Assay Detail
Binding
CHEMBL4394700
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of AMPKalpha1beta1gamma1 (unknown origin) using biotin-labelled STK substrate-1 as substrate incubated for 60 mins by HTRF assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 (CHEMBL2111345) ↗| Type | PROTEIN COMPLEX |
| 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 | 2 | 6.98 | 6.99 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3544911 | PREXASERTIB | 2.0 | 1 | 6.99 |
| CHEMBL4577258 | — | — | 1 | 6.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3544911 | PREXASERTIB | IC50 | = | 101.62 | nM | 6.99 |
| CHEMBL4577258 | — | IC50 | = | 107.5 | nM | 6.97 |