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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
Gi/o αt1 Bovine Only H5 3 - - - - X-ray 3DQB - 3.2 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - Apo (no ligand)
none Apo (no ligand) - - None 10.1038/NATURE07330 2008-09-23
Gi/o αt1 Bovine Only H5 3 - - - - X-ray 3PQR 3PQR_refined 2.9 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - Retinal (all-trans) pubchem
small-molecule Agonist - - - - 2011-03-09
Gi/o αt1 Bovine Only H5 3 - - - - X-ray 2X72 2X72_refined 3.0 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - Retinal (all-trans) pubchem
small-molecule Agonist - - Standfuss J, Edwards PC, D'Antona A, Fransen M, Xie G, Oprian DD, Schertler GF 10.1038/NATURE09795 2011-03-16
Gs αs Bovine - 89 β1 Rat γ2 Bovine X-ray 3SN6 - 3.2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human T4-Lysozyme Antibody - CHEMBL1615159 chembl_ligand pubchem
small-molecule Agonist L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline small-molecule Rasmussen SG, DeVree BT, Zou Y, Kruse AC, Chung KY, Kobilka TS, Thian FS, Chae PS, Pardon E, Calinski D, Mathiesen JM, Shah ST, Lyons JA, Caffrey M, Gellman SH, Steyaert J, Skiniotis G, Weis WI, Sunahara RK, Kobilka BK 10.1038/NATURE10361 2011-07-20
Gi/o αt1 Bovine Only H5 3 - - - - X-ray 4A4M 4A4M_refined 3.3 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - Retinal (all-trans) pubchem
small-molecule Agonist - - Deupi X, Edwards P, Singhal A, Nickle B, Oprian D, Schertler G, Standfuss J 10.1073/PNAS.1114089108 2012-01-25
Gi/o αo Human Mini-Go 51 - - - - X-ray 6FUF - 3.1 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - Retinal (all-trans) pubchem
small-molecule Agonist - - Tsai CJ, Pamula F, Nehme R, Muhle J, Weinert T, Flock T, Nogly P, Edwards PC, Carpenter B, Gruhl T, Ma P, Deupi X, Standfuss J, Tate CG, Schertler GFX 10.1126/SCIADV.AAT7052 2018-10-03
Gs αs Human - 49 β1 Human γ2 Human Cryo-EM 6P9Y - 3.0 PACR PAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - [Ac-His1]PACAP-27 gtoplig chembl_ligand pubchem
peptide Agonist VIP, PHI, PHM, PHV, PACAP-27, PACAP-38 peptide Liang YL, Belousoff MJ, Zhao P, Koole C, Fletcher MM, Truong TT, Julita V, Christopoulos G, Xu HE, Zhang Y, Khoshouei M, Christopoulos A, Danev R, Sexton PM, Wootten D 10.1016/J.MOLCEL.2020.01.012 2020-02-05
Gi/o αt2 Bovine Only H5 3 - - - - X-ray 6PH7 - 2.9 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - Nerol pubchem
small-molecule unknown - - - - 2020-07-01
Gs αs Human - 50 β1 Bovine γ2 Bovine Cryo-EM 7BZ2 7BZ2_refined 3.8 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - Nanobody-35 - ARFORMOTEROL chembl_ligand chembl_ligand chembl_ligand chembl_ligand pubchem
small-molecule Agonist L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline small-molecule Zhang Y, Yang F, Ling S, Lv P, Zhou Y, Fang W, Sun W, Zhang L, Shi P, Tian C 10.1038/S41421-020-0176-9 2020-08-05
Gq/11 αq Human Gq-Gi2-Gs chimera 57 β1 Human γ2 Human Cryo-EM 6WHA - 3.4 5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL scFv16 - CHEMBL5184791 chembl_ligand pubchem
small-molecule Agonist tryptamine, 5-hydroxytryptamine small-molecule Kim K, Che T, Panova O, DiBerto JF, Lyu J, Krumm BE, Wacker D, Robertson MJ, Seven AB, Nichols DE, Shoichet BK, Skiniotis G, Roth BL 10.1016/J.CELL.2020.08.024 2020-09-23
Gi/o 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 60 β1 Rat γ2 Bovine Cryo-EM 7LJD - 3.2 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - dopamine pubchem gtoplig chembl_ligand drugbank drug_central
mevidalen pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Agonist
PAM 		L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine small-molecule - - 2021-03-03
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 7E9G - 3.5 GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human - scFv16 DN13 eglumegad pubchem gtoplig chembl_ligand gtoplig
JNJ-40411813 pubchem gtoplig chembl_ligand drugbank
small-molecule
small-molecule 		Agonist
PAM 		L-glutamic acid small-molecule Lin S, Han S, Cai X, Tan Q, Zhou K, Wang D, Wang X, Du J, Yi C, Chu X, Dai A, Zhou Y, Chen Y, Zhou Y, Liu H, Liu J, Yang D, Wang MW, Zhao Q, Wu B 10.1038/S41586-021-03495-2 2021-06-23
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7EO2 7EO2_refined 2.9 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - (S)-FTY720-phosphate pubchem gtoplig chembl_ligand
small-molecule Agonist 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 - 61 β1 Rat γ2 Bovine Cryo-EM 7T6T 7T6T_refined 3.2 FPR1 FPR1 Formylpeptide A (Rhodopsin) Human - - - synthetic peptide
peptide Agonist fMet-Leu-Phe, cathepsin G, annexin I, spinorphin peptide Zhuang Y, Wang L, Guo J, Sun D, Wang Y, Liu W, Xu HE, Zhang C 10.1038/S41467-022-28586-0 2022-03-30
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7TYF - 2.2 CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP1 		- amylin peptide
peptide Agonist adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP peptide Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM 10.1126/SCIENCE.ABM9609 2022-03-23
Gs αs Human - 53 β1 Rat γ2 Bovine Cryo-EM 7VBH 7VBH_refined 3.0 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Peptide 20
peptide Agonist glucagon-like peptide 1-(7-36) amide, glucagon, 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 2022-04-06
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7X2D 7X2D_refined 3.3 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - TAVAPADON chembl_ligand pubchem
small-molecule Agonist L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine small-molecule - - 2022-06-15
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7XOV - 3.0 CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human - Nanobody-35 - SR146131 pubchem gtoplig chembl_ligand
small-molecule Agonist desulfated cholecystokinin-8, CCK-58, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8 peptide Ding Y, Zhang H, Liao YY, Chen LN, Ji SY, Qin J, Mao C, Shen DD, Lin L, Wang H, Zhang Y, Li XM 10.1038/S41421-022-00420-3 2022-07-20
Gq/11 αq Human Gi2-mini-Gq chimera 57 β1 Human γ2 Human Cryo-EM 8DPI - 3.4 5HT2C 5-HT2C 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - lorcaserin pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist 5-hydroxytryptamine small-molecule Gumpper RH, Fay JF, Roth BL 10.1016/J.CELREP.2022.111211 2022-08-24
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7XZ5 - 3.1 GP119 GPR119 GPR18, GPR55 and GPR119 A (Rhodopsin) Human BRIL Nanobody-35 - (4R,7R,18E)-4,7-dihydroxy-N,N,N-trimethyl-10-oxo-3,5,9-trioxa-4-phosphaheptacos-18-en-1-aminium 4-oxide pubchem
small-molecule Agonist N-oleoylethanolamide, anandamide, N-palmitoylethanolamine, SEA small-molecule Xu P, Huang S, Guo S, Yun Y, Cheng X, He X, Cai P, Lan Y, Zhou H, Jiang H, Jiang Y, Xie X, Xu HE 10.1038/S41594-022-00816-5 2022-08-24
Gs αs Human Mini-Gs 59 β1 Human γ2 Human Cryo-EM 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 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
Gq/11 αq Human Mini-Gq 56 β1 Human γ2 Human Cryo-EM 8E9Y - 2.8 ACM3 M3 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - Clozapine N-oxide pubchem
small-molecule Agonist acetylcholine small-molecule Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL 10.1038/S41586-022-05489-0 2022-11-30
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, neuropeptide Y-(3-36), PYY-(3-36), neuropeptide Y, peptide YY 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 - 62 β1 Human γ2 Human Cryo-EM 7T96 7T96_refined 3.2 ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - acetylcholine pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
LY2119620 pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Agonist
PAM 		acetylcholine small-molecule - - 2023-01-25
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 7Y64 - 2.9 C5AR1 C5a1 Complement peptide A (Rhodopsin) Human - scFv16 - C5a anaphylatoxin
peptide Agonist ribosomal protein S19, C5a, C5a des-Arg, C3a peptide Feng Y, Zhao C, Deng Y, Wang H, Ma L, Liu S, Tian X, Wang B, Bin Y, Chen P, Yan W, Fu P, Shao Z 10.1038/S41422-023-00779-2 2023-03-01
Gs αs Human Mini-Gs 57 β1 Human γ2 Human Cryo-EM 8IRR - 3.2 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - rotigotine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine small-molecule Xu P, Huang S, Krumm BE, Zhuang Y, Mao C, Zhang Y, Wang Y, Huang XP, Liu YF, He X, Li H, Yin W, Jiang Y, Zhang Y, Roth BL, Xu HE 10.1038/S41422-023-00808-0 2023-06-21
Gi/o αi1 Human - 58 β1 Human γ2 Human Cryo-EM 8GDC 8GDC_refined 3.5 PE2R3 EP3 Prostanoid A (Rhodopsin) Human - - - PGE2 pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
small-molecule Agonist thromboxane A2, PGF2α, PGI2, PGD2, PGE1, PGE2 small-molecule Huang SM, Xiong MY, Liu L, Mu J, Wang MW, Jia YL, Cai K, Tie L, Zhang C, Cao S, Wen X, Wang JL, Guo SC, Li Y, Qu CX, He QT, Cai BY, Xue C, Gan S, Xie Y, Cong X, Yang Z, Kong W, Li S, Li Z, Xiao P, Yang F, Yu X, Guan YF, Zhang X, Liu Z, Yang BX, Du Y, Sun JP 10.1073/PNAS.2216329120 2024-01-10
Gq/11 αq Human - 61 β1 Human γ2 Human Cryo-EM 8IA7 8IA7_refined 3.1 GASR CCK2 Cholecystokinin A (Rhodopsin) Human - - - CHEMBL216166 chembl_ligand pubchem
protein Agonist desulfated gastrin-14, desulfated cholecystokinin-8, gastrin-34, gastrin-14, CCK-58, desulfated gastrin-17, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8, desulfated gastrin-34, gastrin-71, 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 2023-12-06
Gs αs Human - 58 β1 Rat γ2 Bovine Cryo-EM 8JIT - 2.9 GLR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - MEDI0382
