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gpcrE/IC50ELECT

Quantitate compound potency against any GPCRscan functional cell-based assay.  Agonist half maximal effective concentrations (EC50s) and antagonist half maximal inhibitory concentrations (IC50s) are calculated from duplicate 10-point dose-response curves.  Measurements are made under optimized conditions to generate consistent and reproducible data that reliably reflects the drug’s potency.

gpcrE/IC50ELECT may be used as an ideal follow-up study tool to quantify the potency of compound-GPCR target interactions identified in primary screens, to supplement existing data, or support lead optimization and SAR activity.

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Watch this short video to learn about allosteric modulators of GPCR and PAM and NAM curves. Watch Recording.

gpcrE/IC50ELECT Assay Panel

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

 
Family ▲Target GeneCommon NameArrestincAMPCalciumInternalization
5-HydroxytryptamineHTR1A5HT1AXX  
5-HydroxytryptamineHTR1B5HT1BXX  
5-HydroxytryptamineHTR1E5HT1EX   
5-HydroxytryptamineHTR1F5HT1FXX  
5-HydroxytryptamineHTR2A5HT2AX XX
5-HydroxytryptamineHTR2C5HT2CX XX
5-HydroxytryptamineHTR5A5HT5AXX  
AcetylcholineCHRM1M1X XX
AcetylcholineCHRM2M2XX X
AcetylcholineCHRM3M3X XX
AcetylcholineCHRM4M4XX X
AcetylcholineCHRM5M5X XX
AdenosineADORA3A3XX  
AdrenoceptorsADRA1Bα1B-adrenoceptorX X 
AdrenoceptorsADRA2Aα2A-adrenoceptorXX  
AdrenoceptorsADRA2Bα2B-adrenoceptorX   
AdrenoceptorsADRA2Cα2C-adrenoceptorXX X
AdrenoceptorsADRB1β1-adrenoreceptorXX  
AdrenoceptorsADRB2β2-adrenoreceptorXX X
AngiotensinAGTR1AT1X X 
ApelinAGTRL1APJXX X
BombesinBRS3BB3X X 
BombesinGRPRBB2X XX
BombesinNMBRBB1X XX
BradykininBDKRB1B1X X 
BradykininBDKRB2B2X XX
CalcitoninCALCRCTXX  
CalcitoninCALCRL-RAMP1Calcitonin receptor-like receptorXX  
CalcitoninCALCRL-RAMP2Calcitonin receptor-like receptorX   
CalcitoninCALCRL-RAMP3Calcitonin receptor-like receptorXX  
CalcitoninCALCR-RAMP2CTXX  
CalcitoninCALCR-RAMP3CTXX  
CannabinoidCNR1CB1XX  
CannabinoidCNR2CB2XX  
ChemerinCMKLR1CMKLR1XX X
ChemokineCCR1CCR1XX X
ChemokineCCR10CCR10XX X
ChemokineCCR2CCR2X  X
ChemokineCCR3CCR3X   
ChemokineCCR4CCR4X  X
ChemokineCCR5CCR5XX X
ChemokineCCR6CCR6XX X
ChemokineCCR7CCR7XX X
ChemokineCCR8CCR8X   
ChemokineCCR9CCR9X   
ChemokineCCRL2CCRL2X   
ChemokineCX3CR1CX3CR1X   
ChemokineCXCR1CXCR1XX X
ChemokineCXCR2CXCR2XX X
ChemokineCXCR3CXCR3XX X
ChemokineCXCR4CXCR4XX X
ChemokineCXCR5CXCR5XX  
ChemokineCXCR6CXCR6XX X
ChemokineCXCR7CXCR7X  X
ChemokineDARCFYX   
CholecystokininCCKARCCK1X XX
CholecystokininCCKBRCCK2X XX
Class A OrphanEBI2GPR183XX X
Class A OrphanGHSR1bGHSR1bX   
Class A OrphanGPR1GPR1X  X
Class A OrphanGPR101GPR101X   
Class A OrphanGPR119GPR119X   
Class A OrphanGPR12GPR12X   
Class A OrphanGPR132GPR132X   
Class A OrphanGPR135GPR135X   
Class A OrphanGPR139GPR139X   
Class A OrphanGPR141GPR141X   
Class A OrphanGPR142GPR142X   
Class A OrphanGPR146GPR146X   
Class A OrphanGPR148GPR148X   
Class A OrphanGPR149GPR149X   
