Assay Detail
ADMET
CHEMBL3540944
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant CYP3A4 (unknown origin) expressed in baculosomes in presence of 1 mM NADPH
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
Mechanism-based inactivation of cytochrome P450 3A4 by mibefradil through heme destruction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 2 | 6.32 | 6.55 |
| Kinact | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL45816 | MIBEFRADIL | 4.0 | 2 | 6.55 |
| CHEMBL3526662 | — | — | 2 | 6.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL45816 | MIBEFRADIL | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL3526662 | — | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL45816 | MIBEFRADIL | Kinact | = | 0.59 | /min | - |
| CHEMBL3526662 | — | Kinact | = | 0.08 | /min | - |