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G PROTEIN
STRUCTURE
RECEPTOR
OTHER PROTEINS
STRUCTURE LIGAND
PHYSIOLOGICAL 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 Authors Reference PDB Date
Gi/o αt1 Bovine Only H5 3 - - - - X-ray 3DQB 3DQB_refined 3.2 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - Apo (no ligand)
none Apo (no ligand) - - Scheerer P, Park JH, Hildebrand PW, Kim YJ, Krauss N, Choe HW, Hofmann KP, Ernst OP 10.1038/NATURE07330 2008-09-23
Gi/o αt1 Bovine Only H5 3 - - - - X-ray 3PQR 3PQR_refined 2.9 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - Retinal (all-trans) pubchem
small-molecule Agonist - - Choe HW, Kim YJ, Park JH, Morizumi T, Pai EF, Krauss N, Hofmann KP, Scheerer P, Ernst OP 10.1038/NATURE09789 2011-03-09
Gi/o αt1 Bovine Only H5 3 - - - - X-ray 2X72 2X72_refined 3.0 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - Retinal (all-trans) pubchem
small-molecule Agonist - - Standfuss J, Edwards PC, D'Antona A, Fransen M, Xie G, Oprian DD, Schertler GF 10.1038/NATURE09795 2011-03-16
Gi/o αt1 Bovine Only H5 3 - - - - X-ray 4X1H 4X1H_refined 2.3 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - B-Nonylglucoside pubchem
small-molecule unknown - - Blankenship E, Vahedi-Faridi A, Lodowski DT 10.1016/J.STR.2015.09.015 2015-11-04
Gi/o αt1 Bovine Only H5 3 - - - - X-ray 6NWE 6NWE_refined 2.7 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - B-Octylglucoside pubchem
small-molecule unknown - - - - 2020-02-12
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 - [Ac-His1]PACAP-27 gtoplig chembl_ligand pubchem
peptide Agonist PHM, PHV, VIP, PACAP-27, PHI, PACAP-38 peptide Kobayashi K, Shihoya W, Nishizawa T, Kadji FMN, Aoki J, Inoue A, Nureki O 10.1038/S41594-020-0386-8 2020-03-11
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7CFM - 3.0 GPBAR GPBA Bile acid A (Rhodopsin) Human - Nanobody-35 - CHEMBL2331646 chembl_ligand pubchem
small-molecule Agonist cholic acid, deoxycholic acid, chenodeoxycholic acid, lithocholic acid small-molecule - - 2020-09-09
Gi/o αi1 Human - 95 β1 Human γT1 Human Cryo-EM 7L0Q - 4.3 NTR1 NTS1 Neurotensin A (Rhodopsin) Rat - - - neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
peptide Agonist neuromedin N, neurotensin peptide Zhang M, Gui M, Wang ZF, Gorgulla C, Yu JJ, Wu H, Sun ZJ, Klenk C, Merklinger L, Morstein L, Hagn F, Pluckthun A, Brown A, Nasr ML, Wagner G 10.1038/S41594-020-00554-6 2021-01-06
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7E32 - 2.9 5HT1D 5-HT1D 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - 5-hydroxytryptamine pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist 5-hydroxytryptamine, 5-HT-moduline small-molecule Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen DD, Yen HY, Robinson CV, Harpsoe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE 10.1038/S41586-021-03376-8 2021-04-21
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7EZH - 3.2 CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human - scFv16 - CCK-8 pubchem gtoplig chembl_ligand drug_central drugbank
peptide Agonist CCK-8, desulfated cholecystokinin-8, CCK-39, CCK-58, CCK-33, CCK-4, gastrin-17 peptide Liu Q, Yang D, Zhuang Y, Croll TI, Cai X, Dai A, He X, Duan J, Yin W, Ye C, Zhou F, Wu B, Zhao Q, Xu HE, Wang MW, Jiang Y 10.1038/S41589-021-00841-3 2021-08-25
Gs αs Human Gs-Gq chimera 49 β1 Human γ2 Human Cryo-EM 7RMI - 3.2 NK1R NK1 Tachykinin A (Rhodopsin) Human - Nanobody-35 - substance P pubchem gtoplig chembl_ligand gtoplig gtoplig
peptide Agonist neuropeptide-γ, hemokinin 1, neurokinin A, neuropeptide K, neurokinin B, substance P peptide Harris JA, Faust B, Gondin AB, Damgen MA, Suomivuori CM, Veldhuis NA, Cheng Y, Dror RO, Thal DM, Manglik A 10.1038/S41589-021-00890-8 2021-11-03
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7RKN - 3.6 US28 US28 Unclassified A (Rhodopsin) strain AD169 - scFv16 - Fractalkine pubchem
peptide Agonist - - Tsutsumi N, Maeda S, Qu Q, Vogele M, Jude KM, Suomivuori CM, Panova O, Waghray D, Kato HE, Velasco A, Dror RO, Skiniotis G, Kobilka BK, Garcia KC 10.1126/SCIADV.ABL5442 2022-01-26
Gi/o αo Human - 61 β1 Human γ2 Human Cryo-EM 7EJ0 - 3.2 ADA2A α2A Adrenoceptors A (Rhodopsin) Human - scFv16 - (-)-noradrenaline pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist (-)-noradrenaline, (-)-adrenaline small-molecule Xu J, Cao S, Hubner H, Weikert D, Chen G, Lu Q, Yuan D, Gmeiner P, Liu Z, Du Y 10.1126/SCIADV.ABJ5347 2022-04-13
Gs αs Human Engineered G alpha 56 β1 Human γ2 Human Cryo-EM 7RA3 - 3.2 GIPR GIP Glucagon B1 (Secretin) Human - scFv16
Nanobody-35 		- gastric inhibitory polypeptide (human) - Incretin pubchem
peptide Agonist gastric inhibitory polypeptide peptide Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW 10.1073/PNAS.2116506119 2022-04-13
Gq/11 αq Human - 60 β1 Rat γ2 Bovine Cryo-EM 8XOR 8XOR_refined 3.0 PAR1 PAR1 Proteinase-activated A (Rhodopsin) Human - scFv16 - Tethered agonist
peptide Agonist thrombin peptide - - 2024-09-18
Gs αs Human - 57 β1 Human γ2 Human Cryo-EM 8YW3 8YW3_refined 2.7 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Retatrutide
peptide Agonist glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide peptide Li W, Zhou Q, Cong Z, Yuan Q, Li W, Zhao F, Xu HE, Zhao LH, Yang D, Wang MW 10.1038/S41421-024-00700-0 2024-09-18
Gs αs Human - 47 β1 Human γ2 Human Cryo-EM 5UZ7 - 4.1 CALCR CT Calcitonin B1 (Secretin) Human - - - calcitonin (salmon synthetic) pubchem
small-molecule Agonist calcitonin, adrenomedullin, amylin, α-CGRP, adrenomedullin 2/intermedin, β-CGRP peptide Liang YL, Khoshouei M, Radjainia M, Zhang Y, Glukhova A, Tarrasch J, Thal DM, Furness SGB, Christopoulos G, Coudrat T, Danev R, Baumeister W, Miller LJ, Christopoulos A, Kobilka BK, Wootten D, Skiniotis G, Sexton PM 10.1038/NATURE22327 2017-05-03
Gi/o αo Human - 59 β1 Human γ2 Human Cryo-EM 6G79 - 3.8 5HT1B 5-HT1B 5-Hydroxytryptamine A (Rhodopsin) Human - - - donitriptan pubchem gtoplig chembl_ligand
small-molecule Agonist 5-hydroxytryptamine, 5-HT-moduline, tryptamine small-molecule Garcia-Nafria J, Nehme R, Edwards PC, Tate CG 10.1038/S41586-018-0241-9 2018-06-20
Gs αs Human - 61 β1 Human γ2 Human Cryo-EM 6WZG 6WZG_refined 2.3 SCTR secretin Glucagon B1 (Secretin) Human - Nanobody-35 - SECRETIN chembl_ligand pubchem
protein Agonist VIP, secretin peptide Dong M, Deganutti G, Piper SJ, Liang YL, Khoshouei M, Belousoff MJ, Harikumar KG, Reynolds CA, Glukhova A, Furness SGB, Christopoulos A, Danev R, Wootten D, Sexton PM, Miller LJ 10.1038/S41467-020-17791-4 2020-08-12
Gi/o αi1 Human Non-canonical conformation 63 β1 Human γT1 Human Cryo-EM 7L0R - 4.2 NTR1 NTS1 Neurotensin A (Rhodopsin) Rat - - - neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
peptide Agonist neuromedin N, neurotensin peptide Zhang M, Gui M, Wang ZF, Gorgulla C, Yu JJ, Wu H, Sun ZJ, Klenk C, Merklinger L, Morstein L, Hagn F, Pluckthun A, Brown A, Nasr ML, Wagner G 10.1038/S41594-020-00554-6 2021-01-06
Gs αs Human - 86 β1 Human γ2 Human X-ray 7JOZ 7JOZ_refined 3.8 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - CHEMBL4453318 chembl_ligand pubchem
small-molecule Agonist L-NOREPINEPHRINE, noradrenaline, (-)-noradrenaline, 5-hydroxytryptamine, dopamine small-molecule Sun B, Feng D, Chu ML, Fish I, Lovera S, Sands ZA, Kelm S, Valade A, Wood M, Ceska T, Kobilka TS, Lebon F, Kobilka BK 10.1038/S41467-021-23519-9 2021-04-14
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7EW2 - 3.1 S1PR3 S1P3 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - (S)-FTY720-phosphate pubchem gtoplig chembl_ligand
small-molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine small-molecule Zhao C, Cheng L, Wang W, Wang H, Luo Y, Feng Y, Wang X, Fu H, Cai Y, Yang S, Fu P, Yan W, Shao Z 10.1038/S41422-021-00567-W 2021-09-29
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7NA7 7NA7_refined 2.7 GHSR ghrelin Ghrelin A (Rhodopsin) Human - Antibody fragment - Ghrelin-27
peptide Agonist [des-Gln14]ghrelin, ghrelin peptide Liu H, Sun D, Myasnikov A, Damian M, Baneres JL, Sun J, Zhang C 10.1038/S41467-021-26735-5 2021-12-15
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 7VGX 7VGX_refined 3.2 NPY1R Y1 Neuropeptide Y A (Rhodopsin) Human - scFv16 - neuropeptide Y pubchem gtoplig chembl_ligand gtoplig gtoplig pubchem pubchem pubchem
peptide Agonist peptide YY, pancreatic polypeptide, neuropeptide Y peptide Park C, Kim J, Ko SB, Choi YK, Jeong H, Woo H, Kang H, Bang I, Kim SA, Yoon TY, Seok C, Im W, Choi HJ 10.1038/S41467-022-28510-6 2022-02-23
Gs αs Bovine - 57 β1 Rat γ2 Bovine Cryo-EM 7FIM - 3.4 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - tirzepatide pubchem gtoplig
peptide Agonist glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide peptide Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW 10.1038/S41467-022-28683-0 2022-03-02
G12/13 α13 Human Gi2-mini-G13 chimera 56 β1 Human γ2 Human Cryo-EM 7SF7 - 2.9 AGRL3 ADGRL3 ADGRL B2 (Adhesion) Human - - - Apo (no ligand)
none Apo (no ligand) - - Barros-Alvarez X, Nwokonko RM, Vizurraga A, Matzov D, He F, Papasergi-Scott MM, Robertson MJ, Panova O, Yardeni EH, Seven AB, Kwarcinski FE, Su H, Peroto MC, Meyerowitz JG, Shalev-Benami M, Tall GG, Skiniotis G 10.1038/S41586-022-04575-7 2022-04-27
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7V68 - 3.4 ACM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - iperoxo pubchem gtoplig chembl_ligand
LY2119620 pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Agonist
PAM 		acetylcholine small-molecule Wang J, Wu M, Chen Z, Wu L, Wang T, Cao D, Wang H, Liu S, Xu Y, Li F, Liu J, Chen N, Zhao S, Cheng J, Wang S, Hua T 10.1038/S41467-022-30595-Y 2022-05-11
Gi/o αi1 Human - 60 β1 Human γ2 Human Cryo-EM 7WJ5 7WJ5_refined 3.7 SSR2 SST2 Somatostatin A (Rhodopsin) Human BRIL scFv16 - SOMATOSTATIN chembl_ligand pubchem
protein Agonist cortistatin-14, SRIF-14, CST-17, SRIF-28 peptide Heo Y, Yoon E, Jeon YE, Yun JH, Ishimoto N, Woo H, Park SY, Song JJ, Lee W 10.7554/ELIFE.76823 2022-07-13
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7XW5 - 3.0 TSHR TSH Glycoprotein hormone A (Rhodopsin) Human - Nanobody-35 - Glycoprotein hormones alpha chain
Thyrotropin subunit beta
N-[4-[[5-[(2S)-3-benzyl-5-hydroxy-4-oxo-1,2-dihydroquinazolin-2-yl]-2-methoxyphenyl]methoxy]phenyl]acetamide pubchem
protein
protein
small-molecule 		Agonist TSH peptide Duan J, Xu P, Luan X, Ji Y, He X, Song N, Yuan Q, Jin Y, Cheng X, Jiang H, Zheng J, Zhang S, Jiang Y, Xu HE 10.1038/S41586-022-05173-3 2022-08-24
Gi/o αo Human - 62 β1 Human γ2 Human Cryo-EM 7T96 7T96_refined 3.2 ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - acetylcholine pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
LY2119620 pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Agonist
PAM 		acetylcholine small-molecule - - 2023-01-25
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 7TRS - 2.8 ACM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - acetylcholine pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
small-molecule Agonist acetylcholine small-molecule - - 2023-05-17
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 8EJK - 3.4 FFAR1 FFA1 Free fatty acid A (Rhodopsin) Human - scFv16 - fasiglifam pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist oleic acid, α-linolenic acid, myristic acid, docosahexaenoic acid small-molecule Kumari P, Inoue A, Chapman K, Lian P, Rosenbaum DM 10.1073/PNAS.2219569120 2023-05-24
