Glafenine hydrochloride is a non-narcotic analgesic and non-steroidal anti-inflammatory drug and an ABCG2 inhibitor with an IC50 of 3.2 μM.

KS176 is a potent and selective inhibitor for the breast cancer resistance protein (BCRP) multidrug transporter with IC50s of 0.59 and 1.39 μM in Pheo A and Hoechst 33342 assays respectively.

ML230 是一种选择性抑制 ABCG2 的化合物，抑制效力为 ABCB1 的 36 倍，EC50 值为 0.13 μM 和 4.65 μM。

YHO-13177 is a selective and potent inhibitor of BCRP, it potentiates the cytotoxicity of SN-38 in cancer cells and has no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells.

Ko 143是一种高效且选择性的 ATP 结合盒亚家族 G 成员 2 (ABCG2/BCRP) 抑制剂，显示出对 P-gp 和 MRP-1 转运蛋白超过 200 倍的选择性。

PCI 29732 是一种高效、口服可利用且可逆的 BTK 抑制剂，显示出对 BTK 的 Kiapp 值为 8.2 nM，对 Lck 为 4.6 nM，对 Lyn 为 2.5 nM。

5,7,3'-Trihydroxy-4'-methoxy-8-prenylflavanone is a natural product isolated and purified from the barks of Azadirachta indica.

YHO-13351 is the water-soluble prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.