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gpcrPANELS - Therapeutic Disease Panels

LeadHunter Discovery Services offers a number of focused therapeutic area assay panels that may be used to broadly screen for new leads or profile compounds of interest. These panels are organized based on current scientific understanding and are updated regularly.

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gpcrPANELS Assay Panel

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

 

Auditory and Otology Panel

Target GeneCommon NameFamily ▲
HTR1A5HT1A5-Hydroxytryptamine
HTR2A5HT2A5-Hydroxytryptamine
HTR2C5HT2C5-Hydroxytryptamine
CHRM1M1Acetylcholine
CHRM2M2Acetylcholine
CHRM3M3Acetylcholine
CHRM5M5Acetylcholine
ADORA3A3Adenosine
ADRB2β2-adrenoreceptorAdrenoceptors
GRPRBB2Bombesin
BDKRB2B2Bradykinin
CALCRL-RAMP1Calcitonin receptor-like receptorCalcitonin
CNR1CB1Cannabinoid
CNR2CB2Cannabinoid
CX3CR1CX3CR1Chemokine
CXCR2CXCR2Chemokine
CXCR4CXCR4Chemokine
CCR2CCR2Chemokine
CCR3CCR3Chemokine
CCR5CCR5Chemokine
CCKARCCK1Cholecystokinin
CCKBRCCK2Cholecystokinin
GALR1GALR1Galanin
HRH1H1Histamine
HRH3H3Histamine
EDG1S1P1Lysophospholipid (S1P)
EDG3S1P3Lysophospholipid (S1P)
EDG5S1P2Lysophospholipid (S1P)
NPBWR1NPBW1Neuropeptide B & W
NTSR1NTS1Neurotensin
OPRD1δOpioid
OPRK1κOpioid
OPRL1NOPOpioid
OPRM1μOpioid
HCRTR1OX1Orexin
PTHR2PTH2Parathyroid hormone
PTAFRPAFPlatelet-activating factor
PROKR2PKR2Prokineticin
PRLHRPRRPProlactin releasing peptide receptor
PTGER2EP2Prostanoid
PTGER3EP3Prostanoid
PTGER4EP4Prostanoid
PTGFRFPProstanoid
PTGIRIP1Prostanoid
F2RPAR1Protease activated
F2RL1PAR2Protease activated
TACR1NK1Tachykinin
TACR2NK2Tachykinin
TACR3NK3Tachykinin
ADCYAP1R1PAC1VIP and PACAP
+

Cancer Panel

Target GeneCommon NameFamily ▲
CHRM1M1Acetylcholine
CHRM2M2Acetylcholine
CHRM3M3Acetylcholine
CHRM4M4Acetylcholine
ADORA3A3Adenosine
ADRB1β1-adrenoreceptorAdrenoceptors
ADRB2β2-adrenoreceptorAdrenoceptors
AGTR1AT1Angiotensin
GRPRBB2Bombesin
BDKRB1B1Bradykinin
BDKRB2B2Bradykinin
CALCRCTCalcitonin
CNR1CB1Cannabinoid
CNR2CB2Cannabinoid
CX3CR1CX3CR1Chemokine
CXCR2CXCR2Chemokine
CXCR3CXCR3Chemokine
CXCR4CXCR4Chemokine
CXCR6CXCR6Chemokine
CXCR7CXCR7Chemokine
CCR10CCR10Chemokine
CCR2CCR2Chemokine
CCR5CCR5Chemokine
CCR6CCR6Chemokine
CCR7CCR7Chemokine
CCKARCCK1Cholecystokinin
CCKBRCCK2Cholecystokinin
GPR119GPR119Class A Orphan
EDNRAETAEndothelin
EDNRBETBEndothelin
FPR1FPR1Formylpeptide
GHSRghrelinGhrelin
FSHRFSHRGlycoprotein hormone receptor
LHCGRLHGlycoprotein hormone receptor
TSHR(L)TSHGlycoprotein hormone receptor
HRH1H1Histamine
HRH2H2Histamine
HRH3H3Histamine
HRH4H4Histamine
KISS1RkisspeptinKisspeptin receptor
LTB4RBLT1Leukotriene
EDG4LPA2Lysophospholipid (LPA)
EDG7LPA3Lysophospholipid (LPA)
EDG5S1P2Lysophospholipid (S1P)
EDG6S1P4Lysophospholipid (S1P)
EDG1S1P1Lysophospholipid (S1P)
EDG3S1P3Lysophospholipid (S1P)
MCHR1MCH1Melanin-concentrating hormone
MC1RMC1Melanocortin
MC3RMC3Melanocortin
MTNR1AMT1Melatonin
NPY2RY2Neuropeptide Y
PPYR1Y4Neuropeptide Y
NTSR1NTS1Neurotensin
HCRTR1OX1Orexin
HCRTR2OX2Orexin
P2RY1P2RY1P2Y
P2RY11P2Y11P2Y
P2RY6P2Y6P2Y
PTHR1PTH1Parathyroid hormone
PTHR2PTH2Parathyroid hormone
PTAFRPAFPlatelet-activating factor
PTGER2EP2Prostanoid
PTGER3EP3Prostanoid
PTGER4EP4Prostanoid
PTGFRFPProstanoid
PTGIRIP1Prostanoid
F2RPAR1Protease activated
F2RL1PAR2Protease activated
F2RL3PAR4Protease activated
SSTR2SST2Somatostatin
SSTR3SST3Somatostatin
SSTR5SST5Somatostatin
TACR1NK1Tachykinin
TACR2NK2Tachykinin
OXTROTVasopressin and Oxytocin
AVPR1AV1AVasopressin and Oxytocin
AVPR1BV1BVasopressin and Oxytocin
AVPR2V2Vasopressin and Oxytocin
ADCYAP1R1PAC1VIP and PACAP
VIPR1VPAC1VIP and PACAP
VIPR2VPAC2VIP and PACAP
+

