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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 | 3DQB | - | 3.2 | OPSD | Rhodopsin | Opsins | A (Rhodopsin) | Bovine | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | None | 10.1038/NATURE07330 | 2008-09-23 | 53851 | |
Gi/o | αt1 | Bovine | Only H5 | 3 | - | - | - | - | X-ray | 3PQR | 3PQR_refined | 2.9 | OPSD | Rhodopsin | Opsins | A (Rhodopsin) | Bovine | - | - | - |
Retinal (all-trans)
pubchem
|
small-molecule | Agonist | - | - | - | - | 2011-03-09 | 53851 | |
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 | 53851 | |
Gs | αs | Bovine | - | 89 | β1 | Rat | γ2 | Bovine | X-ray | 3SN6 | - | 3.2 | ADRB2 | β2 | Adrenoceptors | A (Rhodopsin) | Human | T4-Lysozyme | Antibody | - |
CHEMBL1615159
chembl_ligand
pubchem
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline | small-molecule | Rasmussen SG, DeVree BT, Zou Y, Kruse AC, Chung KY, Kobilka TS, Thian FS, Chae PS, Pardon E, Calinski D, Mathiesen JM, Shah ST, Lyons JA, Caffrey M, Gellman SH, Steyaert J, Skiniotis G, Weis WI, Sunahara RK, Kobilka BK | 10.1038/NATURE10361 | 2011-07-20 | 53756 | |
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 | 53851 | |
Gi/o | αo | Human | Mini-Go | 51 | - | - | - | - | X-ray | 6FUF | - | 3.1 | OPSD | Rhodopsin | Opsins | A (Rhodopsin) | Bovine | - | - | - |
Retinal (all-trans)
pubchem
|
small-molecule | Agonist | - | - | Tsai CJ, Pamula F, Nehme R, Muhle J, Weinert T, Flock T, Nogly P, Edwards PC, Carpenter B, Gruhl T, Ma P, Deupi X, Standfuss J, Tate CG, Schertler GFX | 10.1126/SCIADV.AAT7052 | 2018-10-03 | 53747 | |
Gs | αs | Human | - | 49 | β1 | Human | γ2 | Human | Cryo-EM | 6P9Y | - | 3.0 | PACR | PAC1 | VIP and PACAP | B1 (Secretin) | Human | - | Nanobody-35 | - |
[Ac-His1]PACAP-27
gtoplig
chembl_ligand
pubchem
|
peptide | Agonist | VIP, PHI, PHM, PHV, PACAP-27, PACAP-38 | peptide | Liang YL, Belousoff MJ, Zhao P, Koole C, Fletcher MM, Truong TT, Julita V, Christopoulos G, Xu HE, Zhang Y, Khoshouei M, Christopoulos A, Danev R, Sexton PM, Wootten D | 10.1016/J.MOLCEL.2020.01.012 | 2020-02-05 | 53739 | |
Gi/o | αt2 | Bovine | Only H5 | 3 | - | - | - | - | X-ray | 6PH7 | - | 2.9 | OPSD | Rhodopsin | Opsins | A (Rhodopsin) | Bovine | - | - | - |
Nerol
pubchem
|
small-molecule | unknown | - | - | - | - | 2020-07-01 | 53871 | |
Gs | αs | Human | - | 50 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7BZ2 | 7BZ2_refined | 3.8 | ADRB2 | β2 | Adrenoceptors | A (Rhodopsin) | Human | - | Nanobody-35 | - |
ARFORMOTEROL
chembl_ligand
chembl_ligand
chembl_ligand
chembl_ligand
pubchem
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline | small-molecule | Zhang Y, Yang F, Ling S, Lv P, Zhou Y, Fang W, Sun W, Zhang L, Shi P, Tian C | 10.1038/S41421-020-0176-9 | 2020-08-05 | 53739 | |
Gq/11 | αq | Human | Gq-Gi2-Gs chimera | 57 | β1 | Human | γ2 | Human | Cryo-EM | 6WHA | - | 3.4 | 5HT2A | 5-HT2A | 5-Hydroxytryptamine | A (Rhodopsin) | Human | BRIL | scFv16 | - |
CHEMBL5184791
chembl_ligand
pubchem
|
small-molecule | Agonist | tryptamine, 5-hydroxytryptamine | small-molecule | Kim K, Che T, Panova O, DiBerto JF, Lyu J, Krumm BE, Wacker D, Robertson MJ, Seven AB, Nichols DE, Shoichet BK, Skiniotis G, Roth BL | 10.1016/J.CELL.2020.08.024 | 2020-09-23 | 53749 | |
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 | 53747 | |
Gs | αs | Human | Engineered G alpha | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7LJD | - | 3.2 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
dopamine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
mevidalen pubchem gtoplig chembl_ligand |
small-molecule small-molecule |
Agonist PAM |
L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | - | - | 2021-03-03 | 53739 | |
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 | 53741 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7EO2 | 7EO2_refined | 2.9 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
(S)-FTY720-phosphate
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | Xu Z, Ikuta T, Kawakami K, Kise R, Qian Y, Xia R, Sun MX, Zhang A, Guo C, Cai XH, Huang Z, Inoue A, He Y | 10.1038/S41589-021-00930-3 | 2022-01-05 | 53741 | |
Gi/o | αi1 | Human | - | 61 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7T6T | 7T6T_refined | 3.2 | FPR1 | FPR1 | Formylpeptide | A (Rhodopsin) | Human | - | - | - |
synthetic peptide
|
peptide | Agonist | fMet-Leu-Phe, cathepsin G, annexin I, spinorphin | peptide | Zhuang Y, Wang L, Guo J, Sun D, Wang Y, Liu W, Xu HE, Zhang C | 10.1038/S41467-022-28586-0 | 2022-03-30 | 53741 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7TYF | - | 2.2 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - |
Nanobody-35 RAMP1 |
- |
amylin peptide
|
peptide | Agonist | adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP | peptide | Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM | 10.1126/SCIENCE.ABM9609 | 2022-03-23 | 53739 | |
Gs | αs | Human | - | 53 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7VBH | 7VBH_refined | 3.0 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
Peptide 20
|
peptide | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW | 10.1038/S41467-022-28683-0 | 2022-04-06 | 53739 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7X2D | 7X2D_refined | 3.3 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
TAVAPADON
chembl_ligand
pubchem
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | - | - | 2022-06-15 | 53739 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7XOV | - | 3.0 | CCKAR | CCK1 | Cholecystokinin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
SR146131
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | desulfated cholecystokinin-8, CCK-58, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8 | peptide | Ding Y, Zhang H, Liao YY, Chen LN, Ji SY, Qin J, Mao C, Shen DD, Lin L, Wang H, Zhang Y, Li XM | 10.1038/S41421-022-00420-3 | 2022-07-20 | 53739 | |
Gq/11 | αq | Human | Gi2-mini-Gq chimera | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8DPI | - | 3.4 | 5HT2C | 5-HT2C | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | scFv16 | - |
lorcaserin
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Gumpper RH, Fay JF, Roth BL | 10.1016/J.CELREP.2022.111211 | 2022-08-24 | 53749 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7XZ5 | - | 3.1 | GP119 | GPR119 | GPR18, GPR55 and GPR119 | A (Rhodopsin) | Human | BRIL | Nanobody-35 | - |
(4R,7R,18E)-4,7-dihydroxy-N,N,N-trimethyl-10-oxo-3,5,9-trioxa-4-phosphaheptacos-18-en-1-aminium 4-oxide
pubchem
|
small-molecule | Agonist | N-oleoylethanolamide, anandamide, N-palmitoylethanolamine, SEA | small-molecule | Xu P, Huang S, Guo S, Yun Y, Cheng X, He X, Cai P, Lan Y, Zhou H, Jiang H, Jiang Y, Xie X, Xu HE | 10.1038/S41594-022-00816-5 | 2022-08-24 | 53739 | |
Gs | αs | Human | Mini-Gs | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7WXW | - | 2.8 | AGRF1 | ADGRF1 | ADGRF | B2 (Adhesion) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y | 10.1038/S41467-022-33173-4 | 2022-09-28 | 53739 | |
Gi/o | αgust | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7XP6 | - | 3.0 | T2R46 | TAS2R46 | Taste 2 | T (Taste 2) | Human | - | Nanobody-35 | Endoglucanase H |
strychnine
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
gtoplig
|
small-molecule | Agonist | - | - | Xu W, Wu L, Liu S, Liu X, Cao X, Zhou C, Zhang J, Fu Y, Guo Y, Wu Y, Tan Q, Wang L, Liu J, Jiang L, Fan Z, Pei Y, Yu J, Cheng J, Zhao S, Hao X, Liu ZJ, Hua T | 10.1126/SCIENCE.ABO1633 | 2022-10-12 | 53746 | |
Gq/11 | αq | Human | Mini-Gq | 56 | β1 | Human | γ2 | Human | Cryo-EM | 8E9Y | - | 2.8 | ACM3 | M3 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | scFv16 | - |
Clozapine N-oxide
pubchem
|
small-molecule | Agonist | acetylcholine | small-molecule | Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL | 10.1038/S41586-022-05489-0 | 2022-11-30 | 53749 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7YON | 7YON_refined | 3.0 | NPY2R | Y2 | Neuropeptide Y | A (Rhodopsin) | Human | - | scFv16 | - |
Peptide YY
|
peptide | Agonist | pancreatic polypeptide, neuropeptide Y-(3-36), PYY-(3-36), neuropeptide Y, peptide YY | peptide | Kang H, Park C, Choi YK, Bae J, Kwon S, Kim J, Choi C, Seok C, Im W, Choi HJ | 10.1016/J.STR.2022.11.010 | 2023-03-22 | 53741 | |
Gi/o | αo | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7T96 | 7T96_refined | 3.2 | ACM2 | M2 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | scFv16 | - |
acetylcholine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
LY2119620 pubchem gtoplig chembl_ligand |
small-molecule small-molecule |
Agonist PAM |
acetylcholine | small-molecule | - | - | 2023-01-25 | 53747 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7Y64 | - | 2.9 | C5AR1 | C5a1 | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
C5a anaphylatoxin
|
peptide | Agonist | ribosomal protein S19, C5a, C5a des-Arg, C3a | peptide | Feng Y, Zhao C, Deng Y, Wang H, Ma L, Liu S, Tian X, Wang B, Bin Y, Chen P, Yan W, Fu P, Shao Z | 10.1038/S41422-023-00779-2 | 2023-03-01 | 53741 | |
Gs | αs | Human | Mini-Gs | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8IRR | - | 3.2 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
rotigotine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | Xu P, Huang S, Krumm BE, Zhuang Y, Mao C, Zhang Y, Wang Y, Huang XP, Liu YF, He X, Li H, Yin W, Jiang Y, Zhang Y, Roth BL, Xu HE | 10.1038/S41422-023-00808-0 | 2023-06-21 | 53739 | |
Gi/o | αi1 | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8GDC | 8GDC_refined | 3.5 | PE2R3 | EP3 | Prostanoid | A (Rhodopsin) | Human | - | - | - |
PGE2
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
|
small-molecule | Agonist | thromboxane A2, PGF2α, PGI2, PGD2, PGE1, PGE2 | small-molecule | Huang SM, Xiong MY, Liu L, Mu J, Wang MW, Jia YL, Cai K, Tie L, Zhang C, Cao S, Wen X, Wang JL, Guo SC, Li Y, Qu CX, He QT, Cai BY, Xue C, Gan S, Xie Y, Cong X, Yang Z, Kong W, Li S, Li Z, Xiao P, Yang F, Yu X, Guan YF, Zhang X, Liu Z, Yang BX, Du Y, Sun JP | 10.1073/PNAS.2216329120 | 2024-01-10 | 53741 | |
Gq/11 | αq | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8IA7 | 8IA7_refined | 3.1 | GASR | CCK2 | Cholecystokinin | A (Rhodopsin) | Human | - | - | - |
CHEMBL216166
chembl_ligand
pubchem
|
protein | Agonist | desulfated gastrin-14, desulfated cholecystokinin-8, gastrin-34, gastrin-14, CCK-58, desulfated gastrin-17, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8, desulfated gastrin-34, gastrin-71, desulfated gastrin-71 | peptide | Ding Y, Zhang H, Liao YY, Chen LN, Ji SY, Qin J, Mao C, Shen DD, Lin L, Wang H, Zhang Y, Li XM | 10.1038/S41421-022-00420-3 | 2023-12-06 | 53749 | |
Gs | αs | Human | - | 58 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8JIT | - | 2.9 | GLR | glucagon | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
MEDI0382
|
peptide | Agonist | glucagon | peptide | Li Y, Zhou Q, Dai A, Zhao F, Chang R, Ying T, Wu B, Yang D, Wang MW, Cong Z | 10.1073/PNAS.2303696120 | 2023-09-06 | 53739 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8WC5 | - | 3.3 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Mouse | - | scFv16 | - |
Tetramethylammonium
chembl_ligand
pubchem
|
small-molecule | Agonist | β-phenylethylamine, 3-iodothyronamine, tyramine | small-molecule | Shang P, Rong N, Jiang JJ, Cheng J, Zhang MH, Kang D, Qi L, Guo L, Yang GM, Liu Q, Zhou Z, Li XB, Zhu KK, Meng QB, Han X, Yan W, Kong Y, Yang L, Wang X, Lei D, Feng X, Liu X, Yu X, Wang Y, Li Q, Shao ZH, Yang F, Sun JP | 10.1016/J.CELL.2023.10.014 | 2023-12-27 | 53739 | |
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 | 53739 | |
Gs | αs | Human | - | 48 | β1 | Human | γ2 | Human | Cryo-EM | 6UUN | 6UUN_refined | 3.0 | CALRL | calcitonin-like | Calcitonin | B1 (Secretin) | Human | - |
Nanobody-35 RAMP2 |
- |
Adrenomedullin
pubchem
|
peptide | Agonist | - | - | Liang YL, Belousoff MJ, Fletcher MM, Zhang X, Khoshouei M, Deganutti G, Koole C, Furness SGB, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Danev R, Wootten D, Sexton PM | 10.1021/ACSPTSCI.9B00080 | 2020-03-25 | 53739 | |
Gi/o | αi1 | Human | - | 65 | β1 | Human | γ2 | Human | Cryo-EM | 6LFM | 6LFM_refined | 3.5 | CXCR2 | CXCR2 | Chemokine | A (Rhodopsin) | Human | - | scFv16 | - |
Interleukin-8
pubchem
|
protein | Agonist | CXCL8, CXCL1, CXCL5, CXCL2, CXCL7, CXCL6, CXCL3 | peptide | Liu K, Wu L, Yuan S, Wu M, Xu Y, Sun Q, Li S, Zhao S, Hua T, Liu ZJ | 10.1038/S41586-020-2492-5 | 2020-09-02 | 53741 | |
Gs | αs | Bovine | - | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7FIH | - | 3.2 | LSHR | LH | Glycoprotein hormone | A (Rhodopsin) | Human | - | - | - |
Glycoprotein alpha
gtoplig
Choriogonadotropin beta gtoplig 5-Amino-N-(1,1-dimethylethyl)-2-(methylthio)-4-[3-[[2-(4-morpholinyl)acetyl]amino]phenyl]thieno[2,3-d]pyrimidine-6-carboxamide pubchem |
protein protein small-molecule |
Agonist | hCG, LH | peptide | Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE | 10.1038/S41586-021-03924-2 | 2021-09-29 | 53756 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7U2L | - | 3.2 | OPRM | μ | Opioid | A (Rhodopsin) | Mouse | - | scFv16 | - |
N-(5-carbamimidamidopentyl)-N-[1-(2-phenylethyl)piperidin-4-yl]propanamide
|
small-molecule | Agonist | - | - | Faouzi A, Wang H, Zaidi SA, DiBerto JF, Che T, Qu Q, Robertson MJ, Madasu MK, El Daibani A, Varga BR, Zhang T, Ruiz C, Liu S, Xu J, Appourchaux K, Slocum ST, Eans SO, Cameron MD, Al-Hasani R, Pan YX, Roth BL, McLaughlin JP, Skiniotis G, Katritch V, Kobilka BK, Majumdar S | 10.1038/S41586-022-05588-Y | 2022-05-04 | 53741 | |
Gs | αs | Human | - | 59 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7XJI | - | 3.9 | ADRB3 | β3 | Adrenoceptors | A (Rhodopsin) | Dog | - | Nanobody-35 | - |
3-[3-[2-[[(2~{S})-2-(3-chlorophenyl)-2-oxidanyl-ethyl]amino]ethylamino]phenyl]benzoic acid
pubchem
|
small-molecule | Agonist | - | - | Nureki I, Kobayashi K, Tanaka T, Demura K, Inoue A, Shihoya W, Nureki O | 10.1016/J.BBRC.2022.04.065 | 2022-05-04 | 53739 | |
Gq/11 | αq | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7XJL | 7XJL_refined | 3.5 | GALR2 | GAL2 | Galanin | A (Rhodopsin) | Human | - | scFv16 | - |
Spexin
pubchem
|
small-molecule | Agonist | galanin-like peptide, spexin-1, galanin | peptide | Jiang W, Zheng S | 10.1073/PNAS.2121465119 | 2022-06-29 | 53749 | |
Gq/11 | αq | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7XBD | 7XBD_refined | 3.1 | GALR2 | GAL2 | Galanin | A (Rhodopsin) | Human | - | scFv16 | - |
Galanin, Human
pubchem
|
peptide | Agonist | galanin-like peptide, spexin-1, galanin | peptide | Heo Y, Ishimoto N, Jeon YE, Yun JH, Ohki M, Anraku Y, Sasaki M, Kita S, Fukuhara H, Ikuta T, Kawakami K, Inoue A, Maenaka K, Tame JRH, Lee W, Park SY | 10.1371/JOURNAL.PBIO.3001714 | 2022-07-13 | 53749 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7XMT | 7XMT_refined | 2.8 | SSR4 | SST4 | Somatostatin | A (Rhodopsin) | Human | - | scFv16 | - |
J-2156
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | Zhao W, Han S, Qiu N, Feng W, Lu M, Zhang W, Wang M, Zhou Q, Chen S, Xu W, Du J, Chu X, Yi C, Dai A, Hu L, Shen MY, Sun Y, Zhang Q, Ma Y, Zhong W, Yang D, Wang MW, Wu B, Zhao Q | 10.1038/S41422-022-00679-X | 2022-08-03 | 53741 | |
Gs | αs | Human | - | 57 | β1 | Human | γ2 | Human | Cryo-EM | 7XKF | - | 2.4 | AGRG2 | ADGRG2 | ADGRG | B2 (Adhesion) | Mouse | - | Nanobody-35 | - |
PRASTERONE
chembl_ligand
pubchem
|
small-molecule | Agonist | - | - | Lin H, Xiao P, Bu RQ, Guo S, Yang Z, Yuan D, Zhu ZL, Zhang CX, He QT, Zhang C, Ping YQ, Zhao RJ, Ma CS, Liu CH, Zhang XN, Jiang D, Huang S, Xi YT, Zhang DL, Xue CY, Yang BS, Li JY, Lin HC, Zeng XH, Zhao H, Xu WM, Yi F, Liu Z, Sun JP, Yu X | 10.1038/S41589-022-01084-6 | 2022-08-10 | 53739 | |
Gq/11 | αq | Human | Gi2-mini-Gq chimera | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7SRR | - | 2.9 | 5HT2B | 5-HT2B | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | scFv16 | - |
Lysergide
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Cao C, Barros-Alvarez X, Zhang S, Kim K, Damgen MA, Panova O, Suomivuori CM, Fay JF, Zhong X, Krumm BE, Gumpper RH, Seven AB, Robertson MJ, Krogan NJ, Huttenhain R, Nichols DE, Dror RO, Skiniotis G, Roth BL | 10.1016/J.NEURON.2022.08.006 | 2022-09-21 | 53749 | |
Gi/o | αo | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7W6P | - | 3.5 | ADA2A | α2A | Adrenoceptors | A (Rhodopsin) | Human | - | scFv16 | - |
N-pyridin-4-ylisoquinolin-4-amine
pubchem
|
small-molecule | Agonist | (-)-adrenaline, (-)-noradrenaline | small-molecule | Fink EA, Xu J, Hubner H, Braz JM, Seemann P, Avet C, Craik V, Weikert D, Schmidt MF, Webb CM, Tolmachova NA, Moroz YS, Huang XP, Kalyanaraman C, Gahbauer S, Chen G, Liu Z, Jacobson MP, Irwin JJ, Bouvier M, Du Y, Shoichet BK, Basbaum AI, Gmeiner P | 10.1126/SCIENCE.ABN7065 | 2022-09-28 | 53747 | |
G12/13 | α12 | Human | Mini-G12 | 55 | β1 | Human | γ2 | Human | Cryo-EM | 7WZ7 | - | 2.8 | AGRF1 | ADGRF1 | ADGRF | B2 (Adhesion) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y | 10.1038/S41467-022-33173-4 | 2022-09-28 | 53753 | |
Gi/o | αi1 | Human | - | 63 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7YU8 | - | 4.5 | LPAR1 | LPA1 | Lysophospholipid (LPA) | A (Rhodopsin) | Human | - | scFv16 | - |
[(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate
pubchem
|
small-molecule | Agonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O | 10.1038/S41467-022-33121-2 | 2022-10-05 | 53741 | |
Gs | αs | Bovine | - | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8HAF | - | 3.3 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
PTHrP-(1-36)
pubchem
gtoplig
|
peptide | Agonist | TIP39, PTHrP-(1-36), PTHrP, PTH | peptide | Zhao LH, Yuan QN, Dai AT, He XH, Chen CW, Zhang C, Xu YW, Zhou Y, Wang MW, Yang DH, Xu HE | 10.1038/S41401-022-01032-Z | 2022-12-21 | 53756 | |
Gs | αs | Human | Mini-Gs | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8HJ2 | 8HJ2_refined | 3.8 | GPR21 | GPR21 | A orphans | A (Rhodopsin) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Lin X, Chen B, Wu Y, Han Y, Qi A, Wang J, Yang Z, Wei X, Zhao T, Wu L, Xie X, Sun J, Zheng J, Zhao S, Xu F | 10.1038/S41467-023-35882-W | 2023-03-15 | 53739 | |
Gs | αs | Human | Gs fused to receptor | 57 | β1 | Human | γ2 | Human | Cryo-EM | 7TMW | - | 3.2 | RXFP1 | RXFP1 | Relaxin family peptide | A (Rhodopsin) | Human | - | Nanobody-35 | - |
H2 relaxin
pubchem
|
small-molecule | Agonist | relaxin, relaxin-1, relaxin-3 | peptide | - | - | 2023-02-15 | 53739 | |
Gi/o | αgust | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8DZR | - | 2.6 | OPRK | κ | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
CHEMBL277863
chembl_ligand
pubchem
|
small-molecule | Agonist | [Leu]enkephalin, β-neoendorphin, β-endorphin, dynorphin A, [Met]enkephalin, α-neoendorphin, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13), big dynorphin | peptide | Han J, Zhang J, Nazarova AL, Bernhard SM, Krumm BE, Zhao L, Lam JH, Rangari VA, Majumdar S, Nichols DE, Katritch V, Yuan P, Fay JF, Che T | 10.1038/S41586-023-06030-7 | 2023-05-03 | 53746 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8GUT | 8GUT_refined | 3.0 | CNR2 | CB2 | Cannabinoid | A (Rhodopsin) | Human | - | scFv16 | - |
1-[[4-[5-Fluoro-6-[(oxan-4-ylamino)methyl]pyridin-2-yl]phenyl]methyl]-3-(2-methylpropyl)imidazolidine-2,4-dione
pubchem
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | Li X, Chang H, Bouma J, de Paus LV, Mukhopadhyay P, Paloczi J, Mustafa M, van der Horst C, Kumar SS, Wu L, Yu Y, van den Berg RJBHN, Janssen APA, Lichtman A, Liu ZJ, Pacher P, van der Stelt M, Heitman LH, Hua T | 10.1038/S41467-023-37112-9 | 2023-05-10 | 53741 | |
G12/13 | α13 | Human | Gi2-mini-G13 chimera | 57 | β1 | Human | γ2 | Human | Cryo-EM | 7YDH | - | 3.1 | AGRE5 | ADGRE5 | ADGRE | B2 (Adhesion) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Wang N, Qian Y, Xia R, Zhu X, Xiong Y, Zhang A, Guo C, He Y | 10.1016/J.CHEMBIOL.2023.08.003 | 2023-07-12 | 53754 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8H4I | - | 3.1 | FFAR4 | FFA4 | Free fatty acid | A (Rhodopsin) | Human | - | Nanobody-35 | - |
