Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer.

doi:10.1021/acs.jmedchem.9b02052

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Article

Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer.

Journal of medicinal chemistry - 9 Jul 2020

Fell Jay B, Fischer John P, Baer Brian R, Blake James F, Bouhana Karyn, Briere David M, Brown Karin D, Burgess Laurence E, Burns Aaron C, Burkard Michael R, Chiang Harrah, Chicarelli Mark J, Cook Adam W, Gaudino John J, Hallin Jill, Hanson Lauren, Hartley Dylan P, Hicken Erik J, Hingorani Gary P, Hinklin Ronald J, Mejia Macedonio J, Olson Peter, Otten Jennifer N, Rhodes Susan P, Rodriguez Martha E, Savechenkov Pavel, Smith Darin J, Sudhakar Niranjan, Sullivan Francis X, Tang Tony P, Vigers Guy P, Wollenberg Lance, Christensen James G, Marx Matthew A

Abstract excerpt

Capping off an era marred by drug development failures and punctuated by waning interest and presumed intractability toward direct targeting of KRAS, new technologies and strategies are aiding in the target's resurgence. As previously reported, the tetrahydropyridopyrimidines were identified as irreversible covalent inhibitors of KRASG12C that bind in the switch-II pocket of KRAS and make a covalent bond to...

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PMID: 32250617
DOI: 10.1021/acs.jmedchem.9b02052

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

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