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Assay Detail

CHEMBL4392971

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

Binding
Inhibition of recombinant SIRT2 (unknown origin) using FAM-RHKK(Ac)LM as substrate measured after 60 mins by electrophoretic mobility shift assay
16
Total Activities
16
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

New SIRT2 inhibitors: Histidine-based bleomycin spin-off.
Ali TFS, Ciftci HI, Radwan MO, Koga R, Ohsugi T, Okiyama Y, Honma T, Nakata A, Ito A, Yoshida M, Fujita M, Otsuka M.
Bioorg Med Chem (2019) 27 : 1767 -1775
PubMed 30885568 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.24 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3770903 1 6.68
CHEMBL4551537 1 5.89
CHEMBL4464347 1 5.77
CHEMBL4522115 1 5.60
CHEMBL4562248 1 5.48
CHEMBL4563921 1 5.25
CHEMBL4456341 1 5.23
CHEMBL4527063 1 5.17
CHEMBL4449841 1 5.12
CHEMBL4473932 1 4.99
CHEMBL4465843 1 4.93
CHEMBL4520968 1 4.79
CHEMBL4577801 1 4.69
CHEMBL4583638 1 4.66
CHEMBL4435754 1 4.37
CHEMBL4439273 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3770903 IC50 = 210.0 nM 6.68
CHEMBL4551537 IC50 = 1300.0 nM 5.89
CHEMBL4464347 IC50 = 1700.0 nM 5.77
CHEMBL4522115 IC50 = 2500.0 nM 5.60
CHEMBL4562248 IC50 = 3300.0 nM 5.48
CHEMBL4563921 IC50 = 5600.0 nM 5.25
CHEMBL4456341 IC50 = 5900.0 nM 5.23
CHEMBL4527063 IC50 = 6700.0 nM 5.17
CHEMBL4449841 IC50 = 7500.0 nM 5.12
CHEMBL4473932 IC50 = 10200.0 nM 4.99
CHEMBL4465843 IC50 = 11800.0 nM 4.93
CHEMBL4520968 IC50 = 16400.0 nM 4.79
CHEMBL4577801 IC50 = 20400.0 nM 4.69
CHEMBL4583638 IC50 = 21800.0 nM 4.66
CHEMBL4435754 IC50 = 43000.0 nM 4.37
CHEMBL4439273 IC50 > 100000.0 nM -