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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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ENDOGENOUS 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 | 3PQR | - | 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 | 53654 | |
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 | (-)-noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, 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 | 53559 | |
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 | 53654 | |
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 | 53542 | |
Gi/o | αt3 | Bovine | Only H5 | 3 | - | - | - | - | X-ray | 5EN0 | 5EN0_refined | 2.8 | OPSD | Rhodopsin | Opsins | A (Rhodopsin) | Bovine | - | - | - |
Retinal (all-trans)
pubchem
|
small-molecule | Agonist | - | - | Singhal A, Guo Y, Matkovic M, Schertler G, Deupi X, Yan EC, Standfuss J | 10.15252/EMBR.201642671 | 2016-08-10 | 53698 | |
Gs | αs | Human | - | 47 | β1 | Human | γ2 | Human | Cryo-EM | 5UZ7 | 5UZ7_refined | 4.1 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - | - | - | - | - | - | calcitonin, amylin, adrenomedullin, calcitonin (salmon), 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 | 53542 | |
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 | 53542 | |
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 | 53654 | |
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 | 53654 | |
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 | 53654 | |
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 | 53654 | |
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 | 53654 | |
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 | 53542 | |
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 | 53544 | |
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 | 53544 | |
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 | 53544 | |
Gi/o | αo | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 6G79 | 6G79_refined | 3.8 | 5HT1B | 5-HT1B | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | - | - |
donitriptan
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | 5-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 | 53550 | |
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 | 53550 | |
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 | TIP39, PTH, PTHrP-(1-36), PTHrP | peptide | Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y | 10.1126/SCIENCE.AAV7942 | 2019-04-17 | 53559 | |
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 | 53550 | |
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 | 53544 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 6OS9 | 6OS9_refined | 3.0 | NTR1 | NTS1 | Neurotensin | A (Rhodopsin) | Human | - | scFv16 | - |
JMV449
pubchem
gtoplig
chembl_ligand
|
peptide | Agonist | large neurotensin, large neuromedin N, neurotensin, neuromedin N | peptide | Kato HE, Zhang Y, Hu H, Suomivuori CM, Kadji FMN, Aoki J, Krishna Kumar K, Fonseca R, Hilger D, Huang W, Latorraca NR, Inoue A, Dror RO, Kobilka BK, Skiniotis G | 10.1038/S41586-019-1337-6 | 2019-07-10 | 53544 | |
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 | 53544 | |
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 | - | - | Gao Y, Hu H, Ramachandran S, Erickson JW, Cerione RA, Skiniotis G | 10.1016/J.MOLCEL.2019.06.007 | 2019-07-24 | 53654 | |
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 | (-)-noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, 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 | 53542 | |
Gs | αs | Human | - | 49 | β1 | Human | γ2 | Human | Cryo-EM | 6ORV | - | 3.0 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
CHEMBL3950796
chembl_ligand
pubchem
|
small-molecule | Agonist | glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon | 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 | 53542 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 6KPG | 6KPG_refined | 3.0 | CNR1 | CB1 | Cannabinoid | A (Rhodopsin) | Human | - | scFv16 | - |
AM841
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | anandamide, 2-arachidonoylglycerol | small-molecule | Hua T, Li X, Wu L, Iliopoulos-Tsoutsouvas C, Wang Y, Wu M, Shen L, Brust CA, Nikas SP, Song F, Song X, Yuan S, Sun Q, Wu Y, Jiang S, Grim TW, Benchama O, Stahl EL, Zvonok N, Zhao S, Bohn LM, Makriyannis A, Liu ZJ | 10.1016/J.CELL.2020.01.008 | 2020-02-12 | 53544 | |
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 | 53654 | |
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 | 53542 | |
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 | 15-deoxy-LXA4, annexin I, aspirin triggered lipoxin A4, LTC4, fMet-Leu-Phe, LXA4, aspirin-triggered resolvin D1, resolvin D1, serum amyloid A, LL-37, PrP106-126, LTD4, humanin | 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 | 53544 | |
Gs | αs | Human | - | 57 | β1 | Rat | γ2 | Bovine | Cryo-EM | 6LPB | - | 3.9 | PACR | PAC1 | VIP and PACAP | B1 (Secretin) | Human | - | Nanobody-35 | - |
[Ac-His1]PACAP-27
gtoplig
chembl_ligand
pubchem
|
peptide | Agonist | VIP, PACAP-27, PHV, PHM, 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 | 53542 | |
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 | 53654 | |
Gs | αs | Human | - | 49 | β1 | Human | γ2 | Human | Cryo-EM | 6B3J | 6B3J_refined | 3.3 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | - | - |
Exendin-P5
|
peptide | Agonist | glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon | 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 | 53542 | |
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 | 53545 | |
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 | 53542 | |
Gs | αs | Human | - | 43 | β1 | Human | γ2 | Human | Cryo-EM | 6NIY | 6NIY_refined | 3.3 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - | - | - |
Calcitonin salmon
pubchem
|
peptide | Agonist | calcitonin, amylin, adrenomedullin, calcitonin (salmon), 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 | 53542 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 6N4B | 6N4B_refined | 3.0 | CNR1 | CB1 | Cannabinoid | A (Rhodopsin) | Human | - | scFv16 | - |
MDMB-Fubinaca
pubchem
gtoplig
|
small-molecule | Agonist | anandamide, 2-arachidonoylglycerol | small-molecule | Krishna Kumar K, Shalev-Benami M, Robertson MJ, Hu H, Banister SD, Hollingsworth SA, Latorraca NR, Kato HE, Hilger D, Maeda S, Weis WI, Farrens DL, Dror RO, Malhotra SV, Kobilka BK, Skiniotis G | 10.1016/J.CELL.2018.11.040 | 2019-01-30 | 53544 | |
Gs | αs | Bovine | - | 58 | β1 | Rat | γ2 | Bovine | Cryo-EM | 6NBF | - | 3.0 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
Long-acting parathyroid hormone analog
|
peptide | Agonist | TIP39, PTH, PTHrP-(1-36), PTHrP | peptide | Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y | 10.1126/SCIENCE.AAV7942 | 2019-04-17 | 53559 | |
Gs | αs | Bovine | - | 56 | β1 | Rat | γ2 | Bovine | Cryo-EM | 6NBI | - | 4.0 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
Long-acting parathyroid hormone analog
|
peptide | Agonist | TIP39, PTH, PTHrP-(1-36), PTHrP | peptide | Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y | 10.1126/SCIENCE.AAV7942 | 2019-04-17 | 53559 | |
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 | 53553 | |
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 | (-)-noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, 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 | 53542 | |
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 neurotensin, large neuromedin N, neurotensin, neuromedin N | peptide | Kato HE, Zhang Y, Hu H, Suomivuori CM, Kadji FMN, Aoki J, Krishna Kumar K, Fonseca R, Hilger D, Huang W, Latorraca NR, Inoue A, Dror RO, Kobilka BK, Skiniotis G | 10.1038/S41586-019-1337-6 | 2019-07-10 | 53544 | |
