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G PROTEIN
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STRUCTURE
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RECEPTOR
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OTHER PROTEINS
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STRUCTURE LIGAND
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PHYSIOLOGICAL LIGAND
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REFERENCE
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Fam. | α | Species | Note | % of Seq | β | Species | γ | Species | Method |
PDB
|
Refined structure |
Resolution |
UniProt
|
IUPHAR | Receptor family | Class | Species | Receptor fusion | Antibodies | Other | Name | Type | Function | Name | Type | Authors | Reference | PDB Date | ||
Gi/o | αt1 | Bovine | Only H5 | 3 | - | - | - | - | X-ray | 3DQB | 3DQB_refined | 3.2 | OPSD | Rhodopsin | Opsins | A (Rhodopsin) | Bovine | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Scheerer P, Park JH, Hildebrand PW, Kim YJ, Krauss N, Choe HW, Hofmann KP, Ernst OP | 10.1038/NATURE07330 | 2008-09-23 | 55465 | |
Gi/o | αt1 | Bovine | Only H5 | 3 | - | - | - | - | X-ray | 3PQR | 3PQR_refined | 2.9 | OPSD | Rhodopsin | Opsins | A (Rhodopsin) | Bovine | - | - | - |
Retinal (all-trans)
pubchem
|
small-molecule | Agonist | - | - | Choe HW, Kim YJ, Park JH, Morizumi T, Pai EF, Krauss N, Hofmann KP, Scheerer P, Ernst OP | 10.1038/NATURE09789 | 2011-03-09 | 55465 | |
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 | 55465 | |
Gs | αs | Bovine | - | 89 | β1 | Rat | γ2 | Bovine | X-ray | 3SN6 | - | 3.2 | ADRB2 | β2 | Adrenoceptors | A (Rhodopsin) | Human | T4-Lysozyme | Antibody | - |
CHEMBL1615159
chembl_ligand
pubchem
|
small-molecule | Agonist | (-)-adrenaline, Zn2+, L-NOREPINEPHRINE, noradrenaline, (-)-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 | 55370 | |
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 | 55465 | |
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 2/intermedin, amylin, β-CGRP, α-CGRP, calcitonin, adrenomedullin | 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 | 55353 | |
Gi/o | αt1 | Bovine | Only H5 | 3 | - | - | - | - | X-ray | 5WKT | 5WKT_refined | 3.2 | OPSD | Rhodopsin | Opsins | A (Rhodopsin) | Bovine | - | - | - |
B-Octylglucoside
pubchem
|
small-molecule | unknown | - | - | Broecker J, Morizumi T, Ou WL, Klingel V, Kuo A, Kissick DJ, Ishchenko A, Lee MY, Xu S, Makarov O, Cherezov V, Ogata CM, Ernst OP | 10.1038/NPROT.2017.135 | 2017-12-13 | 55465 | |
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 | 55355 | |
Gi/o | αi1 | Human | - | 100 | β1 | Rat | γ2 | Bovine | Cryo-EM | 6CMO | 6CMO_refined | 4.5 | OPSD | Rhodopsin | Opsins | A (Rhodopsin) | Human | BRIL | Fab | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Kang Y, Kuybeda O, de Waal PW, Mukherjee S, Van Eps N, Dutka P, Zhou XE, Bartesaghi A, Erramilli S, Morizumi T, Gu X, Yin Y, Liu P, Jiang Y, Meng X, Zhao G, Melcher K, Ernst OP, Kossiakoff AA, Subramaniam S, Xu HE | 10.1038/S41586-018-0215-Y | 2018-06-20 | 55355 | |
Gi/o | αo | Human | Mini-Go | 51 | - | - | - | - | X-ray | 6FUF | 6FUF_refined | 3.1 | OPSD | Rhodopsin | Opsins | A (Rhodopsin) | Bovine | - | - | - |
Retinal (all-trans)
pubchem
|
small-molecule | Agonist | - | - | Tsai CJ, Pamula F, Nehme R, Muhle J, Weinert T, Flock T, Nogly P, Edwards PC, Carpenter B, Gruhl T, Ma P, Deupi X, Standfuss J, Tate CG, Schertler GFX | 10.1126/SCIADV.AAT7052 | 2018-10-03 | 55361 | |
Gs | αs | Human | - | 56 | β1 | Human | γ2 | Human | Cryo-EM | 6WPW | 6WPW_refined | 3.1 | GLR | glucagon | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
Glucagon derivative ZP3780
|
peptide | Agonist | glucagon | peptide | Hilger D, Kumar KK, Hu H, Pedersen MF, O'Brien ES, Giehm L, Jennings C, Eskici G, Inoue A, Lerch M, Mathiesen JM, Skiniotis G, Kobilka BK | 10.1126/SCIENCE.ABA3373 | 2020-08-12 | 55353 | |
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 | PACAP-27, PACAP-38, GHRH, VIP, PHM, PHI, secretin | 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 | 55353 | |
Gs | αs | Human | - | 90 | β1 | Human | γ2 | Human | Cryo-EM | 6X18 | - | 2.1 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
CHEMBL410972
chembl_ligand
pubchem
pubchem
|
protein | Agonist | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, Senel P, Stewart GD, Liang YL, Glukhova A, Venugopal H, Christopoulos A, Furness SGB, Miller LJ, Reedtz-Runge S, Langmead CJ, Gloriam DE, Danev R, Sexton PM, Wootten D | 10.1016/J.MOLCEL.2020.09.020 | 2020-09-09 | 55353 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 6XBL | - | 3.9 | SMO | SMO | Frizzled | F (Frizzled) | Human | - | scFv16 | - |
Cholesterol
pubchem
SAG1.3 pubchem gtoplig chembl_ligand |
small-molecule small-molecule |
Agonist PAM |
- | - | Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X | 10.1038/S41589-020-0646-2 | 2020-09-30 | 55355 | |
Gs | αs | Human | - | 56 | β1 | Human | γ2 | Human | Cryo-EM | 6XOX | - | 3.1 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - |
scFv16 Nanobody-35 |
- |
orforglipron
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | Kawai T, Sun B, Yoshino H, Feng D, Suzuki Y, Fukazawa M, Nagao S, Wainscott DB, Showalter AD, Droz BA, Kobilka TS, Coghlan MP, Willard FS, Kawabe Y, Kobilka BK, Sloop KW | 10.1073/PNAS.2014879117 | 2020-11-18 | 55353 | |
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, glucagon-like peptide 2-(3-33) | peptide | Sun W, Chen LN, Zhou Q, Zhao LH, Yang D, Zhang H, Cong Z, Shen DD, Zhao F, Zhou F, Cai X, Chen Y, Zhou Y, Gadgaard S, van der Velden WJC, Zhao S, Jiang Y, Rosenkilde MM, Xu HE, Zhang Y, Wang MW | 10.1038/S41422-020-00442-0 | 2020-12-16 | 55370 | |
Gi/o | αi1 | Human | Non-canonical conformation | 63 | β1 | Human | γT1 | Human | Cryo-EM | 7L0R | - | 4.2 | NTR1 | NTS1 | Neurotensin | A (Rhodopsin) | Rat | - | - | - |
neurotensin
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
|
peptide | Agonist | neuromedin N, neurotensin | peptide | Zhang M, Gui M, Wang ZF, Gorgulla C, Yu JJ, Wu H, Sun ZJ, Klenk C, Merklinger L, Morstein L, Hagn F, Pluckthun A, Brown A, Nasr ML, Wagner G | 10.1038/S41594-020-00554-6 | 2021-01-06 | 55355 | |
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 | 55361 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7JV5 | - | 3.0 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
CHEMBL1160787
chembl_ligand
pubchem
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine, dopamine, (-)-noradrenaline | small-molecule | Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP, Shen DD, Xu T, Liu YF, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE | 10.1016/J.CELL.2021.01.027 | 2021-02-24 | 55353 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7CKX | - | 3.5 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
A77636
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine, dopamine, (-)-noradrenaline | small-molecule | Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z | 10.1016/J.CELL.2021.01.028 | 2021-03-03 | 55353 | |
Gs | αs | Human | Engineered G alpha | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7LJC | - | 3.0 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
CHEMBL1160787
chembl_ligand
pubchem
mevidalen pubchem gtoplig chembl_ligand drugbank |
small-molecule small-molecule |
Agonist PAM |
L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine, dopamine, (-)-noradrenaline | small-molecule | Zhuang Y, Krumm B, Zhang H, Zhou XE, Wang Y, Huang XP, Liu Y, Cheng X, Jiang Y, Jiang H, Zhang C, Yi W, Roth BL, Zhang Y, Xu HE | 10.1038/S41422-021-00482-0 | 2021-03-03 | 55353 | |
Gq/11 | αq | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7DFL | - | 3.3 | HRH1 | H1 | Histamine | A (Rhodopsin) | Human | - | scFv16 | - |
histamine
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
gtoplig
|
small-molecule | Agonist | histamine | small-molecule | Xia R, Wang N, Xu Z, Lu Y, Song J, Zhang A, Guo C, He Y | 10.1038/S41467-021-22427-2 | 2021-03-31 | 55363 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7E2Y | - | 3.0 | 5HT1A | 5-HT1A | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | - | - |
5-hydroxytryptamine
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen DD, Yen HY, Robinson CV, Harpsoe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE | 10.1038/S41586-021-03376-8 | 2021-04-14 | 55355 | |
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 | 55355 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7KH0 | - | 2.8 | V2R | V2 | Vasopressin and oxytocin | A (Rhodopsin) | Human | - |
scFv16 Nanobody-35 |
- |
vasopressin
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
peptide | Agonist | vasopressin, oxytocin | peptide | Wang L, Xu J, Cao S, Sun D, Liu H, Lu Q, Liu Z, Du Y, Zhang C | 10.1038/S41422-021-00483-Z | 2021-05-26 | 55353 | |
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 | 55353 | |
Gi/o | αi3 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7E9H | - | 4.0 | GRM4 | mGlu4 | Metabotropic glutamate | C (Glutamate) | Human | - | scFv16 | - |
L-serine-O-phosphate
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
|
small-molecule | Agonist | L-serine-O-phosphate, 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 | 55357 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7F1R | - | 3.0 | CCR5 | CCR5 | Chemokine | A (Rhodopsin) | Human | - | - | - |
CCL5
gtoplig
|
peptide | Agonist | CCL8, CCL3, CCL7, CCL14, CCL11, CCL4, CCL2, CCL13, CCL5, CCL16 | peptide | - | - | 2021-07-14 | 55355 | |
Gs | αs | Human | - | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7DW9 | - | 2.6 | V2R | V2 | Vasopressin and oxytocin | A (Rhodopsin) | Human | - |
Nanobody-35 scFv16 |
- |
vasopressin
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
peptide | Agonist | vasopressin, oxytocin | peptide | Zhou F, Ye C, Ma X, Yin W, Croll TI, Zhou Q, He X, Zhang X, Yang D, Wang P, Xu HE, Wang MW, Jiang Y | 10.1038/S41422-021-00480-2 | 2021-07-21 | 55353 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7EXD | 7EXD_refined | 3.4 | 5HT1F | 5-HT1F | 5-Hydroxytryptamine | A (Rhodopsin) | Human | BRIL | scFv16 | - |
lasmiditan
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Huang S, Xu P, Tan Y, You C, Zhang Y, Jiang Y, Xu HE | 10.1038/S41422-021-00527-4 | 2021-08-04 | 55355 | |
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, glucagon-like peptide 1-(7-36) amide, 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 | 55353 | |
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 | 55355 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7EZH | - | 3.2 | CCKAR | CCK1 | Cholecystokinin | A (Rhodopsin) | Human | - | scFv16 | - |
CCK-8
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
peptide | Agonist | CCK-33, CCK-4, gastrin-17, CCK-39, desulfated cholecystokinin-8, CCK-8, CCK-58 | 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 | 55355 | |
Gs | αs | Human | - | 59 | β1 | Rat | γ2 | Bovine | Cryo-EM | 5VAI | - | 4.1 | G1SGD4 | GLP-1 | Glucagon | B1 (Secretin) | Rabbit | - | - | - |
CHEMBL410972
chembl_ligand
pubchem
pubchem
|
protein | Agonist | - | - | Zhang Y, Sun B, Feng D, Hu H, Chu M, Qu Q, Tarrasch JT, Li S, Sun Kobilka T, Kobilka BK, Skiniotis G | 10.1038/NATURE22394 | 2017-05-24 | 55353 | |
Gs | αs | Human | - | 49 | β1 | Human | γ2 | Human | Cryo-EM | 6B3J | - | 3.3 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | - | - |
Exendin-P5
|
peptide | Agonist | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | Liang YL, Khoshouei M, Glukhova A, Furness SGB, Zhao P, Clydesdale L, Koole C, Truong TT, Thal DM, Lei S, Radjainia M, Danev R, Baumeister W, Wang MW, Miller LJ, Christopoulos A, Sexton PM, Wootten D | 10.1038/NATURE25773 | 2018-02-21 | 55353 | |
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 | 55353 | |
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 | 55355 | |
Gi/o | αi2 | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 6D9H | 6D9H_refined | 3.6 | AA1R | A1 | Adenosine | A (Rhodopsin) | Human | - | - | - |
adenosine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | adenosine | small-molecule | Draper-Joyce CJ, Khoshouei M, Thal DM, Liang YL, Nguyen ATN, Furness SGB, Venugopal H, Baltos JA, Plitzko JM, Danev R, Baumeister W, May LT, Wootten D, Sexton PM, Glukhova A, Christopoulos A | 10.1038/S41586-018-0236-6 | 2018-06-20 | 55356 | |
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 | 55353 | |
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 2/intermedin, amylin, β-CGRP, α-CGRP, calcitonin, adrenomedullin | 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 | 55353 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 6N4B | 6N4B_refined | 3.0 | CNR1 | CB1 | Cannabinoid | A (Rhodopsin) | Human | - | scFv16 | - |
MDMB-Fubinaca
pubchem
gtoplig
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | Krishna Kumar K, Shalev-Benami M, Robertson MJ, Hu H, Banister SD, Hollingsworth SA, Latorraca NR, Kato HE, Hilger D, Maeda S, Weis WI, Farrens DL, Dror RO, Malhotra SV, Kobilka BK, Skiniotis G | 10.1016/J.CELL.2018.11.040 | 2019-01-30 | 55355 | |
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 | PTH, PTHrP-(1-36), TIP39, PTHrP | peptide | Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y | 10.1126/SCIENCE.AAV7942 | 2019-04-17 | 55370 | |
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 | PTH, PTHrP-(1-36), TIP39, PTHrP | peptide | Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y | 10.1126/SCIENCE.AAV7942 | 2019-04-17 | 55370 | |
Gq/11 | α11 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 6OIJ | 6OIJ_refined | 3.3 | ACM1 | M1 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | Antibody fragment | - |
iperoxo
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | acetylcholine | small-molecule | Maeda S, Qu Q, Robertson MJ, Skiniotis G, Kobilka BK | 10.1126/SCIENCE.AAW5188 | 2019-05-08 | 55364 | |
Gs | αs | Human | Fused partial Gs | 44 | - | - | - | - | X-ray | 6E67 | 6E67_refined | 3.7 | ADRB2 | β2 | Adrenoceptors | A (Rhodopsin) | Human | T4-Lysozyme | - | - |
CHEMBL1615159
chembl_ligand
pubchem
|
small-molecule | Agonist | (-)-adrenaline, Zn2+, L-NOREPINEPHRINE, noradrenaline, (-)-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 | 55353 | |
Gi/o | αi1 | Human | Non-canonical conformation | 62 | β1 | Human | γ2 | Human | Cryo-EM | 6OSA | - | 3.0 | NTR1 | NTS1 | Neurotensin | A (Rhodopsin) | Human | - | - | - |
JMV449
pubchem
gtoplig
chembl_ligand
|
peptide | Agonist | neuromedin N, large neurotensin, neurotensin, large 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 | 55355 | |
Gi/o | αt1 | Bovine | - | 59 | β1 | Bovine | γT1 | Bovine | Cryo-EM | 6OYA | - | 3.3 | OPSD | Rhodopsin | Opsins | A (Rhodopsin) | Bovine | - | Camelid antibody VHH fragment | - |
Retinal (all-trans)
pubchem
|
small-molecule | Agonist | - | - | - | - | 2019-07-24 | 55465 | |
Gs | αs | Human | - | 49 | β1 | Human | γ2 | Human | Cryo-EM | 6P9X | - | 2.9 | CRFR1 | CRF1 | Corticotropin-releasing factor | B1 (Secretin) | Human | - | Nanobody-35 | - |
Corticoliberin
pubchem
|
peptide | Agonist | corticotrophin-releasing hormone, urocortin 2, urocortin 1 | 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 | 55353 | |
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 | PACAP-27, PACAP-38, VIP, PHV, PHM, PHI | 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 | 55353 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 6KPF | 6KPF_refined | 2.9 | CNR2 | CB2 | Cannabinoid | A (Rhodopsin) | Human | - | scFv16 | - |
AM12033
pubchem
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | Hua T, Li X, Wu L, Iliopoulos-Tsoutsouvas C, Wang Y, Wu M, Shen L, Brust CA, Nikas SP, Song F, Song X, Yuan S, Sun Q, Wu Y, Jiang S, Grim TW, Benchama O, Stahl EL, Zvonok N, Zhao S, Bohn LM, Makriyannis A, Liu ZJ | 10.1016/J.CELL.2020.01.008 | 2020-02-12 | 55355 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 6PB1 | 6PB1_refined | 2.8 | CRFR2 | CRF2 | Corticotropin-releasing factor | B1 (Secretin) | Human | - | Nanobody-35 | - |
Urocortin
pubchem
|
peptide | Agonist | corticotrophin-releasing hormone, urocortin 2, urocortin 3, urocortin 1 | peptide | Ma S, Shen Q, Zhao LH, Mao C, Zhou XE, Shen DD, de Waal PW, Bi P, Li C, Jiang Y, Wang MW, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE | 10.1016/J.MOLCEL.2020.01.013 | 2020-02-12 | 55353 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 6OMM | 6OMM_refined | 3.2 | FPR2 | FPR2/ALX | Formylpeptide | A (Rhodopsin) | Human | - | - | - |
CHEMBL552527
chembl_ligand
pubchem
|
protein | Agonist | serum amyloid A, aspirin triggered lipoxin A4, humanin, resolvin D1, LL-37, PrP106-126, annexin I, LXA4, aspirin-triggered resolvin D1 | peptide | Zhuang Y, Liu H, Edward Zhou X, Kumar Verma R, de Waal PW, Jang W, Xu TH, Wang L, Meng X, Zhao G, Kang Y, Melcher K, Fan H, Lambert NA, Eric Xu H, Zhang C | 10.1038/S41467-020-14728-9 | 2020-02-26 | 55355 | |
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 | 55465 | |
Gi/o | αgust | Bovine | Only H5 | 3 | - | - | - | - | X-ray | 5EN0 | 5EN0_refined | 2.8 | OPSD | Rhodopsin | Opsins | A (Rhodopsin) | Bovine | - | - | - |
Retinal (all-trans)
pubchem
|
small-molecule | Agonist | - | - | Singhal A, Guo Y, Matkovic M, Schertler G, Deupi X, Yan EC, Standfuss J | 10.15252/EMBR.201642671 | 2016-08-10 | 55509 | |
Gi/o | αo | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 6G79 | - | 3.8 | 5HT1B | 5-HT1B | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | - | - |
donitriptan
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | tryptamine, 5-hydroxytryptamine, 5-HT-moduline | small-molecule | Garcia-Nafria J, Nehme R, Edwards PC, Tate CG | 10.1038/S41586-018-0241-9 | 2018-06-20 | 55361 | |
Gs | αs | Human | - | 49 | β1 | Human | γ2 | Human | Cryo-EM | 6WI9 | 6WI9_refined | 4.3 | SCTR | secretin | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
SECRETIN
chembl_ligand
pubchem
drugbank
|
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 | 55353 | |
Gs | αs | Human | - | 49 | β1 | Human | γ2 | Human | Cryo-EM | 7C2E | - | 4.2 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
2-[[4-[6-[(4-cyano-2-fluoranyl-phenyl)methoxy]pyridin-2-yl]-3,6-dihydro-2~{H}-pyridin-1-yl]methyl]-3-[[(2~{S})-oxetan-2-yl]methyl]imidazo[4,5-b]pyridine-5-carboxylic acid
pubchem
|
small-molecule | Agonist | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | Ma H, Huang W, Wang X, Zhao L, Jiang Y, Liu F, Guo W, Sun X, Zhong W, Yuan D, Xu HE | 10.1038/S41422-020-0384-8 | 2020-08-26 | 55353 | |
Gs | αs | Human | - | 57 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7BW0 | 7BW0_refined | 3.9 | GPBAR | GPBA | Bile acid | A (Rhodopsin) | Human | BRIL | Nanobody-35 | - | - | - | - | cholic acid, lithocholic acid, chenodeoxycholic acid, deoxycholic acid | small-molecule | Chen G, Wang X, Ge Y, Ma L, Chen Q, Liu H, Du Y, Ye RD, Hu H, Ren R | 10.1038/S41392-020-00262-Z | 2020-09-02 | 55353 | |
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 | 55370 | |
Gs | αs | Human | - | 89 | β1 | Human | γ2 | Human | Cryo-EM | 6X19 | - | 2.1 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
CHU-128
pubchem
|
small-molecule | Agonist | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, Senel P, Stewart GD, Liang YL, Glukhova A, Venugopal H, Christopoulos A, Furness SGB, Miller LJ, Reedtz-Runge S, Langmead CJ, Gloriam DE, Danev R, Sexton PM, Wootten D | 10.1016/J.MOLCEL.2020.09.020 | 2020-09-09 | 55353 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7CFN | 7CFN_refined | 3.0 | GPBAR | GPBA | Bile acid | A (Rhodopsin) | Human | - | Nanobody-35 | - |
INT-777
pubchem
INT-777 pubchem |
small-molecule small-molecule |
Agonist PAM |
cholic acid, lithocholic acid, chenodeoxycholic acid, deoxycholic acid | small-molecule | Yang F, Mao C, Guo L, Lin J, Ming Q, Xiao P, Wu X, Shen Q, Guo S, Shen DD, Lu R, Zhang L, Huang S, Ping Y, Zhang C, Ma C, Zhang K, Liang X, Shen Y, Nan F, Yi F, Luca VC, Zhou J, Jiang C, Sun JP, Xie X, Yu X, Zhang Y | 10.1038/S41586-020-2569-1 | 2020-09-09 | 55353 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 6XBK | - | 3.2 | SMO | SMO | Frizzled | F (Frizzled) | Human | - | scFv16 | - |
Cholesterol
pubchem
|
small-molecule | Agonist | - | - | Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X | 10.1038/S41589-020-0646-2 | 2020-09-30 | 55355 | |
Gs | αs | Human | - | 58 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7D3S | 7D3S_refined | 2.9 | SCTR | secretin | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
SECRETIN
chembl_ligand
pubchem
drugbank
|
protein | Agonist | VIP, secretin | peptide | Fukuhara S, Kobayashi K, Kusakizako T, Iida W, Kato M, Shihoya W, Nureki O | 10.1016/J.BBRC.2020.08.042 | 2020-11-04 | 55353 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7D7M | 7D7M_refined | 3.3 | PE2R4 | EP4 | Prostanoid | A (Rhodopsin) | Human | - | Nanobody-35 | - |
PGE2
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
|
small-molecule | Agonist | thromboxane A2, PGD2, PGE1, PGE2, PGI2, PGF2α | 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 | 55353 | |
Gs | αs | Human | - | 55 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7DHI | - | 3.3 | ADRB2 | β2 | Adrenoceptors | A (Rhodopsin) | Human | - | Nanobody-35 | - |
levosalbutamol
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
small-molecule | Agonist | (-)-adrenaline, Zn2+, L-NOREPINEPHRINE, noradrenaline, (-)-noradrenaline | small-molecule | Yang F, Ling S, Zhou Y, Zhang Y, Lv P, Liu S, Fang W, Sun W, Hu LA, Zhang L, Shi P, Tian C | 10.1093/NSR/NWAA284 | 2020-12-16 | 55353 | |
Gi/o | αi1 | Human | Non-canonical conformation | 95 | β1 | Human | γT1 | Human | Cryo-EM | 7L0S | - | 4.5 | NTR1 | NTS1 | Neurotensin | A (Rhodopsin) | Rat | - | - | - |
neurotensin
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
|
peptide | Agonist | neuromedin N, neurotensin | peptide | Zhang M, Gui M, Wang ZF, Gorgulla C, Yu JJ, Wu H, Sun ZJ, Klenk C, Merklinger L, Morstein L, Hagn F, Pluckthun A, Brown A, Nasr ML, Wagner G | 10.1038/S41594-020-00554-6 | 2021-01-06 | 55355 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7JVP | - | 2.9 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
39YLC3L0ZU
pubchem
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine, dopamine, (-)-noradrenaline | small-molecule | Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP, Shen DD, Xu T, Liu YF, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE | 10.1016/J.CELL.2021.01.027 | 2021-02-24 | 55353 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7CKW | 7CKW_refined | 3.2 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
fenoldopam
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
gtoplig
chembl_ligand
pubchem
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine, dopamine, (-)-noradrenaline | small-molecule | Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z | 10.1016/J.CELL.2021.01.028 | 2021-03-03 | 55353 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7CRH | 7CRH_refined | 3.3 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
CHEMBL1416789
chembl_ligand
pubchem
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine, dopamine, (-)-noradrenaline | small-molecule | Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z | 10.1016/J.CELL.2021.01.028 | 2021-03-03 | 55353 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7CMV | - | 2.7 | DRD3 | D3 | Dopamine | A (Rhodopsin) | Human | BRIL | scFv16 | - |
CHEMBL70565
chembl_ligand
chembl_ligand
pubchem
|
small-molecule | Agonist | dopamine | small-molecule | - | - | 2021-03-10 | 55355 | |
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 | 55355 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7CX2 | - | 2.8 | PE2R2 | EP2 | Prostanoid | A (Rhodopsin) | Human | - | Nanobody-35 | - |
PGE2
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
|
small-molecule | Agonist | thromboxane A2, PGD2, PGE1, PGE2, PGI2, PGF2α | small-molecule | Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y | 10.1126/SCIADV.ABF1268 | 2021-05-05 | 55353 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7CX4 | 7CX4_refined | 2.9 | PE2R2 | EP2 | Prostanoid | A (Rhodopsin) | Human | - | Nanobody-35 | - |
evatanepag
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | thromboxane A2, PGD2, PGE1, PGE2, PGI2, PGF2α | small-molecule | Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y | 10.1126/SCIADV.ABF1268 | 2021-05-05 | 55353 | |
Gq/11 | αq | Human | Gq-Gs-Gi1 chimera | 55 | β1 | Rat | γ2 | Human | Cryo-EM | 7MBY | - | 2.4 | CCKAR | CCK1 | Cholecystokinin | A (Rhodopsin) | Human | - | - | - |
CHEMBL216166
chembl_ligand
pubchem
|
protein | Agonist | CCK-33, CCK-4, gastrin-17, CCK-39, desulfated cholecystokinin-8, CCK-8, CCK-58 | 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 | 55363 | |
Gi/o | αi1 | Human | - | 62 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7O7F | 7O7F_refined | 3.2 | CCR5 | CCR5 | Chemokine | A (Rhodopsin) | Human | - |
Fab heavy chain Fab light chain |
- |
CCL5
gtoplig
|
peptide | Agonist | CCL8, CCL3, CCL7, CCL14, CCL11, CCL4, CCL2, CCL13, CCL5, CCL16 | peptide | Isaikina P, Tsai CJ, Dietz N, Pamula F, Grahl A, Goldie KN, Guixa-Gonzalez R, Branco C, Paolini-Bertrand M, Calo N, Cerini F, Schertler GFX, Hartley O, Stahlberg H, Maier T, Deupi X, Grzesiek S | 10.1126/SCIADV.ABG8685 | 2021-06-30 | 55355 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7F1Q | - | 2.9 | CCR5 | CCR5 | Chemokine | A (Rhodopsin) | Human | - | - | - |
CCL3
gtoplig
|
peptide | Agonist | CCL8, CCL3, CCL7, CCL14, CCL11, CCL4, CCL2, CCL13, CCL5, CCL16 | peptide | - | - | 2021-07-14 | 55355 | |
Gs | αs | Bovine | - | 59 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7DTY | - | 3.0 | GIPR | GIP | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
GIP
pubchem
|
small-molecule | Agonist | gastric inhibitory polypeptide | peptide | Zhao F, Zhang C, Zhou Q, Hang K, Zou X, Chen Y, Wu F, Rao Q, Dai A, Yin W, Shen DD, Zhang Y, Xia T, Stevens RC, Xu HE, Yang D, Zhao L, Wang MW | 10.7554/ELIFE.68719 | 2021-08-04 | 55370 | |
Gs | αs | Human | - | 89 | β1 | Human | γ2 | Human | Cryo-EM | 7KI1 | - | 2.5 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
taspoglutide
pubchem
gtoplig
drugbank
|
peptide | Agonist | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | Zhang X, Belousoff MJ, Liang YL, Danev R, Sexton PM, Wootten D | 10.1016/J.CELREP.2021.109374 | 2021-08-04 | 55353 | |
Gq/11 | αq | Human | Engineered G alpha | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7F9Z | 7F9Z_refined | 3.2 | GHSR | ghrelin | Ghrelin | A (Rhodopsin) | Human | - |
Nanobody-35 scFv16 |
- |
GHRP-6
pubchem
gtoplig
|
peptide | Agonist | [des-Gln14]ghrelin, ghrelin | peptide | Wang Y, Guo S, Zhuang Y, Yun Y, Xu P, He X, Guo J, Yin W, Xu HE, Xie X, Jiang Y | 10.1038/S41467-021-25364-2 | 2021-08-18 | 55363 | |
Gq/11 | αq | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7EZM | - | 2.9 | CCKAR | CCK1 | Cholecystokinin | A (Rhodopsin) | Human | - | scFv16 | - |
CCK-8
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
peptide | Agonist | CCK-33, CCK-4, gastrin-17, CCK-39, desulfated cholecystokinin-8, CCK-8, CCK-58 | 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 | 55363 | |
Gi/o | αi2 | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7LD4 | 7LD4_refined | 3.3 | AA1R | A1 | Adenosine | A (Rhodopsin) | Human | - | - | - |
adenosine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | adenosine | small-molecule | Draper-Joyce CJ, Bhola R, Wang J, Bhattarai A, Nguyen ATN, Cowie-Kent I, O'Sullivan K, Chia LY, Venugopal H, Valant C, Thal DM, Wootten D, Panel N, Carlsson J, Christie MJ, White PJ, Scammells P, May LT, Sexton PM, Danev R, Miao Y, Glukhova A, Imlach WL, Christopoulos A | 10.1038/S41586-021-03897-2 | 2021-09-08 | 55356 | |
Gi/o | αt1 | Bovine | Only H5 | 3 | - | - | - | - | X-ray | 4BEY | 4BEY_refined | 2.9 | OPSD | Rhodopsin | Opsins | A (Rhodopsin) | Bovine | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Singhal A, Ostermaier MK, Vishnivetskiy SA, Panneels V, Homan KT, Tesmer JJ, Veprintsev D, Deupi X, Gurevich VV, Schertler GF, Standfuss J | 10.1038/EMBOR.2013.44 | 2013-05-08 | 55465 | |
Gi/o | αt1 | Bovine | Only H5 | 3 | - | - | - | - | X-ray | 4J4Q | 4J4Q_refined | 2.7 | OPSD | Rhodopsin | Opsins | A (Rhodopsin) | Bovine | - | - | - |
B-Octylglucoside
pubchem
|
small-molecule | unknown | - | - | Park JH, Morizumi T, Li Y, Hong JE, Pai EF, Hofmann KP, Choe HW, Ernst OP | 10.1002/ANIE.201302374 | 2013-10-30 | 55465 | |
Gs | αs | Human | Engineered G protein | 50 | - | - | - | - | X-ray | 5G53 | 5G53_refined | 3.4 | AA2AR | A2A | Adenosine | A (Rhodopsin) | Human | - | - | - |
NECA
pubchem
gtoplig
chembl_ligand
gtoplig
|
small-molecule | Agonist | adenosine | small-molecule | Carpenter B, Nehme R, Warne T, Leslie AG, Tate CG | 10.1038/NATURE18966 | 2016-08-03 | 55353 | |
Gs | αs | Bovine | - | 57 | β1 | Rat | γ2 | Bovine | Cryo-EM | 6NBH | - | 3.5 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
Long-acting parathyroid hormone analog
|
peptide | Agonist | PTH, PTHrP-(1-36), TIP39, PTHrP | peptide | Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y | 10.1126/SCIENCE.AAV7942 | 2019-04-17 | 55370 | |
Gi/o | αo | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 6OIK | 6OIK_refined | 3.6 | ACM2 | M2 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | - | - |
LY2119620
pubchem
gtoplig
chembl_ligand
iperoxo pubchem gtoplig chembl_ligand |
small-molecule small-molecule |
Ago-PAM Agonist |
acetylcholine | small-molecule | Maeda S, Qu Q, Robertson MJ, Skiniotis G, Kobilka BK | 10.1126/SCIENCE.AAW5188 | 2019-05-08 | 55361 | |
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 | 55355 | |
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 | neuromedin N, large neurotensin, neurotensin, large 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 | 55355 | |
Gi/o | αi1 | Human | - | 60 | β1 | Bovine | γT1 | Bovine | Cryo-EM | 6QNO | - | 4.4 | OPSD | Rhodopsin | Opsins | A (Rhodopsin) | Bovine | - |
Fab antibody fragment light chain Fab antibody fragment heavy chain |
- |
Retinal (all-trans)
pubchem
|
small-molecule | Agonist | - | - | Tsai CJ, Marino J, Adaixo R, Pamula F, Muehle J, Maeda S, Flock T, Taylor NM, Mohammed I, Matile H, Dawson RJ, Deupi X, Stahlberg H, Schertler G | 10.7554/ELIFE.46041 | 2019-07-10 | 55355 | |
Gi/o | αt1 | Bovine | - | 64 | β1 | Bovine | γT1 | Bovine | Cryo-EM | 6OY9 | - | 3.9 | OPSD | Rhodopsin | Opsins | A (Rhodopsin) | Bovine | - | - | - |
Retinal (all-trans)
pubchem
|
small-molecule | Agonist | - | - | Gao Y, Hu H, Ramachandran S, Erickson JW, Cerione RA, Skiniotis G | 10.1016/J.MOLCEL.2019.06.007 | 2019-07-24 | 55465 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 6NI3 | 6NI3_refined | 3.8 | ADRB2 | β2 | Adrenoceptors | A (Rhodopsin) | Human | - | Nanobody-35 | - |
CHEMBL1615159
chembl_ligand
pubchem
|
small-molecule | Agonist | (-)-adrenaline, Zn2+, L-NOREPINEPHRINE, noradrenaline, (-)-noradrenaline | small-molecule | Nguyen AH, Thomsen ARB, Cahill TJ 3rd, Huang R, Huang LY, Marcink T, Clarke OB, Heissel S, Masoudi A, Ben-Hail D, Samaan F, Dandey VP, Tan YZ, Hong C, Mahoney JP, Triest S, Little J 4th, Chen X, Sunahara R, Steyaert J, Molina H, Yu Z, des Georges A, Lefkowitz RJ | 10.1038/S41594-019-0330-Y | 2019-11-20 | 55353 | |
Gs | αs | Human | - | 49 | β1 | Human | γ2 | Human | Cryo-EM | 6ORV | 6ORV_refined | 3.0 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
CHEMBL3950796
chembl_ligand
pubchem
|
small-molecule | Agonist | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | Zhao P, Liang YL, Belousoff MJ, Deganutti G, Fletcher MM, Willard FS, Bell MG, Christe ME, Sloop KW, Inoue A, Truong TT, Clydesdale L, Furness SGB, Christopoulos A, Wang MW, Miller LJ, Reynolds CA, Danev R, Sexton PM, Wootten D | 10.1038/s41586-019-1902-z | 2020-01-08 | 55353 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 6KPG | 6KPG_refined | 3.0 | CNR1 | CB1 | Cannabinoid | A (Rhodopsin) | Human | - | scFv16 | - |
