Click Chemistry on Solid Phase:  Parallel Synthesis ofN-Benzyltriazole Carboxamides as Super-Potent G-Protein Coupled Receptor Ligands

2006 ◽  
Vol 8 (2) ◽  
pp. 252-261 ◽  
Author(s):  
Pilar Rodriguez Loaiza ◽  
Stefan Löber ◽  
Harald Hübner ◽  
Peter Gmeiner
Keyword(s):  
Click Chemistry ◽  
G Protein ◽  
Solid Phase ◽  
Parallel Synthesis ◽  
Receptor Ligands ◽  
G Protein Coupled Receptor ◽  
G Protein Coupled

Development of a Homogeneous High Throughput Fluorescence Polarization Assay for G Protein-Coupled Receptor Binding

2000 ◽  
Vol 5 (6) ◽  
pp. 415-419 ◽  
Author(s):  
Paul H. Lee ◽  
Debra J. Bevis
Keyword(s):  
G Protein ◽  
High Throughput ◽  
Fluorescence Polarization ◽  
Binding Assay ◽  
Solid Phase ◽  
Binding Activity ◽  
G Protein Coupled Receptor ◽  
Separation Step ◽  
Fluorescence Polarization Assay ◽  
G Protein Coupled

Traditional methods that follow receptor ligand interactions are competitive assays in which the test compound displaces a radiolabeled molecule. These assays require either a time-consuming step for separation of free ligands from bound ligands or immobilization of receptors and the scintillant on a solid-phase support. In this report, we describe the development of a homogeneous binding assay for a G protein-coupled receptor in the fluorescence polarization format. This homogeneous fluorescence polarization binding assay format is superior to the traditional binding methods because no radioisotope, separation step, or solid-phase support is required. The elimination of the separation step enhances detection of low-affinity ligands and enables a real-time, continuous readout of the binding activity in a high throughput 384-well microplate format.

Quo vadis G protein-coupled receptor ligands? A tool for analysis of the emergence of new groups of compounds over time

2017 ◽  
Vol 27 (3) ◽  
pp. 626-631 ◽  
Author(s):  
Damian Leśniak ◽  
Stanisław Jastrzębski ◽  
Sabina Podlewska ◽  
Wojciech M. Czarnecki ◽  
Andrzej J. Bojarski
Keyword(s):  
G Protein ◽  
Receptor Ligands ◽  
G Protein Coupled Receptor ◽  
Quo Vadis ◽  
G Protein Coupled ◽  
Over Time
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