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 | 53654 | |
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 | 53542 | |
Gs | αs | Human | - | 49 | β1 | Human | γ2 | Human | Cryo-EM | 6P9Y | 6P9Y_refined | 3.0 | PACR | PAC1 | VIP and PACAP | B1 (Secretin) | Human | - | Nanobody-35 | - |
[Ac-His1]PACAP-27
gtoplig
chembl_ligand
pubchem
|
peptide | Agonist | VIP, PACAP-27, PHV, PHM, 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 | 53542 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 6KPF | 6KPF_refined | 2.9 | CNR2 | CB2 | Cannabinoid | A (Rhodopsin) | Human | - | scFv16 | - |
7-[(6aR,9R,10aR)-1-Hydroxy-9-(hydroxymethyl)-6,6-dimethyl-6a,7,8,9,10,10a-hexahydro-6H-benzo[c]chromen-3-yl]-7-methyloctanenitrile
pubchem
|
small-molecule | Agonist | anandamide, 2-arachidonoylglycerol | small-molecule | Hua T, Li X, Wu L, Iliopoulos-Tsoutsouvas C, Wang Y, Wu M, Shen L, Brust CA, Nikas SP, Song F, Song X, Yuan S, Sun Q, Wu Y, Jiang S, Grim TW, Benchama O, Stahl EL, Zvonok N, Zhao S, Bohn LM, Makriyannis A, Liu ZJ | 10.1016/J.CELL.2020.01.008 | 2020-02-12 | 53544 | |
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 | 53542 | |
Gi/o | αi1 | Human | - | 100 | β1 | Human | γ2 | Human | Cryo-EM | 6PT0 | 6PT0_refined | 3.2 | CNR2 | CB2 | Cannabinoid | A (Rhodopsin) | Human | - | scFv16 | - |
WIN55212-2
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | anandamide, 2-arachidonoylglycerol | small-molecule | Xing C, Zhuang Y, Xu TH, Feng Z, Zhou XE, Chen M, Wang L, Meng X, Xue Y, Wang J, Liu H, McGuire TF, Zhao G, Melcher K, Zhang C, Xu HE, Xie XQ | 10.1016/J.CELL.2020.01.007 | 2020-02-12 | 53544 | |
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 | 53542 | |
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 | VIP, PACAP-27, PHV, PHM, 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 | 53542 | |
Gs | αs | Human | - | 48 | β1 | Human | γ2 | Human | Cryo-EM | 6UUN | - | 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 | 53542 | |
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 | 53544 | |
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 | 53542 | |
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 | VIP, PACAP-27, PHV, PHM, 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 | 53542 | |
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 | 53542 | |
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 | 53542 | |
Gi/o | αo | Human | - | 60 | β1 | Mouse | γ2 | Human | Cryo-EM | 6K41 | - | 2.9 | ADA2B | α2B | Adrenoceptors | A (Rhodopsin) | Human | T4-Lysozyme | scFv | - |
dexmedetomidine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | (-)-adrenaline, (-)-noradrenaline | small-molecule | Yuan D, Liu Z, Kaindl J, Maeda S, Zhao J, Sun X, Xu J, Gmeiner P, Wang HW, Kobilka BK | 10.1038/S41589-020-0492-2 | 2020-04-15 | 53550 | |
Gi/o | αi1 | Human | - | 62 | β1 | Mouse | γ2 | Human | Cryo-EM | 6K42 | - | 4.1 | ADA2B | α2B | Adrenoceptors | A (Rhodopsin) | Human | T4-Lysozyme | scFv | - |
dexmedetomidine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | (-)-adrenaline, (-)-noradrenaline | small-molecule | Yuan D, Liu Z, Kaindl J, Maeda S, Zhao J, Sun X, Xu J, Gmeiner P, Wang HW, Kobilka BK | 10.1038/S41589-020-0492-2 | 2020-04-15 | 53544 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 6VMS | 6VMS_refined | 3.8 | DRD2 | D2 | Dopamine | A (Rhodopsin) | Human | T4-Lysozyme | scFv16 | - |
bromocriptine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | dopamine | small-molecule | Yin J, Chen KM, Clark MJ, Hijazi M, Kumari P, Bai XC, Sunahara RK, Barth P, Rosenbaum DM | 10.1038/S41586-020-2379-5 | 2020-06-17 | 53544 | |
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 | 53674 | |
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 | 53674 | |
Gs | αs | Human | - | 57 | β1 | Human | γ2 | Human | Cryo-EM | 6VCB | 6VCB_refined | 3.3 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
glucagon-like peptide 1-(7-37)
pubchem
gtoplig
chembl_ligand
gtoplig
pubchem
pubchem
CHEMBL5197819 chembl_ligand pubchem |
peptide small-molecule |
Agonist PAM |
glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon | 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 | 53542 | |
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 | 53542 | |
Gs | αs | Human | - | 49 | β1 | Human | γ2 | Human | Cryo-EM | 7C2E | 7C2E_refined | 4.2 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
2-[[4-[6-[(4-cyano-2-fluoranyl-phenyl)methoxy]pyridin-2-yl]-3,6-dihydro-2~{H}-pyridin-1-yl]methyl]-3-[[(2~{S})-oxetan-2-yl]methyl]imidazo[4,5-b]pyridine-5-carboxylic acid
pubchem
|
small-molecule | Agonist | glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon | 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 | 53542 | |
Gi/o | αi1 | Human | - | 65 | β1 | Human | γ2 | Human | Cryo-EM | 6LFO | - | 3.4 | CXCR2 | CXCR2 | Chemokine | A (Rhodopsin) | Human | - | scFv16 | - |
Interleukin-8
pubchem
|
protein | Agonist | CXCL3, CXCL2, CXCL7, CXCL5, CXCL1, CXCL8, CXCL6 | 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 | 53544 | |
Gs | αs | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 6VN7 | 6VN7_refined | 3.2 | VIPR1 | VPAC1 | VIP and PACAP | B1 (Secretin) | Human | - | Nanobody-35 | - |
[Ac-His1]PACAP-27
gtoplig
chembl_ligand
pubchem
|
peptide | Agonist | VIP, PACAP-27, PHM, PHI, secretin, GHRH, PACAP-38 | peptide | Duan J, Shen DD, Zhou XE, Bi P, Liu QF, Tan YX, Zhuang YW, Zhang HB, Xu PY, Huang SJ, Ma SS, He XH, Melcher K, Zhang Y, Xu HE, Jiang Y | 10.1038/S41467-020-17933-8 | 2020-09-02 | 53542 | |
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-like peptide 1-(7-36) amide, glucagon | 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 | 53542 | |
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-like peptide 1-(7-36) amide, glucagon | 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 | 53542 | |
Gq/11 | αq | Human | Gq-Gi2-Gs chimera | 59 | 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 | 53552 | |
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 | 53544 | |
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 | 53544 | |
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 | 53542 | |
Gs | αs | Human | - | 56 | β1 | Human | γ2 | Human | Cryo-EM | 6XOX | - | 3.1 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - |
scFv16 Nanobody-35 |
- |
oforglipron
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon | 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 | 53542 | |
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 | PGI2, PGE1, PGD2, thromboxane A2, PGF2α, 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 | 53542 | |
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 | 53559 | |
Gs | αs | Human | - | 49 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7DHR | 7DHR_refined | 3.8 | ADRB2 | β2 | Adrenoceptors | A (Rhodopsin) | Human | - | Nanobody-35 | - |
LEVISOPRENALINE
chembl_ligand
chembl_ligand
pubchem
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, Zn2+, noradrenaline | small-molecule | Liu QS, An HW, Wang XF, Kong FP, Sun YC, Gong YX, Lou SF, Shi YF, Sun N, Deng B, Wang J, Wang JJ | 10.1093/NSR/NWAA284 | 2020-12-16 | 53542 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γT1 | Human | Cryo-EM | 7L0P | - | 4.1 | NTR1 | NTS1 | Neurotensin | A (Rhodopsin) | Rat | - | - | - |
neurotensin
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
|
peptide | Agonist | neurotensin, neuromedin N | peptide | Zhang M, Gui M, Wang ZF, Gorgulla C, Yu JJ, Wu H, Sun ZJ, Klenk C, Merklinger L, Morstein L, Hagn F, Pluckthun A, Brown A, Nasr ML, Wagner G | 10.1038/S41594-020-00554-6 | 2021-01-06 | 53544 | |
