Known GPCR Assay List
DiscoveRx offers an industry leading portfolio of non-force coupled GPCR cell lines designed to detect different GPCR signaling through arrestin recruitment, second messenger signaling and receptor internalization. Access to the same receptor in different technology formats allows multiple signaling pathways to be assayed in parallel and enables the identification of novel biased ligands and characterization of novel drug interactions. The DiscoveRx Services platform leverages this menu of GPCR assays for all screening and profiling services.
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Overview of Available Readouts
Arrestin
Second messenger (cAMP & Calcium)
Internalization
Browse Available Known GPCR Targets
Listed below are the assays currently available for screening and profiling. Assays may be sorted by column name.
Contact us if you don't see your target of interest in the list below as additional catalog assays may be available for screening and profiling as a custom service.
Note: Standard Known GPCR Profile Panel includes Arrestin assays only. Additional known GPCR assays (non-Arrestin) available as a custom panel request.
| Family | Target Gene | Common Name | Species | G protein coupling | Accession Number | Arrestin | cAMP | Calcium | Internalization |
| 5-Hydroxytryptamine | HTR1A | 5HT1A | Human | Gi/Go | NM_000524.2 | X | X | | |
| 5-Hydroxytryptamine | HTR1B | 5HT1B | Human | Gi/Go | NM_000863 | X | X | | |
| 5-Hydroxytryptamine | HTR1E | 5HT1E | Human | Gi/Go | NM_000865 | X | | | |
| 5-Hydroxytryptamine | HTR1F | 5HT1F | Human | Gi/Go | NM_000866.3 | X | X | | |
| 5-Hydroxytryptamine | HTR2A | 5HT2A | Human | Gq | NM_000621.3 | X | | X | X |
| 5-Hydroxytryptamine | HTR2B* | 5HT2B | Human | Gq | NM_000867.4 | | | X | |
| 5-Hydroxytryptamine | HTR2C | 5HT2C | Human | Gq | AF498983 | X | | X | X |
| 5-Hydroxytryptamine | HTR5A | 5HT5A | Human | Gi/Go | NM_024012 | X | X | | |
| 5-Hydroxytryptamine | HTR7A* | 5HT7A | Human | Gs | NM_000872.4 | | X | | |
| 5-Hydroxytryptamine | HTR7B* | 5HT7B | Human | Gs | NM_019860.3 | | X | | |
| 5-Hydroxytryptamine | HTR7D* | 5HT7D | Human | Gs | NM_000872 | | X | | |
| Acetylcholine | CHRM1 | M1 | Human | Gq | AF498915 | X | | X | X |
| Acetylcholine | CHRM2 | M2 | Human | Gi/Go | AF498916 | X | X | | X |
| Acetylcholine | CHRM3 | M3 | Human | Gq | AF498917 | X | | X | X |
| Acetylcholine | CHRM4 | M4 | Human | Gs & Gi/Go | NM_000741.2 | X | X | | |
| Acetylcholine | CHRM5 | M5 | Human | Gq | AF498919 | X | | X | X |
| Adenosine | ADORA1 | A1 | Human | Gi/Go | AY136746 | X | X | X | |
| Adenosine | ADORA2A* | A2A | Human | Gs & Gq | NM_000675.4 | | | X | |