AM841
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | Hua T, Li X, Wu L, Iliopoulos-Tsoutsouvas C, Wang Y, Wu M, Shen L, Brust CA, Nikas SP, Song F, Song X, Yuan S, Sun Q, Wu Y, Jiang S, Grim TW, Benchama O, Stahl EL, Zvonok N, Zhao S, Bohn LM, Makriyannis A, Liu ZJ | 10.1016/J.CELL.2020.01.008 | 2020-02-12 | 55355 | |
Gi/o | αt1 | Bovine | Only H5 | 3 | - | - | - | - | X-ray | 6NWE | 6NWE_refined | 2.7 | OPSD | Rhodopsin | Opsins | A (Rhodopsin) | Bovine | - | - | - |
B-Octylglucoside
pubchem
|
small-molecule | unknown | - | - | - | - | 2020-02-12 | 55465 | |
Gs | αs | Human | Gs-Gi1 chimera | 58 | β1 | Human | γ2 | Human | Cryo-EM | 6PB0 | - | 3.0 | CRFR1 | CRF1 | Corticotropin-releasing factor | B1 (Secretin) | Human | - | Nanobody-35 | - |
Urocortin
pubchem
|
peptide | Agonist | corticotrophin-releasing hormone, urocortin 2, urocortin 1 | peptide | Ma S, Shen Q, Zhao LH, Mao C, Zhou XE, Shen DD, de Waal PW, Bi P, Li C, Jiang Y, Wang MW, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE | 10.1016/J.MOLCEL.2020.01.013 | 2020-02-12 | 55353 | |
Gi/o | αi1 | Human | - | 100 | β1 | Human | γ2 | Human | Cryo-EM | 6PT0 | 6PT0_refined | 3.2 | CNR2 | CB2 | Cannabinoid | A (Rhodopsin) | Human | - | scFv16 | - |
WIN55212-2
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | Xing C, Zhuang Y, Xu TH, Feng Z, Zhou XE, Chen M, Wang L, Meng X, Xue Y, Wang J, Liu H, McGuire TF, Zhao G, Melcher K, Zhang C, Xu HE, Xie XQ | 10.1016/J.CELL.2020.01.007 | 2020-02-12 | 55355 | |
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 | 55353 | |
Gs | αs | Human | - | 55 | β1 | Human | γ2 | Human | Cryo-EM | 6M1H | - | 3.6 | PACR | PAC1 | VIP and PACAP | B1 (Secretin) | Human | - | Nanobody-35 | - |
maxadilan
gtoplig
pubchem
|
peptide | Agonist | PACAP-27, PACAP-38, VIP, PHV, PHM, PHI | peptide | Wang J, Song X, Zhang D, Chen X, Li X, Sun Y, Li C, Song Y, Ding Y, Ren R, Harrington EH, Hu LA, Zhong W, Xu C, Huang X, Wang HW, Ma Y | 10.1038/S41422-020-0280-2 | 2020-03-11 | 55353 | |
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 | 55353 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 6LML | 6LML_refined | 3.9 | GLR | glucagon | Glucagon | B1 (Secretin) | Human | - | scFv16 | - |
glucagon
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
pubchem
pubchem
pubchem
pubchem
|
peptide | Agonist | glucagon | peptide | Qiao A, Han S, Li X, Li Z, Zhao P, Dai A, Chang R, Tai L, Tan Q, Chu X, Ma L, Thorsen TS, Reedtz-Runge S, Yang D, Wang MW, Sexton PM, Wootten D, Sun F, Zhao Q, Wu B | 10.1126/SCIENCE.AAZ5346 | 2020-04-01 | 55355 | |
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 | 55353 | |
Gs | αs | Human | - | 56 | β1 | Human | γ2 | Human | Cryo-EM | 6WHC | 6WHC_refined | 3.4 | GLR | glucagon | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
Dual-agonist peptide P15
|
peptide | Agonist | glucagon | peptide | Chang R, Zhang X, Qiao A, Dai A, Belousoff MJ, Tan Q, Shao L, Zhong L, Lin G, Liang YL, Ma L, Han S, Yang D, Danev R, Wang MW, Wootten D, Wu B, Sexton PM | 10.1074/JBC.RA120.013793 | 2020-05-27 | 55353 | |
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 | 55355 | |
Gi/o | αt2 | Bovine | Only H5 | 3 | - | - | - | - | X-ray | 6PGS | 6PGS_refined | 2.9 | OPSD | Rhodopsin | Opsins | A (Rhodopsin) | Bovine | - | - | - |
Geraniol
pubchem
|
small-molecule | unknown | - | - | - | - | 2020-07-01 | 55485 | |
Gi/o | αt2 | Bovine | Only H5 | 3 | - | - | - | - | X-ray | 6PH7 | 6PH7_refined | 2.9 | OPSD | Rhodopsin | Opsins | A (Rhodopsin) | Bovine | - | - | - |
Nerol
pubchem
|
small-molecule | unknown | - | - | - | - | 2020-07-01 | 55485 | |
Gs | αs | Human | - | 57 | β1 | Human | γ2 | Human | Cryo-EM | 6VCB | - | 3.3 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
glucagon-like peptide 1-(7-37)
pubchem
gtoplig
chembl_ligand
gtoplig
pubchem
pubchem
CHEMBL5197819 chembl_ligand pubchem |
peptide small-molecule |
Agonist PAM |
glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | Bueno AB, Sun B, Willard FS, Feng D, Ho JD, Wainscott DB, Showalter AD, Vieth M, Chen Q, Stutsman C, Chau B, Ficorilli J, Agejas FJ, Cumming GR, Jimenez A, Rojo I, Kobilka TS, Kobilka BK, Sloop KW | 10.1038/S41589-020-0589-7 | 2020-07-22 | 55353 | |
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 | CXCL1, CXCL6, CXCL3, CXCL8, CXCL7, CXCL5, CXCL2 | 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 | 55355 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7CFM | - | 3.0 | GPBAR | GPBA | Bile acid | A (Rhodopsin) | Human | - | Nanobody-35 | - |
CHEMBL2331646
chembl_ligand
pubchem
|
small-molecule | Agonist | cholic acid, lithocholic acid, chenodeoxycholic acid, deoxycholic acid | small-molecule | Yang F, Mao C, Guo L, Lin J, Ming Q, Xiao P, Wu X, Shen Q, Guo S, Shen DD, Lu R, Zhang L, Huang S, Ping Y, Zhang C, Ma C, Zhang K, Liang X, Shen Y, Nan F, Yi F, Luca VC, Zhou J, Jiang C, Sun JP, Xie X, Yu X, Zhang Y | 10.1038/S41586-020-2569-1 | 2020-09-09 | 55353 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 6XBJ | - | 3.9 | SMO | SMO | Frizzled | F (Frizzled) | Human | - | scFv16 | - |
Cholesterol
pubchem
|
small-molecule | Agonist | - | - | Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X | 10.1038/S41589-020-0646-2 | 2020-09-30 | 55355 | |
Gs | αs | Human | - | 58 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7CZ5 | 7CZ5_refined | 2.6 | GHRHR | GHRH | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
Somatoliberin
pubchem
|
peptide | Agonist | GHRH | peptide | Zhou F, Zhang H, Cong Z, Zhao LH, Zhou Q, Mao C, Cheng X, Shen DD, Cai X, Ma C, Wang Y, Dai A, Zhou Y, Sun W, Zhao F, Zhao S, Jiang H, Jiang Y, Yang D, Eric Xu H, Zhang Y, Wang MW | 10.1038/S41467-020-18945-0 | 2020-11-18 | 55353 | |
GPa1 family | αPa1 | strain ATCC 204508 / S288c | Two alpha subunits bound to STE2 dimer | 46 | STE4 | strain ATCC 204508 / S288c | γ | strain ATCC 204508 / S288c | Cryo-EM | 7AD3 | - | 3.5 | STE2 | STE2 | STE2 | D1 (Ste2-like fungal pheromone) | strain ATCC 204508 / S288c | - | - | - |
Alpha-factor mating pheromone
pubchem
|
peptide | Agonist | - | - | Velazhahan V, Ma N, Pandy-Szekeres G, Kooistra AJ, Lee Y, Gloriam DE, Vaidehi N, Tate CG | 10.1038/S41586-020-2994-1 | 2020-12-09 | 55369 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γT1 | Human | Cryo-EM | 7L0P | - | 4.1 | NTR1 | NTS1 | Neurotensin | A (Rhodopsin) | Rat | - | - | - |
neurotensin
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
|
peptide | Agonist | neuromedin N, neurotensin | peptide | Zhang M, Gui M, Wang ZF, Gorgulla C, Yu JJ, Wu H, Sun ZJ, Klenk C, Merklinger L, Morstein L, Hagn F, Pluckthun A, Brown A, Nasr ML, Wagner G | 10.1038/S41594-020-00554-6 | 2021-01-06 | 55355 | |
Gs | αs | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7LCI | 7LCI_refined | 2.9 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | - | - |
danuglipron
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | Zhang X, Johnson RM, Drulyte I, Yu L, Kotecha A, Danev R, Wootten D, Sexton PM, Belousoff MJ | 10.1016/J.STR.2021.04.008 | 2021-01-20 | 55353 | |
Gs | αs | Human | Engineered G alpha | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7L1U | - | 3.2 | OX2R | OX2 | Orexin | A (Rhodopsin) | Human | - | scFv16 | - |
Orexin-A
pubchem
|
peptide | Agonist | orexin-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 | 55353 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7JVR | - | 2.8 | DRD2 | D2 | Dopamine | A (Rhodopsin) | Human | - | scFv16 | - |
bromocriptine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | dopamine | small-molecule | Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP, Shen DD, Xu T, Liu YF, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE | 10.1016/J.CELL.2021.01.027 | 2021-02-24 | 55355 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7CKY | - | 3.2 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
CHEMBL3697578
chembl_ligand
pubchem
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine, dopamine, (-)-noradrenaline | small-molecule | Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z | 10.1016/J.CELL.2021.01.028 | 2021-03-03 | 55353 | |
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 drugbank |
small-molecule small-molecule |
Agonist PAM |
L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine, dopamine, (-)-noradrenaline | small-molecule | Zhuang Y, Krumm B, Zhang H, Zhou XE, Wang Y, Huang XP, Liu Y, Cheng X, Jiang Y, Jiang H, Zhang C, Yi W, Roth BL, Zhang Y, Xu HE | 10.1038/S41422-021-00482-0 | 2021-03-03 | 55353 | |
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 | 55355 | |
Gs | αs | Human | - | 86 | β1 | Human | γ2 | Human | X-ray | 7JOZ | 7JOZ_refined | 3.8 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
CHEMBL4453318
chembl_ligand
pubchem
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine, dopamine, (-)-noradrenaline | 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 | 55353 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7CX3 | - | 2.8 | PE2R2 | EP2 | Prostanoid | A (Rhodopsin) | Human | - | Nanobody-35 | - |
taprenepag
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | thromboxane A2, PGD2, PGE1, PGE2, PGI2, PGF2α | small-molecule | Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y | 10.1126/SCIADV.ABF1268 | 2021-05-05 | 55353 | |
Gs | αs | Human | - | 61 | β1 | Rat | γ2 | Human | Cryo-EM | 7MBX | - | 2.0 | CCKAR | CCK1 | Cholecystokinin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
CHEMBL216166
chembl_ligand
pubchem
|
protein | Agonist | CCK-33, CCK-4, gastrin-17, CCK-39, desulfated cholecystokinin-8, CCK-8, CCK-58 | 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 | 55353 | |
Gs | αs | Human | - | 55 | β1 | Human | γ2 | Human | Cryo-EM | 7BB7 | - | 4.4 | V2R | V2 | Vasopressin and oxytocin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
vasopressin
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
peptide | Agonist | 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 | 55353 | |
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 | 55355 | |
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 drugbank |
small-molecule small-molecule |
Ago-PAM Agonist |
glucagon, glucagon-like peptide 1-(7-36) amide, 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 | 55353 | |
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 | 55355 | |
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) | CCL8, CCL3, CCL7, CCL14, CCL11, CCL4, CCL2, CCL13, CCL5, 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 | 55355 | |
Gs | αs | Human | - | 59 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7DH5 | - | 3.2 | ADRB3 | β3 | Adrenoceptors | A (Rhodopsin) | Dog | - | Nanobody-35 | - |
mirabegron
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | - | - | Nagiri C, Kobayashi K, Tomita A, Kato M, Kobayashi K, Yamashita K, Nishizawa T, Inoue A, Shihoya W, Nureki O | 10.1016/J.MOLCEL.2021.06.024 | 2021-08-04 | 55353 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7EVW | - | 3.2 | FZD7 | FZD7 | Frizzled | F (Frizzled) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Xu L, Chen B, Schihada H, Wright SC, Turku A, Wu Y, Han GW, Kowalski-Jahn M, Kozielewicz P, Bowin CF, Zhang X, Li C, Bouvier M, Schulte G, Xu F | 10.1038/S41422-021-00525-6 | 2021-08-04 | 55353 | |
Gs | αs | Human | - | 53 | β1 | Human | γ2 | Human | Cryo-EM | 7KI0 | - | 2.5 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
semaglutide
pubchem
gtoplig
chembl_ligand
drugbank
pubchem
|
peptide | Agonist | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | Zhang X, Belousoff MJ, Liang YL, Danev R, Sexton PM, Wootten D | 10.1016/J.CELREP.2021.109374 | 2021-08-04 | 55353 | |
Gs | αs | Human | - | 58 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7F16 | - | 2.8 | PTH2R | PTH2 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
TIP39
gtoplig
|
peptide | Agonist | PTH, PTHrP, PTHrP-(1-34) (human), PTHrP-(1-36), TIP39 | peptide | Wang X, Cheng X, Zhao L, Wang Y, Ye C, Zou X, Dai A, Cong Z, Chen J, Zhou Q, Xia T, Jiang H, Xu HE, Yang D, Wang MW | 10.1073/PNAS.2101279118 | 2021-08-18 | 55353 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7EW3 | - | 3.1 | S1PR3 | S1P3 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
Sphingosine 1-phosphate
pubchem
|
lipid | Agonist | sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate | small-molecule | Zhao C, Cheng L, Wang W, Wang H, Luo Y, Feng Y, Wang X, Fu H, Cai Y, Yang S, Fu P, Yan W, Shao Z | 10.1038/S41422-021-00567-W | 2021-09-29 | 55355 | |
Gs | αs | Bovine | - | 91 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7FII | - | 4.3 | LSHR | LH | Glycoprotein hormone | A (Rhodopsin) | Human | - | - | - |
Glycoprotein alpha
gtoplig
Choriogonadotropin beta gtoplig |
protein protein |
Agonist | 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 | 55370 | |
Gq/11 | αq | Human | Gq-Gi1 chimera | 61 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7EIB | - | 3.0 | BKRB1 | B1 | Bradykinin | A (Rhodopsin) | Human | - | - | - |
[des-Arg10]kallidin
pubchem
gtoplig
chembl_ligand
gtoplig
|
peptide | Agonist | [des-Arg9]bradykinin, [des-Arg10]kallidin, T-kinin, Lys-[Hyp3]-bradykinin, kallidin, bradykinin, [Hyp3]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 | 55363 | |
Gq/11 | αq | Human | Gq-Gi1 chimera | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7F2O | - | 2.9 | BKRB2 | B2 | Bradykinin | A (Rhodopsin) | Human | - | scFv16 | - |
bradykinin
pubchem
gtoplig
chembl_ligand
drugbank
gtoplig
|
peptide | Agonist | [des-Arg9]bradykinin, [des-Arg10]kallidin, T-kinin, Lys-[Hyp3]-bradykinin, kallidin, bradykinin, [Hyp3]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 | 55363 | |
Gq/11 | αq | Human | Gq-Gi1 chimera | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7F8W | 7F8W_refined | 3.1 | GASR | CCK2 | Cholecystokinin | A (Rhodopsin) | Human | - | scFv16 | - |
desulfated gastrin-17
pubchem
gtoplig
chembl_ligand
pubchem
|
peptide | Agonist | CCK-33, CCK-4, gastrin-71, desulfated gastrin-71, desulfated gastrin-14, gastrin-14, desulfated gastrin-17, gastrin-17, gastrin-34, CCK-39, desulfated gastrin-34, desulfated cholecystokinin-8, CCK-8, CCK-58 | 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 | 55363 | |
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 | 55353 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7F58 | 7F58_refined | 3.1 | MC4R | MC4 | Melanocortin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
THIQ
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | β-MSH, 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 | 55353 | |
Gs | αs | Human | - | 48 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7PIU | - | 2.6 | MC4R | MC4 | Melanocortin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
setmelanotide
pubchem
gtoplig
drug_central
chembl_ligand
drugbank
|
peptide | Agonist | β-MSH, α-MSH, agouti-related protein, γ-MSH, ACTH | peptide | Heyder NA, Kleinau G, Speck D, Schmidt A, Paisdzior S, Szczepek M, Bauer B, Koch A, Gallandi M, Kwiatkowski D, Burger J, Mielke T, Beck-Sickinger AG, Hildebrand PW, Spahn CMT, Hilger D, Schacherl M, Biebermann H, Hilal T, Kuhnen P, Kobilka BK, Scheerer P | 10.1038/S41422-021-00569-8 | 2021-11-17 | 55353 | |
Gq/11 | αq | Human | Gq-Gs chimera | 57 | β1 | Human | γ2 | Human | Cryo-EM | 7S8N | 7S8N_refined | 2.9 | MRGX2 | MRGPRX2 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
(R)-ZINC-3573
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | PAMP-20 | peptide | Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL | 10.1038/S41586-021-04126-6 | 2021-11-17 | 55363 | |
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 | 55355 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7VV5 | 7VV5_refined | 2.8 | MRGX2 | MRGPRX2 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
compound 48/80
pubchem
gtoplig
|
small-molecule | Agonist | PAMP-20 | peptide | Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP | 10.1038/S41586-021-04077-Y | 2021-12-01 | 55355 | |
Gs | αs | Human | Gs-Gi1 chimera | 57 | β1 | Human | γ2 | Human | Cryo-EM | 7P02 | - | 2.9 | NK1R | NK1 | Tachykinin | A (Rhodopsin) | Human | - | scFv16 | - |
substance P
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
|
peptide | Agonist | substance P, hemokinin 1, neuropeptide-γ, neurokinin A, neurokinin B, neuropeptide K | peptide | Thom C, Ehrenmann J, Vacca S, Waltenspuhl Y, Schoppe J, Medalia O, Pluckthun A | 10.1126/SCIADV.ABK2872 | 2021-12-15 | 55353 | |
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-tryptophan, L-phenylalanine | small-molecule | Zhou Y, Daver H, Trapkov B, Wu L, Wu M, Harpsoe K, Gentry PR, Liu K, Larionova M, Liu J, Chen N, Brauner-Osborne H, Gloriam DE, Hua T, Liu ZJ | 10.1038/S41422-021-00591-W | 2021-12-29 | 55355 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7EO2 | 7EO2_refined | 2.9 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
(S)-FTY720-phosphate
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate | small-molecule | Xu Z, Ikuta T, Kawakami K, Kise R, Qian Y, Xia R, Sun MX, Zhang A, Guo C, Cai XH, Huang Z, Inoue A, He Y | 10.1038/S41589-021-00930-3 | 2022-01-05 | 55355 | |
Gi/o | αo | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7W2Z | 7W2Z_refined | 2.8 | GHSR | ghrelin | Ghrelin | A (Rhodopsin) | Human | - | scFv16 | - |
Ghrelin
pubchem
|
peptide | Agonist | [des-Gln14]ghrelin, ghrelin | peptide | Qin J, Cai Y, Xu Z, Ming Q, Ji SY, Wu C, Zhang H, Mao C, Shen DD, Hirata K, Ma Y, Yan W, Zhang Y, Shao Z | 10.1038/S41467-022-27975-9 | 2022-01-19 | 55361 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7RKM | - | 3.5 | US28 | US28 | Unclassified | A (Rhodopsin) | strain AD169 | - | scFv16 | - |
Fractalkine
pubchem
|
peptide | Agonist | - | - | Tsutsumi N, Maeda S, Qu Q, Vogele M, Jude KM, Suomivuori CM, Panova O, Waghray D, Kato HE, Velasco A, Dror RO, Skiniotis G, Kobilka BK, Garcia KC | 10.1126/SCIADV.ABL5442 | 2022-01-26 | 55355 | |
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 | 55353 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7EW7 | - | 3.3 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
SEW2871
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate | small-molecule | Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z | 10.1038/S41422-021-00566-X | 2021-09-29 | 55355 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7F4I | 7F4I_refined | 3.1 | MSHR | MC1 | Melanocortin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
bremelanotide
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
peptide | Agonist | β-MSH, γ-MSH, ACTH, 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 | 55353 | |
Gi/o | αi1 | Human | - | 62 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7T6U | - | 2.9 | FPR2 | FPR2/ALX | Formylpeptide | A (Rhodopsin) | Human | - | - | - |
synthetic peptide
|
peptide | Agonist | serum amyloid A, aspirin triggered lipoxin A4, humanin, resolvin D1, LL-37, PrP106-126, annexin I, LXA4, aspirin-triggered resolvin D1 | peptide | Zhuang Y, Wang L, Guo J, Sun D, Wang Y, Liu W, Xu HE, Zhang C | 10.1038/S41467-022-28586-0 | 2022-03-30 | 55355 | |
Gi/o | αi3 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7T11 | 7T11_refined | 2.7 | SSR2 | SST2 | Somatostatin | A (Rhodopsin) | Human | - | scFv16 | - |
Octreotide
|
peptide | Agonist | CST-17, cortistatin-14, SRIF-28, SRIF-14 | peptide | Robertson MJ, Meyerowitz JG, Panova O, Borrelli K, Skiniotis G | 10.1038/S41594-022-00727-5 | 2022-03-09 | 55357 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7VLA | 7VLA_refined | 2.7 | CCR1 | CCR1 | Chemokine | A (Rhodopsin) | Human | - | scFv16 | - |
CCL15(27-92)
|
peptide | Agonist | CCL8, CCL23, CCL3, CCL7, CCL14, CCL15, CCL4, CCL13, CCL5, CCL16 | peptide | Shao Z, Shen Q, Yao B, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Ma H, Chen ZH, Xu HE, Ying S, Zhang Y, Shen H | 10.1038/S41589-021-00918-Z | 2022-03-23 | 55355 | |
Gi/o | αi1 | Human | - | 62 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7VGY | - | 3.1 | MTR1A | MT1 | Melatonin | A (Rhodopsin) | Human | - | scFv16 | - |
2-iodo-melatonin
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | melatonin | small-molecule | Wang Q, Lu Q, Guo Q, Teng M, Gong Q, Li X, Du Y, Liu Z, Tao Y | 10.1038/S41467-022-28111-3 | 2022-03-02 | 55355 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7TYL | - | 3.3 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - | Nanobody-35 | - |
Amylin rat
pubchem
|
peptide | Agonist | adrenomedullin 2/intermedin, amylin, β-CGRP, α-CGRP, calcitonin, adrenomedullin | 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 | 55353 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7TYO | - | 2.7 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - | Nanobody-35 | - |
Calcitonin human
pubchem
chembl_ligand
drugbank
|
peptide | Agonist | adrenomedullin 2/intermedin, amylin, β-CGRP, α-CGRP, calcitonin, adrenomedullin | 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 | 55353 | |
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 2/intermedin, amylin, β-CGRP, α-CGRP, calcitonin, adrenomedullin | 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 | 55353 | |
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 | 55353 | |
Gi/o | αo | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7EJ0 | - | 3.2 | ADA2A | α2A | Adrenoceptors | A (Rhodopsin) | Human | - | scFv16 | - |
(-)-noradrenaline
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline | small-molecule | Xu J, Cao S, Hubner H, Weikert D, Chen G, Lu Q, Yuan D, Gmeiner P, Liu Z, Du Y | 10.1126/SCIADV.ABJ5347 | 2022-04-13 | 55361 | |
Gs | αs | Human | - | 57 | β1 | Rat | γ2 | Bovine | Cryo-EM | 6LPB | 6LPB_refined | 3.9 | PACR | PAC1 | VIP and PACAP | B1 (Secretin) | Human | - | Nanobody-35 | - |
[Ac-His1]PACAP-27
gtoplig
chembl_ligand
pubchem
|
peptide | Agonist | PACAP-27, PACAP-38, VIP, PHV, PHM, PHI | peptide | Kobayashi K, Shihoya W, Nishizawa T, Kadji FMN, Aoki J, Inoue A, Nureki O | 10.1038/S41594-020-0386-8 | 2020-03-11 | 55353 | |
Gs | αs | Human | - | 57 | β1 | Human | γ2 | Human | Cryo-EM | 6M1I | - | 3.5 | PACR | PAC1 | VIP and PACAP | B1 (Secretin) | Human | - | Nanobody-35 | - |
[Ac-His1]PACAP-27
gtoplig
chembl_ligand
pubchem
|
peptide | Agonist | PACAP-27, PACAP-38, VIP, PHV, PHM, PHI | peptide | Wang J, Song X, Zhang D, Chen X, Li X, Sun Y, Li C, Song Y, Ding Y, Ren R, Harrington EH, Hu LA, Zhong W, Xu C, Huang X, Wang HW, Ma Y | 10.1038/S41422-020-0280-2 | 2020-03-11 | 55353 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 6LMK | 6LMK_refined | 3.7 | GLR | glucagon | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
glucagon
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
pubchem
pubchem
pubchem
pubchem
|
peptide | Agonist | glucagon | peptide | Qiao A, Han S, Li X, Li Z, Zhao P, Dai A, Chang R, Tai L, Tan Q, Chu X, Ma L, Thorsen TS, Reedtz-Runge S, Yang D, Wang MW, Sexton PM, Wootten D, Sun F, Zhao Q, Wu B | 10.1126/SCIENCE.AAZ5346 | 2020-04-01 | 55353 | |
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 | 55353 | |
Gi/o | αo | Human | - | 60 | β1 | Mouse | γ2 | Human | Cryo-EM | 6K41 | - | 2.9 | ADA2B | α2B | Adrenoceptors | A (Rhodopsin) | Human | T4-Lysozyme | scFv | - |
dexmedetomidine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline | small-molecule | Yuan D, Liu Z, Kaindl J, Maeda S, Zhao J, Sun X, Xu J, Gmeiner P, Wang HW, Kobilka BK | 10.1038/S41589-020-0492-2 | 2020-04-15 | 55361 | |
Gi/o | αi1 | Human | - | 62 | β1 | Mouse | γ2 | Human | Cryo-EM | 6K42 | - | 4.1 | ADA2B | α2B | Adrenoceptors | A (Rhodopsin) | Human | T4-Lysozyme | scFv | - |
dexmedetomidine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline | small-molecule | Yuan D, Liu Z, Kaindl J, Maeda S, Zhao J, Sun X, Xu J, Gmeiner P, Wang HW, Kobilka BK | 10.1038/S41589-020-0492-2 | 2020-04-15 | 55355 | |
Gi/o | αt1 | Bovine | Only H5 | 3 | - | - | - | - | X-ray | 6PEL | 6PEL_refined | 3.2 | OPSD | Rhodopsin | Opsins | A (Rhodopsin) | Bovine | - | - | - |
Citronellol
pubchem
|
small-molecule | unknown | - | - | - | - | 2020-06-24 | 55465 | |
Gi/o | αo | Human | - | 59 | β1 | Rat | γ2 | Mouse | Cryo-EM | 6WWZ | 6WWZ_refined | 3.3 | CCR6 | CCR6 | Chemokine | A (Rhodopsin) | Human | - | scFv16 | - |
CCL20
gtoplig
|
peptide | Agonist | beta-defensin 4A, CCL20 | peptide | Wasilko DJ, Johnson ZL, Ammirati M, Che Y, Griffor MC, Han S, Wu H | 10.1038/S41467-020-16820-6 | 2020-06-24 | 55361 | |
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
drugbank
drugbank
|
small-molecule | Agonist | (-)-adrenaline, Zn2+, L-NOREPINEPHRINE, noradrenaline, (-)-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 | 55353 | |
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
drugbank
|
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 | 55353 | |
Gi/o | αi1 | Human | - | 65 | β1 | Human | γ2 | Human | Cryo-EM | 6LFO | 6LFO_refined | 3.4 | CXCR2 | CXCR2 | Chemokine | A (Rhodopsin) | Human | - | scFv16 | - |
Interleukin-8
pubchem
|
protein | Agonist | CXCL1, CXCL6, CXCL3, CXCL8, CXCL7, CXCL5, CXCL2 | 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 | 55355 | |
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
drugbank
|
small-molecule | Agonist | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, Senel P, Stewart GD, Liang YL, Glukhova A, Venugopal H, Christopoulos A, Furness SGB, Miller LJ, Reedtz-Runge S, Langmead CJ, Gloriam DE, Danev R, Sexton PM, Wootten D | 10.1016/J.MOLCEL.2020.09.020 | 2020-09-09 | 55353 | |
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 | 55363 | |
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 | 55355 | |
Gs | αs | Human | - | 49 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7DHR | 7DHR_refined | 3.8 | ADRB2 | β2 | Adrenoceptors | A (Rhodopsin) | Human | - | Nanobody-35 | - |
LEVISOPRENALINE
chembl_ligand
chembl_ligand
pubchem
|
small-molecule | Agonist | (-)-adrenaline, Zn2+, L-NOREPINEPHRINE, noradrenaline, (-)-noradrenaline | small-molecule | Yang F, Ling S, Zhou Y, Zhang Y, Lv P, Liu S, Fang W, Sun W, Hu LA, Zhang L, Shi P, Tian C | 10.1093/NSR/NWAA284 | 2020-12-16 | 55353 | |
Gi/o | αi1 | Human | - | 95 | β1 | Human | γT1 | Human | Cryo-EM | 7L0Q | - | 4.3 | NTR1 | NTS1 | Neurotensin | A (Rhodopsin) | Rat | - | - | - |
neurotensin
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
|
peptide | Agonist | neuromedin N, neurotensin | peptide | Zhang M, Gui M, Wang ZF, Gorgulla C, Yu JJ, Wu H, Sun ZJ, Klenk C, Merklinger L, Morstein L, Hagn F, Pluckthun A, Brown A, Nasr ML, Wagner G | 10.1038/S41594-020-00554-6 | 2021-01-06 | 55355 | |
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 | 55361 | |
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 | 55353 | |
Gs | αs | Human | Engineered G alpha | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7JVQ | 7JVQ_refined | 3.0 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
apomorphine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine, dopamine, (-)-noradrenaline | small-molecule | Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP, Shen DD, Xu T, Liu YF, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE | 10.1016/J.CELL.2021.01.027 | 2021-02-24 | 55353 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7CKZ | - | 3.1 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
dopamine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
mevidalen pubchem gtoplig chembl_ligand drugbank |
small-molecule small-molecule |
Agonist PAM |
L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine, dopamine, (-)-noradrenaline | small-molecule | Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z | 10.1016/J.CELL.2021.01.028 | 2021-03-03 | 55353 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7CMU | - | 3.0 | DRD3 | D3 | Dopamine | A (Rhodopsin) | Human | BRIL | scFv16 | - |
pramipexole
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | dopamine | small-molecule | Xu P, Huang S, Mao C, Krumm BE, Zhou XE, Tan Y, Huang XP, Liu Y, Shen DD, Jiang Y, Yu X, Jiang H, Melcher K, Roth BL, Cheng X, Zhang Y, Xu HE | 10.1016/J.MOLCEL.2021.01.003 | 2021-03-10 | 55355 | |
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 | 55355 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7AUE | 7AUE_refined | 3.0 | MC4R | MC4 | Melanocortin | A (Rhodopsin) | Human | - | scFv16 | - |
setmelanotide
pubchem
gtoplig
drug_central
chembl_ligand
drugbank
|
peptide | Agonist | β-MSH, α-MSH, agouti-related protein, γ-MSH, ACTH | peptide | Israeli H, Degtjarik O, Fierro F, Chunilal V, Gill AK, Roth NJ, Botta J, Prabahar V, Peleg Y, Chan LF, Ben-Zvi D, McCormick PJ, Niv MY, Shalev-Benami M | 10.1126/SCIENCE.ABF7958 | 2021-04-28 | 55353 | |
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 | 55355 | |
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 | 55355 | |
Gs | αs | Human | - | 61 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7DUQ | - | 2.5 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
N-Tert-butyl-6,7-dichloroquinoxalin-2-amine
pubchem
CHEMBL410972 chembl_ligand pubchem pubchem |
small-molecule protein |
Ago-PAM Agonist |
glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | 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 | 55353 | |
Gs | αs | Human | - | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7EVM | - | 2.5 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
N-Tert-butyl-6,7-dichloroquinoxalin-2-amine
pubchem
|
small-molecule | Ago-PAM | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | 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 | 55353 | |
Gq/11 | αq | Human | Engineered G alpha | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7F9Y | - | 2.9 | GHSR | ghrelin | Ghrelin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
ghrelin
gtoplig
|
peptide | Agonist | [des-Gln14]ghrelin, ghrelin | peptide | Wang Y, Guo S, Zhuang Y, Yun Y, Xu P, He X, Guo J, Yin W, Xu HE, Xie X, Jiang Y | 10.1038/S41467-021-25364-2 | 2021-08-18 | 55363 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7EZK | - | 3.1 | CCKAR | CCK1 | Cholecystokinin | A (Rhodopsin) | Human | - | - | - |
CCK-8
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
peptide | Agonist | CCK-33, CCK-4, gastrin-17, CCK-39, desulfated cholecystokinin-8, CCK-8, CCK-58 | 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 | 55353 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7EW1 | 7EW1_refined | 3.4 | S1PR5 | S1P5 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
siponimod
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
small-molecule | Agonist | sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate | small-molecule | Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z | 10.1038/S41422-021-00566-X | 2021-09-29 | 55355 | |
Gs | αs | Bovine | - | 91 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7FIG | - | 3.9 | LSHR | LH | Glycoprotein hormone | A (Rhodopsin) | Human | - | Nanobody-35 | - |
Glycoprotein alpha
gtoplig
Choriogonadotropin beta gtoplig |
protein protein |
Agonist | 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 | 55370 | |
Gs | αs | Human | - | 55 | β1 | Human | γ2 | Human | Cryo-EM | 7RMH | 7RMH_refined | 3.1 | NK1R | NK1 | Tachykinin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
substance P
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
|
peptide | Agonist | substance P, hemokinin 1, neuropeptide-γ, neurokinin A, neurokinin B, neuropeptide K | peptide | Harris JA, Faust B, Gondin AB, Damgen MA, Suomivuori CM, Veldhuis NA, Cheng Y, Dror RO, Thal DM, Manglik A | 10.1038/S41589-021-00890-8 | 2021-11-03 | 55353 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7S8M | - | 2.5 | MRGX2 | MRGPRX2 | A orphans | A (Rhodopsin) | Human | BRIL | scFv16 | - |
Cortistatin 14
pubchem
|
