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G PROTEIN
STRUCTURE
RECEPTOR
OTHER PROTEINS
STRUCTURE LIGAND
ENDOGENOUS LIGAND
REFERENCE
Fam. α Species Note % of Seq β Species γ Species Method
PDB
Refined
structure
Resolution
UniProt
IUPHAR Receptor family Class Species Receptor fusion Antibodies Other Name Type Function Name Type Last author Reference PDB Date
Gi/o αo Human - 59 β1 Human γ2 Human cryo-EM 6G79 - 3.8 5HT1B 5-HT1B 5-Hydroxytryptamine A (Rhodopsin) Human - - - Donitriptan pubchem
small molecule Agonist 5-hydroxytryptamine,... small molecule Tate CG 10.1038/S41586-018-0241-9 2018-06-20 132
Gi/o αo Human - 60 β1 Mouse γ2 Human cryo-EM 6K41 - 2.9 ADA2B α2B Adrenoceptors A (Rhodopsin) Human T4-Lysozyme scFv - Dexmedetomidine pubchem
small molecule Agonist (-)-adrenaline, (-)-... small molecule Kobilka BK 10.1038/S41589-020-0492-2 2020-04-15 138
Gi/o αi1 Human Non-canonical conformation 62 β1 Human γ2 Human cryo-EM 6OSA 6OSA_refined 3.0 NTR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem
peptide Agonist large neurotensin, n... protein Skiniotis G 10.1038/S41586-019-1337-6 2019-07-10 101
Gs αs Human - 49 β1 Human γ2 Human cryo-EM 6B3J 6B3J_refined 3.3 GLP1R GLP-1 Glucagon B1 (Secretin) Human - - - Exendin-P5
peptide Agonist glucagon-like peptid... peptide Wootten D 10.1038/NATURE25773 2018-02-21 11
Gs αs Bovine - 56 β1 Rat γ2 Bovine cryo-EM 6NBI - 4.0 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - Long-acting parathyr...
peptide Agonist PTHrP, TIP39, PTH, P... protein Zhang Y 10.1126/SCIENCE.AAV7942 2019-04-17 80
Gs αs Human - 58 β1 Human γ2 Human cryo-EM 6PB1 6PB1_refined 2.8 CRFR2 CRF2 Corticotropin-releasing factor B1 (Secretin) Human - Nanobody-35 - Urocortin pubchem chembl_ligand
peptide Agonist urocortin 2, cortico... peptide Xu HE 10.1016/J.MOLCEL.2020.01.013 2020-02-12 29
Gi/o αo Human - 59 β1 Rat γ2 Mouse cryo-EM 6WWZ 6WWZ_refined 3.3 CCR6 CCR6 Chemokine A (Rhodopsin) Human - scFv16 - C-C motif chemokine ...
protein Agonist CCL20, beta-defensin... protein Wu H 10.1038/S41467-020-16820-6 2020-06-24 141
Gq/11 α11 Human - 63 β1 Human γ2 Human cryo-EM 6OIJ 6OIJ_refined 3.3 ACM1 M1 Acetylcholine (muscarinic) A (Rhodopsin) Human - Antibody fragment - Iperoxo pubchem
small molecule Agonist acetylcholine small molecule Kobilka BK 10.1126/SCIENCE.AAW5188 2019-05-08 150
Gi/o αi1 Human - 64 β1 Human γ2 Human cryo-EM 6VMS 6VMS_refined 3.8 DRD2 D2 Dopamine A (Rhodopsin) Human T4-Lysozyme scFv16 - Bromocriptine pubchem
small molecule Agonist dopamine small molecule Rosenbaum DM 10.1038/S41586-020-2379-5 2020-06-17 125
Gs αs Human Mini-Gs 61 β1 Human γ2 Human cryo-EM 6LI3 6LI3_refined 3.3 GPR52 GPR52 A orphans A (Rhodopsin) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Xu F 10.1038/S41586-020-2019-0 2020-02-26 32
Gi/o αi1 Human - 100 β1 Human γ2 Human cryo-EM 6PT0 - 3.2 CNR2 CB2 Cannabinoid A (Rhodopsin) Human - scFv16 - Win 55212-2 pubchem chembl_ligand
small molecule Agonist 2-arachidonoylglycer... small molecule Xie X 10.1016/J.CELL.2020.01.007 2020-02-12 113
Gs αs Human - 56 β1 Human γ2 Human cryo-EM 6WPW 6WPW_refined 3.1 GLR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - Glucagon derivative ...
