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Assay Detail

CHEMBL3107433

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

Binding
Inhibition of human recombinant N-terminal GST-tagged SIRT1 (193 to 741) after 45 mins by fluorescence assay
16
Total Activities
16
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

Synthesis and evaluation of novel benzimidazole derivatives as sirtuin inhibitors with antitumor activities.
Yoon YK, Ali MA, Wei AC, Choon TS, Osman H, Parang K, Shirazi AN.
Bioorg Med Chem (2014) 22 : 703 -710
PubMed 24387981 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 4.20 4.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL491960 CAMBINOL 1 4.32
CHEMBL3105180 1 4.23
CHEMBL3105181 1 4.13
CHEMBL3105182 1 4.10
CHEMBL3105439 1 -
CHEMBL3105184 1 -
CHEMBL3105183 1 -
CHEMBL3105179 1 -
CHEMBL3105178 1 -
CHEMBL3105177 1 -
CHEMBL3105176 1 -
CHEMBL3105175 1 -
CHEMBL3105174 1 -
CHEMBL3105173 1 -
CHEMBL3105172 1 -
CHEMBL3105171 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL491960 CAMBINOL IC50 = 47900.0 nM 4.32
CHEMBL3105180 IC50 = 58430.0 nM 4.23
CHEMBL3105181 IC50 = 74520.0 nM 4.13
CHEMBL3105182 IC50 = 80110.0 nM 4.10
CHEMBL3105439 IC50 - -
CHEMBL3105184 IC50 - -
CHEMBL3105183 IC50 - -
CHEMBL3105179 IC50 - -
CHEMBL3105178 IC50 - -
CHEMBL3105177 IC50 - -
CHEMBL3105176 IC50 - -
CHEMBL3105175 IC50 - -
CHEMBL3105174 IC50 - -
CHEMBL3105173 IC50 - -
CHEMBL3105172 IC50 - -
CHEMBL3105171 IC50 - -