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Assay Detail

CHEMBL859745

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

Binding
Inhibitory activity against human SIRT2
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

NAD-dependent protein deacetylase sirtuin-2 (CHEMBL4462)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of sirtinol analogues as class III histone/protein deacetylase (Sirtuin) inhibitors.
Mai A, Massa S, Lavu S, Pezzi R, Simeoni S, Ragno R, Mariotti FR, Chiani F, Camilloni G, Sinclair DA.
J Med Chem (2005) 48 : 7789 -7795
PubMed 16302818 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 4.40 4.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL372375 1 4.59
CHEMBL200762 1 4.45
CHEMBL197282 1 4.41
CHEMBL198582 1 4.31
CHEMBL380797 SIRTINOL 1 4.24
CHEMBL371286 1 -
CHEMBL200731 1 -
CHEMBL383787 1 -
CHEMBL200725 1 -
CHEMBL200544 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL372375 IC50 = 25900.0 nM 4.59
CHEMBL200762 IC50 = 35700.0 nM 4.45
CHEMBL197282 IC50 = 39400.0 nM 4.41
CHEMBL198582 IC50 = 49300.0 nM 4.31
CHEMBL380797 SIRTINOL IC50 = 57700.0 nM 4.24
CHEMBL371286 IC50 - -
CHEMBL200731 IC50 - -
CHEMBL383787 IC50 - -
CHEMBL200725 IC50 - -
CHEMBL200544 IC50 - -