Assay Detail
Binding
CHEMBL5334563
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]E2 as substrate measured after 20 mins in presence of NAD+ by HPLC analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Placenta |
| Subcellular | Microsome |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
17-beta-hydroxysteroid dehydrogenase type 2 (CHEMBL2789) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Potent Dual Inhibitors of Steroid Sulfatase and 17β-Hydroxysteroid Dehydrogenase Type 1 with a Suitable Pharmacokinetic Profile for <i>In Vivo</i> Proof-of-Principle Studies in an Endometriosis Mouse Model.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.56 | 7.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4071245 | — | — | 1 | 7.44 |
| CHEMBL5431739 | — | — | 1 | 5.62 |
| CHEMBL5080299 | — | — | 1 | 5.50 |
| CHEMBL5440694 | — | — | 1 | 5.50 |
| CHEMBL5440157 | — | — | 1 | 5.36 |
| CHEMBL5429832 | — | — | 1 | 5.21 |
| CHEMBL5417947 | — | — | 1 | 5.19 |
| CHEMBL5394384 | — | — | 1 | 5.12 |
| CHEMBL5394095 | — | — | 1 | 5.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4071245 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL5431739 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL5080299 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL5440694 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL5440157 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL5429832 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL5417947 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL5394384 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL5394095 | — | IC50 | = | 7700.0 | nM | 5.11 |