Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | nuclear receptor subfamily 3, group C, member 1 (glucocorticoid receptor) | Starlite/ChEMBL | References |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (functional) | = 207 nM | Agonist activity at GR by GRE activation assay | ChEMBL. | 17553679 |
EC50 (functional) | > 1000 nM | Antagonist activity at GR assessed as inhibition of dexamethasone-induced GRE activation | ChEMBL. | 17553679 |
Efficacy (functional) | < 10 % | Antagonist activity at GR assessed as inhibition of dexamethasone-induced GRE activation | ChEMBL. | 17553679 |
Efficacy (functional) | = 54 % | Agonist activity at GR by GRE activation assay relative to dexamethasone | ChEMBL. | 17553679 |
Efficacy (functional) | = 94 % | Activity at GR assessed as repression of TNFalpha and IL 1beta induced E-selectin response | ChEMBL. | 17553679 |
IC50 (functional) | = 17 nM | Activity at GR assessed as repression of TNFalpha and IL 1beta induced E-selectin response | ChEMBL. | 17553679 |
Ki (binding) | = 1.9 nM | Displacement of radiolabeled dexamethasone from glucocorticoid receptor | ChEMBL. | 17553679 |
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.
1 literature reference was collected for this gene.