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G PROTEIN
STRUCTURE
RECEPTOR
OTHER PROTEINS
STRUCTURE LIGAND
ENDOGENOUS LIGAND
REFERENCE
Fam. α Species Note % of Seq β Species γ Species Method
PDB
Refined
structure
Resolution
UniProt
IUPHAR Receptor family Class Species Receptor fusion Antibodies Other Name Type Function Name Type Authors Reference PDB Date
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, PTHrP, PTHrP-(1-36), TIP39 peptide - - 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 None 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 - - None 10.1038/S41586-019-1286-0 2019-06-12
Gi/o αi1 Human - 100 β1 Human γ2 Human Cryo-EM 6PT0 6PT0_refined 3.2 CNR2 CB2 Cannabinoid A (Rhodopsin) Human - scFv16 - WIN55212-2 pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist 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
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 - - 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 (-)-noradrenaline, (-)-adrenaline small-molecule Yuan D, Liu Z, Kaindl J, Maeda S, Zhao J, Sun X, Xu J, Gmeiner P, Wang HW, Kobilka BK 10.1038/S41589-020-0492-2 2020-04-15
Gi/o αo Human - 59 β1 Rat γ2 Mouse Cryo-EM 6WWZ 6WWZ_refined 3.3 CCR6 CCR6 Chemokine A (Rhodopsin) Human - scFv16 - CCL20 gtoplig
peptide Agonist CCL20, beta-defensin 4A peptide Wasilko DJ, Johnson ZL, Ammirati M, Che Y, Griffor MC, Han S, Wu H 10.1038/S41467-020-16820-6 2020-06-24
Gs αs Human - 50 β1 Bovine γ2 Bovine Cryo-EM 7BZ2 7BZ2_refined 3.8 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - Nanobody-35 - arformoterol pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline, L-NOREPINEPHRINE small-molecule Zhang Y, Yang F, Ling S, Lv P, Zhou Y, Fang W, Sun W, Zhang L, Shi P, Tian C 10.1038/S41421-020-0176-9 2020-08-05
Gi/o αi1 Human - 65 β1 Human γ2 Human Cryo-EM 6LFO 6LFO_refined 3.4 CXCR2 CXCR2 Chemokine A (Rhodopsin) Human - scFv16 - Interleukin-8 pubchem
protein Agonist CXCL5, CXCL3, CXCL6, CXCL2, CXCL1, CXCL8, CXCL7 peptide Liu K, Wu L, Yuan S, Wu M, Xu Y, Sun Q, Li S, Zhao S, Hua T, Liu ZJ 10.1038/S41586-020-2492-5 2020-09-02
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 6XBM - 3.2 SMO SMO Frizzled F (Frizzled) Human - scFv16 - 24,25-Epoxy-cholesterol pubchem
24,25-Epoxy-cholesterol pubchem
small-molecule
small-molecule
Agonist
PAM
- - Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X 10.1038/S41589-020-0646-2 2020-09-30
Gs αs Human - 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 5-hydroxytryptamine, noradrenaline, dopamine, (-)-noradrenaline, L-NOREPINEPHRINE 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 - 62 β1 Human γ2 Human Cryo-EM 7E32 - 2.9 5HT1D 5-HT1D 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - 5-hydroxytryptamine pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist 5-HT-moduline, 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 2021-04-21
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 ACTH, γ-MSH, α-MSH, agouti-related protein, β-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
Gq/11 αq Human Gq-Gs-Gi1 chimera 55 β1 Rat γ2 Human Cryo-EM 7MBY - 2.4 CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human - - - CHEMBL216166 chembl_ligand pubchem
protein Agonist desulfated cholecystokinin-8, CCK-33, CCK-8, CCK-39, gastrin-17, CCK-58, CCK-4 peptide Mobbs JI, Belousoff MJ, Harikumar KG, Piper SJ, Xu X, Furness SGB, Venugopal H, Christopoulos A, Danev R, Wootten D, Thal DM, Miller LJ, Sexton PM 10.1371/JOURNAL.PBIO.3001295 2021-05-26
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7F1S 7F1S_refined 2.8 CCR5 CCR5 Chemokine A (Rhodopsin) Human - - - Apo (no ligand)
none Apo (no ligand) CCL5, CCL13, CCL3, CCL14, CCL8, CCL2, CCL16, CCL7, CCL11, CCL4 peptide None 10.1038/S41467-021-24438-5 2021-07-14
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 desulfated cholecystokinin-8, CCK-33, CCK-8, CCK-39, gastrin-17, CCK-58, CCK-4 peptide Liu Q, Yang D, Zhuang Y, Croll TI, Cai X, Dai A, He X, Duan J, Yin W, Ye C, Zhou F, Wu B, Zhao Q, Xu HE, Wang MW, Jiang Y 10.1038/S41589-021-00841-3 2021-08-25
Gi/o αi2 Human - 59 β1 Human γ2 Human Cryo-EM 7LD3 - 3.2 AA1R A1 Adenosine A (Rhodopsin) Human - - - {2-Amino-4-[3,5-bis(trifluoromethyl)phenyl]thiophen-3-yl}(4-chlorophenyl)methanone pubchem
adenosine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule
small-molecule
Ago-PAM
Agonist
adenosine small-molecule - - 2021-09-08
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 gastrin-34, desulfated cholecystokinin-8, desulfated gastrin-14, desulfated gastrin-17, gastrin-14, desulfated gastrin-34, gastrin-17, CCK-33, CCK-8, CCK-39, gastrin-71, CCK-4, CCK-58, 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 ACTH, γ-MSH, α-MSH, agouti-related protein, β-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
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7VDH - 2.9 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human - scFv16 - compound 48/80 pubchem gtoplig
small-molecule Agonist PAMP-20 peptide Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP 10.1038/S41586-021-04077-Y 2021-12-01
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7VV5 7VV5_refined 2.8 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human - scFv16 - compound 48/80 pubchem gtoplig
small-molecule Agonist PAMP-20 peptide Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP 10.1038/S41586-021-04077-Y 2021-12-01
Gi/o αi1 Human - 40 β1 Human γ2 Human Cryo-EM 7WF7 7WF7_refined 3.4 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - sphingosine 1-phosphate pubchem gtoplig chembl_ligand pubchem
small-molecule Agonist sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 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 - 57 β1 Rat γ2 Bovine Cryo-EM 7V9M 7V9M_refined 3.3 GHRHR GHRH Glucagon B1 (Secretin) Human - Nanobody-35 - Somatoliberin pubchem
peptide Agonist GHRH peptide Cong Z, Zhou F, Zhang C, Zou X, Zhang H, Wang Y, Zhou Q, Cai X, Liu Q, Li J, Shao L, Mao C, Wang X, Wu J, Xia T, Zhao LH, Jiang H, Zhang Y, Xu HE, Cheng X, Yang D, Wang MW 10.1073/PNAS.2106606118 2021-10-20
Gi/o αi1 Human - 61 β1 Rat γ2 Bovine Cryo-EM 7T6V 7T6V_refined 3.1 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human - scFv16 - synthetic peptide
peptide Agonist aspirin-triggered resolvin D1, LL-37, resolvin D1, 15-deoxy-LXA4, LXA4, LTD4, LTC4, aspirin triggered lipoxin A4, fMet-Leu-Phe, serum amyloid A, PrP106-126, annexin I, humanin peptide Zhuang Y, Wang L, Guo J, Sun D, Wang Y, Liu W, Xu HE, Zhang C 10.1038/S41467-022-28586-0 2022-03-30
Gi/o αi3 Human - 62 β1 Human γ2 Human Cryo-EM 7T11 7T11_refined 2.7 SSR2 SST2 Somatostatin A (Rhodopsin) Human - scFv16 - Octreotide
peptide Agonist SRIF-28, CST-17, cortistatin-14, SRIF-14 peptide Robertson MJ, Meyerowitz JG, Panova O, Borrelli K, Skiniotis G 10.1038/S41594-022-00727-5 2022-03-09
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7VKT 7VKT_refined 2.9 LT4R1 BLT1 Leukotriene A (Rhodopsin) Human - scFv16 - LTB4 pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist LTB4, 12R-HETE, 20-hydroxy-LTB4 small-molecule Wang N, He X, Zhao J, Jiang H, Cheng X, Xia Y, Eric Xu H, He Y 10.1038/S41467-022-28820-9 2022-03-09
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7TYL - 3.3 CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - Amylin rat pubchem
peptide Agonist α-CGRP, calcitonin, adrenomedullin 2/intermedin, adrenomedullin, amylin, calcitonin (salmon), β-CGRP peptide Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM 10.1126/SCIENCE.ABM9609 2022-03-23
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7TYW - 3.0 CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - calcitonin (salmon synthetic) pubchem
small-molecule Agonist α-CGRP, calcitonin, adrenomedullin 2/intermedin, adrenomedullin, amylin, calcitonin (salmon), β-CGRP peptide Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM 10.1126/SCIENCE.ABM9609 2022-03-23
Gs αs Human 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 αi1 Human - 64 β1 Rat γ2 Bovine Cryo-EM 7WQ3 7WQ3_refined 2.7 GALR1 GAL1 Galanin A (Rhodopsin) Human - scFv16 - galanin pubchem gtoplig chembl_ligand gtoplig pubchem pubchem pubchem pubchem
peptide Agonist galanin, galanin-like peptide peptide Duan J, Shen DD, Zhao T, Guo S, He X, Yin W, Xu P, Ji Y, Chen LN, Liu J, Zhang H, Liu Q, Shi Y, Cheng X, Jiang H, Eric Xu H, Zhang Y, Xie X, Jiang Y 10.1038/S41467-022-29072-3 2022-04-20
Gi/o αi1 Human - 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 7α-hydroxycholesterol, 7β, 27-dihydroxycholesterol, 7α,27-dihydroxycholesterol, 7β-hydroxycholesterol, 25-hydroxycholesterol, 27-hydroxycholesterol, 7α,25-dihydroxycholesterol, 7β, 25-dihydroxycholesterol small-molecule Chen H, Huang W, Li X 10.1016/J.STR.2022.04.006 2022-04-13
Gs αs Human - 56 β1 Human γ2 Human Cryo-EM 7RBT 7RBT_refined 3.1 GIPR GIP Glucagon B1 (Secretin) Human - scFv16
Nanobody-35
- tirzepatide pubchem gtoplig
2-fluoro-4-[(1R)-6-methoxy-1-methyl-2-{(1S)-1-[4-(propan-2-yl)phenyl]ethyl}-1,2,3,4-tetrahydroisoquinolin-5-yl]-6-[(2-methylpropyl)amino]phenol pubchem
peptide
small-molecule
Agonist
PAM
gastric inhibitory polypeptide peptide Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW 10.1073/PNAS.2116506119 2022-04-13
Gs αs Bovine - 60 β1 Rat γ2 Bovine Cryo-EM 7WBJ - 3.4 VIPR2 VPAC2 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - PACAP-27 pubchem gtoplig pubchem
peptide Agonist PACAP-27, GHRH, PACAP-38, secretin, VIP, PHI peptide Xu Y, Feng W, Zhou Q, Liang A, Li J, Dai A, Zhao F, Yan J, Chen CW, Li H, Zhao LH, Xia T, Jiang Y, Xu HE, Yang D, Wang MW 10.1038/S41467-022-30041-Z 2022-05-18
Gq/11 αq Human - 63 β1 Human γ2 Human Cryo-EM 7F6I 7F6I_refined 2.8 BKRB2 B2 Bradykinin A (Rhodopsin) Human - - - kallidin pubchem gtoplig
peptide Agonist Lys-[Hyp3]-bradykinin, T-kinin, kallidin, [Hyp3]bradykinin, bradykinin, [des-Arg9]bradykinin, [des-Arg10]kallidin peptide Shen J, Zhang D, Fu Y, Chen A, Yang X, Zhang H 10.1038/S41467-022-28399-1 2022-01-05
Gq/11 αq Human - 58 β1 Human γ2 Human Cryo-EM 7XJK 7XJK_refined 3.3 GALR2 GAL2 Galanin A (Rhodopsin) Human - scFv16 - Galanin, Human pubchem
peptide Agonist galanin, spexin-1, galanin-like peptide peptide - - 2022-06-29
Gs αs Human - 59 β1 Rat γ2 Human Cryo-EM 7X8R - 2.6 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - CHEMBL2158411 chembl_ligand pubchem