Gq/11 α11 Human - 63 β1 Human γ2 Human Cryo-EM 7XXH 7XXH_refined 2.9 P2RY1 P2Y1 P2Y A (Rhodopsin) Human - scFv16 - 2MeSADP pubchem gtoplig chembl_ligand gtoplig
small-molecule Agonist ATP, ADP small-molecule - - 2023-06-07
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8F0J - 2.0 CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - Pramlintide analogue San45
peptide Agonist calcitonin, adrenomedullin, amylin, α-CGRP, adrenomedullin 2/intermedin, β-CGRP peptide Cao J, Belousoff MJ, Gerrard E, Danev R, Fletcher MM, Dal Maso E, Schreuder H, Lorenz K, Evers A, Tiwari G, Besenius M, Li Z, Johnson RM, Wootten D, Sexton PM 10.1038/S41589-023-01393-4 2023-08-02
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8GDA 8GDA_refined 3.3 PE2R4 EP4 Prostanoid A (Rhodopsin) Human - - - (2S,5R)-5-[(1E,3S)-4,4-difluoro-3-hydroxy-4-phenylbut-1-en-1-yl]-1-[6-(1H-tetrazol-5-yl)hexyl]pyrrolidin-2-ol pubchem
small-molecule Agonist PGF2α, PGI2, PGD2, thromboxane A2, PGE1, PGE2 small-molecule Huang SM, Xiong MY, Liu L, Mu J, Wang MW, Jia YL, Cai K, Tie L, Zhang C, Cao S, Wen X, Wang JL, Guo SC, Li Y, Qu CX, He QT, Cai BY, Xue C, Gan S, Xie Y, Cong X, Yang Z, Kong W, Li S, Li Z, Xiao P, Yang F, Yu X, Guan YF, Zhang X, Liu Z, Yang BX, Du Y, Sun JP 10.1073/PNAS.2216329120 2024-01-10
Gi/o αo Human - 59 β1 Human γ2 Human Cryo-EM 8I9L - 3.2 C3AR C3a Complement peptide A (Rhodopsin) Human - scFv16 - C3a anaphylatoxin pubchem
peptide Agonist C5a, C3a peptide Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C 10.1016/J.CELL.2023.09.020 2023-10-18
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8KFY 8KFY_refined 3.1 CCR8 CCR8 Chemokine A (Rhodopsin) Human - scFv16 - ZK 756326 pubchem gtoplig chembl_ligand
small-molecule Agonist CCL8, CCL1 peptide Jiang S, Lin X, Wu L, Wang L, Wu Y, Xu Z, Xu F 10.1126/SCIADV.ADJ7500 2024-02-07
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8U4Q - 3.4 CXCR4 CXCR4 Chemokine A (Rhodopsin) Human - REGN7663 Fab light chain - REGN7663 Fab heavy chain
protein Agonist CXCL12α, CXCL12, CXCL12γ, CXCL12φ, CXCL12β, CXCL12δ, CXCL12ε peptide Saotome K, McGoldrick LL, Ho JH, Ramlall TF, Shah S, Moore MJ, Kim JH, Leidich R, Olson WC, Franklin MC 10.1038/S41594-024-01397-1 2024-03-13
Gq/11 αq Human - 63 β1 Human γ2 Human Cryo-EM 8ZJD - 3.1 KISSR kisspeptin Kisspeptin A (Rhodopsin) Human - scFv16 - Kisspeptin-10 pubchem
peptide Agonist kisspeptin-10, kisspeptin-54, kisspeptin-52, kisspeptin-14, kisspeptin-13 peptide - - 2024-07-03
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 9IJ9 - 2.7 T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human - - - Cholesterol pubchem
compound 28.1 [PMID: 36847646] pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Agonist
Allosteric agonist 		- - - - 2024-07-24
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8XWQ - 4.6 EDNRB ETB Endothelin A (Rhodopsin) Human - scFv16 - ENDOTHELIN chembl_ligand pubchem
protein Agonist endothelin-2, endothelin-3, endothelin-1 peptide Tani K, Maki-Yonekura S, Kanno R, Negami T, Hamaguchi T, Hall M, Mizoguchi A, Humbel BM, Terada T, Yonekura K, Doi T 10.1038/S42003-024-06905-Z 2024-10-02
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 6LML 6LML_refined 3.9 GLR glucagon Glucagon B1 (Secretin) Human - scFv16 - glucagon pubchem gtoplig chembl_ligand drugbank drug_central gtoplig pubchem pubchem pubchem pubchem
peptide Agonist glucagon peptide Qiao A, Han S, Li X, Li Z, Zhao P, Dai A, Chang R, Tai L, Tan Q, Chu X, Ma L, Thorsen TS, Reedtz-Runge S, Yang D, Wang MW, Sexton PM, Wootten D, Sun F, Zhao Q, Wu B 10.1126/SCIENCE.AAZ5346 2020-04-01
GPa1 family αPa1 strain ATCC 204508 / S288c Two alpha subunits bound to STE2 dimer 46 STE4 strain ATCC 204508 / S288c γ strain ATCC 204508 / S288c Cryo-EM 7AD3 - 3.5 STE2 STE2 STE2 D1 (Ste2-like fungal pheromone) strain ATCC 204508 / S288c - - - Alpha-factor mating pheromone pubchem
peptide Agonist - - Velazhahan V, Ma N, Pandy-Szekeres G, Kooistra AJ, Lee Y, Gloriam DE, Vaidehi N, Tate CG 10.1038/S41586-020-2994-1 2020-12-09
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7CKY - 3.2 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - CHEMBL3697578 chembl_ligand pubchem
small-molecule Agonist L-NOREPINEPHRINE, noradrenaline, (-)-noradrenaline, 5-hydroxytryptamine, dopamine small-molecule Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z 10.1016/J.CELL.2021.01.028 2021-03-03
Gs αs Human - 60 β1 Rat γ2 Bovine Cryo-EM 7DUR - 3.3 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - N-Tert-butyl-6,7-dichloroquinoxalin-2-amine pubchem
small-molecule Ago-PAM glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide peptide Cong Z, Chen LN, Ma H, Zhou Q, Zou X, Ye C, Dai A, Liu Q, Huang W, Sun X, Wang X, Xu P, Zhao L, Xia T, Zhong W, Yang D, Eric Xu H, Zhang Y, Wang MW 10.1038/S41467-021-24058-Z 2021-08-11
Gq/11 αq Human Gq-Gi1 chimera 62 β1 Human γ2 Human Cryo-EM 7F8W 7F8W_refined 3.1 GASR CCK2 Cholecystokinin A (Rhodopsin) Human - scFv16 - desulfated gastrin-17 pubchem gtoplig chembl_ligand pubchem
peptide Agonist CCK-8, desulfated cholecystokinin-8, gastrin-14, CCK-58, desulfated gastrin-17, CCK-39, CCK-33, desulfated gastrin-34, gastrin-34, gastrin-71, desulfated gastrin-71, CCK-4, desulfated gastrin-14, gastrin-17 peptide Zhang X, He C, Wang M, Zhou Q, Yang D, Zhu Y, Feng W, Zhang H, Dai A, Chu X, Wang J, Yang Z, Jiang Y, Sensfuss U, Tan Q, Han S, Reedtz-Runge S, Xu HE, Zhao S, Wang MW, Wu B, Zhao Q 10.1038/S41589-021-00866-8 2021-10-13
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7F4F - 2.9 MSHR MC1 Melanocortin A (Rhodopsin) Human - scFv16 - CHEMBL407070 chembl_ligand pubchem pubchem
protein Agonist γ-MSH, β-MSH, α-MSH, ACTH peptide Ma S, Chen Y, Dai A, Yin W, Guo J, Yang D, Zhou F, Jiang Y, Wang MW, Xu HE 10.1038/S41422-021-00557-Y 2021-09-08
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7TYN - 2.6 CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - calcitonin (salmon synthetic) pubchem
small-molecule Agonist calcitonin, adrenomedullin, amylin, α-CGRP, adrenomedullin 2/intermedin, β-CGRP peptide Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM 10.1126/SCIENCE.ABM9609 2022-03-30
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7EJX - 2.4 GPR88 GPR88 A orphans A (Rhodopsin) Human - scFv16 - compound 2 [PMID: 24793972] pubchem gtoplig chembl_ligand
small-molecule Allosteric agonist - - Chen G, Xu J, Inoue A, Schmidt MF, Bai C, Lu Q, Gmeiner P, Liu Z, Du Y 10.1038/S41467-022-30081-5 2022-04-13
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7F0T - 3.1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - dopamine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist L-NOREPINEPHRINE, noradrenaline, (-)-noradrenaline, 5-hydroxytryptamine, dopamine small-molecule Teng X, Chen S, Wang Q, Chen Z, Wang X, Huang N, Zheng S 10.1126/SCIADV.ABO4158 2022-06-15
Gq/11 αq Human Gi2-mini-Gq chimera 60 β1 Human γ2 Human Cryo-EM 7RAN - 3.5 5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - 3-[(3R)-3-methyl-1,2,3,6-tetrahydropyridin-1-ium-5-yl]-1H-pyrrolo[2,3-b]pyridine pubchem
small-molecule Agonist 5-hydroxytryptamine, tryptamine small-molecule Kaplan AL, Confair DN, Kim K, Barros-Alvarez X, Rodriguiz RM, Yang Y, Kweon OS, Che T, McCorvy JD, Kamber DN, Phelan JP, Martins LC, Pogorelov VM, DiBerto JF, Slocum ST, Huang XP, Kumar JM, Robertson MJ, Panova O, Seven AB, Wetsel AQ, Wetsel WC, Irwin JJ, Skiniotis G, Shoichet BK, Roth BL, Ellman JA 10.1038/S41586-022-05258-Z 2022-07-06
Gs αs Bovine - 51 β1 Bovine γ2 Bovine Cryo-EM 8DCS - 2.5 ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey T4-Lysozyme Nanobody-35 - 4-{[(2S)-3-(tert-butylamino)-2-hydroxypropyl]oxy}-3H-indole-2-carbonitrile pubchem
small-molecule Agonist - - Su M, Paknejad N, Zhu L, Wang J, Do HN, Miao Y, Liu W, Hite RK, Huang XY 10.1038/S41467-022-31823-1 2022-07-27
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7XZ6 - 2.8 GP119 GPR119 GPR18, GPR55 and GPR119 A (Rhodopsin) Human BRIL Nanobody-35 - APD668 pubchem gtoplig chembl_ligand
small-molecule Agonist N-palmitoylethanolamine, anandamide, N-oleoylethanolamide, SEA small-molecule Xu P, Huang S, Guo S, Yun Y, Cheng X, He X, Cai P, Lan Y, Zhou H, Jiang H, Jiang Y, Xie X, Xu HE 10.1038/S41594-022-00816-5 2022-08-24
Gs αs Human Mini-Gs 59 β1 Human γ2 Human Cryo-EM 7WY8 - 2.8 AGRL3 ADGRL3 ADGRL B2 (Adhesion) Mouse - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Qian Y, Ma Z, Liu C, Li X, Zhu X, Wang N, Xu Z, Xia R, Liang J, Duan Y, Yin H, Xiong Y, Zhang A, Guo C, Chen Z, Huang Z, He Y 10.1016/J.MOLCEL.2022.10.009 2022-10-26
Gq/11 αq Human Gs-mini-Gq chimera 57 β1 Human γ2 Human Cryo-EM 8DWH 8DWH_refined 3.3 MRGX1 MRGPRX1 A orphans A (Rhodopsin) Human - - - compound 16 [PMID: 31498617] pubchem gtoplig chembl_ligand
small-molecule Agonist bovine adrenal medulla peptide 8-22 peptide Liu Y, Cao C, Huang XP, Gumpper RH, Rachman MM, Shih SL, Krumm BE, Zhang S, Shoichet BK, Fay JF, Roth BL 10.1038/S41589-022-01173-6 2022-11-02
Gs αs Bovine - 60 β1 Rat γ2 Bovine Cryo-EM 8HA0 - 2.6 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - teriparatide pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem pubchem pubchem pubchem pubchem
peptide Agonist PTHrP-(1-36), PTHrP, PTH, TIP39 peptide Zhao LH, Yuan QN, Dai AT, He XH, Chen CW, Zhang C, Xu YW, Zhou Y, Wang MW, Yang DH, Xu HE 10.1038/S41401-022-01032-Z 2022-12-21
Gq/11 αq Human - 57 β1 Human γ2 Human Cryo-EM 8HCQ 8HCQ_refined 3.0 EDNRA ETA Endothelin A (Rhodopsin) Human - scFv16 - ENDOTHELIN chembl_ligand pubchem
protein Agonist endothelin-2, endothelin-3, endothelin-1 peptide - - 2023-03-22
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 8IRS - 3.0 DRD2 D2 Dopamine A (Rhodopsin) Human BRIL scFv16 - rotigotine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist dopamine small-molecule Xu P, Huang S, Krumm BE, Zhuang Y, Mao C, Zhang Y, Wang Y, Huang XP, Liu YF, He X, Li H, Yin W, Jiang Y, Zhang Y, Roth BL, Xu HE 10.1038/S41422-023-00808-0 2023-06-07
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 7Y64 - 2.9 C5AR1 C5a1 Complement peptide A (Rhodopsin) Human - scFv16 - C5a anaphylatoxin
peptide Agonist ribosomal protein S19, C3a, C5a, C5a des-Arg peptide Feng Y, Zhao C, Deng Y, Wang H, Ma L, Liu S, Tian X, Wang B, Bin Y, Chen P, Yan W, Fu P, Shao Z 10.1038/S41422-023-00779-2 2023-03-01
Gi/o αi1 Human - 65 β1 Human γ2 Human Cryo-EM 8IC0 - 3.4 CXCR1 CXCR1 Chemokine A (Rhodopsin) Human - scFv16 - Interleukin-8 pubchem
protein Agonist CXCL8, cytokine domain of tyrosyl tRNA synthetase, CXCL6 peptide Ishimoto N, Park JH, Kawakami K, Tajiri M, Mizutani K, Akashi S, Tame JRH, Inoue A, Park SY 10.1038/S41467-023-39799-2 2023-07-19
Gi/o αo Human - 59 β1 Human γ2 Human Cryo-EM 8IA2 8IA2_refined 3.2 C5AR1 C5a1 Complement peptide A (Rhodopsin) Human - scFv16 - C5a gtoplig
peptide Agonist ribosomal protein S19, C3a, C5a, C5a des-Arg peptide Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C 10.1016/J.CELL.2023.09.020 2023-10-18
