Assay Detail
Binding
CHEMBL4015704
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human GFP-fused ABCG2 expressed in MDCK2 cells assessed as potentiation of SN-38 induced cytotoxicity by measuring cell viability after 72 hrs by MTT assay
3
Total Activities
3
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
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 |
|---|---|---|---|
| EC50 | 3 | 7.32 | 7.67 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4075328 | — | — | 1 | 7.67 |
| CHEMBL4088963 | — | — | 1 | 7.21 |
| CHEMBL4089579 | — | — | 1 | 7.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4075328 | — | EC50 | = | 21.2 | nM | 7.67 |
| CHEMBL4088963 | — | EC50 | = | 62.3 | nM | 7.21 |
| CHEMBL4089579 | — | EC50 | = | 85.0 | nM | 7.07 |