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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 - scFv16 - Parathyroid hormone pubchem
peptide Agonist PTHrP-(1-36), PTHrP, PTH, TIP39 peptide - - 2024-10-16
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 6KPF 6KPF_refined 2.9 CNR2 CB2 Cannabinoid A (Rhodopsin) Human - scFv16 - AM12033 pubchem
small-molecule Agonist 2-arachidonoylglycerol, anandamide small-molecule Hua T, Li X, Wu L, Iliopoulos-Tsoutsouvas C, Wang Y, Wu M, Shen L, Brust CA, Nikas SP, Song F, Song X, Yuan S, Sun Q, Wu Y, Jiang S, Grim TW, Benchama O, Stahl EL, Zvonok N, Zhao S, Bohn LM, Makriyannis A, Liu ZJ 10.1016/J.CELL.2020.01.008 2020-02-12
Gi/o αt2 Bovine Only H5 3 - - - - X-ray 6PH7 6PH7_refined 2.9 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - Nerol pubchem
small-molecule unknown - - - - 2020-07-01
Gi/o αi1 Human - 65 β1 Human γ2 Human Cryo-EM 6LFM 6LFM_refined 3.5 CXCR2 CXCR2 Chemokine A (Rhodopsin) Human - scFv16 - Interleukin-8 pubchem
protein Agonist CXCL3, CXCL8, CXCL7, CXCL2, CXCL1, CXCL6, CXCL5 peptide Liu K, Wu L, Yuan S, Wu M, Xu Y, Sun Q, Li S, Zhao S, Hua T, Liu ZJ 10.1038/S41586-020-2492-5 2020-09-02
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7E33 7E33_refined 2.9 5HT1E 5-HT1E 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - BRL-54443 pubchem gtoplig chembl_ligand
small-molecule Agonist 5-hydroxytryptamine, tryptamine 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
Gq/11 αq Human Engineered G alpha 59 β1 Human γ2 Human Cryo-EM 7F9Y - 2.9 GHSR ghrelin Ghrelin A (Rhodopsin) Human - Nanobody-35 - ghrelin 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
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7VV3 - 3.0 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human - scFv16 - Cortistatin 14 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
Gi/o αi1 Mouse - 62 β1 Bovine γ2 Bovine Cryo-EM 7TD1 - 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 αo Human - 61 β1 Human γ2 Human Cryo-EM 7EJK - 3.4 ADA2A α2A Adrenoceptors A (Rhodopsin) Human - scFv16 - oxymetazoline 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
G12/13 α13 Human - 60 β1 Human γ2 Human Cryo-EM 7T6B 7T6B_refined 3.2 S1PR2 S1P2 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 Chen H, Chen K, Huang W, Staudt LM, Cyster JG, Li X 10.1126/SCIADV.ABN0067 2022-04-06
Gs αs Bovine - 60 β1 Rat γ2 Bovine Cryo-EM 7VQX - 2.7 VIPR2 VPAC2 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - PACAP-27 pubchem gtoplig pubchem
peptide Agonist GHRH, VIP, PACAP-27, PHI, secretin, PACAP-38 peptide Xu Y, Feng W, Zhou Q, Liang A, Li J, Dai A, Zhao F, Yan J, Chen CW, Li H, Zhao LH, Xia T, Jiang Y, Xu HE, Yang D, Wang MW 10.1038/S41467-022-30041-Z 2022-05-18
Gs αs Human - 60 β1 Rat γ2 Human Cryo-EM 7X8S 7X8S_refined 3.1 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - WB4-24 pubchem gtoplig chembl_ligand
small-molecule Agonist glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide peptide Cong Z, Zhou Q, Li Y, Chen LN, Zhang ZC, Liang A, Liu Q, Wu X, Dai A, Xia T, Wu W, Zhang Y, Yang D, Wang MW 10.1073/PNAS.2200155119 2022-06-29
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 7WXU - 2.9 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 7YU6 7YU6_refined 3.5 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 8F7S 8F7S_refined 3.0 OPRD δ Opioid A (Rhodopsin) Human - - - DELTORPHIN II chembl_ligand pubchem
protein Agonist endomorphin-1, α-neoendorphin, β-endorphin, dynorphin A, dynorphin A-(1-8), [Leu]enkephalin, dynorphin A-(1-13), dynorphin B, [Met]enkephalin 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
Gq/11 αq Human - 97 β1 Human γ2 Human Cryo-EM 7F6G 7F6G_refined 2.9 AGTR1 AT1 Angiotensin A (Rhodopsin) Human - - - SAR1-AngII
peptide Agonist angiotensin IV, angiotensin A, angiotensin III, angiotensin II peptide - - 2023-03-29
Gq/11 αq Human Mini-Gq 57 β1 Human γ2 Human Cryo-EM 8FMZ - 2.6 NTR1 NTS1 Neurotensin A (Rhodopsin) Rat - scFv16 - neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
peptide Agonist neuromedin N, neurotensin peptide Krumm BE, DiBerto JF, Olsen RHJ, Kang HJ, Slocum ST, Zhang S, Strachan RT, Huang XP, Slosky LM, Pinkerton AB, Barak LS, Caron MG, Kenakin T, Fay JF, Roth BL 10.1021/ACS.BIOCHEM.3C00029 2023-03-29
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8ID8 - 3.0 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - scFv16 - TUG-891 pubchem gtoplig chembl_ligand
small-molecule Agonist oleic acid, myristic acid, α-linolenic acid, linoleic acid small-molecule Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP 10.1126/SCIENCE.ADD6220 2023-03-15
Gi/o αgust Human - 58 β1 Human γ2 Human Cryo-EM 8DZR - 2.6 OPRK κ Opioid A (Rhodopsin) Human - scFv16 - CHEMBL277863 chembl_ligand pubchem
small-molecule 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 Han J, Zhang J, Nazarova AL, Bernhard SM, Krumm BE, Zhao L, Lam JH, Rangari VA, Majumdar S, Nichols DE, Katritch V, Yuan P, Fay JF, Che T 10.1038/S41586-023-06030-7 2023-05-03
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8FLQ - 2.6 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - Parathyroid hormone
peptide Agonist PTHrP-(1-36), PTHrP, PTH, TIP39 peptide Cary BP, Gerrard EJ, Belousoff MJ, Fletcher MM, Jiang Y, Russell IC, Piper SJ, Wootten D, Sexton PM 10.1016/J.STR.2023.04.002 2023-04-26
Gq/11 αq Human Mini-Gq 60 β1 Human γ2 Human Cryo-EM 8H4K - 3.1 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - Nanobody-35 - GW9508 pubchem gtoplig chembl_ligand
small-molecule Agonist oleic acid, myristic acid, α-linolenic acid, linoleic acid small-molecule Yin H, Inoue A, Ma Z, Zhu X, Xia R, Xu Z, Wang N, Duan Y, Zhang A, Guo C, He Y 10.1038/S41422-023-00835-X 2023-06-21
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8JD3 - 3.3 GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human - - - L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem
JNJ-40411813 pubchem gtoplig chembl_ligand drugbank
small-molecule
small-molecule 		Agonist
PAM 		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 - 60 β1 Human γ2 Human Cryo-EM 8HQM 8HQM_refined 3.0 GP132 GPR132 A orphans A (Rhodopsin) Human BRIL scFv16 - CHEMBL3354065 chembl_ligand pubchem
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 Bovine - 59 β1 Rat γ2 Bovine Cryo-EM 8ITL - 3.2 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 - 61 β1 Human γ2 Human Cryo-EM 8JLN - 3.2 TAAR1 TA1 Trace amine A (Rhodopsin) Human BRIL scFv16 - CHEMBL1182312 chembl_ligand 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
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8GE2 - 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 8GG4 - 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
Gq/11 αq Human - 59 β1 Rat γ2 Bovine Cryo-EM 8JBH 8JBH_refined 2.9 NK3R NK3 Tachykinin A (Rhodopsin) Human - scFv16 - Protachykinin-1
peptide Agonist neurokinin A, substance P, neurokinin B peptide - - 2024-02-07
Gq/11 αq Human - 58 β1 Human γ2 Human Cryo-EM 8XJN 8XJN_refined 3.1 TA2R TP Prostanoid A (Rhodopsin) Human - scFv16 - cloprostenol pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist PGF2α, PGH2, PGI2, PGD2, thromboxane A2, PGE2 small-molecule - - 2024-02-28
Gi/o αi1 Human - 60 β1 Rat γ2 Bovine Cryo-EM 8YKW 8YKW_refined 2.8 SUCR1 succinate Succinate A (Rhodopsin) Human - scFv16 - succinic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem
small-molecule Agonist succinic acid small-molecule Li C, Liu H, Li J, He X, Zhu H, Fu W, Xu HE 10.1038/S41422-024-00984-7 2024-05-29
Gi/o αt1 Bovine Only H5 3 - - - - X-ray 4A4M 4A4M_refined 3.3 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - Retinal (all-trans) pubchem
small-molecule Agonist - - Deupi X, Edwards P, Singhal A, Nickle B, Oprian D, Schertler G, Standfuss J 10.1073/PNAS.1114089108 2012-01-25
Gs αs Human - 43 β1 Human γ2 Human Cryo-EM 6NIY - 3.3 CALCR CT Calcitonin B1 (Secretin) Human - - - calcitonin (salmon synthetic) pubchem
small-molecule Agonist calcitonin, adrenomedullin, amylin, α-CGRP, adrenomedullin 2/intermedin, β-CGRP peptide Dal Maso E, Glukhova A, Zhu Y, Garcia-Nafria J, Tate CG, Atanasio S, Reynolds CA, Ramirez-Aportela E, Carazo JM, Hick CA, Furness SGB, Hay DL, Liang YL, Miller LJ, Christopoulos A, Wang MW, Wootten D, Sexton PM 10.1021/ACSPTSCI.8B00056 2019-01-23
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 6LMK 6LMK_refined 3.7 GLR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - 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
Gi/o αo Human - 61 β1 Human γ2 Human Cryo-EM 7D76 - 3.1 AGRG3 ADGRG3 ADGRG B2 (Adhesion) Human - - - Beclomethasone pubchem
small-molecule Agonist - - Ping YQ, Mao C, Xiao P, Zhao RJ, Jiang Y, Yang Z, An WT, Shen DD, Yang F, Zhang H, Qu C, Shen Q, Tian C, Li ZJ, Li S, Wang GY, Tao X, Wen X, Zhong YN, Yang J, Yi F, Yu X, Xu HE, Zhang Y, Sun JP 10.1038/S41586-020-03083-W 2021-02-03
Gi/o αi3 Human - 63 β1 Human γ2 Human Cryo-EM 7E9H - 4.0 GRM4 mGlu4 Metabotropic glutamate C (Glutamate) Human - scFv16 - L-serine-O-phosphate pubchem gtoplig chembl_ligand drugbank drug_central pubchem
small-molecule Agonist L-glutamic acid, L-serine-O-phosphate small-molecule Lin S, Han S, Cai X, Tan Q, Zhou K, Wang D, Wang X, Du J, Yi C, Chu X, Dai A, Zhou Y, Chen Y, Zhou Y, Liu H, Liu J, Yang D, Wang MW, Zhao Q, Wu B 10.1038/S41586-021-03495-2 2021-06-23
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7S8O - 2.6 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human BRIL scFv16 - (R)-ZINC-3573 pubchem gtoplig chembl_ligand
small-molecule Agonist PAMP-20 peptide 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
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7EO2 7EO2_refined 2.9 S1PR1 S1P1 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 Xu Z, Ikuta T, Kawakami K, Kise R, Qian Y, Xia R, Sun MX, Zhang A, Guo C, Cai XH, Huang Z, Inoue A, He Y 10.1038/S41589-021-00930-3 2022-01-05
Gi/o αi3 Human - 62 β1 Human γ2 Human Cryo-EM 7T11 7T11_refined 2.7 SSR2 SST2 Somatostatin A (Rhodopsin) Human - scFv16 - Octreotide
peptide Agonist cortistatin-14, SRIF-14, CST-17, SRIF-28 peptide Robertson MJ, Meyerowitz JG, Panova O, Borrelli K, Skiniotis G 10.1038/S41594-022-00727-5 2022-03-09
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7TYW - 3.0 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 2022-03-23
Gi/o αi1 Human - 63 β1 Bovine γ2 Bovine Cryo-EM 7S0F - 3.0 ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey - - - LEVISOPRENALINE chembl_ligand chembl_ligand pubchem
small-molecule Agonist - - Alegre KO, Paknejad N, Su M, Lou JS, Huang J, Jordan KD, Eng ET, Meyerson JR, Hite RK, Huang XY 10.1038/S41594-021-00679-2 2021-11-17
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7X2C 7X2C_refined 3.2 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - fenoldopam pubchem gtoplig chembl_ligand drugbank drug_central pubchem gtoplig chembl_ligand pubchem pubchem gtoplig chembl_ligand pubchem
small-molecule Agonist 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 2022-06-29
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7W0N - 4.2 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
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7XW6 - 2.8 TSHR TSH Glycoprotein hormone A (Rhodopsin) Human - Nanobody-35 - M22 antibody light chain
M22 antibody heavy chain
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 2022-08-17
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8J6P - 2.6 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 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
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8WC6 - 3.2 TAAR1 TA1 Trace amine A (Rhodopsin) Mouse - scFv16
Nanobody-35 		- 2-Phenylethanaminium 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 - 60 β1 Human γ2 Human Cryo-EM 8GE3 - 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 - 60 β1 Human γ2 Human Cryo-EM 8GG5 - 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
Gi/o αi1 Human - 41 β1 Human γ2 Human Cryo-EM 8I7V - 2.8 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 Park JH, Kawakami K, Ishimoto N, Ikuta T, Ohki M, Ekimoto T, Ikeguchi M, Lee DS, Lee YH, Tame JRH, Inoue A, Park SY 10.1038/S41467-023-42764-8 2024-02-07
Gs αs Human - 61 β1 Human γ2 Human Cryo-EM 8JHB - 3.3 FZD6 FZD6 Frizzled F (Frizzled) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) Wnt-5a, Wnt-4, 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 αi3 Human - 63 β1 Human γ2 Human Cryo-EM 8SZI - 3.5 CASR CaS Calcium-sensing C (Glutamate) Human - - - L-tryptophan pubchem gtoplig chembl_ligand drugbank drug_central pubchem
L-tryptophan pubchem gtoplig chembl_ligand drugbank drug_central pubchem
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 O 57 β1 Human γ2 Human Cryo-EM 8UNZ 8UNZ_refined 3.8 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 αgust Human - 63 β1 Human γ2 Human Cryo-EM 8XQL - 3.0 T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human - Nanobody-35 Exo-alpha-sialidase aristolochic acid pubchem gtoplig chembl_ligand
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
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 8YW4 8YW4_refined 3.3 GIPR GIP Glucagon B1 (Secretin) Human - Nanobody-35 - Retatrutide
peptide Agonist gastric inhibitory polypeptide 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
Gi/o αo Human - 61 β1 Rat γ2 Human Cryo-EM 9F34 - 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 - 61 β1 Human γ2 Human Cryo-EM 8WJX - 3.2 P2RY1 P2Y1 P2Y A (Rhodopsin) Human BRIL Nanobody-35 - ADP pubchem gtoplig chembl_ligand
small-molecule Agonist ATP, ADP small-molecule - - 2024-10-02
Gi/o αi1 Human - 60 β1 Human γT1 Bovine Cryo-EM 9EPR - 4.9 B1B1U5 Rhodopsin Opsins A (Rhodopsin) Hasarius adansoni - - - Retinal (11-cis) pubchem
small-molecule Agonist - - Tejero O, Pamula F, Koyanagi M, Nagata T, Afanasyev P, Das I, Deupi X, Sheves M, Terakita A, Schertler GFX, Rodrigues MJ, Tsai CJ 10.1038/S41467-024-53208-2 2024-10-30
Gs αs Human - 57 β1 Human γ2 Human Cryo-EM 6GDG 6GDG_refined 4.1 AA2AR A2A Adenosine A (Rhodopsin) Human TrxA Nanobody-35 - NECA pubchem gtoplig chembl_ligand gtoplig
small-molecule Agonist adenosine small-molecule Garcia-Nafria J, Lee Y, Bai X, Carpenter B, Tate CG 10.7554/ELIFE.35946 2018-05-16
Gi/o αi1 Human - 62 β1 Mouse γ2 Human Cryo-EM 6K42 - 4.1 ADA2B α2B Adrenoceptors A (Rhodopsin) Human T4-Lysozyme scFv - dexmedetomidine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist (-)-noradrenaline, (-)-adrenaline small-molecule Yuan D, Liu Z, Kaindl J, Maeda S, Zhao J, Sun X, Xu J, Gmeiner P, Wang HW, Kobilka BK 10.1038/S41589-020-0492-2 2020-04-15
Gs αs Human - 90 β1 Human γ2 Human Cryo-EM 6X18 - 2.1 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - CHEMBL410972 chembl_ligand pubchem pubchem
protein 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 - 62 β1 Human γ2 Human Cryo-EM 7E2X - 3.0 5HT1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human - - - Apo (no ligand)
none Apo (no ligand) 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 - 61 β1 Human γ2 Human Cryo-EM 7F1R - 3.0 CCR5 CCR5 Chemokine A (Rhodopsin) Human - - - CCL5 gtoplig
peptide Agonist CCL11, CCL14, CCL2, CCL8, CCL5, CCL16, CCL4, CCL13, CCL7, CCL3 peptide - - 2021-07-14
Gs αs Human - 48 β1 Rat γ2 Bovine Cryo-EM 7PIU - 2.6 MC4R MC4 Melanocortin A (Rhodopsin) Human - Nanobody-35 - setmelanotide pubchem gtoplig drug_central chembl_ligand drugbank
peptide Agonist γ-MSH, agouti-related protein, β-MSH, α-MSH, ACTH peptide Heyder NA, Kleinau G, Speck D, Schmidt A, Paisdzior S, Szczepek M, Bauer B, Koch A, Gallandi M, Kwiatkowski D, Burger J, Mielke T, Beck-Sickinger AG, Hildebrand PW, Spahn CMT, Hilger D, Schacherl M, Biebermann H, Hilal T, Kuhnen P, Kobilka BK, Scheerer P 10.1038/S41422-021-00569-8 2021-11-17
Gi/o αi1 Human - 40 β1 Human γ2 Human Cryo-EM 7WF7 7WF7_refined 3.4 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 Xu Z, Ikuta T, Kawakami K, Kise R, Qian Y, Xia R, Sun MX, Zhang A, Guo C, Cai XH, Huang Z, Inoue A, He Y 10.1038/S41589-021-00930-3 2022-01-05
Gi/o αi3 Human - 62 β1 Human γ2 Human Cryo-EM 7T10 - 2.5 SSR2 SST2 Somatostatin A (Rhodopsin) Human - scFv16 - SOMATOSTATIN chembl_ligand pubchem
protein Agonist cortistatin-14, SRIF-14, CST-17, SRIF-28 peptide Robertson MJ, Meyerowitz JG, Panova O, Borrelli K, Skiniotis G 10.1038/S41594-022-00727-5 2022-03-09
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7TZF - 2.4 CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP3 		- 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
Gs αs Human - 54 β1 Human γ2 Human Cryo-EM 7EPT - 3.0 AGRD1 ADGRD1 ADGRD B2 (Adhesion) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Ping YQ, Xiao P, Yang F, Zhao RJ, Guo SC, Yan X, Wu X, Zhang C, Lu Y, Zhao F, Zhou F, Xi YT, Yin W, Liu FZ, He DF, Zhang DL, Zhu ZL, Jiang Y, Du L, Feng SQ, Schoneberg T, Liebscher I, Xu HE, Sun JP 10.1038/S41586-022-04619-Y 2022-05-11
Gs αs Human - 57 β1 Human γ2 Human Cryo-EM 7F24 - 4.2 DRD1 D1 Dopamine A (Rhodopsin) Human - - - 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
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7W0L 7W0L_refined 3.6 APJ apelin Apelin A (Rhodopsin) Human BRIL scFv16 - (1R,2S)-N-[4-(2,6-dimethoxyphenyl)-5-(6-methylpyridin-2-yl)-1,2,4-triazol-3-yl]-1-(5-methylpyrimidin-2-yl)-1-oxidanyl-propane-2-sulfonamide pubchem
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 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 - 63 β1 Human γ2 Human Cryo-EM 7XMS - 2.9 SSR4 SST4 Somatostatin A (Rhodopsin) Human - scFv16 - SOMATOSTATIN chembl_ligand pubchem
protein 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 Mini-Gs 56 β1 Human γ2 Human Cryo-EM 7T9N - 2.9 TSHR TSH Glycoprotein hormone A (Rhodopsin) Human - M22 Fab light chain
M22 Fab heavy chain
Nanobody-35 		- M22 antibody light chain
M22 antibody heavy chain
protein
protein 		Agonist TSH peptide Faust B, Billesbolle CB, Suomivuori CM, Singh I, Zhang K, Hoppe N, Pinto AFM, Diedrich JK, Muftuoglu Y, Szkudlinski MW, Saghatelian A, Dror RO, Cheng Y, Manglik A 10.1038/S41586-022-05159-1 2022-08-03
Gs αs Human GTP bound, Class M 62 β1 Human γ2 Human Cryo-EM 8UNX - 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
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8XQS - 3.3 T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human - scFv16 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
Gs αs Human - 57 β1 Human γ2 Human Cryo-EM 8YW5 8YW5_refined 2.8 GLR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - Retatrutide
peptide Agonist glucagon 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 2024-08-07
Gq/11 αq Human - 62 β1 Human γ2 Human Cryo-EM 7YFD - 3.1 HRH4 H4 Histamine A (Rhodopsin) Human - scFv16
Nanobody-35 		- imetit pubchem gtoplig chembl_ligand pubchem
small-molecule Agonist CCL16, histamine small-molecule Im D, Kishikawa JI, Shiimura Y, Hisano H, Ito A, Fujita-Fujiharu Y, Sugita Y, Noda T, Kato T, Asada H, Iwata S 10.1038/S41467-023-42260-Z 2023-10-25
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8HNM - 2.9 CXCR3 CXCR3 Chemokine A (Rhodopsin) Human - scFv16 - CHEMBL2220409 chembl_ligand chembl_ligand pubchem
small-molecule 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
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8IJD - 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 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 - 61 β1 Human γ2 Human Cryo-EM 8JLP - 3.2 TAAR1 TA1 Trace amine A (Rhodopsin) Human - - - ralmitaront pubchem gtoplig chembl_ligand
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
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8GFX - 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
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8J22 8J22_refined 3.2 FFAR2 FFA2 Free fatty acid A (Rhodopsin) Human - scFv16 - CHEMBL4176503 chembl_ligand 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
G12/13 α13 Human - 56 β1 Human γ2 Human Cryo-EM 8KGG - 3.1 P2Y10 P2RY10 A orphans A (Rhodopsin) Human - scFv16 - (2~{S})-2-$l^{4}-azanyl-3-[[(2~{R})-3-octadecanoyloxy-2-oxidanyl-propoxy]-oxidanyl-oxidanylidene-$l^{6}-phosphanyl]oxy-propanoic acid
lipid Agonist LPA, sphingosine 1-phosphate, 1-O-Oleoyl-D-glycerol 3-phosphoric acid, LYSOPHOSPHATIDIC ACID small-molecule Yin H, Kamakura N, Qian Y, Tatsumi M, Ikuta T, Liang J, Xu Z, Xia R, Zhang A, Guo C, Inoue A, He Y 10.1016/J.CHEMBIOL.2024.08.005 2024-07-31
Gq/11 αq Human - 59 β1 Human γ2 Human Cryo-EM 8XOF 8XOF_refined 2.6 GPER1 GPER Estrogen (G protein-coupled) A (Rhodopsin) Human - Nanobody-35 - N1-(7-Chloroquinolin-4-yl)-N2-(2-((7-chloroquinolin-4-yl)amino)ethyl)-N2-methylethane-1,2-diamine pubchem
small-molecule Agonist 17β-estradiol small-molecule - - 2024-04-10
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8XZG 8XZG_refined 3.2 APJ apelin Apelin A (Rhodopsin) Human - - - [Pyr1]apelin-13 gtoplig pubchem
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 2024-03-27
Gi/o αi3 Human - 64 β1 Human γ2 Human Cryo-EM 9AVL - 3.8 CASR CaS Calcium-sensing C (Glutamate) Human - - - Cyclomethyltryptophan pubchem
tecalcet pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Agonist
PAM 		Ca2+, spermine, Mg2+, L-tryptophan small-molecule - - 2024-04-17
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 8YN6 - 2.8 HRH3 H3 Histamine A (Rhodopsin) Human - scFv16 - imetit pubchem gtoplig chembl_ligand pubchem
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
Gs αs Human Engineered G alpha 60 β1 Rat γ2 Bovine Cryo-EM 7LJD - 3.2 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 Zhuang Y, Krumm B, Zhang H, Zhou XE, Wang Y, Huang XP, Liu Y, Cheng X, Jiang Y, Jiang H, Zhang C, Yi W, Roth BL, Zhang Y, Xu HE 10.1038/S41422-021-00482-0 2021-03-03
Gs αs Human - 55 β1 Human γ2 Human Cryo-EM 7BB7 - 4.4 V2R V2 Vasopressin and oxytocin A (Rhodopsin) Human - Nanobody-35 - vasopressin pubchem gtoplig chembl_ligand drugbank drug_central
peptide Agonist oxytocin, vasopressin peptide Bous J, Orcel H, Floquet N, Leyrat C, Lai-Kee-Him J, Gaibelet G, Ancelin A, Saint-Paul J, Trapani S, Louet M, Sounier R, Demene H, Granier S, Bron P, Mouillac B 10.1126/SCIADV.ABG5628 2021-06-02
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7EXD 7EXD_refined 3.4 5HT1F 5-HT1F 5-Hydroxytryptamine A (Rhodopsin) Human BRIL scFv16 - lasmiditan pubchem gtoplig chembl_ligand drug_central drugbank
small-molecule Agonist 5-hydroxytryptamine small-molecule Huang S, Xu P, Tan Y, You C, Zhang Y, Jiang Y, Xu HE 10.1038/S41422-021-00527-4 2021-08-04
Gs αs Human - 55 β1 Human γ2 Human Cryo-EM 7RMH 7RMH_refined 3.1 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 - 62 β1 Human γ2 Human Cryo-EM 7VUG 7VUG_refined 3.2 GP139 GPR139 A orphans A (Rhodopsin) Human - scFv16 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 - 61 β1 Rat γ2 Bovine Cryo-EM 7T6S 7T6S_refined 3.0 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human - scFv16 - N-(4-chlorophenyl)-N'-[1-methyl-3-oxo-2-phenyl-5-(propan-2-yl)-2,3-dihydro-1H-pyrazol-4-yl]urea pubchem
small-molecule 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
Gi/o αi1 Human - 62 β1 Rat γ2 Bovine Cryo-EM 7VGZ 7VGZ_refined 3.3 MTR1A MT1 Melatonin A (Rhodopsin) Human - scFv16 - ramelteon pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist melatonin small-molecule Wang Q, Lu Q, Guo Q, Teng M, Gong Q, Li X, Du Y, Liu Z, Tao Y 10.1038/S41467-022-28111-3 2022-03-02
Gi/o αi2 Human - 63 β1 Human γ2 Human Cryo-EM 7WVW - 3.1 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human BRIL - - FME-TYR-PHE-ILE-ASN-ILE-LEU-THE-LEU
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
Gi/o αi1 Human Mini-Gi1 58 β1 Human γ2 Human Cryo-EM 7WU5 - 3.0 AGRF1 ADGRF1 ADGRF B2 (Adhesion) Human - - - Apo (no ligand)
none Apo (no ligand) - - Qu X, Qiu N, Wang M, Zhang B, Du J, Zhong Z, Xu W, Chu X, Ma L, Yi C, Han S, Shui W, Zhao Q, Wu B 10.1038/S41586-022-04580-W 2022-04-27
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7X9A 7X9A_refined 3.2 NPY1R Y1 Neuropeptide Y A (Rhodopsin) Human - - - neuropeptide Y pubchem gtoplig chembl_ligand gtoplig gtoplig pubchem pubchem pubchem
peptide Agonist peptide YY, pancreatic polypeptide, neuropeptide Y peptide Tang T, Tan Q, Han S, Diemar A, Lobner K, Wang H, Schuss C, Behr V, Morl K, Wang M, Chu X, Yi C, Keller M, Kofoed J, Reedtz-Runge S, Kaiser A, Beck-Sickinger AG, Zhao Q, Wu B 10.1126/SCIADV.ABM1232 2022-05-18
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7XOU - 3.2 CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human - Nanobody-35 - 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 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 7XMR 7XMR_refined 3.1 SSR2 SST2 Somatostatin A (Rhodopsin) Human - - - SOMATOSTATIN chembl_ligand pubchem
protein 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 Mini-Gs 56 β1 Human γ2 Human Cryo-EM 7T9I - 2.9 TSHR TSH Glycoprotein hormone A (Rhodopsin) Human - Nanobody-35 - Glycoprotein hormones alpha chain
Thyrotropin subunit beta
protein
protein 		Agonist TSH peptide Faust B, Billesbolle CB, Suomivuori CM, Singh I, Zhang K, Hoppe N, Pinto AFM, Diedrich JK, Muftuoglu Y, Szkudlinski MW, Saghatelian A, Dror RO, Cheng Y, Manglik A 10.1038/S41586-022-05159-1 2022-08-03
Gi/o αi1 Human - 60 β1 Human γ2 Human Cryo-EM 8HVI 8HVI_refined 3.0 GP132 GPR132 A orphans A (Rhodopsin) Human BRIL scFv16 - NOX-6-7 pubchem gtoplig
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
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8JHY - 2.9 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - scFv16 - compound 9n [PMID: 18752940] pubchem gtoplig chembl_ligand
small-molecule PAM 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
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8K2X 8K2X_refined 3.2 CXCR3 CXCR3 Chemokine A (Rhodopsin) Human BRIL scFv16 - C-X-C motif chemokine 10
small-molecule Agonist CCL11, CXCL10, CXCL12α, CXCL11, CCL5, CCL19, CCL20, CCL13, CXCL9, CCL7 peptide Jiao H, Pang B, Chiang YC, Chen Q, Pan Q, Ren R, Hu H 10.1038/S41421-023-00617-0 2023-11-29
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8WC4 - 3.1 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 8GE1 - 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 - 59 β1 Human γ2 Human Cryo-EM 8GG3 - 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 8JGG 8JGG_refined 3.0 MRGX1 MRGPRX1 A orphans A (Rhodopsin) Human - scFv16 - bovine adrenal medulla peptide 8-22 pubchem gtoplig chembl_ligand pubchem
peptide Agonist bovine adrenal medulla peptide 8-22 peptide Guo L, Zhang Y, Fang G, Tie L, Zhuang Y, Xue C, Liu Q, Zhang M, Zhu K, You C, Xu P, Yuan Q, Zhang C, Liu L, Rong N, Peng S, Liu Y, Wang C, Luo X, Lv Z, Kang D, Yu X, Zhang C, Jiang Y, Dong X, Zhou J, Liu Z, Yang F, Eric Xu H, Sun JP 10.1038/S41467-023-40705-Z 2024-01-10
Gs αs Human - 61 β1 Human γ2 Human Cryo-EM 8SMV 8SMV_refined 2.7 GP161 GPR161 A orphans A (Rhodopsin) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Hoppe N, Harrison S, Hwang SH, Chen Z, Karelina M, Deshpande I, Suomivuori CM, Palicharla VR, Berry SP, Tschaikner P, Regele D, Covey DF, Stefan E, Marks DS, Reiter J, Dror RO, Evers AS, Mukhopadhyay S, Manglik A 10.1101/2023.05.23.540554 2024-02-21
