Assay Detail
Binding
CHEMBL2344977
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at BCRP (unknown origin) expressed in MDCK cells using rhodamine 123 as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by fluorometric analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDCK |
| 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 selective tariquidar bioisosters as potential PET radiotracers for imaging P-gp.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 5.81 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL348475 | TARIQUIDAR | 3.0 | 1 | 8.00 |
| CHEMBL2335007 | — | — | 1 | 7.75 |
| CHEMBL2335006 | — | — | 1 | 6.30 |
| CHEMBL2335002 | — | — | 1 | 6.00 |
| CHEMBL2335008 | — | — | 1 | 5.00 |
| CHEMBL260506 | — | — | 1 | 4.82 |
| CHEMBL2335003 | — | — | 1 | 4.52 |
| CHEMBL260599 | — | — | 1 | 4.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL348475 | TARIQUIDAR | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2335007 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2335006 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL2335002 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2335008 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL260506 | — | EC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL2335003 | — | EC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL260599 | — | EC50 | = | 90000.0 | nM | 4.05 |