Assay Detail
Binding
CHEMBL2186754
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]dofetilide to human ERG expressed in HEK293 cells
7
Total Activities
7
Compounds Tested
1
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
Design and synthesis of a novel series of bicyclic heterocycles as potent γ-secretase modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.45 | 5.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2178521 | — | — | 1 | 5.75 |
| CHEMBL2151218 | — | — | 1 | 5.70 |
| CHEMBL2178522 | — | — | 1 | 5.28 |
| CHEMBL2151164 | — | — | 1 | 5.07 |
| CHEMBL2178524 | — | — | 1 | - |
| CHEMBL2178523 | — | — | 1 | - |
| CHEMBL2178520 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2178521 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL2151218 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2178522 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL2151164 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL2178524 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2178523 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2178520 | — | IC50 | - | — | - |