Assay Detail
Binding
CHEMBL923490
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Inhibition of human P-gp mediated [3H]vinblastine transport activity in human Caco-2 cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Caco-2 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
4-Biphenyl and 2-naphthyl substituted 6,7-dimethoxytetrahydroisoquinoline derivatives as potent P-gp modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 18 | 5.58 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL260505 | — | — | 1 | 7.30 |
| CHEMBL405615 | — | — | 1 | 7.00 |
| CHEMBL406088 | — | — | 1 | 6.52 |
| CHEMBL259095 | — | — | 1 | 6.35 |
| CHEMBL260323 | — | — | 1 | 6.19 |
| CHEMBL259094 | — | — | 1 | 6.10 |
| CHEMBL260599 | — | — | 1 | 5.79 |
| CHEMBL396298 | ELACRIDAR | 2.0 | 1 | 5.70 |
| CHEMBL260508 | — | — | 1 | 5.46 |
| CHEMBL259370 | — | — | 1 | 5.19 |
| CHEMBL259791 | — | — | 1 | 4.82 |
| CHEMBL260321 | — | — | 1 | 4.75 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 4.70 |
| CHEMBL259949 | — | — | 1 | 4.70 |
| CHEMBL438729 | — | — | 1 | 4.55 |
| CHEMBL160 | CYCLOSPORINE | 4.0 | 1 | 4.10 |
| CHEMBL260507 | — | — | 1 | - |
| CHEMBL260506 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL260505 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL405615 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL406088 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL259095 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL260323 | — | EC50 | = | 650.0 | nM | 6.19 |
| CHEMBL259094 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL260599 | — | EC50 | = | 1640.0 | nM | 5.79 |
| CHEMBL396298 | ELACRIDAR | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL260508 | — | EC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL259370 | — | EC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL259791 | — | EC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL260321 | — | EC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL6966 | VERAPAMIL | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL259949 | — | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL438729 | — | EC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL160 | CYCLOSPORINE | EC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL260507 | — | EC50 | - | — | - | |
| CHEMBL260506 | — | EC50 | - | — | - |