Assay Detail
Binding
CHEMBL949251
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Inhibition of human ERG potassium current expressed in HEK293 cells by patch-clamp technique
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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
2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 2. Reduction of hERG activity, observed species selectivity, and structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 5.99 | 6.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL409419 | — | — | 1 | 6.54 |
| CHEMBL409229 | — | — | 1 | 6.38 |
| CHEMBL271606 | — | — | 1 | 6.22 |
| CHEMBL410234 | — | — | 1 | 6.19 |
| CHEMBL270467 | — | — | 1 | 6.02 |
| CHEMBL272637 | — | — | 1 | 6.00 |
| CHEMBL409459 | — | — | 1 | 5.78 |
| CHEMBL429761 | — | — | 1 | 5.73 |
| CHEMBL270314 | — | — | 1 | 5.64 |
| CHEMBL272679 | — | — | 1 | 5.38 |
| CHEMBL429575 | — | — | 1 | - |
| CHEMBL259038 | — | — | 1 | - |
| CHEMBL409230 | — | — | 1 | - |
| CHEMBL270355 | — | — | 1 | - |
| CHEMBL406397 | — | — | 1 | - |
| CHEMBL271786 | — | — | 1 | - |
| CHEMBL406921 | — | — | 1 | - |
| CHEMBL261176 | — | — | 1 | - |
| CHEMBL261177 | — | — | 1 | - |
| CHEMBL409460 | — | — | 1 | - |
| CHEMBL409420 | — | — | 1 | - |
| CHEMBL429428 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL409419 | — | IC50 | = | 285.0 | nM | 6.54 |
| CHEMBL409229 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL271606 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL410234 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL270467 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL272637 | — | IC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL409459 | — | IC50 | = | 1670.0 | nM | 5.78 |
| CHEMBL429761 | — | IC50 | = | 1860.0 | nM | 5.73 |
| CHEMBL270314 | — | IC50 | = | 2280.0 | nM | 5.64 |
| CHEMBL272679 | — | IC50 | = | 4170.0 | nM | 5.38 |
| CHEMBL429575 | — | IC50 | - | — | - | |
| CHEMBL259038 | — | IC50 | - | — | - | |
| CHEMBL409230 | — | IC50 | - | — | - | |
| CHEMBL270355 | — | IC50 | - | — | - | |
| CHEMBL406397 | — | IC50 | - | — | - | |
| CHEMBL271786 | — | IC50 | - | — | - | |
| CHEMBL406921 | — | IC50 | - | — | - | |
| CHEMBL261176 | — | IC50 | - | — | - | |
| CHEMBL261177 | — | IC50 | - | — | - | |
| CHEMBL409460 | — | IC50 | - | — | - | |
| CHEMBL409420 | — | IC50 | - | — | - | |
| CHEMBL429428 | — | IC50 | - | — | - |