peptide Agonist glucagon peptide Kobilka BK 10.1126/SCIENCE.ABA3373 2020-08-12 56
Gi/o αi1 Human - 62 β1 Human γ2 Human cryo-EM 6N4B 6N4B_refined 3.0 CNR1 CB1 Cannabinoid A (Rhodopsin) Human - scFv16 - Fub-mdmb pubchem
small molecule Agonist 2-arachidonoylglycer... small molecule Skiniotis G 10.1016/J.CELL.2018.11.040 2019-01-30 92
Gi/o αi1 Human - 100 β1 Human γ2 Human cryo-EM 6OT0 6OT0_refined 3.9 SMO SMO Frizzled F (Frizzled) Human - Fab light chain
Fab heavy chain
- 24,25-Epoxy-choleste... pubchem
small molecule Agonist constitutive constitutive Li X 10.1038/S41586-019-1286-0 2019-06-12 95
Gs αs Human Engineered G protein 50 - - - - X-ray 5G53 5G53_refined 3.4 AA2AR A2A Adenosine A (Rhodopsin) Human - - - NECA pubchem
small molecule Agonist adenosine small molecule Tate CG 10.1038/NATURE18966 2016-08-03 1
Gs αs Human - 61 β1 Human γ2 Human cryo-EM 6WZG 6WZG_refined 2.3 SCTR secretin Glucagon B1 (Secretin) Human - Nanobody-35 - Secretin pubchem chembl_ligand
peptide Agonist VIP, secretin peptide Miller LJ 10.1038/S41467-020-17791-4 2020-08-12 62
Gs αs Human - 49 β1 Human γ2 Human cryo-EM 6P9Y 6P9Y_refined 3.0 PACR PAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - Pituitary adenylate ... pubchem
peptide Agonist VIP, PACAP-27, PACAP... peptide Wootten D 10.1016/J.MOLCEL.2020.01.012 2020-02-05 23
Gi/o αi2 Human - 59 β1 Human γ2 Human cryo-EM 6D9H 6D9H_refined 3.6 AA1R A1 Adenosine A (Rhodopsin) Human - - - Adenosine pubchem
small molecule Agonist adenosine small molecule Christopoulos A 10.1038/S41586-018-0236-6 2018-06-20 128
Gs αs Human - 43 β1 Human γ2 Human cryo-EM 6NIY 6NIY_refined 3.3 CALCR CT Calcitonin B1 (Secretin) Human - - - PEP
peptide Agonist adrenomedullin, amyl... peptide Sexton PM 10.1021/ACSPTSCI.8B00056 2019-01-23 5
Gs αs Human - 48 β1 Human γ2 Human cryo-EM 6UUS - 2.4 CALRL calcitonin-like Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP3
- Adrenomedullin pubchem
peptide Agonist adrenomedullin, &alp... peptide Sexton PM 10.1021/ACSPTSCI.9B00080 2020-04-01 38
Gs αs Bovine - 89 β1 Rat γ2 Bovine X-ray 3SN6 3SN6_refined 3.2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human T4-Lysozyme Antibody - BI-167107 pubchem
small molecule Agonist (-)-adrenaline, (-)-... small molecule Kobilka BK 10.1038/NATURE10361 2011-07-20 71
Gs αs Human - 57 β1 Human γ2 Human cryo-EM 6GDG 6GDG_refined 4.1 AA2AR A2A Adenosine A (Rhodopsin) Human TrxA Nanobody - NECA pubchem
small molecule Agonist adenosine small molecule Tate CG 10.7554/ELIFE.35946 2018-05-16 14
Gs αs Human - 48 β1 Human γ2 Human cryo-EM 6E3Y 6E3Y_refined 3.3 CALRL calcitonin-like Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP1
- Calcitonin gene-rela... pubchem
peptide Agonist adrenomedullin, &alp... peptide Sexton PM 10.1038/S41586-018-0535-Y 2018-09-19 20
Gs αs Bovine - 58 β1 Rat γ2 Bovine cryo-EM 6NBF 6NBF_refined 3.0 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - Long-acting parathyr...
