PAINS in the assay: Chemical mechanisms of assay interference and promiscuous enzymatic inhibition observed during a sulfhydryl-scavenging HTS

Journal of Medicinal Chemistry

Volumn 58, Issue 5, 2015, Pages 2091-2113

  Dahlin, Jayme L ^a,b   Nissink, J Willem M ^c   Strasser, Jessica M ^d   Francis, Subhashree ^d   Higgins, Leeann ^e   Zhou, Hui ^a   Zhang, Zhiguo ^a   Walters, Michael A ^d  

^a MAYO GRADUATE SCHOOL   (United States)

^b Mayo Clinic   (United States)

^c ASTRAZENECA   (United Kingdom)

^d UNIVERSITY OF MINNESOTA   (United States)

^e UNIVERSITY OF MINNESOTA   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CYSTEINE; ENZYME INHIBITOR; PAN ASSAY INTERFERENCE COMPOUND; PROTEIN; THIOL DERIVATIVE; UNCLASSIFIED DRUG; HISTONE ACETYLTRANSFERASE;

ARTICLE; CONTROLLED STUDY; COVALENT BOND; DRUG DETERMINATION; DRUG IDENTIFICATION; DRUG MECHANISM; ENZYME INHIBITION; FOLLOW UP; HIGH THROUGHPUT SCREENING; IC50; MOLECULAR LIBRARY; STRUCTURE ACTIVITY RELATION; ANTAGONISTS AND INHIBITORS; BIOASSAY; CHEMICAL STRUCTURE; CHEMISTRY; DRUG DESIGN; DRUG DEVELOPMENT; HUMAN; LABORATORY DIAGNOSIS; NUCLEAR MAGNETIC RESONANCE; PRECLINICAL STUDY; STANDARDS;

BIOLOGICAL ASSAY; DRUG DESIGN; DRUG DISCOVERY; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; FALSE POSITIVE REACTIONS; HIGH-THROUGHPUT SCREENING ASSAYS; HISTONE ACETYLTRANSFERASES; HUMANS; MOLECULAR STRUCTURE; NUCLEAR MAGNETIC RESONANCE, BIOMOLECULAR; SULFHYDRYL COMPOUNDS;

EID: 84924692170     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm5019093     Document Type: Article

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