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High throughput screening identified a phenoxyacetic acid scaffold as a novel CRTh2 receptor antagonist chemotype, which could be optimised to furnish a compound with functional potency for inhibition of human eosinophil shape change and oral bioavailability in the rat.


David A Sandham, Clive Aldcroft, Urs Baettig, Lucy Barker, David Beer, Gurdip Bhalay, Zarin Brown, Gerald Dubois, David Budd, Louise Bidlake, Emma Campbell, Brian Cox, Brian Everatt, David Harrison, Catherine J Leblanc, Jodie Manini, Rachael Profit, Rowan Stringer, Katy S Thompson, Katharine L Turner, Morris F Tweed, Christoph Walker, Simon J Watson, Steven Whitebread, Jennifer Willis, Gareth Williams, Caroline Wilson. 2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists. Bioorganic & medicinal chemistry letters. 2007 Aug 1;17(15):4347-50

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PMID: 17531480

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