ACT-246475 (ACT246475) is a potent, selective, reversible P2Y12 receptor antagonist with binding IC50 of 1.0 nM.

Acrivastine (BW825C) is a short acting histamine 1 receptor antagonist for the treatment of allergic rhinitis.

AC264613 is a potent and selective protease-activated receptor 2 (PAR2) agonist (pEC50 = 7.5). Displays no activity at other PAR subtypes and exhibits no significant activity at over 30 other receptors implicated in nociception and inflammation.

AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6.

A synthetic immunosuppressant that functions as a S1P1 receptor agonist.

A small-molecule partial agonist of CXCR7 (ACKR3)..

A small-molecule partial agonist of CXCR7 (ACKR3)..

A small-molecule partial agonist of CXCR7 (ACKR3)..

A small molecule CMKLR1 antagonist that inhibits chemerin-stimulated β-arrestin2 association with CMKLR1 (EC50=9.7 nM).

A potential antipsychotic agent that binds selectively to D4 and 5-HT2A receptors with Ki of 3.0 and 5.8 nM, respectively.

A potent, specific, noncompetitive dual CXCR1 and CXCR2 antagonist with IC50 of 38 nM (vs. CXCL1) and 36 nM (vs. CXCL8), respectively.

A potent, specfic CXCR2 antagonist that inhibits IL8 down-regulation of forskolin-induced cAMP with IC50 of 7.79 uM.

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

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

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

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

A potent, selective, orally active agonist of dopamine D3 receptor with EC50 of 21 nM.

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)..