Assay Detail
Binding
CHEMBL4425525
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of c-terminal GFP-tagged human ABCG2 expressed in MDCK2 cells preincubated for 30 mins before Hoechst 33342 addition by Hoechst 33342 accumulation assay
30
Total Activities
30
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
Broad substrate specificity ATP-binding cassette transporter ABCG2 (CHEMBL5393) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and Biological Evaluation of 4-Anilino-quinazolines and -quinolines as Inhibitors of Breast Cancer Resistance Protein (ABCG2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.14 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4088022 | — | — | 1 | 7.16 |
| CHEMBL4069582 | — | — | 1 | 7.10 |
| CHEMBL2158554 | — | — | 1 | 6.82 |
| CHEMBL1410991 | — | — | 1 | 6.69 |
| CHEMBL488910 | — | — | 1 | 6.66 |
| CHEMBL1307877 | — | — | 1 | 6.56 |
| CHEMBL4558657 | — | — | 1 | 6.54 |
| CHEMBL4085567 | — | — | 1 | 6.45 |
| CHEMBL4528016 | — | — | 1 | 6.25 |
| CHEMBL4458057 | — | — | 1 | 6.21 |
| CHEMBL4453876 | — | — | 1 | 6.17 |
| CHEMBL428402 | — | — | 1 | 6.15 |
| CHEMBL4441055 | — | — | 1 | 6.10 |
| CHEMBL118538 | — | — | 1 | 6.08 |
| CHEMBL4530796 | — | — | 1 | 6.07 |
| CHEMBL4446671 | — | — | 1 | 6.06 |
| CHEMBL120099 | — | — | 1 | 6.03 |
| CHEMBL4455303 | — | — | 1 | 6.02 |
| CHEMBL4458072 | — | — | 1 | 5.97 |
| CHEMBL4578761 | — | — | 1 | 5.97 |
| CHEMBL4564993 | — | — | 1 | 5.97 |
| CHEMBL1474597 | — | — | 1 | 5.94 |
| CHEMBL4447490 | — | — | 1 | 5.92 |
| CHEMBL4513952 | — | — | 1 | 5.84 |
| CHEMBL1534709 | — | — | 1 | 5.83 |
| CHEMBL4437626 | — | — | 1 | 5.79 |
| CHEMBL4462578 | — | — | 1 | 5.72 |
| CHEMBL4441537 | — | — | 1 | 5.67 |
| CHEMBL4475288 | — | — | 1 | 5.25 |
| CHEMBL1624741 | — | — | 1 | 5.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4088022 | — | IC50 | = | 69.9 | nM | 7.16 |
| CHEMBL4069582 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2158554 | — | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL1410991 | — | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL488910 | — | IC50 | = | 221.0 | nM | 6.66 |
| CHEMBL1307877 | — | IC50 | = | 278.0 | nM | 6.56 |
| CHEMBL4558657 | — | IC50 | = | 289.0 | nM | 6.54 |
| CHEMBL4085567 | — | IC50 | = | 355.0 | nM | 6.45 |
| CHEMBL4528016 | — | IC50 | = | 556.0 | nM | 6.25 |
| CHEMBL4458057 | — | IC50 | = | 612.0 | nM | 6.21 |
| CHEMBL4453876 | — | IC50 | = | 672.0 | nM | 6.17 |
| CHEMBL428402 | — | IC50 | = | 704.0 | nM | 6.15 |
| CHEMBL4441055 | — | IC50 | = | 791.0 | nM | 6.10 |
| CHEMBL118538 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL4530796 | — | IC50 | = | 846.0 | nM | 6.07 |
| CHEMBL4446671 | — | IC50 | = | 872.0 | nM | 6.06 |
| CHEMBL120099 | — | IC50 | = | 944.0 | nM | 6.03 |
| CHEMBL4455303 | — | IC50 | = | 951.0 | nM | 6.02 |
| CHEMBL4458072 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL4578761 | — | IC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL4564993 | — | IC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL1474597 | — | IC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL4447490 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL4513952 | — | IC50 | = | 1460.0 | nM | 5.84 |
| CHEMBL1534709 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL4437626 | — | IC50 | = | 1630.0 | nM | 5.79 |
| CHEMBL4462578 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4441537 | — | IC50 | = | 2130.0 | nM | 5.67 |
| CHEMBL4475288 | — | IC50 | = | 5650.0 | nM | 5.25 |
| CHEMBL1624741 | — | IC50 | = | 6380.0 | nM | 5.20 |