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Assay Detail

CHEMBL4330052

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

Binding
Inhibition of full length human N-terminal FLAG-tagged HDAC8 (1 to 377 residues) expressed in HEK293 cells preincubated for 15 mins followed by Boc-[trifluoroacetyl-Lys]-AMC substrate addition measured after 30 mins by fluorimetric method
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone deacetylase 8 (CHEMBL3192)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Molecular Basis for the Selective Inhibition of Histone Deacetylase 6 by a Mercaptoacetamide Inhibitor.
Porter NJ, Shen S, Barinka C, Kozikowski AP, Christianson DW.
ACS Med Chem Lett (2018) 9 : 1301 -1305
PubMed 30613344 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.55 6.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL98 VORINOSTAT 4.0 1 6.17
CHEMBL4065147 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL98 VORINOSTAT IC50 = 669.0 nM 6.17
CHEMBL4065147 IC50 = 12000.0 nM 4.92