Assay Detail
Binding
CHEMBL968701
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG expressed in HEK293 cells by patch-clamp method
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
Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.64 | 6.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221906 | — | — | 1 | 6.48 |
| CHEMBL515919 | — | — | 1 | 5.38 |
| CHEMBL512351 | BETRIXABAN | 4.0 | 1 | 5.05 |
| CHEMBL472967 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221906 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL515919 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL512351 | BETRIXABAN | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL472967 | — | IC50 | - | — | - |