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Page 1
A reversed sulfonamide series of selective RORc inverse agonists.
van Niel MB, Fauber BP, Cartwright M, Gaines S, Killen JC, René O, Ward SI, de Leon Boenig G, Deng Y, Eidenschenk C, Everett C, Gancia E, Ganguli A, Gobbi A, Hawkins J, Johnson AR, Kiefer JR, La H, Lockey P, Norman M, Ouyang W, Qin A, Wakes N, Waszkowycz B, Wong H. van Niel MB, et al. Among authors: lockey p. Bioorg Med Chem Lett. 2014 Dec 15;24(24):5769-5776. doi: 10.1016/j.bmcl.2014.10.037. Epub 2014 Oct 25. Bioorg Med Chem Lett. 2014. PMID: 25453817
Application of virtual screening to the discovery of novel nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with potential for the treatment of cancer and axonopathies.
Clark DE, Waszkowycz B, Wong M, Lockey PM, Adalbert R, Gilley J, Clark J, Coleman MP. Clark DE, et al. Among authors: lockey pm. Bioorg Med Chem Lett. 2016 Jun 15;26(12):2920-2926. doi: 10.1016/j.bmcl.2016.04.039. Epub 2016 Apr 16. Bioorg Med Chem Lett. 2016. PMID: 27158141 Free article.
Identification of tertiary sulfonamides as RORc inverse agonists.
Fauber BP, René O, Burton B, Everett C, Gobbi A, Hawkins J, Johnson AR, Liimatta M, Lockey P, Norman M, Wong H. Fauber BP, et al. Among authors: lockey p. Bioorg Med Chem Lett. 2014 May 1;24(9):2182-7. doi: 10.1016/j.bmcl.2014.03.038. Epub 2014 Mar 21. Bioorg Med Chem Lett. 2014. PMID: 24685544
Reduction in lipophilicity improved the solubility, plasma-protein binding, and permeability of tertiary sulfonamide RORc inverse agonists.
Fauber BP, René O, de Leon Boenig G, Burton B, Deng Y, Eidenschenk C, Everett C, Gobbi A, Hymowitz SG, Johnson AR, La H, Liimatta M, Lockey P, Norman M, Ouyang W, Wang W, Wong H. Fauber BP, et al. Among authors: lockey p. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3891-7. doi: 10.1016/j.bmcl.2014.06.048. Epub 2014 Jun 25. Bioorg Med Chem Lett. 2014. PMID: 25017032
Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action.
René O, Fauber BP, Boenig Gde L, Burton B, Eidenschenk C, Everett C, Gobbi A, Hymowitz SG, Johnson AR, Kiefer JR, Liimatta M, Lockey P, Norman M, Ouyang W, Wallweber HA, Wong H. René O, et al. Among authors: lockey p. ACS Med Chem Lett. 2014 Dec 4;6(3):276-81. doi: 10.1021/ml500420y. eCollection 2015 Mar 12. ACS Med Chem Lett. 2014. PMID: 25815138 Free PMC article.
Discovery of 1-{4-[3-fluoro-4-((3s,6r)-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a potent, selective, and orally bioavailable retinoic acid receptor-related orphan receptor C (RORc or RORγ) inverse agonist.
Fauber BP, René O, Deng Y, DeVoss J, Eidenschenk C, Everett C, Ganguli A, Gobbi A, Hawkins J, Johnson AR, La H, Lesch J, Lockey P, Norman M, Ouyang W, Summerhill S, Wong H. Fauber BP, et al. Among authors: lockey p. J Med Chem. 2015 Jul 9;58(13):5308-22. doi: 10.1021/acs.jmedchem.5b00597. Epub 2015 Jun 23. J Med Chem. 2015. PMID: 26061388
Identification of N-sulfonyl-tetrahydroquinolines as RORc inverse agonists.
Fauber BP, Gobbi A, Savy P, Burton B, Deng Y, Everett C, La H, Johnson AR, Lockey P, Norman M, Wong H. Fauber BP, et al. Among authors: lockey p. Bioorg Med Chem Lett. 2015 Oct 1;25(19):4109-13. doi: 10.1016/j.bmcl.2015.08.028. Epub 2015 Aug 14. Bioorg Med Chem Lett. 2015. PMID: 26321361
Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists.
Cramp S, Dyke HJ, Higgs C, Clark DE, Gill M, Savy P, Jennings N, Price S, Lockey PM, Norman D, Porres S, Wilson F, Jones A, Ramsden N, Mangano R, Leggate D, Andersson M, Hale R. Cramp S, et al. Among authors: lockey pm. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2516-9. doi: 10.1016/j.bmcl.2010.02.097. Epub 2010 Mar 3. Bioorg Med Chem Lett. 2010. PMID: 20299215
Quinazoline and benzimidazole MCH-1R antagonists.
Arienzo R, Cramp S, Dyke HJ, Lockey PM, Norman D, Roach AG, Smith P, Wong M, Wren SP. Arienzo R, et al. Among authors: lockey pm. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1403-7. doi: 10.1016/j.bmcl.2006.11.092. Epub 2006 Dec 2. Bioorg Med Chem Lett. 2007. PMID: 17178222
37 results