Assay Detail
Binding
CHEMBL4048737
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ABCG2 in human PLB-985 cells assessed as increase in accumulation of Hoechst 33342 preincubated for 30 mins followed by Hoechst 33342 addition measured every 60 secs for 120 mins by fluorescence 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
New Inhibitors of Breast Cancer Resistance Protein (ABCG2) Containing a 2,4-Disubstituted Pyridopyrimidine Scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.41 | 6.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4072482 | — | — | 1 | 6.66 |
| CHEMBL488910 | — | — | 1 | 6.63 |
| CHEMBL4066611 | — | — | 1 | 5.93 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4072482 | — | IC50 | = | 219.0 | nM | 6.66 |
| CHEMBL488910 | — | IC50 | = | 233.0 | nM | 6.63 |
| CHEMBL4066611 | — | IC50 | = | 1185.0 | nM | 5.93 |