Assay Detail
Binding
CHEMBL2388439
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant microsomal aromatase-mediated 7-methoxy-4-trifluoromethylcoumarin conversion to 7-hydroxytrifluoromethylcoumarin preincubated for 10 mins measured after 30 mins by fluorescence assay
5
Total Activities
5
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
Synthesis of mixed (E,Z)-, (E)-, and (Z)-norendoxifen with dual aromatase inhibitory and estrogen receptor modulatory activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.95 | 7.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2386285 | — | — | 1 | 7.12 |
| CHEMBL3350384 | — | — | 1 | 6.99 |
| CHEMBL2386284 | — | — | 1 | 5.99 |
| CHEMBL2386286 | — | — | 1 | 5.03 |
| CHEMBL149791 | — | — | 1 | 4.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2386285 | — | IC50 | = | 76.8 | nM | 7.12 |
| CHEMBL3350384 | — | IC50 | = | 102.2 | nM | 6.99 |
| CHEMBL2386284 | — | IC50 | = | 1029.0 | nM | 5.99 |
| CHEMBL2386286 | — | IC50 | = | 9257.0 | nM | 5.03 |
| CHEMBL149791 | — | IC50 | = | 24880.0 | nM | 4.60 |