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Assay Detail

CHEMBL5540961

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

Binding
Inhibition of recombinant human HDAC6 using Boc-Lys(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence based assay
9
Total Activities
9
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

Histone deacetylase 6 (CHEMBL1865)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and Synthesis of Dual-Targeting Inhibitors of sEH and HDAC6 for the Treatment of Neuropathic Pain and Lipopolysaccharide-Induced Mortality.
Chen Y, Sun J, Tong H, Wang J, Cao R, Xu H, Chen L, Morisseau C, Zhang M, Shi Y, Han C, Zhuang J, Jing Y, Liu Z, Hammock BD, Chen G.
J Med Chem (2024) 67 : 2095 -2117
PubMed 38236416 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.19 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5567303 1 8.30
CHEMBL408513 BELINOSTAT 4.0 1 7.85
CHEMBL5592524 1 7.82
CHEMBL5570460 1 7.77
CHEMBL356769 TUBACIN 1 7.72
CHEMBL5564312 1 7.33
CHEMBL5564613 1 6.45
CHEMBL5574790 1 6.05
CHEMBL5571161 1 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5567303 IC50 = 5.0 nM 8.30
CHEMBL408513 BELINOSTAT IC50 = 14.0 nM 7.85
CHEMBL5592524 IC50 = 15.0 nM 7.82
CHEMBL5570460 IC50 = 17.0 nM 7.77
CHEMBL356769 TUBACIN IC50 = 19.0 nM 7.72
CHEMBL5564312 IC50 = 47.0 nM 7.33
CHEMBL5564613 IC50 = 355.0 nM 6.45
CHEMBL5574790 IC50 = 884.0 nM 6.05
CHEMBL5571161 IC50 = 3440.0 nM 5.46