Assay Detail
Binding
CHEMBL831372
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Inhibition of [3H]estradiol binding to human estrogen receptor beta 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 | 6.37 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL328190 | LASOFOXIFENE | 4.0 | 1 | 7.89 |
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 7.62 |
| CHEMBL195216 | — | — | 1 | 6.76 |
| CHEMBL192187 | — | — | 1 | 6.62 |
| CHEMBL195212 | — | — | 1 | 6.60 |
| CHEMBL81 | RALOXIFENE | 4.0 | 1 | 6.58 |
| CHEMBL426461 | — | — | 1 | 6.58 |
| CHEMBL195465 | — | — | 1 | 6.48 |
| CHEMBL101382 | — | — | 1 | 6.46 |
| CHEMBL103650 | — | — | 1 | 6.38 |
| CHEMBL427533 | — | — | 1 | 6.37 |
| CHEMBL372011 | — | — | 1 | 6.06 |
| CHEMBL364492 | — | — | 1 | 6.03 |
| CHEMBL195466 | — | — | 1 | 5.96 |
| CHEMBL192055 | — | — | 1 | 5.94 |
| CHEMBL191646 | — | — | 1 | 5.89 |
| CHEMBL191711 | — | — | 1 | 5.86 |
| CHEMBL194334 | — | — | 1 | 5.78 |
| CHEMBL372029 | — | — | 1 | 5.76 |
| CHEMBL195118 | — | — | 1 | 5.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL328190 | LASOFOXIFENE | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL135 | ESTRADIOL | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL195216 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL192187 | — | IC50 | = | 239.0 | nM | 6.62 |
| CHEMBL195212 | — | IC50 | = | 252.0 | nM | 6.60 |
| CHEMBL81 | RALOXIFENE | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL426461 | — | IC50 | = | 266.0 | nM | 6.58 |
| CHEMBL195465 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL101382 | — | IC50 | = | 346.0 | nM | 6.46 |
| CHEMBL103650 | — | IC50 | = | 421.0 | nM | 6.38 |
| CHEMBL427533 | — | IC50 | = | 428.0 | nM | 6.37 |
| CHEMBL372011 | — | IC50 | = | 879.0 | nM | 6.06 |
| CHEMBL364492 | — | IC50 | = | 943.0 | nM | 6.03 |
| CHEMBL195466 | — | IC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL192055 | — | IC50 | = | 1155.0 | nM | 5.94 |
| CHEMBL191646 | — | IC50 | = | 1285.0 | nM | 5.89 |
| CHEMBL191711 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL194334 | — | IC50 | = | 1677.0 | nM | 5.78 |
| CHEMBL372029 | — | IC50 | = | 1730.0 | nM | 5.76 |
| CHEMBL195118 | — | IC50 | = | 1945.0 | nM | 5.71 |