Assay Detail
Binding
CHEMBL1020710
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ERG in guinea pig ventricular myocytes assessed as blockade of rapid delayed rectifier potassium current by whole cell patch-clamp technique
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Cell Type | Ventricular myocyte |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL5557) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Molecular hybridization, synthesis, and biological evaluation of novel chroman I(Kr) and I(Ks) dual blockers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.02 | 8.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL443619 | — | — | 1 | 8.21 |
| CHEMBL475725 | — | — | 1 | 7.76 |
| CHEMBL520069 | — | — | 1 | 6.97 |
| CHEMBL475111 | — | — | 1 | 6.75 |
| CHEMBL123558 | AZIMILIDE | 3.0 | 1 | 6.75 |
| CHEMBL475724 | — | — | 1 | 6.40 |
| CHEMBL474106 | — | — | 1 | 6.35 |
| CHEMBL515449 | — | — | 1 | 6.35 |
| CHEMBL488372 | — | — | 1 | 6.27 |
| CHEMBL518889 | — | — | 1 | 6.21 |
| CHEMBL475109 | — | — | 1 | 6.00 |
| CHEMBL484801 | — | — | 1 | 5.41 |
| CHEMBL487756 | — | — | 1 | 5.36 |
| CHEMBL473496 | — | — | 1 | 5.33 |
| CHEMBL515594 | — | — | 1 | 5.21 |
| CHEMBL475723 | — | — | 1 | 5.13 |
| CHEMBL475110 | — | — | 1 | 4.93 |
| CHEMBL488159 | — | — | 1 | 4.66 |
| CHEMBL486321 | — | — | 1 | 4.40 |
| CHEMBL516360 | — | — | 1 | - |
| CHEMBL518885 | — | — | 1 | - |
| CHEMBL473292 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL443619 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL475725 | — | IC50 | = | 17.4 | nM | 7.76 |
| CHEMBL520069 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL475111 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL123558 | AZIMILIDE | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL475724 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL474106 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL515449 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL488372 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL518889 | — | IC50 | = | 619.0 | nM | 6.21 |
| CHEMBL475109 | — | IC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL484801 | — | IC50 | = | 3870.0 | nM | 5.41 |
| CHEMBL487756 | — | IC50 | = | 4340.0 | nM | 5.36 |
| CHEMBL473496 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL515594 | — | IC50 | = | 6150.0 | nM | 5.21 |
| CHEMBL475723 | — | IC50 | = | 7470.0 | nM | 5.13 |
| CHEMBL475110 | — | IC50 | = | 11800.0 | nM | 4.93 |
| CHEMBL488159 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL486321 | — | IC50 | = | 39700.0 | nM | 4.40 |
| CHEMBL516360 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL518885 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL473292 | — | IC50 | > | 100000.0 | nM | - |