Identification of novel IP receptor agonists using historical ligand biased chemical arrays

McKeownS.C.; CharltonS.J.; CoxB.; FitchH.; HowsonC.D.; LeblancC.; MeyerA.; RosethorneE.M.; StanleyE.

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Identification of novel IP receptor agonists using historical ligand biased chemical arrays

机译：使用历史配体偏置化学阵列的新型IP受体激动剂的鉴定

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By considering published structural information we have designed high throughput biaryl lipophilic acid arrays leveraging facile chemistry to expedite their synthesis. We rapidly identified multiple hits which were of suitable IP agonist potency. These relatively simple and strategically undecorated molecules present an ideal opportunity for optimization towards our target candidate profile.

机译：通过考虑发表的结构信息，我们设计了高通量的胆汁脂质酸阵列，利用了化学化学来加快它们的合成。我们迅速确定了具有合适的IP激动剂效力的多次命中。这些相对简单和战略性的未污染的分子为我们的目标候选人概况进行了理想的机会。

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来源
《Bioorganic and Medicinal Chemistry Letters》 |2014年第10期|共4页
作者
McKeownS.C.; CharltonS.J.; CoxB.; FitchH.; HowsonC.D.; LeblancC.; MeyerA.; RosethorneE.M.; StanleyE.;
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作者单位

Novartis Institutes for BioMedical Research Wimblehurst Road Horsham West Sussex RH12 5AB;

Novartis Institutes for BioMedical Research Wimblehurst Road Horsham West Sussex RH12 5AB;

Novartis Institutes for BioMedical Research Wimblehurst Road Horsham West Sussex RH12 5AB;

Novartis Institutes for BioMedical Research Wimblehurst Road Horsham West Sussex RH12 5AB;

Novartis Institutes for BioMedical Research Wimblehurst Road Horsham West Sussex RH12 5AB;

Novartis Pharma AG Novartis Institutes for BioMedical Research Postfach CH-4002 Basel;

Novartis Pharma AG Novartis Institutes for BioMedical Research Postfach CH-4002 Basel;

Novartis Institutes for BioMedical Research Wimblehurst Road Horsham West Sussex RH12 5AB;

Novartis Institutes for BioMedical Research Wimblehurst Road Horsham West Sussex RH12 5AB;

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原文格式 PDF
正文语种 eng
中图分类药学;
关键词
IP agonist; Prostanoid; Pulmonary arterial hypertension;

机译：IP激动剂;前列腺;肺动脉高压;

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1. Identification of novel IP receptor agonists using historical ligand biased chemical arrays [J] . McKeownS.C., CharltonS.J., CoxB., Bioorganic and Medicinal Chemistry Letters . 2014,第10期

机译：使用历史配体偏置化学阵列的新型IP受体激动剂的鉴定
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Identification of novel IP receptor agonists using historical ligand biased chemical arrays

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