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 | neurotensin, neuromedin N | peptide | Zhang M, Gui M, Wang ZF, Gorgulla C, Yu JJ, Wu H, Sun ZJ, Klenk C, Merklinger L, Morstein L, Hagn F, Pluckthun A, Brown A, Nasr ML, Wagner G | 10.1038/S41594-020-00554-6 | 2021-01-06 | 53544 | |
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-like peptide 1-(7-36) amide, glucagon | 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 | 53542 | |
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 | 53550 | |
Gs | αs | Human | Engineered G alpha | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7L1U | 7L1U_refined | 3.2 | OX2R | OX2 | Orexin | A (Rhodopsin) | Human | - | scFv16 | - |
Orexin-A
pubchem
|
peptide | Agonist | orexin-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 | 53542 | |
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 | (-)-noradrenaline, dopamine, L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine | 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 | 53542 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7JVR | 7JVR_refined | 2.8 | DRD2 | D2 | Dopamine | A (Rhodopsin) | Human | - | scFv16 | - |
bromocriptine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | dopamine | small-molecule | Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP, Shen DD, Xu T, Liu YF, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE | 10.1016/J.CELL.2021.01.027 | 2021-02-24 | 53544 | |
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 | (-)-noradrenaline, dopamine, L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine | 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 | 53542 | |
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 | (-)-noradrenaline, dopamine, L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine | 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 | 53542 | |
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 | (-)-noradrenaline, dopamine, L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine | 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 | 53542 | |
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 |
(-)-noradrenaline, dopamine, L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine | 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 | 53542 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7CMU | 7CMU_refined | 3.0 | DRD3 | D3 | Dopamine | A (Rhodopsin) | Human | BRIL | scFv16 | - |
pramipexole
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | dopamine | small-molecule | Xu P, Huang S, Mao C, Krumm BE, Zhou XE, Tan Y, Huang XP, Liu Y, Shen DD, Jiang Y, Yu X, Jiang H, Melcher K, Roth BL, Cheng X, Zhang Y, Xu HE | 10.1016/J.MOLCEL.2021.01.003 | 2021-03-10 | 53544 | |
Gq/11 | αq | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7DFL | 7DFL_refined | 3.3 | HRH1 | H1 | Histamine | A (Rhodopsin) | Human | - | scFv16 | - |
histamine
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
gtoplig
|
small-molecule | Agonist | histamine | small-molecule | 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 | 53552 | |
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 | 53544 | |
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 | 53544 | |
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 | 53544 | |
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 | PGI2, PGE1, PGD2, thromboxane A2, PGF2α, 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 | 53542 | |
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 | PGI2, PGE1, PGD2, thromboxane A2, PGF2α, 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 | 53542 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7KH0 | 7KH0_refined | 2.8 | V2R | V2 | Vasopressin and oxytocin | A (Rhodopsin) | Human | - |
scFv16 Nanobody-35 |
- |
vasopressin
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
peptide | Agonist | vasopressin, oxytocin | peptide | Wang L, Xu J, Cao S, Sun D, Liu H, Lu Q, Liu Z, Du Y, Zhang C | 10.1038/S41422-021-00483-Z | 2021-05-26 | 53542 | |
Gs | αs | Human | - | 61 | β1 | Rat | γ2 | Human | Cryo-EM | 7MBX | 7MBX_refined | 2.0 | CCKAR | CCK1 | Cholecystokinin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
CHEMBL216166
chembl_ligand
pubchem
|
protein | Agonist | CCK-8, CCK-33, CCK-4, CCK-39, gastrin-17, CCK-58, desulfated cholecystokinin-8 | peptide | Mobbs JI, Belousoff MJ, Harikumar KG, Piper SJ, Xu X, Furness SGB, Venugopal H, Christopoulos A, Danev R, Wootten D, Thal DM, Miller LJ, Sexton PM | 10.1371/JOURNAL.PBIO.3001295 | 2021-05-26 | 53542 | |
Gs | αs | Human | - | 54 | β1 | Human | γ2 | Human | Cryo-EM | 7BB6 | 7BB6_refined | 4.2 | V2R | V2 | Vasopressin and oxytocin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
vasopressin
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
peptide | Agonist | vasopressin, oxytocin | peptide | Bous J, Orcel H, Floquet N, Leyrat C, Lai-Kee-Him J, Gaibelet G, Ancelin A, Saint-Paul J, Trapani S, Louet M, Sounier R, Demene H, Granier S, Bron P, Mouillac B | 10.1126/SCIADV.ABG5628 | 2021-06-02 | 53542 | |
Gi/o | αi3 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7E9H | - | 4.0 | GRM4 | mGlu4 | Metabotropic glutamate | C (Glutamate) | Human | - | scFv16 | - |
L-serine-O-phosphate
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
|
small-molecule | Agonist | L-serine-O-phosphate, L-glutamic acid | small-molecule | Lin S, Han S, Cai X, Tan Q, Zhou K, Wang D, Wang X, Du J, Yi C, Chu X, Dai A, Zhou Y, Chen Y, Zhou Y, Liu H, Liu J, Yang D, Wang MW, Zhao Q, Wu B | 10.1038/S41586-021-03495-2 | 2021-06-23 | 53546 | |
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
oforglipron pubchem gtoplig chembl_ligand |
small-molecule small-molecule |
Ago-PAM Agonist |
glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon | 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 | 53542 | |
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 | 53544 | |
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 | 53544 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7F1Q | - | 2.9 | CCR5 | CCR5 | Chemokine | A (Rhodopsin) | Human | - | - | - |
CCL3
gtoplig
|
peptide | Agonist | CCL13, CCL2, CCL14, CCL8, CCL4, CCL7, CCL3, CCL16, CCL11, CCL5 | peptide | - | - | 2021-07-14 | 53544 | |
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) | CCL13, CCL2, CCL14, CCL8, CCL4, CCL7, CCL3, CCL16, CCL11, CCL5 | 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 | 53544 | |
Gs | αs | Human | - | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7DW9 | - | 2.6 | V2R | V2 | Vasopressin and oxytocin | A (Rhodopsin) | Human | - |
Nanobody-35 scFv16 |
- |
vasopressin
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
peptide | Agonist | vasopressin, oxytocin | peptide | Zhou F, Ye C, Ma X, Yin W, Croll TI, Zhou Q, He X, Zhang X, Yang D, Wang P, Xu HE, Wang MW, Jiang Y | 10.1038/S41422-021-00480-2 | 2021-07-21 | 53542 | |
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 | 53542 | |
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 | 53559 | |
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-like peptide 1-(7-36) amide, glucagon | peptide | Zhang X, Belousoff MJ, Liang YL, Danev R, Sexton PM, Wootten D | 10.1016/J.CELREP.2021.109374 | 2021-08-04 | 53542 | |
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-like peptide 1-(7-36) amide, glucagon | 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 | 53542 | |
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 | 53544 | |
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 | ghrelin, [des-Gln14]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 | 53552 | |
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 | ghrelin, [des-Gln14]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 | 53552 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7EZK | 7EZK_refined | 3.1 | CCKAR | CCK1 | Cholecystokinin | A (Rhodopsin) | Human | - | - | - |
