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Assay Detail

CHEMBL4310909

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

Binding
Inhibition of HDAC4 catalytic domain (648 to 1057 residues) (unknown origin) using Boc-Lys-TFA as substrate measured after 60 mins by fluorescence assay
20
Total Activities
20
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 4 (CHEMBL3524)
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 20 7.35 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4533107 1 7.77
CHEMBL4461062 1 7.66
CHEMBL4472392 1 7.66
CHEMBL4457713 1 7.66
CHEMBL4454327 1 7.60
CHEMBL4581271 1 7.60
CHEMBL4546422 1 7.60
CHEMBL4535902 1 7.52
CHEMBL4438812 1 7.51
CHEMBL4447877 1 7.48
CHEMBL4437833 1 7.44
CHEMBL4577004 1 7.40
CHEMBL4572214 1 7.31
CHEMBL4456445 1 7.27
CHEMBL4531880 1 7.26
CHEMBL4558414 1 7.24
CHEMBL4452941 1 6.99
CHEMBL4469204 1 6.92
CHEMBL396097 1 6.60
CHEMBL3110003 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4533107 IC50 = 17.0 nM 7.77
CHEMBL4461062 IC50 = 22.0 nM 7.66
CHEMBL4472392 IC50 = 22.0 nM 7.66
CHEMBL4457713 IC50 = 22.0 nM 7.66
CHEMBL4454327 IC50 = 25.0 nM 7.60
CHEMBL4581271 IC50 = 25.0 nM 7.60
CHEMBL4546422 IC50 = 25.0 nM 7.60
CHEMBL4535902 IC50 = 30.0 nM 7.52
CHEMBL4438812 IC50 = 31.0 nM 7.51
CHEMBL4447877 IC50 = 33.0 nM 7.48
CHEMBL4437833 IC50 = 36.0 nM 7.44
CHEMBL4577004 IC50 = 40.0 nM 7.40
CHEMBL4572214 IC50 = 49.0 nM 7.31
CHEMBL4456445 IC50 = 54.0 nM 7.27
CHEMBL4531880 IC50 = 55.0 nM 7.26
CHEMBL4558414 IC50 = 57.0 nM 7.24
CHEMBL4452941 IC50 = 103.0 nM 6.99
CHEMBL4469204 IC50 = 119.0 nM 6.92
CHEMBL396097 IC50 = 250.0 nM 6.60
CHEMBL3110003 IC50 = 330.0 nM 6.48