Navigating in chromone chemical space: discovery of novel and distinct A3 adenosine receptor ligands. Issue 96 (17th October 2015)

• Record Type: Journal Article
• Authors: Cagide, F.; Gaspar, A.; Reis, J.; Chavarria, D.; Vilar, S.; Hripcsak, G.; Uriarte, E.; Kachler, S.; Klotz, K. N.; Borges, F.
• Is Part Of: RSC advances. Volume 5:Issue 96(2015)
• Page Start: 78572
• Page End: 78585
• Publication Date: 2015-10-17
• Subjects: Chemistry -- Periodicals; 540.5
• DOI: 10.1039/c5ra14988f
• Languages: English
• ISSNs: 2046-2069

Abstract

<abstract abstract-type="toc"> <title> <x xml:space="preserve">Abstract</x> </title> <p> <graphic position="anchor" id="ga" xlink:href="ark:/27927/pgj2xwvb48t" xlink:type="simple" xmlns:xlink="http://www.w3.org/1999/xlink" />One of the major hurdles in the development of effective drugs targeting GPCRs is finding ligands selective for a specific receptor subtype. Here we describe a potent and selective hormone-based <italic>h</italic>A₃ AR ligand (<italic>K</italic>_i of 167 nM) with a remarkable selectivity.</p> </abstract>