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GPCR scanLibrary℠

In contrast to the traditional drug discovery model where a target is nominated on the basis of biology and screened against a compound library for putative hits in a single-target high-throughput (HTS) screening campaign, GPCR scanLIBRARY affords researchers the ability to screen an entire compound library against multiple biological targets of interest simultaneously.

As the development of novel GPCR-targeted drugs continues to expand into multiple therapeutic areas, safety and selectivity data will become even more vital. A fully profiled library has a defined ‘footprint’ across the entire family of GPCRs. Knowledge of which targets can or cannot be accessed with the current chemistry reduces the likelihood of pursuing programs ill-suited to achieve the clinical candidate profile. Likewise, compounds that display an array of selectivity patterns that may not only reveal new clinical applications but may also serve as ‘tool’ compounds for investigating activity in vivo. And with the re-emergence of phenotypic screens, GPCR scanLIBRARY provides an opportunity to uncover potent and selective compounds with minimal knowledge about the target receptor and mode of action and these high quality lead like compounds can be used to initiate lead optimization programs.

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GPCRscan Assay Panel

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

 
Family ▲Target GeneCommon NameArrestincAMPCalciumInternalization
5-HydroxytryptamineHTR1A5-hydroxytryptamine receptor 1A (5HT1A)XX  
5-HydroxytryptamineHTR1B5-hydroxytryptamine receptor 1B (5HT1B)XX  
5-HydroxytryptamineHTR1F5-hydroxytryptamine receptor 1F (5HT1F)XX  
5-HydroxytryptamineHTR2A5-hydroxytryptamine receptor 2A (5HT2A)X X 
5-HydroxytryptamineHTR2B5-hydroxytryptamine receptor 2B (5HT2B)  X 
5-HydroxytryptamineHTR2C5-hydroxytryptamine receptor 2C (5HT2C)X XX
5-HydroxytryptamineHTR2C(VGV)5-hydroxytryptamine receptor 2C - VGV isoform (5HT2C)X   
5-HydroxytryptamineHTR2C(VNV)5-hydroxytryptamine receptor 2C - VNV isoform (5HT2C)X   
5-HydroxytryptamineHTR2C(VSV)5-hydroxytryptamine receptor 2C - VSV isoform (5HT2C)X   
5-HydroxytryptamineHTR5A5-hydroxytryptamine receptor 5A (5HT5A)XX  
5-HydroxytryptamineHTR65-hydroxytryptamine receptor 6 (5HT6)X   
5-HydroxytryptamineHTR7D5-hydroxytryptamine receptor 7D (5HT7D) X  
5-HydroxytryptaminemHTR2A5-Hydroxytryptamine receptor 2A (m5HT2A)X   
5-HydroxytryptaminemHTR2C5-Hydroxytryptamine receptor 2C (m5HT2C)X   
5-HydroxytryptaminerHTR2C5-hydroxytryptamine receptor 2C (HTR2C)X   
5-HydroxytryptamineHTR1E5-hydroxytryptamine receptor 1E (5HT1E)X   
AcetylcholinerCHRM4Cholinergic receptor, muscarinic 4 (rM4)X   
AcetylcholineCHRM1Cholinergic receptor, muscarinic 1 (M1)X XX
AcetylcholineCHRM2Cholinergic receptor, muscarinic 2 (M2)XX X
AcetylcholineCHRM3Cholinergic receptor, muscarinic 3 (M3)X XX
AcetylcholineCHRM4Cholinergic receptor, muscarinic 4 (M4)XX X
AcetylcholineCHRM5Cholinergic receptor, muscarinic 5 (M5)X XX
AdenosineADORA1Adenosine receptor A1 (A1)XX  
AdenosineADORA2AAdenosine receptor A2A (A2A)  X 
AdenosineADORA2BAdenosine receptor A2B (A2B) X  
AdenosineADORA3Adenosine receptor A3 (A3)XX  
AdenosinemADORA2BAdenosine receptor A2B (mA2B)X   
AdenosinemADORA3adenosine receptor A3 (mA3)X   
AdrenoceptorsADRA1AAdrenergic receptor alpha 1A (α1A-adrenoceptor)  X 
