Ontology highlight
ABSTRACT:
SUBMITTER: Bosma R
PROVIDER: S-EPMC6536503 | biostudies-literature | 2019 May
REPOSITORIES: biostudies-literature
Bosma Reggie R Stoddart Leigh A LA Georgi Victoria V Bouzo-Lorenzo Monica M Bushby Nick N Inkoom Loretta L Waring Michael J MJ Briddon Stephen J SJ Vischer Henry F HF Sheppard Robert J RJ Fernández-Montalván Amaury A Hill Stephen J SJ Leurs Rob R
Scientific reports 20190527 1
Drug-target binding kinetics are suggested to be important parameters for the prediction of in vivo drug-efficacy. For G protein-coupled receptors (GPCRs), the binding kinetics of ligands are typically determined using association binding experiments in competition with radiolabelled probes, followed by analysis with the widely used competitive binding kinetics theory developed by Motulsky and Mahan. Despite this, the influence of the radioligand binding kinetics on the kinetic parameters derive ...[more]