title: Measuring receptor target coverage: a radioligand competition binding protocol for assessing the association and dissociation rates of unlabeled compounds.
abstract: The kinetics of the ligand-receptor interaction is an important feature in lead optimization for new drug candidates. The protocol described in this unit is a kinetic radioligand competition binding assay that makes possible the determination of both the association and dissociation rates of unlabeled receptor ligands.
authors.affiliation: Novartis Institutes for Biomedical Research, Horsham, West Sussex, United Kingdom.
authors.forename: David A
authors.initials: DA
authors.lastname: Sykes
authors.forename: Mark R
authors.initials: MR
authors.lastname: Dowling
authors.forename: Steven J
authors.initials: SJ
authors.lastname: Charlton
mesh_terms: D000818:Animals; D001667:Binding, Competitive / Q000502:physiology; D016466:CHO Cells; D006224:Cricetinae; D008024:Ligands; D010599:Pharmacokinetics; D011485:Protein Binding; D011869:Radioligand Assay / Q000379:methods*; D011955:Receptors, Drug / Q000378:metabolism*
chemical_list: D008024:Ligands; D011955:Receptors, Drug