Assay Detail
Binding
CHEMBL2344978
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Activity at MDR1 (unknown origin) expressed in MDCK cells using calcein AM as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by fluorometric analysis
10
Total Activities
10
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 |
Publication
Potent and selective tariquidar bioisosters as potential PET radiotracers for imaging P-gp.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 6.01 | 7.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL348475 | TARIQUIDAR | 3.0 | 1 | 7.36 |
| CHEMBL2335007 | — | — | 1 | 6.60 |
| CHEMBL2335002 | — | — | 1 | 6.39 |
| CHEMBL2335008 | — | — | 1 | 6.29 |
| CHEMBL260506 | — | — | 1 | 6.22 |
| CHEMBL2335006 | — | — | 1 | 6.02 |
| CHEMBL260599 | — | — | 1 | 5.82 |
| CHEMBL2335003 | — | — | 1 | 5.71 |
| CHEMBL2335005 | — | — | 1 | 4.96 |
| CHEMBL2335004 | — | — | 1 | 4.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL348475 | TARIQUIDAR | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL2335007 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL2335002 | — | EC50 | = | 410.0 | nM | 6.39 |
| CHEMBL2335008 | — | EC50 | = | 510.0 | nM | 6.29 |
| CHEMBL260506 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL2335006 | — | EC50 | = | 950.0 | nM | 6.02 |
| CHEMBL260599 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2335003 | — | EC50 | = | 1940.0 | nM | 5.71 |
| CHEMBL2335005 | — | EC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL2335004 | — | EC50 | = | 19000.0 | nM | 4.72 |