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Assay Detail

CHEMBL4334556

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Binding
Inhibition of recombinant full length N-terminal GST-tagged human HDAC6 expressed in baculovirus infected Sf9 cells using Z-Lys(Ac)-AMC as substrate incubated for 90 mins followed by trypsin addition and measured after 30 mins by fluorescence based assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity.
Reßing N, Marquardt V, Gertzen CGW, Schöler A, Schramm A, Kurz T, Gohlke H, Aigner A, Remke M, Hansen FK.
Medchemcomm (2019) 10 : 1109 -1115
PubMed 31391882 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.70 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4583725 1 8.00
CHEMBL4455083 1 7.97
CHEMBL4577419 1 7.90
CHEMBL2018302 TUBASTATIN A 1 7.85
CHEMBL4580143 1 7.84
CHEMBL4476049 1 7.83
CHEMBL4539004 1 7.78
CHEMBL4522149 1 7.71
CHEMBL4461005 1 7.69
CHEMBL4549502 1 7.60
CHEMBL4562808 1 7.58
CHEMBL4458544 1 7.51
CHEMBL98 VORINOSTAT 4.0 1 7.46
CHEMBL4066043 1 7.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4583725 IC50 = 10.0 nM 8.00
CHEMBL4455083 IC50 = 10.7 nM 7.97
CHEMBL4577419 IC50 = 12.5 nM 7.90
CHEMBL2018302 TUBASTATIN A IC50 = 14.0 nM 7.85
CHEMBL4580143 IC50 = 14.4 nM 7.84
CHEMBL4476049 IC50 = 14.8 nM 7.83
CHEMBL4539004 IC50 = 16.7 nM 7.78
CHEMBL4522149 IC50 = 19.5 nM 7.71
CHEMBL4461005 IC50 = 20.5 nM 7.69
CHEMBL4549502 IC50 = 25.3 nM 7.60
CHEMBL4562808 IC50 = 26.0 nM 7.58
CHEMBL4458544 IC50 = 31.1 nM 7.51
CHEMBL98 VORINOSTAT IC50 = 34.3 nM 7.46
CHEMBL4066043 IC50 = 85.0 nM 7.07