Assay Detail
Binding
CHEMBL682296
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Ability to displace [3H]17-beta-estradiol from Estrogen receptor alpha by scintillation proximity assay.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
2-Amino-4,6-diarylpyridines as novel ligands for the estrogen receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 6.80 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL81 | RALOXIFENE | 4.0 | 1 | 9.66 |
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 8.66 |
| CHEMBL58714 | — | — | 1 | 7.70 |
| CHEMBL57093 | — | — | 1 | 7.16 |
| CHEMBL58330 | — | — | 1 | 6.89 |
| CHEMBL58563 | — | — | 1 | 6.80 |
| CHEMBL292573 | — | — | 1 | 6.75 |
| CHEMBL58486 | — | — | 1 | 6.68 |
| CHEMBL59184 | — | — | 1 | 6.42 |
| CHEMBL58449 | — | — | 1 | 6.35 |
| CHEMBL57875 | — | — | 1 | 6.31 |
| CHEMBL59552 | — | — | 1 | 6.21 |
| CHEMBL294710 | — | — | 1 | 6.19 |
| CHEMBL58504 | — | — | 1 | 6.18 |
| CHEMBL61026 | — | — | 1 | 6.08 |
| CHEMBL59271 | — | — | 1 | 5.90 |
| CHEMBL60909 | — | — | 1 | 5.70 |
| CHEMBL58741 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL81 | RALOXIFENE | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL135 | ESTRADIOL | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL58714 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL57093 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL58330 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL58563 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL292573 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL58486 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL59184 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL58449 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL57875 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL59552 | — | Ki | = | 620.0 | nM | 6.21 |
| CHEMBL294710 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL58504 | — | Ki | = | 660.0 | nM | 6.18 |
| CHEMBL61026 | — | Ki | = | 830.0 | nM | 6.08 |
| CHEMBL59271 | — | Ki | = | 1260.0 | nM | 5.90 |
| CHEMBL60909 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL58741 | — | Ki | > | 3000.0 | nM | - |