Assay Detail
Binding
CHEMBL5128713
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ABCG2 expressing membrane vesicles assessed inhibition of BCRP- mediated transport of [3H]estrone 3-sulfate for 2 mins using [3H]-estrone sulfate 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 |
| 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 | 7.30 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2103830 | FOSTAMATINIB | 4.0 | 1 | 7.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2103830 | FOSTAMATINIB | IC50 | = | 50.0 | nM | 7.30 |