Assay Detail
ADMET
CHEMBL1743469
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Mechanism based inhibition of human cytochrome P450 3A4 measured by testosterone 6-beta hydroxylation using human liver microsomes
6
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Tissue | Liver |
| Subcellular | Microsome |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 5.61 | 5.86 |
| Kinact | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL36148 | (S)-VERAPAMIL | — | 2 | 5.86 |
| CHEMBL1298 | NORVERAPAMIL | — | 2 | 5.68 |
| CHEMBL197 | DEXVERAPAMIL | 2.0 | 2 | 5.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL36148 | (S)-VERAPAMIL | Ki | = | 1390.0 | nM | 5.86 |
| CHEMBL1298 | NORVERAPAMIL | Ki | = | 2110.0 | nM | 5.68 |
| CHEMBL197 | DEXVERAPAMIL | Ki | = | 5100.0 | nM | 5.29 |
| CHEMBL1298 | NORVERAPAMIL | Kinact | = | 0.21 | min-1 | - |
| CHEMBL197 | DEXVERAPAMIL | Kinact | = | 0.08 | min-1 | - |
| CHEMBL36148 | (S)-VERAPAMIL | Kinact | = | 0.13 | min-1 | - |