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Identification of small molecule agonists of the motilin receptor |
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| Authors: | Heightman Tom D Conway Elizabeth Corbett David F Macdonald Gregor J Stemp Geoffrey Westaway Susan M Celestini Paolo Gagliardi Stefania Riccaboni Mauro Ronzoni Silvano Vaidya Kalindi Butler Sharon McKay Fiona Muir Alison Powney Ben Winborn Kim Wise Alan Jarvie Emma M Sanger Gareth J |
| Affiliation: | Neurology & GI Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. tom.heightman@sgc.ox.ac.uk |
| Abstract: | High-throughput screening resulted in the identification of a series of novel motilin receptor agonists with relatively low molecular weights. The series originated from an array of biphenyl derivatives designed to target 7-transmembrane (7-TM) receptors. Further investigation of the structure-activity relationship within the series resulted in the identification of compound (22) as a potent and selective agonist at the motilin receptor. |
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