peptide Agonist PTHrP, TIP39, PTH, P... protein Zhang Y 10.1126/SCIENCE.AAV7942 2019-04-17 74
Gs αs Human - 57 β1 Rat γ2 Bovine cryo-EM 6LPB 6LPB_refined 3.9 PACR PAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - Pituitary adenylate ... pubchem
peptide Agonist VIP, PACAP-27, PACAP... peptide Nureki O 10.1038/S41594-020-0386-8 2020-03-11 47
Gi/o αi1 Human - 64 β1 Human γ2 Human cryo-EM 6KPG 6KPG_refined 3.0 CNR1 CB1 Cannabinoid A (Rhodopsin) Human - scFv16 - (6Ar,9R,10aR)-9-(hyd... pubchem
small molecule Agonist 2-arachidonoylglycer... small molecule Liu Z 10.1016/J.CELL.2020.01.008 2020-02-12 107
Gs αs Human Gs-Gi1 chimera 58 β1 Human γ2 Human cryo-EM 6PB0 6PB0_refined 3.0 CRFR1 CRF1 Corticotropin-releasing factor B1 (Secretin) Human - Nanobody-35 - Urocortin pubchem chembl_ligand
peptide Agonist urocortin 2, cortico... peptide Xu HE 10.1016/J.MOLCEL.2020.01.013 2020-02-12 26
Gi/o αo Human - 61 β1 Human γ2 Human cryo-EM 6OIK 6OIK_refined 3.6 ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human - - - Iperoxo pubchem
LY2119620 pubchem
small molecule
small molecule
Agonist
PAM
acetylcholine small molecule Kobilka BK 10.1126/SCIENCE.AAW5188 2019-05-08 135
Gi/o αi1 Human - 61 β1 Human γ2 Human cryo-EM 6OMM 6OMM_refined 3.2 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human - - - WKYMVX
peptide Agonist annexin I, humanin, ... protein Zhang C 10.1038/S41467-020-14728-9 2020-02-26 116
Gi/o αi1 Human - 62 β1 Mouse γ2 Human cryo-EM 6K42 6K42_refined 4.1 ADA2B α2B Adrenoceptors A (Rhodopsin) Human T4-Lysozyme scFv - Dexmedetomidine pubchem
small molecule Agonist (-)-adrenaline, (-)-... small molecule Kobilka BK 10.1038/S41589-020-0492-2 2020-04-15 122
Gs αs Human - 57 β1 Human γ2 Human cryo-EM 6VCB 6VCB_refined 3.3 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Glucagon-like peptid...
LSN3160440 pubchem
peptide
small molecule
Agonist
PAM
glucagon-like peptid... peptide Sloop KW 10.1038/S41589-020-0589-7 2020-07-22 50
Gs αs Human - 48 β1 Human γ2 Human cryo-EM 6UUN 6UUN_refined 3.0 CALRL calcitonin-like Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP2
- Adrenomedullin pubchem
peptide Agonist adrenomedullin, &alp... peptide Sexton PM 10.1021/ACSPTSCI.9B00080 2020-03-25 35
Gs αs Human - 56 β1 Human γ2 Human cryo-EM 6M1I 6M1I_refined 3.5 PACR PAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - PACAP pubchem
peptide Agonist VIP, PACAP-27, PACAP... peptide Ma Y 10.1038/S41422-020-0280-2 2020-03-11 68
Gi/o αt1 Bovine - 59 β1 Bovine γT1 Bovine cryo-EM 6OYA 6OYA_refined 3.3 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - Camelid antibody VHH fragment - Retinal (all-trans) pubchem
small molecule Agonist Retinal small molecule Skiniotis G 10.1016/J.MOLCEL.2019.06.007 2019-07-24 147
Gs αs Human - 48 β1 Human γ2 Human cryo-EM 6UVA - 2.3 CALRL calcitonin-like Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP3
- Adrenomedullin-2
peptide Agonist adrenomedullin, &alp... peptide Sexton PM 10.1021/ACSPTSCI.9B00080 2020-04-01 41
Gs αs Human - 47 β1 Human γ2 Human cryo-EM 5UZ7 5UZ7_refined 4.1 CALCR CT Calcitonin B1 (Secretin) Human - - - - - - adrenomedullin, amyl... peptide Sexton PM 10.1038/NATURE22327 2017-05-03 2
Gs αs Human - 56 β1 Human γ2 Human cryo-EM 6WHC 6WHC_refined 3.4 GLR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - Dual-agonist peptide...