peptide | Agonist | PAMP-20 | peptide | Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL | 10.1038/S41586-021-04126-6 | 2021-11-17 | 55355 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7VDM | 7VDM_refined | 3.0 | MRGX2 | MRGPRX2 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
substance P
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
|
peptide | Agonist | PAMP-20 | peptide | Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP | 10.1038/S41586-021-04077-Y | 2021-12-01 | 55355 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7VV3 | - | 3.0 | MRGX2 | MRGPRX2 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
Cortistatin 14
pubchem
|
peptide | Agonist | PAMP-20 | peptide | Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP | 10.1038/S41586-021-04077-Y | 2021-12-01 | 55355 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7NA8 | - | 2.7 | GHSR | ghrelin | Ghrelin | A (Rhodopsin) | Human | - | Antibody fragment | - |
ibutamoren
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | [des-Gln14]ghrelin, ghrelin | peptide | Liu H, Sun D, Myasnikov A, Damian M, Baneres JL, Sun J, Zhang C | 10.1038/S41467-021-26735-5 | 2021-12-15 | 55355 | |
Gs | αs | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7VUH | 7VUH_refined | 3.2 | GP139 | GPR139 | A orphans | A (Rhodopsin) | Human | - | Nanobody-35 | Xylanase |
JNJ-63533054
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | L-tryptophan, L-phenylalanine | small-molecule | Zhou Y, Daver H, Trapkov B, Wu L, Wu M, Harpsoe K, Gentry PR, Liu K, Larionova M, Liu J, Chen N, Brauner-Osborne H, Gloriam DE, Hua T, Liu ZJ | 10.1038/S41422-021-00591-W | 2021-12-29 | 55353 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7S1M | 7S1M_refined | 2.4 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
exendin-4
pubchem
gtoplig
pubchem
|
peptide | Agonist | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | Cary BP, Deganutti G, Zhao P, Truong TT, Piper SJ, Liu X, Belousoff MJ, Danev R, Sexton PM, Wootten D, Gellman SH | 10.1038/S41589-021-00945-W | 2022-01-05 | 55353 | |
Gs | αs | Human | - | 50 | β1 | Human | γ2 | Human | Cryo-EM | 7LLY | 7LLY_refined | 3.3 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
Pro-glucagon
pubchem
|
peptide | Agonist | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | Deganutti G, Liang YL, Zhang X, Khoshouei M, Clydesdale L, Belousoff MJ, Venugopal H, Truong TT, Glukhova A, Keller AN, Gregory KJ, Leach K, Christopoulos A, Danev R, Reynolds CA, Zhao P, Sexton PM, Wootten D | 10.1038/S41467-021-27760-0 | 2022-01-12 | 55353 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7EVZ | - | 3.1 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
cenerimod
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate | small-molecule | Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z | 10.1038/S41422-021-00566-X | 2021-09-29 | 55355 | |
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, γ-MSH, ACTH, 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 | 55353 | |
Gi/o | αi1 | Human | - | 61 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7T6V | 7T6V_refined | 3.1 | FPR2 | FPR2/ALX | Formylpeptide | A (Rhodopsin) | Human | - | scFv16 | - |
synthetic peptide
|
peptide | Agonist | serum amyloid A, aspirin triggered lipoxin A4, humanin, resolvin D1, LL-37, PrP106-126, annexin I, LXA4, aspirin-triggered resolvin D1 | peptide | Zhuang Y, Wang L, Guo J, Sun D, Wang Y, Liu W, Xu HE, Zhang C | 10.1038/S41467-022-28586-0 | 2022-03-30 | 55355 | |
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 | 55363 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7VL9 | - | 2.6 | CCR1 | CCR1 | Chemokine | A (Rhodopsin) | Human | - | scFv16 | - |
CCL15(26-92)
|
peptide | Agonist | CCL8, CCL23, CCL3, CCL7, CCL14, CCL15, CCL4, CCL13, CCL5, CCL16 | peptide | Shao Z, Shen Q, Yao B, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Ma H, Chen ZH, Xu HE, Ying S, Zhang Y, Shen H | 10.1038/S41589-021-00918-Z | 2022-03-23 | 55355 | |
Gi/o | αi1 | Mouse | - | 63 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7TD4 | - | 2.6 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | - | - |
siponimod
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
small-molecule | Agonist | sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate | small-molecule | Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY | 10.1038/S41467-022-28417-2 | 2022-02-09 | 55397 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7TYF | - | 2.2 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - |
Nanobody-35 RAMP1 |
- |
amylin peptide
|
peptide | Agonist | adrenomedullin 2/intermedin, amylin, β-CGRP, α-CGRP, calcitonin, adrenomedullin | 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 | 55353 | |
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 2/intermedin, amylin, β-CGRP, α-CGRP, calcitonin, adrenomedullin | 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 | 55353 | |
Gs | αs | Bovine | - | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7FIY | - | 3.4 | GIPR | GIP | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
tirzepatide
pubchem
gtoplig
|
peptide | Agonist | gastric inhibitory polypeptide | peptide | Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW | 10.1038/S41467-022-28683-0 | 2022-03-02 | 55370 | |
Gs | αs | Human | Mini-Gs | 58 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7VBI | - | 3.0 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | - | - |
tirzepatide
pubchem
gtoplig
|
peptide | Agonist | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW | 10.1038/S41467-022-28683-0 | 2022-03-02 | 55353 | |
Gi/o | αo | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7EJK | - | 3.4 | ADA2A | α2A | Adrenoceptors | A (Rhodopsin) | Human | - | scFv16 | - |
oxymetazoline
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline | small-molecule | Xu J, Cao S, Hubner H, Weikert D, Chen G, Lu Q, Yuan D, Gmeiner P, Liu Z, Du Y | 10.1126/SCIADV.ABJ5347 | 2022-04-13 | 55361 | |
Gi/o | αi2 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7WVX | - | 2.8 | FPR2 | FPR2/ALX | Formylpeptide | A (Rhodopsin) | Human | BRIL | - | - |
humanin
pubchem
gtoplig
chembl_ligand
pubchem
|
peptide | Agonist | serum amyloid A, aspirin triggered lipoxin A4, humanin, resolvin D1, LL-37, PrP106-126, annexin I, LXA4, aspirin-triggered resolvin D1 | peptide | Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B | 10.1038/S41467-022-29361-X | 2022-04-13 | 55356 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7SBF | - | 2.9 | OPRM | μ | Opioid | A (Rhodopsin) | Mouse | BRIL | scFv16 | - |
N-[(2S)-2-(dimethylamino)-3-(4-hydroxyphenyl)propyl]-N'-[(2S)-1-(thiophen-3-yl)propan-2-yl]urea
pubchem
|
small-molecule | Agonist | - | - | Wang H, Hetzer F, Huang W, Qu Q, Meyerowitz J, Kaindl J, Hubner H, Skiniotis G, Kobilka BK, Gmeiner P | 10.1002/ANIE.202200269 | 2022-04-20 | 55355 | |
Gs | αs | Human | - | 56 | β1 | Human | γ2 | Human | Cryo-EM | 7RBT | 7RBT_refined | 3.1 | GIPR | GIP | Glucagon | B1 (Secretin) | Human | - |
scFv16 Nanobody-35 |
- |
tirzepatide
pubchem
gtoplig
2-fluoro-4-[(1R)-6-methoxy-1-methyl-2-{(1S)-1-[4-(propan-2-yl)phenyl]ethyl}-1,2,3,4-tetrahydroisoquinolin-5-yl]-6-[(2-methylpropyl)amino]phenol pubchem |
peptide small-molecule |
Agonist PAM |
gastric inhibitory polypeptide | peptide | Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW | 10.1073/PNAS.2116506119 | 2022-04-13 | 55353 | |
Gs | αs | Human | Mini-Gs | 53 | β1 | Human | γ2 | Human | Cryo-EM | 7WU2 | - | 2.8 | AGRD1 | ADGRD1 | ADGRD | B2 (Adhesion) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Qu X, Qiu N, Wang M, Zhang B, Du J, Zhong Z, Xu W, Chu X, Ma L, Yi C, Han S, Shui W, Zhao Q, Wu B | 10.1038/S41586-022-04580-W | 2022-04-27 | 55353 | |
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 | 55355 | |
Gs | αs | Human | Mini-Gs | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7WUI | - | 3.1 | AGRG2 | ADGRG2 | ADGRG | B2 (Adhesion) | Mouse | - | - | - |
IP15
|
peptide | Agonist | - | - | Xiao P, Guo S, Wen X, He QT, Lin H, Huang SM, Gou L, Zhang C, Yang Z, Zhong YN, Yang CC, Li Y, Gong Z, Tao XN, Yang ZS, Lu Y, Li SL, He JY, Wang C, Zhang L, Kong L, Sun JP, Yu X | 10.1038/S41586-022-04590-8 | 2022-04-27 | 55353 | |
Gi/o | αi1 | Human | - | 63 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7S0F | - | 3.0 | ADRB1 | β1 | Adrenoceptors | A (Rhodopsin) | Wild turkey | - | - | - |
LEVISOPRENALINE
chembl_ligand
chembl_ligand
pubchem
|
small-molecule | Agonist | - | - | Alegre KO, Paknejad N, Su M, Lou JS, Huang J, Jordan KD, Eng ET, Meyerson JR, Hite RK, Huang XY | 10.1038/S41594-021-00679-2 | 2021-11-17 | 55355 | |
Gq/11 | αq | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7W56 | - | 2.9 | NMUR1 | NMU1 | Neuromedin U | A (Rhodopsin) | Human | - | scFv16 | - |
Neuromedin-S
|
peptide | Agonist | neuromedin S-33, neuromedin U-23, neuromedin U-25, neuromedin S-36 | peptide | You C, Zhang Y, Xu P, Huang S, Yin W, Eric Xu H, Jiang Y | 10.1038/S41467-022-29683-W | 2022-04-20 | 55363 | |
Gs | αs | Human | - | 54 | β1 | Human | γ2 | Human | Cryo-EM | 7EPT | - | 3.0 | AGRD1 | ADGRD1 | ADGRD | B2 (Adhesion) | Human | - | Nanobody-35 | - | - | - | - | - | - | Ping YQ, Xiao P, Yang F, Zhao RJ, Guo SC, Yan X, Wu X, Zhang C, Lu Y, Zhao F, Zhou F, Xi YT, Yin W, Liu FZ, He DF, Zhang DL, Zhu ZL, Jiang Y, Du L, Feng SQ, Schoneberg T, Liebscher I, Xu HE, Sun JP | 10.1038/S41586-022-04619-Y | 2022-05-11 | 55353 | |
Gs | αs | Bovine | - | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7EQ1 | - | 3.3 | AGRG5 | ADGRG5 | ADGRG | B2 (Adhesion) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Ping YQ, Xiao P, Yang F, Zhao RJ, Guo SC, Yan X, Wu X, Zhang C, Lu Y, Zhao F, Zhou F, Xi YT, Yin W, Liu FZ, He DF, Zhang DL, Zhu ZL, Jiang Y, Du L, Feng SQ, Schoneberg T, Liebscher I, Xu HE, Sun JP | 10.1038/S41586-022-04619-Y | 2022-05-11 | 55370 | |
Gi/o | αi1 | Human | - | 61 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7SQO | - | 3.2 | OX2R | OX2 | Orexin | A (Rhodopsin) | Human | - | scFv16 | - |
methyl (2R,3S)-3-[(methanesulfonyl)amino]-2-({[(1s,4S)-4-phenylcyclohexyl]oxy}methyl)piperidine-1-carboxylate
pubchem
|
small-molecule | Agonist | orexin-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 | 2022-05-25 | 55355 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7V6A | - | 3.6 | ACM4 | M4 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | scFv16 | - |
methyl 4-[4-(3-methyl-2-oxidanylidene-benzimidazol-1-yl)piperidin-1-yl]piperidine-1-carboxylate
pubchem
|
small-molecule | Allosteric agonist | acetylcholine | small-molecule | Wang J, Wu M, Chen Z, Wu L, Wang T, Cao D, Wang H, Liu S, Xu Y, Li F, Liu J, Chen N, Zhao S, Cheng J, Wang S, Hua T | 10.1038/S41467-022-30595-Y | 2022-05-11 | 55355 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7X9A | 7X9A_refined | 3.2 | NPY1R | Y1 | Neuropeptide Y | A (Rhodopsin) | Human | - | - | - |
neuropeptide Y
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
pubchem
pubchem
pubchem
|
peptide | Agonist | neuropeptide Y, pancreatic polypeptide, 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 | 55355 | |
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 | 55353 | |
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 | 55353 | |
Gi/o | αi1 | Human | - | 64 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7WIG | 7WIG_refined | 2.7 | SSR2 | SST2 | Somatostatin | A (Rhodopsin) | Human | - | scFv16 | - |
~{N}-[(2~{R})-1-[[(1~{R},3~{S})-3-(aminomethyl)cyclohexyl]methylamino]-3-(1~{H}-indol-3-yl)-1-oxidanylidene-propan-2-yl]spiro[indene-1,4'-piperidine]-1'-carboxamide
pubchem
|
small-molecule | Agonist | CST-17, cortistatin-14, SRIF-28, SRIF-14 | peptide | Chen LN, Wang WW, Dong YJ, Shen DD, Guo J, Yu X, Qin J, Ji SY, Zhang H, Shen Q, He Q, Yang B, Zhang Y, Li Q, Mao C | 10.1038/S41422-022-00669-Z | 2022-06-01 | 55355 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7F1O | - | 3.1 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
dopamine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine, dopamine, (-)-noradrenaline | small-molecule | Teng X, Chen S, Wang Q, Chen Z, Wang X, Huang N, Zheng S | 10.1126/SCIADV.ABO4158 | 2022-06-15 | 55353 | |
Gs | αs | Human | - | 57 | β1 | Human | γ2 | Human | Cryo-EM | 7F24 | - | 4.2 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | - | - |
dopamine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine, dopamine, (-)-noradrenaline | small-molecule | Teng X, Chen S, Wang Q, Chen Z, Wang X, Huang N, Zheng S | 10.1126/SCIADV.ABO4158 | 2022-06-15 | 55353 | |
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 drugbank |
small-molecule small-molecule |
Agonist PAM |
L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine, dopamine, (-)-noradrenaline | 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 | 55353 | |
Gi/o | αi2 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7WV9 | - | 3.4 | CNR1 | CB1 | Cannabinoid | A (Rhodopsin) | Human | - | scFv16 | - |
CP55940
pubchem
gtoplig
chembl_ligand
gtoplig
6-methyl-3-[(1S)-2-nitro-1-thiophen-2-yl-ethyl]-2-phenyl-1H-indole pubchem |
small-molecule small-molecule |
Agonist PAM |
2-arachidonoylglycerol, anandamide | small-molecule | Yang X, Wang X, Xu Z, Wu C, Zhou Y, Wang Y, Lin G, Li K, Wu M, Xia A, Liu J, Cheng L, Zou J, Yan W, Shao Z, Yang S | 10.1038/S41589-022-01038-Y | 2022-06-15 | 55356 | |
Gs | αs | Human | - | 60 | β1 | Rat | γ2 | Human | Cryo-EM | 7X8S | 7X8S_refined | 3.1 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
WB4-24
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | Cong Z, Zhou Q, Li Y, Chen LN, Zhang ZC, Liang A, Liu Q, Wu X, Dai A, Xia T, Wu W, Zhang Y, Yang D, Wang MW | 10.1073/PNAS.2200155119 | 2022-06-29 | 55353 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7XT8 | - | 3.1 | 5HT4R | 5-HT4 | 5-Hydroxytryptamine | A (Rhodopsin) | Human | BRIL | Nanobody-35 | - |
5-hydroxytryptamine
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE | 10.1016/J.MOLCEL.2022.05.031 | 2022-07-27 | 55353 | |
Gi/o | αo | Human | Mini-Go | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7UM5 | 7UM5_refined | 2.7 | 5HT5A | 5-HT5A | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | scFv16 | - |
5-CT
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL | 10.1038/S41594-022-00796-6 | 2022-07-20 | 55361 | |
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 | 55353 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7W0L | 7W0L_refined | 3.6 | APJ | apelin | Apelin | A (Rhodopsin) | Human | BRIL | scFv16 | - |
(1R,2S)-N-[4-(2,6-dimethoxyphenyl)-5-(6-methylpyridin-2-yl)-1,2,4-triazol-3-yl]-1-(5-methylpyrimidin-2-yl)-1-oxidanyl-propane-2-sulfonamide
pubchem
|
small-molecule | Agonist | Elabela/Toddler-11, [Pyr1]apelin-13, apelin-17, apelin-36, apelin-13, Elabela/Toddler-21, apelin receptor early endogenous ligand, Elabela/Toddler-32 | peptide | Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F | 10.1038/S41594-022-00797-5 | 2022-07-27 | 55355 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7W0O | 7W0O_refined | 3.8 | APJ | apelin | Apelin | A (Rhodopsin) | Human | BRIL | scFv16 | - |
apelin receptor early endogenous ligand
pubchem
|
peptide | Agonist | Elabela/Toddler-11, [Pyr1]apelin-13, apelin-17, apelin-36, apelin-13, Elabela/Toddler-21, apelin receptor early endogenous ligand, Elabela/Toddler-32 | peptide | Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F | 10.1038/S41594-022-00797-5 | 2022-07-27 | 55355 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7XOV | - | 3.0 | CCKAR | CCK1 | Cholecystokinin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
SR146131
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | CCK-33, CCK-4, gastrin-17, CCK-39, desulfated cholecystokinin-8, CCK-8, CCK-58 | 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 | 55353 | |
Gq/11 | αq | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7XOX | 7XOX_refined | 3.1 | GASR | CCK2 | Cholecystokinin | A (Rhodopsin) | Human | - | scFv16 | - |
CCK-8
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
peptide | Agonist | CCK-33, CCK-4, gastrin-71, desulfated gastrin-71, desulfated gastrin-14, gastrin-14, desulfated gastrin-17, gastrin-17, gastrin-34, CCK-39, desulfated gastrin-34, desulfated cholecystokinin-8, CCK-8, CCK-58 | 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 | 55363 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7XBW | 7XBW_refined | 2.8 | CX3C1 | CX3CR1 | Chemokine | A (Rhodopsin) | Human | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | CX3CL1 | peptide | Lu M, Zhao W, Han S, Lin X, Xu T, Tan Q, Wang M, Yi C, Chu X, Yang W, Zhu Y, Wu B, Zhao Q | 10.1126/SCIADV.ABN8048 | 2022-07-13 | 55355 | |
Gi/o | αi2 | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7LD3 | - | 3.2 | AA1R | A1 | Adenosine | A (Rhodopsin) | Human | - | - | - |
{2-Amino-4-[3,5-bis(trifluoromethyl)phenyl]thiophen-3-yl}(4-chlorophenyl)methanone
pubchem
adenosine pubchem gtoplig chembl_ligand drugbank drug_central |
small-molecule small-molecule |
Ago-PAM Agonist |
adenosine | small-molecule | Draper-Joyce CJ, Bhola R, Wang J, Bhattarai A, Nguyen ATN, Cowie-Kent I, O'Sullivan K, Chia LY, Venugopal H, Valant C, Thal DM, Wootten D, Panel N, Carlsson J, Christie MJ, White PJ, Scammells P, May LT, Sexton PM, Danev R, Miao Y, Glukhova A, Imlach WL, Christopoulos A | 10.1038/S41586-021-03897-2 | 2021-09-08 | 55356 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7EW2 | - | 3.1 | S1PR3 | S1P3 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
(S)-FTY720-phosphate
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate | small-molecule | Zhao C, Cheng L, Wang W, Wang H, Luo Y, Feng Y, Wang X, Fu H, Cai Y, Yang S, Fu P, Yan W, Shao Z | 10.1038/S41422-021-00567-W | 2021-09-29 | 55355 | |
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 | 55370 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7F54 | - | 3.0 | MC4R | MC4 | Melanocortin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
afamelanotide
pubchem
gtoplig
chembl_ligand
drugbank
pubchem
pubchem
pubchem
pubchem
|
peptide | Agonist | 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 | 55353 | |
Gq/11 | αq | Human | Gs-Gq chimera | 52 | β1 | Human | γ2 | Human | Cryo-EM | 7RMI | - | 3.2 | NK1R | NK1 | Tachykinin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
substance P
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
|
peptide | Agonist | substance P, hemokinin 1, neuropeptide-γ, neurokinin A, neurokinin B, neuropeptide K | peptide | Harris JA, Faust B, Gondin AB, Damgen MA, Suomivuori CM, Veldhuis NA, Cheng Y, Dror RO, Thal DM, Manglik A | 10.1038/S41589-021-00890-8 | 2021-11-03 | 55363 | |
Gq/11 | αq | Human | Gq-Gs chimera | 57 | β1 | Human | γ2 | Human | Cryo-EM | 7S8L | - | 2.5 | MRGX2 | MRGPRX2 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
Cortistatin 14
pubchem
|
peptide | Agonist | PAMP-20 | peptide | Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL | 10.1038/S41586-021-04126-6 | 2021-11-17 | 55363 | |
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 | 55355 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7VUY | - | 2.8 | MRGX2 | MRGPRX2 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
PAMP-12
pubchem
|
peptide | Agonist | PAMP-20 | peptide | Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP | 10.1038/S41586-021-04077-Y | 2021-12-01 | 55355 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7NA7 | 7NA7_refined | 2.7 | GHSR | ghrelin | Ghrelin | A (Rhodopsin) | Human | - | Antibody fragment | - |
Ghrelin-27
|
peptide | Agonist | [des-Gln14]ghrelin, ghrelin | peptide | Liu H, Sun D, Myasnikov A, Damian M, Baneres JL, Sun J, Zhang C | 10.1038/S41467-021-26735-5 | 2021-12-15 | 55355 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7VUI | 7VUI_refined | 3.3 | GP139 | GPR139 | A orphans | A (Rhodopsin) | Human | - | Nanobody-35 | Xylanase |
JNJ-63533054
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | L-tryptophan, L-phenylalanine | small-molecule | Zhou Y, Daver H, Trapkov B, Wu L, Wu M, Harpsoe K, Gentry PR, Liu K, Larionova M, Liu J, Chen N, Brauner-Osborne H, Gloriam DE, Hua T, Liu ZJ | 10.1038/S41422-021-00591-W | 2021-12-29 | 55353 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7S3I | - | 2.5 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
exendin-4
pubchem
gtoplig
pubchem
|
peptide | Agonist | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | Cary BP, Deganutti G, Zhao P, Truong TT, Piper SJ, Liu X, Belousoff MJ, Danev R, Sexton PM, Wootten D, Gellman SH | 10.1038/S41589-021-00945-W | 2022-01-05 | 55353 | |
Gi/o | αi1 | Human | - | 40 | β1 | Human | γ2 | Human | Cryo-EM | 7WF7 | 7WF7_refined | 3.4 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
sphingosine 1-phosphate
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate | small-molecule | Xu Z, Ikuta T, Kawakami K, Kise R, Qian Y, Xia R, Sun MX, Zhang A, Guo C, Cai XH, Huang Z, Inoue A, He Y | 10.1038/S41589-021-00930-3 | 2022-01-05 | 55355 | |
Gq/11 | α11 | Human | - | 97 | β1 | Human | γ2 | Human | Cryo-EM | 7RKF | - | 4.0 | US28 | US28 | Unclassified | A (Rhodopsin) | strain AD169 | - | scFv16 | - |
Fractalkine
pubchem
|
peptide | Agonist | - | - | Tsutsumi N, Maeda S, Qu Q, Vogele M, Jude KM, Suomivuori CM, Panova O, Waghray D, Kato HE, Velasco A, Dror RO, Skiniotis G, Kobilka BK, Garcia KC | 10.1126/SCIADV.ABL5442 | 2022-01-26 | 55364 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7EW0 | 7EW0_refined | 3.4 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
ozanimod
pubchem
gtoplig
drug_central
chembl_ligand
drugbank
|
small-molecule | Agonist | sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate | small-molecule | Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z | 10.1038/S41422-021-00566-X | 2021-09-29 | 55355 | |
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, γ-MSH, ACTH, 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 | 55353 | |
Gi/o | αi1 | Human | - | 61 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7T6S | 7T6S_refined | 3.0 | FPR2 | FPR2/ALX | Formylpeptide | A (Rhodopsin) | Human | - | scFv16 | - |
N-(4-chlorophenyl)-N'-[1-methyl-3-oxo-2-phenyl-5-(propan-2-yl)-2,3-dihydro-1H-pyrazol-4-yl]urea
pubchem
|
small-molecule | Agonist | serum amyloid A, aspirin triggered lipoxin A4, humanin, resolvin D1, LL-37, PrP106-126, annexin I, LXA4, aspirin-triggered resolvin D1 | peptide | Zhuang Y, Wang L, Guo J, Sun D, Wang Y, Liu W, Xu HE, Zhang C | 10.1038/S41467-022-28586-0 | 2022-03-30 | 55355 | |
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 | CST-17, cortistatin-14, SRIF-28, SRIF-14 | peptide | Robertson MJ, Meyerowitz JG, Panova O, Borrelli K, Skiniotis G | 10.1038/S41594-022-00727-5 | 2022-03-09 | 55357 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7VL8 | 7VL8_refined | 2.9 | CCR1 | CCR1 | Chemokine | A (Rhodopsin) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | CCL8, CCL23, CCL3, CCL7, CCL14, CCL15, CCL4, CCL13, CCL5, CCL16 | peptide | Shao Z, Shen Q, Yao B, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Ma H, Chen ZH, Xu HE, Ying S, Zhang Y, Shen H | 10.1038/S41589-021-00918-Z | 2022-03-23 | 55355 | |
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 | 55397 | |
Gi/o | αi1 | Mouse | - | 62 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7TD2 | - | 3.1 | LPAR1 | LPA1 | Lysophospholipid (LPA) | A (Rhodopsin) | Human | - | - | - |
lysophosphatidic acid
pubchem
|
small-molecule | Agonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY | 10.1038/S41467-022-28417-2 | 2022-02-09 | 55397 | |
Gi/o | αi1 | Human | - | 62 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7VGZ | 7VGZ_refined | 3.3 | MTR1A | MT1 | Melatonin | A (Rhodopsin) | Human | - | scFv16 | - |
ramelteon
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | melatonin | small-molecule | Wang Q, Lu Q, Guo Q, Teng M, Gong Q, Li X, Du Y, Liu Z, Tao Y | 10.1038/S41467-022-28111-3 | 2022-03-02 | 55355 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7TYH | - | 3.3 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - | Nanobody-35 | - |
Calcitonin human
pubchem
chembl_ligand
drugbank
|
peptide | Agonist | adrenomedullin 2/intermedin, amylin, β-CGRP, α-CGRP, calcitonin, adrenomedullin | 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 | 55353 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7TYN | - | 2.6 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - | Nanobody-35 | - |
calcitonin (salmon synthetic)
pubchem
|
small-molecule | Agonist | adrenomedullin 2/intermedin, amylin, β-CGRP, α-CGRP, calcitonin, adrenomedullin | 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 | 55353 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7TYY | - | 3.0 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - | Nanobody-35 | - |
calcitonin (salmon synthetic)
pubchem
|
small-molecule | Agonist | adrenomedullin 2/intermedin, amylin, β-CGRP, α-CGRP, calcitonin, adrenomedullin | 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 | 55353 | |
Gs | αs | Bovine | - | 57 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7FIM | - | 3.4 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
tirzepatide
pubchem
gtoplig
|
peptide | Agonist | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW | 10.1038/S41467-022-28683-0 | 2022-03-02 | 55370 | |
Gi/o | αo | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7EJA | - | 3.6 | ADA2A | α2A | Adrenoceptors | A (Rhodopsin) | Human | - | scFv16 | - |
dexmedetomidine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline | small-molecule | Xu J, Cao S, Hubner H, Weikert D, Chen G, Lu Q, Yuan D, Gmeiner P, Liu Z, Du Y | 10.1126/SCIADV.ABJ5347 | 2022-04-13 | 55361 | |
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 | serum amyloid A, aspirin triggered lipoxin A4, humanin, resolvin D1, LL-37, PrP106-126, annexin I, LXA4, aspirin-triggered resolvin D1 | peptide | Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B | 10.1038/S41467-022-29361-X | 2022-04-13 | 55356 | |
Gq/11 | αq | Human | - | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7WQ4 | 7WQ4_refined | 2.6 | GALR2 | GAL2 | Galanin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
galanin
pubchem
gtoplig
chembl_ligand
gtoplig
pubchem
pubchem
pubchem
pubchem
|
peptide | Agonist | galanin-like peptide, spexin-1, galanin | peptide | Duan J, Shen DD, Zhao T, Guo S, He X, Yin W, Xu P, Ji Y, Chen LN, Liu J, Zhang H, Liu Q, Shi Y, Cheng X, Jiang H, Eric Xu H, Zhang Y, Xie X, Jiang Y | 10.1038/S41467-022-29072-3 | 2022-04-20 | 55363 | |
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 | 55355 | |
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 | 55353 | |
Gs | αs | Human | Mini-Gs | 56 | β1 | Human | γ2 | Human | Cryo-EM | 7UTZ | - | 2.4 | TSHR | TSH | Glycoprotein hormone | A (Rhodopsin) | Human | - | Nanobody-35 | - |
Thyrotropin subunit beta
Glycoprotein hormones alpha chain analog TR1402 |
protein protein |
Agonist | TSH | peptide | Faust B, Billesbolle CB, Suomivuori CM, Singh I, Zhang K, Hoppe N, Pinto AFM, Diedrich JK, Muftuoglu Y, Szkudlinski MW, Saghatelian A, Dror RO, Cheng Y, Manglik A | 10.1038/S41586-022-05159-1 | 2022-08-03 | 55353 | |
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 | CST-17, cortistatin-14, SRIF-28, SRIF-14 | peptide | Chen S, Teng X, Zheng S | 10.1038/S41589-022-01130-3 | 2022-10-19 | 55363 | |
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 | 55355 | |
Gi/o | αi1 | Human | - | 63 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7YU6 | 7YU6_refined | 3.5 | LPAR1 | LPA1 | Lysophospholipid (LPA) | A (Rhodopsin) | Human | - | scFv16 | - |
[(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate
pubchem
|
small-molecule | Agonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O | 10.1038/S41467-022-33121-2 | 2022-10-05 | 55355 | |
Gq/11 | αq | Human | Gs-mini-Gq chimera | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8DWC | - | 2.9 | MRGX1 | MRGPRX1 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
Proenkephalin-A
|
peptide | Agonist | bovine adrenal medulla peptide 8-22 | peptide | Liu Y, Cao C, Huang XP, Gumpper RH, Rachman MM, Shih SL, Krumm BE, Zhang S, Shoichet BK, Fay JF, Roth BL | 10.1038/S41589-022-01173-6 | 2022-11-02 | 55363 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8E3X | 8E3X_refined | 2.3 | PACR | PAC1 | VIP and PACAP | B1 (Secretin) | Human | - | Nanobody-35 | - |
[Ac-His1]PACAP-27
gtoplig
chembl_ligand
pubchem
|
peptide | Agonist | PACAP-27, PACAP-38, VIP, PHV, PHM, PHI | peptide | Piper SJ, Deganutti G, Lu J, Zhao P, Liang YL, Lu Y, Fletcher MM, Hossain MA, Christopoulos A, Reynolds CA, Danev R, Sexton PM, Wootten D | 10.1038/S41467-022-34629-3 | 2022-11-23 | 55353 | |
Gq/11 | αq | Human | Mini-Gq | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8E9W | - | 2.7 | ACM3 | M3 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | scFv16 | - |
CHEMBL73538
chembl_ligand
pubchem
|
small-molecule | Agonist | acetylcholine | small-molecule | Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL | 10.1038/S41586-022-05489-0 | 2022-11-30 | 55363 | |
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 | 55363 | |
Gi/o | αi1 | Human | - | 64 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8EF6 | 8EF6_refined | 3.2 | OPRM | μ | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
morphine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | endomorphin-1, endomorphin-2, [Met]enkephalin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin A-(1-8), dynorphin B | 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 | 55355 | |
Gi/o | αi1 | Human | - | 61 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8EFQ | - | 3.3 | OPRM | μ | Opioid | A (Rhodopsin) | Human | - | - | - |
DAMGO
pubchem
gtoplig
chembl_ligand
chembl_ligand
|
peptide | Agonist | endomorphin-1, endomorphin-2, [Met]enkephalin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin A-(1-8), dynorphin B | 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 | 55355 | |
Gi/o | αi1 | Human | - | 64 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8F7Q | - | 3.2 | OPRM | μ | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
β-endorphin
pubchem
gtoplig
chembl_ligand
pubchem
|
peptide | Agonist | endomorphin-1, endomorphin-2, [Met]enkephalin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin A-(1-8), dynorphin B | 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 | 55355 | |
Gs | αs | Bovine | - | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8HA0 | - | 2.6 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
teriparatide
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
pubchem
pubchem
pubchem
pubchem
pubchem
|
peptide | Agonist | PTH, PTHrP-(1-36), TIP39, PTHrP | 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 | 55370 | |
Gq/11 | αq | Human | - | 97 | β1 | Human | γ2 | Human | Cryo-EM | 7F6G | 7F6G_refined | 2.9 | AGTR1 | AT1 | Angiotensin | A (Rhodopsin) | Human | - | - | - |
SAR1-AngII
|
peptide | Agonist | angiotensin A, angiotensin II, angiotensin IV, angiotensin III | peptide | - | - | 2023-03-29 | 55363 | |
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 | relaxin-3, relaxin-3 (B chain), INSL5 | peptide | Chen Y, Zhou Q, Wang J, Xu Y, Wang Y, Yan J, Wang Y, Zhu Q, Zhao F, Li C, Chen CW, Cai X, Bathgate RAD, Shen C, Eric Xu H, Yang D, Liu H, Wang MW | 10.1038/S41467-023-36182-Z | 2023-03-01 | 55356 | |
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 | neuropeptide Y, PYY-(3-36), peptide YY, neuropeptide Y-(3-36), pancreatic polypeptide | 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 | 55355 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7Y66 | - | 2.9 | C5AR1 | C5a1 | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
BM213
|
peptide | Agonist | C5a des-Arg, ribosomal protein S19, C5a, 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 | 55355 | |
Gi/o | αo | Human | Mini-Go | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8FN0 | - | 2.9 | NTR1 | NTS1 | Neurotensin | A (Rhodopsin) | Rat | - | scFv16 | - |
