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Ibrutinib targets mutant-EGFR kinase with a distinct binding conformation.
Wang A, Yan XE, Wu H, Wang W, Hu C, Chen C, Zhao Z, Zhao P, Li X, Wang L, Wang B, Ye Z, Wang J, Wang C, Zhang W, Gray NS, Weisberg EL, Chen L, Liu J, Yun CH, Liu Q. Wang A, et al. Among authors: wang w, wang l, wang j, wang c, wang b. Oncotarget. 2016 Oct 25;7(43):69760-69769. doi: 10.18632/oncotarget.11951. Oncotarget. 2016. PMID: 27626175 Free PMC article.
Discovery of 2-((3-Acrylamido-4-methylphenyl)amino)-N-(2-methyl-5-(3,4,5-trimethoxybenzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-BMX-078) as a Highly Potent and Selective Type II Irreversible Bone Marrow Kinase in the X Chromosome (BMX) Kinase Inhibitor.
Liang X, Lv F, Wang B, Yu K, Wu H, Qi Z, Jiang Z, Chen C, Wang A, Miao W, Wang W, Hu Z, Liu J, Liu X, Zhao Z, Wang L, Zhang S, Ye Z, Wang C, Ren T, Wang Y, Liu Q, Liu J. Liang X, et al. Among authors: wang w, wang l, wang y, wang c, wang b, wang a. J Med Chem. 2017 Mar 9;60(5):1793-1816. doi: 10.1021/acs.jmedchem.6b01413. Epub 2017 Feb 14. J Med Chem. 2017. PMID: 28140585
Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode.
Wang A, Li X, Wu H, Zou F, Yan XE, Chen C, Hu C, Yu K, Wang W, Zhao P, Wu J, Qi Z, Wang W, Wang B, Wang L, Ren T, Zhang S, Yun CH, Liu J, Liu Q. Wang A, et al. Among authors: wang w, wang l, wang b. J Med Chem. 2017 Apr 13;60(7):2944-2962. doi: 10.1021/acs.jmedchem.6b01907. Epub 2017 Mar 22. J Med Chem. 2017. PMID: 28282122
Discovery and characterization of a novel irreversible EGFR mutants selective and potent kinase inhibitor CHMFL-EGFR-26 with a distinct binding mode.
Hu C, Wang A, Wu H, Qi Z, Li X, Yan XE, Chen C, Yu K, Zou F, Wang W, Wang W, Wu J, Liu J, Wang B, Wang L, Ren T, Zhang S, Yun CH, Liu J, Liu Q. Hu C, et al. Among authors: wang w, wang l, wang b, wang a. Oncotarget. 2017 Mar 14;8(11):18359-18372. doi: 10.18632/oncotarget.15443. Oncotarget. 2017. PMID: 28407693 Free PMC article.
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: wang w, wang l, wang b, wang a. 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 a highly selective KIT kinase primary V559D mutant inhibitor for gastrointestinal stromal tumors (GISTs).
Yu K, Liu X, Jiang Z, Hu C, Zou F, Chen C, Ge J, Wu J, Liu X, Wang A, Wang W, Wang W, Qi Z, Wang B, Wang L, Yan H, Wang J, Ren T, Tang J, Liu Q, Liu J. Yu K, et al. Among authors: wang w, wang l, wang j, wang b, wang a. Oncotarget. 2017 Nov 15;8(67):111110-111118. doi: 10.18632/oncotarget.22624. eCollection 2017 Dec 19. Oncotarget. 2017. PMID: 29340041 Free PMC article.
Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding.
Wang Q, Liu F, Wang B, Zou F, Qi Z, Chen C, Yu K, Hu C, Qi S, Wang W, Hu Z, Liu J, Wang W, Wang L, Liang Q, Zhang S, Ren T, Liu Q, Liu J. Wang Q, et al. Among authors: wang w, wang l, wang b. J Med Chem. 2017 Jan 12;60(1):273-289. doi: 10.1021/acs.jmedchem.6b01290. Epub 2016 Dec 14. J Med Chem. 2017. PMID: 27966954
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: wang w, wang l, wang b, wang a. 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: wang w, wang l, wang j, wang b, wang a. Sci Rep. 2017 Mar 28;7(1):466. doi: 10.1038/s41598-017-00482-4. Sci Rep. 2017. PMID: 28352114 Free PMC article.
Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutants in FLT3-ITD Positive AML.
Wang A, Li X, Chen C, Wu H, Qi Z, Hu C, Yu K, Wu J, Liu J, Liu X, Hu Z, Wang W, Wang W, Wang W, Wang L, Wang B, Liu Q, Li L, Ge J, Ren T, Zhang S, Xia R, Liu J, Liu Q. Wang A, et al. Among authors: wang w, wang l, wang b. J Med Chem. 2017 Oct 26;60(20):8407-8424. doi: 10.1021/acs.jmedchem.7b00840. Epub 2017 Oct 17. J Med Chem. 2017. PMID: 28956923
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