Cardiovascular Panel

Target GeneCommon NameFamily ▲
HTR1B5HT1B5-Hydroxytryptamine
HTR2A5HT2A5-Hydroxytryptamine
CHRM1M1Acetylcholine
CHRM2M2Acetylcholine
CHRM3M3Acetylcholine
ADORA3A3Adenosine
ADRA1Bα1B-adrenoceptorAdrenoceptors
ADRA2Aα2A-adrenoceptorAdrenoceptors
ADRA2Bα2B-adrenoceptorAdrenoceptors
ADRB1β1-adrenoreceptorAdrenoceptors
ADRB2β2-adrenoreceptorAdrenoceptors
AGTR1AT1Angiotensin
BRS3BB3Bombesin
BDKRB1B1Bradykinin
BDKRB2B2Bradykinin
CALCRL-RAMP1Calcitonin receptor-like receptorCalcitonin
CALCRL-RAMP2Calcitonin receptor-like receptorCalcitonin
CALCRL-RAMP3Calcitonin receptor-like receptorCalcitonin
CCR2CCR2Chemokine
CCR3CCR3Chemokine
CCR5CCR5Chemokine
CX3CR1CX3CR1Chemokine
CXCR2CXCR2Chemokine
CXCR3CXCR3Chemokine
C3AR1C3AComplement peptide
DRD1D1Dopamine
DRD5D5Dopamine
EDNRAETAEndothelin
EDNRBETBEndothelin
FPRL1FPR2/ALXFormylpeptide
GLP1RGLP-1Glucagon
TSHR(L)TSHGlycoprotein hormone receptor
GPR109AHCA2Hydroxycarboxylic acid
EDG7LPA3Lysophospholipid (LPA)
EDG1S1P1Lysophospholipid (S1P)
EDG3S1P3Lysophospholipid (S1P)
EDG5S1P2Lysophospholipid (S1P)
MTNR1AMT1Melatonin
NPY1RY1Neuropeptide Y
NPY2RY2Neuropeptide Y
PPYR1Y4Neuropeptide Y
OPRD1δOpioid
OPRL1NOPOpioid
HCRTR1OX1Orexin
P2RY1P2RY1P2Y
PTHR1PTH1Parathyroid hormone
PTAFRPAFPlatelet-activating factor
PRLHRPRRPProlactin releasing peptide receptor
PTGER2EP2Prostanoid
PTGER3EP3Prostanoid
PTGER4EP4Prostanoid
PTGFRFPProstanoid
PTGIRIP1Prostanoid
TBXA2RTPProstanoid
F2RPAR1Protease activated
F2RL1PAR2Protease activated
F2RL3PAR4Protease activated
SSTR2SST2Somatostatin
TRHRTRH1Thyrotropin releasing hormone
UTR2UTUrotensin
OXTROTVasopressin and Oxytocin
AVPR1AV1AVasopressin and Oxytocin
AVPR2V2Vasopressin and Oxytocin
ADCYAP1R1PAC1VIP and PACAP
VIPR1VPAC1VIP and PACAP
VIPR2VPAC2VIP and PACAP
+

Chemokine Panel

Target GeneCommon NameFamily ▲
CMKLR1CMKLR1Chemerin
CX3CR1CX3CR1Chemokine
CXCR1CXCR1Chemokine
CXCR2CXCR2Chemokine
CXCR3CXCR3Chemokine
CXCR4CXCR4Chemokine
CXCR5CXCR5Chemokine
CXCR6CXCR6Chemokine
CXCR7CXCR7Chemokine
CCR1CCR1Chemokine
CCR10CCR10Chemokine
CCR2CCR2Chemokine
CCR3CCR3Chemokine
CCR4CCR4Chemokine
CCR5CCR5Chemokine
CCR6CCR6Chemokine
CCR7CCR7Chemokine
CCR8CCR8Chemokine
CCR9CCR9Chemokine
+

