Assay Detail
ADMET
CHEMBL4189503
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Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 5 mins followed by NADPH addition measured after 5 mins by LC-MS/MS analysis
9
Total Activities
9
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
Optimization of Selective Mitogen-Activated Protein Kinase Interacting Kinases 1 and 2 Inhibitors for the Treatment of Blast Crisis Leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.33 | 5.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4204438 | — | — | 1 | 5.41 |
| CHEMBL4208772 | — | — | 1 | 5.25 |
| CHEMBL4211649 | TINODASERTIB | 2.0 | 1 | - |
| CHEMBL4203889 | — | — | 1 | - |
| CHEMBL4213168 | — | — | 1 | - |
| CHEMBL4208246 | — | — | 1 | - |
| CHEMBL4213819 | — | — | 1 | - |
| CHEMBL4216991 | — | — | 1 | - |
| CHEMBL4212480 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4204438 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4208772 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL4211649 | TINODASERTIB | IC50 | > | 20000.0 | nM | - |
| CHEMBL4203889 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4213168 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4208246 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4213819 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4216991 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4212480 | — | IC50 | > | 20000.0 | nM | - |