peptide Agonist glucagon peptide Li Y, Zhou Q, Dai A, Zhao F, Chang R, Ying T, Wu B, Yang D, Wang MW, Cong Z 10.1073/PNAS.2303696120 2023-09-06
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8WC5 - 3.3 TAAR1 TA1 Trace amine A (Rhodopsin) Mouse - scFv16 - Tetramethylammonium chembl_ligand pubchem
small-molecule Agonist β-phenylethylamine, 3-iodothyronamine, tyramine small-molecule Shang P, Rong N, Jiang JJ, Cheng J, Zhang MH, Kang D, Qi L, Guo L, Yang GM, Liu Q, Zhou Z, Li XB, Zhu KK, Meng QB, Han X, Yan W, Kong Y, Yang L, Wang X, Lei D, Feng X, Liu X, Yu X, Wang Y, Li Q, Shao ZH, Yang F, Sun JP 10.1016/J.CELL.2023.10.014 2023-12-27
Gs αs Human - 57 β1 Human γ2 Human Cryo-EM 6GDG 6GDG_refined 4.1 AA2AR A2A Adenosine A (Rhodopsin) Human TrxA Nanobody-35 - NECA pubchem gtoplig chembl_ligand gtoplig
small-molecule Agonist adenosine small-molecule Garcia-Nafria J, Lee Y, Bai X, Carpenter B, Tate CG 10.7554/ELIFE.35946 2018-05-16
Gs αs Human - 48 β1 Human γ2 Human Cryo-EM 6UUN 6UUN_refined 3.0 CALRL calcitonin-like Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP2 		- Adrenomedullin pubchem
peptide Agonist - - Liang YL, Belousoff MJ, Fletcher MM, Zhang X, Khoshouei M, Deganutti G, Koole C, Furness SGB, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Danev R, Wootten D, Sexton PM 10.1021/ACSPTSCI.9B00080 2020-03-25
Gi/o αi1 Human - 65 β1 Human γ2 Human Cryo-EM 6LFM 6LFM_refined 3.5 CXCR2 CXCR2 Chemokine A (Rhodopsin) Human - scFv16 - Interleukin-8 pubchem
protein Agonist CXCL8, CXCL1, CXCL5, CXCL2, CXCL7, CXCL6, CXCL3 peptide Liu K, Wu L, Yuan S, Wu M, Xu Y, Sun Q, Li S, Zhao S, Hua T, Liu ZJ 10.1038/S41586-020-2492-5 2020-09-02
Gs αs Bovine - 60 β1 Rat γ2 Bovine Cryo-EM 7FIH - 3.2 LSHR LH Glycoprotein hormone A (Rhodopsin) Human - - - Glycoprotein alpha gtoplig
Choriogonadotropin beta gtoplig
5-Amino-N-(1,1-dimethylethyl)-2-(methylthio)-4-[3-[[2-(4-morpholinyl)acetyl]amino]phenyl]thieno[2,3-d]pyrimidine-6-carboxamide pubchem
protein
protein
small-molecule 		Agonist 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 - 61 β1 Human γ2 Human Cryo-EM 7U2L - 3.2 OPRM μ Opioid A (Rhodopsin) Mouse - scFv16 - N-(5-carbamimidamidopentyl)-N-[1-(2-phenylethyl)piperidin-4-yl]propanamide
small-molecule Agonist - - Faouzi A, Wang H, Zaidi SA, DiBerto JF, Che T, Qu Q, Robertson MJ, Madasu MK, El Daibani A, Varga BR, Zhang T, Ruiz C, Liu S, Xu J, Appourchaux K, Slocum ST, Eans SO, Cameron MD, Al-Hasani R, Pan YX, Roth BL, McLaughlin JP, Skiniotis G, Katritch V, Kobilka BK, Majumdar S 10.1038/S41586-022-05588-Y 2022-05-04
Gs αs Human - 59 β1 Rat γ2 Bovine Cryo-EM 7XJI - 3.9 ADRB3 β3 Adrenoceptors A (Rhodopsin) Dog - Nanobody-35 - 3-[3-[2-[[(2~{S})-2-(3-chlorophenyl)-2-oxidanyl-ethyl]amino]ethylamino]phenyl]benzoic acid pubchem
small-molecule Agonist - - Nureki I, Kobayashi K, Tanaka T, Demura K, Inoue A, Shihoya W, Nureki O 10.1016/J.BBRC.2022.04.065 2022-05-04
Gq/11 αq Human - 58 β1 Human γ2 Human Cryo-EM 7XJL 7XJL_refined 3.5 GALR2 GAL2 Galanin A (Rhodopsin) Human - scFv16 - Spexin pubchem
small-molecule Agonist galanin-like peptide, spexin-1, galanin peptide Jiang W, Zheng S 10.1073/PNAS.2121465119 2022-06-29
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 7XBD 7XBD_refined 3.1 GALR2 GAL2 Galanin A (Rhodopsin) Human - scFv16 - Galanin, Human pubchem
peptide Agonist galanin-like peptide, spexin-1, galanin peptide Heo Y, Ishimoto N, Jeon YE, Yun JH, Ohki M, Anraku Y, Sasaki M, Kita S, Fukuhara H, Ikuta T, Kawakami K, Inoue A, Maenaka K, Tame JRH, Lee W, Park SY 10.1371/JOURNAL.PBIO.3001714 2022-07-13
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 7XMT 7XMT_refined 2.8 SSR4 SST4 Somatostatin A (Rhodopsin) Human - scFv16 - J-2156 pubchem gtoplig chembl_ligand
small-molecule Agonist SRIF-28, cortistatin-14, CST-17, SRIF-14 peptide Zhao W, Han S, Qiu N, Feng W, Lu M, Zhang W, Wang M, Zhou Q, Chen S, Xu W, Du J, Chu X, Yi C, Dai A, Hu L, Shen MY, Sun Y, Zhang Q, Ma Y, Zhong W, Yang D, Wang MW, Wu B, Zhao Q 10.1038/S41422-022-00679-X 2022-08-03
Gs αs Human - 57 β1 Human γ2 Human Cryo-EM 7XKF - 2.4 AGRG2 ADGRG2 ADGRG B2 (Adhesion) Mouse - Nanobody-35 - PRASTERONE chembl_ligand pubchem
small-molecule Agonist - - Lin H, Xiao P, Bu RQ, Guo S, Yang Z, Yuan D, Zhu ZL, Zhang CX, He QT, Zhang C, Ping YQ, Zhao RJ, Ma CS, Liu CH, Zhang XN, Jiang D, Huang S, Xi YT, Zhang DL, Xue CY, Yang BS, Li JY, Lin HC, Zeng XH, Zhao H, Xu WM, Yi F, Liu Z, Sun JP, Yu X 10.1038/S41589-022-01084-6 2022-08-10
Gq/11 αq Human Gi2-mini-Gq chimera 58 β1 Human γ2 Human Cryo-EM 7SRR - 2.9 5HT2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - Lysergide pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist 5-hydroxytryptamine small-molecule Cao C, Barros-Alvarez X, Zhang S, Kim K, Damgen MA, Panova O, Suomivuori CM, Fay JF, Zhong X, Krumm BE, Gumpper RH, Seven AB, Robertson MJ, Krogan NJ, Huttenhain R, Nichols DE, Dror RO, Skiniotis G, Roth BL 10.1016/J.NEURON.2022.08.006 2022-09-21
Gi/o αo Human - 58 β1 Human γ2 Human Cryo-EM 7W6P - 3.5 ADA2A α2A Adrenoceptors A (Rhodopsin) Human - scFv16 - N-pyridin-4-ylisoquinolin-4-amine pubchem
small-molecule Agonist (-)-adrenaline, (-)-noradrenaline small-molecule Fink EA, Xu J, Hubner H, Braz JM, Seemann P, Avet C, Craik V, Weikert D, Schmidt MF, Webb CM, Tolmachova NA, Moroz YS, Huang XP, Kalyanaraman C, Gahbauer S, Chen G, Liu Z, Jacobson MP, Irwin JJ, Bouvier M, Du Y, Shoichet BK, Basbaum AI, Gmeiner P 10.1126/SCIENCE.ABN7065 2022-09-28
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 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
Gs αs Bovine - 60 β1 Rat γ2 Bovine Cryo-EM 8HAF - 3.3 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - PTHrP-(1-36) pubchem gtoplig
peptide Agonist TIP39, PTHrP-(1-36), PTHrP, PTH peptide Zhao LH, Yuan QN, Dai AT, He XH, Chen CW, Zhang C, Xu YW, Zhou Y, Wang MW, Yang DH, Xu HE 10.1038/S41401-022-01032-Z 2022-12-21
Gs αs Human Mini-Gs 61 β1 Human γ2 Human Cryo-EM 8HJ2 8HJ2_refined 3.8 GPR21 GPR21 A orphans A (Rhodopsin) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Lin X, Chen B, Wu Y, Han Y, Qi A, Wang J, Yang Z, Wei X, Zhao T, Wu L, Xie X, Sun J, Zheng J, Zhao S, Xu F 10.1038/S41467-023-35882-W 2023-03-15
Gs αs Human Gs fused to receptor 57 β1 Human γ2 Human Cryo-EM 7TMW - 3.2 RXFP1 RXFP1 Relaxin family peptide A (Rhodopsin) Human - Nanobody-35 - H2 relaxin pubchem
small-molecule Agonist relaxin, relaxin-1, relaxin-3 peptide - - 2023-02-15
Gi/o αgust Human - 58 β1 Human γ2 Human Cryo-EM 8DZR - 2.6 OPRK κ Opioid A (Rhodopsin) Human - scFv16 - CHEMBL277863 chembl_ligand pubchem
small-molecule Agonist [Leu]enkephalin, β-neoendorphin, β-endorphin, dynorphin A, [Met]enkephalin, α-neoendorphin, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13), big dynorphin 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 - 62 β1 Human γ2 Human Cryo-EM 8GUT 8GUT_refined 3.0 CNR2 CB2 Cannabinoid A (Rhodopsin) Human - scFv16 - 1-[[4-[5-Fluoro-6-[(oxan-4-ylamino)methyl]pyridin-2-yl]phenyl]methyl]-3-(2-methylpropyl)imidazolidine-2,4-dione pubchem
small-molecule Agonist 2-arachidonoylglycerol, anandamide small-molecule Li X, Chang H, Bouma J, de Paus LV, Mukhopadhyay P, Paloczi J, Mustafa M, van der Horst C, Kumar SS, Wu L, Yu Y, van den Berg RJBHN, Janssen APA, Lichtman A, Liu ZJ, Pacher P, van der Stelt M, Heitman LH, Hua T 10.1038/S41467-023-37112-9 2023-05-10
G12/13 α13 Human Gi2-mini-G13 chimera 57 β1 Human γ2 Human Cryo-EM 7YDH - 3.1 AGRE5 ADGRE5 ADGRE B2 (Adhesion) Human - scFv16 - Apo (no ligand)
none Apo (no ligand) - - Wang N, Qian Y, Xia R, Zhu X, Xiong Y, Zhang A, Guo C, He Y 10.1016/J.CHEMBIOL.2023.08.003 2023-07-12
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8H4I - 3.1 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - Nanobody-35 - docosahexaenoic acid pubchem gtoplig chembl_ligand drug_central drugbank pubchem
small-molecule Agonist myristic acid, linoleic acid, α-linolenic 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 αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8J1A - 3.2 GPR84 GPR84 A orphans A (Rhodopsin) Human - scFv16 - Apo (no ligand)
none Apo (no ligand) - - Liu H, Zhang Q, He X, Jiang M, Wang S, Yan X, Cheng X, Liu Y, Nan FJ, Xu HE, Xie X, Yin W 10.1038/S41467-023-38985-6 2023-06-21
Gi/o αi1 Human - 62 β1 Mouse γ2 Mouse Cryo-EM 8IHI - 3.1 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human BRIL scFv16 - (5S)-5-methyl-4-oxo-5-phenylfuran-2-carboxylic acid pubchem
small-molecule Agonist β-D-hydroxybutyric acid, butyric acid small-molecule Suzuki S, Tanaka K, Nishikawa K, Suzuki H, Oshima A, Fujiyoshi Y 10.1038/S41467-023-41650-7 2023-08-30
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8JII - 3.2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - scFv16 - nicotinic acid pubchem gtoplig chembl_ligand drugbank drug_central gtoplig pubchem
compound 9n [PMID: 18752940] pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Agonist
PAM 		β-D-hydroxybutyric acid, butyric acid small-molecule Zhao C, Wang H, Liu Y, Cheng L, Wang B, Tian X, Fu H, Wu C, Li Z, Shen C, Yu J, Yang S, Hu H, Fu P, Ma L, Wang C, Yan W, Shao Z 10.1016/J.MOLCEL.2023.07.030 2023-09-06
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8KH5 - 2.8 GP174 GPR174 A orphans A (Rhodopsin) Human - Nanobody-35 - Lysophosphotidylserine pubchem
small-molecule Agonist lysophosphatidylserine small-molecule Nie Y, Qiu Z, Chen S, Chen Z, Song X, Ma Y, Huang N, Cyster JG, Zheng S 10.1038/S41467-023-41654-3 2023-10-18
Gs αs Human - 47 β1 Human γ2 Human Cryo-EM 5UZ7 - 4.1 CALCR CT Calcitonin B1 (Secretin) Human - - - calcitonin (salmon synthetic) pubchem