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8WOG - 3.0 SUCR1 succinate Succinate A (Rhodopsin) Human - - - succinic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem
small-molecule Agonist succinic acid small-molecule Liu A, Liu Y, Zhang W, Ye RD 10.1016/J.CELREP.2024.114381 2024-09-11
Gq/11 αq Human - 58 β1 Human γ2 Human Cryo-EM 8XJL 8XJL_refined 2.8 PF2R FP Prostanoid A (Rhodopsin) Human - scFv16 - PGF2α pubchem gtoplig chembl_ligand drug_central drugbank
small-molecule Agonist PGF2α, PGI2, PGD2, thromboxane A2, PGE2 small-molecule Li X, Zhang X, Wen X, Zhang D, Qu C, Miao X, Zhang W, Zhang R, Liu G, Xiao P, Sun JP, Gong W 10.1016/J.CELREP.2024.113893 2024-02-28
Gi/o αi1 Human - 60 β1 Rat γ2 Bovine Cryo-EM 8YKV - 2.5 SUCR1 succinate Succinate A (Rhodopsin) Human - scFv16 - Sucnr1-IN-2 pubchem
small-molecule Agonist succinic acid small-molecule - - 2024-05-29
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 8ZRK - 2.8 GP119 GPR119 GPR18, GPR55 and GPR119 A (Rhodopsin) Human - Nanobody-35 - GSK-1292263 chembl_ligand pubchem
small-molecule Agonist N-palmitoylethanolamine, anandamide, N-oleoylethanolamide, SEA small-molecule - - 2024-06-19
Gi/o αi1 Human - 65 β1 Human γ2 Human Cryo-EM 8K4O - 3.0 Q76SF8 ORF74 Unclassified A (Rhodopsin) HHV-8 - - - Growth-regulated alpha protein
protein Agonist - - - - 2024-07-24
Gs αs Human Mini-Gs 59 β1 Human γ2 Human Cryo-EM 9GYO - 2.5 GPBAR GPBA Bile acid A (Rhodopsin) Human BRIL Nanobody-35 - CHEMBL2331646 chembl_ligand pubchem
small-molecule Agonist cholic acid, deoxycholic acid, chenodeoxycholic acid, lithocholic acid small-molecule - - 2024-10-09
Gi/o αo Human - 59 β1 Rat γ2 Mouse Cryo-EM 6WWZ 6WWZ_refined 3.3 CCR6 CCR6 Chemokine A (Rhodopsin) Human - scFv16 - CCL20 gtoplig
peptide Agonist CCL20, beta-defensin 4A peptide Wasilko DJ, Johnson ZL, Ammirati M, Che Y, Griffor MC, Han S, Wu H 10.1038/S41467-020-16820-6 2020-06-24
Gs αs Bovine - 57 β1 Bovine γ2 Bovine Cryo-EM 7D68 - 3.0 GLP2R GLP-2 Glucagon B1 (Secretin) Human - Nanobody-35 - glucagon pubchem gtoplig chembl_ligand drugbank drug_central gtoplig pubchem pubchem pubchem pubchem
peptide Agonist glucagon-like peptide 2-(3-33), glucagon-like peptide 2 peptide Sun W, Chen LN, Zhou Q, Zhao LH, Yang D, Zhang H, Cong Z, Shen DD, Zhao F, Zhou F, Cai X, Chen Y, Zhou Y, Gadgaard S, van der Velden WJC, Zhao S, Jiang Y, Rosenkilde MM, Xu HE, Zhang Y, Wang MW 10.1038/S41422-020-00442-0 2020-12-16
Gs αs Human - 60 β1 Rat γ2 Bovine Cryo-EM 7DW9 - 2.6 V2R V2 Vasopressin and oxytocin A (Rhodopsin) Human - Nanobody-35
scFv16 		- vasopressin pubchem gtoplig chembl_ligand drugbank drug_central
peptide Agonist oxytocin, vasopressin peptide Zhou F, Ye C, Ma X, Yin W, Croll TI, Zhou Q, He X, Zhang X, Yang D, Wang P, Xu HE, Wang MW, Jiang Y 10.1038/S41422-021-00480-2 2021-07-21
Gq/11 αq Human Gq-Gs chimera 57 β1 Human γ2 Human Cryo-EM 7S8L - 2.5 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human - scFv16 - Cortistatin 14 pubchem
peptide Agonist PAMP-20 peptide - - 2021-11-17
Gq/11 αq Human Gq-Gs-Gi1 chimera 59 β1 Human γ2 Human Cryo-EM 7P00 - 2.7 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 - 61 β1 Rat γ2 Bovine Cryo-EM 7T6T 7T6T_refined 3.2 FPR1 FPR1 Formylpeptide A (Rhodopsin) Human - - - synthetic peptide
peptide Agonist annexin I, fMet-Leu-Phe, cathepsin G, spinorphin 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
Gi/o αi1 Mouse - 63 β1 Bovine γ2 Bovine Cryo-EM 7TD4 - 2.6 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - - - siponimod pubchem gtoplig chembl_ligand drug_central drugbank
small-molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine 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
Gs αs Human Mini-Gs 58 β1 Rat γ2 Bovine Cryo-EM 7VBI - 3.0 GLP1R GLP-1 Glucagon B1 (Secretin) Human - - - 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
Gs αs Human Mini-Gs 59 β1 Human γ2 Human Cryo-EM 7WUJ - 3.3 AGRG4 ADGRG4 ADGRG B2 (Adhesion) Human - scFv16
Nanobody-35 		- Apo (no ligand)
none Apo (no ligand) - - Xiao P, Guo S, Wen X, He QT, Lin H, Huang SM, Gou L, Zhang C, Yang Z, Zhong YN, Yang CC, Li Y, Gong Z, Tao XN, Yang ZS, Lu Y, Li SL, He JY, Wang C, Zhang L, Kong L, Sun JP, Yu X 10.1038/S41586-022-04590-8 2022-04-27
Gi/o αi1 Human - 64 β1 Rat γ2 Bovine Cryo-EM 7WIG 7WIG_refined 2.7 SSR2 SST2 Somatostatin A (Rhodopsin) Human - scFv16 - ~{N}-[(2~{R})-1-[[(1~{R},3~{S})-3-(aminomethyl)cyclohexyl]methylamino]-3-(1~{H}-indol-3-yl)-1-oxidanylidene-propan-2-yl]spiro[indene-1,4'-piperidine]-1'-carboxamide pubchem
small-molecule Agonist cortistatin-14, SRIF-14, CST-17, SRIF-28 peptide Chen LN, Wang WW, Dong YJ, Shen DD, Guo J, Yu X, Qin J, Ji SY, Zhang H, Shen Q, He Q, Yang B, Zhang Y, Li Q, Mao C 10.1038/S41422-022-00669-Z 2022-06-01
Gi/o αi2 Human - 63 β1 Human γ2 Human Cryo-EM 7WV9 - 3.4 CNR1 CB1 Cannabinoid A (Rhodopsin) Human - scFv16 - CP55940 pubchem gtoplig chembl_ligand gtoplig
6-methyl-3-[(1S)-2-nitro-1-thiophen-2-yl-ethyl]-2-phenyl-1H-indole pubchem
small-molecule
small-molecule 		Agonist
PAM 		anandamide small-molecule Yang X, Wang X, Xu Z, Wu C, Zhou Y, Wang Y, Lin G, Li K, Wu M, Xia A, Liu J, Cheng L, Zou J, Yan W, Shao Z, Yang S 10.1038/S41589-022-01038-Y 2022-06-15
Gi/o αi1 Human - 63 β1 Bovine γ2 Bovine Cryo-EM 7XAU - 3.0 SSR2 SST2 Somatostatin A (Rhodopsin) Human - scFv16 - Octreotide
peptide Agonist cortistatin-14, SRIF-14, CST-17, SRIF-28 peptide Bo Q, Yang F, Li Y, Meng X, Zhang H, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C 10.1038/S41421-022-00405-2 2022-08-31
Gs αs Human - 58 β1 Rat γ2 Bovine Cryo-EM 7VVO 7VVO_refined 4.1 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - Parathyroid hormone
peptide Agonist PTHrP-(1-36), PTHrP, PTH, TIP39 peptide Kobayashi K, Kawakami K, Kusakizako T, Miyauchi H, Tomita A, Kobayashi K, Shihoya W, Yamashita K, Nishizawa T, Kato HE, Inoue A, Nureki O 10.1016/J.MOLCEL.2022.07.003 2022-08-03
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7VIF 7VIF_refined 2.8 S1PR1 S1P1 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 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
Gq/11 αq Human Mini-Gq 60 β1 Human γ2 Human Cryo-EM 7Y26 7Y26_refined 3.3 SSR2 SST2 Somatostatin A (Rhodopsin) Human - scFv16 - Octreotide pubchem
peptide Agonist cortistatin-14, SRIF-14, CST-17, SRIF-28 peptide Chen S, Teng X, Zheng S 10.1038/S41589-022-01130-3 2022-10-19
Gi/o αi1 Human - 64 β1 Rat γ2 Bovine Cryo-EM 8EF6 8EF6_refined 3.2 OPRM μ Opioid A (Rhodopsin) Human - scFv16 - morphine 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
Gi/o αo Human Mini-Go 60 β1 Human γ2 Human Cryo-EM 8FN0 - 2.9 NTR1 NTS1 Neurotensin A (Rhodopsin) Rat - scFv16 - neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
CHEMBL4576388 chembl_ligand pubchem
peptide
small-molecule 		Agonist
PAM 		neuromedin N, neurotensin peptide Krumm BE, DiBerto JF, Olsen RHJ, Kang HJ, Slocum ST, Zhang S, Strachan RT, Huang XP, Slosky LM, Pinkerton AB, Barak LS, Caron MG, Kenakin T, Fay JF, Roth BL 10.1021/ACS.BIOCHEM.3C00029 2023-03-29
Gi/o αi1 Human - 56 β1 Human γ2 Human Cryo-EM 8ID9 8ID9_refined 3.0 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - scFv16 - EPA pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist oleic acid, myristic acid, α-linolenic acid, linoleic acid small-molecule Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP 10.1126/SCIENCE.ADD6220 2023-03-15
Gi/o αi1 Human - 60 β1 Human γ2 Human Cryo-EM 8DZP - 2.7 OPRK κ Opioid A (Rhodopsin) Human - scFv16 - SALVINORIN B METHOXYMETHYL ETHER chembl_ligand pubchem
small-molecule 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 Han J, Zhang J, Nazarova AL, Bernhard SM, Krumm BE, Zhao L, Lam JH, Rangari VA, Majumdar S, Nichols DE, Katritch V, Yuan P, Fay JF, Che T 10.1038/S41586-023-06030-7 2023-05-03
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 8IRV 8IRV_refined 3.1 DRD5 D5 Dopamine A (Rhodopsin) Human BRIL - - rotigotine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist L-NOREPINEPHRINE, noradrenaline, (-)-noradrenaline, 5-hydroxytryptamine, 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
Gq/11 αq Human Mini-Gq 51 - - - - Cryo-EM 7YMH 7YMH_refined 3.5 ADA1A α1A Adrenoceptors A (Rhodopsin) Human - Nanobody-29 - Noradrenaline pubchem
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
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 8H4L - 3.1 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - Nanobody-35 - docosahexaenoic acid pubchem gtoplig chembl_ligand drug_central drugbank pubchem
small-molecule Agonist oleic acid, myristic acid, α-linolenic acid, linoleic acid small-molecule Yin H, Inoue A, Ma Z, Zhu X, Xia R, Xu Z, Wang N, Duan Y, Zhang A, Guo C, He Y 10.1038/S41422-023-00835-X 2023-06-21
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8GCP 8GCP_refined 3.1 PE2R4 EP4 Prostanoid A (Rhodopsin) Human - scFv16 - 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 2024-01-03
Gi/o αo Human - 59 β1 Human γ2 Human Cryo-EM 8I95 - 2.9 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 - 63 β1 Human γ2 Human Cryo-EM 8JIL - 3.5 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 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
Gi/o αo Human - 59 β1 Human γ2 Human Cryo-EM 8JZZ 8JZZ_refined 3.3 C5AR1 C5a1 Complement peptide A (Rhodopsin) Human - scFv16 - C5a des-Arg 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 - 56 β1 Human γ2 Human Cryo-EM 8WC8 - 2.9 TAAR1 TA1 Trace amine A (Rhodopsin) Human - scFv16 - CHEMBL476516 chembl_ligand pubchem
small-molecule Agonist octopamine, β-phenylethylamine, CHEMBL1160703, tyramine, (+)-Octopamine, 3-iodothyronamine, dopamine 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 8GEB 8GEB_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 - 91 β1 Human γ2 Human Cryo-EM 8GGF 8GGF_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
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8JGB 8JGB_refined 2.8 MRGX1 MRGPRX1 A orphans A (Rhodopsin) Human - scFv16 - Conorfamide-Tx2
protein Agonist bovine adrenal medulla peptide 8-22 peptide - - 2024-01-10
Gi/o αi3 Rhesus macaque - 63 β1 Human γ2 Human Cryo-EM 8K9L - 3.1 OPRM μ Opioid A (Rhodopsin) Human BRIL scFv16 - DAMGO pubchem gtoplig chembl_ligand chembl_ligand
(2~{S})-2-(3-bromanyl-4-methoxy-phenyl)-3-(4-chlorophenyl)sulfonyl-1,3-thiazolidine pubchem
peptide
small-molecule 		Agonist
PAM 		endomorphin-1, β-endorphin, dynorphin A, dynorphin A-(1-8), [Leu]enkephalin, dynorphin A-(1-13), dynorphin B, [Met]enkephalin, endomorphin-2 peptide Kaneko S, Imai S, Uchikubo-Kamo T, Hisano T, Asao N, Shirouzu M, Shimada I 10.1038/S41467-024-47792-6 2024-05-29
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8U8F 8U8F_refined 3.5 GPR3 GPR3 A orphans A (Rhodopsin) Human - - - palmitic acid pubchem gtoplig chembl_ligand drugbank pubchem
small-molecule Agonist sphingosine 1-phosphate small-molecule Russell IC, Zhang X, Bumbak F, McNeill SM, Josephs TM, Leeming MG, Christopoulos G, Venugopal H, Flocco MM, Sexton PM, Wootten D, Belousoff MJ 10.1021/ACS.BIOCHEM.3C00647 2024-03-06
Gs αs Human GTP bound, Class J 57 β1 Human γ2 Human Cryo-EM 8UNU - 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
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8WSS 8WSS_refined 3.0 MCHR1 MCH1 Melanin-concentrating hormone A (Rhodopsin) Human - scFv16 - 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 αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8XQO - 2.8 T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human - scFv16 Exo-alpha-sialidase aristolochic acid pubchem gtoplig chembl_ligand
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
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 8ZFJ - 3.1 E7FEL0 GPR4 A orphans A (Rhodopsin) Zebrafish BRIL scFv16 LgBiT Apo (no ligand)
none Apo (no ligand) - - - - 2024-08-07
Gs αs Human - 57 β1 Human γ2 Human Cryo-EM 9AVG - 3.6 CASR CaS Calcium-sensing C (Glutamate) Human - - - Cyclomethyltryptophan pubchem
tecalcet pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Agonist
PAM 		Ca2+, spermine, Mg2+, L-tryptophan small-molecule - - 2024-04-17
Gi/o αo Human Mini-Go 61 β1 Human γ2 Human Cryo-EM 8YN8 - 2.8 HRH3 H3 Histamine A (Rhodopsin) Human - scFv16 - proxyfan pubchem gtoplig chembl_ligand
small-molecule Agonist histamine small-molecule - - 2024-10-16
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 6OS9 6OS9_refined 3.0 NTR1 NTS1 Neurotensin A (Rhodopsin) Human - scFv16 - JMV449 pubchem gtoplig chembl_ligand
peptide Agonist large neuromedin N, neuromedin N, neurotensin, large neurotensin peptide Kato HE, Zhang Y, Hu H, Suomivuori CM, Kadji FMN, Aoki J, Krishna Kumar K, Fonseca R, Hilger D, Huang W, Latorraca NR, Inoue A, Dror RO, Kobilka BK, Skiniotis G 10.1038/S41586-019-1337-6 2019-07-10
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 6PB1 6PB1_refined 2.8 CRFR2 CRF2 Corticotropin-releasing factor B1 (Secretin) Human - Nanobody-35 - Urocortin pubchem
peptide Agonist corticotrophin-releasing hormone, urocortin 1, urocortin 3, urocortin 2 peptide Ma S, Shen Q, Zhao LH, Mao C, Zhou XE, Shen DD, de Waal PW, Bi P, Li C, Jiang Y, Wang MW, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE 10.1016/J.MOLCEL.2020.01.013 2020-02-12
Gs αs Human - 89 β1 Human γ2 Human Cryo-EM 6X19 - 2.1 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - CHU-128 pubchem
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
Gs αs Human Engineered G alpha 58 β1 Human γ2 Human Cryo-EM 7L1U - 3.2 OX2R OX2 Orexin A (Rhodopsin) Human - scFv16 - Orexin-A pubchem
peptide Agonist orexin-B, orexin-A peptide Hong C, Byrne NJ, Zamlynny B, Tummala S, Xiao L, Shipman JM, Partridge AT, Minnick C, Breslin MJ, Rudd MT, Stachel SJ, Rada VL, Kern JC, Armacost KA, Hollingsworth SA, O'Brien JA, Hall DL, McDonald TP, Strickland C, Brooun A, Soisson SM, Hollenstein K 10.1038/S41467-021-21087-6 2021-02-10
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7CX3 - 2.8 PE2R2 EP2 Prostanoid A (Rhodopsin) Human - Nanobody-35 - taprenepag pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist PGF2α, PGI2, PGD2, thromboxane A2, PGE1, PGE2 small-molecule Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y 10.1126/SCIADV.ABF1268 2021-05-05
Gq/11 αq Human - 63 β1 Human γ2 Human Cryo-EM 7EZM - 2.9 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 - 58 β1 Human γ2 Human Cryo-EM 7F55 - 3.1 MC4R MC4 Melanocortin A (Rhodopsin) Human - Nanobody-35 - bremelanotide pubchem gtoplig chembl_ligand drugbank drug_central
peptide Agonist γ-MSH, agouti-related protein, β-MSH, α-MSH, ACTH peptide Zhang H, Chen LN, Yang D, Mao C, Shen Q, Feng W, Shen DD, Dai A, Xie S, Zhou Y, Qin J, Sun JP, Scharf DH, Hou T, Zhou T, Wang MW, Zhang Y 10.1038/S41422-021-00552-3 2021-11-03
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7EVZ - 3.1 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - cenerimod pubchem gtoplig chembl_ligand 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
Gi/o αi1 Human - 64 β1 Rat γ2 Bovine Cryo-EM 7WQ3 7WQ3_refined 2.7 GALR1 GAL1 Galanin A (Rhodopsin) Human - scFv16 - galanin pubchem gtoplig chembl_ligand gtoplig pubchem pubchem pubchem pubchem
peptide Agonist galanin-like peptide, galanin peptide Duan J, Shen DD, Zhao T, Guo S, He X, Yin W, Xu P, Ji Y, Chen LN, Liu J, Zhang H, Liu Q, Shi Y, Cheng X, Jiang H, Eric Xu H, Zhang Y, Xie X, Jiang Y 10.1038/S41467-022-29072-3 2022-04-20
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7EUO 7EUO_refined 2.9 FPR1 FPR1 Formylpeptide A (Rhodopsin) Human - scFv16 - Peptide Agonist fMLF
peptide Agonist annexin I, fMet-Leu-Phe, cathepsin G, spinorphin peptide Chen G, Wang X, Liao Q, Ge Y, Jiao H, Chen Q, Liu Y, Lyu W, Zhu L, van Zundert GCP, Robertson MJ, Skiniotis G, Du Y, Hu H, Ye RD 10.1038/S41467-022-32822-Y 2022-05-25
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7XTB 7XTB_refined 3.3 5HT6R 5-HT6 5-Hydroxytryptamine A (Rhodopsin) Human BRIL Nanobody-35 - 5-hydroxytryptamine pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist 5-hydroxytryptamine small-molecule Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE 10.1016/J.MOLCEL.2022.05.031 2022-07-27
Gi/o αi1 Human - 62 β1 Mouse γ2 Mouse Cryo-EM 7Y15 7Y15_refined 2.9 MRGRD MRGPRD A orphans A (Rhodopsin) Human BRIL scFv16 - Apo (no ligand)
none Apo (no ligand) β-alanine small-molecule Suzuki S, Iida M, Hiroaki Y, Tanaka K, Kawamoto A, Kato T, Oshima A 10.1038/S42003-022-03668-3 2022-07-20
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7VFX 7VFX_refined 2.8 FPR1 FPR1 Formylpeptide A (Rhodopsin) Human - scFv16 - Peptide agonist fMet-Ile-Phe-Leu pubchem
peptide Agonist annexin I, fMet-Leu-Phe, cathepsin G, spinorphin peptide Chen G, Wang X, Liao Q, Ge Y, Jiao H, Chen Q, Liu Y, Lyu W, Zhu L, van Zundert GCP, Robertson MJ, Skiniotis G, Du Y, Hu H, Ye RD 10.1038/S41467-022-32822-Y 2022-09-21
Gi/o αo Human - 60 β1 Human γ2 Human Cryo-EM 7Y24 - 3.3 SSR2 SST2 Somatostatin A (Rhodopsin) Human - scFv16 - Octreotide pubchem
peptide Agonist cortistatin-14, SRIF-14, CST-17, SRIF-28 peptide Chen S, Teng X, Zheng S 10.1038/S41589-022-01130-3 2022-10-19
Gi/o αi1 Human - 64 β1 Rat γ2 Bovine Cryo-EM 8EFB 8EFB_refined 3.2 OPRM μ Opioid A (Rhodopsin) Human - scFv16 - OLICERIDINE chembl_ligand pubchem
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
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 7Y66 - 2.9 C5AR1 C5a1 Complement peptide A (Rhodopsin) Human - scFv16 - BM213
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
Gs αs Human fused Gs 58 β1 Human γ2 Human Cryo-EM 8I2G - 2.8 FSHR FSH Glycoprotein hormone A (Rhodopsin) Human - Nanobody-35 - Glycoprotein alpha
Follitropin subunit beta
FSHR agonist 1 pubchem
peptide
peptide
small-molecule 		Agonist FSH peptide Duan J, Xu P, Zhang H, Luan X, Yang J, He X, Mao C, Shen DD, Ji Y, Cheng X, Jiang H, Jiang Y, Zhang S, Zhang Y, Xu HE 10.1038/S41467-023-36170-3 2023-03-29
Gi/o αi1 Human - 60 β1 Human γ2 Human Cryo-EM 8U1U - 3.1 CCR8 CCR8 Chemokine A (Rhodopsin) Human - scFv16 - CCL1
protein Agonist CCL8, CCL1 peptide - - 2023-12-20
Gs αs Human - 78 β1 Human γ2 Human Cryo-EM 8GEG 8GEG_refined 3.8 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 - 63 β1 Human γ2 Human Cryo-EM 8IZ4 - 2.9 GPR34 GPR34 A orphans A (Rhodopsin) Human - scFv16 - Lysergide pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist lysophosphatidylserine small-molecule - - 2024-04-10
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8KFX 8KFX_refined 3.0 CCR8 CCR8 Chemokine A (Rhodopsin) Human - scFv16 - CHEMBL5268017 chembl_ligand pubchem
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
Gq/11 αq Human - 58 β1 Human γ2 Human Cryo-EM 8XJK 8XJK_refined 2.6 PF2R FP Prostanoid A (Rhodopsin) Human - scFv16 - cloprostenol pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist PGF2α, PGI2, PGD2, thromboxane A2, PGE2 small-molecule - - 2024-02-28
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8YUT - 2.7 HRH2 H2 Histamine A (Rhodopsin) Human - Nanobody-35 - amthamine pubchem gtoplig chembl_ligand
small-molecule Agonist histamine small-molecule - - 2024-06-05
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 9ASB - 3.4 CASR CaS Calcium-sensing C (Glutamate) Human - - - Cyclomethyltryptophan pubchem
tecalcet pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Agonist
PAM 		Ca2+, spermine, Mg2+, L-tryptophan small-molecule - - 2024-04-17
Gi/o αo Human Mini-Go 61 β1 Human γ2 Human Cryo-EM 8YN7 - 2.8 HRH3 H3 Histamine A (Rhodopsin) Human - scFv16 - [(2R)-3-[(E)-hexadec-9-enoyl]oxy-2-octadecanoyloxypropyl] 2-(trimethylazaniumyl)ethyl phosphate pubchem
lipid Agonist histamine small-molecule - - 2024-10-16
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 6N4B 6N4B_refined 3.0 CNR1 CB1 Cannabinoid A (Rhodopsin) Human - scFv16 - MDMB-Fubinaca pubchem gtoplig
small-molecule Agonist anandamide small-molecule Krishna Kumar K, Shalev-Benami M, Robertson MJ, Hu H, Banister SD, Hollingsworth SA, Latorraca NR, Kato HE, Hilger D, Maeda S, Weis WI, Farrens DL, Dror RO, Malhotra SV, Kobilka BK, Skiniotis G 10.1016/J.CELL.2018.11.040 2019-01-30
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 6OMM 6OMM_refined 3.2 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human - - - CHEMBL552527 chembl_ligand pubchem
protein 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, Liu H, Edward Zhou X, Kumar Verma R, de Waal PW, Jang W, Xu TH, Wang L, Meng X, Zhao G, Kang Y, Melcher K, Fan H, Lambert NA, Eric Xu H, Zhang C 10.1038/S41467-020-14728-9 2020-02-26
Gs αs Human - 61 β1 Human γ2 Human Cryo-EM 6VN7 6VN7_refined 3.2 VIPR1 VPAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - [Ac-His1]PACAP-27 gtoplig chembl_ligand pubchem
peptide Agonist PHM, GHRH, VIP, PACAP-27, PHI, secretin, PACAP-38 peptide Duan J, Shen DD, Zhou XE, Bi P, Liu QF, Tan YX, Zhuang YW, Zhang HB, Xu PY, Huang SJ, Ma SS, He XH, Melcher K, Zhang Y, Xu HE, Jiang Y 10.1038/S41467-020-17933-8 2020-09-02
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7CRH 7CRH_refined 3.3 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - CHEMBL1416789 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
Gi/o αi1 Human - 61 β1 Rat γ2 Bovine Cryo-EM 7T6V 7T6V_refined 3.1 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human - scFv16 - 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
Gi/o αi1 Human - 61 β1 Rat γ2 Human Cryo-EM 7VH0 7VH0_refined 3.5 MTR1B MT2 Melatonin A (Rhodopsin) Human - scFv16 - ramelteon pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist melatonin small-molecule Wang Q, Lu Q, Guo Q, Teng M, Gong Q, Li X, Du Y, Liu Z, Tao Y 10.1038/S41467-022-28111-3 2022-03-02
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7WVU 7WVU_refined 3.3 FPR1 FPR1 Formylpeptide A (Rhodopsin) Human - - - FME-LEU-PHE
peptide Agonist annexin I, fMet-Leu-Phe, cathepsin G, spinorphin 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
Gi/o αi1 Human Mini-Gi1 58 β1 Human γ2 Human Cryo-EM 7WU4 - 3.4 AGRF1 ADGRF1 ADGRF B2 (Adhesion) Human - - - Apo (no ligand)
none Apo (no ligand) - - Qu X, Qiu N, Wang M, Zhang B, Du J, Zhong Z, Xu W, Chu X, Ma L, Yi C, Han S, Shui W, Zhao Q, Wu B 10.1038/S41586-022-04580-W 2022-04-27
Gq/11 αq Human - 63 β1 Human γ2 Human Cryo-EM 7F6I 7F6I_refined 2.8 BKRB2 B2 Bradykinin A (Rhodopsin) Human - - - kallidin pubchem gtoplig
peptide Agonist [des-Arg9]bradykinin, kallidin, Lys-[Hyp3]-bradykinin, [des-Arg10]kallidin, T-kinin, [Hyp3]bradykinin, bradykinin peptide Shen J, Zhang D, Fu Y, Chen A, Yang X, Zhang H 10.1038/S41467-022-28399-1 2022-01-05
Gi/o αo Human Mini-Go 60 β1 Human γ2 Human Cryo-EM 7UM6 - 2.8 5HT5A 5-HT5A 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - lisuride pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist 5-hydroxytryptamine small-molecule Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL 10.1038/S41594-022-00796-6 2022-07-20
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7XTQ 7XTQ_refined 3.2 GPBAR GPBA Bile acid A (Rhodopsin) Human - Nanobody-35 - CHEMBL2181246 chembl_ligand pubchem
small-molecule Agonist cholic acid, deoxycholic acid, chenodeoxycholic acid, lithocholic acid small-molecule Ma L, Yang F, Wu X, Mao C, Guo L, Miao T, Zang SK, Jiang X, Shen DD, Wei T, Zhou H, Wei Q, Li S, Shu Q, Feng S, Jiang C, Chu B, Du L, Sun JP, Yu X, Zhang Y, Zhang P 10.1073/PNAS.2117054119 2022-07-06
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7X9Y 7X9Y_refined 3.1 CCR3 CCR3 Chemokine A (Rhodopsin) Human - scFv16 - Apo (no ligand)
none Apo (no ligand) CCL11, CXCL10, CCL28, CCL15, CCL2, CCL8, CXCL11, CCL5, CCL24, CCL13, CXCL9, 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 - 71 β1 Human γ2 Human Cryo-EM 8GED 8GED_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
Gs αs Human - 51 β1 Human γ2 Human Cryo-EM 8IQ6 8IQ6_refined 3.4 PF2R FP Prostanoid A (Rhodopsin) Human - Nanobody-35 - latanoprost (free acid form) pubchem gtoplig chembl_ligand
small-molecule Agonist PGF2α, PGI2, PGD2, thromboxane A2, PGE2 small-molecule Lv X, Gao K, Nie J, Zhang X, Zhang S, Ren Y, Sun X, Li Q, Huang J, Liu L, Zhang X, Zhang W, Liu X 10.1038/S41467-023-43922-8 2024-01-31
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8WG8 8WG8_refined 2.7 GLR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) glucagon 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 8XIR - 2.5 SSR3 SST3 Somatostatin A (Rhodopsin) Human - Nanobody-35 - 004-DTR-LYS-TY5-PHE-A1D5E
peptide Agonist cortistatin-14, SRIF-14, CST-17, SRIF-28 peptide - - 2024-07-03
Gq/11 αq Human Gs-min-Gq chimera 57 β1 Human γ2 Human Cryo-EM 8YRG 8YRG_refined 3.1 MRGX4 MRGPRX4 A orphans A (Rhodopsin) Human BRIL scFv16 - Fospropofol pubchem
small-molecule Agonist - - - - 2024-05-22
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8ZQE 8ZQE_refined 2.9 GPR15 GPR15 A orphans A (Rhodopsin) Human - scFv16 - GPR15LG
peptide Agonist - - Zhang Z, Zheng Y, Xu L, Yue Y, Xu K, Li F, Xu F 10.1038/S41421-024-00698-5 2024-07-10
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8IKH 8IKH_refined 3.3 CNR1 CB1 Cannabinoid A (Rhodopsin) Human - scFv16 - 3-[(1R)-1-(2-methoxyphenyl)-2-nitro-ethyl]-2-phenyl-1H-indole pubchem
small-molecule Agonist anandamide small-molecule Shen S, Wu C, Lin G, Yang X, Zhou Y, Zhao C, Miao Z, Tian X, Wang K, Yang Z, Liu Z, Guo N, Li Y, Xia A, Zhou P, Liu J, Yan W, Ke B, Yang S, Shao Z 10.1073/PNAS.2321532121 2024-06-05
Gi/o αi1 Human - 60 β1 Human γ2 Human Cryo-EM 8XGU - 3.0 KISSR kisspeptin Kisspeptin A (Rhodopsin) Human - scFv16 - TAK448
peptide Agonist kisspeptin-10, kisspeptin-54, kisspeptin-52, kisspeptin-14, kisspeptin-13 peptide Wu Z, Chen G, Qiu C, Yan X, Xu L, Jiang S, Xu J, Han R, Shi T, Liu Y, Gao W, Wang Q, Li J, Ye F, Pan X, Zhang Z, Ning P, Zhang B, Chen J, Du Y 10.1126/SCIADV.ADN7771 2024-10-30
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7CKW 7CKW_refined 3.2 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - fenoldopam pubchem gtoplig chembl_ligand drugbank drug_central pubchem gtoplig chembl_ligand pubchem pubchem gtoplig 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
Gi/o αi1 Human - 58 β1 Human γ2 Human Cryo-EM 7MTS - 3.2 GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human - - - 2-methoxy-6-propyl-N-(2-{4-[(1H-tetrazol-5-yl)methoxy]phenyl}ethyl)thieno[2,3-d]pyrimidin-4-amine pubchem
L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem
small-molecule
small-molecule 		Ago-PAM
Agonist 		L-glutamic acid small-molecule Seven AB, Barros-Alvarez X, de Lapeyriere M, Papasergi-Scott MM, Robertson MJ, Zhang C, Nwokonko RM, Gao Y, Meyerowitz JG, Rocher JP, Schelshorn D, Kobilka BK, Mathiesen JM, Skiniotis G 10.1038/S41586-021-03680-3 2021-07-07
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7VUY - 2.8 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
Gi/o αo Human - 60 β1 Human γ2 Human Cryo-EM 7W2Z 7W2Z_refined 2.8 GHSR ghrelin Ghrelin A (Rhodopsin) Human - scFv16 - Ghrelin pubchem
peptide Agonist [des-Gln14]ghrelin, ghrelin peptide Qin J, Cai Y, Xu Z, Ming Q, Ji SY, Wu C, Zhang H, Mao C, Shen DD, Hirata K, Ma Y, Yan W, Zhang Y, Shao Z 10.1038/S41467-022-27975-9 2022-01-19
