Assay Detail
Binding
CHEMBL1053127
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Reversal of MRP1-mediated doxorubicin-resistance in human 2008/MRP1 cells assessed as reduction of doxorubicin IC50 percent by half
7
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | 2008/MRP1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Multidrug resistance-associated protein 1 (CHEMBL3004) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Modulation of multidrug resistance protein 1 (MRP1/ABCC1)-mediated multidrug resistance by bivalent apigenin homodimers and their derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Activity | 6 | - | - |
| EC50 | 1 | 7.14 | 7.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL539987 | — | — | 1 | 7.14 |
| CHEMBL539150 | — | — | 1 | - |
| CHEMBL540167 | — | — | 1 | - |
| CHEMBL541677 | — | — | 1 | - |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | - |
| CHEMBL897 | PROBENECID | 4.0 | 1 | - |
| CHEMBL15177 | MK-571 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL539987 | — | EC50 | = | 73.0 | nM | 7.14 |
| CHEMBL539150 | — | Activity | = | 105.0 | nM | - |
| CHEMBL540167 | — | Activity | = | 133.0 | nM | - |
| CHEMBL541677 | — | Activity | = | 86.0 | nM | - |
| CHEMBL6966 | VERAPAMIL | Activity | = | 2.6 | uM | - |
| CHEMBL897 | PROBENECID | Activity | - | — | - | |
| CHEMBL15177 | MK-571 | Activity | = | 18.0 | uM | - |