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Assay Detail

CHEMBL3856334

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Binding
Inhibition of human GST-tagged SIRT1 (18 to 340 residues) expressed in Escherichia coli BL21 (DE3)LysS using acetylated HeLa histones as substrate measured after 2 hrs in presence of NAD by scintillation counting method
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

How much successful are the medicinal chemists in modulation of SIRT1: A critical review.
Kumar A, Chauhan S.
Eur J Med Chem (2016) 119 : 45 -69
PubMed 27153347 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 4.42 4.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL380797 SIRTINOL 1 4.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL380797 SIRTINOL IC50 = 38000.0 nM 4.42