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The discovery of a potent Nav1.3 inhibitor with good oral pharmacokinetics.
Pryde, D C; Swain, N A; Stupple, P A; West, C W; Marron, B; Markworth, C J; Printzenhoff, D; Lin, Z; Cox, P J; Suzuki, R; McMurray, S; Waldron, G J; Payne, C E; Warmus, J S; Chapman, M L.
Afiliación
  • Pryde DC; Worldwide Medicinal Chemistry , Pfizer Neuroscience and Pain Research Unit , Portway Building, Granta Park , Cambridge , CB21 6GS , UK . Email: david@curadev.co.uk.
  • Swain NA; Worldwide Medicinal Chemistry , Pfizer Neuroscience and Pain Research Unit , Portway Building, Granta Park , Cambridge , CB21 6GS , UK . Email: david@curadev.co.uk.
  • Stupple PA; Worldwide Medicinal Chemistry , Pfizer Neuroscience and Pain Research Unit , Portway Building, Granta Park , Cambridge , CB21 6GS , UK . Email: david@curadev.co.uk.
  • West CW; Pfizer Neuroscience and Pain Research Unit , 4222 Emperor Boulevard, Suite 350 , Durham , North Carolina NC27703 , USA.
  • Marron B; Pfizer Neuroscience and Pain Research Unit , 4222 Emperor Boulevard, Suite 350 , Durham , North Carolina NC27703 , USA.
  • Markworth CJ; Pfizer Neuroscience and Pain Research Unit , 4222 Emperor Boulevard, Suite 350 , Durham , North Carolina NC27703 , USA.
  • Printzenhoff D; Pfizer Neuroscience and Pain Research Unit , 4222 Emperor Boulevard, Suite 350 , Durham , North Carolina NC27703 , USA.
  • Lin Z; Pfizer Neuroscience and Pain Research Unit , 4222 Emperor Boulevard, Suite 350 , Durham , North Carolina NC27703 , USA.
  • Cox PJ; Pfizer Neuroscience and Pain Research Unit , Portway Building, Granta Park , Cambridge , CB21 6GS , UK.
  • Suzuki R; Pfizer Neuroscience and Pain Research Unit , Portway Building, Granta Park , Cambridge , CB21 6GS , UK.
  • McMurray S; Pfizer Neuroscience and Pain Research Unit , Portway Building, Granta Park , Cambridge , CB21 6GS , UK.
  • Waldron GJ; Pfizer Neuroscience and Pain Research Unit , Portway Building, Granta Park , Cambridge , CB21 6GS , UK.
  • Payne CE; Pfizer Neuroscience and Pain Research Unit , Portway Building, Granta Park , Cambridge , CB21 6GS , UK.
  • Warmus JS; Worldwide Medicinal Chemistry , Pfizer Neuroscience and Pain Research Unit , Groton , CT , USA.
  • Chapman ML; Pfizer Neuroscience and Pain Research Unit , 4222 Emperor Boulevard, Suite 350 , Durham , North Carolina NC27703 , USA.
Medchemcomm ; 8(6): 1255-1267, 2017 Jun 01.
Article en En | MEDLINE | ID: mdl-30108836
In this article, we describe the discovery of an aryl ether series of potent and selective Nav1.3 inhibitors. Based on structural analogy to a similar series of compounds we have previously shown bind to the domain IV voltage sensor region of Nav channels, we propose this series binds in the same location. We describe the development of this series from a published starting point, highlighting key selectivity and potency data, and several studies designed to validate Nav1.3 as a target for pain.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: Medchemcomm Año: 2017 Tipo del documento: Article Pais de publicación: Reino Unido
Texto completo
Añadir a Mi BVS
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: Medchemcomm Año: 2017 Tipo del documento: Article Pais de publicación: Reino Unido