Assay Detail
Binding
CHEMBL3240718
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ABCG2 (unknown origin) transfected in HEK293 cells assessed as inhibition of mitoxantrone efflux after 30 mins by flow cytometry relative to control
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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
Symmetric bis-chalcones as a new type of breast cancer resistance protein inhibitors with a mechanism different from that of chromones.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 6.22 | 7.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL488910 | — | — | 1 | 7.54 |
| CHEMBL2011288 | — | — | 1 | 7.03 |
| CHEMBL3238330 | — | — | 1 | 6.70 |
| CHEMBL3238323 | — | — | 1 | 6.52 |
| CHEMBL3238325 | — | — | 1 | 6.40 |
| CHEMBL3238340 | — | — | 1 | 6.30 |
| CHEMBL3238320 | — | — | 1 | 6.16 |
| CHEMBL3238335 | — | — | 1 | 6.10 |
| CHEMBL3238336 | — | — | 1 | 6.05 |
| CHEMBL3238333 | — | — | 1 | 5.96 |
| CHEMBL3238343 | — | — | 1 | 5.96 |
| CHEMBL3238338 | — | — | 1 | 5.89 |
| CHEMBL3238331 | — | — | 1 | 5.85 |
| CHEMBL3238346 | — | — | 1 | 5.75 |
| CHEMBL1504035 | — | — | 1 | 5.68 |
| CHEMBL3238334 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL488910 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2011288 | — | EC50 | = | 94.0 | nM | 7.03 |
| CHEMBL3238330 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3238323 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3238325 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3238340 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3238320 | — | EC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3238335 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3238336 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3238333 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3238343 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3238338 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3238331 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3238346 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL1504035 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3238334 | — | EC50 | = | 2300.0 | nM | 5.64 |