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Assay Detail

CHEMBL4685847

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

Binding
Inhibition of recombinant human C-terminal His-tagged HDAC9 (604 to 1066 residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC 2A substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay
13
Total Activities
13
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 9 (CHEMBL4145)
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 13 5.23 6.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4757035 1 6.28
CHEMBL4762873 1 6.24
CHEMBL4761847 1 5.90
CHEMBL4753795 1 5.30
CHEMBL4796066 1 5.26
CHEMBL4757768 1 5.19
CHEMBL4753828 1 4.91
CHEMBL4752558 1 4.88
CHEMBL4248676 1 4.54
CHEMBL4751082 1 4.51
CHEMBL98 VORINOSTAT 4.0 1 4.49
CHEMBL4750838 1 -
CHEMBL4799871 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4757035 IC50 = 520.0 nM 6.28
CHEMBL4762873 IC50 = 570.0 nM 6.24
CHEMBL4761847 IC50 = 1250.0 nM 5.90
CHEMBL4753795 IC50 = 4950.0 nM 5.30
CHEMBL4796066 IC50 = 5510.0 nM 5.26
CHEMBL4757768 IC50 = 6420.0 nM 5.19
CHEMBL4753828 IC50 = 12180.0 nM 4.91
CHEMBL4752558 IC50 = 13230.0 nM 4.88
CHEMBL4248676 IC50 = 28960.0 nM 4.54
CHEMBL4751082 IC50 = 31100.0 nM 4.51
CHEMBL98 VORINOSTAT IC50 = 32260.0 nM 4.49
CHEMBL4750838 IC50 > 40000.0 nM -
CHEMBL4799871 IC50 > 40000.0 nM -