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12 results

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Page 1
Identification and Optimization of a Ligand-Efficient Benzoazepinone Bromodomain and Extra Terminal (BET) Family Acetyl-Lysine Mimetic into the Oral Candidate Quality Molecule I-BET432.
Humphreys PG, Anderson NA, Bamborough P, Baxter A, Chung CW, Cookson R, Craggs PD, Dalton T, Fournier JCL, Gordon LJ, Gray HF, Gray MW, Gregory R, Hirst DJ, Jamieson C, Jones KL, Kessedjian H, Lugo D, McGonagle G, Patel VK, Patten C, Poole DL, Prinjha RK, Ramirez-Molina C, Rioja I, Seal G, Stafford KAJ, Shah RR, Tape D, Theodoulou NH, Tomlinson L, Ukuser S, Wall ID, Wellaway N, White G. Humphreys PG, et al. Among authors: wellaway n. J Med Chem. 2022 Nov 24;65(22):15174-15207. doi: 10.1021/acs.jmedchem.2c01102. Epub 2022 Nov 15. J Med Chem. 2022. PMID: 36378954
Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease.
Amour A, Barton N, Cooper AW, Inglis G, Jamieson C, Luscombe CN, Morrell J, Peace S, Perez D, Rowland P, Tame CJ, Uddin S, Vitulli G, Wellaway N. Amour A, et al. Among authors: wellaway n. J Med Chem. 2016 Aug 11;59(15):7239-51. doi: 10.1021/acs.jmedchem.6b00799. Epub 2016 Jul 27. J Med Chem. 2016. PMID: 27429068 Free article.
Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase.
Harris PA, Faucher N, George N, Eidam PM, King BW, White GV, Anderson NA, Bandyopadhyay D, Beal AM, Beneton V, Berger SB, Campobasso N, Campos S, Capriotti CA, Cox JA, Daugan A, Donche F, Fouchet MH, Finger JN, Geddes B, Gough PJ, Grondin P, Hoffman BL, Hoffman SJ, Hutchinson SE, Jeong JU, Jigorel E, Lamoureux P, Leister LK, Lich JD, Mahajan MK, Meslamani J, Mosley JE, Nagilla R, Nassau PM, Ng SL, Ouellette MT, Pasikanti KK, Potvain F, Reilly MA, Rivera EJ, Sautet S, Schaeffer MC, Sehon CA, Sun H, Thorpe JH, Totoritis RD, Ward P, Wellaway N, Wisnoski DD, Woolven JM, Bertin J, Marquis RW. Harris PA, et al. Among authors: wellaway n. J Med Chem. 2019 May 23;62(10):5096-5110. doi: 10.1021/acs.jmedchem.9b00318. Epub 2019 May 2. J Med Chem. 2019. PMID: 31013427
Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening.
Wellaway CR, Amans D, Bamborough P, Barnett H, Bit RA, Brown JA, Carlson NR, Chung CW, Cooper AWJ, Craggs PD, Davis RP, Dean TW, Evans JP, Gordon L, Harada IL, Hirst DJ, Humphreys PG, Jones KL, Lewis AJ, Lindon MJ, Lugo D, Mahmood M, McCleary S, Medeiros P, Mitchell DJ, O'Sullivan M, Le Gall A, Patel VK, Patten C, Poole DL, Shah RR, Smith JE, Stafford KAJ, Thomas PJ, Vimal M, Wall ID, Watson RJ, Wellaway N, Yao G, Prinjha RK. Wellaway CR, et al. Among authors: wellaway n. J Med Chem. 2020 Jan 23;63(2):714-746. doi: 10.1021/acs.jmedchem.9b01670. Epub 2020 Jan 6. J Med Chem. 2020. PMID: 31904959
Investigation of Janus Kinase (JAK) Inhibitors for Lung Delivery and the Importance of Aldehyde Oxidase Metabolism.
Wellaway CR, Baldwin IR, Bamborough P, Barker D, Bartholomew MA, Chung CW, Dümpelfeld B, Evans JP, Fazakerley NJ, Homes P, Keeling SP, Lewell XQ, McNab FW, Morley J, Needham D, Neu M, van Oosterhout AJM, Pal A, Reinhard FBM, Rianjongdee F, Robertson CM, Rowland P, Shah RR, Sherriff EB, Sloan LA, Teague S, Thomas DA, Wellaway N, Wojno-Picon J, Woolven JM, Coe DM. Wellaway CR, et al. Among authors: wellaway n. J Med Chem. 2022 Jan 13;65(1):633-664. doi: 10.1021/acs.jmedchem.1c01765. Epub 2021 Dec 20. J Med Chem. 2022. PMID: 34928601
Discovery of a potent series of non-steroidal non α-trifluoromethyl carbinol glucocorticoid receptor agonists with reduced lipophilicity.
Diallo H, Angell DC, Barnett HA, Biggadike K, Coe DM, Cooper TW, Craven A, Gray JR, House D, Jack TI, Keeling SP, Macdonald SJ, McLay IM, Oliver S, Taylor SJ, Uings IJ, Wellaway N. Diallo H, et al. Among authors: wellaway n. Bioorg Med Chem Lett. 2011 Feb 15;21(4):1126-33. doi: 10.1016/j.bmcl.2010.12.121. Epub 2010 Dec 31. Bioorg Med Chem Lett. 2011. PMID: 21257309
Correction to Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease.
Amour A, Barton N, Cooper AW, Inglis G, Jamieson C, Luscombe CN, Morrell J, Peace S, Perez D, Rowland P, Tame CJ, Uddin S, Vitulli G, Wellaway N. Amour A, et al. Among authors: wellaway n. J Med Chem. 2016 Sep 8;59(17):8148. doi: 10.1021/acs.jmedchem.6b01157. Epub 2016 Aug 22. J Med Chem. 2016. PMID: 27548024 No abstract available.
Correction to Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease.
Amour A, Barton N, Cooper AW, Inglis G, Jamieson C, Luscombe CN, Morrell J, Peace S, Perez D, Rowland P, Tame CJ, Uddin S, Vitulli G, Wellaway N. Amour A, et al. Among authors: wellaway n. J Med Chem. 2016 Oct 27;59(20):9574. doi: 10.1021/acs.jmedchem.6b01461. Epub 2016 Oct 11. J Med Chem. 2016. PMID: 27726364 No abstract available.
12 results