Assay Detail
Binding
CHEMBL975399
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Inhibition of human MRP2 expressed in dog MDCK2 cells
8
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDCK-II |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
ATP-binding cassette sub-family C member 2 (CHEMBL5748) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
A 4-aminobenzoic acid derivative as novel lead for selective inhibitors of multidrug resistance-associated proteins.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 4.74 | 4.87 |
| Activity | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL160 | CYCLOSPORINE | 4.0 | 1 | 4.87 |
| CHEMBL89768 | — | — | 1 | 4.68 |
| CHEMBL510556 | — | — | 1 | 4.67 |
| CHEMBL452241 | — | — | 1 | - |
| CHEMBL452313 | — | — | 1 | - |
| CHEMBL6 | INDOMETHACIN | 4.0 | 1 | - |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | - |
| CHEMBL452312 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL160 | CYCLOSPORINE | IC50 | = | 13600.0 | nM | 4.87 |
| CHEMBL89768 | — | IC50 | = | 20700.0 | nM | 4.68 |
| CHEMBL510556 | — | IC50 | = | 21500.0 | nM | 4.67 |
| CHEMBL452241 | — | Activity | - | — | - | |
| CHEMBL452313 | — | Activity | - | — | - | |
| CHEMBL6 | INDOMETHACIN | IC50 | = | 235000.0 | nM | - |
| CHEMBL6966 | VERAPAMIL | IC50 | > | 200000.0 | nM | - |
| CHEMBL452312 | — | IC50 | > | 200000.0 | nM | - |