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Assay Detail

CHEMBL4345638

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

Binding
Inhibition of HDAC4 (unknown origin) pre-incubated for 5 mins before fluorogenic substrate Boc-Lys (acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC addition and measured after 30 mins by fluorescence based assay
3
Total Activities
3
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 4 (CHEMBL3524)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Peptide Boronate Derivatives as Histone Deacetylase and Proteasome Dual Inhibitors for Overcoming Bortezomib Resistance of Multiple Myeloma.
Zhou Y, Liu X, Xue J, Liu L, Liang T, Li W, Yang X, Hou X, Fang H.
J Med Chem (2020) 63 : 4701 -4715
PubMed 32267687 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.55 4.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4576202 1 4.96
CHEMBL98 VORINOSTAT 4.0 1 4.13
CHEMBL4456886 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4576202 IC50 = 11100.0 nM 4.96
CHEMBL98 VORINOSTAT IC50 = 74000.0 nM 4.13
CHEMBL4456886 IC50 > 100000.0 nM -