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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
16
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pubmed:dateCreated |
2006-7-17
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pubmed:abstractText |
A series of 2-pyrimidyl-5-amidothiophenes has been synthesized and evaluated for AKT inhibition. SAR studies resulted in potent inhibitors of AKT with IC(50) values as low as single digit nanomolar as represented by compound 2aa. Compound 2aa showed cellular activity including antiproliferation and downstream target modulation. Selectivity profile is described. A co-crystal of 2aa with PKA is determined and discussed.
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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 |
Aug
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:ChuDaniel TDT,
pubmed-author:CrawfordKennethK,
pubmed-author:Del RosarioMerciM,
pubmed-author:JeffersonA BAB,
pubmed-author:KaufmanSusanS,
pubmed-author:LinXiaodongX,
pubmed-author:MaSylviaS,
pubmed-author:MurrayJeremy MJM,
pubmed-author:RicoAlice CAC,
pubmed-author:SIMK YKY,
pubmed-author:WangMichael XMX,
pubmed-author:ZhouYasheenY
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pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
16
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4163-8
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:16765046-Cell Line, Tumor,
pubmed-meshheading:16765046-Cell Proliferation,
pubmed-meshheading:16765046-Chemistry, Pharmaceutical,
pubmed-meshheading:16765046-Crystallization,
pubmed-meshheading:16765046-Crystallography, X-Ray,
pubmed-meshheading:16765046-Enzyme Inhibitors,
pubmed-meshheading:16765046-Humans,
pubmed-meshheading:16765046-Inhibitory Concentration 50,
pubmed-meshheading:16765046-Models, Chemical,
pubmed-meshheading:16765046-Models, Molecular,
pubmed-meshheading:16765046-Protein Binding,
pubmed-meshheading:16765046-Proto-Oncogene Proteins c-akt,
pubmed-meshheading:16765046-Structure-Activity Relationship,
pubmed-meshheading:16765046-Thiophenes
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pubmed:year |
2006
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pubmed:articleTitle |
Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies.
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pubmed:affiliation |
Small Molecule Drug Discovery, Biopharma Research, Chiron Corporation, Emeryville, CA, USA. xiaodong_lin@chiron.com
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pubmed:publicationType |
Journal Article
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