Assay Detail
Binding
CHEMBL3378079
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG over-expressed in HEK293 cell membrane by [3H]dofetilide binding assay
9
Total Activities
9
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
2',6'-Dihalostyrylanilines, pyridines, and pyrimidines for the inhibition of the catalytic subunit of methionine S-adenosyltransferase-2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 4.49 | 4.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3314430 | — | — | 1 | 4.70 |
| CHEMBL3314423 | — | — | 1 | 4.68 |
| CHEMBL3314424 | — | — | 1 | 4.68 |
| CHEMBL3314426 | — | — | 1 | 4.66 |
| CHEMBL2153098 | — | — | 1 | 4.49 |
| CHEMBL3314433 | — | — | 1 | 4.39 |
| CHEMBL3314417 | — | — | 1 | 4.31 |
| CHEMBL3314420 | — | — | 1 | 4.30 |
| CHEMBL3314429 | — | — | 1 | 4.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3314430 | — | IC50 | = | 19900.0 | nM | 4.70 |
| CHEMBL3314423 | — | IC50 | = | 21100.0 | nM | 4.68 |
| CHEMBL3314424 | — | IC50 | = | 20700.0 | nM | 4.68 |
| CHEMBL3314426 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL2153098 | — | IC50 | = | 32100.0 | nM | 4.49 |
| CHEMBL3314433 | — | IC50 | = | 40500.0 | nM | 4.39 |
| CHEMBL3314417 | — | IC50 | = | 49100.0 | nM | 4.31 |
| CHEMBL3314420 | — | IC50 | = | 49800.0 | nM | 4.30 |
| CHEMBL3314429 | — | IC50 | = | 59500.0 | nM | 4.22 |