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Assay Detail

CHEMBL4005604

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

Binding
Inhibition of human SIRT2 (25 to 389 residues) using (Z-Lys(Acetyl)-AMC) as substrate after 4 hrs in presence of NAD+ by fluorescence assay
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

Thienopyrimidinone Based Sirtuin-2 (SIRT2)-Selective Inhibitors Bind in the Ligand Induced Selectivity Pocket.
Sundriyal S, Moniot S, Mahmud Z, Yao S, Di Fruscia P, Reynolds CR, Dexter DT, Sternberg MJ, Lam EW, Steegborn C, Fuchter MJ.
J Med Chem (2017) 60 : 1928 -1945
PubMed 28135086 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.40 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3770903 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3770903 IC50 = 400.0 nM 6.40