Assay Detail
Functional
CHEMBL931541
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at glucocorticoid receptor assessed as inhibition of dexamethasone-induced glucose response element transcriptional transactivation by luciferase assay
19
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.71 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL258193 | — | — | 1 | 8.74 |
| CHEMBL404496 | — | — | 1 | 8.00 |
| CHEMBL404879 | — | — | 1 | 7.92 |
| CHEMBL438885 | — | — | 1 | 7.28 |
| CHEMBL404640 | — | — | 1 | 7.17 |
| CHEMBL134260 | — | — | 1 | 7.14 |
| CHEMBL436848 | — | — | 2 | - |
| CHEMBL258191 | — | — | 2 | - |
| CHEMBL402362 | — | — | 1 | - |
| CHEMBL253745 | — | — | 1 | - |
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | - |
| CHEMBL403274 | — | — | 1 | - |
| CHEMBL257152 | — | — | 1 | - |
| CHEMBL256787 | — | — | 1 | - |
| CHEMBL443847 | — | — | 1 | - |
| CHEMBL427899 | — | — | 1 | - |
| CHEMBL429842 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL258193 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL404496 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL404879 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL438885 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL404640 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL134260 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL436848 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL258191 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL258191 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL436848 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL402362 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL131 | PREDNISOLONE | IC50 | > | 1.0 | nM | - |
| CHEMBL429842 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL403274 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL257152 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL256787 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL443847 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL427899 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL253745 | — | IC50 | > | 1000.0 | nM | - |