AdrenoceptorsADRA1BAdrenergic receptor alpha 1B (α1B-adrenoceptor)X X 
AdrenoceptorsADRA2AAdrenergic receptor alpha 2A (α2A-adrenoceptor)XX  
AdrenoceptorsADRA2BAdrenergic receptor alpha 2B (α2B-adrenoceptor)X   
AdrenoceptorsADRA2CAdrenergic receptor alpha 2C (α2C-adrenoceptor)XX X
AdrenoceptorsADRB1Adrenergic receptor beta 1 (β1-adrenoreceptor)XX  
AdrenoceptorsADRB2Adrenergic receptor beta 2 (β2-adrenoreceptor)XX X
AdrenoceptorsADRB3Adrenergic receptor beta 3 (β3-adrenoreceptor) X  
AdrenoceptorsADRA1D(82-572)Adrenergic receptor alpha 1D (α1D-adrenoceptor)X   
AngiotensinAGTR1Angiotensin II receptor, type 1 (AT1)X X 
ApelinAGTRL1Apelin receptor (APJ)XX X
ApelinmAGTRL1Apelin receptor (mAPJ)X   
Bile acidGPBAR1G protein-coupled bile acid receptor 1 (GPBA)XX  
BombesinBRS3Bombesin receptor, subtype 3 (BB3)X X 
BombesinGRPRGastrin releasing peptide receptor (BB2)X XX
BombesinNMBRNeuromedin B Receptor (BB1)X XX
BradykininBDKRB1Bradykinin receptor B1 (B1)X X 
BradykininBDKRB2Bradykinin receptor B2 (B2)X XX
CalcitoninCALCRCalcitonin receptor (CT)XX  
CalcitoninCALCRL-RAMP1Calcitonin receptor-like (Calcitonin receptor-like receptor)XX  
CalcitoninCALCRL-RAMP2Calcitonin receptor-like (Calcitonin receptor-like receptor)X   
CalcitoninCALCRL-RAMP3Calcitonin receptor-like (Calcitonin receptor-like receptor)XX  
CalcitoninCALCR-RAMP2Calcitonin receptor (CT)XX  
CalcitoninCALCR-RAMP3Calcitonin receptor (CT)XX  
Calcium sensingCASRCalcium-sensing receptor (CaS)  X 
CannabinoidCNR1Cannabinoid receptor 1 (CB1)XX  
CannabinoidCNR2Cannabinoid receptor 2 (CB2)XX  
CannabinoidmCNR1Cannabinoid receptor 1 (mCB1)X   
CannabinoidmCNR2Cannabinoid receptor 2 (mCB2)X   
CannabinoidrCNR2Cannabinoid receptor 2 (CB2)X   
ChemerinCMKLR1Chemokine-like receptor 1 (CMKLR1)XX X
ChemokineCCR1Chemokine (C-C motif) receptor 1 (CCR1)XX X
ChemokineCCR10Chemokine (C-C motif) receptor 10 (CCR10)XX X
ChemokineCCR2Chemokine (C-C motif) receptor 2 (CCR2)X  X
ChemokineCCR3Chemokine (C-C motif) receptor 3 (CCR3)X   
ChemokineCCR4Chemokine (C-C motif) receptor 4 (CCR4)X  X
ChemokineCCR5Chemokine (C-C motif) receptor 5 (CCR5)XX X
ChemokineCCR6Chemokine (C-C motif) receptor 6 (CCR6)XX X
ChemokineCCR7Chemokine (C-C motif) receptor 7 (CCR7)XX X
ChemokineCCR8Chemokine (C-C motif) receptor 8 (CCR8)X   
ChemokineCCR9Chemokine (C-C motif) receptor 9 (CCR9)X   
ChemokineCCRL1chemokine (C-C motif) receptor-like 1 (CCRL1)X   
ChemokineCCRL2Chemokine (C-C motif) receptor-like 2 (CCRL2)X   
ChemokineCX3CR1Chemokine C-X3-C receptor 1 (CX3CR1)X   
ChemokineCXCR1Chemokine (C-X-C motif) receptor 1 (CXCR1)XX X
ChemokineCXCR2Chemokine (C-X-C motif) receptor 2 (CXCR2)XX X
ChemokineCXCR3Chemokine (C-X-C motif) receptor 3 (CXCR3)XX X
ChemokineCXCR4Chemokine (C-X-C motif) receptor 4 (CXCR4)XX X
ChemokineCXCR5Burkitt lymphoma receptor (CXCR5)XX  
ChemokineCXCR6Chemokine (C-X-C motif) receptor 6 (CXCR6)X   
ChemokineCXCR7Chemokine (C-X-C motif) receptor 7 (CXCR7)X  X
Chemokinecyno CXCR1Chemokine (C-X-C motif) receptor 1 (CXCR1)X   
Chemokinecyno CXCR2Chemokine (C-X-C motif) receptor 2 (CXCR2)X   
ChemokineDARCDuffy blood group, chemokine receptor (FY)X   
ChemokinemCX3CR1Chemokine (C-X3-C motif) receptor 1 (mCX3CR1)X   
ChemokinemCXCR2Chemokine (C-X-C motif) receptor 2 (mCXCR2)X   
ChemokinemCXCR3Chemokine (C-X-C motif) receptor 3 (mCXCR3)X   
ChemokinemCXCR4Chemokine (C-X-C motif) receptor 4 (mCXCR4)X   
ChemokinemCXCR5Burkitt lymphoma receptor (mCXCR5)X   