Class A OrphanGPR15GPR15X   
Class A OrphanGPR150GPR150X   
Class A OrphanGPR151GPR151X   
Class A OrphanGPR152GPR152X   
Class A OrphanGPR161GPR161X   
Class A OrphanGPR162GPR162X   
Class A OrphanGPR17GPR17X X 
Class A OrphanGPR171GPR171X   
Class A OrphanGPR173GPR173X   
Class A OrphanGPR176GPR176X   
Class A OrphanGPR18GPR18X   
Class A OrphanGPR182GPR182X   
Class A OrphanGPR20GPR20X   
Class A OrphanGPR22GPR22X   
Class A OrphanGPR23LPA4X   
Class A OrphanGPR25GPR25X   
Class A OrphanGPR26GPR26X   
Class A OrphanGPR27GPR27X   
Class A OrphanGPR3GPR3X   
Class A OrphanGPR31GPR31X   
Class A OrphanGPR32GPR32X   
Class A OrphanGPR35GPR35XX X
Class A OrphanGPR37EDNRBLX   
Class A OrphanGPR37L1GPR37L1X   
Class A OrphanGPR39GPR39X X 
Class A OrphanGPR4GPR4X   
Class A OrphanGPR45GPR45X   
Class A OrphanGPR50GPR50X   
Class A OrphanGPR52GPR52X   
Class A OrphanGPR55GPR55X   
Class A OrphanGPR6GPR6X   
Class A OrphanGPR61GPR61X   
Class A OrphanGPR65GPR65X   
Class A OrphanGPR75GPR75X   
Class A OrphanGPR78GPR78X   
Class A OrphanGPR79GPR79X   
Class A OrphanGPR83GPR83X   
Class A OrphanGPR84GPR84XX  
Class A OrphanGPR85GPR85X   
Class A OrphanGPR88GPR88X   
Class A OrphanLGR4LGR4X   
Class A OrphanLGR5LGR5X   
Class A OrphanLGR6LGR6X   
Class A OrphanMRGPRDMRGPRDX   
Class A OrphanMRGPREMRGPREX   
Class A OrphanMRGPRFMRGPRFX   
Class A OrphanMRGPRX1MRGPRX1X X 
Class A OrphanMRGPRX2MRGX2X X 
Class A OrphanMRGPRX4MRGPRX4X   
Class A OrphanOPN5OPN5X   
Class A OrphanOXGR1OXGR1X X 
Class A OrphanP2RY8P2RY8X   
Class A OrphanTAAR5TAAR5X   
Class B OrphanBAI1BAI1X   
Class B OrphanBAI2BAI2X   
Class B OrphanBAI3BAI3X   
Class B OrphanGPR123GPR123X   
Class B OrphanGPR157GPR157X   
Class B OrphanGPR97GPR97X   
Complement peptideC3AR1C3AXX X
Complement peptideC5AR1C5AXX X
Complement peptideC5L2C5L2X  X
Corticotropin-releasing factorCRHR1CRF1XX X
Corticotropin-releasing factorCRHR2CRF2XX X
Cytosolic tyrosine kinaseFGRFGR    
Cytosolic tyrosine kinaseJAK3JAK3    
Cytosolic Tyrosine KinasePRLR-JAK1PRLR    
Cytosolic Tyrosine KinasePRLR-JAK2PRLR    
Cytosolic tyrosine kinaseTYK2TYK2    
DopamineDRD1D1XX X
DopamineDRD2LD2LXX  
DopamineDRD2SD2SXX  
DopamineDRD3D3X   
DopamineDRD4D4XX  
DopamineDRD5D5XX  
EndothelinEDNRAETAX X 
EndothelinEDNRBETBX  X
Estrogen (G protein coupled) receptorGPR30GPERX   
FormylpeptideFPR1FPR1XXXX
FormylpeptideFPRL1FPR2/ALXXX X
Free Fatty AcidFFAR1FFA1X X 
Free fatty acidGPR120FFA4X  X
GalaninGALR1GALR1XX X
GalaninGALR2GALR2X X 
GhrelinGHSRghrelinX X 
GlucagonGCGRglucagonXX X
GlucagonGIPRGIPXX  
GlucagonGLP1RGLP-1XX X
GlucagonGLP2RGLP-2XX X
GlucagonSCTRsecretinXX X
Glycoprotein hormone receptorFSHRFSHRXX  
Glycoprotein hormone receptorLHCGRLHXX  
Glycoprotein hormone receptorTSHR(L)TSHXX  
HistamineHRH1H1X X 
HistamineHRH2H2XXX 
HistamineHRH3H3XX  
HistamineHRH4H4X   
Hydroxycarboxylic acidGPR109AHCA2XX  
Hydroxycarboxylic acidGPR109BHCA3XX  
Kisspeptin receptorKISS1RkisspeptinX   
LeukotrieneLTB4RBLT1XXXX
LeukotrieneOXER1OXEXX X
Lysophospholipid (LPA)EDG4LPA2X X 
Lysophospholipid (LPA)EDG7LPA3X XX
