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Structural Basis for EGFR Mutant Inhibition by Trisubstituted Imidazole Inhibitors

Journal Article · · Journal of Medicinal Chemistry
; ; ; ;
Research Organization:
Brookhaven National Laboratory (BNL), Upton, NY (United States)
Sponsoring Organization:
~OTHER
DOE Contract Number:
SC0012704
OSTI ID:
1690160
Report Number(s):
BNL-220482-2020-JACI
Journal Information:
Journal of Medicinal Chemistry, Journal Name: Journal of Medicinal Chemistry Journal Issue: 8 Vol. 63; ISSN 0022-2623
Country of Publication:
United States
Language:
English

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Structural basis for p38α MAP kinase quinazolinone and pyridol-pyrimidine inhibitor specificity
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Discovery of a Highly Potent and Broadly Effective Epidermal Growth Factor Receptor and HER2 Exon 20 Insertion Mutant Inhibitor journal September 2018
Discovery of novel 9-heterocyclyl substituted 9H-purines as L858R/T790M/C797S mutant EGFR tyrosine kinase inhibitors journal January 2020
Brigatinib combined with anti-EGFR antibody overcomes osimertinib resistance in EGFR-mutated non-small-cell lung cancer journal March 2017
Trisubstituted Imidazoles with a Rigidized Hinge Binding Motif Act As Single Digit nM Inhibitors of Clinically Relevant EGFR L858R/T790M and L858R/T790M/C797S Mutants: An Example of Target Hopping journal May 2017
Acquired EGFR C797S mutation mediates resistance to AZD9291 in non–small cell lung cancer harboring EGFR T790M journal May 2015
Structure-Based Design of 5-Methylpyrimidopyridone Derivatives as New Wild-Type Sparing Inhibitors of the Epidermal Growth Factor Receptor Triple Mutant (EGFR L858R/T790M/C797S ) journal July 2019
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Discovery of Potent and Noncovalent Reversible EGFR Kinase Inhibitors of EGFR L858R/T790M/C797S journal May 2019
Discovery of a potent dual ALK and EGFR T790M inhibitor journal August 2017

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99 GENERAL AND MISCELLANEOUS