Assay Detail
Binding
CHEMBL1048092
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG in L929 cells at 10 uM by whole cell patch-clamp assay
21
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | L929 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structural determinants for histamine H(1) affinity, hERG affinity and QTc prolongation in a series of terfenadine analogs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 15 | - | - |
| IC50 | 6 | 5.96 | 6.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL17157 | TERFENADINE | 4.0 | 2 | 6.51 |
| CHEMBL571389 | — | — | 2 | 6.40 |
| CHEMBL570033 | — | — | 2 | 4.96 |
| CHEMBL914 | FEXOFENADINE | 4.0 | 2 | - |
| CHEMBL571174 | — | — | 2 | - |
| CHEMBL127508 | AZACYCLONOL | 2.0 | 2 | - |
| CHEMBL568892 | — | — | 1 | - |
| CHEMBL571819 | — | — | 1 | - |
| CHEMBL570961 | — | — | 1 | - |
| CHEMBL571073 | — | — | 1 | - |
| CHEMBL570915 | — | — | 1 | - |
| CHEMBL572034 | — | — | 1 | - |
| CHEMBL571390 | — | — | 1 | - |
| CHEMBL571391 | — | — | 1 | - |
| CHEMBL570695 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL17157 | TERFENADINE | IC50 | = | 312.0 | nM | 6.51 |
| CHEMBL571389 | — | IC50 | = | 396.0 | nM | 6.40 |
| CHEMBL570033 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL914 | FEXOFENADINE | Inhibition | = | 3.0 | % | - |
| CHEMBL571389 | — | Inhibition | = | 99.0 | % | - |
| CHEMBL570033 | — | Inhibition | = | 56.0 | % | - |
| CHEMBL571174 | — | Inhibition | = | 85.0 | % | - |
| CHEMBL127508 | AZACYCLONOL | Inhibition | = | 14.0 | % | - |
| CHEMBL568892 | — | Inhibition | = | 100.0 | % | - |
| CHEMBL571819 | — | Inhibition | = | 11.0 | % | - |
| CHEMBL570961 | — | Inhibition | = | 35.0 | % | - |
| CHEMBL571073 | — | Inhibition | = | 71.0 | % | - |
| CHEMBL17157 | TERFENADINE | Inhibition | = | 96.0 | % | - |
| CHEMBL572034 | — | Inhibition | = | 97.0 | % | - |
| CHEMBL571390 | — | Inhibition | = | 100.0 | % | - |
| CHEMBL571391 | — | Inhibition | = | 100.0 | % | - |
| CHEMBL570695 | — | Inhibition | = | 99.0 | % | - |
| CHEMBL914 | FEXOFENADINE | IC50 | > | 100000.0 | nM | - |
| CHEMBL571174 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL127508 | AZACYCLONOL | IC50 | > | 100000.0 | nM | - |
| CHEMBL570915 | — | Inhibition | = | 54.0 | % | - |