GPCR Targets Available
Industry-leading portfolio, multiple signaling pathways, innovative solutions
The foundation of the DiscoveRx outsourced solutions portfolio is our comprehensive collection of highly validated, robust GPCR assays using multiple readout platforms. Access to the same GPCR target in different technology formats allows multiple signaling pathways to be assayed in parallel which affords a unique opportunity to identify drug interactions that may be missed with a single signaling platform.
Overview of Available Readouts
Arrestin
Second messenger (cAMP & Calcium)
Internalization
GPCR Signaling Pathway
Browse Available 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.
| Family | Target Class | Common Name | Species | G protein coupling | Accession Number | Arrestin | cAMP | Calcium | Internalization |
| 5-Hydroxytryptamine | GPCR | m5HT2A | Mouse | Gi/Go | NM_172812 | X | | | |
| 5-Hydroxytryptamine | GPCR | m5HT2C | Mouse | Gi/Go | AF498983 | X | | | |
| 5-Hydroxytryptamine | GPCR | 5HT1A | Human | Gi/Go | NM_000524.2 | X | X | | |
| 5-Hydroxytryptamine | GPCR | 5HT1B | Human | Gi/Go | NM_000863 | X | X | | |
| 5-Hydroxytryptamine | GPCR | 5HT1E | Human | Gi/Go | NM_000865 | X | | | |
| 5-Hydroxytryptamine | GPCR | 5HT1F | Human | Gi/Go | NM_000866.3 | X | X | | |
| 5-Hydroxytryptamine | GPCR | 5HT2A | Human | Gq | NM_000621.3 | X | | X | X |
| 5-Hydroxytryptamine | GPCR | 5HT2B | Human | Gq | NM_000867.4 | | | X | |
| 5-Hydroxytryptamine | GPCR | 5HT2C | Human | Gq | AF498983 | X | | X | X |
| 5-Hydroxytryptamine | GPCR | 5HT5A | Human | Gi/Go | NM_024012 | X | X | | |
| 5-Hydroxytryptamine | GPCR | 5HT7A | Human | Gs | NM_000872.4 | | X | | |
| 5-Hydroxytryptamine | GPCR | 5HT7B | Human | Gs | NM_019860.3 | | X | | |
| 5-Hydroxytryptamine | GPCR | 5HT7D | Human | Gs | NM_000872 | | X | | |
| Acetylcholine | GPCR | rM4 | Rat | Gs & Gi/Go | NM_000741 | X | | | |
| Acetylcholine | GPCR | M1 | Human | Gq | AF498915 | X | | X | X |
| Acetylcholine | GPCR | M2 | Human | Gi/Go | AF498916 | X | X | | X |
| Acetylcholine | GPCR | M3 | Human | Gq | AF498917 | X | | X | X |
| Acetylcholine | GPCR | M4 | Human | Gs & Gi/Go | NM_000741.2 | X | X | | |
| Acetylcholine | GPCR | M5 | Human | Gq | AF498919 | X | | X | X |
| Adenosine | GPCR | mA2B | Mouse | Gs | NM_007413 | X | | | |
| Adenosine | GPCR | mA3 | Mouse | Gi/Go | NM_009631.3 | X | | | |
| Adenosine | GPCR | A1 | Human | Gi/Go | AY136746 | X | X | X | |
| Adenosine | GPCR | A2A | Human | Gs & Gq | NM_000675.4 | | | X | |
| Adenosine | GPCR | A2B | Human | Gs | AY136748 | X | X | | |
| Adenosine | GPCR | A3 | Human | Gi/Go | NM_000677.3 | X | X | | |
| Adrenergic | GPCR | α2C-adrenoreceptor | Human | Gi/Go | NM_000683 | X | X | | |
| Adrenergic | GPCR | β1-adrenoreceptor | Human | Gs | NM_000684 | X | X | | |
| Adrenergic | GPCR | β2-adrenoreceptor | Human | Gs | NM_000024 | X | X | | X |
| Adrenergic | GPCR | β3-adrenoreceptor | Human | Gs | NM_000025 | | X | | |
| Adrenergic | GPCR | α1A-adrenoreceptor | Human | Gq | NM_000680 | | | X | |
| Adrenergic | GPCR | α1B-adrenoreceptor | Human | Gq | NM_000679 | X | | X | |
| Adrenergic | GPCR | α2A-adrenoreceptor | Human | Gi/Go | NM_000681 | X | X | | |
