Mechanism-based inhibition: Deriving kiand kinact directly from time-dependent ic50 values

Journal of Biomolecular Screening

Volumn 14, Issue 8, 2009, Pages 913-923

  Krippendorff, Ben Fillippo ^a,b   Neuhaus, Roland ^c   Lienau, Philip ^c   Reichel, Andreas ^c   Huisinga, Wilhelm ^a,b  

^a NATIONAL UNIVERSITY OF IRELAND   (Ireland)

^b INTERNATIONAL MAX PLANCK RESEARCH SCHOOL FOR COMPUTATIONAL BIOLOGY AND SCIENTIFIC COMPUTING   (Germany)

^c BAYER PHARMA AG   (Germany)

Author keywords

Cheng Prusoff relation; Irreversible inhibition; Time dependent IC50 values

Indexed keywords

BERGAMOTTIN; CYTOCHROME P450 1A2; CYTOCHROME P450 3A4; ERYTHROMYCIN; ETHINYLESTRADIOL; FURAFYLLINE; RALOXIFENE; SUICIDE SUBSTRATE; VERAPAMIL;

ARTICLE; COMPETITIVE INHIBITION; COMPUTER PROGRAM; CONTROLLED STUDY; DRUG ACTIVITY; DRUG POTENCY; DRUG TARGETING; ENZYME INACTIVATION; ENZYME INHIBITION; FLUOROMETRY; IC 50; INHIBITION KINETICS; PHARMACOLOGICAL PARAMETERS; PRIORITY JOURNAL; TIME;

BINDING, COMPETITIVE; CYTOCHROME P-450 CYP1A2; CYTOCHROME P-450 CYP3A; DRUG ANTAGONISM; ENZYME ACTIVATION; ENZYME INHIBITORS; HUMANS; INHIBITORY CONCENTRATION 50; MODELS, CHEMICAL; MODELS, THEORETICAL; TIME FACTORS;

EID: 70349642091     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057109336751     Document Type: Article

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