AH-7614是一种选择性 FFA4 (GPR120) 拮抗剂，具有高选择性，能够阻断多不饱和脂肪酸亚油酸对 FFA4 的激动作用。对于人 FFA4 的 pIC50 值为 7.1。

DC260126是自由脂肪酸受体1（FFA1/GPR40）的拮抗剂，能够抑制FFA诱导的细胞内Ca2+水平升高。

TAK-875 is a selective GPR40 agonist with EC50 of 14 nM in human GPR40 expressing CHO cell line, 400-fold more potent than oleic acid.

AM-1638 is a potent and orally bioavailable GPR40/FFA1 full agonist with an EC50 of 0.16 μM.

GW1100 is a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells stimulated by GW 9508 or linoleic acid with a pIC50 value equal to 5.99.

PBI-4050 acts as an agonist for GPR40 and as an antagonist or inverse agonist for GPR84.