| Adenosine | ADORA2B | A2B | Human | Gs | AY136748 | X | X | | |
| Adenosine | ADORA3 | A3 | Human | Gi/Go | NM_000677.3 | X | X | | |
| Adrenergic | ADRA2C | α2C-adrenoreceptor | Human | Gi/Go | NM_000683 | X | X | | |
| Adrenergic | ADRB1 | β1-adrenoreceptor | Human | Gs | NM_000684 | X | X | | |
| Adrenergic | ADRB2 | β2-adrenoreceptor | Human | Gs | NM_000024 | X | X | | X |
| Adrenergic | ADRB3* | β3-adrenoreceptor | Human | Gs | NM_000025 | | X | | |
| Adrenergic | ADRA1A* | α1A-adrenoreceptor | Human | Gq | NM_000680 | | | X | |
| Adrenergic | ADRA1B | α1B-adrenoreceptor | Human | Gq | NM_000679 | X | | X | |
| Adrenergic | ADRA2A | α2A-adrenoreceptor | Human | Gi/Go | NM_000681 | X | X | | |
| Adrenergic | ADRA2B | α2B-adrenoreceptor | Human | Gi/Go | NM_000682.5 | X | | | |
| Anaphylatoxin | C3AR1 | C3A | Human | Gi/Go | NM_004054.2 | X | X | | X |
| Anaphylatoxin | C5AR1 | C5A | Human | Gi/Go | NM_001736 | X | X | | X |
| Anaphylatoxin | C5L2 | C5L2 | Human | None | NM_018485.1 | X | | | X |
| Angiotensin | AGTR1 | AT1 | Human | Gq | NM_000685 | X | | X | |
| Apelin | AGTRL1 | APJ | Human | Gi/Go | NM_005161 | X | X | | X |
| Bile acid | GPBAR1 | GPBA | Human | Gs | NM_001077194.1 | X | X | | |
| Bombesin | BRS3 | BB3 | Human | Gq | NM_001727 | X | | X | |
| Bombesin | GRPR | BB2 | Human | Gq | NM_005314 | X | | X | X |
| Bradykinin | BDKRB1 | B1 | Human | Gq | NM_000710.2 | X | | X | |
| Bradykinin | BDKRB2 | B2 | Human | Gq | NM_000623.3 | X | | X | X |
| Calcitonin | CALCR | CT | Human | Gs | NM_001742.2 | X | X | | |
| Calcitonin | CALCR + RAMP1* | AMY1 | Human | Gs | NM_001742.2 | | X | | |
| Calcitonin | CALCR + RAMP2 | AMY2 | Human | Gs | NM_001742.2 | X | | | |
| Calcitonin | CALCR + RAMP3 | AMY3 | Human | Gs | NM_001742.2 | X | X | | |
| Calcitonin | CALCRL + RAMP1 | CGRP | Human | Gs | AY389506 | X | X | | |
| Calcitonin | CALCRL + RAMP2 | AM1 | Human | Gs | AY389506 | X | X | | |
| Calcitonin | CALCRL + RAMP3 | AM2 | Human | Gs | AY389506 | X | X | | |
| Calcium sensing | CASR* | CaS | Human | Gq & Gi/Go | NM_000388.3 | | | X | |
| Cannabinoid | CNR1 | CB1 | Human | Gi/Go | AY225225 | X | X | | |
| Cannabinoid | CNR2 | CB2 | Human | Gi/Go | AY242132 | X | X | | |
| Chemokine | CCR1 | CCR1 | Human | Gi/Go | NM_001295 | X | X | | X |
| Chemokine | CCR10 | CCR10 | Human | Gi/Go | AY429103 | X | X | | X |
| Chemokine | CCR2 | CCR2 | Human | Gi/Go | NM_001123396 | X | | | X |
| Chemokine | CCR3 | CCR3 | Human | Gi/Go | NM_001837 | X | | | |
| Chemokine | CCR4 | CCR4 | Human | Gi/Go | AY322539 | X | | | X |
| Chemokine | CCR5 | CCR5 | Human | Gi/Go | BC038398 | X | X | | X |
