J Biomol Screen 2015 Aug 15;20(7):858-68. Epub 2015 Apr 15.
The Scripps Research Institute Molecular Screening Center, Scripps Florida, Jupiter, FL, USA Amgen Inc., Thousand Oaks, CA, USA.
Muscarinic acetylcholine receptors (mAChRs) have long been viewed as viable targets for novel therapeutic agents for the treatment of Alzheimer's disease and other disorders involving impaired cognitive function. In an attempt to identify orthosteric and allosteric modulators of the muscarinic acetylcholine receptor M(4) (M(4)), we developed a homogenous, multiparametric, 1536-well assay to measure M(4) receptor agonism, positive allosteric modulation (PAM), and antagonism in a single well. This assay yielded a Z' of 0. Read More