Discovery of novel allosteric mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors possessing bidentate Ser212 interactions

Journal of Medicinal Chemistry

Volumn 55, Issue 10, 2012, Pages 4594-4604

  Heald, Robert A ^a   Jackson, Philip ^a   Savy, Pascal ^a   Jones, Mark ^a   Gancia, Emanuela ^a   Burton, Brenda ^a   Newman, Richard ^a   Boggs, Jason ^b   Chan, Emily ^b   Chan, Jocelyn ^b   Choo, Edna ^b   Merchant, Mark ^b   Rudewicz, Patrick ^b   Ultsch, Mark ^b   Wiesmann, Christian ^b   Yue, Qin ^b   Belvin, Marcia ^b   Price, Steve ^a  

^a Argenta Discovery Ltd   (United Kingdom)

^b GENENTECH INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 (2 FLUORO 4 IODOPHENYLAMINO) 1H INDAZOLE 5 CARBOXYLIC ACID (2 HYDROXYETHOXY)AMIDE; 7 (2 FLUORO 4 IODOPHENYLAMINO)BENZO[D]ISOTHIAZOLE 6 CARBOXYLIC ACID (2 HYDROXYETHOXY)AMIDE; 7 (2 FLUORO 4 IODOPHENYLAMINO)BENZO[D]ISOTHIAZOLE 6 CARBOXYLIC ACID (2,3 DIHYDROXYPROPOXY)AMIDE; AMINE; ANTINEOPLASTIC AGENT; G 573; G 894; G 925; MITOGEN ACTIVATED PROTEIN KINASE INHIBITOR; MITOGEN ACTIVATED PROTEIN KINASE KINASE 1; SERINE; UNCLASSIFIED DRUG;

ALLOSTERISM; ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; CELL PROLIFERATION; COLORECTAL CANCER; CONTROLLED STUDY; CRYSTAL STRUCTURE; DISTRIBUTION VOLUME; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG EFFICACY; DRUG HALF LIFE; DRUG METABOLISM; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; HUMAN CELL; HYDROGEN BOND; IN VIVO STUDY; MOUSE; NONHUMAN; PHARMACOPHORE; PLASMA PROTEIN BINDING; PROTEIN PURIFICATION; RAT; STEADY STATE; TUMOR XENOGRAFT; X RAY;

ALLOSTERIC REGULATION; ANIMALS; ANTINEOPLASTIC AGENTS; BENZOFURANS; BENZOTHIAZOLES; CELL LINE, TUMOR; CELL PROLIFERATION; CRYSTALLOGRAPHY, X-RAY; DRUG SCREENING ASSAYS, ANTITUMOR; FEMALE; HYDROGEN BONDING; INDAZOLES; MAP KINASE KINASE 1; MAP KINASE KINASE 2; MICE; MODELS, MOLECULAR; MOLECULAR STRUCTURE; NEOPLASM TRANSPLANTATION; RATS; SERINE; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSPLANTATION, HETEROLOGOUS;

EID: 84861494447     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm2017094     Document Type: Article

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