Assay Detail
Binding
CHEMBL5128710
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 membrane vesicles mediated transport of 3[H]-methotrexate for 5 mins using [3H]-methotrexate as substrate by radiometric scintillation analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDCK-II-BCRP |
| Subcellular | Membrane vesicle |
| 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 | 1 | 5.51 | 5.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL461101 | ELTROMBOPAG | 4.0 | 1 | 5.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL461101 | ELTROMBOPAG | IC50 | = | 3100.0 | nM | 5.51 |