Assay Detail
Binding
CHEMBL1014292
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A2780 ADR |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of a small molecule library of 3rd generation multidrug resistance modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 43 | 5.60 | 7.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL348475 | TARIQUIDAR | 3.0 | 1 | 7.11 |
| CHEMBL515247 | — | — | 1 | 6.66 |
| CHEMBL475362 | — | — | 1 | 6.48 |
| CHEMBL411951 | — | — | 1 | 6.37 |
| CHEMBL258882 | — | — | 1 | 6.33 |
| CHEMBL258909 | — | — | 1 | 6.24 |
| CHEMBL260113 | — | — | 1 | 6.20 |
| CHEMBL409234 | — | — | 1 | 6.19 |
| CHEMBL473794 | — | — | 1 | 6.17 |
| CHEMBL515282 | — | — | 1 | 6.17 |
| CHEMBL475554 | — | — | 1 | 6.11 |
| CHEMBL472761 | — | — | 1 | 6.07 |
| CHEMBL473987 | — | — | 1 | 5.96 |
| CHEMBL160 | CYCLOSPORINE | 4.0 | 1 | 5.85 |
| CHEMBL515579 | — | — | 1 | 5.85 |
| CHEMBL259976 | — | — | 1 | 5.85 |
| CHEMBL555611 | — | — | 1 | 5.85 |
| CHEMBL474972 | — | — | 1 | 5.82 |
| CHEMBL471719 | — | — | 1 | 5.82 |
| CHEMBL259789 | — | — | 1 | 5.75 |
| CHEMBL474179 | — | — | 1 | 5.68 |
| CHEMBL261857 | — | — | 1 | 5.62 |
| CHEMBL473795 | — | — | 1 | 5.51 |
| CHEMBL408709 | — | — | 1 | 5.48 |
| CHEMBL473198 | — | — | 1 | 5.47 |
| CHEMBL471170 | — | — | 1 | 5.39 |
| CHEMBL260896 | — | — | 1 | 5.38 |
| CHEMBL261632 | — | — | 1 | 5.36 |
| CHEMBL258575 | — | — | 1 | 5.33 |
| CHEMBL409480 | — | — | 1 | 5.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL348475 | TARIQUIDAR | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL515247 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL475362 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL411951 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL258882 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL258909 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL260113 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL409234 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL473794 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL515282 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL475554 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL472761 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL473987 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL555611 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL259976 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL160 | CYCLOSPORINE | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL515579 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL474972 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL471719 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL259789 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL474179 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL261857 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL473795 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL408709 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL473198 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL471170 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL260896 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL261632 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL258575 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL409480 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL6966 | VERAPAMIL | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL442464 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL261618 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL429515 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL259077 | — | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL410897 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL258574 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL474756 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL258456 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL472819 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL472818 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL474757 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL23 | DILTIAZEM | IC50 | = | 49000.0 | nM | 4.31 |