Assay Detail
Binding
CHEMBL831528
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Inhibition of [3H]estradiol binding to human estrogen receptor alpha expressed in HeLa cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.12 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL328190 | LASOFOXIFENE | 4.0 | 1 | 8.40 |
| CHEMBL101382 | — | — | 1 | 7.72 |
| CHEMBL81 | RALOXIFENE | 4.0 | 1 | 7.66 |
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 7.55 |
| CHEMBL195216 | — | — | 1 | 7.42 |
| CHEMBL195212 | — | — | 1 | 7.20 |
| CHEMBL195465 | — | — | 1 | 7.16 |
| CHEMBL364492 | — | — | 1 | 7.08 |
| CHEMBL192187 | — | — | 1 | 7.06 |
| CHEMBL426461 | — | — | 1 | 6.97 |
| CHEMBL372029 | — | — | 1 | 6.97 |
| CHEMBL195118 | — | — | 1 | 6.92 |
| CHEMBL191711 | — | — | 1 | 6.91 |
| CHEMBL195466 | — | — | 1 | 6.91 |
| CHEMBL372011 | — | — | 1 | 6.79 |
| CHEMBL192055 | — | — | 1 | 6.79 |
| CHEMBL194334 | — | — | 1 | 6.77 |
| CHEMBL191646 | — | — | 1 | 6.75 |
| CHEMBL427533 | — | — | 1 | 6.73 |
| CHEMBL103650 | — | — | 1 | 6.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL328190 | LASOFOXIFENE | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL101382 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL81 | RALOXIFENE | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL135 | ESTRADIOL | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL195216 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL195212 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL195465 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL364492 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL192187 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL426461 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL372029 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL195118 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL191711 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL195466 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL372011 | — | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL192055 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL194334 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL191646 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL427533 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL103650 | — | IC50 | = | 285.0 | nM | 6.54 |