gpcrE/IC50ELECT Assay Panel
Listed below are the assays currently available for screening and profiling.
Family ▲ | Target Gene | Common Name | Arrestin | cAMP | Calcium | Internalization |
5-Hydroxytryptamine | HTR1A | 5HT1A | X | X | | |
5-Hydroxytryptamine | HTR1B | 5HT1B | X | X | | |
5-Hydroxytryptamine | HTR1F | 5HT1F | X | X | | |
5-Hydroxytryptamine | HTR2A | 5HT2A | X | | X | |
5-Hydroxytryptamine | HTR2C | 5HT2C | X | | X | X |
5-Hydroxytryptamine | HTR5A | 5HT5A | X | X | | |
5-Hydroxytryptamine | HTR1E | 5HT1E | X | | | |
Acetylcholine | CHRM1 | M1 | X | | X | X |
Acetylcholine | CHRM2 | M2 | X | X | | X |
Acetylcholine | CHRM3 | M3 | X | | X | X |
Acetylcholine | CHRM4 | M4 | X | X | | X |
Acetylcholine | CHRM5 | M5 | X | | X | X |
Adenosine | ADORA3 | A3 | X | X | | |
Adrenoceptors | ADRA1B | α1B-adrenoceptor | X | | X | |
Adrenoceptors | ADRA2A | α2A-adrenoceptor | X | X | | |
Adrenoceptors | ADRA2B | α2B-adrenoceptor | X | | | |
Adrenoceptors | ADRA2C | α2C-adrenoceptor | X | X | | X |
Adrenoceptors | ADRB1 | β1-adrenoreceptor | X | X | | |
Adrenoceptors | ADRB2 | β2-adrenoreceptor | X | X | | X |
Angiotensin | AGTR1 | AT1 | X | | X | |
Apelin | AGTRL1 | APJ | X | X | | X |
Bombesin | BRS3 | BB3 | X | | X | |
Bombesin | GRPR | BB2 | X | | X | X |
Bombesin | NMBR | BB1 | X | | X | X |
Bradykinin | BDKRB1 | B1 | X | | X | |
Bradykinin | BDKRB2 | B2 | X | | X | X |
Calcitonin | CALCR | CT | X | X | | |
Calcitonin | CALCRL-RAMP1 | Calcitonin receptor-like receptor | X | X | | |
Calcitonin | CALCRL-RAMP2 | Calcitonin receptor-like receptor | X | | | |
Calcitonin | CALCRL-RAMP3 | Calcitonin receptor-like receptor | X | X | | |
Calcitonin | CALCR-RAMP2 | CT | X | X | | |
Calcitonin | CALCR-RAMP3 | CT | X | X | | |
Cannabinoid | CNR1 | CB1 | X | X | | |
Cannabinoid | CNR2 | CB2 | X | X | | |
Chemerin | CMKLR1 | CMKLR1 | X | X | | X |
Chemokine | CCR1 | CCR1 | X | X | | X |
Chemokine | CCR10 | CCR10 | X | X | | X |
Chemokine | CCR2 | CCR2 | X | | | X |
Chemokine | CCR3 | CCR3 | X | | | |
Chemokine | CCR4 | CCR4 | X | | | X |
Chemokine | CCR5 | CCR5 | X | X | | X |
Chemokine | CCR6 | CCR6 | X | X | | X |
Chemokine | CCR7 | CCR7 | X | X | | X |
Chemokine | CCR8 | CCR8 | X | | | |
Chemokine | CCR9 | CCR9 | X | | | |
Chemokine | CCRL2 | CCRL2 | X | | | |
Chemokine | CX3CR1 | CX3CR1 | X | | | |
Chemokine | CXCR1 | CXCR1 | X | X | | X |
Chemokine | CXCR2 | CXCR2 | X | X | | X |
Chemokine | CXCR3 | CXCR3 | X | X | | X |
Chemokine | CXCR4 | CXCR4 | X | X | | X |
Chemokine | CXCR5 | CXCR5 | X | X | | |
