Assay Detail
Binding
CHEMBL974470
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Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A2780 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-activity relationships of new inhibitors of breast cancer resistance protein (ABCG2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 5.69 | 7.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL348475 | TARIQUIDAR | 3.0 | 1 | 7.14 |
| CHEMBL258909 | — | — | 1 | 6.84 |
| CHEMBL444075 | — | — | 1 | 6.78 |
| CHEMBL258882 | — | — | 1 | 6.68 |
| CHEMBL247473 | — | — | 1 | 6.48 |
| CHEMBL428402 | — | — | 1 | 6.45 |
| CHEMBL411951 | — | — | 1 | 6.38 |
| CHEMBL346292 | — | — | 1 | 6.29 |
| CHEMBL258896 | — | — | 1 | 6.28 |
| CHEMBL409234 | — | — | 1 | 6.13 |
| CHEMBL259690 | — | — | 1 | 6.11 |
| CHEMBL260113 | — | — | 1 | 6.11 |
| CHEMBL555611 | — | — | 1 | 5.86 |
| CHEMBL160 | CYCLOSPORINE | 4.0 | 1 | 5.85 |
| CHEMBL518645 | — | — | 1 | 5.85 |
| CHEMBL259976 | — | — | 1 | 5.73 |
| CHEMBL258575 | — | — | 1 | 5.65 |
| CHEMBL261857 | — | — | 1 | 5.61 |
| CHEMBL409480 | — | — | 1 | 5.50 |
| CHEMBL259789 | — | — | 1 | 5.49 |
| CHEMBL772 | RESERPINE | 4.0 | 1 | 5.49 |
| CHEMBL408709 | — | — | 1 | 5.46 |
| CHEMBL410897 | — | — | 1 | 5.38 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 5.34 |
| CHEMBL1484 | NICARDIPINE | 4.0 | 1 | 5.32 |
| CHEMBL471170 | — | — | 1 | 5.32 |
| CHEMBL258574 | — | — | 1 | 5.31 |
| CHEMBL261618 | — | — | 1 | 5.30 |
| CHEMBL260896 | — | — | 1 | 5.27 |
| CHEMBL442464 | — | — | 1 | 5.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL348475 | TARIQUIDAR | IC50 | = | 72.44 | nM | 7.14 |
| CHEMBL258909 | — | IC50 | = | 144.54 | nM | 6.84 |
| CHEMBL444075 | — | IC50 | = | 165.96 | nM | 6.78 |
| CHEMBL258882 | — | IC50 | = | 208.93 | nM | 6.68 |
| CHEMBL247473 | — | IC50 | = | 331.13 | nM | 6.48 |
| CHEMBL428402 | — | IC50 | = | 354.81 | nM | 6.45 |
| CHEMBL411951 | — | IC50 | = | 416.87 | nM | 6.38 |
| CHEMBL346292 | — | IC50 | = | 512.86 | nM | 6.29 |
| CHEMBL258896 | — | IC50 | = | 524.81 | nM | 6.28 |
| CHEMBL409234 | — | IC50 | = | 741.31 | nM | 6.13 |
| CHEMBL259690 | — | IC50 | = | 776.25 | nM | 6.11 |
| CHEMBL260113 | — | IC50 | = | 776.25 | nM | 6.11 |
| CHEMBL555611 | — | IC50 | = | 1380.38 | nM | 5.86 |
| CHEMBL160 | CYCLOSPORINE | IC50 | = | 1412.54 | nM | 5.85 |
| CHEMBL518645 | — | IC50 | = | 1412.54 | nM | 5.85 |
| CHEMBL259976 | — | IC50 | = | 1862.09 | nM | 5.73 |
| CHEMBL258575 | — | IC50 | = | 2238.72 | nM | 5.65 |
| CHEMBL261857 | — | IC50 | = | 2454.71 | nM | 5.61 |
| CHEMBL409480 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL772 | RESERPINE | IC50 | = | 3235.94 | nM | 5.49 |
| CHEMBL259789 | — | IC50 | = | 3235.94 | nM | 5.49 |
| CHEMBL408709 | — | IC50 | = | 3467.37 | nM | 5.46 |
| CHEMBL410897 | — | IC50 | = | 4168.69 | nM | 5.38 |
| CHEMBL6966 | VERAPAMIL | IC50 | = | 4570.88 | nM | 5.34 |
| CHEMBL1484 | NICARDIPINE | IC50 | = | 4786.3 | nM | 5.32 |
| CHEMBL471170 | — | IC50 | = | 4786.3 | nM | 5.32 |
| CHEMBL258574 | — | IC50 | = | 4897.79 | nM | 5.31 |
| CHEMBL261618 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL260896 | — | IC50 | = | 5370.32 | nM | 5.27 |
| CHEMBL442464 | — | IC50 | = | 5495.41 | nM | 5.26 |
| CHEMBL261632 | — | IC50 | = | 7079.46 | nM | 5.15 |
| CHEMBL941 | IMATINIB | IC50 | = | 7244.36 | nM | 5.14 |
| CHEMBL259077 | — | IC50 | = | 9549.93 | nM | 5.02 |
| CHEMBL429515 | — | IC50 | = | 11220.18 | nM | 4.95 |
| CHEMBL258456 | — | IC50 | = | 13489.63 | nM | 4.87 |
| CHEMBL23 | DILTIAZEM | IC50 | = | 42657.95 | nM | 4.37 |
| CHEMBL103 | PROGESTERONE | IC50 | = | 47863.01 | nM | 4.32 |