Assay Detail
ADMET
CHEMBL3539571
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CYP3A4.2 (unknown origin)-mediated testosterone 6beta-hydroxylation incubated for 10 mins prior to NADPH addition measured after 20 mins by HPLC-UV analysis
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Comparison of the inhibitory profiles of itraconazole and cimetidine in cytochrome P450 3A4 genetic variants.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 2 | - | - |
| Ki | 2 | 7.35 | 7.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL64391 | ITRACONAZOLE | 4.0 | 2 | 7.35 |
| CHEMBL30 | CIMETIDINE | 4.0 | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL64391 | ITRACONAZOLE | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL64391 | ITRACONAZOLE | Inhibition | - | % | - | |
| CHEMBL30 | CIMETIDINE | Inhibition | - | % | - | |
| CHEMBL30 | CIMETIDINE | Ki | = | 360000.0 | nM | - |