Loading...
G PROTEIN
STRUCTURE
RECEPTOR
OTHER PROTEINS
STRUCTURE LIGAND
ENDOGENOUS LIGAND
REFERENCE
Fam. α Species Note % of Seq β Species γ Species Method
PDB
 Refined
structure
 Resolution
UniProt
 IUPHAR Receptor family Class Species Receptor fusion Antibodies Other Name Type Function Name Type 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 3SN6_refined 3.2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human T4-Lysozyme Antibody - BI-167107 pubchem
small-molecule Agonist (-)-noradrenaline, L-NOREPINEPHRINE, Zn2+, noradrenaline, (-)-adrenaline 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 - 48 β1 Human γ2 Human cryo-EM 6ORV - 3.0 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - CHEMBL3950796 chembl_ligand pubchem
small-molecule Agonist glucagon, glucagon-like peptide 1-(7-37), 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 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 - 58 β1 Human γ2 Human cryo-EM 6PB1 6PB1_refined 2.8 CRFR2 CRF2 Corticotropin-releasing factor B1 (Secretin) Human - Nanobody-35 - CHEMBL427807 chembl_ligand pubchem
protein Agonist urocortin 2, corticotrophin-releasing hormone, urocortin 3, urocortin 1 peptide Ma S, Shen Q, Zhao LH, Mao C, Zhou XE, Shen DD, de Waal PW, Bi P, Li C, Jiang Y, Wang MW, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE 10.1016/J.MOLCEL.2020.01.013 2020-02-12
Gs αs Human - 57 β1 Rat γ2 Bovine cryo-EM 6LPB 6LPB_refined 3.9 PACR PAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - CHEMBL524658 chembl_ligand pubchem
protein Agonist PHM, VIP, PHV, PACAP-27, PACAP-38, PHI 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 - 59 β1 Human γ2 Human cryo-EM 6LMK 6LMK_refined 3.7 GLR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - glucagon pubchem gtoplig chembl_ligand drugbank drug_central gtoplig pubchem pubchem pubchem pubchem
peptide Agonist glucagon peptide Qiao A, Han S, Li X, Li Z, Zhao P, Dai A, Chang R, Tai L, Tan Q, Chu X, Ma L, Thorsen TS, Reedtz-Runge S, Yang D, Wang MW, Sexton PM, Wootten D, Sun F, Zhao Q, Wu B 10.1126/SCIENCE.AAZ5346 2020-04-01
Gi/o αo Human - 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 (-)-adrenaline, (-)-noradrenaline small-molecule Yuan D, Liu Z, Kaindl J, Maeda S, Zhao J, Sun X, Xu J, Gmeiner P, Wang HW, Kobilka BK 10.1038/S41589-020-0492-2 2020-04-15
Gs αs Human - 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 6VMS_refined 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
Gs αs Human - 50 β1 Bovine γ2 Bovine cryo-EM 7BZ2 7BZ2_refined 3.8 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - Nanobody-35 - arformoterol pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist (-)-noradrenaline, L-NOREPINEPHRINE, Zn2+, noradrenaline, (-)-adrenaline 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 secretin, VIP 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 - 61 β1 Human γ2 Human cryo-EM 6VN7 6VN7_refined 3.2 VIPR1 VPAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - CHEMBL524658 chembl_ligand pubchem
protein Agonist secretin, PHM, VIP, PHV, GHRH, PACAP-27, PACAP-38, PHI 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 6X18_refined 2.1 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - CHEMBL410972 chembl_ligand pubchem pubchem
protein Agonist glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide peptide None 10.1101/2020.08.16.252585 2020-09-09
Gi/o αi1 Human - 61 β1 Human γ2 Human cryo-EM 6XBL 6XBL_refined 3.9 SMO SMO Frizzled F (Frizzled) Human - scFv16 - Cholesterol pubchem
SAG1.3 pubchem gtoplig
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 Bovine - 57 β1 Bovine γ2 Bovine cryo-EM 7D68 7D68_refined 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, glucagon-like peptide 2-(3-33) 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 7L0R_refined 4.2 NTR1 NTS1 Neurotensin A (Rhodopsin) Rat - - - neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
peptide Agonist neurotensin, neuromedin N peptide - - 2021-01-06
Gi/o αo Human - 61 β1 Human γ2 Human cryo-EM 7D77 7D77_refined 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 Engineered G alpha 58 β1 Human γ2 Human cryo-EM 7L1U 7L1U_refined 3.2 OX2R OX2 Orexin A (Rhodopsin) Human - scFv16 - Orexin-A pubchem
peptide Agonist orexin-A, orexin-B 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 - 60 β1 Human γ2 Human cryo-EM 7JVP 7JVP_refined 2.9 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - 39YLC3L0ZU pubchem
small-molecule Agonist dopamine, 5-hydroxytryptamine, (-)-noradrenaline, L-NOREPINEPHRINE, noradrenaline 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 7CKZ_refined 3.1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - dopamine pubchem gtoplig chembl_ligand drugbank drug_central
LY3154207 pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Agonist
PAM 		dopamine, 5-hydroxytryptamine, (-)-noradrenaline, L-NOREPINEPHRINE, noradrenaline 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 7CMU_refined 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 7E2X 7E2X_refined 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 dopamine, 5-hydroxytryptamine, (-)-noradrenaline, L-NOREPINEPHRINE, noradrenaline small-molecule - - 2021-04-14
Gs αs Human Engineered G protein 50 - - - - X-ray 5G53 5G53_refined 3.4 AA2AR A2A Adenosine A (Rhodopsin) Human - - - NECA pubchem gtoplig chembl_ligand gtoplig
small-molecule Agonist adenosine small-molecule Carpenter B, Nehme R, Warne T, Leslie AG, Tate CG 10.1038/NATURE18966 2016-08-03
Gs αs Human - 59 β1 Rat γ2 Bovine cryo-EM 5VAI 5VAI_refined 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
Gi/o αt1 Bovine Only H5 3 - - - - X-ray 5WKT 5WKT_refined 3.2 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - B-Octylglucoside pubchem
small-molecule unknown - - Broecker J, Morizumi T, Ou WL, Klingel V, Kuo A, Kissick DJ, Ishchenko A, Lee MY, Xu S, Makarov O, Cherezov V, Ogata CM, Ernst OP 10.1038/NPROT.2017.135 2017-12-13
Gs αs Human - 49 β1 Human γ2 Human cryo-EM 6B3J 6B3J_refined 3.3 GLP1R GLP-1 Glucagon B1 (Secretin) Human - - - Exendin-P5
peptide Agonist glucagon, glucagon-like peptide 1-(7-37), 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
Gi/o αi1 Human - 61 β1 Human γ2 Human cryo-EM 6DDE 6DDE_refined 3.5 OPRM μ Opioid A (Rhodopsin) Mouse - Antibody - DAMGO pubchem 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 αi1 Human Non-canonical conformation 62 β1 Human γ2 Human cryo-EM 6OSA 6OSA_refined 3.0 NTR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig chembl_ligand
peptide Agonist neurotensin, neuromedin N, large neuromedin N, 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 6OYA_refined 3.3 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - Camelid antibody VHH fragment - Retinal (all-trans) pubchem
small-molecule Agonist - - Gao Y, Hu H, Ramachandran S, Erickson JW, Cerione RA, Skiniotis G 10.1016/J.MOLCEL.2019.06.007 2019-07-24
Gi/o αi1 Human - 62 β1 Human γ2 Human cryo-EM 6KPF 6KPF_refined 2.9 CNR2 CB2 Cannabinoid A (Rhodopsin) Human - scFv16 - AM841 pubchem gtoplig