docosahexaenoic acid
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
pubchem
|
small-molecule | Agonist | myristic acid, linoleic acid, α-linolenic acid, oleic acid | small-molecule | Yin H, Inoue A, Ma Z, Zhu X, Xia R, Xu Z, Wang N, Duan Y, Zhang A, Guo C, He Y | 10.1038/S41422-023-00835-X | 2023-06-21 | 53739 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8J1A | - | 3.2 | GPR84 | GPR84 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Liu H, Zhang Q, He X, Jiang M, Wang S, Yan X, Cheng X, Liu Y, Nan FJ, Xu HE, Xie X, Yin W | 10.1038/S41467-023-38985-6 | 2023-06-21 | 53741 | |
Gi/o | αi1 | Human | - | 62 | β1 | Mouse | γ2 | Mouse | Cryo-EM | 8IHI | - | 3.1 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | BRIL | scFv16 | - |
(5S)-5-methyl-4-oxo-5-phenylfuran-2-carboxylic acid
pubchem
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | Suzuki S, Tanaka K, Nishikawa K, Suzuki H, Oshima A, Fujiyoshi Y | 10.1038/S41467-023-41650-7 | 2023-08-30 | 53741 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 8JII | - | 3.2 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | - | scFv16 | - |
nicotinic acid
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
pubchem
compound 9n [PMID: 18752940] pubchem gtoplig chembl_ligand |
small-molecule small-molecule |
Agonist PAM |
β-D-hydroxybutyric acid, butyric acid | small-molecule | Zhao C, Wang H, Liu Y, Cheng L, Wang B, Tian X, Fu H, Wu C, Li Z, Shen C, Yu J, Yang S, Hu H, Fu P, Ma L, Wang C, Yan W, Shao Z | 10.1016/J.MOLCEL.2023.07.030 | 2023-09-06 | 53741 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8KH5 | - | 2.8 | GP174 | GPR174 | A orphans | A (Rhodopsin) | Human | - | Nanobody-35 | - |
Lysophosphotidylserine
pubchem
|
small-molecule | Agonist | lysophosphatidylserine | small-molecule | Nie Y, Qiu Z, Chen S, Chen Z, Song X, Ma Y, Huang N, Cyster JG, Zheng S | 10.1038/S41467-023-41654-3 | 2023-10-18 | 53739 | |
Gs | αs | Human | - | 47 | β1 | Human | γ2 | Human | Cryo-EM | 5UZ7 | - | 4.1 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - | - | - |
calcitonin (salmon synthetic)
pubchem
|
small-molecule | Agonist | adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP | peptide | Liang YL, Khoshouei M, Radjainia M, Zhang Y, Glukhova A, Tarrasch J, Thal DM, Furness SGB, Christopoulos G, Coudrat T, Danev R, Baumeister W, Miller LJ, Christopoulos A, Kobilka BK, Wootten D, Skiniotis G, Sexton PM | 10.1038/NATURE22327 | 2017-05-03 | 53739 | |
Gs | αs | Human | - | 49 | β1 | Human | γ2 | Human | Cryo-EM | 6ORV | 6ORV_refined | 3.0 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
CHEMBL3950796
chembl_ligand
pubchem
|
small-molecule | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Zhao P, Liang YL, Belousoff MJ, Deganutti G, Fletcher MM, Willard FS, Bell MG, Christe ME, Sloop KW, Inoue A, Truong TT, Clydesdale L, Furness SGB, Christopoulos A, Wang MW, Miller LJ, Reynolds CA, Danev R, Sexton PM, Wootten D | 10.1038/s41586-019-1902-z | 2020-01-08 | 53739 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7D7M | 7D7M_refined | 3.3 | PE2R4 | EP4 | Prostanoid | A (Rhodopsin) | Human | - | Nanobody-35 | - |
PGE2
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
|
small-molecule | Agonist | thromboxane A2, PGF2α, PGI2, PGD2, PGE1, PGE2 | small-molecule | Nojima S, Fujita Y, Kimura KT, Nomura N, Suno R, Morimoto K, Yamamoto M, Noda T, Iwata S, Shigematsu H, Kobayashi T | 10.1016/J.STR.2020.11.007 | 2020-11-18 | 53739 | |
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 | 53741 | |
Gq/11 | αq | Human | Gq-Gi1 chimera | 61 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7EIB | - | 3.0 | BKRB1 | B1 | Bradykinin | A (Rhodopsin) | Human | - | - | - |
[des-Arg10]kallidin
pubchem
gtoplig
chembl_ligand
gtoplig
|
peptide | Agonist | [des-Arg10]kallidin, Lys-[Hyp3]-bradykinin, kallidin, [des-Arg9]bradykinin, [Hyp3]bradykinin, T-kinin, bradykinin | peptide | Yin YL, Ye C, Zhou F, Wang J, Yang D, Yin W, Wang MW, Xu HE, Jiang Y | 10.1038/S41594-021-00645-Y | 2021-10-13 | 53749 | |
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 | 53741 | |
Gi/o | αi3 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7T10 | - | 2.5 | SSR2 | SST2 | Somatostatin | A (Rhodopsin) | Human | - | scFv16 | - |
SOMATOSTATIN
chembl_ligand
pubchem
|
protein | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | Robertson MJ, Meyerowitz JG, Panova O, Borrelli K, Skiniotis G | 10.1038/S41594-022-00727-5 | 2022-03-09 | 53743 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7TZF | - | 2.4 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - |
Nanobody-35 RAMP3 |
- |
amylin peptide
|
peptide | Agonist | adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP | peptide | Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM | 10.1126/SCIENCE.ABM9609 | 2022-03-23 | 53739 | |
Gq/11 | αq | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7W55 | - | 2.8 | NMUR2 | NMU2 | Neuromedin U | A (Rhodopsin) | Human | - | scFv16 | - |
Neuromedin U-25 (human)
pubchem
|
peptide | Agonist | neuromedin U-23, neuromedin S-36, neuromedin S-33, neuromedin U-25 | peptide | You C, Zhang Y, Xu P, Huang S, Yin W, Eric Xu H, Jiang Y | 10.1038/S41467-022-29683-W | 2022-04-20 | 53749 | |
Gq/11 | αq | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7XOW | 7XOW_refined | 3.1 | GASR | CCK2 | Cholecystokinin | A (Rhodopsin) | Human | - | scFv16 | - |
desulfated gastrin-17
pubchem
gtoplig
chembl_ligand
pubchem
|
peptide | Agonist | desulfated gastrin-14, desulfated cholecystokinin-8, gastrin-34, gastrin-14, CCK-58, desulfated gastrin-17, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8, desulfated gastrin-34, gastrin-71, desulfated gastrin-71 | peptide | Ding Y, Zhang H, Liao YY, Chen LN, Ji SY, Qin J, Mao C, Shen DD, Lin L, Wang H, Zhang Y, Li XM | 10.1038/S41421-022-00420-3 | 2022-07-20 | 53749 | |
Gq/11 | αq | Human | - | 57 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7X1T | - | 3.3 | TRFR | TRH1 | Thyrotropin-releasing hormone | A (Rhodopsin) | Human | - | scFv16 | - |
taltirelin
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | TRH | peptide | Yang F, Zhang H, Meng X, Li Y, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C | 10.1038/S41422-022-00646-6 | 2022-08-31 | 53749 | |
Gs | αs | Human | - | 58 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7VVK | - | 3.3 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
teriparatide
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
pubchem
pubchem
pubchem
pubchem
pubchem
|
peptide | Agonist | TIP39, PTHrP-(1-36), PTHrP, PTH | peptide | Kobayashi K, Kawakami K, Kusakizako T, Miyauchi H, Tomita A, Kobayashi K, Shihoya W, Yamashita K, Nishizawa T, Kato HE, Inoue A, Nureki O | 10.1016/J.MOLCEL.2022.07.003 | 2022-08-03 | 53739 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7VIF | 7VIF_refined | 2.8 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
(S)-FTY720-phosphate
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | Yu L, He L, Gan B, Ti R, Xiao Q, Hu H, Zhu L, Wang S, Ren R | 10.1073/PNAS.2117716119 | 2022-09-28 | 53741 | |
Gq/11 | αq | Human | - | 58 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7XW9 | - | 2.7 | TRFR | TRH1 | Thyrotropin-releasing hormone | A (Rhodopsin) | Human | - | scFv16 | - |
TRH
pubchem
|
peptide | Agonist | TRH | peptide | - | - | 2022-12-28 | 53749 | |
Gi/o | αi1 | Human | - | 64 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8EF5 | - | 3.3 | OPRM | μ | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
fentanyl
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | [Leu]enkephalin, β-endorphin, dynorphin A, [Met]enkephalin, endomorphin-1, endomorphin-2, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13) | peptide | Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, Rao Q, Yang J, Liu J, Zhou Q, Wang X, Liu M, Liu W, Jiang X, Yang D, Jiang H, Shen J, Melcher K, Chen H, Jiang Y, Cheng X, Wang MW, Xie X, Xu HE | 10.1016/J.CELL.2022.09.041 | 2022-11-09 | 53741 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 8ID3 | 8ID3_refined | 3.1 | FFAR4 | FFA4 | Free fatty acid | A (Rhodopsin) | Human | - | scFv16 | - |
9-Hydroxyoctadecanoic acid
pubchem
|
small-molecule | Agonist | myristic acid, linoleic acid, α-linolenic acid, oleic acid | small-molecule | Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP | 10.1126/SCIENCE.ADD6220 | 2023-03-15 | 53741 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8IW7 | - | 3.0 | TAAR9 | TAAR9 | A orphans | A (Rhodopsin) | Mouse | - | scFv16 | - |
2-Phenylethanaminium
pubchem
|
small-molecule | Agonist | - | - | Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP | 10.1038/S41586-023-06106-4 | 2023-05-31 | 53739 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8FLS | - | 3.1 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
abaloparatide
pubchem
|
small-molecule | Agonist | TIP39, PTHrP-(1-36), PTHrP, PTH | peptide | Cary BP, Gerrard EJ, Belousoff MJ, Fletcher MM, Jiang Y, Russell IC, Piper SJ, Wootten D, Sexton PM | 10.1016/J.STR.2023.04.002 | 2023-04-26 | 53739 | |
Gs | αs | Human | - | 57 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7Y35 | - | 2.9 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
abaloparatide
pubchem
|
small-molecule | Agonist | TIP39, PTHrP-(1-36), PTHrP, PTH | peptide | - | - | 2023-07-05 | 53739 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8J19 | - | 3.2 | GPR84 | GPR84 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
6-nonylpyridine-2,4-diol
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | - | - | Liu H, Zhang Q, He X, Jiang M, Wang S, Yan X, Cheng X, Liu Y, Nan FJ, Xu HE, Xie X, Yin W | 10.1038/S41467-023-38985-6 | 2023-06-21 | 53741 | |
Gi/o | αi1 | Human | - | 55 | β1 | Human | γ2 | Human | Cryo-EM | 8FEG | - | 2.5 | OPRK | κ | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
ACE-TYR-ALA-DTY-THR-THR-CYS-THR-DPN-XT9
|
peptide | Agonist | [Leu]enkephalin, β-neoendorphin, β-endorphin, dynorphin A, [Met]enkephalin, α-neoendorphin, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13), big dynorphin | peptide | Cheng Y, Prusoff WH | 10.1016/0006-2952(73)90196-2 | 2023-12-06 | 53741 | |
Gq/11 | αq | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8I9A | - | 3.6 | C3AR | C3a | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
EP54 ligand
|
peptide | Agonist | C5a, C3a | peptide | Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C | 10.1016/J.CELL.2023.09.020 | 2023-10-18 | 53749 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 8J6P | - | 2.6 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | - | scFv16 | - |
nicotinic acid
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
pubchem
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | Mao C, Gao M, Zang SK, Zhu Y, Shen DD, Chen LN, Yang L, Wang Z, Zhang H, Wang WW, Shen Q, Lu Y, Ma X, Zhang Y | 10.1038/S41467-023-43537-Z | 2023-12-06 | 53741 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 8SAI | 8SAI_refined | 3.3 | GPR34 | GPR34 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
O-[(S)-Hydroxy{[(2s)-2-Hydroxy-3-(Octadec-9-Enoyloxy)propyl]oxy}phosphoryl]-L-Serine
pubchem
|
small-molecule | Agonist | lysophosphatidylserine | small-molecule | Xia A, Yong X, Zhang C, Lin G, Jia G, Zhao C, Wang X, Hao Y, Wang Y, Zhou P, Yang X, Deng Y, Wu C, Chen Y, Zhu J, Tang X, Liu J, Zhang S, Zhang J, Xu Z, Hu Q, Zhao J, Yue Y, Yan W, Su Z, Wei Y, Zhou R, Dong H, Shao Z, Yang S | 10.1073/PNAS.2308435120 | 2023-10-04 | 53741 | |
Gs | αs | Bovine | - | 56 | β1 | Rat | γ2 | Bovine | Cryo-EM | 6NBI | - | 4.0 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
Long-acting parathyroid hormone analog
|
peptide | Agonist | TIP39, PTHrP-(1-36), PTHrP, PTH | peptide | Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y | 10.1126/SCIENCE.AAV7942 | 2019-04-17 | 53756 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 6PB1 | 6PB1_refined | 2.8 | CRFR2 | CRF2 | Corticotropin-releasing factor | B1 (Secretin) | Human | - | Nanobody-35 | - |
Urocortin
pubchem
|
peptide | Agonist | urocortin 1, corticotrophin-releasing hormone, urocortin 2, urocortin 3 | peptide | Ma S, Shen Q, Zhao LH, Mao C, Zhou XE, Shen DD, de Waal PW, Bi P, Li C, Jiang Y, Wang MW, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE | 10.1016/J.MOLCEL.2020.01.013 | 2020-02-12 | 53739 | |
Gs | αs | Human | - | 89 | β1 | Human | γ2 | Human | Cryo-EM | 6X19 | - | 2.1 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
CHU-128
pubchem
|
small-molecule | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, Senel P, Stewart GD, Liang YL, Glukhova A, Venugopal H, Christopoulos A, Furness SGB, Miller LJ, Reedtz-Runge S, Langmead CJ, Gloriam DE, Danev R, Sexton PM, Wootten D | 10.1016/J.MOLCEL.2020.09.020 | 2020-09-09 | 53739 | |
Gs | αs | Human | - | 55 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7DHI | - | 3.3 | ADRB2 | β2 | Adrenoceptors | A (Rhodopsin) | Human | - | Nanobody-35 | - |
levosalbutamol
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline | small-molecule | Si G, Du Y, Tang P, Ma G, Jia Z, Zhou X, Mu D, Shen Y, Lu Y, Mao Y, Chen C, Li Y, Gu N | 10.1093/NSR/NWAA284 | 2020-12-16 | 53739 | |
Gs | αs | Human | Engineered G alpha | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7JVQ | 7JVQ_refined | 3.0 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
apomorphine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP, Shen DD, Xu T, Liu YF, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE | 10.1016/J.CELL.2021.01.027 | 2021-02-24 | 53739 | |
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 | 53741 | |
Gs | αs | Human | - | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7DUR | - | 3.3 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
N-Tert-butyl-6,7-dichloroquinoxalin-2-amine
pubchem
|
small-molecule | Ago-PAM | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Cong Z, Chen LN, Ma H, Zhou Q, Zou X, Ye C, Dai A, Liu Q, Huang W, Sun X, Wang X, Xu P, Zhao L, Xia T, Zhong W, Yang D, Eric Xu H, Zhang Y, Wang MW | 10.1038/S41467-021-24058-Z | 2021-08-11 | 53739 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7EW2 | - | 3.1 | S1PR3 | S1P3 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
(S)-FTY720-phosphate
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | Zhao C, Cheng L, Wang W, Wang H, Luo Y, Feng Y, Wang X, Fu H, Cai Y, Yang S, Fu P, Yan W, Shao Z | 10.1038/S41422-021-00567-W | 2021-09-29 | 53741 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7F55 | - | 3.1 | MC4R | MC4 | Melanocortin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
bremelanotide
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
peptide | Agonist | β-MSH, α-MSH, agouti-related protein, γ-MSH, ACTH | peptide | Zhang H, Chen LN, Yang D, Mao C, Shen Q, Feng W, Shen DD, Dai A, Xie S, Zhou Y, Qin J, Sun JP, Scharf DH, Hou T, Zhou T, Wang MW, Zhang Y | 10.1038/S41422-021-00552-3 | 2021-11-03 | 53739 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7F4F | - | 2.9 | MSHR | MC1 | Melanocortin | A (Rhodopsin) | Human | - | scFv16 | - |
CHEMBL407070
chembl_ligand
pubchem
pubchem
|
protein | Agonist | β-MSH, ACTH, γ-MSH, α-MSH | peptide | Ma S, Chen Y, Dai A, Yin W, Guo J, Yang D, Zhou F, Jiang Y, Wang MW, Xu HE | 10.1038/S41422-021-00557-Y | 2021-09-08 | 53739 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7TYX | - | 2.6 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - | Nanobody-35 | - |
Amylin rat
pubchem
|
peptide | Agonist | adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP | peptide | Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM | 10.1126/SCIENCE.ABM9609 | 2022-03-30 | 53739 | |
Gi/o | αi1 | Human | Mini-Gi1 | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7WU4 | - | 3.4 | AGRF1 | ADGRF1 | ADGRF | B2 (Adhesion) | Human | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | - | - | 2022-04-27 | 53741 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7X9B | 7X9B_refined | 3.4 | NPY2R | Y2 | Neuropeptide Y | A (Rhodopsin) | Human | - | - | - |
neuropeptide Y
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
pubchem
pubchem
pubchem
|
peptide | Agonist | pancreatic polypeptide, neuropeptide Y-(3-36), PYY-(3-36), neuropeptide Y, peptide YY | peptide | Tang T, Tan Q, Han S, Diemar A, Lobner K, Wang H, Schuss C, Behr V, Morl K, Wang M, Chu X, Yi C, Keller M, Kofoed J, Reedtz-Runge S, Kaiser A, Beck-Sickinger AG, Zhao Q, Wu B | 10.1126/SCIADV.ABM1232 | 2022-05-18 | 53741 | |
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 | 53739 | |
Gi/o | αi1 | Human | - | 63 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7XAT | 7XAT_refined | 2.9 | SSR2 | SST2 | Somatostatin | A (Rhodopsin) | Human | - | scFv16 | - |
SOMATOSTATIN
chembl_ligand
pubchem
|
protein | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | Bo Q, Yang F, Li Y, Meng X, Zhang H, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C | 10.1038/S41421-022-00405-2 | 2022-08-31 | 53741 | |
Gs | αs | Human | Mini-Gs | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7XKE | - | 2.9 | AGRG2 | ADGRG2 | ADGRG | B2 (Adhesion) | Mouse | - | Nanobody-35 | - |
PRASTERONE
chembl_ligand
pubchem
|
small-molecule | Agonist | - | - | Lin H, Xiao P, Bu RQ, Guo S, Yang Z, Yuan D, Zhu ZL, Zhang CX, He QT, Zhang C, Ping YQ, Zhao RJ, Ma CS, Liu CH, Zhang XN, Jiang D, Huang S, Xi YT, Zhang DL, Xue CY, Yang BS, Li JY, Lin HC, Zeng XH, Zhao H, Xu WM, Yi F, Liu Z, Sun JP, Yu X | 10.1038/S41589-022-01084-6 | 2022-08-10 | 53739 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7WCN | 7WCN_refined | 2.9 | GP119 | GPR119 | GPR18, GPR55 and GPR119 | A (Rhodopsin) | Human | - | Nanobody-35 | - |
AR231453
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | N-oleoylethanolamide, anandamide, N-palmitoylethanolamine, SEA | small-molecule | Qian Y, Wang J, Yang L, Liu Y, Wang L, Liu W, Lin Y, Yang H, Ma L, Ye S, Wu S, Qiao A | 10.1038/S41467-022-34696-6 | 2022-12-21 | 53739 | |
Gq/11 | αq | Human | Mini-Gq | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7Y26 | 7Y26_refined | 3.3 | SSR2 | SST2 | Somatostatin | A (Rhodopsin) | Human | - | scFv16 | - |
Octreotide
|
peptide | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | Chen S, Teng X, Zheng S | 10.1038/S41589-022-01130-3 | 2022-10-19 | 53749 | |
Gi/o | αi2 | Human | - | 58 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7YJ4 | - | 3.2 | RL3R2 | RXFP4 | Relaxin family peptide | A (Rhodopsin) | Human | - | scFv16 | - |
Insulin-like peptide INSL5 B chain
pubchem
Insulin-like peptide INSL5 A chain pubchem |
peptide peptide |
Agonist | INSL5, relaxin-3 (B chain), relaxin-3 | peptide | Chen Y, Zhou Q, Wang J, Xu Y, Wang Y, Yan J, Wang Y, Zhu Q, Zhao F, Li C, Chen CW, Cai X, Bathgate RAD, Shen C, Eric Xu H, Yang D, Liu H, Wang MW | 10.1038/S41467-023-36182-Z | 2023-03-01 | 53742 | |
Gs | αs | Human | Mini-Gs | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8HIX | - | 3.1 | GPR21 | GPR21 | A orphans | A (Rhodopsin) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Lin X, Chen B, Wu Y, Han Y, Qi A, Wang J, Yang Z, Wei X, Zhao T, Wu L, Xie X, Sun J, Zheng J, Zhao S, Xu F | 10.1038/S41467-023-35882-W | 2023-03-15 | 53739 | |
Gi/o | αo | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7T8X | 7T8X_refined | 3.2 | ACM2 | M2 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | Antibody fragment | - |
acetylcholine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
|
small-molecule | Agonist | acetylcholine | small-molecule | - | - | 2023-01-25 | 53747 | |
Gi/o | αi1 | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8DZP | - | 2.7 | OPRK | κ | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
SALVINORIN B METHOXYMETHYL ETHER
chembl_ligand
pubchem
|
