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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
3
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pubmed:dateCreated |
2009-1-27
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pubmed:abstractText |
A series of trisubstituted cyclohexanes was designed, synthesized and evaluated as CC chemokine receptor 2 (CCR2) antagonists. This led to the identification of two distinct substitution patterns about the cyclohexane ring as potent and selective CCR2 antagonists. Compound 36 exhibited excellent binding (CCR2 IC(50)=2.4 nM) and functional antagonism (calcium flux IC(50)=2.0 nM and chemotaxis IC(50)=5.1 nM).
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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 |
Feb
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pubmed:issn |
1464-3405
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pubmed:author |
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
19
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
597-601
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pubmed:meshHeading |
pubmed-meshheading:19131247-Binding Sites,
pubmed-meshheading:19131247-Calcium,
pubmed-meshheading:19131247-Chemistry, Pharmaceutical,
pubmed-meshheading:19131247-Chemokine CCL2,
pubmed-meshheading:19131247-Chemotaxis,
pubmed-meshheading:19131247-Cyclohexanes,
pubmed-meshheading:19131247-Drug Design,
pubmed-meshheading:19131247-Humans,
pubmed-meshheading:19131247-Inhibitory Concentration 50,
pubmed-meshheading:19131247-Models, Chemical,
pubmed-meshheading:19131247-Molecular Structure,
pubmed-meshheading:19131247-Protein Binding,
pubmed-meshheading:19131247-Receptors, CCR2,
pubmed-meshheading:19131247-Structure-Activity Relationship
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pubmed:year |
2009
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pubmed:articleTitle |
Discovery of trisubstituted cyclohexanes 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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