Assay Detail
Binding
CHEMBL1106982
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG expressed in HEK cells assessed as blockade of potassium tail current by standard patch clamp analysis
29
Total Activities
29
Compounds Tested
2
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 benzothiophene H1-antihistamines for the treatment of insomnia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 5.97 | 6.62 |
| Ki | 6 | 6.73 | 9.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1091775 | — | — | 1 | 9.14 |
| CHEMBL1092495 | — | — | 1 | 6.62 |
| CHEMBL1092377 | — | — | 1 | 6.48 |
| CHEMBL1091777 | — | — | 1 | 6.31 |
| CHEMBL1092126 | — | — | 1 | 6.04 |
| CHEMBL564144 | — | — | 1 | 5.85 |
| CHEMBL1092766 | — | — | 1 | 5.82 |
| CHEMBL1091782 | — | — | 1 | 5.77 |
| CHEMBL1093294 | — | — | 1 | 5.75 |
| CHEMBL1093058 | — | — | 1 | 5.70 |
| CHEMBL1092765 | — | — | 1 | 5.64 |
| CHEMBL1091069 | — | — | 1 | 5.52 |
| CHEMBL1093044 | — | — | 1 | 5.19 |
| CHEMBL1091792 | — | — | 1 | - |
| CHEMBL1091793 | — | — | 1 | - |
| CHEMBL1091790 | — | — | 1 | - |
| CHEMBL1091778 | — | — | 1 | - |
| CHEMBL1092494 | — | — | 1 | - |
| CHEMBL1091776 | — | — | 1 | - |
| CHEMBL1092496 | — | — | 1 | - |
| CHEMBL1091791 | — | — | 1 | - |
| CHEMBL1092813 | — | — | 1 | - |
| CHEMBL1091774 | — | — | 1 | - |
| CHEMBL1092767 | — | — | 1 | - |
| CHEMBL1090433 | — | — | 1 | - |
| CHEMBL1092118 | — | — | 1 | - |
| CHEMBL1093607 | — | — | 1 | - |
| CHEMBL1090432 | — | — | 1 | - |
| CHEMBL1092812 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1091775 | — | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL1092495 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL1092377 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL1091777 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL1092126 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL564144 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL1092766 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1091782 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1093294 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL1093058 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL1092765 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL1091069 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1093044 | — | Ki | = | 6500.0 | nM | 5.19 |
| CHEMBL1091792 | — | IC50 | - | — | - | |
| CHEMBL1091793 | — | IC50 | - | — | - | |
| CHEMBL1091790 | — | IC50 | - | — | - | |
| CHEMBL1091778 | — | Ki | - | — | - | |
| CHEMBL1092494 | — | IC50 | - | — | - | |
| CHEMBL1091776 | — | Ki | - | — | - | |
| CHEMBL1092496 | — | IC50 | - | — | - | |
| CHEMBL1091791 | — | IC50 | - | — | - | |
| CHEMBL1092813 | — | IC50 | - | — | - | |
| CHEMBL1091774 | — | IC50 | - | — | - | |
| CHEMBL1092767 | — | IC50 | - | — | - | |
| CHEMBL1090433 | — | IC50 | - | — | - | |
| CHEMBL1092118 | — | IC50 | - | — | - | |
| CHEMBL1093607 | — | IC50 | - | — | - | |
| CHEMBL1090432 | — | Ki | - | — | - | |
| CHEMBL1092812 | — | IC50 | - | — | - |