PathHunter® eXpress CHRM1 Activated GPCR Internalization Assay

Background Information:

The PathHunter® CHRM1 Activated GPCR internalization eXpress kit provides an easy to-use cell based assay to study drug candidates affecting GPCR activation and internalization. This kit assesses ligand (e.g. oxotremorine) based internalization of CHRM1 via detection of localization to the early endosome. This product uses EFC technology. The cells included overexpress EA-tagged β-arrestin 2 as well as a PK-tagged early endosome protein and untagged CHRM1. Upon ligand-induced receptor activation, β-arrestin 2 is recruited to the activated GPCR and the resulting CHRM1-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.

Target Class:

GPCR

Family:

Acetylcholine (Muscarinic)

Sub Family:

Class A

Coupling:

Gq

Protein Name:

M1

Protein Aliases:

acetylcholine receptor, muscarinic 1

Accession Number:

AF498915

UniProt Number:

P11229

Gene Name:

CHRM1

Gene ID:

1128

Target Species:

Human

Cell Background:

U2OS