Assay Detail
Functional
CHEMBL658536
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Inhibition of transcriptional repression in CV-1 cells expressing glucocorticoid receptor
29
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CV-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 7.35 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | 8.68 |
| CHEMBL298687 | — | — | 1 | 8.24 |
| CHEMBL266282 | AL-43 | — | 2 | 8.16 |
| CHEMBL48588 | — | — | 1 | 8.15 |
| CHEMBL47463 | — | — | 1 | 7.92 |
| CHEMBL46325 | — | — | 1 | 7.72 |
| CHEMBL50118 | — | — | 1 | 7.70 |
| CHEMBL46199 | — | — | 1 | 7.68 |
| CHEMBL45720 | — | — | 1 | 7.64 |
| CHEMBL49386 | — | — | 1 | 7.64 |
| CHEMBL47742 | — | — | 1 | 7.42 |
| CHEMBL46029 | — | — | 1 | 7.40 |
| CHEMBL48283 | — | — | 1 | 7.38 |
| CHEMBL46329 | — | — | 1 | 7.06 |
| CHEMBL416278 | — | — | 1 | 7.06 |
| CHEMBL296624 | — | — | 1 | 6.96 |
| CHEMBL264560 | — | — | 1 | 6.96 |
| CHEMBL416465 | — | — | 1 | 6.85 |
| CHEMBL296623 | — | — | 1 | 6.85 |
| CHEMBL416831 | — | — | 1 | 6.82 |
| CHEMBL49632 | — | — | 1 | 6.66 |
| CHEMBL49694 | — | — | 1 | 6.66 |
| CHEMBL48308 | — | — | 1 | 6.64 |
| CHEMBL295475 | — | — | 1 | 6.50 |
| CHEMBL49873 | — | — | 1 | 6.36 |
| CHEMBL297850 | — | — | 1 | - |
| CHEMBL47272 | — | — | 1 | - |
| CHEMBL45795 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL131 | PREDNISOLONE | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL298687 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL266282 | AL-43 | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL48588 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL47463 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL266282 | AL-43 | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL46325 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL50118 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL46199 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL49386 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL45720 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL47742 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL46029 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL48283 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL46329 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL416278 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL264560 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL296624 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL416465 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL296623 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL416831 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL49632 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL49694 | — | IC50 | = | 216.7 | nM | 6.66 |
| CHEMBL48308 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL295475 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL49873 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL297850 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL47272 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL45795 | — | IC50 | > | 5000.0 | nM | - |