Assay Detail
ADMET
CHEMBL3423893
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Inhibition of human recombinant CYP2A6 assessed as metabolism of coumarin to 7-hydroxycoumarin after 30 mins by fluorescence assay
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and synthesis of norendoxifen analogues with dual aromatase inhibitory and estrogen receptor modulatory activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 5.20 | 5.20 |
| Ki | 2 | 5.91 | 6.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3422028 | — | — | 2 | 6.15 |
| CHEMBL2386285 | — | — | 2 | 5.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3422028 | — | Ki | = | 710.0 | nM | 6.15 |
| CHEMBL2386285 | — | Ki | = | 2180.0 | nM | 5.66 |
| CHEMBL2386285 | — | IC50 | = | 6370.0 | nM | 5.20 |
| CHEMBL3422028 | — | IC50 | = | 6370.0 | nM | 5.20 |