| Literature DB >> 19171482 |
Hitesh J Sanganee1, Andrew Baxter, Simon Barber, Alastair J H Brown, Denise Grice, Fraser Hunt, Sarah King, David Laughton, Garry Pairaudeau, Bob Thong, Richard Weaver, John Unitt.
Abstract
A novel series of small molecule C5a antagonists is reported. In particular, in vitro metabolic studies and solution based combinatorial synthesis are demonstrated as useful tools for the rapid identification of antagonists with low in vitro clearance. Members of this series specifically inhibited the binding of (125)I-labeled C5a to human recombinant C5a receptor (C5aR). In functional cell assays these compounds displayed surmountable antagonism against C5a and did not demonstrate any detectable agonist activity.Entities:
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Year: 2008 PMID： 19171482 DOI： 10.1016/j.bmcl.2008.12.104
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823