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Discovery and optimization of covalent Bcl-xL antagonists.
Mukherjee H, Su N, Belmonte MA, Hargreaves D, Patel J, Tentarelli S, Aquila B, Grimster NP. Mukherjee H, et al. Among authors: grimster np. Bioorg Med Chem Lett. 2019 Dec 1;29(23):126682. doi: 10.1016/j.bmcl.2019.126682. Epub 2019 Sep 13. Bioorg Med Chem Lett. 2019. PMID: 31606346
Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors.
Grimster NP, Anderson E, Alimzhanov M, Bebernitz G, Bell K, Chuaqui C, Deegan T, Ferguson AD, Gero T, Harsch A, Huszar D, Kawatkar A, Kettle JG, Lyne P, Read JA, Rivard Costa C, Ruston L, Schroeder P, Shi J, Su Q, Throner S, Toader D, Vasbinder M, Woessner R, Wang H, Wu A, Ye M, Zheng W, Zinda M. Grimster NP, et al. J Med Chem. 2018 Jun 28;61(12):5235-5244. doi: 10.1021/acs.jmedchem.8b00076. Epub 2018 Jun 13. J Med Chem. 2018. PMID: 29856615
Discovery of (2R)-N-[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]-1H-indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a Potent and Selective Janus Kinase 1 Inhibitor.
Su Q, Banks E, Bebernitz G, Bell K, Borenstein CF, Chen H, Chuaqui CE, Deng N, Ferguson AD, Kawatkar S, Grimster NP, Ruston L, Lyne PD, Read JA, Peng X, Pei X, Fawell S, Tang Z, Throner S, Vasbinder MM, Wang H, Winter-Holt J, Woessner R, Wu A, Yang W, Zinda M, Kettle JG. Su Q, et al. Among authors: grimster np. J Med Chem. 2020 May 14;63(9):4517-4527. doi: 10.1021/acs.jmedchem.9b01392. Epub 2020 Apr 28. J Med Chem. 2020. PMID: 32297743
Optimization of a series of potent, selective and orally bioavailable SYK inhibitors.
Grimster NP, Gingipalli L, Barlaam B, Su Q, Zheng X, Watson D, Wang H, Simpson I, Pike A, Balazs A, Boiko S, Ikeda TP, Impastato AC, Jones NH, Kawatkar S, Kemmitt P, Lamont S, Patel J, Read J, Sarkar U, Sha L, Tomlinson RC, Wang H, Wilson DM, Zehnder TE, Wang L, Wang P, Goldberg FW, Shao W, Fawell S, Dry H, Dowling JE, Edmondson SD. Grimster NP, et al. Bioorg Med Chem Lett. 2020 Oct 1;30(19):127433. doi: 10.1016/j.bmcl.2020.127433. Epub 2020 Jul 24. Bioorg Med Chem Lett. 2020. PMID: 32717371
Covalent PROTACs: the best of both worlds?
Grimster NP. Grimster NP. RSC Med Chem. 2021 Jul 15;12(9):1452-1458. doi: 10.1039/d1md00191d. eCollection 2021 Sep 23. RSC Med Chem. 2021. PMID: 34671730 Free PMC article.
Discovery of the Potent and Selective Inhaled Janus Kinase 1 Inhibitor AZD4604 and Its Preclinical Characterization.
Nilsson M, Berggren K, Berglund S, Cerboni S, Collins M, Dahl G, Elmqvist D, Grimster NP, Hendrickx R, Johansson JR, Kettle JG, Lepistö M, Rhedin M, Smailagic A, Su Q, Wennberg T, Wu A, Österlund T, Naessens T, Mitra S. Nilsson M, et al. Among authors: grimster np. J Med Chem. 2023 Oct 12;66(19):13400-13415. doi: 10.1021/acs.jmedchem.3c00554. Epub 2023 Sep 22. J Med Chem. 2023. PMID: 37738648
Discovery, Optimization, and Biological Evaluation of Arylpyridones as Cbl-b Inhibitors.
Mfuh AM, Boerth JA, Bommakanti G, Chan C, Chinn AJ, Code E, Fricke PJ, Giblin KA, Gohlke A, Hansel C, Hariparsad N, Hughes SJ, Jin M, Kantae V, Kavanagh SL, Lamb ML, Lane J, Moore R, Puri T, Quinn TR, Reddy I, Robb GR, Robbins KJ, Gancedo Rodrigo M, Schimpl M, Singh B, Singh M, Tang H, Thomson C, Walsh JJ, Ware J, Watson IDG, Ye MW, Wrigley GL, Zhang AX, Zhang Y, Grimster NP. Mfuh AM, et al. Among authors: grimster np. J Med Chem. 2024 Jan 25;67(2):1500-1512. doi: 10.1021/acs.jmedchem.3c02083. Epub 2024 Jan 16. J Med Chem. 2024. PMID: 38227216
28 results