ChemokinemCXCR6Chemokine (C-X-C motif) receptor 6 (mCXCR6)X   
ChemokinemCXCR7Chemokine (C-X-C motif) receptor 7 (mCXCR7)X   
ChemokinemCCR1Chemokine (C-C motif) receptor 1 (mCC1)X   
ChemokinemCCR2Chemokine (C-C motif) receptor 2 (mCCR2)X   
ChemokinemCCR3Chemokine (C-C motif) receptor 3 (mCCR3)X   
ChemokinemCCR4Chemokine (C-C motif) receptor 4 (mCCR4)X   
ChemokinemCCR5Chemokine (C-C motif) receptor 5 (mCCR5)X   
ChemokinemCCR6Chemokine (C-C motif) receptor 6 (mCCR6)X   
ChemokinemCCR7Chemokine (C-C motif) receptor 7 (mCCR7)X   
ChemokinemCCR8Chemokine (C-C motif) receptor 8 (mCCR8)X   
Chemokine mCCR9Chemokine (C-C motif) receptor 9 (mCCR9)X   
ChemokinemCMKLR1Chemokine-Like Receptor 1 (mCMKLR1)X   
CholecystokininCCKARCholecystokinin A receptor (CCK1)X XX
CholecystokininCCKBRCholecystokinin B receptor (CCK2)X XX
Class A OrphanEBI2G protein-coupled receptor 183 (GPR183)XX X
Class A OrphanGPR1G-protein coupled receptor 1 (GPR1)X  X
Class A OrphanGPR101G-protein coupled receptor 101 (GPR101)X   
Class A OrphanGHSR1bGrowth hormone secretagogue receptor 1b (GHSR1b)X   
Class A OrphanGPR119G-protein coupled receptor 119 (GPR119)X   
Class A OrphanGPR12G-protein coupled receptor 12 (GPR12)X   
Class A OrphanGPR132G-protein coupled receptor 132 (GPR132)X   
Class A OrphanGPR135G-protein coupled receptor 135 (GPR135)X   
Class A OrphanGPR139G-protein coupled receptor 139 (GPR139)X   
Class A OrphanGPR141G-protein coupled receptor 141 (GPR141)X   
Class A OrphanGPR142G-protein coupled receptor 142 (GPR142)X   
Class A OrphanGPR146G-protein coupled receptor 146 (GPR146)X   
Class A OrphanGPR148G-protein coupled receptor 148 (GPR148)X   
Class A OrphanGPR149G-protein coupled receptor 149 (GPR149)X   
Class A OrphanGPR15G-protein coupled receptor 15 (GPR15)X   
Class A OrphanGPR150G-protein coupled receptor 150 (GPR150)X   
Class A OrphanGPR151G-protein coupled receptor 151 (GPR151)X   
Class A OrphanGPR152G-protein coupled receptor 152 (GPR152)X   
Class A OrphanGPR31G-protein coupled receptor 31 (GPR31)X   
Class A OrphanGPR32G-protein coupled receptor 32 (GPR32)X   
Class A OrphanGPR35G-protein coupled receptor 35 (GPR35)XX X
Class A OrphanGPR37Endothelin B receptor-like (EDNRBL)X   
Class A OrphanGPR37L1G protein-coupled receptor 37 like 1 (GPR37L1)X   
Class A OrphanGPR39G-protein coupled receptor 39 (GPR39)X X 
Class A OrphanGPR4G-protein coupled receptor 4 (GPR4)X   
Class A OrphanGPR45G-protein coupled receptor 45 (GPR45)X   
Class A OrphanGPR50G-protein coupled receptor 50 (GPR50)X   
Class A OrphanGPR52G-protein coupled receptor 52 (GPR52)X   
Class A OrphanGPR55G protein-coupled receptor 55 (GPR55)X   
Class A OrphanGPR6G-protein coupled receptor 6 (GPR6)X   
Class A OrphanGPR61G-protein coupled receptor 61 (GPR61)X   
Class A OrphanGPR65G-protein coupled receptor 65 (GPR65)X   
Class A OrphanGPR75G-protein coupled receptor 75 (GPR75)X   
Class A OrphanGPR78G-protein coupled receptor 78 (GPR78)X   
Class A OrphanGPR79G protein-coupled receptor 79 pseudogene (GPR79)X   
Class A OrphanMRGPRDMAS-related GPR, member D (MRGPRD)X   
Class A OrphanMRGPREMAS-related GPR, member E (MRGPRE)X   
Class A OrphanMRGPRFMAS-related GPR, member F (MRGPRF)X   
Class A OrphanMRGPRX1MAS-related GPR, member X1 (MRGPRX1)X X 
Class A OrphanMRGPRX2MAS-related GPR, member X2 (MRGX2)X X 
Class A OrphanMRGPRX4MAS-related GPR, member X4 (MRGPRX4)X   
Class A OrphanOPN5Opsin 5 (OPN5)X   