Lysophospholipid (LPA)GPR92GPR92X X 
Lysophospholipid (S1P)EDG1S1P1XX X
Lysophospholipid (S1P)EDG3S1P3X XX
Lysophospholipid (S1P)EDG5S1P2X  X
Lysophospholipid (S1P)EDG6S1P4X   
Melanin-concentrating hormone MCHR1MCH1XX X
Melanin-concentrating hormone MCHR2MCH2X X 
MelanocortinMC1RMC1XX  
MelanocortinMC3RMC3XX X
MelanocortinMC4RMC4XX  
MelanocortinMC5RMC5XX  
MelatoninMTNR1AMT1XX X
MotilinMLNRmotilinX XX
Neuromedin UNMU1RNMU1X XX
Neuropeptide B & WNPBWR1NPBW1XX  
Neuropeptide B & WNPBWR2NPBW2XX  
Neuropeptide FF & AFNPFFR1NPFF1XX  
Neuropeptide SNPSR1bNPS receptorX   
Neuropeptide YNPY1RY1X   
Neuropeptide YNPY2RY2XXXX
Neuropeptide YPPYR1Y4XX  
NeurotensinNTSR1NTS1X XX
NHRARAR    
NHRERαESR1    
NHRFXRNR1H4    
NHRGRNR3C1    
NHRLXRαNR1H3    
NHRLXRβNR1H2    
NHRMRNR3C2    
NHRPPARαPPARA    
NHRPPARγPPARG    
NHRPPARδPPARD    
NHRPRαPGR    
NHRPRβPGR    
NHRRARαRARA    
NHRRARβRARB    
NHRRXRαRXRA    
NHRRXRγRXRG    
NHRTHRαTHRA    
NHRTHRβTHRB    
OpioidOPRD1δXX X
OpioidOPRK1κXX X
OpioidOPRL1NOPXX X
OpioidOPRM1μXX X
OrexinHCRTR1OX1X XX
OrexinHCRTR2OX2X XX
Other 7TM proteinsGPR107GPR107X   
Other 7TM proteinsGPR137TM7SF1X   
Other 7TM proteinsGPR143GPR143X   
P2YP2RY1P2RY1X XX
P2YP2RY11P2Y11X   
P2YP2RY12P2Y12X  X
P2YP2RY2P2Y2X XX
P2YP2RY4P2Y4X  X
P2YP2RY6P2Y6X   
Parathyroid hormonePTHR1PTH1XXXX
Parathyroid hormonePTHR2PTH2XXXX
Peptide P518GPR103QRFPRX X 
Platelet-activating factorPTAFRPAFX XX
ProkineticinPROKR1PKR1XXXX
ProkineticinPROKR2PKR2X  X
Prolactin releasing peptide receptorPRLHRPRRPX XX
ProstanoidCRTH2PTGDR2XX  
ProstanoidPTGER2EP2XX  
ProstanoidPTGER3EP3XXX 
ProstanoidPTGER4EP4X  X
ProstanoidPTGFRFPX XX
ProstanoidPTGIRIP1XX X
ProstanoidTBXA2RTPX XX
Protease activatedF2RPAR1X   
Protease activatedF2RL1PAR2X XX
Protease activatedF2RL3PAR4X XX
Receptor Tyrosine Kinasec-KITKIT    
Receptor Tyrosine Kinasec-Ret-GFRα2RET    
Receptor Tyrosine KinaseDDR1CD167a    
Receptor Tyrosine KinaseEphA5EphA5    
Receptor Tyrosine KinaseEphA7EphA7    
Receptor Tyrosine KinaseEphB2EphB2    
Receptor Tyrosine KinaseEphB3EphB3    
Receptor Tyrosine KinaseEphB4EphB4    
Receptor Tyrosine KinaseErbB1EGFR    
Receptor Tyrosine KinaseErbB2-ErbB3HER2    
Receptor Tyrosine KinaseErbB4HER4    
Receptor Tyrosine KinaseFLT4FLT4    
Receptor Tyrosine KinaseIGF1RIGF1R    
Receptor Tyrosine KinaseINSRbINSR    
Receptor Tyrosine KinaseKDRVEGFR2    
Receptor Tyrosine KinasePDGFRaPDGFRa    
Receptor Tyrosine KinasePDGFRbPDGFRb    
Receptor Tyrosine KinaseTrkA-P75NTRK1    
Receptor Tyrosine KinaseTrkB-P75NTRK2    
Receptor Tyrosine KinaseTrkC-P75NTRK3    
RelaxinRXFP3RXFP3XX X
SomatostatinSSTR1SST1X   
SomatostatinSSTR2SST2XX X
SomatostatinSSTR3SST3XX  
SomatostatinSSTR5SST5XX  
TachykininTACR1NK1X XX
TachykininTACR2NK2X XX
TachykininTACR3NK3XXXX
Thyrotropin releasing hormoneTRHRTRH1X XX
UrotensinUTR2UTX XX
Vasopressin and OxytocinAVPR1AV1AX XX
Vasopressin and OxytocinAVPR1BV1BX XX
Vasopressin and OxytocinAVPR2V2XX X
Vasopressin and OxytocinOXTROTX XX
VIP and PACAPADCYAP1R1PAC1XXXX
VIP and PACAPVIPR1VPAC1XXXX
VIP and PACAPVIPR2VPAC2XXXX

