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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 | L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline | small-molecule | Rasmussen SG, DeVree BT, Zou Y, Kruse AC, Chung KY, Kobilka TS, Thian FS, Chae PS, Pardon E, Calinski D, Mathiesen JM, Shah ST, Lyons JA, Caffrey M, Gellman SH, Steyaert J, Skiniotis G, Weis WI, Sunahara RK, Kobilka BK | 10.1038/NATURE10361 | 2011-07-20 | 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 | calcitonin, adrenomedullin, amylin, α-CGRP, adrenomedullin 2/intermedin, β-CGRP | peptide | Liang YL, Khoshouei M, Radjainia M, Zhang Y, Glukhova A, Tarrasch J, Thal DM, Furness SGB, Christopoulos G, Coudrat T, Danev R, Baumeister W, Miller LJ, Christopoulos A, Kobilka BK, Wootten D, Skiniotis G, Sexton PM | 10.1038/NATURE22327 | 2017-05-03 | 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 | PHM, GHRH, VIP, PACAP-27, PHI, secretin, PACAP-38 | peptide | Duan J, Shen DD, Zhou XE, Bi P, Liu QF, Tan YX, Zhuang YW, Zhang HB, Xu PY, Huang SJ, Ma SS, He XH, Melcher K, Zhang Y, Xu HE, Jiang Y | 10.1038/S41467-020-17933-8 | 2020-09-02 | 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-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide | peptide | Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, Senel P, Stewart GD, Liang YL, Glukhova A, Venugopal H, Christopoulos A, Furness SGB, Miller LJ, Reedtz-Runge S, Langmead CJ, Gloriam DE, Danev R, Sexton PM, Wootten D | 10.1016/J.MOLCEL.2020.09.020 | 2020-09-09 | 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
|
small-molecule | Agonist | glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide | peptide | Kawai T, Sun B, Yoshino H, Feng D, Suzuki Y, Fukazawa M, Nagao S, Wainscott DB, Showalter AD, Droz BA, Kobilka TS, Coghlan MP, Willard FS, Kawabe Y, Kobilka BK, Sloop KW | 10.1073/PNAS.2014879117 | 2020-11-18 | 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-(3-33), glucagon-like peptide 2 | peptide | Sun W, Chen LN, Zhou Q, Zhao LH, Yang D, Zhang H, Cong Z, Shen DD, Zhao F, Zhou F, Cai X, Chen Y, Zhou Y, Gadgaard S, van der Velden WJC, Zhao S, Jiang Y, Rosenkilde MM, Xu HE, Zhang Y, Wang MW | 10.1038/S41422-020-00442-0 | 2020-12-16 | 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, (-)-noradrenaline, 5-hydroxytryptamine, dopamine | small-molecule | Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP, Shen DD, Xu T, Liu YF, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE | 10.1016/J.CELL.2021.01.027 | 2021-02-24 | 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, (-)-noradrenaline, 5-hydroxytryptamine, dopamine | small-molecule | Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z | 10.1016/J.CELL.2021.01.028 | 2021-03-03 | 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 |
small-molecule small-molecule |
Agonist PAM |
L-NOREPINEPHRINE, noradrenaline, (-)-noradrenaline, 5-hydroxytryptamine, dopamine | small-molecule | Zhuang Y, Krumm B, Zhang H, Zhou XE, Wang Y, Huang XP, Liu Y, Cheng X, Jiang Y, Jiang H, Zhang C, Yi W, Roth BL, Zhang Y, Xu HE | 10.1038/S41422-021-00482-0 | 2021-03-03 | 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 | oxytocin, vasopressin | peptide | Wang L, Xu J, Cao S, Sun D, Liu H, Lu Q, Liu Z, Du Y, Zhang C | 10.1038/S41422-021-00483-Z | 2021-05-26 | 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 | oxytocin, vasopressin | peptide | Bous J, Orcel H, Floquet N, Leyrat C, Lai-Kee-Him J, Gaibelet G, Ancelin A, Saint-Paul J, Trapani S, Louet M, Sounier R, Demene H, Granier S, Bron P, Mouillac B | 10.1126/SCIADV.ABG5628 | 2021-06-02 | 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-glutamic acid, L-serine-O-phosphate | small-molecule | Lin S, Han S, Cai X, Tan Q, Zhou K, Wang D, Wang X, Du J, Yi C, Chu X, Dai A, Zhou Y, Chen Y, Zhou Y, Liu H, Liu J, Yang D, Wang MW, Zhao Q, Wu B | 10.1038/S41586-021-03495-2 | 2021-06-23 | 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 | CCL11, CCL14, CCL2, CCL8, CCL5, CCL16, CCL4, CCL13, CCL7, CCL3 | 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 | oxytocin, vasopressin | peptide | Zhou F, Ye C, Ma X, Yin W, Croll TI, Zhou Q, He X, Zhang X, Yang D, Wang P, Xu HE, Wang MW, Jiang Y | 10.1038/S41422-021-00480-2 | 2021-07-21 | 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-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide | peptide | Cong Z, Chen LN, Ma H, Zhou Q, Zou X, Ye C, Dai A, Liu Q, Huang W, Sun X, Wang X, Xu P, Zhao L, Xia T, Zhong W, Yang D, Eric Xu H, Zhang Y, Wang MW | 10.1038/S41467-021-24058-Z | 2021-08-11 | 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-8, desulfated cholecystokinin-8, CCK-39, CCK-58, CCK-33, CCK-4, gastrin-17 | peptide | Liu Q, Yang D, Zhuang Y, Croll TI, Cai X, Dai A, He X, Duan J, Yin W, Ye C, Zhou F, Wu B, Zhao Q, Xu HE, Wang MW, Jiang Y | 10.1038/S41589-021-00841-3 | 2021-08-25 | 