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Assay Detail

CHEMBL5325200

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

Binding
Binding affinity to C-terminal His-tagged human HDAC2 (2 to 488 residues) in transfected in baculovirus infected Sf9 cells assessed as dissociation constant
5
Total Activities
5
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 2 (CHEMBL1937)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Evolution of Slow-Binding Inhibitors Targeting Histone Deacetylase Isoforms.
Mukherjee A, Zamani F, Suzuki T.
J Med Chem (2023) 66 : 11672 -11700
PubMed 37651268 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 5 7.26 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99 TRICHOSTATIN 1.0 1 7.92
CHEMBL470791 1 7.60
CHEMBL235842 1 7.42
CHEMBL98 VORINOSTAT 4.0 1 6.79
CHEMBL27759 ENTINOSTAT 3.0 1 6.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99 TRICHOSTATIN Kd = 12.0 nM 7.92
CHEMBL470791 Kd = 25.0 nM 7.60
CHEMBL235842 Kd = 38.0 nM 7.42
CHEMBL98 VORINOSTAT Kd = 163.0 nM 6.79
CHEMBL27759 ENTINOSTAT Kd = 282.0 nM 6.55