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Table 1 Activity and selectivity of PXS-4728A in vitro

From: Effects of an anti-inflammatory VAP-1/SSAO inhibitor, PXS-4728A, on pulmonary neutrophil migration

Assay

IC 50

 

Recombinant human VAP-1/SSAO (AOC3)

5 nM

 

Gonadal fat tissue homogenate; mouse, rat, dog, rabbit

<10 nM

 

Assay

IC 50

Selectivity

Recombinant diamine oxidase (AOC1)

12.0 μM

>2000x

Recombinant retina specific amine oxidase (AOC2)

2.76 μM

>500x

Purified lysyl oxidase from lung fibroblasts

13.2 μM

>2000x

Recombinant lysyl oxidase like 2

10.4 μM

>2000x

Recombinant monoamine oxidase A

>100 μM

>2000x

Recombinant monoamine oxidase B

2.7 μM

>500x

Recombinant lysine demethylase

>10 μM

>2000x