Dermatology Panel

Target GeneCommon NameFamily ▲
HTR2A5HT2A5-Hydroxytryptamine
CHRM2M2Acetylcholine
CHRM4M4Acetylcholine
ADORA3A3Adenosine
ADRA2Bα2B-adrenoceptorAdrenoceptors
GRPRBB2Bombesin
CALCRL-RAMP1Calcitonin receptor-like receptorCalcitonin
CNR1CB1Cannabinoid
CNR2CB2Cannabinoid
CMKLR1CMKLR1Chemerin
CX3CR1CX3CR1Chemokine
CXCR1CXCR1Chemokine
CXCR2CXCR2Chemokine
CXCR3CXCR3Chemokine
CXCR4CXCR4Chemokine
CXCR6CXCR6Chemokine
CXCR7CXCR7Chemokine
CCR10CCR10Chemokine
CCR2CCR2Chemokine
CCR3CCR3Chemokine
CCR4CCR4Chemokine
CCR5CCR5Chemokine
CCR6CCR6Chemokine
CCR7CCR7Chemokine
CCR8CCR8Chemokine
CCR9CCR9Chemokine
GPR119GPR119Class A Orphan
C5AR1C5AComplement peptide
EDNRBETBEndothelin
FPR1FPR1Formylpeptide
FPRL1FPR2/ALXFormylpeptide
FFAR1FFA1Free Fatty Acid
HRH1H1Histamine
HRH2H2Histamine
GPR109AHCA2Hydroxycarboxylic acid
LTB4RBLT1Leukotriene
EDG1S1P1Lysophospholipid (S1P)
EDG5S1P2Lysophospholipid (S1P)
EDG6S1P4Lysophospholipid (S1P)
MCHR1MCH1Melanin-concentrating hormone
MC1RMC1Melanocortin
NMU1RNMU1Neuromedin U
NTSR1NTS1Neurotensin
OPRD1δOpioid
OPRK1κOpioid
OPRM1μOpioid
PTAFRPAFPlatelet-activating factor
PROKR1PKR1Prokineticin
PTGER2EP2Prostanoid
PTGER3EP3Prostanoid
PTGER4EP4Prostanoid
PTGFRFPProstanoid
PTGIRIP1Prostanoid
F2RPAR1Protease activated
F2RL1PAR2Protease activated
F2RL3PAR4Protease activated
TACR1NK1Tachykinin
VIPR1VPAC1VIP and PACAP
VIPR2VPAC2VIP and PACAP
ADCYAP1R1PAC1VIP and PACAP
+

Digestive & Renal Panel

Target GeneCommon NameFamily ▲
CHRM2M2Acetylcholine
CHRM3M3Acetylcholine
CHRM4M4Acetylcholine
CHRM5M5Acetylcholine
ADRB2β2-adrenoreceptorAdrenoceptors
AGTR1AT1Angiotensin
GRPRBB2Bombesin
BDKRB1B1Bradykinin
BDKRB2B2Bradykinin
CALCRL-RAMP1Calcitonin receptor-like receptorCalcitonin
CNR2CB2Cannabinoid
CCR2CCR2Chemokine
CCR3CCR3Chemokine
CCR6CCR6Chemokine
CCR9CCR9Chemokine
CCKARCCK1Cholecystokinin
CCKBRCCK2Cholecystokinin
CRHR1CRF1Corticotropin-releasing factor
EDNRAETAEndothelin
EDNRBETBEndothelin
GLP1RGLP-1Glucagon
GLP2RGLP-2Glucagon
SCTRsecretinGlucagon
TSHR(L)TSHGlycoprotein hormone receptor
HRH2H2Histamine
GPR109AHCA2Hydroxycarboxylic acid
MC3RMC3Melanocortin
MC5RMC5Melanocortin
MLNRmotilinMotilin
NMU1RNMU1Neuromedin U
NPY2RY2Neuropeptide Y
NTSR1NTS1Neurotensin
OPRD1δOpioid
OPRK1κOpioid
OPRL1NOPOpioid
OPRM1μOpioid
HCRTR1OX1Orexin
P2RY1P2RY1P2Y
PTHR2PTH2Parathyroid hormone
PROKR1PKR1Prokineticin
PROKR2PKR2Prokineticin
PRLHRPRRPProlactin releasing peptide receptor
PTGER2EP2Prostanoid
PTGER3EP3Prostanoid
PTGER4EP4Prostanoid
F2RPAR1Protease activated
F2RL1PAR2Protease activated
F2RL3PAR4Protease activated
SSTR2SST2Somatostatin
TACR1NK1Tachykinin
TACR2NK2Tachykinin
TACR3NK3Tachykinin
TRHRTRH1Thyrotropin releasing hormone
AVPR1AV1AVasopressin and Oxytocin
AVPR2V2Vasopressin and Oxytocin
ADCYAP1R1PAC1VIP and PACAP
VIPR1VPAC1VIP and PACAP
VIPR2VPAC2VIP and PACAP
+

