Assay Detail
Binding
CHEMBL1047707
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Inhibition of BCRP expressed in MDCK cells by pheophorbide A assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | MDCK |
| 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 | 5.26 | 7.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL488910 | — | — | 1 | 7.13 |
| CHEMBL396298 | ELACRIDAR | 2.0 | 1 | 6.37 |
| CHEMBL594336 | — | — | 1 | 6.30 |
| CHEMBL595493 | — | — | 1 | 6.20 |
| CHEMBL348475 | TARIQUIDAR | 3.0 | 1 | 6.07 |
| CHEMBL247473 | — | — | 1 | 6.07 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 5.90 |
| CHEMBL474972 | — | — | 1 | 5.58 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 5.47 |
| CHEMBL555611 | — | — | 1 | 5.36 |
| CHEMBL595550 | — | — | 1 | 5.16 |
| CHEMBL475554 | — | — | 1 | 5.06 |
| CHEMBL475362 | — | — | 1 | 5.04 |
| CHEMBL429515 | — | — | 1 | 4.68 |
| CHEMBL259077 | — | — | 1 | 4.68 |
| CHEMBL442464 | — | — | 1 | 4.40 |
| CHEMBL258456 | — | — | 1 | 4.34 |
| CHEMBL474757 | — | — | 1 | 4.33 |
| CHEMBL472818 | — | — | 1 | 4.23 |
| CHEMBL472819 | — | — | 1 | 4.13 |
| CHEMBL261632 | — | — | 1 | 4.01 |
| CHEMBL36506 | NOVOBIOCIN | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL488910 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL396298 | ELACRIDAR | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL594336 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL595493 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL348475 | TARIQUIDAR | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL247473 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL939 | GEFITINIB | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL474972 | — | IC50 | = | 2610.0 | nM | 5.58 |
| CHEMBL941 | IMATINIB | IC50 | = | 3380.0 | nM | 5.47 |
| CHEMBL555611 | — | IC50 | = | 4380.0 | nM | 5.36 |
| CHEMBL595550 | — | IC50 | = | 6980.0 | nM | 5.16 |
| CHEMBL475554 | — | IC50 | = | 8710.0 | nM | 5.06 |
| CHEMBL475362 | — | IC50 | = | 9080.0 | nM | 5.04 |
| CHEMBL429515 | — | IC50 | = | 20700.0 | nM | 4.68 |
| CHEMBL259077 | — | IC50 | = | 20900.0 | nM | 4.68 |
| CHEMBL442464 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL258456 | — | IC50 | = | 45700.0 | nM | 4.34 |
| CHEMBL474757 | — | IC50 | = | 46400.0 | nM | 4.33 |
| CHEMBL472818 | — | IC50 | = | 58400.0 | nM | 4.23 |
| CHEMBL472819 | — | IC50 | = | 74100.0 | nM | 4.13 |
| CHEMBL261632 | — | IC50 | = | 98200.0 | nM | 4.01 |
| CHEMBL36506 | NOVOBIOCIN | IC50 | = | 104000.0 | nM | - |