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gpcrDUO & gpcrTRIO Multi-Pathway Analysis

DiscoverX is proud to be the only outsourced GPCR service provider that can offer complete compound characterization by providing multiple, functional readouts for the same receptor. Access to the same GPCR target in different technology formats enables identification of G-protein or Arrestin biased ligands. Discover novel ligands with unique attributes, determine mechanism of action or uncover potential side effect profiles of novel drug candidates.

gpcrDUO-TRIO Assay Panel

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

 

gpcrTRIO

Target Gene ▲Common NameArrestincAMPCalciumInternalization
ADCYAP1R1Adenylate cyclase activating polypeptide receptor 1 (PAC1)XXXX
ADRA2CAdrenergic receptor alpha 2C (α2C-adrenoceptor)XX X
ADRB2Adrenergic receptor beta 2 (β2-adrenoreceptor)XX X
AGTRL1Apelin receptor (APJ)XX X
AVPR1AVasopressin receptor 1A (V1A)X XX
AVPR1BVasopressin receptor 1B (V1B)X XX
AVPR2Vasopressin receptor 2 (V2)XX X
BDKRB2Bradykinin receptor B2 (B2)X XX
C3AR1Complement component 3a receptor 1 (C3A)XX X
C5AR1Complement component 5a receptor 1 (C5A)XX X
CCKARCholecystokinin A receptor (CCK1)X XX
CCKBRCholecystokinin B receptor (CCK2)X XX
CCR1Chemokine (C-C motif) receptor 1 (CCR1)XX X
CCR10Chemokine (C-C motif) receptor 10 (CCR10)XX X
CCR5Chemokine (C-C motif) receptor 5 (CCR5)XX X
CCR6Chemokine (C-C motif) receptor 6 (CCR6)XX X
CCR7Chemokine (C-C motif) receptor 7 (CCR7)XX X
CHRM1Cholinergic receptor, muscarinic 1 (M1)X XX
CHRM2Cholinergic receptor, muscarinic 2 (M2)XX X
CHRM3Cholinergic receptor, muscarinic 3 (M3)X XX
CHRM4Cholinergic receptor, muscarinic 4 (M4)XX X
CHRM5Cholinergic receptor, muscarinic 5 (M5)X XX
CMKLR1Chemokine-like receptor 1 (CMKLR1)XX X
CRHR1Corticotropin releasing hormone receptor 1 (CRF1)XX X
CXCR1Chemokine (C-X-C motif) receptor 1 (CXCR1)XX X
CXCR2Chemokine (C-X-C motif) receptor 2 (CXCR2)XX X
CXCR3Chemokine (C-X-C motif) receptor 3 (CXCR3)XX X
CXCR4Chemokine (C-X-C motif) receptor 4 (CXCR4)XX X
CXCR6Chemokine (C-X-C motif) receptor 6 (CXCR6)XX X
DRD1Dopamine receptor D1 (D1)XX X
EBI2G protein-coupled receptor 183 (GPR183)XX X
EDG1Sphingosine 1-phosphate receptor 1 (S1P1)XX X
EDG3Sphingosine 1-phosphate receptor 3 (S1P3)X XX
EDG7Lysophosphatidic acid receptor 3 (LPA3)X XX
F2RL1Coagulation factor II (thrombin) receptor-like 1 (PAR2) (PAR2)X XX
F2RL3Coagulation factor II (thrombin) receptor-like 3 (PAR4) (PAR4)X XX
FPR1Formylpeptide receptor 1 (FPR1)XXXX
FPRL1Formylpeptide receptor-like 1 (FPR2/ALX)XX X
GALR1Galanin receptor 1 (GALR1)XX X
GCGRGlucagon receptor (glucagon)XX X
GIPRGastric inhibitory polypeptide receptor (GIP)XX  
GLP1RGlucagon-like peptide receptor 1 (GLP-1)XX X
GLP2RGlucagon-like peptide receptor 2 (GLP-2)XX X
GPR35G-protein coupled receptor 35 (GPR35)XX X
GRPRGastrin releasing peptide receptor (BB2)X XX
HCRTR1Orexin receptor 1 (OX1)X XX
HCRTR2Orexin receptor 2 (OX2)X XX
HRH2Histamine receptor H2 (H2)XXX 
HTR2A5-hydroxytryptamine receptor 2A (5HT2A)X XX
HTR2C5-hydroxytryptamine receptor 2C (5HT2C)X XX
LTB4RLeukotriene B4 receptor (BLT1)XXXX
MC3RMelanocortin receptor 3 (MC3)XX X
MCHR1Melanin concentrating hormone receptor 1 (MCH1)XX X
MLNRMotilin receptor (motilin)X XX
MTNR1AMelatonin receptor 1A (MT1)XX X
MTNR1BMelatonin receptor 1B (MT2)XX X
NMBRNeuromedin B Receptor (BB1)X XX
NMU1RNeuromedin U receptor 1 (NMU1)X XX
NPY2RNeuropeptide Y receptor Y2 (Y2)XXXX
NTSR1Neurotensin receptor 1 (NTS1)X XX
OPRD1Opioid receptor delta (δ)XX X
OPRK1Opioid receptor kappa (κ)XX X
OPRL1Opioid receptor-like receptor (NOP)XX X
OPRM1Opioid receptor mu (μ)XX X
OXTROxytocin Receptor (OT)X XX
P2RY1Purinergic receptor P2Y, G-protein coupled, 1 (P2RY1)X XX
P2RY2Purinergic receptor P2Y, G-protein coupled, 2 (P2Y2)X XX
P2RY4Pyrimidinergic receptor P2Y, G-protein coupled, 4 (P2Y4)X  X
PROKR1Prokineticin receptor 1 (PKR1)XXXX
PROKR2Prokineticin receptor 2 (PKR2)X  X
PTAFRPlatelet activating receptor (PAF)X XX
PTGFRProstaglandin F receptor (FP) (FP)X XX
PTGIRProstaglandin I2 (prostacyclin) receptor (IP) (IP1)XX X
PTHR1Parathyroid hormone receptor 1 (PTH1)XXXX
PTHR2Parathyroid hormone receptor 2 (PTH2)XXXX
RXFP3Relaxin family peptide receptor 3 (RXFP3)XX X
RXFP4Relaxin family peptide receptor 4 (RXFP4)XX  
SCTRSecretin receptor (secretin)XX X
SSTR2Somatostatin receptor 2 (SST2)XX X
TACR1Tachykinin receptor 1 (NK1)X XX
TACR2Tachykinin receptor 2 (NK2)X XX
TACR3Tachykinin receptor 3 (NK3)XXXX
UTR2Urotensin II receptor (UT)X XX
VIPR1Vasoactive intestinal peptide receptor 1 (VPAC1)XXXX
VIPR2Vasoactive intestinal peptide receptor 2 (VPAC2)XXXX
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gpcrDUO

