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Assay Detail

CHEMBL2318993

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

Binding
Inhibition of human HDAC8 by fluorescence assay
5
Total Activities
5
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 8 (CHEMBL3192)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
Marek L, Hamacher A, Hansen FK, Kuna K, Gohlke H, Kassack MU, Kurz T.
J Med Chem (2013) 56 : 427 -436
PubMed 23252603 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.14 6.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99 TRICHOSTATIN 1.0 1 6.71
CHEMBL2312167 1 6.08
CHEMBL98 VORINOSTAT 4.0 1 6.02
CHEMBL2312164 1 5.98
CHEMBL2312168 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99 TRICHOSTATIN IC50 = 196.0 nM 6.71
CHEMBL2312167 IC50 = 833.0 nM 6.08
CHEMBL98 VORINOSTAT IC50 = 960.0 nM 6.02
CHEMBL2312164 IC50 = 1043.0 nM 5.98
CHEMBL2312168 IC50 = 1278.0 nM 5.89