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Assay Detail

CHEMBL4198677

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ADMET
Inhibition of HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors.
Zhao C, Zang J, Ding Q, Inks ES, Xu W, Chou CJ, Zhang Y.
Eur J Med Chem (2018) 150 : 282 -291
PubMed 29533873 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.23 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL98 VORINOSTAT 4.0 1 7.05
CHEMBL4206936 1 5.82
CHEMBL4218377 1 5.75
CHEMBL4218674 1 5.58
CHEMBL4214401 1 5.23
CHEMBL4210091 1 5.17
CHEMBL4206647 1 4.85
CHEMBL4211116 1 4.61
CHEMBL4213975 1 4.56
CHEMBL4202721 1 4.47
CHEMBL4218901 1 4.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL98 VORINOSTAT IC50 = 90.0 nM 7.05
CHEMBL4206936 IC50 = 1500.0 nM 5.82
CHEMBL4218377 IC50 = 1800.0 nM 5.75
CHEMBL4218674 IC50 = 2600.0 nM 5.58
CHEMBL4214401 IC50 = 5900.0 nM 5.23
CHEMBL4210091 IC50 = 6700.0 nM 5.17
CHEMBL4206647 IC50 = 14100.0 nM 4.85
CHEMBL4211116 IC50 = 24500.0 nM 4.61
CHEMBL4213975 IC50 = 27700.0 nM 4.56
CHEMBL4202721 IC50 = 34000.0 nM 4.47
CHEMBL4218901 IC50 = 40500.0 nM 4.39