Assay Detail
Binding
CHEMBL1787614
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of aromatase in human placental microsomes assessed as inhibition of aromatization of [1,2,6,7-3H] androstenedione by flow scintillation analysis
13
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
Lead optimization of 4-imidazolylflavans: new promising aromatase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.66 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1444 | LETROZOLE | 4.0 | 1 | 7.75 |
| CHEMBL1783177 | — | — | 1 | 7.50 |
| CHEMBL1783178 | — | — | 3 | 7.47 |
| CHEMBL1783176 | — | — | 1 | 7.44 |
| CHEMBL95109 | — | — | 3 | 7.22 |
| CHEMBL256665 | — | — | 1 | 6.20 |
| CHEMBL255108 | — | — | 1 | 5.81 |
| CHEMBL404225 | — | — | 1 | 5.37 |
| CHEMBL488 | AMINOGLUTETHIMIDE | 4.0 | 1 | 5.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1444 | LETROZOLE | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1783177 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1783178 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL1783176 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL95109 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL1783178 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL95109 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL1783178 | — | IC50 | = | 534.0 | nM | 6.27 |
| CHEMBL95109 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL256665 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL255108 | — | IC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL404225 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL488 | AMINOGLUTETHIMIDE | IC50 | = | 5800.0 | nM | 5.24 |