Assay Detail
Binding
CHEMBL4391749
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Inhibition of recombinant human aromatase preincubated for 10 mins followed by substrate and beta-NADP+ addition and measured for 60 mins by fluorescence method
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Rational design of allosteric modulators of the aromatase enzyme: An unprecedented therapeutic strategy to fight breast cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.26 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1444 | LETROZOLE | 4.0 | 1 | 8.00 |
| CHEMBL4437198 | — | — | 1 | 5.29 |
| CHEMBL1093458 | ENDOXIFEN | 3.0 | 1 | 5.21 |
| CHEMBL4568316 | — | — | 1 | 4.96 |
| CHEMBL4474808 | — | — | 1 | 4.68 |
| CHEMBL4453737 | — | — | 1 | 4.66 |
| CHEMBL1991089 | — | — | 1 | 4.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1444 | LETROZOLE | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4437198 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL1093458 | ENDOXIFEN | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL4568316 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4474808 | — | IC50 | = | 20900.0 | nM | 4.68 |
| CHEMBL4453737 | — | IC50 | = | 21700.0 | nM | 4.66 |
| CHEMBL1991089 | — | IC50 | = | 95300.0 | nM | 4.02 |