Discovery of selective 4-amino-pyridopyrimidine inhibitors of MAP4K4 using fragment-based lead identification and optimization

Journal of Medicinal Chemistry

Volumn 57, Issue 8, 2014, Pages 3484-3493

  Crawford, Terry D ^a   Ndubaku, Chudi O ^a   Chen, Huifen ^a   Boggs, Jason W ^a   Bravo, Brandon J ^a   Delatorre, Kelly ^a   Giannetti, Anthony M ^a   Gould, Stephen E ^a   Harris, Seth F ^a   Magnuson, Steven R ^a   McNamara, Erin ^a   Murray, Lesley J ^a   Nonomiya, Jim ^a   Sambrone, Amy ^a   Schmidt, Stephen ^a   Smyczek, Tanya ^a   Stanley, Mark ^a   Vitorino, Philip ^a   Wang, Lan ^a   West, Kristina ^a   Wu, Ping ^a   Ye, Weilan ^a   more..

^a GENENTECH INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4,6 DICHLOROPYRIDO[3,2 D]PYRIMIDINE; 6 (2 FLUOROPYRIDIN 4 YL )PYRIDO[3,2 D]PYRIMIDIN 4 AMINE; 6 (2 FLUOROPYRIDIN 4 YL)PYRIDO[3,2 D]PYRIMIDIN 4 AMINE; 6 CHLOROPYRIDO[3,2 D]PYRIMIDIN 4 AMINE; 6 CHLOROPYRIDO[3,2 D]PYRIMIDIN 4(3H) ONE; ANTINEOPLASTIC AGENT; MITOGEN ACTIVATED PROTEIN KINASE INHIBITOR; MITOGEN ACTIVATED PROTEIN KINASE KINASE KINASE; MITOGEN ACTIVATED PROTEIN KINASE KINASE KINASE KINASE 4; MITOGEN ACTIVATED PROTEIN KINASE KINASE KINASE KINASE 4 INHIBITOR; PYRIMIDINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; BINDING SITE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DOSE RESPONSE; DRUG CLEARANCE; DRUG EXPOSURE; DRUG POTENCY; ENZYME INHIBITION; FEMALE; HYDROGEN BOND; IN VIVO STUDY; LIPOPHILICITY; MOUSE; NONHUMAN; STRUCTURE ACTIVITY RELATION; SURFACE PLASMON RESONANCE; TUMOR XENOGRAFT;

ANIMALS; DRUG DISCOVERY; FEMALE; INTRACELLULAR SIGNALING PEPTIDES AND PROTEINS; MICE; MODELS, MOLECULAR; PROTEIN KINASE INHIBITORS; PROTEIN-SERINE-THREONINE KINASES; PYRIMIDINES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84899541945     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm500155b     Document Type: Article

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