Assay Detail
Binding
CHEMBL4196465
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Inhibition of ABCB1 in human A2780adr cells assessed as reduction in calcein AM levels preincubated for 30 mins followed by calcein AM addition measured immediately at 60 sec time interval for 60 mins by fluorescence assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure activity relationships, multidrug resistance reversal and selectivity of heteroarylphenyl ABCG2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 4.98 | 5.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4210844 | — | — | 1 | 5.23 |
| CHEMBL4202709 | — | — | 1 | 5.07 |
| CHEMBL4209777 | — | — | 1 | 4.96 |
| CHEMBL4202725 | — | — | 1 | 4.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4210844 | — | IC50 | = | 5910.0 | nM | 5.23 |
| CHEMBL4202709 | — | IC50 | = | 8550.0 | nM | 5.07 |
| CHEMBL4209777 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4202725 | — | IC50 | = | 21200.0 | nM | 4.67 |