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7VL9 - 2.6 CCR1 CCR1 Chemokine A (Rhodopsin) Human - scFv16 - CCL15(26-92)
peptide Agonist CCL14, CCL15, CCL8, CCL5, CCL16, CCL4, CCL23, CCL13, CCL7, CCL3 peptide Shao Z, Shen Q, Yao B, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Ma H, Chen ZH, Xu HE, Ying S, Zhang Y, Shen H 10.1038/S41589-021-00918-Z 2022-03-23
Gs αs Human Engineered G alpha 55 β1 Human γ2 Human Cryo-EM 7RGP - 2.9 GLP1R GLP-1 Glucagon B1 (Secretin) Human - scFv16
Nanobody-35 		- tirzepatide pubchem gtoplig
peptide Agonist glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide 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 7X2D 7X2D_refined 3.3 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - tavapadon pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist 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
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7XOV - 3.0 CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human - Nanobody-35 - SR146131 pubchem gtoplig chembl_ligand
small-molecule Agonist CCK-8, desulfated cholecystokinin-8, CCK-39, CCK-58, CCK-33, CCK-4, 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 Bovine γ2 Bovine Cryo-EM 7XAT 7XAT_refined 2.9 SSR2 SST2 Somatostatin A (Rhodopsin) Human - scFv16 - SOMATOSTATIN chembl_ligand pubchem
protein Agonist cortistatin-14, SRIF-14, CST-17, SRIF-28 peptide Bo Q, Yang F, Li Y, Meng X, Zhang H, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C 10.1038/S41421-022-00405-2 2022-08-31
Gs αs Human - 58 β1 Rat γ2 Bovine Cryo-EM 7VVN 7VVN_refined 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 Kobayashi K, Kawakami K, Kusakizako T, Miyauchi H, Tomita A, Kobayashi K, Shihoya W, Yamashita K, Nishizawa T, Kato HE, Inoue A, Nureki O 10.1016/J.MOLCEL.2022.07.003 2022-08-03
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7T2H - 3.2 OPRM μ Opioid A (Rhodopsin) Mouse - scFv16 - LOFENTANIL chembl_ligand pubchem
small-molecule Agonist - - Qu Q, Huang W, Aydin D, Paggi JM, Seven AB, Wang H, Chakraborty S, Che T, DiBerto JF, Robertson MJ, Inoue A, Suomivuori CM, Roth BL, Majumdar S, Dror RO, Kobilka BK, Skiniotis G 10.1038/S41589-022-01208-Y 2022-12-07
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7X2V - 3.1 AGRF1 ADGRF1 ADGRF B2 (Adhesion) Human - scFv16 - 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 - 64 β1 Rat γ2 Bovine Cryo-EM 8EFO - 2.8 OPRM μ Opioid A (Rhodopsin) Human - scFv16 - PZM21 pubchem gtoplig chembl_ligand drugbank
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
Gi/o αi2 Human - 59 β1 Human γ2 Bovine Cryo-EM 7YK6 7YK6_refined 3.0 RL3R2 RXFP4 Relaxin family peptide A (Rhodopsin) Human - scFv16 - CHEMBL4522365 chembl_ligand pubchem
small-molecule Agonist relaxin-3, relaxin-3 (B chain), INSL5 peptide Chen Y, Zhou Q, Wang J, Xu Y, Wang Y, Yan J, Wang Y, Zhu Q, Zhao F, Li C, Chen CW, Cai X, Bathgate RAD, Shen C, Eric Xu H, Yang D, Liu H, Wang MW 10.1038/S41467-023-36182-Z 2023-03-01
Gs αs Human Mini-Gs 55 β1 Human γ2 Human Cryo-EM 8F76 8F76_refined 3.1 O51E2 OR51E2 Odorant family 51 O1 (fish-like odorant) Human - Nanobody-35 - propanoic acid pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist - - Billesbolle CB, de March CA, van der Velden WJC, Ma N, Tewari J, Del Torrent CL, Li L, Faust B, Vaidehi N, Matsunami H, Manglik A 10.1038/S41586-023-05798-Y 2023-03-22
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8HSC - 3.2 GPR20 GPR20 A orphans A (Rhodopsin) Human BRIL Antibody fab fragment light chain
Antibody fab fragment heavy chain
scFv16 		- Apo (no ligand)
none Apo (no ligand) - - Lin X, Jiang S, Wu Y, Wei X, Han GW, Wu L, Liu J, Chen B, Zhang Z, Zhao S, Cherezov V, Xu F 10.1038/S41421-023-00520-8 2023-03-08
Gs αolf Human Golf-Gi chimera 59 β1 Human γ2 Human Cryo-EM 8IW1 - 3.4 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
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8FLS - 3.1 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - abaloparatide pubchem
small-molecule Agonist PTHrP-(1-36), PTHrP, PTH, TIP39 peptide Cary BP, Gerrard EJ, Belousoff MJ, Fletcher MM, Jiang Y, Russell IC, Piper SJ, Wootten D, Sexton PM 10.1016/J.STR.2023.04.002 2023-04-26
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7YKD - 2.8 CML1 chemerin Chemerin receptor A (Rhodopsin) Human - scFv16 - chemerin C-terminal peptide pubchem gtoplig chembl_ligand pubchem
peptide Agonist EPA, resolvin E1, chemerin, chemerin C-terminal peptide, 18R-HEPE peptide Wang J, Chen G, Liao Q, Lyu W, Liu A, Zhu L, Du Y, Ye RD 10.1073/PNAS.2214324120 2023-04-19
Gq/11 αq Human - 99 β1 Human γ2 Human Cryo-EM 8IYS - 3.0 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - scFv16 - TUG-891 pubchem gtoplig chembl_ligand
small-molecule Agonist oleic acid, myristic acid, α-linolenic acid, linoleic acid small-molecule Yin H, Inoue A, Ma Z, Zhu X, Xia R, Xu Z, Wang N, Duan Y, Zhang A, Guo C, He Y 10.1038/S41422-023-00835-X 2023-06-21
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8JR9 - 2.6 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 Zhao LH, He Q, Yuan Q, Gu Y, He X, Shan H, Li J, Wang K, Li Y, Hu W, Wu K, Shen J, Xu HE 10.1038/S41586-023-06467-W 2023-08-02
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8HOC - 3.0 HRH4 H4 Histamine A (Rhodopsin) Human - scFv16 - imetit pubchem gtoplig chembl_ligand pubchem
small-molecule Agonist CCL16, histamine small-molecule - - 2023-12-20
Gs αs Human Gi1-Gs chimera 60 β1 Human γ2 Bovine Cryo-EM 8INR - 2.7 MC5R MC5 Melanocortin A (Rhodopsin) Human - - - INTERMEDINE chembl_ligand pubchem pubchem pubchem
protein Agonist γ-MSH, agouti-related protein, β-MSH, α-MSH, ACTH peptide Chen VB, Arendall WB 3rd, Headd JJ, Keedy DA, Immormino RM, Kapral GJ, Murray LW, Richardson JS, Richardson DC 10.1107/S0907444909042073 2023-09-20
Gs αs Human - 59 β1 Human γ2 Mouse Cryo-EM 8JSO 8JSO_refined 3.4 TAAR1 TA1 Trace amine A (Rhodopsin) Human BRIL scFv16 - dexamfetamine pubchem gtoplig chembl_ligand drugbank drug_central
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
Gs αs Human - 55 β1 Human γ2 Human Cryo-EM 8U26 8U26_refined 2.5 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 Chen M, Schmid MF, Chiu W 10.1038/S41592-023-02082-9 2023-11-15
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 8GE9 8GE9_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
Gs αs Human - 76 β1 Human γ2 Human Cryo-EM 8GG9 8GG9_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
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8JXW 8JXW_refined 3.0 HRH4 H4 Histamine A (Rhodopsin) Human - scFv16 - CHEMBL213912 chembl_ligand pubchem
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
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8XQT - 2.9 T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human - scFv16 Exo-alpha-sialidase Cholesterol pubchem
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
Gq/11 αq Human - 57 β1 Rat γ2 Bovine Cryo-EM 8ZH8 - 3.2 QRFPR QRFP Peptide P518 A (Rhodopsin) Human - scFv16 - QRF-amide
peptide Agonist QRFP26 (26RFa), QRFP43, QRFP43 (43RFa) peptide Iwama A, Kise R, Akasaka H, Sano FK, Oshima HS, Inoue A, Shihoya W, Nureki O 10.1038/S41467-024-49030-5 2024-07-03
Gi/o αi1 Human - 66 β1 Human γ2 Human Cryo-EM 8K4P - 2.8 Q76SF8 ORF74 Unclassified A (Rhodopsin) HHV-8 - - - Apo (no ligand)
none Apo (no ligand) - - - - 2024-07-24
Gq/11 αq Human - 64 β1 Human γ2 Human Cryo-EM 8XGO - 2.7 KISSR kisspeptin Kisspeptin A (Rhodopsin) Human - scFv16 - TAK448
peptide Agonist kisspeptin-10, kisspeptin-54, kisspeptin-52, kisspeptin-14, kisspeptin-13 peptide Wu Z, Chen G, Qiu C, Yan X, Xu L, Jiang S, Xu J, Han R, Shi T, Liu Y, Gao W, Wang Q, Li J, Ye F, Pan X, Zhang Z, Ning P, Zhang B, Chen J, Du Y 10.1126/SCIADV.ADN7771 2024-10-30
Gi/o αt1 Bovine Only H5 3 - - - - X-ray 4J4Q 4J4Q_refined 2.7 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - B-Octylglucoside pubchem
small-molecule unknown - - Park JH, Morizumi T, Li Y, Hong JE, Pai EF, Hofmann KP, Choe HW, Ernst OP 10.1002/ANIE.201302374 2013-10-30
Gs αs Human Engineered G protein 50 - - - - X-ray 5G53 5G53_refined 3.4 AA2AR A2A Adenosine A (Rhodopsin) Human - - - NECA pubchem gtoplig chembl_ligand gtoplig
small-molecule Agonist adenosine small-molecule Carpenter B, Nehme R, Warne T, Leslie AG, Tate CG 10.1038/NATURE18966 2016-08-03
Gs αs Human Gs-Gi1 chimera 58 β1 Human γ2 Human Cryo-EM 6PB0 - 3.0 CRFR1 CRF1 Corticotropin-releasing factor B1 (Secretin) Human - Nanobody-35 - Urocortin pubchem
peptide Agonist corticotrophin-releasing hormone, urocortin 1, urocortin 2 peptide Ma S, Shen Q, Zhao LH, Mao C, Zhou XE, Shen DD, de Waal PW, Bi P, Li C, Jiang Y, Wang MW, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE 10.1016/J.MOLCEL.2020.01.013 2020-02-12
Gs αs Human - 49 β1 Human γ2 Human Cryo-EM 6WI9 6WI9_refined 4.3 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
Gs αs Human - 55 β1 Bovine γ2 Bovine Cryo-EM 7DHI - 3.3 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - Nanobody-35 - levosalbutamol pubchem gtoplig chembl_ligand drug_central drugbank
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule Yang F, Ling S, Zhou Y, Zhang Y, Lv P, Liu S, Fang W, Sun W, Hu LA, Zhang L, Shi P, Tian C 10.1093/NSR/NWAA284 2020-12-16
Gs αs Human Engineered G alpha 60 β1 Human γ2 Human Cryo-EM 7JVQ 7JVQ_refined 3.0 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - apomorphine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist L-NOREPINEPHRINE, noradrenaline, (-)-noradrenaline, 5-hydroxytryptamine, 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
Gi/o αi1 Human - 99 β1 Human γ2 Human Cryo-EM 7EB2 - 3.5 GABR2 GABAB2 GABAB C (Glutamate) Human - scFv16 - (-)-baclofen pubchem gtoplig chembl_ligand drugbank drugbank gtoplig pubchem
BHFF pubchem
small-molecule
small-molecule 		Agonist
PAM 		- - Shen C, Mao C, Xu C, Jin N, Zhang H, Shen DD, Shen Q, Wang X, Hou T, Chen Z, Rondard P, Pin JP, Zhang Y, Liu J 10.1038/S41586-021-03507-1 2021-05-05
Gi/o αi2 Human - 59 β1 Human γ2 Human Cryo-EM 7LD4 7LD4_refined 3.3 AA1R A1 Adenosine A (Rhodopsin) Human - - - adenosine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist adenosine small-molecule - - 2021-09-08
Gi/o αi2 Human - 61 β1 Human γ2 Human Cryo-EM 7F8V - 3.3 GASR CCK2 Cholecystokinin A (Rhodopsin) Human - - - 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
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7VV5 7VV5_refined 2.8 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human - scFv16 - compound 48/80 pubchem gtoplig
small-molecule 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
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7EW7 - 3.3 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - SEW2871 pubchem gtoplig chembl_ligand
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 7TYI - 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 2022-03-30
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7TUZ 7TUZ_refined 3.1 GP183 GPR183 A orphans A (Rhodopsin) Human - scFv16 - (2S,4aS,4bS,7R,8S,8aS,9R,10aR)-7-[(2R,3R)-7-hydroxy-3,7-dimethyloctan-2-yl]-4a,7,8-trimethyltetradecahydrophenanthrene-2,9-diol pubchem
small-molecule Agonist 27-hydroxycholesterol, 25-hydroxycholesterol, 7α,27-dihydroxycholesterol, 7α-hydroxycholesterol, 7β-hydroxycholesterol, 7β, 25-dihydroxycholesterol, 7α,25-dihydroxycholesterol, 7β, 27-dihydroxycholesterol small-molecule Chen H, Huang W, Li X 10.1016/J.STR.2022.04.006 2022-04-13
Gq/11 αq Human - 58 β1 Human γ2 Human Cryo-EM 7SR8 - 3.3 OX2R OX2 Orexin A (Rhodopsin) Human - scFv16 - methyl (2R,3S)-3-[(methanesulfonyl)amino]-2-({[(1s,4S)-4-phenylcyclohexyl]oxy}methyl)piperidine-1-carboxylate pubchem
small-molecule Agonist orexin-B, orexin-A peptide Yin J, Kang Y, McGrath AP, Chapman K, Sjodt M, Kimura E, Okabe A, Koike T, Miyanohana Y, Shimizu Y, Rallabandi R, Lian P, Bai X, Flinspach M, De Brabander JK, Rosenbaum DM 10.1038/S41467-022-30601-3 2022-06-08
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 7WKD - 3.0 TRFR TRH1 Thyrotropin-releasing hormone A (Rhodopsin) Human - scFv16 - TRH pubchem
peptide Agonist TRH peptide Xu Y, Cai H, You C, He X, Yuan Q, Jiang H, Cheng X, Jiang Y, Xu HE 10.1038/S41422-022-00641-X 2022-06-15
Gq/11 αq Human Gi2-mini-Gq chimera 57 β1 Human γ2 Human Cryo-EM 8DPH - 3.2 5HT2C 5-HT2C 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - lorcaserin pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist 5-hydroxytryptamine small-molecule Gumpper RH, Fay JF, Roth BL 10.1016/J.CELREP.2022.111211 2022-08-24
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7XZ5 - 3.1 GP119 GPR119 GPR18, GPR55 and GPR119 A (Rhodopsin) Human BRIL Nanobody-35 - (4R,7R,18E)-4,7-dihydroxy-N,N,N-trimethyl-10-oxo-3,5,9-trioxa-4-phosphaheptacos-18-en-1-aminium 4-oxide pubchem
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
Gq/11 αq Human Mini-Gq 59 β1 Human γ2 Human Cryo-EM 7WY5 - 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 8DWG - 2.7 MRGX1 MRGPRX1 A orphans A (Rhodopsin) Human - scFv16 - Proenkephalin-A
CHEMBL5177388 chembl_ligand pubchem
peptide
small-molecule 		Agonist
PAM 		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
Gi/o αi2 Human - 61 β1 Human γ2 Bovine Cryo-EM 7YK7 7YK7_refined 2.8 RL3R2 RXFP4 Relaxin family peptide A (Rhodopsin) Human - scFv16 - DC591053 pubchem gtoplig
small-molecule Agonist relaxin-3, relaxin-3 (B chain), INSL5 peptide Chen Y, Zhou Q, Wang J, Xu Y, Wang Y, Yan J, Wang Y, Zhu Q, Zhao F, Li C, Chen CW, Cai X, Bathgate RAD, Shen C, Eric Xu H, Yang D, Liu H, Wang MW 10.1038/S41467-023-36182-Z 2023-03-01
Gq/11 αq Human - 61 β1 Human γ2 Human Cryo-EM 8G59 8G59_refined 2.6 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - - - TUG-891 pubchem gtoplig chembl_ligand
small-molecule Agonist oleic acid, myristic acid, α-linolenic acid, linoleic acid small-molecule Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP 10.1126/SCIENCE.ADD6220 2023-03-08
Gi/o αo Human - 62 β1 Human γ2 Human Cryo-EM 7T90 7T90_refined 3.3 ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - acetylcholine pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
small-molecule Agonist acetylcholine small-molecule - - 2023-01-25
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7XV3 7XV3_refined 2.8 GP174 GPR174 A orphans A (Rhodopsin) Human - - - (2~{S})-2-$l^{4}-azanyl-3-[[(2~{R})-3-octadecanoyloxy-2-oxidanyl-propoxy]-oxidanyl-oxidanylidene-$l^{6}-phosphanyl]oxy-propanoic acid pubchem
small-molecule Agonist lysophosphatidylserine small-molecule Liang J, Inoue A, Ikuta T, Xia R, Wang N, Kawakami K, Xu Z, Qian Y, Zhu X, Zhang A, Guo C, Huang Z, He Y 10.1038/S41467-023-36575-0 2023-02-15
Gi/o αz Human - 59 β1 Human γ2 Human Cryo-EM 8DZS - 2.7 OPRK κ Opioid A (Rhodopsin) Human - scFv16 - CHEMBL277863 chembl_ligand pubchem
small-molecule 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 Han J, Zhang J, Nazarova AL, Bernhard SM, Krumm BE, Zhao L, Lam JH, Rangari VA, Majumdar S, Nichols DE, Katritch V, Yuan P, Fay JF, Che T 10.1038/S41586-023-06030-7 2023-05-03
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 8IRT - 2.7 DRD3 D3 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
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8H4I - 3.1 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - Nanobody-35 - docosahexaenoic acid pubchem gtoplig chembl_ligand drug_central drugbank pubchem
small-molecule Agonist oleic acid, myristic acid, α-linolenic acid, linoleic acid small-molecule Yin H, Inoue A, Ma Z, Zhu X, Xia R, Xu Z, Wang N, Duan Y, Zhang A, Guo C, He Y 10.1038/S41422-023-00835-X 2023-06-21
Gi/o αi1 Human - 55 β1 Human γ2 Human Cryo-EM 8FEG - 2.5 OPRK κ Opioid A (Rhodopsin) Human - scFv16 - ACE-TYR-ALA-DTY-THR-THR-CYS-THR-DPN-XT9
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 Muratspahic E, Deibler K, Han J, Tomasevic N, Jadhav KB, Olive-Marti AL, Hochrainer N, Hellinger R, Koehbach J, Fay JF, Rahman MH, Hegazy L, Craven TW, Varga BR, Bhardwaj G, Appourchaux K, Majumdar S, Muttenthaler M, Hosseinzadeh P, Craik DJ, Spetea M, Che T, Baker D, Gruber CW 10.1038/s41467-023-43718-w 2023-12-06
Gq/11 αq Human - 61 β1 Human γ2 Human Cryo-EM 8IA7 8IA7_refined 3.1 GASR CCK2 Cholecystokinin A (Rhodopsin) Human - - - CHEMBL216166 chembl_ligand pubchem
protein 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 2023-12-06
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8KH5 - 2.8 GP174 GPR174 A orphans A (Rhodopsin) Human - Nanobody-35 - Lysophosphotidylserine pubchem
small-molecule Agonist lysophosphatidylserine small-molecule Nie Y, Qiu Z, Chen S, Chen Z, Song X, Ma Y, Huang N, Cyster JG, Zheng S 10.1038/S41467-023-41654-3 2023-10-18
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8WC7 - 3.1 TAAR1 TA1 Trace amine A (Rhodopsin) Mouse - scFv16 - 2-[4-(3-Fluorophenyl)phenyl]ethan-1-amine 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 - 61 β1 Human γ2 Human Cryo-EM 8GEA 8GEA_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
Gs αs Human - 92 β1 Human γ2 Human Cryo-EM 8GGE 8GGE_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
Gi/o αi1 Human - 45 β1 Human γ2 Human Cryo-EM 8I7W 8I7W_refined 3.4 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - scFv16 - GSK256073 pubchem gtoplig chembl_ligand
small-molecule Agonist β-D-hydroxybutyric acid, butyric acid small-molecule Park JH, Kawakami K, Ishimoto N, Ikuta T, Ohki M, Ekimoto T, Ikeguchi M, Lee DS, Lee YH, Tame JRH, Inoue A, Park SY 10.1038/S41467-023-42764-8 2024-02-07
Gq/11 αq Human - 59 β1 Human γ2 Human Cryo-EM 8T3O - 3.1 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - scFv16 - TUG-891 pubchem gtoplig chembl_ligand
small-molecule Agonist oleic acid, myristic acid, α-linolenic acid, linoleic acid small-molecule Zhang X, Guseinov AA, Jenkins L, Li K, Tikhonova IG, Milligan G, Zhang C 10.1126/SCIADV.ADJ2384 2024-01-17
Gs αs Human GTP bound, Class B 57 β1 Human γ2 Human Cryo-EM 8UNM - 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 Gi2-mini-Gq chimera 58 β1 Human γ2 Human Cryo-EM 8UWL - 2.8 5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - lisuride pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist 5-hydroxytryptamine, tryptamine small-molecule Lyu J, Kapolka N, Gumpper R, Alon A, Wang L, Jain MK, Barros-Alvarez X, Sakamoto K, Kim Y, DiBerto J, Kim K, Glenn IS, Tummino TA, Huang S, Irwin JJ, Tarkhanova OO, Moroz Y, Skiniotis G, Kruse AC, Shoichet BK, Roth BL 10.1126/SCIENCE.ADN6354 2024-05-29
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8XIO - 2.7 SSR1 SST1 Somatostatin A (Rhodopsin) Human - Nanobody-35 - (2S)-N-[(4S)-6-amino-2,2,4-trimethylhexyl]-3-naphthalen-1-yl-2-[[2-phenylethyl(2-pyridin-2-ylethyl)carbamoyl]amino]propanamide pubchem
small-molecule Agonist cortistatin-14, SRIF-14, CST-17, SRIF-28 peptide - - 2024-07-03
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8XVI 8XVI_refined 3.3 EDNRA ETA Endothelin A (Rhodopsin) Human - Nanobody-35 Endoglucanase H ENDOTHELIN chembl_ligand pubchem
protein Agonist endothelin-2, endothelin-3, endothelin-1 peptide Hou J, Liu S, Zhang X, Tu G, Wu L, Zhang Y, Yang H, Li X, Liu J, Jiang L, Tan Q, Bai F, Liu Z, Miao C, Hua T, Luo Z 10.1038/S41421-024-00705-9 2024-08-28
Gi/o αi1 Human - 66 β1 Human γ2 Human Cryo-EM 8JJP - 2.9 CML2 chemerin 2 Chemerin receptor A (Rhodopsin) Human - scFv16 - chemerin C-terminal peptide pubchem gtoplig chembl_ligand pubchem
peptide Agonist chemerin peptide - - 2024-08-21
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 8YN9 - 2.3 HRH4 H4 Histamine A (Rhodopsin) Human - scFv16 - histamine pubchem gtoplig chembl_ligand drug_central drugbank gtoplig
small-molecule Agonist CCL16, 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
Gs αs Human - 56 β1 Human γ2 Human Cryo-EM 6WHC 6WHC_refined 3.4 GLR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - Dual-agonist peptide P15
peptide Agonist glucagon peptide Chang R, Zhang X, Qiao A, Dai A, Belousoff MJ, Tan Q, Shao L, Zhong L, Lin G, Liang YL, Ma L, Han S, Yang D, Danev R, Wang MW, Wootten D, Wu B, Sexton PM 10.1074/JBC.RA120.013793 2020-05-27
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7AUE 7AUE_refined 3.0 MC4R MC4 Melanocortin A (Rhodopsin) Human - scFv16 - setmelanotide pubchem gtoplig drug_central chembl_ligand drugbank
peptide Agonist γ-MSH, agouti-related protein, β-MSH, α-MSH, ACTH peptide Israeli H, Degtjarik O, Fierro F, Chunilal V, Gill AK, Roth NJ, Botta J, Prabahar V, Peleg Y, Chan LF, Ben-Zvi D, McCormick PJ, Niv MY, Shalev-Benami M 10.1126/SCIENCE.ABF7958 2021-04-28
Gs αs Human - 58 β1 Rat γ2 Bovine Cryo-EM 7F16 - 2.8 PTH2R PTH2 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - TIP39 gtoplig
peptide Agonist PTHrP-(1-34) (human), PTH, PTHrP, PTHrP-(1-36), TIP39 peptide Wang X, Cheng X, Zhao L, Wang Y, Ye C, Zou X, Dai A, Cong Z, Chen J, Zhou Q, Xia T, Jiang H, Xu HE, Yang D, Wang MW 10.1073/PNAS.2101279118 2021-08-18
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7S8M - 2.5 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human BRIL scFv16 - Cortistatin 14 pubchem
peptide Agonist PAMP-20 peptide 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 - 59 β1 Human γ2 Human Cryo-EM 7S3I - 2.5 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 Cary BP, Deganutti G, Zhao P, Truong TT, Piper SJ, Liu X, Belousoff MJ, Danev R, Sexton PM, Wootten D, Gellman SH 10.1038/S41589-021-00945-W 2022-01-05
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7VKT 7VKT_refined 2.9 LT4R1 BLT1 Leukotriene A (Rhodopsin) Human - scFv16 - LTB4 pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist 12R-HETE, LTB4, 20-hydroxy-LTB4 small-molecule Wang N, He X, Zhao J, Jiang H, Cheng X, Xia Y, Eric Xu H, He Y 10.1038/S41467-022-28820-9 2022-03-09
Gi/o αi2 Human - 63 β1 Human γ2 Human Cryo-EM 7WVV 7WVV_refined 2.9 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human BRIL - - 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 - - 2022-04-13
Gs αs Human Mini-Gs 53 β1 Human γ2 Human Cryo-EM 7WU2 - 2.8 AGRD1 ADGRD1 ADGRD B2 (Adhesion) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Qu X, Qiu N, Wang M, Zhang B, Du J, Zhong Z, Xu W, Chu X, Ma L, Yi C, Han S, Shui W, Zhao Q, Wu B 10.1038/S41586-022-04580-W 2022-04-27
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7V6A - 3.6 ACM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - methyl 4-[4-(3-methyl-2-oxidanylidene-benzimidazol-1-yl)piperidin-1-yl]piperidine-1-carboxylate pubchem
small-molecule Allosteric agonist 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 - 61 β1 Human γ2 Human Cryo-EM 7XBW 7XBW_refined 2.8 CX3C1 CX3CR1 Chemokine A (Rhodopsin) Human - - - Apo (no ligand)
none Apo (no ligand) CX3CL1 peptide Lu M, Zhao W, Han S, Lin X, Xu T, Tan Q, Wang M, Yi C, Chu X, Yang W, Zhu Y, Wu B, Zhao Q 10.1126/SCIADV.ABN8048 2022-07-13
Gq/11 αq Human - 57 β1 Bovine γ2 Bovine Cryo-EM 7X1T - 3.3 TRFR TRH1 Thyrotropin-releasing hormone A (Rhodopsin) Human - scFv16 - taltirelin pubchem gtoplig chembl_ligand
small-molecule Agonist TRH peptide Yang F, Zhang H, Meng X, Li Y, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C 10.1038/S41422-022-00646-6 2022-08-31
Gs αs Human - 59 β1 Rat γ2 Bovine Cryo-EM 7VVJ 7VVJ_refined 3.2 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - PTHrP[1-36]
peptide Agonist PTHrP-(1-36), PTHrP, PTH, TIP39 peptide Kobayashi K, Kawakami K, Kusakizako T, Miyauchi H, Tomita A, Kobayashi K, Shihoya W, Yamashita K, Nishizawa T, Kato HE, Inoue A, Nureki O 10.1016/J.MOLCEL.2022.07.003 2022-08-03
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 7VIG 7VIG_refined 2.9 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - icanbelimod pubchem gtoplig chembl_ligand
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
Gs αs Human - 56 β1 Human γ2 Human Cryo-EM 8E3Y - 2.3 VIPR1 VPAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - [Ac-His1]PACAP-27 gtoplig chembl_ligand pubchem
peptide Agonist PHM, GHRH, VIP, PACAP-27, PHI, secretin, PACAP-38 peptide Piper SJ, Deganutti G, Lu J, Zhao P, Liang YL, Lu Y, Fletcher MM, Hossain MA, Christopoulos A, Reynolds CA, Danev R, Sexton PM, Wootten D 10.1038/S41467-022-34629-3 2022-11-23
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 7Y67 7Y67_refined 2.8 C5AR1 C5a1 Complement peptide A (Rhodopsin) Human - scFv16 - C089
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 - 64 β1 Human γ2 Human Cryo-EM 8ID3 8ID3_refined 3.1 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - scFv16 - 9-Hydroxyoctadecanoic acid pubchem
small-molecule Agonist oleic acid, myristic acid, α-linolenic acid, linoleic acid small-molecule Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP 10.1126/SCIENCE.ADD6220 2023-03-15
Gs αs Human Mini-Gs 59 β1 Human γ2 Human Cryo-EM 8IW9 - 3.1 TAAR9 TAAR9 A orphans A (Rhodopsin) Mouse - scFv16
Nanobody-35 		- Cadaverine 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 - 64 β1 Human γ2 Human Cryo-EM 7TRQ - 2.5 ACM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - iperoxo pubchem gtoplig chembl_ligand
VU0467154 pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Agonist
PAM 		acetylcholine small-molecule - - 2023-05-17
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7TRP - 2.4 ACM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - iperoxo pubchem gtoplig chembl_ligand
LY2033298 pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Agonist
PAM 		acetylcholine small-molecule - - 2023-05-17
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8F2B - 2.0 CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP3 		- 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 8PM2 - 2.9 TAA7F TAAR7F A orphans A (Rhodopsin) Mouse - Nanobody-35 - N,N-Dimethylcyclohexylamine pubchem
small-molecule Agonist - - Gusach A, Lee Y, Khoshgrudi AN, Mukhaleva E, Ma N, Koers EJ, Chen Q, Edwards PC, Huang F, Kim J, Mancia F, Verprintsev DB, Vaidehi N, Weyand SN, Tate CG 10.1101/2023.07.07.547762 2023-08-09
Gi/o αi1 Human - 62 β1 Mouse γ2 Mouse Cryo-EM 8IHF - 3.0 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human BRIL scFv16 - MK 6892 pubchem gtoplig chembl_ligand pubchem
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 2023-08-30
Gs αs Human - 60 β1 Rat γ2 Bovine Cryo-EM 8JIS 8JIS_refined 2.5 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Dual-agonist peptide P15
peptide Agonist glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide 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 2023-11-08
Gi/o αi1 Human - 66 β1 Human γ2 Human Cryo-EM 8FYT - 2.6 5HT1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - Lysergide pubchem gtoplig chembl_ligand drugbank drug_central
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 - 58 β1 Human γ2 Human Cryo-EM 8GFZ - 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
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8J6I 8J6I_refined 2.9 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 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
Gs αs Human - 56 β1 Human γ2 Human Cryo-EM 8QJ2 8QJ2_refined 3.4 MC4R MC4 Melanocortin A (Rhodopsin) Human - Nanobody-35 - pN162
protein Apo (no ligand) γ-MSH, agouti-related protein, β-MSH, α-MSH, ACTH peptide - - 2024-09-25
