Assay Detail
Binding
CHEMBL5128692
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ABCG2 (unknown origin) expressed in human HEK293 cells membrane vesicles assessed inhibition of BCRP- mediated transport of 3[H]-E1S for 1 mins using [3H]-estrone sulfate as substrate by rapid filtration technique
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 | 5 | 5.05 | 5.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1292 | CLOFAZIMINE | 4.0 | 1 | 5.50 |
| CHEMBL561057 | SQ109 | 2.0 | 1 | 5.26 |
| CHEMBL479 | THIORIDAZINE | 4.0 | 1 | 5.18 |
| CHEMBL374478 | RIFAMPIN | 4.0 | 1 | 4.25 |
| CHEMBL2059028 | TIMCODAR | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1292 | CLOFAZIMINE | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL561057 | SQ109 | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL479 | THIORIDAZINE | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL374478 | RIFAMPIN | IC50 | = | 56000.0 | nM | 4.25 |
| CHEMBL2059028 | TIMCODAR | IC50 | > | 100000.0 | nM | - |