|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
22
|
|
pubmed:dateCreated |
2009-11-20
|
|
pubmed:abstractText |
A high-throughput screening campaign to discover small molecule leads for the treatment of bone disorders concluded with the discovery of a compound with a 2-aminopyrimidine template that targeted the Wnt beta-catenin cellular messaging system. Hit-to-lead in vitro optimization for target activity and molecular properties led to the discovery of (1-(4-(naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine (5, WAY-262611). Compound 5 has excellent pharmacokinetic properties and showed a dose dependent increase in the trabecular bone formation rate in ovariectomized rats following oral administration.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Nov
|
|
pubmed:issn |
1520-4804
|
|
pubmed:author |
pubmed-author:AlonNipaN,
pubmed-author:BexFrederick JFJ,
pubmed-author:BhatBheem MBM,
pubmed-author:BodinePeter V NPV,
pubmed-author:BursavichMattew GMG,
pubmed-author:ColeburnValerie EVE,
pubmed-author:FelixLuciana ALA,
pubmed-author:GilbertAdam MAM,
pubmed-author:GreenDaniel MDM,
pubmed-author:GreenPaulaP,
pubmed-author:HauzeDiane BDB,
pubmed-author:KharodeYogendra PYP,
pubmed-author:LamHo-SunHS,
pubmed-author:LockheadSusan RSR,
pubmed-author:LundquistJoseph TJT4th,
pubmed-author:MagoldaRonald LRL,
pubmed-author:MatteoJeanne JJJ,
pubmed-author:MehlmannJohn FJF,
pubmed-author:MilliganColleenC,
pubmed-author:MurrillsRichard JRJ,
pubmed-author:PelletierJeffrey CJC,
pubmed-author:PirrelloJenniferJ,
pubmed-author:SelimSallyS,
pubmed-author:SharpMichael CMC,
pubmed-author:UnwallaRay JRJ,
pubmed-author:VeraMatthew DMD,
pubmed-author:WrobelJay EJE,
pubmed-author:YaworskyPaulP
|
|
pubmed:issnType |
Electronic
|
|
pubmed:day |
26
|
|
pubmed:volume |
52
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
6962-5
|
|
pubmed:dateRevised |
2011-11-2
|
|
pubmed:meshHeading |
pubmed-meshheading:19856966-Animals,
pubmed-meshheading:19856966-Catalytic Domain,
pubmed-meshheading:19856966-Cell Line, Tumor,
pubmed-meshheading:19856966-Glycogen Synthase Kinase 3,
pubmed-meshheading:19856966-Humans,
pubmed-meshheading:19856966-Mice,
pubmed-meshheading:19856966-Models, Molecular,
pubmed-meshheading:19856966-Osteogenesis,
pubmed-meshheading:19856966-Piperidines,
pubmed-meshheading:19856966-Pyrimidines,
pubmed-meshheading:19856966-Rats,
pubmed-meshheading:19856966-Signal Transduction,
pubmed-meshheading:19856966-Wnt Proteins,
pubmed-meshheading:19856966-beta Catenin
|
|
pubmed:year |
2009
|
|
pubmed:articleTitle |
(1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: a wingless beta-catenin agonist that increases bone formation rate.
|
|
pubmed:affiliation |
Chemical Sciences, Drug Safety & Metabolism, Wyeth Research, 500 Arcola Road, Collegeville, Pennsylvania 19426, USA. Pelletj@wyeth.com
|
|
pubmed:publicationType |
Journal Article
|