small-molecule | Agonist | [Leu]enkephalin, β-neoendorphin, β-endorphin, dynorphin A, [Met]enkephalin, α-neoendorphin, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13), big dynorphin | peptide | Han J, Zhang J, Nazarova AL, Bernhard SM, Krumm BE, Zhao L, Lam JH, Rangari VA, Majumdar S, Nichols DE, Katritch V, Yuan P, Fay JF, Che T | 10.1038/S41586-023-06030-7 | 2023-05-03 | 53741 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7YAC | 7YAC_refined | 3.2 | SSR2 | SST2 | Somatostatin | A (Rhodopsin) | Human | - | scFv16 | - |
PALTUSOTINE
chembl_ligand
pubchem
|
small-molecule | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | Zhao J, Fu H, Yu J, Hong W, Tian X, Qi J, Sun S, Zhao C, Wu C, Xu Z, Cheng L, Chai R, Yan W, Wei X, Shao Z | 10.1038/S41467-023-36673-Z | 2023-04-19 | 53741 | |
G12/13 | α12 | Human | Mini-G12 | 55 | β1 | Human | γ2 | Human | Cryo-EM | 7YDJ | - | 3.0 | AGRE5 | ADGRE5 | ADGRE | B2 (Adhesion) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | - | - | 2023-07-12 | 53753 | |
Gq/11 | αq | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8IUK | - | 2.7 | PF2R | FP | Prostanoid | A (Rhodopsin) | Human | - |
scFv16 Nanobody-35 |
- |
PGF2α
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
small-molecule | Agonist | thromboxane A2, PGF2α, PGI2, PGD2, PGE2 | small-molecule | Wu C, Xu Y, He Q, Li D, Duan J, Li C, You C, Chen H, Fan W, Jiang Y, Eric Xu H | 10.1038/S41467-023-38411-X | 2023-07-12 | 53749 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8JLZ | - | 3.1 | 5HT6R | 5-HT6 | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
CHEMBL365751
chembl_ligand
pubchem
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Pei Y, Wen X, Guo SC, Yang ZS, Zhang R, Xiao P, Sun JP | 10.1016/J.BBRC.2023.05.126 | 2023-06-28 | 53739 | |
Gq/11 | αq | Human | - | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8THK | - | 2.6 | ADA1A | α1A | Adrenoceptors | A (Rhodopsin) | Human | T4-Lysozyme | scFv16 | - |
CHEMBL133451
chembl_ligand
pubchem
|
small-molecule | Agonist | (-)-adrenaline, (-)-noradrenaline | small-molecule | Su M, Wang J, Xiang G, Do HN, Levitz J, Miao Y, Huang XY | 10.1038/S41467-023-40524-2 | 2023-08-16 | 53749 | |
Gi/o | αo | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8IA2 | 8IA2_refined | 3.2 | C5AR1 | C5a1 | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
C5a
gtoplig
|
peptide | Agonist | ribosomal protein S19, C5a, C5a des-Arg, C3a | peptide | Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C | 10.1016/J.CELL.2023.09.020 | 2023-10-18 | 53747 | |
Gs | αs | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8JLO | - | 3.5 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Human | - | - | - |
ulotaront
pubchem
gtoplig
drugbank
chembl_ligand
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, dopamine | small-molecule | Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z | 10.1038/S41586-023-06804-Z | 2023-11-15 | 53739 | |
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 | 53741 | |
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 | 53739 | |
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 | 53741 | |
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 | 53741 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7EZK | - | 3.1 | CCKAR | CCK1 | Cholecystokinin | A (Rhodopsin) | Human | - | - | - |
CCK-8
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
peptide | Agonist | desulfated cholecystokinin-8, CCK-58, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8 | peptide | Liu Q, Yang D, Zhuang Y, Croll TI, Cai X, Dai A, He X, Duan J, Yin W, Ye C, Zhou F, Wu B, Zhao Q, Xu HE, Wang MW, Jiang Y | 10.1038/S41589-021-00841-3 | 2021-08-25 | 53739 | |
Gi/o | αi1 | Human | - | 43 | β1 | Human | γ2 | Human | Cryo-EM | 7EO4 | 7EO4_refined | 2.9 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
siponimod
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | Xu Z, Ikuta T, Kawakami K, Kise R, Qian Y, Xia R, Sun MX, Zhang A, Guo C, Cai XH, Huang Z, Inoue A, He Y | 10.1038/S41589-021-00930-3 | 2022-01-05 | 53741 | |
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 | 53749 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7TYH | - | 3.3 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - | Nanobody-35 | - |
Calcitonin human
pubchem
|
peptide | Agonist | adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP | peptide | - | - | 2022-03-23 | 53739 | |
Gs | αs | Human | - | 55 | β1 | Human | γ2 | Human | Cryo-EM | 7WUQ | - | 2.9 | AGRG2 | ADGRG2 | ADGRG | B2 (Adhesion) | Mouse | - | Nanobody-35 | - | - | - | - | - | - | Xiao P, Guo S, Wen X, He QT, Lin H, Huang SM, Gou L, Zhang C, Yang Z, Zhong YN, Yang CC, Li Y, Gong Z, Tao XN, Yang ZS, Lu Y, Li SL, He JY, Wang C, Zhang L, Kong L, Sun JP, Yu X | 10.1038/S41586-022-04590-8 | 2022-04-27 | 53739 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7F0T | - | 3.1 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
dopamine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | Teng X, Chen S, Wang Q, Chen Z, Wang X, Huang N, Zheng S | 10.1126/SCIADV.ABO4158 | 2022-06-15 | 53739 | |
Gs | αs | Human | - | 60 | β1 | Rat | γ2 | Human | Cryo-EM | 7X8S | 7X8S_refined | 3.1 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
WB4-24
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Cong Z, Zhou Q, Li Y, Chen LN, Zhang ZC, Liang A, Liu Q, Wu X, Dai A, Xia T, Wu W, Zhang Y, Yang D, Wang MW | 10.1073/PNAS.2200155119 | 2022-06-29 | 53739 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7XMR | 7XMR_refined | 3.1 | SSR2 | SST2 | Somatostatin | A (Rhodopsin) | Human | - | - | - |
SOMATOSTATIN
chembl_ligand
pubchem
|
protein | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | Zhao W, Han S, Qiu N, Feng W, Lu M, Zhang W, Wang M, Zhou Q, Chen S, Xu W, Du J, Chu X, Yi C, Dai A, Hu L, Shen MY, Sun Y, Zhang Q, Ma Y, Zhong W, Yang D, Wang MW, Wu B, Zhao Q | 10.1038/S41422-022-00679-X | 2022-08-03 | 53741 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7YP7 | - | 3.1 | AGRG2 | ADGRG2 | ADGRG | B2 (Adhesion) | Mouse | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | - | - | 2022-08-24 | 53739 | |
Gi/o | αo | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7W7E | - | 3.4 | ADA2A | α2A | Adrenoceptors | A (Rhodopsin) | Human | - | scFv16 | - |
5-(3-Bicyclo[4.2.0]octa-1,3,5-trienyl)-1,2,3,6-tetrahydropyridine
pubchem
|
small-molecule | Agonist | (-)-adrenaline, (-)-noradrenaline | small-molecule | Fink EA, Xu J, Hubner H, Braz JM, Seemann P, Avet C, Craik V, Weikert D, Schmidt MF, Webb CM, Tolmachova NA, Moroz YS, Huang XP, Kalyanaraman C, Gahbauer S, Chen G, Liu Z, Jacobson MP, Irwin JJ, Bouvier M, Du Y, Shoichet BK, Basbaum AI, Gmeiner P | 10.1126/SCIENCE.ABN7065 | 2022-09-28 | 53747 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7X5H | 7X5H_refined | 3.1 | 5HT5A | 5-HT5A | 5-Hydroxytryptamine | A (Rhodopsin) | Human | BRIL | scFv16 | - |
5-CT
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Tan Y, Xu P, Huang S, Yang G, Zhou F, He X, Ma H, Xu HE, Jiang Y | 10.1038/S41421-022-00412-3 | 2022-09-14 | 53741 | |
Gi/o | αi1 | Human | - | 64 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8F7Q | - | 3.2 | OPRM | μ | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
β-endorphin
pubchem
gtoplig
chembl_ligand
pubchem
|
peptide | Agonist | [Leu]enkephalin, β-endorphin, dynorphin A, [Met]enkephalin, endomorphin-1, endomorphin-2, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13) | peptide | Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y, Roth BL, Xu HE | 10.1016/J.CELL.2022.12.026 | 2022-12-14 | 53741 | |
G12/13 | α13 | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8H8J | 8H8J_refined | 3.2 | GPR35 | GPR35 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
lodoxamide
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
small-molecule | Agonist | 1-Lyso-2-oleoyl-phosphatidic acid, 2-Oleoyllysophosphatydic acid, kynurenic acid, 2-oleoyl-LPA | small-molecule | Duan J, Liu Q, Yuan Q, Ji Y, Zhu S, Tan Y, He X, Xu Y, Shi J, Cheng X, Jiang H, Eric Xu H, Jiang Y | 10.1038/S41421-022-00499-8 | 2023-02-08 | 53754 | |
Gq/11 | αq | Human | - | 79 | β1 | Human | γ2 | Human | Cryo-EM | 7W40 | 7W40_refined | 3.0 | GRPR | BB2 | Bombesin | A (Rhodopsin) | Human | - | scFv16 | - |
Bombesin
|
peptide | Agonist | neuromedin B, gastrin releasing peptide(14-27) (human), GRP-(18-27), gastrin-releasing peptide, neuromedin C | peptide | Peng S, Zhan Y, Zhang D, Ren L, Chen A, Chen ZF, Zhang H | 10.1073/PNAS.2216230120 | 2023-02-22 | 53749 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7TRQ | - | 2.5 | ACM4 | M4 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | scFv16 | - |
iperoxo
pubchem
gtoplig
chembl_ligand
VU0467154 pubchem gtoplig chembl_ligand |
small-molecule small-molecule |
Agonist PAM |
acetylcholine | small-molecule | - | - | 2023-05-17 | 53741 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 8IRT | - | 2.7 | DRD3 | D3 | Dopamine | A (Rhodopsin) | Human | BRIL | scFv16 | - |
rotigotine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | dopamine | small-molecule | Xu P, Huang S, Krumm BE, Zhuang Y, Mao C, Zhang Y, Wang Y, Huang XP, Liu YF, He X, Li H, Yin W, Jiang Y, Zhang Y, Roth BL, Xu HE | 10.1038/S41422-023-00808-0 | 2023-06-07 | 53741 | |
Gs | αs | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8HMP | - | 2.8 | GPR52 | GPR52 | A orphans | A (Rhodopsin) | Human | - | Nanobody-35 | - |
derivative 17 [Nakahata et al., 2018]
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | - | - | Fan Y, Lin X, Pan B, Chen B, Liu D, Wuthrich K, Xu F | 10.1002/MCO2.260 | 2023-06-21 | 53739 | |
Gi/o | αi1 | Mouse | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 8FX5 | - | 2.5 | ACM4 | M4 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | scFv16 | - |
xanomeline
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
small-molecule | Agonist | acetylcholine | small-molecule | Burger WAC, Pham V, Vuckovic Z, Powers AS, Mobbs JI, Laloudakis Y, Glukhova A, Wootten D, Tobin AB, Sexton PM, Paul SM, Felder CC, Danev R, Dror RO, Christopoulos A, Valant C, Thal DM | 10.1038/S41467-023-41199-5 | 2023-09-13 | 53783 | |
Gs | αs | Human | - | 40 | β1 | Human | γ2 | Human | Cryo-EM | 8HTI | - | 3.0 | O52E4 | Olfactory 52E4 | Olfactory | A (Rhodopsin) | Human | - | Nanobody-35 | - |
OCTANOIC ACID
chembl_ligand
pubchem
pubchem
|
small-molecule | Agonist | - | - | Choi C, Bae J, Kim S, Lee S, Kang H, Kim J, Bang I, Kim K, Huh WK, Seok C, Park H, Im W, Choi HJ | 10.1038/S41467-023-43983-9 | 2023-12-20 | 53739 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8W8Q | 8W8Q_refined | 2.9 | GP101 | GPR101 | A orphans | A (Rhodopsin) | Human | BRIL | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Yang Z, Wang JY, Yang F, Zhu KK, Wang GP, Guan Y, Ning SL, Lu Y, Li Y, Zhang C, Zheng Y, Zhou SH, Wang XW, Wang MW, Xiao P, Yi F, Zhang C, Zhang PJ, Xu F, Liu BH, Zhang H, Yu X, Gao N, Sun JP | 10.1038/S41589-023-01456-6 | 2024-01-03 | 53739 | |
Gs | αs | Human | - | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7V9L | - | 2.6 | GHRHR | GHRH | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | GHRH | peptide | Cong Z, Zhou F, Zhang C, Zou X, Zhang H, Wang Y, Zhou Q, Cai X, Liu Q, Li J, Shao L, Mao C, Wang X, Wu J, Xia T, Zhao LH, Jiang H, Zhang Y, Xu HE, Cheng X, Yang D, Wang MW | 10.1073/PNAS.2106606118 | 2022-04-06 | 53739 | |
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 | 53851 | |
Gs | αs | Human | - | 43 | β1 | Human | γ2 | Human | Cryo-EM | 6NIY | - | 3.3 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - | - | - |
calcitonin (salmon synthetic)
pubchem
|
small-molecule | Agonist | adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP | peptide | Dal Maso E, Glukhova A, Zhu Y, Garcia-Nafria J, Tate CG, Atanasio S, Reynolds CA, Ramirez-Aportela E, Carazo JM, Hick CA, Furness SGB, Hay DL, Liang YL, Miller LJ, Christopoulos A, Wang MW, Wootten D, Sexton PM | 10.1021/ACSPTSCI.8B00056 | 2019-01-23 | 53739 | |
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 | 53747 | |
Gs | αs | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 6VN7 | 6VN7_refined | 3.2 | VIPR1 | VPAC1 | VIP and PACAP | B1 (Secretin) | Human | - | Nanobody-35 | - |
[Ac-His1]PACAP-27
gtoplig
chembl_ligand
pubchem
|
peptide | Agonist | VIP, PHI, PHM, secretin, PACAP-27, GHRH, PACAP-38 | peptide | Duan J, Shen DD, Zhou XE, Bi P, Liu QF, Tan YX, Zhuang YW, Zhang HB, Xu PY, Huang SJ, Ma SS, He XH, Melcher K, Zhang Y, Xu HE, Jiang Y | 10.1038/S41467-020-17933-8 | 2020-09-02 | 53739 | |
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 | 53741 | |
Gs | αs | Human | - | 61 | β1 | Rat | γ2 | Human | Cryo-EM | 7MBX | - | 2.0 | CCKAR | CCK1 | Cholecystokinin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
CHEMBL216166
chembl_ligand
pubchem
|
protein | Agonist | desulfated cholecystokinin-8, CCK-58, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8 | peptide | Mobbs JI, Belousoff MJ, Harikumar KG, Piper SJ, Xu X, Furness SGB, Venugopal H, Christopoulos A, Danev R, Wootten D, Thal DM, Miller LJ, Sexton PM | 10.1371/JOURNAL.PBIO.3001295 | 2021-05-26 | 53739 | |
Gs | αs | Human | - | 61 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7DUQ | - | 2.5 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
N-Tert-butyl-6,7-dichloroquinoxalin-2-amine
pubchem
CHEMBL410972 chembl_ligand pubchem pubchem |
small-molecule protein |
Ago-PAM Agonist |
glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Cong Z, Chen LN, Ma H, Zhou Q, Zou X, Ye C, Dai A, Liu Q, Huang W, Sun X, Wang X, Xu P, Zhao L, Xia T, Zhong W, Yang D, Eric Xu H, Zhang Y, Wang MW | 10.1038/S41467-021-24058-Z | 2021-07-14 | 53739 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7EW4 | 7EW4_refined | 3.2 | S1PR3 | S1P3 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
CYM-5541
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | Zhao C, Cheng L, Wang W, Wang H, Luo Y, Feng Y, Wang X, Fu H, Cai Y, Yang S, Fu P, Yan W, Shao Z | 10.1038/S41422-021-00567-W | 2021-09-29 | 53741 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7VGX | 7VGX_refined | 3.2 | NPY1R | Y1 | Neuropeptide Y | A (Rhodopsin) | Human | - | scFv16 | - |
neuropeptide Y
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
pubchem
pubchem
pubchem
|
peptide | Agonist | peptide YY, neuropeptide Y, pancreatic polypeptide | peptide | Park C, Kim J, Ko SB, Choi YK, Jeong H, Woo H, Kang H, Bang I, Kim SA, Yoon TY, Seok C, Im W, Choi HJ | 10.1038/S41467-022-28510-6 | 2022-02-23 | 53741 | |
Gs | αs | Human | Mini-Gs | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7VAB | 7VAB_refined | 3.2 | GIPR | GIP | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
tirzepatide
pubchem
gtoplig
|
peptide | Agonist | gastric inhibitory polypeptide | peptide | Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW | 10.1038/S41467-022-28683-0 | 2022-03-02 | 53739 | |
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 | 53739 | |
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 | 53756 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7E2Z | - | 3.1 | 5HT1A | 5-HT1A | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | - | - |
aripiprazole
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist (partial) | 5-hydroxytryptamine | small-molecule | Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen DD, Yen HY, Robinson CV, Harpsoe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE | 10.1038/S41586-021-03376-8 | 2021-04-14 | 53741 | |
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 | 53741 | |
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 | 53741 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7EW3 | - | 3.1 | S1PR3 | S1P3 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
Sphingosine 1-phosphate
pubchem
|
lipid | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | Zhao C, Cheng L, Wang W, Wang H, Luo Y, Feng Y, Wang X, Fu H, Cai Y, Yang S, Fu P, Yan W, Shao Z | 10.1038/S41422-021-00567-W | 2021-09-29 | 53741 | |
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 | 53749 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7F4D | - | 3.0 | MSHR | MC1 | Melanocortin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
INTERMEDINE
chembl_ligand
pubchem
pubchem
pubchem
|
protein | Agonist | β-MSH, ACTH, γ-MSH, α-MSH | peptide | Ma S, Chen Y, Dai A, Yin W, Guo J, Yang D, Zhou F, Jiang Y, Wang MW, Xu HE | 10.1038/S41422-021-00557-Y | 2021-09-08 | 53739 | |
Gi/o | αi1 | Human | - | 64 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7WQ3 | 7WQ3_refined | 2.7 | GALR1 | GAL1 | Galanin | A (Rhodopsin) | Human | - | scFv16 | - |
galanin
pubchem
gtoplig
chembl_ligand
gtoplig
pubchem
pubchem
pubchem
pubchem
|
peptide | Agonist | galanin-like peptide, galanin | peptide | - | - | 2022-04-20 | 53741 | |
Gq/11 | αq | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7F6I | 7F6I_refined | 2.8 | BKRB2 | B2 | Bradykinin | A (Rhodopsin) | Human | - | - | - |
kallidin
pubchem
gtoplig
|
peptide | Agonist | [des-Arg10]kallidin, Lys-[Hyp3]-bradykinin, kallidin, [des-Arg9]bradykinin, [Hyp3]bradykinin, T-kinin, bradykinin | peptide | Shen J, Zhang D, Fu Y, Chen A, Yang X, Zhang H | 10.1038/S41467-022-28399-1 | 2022-01-05 | 53749 | |
Gs | αs | Human | - | 59 | β1 | Rat | γ2 | Human | Cryo-EM | 7X8R | - | 2.6 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
CHEMBL2158411
chembl_ligand
pubchem
|
small-molecule | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Cong Z, Zhou Q, Li Y, Chen LN, Zhang ZC, Liang A, Liu Q, Wu X, Dai A, Xia T, Wu W, Zhang Y, Yang D, Wang MW | 10.1073/PNAS.2200155119 | 2022-06-29 | 53739 | |
Gq/11 | αq | Human | Mini-Gq | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7WY5 | - | 2.8 | AGRL3 | ADGRL3 | ADGRL | B2 (Adhesion) | Mouse | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Qian Y, Ma Z, Liu C, Li X, Zhu X, Wang N, Xu Z, Xia R, Liang J, Duan Y, Yin H, Xiong Y, Zhang A, Guo C, Chen Z, Huang Z, He Y | 10.1016/J.MOLCEL.2022.10.009 | 2022-10-26 | 53749 | |
Gi/o | αi1 | Human | - | 63 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7YU3 | 7YU3_refined | 3.4 | LPAR1 | LPA1 | Lysophospholipid (LPA) | A (Rhodopsin) | Human | - | scFv16 | - |
[(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate
pubchem
|
small-molecule | Agonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O | 10.1038/S41467-022-33121-2 | 2022-10-05 | 53741 | |
Gi/o | αi1 | Human | - | 61 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8EFQ | - | 3.3 | OPRM | μ | Opioid | A (Rhodopsin) | Human | - | - | - |
DAMGO
pubchem
gtoplig
chembl_ligand
chembl_ligand
|
peptide | Agonist | [Leu]enkephalin, β-endorphin, dynorphin A, [Met]enkephalin, endomorphin-1, endomorphin-2, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13) | peptide | Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, Rao Q, Yang J, Liu J, Zhou Q, Wang X, Liu M, Liu W, Jiang X, Yang D, Jiang H, Shen J, Melcher K, Chen H, Jiang Y, Cheng X, Wang MW, Xie X, Xu HE | 10.1016/J.CELL.2022.09.041 | 2022-11-09 | 53741 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7YS6 | 7YS6_refined | 3.0 | 5HT6R | 5-HT6 | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | scFv16 | - |
5-hydroxytryptamine
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | - | - | 2023-03-29 | 53739 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8GY7 | - | 3.3 | ACTHR | MC2 | Melanocortin | A (Rhodopsin) | Human | BRIL | - | MRAP1 |
ACTH
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
|
peptide | Agonist | ACTH | peptide | Luo P, Feng W, Ma S, Dai A, Wu K, Chen X, Yuan Q, Cai X, Yang D, Wang MW, Eric Xu H, Jiang Y | 10.1038/S41422-022-00751-6 | 2023-01-11 | 53739 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7TRS | - | 2.8 | ACM4 | M4 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | scFv16 | - |
acetylcholine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
|
small-molecule | Agonist | acetylcholine | small-molecule | - | - | 2023-05-17 | 53741 | |
Gq/11 | αq | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8EJK | - | 3.4 | FFAR1 | FFA1 | Free fatty acid | A (Rhodopsin) | Human | - | scFv16 | - |
