Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRAS G12C Inhibitor | Zendy

Joachim Bröker | Zendy; Alex G. Waterson | Zendy; Chris A. Smethurst | Zendy; Dirk Kessler | Zendy; Jark Böttcher | Zendy; Moriz Mayer | Zendy; Gerhard Gmaschitz | Zendy; Jason Phan | Zendy; Andrew J. Little | Zendy; Jason R. Abbott | Zendy; Qi Sun | Zendy; Michael Gmachl | Zendy; Dorothea Rudolph | Zendy; Heribert Arnhof | Zendy; Klaus Rumpel | Zendy; Fabio Savarese | Zendy; Thomas Gerstberger | Zendy; Nikolai Mischerikow | Zendy; Matthias Treu | Zendy; Lorenz Herdeis | Zendy; Tobias Wunberg | Zendy; Andreas Gollner | Zendy; Harald Weinstabl | Zendy; Andreas Mantoulidis | Zendy; Oliver Krämer | Zendy; Darryl B. McConnell | Zendy; Stephen W. Fesik | Zendy

Open Access

Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRAS ^G12C Inhibitor

Author(s) -

Joachim Bröker,

Alex G. Waterson,

Chris A. Smethurst,

Dirk Kessler,

Jark Böttcher,

Moriz Mayer,

Gerhard Gmaschitz,

Jason Phan,

Andrew J. Little,

Jason R. Abbott,

Qi Sun,

Michael Gmachl,

Dorothea Rudolph,

Heribert Arnhof,

Klaus Rumpel,

Fabio Savarese,

Thomas Gerstberger,

Nikolai Mischerikow,

Matthias Treu,

Lorenz Herdeis,

Tobias Wunberg,

Andreas Gollner,

Harald Weinstabl,

Andreas Mantoulidis,

Oliver Krämer,

Darryl B. McConnell,

Stephen W. Fesik

Publication year - 2022

Publication title -

journal of medicinal chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.01

H-Index - 261

eISSN - 1520-4804

pISSN - 0022-2623

DOI - 10.1021/acs.jmedchem.2c01120

Subject(s) - kras , chemistry , in vivo , small molecule , covalent bond , cysteine , binding site , point mutation , mutant , biochemistry , mutation , enzyme , genetics , biology , gene , organic chemistry

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