| Adrenergic | GPCR | α2B-adrenoreceptor | Human | Gi/Go | NM_000682.5 | X | | | |
| Anaphylatoxin | GPCR | C3A | Human | Gi/Go | NM_004054.2 | X | X | | X |
| Anaphylatoxin | GPCR | C5A | Human | Gi/Go | NM_001736 | X | X | | X |
| Anaphylatoxin | GPCR | C5L2 | Human | None | NM_018485.1 | X | | | X |
| Anaphylatoxin | GPCR | mC5AR | Mouse | Gi/Go | NM_007577.3 | X | | | |
| Angiotensin | GPCR | AT1 | Human | Gq | NM_000685 | X | | X | |
| Apelin | GPCR | APJ | Human | Gi/Go | NM_005161 | X | X | | X |
| Apelin | GPCR | mAPJ | Mouse | Gi/Go | NM_011784.2 | X | | | |
| Bile acid | GPCR | GPBA | Human | Gs | NM_001077194.1 | X | X | | |
| Bombesin | GPCR | BB3 | Human | Gq | NM_001727 | X | | X | |
| Bombesin | GPCR | BB2 | Human | Gq | NM_005314 | X | | X | X |
| Bradykinin | GPCR | B1 | Human | Gq | NM_000710.2 | X | | X | |
| Bradykinin | GPCR | B2 | Human | Gq | NM_000623.3 | X | | X | X |
| Calcitonin | GPCR | CT | Human | Gs | NM_001742.2 | X | X | | |
| Calcitonin | GPCR | AMY1 | Human | Gs | NM_001742.2 | | X | | |
| Calcitonin | GPCR | AMY2 | Human | Gs | NM_001742.2 | X | | | |
| Calcitonin | GPCR | AMY3 | Human | Gs | NM_001742.2 | X | X | | |
| Calcitonin | GPCR | CGRP | Human | Gs | AY389506 | X | X | | |
| Calcitonin | GPCR | AM1 | Human | Gs | AY389506 | X | X | | |
| Calcitonin | GPCR | AM2 | Human | Gs | AY389506 | X | X | | |
| Calcium sensing | GPCR | CaS | Human | Gq & Gi/Go | NM_000388.3 | | | X | |
| Cannabinoid | GPCR | CB1 | Human | Gi/Go | AY225225 | X | X | | |
| Cannabinoid | GPCR | CB2 | Human | Gi/Go | AY242132 | X | X | | |
| Cannabinoid | GPCR | mCB1 | Mouse | Gi/Go | NM_007726 | X | | | |
| Cannabinoid | GPCR | mCB2 | Mouse | Gi/Go | NM_009924 | X | | | |
| Chemokine | GPCR | CCR1 | Human | Gi/Go | NM_001295 | X | X | | X |
| Chemokine | GPCR | CCR10 | Human | Gi/Go | AY429103 | X | X | | X |
| Chemokine | GPCR | CCR2 | Human | Gi/Go | NM_001123396 | X | | | X |
| Chemokine | GPCR | CCR3 | Human | Gi/Go | NM_001837 | X | | | |
| Chemokine | GPCR | CCR4 | Human | Gi/Go | AY322539 | X | | | X |
| Chemokine | GPCR | CCR5 | Human | Gi/Go | BC038398 | X | X | | X |
| Chemokine | GPCR | CCR6 | Human | Gi/Go | AY242126 | X | X | | X |
| Chemokine | GPCR | CCR7 | Human | Gi/Go | AY587876 | X | X | | X |
| Chemokine | GPCR | CCR8 | Human | Gi/Go | NM_005201.3 | X | | | |
| Chemokine | GPCR | CCR9 | Human | Gi/Go | AY242127 | X | | | |
| Chemokine | GPCR | CMKLR1 | Human | Gi/Go | NM_004072.2 | X | X | | |
| Chemokine | GPCR | CX3CR1 | Human | Gi/Go | NM_001337 | X | | | |
| Chemokine | GPCR | CXCR1 | Human | Gi/Go | NM_000634 | X | X | | X |
| Chemokine | GPCR | CXCR2 | Human | Gi/Go | NM_001557 | X | X | | X |
| Chemokine | GPCR | CXCR3 | Human | Gi/Go | AY242128 | X | X | | X |
| Chemokine | GPCR | CXCR4 | Human | Gi/Go | AY242129 | X | X | | |
| Chemokine | GPCR | CXCR5 | Human | Gi/Go | NM_001716 | X | X | | |
| Chemokine | GPCR | CXCR6 | Human | Gi/Go | AY322543 | X | X | | X |
| Chemokine | GPCR | CXCR7 | Human | None | NM_020311.2 | X | | | X |
| Chemokine | GPCR | XCR1 | Human | Gi/Go | NM_005283 | X | X | | |
| Chemokine | GPCR | mCC1 | Mouse | Gi/Go | NM_009912 | X | | | |
