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(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells.
Barsyte-Lovejoy D, Li F, Oudhoff MJ, Tatlock JH, Dong A, Zeng H, Wu H, Freeman SA, Schapira M, Senisterra GA, Kuznetsova E, Marcellus R, Allali-Hassani A, Kennedy S, Lambert JP, Couzens AL, Aman A, Gingras AC, Al-Awar R, Fish PV, Gerstenberger BS, Roberts L, Benn CL, Grimley RL, Braam MJ, Rossi FM, Sudol M, Brown PJ, Bunnage ME, Owen DR, Zaph C, Vedadi M, Arrowsmith CH. Barsyte-Lovejoy D, et al. Among authors: roberts l. Proc Natl Acad Sci U S A. 2014 Sep 2;111(35):12853-8. doi: 10.1073/pnas.1407358111. Epub 2014 Aug 18. Proc Natl Acad Sci U S A. 2014. PMID: 25136132 Free PMC article.
Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT₂C) receptor agonists with exquisite functional selectivity over 5-HT₂A and 5-HT₂B receptors.
Storer RI, Brennan PE, Brown AD, Bungay PJ, Conlon KM, Corbett MS, DePianta RP, Fish PV, Heifetz A, Ho DK, Jessiman AS, McMurray G, de Oliveira CA, Roberts LR, Root JA, Shanmugasundaram V, Shapiro MJ, Skerten M, Westbrook D, Wheeler S, Whitlock GA, Wright J. Storer RI, et al. J Med Chem. 2014 Jun 26;57(12):5258-69. doi: 10.1021/jm5003292. Epub 2014 Jun 17. J Med Chem. 2014. PMID: 24878222
Acidic triazoles as soluble guanylate cyclase stimulators.
Roberts LR, Bradley PA, Bunnage ME, England KS, Fairman D, Fobian YM, Fox DN, Gymer GE, Heasley SE, Molette J, Smith GL, Schmidt MA, Tones MA, Dack KN. Roberts LR, et al. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6515-8. doi: 10.1016/j.bmcl.2011.08.071. Epub 2011 Aug 28. Bioorg Med Chem Lett. 2011. PMID: 21924901
Sulfonamides as selective oestrogen receptor β agonists.
Roberts LR, Armor D, Barker C, Bent A, Bess K, Brown A, Favor DA, Ellis D, Irving SL, MacKenny M, Phillips C, Pullen N, Stennett A, Strand L, Styles M. Roberts LR, et al. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5680-3. doi: 10.1016/j.bmcl.2011.08.041. Epub 2011 Aug 16. Bioorg Med Chem Lett. 2011. PMID: 21885279
Discovery of PF-184563, a potent and selective V1a antagonist for the treatment of dysmenorrhoea. The influence of compound flexibility on microsomal stability.
Johnson PS, Ryckmans T, Bryans J, Beal DM, Dack KN, Feeder N, Harrison A, Lewis M, Mason HJ, Mills J, Newman J, Pasquinet C, Rawson DJ, Roberts LR, Russell R, Spark D, Stobie A, Underwood TJ, Ward R, Wheeler S. Johnson PS, et al. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5684-7. doi: 10.1016/j.bmcl.2011.08.038. Epub 2011 Aug 12. Bioorg Med Chem Lett. 2011. PMID: 21885275
Kappa agonist CovX-Bodies.
Roberts LR, Brady K, Brown A, Davey D, Feng L, Huang H, Liu D, Malet L, McMurray G, Phelan A, Saunders K, Bhat A. Roberts LR, et al. Bioorg Med Chem Lett. 2012 Jun 15;22(12):4173-8. doi: 10.1016/j.bmcl.2012.04.040. Epub 2012 Apr 25. Bioorg Med Chem Lett. 2012. PMID: 22583618
3,999 results