Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor.

doi:10.1021/acs.jmedchem.6b00995

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Article

Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor.

Journal of medicinal chemistry - 13 Oct 2016

Chan Bryan K, Hanan Emily J, Bowman Krista K, Bryan Marian C, Burdick Daniel, Chan Emily, Chen Yuan, Clausen Saundra, Dela Vega Trisha, Dotson Jennafer, Eigenbrot Charles, Elliott Richard L, Heald Robert A, Jackson Philip S, Knight Jamie D, La Hank, Lainchbury Michael D, Malek Shiva, Purkey Hans E, Schaefer Gabriele, Schmidt Stephen, Seward Eileen M, Sideris Steve, Shao Lily, Wang Shumei, Yeap Siew Kuen, Yen Ivana, Yu Christine, Heffron Timothy P

Abstract excerpt

Inhibitors targeting the activating mutants of the epidermal growth factor receptor (EGFR) have found success in the treatment of EGFR mutant positive non-small-cell lung cancer. A secondary point mutation (T790M) in the inhibitor binding site has been linked to the acquired resistance against those first generation therapeutics. Herein, we describe the lead optimization of a series of reversible, pan-mutant...

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PMID: 27564586
DOI: 10.1021/acs.jmedchem.6b00995

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EGFR

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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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