Source:http://linkedlifedata.com/resource/pubmed/id/18722120
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
18
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pubmed:dateCreated |
2008-9-15
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pubmed:abstractText |
A series of cis-3,4-disubstituted piperidines was synthesized and evaluated as CC chemokine receptor 2 (CCR2) antagonists. Compound 24 emerged with an attractive profile, possessing excellent binding (CCR2 IC(50)=3.4 nM) and functional antagonism (calcium flux IC(50)=2.0 nM and chemotaxis IC(50)=5.4 nM). Studies to explore the binding of these piperidine analogs utilized a key CCR2 receptor mutant (E291A) with compound 14 and revealed a significant reliance on Glu291 for binding.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
1464-3405
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5063-5
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pubmed:meshHeading |
pubmed-meshheading:18722120-Combinatorial Chemistry Techniques,
pubmed-meshheading:18722120-Glutamic Acid,
pubmed-meshheading:18722120-Inhibitory Concentration 50,
pubmed-meshheading:18722120-Molecular Structure,
pubmed-meshheading:18722120-Piperidines,
pubmed-meshheading:18722120-Receptors, CCR2,
pubmed-meshheading:18722120-Stereoisomerism,
pubmed-meshheading:18722120-Structure-Activity Relationship
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pubmed:year |
2008
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pubmed:articleTitle |
Synthesis and evaluation of cis-3,4-disubstituted piperidines as potent CC chemokine receptor 2 (CCR2) antagonists.
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pubmed:affiliation |
Research and Development, Bristol-Myers Squibb Company, Princeton, NJ 08543-4000, USA. robert.cherney@bms.com
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pubmed:publicationType |
Journal Article
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