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Assay Detail

CHEMBL3783350

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

Binding
Inhibition of human SIRT2 (25 to 389 amino acid residues) expressed in Escherichia coli BL21 (DE3) assessed as deacetylation using Z-Lys(Acetyl)-AMC as substrate measured after 4 hrs by fluorescence based microplate reader method in presence of 500 uM beta-NAD+
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

NAD-dependent protein deacetylase sirtuin-2 (CHEMBL4462)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Simple N(ε)-thioacetyl-lysine-containing cyclic peptides exhibiting highly potent sirtuin inhibition.
Huang Y, Liu J, Yan L, Zheng W.
Bioorg Med Chem Lett (2016) 26 : 1612 -1617
PubMed 26874402 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.85 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3770903 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3770903 IC50 = 140.0 nM 6.85