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Discovery of a potent, covalent BTK inhibitor for B-cell lymphoma.
Wu H, Wang W, Liu F, Weisberg EL, Tian B, Chen Y, Li B, Wang A, Wang B, Zhao Z, McMillin DW, Hu C, Li H, Wang J, Liang Y, Buhrlage SJ, Liang J, Liu J, Yang G, Brown JR, Treon SP, Mitsiades CS, Griffin JD, Liu Q, Gray NS. Wu H, et al. Among authors: chen y. ACS Chem Biol. 2014 May 16;9(5):1086-91. doi: 10.1021/cb4008524. Epub 2014 Mar 17. ACS Chem Biol. 2014. PMID: 24556163 Free PMC article.
Upregulation of IGF1R by mutant RAS in leukemia and potentiation of RAS signaling inhibitors by small-molecule inhibition of IGF1R.
Weisberg E, Nonami A, Chen Z, Nelson E, Chen Y, Liu F, Cho H, Zhang J, Sattler M, Mitsiades C, Wong KK, Liu Q, Gray NS, Griffin JD. Weisberg E, et al. Among authors: chen z, chen y. Clin Cancer Res. 2014 Nov 1;20(21):5483-95. doi: 10.1158/1078-0432.CCR-14-0902. Epub 2014 Sep 3. Clin Cancer Res. 2014. PMID: 25186968 Free PMC article.
Discovery of a Highly Selective STK16 Kinase Inhibitor.
Liu F, Wang J, Yang X, Li B, Wu H, Qi S, Chen C, Liu X, Yu K, Wang W, Zhao Z, Wang A, Chen Y, Wang L, Gray NS, Liu J, Zhang X, Liu Q. Liu F, et al. Among authors: chen c, chen y. ACS Chem Biol. 2016 Jun 17;11(6):1537-43. doi: 10.1021/acschembio.6b00250. Epub 2016 Apr 22. ACS Chem Biol. 2016. PMID: 27082499
Discovery of N-(3-(5-((3-acrylamido-4-(morpholine-4-carbonyl)phenyl)amino)-1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-2-methylphenyl)-4-(tert-butyl)benzamide (CHMFL-BTK-01) as a highly selective irreversible Bruton's tyrosine kinase (BTK) inhibitor.
Liang Q, Chen Y, Yu K, Chen C, Zhang S, Wang A, Wang W, Wu H, Liu X, Wang B, Wang L, Hu Z, Wang W, Ren T, Zhang S, Liu Q, Yun CH, Liu J. Liang Q, et al. Among authors: chen c, chen y. Eur J Med Chem. 2017 May 5;131:107-125. doi: 10.1016/j.ejmech.2017.03.001. Epub 2017 Mar 2. Eur J Med Chem. 2017. PMID: 28315597
Irreversible inhibition of BTK kinase by a novel highly selective inhibitor CHMFL-BTK-11 suppresses inflammatory response in rheumatoid arthritis model.
Wu H, Huang Q, Qi Z, Chen Y, Wang A, Chen C, Liang Q, Wang J, Chen W, Dong J, Yu K, Hu C, Wang W, Liu X, Deng Y, Wang L, Wang B, Li X, Gray NS, Liu J, Wei W, Liu Q. Wu H, et al. Among authors: chen c, chen w, chen y. Sci Rep. 2017 Mar 28;7(1):466. doi: 10.1038/s41598-017-00482-4. Sci Rep. 2017. PMID: 28352114 Free PMC article.
Structure-activity relationship investigation for benzonaphthyridinone derivatives as novel potent Bruton's tyrosine kinase (BTK) irreversible inhibitors.
Wang B, Deng Y, Chen Y, Yu K, Wang A, Liang Q, Wang W, Chen C, Wu H, Hu C, Miao W, Hur W, Wang W, Hu Z, Weisberg EL, Wang J, Ren T, Wang Y, Gray NS, Liu Q, Liu J. Wang B, et al. Among authors: chen c, chen y. Eur J Med Chem. 2017 Sep 8;137:545-557. doi: 10.1016/j.ejmech.2017.06.016. Epub 2017 Jun 9. Eur J Med Chem. 2017. PMID: 28628824
Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR associated drug resistant mutants in NSCLC.
Chen Y, Wu J, Wang A, Qi Z, Jiang T, Chen C, Zou F, Hu C, Wang W, Wu H, Hu Z, Wang W, Wang B, Wang L, Ren T, Zhang S, Liu Q, Liu J. Chen Y, et al. Among authors: chen c. Eur J Med Chem. 2017 Oct 20;139:674-697. doi: 10.1016/j.ejmech.2017.08.035. Epub 2017 Aug 18. Eur J Med Chem. 2017. PMID: 28850922
Discovery of (E)-N-(4-methyl-5-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thiazol-2-yl)-2-(4-methylpiperazin-1-yl)acetamide (IHMT-TRK-284) as a novel orally available type II TRK kinase inhibitor capable of overcoming multiple resistant mutants.
Wang B, Zhang W, Liu X, Zou F, Wang J, Liu Q, Wang A, Hu Z, Chen Y, Qi S, Jiang Z, Chen C, Hu C, Wang L, Wang W, Liu Q, Liu J. Wang B, et al. Among authors: chen c, chen y. Eur J Med Chem. 2020 Dec 1;207:112744. doi: 10.1016/j.ejmech.2020.112744. Epub 2020 Aug 30. Eur J Med Chem. 2020. PMID: 32949955
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