Assay Detail
Functional
CHEMBL834039
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Repression of AP1-luciferase reporter activity in TPA-stimulated U2OS cells expressing rat glucocorticoid receptor
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | U2OS |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design and evaluation of novel nonsteroidal dissociating glucocorticoid receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 8.34 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL433586 | — | — | 1 | 9.70 |
| CHEMBL184109 | — | — | 1 | 8.77 |
| CHEMBL363760 | — | — | 1 | 8.74 |
| CHEMBL181601 | — | — | 1 | 8.52 |
| CHEMBL362556 | — | — | 1 | 8.52 |
| CHEMBL186954 | — | — | 1 | 8.52 |
| CHEMBL186948 | — | — | 1 | 8.52 |
| CHEMBL184578 | — | — | 1 | 8.52 |
| CHEMBL183475 | — | — | 1 | 8.22 |
| CHEMBL186805 | — | — | 1 | 8.15 |
| CHEMBL186683 | — | — | 1 | 8.10 |
| CHEMBL186930 | — | — | 1 | 7.80 |
| CHEMBL362392 | — | — | 1 | 7.77 |
| CHEMBL366093 | — | — | 1 | 7.72 |
| CHEMBL360248 | — | — | 1 | 7.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL433586 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL184109 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL363760 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL181601 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL362556 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL186954 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL186948 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL184578 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL183475 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL186805 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL186683 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL186930 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL362392 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL366093 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL360248 | — | EC50 | = | 31.0 | nM | 7.51 |