Assay Detail
Binding
CHEMBL3777355
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-E2 from human ER-alpha incubated for 16 to 20 hrs by liquid scintillation counting analysis
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
Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 8.06 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3774647 | — | — | 1 | 9.40 |
| CHEMBL2137046 | — | — | 1 | 9.30 |
| CHEMBL3775016 | — | — | 1 | 9.10 |
| CHEMBL3774660 | — | — | 1 | 8.89 |
| CHEMBL3775434 | — | — | 1 | 8.11 |
| CHEMBL83 | TAMOXIFEN | 4.0 | 1 | 8.10 |
| CHEMBL3775283 | — | — | 1 | 7.91 |
| CHEMBL3775129 | — | — | 1 | 7.66 |
| CHEMBL3775224 | — | — | 1 | 7.57 |
| CHEMBL3775410 | — | — | 1 | 7.50 |
| CHEMBL3775375 | — | — | 1 | 7.48 |
| CHEMBL3775006 | — | — | 1 | 7.46 |
| CHEMBL3775978 | — | — | 1 | 7.32 |
| CHEMBL3774642 | — | — | 1 | 7.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3774647 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL2137046 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3775016 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3774660 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3775434 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL83 | TAMOXIFEN | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3775283 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL3775129 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3775224 | — | IC50 | = | 27.1 | nM | 7.57 |
| CHEMBL3775410 | — | IC50 | = | 31.9 | nM | 7.50 |
| CHEMBL3775375 | — | IC50 | = | 33.3 | nM | 7.48 |
| CHEMBL3775006 | — | IC50 | = | 34.5 | nM | 7.46 |
| CHEMBL3775978 | — | IC50 | = | 48.4 | nM | 7.32 |
| CHEMBL3774642 | — | IC50 | = | 81.0 | nM | 7.09 |