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 (binding) | = 74.9 nM | Transrepression activity at glucocorticoid receptor alpha in IL-1beta-stimulated human A549 cells assessed as inhibition of NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay | ChEMBL. | 21899328 |
EC50 (binding) | = 77.9 nM | Transrepression activity at glucocorticoid receptor alpha in phorbol myristate acetate-stimulated human A549 cells assessed as inhibition of AP1 response element by luciferase reporter gene assay | ChEMBL. | 21899328 |
EC50 (binding) | = 610 nM | Transactivation activity at GR-alpha in human NP1 Hela cells assessed as inhibition of GAL4-DBD after 20 hrs by luciferase reporter gene assay | ChEMBL. | 21899328 |
EC50 (binding) | > 5000 nM | Transactivation activity at glucocorticoid receptor alpha human 13D3/Huh7 cells assessed as induction of TAT activity after 4 hrs by spectrophotometry | ChEMBL. | 21899328 |
EC50 (binding) | > 10000 nM | Transactivation activity at GR-alpha in human NP1 Hela cells assessed as induction of GAL4-DBD after 20 hrs by luciferase reporter gene assay | ChEMBL. | 21899328 |
Emax (binding) | = 11 % | Transactivation activity at GR-alpha in human NP1 Hela cells assessed as induction of GAL4-DBD after 20 hrs by luciferase reporter gene assay relative to Dexamethasone | ChEMBL. | 21899328 |
Emax (binding) | = 24 % | Transactivation activity at glucocorticoid receptor alpha human 13D3/Huh7 cells assessed as induction of TAT activity after 4 hrs by spectrophotometry relative to Dexamethasone | ChEMBL. | 21899328 |
Emax (binding) | = 49 % | Transrepression activity at glucocorticoid receptor alpha in IL-1beta-stimulated human A549 cells assessed as inhibition of NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay relative to Dexamethasone | ChEMBL. | 21899328 |
Emax (binding) | = 65 % | Transrepression activity at glucocorticoid receptor alpha in phorbol myristate acetate-stimulated human A549 cells assessed as inhibition of AP1 response element by luciferase reporter gene assay relative to Dexamethasone | ChEMBL. | 21899328 |
Imax (binding) | = 89 % | Transactivation activity at GR-alpha in human NP1 Hela cells assessed as inhibition of GAL4-DBD after 20 hrs by luciferase reporter gene assay in presence of 100 nM Dexamethasone | ChEMBL. | 21899328 |
Ki (binding) | = 8.6 nM | Displacement of GS-red from glucocorticoid receptor by fluorescence polarization assay | ChEMBL. | 21899328 |
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.