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Assay Detail

CHEMBL3748918

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

Binding
Inhibition of human recombinant SIRT1 deacetylase activity using Arg-His-Lys-Lys(epsilon-acetyl)-AMC as substrate incubated for 45 mins by fluorescence analysis
2
Total Activities
2
Compounds Tested
2
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-1 (CHEMBL4506)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and Characterization of 4,11-Diaminoanthra[2,3-b]furan-5,10-diones: Tumor Cell Apoptosis through tNOX-Modulated NAD(+)/NADH Ratio and SIRT1.
Tikhomirov AS, Shchekotikhin AE, Lee YH, Chen YA, Yeh CA, Tatarskiy VV, Dezhenkova LG, Glazunova VA, Balzarini J, Shtil AA, Preobrazhenskaya MN, Chueh PJ.
J Med Chem (2015) 58 : 9522 -9534
PubMed 26633734 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.41 5.41
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3747698 1 5.41
CHEMBL1140 NIACINAMIDE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3747698 IC50 = 3930.0 nM 5.41
CHEMBL1140 NIACINAMIDE Inhibition - % -