| Assay Method Information | |
| | Competition Ligand Binding Assay and Transient Transfection Assay |
| Description: | Polylysine YiO imaging beads (Amersham, GE Healthcare) were coated with histidine-tagged WT PXR LBD. Nonspecific binding sites were blocked with BSA. [N-Methyl-3H]-GW0438X was added to the blocked receptor-bead. The receptor-bead-radioligand mix was added directly to test compounds in 384-well plates. Displacement of [N-methyl-3H]-GW0438 was measured in a microplate imager. Nonspecific binding was determined in the presence of 10 uM GW0438. Data analysis was achieved using a three-parameter fit. The data were calculated as pIC50s. The pEC50 values were obtained from measurement of Luciferase reporter activity in CV-1 cells transfected with full-length hPXR. |
| Affinity data for this assay | |
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