Assay Detail
Binding
CHEMBL5053652
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at ERbeta (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 | 7.82 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL489 | AFIMOXIFENE | 3.0 | 1 | 9.00 |
| CHEMBL5094545 | — | — | 1 | 8.44 |
| CHEMBL5094443 | — | — | 1 | 8.39 |
| CHEMBL5085956 | — | — | 1 | 8.17 |
| CHEMBL5086315 | — | — | 1 | 8.12 |
| CHEMBL5092721 | — | — | 1 | 8.05 |
| CHEMBL5091421 | — | — | 1 | 8.05 |
| CHEMBL5075366 | — | — | 1 | 7.94 |
| CHEMBL5092334 | — | — | 1 | 7.80 |
| CHEMBL5094540 | — | — | 1 | 7.79 |
| CHEMBL5088360 | — | — | 1 | 7.73 |
| CHEMBL5087008 | — | — | 1 | 7.70 |
| CHEMBL5071793 | — | — | 1 | 7.57 |
| CHEMBL5076984 | — | — | 1 | 7.33 |
| CHEMBL5094584 | — | — | 1 | 7.32 |
| CHEMBL1091535 | — | — | 1 | 6.81 |
| CHEMBL5083251 | — | — | 1 | 6.80 |
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL489 | AFIMOXIFENE | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5094545 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5094443 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL5085956 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL5086315 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL5092721 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL5091421 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5075366 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL5092334 | — | IC50 | = | 15.9 | nM | 7.80 |
| CHEMBL5094540 | — | IC50 | = | 16.1 | nM | 7.79 |
| CHEMBL5088360 | — | IC50 | = | 18.7 | nM | 7.73 |
| CHEMBL5087008 | — | IC50 | = | 20.2 | nM | 7.70 |
| CHEMBL5071793 | — | IC50 | = | 26.9 | nM | 7.57 |
| CHEMBL5076984 | — | IC50 | = | 46.5 | nM | 7.33 |
| CHEMBL5094584 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL1091535 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL5083251 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL1358 | FULVESTRANT | IC50 | - | — | - |