Assay Detail
Binding
CHEMBL2013286
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Inhibition of steroid sulfatase in human placental microsomes using [3H]E1S as substrate after 30 mins by scintillation spectrometry
22
Total Activities
21
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Placenta |
| Subcellular | Microsomes |
| 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 | 21 | 7.56 | 10.00 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2011422 | — | — | 1 | 10.00 |
| CHEMBL2011408 | — | — | 1 | 9.10 |
| CHEMBL364332 | — | — | 1 | 8.78 |
| CHEMBL2011415 | — | — | 1 | 8.47 |
| CHEMBL2011416 | — | — | 1 | 8.28 |
| CHEMBL2011414 | — | — | 1 | 8.25 |
| CHEMBL364745 | — | — | 1 | 8.21 |
| CHEMBL122708 | EMATE | — | 2 | 7.75 |
| CHEMBL2011407 | — | — | 1 | 7.16 |
| CHEMBL2011418 | — | — | 1 | 6.70 |
| CHEMBL190451 | — | — | 1 | 6.09 |
| CHEMBL2011417 | — | — | 1 | 5.92 |
| CHEMBL2011409 | — | — | 1 | 5.60 |
| CHEMBL2011411 | — | — | 1 | 5.54 |
| CHEMBL2011413 | — | — | 1 | - |
| CHEMBL2011412 | — | — | 1 | - |
| CHEMBL2011410 | — | — | 1 | - |
| CHEMBL2011419 | — | — | 1 | - |
| CHEMBL2011420 | — | — | 1 | - |
| CHEMBL2011421 | — | — | 1 | - |
| CHEMBL189050 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2011422 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL2011408 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL364332 | — | IC50 | = | 1.65 | nM | 8.78 |
| CHEMBL2011415 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL2011416 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL2011414 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL364745 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL122708 | EMATE | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2011407 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2011418 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL190451 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL2011417 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL2011409 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2011411 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL2011413 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2011412 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2011410 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2011419 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2011420 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2011421 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL189050 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL122708 | EMATE | Inhibition | - | % | - |