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Assay Detail

CHEMBL4326249

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

Binding
Inhibition of human recombinant HDAC6 after 30 mins using fluorogenic substrate by fluorimetric assay
9
Total Activities
9
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

Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4.
Lamaa D, Lin HP, Zig L, Bauvais C, Bollot G, Bignon J, Levaique H, Pamlard O, Dubois J, Ouaissi M, Souce M, Kasselouri A, Saller F, Borgel D, Jayat-Vignoles C, Al-Mouhammad H, Feuillard J, Benihoud K, Alami M, Hamze A.
J Med Chem (2018) 61 : 6574 -6591
PubMed 30004697 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.67 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99 TRICHOSTATIN 1.0 1 7.82
CHEMBL2170177 1 5.51
CHEMBL4460757 1 5.42
CHEMBL4517272 1 5.30
CHEMBL4448903 1 5.16
CHEMBL4542119 1 4.82
CHEMBL4452476 1 -
CHEMBL498271 1 -
CHEMBL96051 SCRIPTAID 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99 TRICHOSTATIN IC50 = 15.0 nM 7.82
CHEMBL2170177 IC50 = 3100.0 nM 5.51
CHEMBL4460757 IC50 = 3800.0 nM 5.42
CHEMBL4517272 IC50 = 5000.0 nM 5.30
CHEMBL4448903 IC50 = 6900.0 nM 5.16
CHEMBL4542119 IC50 = 15000.0 nM 4.82
CHEMBL4452476 IC50 - -
CHEMBL498271 IC50 - -
CHEMBL96051 SCRIPTAID IC50 - -