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rdf:type |
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lifeskim:mentions |
umls-concept:C0039859,
umls-concept:C0220781,
umls-concept:C0243077,
umls-concept:C0599532,
umls-concept:C1150587,
umls-concept:C1367731,
umls-concept:C1527178,
umls-concept:C1705632,
umls-concept:C1705938,
umls-concept:C1707689,
umls-concept:C1883254
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pubmed:issue |
24
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pubmed:dateCreated |
2010-11-24
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pubmed:abstractText |
From high throughput screening, we discovered compound 1, the prototype for a series of disubstituted thiophene inhibitors of JNK which is selective towards closely related MAP kinases p38 and Erk2. Herein we describe the evolution of these compounds to a novel class of thiophene and thiazole JNK inhibitors that retain favorable solubility, permeability, and P-gp properties for development as CNS agents for treatment of neurodegeneration. Compound 61 demonstrated JNK3 IC(50)=77 nM and retained the excellent broad kinase selectivity observed for the series.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:ArtisDean RDR,
pubmed-author:BardFrédériqueF,
pubmed-author:BowersSimeonS,
pubmed-author:BrogleyLouisL,
pubmed-author:FangLarryL,
pubmed-author:Griswold-PrennerIreneI,
pubmed-author:HomRoy KRK,
pubmed-author:KonradiAndrei WAW,
pubmed-author:NauRR,
pubmed-author:NeitzR JeffreyRJ,
pubmed-author:NeitzelMartin LML,
pubmed-author:PowellKyleK,
pubmed-author:ProbstGary DGD,
pubmed-author:QuinnKevinK,
pubmed-author:SauerJohn-MichaelJM,
pubmed-author:SealyJennifer MJM,
pubmed-author:ShamHing LHL,
pubmed-author:TóthGergelyG,
pubmed-author:TruongAnh PAP,
pubmed-author:WuJingJ,
pubmed-author:YaoNanhuaN,
pubmed-author:YednockTed ATA,
pubmed-author:ZhaoRenR
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pubmed:copyrightInfo |
Copyright © 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
7303-7
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pubmed:meshHeading |
pubmed-meshheading:21071223-Animals,
pubmed-meshheading:21071223-Drug Design,
pubmed-meshheading:21071223-Humans,
pubmed-meshheading:21071223-JNK Mitogen-Activated Protein Kinases,
pubmed-meshheading:21071223-Mice,
pubmed-meshheading:21071223-Microsomes, Liver,
pubmed-meshheading:21071223-Mitogen-Activated Protein Kinase 10,
pubmed-meshheading:21071223-Mitogen-Activated Protein Kinase 8,
pubmed-meshheading:21071223-Protein Kinase Inhibitors,
pubmed-meshheading:21071223-Quinolines,
pubmed-meshheading:21071223-Structure-Activity Relationship,
pubmed-meshheading:21071223-Thiazoles,
pubmed-meshheading:21071223-Thiophenes
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pubmed:year |
2010
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pubmed:articleTitle |
Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK.
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pubmed:affiliation |
Department of Chemical Sciences, Elan Pharmaceuticals, South San Francisco, CA 94080, USA. roy.hom@elan.com
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pubmed:publicationType |
Journal Article
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