Triclabendazole sulfoxide (TCBZ-SO), a primary plasma metabolite of Triclabendazole, inhibits the membrane transporter ABCG2/BCRP and demonstrates anti-parasite effects.

Zamicastat (BIA 5-1058) is an inhibitor of dopamine β-hydroxylase (DBH) and a concentration-dependent dual inhibitor of P-gp and BCRP, with IC50 values of 73.8 μM and 17.0 μM, respectively.

YHO-13177 is a potent and specific inhibitor of BCRP, which enhances the cytotoxicity of SN-38 in cancer cells without affecting P-glycoprotein–mediated paclitaxel resistance in [MDR1]-transduced human leukemia [K562] cells.

PCI 29732 is a selective and irreversible Btk inhibitor with IC50 of 8.2 nM in a FRET based biochemical enzymology assay.

Ko 143 is a selective inhibitor of ATP-binding cassette sub-family G member 2 (ABCG2; BCRP).

Brevianamide F (Cyclo(L-Pro-L-Trp)), also known as cyclo-(L-Trp-L-Pro), is a naturally occurring 2,5-diketopiperazine with notable breast cancer resistance protein inhibitory activity.

CP-100356 hydrochloride is an orally active, low micromolar dual inhibitor of MDR1 (P-gp) and BCRP, a nucleotide-derived substrate analogue that inhibits MDR1-mediated Calcein-AM and BCRP-mediated Prazosin transporters. Additionally, CP-100356 inhibits OATP1B1 and induces stomatal opening in the dark.

ABCG2-IN-1 (compound K2), an analog of Ko143, is an orally active inhibitor of ABCG2 with an IC50 of 0.13 μM, demonstrating favorable oral pharmacokinetics in mice and showing promise for further research [1].