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Assay Detail

CHEMBL4828683

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

Binding
Inhibition of recombinant human ful length N-terminal GST-tagged HDAC5 expressed in baculovirus expression system using Nepsilon-Trifluoroacetyl L-lysine as substrate by fluorescent microplate reader assay
4
Total Activities
4
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 5 (CHEMBL2563)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Role of Fluorination in the Histone Deacetylase 6 (HDAC6) Selectivity of Benzohydroxamate-Based Inhibitors.
Sandrone G, Cukier CD, Zrubek K, Marchini M, Vergani B, Caprini G, Fossati G, Steinkühler C, Stevenazzi A.
ACS Med Chem Lett (2021) 12 : 1810 -1817
PubMed 34795871 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.68 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4862563 1 6.16
CHEMBL4448410 1 5.69
CHEMBL4470373 1 5.55
CHEMBL4453121 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4862563 IC50 = 699.0 nM 6.16
CHEMBL4448410 IC50 = 2035.0 nM 5.69
CHEMBL4470373 IC50 = 2788.0 nM 5.55
CHEMBL4453121 IC50 = 4999.0 nM 5.30