A 2-amino quinoline, 5-(3-(2-(7-chloroquinolin-2-yl)ethenyl)phenyl)-8-dimethylcarbamyl-4,6-dithiaoctanoic acid, interacts with PfMDR1 and inhibits its drug transport in Plasmodium falciparum.

•2-Amino quinoline (ML571) is a substrate for PfMDR1 but not wild-type or mutant PfCRT.•MK571 is specific inhibitor of PfMDR1-mediated drug transport.•MK571 inhibits the accumulation of PfMDR1 antimalarials in the digestive vacuole of the parasite.•MK571 inhibits β-hematin formation, in vitro.•Chloroquine-resistant Plasmodium falciparum strains are more susceptible to MK571 than – sensitive strains.