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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 |
Herein, we report the discovery of an effective strategy to modulate liabilities related to affinity of previously disclosed bicyclohexane MCHR-1 antagonists for the hERG channel. This paper describes one of several strategies incorporated to limit hERG binding via modifications of a terminal aryl group in an otherwise promising bicyclohexyl urea series.
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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:CladerJohn WJW,
pubmed-author:CoxKathleenK,
pubmed-author:GuzikHenryH,
pubmed-author:HawesBrianB,
pubmed-author:MargulisMichaelM,
pubmed-author:McBriarMark DMD,
pubmed-author:O'neillKimK,
pubmed-author:ParuchovaJaroslavaJ,
pubmed-author:ShapiroSherryS,
pubmed-author:SorotaSteveS,
pubmed-author:TowMM,
pubmed-author:TuckerKristalK,
pubmed-author:WestonDaniel JDJ
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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 |
4262-5
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pubmed:meshHeading |
pubmed-meshheading:16753297-Chemistry, Pharmaceutical,
pubmed-meshheading:16753297-Drug Design,
pubmed-meshheading:16753297-Ether-A-Go-Go Potassium Channels,
pubmed-meshheading:16753297-Humans,
pubmed-meshheading:16753297-Inhibitory Concentration 50,
pubmed-meshheading:16753297-Kinetics,
pubmed-meshheading:16753297-Melanins,
pubmed-meshheading:16753297-Models, Chemical,
pubmed-meshheading:16753297-Protein Binding,
pubmed-meshheading:16753297-Receptors, Somatostatin,
pubmed-meshheading:16753297-Urea
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pubmed:year |
2006
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pubmed:articleTitle |
Bicyclo[3.1.0]hexyl urea melanin concentrating hormone (MCH) receptor-1 antagonists: impacting hERG liability via aryl modifications.
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pubmed:affiliation |
Schering-Plough Research Institute, Kenilworth, NJ 07033, USA. mark.mcbriar@spcorp.com
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pubmed:publicationType |
Journal Article
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