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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
18
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pubmed:dateCreated |
2006-8-14
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pubmed:abstractText |
We report here the discovery of a class of MCH R1 ligands based on a biphenyl carboxamide template. A docked-in model is presented indicating key interactions in the putative binding site of the receptor. Parallel high throughput synthetic techniques were utilised to allow rapid exploration of the structure-activity relationship around this template, leading to compound SB-568849 which possessed good receptor affinity and selectivity. This compound proved to be an antagonist with stability in vivo, an acceptable brain-blood ratio and oral bioavailability.
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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 |
Sep
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:BatesonJohn HJH,
pubmed-author:HervieuGuillaume JGJ,
pubmed-author:JeffreyPhillipP,
pubmed-author:JohnsonChristopher NCN,
pubmed-author:MuirAlison IAI,
pubmed-author:O'HanlonPeter JPJ,
pubmed-author:StempGeoffreyG,
pubmed-author:StevensAlex JAJ,
pubmed-author:ThewlisKevin MKM,
pubmed-author:WilsonShelaghS,
pubmed-author:WinbornKim YKY,
pubmed-author:WittyDavid RDR
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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 |
4865-71
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pubmed:meshHeading |
pubmed-meshheading:16839761-Amides,
pubmed-meshheading:16839761-Animals,
pubmed-meshheading:16839761-Biphenyl Compounds,
pubmed-meshheading:16839761-Brain,
pubmed-meshheading:16839761-Cattle,
pubmed-meshheading:16839761-Computational Biology,
pubmed-meshheading:16839761-Humans,
pubmed-meshheading:16839761-Ligands,
pubmed-meshheading:16839761-Models, Molecular,
pubmed-meshheading:16839761-Molecular Structure,
pubmed-meshheading:16839761-Receptors, Somatostatin,
pubmed-meshheading:16839761-Structure-Activity Relationship,
pubmed-meshheading:16839761-Sulfur
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pubmed:year |
2006
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pubmed:articleTitle |
SAR of biphenyl carboxamide ligands of the human melanin-concentrating hormone receptor 1 (MCH R1): discovery of antagonist SB-568849.
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pubmed:affiliation |
GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. david.witty@gsk.com
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pubmed:publicationType |
Journal Article
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