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Assay Detail

CHEMBL5059550

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Binding
HyPerBlu POAX enzymatic assay
2
Total Activities
2
Compounds Tested
1
Activity Types
3
Assay Parameters

Assay Information

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

Target

Peroxisomal N(1)-acetyl-spermine/spermidine oxidase (CHEMBL2105)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Data for DCP probe JNJ-9350
SGC Frankfurt
(2022)
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.89 6.10

Assay Parameters

Parameter Type Value Units Text
Additional information Additional information - In this assay Polyamine Oxidase catalyzes the formation of spermidine, 3-acetamidopropanal and hydrogen peroxide using oxygen and N1-acetylspermine as substrates. The addition of 25 µM chlorhexidine compound mixed with the Lumigen HyPerBlu reagent is added to quench the reaction and directly react with hydrogen peroxide, respectively, to generate a chemiluminescence signal measured on the BMG PHERAStar plate reader.
Assay publication Assay publication - Slide 27-37 in JNJ-9350 Inhibitor for SMOX.pdf
Target protein length Target protein length - full length human PAOX with N-terminal his tag

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5094181 1 6.10
CHEMBL5092747 1 5.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5094181 IC50 = 790.0 nM 6.10
CHEMBL5092747 IC50 = 2100.0 nM 5.68