Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.
Bioorg Med Chem Lett
; 21(20): 6188-94, 2011 Oct 15.
Article
em En
| MEDLINE
| ID: mdl-21903390
ABSTRACT
The lead optimisation of the diaminopyrimidine carboxamide series of spleen tyrosine kinase inhibitors is described. The medicinal chemistry strategy was focused on optimising the human whole blood activity whilst achieving a sufficient margin over liability kinases and hERG activity. GSK143 is a potent and highly selective SYK inhibitor showing good efficacy in the rat Arthus model.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Pirimidinas
/
Proteínas Tirosina Quinases
/
Reação de Arthus
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Peptídeos e Proteínas de Sinalização Intracelular
/
Inibidores de Proteínas Quinases
/
Compostos de Anilina
/
Anti-Inflamatórios
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article