Assay Detail
Binding
CHEMBL1048091
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Inhibition of human ERG in L929 cells by whole cell patch-clamp assay
6
Total Activities
6
Compounds Tested
1
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 |
|---|---|---|---|
| IC50 | 6 | 5.96 | 6.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL17157 | TERFENADINE | 4.0 | 1 | 6.51 |
| CHEMBL571389 | — | — | 1 | 6.40 |
| CHEMBL570033 | — | — | 1 | 4.96 |
| CHEMBL127508 | AZACYCLONOL | 2.0 | 1 | - |
| CHEMBL571174 | — | — | 1 | - |
| CHEMBL914 | FEXOFENADINE | 4.0 | 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 |
| CHEMBL127508 | AZACYCLONOL | IC50 | > | 100000.0 | nM | - |
| CHEMBL571174 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL914 | FEXOFENADINE | IC50 | > | 100.0 | nM | - |