Assay Detail
Binding
CHEMBL5053646
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Antagonist activity at ERalpha (unknown origin) assessed as inhibition of fluorescein-labeled PGC-1 coactivator recruitment incubated for 30 mins measured by TR-FRET assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Heterodimeric GW7604 Derivatives: Modification of the Pharmacological Profile by Additional Interactions at the Coactivator Binding Site.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.73 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5086315 | — | — | 1 | 7.68 |
| CHEMBL5076984 | — | — | 1 | 6.90 |
| CHEMBL5092721 | — | — | 1 | 5.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5086315 | — | IC50 | = | 20.88 | nM | 7.68 |
| CHEMBL5076984 | — | IC50 | = | 125.3 | nM | 6.90 |
| CHEMBL5092721 | — | IC50 | = | 2433.0 | nM | 5.61 |