CCK-8
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
peptide | Agonist | CCK-8, CCK-33, CCK-4, CCK-39, gastrin-17, CCK-58, desulfated cholecystokinin-8 | peptide | Liu Q, Yang D, Zhuang Y, Croll TI, Cai X, Dai A, He X, Duan J, Yin W, Ye C, Zhou F, Wu B, Zhao Q, Xu HE, Wang MW, Jiang Y | 10.1038/S41589-021-00841-3 | 2021-08-25 | 53542 | |
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 | 53545 | |
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 | 53542 | |
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 | 53654 | |
Gi/o | αo | Human | - | 59 | β1 | Rat | γ2 | Mouse | Cryo-EM | 6WWZ | 6WWZ_refined | 3.3 | CCR6 | CCR6 | Chemokine | A (Rhodopsin) | Human | - | scFv16 | - |
CCL20
gtoplig
|
peptide | Agonist | beta-defensin 4A, CCL20 | peptide | Wasilko DJ, Johnson ZL, Ammirati M, Che Y, Griffor MC, Han S, Wu H | 10.1038/S41467-020-16820-6 | 2020-06-24 | 53550 | |
Gs | αs | Human | - | 50 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7BZ2 | 7BZ2_refined | 3.8 | ADRB2 | β2 | Adrenoceptors | A (Rhodopsin) | Human | - | Nanobody-35 | - |
arformoterol
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, 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 | 53542 | |
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 | 53542 | |
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 | 53542 | |
Gi/o | αi1 | Human | - | 65 | β1 | Human | γ2 | Human | Cryo-EM | 6LFM | - | 3.5 | CXCR2 | CXCR2 | Chemokine | A (Rhodopsin) | Human | - | scFv16 | - |
Interleukin-8
pubchem
|
protein | Agonist | CXCL3, CXCL2, CXCL7, CXCL5, CXCL1, CXCL8, CXCL6 | 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 | 53544 | |
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 | - | - | - | - | lithocholic acid, chenodeoxycholic acid, deoxycholic acid, cholic 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 | 53542 | |
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 | 53559 | |
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-like peptide 1-(7-36) amide, glucagon | 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 | 53542 | |
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 | lithocholic acid, chenodeoxycholic acid, deoxycholic acid, cholic 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 | 53542 | |
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 |
lithocholic acid, chenodeoxycholic acid, deoxycholic acid, cholic 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 | 53542 | |
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 | 53544 | |
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 | 53544 | |
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 | 53542 | |
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 | 53558 | |
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 | (-)-noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, Zn2+, noradrenaline | small-molecule | Liu QS, An HW, Wang XF, Kong FP, Sun YC, Gong YX, Lou SF, Shi YF, Sun N, Deng B, Wang J, Wang JJ | 10.1093/NSR/NWAA284 | 2020-12-16 | 53542 | |
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 | neurotensin, neuromedin N | peptide | Zhang M, Gui M, Wang ZF, Gorgulla C, Yu JJ, Wu H, Sun ZJ, Klenk C, Merklinger L, Morstein L, Hagn F, Pluckthun A, Brown A, Nasr ML, Wagner G | 10.1038/S41594-020-00554-6 | 2021-01-06 | 53544 | |
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 | neurotensin, neuromedin N | peptide | Zhang M, Gui M, Wang ZF, Gorgulla C, Yu JJ, Wu H, Sun ZJ, Klenk C, Merklinger L, Morstein L, Hagn F, Pluckthun A, Brown A, Nasr ML, Wagner G | 10.1038/S41594-020-00554-6 | 2021-01-06 | 53544 | |
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 | 53550 | |
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 | 53542 | |
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 | (-)-noradrenaline, dopamine, L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine | 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 | 53542 | |
Gs | αs | Human | Engineered G alpha | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7JVQ | - | 3.0 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
apomorphine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | (-)-noradrenaline, dopamine, L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine | 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 | 53542 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7CKX | 7CKX_refined | 3.5 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
A77636
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | (-)-noradrenaline, dopamine, L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine | 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 | 53542 | |
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 |
(-)-noradrenaline, dopamine, L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine | 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 | 53542 | |
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 |
(-)-noradrenaline, dopamine, L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine | 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 | 53542 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7CMV | 7CMV_refined | 2.7 | DRD3 | D3 | Dopamine | A (Rhodopsin) | Human | BRIL | scFv16 | - |
CHEMBL70565
chembl_ligand
chembl_ligand
pubchem
|
small-molecule | Agonist | dopamine | small-molecule | - | - | 2021-03-10 | 53544 | |
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 | 53544 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7E2Z | 7E2Z_refined | 3.1 | 5HT1A | 5-HT1A | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | - | - |
aripiprazole
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist (partial) | 5-hydroxytryptamine | small-molecule | Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen DD, Yen HY, Robinson CV, Harpsoe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE | 10.1038/S41586-021-03376-8 | 2021-04-14 | 53544 | |
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 | (-)-noradrenaline, dopamine, L-NOREPINEPHRINE, noradrenaline, 5-hydroxytryptamine | 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 | 53542 | |
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 | α-MSH, γ-MSH, agouti-related protein, β-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 | 53542 | |
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 | PGI2, PGE1, PGD2, thromboxane A2, PGF2α, 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 | 53542 | |
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 | 53544 | |
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, CCK-33, CCK-4, CCK-39, gastrin-17, CCK-58, desulfated cholecystokinin-8 | peptide | Mobbs JI, Belousoff MJ, Harikumar KG, Piper SJ, Xu X, Furness SGB, Venugopal H, Christopoulos A, Danev R, Wootten D, Thal DM, Miller LJ, Sexton PM | 10.1371/JOURNAL.PBIO.3001295 | 2021-05-26 | 53552 | |
Gs | αs | Human | - | 55 | β1 | Human | γ2 | Human | Cryo-EM | 7BB7 | 7BB7_refined | 4.4 | V2R | V2 | Vasopressin and oxytocin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
vasopressin
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
peptide | Agonist | vasopressin, oxytocin | peptide | Bous J, Orcel H, Floquet N, Leyrat C, Lai-Kee-Him J, Gaibelet G, Ancelin A, Saint-Paul J, Trapani S, Louet M, Sounier R, Demene H, Granier S, Bron P, Mouillac B | 10.1126/SCIADV.ABG5628 | 2021-06-02 | 53542 | |
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 | 53544 | |
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 | CCL13, CCL2, CCL14, CCL8, CCL4, CCL7, CCL3, CCL16, CCL11, CCL5 | 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 | 53544 | |