small-molecule Agonist anandamide, 2-arachidonoylglycerol 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 Gs-Gi1 chimera 58 β1 Human γ2 Human cryo-EM 6PB0 6PB0_refined 3.0 CRFR1 CRF1 Corticotropin-releasing factor B1 (Secretin) Human - Nanobody-35 - CHEMBL427807 chembl_ligand pubchem
protein Agonist urocortin 2, urocortin 1, corticotrophin-releasing hormone peptide Ma S, Shen Q, Zhao LH, Mao C, Zhou XE, Shen DD, de Waal PW, Bi P, Li C, Jiang Y, Wang MW, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE 10.1016/J.MOLCEL.2020.01.013 2020-02-12
Gs αs Human Mini-Gs 61 β1 Human γ2 Human cryo-EM 6LI3 6LI3_refined 3.3 GPR52 GPR52 A orphans A (Rhodopsin) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - 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 - 56 β1 Human γ2 Human cryo-EM 6M1I 6M1I_refined 3.5 PACR PAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - CHEMBL524658 chembl_ligand pubchem
protein Agonist PHM, VIP, PHV, PACAP-27, PACAP-38, PHI 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 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 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 - 48 β1 Human γ2 Human cryo-EM 7C2E 7C2E_refined 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, glucagon-like peptide 1-(7-37), 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 - 56 β1 Rat γ2 Bovine cryo-EM 7BW0 7BW0_refined 3.9 GPBAR GPBA Bile acid A (Rhodopsin) Human BRIL Nanobody-35 - - - - deoxycholic acid, cholic acid, lithocholic acid, chenodeoxycholic 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 7JJO_refined 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 6X19_refined 2.1 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - CHU-128 pubchem
small-molecule Agonist glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide peptide None 10.1101/2020.08.16.252585 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 		deoxycholic acid, cholic acid, lithocholic acid, chenodeoxycholic 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 6XBK_refined 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 - 56 β1 Human γ2 Human cryo-EM 6XOX 6XOX_refined 3.1 GLP1R GLP-1 Glucagon B1 (Secretin) Human - scFv16
Nanobody-35 		- CHEMBL4446782 chembl_ligand pubchem
small-molecule Agonist glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide peptide Kawai T, Sun B, Yoshino H, Feng D, Suzuki Y, Fukazawa M, Nagao S, Wainscott DB, Showalter AD, Droz BA, Kobilka TS, Coghlan MP, Willard FS, Kawabe Y, Kobilka BK, Sloop KW 10.1073/PNAS.2014879117 2020-11-18
Gs αs Human - 55 β1 Bovine γ2 Bovine cryo-EM 7DHI 7DHI_refined 3.3 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - Nanobody-35 - levosalbutamol pubchem gtoplig chembl_ligand drug_central drugbank
small-molecule Agonist (-)-noradrenaline, L-NOREPINEPHRINE, Zn2+, noradrenaline, (-)-adrenaline small-molecule None 10.1093/NSR/NWAA284 2020-12-16
Gi/o αt3 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
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 6DDF_refined 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 αo Human - 59 β1 Human γ2 Human cryo-EM 6G79 6G79_refined 3.8 5HT1B 5-HT1B 5-Hydroxytryptamine A (Rhodopsin) Human - - - donitriptan pubchem gtoplig chembl_ligand
small-molecule Agonist 5-HT-moduline, tryptamine, 5-hydroxytryptamine small-molecule Garcia-Nafria J, Nehme R, Edwards PC, Tate CG 10.1038/S41586-018-0241-9 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 Bovine - 58 β1 Rat γ2 Bovine cryo-EM 6NBF 6NBF_refined 3.0 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - Long-acting parathyroid hormone analog
peptide Agonist PTH, TIP39, PTHrP-(1-36), PTHrP 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 6NBI_refined 4.0 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - Long-acting parathyroid hormone analog
peptide Agonist PTH, TIP39, PTHrP-(1-36), PTHrP 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 - - BI-167107 pubchem
small-molecule Agonist (-)-noradrenaline, L-NOREPINEPHRINE, Zn2+, noradrenaline, (-)-adrenaline 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 - 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 neurotensin, neuromedin N, large neuromedin N, 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 - 64 β1 Bovine γT1 Bovine cryo-EM 6OY9 6OY9_refined 3.9 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - Retinal (all-trans) pubchem
small-molecule Agonist - - Gao Y, Hu H, Ramachandran S, Erickson JW, Cerione RA, Skiniotis G 10.1016/J.MOLCEL.2019.06.007 2019-07-24
Gs αs Human - 49 β1 Human γ2 Human cryo-EM 6P9X 6P9X_refined 2.9 CRFR1 CRF1 Corticotropin-releasing factor B1 (Secretin) Human - Nanobody-35 - Corticoliberin pubchem
peptide Agonist urocortin 2, urocortin 1, corticotrophin-releasing hormone 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 - 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 anandamide, 2-arachidonoylglycerol small-molecule Xing C, Zhuang Y, Xu TH, Feng Z, Zhou XE, Chen M, Wang L, Meng X, Xue Y, Wang J, Liu H, McGuire TF, Zhao G, Melcher K, Zhang C, Xu HE, Xie XQ 10.1016/J.CELL.2020.01.007 2020-02-12
Gi/o αi1 Human - 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 serum amyloid A, LTC4, LXA4, fMet-Leu-Phe, aspirin triggered lipoxin A4, PrP106-126, resolvin D1, LTD4, 15-deoxy-LXA4, annexin I, LL-37, humanin, aspirin-triggered resolvin D1, ATLa2 peptide Zhuang Y, Liu H, Edward Zhou X, Kumar Verma R, de Waal PW, Jang W, Xu TH, Wang L, Meng X, Zhao G, Kang Y, Melcher K, Fan H, Lambert NA, Eric Xu H, Zhang C 10.1038/S41467-020-14728-9 2020-02-26
Gs αs Human - 54 β1 Human γ2 Human cryo-EM 6M1H 6M1H_refined 3.6 PACR PAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - Maxadilan pubchem
peptide Agonist PHM, VIP, PHV, PACAP-27, PACAP-38, PHI peptide Wang J, Song X, Zhang D, Chen X, Li X, Sun Y, Li C, Song Y, Ding Y, Ren R, Harrington EH, Hu LA, Zhong W, Xu C, Huang X, Wang HW, Ma Y 10.1038/S41422-020-0280-2 2020-03-11
Gi/o αi1 Human - 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
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 (-)-adrenaline, (-)-noradrenaline 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 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 - 57 β1 Human γ2 Human cryo-EM 6VCB 6VCB_refined 3.3 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - glucagon-like peptide 1-(7-37) pubchem gtoplig chembl_ligand gtoplig pubchem pubchem
LSN3160440 pubchem
peptide
small-molecule 		Agonist
PAM 		glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide peptide Bueno AB, Sun B, Willard FS, Feng D, Ho JD, Wainscott DB, Showalter AD, Vieth M, Chen Q, Stutsman C, Chau B, Ficorilli J, Agejas FJ, Cumming GR, Jimenez A, Rojo I, Kobilka TS, Kobilka BK, Sloop KW 10.1038/S41589-020-0589-7 2020-07-22
Gs αs Human - 49 β1 Human γ2 Human cryo-EM 6WI9 6WI9_refined 4.3 SCTR secretin Glucagon B1 (Secretin) Human - Nanobody-35 - SECRETIN chembl_ligand pubchem
protein Agonist secretin, VIP 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 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
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
