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Page 1
Discovery of Pyrazolopyrazines as Selective, Potent, and Mutant-Active MET Inhibitors with Intracranial Efficacy.
Bumpers QA, Pipal RW, Benz-Weeden AM, Brewster JT 2nd, Cook A, Crooks AL, Cruz C, Dwulet NC, Gaudino JJ, Golec D, Harrison JA, Hartley DP, Hassanien SH, Hicken EJ, Kahn D, Laird ER, Lemieux C, Lewandowski N, McCown J, McDonald MG, McNulty O, Mou TC, Nguyen P, Oko L, Opie LP, Otten J, Peck SC, Polites VC, Randall SD, Rosen RZ, Savechenkov P, Simpson H, Singh A, Sparks D, Wickersham K, Wollenberg L, Wong CE, Wong J, Wu WI, Elsayed MSA, Hinklin RJ, Tang TP. Bumpers QA, et al. Among authors: hinklin rj. J Med Chem. 2024 Aug 22;67(16):14466-14477. doi: 10.1021/acs.jmedchem.4c01232. Epub 2024 Aug 1. J Med Chem. 2024. PMID: 39088797
Discovery of 5-Azaquinoxaline Derivatives as Potent and Orally Bioavailable Allosteric SHP2 Inhibitors.
Elsayed MSA, Blake JF, Boys ML, Brown E, Chapsal BD, Chicarelli MJ, Cook AW, Fell JB, Fischer JP, Hanson L, Lemieux C, Martinson MC, McCown J, McNulty OT, Mejia MJ, Neitzel NA, Otten JN, Rodriguez ME, Wilcox D, Wong CE, Zhou Y, Hinklin RJ. Elsayed MSA, et al. Among authors: hinklin rj. ACS Med Chem Lett. 2023 Nov 15;14(12):1673-1681. doi: 10.1021/acsmedchemlett.3c00310. eCollection 2023 Dec 14. ACS Med Chem Lett. 2023. PMID: 38116446
SHP2 Inhibition Sensitizes Diverse Oncogene-Addicted Solid Tumors to Re-treatment with Targeted Therapy.
Drilon A, Sharma MR, Johnson ML, Yap TA, Gadgeel S, Nepert D, Feng G, Reddy MB, Harney AS, Elsayed M, Cook AW, Wong CE, Hinklin RJ, Jiang Y, Brown EN, Neitzel NA, Laird ER, Wu WI, Singh A, Wei P, Ching KA, Gaudino JJ, Lee PA, Hartley DP, Rothenberg SM. Drilon A, et al. Among authors: hinklin rj. Cancer Discov. 2023 Aug 4;13(8):1789-1801. doi: 10.1158/2159-8290.CD-23-0361. Cancer Discov. 2023. PMID: 37269335 Free PMC article.
Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer.
Fell JB, Fischer JP, Baer BR, Blake JF, Bouhana K, Briere DM, Brown KD, Burgess LE, Burns AC, Burkard MR, Chiang H, Chicarelli MJ, Cook AW, Gaudino JJ, Hallin J, Hanson L, Hartley DP, Hicken EJ, Hingorani GP, Hinklin RJ, Mejia MJ, Olson P, Otten JN, Rhodes SP, Rodriguez ME, Savechenkov P, Smith DJ, Sudhakar N, Sullivan FX, Tang TP, Vigers GP, Wollenberg L, Christensen JG, Marx MA. Fell JB, et al. Among authors: hinklin rj. J Med Chem. 2020 Jul 9;63(13):6679-6693. doi: 10.1021/acs.jmedchem.9b02052. Epub 2020 Apr 6. J Med Chem. 2020. PMID: 32250617 Free article.
Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator.
Hinklin RJ, Baer BR, Boyd SA, Chicarelli MD, Condroski KR, DeWolf WE Jr, Fischer J, Frank M, Hingorani GP, Lee PA, Neitzel NA, Pratt SA, Singh A, Sullivan FX, Turner T, Voegtli WC, Wallace EM, Williams L, Aicher TD. Hinklin RJ, et al. Bioorg Med Chem. 2020 Jan 1;28(1):115232. doi: 10.1016/j.bmc.2019.115232. Epub 2019 Dec 2. Bioorg Med Chem. 2020. PMID: 31818630
Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity.
Fell JB, Fischer JP, Baer BR, Ballard J, Blake JF, Bouhana K, Brandhuber BJ, Briere DM, Burgess LE, Burkard MR, Chiang H, Chicarelli MJ, Davidson K, Gaudino JJ, Hallin J, Hanson L, Hee K, Hicken EJ, Hinklin RJ, Marx MA, Mejia MJ, Olson P, Savechenkov P, Sudhakar N, Tang TP, Vigers GP, Zecca H, Christensen JG. Fell JB, et al. Among authors: hinklin rj. ACS Med Chem Lett. 2018 Nov 7;9(12):1230-1234. doi: 10.1021/acsmedchemlett.8b00382. eCollection 2018 Dec 13. ACS Med Chem Lett. 2018. PMID: 30613331 Free PMC article.
Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394.
Dransfield PJ, Pattaropong V, Lai S, Fu Z, Kohn TJ, Du X, Cheng A, Xiong Y, Komorowski R, Jin L, Conn M, Tien E, DeWolf WE Jr, Hinklin RJ, Aicher TD, Kraser CF, Boyd SA, Voegtli WC, Condroski KR, Veniant-Ellison M, Medina JC, Houze J, Coward P. Dransfield PJ, et al. Among authors: hinklin rj. ACS Med Chem Lett. 2016 May 23;7(7):714-8. doi: 10.1021/acsmedchemlett.6b00140. eCollection 2016 Jul 14. ACS Med Chem Lett. 2016. PMID: 27437083 Free PMC article.
5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties.
Kohn TJ, Du X, Lai S, Xiong Y, Komorowski R, Veniant M, Fu Z, Jiao X, Pattaropong V, Chow D, Cardozo M, Jin L, Conn M, DeWolf WE Jr, Kraser CF, Hinklin RJ, Boys ML, Medina JC, Houze J, Dransfield P, Coward P. Kohn TJ, et al. Among authors: hinklin rj. ACS Med Chem Lett. 2016 Jun 1;7(7):666-70. doi: 10.1021/acsmedchemlett.6b00145. eCollection 2016 Jul 14. ACS Med Chem Lett. 2016. PMID: 27437074 Free PMC article.
C5-Alkyl-2-methylurea-Substituted Pyridines as a New Class of Glucokinase Activators.
Du X, Hinklin RJ, Xiong Y, Dransfield P, Park J, Kohn TJ, Pattaropong V, Lai S, Fu Z, Jiao X, Chow D, Jin L, Davda J, Veniant MM, Anderson DA, Baer BR, Bencsik JR, Boyd SA, Chicarelli MJ, Mohr PJ, Wang B, Condroski KR, DeWolf WE, Conn M, Tran T, Yang J, Aicher TD, Medina JC, Coward P, Houze JB. Du X, et al. Among authors: hinklin rj. ACS Med Chem Lett. 2014 Nov 22;5(12):1284-9. doi: 10.1021/ml500341w. eCollection 2014 Dec 11. ACS Med Chem Lett. 2014. PMID: 25516785 Free PMC article.
15 results