Gs αs Human GTP bound, Class E 60 β1 Human γ2 Human Cryo-EM 8UNP - 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 8WA3 8WA3_refined 2.9 GIPR GIP Glucagon B1 (Secretin) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) gastric inhibitory polypeptide 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
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 8X7A 8X7A_refined 2.6 PI2R IP Prostanoid A (Rhodopsin) Human - Nanobody-35 - treprostinil pubchem gtoplig chembl_ligand drugbank drug_central
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
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8XZF 8XZF_refined 3.0 APJ apelin Apelin A (Rhodopsin) Human - scFv16 - WN561
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 Gs-Gi chimera 52 β1 Human γ2 Human Cryo-EM 9BKJ - 2.6 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 8UXY - 3.3 OR1F1 OR1F1 Odorant family 1 O2 (tetrapod specific odorant) Human - Nanobody-35 - l-Menthol 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
Gq/11 αq Human - 64 β1 Human γ2 Human Cryo-EM 8XGS - 3.0 KISSR kisspeptin Kisspeptin A (Rhodopsin) Human - scFv16 - Kisspeptin-10 pubchem
peptide Agonist kisspeptin-10, kisspeptin-54, kisspeptin-52, kisspeptin-14, kisspeptin-13 peptide Wu Z, Chen G, Qiu C, Yan X, Xu L, Jiang S, Xu J, Han R, Shi T, Liu Y, Gao W, Wang Q, Li J, Ye F, Pan X, Zhang Z, Ning P, Zhang B, Chen J, Du Y 10.1126/SCIADV.ADN7771 2024-10-30
Gs αs Bovine - 57 β1 Rat γ2 Bovine Cryo-EM 6NBH - 3.5 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
Gi/o αo Human - 60 β1 Mouse γ2 Human Cryo-EM 6K41 - 2.9 ADA2B α2B Adrenoceptors A (Rhodopsin) Human T4-Lysozyme scFv - dexmedetomidine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist (-)-noradrenaline, (-)-adrenaline small-molecule Yuan D, Liu Z, Kaindl J, Maeda S, Zhao J, Sun X, Xu J, Gmeiner P, Wang HW, Kobilka BK 10.1038/S41589-020-0492-2 2020-04-15
Gi/o αi1 Human - 65 β1 Human γ2 Human Cryo-EM 6LFO 6LFO_refined 3.4 CXCR2 CXCR2 Chemokine A (Rhodopsin) Human - scFv16 - Interleukin-8 pubchem
protein Agonist CXCL3, CXCL8, CXCL7, CXCL2, CXCL1, CXCL6, CXCL5 peptide Liu K, Wu L, Yuan S, Wu M, Xu Y, Sun Q, Li S, Zhao S, Hua T, Liu ZJ 10.1038/S41586-020-2492-5 2020-09-02
Gs αs Human Engineered G alpha 60 β1 Rat γ2 Bovine Cryo-EM 7LJC - 3.0 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - CHEMBL1160787 chembl_ligand pubchem
mevidalen pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Agonist
PAM 		L-NOREPINEPHRINE, noradrenaline, (-)-noradrenaline, 5-hydroxytryptamine, dopamine small-molecule Zhuang Y, Krumm B, Zhang H, Zhou XE, Wang Y, Huang XP, Liu Y, Cheng X, Jiang Y, Jiang H, Zhang C, Yi W, Roth BL, Zhang Y, Xu HE 10.1038/S41422-021-00482-0 2021-03-03
Gs αs Human - 89 β1 Human γ2 Human Cryo-EM 7KI1 - 2.5 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - taspoglutide pubchem gtoplig drugbank
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 - 58 β1 Human γ2 Human Cryo-EM 7F54 - 3.0 MC4R MC4 Melanocortin A (Rhodopsin) Human - Nanobody-35 - afamelanotide pubchem gtoplig chembl_ligand drugbank pubchem pubchem pubchem pubchem
peptide Agonist γ-MSH, agouti-related protein, β-MSH, α-MSH, ACTH peptide Zhang H, Chen LN, Yang D, Mao C, Shen Q, Feng W, Shen DD, Dai A, Xie S, Zhou Y, Qin J, Sun JP, Scharf DH, Hou T, Zhou T, Wang MW, Zhang Y 10.1038/S41422-021-00552-3 2021-11-03
Gi/o αi1 Human - 43 β1 Human γ2 Human Cryo-EM 7EO4 7EO4_refined 2.9 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 Xu Z, Ikuta T, Kawakami K, Kise R, Qian Y, Xia R, Sun MX, Zhang A, Guo C, Cai XH, Huang Z, Inoue A, He Y 10.1038/S41589-021-00930-3 2022-01-05
Gq/11 αq Human Gamma subunit fused to alpha subunit 55 β1 Human - - Cryo-EM 7RYC - 2.9 OXYR OT Vasopressin and oxytocin A (Rhodopsin) Human - scFv16 - oxytocin pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
peptide Agonist oxytocin, vasopressin peptide Meyerowitz JG, Robertson MJ, Barros-Alvarez X, Panova O, Nwokonko RM, Gao Y, Skiniotis G 10.1038/S41594-022-00728-4 2022-03-09
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7TYO - 2.7 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
G12/13 α13 Human Gi2-mini-G13 chimera 56 β1 Human γ2 Human Cryo-EM 7SF8 - 2.7 AGRG1 ADGRG1 ADGRG 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 - 61 β1 Bovine γ2 Bovine Cryo-EM 7SQO - 3.2 OX2R OX2 Orexin A (Rhodopsin) Human - scFv16 - methyl (2R,3S)-3-[(methanesulfonyl)amino]-2-({[(1s,4S)-4-phenylcyclohexyl]oxy}methyl)piperidine-1-carboxylate pubchem
small-molecule Agonist orexin-B, orexin-A peptide Yin J, Kang Y, McGrath AP, Chapman K, Sjodt M, Kimura E, Okabe A, Koike T, Miyanohana Y, Shimizu Y, Rallabandi R, Lian P, Bai X, Flinspach M, De Brabander JK, Rosenbaum DM 10.1038/S41467-022-30601-3 2022-05-25
Gi/o αo Human Mini-Go 60 β1 Human γ2 Human Cryo-EM 7UM5 7UM5_refined 2.7 5HT5A 5-HT5A 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - 5-CT pubchem gtoplig chembl_ligand
small-molecule Agonist 5-hydroxytryptamine small-molecule Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL 10.1038/S41594-022-00796-6 2022-07-20
Gi/o αi1 Human - 62 β1 Mouse γ2 Mouse Cryo-EM 7Y12 - 3.1 MRGRD MRGPRD A orphans A (Rhodopsin) Human BRIL scFv16 - β-alanine pubchem gtoplig chembl_ligand drugbank pubchem
small-molecule Agonist β-alanine small-molecule Suzuki S, Iida M, Hiroaki Y, Tanaka K, Kawamoto A, Kato T, Oshima A 10.1038/S42003-022-03668-3 2022-07-20
Gi/o αo Human - 59 β1 Human γ2 Human Cryo-EM 7QVM - 3.3 OXYR OT Vasopressin and oxytocin A (Rhodopsin) Human - scFv16 - oxytocin pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
peptide Agonist oxytocin, vasopressin peptide Waltenspuhl Y, Ehrenmann J, Vacca S, Thom C, Medalia O, Pluckthun A 10.1038/S41467-022-31325-0 2022-08-10
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7YP7 - 3.1 AGRG2 ADGRG2 ADGRG B2 (Adhesion) Mouse - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - - - 2022-08-24
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7VIH 7VIH_refined 3.0 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - icanbelimod pubchem gtoplig chembl_ligand
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
Gq/11 αq Human Mini-Gq 60 β1 Human γ2 Human Cryo-EM 7Y27 7Y27_refined 3.5 SSR2 SST2 Somatostatin A (Rhodopsin) Human - scFv16 - SOMATOSTATIN chembl_ligand pubchem
protein Agonist cortistatin-14, SRIF-14, CST-17, SRIF-28 peptide Chen S, Teng X, Zheng S 10.1038/S41589-022-01130-3 2022-10-19
Gi/o αi1 Human - 61 β1 Rat γ2 Bovine Cryo-EM 8EFQ - 3.3 OPRM μ Opioid A (Rhodopsin) Human - - - DAMGO pubchem gtoplig chembl_ligand chembl_ligand
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 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
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7YON 7YON_refined 3.0 NPY2R Y2 Neuropeptide Y A (Rhodopsin) Human - scFv16 - Peptide YY
peptide Agonist peptide YY, PYY-(3-36), neuropeptide Y-(3-36), pancreatic polypeptide, neuropeptide Y peptide Kang H, Park C, Choi YK, Bae J, Kwon S, Kim J, Choi C, Seok C, Im W, Choi HJ 10.1016/J.STR.2022.11.010 2023-03-22
Gq/11 αq Human - 98 β1 Human γ2 Human Cryo-EM 7W3Z - 3.0 GRPR BB2 Bombesin A (Rhodopsin) Human - scFv16 - Gastrin-releasing peptide pubchem
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
Gs αs Human Mini-Gs 57 β1 Human γ2 Human Cryo-EM 7XY7 - 3.3 AA2BR A2B Adenosine A (Rhodopsin) Human BRIL - - NECA pubchem gtoplig chembl_ligand gtoplig
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 - 59 β1 Human γ2 Human Cryo-EM 8FLT - 3.0 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - M-PTH(1-14)
peptide Agonist PTHrP-(1-36), PTHrP, PTH, TIP39 peptide Cary BP, Gerrard EJ, Belousoff MJ, Fletcher MM, Jiang Y, Russell IC, Piper SJ, Wootten D, Sexton PM 10.1016/J.STR.2023.04.002 2023-04-26
Gq/11 αq Human - 57 β1 Human γ2 Human Cryo-EM 8H0P - 3.2 NMBR BB1 Bombesin A (Rhodopsin) Human - scFv16 - NMB30
peptide Agonist neuromedin B, gastrin-releasing peptide, GRP-(18-27), gastrin releasing peptide(14-27) (human) peptide Li C, Xu Y, Liu H, Cai H, Jiang Y, Xu HE, Yin W 10.1038/S41422-022-00743-6 2023-08-09
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8GDB 8GDB_refined 3.1 PE2R4 EP4 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
Gi/o αo Human - 59 β1 Human γ2 Human Cryo-EM 8I9S 8I9S_refined 3.3 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
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8J6Q - 2.6 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - scFv16 - β-D-hydroxybutyric acid pubchem gtoplig chembl_ligand
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 8JSP - 3.7 5HT1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - ulotaront pubchem gtoplig drugbank chembl_ligand
small-molecule Agonist 5-hydroxytryptamine 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 8WCA - 3.5 TAAR1 TA1 Trace amine A (Rhodopsin) Human - scFv16 - 2-Phenylethanaminium pubchem
small-molecule Agonist octopamine, β-phenylethylamine, CHEMBL1160703, tyramine, (+)-Octopamine, 3-iodothyronamine, dopamine 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 - 60 β1 Human γ2 Human Cryo-EM 8GE8 8GE8_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 - 83 β1 Human γ2 Human Cryo-EM 8GGA 8GGA_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 8JBF - 3.0 NK3R NK3 Tachykinin A (Rhodopsin) Human - scFv16 - senktide pubchem gtoplig chembl_ligand
peptide Agonist neurokinin A, substance P, neurokinin B peptide Sun W, Yang F, Zhang H, Yuan Q, Ling S, Wang Y, Lv P, Li Z, Luo Y, Liu D, Yin W, Shi P, Xu HE, Tian C 10.1038/S41421-023-00564-W 2024-02-28
Gi/o αi3 Human - 63 β1 Human γ2 Human Cryo-EM 8SZH - 3.1 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 - 58 β1 Human γ2 Human Cryo-EM 8WW2 - 2.8 GPR3 GPR3 A orphans A (Rhodopsin) Human - Nanobody-35 - oleic acid pubchem gtoplig chembl_ligand drug_central
small-molecule Agonist sphingosine 1-phosphate small-molecule Xiong Y, Xu Z, Li X, Wang Y, Zhao J, Wang N, Duan Y, Xia R, Han Z, Qian Y, Liang J, Zhang A, Guo C, Inoue A, Xia Y, Chen Z, He Y 10.1038/S41422-024-00932-5 2024-02-14
Gq/11 αq Human - 59 β1 Human γ2 Human Cryo-EM 8XOH 8XOH_refined 3.2 GPER1 GPER Estrogen (G protein-coupled) A (Rhodopsin) Human - scFv16 - PGE2 pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
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
Gq/11 αq Human - 63 β1 Human γ2 Human Cryo-EM 8ZJE - 3.1 KISSR kisspeptin Kisspeptin A (Rhodopsin) Human - scFv16 - ACY-DTY-HYP-ASN-THR-PHE-XZA-LEU-NMM-TRP-NH2
peptide Agonist kisspeptin-10, kisspeptin-54, kisspeptin-52, kisspeptin-14, kisspeptin-13 peptide - - 2024-07-03
Gq/11 αq Human Mini-Gq 64 β1 Human γ2 Human Cryo-EM 8YN4 - 3.0 HRH2 H2 Histamine A (Rhodopsin) Human - scFv16 - 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 9JR3 - 2.8 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - scFv16 - Parathyroid hormone pubchem
peptide Agonist PTHrP-(1-36), PTHrP, PTH, TIP39 peptide - - 2024-10-16
Gi/o αi1 Human - 60 β1 Bovine γT1 Bovine Cryo-EM 6QNO - 4.4 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - Fab antibody fragment light chain
Fab antibody fragment heavy chain 		- Retinal (all-trans) pubchem
small-molecule Agonist - - Tsai CJ, Marino J, Adaixo R, Pamula F, Muehle J, Maeda S, Flock T, Taylor NM, Mohammed I, Matile H, Dawson RJ, Deupi X, Stahlberg H, Schertler G 10.7554/ELIFE.46041 2019-07-10
Gs αs Human - 49 β1 Human γ2 Human Cryo-EM 6P9X - 2.9 CRFR1 CRF1 Corticotropin-releasing factor B1 (Secretin) Human - Nanobody-35 - Corticoliberin pubchem
peptide Agonist corticotrophin-releasing hormone, urocortin 1, urocortin 2 peptide Liang YL, Belousoff MJ, Zhao P, Koole C, Fletcher MM, Truong TT, Julita V, Christopoulos G, Xu HE, Zhang Y, Khoshouei M, Christopoulos A, Danev R, Sexton PM, Wootten D 10.1016/J.MOLCEL.2020.01.012 2020-02-05
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 6XBL - 3.9 SMO SMO Frizzled F (Frizzled) Human - scFv16 - Cholesterol pubchem
SAG1.3 pubchem gtoplig chembl_ligand
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
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 7E9G - 3.5 GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human - scFv16 DN13 eglumegad pubchem gtoplig chembl_ligand gtoplig
JNJ-40411813 pubchem gtoplig chembl_ligand drugbank
small-molecule
small-molecule 		Agonist
PAM 		L-glutamic acid small-molecule Lin S, Han S, Cai X, Tan Q, Zhou K, Wang D, Wang X, Du J, Yi C, Chu X, Dai A, Zhou Y, Chen Y, Zhou Y, Liu H, Liu J, Yang D, Wang MW, Zhao Q, Wu B 10.1038/S41586-021-03495-2 2021-06-23
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7EW1 7EW1_refined 3.4 S1PR5 S1P5 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
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7VLA 7VLA_refined 2.7 CCR1 CCR1 Chemokine A (Rhodopsin) Human - scFv16 - CCL15(27-92)
peptide Agonist CCL14, CCL15, CCL8, CCL5, CCL16, CCL4, CCL23, CCL13, CCL7, CCL3 peptide Shao Z, Shen Q, Yao B, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Ma H, Chen ZH, Xu HE, Ying S, Zhang Y, Shen H 10.1038/S41589-021-00918-Z 2022-03-23
Gs αs Human - 56 β1 Human γ2 Human Cryo-EM 7RG9 7RG9_refined 3.2 GLP1R GLP-1 Glucagon B1 (Secretin) Human - scFv16
Nanobody-35 		- Apo (no ligand)
none Apo (no ligand) glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide 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 - 63 β1 Human γ2 Human Cryo-EM 7F6H 7F6H_refined 2.9 BKRB2 B2 Bradykinin A (Rhodopsin) Human - - - 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 Shen J, Zhang D, Fu Y, Chen A, Yang X, Zhang H 10.1038/S41467-022-28399-1 2022-01-05
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7WZ4 - 3.0 GPR88 GPR88 A orphans A (Rhodopsin) Human - scFv16 - Apo (no ligand)
none Apo (no ligand) - - Chen G, Xu J, Inoue A, Schmidt MF, Bai C, Lu Q, Gmeiner P, Liu Z, Du Y 10.1038/S41467-022-30081-5 2022-10-26
Gq/11 αq Human Mini-Gq 57 β1 Human γ2 Human Cryo-EM 8E9W - 2.7 ACM3 M3 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - CHEMBL73538 chembl_ligand pubchem
small-molecule Agonist acetylcholine small-molecule Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL 10.1038/S41586-022-05489-0 2022-11-30
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8ID6 - 2.8 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - scFv16 - oleic acid pubchem gtoplig chembl_ligand drug_central
small-molecule Agonist oleic acid, myristic acid, α-linolenic acid, linoleic acid small-molecule Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP 10.1126/SCIENCE.ADD6220 2023-03-15
Gq/11 αq Human - 59 β1 Rat γ2 Bovine Cryo-EM 7XWO 7XWO_refined 2.7 NK2R NK2 Tachykinin A (Rhodopsin) Human BRIL scFv16 - HIS-LYS-THR-ASP-SER-PHE-VAL-GLY-LEU-MET-NH2
peptide Agonist hemokinin 1, neurokinin A, neuropeptide K, neurokinin B, substance P, neuropeptide γ peptide - - 2023-05-31
Gi/o αi1 Human - 64 β1 Rat γ2 Bovine Cryo-EM 8HK2 - 2.9 C3AR C3a Complement peptide A (Rhodopsin) Human - scFv16 - C3a anaphylatoxin pubchem
peptide Agonist C5a, C3a 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
Gs αs Human - 61 β1 Human γ2 Human Cryo-EM 8HMP - 2.8 GPR52 GPR52 A orphans A (Rhodopsin) Human - Nanobody-35 - derivative 17 [Nakahata et al., 2018] pubchem gtoplig chembl_ligand
small-molecule Agonist - - Fan Y, Lin X, Pan B, Chen B, Liu D, Wuthrich K, Xu F 10.1002/MCO2.260 2023-06-21
Gi/o αi1 Human - 56 β1 Human γ2 Human Cryo-EM 8GCM - 3.5 PE2R4 EP4 Prostanoid A (Rhodopsin) Human - scFv16 - (5S)-5-[(3R)-4,4-difluoro-3-hydroxy-4-phenylbutyl]-1-[6-(1H-tetrazol-5-yl)hexyl]pyrrolidin-2-one pubchem
lipid 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 2024-01-03
Gi/o αi1 Human - 60 β1 Human γ2 Human Cryo-EM 8HQE 8HQE_refined 3.0 GP132 GPR132 A orphans A (Rhodopsin) Human BRIL scFv16 - Apo (no ligand)
none Apo (no ligand) 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 Gi1-Gs chimera 60 β1 Human γ2 Bovine Cryo-EM 8IOC - 2.9 MC3R MC3 Melanocortin A (Rhodopsin) Human - Nanobody-35 - γ-MSH pubchem gtoplig pubchem
peptide Agonist γ-MSH, agouti-related protein, β-MSH, α-MSH, ACTH peptide Chen VB, Arendall WB 3rd, Headd JJ, Keedy DA, Immormino RM, Kapral GJ, Murray LW, Richardson JS, Richardson DC 10.1107/S0907444909042073 2023-09-20
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8JZ7 8JZ7_refined 2.6 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 Cheng L, Sun S, Wang H, Zhao C, Tian X, Liu Y, Fu P, Shao Z, Chai R, Yan W 10.1038/S41392-023-01625-Y 2023-10-04
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8W8Q 8W8Q_refined 2.9 GP101 GPR101 A orphans A (Rhodopsin) Human BRIL Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Yang Z, Wang JY, Yang F, Zhu KK, Wang GP, Guan Y, Ning SL, Lu Y, Li Y, Zhang C, Zheng Y, Zhou SH, Wang XW, Wang MW, Xiao P, Yi F, Zhang C, Zhang PJ, Xu F, Liu BH, Zhang H, Yu X, Gao N, Sun JP 10.1038/S41589-023-01456-6 2024-01-03
Gi/o αi1 Human - 62 β1 Rat γ2 Bovine Cryo-EM 8XBH 8XBH_refined 2.8 GPR34 GPR34 A orphans A (Rhodopsin) Human - scFv16 - CHEMBL4758243 chembl_ligand pubchem
small-molecule Agonist lysophosphatidylserine small-molecule - - 2023-12-27
Gs αs Human - 79 β1 Human γ2 Human Cryo-EM 8GEJ 8GEJ_refined 4.2 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
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 8JHI - 3.2 FZD3 FZD3 Frizzled F (Frizzled) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - - - 2024-01-17
Gq/11 αq Human - 59 β1 Human γ2 Human Cryo-EM 8T3S - 3.1 FFAR2 FFA2 Free fatty acid A (Rhodopsin) Human - scFv16 - butyric acid pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist propanoic acid, acetic acid, trans-2-methylcrotonic acid, butyric acid small-molecule Zhang X, Guseinov AA, Jenkins L, Li K, Tikhonova IG, Milligan G, Zhang C 10.1126/SCIADV.ADJ2384 2024-01-24
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8UGY - 3.3 5HT1E 5-HT1E 5-Hydroxytryptamine A (Rhodopsin) Human - - - CHEMBL252719 chembl_ligand pubchem
small-molecule Agonist 5-hydroxytryptamine, tryptamine small-molecule Zilberg G, Parpounas AK, Warren AL, Fiorillo B, Provasi D, Filizola M, Wacker D 10.1126/SCIADV.ADK4855 2024-05-01
Gs αs Human GTP bound, Class L 59 β1 Human γ2 Human Cryo-EM 8UNW - 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 Rat γ2 Bovine Cryo-EM 8X16 8X16_refined 3.3 AA3R A3 Adenosine A (Rhodopsin) Human - scFv16 - piclidenoson pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist adenosine small-molecule Cai H, Guo S, Xu Y, Sun J, Li J, Xia Z, Jiang Y, Xie X, Xu HE 10.1038/S41467-024-47207-6 2024-04-24
Gi/o αgust Human - 63 β1 Human γ2 Human Cryo-EM 8XQP - 3.3 T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human - scFv16 Exo-alpha-sialidase aristolochic acid pubchem gtoplig chembl_ligand
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
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8YY8 - 3.2 FZD7 FZD7 Frizzled F (Frizzled) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Xu L, Chen B, Schihada H, Wright SC, Turku A, Wu Y, Han GW, Kowalski-Jahn M, Kozielewicz P, Bowin CF, Zhang X, Li C, Bouvier M, Schulte G, Xu F 10.1038/S41422-021-00525-6 2024-04-24
Gq/11 αq Human Gq-Gs-Gi chimera 59 β1 Human γ2 Human Cryo-EM 9AXF - 3.5 CASR CaS Calcium-sensing C (Glutamate) Human - scFv16 - Cyclomethyltryptophan pubchem
tecalcet pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Agonist
PAM 		Ca2+, spermine, Mg2+, L-tryptophan small-molecule Zuo H, Park J, Frangaj A, Ye J, Lu G, Manning JJ, Asher WB, Lu Z, Hu GB, Wang L, Mendez J, Eng E, Zhang Z, Lin X, Grassucci R, Hendrickson WA, Clarke OB, Javitch JA, Conigrave AD, Fan QR 10.1038/S41586-024-07331-1 2024-04-17
Gs αs Human - 59 β1 Rat γ2 Bovine Cryo-EM 5VAI - 4.1 G1SGD4 GLP-1 Glucagon B1 (Secretin) Rabbit - - - CHEMBL410972 chembl_ligand pubchem pubchem
protein Agonist - - Zhang Y, Sun B, Feng D, Hu H, Chu M, Qu Q, Tarrasch JT, Li S, Sun Kobilka T, Kobilka BK, Skiniotis G 10.1038/NATURE22394 2017-05-24
Gs αs Human - 56 β1 Human γ2 Human Cryo-EM 6WPW 6WPW_refined 3.1 GLR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - Glucagon derivative ZP3780
peptide Agonist glucagon peptide Hilger D, Kumar KK, Hu H, Pedersen MF, O'Brien ES, Giehm L, Jennings C, Eskici G, Inoue A, Lerch M, Mathiesen JM, Skiniotis G, Kobilka BK 10.1126/SCIENCE.ABA3373 2020-08-12
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7CX2 - 2.8 PE2R2 EP2 Prostanoid A (Rhodopsin) Human - Nanobody-35 - PGE2 pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
small-molecule Agonist PGF2α, PGI2, PGD2, thromboxane A2, PGE1, PGE2 small-molecule Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y 10.1126/SCIADV.ABF1268 2021-05-05
Gs αs Human - 49 β1 Bovine γ2 Mouse Cryo-EM 7E14 - 2.9 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - N-Tert-butyl-6,7-dichloroquinoxalin-2-amine pubchem
orforglipron pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Ago-PAM
Agonist 		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 2021-07-07
Gq/11 αq Human Gs-Gq chimera 52 β1 Human γ2 Human Cryo-EM 7RMG - 3.0 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
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7S1M 7S1M_refined 2.4 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 Cary BP, Deganutti G, Zhao P, Truong TT, Piper SJ, Liu X, Belousoff MJ, Danev R, Sexton PM, Wootten D, Gellman SH 10.1038/S41589-021-00945-W 2022-01-05
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7VL8 7VL8_refined 2.9 CCR1 CCR1 Chemokine A (Rhodopsin) Human - scFv16 - Apo (no ligand)
none Apo (no ligand) CCL14, CCL15, CCL8, CCL5, CCL16, CCL4, CCL23, CCL13, CCL7, CCL3 peptide Shao Z, Shen Q, Yao B, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Ma H, Chen ZH, Xu HE, Ying S, Zhang Y, Shen H 10.1038/S41589-021-00918-Z 2022-03-23
Gs αs Bovine - 60 β1 Rat γ2 Bovine Cryo-EM 7FIY - 3.4 GIPR GIP Glucagon B1 (Secretin) Human - Nanobody-35 - tirzepatide pubchem gtoplig
peptide Agonist gastric inhibitory polypeptide 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
Gs αs Human - 53 β1 Rat γ2 Bovine Cryo-EM 7VBH 7VBH_refined 3.0 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Peptide 20
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 2022-04-06
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7F1O - 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
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7XTA 7XTA_refined 3.2 5HT4R 5-HT4 5-Hydroxytryptamine A (Rhodopsin) Human BRIL scFv16 - 5-hydroxytryptamine pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist 5-hydroxytryptamine small-molecule Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE 10.1016/J.MOLCEL.2022.05.031 2022-07-27
Gq/11 αq Human Gi2-mini-Gq chimera 57 β1 Human γ2 Human Cryo-EM 8DPI - 3.4 5HT2C 5-HT2C 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - lorcaserin pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist 5-hydroxytryptamine small-molecule Gumpper RH, Fay JF, Roth BL 10.1016/J.CELREP.2022.111211 2022-08-24
Gs αs Human - 58 β1 Rat γ2 Bovine Cryo-EM 7VVL 7VVL_refined 2.8 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 Kobayashi K, Kawakami K, Kusakizako T, Miyauchi H, Tomita A, Kobayashi K, Shihoya W, Yamashita K, Nishizawa T, Kato HE, Inoue A, Nureki O 10.1016/J.MOLCEL.2022.07.003 2022-08-03
Gi/o αo Human - 59 β1 Human γ2 Human Cryo-EM 7W7E - 3.4 ADA2A α2A Adrenoceptors A (Rhodopsin) Human - scFv16 - 5-(3-Bicyclo[4.2.0]octa-1,3,5-trienyl)-1,2,3,6-tetrahydropyridine pubchem
small-molecule Agonist (-)-noradrenaline, (-)-adrenaline small-molecule Fink EA, Xu J, Hubner H, Braz JM, Seemann P, Avet C, Craik V, Weikert D, Schmidt MF, Webb CM, Tolmachova NA, Moroz YS, Huang XP, Kalyanaraman C, Gahbauer S, Chen G, Liu Z, Jacobson MP, Irwin JJ, Bouvier M, Du Y, Shoichet BK, Basbaum AI, Gmeiner P 10.1126/SCIENCE.ABN7065 2022-09-28
Gi/o αgust Human - 63 β1 Human γ2 Human Cryo-EM 7XP5 - 3.1 T2R46 TAS2R46 Taste 2 T2 (Taste 2) Human - Nanobody-35 Endoglucanase H Apo (no ligand)
none Apo (no ligand) - - 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 αo Human Mini-Go 61 β1 Human γ2 Human Cryo-EM 8E9X - 2.7 ACM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - CHEMBL73538 chembl_ligand pubchem
small-molecule Agonist acetylcholine small-molecule Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL 10.1038/S41586-022-05489-0 2022-11-30
Gq/11 αq Human - 59 β1 Human γ2 Human Cryo-EM 8EIT - 2.8 FFAR1 FFA1 Free fatty acid A (Rhodopsin) Human - scFv16 - docosahexaenoic acid pubchem gtoplig chembl_ligand drug_central drugbank pubchem
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
Gi/o αi1 Human - 63 β1 Rat γ2 Bovine Cryo-EM 8HK3 8HK3_refined 3.2 C3AR C3a Complement peptide A (Rhodopsin) Human - scFv16 - Apo (no ligand)
none Apo (no ligand) C5a, C3a 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
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8GHV 8GHV_refined 2.8 CNR1 CB1 Cannabinoid A (Rhodopsin) Human - scFv16 - CHEMBL4208628 chembl_ligand pubchem
small-molecule Agonist anandamide small-molecule Krishna Kumar K, Robertson MJ, Thadhani E, Wang H, Suomivuori CM, Powers AS, Ji L, Nikas SP, Dror RO, Inoue A, Makriyannis A, Skiniotis G, Kobilka B 10.1038/S41467-023-37864-4 2023-05-24
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8F2A - 2.2 CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - Pramlintide analogue 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
Gi/o αo Human - 60 β1 Human γ2 Human Cryo-EM 8HQC - 3.9 C5AR1 C5a1 Complement peptide A (Rhodopsin) Mouse - - fragment C5a gtoplig
peptide Agonist - - - - 2023-10-18
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8JII - 3.2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - scFv16 - nicotinic acid pubchem gtoplig chembl_ligand drugbank drug_central gtoplig pubchem
compound 9n [PMID: 18752940] pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Agonist
PAM 		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 - 58 β1 Human γ2 Human Cryo-EM 8KGK 8KGK_refined 3.2 GPR61 GPR61 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
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8W8B - 3.0 5HT1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL scFv16 - ulotaront pubchem gtoplig drugbank chembl_ligand
small-molecule Agonist 5-hydroxytryptamine 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 8FYL - 2.9 5HT1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - vilazodone pubchem gtoplig chembl_ligand drugbank drug_central
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 8GG0 - 2.9 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 8J23 8J23_refined 3.2 FFAR2 FFA2 Free fatty acid A (Rhodopsin) Human - scFv16 - Apo (no ligand)
none Apo (no ligand) propanoic acid, acetic acid, trans-2-methylcrotonic acid, butyric acid small-molecule - - 2024-04-17
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8JXX 8JXX_refined 3.1 HRH4 H4 Histamine A (Rhodopsin) Human - scFv16 - clobenpropit pubchem gtoplig chembl_ligand
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
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8WP1 - 3.2 SUCR1 succinate Succinate A (Rhodopsin) Human - - - cis-epoxysuccinic acid pubchem gtoplig chembl_ligand
small-molecule Agonist succinic acid small-molecule Liu A, Liu Y, Zhang W, Ye RD 10.1016/J.CELREP.2024.114381 2024-09-11
