Assay Detail
Binding
CHEMBL5037521
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Inhibition of human aromatase assessed as reduction in fluorescence intensity preincubated with NADPH regenerating system for 10 mins followed by substrate addition incubated for 60 mins by fluorescence based microplate reader analysis
14
Total Activities
14
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
Balanced dual acting compounds targeting aromatase and estrogen receptor α as an emerging therapeutic opportunity to counteract estrogen responsive breast cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.64 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1444 | LETROZOLE | 4.0 | 1 | 8.40 |
| CHEMBL5080066 | — | — | 1 | 7.64 |
| CHEMBL5072101 | — | — | 1 | 7.46 |
| CHEMBL5074047 | — | — | 1 | 7.28 |
| CHEMBL5081446 | — | — | 1 | 7.20 |
| CHEMBL5082681 | — | — | 1 | 6.22 |
| CHEMBL5069811 | — | — | 1 | 6.07 |
| CHEMBL5092560 | — | — | 1 | 6.05 |
| CHEMBL5075144 | — | — | 1 | 6.02 |
| CHEMBL5087363 | — | — | 1 | 6.00 |
| CHEMBL5082245 | — | — | 1 | 5.90 |
| CHEMBL5092843 | — | — | 1 | 5.49 |
| CHEMBL5077976 | — | — | 1 | - |
| CHEMBL1093458 | ENDOXIFEN | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1444 | LETROZOLE | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5080066 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5072101 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5074047 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL5081446 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL5082681 | — | IC50 | = | 596.0 | nM | 6.22 |
| CHEMBL5069811 | — | IC50 | = | 861.0 | nM | 6.07 |
| CHEMBL5092560 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL5075144 | — | IC50 | = | 952.0 | nM | 6.02 |
| CHEMBL5087363 | — | IC50 | = | 1002.0 | nM | 6.00 |
| CHEMBL5082245 | — | IC50 | = | 1253.0 | nM | 5.90 |
| CHEMBL5092843 | — | IC50 | = | 3240.0 | nM | 5.49 |
| CHEMBL5077976 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1093458 | ENDOXIFEN | IC50 | > | 10000.0 | nM | - |