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Assay Detail

CHEMBL3375828

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

Binding
Inhibition of recombinant GST-tagged sirtuin-2 (unknown origin) using KI179 as substrate after 1 hr by fluorescence assay
32
Total Activities
32
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

Chroman-4-one- and chromone-based sirtuin 2 inhibitors with antiproliferative properties in cancer cells.
Seifert T, Malo M, Kokkola T, Engen K, Fridén-Saxin M, Wallén EA, Lahtela-Kakkonen M, Jarho EM, Luthman K.
J Med Chem (2014) 57 : 9870 -9888
PubMed 25383691 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 5.31 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2164016 1 5.82
CHEMBL3354204 1 5.75
CHEMBL3354206 1 5.70
CHEMBL3354201 1 5.43
CHEMBL2164014 1 5.37
CHEMBL2164015 1 5.35
CHEMBL2164005 1 5.17
CHEMBL3354205 1 5.02
CHEMBL3354214 1 4.91
CHEMBL3354221 1 4.54
CHEMBL3354199 1 -
CHEMBL3354216 1 -
CHEMBL3354202 1 -
CHEMBL3354203 1 -
CHEMBL3354207 1 -
CHEMBL3354208 1 -
CHEMBL3354209 1 -
CHEMBL3354210 1 -
CHEMBL3354211 1 -
CHEMBL3354212 1 -
CHEMBL3354198 1 -
CHEMBL3354223 1 -
CHEMBL3354222 1 -
CHEMBL3354220 1 -
CHEMBL3354219 1 -
CHEMBL3354218 1 -
CHEMBL3354217 1 -
CHEMBL3354196 1 -
CHEMBL3354200 1 -
CHEMBL3354197 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2164016 IC50 = 1500.0 nM 5.82
CHEMBL3354204 IC50 = 1800.0 nM 5.75
CHEMBL3354206 IC50 = 2000.0 nM 5.70
CHEMBL3354201 IC50 = 3700.0 nM 5.43
CHEMBL2164014 IC50 = 4300.0 nM 5.37
CHEMBL2164015 IC50 = 4500.0 nM 5.35
CHEMBL2164005 IC50 = 6800.0 nM 5.17
CHEMBL3354205 IC50 = 9600.0 nM 5.02
CHEMBL3354214 IC50 = 12200.0 nM 4.91
CHEMBL3354221 IC50 = 28700.0 nM 4.54
CHEMBL3354216 IC50 - -
CHEMBL3354202 IC50 - -
CHEMBL3354203 IC50 - -
CHEMBL3354207 IC50 - -
CHEMBL3354208 IC50 - -
CHEMBL3354209 IC50 - -
CHEMBL3354210 IC50 - -
CHEMBL3354211 IC50 - -
CHEMBL3354212 IC50 - -
CHEMBL3354213 IC50 - -
CHEMBL3354215 IC50 - -
CHEMBL3354199 IC50 - -
CHEMBL3354198 IC50 - -
CHEMBL3354223 IC50 - -
CHEMBL3354222 IC50 - -
CHEMBL3354220 IC50 - -
CHEMBL3354219 IC50 - -
CHEMBL3354218 IC50 - -
CHEMBL3354217 IC50 - -
CHEMBL3354196 IC50 - -
CHEMBL3354200 IC50 - -
CHEMBL3354197 IC50 - -