GPCR agonists

Golla, R. and Seethala, R., A homogeneous enzyme fragment complementation cyclic AMP screen for GPCR agonists, /. Biomol. Screen., 7, 515, 2002. 

Fig. 2. Distribution of twelve large target-specific groups of pharmaceutical agents within the Kohonen map (a) G-protein-coupled receptors (GPCR) agonists/antagonists (5,432 compounds) (b) matrix metalloproteinase inhibitors (120 compounds) (c) tyrosine kinase inhibitors (175 compounds) (d) caspase inhibitors (50 compounds) (e) NMDA receptor agonists/antagonists (150 compounds) (f) potassium channel blockers/activators (302 compounds) ...

Fig. 6. Distribution of the tested compounds (dottedline) within the Kohonen map (a) the overlap with G-protein-coupled receptors (GPCR) agonists/antagonists area (b) the overlap with chemokine receptor antagonist areas (c) the selection of compounds which can be regarded as potential agents acting against CXCR4 chemokine receptor (shaded area).

Harding, P. J., Hadingham, T. C., McDonnell, J. M., Watts, A. (2006). Direct analysis of a GPCR-agonist interaction by surface plasmon resonance. European Biophysics Journal, 35, 709-712. 

There are some general pitfalls for the medicinal chemist to consider when running and evaluating a cellular GPCR agonist single-point screen. 

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