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Substrate activity of tariquidar for three ABC transporters as measured by the accumulation of [3H]tariquidar in human cells consisting of parental (white bar) and resistant ABC transporter-expressing (black bar) lines. (A) Tariquidar is a substrate for BCRP and (B) binds to P-gp, but (C) has no activity at MRP1. The accumulation of [3H]tariquidar in cells was assayed 240 min after the addition of [3H]tariquidar (1 nM). Bars represent mean ± SD of six observations.
