Assay Detail
Binding
CHEMBL4412989
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MDR1 (unknown origin) expressed in MDCK cells assessed as increase in calcein-AM accumulation after 30 mins by calcein-AM dye based fluorescence assay
19
Total Activities
19
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
Design, Biological Evaluation, and Molecular Modeling of Tetrahydroisoquinoline Derivatives: Discovery of A Potent P-Glycoprotein Ligand Overcoming Multidrug Resistance in Cancer Stem Cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 19 | 5.69 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4470288 | — | — | 1 | 7.82 |
| CHEMBL4474280 | — | — | 1 | 6.50 |
| CHEMBL260505 | — | — | 1 | 6.16 |
| CHEMBL4546814 | — | — | 1 | 6.06 |
| CHEMBL4472875 | — | — | 1 | 6.05 |
| CHEMBL4593615 | — | — | 1 | 6.01 |
| CHEMBL4435542 | — | — | 1 | 5.96 |
| CHEMBL4529961 | — | — | 1 | 5.92 |
| CHEMBL4470538 | — | — | 1 | 5.83 |
| CHEMBL4454350 | — | — | 1 | 5.82 |
| CHEMBL4435829 | — | — | 1 | 5.77 |
| CHEMBL4558681 | — | — | 1 | 5.51 |
| CHEMBL4551628 | — | — | 1 | 5.28 |
| CHEMBL4483077 | — | — | 1 | 5.16 |
| CHEMBL4543755 | — | — | 1 | 4.72 |
| CHEMBL4590701 | — | — | 1 | 4.67 |
| CHEMBL4461082 | — | — | 1 | 4.67 |
| CHEMBL4442691 | — | — | 1 | 4.53 |
| CHEMBL4522904 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4470288 | — | EC50 | = | 15.3 | nM | 7.82 |
| CHEMBL4474280 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL260505 | — | EC50 | = | 690.0 | nM | 6.16 |
| CHEMBL4546814 | — | EC50 | = | 870.0 | nM | 6.06 |
| CHEMBL4472875 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4593615 | — | EC50 | = | 980.0 | nM | 6.01 |
| CHEMBL4435542 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4529961 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4470538 | — | EC50 | = | 1470.0 | nM | 5.83 |
| CHEMBL4454350 | — | EC50 | = | 1520.0 | nM | 5.82 |
| CHEMBL4435829 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4558681 | — | EC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4551628 | — | EC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL4483077 | — | EC50 | = | 6930.0 | nM | 5.16 |
| CHEMBL4543755 | — | EC50 | = | 19200.0 | nM | 4.72 |
| CHEMBL4590701 | — | EC50 | = | 21400.0 | nM | 4.67 |
| CHEMBL4461082 | — | EC50 | = | 21200.0 | nM | 4.67 |
| CHEMBL4442691 | — | EC50 | = | 29500.0 | nM | 4.53 |
| CHEMBL4522904 | — | EC50 | - | — | - |