Concepedia

Probing the Metabotropic Glutamate Receptor 5 (mGlu5) Positive Allosteric Modulator (PAM) Binding Pocket: Discovery of Point Mutations That Engender a “Molecular Switch” in PAM Pharmacology

Karen J. Gregory, Elizabeth D. Nguyen, Sean D. Reiff, Emma F. Squire, Shaun R. Stauffer, Craig W. Lindsley, Jens Meiler, P. Jeffrey Conn

Molecular Pharmacology · 2013 · 73 citations · 52 references

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References

52

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

, , +14

High-Resolution Crystal Structure of an Engineered Human β <sub>2</sub> -Adrenergic G Protein–Coupled Receptor

Vadim Cherezov, Daniel M. Rosenbaum, Michael A. Hanson et al. · Science · 2007 · 3.3K citations · Full text

, , +17

Rosetta3

Andrew Leaver‐Fay, Michael D. Tyka, Steven M. Lewis et al. · Methods in enzymology on CD-ROM/Methods in enzymology · 2010 · 2K citations

2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist

F. Gasparini, Kurt Lingenhöhl, Natacha Stoehr et al. · Neuropharmacology · 1999 · 720 citations

, , +7

ROSETTALIGAND: Protein–small molecule docking with full side‐chain flexibility

Jens Meiler, David Baker · Proteins Structure Function and Bioinformatics · 2006 · 517 citations

, , +17