Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor.

doi:10.1021/acs.jmedchem.1c01688

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Article

Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor.

Journal of medicinal chemistry - 24 Feb 2022

Wang Xiaolun, Allen Shelley, Blake James F, Bowcut Vickie, Briere David M, Calinisan Andrew, Dahlke Joshua R, Fell Jay B, Fischer John P, Gunn Robin J, Hallin Jill, Laguer Jade, Lawson J David, Medwid James, Newhouse Brad, Nguyen Phong, O'Leary Jacob M, Olson Peter, Pajk Spencer, Rahbaek Lisa, Rodriguez Mareli, Smith Christopher R, Tang Tony P, Thomas Nicole C, Vanderpool Darin, Vigers Guy P, Christensen James G, Marx Matthew A

Abstract excerpt

KRASG12D, the most common oncogenic KRAS mutation, is a promising target for the treatment of solid tumors. However, when compared to KRASG12C, selective inhibition of KRASG12D presents a significant challenge due to the requirement of inhibitors to bind KRASG12D with high enough affinity to obviate the need for covalent interactions with the mutant KRAS protein. Here, we report the discovery and characterization...

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PMID: 34889605
DOI: 10.1021/acs.jmedchem.1c01688

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

Source receipt: pubmed, retrieved 7 Sept 2026.

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