Class A OrphanmGPR1G-Protein Coupled Receptor 1 (mGPR1)X   
Class A OrphanOXGR1Oxoglutarate (alpha-ketoglutarate) receptor 1 (OXGR1)X X 
Class A OrphanmEBI2G-protein coupled receptor 183 (GPR183)X   
Class A OrphanLGR4Leucine-rich repeat-containing G protein-coupled receptor 4 (LGR4)X   
Class A OrphanLGR5Leucine-rich repeat-containing G protein-coupled receptor 5 (LGR5)X   
Class A OrphanLGR6Leucine-rich repeat-containing G protein-coupled receptor 6 (LGR6)X   
Class A OrphanGPR161G-protein coupled receptor 161 (GPR161)X   
Class A OrphanGPR162G-protein coupled receptor 162 (GPR162)X   
Class A OrphanGPR17G-protein coupled receptor 17 (GPR17)X X 
Class A OrphanGPR171G-protein coupled receptor 171 (GPR171)X   
Class A OrphanGPR173G-protein coupled receptor 173 (GPR173)X   
Class A OrphanGPR176G-protein coupled receptor 176 (GPR176)X   
Class A OrphanGPR18G-protein coupled receptor 18 (GPR18)X   
Class A OrphanGPR182G-protein coupled receptor 182 (GPR182)X   
Class A OrphanGPR20G-protein coupled receptor 20 (GPR20)X   
Class A OrphanGPR23Lysophosphatidic acid receptor 4 (LPA4)X   
Class A OrphanGPR25G-protein coupled receptor 25 (GPR25)X   
Class A OrphanGPR26G-protein coupled receptor 26 (GPR26)X   
Class A OrphanGPR27G-protein coupled receptor 27 (GPR27)X   
Class A OrphanGPR3G-protein coupled receptor 3 (GPR3)X   
Class A OrphanGPR83G-protein coupled receptor 83 (GPR83)X   
Class A OrphanGPR84G-protein coupled receptor 84 (GPR84)XX  
Class A OrphanGPR85G-protein coupled receptor 85 (GPR85)X   
Class A OrphanGPR88G-protein coupled receptor 88 (GPR88)X   
Class A OrphanP2RY8Purinergic receptor P2Y, G-protein coupled, 8 (P2RY8)X   
Class A OrphanTAAR5Trace amine associated receptor 5 (TAAR5)X   
Class A OrphanrGPR35G-protein coupled receptor 35 (rGPR35)X   
Class A OrphanmGPR84G-protein coupled receptor 84, Mouse (GPR84)X   
Class A OrphanGPR22G-protein coupled receptor 22 (GPR22)X   
Class B OrphanGPR97G-protein coupled receptor 97 (GPR97)X   
Class B OrphanGPR123G-protein coupled receptor 123 (GPR123)X   
Class B OrphanGPR157G-protein coupled receptor 157 (GPR157)X   
Class B OrphanBAI1Brain-specific angiogenesis inhibitor 1 (BAI1)X   
Class B OrphanBAI2Brain-specific angiogenesis inhibitor 2 (BAI2)X   
Class B OrphanBAI3Brain-specific angiogenesis inhibitor 3 (BAI3)X   
Complement peptideC3AR1Complement component 3a receptor 1 (C3A)X   
Complement peptideC5AR1Complement component 5a receptor 1 (C5A)XX X
Complement peptideC5L2G-Protein Coupled Receptor 77 (C5L2)X  X
Complement peptidemC5AR1Complement component 5a receptor 1 (mC5AR)X   
Corticotropin-releasing factormCRHR1Corticotropin releasing hormone receptor 1 (mCRF1)X   
Corticotropin-releasing factorCRHR1Corticotropin releasing hormone receptor 1 (CRF1)XX X
Corticotropin-releasing factorCRHR2Corticotropin releasing hormone receptor 2 (CRF2)XX X
DopamineDRD1Dopamine receptor D1 (D1)XX X
DopamineDRD2LDopamine Receptor D2 (long isoform) (D2L)XX  
DopamineDRD2SDopamine Receptor D2 (short isoform) (D2S)XX  
DopamineDRD3Dopamine Receptor D3 (D3)X   
DopamineDRD4Dopamine Receptor D4 (D4)XX  
DopamineDRD5Dopamine receptor D5 (D5)XX  
DopaminemDRD5Dopamine receptor D5 (mDRD5)X   
DopaminerDRD1Dopamine receptor D1 (rD1)X   
DopaminerDRD2LDopamine Receptor D2 (long isoform) (rD2L)X   
DopaminerDRD2SDopamine Receptor D2 (short isoform) (rD2S)X   
EndothelinmEDNRAEndothelin receptor type A (mETA)X   
EndothelinmEDNRBEndothelin receptor type B (mETB)X   