| Chemokine | GPCR | mCCR10 | Mouse | Gi/Go | AY429103 | X | | | |
| Chemokine | GPCR | mCCR2 | Mouse | Gi/Go | NM_009915.2 | X | | | |
| Chemokine | GPCR | mCCR3 | Mouse | Gi/Go | NM_009914 | X | | | |
| Chemokine | GPCR | mCCR4 | Mouse | Gi/Go | NM_006619 | X | | | |
| Chemokine | GPCR | mCCR5 | Mouse | Gi/Go | NM_009917 | X | | | |
| Chemokine | GPCR | mCCR6 | Mouse | Gi/Go | NM_009835.3 | X | | | |
| Chemokine | GPCR | mCCR7 | Mouse | Gi/Go | NM_007719.2 | X | | | |
| Chemokine | GPCR | mCCR8 | Mouse | Gi/Go | NM_007720.2 | X | | | |
| Chemokine | GPCR | mCMKLR1 | Mouse | Gi/Go | NM_008153.2 | X | | | |
| Chemokine | GPCR | mCXCR2 | Mouse | Gi/Go | NM_009909 | X | | | |
| Chemokine | GPCR | mCXCR3 | Mouse | Gi/Go | NM_009910 | X | | | |
| Chemokine | GPCR | mCXCR4 | Mouse | Gi/Go | XM_001478244.1 | X | | | |
| Chemokine | GPCR | mCXCR5 | Mouse | Gi/Go | NM_007551 | X | | | |
| Chemokine | GPCR | mCXCR6 | Mouse | Gi/Go | NM_030712 | X | | | |
| Chemokine | GPCR | mCXCR7 | Mouse | None | NM_007722 | X | | | |
| Chemokine | GPCR | mCCR9 | Mouse | Gi/Go | NM_007713.5 | X | | | |
| Cholecystokinin | GPCR | CCK1 | Human | Gq | AY322549 | X | | X | X |
| Cholecystokinin | GPCR | CCK2 | Human | Gq | AY322551 | X | | X | X |
| Class A Orphan | GPCR | GPR183 | Human | Gi/Go | NM_080818 | X | | | |
| Class A Orphan | GPCR | GPR1 | Human | N/A | NM_005279 | X | | | X |
| Class A Orphan | GPCR | GPR119 | Human | Unknown | NM_178471 | X | | | |
| Class A Orphan | GPCR | GPR120 | Human | Unknown | NM_181745 | X | | | X |
| Class A Orphan | GPCR | GPR35 | Human | Gi/Go | NM_005301 | X | X | | |
| Class A Orphan | GPCR | GPR55 | Human | Unknown | NM_005683.3 | X | | | |
| Class A Orphan | GPCR | GPR84 | Human | Gi/Go | NM_020370 | X | X | | |
| Class A Orphan | GPCR | SUCNR1 | Human | Unknown | NM_033050 | X | | | |
| Class A Orphan | GPCR | GPR92 | Human | Gq | NM_020400 | X | | X | |
| Class A Orphan | GPCR | MRGX2 | Human | Gq | NM_054030 | X | | X | |
| Class A Orphan | GPCR | CCRL2 | Human | Unknown | NM_003965 | X | | | |
| Class A Orphan | GPCR | GHSR1b | Human | Unknown | NM_004122 | X | | | |
| Class A Orphan | GPCR | GPR101 | Human | Unknown | NM_054021 | X | | | |
| Class A Orphan | GPCR | GPR12 | Human | Unknown | NM_005288 | X | | | |
| Class A Orphan | GPCR | GPR132 | Human | Unknown | NM_013345 | X | | | |
| Class A Orphan | GPCR | GPR135 | Human | Unknown | NM_022571 | X | | | |
| Class A Orphan | GPCR | GPR139 | Human | Unknown | NM_171791 | X | | | |
| Class A Orphan | GPCR | GPR141 | Human | Unknown | NM_181791 | X | | | |
| Class A Orphan | GPCR | GPR142 | Human | Unknown | NM_181790 | X | | | |
| Class A Orphan | GPCR | GPR146 | Human | Unknown | NM_138445 | X | | | |
| Class A Orphan | GPCR | GPR148 | Human | Unknown | XM_293092 | X | | | |
| Class A Orphan | GPCR | GPR149 | Human | Unknown | XM_293580 | X | | | |
| Class A Orphan | GPCR | GPR15 | Human | Unknown | NM_005290.1 | X | | | |
| Class A Orphan | GPCR | GPR150 | Human | Unknown | XM_209675 | X | | | |
| Class A Orphan | GPCR | GPR151 | Human | Unknown | NM_194251 | X | | | |
| Class A Orphan | GPCR | GPR152 | Human | Unknown | XM_352045 | X | | | |