neurotensin
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
CHEMBL4576388 chembl_ligand pubchem |
peptide small-molecule |
Agonist PAM |
neuromedin N, neurotensin | peptide | Krumm BE, DiBerto JF, Olsen RHJ, Kang HJ, Slocum ST, Zhang S, Strachan RT, Huang XP, Slosky LM, Pinkerton AB, Barak LS, Caron MG, Kenakin T, Fay JF, Roth BL | 10.1021/ACS.BIOCHEM.3C00029 | 2023-03-29 | 55361 | |
Gq/11 | αq | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8G59 | 8G59_refined | 2.6 | FFAR4 | FFA4 | Free fatty acid | A (Rhodopsin) | Human | - | - | - |
TUG-891
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | myristic acid, oleic acid, α-linolenic acid, linoleic acid | small-molecule | Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP | 10.1126/SCIENCE.ADD6220 | 2023-03-08 | 55363 | |
G12/13 | α13 | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8H8J | 8H8J_refined | 3.2 | GPR35 | GPR35 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
lodoxamide
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
small-molecule | Agonist | 2-Oleoyllysophosphatydic acid, 2-oleoyl-LPA, kynurenic acid, 1-Lyso-2-oleoyl-phosphatidic acid | small-molecule | Duan J, Liu Q, Yuan Q, Ji Y, Zhu S, Tan Y, He X, Xu Y, Shi J, Cheng X, Jiang H, Eric Xu H, Jiang Y | 10.1038/S41421-022-00499-8 | 2023-02-08 | 55368 | |
Gq/11 | αq | Human | - | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8HCQ | 8HCQ_refined | 3.0 | EDNRA | ETA | Endothelin | A (Rhodopsin) | Human | - | scFv16 | - |
ENDOTHELIN
chembl_ligand
pubchem
|
protein | Agonist | endothelin-3, endothelin-2, endothelin-1 | peptide | - | - | 2023-03-22 | 55363 | |
Gs | αs | Human | Mini-Gs | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8HDP | - | 3.2 | AA2BR | A2B | Adenosine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
adenosine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | adenosine | small-molecule | Cai H, Xu Y, Guo S, He X, Sun J, Li X, Li C, Yin W, Cheng X, Jiang H, Xu HE, Xie X, Jiang Y | 10.1038/S41421-022-00503-1 | 2023-01-18 | 55353 | |
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 | 55353 | |
Gs | αs | Human | fused Gs | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8I2G | - | 2.8 | FSHR | FSH | Glycoprotein hormone | A (Rhodopsin) | Human | - | Nanobody-35 | - |
Follitropin subunit beta
Glycoprotein alpha FSHR agonist 1 pubchem |
peptide peptide small-molecule |
Agonist | FSH | peptide | Duan J, Xu P, Zhang H, Luan X, Yang J, He X, Mao C, Shen DD, Ji Y, Cheng X, Jiang H, Jiang Y, Zhang S, Zhang Y, Xu HE | 10.1038/S41467-023-36170-3 | 2023-03-29 | 55353 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8FLT | - | 3.0 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
M-PTH(1-14)
|
peptide | Agonist | PTH, PTHrP-(1-36), TIP39, PTHrP | 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 | 55353 | |
Gi/o | αi1 | Human | - | 63 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8HK5 | 8HK5_refined | 3.0 | C5AR1 | C5a1 | Complement peptide | A (Rhodopsin) | Human | - | - | - |
C5a
gtoplig
|
peptide | Agonist | C5a des-Arg, ribosomal protein S19, C5a, C3a | peptide | Wang Y, Liu W, Xu Y, He X, Yuan Q, Luo P, Fan W, Zhu J, Zhang X, Cheng X, Jiang Y, Xu HE, Zhuang Y | 10.1038/S41589-023-01339-W | 2023-05-10 | 55355 | |
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 | PTH, PTHrP-(1-36), TIP39, PTHrP | peptide | - | - | 2023-07-05 | 55353 | |
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 | 55367 | |
Gq/11 | αq | Human | Mini-Gq | 51 | - | - | - | - | Cryo-EM | 7YMH | 7YMH_refined | 3.5 | ADA1A | α1A | Adrenoceptors | A (Rhodopsin) | Human | - | Nanobody-29 | - |
Noradrenaline
pubchem
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline | small-molecule | Toyoda Y, Zhu A, Kong F, Shan S, Zhao J, Wang N, Sun X, Zhang L, Yan C, Kobilka BK, Liu X | 10.1038/S41467-023-39310-X | 2023-07-05 | 55363 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8F0K | - | 1.9 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - |
Nanobody-35 RAMP3 |
- |
San385
|
peptide | Agonist | adrenomedullin 2/intermedin, amylin, β-CGRP, α-CGRP, calcitonin, adrenomedullin | 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 | 55353 | |
Gq/11 | αq | Human | - | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8H0P | - | 3.2 | NMBR | BB1 | Bombesin | A (Rhodopsin) | Human | - | scFv16 | - |
NMB30
|
peptide | Agonist | gastrin releasing peptide(14-27) (human), neuromedin B, gastrin-releasing peptide, GRP-(18-27) | peptide | - | - | 2023-08-09 | 55363 | |
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 | 55353 | |
Gs | αs | Human | Mini-Gs | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8IRR | - | 3.2 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
rotigotine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine, dopamine, (-)-noradrenaline | 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 | 55353 | |
Gi/o | αi1 | Human | - | 62 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8IY5 | - | 2.8 | EDNRB | ETB | Endothelin | A (Rhodopsin) | Human | - | scFv16 | - |
ENDOTHELIN
chembl_ligand
pubchem
|
protein | Agonist | endothelin-3, endothelin-2, endothelin-1 | peptide | Sano FK, Akasaka H, Shihoya W, Nureki O | 10.7554/ELIFE.85821 | 2023-08-16 | 55355 | |
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 | 55355 | |
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 | 55353 | |
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 |
neuromedin N, large neurotensin, neurotensin, large neuromedin N | peptide | Duan J, Liu H, Zhao F, Yuan Q, Ji Y, Cai X, He X, Li X, Li J, Wu K, Gao T, Zhu S, Lin S, Wang MW, Cheng X, Yin W, Jiang Y, Yang D, Xu HE | 10.1038/S41586-023-06395-9 | 2023-08-09 | 55363 | |
Gq/11 | αq | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7YFC | - | 3.0 | HRH4 | H4 | Histamine | A (Rhodopsin) | Human | - |
scFv16 Nanobody-35 |
- |
histamine
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
gtoplig
|
small-molecule | Agonist | 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 | 55363 | |
Gi/o | αi1 | Human | - | 56 | β1 | Human | γ2 | Human | Cryo-EM | 8GCM | - | 3.5 | PE2R4 | EP4 | Prostanoid | A (Rhodopsin) | Human | - | scFv16 | - |
(5S)-5-[(3R)-4,4-difluoro-3-hydroxy-4-phenylbutyl]-1-[6-(1H-tetrazol-5-yl)hexyl]pyrrolidin-2-one
pubchem
|
lipid | Agonist | thromboxane A2, PGD2, PGE1, PGE2, PGI2, PGF2α | small-molecule | Huang SM, Xiong MY, Liu L, Mu J, Wang MW, Jia YL, Cai K, Tie L, Zhang C, Cao S, Wen X, Wang JL, Guo SC, Li Y, Qu CX, He QT, Cai BY, Xue C, Gan S, Xie Y, Cong X, Yang Z, Kong W, Li S, Li Z, Xiao P, Yang F, Yu X, Guan YF, Zhang X, Liu Z, Yang BX, Du Y, Sun JP | 10.1073/PNAS.2216329120 | 2024-01-03 | 55355 | |
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, PGD2, PGE1, PGE2, PGI2, PGF2α | 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 | 55353 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8HNM | - | 2.9 | CXCR3 | CXCR3 | Chemokine | A (Rhodopsin) | Human | - | scFv16 | - |
CHEMBL2220409
chembl_ligand
chembl_ligand
pubchem
|
small-molecule | Agonist | CXCL11, CXCL9, CXCL12α, CCL19, CCL20, CCL7, CCL11, CXCL10, CCL13, CCL5 | 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 | 55355 | |
Gi/o | αo | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8HQC | - | 3.9 | C5AR1 | C5a1 | Complement peptide | A (Rhodopsin) | Mouse | - | - | fragment |
C5a
gtoplig
|
peptide | Agonist | - | - | None | HTTPS://DOI.ORG/10.1016/J.CELL.2023.09.020 | 2023-10-18 | 55361 | |
Gi/o | αi1 | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8HVI | 8HVI_refined | 3.0 | GP132 | GPR132 | A orphans | A (Rhodopsin) | Human | BRIL | scFv16 | - |
NOX-6-7
pubchem
gtoplig
|
small-molecule | Agonist | 9-hydroxyoctadecadienoic acid | small-molecule | Wang JL, Dou XD, Cheng J, Gao MX, Xu GF, Ding W, Ding JH, Li Y, Wang SH, Ji ZW, Zhao XY, Huo TY, Zhang CF, Liu YM, Sha XY, Gao JR, Zhang WH, Hao Y, Zhang C, Sun JP, Jiao N, Yu X | 10.1038/S42255-023-00899-4 | 2023-10-11 | 55355 | |
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 | 55361 | |
Gi/o | αi1 | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8U1U | - | 3.1 | CCR8 | CCR8 | Chemokine | A (Rhodopsin) | Human | - | scFv16 | - |
CCL1
|
protein | Agonist | CCL8, CCL1 | peptide | - | - | 2023-12-20 | 55355 | |
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, tyramine, 3-iodothyronamine | 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 | 55353 | |
Gs | αs | Human | - | 56 | β1 | Human | γ2 | Human | Cryo-EM | 8WC8 | - | 2.9 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Human | - | scFv16 | - |
CHEMBL476516
chembl_ligand
pubchem
|
small-molecule | Agonist | octopamine, tyramine, β-phenylethylamine, 3-iodothyronamine, dopamine, CHEMBL1160703, (+)-Octopamine | 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 | 55353 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7EW4 | 7EW4_refined | 3.2 | S1PR3 | S1P3 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
CYM-5541
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate | small-molecule | Zhao C, Cheng L, Wang W, Wang H, Luo Y, Feng Y, Wang X, Fu H, Cai Y, Yang S, Fu P, Yan W, Shao Z | 10.1038/S41422-021-00567-W | 2021-09-29 | 55355 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7RTB | 7RTB_refined | 2.1 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
Peptide-19
|
peptide | Agonist | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | Johnson RM, Zhang X, Piper SJ, Nettleton TJ, Vandekolk TH, Langmead CJ, Danev R, Sexton PM, Wootten D | 10.1016/J.BBRC.2021.09.016 | 2021-10-06 | 55353 | |
Gi/o | αi2 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7F8V | - | 3.3 | GASR | CCK2 | Cholecystokinin | A (Rhodopsin) | Human | - | - | - |
desulfated gastrin-17
pubchem
gtoplig
chembl_ligand
pubchem
|
peptide | Agonist | CCK-33, CCK-4, gastrin-71, desulfated gastrin-71, desulfated gastrin-14, gastrin-14, desulfated gastrin-17, gastrin-17, gastrin-34, CCK-39, desulfated gastrin-34, desulfated cholecystokinin-8, CCK-8, CCK-58 | 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 | 55356 | |
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 | 55353 | |
Gq/11 | αq | Human | Gs-Gq chimera | 52 | β1 | Human | γ2 | Human | Cryo-EM | 7RMG | - | 3.0 | NK1R | NK1 | Tachykinin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
substance P
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
|
peptide | Agonist | substance P, hemokinin 1, neuropeptide-γ, neurokinin A, neurokinin B, neuropeptide K | peptide | Harris JA, Faust B, Gondin AB, Damgen MA, Suomivuori CM, Veldhuis NA, Cheng Y, Dror RO, Thal DM, Manglik A | 10.1038/S41589-021-00890-8 | 2021-11-03 | 55363 | |
Gs | αs | Human | - | 46 | β1 | Rat | γ2 | Mouse | Cryo-EM | 7PIV | 7PIV_refined | 2.9 | MC4R | MC4 | Melanocortin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
afamelanotide
pubchem
gtoplig
chembl_ligand
drugbank
pubchem
pubchem
pubchem
pubchem
|
peptide | Agonist | β-MSH, α-MSH, agouti-related protein, γ-MSH, ACTH | peptide | Heyder NA, Kleinau G, Speck D, Schmidt A, Paisdzior S, Szczepek M, Bauer B, Koch A, Gallandi M, Kwiatkowski D, Burger J, Mielke T, Beck-Sickinger AG, Hildebrand PW, Spahn CMT, Hilger D, Schacherl M, Biebermann H, Hilal T, Kuhnen P, Kobilka BK, Scheerer P | 10.1038/S41422-021-00569-8 | 2021-11-17 | 55353 | |
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 | 55363 | |
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 | 55355 | |
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 | 55355 | |
Gq/11 | αq | Human | Gq-Gs-Gi1 chimera | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7P00 | - | 2.7 | NK1R | NK1 | Tachykinin | A (Rhodopsin) | Human | - | scFv16 | - |
substance P
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
|
peptide | Agonist | substance P, hemokinin 1, neuropeptide-γ, neurokinin A, neurokinin B, neuropeptide K | peptide | Thom C, Ehrenmann J, Vacca S, Waltenspuhl Y, Schoppe J, Medalia O, Pluckthun A | 10.1126/SCIADV.ABK2872 | 2021-12-15 | 55363 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7VUJ | 7VUJ_refined | 3.8 | GP139 | GPR139 | A orphans | A (Rhodopsin) | Human | - | Nanobody-35 | Xylanase |
JNJ-63533054
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | L-tryptophan, L-phenylalanine | small-molecule | Zhou Y, Daver H, Trapkov B, Wu L, Wu M, Harpsoe K, Gentry PR, Liu K, Larionova M, Liu J, Chen N, Brauner-Osborne H, Gloriam DE, Hua T, Liu ZJ | 10.1038/S41422-021-00591-W | 2021-12-29 | 55353 | |
Gi/o | αi1 | Human | - | 43 | β1 | Human | γ2 | Human | Cryo-EM | 7EO4 | 7EO4_refined | 2.9 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
siponimod
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
small-molecule | Agonist | sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate | small-molecule | Xu Z, Ikuta T, Kawakami K, Kise R, Qian Y, Xia R, Sun MX, Zhang A, Guo C, Cai XH, Huang Z, Inoue A, He Y | 10.1038/S41589-021-00930-3 | 2022-01-05 | 55355 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7LLL | - | 3.7 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
exendin-4
pubchem
gtoplig
pubchem
|
peptide | Agonist | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | Deganutti G, Liang YL, Zhang X, Khoshouei M, Clydesdale L, Belousoff MJ, Venugopal H, Truong TT, Glukhova A, Keller AN, Gregory KJ, Leach K, Christopoulos A, Danev R, Reynolds CA, Zhao P, Sexton PM, Wootten D | 10.1038/S41467-021-27760-0 | 2022-01-12 | 55353 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7RKN | - | 3.6 | US28 | US28 | Unclassified | A (Rhodopsin) | strain AD169 | - | scFv16 | - |
Fractalkine
pubchem
|
peptide | Agonist | - | - | Tsutsumi N, Maeda S, Qu Q, Vogele M, Jude KM, Suomivuori CM, Panova O, Waghray D, Kato HE, Velasco A, Dror RO, Skiniotis G, Kobilka BK, Garcia KC | 10.1126/SCIADV.ABL5442 | 2022-01-26 | 55355 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7EVY | - | 3.0 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
siponimod
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
small-molecule | Agonist | sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate | small-molecule | Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z | 10.1038/S41422-021-00566-X | 2021-09-29 | 55355 | |
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, γ-MSH, ACTH, 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 | 55353 | |
Gi/o | αi1 | Human | - | 61 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7T6T | 7T6T_refined | 3.2 | FPR1 | FPR1 | Formylpeptide | A (Rhodopsin) | Human | - | - | - |
synthetic peptide
|
peptide | Agonist | annexin I, fMet-Leu-Phe, spinorphin, cathepsin G | 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 | 55355 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7VGX | 7VGX_refined | 3.2 | NPY1R | Y1 | Neuropeptide Y | A (Rhodopsin) | Human | - | scFv16 | - |
neuropeptide Y
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
pubchem
pubchem
pubchem
|
peptide | Agonist | neuropeptide Y, pancreatic polypeptide, peptide YY | 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 | 55355 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7VKT | 7VKT_refined | 2.9 | LT4R1 | BLT1 | Leukotriene | A (Rhodopsin) | Human | - | scFv16 | - |
LTB4
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | 20-hydroxy-LTB4, 12R-HETE, LTB4 | small-molecule | Wang N, He X, Zhao J, Jiang H, Cheng X, Xia Y, Eric Xu H, He Y | 10.1038/S41467-022-28820-9 | 2022-03-09 | 55355 | |
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 | 55397 | |
Gi/o | αi1 | Mouse | - | 63 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7TD3 | - | 3.0 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | - | - |
sphingosine 1-phosphate
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate | small-molecule | Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY | 10.1038/S41467-022-28417-2 | 2022-02-09 | 55397 | |
Gi/o | αi1 | Human | - | 61 | β1 | Rat | γ2 | Human | Cryo-EM | 7VH0 | 7VH0_refined | 3.5 | MTR1B | MT2 | Melatonin | A (Rhodopsin) | Human | - | scFv16 | - |
ramelteon
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | melatonin | small-molecule | Wang Q, Lu Q, Guo Q, Teng M, Gong Q, Li X, Du Y, Liu Z, Tao Y | 10.1038/S41467-022-28111-3 | 2022-03-02 | 55355 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7TYI | - | 3.3 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - | Nanobody-35 | - |
Amylin rat
pubchem
|
peptide | Agonist | adrenomedullin 2/intermedin, amylin, β-CGRP, α-CGRP, calcitonin, adrenomedullin | 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 | 55353 | |
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 2/intermedin, amylin, β-CGRP, α-CGRP, calcitonin, adrenomedullin | 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 | 55353 | |
Gs | αs | Bovine | - | 59 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7FIN | - | 3.1 | GIPR | GIP | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
Peptide-20
|
peptide | Agonist | gastric inhibitory polypeptide | peptide | Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW | 10.1038/S41467-022-28683-0 | 2022-02-23 | 55370 | |
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 | 55353 | |
Gi/o | αo | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7EJ8 | - | 3.0 | ADA2A | α2A | Adrenoceptors | A (Rhodopsin) | Human | - | scFv16 | - |
brimonidine (UK14304)
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline | small-molecule | Xu J, Cao S, Hubner H, Weikert D, Chen G, Lu Q, Yuan D, Gmeiner P, Liu Z, Du Y | 10.1126/SCIADV.ABJ5347 | 2022-04-13 | 55361 | |
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 | serum amyloid A, aspirin triggered lipoxin A4, humanin, resolvin D1, LL-37, PrP106-126, annexin I, LXA4, aspirin-triggered resolvin D1 | peptide | Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B | 10.1038/S41467-022-29361-X | 2022-04-13 | 55356 | |
Gi/o | αi1 | Human | - | 64 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7WQ3 | 7WQ3_refined | 2.7 | GALR1 | GAL1 | Galanin | A (Rhodopsin) | Human | - | scFv16 | - |
galanin
pubchem
gtoplig
chembl_ligand
gtoplig
pubchem
pubchem
pubchem
pubchem
|
peptide | Agonist | galanin-like peptide, galanin | peptide | Duan J, Shen DD, Zhao T, Guo S, He X, Yin W, Xu P, Ji Y, Chen LN, Liu J, Zhang H, Liu Q, Shi Y, Cheng X, Jiang H, Eric Xu H, Zhang Y, Xie X, Jiang Y | 10.1038/S41467-022-29072-3 | 2022-04-20 | 55355 | |
G12/13 | α13 | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7T6B | 7T6B_refined | 3.2 | S1PR2 | S1P2 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
sphingosine 1-phosphate
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate | small-molecule | Chen H, Chen K, Huang W, Staudt LM, Cyster JG, Li X | 10.1126/SCIADV.ABN0067 | 2022-04-06 | 55368 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7TUZ | 7TUZ_refined | 3.1 | GP183 | GPR183 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
(2S,4aS,4bS,7R,8S,8aS,9R,10aR)-7-[(2R,3R)-7-hydroxy-3,7-dimethyloctan-2-yl]-4a,7,8-trimethyltetradecahydrophenanthrene-2,9-diol
pubchem
|
small-molecule | Agonist | 7α,25-dihydroxycholesterol, 7β, 27-dihydroxycholesterol, 27-hydroxycholesterol, 7β, 25-dihydroxycholesterol, 7α,27-dihydroxycholesterol, 7β-hydroxycholesterol, 7α-hydroxycholesterol, 25-hydroxycholesterol | small-molecule | Chen H, Huang W, Li X | 10.1016/J.STR.2022.04.006 | 2022-04-13 | 55355 | |
Gs | αs | Human | Engineered G alpha | 55 | β1 | Human | γ2 | Human | Cryo-EM | 7RGP | - | 2.9 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - |
scFv16 Nanobody-35 |
- |
tirzepatide
pubchem
gtoplig
|
peptide | Agonist | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW | 10.1073/PNAS.2116506119 | 2022-04-13 | 55353 | |
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 | 55353 | |
G12/13 | α13 | Human | Gi2-mini-G13 chimera | 56 | β1 | Human | γ2 | Human | Cryo-EM | 7SF7 | - | 2.9 | AGRL3 | ADGRL3 | ADGRL | B2 (Adhesion) | Human | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Barros-Alvarez X, Nwokonko RM, Vizurraga A, Matzov D, He F, Papasergi-Scott MM, Robertson MJ, Panova O, Yardeni EH, Seven AB, Kwarcinski FE, Su H, Peroto MC, Meyerowitz JG, Shalev-Benami M, Tall GG, Skiniotis G | 10.1038/S41586-022-04575-7 | 2022-04-27 | 55368 | |
Gs | αs | Human | Mini-Gs | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7WUJ | - | 3.3 | AGRG4 | ADGRG4 | ADGRG | B2 (Adhesion) | Human | - |
scFv16 Nanobody-35 |
- |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Xiao P, Guo S, Wen X, He QT, Lin H, Huang SM, Gou L, Zhang C, Yang Z, Zhong YN, Yang CC, Li Y, Gong Z, Tao XN, Yang ZS, Lu Y, Li SL, He JY, Wang C, Zhang L, Kong L, Sun JP, Yu X | 10.1038/S41586-022-04590-8 | 2022-04-27 | 55353 | |
Gs | αs | Bovine | Gi1-Gs chimera | 56 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7S0G | - | 3.9 | ADRB1 | β1 | Adrenoceptors | A (Rhodopsin) | Wild turkey | - | - | - |
LEVISOPRENALINE
chembl_ligand
chembl_ligand
pubchem
|
small-molecule | Agonist | - | - | Alegre KO, Paknejad N, Su M, Lou JS, Huang J, Jordan KD, Eng ET, Meyerson JR, Hite RK, Huang XY | 10.1038/S41594-021-00679-2 | 2021-11-17 | 55370 | |
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 S-33, neuromedin U-23, neuromedin U-25, neuromedin S-36 | peptide | You C, Zhang Y, Xu P, Huang S, Yin W, Eric Xu H, Jiang Y | 10.1038/S41467-022-29683-W | 2022-04-20 | 55363 | |
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 | 55353 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7EUO | 7EUO_refined | 2.9 | FPR1 | FPR1 | Formylpeptide | A (Rhodopsin) | Human | - | scFv16 | - |
Peptide Agonist fMLF
|
peptide | Agonist | annexin I, fMet-Leu-Phe, spinorphin, cathepsin G | 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 | 55355 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7V68 | - | 3.4 | ACM4 | M4 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | scFv16 | - |
iperoxo
pubchem
gtoplig
chembl_ligand
LY2119620 pubchem gtoplig chembl_ligand |
small-molecule small-molecule |
Agonist PAM |
acetylcholine | small-molecule | Wang J, Wu M, Chen Z, Wu L, Wang T, Cao D, Wang H, Liu S, Xu Y, Li F, Liu J, Chen N, Zhao S, Cheng J, Wang S, Hua T | 10.1038/S41467-022-30595-Y | 2022-05-11 | 55355 | |
Gs | αs | Bovine | - | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7WBJ | - | 3.4 | VIPR2 | VPAC2 | VIP and PACAP | B1 (Secretin) | Human | - | Nanobody-35 | - |
PACAP-27
pubchem
gtoplig
pubchem
|
peptide | Agonist | PACAP-27, PACAP-38, GHRH, VIP, PHI, secretin | peptide | Xu Y, Feng W, Zhou Q, Liang A, Li J, Dai A, Zhao F, Yan J, Chen CW, Li H, Zhao LH, Xia T, Jiang Y, Xu HE, Yang D, Wang MW | 10.1038/S41467-022-30041-Z | 2022-05-18 | 55370 | |
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 | neuropeptide Y, PYY-(3-36), peptide YY, neuropeptide Y-(3-36), pancreatic polypeptide | 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 | 55355 | |
Gq/11 | αq | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7F6H | 7F6H_refined | 2.9 | BKRB2 | B2 | Bradykinin | A (Rhodopsin) | Human | - | - | - |
bradykinin
pubchem
gtoplig
chembl_ligand
drugbank
gtoplig
|
peptide | Agonist | [des-Arg9]bradykinin, [des-Arg10]kallidin, T-kinin, Lys-[Hyp3]-bradykinin, kallidin, bradykinin, [Hyp3]bradykinin | peptide | Shen J, Zhang D, Fu Y, Chen A, Yang X, Zhang H | 10.1038/S41467-022-28399-1 | 2022-01-05 | 55363 | |
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 | 55363 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7F0T | - | 3.1 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
dopamine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine, dopamine, (-)-noradrenaline | small-molecule | Teng X, Chen S, Wang Q, Chen Z, Wang X, Huang N, Zheng S | 10.1126/SCIADV.ABO4158 | 2022-06-15 | 55353 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7F23 | - | 3.6 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
dopamine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine, dopamine, (-)-noradrenaline | small-molecule | Teng X, Chen S, Wang Q, Chen Z, Wang X, Huang N, Zheng S | 10.1126/SCIADV.ABO4158 | 2022-06-15 | 55353 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7X2D | 7X2D_refined | 3.3 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
tavapadon
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine, dopamine, (-)-noradrenaline | 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 | 55353 | |
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
|
peptide | Agonist | galanin-like peptide, spexin-1, galanin | peptide | Jiang W, Zheng S | 10.1073/PNAS.2121465119 | 2022-06-29 | 55363 | |
Gs | αs | Human | - | 59 | β1 | Rat | γ2 | Human | Cryo-EM | 7X8R | - | 2.6 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
CHEMBL2158411
chembl_ligand
pubchem
|
small-molecule | Agonist | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | Cong Z, Zhou Q, Li Y, Chen LN, Zhang ZC, Liang A, Liu Q, Wu X, Dai A, Xia T, Wu W, Zhang Y, Yang D, Wang MW | 10.1073/PNAS.2200155119 | 2022-06-29 | 55353 | |
Gq/11 | αq | Human | Gi2-mini-Gq chimera | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7RAN | - | 3.5 | 5HT2A | 5-HT2A | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | scFv16 | - |
3-[(3R)-3-methyl-1,2,3,6-tetrahydropyridin-1-ium-5-yl]-1H-pyrrolo[2,3-b]pyridine
pubchem
|
small-molecule | Agonist | tryptamine, 5-hydroxytryptamine | small-molecule | Kaplan AL, Confair DN, Kim K, Barros-Alvarez X, Rodriguiz RM, Yang Y, Kweon OS, Che T, McCorvy JD, Kamber DN, Phelan JP, Martins LC, Pogorelov VM, DiBerto JF, Slocum ST, Huang XP, Kumar JM, Robertson MJ, Panova O, Seven AB, Wetsel AQ, Wetsel WC, Irwin JJ, Skiniotis G, Shoichet BK, Roth BL, Ellman JA | 10.1038/S41586-022-05258-Z | 2022-07-06 | 55363 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7XTA | 7XTA_refined | 3.2 | 5HT4R | 5-HT4 | 5-Hydroxytryptamine | A (Rhodopsin) | Human | BRIL | scFv16 | - |
5-hydroxytryptamine
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE | 10.1016/J.MOLCEL.2022.05.031 | 2022-07-27 | 55355 | |
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 | 55361 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7W0M | 7W0M_refined | 3.7 | APJ | apelin | Apelin | A (Rhodopsin) | Human | BRIL | scFv16 | - |
(1R,2S)-N-[4-(2,6-dimethoxyphenyl)-5-(6-methylpyridin-2-yl)-1,2,4-triazol-3-yl]-1-(5-methylpyrimidin-2-yl)-1-oxidanyl-propane-2-sulfonamide
pubchem
|
small-molecule | Agonist | Elabela/Toddler-11, [Pyr1]apelin-13, apelin-17, apelin-36, apelin-13, Elabela/Toddler-21, apelin receptor early endogenous ligand, Elabela/Toddler-32 | peptide | Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F | 10.1038/S41594-022-00797-5 | 2022-07-27 | 55355 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7W0P | 7W0P_refined | 3.2 | APJ | apelin | Apelin | A (Rhodopsin) | Human | BRIL | scFv16 | - |
apelin receptor early endogenous ligand
pubchem
|
peptide | Agonist | Elabela/Toddler-11, [Pyr1]apelin-13, apelin-17, apelin-36, apelin-13, Elabela/Toddler-21, apelin receptor early endogenous ligand, Elabela/Toddler-32 | peptide | Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F | 10.1038/S41594-022-00797-5 | 2022-07-27 | 55355 | |
Gq/11 | αq | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7XOW | 7XOW_refined | 3.1 | GASR | CCK2 | Cholecystokinin | A (Rhodopsin) | Human | - | scFv16 | - |
desulfated gastrin-17
pubchem
gtoplig
chembl_ligand
pubchem
|
peptide | Agonist | CCK-33, CCK-4, gastrin-71, desulfated gastrin-71, desulfated gastrin-14, gastrin-14, desulfated gastrin-17, gastrin-17, gastrin-34, CCK-39, desulfated gastrin-34, desulfated cholecystokinin-8, CCK-8, CCK-58 | 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 | 55363 | |
Gi/o | αi1 | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7WJ5 | 7WJ5_refined | 3.7 | SSR2 | SST2 | Somatostatin | A (Rhodopsin) | Human | BRIL | scFv16 | - |
SOMATOSTATIN
chembl_ligand
pubchem
|
protein | Agonist | CST-17, cortistatin-14, SRIF-28, SRIF-14 | peptide | Heo Y, Yoon E, Jeon YE, Yun JH, Ishimoto N, Woo H, Park SY, Song JJ, Lee W | 10.7554/ELIFE.76823 | 2022-07-13 | 55355 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7XTQ | 7XTQ_refined | 3.2 | GPBAR | GPBA | Bile acid | A (Rhodopsin) | Human | - | Nanobody-35 | - |
CHEMBL2181246
chembl_ligand
pubchem
|
small-molecule | Agonist | cholic acid, lithocholic acid, chenodeoxycholic acid, deoxycholic acid | small-molecule | Ma L, Yang F, Wu X, Mao C, Guo L, Miao T, Zang SK, Jiang X, Shen DD, Wei T, Zhou H, Wei Q, Li S, Shu Q, Feng S, Jiang C, Chu B, Du L, Sun JP, Yu X, Zhang Y, Zhang P | 10.1073/PNAS.2117054119 | 2022-07-06 | 55353 | |
Gi/o | αi1 | Human | - | 62 | β1 | Mouse | γ2 | Mouse | Cryo-EM | 7Y12 | - | 3.1 | MRGRD | MRGPRD | A orphans | A (Rhodopsin) | Human | BRIL | scFv16 | - |
β-alanine
pubchem
gtoplig
chembl_ligand
drugbank
pubchem
|
small-molecule | Agonist | β-alanine | small-molecule | Suzuki S, Iida M, Hiroaki Y, Tanaka K, Kawamoto A, Kato T, Oshima A | 10.1038/S42003-022-03668-3 | 2022-07-20 | 55355 | |
Gs | αs | Bovine | - | 51 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 8DCR | - | 2.6 | ADRB1 | β1 | Adrenoceptors | A (Rhodopsin) | Wild turkey | T4-Lysozyme | Nanobody-35 | - |
Dobutamine
pubchem
|
small-molecule | Agonist | - | - | Su M, Paknejad N, Zhu L, Wang J, Do HN, Miao Y, Liu W, Hite RK, Huang XY | 10.1038/S41467-022-31823-1 | 2022-07-27 | 55370 | |
Gq/11 | αq | Human | Gi2-mini-Gq chimera | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8DPG | - | 3.6 | 5HT2C | 5-HT2C | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | scFv16 | - |
psilocin
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Gumpper RH, Fay JF, Roth BL | 10.1016/J.CELREP.2022.111211 | 2022-08-24 | 55363 | |
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 | CST-17, cortistatin-14, SRIF-28, 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 | 55355 | |
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 | CST-17, cortistatin-14, SRIF-28, 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 | 55355 | |
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 | 55363 | |
Gq/11 | αq | Human | - | 57 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7X1U | 7X1U_refined | 3.2 | TRFR | TRH1 | Thyrotropin-releasing hormone | A (Rhodopsin) | Human | - | scFv16 | - |
TRH
pubchem
|
peptide | Agonist | TRH | peptide | Yang F, Zhang H, Meng X, Li Y, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C | 10.1038/S41422-022-00646-6 | 2022-08-31 | 55363 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7X9Y | 7X9Y_refined | 3.1 | CCR3 | CCR3 | Chemokine | A (Rhodopsin) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | CCL11, CCL8, CCL26, CXCL11, CXCL10, CCL24, CCL28, CXCL9, CCL7, CCL15, CCL2, CCL13, CCL5 | peptide | Shao Z, Tan Y, Shen Q, Hou L, Yao B, Qin J, Xu P, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Chen ZH, Jiang Y, Xu HE, Ying S, Ma H, Zhang Y, Shen H | 10.1038/S41421-022-00403-4 | 2022-08-24 | 55355 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7XW6 | - | 2.8 | TSHR | TSH | Glycoprotein hormone | A (Rhodopsin) | Human | - | Nanobody-35 | - |
M22 antibody heavy chain
M22 antibody light chain N-[4-[[5-[(2S)-3-benzyl-5-hydroxy-4-oxo-1,2-dihydroquinazolin-2-yl]-2-methoxyphenyl]methoxy]phenyl]acetamide pubchem |
protein protein small-molecule |
Agonist | TSH | peptide | Duan J, Xu P, Luan X, Ji Y, He X, Song N, Yuan Q, Jin Y, Cheng X, Jiang H, Zheng J, Zhang S, Jiang Y, Xu HE | 10.1038/S41586-022-05173-3 | 2022-08-17 | 55353 | |
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 | 55353 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 8ID6 | - | 2.8 | FFAR4 | FFA4 | Free fatty acid | A (Rhodopsin) | Human | - | scFv16 | - |
oleic acid
pubchem
gtoplig
chembl_ligand
drug_central
|
small-molecule | Agonist | myristic acid, oleic acid, α-linolenic acid, linoleic acid | small-molecule | Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP | 10.1126/SCIENCE.ADD6220 | 2023-03-15 | 55355 | |
