Your browser doesn't support javascript.
loading
From astemizole to a novel hit series of small-molecule somatostatin 5 receptor antagonists via GPCR affinity profiling.
Guba, Wolfgang; Green, Luke G; Martin, Rainer E; Roche, Olivier; Kratochwil, Nicole; Mauser, Harald; Bissantz, Caterina; Christ, Andreas; Stahl, Martin.
Affiliation
  • Guba W; Discovery Chemistry, Lead Generation, F. Hoffmann-La Roche Ltd., 4070 Basel, Switzerland. wolfgang.guba@roche.com
J Med Chem ; 50(25): 6295-8, 2007 Dec 13.
Article in En | MEDLINE | ID: mdl-18020391
ABSTRACT
The H1R antagonist astemizole was identified as a somatostatin 5 (SST5) receptor antagonist by a comparative sequence analysis of the consensus drug binding pocket of GPCRs. Subsequently, a similarity analysis of GPCR affinity profiles of astemizole versus a set of in-house GPCR-biased combinatorial libraries revealed new chemical entry points that led to a second lead series with nanomolar binding affinity.
Subject(s)
Search on Google
Add to My VHL
Print
XML
PubMed Links

Collection: 01-internacional Database: MEDLINE Main subject: Piperidines / Spiro Compounds / Astemizole / Receptors, Somatostatin / Receptors, G-Protein-Coupled / Histamine H1 Antagonists Limits: Humans Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2007 Document type: Article Affiliation country:
Search on Google
Add to My VHL
Print
XML
PubMed Links

Collection: 01-internacional Database: MEDLINE Main subject: Piperidines / Spiro Compounds / Astemizole / Receptors, Somatostatin / Receptors, G-Protein-Coupled / Histamine H1 Antagonists Limits: Humans Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2007 Document type: Article Affiliation country: