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Assay Detail

CHEMBL3755646

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

Binding
Inhibition of recombinant human C-terminal His-tagged SIRT2 (13 to 319 residues) using human p53 derived peptides as substrate incubated for 45 mins by fluorescence assay
11
Total Activities
11
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

Discovery of a potent and highly fluorescent sirtuin inhibitor
Yoon YK, Ali MA, Wei AC, Choon TS, Shirazi AN, Parang K
Medchemcomm (2015) 6 : 1857 -1863
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 4.71 5.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL224864 1 5.10
CHEMBL3754317 1 5.05
CHEMBL3752617 1 4.87
CHEMBL595354 1 4.57
CHEMBL420311 1 4.36
CHEMBL3752305 1 4.28
CHEMBL3752528 1 -
CHEMBL3751949 1 -
CHEMBL3752548 1 -
CHEMBL3754315 1 -
CHEMBL3751867 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL224864 IC50 = 7900.0 nM 5.10
CHEMBL3754317 IC50 = 9000.0 nM 5.05
CHEMBL3752617 IC50 = 13600.0 nM 4.87
CHEMBL595354 IC50 = 27000.0 nM 4.57
CHEMBL420311 IC50 = 43700.0 nM 4.36
CHEMBL3752305 IC50 = 52910.0 nM 4.28
CHEMBL3752528 IC50 - -
CHEMBL3751949 IC50 - -
CHEMBL3752548 IC50 - -
CHEMBL3754315 IC50 - -
CHEMBL3751867 IC50 - -