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Page 1
Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor.
Miller DC, Reuillon T, Molyneux L, Blackburn T, Cook SJ, Edwards N, Endicott JA, Golding BT, Griffin RJ, Hardcastle I, Harnor SJ, Heptinstall A, Lochhead P, Martin MP, Martin NC, Myers S, Newell DR, Noble RA, Phillips N, Rigoreau L, Thomas H, Tucker JA, Wang LZ, Waring MJ, Wong AC, Wedge SR, Noble MEM, Cano C. Miller DC, et al. Among authors: newell dr. J Med Chem. 2022 May 12;65(9):6513-6540. doi: 10.1021/acs.jmedchem.1c01756. Epub 2022 Apr 25. J Med Chem. 2022. PMID: 35468293 Free PMC article.
Structure-Based Design of Potent and Orally Active Isoindolinone Inhibitors of MDM2-p53 Protein-Protein Interaction.
Chessari G, Hardcastle IR, Ahn JS, Anil B, Anscombe E, Bawn RH, Bevan LD, Blackburn TJ, Buck I, Cano C, Carbain B, Castro J, Cons B, Cully SJ, Endicott JA, Fazal L, Golding BT, Griffin RJ, Haggerty K, Harnor SJ, Hearn K, Hobson S, Holvey RS, Howard S, Jennings CE, Johnson CN, Lunec J, Miller DC, Newell DR, Noble MEM, Reeks J, Revill CH, Riedinger C, St Denis JD, Tamanini E, Thomas H, Thompson NT, Vinković M, Wedge SR, Williams PA, Wilsher NE, Zhang B, Zhao Y. Chessari G, et al. Among authors: newell dr. J Med Chem. 2021 Apr 8;64(7):4071-4088. doi: 10.1021/acs.jmedchem.0c02188. Epub 2021 Mar 24. J Med Chem. 2021. PMID: 33761253
2-Arylamino-6-ethynylpurines are cysteine-targeting irreversible inhibitors of Nek2 kinase.
Matheson CJ, Coxon CR, Bayliss R, Boxall K, Carbain B, Fry AM, Hardcastle IR, Harnor SJ, Mas-Droux C, Newell DR, Richards MW, Sivaprakasam M, Turner D, Griffin RJ, Golding BT, Cano C. Matheson CJ, et al. Among authors: newell dr. RSC Med Chem. 2020 May 22;11(6):707-731. doi: 10.1039/d0md00074d. eCollection 2020 Jun 1. RSC Med Chem. 2020. PMID: 33479670 Free PMC article.
Selective DNA-PKcs inhibition extends the therapeutic index of localized radiotherapy and chemotherapy.
Willoughby CE, Jiang Y, Thomas HD, Willmore E, Kyle S, Wittner A, Phillips N, Zhao Y, Tudhope SJ, Prendergast L, Junge G, Lourenco LM, Finlay MRV, Turner P, Munck JM, Griffin RJ, Rennison T, Pickles J, Cano C, Newell DR, Reeves HL, Ryan AJ, Wedge SR. Willoughby CE, et al. Among authors: newell dr. J Clin Invest. 2020 Jan 2;130(1):258-271. doi: 10.1172/JCI127483. J Clin Invest. 2020. PMID: 31581151 Free PMC article.
Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4.
Myers SM, Miller DC, Molyneux L, Arasta M, Bawn RH, Blackburn TJ, Cook SJ, Edwards N, Endicott JA, Golding BT, Griffin RJ, Hammonds T, Hardcastle IR, Harnor SJ, Heptinstall AB, Lochhead PA, Martin MP, Martin NC, Newell DR, Owen PJ, Pang LC, Reuillon T, Rigoreau LJM, Thomas HD, Tucker JA, Wang LZ, Wong AC, Noble MEM, Wedge SR, Cano C. Myers SM, et al. Among authors: newell dr. Eur J Med Chem. 2019 Sep 15;178:530-543. doi: 10.1016/j.ejmech.2019.05.057. Epub 2019 May 25. Eur J Med Chem. 2019. PMID: 31212132
208 results