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Circumventing seizure activity in a series of G protein coupled receptor 119 (GPR119) agonists.
Scott JS, Bowker SS, Brocklehurst KJ, Brown HS, Clarke DS, Easter A, Ertan A, Goldberg K, Hudson JA, Kavanagh S, Laber D, Leach AG, MacFaul PA, Martin EA, McKerrecher D, Schofield P, Svensson PH, Teague J. Scott JS, et al. Among authors: clarke ds. J Med Chem. 2014 Nov 13;57(21):8984-98. doi: 10.1021/jm5011012. Epub 2014 Nov 3. J Med Chem. 2014. PMID: 25286150
Identification, optimization, and pharmacology of acylurea GHS-R1a inverse agonists.
McCoull W, Barton P, Brown AJ, Bowker SS, Cameron J, Clarke DS, Davies RD, Dossetter AG, Ertan A, Fenwick M, Green C, Holmes JL, Martin N, Masters D, Moore JE, Newcombe NJ, Newton C, Pointon H, Robb GR, Sheldon C, Stokes S, Morgan D. McCoull W, et al. Among authors: clarke ds. J Med Chem. 2014 Jul 24;57(14):6128-40. doi: 10.1021/jm500610n. Epub 2014 Jul 8. J Med Chem. 2014. PMID: 24967667
Use of small-molecule crystal structures to address solubility in a novel series of G protein coupled receptor 119 agonists: optimization of a lead and in vivo evaluation.
Scott JS, Birch AM, Brocklehurst KJ, Broo A, Brown HS, Butlin RJ, Clarke DS, Davidsson O, Ertan A, Goldberg K, Groombridge SD, Hudson JA, Laber D, Leach AG, Macfaul PA, McKerrecher D, Pickup A, Schofield P, Svensson PH, Sörme P, Teague J. Scott JS, et al. Among authors: clarke ds. J Med Chem. 2012 Jun 14;55(11):5361-79. doi: 10.1021/jm300310c. Epub 2012 May 17. J Med Chem. 2012. PMID: 22545772
Discovery, optimisation and in vivo evaluation of novel GPR119 agonists.
Brocklehurst KJ, Broo A, Butlin RJ, Brown HS, Clarke DS, Davidsson Ö, Goldberg K, Groombridge SD, Kelly EE, Leach A, McKerrecher D, O'Donnell C, Poucher S, Schofield P, Scott JS, Teague J, Westgate L, Wood MJ. Brocklehurst KJ, et al. Among authors: clarke ds. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7310-6. doi: 10.1016/j.bmcl.2011.10.033. Epub 2011 Oct 18. Bioorg Med Chem Lett. 2011. PMID: 22061639
17 results