| Assay Method Information | |
| | Competition-Based Ligand Binding Assay and Transactivation Assay. |
| Description: | Ligand binding was determined using a scintillation proximity assay with streptavidin-coated SPA beads (Amersham) and biotinylated receptor. Receptor-bound [3H]estrone was determined by scintillation counting (Perkin-Elmer). The binding IC50 value (the concentration of compound required for 50% inhibition of [3H]estrone binding to ER was calculated using XL-fit one-site dose response. To determine the agonist activity of the compounds on receptors, the full length receptors were stably expressed under ERE promoter with luciferase as reporter in Hela cells. The transactivation EC50 (the concentration of compound required to achieve 50% of transactivation caused by 10 nM estradiol) was calculated using XL-fit one-site dose response. |
| Affinity data for this assay | |
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