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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
2010-12-24
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pubmed:abstractText |
High-throughput screening of 3.87 million compounds delivered a novel series of non-steroidal GR antagonists. Subsequent rounds of optimisation allowed progression from a non-selective ligand with a poor ADMET profile to an orally bioavailable, selective, stable, glucocorticoid receptor antagonist.
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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 |
Jan
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BosiesMichaelM,
pubmed-author:BrownAngus RAR,
pubmed-author:CameronHelenH,
pubmed-author:ClarkJohnJ,
pubmed-author:CowleyAngelaA,
pubmed-author:CraigheadMarkM,
pubmed-author:ElmoreMoira AMA,
pubmed-author:FirthAlistairA,
pubmed-author:GoodwinRichardR,
pubmed-author:GoutcherSusanS,
pubmed-author:GrantEmmaE,
pubmed-author:GrassieMoragM,
pubmed-author:GroveSimon J ASJ,
pubmed-author:HamiltonNiall MNM,
pubmed-author:HampsonHannahH,
pubmed-author:HillierAlisonA,
pubmed-author:HoKoc-KanKK,
pubmed-author:KiczunMichaelM,
pubmed-author:KingsburyCeliaC,
pubmed-author:KultgenSteven GSG,
pubmed-author:LittlewoodPeter T APT,
pubmed-author:LusherScott JSJ,
pubmed-author:MacdonaldSusanS,
pubmed-author:McIntoshLorraineL,
pubmed-author:McIntyreTheresaT,
pubmed-author:MistryAshvinA,
pubmed-author:MorphyJ RichardJR,
pubmed-author:NimzOlafO,
pubmed-author:OhlmeyerMichaelM,
pubmed-author:RankovicZoranZ,
pubmed-author:SherborneBradB,
pubmed-author:SmithAlasdairA,
pubmed-author:SpeakeMichaelM,
pubmed-author:SpinksGayleG,
pubmed-author:ThomsonFionaF,
pubmed-author:VermaVivekV,
pubmed-author:WatsonLynnL,
pubmed-author:WestonMarkM
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pubmed:copyrightInfo |
Copyright © 2010. Published by Elsevier Ltd.
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
21
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
137-40
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pubmed:meshHeading |
pubmed-meshheading:21129964-Animals,
pubmed-meshheading:21129964-Drug Evaluation, Preclinical,
pubmed-meshheading:21129964-High-Throughput Screening Assays,
pubmed-meshheading:21129964-Humans,
pubmed-meshheading:21129964-Hydrocortisone,
pubmed-meshheading:21129964-Microsomes,
pubmed-meshheading:21129964-Rats,
pubmed-meshheading:21129964-Receptors, Glucocorticoid,
pubmed-meshheading:21129964-Structure-Activity Relationship,
pubmed-meshheading:21129964-Sulfonamides
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pubmed:year |
2011
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pubmed:articleTitle |
Discovery and optimisation of a selective non-steroidal glucocorticoid receptor antagonist.
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pubmed:affiliation |
Merck Research Laboratories (MSD), Newhouse, Motherwell, Lanarkshire ML1 5SH, UK. angus.brown@merck.com
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pubmed:publicationType |
Journal Article
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