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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-HydroxytryptamineHTR1F5HT1FXX  
5-HydroxytryptamineHTR2A5HT2AX XX
5-HydroxytryptamineHTR2C5HT2CX XX
5-HydroxytryptamineHTR5A5HT5AXX  
5-HydroxytryptamineHTR1E5HT1EX   
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  
ChemokineCXCR6CXCR6X   
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 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 A OrphanGPR22GPR22X   
Class B OrphanBAI1BAI1X   
Class B OrphanBAI2BAI2X   
Class B OrphanBAI3BAI3X   
Class B OrphanGPR123GPR123X   
Class B OrphanGPR157GPR157X   
Class B OrphanGPR97GPR97X   
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    
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