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Assay Detail

CHEMBL2433166

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

Binding
Inhibition of HDAC6 in human HeLa cells using acetyl tubulin as substrate assessed as Ac-Lys accumulation in nuclear histones after 6 hrs by immunofluorescence assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HeLa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone deacetylase 6 (CHEMBL1865)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent histone deacetylase inhibitors derived from 4-(aminomethyl)-N-hydroxybenzamide with high selectivity for the HDAC6 isoform.
Blackburn C, Barrett C, Chin J, Garcia K, Gigstad K, Gould A, Gutierrez J, Harrison S, Hoar K, Lynch C, Rowland RS, Tsu C, Ringeling J, Xu H.
J Med Chem (2013) 56 : 7201 -7211
PubMed 23964961 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.33 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2431916 1 8.30
CHEMBL2431919 1 7.75
CHEMBL2431918 1 7.30
CHEMBL2431917 1 6.80
CHEMBL2431921 1 6.79
CHEMBL2431920 1 6.75
CHEMBL2431901 1 6.68
CHEMBL2431905 1 6.47
CHEMBL2431906 1 6.47
CHEMBL2431902 1 6.37
CHEMBL2431862 1 6.34
CHEMBL2431903 1 6.27
CHEMBL2431907 1 6.25
CHEMBL2431909 1 6.24
CHEMBL2431904 1 5.89
CHEMBL2431912 1 5.83
CHEMBL2431908 1 5.82
CHEMBL2431910 1 5.70
CHEMBL2431911 1 5.58
CHEMBL356769 TUBACIN 1 5.54
CHEMBL2431914 1 5.54
CHEMBL2431915 1 5.51
CHEMBL2431913 1 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2431916 IC50 = 5.0 nM 8.30
CHEMBL2431919 IC50 = 18.0 nM 7.75
CHEMBL2431918 IC50 = 50.0 nM 7.30
CHEMBL2431917 IC50 = 158.0 nM 6.80
CHEMBL2431921 IC50 = 162.0 nM 6.79
CHEMBL2431920 IC50 = 177.0 nM 6.75
CHEMBL2431901 IC50 = 210.0 nM 6.68
CHEMBL2431905 IC50 = 340.0 nM 6.47
CHEMBL2431906 IC50 = 340.0 nM 6.47
CHEMBL2431902 IC50 = 430.0 nM 6.37
CHEMBL2431862 IC50 = 460.0 nM 6.34
CHEMBL2431903 IC50 = 540.0 nM 6.27
CHEMBL2431907 IC50 = 560.0 nM 6.25
CHEMBL2431909 IC50 = 580.0 nM 6.24
CHEMBL2431904 IC50 = 1300.0 nM 5.89
CHEMBL2431912 IC50 = 1480.0 nM 5.83
CHEMBL2431908 IC50 = 1510.0 nM 5.82
CHEMBL2431910 IC50 = 2000.0 nM 5.70
CHEMBL2431911 IC50 = 2600.0 nM 5.58
CHEMBL356769 TUBACIN IC50 = 2900.0 nM 5.54
CHEMBL2431914 IC50 = 2900.0 nM 5.54
CHEMBL2431915 IC50 = 3090.0 nM 5.51
CHEMBL2431913 IC50 = 3680.0 nM 5.43