Assay Detail
Binding
CHEMBL5737934
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In Vitro pAMPK1 Kinase Activation Assay: Compound effect on AMPK enzyme activation was determined in a cell-free format with a 12-point concentration curve. The ADP-Glo detection system was used to determine phosphorylation of a SAMS peptide substrate. Recombinant AMPK α1/β1/γ1 complex was pre-activated by phosphorylation with CAMKK2 followed by incubated with compound for 15 minutes prior to the SAMS phosphorylation reaction. Activity curves and EC50 values were fitted by interpolation to an ATP:ADP standard curve as indicated by the ADP-Glo manufacturer using Prism software.
27
Total Activities
9
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 (CHEMBL2111345) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
AMPK activators
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 8.05 | 9.26 |
| kon | 9 | - | - |
| k_off | 9 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6032116 | — | — | 3 | 9.26 |
| CHEMBL5991168 | — | — | 3 | 9.01 |
| CHEMBL5806531 | — | — | 3 | 8.96 |
| CHEMBL5938736 | — | — | 3 | 8.85 |
| CHEMBL6012912 | — | — | 3 | 8.62 |
| CHEMBL5843682 | — | — | 3 | 7.70 |
| CHEMBL5913892 | — | — | 3 | 7.37 |
| CHEMBL3393133 | — | — | 3 | 6.70 |
| CHEMBL5929531 | — | — | 3 | 5.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6032116 | — | EC50 | = | 0.55 | nM | 9.26 |
| CHEMBL5991168 | — | EC50 | = | 0.97 | nM | 9.01 |
| CHEMBL5806531 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5938736 | — | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL6012912 | — | EC50 | = | 2.38 | nM | 8.62 |
| CHEMBL5843682 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5913892 | — | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3393133 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5929531 | — | EC50 | = | 1123.0 | nM | 5.95 |
| CHEMBL3393133 | — | kon | = | - | — | - |
| CHEMBL3393133 | — | k_off | = | - | s-1 | - |
| CHEMBL5938736 | — | kon | = | - | — | - |
| CHEMBL5938736 | — | k_off | = | - | s-1 | - |
| CHEMBL5991168 | — | kon | = | - | — | - |
| CHEMBL5991168 | — | k_off | = | - | s-1 | - |
| CHEMBL6012912 | — | kon | = | - | — | - |
| CHEMBL6012912 | — | k_off | = | - | s-1 | - |
| CHEMBL6032116 | — | k_off | = | - | s-1 | - |
| CHEMBL5929531 | — | kon | = | - | — | - |
| CHEMBL5806531 | — | k_off | = | - | s-1 | - |
| CHEMBL5806531 | — | kon | = | - | — | - |
| CHEMBL5843682 | — | k_off | = | - | s-1 | - |
| CHEMBL5843682 | — | kon | = | - | — | - |
| CHEMBL5913892 | — | k_off | = | - | s-1 | - |
| CHEMBL5913892 | — | kon | = | - | — | - |
| CHEMBL6032116 | — | kon | = | - | — | - |
| CHEMBL5929531 | — | k_off | = | - | s-1 | - |