Assay Detail
Binding
CHEMBL2166760
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-astemizole from human ERG expressed in HEK293 cells after 60 mins by liquid scintillation counter
4
Total Activities
4
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
Novel N-linked aminopiperidine inhibitors of bacterial topoisomerase type II with reduced pK(a): antibacterial agents with an improved safety profile.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 4.33 | 4.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2165062 | — | — | 1 | 4.41 |
| CHEMBL2165068 | — | — | 1 | 4.24 |
| CHEMBL2165064 | — | — | 1 | - |
| CHEMBL2165065 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2165062 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL2165068 | — | IC50 | = | 57000.0 | nM | 4.24 |
| CHEMBL2165064 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL2165065 | — | IC50 | > | 200000.0 | nM | - |