Table 2. IC50 Values of Active Compounds That Had an Inhibition Level of At Least 20% [+ Standard Error of the Mean (SEM)] against ABCB1, ABCC1, and/or ABCG2 in the Initial Screening (Figure 5A–C)#.
ABCB1-overexpressing A2780/ADR, ABCC1-overexpressing H69AR, or ABCG2-overexpressing MDCK II BCRP cells in either calcein AM (ABCB1 and ABCC1) or pheophorbide A (ABCG2) assays were used.14−16,56 The positive control (100%) was defined by the effect value of 10 μM cyclosporine A (ABCB1 and ABCC1) or compound 34 (ABCG2), while buffer medium served as a negative control (0%). Shown is the mean ± SEM of at least three independent experiments. Rose mark: discovered triple ABCB1, ABCC1, and ABCG2 inhibitors.
