Assay Detail
Binding
CHEMBL2050879
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ABCG2-mediated mitoxantrone efflux expressed in HEK293 cells after 48 hrs by flow cytometric analysis
6
Total Activities
6
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
Investigation of chalcones as selective inhibitors of the breast cancer resistance protein: critical role of methoxylation in both inhibition potency and cytotoxicity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.53 | 6.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL404782 | — | — | 1 | 6.77 |
| CHEMBL406837 | — | — | 1 | 6.58 |
| CHEMBL1834565 | — | — | 1 | 6.57 |
| CHEMBL260654 | — | — | 1 | 6.46 |
| CHEMBL1834568 | — | — | 1 | 6.46 |
| CHEMBL1834566 | — | — | 1 | 6.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL404782 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL406837 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL1834565 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL260654 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL1834568 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL1834566 | — | IC50 | = | 450.0 | nM | 6.35 |