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 | 55361 | |
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 | 55361 | |
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 | GRP-(18-27), neuromedin B, gastrin releasing peptide(14-27) (human), neuromedin C, gastrin-releasing peptide | peptide | Peng S, Zhan Y, Zhang D, Ren L, Chen A, Chen ZF, Zhang H | 10.1073/PNAS.2216230120 | 2023-02-22 | 55363 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7XK8 | 7XK8_refined | 3.3 | NMUR2 | NMU2 | Neuromedin U | A (Rhodopsin) | Human | - | - | - |
Neuromedin U-25 (human)
pubchem
|
peptide | Agonist | neuromedin S-33, neuromedin U-23, neuromedin U-25, neuromedin S-36 | peptide | Zhao W, Zhang W, Wang M, Lu M, Chen S, Tang T, Schnapp G, Wagner H, Brennauer A, Yi C, Chu X, Han S, Wu B, Zhao Q | 10.1038/S41467-022-34814-4 | 2023-02-22 | 55355 | |
Gs | αolf | Human | Golf-Gi chimera | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8IW1 | - | 3.4 | TAAR9 | TAAR9 | A orphans | A (Rhodopsin) | Mouse | - | scFv16 | - |
2-Phenylethanaminium
pubchem
|
small-molecule | Agonist | - | - | Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP | 10.1038/S41586-023-06106-4 | 2023-05-31 | 55354 | |
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 | 55353 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8GUS | - | 3.0 | CNR2 | CB2 | Cannabinoid | A (Rhodopsin) | Human | - | scFv16 | - |
CHEMBL2179724
chembl_ligand
pubchem
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | Li X, Chang H, Bouma J, de Paus LV, Mukhopadhyay P, Paloczi J, Mustafa M, van der Horst C, Kumar SS, Wu L, Yu Y, van den Berg RJBHN, Janssen APA, Lichtman A, Liu ZJ, Pacher P, van der Stelt M, Heitman LH, Hua T | 10.1038/S41467-023-37112-9 | 2023-05-10 | 55355 | |
Gi/o | αi2 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7XXI | 7XXI_refined | 3.0 | P2Y12 | P2Y12 | P2Y | A (Rhodopsin) | Human | - | - | - |
2MeSADP
pubchem
gtoplig
chembl_ligand
gtoplig
|
small-molecule | Agonist | ATP, ADP | small-molecule | - | - | 2023-06-07 | 55356 | |
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 | big dynorphin, β-neoendorphin, [Met]enkephalin, α-neoendorphin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin A-(1-8), dynorphin B | 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 | 55360 | |
Gq/11 | αq | Human | - | 59 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7XWO | 7XWO_refined | 2.7 | NK2R | NK2 | Tachykinin | A (Rhodopsin) | Human | BRIL | scFv16 | - |
HIS-LYS-THR-ASP-SER-PHE-VAL-GLY-LEU-MET-NH2
|
peptide | Agonist | substance P, hemokinin 1, neurokinin A, neurokinin B, neuropeptide γ, neuropeptide K | peptide | - | - | 2023-05-31 | 55363 | |
Gs | αs | Human | - | 56 | β1 | Human | γ2 | Human | Cryo-EM | 7Y3G | 7Y3G_refined | 2.8 | GPR12 | GPR12 | A orphans | A (Rhodopsin) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | sphingosine 1-phosphate | small-molecule | Li H, Zhang J, Yu Y, Luo F, Wu L, Liu J, Chen N, Liu Z, Hua T | 10.1016/J.SCIB.2022.12.023 | 2023-06-07 | 55353 | |
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 | 55355 | |
Gi/o | αo | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8DZQ | 8DZQ_refined | 2.8 | OPRK | κ | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
SALVINORIN B METHOXYMETHYL ETHER
chembl_ligand
pubchem
|
small-molecule | Agonist | big dynorphin, β-neoendorphin, [Met]enkephalin, α-neoendorphin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin A-(1-8), dynorphin B | 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 | 55361 | |
Gi/o | αz | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8DZS | - | 2.7 | OPRK | κ | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
CHEMBL277863
chembl_ligand
pubchem
|
small-molecule | Agonist | big dynorphin, β-neoendorphin, [Met]enkephalin, α-neoendorphin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin A-(1-8), dynorphin B | 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 | 55362 | |
Gq/11 | αq | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8IBU | 8IBU_refined | 3.5 | MTLR | motilin | Motilin | A (Rhodopsin) | Human | BRIL | scFv16 | - |
erythromycin
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | motilin | peptide | You C, Zhang Y, Xu Y, Xu P, Li Z, Li H, Huang S, Chen Z, Li J, Xu HE, Jiang Y | 10.1126/SCIADV.ADE9020 | 2023-04-12 | 55363 | |
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 | 55355 | |
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
chembl_ligand
drugbank
|
small-molecule | Agonist | CST-17, cortistatin-14, SRIF-28, 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 | 55355 | |
Gi/o | αi1 | Human | - | 64 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8HK2 | - | 2.9 | C3AR | C3a | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
C3a anaphylatoxin
pubchem
|
peptide | Agonist | C5a, C3a | peptide | Wang Y, Liu W, Xu Y, He X, Yuan Q, Luo P, Fan W, Zhu J, Zhang X, Cheng X, Jiang Y, Xu HE, Zhuang Y | 10.1038/S41589-023-01339-W | 2023-05-10 | 55355 | |
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 | 55355 | |
Gq/11 | α11 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7XXH | 7XXH_refined | 2.9 | P2RY1 | P2Y1 | P2Y | A (Rhodopsin) | Human | - | scFv16 | - |
2MeSADP
pubchem
gtoplig
chembl_ligand
gtoplig
|
small-molecule | Agonist | ATP, ADP | small-molecule | - | - | 2023-06-07 | 55364 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8FLR | - | 2.9 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
PTHrP[1-36]
|
peptide | Agonist | PTH, PTHrP-(1-36), TIP39, PTHrP | 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 | 55353 | |
Gq/11 | αq | Human | Mini-Gq | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7YDM | - | 2.9 | AGRE5 | ADGRE5 | ADGRE | B2 (Adhesion) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Wang N, Qian Y, Xia R, Zhu X, Xiong Y, Zhang A, Guo C, He Y | 10.1016/J.CHEMBIOL.2023.08.003 | 2023-07-12 | 55363 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8F2A | - | 2.2 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - | Nanobody-35 | - |
Pramlintide analogue San385
|
peptide | Agonist | adrenomedullin 2/intermedin, amylin, β-CGRP, α-CGRP, calcitonin, adrenomedullin | 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 | 55353 | |
Gq/11 | αq | Human | - | 56 | β1 | Human | γ2 | Human | Cryo-EM | 8H0Q | - | 3.3 | GRPR | BB2 | Bombesin | A (Rhodopsin) | Human | - | - | - |
Gastrin-releasing peptide
pubchem
|
peptide | Agonist | GRP-(18-27), neuromedin B, gastrin releasing peptide(14-27) (human), neuromedin C, gastrin-releasing peptide | peptide | Li C, Xu Y, Liu H, Cai H, Jiang Y, Xu HE, Yin W | 10.1038/S41422-022-00743-6 | 2023-08-09 | 55363 | |
Gq/11 | αq | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8H4L | - | 3.1 | FFAR4 | FFA4 | Free fatty acid | A (Rhodopsin) | Human | - | Nanobody-35 | - |
docosahexaenoic acid
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
pubchem
|
small-molecule | Agonist | myristic acid, oleic acid, α-linolenic acid, linoleic acid | small-molecule | Yin H, Inoue A, Ma Z, Zhu X, Xia R, Xu Z, Wang N, Duan Y, Zhang A, Guo C, He Y | 10.1038/S41422-023-00835-X | 2023-06-21 | 55363 | |
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, PGD2, PGE2, PGI2, PGF2α | 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 | 55363 | |
Gq/11 | αq | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8IUL | - | 2.8 | PF2R | FP | Prostanoid | A (Rhodopsin) | Human | - | scFv16 | - |
latanoprost (free acid form)
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | thromboxane A2, PGD2, PGE2, PGI2, PGF2α | 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 | 55363 | |
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 | 55355 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7WVU | 7WVU_refined | 3.3 | FPR1 | FPR1 | Formylpeptide | A (Rhodopsin) | Human | - | - | - |
FME-LEU-PHE
|
peptide | Agonist | annexin I, fMet-Leu-Phe, spinorphin, cathepsin G | 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 | 55355 | |
Gi/o | αi2 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7WVY | 7WVY_refined | 3.0 | FPR2 | FPR2/ALX | Formylpeptide | A (Rhodopsin) | Human | BRIL | - | - |
Amyloid beta-Peptide (1-42)
pubchem
|
peptide | Agonist | serum amyloid A, aspirin triggered lipoxin A4, humanin, resolvin D1, LL-37, PrP106-126, annexin I, LXA4, aspirin-triggered resolvin D1 | peptide | Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B | 10.1038/S41467-022-29361-X | 2022-04-13 | 55356 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7SCG | - | 3.0 | OPRM | μ | Opioid | A (Rhodopsin) | Mouse | - | scFv16 | - |
(2E)-N-[(2S)-2-(dimethylamino)-3-(4-hydroxyphenyl)propyl]-3-(naphthalen-1-yl)prop-2-enamide
pubchem
|
small-molecule | Agonist | - | - | Wang H, Hetzer F, Huang W, Qu Q, Meyerowitz J, Kaindl J, Hubner H, Skiniotis G, Kobilka BK, Gmeiner P | 10.1002/ANIE.202200269 | 2022-04-20 | 55355 | |
Gs | αs | Human | - | 56 | β1 | Human | γ2 | Human | Cryo-EM | 7RG9 | 7RG9_refined | 3.2 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - |
scFv16 Nanobody-35 |
- |
Apo (no ligand)
|
none | Apo (no ligand) | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW | 10.1073/PNAS.2116506119 | 2022-04-13 | 55353 | |
Gs | αs | Human | - | 53 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7VBH | 7VBH_refined | 3.0 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
Peptide 20
|
peptide | Agonist | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW | 10.1038/S41467-022-28683-0 | 2022-04-06 | 55353 | |
Gi/o | αi1 | Human | Mini-Gi1 | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7WU4 | - | 3.4 | AGRF1 | ADGRF1 | ADGRF | B2 (Adhesion) | Human | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Qu X, Qiu N, Wang M, Zhang B, Du J, Zhong Z, Xu W, Chu X, Ma L, Yi C, Han S, Shui W, Zhao Q, Wu B | 10.1038/S41586-022-04580-W | 2022-04-27 | 55355 | |
G12/13 | α13 | Human | Gi2-mini-G13 chimera | 56 | β1 | Human | γ2 | Human | Cryo-EM | 7SF8 | - | 2.7 | AGRG1 | ADGRG1 | ADGRG | B2 (Adhesion) | Human | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Barros-Alvarez X, Nwokonko RM, Vizurraga A, Matzov D, He F, Papasergi-Scott MM, Robertson MJ, Panova O, Yardeni EH, Seven AB, Kwarcinski FE, Su H, Peroto MC, Meyerowitz JG, Shalev-Benami M, Tall GG, Skiniotis G | 10.1038/S41586-022-04575-7 | 2022-04-27 | 55368 | |
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 | 55355 | |
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 S-33, neuromedin U-23, neuromedin U-25, neuromedin S-36 | peptide | You C, Zhang Y, Xu P, Huang S, Yin W, Eric Xu H, Jiang Y | 10.1038/S41467-022-29683-W | 2022-04-20 | 55363 | |
Gq/11 | αq | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7W57 | - | 3.2 | NMUR2 | NMU2 | Neuromedin U | A (Rhodopsin) | Human | - | scFv16 | - |
Neuromedin-S
|
peptide | Agonist | neuromedin S-33, neuromedin U-23, neuromedin U-25, neuromedin S-36 | peptide | You C, Zhang Y, Xu P, Huang S, Yin W, Eric Xu H, Jiang Y | 10.1038/S41467-022-29683-W | 2022-04-20 | 55363 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7V69 | - | 3.4 | ACM4 | M4 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | acetylcholine | small-molecule | Wang J, Wu M, Chen Z, Wu L, Wang T, Cao D, Wang H, Liu S, Xu Y, Li F, Liu J, Chen N, Zhao S, Cheng J, Wang S, Hua T | 10.1038/S41467-022-30595-Y | 2022-05-11 | 55355 | |
Gs | αs | Bovine | - | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7VQX | - | 2.7 | VIPR2 | VPAC2 | VIP and PACAP | B1 (Secretin) | Human | - | Nanobody-35 | - |
PACAP-27
pubchem
gtoplig
pubchem
|
peptide | Agonist | PACAP-27, PACAP-38, GHRH, VIP, PHI, secretin | peptide | Xu Y, Feng W, Zhou Q, Liang A, Li J, Dai A, Zhao F, Yan J, Chen CW, Li H, Zhao LH, Xia T, Jiang Y, Xu HE, Yang D, Wang MW | 10.1038/S41467-022-30041-Z | 2022-05-18 | 55370 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7X9C | 7X9C_refined | 3.0 | NPY4R | Y4 | Neuropeptide Y | A (Rhodopsin) | Human | - | - | - |
Pancreatic polypeptide
pubchem
|
peptide | Agonist | neuropeptide Y, PYY-(3-36), pancreatic polypeptide, 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 | 55355 | |
Gq/11 | αq | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7F6I | 7F6I_refined | 2.8 | BKRB2 | B2 | Bradykinin | A (Rhodopsin) | Human | - | - | - |
kallidin
pubchem
gtoplig
|
peptide | Agonist | [des-Arg9]bradykinin, [des-Arg10]kallidin, T-kinin, Lys-[Hyp3]-bradykinin, kallidin, bradykinin, [Hyp3]bradykinin | peptide | Shen J, Zhang D, Fu Y, Chen A, Yang X, Zhang H | 10.1038/S41467-022-28399-1 | 2022-01-05 | 55363 | |
Gi/o | αi1 | Human | - | 64 | β1 | Rat | γ2 | Human | Cryo-EM | 7WIC | - | 2.8 | SSR2 | SST2 | Somatostatin | A (Rhodopsin) | Human | - | scFv16 | - |
SOMATOSTATIN
chembl_ligand
pubchem
|
protein | Agonist | CST-17, cortistatin-14, SRIF-28, SRIF-14 | peptide | Chen LN, Wang WW, Dong YJ, Shen DD, Guo J, Yu X, Qin J, Ji SY, Zhang H, Shen Q, He Q, Yang B, Zhang Y, Li Q, Mao C | 10.1038/S41422-022-00669-Z | 2022-06-01 | 55355 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7F1Z | - | 3.5 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | - | - |
dopamine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine, dopamine, (-)-noradrenaline | small-molecule | Teng X, Chen S, Wang Q, Chen Z, Wang X, Huang N, Zheng S | 10.1126/SCIADV.ABO4158 | 2022-06-15 | 55353 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7X2C | 7X2C_refined | 3.2 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
fenoldopam
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
gtoplig
chembl_ligand
pubchem
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine, dopamine, (-)-noradrenaline | small-molecule | Teng X, Chen S, Nie Y, Xiao P, Yu X, Shao Z, Zheng S | 10.1038/S41467-022-30929-W | 2022-06-29 | 55353 | |
Gq/11 | αq | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7XJK | 7XJK_refined | 3.3 | GALR2 | GAL2 | Galanin | A (Rhodopsin) | Human | - | scFv16 | - |
Galanin, Human
pubchem
|
peptide | Agonist | galanin-like peptide, spexin-1, galanin | peptide | Jiang W, Zheng S | 10.1073/PNAS.2121465119 | 2022-06-29 | 55363 | |
Gq/11 | αq | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7WKD | - | 3.0 | TRFR | TRH1 | Thyrotropin-releasing hormone | A (Rhodopsin) | Human | - | scFv16 | - |
TRH
pubchem
|
peptide | Agonist | TRH | peptide | Xu Y, Cai H, You C, He X, Yuan Q, Jiang H, Cheng X, Jiang Y, Xu HE | 10.1038/S41422-022-00641-X | 2022-06-15 | 55363 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7XT9 | - | 3.2 | 5HT4R | 5-HT4 | 5-Hydroxytryptamine | A (Rhodopsin) | Human | BRIL | - | - |
5-hydroxytryptamine
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE | 10.1016/J.MOLCEL.2022.05.031 | 2022-07-27 | 55353 | |
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 | 55361 | |
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 | 55353 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7W0N | - | 4.2 | APJ | apelin | Apelin | A (Rhodopsin) | Human | BRIL | scFv16 | - |
apelin receptor early endogenous ligand
pubchem
|
peptide | Agonist | Elabela/Toddler-11, [Pyr1]apelin-13, apelin-17, apelin-36, apelin-13, Elabela/Toddler-21, apelin receptor early endogenous ligand, Elabela/Toddler-32 | peptide | Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F | 10.1038/S41594-022-00797-5 | 2022-07-27 | 55355 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7XOU | - | 3.2 | CCKAR | CCK1 | Cholecystokinin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
CCK-8
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
peptide | Agonist | CCK-33, CCK-4, gastrin-17, CCK-39, desulfated cholecystokinin-8, CCK-8, CCK-58 | 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 | 55353 | |
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 | 55363 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7XBX | - | 3.4 | CX3C1 | CX3CR1 | Chemokine | A (Rhodopsin) | Human | - | - | - |
CX3CL1
|
peptide | Agonist | CX3CL1 | peptide | - | - | 2022-07-13 | 55355 | |
Gq/11 | αq | Human | Gi2-mini-Gq chimera | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8DPF | - | 2.8 | 5HT2C | 5-HT2C | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | scFv16 | - |
lorcaserin
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Gumpper RH, Fay JF, Roth BL | 10.1016/J.CELREP.2022.111211 | 2022-08-24 | 55363 | |
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 | 55363 | |
Gi/o | αi1 | Human | - | 63 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7XAV | 7XAV_refined | 2.9 | SSR2 | SST2 | Somatostatin | A (Rhodopsin) | Human | - | scFv16 | - |
lanreotide
pubchem
gtoplig
drugbank
|
peptide | Agonist | CST-17, cortistatin-14, SRIF-28, 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 | 55355 | |
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 | CST-17, cortistatin-14, SRIF-28, 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 | 55355 | |
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 | 55361 | |
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 | 55353 | |
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 | PTH, PTHrP-(1-36), TIP39, PTHrP | 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 | 55353 | |
Gs | αs | Human | - | 58 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7VVM | 7VVM_refined | 3.2 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
Parathyroid hormone
|
peptide | Agonist | PTH, PTHrP-(1-36), TIP39, PTHrP | 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 | 55353 | |
Gs | αs | Human | - | 58 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7VVO | 7VVO_refined | 4.1 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
Parathyroid hormone
|
peptide | Agonist | PTH, PTHrP-(1-36), TIP39, PTHrP | 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 | 55353 | |
Gs | αs | Human | - | 57 | β1 | Human | γ2 | Human | Cryo-EM | 7XKD | - | 2.4 | AGRG2 | ADGRG2 | ADGRG | B2 (Adhesion) | Mouse | - | Nanobody-35 | - |
PRASTERONE
chembl_ligand
pubchem
|
small-molecule | Agonist | - | - | Lin H, Xiao P, Bu RQ, Guo S, Yang Z, Yuan D, Zhu ZL, Zhang CX, He QT, Zhang C, Ping YQ, Zhao RJ, Ma CS, Liu CH, Zhang XN, Jiang D, Huang S, Xi YT, Zhang DL, Xue CY, Yang BS, Li JY, Lin HC, Zeng XH, Zhao H, Xu WM, Yi F, Liu Z, Sun JP, Yu X | 10.1038/S41589-022-01084-6 | 2022-08-10 | 55353 | |
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 | 55353 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7XZ6 | - | 2.8 | GP119 | GPR119 | GPR18, GPR55 and GPR119 | A (Rhodopsin) | Human | BRIL | Nanobody-35 | - |
APD668
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | SEA, N-palmitoylethanolamine, N-oleoylethanolamide, anandamide | 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 | 55353 | |
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 | 55363 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7WYB | - | 3.0 | AGRL3 | ADGRL3 | ADGRL | B2 (Adhesion) | Mouse | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Qian Y, Ma Z, Liu C, Li X, Zhu X, Wang N, Xu Z, Xia R, Liang J, Duan Y, Yin H, Xiong Y, Zhang A, Guo C, Chen Z, Huang Z, He Y | 10.1016/J.MOLCEL.2022.10.009 | 2022-10-26 | 55355 | |
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 | 55367 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7X2V | - | 3.1 | AGRF1 | ADGRF1 | ADGRF | B2 (Adhesion) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y | 10.1038/S41467-022-33173-4 | 2022-09-28 | 55355 | |
Gi/o | αgust | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7XP4 | - | 3.0 | T2R46 | TAS2R46 | Taste 2 | T2 (Taste 2) | Human | - | Nanobody-35 | Endoglucanase H |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Xu W, Wu L, Liu S, Liu X, Cao X, Zhou C, Zhang J, Fu Y, Guo Y, Wu Y, Tan Q, Wang L, Liu J, Jiang L, Fan Z, Pei Y, Yu J, Cheng J, Zhao S, Hao X, Liu ZJ, Hua T | 10.1126/SCIENCE.ABO1633 | 2022-10-12 | 55360 | |
Gi/o | αgust | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7XP6 | - | 3.0 | T2R46 | TAS2R46 | Taste 2 | T2 (Taste 2) | Human | - | Nanobody-35 | Endoglucanase H |
strychnine
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
gtoplig
|
small-molecule | Agonist | - | - | Xu W, Wu L, Liu S, Liu X, Cao X, Zhou C, Zhang J, Fu Y, Guo Y, Wu Y, Tan Q, Wang L, Liu J, Jiang L, Fan Z, Pei Y, Yu J, Cheng J, Zhao S, Hao X, Liu ZJ, Hua T | 10.1126/SCIENCE.ABO1633 | 2022-10-12 | 55360 | |
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 | 55363 | |
Gq/11 | αq | Human | Mini-Gq | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7Y27 | 7Y27_refined | 3.5 | SSR2 | SST2 | Somatostatin | A (Rhodopsin) | Human | - | scFv16 | - |
SOMATOSTATIN
chembl_ligand
pubchem
|
protein | Agonist | CST-17, cortistatin-14, SRIF-28, SRIF-14 | peptide | Chen S, Teng X, Zheng S | 10.1038/S41589-022-01130-3 | 2022-10-19 | 55363 | |
Gi/o | αi1 | Human | - | 63 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7YU7 | - | 3.8 | LPAR1 | LPA1 | Lysophospholipid (LPA) | A (Rhodopsin) | Human | - | scFv16 | - |
[(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate
pubchem
|
small-molecule | Agonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O | 10.1038/S41467-022-33121-2 | 2022-10-05 | 55355 | |
Gq/11 | αq | Human | Gs-mini-Gq chimera | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8DWG | - | 2.7 | MRGX1 | MRGPRX1 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
Proenkephalin-A
CHEMBL5177388 chembl_ligand pubchem |
peptide small-molecule |
Agonist PAM |
bovine adrenal medulla peptide 8-22 | peptide | Liu Y, Cao C, Huang XP, Gumpper RH, Rachman MM, Shih SL, Krumm BE, Zhang S, Shoichet BK, Fay JF, Roth BL | 10.1038/S41589-022-01173-6 | 2022-11-02 | 55363 | |
Gs | αs | Human | - | 56 | β1 | Human | γ2 | Human | Cryo-EM | 8E3Y | - | 2.3 | VIPR1 | VPAC1 | VIP and PACAP | B1 (Secretin) | Human | - | Nanobody-35 | - |
[Ac-His1]PACAP-27
gtoplig
chembl_ligand
pubchem
|
peptide | Agonist | PACAP-27, PACAP-38, GHRH, VIP, PHM, PHI, secretin | peptide | Piper SJ, Deganutti G, Lu J, Zhao P, Liang YL, Lu Y, Fletcher MM, Hossain MA, Christopoulos A, Reynolds CA, Danev R, Sexton PM, Wootten D | 10.1038/S41467-022-34629-3 | 2022-11-23 | 55353 | |
Gi/o | αo | Human | Mini-Go | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8E9X | - | 2.7 | ACM4 | M4 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | scFv16 | - |
CHEMBL73538
chembl_ligand
pubchem
|
small-molecule | Agonist | acetylcholine | small-molecule | Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL | 10.1038/S41586-022-05489-0 | 2022-11-30 | 55361 | |
Gi/o | αi1 | Human | - | 64 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8EFB | 8EFB_refined | 3.2 | OPRM | μ | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
OLICERIDINE
chembl_ligand
pubchem
drugbank
|
small-molecule | Agonist | endomorphin-1, endomorphin-2, [Met]enkephalin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin A-(1-8), dynorphin B | 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 | 55355 | |
Gi/o | αi1 | Human | - | 64 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8EFO | - | 2.8 | OPRM | μ | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
PZM21
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | endomorphin-1, endomorphin-2, [Met]enkephalin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin A-(1-8), dynorphin B | 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 | 55355 | |
Gi/o | αi1 | Human | - | 62 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8F7S | 8F7S_refined | 3.0 | OPRD | δ | Opioid | A (Rhodopsin) | Human | - | - | - |
DELTORPHIN II
chembl_ligand
pubchem
|
protein | Agonist | endomorphin-1, [Met]enkephalin, α-neoendorphin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin A-(1-8), dynorphin B | 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 | 55355 | |
Gi/o | αi1 | Human | - | 62 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8F7X | 8F7X_refined | 3.3 | OPRX | NOP | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
nociceptin/orphanin FQ
pubchem
gtoplig
chembl_ligand
gtoplig
pubchem
pubchem
|
peptide | Agonist | nociceptin/orphanin FQ | peptide | Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y, Roth BL, Xu HE | 10.1016/J.CELL.2022.12.026 | 2022-12-14 | 55355 | |
Gs | αs | Bovine | - | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8HAO | - | 3.8 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
teriparatide
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
pubchem
pubchem
pubchem
pubchem
pubchem
|
peptide | Agonist | PTH, PTHrP-(1-36), TIP39, PTHrP | 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 | 55370 | |
Gi/o | αi2 | Human | - | 59 | β1 | Human | γ2 | Bovine | Cryo-EM | 7YK6 | 7YK6_refined | 3.0 | RL3R2 | RXFP4 | Relaxin family peptide | A (Rhodopsin) | Human | - | scFv16 | - |
CHEMBL4522365
chembl_ligand
pubchem
|
small-molecule | Agonist | relaxin-3, relaxin-3 (B chain), INSL5 | peptide | Chen Y, Zhou Q, Wang J, Xu Y, Wang Y, Yan J, Wang Y, Zhu Q, Zhao F, Li C, Chen CW, Cai X, Bathgate RAD, Shen C, Eric Xu H, Yang D, Liu H, Wang MW | 10.1038/S41467-023-36182-Z | 2023-03-01 | 55356 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7Y67 | 7Y67_refined | 2.8 | C5AR1 | C5a1 | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
C089
|
peptide | Agonist | C5a des-Arg, ribosomal protein S19, C5a, 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 | 55355 | |
Gs | αs | Human | Mini-Gs | 55 | β1 | Human | γ2 | Human | Cryo-EM | 8F76 | 8F76_refined | 3.1 | O51E2 | OR51E2 | Odorant family 51 | O1 (fish-like odorant) | Human | - | Nanobody-35 | - |
propanoic acid
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | - | - | Billesbolle CB, de March CA, van der Velden WJC, Ma N, Tewari J, Del Torrent CL, Li L, Faust B, Vaidehi N, Matsunami H, Manglik A | 10.1038/S41586-023-05798-Y | 2023-03-22 | 55353 | |
Gi/o | αo | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8FN1 | - | 2.9 | NTR1 | NTS1 | Neurotensin | A (Rhodopsin) | Rat | - | scFv16 | - |
neurotensin
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
|
peptide | Agonist | neuromedin N, neurotensin | peptide | Krumm BE, DiBerto JF, Olsen RHJ, Kang HJ, Slocum ST, Zhang S, Strachan RT, Huang XP, Slosky LM, Pinkerton AB, Barak LS, Caron MG, Kenakin T, Fay JF, Roth BL | 10.1021/ACS.BIOCHEM.3C00029 | 2023-03-29 | 55361 | |
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 | 55353 | |
Gq/11 | αq | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8HCX | 8HCX_refined | 3.5 | EDNRB | ETB | Endothelin | A (Rhodopsin) | Human | - | scFv16 | - |
ENDOTHELIN
chembl_ligand
pubchem
|
protein | Agonist | endothelin-3, endothelin-2, endothelin-1 | peptide | - | - | 2023-03-22 | 55363 | |
Gs | αs | Human | Mini-Gs | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8HJ0 | - | 3.1 | GPR21 | GPR21 | A orphans | A (Rhodopsin) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Lin X, Chen B, Wu Y, Han Y, Qi A, Wang J, Yang Z, Wei X, Zhao T, Wu L, Xie X, Sun J, Zheng J, Zhao S, Xu F | 10.1038/S41467-023-35882-W | 2023-03-15 | 55353 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8HS3 | - | 3.1 | GPR20 | GPR20 | A orphans | A (Rhodopsin) | Human | BRIL | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Lin X, Jiang S, Wu Y, Wei X, Han GW, Wu L, Liu J, Chen B, Zhang Z, Zhao S, Cherezov V, Xu F | 10.1038/S41421-023-00520-8 | 2023-03-08 | 55355 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 8ID4 | - | 3.1 | FFAR4 | FFA4 | Free fatty acid | A (Rhodopsin) | Human | - | scFv16 | - |
linoleic acid
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
small-molecule | Agonist | myristic acid, oleic acid, α-linolenic acid, linoleic acid | small-molecule | Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP | 10.1126/SCIENCE.ADD6220 | 2023-03-15 | 55355 | |
Gi/o | αi1 | Human | - | 56 | β1 | Human | γ2 | Human | Cryo-EM | 8ID9 | 8ID9_refined | 3.0 | FFAR4 | FFA4 | Free fatty acid | A (Rhodopsin) | Human | - | scFv16 | - |
EPA
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | myristic acid, oleic acid, α-linolenic acid, linoleic acid | small-molecule | Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP | 10.1126/SCIENCE.ADD6220 | 2023-03-15 | 55355 | |
Gi/o | αo | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7T94 | - | 3.2 | ACM2 | M2 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | Antibody fragment | - |
acetylcholine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
LY2119620 pubchem gtoplig chembl_ligand |
small-molecule small-molecule |
Agonist PAM |
acetylcholine | small-molecule | - | - | 2023-01-25 | 55361 | |
Gq/11 | αq | Human | - | 98 | β1 | Human | γ2 | Human | Cryo-EM | 7W3Z | - | 3.0 | GRPR | BB2 | Bombesin | A (Rhodopsin) | Human | - | scFv16 | - |
Gastrin-releasing peptide
pubchem
|
peptide | Agonist | GRP-(18-27), neuromedin B, gastrin releasing peptide(14-27) (human), neuromedin C, gastrin-releasing peptide | peptide | Peng S, Zhan Y, Zhang D, Ren L, Chen A, Chen ZF, Zhang H | 10.1073/PNAS.2216230120 | 2023-02-22 | 55363 | |
Gq/11 | αq | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8EIT | - | 2.8 | FFAR1 | FFA1 | Free fatty acid | A (Rhodopsin) | Human | - | scFv16 | - |
docosahexaenoic acid
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
pubchem
|
small-molecule | Agonist | oleic acid, docosahexaenoic acid, α-linolenic acid, myristic acid | small-molecule | Kumari P, Inoue A, Chapman K, Lian P, Rosenbaum DM | 10.1073/PNAS.2219569120 | 2023-05-24 | 55363 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 8IRS | - | 3.0 | DRD2 | D2 | Dopamine | A (Rhodopsin) | Human | BRIL | scFv16 | - |
rotigotine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | dopamine | small-molecule | Xu P, Huang S, Krumm BE, Zhuang Y, Mao C, Zhang Y, Wang Y, Huang XP, Liu YF, He X, Li H, Yin W, Jiang Y, Zhang Y, Roth BL, Xu HE | 10.1038/S41422-023-00808-0 | 2023-06-07 | 55355 | |
Gs | αs | Human | Mini-Gs | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8IW9 | - | 3.1 | TAAR9 | TAAR9 | A orphans | A (Rhodopsin) | Mouse | - |
scFv16 Nanobody-35 |
- |
Cadaverine
pubchem
|
small-molecule | Agonist | - | - | Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP | 10.1038/S41586-023-06106-4 | 2023-05-31 | 55353 | |
Gq/11 | αq | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8IBV | 8IBV_refined | 3.2 | MTLR | motilin | Motilin | A (Rhodopsin) | Human | BRIL | scFv16 | - |
motilin
pubchem
gtoplig
chembl_ligand
gtoplig
pubchem
pubchem
|
peptide | Agonist | motilin | peptide | You C, Zhang Y, Xu Y, Xu P, Li Z, Li H, Huang S, Chen Z, Li J, Xu HE, Jiang Y | 10.1126/SCIADV.ADE9020 | 2023-04-12 | 55363 | |
Gq/11 | αq | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8HJ5 | 8HJ5_refined | 3.0 | MRGX1 | MRGPRX1 | A orphans | A (Rhodopsin) | Human | BRIL |
scFv16 Nanobody-35 |
- |
compound 16 [PMID: 31498617]
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | bovine adrenal medulla peptide 8-22 | peptide | - | - | 2023-05-31 | 55363 | |
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 | PTH, PTHrP-(1-36), TIP39, PTHrP | 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 | 55353 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8G94 | 8G94_refined | 3.2 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
Early activation antigen CD69
pubchem
|
peptide | Agonist | sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate | small-molecule | Chen H, Qin Y, Chou M, Cyster JG, Li X | 10.7554/ELIFE.88204 | 2023-04-19 | 55355 | |
Gq/11 | αq | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8EJC | - | 3.0 | FFAR1 | FFA1 | Free fatty acid | A (Rhodopsin) | Human | - | scFv16 | - |
fasiglifam
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | oleic acid, docosahexaenoic acid, α-linolenic acid, myristic acid | small-molecule | Kumari P, Inoue A, Chapman K, Lian P, Rosenbaum DM | 10.1073/PNAS.2219569120 | 2023-05-24 | 55363 | |