| Class A Orphan | GPCR | GPR161 | Human | Unknown | NM_153832.1 | X | | | |
| Class A Orphan | GPCR | GPR162 | Human | Unknown | NM_019858 | X | | | |
| Class A Orphan | GPCR | GPR17 | Human | Unknown | NM_005291 | X | | | |
| Class A Orphan | GPCR | GPR171 | Human | Unknown | NM_013308 | X | | | |
| Class A Orphan | GPCR | GPR173 | Human | Unknown | NM_018969 | X | | | |
| Class A Orphan | GPCR | GPR176 | Human | Unknown | NM_007223 | X | | | |
| Class A Orphan | GPCR | GPR18 | Human | Unknown | NM_005292 | X | | | |
| Class A Orphan | GPCR | GPR182 | Human | Unknown | NM_007264 | X | | | |
| Class A Orphan | GPCR | GPR20 | Human | Unknown | NM_005293 | X | | | |
| Class A Orphan | GPCR | LPA4 | Human | Unknown | NM_005296 | X | | | |
| Class A Orphan | GPCR | GPR25 | Human | Unknown | NM_005298 | X | | | |
| Class A Orphan | GPCR | GPR26 | Human | Unknown | NM_153442 | X | | | |
| Class A Orphan | GPCR | GPR27 | Human | Unknown | NM_018971 | X | | | |
| Class A Orphan | GPCR | GPR3 | Human | Unknown | NM_005281 | X | | | |
| Class A Orphan | GPCR | GPR31 | Human | Unknown | NM_005299 | X | | | |
| Class A Orphan | GPCR | GPR32 | Human | Unknown | NM_001506 | X | | | |
| Class A Orphan | GPCR | EDNRBL | Human | Unknown | NM_005302 | X | | | |
| Class A Orphan | GPCR | GPR37L1 | Human | Unknown | NM_004767 | X | | | |
| Class A Orphan | GPCR | GPR39 | Human | Gq | NM_001508 | X | | | |
| Class A Orphan | GPCR | GPR4 | Human | Unknown | NM_005282 | X | | | |
| Class A Orphan | GPCR | GPR45 | Human | Unknown | NM_007227 | X | | | |
| Class A Orphan | GPCR | GPR50 | Human | Unknown | NM_004224 | X | | | |
| Class A Orphan | GPCR | GPR52 | Human | Unknown | NM_005684 | X | | | |
| Class A Orphan | GPCR | GPR6 | Human | Unknown | NM_005284 | X | | | |
| Class A Orphan | GPCR | GPR61 | Human | Unknown | NM_031936 | X | | | |
| Class A Orphan | GPCR | GPR65 | Human | Unknown | NM_003608 | X | | | |
| Class A Orphan | GPCR | GPR75 | Human | Unknown | NM_006794 | X | | | |
| Class A Orphan | GPCR | GPR78 | Human | Unknown | NM_080819 | X | | | |
| Class A Orphan | GPCR | GPR79 | Human | Unknown | NM_001272 | X | | | |
| Class A Orphan | GPCR | GPR83 | Human | Unknown | NM_016540 | X | | | |
| Class A Orphan | GPCR | GPR85 | Human | Unknown | NM_018970 | X | | | |
| Class A Orphan | GPCR | GPR88 | Human | Unknown | NM_022049 | X | | | |
| Class A Orphan | GPCR | LGR4 | Human | Unknown | NM_018490 | X | | | |
| Class A Orphan | GPCR | LGR5 | Human | Unknown | NM_003667 | X | | | |
| Class A Orphan | GPCR | LGR6 | Human | Unknown | XM_097508 | X | | | |
| Class A Orphan | GPCR | MRGPRD | Human | Unknown | NM_198923 | X | | | |
| Class A Orphan | GPCR | MRGPRE | Human | Unknown | XM_171536 | X | | | |
| Class A Orphan | GPCR | MRGPRF | Human | Unknown | NM_145015 | X | | | |
| Class A Orphan | GPCR | MRGPRX1 | Human | Gq | NM_147199 | X | | X | |
| Class A Orphan | GPCR | MRGPRX4 | Human | Unknown | NM_054032 | X | | | |
| Class A Orphan | GPCR | OPN5 | Human | Unknown | NM_181744.2 | X | | | |
| Class A Orphan | GPCR | OXGR1 | Human | Gq | NM_080818.3 | X | | | |
| Class A Orphan | GPCR | P2RY8 | Human | Unknown | NM_178129 | X | | | |
