Assay Detail
ADMET
CHEMBL4051804
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Inhibition of human placental cytosolic 17beta-HSD2 using [3H]-E2/E2 substrate and NAD+ after 20 mins by HPLC based radio-detection method
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| 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
First Dual Inhibitors of Steroid Sulfatase (STS) and 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Designed Multiple Ligands as Novel Potential Therapeutics for Estrogen-Dependent Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.64 | 8.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4088890 | — | — | 1 | 8.39 |
| CHEMBL4102153 | — | — | 1 | 7.86 |
| CHEMBL4066635 | — | — | 1 | 7.76 |
| CHEMBL4072794 | — | — | 1 | 7.74 |
| CHEMBL4064200 | — | — | 1 | 7.72 |
| CHEMBL4091943 | — | — | 1 | 7.65 |
| CHEMBL4099681 | — | — | 1 | 7.63 |
| CHEMBL4076477 | — | — | 1 | 7.55 |
| CHEMBL4083248 | — | — | 1 | 7.51 |
| CHEMBL4078356 | — | — | 1 | 7.50 |
| CHEMBL4071245 | — | — | 1 | 7.44 |
| CHEMBL4084183 | — | — | 1 | 7.40 |
| CHEMBL4071588 | — | — | 1 | 7.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4088890 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4102153 | — | IC50 | = | 13.7 | nM | 7.86 |
| CHEMBL4066635 | — | IC50 | = | 17.4 | nM | 7.76 |
| CHEMBL4072794 | — | IC50 | = | 18.4 | nM | 7.74 |
| CHEMBL4064200 | — | IC50 | = | 19.1 | nM | 7.72 |
| CHEMBL4091943 | — | IC50 | = | 22.2 | nM | 7.65 |
| CHEMBL4099681 | — | IC50 | = | 23.2 | nM | 7.63 |
| CHEMBL4076477 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4083248 | — | IC50 | = | 31.2 | nM | 7.51 |
| CHEMBL4078356 | — | IC50 | = | 31.3 | nM | 7.50 |
| CHEMBL4071245 | — | IC50 | = | 36.1 | nM | 7.44 |
| CHEMBL4084183 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4071588 | — | IC50 | = | 71.3 | nM | 7.15 |