small-molecule Agonist glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) peptide Cong Z, Zhou Q, Li Y, Chen LN, Zhang ZC, Liang A, Liu Q, Wu X, Dai A, Xia T, Wu W, Zhang Y, Yang D, Wang MW 10.1073/PNAS.2200155119 2022-06-29
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7XT8 - 3.1 5HT4R 5-HT4 5-Hydroxytryptamine A (Rhodopsin) Human BRIL Nanobody-35 - 5-hydroxytryptamine pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist 5-hydroxytryptamine small-molecule Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE 10.1016/J.MOLCEL.2022.05.031 2022-07-27
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7XBW 7XBW_refined 2.8 CX3C1 CX3CR1 Chemokine A (Rhodopsin) Human - - - Apo (no ligand)
none Apo (no ligand) CX3CL1 peptide Lu M, Zhao W, Han S, Lin X, Xu T, Tan Q, Wang M, Yi C, Chu X, Yang W, Zhu Y, Wu B, Zhao Q 10.1126/SCIADV.ABN8048 2022-07-13
Gq/11 αq Human Gi2-mini-Gq chimera 57 β1 Human γ2 Human Cryo-EM 8DPF - 2.8 5HT2C 5-HT2C 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - lorcaserin pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist 5-hydroxytryptamine small-molecule Gumpper RH, Fay JF, Roth BL 10.1016/J.CELREP.2022.111211 2022-08-24
Gq/11 αq Human - 57 β1 Bovine γ2 Bovine Cryo-EM 7X1T - 3.3 TRFR TRH1 Thyrotropin-releasing hormone A (Rhodopsin) Human - scFv16 - taltirelin pubchem gtoplig chembl_ligand
small-molecule Agonist TRH peptide Yang F, Zhang H, Meng X, Li Y, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C 10.1038/S41422-022-00646-6 2022-08-31
Gs αs Human - 58 β1 Rat γ2 Bovine Cryo-EM 7VVM 7VVM_refined 3.2 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - Parathyroid hormone
peptide Agonist PTH, PTHrP, PTHrP-(1-36), TIP39 peptide Kobayashi K, Kawakami K, Kusakizako T, Miyauchi H, Tomita A, Kobayashi K, Shihoya W, Yamashita K, Nishizawa T, Kato HE, Inoue A, Nureki O 10.1016/J.MOLCEL.2022.07.003 2022-08-03
Gi/o αo Human - 63 β1 Rat γ2 Mouse Cryo-EM 7TS0 7TS0_refined 2.8 CRFR2 CRF2 Corticotropin-releasing factor B1 (Secretin) Human - scFv16 - Urocortin pubchem
peptide Agonist urocortin 2, urocortin 3, urocortin 1, corticotrophin-releasing hormone peptide Zhao LH, Lin J, Ji SY, Zhou XE, Mao C, Shen DD, He X, Xiao P, Sun J, Melcher K, Zhang Y, Yu X, Xu HE 10.1038/S41467-022-33851-3 2022-11-09
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7U2K - 3.3 OPRM μ Opioid A (Rhodopsin) Mouse - - - CHEMBL147044 chembl_ligand pubchem
small-molecule Agonist - - Faouzi A, Wang H, Zaidi SA, DiBerto JF, Che T, Qu Q, Robertson MJ, Madasu MK, El Daibani A, Varga BR, Zhang T, Ruiz C, Liu S, Xu J, Appourchaux K, Slocum ST, Eans SO, Cameron MD, Al-Hasani R, Pan YX, Roth BL, McLaughlin JP, Skiniotis G, Katritch V, Kobilka BK, Majumdar S 10.1038/S41586-022-05588-Y 2022-12-07
G12/13 α12 Human Mini-G12 55 β1 Human γ2 Human Cryo-EM 7WZ7 - 2.8 AGRF1 ADGRF1 ADGRF B2 (Adhesion) Human - scFv16 - Apo (no ligand)
none Apo (no ligand) - - Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y 10.1038/S41467-022-33173-4 2022-09-28
Gi/o αi1 Human - 63 β1 Rat γ2 Bovine Cryo-EM 7YU5 7YU5_refined 3.3 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human - scFv16 - [(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate pubchem
small-molecule Agonist 1-O-Oleoyl-D-glycerol 3-phosphoric acid small-molecule Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O 10.1038/S41467-022-33121-2 2022-10-05
Gi/o αi1 Human - 63 β1 Rat γ2 Bovine Cryo-EM 7YU8 - 4.5 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human - scFv16 - [(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate pubchem
small-molecule Agonist 1-O-Oleoyl-D-glycerol 3-phosphoric acid small-molecule Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O 10.1038/S41467-022-33121-2 2022-10-05
Gi/o αo Human Mini-Go 61 β1 Human γ2 Human Cryo-EM 8E9X - 2.7 ACM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - CHEMBL73538 chembl_ligand pubchem
small-molecule Agonist acetylcholine small-molecule - - 2022-11-30
Gi/o αi1 Human - 62 β1 Rat γ2 Bovine Cryo-EM 8F7S 8F7S_refined 3.0 OPRD δ Opioid A (Rhodopsin) Human - - - DELTORPHIN II chembl_ligand pubchem
protein Agonist dynorphin A-(1-13), dynorphin A-(1-8), [Met]enkephalin, α-neoendorphin, dynorphin A, dynorphin B, endomorphin-1, β-endorphin, [Leu]enkephalin peptide Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y, Roth BL, Xu HE 10.1016/J.CELL.2022.12.026 2022-12-14
Gi/o αi2 Human - 58 β1 Bovine γ2 Bovine Cryo-EM 7YJ4 - 3.2 RL3R2 RXFP4 Relaxin family peptide A (Rhodopsin) Human - scFv16 - Insulin-like peptide INSL5 A chain pubchem
Insulin-like peptide INSL5 B chain pubchem
peptide
peptide
Agonist relaxin-3, relaxin-3 (B chain), INSL5 peptide - - 2023-03-01
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7YON 7YON_refined 3.0 NPY2R Y2 Neuropeptide Y A (Rhodopsin) Human - scFv16 - Peptide YY
peptide Agonist pancreatic polypeptide, PYY-(3-36), peptide YY, neuropeptide Y-(3-36), neuropeptide Y peptide Kang H, Park C, Choi YK, Bae J, Kwon S, Kim J, Choi C, Seok C, Im W, Choi HJ 10.1016/J.STR.2022.11.010 2023-03-22
Gi/o αo Human Mini-Go 60 β1 Human γ2 Human Cryo-EM 8FN0 - 2.9 NTR1 NTS1 Neurotensin A (Rhodopsin) Rat - scFv16 - neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
CHEMBL4576388 chembl_ligand pubchem
peptide
small-molecule
Agonist
PAM
neuromedin N, neurotensin peptide - - 2023-03-29
Gs αs Human Mini-Gs 59 β1 Human γ2 Human Cryo-EM 8HDO - 2.9 AA2BR A2B Adenosine A (Rhodopsin) Human - Nanobody-35 - BAY 60-6583 pubchem gtoplig chembl_ligand
small-molecule Agonist adenosine small-molecule None 10.1038/S41421-022-00503-1 2023-01-18
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) - - None 10.1038/NATURE07330 2008-09-23
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 - 64 β1 Human γ2 Human Cryo-EM 6KPG 6KPG_refined 3.0 CNR1 CB1 Cannabinoid A (Rhodopsin) Human - scFv16 - AM841 pubchem gtoplig chembl_ligand
small-molecule Agonist anandamide, 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
Gi/o αo Human - 60 β1 Mouse γ2 Human Cryo-EM 6K41 - 2.9 ADA2B α2B Adrenoceptors A (Rhodopsin) Human T4-Lysozyme scFv - dexmedetomidine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist (-)-noradrenaline, (-)-adrenaline small-molecule Yuan D, Liu Z, Kaindl J, Maeda S, Zhao J, Sun X, Xu J, Gmeiner P, Wang HW, Kobilka BK 10.1038/S41589-020-0492-2 2020-04-15
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 6VMS - 3.8 DRD2 D2 Dopamine A (Rhodopsin) Human T4-Lysozyme scFv16 - bromocriptine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist dopamine small-molecule Yin J, Chen KM, Clark MJ, Hijazi M, Kumari P, Bai XC, Sunahara RK, Barth P, Rosenbaum DM 10.1038/S41586-020-2379-5 2020-06-17
Gs αs 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
Gs αs Human - 89 β1 Human γ2 Human Cryo-EM 6X19 - 2.1 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - CHU-128 pubchem
small-molecule Agonist glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) peptide Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, Senel P, Stewart GD, Liang YL, Glukhova A, Venugopal H, Christopoulos A, Furness SGB, Miller LJ, Reedtz-Runge S, Langmead CJ, Gloriam DE, Danev R, Sexton PM, Wootten D 10.1016/J.MOLCEL.2020.09.020 2020-09-09
Gi/o αo Human - 61 β1 Human γ2 Human Cryo-EM 7D77 - 2.9 AGRG3 ADGRG3 ADGRG B2 (Adhesion) Human - scFv16 - HYDROCORTISONE chembl_ligand pubchem
small-molecule Agonist - - Ping YQ, Mao C, Xiao P, Zhao RJ, Jiang Y, Yang Z, An WT, Shen DD, Yang F, Zhang H, Qu C, Shen Q, Tian C, Li ZJ, Li S, Wang GY, Tao X, Wen X, Zhong YN, Yang J, Yi F, Yu X, Xu HE, Zhang Y, Sun JP 10.1038/S41586-020-03083-W 2021-02-03
Gs αs Human Engineered G alpha 58 β1 Human γ2 Human Cryo-EM 7L1V - 3.0 OX2R OX2 Orexin A (Rhodopsin) Human - scFv16
Nanobody-51
- compound 1 [PMID: 33547286] pubchem gtoplig chembl_ligand
small-molecule Agonist orexin-B, orexin-A peptide Hong C, Byrne NJ, Zamlynny B, Tummala S, Xiao L, Shipman JM, Partridge AT, Minnick C, Breslin MJ, Rudd MT, Stachel SJ, Rada VL, Kern JC, Armacost KA, Hollingsworth SA, O'Brien JA, Hall DL, McDonald TP, Strickland C, Brooun A, Soisson SM, Hollenstein K 10.1038/S41467-021-21087-6 2021-02-10
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 - 49 β1 Bovine γ2 Mouse Cryo-EM 7E14 - 2.9 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - N-Tert-butyl-6,7-dichloroquinoxalin-2-amine pubchem
orforglipron pubchem gtoplig chembl_ligand
small-molecule
small-molecule
Ago-PAM
Agonist
glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) peptide None 10.1038/S41467-021-24058-Z 2021-07-07
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7EW4 7EW4_refined 3.2 S1PR3 S1P3 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - CYM-5541 pubchem gtoplig chembl_ligand
small-molecule Agonist sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 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
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7S8O - 2.6 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human BRIL scFv16 - (R)-ZINC-3573 pubchem gtoplig chembl_ligand
small-molecule Agonist PAMP-20 peptide Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL 10.1038/S41586-021-04126-6 2021-11-17
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7VUJ 7VUJ_refined 3.8 GP139 GPR139 A orphans A (Rhodopsin) Human - Nanobody-35 Xylanase JNJ-63533054 pubchem gtoplig chembl_ligand
small-molecule Agonist L-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 7F4D - 3.0 MSHR MC1 Melanocortin A (Rhodopsin) Human - Nanobody-35 - INTERMEDINE chembl_ligand pubchem pubchem pubchem
protein Agonist ACTH, α-MSH, γ-MSH, β-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 Mouse - 62 β1 Bovine γ2 Bovine Cryo-EM 7TD2 - 3.1 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human - - - lysophosphatidic acid pubchem
small-molecule Agonist 1-O-Oleoyl-D-glycerol 3-phosphoric acid small-molecule Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY 10.1038/S41467-022-28417-2 2022-02-09
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7TYN - 2.6 CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - calcitonin (salmon synthetic) pubchem
small-molecule Agonist α-CGRP, calcitonin, adrenomedullin 2/intermedin, adrenomedullin, amylin, calcitonin (salmon), β-CGRP peptide Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM 10.1126/SCIENCE.ABM9609 2022-03-30