Inflammation Panel

Target GeneCommon NameFamily ▲
HTR2A5HT2A5-Hydroxytryptamine
CHRM2M2Acetylcholine
CHRM3M3Acetylcholine
CHRM4M4Acetylcholine
ADORA3A3Adenosine
ADRA2Aα2A-adrenoceptorAdrenoceptors
ADRA2Cα2C-adrenoceptorAdrenoceptors
ADRB2β2-adrenoreceptorAdrenoceptors
BRS3BB3Bombesin
GRPRBB2Bombesin
BDKRB1B1Bradykinin
BDKRB2B2Bradykinin
CALCRCTCalcitonin
CALCRL-RAMP1Calcitonin receptor-like receptorCalcitonin
CNR1CB1Cannabinoid
CNR2CB2Cannabinoid
CMKLR1CMKLR1Chemerin
CX3CR1CX3CR1Chemokine
CXCR1CXCR1Chemokine
CXCR2CXCR2Chemokine
CXCR3CXCR3Chemokine
CXCR4CXCR4Chemokine
CXCR6CXCR6Chemokine
CXCR7CXCR7Chemokine
CCR10CCR10Chemokine
CCR2CCR2Chemokine
CCR3CCR3Chemokine
CCR4CCR4Chemokine
CCR5CCR5Chemokine
CCR6CCR6Chemokine
CCR7CCR7Chemokine
CCR8CCR8Chemokine
CCR9CCR9Chemokine
CCKARCCK1Cholecystokinin
CCKBRCCK2Cholecystokinin
C3AR1C3AComplement peptide
C5AR1C5AComplement peptide
C5L2C5L2Complement peptide
CRHR1CRF1Corticotropin-releasing factor
CRHR2CRF2Corticotropin-releasing factor
DRD1D1Dopamine
DRD2LD2LDopamine
EDNRAETAEndothelin
EDNRBETBEndothelin
FPR1FPR1Formylpeptide
FPRL1FPR2/ALXFormylpeptide
FFAR1FFA1Free Fatty Acid
GPR120FFA4Free fatty acid
GLP1RGLP-1Glucagon
GLP2RGLP-2Glucagon
HRH1H1Histamine
HRH2H2Histamine
HRH3H3Histamine
HRH4H4Histamine
GPR109AHCA2Hydroxycarboxylic acid
LTB4RBLT1Leukotriene
EDG4LPA2Lysophospholipid (LPA)
EDG7LPA3Lysophospholipid (LPA)
EDG5S1P2Lysophospholipid (S1P)
EDG6S1P4Lysophospholipid (S1P)
EDG1S1P1Lysophospholipid (S1P)
EDG3S1P3Lysophospholipid (S1P)
MC1RMC1Melanocortin
MC3RMC3Melanocortin
MC4RMC4Melanocortin
MC5RMC5Melanocortin
MTNR1AMT1Melatonin
NMU1RNMU1Neuromedin U
NTSR1NTS1Neurotensin
OPRD1δOpioid
OPRK1κOpioid
OPRM1μOpioid
P2RY11P2Y11P2Y
P2RY12P2Y12P2Y
P2RY2P2Y2P2Y
P2RY4P2Y4P2Y
P2RY6P2Y6P2Y
PTHR1PTH1Parathyroid hormone
PTHR2PTH2Parathyroid hormone
PTAFRPAFPlatelet-activating factor
PROKR1PKR1Prokineticin
PROKR2PKR2Prokineticin
PTGER2EP2Prostanoid
PTGER3EP3Prostanoid
PTGER4EP4Prostanoid
PTGFRFPProstanoid
PTGIRIP1Prostanoid
TBXA2RTPProstanoid
F2RPAR1Protease activated
F2RL1PAR2Protease activated
F2RL3PAR4Protease activated
SSTR1SST1Somatostatin
SSTR2SST2Somatostatin
SSTR3SST3Somatostatin
SSTR5SST5Somatostatin
TACR1NK1Tachykinin
TACR2NK2Tachykinin
TACR3NK3Tachykinin
VIPR1VPAC1VIP and PACAP
VIPR2VPAC2VIP and PACAP
ADCYAP1R1PAC1VIP and PACAP
+