Chemokine | CXCR6 | CXCR6 | X | | | |
Chemokine | CXCR7 | CXCR7 | X | | | X |
Chemokine | DARC | FY | X | | | |
Cholecystokinin | CCKAR | CCK1 | X | | X | X |
Cholecystokinin | CCKBR | CCK2 | X | | X | X |
Class A Orphan | EBI2 | GPR183 | X | X | | X |
Class A Orphan | GHSR1b | GHSR1b | X | | | |
Class A Orphan | GPR1 | GPR1 | X | | | X |
Class A Orphan | GPR101 | GPR101 | X | | | |
Class A Orphan | GPR119 | GPR119 | X | | | |
Class A Orphan | GPR12 | GPR12 | X | | | |
Class A Orphan | GPR132 | GPR132 | X | | | |
Class A Orphan | GPR135 | GPR135 | X | | | |
Class A Orphan | GPR139 | GPR139 | X | | | |
Class A Orphan | GPR141 | GPR141 | X | | | |
Class A Orphan | GPR142 | GPR142 | X | | | |
Class A Orphan | GPR146 | GPR146 | X | | | |
Class A Orphan | GPR148 | GPR148 | X | | | |
Class A Orphan | GPR149 | GPR149 | X | | | |
Class A Orphan | GPR15 | GPR15 | X | | | |
Class A Orphan | GPR150 | GPR150 | X | | | |
Class A Orphan | GPR151 | GPR151 | X | | | |
Class A Orphan | GPR152 | GPR152 | X | | | |
Class A Orphan | GPR161 | GPR161 | X | | | |
Class A Orphan | GPR162 | GPR162 | X | | | |
Class A Orphan | GPR17 | GPR17 | X | | X | |
Class A Orphan | GPR171 | GPR171 | X | | | |
Class A Orphan | GPR173 | GPR173 | X | | | |
Class A Orphan | GPR176 | GPR176 | X | | | |
Class A Orphan | GPR18 | GPR18 | X | | | |
Class A Orphan | GPR182 | GPR182 | X | | | |
Class A Orphan | GPR20 | GPR20 | X | | | |
Class A Orphan | GPR23 | LPA4 | X | | | |
Class A Orphan | GPR25 | GPR25 | X | | | |
Class A Orphan | GPR26 | GPR26 | X | | | |
Class A Orphan | GPR27 | GPR27 | X | | | |
Class A Orphan | GPR3 | GPR3 | X | | | |
Class A Orphan | GPR31 | GPR31 | X | | | |
Class A Orphan | GPR32 | GPR32 | X | | | |
Class A Orphan | GPR35 | GPR35 | X | X | | X |
Class A Orphan | GPR37 | EDNRBL | X | | | |
Class A Orphan | GPR37L1 | GPR37L1 | X | | | |
Class A Orphan | GPR39 | GPR39 | X | | X | |
Class A Orphan | GPR4 | GPR4 | X | | | |
Class A Orphan | GPR45 | GPR45 | X | | | |
Class A Orphan | GPR50 | GPR50 | X | | | |
Class A Orphan | GPR52 | GPR52 | X | | | |
Class A Orphan | GPR55 | GPR55 | X | | | |
Class A Orphan | GPR6 | GPR6 | X | | | |
Class A Orphan | GPR61 | GPR61 | X | | | |
Class A Orphan | GPR65 | GPR65 | X | | | |
Class A Orphan | GPR75 | GPR75 | X | | | |
Class A Orphan | GPR78 | GPR78 | X | | | |
Class A Orphan | GPR79 | GPR79 | X | | | |
Class A Orphan | GPR83 | GPR83 | X | | | |
Class A Orphan | GPR84 | GPR84 | X | X | | |
Class A Orphan | GPR85 | GPR85 | X | | | |
Class A Orphan | GPR88 | GPR88 | X | | | |