Gs αs Human - 47 β1 Human γ2 Human cryo-EM 5UZ7 5UZ7_refined 4.1 CALCR CT Calcitonin B1 (Secretin) Human - - - - - - adrenomedullin 2/intermedin, amylin, adrenomedullin, calcitonin (salmon), α-CGRP, β-CGRP, calcitonin 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 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
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 - 43 β1 Human γ2 Human cryo-EM 6NIY 6NIY_refined 3.3 CALCR CT Calcitonin B1 (Secretin) Human - - - calcitonin (salmon synthetic) pubchem
small-molecule Agonist adrenomedullin 2/intermedin, amylin, adrenomedullin, calcitonin (salmon), α-CGRP, β-CGRP, calcitonin 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 anandamide, 2-arachidonoylglycerol 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 - 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 PTH, TIP39, PTHrP-(1-36), PTHrP 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 - - - iperoxo pubchem gtoplig chembl_ligand
LY2119620 pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Agonist
PAM 		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 - 60 β1 Bovine γT1 Bovine cryo-EM 6QNO 6QNO_refined 4.4 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - Fab antibody fragment light chain
Fab antibody fragment heavy chain 		- Retinal (all-trans) pubchem
small-molecule Agonist - - Tsai CJ, Marino J, Adaixo R, Pamula F, Muehle J, Maeda S, Flock T, Taylor NM, Mohammed I, Matile H, Dawson RJ, Deupi X, Stahlberg H, Schertler G 10.7554/ELIFE.46041 2019-07-10
Gs αs Human - 59 β1 Human γ2 Human cryo-EM 6NI3 6NI3_refined 3.8 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - Nanobody-35 - BI-167107 pubchem
small-molecule Agonist (-)-noradrenaline, L-NOREPINEPHRINE, Zn2+, noradrenaline, (-)-adrenaline 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 6P9Y 6P9Y_refined 3.0 PACR PAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - CHEMBL524658 chembl_ligand pubchem
protein Agonist PHM, VIP, PHV, PACAP-27, PACAP-38, PHI peptide - - 2020-02-05
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
small-molecule Agonist anandamide, 2-arachidonoylglycerol 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 - 48 β1 Human γ2 Human cryo-EM 6UUN 6UUN_refined 3.0 CALRL calcitonin-like Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP2 		- Adrenomedullin pubchem
peptide Agonist - - Liang YL, Belousoff MJ, Fletcher MM, Zhang X, Khoshouei M, Deganutti G, Koole C, Furness SGB, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Danev R, Wootten D, Sexton PM 10.1021/ACSPTSCI.9B00080 2020-03-25
Gs αs Human - 48 β1 Human γ2 Human cryo-EM 6UVA 6UVA_refined 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
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
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
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 CXCL7, CXCL6, CXCL5, CXCL8, CXCL1, CXCL2, CXCL3 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 7CFM_refined 3.0 GPBAR GPBA Bile acid A (Rhodopsin) Human - Nanobody-35 - CHEMBL2331646 chembl_ligand pubchem
small-molecule Agonist deoxycholic acid, cholic acid, lithocholic acid, chenodeoxycholic 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 6XBJ_refined 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 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 thromboxane A2, PGD2, PGE2, PGE1, PGI2, PGF2α small-molecule - - 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 Non-canonical conformation 95 β1 Human γT1 Human cryo-EM 7L0S 7L0S_refined 4.5 NTR1 NTS1 Neurotensin A (Rhodopsin) Rat - - - neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
peptide Agonist neurotensin, neuromedin N peptide - - 2021-01-06
Gs αs Human Engineered G alpha 58 β1 Human γ2 Human cryo-EM 7L1V 7L1V_refined 3.0 OX2R OX2 Orexin A (Rhodopsin) Human - scFv16
Nanobody-51 		- compound 1 [PMID: 33547286] pubchem gtoplig
small-molecule Agonist orexin-A, orexin-B 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 dopamine, 5-hydroxytryptamine, (-)-noradrenaline, L-NOREPINEPHRINE, noradrenaline 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 dopamine, 5-hydroxytryptamine, (-)-noradrenaline, L-NOREPINEPHRINE, noradrenaline 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 dopamine, 5-hydroxytryptamine, (-)-noradrenaline, L-NOREPINEPHRINE, noradrenaline 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 7CMV_refined 2.7 DRD3 D3 Dopamine A (Rhodopsin) Human BRIL scFv16 - CHEMBL70565 chembl_ligand chembl_ligand pubchem
small-molecule Agonist dopamine small-molecule Xu P, Huang S, Mao C, Krumm BE, Zhou XE, Tan Y, Huang XP, Liu Y, Shen DD, Jiang Y, Yu X, Jiang H, Melcher K, Roth BL, Cheng X, Zhang Y, Xu HE 10.1016/J.MOLCEL.2021.01.003 2021-03-10
Gi/o αi1 Human - 62 β1 Human γ2 Human cryo-EM 7E2Z 7E2Z_refined 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 β-MSH, ACTH, γ-MSH, agouti-related protein, α-MSH peptide Israeli H, Degtjarik O, Fierro F, Chunilal V, Gill AK, Roth NJ, Botta J, Prabahar V, Peleg Y, Chan LF, Ben-Zvi D, McCormick PJ, Niv MY, Shalev-Benami M 10.1126/SCIENCE.ABF7958 2021-04-28
Gs αs Human - 58 β1 Human γ2 Human cryo-EM 7KH0 7KH0_refined 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 7BB6_refined 4.2 V2R V2 Vasopressin and oxytocin A (Rhodopsin) Human - Nanobody-35 - vasopressin pubchem gtoplig chembl_ligand drugbank drug_central
peptide Agonist oxytocin, vasopressin peptide Bous J, Orcel H, Floquet N, Leyrat C, Lai-Kee-Him J, Gaibelet G, Ancelin A, Saint-Paul J, Trapani S, Louet M, Sounier R, Demene H, Granier S, Bron P, Mouillac B 10.1126/SCIADV.ABG5628 2021-06-02
Gs αs Human - 48 β1 Bovine γ2 Mouse cryo-EM 7E14 7E14_refined 2.9 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - N-Tert-butyl-6,7-dichloroquinoxalin-2-amine pubchem
CHEMBL4446782 chembl_ligand pubchem
small-molecule
small-molecule 		Ago-PAM
Agonist 		glucagon, glucagon-like peptide 1-(7-37), 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 7MTS_refined 3.2 GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human - - - 2-methoxy-6-propyl-N-(2-{4-[(1H-tetrazol-5-yl)methoxy]phenyl}ethyl)thieno[2,3-d]pyrimidin-4-amine pubchem
L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem
small-molecule
small-molecule 		Ago-PAM
Agonist 		L-glutamic acid small-molecule Seven AB, Barros-Alvarez X, de Lapeyriere M, Papasergi-Scott MM, Robertson MJ, Zhang C, Nwokonko RM, Gao Y, Meyerowitz JG, Rocher JP, Schelshorn D, Kobilka BK, Mathiesen JM, Skiniotis G 10.1038/S41586-021-03680-3 2021-07-07
Gi/o αi1 Human - 64 β1 Human γ2 Human cryo-EM 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, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate 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 - 58 β1 Human γ2 Human cryo-EM 7F54 7F54_refined 3.0 MC4R MC4 Melanocortin A (Rhodopsin) Human - Nanobody-35 - afamelanotide pubchem gtoplig chembl_ligand drugbank pubchem pubchem pubchem pubchem
