Novel ATP competitive MK2 inhibitors with potent biochemical and cell-based activity throughout the series

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 1, 2012, Pages 613-618

  Oubrie, Arthur ^a   Kaptein, Allard ^a   De Zwart, Edwin ^a   Hoogenboom, Niels ^a   Goorden, Rianne ^a   Van De Kar, Bas ^a   Van Hoek, Maaike ^a   De Kimpe, Vera ^a   Van Der Heijden, Ruud ^a   Borsboom, Judith ^a   Kazemier, Bert ^a   De Roos, Jeroen ^a   Scheffers, Michiel ^a   Lommerse, Jos ^a   Schultz Fademrecht, Carsten ^a   Barf, Tjeerd ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Anti TNF ; HSP27; MAPKAPK2; MK2; Rheumatoid arthritis

Indexed keywords

ADENOSINE TRIPHOSPHATE; CYTOKINE; HEAT SHOCK PROTEIN 27; LIPOPOLYSACCHARIDE; MITOGEN ACTIVATED PROTEIN KINASE 1; MITOGEN ACTIVATED PROTEIN KINASE 1 INHIBITOR; MITOGEN ACTIVATED PROTEIN KINASE INHIBITOR; TUMOR NECROSIS FACTOR ALPHA; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CELL ASSAY; CHEMICAL ANALYSIS; COMPUTATIONAL FLUID DYNAMICS; CONTROLLED STUDY; CYTOKINE PRODUCTION; DRUG BINDING; DRUG BIOAVAILABILITY; DRUG INHIBITION; DRUG PENETRATION; DRUG POTENCY; DRUG SELECTIVITY; GROWTH INHIBITION; NONHUMAN; PERIPHERAL BLOOD MONONUCLEAR CELL; PHARMACODYNAMICS; PROTEIN PHOSPHORYLATION; RAT; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

BENZAMIDES; CHEMISTRY, PHARMACEUTICAL; COMPUTER SIMULATION; CRYSTALLOGRAPHY, X-RAY; CYTOKINES; DRUG DESIGN; HSP27 HEAT-SHOCK PROTEINS; HUMANS; INTRACELLULAR SIGNALING PEPTIDES AND PROTEINS; MODELS, CHEMICAL; PHOSPHORYLATION; PIPERIDONES; PROTEIN KINASE INHIBITORS; PROTEIN-SERINE-THREONINE KINASES; PYRROLES; TUMOR NECROSIS FACTOR-ALPHA;

EID: 84655164865     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.10.071     Document Type: Article

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