Assay Detail
Binding
CHEMBL5733101
Review assay metadata, readout intent, target linkage, and publication context from the same page.
hERG Binding Assay: hERG (human ether a go go-related gene) potassium channels are essential for normal electrical activity in the heart. Arrhythmia can be induced by a blockage of hERG channels by a diverse group of drugs. This side effect is a common reason for drug failure in preclinical safety trials [Sanguinetti et al., Nature, 2006, 440, 463-469.] and therefore minimisation of hERG channel blocking activity may be a desirable property for drug candidates.The purpose of the hERG binding assay is to evaluate the effects of test compounds on the voltage-dependent potassium channel encoded by the human ether go go-related gene (hERG) using a constitutively expressing CHO cell line on the Nanion Syncropatch 384PE automated patch clamp system.
381
Total Activities
126
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Chemical compounds
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 127 | 5.28 | 5.82 |
| kon | 127 | - | - |
| k_off | 127 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5400637 | — | — | 3 | 5.82 |
| CHEMBL5772929 | — | — | 3 | 5.70 |
| CHEMBL6011841 | — | — | 3 | 5.64 |
| CHEMBL5796450 | — | — | 3 | 5.62 |
| CHEMBL5933859 | — | — | 3 | 5.58 |
| CHEMBL5871237 | — | — | 3 | 5.58 |
| CHEMBL5804138 | — | — | 3 | 5.57 |
| CHEMBL5846746 | — | — | 3 | 5.57 |
| CHEMBL5839498 | — | — | 3 | 5.57 |
| CHEMBL5988920 | — | — | 3 | 5.57 |
| CHEMBL5741828 | — | — | 3 | 5.55 |
| CHEMBL5849595 | — | — | 3 | 5.55 |
| CHEMBL5902781 | — | — | 3 | 5.54 |
| CHEMBL5837180 | — | — | 3 | 5.51 |
| CHEMBL5806518 | — | — | 3 | 5.50 |
| CHEMBL5886475 | — | — | 3 | 5.47 |
| CHEMBL5943322 | — | — | 3 | 5.46 |
| CHEMBL5998681 | — | — | 3 | 5.46 |
| CHEMBL5398790 | — | — | 3 | 5.44 |
| CHEMBL6051199 | — | — | 3 | 5.44 |
| CHEMBL5874010 | — | — | 3 | 5.42 |
| CHEMBL5423660 | — | — | 3 | 5.42 |
| CHEMBL5954593 | — | — | 3 | 5.41 |
| CHEMBL5952392 | — | — | 3 | 5.41 |
| CHEMBL5974706 | — | — | 3 | 5.41 |
| CHEMBL5775436 | — | — | 3 | 5.40 |
| CHEMBL5424734 | — | — | 3 | 5.39 |
| CHEMBL5967894 | — | — | 3 | 5.39 |
| CHEMBL5908705 | — | — | 3 | 5.39 |
| CHEMBL5855181 | — | — | 3 | 5.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5400637 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL5772929 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL6011841 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL5796450 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL5871237 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL5933859 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL5988920 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL5839498 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL5804138 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL5846746 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL5741828 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL5849595 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL5902781 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL5837180 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL5806518 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL5886475 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL5998681 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL5943322 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL6051199 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL5398790 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL5423660 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL5874010 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL5952392 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL5974706 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL5954593 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL5775436 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5967894 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL5855181 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL5424734 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL5908705 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL5972799 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL5743400 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL5975525 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL5927490 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL5926652 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL5978181 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL5788221 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL5400175 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL5912040 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL5407684 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL5432698 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL5760349 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL6007627 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL5969609 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL5934302 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL5752521 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL5832006 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5834106 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5775252 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5421791 | — | IC50 | = | 5100.0 | nM | 5.29 |