small-molecule Agonist adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP peptide Liang YL, Khoshouei M, Radjainia M, Zhang Y, Glukhova A, Tarrasch J, Thal DM, Furness SGB, Christopoulos G, Coudrat T, Danev R, Baumeister W, Miller LJ, Christopoulos A, Kobilka BK, Wootten D, Skiniotis G, Sexton PM 10.1038/NATURE22327 2017-05-03
Gs αs Human - 49 β1 Human γ2 Human Cryo-EM 6ORV 6ORV_refined 3.0 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - CHEMBL3950796 chembl_ligand pubchem
small-molecule Agonist glucagon-like peptide 1-(7-36) amide, glucagon, 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 - 58 β1 Human γ2 Human Cryo-EM 7D7M 7D7M_refined 3.3 PE2R4 EP4 Prostanoid A (Rhodopsin) Human - Nanobody-35 - PGE2 pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
small-molecule Agonist thromboxane A2, PGF2α, PGI2, PGD2, PGE1, PGE2 small-molecule Nojima S, Fujita Y, Kimura KT, Nomura N, Suno R, Morimoto K, Yamamoto M, Noda T, Iwata S, Shigematsu H, Kobayashi T 10.1016/J.STR.2020.11.007 2020-11-18
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7E2X - 3.0 5HT1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human - - - Apo (no ligand)
none Apo (no ligand) 5-hydroxytryptamine small-molecule Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen DD, Yen HY, Robinson CV, Harpsoe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE 10.1038/S41586-021-03376-8 2021-04-14
Gq/11 αq Human Gq-Gi1 chimera 61 β1 Rat γ2 Bovine Cryo-EM 7EIB - 3.0 BKRB1 B1 Bradykinin A (Rhodopsin) Human - - - [des-Arg10]kallidin pubchem gtoplig chembl_ligand gtoplig
peptide Agonist [des-Arg10]kallidin, Lys-[Hyp3]-bradykinin, kallidin, [des-Arg9]bradykinin, [Hyp3]bradykinin, T-kinin, bradykinin peptide Yin YL, Ye C, Zhou F, Wang J, Yang D, Yin W, Wang MW, Xu HE, Jiang Y 10.1038/S41594-021-00645-Y 2021-10-13
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7VDL - 3.2 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human - scFv16 - Cortistatin 14 pubchem
peptide Agonist PAMP-20 peptide Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP 10.1038/S41586-021-04077-Y 2021-12-01
Gi/o αi3 Human - 62 β1 Human γ2 Human Cryo-EM 7T10 - 2.5 SSR2 SST2 Somatostatin A (Rhodopsin) Human - scFv16 - SOMATOSTATIN chembl_ligand pubchem
protein Agonist SRIF-28, cortistatin-14, CST-17, SRIF-14 peptide Robertson MJ, Meyerowitz JG, Panova O, Borrelli K, Skiniotis G 10.1038/S41594-022-00727-5 2022-03-09
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7TZF - 2.4 CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP3 		- amylin peptide
peptide Agonist adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP peptide Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM 10.1126/SCIENCE.ABM9609 2022-03-23
Gq/11 αq Human - 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-23, neuromedin S-36, neuromedin S-33, neuromedin U-25 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 desulfated gastrin-14, desulfated cholecystokinin-8, gastrin-34, gastrin-14, CCK-58, desulfated gastrin-17, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8, desulfated gastrin-34, gastrin-71, 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
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 7VVK - 3.3 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - teriparatide pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem pubchem pubchem pubchem pubchem
peptide Agonist TIP39, PTHrP-(1-36), PTHrP, PTH peptide Kobayashi K, Kawakami K, Kusakizako T, Miyauchi H, Tomita A, Kobayashi K, Shihoya W, Yamashita K, Nishizawa T, Kato HE, Inoue A, Nureki O 10.1016/J.MOLCEL.2022.07.003 2022-08-03
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7VIF 7VIF_refined 2.8 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - (S)-FTY720-phosphate pubchem gtoplig chembl_ligand
small-molecule Agonist 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
Gq/11 αq Human - 58 β1 Rat γ2 Bovine Cryo-EM 7XW9 - 2.7 TRFR TRH1 Thyrotropin-releasing hormone A (Rhodopsin) Human - scFv16 - TRH pubchem
peptide Agonist TRH peptide - - 2022-12-28
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 [Leu]enkephalin, β-endorphin, dynorphin A, [Met]enkephalin, endomorphin-1, endomorphin-2, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13) peptide Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, Rao Q, Yang J, Liu J, Zhou Q, Wang X, Liu M, Liu W, Jiang X, Yang D, Jiang H, Shen J, Melcher K, Chen H, Jiang Y, Cheng X, Wang MW, Xie X, Xu HE 10.1016/J.CELL.2022.09.041 2022-11-09
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8ID3 8ID3_refined 3.1 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - scFv16 - 9-Hydroxyoctadecanoic acid pubchem
small-molecule Agonist myristic acid, linoleic acid, α-linolenic acid, oleic acid small-molecule Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP 10.1126/SCIENCE.ADD6220 2023-03-15
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8IW7 - 3.0 TAAR9 TAAR9 A orphans A (Rhodopsin) Mouse - scFv16 - 2-Phenylethanaminium pubchem
small-molecule Agonist - - Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP 10.1038/S41586-023-06106-4 2023-05-31
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8FLS - 3.1 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - abaloparatide pubchem
small-molecule Agonist TIP39, PTHrP-(1-36), PTHrP, PTH 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 - 57 β1 Rat γ2 Bovine Cryo-EM 7Y35 - 2.9 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - abaloparatide pubchem
small-molecule Agonist TIP39, PTHrP-(1-36), PTHrP, PTH peptide - - 2023-07-05
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8J19 - 3.2 GPR84 GPR84 A orphans A (Rhodopsin) Human - scFv16 - 6-nonylpyridine-2,4-diol pubchem gtoplig chembl_ligand
small-molecule Agonist - - Liu H, Zhang Q, He X, Jiang M, Wang S, Yan X, Cheng X, Liu Y, Nan FJ, Xu HE, Xie X, Yin W 10.1038/S41467-023-38985-6 2023-06-21
Gi/o αi1 Human - 55 β1 Human γ2 Human Cryo-EM 8FEG - 2.5 OPRK κ Opioid A (Rhodopsin) Human - scFv16 - ACE-TYR-ALA-DTY-THR-THR-CYS-THR-DPN-XT9
peptide Agonist [Leu]enkephalin, β-neoendorphin, β-endorphin, dynorphin A, [Met]enkephalin, α-neoendorphin, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13), big dynorphin peptide Cheng Y, Prusoff WH 10.1016/0006-2952(73)90196-2 2023-12-06
Gq/11 αq Human - 58 β1 Human γ2 Human Cryo-EM 8I9A - 3.6 C3AR C3a Complement peptide A (Rhodopsin) Human - scFv16 - EP54 ligand
peptide Agonist C5a, C3a peptide Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C 10.1016/J.CELL.2023.09.020 2023-10-18
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8J6P - 2.6 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - scFv16 - nicotinic acid pubchem gtoplig chembl_ligand drugbank drug_central gtoplig pubchem
small-molecule Agonist β-D-hydroxybutyric acid, butyric acid small-molecule Mao C, Gao M, Zang SK, Zhu Y, Shen DD, Chen LN, Yang L, Wang Z, Zhang H, Wang WW, Shen Q, Lu Y, Ma X, Zhang Y 10.1038/S41467-023-43537-Z 2023-12-06
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8SAI 8SAI_refined 3.3 GPR34 GPR34 A orphans A (Rhodopsin) Human - scFv16 - O-[(S)-Hydroxy{[(2s)-2-Hydroxy-3-(Octadec-9-Enoyloxy)propyl]oxy}phosphoryl]-L-Serine pubchem
small-molecule Agonist lysophosphatidylserine small-molecule Xia A, Yong X, Zhang C, Lin G, Jia G, Zhao C, Wang X, Hao Y, Wang Y, Zhou P, Yang X, Deng Y, Wu C, Chen Y, Zhu J, Tang X, Liu J, Zhang S, Zhang J, Xu Z, Hu Q, Zhao J, Yue Y, Yan W, Su Z, Wei Y, Zhou R, Dong H, Shao Z, Yang S 10.1073/PNAS.2308435120 2023-10-04
Gs αs Bovine - 56 β1 Rat γ2 Bovine Cryo-EM 6NBI - 4.0 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - Long-acting parathyroid hormone analog
peptide Agonist TIP39, PTHrP-(1-36), PTHrP, PTH peptide Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y 10.1126/SCIENCE.AAV7942 2019-04-17
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 6PB1 6PB1_refined 2.8 CRFR2 CRF2 Corticotropin-releasing factor B1 (Secretin) Human - Nanobody-35 - Urocortin pubchem
peptide Agonist urocortin 1, corticotrophin-releasing hormone, urocortin 2, urocortin 3 peptide Ma S, Shen Q, Zhao LH, Mao C, Zhou XE, Shen DD, de Waal PW, Bi P, Li C, Jiang Y, Wang MW, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE 10.1016/J.MOLCEL.2020.01.013 2020-02-12
Gs αs Human - 89 β1 Human γ2 Human Cryo-EM 6X19 - 2.1 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - CHU-128 pubchem
small-molecule Agonist glucagon-like peptide 1-(7-36) amide, glucagon, 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
Gs αs Human - 55 β1 Bovine γ2 Bovine Cryo-EM 7DHI - 3.3 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - Nanobody-35 - levosalbutamol pubchem gtoplig chembl_ligand drug_central drugbank
small-molecule Agonist L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline small-molecule Si G, Du Y, Tang P, Ma G, Jia Z, Zhou X, Mu D, Shen Y, Lu Y, Mao Y, Chen C, Li Y, Gu N 10.1093/NSR/NWAA284 2020-12-16
Gs αs Human Engineered G alpha 60 β1 Human γ2 Human Cryo-EM 7JVQ 7JVQ_refined 3.0 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - apomorphine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine small-molecule Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP, Shen DD, Xu T, Liu YF, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE 10.1016/J.CELL.2021.01.027 2021-02-24
Gi/o αi1 Human - 99 β1 Human γ2 Human Cryo-EM 7EB2 - 3.5 GABR2 GABAB2 GABAB C (Glutamate) Human - scFv16 - (-)-baclofen pubchem gtoplig chembl_ligand drugbank drugbank gtoplig pubchem
BHFF pubchem
small-molecule
small-molecule 		Agonist
