Assay Detail
Binding
CHEMBL3789676
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-dofetilide from human ERG channel expressed in HEK293 cells
4
Total Activities
4
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
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.89 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1614712 | — | — | 1 | 6.89 |
| CHEMBL3785500 | — | — | 1 | 5.96 |
| CHEMBL3787636 | — | — | 1 | 4.82 |
| CHEMBL3786634 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1614712 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3785500 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3787636 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL3786634 | — | IC50 | > | 30000.0 | nM | - |