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Assay Detail

CHEMBL4144353

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Binding
Inhibition of recombinant full length human C-terminal His/flag-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells after 30 mins by fluorescence assay
11
Total Activities
11
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 1 (CHEMBL325)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery.
Chen W, Dong G, Wu Y, Zhang W, Miao C, Sheng C.
ACS Med Chem Lett (2018) 9 : 34 -38
PubMed 29348808 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.41 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4170617 1 8.70
CHEMBL98 VORINOSTAT 4.0 1 7.58
CHEMBL4163681 1 7.44
CHEMBL4166793 1 7.44
CHEMBL4170109 1 7.36
CHEMBL4162202 1 7.34
CHEMBL4163345 1 7.22
CHEMBL4159972 1 7.04
CHEMBL4174058 1 7.02
CHEMBL4171570 1 7.00
CHEMBL566757 DAPORINAD 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4170617 IC50 = 2.0 nM 8.70
CHEMBL98 VORINOSTAT IC50 = 26.0 nM 7.58
CHEMBL4163681 IC50 = 36.0 nM 7.44
CHEMBL4166793 IC50 = 36.0 nM 7.44
CHEMBL4170109 IC50 = 44.0 nM 7.36
CHEMBL4162202 IC50 = 46.0 nM 7.34
CHEMBL4163345 IC50 = 60.0 nM 7.22
CHEMBL4159972 IC50 = 91.0 nM 7.04
CHEMBL4174058 IC50 = 95.0 nM 7.02
CHEMBL4171570 IC50 = 100.0 nM 7.00
CHEMBL566757 DAPORINAD IC50 - -