Assay Detail
Binding
CHEMBL1664451
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Displacement of [3H]E1 from human placental 17beta-HSD1 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 |
| 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 | 7.40 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1650658 | — | — | 1 | 7.82 |
| CHEMBL469227 | — | — | 1 | 7.70 |
| CHEMBL1650645 | — | — | 1 | 7.58 |
| CHEMBL1650646 | — | — | 1 | 7.48 |
| CHEMBL1650652 | — | — | 1 | 7.44 |
| CHEMBL1650654 | — | — | 1 | 7.28 |
| CHEMBL1650647 | — | — | 1 | 7.19 |
| CHEMBL1650644 | — | — | 1 | 7.16 |
| CHEMBL195217 | — | — | 1 | 6.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1650658 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL469227 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1650645 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1650646 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL1650652 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL1650654 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL1650647 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL1650644 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL195217 | — | IC50 | = | 116.0 | nM | 6.94 |