AF64394 is a novel and selective GPR3 inverse agonist, and the first small molecule inhibitor of GPR3 receptor function.

ML-191( also known as CCG-152883), is a GPR55 antagonist .

JMS-17-2 is a novel, potent and selective antagonist of CX3CR1 with anticancer activity.

AR231453 (AR-231453) is a potent, selective and orally bioavailable GPR119 agonist used as an antidiabetic agent.

CID-16020046 (CI-16020046) is a novel, potent and selective GPR55 (LPI receptor) antagonist / inverse agonist which can block GPR55-mediated endothelial wound healing and reverse LPI-inhibited platelet aggregation.

NIBR-189 is a novel and potent EBI2 (GPR183) receptor antagonist.

CID-2440433 (ML-184; ML184) is a novel and potent agonist of GPR55 with EC50 of 263 nM.

APD668 (also known as JNJ-28630368) is a novel and potent agonist of the pancreatic and GI-expressed orphan G-protein coupled receptor GPR119, with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119 respectively.

APD597 (formerly known as JNJ-38431055) is a novel potent and selective GPR119 agonist/modulator, which has the potential for the treatment of type 2 diabetes.

GTPL5846 is a novel and potent stimulates production of pro-inflammatory cytokines.