Assay Detail
Binding
CHEMBL4423277
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ABCB1 in human A2780/ADR cells preincubated for 30 mins followed by calcein AM addition and measured every 60 secs for 1 hr by fluorescence assay
16
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel chalcone and flavone derivatives as selective and dual inhibitors of the transport proteins ABCB1 and ABCG2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 5.41 | 5.85 |
| Imax | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4474709 | — | — | 2 | 5.85 |
| CHEMBL4462468 | — | — | 1 | 5.72 |
| CHEMBL4470070 | — | — | 1 | 5.30 |
| CHEMBL4540332 | — | — | 1 | 5.26 |
| CHEMBL4210110 | — | — | 1 | 4.93 |
| CHEMBL4524909 | — | — | 1 | - |
| CHEMBL4528836 | — | — | 1 | - |
| CHEMBL4567676 | — | — | 1 | - |
| CHEMBL4451229 | — | — | 1 | - |
| CHEMBL4583169 | — | — | 1 | - |
| CHEMBL4205213 | — | — | 1 | - |
| CHEMBL4555106 | — | — | 1 | - |
| CHEMBL4463976 | — | — | 1 | - |
| CHEMBL4583488 | — | — | 1 | - |
| CHEMBL4440031 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4474709 | — | IC50 | = | 1410.0 | nM | 5.85 |
| CHEMBL4462468 | — | IC50 | = | 1890.0 | nM | 5.72 |
| CHEMBL4470070 | — | IC50 | = | 5010.0 | nM | 5.30 |
| CHEMBL4540332 | — | IC50 | = | 5430.0 | nM | 5.26 |
| CHEMBL4210110 | — | IC50 | = | 11700.0 | nM | 4.93 |
| CHEMBL4524909 | — | IC50 | - | — | - | |
| CHEMBL4474709 | — | Imax | = | 51.0 | % | - |
| CHEMBL4528836 | — | IC50 | - | — | - | |
| CHEMBL4567676 | — | IC50 | - | — | - | |
| CHEMBL4451229 | — | IC50 | - | — | - | |
| CHEMBL4583169 | — | IC50 | - | — | - | |
| CHEMBL4205213 | — | IC50 | - | — | - | |
| CHEMBL4555106 | — | IC50 | - | — | - | |
| CHEMBL4463976 | — | IC50 | - | — | - | |
| CHEMBL4583488 | — | IC50 | - | — | - | |
| CHEMBL4440031 | — | IC50 | - | — | - |