Assay Detail
Binding
CHEMBL2014643
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Inhibition of ABCG2-mediated mitoxantrone efflux in HEK293 cells by flow cytometry
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| 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
Substituted chromones as highly potent nontoxic inhibitors, specific for the breast cancer resistance protein.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.80 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL488910 | — | — | 1 | 7.30 |
| CHEMBL2011288 | — | — | 1 | 6.96 |
| CHEMBL2011290 | — | — | 1 | 6.80 |
| CHEMBL2011282 | — | — | 1 | 6.77 |
| CHEMBL2011287 | — | — | 1 | 6.75 |
| CHEMBL2011289 | — | — | 1 | 6.70 |
| CHEMBL2011286 | — | — | 1 | 6.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL488910 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2011288 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2011290 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2011282 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2011287 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL2011289 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2011286 | — | IC50 | = | 470.0 | nM | 6.33 |