Pregnane X receptor (PXR) is a nuclear receptor considered to be a master xenobiotic receptor that coordinately regulates the expression of genes encoding drug-metabolizing enzymes and drug transporters to essentially detoxify and eliminate xenobiotics and endotoxins from the body. The function of PXR in the regulation of xenobiotic metabolism has been extensively studied, and the role of PXR as a xenobiotic sensor has been well established. In addition, recent studies have discovered the roles of PXR in inflammatory response, cell proliferation, and cell migration. These recent discoveries of the role of PXR in the physiologic and pathophysiologic conditions of other cellular processes provide the possibility of novel targets for drug discovery. Signosis has launched PXR GAL4 reporter HEK293 stable cell line for studying xenobiotic paythway and drug toxicity.