DiscoverX PathHunter™ eXpress CMKLR1 Activated GPCR Internalization Assay

The PathHunter™ CMKLR1 Activated GPCR internalization eXpress kit provides an easy to-use cell based assay to study drug candidates (small molecules or biologics) affecting GPCR activation and internalization. This kit assesses ligand (e.g. chemerin) based internalization of CMKLR1 via detection of localization to the early endosome. This product uses EFC technology. The included cells overexpress EA-tagged β-arrestin 2 as well as a PK-tagged early endosome protein and untagged CMKLR1. Upon ligand-induced receptor activation, β-arrestin 2 is recruited to the activated GPCR and the resulting CMKLR1-arrestin complex is internalized to the early endosome, leading to production of EFC signal. eXpress kits are a convenient, ready-to-use format which contains all materials needed to run the assay, including single-use vials of cryopreserved cells, cell plating media, detection reagent, and assay plates.