Metabolic Panel

Target GeneCommon NameFamily ▲
HTR1B5HT1B5-Hydroxytryptamine
HTR2C5HT2C5-Hydroxytryptamine
CHRM1M1Acetylcholine
CHRM2M2Acetylcholine
CHRM3M3Acetylcholine
ADRA1Bα1B-adrenoceptorAdrenoceptors
ADRA2Aα2A-adrenoceptorAdrenoceptors
AGTR1AT1Angiotensin
BRS3BB3Bombesin
GRPRBB2Bombesin
BDKRB1B1Bradykinin
BDKRB2B2Bradykinin
CALCRCTCalcitonin
CALCRL-RAMP1Calcitonin receptor-like receptorCalcitonin
CNR1CB1Cannabinoid
CNR2CB2Cannabinoid
CCR2CCR2Chemokine
CCR4CCR4Chemokine
CXCR3CXCR3Chemokine
CCKARCCK1Cholecystokinin
C3AR1C3AComplement peptide
CRHR2CRF2Corticotropin-releasing factor
DRD3D3Dopamine
FFAR1FFA1Free Fatty Acid
GALR2GALR2Galanin
GCGRglucagonGlucagon
GLP1RGLP-1Glucagon
SCTRsecretinGlucagon
TSHR(L)TSHGlycoprotein hormone receptor
HRH1H1Histamine
HRH3H3Histamine
HRH4H4Histamine
GPR109AHCA2Hydroxycarboxylic acid
MCHR1MCH1Melanin-concentrating hormone
MC1RMC1Melanocortin
MC3RMC3Melanocortin
MC4RMC4Melanocortin
MC5RMC5Melanocortin
MTNR1AMT1Melatonin
NPBWR1NPBW1Neuropeptide B & W
NPY1RY1Neuropeptide Y
NPY2RY2Neuropeptide Y
PPYR1Y4Neuropeptide Y
NTSR1NTS1Neurotensin
OPRK1κOpioid
OPRL1NOPOpioid
OPRM1μOpioid
HCRTR1OX1Orexin
HCRTR2OX2Orexin
PTHR1PTH1Parathyroid hormone
PTHR2PTH2Parathyroid hormone
GPR103QRFPRPeptide P518
PROKR2PKR2Prokineticin
PRLHRPRRPProlactin releasing peptide receptor
PTGER2EP2Prostanoid
PTGER4EP4Prostanoid
TBXA2RTPProstanoid
SSTR2SST2Somatostatin
SSTR5SST5Somatostatin
UTR2UTUrotensin
OXTROTVasopressin and Oxytocin
AVPR1AV1AVasopressin and Oxytocin
ADCYAP1R1PAC1VIP and PACAP
VIPR2VPAC2VIP and PACAP
+

Neurological Panel

Target GeneCommon NameFamily ▲
HTR1A5HT1A5-Hydroxytryptamine
HTR1B5HT1B5-Hydroxytryptamine
HTR1F5HT1F5-Hydroxytryptamine
HTR2A5HT2A5-Hydroxytryptamine
HTR2C5HT2C5-Hydroxytryptamine
HTR5A5HT5A5-Hydroxytryptamine
HTR1E5HT1E5-Hydroxytryptamine
CHRM1M1Acetylcholine
CHRM2M2Acetylcholine
CHRM3M3Acetylcholine
CHRM4M4Acetylcholine
CHRM5M5Acetylcholine
ADORA3A3Adenosine
ADRA1Bα1B-adrenoceptorAdrenoceptors
ADRA2Aα2A-adrenoceptorAdrenoceptors
ADRA2Bα2B-adrenoceptorAdrenoceptors
ADRA2Cα2C-adrenoceptorAdrenoceptors
ADRB2β2-adrenoreceptorAdrenoceptors
AGTR1AT1Angiotensin
BRS3BB3Bombesin
GRPRBB2Bombesin
BDKRB1B1Bradykinin
BDKRB2B2Bradykinin
CALCRL-RAMP1Calcitonin receptor-like receptorCalcitonin
CNR1CB1Cannabinoid
CNR2CB2Cannabinoid
CX3CR1CX3CR1Chemokine
CXCR2CXCR2Chemokine
CXCR3CXCR3Chemokine
CXCR4CXCR4Chemokine
CCR2CCR2Chemokine
CCR4CCR4Chemokine
CCR5CCR5Chemokine
CCKARCCK1Cholecystokinin
CCKBRCCK2Cholecystokinin
GPR119GPR119Class A Orphan
CRHR1CRF1Corticotropin-releasing factor
CRHR2CRF2Corticotropin-releasing factor
DRD1D1Dopamine
DRD2LD2LDopamine
DRD2SD2SDopamine
DRD3D3Dopamine
DRD4D4Dopamine
DRD5D5Dopamine
EDNRAETAEndothelin
EDNRBETBEndothelin
FPR1FPR1Formylpeptide
FPRL1FPR2/ALXFormylpeptide
FFAR1FFA1Free Fatty Acid
GALR1GALR1Galanin
GALR2GALR2Galanin
GHSRghrelinGhrelin
GLP1RGLP-1Glucagon
SCTRsecretinGlucagon
TSHR(L)TSHGlycoprotein hormone receptor
HRH1H1Histamine
HRH2H2Histamine
HRH3H3Histamine
GPR109AHCA2Hydroxycarboxylic acid
EDG7LPA3Lysophospholipid (LPA)
EDG1S1P1Lysophospholipid (S1P)
EDG3S1P3Lysophospholipid (S1P)
EDG5S1P2Lysophospholipid (S1P)
MCHR1MCH1Melanin-concentrating hormone
MC3RMC3Melanocortin
MC4RMC4Melanocortin
MTNR1AMT1Melatonin
MLNRmotilinMotilin
NPBWR1NPBW1Neuropeptide B & W
NPBWR2NPBW2Neuropeptide B & W
NPY1RY1Neuropeptide Y
NPY2RY2Neuropeptide Y
NTSR1NTS1Neurotensin
OPRD1δOpioid
OPRK1κOpioid
OPRL1NOPOpioid
OPRM1μOpioid
HCRTR1OX1Orexin
HCRTR2OX2Orexin
P2RY1P2RY1P2Y
PTAFRPAFPlatelet-activating factor
PRLHRPRRPProlactin releasing peptide receptor
PTGER2EP2Prostanoid
PTGER3EP3Prostanoid
PTGER4EP4Prostanoid
PTGIRIP1Prostanoid
SSTR1SST1Somatostatin
SSTR2SST2Somatostatin
SSTR5SST5Somatostatin
TACR1NK1Tachykinin
TACR2NK2Tachykinin
TACR3NK3Tachykinin
TRHRTRH1Thyrotropin releasing hormone
AVPR1AV1AVasopressin and Oxytocin
AVPR1BV1BVasopressin and Oxytocin
ADCYAP1R1PAC1VIP and PACAP
VIPR1VPAC1VIP and PACAP
VIPR2VPAC2VIP and PACAP
+

