| 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 529647 | J 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 529647 | J 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 526991 | Bioorg 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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