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Assay Detail

CHEMBL4390493

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

Binding
Inhibition of recombinant human full-length C-terminal FLAG-tagged HDAC1 expressed in baculovirus expression system using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition by fluorescence assay
23
Total Activities
23
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 1 (CHEMBL325)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2.
Yu Y, Ran D, Jiang J, Pan T, Dan Y, Tang Q, Li W, Zhang L, Gan L, Gan Z.
Bioorg Med Chem Lett (2019) 29 : 2136 -2140
PubMed 31272794 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 8.54 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL483254 PANOBINOSTAT 4.0 1 9.22
CHEMBL4549278 1 8.24
CHEMBL4476140 1 8.15
CHEMBL4558240 1 -
CHEMBL4467203 1 -
CHEMBL4437857 1 -
CHEMBL4554150 1 -
CHEMBL4465985 1 -
CHEMBL4519918 1 -
CHEMBL4454438 1 -
CHEMBL4539693 1 -
CHEMBL4578621 1 -
CHEMBL4448341 1 -
CHEMBL4569947 1 -
CHEMBL4531989 1 -
CHEMBL4532028 1 -
CHEMBL4513637 1 -
CHEMBL4445944 1 -
CHEMBL4545344 1 -
CHEMBL4450509 1 -
CHEMBL98 VORINOSTAT 4.0 1 -
CHEMBL14762 SELICICLIB 2.0 1 -
CHEMBL4466310 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL483254 PANOBINOSTAT IC50 = 0.6 nM 9.22
CHEMBL4549278 IC50 = 5.8 nM 8.24
CHEMBL4476140 IC50 = 7.0 nM 8.15
CHEMBL4558240 IC50 - -
CHEMBL4467203 IC50 - -
CHEMBL4437857 IC50 - -
CHEMBL4554150 IC50 - -
CHEMBL4465985 IC50 - -
CHEMBL4519918 IC50 - -
CHEMBL4454438 IC50 - -
CHEMBL4539693 IC50 - -
CHEMBL4578621 IC50 - -
CHEMBL4448341 IC50 - -
CHEMBL4569947 IC50 - -
CHEMBL4531989 IC50 - -
CHEMBL4532028 IC50 - -
CHEMBL4513637 IC50 - -
CHEMBL4445944 IC50 - -
CHEMBL4545344 IC50 - -
CHEMBL4450509 IC50 - -
CHEMBL98 VORINOSTAT IC50 - -
CHEMBL14762 SELICICLIB IC50 - -
CHEMBL4466310 IC50 - -