Target Gene ▲Common NameArrestincAMPCalciumInternalization
ADCYAP1R1Adenylate cyclase activating polypeptide receptor 1 (PAC1)XXXX
ADORA1Adenosine receptor A1 (A1)XX  
ADORA3Adenosine receptor A3 (A3)XX  
ADRA1BAdrenergic receptor alpha 1B (α1B-adrenoceptor)X X 
ADRA2AAdrenergic receptor alpha 2A (α2A-adrenoceptor)XX  
ADRA2CAdrenergic receptor alpha 2C (α2C-adrenoceptor)XX X
ADRB1Adrenergic receptor beta 1 (β1-adrenoreceptor)XX  
ADRB2Adrenergic receptor beta 2 (β2-adrenoreceptor)XX X
AGTR1Angiotensin II receptor, type 1 (AT1)X X 
AGTRL1Apelin receptor (APJ)XX X
AVPR1AVasopressin receptor 1A (V1A)X XX
AVPR1BVasopressin receptor 1B (V1B)X XX
AVPR2Vasopressin receptor 2 (V2)XX X
BDKRB1Bradykinin receptor B1 (B1)X X 
BDKRB2Bradykinin receptor B2 (B2)X XX
BRS3Bombesin receptor, subtype 3 (BB3)X X 
C3AR1Complement component 3a receptor 1 (C3A)XX X
C5AR1Complement component 5a receptor 1 (C5A)XX X
C5L2G-Protein Coupled Receptor 77 (C5L2)X  X
CALCRCalcitonin receptor (CT)XX  
CALCRL-RAMP1Calcitonin receptor-like (Calcitonin receptor-like receptor)XX  
CALCRL-RAMP3Calcitonin receptor-like (Calcitonin receptor-like receptor)XX  
CALCR-RAMP3Calcitonin receptor (CT)XX  
CCKARCholecystokinin A receptor (CCK1)X XX
CCKBRCholecystokinin B receptor (CCK2)X XX
CCR1Chemokine (C-C motif) receptor 1 (CCR1)XX X
CCR10Chemokine (C-C motif) receptor 10 (CCR10)XX X
CCR2Chemokine (C-C motif) receptor 2 (CCR2)X  X
CCR4Chemokine (C-C motif) receptor 4 (CCR4)X  X
CCR5Chemokine (C-C motif) receptor 5 (CCR5)XX X
CCR6Chemokine (C-C motif) receptor 6 (CCR6)XX X
CCR7Chemokine (C-C motif) receptor 7 (CCR7)XX X
CHRM1Cholinergic receptor, muscarinic 1 (M1)X XX
CHRM2Cholinergic receptor, muscarinic 2 (M2)XX X
CHRM3Cholinergic receptor, muscarinic 3 (M3)X XX
CHRM4Cholinergic receptor, muscarinic 4 (M4)XX X
CHRM5Cholinergic receptor, muscarinic 5 (M5)X XX
CMKLR1Chemokine-like receptor 1 (CMKLR1)XX X
CNR1Cannabinoid receptor 1 (CB1)XX  
CNR2Cannabinoid receptor 2 (CB2)XX  
CRHR1Corticotropin releasing hormone receptor 1 (CRF1)XX X
CRHR2Corticotropin releasing hormone receptor 2 (CRF2)XX X
CRTH2prostaglandin D2 receptor 2 (PTGDR2)XX  
CXCR1Chemokine (C-X-C motif) receptor 1 (CXCR1)XX X
CXCR2Chemokine (C-X-C motif) receptor 2 (CXCR2)XX X
CXCR3Chemokine (C-X-C motif) receptor 3 (CXCR3)XX X
CXCR4Chemokine (C-X-C motif) receptor 4 (CXCR4)XX X
CXCR5Burkitt lymphoma receptor (CXCR5)XX  
CXCR6Chemokine (C-X-C motif) receptor 6 (CXCR6)XX X
CXCR7Chemokine (C-X-C motif) receptor 7 (CXCR7)X  X