| Chemokine | CCR6 | CCR6 | Human | Gi/Go | AY242126 | X | X | | X |
| Chemokine | CCR7 | CCR7 | Human | Gi/Go | AY587876 | X | X | | X |
| Chemokine | CCR8 | CCR8 | Human | Gi/Go | NM_005201.3 | X | | | |
| Chemokine | CCR9 | CCR9 | Human | Gi/Go | AY242127 | X | | | |
| Chemokine | CMKLR1 | CMKLR1 | Human | Gi/Go | NM_004072.2 | X | X | | |
| Chemokine | CX3CR1 | CX3CR1 | Human | Gi/Go | NM_001337 | X | | | |
| Chemokine | CXCR1 | CXCR1 | Human | Gi/Go | NM_000634 | X | X | | X |
| Chemokine | CXCR2 | CXCR2 | Human | Gi/Go | NM_001557 | X | X | | X |
| Chemokine | CXCR3 | CXCR3 | Human | Gi/Go | AY242128 | X | X | | X |
| Chemokine | CXCR4 | CXCR4 | Human | Gi/Go | AY242129 | X | X | | |
| Chemokine | CXCR5 | CXCR5 | Human | Gi/Go | NM_001716 | X | X | | |
| Chemokine | CXCR6 | CXCR6 | Human | Gi/Go | AY322543 | X | X | | X |
| Chemokine | CXCR7 | CXCR7 | Human | None | NM_020311.2 | X | | | X |
| Chemokine | XCR1 | XCR1 | Human | Gi/Go | NM_005283 | X | X | | |
| Cholecystokinin | CCKAR | CCK1 | Human | Gq | AY322549 | X | | X | X |
| Cholecystokinin | CCKBR | CCK2 | Human | Gq | AY322551 | X | | X | X |
| Class A Orphan | EBI2 | GPR183 | Human | Gi/Go | NM_080818 | X | | | |
| Class A Orphan | GPR1 | GPR1 | Human | N/A | NM_005279 | X | | | X |
| Class A Orphan | GPR119 | GPR119 | Human | Unknown | NM_178471 | X | | | |
| Class A Orphan | GPR120 | GPR120 | Human | Unknown | NM_181745 | X | | | X |
| Class A Orphan | GPR35 | GPR35 | Human | Gi/Go | NM_005301 | X | X | | |
| Class A Orphan | GPR55 | GPR55 | Human | Unknown | NM_005683.3 | X | | | |
| Class A Orphan | GPR84 | GPR84 | Human | Gi/Go | NM_020370 | X | X | | |
| Class A Orphan | GPR91 | SUCNR1 | Human | Unknown | NM_033050 | X | | | |
| Class A Orphan | GPR92 | GPR92 | Human | Gq | NM_020400 | X | | X | |
| Class A Orphan | MRGPRX2 | MRGX2 | Human | Gq | NM_054030 | X | | X | |
| Corticotropin | CRHR1 | CRF1 | Human | Gs | AY457172 | X | X | | X |
| Corticotropin | CRHR2 | CRF2 | Human | Gs | AY449734 | X | X | | |
| Dopamine | DRD1 | D1 | Human | Gs | NM_000794.3 | X | X | | |
| Dopamine | DRD2L | D2L | Human | Gi/Go | NM_000795.3 | X | X | | |
| Dopamine | DRD2S | D2S | Human | Gi/Go | NM_016574.3 | X | X | | |
| Dopamine | DRD3 | D3 | Human | Gi/Go | NM_000796.3 | X | | | |
| Dopamine | DRD4 | D4 | Human | Gi/Go | NM_000797.2 | X | X | | |
| Dopamine | DRD5 | D5 | Human | Gs | NM_000798.3 | X | X | | |
| Endothelin | EDNRA | ETA | Human | Gq | AY275462 | X | | X | |
| Endothelin | EDNRB | ETB | Human | Gs & Gi/Go | NM_000115.2 | X | | | X |
| Formylpeptide | FPR1 | FPR1 | Human | Gi/Go | NM_002029 | X | X | | X |
| Formylpeptide | FPRL1 | FPR2/ALX | Human | Gi/Go | AY225226 | X | X | | X |
