GPCRs Assays

G protein-coupled receptors (GPCRs), also known as 7TM receptors, constitute the largest superfamily of cell surface receptors. These receptors play key roles in regulation of a wide variety of physiological processes, including cognition, metabolism, inflammation, immunity and cell proliferation, as well as development. Despite the large number of GPCRs that are available as potential drug targets, currently approved drugs only address a small portion of the known receptors; many GPCRs remain uncharacterized. Thus, this target class remains an area of strong interest in drug discovery.

GPCR Signaling Pathway

Figure 1 GPCR Signaling Pathway

MedAI provides GPCR radioligand binding assays for different targets. Gold standard filtration assays are conducted with an agonist or antagonist at a single concentration or a dose response for IC50 determination.

GPCR functional assays that cover multiple second messenger pathways are available. These include cAMP for Gi and Gs coupled receptors, IP1 and IP3/calcium flux for Gq coupled receptors, label free assays for endogenous signaling and traditional GTPγS assays. Agonist and antagonist assays are available in single or dose response for EC50 and IC50 determination.

GPCRs gene list that are targets for approved drugs
ACKR3 HCRTR2 CRHR1 P2RY11 AVPR1B LHCGR GCGR S1PR3
ADGRG3 HRH1 CXCR4 P2RY12 AVPR2 MC1R GHRHR S1PR4
ADORA1 HRH2 CYSLTR1 P2RY13 BDKRB1 MC2R GLP1R S1PR5
ADORA2A HRH3 CYSLTR2 P2RY2 BDKRB2 MC3R GLP2R SCTR
ADORA2B HRH4 DRD1 P2RY6 CALCR MC4R GNRHR SMO
ADORA3 HTR1A DRD2 PTGDR CASR MC5R GPBAR1 SSTR1
ADRA1A HTR1B DRD3 PTGDR2 CCKAR MLNR GPER1 SSTR2
ADRA1B HTR1D DRD4 PTGER1 CCKBR MRGPRX1 GPR143 SSTR3
ADRA1D HTR1E DRD5 PTGER2 CCR4 MTNR1A GPR18 SSTR4
ADRA2A HTR1F EDNRA PTGER3 CCR5 MTNR1B GPR35 SSTR5
ADRA2B HTR2A EDNRB PTGER4 CHRM1 NPY4R GPR55 SUCNR1
ADRA2C HTR2B F2R PTGFR CHRM2 NTSR2 GPR68 TAAR1
ADRB1 HTR2C FFAR1 PTGIR CHRM3 OPRD1 HCAR1 TACR1
ADRB2 HTR4 FPR1 PTH1R CHRM4 OPRK1 HCAR2 TBXA2R
ADRB3 HTR5A FSHR PTH2R CHRM5 OPRM1 HCAR3 TRHR
AGTR1 HTR6 GABBR1 S1PR1 CNR1 OXTR HCRTR1 TSHR
AVPR1A HTR7 GABBR2 S1PR2 CNR2 P2RY1    

It is important to understand GPCR's on-and-off target activity, when assessing the potential efficacy and liabilities of GPCR therapeutics. Methods to measure GPCRs come in many forms- In addition to measures of direct ligand binding, many are indirect assays that measure events proximal to binding the represent different signaling pathways- these include reporter assays, cAMP quantitation, β-Arrestin recruitment, IP3 measurements and calcium flux to name a few. GPCR screening and profiling assays from MedAI provide the most comprehensive cell-based assay offering along with the fastest turnaround time in the industry for rapid efficacy, potency, and selectivity determination during SAR and Lead Optimization.

Related Platform:

Online Inquiry

Please submit a detailed description of your project. We will provide you with a customized project plan to meet your research requests. You can also send emails directly to inquiry@protheragen.com for inquiries.

Verification code

Copyright © 2021 Protheragen Inc. All Rights Reserved.