(A) U2OS cells expressing nucleoBAS, the bile acid uptake transporter NA+-taurocholate co-transporting polypeptide, and OSTα-OSTβ (left) were used to analyze the inhibitory effect of 1280 compounds on OSTα-OSTβ–mediated transport. U2OS cells expressing nucleoBAS and NA+-taurocholate co-transporting polypeptide but no OSTα-OSTβ served as a positive control (right). (B) FACS plots of U2OS cells transfected with nucleoBAS were treated with dimethyl sulfoxide (DMSO) (left), TCDCA (middle), or GW4064 (right). (C) Percentage of cells in gate P4, plotted in a bar graph. (D) FACS plots of U2OS nucleoBAS cells co-transfected with a bile acid uptake transporter (NA+-taurocholate co-transporting polypeptide) and OSTα-OSTβ also were treated with DMSO (left), TCDCA (middle), or GW4064 (right). (E) Percentage of cells in gate P4, plotted in a bar graph. Data are represented as means ± SD. ***P < .001 (1-way analysis of variance; post hoc: Dunnett multiple comparison).