peptide Agonist β-MSH, ACTH, γ-MSH, agouti-related protein, α-MSH 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 - 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 neurokinin B, neuropeptide K, hemokinin 1, neuropeptide-γ, neurokinin A, 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 7S8L_refined 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 7S8O_refined 2.6 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human BRIL scFv16 - (R)-ZINC-3573 pubchem gtoplig chembl_ligand
small-molecule Agonist PAMP-20 peptide Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL 10.1038/S41586-021-04126-6 2021-11-17
Gi/o αi1 Human - 62 β1 Human γ2 Human cryo-EM 7VDH 7VDH_refined 2.9 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human - scFv16 - compound 48/80 pubchem gtoplig
small-molecule Agonist PAMP-20 peptide - - 2021-12-01
Gi/o αi1 Human - 62 β1 Human γ2 Human cryo-EM 7VUZ - 2.9 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human - scFv16 - PAMP-12 pubchem
peptide Agonist PAMP-20 peptide - - 2021-12-01
Gq/11 αq Human Gq-Gs-Gi1 chimera 59 β1 Human γ2 Human cryo-EM 7P00 7P00_refined 2.7 NK1R NK1 Tachykinin A (Rhodopsin) Human - scFv16 - substance P pubchem gtoplig chembl_ligand gtoplig gtoplig
peptide Agonist neurokinin B, neuropeptide K, hemokinin 1, neuropeptide-γ, neurokinin A, substance P peptide Thom C, Ehrenmann J, Vacca S, Waltenspuhl Y, Schoppe J, Medalia O, Pluckthun A 10.1126/SCIADV.ABK2872 2021-12-15
Gs αs Human - 58 β1 Human γ2 Human cryo-EM 7VUJ - 3.8 GP139 GPR139 A orphans A (Rhodopsin) Human - Nanobody-35 Xylanase JNJ-63533054 pubchem gtoplig chembl_ligand
small-molecule Agonist L-tryptophan, L-phenylalanine 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 - 43 β1 Human γ2 Human cryo-EM 7EO4 7EO4_refined 2.9 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - siponimod pubchem gtoplig chembl_ligand drug_central drugbank
small-molecule Agonist sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate 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
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, glucagon-like peptide 1-(7-37), 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 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, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate 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 7F4H_refined 2.7 MSHR MC1 Melanocortin A (Rhodopsin) Human - Nanobody-35
scFv16 		- CHEMBL407070 chembl_ligand pubchem pubchem
protein Agonist β-MSH, α-MSH, ACTH, γ-MSH 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 7T6U_refined 2.9 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human - - - synthetic peptide
peptide Agonist serum amyloid A, LTC4, LXA4, fMet-Leu-Phe, aspirin triggered lipoxin A4, PrP106-126, resolvin D1, LTD4, 15-deoxy-LXA4, annexin I, LL-37, humanin, aspirin-triggered resolvin D1, ATLa2 peptide - - 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 pubchem gtoplig chembl_ligand drugbank chembl_ligand pubchem
peptide Agonist cortistatin-14, SRIF-14, SRIF-28, CST-17 peptide Robertson MJ, Meyerowitz JG, Panova O, Borrelli K, Skiniotis G 10.1038/S41594-022-00727-5 2022-03-09
Gi/o αi1 Human - 62 β1 Human γ2 Human cryo-EM 7VL8 7VL8_refined 2.9 CCR1 CCR1 Chemokine A (Rhodopsin) Human - scFv16 - Apo (no ligand)
none Apo (no ligand) CCL14, CCL23, CCL15, CCL8, CCL7, CCL16, CCL13, CCL5, CCL3, CCL4 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 - 62 β1 Bovine γ2 Bovine cryo-EM 7TD0 7TD0_refined 2.8 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human - - - (2r)-2-Hydroxy-3-(Phosphonooxy)propyl (9e)-Octadec-9-Enoate pubchem
small-molecule Agonist 1-O-Oleoyl-D-glycerol 3-phosphoric acid small-molecule Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY 10.1038/S41467-022-28417-2 2022-02-09
Gi/o αi1 Mouse - 62 β1 Bovine γ2 Bovine cryo-EM 7TD2 7TD2_refined 3.1 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human - - - (2r)-2-Hydroxy-3-(Phosphonooxy)propyl (9e)-Octadec-9-Enoate pubchem
small-molecule Agonist 1-O-Oleoyl-D-glycerol 3-phosphoric acid small-molecule Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY 10.1038/S41467-022-28417-2 2022-02-09
Gi/o αi1 Human - 62 β1 Rat γ2 Bovine cryo-EM 7VGZ 7VGZ_refined 3.3 MTR1A MT1 Melatonin A (Rhodopsin) Human - scFv16 - ramelteon pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist melatonin small-molecule - - 2022-03-02
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 adrenomedullin 2/intermedin, amylin, adrenomedullin, calcitonin (salmon), α-CGRP, β-CGRP, calcitonin 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 peptide
peptide Agonist adrenomedullin 2/intermedin, amylin, adrenomedullin, calcitonin (salmon), α-CGRP, β-CGRP, calcitonin 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 7FIY_refined 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 7VBI_refined 3.0 GLP1R GLP-1 Glucagon B1 (Secretin) Human - - - tirzepatide pubchem gtoplig
peptide Agonist glucagon, glucagon-like peptide 1-(7-37), 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 7EJK_refined 3.4 ADA2A α2A Adrenoceptors A (Rhodopsin) Human - scFv16 - oxymetazoline pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist (-)-adrenaline, (-)-noradrenaline small-molecule - - 2022-04-13
Gi/o αi2 Human - 61 β1 Human γ2 Human cryo-EM 7WVX 7WVX_refined 2.8 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human BRIL - - humanin pubchem gtoplig chembl_ligand pubchem
peptide Agonist serum amyloid A, LTC4, LXA4, fMet-Leu-Phe, aspirin triggered lipoxin A4, PrP106-126, resolvin D1, LTD4, 15-deoxy-LXA4, annexin I, LL-37, humanin, aspirin-triggered resolvin D1, ATLa2 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 7SBF_refined 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 - 54 β1 Human γ2 Human cryo-EM 7RG9 - 3.2 GLP1R GLP-1 Glucagon B1 (Secretin) Human - scFv16
Nanobody-35 		- Apo (no ligand)
none Apo (no ligand) glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide peptide Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW 10.1073/PNAS.2116506119 2022-04-13
Gs αs Human - 53 β1 Rat γ2 Bovine cryo-EM 7VBH 7VBH_refined 3.0 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Peptide 20
peptide Agonist glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide peptide Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW 10.1038/S41467-022-28683-0 2022-04-06
G12/13 α13 Human Gi2-mini-G13 chimera 54 β1 Human γ2 Human cryo-EM 7SF7 - 2.9 AGRL3 ADGRL3 ADGRL B2 (Adhesion) Human - - - Apo (no ligand)
none Apo (no ligand) - - Barros-Alvarez X, Nwokonko RM, Vizurraga A, Matzov D, He F, Papasergi-Scott MM, Robertson MJ, Panova O, Yardeni EH, Seven AB, Kwarcinski FE, Su H, Peroto MC, Meyerowitz JG, Shalev-Benami M, Tall GG, Skiniotis G 10.1038/S41586-022-04575-7 2022-04-27
G12/13 α13 Human Gi2-mini-G13 chimera 53 β1 Human γ2 Human cryo-EM 7SF8 - 2.7 AGRG1 ADGRG1 ADGRG B2 (Adhesion) Human - - - Apo (no ligand)
none Apo (no ligand) - - Barros-Alvarez X, Nwokonko RM, Vizurraga A, Matzov D, He F, Papasergi-Scott MM, Robertson MJ, Panova O, Yardeni EH, Seven AB, Kwarcinski FE, Su H, Peroto MC, Meyerowitz JG, Shalev-Benami M, Tall GG, Skiniotis G 10.1038/S41586-022-04575-7 2022-04-27
