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32 results

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Page 1
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: baer br. 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 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: baer br. 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.
The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients.
Hallin J, Engstrom LD, Hargis L, Calinisan A, Aranda R, Briere DM, Sudhakar N, Bowcut V, Baer BR, Ballard JA, Burkard MR, Fell JB, Fischer JP, Vigers GP, Xue Y, Gatto S, Fernandez-Banet J, Pavlicek A, Velastagui K, Chao RC, Barton J, Pierobon M, Baldelli E, Patricoin EF 3rd, Cassidy DP, Marx MA, Rybkin II, Johnson ML, Ou SI, Lito P, Papadopoulos KP, Jänne PA, Olson P, Christensen JG. Hallin J, et al. Among authors: baer br. Cancer Discov. 2020 Jan;10(1):54-71. doi: 10.1158/2159-8290.CD-19-1167. Epub 2019 Oct 28. Cancer Discov. 2020. PMID: 31658955 Free PMC article.
Discovery of 2-pyridylureas as glucokinase activators.
Hinklin RJ, Aicher TD, Anderson DA, Baer BR, Boyd SA, Condroski KR, DeWolf WE Jr, Kraser CF, McVean M, Rhodes SP, Sturgis HL, Voegtli WC, Williams L, Houze JB. Hinklin RJ, et al. Among authors: baer br. J Med Chem. 2014 Oct 9;57(19):8180-6. doi: 10.1021/jm501204z. Epub 2014 Sep 17. J Med Chem. 2014. PMID: 25203462
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. Among authors: baer br. 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
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: baer br. 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.
Characterization of a novel glucokinase activator in rat and mouse models.
Lu M, Li P, Bandyopadhyay G, Lagakos W, Dewolf WE Jr, Alford T, Chicarelli MJ, Williams L, Anderson DA, Baer BR, McVean M, Conn M, Véniant MM, Coward P. Lu M, et al. Among authors: baer br. PLoS One. 2014 Feb 12;9(2):e88431. doi: 10.1371/journal.pone.0088431. eCollection 2014. PLoS One. 2014. PMID: 24533087 Free PMC article.
32 results