Assay Detail
Binding
CHEMBL1664450
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]E2 from human placental 17beta-HSD2 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 2 (CHEMBL2789) ↗| 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 | 5.96 | 6.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1650658 | — | — | 1 | 6.39 |
| CHEMBL1650646 | — | — | 1 | 6.28 |
| CHEMBL1650644 | — | — | 1 | 6.28 |
| CHEMBL469227 | — | — | 1 | 6.27 |
| CHEMBL1650652 | — | — | 1 | 6.02 |
| CHEMBL1650645 | — | — | 1 | 5.94 |
| CHEMBL1650654 | — | — | 1 | 5.75 |
| CHEMBL1650647 | — | — | 1 | 5.48 |
| CHEMBL195217 | — | — | 1 | 5.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1650658 | — | IC50 | = | 403.0 | nM | 6.39 |
| CHEMBL1650646 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL1650644 | — | IC50 | = | 527.0 | nM | 6.28 |
| CHEMBL469227 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL1650652 | — | IC50 | = | 959.0 | nM | 6.02 |
| CHEMBL1650645 | — | IC50 | = | 1157.0 | nM | 5.94 |
| CHEMBL1650654 | — | IC50 | = | 1757.0 | nM | 5.75 |
| CHEMBL1650647 | — | IC50 | = | 3340.0 | nM | 5.48 |
| CHEMBL195217 | — | IC50 | = | 5641.0 | nM | 5.25 |