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 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 CXCL7, CXCL6, CXCL5, CXCL8, CXCL1, CXCL2, CXCL3 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 6X1A_refined 2.5 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - DANUGLIPRON chembl_ligand pubchem
small-molecule Agonist glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide peptide None 10.1101/2020.08.16.252585 2020-09-09
Gq/11 αq Human Gq-Gi2-Gs chimera 59 β1 Human γ2 Human cryo-EM 6WHA 6WHA_refined 3.4 5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL scFv16 - 25-CN-NBOH pubchem
small-molecule Agonist tryptamine, 5-hydroxytryptamine 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 6XBM_refined 3.2 SMO SMO Frizzled F (Frizzled) Human - scFv16 - 24,25-Epoxy-cholesterol pubchem
24,25-Epoxy-cholesterol pubchem
small-molecule
small-molecule 		Agonist
PAM 		- - Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X 10.1038/S41589-020-0646-2 2020-09-30
Gs αs Human - 58 β1 Rat γ2 Bovine cryo-EM 7D3S 7D3S_refined 2.9 SCTR secretin Glucagon B1 (Secretin) Human - Nanobody-35 - SECRETIN chembl_ligand pubchem
protein Agonist secretin, VIP 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 Rat γ2 Bovine cryo-EM 7CZ5 7CZ5_refined 2.6 GHRHR GHRH Glucagon B1 (Secretin) Human - Nanobody-35 - Somatoliberin pubchem
peptide Agonist GHRH peptide Zhou F, Zhang H, Cong Z, Zhao LH, Zhou Q, Mao C, Cheng X, Shen DD, Cai X, Ma C, Wang Y, Dai A, Zhou Y, Sun W, Zhao F, Zhao S, Jiang H, Jiang Y, Yang D, Eric Xu H, Zhang Y, Wang MW 10.1038/S41467-020-18945-0 2020-11-18
Gs αs Human - 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 (-)-noradrenaline, L-NOREPINEPHRINE, Zn2+, noradrenaline, (-)-adrenaline small-molecule None 10.1093/NSR/NWAA284 2020-12-16
Gi/o αi1 Human - 95 β1 Human γT1 Human cryo-EM 7L0Q 7L0Q_refined 4.3 NTR1 NTS1 Neurotensin A (Rhodopsin) Rat - - - neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
peptide Agonist neurotensin, neuromedin N peptide - - 2021-01-06
Gi/o αo Human - 59 β1 Human γ2 Human cryo-EM 7D76 - 3.1 AGRG3 ADGRG3 ADGRG B2 (Adhesion) Human - - - Beclomethasone pubchem
small-molecule Agonist - - Ping YQ, Mao C, Xiao P, Zhao RJ, Jiang Y, Yang Z, An WT, Shen DD, Yang F, Zhang H, Qu C, Shen Q, Tian C, Li ZJ, Li S, Wang GY, Tao X, Wen X, Zhong YN, Yang J, Yi F, Yu X, Xu HE, Zhang Y, Sun JP 10.1038/S41586-020-03083-W 2021-02-03
Gi/o αi1 Human - 63 β1 Human γ2 Human cryo-EM 7JVR 7JVR_refined 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 7CKY_refined 3.2 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - CHEMBL3697578 chembl_ligand pubchem
small-molecule Agonist dopamine, 5-hydroxytryptamine, (-)-noradrenaline, L-NOREPINEPHRINE, noradrenaline 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 58 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
LY3154207 pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Agonist
PAM 		dopamine, 5-hydroxytryptamine, (-)-noradrenaline, L-NOREPINEPHRINE, noradrenaline small-molecule None 10.1101/2021.02.07.430101 2021-03-03
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 tryptamine, 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 - 58 β1 Human γ2 Human cryo-EM 7CX2 7CX2_refined 2.8 PE2R2 EP2 Prostanoid A (Rhodopsin) Human - Nanobody-35 - PGE2 pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
small-molecule Agonist thromboxane A2, PGD2, PGE2, PGE1, PGI2, PGF2α 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
Gi/o αi1 Human - 99 β1 Human γ2 Human cryo-EM 7EB2 7EB2_refined 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 αi3 Human - 63 β1 Human γ2 Human cryo-EM 7E9H 7E9H_refined 4.0 GRM4 mGlu4 Metabotropic glutamate C (Glutamate) Human - scFv16 - L-serine-O-phosphate pubchem gtoplig chembl_ligand drugbank drug_central pubchem
small-molecule Agonist L-glutamic acid, L-serine-O-phosphate small-molecule Lin S, Han S, Cai X, Tan Q, Zhou K, Wang D, Wang X, Du J, Yi C, Chu X, Dai A, Zhou Y, Chen Y, Zhou Y, Liu H, Liu J, Yang D, Wang MW, Zhao Q, Wu B 10.1038/S41586-021-03495-2 2021-06-23
Gi/o αi1 Human - 62 β1 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 CCL14, CCL2, CCL8, CCL7, CCL16, CCL13, CCL11, CCL5, CCL3, CCL4 peptide Isaikina P, Tsai CJ, Dietz N, Pamula F, Grahl A, Goldie KN, Guixa-Gonzalez R, Branco C, Paolini-Bertrand M, Calo N, Cerini F, Schertler GFX, Hartley O, Stahlberg H, Maier T, Deupi X, Grzesiek S 10.1126/SCIADV.ABG8685 2021-06-30
Gs αs Human - 61 β1 Rat γ2 Bovine cryo-EM 7DUQ 7DUQ_refined 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, glucagon-like peptide 1-(7-37), 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
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) CCL14, CCL2, CCL8, CCL7, CCL16, CCL13, CCL11, CCL5, CCL3, CCL4 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 - 56 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
Gs αs Human - 59 β1 Rat γ2 Bovine cryo-EM 7DH5 7DH5_refined 3.2 ADRB3 β3 Adrenoceptors A (Rhodopsin) Dog - Nanobody-35 - mirabegron pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist - - Nagiri C, Kobayashi K, Tomita A, Kato M, Kobayashi K, Yamashita K, Nishizawa T, Inoue A, Shihoya W, Nureki O 10.1016/J.MOLCEL.2021.06.024 2021-08-04
Gs αs Bovine - 59 β1 Rat γ2 Bovine cryo-EM 7DTY 7DTY_refined 3.0 GIPR GIP Glucagon B1 (Secretin) Human - Nanobody-35 - GIP pubchem 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 - 58 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
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 - 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, glucagon-like peptide 1-(7-37), 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 - 89 β1 Human γ2 Human cryo-EM 7KI1 7KI1_refined 2.5 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Taspoglutide pubchem
peptide Agonist glucagon, glucagon-like peptide 1-(7-37), 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 - 60 β1 Rat γ2 Bovine cryo-EM 7EVM 7EVM_refined 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, glucagon-like peptide 1-(7-37), 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
Gs αs Human - 58 β1 Rat γ2 Bovine cryo-EM 7F16 7F16_refined 2.8 PTH2R PTH2 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - TIP39 gtoplig
peptide Agonist PTHrP-(1-34) (human), TIP39, PTHrP, PTH, PTHrP-(1-36) 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
Gs αs Human - 58 β1 Human γ2 Human cryo-EM 7EZK 7EZK_refined 3.1 CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human - - - CCK-8 pubchem gtoplig chembl_ligand drug_central drugbank
peptide Agonist CCK-58, CCK-33, desulfated cholecystokinin-8, CCK-4, gastrin-17, CCK-8, CCK-39 peptide - - 2021-08-25
Gi/o αi2 Human - 59 β1 Human γ2 Human cryo-EM 7LD3 7LD3_refined 3.2 AA1R A1 Adenosine A (Rhodopsin) Human - - - adenosine pubchem gtoplig chembl_ligand drugbank drug_central
{2-Amino-4-[3,5-bis(trifluoromethyl)phenyl]thiophen-3-yl}(4-chlorophenyl)methanone pubchem
small-molecule
small-molecule 		Agonist
PAM 		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 7EW2_refined 3.1 S1PR3 S1P3 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - (S)-FTY720-phosphate pubchem gtoplig chembl_ligand
