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Assay Detail

CHEMBL3242722

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

Binding
Inhibition of SIRT2 (unknown origin) by luminescence assay
6
Total Activities
6
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

Development of pyrazolone and isoxazol-5-one cambinol analogues as sirtuin inhibitors.
Mahajan SS, Scian M, Sripathy S, Posakony J, Lao U, Loe TK, Leko V, Thalhofer A, Schuler AD, Bedalov A, Simon JA.
J Med Chem (2014) 57 : 3283 -3294
PubMed 24697269 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 4.46 4.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3233749 1 4.89
CHEMBL3233733 1 4.50
CHEMBL491960 CAMBINOL 1 4.29
CHEMBL3233748 1 4.17
CHEMBL3233739 1 -
CHEMBL3233742 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3233749 IC50 = 13000.0 nM 4.89
CHEMBL3233733 IC50 = 32000.0 nM 4.50
CHEMBL491960 CAMBINOL IC50 = 51000.0 nM 4.29
CHEMBL3233748 IC50 = 68000.0 nM 4.17
CHEMBL3233739 IC50 > 200000.0 nM -
CHEMBL3233742 IC50 > 200000.0 nM -