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Assay Detail

CHEMBL971412

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

Binding
Inhibition of human recombinant HDAC6
14
Total Activities
14
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

Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity.
Tapadar S, He R, Luchini DN, Billadeau DD, Kozikowski AP.
Bioorg Med Chem Lett (2009) 19 : 3023 -3026
PubMed 19419863 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.93 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL511212 1 8.52
CHEMBL468935 1 8.52
CHEMBL512644 1 8.30
CHEMBL98 VORINOSTAT 4.0 1 7.85
CHEMBL511715 1 7.29
CHEMBL469134 1 7.17
CHEMBL511432 1 7.09
CHEMBL468527 1 6.05
CHEMBL466459 1 5.77
CHEMBL466171 1 4.91
CHEMBL507592 1 4.77
CHEMBL466031 1 -
CHEMBL466032 1 -
CHEMBL466033 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL511212 IC50 = 3.0 nM 8.52
CHEMBL468935 IC50 = 3.0 nM 8.52
CHEMBL512644 IC50 = 5.0 nM 8.30
CHEMBL98 VORINOSTAT IC50 = 14.0 nM 7.85
CHEMBL511715 IC50 = 51.0 nM 7.29
CHEMBL469134 IC50 = 68.0 nM 7.17
CHEMBL511432 IC50 = 82.0 nM 7.09
CHEMBL468527 IC50 = 885.0 nM 6.05
CHEMBL466459 IC50 = 1710.0 nM 5.77
CHEMBL466171 IC50 = 12300.0 nM 4.91
CHEMBL507592 IC50 = 17100.0 nM 4.77
CHEMBL466031 IC50 > 30000.0 nM -
CHEMBL466032 IC50 > 30000.0 nM -
CHEMBL466033 IC50 > 30000.0 nM -