Assay Detail
Binding
CHEMBL677815
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Inhibition of estradiol binding to estrogen receptor
10
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Discovery and preclinical pharmacology of a novel, potent, nonsteroidal estrogen receptor agonist/antagonist, CP-336156, a diaryltetrahydronaphthalene.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.82 | 9.45 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 9.45 |
| CHEMBL81 | RALOXIFENE | 4.0 | 1 | 8.73 |
| CHEMBL317748 | — | — | 1 | 8.01 |
| CHEMBL98892 | — | — | 1 | 7.96 |
| CHEMBL328190 | LASOFOXIFENE | 4.0 | 2 | 7.96 |
| CHEMBL28211 | NAFOXIDINE | 2.0 | 1 | 7.39 |
| CHEMBL98116 | — | — | 1 | 7.33 |
| CHEMBL421389 | — | — | 1 | 6.88 |
| CHEMBL100303 | — | — | 1 | 6.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | IC50 | = | 0.354 | nM | 9.45 |
| CHEMBL81 | RALOXIFENE | IC50 | = | 1.85 | nM | 8.73 |
| CHEMBL317748 | — | IC50 | = | 9.75 | nM | 8.01 |
| CHEMBL98892 | — | IC50 | = | 11.1 | nM | 7.96 |
| CHEMBL328190 | LASOFOXIFENE | IC50 | = | 11.1 | nM | 7.96 |
| CHEMBL328190 | LASOFOXIFENE | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL28211 | NAFOXIDINE | IC50 | = | 40.9 | nM | 7.39 |
| CHEMBL98116 | — | IC50 | = | 47.1 | nM | 7.33 |
| CHEMBL421389 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL100303 | — | IC50 | = | 270.0 | nM | 6.57 |