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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
5
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pubmed:dateCreated |
2010-2-22
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pubmed:abstractText |
Piperazine-bisamide analogs were discovered as partial agonists of human growth hormone secretagogue receptor (GHSR) in a high throughput screen. The partial agonists were optimized for potency and converted into antagonists through structure-activity relationship (SAR) studies. The efforts also led to the identification of potent antagonist with favorable PK profile suitable as a tool compound for in vivo studies.
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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 |
Mar
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BeckmannHolgerH,
pubmed-author:ConnorsRichardR,
pubmed-author:DaiKangK,
pubmed-author:EskaP LPL,
pubmed-author:HallerKatrinK,
pubmed-author:LiLepingL,
pubmed-author:LiangLingmingL,
pubmed-author:LindstromMichelleM,
pubmed-author:LizarzaburuMikeM,
pubmed-author:MedinaJulio CJC,
pubmed-author:MotaniAlykhanA,
pubmed-author:PyeS DSD,
pubmed-author:WanskaMalgorzataM,
pubmed-author:YuMingM,
pubmed-author:ZhangAlexA
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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 |
1
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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 |
1758-62
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pubmed:meshHeading |
pubmed-meshheading:20137933-Amides,
pubmed-meshheading:20137933-Animals,
pubmed-meshheading:20137933-Anti-Obesity Agents,
pubmed-meshheading:20137933-High-Throughput Screening Assays,
pubmed-meshheading:20137933-Humans,
pubmed-meshheading:20137933-Indoles,
pubmed-meshheading:20137933-Obesity,
pubmed-meshheading:20137933-Piperazines,
pubmed-meshheading:20137933-Rats,
pubmed-meshheading:20137933-Receptors, Ghrelin,
pubmed-meshheading:20137933-Structure-Activity Relationship
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pubmed:year |
2010
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pubmed:articleTitle |
Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity.
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pubmed:affiliation |
Amgen Inc. 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. yum@amgen.com
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pubmed:publicationType |
Journal Article
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