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-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide | peptide | Liang YL, Khoshouei M, Glukhova A, Furness SGB, Zhao P, Clydesdale L, Koole C, Truong TT, Thal DM, Lei S, Radjainia M, Danev R, Baumeister W, Wang MW, Miller LJ, Christopoulos A, Sexton PM, Wootten D | 10.1038/NATURE25773 | 2018-02-21 | 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 | calcitonin, adrenomedullin, amylin, α-CGRP, adrenomedullin 2/intermedin, β-CGRP | peptide | Dal Maso E, Glukhova A, Zhu Y, Garcia-Nafria J, Tate CG, Atanasio S, Reynolds CA, Ramirez-Aportela E, Carazo JM, Hick CA, Furness SGB, Hay DL, Liang YL, Miller LJ, Christopoulos A, Wang MW, Wootten D, Sexton PM | 10.1021/ACSPTSCI.8B00056 | 2019-01-23 | 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 | PTHrP-(1-36), PTHrP, PTH, TIP39 | peptide | Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y | 10.1126/SCIENCE.AAV7942 | 2019-04-17 | 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 | PTHrP-(1-36), PTHrP, PTH, TIP39 | peptide | Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y | 10.1126/SCIENCE.AAV7942 | 2019-04-17 | 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 | L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline | small-molecule | Liu X, Xu X, Hilger D, Aschauer P, Tiemann JKS, Du Y, Liu H, Hirata K, Sun X, Guixa-Gonzalez R, Mathiesen JM, Hildebrand PW, Kobilka BK | 10.1016/J.CELL.2019.04.021 | 2019-06-05 | 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 | large neuromedin N, neuromedin N, neurotensin, large neurotensin | peptide | Kato HE, Zhang Y, Hu H, Suomivuori CM, Kadji FMN, Aoki J, Krishna Kumar K, Fonseca R, Hilger D, Huang W, Latorraca NR, Inoue A, Dror RO, Kobilka BK, Skiniotis G | 10.1038/S41586-019-1337-6 | 2019-07-10 | 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 1, urocortin 2 | peptide | Liang YL, Belousoff MJ, Zhao P, Koole C, Fletcher MM, Truong TT, Julita V, Christopoulos G, Xu HE, Zhang Y, Khoshouei M, Christopoulos A, Danev R, Sexton PM, Wootten D | 10.1016/J.MOLCEL.2020.01.012 | 2020-02-05 | 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 | PHM, PHV, VIP, PACAP-27, PHI, PACAP-38 | peptide | Liang YL, Belousoff MJ, Zhao P, Koole C, Fletcher MM, Truong TT, Julita V, Christopoulos G, Xu HE, Zhang Y, Khoshouei M, Christopoulos A, Danev R, Sexton PM, Wootten D | 10.1016/J.MOLCEL.2020.01.012 | 2020-02-05 | 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 1, urocortin 3, urocortin 2 | peptide | Ma S, Shen Q, Zhao LH, Mao C, Zhou XE, Shen DD, de Waal PW, Bi P, Li C, Jiang Y, Wang MW, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE | 10.1016/J.MOLCEL.2020.01.013 | 2020-02-12 | 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 | LXA4, serum amyloid A, PrP106-126, aspirin-triggered resolvin D1, humanin, aspirin triggered lipoxin A4, LL-37, annexin I, resolvin D1 | peptide | Zhuang Y, Liu H, Edward Zhou X, Kumar Verma R, de Waal PW, Jang W, Xu TH, Wang L, Meng X, Zhao G, Kang Y, Melcher K, Fan H, Lambert NA, Eric Xu H, Zhang C | 10.1038/S41467-020-14728-9 | 2020-02-26 | 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 | 5-hydroxytryptamine, 5-HT-moduline, tryptamine | small-molecule | Garcia-Nafria J, Nehme R, Edwards PC, Tate CG | 10.1038/S41586-018-0241-9 | 2018-06-20 | 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
|
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-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide | peptide | Ma H, Huang W, Wang X, Zhao L, Jiang Y, Liu F, Guo W, Sun X, Zhong W, Yuan D, Xu HE | 10.1038/S41422-020-0384-8 | 2020-08-26 | 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, deoxycholic acid, chenodeoxycholic acid, lithocholic acid | small-molecule | Chen G, Wang X, Ge Y, Ma L, Chen Q, Liu H, Du Y, Ye RD, Hu H, Ren R | 10.1038/S41392-020-00262-Z | 2020-09-02 | 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-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide | peptide | Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, Senel P, Stewart GD, Liang YL, Glukhova A, Venugopal H, Christopoulos A, Furness SGB, Miller LJ, Reedtz-Runge S, Langmead CJ, Gloriam DE, Danev R, Sexton PM, Wootten D | 10.1016/J.MOLCEL.2020.09.020 | 2020-09-09 | 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, deoxycholic acid, chenodeoxycholic acid, lithocholic acid | small-molecule | Yang F, Mao C, Guo L, Lin J, Ming Q, Xiao P, Wu X, Shen Q, Guo S, Shen DD, Lu R, Zhang L, Huang S, Ping Y, Zhang C, Ma C, Zhang K, Liang X, Shen Y, Nan F, Yi F, Luca VC, Zhou J, Jiang C, Sun JP, Xie X, Yu X, Zhang Y | 10.1038/S41586-020-2569-1 | 2020-09-09 | 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
|