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8JLQ - 2.8 TAAR1 TA1 Trace amine A (Rhodopsin) Human BRIL scFv16 - fenoldopam pubchem gtoplig chembl_ligand drugbank drug_central pubchem gtoplig chembl_ligand pubchem pubchem gtoplig chembl_ligand pubchem
small-molecule Agonist octopamine, β-phenylethylamine, CHEMBL1160703, tyramine, (+)-Octopamine, 3-iodothyronamine, dopamine small-molecule Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z 10.1038/S41586-023-06804-Z 2023-11-15
Gq/11 αq Human - 57 β1 Human γ2 Human Cryo-EM 8WCB - 3.1 TAAR1 TA1 Trace amine A (Rhodopsin) Mouse - scFv16 - Cyclohexylammonium ion pubchem
small-molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine small-molecule Shang P, Rong N, Jiang JJ, Cheng J, Zhang MH, Kang D, Qi L, Guo L, Yang GM, Liu Q, Zhou Z, Li XB, Zhu KK, Meng QB, Han X, Yan W, Kong Y, Yang L, Wang X, Lei D, Feng X, Liu X, Yu X, Wang Y, Li Q, Shao ZH, Yang F, Sun JP 10.1016/J.CELL.2023.10.014 2023-12-27
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8GE7 8GE7_refined 3.4 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol pubchem
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human - 79 β1 Human γ2 Human Cryo-EM 8GGB 8GGB_refined 3.5 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol pubchem
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gq/11 αq Human - 59 β1 Rat γ2 Bovine Cryo-EM 8JBG 8JBG_refined 2.8 NK3R NK3 Tachykinin A (Rhodopsin) Human - scFv16 - neurokinin B pubchem gtoplig chembl_ligand
peptide Agonist neurokinin A, substance P, neurokinin B peptide - - 2024-02-07
Gq/11 αq Human - 61 β1 Human γ2 Human Cryo-EM 8SZG - 3.6 CASR CaS Calcium-sensing C (Glutamate) Human - - - L-tryptophan pubchem gtoplig chembl_ligand drugbank drug_central pubchem
cinacalcet pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule
small-molecule 		Agonist
PAM 		Ca2+, spermine, Mg2+, L-tryptophan small-molecule He F, Wu CG, Gao Y, Rahman SN, Zaoralova M, Papasergi-Scott MM, Gu TJ, Robertson MJ, Seven AB, Li L, Mathiesen JM, Skiniotis G 10.1038/S41586-024-07055-2 2024-02-07
Gs αs Human GTP bound, Class N 60 β1 Human γ2 Human Cryo-EM 8UNY - 3.6 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol pubchem
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gq/11 αq Human - 59 β1 Human γ2 Human Cryo-EM 8XOI 8XOI_refined 3.2 GPER1 GPER Estrogen (G protein-coupled) A (Rhodopsin) Human - scFv16 - fulvestrant pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist 17β-estradiol small-molecule Liu H, Guo S, Dai A, Xu P, Li X, Huang S, He X, Wu K, Zhang X, Yang D, Xie X, Xu HE 10.1038/S41422-024-00963-Y 2024-04-10
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8XZJ 8XZJ_refined 3.0 APJ apelin Apelin A (Rhodopsin) Human - scFv16 - WN353
peptide Agonist apelin-36, apelin-17, apelin-13, Elabela/Toddler-21, Elabela/Toddler-32, Elabela/Toddler-11, [Pyr1]apelin-13, apelin receptor early endogenous ligand peptide Wang WW, Ji SY, Zhang W, Zhang J, Cai C, Hu R, Zang SK, Miao L, Xu H, Chen LN, Yang Z, Guo J, Qin J, Shen DD, Liang P, Zhang Y, Zhang Y 10.1016/J.CELL.2024.02.004 2024-03-20
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 9BQJ - 3.3 OPRM μ Opioid A (Rhodopsin) Mouse - scFv16 - N-[[3-(hydroxymethyl)phenyl]methyl]-N-[1-(2-phenylethyl)piperidin-4-yl]propanamide pubchem
small-molecule Agonist - - - - 2024-09-11
Gi/o αi2 Human - 63 β1 Human γ2 Human Cryo-EM 8K6O 8K6O_refined 3.3 NPY1R Y1 Neuropeptide Y A (Rhodopsin) Human - scFv16 - neuropeptide Y pubchem gtoplig chembl_ligand gtoplig gtoplig pubchem pubchem pubchem
peptide Agonist peptide YY, pancreatic polypeptide, neuropeptide Y peptide - - 2024-07-31
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 9EPP - 4.1 B1B1U5 Rhodopsin Opsins A (Rhodopsin) Hasarius adansoni - - - 11,20-Ethanoretinal pubchem
small-molecule Agonist - - - - 2024-10-23
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 gtoplig chembl_ligand
small-molecule Agonist acetylcholine small-molecule Maeda S, Qu Q, Robertson MJ, Skiniotis G, Kobilka BK 10.1126/SCIENCE.AAW5188 2019-05-08
Gs αs Human - 57 β1 Human γ2 Human Cryo-EM 6M1I - 3.5 PACR PAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - [Ac-His1]PACAP-27 gtoplig chembl_ligand pubchem
peptide Agonist PHM, PHV, VIP, PACAP-27, PHI, PACAP-38 peptide Wang J, Song X, Zhang D, Chen X, Li X, Sun Y, Li C, Song Y, Ding Y, Ren R, Harrington EH, Hu LA, Zhong W, Xu C, Huang X, Wang HW, Ma Y 10.1038/S41422-020-0280-2 2020-03-11
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 6XBM - 3.2 SMO SMO Frizzled F (Frizzled) Human - scFv16 - 24,25-Epoxy-cholesterol pubchem
24,25-Epoxy-cholesterol pubchem
small-molecule
small-molecule 		Agonist
PAM 		- - Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X 10.1038/S41589-020-0646-2 2020-09-30
Gs αs Human - 58 β1 Rat γ2 Bovine Cryo-EM 7CZ5 7CZ5_refined 2.6 GHRHR GHRH Glucagon B1 (Secretin) Human - Nanobody-35 - Somatoliberin pubchem
peptide Agonist GHRH peptide Zhou F, Zhang H, Cong Z, Zhao LH, Zhou Q, Mao C, Cheng X, Shen DD, Cai X, Ma C, Wang Y, Dai A, Zhou Y, Sun W, Zhao F, Zhao S, Jiang H, Jiang Y, Yang D, Eric Xu H, Zhang Y, Wang MW 10.1038/S41467-020-18945-0 2020-11-18
Gs αs Human - 53 β1 Human γ2 Human Cryo-EM 7KI0 - 2.5 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - semaglutide pubchem gtoplig chembl_ligand drugbank pubchem
peptide Agonist glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide peptide Zhang X, Belousoff MJ, Liang YL, Danev R, Sexton PM, Wootten D 10.1016/J.CELREP.2021.109374 2021-08-04
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7VUI 7VUI_refined 3.3 GP139 GPR139 A orphans A (Rhodopsin) Human - Nanobody-35 Xylanase JNJ-63533054 pubchem gtoplig chembl_ligand
small-molecule Agonist L-phenylalanine, L-tryptophan small-molecule Zhou Y, Daver H, Trapkov B, Wu L, Wu M, Harpsoe K, Gentry PR, Liu K, Larionova M, Liu J, Chen N, Brauner-Osborne H, Gloriam DE, Hua T, Liu ZJ 10.1038/S41422-021-00591-W 2021-12-29
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7EVY - 3.0 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - siponimod pubchem gtoplig chembl_ligand drug_central drugbank
small-molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine small-molecule Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z 10.1038/S41422-021-00566-X 2021-09-29
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7TYH - 3.3 CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - Calcitonin human pubchem
peptide Agonist calcitonin, adrenomedullin, amylin, α-CGRP, adrenomedullin 2/intermedin, β-CGRP peptide Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM 10.1126/SCIENCE.ABM9609 2022-03-23
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7SCG - 3.0 OPRM μ Opioid A (Rhodopsin) Mouse - scFv16 - (2E)-N-[(2S)-2-(dimethylamino)-3-(4-hydroxyphenyl)propyl]-3-(naphthalen-1-yl)prop-2-enamide pubchem
small-molecule Agonist - - Wang H, Hetzer F, Huang W, Qu Q, Meyerowitz J, Kaindl J, Hubner H, Skiniotis G, Kobilka BK, Gmeiner P 10.1002/ANIE.202200269 2022-04-20
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7X9B 7X9B_refined 3.4 NPY2R Y2 Neuropeptide Y A (Rhodopsin) Human - - - neuropeptide Y pubchem gtoplig chembl_ligand gtoplig gtoplig pubchem pubchem pubchem
peptide Agonist peptide YY, PYY-(3-36), neuropeptide Y-(3-36), pancreatic polypeptide, neuropeptide Y peptide - - 2022-05-18
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7W0P 7W0P_refined 3.2 APJ apelin Apelin A (Rhodopsin) Human BRIL scFv16 - Apelin receptor early endogenous ligand
peptide Agonist apelin-36, apelin-17, apelin-13, Elabela/Toddler-21, Elabela/Toddler-32, Elabela/Toddler-11, [Pyr1]apelin-13, apelin receptor early endogenous ligand peptide Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F 10.1038/S41594-022-00797-5 2022-07-27
Gi/o αi1 Human - 65 β1 Human γ2 Human Cryo-EM 7XA3 7XA3_refined 2.9 CCR2 CCR2 Chemokine A (Rhodopsin) Human - scFv16 - C-C motif chemokine 2
peptide Agonist CCL11, CCL2, CCL8, CCL16, CCL24, CCL13, CCL7, CCL26 peptide Shao Z, Tan Y, Shen Q, Hou L, Yao B, Qin J, Xu P, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Chen ZH, Jiang Y, Xu HE, Ying S, Ma H, Zhang Y, Shen H 10.1038/S41421-022-00403-4 2022-08-24
Gs αs Human Mini-Gs 59 β1 Human γ2 Human Cryo-EM 7WXW - 2.8 AGRF1 ADGRF1 ADGRF B2 (Adhesion) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y 10.1038/S41467-022-33173-4 2022-09-28
Gi/o αi1 Human - 63 β1 Rat γ2 Bovine Cryo-EM 7YU5 7YU5_refined 3.3 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human - scFv16 - [(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate pubchem
small-molecule Agonist 1-O-Oleoyl-D-glycerol 3-phosphoric acid small-molecule Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O 10.1038/S41467-022-33121-2 2022-10-05
Gi/o αi1 Human - 64 β1 Rat γ2 Bovine Cryo-EM 8F7Q - 3.2 OPRM μ Opioid A (Rhodopsin) Human - scFv16 - β-endorphin pubchem gtoplig chembl_ligand pubchem
peptide Agonist endomorphin-1, β-endorphin, dynorphin A, dynorphin A-(1-8), [Leu]enkephalin, dynorphin A-(1-13), dynorphin B, [Met]enkephalin, endomorphin-2 peptide Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y, Roth BL, Xu HE 10.1016/J.CELL.2022.12.026 2022-12-14
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8HBD 8HBD_refined 3.0 EDNRB ETB Endothelin A (Rhodopsin) Human - scFv16 - sovateltide pubchem gtoplig chembl_ligand gtoplig pubchem pubchem
peptide Agonist endothelin-2, endothelin-3, endothelin-1 peptide - - 2023-03-22
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8IW7 - 3.0 TAAR9 TAAR9 A orphans A (Rhodopsin) Mouse - scFv16 - 2-Phenylethanaminium pubchem
small-molecule Agonist - - Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP 10.1038/S41586-023-06106-4 2023-05-31
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8GUQ 8GUQ_refined 3.1 CNR2 CB2 Cannabinoid A (Rhodopsin) Human - scFv16 - olorinab pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist 2-arachidonoylglycerol, anandamide small-molecule Li X, Chang H, Bouma J, de Paus LV, Mukhopadhyay P, Paloczi J, Mustafa M, van der Horst C, Kumar SS, Wu L, Yu Y, van den Berg RJBHN, Janssen APA, Lichtman A, Liu ZJ, Pacher P, van der Stelt M, Heitman LH, Hua T 10.1038/S41467-023-37112-9 2023-05-10
Gq/11 αq Human Mini-Gq 60 β1 Human γ2 Human Cryo-EM 7YDM - 2.9 AGRE5 ADGRE5 ADGRE B2 (Adhesion) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Wang N, Qian Y, Xia R, Zhu X, Xiong Y, Zhang A, Guo C, He Y 10.1016/J.CHEMBIOL.2023.08.003 2023-07-12
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 8IUL - 2.8 PF2R FP Prostanoid A (Rhodopsin) Human - scFv16 - latanoprost (free acid form) pubchem gtoplig chembl_ligand
small-molecule Agonist PGF2α, PGI2, PGD2, thromboxane A2, PGE2 small-molecule Wu C, Xu Y, He Q, Li D, Duan J, Li C, You C, Chen H, Fan W, Jiang Y, Eric Xu H 10.1038/S41467-023-38411-X 2023-07-12
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 8JD5 - 3.6 GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human - scFv16 - ADX88178 pubchem gtoplig chembl_ligand
L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem
JNJ-40411813 pubchem gtoplig chembl_ligand drugbank
small-molecule
small-molecule
small-molecule 		Agonist L-glutamic acid small-molecule Wang X, Wang M, Xu T, Feng Y, Shao Q, Han S, Chu X, Xu Y, Lin S, Zhao Q, Wu B 10.1038/S41422-023-00830-2 2023-06-21
