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Structure-Based Design of Potent, Selective, and Orally Bioavailable VPS34 Kinase Inhibitors.
Hu DX, Patel S, Chen H, Wang S, Staben ST, Dimitrova YN, Wallweber HA, Lee JY, Chan GKY, Sneeringer CJ, Prangley MS, Moffat JG, Wu KC, Schutt LK, Salphati L, Pang J, McNamara E, Huang H, Chen Y, Wang Y, Zhao W, Lim J, Murthy A, Siu M. Hu DX, et al. Among authors: chan gky. J Med Chem. 2022 Sep 8;65(17):11500-11512. doi: 10.1021/acs.jmedchem.1c01180. Epub 2021 Nov 15. J Med Chem. 2022. PMID: 34779204
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: chan gky. 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 3,5-substituted 6-azaindazoles as potent pan-Pim inhibitors.
Hu H, Wang X, Chan GK, Chang JH, Do S, Drummond J, Ebens A, Lee W, Ly J, Lyssikatos JP, Murray J, Moffat JG, Chao Q, Tsui V, Wallweber H, Kolesnikov A. Hu H, et al. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5258-64. doi: 10.1016/j.bmcl.2015.09.052. Epub 2015 Sep 30. Bioorg Med Chem Lett. 2015. PMID: 26459208
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: chan gky. 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
The discovery of tricyclic pyridone JAK2 inhibitors. Part 1: hit to lead.
Siu T, Kozina ES, Jung J, Rosenstein C, Mathur A, Altman MD, Chan G, Xu L, Bachman E, Mo JR, Bouthillette M, Rush T, Dinsmore CJ, Marshall CG, Young JR. Siu T, et al. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7421-5. doi: 10.1016/j.bmcl.2010.10.031. Epub 2010 Oct 12. Bioorg Med Chem Lett. 2010. PMID: 21044843
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