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gpcrMAX GPCR Assay Panel

The largest commercial panel of functional cell-based assays available, gpcrMAX contains a set of 168 GPCRs covering over 60 distinct receptor families including Adrenergic, Dopamine, P2Y, Serotonin and many others. Powered by the PathHunter® technology, this panel utilizes Arrestin recruitment to rapidly, reliably and reproducibly profile compounds using a common G-protein independent readout.

With the largest menu of functional GPCR assays and regularly scheduled test dates, gpcrMAX is an ideal choice for all stages of drug discovery and development, from lead discovery & hit identification to lead optimization, preclinical and compound safety.

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gpcrMAX Assay Panel

Listed below are the assays currently available for screening and profiling.

 
Family ▲Target GeneCommon NameArrestin
5-HydroxytryptamineHTR1A5HT1AX
5-HydroxytryptamineHTR1B5HT1BX
5-HydroxytryptamineHTR1F5HT1FX
5-HydroxytryptamineHTR2A5HT2AX
5-HydroxytryptamineHTR2C5HT2CX
5-HydroxytryptamineHTR5A5HT5AX
5-HydroxytryptamineHTR1E5HT1EX
AcetylcholineCHRM1M1X
AcetylcholineCHRM2M2X
AcetylcholineCHRM3M3X
AcetylcholineCHRM4M4X
AcetylcholineCHRM5M5X
AdenosineADORA3A3X
AdrenoceptorsADRA1Bα1B-adrenoceptorX
AdrenoceptorsADRA2Aα2A-adrenoceptorX
AdrenoceptorsADRA2Bα2B-adrenoceptorX
AdrenoceptorsADRA2Cα2C-adrenoceptorX
AdrenoceptorsADRB1β1-adrenoreceptorX
AdrenoceptorsADRB2β2-adrenoreceptorX
AngiotensinAGTR1AT1X
ApelinAGTRL1APJX
BombesinBRS3BB3X
BombesinGRPRBB2X
BombesinNMBRBB1X
BradykininBDKRB1B1X
BradykininBDKRB2B2X
CalcitoninCALCRCTX
CalcitoninCALCRL-RAMP1Calcitonin receptor-like receptorX
CalcitoninCALCRL-RAMP2Calcitonin receptor-like receptorX
CalcitoninCALCRL-RAMP3Calcitonin receptor-like receptorX
CalcitoninCALCR-RAMP2CTX
CalcitoninCALCR-RAMP3CTX
CannabinoidCNR1CB1X
CannabinoidCNR2CB2X
ChemerinCMKLR1CMKLR1X
ChemokineCCR1CCR1X
ChemokineCCR10CCR10X
ChemokineCCR2CCR2X
ChemokineCCR3CCR3X
ChemokineCCR4CCR4X
ChemokineCCR5CCR5X
ChemokineCCR6CCR6X
ChemokineCCR7CCR7X
ChemokineCCR8CCR8X
ChemokineCCR9CCR9X
ChemokineCX3CR1CX3CR1X
ChemokineCXCR1CXCR1X
ChemokineCXCR2CXCR2X
ChemokineCXCR3CXCR3X
ChemokineCXCR4CXCR4X
ChemokineCXCR5CXCR5X
ChemokineCXCR6CXCR6X
ChemokineCXCR7CXCR7X
CholecystokininCCKARCCK1X
CholecystokininCCKBRCCK2X
Class A OrphanEBI2GPR183X
Class A OrphanGPR1GPR1X
Class A OrphanGPR119GPR119X
Class A OrphanGPR35GPR35X
Class A OrphanMRGPRX1MRGPRX1X
Class A OrphanMRGPRX2MRGX2X
Complement peptideC3AR1C3AX
Complement peptideC5AR1C5AX
Complement peptideC5L2C5L2X
Corticotropin-releasing factorCRHR1CRF1X
Corticotropin-releasing factorCRHR2CRF2X
DopamineDRD1D1X
DopamineDRD2LD2LX
DopamineDRD2SD2SX
DopamineDRD3D3X
DopamineDRD4D4X
DopamineDRD5D5X
EndothelinEDNRAETAX
EndothelinEDNRBETBX
FormylpeptideFPR1FPR1X
FormylpeptideFPRL1FPR2/ALXX
Free Fatty AcidFFAR1FFA1X
Free fatty acidGPR120FFA4X
GalaninGALR1GALR1X
GalaninGALR2GALR2X
GhrelinGHSRghrelinX
GlucagonGCGRglucagonX
GlucagonGIPRGIPX
GlucagonGLP1RGLP-1X
GlucagonGLP2RGLP-2X
GlucagonSCTRsecretinX
Glycoprotein hormone receptorFSHRFSHRX
Glycoprotein hormone receptorLHCGRLHX
Glycoprotein hormone receptorTSHR(L)TSHX
HistamineHRH1H1X
HistamineHRH2H2X
HistamineHRH3H3X
HistamineHRH4H4X
Hydroxycarboxylic acidGPR109AHCA2X
Hydroxycarboxylic acidGPR109BHCA3X
Kisspeptin receptorKISS1RkisspeptinX
LeukotrieneLTB4RBLT1X
LeukotrieneOXER1OXEX
Lysophospholipid (LPA)EDG4LPA2X
Lysophospholipid (LPA)EDG7LPA3X
Lysophospholipid (LPA)GPR92GPR92X
Lysophospholipid (S1P)EDG1S1P1X
Lysophospholipid (S1P)EDG3S1P3X
Lysophospholipid (S1P)EDG5S1P2X
Lysophospholipid (S1P)EDG6S1P4X
Melanin-concentrating hormone MCHR1MCH1X
Melanin-concentrating hormone MCHR2MCH2X
MelanocortinMC1RMC1X
MelanocortinMC3RMC3X
MelanocortinMC4RMC4X
MelanocortinMC5RMC5X
MelatoninMTNR1AMT1X
MotilinMLNRmotilinX
Neuromedin UNMU1RNMU1X
Neuropeptide B & WNPBWR1NPBW1X
Neuropeptide B & WNPBWR2NPBW2X
Neuropeptide FF & AFNPFFR1NPFF1X
Neuropeptide SNPSR1bNPS receptorX
Neuropeptide YNPY1RY1X
Neuropeptide YNPY2RY2X
Neuropeptide YPPYR1Y4X
NeurotensinNTSR1NTS1X
OpioidOPRD1δX
OpioidOPRK1κX
OpioidOPRL1NOPX
OpioidOPRM1μX
OrexinHCRTR1OX1X
OrexinHCRTR2OX2X
P2YP2RY1P2RY1X
P2YP2RY11P2Y11X
P2YP2RY12P2Y12X
P2YP2RY2P2Y2X
P2YP2RY4P2Y4X
P2YP2RY6P2Y6X
Parathyroid hormonePTHR1PTH1X
Parathyroid hormonePTHR2PTH2X
Peptide P518GPR103QRFPRX
Platelet-activating factorPTAFRPAFX
ProkineticinPROKR1PKR1X
ProkineticinPROKR2PKR2X
Prolactin releasing peptide receptorPRLHRPRRPX
ProstanoidCRTH2PTGDR2X
ProstanoidPTGER2EP2X
ProstanoidPTGER3EP3X
ProstanoidPTGER4EP4X
ProstanoidPTGFRFPX
ProstanoidPTGIRIP1X
ProstanoidTBXA2RTPX
Protease activatedF2RPAR1X
Protease activatedF2RL1PAR2X
Protease activatedF2RL3PAR4X
RelaxinRXFP3RXFP3X
SomatostatinSSTR1SST1X
SomatostatinSSTR2SST2X
SomatostatinSSTR3SST3X
SomatostatinSSTR5SST5X
TachykininTACR1NK1X
TachykininTACR2NK2X
TachykininTACR3NK3X
Thyrotropin releasing hormoneTRHRTRH1X
UrotensinUTR2UTX
Vasopressin and OxytocinAVPR1AV1AX
Vasopressin and OxytocinAVPR1BV1BX
Vasopressin and OxytocinAVPR2V2X
Vasopressin and OxytocinOXTROTX
VIP and PACAPADCYAP1R1PAC1X
VIP and PACAPVIPR1VPAC1X
VIP and PACAPVIPR2VPAC2X