Ocular Panel

Target GeneCommon NameFamily ▲
HTR1A5HT1A5-Hydroxytryptamine
HTR1B5HT1B5-Hydroxytryptamine
HTR1F5HT1F5-Hydroxytryptamine
HTR2A5HT2A5-Hydroxytryptamine
HTR2C5HT2C5-Hydroxytryptamine
HTR5A5HT5A5-Hydroxytryptamine
HTR1E5HT1E5-Hydroxytryptamine
CHRM1M1Acetylcholine
CHRM2M2Acetylcholine
CHRM3M3Acetylcholine
CHRM4M4Acetylcholine
CHRM5M5Acetylcholine
ADORA3A3Adenosine
ADRA1Bα1B-adrenoceptorAdrenoceptors
ADRA2Aα2A-adrenoceptorAdrenoceptors
ADRA2Bα2B-adrenoceptorAdrenoceptors
ADRA2Cα2C-adrenoceptorAdrenoceptors
ADRB2β2-adrenoreceptorAdrenoceptors
AGTR1AT1Angiotensin
BRS3BB3Bombesin
GRPRBB2Bombesin
BDKRB1B1Bradykinin
BDKRB2B2Bradykinin
CALCRL-RAMP1Calcitonin receptor-like receptorCalcitonin
CNR1CB1Cannabinoid
CNR2CB2Cannabinoid
CX3CR1CX3CR1Chemokine
CXCR2CXCR2Chemokine
CXCR3CXCR3Chemokine
CXCR4CXCR4Chemokine
CCR2CCR2Chemokine
CCR4CCR4Chemokine
CCR5CCR5Chemokine
CCKARCCK1Cholecystokinin
CCKBRCCK2Cholecystokinin
GPR119GPR119Class A Orphan
CRHR1CRF1Corticotropin-releasing factor
CRHR2CRF2Corticotropin-releasing factor
DRD1D1Dopamine
DRD2LD2LDopamine
DRD2SD2SDopamine
DRD3D3Dopamine
DRD4D4Dopamine
DRD5D5Dopamine
EDNRAETAEndothelin
EDNRBETBEndothelin
FPR1FPR1Formylpeptide
FPRL1FPR2/ALXFormylpeptide
FFAR1FFA1Free Fatty Acid
GALR1GALR1Galanin
GALR2GALR2Galanin
GHSRghrelinGhrelin
GLP1RGLP-1Glucagon
SCTRsecretinGlucagon
TSHR(L)TSHGlycoprotein hormone receptor
HRH1H1Histamine
HRH2H2Histamine
HRH3H3Histamine
GPR109AHCA2Hydroxycarboxylic acid
EDG7LPA3Lysophospholipid (LPA)
EDG1S1P1Lysophospholipid (S1P)
EDG3S1P3Lysophospholipid (S1P)
EDG5S1P2Lysophospholipid (S1P)
MCHR1MCH1Melanin-concentrating hormone
MC3RMC3Melanocortin
MC4RMC4Melanocortin
MTNR1AMT1Melatonin
MLNRmotilinMotilin
NPBWR1NPBW1Neuropeptide B & W
NPBWR2NPBW2Neuropeptide B & W
NPY1RY1Neuropeptide Y
NPY2RY2Neuropeptide Y
NTSR1NTS1Neurotensin
OPRD1δOpioid
OPRK1κOpioid
OPRL1NOPOpioid
OPRM1μOpioid
HCRTR1OX1Orexin
HCRTR2OX2Orexin
P2RY1P2RY1P2Y
PTAFRPAFPlatelet-activating factor
PRLHRPRRPProlactin releasing peptide receptor
PTGER2EP2Prostanoid
PTGER3EP3Prostanoid
PTGER4EP4Prostanoid
PTGIRIP1Prostanoid
SSTR1SST1Somatostatin
SSTR2SST2Somatostatin
SSTR5SST5Somatostatin
TACR1NK1Tachykinin
TACR2NK2Tachykinin
TACR3NK3Tachykinin
TRHRTRH1Thyrotropin releasing hormone
AVPR1AV1AVasopressin and Oxytocin
AVPR1BV1BVasopressin and Oxytocin
ADCYAP1R1PAC1VIP and PACAP
VIPR1VPAC1VIP and PACAP
VIPR2VPAC2VIP and PACAP
+

