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| | Scintillation Proximity Assay (Ki) and Cell-Based Transcription Assay (EC50) |
| Description: | The human PPARalpha ligand binding was directly measured using a scintillation proximity assay. Plates were read on a Packard TopCount. IC50 values for test compounds were determined from nonlinear regression analysis of data collected from ligand displacement binding experiments. The inhibition constant (Ki) was calculated from IC50 value by the Cheng and Prusoff equation. EC50 is the concentration of test compounds needed to induce 50% of the maximum luciferase activity in CV-1 cells transfected with hPPARalpha ligand binding domain and a GAL4 reporter construct. Four hours post-transfection, test compounds were added, and luciferase activity was measured 20 h later. |
| Affinity data for this assay | |
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