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 | PGF2α, PGI2, PGD2, thromboxane A2, PGE1, PGE2 | small-molecule | Nojima S, Fujita Y, Kimura KT, Nomura N, Suno R, Morimoto K, Yamamoto M, Noda T, Iwata S, Shigematsu H, Kobayashi T | 10.1016/J.STR.2020.11.007 | 2020-11-18 | 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 | L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline | small-molecule | Yang F, Ling S, Zhou Y, Zhang Y, Lv P, Liu S, Fang W, Sun W, Hu LA, Zhang L, Shi P, Tian C | 10.1093/NSR/NWAA284 | 2020-12-16 | 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, (-)-noradrenaline, 5-hydroxytryptamine, dopamine | small-molecule | Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP, Shen DD, Xu T, Liu YF, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE | 10.1016/J.CELL.2021.01.027 | 2021-02-24 | 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, (-)-noradrenaline, 5-hydroxytryptamine, dopamine | small-molecule | Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z | 10.1016/J.CELL.2021.01.028 | 2021-03-03 | 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, (-)-noradrenaline, 5-hydroxytryptamine, dopamine | small-molecule | Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z | 10.1016/J.CELL.2021.01.028 | 2021-03-03 | 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 | 5-hydroxytryptamine, tryptamine | small-molecule | Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen DD, Yen HY, Robinson CV, Harpsoe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE | 10.1038/S41586-021-03376-8 | 2021-04-14 | 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 | PGF2α, PGI2, PGD2, thromboxane A2, PGE1, PGE2 | small-molecule | Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y | 10.1126/SCIADV.ABF1268 | 2021-05-05 | 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 | PGF2α, PGI2, PGD2, thromboxane A2, PGE1, PGE2 | small-molecule | Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y | 10.1126/SCIADV.ABF1268 | 2021-05-05 | 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-8, desulfated cholecystokinin-8, CCK-39, CCK-58, CCK-33, CCK-4, gastrin-17 | peptide | Mobbs JI, Belousoff MJ, Harikumar KG, Piper SJ, Xu X, Furness SGB, Venugopal H, Christopoulos A, Danev R, Wootten D, Thal DM, Miller LJ, Sexton PM | 10.1371/JOURNAL.PBIO.3001295 | 2021-05-26 | 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 | CCL11, CCL14, CCL2, CCL8, CCL5, CCL16, CCL4, CCL13, CCL7, CCL3 | peptide | Isaikina P, Tsai CJ, Dietz N, Pamula F, Grahl A, Goldie KN, Guixa-Gonzalez R, Branco C, Paolini-Bertrand M, Calo N, Cerini F, Schertler GFX, Hartley O, Stahlberg H, Maier T, Deupi X, Grzesiek S | 10.1126/SCIADV.ABG8685 | 2021-06-30 | 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 | CCL11, CCL14, CCL2, CCL8, CCL5, CCL16, CCL4, CCL13, CCL7, CCL3 | 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-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide | peptide | Zhang X, Belousoff MJ, Liang YL, Danev R, Sexton PM, Wootten D | 10.1016/J.CELREP.2021.109374 | 2021-08-04 | 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-8, desulfated cholecystokinin-8, CCK-39, CCK-58, CCK-33, CCK-4, gastrin-17 | peptide | Liu Q, Yang D, Zhuang Y, Croll TI, Cai X, Dai A, He X, Duan J, Yin W, Ye C, Zhou F, Wu B, Zhao Q, Xu HE, Wang MW, Jiang Y | 10.1038/S41589-021-00841-3 | 2021-08-25 | 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 | PTHrP-(1-36), PTHrP, PTH, TIP39 | peptide | Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y | 10.1126/SCIENCE.AAV7942 | 2019-04-17 | 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 | large neuromedin N, neuromedin N, neurotensin, large neurotensin | peptide | Kato HE, Zhang Y, Hu H, Suomivuori CM, Kadji FMN, Aoki J, Krishna Kumar K, Fonseca R, Hilger D, Huang W, Latorraca NR, Inoue A, Dror RO, Kobilka BK, Skiniotis G | 10.1038/S41586-019-1337-6 | 2019-07-10 | 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 | L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline | small-molecule | Nguyen AH, Thomsen ARB, Cahill TJ 3rd, Huang R, Huang LY, Marcink T, Clarke OB, Heissel S, Masoudi A, Ben-Hail D, Samaan F, Dandey VP, Tan YZ, Hong C, Mahoney JP, Triest S, Little J 4th, Chen X, Sunahara R, Steyaert J, Molina H, Yu Z, des Georges A, Lefkowitz RJ | 10.1038/S41594-019-0330-Y | 2019-11-20 | 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-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide | peptide | Zhao P, Liang YL, Belousoff MJ, Deganutti G, Fletcher MM, Willard FS, Bell MG, Christe ME, Sloop KW, Inoue A, Truong TT, Clydesdale L, Furness SGB, Christopoulos A, Wang MW, Miller LJ, Reynolds CA, Danev R, Sexton PM, Wootten D | 10.1038/s41586-019-1902-z | 2020-01-08 | 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 1, urocortin 2 | peptide | Ma S, Shen Q, Zhao LH, Mao C, Zhou XE, Shen DD, de Waal PW, Bi P, Li C, Jiang Y, Wang MW, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE | 10.1016/J.MOLCEL.2020.01.013 | 2020-02-12 | 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 | PHM, PHV, VIP, PACAP-27, PHI, PACAP-38 | peptide | Wang J, Song X, Zhang D, Chen X, Li X, Sun Y, Li C, Song Y, Ding Y, Ren R, Harrington EH, Hu LA, Zhong W, Xu C, Huang