Assay Detail
Binding
CHEMBL892735
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Inhibition of ABCG2 expressed in HEK293 cells assessed as mitoxantrone-mediated efflux by flow cytometry
14
Total Activities
14
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
Acridone derivatives: design, synthesis, and inhibition of breast cancer resistance protein ABCG2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.89 | 6.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL397235 | — | — | 1 | 6.46 |
| CHEMBL396298 | ELACRIDAR | 2.0 | 1 | 6.39 |
| CHEMBL243167 | — | — | 1 | 6.35 |
| CHEMBL243168 | — | — | 1 | 6.25 |
| CHEMBL242513 | — | — | 1 | 6.11 |
| CHEMBL243169 | — | — | 1 | 5.86 |
| CHEMBL388886 | — | — | 1 | 5.32 |
| CHEMBL243813 | — | — | 1 | 5.20 |
| CHEMBL243814 | — | — | 1 | 5.10 |
| CHEMBL242512 | — | — | 1 | - |
| CHEMBL242943 | — | — | 1 | - |
| CHEMBL242942 | — | — | 1 | - |
| CHEMBL242515 | — | — | 1 | - |
| CHEMBL397685 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL397235 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL396298 | ELACRIDAR | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL243167 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL243168 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL242513 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL243169 | — | IC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL388886 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL243813 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL243814 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL242512 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL242943 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL242942 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL242515 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL397685 | — | IC50 | > | 20000.0 | nM | - |