Quantitative Measurement of Drug Potency

gpcrE/IC50ELECT is the ideal follow-up study tool to quantify the potency of compound-GPCR target interactions identified in primary screens.

PathHunter Arrestin cells expressing the CRTH2 receptor were tested with a panel of known ligands. These assays are able to provide quantitative affinity measurements for a variety of compounds including agonists, antagonists, inverse agonists and allosteric modulators.

Confirmation of Novel Hits

gpcrE/IC50ELECT is the ideal follow-up study tool to quantify the potency of compound-GPCR target interactions identified in primary screens.

Full GPCR panel profiling was performed at a single concentration of a ligand (Left panel), resulting in 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.

Data Analysis & Interpretation 

What does the term EC50 mean?

The term half maximal effective concentration (EC50) refers to the concentration of a drug or biologic which induces a response halfway between the baseline and the maximum. Therefore, the EC50 of a compound or biologic represents the concentration where 50% of it’s maximal effect can be observed. It is commonly used as a measure of the drug’s potency.

What does an IC50 measure?

The term half maximal inhibitory concentration (EC50) is a measure of the effectiveness of a compound to inhibit a given biological response. Therefore, the IC50 of a compound or biologic represents the half maximal (50%) inhibitory concentration and is commonly used as a measure of antagonist drug’s potency.

How are the EC50/IC50s calculated?

For each compound/GPCR target interaction, dose response curves  are generated using 10 concentrations of agonist or antagonist (10-point curve). The results are reported as EC50/IC50 which derived using the Hill equation:

hill equation

Panel Features and Benefits

  • 10-point dose response curve in duplicate
  • Broad dynamic range – can detect full receptor occupancy
  • Differentiate between full and partial agonists, inverse agonists and allosteric modulator
  • Large assay windows, even for Gi targets 
 

Arrestin

2nd Messenger

Internalization

 
 
How it Works
How it Works
How it Works