This new and powerful technology has been used for a couple of years only in a range of interesting applications in academia and drug discovery:

• GPCR functional assay incl. orphan receptors
• Receptor oligimerization
• Membrane reorganisation 
• Protein-protein interactions e.g. interaction of circadian clock proteins

Especially in the field of GPCR research BRET opens new opportunities to the researcher as has some very important advantages over other technologies (e.g. FP, SPA, Aequorin luminescence, radio-ligand or fluo-ligand binding)

• Homogenous: no separation step required
• Non-radioactive: luminescent and fluorescent labels
• Universal: all GPCRs can be screened without limitation to either Gi, Gs or Gq Stable signal: time lag between agonist/antagonist addition is not critical; dependent only on the available amount of substrate
• Ratiometric readout: minimal interference of cell numbers and environmental conditions
• Kinetic opportunities
• No labelling: “labels” are proteins which are co-expressed
• Ultra-low background: no autofluorescence of cellular or medium substances as no excitation is necessary

To get some idea of how important GPCRs are in drug discovery:

• Currently ~ 30 % of drugs are targeted against GPCRs
• Only 5 % of the known receptors are targeted with drugs
• To only 20 % of the rest the corresponding ligands are known

And – the Mithras LB 940 and TriStar LB 941 are currently the only instruments meeting the needs for sensitivity and consistency which offers injection possibilities.