Class A Orphan | LGR4 | LGR4 | X | | | |
Class A Orphan | LGR5 | LGR5 | X | | | |
Class A Orphan | LGR6 | LGR6 | X | | | |
Class A Orphan | MRGPRD | MRGPRD | X | | | |
Class A Orphan | MRGPRE | MRGPRE | X | | | |
Class A Orphan | MRGPRF | MRGPRF | X | | | |
Class A Orphan | MRGPRX1 | MRGPRX1 | X | | X | |
Class A Orphan | MRGPRX2 | MRGX2 | X | | X | |
Class A Orphan | MRGPRX4 | MRGPRX4 | X | | | |
Class A Orphan | OPN5 | OPN5 | X | | | |
Class A Orphan | OXGR1 | OXGR1 | X | | X | |
Class A Orphan | P2RY8 | P2RY8 | X | | | |
Class A Orphan | TAAR5 | TAAR5 | X | | | |
Class A Orphan | GPR22 | GPR22 | X | | | |
Class B Orphan | BAI1 | BAI1 | X | | | |
Class B Orphan | BAI2 | BAI2 | X | | | |
Class B Orphan | BAI3 | BAI3 | X | | | |
Class B Orphan | GPR123 | GPR123 | X | | | |
Class B Orphan | GPR157 | GPR157 | X | | | |
Class B Orphan | GPR97 | GPR97 | X | | | |
Complement peptide | C5AR1 | C5A | X | X | | X |
Complement peptide | C5L2 | C5L2 | X | | | X |
Corticotropin-releasing factor | CRHR1 | CRF1 | X | X | | X |
Corticotropin-releasing factor | CRHR2 | CRF2 | X | X | | X |
Cytosolic tyrosine kinase | FGR | FGR | | | | |
Cytosolic tyrosine kinase | JAK3 | JAK3 | | | | |
Cytosolic Tyrosine Kinase | PRLR-JAK1 | PRLR | | | | |
Cytosolic Tyrosine Kinase | PRLR-JAK2 | PRLR | | | | |
Cytosolic tyrosine kinase | TYK2 | TYK2 | | | | |
Dopamine | DRD1 | D1 | X | X | | X |
Dopamine | DRD2L | D2L | X | X | | |
Dopamine | DRD2S | D2S | X | X | | |
Dopamine | DRD3 | D3 | X | | | |
Dopamine | DRD4 | D4 | X | X | | |
Dopamine | DRD5 | D5 | X | X | | |
Endothelin | EDNRA | ETA | X | | X | |
Endothelin | EDNRB | ETB | X | | | X |
Estrogen (G protein coupled) receptor | GPR30 | GPER | X | | | |
Formylpeptide | FPR1 | FPR1 | X | X | | X |
Formylpeptide | FPRL1 | FPR2/ALX | X | X | | X |
Free Fatty Acid | FFAR1 | FFA1 | X | | X | |
Free fatty acid | GPR120 | FFA4 | X | | | X |
Galanin | GALR1 | GALR1 | X | X | | X |
Galanin | GALR2 | GALR2 | X | | X | |
Ghrelin | GHSR | ghrelin | X | | X | |
Glucagon | GCGR | glucagon | X | X | | X |
Glucagon | GIPR | GIP | X | X | | |
Glucagon | GLP1R | GLP-1 | X | X | | X |
Glucagon | GLP2R | GLP-2 | X | X | | X |
Glucagon | SCTR | secretin | X | X | | X |
Glycoprotein hormone receptor | FSHR | FSHR | X | X | | |
Glycoprotein hormone receptor | LHCGR | LH | X | X | | |
Glycoprotein hormone receptor | TSHR(L) | TSH | X | X | | |
Histamine | HRH1 | H1 | X | | X | |
Histamine | HRH2 | H2 | X | X | X | |
Histamine | HRH3 | H3 | X | X | | |
Histamine | HRH4 | H4 | X | | | |
