Assay Detail
Binding
CHEMBL894570
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at human glucocorticoid receptor in human HepG2 cells assessed as tyrosine amino transferase activity
21
Total Activities
21
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| 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 | 6.34 | 7.62 |
| Activity | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | 7.62 |
| CHEMBL372684 | — | — | 1 | 6.45 |
| CHEMBL233588 | — | — | 1 | 6.17 |
| CHEMBL236201 | — | — | 1 | 6.15 |
| CHEMBL392376 | — | — | 1 | 5.88 |
| CHEMBL236202 | — | — | 1 | 5.79 |
| CHEMBL439386 | — | — | 1 | - |
| CHEMBL233789 | — | — | 1 | - |
| CHEMBL363179 | — | — | 1 | - |
| CHEMBL232606 | — | — | 1 | - |
| CHEMBL195972 | — | — | 1 | - |
| CHEMBL411825 | — | — | 1 | - |
| CHEMBL393194 | — | — | 1 | - |
| CHEMBL233390 | — | — | 1 | - |
| CHEMBL233389 | — | — | 1 | - |
| CHEMBL233217 | — | — | 1 | - |
| CHEMBL311034 | — | — | 1 | - |
| CHEMBL79807 | — | — | 1 | - |
| CHEMBL393309 | — | — | 1 | - |
| CHEMBL233589 | — | — | 1 | - |
| CHEMBL429628 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL131 | PREDNISOLONE | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL372684 | — | EC50 | = | 356.0 | nM | 6.45 |
| CHEMBL233588 | — | EC50 | = | 675.0 | nM | 6.17 |
| CHEMBL236201 | — | EC50 | = | 703.0 | nM | 6.15 |
| CHEMBL392376 | — | EC50 | = | 1315.0 | nM | 5.88 |
| CHEMBL236202 | — | EC50 | = | 1624.0 | nM | 5.79 |
| CHEMBL439386 | — | EC50 | - | — | - | |
| CHEMBL233789 | — | EC50 | - | — | - | |
| CHEMBL363179 | — | EC50 | - | — | - | |
| CHEMBL232606 | — | Activity | - | — | - | |
| CHEMBL195972 | — | EC50 | - | — | - | |
| CHEMBL411825 | — | EC50 | - | — | - | |
| CHEMBL393194 | — | EC50 | - | — | - | |
| CHEMBL233390 | — | EC50 | - | — | - | |
| CHEMBL233389 | — | EC50 | - | — | - | |
| CHEMBL233217 | — | EC50 | - | — | - | |
| CHEMBL311034 | — | EC50 | - | — | - | |
| CHEMBL79807 | — | EC50 | - | — | - | |
| CHEMBL393309 | — | Activity | - | — | - | |
| CHEMBL233589 | — | Activity | - | — | - | |
| CHEMBL429628 | — | Activity | - | — | - |