| Literature DB >> 11549467 |
L L Chang1, K L Sidler, M A Cascieri, S de Laszlo, G Koch, B Li, M MacCoss, N Mantlo, S O'Keefe, M Pang, A Rolando, W K Hagmann.
Abstract
A modestly active, nonselective triarylimidazole lead was optimized for binding affinity with the human glucagon receptor. This led to the identification of a 2- and/or 4-alkyl or alkyloxy substituent on the imidazole C4-aryl group as a structural determinant for significant enhancement in binding with the glucagon receptor (e.g., 41, IC(50)=0.053 microM) and selectivity (>1000x) over p38MAP kinase in this class of compounds.Entities:
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Year: 2001 PMID： 11549467 DOI： 10.1016/s0960-894x(01)00498-x
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823