| Class A Orphan | GPCR | TAAR5 | Human | Unknown | NM_003967.2 | X | | | |
| Class A Orphan | GPCR | mGPR1 | Mouse | Unknown | NM_146250 | X | | | |
| Class A Orphan | GPCR | mGPR120 | Mouse | Unknown | NM_181748 | X | | | |
| Class B Orphan | GPCR | BAI1 | Human | unknown | NM_001702.2 | X | | | |
| Class B Orphan | GPCR | BAI2 | Human | unknown | NM_001703.2 | X | | | |
| Class B Orphan | GPCR | BAI3 | Human | unknown | NM_001704.2 | X | | | |
| Class B Orphan | GPCR | GPR123 | Human | Unknown | NM_001083909 | X | | | |
| Class B Orphan | GPCR | GPR157 | Human | Unknown | NM_024980 | X | | | |
| Class B Orphan | GPCR | GPR97 | Human | Unknown | NM_170776 | X | | | |
| Corticotropin | GPCR | CRF1 | Human | Gs | AY457172 | X | X | | X |
| Corticotropin | GPCR | CRF2 | Human | Gs | AY449734 | X | X | | |
| Corticotropin | GPCR | mCRF1 | Mouse | Gs | NM_007762 | X | | | |
| Dopamine | GPCR | D1 | Human | Gs | NM_000794.3 | X | X | | |
| Dopamine | GPCR | D2L | Human | Gi/Go | NM_000795.3 | X | X | | |
| Dopamine | GPCR | D2S | Human | Gi/Go | NM_016574.3 | X | X | | |
| Dopamine | GPCR | D3 | Human | Gi/Go | NM_000796.3 | X | | | |
| Dopamine | GPCR | D4 | Human | Gi/Go | NM_000797.2 | X | X | | |
| Dopamine | GPCR | D5 | Human | Gs | NM_000798.3 | X | X | | |
| Dopamine | GPCR | mDRD5 | Mouse | Gs | NM_013503.2 | X | | | |
| Dopamine | GPCR | rD2L | Rat | Gi/Go | NM_012547.1 | X | | | |
| Dopamine | GPCR | rD2S | Rat | Gi/Go | NM_016574.3 | X | | | |
| Dopamine | GPCR | rD5 | Rat | Gs | NM_000798.3 | X | | | |
| Endothelin | GPCR | ETA | Human | Gq | AY275462 | X | | X | |
| Endothelin | GPCR | ETB | Human | Gs & Gi/Go | NM_000115.2 | X | | | X |
| Endothelin | GPCR | mETA | Mouse | Gq | NM_010332.2 | X | | | |
| Endothelin | GPCR | mETB | Mouse | Gi/Go & Gs | NM_007904.3 | X | | | |
| Estrogen (G protein coupled) receptor | GPCR | GPER | Human | Gi/Go & Gs | NM_001505 | X | | | |
| Formylpeptide | GPCR | FPR1 | Human | Gi/Go | NM_002029 | X | X | | X |
| Formylpeptide | GPCR | FPR2/ALX | Human | Gi/Go | AY225226 | X | X | | X |
| Formylpeptide | GPCR | mFPR1 | Mouse | Gq | NM_013521.2 | X | | | |
| Free Fatty Acid | GPCR | FFA1 | Human | Gq | NM_005303.2 | X | | X | |
| Free Fatty Acid | GPCR | GPR43 | Human | Gq & Gi/Go | NM_005306.2 | | | X | |
| Free Fatty Acid | GPCR | GPR41 | Human | Gi/Go | NM_005304.3 | | X | | |
| GABAB | GPCR | GABB1 | Human | N/A | NM_021903.2 | | X | | |
| Galanin | GPCR | GALR1 | Human | Gi/Go | AY541036 | X | X | | X |
| Galanin | GPCR | GALR2 | Human | Gq & Gs | NM_003857 | X | X | X | |
| Galanin | GPCR | mGALR2 | Mouse | Gi/Go | NM_010254.4 | X | | | |
| Ghrelin | GPCR | ghrelin | Human | Gq | NM_198407 | X | | X | |
| Ghrelin | GPCR | ghrelin | Mouse | Gq | NM_177330 | X | | | |
| Glucagon | GPCR | glucagon | Human | Gs | NM_000160 | X | X | | X |
| Glucagon | GPCR | GHRH | Human | Gs | NM_000823.2 | | X | | |
| Glucagon | GPCR | GIP | Human | Gs | NM_000164 | X | X | | X |
| Glucagon | GPCR | GLP-1 | Human | Gs | BC112126 | X | X | | X |
| Glucagon | GPCR | GLP-2 | Human | Gs | NM004246.1 | X | X | | X |
| Glucagon | GPCR | secretin | Human | Gs | AY462218 | X | X | | X |
| Glucagon | GPCR | glucagon | Mouse | Gs | NM_008101.2 | X | | | |