fasiglifam
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | myristic acid, oleic acid, α-linolenic acid, docosahexaenoic acid | small-molecule | Kumari P, Inoue A, Chapman K, Lian P, Rosenbaum DM | 10.1073/PNAS.2219569120 | 2023-05-24 | 53749 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7YKD | - | 2.8 | CML1 | chemerin | Chemerin receptor | A (Rhodopsin) | Human | - | scFv16 | - |
chemerin C-terminal peptide
pubchem
gtoplig
chembl_ligand
pubchem
|
peptide | Agonist | 18R-HEPE, chemerin C-terminal peptide, EPA, resolvin E1, chemerin | peptide | Wang J, Chen G, Liao Q, Lyu W, Liu A, Zhu L, Du Y, Ye RD | 10.1073/PNAS.2214324120 | 2023-04-19 | 53741 | |
Gq/11 | αq | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7YFD | - | 3.1 | HRH4 | H4 | Histamine | A (Rhodopsin) | Human | - |
scFv16 Nanobody-35 |
- |
imetit
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | histamine, CCL16 | small-molecule | Im D, Kishikawa JI, Shiimura Y, Hisano H, Ito A, Fujita-Fujiharu Y, Sugita Y, Noda T, Kato T, Asada H, Iwata S | 10.1038/S41467-023-42260-Z | 2023-10-25 | 53749 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8HNK | - | 3.0 | CXCR3 | CXCR3 | Chemokine | A (Rhodopsin) | Human | - | scFv16 | - |
CXCL11
gtoplig
|
peptide | Agonist | CCL19, CXCL11, CCL13, CXCL9, CXCL10, CCL7, CCL5, CCL11, CXCL12α, CCL20 | peptide | Jiao H, Pang B, Liu A, Chen Q, Pan Q, Wang X, Xu Y, Chiang YC, Ren R, Hu H | 10.1038/S41594-023-01175-5 | 2023-11-29 | 53741 | |
Gs | αs | Human | - | 56 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8JIQ | 8JIQ_refined | 3.4 | GLR | glucagon | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
Dual-agonist peptide P15
|
peptide | Agonist | glucagon | peptide | Li Y, Zhou Q, Dai A, Zhao F, Chang R, Ying T, Wu B, Yang D, Wang MW, Cong Z | 10.1073/PNAS.2303696120 | 2023-09-13 | 53739 | |
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 | 53741 | |
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 | 53741 | |
Gs | αs | Human | Gs-Gi1 chimera | 58 | β1 | Human | γ2 | Human | Cryo-EM | 6PB0 | - | 3.0 | CRFR1 | CRF1 | Corticotropin-releasing factor | B1 (Secretin) | Human | - | Nanobody-35 | - |
Urocortin
pubchem
|
peptide | Agonist | urocortin 1, corticotrophin-releasing hormone, urocortin 2 | peptide | Ma S, Shen Q, Zhao LH, Mao C, Zhou XE, Shen DD, de Waal PW, Bi P, Li C, Jiang Y, Wang MW, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE | 10.1016/J.MOLCEL.2020.01.013 | 2020-02-12 | 53739 | |
Gs | αs | Human | - | 89 | β1 | Human | γ2 | Human | Cryo-EM | 6X1A | - | 2.5 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
danuglipron
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, Senel P, Stewart GD, Liang YL, Glukhova A, Venugopal H, Christopoulos A, Furness SGB, Miller LJ, Reedtz-Runge S, Langmead CJ, Gloriam DE, Danev R, Sexton PM, Wootten D | 10.1016/J.MOLCEL.2020.09.020 | 2020-09-09 | 53739 | |
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 | 53756 | |
Gi/o | αi2 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7F8V | - | 3.3 | GASR | CCK2 | Cholecystokinin | A (Rhodopsin) | Human | - | - | - |
desulfated gastrin-17
pubchem
gtoplig
chembl_ligand
pubchem
|
peptide | Agonist | desulfated gastrin-14, desulfated cholecystokinin-8, gastrin-34, gastrin-14, CCK-58, desulfated gastrin-17, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8, desulfated gastrin-34, gastrin-71, desulfated gastrin-71 | peptide | Zhang X, He C, Wang M, Zhou Q, Yang D, Zhu Y, Feng W, Zhang H, Dai A, Chu X, Wang J, Yang Z, Jiang Y, Sensfuss U, Tan Q, Han S, Reedtz-Runge S, Xu HE, Zhao S, Wang MW, Wu B, Zhao Q | 10.1038/S41589-021-00866-8 | 2021-10-13 | 53742 | |
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 | 53741 | |
Gs | αs | Human | - | 50 | β1 | Human | γ2 | Human | Cryo-EM | 7LLY | 7LLY_refined | 3.3 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
Pro-glucagon
pubchem
|
peptide | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Deganutti G, Liang YL, Zhang X, Khoshouei M, Clydesdale L, Belousoff MJ, Venugopal H, Truong TT, Glukhova A, Keller AN, Gregory KJ, Leach K, Christopoulos A, Danev R, Reynolds CA, Zhao P, Sexton PM, Wootten D | 10.1038/S41467-021-27760-0 | 2022-01-12 | 53739 | |
Gi/o | αi1 | Mouse | - | 62 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7TD0 | - | 2.8 | LPAR1 | LPA1 | Lysophospholipid (LPA) | A (Rhodopsin) | Human | - | - | - |
lysophosphatidic acid
pubchem
|
small-molecule | Agonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY | 10.1038/S41467-022-28417-2 | 2022-02-09 | 53783 | |
Gi/o | αi2 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7WVV | 7WVV_refined | 2.9 | FPR2 | FPR2/ALX | Formylpeptide | A (Rhodopsin) | Human | BRIL | - | - |
synthetic peptide
|
peptide | Agonist | humanin, aspirin-triggered resolvin D1, LXA4, resolvin D1, serum amyloid A, PrP106-126, 15-deoxy-LXA4, aspirin triggered lipoxin A4, LL-37, LTC4, annexin I, fMet-Leu-Phe, LTD4 | peptide | Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B | 10.1038/S41467-022-29361-X | 2022-04-13 | 53742 | |
Gi/o | αi1 | Human | Mini-Gi1 | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7WU5 | - | 3.0 | AGRF1 | ADGRF1 | ADGRF | B2 (Adhesion) | Human | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Qu X, Qiu N, Wang M, Zhang B, Du J, Zhong Z, Xu W, Chu X, Ma L, Yi C, Han S, Shui W, Zhao Q, Wu B | 10.1038/S41586-022-04580-W | 2022-04-27 | 53741 | |
Gs | αs | Human | - | 59 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7XJH | - | 3.3 | ADRB3 | β3 | Adrenoceptors | A (Rhodopsin) | Dog | - | Nanobody-35 | - |
LEVISOPRENALINE
chembl_ligand
chembl_ligand
pubchem
|
small-molecule | Agonist | - | - | Nagiri C, Kobayashi K, Tomita A, Kato M, Kobayashi K, Yamashita K, Nishizawa T, Inoue A, Shihoya W, Nureki O | 10.1016/J.MOLCEL.2021.06.024 | 2022-05-04 | 53739 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7X2F | 7X2F_refined | 3.0 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
dopamine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
mevidalen pubchem gtoplig chembl_ligand |
small-molecule small-molecule |
Agonist PAM |
L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | Teng X, Chen S, Nie Y, Xiao P, Yu X, Shao Z, Zheng S | 10.1038/S41467-022-30929-W | 2022-06-15 | 53739 | |
Gq/11 | αq | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7XOX | 7XOX_refined | 3.1 | GASR | CCK2 | Cholecystokinin | A (Rhodopsin) | Human | - | scFv16 | - |
CCK-8
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
peptide | Agonist | desulfated gastrin-14, desulfated cholecystokinin-8, gastrin-34, gastrin-14, CCK-58, desulfated gastrin-17, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8, desulfated gastrin-34, gastrin-71, desulfated gastrin-71 | peptide | Ding Y, Zhang H, Liao YY, Chen LN, Ji SY, Qin J, Mao C, Shen DD, Lin L, Wang H, Zhang Y, Li XM | 10.1038/S41421-022-00420-3 | 2022-07-20 | 53749 | |
Gi/o | αo | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7QVM | - | 3.3 | OXYR | OT | Vasopressin and oxytocin | A (Rhodopsin) | Human | - | scFv16 | - |
oxytocin
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
|
peptide | Agonist | vasopressin, oxytocin | peptide | Waltenspuhl Y, Ehrenmann J, Vacca S, Thom C, Medalia O, Pluckthun A | 10.1038/S41467-022-31325-0 | 2022-08-10 | 53747 | |
Gs | αs | Human | - | 57 | β1 | Human | γ2 | Human | Cryo-EM | 7XKD | - | 2.4 | AGRG2 | ADGRG2 | ADGRG | B2 (Adhesion) | Mouse | - | Nanobody-35 | - |
PRASTERONE
chembl_ligand
pubchem
|
small-molecule | Agonist | - | - | - | - | 2022-08-10 | 53739 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7VIH | 7VIH_refined | 3.0 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
icanbelimod
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | Yu L, He L, Gan B, Ti R, Xiao Q, Hu H, Zhu L, Wang S, Ren R | 10.1073/PNAS.2117716119 | 2022-09-28 | 53741 | |
Gi/o | αo | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7Y24 | - | 3.3 | SSR2 | SST2 | Somatostatin | A (Rhodopsin) | Human | - | scFv16 | - |
Octreotide
|
peptide | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | Chen S, Teng X, Zheng S | 10.1038/S41589-022-01130-3 | 2022-10-19 | 53747 | |
Gi/o | αi1 | Human | - | 64 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8EFO | - | 2.8 | OPRM | μ | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
PZM21
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | [Leu]enkephalin, β-endorphin, dynorphin A, [Met]enkephalin, endomorphin-1, endomorphin-2, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13) | peptide | Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, Rao Q, Yang J, Liu J, Zhou Q, Wang X, Liu M, Liu W, Jiang X, Yang D, Jiang H, Shen J, Melcher K, Chen H, Jiang Y, Cheng X, Wang MW, Xie X, Xu HE | 10.1016/J.CELL.2022.09.041 | 2022-11-09 | 53741 | |
Gs | αs | Human | Mini-Gs | 55 | β1 | Human | γ2 | Human | Cryo-EM | 8F76 | 8F76_refined | 3.1 | O51E2 | Olfactory 51E2 | Olfactory | A (Rhodopsin) | Human | - | Nanobody-35 | - |
propanoic acid
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | - | - | Billesbolle CB, de March CA, van der Velden WJC, Ma N, Tewari J, Del Torrent CL, Li L, Faust B, Vaidehi N, Matsunami H, Manglik A | 10.1038/S41586-023-05798-Y | 2023-03-22 | 53739 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8HMV | 8HMV_refined | 2.9 | GPR21 | GPR21 | A orphans | A (Rhodopsin) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Wong TS, Gao W, Chen G, Qiu C, He G, Ye F, Wu Z, Zeng Z, Du Y | 10.1002/MCO2.205 | 2023-03-01 | 53739 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7XK2 | 7XK2_refined | 3.1 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | - | scFv16 | - |
MK 6892
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | Yang Y, Kang HJ, Gao R, Wang J, Han GW, DiBerto JF, Wu L, Tong J, Qu L, Wu Y, Pileski R, Li X, Zhang XC, Zhao S, Kenakin T, Wang Q, Stevens RC, Peng W, Roth BL, Rao Z, Liu ZJ | 10.1038/S41467-023-37177-6 | 2023-02-22 | 53741 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7Y1F | 7Y1F_refined | 3.3 | OPRK | κ | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
dynorphin A-(1-8)
pubchem
gtoplig
chembl_ligand
pubchem
pubchem
|
peptide | Agonist | [Leu]enkephalin, β-neoendorphin, β-endorphin, dynorphin A, [Met]enkephalin, α-neoendorphin, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13), big dynorphin | peptide | Chen Y, Chen B, Wu T, Zhou F, Xu F | 10.1093/PROCEL/PWAC033 | 2023-05-24 | 53741 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 8GUR | 8GUR_refined | 2.8 | CNR2 | CB2 | Cannabinoid | A (Rhodopsin) | Human | - | scFv16 | - |
CP55940
pubchem
gtoplig
chembl_ligand
gtoplig
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | Li X, Chang H, Bouma J, de Paus LV, Mukhopadhyay P, Paloczi J, Mustafa M, van der Horst C, Kumar SS, Wu L, Yu Y, van den Berg RJBHN, Janssen APA, Lichtman A, Liu ZJ, Pacher P, van der Stelt M, Heitman LH, Hua T | 10.1038/S41467-023-37112-9 | 2023-05-10 | 53741 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8J18 | - | 2.9 | GPR84 | GPR84 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
(3R)-3-HYDROXYDODECANOIC ACID
pubchem
|
small-molecule | Agonist | - | - | Liu H, Zhang Q, He X, Jiang M, Wang S, Yan X, Cheng X, Liu Y, Nan FJ, Xu HE, Xie X, Yin W | 10.1038/S41467-023-38985-6 | 2023-06-21 | 53741 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8JR9 | - | 2.6 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
PCO371
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | TIP39, PTHrP-(1-36), PTHrP, PTH | peptide | Zhao LH, He Q, Yuan Q, Gu Y, He X, Shan H, Li J, Wang K, Li Y, Hu W, Wu K, Shen J, Xu HE | 10.1038/S41586-023-06467-W | 2023-08-02 | 53739 | |
Gs | αs | Human | Gi1-Gs chimera | 60 | β1 | Human | γ2 | Bovine | Cryo-EM | 8INR | - | 2.7 | MC5R | MC5 | Melanocortin | A (Rhodopsin) | Human | - | - | - |
INTERMEDINE
chembl_ligand
pubchem
pubchem
pubchem
|
protein | Agonist | β-MSH, α-MSH, agouti-related protein, γ-MSH, ACTH | peptide | Chen VB, Arendall WB 3rd, Headd JJ, Keedy DA, Immormino RM, Kapral GJ, Murray LW, Richardson JS, Richardson DC | 10.1107/S0907444909042073 | 2023-09-20 | 53739 | |
Gs | αs | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8JLP | - | 3.2 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Human | - | - | - |
ralmitaront
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, dopamine | small-molecule | Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z | 10.1038/S41586-023-06804-Z | 2023-11-15 | 53739 | |
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 | 53739 | |
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 | 53739 | |
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 | 53739 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7E33 | 7E33_refined | 2.9 | 5HT1E | 5-HT1E | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | scFv16 | - |
BRL-54443
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | tryptamine, 5-hydroxytryptamine | small-molecule | Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen DD, Yen HY, Robinson CV, Harpsoe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE | 10.1038/S41586-021-03376-8 | 2021-04-14 | 53741 | |
Gs | αs | Human | - | 49 | β1 | Bovine | γ2 | Mouse | Cryo-EM | 7E14 | - | 2.9 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
N-Tert-butyl-6,7-dichloroquinoxalin-2-amine
pubchem
orforglipron pubchem gtoplig chembl_ligand |
small-molecule small-molecule |
Ago-PAM Agonist |
glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Cong Z, Chen LN, Ma H, Zhou Q, Zou X, Ye C, Dai A, Liu Q, Huang W, Sun X, Wang X, Xu P, Zhao L, Xia T, Zhong W, Yang D, Eric Xu H, Zhang Y, Wang MW | 10.1038/S41467-021-24058-Z | 2021-07-07 | 53739 | |
Gq/11 | αq | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7EZM | - | 2.9 | CCKAR | CCK1 | Cholecystokinin | A (Rhodopsin) | Human | - | scFv16 | - |
CCK-8
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
peptide | Agonist | desulfated cholecystokinin-8, CCK-58, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8 | peptide | Liu Q, Yang D, Zhuang Y, Croll TI, Cai X, Dai A, He X, Duan J, Yin W, Ye C, Zhou F, Wu B, Zhao Q, Xu HE, Wang MW, Jiang Y | 10.1038/S41589-021-00841-3 | 2021-08-25 | 53749 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7F53 | - | 3.0 | MC4R | MC4 | Melanocortin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
α-MSH
pubchem
gtoplig
|
peptide | Agonist | β-MSH, α-MSH, agouti-related protein, γ-MSH, ACTH | peptide | Zhang H, Chen LN, Yang D, Mao C, Shen Q, Feng W, Shen DD, Dai A, Xie S, Zhou Y, Qin J, Sun JP, Scharf DH, Hou T, Zhou T, Wang MW, Zhang Y | 10.1038/S41422-021-00552-3 | 2021-11-03 | 53739 | |
Gs | αs | Human | Gs-Gi1 chimera | 57 | β1 | Human | γ2 | Human | Cryo-EM | 7P02 | - | 2.9 | NK1R | NK1 | Tachykinin | A (Rhodopsin) | Human | - | scFv16 | - |
substance P
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
|
peptide | Agonist | neuropeptide-γ, neurokinin A, neuropeptide K, neurokinin B, hemokinin 1, substance P | peptide | Thom C, Ehrenmann J, Vacca S, Waltenspuhl Y, Schoppe J, Medalia O, Pluckthun A | 10.1126/SCIADV.ABK2872 | 2021-12-15 | 53739 | |
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 | 53739 | |
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 | 53783 | |
Gi/o | αi2 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7WVW | - | 3.1 | FPR2 | FPR2/ALX | Formylpeptide | A (Rhodopsin) | Human | BRIL | - | - |
FME-TYR-PHE-ILE-ASN-ILE-LEU-THE-LEU
|
peptide | Agonist | humanin, aspirin-triggered resolvin D1, LXA4, resolvin D1, serum amyloid A, PrP106-126, 15-deoxy-LXA4, aspirin triggered lipoxin A4, LL-37, LTC4, annexin I, fMet-Leu-Phe, LTD4 | peptide | Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B | 10.1038/S41467-022-29361-X | 2022-04-13 | 53742 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7EJX | - | 2.4 | GPR88 | GPR88 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
compound 2 [PMID: 24793972]
pubchem
gtoplig
chembl_ligand
|
small-molecule | Allosteric agonist | - | - | Chen G, Xu J, Inoue A, Schmidt MF, Bai C, Lu Q, Gmeiner P, Liu Z, Du Y | 10.1038/S41467-022-30081-5 | 2022-04-13 | 53741 | |
Gq/11 | αq | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7SR8 | - | 3.3 | OX2R | OX2 | Orexin | A (Rhodopsin) | Human | - | scFv16 | - |
methyl (2R,3S)-3-[(methanesulfonyl)amino]-2-({[(1s,4S)-4-phenylcyclohexyl]oxy}methyl)piperidine-1-carboxylate
pubchem
|
small-molecule | Agonist | orexin-A, orexin-B | peptide | Yin J, Kang Y, McGrath AP, Chapman K, Sjodt M, Kimura E, Okabe A, Koike T, Miyanohana Y, Shimizu Y, Rallabandi R, Lian P, Bai X, Flinspach M, De Brabander JK, Rosenbaum DM | 10.1038/S41467-022-30601-3 | 2022-06-08 | 53749 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7XTB | 7XTB_refined | 3.3 | 5HT6R | 5-HT6 | 5-Hydroxytryptamine | A (Rhodopsin) | Human | BRIL | Nanobody-35 | - |
5-hydroxytryptamine
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE | 10.1016/J.MOLCEL.2022.05.031 | 2022-07-27 | 53739 | |
Gs | αs | Human | Mini-Gs | 56 | β1 | Human | γ2 | Human | Cryo-EM | 7T9N | - | 2.9 | TSHR | TSH | Glycoprotein hormone | A (Rhodopsin) | Human | - |
M22 Fab light chain M22 Fab heavy chain Nanobody-35 |
- |
M22 antibody heavy chain
M22 antibody light chain |
protein protein |
Agonist | TSH | peptide | Faust B, Billesbolle CB, Suomivuori CM, Singh I, Zhang K, Hoppe N, Pinto AFM, Diedrich JK, Muftuoglu Y, Szkudlinski MW, Saghatelian A, Dror RO, Cheng Y, Manglik A | 10.1038/S41586-022-05159-1 | 2022-08-03 | 53739 | |
Gs | αs | Human | Engineered G protein | 50 | - | - | - | - | X-ray | 5G53 | - | 3.4 | AA2AR | A2A | Adenosine | A (Rhodopsin) | Human | - | - | - |
NECA
pubchem
gtoplig
chembl_ligand
gtoplig
|
small-molecule | Agonist | adenosine | small-molecule | Carpenter B, Nehme R, Warne T, Leslie AG, Tate CG | 10.1038/NATURE18966 | 2016-08-03 | 53739 | |
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 | 53741 | |
Gs | αs | Human | Fused partial Gs | 44 | - | - | - | - | X-ray | 6E67 | - | 3.7 | ADRB2 | β2 | Adrenoceptors | A (Rhodopsin) | Human | T4-Lysozyme | - | - |
CHEMBL1615159
chembl_ligand
pubchem
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline | small-molecule | Liu X, Xu X, Hilger D, Aschauer P, Tiemann JKS, Du Y, Liu H, Hirata K, Sun X, Guixa-Gonzalez R, Mathiesen JM, Hildebrand PW, Kobilka BK | 10.1016/J.CELL.2019.04.021 | 2019-06-05 | 53739 | |
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 | 53739 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7CFN | 7CFN_refined | 3.0 | GPBAR | GPBA | Bile acid | A (Rhodopsin) | Human | - | Nanobody-35 | - |
INT-777
pubchem
INT-777 pubchem |
small-molecule small-molecule |
Agonist PAM |
deoxycholic acid, cholic acid, chenodeoxycholic acid, lithocholic acid | small-molecule | - | - | 2020-09-09 | 53739 | |
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 | 53747 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7CRH | 7CRH_refined | 3.3 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
CHEMBL1416789
chembl_ligand
pubchem
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z | 10.1016/J.CELL.2021.01.028 | 2021-03-03 | 53739 | |
Gs | αs | Human | - | 54 | β1 | Human | γ2 | Human | Cryo-EM | 7BB6 | - | 4.2 | V2R | V2 | Vasopressin and oxytocin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
vasopressin
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
peptide | Agonist | vasopressin, oxytocin | peptide | Bous J, Orcel H, Floquet N, Leyrat C, Lai-Kee-Him J, Gaibelet G, Ancelin A, Saint-Paul J, Trapani S, Louet M, Sounier R, Demene H, Granier S, Bron P, Mouillac B | 10.1126/SCIADV.ABG5628 | 2021-06-02 | 53739 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7F1S | 7F1S_refined | 2.8 | CCR5 | CCR5 | Chemokine | A (Rhodopsin) | Human | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | CCL14, CCL8, CCL13, CCL4, CCL7, CCL2, CCL5, CCL11, CCL3, CCL16 | peptide | Zhang H, Chen K, Tan Q, Shao Q, Han S, Zhang C, Yi C, Chu X, Zhu Y, Xu Y, Zhao Q, Wu B | 10.1038/S41467-021-24438-5 | 2021-07-14 | 53741 | |
