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Assay Detail

CHEMBL933817

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

Binding
Activation of human SIRT1 expressed in Escherichia coli BL21 by mass spectrometry assay
8
Total Activities
4
Compounds Tested
2
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

Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes.
Milne JC, Lambert PD, Schenk S, Carney DP, Smith JJ, Gagne DJ, Jin L, Boss O, Perni RB, Vu CB, Bemis JE, Xie R, Disch JS, Ng PY, Nunes JJ, Lynch AV, Yang H, Galonek H, Israelian K, Choy W, Iffland A, Lavu S, Medvedik O, Sinclair DA, Olefsky JM, Jirousek MR, Elliott PJ, Westphal CH.
Nature (2007) 450 : 712 -716
PubMed 18046409 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 5.78 6.80
Activity 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL257991 2 6.80
CHEMBL403308 2 6.44
CHEMBL254156 2 5.54
CHEMBL165 RESVERATROL 3.0 2 4.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL257991 EC50 = 160.0 nM 6.80
CHEMBL403308 EC50 = 360.0 nM 6.44
CHEMBL254156 EC50 = 2900.0 nM 5.54
CHEMBL165 RESVERATROL EC50 = 46200.0 nM 4.33
CHEMBL165 RESVERATROL Activity = 201.0 % -
CHEMBL254156 Activity = 447.0 % -
CHEMBL403308 Activity = 296.0 % -
CHEMBL257991 Activity = 781.0 % -