EndothelinEDNRAEndothelin receptor type A (ETA)X X 
EndothelinEDNRBEndothelin receptor type B (ETB)X  X
Estrogen (G protein coupled) receptorGPR30G protein-coupled estrogen receptor 1 (GPER)X   
Formylpeptide mFPR1Formylpeptide receptor 1 (mFPR1)X   
FormylpeptidemFPR2Formylpeptide receptor 2 (FPR2)X   
FormylpeptideFPR1Formylpeptide receptor 1 (FPR1)XX X
FormylpeptideFPR3Formyl peptide receptor 3 (FPRL2) X  
FormylpeptideFPRL1Formylpeptide receptor-like 1 (FPR2/ALX)XX X
Free fatty acidGPR120G-protein coupled receptor 120, long isoform (FFA4)X  X
Free fatty acidGPR120SG-protein Coupled Receptor 120, short isoform (FFA4)X   
Free Fatty AcidFFAR1Free fatty acid receptor 1 (FFA1)X X 
Free Fatty AcidFFAR2Free fatty acid receptor 2 (GPR43)  X 
Free Fatty AcidFFAR3Free fatty acid receptor 3 (GPR41) X  
Free fatty acidcyno GPR120G-protein coupled receptor 120 (FFA4)X   
Free Fatty AcidmFFAR1Free fatty acid receptor 1 (FFA1)X   
Free Fatty AcidrFFAR1Free fatty acid receptor 1 (FFA1)X   
Free fatty acidrGPR120G-protein coupled receptor 120 (FFA4)X   
GABABGABBR1-GABBR2gamma-aminobutyric acid (GABA) B receptor, 1 (GABB1) X  
GalaninGALR1Galanin receptor 1 (GALR1)XX X
GalaninGALR2Galanin receptor 2 (GALR2)X X 
GalaninmGALR2Galanin Receptor 2 (mGALR2)X   
GhrelinmGHSRGhrelin receptor (ghrelin)X   
GhrelinGHSRGhrelin receptor (ghrelin)X X 
GlucagonGIPRGastric inhibitory polypeptide receptor (GIP)XX  
GlucagonGLP1RGlucagon-like peptide receptor 1 (GLP-1)XX X
GlucagonGLP2RGlucagon-like peptide receptor 2 (GLP-2)XX X
GlucagonGCGRGlucagon receptor (glucagon)XX X
GlucagonGHRHRGrowth hormone releasing hormone receptor (GHRH) X  
GlucagonmGIPRGastric inhibitory polypeptide receptor (mGIP)X   
GlucagonmGLP1RGlucagon-like peptide receptor 1 (mGLP-1)X   
GlucagonmGCGRGlucagon Receptor (glucagon)X   
GlucagonSCTRSecretin receptor (secretin)XX X
Glycoprotein hormone receptorTSHR(L)Thyroid Stimulating Hormone Receptor (TSH)XX  
Glycoprotein hormone receptorLHCGRChoriogonadotropin receptor (LH)XX  
Glycoprotein hormone receptorFSHRFollicle stimulating hormone receptor (FSHR)XX  
Gonadotropin-releasing hormoneGNRHRGonadotropin-releasing hormone receptor (GnRH)  X 
HistamineHRH1Histamine receptor H1 (H1)X X 
HistamineHRH2Histamine receptor H2 (H2)XXX 
HistamineHRH3Histamine receptor H3 (H3)XX  
HistamineHRH4Histamine receptor H4 (H4)X   
Hydroxycarboxylic acidGPR109AHydroxycarboxylic acid receptor 2 (HCA2)XX  
Hydroxycarboxylic acidGPR109BHydroxycarboxylic acid receptor 3 (HCA3)XX  
Hydroxycarboxylic acidGPR81Hydroxycarboxylic acid receptor 1 (HCA1) X  
Kisspeptin receptorKISS1RKISS1-derived peptide receptor (kisspeptin)X   
LeukotrieneLTB4RLeukotriene B4 receptor (BLT1)XXXX
LeukotrienemLTB4RLeukotriene B4 receptor (mBLT1)X   
LeukotrieneOXER1Oxoeicosanoid (OXE) receptor 1 (OXE)XX X
Leukotriene CYSLTR2Cysteinyl leukotriene receptor 2 (CYSLT2)  X 
Lysophospholipid (LPA)EDG2Lysophosphatidic acid receptor 1 (LPA1)  XX
Lysophospholipid (LPA)EDG4Lysophosphatidic acid receptor 2 (LPA2)X X 
Lysophospholipid (LPA)EDG7Lysophosphatidic acid receptor 3 (LPA3)X XX
Lysophospholipid (LPA)GPR92Lysophosphatidic acid receptor 5 (GPR92)X X 
Lysophospholipid (S1P)mEDG1Sphingosine 1-phosphate receptor 1 (mS1P1)X   
Lysophospholipid (S1P)mEDG3Sphingosine 1-phosphate receptor 3 (S1P3)X   
Lysophospholipid (S1P)mEDG5Sphingosine 1-phosphate receptor 2 (mS1P2)X   
Lysophospholipid (S1P)EDG5Sphingosine 1-phosphate receptor 2 (S1P2)X  X
