Assay Detail
Binding
CHEMBL4825988
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of P-gp (unknown origin) expressed in MES-SA/DX5 cells assessed as cell growth inhibition after 3 days in presence of 200 nM paclitaxel by MTT assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MES-SA/Dx5 |
| 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 |
|---|---|---|---|
| EC50 | 3 | 7.60 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4594298 | ENCEQUIDAR | 3.0 | 1 | 7.89 |
| CHEMBL348475 | TARIQUIDAR | 3.0 | 1 | 7.80 |
| CHEMBL4873470 | — | — | 1 | 7.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4594298 | ENCEQUIDAR | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL348475 | TARIQUIDAR | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4873470 | — | EC50 | = | 75.0 | nM | 7.12 |