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Assay Detail

CHEMBL5374989

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

Binding
Inhibition of human Sirt2 (25 to 389 residues) expressed in Escherichia coli BL21(DE3) Codon plus RIPL cells using ZMAL as substrate incubated for 4 hrs in presence of NAD+ by fluorescence based analysis
2
Total Activities
2
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

Development of First-in-Class Dual Sirt2/HDAC6 Inhibitors as Molecular Tools for Dual Inhibition of Tubulin Deacetylation.
Sinatra L, Vogelmann A, Friedrich F, Tararina MA, Neuwirt E, Colcerasa A, König P, Toy L, Yesiloglu TZ, Hilscher S, Gaitzsch L, Papenkordt N, Zhai S, Zhang L, Romier C, Einsle O, Sippl W, Schutkowski M, Gross O, Bendas G, Christianson DW, Hansen FK, Jung M, Schiedel M.
J Med Chem (2023) 66 : 14787 -14814
PubMed 37902787 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.90 6.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3770903 1 6.36
CHEMBL3769988 1 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3770903 IC50 = 440.0 nM 6.36
CHEMBL3769988 IC50 = 3700.0 nM 5.43