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Assay Detail

CHEMBL4310908

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

Binding
Inhibition of human C-terminal His-tagged HDAC5 catalytic domain (656 to 1122 residues) expressed in baculovirus infected Sf9 insect cells using Boc-Lys-TFA as substrate measured after 60 mins by fluorescence assay
4
Total Activities
4
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 5 (CHEMBL2563)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development and characterization of a CNS-penetrant benzhydryl hydroxamic acid class IIa histone deacetylase inhibitor.
Luckhurst CA, Aziz O, Beaumont V, Bürli RW, Breccia P, Maillard MC, Haughan AF, Lamers M, Leonard P, Matthews KL, Raphy G, Stott AJ, Munoz-Sanjuan I, Thomas B, Wall M, Wishart G, Yates D, Dominguez C.
Bioorg Med Chem Lett (2019) 29 : 83 -88
PubMed 30463802 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.16 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4437833 1 7.80
CHEMBL4456445 1 7.22
CHEMBL3110003 1 6.82
CHEMBL396097 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4437833 IC50 = 16.0 nM 7.80
CHEMBL4456445 IC50 = 60.0 nM 7.22
CHEMBL3110003 IC50 = 150.0 nM 6.82
CHEMBL396097 IC50 = 160.0 nM 6.80