Assay Detail
Binding
CHEMBL4015697
Review assay metadata, readout intent, target linkage, and publication context from the same page.
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
11
Total Activities
11
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
4-Anilino-2-pyridylquinazolines and -pyrimidines as Highly Potent and Nontoxic Inhibitors of Breast Cancer Resistance Protein (ABCG2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 5.50 | 6.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4099533 | — | — | 1 | 6.48 |
| CHEMBL160 | CYCLOSPORINE | 4.0 | 1 | 5.92 |
| CHEMBL4082355 | — | — | 1 | 5.68 |
| CHEMBL4060577 | — | — | 1 | 5.56 |
| CHEMBL4100665 | — | — | 1 | 5.51 |
| CHEMBL3770841 | — | — | 1 | 5.43 |
| CHEMBL4071162 | — | — | 1 | 5.32 |
| CHEMBL4090505 | — | — | 1 | 5.26 |
| CHEMBL4082677 | — | — | 1 | 5.20 |
| CHEMBL1445052 | — | — | 1 | 5.20 |
| CHEMBL4098216 | — | — | 1 | 4.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4099533 | — | IC50 | = | 334.0 | nM | 6.48 |
| CHEMBL160 | CYCLOSPORINE | IC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL4082355 | — | IC50 | = | 2080.0 | nM | 5.68 |
| CHEMBL4060577 | — | IC50 | = | 2780.0 | nM | 5.56 |
| CHEMBL4100665 | — | IC50 | = | 3110.0 | nM | 5.51 |
| CHEMBL3770841 | — | IC50 | = | 3670.0 | nM | 5.43 |
| CHEMBL4071162 | — | IC50 | = | 4780.0 | nM | 5.32 |
| CHEMBL4090505 | — | IC50 | = | 5430.0 | nM | 5.26 |
| CHEMBL4082677 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL1445052 | — | IC50 | = | 6370.0 | nM | 5.20 |
| CHEMBL4098216 | — | IC50 | = | 12700.0 | nM | 4.90 |