| Glucagon | GPCR | mGIP | Mouse | Gs | NM_001080815.1 | X | | | |
| Glucagon | GPCR | mGLP-1 | Mouse | Gs | NM_021332 | X | | | |
| Glutamate | GPCR | mGlu1 | Human | Gq | NM_000838.2 | | | X | |
| Glutamate | GPCR | mGlu2 | Human | Gi/Go | NM_000839 | | X | | |
| Glutamate | GPCR | MGlu3 | Human | Gi/Go | NM_000840.2 | | X | | |
| Glutamate | GPCR | mGlu4 | Human | Gi/Go | NM_000841 | | X | | |
| Glutamate | GPCR | mGlu6 | Human | Gi/Go | NM_000843 | | X | | |
| Glycoprotein hormone receptor | GPCR | FSHR | Human | Gs | NM_000145 | X | X | | |
| Glycoprotein hormone receptor | GPCR | LH | Human | Gs | NM_000233 | X | X | | |
| Glycoprotein hormone receptor | GPCR | TSH | Human | Gs | NM_000369.2 | X | X | | |
| Gonadotropin-releasing hormone | GPCR | GnRH | Human | Gq | NM_000406.2 | | | X | |
| Histamine | GPCR | H1 | Human | Gq | AY136743 | X | | X | |
| Histamine | GPCR | H2 | Human | Gs | AY136744 | X | X | | |
| Histamine | GPCR | H3 | Human | Gi/Go | NM_007232 | X | X | | |
| Histamine | GPCR | H4 | Human | Gi/Go | NM_021624 | X | | | |
| Hydroxycarboxylic acid | GPCR | HCA2 | Human | Gi/Go | NM_177551 | X | X | | |
| Hydroxycarboxylic acid | GPCR | HCA3 | Human | Gi/Go | NM_006018 | X | X | | |
| Hydroxycarboxylic acid | GPCR | HCA1 | Human | Gi/Go | NM_032554 | X | X | | |
| Kisspeptin receptor | GPCR | kisspeptin | Human | Gq | NM_032551 | X | | | |
| Leukotriene | GPCR | BLT1 | Human | Gi/Go & Gq | AY322535 | X | X | X | X |
| Leukotriene | GPCR | OXE | Human | Gi/Go | NM_148962.4 | | X | | |
| Leukotriene | GPCR | CYSLT2 | Human | Gq | NM_020377.2 | | | X | |
| Leukotriene | GPCR | mBLT1 | Mouse | Gi/Go & Gq | NM_008519.2 | X | | | |
| Lysophospholipid | GPCR | S1P1 | Human | Gi/Go | NM_001400 | X | X | | X |
| Lysophospholipid | GPCR | LPA1 | Human | Gi/Go | NM_001401.3 | X | | | X |
| Lysophospholipid | GPCR | S1P3 | Human | Gq | NM_005226 | X | | X | X |
| Lysophospholipid | GPCR | LPA2 | Human | Gq | AY322548 | X | | X | |
| Lysophospholipid | GPCR | S1P2 | Human | Gs | NM_004230.3 | X | | | X |
| Lysophospholipid | GPCR | S1P4 | Human | Gq | AY322537 | X | | | |
| Lysophospholipid | GPCR | LPA3 | Human | Gq | NM_012152.2 | X | | X | X |
| Lysophospholipid | GPCR | S1P5 | Human | Gi/Go | NM_030760.4 | X | | | |
| Lysophospholipid | GPCR | cS1P2 | Canine | Gs | XM_542076.2 | X | | | |
| Lysophospholipid | GPCR | mS1P1 | Mouse | Gi/Go | NM_007901 | X | | | |
| Lysophospholipid | GPCR | mS1P2 | Mouse | Gs | NM_010333.4 | X | | | |
| Lysophospholipid | GPCR | mS1P4 | Mouse | Gq | NM_010102.2 | X | | | |
| Lysophospholipid | GPCR | rS1P2 | Rat | Gs | NM_017192.2 | X | | | |
| Lysophospholipid | GPCR | sS1P2 | Simian | Gs | XM_001100481.1 | X | | | |
| Melanin-concentrating hormone | GPCR | MCH1 | Human | Gi/Go | AY562945 | X | X | | |
| Melanin-concentrating hormone | GPCR | MCH2 | Human | Gq | NM_000706.3 | X | | X | |
| Melanin-concentrating hormone | GPCR | MCH1 | Mouse | Gi/Go | NM_145132 | X | | | |
| Melanocortin | GPCR | MC1 | Human | Gs | NM_002386 | X | X | | |
| Melanocortin | GPCR | MC3 | Human | Gs | AY227893 | X | X | | X |
| Melanocortin | GPCR | MC4 | Human | Gs | AY236539 | X | X | | |
