AR 231453 is a potent and selective small molecule agonist of GPR119 that enhances glucose-dependent insulin secretion and glucagon-like peptide 1 (GLP-1) release, used as an antidiabetic agent.

CID-16020046 is a selective GPR55 (LPI receptor) antagonist with IC50 of 0.15 μM.

TUG-770 is a highly potent free fatty acid receptor 1 (FFA1/GPR40) agonist with EC50 of 6 nM for hFFA1.

GSK137647A is an agonist of FFA4 with pEC50 of 6.3.

BAR501 is an agonist of GPBAR1 with EC50 of 1 μM. It can effectively reduce hepatic perfusion pressure.

MK 1903 is a potent and selective hydroxycarboxylic acid receptor 2 (HCA2, GPR109A) full agonist.

F64394 is an inverse agonist of GPR3 with pIC50 of 7.3.

TAK-875 is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 0.072 μM.

CYM-5541 is an allosteric agonist of S1P3 with EC50 of 72 nM - 132 nM.

ML401 is a selective inhibitor of GPR183.

NE 52-QQ57 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM. NE 52-QQ57 has anti-inflammatory activity.

TUG-891 is a selective agonist of long chain free fatty acid (LCFA) receptor 4 (GPR120).

INT-777 is a potent and selective TGR5 agonist with remarkable in vivo activity (EC50=0.82 μM).

ML 193 is a selective GPR55 antagonist with IC50 of 221 nM.

Etrasimod is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.

G-1 is a nonsteroidal, high-affinity, selective agonist of GPR30 that binds with a Ki value of 11 nM.

GPR120-IN-1 is a selective Gpr120 agonist with a logEC50 of −7.62.

IBC 293 is a selective agonist of GPR109B (HM74).

MS 21570 is an antagonist of GPR171 with IC50 of 220 nM.