| Assay Method Information | |
| | Competitive Ligand Binding Assay, GR-Mediated Antagonist Activity Assay, and IL-6 Repression Assay |
| Description: | Competitive Ligand Binding Assay- 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. GR-Mediated Antagonist Activity Assay- GR-mediated antagonist activity is measured in the presence of a concentration of dexamethasone empirically determined to give half-maximal response. The antagonist activity of compounds, their activity in inhibiting dexamethasone response to basal level, is reported as % absolute efficacy. Potencies of compounds are reported as the concentration at which they reach half their antagonist (IC50) activity. IL-6 Repression Assay- The GR-mediated repression of IL-6 production in a human fibroblast (NHDFneo) cell line is measured with a modified ELISA assay. |
| Affinity data for this assay | |
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