small-molecule Agonist sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate 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 - 56 β1 Rat γ2 Bovine cryo-EM 7FIH - 3.2 LSHR LH Glycoprotein hormone A (Rhodopsin) Human - - - Choriogonadotropin beta gtoplig
Glycoprotein alpha gtoplig
5-Amino-N-(1,1-dimethylethyl)-2-(methylthio)-4-[3-[[2-(4-morpholinyl)acetyl]amino]phenyl]thieno[2,3-d]pyrimidine-6-carboxamide pubchem
protein
protein
small-molecule 		Agonist LH, hCG peptide Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE 10.1038/S41586-021-03924-2 2021-09-29
Gq/11 αq Human Gq-Gi1 chimera 60 β1 Rat γ2 Bovine cryo-EM 7F2O 7F2O_refined 2.9 BKRB2 B2 Bradykinin A (Rhodopsin) Human - scFv16 - bradykinin pubchem gtoplig chembl_ligand drugbank gtoplig
peptide Agonist kallidin, bradykinin, [des-Arg10]kallidin, Lys-[Hyp3]-bradykinin, [Hyp3]bradykinin, T-kinin, [des-Arg9]bradykinin peptide Yin YL, Ye C, Zhou F, Wang J, Yang D, Yin W, Wang MW, Xu HE, Jiang Y 10.1038/S41594-021-00645-Y 2021-10-13
Gi/o αi2 Human - 61 β1 Human γ2 Human cryo-EM 7F8V 7F8V_refined 3.3 GASR CCK2 Cholecystokinin A (Rhodopsin) Human - - - desulfated gastrin-17 pubchem gtoplig chembl_ligand pubchem
peptide Agonist desulfated gastrin-34, desulfated gastrin-14, desulfated cholecystokinin-8, CCK-33, CCK-4, CCK-58, gastrin-71, gastrin-34, desulfated gastrin-17, gastrin-17, CCK-8, gastrin-14, CCK-39, desulfated gastrin-71 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 7F55 7F55_refined 3.1 MC4R MC4 Melanocortin A (Rhodopsin) Human - Nanobody-35 - bremelanotide pubchem gtoplig chembl_ligand drugbank drug_central
peptide Agonist β-MSH, ACTH, γ-MSH, agouti-related protein, α-MSH 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 Gs-Gq chimera 49 β1 Human γ2 Human cryo-EM 7RMI 7RMI_refined 3.2 NK1R NK1 Tachykinin A (Rhodopsin) Human - Nanobody-35 - substance P pubchem gtoplig chembl_ligand gtoplig gtoplig
peptide Agonist neurokinin B, neuropeptide K, hemokinin 1, neuropeptide-γ, neurokinin A, 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 7S8M_refined 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 - 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 - - 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 7VUH - 3.2 GP139 GPR139 A orphans A (Rhodopsin) Human - Nanobody-35 Xylanase JNJ-63533054 pubchem gtoplig chembl_ligand
small-molecule Agonist L-tryptophan, L-phenylalanine 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, glucagon-like peptide 1-(7-37), 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 - 59 β1 Human γ2 Human cryo-EM 7LLL 7LLL_refined 3.7 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - exendin-4 pubchem gtoplig pubchem
peptide Agonist glucagon, glucagon-like peptide 1-(7-37), 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 - 61 β1 Human γ2 Human cryo-EM 7RKN 7RKN_refined 3.6 US28 US28 Unclassified A (Rhodopsin) strain AD169 - scFv16 - Fractalkine pubchem
peptide Agonist - - Tsutsumi N, Maeda S, Qu Q, Vogele M, Jude KM, Suomivuori CM, Panova O, Waghray D, Kato HE, Velasco A, Dror RO, Skiniotis G, Kobilka BK, Garcia KC 10.1126/SCIADV.ABL5442 2022-01-26
Gi/o αi1 Human - 64 β1 Human γ2 Human cryo-EM 7EVY 7EVY_refined 3.0 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - siponimod pubchem gtoplig chembl_ligand drug_central drugbank
small-molecule Agonist sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate 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 7F4D_refined 3.0 MSHR MC1 Melanocortin A (Rhodopsin) Human - Nanobody-35 - INTERMEDINE chembl_ligand pubchem pubchem pubchem
protein Agonist β-MSH, α-MSH, ACTH, γ-MSH 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 serum amyloid A, LTC4, LXA4, fMet-Leu-Phe, aspirin triggered lipoxin A4, PrP106-126, resolvin D1, LTD4, 15-deoxy-LXA4, annexin I, LL-37, humanin, aspirin-triggered resolvin D1, ATLa2 peptide - - 2022-03-30
Gq/11 αq Human Gamma subunit fused to alpha subunit 57 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 - 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, CCL23, CCL15, CCL8, CCL7, CCL16, CCL13, CCL5, CCL3, CCL4 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 7TD4_refined 2.6 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - - - siponimod pubchem gtoplig chembl_ligand drug_central drugbank
small-molecule Agonist sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate 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 7TYH 7TYH_refined 3.3 CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - calcitonin human pubchem
small-molecule Agonist adrenomedullin 2/intermedin, amylin, adrenomedullin, calcitonin (salmon), α-CGRP, β-CGRP, calcitonin peptide - - 2022-03-23
Gs αs Human - 58 β1 Human γ2 Human cryo-EM 7TYN 7TYN_refined 2.6 CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - calcitonin (salmon synthetic) pubchem
small-molecule Agonist adrenomedullin 2/intermedin, amylin, adrenomedullin, calcitonin (salmon), α-CGRP, β-CGRP, calcitonin 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 Human - 58 β1 Human γ2 Human cryo-EM 7TYY 7TYY_refined 3.0 CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - calcitonin (salmon synthetic) pubchem
small-molecule Agonist adrenomedullin 2/intermedin, amylin, adrenomedullin, calcitonin (salmon), α-CGRP, β-CGRP, calcitonin 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 Mini-Gs 60 β1 Rat γ2 Bovine cryo-EM 7VAB 7VAB_refined 3.2 GIPR GIP Glucagon B1 (Secretin) Human - Nanobody-35 - tirzepatide pubchem gtoplig
peptide Agonist gastric inhibitory polypeptide peptide Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW 10.1038/S41467-022-28683-0 2022-03-02
Gi/o αo Human - 61 β1 Human γ2 Human cryo-EM 7EJ8 7EJ8_refined 3.0 ADA2A α2A Adrenoceptors A (Rhodopsin) Human - scFv16 - brimonidine pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
small-molecule Agonist (-)-adrenaline, (-)-noradrenaline small-molecule - - 2022-04-13
Gi/o αi2 Human - 63 β1 Human γ2 Human cryo-EM 7WVV 7WVV_refined 2.9 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human BRIL - - FME-LEU-PHE-ILE-ILE
peptide Agonist serum amyloid A, LTC4, LXA4, fMet-Leu-Phe, aspirin triggered lipoxin A4, PrP106-126, resolvin D1, LTD4, 15-deoxy-LXA4, annexin I, LL-37, humanin, aspirin-triggered resolvin D1, ATLa2 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 - 64 β1 Rat γ2 Bovine cryo-EM 7WQ3 7WQ3_refined 2.7 GALR1 GAL1 Galanin A (Rhodopsin) Human - scFv16 - galanin gtoplig chembl_ligand gtoplig pubchem pubchem pubchem pubchem pubchem
peptide Agonist galanin, galanin-like peptide peptide - - 2022-04-20
Gi/o αi1 Human - 61 β1 Human γ2 Human cryo-EM 7U2L 7U2L_refined 3.2 OPRM μ Opioid A (Rhodopsin) Mouse - scFv16 - N-(5-carbamimidamidopentyl)-N-[1-(2-phenylethyl)piperidin-4-yl]propanamide
small-molecule Agonist - - - - 2022-05-04
Gs αs Human Engineered G alpha 56 β1 Human γ2 Human cryo-EM 7RA3 7RA3_refined 3.2 GIPR GIP Glucagon B1 (Secretin) Human - scFv16
Nanobody-35 		- GIP pubchem pubchem
