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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
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
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 - 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 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
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 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 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
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 - 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 - 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 - 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
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 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
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
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 - 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 - 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 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 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
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
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 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
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 - 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
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 - 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 - 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
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 - 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
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
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 - 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 - 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 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 - 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 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 - 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
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
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 2-arachidonoylglycerol, 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
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 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
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 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
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
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 - - - - 2019-07-24
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
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 - 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
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
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
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 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 - 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 - 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 - 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 - 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 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 - 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 - 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 - 61 β1 Human γ2 Human Cryo-EM 6XBK - 3.2 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 - 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
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 - 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
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
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
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
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 - 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 - - 2021-03-10
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
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 - 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
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 - 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
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 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 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
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 - 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
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 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
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 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 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 - 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
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
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
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
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 - 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 - 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
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 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 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 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
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
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
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 - 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
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
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 - 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
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
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
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
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
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
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 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 - 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 - 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
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
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
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
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
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 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 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
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
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
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
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
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 - 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
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
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 - 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
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 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 - 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 - 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 - 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
Gs αs Bovine - 91 β1 Rat γ2 Bovine Cryo-EM 7FII - 4.3 LSHR LH Glycoprotein hormone A (Rhodopsin) Human - - - Glycoprotein alpha gtoplig
Choriogonadotropin beta 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
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
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
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 - 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 - 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 - 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
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
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
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
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 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 - 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 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 - 61 β1 Human γ2 Human Cryo-EM 7RKM - 3.5 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 - 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 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 - 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
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
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
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
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
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 - 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
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 - 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
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 - 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 - 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
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
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 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 - 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
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 - 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 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
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 - 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 - 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
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 - 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 - 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
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 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
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 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
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
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 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
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
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 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
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 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
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
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
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
Gs αs Bovine - 91 β1 Rat γ2 Bovine Cryo-EM 7FIG - 3.9 LSHR LH Glycoprotein hormone A (Rhodopsin) Human - Nanobody-35 - Glycoprotein alpha gtoplig
Choriogonadotropin beta 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
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 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
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
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 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 - 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 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 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
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 - 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
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 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
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
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
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
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 - 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
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
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 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
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
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
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 - 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 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 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
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
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
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
Gs αs Human - 54 β1 Human γ2 Human Cryo-EM 7EPT - 3.0 AGRD1 ADGRD1 ADGRD B2 (Adhesion) Human - Nanobody-35 - - - - - - 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 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 - 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 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 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 - 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
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
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
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
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
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 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 		2-arachidonoylglycerol, 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
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
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
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
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 - 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 - 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 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 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 - 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
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 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
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
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
Gs αs Bovine - 60 β1 Rat γ2 Bovine Cryo-EM 7FIH - 3.2 LSHR LH Glycoprotein hormone A (Rhodopsin) Human - - - Glycoprotein alpha gtoplig
Choriogonadotropin beta 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
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
Gq/11 αq Human Gs-Gq chimera 52 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
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 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 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 - 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 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
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
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 - 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
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
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 - 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
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 αi3 Human - 62 β1 Human γ2 Human Cryo-EM 7T10 - 2.5 SSR2 SST2 Somatostatin A (Rhodopsin) Human - scFv16 - SOMATOSTATIN chembl_ligand pubchem