Hydroxycarboxylic acid | GPR109A | HCA2 | X | X | | |
Hydroxycarboxylic acid | GPR109B | HCA3 | X | X | | |
Kisspeptin receptor | KISS1R | kisspeptin | X | | | |
Leukotriene | LTB4R | BLT1 | X | X | X | X |
Leukotriene | OXER1 | OXE | X | X | | X |
Lysophospholipid (LPA) | EDG4 | LPA2 | X | | X | |
Lysophospholipid (LPA) | EDG7 | LPA3 | X | | X | X |
Lysophospholipid (LPA) | GPR92 | GPR92 | X | | X | |
Lysophospholipid (S1P) | EDG1 | S1P1 | X | X | | X |
Lysophospholipid (S1P) | EDG3 | S1P3 | X | | X | X |
Lysophospholipid (S1P) | EDG5 | S1P2 | X | | | X |
Lysophospholipid (S1P) | EDG6 | S1P4 | X | | | |
Melanin-concentrating hormone | MCHR1 | MCH1 | X | X | | X |
Melanin-concentrating hormone | MCHR2 | MCH2 | X | | X | |
Melanocortin | MC1R | MC1 | X | X | | |
Melanocortin | MC3R | MC3 | X | X | | X |
Melanocortin | MC4R | MC4 | X | X | | |
Melanocortin | MC5R | MC5 | X | X | | |
Melatonin | MTNR1A | MT1 | X | X | | X |
Motilin | MLNR | motilin | X | | X | X |
Neuromedin U | NMU1R | NMU1 | X | | X | X |
Neuropeptide B & W | NPBWR1 | NPBW1 | X | X | | |
Neuropeptide B & W | NPBWR2 | NPBW2 | X | X | | |
Neuropeptide FF & AF | NPFFR1 | NPFF1 | X | X | | |
Neuropeptide S | NPSR1b | NPS receptor | X | | | |
Neuropeptide Y | NPY1R | Y1 | X | | | |
Neuropeptide Y | NPY2R | Y2 | X | X | X | X |
Neuropeptide Y | PPYR1 | Y4 | X | X | | |
Neurotensin | NTSR1 | NTS1 | X | | X | X |
NHR | AR | AR | | | | |
NHR | ERα | ESR1 | | | | |
NHR | FXR | NR1H4 | | | | |
NHR | GR | NR3C1 | | | | |
NHR | LXRα | NR1H3 | | | | |
NHR | LXRβ | NR1H2 | | | | |
NHR | MR | NR3C2 | | | | |
NHR | PPARα | PPARA | | | | |
NHR | PPARγ | PPARG | | | | |
NHR | PPARδ | PPARD | | | | |
NHR | PRα | PGR | | | | |
NHR | PRβ | PGR | | | | |
NHR | RARα | RARA | | | | |
NHR | RXRα | RXRA | | | | |
NHR | RXRγ | RXRG | | | | |
NHR | THRα | THRA | | | | |
NHR | THRβ | THRB | | | | |
Opioid | OPRD1 | δ | X | X | | X |
Opioid | OPRK1 | κ | X | X | | X |
Opioid | OPRL1 | NOP | X | X | | X |
Opioid | OPRM1 | μ | X | X | | X |
Orexin | HCRTR1 | OX1 | X | | X | X |
Orexin | HCRTR2 | OX2 | X | | X | X |
Other 7TM proteins | GPR107 | GPR107 | X | | | |
Other 7TM proteins | GPR137 | TM7SF1 | X | | | |
Other 7TM proteins | GPR143 | GPR143 | X | | | |
P2Y | P2RY1 | P2RY1 | X | | X | X |
P2Y | P2RY11 | P2Y11 | X | | | |
P2Y | P2RY12 | P2Y12 | X | | | X |
P2Y | P2RY2 | P2Y2 | X | | X | X |
P2Y | P2RY4 | P2Y4 | X | | | X |
P2Y | P2RY6 | P2Y6 | X | | | |
Parathyroid hormone | PTHR1 | PTH1 | X | X | X | X |
Parathyroid hormone | PTHR2 | PTH2 | X | X | X | X |
Peptide P518 | GPR103 | QRFPR | X | | X | |
