A three-step protocol for lead optimization: Quick identification of key conformational features and functional groups in the SAR studies of non-ATP competitive MK2 (MAPKAPK2) inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 1, 2012, Pages 65-70

  Huang, Xianhai ^a   Zhu, Xiaohong ^a   Chen, Xiao ^a   Zhou, Wei ^a   Xiao, Dong ^a   Degrado, Sylvia ^a   Aslanian, Robert ^a   Fossetta, James ^a   Lundell, Daniel ^a   Tian, Fang ^a   Trivedi, Prashant ^a   Palani, Anandan ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Conformation; Inhibitor; MK2; Non ATP competitive; SAR; Three step protocol; TNF

Indexed keywords

ADENOSINE TRIPHOSPHATE; MITOGEN ACTIVATED PROTEIN KINASE P38 INHIBITOR;

ARTICLE; BINDING AFFINITY; BINDING COMPETITION; CELL ACTIVITY; CONTROLLED STUDY; DRUG CONFORMATION; DRUG IDENTIFICATION; DRUG TARGETING; IC 50; NONHUMAN; STRUCTURE ACTIVITY RELATION;

ADENOSINE TRIPHOSPHATE; ANIMALS; CHEMISTRY, PHARMACEUTICAL; DRUG DESIGN; HUMANS; INHIBITORY CONCENTRATION 50; INTRACELLULAR SIGNALING PEPTIDES AND PROTEINS; MICE; MODELS, CHEMICAL; MOLECULAR CONFORMATION; PROTEIN BINDING; PROTEIN KINASE INHIBITORS; PROTEIN-SERINE-THREONINE KINASES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84655163968     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.11.074     Document Type: Article

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