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8IJA - 2.7 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - scFv16 - nicotinic acid pubchem gtoplig chembl_ligand drugbank drug_central gtoplig pubchem
small-molecule Agonist β-D-hydroxybutyric acid, butyric acid small-molecule Pan X, Ye F, Ning P, Zhang Z, Li X, Zhang B, Wang Q, Chen G, Gao W, Qiu C, Wu Z, Li J, Zhu L, Xia J, Gong K, Du Y 10.1038/S41421-023-00610-7 2024-01-03
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8JLJ - 3.1 TAAR1 TA1 Trace amine A (Rhodopsin) Mouse BRIL scFv16 - CHEMBL1182312 chembl_ligand chembl_ligand pubchem
small-molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine small-molecule Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z 10.1038/S41586-023-06804-Z 2023-11-15
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8SAI 8SAI_refined 3.3 GPR34 GPR34 A orphans A (Rhodopsin) Human - scFv16 - O-[(S)-Hydroxy{[(2s)-2-Hydroxy-3-(Octadec-9-Enoyloxy)propyl]oxy}phosphoryl]-L-Serine pubchem
small-molecule Agonist lysophosphatidylserine small-molecule Xia A, Yong X, Zhang C, Lin G, Jia G, Zhao C, Wang X, Hao Y, Wang Y, Zhou P, Yang X, Deng Y, Wu C, Chen Y, Zhu J, Tang X, Liu J, Zhang S, Zhang J, Xu Z, Hu Q, Zhao J, Yue Y, Yan W, Su Z, Wei Y, Zhou R, Dong H, Shao Z, Yang S 10.1073/PNAS.2308435120 2023-10-04
Gs αs Human - 75 β1 Human γ2 Human Cryo-EM 8GGC - 3.4 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol pubchem
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8J6L 8J6L_refined 3.1 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - scFv16 - nicotinic acid pubchem gtoplig chembl_ligand drugbank drug_central gtoplig pubchem
small-molecule Agonist β-D-hydroxybutyric acid, butyric acid small-molecule Zhu S, Yuan Q, Li X, He X, Shen S, Wang D, Li J, Cheng X, Duan X, Xu HE, Duan J 10.1016/J.CELREP.2023.113406 2024-04-03
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8KFZ 8KFZ_refined 3.3 CCR8 CCR8 Chemokine A (Rhodopsin) Human - scFv16 - Apo (no ligand)
none Apo (no ligand) CCL8, CCL1 peptide Jiang S, Lin X, Wu L, Wang L, Wu Y, Xu Z, Xu F 10.1126/SCIADV.ADJ7500 2024-02-07
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8U4N 8U4N_refined 2.7 CXCR4 CXCR4 Chemokine A (Rhodopsin) Human - - - Apo (no ligand)
none Apo (no ligand) CXCL12α, CXCL12, CXCL12γ, CXCL12φ, CXCL12β, CXCL12δ, CXCL12ε peptide Saotome K, McGoldrick LL, Ho JH, Ramlall TF, Shah S, Moore MJ, Kim JH, Leidich R, Olson WC, Franklin MC 10.1038/S41594-024-01397-1 2024-03-13
Gs αs Human GTP bound, Class G 61 β1 Human γ2 Human Cryo-EM 8UNR - 3.4 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol pubchem
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gi/o αi1 Human - 66 β1 Human γ2 Human Cryo-EM 8XGM - 3.3 CML2 chemerin 2 Chemerin receptor A (Rhodopsin) Human - scFv16 - Retinoic acid receptor responder protein 2
protein Agonist chemerin peptide - - 2024-08-21
Gi/o αo Human - 61 β1 Rat γ2 Human Cryo-EM 9F33 - 3.1 DRD3 D3 Dopamine A (Rhodopsin) Human - scFv16 GFP CHEMBL4551160 chembl_ligand pubchem
small-molecule Agonist dopamine small-molecule - - 2024-09-18
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 8VHF 8VHF_refined 3.5 GP119 GPR119 GPR18, GPR55 and GPR119 A (Rhodopsin) Human BRIL Nanobody-35 - MBX-2982 pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist N-palmitoylethanolamine, anandamide, N-oleoylethanolamide, SEA small-molecule - - 2024-10-30
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) - - Kang Y, Kuybeda O, de Waal PW, Mukherjee S, Van Eps N, Dutka P, Zhou XE, Bartesaghi A, Erramilli S, Morizumi T, Gu X, Yin Y, Liu P, Jiang Y, Meng X, Zhao G, Melcher K, Ernst OP, Kossiakoff AA, Subramaniam S, Xu HE 10.1038/S41586-018-0215-Y 2018-06-20
Gi/o αt1 Bovine - 59 β1 Bovine γT1 Bovine Cryo-EM 6OYA - 3.3 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - Camelid antibody VHH fragment - Retinal (all-trans) pubchem
small-molecule Agonist - - Gao Y, Hu H, Ramachandran S, Erickson JW, Cerione RA, Skiniotis G 10.1016/J.MOLCEL.2019.06.007 2019-07-24
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 - - Liang YL, Belousoff MJ, Fletcher MM, Zhang X, Khoshouei M, Deganutti G, Koole C, Furness SGB, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Danev R, Wootten D, Sexton PM 10.1021/ACSPTSCI.9B00080 2020-03-25
Gs αs Human - 89 β1 Human γ2 Human Cryo-EM 6X1A - 2.5 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - danuglipron pubchem gtoplig chembl_ligand
small-molecule Agonist glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide peptide Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, Senel P, Stewart GD, Liang YL, Glukhova A, Venugopal H, Christopoulos A, Furness SGB, Miller LJ, Reedtz-Runge S, Langmead CJ, Gloriam DE, Danev R, Sexton PM, Wootten D 10.1016/J.MOLCEL.2020.09.020 2020-09-09
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 7JVR - 2.8 DRD2 D2 Dopamine A (Rhodopsin) Human - scFv16 - bromocriptine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist dopamine small-molecule Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP, Shen DD, Xu T, Liu YF, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE 10.1016/J.CELL.2021.01.027 2021-02-24
Gs αs Bovine - 59 β1 Rat γ2 Bovine Cryo-EM 7DTY - 3.0 GIPR GIP Glucagon B1 (Secretin) Human - Nanobody-35 - GIP pubchem
small-molecule Agonist gastric inhibitory polypeptide peptide Zhao F, Zhang C, Zhou Q, Hang K, Zou X, Chen Y, Wu F, Rao Q, Dai A, Yin W, Shen DD, Zhang Y, Xia T, Stevens RC, Xu HE, Yang D, Zhao L, Wang MW 10.7554/ELIFE.68719 2021-08-04
Gs αs Bovine - 91 β1 Rat γ2 Bovine Cryo-EM 7FII - 4.3 LSHR LH Glycoprotein hormone A (Rhodopsin) Human - - - Choriogonadotropin beta gtoplig
Glycoprotein alpha gtoplig
protein
protein 		Agonist LH, hCG peptide Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE 10.1038/S41586-021-03924-2 2021-09-29
Gi/o αi1 Mouse - 62 β1 Bovine γ2 Bovine Cryo-EM 7TD0 - 2.8 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human - - - lysophosphatidic acid pubchem
small-molecule Agonist 1-O-Oleoyl-D-glycerol 3-phosphoric acid small-molecule Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY 10.1038/S41467-022-28417-2 2022-02-09
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7SBF - 2.9 OPRM μ Opioid A (Rhodopsin) Mouse BRIL scFv16 - N-[(2S)-2-(dimethylamino)-3-(4-hydroxyphenyl)propyl]-N'-[(2S)-1-(thiophen-3-yl)propan-2-yl]urea pubchem
small-molecule Agonist - - Wang H, Hetzer F, Huang W, Qu Q, Meyerowitz J, Kaindl J, Hubner H, Skiniotis G, Kobilka BK, Gmeiner P 10.1002/ANIE.202200269 2022-04-20
Gs αs Human - 59 β1 Rat γ2 Bovine Cryo-EM 7XJH - 3.3 ADRB3 β3 Adrenoceptors A (Rhodopsin) Dog - Nanobody-35 - LEVISOPRENALINE chembl_ligand chembl_ligand pubchem
small-molecule Agonist - - Nagiri C, Kobayashi K, Tomita A, Kato M, Kobayashi K, Yamashita K, Nishizawa T, Inoue A, Shihoya W, Nureki O 10.1016/J.MOLCEL.2021.06.024 2022-05-04
Gq/11 αq Human - 58 β1 Human γ2 Human Cryo-EM 7XJL 7XJL_refined 3.5 GALR2 GAL2 Galanin A (Rhodopsin) Human - scFv16 - Spexin pubchem
small-molecule Agonist spexin-1, galanin-like peptide, galanin peptide Jiang W, Zheng S 10.1073/PNAS.2121465119 2022-06-29
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7WYB - 3.0 AGRL3 ADGRL3 ADGRL B2 (Adhesion) Mouse - scFv16 - Apo (no ligand)
none Apo (no ligand) - - Qian Y, Ma Z, Liu C, Li X, Zhu X, Wang N, Xu Z, Xia R, Liang J, Duan Y, Yin H, Xiong Y, Zhang A, Guo C, Chen Z, Huang Z, He Y 10.1016/J.MOLCEL.2022.10.009 2022-10-26
Gs αs Bovine - 60 β1 Rat γ2 Bovine Cryo-EM 8HAO - 3.8 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - teriparatide pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem pubchem pubchem pubchem pubchem
peptide Agonist PTHrP-(1-36), PTHrP, PTH, TIP39 peptide Zhao LH, Yuan QN, Dai AT, He XH, Chen CW, Zhang C, Xu YW, Zhou Y, Wang MW, Yang DH, Xu HE 10.1038/S41401-022-01032-Z 2022-12-21
Gi/o αo Human - 62 β1 Human γ2 Human Cryo-EM 7T94 - 3.2 ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human - Antibody fragment - acetylcholine pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
LY2119620 pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Agonist
PAM 		acetylcholine small-molecule - - 2023-01-25
Gs αs Human - 56 β1 Human γ2 Human Cryo-EM 7Y3G 7Y3G_refined 2.8 GPR12 GPR12 A orphans A (Rhodopsin) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) sphingosine 1-phosphate small-molecule Li H, Zhang J, Yu Y, Luo F, Wu L, Liu J, Chen N, Liu Z, Hua T 10.1016/J.SCIB.2022.12.023 2023-06-07
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8IA8 - 2.9 C3AR C3a Complement peptide A (Rhodopsin) Human - scFv16 - ALA-SER-LYS-LEU-GLY-LEU-ALA-ARG
peptide Agonist C5a, C3a peptide - - 2023-05-24
Gq/11 αq Human Mini-Gq 46 - - - - Cryo-EM 7YM8 7YM8_refined 2.9 ADA1A α1A Adrenoceptors A (Rhodopsin) Human - Nanobody-29 - oxymetazoline pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist (-)-noradrenaline, (-)-adrenaline small-molecule Toyoda Y, Zhu A, Kong F, Shan S, Zhao J, Wang N, Sun X, Zhang L, Yan C, Kobilka BK, Liu X 10.1038/S41467-023-39310-X 2023-07-05
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8F0K - 1.9 CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP3 		- San385
peptide Agonist calcitonin, adrenomedullin, amylin, α-CGRP, adrenomedullin 2/intermedin, β-CGRP peptide Cao J, Belousoff MJ, Gerrard E, Danev R, Fletcher MM, Dal Maso E, Schreuder H, Lorenz K, Evers A, Tiwari G, Besenius M, Li Z, Johnson RM, Wootten D, Sexton PM 10.1038/S41589-023-01393-4 2023-08-02
Gs αs Human - 61 β1 Human γ2 Human Cryo-EM 8HJ1 8HJ1_refined 3.3 GPR21 GPR21 A orphans A (Rhodopsin) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Lin X, Chen B, Wu Y, Han Y, Qi A, Wang J, Yang Z, Wei X, Zhao T, Wu L, Xie X, Sun J, Zheng J, Zhao S, Xu F 10.1038/S41467-023-35882-W 2023-12-27
Gi/o αi1 Human - 62 β1 Mouse γ2 Mouse Cryo-EM 8IHB - 2.9 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human BRIL - - GSK256073 pubchem gtoplig chembl_ligand
small-molecule Agonist β-D-hydroxybutyric acid, butyric acid small-molecule Suzuki S, Tanaka K, Nishikawa K, Suzuki H, Oshima A, Fujiyoshi Y 10.1038/S41467-023-41650-7 2023-09-13
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8JIM - 3.0 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - scFv16 - CHEMBL3354065 chembl_ligand pubchem
small-molecule Agonist β-D-hydroxybutyric acid, butyric acid small-molecule Zhao C, Wang H, Liu Y, Cheng L, Wang B, Tian X, Fu H, Wu C, Li Z, Shen C, Yu J, Yang S, Hu H, Fu P, Ma L, Wang C, Yan W, Shao Z 10.1016/J.MOLCEL.2023.07.030 2023-09-06
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 8W88 - 2.6 TAAR1 TA1 Trace amine A (Rhodopsin) Human - Nanobody-35 - ulotaront pubchem gtoplig drugbank chembl_ligand
small-molecule Agonist octopamine, β-phenylethylamine, CHEMBL1160703, tyramine, (+)-Octopamine, 3-iodothyronamine, dopamine small-molecule Liu H, Zheng Y, Wang Y, Wang Y, He X, Xu P, Huang S, Yuan Q, Zhang X, Wang L, Jiang K, Chen H, Li Z, Liu W, Wang S, Xu HE, Xu F 10.1038/S41586-023-06775-1 2023-11-22
Gi/o αi1 Human - 66 β1 Human γ2 Human Cryo-EM 8FY8 - 2.8 5HT1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - 5-MeO-DMT pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist 5-hydroxytryptamine small-molecule Warren AL, Lankri D, Cunningham MJ, Serrano IC, Parise LF, Kruegel AC, Duggan P, Zilberg G, Capper MJ, Havel V, Russo SJ, Sames D, Wacker D 10.1038/S41586-024-07403-2 2024-05-15
