Rapid Determination of the Specificity Constant of Irreversible Inhibitors (kinact/KI) by Means of an Endpoint Competition Assay

Angewandte Chemie - International Edition

Volumn 54, Issue 47, 2015, Pages 14099-14102

  Miyahisa, Ikuo ^a   Sameshima, Tomoya ^a   Hixon, Mark S ^b  

^a TAKEDA PHARMACEUTICAL COMPANY LIMITED   (Japan)

^b Takeda San Diego Inc   (United States)

Author keywords

covalent inhibitors; drug discovery; enzyme kinetics; irreversible inhibition

Indexed keywords

ASSAYS; ENZYME INHIBITION; ENZYME KINETICS;

COMPETITION ASSAYS; COMPETITIVE ASSAYS; DRUG DISCOVERY; HIGH THROUGHPUT; IRREVERSIBLE INHIBITIONS; KINETIC EVALUATIONS; LONG DURATION; SIMPLE APPROACH;

PROBES;

CANERTINIB; ENZYME INHIBITOR; EPIDERMAL GROWTH FACTOR RECEPTOR; MORPHOLINE DERIVATIVE;

ANTAGONISTS AND INHIBITORS; BIOASSAY; CHEMICAL STRUCTURE; CHEMISTRY; HUMAN; KINETICS; METABOLISM; STRUCTURE ACTIVITY RELATION; TIME FACTOR;

ENDPOINT DETERMINATION; ENZYME INHIBITORS; HUMANS; KINETICS; MOLECULAR STRUCTURE; MORPHOLINES; RECEPTOR, EPIDERMAL GROWTH FACTOR; STRUCTURE-ACTIVITY RELATIONSHIP; TIME FACTORS;

EID: 84954408628     PISSN: 14337851     EISSN: 15213773     Source Type: Journal    
DOI: 10.1002/anie.201505800     Document Type: Article

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