Assay Detail
Binding
CHEMBL1047706
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Inhibition of BCRP expressed in MCF7 MX cells by Hoechst 33342 staining
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | MCF7 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Broad substrate specificity ATP-binding cassette transporter ABCG2 (CHEMBL5393) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel lead for potent inhibitors of breast cancer resistance protein (BCRP).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 5.24 | 6.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL488910 | — | — | 1 | 6.64 |
| CHEMBL396298 | ELACRIDAR | 2.0 | 1 | 6.40 |
| CHEMBL594336 | — | — | 1 | 6.27 |
| CHEMBL348475 | TARIQUIDAR | 3.0 | 1 | 6.17 |
| CHEMBL595493 | — | — | 1 | 6.16 |
| CHEMBL247473 | — | — | 1 | 6.03 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 5.96 |
| CHEMBL474972 | — | — | 1 | 5.41 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 5.39 |
| CHEMBL475554 | — | — | 1 | 5.17 |
| CHEMBL555611 | — | — | 1 | 5.16 |
| CHEMBL475362 | — | — | 1 | 4.99 |
| CHEMBL595550 | — | — | 1 | 4.99 |
| CHEMBL259077 | — | — | 1 | 4.75 |
| CHEMBL429515 | — | — | 1 | 4.49 |
| CHEMBL258456 | — | — | 1 | 4.29 |
| CHEMBL472818 | — | — | 1 | 4.18 |
| CHEMBL474757 | — | — | 1 | 4.13 |
| CHEMBL442464 | — | — | 1 | 4.11 |
| CHEMBL36506 | NOVOBIOCIN | 4.0 | 1 | 4.07 |
| CHEMBL261632 | — | — | 1 | - |
| CHEMBL472819 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL488910 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL396298 | ELACRIDAR | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL594336 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL348475 | TARIQUIDAR | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL595493 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL247473 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL939 | GEFITINIB | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL474972 | — | IC50 | = | 3890.0 | nM | 5.41 |
| CHEMBL941 | IMATINIB | IC50 | = | 4070.0 | nM | 5.39 |
| CHEMBL475554 | — | IC50 | = | 6760.0 | nM | 5.17 |
| CHEMBL555611 | — | IC50 | = | 6920.0 | nM | 5.16 |
| CHEMBL475362 | — | IC50 | = | 10200.0 | nM | 4.99 |
| CHEMBL595550 | — | IC50 | = | 10200.0 | nM | 4.99 |
| CHEMBL259077 | — | IC50 | = | 17800.0 | nM | 4.75 |
| CHEMBL429515 | — | IC50 | = | 32400.0 | nM | 4.49 |
| CHEMBL258456 | — | IC50 | = | 51300.0 | nM | 4.29 |
| CHEMBL472818 | — | IC50 | = | 66100.0 | nM | 4.18 |
| CHEMBL474757 | — | IC50 | = | 74100.0 | nM | 4.13 |
| CHEMBL442464 | — | IC50 | = | 77600.0 | nM | 4.11 |
| CHEMBL36506 | NOVOBIOCIN | IC50 | = | 85100.0 | nM | 4.07 |
| CHEMBL261632 | — | IC50 | = | 219000.0 | nM | - |
| CHEMBL472819 | — | IC50 | = | 102000.0 | nM | - |