| Assay Method Information | |
| | AR Transcriptional Activation Assay and MDA Whole-Cell Binding Assay |
| Description: | The compounds were evaluated in a transcriptional activation assay with hAR in a mammalian cell background (CV-1) as the primary in vitro assay. Receptor binding assays for hAR were performed in a whole cell format using MDA-MB-453 cells. After correcting for nonspecific binding, IC50 values were determined. The IC50 value is defined as the concentration of competing ligand required to decrease specific binding by 50%. The IC50 value was determined with the aid of the log-logit (Hill) method, which linearized the concentration response curve. Linear regression was then used to determine the IC50 value. The Ki values were determined by the application of the Cheng-Prusoff equation: Ki=IC50/(1+[L]/Kd) where [L] is the concentration of labeled ligand and Kd is the dissociation constant of the labeled ligand determined in the saturation analysis. |
| Affinity data for this assay | |
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