A proposed screening paradigm for discovery of covalent inhibitor drugs

Drug Metabolism Letters

Volumn 8, Issue 1, 2014, Pages 19-30

  Moghaddam, Mehran F ^a   Tang, Yang ^a   O’Brien, Zhihong ^a   Richardson, Samantha J ^a   Bacolod, Maria ^b   Chaturvedi, Prasoon ^b   Apuy, Julius ^a   Kulkarni, Ashutosh ^a  

^a CELGENE CORPORATION   (United States)

^b Celgene Avilomics Research   (United States)

Author keywords

ADME; Covalent; Discovery; Irreversible; Mass modification; Pharmacokinetics; Screening

Indexed keywords

ABIRATERONE; AFATINIB; BOCEPREVIR; CANERTINIB; CARFILZOMIB; DACOMITINIB; IBRUTINIB; INIPARIB; NERATINIB; TELAPREVIR; VIGABATRIN; CYTOCHROME P450; CYTOCHROME P450 INHIBITOR; ISOENZYME; PROTEIN BINDING;

AREA UNDER THE CURVE; ARTICLE; CACO 2 CELL LINE; CONTROLLED STUDY; DRUG PENETRATION; DRUG SCREENING; DRUG STABILITY; HUMAN; IN VITRO STUDY; IN VIVO STUDY; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; PLASMA CLEARANCE; PRIORITY JOURNAL; RAT; SEQUENCE ANALYSIS; TIME TO MAXIMUM PLASMA CONCENTRATION; TURNOVER TIME; ANIMAL; BIOLOGICAL MODEL; BLOOD; DRUG DEVELOPMENT; DRUG EFFECTS; ENZYME SPECIFICITY; ENZYMOLOGY; HIGH THROUGHPUT SCREENING; INTESTINE ABSORPTION; INTESTINE MUCOSA; INTRAVENOUS DRUG ADMINISTRATION; KINETICS; LIVER MICROSOME; MALE; METABOLISM; ORAL DRUG ADMINISTRATION; PERMEABILITY; PROCEDURES; WORKFLOW;

RATTUS;

ADMINISTRATION, INTRAVENOUS; ADMINISTRATION, ORAL; ANIMALS; CACO-2 CELLS; CYTOCHROME P-450 ENZYME INHIBITORS; CYTOCHROME P-450 ENZYME SYSTEM; DRUG DISCOVERY; DRUG STABILITY; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; INTESTINAL ABSORPTION; INTESTINAL MUCOSA; ISOENZYMES; KINETICS; MALE; MICROSOMES, LIVER; MODELS, BIOLOGICAL; PERMEABILITY; PROTEIN BINDING; RATS; SUBSTRATE SPECIFICITY; WORKFLOW;

EID: 84925446013     PISSN: 18723128     EISSN: None     Source Type: Journal    
DOI: 10.2174/1872312808666140317151735     Document Type: Article

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