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-like peptide 1-(7-36) amide, glucagon | 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 | 53542 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7F1R | - | 3.0 | CCR5 | CCR5 | Chemokine | A (Rhodopsin) | Human | - | - | - |
CCL5
gtoplig
|
peptide | Agonist | CCL13, CCL2, CCL14, CCL8, CCL4, CCL7, CCL3, CCL16, CCL11, CCL5 | peptide | - | - | 2021-07-14 | 53544 | |
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 | 53542 | |
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 | 53544 | |
Gs | αs | Human | - | 89 | β1 | Human | γ2 | Human | Cryo-EM | 7KI1 | - | 2.5 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
Taspoglutide
pubchem
|
peptide | Agonist | glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon | peptide | Zhang X, Belousoff MJ, Liang YL, Danev R, Sexton PM, Wootten D | 10.1016/J.CELREP.2021.109374 | 2021-08-04 | 53542 | |
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-like peptide 1-(7-36) amide, glucagon | 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 | 53542 | |
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 | TIP39, PTHrP-(1-36), PTHrP, PTH, PTHrP-(1-34) (human) | 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 | 53542 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7EZH | 7EZH_refined | 3.2 | CCKAR | CCK1 | Cholecystokinin | A (Rhodopsin) | Human | - | scFv16 | - |
CCK-8
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
peptide | Agonist | CCK-8, CCK-33, CCK-4, CCK-39, gastrin-17, CCK-58, desulfated cholecystokinin-8 | peptide | Liu Q, Yang D, Zhuang Y, Croll TI, Cai X, Dai A, He X, Duan J, Yin W, Ye C, Zhou F, Wu B, Zhao Q, Xu HE, Wang MW, Jiang Y | 10.1038/S41589-021-00841-3 | 2021-08-25 | 53544 | |
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, CCK-33, CCK-4, CCK-39, gastrin-17, CCK-58, desulfated cholecystokinin-8 | peptide | Liu Q, Yang D, Zhuang Y, Croll TI, Cai X, Dai A, He X, Duan J, Yin W, Ye C, Zhou F, Wu B, Zhao Q, Xu HE, Wang MW, Jiang Y | 10.1038/S41589-021-00841-3 | 2021-08-25 | 53552 | |
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 | 53545 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7EW2 | 7EW2_refined | 3.1 | S1PR3 | S1P3 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
(S)-FTY720-phosphate
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | sphingosylphosphorylcholine, sphingosine 1-phosphate, dihydrosphingosine 1-phosphate | small-molecule | Zhao C, Cheng L, Wang W, Wang H, Luo Y, Feng Y, Wang X, Fu H, Cai Y, Yang S, Fu P, Yan W, Shao Z | 10.1038/S41422-021-00567-W | 2021-09-29 | 53544 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7EW4 | 7EW4_refined | 3.2 | S1PR3 | S1P3 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
CYM-5541
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | sphingosylphosphorylcholine, sphingosine 1-phosphate, dihydrosphingosine 1-phosphate | small-molecule | Zhao C, Cheng L, Wang W, Wang H, Luo Y, Feng Y, Wang X, Fu H, Cai Y, Yang S, Fu P, Yan W, Shao Z | 10.1038/S41422-021-00567-W | 2021-09-29 | 53544 | |
Gs | αs | Bovine | - | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7FIH | - | 3.2 | LSHR | LH | Glycoprotein hormone | A (Rhodopsin) | Human | - | - | - |
Choriogonadotropin beta
gtoplig
Glycoprotein alpha gtoplig 5-Amino-N-(1,1-dimethylethyl)-2-(methylthio)-4-[3-[[2-(4-morpholinyl)acetyl]amino]phenyl]thieno[2,3-d]pyrimidine-6-carboxamide pubchem |
protein protein small-molecule |
Agonist | LH, hCG | peptide | Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE | 10.1038/S41586-021-03924-2 | 2021-09-29 | 53559 | |
Gs | αs | Bovine | - | 91 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7FII | - | 4.3 | LSHR | LH | Glycoprotein hormone | A (Rhodopsin) | Human | - | - | - |
Choriogonadotropin beta
gtoplig
Glycoprotein alpha gtoplig |
protein protein |
Agonist | LH, hCG | peptide | Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE | 10.1038/S41586-021-03924-2 | 2021-09-29 | 53559 | |
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 | [Hyp3]bradykinin, Lys-[Hyp3]-bradykinin, bradykinin, kallidin, [des-Arg10]kallidin, [des-Arg9]bradykinin, T-kinin | 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 | 53552 | |
Gi/o | αi2 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7F8V | 7F8V_refined | 3.3 | GASR | CCK2 | Cholecystokinin | A (Rhodopsin) | Human | - | - | - |
desulfated gastrin-17
pubchem
gtoplig
chembl_ligand
pubchem
|
peptide | Agonist | CCK-8, CCK-33, CCK-4, desulfated gastrin-17, gastrin-34, CCK-39, gastrin-17, gastrin-71, desulfated gastrin-34, CCK-58, desulfated cholecystokinin-8, gastrin-14, desulfated gastrin-71, desulfated gastrin-14 | 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 | 53545 | |
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 | α-MSH, γ-MSH, agouti-related protein, β-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 | 53542 | |
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 | α-MSH, γ-MSH, agouti-related protein, β-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 | 53542 | |
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 | hemokinin 1, substance P, neurokinin A, neurokinin B, neuropeptide K, neuropeptide-γ | peptide | Harris JA, Faust B, Gondin AB, Damgen MA, Suomivuori CM, Veldhuis NA, Cheng Y, Dror RO, Thal DM, Manglik A | 10.1038/S41589-021-00890-8 | 2021-11-03 | 53542 | |
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 | α-MSH, γ-MSH, agouti-related protein, β-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 | 53542 | |
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 | 53552 | |
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 | 53544 | |
Gq/11 | αq | Human | Gq-Gs chimera | 57 | β1 | Human | γ2 | Human | Cryo-EM | 7S8P | 7S8P_refined | 2.6 | MRGX4 | MRGPRX4 | A orphans | A (Rhodopsin) | Human | BRIL | scFv16 | - |
N-[(1r,3R,5S,7R)-3,5-dimethyltricyclo[3.3.1.1~3,7~]decane-1-carbonyl]-D-phenylalanine
pubchem
|
small-molecule | Agonist | - | - | Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL | 10.1038/S41586-021-04126-6 | 2021-11-17 | 53552 | |
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 | 53544 | |
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 | 53544 | |
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 | 53544 | |
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 | ghrelin, [des-Gln14]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 | 53544 | |
Gq/11 | αq | Human | Gq-Gs-Gi1 chimera | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7P00 | - | 2.7 | NK1R | NK1 | Tachykinin | A (Rhodopsin) | Human | - | scFv16 | - |
substance P
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
|
peptide | Agonist | hemokinin 1, substance P, neurokinin A, neurokinin B, neuropeptide K, neuropeptide-γ | peptide | Thom C, Ehrenmann J, Vacca S, Waltenspuhl Y, Schoppe J, Medalia O, Pluckthun A | 10.1126/SCIADV.ABK2872 | 2021-12-15 | 53552 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7EW1 | 7EW1_refined | 3.4 | S1PR5 | S1P5 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
siponimod
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
small-molecule | Agonist | sphingosylphosphorylcholine, sphingosine 1-phosphate, dihydrosphingosine 1-phosphate | small-molecule | Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z | 10.1038/S41422-021-00566-X | 2021-09-29 | 53544 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7EW3 | 7EW3_refined | 3.1 | S1PR3 | S1P3 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
Sphingosine 1-phosphate
pubchem
|
lipid | Agonist | sphingosylphosphorylcholine, sphingosine 1-phosphate, dihydrosphingosine 1-phosphate | small-molecule | Zhao C, Cheng L, Wang W, Wang H, Luo Y, Feng Y, Wang X, Fu H, Cai Y, Yang S, Fu P, Yan W, Shao Z | 10.1038/S41422-021-00567-W | 2021-09-29 | 53544 | |
