 receptor agonist with Ki of 12.1 and 7.9 nM for rat and human D4 receptors, respectively.

A potent, selective dopamine D1 receptor antagonist with Ki of 0.56 nM.

A potent, selective cholecystokinin receptor CCK2 antagonist for treatment of gastroesophageal reflux disease (GERD)..

A potent, selective and orally available CGRP receptor antagonist for the prevention of migraine. Migraine.

A potent, selective and competitive CXCR2 inhibitor that selectively inhibits CXCR2-mediated recruitment of β-arrestin-2 with pKi of 8.92.

A potent, orally bioavailable, full agonist of GPR40/FFA1 with EC50 of 0.16 uM.

A potent, orally active, dual NK1 receptor antagonist (IC50=0.5 nM) and SERT inhibitor (IC50=5.2 nM).

A potent, mixed sigma2 agonist and sigma1 antagonist with Ki of 0.28 and 13.0 nM, respectively.

A potent, highly selective, CNS penetrant mGlu7 negative allosteric modulator with IC50 of 0.76 uM.

A potent, highly selective 5-HT1A receptor partial agonist with Ki of 0.1 nM, displays 460- and 260-fold selectivity for 5-HT1A over the α1-adrenergic and D2 receptors, respectively..

A potent, equipotent CXCR1 and CXCR2 antagonist with IC50 of 31 nM and 21 nM, respectively.

A potent CXCR7 (ACKR3) agonist..

A potent and orally bioavailable dual antagonist of CCR2 and CCR5 with binding IC50 of 0.7 nM and 2.4 nM, respectively.

A potent and highly selective D4 dopamine receptor antagonist with Ki of 3.5 nM, >200-fold selectivity over D2 and D3 receptors.

A novel potent, slow tight binding LPA1 receptor antagonist with IC50 of 86 nM, Kd of 0.34 nM.

A novel potent, selective CXCR2 inhibitor with IC50 of 7.6 nM.

A novel potent, selective CXCR2 inhibitor with IC50 of 0.4 nM.

A novel potent and selective agonist of GPR84 that induces calcium response with EC50 of 0.213 uM.

A novel 5-HT receptor antagonist for the treatment of Parkinson's disease..

A moderately potent, but highly selective α2-adrenoceptor antagonist, the only reported selective antagonist at the α2B-adrenoceptor not having potent α1-adrenoceptor antagonist activity.