GPCR assays  

Challenging targets, such as GPCRs and RTKs, are very attractive for drug discovery because they are easily accessible on cell surfaces. Yet, it is exactly this feature which makes assay development so difficult – these membrane proteins are usually not stable enough upon purification. We therefore invested in establishing RTK and GPCR assays to provide our clients with ready-made solutions, which require little investment.

Our established biochemical assays enable measuring affinities and kinetics of label-free ligand-GPCR interaction. The assays leverage carefully optimized solubilization conditions that allow production of monodisperse GPCR particles. Available for CXCR4, CXCR7, CCK2, NTSR1, ADRB2, NOP, ETA, KOR, chimeric MOR, AT1, SST2, APJ and NK1. Please contact us for a quote. If you don't find your GPCR assay among the established ones, we are happy to discuss feasibility of a customized solution.

We recently published with our customer Merck KGaA the use of FCCS to support the identification of Methionine Aminopeptidase-2 (MetAP-2) inhibitor M8891.

See our new publication on the quantifiaction of target occupancy in tissue:

Check out our new GPCR-ligand interaction assay!