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Assay Detail

CHEMBL4683033

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

Binding
Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using Boc-Lys (Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone deacetylase 1 (CHEMBL325)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
Huang M,Xie X,Gong P,Wei Y,Du H,Xu Y,Xu Q,Jing Y,Zhao L
Eur J Med Chem (2020) 188 : 111991 -111991
PubMed 31883490 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.51 7.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL98 VORINOSTAT 4.0 1 7.42
CHEMBL4749523 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL98 VORINOSTAT IC50 = 38.0 nM 7.42
CHEMBL4749523 IC50 = 2512.0 nM 5.60