Assay Detail
Binding
CHEMBL4478439
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Inhibition of human ABCG2 expressed in baculovirus infected Sf9 cell membrane assessed as inhibition of vanadate sensitive quercetin-stimulated ATPase activity after 20 mins by colorimetric method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| 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
Synthesis and Investigation of Tetrahydro-β-carboline Derivatives as Inhibitors of the Breast Cancer Resistance Protein (ABCG2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.47 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL488910 | — | — | 1 | 7.55 |
| CHEMBL4483061 | — | — | 1 | 6.58 |
| CHEMBL4568473 | — | — | 1 | 6.58 |
| CHEMBL4534001 | — | — | 1 | 6.54 |
| CHEMBL4536788 | — | — | 1 | 6.52 |
| CHEMBL4517488 | — | — | 1 | 6.25 |
| CHEMBL4575180 | — | — | 1 | 6.06 |
| CHEMBL4581843 | — | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL488910 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4483061 | — | IC50 | = | 262.0 | nM | 6.58 |
| CHEMBL4568473 | — | IC50 | = | 262.0 | nM | 6.58 |
| CHEMBL4534001 | — | IC50 | = | 285.0 | nM | 6.54 |
| CHEMBL4536788 | — | IC50 | = | 299.0 | nM | 6.52 |
| CHEMBL4517488 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL4575180 | — | IC50 | = | 863.0 | nM | 6.06 |
| CHEMBL4581843 | — | IC50 | = | 2020.0 | nM | 5.70 |