Assay Detail
Binding
CHEMBL4178742
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 after 90 mins by liquid scintillation counting method
13
Total Activities
13
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
Development of Selective, Orally Active GPR4 Antagonists with Modulatory Effects on Nociception, Inflammation, and Angiogenesis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.18 | 6.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3675746 | — | — | 1 | 6.00 |
| CHEMBL4209248 | — | — | 1 | 5.68 |
| CHEMBL4205308 | — | — | 1 | 5.64 |
| CHEMBL3639746 | — | — | 1 | 5.35 |
| CHEMBL4208267 | — | — | 1 | 5.28 |
| CHEMBL4211343 | — | — | 1 | 5.24 |
| CHEMBL3675743 | — | — | 1 | 4.72 |
| CHEMBL4212656 | — | — | 1 | 4.64 |
| CHEMBL4213196 | — | — | 1 | 4.62 |
| CHEMBL4207309 | — | — | 1 | 4.60 |
| CHEMBL4204864 | — | — | 1 | - |
| CHEMBL4210921 | — | — | 1 | - |
| CHEMBL4217603 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3675746 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4209248 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4205308 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3639746 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL4208267 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4211343 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL3675743 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL4212656 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL4213196 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL4207309 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL4204864 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4210921 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4217603 | — | IC50 | > | 30000.0 | nM | - |