Assay Detail
Binding
CHEMBL5035553
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BCRP in HEK293/R2 cells assessed as reversal of topotecan resistance by measuring topotecan IC50 at 1 uM after 5 days by Cell Titer-Glo luminescence assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293/R2 |
| 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 evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 7.17 | 7.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5089855 | — | — | 1 | 7.34 |
| CHEMBL5088809 | — | — | 1 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5089855 | — | IC50 | = | 45.5 | nM | 7.34 |
| CHEMBL5088809 | — | IC50 | = | 100.8 | nM | 7.00 |