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 | 53741 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7EW7 | - | 3.3 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
SEW2871
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z | 10.1038/S41422-021-00566-X | 2021-09-29 | 53741 | |
Gi/o | αi1 | Mouse | - | 63 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7TD3 | - | 3.0 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | - | - |
sphingosine 1-phosphate
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY | 10.1038/S41467-022-28417-2 | 2022-02-09 | 53783 | |
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 | 53739 | |
Gq/11 | αq | Human | - | 54 | β1 | Human | γ2 | Human | Cryo-EM | 7W53 | - | 3.2 | NMUR1 | NMU1 | Neuromedin U | A (Rhodopsin) | Human | - | scFv16 | - |
Neuromedin U-25 (human)
pubchem
|
peptide | Agonist | neuromedin U-23, neuromedin S-36, neuromedin S-33, neuromedin U-25 | peptide | You C, Zhang Y, Xu P, Huang S, Yin W, Eric Xu H, Jiang Y | 10.1038/S41467-022-29683-W | 2022-04-20 | 53749 | |
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 | 53747 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7XW5 | - | 3.0 | TSHR | TSH | Glycoprotein hormone | A (Rhodopsin) | Human | - | Nanobody-35 | - |
Thyrotropin subunit beta
Glycoprotein hormones alpha chain N-[4-[[5-[(2S)-3-benzyl-5-hydroxy-4-oxo-1,2-dihydroquinazolin-2-yl]-2-methoxyphenyl]methoxy]phenyl]acetamide pubchem |
protein protein small-molecule |
Agonist | TSH | peptide | Duan J, Xu P, Luan X, Ji Y, He X, Song N, Yuan Q, Jin Y, Cheng X, Jiang H, Zheng J, Zhang S, Jiang Y, Xu HE | 10.1038/S41586-022-05173-3 | 2022-08-24 | 53739 | |
Gi/o | αi2 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7XXI | 7XXI_refined | 3.0 | P2Y12 | P2Y12 | P2Y | A (Rhodopsin) | Human | - | - | - |
2MeSADP
pubchem
gtoplig
chembl_ligand
gtoplig
|
small-molecule | Agonist | ADP, ATP | small-molecule | - | - | 2023-06-07 | 53742 | |
Gq/11 | αq | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8EJC | - | 3.0 | FFAR1 | FFA1 | Free fatty acid | A (Rhodopsin) | Human | - | scFv16 | - |
fasiglifam
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | myristic acid, oleic acid, α-linolenic acid, docosahexaenoic acid | small-molecule | Kumari P, Inoue A, Chapman K, Lian P, Rosenbaum DM | 10.1073/PNAS.2219569120 | 2023-05-24 | 53749 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8FLU | - | 2.8 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
PTH
|
peptide | Agonist | TIP39, PTHrP-(1-36), PTHrP, PTH | peptide | Cary BP, Gerrard EJ, Belousoff MJ, Fletcher MM, Jiang Y, Russell IC, Piper SJ, Wootten D, Sexton PM | 10.1016/J.STR.2023.04.002 | 2023-04-26 | 53739 | |
Gi/o | αi1 | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8IRU | - | 3.2 | DRD4 | D4 | Dopamine | A (Rhodopsin) | Human | - | scFv16 | - |
rotigotine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | dopamine | small-molecule | Xu P, Huang S, Krumm BE, Zhuang Y, Mao C, Zhang Y, Wang Y, Huang XP, Liu YF, He X, Li H, Yin W, Jiang Y, Zhang Y, Roth BL, Xu HE | 10.1038/S41422-023-00808-0 | 2023-06-21 | 53741 | |
Gq/11 | αq | Human | GRK2 bound | 88 | - | - | - | - | Cryo-EM | 8JPB | - | 3.1 | NTR1 | NTS1 | Neurotensin | A (Rhodopsin) | Human | - | GRK2 | GRK2 |
JMV431
gtoplig
chembl_ligand
pubchem
CHEMBL4576388 chembl_ligand pubchem |
peptide small-molecule |
Agonist PAM |
large neurotensin, large neuromedin N, neurotensin, neuromedin N | peptide | Duan J, Liu H, Zhao F, Yuan Q, Ji Y, Cai X, He X, Li X, Li J, Wu K, Gao T, Zhu S, Lin S, Wang MW, Cheng X, Yin W, Jiang Y, Yang D, Xu HE | 10.1038/S41586-023-06395-9 | 2023-08-09 | 53749 | |
Gi/o | αo | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8HPT | - | 3.4 | C5AR1 | C5a1 | Complement peptide | A (Rhodopsin) | Mouse | - | scFv16 | - |
C5a
|
peptide | Agonist | - | - | None | HTTPS://DOI.ORG/10.1016/J.CELL.2023.09.020 | 2023-10-18 | 53747 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8IJB | 8IJB_refined | 3.2 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | - | scFv16 | - |
5-Methyl-4-oxidanyl-pyrazin-4-ium-2-carboxylic acid
pubchem
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | Pan X, Ye F, Ning P, Zhang Z, Li X, Zhang B, Wang Q, Chen G, Gao W, Qiu C, Wu Z, Li J, Zhu L, Xia J, Gong K, Du Y | 10.1038/S41421-023-00610-7 | 2024-01-03 | 53741 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8KGK | 8KGK_refined | 3.2 | GPR61 | GPR61 | A orphans | A (Rhodopsin) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Nie Y, Qiu Z, Chen S, Chen Z, Song X, Ma Y, Huang N, Cyster JG, Zheng S | 10.1038/S41467-023-41654-3 | 2023-10-11 | 53739 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8W8B | - | 3.0 | 5HT1A | 5-HT1A | 5-Hydroxytryptamine | A (Rhodopsin) | Human | BRIL | scFv16 | - |
ulotaront
pubchem
gtoplig
drugbank
chembl_ligand
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Liu H, Zheng Y, Wang Y, Wang Y, He X, Xu P, Huang S, Yuan Q, Zhang X, Wang L, Jiang K, Chen H, Li Z, Liu W, Wang S, Xu HE, Xu F | 10.1038/S41586-023-06775-1 | 2023-11-22 | 53741 | |
Gs | αs | Bovine | - | 58 | β1 | Rat | γ2 | Bovine | Cryo-EM | 6NBF | - | 3.0 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
Long-acting parathyroid hormone analog
|
peptide | Agonist | TIP39, PTHrP-(1-36), PTHrP, PTH | peptide | Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y | 10.1126/SCIENCE.AAV7942 | 2019-04-17 | 53756 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 6VMS | - | 3.8 | DRD2 | D2 | Dopamine | A (Rhodopsin) | Human | T4-Lysozyme | scFv16 | - |
bromocriptine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | dopamine | small-molecule | Yin J, Chen KM, Clark MJ, Hijazi M, Kumari P, Bai XC, Sunahara RK, Barth P, Rosenbaum DM | 10.1038/S41586-020-2379-5 | 2020-06-17 | 53741 | |
Gs | αs | Human | - | 49 | β1 | Human | γ2 | Human | Cryo-EM | 7C2E | - | 4.2 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
2-[[4-[6-[(4-cyano-2-fluoranyl-phenyl)methoxy]pyridin-2-yl]-3,6-dihydro-2~{H}-pyridin-1-yl]methyl]-3-[[(2~{S})-oxetan-2-yl]methyl]imidazo[4,5-b]pyridine-5-carboxylic acid
pubchem
|
small-molecule | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Ma H, Huang W, Wang X, Zhao L, Jiang Y, Liu F, Guo W, Sun X, Zhong W, Yuan D, Xu HE | 10.1038/S41422-020-0384-8 | 2020-08-26 | 53739 | |
Gs | αs | Human | Engineered G alpha | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7L1V | - | 3.0 | OX2R | OX2 | Orexin | A (Rhodopsin) | Human | - |
scFv16 Nanobody-51 |
- |
compound 1 [PMID: 33547286]
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | orexin-A, orexin-B | peptide | Hong C, Byrne NJ, Zamlynny B, Tummala S, Xiao L, Shipman JM, Partridge AT, Minnick C, Breslin MJ, Rudd MT, Stachel SJ, Rada VL, Kern JC, Armacost KA, Hollingsworth SA, O'Brien JA, Hall DL, McDonald TP, Strickland C, Brooun A, Soisson SM, Hollenstein K | 10.1038/S41467-021-21087-6 | 2021-02-10 | 53739 | |
Gs | αs | Human | - | 86 | β1 | Human | γ2 | Human | X-ray | 7JOZ | 7JOZ_refined | 3.8 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
CHEMBL4453318
chembl_ligand
pubchem
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | Sun B, Feng D, Chu ML, Fish I, Lovera S, Sands ZA, Kelm S, Valade A, Wood M, Ceska T, Kobilka TS, Lebon F, Kobilka BK | 10.1038/S41467-021-23519-9 | 2021-04-14 | 53739 | |
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 | 53741 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7S8O | - | 2.6 | MRGX2 | MRGPRX2 | A orphans | A (Rhodopsin) | Human | BRIL | scFv16 | - |
(R)-ZINC-3573
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | PAMP-20 | peptide | Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL | 10.1038/S41586-021-04126-6 | 2021-11-17 | 53741 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7VUG | 7VUG_refined | 3.2 | GP139 | GPR139 | A orphans | A (Rhodopsin) | Human | - | scFv16 | Xylanase |
JNJ-63533054
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | L-phenylalanine, L-tryptophan | small-molecule | Zhou Y, Daver H, Trapkov B, Wu L, Wu M, Harpsoe K, Gentry PR, Liu K, Larionova M, Liu J, Chen N, Brauner-Osborne H, Gloriam DE, Hua T, Liu ZJ | 10.1038/S41422-021-00591-W | 2021-12-29 | 53741 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7F4H | - | 2.7 | MSHR | MC1 | Melanocortin | A (Rhodopsin) | Human | - |
Nanobody-35 scFv16 |
- |
CHEMBL407070
chembl_ligand
pubchem
pubchem
|
protein | Agonist | β-MSH, ACTH, γ-MSH, α-MSH | peptide | Ma S, Chen Y, Dai A, Yin W, Guo J, Yang D, Zhou F, Jiang Y, Wang MW, Xu HE | 10.1038/S41422-021-00557-Y | 2021-09-08 | 53739 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7TYW | - | 3.0 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - | Nanobody-35 | - |
calcitonin (salmon synthetic)
pubchem
|
small-molecule | Agonist | adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP | peptide | Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM | 10.1126/SCIENCE.ABM9609 | 2022-03-23 | 53739 | |
Gs | αs | Human | Mini-Gs | 54 | β1 | Human | γ2 | Human | Cryo-EM | 7WU3 | - | 3.1 | AGRF1 | ADGRF1 | ADGRF | B2 (Adhesion) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Qu X, Qiu N, Wang M, Zhang B, Du J, Zhong Z, Xu W, Chu X, Ma L, Yi C, Han S, Shui W, Zhao Q, Wu B | 10.1038/S41586-022-04580-W | 2022-04-27 | 53739 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7EUO | 7EUO_refined | 2.9 | FPR1 | FPR1 | Formylpeptide | A (Rhodopsin) | Human | - | scFv16 | - |
Peptide Agonist fMLF
|
peptide | Agonist | fMet-Leu-Phe, cathepsin G, annexin I, spinorphin | peptide | Chen G, Wang X, Liao Q, Ge Y, Jiao H, Chen Q, Liu Y, Lyu W, Zhu L, van Zundert GCP, Robertson MJ, Skiniotis G, Du Y, Hu H, Ye RD | 10.1038/S41467-022-32822-Y | 2022-05-25 | 53741 | |
Gi/o | αo | Human | Mini-Go | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7UM6 | - | 2.8 | 5HT5A | 5-HT5A | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | scFv16 | - |
lisuride
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL | 10.1038/S41594-022-00796-6 | 2022-07-20 | 53747 | |
Gq/11 | αq | Human | Mini-Gq | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8E9Z | - | 2.7 | ACM3 | M3 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | scFv16 | - |
iperoxo
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | acetylcholine | small-molecule | Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL | 10.1038/S41586-022-05489-0 | 2022-11-30 | 53749 | |
Gi/o | αi2 | Human | - | 59 | β1 | Human | γ2 | Bovine | Cryo-EM | 7YK6 | 7YK6_refined | 3.0 | RL3R2 | RXFP4 | Relaxin family peptide | A (Rhodopsin) | Human | - | scFv16 | - |
CHEMBL4522365
chembl_ligand
pubchem
|
small-molecule | Agonist | INSL5, relaxin-3 (B chain), relaxin-3 | peptide | Chen Y, Zhou Q, Wang J, Xu Y, Wang Y, Yan J, Wang Y, Zhu Q, Zhao F, Li C, Chen CW, Cai X, Bathgate RAD, Shen C, Eric Xu H, Yang D, Liu H, Wang MW | 10.1038/S41467-023-36182-Z | 2023-03-01 | 53742 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 8ID8 | - | 3.0 | FFAR4 | FFA4 | Free fatty acid | A (Rhodopsin) | Human | - | scFv16 | - |
TUG-891
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | myristic acid, linoleic acid, α-linolenic acid, oleic acid | small-molecule | Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP | 10.1126/SCIENCE.ADD6220 | 2023-03-15 | 53741 | |
Gq/11 | αq | Human | Gs-mini-Gq chimera | 52 | β1 | Human | γ2 | Human | Cryo-EM | 8G2Y | - | 3.4 | AGRF1 | ADGRF1 | ADGRF | B2 (Adhesion) | Human | - | Nanobody-35 | - |
[1-Myristoyl-glycerol-3-YL]phosphonylcholine
pubchem
|
small-molecule | Agonist | - | - | Jones DTD, Dates AN, Rawson SD, Burruss MM, Lipper CH, Blacklow SC | 10.1038/S41467-023-38083-7 | 2023-05-10 | 53749 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7YAE | 7YAE_refined | 3.4 | SSR2 | SST2 | Somatostatin | A (Rhodopsin) | Human | - | scFv16 | - |
Octreotide
|
peptide | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | Zhao J, Fu H, Yu J, Hong W, Tian X, Qi J, Sun S, Zhao C, Wu C, Xu Z, Cheng L, Chai R, Yan W, Wei X, Shao Z | 10.1038/S41467-023-36673-Z | 2023-04-19 | 53741 | |
Gq/11 | α11 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7XXH | 7XXH_refined | 2.9 | P2RY1 | P2Y1 | P2Y | A (Rhodopsin) | Human | - | scFv16 | - |
2MeSADP
pubchem
gtoplig
chembl_ligand
gtoplig
|
small-molecule | Agonist | ADP, ATP | small-molecule | - | - | 2023-06-07 | 53750 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8F0J | - | 2.0 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - | Nanobody-35 | - |
Pramlintide analogue San45
|
peptide | Agonist | adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP | peptide | Cao J, Belousoff MJ, Gerrard E, Danev R, Fletcher MM, Dal Maso E, Schreuder H, Lorenz K, Evers A, Tiwari G, Besenius M, Li Z, Johnson RM, Wootten D, Sexton PM | 10.1038/S41589-023-01393-4 | 2023-08-02 | 53739 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8GDB | 8GDB_refined | 3.1 | PE2R4 | EP4 | Prostanoid | A (Rhodopsin) | Human | - | - | - |
PGE2
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
|
small-molecule | Agonist | thromboxane A2, PGF2α, PGI2, PGD2, PGE1, PGE2 | small-molecule | Huang SM, Xiong MY, Liu L, Mu J, Wang MW, Jia YL, Cai K, Tie L, Zhang C, Cao S, Wen X, Wang JL, Guo SC, Li Y, Qu CX, He QT, Cai BY, Xue C, Gan S, Xie Y, Cong X, Yang Z, Kong W, Li S, Li Z, Xiao P, Yang F, Yu X, Guan YF, Zhang X, Liu Z, Yang BX, Du Y, Sun JP | 10.1073/PNAS.2216329120 | 2024-01-10 | 53739 | |
Gi/o | αo | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8I9L | - | 3.2 | C3AR | C3a | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
C3a anaphylatoxin
pubchem
|
peptide | Agonist | C5a, C3a | peptide | Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C | 10.1016/J.CELL.2023.09.020 | 2023-10-18 | 53747 | |
Gi/o | αi1 | Human | - | 65 | β1 | Human | γ2 | Human | Cryo-EM | 6LFO | 6LFO_refined | 3.4 | CXCR2 | CXCR2 | Chemokine | A (Rhodopsin) | Human | - | scFv16 | - |
Interleukin-8
pubchem
|
protein | Agonist | CXCL8, CXCL1, CXCL5, CXCL2, CXCL7, CXCL6, CXCL3 | peptide | Liu K, Wu L, Yuan S, Wu M, Xu Y, Sun Q, Li S, Zhao S, Hua T, Liu ZJ | 10.1038/S41586-020-2492-5 | 2020-09-02 | 53741 | |
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 | neuropeptide-γ, neurokinin A, neuropeptide K, neurokinin B, hemokinin 1, substance P | peptide | Thom C, Ehrenmann J, Vacca S, Waltenspuhl Y, Schoppe J, Medalia O, Pluckthun A | 10.1126/SCIADV.ABK2872 | 2021-12-15 | 53749 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7EW0 | 7EW0_refined | 3.4 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
ozanimod
pubchem
gtoplig
drug_central
chembl_ligand
drugbank
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z | 10.1038/S41422-021-00566-X | 2021-09-29 | 53741 | |
Gi/o | αi1 | Mouse | - | 63 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7TD4 | - | 2.6 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | - | - |
siponimod
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY | 10.1038/S41467-022-28417-2 | 2022-02-09 | 53783 | |
Gs | αs | Human | Mini-Gs | 58 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7VBI | - | 3.0 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | - | - |
tirzepatide
pubchem
gtoplig
|
peptide | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW | 10.1038/S41467-022-28683-0 | 2022-03-02 | 53739 | |
Gi/o | αi1 | Human | - | 63 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7S0F | - | 3.0 | ADRB1 | β1 | Adrenoceptors | A (Rhodopsin) | Wild turkey | - | - | - |
LEVISOPRENALINE
chembl_ligand
chembl_ligand
pubchem
|
small-molecule | Agonist | - | - | Alegre KO, Paknejad N, Su M, Lou JS, Huang J, Jordan KD, Eng ET, Meyerson JR, Hite RK, Huang XY | 10.1038/S41594-021-00679-2 | 2021-11-17 | 53741 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7F1O | - | 3.1 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
dopamine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | Teng X, Chen S, Wang Q, Chen Z, Wang X, Huang N, Zheng S | 10.1126/SCIADV.ABO4158 | 2022-06-15 | 53739 | |
Gq/11 | αq | Human | Gi2-mini-Gq chimera | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7RAN | - | 3.5 | 5HT2A | 5-HT2A | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | scFv16 | - |
3-[(3R)-3-methyl-1,2,3,6-tetrahydropyridin-1-ium-5-yl]-1H-pyrrolo[2,3-b]pyridine
pubchem
|
small-molecule | Agonist | tryptamine, 5-hydroxytryptamine | small-molecule | Kaplan AL, Confair DN, Kim K, Barros-Alvarez X, Rodriguiz RM, Yang Y, Kweon OS, Che T, McCorvy JD, Kamber DN, Phelan JP, Martins LC, Pogorelov VM, DiBerto JF, Slocum ST, Huang XP, Kumar JM, Robertson MJ, Panova O, Seven AB, Wetsel AQ, Wetsel WC, Irwin JJ, Skiniotis G, Shoichet BK, Roth BL, Ellman JA | 10.1038/S41586-022-05258-Z | 2022-07-06 | 53749 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7XBW | 7XBW_refined | 2.8 | CX3C1 | CX3CR1 | Chemokine | A (Rhodopsin) | Human | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | CX3CL1 | peptide | Lu M, Zhao W, Han S, Lin X, Xu T, Tan Q, Wang M, Yi C, Chu X, Yang W, Zhu Y, Wu B, Zhao Q | 10.1126/SCIADV.ABN8048 | 2022-07-13 | 53741 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7XMS | - | 2.9 | SSR4 | SST4 | Somatostatin | A (Rhodopsin) | Human | - | scFv16 | - |
SOMATOSTATIN
chembl_ligand
pubchem
|
protein | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | Zhao W, Han S, Qiu N, Feng W, Lu M, Zhang W, Wang M, Zhou Q, Chen S, Xu W, Du J, Chu X, Yi C, Dai A, Hu L, Shen MY, Sun Y, Zhang Q, Ma Y, Zhong W, Yang D, Wang MW, Wu B, Zhao Q | 10.1038/S41422-022-00679-X | 2022-08-03 | 53741 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7T2G | - | 2.5 | OPRM | μ | Opioid | A (Rhodopsin) | Mouse | BRIL | - | - |
CHEMBL58362
chembl_ligand
pubchem
|
small-molecule | Agonist | - | - | Qu Q, Huang W, Aydin D, Paggi JM, Seven AB, Wang H, Chakraborty S, Che T, DiBerto JF, Robertson MJ, Inoue A, Suomivuori CM, Roth BL, Majumdar S, Dror RO, Kobilka BK, Skiniotis G | 10.1038/S41589-022-01208-Y | 2022-12-07 | 53741 | |
Gs | αs | Human | Mini-Gs | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7WY8 | - | 2.8 | AGRL3 | ADGRL3 | ADGRL | B2 (Adhesion) | Mouse | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Qian Y, Ma Z, Liu C, Li X, Zhu X, Wang N, Xu Z, Xia R, Liang J, Duan Y, Yin H, Xiong Y, Zhang A, Guo C, Chen Z, Huang Z, He Y | 10.1016/J.MOLCEL.2022.10.009 | 2022-10-26 | 53739 | |
Gi/o | αi1 | Human | - | 63 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7YU6 | 7YU6_refined | 3.5 | LPAR1 | LPA1 | Lysophospholipid (LPA) | A (Rhodopsin) | Human | - | scFv16 | - |
[(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate
pubchem
|
small-molecule | Agonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O | 10.1038/S41467-022-33121-2 | 2022-10-05 | 53741 | |
Gi/o | αi1 | Human | - | 64 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8F7W | 8F7W_refined | 3.2 | OPRK | κ | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
dynorphin A-(1-8)
pubchem
gtoplig
chembl_ligand
pubchem
pubchem
|
peptide | Agonist | [Leu]enkephalin, β-neoendorphin, β-endorphin, dynorphin A, [Met]enkephalin, α-neoendorphin, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13), big dynorphin | peptide | Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y, Roth BL, Xu HE | 10.1016/J.CELL.2022.12.026 | 2022-12-14 | 53741 | |
Gs | αs | Human | Mini-Gs | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8HDO | - | 2.9 | AA2BR | A2B | Adenosine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
BAY 60-6583
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | adenosine | small-molecule | Cai H, Xu Y, Guo S, He X, Sun J, Li X, Li C, Yin W, Cheng X, Jiang H, Xu HE, Xie X, Jiang Y | 10.1038/S41421-022-00503-1 | 2023-01-18 | 53739 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7XV3 | 7XV3_refined | 2.8 | GP174 | GPR174 | A orphans | A (Rhodopsin) | Human | - | - | - |