X, Wang HW, Ma Y | 10.1038/S41422-020-0280-2 | 2020-03-11 | 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-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide | peptide | Bueno AB, Sun B, Willard FS, Feng D, Ho JD, Wainscott DB, Showalter AD, Vieth M, Chen Q, Stutsman C, Chau B, Ficorilli J, Agejas FJ, Cumming GR, Jimenez A, Rojo I, Kobilka TS, Kobilka BK, Sloop KW | 10.1038/S41589-020-0589-7 | 2020-07-22 | 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 | CXCL3, CXCL8, CXCL7, CXCL2, CXCL1, CXCL6, CXCL5 | peptide | Liu K, Wu L, Yuan S, Wu M, Xu Y, Sun Q, Li S, Zhao S, Hua T, Liu ZJ | 10.1038/S41586-020-2492-5 | 2020-09-02 | 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, deoxycholic acid, chenodeoxycholic acid, lithocholic acid | small-molecule | Yang F, Mao C, Guo L, Lin J, Ming Q, Xiao P, Wu X, Shen Q, Guo S, Shen DD, Lu R, Zhang L, Huang S, Ping Y, Zhang C, Ma C, Zhang K, Liang X, Shen Y, Nan F, Yi F, Luca VC, Zhou J, Jiang C, Sun JP, Xie X, Yu X, Zhang Y | 10.1038/S41586-020-2569-1 | 2020-09-09 | 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
|
small-molecule | Agonist | glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide | peptide | Zhang X, Johnson RM, Drulyte I, Yu L, Kotecha A, Danev R, Wootten D, Sexton PM, Belousoff MJ | 10.1016/J.STR.2021.04.008 | 2021-01-20 | 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-B, orexin-A | peptide | Hong C, Byrne NJ, Zamlynny B, Tummala S, Xiao L, Shipman JM, Partridge AT, Minnick C, Breslin MJ, Rudd MT, Stachel SJ, Rada VL, Kern JC, Armacost KA, Hollingsworth SA, O'Brien JA, Hall DL, McDonald TP, Strickland C, Brooun A, Soisson SM, Hollenstein K | 10.1038/S41467-021-21087-6 | 2021-02-10 | 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, (-)-noradrenaline, 5-hydroxytryptamine, dopamine | small-molecule | Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z | 10.1016/J.CELL.2021.01.028 | 2021-03-03 | 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 |
small-molecule small-molecule |
Agonist PAM |
L-NOREPINEPHRINE, noradrenaline, (-)-noradrenaline, 5-hydroxytryptamine, dopamine | small-molecule | Zhuang Y, Krumm B, Zhang H, Zhou XE, Wang Y, Huang XP, Liu Y, Cheng X, Jiang Y, Jiang H, Zhang C, Yi W, Roth BL, Zhang Y, Xu HE | 10.1038/S41422-021-00482-0 | 2021-03-03 | 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, (-)-noradrenaline, 5-hydroxytryptamine, dopamine | small-molecule | Sun B, Feng D, Chu ML, Fish I, Lovera S, Sands ZA, Kelm S, Valade A, Wood M, Ceska T, Kobilka TS, Lebon F, Kobilka BK | 10.1038/S41467-021-23519-9 | 2021-04-14 | 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 | PGF2α, PGI2, PGD2, thromboxane A2, PGE1, PGE2 | small-molecule | Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y | 10.1126/SCIADV.ABF1268 | 2021-05-05 | 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-8, desulfated cholecystokinin-8, CCK-39, CCK-58, CCK-33, CCK-4, gastrin-17 | peptide | Mobbs JI, Belousoff MJ, Harikumar KG, Piper SJ, Xu X, Furness SGB, Venugopal H, Christopoulos A, Danev R, Wootten D, Thal DM, Miller LJ, Sexton PM | 10.1371/JOURNAL.PBIO.3001295 | 2021-05-26 | 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 | oxytocin, vasopressin | peptide | Bous J, Orcel H, Floquet N, Leyrat C, Lai-Kee-Him J, Gaibelet G, Ancelin A, Saint-Paul J, Trapani S, Louet M, Sounier R, Demene H, Granier S, Bron P, Mouillac B | 10.1126/SCIADV.ABG5628 | 2021-06-02 | 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 |
small-molecule small-molecule |
Ago-PAM Agonist |
glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide | peptide | Cong Z, Chen LN, Ma H, Zhou Q, Zou X, Ye C, Dai A, Liu Q, Huang W, Sun X, Wang X, Xu P, Zhao L, Xia T, Zhong W, Yang D, Eric Xu H, Zhang Y, Wang MW | 10.1038/S41467-021-24058-Z | 2021-07-07 | 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) | CCL11, CCL14, CCL2, CCL8, CCL5, CCL16, CCL4, CCL13, CCL7, CCL3 | peptide | Zhang H, Chen K, Tan Q, Shao Q, Han S, Zhang C, Yi C, Chu X, Zhu Y, Xu Y, Zhao Q, Wu B | 10.1038/S41467-021-24438-5 | 2021-07-14 | 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-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide | peptide | Zhang X, Belousoff MJ, Liang YL, Danev R, Sexton PM, Wootten D | 10.1016/J.CELREP.2021.109374 | 2021-08-04 | 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 | PTHrP-(1-34) (human), PTH, PTHrP, PTHrP-(1-36), TIP39 | peptide | Wang X, Cheng X, Zhao L, Wang Y, Ye C, Zou X, Dai A, Cong Z, Chen J, Zhou Q, Xia T, Jiang H, Xu HE, Yang D, Wang MW | 10.1073/PNAS.2101279118 | 2021-08-18 | 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, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine | small-molecule | Zhao C, Cheng L, Wang W, Wang H, Luo Y, Feng Y, Wang X, Fu H, Cai Y, Yang S, Fu P, Yan W, Shao Z | 10.1038/S41422-021-00567-W | 2021-09-29 | 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 | LH, hCG | peptide | Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE | 10.1038/S41586-021-03924-2 | 2021-09-29 | 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, kallidin, Lys-[Hyp3]-bradykinin, [des-Arg10]kallidin, T-kinin, [Hyp3]bradykinin, bradykinin | peptide | Yin YL, Ye C, Zhou F, Wang J, Yang D, Yin W, Wang MW, Xu HE, Jiang Y | 10.1038/S41594-021-00645-Y | 2021-10-13 | 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, kallidin, Lys-[Hyp3]-bradykinin, [des-Arg10]kallidin, T-kinin, [Hyp3]bradykinin, bradykinin | peptide | Yin YL, Ye C, Zhou F, Wang J, Yang D, Yin W, Wang MW, Xu HE, Jiang Y | 10.1038/S41594-021-00645-Y | 2021-10-13 | 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-8, desulfated cholecystokinin-8, gastrin-14, CCK-58, desulfated gastrin-17, CCK-39, CCK-33, desulfated gastrin-34, gastrin-34, gastrin-71, desulfated gastrin-71, CCK-4, desulfated gastrin-14, gastrin-17 | peptide | Zhang X, He C, Wang M, Zhou Q, Yang D, Zhu Y, Feng W, Zhang H, Dai A, Chu X, Wang J, Yang Z, Jiang Y, Sensfuss U, Tan Q, Han S, Reedtz-Runge S, Xu HE, Zhao S, Wang MW, Wu B, Zhao Q | 10.1038/S41589-021-00866-8 | 2021-10-13 | 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 | γ-MSH, agouti-related protein, β-MSH, α-MSH, ACTH | peptide | Zhang H, Chen LN, Yang D, Mao C, Shen Q, Feng W, Shen DD, Dai A, Xie S, Zhou Y, Qin J, Sun JP, Scharf DH, Hou T, Zhou T, Wang MW, Zhang Y | 10.1038/S41422-021-00552-3 | 2021-11-03 | 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 | γ-MSH, agouti-related protein, β-MSH, α-MSH, ACTH | peptide | Zhang H, Chen LN, Yang D, Mao C, Shen Q, Feng W, Shen DD, Dai A, Xie S, Zhou Y, Qin J, Sun JP, Scharf DH, Hou T, Zhou T, Wang MW, Zhang Y | 10.1038/S41422-021-00552-3 | 2021-11-03 | 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 | γ-MSH, agouti-related protein, β-MSH, α-MSH, ACTH | peptide | Heyder NA, Kleinau G, Speck D, Schmidt A, Paisdzior S, Szczepek M, Bauer B, Koch A, Gallandi M, Kwiatkowski D, Burger J, Mielke T, Beck-Sickinger AG, Hildebrand PW, Spahn CMT, Hilger D, Schacherl M, Biebermann H, Hilal T, Kuhnen P, Kobilka BK, Scheerer P | 10.1038/S41422-021-00569-8 | 2021-11-17 | 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 | neuropeptide-γ, hemokinin 1, neurokinin A, neuropeptide K, neurokinin B, substance P | peptide | Thom C, Ehrenmann J, Vacca S, Waltenspuhl Y, Schoppe J, Medalia O, Pluckthun A | 10.1126/SCIADV.ABK2872 | 2021-12-15 | 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-phenylalanine, L-tryptophan | small-molecule | Zhou Y, Daver H, Trapkov B, Wu L, Wu M, Harpsoe K, Gentry PR, Liu K, Larionova M, Liu J, Chen N, Brauner-Osborne H, Gloriam DE, Hua T, Liu ZJ | 10.1038/S41422-021-00591-W | 2021-12-29 | 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, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine | small-molecule | Xu Z, Ikuta T, Kawakami K, Kise R, Qian Y, Xia R, Sun MX, Zhang A, Guo C, Cai XH, Huang Z, Inoue A, He Y | 10.1038/S41589-021-00930-3 | 2022-01-05 | 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, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine | small-molecule | Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z | 10.1038/S41422-021-00566-X | 2021-09-29 | 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 | γ-MSH, β-MSH, α-MSH, ACTH | peptide | Ma S, Chen Y, Dai A, Yin W, Guo J, Yang D, Zhou F, Jiang Y, Wang MW, Xu HE | 10.1038/S41422-021-00557-Y | 2021-09-08 | 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 | LXA4, serum amyloid A, PrP106-126, aspirin-triggered resolvin D1, humanin, aspirin triggered lipoxin A4, LL-37, annexin I, resolvin D1 | peptide | Zhuang Y, Wang L, Guo J, Sun D, Wang Y, Liu W, Xu HE, Zhang C | 10.1038/S41467-022-28586-0 | 2022-03-30 | 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 | cortistatin-14, SRIF-14, CST-17, SRIF-28 | peptide | Robertson MJ, Meyerowitz JG, Panova O, Borrelli K, Skiniotis G | 10.1038/S41594-022-00727-5 | 2022-03-09 | 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 | CCL14, CCL15, CCL8, CCL5, CCL16, CCL4, CCL23, CCL13, CCL7, CCL3 | peptide | Shao Z, Shen Q, Yao B, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Ma H, Chen ZH, Xu HE, Ying S, Zhang Y, Shen H | 10.1038/S41589-021-00918-Z | 2022-03-23 | 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 | calcitonin, adrenomedullin, amylin, α-CGRP, adrenomedullin 2/intermedin, β-CGRP | peptide | Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM | 10.1126/SCIENCE.ABM9609 | 2022-03-23 | 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
|
