Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists.
Bioorg Med Chem Lett
; 20(8): 2516-9, 2010 Apr 15.
Article
en En
| MEDLINE
| ID: mdl-20299215
ABSTRACT
The identification and hit-to-lead exploration of a novel, potent and selective series of histamine H(4) receptor inverse agonists is described. The initial hit, 3A (IC(50) 19 nM) was identified by means of a ligand-based virtual screening approach. Subsequent medicinal chemistry exploration yielded 18I which possessed increased potency (R-enantiomer IC(50) 1 nM) as well as enhanced microsomal stability.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Receptores Acoplados a Proteínas G
/
Antagonistas de los Receptores Histamínicos
Tipo de estudio:
Diagnostic_studies
Límite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2010
Tipo del documento:
Article
País de afiliación:
Reino Unido