Assay Detail
ADMET
CHEMBL3268199
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Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate measured after 30 mins preincubation by LC-MS/MS analysis in presence of NADPH
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 | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimizing the Physicochemical Properties of Raf/MEK Inhibitors by Nitrogen Scanning.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.11 | 5.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3092189 | — | — | 1 | 5.25 |
| CHEMBL3092195 | — | — | 1 | 4.96 |
| CHEMBL3264002 | AVUTOMETINIB | 3.0 | 1 | - |
| CHEMBL3263996 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3092189 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL3092195 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL3264002 | AVUTOMETINIB | IC50 | > | 100000.0 | nM | - |
| CHEMBL3263996 | — | IC50 | > | 100000.0 | nM | - |