Assay Detail
Binding
CHEMBL925479
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Inhibition of P-glycoprotein expressed in A2780/ADR cells by calcein AM assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A2780 ADR |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
New functional assay of P-glycoprotein activity using Hoechst 33342.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.48 | 6.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL247473 | — | — | 1 | 6.47 |
| CHEMBL428402 | — | — | 1 | 6.31 |
| CHEMBL248480 | — | — | 1 | 6.09 |
| CHEMBL346292 | — | — | 1 | 6.07 |
| CHEMBL160 | CYCLOSPORINE | 4.0 | 1 | 5.85 |
| CHEMBL772 | RESERPINE | 4.0 | 1 | 5.49 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 5.34 |
| CHEMBL1484 | NICARDIPINE | 4.0 | 1 | 5.32 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 5.14 |
| CHEMBL159 | VINBLASTINE | 4.0 | 1 | 4.98 |
| CHEMBL23 | DILTIAZEM | 4.0 | 1 | 4.37 |
| CHEMBL103 | PROGESTERONE | 4.0 | 1 | 4.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL247473 | — | IC50 | = | 338.84 | nM | 6.47 |
| CHEMBL428402 | — | IC50 | = | 489.78 | nM | 6.31 |
| CHEMBL248480 | — | IC50 | = | 812.83 | nM | 6.09 |
| CHEMBL346292 | — | IC50 | = | 851.14 | nM | 6.07 |
| CHEMBL160 | CYCLOSPORINE | IC50 | = | 1412.54 | nM | 5.85 |
| CHEMBL772 | RESERPINE | IC50 | = | 3235.94 | nM | 5.49 |
| CHEMBL6966 | VERAPAMIL | IC50 | = | 4570.88 | nM | 5.34 |
| CHEMBL1484 | NICARDIPINE | IC50 | = | 4786.3 | nM | 5.32 |
| CHEMBL941 | IMATINIB | IC50 | = | 7244.36 | nM | 5.14 |
| CHEMBL159 | VINBLASTINE | IC50 | = | 10471.29 | nM | 4.98 |
| CHEMBL23 | DILTIAZEM | IC50 | = | 42657.95 | nM | 4.37 |
| CHEMBL103 | PROGESTERONE | IC50 | = | 47863.01 | nM | 4.32 |