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 | C5a des-Arg, ribosomal protein S19, C5a, 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 | 55355 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8IRV | 8IRV_refined | 3.1 | DRD5 | D5 | Dopamine | A (Rhodopsin) | Human | BRIL | - | - |
rotigotine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine, dopamine, (-)-noradrenaline | 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 | 55353 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8GUQ | 8GUQ_refined | 3.1 | CNR2 | CB2 | Cannabinoid | A (Rhodopsin) | Human | - | scFv16 | - |
olorinab
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | Li X, Chang H, Bouma J, de Paus LV, Mukhopadhyay P, Paloczi J, Mustafa M, van der Horst C, Kumar SS, Wu L, Yu Y, van den Berg RJBHN, Janssen APA, Lichtman A, Liu ZJ, Pacher P, van der Stelt M, Heitman LH, Hua T | 10.1038/S41467-023-37112-9 | 2023-05-10 | 55355 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8ITF | - | 3.5 | TAAR9 | TAAR9 | A orphans | A (Rhodopsin) | Mouse | - |
scFv16 Nanobody-35 |
- |
N,N-Dimethylcyclohexylamine
pubchem
|
small-molecule | Agonist | - | - | Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP | 10.1038/S41586-023-06106-4 | 2023-05-31 | 55353 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8GHV | 8GHV_refined | 2.8 | CNR1 | CB1 | Cannabinoid | A (Rhodopsin) | Human | - | scFv16 | - |
CHEMBL4208628
chembl_ligand
pubchem
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | Krishna Kumar K, Robertson MJ, Thadhani E, Wang H, Suomivuori CM, Powers AS, Ji L, Nikas SP, Dror RO, Inoue A, Makriyannis A, Skiniotis G, Kobilka B | 10.1038/S41467-023-37864-4 | 2023-05-24 | 55355 | |
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 | 55355 | |
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 | resolvin E1, chemerin C-terminal peptide, chemerin, 18R-HEPE, EPA | peptide | Wang J, Chen G, Liao Q, Lyu W, Liu A, Zhu L, Du Y, Ye RD | 10.1073/PNAS.2214324120 | 2023-04-19 | 55355 | |
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 | 55368 | |
Gs | αs | Human | Mini-Gs | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7YDP | - | 3.1 | AGRE5 | ADGRE5 | ADGRE | B2 (Adhesion) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Wang N, Qian Y, Xia R, Zhu X, Xiong Y, Zhang A, Guo C, He Y | 10.1016/J.CHEMBIOL.2023.08.003 | 2023-07-12 | 55353 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8F2B | - | 2.0 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - |
Nanobody-35 RAMP3 |
- |
Pramlintide analogue San45
|
peptide | Agonist | adrenomedullin 2/intermedin, amylin, β-CGRP, α-CGRP, calcitonin, adrenomedullin | 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 | 55353 | |
Gq/11 | αq | Human | Mini-Gq | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8H4K | - | 3.1 | FFAR4 | FFA4 | Free fatty acid | A (Rhodopsin) | Human | - | Nanobody-35 | - |
GW9508
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | myristic acid, oleic acid, α-linolenic acid, linoleic acid | small-molecule | Yin H, Inoue A, Ma Z, Zhu X, Xia R, Xu Z, Wang N, Duan Y, Zhang A, Guo C, He Y | 10.1038/S41422-023-00835-X | 2023-06-21 | 55363 | |
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 | 55355 | |
Gq/11 | αq | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8IUM | - | 3.1 | PF2R | FP | Prostanoid | A (Rhodopsin) | Human | - |
scFv16 Nanobody-35 |
- |
tafluprost acid
pubchem
gtoplig
|
small-molecule | Agonist | thromboxane A2, PGD2, PGE2, PGI2, PGF2α | 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 | 55363 | |
Gq/11 | αq | Human | - | 99 | β1 | Human | γ2 | Human | Cryo-EM | 8IYS | - | 3.0 | FFAR4 | FFA4 | Free fatty acid | A (Rhodopsin) | Human | - | scFv16 | - |
TUG-891
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | myristic acid, oleic acid, α-linolenic acid, linoleic acid | small-molecule | Yin H, Inoue A, Ma Z, Zhu X, Xia R, Xu Z, Wang N, Duan Y, Zhang A, Guo C, He Y | 10.1038/S41422-023-00835-X | 2023-06-21 | 55363 | |
Gi/o | αi3 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 8JD6 | - | 3.4 | GRM4 | mGlu4 | Metabotropic glutamate | C (Glutamate) | Human | - | scFv16 | - |
VU0364770
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | L-serine-O-phosphate, L-glutamic acid | small-molecule | Wang X, Wang M, Xu T, Feng Y, Shao Q, Han S, Chu X, Xu Y, Lin S, Zhao Q, Wu B | 10.1038/S41422-023-00830-2 | 2023-06-21 | 55357 | |
Gq/11 | αq | Human | GRK2 bound | 88 | - | - | - | - | Cryo-EM | 8JPC | - | 3.1 | NTR1 | NTS1 | Neurotensin | A (Rhodopsin) | Human | - | GRK2 | GRK2 |
JMV431
gtoplig
chembl_ligand
pubchem
CHEMBL4576388 chembl_ligand pubchem |
peptide small-molecule |
Agonist PAM |
neuromedin N, large neurotensin, neurotensin, large neuromedin N | peptide | Duan J, Liu H, Zhao F, Yuan Q, Ji Y, Cai X, He X, Li X, Li J, Wu K, Gao T, Zhu S, Lin S, Wang MW, Cheng X, Yin W, Jiang Y, Yang D, Xu HE | 10.1038/S41586-023-06395-9 | 2023-08-09 | 55363 | |
Gq/11 | αq | Human | - | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8THL | - | 3.1 | ADA1A | α1A | Adrenoceptors | A (Rhodopsin) | Human | T4-Lysozyme | scFv16 | - |
(-)-adrenaline
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline | small-molecule | Su M, Wang J, Xiang G, Do HN, Levitz J, Miao Y, Huang XY | 10.1038/S41467-023-40524-2 | 2023-08-16 | 55363 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 8G05 | - | 3.0 | GPR84 | GPR84 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
6-Octylimino-1,3-diazinane-2,4-dione
pubchem
|
lipid | Agonist | - | - | Zhang X, Wang Y, Supekar S, Cao X, Zhou J, Dang J, Chen S, Jenkins L, Marsango S, Li X, Liu G, Milligan G, Feng M, Fan H, Gong W, Zhang C | 10.1038/S41467-023-41201-0 | 2023-11-01 | 55355 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8GDA | - | 3.3 | PE2R4 | EP4 | Prostanoid | A (Rhodopsin) | Human | - | - | - |
(2S,5R)-5-[(1E,3S)-4,4-difluoro-3-hydroxy-4-phenylbut-1-en-1-yl]-1-[6-(1H-tetrazol-5-yl)hexyl]pyrrolidin-2-ol
pubchem
|
small-molecule | Agonist | thromboxane A2, PGD2, PGE1, PGE2, PGI2, PGF2α | 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 | 55353 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 8H2G | 8H2G_refined | 3.0 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | - | scFv16 | - |
nicotinic acid
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
pubchem
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | - | - | 2023-10-11 | 55355 | |
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 | 55361 | |
Gi/o | αi1 | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8HQM | 8HQM_refined | 3.0 | GP132 | GPR132 | A orphans | A (Rhodopsin) | Human | BRIL | scFv16 | - |
CHEMBL3354065
chembl_ligand
pubchem
|
small-molecule | Agonist | 9-hydroxyoctadecadienoic acid | small-molecule | Wang JL, Dou XD, Cheng J, Gao MX, Xu GF, Ding W, Ding JH, Li Y, Wang SH, Ji ZW, Zhao XY, Huo TY, Zhang CF, Liu YM, Sha XY, Gao JR, Zhang WH, Hao Y, Zhang C, Sun JP, Jiao N, Yu X | 10.1038/S42255-023-00899-4 | 2023-10-11 | 55355 | |
Gi/o | αi1 | Human | - | 62 | β1 | Mouse | γ2 | Mouse | Cryo-EM | 7Y15 | 7Y15_refined | 2.9 | MRGRD | MRGPRD | A orphans | A (Rhodopsin) | Human | BRIL | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | β-alanine | small-molecule | Suzuki S, Iida M, Hiroaki Y, Tanaka K, Kawamoto A, Kato T, Oshima A | 10.1038/S42003-022-03668-3 | 2022-07-20 | 55355 | |
Gs | αs | Bovine | - | 51 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 8DCS | - | 2.5 | ADRB1 | β1 | Adrenoceptors | A (Rhodopsin) | Wild turkey | T4-Lysozyme | Nanobody-35 | - |
4-{[(2S)-3-(tert-butylamino)-2-hydroxypropyl]oxy}-3H-indole-2-carbonitrile
pubchem
|
small-molecule | Agonist | - | - | Su M, Paknejad N, Zhu L, Wang J, Do HN, Miao Y, Liu W, Hite RK, Huang XY | 10.1038/S41467-022-31823-1 | 2022-07-27 | 55370 | |
Gq/11 | αq | Human | Gi2-mini-Gq chimera | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8DPH | - | 3.2 | 5HT2C | 5-HT2C | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | scFv16 | - |
lorcaserin
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Gumpper RH, Fay JF, Roth BL | 10.1016/J.CELREP.2022.111211 | 2022-08-24 | 55363 | |
Gi/o | αi1 | Human | - | 63 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7XAU | - | 3.0 | SSR2 | SST2 | Somatostatin | A (Rhodopsin) | Human | - | scFv16 | - |
Octreotide
|
peptide | Agonist | CST-17, cortistatin-14, SRIF-28, 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 | 55355 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7XMS | - | 2.9 | SSR4 | SST4 | Somatostatin | A (Rhodopsin) | Human | - | scFv16 | - |
SOMATOSTATIN
chembl_ligand
pubchem
|
protein | Agonist | CST-17, cortistatin-14, SRIF-28, 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 | 55355 | |
Gi/o | αi1 | Human | - | 65 | β1 | Human | γ2 | Human | Cryo-EM | 7XA3 | 7XA3_refined | 2.9 | CCR2 | CCR2 | Chemokine | A (Rhodopsin) | Human | - | scFv16 | - |
C-C motif chemokine 2
|
peptide | Agonist | CCL8, CCL26, CCL24, CCL7, CCL11, CCL2, CCL13, CCL16 | peptide | Shao Z, Tan Y, Shen Q, Hou L, Yao B, Qin J, Xu P, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Chen ZH, Jiang Y, Xu HE, Ying S, Ma H, Zhang Y, Shen H | 10.1038/S41421-022-00403-4 | 2022-08-24 | 55355 | |
Gi/o | αi1 | Human | - | 38 | β1 | Human | γ2 | Human | Cryo-EM | 7WU9 | 7WU9_refined | 3.4 | PE2R3 | EP3 | Prostanoid | A (Rhodopsin) | Human | - | scFv16 | - | - | - | - | thromboxane A2, PGD2, PGE1, PGE2, PGI2, PGF2α | small-molecule | Suno R, Sugita Y, Morimoto K, Takazaki H, Tsujimoto H, Hirose M, Suno-Ikeda C, Nomura N, Hino T, Inoue A, Iwasaki K, Kato T, Iwata S, Kobayashi T | 10.1016/J.CELREP.2022.111323 | 2022-08-17 | 55355 | |
Gs | αs | Human | - | 59 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7VVJ | 7VVJ_refined | 3.2 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
PTHrP[1-36]
|
peptide | Agonist | PTH, PTHrP-(1-36), TIP39, PTHrP | 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 | 55353 | |
Gs | αs | Human | - | 58 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7VVL | 7VVL_refined | 2.8 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
teriparatide
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
pubchem
pubchem
pubchem
pubchem
pubchem
|
peptide | Agonist | PTH, PTHrP-(1-36), TIP39, PTHrP | 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 | 55353 | |
Gs | αs | Human | - | 58 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7VVN | 7VVN_refined | 3.8 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
teriparatide
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
pubchem
pubchem
pubchem
pubchem
pubchem
|
peptide | Agonist | PTH, PTHrP-(1-36), TIP39, PTHrP | 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 | 55353 | |
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 | 55353 | |
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 | 55353 | |
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 | SEA, N-palmitoylethanolamine, N-oleoylethanolamide, anandamide | 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 | 55353 | |
Gs | αs | Human | Mini-Gs | 56 | β1 | Human | γ2 | Human | Cryo-EM | 7T9I | - | 2.9 | TSHR | TSH | Glycoprotein hormone | A (Rhodopsin) | Human | - | Nanobody-35 | - |
Thyrotropin subunit beta
Glycoprotein hormones alpha 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 | 55353 | |
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 | 55363 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7T2G | - | 2.5 | OPRM | μ | Opioid | A (Rhodopsin) | Mouse | BRIL | - | - |
CHEMBL58362
chembl_ligand
pubchem
|
small-molecule | Agonist | - | - | Qu Q, Huang W, Aydin D, Paggi JM, Seven AB, Wang H, Chakraborty S, Che T, DiBerto JF, Robertson MJ, Inoue A, Suomivuori CM, Roth BL, Majumdar S, Dror RO, Kobilka BK, Skiniotis G | 10.1038/S41589-022-01208-Y | 2022-12-07 | 55355 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7T2H | - | 3.2 | OPRM | μ | Opioid | A (Rhodopsin) | Mouse | - | scFv16 | - |
LOFENTANIL
chembl_ligand
pubchem
|
small-molecule | Agonist | - | - | Qu Q, Huang W, Aydin D, Paggi JM, Seven AB, Wang H, Chakraborty S, Che T, DiBerto JF, Robertson MJ, Inoue A, Suomivuori CM, Roth BL, Majumdar S, Dror RO, Kobilka BK, Skiniotis G | 10.1038/S41589-022-01208-Y | 2022-12-07 | 55355 | |
Gq/11 | α11 | Human | - | 62 | β1 | Rat | γ2 | Mouse | Cryo-EM | 7TRY | - | 3.7 | CRFR2 | CRF2 | Corticotropin-releasing factor | B1 (Secretin) | Human | - | - | - |
Urocortin
pubchem
|
peptide | Agonist | corticotrophin-releasing hormone, urocortin 2, urocortin 3, urocortin 1 | peptide | Zhao LH, Lin J, Ji SY, Zhou XE, Mao C, Shen DD, He X, Xiao P, Sun J, Melcher K, Zhang Y, Yu X, Xu HE | 10.1038/S41467-022-33851-3 | 2022-11-09 | 55364 | |
Gi/o | αo | Human | - | 63 | β1 | Rat | γ2 | Mouse | Cryo-EM | 7TS0 | 7TS0_refined | 2.8 | CRFR2 | CRF2 | Corticotropin-releasing factor | B1 (Secretin) | Human | - | scFv16 | - |
Urocortin
pubchem
|
peptide | Agonist | corticotrophin-releasing hormone, urocortin 2, urocortin 3, urocortin 1 | peptide | Zhao LH, Lin J, Ji SY, Zhou XE, Mao C, Shen DD, He X, Xiao P, Sun J, Melcher K, Zhang Y, Yu X, Xu HE | 10.1038/S41467-022-33851-3 | 2022-11-09 | 55361 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7U2K | - | 3.3 | OPRM | μ | Opioid | A (Rhodopsin) | Mouse | - | - | - |
CHEMBL147044
chembl_ligand
pubchem
|
small-molecule | Agonist | - | - | Faouzi A, Wang H, Zaidi SA, DiBerto JF, Che T, Qu Q, Robertson MJ, Madasu MK, El Daibani A, Varga BR, Zhang T, Ruiz C, Liu S, Xu J, Appourchaux K, Slocum ST, Eans SO, Cameron MD, Al-Hasani R, Pan YX, Roth BL, McLaughlin JP, Skiniotis G, Katritch V, Kobilka BK, Majumdar S | 10.1038/S41586-022-05588-Y | 2022-12-07 | 55355 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7VFX | 7VFX_refined | 2.8 | FPR1 | FPR1 | Formylpeptide | A (Rhodopsin) | Human | - | scFv16 | - |
Peptide agonist fMet-Ile-Phe-Leu
pubchem
|
peptide | Agonist | annexin I, fMet-Leu-Phe, spinorphin, cathepsin G | peptide | Chen G, Wang X, Liao Q, Ge Y, Jiao H, Chen Q, Liu Y, Lyu W, Zhu L, van Zundert GCP, Robertson MJ, Skiniotis G, Du Y, Hu H, Ye RD | 10.1038/S41467-022-32822-Y | 2022-09-21 | 55355 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7VIE | 7VIE_refined | 2.9 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
sphingosine 1-phosphate
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 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 | 55355 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7VIF | 7VIF_refined | 2.8 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
(S)-FTY720-phosphate
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 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 | 55355 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7VIG | 7VIG_refined | 2.9 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
icanbelimod
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 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 | 55355 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7VIH | 7VIH_refined | 3.0 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
icanbelimod
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 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 | 55355 | |
Gi/o | αo | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7W6P | - | 3.5 | ADA2A | α2A | Adrenoceptors | A (Rhodopsin) | Human | - | scFv16 | - |
N-pyridin-4-ylisoquinolin-4-amine
pubchem
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline | small-molecule | Fink EA, Xu J, Hubner H, Braz JM, Seemann P, Avet C, Craik V, Weikert D, Schmidt MF, Webb CM, Tolmachova NA, Moroz YS, Huang XP, Kalyanaraman C, Gahbauer S, Chen G, Liu Z, Jacobson MP, Irwin JJ, Bouvier M, Du Y, Shoichet BK, Basbaum AI, Gmeiner P | 10.1126/SCIENCE.ABN7065 | 2022-09-28 | 55361 | |
Gi/o | αo | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7W7E | - | 3.4 | ADA2A | α2A | Adrenoceptors | A (Rhodopsin) | Human | - | scFv16 | - |
5-(3-Bicyclo[4.2.0]octa-1,3,5-trienyl)-1,2,3,6-tetrahydropyridine
pubchem
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline | small-molecule | Fink EA, Xu J, Hubner H, Braz JM, Seemann P, Avet C, Craik V, Weikert D, Schmidt MF, Webb CM, Tolmachova NA, Moroz YS, Huang XP, Kalyanaraman C, Gahbauer S, Chen G, Liu Z, Jacobson MP, Irwin JJ, Bouvier M, Du Y, Shoichet BK, Basbaum AI, Gmeiner P | 10.1126/SCIENCE.ABN7065 | 2022-09-28 | 55361 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7WCM | 7WCM_refined | 2.3 | GP119 | GPR119 | GPR18, GPR55 and GPR119 | A (Rhodopsin) | Human | - | Nanobody-35 | - |
MBX-2982
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | SEA, N-palmitoylethanolamine, N-oleoylethanolamide, anandamide | 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 | 55353 | |
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 | SEA, N-palmitoylethanolamine, N-oleoylethanolamide, anandamide | 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 | 55353 | |
Gq/11 | αq | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7WXU | - | 2.9 | AGRF1 | ADGRF1 | ADGRF | B2 (Adhesion) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y | 10.1038/S41467-022-33173-4 | 2022-09-28 | 55363 | |
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 | 55353 | |
G12/13 | α13 | Human | - | 55 | β1 | Human | γ2 | Human | Cryo-EM | 7WY0 | - | 2.8 | AGRF1 | ADGRF1 | ADGRF | B2 (Adhesion) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y | 10.1038/S41467-022-33173-4 | 2022-09-28 | 55368 | |
Gs | αs | Human | Mini-Gs | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7WY8 | - | 2.8 | AGRL3 | ADGRL3 | ADGRL | B2 (Adhesion) | Mouse | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Qian Y, Ma Z, Liu C, Li X, Zhu X, Wang N, Xu Z, Xia R, Liang J, Duan Y, Yin H, Xiong Y, Zhang A, Guo C, Chen Z, Huang Z, He Y | 10.1016/J.MOLCEL.2022.10.009 | 2022-10-26 | 55353 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7WZ4 | - | 3.0 | GPR88 | GPR88 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Chen G, Xu J, Inoue A, Schmidt MF, Bai C, Lu Q, Gmeiner P, Liu Z, Du Y | 10.1038/S41467-022-30081-5 | 2022-10-26 | 55355 | |
G12/13 | α12 | Human | - | 55 | β1 | Human | γ2 | Human | Cryo-EM | 7X10 | - | 2.9 | AGRL3 | ADGRL3 | ADGRL | B2 (Adhesion) | Mouse | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Qian Y, Ma Z, Liu C, Li X, Zhu X, Wang N, Xu Z, Xia R, Liang J, Duan Y, Yin H, Xiong Y, Zhang A, Guo C, Chen Z, Huang Z, He Y | 10.1016/J.MOLCEL.2022.10.009 | 2022-11-09 | 55367 | |
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 | 55355 | |
Gi/o | αgust | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7XP5 | - | 3.1 | T2R46 | TAS2R46 | Taste 2 | T2 (Taste 2) | Human | - | Nanobody-35 | Endoglucanase H |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Xu W, Wu L, Liu S, Liu X, Cao X, Zhou C, Zhang J, Fu Y, Guo Y, Wu Y, Tan Q, Wang L, Liu J, Jiang L, Fan Z, Pei Y, Yu J, Cheng J, Zhao S, Hao X, Liu ZJ, Hua T | 10.1126/SCIENCE.ABO1633 | 2022-10-12 | 55360 | |
Gi/o | αo | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7Y24 | - | 3.3 | SSR2 | SST2 | Somatostatin | A (Rhodopsin) | Human | - | scFv16 | - |
Octreotide
|
peptide | Agonist | CST-17, cortistatin-14, SRIF-28, SRIF-14 | peptide | Chen S, Teng X, Zheng S | 10.1038/S41589-022-01130-3 | 2022-10-19 | 55361 | |
Gi/o | αi1 | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7Y89 | - | 3.0 | GPR17 | GPR17 | A orphans | A (Rhodopsin) | Human | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | UDP, LTD4, ATP, UDP-glucose, LTE4, UDP-galactose, LTC4 | small-molecule | Ye F, Wong TS, Chen G, Zhang Z, Zhang B, Gan S, Gao W, Li J, Wu Z, Pan X, Du Y | 10.1002/MCO2.159 | 2022-10-12 | 55355 | |
Gi/o | αi1 | Human | - | 63 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7YU5 | 7YU5_refined | 3.3 | LPAR1 | LPA1 | Lysophospholipid (LPA) | A (Rhodopsin) | Human | - | scFv16 | - |
[(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate
pubchem
|
small-molecule | Agonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O | 10.1038/S41467-022-33121-2 | 2022-10-05 | 55355 | |
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 | 55355 | |
Gq/11 | αq | Human | Gs-mini-Gq chimera | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8DWH | 8DWH_refined | 3.3 | MRGX1 | MRGPRX1 | A orphans | A (Rhodopsin) | Human | - | - | - |
compound 16 [PMID: 31498617]
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | bovine adrenal medulla peptide 8-22 | peptide | Liu Y, Cao C, Huang XP, Gumpper RH, Rachman MM, Shih SL, Krumm BE, Zhang S, Shoichet BK, Fay JF, Roth BL | 10.1038/S41589-022-01173-6 | 2022-11-02 | 55363 | |
Gs | αs | Human | - | 55 | β1 | Human | γ2 | Human | Cryo-EM | 8E3Z | 8E3Z_refined | 2.7 | VIPR1 | VPAC1 | VIP and PACAP | B1 (Secretin) | Human | - | Nanobody-35 | - |
Vasoactive intestinal polypeptide
pubchem
|
small-molecule | Agonist | PACAP-27, PACAP-38, GHRH, VIP, PHM, PHI, secretin | peptide | Piper SJ, Deganutti G, Lu J, Zhao P, Liang YL, Lu Y, Fletcher MM, Hossain MA, Christopoulos A, Reynolds CA, Danev R, Sexton PM, Wootten D | 10.1038/S41467-022-34629-3 | 2022-11-23 | 55353 | |
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 | 55363 | |
Gi/o | αi1 | Human | - | 64 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8EF5 | - | 3.3 | OPRM | μ | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
fentanyl
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | endomorphin-1, endomorphin-2, [Met]enkephalin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin A-(1-8), dynorphin B | 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 | 55355 | |
Gi/o | αi1 | Human | - | 64 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8EFL | 8EFL_refined | 3.2 | OPRM | μ | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
CHEMBL4452384
chembl_ligand
pubchem
|
small-molecule | Agonist | endomorphin-1, endomorphin-2, [Met]enkephalin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin A-(1-8), dynorphin B | 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 | 55355 | |
Gi/o | αi1 | Human | - | 63 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8F7R | - | 3.3 | OPRM | μ | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
endomorphin-1
pubchem
gtoplig
chembl_ligand
|
peptide | Agonist | endomorphin-1, endomorphin-2, [Met]enkephalin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin A-(1-8), dynorphin B | 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 | 55355 | |
Gi/o | αi1 | Human | - | 64 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8F7W | 8F7W_refined | 3.2 | OPRK | κ | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
dynorphin A-(1-8)
pubchem
gtoplig
chembl_ligand
pubchem
pubchem
|
peptide | Agonist | big dynorphin, β-neoendorphin, [Met]enkephalin, α-neoendorphin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin A-(1-8), dynorphin B | 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 | 55355 | |
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 | PTH, PTHrP-(1-36), TIP39, PTHrP | 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 | 55370 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7Y65 | - | 3.2 | C5AR1 | C5a1 | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
C5a
|
peptide | Agonist | C5a des-Arg, ribosomal protein S19, C5a, 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 | 55355 | |
Gi/o | αi2 | Human | - | 61 | β1 | Human | γ2 | Bovine | Cryo-EM | 7YK7 | 7YK7_refined | 2.8 | RL3R2 | RXFP4 | Relaxin family peptide | A (Rhodopsin) | Human | - | scFv16 | - |
DC591053
pubchem
gtoplig
|
small-molecule | Agonist | relaxin-3, relaxin-3 (B chain), INSL5 | peptide | Chen Y, Zhou Q, Wang J, Xu Y, Wang Y, Yan J, Wang Y, Zhu Q, Zhao F, Li C, Chen CW, Cai X, Bathgate RAD, Shen C, Eric Xu H, Yang D, Liu H, Wang MW | 10.1038/S41467-023-36182-Z | 2023-03-01 | 55356 | |
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 | 55353 | |
Gq/11 | αq | Human | Mini-Gq | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8FMZ | - | 2.6 | NTR1 | NTS1 | Neurotensin | A (Rhodopsin) | Rat | - | scFv16 | - |
neurotensin
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
|
peptide | Agonist | neuromedin N, neurotensin | peptide | Krumm BE, DiBerto JF, Olsen RHJ, Kang HJ, Slocum ST, Zhang S, Strachan RT, Huang XP, Slosky LM, Pinkerton AB, Barak LS, Caron MG, Kenakin T, Fay JF, Roth BL | 10.1021/ACS.BIOCHEM.3C00029 | 2023-03-29 | 55363 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8HBD | 8HBD_refined | 3.0 | EDNRB | ETB | Endothelin | A (Rhodopsin) | Human | - | scFv16 | - |
sovateltide
pubchem
gtoplig
chembl_ligand
gtoplig
pubchem
pubchem
pubchem
drugbank
|
peptide | Agonist | endothelin-3, endothelin-2, endothelin-1 | peptide | - | - | 2023-03-22 | 55355 | |
Gs | αs | Human | Mini-Gs | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8HDO | - | 2.9 | AA2BR | A2B | Adenosine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
BAY 60-6583
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | adenosine | small-molecule | Cai H, Xu Y, Guo S, He X, Sun J, Li X, Li C, Yin W, Cheng X, Jiang H, Xu HE, Xie X, Jiang Y | 10.1038/S41421-022-00503-1 | 2023-01-18 | 55353 | |
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 | 55353 | |
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 | 55353 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8HSC | - | 3.2 | GPR20 | GPR20 | A orphans | A (Rhodopsin) | Human | BRIL |
Antibody fab fragment light chain Antibody fab fragment heavy chain scFv16 |
- |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Lin X, Jiang S, Wu Y, Wei X, Han GW, Wu L, Liu J, Chen B, Zhang Z, Zhao S, Cherezov V, Xu F | 10.1038/S41421-023-00520-8 | 2023-03-08 | 55355 | |
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, oleic acid, α-linolenic acid, linoleic acid | small-molecule | Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP | 10.1126/SCIENCE.ADD6220 | 2023-03-15 | 55355 | |
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, oleic acid, α-linolenic acid, linoleic acid | small-molecule | Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP | 10.1126/SCIENCE.ADD6220 | 2023-03-15 | 55355 | |
Gi/o | αo | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7T90 | 7T90_refined | 3.3 | ACM2 | M2 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | scFv16 | - |
acetylcholine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
|
small-molecule | Agonist | acetylcholine | small-molecule | - | - | 2023-01-25 | 55361 | |
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
chembl_ligand
drugbank
|
small-molecule | Agonist | relaxin-3, relaxin-1, relaxin | peptide | - | - | 2023-02-15 | 55353 | |
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 | 55355 | |
Gs | αs | Human | - | 54 | β1 | Human | γ2 | Human | Cryo-EM | 8FU6 | 8FU6_refined | 2.9 | GLR | glucagon | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
Glucagon derivative ZP3780
|
peptide | Agonist | glucagon | peptide | Krishna Kumar K, O'Brien ES, Habrian CH, Latorraca NR, Wang H, Tuneew I, Montabana E, Marqusee S, Hilger D, Isacoff EY, Mathiesen JM, Kobilka BK | 10.1016/J.CELL.2023.02.028 | 2023-04-12 | 55353 | |
Gs | αs | Human | - | 45 | β1 | Human | γ2 | Human | Cryo-EM | 8IW4 | - | 3.5 | TAAR9 | TAAR9 | A orphans | A (Rhodopsin) | Mouse | - | scFv16 | - |
SPERMIDINE
chembl_ligand
pubchem
|
small-molecule | Agonist | - | - | Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP | 10.1038/S41586-023-06106-4 | 2023-05-31 | 55353 | |
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 | 55363 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7XV3 | 7XV3_refined | 2.8 | GP174 | GPR174 | A orphans | A (Rhodopsin) | Human | - | - | - |
(2~{S})-2-$l^{4}-azanyl-3-[[(2~{R})-3-octadecanoyloxy-2-oxidanyl-propoxy]-oxidanyl-oxidanylidene-$l^{6}-phosphanyl]oxy-propanoic acid
pubchem
|
small-molecule | Agonist | lysophosphatidylserine | small-molecule | Liang J, Inoue A, Ikuta T, Xia R, Wang N, Kawakami K, Xu Z, Qian Y, Zhu X, Zhang A, Guo C, Huang Z, He Y | 10.1038/S41467-023-36575-0 | 2023-02-15 | 55353 | |
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 | big dynorphin, β-neoendorphin, [Met]enkephalin, α-neoendorphin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin A-(1-8), dynorphin B | 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 | 55355 | |
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 | 55355 | |
Gi/o | αo | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7XJJ | 7XJJ_refined | 3.3 | GALR1 | GAL1 | Galanin | A (Rhodopsin) | Human | - | scFv16 | - |
galanin
pubchem
gtoplig
chembl_ligand
gtoplig
pubchem
pubchem
pubchem
pubchem
|
peptide | Agonist | galanin-like peptide, galanin | peptide | - | - | 2023-05-03 | 55361 | |
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 | big dynorphin, β-neoendorphin, [Met]enkephalin, α-neoendorphin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin A-(1-8), dynorphin B | peptide | Chen Y, Chen B, Wu T, Zhou F, Xu F | 10.1093/PROCEL/PWAC033 | 2023-05-24 | 55355 | |
Gs | αs | Human | Mini-Gs | 57 | β1 | Human | γ2 | Human | Cryo-EM | 7XY7 | - | 3.3 | AA2BR | A2B | Adenosine | A (Rhodopsin) | Human | BRIL | - | - |
NECA
pubchem
gtoplig
chembl_ligand
gtoplig
|
small-molecule | Agonist | adenosine | small-molecule | Chen Y, Zhang J, Weng Y, Xu Y, Lu W, Liu W, Liu M, Hua T, Song G | 10.1126/SCIADV.ADD3709 | 2023-05-03 | 55353 | |
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 | CST-17, cortistatin-14, SRIF-28, 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 | 55355 | |
Gi/o | αi1 | Human | - | 63 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8HK3 | 8HK3_refined | 3.2 | C3AR | C3a | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | C5a, C3a | peptide | Wang Y, Liu W, Xu Y, He X, Yuan Q, Luo P, Fan W, Zhu J, Zhang X, Cheng X, Jiang Y, Xu HE, Zhuang Y | 10.1038/S41589-023-01339-W | 2023-05-10 | 55355 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8FLQ | - | 2.6 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
Parathyroid hormone
|
peptide | Agonist | PTH, PTHrP-(1-36), TIP39, PTHrP | 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 | 55353 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7TRK | - | 2.8 | ACM4 | M4 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | scFv16 | - |
iperoxo
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | acetylcholine | small-molecule | - | - | 2023-05-17 | 55355 | |
Gq/11 | αq | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8EJK | - | 3.4 | FFAR1 | FFA1 | Free fatty acid | A (Rhodopsin) | Human | - | scFv16 | - |
fasiglifam
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | oleic acid, docosahexaenoic acid, α-linolenic acid, myristic acid | small-molecule | Kumari P, Inoue A, Chapman K, Lian P, Rosenbaum DM | 10.1073/PNAS.2219569120 | 2023-05-24 | 55363 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8IA8 | - | 2.9 | C3AR | C3a | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
ALA-SER-LYS-LEU-GLY-LEU-ALA-ARG
|
peptide | Agonist | C5a, C3a | peptide | - | - | 2023-05-24 | 55355 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8FLU | - | 2.8 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
PTH
|
peptide | Agonist | PTH, PTHrP-(1-36), TIP39, PTHrP | 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 | 55353 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7TRP | - | 2.4 | ACM4 | M4 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | scFv16 | - |
iperoxo
pubchem
gtoplig
chembl_ligand
LY2033298 pubchem gtoplig chembl_ligand |
small-molecule small-molecule |
Agonist PAM |
acetylcholine | small-molecule | - | - | 2023-05-17 | 55355 | |
Gs | αs | Human | - | 57 | β1 | Human | γ2 | Human | Cryo-EM | 7XY6 | - | 3.0 | AA2BR | A2B | Adenosine | A (Rhodopsin) | Human | BRIL | - | - |
BAY 60-6583
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | adenosine | small-molecule | Chen Y, Zhang J, Weng Y, Xu Y, Lu W, Liu W, Liu M, Hua T, Song G | 10.1126/SCIADV.ADD3709 | 2023-05-03 | 55353 | |
Gs | αs | Human | - | 57 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7Y36 | - | 2.8 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
