Assay Detail
ADMET
CHEMBL3531927
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Inhibition of CYP2B6 variant in human liver microsomes harboring CYP2B6*1/*1 genotype assessed as 8-hydroxyefavirenz formation using efavirenz as substrate after 15 mins by LC/MS/MS analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Tissue | Liver |
| Subcellular | Microsomes |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 6.63 | 6.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1771 | CLOPIDOGREL | 4.0 | 1 | 6.85 |
| CHEMBL638 | VORICONAZOLE | 4.0 | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1771 | CLOPIDOGREL | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL638 | VORICONAZOLE | IC50 | = | 400.0 | nM | 6.40 |