Positive Allosteric Modulators of Metabotropic Glutamate Receptor 5 as Tool Compounds to Study Signaling Bias

Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction

Yung-Chi Cheng, William H. Prusoff · Biochemical Pharmacology · 1973 · 12.9K citations

Life Sciences, Biochemistry, Chemical Kinetics +14

The kinetics of competitive radioligand binding predicted by the law of mass action.

Harvey Motulsky, L C Mahan · Molecular Pharmacology · 1984 · 419 citations

Medicine, Chemistry, Pharmacology +17

Structure of class C GPCR metabotropic glutamate receptor 5 transmembrane domain

A.S. Dore, Krzysztof Okrasa, Jayesh C. Patel et al. · Nature · 2014 · 411 citations

Life Sciences, Molecular Biology, Neuroscience +12

LY341495 is a nanomolar potent and selective antagonist of group II metabotropic glutamate receptors

Anne Kingston, Paul L. Ornstein, Rebecca A. Wright et al. · Neuropharmacology · 1998 · 365 citations

Life Sciences, Neuroscience, Pharmacology +16

The role of kinetic context in apparent biased agonism at GPCRs

Carmen Klein Herenbrink, David A. Sykes, Prashant Donthamsetti et al. · Nature Communications · 2016 · 337 citations · Full text

Medicine, Medicinal Chemistry, Pharmacology +17