Assay Detail
Binding
CHEMBL679543
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Estrone sulfatase activity against homogenized human JEG-3 cells was determined by measuring the [3H]E1 obtained from [3H]E1S
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | JEG-3 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
17 alpha-alkyl- or 17 alpha-substituted benzyl-17 beta-estradiols: a new family of estrone-sulfatase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.32 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1627429 | — | — | 1 | 7.62 |
| CHEMBL518966 | — | — | 1 | 7.55 |
| CHEMBL1628091 | — | — | 1 | 7.10 |
| CHEMBL1627418 | — | — | 1 | 6.96 |
| CHEMBL1627421 | — | — | 1 | 6.96 |
| CHEMBL482212 | — | — | 1 | 6.51 |
| CHEMBL1627427 | — | — | 1 | 6.36 |
| CHEMBL1627417 | — | — | 1 | 6.11 |
| CHEMBL1627410 | — | — | 1 | 6.08 |
| CHEMBL1627433 | — | — | 1 | 6.03 |
| CHEMBL1627411 | — | — | 1 | 5.70 |
| CHEMBL494753 | ESTRONE SULFURIC ACID | 4.0 | 1 | 5.12 |
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 4.08 |
| CHEMBL1627425 | — | — | 1 | - |
| CHEMBL1628149 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1627429 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL518966 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1628091 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1627418 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1627421 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL482212 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL1627427 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL1627417 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL1627410 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL1627433 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL1627411 | — | IC50 | = | 1980.0 | nM | 5.70 |
| CHEMBL494753 | ESTRONE SULFURIC ACID | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL135 | ESTRADIOL | IC50 | = | 84000.0 | nM | 4.08 |
| CHEMBL1627425 | — | IC50 | ~ | 1000.0 | nM | - |
| CHEMBL1628149 | — | IC50 | ~ | 6000.0 | nM | - |