Assay Detail
Binding
CHEMBL5053651
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Antagonist activity at ERalpha (unknown origin) expressed in human U2OS cells assessed as inhibition of E2-induced transactivation by dual luciferase reporter gene assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| 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 | 18 | 7.52 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL489 | AFIMOXIFENE | 3.0 | 1 | 8.64 |
| CHEMBL5094545 | — | — | 1 | 8.28 |
| CHEMBL5092721 | — | — | 1 | 8.04 |
| CHEMBL5091421 | — | — | 1 | 8.03 |
| CHEMBL5085956 | — | — | 1 | 8.01 |
| CHEMBL5086315 | — | — | 1 | 7.73 |
| CHEMBL5094540 | — | — | 1 | 7.70 |
| CHEMBL5071793 | — | — | 1 | 7.67 |
| CHEMBL5087008 | — | — | 1 | 7.58 |
| CHEMBL5094443 | — | — | 1 | 7.52 |
| CHEMBL5076984 | — | — | 1 | 7.51 |
| CHEMBL5075366 | — | — | 1 | 7.46 |
| CHEMBL5088360 | — | — | 1 | 7.09 |
| CHEMBL5094584 | — | — | 1 | 6.98 |
| CHEMBL5092334 | — | — | 1 | 6.97 |
| CHEMBL1091535 | — | — | 1 | 6.62 |
| CHEMBL5083251 | — | — | 1 | 6.04 |
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL489 | AFIMOXIFENE | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5094545 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL5092721 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL5091421 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL5085956 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL5086315 | — | IC50 | = | 18.5 | nM | 7.73 |
| CHEMBL5094540 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5071793 | — | IC50 | = | 21.5 | nM | 7.67 |
| CHEMBL5087008 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5094443 | — | IC50 | = | 30.2 | nM | 7.52 |
| CHEMBL5076984 | — | IC50 | = | 30.9 | nM | 7.51 |
| CHEMBL5075366 | — | IC50 | = | 34.5 | nM | 7.46 |
| CHEMBL5088360 | — | IC50 | = | 80.8 | nM | 7.09 |
| CHEMBL5094584 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL5092334 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL1091535 | — | IC50 | = | 238.0 | nM | 6.62 |
| CHEMBL5083251 | — | IC50 | = | 914.0 | nM | 6.04 |
| CHEMBL1358 | FULVESTRANT | IC50 | - | — | - |