Assay Detail
ADMET
CHEMBL4346904
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CYP3A4 in human liver microsomes assessed as reduction in metabolite formation using midazolam as substrate incubated for 10 mins in presence of NADPH by HPLC based mass spectrometric method
5
Total Activities
5
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
Design, synthesis and structure-activity relationships of novel macrolones: Hybrids of 2-fluoro 9-oxime ketolides and carbamoyl quinolones with highly improved activity against resistant pathogens.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.48 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL157101 | KETOCONAZOLE | 4.0 | 1 | 7.22 |
| CHEMBL4459487 | — | — | 1 | 5.29 |
| CHEMBL4537107 | — | — | 1 | 5.13 |
| CHEMBL1136 | TELITHROMYCIN | 4.0 | 1 | 4.93 |
| CHEMBL4466824 | — | — | 1 | 4.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL157101 | KETOCONAZOLE | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4459487 | — | IC50 | = | 5140.0 | nM | 5.29 |
| CHEMBL4537107 | — | IC50 | = | 7320.0 | nM | 5.13 |
| CHEMBL1136 | TELITHROMYCIN | IC50 | = | 11800.0 | nM | 4.93 |
| CHEMBL4466824 | — | IC50 | = | 14900.0 | nM | 4.83 |