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Table 2 Screening for target and off target effects

From: The neurotrophic compound J147 reverses cognitive impairment in aged Alzheimer's disease mice

Screen

Company

Lead Profile Screen (60 CNS receptors/transporters)

Ricerca-MDS

Protein Kinase Screen (50 kinases - activity)

Nova Screen

Protein Kinase (352 kinases - binding)

Ambit

All phosphatases (Tyr and Ser/Thr)

Caliper

Known proteases

Caliper and Ricerca

Deubiquitinases, Esterases, Secretases, Caspases

Caliper

5-, 12-, 15-LOX, COX-1 and 2, NADPH oxidase

MDS

Deacetylase, Sirtuin SIRT-1, -2, -3, Proteasome, MAO A and B

Ricerca

All phosphodiesterases and 5-CYPs

MDS

  1. Various CROs screened a wide variety of potential targets at 10 μM J147 with no significant reproducible inhibition above 60% except for monoamine oxidase B (MAO B) and the dopamine transporter.