Assay Detail
Binding
CHEMBL1102465
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Displacement of [3H]17beta-estradiol from human ERalpha expressed in SF9 cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-based design, synthesis and in vitro characterization of potent 17beta-hydroxysteroid dehydrogenase type 1 inhibitors based on 2-substitutions of estrone and D-homo-estrone.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.24 | 7.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 7.90 |
| CHEMBL1405 | ESTRONE | 4.0 | 1 | 7.02 |
| CHEMBL1081361 | — | — | 1 | 6.11 |
| CHEMBL1076306 | — | — | 1 | 5.21 |
| CHEMBL425194 | — | — | 1 | 4.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | IC50 | = | 12.5 | nM | 7.90 |
| CHEMBL1405 | ESTRONE | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL1081361 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL1076306 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL425194 | — | IC50 | = | 11000.0 | nM | 4.96 |