DRD1Dopamine receptor D1 (D1)XX X
DRD2LDopamine Receptor D2 (long isoform) (D2L)XX  
DRD2SDopamine Receptor D2 (short isoform) (D2S)XX  
DRD4Dopamine Receptor D4 (D4)XX  
DRD5Dopamine receptor D5 (D5)XX  
EBI2G protein-coupled receptor 183 (GPR183)XX X
EDG1Sphingosine 1-phosphate receptor 1 (S1P1)XX X
EDG2Lysophosphatidic acid receptor 1 (LPA1)  XX
EDG3Sphingosine 1-phosphate receptor 3 (S1P3)X XX
EDG4Lysophosphatidic acid receptor 2 (LPA2)X X 
EDG5Sphingosine 1-phosphate receptor 2 (S1P2)X  X
EDG7Lysophosphatidic acid receptor 3 (LPA3)X XX
EDNRAEndothelin receptor type A (ETA)X X 
EDNRBEndothelin receptor type B (ETB)X  X
F2RL1Coagulation factor II (thrombin) receptor-like 1 (PAR2) (PAR2)X XX
F2RL3Coagulation factor II (thrombin) receptor-like 3 (PAR4) (PAR4)X XX
FFAR1Free fatty acid receptor 1 (FFA1)X X 
FPR1Formylpeptide receptor 1 (FPR1)XXXX
FPRL1Formylpeptide receptor-like 1 (FPR2/ALX)XX X
FSHRFollicle stimulating hormone receptor (FSHR)XX  
GALR1Galanin receptor 1 (GALR1)XX X
GALR2Galanin receptor 2 (GALR2)X X 
GCGRGlucagon receptor (glucagon)XX X
GHSRGhrelin receptor (ghrelin)X X 
GIPRGastric inhibitory polypeptide receptor (GIP)XX  
GLP1RGlucagon-like peptide receptor 1 (GLP-1)XX X
GLP2RGlucagon-like peptide receptor 2 (GLP-2)XX X
GPBAR1G protein-coupled bile acid receptor 1 (GPBA)XX  
GPR1G-protein coupled receptor 1 (GPR1)X  X
GPR103pyroglutamylated RFamide peptide receptor (QRFPR)X X 
GPR109AHydroxycarboxylic acid receptor 2 (HCA2)XX  
GPR109BHydroxycarboxylic acid receptor 3 (HCA3)XX  
GPR120G-protein coupled receptor 120, long isoform (FFA4)X  X
GPR35G-protein coupled receptor 35 (GPR35)XX X
GPR92Lysophosphatidic acid receptor 5 (GPR92)X X 
GRPRGastrin releasing peptide receptor (BB2)X XX
HCRTR1Orexin receptor 1 (OX1)X XX
HCRTR2Orexin receptor 2 (OX2)X XX
HRH1Histamine receptor H1 (H1)X X 
HRH2Histamine receptor H2 (H2)XXX 
HRH3Histamine receptor H3 (H3)XX  
HTR1A5-hydroxytryptamine receptor 1A (5HT1A)XX  
HTR1B5-hydroxytryptamine receptor 1B (5HT1B)XX  
HTR1F5-hydroxytryptamine receptor 1F (5HT1F)XX  
HTR2A5-hydroxytryptamine receptor 2A (5HT2A)X XX
HTR2C5-hydroxytryptamine receptor 2C (5HT2C)X XX
HTR5A5-hydroxytryptamine receptor 5A (5HT5A)XX  
LHCGRChoriogonadotropin receptor (LH)XX  
LTB4RLeukotriene B4 receptor (BLT1)XXXX
MC1RMelanocortin receptor 1 (MC1)XX  
MC3RMelanocortin receptor 3 (MC3)XX X
MC4RMelanocortin receptor 4 (MC4)XX  
MC5RMelanocortin receptor 5 (MC5)XX  
