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Assay Detail

CHEMBL3241376

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

Binding
Inhibition of human recombinant SIRT2 using Fluor-de-Lys as substrate incubated for 60 mins prior to substrate addition measured after 60 mins by fluorometric analysis
3
Total Activities
3
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

Identification of novel SIRT2-selective inhibitors using a click chemistry approach.
Tatum PR, Sawada H, Ota Y, Itoh Y, Zhan P, Ieda N, Nakagawa H, Miyata N, Suzuki T.
Bioorg Med Chem Lett (2014) 24 : 1871 -1874
PubMed 24675380 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.31 5.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL224864 1 5.46
CHEMBL3236132 1 5.28
CHEMBL3236133 1 5.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL224864 IC50 = 3500.0 nM 5.46
CHEMBL3236132 IC50 = 5300.0 nM 5.28
CHEMBL3236133 IC50 = 6300.0 nM 5.20