Gq/11 αq Human - 58 β1 Human γ2 Human Cryo-EM 8XJM 8XJM_refined 2.9 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 Li X, Zhang X, Wen X, Zhang D, Qu C, Miao X, Zhang W, Zhang R, Liu G, Xiao P, Sun JP, Gong W 10.1016/J.CELREP.2024.113893 2024-02-28
Gi/o αgust Human - 61 β1 Human γ2 Human Cryo-EM 8YKY - 3.0 T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human - scFv16 Exo-alpha-sialidase compound 28.1 [PMID: 36847646] pubchem gtoplig chembl_ligand
small-molecule Agonist - - - - 2024-07-10
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8ZSJ - 2.8 TAAR1 TA1 Trace amine A (Rhodopsin) Human BRIL Nanobody-35 - Apo (no ligand)
none Apo (no ligand) octopamine, β-phenylethylamine, CHEMBL1160703, tyramine, (+)-Octopamine, 3-iodothyronamine, dopamine small-molecule Jiang K, Zheng Y, Zeng L, Wang L, Li F, Pu J, Lu Y, Zhao S, Xu F 10.1016/J.CELREP.2024.114505 2024-07-24
Gi/o αgust Human - 64 β1 Human γ2 Human Cryo-EM 9IIX - 2.9 T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human - - - compound 28.1 [PMID: 36847646] pubchem gtoplig chembl_ligand
compound 28.1 [PMID: 36847646] pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Agonist
Allosteric agonist 		- - - - 2024-07-24
Gi/o αi1 Human - 100 β1 Human γ2 Human Cryo-EM 6OT0 - 3.9 SMO SMO Frizzled F (Frizzled) Human - Fab light chain
Fab heavy chain 		- 24,25-Epoxy-cholesterol pubchem
small-molecule Agonist - - Qi X, Liu H, Thompson B, McDonald J, Zhang C, Li X 10.1038/S41586-019-1286-0 2019-06-12
Gs αs Human - 49 β1 Human γ2 Human Cryo-EM 6P9Y - 3.0 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 Liang YL, Belousoff MJ, Zhao P, Koole C, Fletcher MM, Truong TT, Julita V, Christopoulos G, Xu HE, Zhang Y, Khoshouei M, Christopoulos A, Danev R, Sexton PM, Wootten D 10.1016/J.MOLCEL.2020.01.012 2020-02-05
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 6XBJ - 3.9 SMO SMO Frizzled F (Frizzled) Human - scFv16 - Cholesterol pubchem
small-molecule Agonist - - Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X 10.1038/S41589-020-0646-2 2020-09-30
Gs αs Human - 56 β1 Human γ2 Human Cryo-EM 6XOX - 3.1 GLP1R GLP-1 Glucagon B1 (Secretin) Human - scFv16
Nanobody-35 		- orforglipron pubchem gtoplig chembl_ligand
small-molecule Agonist glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide peptide Kawai T, Sun B, Yoshino H, Feng D, Suzuki Y, Fukazawa M, Nagao S, Wainscott DB, Showalter AD, Droz BA, Kobilka TS, Coghlan MP, Willard FS, Kawabe Y, Kobilka BK, Sloop KW 10.1073/PNAS.2014879117 2020-11-18
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7CKX - 3.5 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - A77636 pubchem gtoplig chembl_ligand
small-molecule Agonist L-NOREPINEPHRINE, noradrenaline, (-)-noradrenaline, 5-hydroxytryptamine, dopamine small-molecule - - 2021-03-03
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7F1S 7F1S_refined 2.8 CCR5 CCR5 Chemokine A (Rhodopsin) Human - - - Apo (no ligand)
none Apo (no ligand) CCL11, CCL14, CCL2, CCL8, CCL5, CCL16, CCL4, CCL13, CCL7, CCL3 peptide Zhang H, Chen K, Tan Q, Shao Q, Han S, Zhang C, Yi C, Chu X, Zhu Y, Xu Y, Zhao Q, Wu B 10.1038/S41467-021-24438-5 2021-07-14
Gq/11 αq Human Gq-Gs chimera 57 β1 Human γ2 Human Cryo-EM 7S8N 7S8N_refined 2.9 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human - scFv16 - (R)-ZINC-3573 pubchem gtoplig chembl_ligand
small-molecule Agonist PAMP-20 peptide 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
Gq/11 α11 Human - 97 β1 Human γ2 Human Cryo-EM 7RKF - 4.0 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
Gs αs Human Mini-Gs 60 β1 Rat γ2 Bovine Cryo-EM 7VAB 7VAB_refined 3.2 GIPR GIP Glucagon B1 (Secretin) Human - Nanobody-35 - tirzepatide pubchem gtoplig
peptide Agonist gastric inhibitory polypeptide 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
Gs αs Human Mini-Gs 54 β1 Human γ2 Human Cryo-EM 7WU3 - 3.1 AGRF1 ADGRF1 ADGRF B2 (Adhesion) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Qu X, Qiu N, Wang M, Zhang B, Du J, Zhong Z, Xu W, Chu X, Ma L, Yi C, Han S, Shui W, Zhao Q, Wu B 10.1038/S41586-022-04580-W 2022-04-27
Gs αs Bovine - 60 β1 Rat γ2 Bovine Cryo-EM 7WBJ - 3.4 VIPR2 VPAC2 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - PACAP-27 pubchem gtoplig pubchem
peptide Agonist GHRH, VIP, PACAP-27, PHI, secretin, PACAP-38 peptide Xu Y, Feng W, Zhou Q, Liang A, Li J, Dai A, Zhao F, Yan J, Chen CW, Li H, Zhao LH, Xia T, Jiang Y, Xu HE, Yang D, Wang MW 10.1038/S41467-022-30041-Z 2022-05-18
Gs αs Human - 59 β1 Rat γ2 Human Cryo-EM 7X8R - 2.6 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - CHEMBL2158411 chembl_ligand pubchem
small-molecule Agonist glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide peptide Cong Z, Zhou Q, Li Y, Chen LN, Zhang ZC, Liang A, Liu Q, Wu X, Dai A, Xia T, Wu W, Zhang Y, Yang D, Wang MW 10.1073/PNAS.2200155119 2022-06-29
Gq/11 αq Human Gs-mini-Gq chimera 57 β1 Human γ2 Human Cryo-EM 8DWC - 2.9 MRGX1 MRGPRX1 A orphans A (Rhodopsin) Human - scFv16 - Proenkephalin-A
peptide 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
Gi/o αi2 Human - 58 β1 Bovine γ2 Bovine Cryo-EM 7YJ4 - 3.2 RL3R2 RXFP4 Relaxin family peptide A (Rhodopsin) Human - scFv16 - Insulin-like peptide INSL5 A chain pubchem
Insulin-like peptide INSL5 B chain pubchem
peptide
peptide 		Agonist relaxin-3, relaxin-3 (B chain), INSL5 peptide Chen Y, Zhou Q, Wang J, Xu Y, Wang Y, Yan J, Wang Y, Zhu Q, Zhao F, Li C, Chen CW, Cai X, Bathgate RAD, Shen C, Eric Xu H, Yang D, Liu H, Wang MW 10.1038/S41467-023-36182-Z 2023-03-01
Gs αs Human Mini-Gs 61 β1 Human γ2 Human Cryo-EM 8HIX - 3.1 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 2023-03-15
Gs αs Human Gs fused to receptor 57 β1 Human γ2 Human Cryo-EM 7TMW - 3.2 RXFP1 RXFP1 Relaxin family peptide A (Rhodopsin) Human - Nanobody-35 - H2 relaxin pubchem
small-molecule Agonist relaxin, relaxin-3, relaxin-1 peptide - - 2023-02-15
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 8HJ5 8HJ5_refined 3.0 MRGX1 MRGPRX1 A orphans A (Rhodopsin) Human BRIL scFv16
Nanobody-35 		- compound 16 [PMID: 31498617] pubchem gtoplig chembl_ligand
small-molecule Agonist bovine adrenal medulla peptide 8-22 peptide - - 2023-05-31
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7TRK - 2.8 ACM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - iperoxo pubchem gtoplig chembl_ligand
small-molecule Agonist acetylcholine small-molecule - - 2023-05-17
Gs αs Human - 57 β1 Rat γ2 Bovine Cryo-EM 7Y35 - 2.9 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - abaloparatide pubchem
small-molecule Agonist PTHrP-(1-36), PTHrP, PTH, TIP39 peptide - - 2023-07-05
Gi/o αi1 Human - 62 β1 Rat γ2 Bovine Cryo-EM 8IY5 - 2.8 EDNRB ETB Endothelin A (Rhodopsin) Human - scFv16 - ENDOTHELIN chembl_ligand pubchem
protein Agonist endothelin-2, endothelin-3, endothelin-1 peptide Sano FK, Akasaka H, Shihoya W, Nureki O 10.7554/ELIFE.85821 2023-08-16
Gi/o αi1 Human - 62 β1 Mouse γ2 Mouse Cryo-EM 8IHJ 8IHJ_refined 3.1 HCAR3 HCA3 Hydroxycarboxylic acid A (Rhodopsin) Human BRIL scFv16 - (5S)-5-methyl-4-oxo-5-phenylfuran-2-carboxylic acid pubchem
small-molecule Agonist 3-hydroxyoctanoic acid small-molecule Suzuki S, Tanaka K, Nishikawa K, Suzuki H, Oshima A, Fujiyoshi Y 10.1038/S41467-023-41650-7 2023-08-30
Gs αs Human - 58 β1 Rat γ2 Bovine Cryo-EM 8JIT - 2.9 GLR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - MEDI0382
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 2023-09-06
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8WC5 - 3.3 TAAR1 TA1 Trace amine A (Rhodopsin) Mouse - scFv16 - Tetramethylammonium 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
Gi/o αi1 Human - 66 β1 Human γ2 Human Cryo-EM 8FYX - 2.6 5HT1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - buspirone pubchem gtoplig chembl_ligand drugbank drug_central
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 8GG1 - 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 - 60 β1 Human γ2 Human Cryo-EM 8JGF 8JGF_refined 2.7 MRGX1 MRGPRX1 A orphans A (Rhodopsin) Human - scFv16 - bovine adrenal medulla peptide 8-22 pubchem gtoplig chembl_ligand pubchem
peptide Agonist bovine adrenal medulla peptide 8-22 peptide Guo L, Zhang Y, Fang G, Tie L, Zhuang Y, Xue C, Liu Q, Zhang M, Zhu K, You C, Xu P, Yuan Q, Zhang C, Liu L, Rong N, Peng S, Liu Y, Wang C, Luo X, Lv Z, Kang D, Yu X, Zhang C, Jiang Y, Dong X, Zhou J, Liu Z, Yang F, Eric Xu H, Sun JP 10.1038/S41467-023-40705-Z 2024-01-10
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8PKM - 2.9 5HT1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human - - - BEFIRADOL chembl_ligand 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 - 60 β1 Human γ2 Human Cryo-EM 8UHB 8UHB_refined 3.4 TAAR1 TA1 Trace amine A (Rhodopsin) Human BRIL Nanobody-35 - CHEMBL3684869 chembl_ligand pubchem
small-molecule Agonist octopamine, β-phenylethylamine, CHEMBL1160703, tyramine, (+)-Octopamine, 3-iodothyronamine, dopamine small-molecule Zilberg G, Parpounas AK, Warren AL, Yang S, Wacker D 10.1038/S41467-023-44601-4 2024-01-10
Gq/11 αq Human Gi2-mini-Gq chimera 57 β1 Human γ2 Human Cryo-EM 8V6U - 3.0 5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - 4-{(3R)-1-[(1R)-1-(pyrimidin-2-yl)ethyl]piperidin-3-yl}phenol pubchem
small-molecule Agonist 5-hydroxytryptamine, tryptamine small-molecule Lyu J, Kapolka N, Gumpper R, Alon A, Wang L, Jain MK, Barros-Alvarez X, Sakamoto K, Kim Y, DiBerto J, Kim K, Glenn IS, Tummino TA, Huang S, Irwin JJ, Tarkhanova OO, Moroz Y, Skiniotis G, Kruse AC, Shoichet BK, Roth BL 10.1126/SCIENCE.ADN6354 2024-05-29
Gi/o αi1 Human - 62 β1 Rat γ2 Bovine Cryo-EM 8XBE 8XBE_refined 3.4 GPR34 GPR34 A orphans A (Rhodopsin) Human - scFv16 - CHEMBL4782438 chembl_ligand pubchem
small-molecule Agonist lysophosphatidylserine small-molecule Izume T, Kawahara R, Uwamizu A, Chen L, Yaginuma S, Omi J, Kawana H, Hou F, Sano FK, Tanaka T, Kobayashi K, Okamoto HH, Kise Y, Ohwada T, Aoki J, Shihoya W, Nureki O 10.1038/S41467-024-45046-Z 2024-05-15
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8XVE 8XVE_refined 3.0 EDNRB ETB Endothelin A (Rhodopsin) Human - Nanobody-35 Exo-alpha-sialidase BQ3020
peptide Agonist endothelin-2, endothelin-3, endothelin-1 peptide Hou J, Liu S, Zhang X, Tu G, Wu L, Zhang Y, Yang H, Li X, Liu J, Jiang L, Tan Q, Bai F, Liu Z, Miao C, Hua T, Luo Z 10.1038/S41421-024-00705-9 2024-08-28
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8ZSP - 3.1 TAAR1 TA1 Trace amine A (Rhodopsin) Human BRIL Nanobody-35 - Lysergide pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist octopamine, β-phenylethylamine, CHEMBL1160703, tyramine, (+)-Octopamine, 3-iodothyronamine, dopamine small-molecule Jiang K, Zheng Y, Zeng L, Wang L, Li F, Pu J, Lu Y, Zhao S, Xu F 10.1016/J.CELREP.2024.114505 2024-07-24
Gs αs Human - 57 β1 Rat γ2 Bovine Cryo-EM 9IJE 9IJE_refined 2.3 ADRB3 β3 Adrenoceptors A (Rhodopsin) Human - scFv16
Camelid antibody VHH fragment 		- (-)-adrenaline pubchem gtoplig chembl_ligand drugbank drug_central pubchem
small-molecule Agonist (-)-noradrenaline, (-)-adrenaline, (±)-adrenaline, (+)-adrenaline small-molecule - - 2024-08-21
Gs αs Human - 48 β1 Human γ2 Human Cryo-EM 6UUS 6UUS_refined 2.4 CALRL calcitonin-like Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP3 		- 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 2020-04-01
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 6XBK - 3.2 SMO SMO Frizzled F (Frizzled) Human - scFv16 - Cholesterol pubchem
small-molecule Agonist - - - - 2020-09-30
Gs αs Human - 62 β1 Human γ2 Human Cryo-EM 7LCI 7LCI_refined 2.9 GLP1R GLP-1 Glucagon B1 (Secretin) Human - - - 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, Johnson RM, Drulyte I, Yu L, Kotecha A, Danev R, Wootten D, Sexton PM, Belousoff MJ 10.1016/J.STR.2021.04.008 2021-01-20
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7E2Y - 3.0 5HT1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human - - - 5-hydroxytryptamine pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist 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 Human γ2 Human Cryo-EM 7JHJ - 3.2 Q3KSP2 BILF1 Unclassified A (Rhodopsin) strain GD1 - scFv16 - Apo (no ligand)
none Apo (no ligand) - - Tsutsumi N, Qu Q, Mavri M, Baggesen MS, Maeda S, Waghray D, Berg C, Kobilka BK, Rosenkilde MM, Skiniotis G, Garcia KC 10.1016/J.IMMUNI.2021.06.001 2021-07-07
Gq/11 αq Human Gq-Gi1 chimera 61 β1 Rat γ2 Bovine Cryo-EM 7EIB - 3.0 BKRB1 B1 Bradykinin A (Rhodopsin) Human - - - [des-Arg10]kallidin pubchem gtoplig chembl_ligand 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 - 61 β1 Human γ2 Human Cryo-EM 7VDM 7VDM_refined 3.0 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human - scFv16 - substance P pubchem gtoplig chembl_ligand gtoplig gtoplig
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 7F4D - 3.0 MSHR MC1 Melanocortin A (Rhodopsin) Human - Nanobody-35 - INTERMEDINE chembl_ligand pubchem pubchem pubchem
protein Agonist γ-MSH, β-MSH, α-MSH, ACTH peptide - - 2021-09-08
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7TYY - 3.0 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 2022-03-23
Gq/11 αq Human - 54 β1 Human γ2 Human Cryo-EM 7W53 - 3.2 NMUR1 NMU1 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 - - 2022-04-20
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7XT9 - 3.2 5HT4R 5-HT4 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - 5-hydroxytryptamine pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist 5-hydroxytryptamine small-molecule Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE 10.1016/J.MOLCEL.2022.05.031 2022-07-27
Gs αs Bovine - 51 β1 Bovine γ2 Bovine Cryo-EM 8DCR - 2.6 ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey T4-Lysozyme Nanobody-35 - Dobutamine 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
Gi/o αo Human - 58 β1 Human γ2 Human Cryo-EM 7W6P - 3.5 ADA2A α2A Adrenoceptors A (Rhodopsin) Human - scFv16 - N-pyridin-4-ylisoquinolin-4-amine pubchem
small-molecule Agonist (-)-noradrenaline, (-)-adrenaline small-molecule Fink EA, Xu J, Hubner H, Braz JM, Seemann P, Avet C, Craik V, Weikert D, Schmidt MF, Webb CM, Tolmachova NA, Moroz YS, Huang XP, Kalyanaraman C, Gahbauer S, Chen G, Liu Z, Jacobson MP, Irwin JJ, Bouvier M, Du Y, Shoichet BK, Basbaum AI, Gmeiner P 10.1126/SCIENCE.ABN7065 2022-09-28
Gi/o αgust Human - 63 β1 Human γ2 Human Cryo-EM 7XP4 - 3.0 T2R46 TAS2R46 Taste 2 T2 (Taste 2) Human - Nanobody-35 Endoglucanase H Apo (no ligand)
none Apo (no ligand) - - 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
Gq/11 αq Human Mini-Gq 57 β1 Human γ2 Human Cryo-EM 8E9Z - 2.7 ACM3 M3 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - iperoxo pubchem gtoplig chembl_ligand
small-molecule Agonist acetylcholine small-molecule Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL 10.1038/S41586-022-05489-0 2022-11-30
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8GY7 - 3.3 ACTHR MC2 Melanocortin A (Rhodopsin) Human BRIL - MRAP1 ACTH pubchem gtoplig chembl_ligand drugbank drug_central pubchem
peptide Agonist ACTH peptide Luo P, Feng W, Ma S, Dai A, Wu K, Chen X, Yuan Q, Cai X, Yang D, Wang MW, Eric Xu H, Jiang Y 10.1038/S41422-022-00751-6 2023-01-11
Gs αs Human - 54 β1 Human γ2 Human Cryo-EM 8FU6 8FU6_refined 2.9 GLR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - Glucagon derivative ZP3780
peptide Agonist glucagon peptide Krishna Kumar K, O'Brien ES, Habrian CH, Latorraca NR, Wang H, Tuneew I, Montabana E, Marqusee S, Hilger D, Isacoff EY, Mathiesen JM, Kobilka BK 10.1016/J.CELL.2023.02.028 2023-04-12
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8GUT 8GUT_refined 3.0 CNR2 CB2 Cannabinoid A (Rhodopsin) Human - scFv16 - 1-[[4-[5-Fluoro-6-[(oxan-4-ylamino)methyl]pyridin-2-yl]phenyl]methyl]-3-(2-methylpropyl)imidazolidine-2,4-dione pubchem
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
Gs αs Human - 57 β1 Rat γ2 Bovine Cryo-EM 7Y36 - 2.8 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - Parathyroid hormone pubchem
peptide Agonist PTHrP-(1-36), PTHrP, PTH, TIP39 peptide - - 2023-07-05
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 8IZB - 3.1 GP174 GPR174 A orphans A (Rhodopsin) Human - Nanobody-35 - L-serine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
LYSOPHOSPHATIDIC ACID chembl_ligand pubchem
small-molecule
small-molecule 		Agonist lysophosphatidylserine small-molecule Liu G, Li X, Wang Y, Zhang X, Gong W 10.1371/JOURNAL.PBIO.3002387 2023-11-01
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 8W8A - 2.8 TAAR1 TA1 Trace amine A (Rhodopsin) Human - Nanobody-35 - CHEMBL3684869 chembl_ligand pubchem
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 - 62 β1 Human γ2 Human Cryo-EM 8GAG 8GAG_refined 3.3 CNR1 CB1 Cannabinoid A (Rhodopsin) Human - scFv16 - methyl (2R)-2-({(1M)-5-methyl-1-[3-(trifluoromethyl)phenyl]-1H-pyrazole-3-carbonyl}amino)-2-(thiophen-2-yl)propanoate pubchem
small-molecule Agonist anandamide small-molecule - - 2024-02-28
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8GFW - 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
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 8J21 8J21_refined 3.3 FFAR3 FFA3 Free fatty acid A (Rhodopsin) Human - scFv16 - butyric acid pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist propanoic 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
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8JT6 - 3.0 5HT1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL scFv16 - 1-(4-fluorophenyl)-4-[(7R)-2,5,11-triazatetracyclo[7.6.1.0^2,7.0^12,16]hexadeca-1(15),9,12(16),13-tetraen-5-yl]butan-1-one pubchem
small-molecule Agonist 5-hydroxytryptamine small-molecule Chen Z, Yu J, Wang H, Xu P, Fan L, Sun F, Huang S, Zhang P, Huang H, Gu S, Zhang B, Zhou Y, Wan X, Pei G, Xu HE, Cheng J, Wang S 10.1016/J.CELL.2024.02.034 2024-02-28
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8X8L 8X8L_refined 2.7 SSR5 SST5 Somatostatin A (Rhodopsin) Human - scFv16 - Cortistatin
peptide Agonist cortistatin-14, SRIF-14, CST-17, SRIF-28 peptide - - 2024-06-12
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8YUV - 3.0 HRH3 H3 Histamine A (Rhodopsin) Human - - - immepip pubchem gtoplig chembl_ligand
small-molecule Agonist histamine small-molecule - - 2024-06-05
Gi/o αi1 Human - 60 β1 Bovine γ2 Bovine Cryo-EM 9CBM - 3.2 ADA2A α2A Adrenoceptors A (Rhodopsin) Human T4-Lysozyme - - dexmedetomidine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist (-)-noradrenaline, (-)-adrenaline small-molecule Lou JS, Su M, Wang J, Do HN, Miao Y, Huang XY 10.1038/S12276-024-01296-X 2024-09-11
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 8YN5 - 2.7 HRH3 H3 Histamine A (Rhodopsin) Human - scFv16 - 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
Gi/o αi2 Human - 59 β1 Human γ2 Human Cryo-EM 6D9H 6D9H_refined 3.6 AA1R A1 Adenosine A (Rhodopsin) Human - - - adenosine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist adenosine small-molecule Draper-Joyce CJ, Khoshouei M, Thal DM, Liang YL, Nguyen ATN, Furness SGB, Venugopal H, Baltos JA, Plitzko JM, Danev R, Baumeister W, May LT, Wootten D, Sexton PM, Glukhova A, Christopoulos A 10.1038/S41586-018-0236-6 2018-06-20
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7JVP - 2.9 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - 39YLC3L0ZU pubchem
small-molecule Agonist L-NOREPINEPHRINE, noradrenaline, (-)-noradrenaline, 5-hydroxytryptamine, 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
Gq/11 αq Human Gq-Gs-Gi1 chimera 55 β1 Rat γ2 Human Cryo-EM 7MBY - 2.4 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 Mobbs JI, Belousoff MJ, Harikumar KG, Piper SJ, Xu X, Furness SGB, Venugopal H, Christopoulos A, Danev R, Wootten D, Thal DM, Miller LJ, Sexton PM 10.1371/JOURNAL.PBIO.3001295 2021-05-26
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7EW4 7EW4_refined 3.2 S1PR3 S1P3 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - CYM-5541 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 7VDL - 3.2 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human - scFv16 - Cortistatin 14 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 - 50 β1 Human γ2 Human Cryo-EM 7LLY 7LLY_refined 3.3 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Pro-glucagon 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 Human - 62 β1 Rat γ2 Bovine Cryo-EM 7VGY - 3.1 MTR1A MT1 Melatonin A (Rhodopsin) Human - scFv16 - 2-iodo-melatonin pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist melatonin small-molecule Wang Q, Lu Q, Guo Q, Teng M, Gong Q, Li X, Du Y, Liu Z, Tao Y 10.1038/S41467-022-28111-3 2022-03-02
Gi/o αo Human - 61 β1 Human γ2 Human Cryo-EM 7EJ8 - 3.0 ADA2A α2A Adrenoceptors A (Rhodopsin) Human - scFv16 - brimonidine (UK14304) pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
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
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7U2L - 3.2 OPRM μ Opioid A (Rhodopsin) Mouse - scFv16 - N-(5-carbamimidamidopentyl)-N-[1-(2-phenylethyl)piperidin-4-yl]propanamide
small-molecule Agonist - - Faouzi A, Wang H, Zaidi SA, DiBerto JF, Che T, Qu Q, Robertson MJ, Madasu MK, El Daibani A, Varga BR, Zhang T, Ruiz C, Liu S, Xu J, Appourchaux K, Slocum ST, Eans SO, Cameron MD, Al-Hasani R, Pan YX, Roth BL, McLaughlin JP, Skiniotis G, Katritch V, Kobilka BK, Majumdar S 10.1038/S41586-022-05588-Y 2022-05-04
Gs αs Human - 59 β1 Rat γ2 Bovine Cryo-EM 7XJI - 3.9 ADRB3 β3 Adrenoceptors A (Rhodopsin) Dog - Nanobody-35 - 3-[3-[2-[[(2~{S})-2-(3-chlorophenyl)-2-oxidanyl-ethyl]amino]ethylamino]phenyl]benzoic acid pubchem
small-molecule Agonist - - Nureki I, Kobayashi K, Tanaka T, Demura K, Inoue A, Shihoya W, Nureki O 10.1016/J.BBRC.2022.04.065 2022-05-04
Gq/11 αq Human - 58 β1 Human γ2 Human Cryo-EM 7XJK 7XJK_refined 3.3 GALR2 GAL2 Galanin A (Rhodopsin) Human - scFv16 - Galanin, Human pubchem
peptide Agonist spexin-1, galanin-like peptide, galanin peptide Jiang W, Zheng S 10.1073/PNAS.2121465119 2022-06-29
Gq/11 αq Human Gi2-mini-Gq chimera 58 β1 Human γ2 Human Cryo-EM 7SRR - 2.9 5HT2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - Lysergide pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist 5-hydroxytryptamine small-molecule Cao C, Barros-Alvarez X, Zhang S, Kim K, Damgen MA, Panova O, Suomivuori CM, Fay JF, Zhong X, Krumm BE, Gumpper RH, Seven AB, Robertson MJ, Krogan NJ, Huttenhain R, Nichols DE, Dror RO, Skiniotis G, Roth BL 10.1016/J.NEURON.2022.08.006 2022-09-21
G12/13 α13 Human - 55 β1 Human γ2 Human Cryo-EM 7WY0 - 2.8 AGRF1 ADGRF1 ADGRF B2 (Adhesion) Human - scFv16 - 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 7YU7 - 3.8 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 - 63 β1 Rat γ2 Bovine Cryo-EM 8F7R - 3.3 OPRM μ Opioid A (Rhodopsin) Human - scFv16 - endomorphin-1 pubchem gtoplig chembl_ligand
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
Gs αs Human Mini-Gs 61 β1 Human γ2 Human Cryo-EM 8HJ0 - 3.1 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 2023-03-15
Gi/o αo Human - 61 β1 Human γ2 Human Cryo-EM 7XJJ 7XJJ_refined 3.3 GALR1 GAL1 Galanin A (Rhodopsin) Human - scFv16 - galanin pubchem gtoplig chembl_ligand gtoplig pubchem pubchem pubchem pubchem
peptide Agonist galanin-like peptide, galanin peptide - - 2023-05-03
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8ITF - 3.5 TAAR9 TAAR9 A orphans A (Rhodopsin) Mouse - scFv16
Nanobody-35 		- N,N-Dimethylcyclohexylamine 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
G12/13 α13 Human Gi2-mini-G13 chimera 57 β1 Human γ2 Human Cryo-EM 7YDH - 3.1 AGRE5 ADGRE5 ADGRE B2 (Adhesion) Human - scFv16 - 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 - 56 β1 Human γ2 Human Cryo-EM 8H0Q - 3.3 GRPR BB2 Bombesin A (Rhodopsin) Human - - - Gastrin-releasing peptide pubchem
peptide Agonist neuromedin B, gastrin releasing peptide(14-27) (human), GRP-(18-27), neuromedin C, gastrin-releasing peptide peptide Li C, Xu Y, Liu H, Cai H, Jiang Y, Xu HE, Yin W 10.1038/S41422-022-00743-6 2023-08-09
Gi/o αi3 Human - 63 β1 Human γ2 Human Cryo-EM 8JD6 - 3.4 GRM4 mGlu4 Metabotropic glutamate C (Glutamate) Human - scFv16 - VU0364770 pubchem gtoplig chembl_ligand
small-molecule Agonist L-glutamic acid, L-serine-O-phosphate 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 - 62 β1 Mouse γ2 Mouse Cryo-EM 8IHI - 3.1 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human BRIL scFv16 - (5S)-5-methyl-4-oxo-5-phenylfuran-2-carboxylic acid pubchem
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 2023-08-30
Gs αs Human - 56 β1 Rat γ2 Bovine Cryo-EM 8JIQ 8JIQ_refined 3.4 GLR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - Dual-agonist peptide P15
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
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8GEC 8GEC_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
Gs αs Human - 51 β1 Human γ2 Human Cryo-EM 8IQ4 8IQ4_refined 2.7 PF2R FP Prostanoid A (Rhodopsin) Human - Nanobody-35 - Carboprost pubchem
small-molecule Agonist PGF2α, PGI2, PGD2, thromboxane A2, PGE2 small-molecule Lv X, Gao K, Nie J, Zhang X, Zhang S, Ren Y, Sun X, Li Q, Huang J, Liu L, Zhang X, Zhang W, Liu X 10.1038/S41467-023-43922-8 2024-01-31
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8JPN - 2.9 SUCR1 succinate Succinate A (Rhodopsin) Human BRIL scFv16 - cis-epoxysuccinic acid pubchem gtoplig chembl_ligand
small-molecule Agonist succinic acid small-molecule Wang T, Tang W, Zhu X, Lv Z, Chen J, Li Y, Sun X, Lv H, Gu Q, Li F, Wang J 10.1038/S41422-024-00968-7 2024-05-22
Gs αs Human GTP bound, Class S 91 β1 Human γ2 Human Cryo-EM 8UO3 8UO3_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
Gi/o αi1 Human - 61 β1 Rat γ2 Bovine Cryo-EM 8X17 8X17_refined 3.2 AA3R A3 Adenosine A (Rhodopsin) Human - scFv16 - Cl-IB-MECA pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist adenosine small-molecule - - 2024-04-24
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8XQN - 3.1 T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human - scFv16 Exo-alpha-sialidase aristolochic acid pubchem gtoplig chembl_ligand
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 - 60 β1 Rat γ2 Mouse Cryo-EM 8ZBE 8ZBE_refined 3.2 SSR5 SST5 Somatostatin A (Rhodopsin) Human - scFv16 LgBiT Octreotide
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 - 60 β1 Human γ2 Human Cryo-EM 9CBL - 2.8 ADA2A α2A Adrenoceptors A (Rhodopsin) Human T4-Lysozyme - - (-)-adrenaline pubchem gtoplig chembl_ligand drugbank drug_central pubchem
small-molecule Agonist (-)-noradrenaline, (-)-adrenaline small-molecule Lou JS, Su M, Wang J, Do HN, Miao Y, Huang XY 10.1038/S12276-024-01296-X 2024-09-11
Gi/o αi1 Human - 66 β1 Human γ2 Human Cryo-EM 8K3Z - 2.8 CXCR4 CXCR4 Chemokine A (Rhodopsin) Human - scFv16 - Stromal cell-derived factor 1
peptide Agonist CXCL12α, CXCL12, CXCL12γ, CXCL12φ, CXCL12β, CXCL12δ, CXCL12ε peptide - - 2024-07-17
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 9EW2 - 3.2 FZD7 FZD7 Frizzled F (Frizzled) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - - - 2024-10-02
Gi/o αgust Bovine Only H5 3 - - - - X-ray 5EN0 5EN0_refined 2.8 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - Retinal (all-trans) pubchem
