Assay Detail
Functional
CHEMBL838116
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Effective concentration against MMTV in transactivation assay in U2OS cells expressing rat GR
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 | 8.20 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL433586 | — | — | 1 | 9.70 |
| CHEMBL181601 | — | — | 1 | 8.52 |
| CHEMBL184578 | — | — | 1 | 8.52 |
| CHEMBL186954 | — | — | 1 | 8.40 |
| CHEMBL183475 | — | — | 1 | 8.40 |
| CHEMBL366093 | — | — | 1 | 8.40 |
| CHEMBL186683 | — | — | 1 | 8.30 |
| CHEMBL184109 | — | — | 1 | 8.10 |
| CHEMBL362556 | — | — | 1 | 8.05 |
| CHEMBL362392 | — | — | 1 | 8.05 |
| CHEMBL186805 | — | — | 1 | 7.96 |
| CHEMBL363760 | — | — | 1 | 7.70 |
| CHEMBL186930 | — | — | 1 | 7.70 |
| CHEMBL186948 | — | — | 1 | 7.66 |
| CHEMBL360248 | — | — | 1 | 7.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL433586 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL181601 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL184578 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL186954 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL183475 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL366093 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL186683 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL184109 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL362556 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL362392 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL186805 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL363760 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL186930 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL186948 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL360248 | — | EC50 | = | 31.0 | nM | 7.51 |