Gi/o αi2 Human - 63 β1 Human γ2 Human Cryo-EM 7WVW - 3.1 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human BRIL - - FME-TYR-PHE-ILE-ASN-ILE-LEU-THE-LEU
peptide Agonist aspirin-triggered resolvin D1, LL-37, resolvin D1, 15-deoxy-LXA4, LXA4, LTD4, LTC4, aspirin triggered lipoxin A4, fMet-Leu-Phe, serum amyloid A, PrP106-126, annexin I, humanin 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 αi2 Human - 61 β1 Human γ2 Human Cryo-EM 7WVX - 2.8 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human BRIL - - humanin pubchem gtoplig chembl_ligand pubchem
peptide Agonist aspirin-triggered resolvin D1, LL-37, resolvin D1, 15-deoxy-LXA4, LXA4, LTD4, LTC4, aspirin triggered lipoxin A4, fMet-Leu-Phe, serum amyloid A, PrP106-126, annexin I, humanin 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
Gs αs Bovine Gi1-Gs chimera 56 β1 Bovine γ2 Bovine Cryo-EM 7S0G - 3.9 ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey - - - LEVISOPRENALINE chembl_ligand chembl_ligand pubchem
small-molecule Agonist - - Alegre KO, Paknejad N, Su M, Lou JS, Huang J, Jordan KD, Eng ET, Meyerson JR, Hite RK, Huang XY 10.1038/S41594-021-00679-2 2021-11-17
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7V69 - 3.4 ACM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - Apo (no ligand)
none Apo (no ligand) acetylcholine small-molecule Wang J, Wu M, Chen Z, Wu L, Wang T, Cao D, Wang H, Liu S, Xu Y, Li F, Liu J, Chen N, Zhao S, Cheng J, Wang S, Hua T 10.1038/S41467-022-30595-Y 2022-05-11
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7F1O - 3.1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - dopamine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine, (-)-noradrenaline, L-NOREPINEPHRINE small-molecule Teng X, Chen S, Wang Q, Chen Z, Wang X, Huang N, Zheng S 10.1126/SCIADV.ABO4158 2022-06-15
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7X2C 7X2C_refined 3.2 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - fenoldopam pubchem gtoplig chembl_ligand drugbank drug_central pubchem gtoplig chembl_ligand pubchem pubchem gtoplig chembl_ligand pubchem
small-molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine, (-)-noradrenaline, L-NOREPINEPHRINE small-molecule Teng X, Chen S, Nie Y, Xiao P, Yu X, Shao Z, Zheng S 10.1038/S41467-022-30929-W 2022-06-29
Gs αs Human - 60 β1 Rat γ2 Human Cryo-EM 7X8S 7X8S_refined 3.1 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - WB4-24 pubchem gtoplig chembl_ligand
small-molecule Agonist glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) peptide Cong Z, Zhou Q, Li Y, Chen LN, Zhang ZC, Liang A, Liu Q, Wu X, Dai A, Xia T, Wu W, Zhang Y, Yang D, Wang MW 10.1073/PNAS.2200155119 2022-06-29
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7XTB 7XTB_refined 3.3 5HT6R 5-HT6 5-Hydroxytryptamine A (Rhodopsin) Human BRIL Nanobody-35 - 5-hydroxytryptamine pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist 5-hydroxytryptamine small-molecule Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE 10.1016/J.MOLCEL.2022.05.031 2022-07-27
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7XTQ 7XTQ_refined 3.2 GPBAR GPBA Bile acid A (Rhodopsin) Human - Nanobody-35 - CHEMBL2181246 chembl_ligand pubchem
small-molecule Agonist cholic acid, chenodeoxycholic acid, lithocholic acid, deoxycholic acid small-molecule Ma L, Yang F, Wu X, Mao C, Guo L, Miao T, Zang SK, Jiang X, Shen DD, Wei T, Zhou H, Wei Q, Li S, Shu Q, Feng S, Jiang C, Chu B, Du L, Sun JP, Yu X, Zhang Y, Zhang P 10.1073/PNAS.2117054119 2022-07-06
Gi/o αi1 Human - 62 β1 Mouse γ2 Mouse Cryo-EM 7Y15 7Y15_refined 2.9 MRGRD MRGPRD A orphans A (Rhodopsin) Human BRIL scFv16 - Apo (no ligand)
none Apo (no ligand) β-alanine small-molecule Suzuki S, Iida M, Hiroaki Y, Tanaka K, Kawamoto A, Kato T, Oshima A 10.1038/S42003-022-03668-3 2022-07-20
Gi/o αo Human - 59 β1 Human γ2 Human Cryo-EM 7QVM - 3.3 OXYR OT Vasopressin and oxytocin A (Rhodopsin) Human - scFv16 - oxytocin pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
peptide Agonist vasopressin, oxytocin peptide Waltenspuhl Y, Ehrenmann J, Vacca S, Thom C, Medalia O, Pluckthun A 10.1038/S41467-022-31325-0 2022-08-10
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7XW6 - 2.8 TSHR TSH Glycoprotein hormone A (Rhodopsin) Human - Nanobody-35 - M22 antibody light chain
M22 antibody heavy chain
N-[4-[[5-[(2S)-3-benzyl-5-hydroxy-4-oxo-1,2-dihydroquinazolin-2-yl]-2-methoxyphenyl]methoxy]phenyl]acetamide pubchem
protein
protein
small-molecule
Agonist TSH peptide Duan J, Xu P, Luan X, Ji Y, He X, Song N, Yuan Q, Jin Y, Cheng X, Jiang H, Zheng J, Zhang S, Jiang Y, Xu HE 10.1038/S41586-022-05173-3 2022-08-17
Gs αs Human - 57 β1 Human γ2 Human Cryo-EM 7XKF - 2.4 AGRG2 ADGRG2 ADGRG B2 (Adhesion) Mouse - Nanobody-35 - PRASTERONE chembl_ligand pubchem
small-molecule Agonist - - Lin H, Xiao P, Bu RQ, Guo S, Yang Z, Yuan D, Zhu ZL, Zhang CX, He QT, Zhang C, Ping YQ, Zhao RJ, Ma CS, Liu CH, Zhang XN, Jiang D, Huang S, Xi YT, Zhang DL, Xue CY, Yang BS, Li JY, Lin HC, Zeng XH, Zhao H, Xu WM, Yi F, Liu Z, Sun JP, Yu X 10.1038/S41589-022-01084-6 2022-08-10
Gs αs Human Mini-Gs 59 β1 Human γ2 Human Cryo-EM 7WXW - 2.8 AGRF1 ADGRF1 ADGRF B2 (Adhesion) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y 10.1038/S41467-022-33173-4 2022-09-28
Gi/o αgust Human - 63 β1 Human γ2 Human Cryo-EM 7XP4 - 3.0 T2R46 TAS2R46 Taste 2 T (Taste 2) Human - Nanobody-35 Endoglucanase H Apo (no ligand)
none Apo (no ligand) - - Xu W, Wu L, Liu S, Liu X, Cao X, Zhou C, Zhang J, Fu Y, Guo Y, Wu Y, Tan Q, Wang L, Liu J, Jiang L, Fan Z, Pei Y, Yu J, Cheng J, Zhao S, Hao X, Liu ZJ, Hua T 10.1126/SCIENCE.ABO1633 2022-10-12
Gs αs Human - 56 β1 Human γ2 Human Cryo-EM 8E3Y - 2.3 VIPR1 VPAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - [Ac-His1]PACAP-27 gtoplig chembl_ligand pubchem
peptide Agonist PHM, PACAP-27, GHRH, PACAP-38, secretin, VIP, PHI peptide - - 2022-11-23
Gs αs Human Mini-Gs 61 β1 Human γ2 Human Cryo-EM 8HJ2 8HJ2_refined 3.8 GPR21 GPR21 A orphans A (Rhodopsin) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - - - 2023-03-15
Gi/o αo Human - 62 β1 Human γ2 Human Cryo-EM 7T96 7T96_refined 3.2 ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - acetylcholine pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
LY2119620 pubchem gtoplig chembl_ligand
small-molecule
small-molecule
Agonist
PAM
acetylcholine small-molecule - - 2023-01-25
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7YAE 7YAE_refined 3.4 SSR2 SST2 Somatostatin A (Rhodopsin) Human - scFv16 - Octreotide
peptide Agonist SRIF-28, CST-17, cortistatin-14, SRIF-14 peptide Zhao J, Fu H, Yu J, Hong W, Tian X, Qi J, Sun S, Zhao C, Wu C, Xu Z, Cheng L, Chai R, Yan W, Wei X, Shao Z 10.1038/S41467-023-36673-Z 2023-04-19
Gs αs Human - 57 β1 Rat γ2 Bovine Cryo-EM 7Y36 - 2.8 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - teriparatide pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem pubchem pubchem pubchem pubchem
peptide Agonist PTH, PTHrP, PTHrP-(1-36), TIP39 peptide - - 2023-07-05
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 8IUL - 2.8 PF2R FP Prostanoid A (Rhodopsin) Human - scFv16 - latanoprost (free acid form) pubchem gtoplig chembl_ligand
small-molecule Agonist PGF, thromboxane A2, PGI2, PGD2, PGE2 small-molecule Wu C, Xu Y, He Q, Li D, Duan J, Li C, You C, Chen H, Fan W, Jiang Y, Eric Xu H 10.1038/S41467-023-38411-X 2023-07-12
Gi/o 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 - - None 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 - - None 10.1038/NATURE09795 2011-03-16
Gs αs Bovine - 89 β1 Rat γ2 Bovine X-ray 3SN6 - 3.2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human T4-Lysozyme Antibody - CHEMBL1615159 chembl_ligand pubchem
small-molecule Agonist (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline, L-NOREPINEPHRINE small-molecule None 10.1038/NATURE10361 2011-07-20
Gi/o αt1 Bovine Only H5 3 - - - - X-ray 4J4Q 4J4Q_refined 2.7 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - B-Octylglucoside pubchem
small-molecule unknown - - Park JH, Morizumi T, Li Y, Hong JE, Pai EF, Hofmann KP, Choe HW, Ernst OP 10.1002/ANIE.201302374 2013-10-30
Gs αs Human Engineered G protein 50 - - - - X-ray 5G53 5G53_refined 3.4 AA2AR A2A Adenosine A (Rhodopsin) Human - - - NECA pubchem gtoplig chembl_ligand gtoplig
small-molecule Agonist adenosine small-molecule Carpenter B, Nehme R, Warne T, Leslie AG, Tate CG 10.1038/NATURE18966 2016-08-03
Gs αs Human - 47 β1 Human γ2 Human Cryo-EM 5UZ7 - 4.1 CALCR CT Calcitonin B1 (Secretin) Human - - - calcitonin (salmon synthetic) pubchem
small-molecule Agonist α-CGRP, calcitonin, adrenomedullin 2/intermedin, adrenomedullin, amylin, calcitonin (salmon), β-CGRP peptide Liang YL, Khoshouei M, Radjainia M, Zhang Y, Glukhova A, Tarrasch J, Thal DM, Furness SGB, Christopoulos G, Coudrat T, Danev R, Baumeister W, Miller LJ, Christopoulos A, Kobilka BK, Wootten D, Skiniotis G, Sexton PM 10.1038/NATURE22327 2017-05-03
Gs αs Human - 59 β1 Rat γ2 Bovine Cryo-EM 5VAI - 4.1 G1SGD4 GLP-1 Glucagon B1 (Secretin) Rabbit - - - CHEMBL410972 chembl_ligand pubchem pubchem
protein Agonist - - Zhang Y, Sun B, Feng D, Hu H, Chu M, Qu Q, Tarrasch JT, Li S, Sun Kobilka T, Kobilka BK, Skiniotis G 10.1038/NATURE22394 2017-05-24
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 - 56 β1 Human γ2 Human Cryo-EM 6XOX - 3.1 GLP1R GLP-1 Glucagon B1 (Secretin) Human - scFv16
Nanobody-35
- orforglipron pubchem gtoplig chembl_ligand
small-molecule Agonist glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) peptide Kawai T, Sun B, Yoshino H, Feng D, Suzuki Y, Fukazawa M, Nagao S, Wainscott DB, Showalter AD, Droz BA, Kobilka TS, Coghlan MP, Willard FS, Kawabe Y, Kobilka BK, Sloop KW 10.1073/PNAS.2014879117 2020-11-18
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7JVP - 2.9 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - 39YLC3L0ZU pubchem
small-molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine, (-)-noradrenaline, L-NOREPINEPHRINE small-molecule - - 2021-02-24
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7KH0 - 2.8 V2R V2 Vasopressin and oxytocin A (Rhodopsin) Human - scFv16
Nanobody-35
- vasopressin pubchem gtoplig chembl_ligand drugbank drug_central
peptide Agonist vasopressin, oxytocin 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