Platelet-activating factor | PTAFR | PAF | X | | X | X |
Prokineticin | PROKR1 | PKR1 | X | X | X | X |
Prokineticin | PROKR2 | PKR2 | X | | | X |
Prolactin releasing peptide receptor | PRLHR | PRRP | X | | X | X |
Prostanoid | CRTH2 | PTGDR2 | X | X | | |
Prostanoid | PTGER2 | EP2 | X | X | | |
Prostanoid | PTGER3 | EP3 | X | X | X | |
Prostanoid | PTGER4 | EP4 | X | | | X |
Prostanoid | PTGFR | FP | X | | X | X |
Prostanoid | PTGIR | IP1 | X | X | | X |
Prostanoid | TBXA2R | TP | X | | X | X |
Protease activated | F2R | PAR1 | X | | | |
Protease activated | F2RL1 | PAR2 | X | | X | X |
Protease activated | F2RL3 | PAR4 | X | | X | X |
Receptor Tyrosine Kinase | c-KIT | KIT | | | | |
Receptor Tyrosine Kinase | c-Ret-GFRα2 | RET | | | | |
Receptor Tyrosine Kinase | DDR1 | CD167a | | | | |
Receptor Tyrosine Kinase | EphA5 | EphA5 | | | | |
Receptor Tyrosine Kinase | EphA7 | EphA7 | | | | |
Receptor Tyrosine Kinase | EphB2 | EphB2 | | | | |
Receptor Tyrosine Kinase | EphB3 | EphB3 | | | | |
Receptor Tyrosine Kinase | EphB4 | EphB4 | | | | |
Receptor Tyrosine Kinase | ErbB1 | EGFR | | | | |
Receptor Tyrosine Kinase | ErbB2-ErbB3 | HER2 | | | | |
Receptor Tyrosine Kinase | ErbB4 | HER4 | | | | |
Receptor Tyrosine Kinase | FLT4 | FLT4 | | | | |
Receptor Tyrosine Kinase | IGF1R | IGF1R | | | | |
Receptor Tyrosine Kinase | INSRb | INSR | | | | |
Receptor Tyrosine Kinase | KDR | VEGFR2 | | | | |
Receptor Tyrosine Kinase | PDGFRa | PDGFRa | | | | |
Receptor Tyrosine Kinase | PDGFRb | PDGFRb | | | | |
Receptor Tyrosine Kinase | TrkA-P75 | NTRK1 | | | | |
Receptor Tyrosine Kinase | TrkB-P75 | NTRK2 | | | | |
Receptor Tyrosine Kinase | TrkC-P75 | NTRK3 | | | | |
Relaxin | RXFP3 | RXFP3 | X | X | | X |
Somatostatin | SSTR1 | SST1 | X | | | |
Somatostatin | SSTR2 | SST2 | X | X | | X |
Somatostatin | SSTR3 | SST3 | X | X | | |
Somatostatin | SSTR5 | SST5 | X | X | | |
Tachykinin | TACR1 | NK1 | X | | X | X |
Tachykinin | TACR2 | NK2 | X | | X | X |
Tachykinin | TACR3 | NK3 | X | X | X | X |
Thyrotropin releasing hormone | TRHR | TRH1 | X | | X | X |
Urotensin | UTR2 | UT | X | | X | X |
Vasopressin and Oxytocin | AVPR1A | V1A | X | | X | X |
Vasopressin and Oxytocin | AVPR1B | V1B | X | | X | X |
Vasopressin and Oxytocin | AVPR2 | V2 | X | X | | X |
Vasopressin and Oxytocin | OXTR | OT | X | | X | X |
VIP and PACAP | ADCYAP1R1 | PAC1 | X | X | X | X |
VIP and PACAP | VIPR1 | VPAC1 | X | X | X | X |
VIP and PACAP | VIPR2 | VPAC2 | X | X | X | X |
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:
