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Title: Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vi

Journal Article · · J. Med. Chem.

Research Organization:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Organization:
DOE - Office Of Science; National Institutes of Health (NIH)
Journal Information:
J. Med. Chem., Vol. 65, Issue (21)
Country of Publication:
United States

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Small-molecule ligands bind to a distinct pocket in Ras and inhibit SOS-mediated nucleotide exchange activity journal March 2012
Discovery of Small Molecules that Bind to K-Ras and Inhibit Sos-Mediated Activation journal May 2012
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K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions journal November 2013
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Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor journal December 2021
Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity journal January 2019
Abstract 1271: In vitro and in vivo characterization of BI 1823911 - a novel KRASG12C selective small molecule inhibitor journal July 2021