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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. Among authors: ryckmans t. 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
N-[(3S)-Pyrrolidin-3-yl]benzamides as novel dual serotonin and noradrenaline reuptake inhibitors: impact of small structural modifications on P-gp recognition and CNS penetration.
Wakenhut F, Allan GA, Fish PV, Fray MJ, Harrison AC, McCoy R, Phillips SC, Ryckmans T, Stobie A, Westbrook D, Westbrook SL, Whitlock GA. Wakenhut F, et al. Among authors: ryckmans t. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5078-81. doi: 10.1016/j.bmcl.2009.07.049. Epub 2009 Jul 31. Bioorg Med Chem Lett. 2009. PMID: 19647430
TAK1 inhibition in the DFG-out conformation.
Kilty I, Green MP, Bell AS, Brown DG, Dodd PG, Hewson C, Hughes SJ, Phillips C, Ryckmans T, Smith RT, van Hoorn WP, Cohen P, Jones LH. Kilty I, et al. Among authors: ryckmans t. Chem Biol Drug Des. 2013 Nov;82(5):500-5. doi: 10.1111/cbdd.12169. Chem Biol Drug Des. 2013. PMID: 23745990
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