Assay Detail
Binding
CHEMBL5128702
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ABCG2 (unknown origin) expressed in human MCF7/MX cells mediated mitoxantrone efflux assessed as intracellular mitoxantrone level and measured after 30 mins by FACSflow cytometry analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MCF7/MX |
| 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
Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 5.11 | 5.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL941 | IMATINIB | 4.0 | 1 | 5.43 |
| CHEMBL1275655 | — | — | 1 | 5.21 |
| CHEMBL475534 | NITRENDIPINE | 3.0 | 1 | 4.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL941 | IMATINIB | IC50 | = | 3710.0 | nM | 5.43 |
| CHEMBL1275655 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL475534 | NITRENDIPINE | IC50 | = | 21100.0 | nM | 4.68 |