(2~{S})-2-$l^{4}-azanyl-3-[[(2~{R})-3-octadecanoyloxy-2-oxidanyl-propoxy]-oxidanyl-oxidanylidene-$l^{6}-phosphanyl]oxy-propanoic acid
pubchem
|
small-molecule | Agonist | lysophosphatidylserine | small-molecule | Liang J, Inoue A, Ikuta T, Xia R, Wang N, Kawakami K, Xu Z, Qian Y, Zhu X, Zhang A, Guo C, Huang Z, He Y | 10.1038/S41467-023-36575-0 | 2023-02-15 | 53739 | |
Gi/o | αz | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8DZS | - | 2.7 | OPRK | κ | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
CHEMBL277863
chembl_ligand
pubchem
|
small-molecule | Agonist | [Leu]enkephalin, β-neoendorphin, β-endorphin, dynorphin A, [Met]enkephalin, α-neoendorphin, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13), big dynorphin | peptide | Han J, Zhang J, Nazarova AL, Bernhard SM, Krumm BE, Zhao L, Lam JH, Rangari VA, Majumdar S, Nichols DE, Katritch V, Yuan P, Fay JF, Che T | 10.1038/S41586-023-06030-7 | 2023-05-03 | 53748 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7TRP | - | 2.4 | ACM4 | M4 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | scFv16 | - |
iperoxo
pubchem
gtoplig
chembl_ligand
LY2033298 pubchem gtoplig chembl_ligand |
small-molecule small-molecule |
Agonist PAM |
acetylcholine | small-molecule | - | - | 2023-05-17 | 53741 | |
Gq/11 | αq | Human | - | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8H0P | - | 3.2 | NMBR | BB1 | Bombesin | A (Rhodopsin) | Human | - | scFv16 | - |
NMB30
|
peptide | Agonist | neuromedin B, gastrin releasing peptide(14-27) (human), GRP-(18-27), gastrin-releasing peptide | peptide | Li C, Xu Y, Liu H, Cai H, Jiang Y, Xu HE, Yin W | 10.1038/S41422-022-00743-6 | 2023-08-09 | 53749 | |
Gq/11 | αq | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7YFC | - | 3.0 | HRH4 | H4 | Histamine | A (Rhodopsin) | Human | - |
scFv16 Nanobody-35 |
- |
histamine
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
gtoplig
|
small-molecule | Agonist | histamine, CCL16 | small-molecule | Im D, Kishikawa JI, Shiimura Y, Hisano H, Ito A, Fujita-Fujiharu Y, Sugita Y, Noda T, Kato T, Asada H, Iwata S | 10.1038/S41467-023-42260-Z | 2023-10-25 | 53749 | |
Gs | αs | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8HJ1 | 8HJ1_refined | 3.3 | GPR21 | GPR21 | A orphans | A (Rhodopsin) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Lin X, Chen B, Wu Y, Han Y, Qi A, Wang J, Yang Z, Wei X, Zhao T, Wu L, Xie X, Sun J, Zheng J, Zhao S, Xu F | 10.1038/S41467-023-35882-W | 2023-12-27 | 53739 | |
Gi/o | αo | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8I9S | 8I9S_refined | 3.3 | C3AR | C3a | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | C5a, C3a | peptide | Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C | 10.1016/J.CELL.2023.09.020 | 2023-10-18 | 53747 | |
Gi/o | αo | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8J6D | 8J6D_refined | 3.1 | C3AR | C3a | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
EP141 peptide agonist
|
peptide | Agonist | C5a, C3a | peptide | Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C | 10.1016/J.CELL.2023.09.020 | 2023-10-18 | 53747 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8JSP | - | 3.7 | 5HT1A | 5-HT1A | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | scFv16 | - |
ulotaront
pubchem
gtoplig
drugbank
chembl_ligand
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z | 10.1038/S41586-023-06804-Z | 2023-11-15 | 53741 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8W89 | - | 3.0 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
2-Phenylethanaminium
pubchem
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, dopamine | small-molecule | Liu H, Zheng Y, Wang Y, Wang Y, He X, Xu P, Huang S, Yuan Q, Zhang X, Wang L, Jiang K, Chen H, Li Z, Liu W, Wang S, Xu HE, Xu F | 10.1038/S41586-023-06775-1 | 2023-11-22 | 53739 | |
Gi/o | αi1 | Human | - | 62 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8XBH | 8XBH_refined | 2.8 | GPR34 | GPR34 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
CHEMBL4758243
chembl_ligand
pubchem
|
small-molecule | Agonist | lysophosphatidylserine | small-molecule | - | - | 2023-12-27 | 53741 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 6KPF | 6KPF_refined | 2.9 | CNR2 | CB2 | Cannabinoid | A (Rhodopsin) | Human | - | scFv16 | - |
AM12033
pubchem
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | Hua T, Li X, Wu L, Iliopoulos-Tsoutsouvas C, Wang Y, Wu M, Shen L, Brust CA, Nikas SP, Song F, Song X, Yuan S, Sun Q, Wu Y, Jiang S, Grim TW, Benchama O, Stahl EL, Zvonok N, Zhao S, Bohn LM, Makriyannis A, Liu ZJ | 10.1016/J.CELL.2020.01.008 | 2020-02-12 | 53741 | |
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 | 53739 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7CMU | - | 3.0 | DRD3 | D3 | Dopamine | A (Rhodopsin) | Human | BRIL | scFv16 | - |
pramipexole
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | dopamine | small-molecule | Xu P, Huang S, Mao C, Krumm BE, Zhou XE, Tan Y, Huang XP, Liu Y, Shen DD, Jiang Y, Yu X, Jiang H, Melcher K, Roth BL, Cheng X, Zhang Y, Xu HE | 10.1016/J.MOLCEL.2021.01.003 | 2021-03-10 | 53741 | |
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-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Cong Z, Chen LN, Ma H, Zhou Q, Zou X, Ye C, Dai A, Liu Q, Huang W, Sun X, Wang X, Xu P, Zhao L, Xia T, Zhong W, Yang D, Eric Xu H, Zhang Y, Wang MW | 10.1038/S41467-021-24058-Z | 2021-08-11 | 53739 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7EW1 | 7EW1_refined | 3.4 | S1PR5 | S1P5 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
siponimod
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z | 10.1038/S41422-021-00566-X | 2021-09-29 | 53741 | |
Gs | αs | Human | - | 46 | β1 | Rat | γ2 | Mouse | Cryo-EM | 7PIV | 7PIV_refined | 2.9 | MC4R | MC4 | Melanocortin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
afamelanotide
pubchem
gtoplig
chembl_ligand
drugbank
pubchem
pubchem
pubchem
pubchem
|
peptide | Agonist | β-MSH, α-MSH, agouti-related protein, γ-MSH, ACTH | peptide | Heyder NA, Kleinau G, Speck D, Schmidt A, Paisdzior S, Szczepek M, Bauer B, Koch A, Gallandi M, Kwiatkowski D, Burger J, Mielke T, Beck-Sickinger AG, Hildebrand PW, Spahn CMT, Hilger D, Schacherl M, Biebermann H, Hilal T, Kuhnen P, Kobilka BK, Scheerer P | 10.1038/S41422-021-00569-8 | 2021-11-17 | 53739 | |
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-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Cary BP, Deganutti G, Zhao P, Truong TT, Piper SJ, Liu X, Belousoff MJ, Danev R, Sexton PM, Wootten D, Gellman SH | 10.1038/S41589-021-00945-W | 2022-01-05 | 53739 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7EVY | - | 3.0 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
siponimod
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z | 10.1038/S41422-021-00566-X | 2021-09-29 | 53741 | |
Gi/o | αi1 | Mouse | - | 62 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7TD2 | - | 3.1 | LPAR1 | LPA1 | Lysophospholipid (LPA) | A (Rhodopsin) | Human | - | - | - |
lysophosphatidic acid
pubchem
|
small-molecule | Agonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY | 10.1038/S41467-022-28417-2 | 2022-02-09 | 53783 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7WVU | 7WVU_refined | 3.3 | FPR1 | FPR1 | Formylpeptide | A (Rhodopsin) | Human | - | - | - |
FME-LEU-PHE
|
peptide | Agonist | fMet-Leu-Phe, cathepsin G, annexin I, spinorphin | peptide | Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B | 10.1038/S41467-022-29361-X | 2022-04-13 | 53741 | |
Gs | αs | Human | Mini-Gs | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7WUJ | - | 3.3 | AGRG4 | ADGRG4 | ADGRG | B2 (Adhesion) | Human | - |
scFv16 Nanobody-35 |
- |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | - | - | 2022-04-27 | 53739 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7X9C | 7X9C_refined | 3.0 | NPY4R | Y4 | Neuropeptide Y | A (Rhodopsin) | Human | - | - | - |
Pancreatic polypeptide
pubchem
|
peptide | Agonist | peptide YY, neuropeptide Y, PYY-(3-36), pancreatic polypeptide | peptide | Tang T, Tan Q, Han S, Diemar A, Lobner K, Wang H, Schuss C, Behr V, Morl K, Wang M, Chu X, Yi C, Keller M, Kofoed J, Reedtz-Runge S, Kaiser A, Beck-Sickinger AG, Zhao Q, Wu B | 10.1126/SCIADV.ABM1232 | 2022-05-18 | 53741 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7W0L | 7W0L_refined | 3.6 | APJ | apelin | Apelin | A (Rhodopsin) | Human | BRIL | scFv16 | - |
(1R,2S)-N-[4-(2,6-dimethoxyphenyl)-5-(6-methylpyridin-2-yl)-1,2,4-triazol-3-yl]-1-(5-methylpyrimidin-2-yl)-1-oxidanyl-propane-2-sulfonamide
pubchem
|
small-molecule | Agonist | Elabela/Toddler-21, apelin-17, [Pyr1]apelin-13, Elabela/Toddler-11, Elabela/Toddler-32, apelin-13, apelin-36, apelin receptor early endogenous ligand | peptide | Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F | 10.1038/S41594-022-00797-5 | 2022-07-27 | 53741 | |
Gs | αs | Bovine | - | 51 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 8DCR | - | 2.6 | ADRB1 | β1 | Adrenoceptors | A (Rhodopsin) | Wild turkey | T4-Lysozyme | Nanobody-35 | - |
Dobutamine
pubchem
|
small-molecule | Agonist | - | - | Su M, Paknejad N, Zhu L, Wang J, Do HN, Miao Y, Liu W, Hite RK, Huang XY | 10.1038/S41467-022-31823-1 | 2022-07-27 | 53756 | |
Gs | αs | Human | - | 58 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7VVL | 7VVL_refined | 2.8 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
teriparatide
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
pubchem
pubchem
pubchem
pubchem
pubchem
|
peptide | Agonist | TIP39, PTHrP-(1-36), PTHrP, PTH | peptide | Kobayashi K, Kawakami K, Kusakizako T, Miyauchi H, Tomita A, Kobayashi K, Shihoya W, Yamashita K, Nishizawa T, Kato HE, Inoue A, Nureki O | 10.1016/J.MOLCEL.2022.07.003 | 2022-08-03 | 53739 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7WCM | 7WCM_refined | 2.3 | GP119 | GPR119 | GPR18, GPR55 and GPR119 | A (Rhodopsin) | Human | - | Nanobody-35 | - |
MBX-2982
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | N-oleoylethanolamide, anandamide, N-palmitoylethanolamine, SEA | small-molecule | Qian Y, Wang J, Yang L, Liu Y, Wang L, Liu W, Lin Y, Yang H, Ma L, Ye S, Wu S, Qiao A | 10.1038/S41467-022-34696-6 | 2022-12-21 | 53739 | |
Gi/o | αgust | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7XP5 | - | 3.1 | T2R46 | TAS2R46 | Taste 2 | T (Taste 2) | Human | - | Nanobody-35 | Endoglucanase H |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Xu W, Wu L, Liu S, Liu X, Cao X, Zhou C, Zhang J, Fu Y, Guo Y, Wu Y, Tan Q, Wang L, Liu J, Jiang L, Fan Z, Pei Y, Yu J, Cheng J, Zhao S, Hao X, Liu ZJ, Hua T | 10.1126/SCIENCE.ABO1633 | 2022-10-12 | 53746 | |
Gq/11 | αq | Human | Mini-Gq | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8E9W | - | 2.7 | ACM3 | M3 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | scFv16 | - |
CHEMBL73538
chembl_ligand
pubchem
|
small-molecule | Agonist | acetylcholine | small-molecule | Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL | 10.1038/S41586-022-05489-0 | 2022-11-30 | 53749 | |
Gi/o | αi2 | Human | - | 61 | β1 | Human | γ2 | Bovine | Cryo-EM | 7YK7 | 7YK7_refined | 2.8 | RL3R2 | RXFP4 | Relaxin family peptide | A (Rhodopsin) | Human | - | scFv16 | - |
DC591053
pubchem
gtoplig
|
small-molecule | Agonist | INSL5, relaxin-3 (B chain), relaxin-3 | peptide | Chen Y, Zhou Q, Wang J, Xu Y, Wang Y, Yan J, Wang Y, Zhu Q, Zhao F, Li C, Chen CW, Cai X, Bathgate RAD, Shen C, Eric Xu H, Yang D, Liu H, Wang MW | 10.1038/S41467-023-36182-Z | 2023-03-01 | 53742 | |
Gq/11 | αq | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8G59 | 8G59_refined | 2.6 | FFAR4 | FFA4 | Free fatty acid | A (Rhodopsin) | Human | - | - | - |
TUG-891
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | myristic acid, linoleic acid, α-linolenic acid, oleic acid | small-molecule | Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP | 10.1126/SCIENCE.ADD6220 | 2023-03-08 | 53749 | |
Gi/o | αo | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7T90 | 7T90_refined | 3.3 | ACM2 | M2 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | scFv16 | - |
acetylcholine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
|
small-molecule | Agonist | acetylcholine | small-molecule | - | - | 2023-01-25 | 53747 | |
Gq/11 | αq | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8HJ5 | 8HJ5_refined | 3.0 | MRGX1 | MRGPRX1 | A orphans | A (Rhodopsin) | Human | BRIL |
scFv16 Nanobody-35 |
- |
compound 16 [PMID: 31498617]
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | bovine adrenal medulla peptide 8-22 | peptide | - | - | 2023-05-31 | 53749 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8IRV | 8IRV_refined | 3.1 | DRD5 | D5 | Dopamine | A (Rhodopsin) | Human | BRIL | - | - |
rotigotine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | Xu P, Huang S, Krumm BE, Zhuang Y, Mao C, Zhang Y, Wang Y, Huang XP, Liu YF, He X, Li H, Yin W, Jiang Y, Zhang Y, Roth BL, Xu HE | 10.1038/S41422-023-00808-0 | 2023-06-07 | 53739 | |
Gs | αs | Human | Mini-Gs | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7YDP | - | 3.1 | AGRE5 | ADGRE5 | ADGRE | B2 (Adhesion) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Wang N, Qian Y, Xia R, Zhu X, Xiong Y, Zhang A, Guo C, He Y | 10.1016/J.CHEMBIOL.2023.08.003 | 2023-07-12 | 53739 | |
Gi/o | αi1 | Human | - | 62 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8IY5 | - | 2.8 | EDNRB | ETB | Endothelin | A (Rhodopsin) | Human | - | scFv16 | - |
ENDOTHELIN
chembl_ligand
pubchem
|
protein | Agonist | endothelin-1, endothelin-2, endothelin-3 | peptide | Sano FK, Akasaka H, Shihoya W, Nureki O | 10.7554/ELIFE.85821 | 2023-08-16 | 53741 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8HNM | - | 2.9 | CXCR3 | CXCR3 | Chemokine | A (Rhodopsin) | Human | - | scFv16 | - |
CHEMBL2220409
chembl_ligand
chembl_ligand
pubchem
|
small-molecule | Agonist | CCL19, CXCL11, CCL13, CXCL9, CXCL10, CCL7, CCL5, CCL11, CXCL12α, CCL20 | peptide | Jiao H, Pang B, Liu A, Chen Q, Pan Q, Wang X, Xu Y, Chiang YC, Ren R, Hu H | 10.1038/S41594-023-01175-5 | 2023-11-29 | 53741 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8IJD | - | 3.3 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | - | scFv16 | - |
MK 6892
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | Pan X, Ye F, Ning P, Zhang Z, Li X, Zhang B, Wang Q, Chen G, Gao W, Qiu C, Wu Z, Li J, Zhu L, Xia J, Gong K, Du Y | 10.1038/S41421-023-00610-7 | 2024-01-03 | 53741 | |
Gs | αs | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8JLN | - | 3.2 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Human | BRIL | scFv16 | - |
CHEMBL1182312
chembl_ligand
chembl_ligand
pubchem
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, dopamine | small-molecule | Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z | 10.1038/S41586-023-06804-Z | 2023-11-15 | 53739 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8SG1 | - | 2.9 | CML1 | chemerin | Chemerin receptor | A (Rhodopsin) | Human | - | scFv16 | - |
chemerin C-terminal peptide
pubchem
gtoplig
chembl_ligand
pubchem
|
peptide | Agonist | 18R-HEPE, chemerin C-terminal peptide, EPA, resolvin E1, chemerin | peptide | Zhang X, Weiss T, Cheng MH, Chen S, Ambrosius CK, Czerniak AS, Li K, Feng M, Bahar I, Beck-Sickinger AG, Zhang C | 10.1371/JOURNAL.PBIO.3002188 | 2023-11-01 | 53741 | |
Gq/11 | αq | Human | Gi2-mini-Gq chimera | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8WPU | - | 3.1 | CASR | CaS | Calcium-sensing | C (Glutamate) | Human | - | scFv16 | - |
cinacalcet
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
Calcium pubchem |
small-molecule small-molecule |
Agonist | Mg2+, L-tryptophan, spermine, Ca2+ | small-molecule | Ling S, Meng X, Zhang Y, Xia Z, Zhou Y, Yang F, Shi P, Shi C, Tian C | 10.1038/S41422-023-00892-2 | 2023-11-22 | 53749 | |
Gs | αs | Human | - | 49 | β1 | Human | γ2 | Human | Cryo-EM | 6B3J | - | 3.3 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | - | - |
Exendin-P5
|
peptide | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Liang YL, Khoshouei M, Glukhova A, Furness SGB, Zhao P, Clydesdale L, Koole C, Truong TT, Thal DM, Lei S, Radjainia M, Danev R, Baumeister W, Wang MW, Miller LJ, Christopoulos A, Sexton PM, Wootten D | 10.1038/NATURE25773 | 2018-02-21 | 53739 | |
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 | 53741 | |
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, PHI, PHM, PHV, PACAP-27, 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 | 53739 | |
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 | deoxycholic acid, cholic acid, chenodeoxycholic acid, lithocholic acid | small-molecule | Yang F, Mao C, Guo L, Lin J, Ming Q, Xiao P, Wu X, Shen Q, Guo S, Shen DD, Lu R, Zhang L, Huang S, Ping Y, Zhang C, Ma C, Zhang K, Liang X, Shen Y, Nan F, Yi F, Luca VC, Zhou J, Jiang C, Sun JP, Xie X, Yu X, Zhang Y | 10.1038/S41586-020-2569-1 | 2020-09-09 | 53739 | |
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 | 53741 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7F1R | - | 3.0 | CCR5 | CCR5 | Chemokine | A (Rhodopsin) | Human | - | - | - |
CCL5
gtoplig
|
peptide | Agonist | CCL14, CCL8, CCL13, CCL4, CCL7, CCL2, CCL5, CCL11, CCL3, CCL16 | peptide | - | - | 2021-07-14 | 53741 | |
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 | 53741 | |
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 | - | - | 2021-12-29 | 53739 | |
Gi/o | αi1 | Human | - | 61 | β1 | Rat | γ2 | Human | Cryo-EM | 7VH0 | 7VH0_refined | 3.5 | MTR1B | MT2 | Melatonin | A (Rhodopsin) | Human | - | scFv16 | - |
ramelteon
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | melatonin | small-molecule | Wang Q, Lu Q, Guo Q, Teng M, Gong Q, Li X, Du Y, Liu Z, Tao Y | 10.1038/S41467-022-28111-3 | 2022-03-02 | 53741 | |
Gs | αs | Human | - | 56 | β1 | Human | γ2 | Human | Cryo-EM | 7RBT | 7RBT_refined | 3.1 | GIPR | GIP | Glucagon | B1 (Secretin) | Human | - |
scFv16 Nanobody-35 |
- |
tirzepatide
pubchem
gtoplig
2-fluoro-4-[(1R)-6-methoxy-1-methyl-2-{(1S)-1-[4-(propan-2-yl)phenyl]ethyl}-1,2,3,4-tetrahydroisoquinolin-5-yl]-6-[(2-methylpropyl)amino]phenol pubchem |
peptide small-molecule |
Agonist PAM |
gastric inhibitory polypeptide | peptide | Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW | 10.1073/PNAS.2116506119 | 2022-04-13 | 53739 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7W0O | 7W0O_refined | 3.8 | APJ | apelin | Apelin | A (Rhodopsin) | Human | BRIL | scFv16 | - |
apelin receptor early endogenous ligand
pubchem
|
peptide | Agonist | Elabela/Toddler-21, apelin-17, [Pyr1]apelin-13, Elabela/Toddler-11, Elabela/Toddler-32, apelin-13, apelin-36, apelin receptor early endogenous ligand | peptide | Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F | 10.1038/S41594-022-00797-5 | 2022-07-27 | 53741 | |
Gs | αs | Human | - | 58 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7VVM | 7VVM_refined | 3.2 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
Parathyroid hormone
|
peptide | Agonist | TIP39, PTHrP-(1-36), PTHrP, PTH | peptide | Kobayashi K, Kawakami K, Kusakizako T, Miyauchi H, Tomita A, Kobayashi K, Shihoya W, Yamashita K, Nishizawa T, Kato HE, Inoue A, Nureki O | 10.1016/J.MOLCEL.2022.07.003 | 2022-08-03 | 53739 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7VIE | 7VIE_refined | 2.9 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
sphingosine 1-phosphate
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | Yu L, He L, Gan B, Ti R, Xiao Q, Hu H, Zhu L, Wang S, Ren R | 10.1073/PNAS.2117716119 | 2022-09-28 | 53741 | |
G12/13 | α12 | Human | - | 55 | β1 | Human | γ2 | Human | Cryo-EM | 7X10 | - | 2.9 | AGRL3 | ADGRL3 | ADGRL | B2 (Adhesion) | Mouse | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Qian Y, Ma Z, Liu C, Li X, Zhu X, Wang N, Xu Z, Xia R, Liang J, Duan Y, Yin H, Xiong Y, Zhang A, Guo C, Chen Z, Huang Z, He Y | 10.1016/J.MOLCEL.2022.10.009 | 2022-11-09 | 53753 | |
Gq/11 | αq | Human | Gs-mini-Gq chimera | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8DWC | - | 2.9 | MRGX1 | MRGPRX1 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
