Assay Detail
Binding
CHEMBL3584585
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Modulation of BCRP (unknown origin) transfected in human HEK293/R2 cells assessed as potentiation of topotecan-induced cytotoxicity measured as topotecan IC50 at 1 uM after 5 days by MTS assay
6
Total Activities
6
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
Potent and Nontoxic Chemosensitizer of P-Glycoprotein-Mediated Multidrug Resistance in Cancer: Synthesis and Evaluation of Methylated Epigallocatechin, Gallocatechin, and Dihydromyricetin Derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.05 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL488910 | — | — | 1 | 7.62 |
| CHEMBL3582168 | — | — | 1 | 7.42 |
| CHEMBL3582167 | — | — | 1 | 7.35 |
| CHEMBL3582155 | — | — | 1 | 6.75 |
| CHEMBL3582156 | — | — | 1 | 6.68 |
| CHEMBL3582149 | — | — | 1 | 6.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL488910 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3582168 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3582167 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3582155 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL3582156 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL3582149 | — | IC50 | = | 357.0 | nM | 6.45 |