Assay Detail
Binding
CHEMBL967987
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Inhibition of aromatase in human placental microsomes
9
Total Activities
9
Compounds Tested
1
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 of 6- or 4-functionalized indoles via a reductive cyclization approach and evaluation as aromatase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.08 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1399 | ANASTROZOLE | 4.0 | 1 | 8.00 |
| CHEMBL469260 | — | — | 1 | 7.94 |
| CHEMBL1444 | LETROZOLE | 4.0 | 1 | 7.94 |
| CHEMBL468410 | — | — | 1 | 7.73 |
| CHEMBL205177 | — | — | 1 | 7.71 |
| CHEMBL512994 | — | — | 1 | 7.03 |
| CHEMBL513168 | — | — | 1 | 5.79 |
| CHEMBL488 | AMINOGLUTETHIMIDE | 4.0 | 1 | 4.53 |
| CHEMBL468419 | FADROZOLE HYDROCHLORIDE | -1.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1399 | ANASTROZOLE | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL469260 | — | IC50 | = | 11.5 | nM | 7.94 |
| CHEMBL1444 | LETROZOLE | IC50 | = | 11.5 | nM | 7.94 |
| CHEMBL468410 | — | IC50 | = | 18.7 | nM | 7.73 |
| CHEMBL205177 | — | IC50 | = | 19.3 | nM | 7.71 |
| CHEMBL512994 | — | IC50 | = | 93.8 | nM | 7.03 |
| CHEMBL513168 | — | IC50 | = | 1620.0 | nM | 5.79 |
| CHEMBL488 | AMINOGLUTETHIMIDE | IC50 | = | 29750.0 | nM | 4.53 |
| CHEMBL468419 | FADROZOLE HYDROCHLORIDE | IC50 | = | 30.0 | nM | - |