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Assay Detail

CHEMBL3744289

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Binding
Inhibition of HDAC6 in human HeLa cells assessed as inhibition of tubulin deacetylation incubated for overnight by cELISA
5
Total Activities
5
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

Cross metathesis with hydroxamate and benzamide BOC-protected alkenes to access HDAC inhibitors and their biological evaluation highlighted intrinsic activity of BOC-protected dihydroxamates.
Zwick V, Nurisso A, Simões-Pires C, Bouchet S, Martinet N, Lehotzky A, Ovadi J, Cuendet M, Blanquart C, Bertrand P.
Bioorg Med Chem Lett (2016) 26 : 154 -159
PubMed 26611919 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 6.39 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99 TRICHOSTATIN 1.0 1 8.28
CHEMBL98 VORINOSTAT 4.0 1 7.66
CHEMBL320497 SUBEROHYDROXAMIC ACID 1 5.96
CHEMBL3739529 1 5.30
CHEMBL3740591 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99 TRICHOSTATIN EC50 = 5.2 nM 8.28
CHEMBL98 VORINOSTAT EC50 = 21.7 nM 7.66
CHEMBL320497 SUBEROHYDROXAMIC ACID EC50 = 1100.0 nM 5.96
CHEMBL3739529 EC50 = 5000.0 nM 5.30
CHEMBL3740591 EC50 = 17700.0 nM 4.75