| Free Fatty Acid | FFAR1 | FFA1 | Human | Gq | NM_005303.2 | X | | X | |
| Free Fatty Acid | FFAR2* | GPR43 | Human | Gq & Gi/Go | NM_005306.2 | | | X | |
| Free Fatty Acid | FFAR3* | GPR41 | Human | Gi/Go | NM_005304.3 | | X | | |
| GABAB | GABBR1* | GABB1 | Human | N/A | NM_021903.2 | | X | | |
| Galanin | GALR1 | GALR1 | Human | Gi/Go | AY541036 | X | X | | X |
| Galanin | GALR2 | GALR2 | Human | Gq & Gs | NM_003857 | X | X | X | |
| Ghrelin | GHSR1a | ghrelin | Human | Gq | NM_198407 | X | | X | |
| Glucagon | GCGR | glucagon | Human | Gs | NM_000160 | X | X | | X |
| Glucagon | GHRHR* | GHRH | Human | Gs | NM_000823.2 | | X | | |
| Glucagon | GIPR | GIP | Human | Gs | NM_000164 | X | X | | X |
| Glucagon | GLP1R | GLP-1 | Human | Gs | BC112126 | X | X | | X |
| Glucagon | GLP2R | GLP-2 | Human | Gs | NM004246.1 | X | X | | X |
| Glucagon | SCTR | secretin | Human | Gs | AY462218 | X | X | | X |
| Glutamate | GRM1* | mGlu1 | Human | Gq | NM_000838.2 | | | X | |
| Glutamate | GRM2* | mGlu2 | Human | Gi/Go | NM_000839 | | X | | |
| Glutamate | GRM3* | MGlu3 | Human | Gi/Go | NM_000840.2 | | X | | |
| Glutamate | GRM4* | mGlu4 | Human | Gi/Go | NM_000841 | | X | | |
| Glutamate | GRM6* | mGlu6 | Human | Gi/Go | NM_000843 | | X | | |
| Glycoprotein hormone receptor | FSHR | FSHR | Human | Gs | NM_000145 | X | X | | |
| Glycoprotein hormone receptor | LHCGR | LH | Human | Gs | NM_000233 | X | X | | |
| Glycoprotein hormone receptor | TSHR(L) | TSH | Human | Gs | NM_000369.2 | X | X | | |
| Gonadotropin-releasing hormone | GNRHR* | GnRH | Human | Gq | NM_000406.2 | | | X | |
| Histamine | HRH1 | H1 | Human | Gq | AY136743 | X | | X | |
| Histamine | HRH2 | H2 | Human | Gs | AY136744 | X | X | | |
| Histamine | HRH3 | H3 | Human | Gi/Go | NM_007232 | X | X | | |
| Histamine | HRH4 | H4 | Human | Gi/Go | NM_021624 | X | | | |
| Hydroxycarboxylic acid | GPR109A | HCA2 | Human | Gi/Go | NM_177551 | X | X | | |
| Hydroxycarboxylic acid | GPR109B | HCA3 | Human | Gi/Go | NM_006018 | X | X | | |
| Hydroxycarboxylic acid | GPR81 | HCA1 | Human | Gi/Go | NM_032554 | X | X | | |
| Kisspeptin receptor | KISS1R | kisspeptin | Human | Gq | NM_032551 | X | | | |
| Leukotriene | LTB4R | BLT1 | Human | Gi/Go & Gq | AY322535 | X | X | X | X |
| Leukotriene | OXER1* | OXE | Human | Gi/Go | NM_148962.4 | | X | | |
| Leukotriene | CYSLTR2* | CYSLT2 | Human | Gq | NM_020377.2 | | | X | |
| Lysophospholipid | EDG1 | S1P1 | Human | Gi/Go | NM_001400 | X | X | | X |
| Lysophospholipid | EDG2 | LPA1 | Human | Gi/Go | NM_001401.3 | X | | | X |
| Lysophospholipid | EDG3 | S1P3 | Human | Gq | NM_005226 | X | | X | X |
