|
rdf:type |
|
|
lifeskim:mentions |
umls-concept:C0037659,
umls-concept:C0085170,
umls-concept:C0205314,
umls-concept:C0205549,
umls-concept:C0243076,
umls-concept:C0597357,
umls-concept:C0679622,
umls-concept:C0682972,
umls-concept:C1367690,
umls-concept:C1426330,
umls-concept:C1428424,
umls-concept:C1510827,
umls-concept:C1708373,
umls-concept:C2003903
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|
pubmed:issue |
25
|
|
pubmed:dateCreated |
2007-12-6
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|
pubmed:abstractText |
The H1R antagonist astemizole was identified as a somatostatin 5 (SST5) receptor antagonist by a comparative sequence analysis of the consensus drug binding pocket of GPCRs. Subsequently, a similarity analysis of GPCR affinity profiles of astemizole versus a set of in-house GPCR-biased combinatorial libraries revealed new chemical entry points that led to a second lead series with nanomolar binding affinity.
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pubmed:language |
eng
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|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Dec
|
|
pubmed:issn |
0022-2623
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|
pubmed:author |
|
|
pubmed:issnType |
Print
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|
pubmed:day |
13
|
|
pubmed:volume |
50
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
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pubmed:pagination |
6295-8
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pubmed:meshHeading |
pubmed-meshheading:18020391-Astemizole,
pubmed-meshheading:18020391-Binding Sites,
pubmed-meshheading:18020391-Combinatorial Chemistry Techniques,
pubmed-meshheading:18020391-Databases, Factual,
pubmed-meshheading:18020391-Histamine H1 Antagonists,
pubmed-meshheading:18020391-Humans,
pubmed-meshheading:18020391-Piperidines,
pubmed-meshheading:18020391-Receptors, G-Protein-Coupled,
pubmed-meshheading:18020391-Receptors, Somatostatin,
pubmed-meshheading:18020391-Spiro Compounds,
pubmed-meshheading:18020391-Structure-Activity Relationship
|
|
pubmed:year |
2007
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|
pubmed:articleTitle |
From astemizole to a novel hit series of small-molecule somatostatin 5 receptor antagonists via GPCR affinity profiling.
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|
pubmed:affiliation |
Discovery Chemistry, Lead Generation, F. Hoffmann-La Roche Ltd., 4070 Basel, Switzerland. wolfgang.guba@roche.com
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pubmed:publicationType |
Journal Article
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