small-molecule Agonist gastric inhibitory polypeptide peptide Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW 10.1073/PNAS.2116506119 2022-04-13
Gi/o αi1 Human - 63 β1 Human γT1 Human cryo-EM 7L0P 7L0P_refined 4.1 NTR1 NTS1 Neurotensin A (Rhodopsin) Rat - - - neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
peptide Agonist neurotensin, neuromedin N peptide - - 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 chembl_ligand pubchem
small-molecule Agonist glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide peptide - - 2021-01-20
Gs αs Human - 60 β1 Human γ2 Human cryo-EM 7JV5 7JV5_refined 3.0 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - CHEMBL1160787 chembl_ligand pubchem
small-molecule Agonist dopamine, 5-hydroxytryptamine, (-)-noradrenaline, L-NOREPINEPHRINE, noradrenaline 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 7CKX_refined 3.5 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - A77636 pubchem gtoplig chembl_ligand
small-molecule Agonist dopamine, 5-hydroxytryptamine, (-)-noradrenaline, L-NOREPINEPHRINE, noradrenaline 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 58 β1 Rat γ2 Bovine cryo-EM 7LJC - 3.0 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - CHEMBL1160787 chembl_ligand pubchem
LY3154207 pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Agonist
PAM 		dopamine, 5-hydroxytryptamine, (-)-noradrenaline, L-NOREPINEPHRINE, noradrenaline small-molecule None 10.1101/2021.02.07.430101 2021-03-03
Gq/11 αq Human - 63 β1 Human γ2 Human cryo-EM 7DFL 7DFL_refined 3.3 HRH1 H1 Histamine A (Rhodopsin) Human - scFv16 - histamine pubchem gtoplig chembl_ligand drug_central drugbank gtoplig
small-molecule Agonist histamine small-molecule - - 2021-03-31
Gi/o αi1 Human - 62 β1 Human γ2 Human cryo-EM 7E2Y 7E2Y_refined 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 7E32_refined 2.9 5HT1D 5-HT1D 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - 5-hydroxytryptamine pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist 5-HT-moduline, 5-hydroxytryptamine peptide 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 7CX4 7CX4_refined 2.9 PE2R2 EP2 Prostanoid A (Rhodopsin) Human - Nanobody-35 - evatanepag pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist thromboxane A2, PGD2, PGE2, PGE1, PGI2, PGF2α 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 7MBY_refined 2.4 CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human - - - CHEMBL216166 chembl_ligand pubchem
protein Agonist CCK-58, CCK-33, desulfated cholecystokinin-8, CCK-4, gastrin-17, CCK-8, CCK-39 peptide - - 2021-05-26
Gi/o αi1 Human - 61 β1 Human γ2 Human cryo-EM 7F1R 7F1R_refined 3.0 CCR5 CCR5 Chemokine A (Rhodopsin) Human - - - CCL5 gtoplig
peptide Agonist CCL14, CCL2, CCL8, CCL7, CCL16, CCL13, CCL11, CCL5, CCL3, CCL4 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 - 60 β1 Rat γ2 Bovine cryo-EM 7DUR 7DUR_refined 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, glucagon-like peptide 1-(7-37), 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
Gq/11 αq Human Engineered G alpha 59 β1 Human γ2 Human cryo-EM 7F9Y 7F9Y_refined 2.9 GHSR ghrelin Ghrelin A (Rhodopsin) Human - Nanobody-35 - ghrelin gtoplig
peptide Agonist [des-Gln14]ghrelin, ghrelin peptide - - 2021-08-18
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 - - 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-58, CCK-33, desulfated cholecystokinin-8, CCK-4, gastrin-17, CCK-8, CCK-39 peptide - - 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 αi1 Human - 64 β1 Human γ2 Human cryo-EM 7EW4 - 3.2 S1PR3 S1P3 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - CYM-5541 pubchem gtoplig chembl_ligand
small-molecule Agonist sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate 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 Human - 60 β1 Human γ2 Human cryo-EM 7RTB 7RTB_refined 2.1 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Peptide-19
peptide Agonist glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide peptide Johnson RM, Zhang X, Piper SJ, Nettleton TJ, Vandekolk TH, Langmead CJ, Danev R, Sexton PM, Wootten D 10.1016/J.BBRC.2021.09.016 2021-10-06
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 desulfated gastrin-34, desulfated gastrin-14, desulfated cholecystokinin-8, CCK-33, CCK-4, CCK-58, gastrin-71, gastrin-34, desulfated gastrin-17, gastrin-17, CCK-8, gastrin-14, CCK-39, desulfated gastrin-71 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 7F58 7F58_refined 3.1 MC4R MC4 Melanocortin A (Rhodopsin) Human - Nanobody-35 - THIQ pubchem gtoplig chembl_ligand
small-molecule Agonist β-MSH, ACTH, γ-MSH, agouti-related protein, α-MSH 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 β-MSH, ACTH, γ-MSH, agouti-related protein, α-MSH 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 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 - - 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 - - 2021-12-01
Gi/o αi1 Human - 61 β1 Human γ2 Human cryo-EM 7NA8 7NA8_refined 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 - 57 β1 Human γ2 Human cryo-EM 7VUI - 3.3 GP139 GPR139 A orphans A (Rhodopsin) Human - Nanobody-35 Xylanase JNJ-63533054 pubchem gtoplig chembl_ligand
small-molecule Agonist L-tryptophan, L-phenylalanine 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, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate 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 - 96 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 7EVZ 7EVZ_refined 3.1 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - cenerimod pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate 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 7F4F 7F4F_refined 2.9 MSHR MC1 Melanocortin A (Rhodopsin) Human - scFv16 - CHEMBL407070 chembl_ligand pubchem pubchem
protein Agonist β-MSH, α-MSH, ACTH, γ-MSH 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 7T6T 7T6T_refined 3.2 FPR1 FPR1 Formylpeptide A (Rhodopsin) Human - - - synthetic peptide
peptide Agonist fMet-Leu-Phe, spinorphin, annexin I, cathepsin G peptide - - 2022-03-30
Gi/o αi1 Human - 63 β1 Human γ2 Human cryo-EM 7VGX 7VGX_refined 3.2 NPY1R Y1 Neuropeptide Y A (Rhodopsin) Human - scFv16 - neuropeptide Y pubchem gtoplig chembl_ligand gtoplig gtoplig pubchem pubchem pubchem
peptide Agonist peptide YY, pancreatic polypeptide, neuropeptide Y peptide Park C, Kim J, Ko SB, Choi YK, Jeong H, Woo H, Kang H, Bang I, Kim SA, Yoon TY, Seok C, Im W, Choi HJ 10.1038/S41467-022-28510-6 2022-02-23
Gi/o αi1 Human - 64 β1 Human γ2 Human cryo-EM 7VKT 7VKT_refined 2.9 LT4R1 BLT1 Leukotriene A (Rhodopsin) Human - scFv16 - LTB4 pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist LTB4, 20-hydroxy-LTB4, 12R-HETE small-molecule Wang N, He X, Zhao J, Jiang H, Cheng X, Xia Y, Eric Xu H, He Y 10.1038/S41467-022-28820-9 2022-03-09
Gi/o αi1 Mouse - 62 β1 Bovine γ2 Bovine cryo-EM 7TD1 7TD1_refined 3.1 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human - - - (2r)-2-Hydroxy-3-(Phosphonooxy)propyl (9e)-Octadec-9-Enoate pubchem