teriparatide
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
pubchem
pubchem
pubchem
pubchem
pubchem
|
peptide | Agonist | PTH, PTHrP-(1-36), TIP39, PTHrP | peptide | - | - | 2023-07-05 | 55353 | |
Gq/11 | αq | Human | Mini-Gq | 46 | - | - | - | - | Cryo-EM | 7YM8 | 7YM8_refined | 2.9 | ADA1A | α1A | Adrenoceptors | A (Rhodopsin) | Human | - | Nanobody-29 | - |
oxymetazoline
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline | small-molecule | Toyoda Y, Zhu A, Kong F, Shan S, Zhao J, Wang N, Sun X, Zhang L, Yan C, Kobilka BK, Liu X | 10.1038/S41467-023-39310-X | 2023-07-05 | 55363 | |
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 2/intermedin, amylin, β-CGRP, α-CGRP, calcitonin, adrenomedullin | 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 | 55353 | |
Gs | αs | Human | - | 58 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8GW8 | - | 2.9 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
PCO371
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | PTH, PTHrP-(1-36), TIP39, PTHrP | peptide | Kobayashi K, Kawakami K, Kusakizako T, Tomita A, Nishimura M, Sawada K, Okamoto HH, Hiratsuka S, Nakamura G, Kuwabara R, Noda H, Muramatsu H, Shimizu M, Taguchi T, Inoue A, Murata T, Nureki O | 10.1038/S41586-023-06169-3 | 2023-06-14 | 55353 | |
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, oleic acid, α-linolenic acid, linoleic acid | small-molecule | Yin H, Inoue A, Ma Z, Zhu X, Xia R, Xu Z, Wang N, Duan Y, Zhang A, Guo C, He Y | 10.1038/S41422-023-00835-X | 2023-06-21 | 55353 | |
Gi/o | αi1 | Human | - | 65 | β1 | Human | γ2 | Human | Cryo-EM | 8IC0 | - | 3.4 | CXCR1 | CXCR1 | Chemokine | A (Rhodopsin) | Human | - | scFv16 | - |
Interleukin-8
pubchem
|
protein | Agonist | cytokine domain of tyrosyl tRNA synthetase, CXCL6, CXCL8 | peptide | Ishimoto N, Park JH, Kawakami K, Tajiri M, Mizutani K, Akashi S, Tame JRH, Inoue A, Park SY | 10.1038/S41467-023-39799-2 | 2023-07-19 | 55355 | |
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 | 55355 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8JD3 | - | 3.3 | GRM2 | mGlu2 | Metabotropic glutamate | C (Glutamate) | Human | - | - | - |
L-glutamic acid
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
pubchem
JNJ-40411813 pubchem gtoplig chembl_ligand drugbank |
small-molecule small-molecule |
Agonist PAM |
L-glutamic acid | small-molecule | Wang X, Wang M, Xu T, Feng Y, Shao Q, Han S, Chu X, Xu Y, Lin S, Zhao Q, Wu B | 10.1038/S41422-023-00830-2 | 2023-06-21 | 55355 | |
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 | PTH, PTHrP-(1-36), TIP39, PTHrP | 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 | 55353 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 8JD5 | - | 3.6 | GRM2 | mGlu2 | Metabotropic glutamate | C (Glutamate) | Human | - | scFv16 | - |
L-glutamic acid
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
pubchem
ADX88178 pubchem gtoplig chembl_ligand JNJ-40411813 pubchem gtoplig chembl_ligand drugbank |
small-molecule small-molecule small-molecule |
Agonist | L-glutamic acid | small-molecule | Wang X, Wang M, Xu T, Feng Y, Shao Q, Han S, Chu X, Xu Y, Lin S, Zhao Q, Wu B | 10.1038/S41422-023-00830-2 | 2023-06-21 | 55355 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8PM2 | - | 2.9 | TAA7F | TAAR7F | A orphans | A (Rhodopsin) | Mouse | - | Nanobody-35 | - |
N,N-Dimethylcyclohexylamine
pubchem
|
small-molecule | Agonist | - | - | Gusach A, Lee Y, Khoshgrudi AN, Mukhaleva E, Ma N, Koers EJ, Chen Q, Edwards PC, Huang F, Kim J, Mancia F, Verprintsev DB, Vaidehi N, Weyand SN, Tate CG | 10.1101/2023.07.07.547762 | 2023-08-09 | 55353 | |
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 | 55363 | |
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 | big dynorphin, β-neoendorphin, [Met]enkephalin, α-neoendorphin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin A-(1-8), dynorphin B | peptide | Muratspahic E, Deibler K, Han J, Tomasevic N, Jadhav KB, Olive-Marti AL, Hochrainer N, Hellinger R, Koehbach J, Fay JF, Rahman MH, Hegazy L, Craven TW, Varga BR, Bhardwaj G, Appourchaux K, Majumdar S, Muttenthaler M, Hosseinzadeh P, Craik DJ, Spetea M, Che T, Baker D, Gruber CW | 10.1038/s41467-023-43718-w | 2023-12-06 | 55355 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8GCP | 8GCP_refined | 3.1 | PE2R4 | EP4 | Prostanoid | A (Rhodopsin) | Human | - | scFv16 | - |
PGE2
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
|
small-molecule | Agonist | thromboxane A2, PGD2, PGE1, PGE2, PGI2, PGF2α | small-molecule | Huang SM, Xiong MY, Liu L, Mu J, Wang MW, Jia YL, Cai K, Tie L, Zhang C, Cao S, Wen X, Wang JL, Guo SC, Li Y, Qu CX, He QT, Cai BY, Xue C, Gan S, Xie Y, Cong X, Yang Z, Kong W, Li S, Li Z, Xiao P, Yang F, Yu X, Guan YF, Zhang X, Liu Z, Yang BX, Du Y, Sun JP | 10.1073/PNAS.2216329120 | 2024-01-03 | 55355 | |
Gs | αs | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8HJ1 | 8HJ1_refined | 3.3 | GPR21 | GPR21 | A orphans | A (Rhodopsin) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Lin X, Chen B, Wu Y, Han Y, Qi A, Wang J, Yang Z, Wei X, Zhao T, Wu L, Xie X, Sun J, Zheng J, Zhao S, Xu F | 10.1038/S41467-023-35882-W | 2023-12-27 | 55353 | |
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 | CXCL11, CXCL9, CXCL12α, CCL19, CCL20, CCL7, CCL11, CXCL10, CCL13, CCL5 | 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 | 55355 | |
Gi/o | αi1 | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8HQN | 8HQN_refined | 3.0 | GP132 | GPR132 | A orphans | A (Rhodopsin) | Human | BRIL | scFv16 | - |
9-hydroxyoctadecadienoic acid
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | 9-hydroxyoctadecadienoic acid | small-molecule | Wang JL, Dou XD, Cheng J, Gao MX, Xu GF, Ding W, Ding JH, Li Y, Wang SH, Ji ZW, Zhao XY, Huo TY, Zhang CF, Liu YM, Sha XY, Gao JR, Zhang WH, Hao Y, Zhang C, Sun JP, Jiao N, Yu X | 10.1038/S42255-023-00899-4 | 2023-10-11 | 55355 | |
Gi/o | αo | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8I97 | 8I97_refined | 3.2 | C3AR | C3a | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | C5a, C3a | peptide | Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C | 10.1016/J.CELL.2023.09.020 | 2023-10-18 | 55361 | |
Gi/o | αo | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8I9S | 8I9S_refined | 3.3 | C3AR | C3a | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | C5a, C3a | peptide | Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C | 10.1016/J.CELL.2023.09.020 | 2023-10-18 | 55361 | |
Gi/o | αi1 | Human | - | 62 | β1 | Mouse | γ2 | Mouse | Cryo-EM | 8IHB | - | 2.9 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | BRIL | - | - |
GSK256073
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | Suzuki S, Tanaka K, Nishikawa K, Suzuki H, Oshima A, Fujiyoshi Y | 10.1038/S41467-023-41650-7 | 2023-09-13 | 55355 | |
Gi/o | αi1 | Human | - | 62 | β1 | Mouse | γ2 | Mouse | Cryo-EM | 8IHH | - | 3.1 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | BRIL | scFv16 | - |
5-butyl-1H-pyrazole-3-carboxylic acid
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | Suzuki S, Tanaka K, Nishikawa K, Suzuki H, Oshima A, Fujiyoshi Y | 10.1038/S41467-023-41650-7 | 2023-08-30 | 55355 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8IJA | - | 2.7 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | - | scFv16 | - |
nicotinic acid
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
pubchem
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | Pan X, Ye F, Ning P, Zhang Z, Li X, Zhang B, Wang Q, Chen G, Gao W, Qiu C, Wu Z, Li J, Zhu L, Xia J, Gong K, Du Y | 10.1038/S41421-023-00610-7 | 2024-01-03 | 55355 | |
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 | 55353 | |
Gs | αs | Bovine | - | 59 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8ITL | - | 3.2 | GIPR | GIP | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | gastric inhibitory polypeptide | peptide | Zhao F, Hang K, Zhou Q, Shao L, Li H, Li W, Lin S, Dai A, Cai X, Liu Y, Xu Y, Feng W, Yang D, Wang MW | 10.1073/PNAS.2306145120 | 2023-10-18 | 55370 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8IZB | - | 3.1 | GP174 | GPR174 | A orphans | A (Rhodopsin) | Human | - | Nanobody-35 | - |
LYSOPHOSPHATIDIC ACID
chembl_ligand
pubchem
L-serine pubchem gtoplig chembl_ligand drugbank drug_central pubchem |
small-molecule small-molecule |
Agonist | lysophosphatidylserine | small-molecule | Liu G, Li X, Wang Y, Zhang X, Gong W | 10.1371/JOURNAL.PBIO.3002387 | 2023-11-01 | 55353 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 8J6R | - | 2.8 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | - | scFv16 | - |
MK 6892
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | Mao C, Gao M, Zang SK, Zhu Y, Shen DD, Chen LN, Yang L, Wang Z, Zhang H, Wang WW, Shen Q, Lu Y, Ma X, Zhang Y | 10.1038/S41467-023-43537-Z | 2023-12-06 | 55355 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 8JIL | - | 3.5 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | - | scFv16 | - |
nicotinic acid
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
pubchem
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | Zhao C, Wang H, Liu Y, Cheng L, Wang B, Tian X, Fu H, Wu C, Li Z, Shen C, Yu J, Yang S, Hu H, Fu P, Ma L, Wang C, Yan W, Shao Z | 10.1016/J.MOLCEL.2023.07.030 | 2023-09-06 | 55355 | |
Gs | αs | Human | - | 62 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8JIP | 8JIP_refined | 2.9 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
MEDI0382
|
peptide | Agonist | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | 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 | 55353 | |
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 | 55353 | |
Gs | αs | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8JLN | - | 3.2 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Human | BRIL | scFv16 | - |
CHEMBL1182312
chembl_ligand
chembl_ligand
pubchem
|
small-molecule | Agonist | octopamine, tyramine, β-phenylethylamine, 3-iodothyronamine, dopamine, CHEMBL1160703, (+)-Octopamine | 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 | 55353 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8JLQ | - | 2.8 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Human | BRIL | scFv16 | - |
fenoldopam
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
gtoplig
chembl_ligand
pubchem
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | octopamine, tyramine, β-phenylethylamine, 3-iodothyronamine, dopamine, CHEMBL1160703, (+)-Octopamine | 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 | 55353 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Mouse | Cryo-EM | 8JSO | 8JSO_refined | 3.4 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Human | BRIL | scFv16 | - |
dexamfetamine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | octopamine, tyramine, β-phenylethylamine, 3-iodothyronamine, dopamine, CHEMBL1160703, (+)-Octopamine | 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 | 55353 | |
Gi/o | αo | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8JZZ | 8JZZ_refined | 3.3 | C5AR1 | C5a1 | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
C5a des-Arg
gtoplig
|
peptide | Agonist | C5a des-Arg, ribosomal protein S19, 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 | 55361 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8KH4 | 8KH4_refined | 3.1 | GP161 | GPR161 | A orphans | A (Rhodopsin) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Nie Y, Qiu Z, Chen S, Chen Z, Song X, Ma Y, Huang N, Cyster JG, Zheng S | 10.1038/S41467-023-41654-3 | 2023-10-11 | 55353 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8W87 | - | 2.8 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
METHAMPHETAMINE
chembl_ligand
pubchem
|
small-molecule | Agonist | octopamine, tyramine, β-phenylethylamine, 3-iodothyronamine, dopamine, CHEMBL1160703, (+)-Octopamine | 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 | 55353 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8W89 | - | 3.0 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
2-Phenylethanaminium
pubchem
|
small-molecule | Agonist | octopamine, tyramine, β-phenylethylamine, 3-iodothyronamine, dopamine, CHEMBL1160703, (+)-Octopamine | 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 | 55353 | |
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 | 55353 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8WC4 | - | 3.1 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Mouse | - | scFv16 | - |
CHEMBL476516
chembl_ligand
pubchem
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine | 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 | 55353 | |
Gq/11 | αq | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8WC9 | - | 3.2 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Mouse | - | scFv16 | - |
CHEMBL476516
chembl_ligand
pubchem
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine | 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 | 55363 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 8WRB | - | 2.9 | GPR34 | GPR34 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
LYSOPHOSPHATIDIC ACID
chembl_ligand
pubchem
|
small-molecule | Agonist | lysophosphatidylserine | small-molecule | Liu G, Li X, Wang Y, Zhang X, Gong W | 10.1371/JOURNAL.PBIO.3002387 | 2023-11-08 | 55355 | |
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 | 55353 | |
Gq/11 | αq | Human | - | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8THK | - | 2.6 | ADA1A | α1A | Adrenoceptors | A (Rhodopsin) | Human | T4-Lysozyme | scFv16 | - |
CHEMBL133451
chembl_ligand
pubchem
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline | small-molecule | Su M, Wang J, Xiang G, Do HN, Levitz J, Miao Y, Huang XY | 10.1038/S41467-023-40524-2 | 2023-08-16 | 55363 | |
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 | 55397 | |
Gs | αs | Human | - | 54 | β1 | Human | γ2 | Human | Cryo-EM | 8GD9 | - | 3.2 | PE2R4 | EP4 | Prostanoid | A (Rhodopsin) | Human | - | - | - |
4-({2-[(1R,2R,3R,5S)-3,5-dihydroxy-2-{(3S)-3-hydroxy-4-[3-(methoxymethyl)phenyl]butyl}cyclopentyl]ethyl}sulfanyl)butanoic acid
pubchem
|
small-molecule | Agonist | thromboxane A2, PGD2, PGE1, PGE2, PGI2, PGF2α | 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 | 55353 | |
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, PGD2, PGE1, PGE2, PGI2, PGF2α | 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 | 55355 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8HN8 | - | 3.0 | HRH4 | H4 | Histamine | A (Rhodopsin) | Human | - | scFv16 | - |
histamine
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
gtoplig
|
small-molecule | Agonist | histamine, CCL16 | small-molecule | - | - | 2023-12-20 | 55355 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 8HOC | - | 3.0 | HRH4 | H4 | Histamine | A (Rhodopsin) | Human | - | scFv16 | - |
imetit
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | histamine, CCL16 | small-molecule | - | - | 2023-12-20 | 55355 | |
Gi/o | αi1 | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8HQE | 8HQE_refined | 3.0 | GP132 | GPR132 | A orphans | A (Rhodopsin) | Human | BRIL | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | 9-hydroxyoctadecadienoic acid | small-molecule | Wang JL, Dou XD, Cheng J, Gao MX, Xu GF, Ding W, Ding JH, Li Y, Wang SH, Ji ZW, Zhao XY, Huo TY, Zhang CF, Liu YM, Sha XY, Gao JR, Zhang WH, Hao Y, Zhang C, Sun JP, Jiao N, Yu X | 10.1038/S42255-023-00899-4 | 2023-10-11 | 55355 | |
Gs | αs | Human | - | 40 | β1 | Human | γ2 | Human | Cryo-EM | 8HTI | - | 3.0 | O52E4 | OR52E4 | Odorant family 52 | O1 (fish-like odorant) | Human | - | Nanobody-35 | - |
OCTANOIC ACID
chembl_ligand
pubchem
pubchem
|
small-molecule | Agonist | - | - | Choi C, Bae J, Kim S, Lee S, Kang H, Kim J, Bang I, Kim K, Huh WK, Seok C, Park H, Im W, Choi HJ | 10.1038/S41467-023-43983-9 | 2023-12-20 | 55353 | |
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 | 55363 | |
Gq/11 | αq | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8IA7 | 8IA7_refined | 3.1 | GASR | CCK2 | Cholecystokinin | A (Rhodopsin) | Human | - | - | - |
CHEMBL216166
chembl_ligand
pubchem
|
protein | Agonist | CCK-33, CCK-4, gastrin-71, desulfated gastrin-71, desulfated gastrin-14, gastrin-14, desulfated gastrin-17, gastrin-17, gastrin-34, CCK-39, desulfated gastrin-34, desulfated cholecystokinin-8, CCK-8, CCK-58 | 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 | 55363 | |
Gi/o | αi1 | Human | - | 62 | β1 | Mouse | γ2 | Mouse | Cryo-EM | 8IHF | - | 3.0 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | BRIL | scFv16 | - |
MK 6892
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | Suzuki S, Tanaka K, Nishikawa K, Suzuki H, Oshima A, Fujiyoshi Y | 10.1038/S41467-023-41650-7 | 2023-08-30 | 55355 | |
Gi/o | αi1 | Human | - | 62 | β1 | Mouse | γ2 | Mouse | Cryo-EM | 8IHJ | 8IHJ_refined | 3.1 | HCAR3 | HCA3 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | BRIL | scFv16 | - |
(5S)-5-methyl-4-oxo-5-phenylfuran-2-carboxylic acid
pubchem
|
small-molecule | Agonist | 3-hydroxyoctanoic acid | small-molecule | Suzuki S, Tanaka K, Nishikawa K, Suzuki H, Oshima A, Fujiyoshi Y | 10.1038/S41467-023-41650-7 | 2023-08-30 | 55355 | |
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 | 55355 | |
Gs | αs | Human | Gi1-Gs chimera | 60 | β1 | Human | γ2 | Bovine | Cryo-EM | 8IOC | - | 2.9 | MC3R | MC3 | Melanocortin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
γ-MSH
pubchem
gtoplig
pubchem
|
peptide | Agonist | 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 | 55353 | |
Gs | αs | Bovine | - | 59 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8ITM | - | 3.1 | GIPR | GIP | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | gastric inhibitory polypeptide | peptide | Zhao F, Hang K, Zhou Q, Shao L, Li H, Li W, Lin S, Dai A, Cai X, Liu Y, Xu Y, Feng W, Yang D, Wang MW | 10.1073/PNAS.2306145120 | 2023-10-18 | 55370 | |
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 | 55355 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 8JHY | - | 2.9 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | - | scFv16 | - |
compound 9n [PMID: 18752940]
pubchem
gtoplig
chembl_ligand
|
small-molecule | PAM | β-D-hydroxybutyric acid, butyric acid | small-molecule | Zhao C, Wang H, Liu Y, Cheng L, Wang B, Tian X, Fu H, Wu C, Li Z, Shen C, Yu J, Yang S, Hu H, Fu P, Ma L, Wang C, Yan W, Shao Z | 10.1016/J.MOLCEL.2023.07.030 | 2023-09-06 | 55355 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 8JIM | - | 3.0 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | - | scFv16 | - |
CHEMBL3354065
chembl_ligand
pubchem
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | Zhao C, Wang H, Liu Y, Cheng L, Wang B, Tian X, Fu H, Wu C, Li Z, Shen C, Yu J, Yang S, Hu H, Fu P, Ma L, Wang C, Yan W, Shao Z | 10.1016/J.MOLCEL.2023.07.030 | 2023-09-06 | 55355 | |
Gs | αs | Human | - | 58 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8JIR | 8JIR_refined | 2.6 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
SAR425899
|
peptide | Agonist | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | 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 | 55353 | |
Gs | αs | Human | - | 59 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8JIU | 8JIU_refined | 2.8 | GLR | glucagon | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
SAR425899
|
peptide | Agonist | glucagon | peptide | Li Y, Zhou Q, Dai A, Zhao F, Chang R, Ying T, Wu B, Yang D, Wang MW, Cong Z | 10.1073/PNAS.2303696120 | 2023-09-13 | 55353 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8JLK | - | 3.2 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Mouse | - | scFv16 | - |
ulotaront
pubchem
gtoplig
drugbank
chembl_ligand
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine | 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 | 55353 | |
Gs | αs | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8JLP | - | 3.2 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Human | - | - | - |
ralmitaront
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | octopamine, tyramine, β-phenylethylamine, 3-iodothyronamine, dopamine, CHEMBL1160703, (+)-Octopamine | 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 | 55353 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8JSP | - | 3.7 | 5HT1A | 5-HT1A | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | scFv16 | - |
ulotaront
pubchem
gtoplig
drugbank
chembl_ligand
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z | 10.1038/S41586-023-06804-Z | 2023-11-15 | 55355 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8K4N | 8K4N_refined | 2.8 | GPR34 | GPR34 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
(2R)-2-azanyl-3-[oxidanyl-[(2R)-2-oxidanyl-3-tetradec-9-enoyloxy-propoxy]phosphoryl]oxy-propanoic acid
pubchem
|
small-molecule | Agonist | lysophosphatidylserine | small-molecule | - | - | 2023-10-25 | 55355 | |
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 | 55353 | |
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 | 55355 | |
Gs | αs | Human | - | 56 | β1 | Human | γ2 | Human | Cryo-EM | 8TB0 | 8TB0_refined | 3.5 | GPR61 | GPR61 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | - | - | 2023-10-04 | 55353 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8W88 | - | 2.6 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
ulotaront
pubchem
gtoplig
drugbank
chembl_ligand
|
small-molecule | Agonist | octopamine, tyramine, β-phenylethylamine, 3-iodothyronamine, dopamine, CHEMBL1160703, (+)-Octopamine | 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 | 55353 | |
Gi/o | αi2 | Human | - | 0 | β1 | Human | γ2 | Human | Cryo-EM | 8W8A | - | 2.8 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
CHEMBL3684869
chembl_ligand
pubchem
|
small-molecule | Agonist | octopamine, tyramine, β-phenylethylamine, 3-iodothyronamine, dopamine, CHEMBL1160703, (+)-Octopamine | 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 | 55356 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8W8R | - | 3.3 | GP101 | GPR101 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
1-(4-Methylpyridin-2-yl)-3-[3-(trifluoromethyl)phenyl]thiourea
pubchem
|
small-molecule | Agonist | - | - | Yang Z, Wang JY, Yang F, Zhu KK, Wang GP, Guan Y, Ning SL, Lu Y, Li Y, Zhang C, Zheng Y, Zhou SH, Wang XW, Wang MW, Xiao P, Yi F, Zhang C, Zhang PJ, Xu F, Liu BH, Zhang H, Yu X, Gao N, Sun JP | 10.1038/S41589-023-01456-6 | 2024-01-03 | 55353 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8WC6 | - | 3.2 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Mouse | - |
scFv16 Nanobody-35 |
- |
2-Phenylethanaminium
pubchem
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine | 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 | 55353 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8WCA | - | 3.5 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Human | - | scFv16 | - |
2-Phenylethanaminium
pubchem
|
small-molecule | Agonist | octopamine, tyramine, β-phenylethylamine, 3-iodothyronamine, dopamine, CHEMBL1160703, (+)-Octopamine | 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 | 55353 | |
Gq/11 | αq | Human | Gi2-mini-Gq chimera | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8WPU | - | 3.1 | CASR | CaS | Calcium-sensing | C (Glutamate) | Human | - | scFv16 | - |
cinacalcet
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
Calcium pubchem |
small-molecule small-molecule |
Agonist | L-tryptophan, spermine, Mg2+, Ca2+ | small-molecule | Ling S, Meng X, Zhang Y, Xia Z, Zhou Y, Yang F, Shi P, Shi C, Tian C | 10.1038/S41422-023-00892-2 | 2023-11-22 | 55363 | |
Gi/o | αo | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8I95 | - | 2.9 | C3AR | C3a | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
EP54 ligand
|
peptide | Agonist | C5a, C3a | peptide | Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C | 10.1016/J.CELL.2023.09.020 | 2023-10-18 | 55361 | |
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 | C5a des-Arg, ribosomal protein S19, 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 | 55361 | |
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 | 55355 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8IJ3 | 8IJ3_refined | 3.3 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | β-D-hydroxybutyric acid, butyric acid | small-molecule | Pan X, Ye F, Ning P, Zhang Z, Li X, Zhang B, Wang Q, Chen G, Gao W, Qiu C, Wu Z, Li J, Zhu L, Xia J, Gong K, Du Y | 10.1038/S41421-023-00610-7 | 2024-01-03 | 55355 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8IJD | - | 3.3 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | - | scFv16 | - |
MK 6892
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | Pan X, Ye F, Ning P, Zhang Z, Li X, Zhang B, Wang Q, Chen G, Gao W, Qiu C, Wu Z, Li J, Zhu L, Xia J, Gong K, Du Y | 10.1038/S41421-023-00610-7 | 2024-01-03 | 55355 | |
Gs | αs | Human | Gi1-Gs chimera | 59 | β1 | Human | γ2 | Bovine | Cryo-EM | 8IOD | - | 2.6 | MC5R | MC5 | Melanocortin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
PG-901
pubchem
|
peptide | Agonist | 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 | 55353 | |
Gi/o | αo | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8J6D | 8J6D_refined | 3.1 | C3AR | C3a | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
EP141 peptide agonist
|
peptide | Agonist | C5a, C3a | peptide | Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C | 10.1016/J.CELL.2023.09.020 | 2023-10-18 | 55361 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 8J6Q | - | 2.6 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | - | scFv16 | - |
β-D-hydroxybutyric acid
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | Mao C, Gao M, Zang SK, Zhu Y, Shen DD, Chen LN, Yang L, Wang Z, Zhang H, Wang WW, Shen Q, Lu Y, Ma X, Zhang Y | 10.1038/S41467-023-43537-Z | 2023-12-06 | 55355 | |
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 | 55355 | |
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 | 55353 | |
Gs | αs | Human | - | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8JIS | 8JIS_refined | 2.5 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
Dual-agonist peptide P15
|
peptide | Agonist | glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) | peptide | Li Y, Zhou Q, Dai A, Zhao F, Chang R, Ying T, Wu B, Yang D, Wang MW, Cong Z | 10.1073/PNAS.2303696120 | 2023-11-08 | 55353 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8JLJ | - | 3.1 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Mouse | BRIL | scFv16 | - |
CHEMBL1182312
chembl_ligand
chembl_ligand
pubchem
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine | 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 | 55353 | |
Gs | αs | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8JLO | - | 3.5 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Human | - | - | - |
ulotaront
pubchem
gtoplig
drugbank
chembl_ligand
|
small-molecule | Agonist | octopamine, tyramine, β-phenylethylamine, 3-iodothyronamine, dopamine, CHEMBL1160703, (+)-Octopamine | 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 | 55353 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8JLR | - | 3.0 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Human | BRIL | scFv16 | - |
(1~{S},3~{R})-3-(1-adamantyl)-1-(aminomethyl)-3,4-dihydro-1~{H}-isochromene-5,6-diol
pubchem
|
small-molecule | Agonist | octopamine, tyramine, β-phenylethylamine, 3-iodothyronamine, dopamine, CHEMBL1160703, (+)-Octopamine | 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 | 55353 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 8JZ7 | 8JZ7_refined | 2.6 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | - | scFv16 | - |
MK 6892
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | Cheng L, Sun S, Wang H, Zhao C, Tian X, Liu Y, Fu P, Shao Z, Chai R, Yan W | 10.1038/S41392-023-01625-Y | 2023-10-04 | 55355 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8K2X | 8K2X_refined | 3.2 | CXCR3 | CXCR3 | Chemokine | A (Rhodopsin) | Human | BRIL | scFv16 | - |
C-X-C motif chemokine 10
|
small-molecule | Agonist | CXCL11, CXCL9, CXCL12α, CCL19, CCL20, CCL7, CCL11, CXCL10, CCL13, CCL5 | peptide | Jiao H, Pang B, Chiang YC, Chen Q, Pan Q, Ren R, Hu H | 10.1038/S41421-023-00617-0 | 2023-11-29 | 55355 | |
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 | 55353 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8SG1 | - | 2.9 | CML1 | chemerin | Chemerin receptor | A (Rhodopsin) | Human | - | scFv16 | - |
chemerin C-terminal peptide
pubchem
gtoplig
chembl_ligand
pubchem
|
peptide | Agonist | resolvin E1, chemerin C-terminal peptide, chemerin, 18R-HEPE, EPA | peptide | Zhang X, Weiss T, Cheng MH, Chen S, Ambrosius CK, Czerniak AS, Li K, Feng M, Bahar I, Beck-Sickinger AG, Zhang C | 10.1371/JOURNAL.PBIO.3002188 | 2023-11-01 | 55355 | |
Gs | αs | Human | - | 55 | β1 | Human | γ2 | Human | Cryo-EM | 8U26 | 8U26_refined | 2.5 | NK1R | NK1 | Tachykinin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
substance P
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
|
peptide | Agonist | substance P, hemokinin 1, neuropeptide-γ, neurokinin A, neurokinin B, neuropeptide K | peptide | Chen M, Schmid MF, Chiu W | 10.1038/S41592-023-02082-9 | 2023-11-15 | 55353 | |
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 | 55355 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8WC3 | - | 3.0 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Mouse | - | scFv16 | - |
ulotaront
pubchem
gtoplig
drugbank
chembl_ligand
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine | 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 | 55353 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8WC7 | - | 3.1 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Mouse | - | scFv16 | - |
2-[4-(3-Fluorophenyl)phenyl]ethan-1-amine
pubchem
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine | 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 | 55353 | |
Gq/11 | αq | Human | - | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8WCB | - | 3.1 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Mouse | - | scFv16 | - |
Cyclohexylammonium ion
pubchem
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine | 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 | 55363 | |
Gi/o | αi1 | Human | - | 62 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8XBH | 8XBH_refined | 2.8 | GPR34 | GPR34 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
CHEMBL4758243
chembl_ligand
pubchem
|
small-molecule | Agonist | lysophosphatidylserine | small-molecule | - | - | 2023-12-27 | 55355 | |
Gs | αs2 | Rat | - | 100 | β1 | Human | γ2 | Human | Cryo-EM | 8UHB | - | 3.4 | - | - | - | - | - | - | Nanobody-35 | - | - | - | - | - | - | Zilberg G, Parpounas AK, Warren AL, Yang S, Wacker D | 38168118 | 2024-01-10 | 55372 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 1AZS | - | 2.3 | - | - | - | - | - | - | - |
VC1 IIC2 |
- | - | - | - | - | Tesmer JJ, Sunahara RK, Gilman AG, Sprang SR | 9417641 | 1998-02-25 | 55370 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 1AZT | - | 2.3 | - | - | - | - | - | - | - | - | - | - | - | - | - | Sunahara RK, Tesmer JJ, Gilman AG, Sprang SR | 9395396 | 1998-02-25 | 55370 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 1CJK | - | 3.0 | - | - | - | - | - | - | - |
Adenylate cyclase type V ADENYLATE CYCLASE TYPE II |
- | - | - | - | - | Tesmer JJ, Sunahara RK, Johnson RA, Gosselin G, Gilman AG, Sprang SR | 10427002 | 1999-08-31 | 55370 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 1CJT | - | 2.8 | - | - | - | - | - | - | - |
Adenylate cyclase type V ADENYLATE CYCLASE TYPE II |
- | - | - | - | - | Tesmer JJ, Sunahara RK, Johnson RA, Gosselin G, Gilman AG, Sprang SR | 10427002 | 1999-08-31 | 55370 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 1CJU | - | 2.8 | - | - | - | - | - | - | - |
Adenylate cyclase type V ADENYLATE CYCLASE TYPE II |
