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 |
---|---|---|---|---|
Cp (ADMET) | = 4.5 nmol/ml | Plasma concentration in Sprague-Dawley rat after 7 hrs at 100 mg/kg, po | ChEMBL. | 16987661 |
Drug uptake (ADMET) | = 26.5 % | Liver concentration in Sprague-Dawley rat after 7 hrs at 100 mg/kg, po | ChEMBL. | 16987661 |
IC50 (binding) | = 1.2 nM | Binding affinity to human GR | ChEMBL. | 16987661 |
IC50 (binding) | = 1.2 nM | Binding affinity to human GR | ChEMBL. | 16987661 |
IC50 (binding) | = 10 nM | Activity at GR expressed in CHO cells assessed as decrease in dexamethasone-stimulated alkaline phosphatase production by GRAF assay | ChEMBL. | 16987661 |
IC50 (binding) | = 10 nM | Activity at GR expressed in CHO cells assessed as decrease in dexamethasone-stimulated alkaline phosphatase production by GRAF assay | ChEMBL. | 16987661 |
Inhibition (functional) | = 9 % | Inhibition of prednisilone-induced lymphopenia in Sprague-Dawley rat at 100 mg/kg, po | ChEMBL. | 16987661 |
Inhibition (functional) | = 72 % | Inhibition of prednisilone-stimulated TAT production in Sprague-Dawley rat at 100 mg/kg, po | ChEMBL. | 16987661 |
Inhibition (functional) | = 86 % | Inhibition of prednisilone-induced glycogen deposition in Sprague-Dawley rat at 100 mg/kg, po | ChEMBL. | 16987661 |
PPB (ADMET) | = 95.9 % | Protein binding in rat plasma | ChEMBL. | 16987661 |
Stabilty (ADMET) | = 98 % | Stability in rat liver microsomes after 20 mins | ChEMBL. | 16987661 |
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.