Assay Detail
Binding
CHEMBL2379703
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]astemizole from human ERG channel
21
Total Activities
21
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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
A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: comparison of hERG binding and target residence time with PF-3893787.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 5.27 | 6.08 |
| pKi | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2376790 | — | — | 1 | 6.08 |
| CHEMBL2376795 | — | — | 1 | 5.82 |
| CHEMBL2376796 | — | — | 1 | 5.61 |
| CHEMBL2376797 | — | — | 1 | 5.56 |
| CHEMBL1935574 | — | — | 1 | 5.49 |
| CHEMBL2376789 | — | — | 1 | 5.47 |
| CHEMBL1915540 | ADRIFORANT | 2.0 | 1 | 5.46 |
| CHEMBL2376794 | — | — | 1 | 5.44 |
| CHEMBL2376793 | — | — | 1 | 5.33 |
| CHEMBL2376805 | — | — | 1 | 4.89 |
| CHEMBL2376799 | — | — | 1 | 4.57 |
| CHEMBL2376800 | — | — | 1 | 4.46 |
| CHEMBL2376801 | — | — | 1 | 4.36 |
| CHEMBL2376798 | — | — | 1 | - |
| CHEMBL2376791 | — | — | 1 | - |
| CHEMBL2376792 | — | — | 1 | - |
| CHEMBL2376807 | — | — | 1 | - |
| CHEMBL2376802 | — | — | 1 | - |
| CHEMBL2376803 | — | — | 1 | - |
| CHEMBL2376804 | — | — | 1 | - |
| CHEMBL2376806 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2376790 | — | Ki | = | 831.76 | nM | 6.08 |
| CHEMBL2376795 | — | Ki | = | 1513.56 | nM | 5.82 |
| CHEMBL2376796 | — | Ki | = | 2454.71 | nM | 5.61 |
| CHEMBL2376797 | — | Ki | = | 2754.23 | nM | 5.56 |
| CHEMBL1935574 | — | Ki | = | 3235.94 | nM | 5.49 |
| CHEMBL2376789 | — | Ki | = | 3388.44 | nM | 5.47 |
| CHEMBL1915540 | ADRIFORANT | Ki | = | 3467.37 | nM | 5.46 |
| CHEMBL2376794 | — | Ki | = | 3630.78 | nM | 5.44 |
| CHEMBL2376793 | — | Ki | = | 4677.35 | nM | 5.33 |
| CHEMBL2376805 | — | Ki | = | 12882.5 | nM | 4.89 |
| CHEMBL2376799 | — | Ki | = | 26915.35 | nM | 4.57 |
| CHEMBL2376800 | — | Ki | = | 34673.69 | nM | 4.46 |
| CHEMBL2376801 | — | Ki | = | 43651.58 | nM | 4.36 |
| CHEMBL2376798 | — | pKi | - | — | - | |
| CHEMBL2376791 | — | pKi | - | — | - | |
| CHEMBL2376792 | — | pKi | - | — | - | |
| CHEMBL2376807 | — | pKi | - | — | - | |
| CHEMBL2376802 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL2376803 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL2376804 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL2376806 | — | Ki | > | 100000.0 | nM | - |