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Estimation of the dissociation rate of unlabelled ligand–receptor complexes by a ‘two‐step’ competition binding approach
Author(s) -
Packeu A,
Wennerberg M,
Balendran A,
Vauquelin G
Publication year - 2010
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.2010.00931.x
Subject(s) - radioligand , radioligand assay , ligand (biochemistry) , chemistry , receptor , biophysics , dissociation (chemistry) , stereochemistry , ligand binding assay , receptor–ligand kinetics , affinities , biochemistry , biology , organic chemistry
Because the in vivo effectiveness of ligands may also be determined by the rate by which they dissociate from their target receptors, drug candidates are being increasingly screened for this kinetic property. The dissociation rate of unlabelled ligand-receptor complexes can be estimated indirectly from their ability to slow the association of subsequently added radioligand molecules.