Lysophospholipid (S1P)EDG6Sphingosine 1-phosphate receptor 4 (S1P4)X   
Lysophospholipid (S1P)EDG3Sphingosine 1-phosphate receptor 3 (S1P3)X XX
Lysophospholipid (S1P)EDG1Sphingosine 1-phosphate receptor 1 (S1P1)XX X
Lysophospholipid (S1P)cEDG5Sphingosine 1-phosphate receptor 2 (cS1P2)X   
Lysophospholipid (S1P)sEDG5Sphingosine 1-phosphate receptor 2 (sS1P2)X   
Lysophospholipid (S1P)rEDG5Sphingosine 1-phosphate receptor 2 (rS1P2)X   
Melanin-concentrating hormone MCHR1Melanin concentrating hormone receptor 1 (MCH1)XX X
Melanin-concentrating hormone MCHR2Melanin-concentrating hormone receptor 2 (MCH2)X X 
Melanin-concentrating hormonemMCHR1Melanin concentrating hormone receptor 1 (MCH1)X   
MelanocortinMC5RMelanocortin receptor 5 (MC5)XX  
MelanocortinMC1RMelanocortin receptor 1 (MC1)XX  
MelanocortinMC3RMelanocortin receptor 3 (MC3)XX X
MelanocortinMC4RMelanocortin receptor 4 (MC4)XX  
MelatoninMTNR1AMelatonin receptor 1A (MT1)XX X
MelatoninMTNR1BMelatonin receptor 1B (MT2)XX X
Metabotropic glutamateGRM1Metabotropic glutamate receptor 1 (mGlu1)  X 
Metabotropic glutamateGRM2Metabotropic glutamate receptor 2 (mGlu2) X  
Metabotropic glutamateGRM3Metabotropic glutamate receptor 3 (MGlu3) X  
Metabotropic glutamateGRM4Metabotropic glutamate receptor 4 (mGlu4) X  
Metabotropic glutamateGRM5Metabotropic glutamate receptor 5 (mGlu5)  X 
Metabotropic glutamateGRM6Metabotropic glutamate receptor 6 (mGlu6) X  
MotilinMLNRMotilin receptor (motilin)X XX
Neuromedin UNMU1RNeuromedin U receptor 1 (NMU1)X XX
Neuropeptide B & WNPBWR1Neuropeptides B/W receptor 1 (NPBW1)XX  
Neuropeptide B & WNPBWR2Neuropeptides B/W receptor 2 (NPBW2)XX  
Neuropeptide FF & AFNPFFR1Neuropeptide FF receptor 1 (NPFF1)XX  
Neuropeptide SNPSR1bneuropeptide S receptor 1 (NPS receptor)X   
Neuropeptide YNPY1RNeuropeptide Y receptor Y1 (Y1)X   
Neuropeptide YNPY2RNeuropeptide Y receptor Y2 (Y2)XXXX
Neuropeptide YmPPYR1Pancreatic polypeptide receptor 1 (Y4)X   
Neuropeptide YmNPY1RNeuropeptide Y1 receptor (Y1)X   
Neuropeptide YmNPY2RNeuropeptide Y2 receptor (NPY2R)X   
Neuropeptide YPPYR1Pancreatic polypeptide receptor 1 (Y4)XX  
NeurotensinNTSR1Neurotensin receptor 1 (NTS1)X XX
OpioidOPRD1Opioid receptor delta (δ)XX X
OpioidOPRK1Opioid receptor kappa (κ)XX X
OpioidOPRL1Opioid receptor-like receptor (NOP)XX X
OpioidOPRM1Opioid receptor mu (μ)XX X
OpioidmOPRD1Opioid receptor delta (δ (murine))X   
OpioidmOPRK1Opioid receptor kappa (κ (murine))X   
OpioidmOPRM1Opioid receptor mu (μ (murine))X   
OpioidrOPRM1Opioid receptor mu (μ)X   
OrexinHCRTR1Orexin receptor 1 (OX1)X XX
OrexinHCRTR2Orexin receptor 2 (OX2)X XX
Other 7TM proteinsGPR107G-protein coupled receptor 107 (GPR107)X   
Other 7TM proteinsGPR137G-protein coupled receptor 137B (TM7SF1)X   
Other 7TM proteinsGPR143G-protein coupled receptor 143 (GPR143)X   
P2YmP2RY12P2Y Purinoceptor 12 (mP2Y12)X   
P2YmP2RY6P2Y Purinoceptor 6 (P2Y6)X   
P2YP2RY1Purinergic receptor P2Y, G-protein coupled, 1 (P2RY1)X XX
P2YP2RY11Purinergic receptor P2Y, G-protein coupled, 11 (P2Y11)X   
P2YP2RY12Purinergic receptor P2Y, G-protein coupled, 12 (P2Y12)X  X
P2YP2RY2Purinergic receptor P2Y, G-protein coupled, 2 (P2Y2)X XX
P2YP2RY4Pyrimidinergic receptor P2Y, G-protein coupled, 4 (P2Y4)X  X
P2YP2RY6Pyrimidinergic receptor P2Y, G-protein coupled, 6 (P2Y6)X   
Parathyroid hormonePTHR1Parathyroid hormone receptor 1 (PTH1)XXXX
Parathyroid hormonePTHR2Parathyroid hormone receptor 2 (PTH2)XXXX
