Assay Detail
Binding
CHEMBL4219451
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of fluorescein-labeled estradiol (fluoromone) from human recombinant full-length estrogen receptor beta after 2 hrs by fluorescence polarization assay
24
Total Activities
24
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
Lead Optimization of Benzoxepin-Type Selective Estrogen Receptor (ER) Modulators and Downregulators with Subtype-Specific ERα and ERβ Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 7.28 | 9.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4228617 | — | — | 1 | 9.26 |
| CHEMBL4227113 | — | — | 1 | 9.03 |
| CHEMBL4225078 | — | — | 1 | 8.91 |
| CHEMBL4228923 | — | — | 1 | 8.62 |
| CHEMBL4224880 | — | — | 1 | 8.51 |
| CHEMBL1091535 | — | — | 1 | 8.17 |
| CHEMBL4225102 | — | — | 1 | 7.60 |
| CHEMBL2137046 | — | — | 1 | 7.58 |
| CHEMBL4225690 | — | — | 1 | 7.47 |
| CHEMBL4225156 | — | — | 1 | 7.37 |
| CHEMBL4228388 | — | — | 1 | 7.34 |
| CHEMBL4224834 | — | — | 1 | 7.14 |
| CHEMBL4228649 | — | — | 1 | 7.14 |
| CHEMBL4229221 | — | — | 1 | 6.92 |
| CHEMBL83 | TAMOXIFEN | 4.0 | 1 | 6.77 |
| CHEMBL4227881 | — | — | 1 | 6.76 |
| CHEMBL4228974 | — | — | 1 | 6.69 |
| CHEMBL4225680 | — | — | 1 | 6.45 |
| CHEMBL4228886 | — | — | 1 | 6.40 |
| CHEMBL4225431 | — | — | 1 | 6.35 |
| CHEMBL4225954 | — | — | 1 | 6.23 |
| CHEMBL4225599 | — | — | 1 | 5.99 |
| CHEMBL4225059 | — | — | 1 | 4.84 |
| CHEMBL4228142 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4228617 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL4227113 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL4225078 | — | IC50 | = | 1.23 | nM | 8.91 |
| CHEMBL4228923 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4224880 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL1091535 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL4225102 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2137046 | — | IC50 | = | 26.1 | nM | 7.58 |
| CHEMBL4225690 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4225156 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4228388 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4224834 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4228649 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4229221 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL83 | TAMOXIFEN | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4227881 | — | IC50 | = | 175.0 | nM | 6.76 |
| CHEMBL4228974 | — | IC50 | = | 203.0 | nM | 6.69 |
| CHEMBL4225680 | — | IC50 | = | 354.0 | nM | 6.45 |
| CHEMBL4228886 | — | IC50 | = | 395.0 | nM | 6.40 |
| CHEMBL4225431 | — | IC50 | = | 447.0 | nM | 6.35 |
| CHEMBL4225954 | — | IC50 | = | 585.0 | nM | 6.23 |
| CHEMBL4225599 | — | IC50 | = | 1014.0 | nM | 5.99 |
| CHEMBL4225059 | — | IC50 | = | 14340.0 | nM | 4.84 |
| CHEMBL4228142 | — | IC50 | - | — | - |