Assay Detail
ADMET
CHEMBL5155622
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 6-beta-hydroxy-testosterone formation using testosterone as substrate preincubated for 20 mins in absence of NADPH followed by incubation with substrate for 10 mins by LC-MS/MS analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Tissue | Liver |
| Subcellular | Microsome |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, and characterization of novel aminoalcohol quinolines with strong in vitro antimalarial activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 4.99 | 5.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5183354 | — | — | 1 | 5.54 |
| CHEMBL411329 | (R,S)-MEFLOQUINE | — | 1 | 4.72 |
| CHEMBL172 | (S,R)-MEFLOQUINE | — | 1 | 4.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5183354 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL411329 | (R,S)-MEFLOQUINE | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL172 | (S,R)-MEFLOQUINE | IC50 | = | 19000.0 | nM | 4.72 |