Assay Detail
Binding
CHEMBL5037522
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human ERalpha measured after 2 hrs by fluorescence polarization plate reader
14
Total Activities
14
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
Balanced dual acting compounds targeting aromatase and estrogen receptor α as an emerging therapeutic opportunity to counteract estrogen responsive breast cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.52 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5080066 | — | — | 1 | 7.72 |
| CHEMBL1093458 | ENDOXIFEN | 3.0 | 1 | 7.52 |
| CHEMBL5092560 | — | — | 1 | 7.48 |
| CHEMBL5077976 | — | — | 1 | 7.12 |
| CHEMBL5074047 | — | — | 1 | 6.71 |
| CHEMBL5082681 | — | — | 1 | 6.65 |
| CHEMBL5092843 | — | — | 1 | 6.50 |
| CHEMBL5075144 | — | — | 1 | 5.97 |
| CHEMBL5081446 | — | — | 1 | 5.76 |
| CHEMBL5069811 | — | — | 1 | 5.75 |
| CHEMBL5072101 | — | — | 1 | 5.74 |
| CHEMBL5087363 | — | — | 1 | 5.30 |
| CHEMBL5082245 | — | — | 1 | - |
| CHEMBL1444 | LETROZOLE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5080066 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1093458 | ENDOXIFEN | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5092560 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5077976 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL5074047 | — | IC50 | = | 197.0 | nM | 6.71 |
| CHEMBL5082681 | — | IC50 | = | 223.0 | nM | 6.65 |
| CHEMBL5092843 | — | IC50 | = | 313.0 | nM | 6.50 |
| CHEMBL5075144 | — | IC50 | = | 1073.0 | nM | 5.97 |
| CHEMBL5081446 | — | IC50 | = | 1737.0 | nM | 5.76 |
| CHEMBL5069811 | — | IC50 | = | 1770.0 | nM | 5.75 |
| CHEMBL5072101 | — | IC50 | = | 1803.0 | nM | 5.74 |
| CHEMBL5087363 | — | IC50 | = | 4950.0 | nM | 5.30 |
| CHEMBL5082245 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1444 | LETROZOLE | IC50 | > | 10000.0 | nM | - |