PAM 		- - Shen C, Mao C, Xu C, Jin N, Zhang H, Shen DD, Shen Q, Wang X, Hou T, Chen Z, Rondard P, Pin JP, Zhang Y, Liu J 10.1038/S41586-021-03507-1 2021-05-05
Gs αs Human - 60 β1 Rat γ2 Bovine Cryo-EM 7DUR - 3.3 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - N-Tert-butyl-6,7-dichloroquinoxalin-2-amine pubchem
small-molecule Ago-PAM glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) peptide Cong Z, Chen LN, Ma H, Zhou Q, Zou X, Ye C, Dai A, Liu Q, Huang W, Sun X, Wang X, Xu P, Zhao L, Xia T, Zhong W, Yang D, Eric Xu H, Zhang Y, Wang MW 10.1038/S41467-021-24058-Z 2021-08-11
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7EW2 - 3.1 S1PR3 S1P3 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - (S)-FTY720-phosphate 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
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7F55 - 3.1 MC4R MC4 Melanocortin A (Rhodopsin) Human - Nanobody-35 - bremelanotide pubchem gtoplig chembl_ligand drugbank drug_central
peptide Agonist β-MSH, α-MSH, agouti-related protein, γ-MSH, ACTH peptide Zhang H, Chen LN, Yang D, Mao C, Shen Q, Feng W, Shen DD, Dai A, Xie S, Zhou Y, Qin J, Sun JP, Scharf DH, Hou T, Zhou T, Wang MW, Zhang Y 10.1038/S41422-021-00552-3 2021-11-03
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7F4F - 2.9 MSHR MC1 Melanocortin A (Rhodopsin) Human - scFv16 - CHEMBL407070 chembl_ligand pubchem pubchem
protein Agonist β-MSH, ACTH, γ-MSH, α-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
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7TYX - 2.6 CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - Amylin rat pubchem
peptide Agonist adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP peptide Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM 10.1126/SCIENCE.ABM9609 2022-03-30
Gi/o αi1 Human Mini-Gi1 58 β1 Human γ2 Human Cryo-EM 7WU4 - 3.4 AGRF1 ADGRF1 ADGRF B2 (Adhesion) Human - - - Apo (no ligand)
none Apo (no ligand) - - - - 2022-04-27
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7X9B 7X9B_refined 3.4 NPY2R Y2 Neuropeptide Y A (Rhodopsin) Human - - - neuropeptide Y pubchem gtoplig chembl_ligand gtoplig gtoplig pubchem pubchem pubchem
peptide Agonist pancreatic polypeptide, neuropeptide Y-(3-36), PYY-(3-36), neuropeptide Y, peptide YY peptide Tang T, Tan Q, Han S, Diemar A, Lobner K, Wang H, Schuss C, Behr V, Morl K, Wang M, Chu X, Yi C, Keller M, Kofoed J, Reedtz-Runge S, Kaiser A, Beck-Sickinger AG, Zhao Q, Wu B 10.1126/SCIADV.ABM1232 2022-05-18
Gs αs Human - 61 β1 Human γ2 Human Cryo-EM 7XTC 7XTC_refined 3.2 5HT7R 5-HT7 5-Hydroxytryptamine A (Rhodopsin) Human BRIL Nanobody-35 - 5-CT pubchem gtoplig chembl_ligand
small-molecule Agonist 5-hydroxytryptamine small-molecule Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE 10.1016/J.MOLCEL.2022.05.031 2022-07-27
Gi/o αi1 Human - 63 β1 Bovine γ2 Bovine Cryo-EM 7XAT 7XAT_refined 2.9 SSR2 SST2 Somatostatin A (Rhodopsin) Human - scFv16 - SOMATOSTATIN chembl_ligand pubchem
protein Agonist SRIF-28, cortistatin-14, CST-17, 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 Mini-Gs 60 β1 Human γ2 Human Cryo-EM 7XKE - 2.9 AGRG2 ADGRG2 ADGRG B2 (Adhesion) Mouse - Nanobody-35 - PRASTERONE chembl_ligand pubchem
small-molecule Agonist - - Lin H, Xiao P, Bu RQ, Guo S, Yang Z, Yuan D, Zhu ZL, Zhang CX, He QT, Zhang C, Ping YQ, Zhao RJ, Ma CS, Liu CH, Zhang XN, Jiang D, Huang S, Xi YT, Zhang DL, Xue CY, Yang BS, Li JY, Lin HC, Zeng XH, Zhao H, Xu WM, Yi F, Liu Z, Sun JP, Yu X 10.1038/S41589-022-01084-6 2022-08-10
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7WCN 7WCN_refined 2.9 GP119 GPR119 GPR18, GPR55 and GPR119 A (Rhodopsin) Human - Nanobody-35 - AR231453 pubchem gtoplig chembl_ligand
small-molecule Agonist N-oleoylethanolamide, anandamide, N-palmitoylethanolamine, SEA small-molecule Qian Y, Wang J, Yang L, Liu Y, Wang L, Liu W, Lin Y, Yang H, Ma L, Ye S, Wu S, Qiao A 10.1038/S41467-022-34696-6 2022-12-21
Gq/11 αq Human Mini-Gq 60 β1 Human γ2 Human Cryo-EM 7Y26 7Y26_refined 3.3 SSR2 SST2 Somatostatin A (Rhodopsin) Human - scFv16 - Octreotide
peptide Agonist SRIF-28, cortistatin-14, CST-17, SRIF-14 peptide Chen S, Teng X, Zheng S 10.1038/S41589-022-01130-3 2022-10-19
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 B chain pubchem
Insulin-like peptide INSL5 A chain pubchem
peptide
peptide 		Agonist INSL5, relaxin-3 (B chain), relaxin-3 peptide Chen Y, Zhou Q, Wang J, Xu Y, Wang Y, Yan J, Wang Y, Zhu Q, Zhao F, Li C, Chen CW, Cai X, Bathgate RAD, Shen C, Eric Xu H, Yang D, Liu H, Wang MW 10.1038/S41467-023-36182-Z 2023-03-01
Gs αs Human Mini-Gs 61 β1 Human γ2 Human Cryo-EM 8HIX - 3.1 GPR21 GPR21 A orphans A (Rhodopsin) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Lin X, Chen B, Wu Y, Han Y, Qi A, Wang J, Yang Z, Wei X, Zhao T, Wu L, Xie X, Sun J, Zheng J, Zhao S, Xu F 10.1038/S41467-023-35882-W 2023-03-15
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
Gi/o αi1 Human - 60 β1 Human γ2 Human Cryo-EM 8DZP - 2.7 OPRK κ Opioid A (Rhodopsin) Human - scFv16 - SALVINORIN B METHOXYMETHYL ETHER chembl_ligand pubchem
small-molecule Agonist [Leu]enkephalin, β-neoendorphin, β-endorphin, dynorphin A, [Met]enkephalin, α-neoendorphin, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13), big dynorphin 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 - 64 β1 Human γ2 Human Cryo-EM 7YAC 7YAC_refined 3.2 SSR2 SST2 Somatostatin A (Rhodopsin) Human - scFv16 - PALTUSOTINE chembl_ligand pubchem
small-molecule Agonist SRIF-28, cortistatin-14, CST-17, 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
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 8IUK - 2.7 PF2R FP Prostanoid A (Rhodopsin) Human - scFv16
Nanobody-35 		- PGF2α pubchem gtoplig chembl_ligand drug_central drugbank
small-molecule Agonist thromboxane A2, PGF2α, 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
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8JLZ - 3.1 5HT6R 5-HT6 5-Hydroxytryptamine A (Rhodopsin) Human - Nanobody-35 - CHEMBL365751 chembl_ligand pubchem
small-molecule Agonist 5-hydroxytryptamine small-molecule Pei Y, Wen X, Guo SC, Yang ZS, Zhang R, Xiao P, Sun JP 10.1016/J.BBRC.2023.05.126 2023-06-28
Gq/11 αq Human - 57 β1 Human γ2 Human Cryo-EM 8THK - 2.6 ADA1A α1A Adrenoceptors A (Rhodopsin) Human T4-Lysozyme scFv16 - CHEMBL133451 chembl_ligand pubchem
small-molecule Agonist (-)-adrenaline, (-)-noradrenaline small-molecule Su M, Wang J, Xiang G, Do HN, Levitz J, Miao Y, Huang XY 10.1038/S41467-023-40524-2 2023-08-16
Gi/o αo Human - 59 β1 Human γ2 Human Cryo-EM 8IA2 8IA2_refined 3.2 C5AR1 C5a1 Complement peptide A (Rhodopsin) Human - scFv16 - C5a gtoplig
peptide Agonist ribosomal protein S19, C5a, C5a des-Arg, C3a peptide Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C 10.1016/J.CELL.2023.09.020 2023-10-18
Gs αs Human - 61 β1 Human γ2 Human Cryo-EM 8JLO - 3.5 TAAR1 TA1 Trace amine A (Rhodopsin) Human - - - ulotaront pubchem gtoplig drugbank chembl_ligand
small-molecule Agonist β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, dopamine small-molecule Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z 10.1038/S41586-023-06804-Z 2023-11-15
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 6OS9 6OS9_refined 3.0 NTR1 NTS1 Neurotensin A (Rhodopsin) Human - scFv16 - JMV449 pubchem gtoplig chembl_ligand
peptide Agonist large neurotensin, large neuromedin N, neurotensin, neuromedin N peptide Kato HE, Zhang Y, Hu H, Suomivuori CM, Kadji FMN, Aoki J, Krishna Kumar K, Fonseca R, Hilger D, Huang W, Latorraca NR, Inoue A, Dror RO, Kobilka BK, Skiniotis G 10.1038/S41586-019-1337-6 2019-07-10
Gs αs Human - 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
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
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7E32 - 2.9 5HT1D 5-HT1D 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - 5-hydroxytryptamine pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist 5-hydroxytryptamine, 5-HT-moduline small-molecule Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen DD, Yen HY, Robinson CV, Harpsoe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE 10.1038/S41586-021-03376-8 2021-04-21
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7EZK - 3.1 CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human - - - CCK-8 pubchem gtoplig chembl_ligand drug_central drugbank
peptide Agonist desulfated cholecystokinin-8, CCK-58, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8 peptide Liu Q, Yang D, Zhuang Y, Croll TI, Cai X, Dai A, He X, Duan J, Yin W, Ye C, Zhou F, Wu B, Zhao Q, Xu HE, Wang MW, Jiang Y 10.1038/S41589-021-00841-3 2021-08-25
Gi/o αi1 Human - 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
Gq/11 αq Human Gamma subunit fused to alpha subunit 55 β1 Human - - Cryo-EM 7RYC - 2.9 OXYR OT Vasopressin and oxytocin A (Rhodopsin) Human - scFv16 - oxytocin pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
peptide Agonist vasopressin, oxytocin peptide Meyerowitz JG, Robertson MJ, Barros-Alvarez X, Panova O, Nwokonko RM, Gao Y, Skiniotis G 10.1038/S41594-022-00728-4 2022-03-09
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7TYH - 3.3 CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - Calcitonin human pubchem
peptide Agonist adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP peptide - - 2022-03-23
Gs αs Human - 55 β1 Human γ2 Human Cryo-EM 7WUQ - 2.9 AGRG2 ADGRG2 ADGRG B2 (Adhesion) Mouse - Nanobody-35 - - - - - - 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 - 58 β1 Human γ2 Human Cryo-EM 7F0T - 3.1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - dopamine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine small-molecule Teng X, Chen S, Wang Q, Chen Z, Wang X, Huang N, Zheng S 10.1126/SCIADV.ABO4158 2022-06-15