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8GFV - 3.1 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol pubchem
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8J24 8J24_refined 2.6 FFAR2 FFA2 Free fatty acid A (Rhodopsin) Human - scFv16 - Acetic acid pubchem
small-molecule Agonist propanoic acid, acetic acid, trans-2-methylcrotonic acid, butyric acid small-molecule Li F, Tai L, Sun X, Lv Z, Tang W, Wang T, Zhao Z, Gong D, Ma S, Tang S, Gu Q, Zhu X, Yu M, Liu X, Wang J 10.1038/S41422-023-00914-Z 2024-01-24
Gs αs Human - 61 β1 Human γ2 Human Cryo-EM 8K8J - 2.9 CNR1 CB1 Cannabinoid A (Rhodopsin) Human BRIL Nanobody-35 - FENOFIBRATE chembl_ligand pubchem
small-molecule Agonist anandamide small-molecule Wang T, Tang W, Zhao Z, Zhao R, Lv Z, Guo X, Gu Q, Liu B, Lv H, Chen J, Zhang K, Li F, Wang J 10.1002/ADVS.202306311 2024-02-14
Gi/o αo Human - 62 β1 Human γ2 Human Cryo-EM 8TZQ 8TZQ_refined 3.2 DRD2 D2 Dopamine A (Rhodopsin) Human - scFv16 - dopamine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist dopamine small-molecule Knight KM, Krumm BE, Kapolka NJ, Ludlam WG, Cui M, Mani S, Prytkova I, Obarow EG, Lefevre TJ, Wei W, Ma N, Huang XP, Fay JF, Vaidehi N, Smrcka AV, Slesinger PA, Logothetis DE, Martemyanov KA, Roth BL, Dohlman HG 10.1038/S41467-024-50964-Z 2024-08-21
Gs αs Human GTP bound, Class H 61 β1 Human γ2 Human Cryo-EM 8UNS - 3.4 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol pubchem
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gq/11 αq Human - 59 β1 Human γ2 Human Cryo-EM 8WST 8WST_refined 2.4 MCHR2 MCH2 Melanin-concentrating hormone A (Rhodopsin) Human - Nanobody-35 - pro-MCH
peptide Agonist melanin-concentrating hormone peptide He Q, Yuan Q, Shan H, Wu C, Gu Y, Wu K, Hu W, Zhang Y, He X, Xu HE, Zhao LH 10.1038/S41421-024-00679-8 2024-06-19
Gi/o αgust Human - 63 β1 Human γ2 Human Cryo-EM 8XQR - 3.2 T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human - Nanobody-35 Exo-alpha-sialidase flufenamic acid pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist - - Hu X, Ao W, Gao M, Wu L, Pei Y, Liu S, Wu Y, Zhao F, Sun Q, Liu J, Jiang L, Wang X, Li Y, Tan Q, Cheng J, Yang F, Yang C, Sun J, Hua T, Liu ZJ 10.1038/S41586-024-07569-9 2024-07-10
Gi/o αi1 Human - 63 β1 Rat γ2 Bovine Cryo-EM 8ZCJ 8ZCJ_refined 3.1 SSR5 SST5 Somatostatin A (Rhodopsin) Human - scFv16 LgBiT 004-DTR-LYS-TYR-PHA-HYP
peptide Agonist cortistatin-14, SRIF-14, CST-17, SRIF-28 peptide Li YG, Meng XY, Yang X, Ling SL, Shi P, Tian CL, Yang F 10.1038/S41401-024-01314-8 2024-07-10
Gi/o αi1 Human - 100 β1 Human γ2 Human Cryo-EM 6PT0 6PT0_refined 3.2 CNR2 CB2 Cannabinoid A (Rhodopsin) Human - scFv16 - WIN55212-2 pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist 2-arachidonoylglycerol, anandamide small-molecule Xing C, Zhuang Y, Xu TH, Feng Z, Zhou XE, Chen M, Wang L, Meng X, Xue Y, Wang J, Liu H, McGuire TF, Zhao G, Melcher K, Zhang C, Xu HE, Xie XQ 10.1016/J.CELL.2020.01.007 2020-02-12
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 6VMS - 3.8 DRD2 D2 Dopamine A (Rhodopsin) Human T4-Lysozyme scFv16 - bromocriptine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist dopamine small-molecule Yin J, Chen KM, Clark MJ, Hijazi M, Kumari P, Bai XC, Sunahara RK, Barth P, Rosenbaum DM 10.1038/S41586-020-2379-5 2020-06-17
Gs αs Bovine - 51 β1 Bovine γ2 Bovine Cryo-EM 7JJO - 2.6 ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey - Nanobody-35 - LEVISOPRENALINE chembl_ligand chembl_ligand pubchem
small-molecule Agonist - - Su M, Zhu L, Zhang Y, Paknejad N, Dey R, Huang J, Lee MY, Williams D, Jordan KD, Eng ET, Ernst OP, Meyerson JR, Hite RK, Walz T, Liu W, Huang XY 10.1016/J.MOLCEL.2020.08.001 2020-09-02
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7CKZ - 3.1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - dopamine pubchem gtoplig chembl_ligand drugbank drug_central
mevidalen pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Agonist
PAM 		L-NOREPINEPHRINE, noradrenaline, (-)-noradrenaline, 5-hydroxytryptamine, dopamine small-molecule Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z 10.1016/J.CELL.2021.01.028 2021-03-03
Gq/11 αq Human Engineered G alpha 59 β1 Human γ2 Human Cryo-EM 7F9Z 7F9Z_refined 3.2 GHSR ghrelin Ghrelin A (Rhodopsin) Human - Nanobody-35
scFv16 		- GHRP-6 pubchem gtoplig
peptide Agonist [des-Gln14]ghrelin, ghrelin peptide Wang Y, Guo S, Zhuang Y, Yun Y, Xu P, He X, Guo J, Yin W, Xu HE, Xie X, Jiang Y 10.1038/S41467-021-25364-2 2021-08-18
Gq/11 αq Human Gq-Gi1 chimera 60 β1 Rat γ2 Bovine Cryo-EM 7F2O - 2.9 BKRB2 B2 Bradykinin A (Rhodopsin) Human - scFv16 - bradykinin pubchem gtoplig chembl_ligand drugbank gtoplig
peptide Agonist [des-Arg9]bradykinin, kallidin, Lys-[Hyp3]-bradykinin, [des-Arg10]kallidin, T-kinin, [Hyp3]bradykinin, bradykinin peptide Yin YL, Ye C, Zhou F, Wang J, Yang D, Yin W, Wang MW, Xu HE, Jiang Y 10.1038/S41594-021-00645-Y 2021-10-13
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7VUZ 7VUZ_refined 2.9 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human - scFv16 - PAMP-12 pubchem
peptide Agonist PAMP-20 peptide Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP 10.1038/S41586-021-04077-Y 2021-12-01
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7LLL - 3.7 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - exendin-4 pubchem gtoplig pubchem
peptide Agonist glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide peptide Deganutti G, Liang YL, Zhang X, Khoshouei M, Clydesdale L, Belousoff MJ, Venugopal H, Truong TT, Glukhova A, Keller AN, Gregory KJ, Leach K, Christopoulos A, Danev R, Reynolds CA, Zhao P, Sexton PM, Wootten D 10.1038/S41467-021-27760-0 2022-01-12
Gi/o αi1 Mouse - 62 β1 Bovine γ2 Bovine Cryo-EM 7TD2 - 3.1 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human - - - lysophosphatidic acid pubchem
small-molecule Agonist 1-O-Oleoyl-D-glycerol 3-phosphoric acid small-molecule Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY 10.1038/S41467-022-28417-2 2022-02-09
Gi/o αi2 Human - 61 β1 Human γ2 Human Cryo-EM 7WVX - 2.8 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human BRIL - - humanin pubchem gtoplig chembl_ligand pubchem
peptide Agonist LXA4, serum amyloid A, PrP106-126, aspirin-triggered resolvin D1, humanin, aspirin triggered lipoxin A4, LL-37, annexin I, resolvin D1 peptide Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B 10.1038/S41467-022-29361-X 2022-04-13
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 7W55 - 2.8 NMUR2 NMU2 Neuromedin U A (Rhodopsin) Human - scFv16 - Neuromedin U-25 (human) pubchem
peptide Agonist neuromedin U-25, neuromedin S-36, neuromedin S-33, neuromedin U-23 peptide You C, Zhang Y, Xu P, Huang S, Yin W, Eric Xu H, Jiang Y 10.1038/S41467-022-29683-W 2022-04-20
Gq/11 αq Human - 61 β1 Human γ2 Human Cryo-EM 7XOW 7XOW_refined 3.1 GASR CCK2 Cholecystokinin A (Rhodopsin) Human - scFv16 - desulfated gastrin-17 pubchem gtoplig chembl_ligand pubchem
peptide Agonist CCK-8, desulfated cholecystokinin-8, gastrin-14, CCK-58, desulfated gastrin-17, CCK-39, CCK-33, desulfated gastrin-34, gastrin-34, gastrin-71, desulfated gastrin-71, CCK-4, desulfated gastrin-14, gastrin-17 peptide Ding Y, Zhang H, Liao YY, Chen LN, Ji SY, Qin J, Mao C, Shen DD, Lin L, Wang H, Zhang Y, Li XM 10.1038/S41421-022-00420-3 2022-07-20
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 7XMT 7XMT_refined 2.8 SSR4 SST4 Somatostatin A (Rhodopsin) Human - scFv16 - J-2156 pubchem gtoplig chembl_ligand
small-molecule Agonist cortistatin-14, SRIF-14, CST-17, SRIF-28 peptide Zhao W, Han S, Qiu N, Feng W, Lu M, Zhang W, Wang M, Zhou Q, Chen S, Xu W, Du J, Chu X, Yi C, Dai A, Hu L, Shen MY, Sun Y, Zhang Q, Ma Y, Zhong W, Yang D, Wang MW, Wu B, Zhao Q 10.1038/S41422-022-00679-X 2022-08-03
Gs αs Human - 57 β1 Human γ2 Human Cryo-EM 7XKF - 2.4 AGRG2 ADGRG2 ADGRG B2 (Adhesion) Mouse - Nanobody-35 - PRASTERONE chembl_ligand pubchem
small-molecule Agonist - - Lin H, Xiao P, Bu RQ, Guo S, Yang Z, Yuan D, Zhu ZL, Zhang CX, He QT, Zhang C, Ping YQ, Zhao RJ, Ma CS, Liu CH, Zhang XN, Jiang D, Huang S, Xi YT, Zhang DL, Xue CY, Yang BS, Li JY, Lin HC, Zeng XH, Zhao H, Xu WM, Yi F, Liu Z, Sun JP, Yu X 10.1038/S41589-022-01084-6 2022-08-10
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7VIE 7VIE_refined 2.9 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - sphingosine 1-phosphate pubchem gtoplig chembl_ligand pubchem
small-molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine small-molecule Yu L, He L, Gan B, Ti R, Xiao Q, Hu H, Zhu L, Wang S, Ren R 10.1073/PNAS.2117716119 2022-09-28
Gi/o αi1 Human - 58 β1 Human γ2 Human Cryo-EM 7Y89 - 3.0 GPR17 GPR17 A orphans A (Rhodopsin) Human - - - Apo (no ligand)
none Apo (no ligand) UDP, LTD4, UDP-galactose, LTC4, UDP-glucose, ATP, LTE4 small-molecule Ye F, Wong TS, Chen G, Zhang Z, Zhang B, Gan S, Gao W, Li J, Wu Z, Pan X, Du Y 10.1002/MCO2.159 2022-10-12
Gs αs Bovine - 60 β1 Rat γ2 Bovine Cryo-EM 8HAF - 3.3 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - PTHrP-(1-36) pubchem gtoplig
peptide Agonist PTHrP-(1-36), PTHrP, PTH, TIP39 peptide Zhao LH, Yuan QN, Dai AT, He XH, Chen CW, Zhang C, Xu YW, Zhou Y, Wang MW, Yang DH, Xu HE 10.1038/S41401-022-01032-Z 2022-12-21
Gs αs Human Mini-Gs 60 β1 Human γ2 Human Cryo-EM 8HDP - 3.2 AA2BR A2B Adenosine A (Rhodopsin) Human - Nanobody-35 - adenosine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist adenosine small-molecule Cai H, Xu Y, Guo S, He X, Sun J, Li X, Li C, Yin W, Cheng X, Jiang H, Xu HE, Xie X, Jiang Y 10.1038/S41421-022-00503-1 2023-01-18
Gi/o αi2 Human - 61 β1 Human γ2 Human Cryo-EM 7XXI 7XXI_refined 3.0 P2Y12 P2Y12 P2Y A (Rhodopsin) Human - - - 2MeSADP pubchem gtoplig chembl_ligand gtoplig
small-molecule Agonist ATP, ADP small-molecule - - 2023-06-07
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 8IBU 8IBU_refined 3.5 MTLR motilin Motilin A (Rhodopsin) Human BRIL scFv16 - erythromycin pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist motilin peptide You C, Zhang Y, Xu Y, Xu P, Li Z, Li H, Huang S, Chen Z, Li J, Xu HE, Jiang Y 10.1126/SCIADV.ADE9020 2023-04-12
Gs αs Human Mini-Gs 59 β1 Human γ2 Human Cryo-EM 7YDP - 3.1 AGRE5 ADGRE5 ADGRE B2 (Adhesion) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Wang N, Qian Y, Xia R, Zhu X, Xiong Y, Zhang A, Guo C, He Y 10.1016/J.CHEMBIOL.2023.08.003 2023-07-12
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 8IUM - 3.1 PF2R FP Prostanoid A (Rhodopsin) Human - scFv16
Nanobody-35 		- tafluprost acid pubchem gtoplig
small-molecule Agonist PGF2α, PGI2, PGD2, thromboxane A2, PGE2 small-molecule Wu C, Xu Y, He Q, Li D, Duan J, Li C, You C, Chen H, Fan W, Jiang Y, Eric Xu H 10.1038/S41467-023-38411-X 2023-07-12
Gs αs Human - 54 β1 Human γ2 Human Cryo-EM 8GD9 - 3.2 PE2R4 EP4 Prostanoid A (Rhodopsin) Human - - - 4-({2-[(1R,2R,3R,5S)-3,5-dihydroxy-2-{(3S)-3-hydroxy-4-[3-(methoxymethyl)phenyl]butyl}cyclopentyl]ethyl}sulfanyl)butanoic acid pubchem
small-molecule Agonist PGF2α, PGI2, PGD2, thromboxane A2, PGE1, PGE2 small-molecule Huang SM, Xiong MY, Liu L, Mu J, Wang MW, Jia YL, Cai K, Tie L, Zhang C, Cao S, Wen X, Wang JL, Guo SC, Li Y, Qu CX, He QT, Cai BY, Xue C, Gan S, Xie Y, Cong X, Yang Z, Kong W, Li S, Li Z, Xiao P, Yang F, Yu X, Guan YF, Zhang X, Liu Z, Yang BX, Du Y, Sun JP 10.1073/PNAS.2216329120 2024-01-10
