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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
24
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pubmed:dateCreated |
2010-11-24
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pubmed:abstractText |
This paper describes the discovery and design of a novel class of JAK2 inhibitors. Furthermore, we detail the optimization of a screening hit using ligand binding efficiency and log D. These efforts led to the identification of compound 41, which demonstrates in vivo activity in our study.
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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:AltmanMichael DMD,
pubmed-author:BachmanEricE,
pubmed-author:BouthilletteMelaneyM,
pubmed-author:ChanGraceG,
pubmed-author:DinsmoreChristopher JCJ,
pubmed-author:KozinaEkaterina SES,
pubmed-author:LiN CNC,
pubmed-author:MarshallC GaryCG,
pubmed-author:MathurAnjiliA,
pubmed-author:MoJan-RungJR,
pubmed-author:ObiG OGO,
pubmed-author:RosensteinCraigC,
pubmed-author:RushThomasT,
pubmed-author:SiuTonyT,
pubmed-author:YoungJonathan RJR
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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 |
7421-5
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pubmed:meshHeading |
pubmed-meshheading:21044843-Animals,
pubmed-meshheading:21044843-Binding Sites,
pubmed-meshheading:21044843-Computer Simulation,
pubmed-meshheading:21044843-Cyclization,
pubmed-meshheading:21044843-Drug Evaluation, Preclinical,
pubmed-meshheading:21044843-Heterocyclic Compounds, 3-Ring,
pubmed-meshheading:21044843-Janus Kinase 2,
pubmed-meshheading:21044843-Mice,
pubmed-meshheading:21044843-Mice, Inbred C57BL,
pubmed-meshheading:21044843-Pyridones,
pubmed-meshheading:21044843-STAT5 Transcription Factor,
pubmed-meshheading:21044843-Structure-Activity Relationship
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pubmed:year |
2010
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pubmed:articleTitle |
The discovery of tricyclic pyridone JAK2 inhibitors. Part 1: hit to lead.
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pubmed:affiliation |
Department of Chemistry, Merck & Co., Boston, MA 02115, USA. tony_siu@merck.com
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pubmed:publicationType |
Journal Article
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