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Assay Detail

CHEMBL4685853

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

Binding
Inhibition of recombinant human C-terminal His-tagged HDAC2 (1 to 488 residues) expressed in Sf9 insect cells using fluor de lys SIRT1 as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay
3
Total Activities
3
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 2 (CHEMBL1937)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease.
Tseng HJ,Lin MH,Shiao YJ,Yang YC,Chu JC,Chen CY,Chen YY,Lin TE,Su CJ,Pan SL,Chen LC,Wang CY,Hsu KC,Huang WJ
Eur J Med Chem (2020) 192 : 112193 -112193
PubMed 32151835 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.39 7.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL98 VORINOSTAT 4.0 1 7.04
CHEMBL4796066 1 6.32
CHEMBL4762873 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL98 VORINOSTAT IC50 = 91.0 nM 7.04
CHEMBL4796066 IC50 = 480.0 nM 6.32
CHEMBL4762873 IC50 = 1570.0 nM 5.80