| Melanocortin | GPCR | MC5 | Human | Gs | NM_005913 | X | X | | |
| Melatonin | GPCR | MT1 | Human | Gi/Go | NM_005958 | X | X | | |
| Melatonin | GPCR | MT2 | Human | Gi/Go | NM_005959.3 | X | X | | |
| Motilin | GPCR | motilin | Human | Gq | AY603964 | X | | X | X |
| Neuromedin U | GPCR | NMU1 | Human | Gq | NM_006056 | X | | X | X |
| Neuropeptide B & W | GPCR | NPBW1 | Human | Gi/Go | NM_005285 | X | X | | |
| Neuropeptide B & W | GPCR | NPBW2 | Human | Gi/Go | NM_005286 | X | X | | |
| Neuropeptide F | GPCR | NPFF1 | Human | Gi/Go | NM_022146 | X | X | | |
| Neuropeptide F | GPCR | NPFF2 | Human | Gi/Go | NM_053036.2 | | X | | |
| Neuropeptide S | GPCR | NPS receptor | Human | Gq | NM_207172 | X | | | |
| Neuropeptide Y | GPCR | Y1 | Human | Gi/Go | AY548168 | X | X | | |
| Neuropeptide Y | GPCR | Y2 | Human | Gi/Go | AY236540 | X | X | X | X |
| Neuropeptide Y | GPCR | Y4 | Human | Gi/Go | AY268432 | X | X | | |
| Neuropeptide Y | GPCR | Y1 | Mouse | Gi/Go | NM_010934.4 | X | | | |
| Neuropeptide Y | GPCR | NPY2R | Mouse | Gi/Go & Gq | NM_008731.3 | X | | | |
| Neuropeptide Y | GPCR | Y4 | Mouse | Gi/Go | NM_008919.4 | X | | | |
| Neurotensin | GPCR | NTS1 | Human | Gq | AY429106 | X | | X | X |
| Non-signalling 7TM chemokine-binding proteins | GPCR | FY | Human | Unknown | NM_002027 | X | | | |
| Opioid | GPCR | δ | Human | Gi/Go | NM_000911 | X | X | | X |
| Opioid | GPCR | κ | Human | Gi/Go | AF498922 | X | X | | X |
| Opioid | GPCR | NOP | Human | Gi/Go | AY268428 | X | X | | |
| Opioid | GPCR | μ | Human | Gi/Go | NM_000914.3 | X | X | | X |
| Opioid | GPCR | δ (murine) | Mouse | Gi/Go | NM_013622.3 | X | | | |
| Opioid | GPCR | κ (murine) | Mouse | Gi/Go | NM_011011 | X | | | |
| Opioid | GPCR | μ (murine) | Mouse | Gi/Go | NM_001039652 | X | | | |
| Opioid | GPCR | μ | Rat | Gi/Go | NM_013071 | X | | | |
| Orexin | GPCR | OX1 | Human | Gq | NM_001525.2 | X | | X | X |
| Orexin | GPCR | OX2 | Human | Gq | AF041245 | X | | X | X |
| Orexin | GPCR | mOX1 | Mouse | Gq | AY062030 | X | | | |
| Other 7TM proteins | GPCR | GPR107 | Human | Unknown | NM_020960 | X | | | |
| Other 7TM proteins | GPCR | TM7SF1 | Human | Unknown | NM_003272 | X | | | |
| Other 7TM proteins | GPCR | GPR143 | Human | Unknown | NM_000273 | X | | | |
| P2Y | GPCR | P2RY1 | Human | Gq | NM_002563.2 | X | | X | |
| P2Y | GPCR | P2Y11 | Human | Gs & Gq | AY449733 | X | | X | X |
| P2Y | GPCR | P2Y12 | Human | Gi/Go | AY136754 | X | | | |
| P2Y | GPCR | P2Y2 | Human | Gq | AY136753 | X | | X | X |
| P2Y | GPCR | P2Y4 | Human | Gq | NM_002565 | X | | X | X |
| P2Y | GPCR | P2Y6 | Human | Gq | NM_004154 | X | | | |
| P2Y | GPCR | mP2Y12 | Mouse | Gi/Go | NM_027571.3 | X | | | |
| P2Y | GPCR | P2Y6 | Mouse | Gq | NM_183168.1 | X | | | |
| Parathyroid | GPCR | PTH1 | Human | Gs & Gq | AY449732 | X | X | X | X |
| Parathyroid | GPCR | PTH2 | Human | Gs | AY497546 | X | X | X | X |
| Peptide P518 receptor | GPCR | QRFPR | Human | Gq | NM_198179 | X | | X | |
| Platelet-activating factor | GPCR | PAF | Human | Gi/Go & Gq | AY275466 | X | X | X | X |
| Platelet-activating factor | GPCR | mPAF | Mouse | Gi/Go & Gq | NM_001081211.1 | X | | | |
