Assay Detail
Binding
CHEMBL4394729
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG expressed in CHO cells at -80 mV holding potential by automated patch clamp assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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 (R)-5-((5-(1-methyl-1H-pyrazol-4-yl)-4-(methylamino)pyrimidin-2-yl)amino)-3-(piperidin-3-yloxy)picolinonitrile, a novel CHK1 inhibitor for hematologic malignancies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 4.63 | 4.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3544911 | PREXASERTIB | 2.0 | 1 | 4.70 |
| CHEMBL3039517 | RABUSERTIB | 2.0 | 1 | 4.55 |
| CHEMBL4448921 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3544911 | PREXASERTIB | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL3039517 | RABUSERTIB | IC50 | = | 28100.0 | nM | 4.55 |
| CHEMBL4448921 | — | IC50 | > | 40000.0 | nM | - |