Assay Detail
Binding
CHEMBL950430
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG by electrophysiology assay
3
Total Activities
3
Compounds Tested
2
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
Lead optimization of 4-acetylamino-2-(3,5-dimethylpyrazol-1-yl)-6-pyridylpyrimidines as A2A adenosine receptor antagonists for the treatment of Parkinson's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 5.45 | 6.27 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL486162 | — | — | 1 | 6.27 |
| CHEMBL458242 | — | — | 1 | 4.62 |
| CHEMBL520229 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL486162 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL458242 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL520229 | — | Activity | - | — | - |