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Assay Detail

CHEMBL1921156

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

Binding
Inhibition of human recombinant HDAC8 using Fluor de Lys as substrate
10
Total Activities
10
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

Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
Neelarapu R, Holzle DL, Velaparthi S, Bai H, Brunsteiner M, Blond SY, Petukhov PA.
J Med Chem (2011) 54 : 4350 -4364
PubMed 21548582 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.65 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1914708 1 7.77
CHEMBL1914705 1 7.55
CHEMBL1914703 1 7.12
CHEMBL1914704 1 7.09
CHEMBL1914706 1 6.83
CHEMBL98 VORINOSTAT 4.0 1 6.36
CHEMBL1914707 1 6.31
CHEMBL1914702 1 6.19
CHEMBL1914701 1 6.15
CHEMBL585164 1 5.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1914708 IC50 = 17.0 nM 7.77
CHEMBL1914705 IC50 = 28.0 nM 7.55
CHEMBL1914703 IC50 = 76.0 nM 7.12
CHEMBL1914704 IC50 = 82.0 nM 7.09
CHEMBL1914706 IC50 = 147.0 nM 6.83
CHEMBL98 VORINOSTAT IC50 = 440.0 nM 6.36
CHEMBL1914707 IC50 = 487.0 nM 6.31
CHEMBL1914702 IC50 = 651.0 nM 6.19
CHEMBL1914701 IC50 = 707.0 nM 6.15
CHEMBL585164 IC50 = 7340.0 nM 5.13