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Assay Detail

CHEMBL4034612

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

Binding
Inhibition of HDAC6 (unknown origin) preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay
12
Total Activities
12
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, synthesis and anticancer potential of NSC-319745 hydroxamic acid derivatives as DNMT and HDAC inhibitors.
Yuan Z, Sun Q, Li D, Miao S, Chen S, Song L, Gao C, Chen Y, Tan C, Jiang Y.
Eur J Med Chem (2017) 134 : 281 -292
PubMed 28419930 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.90 8.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4076931 1 8.33
CHEMBL4069152 1 8.28
CHEMBL4078380 1 8.15
CHEMBL98 VORINOSTAT 4.0 1 8.11
CHEMBL4093350 1 8.08
CHEMBL4102654 1 7.97
CHEMBL4075984 1 7.93
CHEMBL4068870 1 7.92
CHEMBL4067480 1 7.76
CHEMBL4069669 1 7.44
CHEMBL4087230 1 7.40
CHEMBL4089964 1 7.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4076931 IC50 = 4.68 nM 8.33
CHEMBL4069152 IC50 = 5.28 nM 8.28
CHEMBL4078380 IC50 = 7.1 nM 8.15
CHEMBL98 VORINOSTAT IC50 = 7.76 nM 8.11
CHEMBL4093350 IC50 = 8.35 nM 8.08
CHEMBL4102654 IC50 = 10.72 nM 7.97
CHEMBL4075984 IC50 = 11.87 nM 7.93
CHEMBL4068870 IC50 = 12.0 nM 7.92
CHEMBL4067480 IC50 = 17.39 nM 7.76
CHEMBL4069669 IC50 = 35.94 nM 7.44
CHEMBL4087230 IC50 = 39.93 nM 7.40
CHEMBL4089964 IC50 = 41.43 nM 7.38