NR1I2 and colorectal cancer: Comprehensive characterization using different biochemical assays, assessing direct ligand binding, and cellular assays, addressing the interaction of PXR with coregulatory proteins, as well as gene expression analyses in colorectal cancer cells and differentiated hepatocytes, identified the novel inhibitors as passive mixed competitive/noncompetitive antagonists of PXR, which elicit gene- and tissue-specific modulation of PXR target gene expression.