Assay Detail
Binding
CHEMBL4339665
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]dofetilide from recombinant human ERG expressed in HEK293 cell membranes measured after 80 mins by TopCount scintillation analysis
30
Total Activities
30
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
1H-Pyrrolo[3,2-b]pyridine GluN2B-Selective Negative Allosteric Modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 5.28 | 5.28 |
| Ki | 11 | 5.64 | 6.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4526512 | — | — | 1 | 6.05 |
| CHEMBL4537967 | — | — | 1 | 5.96 |
| CHEMBL4539619 | — | — | 1 | 5.85 |
| CHEMBL4446706 | — | — | 1 | 5.62 |
| CHEMBL4443868 | — | — | 1 | 5.54 |
| CHEMBL4445829 | — | — | 1 | 5.54 |
| CHEMBL4475155 | — | — | 1 | 5.31 |
| CHEMBL4515350 | — | — | 1 | 5.28 |
| CHEMBL4302264 | — | — | 1 | 5.23 |
| CHEMBL4474982 | — | — | 1 | - |
| CHEMBL4451099 | — | — | 1 | - |
| CHEMBL4513602 | — | — | 1 | - |
| CHEMBL4462073 | — | — | 1 | - |
| CHEMBL4463483 | — | — | 1 | - |
| CHEMBL4571666 | — | — | 1 | - |
| CHEMBL4462496 | — | — | 1 | - |
| CHEMBL4471014 | — | — | 1 | - |
| CHEMBL4590530 | — | — | 1 | - |
| CHEMBL4550955 | — | — | 1 | - |
| CHEMBL4593473 | — | — | 1 | - |
| CHEMBL4547576 | — | — | 1 | - |
| CHEMBL4467491 | — | — | 1 | - |
| CHEMBL4591770 | — | — | 1 | - |
| CHEMBL4442512 | — | — | 1 | - |
| CHEMBL4531750 | — | — | 1 | - |
| CHEMBL4575739 | — | — | 1 | - |
| CHEMBL4529810 | — | — | 1 | - |
| CHEMBL4211247 | — | — | 1 | - |
| CHEMBL4451514 | — | — | 1 | - |
| CHEMBL4529074 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4526512 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL4537967 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL4539619 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL4446706 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL4443868 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL4445829 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL4475155 | — | Ki | = | 4900.0 | nM | 5.31 |
| CHEMBL4515350 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4302264 | — | Ki | = | 5900.0 | nM | 5.23 |
| CHEMBL4474982 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4451099 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4513602 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4462073 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4463483 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4571666 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4462496 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4471014 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4590530 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4550955 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4593473 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4547576 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4467491 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4591770 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4442512 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4531750 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4575739 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4529810 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4211247 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4451514 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4529074 | — | IC50 | > | 10000.0 | nM | - |