Assay Detail
ADMET
CHEMBL4180122
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Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins 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
Discovery of aminocyclohexene analogues as selective and orally bioavailable hNav1.7 inhibitors for analgesia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 4.72 | 5.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4204264 | — | — | 1 | 5.29 |
| CHEMBL4212007 | — | — | 1 | 4.78 |
| CHEMBL4216985 | — | — | 1 | 4.67 |
| CHEMBL4210866 | — | — | 1 | 4.48 |
| CHEMBL4203948 | — | — | 1 | 4.36 |
| CHEMBL4076061 | — | — | 1 | - |
| CHEMBL4206499 | — | — | 1 | - |
| CHEMBL4209130 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4204264 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL4212007 | — | IC50 | = | 16500.0 | nM | 4.78 |
| CHEMBL4216985 | — | IC50 | = | 21600.0 | nM | 4.67 |
| CHEMBL4210866 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL4203948 | — | IC50 | = | 43400.0 | nM | 4.36 |
| CHEMBL4076061 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4206499 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4209130 | — | IC50 | > | 50000.0 | nM | - |