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Assay Detail

CHEMBL4617627

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

Binding
Inhibition of SIRT2 deacetylation activity (unknown origin) using H3K9Ac ( 4 to 15 residues) as substrate by HPLC analysis
6
Total Activities
6
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

Unexpected small molecules as novel SIRT2 suicide inhibitors.
Chen X, Zou Y, Wang J, Cao Z, Liu J, Li Y, Zhao Y, He B.
Bioorg Med Chem (2020) 28 : 115353 -115353
PubMed 32061485 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 4.65 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3770903 1 6.22
CHEMBL4643733 1 4.84
CHEMBL4638076 1 4.37
CHEMBL4634872 1 4.25
CHEMBL4634985 1 4.13
CHEMBL4640752 1 4.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3770903 IC50 = 600.0 nM 6.22
CHEMBL4643733 IC50 = 14300.0 nM 4.84
CHEMBL4638076 IC50 = 42700.0 nM 4.37
CHEMBL4634872 IC50 = 56600.0 nM 4.25
CHEMBL4634985 IC50 = 74000.0 nM 4.13
CHEMBL4640752 IC50 = 77100.0 nM 4.11