Assay Detail
Binding
CHEMBL1022034
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at GR ligand binding domain expressed in human NP1 cells assessed as glucocorticoid response element transactivation by GAL4 luciferase reporter gene assay
17
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | NP1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Discovery of novel dihydro-9,10-ethano-anthracene carboxamides as glucocorticoid receptor modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 17 | 7.07 | 8.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 1 | 8.38 |
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | 7.08 |
| CHEMBL514630 | — | — | 3 | 6.96 |
| CHEMBL474189 | — | — | 3 | 6.93 |
| CHEMBL474188 | — | — | 1 | 6.76 |
| CHEMBL514636 | — | — | 1 | 6.49 |
| CHEMBL475159 | — | — | 1 | - |
| CHEMBL516386 | — | — | 1 | - |
| CHEMBL514481 | — | — | 1 | - |
| CHEMBL515127 | — | — | 1 | - |
| CHEMBL474966 | — | — | 1 | - |
| CHEMBL473801 | — | — | 1 | - |
| CHEMBL473802 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL384467 | DEXAMETHASONE | EC50 | = | 4.2 | nM | 8.38 |
| CHEMBL131 | PREDNISOLONE | EC50 | = | 82.7 | nM | 7.08 |
| CHEMBL514630 | — | EC50 | = | 110.9 | nM | 6.96 |
| CHEMBL474189 | — | EC50 | = | 117.0 | nM | 6.93 |
| CHEMBL474189 | — | EC50 | = | 121.0 | nM | 6.92 |
| CHEMBL474188 | — | EC50 | = | 174.9 | nM | 6.76 |
| CHEMBL514636 | — | EC50 | = | 321.9 | nM | 6.49 |
| CHEMBL514630 | — | EC50 | > | 2500.0 | nM | - |
| CHEMBL475159 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL474189 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL516386 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL473802 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL473801 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL514630 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL514481 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL515127 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL474966 | — | EC50 | > | 10000.0 | nM | - |