Assay Detail
Binding
CHEMBL921229
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Inhibition of human Pgp mediated [3H]vinblastine transport in human Caco-2 cells
16
Total Activities
16
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
Small P-gp modulating molecules: SAR studies on tetrahydroisoquinoline derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 4.98 | 6.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL53325 | — | — | 1 | 6.26 |
| CHEMBL260599 | — | — | 1 | 5.79 |
| CHEMBL396298 | ELACRIDAR | 2.0 | 1 | 5.70 |
| CHEMBL405448 | — | — | 1 | 5.31 |
| CHEMBL259582 | — | — | 1 | 5.20 |
| CHEMBL259367 | — | — | 1 | 5.09 |
| CHEMBL264424 | — | — | 1 | 5.09 |
| CHEMBL405372 | — | — | 1 | 4.99 |
| CHEMBL408993 | — | — | 1 | 4.82 |
| CHEMBL415560 | — | — | 1 | 4.82 |
| CHEMBL259366 | — | — | 1 | 4.75 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 4.70 |
| CHEMBL261802 | — | — | 1 | 4.50 |
| CHEMBL260499 | — | — | 1 | 4.45 |
| CHEMBL160 | CYCLOSPORINE | 4.0 | 1 | 4.10 |
| CHEMBL260377 | — | — | 1 | 4.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL53325 | — | EC50 | = | 550.0 | nM | 6.26 |
| CHEMBL260599 | — | EC50 | = | 1640.0 | nM | 5.79 |
| CHEMBL396298 | ELACRIDAR | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL405448 | — | EC50 | = | 4860.0 | nM | 5.31 |
| CHEMBL259582 | — | EC50 | = | 6350.0 | nM | 5.20 |
| CHEMBL259367 | — | EC50 | = | 8150.0 | nM | 5.09 |
| CHEMBL264424 | — | EC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL405372 | — | EC50 | = | 10200.0 | nM | 4.99 |
| CHEMBL408993 | — | EC50 | = | 15200.0 | nM | 4.82 |
| CHEMBL415560 | — | EC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL259366 | — | EC50 | = | 17900.0 | nM | 4.75 |
| CHEMBL6966 | VERAPAMIL | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL261802 | — | EC50 | = | 31600.0 | nM | 4.50 |
| CHEMBL260499 | — | EC50 | = | 35500.0 | nM | 4.45 |
| CHEMBL160 | CYCLOSPORINE | EC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL260377 | — | EC50 | = | 83700.0 | nM | 4.08 |