Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR

Journal of Medicinal Chemistry

Volumn 60, Issue 7, 2017, Pages 3002-3019

  Planken, Simon ^a   Behenna, Douglas C ^a   Nair, Sajiv K ^a   Johnson, Theodore O ^a   Nagata, Asako ^a   Almaden, Chau ^a   Bailey, Simon ^a   Ballard, T Eric ^a   Bernier, Louise ^a   Cheng, Hengmiao ^a   Cho Schultz, Sujin ^a   Dalvie, Deepak ^a   Deal, Judith G ^a   Dinh, Dac M ^a   Edwards, Martin P ^a   Ferre, Rose Ann ^a   Gajiwala, Ketan S ^a   Hemkens, Michelle ^a   Kania, Robert S ^a   Kath, John C ^a   Matthews, Jean ^a   Murray, Brion W ^a   Niessen, Sherry ^a   Orr, Suvi T M ^a   Pairish, Mason ^a   Sach, Neal W ^a   Shen, Hong ^a   Shi, Manli ^a   Solowiej, James ^a   Tran, Khanh ^a   Tseng, Elaine ^a   Vicini, Paolo ^a   Wang, Yuli ^a   Weinrich, Scott L ^a   Zhou, Ru ^a   Zientek, Michael ^b   Liu, Longqing ^b   Luo, Yiqin ^b   Xin, Shuibo ^b   Zhang, Chengyi ^b   Lafontaine, Jennifer ^a   more..

^a PFIZER INC   (United States)

^b WUXI APPTEC   (China)

Author keywords

[No Author keywords available]

Indexed keywords

EPIDERMAL GROWTH FACTOR RECEPTOR; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; ERLOTINIB; FLUORINE; MUTANT PROTEIN; OSIMERTINIB; PF 06747775; UNCLASSIFIED DRUG; ACRYLAMIDE DERIVATIVE; EGFR PROTEIN, HUMAN; PROTEIN KINASE INHIBITOR; PYRROLIDINE DERIVATIVE;

ANIMAL EXPERIMENT; ARTICLE; COMPUTER MODEL; CONTROLLED STUDY; DOG; DRUG DESIGN; DRUG SELECTIVITY; DRUG TARGETING; ENZYME INHIBITION; FEMALE; HUMAN; HUMAN CELL; HYDROGEN BOND; IC50; IN VITRO STUDY; IN VIVO STUDY; MALE; MOUSE; MUTATION; NONHUMAN; PLASMA CLEARANCE; PLASMA HALF LIFE; RAT; SINGLE DRUG DOSE; ANIMAL; ANTAGONISTS AND INHIBITORS; CARCINOMA, NON-SMALL-CELL LUNG; CHEMISTRY; DRUG EFFECTS; GENETICS; HALOGENATION; LUNG; LUNG NEOPLASMS; METABOLISM; MOLECULAR DOCKING; MOLECULAR MODEL; TUMOR CELL LINE;

ACRYLAMIDES; ANIMALS; CARCINOMA, NON-SMALL-CELL LUNG; CELL LINE, TUMOR; DOGS; DRUG DESIGN; HALOGENATION; HUMANS; LUNG; LUNG NEOPLASMS; MICE; MODELS, MOLECULAR; MOLECULAR DOCKING SIMULATION; MUTATION; PROTEIN KINASE INHIBITORS; PYRROLIDINES; RATS; RECEPTOR, EPIDERMAL GROWTH FACTOR;

EID: 85017666129     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.6b01894     Document Type: Article

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