small-molecule Agonist - - Singhal A, Guo Y, Matkovic M, Schertler G, Deupi X, Yan EC, Standfuss J 10.15252/EMBR.201642671 2016-08-10
Gi/o αo Human - 61 β1 Human γ2 Human Cryo-EM 6OIK 6OIK_refined 3.6 ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human - - - LY2119620 pubchem gtoplig chembl_ligand
iperoxo pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Ago-PAM
Agonist 		acetylcholine small-molecule Maeda S, Qu Q, Robertson MJ, Skiniotis G, Kobilka BK 10.1126/SCIENCE.AAW5188 2019-05-08
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 6NI3 6NI3_refined 3.8 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - Nanobody-35 - CHEMBL1615159 chembl_ligand pubchem
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule Nguyen AH, Thomsen ARB, Cahill TJ 3rd, Huang R, Huang LY, Marcink T, Clarke OB, Heissel S, Masoudi A, Ben-Hail D, Samaan F, Dandey VP, Tan YZ, Hong C, Mahoney JP, Triest S, Little J 4th, Chen X, Sunahara R, Steyaert J, Molina H, Yu Z, des Georges A, Lefkowitz RJ 10.1038/S41594-019-0330-Y 2019-11-20
Gs αs Human - 50 β1 Bovine γ2 Bovine Cryo-EM 7BZ2 7BZ2_refined 3.8 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - Nanobody-35 - ARFORMOTEROL chembl_ligand chembl_ligand chembl_ligand chembl_ligand pubchem
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule Zhang Y, Yang F, Ling S, Lv P, Zhou Y, Fang W, Sun W, Zhang L, Shi P, Tian C 10.1038/S41421-020-0176-9 2020-08-05
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7CMV - 2.7 DRD3 D3 Dopamine A (Rhodopsin) Human BRIL scFv16 - CHEMBL70565 chembl_ligand chembl_ligand pubchem
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 αi1 Human - 62 β1 Bovine γ2 Bovine Cryo-EM 7O7F 7O7F_refined 3.2 CCR5 CCR5 Chemokine A (Rhodopsin) Human - Fab heavy chain
Fab light chain 		- CCL5 gtoplig
peptide Agonist CCL11, CCL14, CCL2, CCL8, CCL5, CCL16, CCL4, CCL13, CCL7, CCL3 peptide Isaikina P, Tsai CJ, Dietz N, Pamula F, Grahl A, Goldie KN, Guixa-Gonzalez R, Branco C, Paolini-Bertrand M, Calo N, Cerini F, Schertler GFX, Hartley O, Stahlberg H, Maier T, Deupi X, Grzesiek S 10.1126/SCIADV.ABG8685 2021-06-30
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7F58 7F58_refined 3.1 MC4R MC4 Melanocortin A (Rhodopsin) Human - Nanobody-35 - THIQ pubchem gtoplig chembl_ligand
small-molecule Agonist γ-MSH, agouti-related protein, β-MSH, α-MSH, ACTH peptide Zhang H, Chen LN, Yang D, Mao C, Shen Q, Feng W, Shen DD, Dai A, Xie S, Zhou Y, Qin J, Sun JP, Scharf DH, Hou T, Zhou T, Wang MW, Zhang Y 10.1038/S41422-021-00552-3 2021-11-03
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7VUJ 7VUJ_refined 3.8 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
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7F4H - 2.7 MSHR MC1 Melanocortin A (Rhodopsin) Human - Nanobody-35
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 - 59 β1 Human γ2 Human Cryo-EM 7TYX - 2.6 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 2022-03-30
Gq/11 αq Human - 59 β1 Human γ2 Human Cryo-EM 7W56 - 2.9 NMUR1 NMU1 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
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7W0O 7W0O_refined 3.8 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
Gq/11 αq Human - 57 β1 Bovine γ2 Bovine Cryo-EM 7X1U 7X1U_refined 3.2 TRFR TRH1 Thyrotropin-releasing hormone A (Rhodopsin) Human - scFv16 - TRH pubchem
peptide Agonist TRH peptide Yang F, Zhang H, Meng X, Li Y, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C 10.1038/S41422-022-00646-6 2022-08-31
Gs αs Human - 58 β1 Rat γ2 Bovine Cryo-EM 7VVM 7VVM_refined 3.2 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - Parathyroid hormone
peptide Agonist PTHrP-(1-36), PTHrP, PTH, TIP39 peptide Kobayashi K, Kawakami K, Kusakizako T, Miyauchi H, Tomita A, Kobayashi K, Shihoya W, Yamashita K, Nishizawa T, Kato HE, Inoue A, Nureki O 10.1016/J.MOLCEL.2022.07.003 2022-08-03
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7U2K - 3.3 OPRM μ Opioid A (Rhodopsin) Mouse - - - CHEMBL147044 chembl_ligand pubchem
small-molecule Agonist - - Faouzi A, Wang H, Zaidi SA, DiBerto JF, Che T, Qu Q, Robertson MJ, Madasu MK, El Daibani A, Varga BR, Zhang T, Ruiz C, Liu S, Xu J, Appourchaux K, Slocum ST, Eans SO, Cameron MD, Al-Hasani R, Pan YX, Roth BL, McLaughlin JP, Skiniotis G, Katritch V, Kobilka BK, Majumdar S 10.1038/S41586-022-05588-Y 2022-12-07
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 7X5H 7X5H_refined 3.1 5HT5A 5-HT5A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL scFv16 - 5-CT pubchem gtoplig chembl_ligand
small-molecule Agonist 5-hydroxytryptamine small-molecule Tan Y, Xu P, Huang S, Yang G, Zhou F, He X, Ma H, Xu HE, Jiang Y 10.1038/S41421-022-00412-3 2022-09-14
Gi/o αi1 Human - 64 β1 Rat γ2 Bovine Cryo-EM 8F7W 8F7W_refined 3.2 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 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 - 64 β1 Human γ2 Human Cryo-EM 7Y65 - 3.2 C5AR1 C5a1 Complement peptide A (Rhodopsin) Human - scFv16 - C5a
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 - 62 β1 Human γ2 Human Cryo-EM 8HS3 - 3.1 GPR20 GPR20 A orphans A (Rhodopsin) Human BRIL scFv16 - Apo (no ligand)
none Apo (no ligand) - - Lin X, Jiang S, Wu Y, Wei X, Han GW, Wu L, Liu J, Chen B, Zhang Z, Zhao S, Cherezov V, Xu F 10.1038/S41421-023-00520-8 2023-03-08
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8GUS - 3.0 CNR2 CB2 Cannabinoid A (Rhodopsin) Human - scFv16 - CHEMBL2179724 chembl_ligand pubchem
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
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7YAC 7YAC_refined 3.2 SSR2 SST2 Somatostatin A (Rhodopsin) Human - scFv16 - PALTUSOTINE chembl_ligand pubchem
small-molecule Agonist cortistatin-14, SRIF-14, CST-17, SRIF-28 peptide Zhao J, Fu H, Yu J, Hong W, Tian X, Qi J, Sun S, Zhao C, Wu C, Xu Z, Cheng L, Chai R, Yan W, Wei X, Shao Z 10.1038/S41467-023-36673-Z 2023-04-19
G12/13 α12 Human Mini-G12 55 β1 Human γ2 Human Cryo-EM 7YDJ - 3.0 AGRE5 ADGRE5 ADGRE B2 (Adhesion) Human - scFv16 - Apo (no ligand)
none Apo (no ligand) - - - - 2023-07-12
Gi/o αi1 Human - 60 β1 Human γ2 Human Cryo-EM 8IRU - 3.2 DRD4 D4 Dopamine A (Rhodopsin) Human - 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 2023-06-21
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8JLZ - 3.1 5HT6R 5-HT6 5-Hydroxytryptamine A (Rhodopsin) Human - Nanobody-35 - CHEMBL365751 chembl_ligand pubchem
small-molecule Agonist 5-hydroxytryptamine small-molecule Pei Y, Wen X, Guo SC, Yang ZS, Zhang R, Xiao P, Sun JP 10.1016/J.BBRC.2023.05.126 2023-06-28
Gq/11 αq Human - 57 β1 Human γ2 Human Cryo-EM 8THL - 3.1 ADA1A α1A Adrenoceptors A (Rhodopsin) Human T4-Lysozyme scFv16 - (-)-adrenaline pubchem gtoplig chembl_ligand drugbank drug_central pubchem
small-molecule Agonist (-)-noradrenaline, (-)-adrenaline small-molecule Su M, Wang J, Xiang G, Do HN, Levitz J, Miao Y, Huang XY 10.1038/S41467-023-40524-2 2023-08-16
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8IJB 8IJB_refined 3.2 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 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 - 61 β1 Human γ2 Human Cryo-EM 8JLO - 3.5 TAAR1 TA1 Trace amine A (Rhodopsin) Human - - - ulotaront pubchem gtoplig drugbank chembl_ligand
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
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8SG1 - 2.9 CML1 chemerin Chemerin receptor A (Rhodopsin) Human - scFv16 - chemerin C-terminal peptide pubchem gtoplig chembl_ligand pubchem
peptide Agonist EPA, resolvin E1, chemerin, chemerin C-terminal peptide, 18R-HEPE peptide Zhang X, Weiss T, Cheng MH, Chen S, Ambrosius CK, Czerniak AS, Li K, Feng M, Bahar I, Beck-Sickinger AG, Zhang C 10.1371/JOURNAL.PBIO.3002188 2023-11-01
Gq/11 αq Human Gi2-mini-Gq chimera 58 β1 Human γ2 Human Cryo-EM 8WPU - 3.1 CASR CaS Calcium-sensing C (Glutamate) Human - scFv16 - cinacalcet pubchem gtoplig chembl_ligand drugbank drug_central
Calcium pubchem
small-molecule
small-molecule 		Agonist Ca2+, spermine, Mg2+, L-tryptophan small-molecule Ling S, Meng X, Zhang Y, Xia Z, Zhou Y, Yang F, Shi P, Shi C, Tian C 10.1038/S41422-023-00892-2 2023-11-22
Gi/o αo Human - 59 β1 Human γ2 Human Cryo-EM 8IY9 8IY9_refined 3.4 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 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 - 60 β1 Human γ2 Human Cryo-EM 8JPP - 3.2 SUCR1 succinate Succinate A (Rhodopsin) Human BRIL - - succinic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem
small-molecule Agonist succinic acid small-molecule Wang T, Tang W, Zhu X, Lv Z, Chen J, Li Y, Sun X, Lv H, Gu Q, Li F, Wang J 10.1038/S41422-024-00968-7 2024-05-22
Gq/11 αq Human - 59 β1 Human γ2 Human Cryo-EM 8T3V - 3.4 FFAR1 FFA1 Free fatty acid A (Rhodopsin) Human - scFv16 - docosahexaenoic acid pubchem gtoplig chembl_ligand drug_central drugbank pubchem
small-molecule Agonist oleic acid, α-linolenic acid, myristic acid, docosahexaenoic acid small-molecule Zhang X, Guseinov AA, Jenkins L, Li K, Tikhonova IG, Milligan G, Zhang C 10.1126/SCIADV.ADJ2384 2024-01-24
Gs αs Human GTP bound, Class C 59 β1 Human γ2 Human Cryo-EM 8UNN - 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 - 63 β1 Human γ2 Human Cryo-EM 8VY7 - 2.7 T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human - scFv16 - compound 28.1 [PMID: 36847646] pubchem gtoplig chembl_ligand
small-molecule Agonist - - - - 2024-04-03
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8XIQ - 2.7 SSR3 SST3 Somatostatin A (Rhodopsin) Human - Nanobody-35 - NIT-FC0-NLE-A1D5B
peptide Agonist cortistatin-14, SRIF-14, CST-17, SRIF-28 peptide - - 2024-07-03
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 8Y53 8Y53_refined 2.9 BRS3 BB3 Bombesin A (Rhodopsin) Human - scFv16
Nanobody-35 		- MK-5046 pubchem gtoplig chembl_ligand
small-molecule Agonist - - - - 2024-09-11
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8ZSS - 3.1 TAAR1 TA1 Trace amine A (Rhodopsin) Human BRIL Nanobody-35 - RO5256390 pubchem gtoplig chembl_ligand
small-molecule Agonist octopamine, β-phenylethylamine, CHEMBL1160703, tyramine, (+)-Octopamine, 3-iodothyronamine, dopamine small-molecule - - 2024-07-24
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8IKG 8IKG_refined 3.4 CNR1 CB1 Cannabinoid A (Rhodopsin) Human - scFv16 - 3-[(1S)-1-(furan-2-yl)-2-nitro-ethyl]-2-phenyl-1H-indole pubchem
small-molecule Agonist anandamide small-molecule Shen S, Wu C, Lin G, Yang X, Zhou Y, Zhao C, Miao Z, Tian X, Wang K, Yang Z, Liu Z, Guo N, Li Y, Xia A, Zhou P, Liu J, Yan W, Ke B, Yang S, Shao Z 10.1073/PNAS.2321532121 2024-06-05
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8XWP 8XWP_refined 3.2 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 Non-canonical conformation 62 β1 Human γ2 Human Cryo-EM 6OSA - 3.0 NTR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig chembl_ligand
peptide Agonist large neuromedin N, neuromedin N, neurotensin, large neurotensin peptide Kato HE, Zhang Y, Hu H, Suomivuori CM, Kadji FMN, Aoki J, Krishna Kumar K, Fonseca R, Hilger D, Huang W, Latorraca NR, Inoue A, Dror RO, Kobilka BK, Skiniotis G 10.1038/S41586-019-1337-6 2019-07-10
Gs αs Human - 55 β1 Human γ2 Human Cryo-EM 6M1H - 3.6 PACR PAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - maxadilan gtoplig 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
Gs αs Human - 57 β1 Rat γ2 Bovine Cryo-EM 7BW0 7BW0_refined 3.9 GPBAR GPBA Bile acid A (Rhodopsin) Human BRIL Nanobody-35 - - - - cholic acid, deoxycholic acid, chenodeoxycholic acid, lithocholic acid small-molecule Chen G, Wang X, Ge Y, Ma L, Chen Q, Liu H, Du Y, Ye RD, Hu H, Ren R 10.1038/S41392-020-00262-Z 2020-09-02
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7D7M 7D7M_refined 3.3 PE2R4 EP4 Prostanoid A (Rhodopsin) Human - Nanobody-35 - PGE2 pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
small-molecule Agonist PGF2α, PGI2, PGD2, thromboxane A2, PGE1, PGE2 small-molecule Nojima S, Fujita Y, Kimura KT, Nomura N, Suno R, Morimoto K, Yamamoto M, Noda T, Iwata S, Shigematsu H, Kobayashi T 10.1016/J.STR.2020.11.007 2020-11-18
Gs αs Human Engineered G alpha 58 β1 Human γ2 Human Cryo-EM 7L1V - 3.0 OX2R OX2 Orexin A (Rhodopsin) Human - scFv16
Nanobody-51 		- compound 1 [PMID: 33547286] pubchem gtoplig chembl_ligand
small-molecule Agonist orexin-B, orexin-A peptide Hong C, Byrne NJ, Zamlynny B, Tummala S, Xiao L, Shipman JM, Partridge AT, Minnick C, Breslin MJ, Rudd MT, Stachel SJ, Rada VL, Kern JC, Armacost KA, Hollingsworth SA, O'Brien JA, Hall DL, McDonald TP, Strickland C, Brooun A, Soisson SM, Hollenstein K 10.1038/S41467-021-21087-6 2021-02-10
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7CX4 7CX4_refined 2.9 PE2R2 EP2 Prostanoid A (Rhodopsin) Human - Nanobody-35 - evatanepag pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist PGF2α, PGI2, PGD2, thromboxane A2, PGE1, PGE2 small-molecule Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y 10.1126/SCIADV.ABF1268 2021-05-05
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7EZK - 3.1 CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human - - - 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 - 46 β1 Rat γ2 Mouse Cryo-EM 7PIV 7PIV_refined 2.9 MC4R MC4 Melanocortin A (Rhodopsin) Human - Nanobody-35 - afamelanotide pubchem gtoplig chembl_ligand drugbank pubchem pubchem pubchem pubchem
peptide Agonist γ-MSH, agouti-related protein, β-MSH, α-MSH, ACTH peptide Heyder NA, Kleinau G, Speck D, Schmidt A, Paisdzior S, Szczepek M, Bauer B, Koch A, Gallandi M, Kwiatkowski D, Burger J, Mielke T, Beck-Sickinger AG, Hildebrand PW, Spahn CMT, Hilger D, Schacherl M, Biebermann H, Hilal T, Kuhnen P, Kobilka BK, Scheerer P 10.1038/S41422-021-00569-8 2021-11-17
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7RKM - 3.5 US28 US28 Unclassified A (Rhodopsin) strain AD169 - scFv16 - Fractalkine pubchem
peptide Agonist - - - - 2022-01-26
Gq/11 αq Human - 60 β1 Rat γ2 Bovine Cryo-EM 7WQ4 7WQ4_refined 2.6 GALR2 GAL2 Galanin A (Rhodopsin) Human - Nanobody-35 - galanin pubchem gtoplig chembl_ligand gtoplig pubchem pubchem pubchem pubchem
peptide Agonist spexin-1, galanin-like peptide, galanin peptide Duan J, Shen DD, Zhao T, Guo S, He X, Yin W, Xu P, Ji Y, Chen LN, Liu J, Zhang H, Liu Q, Shi Y, Cheng X, Jiang H, Eric Xu H, Zhang Y, Xie X, Jiang Y 10.1038/S41467-022-29072-3 2022-04-20
Gs αs Bovine - 60 β1 Rat γ2 Bovine Cryo-EM 7EQ1 - 3.3 AGRG5 ADGRG5 ADGRG B2 (Adhesion) Human - scFv16 - Apo (no ligand)
none Apo (no ligand) - - Ping YQ, Xiao P, Yang F, Zhao RJ, Guo SC, Yan X, Wu X, Zhang C, Lu Y, Zhao F, Zhou F, Xi YT, Yin W, Liu FZ, He DF, Zhang DL, Zhu ZL, Jiang Y, Du L, Feng SQ, Schoneberg T, Liebscher I, Xu HE, Sun JP 10.1038/S41586-022-04619-Y 2022-05-11
Gi/o αi1 Human - 64 β1 Rat γ2 Human Cryo-EM 7WIC - 2.8 SSR2 SST2 Somatostatin A (Rhodopsin) Human - scFv16 - SOMATOSTATIN chembl_ligand pubchem
protein Agonist cortistatin-14, SRIF-14, CST-17, SRIF-28 peptide Chen LN, Wang WW, Dong YJ, Shen DD, Guo J, Yu X, Qin J, Ji SY, Zhang H, Shen Q, He Q, Yang B, Zhang Y, Li Q, Mao C 10.1038/S41422-022-00669-Z 2022-06-01
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7XT8 - 3.1 5HT4R 5-HT4 5-Hydroxytryptamine A (Rhodopsin) Human BRIL Nanobody-35 - 5-hydroxytryptamine pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist 5-hydroxytryptamine small-molecule Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE 10.1016/J.MOLCEL.2022.05.031 2022-07-27
Gq/11 αq Human Gi2-mini-Gq chimera 57 β1 Human γ2 Human Cryo-EM 8DPF - 2.8 5HT2C 5-HT2C 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - lorcaserin pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist 5-hydroxytryptamine small-molecule Gumpper RH, Fay JF, Roth BL 10.1016/J.CELREP.2022.111211 2022-08-24
Gi/o αi1 Human - 38 β1 Human γ2 Human Cryo-EM 7WU9 7WU9_refined 3.4 PE2R3 EP3 Prostanoid A (Rhodopsin) Human - scFv16 - Apo (no ligand)
none Apo (no ligand) PGF2α, PGI2, PGD2, thromboxane A2, PGE1, PGE2 small-molecule Suno R, Sugita Y, Morimoto K, Takazaki H, Tsujimoto H, Hirose M, Suno-Ikeda C, Nomura N, Hino T, Inoue A, Iwasaki K, Kato T, Iwata S, Kobayashi T 10.1016/J.CELREP.2022.111323 2022-08-17
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7WCM 7WCM_refined 2.3 GP119 GPR119 GPR18, GPR55 and GPR119 A (Rhodopsin) Human - Nanobody-35 - MBX-2982 pubchem gtoplig chembl_ligand drugbank
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 7YU3 7YU3_refined 3.4 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 8EFL 8EFL_refined 3.2 OPRM μ Opioid A (Rhodopsin) Human - scFv16 - CHEMBL4452384 chembl_ligand pubchem
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
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8ID4 - 3.1 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - scFv16 - linoleic acid pubchem gtoplig chembl_ligand drug_central drugbank
small-molecule Agonist oleic acid, myristic acid, α-linolenic acid, linoleic acid small-molecule Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP 10.1126/SCIENCE.ADD6220 2023-03-15
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 8IBV 8IBV_refined 3.2 MTLR motilin Motilin A (Rhodopsin) Human BRIL scFv16 - motilin pubchem gtoplig chembl_ligand gtoplig pubchem pubchem
peptide 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
Gi/o αi1 Mouse - 64 β1 Human γ2 Human Cryo-EM 8FX5 - 2.5 ACM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - xanomeline pubchem gtoplig chembl_ligand drug_central drugbank
small-molecule Agonist acetylcholine small-molecule Burger WAC, Pham V, Vuckovic Z, Powers AS, Mobbs JI, Laloudakis Y, Glukhova A, Wootten D, Tobin AB, Sexton PM, Paul SM, Felder CC, Danev R, Dror RO, Christopoulos A, Valant C, Thal DM 10.1038/S41467-023-41199-5 2023-09-13
Gs αs Human - 40 β1 Human γ2 Human Cryo-EM 8HTI - 3.0 O52E4 OR52E4 Odorant family 52 O1 (fish-like odorant) Human - Nanobody-35 - OCTANOIC ACID chembl_ligand pubchem pubchem
small-molecule Agonist - - Choi C, Bae J, Kim S, Lee S, Kang H, Kim J, Bang I, Kim K, Huh WK, Seok C, Park H, Im W, Choi HJ 10.1038/S41467-023-43983-9 2023-12-20
Gi/o αo Human - 59 β1 Human γ2 Human Cryo-EM 8J6D 8J6D_refined 3.1 C3AR C3a Complement peptide A (Rhodopsin) Human - scFv16 - EP141 peptide agonist
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
Gs αs Human - 71 β1 Human γ2 Human Cryo-EM 8GEF 8GEF_refined 3.8 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 - 59 β1 Human γ2 Bovine Cryo-EM 8IU2 8IU2_refined 3.4 OPSR OPN1LW Opsins A (Rhodopsin) Human - scFv16 - Retinal (11-cis) pubchem
small-molecule Agonist - - - - 2024-03-27
Gi/o αo Human - 58 β1 Human γ2 Human Cryo-EM 8JHN 8JHN_refined 3.8 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - scFv16 - monomethyl fumarate pubchem gtoplig chembl_ligand drugbank
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
Gq/11 αq Human - 59 β1 Human γ2 Human Cryo-EM 8T3Q 8T3Q_refined 3.1 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - scFv16 - docosahexaenoic acid pubchem gtoplig chembl_ligand drug_central drugbank pubchem
small-molecule Agonist oleic acid, myristic acid, α-linolenic acid, linoleic acid small-molecule Zhang X, Guseinov AA, Jenkins L, Li K, Tikhonova IG, Milligan G, Zhang C 10.1126/SCIADV.ADJ2384 2024-01-24
Gs αs Human GTP bound, Class D 57 β1 Human γ2 Human Cryo-EM 8UNO - 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 αgust Human - 63 β1 Human γ2 Human Cryo-EM 8VY9 - 2.9 T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human - scFv16 - compound 28.1 [PMID: 36847646] pubchem gtoplig chembl_ligand
small-molecule Agonist - - - - 2024-04-03
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8XIP - 3.3 SSR1 SST1 Somatostatin A (Rhodopsin) Human - Nanobody-35 - 004-DTR-LYS-TY5-PHE-A1D5E
peptide Agonist cortistatin-14, SRIF-14, CST-17, SRIF-28 peptide - - 2024-07-03
Gs αs Human Mini-Gs 55 β1 Human γ2 Human Cryo-EM 8UYQ - 3.5 OR4D5 OR4D5 Odorant family 4 O2 (tetrapod specific odorant) Human - Nanobody-35 - (2R)-2-methyl-1,3-thiazolidine 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 αt1 Bovine Only H5 3 - - - - X-ray 5WKT 5WKT_refined 3.2 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - B-Octylglucoside pubchem
small-molecule unknown - - Broecker J, Morizumi T, Ou WL, Klingel V, Kuo A, Kissick DJ, Ishchenko A, Lee MY, Xu S, Makarov O, Cherezov V, Ogata CM, Ernst OP 10.1038/NPROT.2017.135 2017-12-13
Gs αs Human - 48 β1 Human γ2 Human Cryo-EM 6E3Y 6E3Y_refined 3.3 CALRL calcitonin-like Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP1 		- Calcitonin gene-related peptide 1 pubchem
peptide Agonist - - Liang YL, Khoshouei M, Deganutti G, Glukhova A, Koole C, Peat TS, Radjainia M, Plitzko JM, Baumeister W, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Wootten D, Sexton PM 10.1038/S41586-018-0535-Y 2018-09-19
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 6KPG 6KPG_refined 3.0 CNR1 CB1 Cannabinoid A (Rhodopsin) Human - scFv16 - AM841 pubchem gtoplig chembl_ligand
small-molecule Agonist anandamide small-molecule Hua T, Li X, Wu L, Iliopoulos-Tsoutsouvas C, Wang Y, Wu M, Shen L, Brust CA, Nikas SP, Song F, Song X, Yuan S, Sun Q, Wu Y, Jiang S, Grim TW, Benchama O, Stahl EL, Zvonok N, Zhao S, Bohn LM, Makriyannis A, Liu ZJ 10.1016/J.CELL.2020.01.008 2020-02-12
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7CFN 7CFN_refined 3.0 GPBAR GPBA Bile acid A (Rhodopsin) Human - Nanobody-35 - INT-777 pubchem
INT-777 pubchem
small-molecule
small-molecule 		Agonist
PAM 		cholic acid, deoxycholic acid, chenodeoxycholic acid, lithocholic acid small-molecule Yang F, Mao C, Guo L, Lin J, Ming Q, Xiao P, Wu X, Shen Q, Guo S, Shen DD, Lu R, Zhang L, Huang S, Ping Y, Zhang C, Ma C, Zhang K, Liang X, Shen Y, Nan F, Yi F, Luca VC, Zhou J, Jiang C, Sun JP, Xie X, Yu X, Zhang Y 10.1038/S41586-020-2569-1 2020-09-09
Gi/o αi1 Human - 63 β1 Human γT1 Human Cryo-EM 7L0P - 4.1 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
Gq/11 αq Human - 63 β1 Human γ2 Human Cryo-EM 7DFL - 3.3 HRH1 H1 Histamine A (Rhodopsin) Human - scFv16 - histamine pubchem gtoplig chembl_ligand drug_central drugbank gtoplig
small-molecule Agonist histamine small-molecule Xia R, Wang N, Xu Z, Lu Y, Song J, Zhang A, Guo C, He Y 10.1038/S41467-021-22427-2 2021-03-31
Gs αs Human - 61 β1 Rat γ2 Bovine Cryo-EM 7DUQ - 2.5 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - N-Tert-butyl-6,7-dichloroquinoxalin-2-amine pubchem
CHEMBL410972 chembl_ligand pubchem pubchem
small-molecule
protein 		Ago-PAM
Agonist 		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 2021-07-14
Gs αs Bovine - 91 β1 Rat γ2 Bovine Cryo-EM 7FIG - 3.9 LSHR LH Glycoprotein hormone A (Rhodopsin) Human - Nanobody-35 - 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 αi2 Human - 63 β1 Human γ2 Human Cryo-EM 7WVY 7WVY_refined 3.0 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human BRIL - - Amyloid beta-Peptide (1-42) 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
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7V69 - 3.4 ACM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - Apo (no ligand)
none Apo (no ligand) 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
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 7XBD 7XBD_refined 3.1 GALR2 GAL2 Galanin A (Rhodopsin) Human - scFv16 - Galanin, Human pubchem
peptide Agonist spexin-1, galanin-like peptide, galanin peptide Heo Y, Ishimoto N, Jeon YE, Yun JH, Ohki M, Anraku Y, Sasaki M, Kita S, Fukuhara H, Ikuta T, Kawakami K, Inoue A, Maenaka K, Tame JRH, Lee W, Park SY 10.1371/JOURNAL.PBIO.3001714 2022-07-13
Gs αs Human Mini-Gs 60 β1 Human γ2 Human Cryo-EM 7XKE - 2.9 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
Gq/11 α11 Human - 62 β1 Rat γ2 Mouse Cryo-EM 7TRY - 3.7 CRFR2 CRF2 Corticotropin-releasing factor B1 (Secretin) Human - - - Urocortin pubchem
peptide Agonist corticotrophin-releasing hormone, urocortin 1, urocortin 3, urocortin 2 peptide Zhao LH, Lin J, Ji SY, Zhou XE, Mao C, Shen DD, He X, Xiao P, Sun J, Melcher K, Zhang Y, Yu X, Xu HE 10.1038/S41467-022-33851-3 2022-11-09
G12/13 α12 Human Mini-G12 55 β1 Human γ2 Human Cryo-EM 7WZ7 - 2.8 AGRF1 ADGRF1 ADGRF B2 (Adhesion) Human - scFv16 - 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
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8E3X 8E3X_refined 2.3 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 Piper SJ, Deganutti G, Lu J, Zhao P, Liang YL, Lu Y, Fletcher MM, Hossain MA, Christopoulos A, Reynolds CA, Danev R, Sexton PM, Wootten D 10.1038/S41467-022-34629-3 2022-11-23
Gs αs Human Mini-Gs 61 β1 Human γ2 Human Cryo-EM 8HJ2 8HJ2_refined 3.8 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 2023-03-15
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7XK8 7XK8_refined 3.3 NMUR2 NMU2 Neuromedin U A (Rhodopsin) Human - - - Neuromedin U-25 (human) pubchem
peptide Agonist neuromedin U-25, neuromedin S-36, neuromedin S-33, neuromedin U-23 peptide Zhao W, Zhang W, Wang M, Lu M, Chen S, Tang T, Schnapp G, Wagner H, Brennauer A, Yi C, Chu X, Han S, Wu B, Zhao Q 10.1038/S41467-022-34814-4 2023-02-22
Gi/o αo Human - 61 β1 Human γ2 Human Cryo-EM 8DZQ 8DZQ_refined 2.8 OPRK κ Opioid A (Rhodopsin) Human - scFv16 - SALVINORIN B METHOXYMETHYL ETHER chembl_ligand pubchem
small-molecule 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 Han J, Zhang J, Nazarova AL, Bernhard SM, Krumm BE, Zhao L, Lam JH, Rangari VA, Majumdar S, Nichols DE, Katritch V, Yuan P, Fay JF, Che T 10.1038/S41586-023-06030-7 2023-05-03
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8FLU - 2.8 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - PTH
peptide Agonist PTHrP-(1-36), PTHrP, PTH, TIP39 peptide Cary BP, Gerrard EJ, Belousoff MJ, Fletcher MM, Jiang Y, Russell IC, Piper SJ, Wootten D, Sexton PM 10.1016/J.STR.2023.04.002 2023-04-26
Gs αs Human Mini-Gs 57 β1 Human γ2 Human Cryo-EM 8IRR - 3.2 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - rotigotine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist L-NOREPINEPHRINE, noradrenaline, (-)-noradrenaline, 5-hydroxytryptamine, 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 2023-06-21
Gq/11 αq Human - 62 β1 Human γ2 Human Cryo-EM 7YFC - 3.0 HRH4 H4 Histamine A (Rhodopsin) Human - scFv16
Nanobody-35 		- histamine pubchem gtoplig chembl_ligand drug_central drugbank gtoplig
small-molecule Agonist CCL16, histamine small-molecule Im D, Kishikawa JI, Shiimura Y, Hisano H, Ito A, Fujita-Fujiharu Y, Sugita Y, Noda T, Kato T, Asada H, Iwata S 10.1038/S41467-023-42260-Z 2023-10-25
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8HN8 - 3.0 HRH4 H4 Histamine A (Rhodopsin) Human - scFv16 - histamine pubchem gtoplig chembl_ligand drug_central drugbank gtoplig
small-molecule Agonist CCL16, histamine small-molecule - - 2023-12-20
Gs αs Human - 62 β1 Rat γ2 Bovine Cryo-EM 8JIP 8JIP_refined 2.9 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - MEDI0382
peptide Agonist glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide 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 2023-09-06
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8W87 - 2.8 TAAR1 TA1 Trace amine A (Rhodopsin) Human - Nanobody-35 - METHAMPHETAMINE chembl_ligand pubchem
