Assay Detail
Binding
CHEMBL4132963
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ABCC1 in human H69AR cells assessed as reduction in calcein-AM efflux preincubated for 30 mins followed by calcein-AM addition measured at 60 secs interval for 60 mins by fluorescence assay
10
Total Activities
10
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 |
Target
Multidrug resistance-associated protein 1 (CHEMBL3004) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological investigation of 2,4-substituted quinazolines as highly potent inhibitors of breast cancer resistance protein (ABCG2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 4.83 | 5.45 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL160 | CYCLOSPORINE | 4.0 | 1 | 5.45 |
| CHEMBL4159635 | — | — | 1 | 5.11 |
| CHEMBL3092486 | — | — | 1 | 4.39 |
| CHEMBL4160529 | — | — | 1 | 4.36 |
| CHEMBL4172917 | — | — | 1 | - |
| CHEMBL4161421 | — | — | 1 | - |
| CHEMBL4171304 | — | — | 1 | - |
| CHEMBL4163917 | — | — | 1 | - |
| CHEMBL4171781 | — | — | 1 | - |
| CHEMBL4161988 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL160 | CYCLOSPORINE | IC50 | = | 3530.0 | nM | 5.45 |
| CHEMBL4159635 | — | IC50 | = | 7720.0 | nM | 5.11 |
| CHEMBL3092486 | — | IC50 | = | 40600.0 | nM | 4.39 |
| CHEMBL4160529 | — | IC50 | = | 44200.0 | nM | 4.36 |
| CHEMBL4172917 | — | IC50 | - | — | - | |
| CHEMBL4161421 | — | IC50 | - | — | - | |
| CHEMBL4171304 | — | IC50 | - | — | - | |
| CHEMBL4163917 | — | IC50 | - | — | - | |
| CHEMBL4171781 | — | IC50 | - | — | - | |
| CHEMBL4161988 | — | IC50 | - | — | - |