Gs αs Human - 60 β1 Rat γ2 Human Cryo-EM 7X8S 7X8S_refined 3.1 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - WB4-24 pubchem gtoplig chembl_ligand
small-molecule Agonist glucagon-like peptide 1-(7-36) amide, glucagon, 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
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, cortistatin-14, CST-17, SRIF-14 peptide Zhao W, Han S, Qiu N, Feng W, Lu M, Zhang W, Wang M, Zhou Q, Chen S, Xu W, Du J, Chu X, Yi C, Dai A, Hu L, Shen MY, Sun Y, Zhang Q, Ma Y, Zhong W, Yang D, Wang MW, Wu B, Zhao Q 10.1038/S41422-022-00679-X 2022-08-03
Gs αs Human - 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 αo Human - 59 β1 Human γ2 Human Cryo-EM 7W7E - 3.4 ADA2A α2A Adrenoceptors A (Rhodopsin) Human - scFv16 - 5-(3-Bicyclo[4.2.0]octa-1,3,5-trienyl)-1,2,3,6-tetrahydropyridine pubchem
small-molecule Agonist (-)-adrenaline, (-)-noradrenaline small-molecule Fink EA, Xu J, Hubner H, Braz JM, Seemann P, Avet C, Craik V, Weikert D, Schmidt MF, Webb CM, Tolmachova NA, Moroz YS, Huang XP, Kalyanaraman C, Gahbauer S, Chen G, Liu Z, Jacobson MP, Irwin JJ, Bouvier M, Du Y, Shoichet BK, Basbaum AI, Gmeiner P 10.1126/SCIENCE.ABN7065 2022-09-28
Gi/o 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 8F7Q - 3.2 OPRM μ Opioid A (Rhodopsin) Human - scFv16 - β-endorphin pubchem gtoplig chembl_ligand pubchem
peptide Agonist [Leu]enkephalin, β-endorphin, dynorphin A, [Met]enkephalin, endomorphin-1, endomorphin-2, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13) 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
G12/13 α13 Human - 60 β1 Human γ2 Human Cryo-EM 8H8J 8H8J_refined 3.2 GPR35 GPR35 A orphans A (Rhodopsin) Human - scFv16 - lodoxamide pubchem gtoplig chembl_ligand drug_central drugbank
small-molecule Agonist 1-Lyso-2-oleoyl-phosphatidic acid, 2-Oleoyllysophosphatydic acid, kynurenic acid, 2-oleoyl-LPA small-molecule Duan J, Liu Q, Yuan Q, Ji Y, Zhu S, Tan Y, He X, Xu Y, Shi J, Cheng X, Jiang H, Eric Xu H, Jiang Y 10.1038/S41421-022-00499-8 2023-02-08
Gq/11 αq Human - 79 β1 Human γ2 Human Cryo-EM 7W40 7W40_refined 3.0 GRPR BB2 Bombesin A (Rhodopsin) Human - scFv16 - Bombesin
peptide Agonist neuromedin B, gastrin releasing peptide(14-27) (human), GRP-(18-27), gastrin-releasing peptide, neuromedin C peptide Peng S, Zhan Y, Zhang D, Ren L, Chen A, Chen ZF, Zhang H 10.1073/PNAS.2216230120 2023-02-22
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7TRQ - 2.5 ACM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - iperoxo pubchem gtoplig chembl_ligand
VU0467154 pubchem gtoplig chembl_ligand
small-molecule
small-molecule 		Agonist
PAM 		acetylcholine small-molecule - - 2023-05-17
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 8IRT - 2.7 DRD3 D3 Dopamine A (Rhodopsin) Human BRIL scFv16 - rotigotine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist dopamine small-molecule Xu P, Huang S, Krumm BE, Zhuang Y, Mao C, Zhang Y, Wang Y, Huang XP, Liu YF, He X, Li H, Yin W, Jiang Y, Zhang Y, Roth BL, Xu HE 10.1038/S41422-023-00808-0 2023-06-07
Gs αs Human - 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 Mouse - 64 β1 Human γ2 Human Cryo-EM 8FX5 - 2.5 ACM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - xanomeline pubchem gtoplig chembl_ligand drug_central drugbank
small-molecule Agonist acetylcholine small-molecule Burger WAC, Pham V, Vuckovic Z, Powers AS, Mobbs JI, Laloudakis Y, Glukhova A, Wootten D, Tobin AB, Sexton PM, Paul SM, Felder CC, Danev R, Dror RO, Christopoulos A, Valant C, Thal DM 10.1038/S41467-023-41199-5 2023-09-13
Gs αs Human - 40 β1 Human γ2 Human Cryo-EM 8HTI - 3.0 O52E4 Olfactory 52E4 Olfactory A (Rhodopsin) Human - Nanobody-35 - OCTANOIC ACID chembl_ligand pubchem pubchem
small-molecule Agonist - - Choi C, Bae J, Kim S, Lee S, Kang H, Kim J, Bang I, Kim K, Huh WK, Seok C, Park H, Im W, Choi HJ 10.1038/S41467-023-43983-9 2023-12-20
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8W8Q 8W8Q_refined 2.9 GP101 GPR101 A orphans A (Rhodopsin) Human BRIL Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Yang Z, Wang JY, Yang F, Zhu KK, Wang GP, Guan Y, Ning SL, Lu Y, Li Y, Zhang C, Zheng Y, Zhou SH, Wang XW, Wang MW, Xiao P, Yi F, Zhang C, Zhang PJ, Xu F, Liu BH, Zhang H, Yu X, Gao N, Sun JP 10.1038/S41589-023-01456-6 2024-01-03
Gs αs Human - 60 β1 Rat γ2 Bovine Cryo-EM 7V9L - 2.6 GHRHR GHRH Glucagon B1 (Secretin) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) GHRH peptide Cong Z, Zhou F, Zhang C, Zou X, Zhang H, Wang Y, Zhou Q, Cai X, Liu Q, Li J, Shao L, Mao C, Wang X, Wu J, Xia T, Zhao LH, Jiang H, Zhang Y, Xu HE, Cheng X, Yang D, Wang MW 10.1073/PNAS.2106606118 2022-04-06
Gi/o αt1 Bovine Only H5 3 - - - - X-ray 4X1H 4X1H_refined 2.3 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - - - B-Nonylglucoside pubchem
small-molecule unknown - - Blankenship E, Vahedi-Faridi A, Lodowski DT 10.1016/J.STR.2015.09.015 2015-11-04
Gs αs Human - 43 β1 Human γ2 Human Cryo-EM 6NIY - 3.3 CALCR CT Calcitonin B1 (Secretin) Human - - - calcitonin (salmon synthetic) pubchem
small-molecule Agonist adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP peptide Dal Maso E, Glukhova A, Zhu Y, Garcia-Nafria J, Tate CG, Atanasio S, Reynolds CA, Ramirez-Aportela E, Carazo JM, Hick CA, Furness SGB, Hay DL, Liang YL, Miller LJ, Christopoulos A, Wang MW, Wootten D, Sexton PM 10.1021/ACSPTSCI.8B00056 2019-01-23
Gi/o αo Human - 60 β1 Mouse γ2 Human Cryo-EM 6K41 - 2.9 ADA2B α2B Adrenoceptors A (Rhodopsin) Human T4-Lysozyme scFv - dexmedetomidine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist (-)-adrenaline, (-)-noradrenaline small-molecule Yuan D, Liu Z, Kaindl J, Maeda S, Zhao J, Sun X, Xu J, Gmeiner P, Wang HW, Kobilka BK 10.1038/S41589-020-0492-2 2020-04-15
Gs αs Human - 61 β1 Human γ2 Human Cryo-EM 6VN7 6VN7_refined 3.2 VIPR1 VPAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - [Ac-His1]PACAP-27 gtoplig chembl_ligand pubchem
peptide Agonist VIP, PHI, PHM, secretin, PACAP-27, GHRH, PACAP-38 peptide Duan J, Shen DD, Zhou XE, Bi P, Liu QF, Tan YX, Zhuang YW, Zhang HB, Xu PY, Huang SJ, Ma SS, He XH, Melcher K, Zhang Y, Xu HE, Jiang Y 10.1038/S41467-020-17933-8 2020-09-02
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 neurotensin, neuromedin N 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 - 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-58, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8 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-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) peptide Cong Z, Chen LN, Ma H, Zhou Q, Zou X, Ye C, Dai A, Liu Q, Huang W, Sun X, Wang X, Xu P, Zhao L, Xia T, Zhong W, Yang D, Eric Xu H, Zhang Y, Wang MW 10.1038/S41467-021-24058-Z 2021-07-14
Gi/o αi1 Human - 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 - 63 β1 Human γ2 Human Cryo-EM 7VGX 7VGX_refined 3.2 NPY1R Y1 Neuropeptide Y A (Rhodopsin) Human - scFv16 - neuropeptide Y pubchem gtoplig chembl_ligand gtoplig gtoplig pubchem pubchem pubchem
peptide Agonist peptide YY, neuropeptide Y, 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 Human Mini-Gs 60 β1 Rat γ2 Bovine Cryo-EM 7VAB 7VAB_refined 3.2 GIPR GIP Glucagon B1 (Secretin) Human - Nanobody-35 - tirzepatide pubchem gtoplig
peptide Agonist gastric inhibitory polypeptide peptide Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW 10.1038/S41467-022-28683-0 2022-03-02
Gs αs Human Engineered G alpha 56 β1 Human γ2 Human Cryo-EM 7RA3 - 3.2 GIPR GIP Glucagon B1 (Secretin) Human - scFv16
Nanobody-35 		- gastric inhibitory polypeptide (human) - Incretin pubchem
peptide Agonist gastric inhibitory polypeptide peptide Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW 10.1073/PNAS.2116506119 2022-04-13
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 7E2Z - 3.1 5HT1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human - - - aripiprazole pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist (partial) 5-hydroxytryptamine small-molecule Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen DD, Yen HY, Robinson CV, Harpsoe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE 10.1038/S41586-021-03376-8 2021-04-14
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7JHJ - 3.2 Q3KSP2 BILF1 Unclassified A (Rhodopsin) strain GD1 - scFv16 - Apo (no ligand)
none Apo (no ligand) - - Tsutsumi N, Qu Q, Mavri M, Baggesen MS, Maeda S, Waghray D, Berg C, Kobilka BK, Rosenkilde MM, Skiniotis G, Garcia KC 10.1016/J.IMMUNI.2021.06.001 2021-07-07
Gi/o αi1 Human - 62 β1 Rat γ2 Bovine Cryo-EM 7DB6 7DB6_refined 3.3 MTR1A MT1 Melatonin A (Rhodopsin) Human - scFv16 - ramelteon pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist melatonin small-molecule Okamoto HH, Miyauchi H, Inoue A, Raimondi F, Tsujimoto H, Kusakizako T, Shihoya W, Yamashita K, Suno R, Nomura N, Kobayashi T, Iwata S, Nishizawa T, Nureki O 10.1038/S41594-021-00634-1 2021-08-18
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7EW3 - 3.1 S1PR3 S1P3 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - Sphingosine 1-phosphate pubchem
lipid 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
Gq/11 αq Human Gq-Gs chimera 57 β1 Human γ2 Human Cryo-EM 7S8P 7S8P_refined 2.6 MRGX4 MRGPRX4 A orphans A (Rhodopsin) Human BRIL scFv16 - N-[(1r,3R,5S,7R)-3,5-dimethyltricyclo[3.3.1.1~3,7~]decane-1-carbonyl]-D-phenylalanine pubchem
small-molecule Agonist - - Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL 10.1038/S41586-021-04126-6 2021-11-17
