Assay Detail
Binding
CHEMBL4328827
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ABCB1 in human A2780/ADR cells assessed as calcein-AM accumulation preincubated for 30 mins followed by calcein-AM addition measured over 60 mins at 60 secs time interval by fluorescence assay
6
Total Activities
6
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
Synthesis and biological evaluation of quinazoline derivatives - A SAR study of novel inhibitors of ABCG2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.34 | 5.93 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL160 | CYCLOSPORINE | 4.0 | 1 | 5.93 |
| CHEMBL4475108 | — | — | 1 | 5.74 |
| CHEMBL4446794 | — | — | 1 | 5.73 |
| CHEMBL4448170 | — | — | 1 | 5.09 |
| CHEMBL1307612 | — | — | 1 | 4.83 |
| CHEMBL4469532 | — | — | 1 | 4.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL160 | CYCLOSPORINE | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL4475108 | — | IC50 | = | 1810.0 | nM | 5.74 |
| CHEMBL4446794 | — | IC50 | = | 1880.0 | nM | 5.73 |
| CHEMBL4448170 | — | IC50 | = | 8030.0 | nM | 5.09 |
| CHEMBL1307612 | — | IC50 | = | 14700.0 | nM | 4.83 |
| CHEMBL4469532 | — | IC50 | = | 18800.0 | nM | 4.73 |