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Assay Detail

CHEMBL3859847

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Activation of full length human phosphorylated His-tagged AMPK alpha1/beta1/gamma1 expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL using SAMS peptide substrate preincubated for 15 mins followed by PP2A addition for 90 mins followed by substrate addition measured after 60 mins in presence of [33P]ATP by scintillation counting method
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

Publication

Recent progress in the identification of adenosine monophosphate-activated protein kinase (AMPK) activators.
Cameron KO, Kurumbail RG.
Bioorg Med Chem Lett (2016) 26 : 5139 -5148
PubMed 27727125 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 8.23 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3891221 1 8.38
CHEMBL3936111 1 8.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3891221 EC50 = 4.2 nM 8.38
CHEMBL3936111 EC50 = 8.3 nM 8.08