Fig. 5.

Structural predictions and biochemical results translate to cellular PXR activity. 293T cells were cotransfected with a PXR-responsive luciferase reporter and either an empty vector (EV) or PXR-expressing plasmid. Cells were treated for 24 h with the indicated compounds and assayed for luciferase activity. Compounds were used in threefold dilution series starting at 30 µM, and concentrations that exhibited signal reduction in the EV wells were excluded from analysis in the PXR-transfected samples. Results are shown as fold change (FC) relative to the averaged dimethyl sulfoxide (DMSO) controls of PXR-transfected cells, and compounds are split based on their previous designations: (A) T0901317 analogs, (B) group 1 rifampicin analogs, and (C) group 2 rifampicin analogs.