Screening of the inhibitory effects of 22 anti-TB drugs on uptake ability. (A) [3H]ES (45 nM) in stably transfected HEK-OATP1B1 cells. (B) [3H]ES (45 nM) in stably transfected HEK-OATP2B1 cells. (C) [3H]E2G (60 nM) in transiently transfected HEK-OATP1B3 cells. In the absence of any inhibitors, OATP1B1-, OATP2B1-, and OATP1B3-mediated uptake, as a control, was compared with TB drug-mediated uptake inhibition. Rifampin for OATP1B1 and bromosulfophthalein (BSP) for OATP2B1 and OATP1B3 were used as positive controls for uptake inhibition. Data are presented as the mean ± SD value from three or more independent experiments. *, P < 0.05, **, P < 0.01, and ***, P < 0.001, significantly different compared with the percentage of uptake in the control (no inhibitor).