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899 results

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Page 1
Discovery of Spiro-azaindoline Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1).
Chan BK, Seward E, Lainchbury M, Brewer TF, An L, Blench T, Cartwright MW, Chan GKY, Choo EF, Drummond J, Elliott RL, Gancia E, Gazzard L, Hu B, Jones GE, Luo X, Madin A, Malhotra S, Moffat JG, Pang J, Salphati L, Sneeringer CJ, Stivala CE, Wei B, Wang W, Wu P, Heffron TP. Chan BK, et al. Among authors: drummond j. ACS Med Chem Lett. 2021 Dec 8;13(1):84-91. doi: 10.1021/acsmedchemlett.1c00473. eCollection 2022 Jan 13. ACS Med Chem Lett. 2021. PMID: 35059127 Free PMC article.
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
Estrada AA, Liu X, Baker-Glenn C, Beresford A, Burdick DJ, Chambers M, Chan BK, Chen H, Ding X, DiPasquale AG, Dominguez SL, Dotson J, Drummond J, Flagella M, Flynn S, Fuji R, Gill A, Gunzner-Toste J, Harris SF, Heffron TP, Kleinheinz T, Lee DW, Le Pichon CE, Lyssikatos JP, Medhurst AD, Moffat JG, Mukund S, Nash K, Scearce-Levie K, Sheng Z, Shore DG, Tran T, Trivedi N, Wang S, Zhang S, Zhang X, Zhao G, Zhu H, Sweeney ZK. Estrada AA, et al. Among authors: drummond j. J Med Chem. 2012 Nov 26;55(22):9416-33. doi: 10.1021/jm301020q. Epub 2012 Oct 15. J Med Chem. 2012. PMID: 22985112
Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
Estrada AA, Chan BK, Baker-Glenn C, Beresford A, Burdick DJ, Chambers M, Chen H, Dominguez SL, Dotson J, Drummond J, Flagella M, Fuji R, Gill A, Halladay J, Harris SF, Heffron TP, Kleinheinz T, Lee DW, Le Pichon CE, Liu X, Lyssikatos JP, Medhurst AD, Moffat JG, Nash K, Scearce-Levie K, Sheng Z, Shore DG, Wong S, Zhang S, Zhang X, Zhu H, Sweeney ZK. Estrada AA, et al. Among authors: drummond j. J Med Chem. 2014 Feb 13;57(3):921-36. doi: 10.1021/jm401654j. Epub 2014 Jan 15. J Med Chem. 2014. PMID: 24354345
Discovery of a Highly Selective, Brain-Penetrant Aminopyrazole LRRK2 Inhibitor.
Chan BK, Estrada AA, Chen H, Atherall J, Baker-Glenn C, Beresford A, Burdick DJ, Chambers M, Dominguez SL, Drummond J, Gill A, Kleinheinz T, Le Pichon CE, Medhurst AD, Liu X, Moffat JG, Nash K, Scearce-Levie K, Sheng Z, Shore DG, Van de Poël H, Zhang S, Zhu H, Sweeney ZK. Chan BK, et al. Among authors: drummond j. ACS Med Chem Lett. 2012 Nov 23;4(1):85-90. doi: 10.1021/ml3003007. eCollection 2013 Jan 10. ACS Med Chem Lett. 2012. PMID: 24900567 Free PMC article.
Discovery of potent azaindazole leucine-rich repeat kinase 2 (LRRK2) inhibitors possessing a key intramolecular hydrogen bond - Part 2.
Shore DGM, Sweeney ZK, Beresford A, Chan BK, Chen H, Drummond J, Gill A, Kleinheinz T, Liu X, Medhurst AD, McIver EG, Moffat JG, Zhu H, Estrada AA. Shore DGM, et al. Among authors: drummond j. Bioorg Med Chem Lett. 2019 Feb 15;29(4):674-680. doi: 10.1016/j.bmcl.2018.10.017. Epub 2018 Oct 12. Bioorg Med Chem Lett. 2019. PMID: 30522953
Discovery of 5-Azaindazole (GNE-955) as a Potent Pan-Pim Inhibitor with Optimized Bioavailability.
Wang X, Kolesnikov A, Tay S, Chan G, Chao Q, Do S, Drummond J, Ebens AJ, Liu N, Ly J, Harstad E, Hu H, Moffat J, Munugalavadla V, Murray J, Slaga D, Tsui V, Volgraf M, Wallweber H, Chang JH. Wang X, et al. Among authors: drummond j. J Med Chem. 2017 May 25;60(10):4458-4473. doi: 10.1021/acs.jmedchem.7b00418. Epub 2017 May 5. J Med Chem. 2017. PMID: 28445037
Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma.
Wang X, Blackaby W, Allen V, Chan GKY, Chang JH, Chiang PC, Diène C, Drummond J, Do S, Fan E, Harstad EB, Hodges A, Hu H, Jia W, Kofie W, Kolesnikov A, Lyssikatos JP, Ly J, Matteucci M, Moffat JG, Munugalavadla V, Murray J, Nash D, Noland CL, Del Rosario G, Ross L, Rouse C, Sharpe A, Slaga D, Sun M, Tsui V, Wallweber H, Yu SF, Ebens AJ. Wang X, et al. Among authors: drummond j. J Med Chem. 2019 Feb 28;62(4):2140-2153. doi: 10.1021/acs.jmedchem.8b01857. Epub 2019 Feb 20. J Med Chem. 2019. PMID: 30715878
A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B.
Aliagas-Martin I, Burdick D, Corson L, Dotson J, Drummond J, Fields C, Huang OW, Hunsaker T, Kleinheinz T, Krueger E, Liang J, Moffat J, Phillips G, Pulk R, Rawson TE, Ultsch M, Walker L, Wiesmann C, Zhang B, Zhu BY, Cochran AG. Aliagas-Martin I, et al. Among authors: drummond j. J Med Chem. 2009 May 28;52(10):3300-7. doi: 10.1021/jm9000314. J Med Chem. 2009. PMID: 19402633
899 results