- | - | - | - | - | Tesmer JJ, Sunahara RK, Johnson RA, Gosselin G, Gilman AG, Sprang SR | 10427002 | 1999-08-31 | 55370 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 1CJV | - | 3.0 | - | - | - | - | - | - | - |
Adenylate cyclase type V ADENYLATE CYCLASE TYPE II |
- | - | - | - | - | Tesmer JJ, Sunahara RK, Johnson RA, Gosselin G, Gilman AG, Sprang SR | 10427002 | 1999-08-31 | 55370 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 1CS4 | - | 2.5 | - | - | - | - | - | - | - |
TYPE V ADENYLATE CYCLASE TYPE II ADENYLATE CYCLASE |
- | - | - | - | - | Tesmer JJ, Dessauer CW, Sunahara RK, Murray LD, Johnson RA, Gilman AG, Sprang SR | 11087399 | 2001-01-10 | 55370 | |
Gs | αs2 | Bovine | - | 96 | - | - | - | - | X-ray | 1CUL | - | 2.4 | - | - | - | - | - | - | - |
TYPE V ADENYLYL CYCLASE TYPE II ADENYLYL CYCLASE |
- | - | - | - | - | Tesmer JJ, Dessauer CW, Sunahara RK, Murray LD, Johnson RA, Gilman AG, Sprang SR | 11087399 | 2001-01-10 | 55370 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 1TL7 | - | 2.8 | - | - | - | - | - | - | - |
Adenylate cyclase type V Adenylate cyclase type II |
- | - | - | - | - | Mou TC, Gille A, Fancy DA, Seifert R, Sprang SR | 15591060 | 2004-12-14 | 55370 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 1U0H | - | 2.9 | - | - | - | - | - | - | - |
Adenylate cyclase type V Adenylate cyclase type II |
- | - | - | - | - | Mou TC, Gille A, Fancy DA, Seifert R, Sprang SR | 15591060 | 2004-12-14 | 55370 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 2GVD | - | 2.9 | - | - | - | - | - | - | - |
Adenylate cyclase type 5 Adenylate cyclase type 2 |
- | - | - | - | - | Mou TC, Gille A, Suryanarayana S, Richter M, Seifert R, Sprang SR | 16766715 | 2006-07-04 | 55370 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 2GVZ | - | 3.3 | - | - | - | - | - | - | - |
Adenylate cyclase type 5 Adenylate cyclase type 2 |
- | - | - | - | - | Mou TC, Gille A, Suryanarayana S, Richter M, Seifert R, Sprang SR | 16766715 | 2006-07-04 | 55370 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 3C14 | - | 2.7 | - | - | - | - | - | - | - |
Adenylate cyclase type 5 Adenylate cyclase type 2 |
- | - | - | - | - | Mou TC, Masada N, Cooper DM, Sprang SR | 19243146 | 2009-02-03 | 55370 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 3C15 | - | 2.8 | - | - | - | - | - | - | - |
Adenylate cyclase type 5 Adenylate cyclase type 2 |
- | - | - | - | - | Mou TC, Masada N, Cooper DM, Sprang SR | 19243146 | 2009-02-03 | 55370 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 3C16 | - | 2.9 | - | - | - | - | - | - | - |
Adenylate cyclase type 5 Adenylate cyclase type 2 |
- | - | - | - | - | Mou TC, Masada N, Cooper DM, Sprang SR | 19243146 | 2009-02-03 | 55370 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 3G82 | - | 3.1 | - | - | - | - | - | - | - |
Adenylate cyclase type 5 Adenylate cyclase type 2 |
- | - | - | - | - | - | - | 2010-02-16 | 55370 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 3MAA | - | 3.0 | - | - | - | - | - | - | - |
Adenylate cyclase type 5 Adenylate cyclase type 2 |
- | - | - | - | - | Mou TC, Masada N, Cooper DM, Sprang SR | 19243146 | 2010-04-07 | 55370 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | Cryo-EM | 6R3Q | - | 3.4 | - | - | - | - | - | - | - | Adenylate cyclase 9 | - | - | - | - | - | Qi C, Sorrentino S, Medalia O, Korkhov VM | 31023924 | 2019-05-08 | 55370 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | Cryo-EM | 6R4O | - | 4.2 | - | - | - | - | - | - | - | Adenylate cyclase 9 | - | - | - | - | - | Qi C, Sorrentino S, Medalia O, Korkhov VM | 31023924 | 2019-05-08 | 55370 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | Cryo-EM | 6R4P | - | 3.1 | - | - | - | - | - | - | - | Adenylate cyclase 9 | - | - | - | - | - | Qi C, Sorrentino S, Medalia O, Korkhov VM | 31023924 | 2019-05-08 | 55370 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | Cryo-EM | 7PDE | - | 4.5 | - | - | - | - | - | - | - | Adenylate cyclase 9 | - | - | - | - | - | Qi C, Lavriha P, Mehta V, Khanppnavar B, Mohammed I, Li Y, Lazaratos M, Schaefer JV, Dreier B, Pluckthun A, Bondar AN, Dessauer CW, Korkhov VM | 35210418 | 2022-01-19 | 55370 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | Cryo-EM | 7PDF | - | 3.8 | - | - | - | - | - | - | - | Adenylate cyclase 9 | - | - | - | - | - | Qi C, Lavriha P, Mehta V, Khanppnavar B, Mohammed I, Li Y, Lazaratos M, Schaefer JV, Dreier B, Pluckthun A, Bondar AN, Dessauer CW, Korkhov VM | 35210418 | 2022-01-26 | 55370 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | Cryo-EM | 8BUZ | - | 3.5 | - | - | - | - | - | - | - | Adenylate cyclase type 8 | - | - | - | - | - | Khanppnavar B, Schuster D, Lavriha P, Uliana F, Ozel M, Mehta V, Leitner A, Picotti P, Korkhov VM | 38351373 | 2023-12-13 | 55370 | |
Gs | αs2 | Human | - | 96 | - | - | - | - | X-ray | 6AU6 | - | 1.7 | - | - | - | - | - | - | - | - | - | - | - | - | - | Hu Q, Shokat KM | 29628140 | 2018-05-09 | 55353 | |
Gs | αs2 | Human | - | 97 | β1 | Human | γ2 | Human | X-ray | 6EG8 | - | 2.8 | - | - | - | - | - | - | - | - | - | - | - | - | - | Liu X, Xu X, Hilger D, Aschauer P, Tiemann JKS, Du Y, Liu H, Hirata K, Sun X, Guixa-Gonzalez R, Mathiesen JM, Hildebrand PW, Kobilka BK | 31080070 | 2019-06-05 | 55353 | |
Gs | αs2 | Human | - | 96 | - | - | - | - | X-ray | 7BPH | - | 1.6 | - | - | - | - | - | - | - | GN13 | - | - | - | - | - | Dai SA, Hu Q, Gao R, Blythe EE, Touhara KK, Peacock H, Zhang Z, von Zastrow M, Suga H, Shokat KM | 36170854 | 2021-03-31 | 55353 | |
Gs | αs2 | Human | - | 88 | - | - | - | - | X-ray | 7E5E | - | 2.0 | - | - | - | - | - | - | - | GD20 | - | - | - | - | - | Dai SA, Hu Q, Gao R, Blythe EE, Touhara KK, Peacock H, Zhang Z, von Zastrow M, Suga H, Shokat KM | 36170854 | 2022-03-02 | 55353 | |
Gs | αs2 | Human | - | 96 | - | - | - | - | Cryo-EM | 8EL7 | - | 2.8 | - | - | - | - | - | - | - | Isoform 1 of Synembryn-B | - | - | - | - | - | Papasergi-Scott MM, Kwarcinski FE, Yu M, Panova O, Ovrutsky AM, Skiniotis G, Tall GG | 36931277 | 2023-03-01 | 55353 | |
Gs | αl | Mouse | - | 100 | - | - | - | - | X-ray | 8HTG | - | 2.9 | - | - | - | - | - | - | - | - | - | - | - | - | - | Choi C, Bae J, Kim S, Lee S, Kang H, Kim J, Bang I, Kim K, Huh WK, Seok C, Park H, Im W, Choi HJ | 38062020 | 2023-12-20 | 55388 | |
Gs | αl | Human | - | 100 | - | - | - | - | Cryo-EM | 8EL8 | - | 3.2 | - | - | - | - | - | - | - | Isoform 1 of Synembryn-B | - | - | - | - | - | Papasergi-Scott MM, Kwarcinski FE, Yu M, Panova O, Ovrutsky AM, Skiniotis G, Tall GG | 36931277 | 2023-03-01 | 55354 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1AGR | - | 2.8 | - | - | - | - | - | - | - | RGS4 | - | - | - | - | - | Tesmer JJ, Berman DM, Gilman AG, Sprang SR | 9108480 | 1997-06-16 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1AS0 | - | 2.0 | - | - | - | - | - | - | - | - | - | - | - | - | - | Raw AS, Coleman DE, Gilman AG, Sprang SR | 9398294 | 1997-11-12 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1AS2 | - | 2.8 | - | - | - | - | - | - | - | - | - | - | - | - | - | Raw AS, Coleman DE, Gilman AG, Sprang SR | 9398294 | 1997-11-12 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1AS3 | - | 2.4 | - | - | - | - | - | - | - | - | - | - | - | - | - | Raw AS, Coleman DE, Gilman AG, Sprang SR | 9398294 | 1997-11-12 | 55415 | |
Gi/o | αi1 | Rat | - | 89 | - | - | - | - | X-ray | 1BH2 | - | 2.1 | - | - | - | - | - | - | - | - | - | - | - | - | - | Posner BA, Mixon MB, Wall MA, Sprang SR, Gilman AG | 9705312 | 1998-11-04 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1BOF | - | 2.2 | - | - | - | - | - | - | - | - | - | - | - | - | - | Coleman DE, Sprang SR | 9772163 | 1999-01-06 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1CIP | - | 1.5 | - | - | - | - | - | - | - | - | - | - | - | - | - | Coleman DE, Sprang SR | 10358003 | 1999-04-09 | 55415 | |
Gi/o | αi1 | Rat | - | 92 | - | - | - | - | X-ray | 1FQJ | - | 2.0 | - | - | - | - | - | - | - | Regulator of G-protein signaling 9 | - | - | - | - | - | Slep KC, Kercher MA, He W, Cowan CW, Wensel TG, Sigler PB | 11234020 | 2001-02-28 | 55415 | |
Gi/o | αi1 | Rat | - | 92 | - | - | - | - | X-ray | 1FQK | - | 2.3 | - | - | - | - | - | - | - | Regulator of G-protein signaling 9 | - | - | - | - | - | Slep KC, Kercher MA, He W, Cowan CW, Wensel TG, Sigler PB | 11234020 | 2001-02-28 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1GDD | - | 2.2 | - | - | - | - | - | - | - | - | - | - | - | - | - | Mixon MB, Lee E, Coleman DE, Berghuis AM, Gilman AG, Sprang SR | 7481799 | 1995-11-27 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1GFI | - | 2.2 | - | - | - | - | - | - | - | - | - | - | - | - | - | Coleman DE, Berghuis AM, Lee E, Linder ME, Gilman AG, Sprang SR | 8073283 | 1995-03-31 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | β1 | Bovine | γ2 | Bovine | X-ray | 1GG2 | - | 2.4 | - | - | - | - | - | - | - | - | - | - | - | - | - | Wall MA, Coleman DE, Lee E, Iniguez-Lluhi JA, Posner BA, Gilman AG, Sprang SR | 8521505 | 1997-02-12 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1GIA | - | 2.0 | - | - | - | - | - | - | - | - | - | - | - | - | - | Coleman DE, Berghuis AM, Lee E, Linder ME, Gilman AG, Sprang SR | 8073283 | 1994-09-30 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1GIL | - | 2.3 | - | - | - | - | - | - | - | - | - | - | - | - | - | Coleman DE, Berghuis AM, Lee E, Linder ME, Gilman AG, Sprang SR | 8073283 | 1995-02-14 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1GIT | - | 2.6 | - | - | - | - | - | - | - | - | - | - | - | - | - | Berghuis AM, Lee E, Raw AS, Gilman AG, Sprang SR | 8939752 | 1997-02-12 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | β1 | Bovine | γ2 | Bovine | X-ray | 1GP2 | - | 2.3 | - | - | - | - | - | - | - | - | - | - | - | - | - | Wall MA, Coleman DE, Lee E, Iniguez-Lluhi JA, Posner BA, Gilman AG, Sprang SR | 8521505 | 1997-02-12 | 55415 | |
Gi/o | αi1 | Rat | - | 96 | - | - | - | - | X-ray | 1SHZ | - | 2.9 | - | - | - | - | - | - | - |
Guanine Nucleotide-Binding Protein Galpha(13):Galpha(i1) Chimera Rho guanine nucleotide exchange factor 1 |
- | - | - | - | - | Chen Z, Singer WD, Sternweis PC, Sprang SR | 15665872 | 2005-01-18 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1SVK | - | 2.0 | - | - | - | - | - | - | - | - | - | - | - | - | - | Thomas CJ, Du X, Li P, Wang Y, Ross EM, Sprang SR | 15128951 | 2004-06-01 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1SVS | - | 1.5 | - | - | - | - | - | - | - | - | - | - | - | - | - | Thomas CJ, Du X, Li P, Wang Y, Ross EM, Sprang SR | 15128951 | 2004-06-01 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | β1 | Bovine | γ2 | Bovine | X-ray | 2BCJ | - | 3.1 | - | - | - | - | - | - | - | G-protein-coupled receptor kinase 2 | - | - | - | - | - | Tesmer VM, Kawano T, Shankaranarayanan A, Kozasa T, Tesmer JJ | 16339447 | 2005-12-20 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 2RGN | - | 3.5 | - | - | - | - | - | - | - |
Rho guanine nucleotide exchange factor 25 Transforming protein RhoA |
- | - | - | - | - | Lutz S, Shankaranarayanan A, Coco C, Ridilla M, Nance MR, Vettel C, Baltus D, Evelyn CR, Neubig RR, Wieland T, Tesmer JJ | 18096806 | 2008-01-15 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 2ZJY | - | 2.8 | - | - | - | - | - | - | - | - | - | - | - | - | - | - | - | 2009-03-24 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 2ZJZ | - | 2.6 | - | - | - | - | - | - | - | - | - | - | - | - | - | - | - | 2009-03-24 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | β1 | Bovine | γ2 | Bovine | X-ray | 3AH8 | - | 2.9 | - | - | - | - | - | - | - | YM-254890 | - | - | - | - | - | Nishimura A, Kitano K, Takasaki J, Taniguchi M, Mizuno N, Tago K, Hakoshima T, Itoh H | 20639466 | 2010-07-21 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 3D7M | - | 2.9 | - | - | - | - | - | - | - | - | - | - | - | - | - | Preininger AM, Funk MA, Oldham WM, Meier SM, Johnston CA, Adhikary S, Kimple AJ, Siderovski DP, Hamm HE, Iverson TM | 19222191 | 2009-03-03 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 3FFA | - | 2.3 | - | - | - | - | - | - | - | - | - | - | - | - | - | Kapoor N, Menon ST, Chauhan R, Sachdev P, Sakmar TP | 19703466 | 2009-10-06 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 3FFB | - | 2.6 | - | - | - | - | - | - | - | - | - | - | - | - | - | Kapoor N, Menon ST, Chauhan R, Sachdev P, Sakmar TP | 19703466 | 2009-10-06 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 3V00 | - | 2.9 | - | - | - | - | - | - | - | - | - | - | - | - | - | Singh G, Ramachandran S, Cerione RA | 22448927 | 2012-04-18 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 4N0D | - | 1.6 | - | - | - | - | - | - | - | - | - | - | - | - | - | Thaker TM, Sarwar M, Preininger AM, Hamm HE, Iverson TM | 24596087 | 2014-03-12 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 4N0E | - | 2.1 | - | - | - | - | - | - | - | - | - | - | - | - | - | Thaker TM, Sarwar M, Preininger AM, Hamm HE, Iverson TM | 24596087 | 2014-03-12 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 4PAM | - | 2.1 | - | - | - | - | - | - | - | - | - | - | - | - | - | Kaya AI, Lokits AD, Gilbert JA, Iverson TM, Meiler J, Hamm HE | 25037222 | 2014-07-30 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 4PAN | - | 2.4 | - | - | - | - | - | - | - | - | - | - | - | - | - | Kaya AI, Lokits AD, Gilbert JA, Iverson TM, Meiler J, Hamm HE | 25037222 | 2014-07-30 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 4PAO | - | 2.0 | - | - | - | - | - | - | - | - | - | - | - | - | - | Kaya AI, Lokits AD, Gilbert JA, Iverson TM, Meiler J, Hamm HE | 25037222 | 2014-07-30 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 4PAQ | - | 2.0 | - | - | - | - | - | - | - | - | - | - | - | - | - | Kaya AI, Lokits AD, Gilbert JA, Iverson TM, Meiler J, Hamm HE | 25037222 | 2014-07-30 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 5KDL | - | 2.7 | - | - | - | - | - | - | - | - | - | - | - | - | - | Kaya AI, Lokits AD, Gilbert JA, Iverson TM, Meiler J, Hamm HE | 27462082 | 2016-08-03 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | β1 | Bovine | γT1 | Bovine | X-ray | 5KDO | - | 1.9 | - | - | - | - | - | - | - | - | - | - | - | - | - | Kaya AI, Lokits AD, Gilbert JA, Iverson TM, Meiler J, Hamm HE | 27462082 | 2016-08-03 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 6M8H | - | 2.1 | - | - | - | - | - | - | - | - | - | - | - | - | - | - | - | 2019-08-21 | 55415 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 6TYL | - | 3.3 | - | - | - | - | - | - |
Nanobody A Nanobody B Nanobody C |
Resistance to inhibitors of cholinesterase 8 homolog A (C. elegans) | - | - | - | - | - | McClelland LJ, Zhang K, Mou TC, Johnston J, Yates-Hansen C, Li S, Thomas CJ, Doukov TI, Triest S, Wohlkonig A, Tall GG, Steyaert J, Chiu W, Sprang SR | 32103024 | 2020-03-11 | 55415 | |
Gi/o | αi1 | Rat | - | 91 | - | - | - | - | Cryo-EM | 6UKT | - | 3.9 | - | - | - | - | - | - |
NB8109 NB8117 NB8119 NB9156 |
Resistance to inhibitors of cholinesterase 8 homolog A (C. elegans) | - | - | - | - | - | McClelland LJ, Zhang K, Mou TC, Johnston J, Yates-Hansen C, Li S, Thomas CJ, Doukov TI, Triest S, Wohlkonig A, Tall GG, Steyaert J, Chiu W, Sprang SR | 32103024 | 2020-03-11 | 55415 | |
Gi/o | αi1 | Human | - | 92 | - | - | - | - | X-ray | 1KJY | - | 2.7 | - | - | - | - | - | - | - | Regulator of G-protein signaling 14 | - | - | - | - | - | Kimple RJ, Kimple ME, Betts L, Sondek J, Siderovski DP | 11976690 | 2002-05-08 | 55355 | |
Gi/o | αi1 | Human | - | 93 | - | - | - | - | X-ray | 1Y3A | - | 2.5 | - | - | - | - | - | - | - | KB752 peptide | - | - | - | - | - | Johnston CA, Willard FS, Jezyk MR, Fredericks Z, Bodor ET, Jones MB, Blaesius R, Watts VJ, Harden TK, Sondek J, Ramer JK, Siderovski DP | 16004878 | 2005-07-12 | 55355 | |
Gi/o | αi1 | Human | - | 88 | - | - | - | - | X-ray | 2G83 | - | 2.8 | - | - | - | - | - | - | - | KB-1753 phage display peptide | - | - | - | - | - | Johnston CA, Lobanova ES, Shavkunov AS, Low J, Ramer JK, Blaesius R, Fredericks Z, Willard FS, Kuhlman B, Arshavsky VY, Siderovski DP | 16981699 | 2006-10-10 | 55355 | |
Gi/o | αi1 | Human | - | 91 | - | - | - | - | X-ray | 2GTP | - | 2.6 | - | - | - | - | - | - | - | Regulator of G-protein signaling 1 | - | - | - | - | - | Soundararajan M, Willard FS, Kimple AJ, Turnbull AP, Ball LJ, Schoch GA, Gileadi C, Fedorov OY, Dowler EF, Higman VA, Hutsell SQ, Sundstrom M, Doyle DA, Siderovski DP | 18434541 | 2006-05-23 | 55355 | |
Gi/o | αi1 | Human | - | 92 | - | - | - | - | X-ray | 2IK8 | - | 2.7 | - | - | - | - | - | - | - | Regulator of G-protein signaling 16 | - | - | - | - | - | Soundararajan M, Willard FS, Kimple AJ, Turnbull AP, Ball LJ, Schoch GA, Gileadi C, Fedorov OY, Dowler EF, Higman VA, Hutsell SQ, Sundstrom M, Doyle DA, Siderovski DP | 18434541 | 2006-11-21 | 55355 | |
Gi/o | αi1 | Human | - | 92 | - | - | - | - | X-ray | 2OM2 | - | 2.2 | - | - | - | - | - | - | - | Regulator of G-protein signalling 14 GoLoco motif peptide | - | - | - | - | - | Sammond DW, Eletr ZM, Purbeck C, Kimple RJ, Siderovski DP, Kuhlman B | 17603074 | 2007-07-10 | 55355 | |
Gi/o | αi1 | Human | - | 92 | - | - | - | - | X-ray | 2XNS | - | 3.4 | - | - | - | - | - | - | - | Regulator of G-protein signaling 14 | - | - | - | - | - | Sammond DW, Bosch DE, Butterfoss GL, Purbeck C, Machius M, Siderovski DP, Kuhlman B | 21388199 | 2011-06-08 | 55355 | |
Gi/o | αi1 | Human | - | 93 | - | - | - | - | X-ray | 3ONW | - | 2.4 | - | - | - | - | - | - | - | Regulator of G-protein signaling 14 | - | - | - | - | - | Bosch DE, Kimple AJ, Sammond DW, Muller RE, Miley MJ, Machius M, Kuhlman B, Willard FS, Siderovski DP | 21115486 | 2010-11-24 | 55355 | |
Gi/o | αi1 | Human | - | 92 | - | - | - | - | X-ray | 3QE0 | - | 3.0 | - | - | - | - | - | - | - | KB752 peptide | - | - | - | - | - | Bosch DE, Willard FS, Ramanujam R, Kimple AJ, Willard MD, Naqvi NI, Siderovski DP | 22383884 | 2012-01-25 | 55355 | |
Gi/o | αi1 | Human | - | 93 | - | - | - | - | X-ray | 3QI2 | - | 2.8 | - | - | - | - | - | - | - | Regulator of G-protein signaling 14 | - | - | - | - | - | Bosch DE, Willard FS, Ramanujam R, Kimple AJ, Willard MD, Naqvi NI, Siderovski DP | 22383884 | 2012-02-01 | 55355 | |
Gi/o | αi1 | Human | - | 100 | - | - | - | - | X-ray | 3UMR | - | 2.0 | - | - | - | - | - | - | - | - | - | - | - | - | - | - | - | 2012-10-24 | 55355 | |
Gi/o | αi1 | Human | - | 100 | - | - | - | - | X-ray | 3UMS | - | 2.3 | - | - | - | - | - | - | - | - | - | - | - | - | - | - | - | 2012-02-08 | 55355 | |
Gi/o | αi1 | Human | - | 93 | - | - | - | - | X-ray | 4G5Q | - | 2.9 | - | - | - | - | - | - | - | G-protein-signaling modulator 2 | - | - | - | - | - | - | - | 2012-09-05 | 55355 | |
Gi/o | αi1 | Human | - | 100 | β1 | Rat | γ2 | Bovine | X-ray | 5TDH | - | 3.0 | - | - | - | - | - | - | - | - | - | - | - | - | - | Liu P, Jia MZ, Zhou XE, De Waal PW, Dickson BM, Liu B, Hou L, Yin YT, Kang YY, Shi Y, Melcher K, Xu HE, Jiang Y | 27498775 | 2016-11-09 | 55355 | |
Gi/o | αi1 | Human | - | 100 | β1 | Human | γ2 | Human | X-ray | 6CRK | - | 2.0 | - | - | - | - | - | - | single-chain Fv | - | - | - | - | - | - | Maeda S, Koehl A, Matile H, Hu H, Hilger D, Schertler GFX, Manglik A, Skiniotis G, Dawson RJP, Kobilka BK | 30213947 | 2018-10-24 | 55355 | |
Gi/o | αi1 | Human | - | 100 | - | - | - | - | Cryo-EM | 6VU8 | - | 4.1 | - | - | - | - | - | - | - | Resistance to inhibitors of cholinesterase 8 homolog A (C. elegans) | - | - | - | - | - | Seven AB, Hilger D, Papasergi-Scott MM, Zhang L, Qu Q, Kobilka BK, Tall GG, Skiniotis G | 32126208 | 2020-03-18 | 55355 | |
Gi/o | αi1 | Human | - | 100 | β1 | Human | γ2 | Human | Cryo-EM | 7RKX | - | 3.1 | - | - | - | - | - | - | Antibody fragment scFv16 | G-protein coupled receptor homolog US27 | - | - | - | - | - | - | - | 2022-01-26 | 55355 | |
Gi/o | αi1 | Human | - | 100 | β1 | Human | γ2 | Human | Cryo-EM | 7RKY | - | 3.8 | - | - | - | - | - | - | Antibody fragment scFv16 | G-protein coupled receptor homolog US27 | - | - | - | - | - | - | - | 2022-01-26 | 55355 | |
Gi/o | αi1 | Human | - | 100 | β1 | Human | γ2 | Human | Cryo-EM | 7YOO | - | 3.1 | - | - | - | - | - | - | single-chain antibody Fv fragment (scFv16) |
Neuropeptide Y Neuropeptide Y receptor type 2 |
- | - | - | - | - | Kang H, Park C, Choi YK, Bae J, Kwon S, Kim J, Choi C, Seok C, Im W, Choi HJ | 36525977 | 2023-03-22 | 55355 | |
Gi/o | αi1 | Human | - | 100 | β1 | Human | γ2 | Human | Cryo-EM | 8HNL | - | 3.0 | - | - | - | - | - | - | single-chain variable fragment scFv16 | - | - | - | - | - | - | Jiao H, Pang B, Liu A, Chen Q, Pan Q, Wang X, Xu Y, Chiang YC, Ren R, Hu H | 38177682 | 2023-11-29 | 55355 | |
Gi/o | αi1 | Human | - | 100 | β1 | Human | γ2 | Human | Cryo-EM | 8J6J | - | 2.8 | - | - | - | - | - | - | - |
Scfv16 Hydroxycarboxylic acid receptor 2 hydroxycarboxylic acid receptor 2 |
- | - | - | - | - | Zhu S, Yuan Q, Li X, He X, Shen S, Wang D, Li J, Cheng X, Duan X, Xu HE, Duan J | 37952153 | 2024-01-10 | 55355 | |
Gi/o | αi1 | Human | - | 100 | β1 | Human | γ2 | Human | Cryo-EM | 8JGB | - | 2.8 | - | - | - | - | - | - | scFv16 |
Conorfamide-Tx2 Mas-related G-protein coupled receptor member X1 |
- | - | - | - | - | Guo L, Zhang Y, Fang G, Tie L, Zhuang Y, Xue C, Liu Q, Zhang M, Zhu K, You C, Xu P, Yuan Q, Zhang C, Liu L, Rong N, Peng S, Liu Y, Wang C, Luo X, Lv Z, Kang D, Yu X, Zhang C, Jiang Y, Dong X, Zhou J, Liu Z, Yang F, Eric Xu H, Sun JP | 37591889 | 2024-01-10 | 55355 | |
Gi/o | αi1 | Human | - | 100 | β1 | Human | γ2 | Human | Cryo-EM | 8JGG | - | 3.0 | - | - | - | - | - | - | - |
BAM8-22 Single-Chain Fragment Variable 16 Mas-related G-protein coupled receptor member X1 |
- | - | - | - | - | Guo L, Zhang Y, Fang G, Tie L, Zhuang Y, Xue C, Liu Q, Zhang M, Zhu K, You C, Xu P, Yuan Q, Zhang C, Liu L, Rong N, Peng S, Liu Y, Wang C, Luo X, Lv Z, Kang D, Yu X, Zhang C, Jiang Y, Dong X, Zhou J, Liu Z, Yang F, Eric Xu H, Sun JP | 37591889 | 2024-01-10 | 55355 | |
Gi/o | αi3 | Rat | - | 99 | - | - | - | - | X-ray | 6MHE | - | 2.2 | - | - | - | - | - | - | - | KB752 peptide | - | - | - | - | - | Kalogriopoulos NA, Rees SD, Ngo T, Kopcho NJ, Ilatovskiy AV, Sun N, Komives EA, Chang G, Ghosh P, Kufareva I | 31363053 | 2019-07-31 | 55462 | |
Gi/o | αi3 | Rat | - | 99 | - | - | - | - | X-ray | 6MHF | - | 2.0 | - | - | - | - | - | - | - | Girdin | - | - | - | - | - | Kalogriopoulos NA, Rees SD, Ngo T, Kopcho NJ, Ilatovskiy AV, Sun N, Komives EA, Chang G, Ghosh P, Kufareva I | 31363053 | 2019-07-31 | 55462 | |
Gi/o | αi3 | Human | - | 91 | - | - | - | - | X-ray | 2IHB | - | 2.7 | - | - | - | - | - | - | - | Regulator of G-protein signalling 10 | - | - | - | - | - | Soundararajan M, Willard FS, Kimple AJ, Turnbull AP, Ball LJ, Schoch GA, Gileadi C, Fedorov OY, Dowler EF, Higman VA, Hutsell SQ, Sundstrom M, Doyle DA, Siderovski DP | 18434541 | 2006-11-21 | 55357 | |
Gi/o | αi3 | Human | - | 99 | - | - | - | - | X-ray | 2ODE | - | 1.9 | - | - | - | - | - | - | - | Regulator of G-protein signaling 8 | - | - | - | - | - | Soundararajan M, Willard FS, Kimple AJ, Turnbull AP, Ball LJ, Schoch GA, Gileadi C, Fedorov OY, Dowler EF, Higman VA, Hutsell SQ, Sundstrom M, Doyle DA, Siderovski DP | 18434541 | 2007-02-06 | 55357 | |
Gi/o | αi3 | Human | - | 99 | - | - | - | - | X-ray | 2V4Z | - | 2.8 | - | - | - | - | - | - | - | REGULATOR OF G-PROTEIN SIGNALING 2 | - | - | - | - | - | Kimple AJ, Soundararajan M, Hutsell SQ, Roos AK, Urban DJ, Setola V, Temple BR, Roth BL, Knapp S, Willard FS, Siderovski DP | 19478087 | 2008-11-04 | 55357 | |
Gi/o | αi3 | Human | - | 93 | - | - | - | - | X-ray | 4G5O | - | 2.9 | - | - | - | - | - | - | - | G-protein-signaling modulator 2 | - | - | - | - | - | - | - | 2012-09-05 | 55357 | |
Gi/o | αi3 | Human | - | 93 | - | - | - | - | X-ray | 4G5R | - | 3.5 | - | - | - | - | - | - | - | G-protein-signaling modulator 2 | - | - | - | - | - | - | - | 2012-09-05 | 55357 | |
Gi/o | αi3 | Human | - | 93 | - | - | - | - | X-ray | 4G5S | - | 3.6 | - | - | - | - | - | - | - | G-protein-signaling modulator 2 | - | - | - | - | - | - | - | 2012-09-05 | 55357 | |
Gi/o | αi3 | Human | - | 100 | - | - | - | - | Cryo-EM | 7X6I | - | 3.9 | - | - | - | - | - | - | - | Short transient receptor potential channel 5 | - | - | - | - | - | Won J, Kim J, Jeong H, Kim J, Feng S, Jeong B, Kwak M, Ko J, Im W, So I, Lee HH | 37137991 | 2023-04-26 | 55357 | |
Gi/o | αi3 | Human | - | 100 | - | - | - | - | Cryo-EM | 8GVX | - | 3.9 | - | - | - | - | - | - | - | Short transient receptor potential channel 5 | - | - | - | - | - | Won J, Kim J, Jeong H, Kim J, Feng S, Jeong B, Kwak M, Ko J, Im W, So I, Lee HH | 37137991 | 2023-05-24 | 55357 | |
Gi/o | αt1 | Bovine | - | 100 | β1 | Bovine | γT1 | Bovine | X-ray | 1GOT | - | 2.0 | - | - | - | - | - | - | - | - | - | - | - | - | - | Lambright DG, Sondek J, Bohm A, Skiba NP, Hamm HE, Sigler PB | 8552184 | 1997-03-12 | 55465 | |
Gi/o | αt1 | Bovine | - | 93 | - | - | - | - | X-ray | 1TAD | - | 1.7 | - | - | - | - | - | - | - | - | - | - | - | - | - | Sondek J, Lambright DG, Noel JP, Hamm HE, Sigler PB | 7969474 | 1995-05-08 | 55465 | |
Gi/o | αt1 | Bovine | - | 93 | - | - | - | - | X-ray | 1TAG | - | 1.8 | - | - | - | - | - | - | - | - | - | - | - | - | - | Lambright DG, Noel JP, Hamm HE, Sigler PB | 8208289 | 1995-02-07 | 55465 | |
Gi/o | αt1 | Bovine | - | 93 | - | - | - | - | X-ray | 1TND | - | 2.2 | - | - | - | - | - | - | - | - | - | - | - | - | - | Noel JP, Hamm HE, Sigler PB | 8259210 | 1994-07-31 | 55465 | |
Gi/o | αt1 | Bovine | - | 100 | - | - | - | - | Cryo-EM | 7JSN | - | 3.2 | - | - | - | - | - | - | - |
Rod cGMP-specific 3' 5'-cyclic phosphodiesterase subunit alpha Rod cGMP-specific 3' 5'-cyclic phosphodiesterase subunit beta |
- | - | - | - | - | Gao Y, Eskici G, Ramachandran S, Poitevin F, Seven AB, Panova O, Skiniotis G, Cerione RA | 33007200 | 2020-10-21 | 55465 | |
Gi/o | αt1 | Human | - | 3 | - | - | - | - | X-ray | 3RBQ | - | 2.0 | - | - | - | - | - | - | - | Protein unc-119 homolog A | - | - | - | - | - | Zhang H, Constantine R, Vorobiev S, Chen Y, Seetharaman J, Huang YJ, Xiao R, Montelione GT, Gerstner CD, Davis MW, Inana G, Whitby FG, Jorgensen EM, Hill CP, Tong L, Baehr W | 21642972 | 2011-06-08 | 55358 | |
Gi/o | αt2 | Human | - | 100 | - | - | - | - | X-ray | 6N84 | - | 1.8 | - | - | - | - | - | - | - | - | - | - | - | - | - | Srivastava D, Gakhar L, Artemyev NO | 31300652 | 2019-07-10 | 55359 | |
Gi/o | αt2 | Human | - | 100 | - | - | - | - | X-ray | 6N85 | - | 2.5 | - | - | - | - | - | - | - | Synembryn-A | - | - | - | - | - | Srivastava D, Gakhar L, Artemyev NO | 31300652 | 2019-07-10 | 55359 | |
Gi/o | αo | Mouse | - | 94 | - | - | - | - | X-ray | 3C7K | - | 2.9 | - | - | - | - | - | - | - | Regulator of G-protein signaling 16 | - | - | - | - | - | Slep KC, Kercher MA, Wieland T, Chen CK, Simon MI, Sigler PB | 18434540 | 2008-05-06 | 55540 | |
Gq/11 | αq | Mouse | - | 97 | - | - | - | - | X-ray | 4EKC | - | 7.4 | - | - | - | - | - | - | - | Regulator of G-protein signaling 2 | - | - | - | - | - | Nance MR, Kreutz B, Tesmer VM, Sterne-Marr R, Kozasa T, Tesmer JJ | 23434405 | 2013-01-30 | 55577 | |
Gq/11 | αq | Mouse | - | 97 | - | - | - | - | X-ray | 4EKD | - | 2.7 | - | - | - | - | - | - | - | Regulator of G-protein signaling 2 | - | - | - | - | - | Nance MR, Kreutz B, Tesmer VM, Sterne-Marr R, Kozasa T, Tesmer JJ | 23434405 | 2013-01-30 | 55577 | |
Gq/11 | αq | Mouse | - | 98 | - | - | - | - | X-ray | 4GNK | - | 4.0 | - | - | - | - | - | - | - |
1-phosphatidylinositol 4 5-bisphosphate phosphodiesterase beta-3 |
- | - | - | - | - | Lyon AM, Dutta S, Boguth CA, Skiniotis G, Tesmer JJ | 23377541 | 2013-02-06 | 55577 | |
Gq/11 | αq | Mouse | - | 100 | - | - | - | - | X-ray | 4QJ3 | - | 3.0 | - | - | - | - | - | - | - |
1-phosphatidylinositol 4 5-bisphosphate phosphodiesterase beta-3 |
- | - | - | - | - | Lyon AM, Begley JA, Manett TD, Tesmer JJG | 25435326 | 2014-10-22 | 55577 | |
Gq/11 | αq | Mouse | - | 100 | - | - | - | - | X-ray | 4QJ4 | - | 3.3 | - | - | - | - | - | - | - |
1-phosphatidylinositol 4 5-bisphosphate phosphodiesterase beta-3 |
- | - | - | - | - | Lyon AM, Begley JA, Manett TD, Tesmer JJG | 25435326 | 2014-10-22 | 55577 | |
Gq/11 | αq | Mouse | - | 100 | - | - | - | - | X-ray | 4QJ5 | - | 3.4 | - | - | - | - | - | - | - |
1-phosphatidylinositol 4 5-bisphosphate phosphodiesterase beta-3 |
- | - | - | - | - | Lyon AM, Begley JA, Manett TD, Tesmer JJG | 25435326 | 2014-10-22 | 55577 | |
Gq/11 | αq | Mouse | - | 87 | - | - | - | - | X-ray | 5DO9 | - | 2.6 | - | - | - | - | - | - | - | Regulator of G-protein signaling 8 | - | - | - | - | - | Taylor VG, Bommarito PA, Tesmer JJ | 26755720 | 2016-01-20 | 55577 | |
Gq/11 | αq | Mouse | - | 91 | - | - | - | - | X-ray | 7SQ2 | - | 2.6 | - | - | - | - | - | - | - |
1-phosphatidylinositol 4 5-bisphosphate phosphodiesterase beta-3 |
- | - | - | - | - | Waldo GL, Ricks TK, Hicks SN, Cheever ML, Kawano T, Tsuboi K, Wang X, Montell C, Kozasa T, Sondek J, Harden TK | 20966218 | 2021-11-17 | 55577 | |
Gq/11 | αq | Human | - | 100 | - | - | - | - | Cryo-EM | 6VU5 | - | 3.5 | - | - | - | - | - | - | - | Resistance to inhibitors of cholinesterase-8A (Ric-8A) | - | - | - | - | - | Seven AB, Hilger D, Papasergi-Scott MM, Zhang L, Qu Q, Kobilka BK, Tall GG, Skiniotis G | 32126208 | 2020-03-18 | 55363 | |
Gq/11 | αq | Human | - | 98 | - | - | - | - | Cryo-EM | 8JPE | - | 2.9 | - | - | - | - | - | - | - | - | - | - | - | - | - | Duan J, Liu H, Zhao F, Yuan Q, Ji Y, Cai X, He X, Li X, Li J, Wu K, Gao T, Zhu S, Lin S, Wang MW, Cheng X, Yin W, Jiang Y, Yang D, Xu HE | 37532940 | 2023-08-09 | 55363 | |
Gq/11 | αq | Human | - | 99 | - | - | - | - | Cryo-EM | 8UQN | - | 3.4 | - | - | - | - | - | - | - |
1-phosphatidylinositol 4 5-bisphosphate phosphodiesterase beta-3 |
- | - | - | - | - | Falzone ME, MacKinnon R | 37991948 | 2023-12-06 | 55363 | |
Gq/11 | αq | Human | - | 99 | β1 | Human | γ2 | Human | Cryo-EM | 8UQO | - | 3.4 | - | - | - | - | - | - | - |
1-phosphatidylinositol 4 5-bisphosphate phosphodiesterase beta-3 |
- | - | - | - | - | Falzone ME, MacKinnon R | 37991948 | 2023-12-06 | 55363 | |
G12/13 | α12 | Mouse | - | 95 | - | - | - | - | X-ray | 1ZCA | - | 2.9 | - | - | - | - | - | - | - | - | - | - | - | - | - | Kreutz B, Yau DM, Nance MR, Tanabe S, Tesmer JJ, Kozasa T | 16388592 | 2005-11-15 | 55641 | |
G12/13 | α13 | Mouse | - | 96 | - | - | - | - | X-ray | 1ZCB | - | 2.0 | - | - | - | - | - | - | - | - | - | - | - | - | - | Kreutz B, Yau DM, Nance MR, Tanabe S, Tesmer JJ, Kozasa T | 16388592 | 2005-11-15 | 55660 | |
G12/13 | α13 | Mouse | - | 96 | - | - | - | - | X-ray | 3AB3 | - | 2.4 | - | - | - | - | - | - | - | Rho guanine nucleotide exchange factor 1 | - | - | - | - | - | Hajicek N, Kukimoto-Niino M, Mishima-Tsumagari C, Chow CR, Shirouzu M, Terada T, Patel M, Yokoyama S, Kozasa T | 21507947 | 2010-12-29 | 55660 | |
G12/13 | α13 | Mouse | - | 90 | - | - | - | - | X-ray | 3CX6 | - | 2.5 | - | - | - | - | - | - | - | Rho guanine nucleotide exchange factor 11 | - | - | - | - | - | Chen Z, Singer WD, Danesh SM, Sternweis PC, Sprang SR | 18940608 | 2008-10-28 | 55660 | |
G12/13 | α13 | Mouse | - | 90 | - | - | - | - | X-ray | 3CX7 | - | 2.3 | - | - | - | - | - | - | - | Glutamate Transporter Associated Protein 48 | - | - | - | - | - | Chen Z, Singer WD, Danesh SM, Sternweis PC, Sprang SR | 18940608 | 2008-10-28 | 55660 | |
G12/13 | α13 | Mouse | - | 90 | - | - | - | - | X-ray | 3CX8 | - | 2.0 | - | - | - | - | - | - | - | Rho guanine nucleotide exchange factor 11 | - | - | - | - | - | Chen Z, Singer WD, Danesh SM, Sternweis PC, Sprang SR | 18940608 | 2008-10-28 | 55660 |
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G protein family | Subtype | PDB | UniProt | IUPHAR | Rec. family | Class | Species | PDB Date |
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