Pain and Addiction Panel

Target GeneCommon NameFamily ▲
HTR1A5HT1A5-Hydroxytryptamine
HTR2A5HT2A5-Hydroxytryptamine
HTR2C5HT2C5-Hydroxytryptamine
CHRM1M1Acetylcholine
CHRM3M3Acetylcholine
CHRM4M4Acetylcholine
CHRM5M5Acetylcholine
ADORA3A3Adenosine
ADRA1Bα1B-adrenoceptorAdrenoceptors
ADRA2Aα2A-adrenoceptorAdrenoceptors
ADRA2Bα2B-adrenoceptorAdrenoceptors
ADRA2Cα2C-adrenoceptorAdrenoceptors
ADRB1β1-adrenoreceptorAdrenoceptors
ADRB2β2-adrenoreceptorAdrenoceptors
AGTRL1APJApelin
CNR1CB1Cannabinoid
CNR2CB2Cannabinoid
CX3CR1CX3CR1Chemokine
CXCR3CXCR3Chemokine
CXCR4CXCR4Chemokine
CCR2CCR2Chemokine
CCR5CCR5Chemokine
CCR7CCR7Chemokine
EDNRAETAEndothelin
EDNRBETBEndothelin
HRH1H1Histamine
HRH2H2Histamine
HRH3H3Histamine
HRH4H4Histamine
MC5RMC5Melanocortin
NMU1RNMU1Neuromedin U
PTGER2EP2Prostanoid
PTGER3EP3Prostanoid
PTGER4EP4Prostanoid
PTGFRFPProstanoid
PTGIRIP1Prostanoid
TBXA2RTPProstanoid
+

Post-Traumatic Stress Disorder Panel

Target GeneCommon NameFamily ▲
HTR1A5HT1A5-Hydroxytryptamine
HTR1B5HT1B5-Hydroxytryptamine
HTR1F5HT1F5-Hydroxytryptamine
HTR2A5HT2A5-Hydroxytryptamine
HTR2C5HT2C5-Hydroxytryptamine
HTR5A5HT5A5-Hydroxytryptamine
HTR1E5HT1E5-Hydroxytryptamine
CHRM1M1Acetylcholine
CHRM2M2Acetylcholine
CHRM3M3Acetylcholine
CHRM4M4Acetylcholine
CHRM5M5Acetylcholine
ADRA1Bα1B-adrenoceptorAdrenoceptors
ADRA2Aα2A-adrenoceptorAdrenoceptors
ADRA2Bα2B-adrenoceptorAdrenoceptors
ADRA2Cα2C-adrenoceptorAdrenoceptors
ADRB1β1-adrenoreceptorAdrenoceptors
ADRB2β2-adrenoreceptorAdrenoceptors
GRPRBB2Bombesin
CNR1CB1Cannabinoid
CCKARCCK1Cholecystokinin
CCKBRCCK2Cholecystokinin
CRHR1CRF1Corticotropin-releasing factor
CRHR2CRF2Corticotropin-releasing factor
DRD1D1Dopamine
DRD2LD2LDopamine
DRD2SD2SDopamine
DRD3D3Dopamine
DRD4D4Dopamine
HRH3H3Histamine
NPSR1bNPS receptorNeuropeptide S
NPY1RY1Neuropeptide Y
NPY2RY2Neuropeptide Y
PPYR1Y4Neuropeptide Y
NTSR1NTS1Neurotensin
OPRD1δOpioid
OPRK1κOpioid
OPRL1NOPOpioid
OPRM1μOpioid
F2RL3PAR4Protease activated
TACR1NK1Tachykinin
AVPR1AV1AVasopressin and Oxytocin
ADCYAP1R1PAC1VIP and PACAP
+