peptide | Agonist | calcitonin, adrenomedullin, amylin, α-CGRP, adrenomedullin 2/intermedin, β-CGRP | peptide | Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM | 10.1126/SCIENCE.ABM9609 | 2022-03-23 | 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 | calcitonin, adrenomedullin, amylin, α-CGRP, adrenomedullin 2/intermedin, β-CGRP | peptide | Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM | 10.1126/SCIENCE.ABM9609 | 2022-03-23 | 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 | PHM, PHV, VIP, PACAP-27, PHI, PACAP-38 | peptide | Kobayashi K, Shihoya W, Nishizawa T, Kadji FMN, Aoki J, Inoue A, Nureki O | 10.1038/S41594-020-0386-8 | 2020-03-11 | 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 | PHM, PHV, VIP, PACAP-27, PHI, PACAP-38 | peptide | Wang J, Song X, Zhang D, Chen X, Li X, Sun Y, Li C, Song Y, Ding Y, Ren R, Harrington EH, Hu LA, Zhong W, Xu C, Huang X, Wang HW, Ma Y | 10.1038/S41422-020-0280-2 | 2020-03-11 | 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 | CCL20, beta-defensin 4A | peptide | Wasilko DJ, Johnson ZL, Ammirati M, Che Y, Griffor MC, Han S, Wu H | 10.1038/S41467-020-16820-6 | 2020-06-24 | 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
|
small-molecule | Agonist | L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline | small-molecule | Zhang Y, Yang F, Ling S, Lv P, Zhou Y, Fang W, Sun W, Zhang L, Shi P, Tian C | 10.1038/S41421-020-0176-9 | 2020-08-05 | 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
|
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 | CXCL3, CXCL8, CXCL7, CXCL2, CXCL1, CXCL6, CXCL5 | peptide | Liu K, Wu L, Yuan S, Wu M, Xu Y, Sun Q, Li S, Zhao S, Hua T, Liu ZJ | 10.1038/S41586-020-2492-5 | 2020-09-02 | 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
|
small-molecule | Agonist | glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide | peptide | Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, Senel P, Stewart GD, Liang YL, Glukhova A, Venugopal H, Christopoulos A, Furness SGB, Miller LJ, Reedtz-Runge S, Langmead CJ, Gloriam DE, Danev R, Sexton PM, Wootten D | 10.1016/J.MOLCEL.2020.09.020 | 2020-09-09 | 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 | 5-hydroxytryptamine, tryptamine | small-molecule | Kim K, Che T, Panova O, DiBerto JF, Lyu J, Krumm BE, Wacker D, Robertson MJ, Seven AB, Nichols DE, Shoichet BK, Skiniotis G, Roth BL | 10.1016/J.CELL.2020.08.024 | 2020-09-23 | 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 | L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline | small-molecule | Yang F, Ling S, Zhou Y, Zhang Y, Lv P, Liu S, Fang W, Sun W, Hu LA, Zhang L, Shi P, Tian C | 10.1093/NSR/NWAA284 | 2020-12-16 | 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-B, orexin-A | peptide | Hong C, Byrne NJ, Zamlynny B, Tummala S, Xiao L, Shipman JM, Partridge AT, Minnick C, Breslin MJ, Rudd MT, Stachel SJ, Rada VL, Kern JC, Armacost KA, Hollingsworth SA, O'Brien JA, Hall DL, McDonald TP, Strickland C, Brooun A, Soisson SM, Hollenstein K | 10.1038/S41467-021-21087-6 | 2021-02-10 | 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, (-)-noradrenaline, 5-hydroxytryptamine, dopamine | small-molecule | Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP, Shen DD, Xu T, Liu YF, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE | 10.1016/J.CELL.2021.01.027 | 2021-02-24 | 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 |
small-molecule small-molecule |
Agonist PAM |
L-NOREPINEPHRINE, noradrenaline, (-)-noradrenaline, 5-hydroxytryptamine, dopamine | small-molecule | Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z | 10.1016/J.CELL.2021.01.028 | 2021-03-03 | 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 | γ-MSH, agouti-related protein, β-MSH, α-MSH, ACTH | peptide | Israeli H, Degtjarik O, Fierro F, Chunilal V, Gill AK, Roth NJ, Botta J, Prabahar V, Peleg Y, Chan LF, Ben-Zvi D, McCormick PJ, Niv MY, Shalev-Benami M | 10.1126/SCIENCE.ABF7958 | 2021-04-28 | 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-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide | peptide | Cong Z, Chen LN, Ma H, Zhou Q, Zou X, Ye C, Dai A, Liu Q, Huang W, Sun X, Wang X, Xu P, Zhao L, Xia T, Zhong W, Yang D, Eric Xu H, Zhang Y, Wang MW | 10.1038/S41467-021-24058-Z | 2021-07-14 | 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-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide | peptide | Cong Z, Chen LN, Ma H, Zhou Q, Zou X, Ye C, Dai A, Liu Q, Huang W, Sun X, Wang X, Xu P, Zhao L, Xia T, Zhong W, Yang D, Eric Xu H, Zhang Y, Wang MW | 10.1038/S41467-021-24058-Z | 2021-08-11 | 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-8, desulfated cholecystokinin-8, CCK-39, CCK-58, CCK-33, CCK-4, gastrin-17 | peptide | Liu Q, Yang D, Zhuang Y, Croll TI, Cai X, Dai A, He X, Duan J, Yin W, Ye C, Zhou F, Wu B, Zhao Q, Xu HE, Wang MW, Jiang Y | 10.1038/S41589-021-00841-3 | 2021-08-25 | 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, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine | small-molecule | Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z | 10.1038/S41422-021-00566-X | 2021-09-29 | 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 | LH, hCG | peptide | Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE | 10.1038/S41586-021-03924-2 | 2021-09-29 | 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 | neuropeptide-γ, hemokinin 1, neurokinin A, neuropeptide K, neurokinin B, substance P | peptide | Harris JA, Faust B, Gondin AB, Damgen MA, Suomivuori CM, Veldhuis NA, Cheng Y, Dror RO, Thal DM, Manglik A | 10.1038/S41589-021-00890-8 | 2021-11-03 | 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-phenylalanine, L-tryptophan | small-molecule | Zhou Y, Daver H, Trapkov B, Wu L, Wu M, Harpsoe K, Gentry PR, Liu K, Larionova M, Liu J, Chen N, Brauner-Osborne H, Gloriam DE, Hua T, Liu ZJ | 10.1038/S41422-021-00591-W | 2021-12-29 | 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-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide | peptide | Cary BP, Deganutti G, Zhao P, Truong TT, Piper SJ, Liu X, Belousoff MJ, Danev R, Sexton PM, Wootten D, Gellman SH | 10.1038/S41589-021-00945-W | 2022-01-05 | 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-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide | peptide | Deganutti G, Liang YL, Zhang X, Khoshouei M, Clydesdale L, Belousoff MJ, Venugopal H, Truong TT, Glukhova A, Keller AN, Gregory KJ, Leach K, Christopoulos A, Danev R, Reynolds CA, Zhao P, Sexton PM, Wootten D | 10.1038/S41467-021-27760-0 | 2022-01-12 | 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, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine | small-molecule | Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z | 10.1038/S41422-021-00566-X | 2021-09-29 | 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 | γ-MSH, β-MSH, α-MSH, ACTH | peptide | Ma S, Chen Y, Dai A, Yin W, Guo J, Yang D, Zhou F, Jiang Y, Wang MW, Xu HE | 10.1038/S41422-021-00557-Y | 2021-09-08 | 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 | LXA4, serum amyloid A, PrP106-126, aspirin-triggered resolvin D1, humanin, aspirin triggered lipoxin A4, LL-37, annexin I, resolvin D1 | peptide | Zhuang Y, Wang L, Guo J, Sun D, Wang Y, Liu W, Xu HE, Zhang C | 10.1038/S41467-022-28586-0 | 2022-03-30 | 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 | oxytocin, vasopressin | peptide | Meyerowitz JG, Robertson MJ, Barros-Alvarez X, Panova O, Nwokonko RM, Gao Y, Skiniotis G | 10.1038/S41594-022-00728-4 | 2022-03-09 | 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 | CCL14, CCL15, CCL8, CCL5, CCL16, CCL4, CCL23, CCL13, CCL7, CCL3 | peptide | Shao Z, Shen Q, Yao B, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Ma H, Chen ZH, Xu HE, Ying S, Zhang Y, Shen H | 10.1038/S41589-021-00918-Z | 2022-03-23 | 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, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine | small-molecule | Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY | 10.1038/S41467-022-28417-2 | 2022-02-09 | 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 | calcitonin, adrenomedullin, amylin, α-CGRP, adrenomedullin 2/intermedin, β-CGRP | peptide | Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM | 10.1126/SCIENCE.ABM9609 | 2022-03-23 | 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 | calcitonin, adrenomedullin, amylin, α-CGRP, adrenomedullin 2/intermedin, β-CGRP | peptide | Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM | 10.1126/SCIENCE.ABM9609 | 2022-03-30 | 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-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide | peptide | Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW | 10.1038/S41467-022-28683-0 | 2022-03-02 | 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 | LXA4, serum amyloid A, PrP106-126, aspirin-triggered resolvin D1, humanin, aspirin triggered lipoxin A4, LL-37, annexin I, resolvin D1 | peptide | Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B | 10.1038/S41467-022-29361-X | 2022-04-13 | 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 U-25, neuromedin S-36, neuromedin S-33, neuromedin U-23 | peptide | You C, Zhang Y, Xu P, Huang S, Yin W, Eric Xu H, Jiang Y | 10.1038/S41467-022-29683-W | 2022-04-20 | 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-B, orexin-A | peptide | Yin J, Kang Y, McGrath AP, Chapman K, Sjodt M, Kimura E, Okabe A, Koike T, Miyanohana Y, Shimizu Y, Rallabandi R, Lian P, Bai X, Flinspach M, De Brabander JK, Rosenbaum DM | 10.1038/S41467-022-30601-3 | 2022-05-25 | 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 | peptide YY, pancreatic polypeptide, neuropeptide Y | peptide | Tang T, Tan Q, Han S, Diemar A, Lobner K, Wang H, Schuss C, Behr V, Morl K, Wang M, Chu X, Yi C, Keller M, Kofoed J, Reedtz-Runge S, Kaiser A, Beck-Sickinger AG, Zhao Q, Wu B | 10.1126/SCIADV.ABM1232 | 2022-05-18 | 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 | cortistatin-14, SRIF-14, CST-17, SRIF-28 | peptide | Chen LN, Wang WW, Dong YJ, Shen DD, Guo J, Yu X, Qin J, Ji SY, Zhang H, Shen Q, He Q, Yang B, Zhang Y, Li Q, Mao C | 10.1038/S41422-022-00669-Z | 2022-06-01 | 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, (-)-noradrenaline, 5-hydroxytryptamine, dopamine | small-molecule | Teng X, Chen S, Wang Q, Chen Z, Wang X, Huang N, Zheng S | 10.1126/SCIADV.ABO4158 | 2022-06-15 | 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, (-)-noradrenaline, 5-hydroxytryptamine, dopamine | small-molecule | Teng X, Chen S, Wang Q, Chen Z, Wang X, Huang N, Zheng S | 10.1126/SCIADV.ABO4158 | 2022-06-15 | 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 |