MCHR1Melanin concentrating hormone receptor 1 (MCH1)XX X
MCHR2Melanin-concentrating hormone receptor 2 (MCH2)X X 
MLNRMotilin receptor (motilin)X XX
MRGPRX1MAS-related GPR, member X1 (MRGPRX1)X X 
MRGPRX2MAS-related GPR, member X2 (MRGX2)X X 
MTNR1AMelatonin receptor 1A (MT1)XX X
MTNR1BMelatonin receptor 1B (MT2)XX X
NMBRNeuromedin B Receptor (BB1)X XX
NMU1RNeuromedin U receptor 1 (NMU1)X XX
NPBWR1Neuropeptides B/W receptor 1 (NPBW1)XX  
NPBWR2Neuropeptides B/W receptor 2 (NPBW2)XX  
NPFFR1Neuropeptide FF receptor 1 (NPFF1)XX  
NPY2RNeuropeptide Y receptor Y2 (Y2)XXXX
NTSR1Neurotensin receptor 1 (NTS1)X XX
OPRD1Opioid receptor delta (δ)XX X
OPRK1Opioid receptor kappa (κ)XX X
OPRL1Opioid receptor-like receptor (NOP)XX X
OPRM1Opioid receptor mu (μ)XX X
OXER1Oxoeicosanoid (OXE) receptor 1 (OXE)XX X
OXTROxytocin Receptor (OT)X XX
P2RY1Purinergic receptor P2Y, G-protein coupled, 1 (P2RY1)X XX
P2RY11Purinergic receptor P2Y, G-protein coupled, 11 (P2Y11)X   
P2RY2Purinergic receptor P2Y, G-protein coupled, 2 (P2Y2)X XX
P2RY4Pyrimidinergic receptor P2Y, G-protein coupled, 4 (P2Y4)X  X
PPYR1Pancreatic polypeptide receptor 1 (Y4)XX  
PRLHRProlactin releasing hormone receptor (PRRP)X XX
PROKR1Prokineticin receptor 1 (PKR1)XXXX
PROKR2Prokineticin receptor 2 (PKR2)X  X
PTAFRPlatelet activating receptor (PAF)X XX
PTGER3Prostaglandin E receptor 3 (subtype EP3) (EP3)XXX 
PTGER4Prostaglandin E receptor 4 (subtype EP4) (EP4)X  X
PTGFRProstaglandin F receptor (FP) (FP)X XX
PTGIRProstaglandin I2 (prostacyclin) receptor (IP) (IP1)XX X
PTHR1Parathyroid hormone receptor 1 (PTH1)XXXX
PTHR2Parathyroid hormone receptor 2 (PTH2)XXXX
RXFP3Relaxin family peptide receptor 3 (RXFP3)XX X
RXFP4Relaxin family peptide receptor 4 (RXFP4)XX  
SCTRSecretin receptor (secretin)XX X
SSTR2Somatostatin receptor 2 (SST2)XX X
SSTR3Somatostatin receptor 3 (SST3)XX  
SSTR4Somatostatin receptor 4 (SST4)XX  
SSTR5Somatostatin receptor 5 (SST5)XX  
TACR1Tachykinin receptor 1 (NK1)X XX
TACR2Tachykinin receptor 2 (NK2)X XX
TACR3Tachykinin receptor 3 (NK3)XXXX
TBXA2RThromboxane A2 receptor (TP)X XX
TRHRThyrotropin-releasing hormone receptor (TRH1)X XX
TSHR(L)Thyroid Stimulating Hormone Receptor (TSH)XX  
UTR2Urotensin II receptor (UT)X XX
VIPR1Vasoactive intestinal peptide receptor 1 (VPAC1)XXXX
VIPR2Vasoactive intestinal peptide receptor 2 (VPAC2)XXXX
XCR1Chemokine (C motif) XC receptor 1 (XCR1)XX  
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Multi-mode Screening and Profiling

