| pubmed-article:19574047 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:19574047 | lifeskim:mentions | umls-concept:C0226896 | lld:lifeskim |
| pubmed-article:19574047 | lifeskim:mentions | umls-concept:C0205531 | lld:lifeskim |
| pubmed-article:19574047 | lifeskim:mentions | umls-concept:C0442027 | lld:lifeskim |
| pubmed-article:19574047 | lifeskim:mentions | umls-concept:C1527415 | lld:lifeskim |
| pubmed-article:19574047 | lifeskim:mentions | umls-concept:C0034242 | lld:lifeskim |
| pubmed-article:19574047 | lifeskim:mentions | umls-concept:C0257535 | lld:lifeskim |
| pubmed-article:19574047 | lifeskim:mentions | umls-concept:C1261322 | lld:lifeskim |
| pubmed-article:19574047 | lifeskim:mentions | umls-concept:C0038477 | lld:lifeskim |
| pubmed-article:19574047 | lifeskim:mentions | umls-concept:C0470187 | lld:lifeskim |
| pubmed-article:19574047 | lifeskim:mentions | umls-concept:C1708111 | lld:lifeskim |
| pubmed-article:19574047 | lifeskim:mentions | umls-concept:C0243077 | lld:lifeskim |
| pubmed-article:19574047 | pubmed:issue | 16 | lld:pubmed |
| pubmed-article:19574047 | pubmed:dateCreated | 2009-7-29 | lld:pubmed |
| pubmed-article:19574047 | pubmed:abstractText | A novel class of fused pyrazole-derived inhibitors of p38alpha mitogen-activated protein kinase (MAPK) is disclosed. These inhibitors were evaluated for their ability to inhibit the p38alpha enzyme, the secretion of TNFalpha in a LPS-challenged THP1 cell line and TNFalpha-induced production of IL-8 in 50% human whole blood. This series was optimized through a SAR investigation to provide inhibitors with IC(50) values in the low single-digit nanomolar range in whole blood. Further investigation of their pharmacokinetic profiles led to the identification of two potent and orally bioavailable p38 inhibitors 10 m and 10 q. Inhibitor 10 m was found to be efficacious in vivo in the inhibition of TNFalpha production in LPS-stimulated Lewis rats with an ED(50) of 0.1mg/kg while 10 q was found to have an ED(50) of 0.05-0.07 mg/kg. | lld:pubmed |
| pubmed-article:19574047 | pubmed:language | eng | lld:pubmed |
| pubmed-article:19574047 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19574047 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:19574047 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19574047 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19574047 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19574047 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19574047 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19574047 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19574047 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19574047 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19574047 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:19574047 | pubmed:month | Aug | lld:pubmed |
| pubmed-article:19574047 | pubmed:issn | 1464-3405 | lld:pubmed |
| pubmed-article:19574047 | pubmed:author | pubmed-author:HsiehFayeF | lld:pubmed |
| pubmed-article:19574047 | pubmed:author | pubmed-author:McBrideHelenH | lld:pubmed |
| pubmed-article:19574047 | pubmed:author | pubmed-author:WurzRyan PRP | lld:pubmed |
| pubmed-article:19574047 | pubmed:author | pubmed-author:MohrChristoph... | lld:pubmed |
| pubmed-article:19574047 | pubmed:author | pubmed-author:TaskerAndrew... | lld:pubmed |
| pubmed-article:19574047 | pubmed:author | pubmed-author:XuShiminS | lld:pubmed |
| pubmed-article:19574047 | pubmed:author | pubmed-author:LeeMatthew... | lld:pubmed |
| pubmed-article:19574047 | pubmed:author | pubmed-author:SarisChristia... | lld:pubmed |
| pubmed-article:19574047 | pubmed:author | pubmed-author:WongLu MinLM | lld:pubmed |
| pubmed-article:19574047 | pubmed:author | pubmed-author:HenkleBradley... | lld:pubmed |
| pubmed-article:19574047 | pubmed:author | pubmed-author:PlantMatthewM | lld:pubmed |
| pubmed-article:19574047 | pubmed:author | pubmed-author:PettusLiping... | lld:pubmed |
| pubmed-article:19574047 | pubmed:author | pubmed-author:ShermanLisaL | lld:pubmed |
| pubmed-article:19574047 | pubmed:author | pubmed-author:MinerKentK | lld:pubmed |
| pubmed-article:19574047 | pubmed:author | pubmed-author:ChmaitSamerS | lld:pubmed |
| pubmed-article:19574047 | pubmed:issnType | Electronic | lld:pubmed |
| pubmed-article:19574047 | pubmed:day | 15 | lld:pubmed |
| pubmed-article:19574047 | pubmed:volume | 19 | lld:pubmed |
| pubmed-article:19574047 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:19574047 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:19574047 | pubmed:pagination | 4724-8 | lld:pubmed |
| pubmed-article:19574047 | pubmed:dateRevised | 2009-11-19 | lld:pubmed |
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| pubmed-article:19574047 | pubmed:meshHeading | pubmed-meshheading:19574047... | lld:pubmed |
| pubmed-article:19574047 | pubmed:year | 2009 | lld:pubmed |
| pubmed-article:19574047 | pubmed:articleTitle | Part 1: Structure-Activity Relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase. | lld:pubmed |
| pubmed-article:19574047 | pubmed:affiliation | Department of Chemistry Research & Discovery, Amgen Inc, Thousand Oaks, CA 91320, USA. rwurz@amgen.com | lld:pubmed |
| pubmed-article:19574047 | pubmed:publicationType | Journal Article | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:19574047 | lld:chembl |