Gs αs Human - 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 β-MSH, ACTH, γ-MSH, α-MSH peptide Ma S, Chen Y, Dai A, Yin W, Guo J, Yang D, Zhou F, Jiang Y, Wang MW, Xu HE 10.1038/S41422-021-00557-Y 2021-09-08
Gi/o αi1 Human - 64 β1 Rat γ2 Bovine Cryo-EM 7WQ3 7WQ3_refined 2.7 GALR1 GAL1 Galanin A (Rhodopsin) Human - scFv16 - galanin pubchem gtoplig chembl_ligand gtoplig pubchem pubchem pubchem pubchem
peptide Agonist galanin-like peptide, galanin peptide - - 2022-04-20
Gq/11 αq Human - 63 β1 Human γ2 Human Cryo-EM 7F6I 7F6I_refined 2.8 BKRB2 B2 Bradykinin A (Rhodopsin) Human - - - kallidin pubchem gtoplig
peptide Agonist [des-Arg10]kallidin, Lys-[Hyp3]-bradykinin, kallidin, [des-Arg9]bradykinin, [Hyp3]bradykinin, T-kinin, bradykinin peptide Shen J, Zhang D, Fu Y, Chen A, Yang X, Zhang H 10.1038/S41467-022-28399-1 2022-01-05
Gs αs Human - 59 β1 Rat γ2 Human Cryo-EM 7X8R - 2.6 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - CHEMBL2158411 chembl_ligand pubchem
small-molecule Agonist glucagon-like peptide 1-(7-36) amide, glucagon, 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
Gq/11 αq Human Mini-Gq 59 β1 Human γ2 Human Cryo-EM 7WY5 - 2.8 AGRL3 ADGRL3 ADGRL B2 (Adhesion) Mouse - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Qian Y, Ma Z, Liu C, Li X, Zhu X, Wang N, Xu Z, Xia R, Liang J, Duan Y, Yin H, Xiong Y, Zhang A, Guo C, Chen Z, Huang Z, He Y 10.1016/J.MOLCEL.2022.10.009 2022-10-26
Gi/o αi1 Human - 63 β1 Rat γ2 Bovine Cryo-EM 7YU3 7YU3_refined 3.4 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human - scFv16 - [(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate pubchem
small-molecule Agonist 1-O-Oleoyl-D-glycerol 3-phosphoric acid small-molecule Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O 10.1038/S41467-022-33121-2 2022-10-05
Gi/o αi1 Human - 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 [Leu]enkephalin, β-endorphin, dynorphin A, [Met]enkephalin, endomorphin-1, endomorphin-2, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13) 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 Luo P, Feng W, Ma S, Dai A, Wu K, Chen X, Yuan Q, Cai X, Yang D, Wang MW, Eric Xu H, Jiang Y 10.1038/S41422-022-00751-6 2023-01-11
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 7TRS - 2.8 ACM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - acetylcholine pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
small-molecule Agonist acetylcholine small-molecule - - 2023-05-17
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 8EJK - 3.4 FFAR1 FFA1 Free fatty acid A (Rhodopsin) Human - scFv16 - fasiglifam pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist myristic acid, oleic acid, α-linolenic acid, docosahexaenoic acid small-molecule Kumari P, Inoue A, Chapman K, Lian P, Rosenbaum DM 10.1073/PNAS.2219569120 2023-05-24
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7YKD - 2.8 CML1 chemerin Chemerin receptor A (Rhodopsin) Human - scFv16 - chemerin C-terminal peptide pubchem gtoplig chembl_ligand pubchem
peptide Agonist 18R-HEPE, chemerin C-terminal peptide, EPA, resolvin E1, 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 - 62 β1 Human γ2 Human Cryo-EM 7YFD - 3.1 HRH4 H4 Histamine A (Rhodopsin) Human - scFv16
Nanobody-35 		- imetit pubchem gtoplig chembl_ligand pubchem
small-molecule Agonist histamine, CCL16 small-molecule Im D, Kishikawa JI, Shiimura Y, Hisano H, Ito A, Fujita-Fujiharu Y, Sugita Y, Noda T, Kato T, Asada H, Iwata S 10.1038/S41467-023-42260-Z 2023-10-25
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8HNK - 3.0 CXCR3 CXCR3 Chemokine A (Rhodopsin) Human - scFv16 - CXCL11 gtoplig
peptide Agonist CCL19, CXCL11, CCL13, CXCL9, CXCL10, CCL7, CCL5, CCL11, CXCL12α, CCL20 peptide Jiao H, Pang B, Liu A, Chen Q, Pan Q, Wang X, Xu Y, Chiang YC, Ren R, Hu H 10.1038/S41594-023-01175-5 2023-11-29
Gs αs Human - 56 β1 Rat γ2 Bovine Cryo-EM 8JIQ 8JIQ_refined 3.4 GLR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - Dual-agonist peptide P15
peptide Agonist glucagon peptide Li Y, Zhou Q, Dai A, Zhao F, Chang R, Ying T, Wu B, Yang D, Wang MW, Cong Z 10.1073/PNAS.2303696120 2023-09-13
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 6DDF - 3.5 OPRM μ Opioid A (Rhodopsin) Mouse - - - DAMGO pubchem gtoplig chembl_ligand chembl_ligand
peptide Agonist - - Koehl A, Hu H, Maeda S, Zhang Y, Qu Q, Paggi JM, Latorraca NR, Hilger D, Dawson R, Matile H, Schertler GFX, Granier S, Weis WI, Dror RO, Manglik A, Skiniotis G, Kobilka BK 10.1038/S41586-018-0219-7 2018-06-13
Gi/o αi1 Human - 100 β1 Human γ2 Human Cryo-EM 6OT0 - 3.9 SMO SMO Frizzled F (Frizzled) Human - Fab light chain
Fab heavy chain 		- 24,25-Epoxy-cholesterol pubchem
small-molecule Agonist - - Qi X, Liu H, Thompson B, McDonald J, Zhang C, Li X 10.1038/S41586-019-1286-0 2019-06-12
Gs αs Human Gs-Gi1 chimera 58 β1 Human γ2 Human Cryo-EM 6PB0 - 3.0 CRFR1 CRF1 Corticotropin-releasing factor B1 (Secretin) Human - Nanobody-35 - Urocortin pubchem
peptide Agonist urocortin 1, corticotrophin-releasing hormone, urocortin 2 peptide Ma S, Shen Q, Zhao LH, Mao C, Zhou XE, Shen DD, de Waal PW, Bi P, Li C, Jiang Y, Wang MW, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE 10.1016/J.MOLCEL.2020.01.013 2020-02-12
Gs αs Human - 89 β1 Human γ2 Human Cryo-EM 6X1A - 2.5 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - danuglipron pubchem gtoplig chembl_ligand
small-molecule Agonist glucagon-like peptide 1-(7-36) amide, glucagon, 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
Gs αs Bovine - 57 β1 Bovine γ2 Bovine Cryo-EM 7D68 - 3.0 GLP2R GLP-2 Glucagon B1 (Secretin) Human - Nanobody-35 - glucagon pubchem gtoplig chembl_ligand drugbank drug_central gtoplig pubchem pubchem pubchem pubchem
peptide Agonist glucagon-like peptide 2-(3-33), glucagon-like peptide 2 peptide Sun W, Chen LN, Zhou Q, Zhao LH, Yang D, Zhang H, Cong Z, Shen DD, Zhao F, Zhou F, Cai X, Chen Y, Zhou Y, Gadgaard S, van der Velden WJC, Zhao S, Jiang Y, Rosenkilde MM, Xu HE, Zhang Y, Wang MW 10.1038/S41422-020-00442-0 2020-12-16
Gi/o 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 desulfated gastrin-14, desulfated cholecystokinin-8, gastrin-34, gastrin-14, CCK-58, desulfated gastrin-17, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8, desulfated gastrin-34, gastrin-71, 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 7VUZ 7VUZ_refined 2.9 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human - scFv16 - PAMP-12 pubchem
peptide Agonist PAMP-20 peptide Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP 10.1038/S41586-021-04077-Y 2021-12-01
Gs αs Human - 50 β1 Human γ2 Human Cryo-EM 7LLY 7LLY_refined 3.3 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Pro-glucagon pubchem
peptide Agonist glucagon-like peptide 1-(7-36) amide, glucagon, 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 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 humanin, aspirin-triggered resolvin D1, LXA4, resolvin D1, serum amyloid A, PrP106-126, 15-deoxy-LXA4, aspirin triggered lipoxin A4, LL-37, LTC4, annexin I, fMet-Leu-Phe, LTD4 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 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 		L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine small-molecule Teng X, Chen S, Nie Y, Xiao P, Yu X, Shao Z, Zheng S 10.1038/S41467-022-30929-W 2022-06-15
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 desulfated gastrin-14, desulfated cholecystokinin-8, gastrin-34, gastrin-14, CCK-58, desulfated gastrin-17, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8, desulfated gastrin-34, gastrin-71, 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 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 - 57 β1 Human γ2 Human Cryo-EM 7XKD - 2.4 AGRG2 ADGRG2 ADGRG B2 (Adhesion) Mouse - Nanobody-35 - PRASTERONE chembl_ligand pubchem
small-molecule Agonist - - - - 2022-08-10
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7VIH 7VIH_refined 3.0 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - icanbelimod pubchem gtoplig chembl_ligand
small-molecule Agonist 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 αo Human - 60 β1 Human γ2 Human Cryo-EM 7Y24 - 3.3 SSR2 SST2 Somatostatin A (Rhodopsin) Human - scFv16 - Octreotide
peptide Agonist SRIF-28, cortistatin-14, CST-17, SRIF-14 peptide Chen S, Teng X, Zheng S 10.1038/S41589-022-01130-3 2022-10-19
Gi/o αi1 Human - 64 β1 Rat γ2 Bovine Cryo-EM 8EFO - 2.8 OPRM μ Opioid A (Rhodopsin) Human - scFv16 - PZM21 pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist [Leu]enkephalin, β-endorphin, dynorphin A, [Met]enkephalin, endomorphin-1, endomorphin-2, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13) 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 Mini-Gs 55 β1 Human γ2 Human Cryo-EM 8F76 8F76_refined 3.1 O51E2 Olfactory 51E2 Olfactory A (Rhodopsin) Human - Nanobody-35 - propanoic acid pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist - - Billesbolle CB, de March CA, van der Velden WJC, Ma N, Tewari J, Del Torrent CL, Li L, Faust B, Vaidehi N, Matsunami H, Manglik A 10.1038/S41586-023-05798-Y 2023-03-22
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8HMV 8HMV_refined 2.9 GPR21 GPR21 A orphans A (Rhodopsin) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Wong TS, Gao W, Chen G, Qiu C, He G, Ye F, Wu Z, Zeng Z, Du Y 10.1002/MCO2.205 2023-03-01
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 7XK2 7XK2_refined 3.1 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - scFv16 - MK 6892 pubchem gtoplig chembl_ligand pubchem