Gs | αs | Bovine | - | 91 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7FIG | - | 3.9 | LSHR | LH | Glycoprotein hormone | A (Rhodopsin) | Human | - | Nanobody-35 | - |
Choriogonadotropin beta
gtoplig
Glycoprotein alpha gtoplig |
protein protein |
Agonist | LH, hCG | peptide | Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE | 10.1038/S41586-021-03924-2 | 2021-09-29 | 53559 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7RTB | 7RTB_refined | 2.1 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
Peptide-19
|
peptide | Agonist | glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon | peptide | Johnson RM, Zhang X, Piper SJ, Nettleton TJ, Vandekolk TH, Langmead CJ, Danev R, Sexton PM, Wootten D | 10.1016/J.BBRC.2021.09.016 | 2021-10-06 | 53542 | |
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 | [Hyp3]bradykinin, Lys-[Hyp3]-bradykinin, bradykinin, kallidin, [des-Arg10]kallidin, [des-Arg9]bradykinin, T-kinin | 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 | 53552 | |
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, CCK-33, CCK-4, desulfated gastrin-17, gastrin-34, CCK-39, gastrin-17, gastrin-71, desulfated gastrin-34, CCK-58, desulfated cholecystokinin-8, gastrin-14, desulfated gastrin-71, desulfated gastrin-14 | 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 | 53552 | |
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 | α-MSH, γ-MSH, agouti-related protein, β-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 | 53542 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7F55 | - | 3.1 | MC4R | MC4 | Melanocortin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
bremelanotide
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
peptide | Agonist | α-MSH, γ-MSH, agouti-related protein, β-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 | 53542 | |
Gs | αs | Human | Gs-Gq chimera | 49 | β1 | Human | γ2 | Human | Cryo-EM | 7RMG | - | 3.0 | NK1R | NK1 | Tachykinin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
substance P
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
|
peptide | Agonist | hemokinin 1, substance P, neurokinin A, neurokinin B, neuropeptide K, neuropeptide-γ | peptide | Harris JA, Faust B, Gondin AB, Damgen MA, Suomivuori CM, Veldhuis NA, Cheng Y, Dror RO, Thal DM, Manglik A | 10.1038/S41589-021-00890-8 | 2021-11-03 | 53542 | |
Gs | αs | Human | Gs-Gq chimera | 49 | 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 | hemokinin 1, substance P, neurokinin A, neurokinin B, neuropeptide K, neuropeptide-γ | peptide | Harris JA, Faust B, Gondin AB, Damgen MA, Suomivuori CM, Veldhuis NA, Cheng Y, Dror RO, Thal DM, Manglik A | 10.1038/S41589-021-00890-8 | 2021-11-03 | 53542 | |
Gs | αs | Human | - | 46 | β1 | Rat | γ2 | Mouse | Cryo-EM | 7PIV | 7PIV_refined | 2.9 | MC4R | MC4 | Melanocortin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
afamelanotide
pubchem
gtoplig
chembl_ligand
drugbank
pubchem
pubchem
pubchem
pubchem
|
peptide | Agonist | α-MSH, γ-MSH, agouti-related protein, β-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 | 53542 | |
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 | 53552 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7S8O | 7S8O_refined | 2.6 | MRGX2 | MRGPRX2 | A orphans | A (Rhodopsin) | Human | BRIL | scFv16 | - |
(R)-ZINC-3573
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | PAMP-20 | peptide | Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL | 10.1038/S41586-021-04126-6 | 2021-11-17 | 53544 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7VDH | - | 2.9 | MRGX2 | MRGPRX2 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
compound 48/80
pubchem
gtoplig
|
small-molecule | Agonist | PAMP-20 | peptide | Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP | 10.1038/S41586-021-04077-Y | 2021-12-01 | 53544 | |
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 | 53544 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7VUZ | 7VUZ_refined | 2.9 | MRGX2 | MRGPRX2 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
PAMP-12
pubchem
|
peptide | Agonist | PAMP-20 | peptide | Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP | 10.1038/S41586-021-04077-Y | 2021-12-01 | 53544 | |
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 | 53544 | |
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 | ghrelin, [des-Gln14]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 | 53544 | |
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 | hemokinin 1, substance P, neurokinin A, neurokinin B, neuropeptide K, neuropeptide-γ | peptide | Thom C, Ehrenmann J, Vacca S, Waltenspuhl Y, Schoppe J, Medalia O, Pluckthun A | 10.1126/SCIADV.ABK2872 | 2021-12-15 | 53542 | |
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 | 53542 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7VUJ | 7VUJ_refined | 3.8 | GP139 | GPR139 | A orphans | A (Rhodopsin) | Human | - | Nanobody-35 | Xylanase |
JNJ-63533054
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | L-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 | 53542 | |
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-like peptide 1-(7-36) amide, glucagon | 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 | 53542 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7EO2 | 7EO2_refined | 2.9 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
(S)-FTY720-phosphate
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | sphingosylphosphorylcholine, sphingosine 1-phosphate, dihydrosphingosine 1-phosphate | small-molecule | Xu Z, Ikuta T, Kawakami K, Kise R, Qian Y, Xia R, Sun MX, Zhang A, Guo C, Cai XH, Huang Z, Inoue A, He Y | 10.1038/S41589-021-00930-3 | 2022-01-05 | 53544 | |
Gi/o | αi1 | Human | - | 40 | β1 | Human | γ2 | Human | Cryo-EM | 7WF7 | 7WF7_refined | 3.4 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
sphingosine 1-phosphate
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | sphingosylphosphorylcholine, sphingosine 1-phosphate, dihydrosphingosine 1-phosphate | small-molecule | Xu Z, Ikuta T, Kawakami K, Kise R, Qian Y, Xia R, Sun MX, Zhang A, Guo C, Cai XH, Huang Z, Inoue A, He Y | 10.1038/S41589-021-00930-3 | 2022-01-05 | 53544 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7LLL | 7LLL_refined | 3.7 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
exendin-4
pubchem
gtoplig
pubchem
|
peptide | Agonist | glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon | 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 | 53542 | |
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 | 53553 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7RKN | - | 3.6 | US28 | US28 | Unclassified | A (Rhodopsin) | strain AD169 | - | scFv16 | - |
Fractalkine
pubchem
|
peptide | Agonist | - | - | Tsutsumi N, Maeda S, Qu Q, Vogele M, Jude KM, Suomivuori CM, Panova O, Waghray D, Kato HE, Velasco A, Dror RO, Skiniotis G, Kobilka BK, Garcia KC | 10.1126/SCIADV.ABL5442 | 2022-01-26 | 53544 | |
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 | 53542 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7EVZ | - | 3.1 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
cenerimod
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | sphingosylphosphorylcholine, sphingosine 1-phosphate, dihydrosphingosine 1-phosphate | small-molecule | Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z | 10.1038/S41422-021-00566-X | 2021-09-29 | 53544 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7EW7 | 7EW7_refined | 3.3 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
SEW2871
