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Assay Detail

CHEMBL3388102

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

Binding
Inhibition of full length C-terminal 6x-His tagged human HDAC3 using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay
6
Total Activities
6
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 3 (CHEMBL1829)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform.
Blackburn C, Barrett C, Brunson M, Chin J, England D, Garcia K, Gigstad K, Gould A, Gutierrez J, Hoar K, Rowland RS, Tsu C, Ringeling J, Wager K, Xu H.
Bioorg Med Chem Lett (2014) 24 : 5450 -5454
PubMed 25454270 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.53 6.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL98 VORINOSTAT 4.0 1 6.97
CHEMBL356769 TUBACIN 1 5.90
CHEMBL2431862 1 5.35
CHEMBL3353053 1 5.07
CHEMBL2431901 1 4.34
CHEMBL2018302 TUBASTATIN A 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL98 VORINOSTAT IC50 = 106.0 nM 6.97
CHEMBL356769 TUBACIN IC50 = 1270.0 nM 5.90
CHEMBL2431862 IC50 = 4500.0 nM 5.35
CHEMBL3353053 IC50 = 8500.0 nM 5.07
CHEMBL2431901 IC50 = 46000.0 nM 4.34
CHEMBL2018302 TUBASTATIN A IC50 > 30000.0 nM -