Peptide P518GPR103pyroglutamylated RFamide peptide receptor (QRFPR)X X 
Platelet-activating factorPTAFRPlatelet activating receptor (PAF)X XX
Platelet-activating factor mPTAFRPlatelet-activating factor receptor (mPAF)X   
ProkineticinPROKR1Prokineticin receptor 1 (PKR1)XXXX
ProkineticinPROKR2Prokineticin receptor 2 (PKR2)X  X
ProkineticinrPROKR1Prokineticin receptor 1 (rPROKR1)X   
ProkineticinrPROKR2Prokineticin receptor 2 (rPKR2)X   
Prolactin releasing peptide receptorPRLHRProlactin releasing hormone receptor (PRRP)X XX
ProstanoidrCRTH2Prostanoid DP2 receptor (rGPR44)X   
ProstanoidrPTGER4Prostaglandin E receptor 4 (subtype EP4), rat (rEP4)X   
ProstanoidTBXA2RThromboxane A2 receptor (TP)X XX
ProstanoidmPTGER4Prostaglandin E receptor 4 (subtype EP4) (EP4)X   
ProstanoidPTGDRProstaglandin D2 receptor (DP1) X  
ProstanoidPTGER1Prostaglandin E receptor 1 (subtype EP1) (EP1)X X 
ProstanoidPTGER2Prostaglandin E receptor 2 (subtype EP2) (EP2)XX  
ProstanoidPTGER3Prostaglandin E receptor 3 (subtype EP3) (EP3)XXX 
ProstanoidPTGER4Prostaglandin E receptor 4 (subtype EP4) (EP4)X  X
ProstanoidPTGFRProstaglandin F receptor (FP) (FP)X XX
ProstanoidPTGIRProstaglandin I2 (prostacyclin) receptor (IP) (IP1)XX X
ProstanoidmCRTH2Prostanoid DP2 receptor (mDP2)X   
ProstanoidCRTH2prostaglandin D2 receptor 2 (PTGDR2)XX  
Protease activatedF2RCoagulation factor II (thrombin) receptor (PAR1)X   
Protease activatedF2RL1Coagulation factor II (thrombin) receptor-like 1 (PAR2) (PAR2)X XX
Protease activatedF2RL3Coagulation factor II (thrombin) receptor-like 3 (PAR4) (PAR4)X XX
RelaxinmRXFP3Relaxin family peptide receptor 3 (RXFP3)X   
RelaxinmRXFP4Relaxin family peptide receptor 4 (RXFP4)X   
RelaxinRXFP1Relaxin family peptide receptor 1 (RXFP1) X  
RelaxinRXFP2Relaxin family peptide receptor 2 (RXFP2) X  
RelaxinRXFP3Relaxin family peptide receptor 3 (RXFP3)XX X
RelaxinRXFP4Relaxin family peptide receptor 4 (RXFP4)XX  
SomatostatinSSTR1Somatostatin receptor 1 (SST1)X   
SomatostatinSSTR2Somatostatin receptor 2 (SST2)XX X
SomatostatinSSTR3Somatostatin receptor 3 (SST3)XX  
SomatostatinSSTR4Somatostatin receptor 4 (SST4)XX  
SomatostatinSSTR5Somatostatin receptor 5 (SST5)XX  
SomatostatinmSSTR2Somatostatin receptor 2 (mSST2)X   
SomatostatinmSSTR5Somatostatin receptor 5 (mSRIF1B)X   
TachykininTACR1Tachykinin receptor 1 (NK1)X XX
TachykininTACR2Tachykinin receptor 2 (NK2)X XX
TachykininTACR3Tachykinin receptor 3 (NK3)XXXX
Thyrotropin releasing hormoneTRHRThyrotropin-releasing hormone receptor (TRH1)X XX
Trace amineTAAR1trace amine associated receptor 1 (TA1) X  
UrotensinUTR2Urotensin II receptor (UT)X XX
UrotensinmUTR2Urotensin II receptor (mUT)X   
Vasopressin and OxytocinOXTROxytocin Receptor (OT)X XX
Vasopressin and OxytocinmOXTROxytocin recepter (OT)X   
Vasopressin and OxytocinAVPR1AVasopressin receptor 1A (V1A)X XX
Vasopressin and OxytocinAVPR1BVasopressin receptor 1B (V1B)X XX
Vasopressin and OxytocinAVPR2Vasopressin receptor 2 (V2)XX X
VIP and PACAPADCYAP1R1Adenylate cyclase activating polypeptide receptor 1 (PAC1)XXXX
VIP and PACAPmVIPR1Vasoactive intestinal peptide receptor 1 (mVPAC1)X   
VIP and PACAPmADCYAP1R1Adenylate Cyclase Activating Polypeptide 1 Receptor 1 (mPAC1)X   
VIP and PACAPVIPR1Vasoactive intestinal peptide receptor 1 (VPAC1)XXXX
VIP and PACAPVIPR2Vasoactive intestinal peptide receptor 2 (VPAC2)XXXX
VIP and PACAPrVIPR1Vasoactive intestinal peptide receptor 1 (rVPAC1)X   