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | sphingosylphosphorylcholine, sphingosine 1-phosphate, dihydrosphingosine 1-phosphate | small-molecule | Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z | 10.1038/S41422-021-00566-X | 2021-09-29 | 53544 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7F4F | - | 2.9 | MSHR | MC1 | Melanocortin | A (Rhodopsin) | Human | - | scFv16 | - |
CHEMBL407070
chembl_ligand
pubchem
pubchem
|
protein | Agonist | γ-MSH, ACTH, β-MSH, α-MSH | peptide | Ma S, Chen Y, Dai A, Yin W, Guo J, Yang D, Zhou F, Jiang Y, Wang MW, Xu HE | 10.1038/S41422-021-00557-Y | 2021-09-08 | 53542 | |
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, ACTH, β-MSH, α-MSH | peptide | Ma S, Chen Y, Dai A, Yin W, Guo J, Yang D, Zhou F, Jiang Y, Wang MW, Xu HE | 10.1038/S41422-021-00557-Y | 2021-09-08 | 53542 | |
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 | 15-deoxy-LXA4, annexin I, aspirin triggered lipoxin A4, LTC4, fMet-Leu-Phe, LXA4, aspirin-triggered resolvin D1, resolvin D1, serum amyloid A, LL-37, PrP106-126, LTD4, humanin | peptide | Zhuang Y, Wang L, Guo J, Sun D, Wang Y, Liu W, Xu HE, Zhang C | 10.1038/S41467-022-28586-0 | 2022-03-30 | 53544 | |
Gi/o | αi1 | Human | - | 61 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7T6V | - | 3.1 | FPR2 | FPR2/ALX | Formylpeptide | A (Rhodopsin) | Human | - | scFv16 | - |
synthetic peptide
|
peptide | Agonist | 15-deoxy-LXA4, annexin I, aspirin triggered lipoxin A4, LTC4, fMet-Leu-Phe, LXA4, aspirin-triggered resolvin D1, resolvin D1, serum amyloid A, LL-37, PrP106-126, LTD4, humanin | peptide | Zhuang Y, Wang L, Guo J, Sun D, Wang Y, Liu W, Xu HE, Zhang C | 10.1038/S41467-022-28586-0 | 2022-03-30 | 53544 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7VGX | 7VGX_refined | 3.2 | NPY1R | Y1 | Neuropeptide Y | A (Rhodopsin) | Human | - | scFv16 | - |
neuropeptide Y
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
pubchem
pubchem
pubchem
|
peptide | Agonist | peptide YY, pancreatic polypeptide, neuropeptide Y | peptide | Park C, Kim J, Ko SB, Choi YK, Jeong H, Woo H, Kang H, Bang I, Kim SA, Yoon TY, Seok C, Im W, Choi HJ | 10.1038/S41467-022-28510-6 | 2022-02-23 | 53544 | |
Gq/11 | αq | Human | Gamma subunit fused to alpha subunit | 55 | β1 | Human | - | - | Cryo-EM | 7RYC | - | 2.9 | OXYR | OT | Vasopressin and oxytocin | A (Rhodopsin) | Human | - | scFv16 | - |
oxytocin
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
|
peptide | Agonist | vasopressin, oxytocin | peptide | Meyerowitz JG, Robertson MJ, Barros-Alvarez X, Panova O, Nwokonko RM, Gao Y, Skiniotis G | 10.1038/S41594-022-00728-4 | 2022-03-09 | 53552 | |
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 | CCL13, CCL14, CCL15, CCL4, CCL3, CCL23, CCL7, CCL8, CCL16, CCL5 | 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 | 53544 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7VKT | 7VKT_refined | 2.9 | LT4R1 | BLT1 | Leukotriene | A (Rhodopsin) | Human | - | scFv16 | - |
LTB4
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | LTB4, 20-hydroxy-LTB4, 12R-HETE | small-molecule | Wang N, He X, Zhao J, Jiang H, Cheng X, Xia Y, Eric Xu H, He Y | 10.1038/S41467-022-28820-9 | 2022-03-09 | 53544 | |
Gi/o | αi1 | Mouse | - | 62 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7TD1 | - | 3.1 | LPAR1 | LPA1 | Lysophospholipid (LPA) | A (Rhodopsin) | Human | - | - | - |
lysophosphatidic acid
pubchem
|
small-molecule | Agonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY | 10.1038/S41467-022-28417-2 | 2022-02-09 | 53586 | |
Gi/o | αi1 | Mouse | - | 63 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7TD3 | - | 3.0 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | - | - |
sphingosine 1-phosphate
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | sphingosylphosphorylcholine, sphingosine 1-phosphate, dihydrosphingosine 1-phosphate | small-molecule | Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY | 10.1038/S41467-022-28417-2 | 2022-02-09 | 53586 | |
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 | 53544 | |
Gi/o | αi1 | Human | - | 62 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7VGZ | 7VGZ_refined | 3.3 | MTR1A | MT1 | Melatonin | A (Rhodopsin) | Human | - | scFv16 | - |
ramelteon
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | melatonin | small-molecule | Wang Q, Lu Q, Guo Q, Teng M, Gong Q, Li X, Du Y, Liu Z, Tao Y | 10.1038/S41467-022-28111-3 | 2022-03-02 | 53544 | |
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, amylin, adrenomedullin, calcitonin (salmon), 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 | 53542 | |
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, amylin, adrenomedullin, calcitonin (salmon), 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 | 53542 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7TYO | 7TYO_refined | 2.7 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - | Nanobody-35 | - |
Calcitonin human
pubchem
|
peptide | Agonist | calcitonin, amylin, adrenomedullin, calcitonin (salmon), 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 | 53542 | |
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, amylin, adrenomedullin, calcitonin (salmon), 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 | 53542 | |
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, amylin, adrenomedullin, calcitonin (salmon), 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 | 53542 | |
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 | 53559 | |
Gs | αs | Bovine | - | 57 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7FIM | - | 3.4 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
tirzepatide
pubchem
gtoplig
|
peptide | Agonist | glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, 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 | 53559 | |
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 | 53542 | |
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 | (-)-adrenaline, (-)-noradrenaline | 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 | 53550 | |
Gi/o | αo | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7EJA | 7EJA_refined | 3.6 | ADA2A | α2A | Adrenoceptors | A (Rhodopsin) | Human | - | scFv16 | - |
dexmedetomidine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | (-)-adrenaline, (-)-noradrenaline | small-molecule | 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 | 53550 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7WVU | 7WVU_refined | 3.3 | FPR1 | FPR1 | Formylpeptide | A (Rhodopsin) | Human | - | - | - |
FME-LEU-PHE
|
peptide | Agonist | cathepsin G, spinorphin, annexin I, fMet-Leu-Phe | 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 | 53544 | |
Gi/o | αi2 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7WVW | 7WVW_refined | 3.1 | FPR2 | FPR2/ALX | Formylpeptide | A (Rhodopsin) | Human | BRIL | - | - |
FME-TYR-PHE-ILE-ASN-ILE-LEU-THE-LEU
|
peptide | Agonist | 15-deoxy-LXA4, annexin I, aspirin triggered lipoxin A4, LTC4, fMet-Leu-Phe, LXA4, aspirin-triggered resolvin D1, resolvin D1, serum amyloid A, LL-37, PrP106-126, LTD4, humanin | peptide | Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B | 10.1038/S41467-022-29361-X | 2022-04-13 | 53545 | |
Gi/o | αi2 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7WVY | - | 3.0 | FPR2 | FPR2/ALX | Formylpeptide | A (Rhodopsin) | Human | BRIL | - | - |
Amyloid beta-Peptide (1-42)
pubchem
|
peptide | Agonist | 15-deoxy-LXA4, annexin I, aspirin triggered lipoxin A4, LTC4, fMet-Leu-Phe, LXA4, aspirin-triggered resolvin D1, resolvin D1, serum amyloid A, LL-37, PrP106-126, LTD4, humanin | peptide | Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B | 10.1038/S41467-022-29361-X | 2022-04-13 | 53545 | |
Gq/11 | αq | Human | - | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7WQ4 | 7WQ4_refined | 2.6 | GALR2 | GAL2 | Galanin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