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7F1Q - 2.9 CCR5 CCR5 Chemokine A (Rhodopsin) Human - - - CCL3 gtoplig
peptide Agonist CCL5, CCL13, CCL3, CCL14, CCL8, CCL2, CCL16, CCL7, CCL11, CCL4 peptide - - 2021-07-14
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
Gs αs Human Gs-Gi1 chimera 57 β1 Human γ2 Human Cryo-EM 7P02 - 2.9 NK1R NK1 Tachykinin A (Rhodopsin) Human - scFv16 - substance P pubchem gtoplig chembl_ligand gtoplig gtoplig
peptide Agonist substance P, neurokinin B, neuropeptide K, hemokinin 1, neurokinin A, neuropeptide-γ peptide Thom C, Ehrenmann J, Vacca S, Waltenspuhl Y, Schoppe J, Medalia O, Pluckthun A 10.1126/SCIADV.ABK2872 2021-12-15
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7EVY - 3.0 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - siponimod pubchem gtoplig chembl_ligand drug_central drugbank
small-molecule Agonist sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 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 Mini-Gs 58 β1 Rat γ2 Bovine Cryo-EM 7VBI - 3.0 GLP1R GLP-1 Glucagon B1 (Secretin) Human - - - tirzepatide pubchem gtoplig
peptide Agonist glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) 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 αi1 Human - 63 β1 Bovine γ2 Bovine Cryo-EM 7S0F - 3.0 ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey - - - LEVISOPRENALINE chembl_ligand chembl_ligand pubchem
small-molecule Agonist - - Alegre KO, Paknejad N, Su M, Lou JS, Huang J, Jordan KD, Eng ET, Meyerson JR, Hite RK, Huang XY 10.1038/S41594-021-00679-2 2021-11-17
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7F1Z - 3.5 DRD1 D1 Dopamine A (Rhodopsin) Human - - - dopamine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine, (-)-noradrenaline, L-NOREPINEPHRINE small-molecule Teng X, Chen S, Wang Q, Chen Z, Wang X, Huang N, Zheng S 10.1126/SCIADV.ABO4158 2022-06-15
Gq/11 αq Human Gi2-mini-Gq chimera 60 β1 Human γ2 Human Cryo-EM 7RAN - 3.5 5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - 3-[(3R)-3-methyl-1,2,3,6-tetrahydropyridin-1-ium-5-yl]-1H-pyrrolo[2,3-b]pyridine pubchem
small-molecule Agonist tryptamine, 5-hydroxytryptamine small-molecule Kaplan AL, Confair DN, Kim K, Barros-Alvarez X, Rodriguiz RM, Yang Y, Kweon OS, Che T, McCorvy JD, Kamber DN, Phelan JP, Martins LC, Pogorelov VM, DiBerto JF, Slocum ST, Huang XP, Kumar JM, Robertson MJ, Panova O, Seven AB, Wetsel AQ, Wetsel WC, Irwin JJ, Skiniotis G, Shoichet BK, Roth BL, Ellman JA 10.1038/S41586-022-05258-Z 2022-07-06
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7XBX - 3.4 CX3C1 CX3CR1 Chemokine A (Rhodopsin) Human - - - CX3CL1
peptide Agonist CX3CL1 peptide - - 2022-07-13
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7VIE 7VIE_refined 2.9 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - sphingosine 1-phosphate pubchem gtoplig chembl_ligand pubchem
small-molecule Agonist sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate small-molecule Yu L, He L, Gan B, Ti R, Xiao Q, Hu H, Zhu L, Wang S, Ren R 10.1073/PNAS.2117716119 2022-09-28
Gi/o αgust Human - 63 β1 Human γ2 Human Cryo-EM 7XP6 - 3.0 T2R46 TAS2R46 Taste 2 T (Taste 2) Human - Nanobody-35 Endoglucanase H strychnine pubchem gtoplig chembl_ligand drug_central drugbank gtoplig
small-molecule Agonist - - Xu W, Wu L, Liu S, Liu X, Cao X, Zhou C, Zhang J, Fu Y, Guo Y, Wu Y, Tan Q, Wang L, Liu J, Jiang L, Fan Z, Pei Y, Yu J, Cheng J, Zhao S, Hao X, Liu ZJ, Hua T 10.1126/SCIENCE.ABO1633 2022-10-12
Gi/o αi1 Human - 64 β1 Rat γ2 Bovine Cryo-EM 8EF5 - 3.3 OPRM μ Opioid A (Rhodopsin) Human - scFv16 - fentanyl pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist dynorphin A-(1-13), dynorphin A-(1-8), [Met]enkephalin, endomorphin-2, dynorphin A, dynorphin B, endomorphin-1, β-endorphin, [Leu]enkephalin peptide Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, Rao Q, Yang J, Liu J, Zhou Q, Wang X, Liu M, Liu W, Jiang X, Yang D, Jiang H, Shen J, Melcher K, Chen H, Jiang Y, Cheng X, Wang MW, Xie X, Xu HE 10.1016/J.CELL.2022.09.041 2022-11-09
Gi/o αi1 Human - 56 β1 Human γ2 Human Cryo-EM 8ID9 8ID9_refined 3.0 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - scFv16 - EPA pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist myristic acid, α-linolenic acid, linoleic acid, oleic acid small-molecule None 10.1126/SCIENCE.ADD6220 2023-03-15
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8GUS - 3.0 CNR2 CB2 Cannabinoid A (Rhodopsin) Human - scFv16 - CHEMBL2179724 chembl_ligand pubchem
small-molecule Agonist anandamide, 2-arachidonoylglycerol small-molecule Li X, Chang H, Bouma J, de Paus LV, Mukhopadhyay P, Paloczi J, Mustafa M, van der Horst C, Kumar SS, Wu L, Yu Y, van den Berg RJBHN, Janssen APA, Lichtman A, Liu ZJ, Pacher P, van der Stelt M, Heitman LH, Hua T 10.1038/S41467-023-37112-9 2023-05-10
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7YAC 7YAC_refined 3.2 SSR2 SST2 Somatostatin A (Rhodopsin) Human - scFv16 - Paltusotine pubchem
small-molecule Agonist SRIF-28, CST-17, cortistatin-14, SRIF-14 peptide Zhao J, Fu H, Yu J, Hong W, Tian X, Qi J, Sun S, Zhao C, Wu C, Xu Z, Cheng L, Chai R, Yan W, Wei X, Shao Z 10.1038/S41467-023-36673-Z 2023-04-19
G12/13 α12 Human Mini-G12 55 β1 Human γ2 Human Cryo-EM 7YDJ - 3.0 AGRE5 ADGRE5 ADGRE B2 (Adhesion) Human - scFv16 - Apo (no ligand)
none Apo (no ligand) - - - - 2023-07-12
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8F0J - 2.0 CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - Pramlintide analogue San45
peptide Agonist α-CGRP, calcitonin, adrenomedullin 2/intermedin, adrenomedullin, amylin, calcitonin (salmon), β-CGRP peptide Cao J, Belousoff MJ, Gerrard E, Danev R, Fletcher MM, Dal Maso E, Schreuder H, Lorenz K, Evers A, Tiwari G, Besenius M, Li Z, Johnson RM, Wootten D, Sexton PM 10.1038/S41589-023-01393-4 2023-08-02
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8JD3 - 3.3 GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human - - - L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem
JNJ-40411813 pubchem gtoplig chembl_ligand drugbank
small-molecule
small-molecule
Agonist
PAM
L-glutamic acid small-molecule Wang X, Wang M, Xu T, Feng Y, Shao Q, Han S, Chu X, Xu Y, Lin S, Zhao Q, Wu B 10.1038/S41422-023-00830-2 2023-06-21
Gi/o αt1 Bovine - 59 β1 Bovine γT1 Bovine Cryo-EM 6OYA - 3.3 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - Camelid antibody VHH fragment - Retinal (all-trans) pubchem
small-molecule Agonist - - - - 2019-07-24
Gs αs Human Mini-Gs 61 β1 Human γ2 Human Cryo-EM 6LI3 - 3.3 GPR52 GPR52 A orphans A (Rhodopsin) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Lin X, Li M, Wang N, Wu Y, Luo Z, Guo S, Han GW, Li S, Yue Y, Wei X, Xie X, Chen Y, Zhao S, Wu J, Lei M, Xu F 10.1038/S41586-020-2019-0 2020-02-26
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 6XBL - 3.9 SMO SMO Frizzled F (Frizzled) Human - scFv16 - Cholesterol pubchem
SAG1.3 pubchem gtoplig chembl_ligand
small-molecule
small-molecule
Agonist
PAM
- - Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X 10.1038/S41589-020-0646-2 2020-09-30
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7CX2 - 2.8 PE2R2 EP2 Prostanoid A (Rhodopsin) Human - Nanobody-35 - PGE2 pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
small-molecule Agonist PGE1, PGF, thromboxane A2, PGI2, PGD2, PGE2 small-molecule Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y 10.1126/SCIADV.ABF1268 2021-05-05
Gs αs Human - 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-(7-36) amide, glucagon-like peptide 1-(7-37) 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
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7LLL - 3.7 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - exendin-4 pubchem gtoplig pubchem
peptide Agonist glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) peptide Deganutti G, Liang YL, Zhang X, Khoshouei M, Clydesdale L, Belousoff MJ, Venugopal H, Truong TT, Glukhova A, Keller AN, Gregory KJ, Leach K, Christopoulos A, Danev R, Reynolds CA, Zhao P, Sexton PM, Wootten D 10.1038/S41467-021-27760-0 2022-01-12
Gi/o αi1 Mouse - 62 β1 Bovine γ2 Bovine Cryo-EM 7TD0 - 2.8 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human - - - lysophosphatidic acid pubchem
small-molecule Agonist 1-O-Oleoyl-D-glycerol 3-phosphoric acid small-molecule Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY 10.1038/S41467-022-28417-2 2022-02-09
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7WVU 7WVU_refined 3.3 FPR1 FPR1 Formylpeptide A (Rhodopsin) Human - - - FME-LEU-PHE
peptide Agonist fMet-Leu-Phe, cathepsin G, annexin I, spinorphin peptide Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B 10.1038/S41467-022-29361-X 2022-04-13
Gi/o αi1 Human Mini-Gi1 58 β1 Human γ2 Human Cryo-EM 7WU5 - 3.0 AGRF1 ADGRF1 ADGRF B2 (Adhesion) Human - - - Apo (no ligand)
none Apo (no ligand) - - Qu X, Qiu N, Wang M, Zhang B, Du J, Zhong Z, Xu W, Chu X, Ma L, Yi C, Han S, Shui W, Zhao Q, Wu B 10.1038/S41586-022-04580-W 2022-04-27
Gs αs Human - 59 β1 Rat γ2 Bovine Cryo-EM 7XJI - 3.9 ADRB3 β3 Adrenoceptors A (Rhodopsin) Dog - Nanobody-35 - 3-[3-[2-[[(2~{S})-2-(3-chlorophenyl)-2-oxidanyl-ethyl]amino]ethylamino]phenyl]benzoic acid pubchem
small-molecule Agonist - - Nureki I, Kobayashi K, Tanaka T, Demura K, Inoue A, Shihoya W, Nureki O 10.1016/J.BBRC.2022.04.065 2022-05-04
Gi/o αo Human Mini-Go 60 β1 Human γ2 Human Cryo-EM 7UM7 7UM7_refined 2.8 5HT5A 5-HT5A 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - methylergonovine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist 5-hydroxytryptamine small-molecule Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL 10.1038/S41594-022-00796-6 2022-07-20
Gi/o αi1 Human - 61 β1 Rat γ2 Bovine Cryo-EM 8EFQ - 3.3 OPRM μ Opioid A (Rhodopsin) Human - - - DAMGO pubchem gtoplig chembl_ligand chembl_ligand
peptide Agonist dynorphin A-(1-13), dynorphin A-(1-8), [Met]enkephalin, endomorphin-2, dynorphin A, dynorphin B, endomorphin-1, β-endorphin, [Leu]enkephalin peptide Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, Rao Q, Yang J, Liu J, Zhou Q, Wang X, Liu M, Liu W, Jiang X, Yang D, Jiang H, Shen J, Melcher K, Chen H, Jiang Y, Cheng X, Wang MW, Xie X, Xu HE 10.1016/J.CELL.2022.09.041 2022-11-09