Assay Performance

Our gpcrMAX panel can identify a specific ligand interaction with a receptor. Once identified, each hit can be confirmed using one of our alternate functional readouts.

Identification and Confirmation of Novel Hits

GPCRsvcs panels performance
Full GPCR panel profiling was performed at a single ligand concentration (Left panel), resulting in the identification of a potent interaction. Follow-up IC50s were determined using PathHunter Arrestin and HitHunter cAMP assays to confirm ligand potency for the target, which revealed a novel ligand (Right panels).

 

Data Analysis & Interpretation 

Definitions

Percent Activity/Inhibition

The results for single concentration (primary screen) for tested compound(s) are reported in your study report and spreadsheets as '% Activity' or '% Inhibition' and are calculated in the following manner:
 

% Activity
(Agonist Mode) =
100% x
[
Mean RLU (test sample)- Mean RLU(vehicle control)

Mean MAX RLU (control ligand)- Mean RLU (vehicle control)
]
 

test sample = client supplied compound
vehicle control = DMSO (0% activity)
control ligand = control compound (100% activity)

 

% Inhibition
(Antagonist mode) =
100% x
[ 1- 
Mean RLU (test sample)- Mean RLU(vehicle control)

Mean MAX RLU (control ligand)- Mean RLU (vehicle control)
]
 

test sample = client supplied compound
vehicle control = DMSO (0% activity)
EC80 control = control compound (80% activity) 

 

Dose Response Curve (EC50/IC50)

The results for 10-point dose response curve compound/target interactions are reported in the study report and spreadsheets as EC50/IC50, which are values derived using the Hill equation:

hill equation

Panel Features & Benefits

  • Comprehensive panel of functional cell-based assays for 168 known GPCRs
  • Single, G-protein independent readout for reliable data comparison across all receptors
  • Run in agonist and antagonist modes
  • Regularly scheduled panel dates
  • Broad applications including target identification, specificity and selectivity
  • Additional confirmation services available – Arrestin, cAMP, Calcium or Internalization readouts
How it Works

To ensure your compounds are included in the Test Date of your choosing, submit your compounds and PO by the date indicated in the "Compounds & PO Due" column below.

2017 gpcrMAX and orphanMAX Panel Run Schedule

Panel Test Dates Compounds & PO Due Report & Invoicing
gpcrMAX,
orphanMAX
January 31 January 27 February 28
March 14 March 10 April 11
April 25 April 21 May 23
June 6 June 2 July 4
July 18 July 14 August 15
August 29 August 25 September 26
October 10 October 6 November 7
November 28 November 22 December 26
 

2017 nhrMAX, tkMAX, and pathMAX Panel Run Schedule

Panel Test Dates Compounds & PO Due Report & Invoicing

nhrMAX,
tkMAX, pathMAX

February 14 February 10 March 14
March 28 March 24 April 25
May 9 May 5 June 6
June 20 June 16 July 18
August 1 July 28 August 29
September 12 September 8 October 10
October 24 October 20 November 21