Assay Detail
ADMET
CHEMBL5045402
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Time dependent inhibition of CYP3A in human liver microsomes using midazolam as substrate preincubated for 30 mins in presence of NADPH generating system followed by substrate addition incubated for 30 mins by LC-MS/MS analysi
4
Total Activities
4
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
Unique Oxidative Metabolism of Bufalin Generates Two Reactive Metabolites That Strongly Inactivate Human Cytochrome P450 3A.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.26 | 6.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2068968 | — | — | 1 | 6.35 |
| CHEMBL451719 | — | — | 1 | 6.28 |
| CHEMBL2069016 | — | — | 1 | 6.27 |
| CHEMBL399680 | BUFALIN | — | 1 | 6.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2068968 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL451719 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL2069016 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL399680 | BUFALIN | IC50 | = | 740.0 | nM | 6.13 |