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7YS6 7YS6_refined 3.0 5HT6R 5-HT6 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - 5-hydroxytryptamine pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist 5-hydroxytryptamine small-molecule - - 2023-03-29
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8GY7 - 3.3 ACTHR MC2 Melanocortin A (Rhodopsin) Human BRIL - MRAP1 ACTH pubchem gtoplig chembl_ligand drugbank drug_central pubchem
peptide Agonist ACTH peptide None 10.1038/S41422-022-00751-6 2023-01-11
Gs αs Human - 45 β1 Human γ2 Human Cryo-EM 8IW4 - 3.5 TAAR9 TAAR9 A orphans A (Rhodopsin) Mouse - scFv16 - SPERMIDINE chembl_ligand pubchem
small-molecule Agonist - - Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP 10.1038/S41586-023-06106-4 2023-05-31
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7Y1F 7Y1F_refined 3.3 OPRK κ Opioid A (Rhodopsin) Human - scFv16 - dynorphin A-(1-8) pubchem gtoplig chembl_ligand pubchem pubchem
peptide Agonist dynorphin A-(1-13), β-neoendorphin, dynorphin A-(1-8), big dynorphin, [Met]enkephalin, α-neoendorphin, dynorphin A, dynorphin B, β-endorphin, [Leu]enkephalin peptide Chen Y, Chen B, Wu T, Zhou F, Xu F 10.1093/PROCEL/PWAC033 2023-05-24
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8FLU - 2.8 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - PTH
peptide Agonist PTH, PTHrP, PTHrP-(1-36), TIP39 peptide Cary BP, Gerrard EJ, Belousoff MJ, Fletcher MM, Jiang Y, Russell IC, Piper SJ, Wootten D, Sexton PM 10.1016/J.STR.2023.04.002 2023-04-26
Gs αs Human - 61 β1 Human γ2 Human Cryo-EM 8HMP - 2.8 GPR52 GPR52 A orphans A (Rhodopsin) Human - Nanobody-35 - derivative 17 [Nakahata et al., 2018] pubchem gtoplig chembl_ligand
small-molecule Agonist - - Fan Y, Lin X, Pan B, Chen B, Liu D, Wuthrich K, Xu F 10.1002/MCO2.260 2023-06-21
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 6DDE - 3.5 OPRM μ Opioid A (Rhodopsin) Mouse - Antibody - DAMGO pubchem gtoplig chembl_ligand chembl_ligand
peptide Agonist - - Koehl A, Hu H, Maeda S, Zhang Y, Qu Q, Paggi JM, Latorraca NR, Hilger D, Dawson R, Matile H, Schertler GFX, Granier S, Weis WI, Dror RO, Manglik A, Skiniotis G, Kobilka BK 10.1038/S41586-018-0219-7 2018-06-13
Gs αs Human - 48 β1 Human γ2 Human Cryo-EM 6UVA - 2.3 CALRL calcitonin-like Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP3
- adrenomedullin 2/intermedin gtoplig
peptide Agonist - - Liang YL, Belousoff MJ, Fletcher MM, Zhang X, Khoshouei M, Deganutti G, Koole C, Furness SGB, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Danev R, Wootten D, Sexton PM 10.1021/ACSPTSCI.9B00080 2020-04-01
Gs αs Human - 60 β1 Rat γ2 Bovine Cryo-EM 7EVM - 2.5 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - N-Tert-butyl-6,7-dichloroquinoxalin-2-amine pubchem
small-molecule Ago-PAM glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) peptide None 10.1038/S41467-021-24058-Z 2021-08-11
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 sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 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
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7S8M - 2.5 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human BRIL scFv16 - Cortistatin 14 pubchem
peptide Agonist PAMP-20 peptide Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL 10.1038/S41586-021-04126-6 2021-11-17
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7RKM - 3.5 US28 US28 Unclassified A (Rhodopsin) strain AD169 - scFv16 - Fractalkine pubchem
peptide Agonist - - Tsutsumi N, Maeda S, Qu Q, Vogele M, Jude KM, Suomivuori CM, Panova O, Waghray D, Kato HE, Velasco A, Dror RO, Skiniotis G, Kobilka BK, Garcia KC 10.1126/SCIADV.ABL5442 2022-01-26
Gi/o αo Human - 59 β1 Human γ2 Human Cryo-EM 7EJA - 3.6 ADA2A α2A Adrenoceptors A (Rhodopsin) Human - scFv16 - dexmedetomidine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist (-)-noradrenaline, (-)-adrenaline small-molecule Xu J, Cao S, Hubner H, Weikert D, Chen G, Lu Q, Yuan D, Gmeiner P, Liu Z, Du Y 10.1126/SCIADV.ABJ5347 2022-04-13
G12/13 α13 Human - 60 β1 Human γ2 Human Cryo-EM 7T6B 7T6B_refined 3.2 S1PR2 S1P2 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - sphingosine 1-phosphate pubchem gtoplig chembl_ligand pubchem
small-molecule Agonist sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate small-molecule Chen H, Chen K, Huang W, Staudt LM, Cyster JG, Li X 10.1126/SCIADV.ABN0067 2022-04-06
Gi/o αi1 Human - 61 β1 Bovine γ2 Bovine Cryo-EM 7SQO - 3.2 OX2R OX2 Orexin A (Rhodopsin) Human - scFv16 - methyl (2R,3S)-3-[(methanesulfonyl)amino]-2-({[(1s,4S)-4-phenylcyclohexyl]oxy}methyl)piperidine-1-carboxylate pubchem
small-molecule Agonist orexin-B, orexin-A peptide Yin J, Kang Y, McGrath AP, Chapman K, Sjodt M, Kimura E, Okabe A, Koike T, Miyanohana Y, Shimizu Y, Rallabandi R, Lian P, Bai X, Flinspach M, De Brabander JK, Rosenbaum DM 10.1038/S41467-022-30601-3 2022-05-25
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7W0O 7W0O_refined 3.8 APJ apelin Apelin A (Rhodopsin) Human BRIL scFv16 - apelin receptor early endogenous ligand pubchem
peptide Agonist apelin-13, apelin-36, Elabela/Toddler-32, apelin-17, Elabela/Toddler-11, apelin receptor early endogenous ligand, Elabela/Toddler-21, [Pyr1]apelin-13 peptide Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F 10.1038/S41594-022-00797-5 2022-07-27
Gs αs Human Mini-Gs 56 β1 Human γ2 Human Cryo-EM 7UTZ - 2.4 TSHR TSH Glycoprotein hormone A (Rhodopsin) Human - Nanobody-35 - Thyrotropin subunit beta
Glycoprotein hormones alpha chain analog TR1402
protein
protein
Agonist TSH peptide Faust B, Billesbolle CB, Suomivuori CM, Singh I, Zhang K, Hoppe N, Pinto AFM, Diedrich JK, Muftuoglu Y, Szkudlinski MW, Saghatelian A, Dror RO, Cheng Y, Manglik A 10.1038/S41586-022-05159-1 2022-08-03
Gs αs Human - 43 β1 Human γ2 Human Cryo-EM 6NIY - 3.3 CALCR CT Calcitonin B1 (Secretin) Human - - - calcitonin (salmon synthetic) pubchem
small-molecule Agonist α-CGRP, calcitonin, adrenomedullin 2/intermedin, adrenomedullin, amylin, calcitonin (salmon), β-CGRP peptide None 10.1021/ACSPTSCI.8B00056 2019-01-23
Gs αs Human - 49 β1 Human γ2 Human Cryo-EM 7C2E - 4.2 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - 2-[[4-[6-[(4-cyano-2-fluoranyl-phenyl)methoxy]pyridin-2-yl]-3,6-dihydro-2~{H}-pyridin-1-yl]methyl]-3-[[(2~{S})-oxetan-2-yl]methyl]imidazo[4,5-b]pyridine-5-carboxylic acid pubchem
small-molecule Agonist glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) 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 - 61 β1 Rat γ2 Human Cryo-EM 7MBX - 2.0 CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human - Nanobody-35 - CHEMBL216166 chembl_ligand pubchem
protein Agonist desulfated cholecystokinin-8, CCK-33, CCK-8, CCK-39, gastrin-17, CCK-58, CCK-4 peptide Mobbs JI, Belousoff MJ, Harikumar KG, Piper SJ, Xu X, Furness SGB, Venugopal H, Christopoulos A, Danev R, Wootten D, Thal DM, Miller LJ, Sexton PM 10.1371/JOURNAL.PBIO.3001295 2021-05-26
Gs αs Human - 61 β1 Rat γ2 Bovine Cryo-EM 7DUQ - 2.5 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - N-Tert-butyl-6,7-dichloroquinoxalin-2-amine pubchem
CHEMBL410972 chembl_ligand pubchem pubchem
small-molecule
protein
Ago-PAM
Agonist
glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) peptide None 10.1038/S41467-021-24058-Z 2021-07-14
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 hCG, LH peptide Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE 10.1038/S41586-021-03924-2 2021-09-29
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7EVZ - 3.1 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - cenerimod pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 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
Gi/o αi1 Mouse - 63 β1 Bovine γ2 Bovine Cryo-EM 7TD3 - 3.0 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - - - sphingosine 1-phosphate pubchem gtoplig chembl_ligand pubchem
small-molecule Agonist sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 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 Bovine - 57 β1 Rat γ2 Bovine Cryo-EM 7FIM - 3.4 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - tirzepatide pubchem gtoplig
peptide Agonist glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) peptide Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW 10.1038/S41467-022-28683-0 2022-03-02
Gs αs Human Mini-Gs 59 β1 Human γ2 Human Cryo-EM 7WUJ - 3.3 AGRG4 ADGRG4 ADGRG B2 (Adhesion) Human - scFv16
Nanobody-35
- Apo (no ligand)
none Apo (no ligand) - - Xiao P, Guo S, Wen X, He QT, Lin H, Huang SM, Gou L, Zhang C, Yang Z, Zhong YN, Yang CC, Li Y, Gong Z, Tao XN, Yang ZS, Lu Y, Li SL, He JY, Wang C, Zhang L, Kong L, Sun JP, Yu X 10.1038/S41586-022-04590-8 2022-04-27
Gs αs Human - 59 β1 Rat γ2 Bovine Cryo-EM 7XJH - 3.3 ADRB3 β3 Adrenoceptors A (Rhodopsin) Dog - Nanobody-35 - LEVISOPRENALINE chembl_ligand chembl_ligand pubchem
small-molecule Agonist - - Nagiri C, Kobayashi K, Tomita A, Kato M, Kobayashi K, Yamashita K, Nishizawa T, Inoue A, Shihoya W, Nureki O 10.1016/J.MOLCEL.2021.06.024 2022-05-04
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7X2F 7X2F_refined 3.0 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - dopamine pubchem gtoplig chembl_ligand drugbank drug_central
mevidalen pubchem gtoplig chembl_ligand
small-molecule
small-molecule
Agonist
PAM
5-hydroxytryptamine, noradrenaline, dopamine, (-)-noradrenaline, L-NOREPINEPHRINE small-molecule Teng X, Chen S, Nie Y, Xiao P, Yu X, Shao Z, Zheng S 10.1038/S41467-022-30929-W 2022-06-15
Gq/11 αq Human - 61 β1 Human γ2 Human Cryo-EM 7XOX 7XOX_refined 3.1 GASR CCK2 Cholecystokinin A (Rhodopsin) Human - scFv16 - CCK-8 pubchem gtoplig chembl_ligand drug_central drugbank
peptide Agonist gastrin-34, desulfated cholecystokinin-8, desulfated gastrin-14, desulfated gastrin-17, gastrin-14, desulfated gastrin-34, gastrin-17, CCK-33, CCK-8, CCK-39, gastrin-71, CCK-4, CCK-58, desulfated gastrin-71 peptide Ding Y, Zhang H, Liao YY, Chen LN, Ji SY, Qin J, Mao C, Shen DD, Lin L, Wang H, Zhang Y, Li XM 10.1038/S41421-022-00420-3 2022-07-20
Gi/o αi1 Human - 63 β1 Bovine γ2 Bovine Cryo-EM 7XAV 7XAV_refined 2.9 SSR2 SST2 Somatostatin A (Rhodopsin) Human - scFv16 - lanreotide pubchem gtoplig drugbank
peptide Agonist SRIF-28, CST-17, cortistatin-14, SRIF-14 peptide Bo Q, Yang F, Li Y, Meng X, Zhang H, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C 10.1038/S41421-022-00405-2 2022-08-31