small-molecule Agonist 1-O-Oleoyl-D-glycerol 3-phosphoric acid small-molecule Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY 10.1038/S41467-022-28417-2 2022-02-09
Gi/o αi1 Human - 62 β1 Rat γ2 Bovine cryo-EM 7VGY 7VGY_refined 3.1 MTR1A MT1 Melatonin A (Rhodopsin) Human - scFv16 - 2-iodo-melatonin pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist melatonin small-molecule - - 2022-03-02
Gs αs Human - 58 β1 Human γ2 Human cryo-EM 7TYI 7TYI_refined 3.3 CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - Amylin rat pubchem
peptide Agonist adrenomedullin 2/intermedin, amylin, adrenomedullin, calcitonin (salmon), α-CGRP, β-CGRP, calcitonin 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 Human - 58 β1 Human γ2 Human cryo-EM 7TYW 7TYW_refined 3.0 CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - calcitonin (salmon synthetic) pubchem
small-molecule Agonist adrenomedullin 2/intermedin, amylin, adrenomedullin, calcitonin (salmon), α-CGRP, β-CGRP, calcitonin 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 Bovine - 59 β1 Rat γ2 Bovine cryo-EM 7FIN 7FIN_refined 3.1 GIPR GIP Glucagon B1 (Secretin) Human - Nanobody-35 - Peptide-20
peptide Agonist gastric inhibitory polypeptide peptide Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW 10.1038/S41467-022-28683-0 2022-02-23
Gs αs Bovine - 57 β1 Rat γ2 Bovine cryo-EM 7FIM 7FIM_refined 3.4 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - tirzepatide pubchem gtoplig
peptide Agonist glucagon, glucagon-like peptide 1-(7-37), 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 - 59 β1 Human γ2 Human cryo-EM 7EJA 7EJA_refined 3.6 ADA2A α2A Adrenoceptors A (Rhodopsin) Human - scFv16 - dexmedetomidine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist (-)-adrenaline, (-)-noradrenaline small-molecule - - 2022-04-13
Gi/o αi2 Human - 63 β1 Human γ2 Human cryo-EM 7WVW 7WVW_refined 3.1 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human BRIL - - FME-TYR-PHE-ILE-ASN-ILE-LEU-THE-LEU
peptide Agonist serum amyloid A, LTC4, LXA4, fMet-Leu-Phe, aspirin triggered lipoxin A4, PrP106-126, resolvin D1, LTD4, 15-deoxy-LXA4, annexin I, LL-37, humanin, aspirin-triggered resolvin D1, ATLa2 peptide Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B 10.1038/S41467-022-29361-X 2022-04-13
Gq/11 αq Human - 60 β1 Rat γ2 Bovine cryo-EM 7WQ4 7WQ4_refined 2.6 GALR2 GAL2 Galanin A (Rhodopsin) Human - Nanobody-35 - galanin gtoplig chembl_ligand gtoplig pubchem pubchem pubchem pubchem pubchem
peptide Agonist spexin-1, galanin, galanin-like peptide peptide - - 2022-04-20
G12/13 α13 Human - 60 β1 Human γ2 Human cryo-EM 7T6B - 3.2 S1PR2 S1P2 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - sphingosine 1-phosphate pubchem gtoplig chembl_ligand pubchem
small-molecule Agonist sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate small-molecule - - 2022-04-06
Gi/o αi1 Human - 64 β1 Human γ2 Human cryo-EM 7TUZ 7TUZ_refined 3.1 GP183 GPR183 A orphans A (Rhodopsin) Human - scFv16 - (2S,4aS,4bS,7R,8S,8aS,9R,10aR)-7-[(2R,3R)-7-hydroxy-3,7-dimethyloctan-2-yl]-4a,7,8-trimethyltetradecahydrophenanthrene-2,9-diol pubchem
small-molecule Agonist 25-hydroxycholesterol, 7β-hydroxycholesterol, 7β, 27-dihydroxycholesterol, 7α,25-dihydroxycholesterol, 7β, 25-dihydroxycholesterol, 27-hydroxycholesterol, 7α,27-dihydroxycholesterol, 7α-hydroxycholesterol small-molecule Chen H, Huang W, Li X 10.1016/J.STR.2022.04.006 2022-04-13
Gs αs Human Engineered G alpha 53 β1 Human γ2 Human cryo-EM 7RGP - 2.9 GLP1R GLP-1 Glucagon B1 (Secretin) Human - scFv16
Nanobody-35 		- tirzepatide pubchem gtoplig
peptide Agonist glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide peptide Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW 10.1073/PNAS.2116506119 2022-04-13
Gi/o αi1 Human Mini-Gi1 58 β1 Human γ2 Human cryo-EM 7WU4 7WU4_refined 3.4 AGRF1 ADGRF1 ADGRF B2 (Adhesion) Human - - - Apo (no ligand)
none Apo (no ligand) - - Qu X, Qiu N, Wang M, Zhang B, Du J, Zhong Z, Xu W, Chu X, Ma L, Yi C, Han S, Shui W, Zhao Q, Wu B 10.1038/S41586-022-04580-W 2022-04-27
Gs αs Human Mini-Gs 55 β1 Human γ2 Human cryo-EM 7WUJ - 3.3 AGRG4 ADGRG4 ADGRG B2 (Adhesion) Human - scFv16
Nanobody-35 		- Apo (no ligand)
none Apo (no ligand) - - Xiao P, Guo S, Wen X, He QT, Lin H, Huang SM, Gou L, Zhang C, Yang Z, Zhong YN, Yang CC, Li Y, Gong Z, Tao XN, Yang ZS, Lu Y, Li SL, He JY, Wang C, Zhang L, Kong L, Sun JP, Yu X 10.1038/S41586-022-04590-8 2022-04-27
Gs αs Human - 60 β1 Human γ2 Human cryo-EM 7XTB - 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
Gs αs Human - 58 β1 Human γ2 Human cryo-EM 7CX3 7CX3_refined 2.8 PE2R2 EP2 Prostanoid A (Rhodopsin) Human - Nanobody-35 - taprenepag pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist thromboxane A2, PGD2, PGE2, PGE1, PGI2, PGF2α 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 7MBX_refined 2.0 CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human - Nanobody-35 - CHEMBL216166 chembl_ligand pubchem
protein Agonist CCK-58, CCK-33, desulfated cholecystokinin-8, CCK-4, gastrin-17, CCK-8, CCK-39 peptide - - 2021-05-26
Gs αs Human - 55 β1 Human γ2 Human cryo-EM 7BB7 7BB7_refined 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 7E9G_refined 3.5 GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human - scFv16 DN13 eglumegad pubchem gtoplig chembl_ligand gtoplig
JNJ-40411813 pubchem gtoplig chembl_ligand drugbank
small-molecule
small-molecule 		Agonist
PAM 		L-glutamic acid small-molecule Lin S, Han S, Cai X, Tan Q, Zhou K, Wang D, Wang X, Du J, Yi C, Chu X, Dai A, Zhou Y, Chen Y, Zhou Y, Liu H, Liu J, Yang D, Wang MW, Zhao Q, Wu B 10.1038/S41586-021-03495-2 2021-06-23
Gi/o αi1 Human - 62 β1 Human γ2 Human cryo-EM 7JHJ 7JHJ_refined 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
Gi/o αi1 Human - 61 β1 Human γ2 Human cryo-EM 7F1Q 7F1Q_refined 2.9 CCR5 CCR5 Chemokine A (Rhodopsin) Human - - - CCL3 gtoplig
peptide Agonist CCL14, CCL2, CCL8, CCL7, CCL16, CCL13, CCL11, CCL5, CCL3, CCL4 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
Gi/o αi1 Human - 61 β1 Human γ2 Human cryo-EM 7EZH 7EZH_refined 3.2 CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human - scFv16 - CCK-8 pubchem gtoplig chembl_ligand drug_central drugbank
peptide Agonist CCK-58, CCK-33, desulfated cholecystokinin-8, CCK-4, gastrin-17, CCK-8, CCK-39 peptide - - 2021-08-25
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, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate 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 - - - Choriogonadotropin beta gtoplig
Glycoprotein alpha gtoplig
protein
protein 		Agonist LH, hCG peptide Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE 10.1038/S41586-021-03924-2 2021-09-29
Gq/11 αq Human Gq-Gi1 chimera 61 β1 Rat γ2 Bovine cryo-EM 7EIB 7EIB_refined 3.0 BKRB1 B1 Bradykinin A (Rhodopsin) Human - - - [des-Arg10]kallidin pubchem gtoplig chembl_ligand gtoplig
peptide Agonist kallidin, bradykinin, [des-Arg10]kallidin, Lys-[Hyp3]-bradykinin, [Hyp3]bradykinin, T-kinin, [des-Arg9]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
Gs