With gpcrDUO, screen or profile compounds using two different assay readouts in parallel. The complex relationship that exists between G-protein and β-Arrestin signaling determines both the efficacy and potential side effects of GPCR-targeted drugs. Quantitatively examining these pathways in parallel can aid in defining compound function and can lead to the discovery of novel biased ligands with unique attributes.

 
gpcrDUO Multi-Mode Screening and Profiling
 

Species Selectivity of Lead Compounds

gpcrDUO allows identification of species selective agonists and superagonists, as well as determining compound dosing prior to testing in expensive animal models.

 
GPCR_Duo_data.png
 

Mode of Action Studies

Our flexible gpcrTRIO capabilities help you identify novel compounds with distinct activation or recycling profiles and allow you to uncover potency and efficacy differences between compounds based on different stages of receptor signaling. Utilize gpcrTRIO for better prediction of compound activity in vivo.

 
GPCR_Trio_data.png
 
Cell lines over expressing the human Opioid Receptor δ (OPRD1, hDOR) in the (A) cAMP (B) Arrestin and (C) Internalization formats were treated with known hDOR agonists. To enable a graphic representation and agonist comparison, data was normalized to the reference agonist, [Met5]-Enkephalin in potency (set equal to 1) and efficacy (set equal to 100%).

 

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
gpcrDUO Select a single target in 2 different assay readouts (Arrestin, cAMP, or Calcium and Internalization) or determine species selectivity by comparing pharmacology of your compound against human and ortholog receptors.
gpcrTRIO Go beyond potency and selectivity to determine mode of action by studying the same target using all 3 assay readouts (Arrestin, cAMP, or Calcium and Internalization). gpcrTRIO is an ideal tool for understanding how GPCR receptor activation (G-protein-dependent or -independent) or desensitization determines compound activity.