| Lysophospholipid | EDG4 | LPA2 | Human | Gq | AY322548 | X | | X | |
| Lysophospholipid | EDG5 | S1P2 | Human | Gs | NM_004230.3 | X | | | X |
| Lysophospholipid | EDG6 | S1P4 | Human | Gq | AY322537 | X | | | |
| Lysophospholipid | EDG7 | LPA3 | Human | Gq | NM_012152.2 | X | | X | X |
| Lysophospholipid | EDG8 | S1P5 | Human | Gi/Go | NM_030760.4 | X | | | |
| Melanin-concentrating hormone | MCHR1 | MCH1 | Human | Gi/Go | AY562945 | X | X | | |
| Melanin-concentrating hormone | MCHR2 | MCH2 | Human | Gq | NM_000706.3 | X | | X | |
| Melanocortin | MC1R | MC1 | Human | Gs | NM_002386 | X | X | | |
| Melanocortin | MC3R | MC3 | Human | Gs | AY227893 | X | X | | X |
| Melanocortin | MC4R | MC4 | Human | Gs | AY236539 | X | X | | |
| Melanocortin | MC5R | MC5 | Human | Gs | NM_005913 | X | X | | |
| Melatonin | MTNR1A | MT1 | Human | Gi/Go | NM_005958 | X | X | | |
| Melatonin | MTNR1B | MT2 | Human | Gi/Go | NM_005959.3 | X | X | | |
| Motilin | MLNR | motilin | Human | Gq | AY603964 | X | | X | X |
| Neuromedin U | NMU1R | NMU1 | Human | Gq | NM_006056 | X | | X | X |
| Neuropeptide B & W | NPBWR1 | NPBW1 | Human | Gi/Go | NM_005285 | X | X | | |
| Neuropeptide B & W | NPBWR2 | NPBW2 | Human | Gi/Go | NM_005286 | X | X | | |
| Neuropeptide F | NPFFR1 | NPFF1 | Human | Gi/Go | NM_022146 | X | X | | |
| Neuropeptide F | NPFFR2* | NPFF2 | Human | Gi/Go | NM_053036.2 | | X | | |
| Neuropeptide S | NPSR1B | NPS receptor | Human | Gq | NM_207172 | X | | | |
| Neuropeptide Y | NPY1R | Y1 | Human | Gi/Go | AY548168 | X | X | | |
| Neuropeptide Y | NPY2R | Y2 | Human | Gi/Go | AY236540 | X | X | X | X |
| Neuropeptide Y | PPYR1 | Y4 | Human | Gi/Go | AY268432 | X | X | | |
| Neurotensin | NTSR1 | NTS1 | Human | Gq | AY429106 | X | | X | X |
| Opioid | OPRD1 | δ | Human | Gi/Go | NM_000911 | X | X | | X |
| Opioid | OPRK1 | κ | Human | Gi/Go | AF498922 | X | X | | X |
| Opioid | OPRL1 | NOP | Human | Gi/Go | AY268428 | X | X | | |
| Opioid | OPRM1 | μ | Human | Gi/Go | NM_000914.3 | X | X | | X |
| Orexin | HCRTR1 | OX1 | Human | Gq | NM_001525.2 | X | | X | X |
| Orexin | HCRTR2 | OX2 | Human | Gq | AF041245 | X | | X | X |
| P2Y | P2RY1 | P2RY1 | Human | Gq | NM_002563.2 | X | | X | |
| P2Y | P2RY11 | P2Y11 | Human | Gs & Gq | AY449733 | X | | X | X |
| P2Y | P2RY12 | P2Y12 | Human | Gi/Go | AY136754 | X | | | |
| P2Y | P2RY2 | P2Y2 | Human | Gq | AY136753 | X | | X | X |
| P2Y | P2RY4 | P2Y4 | Human | Gq | NM_002565 | X | | X | X |
| P2Y | P2RY6 | P2Y6 | Human | Gq | NM_004154 | X | | | |
| Parathyroid | PTHR1 | PTH1 | Human | Gs & Gq | AY449732 | X | X | X | X |
| Parathyroid | PTHR2 | PTH2 | Human | Gs | AY497546 | X | X | X | X |
