Assay Detail
Binding
CHEMBL5128686
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ABCG2 (unknown origin) expressed in human HEK293-A cells membrane vesicles assessed inhibition of ABCG2-mediated urate transport activity by rapid filtration technique
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293-A |
| 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 | 7 | 5.95 | 7.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1164729 | FEBUXOSTAT | 4.0 | 1 | 7.57 |
| CHEMBL1078685 | TOPIROXOSTAT | 2.0 | 1 | 6.75 |
| CHEMBL388590 | BENZBROMARONE | 4.0 | 1 | 6.70 |
| CHEMBL35 | FUROSEMIDE | 4.0 | 1 | 5.50 |
| CHEMBL1487 | ATORVASTATIN | 4.0 | 1 | 5.37 |
| CHEMBL672 | FENOFIBRATE | 4.0 | 1 | 5.29 |
| CHEMBL191 | LOSARTAN | 4.0 | 1 | 4.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1164729 | FEBUXOSTAT | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1078685 | TOPIROXOSTAT | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL388590 | BENZBROMARONE | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL35 | FUROSEMIDE | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL1487 | ATORVASTATIN | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL672 | FENOFIBRATE | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL191 | LOSARTAN | IC50 | = | 35000.0 | nM | 4.46 |