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

Journal of Medicinal Chemistry

Volumn 59, Issue 19, 2016, Pages 9080-9093

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

^a GENENTECH INC   (United States)

^b CHARLES RIVER LABORATORIES   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

2 [1 [1 (SEC BUTYL) 6 [[2 [1 (CYCLOPROPYLSULFONYL) 1H PYRAZOL 4 YL]PYRIMIDIN 4 YL]AMINO] 1H PYRAZOLO[4,3 C]PYRIDIN 3 YL]AZETIDIN 3 YL]PROPAN 2 OL; 2 [1 [6 [[2 [1 (CYCLOPROPYLSULFONYL) 1H PYRAZOL 4 YL]PYRIMIDIN 4 YL]AMINO] 1 ISOPROPYL 1H PYRAZOLO[4,3 C]PYRIDIN 3 YL]AZETIDIN 3 YL]PROPAN 2 OL; 6 [[2 [1 (CYCLOPROPYLSULFONYL) 1H PYRAZOL 4 YL]PYRIMIDIN 4 YL]AMINO] 1 ISOPROPYL 1H PYRROLO[3,2 C]PYRIDIN 3 CARBOXAMIDE; AFATINIB; ANTINEOPLASTIC AGENT; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; ERLOTINIB; GEFITINIB; N [2 [1 (CYCLOPROPYLSULFONYL) 1H PYRAZOL 4 Y]PYRIMIDIN 4 YL] 1 ISOPROPYL 2 METHYL 1H IMIDAZO[4,5 C]PYRIDIN 6 AMINE; N [2 [1 (CYCLOPROPYLSULFONYL) 1H PYRAZOL 4 Y]PYRIMIDIN 4 YL] 1 ISOPROPYL 3 MORPHOLINO 1H PYRAZOLO[4,3 C]PYRIDIN 6 AMINE; OSIMERTINIB; UNCLASSIFIED DRUG; EPIDERMAL GROWTH FACTOR RECEPTOR; PROTEIN KINASE INHIBITOR;

ALKYLATION; ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DOG; DRUG BINDING; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG POTENCY; DRUG SELECTIVITY; DRUG SOLUBILITY; DRUG STABILITY; DRUG TARGETING; ENANTIOMER; HEPATIC CLEARANCE; HUMAN; HUMAN CELL; HYDROGEN BOND; HYDROGENATION; IC50; IODINATION; LIPOPHILICITY; LIVER CELL; LIVER MICROSOME; MOUSE; MUTANT; NONHUMAN; PLASMA CLEARANCE; SINGLE DRUG DOSE; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION; SUZUKI REACTION; ANIMAL; ANTAGONISTS AND INHIBITORS; CARCINOMA, NON-SMALL-CELL LUNG; CELL PROLIFERATION; CHEMISTRY; DRUG EFFECTS; DRUG RESISTANCE; GENETICS; LUNG; LUNG NEOPLASMS; METABOLISM; MOLECULAR MODEL; MUTATION; PATHOLOGY; TUMOR CELL LINE; X RAY CRYSTALLOGRAPHY;

ANIMALS; ANTINEOPLASTIC AGENTS; CARCINOMA, NON-SMALL-CELL LUNG; CELL LINE, TUMOR; CELL PROLIFERATION; CRYSTALLOGRAPHY, X-RAY; DRUG RESISTANCE, NEOPLASM; HUMANS; LUNG; LUNG NEOPLASMS; MICE; MODELS, MOLECULAR; MUTATION; PROTEIN KINASE INHIBITORS; RECEPTOR, EPIDERMAL GROWTH FACTOR;

EID: 84991376225     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.6b00995     Document Type: Article

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