Assay Detail
Binding
CHEMBL974473
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Inhibition of ABCG2 in human mitoxantrone-resistant MCF7 cells by Hoechst 33342 assay
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MCF7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Broad substrate specificity ATP-binding cassette transporter ABCG2 (CHEMBL5393) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-activity relationships of new inhibitors of breast cancer resistance protein (ABCG2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 4.89 | 6.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL488910 | — | — | 1 | 6.51 |
| CHEMBL428402 | — | — | 1 | 6.00 |
| CHEMBL348475 | TARIQUIDAR | 3.0 | 1 | 5.84 |
| CHEMBL247473 | — | — | 1 | 5.68 |
| CHEMBL258896 | — | — | 1 | 5.41 |
| CHEMBL346292 | — | — | 1 | 5.40 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 5.31 |
| CHEMBL411951 | — | — | 1 | 5.30 |
| CHEMBL444075 | — | — | 1 | 5.30 |
| CHEMBL259690 | — | — | 1 | 5.22 |
| CHEMBL258882 | — | — | 1 | 5.22 |
| CHEMBL261618 | — | — | 1 | 5.18 |
| CHEMBL260113 | — | — | 1 | 5.14 |
| CHEMBL555611 | — | — | 1 | 5.12 |
| CHEMBL261857 | — | — | 1 | 4.94 |
| CHEMBL259976 | — | — | 1 | 4.89 |
| CHEMBL409234 | — | — | 1 | 4.84 |
| CHEMBL518645 | — | — | 1 | 4.82 |
| CHEMBL1484 | NICARDIPINE | 4.0 | 1 | 4.78 |
| CHEMBL408709 | — | — | 1 | 4.66 |
| CHEMBL259789 | — | — | 1 | 4.64 |
| CHEMBL258909 | — | — | 1 | 4.62 |
| CHEMBL471170 | — | — | 1 | 4.61 |
| CHEMBL772 | RESERPINE | 4.0 | 1 | 4.58 |
| CHEMBL258575 | — | — | 1 | 4.44 |
| CHEMBL409480 | — | — | 1 | 4.35 |
| CHEMBL260896 | — | — | 1 | 4.32 |
| CHEMBL160 | CYCLOSPORINE | 4.0 | 1 | 4.20 |
| CHEMBL258574 | — | — | 1 | 4.19 |
| CHEMBL36506 | NOVOBIOCIN | 4.0 | 1 | 4.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL488910 | — | IC50 | = | 309.03 | nM | 6.51 |
| CHEMBL428402 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL348475 | TARIQUIDAR | IC50 | = | 1445.44 | nM | 5.84 |
| CHEMBL247473 | — | IC50 | = | 2089.3 | nM | 5.68 |
| CHEMBL258896 | — | IC50 | = | 3890.45 | nM | 5.41 |
| CHEMBL346292 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL941 | IMATINIB | IC50 | = | 4897.79 | nM | 5.31 |
| CHEMBL411951 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL444075 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL259690 | — | IC50 | = | 6025.6 | nM | 5.22 |
| CHEMBL258882 | — | IC50 | = | 6025.6 | nM | 5.22 |
| CHEMBL261618 | — | IC50 | = | 6606.93 | nM | 5.18 |
| CHEMBL260113 | — | IC50 | = | 7244.36 | nM | 5.14 |
| CHEMBL555611 | — | IC50 | = | 7585.78 | nM | 5.12 |
| CHEMBL261857 | — | IC50 | = | 11481.54 | nM | 4.94 |
| CHEMBL259976 | — | IC50 | = | 12882.5 | nM | 4.89 |
| CHEMBL409234 | — | IC50 | = | 14454.4 | nM | 4.84 |
| CHEMBL518645 | — | IC50 | = | 15135.61 | nM | 4.82 |
| CHEMBL1484 | NICARDIPINE | IC50 | = | 16595.87 | nM | 4.78 |
| CHEMBL408709 | — | IC50 | = | 21877.62 | nM | 4.66 |
| CHEMBL259789 | — | IC50 | = | 22908.68 | nM | 4.64 |
| CHEMBL258909 | — | IC50 | = | 23988.33 | nM | 4.62 |
| CHEMBL471170 | — | IC50 | = | 24547.09 | nM | 4.61 |
| CHEMBL772 | RESERPINE | IC50 | = | 26302.68 | nM | 4.58 |
| CHEMBL258575 | — | IC50 | = | 36307.81 | nM | 4.44 |
| CHEMBL409480 | — | IC50 | = | 44668.36 | nM | 4.35 |
| CHEMBL260896 | — | IC50 | = | 47863.01 | nM | 4.32 |
| CHEMBL160 | CYCLOSPORINE | IC50 | = | 63095.73 | nM | 4.20 |
| CHEMBL258574 | — | IC50 | = | 64565.42 | nM | 4.19 |
| CHEMBL36506 | NOVOBIOCIN | IC50 | = | 66069.34 | nM | 4.18 |
| CHEMBL259077 | — | IC50 | = | 74131.02 | nM | 4.13 |
| CHEMBL410897 | — | IC50 | = | 77624.71 | nM | 4.11 |
| CHEMBL258456 | — | IC50 | = | 79432.82 | nM | 4.10 |
| CHEMBL429515 | — | IC50 | = | 85113.8 | nM | 4.07 |
| CHEMBL261632 | — | IC50 | = | 263026.8 | nM | - |
| CHEMBL23 | DILTIAZEM | IC50 | = | 851138.04 | nM | - |
| CHEMBL103 | PROGESTERONE | IC50 | = | 125892.54 | nM | - |
| CHEMBL6966 | VERAPAMIL | IC50 | = | 524807.46 | nM | - |
| CHEMBL442464 | — | IC50 | = | 109647.82 | nM | - |