Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | nuclear receptor subfamily 3, group C, member 2 | Starlite/ChEMBL | No references |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 33 nM | BindingDB_Patents: Competitive Molecular Binding Assay. The MR competitive binding assay is based on the binding and displacement of a TAMRA-labeled Dexamethasone probe with fluorescence polarization (FP) detection. The assay is performed in 384-well, low volume NBS black plates (Corning #3676) in assay buffer consisting of 10 mM TES, pH 7.4, 50 mM KCl, 20 mM Sodium molybdate, 1.5 mM EDTA, 0.04% CHAPS, 10% Glycerol and 1 mM DTT. Full Length human mineralocorticoid receptor (hMR) present in a baculovirus infected insect cell lysate is diluted 2 fold in assay buffer and 10 µL of this dilution is added to the assay plate. Blank wells receive 10 µL of the diluted MR lysate containing 3 µM Dexamethasone. 2 µL diluted test compound is transferred to the assay plate for a final starting top concentration of 10 µM in 1% DMSO. The reaction is started by adding 3 µL of 25 nM probe in assay buffer for a final assay concentration of 5 nM. | ChEMBL. | No reference |
Many chemical entities in TDR Targets come from high-throughput screenings with whole cells or tissue samples, and not all assayed compounds have been tested against a single a single target protein, probably because they get ruled out during screening process. Even if these compounds may have not been of interest in the original screening, they may come as interesting leads for other screening assays. Furthermore, we may be able to propose drug-target associations using chemical similarities and network patterns.