| Prokineticin | GPCR | PKR1 | Human | Gs & Gq | NM_138964 | X | X | X | X |
| Prokineticin | GPCR | PKR2 | Human | Gs | NM_144773 | X | | | X |
| Prokineticin | GPCR | rPROKR1 | Rat | Gs & Gq | | X | | | |
| Prokineticin | GPCR | rPKR2 | Rat | Gs | NM_138978 | X | | | |
| Prolactin releasing peptide receptor | GPCR | PRRP | Human | Gq | NM_004248 | X | | X | X |
| Prostanoid | GPCR | EP2 | Human | Gs | AY275471 | X | | | |
| Prostanoid | GPCR | EP3 | Human | Gi/Go & Gq | NM_198716 | X | X | X | |
| Prostanoid | GPCR | EP4 | Human | Gs | AY429109 | X | | | X |
| Prostanoid | GPCR | FP | Human | Gq | NM_000959.3 | X | | X | X |
| Prostanoid | GPCR | IP1 | Human | Gs | AY242134 | X | X | | X |
| Prostanoid | GPCR | TP | Human | Gq | NM_001060 | X | | X | |
| Prostanoid | GPCR | DP2 | Human | Gi/Go | AY507142 | X | X | | |
| Prostanoid | GPCR | DP1 | Human | Gs | NM_000953 | | X | | |
| Prostanoid | GPCR | EP1 | Human | Gq | NM_000955.2 | X | | X | |
| Prostanoid | GPCR | mDP2 | Mouse | Gi/Go | NM_009962.2 | X | | | |
| Prostanoid | GPCR | rGPR44 | Rat | Gi/Go | NM_001012070.1 | X | | | |
| Protease activated | GPCR | PAR1 | Human | Gi/Go | BC002464 | X | | X | |
| Protease activated | GPCR | PAR2 | Human | Gi/Go & Gq | NM_005242.4 | X | | X | X |
| Protease activated | GPCR | PAR4 | Human | Gi/Go & Gq | AY431102 | X | | X | X |
| Relaxin | GPCR | RXFP1 | Human | Gs | NM_021634.2 | | X | | |
| Relaxin | GPCR | RXFP3 | Human | Gi/Go | NM_016568.2 | X | X | | |
| Relaxin | GPCR | RXFP4 | Human | Gi/Go | NM_181885.2 | X | X | X | |
| Somatostatin | GPCR | SST1 | Human | Gi/Go | NM_001049 | X | | | |
| Somatostatin | GPCR | SST2 | Human | Gi/Go | AY236542 | X | X | | X |
| Somatostatin | GPCR | SST3 | Human | Gi/Go | AY322541 | X | X | | |
| Somatostatin | GPCR | SST4 | Human | Gi/Go | AY548169 | X | X | | |
| Somatostatin | GPCR | SST5 | Human | Gi/Go | NM_001053 | X | X | | |
| Somatostatin | GPCR | mSST2 | Mouse | Gi/Go | NM_001042606.1 | X | | | |
| Somatostatin | GPCR | mSRIF1B | Mouse | Gi/Go | NM_011425.2 | X | | | |
| Tachykinin | GPCR | NK1 | Human | Gq | NM_001058 | X | | X | X |
| Tachykinin | GPCR | NK2 | Human | Gq | AY322545 | X | | X | X |
| Tachykinin | GPCR | NK3 | Human | Gs & Gq | NM_001059 | X | X | X | X |
| TRH | GPCR | TRH1 | Human | Gq | AY493373 | X | | X | |
| Urotensin | GPCR | UT | Human | Gq | NM_018949 | X | | X | X |
| Urotensin | GPCR | mUT | Mouse | Gq | NM_145440 | X | | | |
| Vasopressin and Oxytocin | GPCR | V1A | Human | Gq | NM_000706.3 | X | | X | X |
| Vasopressin and Oxytocin | GPCR | V1B | Human | Gq | NM_000707.3 | X | | X | X |
| Vasopressin and Oxytocin | GPCR | V2 | Human | Gs | NM_000054.4 | X | X | | X |
| Vasopressin and Oxytocin | GPCR | OT | Human | Gq | AY389507 | X | | X | X |
| Vasopressin and Oxytocin | GPCR | mOT | Mouse | Gq | NM_001081147.1 | X | | | |
| VIP and PACAP | GPCR | PAC1 | Human | Gs & Gq | AY366498 | X | X | X | X |
| VIP and PACAP | GPCR | VPAC1 | Human | Gs & Gq | NM_004624 | X | X | | X |
| VIP and PACAP | GPCR | VPAC2 | Human | Gs | NM_003382 | X | X | | X |
| VIP and PACAP | GPCR | mPAC1 | Mouse | Gs & Gq | NM_001025372.1 | X | | | |
| VIP and PACAP | GPCR | mVPAC1 | Mouse | Gs | NM_011703.4 | X | | | |