Assay Detail
Binding
CHEMBL5053639
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of fluorescent-labeled E2 from LBD of ERalpha (unknown origin) by TR-FRET assay
18
Total Activities
18
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 | 18 | 8.64 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 9.48 |
| CHEMBL5076984 | — | — | 1 | 8.89 |
| CHEMBL5086315 | — | — | 1 | 8.85 |
| CHEMBL5087008 | — | — | 1 | 8.84 |
| CHEMBL5092721 | — | — | 1 | 8.81 |
| CHEMBL5092334 | — | — | 1 | 8.79 |
| CHEMBL5075366 | — | — | 1 | 8.65 |
| CHEMBL489 | AFIMOXIFENE | 3.0 | 1 | 8.65 |
| CHEMBL5091421 | — | — | 1 | 8.58 |
| CHEMBL5085956 | — | — | 1 | 8.56 |
| CHEMBL5088360 | — | — | 1 | 8.56 |
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | 8.54 |
| CHEMBL5094540 | — | — | 1 | 8.47 |
| CHEMBL5094443 | — | — | 1 | 8.40 |
| CHEMBL5071793 | — | — | 1 | 8.39 |
| CHEMBL5083251 | — | — | 1 | 8.37 |
| CHEMBL5094584 | — | — | 1 | 8.33 |
| CHEMBL1091535 | — | — | 1 | 8.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL5076984 | — | IC50 | = | 1.28 | nM | 8.89 |
| CHEMBL5086315 | — | IC50 | = | 1.41 | nM | 8.85 |
| CHEMBL5087008 | — | IC50 | = | 1.45 | nM | 8.84 |
| CHEMBL5092721 | — | IC50 | = | 1.56 | nM | 8.81 |
| CHEMBL5092334 | — | IC50 | = | 1.62 | nM | 8.79 |
| CHEMBL5075366 | — | IC50 | = | 2.22 | nM | 8.65 |
| CHEMBL489 | AFIMOXIFENE | IC50 | = | 2.24 | nM | 8.65 |
| CHEMBL5091421 | — | IC50 | = | 2.61 | nM | 8.58 |
| CHEMBL5085956 | — | IC50 | = | 2.75 | nM | 8.56 |
| CHEMBL5088360 | — | IC50 | = | 2.72 | nM | 8.56 |
| CHEMBL1358 | FULVESTRANT | IC50 | = | 2.85 | nM | 8.54 |
| CHEMBL5094540 | — | IC50 | = | 3.41 | nM | 8.47 |
| CHEMBL5094443 | — | IC50 | = | 4.01 | nM | 8.40 |
| CHEMBL5071793 | — | IC50 | = | 4.11 | nM | 8.39 |
| CHEMBL5083251 | — | IC50 | = | 4.23 | nM | 8.37 |
| CHEMBL5094584 | — | IC50 | = | 4.63 | nM | 8.33 |
| CHEMBL1091535 | — | IC50 | = | 5.35 | nM | 8.27 |