Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | nuclear receptor subfamily 3, group C, member 2 | Starlite/ChEMBL | References |
Homo sapiens | progesterone receptor | Starlite/ChEMBL | References |
Homo sapiens | nuclear receptor subfamily 3, group C, member 1 (glucocorticoid receptor) | Starlite/ChEMBL | References |
Homo sapiens | androgen receptor | Starlite/ChEMBL | References |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (functional) | = 370 nM | Agonist activity at glucocorticoid receptor in human HepG2 cells co-transfected with GRE assessed as transactivation activity by luciferase reporter gene assay | ChEMBL. | 21115247 |
Efficacy (binding) | = 40 % | Transrepression activity at glucocorticoid receptor in IL-1beta-stimulated human HepG2 cells assessed as inhibition of AP1 response element-induced IL-6 production by ELISA relative to Dexamethasone | ChEMBL. | 21115247 |
Efficacy (binding) | = 69 % | Transrepression activity at glucocorticoid receptor in TNFalpha/IL1beta-stimulated human HepG2 cells assessed as inhibition of NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay relative to Dexamethasone | ChEMBL. | 21115247 |
Efficacy (functional) | = 71 % | Agonist activity at glucocorticoid receptor in human HepG2 cells co-transfected with GRE assessed as transactivation activity by luciferase reporter gene assay relative to Dexamethasone | ChEMBL. | 21115247 |
IC50 (binding) | = 24 nM | Transrepression activity at glucocorticoid receptor in TNFalpha/IL1beta-stimulated human HepG2 cells assessed as inhibition of NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay | ChEMBL. | 21115247 |
Ki (binding) | = 10 nM | Displacement of radiolabeled Dexamethasone from glucocorticoid receptor expressed in baculovirus | ChEMBL. | 21115247 |
Ki (binding) | = 400 nM | Binding affinity to androgen receptor | ChEMBL. | 21115247 |
Ki (binding) | = 1100 nM | Binding affinity to progesterone receptor | ChEMBL. | 21115247 |
Ki (binding) | = 1200 nM | Binding affinity to mineralocorticoid receptor | ChEMBL. | 21115247 |
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.