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Assay Detail

CHEMBL4322646

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

ADMET
Inhibition of N-terminal His6 tagged human sirtuin 2 (25 to 389 residues) using Cbz-Lys(acetyl)-AMC as substrate after 4 hrs in presence of NAD+ by homogeneous fluorescence based analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
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

Structure-Reactivity Relationships on Substrates and Inhibitors of the Lysine Deacylase Sirtuin 2 from Schistosoma mansoni (SmSirt2).
Monaldi D, Rotili D, Lancelot J, Marek M, Wössner N, Lucidi A, Tomaselli D, Ramos-Morales E, Romier C, Pierce RJ, Mai A, Jung M.
J Med Chem (2019) 62 : 8733 -8759
PubMed 31496251 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 4.85 5.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3431191 1 5.44
CHEMBL4526249 1 4.88
CHEMBL252556 IDEBENONE 4.0 1 4.81
CHEMBL4444104 1 4.67
CHEMBL4459211 1 4.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3431191 IC50 = 3600.0 nM 5.44
CHEMBL4526249 IC50 = 13300.0 nM 4.88
CHEMBL252556 IDEBENONE IC50 = 15400.0 nM 4.81
CHEMBL4444104 IC50 = 21500.0 nM 4.67
CHEMBL4459211 IC50 = 36700.0 nM 4.43