Assay Detail
Binding
CHEMBL4708434
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Inhibition of ABCG2 (unknown origin) in HEK293 cells assessed as maximal inhibition of mitoxantrone efflux by fluorescence based flow cytometry
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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
Chromones bearing amino acid residues: Easily accessible and potent inhibitors of the breast cancer resistance protein ABCG2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 6.66 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4754283 | — | — | 1 | 7.30 |
| CHEMBL4798617 | — | — | 1 | 7.16 |
| CHEMBL4743102 | — | — | 1 | 7.16 |
| CHEMBL488910 | — | — | 1 | 7.05 |
| CHEMBL4786687 | — | — | 1 | 7.00 |
| CHEMBL4793491 | — | — | 1 | 7.00 |
| CHEMBL4751998 | — | — | 1 | 6.96 |
| CHEMBL2011288 | — | — | 1 | 6.89 |
| CHEMBL4763093 | — | — | 1 | 6.85 |
| CHEMBL4791750 | — | — | 1 | 6.60 |
| CHEMBL4797201 | — | — | 1 | 6.57 |
| CHEMBL4779178 | — | — | 1 | 6.32 |
| CHEMBL4795949 | — | — | 1 | 6.23 |
| CHEMBL4797214 | — | — | 1 | 6.22 |
| CHEMBL4777166 | — | — | 1 | 4.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4754283 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4798617 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4743102 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL488910 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4786687 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4793491 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4751998 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2011288 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4763093 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4791750 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4797201 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4779178 | — | EC50 | = | 480.0 | nM | 6.32 |
| CHEMBL4795949 | — | EC50 | = | 590.0 | nM | 6.23 |
| CHEMBL4797214 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4777166 | — | EC50 | = | 29000.0 | nM | 4.54 |