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
Gs αs Human - 60 β1 Rat γ2 Bovine Cryo-EM 7V9L - 2.6 GHRHR GHRH Glucagon B1 (Secretin) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) GHRH peptide Cong Z, Zhou F, Zhang C, Zou X, Zhang H, Wang Y, Zhou Q, Cai X, Liu Q, Li J, Shao L, Mao C, Wang X, Wu J, Xia T, Zhao LH, Jiang H, Zhang Y, Xu HE, Cheng X, Yang D, Wang MW 10.1073/PNAS.2106606118 2022-04-06
Gs αs Human - 69 β1 Human γ2 Human Cryo-EM 8GEE 8GEE_refined 3.7 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 - 57 β1 Human γ2 Human Cryo-EM 8IYW 8IYW_refined 3.5 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - scFv16 - GSK256073 pubchem gtoplig chembl_ligand
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
Gi/o αi1 Human - 58 β1 Human γ2 Human Cryo-EM 8JXV - 3.2 HRH4 H4 Histamine A (Rhodopsin) Human - scFv16 - clozapine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist CCL16, histamine small-molecule - - 2024-03-20
Gq/11 αq Human - 58 β1 Human γ2 Human Cryo-EM 8XJO 8XJO_refined 3.1 TA2R TP Prostanoid A (Rhodopsin) Human - scFv16 - U46619 pubchem gtoplig chembl_ligand gtoplig
small-molecule Agonist PGF2α, PGH2, PGI2, PGD2, thromboxane A2, PGE2 small-molecule Li X, Zhang X, Wen X, Zhang D, Qu C, Miao X, Zhang W, Zhang R, Liu G, Xiao P, Sun JP, Gong W 10.1016/J.CELREP.2024.113893 2024-02-28
Gi/o αi1 Human - 60 β1 Rat γ2 Bovine Cryo-EM 8YKX 8YKX_refined 2.7 SUCR1 succinate Succinate A (Rhodopsin) Human - scFv16 - maleic acid pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist succinic acid small-molecule Li C, Liu H, Li J, He X, Zhu H, Fu W, Xu HE 10.1038/S41422-024-00984-7 2024-05-29
Gq/11 αq Human - 59 β1 Human γ2 Human Cryo-EM 8ZPT 8ZPT_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
Gq/11 αq Human Mini-Gq 64 β1 Human γ2 Human Cryo-EM 8YN2 - 2.7 HRH1 H1 Histamine A (Rhodopsin) Human - scFv16 - 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
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 9JKQ 9JKQ_refined 2.7 TAAR1 TA1 Trace amine A (Rhodopsin) Human BRIL Nanobody-35 - METHAMPHETAMINE chembl_ligand pubchem
small-molecule Agonist octopamine, β-phenylethylamine, CHEMBL1160703, tyramine, (+)-Octopamine, 3-iodothyronamine, dopamine small-molecule Lin Y, Wang J, Shi F, Yang L, Wu S, Qiao A, Ye S 10.1021/ACS.JMEDCHEM.4C01961 2024-10-16
Gs αs Human - 49 β1 Human γ2 Human Cryo-EM 6B3J - 3.3 GLP1R GLP-1 Glucagon B1 (Secretin) Human - - - Exendin-P5
peptide Agonist glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide peptide Liang YL, Khoshouei M, Glukhova A, Furness SGB, Zhao P, Clydesdale L, Koole C, Truong TT, Thal DM, Lei S, Radjainia M, Danev R, Baumeister W, Wang MW, Miller LJ, Christopoulos A, Sexton PM, Wootten D 10.1038/NATURE25773 2018-02-21
Gs αs Bovine - 58 β1 Rat γ2 Bovine Cryo-EM 6NBF - 3.0 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 Mini-Gs 61 β1 Human γ2 Human Cryo-EM 6LI3 - 3.3 GPR52 GPR52 A orphans A (Rhodopsin) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Lin X, Li M, Wang N, Wu Y, Luo Z, Guo S, Han GW, Li S, Yue Y, Wei X, Xie X, Chen Y, Zhao S, Wu J, Lei M, Xu F 10.1038/S41586-020-2019-0 2020-02-26
Gi/o αt2 Bovine Only H5 3 - - - - X-ray 6PGS 6PGS_refined 2.9 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - Geraniol pubchem
small-molecule unknown - - - - 2020-07-01
Gs αs Human - 57 β1 Human γ2 Human Cryo-EM 6VCB - 3.3 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - glucagon-like peptide 1-(7-37) pubchem gtoplig chembl_ligand gtoplig pubchem pubchem
CHEMBL5197819 chembl_ligand pubchem
peptide
small-molecule 		Agonist
PAM 		glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide peptide Bueno AB, Sun B, Willard FS, Feng D, Ho JD, Wainscott DB, Showalter AD, Vieth M, Chen Q, Stutsman C, Chau B, Ficorilli J, Agejas FJ, Cumming GR, Jimenez A, Rojo I, Kobilka TS, Kobilka BK, Sloop KW 10.1038/S41589-020-0589-7 2020-07-22
Gs αs Human - 49 β1 Bovine γ2 Bovine Cryo-EM 7DHR 7DHR_refined 3.8 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - Nanobody-35 - LEVISOPRENALINE chembl_ligand chembl_ligand pubchem
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule Yang F, Ling S, Zhou Y, Zhang Y, Lv P, Liu S, Fang W, Sun W, Hu LA, Zhang L, Shi P, Tian C 10.1093/NSR/NWAA284 2020-12-16
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7JV5 - 3.0 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - CHEMBL1160787 chembl_ligand pubchem
small-molecule Agonist L-NOREPINEPHRINE, noradrenaline, (-)-noradrenaline, 5-hydroxytryptamine, 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 Human - 58 β1 Human γ2 Human Cryo-EM 7KH0 - 2.8 V2R V2 Vasopressin and oxytocin A (Rhodopsin) Human - scFv16
Nanobody-35 		- vasopressin pubchem gtoplig chembl_ligand drugbank drug_central
peptide Agonist oxytocin, vasopressin peptide Wang L, Xu J, Cao S, Sun D, Liu H, Lu Q, Liu Z, Du Y, Zhang C 10.1038/S41422-021-00483-Z 2021-05-26
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7EVW - 3.2 FZD7 FZD7 Frizzled F (Frizzled) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Xu L, Chen B, Schihada H, Wright SC, Turku A, Wu Y, Han GW, Kowalski-Jahn M, Kozielewicz P, Bowin CF, Zhang X, Li C, Bouvier M, Schulte G, Xu F 10.1038/S41422-021-00525-6 2021-08-04
Gs αs Human - 60 β1 Rat γ2 Bovine Cryo-EM 7EVM - 2.5 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
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7EW3 - 3.1 S1PR3 S1P3 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - Sphingosine 1-phosphate pubchem
lipid 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 - 62 β1 Human γ2 Human Cryo-EM 7VDH - 2.9 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human - scFv16 - compound 48/80 pubchem gtoplig
small-molecule 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 - 57 β1 Rat γ2 Bovine Cryo-EM 7V9M 7V9M_refined 3.3 GHRHR GHRH Glucagon B1 (Secretin) Human - Nanobody-35 - Somatoliberin pubchem
peptide Agonist GHRH peptide Cong Z, Zhou F, Zhang C, Zou X, Zhang H, Wang Y, Zhou Q, Cai X, Liu Q, Li J, Shao L, Mao C, Wang X, Wu J, Xia T, Zhao LH, Jiang H, Zhang Y, Xu HE, Cheng X, Yang D, Wang MW 10.1073/PNAS.2106606118 2021-10-20
Gi/o αi1 Mouse - 63 β1 Bovine γ2 Bovine Cryo-EM 7TD3 - 3.0 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - - - sphingosine 1-phosphate pubchem gtoplig chembl_ligand pubchem
small-molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine 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
Gs αs Bovine - 59 β1 Rat γ2 Bovine Cryo-EM 7FIN - 3.1 GIPR GIP Glucagon B1 (Secretin) Human - Nanobody-35 - Peptide-20
peptide Agonist gastric inhibitory polypeptide 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 2022-02-23
Gs αs Human Mini-Gs 58 β1 Human γ2 Human Cryo-EM 7WUI - 3.1 AGRG2 ADGRG2 ADGRG B2 (Adhesion) Mouse - - - IP15
peptide Agonist - - Xiao P, Guo S, Wen X, He QT, Lin H, Huang SM, Gou L, Zhang C, Yang Z, Zhong YN, Yang CC, Li Y, Gong Z, Tao XN, Yang ZS, Lu Y, Li SL, He JY, Wang C, Zhang L, Kong L, Sun JP, Yu X 10.1038/S41586-022-04590-8 2022-04-27
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7F23 - 3.6 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
Gs αs Human - 61 β1 Human γ2 Human Cryo-EM 7XTC 7XTC_refined 3.2 5HT7R 5-HT7 5-Hydroxytryptamine A (Rhodopsin) Human BRIL Nanobody-35 - 5-CT pubchem gtoplig chembl_ligand
small-molecule Agonist 5-hydroxytryptamine small-molecule Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE 10.1016/J.MOLCEL.2022.05.031 2022-07-27
Gq/11 αq Human Gi2-mini-Gq chimera 57 β1 Human γ2 Human Cryo-EM 8DPG - 3.6 5HT2C 5-HT2C 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - psilocin pubchem gtoplig chembl_ligand
small-molecule Agonist 5-hydroxytryptamine small-molecule Gumpper RH, Fay JF, Roth BL 10.1016/J.CELREP.2022.111211 2022-08-24
Gs αs Human - 58 β1 Rat γ2 Bovine Cryo-EM 7VVK - 3.3 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 Kobayashi K, Kawakami K, Kusakizako T, Miyauchi H, Tomita A, Kobayashi K, Shihoya W, Yamashita K, Nishizawa T, Kato HE, Inoue A, Nureki O 10.1016/J.MOLCEL.2022.07.003 2022-08-03
Gi/o αo Human - 63 β1 Rat γ2 Mouse Cryo-EM 7TS0 7TS0_refined 2.8 CRFR2 CRF2 Corticotropin-releasing factor B1 (Secretin) Human - scFv16 - Urocortin pubchem
peptide Agonist corticotrophin-releasing hormone, urocortin 1, urocortin 3, urocortin 2 peptide Zhao LH, Lin J, Ji SY, Zhou XE, Mao C, Shen DD, He X, Xiao P, Sun J, Melcher K, Zhang Y, Yu X, Xu HE 10.1038/S41467-022-33851-3 2022-11-09
Gq/11 αq Human - 58 β1 Rat γ2 Bovine Cryo-EM 7XW9 - 2.7 TRFR TRH1 Thyrotropin-releasing hormone A (Rhodopsin) Human - scFv16 - TRH pubchem
peptide Agonist TRH peptide - - 2022-12-28
Gs αs Human - 55 β1 Human γ2 Human Cryo-EM 8E3Z 8E3Z_refined 2.7 VIPR1 VPAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - Vasoactive intestinal polypeptide pubchem
small-molecule Agonist PHM, GHRH, VIP, PACAP-27, PHI, secretin, PACAP-38 peptide Piper SJ, Deganutti G, Lu J, Zhao P, Liang YL, Lu Y, Fletcher MM, Hossain MA, Christopoulos A, Reynolds CA, Danev R, Sexton PM, Wootten D 10.1038/S41467-022-34629-3 2022-11-23
Gi/o αo Human - 60 β1 Human γ2 Human Cryo-EM 8FN1 - 2.9 NTR1 NTS1 Neurotensin A (Rhodopsin) Rat - scFv16 - neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
peptide Agonist neuromedin N, neurotensin peptide Krumm BE, DiBerto JF, Olsen RHJ, Kang HJ, Slocum ST, Zhang S, Strachan RT, Huang XP, Slosky LM, Pinkerton AB, Barak LS, Caron MG, Kenakin T, Fay JF, Roth BL 10.1021/ACS.BIOCHEM.3C00029 2023-03-29
Gi/o αo Human - 62 β1 Human γ2 Human Cryo-EM 7T8X 7T8X_refined 3.2 ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human - Antibody fragment - acetylcholine pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
small-molecule Agonist acetylcholine small-molecule - - 2023-01-25
Gq/11 αq Human Gs-mini-Gq chimera 52 β1 Human γ2 Human Cryo-EM 8G2Y - 3.4 AGRF1 ADGRF1 ADGRF B2 (Adhesion) Human - Nanobody-35 - [1-Myristoyl-glycerol-3-YL]phosphonylcholine pubchem
small-molecule Agonist - - Jones DTD, Dates AN, Rawson SD, Burruss MM, Lipper CH, Blacklow SC 10.1038/S41467-023-38083-7 2023-05-10
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7YAE 7YAE_refined 3.4 SSR2 SST2 Somatostatin A (Rhodopsin) Human - scFv16 - Octreotide
peptide Agonist cortistatin-14, SRIF-14, CST-17, SRIF-28 peptide Zhao J, Fu H, Yu J, Hong W, Tian X, Qi J, Sun S, Zhao C, Wu C, Xu Z, Cheng L, Chai R, Yan W, Wei X, Shao Z 10.1038/S41467-023-36673-Z 2023-04-19
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8FLR - 2.9 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - PTHrP[1-36]
peptide Agonist PTHrP-(1-36), PTHrP, PTH, TIP39 peptide Cary BP, Gerrard EJ, Belousoff MJ, Fletcher MM, Jiang Y, Russell IC, Piper SJ, Wootten D, Sexton PM 10.1016/J.STR.2023.04.002 2023-04-26
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8J1A - 3.2 GPR84 GPR84 A orphans A (Rhodopsin) Human - scFv16 - Apo (no ligand)
none Apo (no ligand) - - 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 - 57 β1 Human γ2 Human Cryo-EM 8THK - 2.6 ADA1A α1A Adrenoceptors A (Rhodopsin) Human T4-Lysozyme scFv16 - CHEMBL133451 chembl_ligand pubchem
small-molecule Agonist (-)-noradrenaline, (-)-adrenaline small-molecule Su M, Wang J, Xiang G, Do HN, Levitz J, Miao Y, Huang XY 10.1038/S41467-023-40524-2 2023-08-16
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 8H2G 8H2G_refined 3.0 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 - - 2023-10-11
Gi/o αi1 Human - 62 β1 Mouse γ2 Mouse Cryo-EM 8IHH - 3.1 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human BRIL scFv16 - 5-butyl-1H-pyrazole-3-carboxylic acid 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 2023-08-30
Gs αs Human - 58 β1 Rat γ2 Bovine Cryo-EM 8JIR 8JIR_refined 2.6 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - SAR425899
peptide Agonist glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide 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 2023-09-06
Gs αs Human - 56 β1 Human γ2 Human Cryo-EM 8TB0 8TB0_refined 3.5 GPR61 GPR61 A orphans A (Rhodopsin) Human - scFv16 - Apo (no ligand)
none Apo (no ligand) - - - - 2023-10-04
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8GE4 - 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 - 60 β1 Human γ2 Human Cryo-EM 8GG6 - 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 - 61 β1 Human γ2 Human Cryo-EM 8IED - 3.3 GP156 GPR156 C Orphans C (Glutamate) Human - - - [(2R)-3-[(E)-hexadec-9-enoyl]oxy-2-octadecanoyloxypropyl] 2-(trimethylazaniumyl)ethyl phosphate pubchem
lipid Agonist - - - - 2024-02-14
Gi/o αi3 Rhesus macaque - 63 β1 Human γ2 Human Cryo-EM 8K9K - 3.0 OPRM μ Opioid A (Rhodopsin) Human BRIL scFv16 - DAMGO pubchem gtoplig chembl_ligand chembl_ligand
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 Kaneko S, Imai S, Uchikubo-Kamo T, Hisano T, Asao N, Shirouzu M, Shimada I 10.1038/S41467-024-47792-6 2024-05-29
Gi/o αo Human - 97 β1 Human γ2 Human Cryo-EM 8U02 8U02_refined 3.3 DRD2 D2 Dopamine A (Rhodopsin) Human - - - 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 I 60 β1 Human γ2 Human Cryo-EM 8UNT - 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 αt1 Bovine - 59 β1 Rat γ2 Bovine Cryo-EM 8XGR - 3.2 EDNRB ETB Endothelin A (Rhodopsin) Human - Camelid antibody VHH fragment - ENDOTHELIN chembl_ligand pubchem
protein Agonist endothelin-2, endothelin-3, endothelin-1 peptide - - 2024-04-03
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8YUU - 2.7 HRH3 H3 Histamine A (Rhodopsin) Human - scFv16 - histamine pubchem gtoplig chembl_ligand drug_central drugbank gtoplig
small-molecule Agonist histamine small-molecule Shen Q, Tang X, Wen X, Cheng S, Xiao P, Zang SK, Shen DD, Jiang L, Zheng Y, Zhang H, Xu H, Mao C, Zhang M, Hu W, Sun JP, Zhang Y, Chen Z 10.1002/ADVS.202310120 2024-06-05
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8ZSV - 3.0 TAAR1 TA1 Trace amine A (Rhodopsin) Mouse BRIL Nanobody-35 - RO5256390 pubchem gtoplig chembl_ligand
small-molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine small-molecule - - 2024-07-24
Gs αs Human - 57 β1 Rat γ2 Bovine Cryo-EM 9IJD - 2.8 ADRB3 β3 Adrenoceptors A (Rhodopsin) Human - Camelid antibody VHH fragment - Carazolol pubchem
small-molecule Inverse agonist (-)-noradrenaline, (-)-adrenaline, (±)-adrenaline, (+)-adrenaline small-molecule Zheng S, Zhang S, Dai S, Chen K, Gao K, Sun X, Lin B, Liu X 10.1002/CPLU.202400288 2024-08-21
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 6DDE - 3.5 OPRM μ Opioid A (Rhodopsin) Mouse - Antibody - DAMGO pubchem gtoplig chembl_ligand chembl_ligand
peptide Agonist - - Koehl A, Hu H, Maeda S, Zhang Y, Qu Q, Paggi JM, Latorraca NR, Hilger D, Dawson R, Matile H, Schertler GFX, Granier S, Weis WI, Dror RO, Manglik A, Skiniotis G, Kobilka BK 10.1038/S41586-018-0219-7 2018-06-13
Gi/o αt1 Bovine Only H5 3 - - - - X-ray 6PEL 6PEL_refined 3.2 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - Citronellol pubchem
small-molecule unknown - - - - 2020-06-24
Gi/o αo Human - 61 β1 Human γ2 Human Cryo-EM 7D77 - 2.9 AGRG3 ADGRG3 ADGRG B2 (Adhesion) Human - scFv16 - HYDROCORTISONE chembl_ligand pubchem
small-molecule Agonist - - Ping YQ, Mao C, Xiao P, Zhao RJ, Jiang Y, Yang Z, An WT, Shen DD, Yang F, Zhang H, Qu C, Shen Q, Tian C, Li ZJ, Li S, Wang GY, Tao X, Wen X, Zhong YN, Yang J, Yi F, Yu X, Xu HE, Zhang Y, Sun JP 10.1038/S41586-020-03083-W 2021-02-03
Gs αs Human - 61 β1 Rat γ2 Human Cryo-EM 7MBX - 2.0 CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human - Nanobody-35 - CHEMBL216166 chembl_ligand pubchem
protein Agonist CCK-8, desulfated cholecystokinin-8, CCK-39, CCK-58, CCK-33, CCK-4, gastrin-17 peptide Mobbs JI, Belousoff MJ, Harikumar KG, Piper SJ, Xu X, Furness SGB, Venugopal H, Christopoulos A, Danev R, Wootten D, Thal DM, Miller LJ, Sexton PM 10.1371/JOURNAL.PBIO.3001295 2021-05-26
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7F1Q - 2.9 CCR5 CCR5 Chemokine A (Rhodopsin) Human - - - CCL3 gtoplig
peptide Agonist CCL11, CCL14, CCL2, CCL8, CCL5, CCL16, CCL4, CCL13, CCL7, CCL3 peptide - - 2021-07-14
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7F53 - 3.0 MC4R MC4 Melanocortin A (Rhodopsin) Human - Nanobody-35 - α-MSH pubchem gtoplig
peptide Agonist γ-MSH, agouti-related protein, β-MSH, α-MSH, ACTH peptide Zhang H, Chen LN, Yang D, Mao C, Shen Q, Feng W, Shen DD, Dai A, Xie S, Zhou Y, Qin J, Sun JP, Scharf DH, Hou T, Zhou T, Wang MW, Zhang Y 10.1038/S41422-021-00552-3 2021-11-03
Gs αs Human - 61 β1 Human γ2 Human Cryo-EM 7VUH 7VUH_refined 3.2 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 - - 2021-12-29
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7EW0 7EW0_refined 3.4 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - ozanimod pubchem gtoplig drug_central chembl_ligand 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 - 53 β1 Rat γ2 Bovine Cryo-EM 7V35 7V35_refined 3.4 GLR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - Peptide-20
peptide Agonist glucagon 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
Gs αs Bovine Gi1-Gs chimera 56 β1 Bovine γ2 Bovine Cryo-EM 7S0G - 3.9 ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey - - - LEVISOPRENALINE chembl_ligand chembl_ligand pubchem
small-molecule Agonist - - Alegre KO, Paknejad N, Su M, Lou JS, Huang J, Jordan KD, Eng ET, Meyerson JR, Hite RK, Huang XY 10.1038/S41594-021-00679-2 2021-11-17
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7X9C 7X9C_refined 3.0 NPY4R Y4 Neuropeptide Y A (Rhodopsin) Human - - - Pancreatic polypeptide pubchem
peptide Agonist peptide YY, pancreatic polypeptide, neuropeptide Y, PYY-(3-36) peptide Tang T, Tan Q, Han S, Diemar A, Lobner K, Wang H, Schuss C, Behr V, Morl K, Wang M, Chu X, Yi C, Keller M, Kofoed J, Reedtz-Runge S, Kaiser A, Beck-Sickinger AG, Zhao Q, Wu B 10.1126/SCIADV.ABM1232 2022-05-18
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7W0M 7W0M_refined 3.7 APJ apelin Apelin A (Rhodopsin) Human BRIL scFv16 - (1R,2S)-N-[4-(2,6-dimethoxyphenyl)-5-(6-methylpyridin-2-yl)-1,2,4-triazol-3-yl]-1-(5-methylpyrimidin-2-yl)-1-oxidanyl-propane-2-sulfonamide pubchem
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 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 - 63 β1 Bovine γ2 Bovine Cryo-EM 7XAV 7XAV_refined 2.9 SSR2 SST2 Somatostatin A (Rhodopsin) Human - scFv16 - lanreotide pubchem gtoplig drugbank
peptide Agonist cortistatin-14, SRIF-14, CST-17, SRIF-28 peptide Bo Q, Yang F, Li Y, Meng X, Zhang H, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C 10.1038/S41421-022-00405-2 2022-08-31
Gs αs Human - 57 β1 Human γ2 Human Cryo-EM 7XKD - 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 - 62 β1 Human γ2 Human Cryo-EM 7T2G - 2.5 OPRM μ Opioid A (Rhodopsin) Mouse BRIL - - CHEMBL58362 chembl_ligand pubchem
small-molecule Agonist - - Qu Q, Huang W, Aydin D, Paggi JM, Seven AB, Wang H, Chakraborty S, Che T, DiBerto JF, Robertson MJ, Inoue A, Suomivuori CM, Roth BL, Majumdar S, Dror RO, Kobilka BK, Skiniotis G 10.1038/S41589-022-01208-Y 2022-12-07
G12/13 α12 Human - 55 β1 Human γ2 Human Cryo-EM 7X10 - 2.9 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 2022-11-09
Gq/11 αq Human Mini-Gq 56 β1 Human γ2 Human Cryo-EM 8E9Y - 2.8 ACM3 M3 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - Clozapine N-oxide pubchem
small-molecule Agonist acetylcholine small-molecule Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL 10.1038/S41586-022-05489-0 2022-11-30
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7YS6 7YS6_refined 3.0 5HT6R 5-HT6 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - 5-hydroxytryptamine pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist 5-hydroxytryptamine small-molecule - - 2023-03-29
Gs αs Human Mini-Gs 59 β1 Human γ2 Human Cryo-EM 8HDO - 2.9 AA2BR A2B Adenosine A (Rhodopsin) Human - Nanobody-35 - BAY 60-6583 pubchem gtoplig chembl_ligand
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 αi1 Human - 63 β1 Human γ2 Human Cryo-EM 7XK2 7XK2_refined 3.1 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 Yang Y, Kang HJ, Gao R, Wang J, Han GW, DiBerto JF, Wu L, Tong J, Qu L, Wu Y, Pileski R, Li X, Zhang XC, Zhao S, Kenakin T, Wang Q, Stevens RC, Peng W, Roth BL, Rao Z, Liu ZJ 10.1038/S41467-023-37177-6 2023-02-22
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 8EJC - 3.0 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
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8GUR 8GUR_refined 2.8 CNR2 CB2 Cannabinoid A (Rhodopsin) Human - scFv16 - CP55940 pubchem gtoplig chembl_ligand gtoplig
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
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8J18 - 2.9 GPR84 GPR84 A orphans A (Rhodopsin) Human - scFv16 - (3R)-3-HYDROXYDODECANOIC ACID pubchem
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 8JPB - 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 αo Human - 58 β1 Human γ2 Human Cryo-EM 8HPT - 3.4 C5AR1 C5a1 Complement peptide A (Rhodopsin) Mouse - scFv16 - C5a
peptide Agonist - - None HTTPS://DOI.ORG/10.1016/J.CELL.2023.09.020 2023-10-18
Gs αs Human Gi1-Gs chimera 59 β1 Human γ2 Bovine Cryo-EM 8IOD - 2.6 MC5R MC5 Melanocortin A (Rhodopsin) Human - Nanobody-35 - PG-901 pubchem
peptide Agonist γ-MSH, agouti-related protein, β-MSH, α-MSH, ACTH peptide Chen VB, Arendall WB 3rd, Headd JJ, Keedy DA, Immormino RM, Kapral GJ, Murray LW, Richardson JS, Richardson DC 10.1107/S0907444909042073 2023-09-20
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8JLR - 3.0 TAAR1 TA1 Trace amine A (Rhodopsin) Human BRIL scFv16 - (1~{S},3~{R})-3-(1-adamantyl)-1-(aminomethyl)-3,4-dihydro-1~{H}-isochromene-5,6-diol 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
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 8W89 - 3.0 TAAR1 TA1 Trace amine A (Rhodopsin) Human - Nanobody-35 - 2-Phenylethanaminium pubchem
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
Gs αs Human - 70 β1 Human γ2 Human Cryo-EM 8GEI - 4.1 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 - 63 β1 Human γ2 Human Cryo-EM 8J20 - 3.2 FFAR3 FFA3 Free fatty acid A (Rhodopsin) Human - scFv16 - pentanoic acid pubchem gtoplig chembl_ligand drugbank
(4R)-N-[2,5-bis(chloranyl)phenyl]-4-(furan-2-yl)-2-methyl-5-oxidanylidene-4,6,7,8-tetrahydro-1H-quinoline-3-carboxamide pubchem
small-molecule
small-molecule 		Agonist
PAM 		propanoic 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 GTP bound, Class A 59 β1 Human γ2 Human Cryo-EM 8UNL - 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 GTP bound, Class T 74 β1 Human γ2 Human Cryo-EM 8UO4 8UO4_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
Gq/11 αq Human - 60 β1 Rat γ2 Bovine Cryo-EM 8WZ2 8WZ2_refined 2.7 QRFPR QRFP Peptide P518 A (Rhodopsin) Human - scFv16 - Orexigenic neuropeptide QRFP
peptide Agonist QRFP26 (26RFa), QRFP43, QRFP43 (43RFa) peptide Jin S, Guo S, Xu Y, Li X, Wu C, He X, Pan B, Xin W, Zhang H, Hu W, Yin Y, Zhang T, Wu K, Yuan Q, Xu HE, Xie X, Jiang Y 10.1038/S41421-024-00670-3 2024-06-19
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8XVH 8XVH_refined 3.3 EDNRB ETB Endothelin A (Rhodopsin) Human - Nanobody-35 Exo-alpha-sialidase ENDOTHELIN chembl_ligand pubchem
protein Agonist endothelin-2, endothelin-3, endothelin-1 peptide Hou J, Liu S, Zhang X, Tu G, Wu L, Zhang Y, Yang H, Li X, Liu J, Jiang L, Tan Q, Bai F, Liu Z, Miao C, Hua T, Luo Z 10.1038/S41421-024-00705-9 2024-08-28
Gi/o αi1 Human - 60 β1 Human γ2 Human Cryo-EM 9AYF - 3.6 CASR CaS Calcium-sensing C (Glutamate) Human - scFv16 - Cyclomethyltryptophan pubchem
tecalcet pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Agonist
PAM 		Ca2+, spermine, Mg2+, L-tryptophan small-molecule Zuo H, Park J, Frangaj A, Ye J, Lu G, Manning JJ, Asher WB, Lu Z, Hu GB, Wang L, Mendez J, Eng E, Zhang Z, Lin X, Grassucci R, Hendrickson WA, Clarke OB, Javitch JA, Conigrave AD, Fan QR 10.1038/S41586-024-07331-1 2024-04-17
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 6DDF - 3.5 OPRM μ Opioid A (Rhodopsin) Mouse - - - DAMGO pubchem gtoplig chembl_ligand chembl_ligand
peptide Agonist - - Koehl A, Hu H, Maeda S, Zhang Y, Qu Q, Paggi JM, Latorraca NR, Hilger D, Dawson R, Matile H, Schertler GFX, Granier S, Weis WI, Dror RO, Manglik A, Skiniotis G, Kobilka BK 10.1038/S41586-018-0219-7 2018-06-13
Gi/o αt1 Bovine - 64 β1 Bovine γT1 Bovine Cryo-EM 6OY9 - 3.9 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - 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 - 49 β1 Human γ2 Human Cryo-EM 6ORV 6ORV_refined 3.0 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - CHEMBL3950796 chembl_ligand pubchem
small-molecule Agonist glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide peptide Zhao P, Liang YL, Belousoff MJ, Deganutti G, Fletcher MM, Willard FS, Bell MG, Christe ME, Sloop KW, Inoue A, Truong TT, Clydesdale L, Furness SGB, Christopoulos A, Wang MW, Miller LJ, Reynolds CA, Danev R, Sexton PM, Wootten D 10.1038/s41586-019-1902-z 2020-01-08
Gs αs Human - 49 β1 Human γ2 Human Cryo-EM 7C2E - 4.2 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - 2-[[4-[6-[(4-cyano-2-fluoranyl-phenyl)methoxy]pyridin-2-yl]-3,6-dihydro-2~{H}-pyridin-1-yl]methyl]-3-[[(2~{S})-oxetan-2-yl]methyl]imidazo[4,5-b]pyridine-5-carboxylic acid pubchem
small-molecule Agonist glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide peptide Ma H, Huang W, Wang X, Zhao L, Jiang Y, Liu F, Guo W, Sun X, Zhong W, Yuan D, Xu HE 10.1038/S41422-020-0384-8 2020-08-26
Gs αs Human - 54 β1 Human γ2 Human Cryo-EM 7BB6 - 4.2 V2R V2 Vasopressin and oxytocin A (Rhodopsin) Human - Nanobody-35 - vasopressin pubchem gtoplig chembl_ligand drugbank drug_central
peptide Agonist oxytocin, vasopressin peptide Bous J, Orcel H, Floquet N, Leyrat C, Lai-Kee-Him J, Gaibelet G, Ancelin A, Saint-Paul J, Trapani S, Louet M, Sounier R, Demene H, Granier S, Bron P, Mouillac B 10.1126/SCIADV.ABG5628 2021-06-02
Gs αs Human - 59 β1 Rat γ2 Bovine Cryo-EM 7DH5 - 3.2 ADRB3 β3 Adrenoceptors A (Rhodopsin) Dog - Nanobody-35 - mirabegron pubchem gtoplig chembl_ligand drugbank drug_central
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 2021-08-04
Gs αs Bovine - 60 β1 Rat γ2 Bovine Cryo-EM 7FIH - 3.2 LSHR LH Glycoprotein hormone A (Rhodopsin) Human - - - Choriogonadotropin beta gtoplig
Glycoprotein alpha gtoplig
5-Amino-N-(1,1-dimethylethyl)-2-(methylthio)-4-[3-[[2-(4-morpholinyl)acetyl]amino]phenyl]thieno[2,3-d]pyrimidine-6-carboxamide pubchem
protein
protein
small-molecule 		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 αo Human - 59 β1 Human γ2 Human Cryo-EM 7EJA - 3.6 ADA2A α2A Adrenoceptors A (Rhodopsin) Human - scFv16 - dexmedetomidine 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 - 55 β1 Human γ2 Human Cryo-EM 7WUQ - 2.9 AGRG2 ADGRG2 ADGRG B2 (Adhesion) Mouse - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Xiao P, Guo S, Wen X, He QT, Lin H, Huang SM, Gou L, Zhang C, Yang Z, Zhong YN, Yang CC, Li Y, Gong Z, Tao XN, Yang ZS, Lu Y, Li SL, He JY, Wang C, Zhang L, Kong L, Sun JP, Yu X 10.1038/S41586-022-04590-8 2022-04-27
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7F1Z - 3.5 DRD1 D1 Dopamine A (Rhodopsin) Human - - - 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