Gi/o αo Human - 59 β1 Human γ2 Human Cryo-EM 8I97 8I97_refined 3.2 C3AR C3a Complement peptide A (Rhodopsin) Human - scFv16 - Apo (no ligand)
none Apo (no ligand) C5a, C3a peptide Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C 10.1016/J.CELL.2023.09.020 2023-10-18
Gs αs Bovine - 59 β1 Rat γ2 Bovine Cryo-EM 8ITM - 3.1 GIPR GIP Glucagon B1 (Secretin) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) gastric inhibitory polypeptide peptide Zhao F, Hang K, Zhou Q, Shao L, Li H, Li W, Lin S, Dai A, Cai X, Liu Y, Xu Y, Feng W, Yang D, Wang MW 10.1073/PNAS.2306145120 2023-10-18
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8JLK - 3.2 TAAR1 TA1 Trace amine A (Rhodopsin) Mouse - scFv16 - ulotaront pubchem gtoplig drugbank chembl_ligand
small-molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine small-molecule Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z 10.1038/S41586-023-06804-Z 2023-11-15
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8GE5 - 3.2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol pubchem
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
G12/13 α13 Human - 56 β1 Human γ2 Human Cryo-EM 8IKL - 2.3 AGRE5 ADGRE5 ADGRE B2 (Adhesion) Human - - - Apo (no ligand)
none Apo (no ligand) - - Mao C, Zhao RJ, Dong YJ, Gao M, Chen LN, Zhang C, Xiao P, Guo J, Qin J, Shen DD, Ji SY, Zang SK, Zhang H, Wang WW, Shen Q, Sun JP, Zhang Y 10.1016/J.MOLCEL.2023.12.020 2024-01-24
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8U4O - 3.3 CXCR4 CXCR4 Chemokine A (Rhodopsin) Human - - - CXC12
protein Agonist CXCL12α, CXCL12, CXCL12γ, CXCL12φ, CXCL12β, CXCL12δ, CXCL12ε peptide Saotome K, McGoldrick LL, Ho JH, Ramlall TF, Shah S, Moore MJ, Kim JH, Leidich R, Olson WC, Franklin MC 10.1038/S41594-024-01397-1 2024-03-13
Gs αs Human GTP bound, Class P 58 β1 Human γ2 Human Cryo-EM 8UO0 - 3.5 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol pubchem
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human - 55 β1 Human γ2 Human Cryo-EM 8X2K - 3.0 GPR3 GPR3 A orphans A (Rhodopsin) Human BRIL scFv16 - N-oleoylethanolamide pubchem gtoplig chembl_ligand
small-molecule Agonist sphingosine 1-phosphate small-molecule Chen G, Staffen N, Wu Z, Xu X, Pan J, Inoue A, Shi T, Gmeiner P, Du Y, Xu J 10.1038/S41422-023-00919-8 2024-04-03
Gq/11 αq Human - 59 β1 Human γ2 Human Cryo-EM 8XOJ 8XOJ_refined 3.1 GPER1 GPER Estrogen (G protein-coupled) A (Rhodopsin) Human - scFv16 - - - - 17β-estradiol small-molecule Liu H, Guo S, Dai A, Xu P, Li X, Huang S, He X, Wu K, Zhang X, Yang D, Xie X, Xu HE 10.1038/S41422-024-00963-Y 2024-04-10
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8XZH 8XZH_refined 2.6 APJ apelin Apelin A (Rhodopsin) Human - scFv16 - MM07 pubchem gtoplig chembl_ligand
peptide Agonist apelin-36, apelin-17, apelin-13, Elabela/Toddler-21, Elabela/Toddler-32, Elabela/Toddler-11, [Pyr1]apelin-13, apelin receptor early endogenous ligand peptide Wang WW, Ji SY, Zhang W, Zhang J, Cai C, Hu R, Zang SK, Miao L, Xu H, Chen LN, Yang Z, Guo J, Qin J, Shen DD, Liang P, Zhang Y, Zhang Y 10.1016/J.CELL.2024.02.004 2024-03-20
Gs αs Human - 52 β1 Human γ2 Human Cryo-EM 9BKK - 2.5 CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human - - - CHEMBL216166 chembl_ligand pubchem
protein Agonist CCK-8, desulfated cholecystokinin-8, CCK-39, CCK-58, CCK-33, CCK-4, gastrin-17 peptide Harikumar KG, Zhao P, Cary BP, Xu X, Desai AJ, Dong M, Mobbs JI, Toufaily C, Furness SGB, Christopoulos A, Belousoff MJ, Wootten D, Sexton PM, Miller LJ 10.1371/JOURNAL.PBIO.3002673 2024-05-22
Gs αs Human Mini-Gs 56 β1 Human γ2 Human Cryo-EM 8UXV - 3.2 O51G2 OR51G2 Odorant family 51 O1 (fish-like odorant) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - de March CA, Ma N, Billesbolle CB, Tewari J, Llinas Del Torrent C, van der Velden WJC, Ojiro I, Takayama I, Faust B, Li L, Vaidehi N, Manglik A, Matsunami H 10.1038/S41586-024-08126-0 2024-10-30
Gi/o αi3 Human - 63 β1 Human γ2 Human Cryo-EM 8WGB - 3.7 GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human - - - VU0155041 pubchem gtoplig chembl_ligand
small-molecule Agonist L-glutamic acid small-molecule Huang W, Jin N, Guo J, Shen C, Xu C, Xi K, Bonhomme L, Quast RB, Shen DD, Qin J, Liu YR, Song Y, Gao Y, Margeat E, Rondard P, Pin JP, Zhang Y, Liu J 10.1038/S41467-024-54744-7 2024-10-30
Gs αs Bovine - 89 β1 Rat γ2 Bovine X-ray 3SN6 - 3.2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human T4-Lysozyme Antibody - CHEMBL1615159 chembl_ligand pubchem
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule Rasmussen SG, DeVree BT, Zou Y, Kruse AC, Chung KY, Kobilka TS, Thian FS, Chae PS, Pardon E, Calinski D, Mathiesen JM, Shah ST, Lyons JA, Caffrey M, Gellman SH, Steyaert J, Skiniotis G, Weis WI, Sunahara RK, Kobilka BK 10.1038/NATURE10361 2011-07-20
Gs αs Human Fused partial Gs 44 - - - - X-ray 6E67 6E67_refined 3.7 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human T4-Lysozyme - - CHEMBL1615159 chembl_ligand pubchem
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule Liu X, Xu X, Hilger D, Aschauer P, Tiemann JKS, Du Y, Liu H, Hirata K, Sun X, Guixa-Gonzalez R, Mathiesen JM, Hildebrand PW, Kobilka BK 10.1016/J.CELL.2019.04.021 2019-06-05
Gq/11 αq Human Gq-Gi2-Gs chimera 57 β1 Human γ2 Human Cryo-EM 6WHA - 3.4 5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL scFv16 - CHEMBL5184791 chembl_ligand pubchem
small-molecule Agonist 5-hydroxytryptamine, tryptamine small-molecule Kim K, Che T, Panova O, DiBerto JF, Lyu J, Krumm BE, Wacker D, Robertson MJ, Seven AB, Nichols DE, Shoichet BK, Skiniotis G, Roth BL 10.1016/J.CELL.2020.08.024 2020-09-23
Gi/o αi1 Human Non-canonical conformation 95 β1 Human γT1 Human Cryo-EM 7L0S - 4.5 NTR1 NTS1 Neurotensin A (Rhodopsin) Rat - - - neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
peptide Agonist neuromedin N, neurotensin peptide Zhang M, Gui M, Wang ZF, Gorgulla C, Yu JJ, Wu H, Sun ZJ, Klenk C, Merklinger L, Morstein L, Hagn F, Pluckthun A, Brown A, Nasr ML, Wagner G 10.1038/S41594-020-00554-6 2021-01-06
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7E2Z - 3.1 5HT1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human - - - aripiprazole pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist (partial) 5-hydroxytryptamine small-molecule Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen DD, Yen HY, Robinson CV, Harpsoe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE 10.1038/S41586-021-03376-8 2021-04-14
Gi/o αi1 Human - 62 β1 Rat γ2 Bovine Cryo-EM 7DB6 7DB6_refined 3.3 MTR1A MT1 Melatonin A (Rhodopsin) Human - scFv16 - ramelteon pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist melatonin small-molecule Okamoto HH, Miyauchi H, Inoue A, Raimondi F, Tsujimoto H, Kusakizako T, Shihoya W, Yamashita K, Suno R, Nomura N, Kobayashi T, Iwata S, Nishizawa T, Nureki O 10.1038/S41594-021-00634-1 2021-08-18
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7RTB 7RTB_refined 2.1 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Peptide-19
peptide Agonist glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide peptide Johnson RM, Zhang X, Piper SJ, Nettleton TJ, Vandekolk TH, Langmead CJ, Danev R, Sexton PM, Wootten D 10.1016/J.BBRC.2021.09.016 2021-10-06
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7NA8 - 2.7 GHSR ghrelin Ghrelin A (Rhodopsin) Human - Antibody fragment - ibutamoren pubchem gtoplig chembl_ligand
small-molecule Agonist [des-Gln14]ghrelin, ghrelin peptide Liu H, Sun D, Myasnikov A, Damian M, Baneres JL, Sun J, Zhang C 10.1038/S41467-021-26735-5 2021-12-15
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7F4I 7F4I_refined 3.1 MSHR MC1 Melanocortin A (Rhodopsin) Human - Nanobody-35 - bremelanotide pubchem gtoplig chembl_ligand drugbank drug_central
peptide Agonist γ-MSH, β-MSH, α-MSH, ACTH peptide Ma S, Chen Y, Dai A, Yin W, Guo J, Yang D, Zhou F, Jiang Y, Wang MW, Xu HE 10.1038/S41422-021-00557-Y 2021-09-08
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7TYL - 3.3 CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - Amylin rat pubchem
peptide Agonist calcitonin, adrenomedullin, amylin, α-CGRP, adrenomedullin 2/intermedin, β-CGRP peptide Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM 10.1126/SCIENCE.ABM9609 2022-03-23
Gs αs Human - 56 β1 Human γ2 Human Cryo-EM 7RBT 7RBT_refined 3.1 GIPR GIP Glucagon B1 (Secretin) Human - scFv16
Nanobody-35 		- tirzepatide pubchem gtoplig
2-fluoro-4-[(1R)-6-methoxy-1-methyl-2-{(1S)-1-[4-(propan-2-yl)phenyl]ethyl}-1,2,3,4-tetrahydroisoquinolin-5-yl]-6-[(2-methylpropyl)amino]phenol pubchem
peptide
small-molecule 		Agonist
PAM 		gastric inhibitory polypeptide peptide Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW 10.1073/PNAS.2116506119 2022-04-13
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7X2F 7X2F_refined 3.0 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - dopamine pubchem gtoplig chembl_ligand drugbank drug_central
mevidalen pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Agonist
PAM 		L-NOREPINEPHRINE, noradrenaline, (-)-noradrenaline, 5-hydroxytryptamine, dopamine small-molecule Teng X, Chen S, Nie Y, Xiao P, Yu X, Shao Z, Zheng S 10.1038/S41467-022-30929-W 2022-06-15
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7XBX - 3.4 CX3C1 CX3CR1 Chemokine A (Rhodopsin) Human - - - CX3CL1
peptide Agonist CX3CL1 peptide - - 2022-07-13
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7WCN 7WCN_refined 2.9 GP119 GPR119 GPR18, GPR55 and GPR119 A (Rhodopsin) Human - Nanobody-35 - AR231453 pubchem gtoplig chembl_ligand
small-molecule Agonist N-palmitoylethanolamine, anandamide, N-oleoylethanolamide, SEA small-molecule Qian Y, Wang J, Yang L, Liu Y, Wang L, Liu W, Lin Y, Yang H, Ma L, Ye S, Wu S, Qiao A 10.1038/S41467-022-34696-6 2022-12-21
Gi/o αi1 Human - 63 β1 Rat γ2 Bovine Cryo-EM 7YU8 - 4.5 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human - scFv16 - [(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate pubchem
small-molecule Agonist 1-O-Oleoyl-D-glycerol 3-phosphoric acid small-molecule Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O 10.1038/S41467-022-33121-2 2022-10-05
Gi/o αi1 Human - 62 β1 Rat γ2 Bovine Cryo-EM 8F7X 8F7X_refined 3.3 OPRX NOP Opioid A (Rhodopsin) Human - scFv16 - nociceptin/orphanin FQ pubchem gtoplig chembl_ligand gtoplig pubchem pubchem
peptide Agonist nociceptin/orphanin FQ peptide Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y, Roth BL, Xu HE 10.1016/J.CELL.2022.12.026 2022-12-14
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8HMV 8HMV_refined 2.9 GPR21 GPR21 A orphans A (Rhodopsin) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Wong TS, Gao W, Chen G, Qiu C, He G, Ye F, Wu Z, Zeng Z, Du Y 10.1002/MCO2.205 2023-03-01
Gq/11 αq Human - 79 β1 Human γ2 Human Cryo-EM 7W40 7W40_refined 3.0 GRPR BB2 Bombesin A (Rhodopsin) Human - scFv16 - Bombesin
peptide Agonist neuromedin B, gastrin releasing peptide(14-27) (human), GRP-(18-27), neuromedin C, gastrin-releasing peptide peptide Peng S, Zhan Y, Zhang D, Ren L, Chen A, Chen ZF, Zhang H 10.1073/PNAS.2216230120 2023-02-22
