Assay Detail
Binding
CHEMBL894572
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Activity at human glucocorticoid receptor in C57BI/6 mouse peritoneal exudate cells assessed as repression of mouse IL6
21
Total Activities
21
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Novel glucocorticoids containing a 6,5-bicyclic core fused to a pyrazole ring: synthesis, in vitro profile, molecular modeling studies, and in vivo experiments.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 17 | 7.56 | 8.24 |
| Activity | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | 8.24 |
| CHEMBL311034 | — | — | 1 | 8.19 |
| CHEMBL372684 | — | — | 1 | 7.96 |
| CHEMBL236202 | — | — | 1 | 7.89 |
| CHEMBL233588 | — | — | 1 | 7.85 |
| CHEMBL233789 | — | — | 1 | 7.80 |
| CHEMBL79807 | — | — | 1 | 7.66 |
| CHEMBL233390 | — | — | 1 | 7.64 |
| CHEMBL236201 | — | — | 1 | 7.50 |
| CHEMBL392376 | — | — | 1 | 7.48 |
| CHEMBL195972 | — | — | 1 | 7.38 |
| CHEMBL439386 | — | — | 1 | 7.34 |
| CHEMBL363179 | — | — | 1 | 7.27 |
| CHEMBL393194 | — | — | 1 | 6.84 |
| CHEMBL233389 | — | — | 1 | 6.41 |
| CHEMBL429628 | — | — | 1 | - |
| CHEMBL393309 | — | — | 1 | - |
| CHEMBL233217 | — | — | 1 | - |
| CHEMBL411825 | — | — | 1 | - |
| CHEMBL232606 | — | — | 1 | - |
| CHEMBL233589 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL131 | PREDNISOLONE | EC50 | = | 5.7 | nM | 8.24 |
| CHEMBL311034 | — | EC50 | = | 6.5 | nM | 8.19 |
| CHEMBL372684 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL236202 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL233588 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL233789 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL79807 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL233390 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL236201 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL392376 | — | EC50 | = | 33.0 | nM | 7.48 |
| CHEMBL195972 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL439386 | — | EC50 | = | 46.0 | nM | 7.34 |
| CHEMBL363179 | — | EC50 | = | 54.0 | nM | 7.27 |
| CHEMBL393194 | — | EC50 | = | 145.0 | nM | 6.84 |
| CHEMBL233389 | — | EC50 | = | 392.0 | nM | 6.41 |
| CHEMBL429628 | — | Activity | - | — | - | |
| CHEMBL393309 | — | Activity | - | — | - | |
| CHEMBL233217 | — | EC50 | - | — | - | |
| CHEMBL411825 | — | Activity | - | — | - | |
| CHEMBL232606 | — | EC50 | - | — | - | |
| CHEMBL233589 | — | Activity | - | — | - |