| pubmed-article:19591487 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:19591487 | lifeskim:mentions | umls-concept:C0020924 | lld:lifeskim |
| pubmed-article:19591487 | lifeskim:mentions | umls-concept:C0054846 | lld:lifeskim |
| pubmed-article:19591487 | lifeskim:mentions | umls-concept:C0257535 | lld:lifeskim |
| pubmed-article:19591487 | lifeskim:mentions | umls-concept:C0243077 | lld:lifeskim |
| pubmed-article:19591487 | lifeskim:mentions | umls-concept:C1554184 | lld:lifeskim |
| pubmed-article:19591487 | pubmed:issue | 23 | lld:pubmed |
| pubmed-article:19591487 | pubmed:dateCreated | 2009-12-3 | lld:pubmed |
| pubmed-article:19591487 | pubmed:abstractText | In this study, we report on the discovery of isoxazole 1 as a potent dual inhibitor of p38alpha (IC(50) = 0.45 microM) and CK1delta (IC(50) = 0.23 microM). Because only a few effective small molecule inhibitors of CK1 have been described so far, we aimed to develop this structural class toward specific agents. Molecular modeling studies comparing p38alpha/CK1delta suggested an optimization strategy leading to design, synthesis, biological characterization, and SAR of highly potent compounds including 9 (IC(50) p38alpha = 0.006 microM; IC(50) CK1delta = 1.6 microM), 13 (IC(50) p38alpha = 2.52 microM; IC(50) CK1delta = 0.033 microM), 17 (IC(50) p38alpha = 0.019 microM; IC(50) CK1delta = 0.004 microM; IC(50) CK1epsilon = 0.073 microM), and 18 (CKP138) (IC(50) p38alpha = 0.041 microM; IC(50) CK1delta = 0.005 microM; IC(50) CK1epsilon = 0.447 microM) possessing differentiated specificity. Selected compounds were profiled over 76 kinases and evaluation of their cellular efficacy showed 18 (CKP138) to be a highly potent and dual-specific inhibitor of CK1delta and p38alpha. | lld:pubmed |
| pubmed-article:19591487 | pubmed:language | eng | lld:pubmed |
| pubmed-article:19591487 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19591487 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:19591487 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19591487 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19591487 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19591487 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19591487 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19591487 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19591487 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19591487 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:19591487 | pubmed:month | Dec | lld:pubmed |
| pubmed-article:19591487 | pubmed:issn | 1520-4804 | lld:pubmed |
| pubmed-article:19591487 | pubmed:author | pubmed-author:LauferStefanS | lld:pubmed |
| pubmed-article:19591487 | pubmed:author | pubmed-author:KnippschildUw... | lld:pubmed |
| pubmed-article:19591487 | pubmed:author | pubmed-author:PeiferChristi... | lld:pubmed |
| pubmed-article:19591487 | pubmed:author | pubmed-author:AbadlehMohamm... | lld:pubmed |
| pubmed-article:19591487 | pubmed:author | pubmed-author:HirnerHeidrun... | lld:pubmed |
| pubmed-article:19591487 | pubmed:author | pubmed-author:HauserDominik... | lld:pubmed |
| pubmed-article:19591487 | pubmed:author | pubmed-author:SchattelVeren... | lld:pubmed |
| pubmed-article:19591487 | pubmed:author | pubmed-author:BischofJoachi... | lld:pubmed |
| pubmed-article:19591487 | pubmed:issnType | Electronic | lld:pubmed |
| pubmed-article:19591487 | pubmed:day | 10 | lld:pubmed |
| pubmed-article:19591487 | pubmed:volume | 52 | lld:pubmed |
| pubmed-article:19591487 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:19591487 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:19591487 | pubmed:pagination | 7618-30 | lld:pubmed |
| pubmed-article:19591487 | pubmed:meshHeading | pubmed-meshheading:19591487... | lld:pubmed |
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| pubmed-article:19591487 | pubmed:meshHeading | pubmed-meshheading:19591487... | lld:pubmed |
| pubmed-article:19591487 | pubmed:year | 2009 | lld:pubmed |
| pubmed-article:19591487 | pubmed:articleTitle | 3,4-Diaryl-isoxazoles and -imidazoles as potent dual inhibitors of p38alpha mitogen activated protein kinase and casein kinase 1delta. | lld:pubmed |
| pubmed-article:19591487 | pubmed:affiliation | Department of Pharmacy, Eberhard-Karls-University, Auf der Morgenstelle 8, D-72076 Tuebingen, Germany. Peifer@uni-tuebingen.de | lld:pubmed |
| pubmed-article:19591487 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:19591487 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:19591487 | lld:chembl |