Gs αs Human - 58 β1 Rat γ2 Bovine Cryo-EM 7VVO 7VVO_refined 4.1 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - Parathyroid hormone
peptide Agonist PTH, PTHrP, PTHrP-(1-36), TIP39 peptide Kobayashi K, Kawakami K, Kusakizako T, Miyauchi H, Tomita A, Kobayashi K, Shihoya W, Yamashita K, Nishizawa T, Kato HE, Inoue A, Nureki O 10.1016/J.MOLCEL.2022.07.003 2022-08-03
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7VFX 7VFX_refined 2.8 FPR1 FPR1 Formylpeptide A (Rhodopsin) Human - scFv16 - Peptide agonist fMet-Ile-Phe-Leu pubchem
peptide Agonist fMet-Leu-Phe, cathepsin G, annexin I, spinorphin peptide Chen G, Wang X, Liao Q, Ge Y, Jiao H, Chen Q, Liu Y, Lyu W, Zhu L, van Zundert GCP, Robertson MJ, Skiniotis G, Du Y, Hu H, Ye RD 10.1038/S41467-022-32822-Y 2022-09-21
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 7X5H 7X5H_refined 3.1 5HT5A 5-HT5A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL scFv16 - 5-CT pubchem gtoplig chembl_ligand
small-molecule Agonist 5-hydroxytryptamine small-molecule Tan Y, Xu P, Huang S, Yang G, Zhou F, He X, Ma H, Xu HE, Jiang Y 10.1038/S41421-022-00412-3 2022-09-14
Gi/o αi1 Human - 64 β1 Rat γ2 Bovine Cryo-EM 8EFO - 2.8 OPRM μ Opioid A (Rhodopsin) Human - scFv16 - PZM21 pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist dynorphin A-(1-13), dynorphin A-(1-8), [Met]enkephalin, endomorphin-2, dynorphin A, dynorphin B, endomorphin-1, β-endorphin, [Leu]enkephalin peptide Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, Rao Q, Yang J, Liu J, Zhou Q, Wang X, Liu M, Liu W, Jiang X, Yang D, Jiang H, Shen J, Melcher K, Chen H, Jiang Y, Cheng X, Wang MW, Xie X, Xu HE 10.1016/J.CELL.2022.09.041 2022-11-09
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 7Y67 7Y67_refined 2.8 C5AR1 C5a1 Complement peptide A (Rhodopsin) Human - scFv16 - C089
peptide Agonist C3a, ribosomal protein S19, C5a des-Arg, C5a peptide Feng Y, Zhao C, Deng Y, Wang H, Ma L, Liu S, Tian X, Wang B, Bin Y, Chen P, Yan W, Fu P, Shao Z 10.1038/S41422-023-00779-2 2023-03-01
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8HS3 - 3.1 GPR20 GPR20 A orphans A (Rhodopsin) Human BRIL scFv16 - Apo (no ligand)
none Apo (no ligand) - - - - 2023-03-08
Gs αolf Human Golf-Gi chimera 59 β1 Human γ2 Human Cryo-EM 8IW1 - 3.4 TAAR9 TAAR9 A orphans A (Rhodopsin) Mouse - scFv16 - 2-Phenylethanaminium pubchem
small-molecule Agonist - - Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP 10.1038/S41586-023-06106-4 2023-05-31
Gi/o αo Human - 61 β1 Human γ2 Human Cryo-EM 7XJJ 7XJJ_refined 3.3 GALR1 GAL1 Galanin A (Rhodopsin) Human - scFv16 - galanin pubchem gtoplig chembl_ligand gtoplig pubchem pubchem pubchem pubchem
peptide Agonist galanin, galanin-like peptide peptide - - 2023-05-03
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8ITF - 3.5 TAAR9 TAAR9 A orphans A (Rhodopsin) Mouse - scFv16
Nanobody-35
- N,N-Dimethylcyclohexylamine pubchem
small-molecule Agonist - - Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP 10.1038/S41586-023-06106-4 2023-05-31
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 8IUK - 2.7 PF2R FP Prostanoid A (Rhodopsin) Human - scFv16
Nanobody-35
- PGF pubchem gtoplig chembl_ligand drug_central drugbank
small-molecule Agonist PGF, thromboxane A2, PGI2, PGD2, PGE2 small-molecule Wu C, Xu Y, He Q, Li D, Duan J, Li C, You C, Chen H, Fan W, Jiang Y, Eric Xu H 10.1038/S41467-023-38411-X 2023-07-12
Gi/o αi1 Human Non-canonical conformation 62 β1 Human γ2 Human Cryo-EM 6OSA - 3.0 NTR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig chembl_ligand
peptide Agonist neurotensin, neuromedin N, large neurotensin, large neuromedin N peptide - - 2019-07-10
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 (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline, L-NOREPINEPHRINE small-molecule Jin Y, Zhao Q, Zhu W, Feng Y, Xiao T, Zhang P, Jiang L, Hou Y, Guo C, Huang H, Chen Y, Tong X, Cao J, Li F, Zhu X, Qin J, Gao D, Liu XY, Zhang H, Chen L, Thomas RK, Wong KK, Zhang L, Wang Y, Hu L, Ji H 10.1093/NSR/NWAA284 2020-12-16
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7JV5 - 3.0 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - CHEMBL1160787 chembl_ligand pubchem
small-molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine, (-)-noradrenaline, L-NOREPINEPHRINE small-molecule Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP, Shen DD, Xu T, Liu YF, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE 10.1016/J.CELL.2021.01.027 2021-02-24
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7CX3 - 2.8 PE2R2 EP2 Prostanoid A (Rhodopsin) Human - Nanobody-35 - taprenepag pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist PGE1, PGF, thromboxane A2, PGI2, PGD2, PGE2 small-molecule Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y 10.1126/SCIADV.ABF1268 2021-05-05
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7JHJ - 3.2 Q3KSP2 BILF1 Unclassified A (Rhodopsin) strain GD1 - scFv16 - Apo (no ligand)
none Apo (no ligand) - - None 10.1016/J.IMMUNI.2021.06.001 2021-07-07
Gs αs Human - 58 β1 Rat γ2 Bovine Cryo-EM 7F16 - 2.8 PTH2R PTH2 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - TIP39 gtoplig
peptide Agonist PTH, PTHrP-(1-36), TIP39, PTHrP-(1-34) (human), PTHrP 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 - 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 substance P, neurokinin B, neuropeptide K, hemokinin 1, neurokinin A, neuropeptide-γ peptide Harris JA, Faust B, Gondin AB, Damgen MA, Suomivuori CM, Veldhuis NA, Cheng Y, Dror RO, Thal DM, Manglik A 10.1038/S41589-021-00890-8 2021-11-03
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7VUI 7VUI_refined 3.3 GP139 GPR139 A orphans A (Rhodopsin) Human - Nanobody-35 Xylanase JNJ-63533054 pubchem gtoplig chembl_ligand
small-molecule Agonist L-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 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
Gi/o αo Human - 61 β1 Human γ2 Human Cryo-EM 7EJ8 - 3.0 ADA2A α2A Adrenoceptors A (Rhodopsin) Human - scFv16 - brimonidine pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
small-molecule Agonist (-)-noradrenaline, (-)-adrenaline small-molecule Xu J, Cao S, Hubner H, Weikert D, Chen G, Lu Q, Yuan D, Gmeiner P, Liu Z, Du Y 10.1126/SCIADV.ABJ5347 2022-04-13
Gq/11 αq Human - 59 β1 Human γ2 Human Cryo-EM 7W57 - 3.2 NMUR2 NMU2 Neuromedin U A (Rhodopsin) Human - scFv16 - Neuromedin-S
peptide Agonist neuromedin U-25, neuromedin S-33, neuromedin U-23, neuromedin S-36 peptide You C, Zhang Y, Xu P, Huang S, Yin W, Eric Xu H, Jiang Y 10.1038/S41467-022-29683-W 2022-04-20
Gi/o αi1 Human - 62 β1 Mouse γ2 Mouse Cryo-EM 7Y12 - 3.1 MRGRD MRGPRD A orphans A (Rhodopsin) Human BRIL scFv16 - β-alanine pubchem gtoplig chembl_ligand drugbank pubchem
small-molecule Agonist β-alanine small-molecule Suzuki S, Iida M, Hiroaki Y, Tanaka K, Kawamoto A, Kato T, Oshima A 10.1038/S42003-022-03668-3 2022-07-20
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7XW5 - 3.0 TSHR TSH Glycoprotein hormone A (Rhodopsin) Human - Nanobody-35 - Glycoprotein hormones alpha chain
Thyrotropin subunit beta
N-[4-[[5-[(2S)-3-benzyl-5-hydroxy-4-oxo-1,2-dihydroquinazolin-2-yl]-2-methoxyphenyl]methoxy]phenyl]acetamide pubchem
protein
protein
small-molecule
Agonist TSH peptide Duan J, Xu P, Luan X, Ji Y, He X, Song N, Yuan Q, Jin Y, Cheng X, Jiang H, Zheng J, Zhang S, Jiang Y, Xu HE 10.1038/S41586-022-05173-3 2022-08-24
Gi/o αz Human - 59 β1 Human γ2 Human Cryo-EM 8DZS - 2.7 OPRK κ Opioid A (Rhodopsin) Human - scFv16 - CHEMBL277863 chembl_ligand pubchem
small-molecule Agonist dynorphin A-(1-13), β-neoendorphin, dynorphin A-(1-8), big dynorphin, [Met]enkephalin, α-neoendorphin, dynorphin A, dynorphin B, β-endorphin, [Leu]enkephalin peptide Han J, Zhang J, Nazarova AL, Bernhard SM, Krumm BE, Zhao L, Lam JH, Rangari VA, Majumdar S, Nichols DE, Katritch V, Yuan P, Fay JF, Che T 10.1038/S41586-023-06030-7 2023-05-03
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 8IRT - 2.7 DRD3 D3 Dopamine A (Rhodopsin) Human BRIL scFv16 - rotigotine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist dopamine small-molecule Xu P, Huang S, Krumm BE, Zhuang Y, Mao C, Zhang Y, Wang Y, Huang XP, Liu YF, He X, Li H, Yin W, Jiang Y, Zhang Y, Roth BL, Xu HE 10.1038/S41422-023-00808-0 2023-06-07
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8J18 - 2.9 GPR84 GPR84 A orphans A (Rhodopsin) Human - scFv16 - (3R)-3-HYDROXYDODECANOIC ACID pubchem
small-molecule Agonist - - Liu H, Zhang Q, He X, Jiang M, Wang S, Yan X, Cheng X, Liu Y, Nan FJ, Xu HE, Xie X, Yin W 10.1038/S41467-023-38985-6 2023-06-21
Gq/11 αq Human GRK2 bound 88 - - - - Cryo-EM 8JPB - 3.1 NTR1 NTS1 Neurotensin A (Rhodopsin) Human - GRK2 GRK2 JMV431 gtoplig chembl_ligand pubchem
CHEMBL4576388 chembl_ligand pubchem
peptide
small-molecule
Agonist
PAM
neurotensin, neuromedin N, large neurotensin, large neuromedin N peptide Duan J, Liu H, Zhao F, Yuan Q, Ji Y, Cai X, He X, Li X, Li J, Wu K, Gao T, Zhu S, Lin S, Wang MW, Cheng X, Yin W, Jiang Y, Yang D, Xu HE 10.1038/S41586-023-06395-9 2023-08-09
Gs αs Human - 49 β1 Human γ2 Human Cryo-EM 6ORV 6ORV_refined 3.0 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - CHEMBL3950796 chembl_ligand pubchem
small-molecule Agonist glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) peptide Zhao P, Liang YL, Belousoff MJ, Deganutti G, Fletcher MM, Willard FS, Bell MG, Christe ME, Sloop KW, Inoue A, Truong TT, Clydesdale L, Furness SGB, Christopoulos A, Wang MW, Miller LJ, Reynolds CA, Danev R, Sexton PM, Wootten D 10.1038/s41586-019-1902-z 2020-01-08
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7CFN 7CFN_refined 3.0 GPBAR GPBA Bile acid A (Rhodopsin) Human - Nanobody-35 - INT-777 pubchem
INT-777 pubchem
small-molecule
small-molecule
Agonist
PAM
cholic acid, chenodeoxycholic acid, lithocholic acid, deoxycholic 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 αo Human - 61 β1 Human γ2 Human Cryo-EM 7D76 - 3.1 AGRG3 ADGRG3 ADGRG B2 (Adhesion) Human - - - Beclomethasone pubchem
small-molecule Agonist - - Ping YQ, Mao C, Xiao P, Zhao RJ, Jiang Y, Yang Z, An WT, Shen DD, Yang F, Zhang H, Qu C, Shen Q, Tian C, Li ZJ, Li S, Wang GY, Tao X, Wen X, Zhong YN, Yang J, Yi F, Yu X, Xu HE, Zhang Y, Sun JP 10.1038/S41586-020-03083-W 2021-02-03
