Assay Detail
Binding
CHEMBL863237
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Inhibition of binding to recombinant human ERbeta by scintillation proximity assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Estrogen receptor ligands. Part 14: application of novel antagonist side chains to existing platforms.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 8.18 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL437695 | — | — | 1 | 9.22 |
| CHEMBL197495 | — | — | 1 | 9.05 |
| CHEMBL328190 | LASOFOXIFENE | 4.0 | 1 | 8.74 |
| CHEMBL372808 | — | — | 1 | 8.64 |
| CHEMBL198914 | — | — | 1 | 8.62 |
| CHEMBL198803 | — | — | 1 | 8.59 |
| CHEMBL372337 | — | — | 1 | 8.51 |
| CHEMBL46740 | BAZEDOXIFENE | 4.0 | 1 | 8.42 |
| CHEMBL81 | RALOXIFENE | 4.0 | 1 | 7.92 |
| CHEMBL180300 | — | — | 1 | 7.35 |
| CHEMBL182402 | — | — | 1 | 7.28 |
| CHEMBL362623 | — | — | 1 | 7.19 |
| CHEMBL183584 | — | — | 1 | 6.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL437695 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL197495 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL328190 | LASOFOXIFENE | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL372808 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL198914 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL198803 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL372337 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL46740 | BAZEDOXIFENE | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL81 | RALOXIFENE | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL180300 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL182402 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL362623 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL183584 | — | IC50 | = | 161.0 | nM | 6.79 |