Drug discovery considerations in the development of covalent inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 24, Issue 1, 2014, Pages 33-39

  Mah, Robert ^a   Thomas, Jason R ^b   Shafer, Cynthia M ^b  

^a NOVARTIS PHARMA AG   (Switzerland)

^b NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

Author keywords

Activity based protein profiling (ABPP); Click chemistry; Covalent inhibitor; kinact Ki; Mechanism based inhibitor; Targeted covalent inhibitor (TCI); Warhead reactivity

Indexed keywords

COVALENT INHIBITOR; MISCELLANEOUS DRUGS AND AGENTS; UNCLASSIFIED DRUG;

ARTICLE; CLICK CHEMISTRY; COVALENT BOND; CROSS REACTION; DRUG SYNTHESIS; ELECTROPHILICITY; FOOD AND DRUG ADMINISTRATION; HUMAN; NUCLEOPHILICITY; PEPTIDE MAPPING; PROTEIN DATABASE; SEQUENCE ALIGNMENT; SITE DIRECTED MUTAGENESIS; SUICIDE SUBSTRATE; TANDEM MASS SPECTROMETRY;

ACTIVITY-BASED PROTEIN PROFILING (ABPP); CLICK CHEMISTRY; COVALENT INHIBITOR; K(INACT)/K(I); MECHANISM-BASED INHIBITOR; TARGETED COVALENT INHIBITOR (TCI); WARHEAD REACTIVITY;

ANIMALS; DRUG DISCOVERY; ENZYME INHIBITORS; ENZYMES; HUMANS; MOLECULAR STRUCTURE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84891496533     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.10.003     Document Type: Review

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