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Assay Detail

CHEMBL4020989

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

Binding
Inhibition of recombinant human full length HDAC6 using Fluor-de-Lys as substrate after 60 mins by spectrofluorimetric analysis
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 6 (CHEMBL1865)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.
Mehndiratta S, Wang RS, Huang HL, Su CJ, Hsu CM, Wu YW, Pan SL, Liou JP.
Eur J Med Chem (2017) 134 : 13 -23
PubMed 28395150 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.81 8.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4065026 1 8.17
CHEMBL4069853 1 8.08
CHEMBL408513 BELINOSTAT 4.0 1 8.01
CHEMBL4080164 1 7.84
CHEMBL98 VORINOSTAT 4.0 1 6.96
CHEMBL27759 ENTINOSTAT 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4065026 IC50 = 6.8 nM 8.17
CHEMBL4069853 IC50 = 8.32 nM 8.08
CHEMBL408513 BELINOSTAT IC50 = 9.85 nM 8.01
CHEMBL4080164 IC50 = 14.4 nM 7.84
CHEMBL98 VORINOSTAT IC50 = 110.0 nM 6.96
CHEMBL27759 ENTINOSTAT IC50 > 10000.0 nM -