Assay Detail
Binding
CHEMBL5128685
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ABCG2 expressed in dog MDCK-II-BCRP cells mediated pheophorbide A efflux and measured after 60 mins using pheophorbide A as fluorescent substrate by flow cytometry
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDCK-II-BCRP |
| 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 | 2 | 5.04 | 5.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1014 | CANDESARTAN CILEXETIL | 4.0 | 1 | 5.30 |
| CHEMBL1017 | TELMISARTAN | 4.0 | 1 | 4.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1014 | CANDESARTAN CILEXETIL | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL1017 | TELMISARTAN | IC50 | = | 16900.0 | nM | 4.77 |