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417 results

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Page 1
Discovery of novel PI3-kinase δ specific inhibitors for the treatment of rheumatoid arthritis: taming CYP3A4 time-dependent inhibition.
Safina BS, Baker S, Baumgardner M, Blaney PM, Chan BK, Chen YH, Cartwright MW, Castanedo G, Chabot C, Cheguillaume AJ, Goldsmith P, Goldstein DM, Goyal B, Hancox T, Handa RK, Iyer PS, Kaur J, Kondru R, Kenny JR, Krintel SL, Li J, Lesnick J, Lucas MC, Lewis C, Mukadam S, Murray J, Nadin AJ, Nonomiya J, Padilla F, Palmer WS, Pang J, Pegg N, Price S, Reif K, Salphati L, Savy PA, Seward EM, Shuttleworth S, Sohal S, Sweeney ZK, Tay S, Tivitmahaisoon P, Waszkowycz B, Wei B, Yue Q, Zhang C, Sutherlin DP. Safina BS, et al. Among authors: goldsmith p. J Med Chem. 2012 Jun 28;55(12):5887-900. doi: 10.1021/jm3003747. Epub 2012 Jun 11. J Med Chem. 2012. PMID: 22626259
Rational design of phosphoinositide 3-kinase α inhibitors that exhibit selectivity over the phosphoinositide 3-kinase β isoform.
Heffron TP, Wei B, Olivero A, Staben ST, Tsui V, Do S, Dotson J, Folkes AJ, Goldsmith P, Goldsmith R, Gunzner J, Lesnick J, Lewis C, Mathieu S, Nonomiya J, Shuttleworth S, Sutherlin DP, Wan NC, Wang S, Wiesmann C, Zhu BY. Heffron TP, et al. Among authors: goldsmith p, goldsmith r. J Med Chem. 2011 Nov 24;54(22):7815-33. doi: 10.1021/jm2007084. Epub 2011 Oct 21. J Med Chem. 2011. PMID: 21985639
Potent and selective inhibitors of PI3Kδ: obtaining isoform selectivity from the affinity pocket and tryptophan shelf.
Sutherlin DP, Baker S, Bisconte A, Blaney PM, Brown A, Chan BK, Chantry D, Castanedo G, DePledge P, Goldsmith P, Goldstein DM, Hancox T, Kaur J, Knowles D, Kondru R, Lesnick J, Lucas MC, Lewis C, Murray J, Nadin AJ, Nonomiya J, Pang J, Pegg N, Price S, Reif K, Safina BS, Salphati L, Staben S, Seward EM, Shuttleworth S, Sohal S, Sweeney ZK, Ultsch M, Waszkowycz B, Wei B. Sutherlin DP, et al. Among authors: goldsmith p. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4296-302. doi: 10.1016/j.bmcl.2012.05.027. Epub 2012 May 17. Bioorg Med Chem Lett. 2012. PMID: 22672799
Discovery of novel, non-acidic 1,5-biaryl pyrrole EP1 receptor antagonists.
Hall A, Atkinson S, Brown SH, Chessell IP, Chowdhury A, Giblin GM, Goldsmith P, Healy MP, Jandu KS, Johnson MR, Michel AD, Naylor A, Sweeting JA. Hall A, et al. Among authors: goldsmith p. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1200-5. doi: 10.1016/j.bmcl.2006.12.021. Epub 2006 Dec 12. Bioorg Med Chem Lett. 2007. PMID: 17196385
Discovery of a novel series of nonacidic benzofuran EP1 receptor antagonists.
Allan AC, Billinton A, Brown SH, Chowdhury A, Eatherton AJ, Fieldhouse C, Giblin GM, Goldsmith P, Hall A, Hurst DN, Naylor A, Rawlings DA, Sime M, Scoccitti T, Theobald PJ. Allan AC, et al. Among authors: goldsmith p. Bioorg Med Chem Lett. 2011 Jul 15;21(14):4343-8. doi: 10.1016/j.bmcl.2011.05.047. Epub 2011 May 23. Bioorg Med Chem Lett. 2011. PMID: 21676612
Discovery of 1-[4-(3-chlorophenylamino)-1-methyl-1H-pyrrolo[3,2-c]pyridin-7-yl]-1-morpholin-4-ylmethanone (GSK554418A), a brain penetrant 5-azaindole CB2 agonist for the treatment of chronic pain.
Giblin GM, Billinton A, Briggs M, Brown AJ, Chessell IP, Clayton NM, Eatherton AJ, Goldsmith P, Haslam C, Johnson MR, Mitchell WL, Naylor A, Perboni A, Slingsby BP, Wilson AW. Giblin GM, et al. Among authors: goldsmith p. J Med Chem. 2009 Oct 8;52(19):5785-8. doi: 10.1021/jm9009857. J Med Chem. 2009. PMID: 19743867
Discovery of a novel indole series of EP1 receptor antagonists by scaffold hopping.
Hall A, Billinton A, Brown SH, Chowdhury A, Giblin GM, Goldsmith P, Hurst DN, Naylor A, Patel S, Scoccitti T, Theobald PJ. Hall A, et al. Among authors: goldsmith p. Bioorg Med Chem Lett. 2008 Apr 15;18(8):2684-90. doi: 10.1016/j.bmcl.2008.03.018. Epub 2008 Mar 10. Bioorg Med Chem Lett. 2008. PMID: 18378447
Synthesis and Preclinical Characterization of LY3154885, a Human Dopamine D1 Receptor Positive Allosteric Modulator with an Improved Nonclinical Drug-Drug Interaction Risk Profile.
Hao J, Beck J, Zhou X, Lackner GL, Johnston R, Reinhard M, Goldsmith P, Hollinshead S, Dehlinger V, Filla SA, Wang XS, Richardson J, Posada M, Mohutsky M, Schober D, Katner JS, Chen Q, Hu B, Remick DM, Coates DA, Mathes BM, Hawk MK, Svensson KA, Hembre E. Hao J, et al. Among authors: goldsmith p. J Med Chem. 2022 Mar 10;65(5):3786-3797. doi: 10.1021/acs.jmedchem.1c01887. Epub 2022 Feb 17. J Med Chem. 2022. PMID: 35175768
Identification of novel pyrazole acid antagonists for the EP1 receptor.
McKeown SC, Hall A, Giblin GM, Lorthioir O, Blunt R, Lewell XQ, Wilson RJ, Brown SH, Chowdhury A, Coleman T, Watson SP, Chessell IP, Pipe A, Clayton N, Goldsmith P. McKeown SC, et al. Among authors: goldsmith p. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4767-71. doi: 10.1016/j.bmcl.2006.06.086. Epub 2006 Jul 14. Bioorg Med Chem Lett. 2006. PMID: 16843659
Discovery of brain penetrant, soluble, pyrazole amide EP1 receptor antagonists.
Hall A, Billinton A, Bristow AK, Brown SH, Chowdhury A, Cutler L, Giblin GM, Goldsmith P, Hayhow TG, Kilford IR, Naylor A, Passingham B, Rawlings DA. Hall A, et al. Among authors: goldsmith p. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4027-32. doi: 10.1016/j.bmcl.2008.05.118. Epub 2008 Jun 5. Bioorg Med Chem Lett. 2008. PMID: 18571922
417 results