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Assay Detail

CHEMBL4305709

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

Binding
Inhibition of recombinant human SIRT3 (118 to 399 residues) demyristoylase activity expressed in Escherichia coli using p53(Myr)-AMC as substrate measured after 3 hrs in presence of NAD+ and trypsin by fluorescence assay
9
Total Activities
9
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

Publication

Development of Peptide-Based Sirtuin Defatty-Acylase Inhibitors Identified by the Fluorescence Probe, SFP3, That Can Efficiently Measure Defatty-Acylase Activity of Sirtuin.
Kawaguchi M, Ieda N, Nakagawa H.
J Med Chem (2019) 62 : 5434 -5452
PubMed 31117516 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.58 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4438193 1 6.89
CHEMBL4446458 1 6.72
CHEMBL4457496 1 6.48
CHEMBL4447813 1 6.47
CHEMBL4461872 1 6.32
CHEMBL4529328 1 -
CHEMBL4553811 1 -
CHEMBL1140 NIACINAMIDE 4.0 1 -
CHEMBL3770903 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4438193 IC50 = 130.0 nM 6.89
CHEMBL4446458 IC50 = 190.0 nM 6.72
CHEMBL4457496 IC50 = 330.0 nM 6.48
CHEMBL4447813 IC50 = 340.0 nM 6.47
CHEMBL4461872 IC50 = 480.0 nM 6.32
CHEMBL4529328 IC50 - -
CHEMBL4553811 IC50 - -
CHEMBL1140 NIACINAMIDE IC50 - -
CHEMBL3770903 IC50 - -