Assay Detail
Binding
CHEMBL1687396
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MDR1 expressed in MDCK cells using rhodamine 123 staining by flow cytometry
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | MDCK |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Structure-activity relationships of flavonoids as inhibitors of breast cancer resistance protein (BCRP).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 4.93 | 6.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL348475 | TARIQUIDAR | 3.0 | 1 | 6.68 |
| CHEMBL1685073 | — | — | 1 | 5.85 |
| CHEMBL1685072 | NEOCALYCOPTERON | — | 1 | 5.10 |
| CHEMBL1685074 | CALYFLORENON B | — | 1 | 5.10 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 5.01 |
| CHEMBL74898 | AYANIN | — | 1 | 4.89 |
| CHEMBL165509 | PENDULETIN | — | 1 | 4.85 |
| CHEMBL1685068 | DIMETHYLCRYPTOSTROBIN | — | 1 | 4.82 |
| CHEMBL137586 | 6-METHOXYFLAVONE | — | 1 | 4.82 |
| CHEMBL77966 | RETUSIN | — | 1 | 4.80 |
| CHEMBL1685069 | Strobochrysin-dimethylether | — | 1 | 4.72 |
| CHEMBL1685067 | STROBOPININ-7-METHYLETHER | — | 1 | 4.54 |
| CHEMBL226507 | SINENSETIN | — | 1 | 4.54 |
| CHEMBL77993 | 3,5,6,7,8,3',4'-HEPTAMETHOXYFLAVONE | — | 1 | 4.51 |
| CHEMBL73930 | TANGERETIN | — | 1 | 4.41 |
| CHEMBL476292 | — | — | 1 | 4.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL348475 | TARIQUIDAR | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL1685073 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL1685072 | NEOCALYCOPTERON | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL1685074 | CALYFLORENON B | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL6966 | VERAPAMIL | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL74898 | AYANIN | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL165509 | PENDULETIN | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL1685068 | DIMETHYLCRYPTOSTROBIN | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL137586 | 6-METHOXYFLAVONE | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL77966 | RETUSIN | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL1685069 | Strobochrysin-dimethylether | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL1685067 | STROBOPININ-7-METHYLETHER | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL226507 | SINENSETIN | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL77993 | 3,5,6,7,8,3',4'-HEPTAMETHOXYFLAVONE | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL73930 | TANGERETIN | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL476292 | — | IC50 | = | 64000.0 | nM | 4.19 |