peptide Agonist glucagon peptide Sexton PM 10.1074/JBC.RA120.013793 2020-05-27 53
Gi/o αi1 Human - 62 β1 Human γ2 Human cryo-EM 6KPF - 2.9 CNR2 CB2 Cannabinoid A (Rhodopsin) Human - scFv16 - (6Ar,9R,10aR)-9-(hyd... pubchem
small molecule Agonist 2-arachidonoylglycer... small molecule Liu Z 10.1016/J.CELL.2020.01.008 2020-02-12 110
Gi/o αi1 Human - 62 β1 Human γ2 Human cryo-EM 6OS9 6OS9_refined 3.0 NTR1 NTS1 Neurotensin A (Rhodopsin) Human - scFv16 - JMV449 pubchem
peptide Agonist large neurotensin, n... protein Skiniotis G 10.1038/S41586-019-1337-6 2019-07-10 98
Gs αs Human - 49 β1 Human γ2 Human cryo-EM 6WI9 6WI9_refined 4.3 SCTR secretin Glucagon B1 (Secretin) Human - Nanobody-35 - Secretin pubchem chembl_ligand
peptide Agonist VIP, secretin peptide Miller LJ 10.1038/S41467-020-17791-4 2020-08-12 59
Gi/o αi1 Human - 61 β1 Human γ2 Human cryo-EM 6DDF 6DDF_refined 3.5 OPRM μ Opioid A (Rhodopsin) Mouse - - - DAMGO pubchem chembl_ligand
peptide Agonist [Leu]enkephalin, [Me... peptide Kobilka BK 10.1038/S41586-018-0219-7 2018-06-13 86
Gs αs Human - 59 β1 Rat γ2 Bovine cryo-EM 5VAI 5VAI_refined 4.1 G1SGD4 GLP-1 Glucagon B1 (Secretin) Rabbit - - - GLP-1 pubchem
peptide Agonist glucagon-like peptid... peptide Skiniotis G 10.1038/NATURE22394 2017-05-24 8
Gi/o αi1 Human - 100 β1 Rat γ2 Bovine cryo-EM 6CMO 6CMO_refined 4.5 OPSD Rhodopsin Opsins A (Rhodopsin) Human BRIL Fab - Apo (no ligand)
none Apo (no ligand) Retinal small molecule Xu HE 10.1038/S41586-018-0215-Y 2018-06-20 89
Gs αs Human - 59 β1 Human γ2 Human cryo-EM 6LMK 6LMK_refined 3.7 GLR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - Glucagon
peptide Agonist glucagon peptide Wu B 10.1126/SCIENCE.AAZ5346 2020-04-01 44
Gi/o αo Human mini-Go 51 - - - - X-ray 6FUF 6FUF_refined 3.1 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - Retinal (all-trans) pubchem
small molecule Agonist Retinal small molecule Schertler GFX 10.1126/SCIADV.AAT7052 2018-10-03 131
Gs αs Bovine - 57 β1 Rat γ2 Bovine cryo-EM 6NBH 6NBH_refined 3.5 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - Long-acting parathyr...
peptide Agonist PTHrP, TIP39, PTH, P... protein Zhang Y 10.1126/SCIENCE.AAV7942 2019-04-17 77
Gi/o αi1 Human - 61 β1 Human γ2 Human cryo-EM 6DDE 6DDE_refined 3.5 OPRM μ Opioid A (Rhodopsin) Mouse - Antibody - DAMGO pubchem chembl_ligand
peptide Agonist [Leu]enkephalin, [Me... peptide Kobilka BK 10.1038/S41586-018-0219-7 2018-06-13 83
Gs αs Human - 54 β1 Human γ2 Human cryo-EM 6M1H 6M1H_refined 3.6 PACR PAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - Maxadilan pubchem
peptide Agonist VIP, PACAP-27, PACAP... peptide Ma Y 10.1038/S41422-020-0280-2 2020-03-11 65
Gi/o αi1 Human - 60 β1 Bovine γT1 Bovine cryo-EM 6QNO 6QNO_refined 4.4 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - Fab antibody fragment light chain
Fab antibody fragment heavy chain
- Retinal (all-trans) pubchem
small molecule Agonist Retinal small molecule Schertler G 10.7554/ELIFE.46041 2019-07-10 104
Gi/o αt1 Bovine - 64 β1 Bovine γT1 Bovine cryo-EM 6OY9 6OY9_refined 3.9 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - Retinal (all-trans) pubchem
small molecule Agonist Retinal small molecule Skiniotis G 10.1016/J.MOLCEL.2019.06.007 2019-07-24 144
Gi/o αi1 Human - 63 β1 Human γ2 Human cryo-EM 6LML 6LML_refined 3.9 GLR glucagon Glucagon B1 (Secretin) Human - scFv16 - Glucagon
peptide Agonist glucagon peptide Wu B 10.1126/SCIENCE.AAZ5346 2020-04-01 119
Gs αs Human - 59 β1 Human γ2 Human cryo-EM 6NI3 6NI3_refined 3.8 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - Nanobody-35 - 5-Hydroxy-8-[(1R)-1-... pubchem
small molecule Agonist (-)-adrenaline, (-)-... small molecule Lefkowitz RJ 10.1038/S41594-019-0330-Y 2019-11-20 17