| Platelet-activating factor | PTAFR | PAF | Human | Gi/Go & Gq | AY275466 | X | X | X | X |
| Prokineticin | PROKR1 | PKR1 | Human | Gs & Gq | NM_138964 | X | X | X | X |
| Prokineticin | PROKR2 | PKR2 | Human | Gs | NM_144773 | X | | | X |
| Prolactin releasing peptide receptor | PRLHR | PRRP | Human | Gq | NM_004248 | X | | X | X |
| Prostanoid | PTGER2 | EP2 | Human | Gs | AY275471 | X | | | |
| Prostanoid | PTGER3 | EP3 | Human | Gi/Go & Gq | NM_198716 | X | X | X | |
| Prostanoid | PTGER4 | EP4 | Human | Gs | AY429109 | X | | | X |
| Prostanoid | PTGFR | FP | Human | Gq | NM_000959.3 | X | | X | X |
| Prostanoid | PTGIR | IP1 | Human | Gs | AY242134 | X | X | | X |
| Prostanoid | TBXA2R | TP | Human | Gq | NM_001060 | X | | X | |
| Prostanoid | CRTH2 | DP2 | Human | Gi/Go | AY507142 | X | X | | |
| Prostanoid | PTGDR* | DP1 | Human | Gs | NM_000953 | | X | | |
| Prostanoid | PTGER1 | EP1 | Human | Gq | NM_000955.2 | X | | X | |
| Protease activated | F2R | PAR1 | Human | Gi/Go | BC002464 | X | | X | |
| Protease activated | F2RL1 | PAR2 | Human | Gi/Go & Gq | NM_005242.4 | X | | X | X |
| Protease activated | F2RL3 | PAR4 | Human | Gi/Go & Gq | AY431102 | X | | X | X |
| Relaxin | RXFP1* | RXFP1 | Human | Gs | NM_021634.2 | | X | | |
| Relaxin | RXFP3 | RXFP3 | Human | Gi/Go | NM_016568.2 | X | X | | |
| Relaxin | RXFP4 | RXFP4 | Human | Gi/Go | NM_181885.2 | X | X | X | |
| Somatostatin | SSTR1 | SST1 | Human | Gi/Go | NM_001049 | X | | | |
| Somatostatin | SSTR2 | SST2 | Human | Gi/Go | AY236542 | X | X | | X |
| Somatostatin | SSTR3 | SST3 | Human | Gi/Go | AY322541 | X | X | | |
| Somatostatin | SSTR4 | SST4 | Human | Gi/Go | AY548169 | X | X | | |
| Somatostatin | SSTR5 | SST5 | Human | Gi/Go | NM_001053 | X | X | | |
| Tachykinin | TACR1 | NK1 | Human | Gq | NM_001058 | X | | X | X |
| Tachykinin | TACR2 | NK2 | Human | Gq | AY322545 | X | | X | X |
| Tachykinin | TACR3 | NK3 | Human | Gs & Gq | NM_001059 | X | X | X | X |
| TRH | TRHR | TRH1 | Human | Gq | AY493373 | X | | X | |
| Urotensin | UTR2 | UT | Human | Gq | NM_018949 | X | | X | X |
| Vasopressin and Oxytocin | AVPR1A | V1A | Human | Gq | NM_000706.3 | X | | X | X |
| Vasopressin and Oxytocin | AVPR1B | V1B | Human | Gq | NM_000707.3 | X | | X | X |
| Vasopressin and Oxytocin | AVPR2 | V2 | Human | Gs | NM_000054.4 | X | X | | X |
| Vasopressin and Oxytocin | OXTR | OT | Human | Gq | AY389507 | X | | X | X |
| VIP and PACAP | ADCYAP1R1 | PAC1 | Human | Gs & Gq | AY366498 | X | X | X | X |
| VIP and PACAP | VIPR1 | VPAC1 | Human | Gs & Gq | NM_004624 | X | X | | X |
| VIP and PACAP | VIPR2 | VPAC2 | Human | Gs | NM_003382 | X | X | | X |