small-molecule Agonist β-D-hydroxybutyric acid, butyric acid small-molecule Yang Y, Kang HJ, Gao R, Wang J, Han GW, DiBerto JF, Wu L, Tong J, Qu L, Wu Y, Pileski R, Li X, Zhang XC, Zhao S, Kenakin T, Wang Q, Stevens RC, Peng W, Roth BL, Rao Z, Liu ZJ 10.1038/S41467-023-37177-6 2023-02-22
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 [Leu]enkephalin, β-neoendorphin, β-endorphin, dynorphin A, [Met]enkephalin, α-neoendorphin, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13), big dynorphin peptide Chen Y, Chen B, Wu T, Zhou F, Xu F 10.1093/PROCEL/PWAC033 2023-05-24
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 8GUR 8GUR_refined 2.8 CNR2 CB2 Cannabinoid A (Rhodopsin) Human - scFv16 - CP55940 pubchem gtoplig chembl_ligand gtoplig
small-molecule Agonist 2-arachidonoylglycerol, anandamide small-molecule Li X, Chang H, Bouma J, de Paus LV, Mukhopadhyay P, Paloczi J, Mustafa M, van der Horst C, Kumar SS, Wu L, Yu Y, van den Berg RJBHN, Janssen APA, Lichtman A, Liu ZJ, Pacher P, van der Stelt M, Heitman LH, Hua T 10.1038/S41467-023-37112-9 2023-05-10
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8J18 - 2.9 GPR84 GPR84 A orphans A (Rhodopsin) Human - scFv16 - (3R)-3-HYDROXYDODECANOIC ACID pubchem
small-molecule Agonist - - Liu H, Zhang Q, He X, Jiang M, Wang S, Yan X, Cheng X, Liu Y, Nan FJ, Xu HE, Xie X, Yin W 10.1038/S41467-023-38985-6 2023-06-21
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8JR9 - 2.6 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - PCO371 pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist TIP39, PTHrP-(1-36), PTHrP, PTH peptide Zhao LH, He Q, Yuan Q, Gu Y, He X, Shan H, Li J, Wang K, Li Y, Hu W, Wu K, Shen J, Xu HE 10.1038/S41586-023-06467-W 2023-08-02
Gs αs Human Gi1-Gs chimera 60 β1 Human γ2 Bovine Cryo-EM 8INR - 2.7 MC5R MC5 Melanocortin A (Rhodopsin) Human - - - INTERMEDINE chembl_ligand pubchem pubchem pubchem
protein Agonist β-MSH, α-MSH, agouti-related protein, γ-MSH, ACTH peptide Chen VB, Arendall WB 3rd, Headd JJ, Keedy DA, Immormino RM, Kapral GJ, Murray LW, Richardson JS, Richardson DC 10.1107/S0907444909042073 2023-09-20
Gs αs Human - 61 β1 Human γ2 Human Cryo-EM 8JLP - 3.2 TAAR1 TA1 Trace amine A (Rhodopsin) Human - - - ralmitaront pubchem gtoplig chembl_ligand
small-molecule Agonist β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, dopamine small-molecule Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z 10.1038/S41586-023-06804-Z 2023-11-15
Gs αs Human - 48 β1 Human γ2 Human Cryo-EM 6E3Y 6E3Y_refined 3.3 CALRL calcitonin-like Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP1 		- Calcitonin gene-related peptide 1 pubchem
peptide Agonist - - Liang YL, Khoshouei M, Deganutti G, Glukhova A, Koole C, Peat TS, Radjainia M, Plitzko JM, Baumeister W, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Wootten D, Sexton PM 10.1038/S41586-018-0535-Y 2018-09-19
Gs αs Human Mini-Gs 61 β1 Human γ2 Human Cryo-EM 6LI3 - 3.3 GPR52 GPR52 A orphans A (Rhodopsin) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Lin X, Li M, Wang N, Wu Y, Luo Z, Guo S, Han GW, Li S, Yue Y, Wei X, Xie X, Chen Y, Zhao S, Wu J, Lei M, Xu F 10.1038/S41586-020-2019-0 2020-02-26
Gs αs Human - 61 β1 Human γ2 Human Cryo-EM 6WZG 6WZG_refined 2.3 SCTR secretin Glucagon B1 (Secretin) Human - Nanobody-35 - SECRETIN chembl_ligand pubchem
protein Agonist VIP, secretin peptide Dong M, Deganutti G, Piper SJ, Liang YL, Khoshouei M, Belousoff MJ, Harikumar KG, Reynolds CA, Glukhova A, Furness SGB, Christopoulos A, Danev R, Wootten D, Sexton PM, Miller LJ 10.1038/S41467-020-17791-4 2020-08-12
Gi/o αi1 Human - 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-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) peptide Cong Z, Chen LN, Ma H, Zhou Q, Zou X, Ye C, Dai A, Liu Q, Huang W, Sun X, Wang X, Xu P, Zhao L, Xia T, Zhong W, Yang D, Eric Xu H, Zhang Y, Wang MW 10.1038/S41467-021-24058-Z 2021-07-07
Gq/11 αq Human - 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-58, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8 peptide Liu Q, Yang D, Zhuang Y, Croll TI, Cai X, Dai A, He X, Duan J, Yin W, Ye C, Zhou F, Wu B, Zhao Q, Xu HE, Wang MW, Jiang Y 10.1038/S41589-021-00841-3 2021-08-25
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 7F53 - 3.0 MC4R MC4 Melanocortin A (Rhodopsin) Human - Nanobody-35 - α-MSH pubchem gtoplig
peptide Agonist β-MSH, α-MSH, agouti-related protein, γ-MSH, ACTH peptide Zhang H, Chen LN, Yang D, Mao C, Shen Q, Feng W, Shen DD, Dai A, Xie S, Zhou Y, Qin J, Sun JP, Scharf DH, Hou T, Zhou T, Wang MW, Zhang Y 10.1038/S41422-021-00552-3 2021-11-03
Gs αs Human Gs-Gi1 chimera 57 β1 Human γ2 Human Cryo-EM 7P02 - 2.9 NK1R NK1 Tachykinin A (Rhodopsin) Human - scFv16 - substance P pubchem gtoplig chembl_ligand gtoplig gtoplig
peptide Agonist neuropeptide-γ, neurokinin A, neuropeptide K, neurokinin B, hemokinin 1, substance P peptide Thom C, Ehrenmann J, Vacca S, Waltenspuhl Y, Schoppe J, Medalia O, Pluckthun A 10.1126/SCIADV.ABK2872 2021-12-15
Gs αs Human - 57 β1 Rat γ2 Bovine Cryo-EM 7V9M 7V9M_refined 3.3 GHRHR GHRH Glucagon B1 (Secretin) Human - Nanobody-35 - Somatoliberin pubchem
peptide Agonist GHRH peptide Cong Z, Zhou F, Zhang C, Zou X, Zhang H, Wang Y, Zhou Q, Cai X, Liu Q, Li J, Shao L, Mao C, Wang X, Wu J, Xia T, Zhao LH, Jiang H, Zhang Y, Xu HE, Cheng X, Yang D, Wang MW 10.1073/PNAS.2106606118 2021-10-20
Gi/o αi1 Mouse - 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 7WVW - 3.1 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human BRIL - - FME-TYR-PHE-ILE-ASN-ILE-LEU-THE-LEU
peptide Agonist humanin, aspirin-triggered resolvin D1, LXA4, resolvin D1, serum amyloid A, PrP106-126, 15-deoxy-LXA4, aspirin triggered lipoxin A4, LL-37, LTC4, annexin I, fMet-Leu-Phe, LTD4 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-A, orexin-B 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
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 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 heavy chain
M22 antibody light chain
protein
protein 		Agonist TSH peptide Faust B, Billesbolle CB, Suomivuori CM, Singh I, Zhang K, Hoppe N, Pinto AFM, Diedrich JK, Muftuoglu Y, Szkudlinski MW, Saghatelian A, Dror RO, Cheng Y, Manglik A 10.1038/S41586-022-05159-1 2022-08-03
Gs αs Human Engineered G protein 50 - - - - X-ray 5G53 - 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
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 Fused partial Gs 44 - - - - X-ray 6E67 - 3.7 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human T4-Lysozyme - - CHEMBL1615159 chembl_ligand pubchem
small-molecule Agonist L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline small-molecule Liu X, Xu X, Hilger D, Aschauer P, Tiemann JKS, Du Y, Liu H, Hirata K, Sun X, Guixa-Gonzalez R, Mathiesen JM, Hildebrand PW, Kobilka BK 10.1016/J.CELL.2019.04.021 2019-06-05
Gs αs Human - 48 β1 Human γ2 Human Cryo-EM 6UUS 6UUS_refined 2.4 CALRL calcitonin-like Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP3 		- Adrenomedullin pubchem
peptide Agonist - - Liang YL, Belousoff MJ, Fletcher MM, Zhang X, Khoshouei M, Deganutti G, Koole C, Furness SGB, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Danev R, Wootten D, Sexton PM 10.1021/ACSPTSCI.9B00080 2020-04-01
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7CFN 7CFN_refined 3.0 GPBAR GPBA Bile acid A (Rhodopsin) Human - Nanobody-35 - INT-777 pubchem
INT-777 pubchem
small-molecule
small-molecule 		Agonist
PAM 		deoxycholic acid, cholic acid, chenodeoxycholic acid, lithocholic acid small-molecule - - 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
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7CRH 7CRH_refined 3.3 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - CHEMBL1416789 chembl_ligand pubchem
small-molecule Agonist L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine small-molecule Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z 10.1016/J.CELL.2021.01.028 2021-03-03
Gs αs Human - 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
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7F1S 7F1S_refined 2.8 CCR5 CCR5 Chemokine A (Rhodopsin) Human - - - Apo (no ligand)
none Apo (no ligand) CCL14, CCL8, CCL13, CCL4, CCL7, CCL2, CCL5, CCL11, CCL3, CCL16 peptide Zhang H, Chen K, Tan Q, Shao Q, Han S, Zhang C, Yi C, Chu X, Zhu Y, Xu Y, Zhao Q, Wu B 10.1038/S41467-021-24438-5 2021-07-14
Gi/o αi1 Human - 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 7EW7 - 3.3 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - scFv16 - SEW2871 pubchem gtoplig chembl_ligand
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 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 - 54 β1 Human γ2 Human Cryo-EM 7W53 - 3.2 NMUR1 NMU1 Neuromedin U A (Rhodopsin) Human - scFv16 - Neuromedin U-25 (human) pubchem
peptide Agonist neuromedin U-23, neuromedin S-36, neuromedin S-33, neuromedin U-25 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 αo Human Mini-Go 60 β1 Human γ2 Human Cryo-EM 7UM7 7UM7_refined 2.8 5HT5A 5-HT5A 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - methylergonovine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist 5-hydroxytryptamine small-molecule Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL 10.1038/S41594-022-00796-6 2022-07-20
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 7XW5 - 3.0 TSHR TSH Glycoprotein hormone A (Rhodopsin) Human - Nanobody-35 - Thyrotropin subunit beta
Glycoprotein hormones alpha 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 2022-08-24
Gi/o αi2 Human - 61 β1 Human γ2 Human Cryo-EM 7XXI 7XXI_refined 3.0 P2Y12 P2Y12 P2Y A (Rhodopsin) Human - - - 2MeSADP pubchem gtoplig chembl_ligand gtoplig