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8G94 8G94_refined 3.2 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - Early activation antigen CD69 pubchem
peptide Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine small-molecule Chen H, Qin Y, Chou M, Cyster JG, Li X 10.7554/ELIFE.88204 2023-04-19
Gs αs Human - 57 β1 Human γ2 Human Cryo-EM 7XY6 - 3.0 AA2BR A2B Adenosine A (Rhodopsin) Human BRIL - - BAY 60-6583 pubchem gtoplig chembl_ligand
small-molecule Agonist adenosine small-molecule Chen Y, Zhang J, Weng Y, Xu Y, Lu W, Liu W, Liu M, Hua T, Song G 10.1126/SCIADV.ADD3709 2023-05-03
Gs αs Human - 58 β1 Rat γ2 Bovine Cryo-EM 8GW8 - 2.9 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - PCO371 pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist PTHrP-(1-36), PTHrP, PTH, TIP39 peptide Kobayashi K, Kawakami K, Kusakizako T, Tomita A, Nishimura M, Sawada K, Okamoto HH, Hiratsuka S, Nakamura G, Kuwabara R, Noda H, Muramatsu H, Shimizu M, Taguchi T, Inoue A, Murata T, Nureki O 10.1038/S41586-023-06169-3 2023-06-14
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8J19 - 3.2 GPR84 GPR84 A orphans A (Rhodopsin) Human - scFv16 - 6-nonylpyridine-2,4-diol pubchem gtoplig chembl_ligand
small-molecule Agonist - - Liu H, Zhang Q, He X, Jiang M, Wang S, Yan X, Cheng X, Liu Y, Nan FJ, Xu HE, Xie X, Yin W 10.1038/S41467-023-38985-6 2023-06-21
Gq/11 αq Human GRK2 bound 88 - - - - Cryo-EM 8JPC - 3.1 NTR1 NTS1 Neurotensin A (Rhodopsin) Human - GRK2 GRK2 JMV431 gtoplig chembl_ligand pubchem
CHEMBL4576388 chembl_ligand pubchem
peptide
small-molecule 		Agonist
PAM 		large neuromedin N, neuromedin N, neurotensin, large neurotensin peptide Duan J, Liu H, Zhao F, Yuan Q, Ji Y, Cai X, He X, Li X, Li J, Wu K, Gao T, Zhu S, Lin S, Wang MW, Cheng X, Yin W, Jiang Y, Yang D, Xu HE 10.1038/S41586-023-06395-9 2023-08-09
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8HNK - 3.0 CXCR3 CXCR3 Chemokine A (Rhodopsin) Human - scFv16 - CXCL11 gtoplig
peptide Agonist CCL11, CXCL10, CXCL12α, CXCL11, CCL5, CCL19, CCL20, CCL13, CXCL9, CCL7 peptide Jiao H, Pang B, Liu A, Chen Q, Pan Q, Wang X, Xu Y, Chiang YC, Ren R, Hu H 10.1038/S41594-023-01175-5 2023-11-29
Gs αs Human - 59 β1 Rat γ2 Bovine Cryo-EM 8JIU 8JIU_refined 2.8 GLR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - SAR425899
peptide Agonist glucagon peptide Li Y, Zhou Q, Dai A, Zhao F, Chang R, Ying T, Wu B, Yang D, Wang MW, Cong Z 10.1073/PNAS.2303696120 2023-09-13
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 8WRB - 2.9 GPR34 GPR34 A orphans A (Rhodopsin) Human - scFv16 - LYSOPHOSPHATIDIC ACID chembl_ligand pubchem
small-molecule Agonist lysophosphatidylserine small-molecule Liu G, Li X, Wang Y, Zhang X, Gong W 10.1371/JOURNAL.PBIO.3002387 2023-11-08
Gs αs Human - 76 β1 Human γ2 Human Cryo-EM 8GEH 8GEH_refined 4.0 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol pubchem
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gi/o αo Human - 58 β1 Human γ2 Human Cryo-EM 8IYH 8IYH_refined 3.3 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - scFv16 - MK 6892 pubchem gtoplig chembl_ligand pubchem
small-molecule Agonist β-D-hydroxybutyric acid, butyric acid small-molecule - - 2024-03-06
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8JXT 8JXT_refined 3.1 HRH4 H4 Histamine A (Rhodopsin) Human - scFv16 - histamine pubchem gtoplig chembl_ligand drug_central drugbank gtoplig
small-molecule Agonist CCL16, histamine small-molecule Xia R, Shi S, Xu Z, Vischer HF, Windhorst AD, Qian Y, Duan Y, Liang J, Chen K, Zhang A, Guo C, Leurs R, He Y 10.1038/S41467-024-46840-5 2024-03-20
Gs αs Human GTP bound, Class Q 85 β1 Human γ2 Human Cryo-EM 8UO1 8UO1_refined 3.6 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol pubchem
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8X79 8X79_refined 2.4 PI2R IP Prostanoid A (Rhodopsin) Human - Nanobody-35 - MRE-269 pubchem gtoplig chembl_ligand
small-molecule Agonist PGF2α, PGI2, PGD2, thromboxane A2, PGE1, PGE2 small-molecule Wang JJ, Jin S, Zhang H, Xu Y, Hu W, Jiang Y, Chen C, Wang DW, Xu HE, Wu C 10.1126/SCIADV.ADK5184 2024-03-06
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 8Y52 8Y52_refined 2.9 BRS3 BB3 Bombesin A (Rhodopsin) Human - - - Bombesin
peptide Agonist - - Li C, Xu Y, Su W, He X, Li J, Li X, Xu HE, Yin W 10.1016/J.CELREP.2024.114511 2024-09-11
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 9ERX 9ERX_refined 2.9 CNR1 CB1 Cannabinoid A (Rhodopsin) Human - scFv16 - HU-210 pubchem gtoplig chembl_ligand
small-molecule Agonist anandamide small-molecule - - 2024-06-26
Gs αs Human Mini-Gs 55 β1 Human γ2 Human Cryo-EM 8UY0 - 3.2 OR2T2 OR2T2 Odorant family 2 O2 (tetrapod specific odorant) Human - Nanobody-35 - (5S)-2-methyl-5-(prop-1-en-2-yl)cyclohex-2-en-1-one pubchem
small-molecule Agonist - - de March CA, Ma N, Billesbolle CB, Tewari J, Llinas Del Torrent C, van der Velden WJC, Ojiro I, Takayama I, Faust B, Li L, Vaidehi N, Manglik A, Matsunami H 10.1038/S41586-024-08126-0 2024-10-30
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 8YNA - 2.6 HRH4 H4 Histamine A (Rhodopsin) Human - scFv16 - immepip pubchem gtoplig chembl_ligand
small-molecule Agonist CCL16, histamine small-molecule - - 2024-10-09
Gs αs Bovine - 56 β1 Rat γ2 Bovine Cryo-EM 6NBI - 4.0 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - Long-acting parathyroid hormone analog
peptide Agonist PTHrP-(1-36), PTHrP, PTH, TIP39 peptide Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y 10.1126/SCIENCE.AAV7942 2019-04-17
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/intermedin gtoplig
peptide Agonist - - Liang YL, Belousoff MJ, Fletcher MM, Zhang X, Khoshouei M, Deganutti G, Koole C, Furness SGB, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Danev R, Wootten D, Sexton PM 10.1021/ACSPTSCI.9B00080 2020-04-01
Gs αs Human - 58 β1 Rat γ2 Bovine Cryo-EM 7D3S 7D3S_refined 2.9 SCTR secretin Glucagon B1 (Secretin) Human - Nanobody-35 - SECRETIN chembl_ligand pubchem
protein Agonist VIP, secretin peptide Fukuhara S, Kobayashi K, Kusakizako T, Iida W, Kato M, Shihoya W, Nureki O 10.1016/J.BBRC.2020.08.042 2020-11-04
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7CMU - 3.0 DRD3 D3 Dopamine A (Rhodopsin) Human BRIL scFv16 - pramipexole pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist dopamine small-molecule Xu P, Huang S, Mao C, Krumm BE, Zhou XE, Tan Y, Huang XP, Liu Y, Shen DD, Jiang Y, Yu X, Jiang H, Melcher K, Roth BL, Cheng X, Zhang Y, Xu HE 10.1016/J.MOLCEL.2021.01.003 2021-03-10
Gi/o αi2 Human - 59 β1 Human γ2 Human Cryo-EM 7LD3 - 3.2 AA1R A1 Adenosine A (Rhodopsin) Human - - - {2-Amino-4-[3,5-bis(trifluoromethyl)phenyl]thiophen-3-yl}(4-chlorophenyl)methanone pubchem
adenosine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule
small-molecule 		Ago-PAM
Agonist 		adenosine small-molecule Draper-Joyce CJ, Bhola R, Wang J, Bhattarai A, Nguyen ATN, Cowie-Kent I, O'Sullivan K, Chia LY, Venugopal H, Valant C, Thal DM, Wootten D, Panel N, Carlsson J, Christie MJ, White PJ, Scammells P, May LT, Sexton PM, Danev R, Miao Y, Glukhova A, Imlach WL, Christopoulos A 10.1038/S41586-021-03897-2 2021-09-08
Gq/11 αq Human Gq-Gs chimera 57 β1 Human γ2 Human Cryo-EM 7S8P 7S8P_refined 2.6 MRGX4 MRGPRX4 A orphans A (Rhodopsin) Human BRIL scFv16 - N-[(1r,3R,5S,7R)-3,5-dimethyltricyclo[3.3.1.1~3,7~]decane-1-carbonyl]-D-phenylalanine pubchem
small-molecule Agonist - - Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL 10.1038/S41586-021-04126-6 2021-11-17
Gs αs Human Gs-Gi1 chimera 57 β1 Human γ2 Human Cryo-EM 7P02 - 2.9 NK1R NK1 Tachykinin A (Rhodopsin) Human - scFv16 - substance P pubchem gtoplig chembl_ligand gtoplig gtoplig
peptide Agonist neuropeptide-γ, hemokinin 1, neurokinin A, neuropeptide K, neurokinin B, substance P peptide Thom C, Ehrenmann J, Vacca S, Waltenspuhl Y, Schoppe J, Medalia O, Pluckthun A 10.1126/SCIADV.ABK2872 2021-12-15
Gi/o αi1 Human - 62 β1 Rat γ2 Bovine Cryo-EM 7T6U - 2.9 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human - - - synthetic peptide
peptide Agonist LXA4, serum amyloid A, PrP106-126, aspirin-triggered resolvin D1, humanin, aspirin triggered lipoxin A4, LL-37, annexin I, resolvin D1 peptide Zhuang Y, Wang L, Guo J, Sun D, Wang Y, Liu W, Xu HE, Zhang C 10.1038/S41467-022-28586-0 2022-03-30
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7TYF - 2.2 CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP1 		- amylin peptide
peptide Agonist calcitonin, adrenomedullin, amylin, α-CGRP, adrenomedullin 2/intermedin, β-CGRP peptide Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM 10.1126/SCIENCE.ABM9609 2022-03-23
Gq/11 αq Human - 59 β1 Human γ2 Human Cryo-EM 7W57 - 3.2 NMUR2 NMU2 Neuromedin U A (Rhodopsin) Human - scFv16 - Neuromedin-S
peptide Agonist neuromedin U-25, neuromedin S-36, neuromedin S-33, neuromedin U-23 peptide You C, Zhang Y, Xu P, Huang S, Yin W, Eric Xu H, Jiang Y 10.1038/S41467-022-29683-W 2022-04-20
Gq/11 αq Human - 61 β1 Human γ2 Human Cryo-EM 7XOX 7XOX_refined 3.1 GASR CCK2 Cholecystokinin A (Rhodopsin) Human - scFv16 - CCK-8 pubchem gtoplig chembl_ligand drug_central drugbank
peptide Agonist CCK-8, desulfated cholecystokinin-8, gastrin-14, CCK-58, desulfated gastrin-17, CCK-39, CCK-33, desulfated gastrin-34, gastrin-34, gastrin-71, desulfated gastrin-71, CCK-4, desulfated gastrin-14, gastrin-17 peptide Ding Y, Zhang H, Liao YY, Chen LN, Ji SY, Qin J, Mao C, Shen DD, Lin L, Wang H, Zhang Y, Li XM 10.1038/S41421-022-00420-3 2022-07-20
Gi/o αgust Human - 63 β1 Human γ2 Human Cryo-EM 7XP6 - 3.0 T2R46 TAS2R46 Taste 2 T2 (Taste 2) Human - Nanobody-35 Endoglucanase H strychnine pubchem gtoplig chembl_ligand drug_central drugbank gtoplig
small-molecule Agonist - - Xu W, Wu L, Liu S, Liu X, Cao X, Zhou C, Zhang J, Fu Y, Guo Y, Wu Y, Tan Q, Wang L, Liu J, Jiang L, Fan Z, Pei Y, Yu J, Cheng J, Zhao S, Hao X, Liu ZJ, Hua T 10.1126/SCIENCE.ABO1633 2022-10-12
Gi/o αi1 Human - 64 β1 Rat γ2 Bovine Cryo-EM 8EF5 - 3.3 OPRM μ Opioid A (Rhodopsin) Human - scFv16 - fentanyl pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist endomorphin-1, β-endorphin, dynorphin A, dynorphin A-(1-8), [Leu]enkephalin, dynorphin A-(1-13), dynorphin B, [Met]enkephalin, endomorphin-2 peptide Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, Rao Q, Yang J, Liu J, Zhou Q, Wang X, Liu M, Liu W, Jiang X, Yang D, Jiang H, Shen J, Melcher K, Chen H, Jiang Y, Cheng X, Wang MW, Xie X, Xu HE 10.1016/J.CELL.2022.09.041 2022-11-09
G12/13 α13 Human - 60 β1 Human γ2 Human Cryo-EM 8H8J 8H8J_refined 3.2 GPR35 GPR35 A orphans A (Rhodopsin) Human - scFv16 - lodoxamide pubchem gtoplig chembl_ligand drug_central drugbank
small-molecule Agonist 2-Oleoyllysophosphatydic acid, 2-oleoyl-LPA, 1-Lyso-2-oleoyl-phosphatidic acid, kynurenic acid small-molecule Duan J, Liu Q, Yuan Q, Ji Y, Zhu S, Tan Y, He X, Xu Y, Shi J, Cheng X, Jiang H, Eric Xu H, Jiang Y 10.1038/S41421-022-00499-8 2023-02-08
Gq/11 αq Human - 61 β1 Human γ2 Human Cryo-EM 8HCX 8HCX_refined 3.5 EDNRB ETB Endothelin A (Rhodopsin) Human - scFv16 - ENDOTHELIN chembl_ligand pubchem
protein Agonist endothelin-2, endothelin-3, endothelin-1 peptide - - 2023-03-22
Gs αs Human - 45 β1 Human γ2 Human Cryo-EM 8IW4 - 3.5 TAAR9 TAAR9 A orphans A (Rhodopsin) Mouse - scFv16 - SPERMIDINE chembl_ligand pubchem
