rdf:type |
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lifeskim:mentions |
|
pubmed:issue |
8
|
pubmed:dateCreated |
2010-4-5
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pubmed:abstractText |
Starting from an initial HTS screening lead, a novel series of C(5)-substituted diaryl pyrazoles were developed that showed potent inhibition of p38alpha kinase. Key to this outcome was the switch from a pyridyl to pyrimidine at the C(4)-position leading to analogs that were potent in human whole blood based cell assay as well as in a number of animal efficacy models for rheumatoid arthritis. Ultimately, we identified a clinical candidate from this substrate; SD-0006.
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pubmed:language |
eng
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pubmed:journal |
|
pubmed:citationSubset |
IM
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pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Apr
|
pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BensonAlan GAG,
pubmed-author:DevrajRajesh VRV,
pubmed-author:DiceTomT,
pubmed-author:FlynnDaniel LDL,
pubmed-author:HepperleMichael EME,
pubmed-author:KimTinaT,
pubmed-author:KurambailRaviR,
pubmed-author:LindmarkR JRJ,
pubmed-author:MessingDean MDM,
pubmed-author:MonahanJoseph BJB,
pubmed-author:NaingWinW,
pubmed-author:PortanovaJosephJ,
pubmed-author:SelnessShaun RSR,
pubmed-author:ShiehHueyH,
pubmed-author:WalkerJohn KJK,
pubmed-author:YangSyaulanS
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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
|
pubmed:volume |
20
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
2634-8
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pubmed:meshHeading |
|
pubmed:year |
2010
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pubmed:articleTitle |
Identification of SD-0006, a potent diaryl pyrazole inhibitor of p38 MAP kinase.
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pubmed:affiliation |
Pfizer Global Research and Development, St. Louis, MO 63017, USA. jkwalker24@sbcglobal.net
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pubmed:publicationType |
Journal Article
|