Assay Detail
Binding
CHEMBL5334556
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human 17beta-HSD1 expressed in human T47D cells using [3H]E1 as substrate incubated for 1 hr followed by substrate addition measured after 40 mins in presence of E1 by HPLC analysis
12
Total Activities
12
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
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 | 12 | 7.51 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5080299 | — | — | 1 | 8.54 |
| CHEMBL5440157 | — | — | 1 | 8.49 |
| CHEMBL4071588 | — | — | 1 | 8.10 |
| CHEMBL5429832 | — | — | 1 | 7.96 |
| CHEMBL4071245 | — | — | 1 | 7.66 |
| CHEMBL5394384 | — | — | 1 | 7.28 |
| CHEMBL5393885 | — | — | 1 | 7.24 |
| CHEMBL5417947 | — | — | 1 | 7.10 |
| CHEMBL5431739 | — | — | 1 | 7.06 |
| CHEMBL5394095 | — | — | 1 | 6.96 |
| CHEMBL5440694 | — | — | 1 | 6.85 |
| CHEMBL5415093 | — | — | 1 | 6.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5080299 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5440157 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4071588 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL5429832 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4071245 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5394384 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5393885 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL5417947 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL5431739 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL5394095 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5440694 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5415093 | — | IC50 | = | 140.0 | nM | 6.85 |