Assay Detail
Binding
CHEMBL4826012
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of P-gp in human Caco-2 cells assessed as reduction in paclitaxel efflux pre-incubated for 30 mins and measured after 120 mins by LC-MS/MS analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Caco-2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Encequidar, First-in-Class Intestine Specific P-glycoprotein Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 1 | 7.28 | 7.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4594298 | ENCEQUIDAR | 3.0 | 1 | 7.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4594298 | ENCEQUIDAR | IC50 | = | 53.0 | nM | 7.28 |