small-molecule Agonist - - Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP 10.1038/S41586-023-06106-4 2023-05-31
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7Y1F 7Y1F_refined 3.3 OPRK κ Opioid A (Rhodopsin) Human - scFv16 - dynorphin A-(1-8) pubchem gtoplig chembl_ligand pubchem pubchem
peptide Agonist α-neoendorphin, big dynorphin, β-endorphin, dynorphin A, dynorphin A-(1-8), [Leu]enkephalin, dynorphin A-(1-13), β-neoendorphin, dynorphin B, [Met]enkephalin peptide Chen Y, Chen B, Wu T, Zhou F, Xu F 10.1093/PROCEL/PWAC033 2023-05-24
Gi/o αi1 Human - 63 β1 Rat γ2 Bovine Cryo-EM 8HK5 8HK5_refined 3.0 C5AR1 C5a1 Complement peptide A (Rhodopsin) Human - - - C5a gtoplig
peptide Agonist ribosomal protein S19, C3a, C5a, C5a des-Arg peptide Wang Y, Liu W, Xu Y, He X, Yuan Q, Luo P, Fan W, Zhu J, Zhang X, Cheng X, Jiang Y, Xu HE, Zhuang Y 10.1038/S41589-023-01339-W 2023-05-10
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 8IUK - 2.7 PF2R FP Prostanoid A (Rhodopsin) Human - scFv16
Nanobody-35 		- PGF2α pubchem gtoplig chembl_ligand drug_central drugbank
small-molecule Agonist PGF2α, PGI2, PGD2, thromboxane A2, PGE2 small-molecule - - 2023-07-12
Gi/o αi1 Human - 58 β1 Human γ2 Human Cryo-EM 8GDC 8GDC_refined 3.5 PE2R3 EP3 Prostanoid A (Rhodopsin) Human - - - PGE2 pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
small-molecule Agonist PGF2α, PGI2, PGD2, thromboxane A2, PGE1, PGE2 small-molecule Huang SM, Xiong MY, Liu L, Mu J, Wang MW, Jia YL, Cai K, Tie L, Zhang C, Cao S, Wen X, Wang JL, Guo SC, Li Y, Qu CX, He QT, Cai BY, Xue C, Gan S, Xie Y, Cong X, Yang Z, Kong W, Li S, Li Z, Xiao P, Yang F, Yu X, Guan YF, Zhang X, Liu Z, Yang BX, Du Y, Sun JP 10.1073/PNAS.2216329120 2024-01-10
Gq/11 αq Human - 58 β1 Human γ2 Human Cryo-EM 8I9A - 3.6 C3AR C3a Complement peptide A (Rhodopsin) Human - scFv16 - EP54 ligand
peptide Agonist C5a, C3a peptide Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C 10.1016/J.CELL.2023.09.020 2023-10-18
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8J6R - 2.8 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - scFv16 - MK 6892 pubchem gtoplig chembl_ligand pubchem
small-molecule Agonist β-D-hydroxybutyric acid, butyric acid small-molecule Mao C, Gao M, Zang SK, Zhu Y, Shen DD, Chen LN, Yang L, Wang Z, Zhang H, Wang WW, Shen Q, Lu Y, Ma X, Zhang Y 10.1038/S41467-023-43537-Z 2023-12-06
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8K4N 8K4N_refined 2.8 GPR34 GPR34 A orphans A (Rhodopsin) Human - scFv16 - (2R)-2-azanyl-3-[oxidanyl-[(2R)-2-oxidanyl-3-tetradec-9-enoyloxy-propoxy]phosphoryl]oxy-propanoic acid pubchem
small-molecule Agonist lysophosphatidylserine small-molecule - - 2023-10-25
Gq/11 αq Human - 58 β1 Human γ2 Human Cryo-EM 8WC9 - 3.2 TAAR1 TA1 Trace amine A (Rhodopsin) Mouse - scFv16 - CHEMBL476516 chembl_ligand pubchem
small-molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine small-molecule Shang P, Rong N, Jiang JJ, Cheng J, Zhang MH, Kang D, Qi L, Guo L, Yang GM, Liu Q, Zhou Z, Li XB, Zhu KK, Meng QB, Han X, Yan W, Kong Y, Yang L, Wang X, Lei D, Feng X, Liu X, Yu X, Wang Y, Li Q, Shao ZH, Yang F, Sun JP 10.1016/J.CELL.2023.10.014 2023-12-27
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8GE6 8GE6_refined 3.4 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol pubchem
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human - 61 β1 Human γ2 Human Cryo-EM 8GG8 - 3.3 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol pubchem
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gi/o αo Human - 58 β1 Human γ2 Human Cryo-EM 8JER 8JER_refined 3.5 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - scFv16 - 5-Methyl-4-oxidanyl-pyrazin-4-ium-2-carboxylic acid pubchem
small-molecule Agonist β-D-hydroxybutyric acid, butyric acid small-molecule Yadav MK, Sarma P, Maharana J, Ganguly M, Mishra S, Zaidi N, Dalal A, Singh V, Saha S, Mahajan G, Sharma S, Chami M, Banerjee R, Shukla AK 10.1038/S41467-024-46239-2 2024-03-06
Gs αs Human - 56 β1 Human γ2 Human Cryo-EM 8POK 8POK_refined 3.4 HRH2 H2 Histamine A (Rhodopsin) Human - Nanobody-35 - histamine pubchem gtoplig chembl_ligand drug_central drugbank gtoplig
small-molecule Agonist histamine small-molecule Kock Z, Schnelle K, Persechino M, Umbach S, Schihada H, Januliene D, Parey K, Pockes S, Kolb P, Dotsch V, Moller A, Hilger D, Bernhard F 10.1038/S41467-024-46096-Z 2024-03-06
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8U4P - 3.2 CXCR4 CXCR4 Chemokine A (Rhodopsin) Human - - - plerixafor pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist CXCL12α, CXCL12, CXCL12γ, CXCL12φ, CXCL12β, CXCL12δ, CXCL12ε peptide Saotome K, McGoldrick LL, Ho JH, Ramlall TF, Shah S, Moore MJ, Kim JH, Leidich R, Olson WC, Franklin MC 10.1038/S41594-024-01397-1 2024-03-13
Gs αs Human GTP bound, Class K 59 β1 Human γ2 Human Cryo-EM 8UNV - 3.3 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol pubchem
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gq/11 αq Human - 59 β1 Human γ2 Human Cryo-EM 8XOG - 2.9 GPER1 GPER Estrogen (G protein-coupled) A (Rhodopsin) Human - scFv16 - Apo (no ligand)
none Apo (no ligand) 17β-estradiol small-molecule Liu H, Guo S, Dai A, Xu P, Li X, Huang S, He X, Wu K, Zhang X, Yang D, Xie X, Xu HE 10.1038/S41422-024-00963-Y 2024-04-10
Gi/o αi1 Human - 57 β1 Human γ2 Human Cryo-EM 8ZPS 8ZPS_refined 3.0 PRLHR PrRP Prolactin-releasing peptide A (Rhodopsin) Human - scFv16 - Prolactin-releasing peptide PrRP20
peptide Agonist PrRP-20, neuropeptide Y, PrRP-31, PTHrP peptide Li Y, Yuan Q, He X, Zhang Y, You C, Wu C, Li J, Xu HE, Zhao LH 10.1038/S41421-024-00724-6 2024-09-25
Gi/o αi2 Human - 63 β1 Human γ2 Human Cryo-EM 8K6M 8K6M_refined 3.3 NPY1R Y1 Neuropeptide Y A (Rhodopsin) Human - scFv16 - neuropeptide Y pubchem gtoplig chembl_ligand gtoplig gtoplig pubchem pubchem pubchem
peptide Agonist peptide YY, pancreatic polypeptide, neuropeptide Y peptide - - 2024-07-31
Gi/o αi1 Human - 65 β1 Human γ2 Human Cryo-EM 9EPQ - 4.2 B1B1U5 Rhodopsin Opsins A (Rhodopsin) Hasarius adansoni - - - 11,20-Ethanoretinal pubchem
small-molecule Agonist - - - - 2024-10-23
Gi/o αt1 Bovine Only H5 3 - - - - X-ray 4BEY 4BEY_refined 2.9 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - Apo (no ligand)
none Apo (no ligand) - - Singhal A, Ostermaier MK, Vishnivetskiy SA, Panneels V, Homan KT, Tesmer JJ, Veprintsev D, Deupi X, Gurevich VV, Schertler GF, Standfuss J 10.1038/EMBOR.2013.44 2013-05-08
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 - - Tsai CJ, Pamula F, Nehme R, Muhle J, Weinert T, Flock T, Nogly P, Edwards PC, Carpenter B, Gruhl T, Ma P, Deupi X, Standfuss J, Tate CG, Schertler GFX 10.1126/SCIADV.AAT7052 2018-10-03
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 8G05 - 3.0 GPR84 GPR84 A orphans A (Rhodopsin) Human - scFv16 - 6-Octylimino-1,3-diazinane-2,4-dione pubchem
lipid Agonist - - Zhang X, Wang Y, Supekar S, Cao X, Zhou J, Dang J, Chen S, Jenkins L, Marsango S, Li X, Liu G, Milligan G, Feng M, Fan H, Gong W, Zhang C 10.1038/S41467-023-41201-0 2023-11-01
Gi/o αi1 Human - 60 β1 Human γ2 Human Cryo-EM 8HQN 8HQN_refined 3.0 GP132 GPR132 A orphans A (Rhodopsin) Human BRIL scFv16 - 9-hydroxyoctadecadienoic acid pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist 9-hydroxyoctadecadienoic acid small-molecule Wang JL, Dou XD, Cheng J, Gao MX, Xu GF, Ding W, Ding JH, Li Y, Wang SH, Ji ZW, Zhao XY, Huo TY, Zhang CF, Liu YM, Sha XY, Gao JR, Zhang WH, Hao Y, Zhang C, Sun JP, Jiao N, Yu X 10.1038/S42255-023-00899-4 2023-10-11
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8KH4 8KH4_refined 3.1 GP161 GPR161 A orphans A (Rhodopsin) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Nie Y, Qiu Z, Chen S, Chen Z, Song X, Ma Y, Huang N, Cyster JG, Zheng S 10.1038/S41467-023-41654-3 2023-10-11
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8WC3 - 3.0 TAAR1 TA1 Trace amine A (Rhodopsin) Mouse - scFv16 - ulotaront pubchem gtoplig drugbank chembl_ligand
small-molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine small-molecule Shang P, Rong N, Jiang JJ, Cheng J, Zhang MH, Kang D, Qi L, Guo L, Yang GM, Liu Q, Zhou Z, Li XB, Zhu KK, Meng QB, Han X, Yan W, Kong Y, Yang L, Wang X, Lei D, Feng X, Liu X, Yu X, Wang Y, Li Q, Shao ZH, Yang F, Sun JP 10.1016/J.CELL.2023.10.014 2023-12-27
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8GDZ - 3.5 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol pubchem
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8GG2 - 3.0 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol pubchem
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gq/11 αq Human Gq-Gs chimera 60 β1 Human γ2 Human Cryo-EM 8J9N - 3.5 FZD1 FZD1 Frizzled F (Frizzled) Human - scFv16 - Apo (no ligand)
none Apo (no ligand) Wnt-7b, Wnt-5a, Wnt-1, Wnt-2, Wnt-3a peptide Zhang Z, Lin X, Wei L, Wu Y, Xu L, Wu L, Wei X, Zhao S, Zhu X, Xu F 10.1038/S41421-023-00627-Y 2024-01-17
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 8PJK - 2.4 5HT1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human - - - 6-[3-[2-(2-methoxyphenoxy)ethylamino]propoxy]-4~{H}-1,4-benzoxazin-3-one pubchem
(2r)-1-(Heptadecanoyloxy)-3-{[(R)-Hydroxy{[(1r,2r,3r,4r,5s,6r)-2,3,5,6-Tetrahydroxy-4-(Phosphonooxy)cyclohexyl]oxy}phosphoryl]oxy}propan-2-Yl (5z,8z,11z,14z)-Icosa-5,8,11,14-Tetraenoate pubchem
small-molecule
small-molecule 		Agonist
PAM 		5-hydroxytryptamine small-molecule - - 2024-05-29
Gs αs Human GTP bound, Class F 61 β1 Human γ2 Human Cryo-EM 8UNQ - 3.3 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol pubchem
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8WG7 8WG7_refined 2.5 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide peptide Cong Z, Zhao F, Li Y, Luo G, Mai Y, Chen X, Chen Y, Lin S, Cai X, Zhou Q, Yang D, Wang MW 10.1038/S41421-024-00649-0 2024-03-06
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8X8N 8X8N_refined 2.9 SSR5 SST5 Somatostatin A (Rhodopsin) Human - scFv16 - Octreotide pubchem
peptide Agonist cortistatin-14, SRIF-14, CST-17, SRIF-28 peptide - - 2024-06-12
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8XZI 8XZI_refined 2.7 APJ apelin Apelin A (Rhodopsin) Human - - - CMF-019 pubchem gtoplig chembl_ligand
small-molecule Agonist apelin-36, apelin-17, apelin-13, Elabela/Toddler-21, Elabela/Toddler-32, Elabela/Toddler-11, [Pyr1]apelin-13, apelin receptor early endogenous ligand peptide - - 2024-03-20
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 9AUC - 2.4 CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP1 		- Calcitonin gene-related peptide 1 pubchem
peptide Agonist calcitonin, adrenomedullin, amylin, α-CGRP, adrenomedullin 2/intermedin, β-CGRP peptide Cao J, Belousoff MJ, Danev R, Christopoulos A, Wootten D, Sexton PM 10.1021/ACS.BIOCHEM.4C00114 2024-04-24
Gs αs Human Mini-Gq 60 β1 Human γ2 Human Cryo-EM 8YN3 - 2.6 HRH2 H2 Histamine A (Rhodopsin) Human - Nanobody-35 - histamine pubchem gtoplig chembl_ligand drug_central drugbank gtoplig
small-molecule Agonist histamine small-molecule Zhang X, Liu G, Zhong YN, Zhang R, Yang CC, Niu C, Pu X, Sun J, Zhang T, Yang L, Zhang C, Li X, Shen X, Xiao P, Sun JP, Gong W 10.1038/S41467-024-52585-Y 2024-10-09
Gq/11 αq Human Mini-Gq 57 β1 Rat γ2 Bovine Cryo-EM 9JR2 - 2.8 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human