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493 results

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Page 1
Identification of a novel allosteric GLP-1R antagonist HTL26119 using structure- based drug design.
O'Brien A, Andrews SP, Baig AH, Bortolato A, Brown AJH, Brown GA, Brown SH, Christopher JA, Congreve M, Cooke RM, De Graaf C, Errey JC, Fieldhouse C, Jazayeri A, Marshall FH, Mason JS, Mobarec JC, Okrasa K, Steele KN, Southall SM, Teobald I, Watson SP, Weir M. O'Brien A, et al. Among authors: watson sp. Bioorg Med Chem Lett. 2019 Oct 15;29(20):126611. doi: 10.1016/j.bmcl.2019.08.015. Epub 2019 Aug 9. Bioorg Med Chem Lett. 2019. PMID: 31447084
The design and SAR of a novel series of 2-aminopyridine based LRRK2 inhibitors.
Smith GP, Badolo L, Chell V, Chen IJ, Christensen KV, David L, Daechsel JA, Hentzer M, Herzig MC, Mikkelsen GK, Watson SP, Williamson DS. Smith GP, et al. Among authors: watson sp. Bioorg Med Chem Lett. 2017 Sep 15;27(18):4500-4505. doi: 10.1016/j.bmcl.2017.07.072. Epub 2017 Aug 1. Bioorg Med Chem Lett. 2017. PMID: 28802631
The characterization of a novel V1b antagonist lead series.
Smethurst CA, Borthwick JA, Gaines S, Watson S, Green A, Schulz MJ, Burton G, Buson AA, Arban R. Smethurst CA, et al. Bioorg Med Chem Lett. 2011 Jan 1;21(1):92-6. doi: 10.1016/j.bmcl.2010.11.061. Epub 2010 Nov 19. Bioorg Med Chem Lett. 2011. PMID: 21146408
The identification of structurally novel, selective, orally bioavailable positive modulators of mGluR2.
D'Alessandro PL, Corti C, Roth A, Ugolini A, Sava A, Montanari D, Bianchi F, Garland SL, Powney B, Koppe EL, Rocheville M, Osborne G, Perez P, de la Fuente J, De Los Frailes M, Smith PW, Branch C, Nash D, Watson SP. D'Alessandro PL, et al. Among authors: watson sp. Bioorg Med Chem Lett. 2010 Jan 15;20(2):759-62. doi: 10.1016/j.bmcl.2009.11.032. Epub 2009 Nov 26. Bioorg Med Chem Lett. 2010. PMID: 20005096
The identification of novel orally active mGluR5 antagonist GSK2210875.
Pilla M, Andreoli M, Tessari M, Delle-Fratte S, Roth A, Butler S, Brown F, Shah P, Bettini E, Cavallini P, Benedetti R, Minick D, Smith P, Tehan B, D'Alessandro P, Lorthioir O, Ball C, Garzya V, Goodacre C, Watson S. Pilla M, et al. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7521-4. doi: 10.1016/j.bmcl.2010.09.120. Epub 2010 Nov 2. Bioorg Med Chem Lett. 2010. PMID: 21051228
The identification of a selective dopamine D2 partial agonist, D3 antagonist displaying high levels of brain exposure.
Holmes IP, Blunt RJ, Lorthioir OE, Blowers SM, Gribble A, Payne AH, Stansfield IG, Wood M, Woollard PM, Reavill C, Howes CM, Micheli F, Di Fabio R, Donati D, Terreni S, Hamprecht D, Arista L, Worby A, Watson SP. Holmes IP, et al. Among authors: watson sp. Bioorg Med Chem Lett. 2010 Mar 15;20(6):2013-6. doi: 10.1016/j.bmcl.2010.01.090. Epub 2010 Jan 25. Bioorg Med Chem Lett. 2010. PMID: 20153647
The identification of a series of novel, soluble non-peptidic neuropeptide Y Y2 receptor antagonists.
Lunniss GE, Barnes AA, Barton N, Biagetti M, Bianchi F, Blowers SM, Caberlotto LL, Emmons A, Holmes IP, Montanari D, Norris R, Puckey GV, Walters DJ, Watson SP, Willis J. Lunniss GE, et al. Among authors: watson sp. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7341-4. doi: 10.1016/j.bmcl.2010.10.065. Epub 2010 Nov 10. Bioorg Med Chem Lett. 2010. PMID: 21074426
493 results