Assay Detail
Binding
CHEMBL2013287
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Inhibition of steroid sulfatase in human MCF7 cells using [3H]E1S as substrate after 20 hrs by scintillation spectrometry
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MCF7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and evaluation of analogues of estrone-3-O-sulfamate as potent steroid sulfatase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 8.74 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2011408 | — | — | 1 | 11.00 |
| CHEMBL364332 | — | — | 1 | 9.96 |
| CHEMBL2011415 | — | — | 1 | 9.36 |
| CHEMBL2011414 | — | — | 1 | 9.21 |
| CHEMBL364745 | — | — | 1 | 9.09 |
| CHEMBL122708 | EMATE | — | 1 | 9.08 |
| CHEMBL2011416 | — | — | 1 | 8.92 |
| CHEMBL2011407 | — | — | 1 | 8.08 |
| CHEMBL2011409 | — | — | 1 | 7.43 |
| CHEMBL2011417 | — | — | 1 | 7.38 |
| CHEMBL2011411 | — | — | 1 | 6.63 |
| CHEMBL2011419 | — | — | 1 | - |
| CHEMBL2011420 | — | — | 1 | - |
| CHEMBL2011421 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2011408 | — | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL364332 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL2011415 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL2011414 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL364745 | — | IC50 | = | 0.81 | nM | 9.09 |
| CHEMBL122708 | EMATE | IC50 | = | 0.83 | nM | 9.08 |
| CHEMBL2011416 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL2011407 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL2011409 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL2011417 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL2011411 | — | IC50 | = | 236.0 | nM | 6.63 |
| CHEMBL2011419 | — | IC50 | - | — | - | |
| CHEMBL2011420 | — | IC50 | - | — | - | |
| CHEMBL2011421 | — | IC50 | - | — | - |