Gi/o 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 CCL5, CCL13, CCL3, CCL14, CCL8, CCL2, CCL16, CCL7, CCL11, CCL4 peptide None 10.1126/SCIADV.ABG8685 2021-06-30
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
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7F4I 7F4I_refined 3.1 MSHR MC1 Melanocortin A (Rhodopsin) Human - Nanobody-35 - bremelanotide pubchem gtoplig chembl_ligand drugbank drug_central
peptide Agonist ACTH, α-MSH, γ-MSH, β-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 Mouse - 63 β1 Bovine γ2 Bovine Cryo-EM 7TD4 - 2.6 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - - - siponimod pubchem gtoplig chembl_ligand drug_central drugbank
small-molecule Agonist sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 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 - 56 β1 Human γ2 Human Cryo-EM 7RG9 7RG9_refined 3.2 GLP1R GLP-1 Glucagon B1 (Secretin) Human - scFv16
Nanobody-35
- Apo (no ligand)
none Apo (no ligand) glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) 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 - 62 β1 Human γ2 Human Cryo-EM 7V68 - 3.4 ACM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - iperoxo pubchem gtoplig chembl_ligand
LY2119620 pubchem gtoplig chembl_ligand
small-molecule
small-molecule
Agonist
PAM
acetylcholine small-molecule Wang J, Wu M, Chen Z, Wu L, Wang T, Cao D, Wang H, Liu S, Xu Y, Li F, Liu J, Chen N, Zhao S, Cheng J, Wang S, Hua T 10.1038/S41467-022-30595-Y 2022-05-11
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 7WKD - 3.0 TRFR TRH1 Thyrotropin-releasing hormone A (Rhodopsin) Human - scFv16 - TRH pubchem
peptide Agonist TRH peptide Xu Y, Cai H, You C, He X, Yuan Q, Jiang H, Cheng X, Jiang Y, Xu HE 10.1038/S41422-022-00641-X 2022-06-15
Gs αs Human Mini-Gs 56 β1 Human γ2 Human Cryo-EM 7T9N - 2.9 TSHR TSH Glycoprotein hormone A (Rhodopsin) Human - M22 Fab light chain
M22 Fab heavy chain
Nanobody-35
- M22 antibody light chain
M22 antibody heavy chain
protein
protein
Agonist TSH peptide Faust B, Billesbolle CB, Suomivuori CM, Singh I, Zhang K, Hoppe N, Pinto AFM, Diedrich JK, Muftuoglu Y, Szkudlinski MW, Saghatelian A, Dror RO, Cheng Y, Manglik A 10.1038/S41586-022-05159-1 2022-08-03
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 4X1H 4X1H_refined 2.3 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - B-Nonylglucoside pubchem
small-molecule unknown - - Blankenship E, Vahedi-Faridi A, Lodowski DT 10.1016/J.STR.2015.09.015 2015-11-04
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 6LML 6LML_refined 3.9 GLR glucagon Glucagon B1 (Secretin) Human - scFv16 - glucagon pubchem gtoplig chembl_ligand drugbank drug_central gtoplig pubchem pubchem pubchem pubchem
peptide Agonist glucagon peptide Qiao A, Han S, Li X, Li Z, Zhao P, Dai A, Chang R, Tai L, Tan Q, Chu X, Ma L, Thorsen TS, Reedtz-Runge S, Yang D, Wang MW, Sexton PM, Wootten D, Sun F, Zhao Q, Wu B 10.1126/SCIENCE.AAZ5346 2020-04-01
Gs αs Bovine - 51 β1 Bovine γ2 Bovine Cryo-EM 7JJO - 2.6 ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey - Nanobody-35 - LEVISOPRENALINE chembl_ligand chembl_ligand pubchem
small-molecule Agonist - - Su M, Zhu L, Zhang Y, Paknejad N, Dey R, Huang J, Lee MY, Williams D, Jordan KD, Eng ET, Ernst OP, Meyerson JR, Hite RK, Walz T, Liu W, Huang XY 10.1016/J.MOLCEL.2020.08.001 2020-09-02
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7E2Y - 3.0 5HT1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human - - - 5-hydroxytryptamine pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist 5-hydroxytryptamine small-molecule Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen DD, Yen HY, Robinson CV, Harpsoe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE 10.1038/S41586-021-03376-8 2021-04-14
Gi/o αi2 Human - 61 β1 Human γ2 Human Cryo-EM 7F8V - 3.3 GASR CCK2 Cholecystokinin A (Rhodopsin) Human - - - desulfated gastrin-17 pubchem gtoplig chembl_ligand pubchem
peptide Agonist gastrin-34, desulfated cholecystokinin-8, desulfated gastrin-14, desulfated gastrin-17, gastrin-14, desulfated gastrin-34, gastrin-17, CCK-33, CCK-8, CCK-39, gastrin-71, CCK-4, CCK-58, 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
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7VV3 - 3.0 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human - scFv16 - Cortistatin 14 pubchem
peptide Agonist PAMP-20 peptide Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP 10.1038/S41586-021-04077-Y 2021-12-01
Gq/11 α11 Human - 97 β1 Human γ2 Human Cryo-EM 7RKF - 4.0 US28 US28 Unclassified A (Rhodopsin) strain AD169 - scFv16 - Fractalkine pubchem
peptide Agonist - - Tsutsumi N, Maeda S, Qu Q, Vogele M, Jude KM, Suomivuori CM, Panova O, Waghray D, Kato HE, Velasco A, Dror RO, Skiniotis G, Kobilka BK, Garcia KC 10.1126/SCIADV.ABL5442 2022-01-26
Gs αs Human - 53 β1 Rat γ2 Bovine Cryo-EM 7V35 7V35_refined 3.4 GLR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - Peptide-20
peptide Agonist glucagon peptide Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW 10.1038/S41467-022-28683-0 2022-03-02
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 7W55 - 2.8 NMUR2 NMU2 Neuromedin U A (Rhodopsin) Human - scFv16 - Neuromedin U-25 (human) pubchem
peptide Agonist neuromedin U-25, neuromedin S-33, neuromedin U-23, neuromedin S-36 peptide You C, Zhang Y, Xu P, Huang S, Yin W, Eric Xu H, Jiang Y 10.1038/S41467-022-29683-W 2022-04-20
Gq/11 αq Human - 61 β1 Human γ2 Human Cryo-EM 7XOW 7XOW_refined 3.1 GASR CCK2 Cholecystokinin A (Rhodopsin) Human - scFv16 - desulfated gastrin-17 pubchem gtoplig chembl_ligand pubchem
peptide Agonist gastrin-34, desulfated cholecystokinin-8, desulfated gastrin-14, desulfated gastrin-17, gastrin-14, desulfated gastrin-34, gastrin-17, CCK-33, CCK-8, CCK-39, gastrin-71, CCK-4, CCK-58, desulfated gastrin-71 peptide Ding Y, Zhang H, Liao YY, Chen LN, Ji SY, Qin J, Mao C, Shen DD, Lin L, Wang H, Zhang Y, Li XM 10.1038/S41421-022-00420-3 2022-07-20
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 7XMR 7XMR_refined 3.1 SSR2 SST2 Somatostatin A (Rhodopsin) Human - - - SOMATOSTATIN chembl_ligand pubchem
protein Agonist SRIF-28, CST-17, cortistatin-14, SRIF-14 peptide - - 2022-08-03
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7YP7 - 3.1 AGRG2 ADGRG2 ADGRG B2 (Adhesion) Mouse - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - - - 2022-08-24
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7T2G - 2.5 OPRM μ Opioid A (Rhodopsin) Mouse BRIL - - CHEMBL58362 chembl_ligand pubchem
small-molecule Agonist - - Qu Q, Huang W, Aydin D, Paggi JM, Seven AB, Wang H, Chakraborty S, Che T, DiBerto JF, Robertson MJ, Inoue A, Suomivuori CM, Roth BL, Majumdar S, Dror RO, Kobilka BK, Skiniotis G 10.1038/S41589-022-01208-Y 2022-12-07
Gs αs Human Mini-Gs 59 β1 Human γ2 Human Cryo-EM 7WY8 - 2.8 AGRL3 ADGRL3 ADGRL B2 (Adhesion) Mouse - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Qian Y, Ma Z, Liu C, Li X, Zhu X, Wang N, Xu Z, Xia R, Liang J, Duan Y, Yin H, Xiong Y, Zhang A, Guo C, Chen Z, Huang Z, He Y 10.1016/J.MOLCEL.2022.10.009 2022-10-26
Gi/o αi1 Human - 63 β1 Rat γ2 Bovine Cryo-EM 7YU6 7YU6_refined 3.5 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human - scFv16 - [(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate pubchem
small-molecule Agonist 1-O-Oleoyl-D-glycerol 3-phosphoric acid small-molecule Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O 10.1038/S41467-022-33121-2 2022-10-05
Gi/o αi1 Human - 62 β1 Rat γ2 Bovine Cryo-EM 8F7X 8F7X_refined 3.3 OPRX NOP Opioid A (Rhodopsin) Human - scFv16 - nociceptin/orphanin FQ pubchem gtoplig chembl_ligand gtoplig pubchem pubchem
peptide Agonist nociceptin/orphanin FQ peptide Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y, Roth BL, Xu HE 10.1016/J.CELL.2022.12.026 2022-12-14
Gi/o αo Human - 60 β1 Human γ2 Human Cryo-EM 8FN1 - 2.9 NTR1 NTS1 Neurotensin A (Rhodopsin) Rat - scFv16 - neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
peptide Agonist neuromedin N, neurotensin peptide - - 2023-03-29
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8ID4 - 3.1 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - scFv16 - linoleic acid pubchem gtoplig chembl_ligand drug_central drugbank
small-molecule Agonist myristic acid, α-linolenic acid, linoleic acid, oleic acid small-molecule None 10.1126/SCIENCE.ADD6220 2023-03-15
Gq/11 αq Human Gs-mini-Gq chimera 52 β1 Human γ2 Human Cryo-EM 8G2Y - 3.4 AGRF1 ADGRF1 ADGRF B2 (Adhesion) Human - Nanobody-35 - [1-Myristoyl-glycerol-3-YL]phosphonylcholine pubchem
small-molecule Agonist - - Jones DTD, Dates AN, Rawson SD, Burruss MM, Lipper CH, Blacklow SC 10.1038/S41467-023-38083-7 2023-05-10
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7TRQ - 2.5 ACM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - iperoxo pubchem gtoplig chembl_ligand
VU0467154 pubchem gtoplig chembl_ligand
small-molecule
small-molecule
Agonist
PAM
acetylcholine small-molecule - - 2023-05-17
Gq/11 α11 Human - 63 β1 Human γ2 Human Cryo-EM 7XXH 7XXH_refined 2.9 P2RY1 P2Y1 P2Y A (Rhodopsin) Human - scFv16 - 2MeSADP pubchem gtoplig chembl_ligand gtoplig
small-molecule Agonist ADP, ATP small-molecule - - 2023-06-07
Gq/11 αq Human - 56 β1 Human γ2 Human Cryo-EM 8H0P - 3.2 NMBR BB1 Bombesin A (Rhodopsin) Human - scFv16 - NMB30
peptide Agonist gastrin-releasing peptide, GRP-(18-27), gastrin releasing peptide(14-27) (human), neuromedin B peptide Li C, Xu Y, Liu H, Cai H, Jiang Y, Xu HE, Yin W 10.1038/S41422-022-00743-6 2023-08-09
Gs αs Human - 57 β1 Human γ2 Human Cryo-EM 6VCB - 3.3 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - glucagon-like peptide 1-(7-37) pubchem gtoplig chembl_ligand gtoplig pubchem pubchem
CHEMBL5197819 chembl_ligand pubchem
peptide
small-molecule
Agonist
PAM
glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) peptide Bueno AB, Sun B, Willard FS, Feng D, Ho JD, Wainscott DB, Showalter AD, Vieth M, Chen Q, Stutsman C, Chau B, Ficorilli J, Agejas FJ, Cumming GR, Jimenez A, Rojo I, Kobilka TS, Kobilka BK, Sloop KW 10.1038/S41589-020-0589-7 2020-07-22
Gi/o αi1 Human - 63 β1 Human γT1 Human Cryo-EM 7L0P - 4.1 NTR1 NTS1 Neurotensin A (Rhodopsin) Rat - - - neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
peptide Agonist neuromedin N, neurotensin peptide Zhang M, Gui M, Wang ZF, Gorgulla C, Yu JJ, Wu H, Sun ZJ, Klenk C, Merklinger L, Morstein L, Hagn F, Pluckthun A, Brown A, Nasr ML, Wagner G 10.1038/S41594-020-00554-6 2021-01-06
