Assay Detail
Binding
CHEMBL4739474
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human ERG expressed in CHO cells incubated for 12 mins by whole cell voltage clamp method
6
Total Activities
6
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
Systematic evaluation of structure-property relationships and pharmacokinetics in 6-(hetero)aryl-substituted matched pair analogs of amiloride and 5-(N,N-hexamethylene)amiloride.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.32 | 5.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL501701 | N,N-HEXAMETHYLENEAMILORIDE | — | 1 | 5.48 |
| CHEMBL4473654 | — | — | 1 | 5.16 |
| CHEMBL945 | AMILORIDE | 4.0 | 1 | - |
| CHEMBL4513418 | — | — | 1 | - |
| CHEMBL4217043 | — | — | 1 | - |
| CHEMBL4213248 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL501701 | N,N-HEXAMETHYLENEAMILORIDE | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4473654 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL945 | AMILORIDE | IC50 | > | 30000.0 | nM | - |
| CHEMBL4513418 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4217043 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4213248 | — | IC50 | < | 3000.0 | nM | - |