Table 1 Effect of LTA4H inhibitors to have entered the clinic and purportedly selective modulators on inhibition (IC50) of the epoxide hydrolase (LTB4 generation) and aminopeptidase (PGP degradation) activities of LTA4H in our assays, as described in Materials and methods.

From: The development of novel LTA4H modulators to selectively target LTB4 generation

Compound

Epoxide Hydrolase IC50 ± SEM (nM)

Aminopeptidase IC50 ± SEM (nM)

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110 ± 23.5

74 ± 7.3

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680 ± 10.0

150 ± 19.4

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9.0 ± 0.09

9.4 ± 1.3

48,900 ± 9,538

75,210 ± 9,752

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600 ± 66.2

9,110 ± 1,092

  1. IC50 curves were generated from 3 technical replicates at each concentration of test compound and at least 2 biological replicates. Results depicted as mean ± SEM.