small-molecule small-molecule |
Agonist PAM |
L-NOREPINEPHRINE, noradrenaline, (-)-noradrenaline, 5-hydroxytryptamine, dopamine | small-molecule | Teng X, Chen S, Nie Y, Xiao P, Yu X, Shao Z, Zheng S | 10.1038/S41467-022-30929-W | 2022-06-15 | 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-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide | peptide | Cong Z, Zhou Q, Li Y, Chen LN, Zhang ZC, Liang A, Liu Q, Wu X, Dai A, Xia T, Wu W, Zhang Y, Yang D, Wang MW | 10.1073/PNAS.2200155119 | 2022-06-29 | 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 | apelin-36, apelin-17, apelin-13, Elabela/Toddler-21, Elabela/Toddler-32, Elabela/Toddler-11, [Pyr1]apelin-13, apelin receptor early endogenous ligand | peptide | Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F | 10.1038/S41594-022-00797-5 | 2022-07-27 | 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 | apelin-36, apelin-17, apelin-13, Elabela/Toddler-21, Elabela/Toddler-32, Elabela/Toddler-11, [Pyr1]apelin-13, apelin receptor early endogenous ligand | peptide | Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F | 10.1038/S41594-022-00797-5 | 2022-07-27 | 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-8, desulfated cholecystokinin-8, CCK-39, CCK-58, CCK-33, CCK-4, gastrin-17 | peptide | Ding Y, Zhang H, Liao YY, Chen LN, Ji SY, Qin J, Mao C, Shen DD, Lin L, Wang H, Zhang Y, Li XM | 10.1038/S41421-022-00420-3 | 2022-07-20 | 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-8, desulfated cholecystokinin-8, gastrin-14, CCK-58, desulfated gastrin-17, CCK-39, CCK-33, desulfated gastrin-34, gastrin-34, gastrin-71, desulfated gastrin-71, CCK-4, desulfated gastrin-14, gastrin-17 | peptide | Ding Y, Zhang H, Liao YY, Chen LN, Ji SY, Qin J, Mao C, Shen DD, Lin L, Wang H, Zhang Y, Li XM | 10.1038/S41421-022-00420-3 | 2022-07-20 | 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, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine | small-molecule | Zhao C, Cheng L, Wang W, Wang H, Luo Y, Feng Y, Wang X, Fu H, Cai Y, Yang S, Fu P, Yan W, Shao Z | 10.1038/S41422-021-00567-W | 2021-09-29 | 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 | LH, hCG | peptide | Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE | 10.1038/S41586-021-03924-2 | 2021-09-29 | 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 | γ-MSH, agouti-related protein, β-MSH, α-MSH, ACTH | peptide | Zhang H, Chen LN, Yang D, Mao C, Shen Q, Feng W, Shen DD, Dai A, Xie S, Zhou Y, Qin J, Sun JP, Scharf DH, Hou T, Zhou T, Wang MW, Zhang Y | 10.1038/S41422-021-00552-3 | 2021-11-03 | 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 | neuropeptide-γ, hemokinin 1, neurokinin A, neuropeptide K, neurokinin B, substance P | peptide | Harris JA, Faust B, Gondin AB, Damgen MA, Suomivuori CM, Veldhuis NA, Cheng Y, Dror RO, Thal DM, Manglik A | 10.1038/S41589-021-00890-8 | 2021-11-03 | 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-phenylalanine, L-tryptophan | small-molecule | Zhou Y, Daver H, Trapkov B, Wu L, Wu M, Harpsoe K, Gentry PR, Liu K, Larionova M, Liu J, Chen N, Brauner-Osborne H, Gloriam DE, Hua T, Liu ZJ | 10.1038/S41422-021-00591-W | 2021-12-29 | 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-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide | peptide | Cary BP, Deganutti G, Zhao P, Truong TT, Piper SJ, Liu X, Belousoff MJ, Danev R, Sexton PM, Wootten D, Gellman SH | 10.1038/S41589-021-00945-W | 2022-01-05 | 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, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine | small-molecule | Xu Z, Ikuta T, Kawakami K, Kise R, Qian Y, Xia R, Sun MX, Zhang A, Guo C, Cai XH, Huang Z, Inoue A, He Y | 10.1038/S41589-021-00930-3 | 2022-01-05 | 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, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine | small-molecule | Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z | 10.1038/S41422-021-00566-X | 2021-09-29 | 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 | γ-MSH, β-MSH, α-MSH, ACTH | peptide | Ma S, Chen Y, Dai A, Yin W, Guo J, Yang D, Zhou F, Jiang Y, Wang MW, Xu HE | 10.1038/S41422-021-00557-Y | 2021-09-08 | 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 | LXA4, serum amyloid A, PrP106-126, aspirin-triggered resolvin D1, humanin, aspirin triggered lipoxin A4, LL-37, annexin I, resolvin D1 | peptide | Zhuang Y, Wang L, Guo J, Sun D, Wang Y, Liu W, Xu HE, Zhang C | 10.1038/S41467-022-28586-0 | 2022-03-30 | 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 |