Assay Detail
Binding
CHEMBL4234644
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activation of full-length recombinant N-terminal His-tagged human AMPKalpha1beta1gamma1 expressed in Escherichia coli BL21 cells using Cy-5 SAMS peptide as substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins in presence of PP2a by TR-FRET assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Intermediate |
Target
AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 (CHEMBL2111345) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Acyl Glucuronide Metabolites of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1 H-indole-3-carboxylic Acid (PF-06409577) and Related Indole-3-carboxylic Acid Derivatives are Direct Activators of Adenosine Monophosphate-Activated Protein Kinase (AMPK).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 7.79 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3891221 | — | — | 1 | 8.72 |
| CHEMBL3986871 | — | — | 1 | 8.15 |
| CHEMBL4105032 | — | — | 1 | 8.10 |
| CHEMBL4249790 | — | — | 1 | 7.42 |
| CHEMBL4246000 | — | — | 1 | 7.23 |
| CHEMBL4250253 | — | — | 1 | 7.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3891221 | — | EC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3986871 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4105032 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4249790 | — | EC50 | = | 38.1 | nM | 7.42 |
| CHEMBL4246000 | — | EC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4250253 | — | EC50 | = | 76.0 | nM | 7.12 |