Assay Detail
ADMET
CHEMBL3867192
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Inhibition of CYP3A4 in human liver microsomes using testosterone as substrate in presence of NADPH by LC-MS/MS analysis
8
Total Activities
8
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
Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.16 | 7.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3127521 | — | — | 1 | 7.05 |
| CHEMBL17289 | CHS-828 | 1.0 | 1 | 6.66 |
| CHEMBL566757 | DAPORINAD | 2.0 | 1 | 5.82 |
| CHEMBL3260358 | — | — | 1 | 5.10 |
| CHEMBL2420629 | — | — | 1 | - |
| CHEMBL2391568 | — | — | 1 | - |
| CHEMBL2419515 | — | — | 1 | - |
| CHEMBL3394738 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3127521 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL17289 | CHS-828 | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL566757 | DAPORINAD | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3260358 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL2420629 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2391568 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2419515 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3394738 | — | IC50 | > | 10000.0 | nM | - |