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Identification of novel IP receptor agonists using historical ligand biased chemical arrays.
McKeown, Stephen C; Charlton, Steven J; Cox, Brian; Fitch, Helen; Howson, Christopher D; Leblanc, Catherine; Meyer, Arndt; Rosethorne, Elizabeth M; Stanley, Emily.
Afiliação
  • McKeown SC; Novartis Institutes for BioMedical Research, Wimblehurst Road, Horsham, West Sussex RH12 5AB, UK. Electronic address: steve.mckeown@novartis.com.
  • Charlton SJ; Novartis Institutes for BioMedical Research, Wimblehurst Road, Horsham, West Sussex RH12 5AB, UK.
  • Cox B; Novartis Institutes for BioMedical Research, Wimblehurst Road, Horsham, West Sussex RH12 5AB, UK.
  • Fitch H; Novartis Institutes for BioMedical Research, Wimblehurst Road, Horsham, West Sussex RH12 5AB, UK.
  • Howson CD; Novartis Institutes for BioMedical Research, Wimblehurst Road, Horsham, West Sussex RH12 5AB, UK.
  • Leblanc C; Novartis Pharma AG, Novartis Institutes for BioMedical Research, Postfach, CH-4002 Basel, Switzerland.
  • Meyer A; Novartis Pharma AG, Novartis Institutes for BioMedical Research, Postfach, CH-4002 Basel, Switzerland.
  • Rosethorne EM; Novartis Institutes for BioMedical Research, Wimblehurst Road, Horsham, West Sussex RH12 5AB, UK.
  • Stanley E; Novartis Institutes for BioMedical Research, Wimblehurst Road, Horsham, West Sussex RH12 5AB, UK.
Bioorg Med Chem Lett ; 24(10): 2247-50, 2014 May 15.
Article em En | MEDLINE | ID: mdl-24736116
ABSTRACT
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.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Compostos Bicíclicos com Pontes / Receptores de Epoprostenol / Anti-Hipertensivos Tipo de estudo: Diagnostic_studies / Prognostic_studies Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2014 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Compostos Bicíclicos com Pontes / Receptores de Epoprostenol / Anti-Hipertensivos Tipo de estudo: Diagnostic_studies / Prognostic_studies Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2014 Tipo de documento: Article