Assay Detail
Functional
CHEMBL907144
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Inhibition of Pgp measured as inhibition of [3H]vinblastine basolateral to apical transport in Caco-2 cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Caco-2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 4.54 | 5.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL396298 | ELACRIDAR | 2.0 | 1 | 5.70 |
| CHEMBL217886 | — | — | 1 | 4.76 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 4.70 |
| CHEMBL387052 | — | — | 1 | 4.56 |
| CHEMBL214739 | — | — | 1 | 4.03 |
| CHEMBL384538 | — | — | 1 | 4.02 |
| CHEMBL216198 | — | — | 1 | 4.00 |
| CHEMBL215010 | — | — | 1 | - |
| CHEMBL217281 | — | — | 1 | - |
| CHEMBL217425 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL396298 | ELACRIDAR | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL217886 | — | EC50 | = | 17200.0 | nM | 4.76 |
| CHEMBL6966 | VERAPAMIL | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL387052 | — | EC50 | = | 27600.0 | nM | 4.56 |
| CHEMBL214739 | — | EC50 | = | 92800.0 | nM | 4.03 |
| CHEMBL384538 | — | EC50 | = | 95600.0 | nM | 4.02 |
| CHEMBL216198 | — | EC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL215010 | — | EC50 | - | — | - | |
| CHEMBL217281 | — | EC50 | - | — | - | |
| CHEMBL217425 | — | EC50 | = | 125000.0 | nM | - |