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Assay Detail

CHEMBL4017028

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

Binding
Inhibition of N-terminal GST-tagged recombinant human HDAC6 expressed in baculovirus infected Sf9 insect cells using Z-(Ac)Lys-AMC as substrate measured after 90 mins by fluorescence assay
5
Total Activities
5
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, Multicomponent Synthesis, and Anticancer Activity of a Focused Histone Deacetylase (HDAC) Inhibitor Library with Peptoid-Based Cap Groups.
Krieger V, Hamacher A, Gertzen CGW, Senger J, Zwinderman MRH, Marek M, Romier C, Dekker FJ, Kurz T, Jung M, Gohlke H, Kassack MU, Hansen FK.
J Med Chem (2017) 60 : 5493 -5506
PubMed 28574690 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.81 6.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4080343 1 6.97
CHEMBL98 VORINOSTAT 4.0 1 6.97
CHEMBL4090647 1 6.87
CHEMBL4095934 1 6.67
CHEMBL4069631 1 6.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4080343 IC50 = 106.0 nM 6.97
CHEMBL98 VORINOSTAT IC50 = 108.0 nM 6.97
CHEMBL4090647 IC50 = 135.0 nM 6.87
CHEMBL4095934 IC50 = 214.0 nM 6.67
CHEMBL4069631 IC50 = 281.0 nM 6.55