Initial optimization and series evolution of diaminopyrimidine inhibitors of interleukin-1 receptor associated kinase 4

Bioorganic and Medicinal Chemistry Letters

Volumn 25, Issue 16, 2015, Pages 3203-3207

  Seganish, W Michael ^a   McElroy, William T ^a   Herr, R Jason ^b   Brumfield, Stephanie ^a   Greenlee, William J ^a   Harding, James ^b   Komanduri, Venukrishnan ^c   Matasi, Julius ^a   Prakash, Koraboina Chandra ^c   Tulshian, Deen ^a   Yang, Jinhai ^b   Yet, Larry ^b   Devito, Kristine ^a   Fossetta, James ^a   Garlisi, Charles G ^a   Lundell, Daniel ^a   Niu, Xiaoda ^a   Sondey, Christopher ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

^b ALBANY MOLECULAR RESEARCH INC   (United States)

^c AMRI Singapore Research Centre   (Singapore)

Author keywords

Aminopyrimidine; Inflammation; IRAK4; Kinase; Structure activity relationships

Indexed keywords

LIPOPOLYSACCHARIDE; PROTEIN SERINE THREONINE KINASE INHIBITOR; PYRIMIDINE; TOLL LIKE RECEPTOR AGONIST; ENZYME INHIBITOR; INTERLEUKIN 1 RECEPTOR ASSOCIATED KINASE; IRAK4 PROTEIN, HUMAN; NONSTEROID ANTIINFLAMMATORY AGENT; PYRIMIDINE DERIVATIVE; TOLL LIKE RECEPTOR 4;

ARTICLE; DRUG POTENCY; DRUG SELECTIVITY; DRUG SOLUBILITY; IC50; PROCESS OPTIMIZATION; STRUCTURE ACTIVITY RELATION; ANTAGONISTS AND INHIBITORS; CELL LINE; ENZYME SPECIFICITY; HIGH THROUGHPUT SCREENING; HUMAN; SYNTHESIS;

ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; CELL LINE; ENZYME INHIBITORS; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASES; LIPOPOLYSACCHARIDES; PYRIMIDINES; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY; TOLL-LIKE RECEPTOR 4;

EID: 84934852909     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2015.05.097     Document Type: Article

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