Assay Detail
Binding
CHEMBL4819608
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Mixed inhibition of human ABCG2 transfected in human HEK293 cells assessed as Ki2 for inhibition of mitoxantrone efflux measured after 30 mins by FACS Calibur cytometric analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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
Uncompetitive nanomolar dimeric indenoindole inhibitors of the human breast cancer resistance pump ABCG2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 6.66 | 7.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4876781 | — | — | 1 | 7.38 |
| CHEMBL4875810 | — | — | 1 | 6.53 |
| CHEMBL3353414 | — | — | 1 | 6.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4876781 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL4875810 | — | Ki | = | 294.0 | nM | 6.53 |
| CHEMBL3353414 | — | Ki | = | 843.0 | nM | 6.07 |