Assay Detail
Binding
CHEMBL1664595
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Displacement of [3H]E1 from 17beta-HSD1 in human T47D cells after 10 mins by fluid scintillation counting
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | T47D |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
17-beta-hydroxysteroid dehydrogenase type 1 (CHEMBL3181) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17β-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of estrogen-dependent diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.71 | 7.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1650658 | — | — | 1 | 7.15 |
| CHEMBL1650652 | — | — | 1 | 6.94 |
| CHEMBL1650645 | — | — | 1 | 6.78 |
| CHEMBL195217 | — | — | 1 | 6.64 |
| CHEMBL469227 | — | — | 1 | 6.55 |
| CHEMBL1650646 | — | — | 1 | 6.17 |
| CHEMBL1650654 | — | — | 1 | - |
| CHEMBL1650647 | — | — | 1 | - |
| CHEMBL1650644 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1650658 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL1650652 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL1650645 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL195217 | — | IC50 | = | 229.0 | nM | 6.64 |
| CHEMBL469227 | — | IC50 | = | 281.0 | nM | 6.55 |
| CHEMBL1650646 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL1650654 | — | IC50 | - | — | - | |
| CHEMBL1650647 | — | IC50 | - | — | - | |
| CHEMBL1650644 | — | IC50 | - | — | - |