BMS-309403是一种高效、口服活性和选择性的脂肪细胞脂肪酸结合蛋白（FABP4, aP2）抑制剂，对FABP4、FABP3和FABP5的Ki值分别为<2、250和350 nM。它与蛋白内部的脂肪酸结合口袋相互作用，竞争性抑制内源性脂肪酸的结合。BMS-309403改善载脂蛋白E缺陷小鼠和培养的人内皮细胞的内皮功能。

HM 50316 is a selecive inhibitor of FABP4 with Ki of < 1 nM.

SB-FI-26, an antinociceptive agent which binds to anandamide transporters FABP5 and FABP7, suppresses the proliferation, migration, invasiveness and colony formation of PC3-M cells in vitro.

FABP5-IN-1(Compounds 4j) is a selective and high affinity fatty acid binding protein 5 (FABP5) inhibitor with a Ki value of 1.7 μM, and does not bind to both FABP3 and FABP7. FABP5-IN-1 shows potent antinociceptive effects[1].