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Assay Detail

CHEMBL1069455

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

Binding
Inhibition of human recombinant SIRT1 by Flour de Lys assay
12
Total Activities
12
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-1 (CHEMBL4506)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Characterization of sirtuin inhibitors in nematodes expressing a muscular dystrophy protein reveals muscle cell and behavioral protection by specific sirtinol analogues.
Pasco MY, Rotili D, Altucci L, Farina F, Rouleau GA, Mai A, Néri C.
J Med Chem (2010) 53 : 1407 -1411
PubMed 20041717 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 4.69 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL597477 1 6.80
CHEMBL611665 1 5.28
CHEMBL596657 1 5.08
CHEMBL596656 1 4.39
CHEMBL597845 SALERMIDE 1 4.37
CHEMBL596655 1 4.36
CHEMBL372375 1 4.32
CHEMBL200762 1 4.23
CHEMBL490905 1 4.05
CHEMBL86537 SPLITOMICIN 1 4.02
CHEMBL380797 SIRTINOL 1 -
CHEMBL224864 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL597477 IC50 = 160.0 nM 6.80
CHEMBL611665 IC50 = 5300.0 nM 5.28
CHEMBL596657 IC50 = 8400.0 nM 5.08
CHEMBL596656 IC50 = 40300.0 nM 4.39
CHEMBL597845 SALERMIDE IC50 = 42800.0 nM 4.37
CHEMBL596655 IC50 = 44100.0 nM 4.36
CHEMBL372375 IC50 = 48100.0 nM 4.32
CHEMBL200762 IC50 = 58600.0 nM 4.23
CHEMBL490905 IC50 = 89800.0 nM 4.05
CHEMBL86537 SPLITOMICIN IC50 = 96200.0 nM 4.02
CHEMBL380797 SIRTINOL IC50 = 123300.0 nM -
CHEMBL224864 IC50 > 50000.0 nM -