Target Validation Information
Target ID T07173
Target Name Neurotrophic tyrosine kinase receptor 1
Target Type
Clinical Trial
Drug Potency against Target CEP-6331 Drug Info IC50 = 1055 nM [529647]
CEP-5104 Drug Info IC50 = 1270 nM [529647]
GW-5074 Drug Info IC50 = 4700 nM [526991]
The Effect of Target Knockout, Knockdown or Genetic Variations AD-like neurodegeneration, including cortical atrophy, memory deficits and amyloid deposits (NGF knockdown); hippocampal cholinergic defects and reduced memory acquisition and retention(NGF knock of one allele of a gene) [529647]
References
Ref 529647J Med Chem. 2008 Sep 25;51(18):5680-9. Epub 2008 Aug 21.Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models.
Ref 529647J Med Chem. 2008 Sep 25;51(18):5680-9. Epub 2008 Aug 21.Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models.
Ref 526991Bioorg Med Chem Lett. 2004 Feb 23;14(4):953-7.Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles.

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