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7CKX - 3.5 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - A77636 pubchem gtoplig chembl_ligand
small-molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine, (-)-noradrenaline, L-NOREPINEPHRINE 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 - 54 β1 Human γ2 Human Cryo-EM 7BB6 - 4.2 V2R V2 Vasopressin and oxytocin A (Rhodopsin) Human - Nanobody-35 - vasopressin pubchem gtoplig chembl_ligand drugbank drug_central
peptide Agonist vasopressin, oxytocin 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 - 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-(7-36) amide, glucagon-like peptide 1-(7-37) peptide Deganutti G, Liang YL, Zhang X, Khoshouei M, Clydesdale L, Belousoff MJ, Venugopal H, Truong TT, Glukhova A, Keller AN, Gregory KJ, Leach K, Christopoulos A, Danev R, Reynolds CA, Zhao P, Sexton PM, Wootten D 10.1038/S41467-021-27760-0 2022-01-12
Gi/o αi1 Mouse - 62 β1 Bovine γ2 Bovine Cryo-EM 7TD1 - 3.1 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human - - - lysophosphatidic acid pubchem
small-molecule Agonist 1-O-Oleoyl-D-glycerol 3-phosphoric acid small-molecule Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY 10.1038/S41467-022-28417-2 2022-02-09
Gi/o αi2 Human - 63 β1 Human γ2 Human Cryo-EM 7WVV 7WVV_refined 2.9 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human BRIL - - synthetic peptide
peptide Agonist aspirin-triggered resolvin D1, LL-37, resolvin D1, 15-deoxy-LXA4, LXA4, LTD4, LTC4, aspirin triggered lipoxin A4, fMet-Leu-Phe, serum amyloid A, PrP106-126, annexin I, humanin 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 7EJX - 2.4 GPR88 GPR88 A orphans A (Rhodopsin) Human - scFv16 - compound 2 [PMID: 24793972] pubchem gtoplig chembl_ligand
small-molecule Allosteric agonist - - Chen G, Xu J, Inoue A, Schmidt MF, Bai C, Lu Q, Gmeiner P, Liu Z, Du Y 10.1038/S41467-022-30081-5 2022-04-13
Gq/11 αq Human - 58 β1 Human γ2 Human Cryo-EM 7SR8 - 3.3 OX2R OX2 Orexin A (Rhodopsin) Human - scFv16 - methyl (2R,3S)-3-[(methanesulfonyl)amino]-2-({[(1s,4S)-4-phenylcyclohexyl]oxy}methyl)piperidine-1-carboxylate pubchem
small-molecule Agonist orexin-B, orexin-A peptide Yin J, Kang Y, McGrath AP, Chapman K, Sjodt M, Kimura E, Okabe A, Koike T, Miyanohana Y, Shimizu Y, Rallabandi R, Lian P, Bai X, Flinspach M, De Brabander JK, Rosenbaum DM 10.1038/S41467-022-30601-3 2022-06-08
Gq/11 αq Human Mini-Gq 57 β1 Human γ2 Human Cryo-EM 8E9W - 2.7 ACM3 M3 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - CHEMBL73538 chembl_ligand pubchem
small-molecule Agonist acetylcholine small-molecule - - 2022-11-30
Gs αs Bovine - 60 β1 Rat γ2 Bovine Cryo-EM 8HAO - 3.8 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - teriparatide pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem pubchem pubchem pubchem pubchem
peptide Agonist PTH, PTHrP, PTHrP-(1-36), TIP39 peptide Zhao LH, Yuan QN, Dai AT, He XH, Chen CW, Zhang C, Xu YW, Zhou Y, Wang MW, Yang DH, Xu HE 10.1038/S41401-022-01032-Z 2022-12-21
Gi/o αo Human - 62 β1 Human γ2 Human Cryo-EM 7T8X 7T8X_refined 3.2 ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human - Antibody fragment - acetylcholine pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
small-molecule Agonist acetylcholine small-molecule - - 2023-01-25
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7XV3 7XV3_refined 2.8 GP174 GPR174 A orphans A (Rhodopsin) Human - - - (2~{S})-2-$l^{4}-azanyl-3-[[(2~{R})-3-octadecanoyloxy-2-oxidanyl-propoxy]-oxidanyl-oxidanylidene-$l^{6}-phosphanyl]oxy-propanoic acid pubchem
small-molecule Agonist lysophosphatidylserine small-molecule Liang J, Inoue A, Ikuta T, Xia R, Wang N, Kawakami K, Xu Z, Qian Y, Zhu X, Zhang A, Guo C, Huang Z, He Y 10.1038/S41467-023-36575-0 2023-02-15
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 8IBU 8IBU_refined 3.5 MTLR motilin Motilin A (Rhodopsin) Human BRIL scFv16 - erythromycin pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist motilin peptide You C, Zhang Y, Xu Y, Xu P, Li Z, Li H, Huang S, Chen Z, Li J, Xu HE, Jiang Y 10.1126/SCIADV.ADE9020 2023-04-12
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7YKD - 2.8 CML1 chemerin Chemerin receptor A (Rhodopsin) Human - scFv16 - chemerin C-terminal peptide pubchem gtoplig chembl_ligand
peptide Agonist EPA, resolvin E1, 18R-HEPE, chemerin C-terminal peptide, chemerin peptide Wang J, Chen G, Liao Q, Lyu W, Liu A, Zhu L, Du Y, Ye RD 10.1073/PNAS.2214324120 2023-04-19
Gq/11 αq Human - 99 β1 Human γ2 Human Cryo-EM 8IYS - 3.0 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - scFv16 - TUG-891 pubchem gtoplig chembl_ligand
small-molecule Agonist myristic acid, α-linolenic acid, linoleic acid, oleic acid small-molecule Yin H, Inoue A, Ma Z, Zhu X, Xia R, Xu Z, Wang N, Duan Y, Zhang A, Guo C, He Y 10.1038/S41422-023-00835-X 2023-06-21
Gi/o αt1 Bovine - 64 β1 Bovine γT1 Bovine Cryo-EM 6OY9 - 3.9 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - Retinal (all-trans) pubchem
small-molecule Agonist - - None 10.1016/J.MOLCEL.2019.06.007 2019-07-24
Gs αs Human - 55 β1 Bovine γ2 Bovine Cryo-EM 7DHI - 3.3 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - Nanobody-35 - levosalbutamol pubchem gtoplig chembl_ligand drug_central drugbank
small-molecule Agonist (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline, L-NOREPINEPHRINE small-molecule - - 2020-12-16
Gs αs Human Engineered G alpha 60 β1 Human γ2 Human Cryo-EM 7JVQ 7JVQ_refined 3.0 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - apomorphine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine, (-)-noradrenaline, L-NOREPINEPHRINE small-molecule Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP, Shen DD, Xu T, Liu YF, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE 10.1016/J.CELL.2021.01.027 2021-02-24
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7CX4 7CX4_refined 2.9 PE2R2 EP2 Prostanoid A (Rhodopsin) Human - Nanobody-35 - evatanepag pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist PGE1, PGF, thromboxane A2, PGI2, PGD2, PGE2 small-molecule Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y 10.1126/SCIADV.ABF1268 2021-05-05
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 - 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 sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 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
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 neuropeptide Y, peptide YY, pancreatic polypeptide peptide Park C, Kim J, Ko SB, Choi YK, Jeong H, Woo H, Kang H, Bang I, Kim SA, Yoon TY, Seok C, Im W, Choi HJ 10.1038/S41467-022-28510-6 2022-02-23
Gs αs Bovine - 60 β1 Rat γ2 Bovine Cryo-EM 7FIY - 3.4 GIPR GIP Glucagon B1 (Secretin) Human - Nanobody-35 - tirzepatide pubchem gtoplig
peptide Agonist gastric inhibitory polypeptide peptide Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW 10.1038/S41467-022-28683-0 2022-03-02
G12/13 α13 Human Gi2-mini-G13 chimera 56 β1 Human γ2 Human Cryo-EM 7SF8 - 2.7 AGRG1 ADGRG1 ADGRG B2 (Adhesion) Human - - - Apo (no ligand)
none Apo (no ligand) - - - - 2022-04-27
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7V6A - 3.6 ACM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - methyl 4-[4-(3-methyl-2-oxidanylidene-benzimidazol-1-yl)piperidin-1-yl]piperidine-1-carboxylate pubchem
small-molecule Allosteric agonist acetylcholine small-molecule Wang J, Wu M, Chen Z, Wu L, Wang T, Cao D, Wang H, Liu S, Xu Y, Li F, Liu J, Chen N, Zhao S, Cheng J, Wang S, Hua T 10.1038/S41467-022-30595-Y 2022-05-11
Gq/11 αq Human - 58 β1 Human γ2 Human Cryo-EM 7XJL 7XJL_refined 3.5 GALR2 GAL2 Galanin A (Rhodopsin) Human - scFv16 - Spexin pubchem
small-molecule Agonist galanin, spexin-1, galanin-like peptide peptide Jiang W, Zheng S 10.1073/PNAS.2121465119 2022-06-29
Gi/o αi1 Human - 60 β1 Human γ2 Human Cryo-EM 7WJ5 7WJ5_refined 3.7 SSR2 SST2 Somatostatin A (Rhodopsin) Human BRIL scFv16 - SOMATOSTATIN chembl_ligand pubchem
protein Agonist SRIF-28, CST-17, cortistatin-14, SRIF-14 peptide Heo Y, Yoon E, Jeon YE, Yun JH, Ishimoto N, Woo H, Park SY, Song JJ, Lee W 10.7554/ELIFE.76823 2022-07-13
Gq/11 α11 Human - 62 β1 Rat γ2 Mouse Cryo-EM 7TRY - 3.7 CRFR2 CRF2 Corticotropin-releasing factor B1 (Secretin) Human - - - Urocortin pubchem
peptide Agonist urocortin 2, urocortin 3, urocortin 1, corticotrophin-releasing hormone peptide Zhao LH, Lin J, Ji SY, Zhou XE, Mao C, Shen DD, He X, Xiao P, Sun J, Melcher K, Zhang Y, Yu X, Xu HE 10.1038/S41467-022-33851-3 2022-11-09
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7WZ4 - 3.0 GPR88 GPR88 A orphans A (Rhodopsin) Human - scFv16 - Apo (no ligand)
none Apo (no ligand) - - Chen G, Xu J, Inoue A, Schmidt MF, Bai C, Lu Q, Gmeiner P, Liu Z, Du Y 10.1038/S41467-022-30081-5 2022-10-26
Gq/11 αq Human Gs-mini-Gq chimera 57 β1 Human γ2 Human Cryo-EM 8DWG - 2.7 MRGX1 MRGPRX1 A orphans A (Rhodopsin) Human - scFv16 - Proenkephalin-A
CHEMBL5177388 chembl_ligand pubchem
peptide
small-molecule
Agonist
PAM
bovine adrenal medulla peptide 8-22 peptide - - 2022-11-02
Gi/o αi2 Human - 61 β1 Human γ2 Bovine Cryo-EM 7YK7 7YK7_refined 2.8 RL3R2 RXFP4 Relaxin family peptide A (Rhodopsin) Human - scFv16 - DC591053 pubchem gtoplig
small-molecule Agonist relaxin-3, relaxin-3 (B chain), INSL5 peptide Chen Y, Zhou Q, Wang J, Xu Y, Wang Y, Yan J, Wang Y, Zhu Q, Zhao F, Li C, Chen CW, Cai X, Bathgate RAD, Shen C, Eric Xu H, Yang D, Liu H, Wang MW 10.1038/S41467-023-36182-Z 2023-03-01
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8ID6 - 2.8 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - scFv16 - oleic acid pubchem gtoplig chembl_ligand drug_central
small-molecule Agonist myristic acid, α-linolenic acid, linoleic acid, oleic acid small-molecule None 10.1126/SCIENCE.ADD6220 2023-03-15
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 8IBV 8IBV_refined 3.2 MTLR motilin Motilin A (Rhodopsin) Human BRIL scFv16 - motilin pubchem gtoplig chembl_ligand gtoplig pubchem pubchem
peptide Agonist motilin peptide You C, Zhang Y, Xu Y, Xu P, Li Z, Li H, Huang S, Chen Z, Li J, Xu HE, Jiang Y 10.1126/SCIADV.ADE9020 2023-04-12
Gq/11 αq Human Mini-Gq 60 β1 Human γ2 Human Cryo-EM 7YDM - 2.9 AGRE5 ADGRE5 ADGRE B2 (Adhesion) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - - - 2023-07-12