galanin
gtoplig
chembl_ligand
gtoplig
pubchem
pubchem
pubchem
pubchem
pubchem
|
peptide | Agonist | galanin, spexin-1, galanin-like peptide | peptide | Duan J, Shen DD, Zhao T, Guo S, He X, Yin W, Xu P, Ji Y, Chen LN, Liu J, Zhang H, Liu Q, Shi Y, Cheng X, Jiang H, Eric Xu H, Zhang Y, Xie X, Jiang Y | 10.1038/S41467-022-29072-3 | 2022-04-20 | 53552 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7SCG | - | 3.0 | OPRM | μ | Opioid | A (Rhodopsin) | Mouse | - | scFv16 | - |
(2E)-N-[(2S)-2-(dimethylamino)-3-(4-hydroxyphenyl)propyl]-3-(naphthalen-1-yl)prop-2-enamide
pubchem
|
small-molecule | Agonist | - | - | Wang H, Hetzer F, Huang W, Qu Q, Meyerowitz J, Kaindl J, Hubner H, Skiniotis G, Kobilka BK, Gmeiner P | 10.1002/ANIE.202200269 | 2022-04-20 | 53544 | |
G12/13 | α13 | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7T6B | 7T6B_refined | 3.2 | S1PR2 | S1P2 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
sphingosine 1-phosphate
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | sphingosylphosphorylcholine, sphingosine 1-phosphate, dihydrosphingosine 1-phosphate | small-molecule | Chen H, Chen K, Huang W, Staudt LM, Cyster JG, Li X | 10.1126/SCIADV.ABN0067 | 2022-04-06 | 53557 | |
Gs | αs | Human | Engineered G alpha | 56 | β1 | Human | γ2 | Human | Cryo-EM | 7RA3 | - | 3.2 | GIPR | GIP | Glucagon | B1 (Secretin) | Human | - |
scFv16 Nanobody-35 |
- |
gastric inhibitory polypeptide (human) - Incretin
pubchem
|
peptide | Agonist | gastric inhibitory polypeptide | peptide | Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW | 10.1073/PNAS.2116506119 | 2022-04-13 | 53542 | |
Gi/o | αo | Human | Mini-Go | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7UM7 | 7UM7_refined | 2.8 | 5HT5A | 5-HT5A | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | scFv16 | - |
methylergonovine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL | 10.1038/S41594-022-00796-6 | 2022-07-20 | 53550 | |
Gs | αs | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7XTC | 7XTC_refined | 3.2 | 5HT7R | 5-HT7 | 5-Hydroxytryptamine | A (Rhodopsin) | Human | BRIL | Nanobody-35 | - |
5-CT
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE | 10.1016/J.MOLCEL.2022.05.031 | 2022-07-27 | 53542 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7W0M | 7W0M_refined | 3.7 | APJ | apelin | Apelin | A (Rhodopsin) | Human | BRIL | scFv16 | - |
(1R,2S)-N-[4-(2,6-dimethoxyphenyl)-5-(6-methylpyridin-2-yl)-1,2,4-triazol-3-yl]-1-(5-methylpyrimidin-2-yl)-1-oxidanyl-propane-2-sulfonamide
pubchem
|
small-molecule | Agonist | [Pyr1]apelin-13, Elabela/Toddler-32, Elabela/Toddler-21, apelin receptor early endogenous ligand, apelin-36, Elabela/Toddler-11, apelin-13, apelin-17 | 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 | 53544 | |
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 | [Pyr1]apelin-13, Elabela/Toddler-32, Elabela/Toddler-21, apelin receptor early endogenous ligand, apelin-36, Elabela/Toddler-11, apelin-13, apelin-17 | 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 | 53544 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7XOU | - | 3.2 | CCKAR | CCK1 | Cholecystokinin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
CCK-8
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
peptide | Agonist | CCK-8, CCK-33, CCK-4, CCK-39, gastrin-17, CCK-58, desulfated cholecystokinin-8 | peptide | Ding Y, Zhang H, Liao YY, Chen LN, Ji SY, Qin J, Mao C, Shen DD, Lin L, Wang H, Zhang Y, Li XM | 10.1038/S41421-022-00420-3 | 2022-07-20 | 53542 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7XOV | 7XOV_refined | 3.0 | CCKAR | CCK1 | Cholecystokinin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
SR146131
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | CCK-8, CCK-33, CCK-4, CCK-39, gastrin-17, CCK-58, desulfated cholecystokinin-8 | peptide | Ding Y, Zhang H, Liao YY, Chen LN, Ji SY, Qin J, Mao C, Shen DD, Lin L, Wang H, Zhang Y, Li XM | 10.1038/S41421-022-00420-3 | 2022-07-20 | 53542 | |
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, CCK-33, CCK-4, desulfated gastrin-17, gastrin-34, CCK-39, gastrin-17, gastrin-71, desulfated gastrin-34, CCK-58, desulfated cholecystokinin-8, gastrin-14, desulfated gastrin-71, desulfated gastrin-14 | 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 | 53552 | |
Gi/o | αi1 | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7WJ5 | - | 3.7 | SSR2 | SST2 | Somatostatin | A (Rhodopsin) | Human | BRIL | scFv16 | - |
SOMATOSTATIN
chembl_ligand
pubchem
|
protein | Agonist | SRIF-14, cortistatin-14, SRIF-28, CST-17 | peptide | Heo Y, Yoon E, Jeon YE, Yun JH, Ishimoto N, Woo H, Park SY, Song JJ, Lee W | 10.7554/ELIFE.76823 | 2022-07-13 | 53544 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7XTQ | 7XTQ_refined | 3.2 | GPBAR | GPBA | Bile acid | A (Rhodopsin) | Human | - | Nanobody-35 | - |
CHEMBL2181246
chembl_ligand
pubchem
|
small-molecule | Agonist | lithocholic acid, chenodeoxycholic acid, deoxycholic acid, cholic acid | small-molecule | Ma L, Yang F, Wu X, Mao C, Guo L, Miao T, Zang SK, Jiang X, Shen DD, Wei T, Zhou H, Wei Q, Li S, Shu Q, Feng S, Jiang C, Chu B, Du L, Sun JP, Yu X, Zhang Y, Zhang P | 10.1073/PNAS.2117054119 | 2022-07-06 | 53542 | |
Gi/o | αi1 | Human | - | 62 | β1 | Mouse | γ2 | Mouse | Cryo-EM | 7Y12 | - | 3.1 | MRGRD | MRGPRD | A orphans | A (Rhodopsin) | Human | BRIL | scFv16 | - |
β-alanine
pubchem
gtoplig
chembl_ligand
drugbank
pubchem
|
small-molecule | Agonist | β-alanine | small-molecule | Suzuki S, Iida M, Hiroaki Y, Tanaka K, Kawamoto A, Kato T, Oshima A | 10.1038/S42003-022-03668-3 | 2022-07-20 | 53544 | |
Gi/o | αi1 | Human | - | 62 | β1 | Mouse | γ2 | Mouse | Cryo-EM | 7Y15 | 7Y15_refined | 2.9 | MRGRD | MRGPRD | A orphans | A (Rhodopsin) | Human | BRIL | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | β-alanine | small-molecule | Suzuki S, Iida M, Hiroaki Y, Tanaka K, Kawamoto A, Kato T, Oshima A | 10.1038/S42003-022-03668-3 | 2022-07-20 | 53544 | |
Gs | αs | Bovine | - | 51 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 8DCS | - | 2.5 | ADRB1 | β1 | Adrenoceptors | A (Rhodopsin) | Wild turkey | T4-Lysozyme | Nanobody-35 | - |
4-{[(2S)-3-(tert-butylamino)-2-hydroxypropyl]oxy}-3H-indole-2-carbonitrile
pubchem
|
small-molecule | Agonist | - | - | Su M, Paknejad N, Zhu L, Wang J, Do HN, Miao Y, Liu W, Hite RK, Huang XY | 10.1038/S41467-022-31823-1 | 2022-07-27 | 53559 | |
Gq/11 | αq | Human | Gi2-mini-Gq chimera | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8DPG | - | 3.6 | 5HT2C | 5-HT2C | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | scFv16 | - |
psilocin
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Gumpper RH, Fay JF, Roth BL | 10.1016/J.CELREP.2022.111211 | 2022-08-24 | 53552 | |
Gq/11 | αq | Human | Gi2-mini-Gq chimera | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8DPI | - | 3.4 | 5HT2C | 5-HT2C | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | scFv16 | - |
lorcaserin
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Gumpper RH, Fay JF, Roth BL | 10.1016/J.CELREP.2022.111211 | 2022-08-24 | 53552 | |
Gi/o | αi1 | Human | - | 63 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7XAU | - | 3.0 | SSR2 | SST2 | Somatostatin | A (Rhodopsin) | Human | - | scFv16 | - |
Octreotide
|
peptide | Agonist | SRIF-14, cortistatin-14, SRIF-28, CST-17 | peptide | Bo Q, Yang F, Li Y, Meng X, Zhang H, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C | 10.1038/S41421-022-00405-2 | 2022-08-31 | 53544 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7XMR | - | 3.1 | SSR2 | SST2 | Somatostatin | A (Rhodopsin) | Human | - | - | - |
SOMATOSTATIN
chembl_ligand
pubchem
|