Proenkephalin-A
|
peptide | Agonist | bovine adrenal medulla peptide 8-22 | peptide | Liu Y, Cao C, Huang XP, Gumpper RH, Rachman MM, Shih SL, Krumm BE, Zhang S, Shoichet BK, Fay JF, Roth BL | 10.1038/S41589-022-01173-6 | 2022-11-02 | 53749 | |
Gs | αs | Bovine | - | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8HA0 | - | 2.6 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
teriparatide
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
pubchem
pubchem
pubchem
pubchem
pubchem
|
peptide | Agonist | TIP39, PTHrP-(1-36), PTHrP, PTH | peptide | Zhao LH, Yuan QN, Dai AT, He XH, Chen CW, Zhang C, Xu YW, Zhou Y, Wang MW, Yang DH, Xu HE | 10.1038/S41401-022-01032-Z | 2022-12-21 | 53756 | |
Gs | αs | Human | Mini-Gs | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8HJ0 | - | 3.1 | GPR21 | GPR21 | A orphans | A (Rhodopsin) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Lin X, Chen B, Wu Y, Han Y, Qi A, Wang J, Yang Z, Wei X, Zhao T, Wu L, Xie X, Sun J, Zheng J, Zhao S, Xu F | 10.1038/S41467-023-35882-W | 2023-03-15 | 53739 | |
Gi/o | αo | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7T94 | - | 3.2 | ACM2 | M2 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | Antibody fragment | - |
acetylcholine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
LY2119620 pubchem gtoplig chembl_ligand |
small-molecule small-molecule |
Agonist PAM |
acetylcholine | small-molecule | - | - | 2023-01-25 | 53747 | |
Gi/o | αo | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8DZQ | 8DZQ_refined | 2.8 | OPRK | κ | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
SALVINORIN B METHOXYMETHYL ETHER
chembl_ligand
pubchem
|
small-molecule | Agonist | [Leu]enkephalin, β-neoendorphin, β-endorphin, dynorphin A, [Met]enkephalin, α-neoendorphin, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13), big dynorphin | peptide | Han J, Zhang J, Nazarova AL, Bernhard SM, Krumm BE, Zhao L, Lam JH, Rangari VA, Majumdar S, Nichols DE, Katritch V, Yuan P, Fay JF, Che T | 10.1038/S41586-023-06030-7 | 2023-05-03 | 53747 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8GHV | 8GHV_refined | 2.8 | CNR1 | CB1 | Cannabinoid | A (Rhodopsin) | Human | - | scFv16 | - |
CHEMBL4208628
chembl_ligand
pubchem
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | Krishna Kumar K, Robertson MJ, Thadhani E, Wang H, Suomivuori CM, Powers AS, Ji L, Nikas SP, Dror RO, Inoue A, Makriyannis A, Skiniotis G, Kobilka B | 10.1038/S41467-023-37864-4 | 2023-05-24 | 53741 | |
Gs | αs | Human | - | 58 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8GW8 | - | 2.9 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
PCO371
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | TIP39, PTHrP-(1-36), PTHrP, PTH | peptide | Kobayashi K, Kawakami K, Kusakizako T, Tomita A, Nishimura M, Sawada K, Okamoto HH, Hiratsuka S, Nakamura G, Kuwabara R, Noda H, Muramatsu H, Shimizu M, Taguchi T, Inoue A, Murata T, Nureki O | 10.1038/S41586-023-06169-3 | 2023-06-14 | 53739 | |
Gq/11 | αq | Human | - | 99 | β1 | Human | γ2 | Human | Cryo-EM | 8IYS | - | 3.0 | FFAR4 | FFA4 | Free fatty acid | A (Rhodopsin) | Human | - | scFv16 | - |
TUG-891
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | myristic acid, linoleic acid, α-linolenic acid, oleic acid | small-molecule | Yin H, Inoue A, Ma Z, Zhu X, Xia R, Xu Z, Wang N, Duan Y, Zhang A, Guo C, He Y | 10.1038/S41422-023-00835-X | 2023-06-21 | 53749 | |
Gq/11 | αq | Human | - | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8THL | - | 3.1 | ADA1A | α1A | Adrenoceptors | A (Rhodopsin) | Human | T4-Lysozyme | scFv16 | - |
(-)-adrenaline
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
|
small-molecule | Agonist | (-)-adrenaline, (-)-noradrenaline | small-molecule | Su M, Wang J, Xiang G, Do HN, Levitz J, Miao Y, Huang XY | 10.1038/S41467-023-40524-2 | 2023-08-16 | 53749 | |
Gi/o | αi1 | Human | - | 62 | β1 | Mouse | γ2 | Mouse | Cryo-EM | 8IHH | - | 3.1 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | BRIL | scFv16 | - |
5-butyl-1H-pyrazole-3-carboxylic acid
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | Suzuki S, Tanaka K, Nishikawa K, Suzuki H, Oshima A, Fujiyoshi Y | 10.1038/S41467-023-41650-7 | 2023-08-30 | 53741 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 8JIM | - | 3.0 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | - | scFv16 | - |
CHEMBL3354065
chembl_ligand
pubchem
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | Zhao C, Wang H, Liu Y, Cheng L, Wang B, Tian X, Fu H, Wu C, Li Z, Shen C, Yu J, Yang S, Hu H, Fu P, Ma L, Wang C, Yan W, Shao Z | 10.1016/J.MOLCEL.2023.07.030 | 2023-09-06 | 53741 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8W88 | - | 2.6 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
ulotaront
pubchem
gtoplig
drugbank
chembl_ligand
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, dopamine | small-molecule | Liu H, Zheng Y, Wang Y, Wang Y, He X, Xu P, Huang S, Yuan Q, Zhang X, Wang L, Jiang K, Chen H, Li Z, Liu W, Wang S, Xu HE, Xu F | 10.1038/S41586-023-06775-1 | 2023-11-22 | 53739 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 6NI3 | 6NI3_refined | 3.8 | ADRB2 | β2 | Adrenoceptors | A (Rhodopsin) | Human | - | Nanobody-35 | - |
CHEMBL1615159
chembl_ligand
pubchem
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, 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 | 53739 | |
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 | 53741 | |
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 | 53741 | |
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 | CCL14, CCL8, CCL13, CCL4, CCL7, CCL2, CCL5, CCL11, CCL3, CCL16 | peptide | Isaikina P, Tsai CJ, Dietz N, Pamula F, Grahl A, Goldie KN, Guixa-Gonzalez R, Branco C, Paolini-Bertrand M, Calo N, Cerini F, Schertler GFX, Hartley O, Stahlberg H, Maier T, Deupi X, Grzesiek S | 10.1126/SCIADV.ABG8685 | 2021-06-30 | 53741 | |
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 | 53749 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7NA7 | 7NA7_refined | 2.7 | GHSR | ghrelin | Ghrelin | A (Rhodopsin) | Human | - | Antibody fragment | - |
Ghrelin-27
|
peptide | Agonist | [des-Gln14]ghrelin, ghrelin | peptide | Liu H, Sun D, Myasnikov A, Damian M, Baneres JL, Sun J, Zhang C | 10.1038/S41467-021-26735-5 | 2021-12-15 | 53741 | |
Gi/o | αi1 | Human | - | 61 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7T6V | 7T6V_refined | 3.1 | FPR2 | FPR2/ALX | Formylpeptide | A (Rhodopsin) | Human | - | scFv16 | - |
synthetic peptide
|
peptide | Agonist | humanin, aspirin-triggered resolvin D1, LXA4, resolvin D1, serum amyloid A, PrP106-126, 15-deoxy-LXA4, aspirin triggered lipoxin A4, LL-37, LTC4, annexin I, fMet-Leu-Phe, LTD4 | peptide | 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 | 53741 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7TYN | - | 2.6 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - | Nanobody-35 | - |
calcitonin (salmon synthetic)
pubchem
|
small-molecule | Agonist | adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP | peptide | Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM | 10.1126/SCIENCE.ABM9609 | 2022-03-30 | 53739 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7TUZ | 7TUZ_refined | 3.1 | GP183 | GPR183 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
(2S,4aS,4bS,7R,8S,8aS,9R,10aR)-7-[(2R,3R)-7-hydroxy-3,7-dimethyloctan-2-yl]-4a,7,8-trimethyltetradecahydrophenanthrene-2,9-diol
pubchem
|
small-molecule | Agonist | 7α,25-dihydroxycholesterol, 7α,27-dihydroxycholesterol, 25-hydroxycholesterol, 7α-hydroxycholesterol, 27-hydroxycholesterol, 7β-hydroxycholesterol, 7β, 25-dihydroxycholesterol, 7β, 27-dihydroxycholesterol | small-molecule | Chen H, Huang W, Li X | 10.1016/J.STR.2022.04.006 | 2022-04-13 | 53741 | |
Gs | αs | Human | - | 57 | β1 | Human | γ2 | Human | Cryo-EM | 7F24 | - | 4.2 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | - | - |
dopamine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | Teng X, Chen S, Wang Q, Chen Z, Wang X, Huang N, Zheng S | 10.1126/SCIADV.ABO4158 | 2022-06-15 | 53739 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7W0P | 7W0P_refined | 3.2 | APJ | apelin | Apelin | A (Rhodopsin) | Human | BRIL | scFv16 | - |
apelin receptor early endogenous ligand
pubchem
|
peptide | Agonist | Elabela/Toddler-21, apelin-17, [Pyr1]apelin-13, Elabela/Toddler-11, Elabela/Toddler-32, apelin-13, apelin-36, apelin receptor early endogenous ligand | peptide | Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F | 10.1038/S41594-022-00797-5 | 2022-07-27 | 53741 | |
Gi/o | αi1 | Human | - | 63 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7XAV | 7XAV_refined | 2.9 | SSR2 | SST2 | Somatostatin | A (Rhodopsin) | Human | - | scFv16 | - |
lanreotide
pubchem
gtoplig
drugbank
|
peptide | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | Bo Q, Yang F, Li Y, Meng X, Zhang H, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C | 10.1038/S41421-022-00405-2 | 2022-08-31 | 53741 | |
Gs | αs | Human | - | 58 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7VVN | 7VVN_refined | 3.8 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
teriparatide
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
pubchem
pubchem
pubchem
pubchem
pubchem
|
peptide | Agonist | TIP39, PTHrP-(1-36), PTHrP, PTH | peptide | Kobayashi K, Kawakami K, Kusakizako T, Miyauchi H, Tomita A, Kobayashi K, Shihoya W, Yamashita K, Nishizawa T, Kato HE, Inoue A, Nureki O | 10.1016/J.MOLCEL.2022.07.003 | 2022-08-03 | 53739 | |
Gq/11 | α11 | Human | - | 62 | β1 | Rat | γ2 | Mouse | Cryo-EM | 7TRY | - | 3.7 | CRFR2 | CRF2 | Corticotropin-releasing factor | B1 (Secretin) | Human | - | - | - |
Urocortin
pubchem
|
peptide | Agonist | urocortin 1, corticotrophin-releasing hormone, urocortin 2, urocortin 3 | peptide | Zhao LH, Lin J, Ji SY, Zhou XE, Mao C, Shen DD, He X, Xiao P, Sun J, Melcher K, Zhang Y, Yu X, Xu HE | 10.1038/S41467-022-33851-3 | 2022-11-09 | 53750 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7X2V | - | 3.1 | AGRF1 | ADGRF1 | ADGRF | B2 (Adhesion) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y | 10.1038/S41467-022-33173-4 | 2022-09-28 | 53741 | |
Gi/o | αi1 | Human | - | 64 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8EF6 | 8EF6_refined | 3.2 | OPRM | μ | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
morphine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | [Leu]enkephalin, β-endorphin, dynorphin A, [Met]enkephalin, endomorphin-1, endomorphin-2, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13) | peptide | Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, Rao Q, Yang J, Liu J, Zhou Q, Wang X, Liu M, Liu W, Jiang X, Yang D, Jiang H, Shen J, Melcher K, Chen H, Jiang Y, Cheng X, Wang MW, Xie X, Xu HE | 10.1016/J.CELL.2022.09.041 | 2022-11-09 | 53741 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8GUS | - | 3.0 | CNR2 | CB2 | Cannabinoid | A (Rhodopsin) | Human | - | scFv16 | - |
CHEMBL2179724
chembl_ligand
pubchem
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | Li X, Chang H, Bouma J, de Paus LV, Mukhopadhyay P, Paloczi J, Mustafa M, van der Horst C, Kumar SS, Wu L, Yu Y, van den Berg RJBHN, Janssen APA, Lichtman A, Liu ZJ, Pacher P, van der Stelt M, Heitman LH, Hua T | 10.1038/S41467-023-37112-9 | 2023-05-10 | 53741 | |
Gq/11 | αq | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8IBU | 8IBU_refined | 3.5 | MTLR | motilin | Motilin | A (Rhodopsin) | Human | BRIL | scFv16 | - |
erythromycin
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | motilin | peptide | You C, Zhang Y, Xu Y, Xu P, Li Z, Li H, Huang S, Chen Z, Li J, Xu HE, Jiang Y | 10.1126/SCIADV.ADE9020 | 2023-04-12 | 53749 | |
Gq/11 | αq | Human | Mini-Gq | 46 | - | - | - | - | Cryo-EM | 7YM8 | 7YM8_refined | 2.9 | ADA1A | α1A | Adrenoceptors | A (Rhodopsin) | Human | - | Nanobody-29 | - |
oxymetazoline
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | (-)-adrenaline, (-)-noradrenaline | small-molecule | Toyoda Y, Zhu A, Kong F, Shan S, Zhao J, Wang N, Sun X, Zhang L, Yan C, Kobilka BK, Liu X | 10.1038/S41467-023-39310-X | 2023-07-05 | 53749 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8F2A | - | 2.2 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - | Nanobody-35 | - |
Pramlintide analogue San385
|
peptide | Agonist | adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP | peptide | Cao J, Belousoff MJ, Gerrard E, Danev R, Fletcher MM, Dal Maso E, Schreuder H, Lorenz K, Evers A, Tiwari G, Besenius M, Li Z, Johnson RM, Wootten D, Sexton PM | 10.1038/S41589-023-01393-4 | 2023-08-02 | 53739 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8JD3 | - | 3.3 | GRM2 | mGlu2 | Metabotropic glutamate | C (Glutamate) | Human | - | - | - |
L-glutamic acid
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
pubchem
JNJ-40411813 pubchem gtoplig chembl_ligand drugbank |
small-molecule small-molecule |
Agonist PAM |
L-glutamic acid | small-molecule | Wang X, Wang M, Xu T, Feng Y, Shao Q, Han S, Chu X, Xu Y, Lin S, Zhao Q, Wu B | 10.1038/S41422-023-00830-2 | 2023-06-21 | 53741 | |
Gi/o | αi1 | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8HQM | 8HQM_refined | 3.0 | GP132 | GPR132 | A orphans | A (Rhodopsin) | Human | BRIL | scFv16 | - |
CHEMBL3354065
chembl_ligand
pubchem
|
small-molecule | Agonist | 9-hydroxyoctadecadienoic acid | small-molecule | Wang JL, Dou XD, Cheng J, Gao MX, Xu GF, Ding W, Ding JH, Li Y, Wang SH, Ji ZW, Zhao XY, Huo TY, Zhang CF, Liu YM, Sha XY, Gao JR, Zhang WH, Hao Y, Zhang C, Sun JP, Jiao N, Yu X | 10.1038/S42255-023-00899-4 | 2023-10-11 | 53741 | |
Gs | αs | Bovine | - | 59 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8ITM | - | 3.1 | GIPR | GIP | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | gastric inhibitory polypeptide | peptide | Zhao F, Hang K, Zhou Q, Shao L, Li H, Li W, Lin S, Dai A, Cai X, Liu Y, Xu Y, Feng W, Yang D, Wang MW | 10.1073/PNAS.2306145120 | 2023-10-18 | 53756 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8JLJ | - | 3.1 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Mouse | BRIL | scFv16 | - |
CHEMBL1182312
chembl_ligand
chembl_ligand
pubchem
|
small-molecule | Agonist | β-phenylethylamine, 3-iodothyronamine, tyramine | small-molecule | Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z | 10.1038/S41586-023-06804-Z | 2023-11-15 | 53739 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8WC6 | - | 3.2 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Mouse | - |
scFv16 Nanobody-35 |
- |
2-Phenylethanaminium
pubchem
|
small-molecule | Agonist | β-phenylethylamine, 3-iodothyronamine, tyramine | small-molecule | Shang P, Rong N, Jiang JJ, Cheng J, Zhang MH, Kang D, Qi L, Guo L, Yang GM, Liu Q, Zhou Z, Li XB, Zhu KK, Meng QB, Han X, Yan W, Kong Y, Yang L, Wang X, Lei D, Feng X, Liu X, Yu X, Wang Y, Li Q, Shao ZH, Yang F, Sun JP | 10.1016/J.CELL.2023.10.014 | 2023-12-27 | 53739 | |
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 | 53747 | |
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 | urocortin 1, corticotrophin-releasing hormone, 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 | 53739 | |
Gi/o | αt2 | Bovine | Only H5 | 3 | - | - | - | - | X-ray | 6PGS | - | 2.9 | OPSD | Rhodopsin | Opsins | A (Rhodopsin) | Bovine | - | - | - |
Geraniol
pubchem
|
small-molecule | unknown | - | - | - | - | 2020-07-01 | 53871 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7CX2 | - | 2.8 | PE2R2 | EP2 | Prostanoid | A (Rhodopsin) | Human | - | Nanobody-35 | - |
PGE2
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
|
small-molecule | Agonist | thromboxane A2, PGF2α, PGI2, PGD2, PGE1, PGE2 | small-molecule | Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y | 10.1126/SCIADV.ABF1268 | 2021-05-05 | 53739 | |
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 | 53742 | |
Gq/11 | αq | Human | Gq-Gi1 chimera | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7F2O | - | 2.9 | BKRB2 | B2 | Bradykinin | A (Rhodopsin) | Human | - | scFv16 | - |
bradykinin
pubchem
gtoplig
chembl_ligand
drugbank
gtoplig
|
peptide | Agonist | [des-Arg10]kallidin, Lys-[Hyp3]-bradykinin, kallidin, [des-Arg9]bradykinin, [Hyp3]bradykinin, T-kinin, bradykinin | peptide | Yin YL, Ye C, Zhou F, Wang J, Yang D, Yin W, Wang MW, Xu HE, Jiang Y | 10.1038/S41594-021-00645-Y | 2021-10-13 | 53749 | |
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 | 53741 | |
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 | humanin, aspirin-triggered resolvin D1, LXA4, resolvin D1, serum amyloid A, PrP106-126, 15-deoxy-LXA4, aspirin triggered lipoxin A4, LL-37, LTC4, annexin I, fMet-Leu-Phe, LTD4 | peptide | 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 | 53741 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7TYI | - | 3.3 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - | Nanobody-35 | - |
Amylin rat
pubchem
|
peptide | Agonist | adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP | peptide | Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM | 10.1126/SCIENCE.ABM9609 | 2022-03-30 | 53739 | |
Gs | αs | Human | Engineered G alpha | 55 | β1 | Human | γ2 | Human | Cryo-EM | 7RGP | - | 2.9 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - |
scFv16 Nanobody-35 |
- |
tirzepatide
pubchem
gtoplig
|
peptide | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW | 10.1073/PNAS.2116506119 | 2022-04-13 | 53739 | |
Gq/11 | αq | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7XJK | 7XJK_refined | 3.3 | GALR2 | GAL2 | Galanin | A (Rhodopsin) | Human | - | scFv16 | - |
Galanin, Human
pubchem
|
peptide | Agonist | galanin-like peptide, spexin-1, galanin | peptide | Jiang W, Zheng S | 10.1073/PNAS.2121465119 | 2022-06-29 | 53749 | |
Gi/o | αi1 | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7WJ5 | 7WJ5_refined | 3.7 | SSR2 | SST2 | Somatostatin | A (Rhodopsin) | Human | BRIL | scFv16 | - |
SOMATOSTATIN
chembl_ligand
pubchem
|
protein | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | Heo Y, Yoon E, Jeon YE, Yun JH, Ishimoto N, Woo H, Park SY, Song JJ, Lee W | 10.7554/ELIFE.76823 | 2022-07-13 | 53741 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7T2H | - | 3.2 | OPRM | μ | Opioid | A (Rhodopsin) | Mouse | - | scFv16 | - |
LOFENTANIL
chembl_ligand
pubchem
|
small-molecule | Agonist | - | - | Qu Q, Huang W, Aydin D, Paggi JM, Seven AB, Wang H, Chakraborty S, Che T, DiBerto JF, Robertson MJ, Inoue A, Suomivuori CM, Roth BL, Majumdar S, Dror RO, Kobilka BK, Skiniotis G | 10.1038/S41589-022-01208-Y | 2022-12-07 | 53741 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7WYB | - | 3.0 | AGRL3 | ADGRL3 | ADGRL | B2 (Adhesion) | Mouse | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Qian Y, Ma Z, Liu C, Li X, Zhu X, Wang N, Xu Z, Xia R, Liang J, Duan Y, Yin H, Xiong Y, Zhang A, Guo C, Chen Z, Huang Z, He Y | 10.1016/J.MOLCEL.2022.10.009 | 2022-10-26 | 53741 | |
Gq/11 | αq | Human | Gs-mini-Gq chimera | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8DWG | - | 2.7 | MRGX1 | MRGPRX1 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
Proenkephalin-A
CHEMBL5177388 chembl_ligand pubchem |
peptide small-molecule |
Agonist PAM |
bovine adrenal medulla peptide 8-22 | peptide | Liu Y, Cao C, Huang XP, Gumpper RH, Rachman MM, Shih SL, Krumm BE, Zhang S, Shoichet BK, Fay JF, Roth BL | 10.1038/S41589-022-01173-6 | 2022-11-02 | 53749 | |
Gs | αs | Bovine | - | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8HAO | - | 3.8 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
teriparatide
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
pubchem
pubchem
pubchem
pubchem
pubchem
|
peptide | Agonist | TIP39, PTHrP-(1-36), PTHrP, PTH | peptide | Zhao LH, Yuan QN, Dai AT, He XH, Chen CW, Zhang C, Xu YW, Zhou Y, Wang MW, Yang DH, Xu HE | 10.1038/S41401-022-01032-Z | 2022-12-21 | 53756 | |
Gq/11 | αq | Human | - | 98 | β1 | Human | γ2 | Human | Cryo-EM | 7W3Z | - | 3.0 | GRPR | BB2 | Bombesin | A (Rhodopsin) | Human | - | scFv16 | - |