Reproduction Panel

Target GeneCommon NameFamily ▲
ADORA3A3Adenosine
AGTR1AT1Angiotensin
BRS3BB3Bombesin
BDKRB2B2Bradykinin
CCR10CCR10Chemokine
CCR7CCR7Chemokine
CXCR4CXCR4Chemokine
CRHR1CRF1Corticotropin-releasing factor
DRD2LD2LDopamine
DRD3D3Dopamine
EDNRAETAEndothelin
EDNRBETBEndothelin
FSHRFSHRGlycoprotein hormone receptor
LHCGRLHGlycoprotein hormone receptor
GPR109AHCA2Hydroxycarboxylic acid
KISS1RkisspeptinKisspeptin receptor
EDG1S1P1Lysophospholipid (S1P)
EDG5S1P2Lysophospholipid (S1P)
MTNR1AMT1Melatonin
NPBWR1NPBW1Neuropeptide B & W
PPYR1Y4Neuropeptide Y
OPRK1κOpioid
OPRM1μOpioid
PTHR1PTH1Parathyroid hormone
PROKR2PKR2Prokineticin
PRLHRPRRPProlactin releasing peptide receptor
PTGER2EP2Prostanoid
PTGER3EP3Prostanoid
PTGER4EP4Prostanoid
PTGFRFPProstanoid
TRHRTRH1Thyrotropin releasing hormone
OXTROTVasopressin and Oxytocin
VIPR1VPAC1VIP and PACAP
VIPR2VPAC2VIP and PACAP
ADCYAP1R1PAC1VIP and PACAP
+

Respiratory Panel

Target GeneCommon NameFamily ▲
HTR2A5HT2A5-Hydroxytryptamine
HTR2C5HT2C5-Hydroxytryptamine
CHRM1M1Acetylcholine
CHRM2M2Acetylcholine
CHRM3M3Acetylcholine
CHRM4M4Acetylcholine
ADORA3A3Adenosine
ADRB1β1-adrenoreceptorAdrenoceptors
ADRB2β2-adrenoreceptorAdrenoceptors
GRPRBB2Bombesin
BDKRB1B1Bradykinin
BDKRB2B2Bradykinin
CALCRL-RAMP1Calcitonin receptor-like receptorCalcitonin
CCR2CCR2Chemokine
CCR3CCR3Chemokine
CCR4CCR4Chemokine
CCR6CCR6Chemokine
CXCR1CXCR1Chemokine
CXCR2CXCR2Chemokine
CXCR3CXCR3Chemokine
CXCR4CXCR4Chemokine
CCKARCCK1Cholecystokinin
CCKBRCCK2Cholecystokinin
MRGPRX2MRGX2Class A Orphan
C3AR1C3AComplement peptide
C5AR1C5AComplement peptide
EDNRAETAEndothelin
EDNRBETBEndothelin
GLP1RGLP-1Glucagon
HRH1H1Histamine
HRH2H2Histamine
HRH3H3Histamine
HRH4H4Histamine
LTB4RBLT1Leukotriene
EDG7LPA3Lysophospholipid (LPA)
EDG1S1P1Lysophospholipid (S1P)
EDG3S1P3Lysophospholipid (S1P)
EDG6S1P4Lysophospholipid (S1P)
OPRD1δOpioid
OPRK1κOpioid
OPRM1μOpioid
P2RY1P2RY1P2Y
P2RY12P2Y12P2Y
P2RY2P2Y2P2Y
P2RY6P2Y6P2Y
PTAFRPAFPlatelet-activating factor
PTGER2EP2Prostanoid
PTGER3EP3Prostanoid
PTGER4EP4Prostanoid
PTGFRFPProstanoid
PTGIRIP1Prostanoid
TBXA2RTPProstanoid
F2RPAR1Protease activated
SSTR1SST1Somatostatin
SSTR2SST2Somatostatin
SSTR3SST3Somatostatin
SSTR5SST5Somatostatin
TACR1NK1Tachykinin
TACR2NK2Tachykinin
TACR3NK3Tachykinin
VIPR1VPAC1VIP and PACAP
VIPR2VPAC2VIP and PACAP
ADCYAP1R1PAC1VIP and PACAP
+

Chemokine Family Selectivity Panel

With the complete family of 20 functional, cell-based chemokine assays available and regularly scheduled test dates, our goal is to help you make more informed decisions about the therapeutic potential and off target liabilities of your compounds.
The complete family of PathHunter Arrestin Chemokine receptors were tested in agonist mode (1uM screening concenration) to screen for highly selective agonist compounds. The Arrestin panel was able to detect both full and partial agonist responses due to its broad dynamic range.
The PathHunter arrestin chemokine panel was were tested with 6 reference antagonists to generate a ligand profile for the chemokine family.  Three compounds (right panels) exhibited low specificity and inhibited a wide range of targets.  In contrast, BMSCCR2 22, AMD3100 and Miraviroc had significantly lower cross reactivity. Of note, the highly specific AMD3100 and Maraviroc  antagonists have previously gained FDA approval.

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 and Benefits

  • Pre-set GPCR panels organized by therapeutic relevance
  • Single, G-protein independent readout for reliable data comparison across all receptors
  • Agonist, antagonist, inverse agonist, allosteric modulator modes available
  • High quality reproducible data
  • Fast turn around times
  • Economically priced
How it Works