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Assay Detail

CHEMBL4179396

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

Binding
Inhibition of human recombinant SIRT6 assessed as reduction in NAD+-dependent deacetylase activity using Arg-His-Lys-Lys(epsilon-acetyl)-AMC substrate and NAD+ by fluorescence based assay
4
Total Activities
4
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 deacylase sirtuin-6 (CHEMBL2163182)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

SIRT6 inhibitors with salicylate-like structure show immunosuppressive and chemosensitizing effects.
Damonte P, Sociali G, Parenti MD, Soncini D, Bauer I, Boero S, Grozio A, Holtey MV, Piacente F, Becherini P, Sanguineti R, Salis A, Damonte G, Cea M, Murone M, Poggi A, Nencioni A, Del Rio A, Bruzzone S.
Bioorg Med Chem (2017) 25 : 5849 -5858
PubMed 28958848 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 4.47 4.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4217987 1 4.70
CHEMBL4205716 1 4.66
CHEMBL4206619 1 4.47
CHEMBL1588664 1 4.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4217987 IC50 = 20000.0 nM 4.70
CHEMBL4205716 IC50 = 22000.0 nM 4.66
CHEMBL4206619 IC50 = 34000.0 nM 4.47
CHEMBL1588664 IC50 = 89000.0 nM 4.05