Kinetics of nonpeptide antagonist binding to the human gonadotropin-releasing hormone receptor: Implications for structure-activity relationships and insurmountable antagonism

Biochemical Pharmacology

Volumn 72, Issue 7, 2006, Pages 838-849

  Sullivan, Susan K ^a   Hoare, Sam R J ^a   Fleck, Beth A ^a   Zhu, Yun Fei ^a   Heise, Christopher E ^a   Struthers, R Scott ^a   Crowe, Paul D ^a  

^a NEUROCRINE BIOSCIENCES INC   (United States)

Author keywords

Dissociation rate constant; G protein coupled receptor; Gonadotropin releasing hormone; Nonpeptide antagonist; Receptor kinetics; Structure activity relationship

Indexed keywords

1 (2 FLUORO,6 METHANESULFINYLBENZYL) 3 (AMINO 2 PHENETHYL) 5 (2 FLUORO 3 METHOXYPHENYL) 6 METHYLURACIL; 1 (2 FLUORO,6 METHANESULFONYLBENZYL) 3 (AMINO 2 PHENETHYL) 5 (2 FLUORO 3 METHOXYPHENYL) 6 METHYLURACIL; 1 (2 FLUORO,6 TRIFLUOROMETHYLBENZYL) 3 (AMINO 2 PHENETHYL) 5 (2 FLUORO 3 METHOXYPHENYL) 6 METHYLURACIL; 1 (2,6 DIFLUOROBENZYL) 3 (AMINO 2 PHENETHYL) 5 (2 FLUORO 3 METHOXYPHENYL) 6 METHYLURACIL; FUNCTIONAL GROUP; GONADORELIN; GONADORELIN ANTAGONIST; GONADORELIN RECEPTOR; INOSITOL PHOSPHATE; LIGAND; NBI 42902; RADIOLIGAND; TRITIUM; UNCLASSIFIED DRUG; URACIL; URACIL DERIVATIVE;

ANIMAL CELL; ARTICLE; BINDING COMPETITION; BINDING KINETICS; BIOACCUMULATION; CONTROLLED STUDY; DISSOCIATION CONSTANT; DRUG ANTAGONISM; DRUG IDENTIFICATION; DRUG RECEPTOR BINDING; ISOTOPE LABELING; NONHUMAN; PRIORITY JOURNAL; RAT; STRUCTURE ACTIVITY RELATION;

BINDING, COMPETITIVE; HUMANS; KINETICS; LIGANDS; MOLECULAR STRUCTURE; QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIP; RADIOLIGAND ASSAY; RECEPTORS, LHRH; THYMINE; TRITIUM; URACIL;

EID: 33748074796     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bcp.2006.07.011     Document Type: Article

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