small-molecule Agonist ADP, ATP small-molecule - - 2023-06-07
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 8EJC - 3.0 FFAR1 FFA1 Free fatty acid A (Rhodopsin) Human - scFv16 - fasiglifam pubchem gtoplig chembl_ligand drugbank
small-molecule Agonist myristic acid, oleic acid, α-linolenic acid, docosahexaenoic acid small-molecule Kumari P, Inoue A, Chapman K, Lian P, Rosenbaum DM 10.1073/PNAS.2219569120 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 TIP39, PTHrP-(1-36), PTHrP, PTH peptide Cary BP, Gerrard EJ, Belousoff MJ, Fletcher MM, Jiang Y, Russell IC, Piper SJ, Wootten D, Sexton PM 10.1016/J.STR.2023.04.002 2023-04-26
Gi/o αi1 Human - 60 β1 Human γ2 Human Cryo-EM 8IRU - 3.2 DRD4 D4 Dopamine A (Rhodopsin) Human - scFv16 - rotigotine pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist dopamine small-molecule Xu P, Huang S, Krumm BE, Zhuang Y, Mao C, Zhang Y, Wang Y, Huang XP, Liu YF, He X, Li H, Yin W, Jiang Y, Zhang Y, Roth BL, Xu HE 10.1038/S41422-023-00808-0 2023-06-21
Gq/11 αq Human GRK2 bound 88 - - - - Cryo-EM 8JPB - 3.1 NTR1 NTS1 Neurotensin A (Rhodopsin) Human - GRK2 GRK2 JMV431 gtoplig chembl_ligand pubchem
CHEMBL4576388 chembl_ligand pubchem
peptide
small-molecule 		Agonist
PAM 		large neurotensin, large neuromedin N, neurotensin, 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
Gi/o αo Human - 58 β1 Human γ2 Human Cryo-EM 8HPT - 3.4 C5AR1 C5a1 Complement peptide A (Rhodopsin) Mouse - scFv16 - C5a
peptide Agonist - - None HTTPS://DOI.ORG/10.1016/J.CELL.2023.09.020 2023-10-18
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8IJB 8IJB_refined 3.2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - scFv16 - 5-Methyl-4-oxidanyl-pyrazin-4-ium-2-carboxylic acid pubchem
small-molecule Agonist β-D-hydroxybutyric acid, butyric acid small-molecule Pan X, Ye F, Ning P, Zhang Z, Li X, Zhang B, Wang Q, Chen G, Gao W, Qiu C, Wu Z, Li J, Zhu L, Xia J, Gong K, Du Y 10.1038/S41421-023-00610-7 2024-01-03
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 8KGK 8KGK_refined 3.2 GPR61 GPR61 A orphans A (Rhodopsin) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Nie Y, Qiu Z, Chen S, Chen Z, Song X, Ma Y, Huang N, Cyster JG, Zheng S 10.1038/S41467-023-41654-3 2023-10-11
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8W8B - 3.0 5HT1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL scFv16 - ulotaront pubchem gtoplig drugbank chembl_ligand
small-molecule Agonist 5-hydroxytryptamine small-molecule Liu H, Zheng Y, Wang Y, Wang Y, He X, Xu P, Huang S, Yuan Q, Zhang X, Wang L, Jiang K, Chen H, Li Z, Liu W, Wang S, Xu HE, Xu F 10.1038/S41586-023-06775-1 2023-11-22
Gs αs Bovine - 58 β1 Rat γ2 Bovine Cryo-EM 6NBF - 3.0 PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - Long-acting parathyroid hormone analog
peptide Agonist TIP39, PTHrP-(1-36), PTHrP, PTH peptide Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y 10.1126/SCIENCE.AAV7942 2019-04-17
Gi/o 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 7C2E - 4.2 GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - 2-[[4-[6-[(4-cyano-2-fluoranyl-phenyl)methoxy]pyridin-2-yl]-3,6-dihydro-2~{H}-pyridin-1-yl]methyl]-3-[[(2~{S})-oxetan-2-yl]methyl]imidazo[4,5-b]pyridine-5-carboxylic acid pubchem
small-molecule Agonist glucagon-like peptide 1-(7-36) amide, glucagon, 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 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-A, orexin-B peptide Hong C, Byrne NJ, Zamlynny B, Tummala S, Xiao L, Shipman JM, Partridge AT, Minnick C, Breslin MJ, Rudd MT, Stachel SJ, Rada VL, Kern JC, Armacost KA, Hollingsworth SA, O'Brien JA, Hall DL, McDonald TP, Strickland C, Brooun A, Soisson SM, Hollenstein K 10.1038/S41467-021-21087-6 2021-02-10
Gs αs Human - 86 β1 Human γ2 Human X-ray 7JOZ 7JOZ_refined 3.8 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - CHEMBL4453318 chembl_ligand pubchem
small-molecule Agonist L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine small-molecule Sun B, Feng D, Chu ML, Fish I, Lovera S, Sands ZA, Kelm S, Valade A, Wood M, Ceska T, Kobilka TS, Lebon F, Kobilka BK 10.1038/S41467-021-23519-9 2021-04-14
Gi/o αi1 Human - 58 β1 Human γ2 Human Cryo-EM 7MTS - 3.2 GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human - - - 2-methoxy-6-propyl-N-(2-{4-[(1H-tetrazol-5-yl)methoxy]phenyl}ethyl)thieno[2,3-d]pyrimidin-4-amine pubchem
L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem
small-molecule
small-molecule 		Ago-PAM
Agonist 		L-glutamic acid small-molecule Seven AB, Barros-Alvarez X, de Lapeyriere M, Papasergi-Scott MM, Robertson MJ, Zhang C, Nwokonko RM, Gao Y, Meyerowitz JG, Rocher JP, Schelshorn D, Kobilka BK, Mathiesen JM, Skiniotis G 10.1038/S41586-021-03680-3 2021-07-07
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7S8O - 2.6 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human BRIL scFv16 - (R)-ZINC-3573 pubchem gtoplig chembl_ligand
small-molecule Agonist PAMP-20 peptide Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL 10.1038/S41586-021-04126-6 2021-11-17
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7VUG 7VUG_refined 3.2 GP139 GPR139 A orphans A (Rhodopsin) Human - scFv16 Xylanase JNJ-63533054 pubchem gtoplig chembl_ligand
small-molecule Agonist L-phenylalanine, L-tryptophan small-molecule Zhou Y, Daver H, Trapkov B, Wu L, Wu M, Harpsoe K, Gentry PR, Liu K, Larionova M, Liu J, Chen N, Brauner-Osborne H, Gloriam DE, Hua T, Liu ZJ 10.1038/S41422-021-00591-W 2021-12-29
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 7F4H - 2.7 MSHR MC1 Melanocortin A (Rhodopsin) Human - Nanobody-35
scFv16 		- CHEMBL407070 chembl_ligand pubchem pubchem
protein Agonist β-MSH, ACTH, γ-MSH, α-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
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 adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP peptide Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM 10.1126/SCIENCE.ABM9609 2022-03-23
Gs αs Human Mini-Gs 54 β1 Human γ2 Human Cryo-EM 7WU3 - 3.1 AGRF1 ADGRF1 ADGRF B2 (Adhesion) Human - Nanobody-35 - Apo (no ligand)
none Apo (no ligand) - - Qu X, Qiu N, Wang M, Zhang B, Du J, Zhong Z, Xu W, Chu X, Ma L, Yi C, Han S, Shui W, Zhao Q, Wu B 10.1038/S41586-022-04580-W 2022-04-27
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7EUO 7EUO_refined 2.9 FPR1 FPR1 Formylpeptide A (Rhodopsin) Human - scFv16 - Peptide Agonist fMLF
peptide Agonist 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 2022-05-25
Gi/o αo Human Mini-Go 60 β1 Human γ2 Human Cryo-EM 7UM6 - 2.8 5HT5A 5-HT5A 5-Hydroxytryptamine A (Rhodopsin) Human - scFv16 - lisuride pubchem gtoplig chembl_ligand drugbank drug_central
small-molecule Agonist 5-hydroxytryptamine small-molecule Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL 10.1038/S41594-022-00796-6 2022-07-20
Gq/11 αq Human Mini-Gq 57 β1 Human γ2 Human Cryo-EM 8E9Z - 2.7 ACM3 M3 Acetylcholine (muscarinic) A (Rhodopsin) Human - scFv16 - iperoxo pubchem gtoplig chembl_ligand
small-molecule Agonist acetylcholine small-molecule Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL 10.1038/S41586-022-05489-0 2022-11-30
Gi/o αi2 Human - 59 β1 Human γ2 Bovine Cryo-EM 7YK6 7YK6_refined 3.0 RL3R2 RXFP4 Relaxin family peptide A (Rhodopsin) Human - scFv16 - CHEMBL4522365 chembl_ligand pubchem
small-molecule Agonist INSL5, relaxin-3 (B chain), relaxin-3 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 8ID8 - 3.0 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - scFv16 - TUG-891 pubchem gtoplig chembl_ligand
small-molecule Agonist myristic acid, linoleic acid, α-linolenic acid, oleic acid small-molecule Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP 10.1126/SCIENCE.ADD6220 2023-03-15
Gq/11 αq Human Gs-mini-Gq chimera 52 β1 Human γ2 Human Cryo-EM 8G2Y - 3.4 AGRF1 ADGRF1 ADGRF B2 (Adhesion) Human - Nanobody-35 - [1-Myristoyl-glycerol-3-YL]phosphonylcholine pubchem
small-molecule Agonist - - Jones DTD, Dates AN, Rawson SD, Burruss MM, Lipper CH, Blacklow SC 10.1038/S41467-023-38083-7 2023-05-10
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7YAE 7YAE_refined 3.4 SSR2 SST2 Somatostatin A (Rhodopsin) Human - scFv16 - Octreotide
peptide Agonist SRIF-28, cortistatin-14, CST-17, 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
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
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 adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP peptide Cao J, Belousoff MJ, Gerrard E, Danev R, Fletcher MM, Dal Maso E, Schreuder H, Lorenz K, Evers A, Tiwari G, Besenius M, Li Z, Johnson RM, Wootten D, Sexton PM 10.1038/S41589-023-01393-4 2023-08-02
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 8GDB 8GDB_refined 3.1 PE2R4 EP4 Prostanoid A (Rhodopsin) Human - - - PGE2 pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
small-molecule Agonist thromboxane A2, PGF2α, PGI2, PGD2, PGE1, PGE2 small-molecule Huang SM, Xiong MY, Liu L, Mu J, Wang MW, Jia YL, Cai K, Tie L, Zhang C, Cao S, Wen X, Wang JL, Guo SC, Li Y, Qu CX, He QT, Cai BY, Xue C, Gan S, Xie Y, Cong X, Yang Z, Kong W, Li S, Li Z, Xiao P, Yang F, Yu X, Guan YF, Zhang X, Liu Z, Yang BX, Du Y, Sun JP 10.1073/PNAS.2216329120 2024-01-10
Gi/o αo Human - 59 β1 Human γ2 Human Cryo-EM 8I9L - 3.2 C3AR C3a Complement peptide A (Rhodopsin) Human - scFv16 - C3a anaphylatoxin pubchem
peptide Agonist C5a, C3a peptide Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C 10.1016/J.CELL.2023.09.020 2023-10-18
Gi/o αi1 Human - 65 β1 Human γ2 Human Cryo-EM 6LFO 6LFO_refined