Assay Detail
Binding
CHEMBL894568
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at human glucocorticoid receptor in human A549 cells assessed as repression of human IL6
21
Total Activities
21
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A549 |
| 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 | 20 | 8.08 | 9.00 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL233390 | — | — | 1 | 9.00 |
| CHEMBL411825 | — | — | 1 | 8.68 |
| CHEMBL236202 | — | — | 1 | 8.52 |
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | 8.35 |
| CHEMBL392376 | — | — | 1 | 8.30 |
| CHEMBL233789 | — | — | 1 | 8.30 |
| CHEMBL233389 | — | — | 1 | 8.22 |
| CHEMBL372684 | — | — | 1 | 8.22 |
| CHEMBL79807 | — | — | 1 | 8.01 |
| CHEMBL233588 | — | — | 1 | 8.00 |
| CHEMBL311034 | — | — | 1 | 7.78 |
| CHEMBL363179 | — | — | 1 | 7.75 |
| CHEMBL195972 | — | — | 1 | 7.72 |
| CHEMBL393194 | — | — | 1 | 7.68 |
| CHEMBL236201 | — | — | 1 | 7.48 |
| CHEMBL439386 | — | — | 1 | 7.32 |
| CHEMBL393309 | — | — | 1 | - |
| CHEMBL232606 | — | — | 1 | - |
| CHEMBL233589 | — | — | 1 | - |
| CHEMBL429628 | — | — | 1 | - |
| CHEMBL233217 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL233390 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL411825 | — | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL236202 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL131 | PREDNISOLONE | EC50 | = | 4.5 | nM | 8.35 |
| CHEMBL392376 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL233789 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL233389 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL372684 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL79807 | — | EC50 | = | 9.7 | nM | 8.01 |
| CHEMBL233588 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL311034 | — | EC50 | = | 16.5 | nM | 7.78 |
| CHEMBL363179 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL195972 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL393194 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL236201 | — | EC50 | = | 33.0 | nM | 7.48 |
| CHEMBL439386 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL393309 | — | Activity | - | — | - | |
| CHEMBL232606 | — | EC50 | - | — | - | |
| CHEMBL233589 | — | EC50 | - | — | - | |
| CHEMBL429628 | — | EC50 | - | — | - | |
| CHEMBL233217 | — | EC50 | - | — | - |