Gi/o αo Human Mini-Go 60 β1 Human γ2 Human Cryo-EM 7UM7 7UM7_refined 2.8 5HT5A 5-HT5A 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - methylergonovine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist 5-hydroxytryptamine small-molecule Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL 10.1038/S41594-022-00796-6 2022-07-20
Gs αs Human Mini-Gs 56 β1 Human γ2 Human Cryo-EM 7UTZ - 2.4 TSHR TSH Glycoprotein hormone A (Rhodopsin) Human - Nanobody-35 - Glycoprotein hormones alpha chain analog TR1402
Thyrotropin subunit beta
protein
protein 		Agonist TSH peptide Faust B, Billesbolle CB, Suomivuori CM, Singh I, Zhang K, Hoppe N, Pinto AFM, Diedrich JK, Muftuoglu Y, Szkudlinski MW, Saghatelian A, Dror RO, Cheng Y, Manglik A 10.1038/S41586-022-05159-1 2022-08-03
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8IJ3 8IJ3_refined 3.3 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - scFv16 - Apo (no ligand)
none Apo (no ligand) 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 - 60 β1 Human γ2 Human Cryo-EM 8W8R - 3.3 GP101 GPR101 A orphans A (Rhodopsin) Human - scFv16 - 1-(4-Methylpyridin-2-yl)-3-[3-(trifluoromethyl)phenyl]thiourea pubchem
small-molecule Agonist - - Yang Z, Wang JY, Yang F, Zhu KK, Wang GP, Guan Y, Ning SL, Lu Y, Li Y, Zhang C, Zheng Y, Zhou SH, Wang XW, Wang MW, Xiao P, Yi F, Zhang C, Zhang PJ, Xu F, Liu BH, Zhang H, Yu X, Gao N, Sun JP 10.1038/S41589-023-01456-6 2024-01-03
Gi/o αi1 Human - 66 β1 Human γ2 Human Cryo-EM 8FYE - 2.9 5HT1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - CHEMBL352186 chembl_ligand pubchem
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 - 58 β1 Human γ2 Human Cryo-EM 8GFY - 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
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8J6J 8J6J_refined 2.8 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - scFv16 - GSK256073 pubchem gtoplig chembl_ligand
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 2024-01-10
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8UH3 - 3.3 5HT1E 5-HT1E 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - SETIPTILINE chembl_ligand pubchem
small-molecule Agonist 5-hydroxytryptamine, tryptamine small-molecule Zilberg G, Parpounas AK, Warren AL, Fiorillo B, Provasi D, Filizola M, Wacker D 10.1126/SCIADV.ADK4855 2024-05-01
Gs αs Human GTP bound, Class R 72 β1 Human γ2 Human Cryo-EM 8UO2 8UO2_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
Gi/o αi1 Human - 61 β1 Rat γ2 Bovine Cryo-EM 8XOS - 3.2 PAR1 PAR1 Proteinase-activated A (Rhodopsin) Human - scFv16 - Tethered agonist
peptide Agonist thrombin peptide - - 2024-09-18
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 8ZR5 - 3.3 GP119 GPR119 GPR18, GPR55 and GPR119 A (Rhodopsin) Human - Nanobody-35 - DS-8500a pubchem gtoplig
small-molecule Agonist N-palmitoylethanolamine, anandamide, N-oleoylethanolamide, SEA small-molecule - - 2024-06-19
Gi/o αi2 Human - 63 β1 Human γ2 Human Cryo-EM 8K6N 8K6N_refined 3.2 NPY2R Y2 Neuropeptide Y A (Rhodopsin) Human - scFv16 - 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 - - 2024-07-31
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 9IQT 9IQT_refined 2.9 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 Liu Y, Zhou Z, Guan F, Han Z, Zhu C, Ye S, Yu X, Qiao A 10.1016/J.JMB.2024.168795 2024-10-02
Gs αs2 Bovine - 100 - - - - X-ray 1AZS - 2.3 - - - - - - - VC1
IIC2 		- - - - - Tesmer JJ, Sunahara RK, Gilman AG, Sprang SR 9417641 1998-02-25
Gs αs2 Bovine - 100 - - - - X-ray 1AZT - 2.3 - - - - - - - - - - - - - Sunahara RK, Tesmer JJ, Gilman AG, Sprang SR 9395396 1998-02-25
Gs αs2 Bovine - 100 - - - - X-ray 1CJK - 3.0 - - - - - - - Adenylate cyclase
type V
ADENYLATE CYCLASE
TYPE II 		- - - - - Tesmer JJ, Sunahara RK, Johnson RA, Gosselin G, Gilman AG, Sprang SR 10427002 1999-08-31
Gs αs2 Bovine - 100 - - - - X-ray 1CJT - 2.8 - - - - - - - Adenylate cyclase
type V
ADENYLATE CYCLASE
TYPE II 		- - - - - Tesmer JJ, Sunahara RK, Johnson RA, Gosselin G, Gilman AG, Sprang SR 10427002 1999-08-31
Gs αs2 Bovine - 100 - - - - X-ray 1CJU - 2.8 - - - - - - - Adenylate cyclase
type V
ADENYLATE CYCLASE
TYPE II 		- - - - - Tesmer JJ, Sunahara RK, Johnson RA, Gosselin G, Gilman AG, Sprang SR 10427002 1999-08-31
Gs αs2 Bovine - 100 - - - - X-ray 1CJV - 3.0 - - - - - - - Adenylate cyclase
type V
ADENYLATE CYCLASE
TYPE II 		- - - - - Tesmer JJ, Sunahara RK, Johnson RA, Gosselin G, Gilman AG, Sprang SR 10427002 1999-08-31
Gs αs2 Bovine - 100 - - - - X-ray 1CS4 - 2.5 - - - - - - - TYPE V ADENYLATE CYCLASE
TYPE II ADENYLATE CYCLASE 		- - - - - Tesmer JJ, Dessauer CW, Sunahara RK, Murray LD, Johnson RA, Gilman AG, Sprang SR 11087399 2001-01-10
Gs αs2 Bovine - 96 - - - - X-ray 1CUL - 2.4 - - - - - - - TYPE V ADENYLYL CYCLASE
TYPE II ADENYLYL CYCLASE 		- - - - - Tesmer JJ, Dessauer CW, Sunahara RK, Murray LD, Johnson RA, Gilman AG, Sprang SR 11087399 2001-01-10
Gs αs2 Bovine - 100 - - - - X-ray 1TL7 - 2.8 - - - - - - - Adenylate cyclase
type V
Adenylate cyclase
type II 		- - - - - Mou TC, Gille A, Fancy DA, Seifert R, Sprang SR 15591060 2004-12-14
Gs αs2 Bovine - 100 - - - - X-ray 1U0H - 2.9 - - - - - - - Adenylate cyclase
type V
Adenylate cyclase
type II 		- - - - - Mou TC, Gille A, Fancy DA, Seifert R, Sprang SR 15591060 2004-12-14
Gs αs2 Bovine - 100 - - - - X-ray 2GVD - 2.9 - - - - - - - Adenylate cyclase type 5
Adenylate cyclase type 2 		- - - - - Mou TC, Gille A, Suryanarayana S, Richter M, Seifert R, Sprang SR 16766715 2006-07-04
Gs αs2 Bovine - 100 - - - - X-ray 2GVZ - 3.3 - - - - - - - Adenylate cyclase type 5
Adenylate cyclase type 2 		- - - - - Mou TC, Gille A, Suryanarayana S, Richter M, Seifert R, Sprang SR 16766715 2006-07-04
Gs αs2 Bovine - 100 - - - - X-ray 3C14 - 2.7 - - - - - - - Adenylate cyclase type 5
Adenylate cyclase type 2 		- - - - - Mou TC, Masada N, Cooper DM, Sprang SR 19243146 2009-02-03
Gs αs2 Bovine - 100 - - - - X-ray 3C15 - 2.8 - - - - - - - Adenylate cyclase type 5
Adenylate cyclase type 2 		- - - - - Mou TC, Masada N, Cooper DM, Sprang SR 19243146 2009-02-03
Gs αs2 Bovine - 100 - - - - X-ray 3C16 - 2.9 - - - - - - - Adenylate cyclase type 5
Adenylate cyclase type 2 		- - - - - Mou TC, Masada N, Cooper DM, Sprang SR 19243146 2009-02-03
Gs αs2 Bovine - 100 - - - - X-ray 3G82 - 3.1 - - - - - - - Adenylate cyclase type 5
Adenylate cyclase type 2 		- - - - - - - 2010-02-16
Gs αs2 Bovine - 100 - - - - X-ray 3MAA - 3.0 - - - - - - - Adenylate cyclase type 5
Adenylate cyclase type 2 		- - - - - Mou TC, Masada N, Cooper DM, Sprang SR 19243146 2010-04-07
Gs αs2 Bovine - 100 - - - - Cryo-EM 6R3Q - 3.4 - - - - - - - Adenylate cyclase 9 - - - - - Qi C, Sorrentino S, Medalia O, Korkhov VM 31023924 2019-05-08
Gs αs2 Bovine - 100 - - - - Cryo-EM 6R4O - 4.2 - - - - - - - Adenylate cyclase 9 - - - - - Qi C, Sorrentino S, Medalia O, Korkhov VM 31023924 2019-05-08
Gs αs2 Bovine - 100 - - - - Cryo-EM 6R4P - 3.1 - - - - - - - Adenylate cyclase 9 - - - - - Qi C, Sorrentino S, Medalia O, Korkhov VM 31023924 2019-05-08
Gs αs2 Bovine - 100 - - - - Cryo-EM 7PDE - 4.5 - - - - - - - Adenylate cyclase 9 - - - - - Qi C, Lavriha P, Mehta V, Khanppnavar B, Mohammed I, Li Y, Lazaratos M, Schaefer JV, Dreier B, Pluckthun A, Bondar AN, Dessauer CW, Korkhov VM 35210418 2022-01-19
Gs αs2 Bovine - 100 - - - - Cryo-EM 7PDF - 3.8 - - - - - - - Adenylate cyclase 9 - - - - - Qi C, Lavriha P, Mehta V, Khanppnavar B, Mohammed I, Li Y, Lazaratos M, Schaefer JV, Dreier B, Pluckthun A, Bondar AN, Dessauer CW, Korkhov VM 35210418 2022-01-26
Gs αs2 Bovine - 100 - - - - Cryo-EM 8BUZ - 3.5 - - - - - - - Adenylate cyclase type 8 - - - - - Khanppnavar B, Schuster D, Lavriha P, Uliana F, Ozel M, Mehta V, Leitner A, Picotti P, Korkhov VM 38351373 2023-12-13
Gs αs2 Bovine - 100 - - - - Cryo-EM 8BV5 - 3.5 - - - - - - - Adenylate cyclase type 8 - - - - - Khanppnavar B, Schuster D, Lavriha P, Uliana F, Ozel M, Mehta V, Leitner A, Picotti P, Korkhov VM 38351373 2024-01-17
Gs αs2 Human - 96 - - - - X-ray 6AU6 - 1.7 - - - - - - - - - - - - - Hu Q, Shokat KM 29628140 2018-05-09
Gs αs2 Human - 97 β1 Human γ2 Human X-ray 6EG8 - 2.8 - - - - - - - - - - - - - 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 31080070 2019-06-05
Gs αs2 Human - 96 - - - - X-ray 7BPH - 1.6 - - - - - - - GN13 - - - - - Dai SA, Hu Q, Gao R, Blythe EE, Touhara KK, Peacock H, Zhang Z, von Zastrow M, Suga H, Shokat KM 36170854 2021-03-31
Gs αs2 Human - 88 - - - - X-ray 7E5E - 2.0 - - - - - - - GD20 - - - - - Dai SA, Hu Q, Gao R, Blythe EE, Touhara KK, Peacock H, Zhang Z, von Zastrow M, Suga H, Shokat KM 36170854 2022-03-02
Gs αs2 Human - 96 - - - - Cryo-EM 8EL7 - 2.8 - - - - - - - Isoform 1 of Synembryn-B - - - - - Papasergi-Scott MM, Kwarcinski FE, Yu M, Panova O, Ovrutsky AM, Skiniotis G, Tall GG 36931277 2023-03-01
Gs αs2 Human - 96 β1 Human γ2 Human Cryo-EM 8GG7 - 3.3 - - - - - - - Beta-2 adrenergic receptor - - - - - 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 38480881 2024-03-06
Gs αl Mouse - 100 - - - - X-ray 8HTG - 2.9 - - - - - - - - - - - - - Choi C, Bae J, Kim S, Lee S, Kang H, Kim J, Bang I, Kim K, Huh WK, Seok C, Park H, Im W, Choi HJ 38062020 2023-12-20
Gs αl Human - 100 - - - - Cryo-EM 8EL8 - 3.2 - - - - - - - Isoform 1 of Synembryn-B - - - - - Papasergi-Scott MM, Kwarcinski FE, Yu M, Panova O, Ovrutsky AM, Skiniotis G, Tall GG 36931277 2023-03-01
Gi/o αi1 Rat - 100 - - - - X-ray 1AGR - 2.8 - - - - - - - RGS4 - - - - - Tesmer JJ, Berman DM, Gilman AG, Sprang SR 9108480 1997-06-16
Gi/o αi1 Rat - 100 - - - - X-ray 1AS0 - 2.0 - - - - - - - - - - - - - Raw AS, Coleman DE, Gilman AG, Sprang SR 9398294 1997-11-12
Gi/o αi1 Rat - 100 - - - - X-ray 1AS2 - 2.8 - - - - - - - - - - - - - Raw AS, Coleman DE, Gilman AG, Sprang SR 9398294 1997-11-12
Gi/o αi1 Rat - 100 - - - - X-ray 1AS3 - 2.4 - - - - - - - - - - - - - Raw AS, Coleman DE, Gilman AG, Sprang SR 9398294 1997-11-12
Gi/o αi1 Rat - 89 - - - - X-ray 1BH2 - 2.1 - - - - - - - - - - - - - Posner BA, Mixon MB, Wall MA, Sprang SR, Gilman AG 9705312 1998-11-04
Gi/o αi1 Rat - 100 - - - - X-ray 1BOF - 2.2 - - - - - - - - - - - - - Coleman DE, Sprang SR 9772163 1999-01-06
Gi/o αi1 Rat - 100 - - - - X-ray 1CIP - 1.5 - - - - - - - - - - - - - Coleman DE, Sprang SR 10358003 1999-04-09
Gi/o αi1 Rat - 92 - - - - X-ray 1FQJ - 2.0 - - - - - - - Regulator of G-protein signaling 9 - - - - - Slep KC, Kercher MA, He W, Cowan CW, Wensel TG, Sigler PB 11234020 2001-02-28
Gi/o αi1 Rat - 92 - - - - X-ray 1FQK - 2.3 - - - - - - - Regulator of G-protein signaling 9 - - - - - Slep KC, Kercher MA, He W, Cowan CW, Wensel TG, Sigler PB 11234020 2001-02-28
Gi/o αi1 Rat - 100 - - - - X-ray 1GDD - 2.2 - - - - - - - - - - - - - Mixon MB, Lee E, Coleman DE, Berghuis AM, Gilman AG, Sprang SR 7481799 1995-11-27
Gi/o αi1 Rat - 100 - - - - X-ray 1GFI - 2.2 - - - - - - - - - - - - - Coleman DE, Berghuis AM, Lee E, Linder ME, Gilman AG, Sprang SR 8073283 1995-03-31
Gi/o αi1 Rat - 100 β1 Bovine γ2 Bovine X-ray 1GG2 - 2.4 - - - - - - - - - - - - - Wall MA, Coleman DE, Lee E, Iniguez-Lluhi JA, Posner BA, Gilman AG, Sprang SR 8521505 1997-02-12
Gi/o αi1 Rat - 100 - - - - X-ray 1GIA - 2.0 - - - - - - - - - - - - - Coleman DE, Berghuis AM, Lee E, Linder ME, Gilman AG, Sprang SR 8073283 1994-09-30
Gi/o αi1 Rat - 100 - - - - X-ray 1GIL - 2.3 - - - - - - - - - - - - - Coleman DE, Berghuis AM, Lee E, Linder ME, Gilman AG, Sprang SR 8073283 1995-02-14
Gi/o αi1 Rat - 100 - - - - X-ray 1GIT - 2.6 - - - - - - - - - - - - - Berghuis AM, Lee E, Raw AS, Gilman AG, Sprang SR 8939752 1997-02-12
Gi/o αi1 Rat - 100 β1 Bovine γ2 Bovine X-ray 1GP2 - 2.3 - - - - - - - - - - - - - Wall MA, Coleman DE, Lee E, Iniguez-Lluhi JA, Posner BA, Gilman AG, Sprang SR 8521505 1997-02-12
Gi/o αi1 Rat - 96 - - - - X-ray 1SHZ - 2.9 - - - - - - - Guanine Nucleotide-Binding Protein Galpha(13):Galpha(i1) Chimera
Rho guanine nucleotide exchange factor 1 		- - - - - Chen Z, Singer WD, Sternweis PC, Sprang SR 15665872 2005-01-18
Gi/o αi1 Rat - 100 - - - - X-ray 1SVK - 2.0 - - - - - - - - - - - - - Thomas CJ, Du X, Li P, Wang Y, Ross EM, Sprang SR 15128951 2004-06-01
Gi/o αi1 Rat - 100 - - - - X-ray 1SVS - 1.5 - - - - - - - - - - - - - Thomas CJ, Du X, Li P, Wang Y, Ross EM, Sprang SR 15128951 2004-06-01
Gi/o αi1 Rat - 100 β1 Bovine γ2 Bovine X-ray 2BCJ - 3.1 - - - - - - - G-protein-coupled receptor kinase 2 - - - - - Tesmer VM, Kawano T, Shankaranarayanan A, Kozasa T, Tesmer JJ 16339447 2005-12-20
Gi/o αi1 Rat - 100 - - - - X-ray 2RGN - 3.5 - - - - - - - Rho guanine nucleotide exchange factor 25
Transforming protein RhoA 		- - - - - Lutz S, Shankaranarayanan A, Coco C, Ridilla M, Nance MR, Vettel C, Baltus D, Evelyn CR, Neubig RR, Wieland T, Tesmer JJ 18096806 2008-01-15
Gi/o αi1 Rat - 100 - - - - X-ray 2ZJY - 2.8 - - - - - - - - - - - - - - - 2009-03-24
Gi/o αi1 Rat - 100 - - - - X-ray 2ZJZ - 2.6 - - - - - - - - - - - - - - - 2009-03-24
Gi/o αi1 Rat - 100 β1 Bovine γ2 Bovine X-ray 3AH8 - 2.9 - - - - - - - YM-254890 - - - - - Nishimura A, Kitano K, Takasaki J, Taniguchi M, Mizuno N, Tago K, Hakoshima T, Itoh H 20639466 2010-07-21
Gi/o αi1 Rat - 100 - - - - X-ray 3D7M - 2.9 - - - - - - - - - - - - - Preininger AM, Funk MA, Oldham WM, Meier SM, Johnston CA, Adhikary S, Kimple AJ, Siderovski DP, Hamm HE, Iverson TM 19222191 2009-03-03
Gi/o αi1 Rat - 100 - - - - X-ray 3FFA - 2.3 - - - - - - - - - - - - - Kapoor N, Menon ST, Chauhan R, Sachdev P, Sakmar TP 19703466 2009-10-06
Gi/o αi1 Rat - 100 - - - - X-ray 3FFB - 2.6 - - - - - - - - - - - - - Kapoor N, Menon ST, Chauhan R, Sachdev P, Sakmar TP 19703466 2009-10-06
Gi/o αi1 Rat - 100 - - - - X-ray 3V00 - 2.9 - - - - - - - - - - - - - Singh G, Ramachandran S, Cerione RA 22448927 2012-04-18
Gi/o αi1 Rat - 100 - - - - X-ray 4N0D - 1.6 - - - - - - - - - - - - - Thaker TM, Sarwar M, Preininger AM, Hamm HE, Iverson TM 24596087 2014-03-12
Gi/o αi1 Rat - 100 - - - - X-ray 4N0E - 2.1 - - - - - - - - - - - - - Thaker TM, Sarwar M, Preininger AM, Hamm HE, Iverson TM 24596087 2014-03-12
Gi/o αi1 Rat - 100 - - - - X-ray 4PAM - 2.1 - - - - - - - - - - - - - Kaya AI, Lokits AD, Gilbert JA, Iverson TM, Meiler J, Hamm HE 25037222 2014-07-30
Gi/o αi1 Rat - 100 - - - - X-ray 4PAN - 2.4 - - - - - - - - - - - - - Kaya AI, Lokits AD, Gilbert JA, Iverson TM, Meiler J, Hamm HE 25037222 2014-07-30
Gi/o αi1 Rat - 100 - - - - X-ray 4PAO - 2.0 - - - - - - - - - - - - - Kaya AI, Lokits AD, Gilbert JA, Iverson TM, Meiler J, Hamm HE 25037222 2014-07-30
Gi/o αi1 Rat - 100 - - - - X-ray 4PAQ - 2.0 - - - - - - - - - - - - - Kaya AI, Lokits AD, Gilbert JA, Iverson TM, Meiler J, Hamm HE 25037222 2014-07-30
Gi/o αi1 Rat - 100 - - - - X-ray 5KDL - 2.7 - - - - - - - - - - - - - Kaya AI, Lokits AD, Gilbert JA, Iverson TM, Meiler J, Hamm HE 27462082 2016-08-03
Gi/o αi1 Rat - 100 β1 Bovine γT1 Bovine X-ray 5KDO - 1.9 - - - - - - - - - - - - - Kaya AI, Lokits AD, Gilbert JA, Iverson TM, Meiler J, Hamm HE 27462082 2016-08-03
Gi/o αi1 Rat - 100 - - - - X-ray 6M8H - 2.1 - - - - - - - - - - - - - - - 2019-08-21
Gi/o αi1 Rat - 100 - - - - X-ray 6TYL - 3.3 - - - - - - Nanobody A
Nanobody B
Nanobody C 		Resistance to inhibitors of cholinesterase 8 homolog A (C. elegans) - - - - - McClelland LJ, Zhang K, Mou TC, Johnston J, Yates-Hansen C, Li S, Thomas CJ, Doukov TI, Triest S, Wohlkonig A, Tall GG, Steyaert J, Chiu W, Sprang SR 32103024 2020-03-11
Gi/o αi1 Rat - 91 - - - - Cryo-EM 6UKT - 3.9 - - - - - - NB8109
NB8117
NB8119
NB9156 		Resistance to inhibitors of cholinesterase 8 homolog A (C. elegans) - - - - - McClelland LJ, Zhang K, Mou TC, Johnston J, Yates-Hansen C, Li S, Thomas CJ, Doukov TI, Triest S, Wohlkonig A, Tall GG, Steyaert J, Chiu W, Sprang SR 32103024 2020-03-11
Gi/o αi1 Human - 92 - - - - X-ray 1KJY - 2.7 - - - - - - - Regulator of G-protein signaling 14 - - - - - Kimple RJ, Kimple ME, Betts L, Sondek J, Siderovski DP 11976690 2002-05-08
Gi/o αi1 Human - 93 - - - - X-ray 1Y3A - 2.5 - - - - - - - KB752 peptide - - - - - Johnston CA, Willard FS, Jezyk MR, Fredericks Z, Bodor ET, Jones MB, Blaesius R, Watts VJ, Harden TK, Sondek J, Ramer JK, Siderovski DP 16004878 2005-07-12
Gi/o αi1 Human - 88 - - - - X-ray 2G83 - 2.8 - - - - - - - KB-1753 phage display peptide - - - - - Johnston CA, Lobanova ES, Shavkunov AS, Low J, Ramer JK, Blaesius R, Fredericks Z, Willard FS, Kuhlman B, Arshavsky VY, Siderovski DP 16981699 2006-10-10
Gi/o αi1 Human - 91 - - - - X-ray 2GTP - 2.6 - - - - - - - Regulator of G-protein signaling 1 - - - - - Soundararajan M, Willard FS, Kimple AJ, Turnbull AP, Ball LJ, Schoch GA, Gileadi C, Fedorov OY, Dowler EF, Higman VA, Hutsell SQ, Sundstrom M, Doyle DA, Siderovski DP 18434541 2006-05-23
Gi/o αi1 Human - 92 - - - - X-ray 2IK8 - 2.7 - - - - - - - Regulator of G-protein signaling 16 - - - - - Soundararajan M, Willard FS, Kimple AJ, Turnbull AP, Ball LJ, Schoch GA, Gileadi C, Fedorov OY, Dowler EF, Higman VA, Hutsell SQ, Sundstrom M, Doyle DA, Siderovski DP 18434541 2006-11-21
Gi/o αi1 Human - 92 - - - - X-ray 2OM2 - 2.2 - - - - - - - Regulator of G-protein signalling 14 GoLoco motif peptide - - - - - Sammond DW, Eletr ZM, Purbeck C, Kimple RJ, Siderovski DP, Kuhlman B 17603074 2007-07-10
Gi/o αi1 Human - 92 - - - - X-ray 2XNS - 3.4 - - - - - - - Regulator of G-protein signaling 14 - - - - - Sammond DW, Bosch DE, Butterfoss GL, Purbeck C, Machius M, Siderovski DP, Kuhlman B 21388199 2011-06-08
Gi/o αi1 Human - 93 - - - - X-ray 3ONW - 2.4 - - - - - - - Regulator of G-protein signaling 14 - - - - - Bosch DE, Kimple AJ, Sammond DW, Muller RE, Miley MJ, Machius M, Kuhlman B, Willard FS, Siderovski DP 21115486 2010-11-24
Gi/o αi1 Human - 92 - - - - X-ray 3QE0 - 3.0 - - - - - - - KB752 peptide - - - - - Bosch DE, Willard FS, Ramanujam R, Kimple AJ, Willard MD, Naqvi NI, Siderovski DP 22383884 2012-01-25
Gi/o αi1 Human - 93 - - - - X-ray 3QI2 - 2.8 - - - - - - - Regulator of G-protein signaling 14 - - - - - Bosch DE, Willard FS, Ramanujam R, Kimple AJ, Willard MD, Naqvi NI, Siderovski DP 22383884 2012-02-01
Gi/o αi1 Human - 100 - - - - X-ray 3UMR - 2.0 - - - - - - - - - - - - - - - 2012-10-24
Gi/o αi1 Human - 100 - - - - X-ray 3UMS - 2.3 - - - - - - - - - - - - - - - 2012-02-08
Gi/o αi1 Human - 93 - - - - X-ray 4G5Q - 2.9 - - - - - - - G-protein-signaling modulator 2 - - - - - - - 2012-09-05
Gi/o αi1 Human - 100 β1 Rat γ2 Bovine X-ray 5TDH - 3.0 - - - - - - - - - - - - - Liu P, Jia MZ, Zhou XE, De Waal PW, Dickson BM, Liu B, Hou L, Yin YT, Kang YY, Shi Y, Melcher K, Xu HE, Jiang Y 27498775 2016-11-09
Gi/o αi1 Human - 100 β1 Human γ2 Human X-ray 6CRK - 2.0 - - - - - - single-chain Fv - - - - - - Maeda S, Koehl A, Matile H, Hu H, Hilger D, Schertler GFX, Manglik A, Skiniotis G, Dawson RJP, Kobilka BK 30213947 2018-10-24
Gi/o αi1 Human - 100 - - - - Cryo-EM 6VU8 - 4.1 - - - - - - - Resistance to inhibitors of cholinesterase 8 homolog A (C. elegans) - - - - - Seven AB, Hilger D, Papasergi-Scott MM, Zhang L, Qu Q, Kobilka BK, Tall GG, Skiniotis G 32126208 2020-03-18
Gi/o αi1 Human - 100 β1 Human γ2 Human Cryo-EM 7RKX - 3.1 - - - - - - Antibody fragment scFv16 G-protein coupled receptor homolog US27 - - - - - - - 2022-01-26
Gi/o αi1 Human - 100 β1 Human γ2 Human Cryo-EM 7RKY - 3.8 - - - - - - Antibody fragment scFv16 G-protein coupled receptor homolog US27 - - - - - - - 2022-01-26
Gi/o αi1 Human - 100 β1 Human γ2 Human Cryo-EM 7YOO - 3.1 - - - - - - single-chain antibody Fv fragment (scFv16) Neuropeptide Y
Neuropeptide Y receptor type 2 		- - - - - Kang H, Park C, Choi YK, Bae J, Kwon S, Kim J, Choi C, Seok C, Im W, Choi HJ 36525977 2023-03-22
Gi/o αi1 Human - 100 β1 Human γ2 Human Cryo-EM 8HNL - 3.0 - - - - - - single-chain variable fragment scFv16 - - - - - - Jiao H, Pang B, Liu A, Chen Q, Pan Q, Wang X, Xu Y, Chiang YC, Ren R, Hu H 38177682 2023-11-29
Gi/o αi3 Rat - 99 - - - - X-ray 6MHE - 2.2 - - - - - - - KB752 peptide - - - - - Kalogriopoulos NA, Rees SD, Ngo T, Kopcho NJ, Ilatovskiy AV, Sun N, Komives EA, Chang G, Ghosh P, Kufareva I 31363053 2019-07-31
Gi/o αi3 Rat - 99 - - - - X-ray 6MHF - 2.0 - - - - - - - Girdin - - - - - Kalogriopoulos NA, Rees SD, Ngo T, Kopcho NJ, Ilatovskiy AV, Sun N, Komives EA, Chang G, Ghosh P, Kufareva I 31363053 2019-07-31
Gi/o αi3 Human - 91 - - - - X-ray 2IHB - 2.7 - - - - - - - Regulator of G-protein signalling 10 - - - - - Soundararajan M, Willard FS, Kimple AJ, Turnbull AP, Ball LJ, Schoch GA, Gileadi C, Fedorov OY, Dowler EF, Higman VA, Hutsell SQ, Sundstrom M, Doyle DA, Siderovski DP 18434541 2006-11-21
Gi/o αi3 Human - 99 - - - - X-ray 2ODE - 1.9 - - - - - - - Regulator of G-protein signaling 8 - - - - - Soundararajan M, Willard FS, Kimple AJ, Turnbull AP, Ball LJ, Schoch GA, Gileadi C, Fedorov OY, Dowler EF, Higman VA, Hutsell SQ, Sundstrom M, Doyle DA, Siderovski DP 18434541 2007-02-06
Gi/o αi3 Human - 99 - - - - X-ray 2V4Z - 2.8 - - - - - - - REGULATOR OF G-PROTEIN SIGNALING 2 - - - - - Kimple AJ, Soundararajan M, Hutsell SQ, Roos AK, Urban DJ, Setola V, Temple BR, Roth BL, Knapp S, Willard FS, Siderovski DP 19478087 2008-11-04
Gi/o αi3 Human - 93 - - - - X-ray 4G5O - 2.9 - - - - - - - G-protein-signaling modulator 2 - - - - - - - 2012-09-05
Gi/o αi3 Human - 93 - - - - X-ray 4G5R - 3.5 - - - - - - - G-protein-signaling modulator 2 - - - - - - - 2012-09-05
Gi/o αi3 Human - 93 - - - - X-ray 4G5S - 3.6 - - - - - - - G-protein-signaling modulator 2 - - - - - - - 2012-09-05
Gi/o αi3 Human - 100 - - - - Cryo-EM 7X6I - 3.9 - - - - - - - Short transient receptor potential channel 5 - - - - - Won J, Kim J, Jeong H, Kim J, Feng S, Jeong B, Kwak M, Ko J, Im W, So I, Lee HH 37137991 2023-04-26
Gi/o αi3 Human - 100 - - - - Cryo-EM 8GVX - 3.9 - - - - - - - Short transient receptor potential channel 5 - - - - - Won J, Kim J, Jeong H, Kim J, Feng S, Jeong B, Kwak M, Ko J, Im W, So I, Lee HH 37137991 2023-05-24
Gi/o αi3 Human - 91 - - - - X-ray 8OY1 - 3.3 - - - - - - - - - - - - - - - 2024-05-15
Gi/o αt1 Bovine - 100 β1 Bovine γT1 Bovine X-ray 1GOT - 2.0 - - - - - - - - - - - - - Lambright DG, Sondek J, Bohm A, Skiba NP, Hamm HE, Sigler PB 8552184 1997-03-12
Gi/o αt1 Bovine - 93 - - - - X-ray 1TAD - 1.7 - - - - - - - - - - - - - Sondek J, Lambright DG, Noel JP, Hamm HE, Sigler PB 7969474 1995-05-08
Gi/o αt1 Bovine - 93 - - - - X-ray 1TAG - 1.8 - - - - - - - - - - - - - Lambright DG, Noel JP, Hamm HE, Sigler PB 8208289 1995-02-07
Gi/o αt1 Bovine - 93 - - - - X-ray 1TND - 2.2 - - - - - - - - - - - - - Noel JP, Hamm HE, Sigler PB 8259210 1994-07-31
Gi/o αt1 Bovine - 100 - - - - Cryo-EM 7JSN - 3.2 - - - - - - - Rod cGMP-specific 3'
5'-cyclic phosphodiesterase subunit alpha
Rod cGMP-specific 3'
5'-cyclic phosphodiesterase subunit beta 		- - - - - Gao Y, Eskici G, Ramachandran S, Poitevin F, Seven AB, Panova O, Skiniotis G, Cerione RA 33007200 2020-10-21
Gi/o αt1 Human - 3 - - - - X-ray 3RBQ - 2.0 - - - - - - - Protein unc-119 homolog A - - - - - Zhang H, Constantine R, Vorobiev S, Chen Y, Seetharaman J, Huang YJ, Xiao R, Montelione GT, Gerstner CD, Davis MW, Inana G, Whitby FG, Jorgensen EM, Hill CP, Tong L, Baehr W 21642972 2011-06-08
Gi/o αt2 Human - 100 - - - - X-ray 6N84 - 1.8 - - - - - - - - - - - - - Srivastava D, Gakhar L, Artemyev NO 31300652 2019-07-10
Gi/o αt2 Human - 100 - - - - X-ray 6N85 - 2.5 - - - - - - - Synembryn-A - - - - - Srivastava D, Gakhar L, Artemyev NO 31300652 2019-07-10
Gi/o αo Mouse - 94 - - - - X-ray 3C7K - 2.9 - - - - - - - Regulator of G-protein signaling 16 - - - - - Slep KC, Kercher MA, Wieland T, Chen CK, Simon MI, Sigler PB 18434540 2008-05-06
Gi/o αo Human - 64 β1 Human γ2 Human Cryo-EM 8IEC - 3.2 - - - - - - Single-chain variable fragment scFv16 - - - - - - Shin J, Park J, Jeong J, Lam JH, Qiu X, Wu D, Kim K, Lee JY, Robinson CV, Hyun J, Katritch V, Kim KP, Cho Y 38332368 2024-02-14
Gq/11 αq Mouse - 97 - - - - X-ray 4EKC - 7.4 - - - - - - - Regulator of G-protein signaling 2 - - - - - Nance MR, Kreutz B, Tesmer VM, Sterne-Marr R, Kozasa T, Tesmer JJ 23434405 2013-01-30
Gq/11 αq Mouse - 97 - - - - X-ray 4EKD - 2.7 - - - - - - - Regulator of G-protein signaling 2 - - - - - Nance MR, Kreutz B, Tesmer VM, Sterne-Marr R, Kozasa T, Tesmer JJ 23434405 2013-01-30
Gq/11 αq Mouse - 98 - - - - X-ray 4GNK - 4.0 - - - - - - - 1-phosphatidylinositol 4
5-bisphosphate phosphodiesterase beta-3 		- - - - - Lyon AM, Dutta S, Boguth CA, Skiniotis G, Tesmer JJ 23377541 2013-02-06
Gq/11 αq Mouse - 100 - - - - X-ray 4QJ3 - 3.0 - - - - - - - 1-phosphatidylinositol 4
5-bisphosphate phosphodiesterase beta-3 		- - - - - Lyon AM, Begley JA, Manett TD, Tesmer JJG 25435326 2014-10-22
Gq/11 αq Mouse - 100 - - - - X-ray 4QJ4 - 3.3 - - - - - - - 1-phosphatidylinositol 4
5-bisphosphate phosphodiesterase beta-3 		- - - - - Lyon AM, Begley JA, Manett TD, Tesmer JJG 25435326 2014-10-22
Gq/11 αq Mouse - 100 - - - - X-ray 4QJ5 - 3.4 - - - - - - - 1-phosphatidylinositol 4
5-bisphosphate phosphodiesterase beta-3 		- - - - - Lyon AM, Begley JA, Manett TD, Tesmer JJG 25435326 2014-10-22
Gq/11 αq Mouse - 87 - - - - X-ray 5DO9 - 2.6 - - - - - - - Regulator of G-protein signaling 8 - - - - - Taylor VG, Bommarito PA, Tesmer JJ 26755720 2016-01-20
Gq/11 αq Mouse - 91 - - - - X-ray 7SQ2 - 2.6 - - - - - - - 1-phosphatidylinositol 4
5-bisphosphate phosphodiesterase beta-3 		- - - - - Waldo GL, Ricks TK, Hicks SN, Cheever ML, Kawano T, Tsuboi K, Wang X, Montell C, Kozasa T, Sondek J, Harden TK 20966218 2021-11-17
Gq/11 αq Human - 100 - - - - Cryo-EM 6VU5 - 3.5 - - - - - - - Resistance to inhibitors of cholinesterase-8A (Ric-8A) - - - - - Seven AB, Hilger D, Papasergi-Scott MM, Zhang L, Qu Q, Kobilka BK, Tall GG, Skiniotis G 32126208 2020-03-18
Gq/11 αq Human - 98 - - - - Cryo-EM 8JPE - 2.9 - - - - - - - - - - - - - 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 37532940 2023-08-09
Gq/11 αq Human - 99 - - - - Cryo-EM 8UQN - 3.4 - - - - - - - 1-phosphatidylinositol 4
5-bisphosphate phosphodiesterase beta-3 		- - - - - Falzone ME, MacKinnon R 37991948 2023-12-06
Gq/11 αq Human - 99 β1 Human γ2 Human Cryo-EM 8UQO - 3.4 - - - - - - - 1-phosphatidylinositol 4
5-bisphosphate phosphodiesterase beta-3 		- - - - - Falzone ME, MacKinnon R 37991948 2023-12-06
G12/13 α12 Mouse - 95 - - - - X-ray 1ZCA - 2.9 - - - - - - - - - - - - - Kreutz B, Yau DM, Nance MR, Tanabe S, Tesmer JJ, Kozasa T 16388592 2005-11-15
G12/13 α13 Mouse - 96 - - - - X-ray 1ZCB - 2.0 - - - - - - - - - - - - - Kreutz B, Yau DM, Nance MR, Tanabe S, Tesmer JJ, Kozasa T 16388592 2005-11-15
G12/13 α13 Mouse - 96 - - - - X-ray 3AB3 - 2.4 - - - - - - - Rho guanine nucleotide exchange factor 1 - - - - - Hajicek N, Kukimoto-Niino M, Mishima-Tsumagari C, Chow CR, Shirouzu M, Terada T, Patel M, Yokoyama S, Kozasa T 21507947 2010-12-29
G12/13 α13 Mouse - 90 - - - - X-ray 3CX6 - 2.5 - - - - - - - Rho guanine nucleotide exchange factor 11 - - - - - Chen Z, Singer WD, Danesh SM, Sternweis PC, Sprang SR 18940608 2008-10-28
G12/13 α13 Mouse - 90 - - - - X-ray 3CX7 - 2.3 - - - - - - - Glutamate Transporter Associated Protein 48 - - - - - Chen Z, Singer WD, Danesh SM, Sternweis PC, Sprang SR 18940608 2008-10-28
G12/13 α13 Mouse - 90 - - - - X-ray 3CX8 - 2.0 - - - - - - - Rho guanine nucleotide exchange factor 11 - - - - - Chen Z, Singer WD, Danesh SM, Sternweis PC, Sprang SR 18940608 2008-10-28