High Quality Starting Point From Library Profiling

In contrast to the traditional and largely linear GPCR discovery model in which one GPCR target is assessed at a time, GPCRscan affords the unprecedented ability to comprehensively annotate entire compound collections against a large number of GPCRs.  This highly parallel approach enables organizations to identify multiple targets of interest, defined by target biology, for which high quality lead like compounds exist and to focus resources on those programs most likely to succeed.

Screening of large Compound Libraries Against Entire gpcrMAX Panel

In contrast to the traditional and largely linear GPCR discovery model in which one GPCR target is assessed at a time, GPCRscan affords the unprecedented ability to comprehensively annotate entire compound collections against a large number of GPCRs.  This highly parallel approach enables organizations to identify multiple targets of interest, defined by target biology, for which high quality lead like compounds exist and to focus resources on those programs most likely to succeed.

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

Platform Benefits

  • Screen compound libraries against any GPCRscan assay panel or single target in our portfolio
  • Reveal opportunities and leverage the value inherent in your GPCR-focused compound collections
  • Make decisions on programs most likely to succeed with existing chemistry
  • Reduce time to clinical candidate and with high quality starting points
  • Rapidly respond to novel biological targets
 

Arrestin

2nd Messenger

Internalization

  
 
How it Works
How it Works
How it Works