Assay Detail
Binding
CHEMBL1820252
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG Y652A mutant channel expressed in CHO cells by whole-cell patch clamp technique
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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
Block of the hERG channel by bupivacaine: Electrophysiological and modeling insights towards stereochemical optimization.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 4.05 | 4.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1200749 | LEVOBUPIVACAINE HYDROCHLORIDE | 4.0 | 1 | 4.08 |
| CHEMBL1200396 | BUPIVACAINE HYDROCHLORIDE | 4.0 | 1 | 4.02 |
| CHEMBL2447962 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1200749 | LEVOBUPIVACAINE HYDROCHLORIDE | IC50 | = | 83000.0 | nM | 4.08 |
| CHEMBL1200396 | BUPIVACAINE HYDROCHLORIDE | IC50 | = | 95000.0 | nM | 4.02 |
| CHEMBL2447962 | — | IC50 | - | — | - |