Gastrin-releasing peptide
pubchem
|
peptide | Agonist | neuromedin B, gastrin releasing peptide(14-27) (human), GRP-(18-27), gastrin-releasing peptide, neuromedin C | peptide | Peng S, Zhan Y, Zhang D, Ren L, Chen A, Chen ZF, Zhang H | 10.1073/PNAS.2216230120 | 2023-02-22 | 53749 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8G94 | 8G94_refined | 3.2 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
Early activation antigen CD69
pubchem
|
peptide | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | Chen H, Qin Y, Chou M, Cyster JG, Li X | 10.7554/ELIFE.88204 | 2023-04-19 | 53741 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8FLR | - | 2.9 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
PTHrP[1-36]
|
peptide | Agonist | TIP39, PTHrP-(1-36), PTHrP, PTH | peptide | Cary BP, Gerrard EJ, Belousoff MJ, Fletcher MM, Jiang Y, Russell IC, Piper SJ, Wootten D, Sexton PM | 10.1016/J.STR.2023.04.002 | 2023-04-26 | 53739 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8GCP | 8GCP_refined | 3.1 | PE2R4 | EP4 | Prostanoid | A (Rhodopsin) | Human | - | scFv16 | - |
PGE2
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
|
small-molecule | Agonist | thromboxane A2, PGF2α, PGI2, PGD2, PGE1, PGE2 | small-molecule | Huang SM, Xiong MY, Liu L, Mu J, Wang MW, Jia YL, Cai K, Tie L, Zhang C, Cao S, Wen X, Wang JL, Guo SC, Li Y, Qu CX, He QT, Cai BY, Xue C, Gan S, Xie Y, Cong X, Yang Z, Kong W, Li S, Li Z, Xiao P, Yang F, Yu X, Guan YF, Zhang X, Liu Z, Yang BX, Du Y, Sun JP | 10.1073/PNAS.2216329120 | 2024-01-03 | 53741 | |
Gi/o | αi1 | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8HVI | 8HVI_refined | 3.0 | GP132 | GPR132 | A orphans | A (Rhodopsin) | Human | BRIL | scFv16 | - |
NOX-6-7
gtoplig
pubchem
|
small-molecule | Agonist | 9-hydroxyoctadecadienoic acid | small-molecule | Wang JL, Dou XD, Cheng J, Gao MX, Xu GF, Ding W, Ding JH, Li Y, Wang SH, Ji ZW, Zhao XY, Huo TY, Zhang CF, Liu YM, Sha XY, Gao JR, Zhang WH, Hao Y, Zhang C, Sun JP, Jiao N, Yu X | 10.1038/S42255-023-00899-4 | 2023-10-11 | 53741 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 8J6Q | - | 2.6 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | - | scFv16 | - |
β-D-hydroxybutyric acid
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | Mao C, Gao M, Zang SK, Zhu Y, Shen DD, Chen LN, Yang L, Wang Z, Zhang H, Wang WW, Shen Q, Lu Y, Ma X, Zhang Y | 10.1038/S41467-023-43537-Z | 2023-12-06 | 53741 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Mouse | Cryo-EM | 8JSO | 8JSO_refined | 3.4 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Human | BRIL | scFv16 | - |
dexamfetamine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, dopamine | small-molecule | Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z | 10.1038/S41586-023-06804-Z | 2023-11-15 | 53739 | |
Gq/11 | αq | Human | - | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8WCB | - | 3.1 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Mouse | - | scFv16 | - |
Cyclohexylammonium ion
pubchem
|
small-molecule | Agonist | β-phenylethylamine, 3-iodothyronamine, tyramine | small-molecule | Shang P, Rong N, Jiang JJ, Cheng J, Zhang MH, Kang D, Qi L, Guo L, Yang GM, Liu Q, Zhou Z, Li XB, Zhu KK, Meng QB, Han X, Yan W, Kong Y, Yang L, Wang X, Lei D, Feng X, Liu X, Yu X, Wang Y, Li Q, Shao ZH, Yang F, Sun JP | 10.1016/J.CELL.2023.10.014 | 2023-12-27 | 53749 | |
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 | 53742 | |
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 | 53741 | |
Gs | αs | Human | - | 57 | β1 | Rat | γ2 | Bovine | Cryo-EM | 6LPB | 6LPB_refined | 3.9 | PACR | PAC1 | VIP and PACAP | B1 (Secretin) | Human | - | Nanobody-35 | - |
[Ac-His1]PACAP-27
gtoplig
chembl_ligand
pubchem
|
peptide | Agonist | VIP, PHI, PHM, PHV, PACAP-27, 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 | 53739 | |
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 | - | - | - | - | deoxycholic acid, cholic acid, chenodeoxycholic acid, lithocholic acid | small-molecule | Chen G, Wang X, Ge Y, Ma L, Chen Q, Liu H, Du Y, Ye RD, Hu H, Ren R | 10.1038/S41392-020-00262-Z | 2020-09-02 | 53739 | |
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 | 53739 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7JVR | - | 2.8 | DRD2 | D2 | Dopamine | A (Rhodopsin) | Human | - | scFv16 | - |
bromocriptine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | dopamine | small-molecule | Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP, Shen DD, Xu T, Liu YF, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE | 10.1016/J.CELL.2021.01.027 | 2021-02-24 | 53741 | |
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 | 53741 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7F4I | 7F4I_refined | 3.1 | MSHR | MC1 | Melanocortin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
bremelanotide
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
peptide | Agonist | β-MSH, ACTH, γ-MSH, α-MSH | peptide | Ma S, Chen Y, Dai A, Yin W, Guo J, Yang D, Zhou F, Jiang Y, Wang MW, Xu HE | 10.1038/S41422-021-00557-Y | 2021-09-08 | 53739 | |
Gq/11 | αq | Human | - | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7WQ4 | 7WQ4_refined | 2.6 | GALR2 | GAL2 | Galanin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
galanin
pubchem
gtoplig
chembl_ligand
gtoplig
pubchem
pubchem
pubchem
pubchem
|
peptide | Agonist | galanin-like peptide, spexin-1, galanin | peptide | Duan J, Shen DD, Zhao T, Guo S, He X, Yin W, Xu P, Ji Y, Chen LN, Liu J, Zhang H, Liu Q, Shi Y, Cheng X, Jiang H, Eric Xu H, Zhang Y, Xie X, Jiang Y | 10.1038/S41467-022-29072-3 | 2022-04-20 | 53749 | |
Gs | αs | Bovine | - | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7EQ1 | - | 3.3 | AGRG5 | ADGRG5 | ADGRG | B2 (Adhesion) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Ping YQ, Xiao P, Yang F, Zhao RJ, Guo SC, Yan X, Wu X, Zhang C, Lu Y, Zhao F, Zhou F, Xi YT, Yin W, Liu FZ, He DF, Zhang DL, Zhu ZL, Jiang Y, Du L, Feng SQ, Schoneberg T, Liebscher I, Xu HE, Sun JP | 10.1038/S41586-022-04619-Y | 2022-05-11 | 53756 | |
Gi/o | αi1 | Human | - | 64 | β1 | Rat | γ2 | Human | Cryo-EM | 7WIC | - | 2.8 | SSR2 | SST2 | Somatostatin | A (Rhodopsin) | Human | - | scFv16 | - |
SOMATOSTATIN
chembl_ligand
pubchem
|
protein | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | Chen LN, Wang WW, Dong YJ, Shen DD, Guo J, Yu X, Qin J, Ji SY, Zhang H, Shen Q, He Q, Yang B, Zhang Y, Li Q, Mao C | 10.1038/S41422-022-00669-Z | 2022-06-01 | 53741 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7W0M | 7W0M_refined | 3.7 | APJ | apelin | Apelin | A (Rhodopsin) | Human | BRIL | scFv16 | - |
(1R,2S)-N-[4-(2,6-dimethoxyphenyl)-5-(6-methylpyridin-2-yl)-1,2,4-triazol-3-yl]-1-(5-methylpyrimidin-2-yl)-1-oxidanyl-propane-2-sulfonamide
pubchem
|
small-molecule | Agonist | Elabela/Toddler-21, apelin-17, [Pyr1]apelin-13, Elabela/Toddler-11, Elabela/Toddler-32, apelin-13, apelin-36, apelin receptor early endogenous ligand | peptide | Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F | 10.1038/S41594-022-00797-5 | 2022-07-27 | 53741 | |
Gq/11 | αq | Human | Gi2-mini-Gq chimera | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8DPF | - | 2.8 | 5HT2C | 5-HT2C | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | scFv16 | - |
lorcaserin
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Gumpper RH, Fay JF, Roth BL | 10.1016/J.CELREP.2022.111211 | 2022-08-24 | 53749 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7XW6 | - | 2.8 | TSHR | TSH | Glycoprotein hormone | A (Rhodopsin) | Human | - | Nanobody-35 | - |
M22 antibody heavy chain
M22 antibody light chain N-[4-[[5-[(2S)-3-benzyl-5-hydroxy-4-oxo-1,2-dihydroquinazolin-2-yl]-2-methoxyphenyl]methoxy]phenyl]acetamide pubchem |
protein protein small-molecule |
Agonist | TSH | peptide | Duan J, Xu P, Luan X, Ji Y, He X, Song N, Yuan Q, Jin Y, Cheng X, Jiang H, Zheng J, Zhang S, Jiang Y, Xu HE | 10.1038/S41586-022-05173-3 | 2022-08-17 | 53739 | |
Gs | αs | Human | - | 58 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8JIR | 8JIR_refined | 2.6 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
SAR425899
|
peptide | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Li Y, Zhou Q, Dai A, Zhao F, Chang R, Ying T, Wu B, Yang D, Wang MW, Cong Z | 10.1073/PNAS.2303696120 | 2023-09-06 | 53739 | |
Gs | αs | Human | - | 56 | β1 | Human | γ2 | Human | Cryo-EM | 8TB0 | 8TB0_refined | 3.5 | GPR61 | GPR61 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | - | - | 2023-10-04 | 53739 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8WCA | - | 3.5 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Human | - | scFv16 | - |
2-Phenylethanaminium
pubchem
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, dopamine | small-molecule | Shang P, Rong N, Jiang JJ, Cheng J, Zhang MH, Kang D, Qi L, Guo L, Yang GM, Liu Q, Zhou Z, Li XB, Zhu KK, Meng QB, Han X, Yan W, Kong Y, Yang L, Wang X, Lei D, Feng X, Liu X, Yu X, Wang Y, Li Q, Shao ZH, Yang F, Sun JP | 10.1016/J.CELL.2023.10.014 | 2023-12-27 | 53739 | |
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 | humanin, aspirin-triggered resolvin D1, LXA4, resolvin D1, serum amyloid A, PrP106-126, 15-deoxy-LXA4, aspirin triggered lipoxin A4, LL-37, LTC4, annexin I, fMet-Leu-Phe, LTD4 | peptide | 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 | 53741 | |
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 | 53741 | |
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-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Zhang X, Johnson RM, Drulyte I, Yu L, Kotecha A, Danev R, Wootten D, Sexton PM, Belousoff MJ | 10.1016/J.STR.2021.04.008 | 2021-01-20 | 53739 | |
Gs | αs | Human | Engineered G alpha | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7LJC | - | 3.0 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
CHEMBL1160787
chembl_ligand
pubchem
mevidalen pubchem gtoplig chembl_ligand |
small-molecule small-molecule |
Agonist PAM |
L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | Zhuang Y, Krumm B, Zhang H, Zhou XE, Wang Y, Huang XP, Liu Y, Cheng X, Jiang Y, Jiang H, Zhang C, Yi W, Roth BL, Zhang Y, Xu HE | 10.1038/S41422-021-00482-0 | 2021-03-03 | 53739 | |
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-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Zhang X, Belousoff MJ, Liang YL, Danev R, Sexton PM, Wootten D | 10.1016/J.CELREP.2021.109374 | 2021-08-04 | 53739 | |
Gq/11 | αq | Human | Gs-Gq chimera | 52 | β1 | Human | γ2 | Human | Cryo-EM | 7RMI | - | 3.2 | NK1R | NK1 | Tachykinin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
substance P
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
|
peptide | Agonist | neuropeptide-γ, neurokinin A, neuropeptide K, neurokinin B, hemokinin 1, substance P | peptide | Harris JA, Faust B, Gondin AB, Damgen MA, Suomivuori CM, Veldhuis NA, Cheng Y, Dror RO, Thal DM, Manglik A | 10.1038/S41589-021-00890-8 | 2021-11-03 | 53749 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7NA8 | - | 2.7 | GHSR | ghrelin | Ghrelin | A (Rhodopsin) | Human | - | Antibody fragment | - |
ibutamoren
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | [des-Gln14]ghrelin, ghrelin | peptide | Liu H, Sun D, Myasnikov A, Damian M, Baneres JL, Sun J, Zhang C | 10.1038/S41467-021-26735-5 | 2021-12-15 | 53741 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7EVZ | - | 3.1 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
cenerimod
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z | 10.1038/S41422-021-00566-X | 2021-09-29 | 53741 | |
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 | 53741 | |
Gi/o | αo | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7EJ8 | - | 3.0 | ADA2A | α2A | Adrenoceptors | A (Rhodopsin) | Human | - | scFv16 | - |
brimonidine (UK14304)
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
|
small-molecule | Agonist | (-)-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 | 53747 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7SBF | - | 2.9 | OPRM | μ | Opioid | A (Rhodopsin) | Mouse | BRIL | scFv16 | - |
N-[(2S)-2-(dimethylamino)-3-(4-hydroxyphenyl)propyl]-N'-[(2S)-1-(thiophen-3-yl)propan-2-yl]urea
pubchem
|
small-molecule | Agonist | - | - | Wang H, Hetzer F, Huang W, Qu Q, Meyerowitz J, Kaindl J, Hubner H, Skiniotis G, Kobilka BK, Gmeiner P | 10.1002/ANIE.202200269 | 2022-04-20 | 53741 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7X9A | 7X9A_refined | 3.2 | NPY1R | Y1 | Neuropeptide Y | A (Rhodopsin) | Human | - | - | - |
neuropeptide Y
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
pubchem
pubchem
pubchem
|
peptide | Agonist | peptide YY, neuropeptide Y, pancreatic polypeptide | peptide | Tang T, Tan Q, Han S, Diemar A, Lobner K, Wang H, Schuss C, Behr V, Morl K, Wang M, Chu X, Yi C, Keller M, Kofoed J, Reedtz-Runge S, Kaiser A, Beck-Sickinger AG, Zhao Q, Wu B | 10.1126/SCIADV.ABM1232 | 2022-05-18 | 53741 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7W0N | - | 4.2 | APJ | apelin | Apelin | A (Rhodopsin) | Human | BRIL | scFv16 | - |
apelin receptor early endogenous ligand
pubchem
|
peptide | Agonist | Elabela/Toddler-21, apelin-17, [Pyr1]apelin-13, Elabela/Toddler-11, Elabela/Toddler-32, apelin-13, apelin-36, apelin receptor early endogenous ligand | peptide | Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F | 10.1038/S41594-022-00797-5 | 2022-07-27 | 53741 | |
Gi/o | αi1 | Human | - | 65 | β1 | Human | γ2 | Human | Cryo-EM | 7XA3 | 7XA3_refined | 2.9 | CCR2 | CCR2 | Chemokine | A (Rhodopsin) | Human | - | scFv16 | - |
C-C motif chemokine 2
|
peptide | Agonist | CCL8, CCL13, CCL7, CCL2, CCL11, CCL24, CCL16, CCL26 | peptide | Shao Z, Tan Y, Shen Q, Hou L, Yao B, Qin J, Xu P, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Chen ZH, Jiang Y, Xu HE, Ying S, Ma H, Zhang Y, Shen H | 10.1038/S41421-022-00403-4 | 2022-08-24 | 53741 | |
G12/13 | α13 | Human | - | 55 | β1 | Human | γ2 | Human | Cryo-EM | 7WY0 | - | 2.8 | AGRF1 | ADGRF1 | ADGRF | B2 (Adhesion) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y | 10.1038/S41467-022-33173-4 | 2022-09-28 | 53754 | |
Gs | αs | Human | - | 56 | β1 | Human | γ2 | Human | Cryo-EM | 8E3Y | - | 2.3 | VIPR1 | VPAC1 | VIP and PACAP | B1 (Secretin) | Human | - | Nanobody-35 | - |
[Ac-His1]PACAP-27
gtoplig
chembl_ligand
pubchem
|
peptide | Agonist | VIP, PHI, PHM, secretin, PACAP-27, GHRH, PACAP-38 | peptide | Piper SJ, Deganutti G, Lu J, Zhao P, Liang YL, Lu Y, Fletcher MM, Hossain MA, Christopoulos A, Reynolds CA, Danev R, Sexton PM, Wootten D | 10.1038/S41467-022-34629-3 | 2022-11-23 | 53739 | |
Gq/11 | αq | Human | - | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8HCQ | 8HCQ_refined | 3.0 | EDNRA | ETA | Endothelin | A (Rhodopsin) | Human | - | scFv16 | - |
ENDOTHELIN
chembl_ligand
pubchem
|
protein | Agonist | endothelin-1, endothelin-2, endothelin-3 | peptide | - | - | 2023-03-22 | 53749 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 8IRS | - | 3.0 | DRD2 | D2 | Dopamine | A (Rhodopsin) | Human | BRIL | scFv16 | - |
rotigotine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | dopamine | small-molecule | Xu P, Huang S, Krumm BE, Zhuang Y, Mao C, Zhang Y, Wang Y, Huang XP, Liu YF, He X, Li H, Yin W, Jiang Y, Zhang Y, Roth BL, Xu HE | 10.1038/S41422-023-00808-0 | 2023-06-07 | 53741 | |
Gi/o | αi1 | Human | - | 63 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8HK3 | 8HK3_refined | 3.2 | C3AR | C3a | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | C5a, C3a | peptide | Wang Y, Liu W, Xu Y, He X, Yuan Q, Luo P, Fan W, Zhu J, Zhang X, Cheng X, Jiang Y, Xu HE, Zhuang Y | 10.1038/S41589-023-01339-W | 2023-05-10 | 53741 | |
Gi/o | αi1 | Human | - | 63 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8HK5 | 8HK5_refined | 3.0 | C5AR1 | C5a1 | Complement peptide | A (Rhodopsin) | Human | - | - | - |
C5a
gtoplig
|
peptide | Agonist | ribosomal protein S19, C5a, C5a des-Arg, C3a | peptide | Wang Y, Liu W, Xu Y, He X, Yuan Q, Luo P, Fan W, Zhu J, Zhang X, Cheng X, Jiang Y, Xu HE, Zhuang Y | 10.1038/S41589-023-01339-W | 2023-05-10 | 53741 | |
Gq/11 | αq | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8IUL | - | 2.8 | PF2R | FP | Prostanoid | A (Rhodopsin) | Human | - | scFv16 | - |
latanoprost (free acid form)
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | thromboxane A2, PGF2α, PGI2, PGD2, PGE2 | small-molecule | Wu C, Xu Y, He Q, Li D, Duan J, Li C, You C, Chen H, Fan W, Jiang Y, Eric Xu H | 10.1038/S41467-023-38411-X | 2023-07-12 | 53749 | |
Gi/o | αi3 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 8JD6 | - | 3.4 | GRM4 | mGlu4 | Metabotropic glutamate | C (Glutamate) | Human | - | scFv16 | - |
VU0364770
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | L-serine-O-phosphate, L-glutamic acid | small-molecule | Wang X, Wang M, Xu T, Feng Y, Shao Q, Han S, Chu X, Xu Y, Lin S, Zhao Q, Wu B | 10.1038/S41422-023-00830-2 | 2023-06-21 | 53743 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 8H2G | 8H2G_refined | 3.0 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | - | scFv16 | - |
nicotinic acid
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
pubchem
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | - | - | 2023-10-11 | 53741 | |
Gi/o | αi1 | Human | - | 62 | β1 | Mouse | γ2 | Mouse | Cryo-EM | 8IHF | - | 3.0 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | BRIL | scFv16 | - |
MK 6892
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | Suzuki S, Tanaka K, Nishikawa K, Suzuki H, Oshima A, Fujiyoshi Y | 10.1038/S41467-023-41650-7 | 2023-08-30 | 53741 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8W8R | - | 3.3 | GP101 | GPR101 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
1-(4-Methylpyridin-2-yl)-3-[3-(trifluoromethyl)phenyl]thiourea
pubchem
|
small-molecule | Agonist | - | - | Yang Z, Wang JY, Yang F, Zhu KK, Wang GP, Guan Y, Ning SL, Lu Y, Li Y, Zhang C, Zheng Y, Zhou SH, Wang XW, Wang MW, Xiao P, Yi F, Zhang C, Zhang PJ, Xu F, Liu BH, Zhang H, Yu X, Gao N, Sun JP | 10.1038/S41589-023-01456-6 | 2024-01-03 | 53739 | |
Gi/o | αgust | Bovine | Only H5 | 3 | - | - | - | - | X-ray | 5EN0 | - | 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 | 53895 | |
Gi/o | αo | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 6G79 | - | 3.8 | 5HT1B | 5-HT1B | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | - | - |
donitriptan
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | tryptamine, 5-hydroxytryptamine, 5-HT-moduline | small-molecule | Garcia-Nafria J, Nehme R, Edwards PC, Tate CG | 10.1038/S41586-018-0241-9 | 2018-06-20 | 53747 | |
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 | 53851 | |
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 | 53739 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7CKZ | - | 3.1 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
dopamine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
mevidalen pubchem gtoplig chembl_ligand |
small-molecule small-molecule |
Agonist PAM |
L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z | 10.1016/J.CELL.2021.01.028 | 2021-03-03 | 53739 | |
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 | 53739 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7F54 | - | 3.0 | MC4R | MC4 | Melanocortin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
afamelanotide
pubchem
gtoplig
chembl_ligand
drugbank
pubchem
pubchem
pubchem
pubchem
|
peptide | Agonist | β-MSH, α-MSH, agouti-related protein, γ-MSH, ACTH | peptide | Zhang H, Chen LN, Yang D, Mao C, Shen Q, Feng W, Shen DD, Dai A, Xie S, Zhou Y, Qin J, Sun JP, Scharf DH, Hou T, Zhou T, Wang MW, Zhang Y | 10.1038/S41422-021-00552-3 | 2021-11-03 | 53739 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7LLL | - | 3.7 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
exendin-4
pubchem
gtoplig
pubchem
|
peptide | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Deganutti G, Liang YL, Zhang X, Khoshouei M, Clydesdale L, Belousoff MJ, Venugopal H, Truong TT, Glukhova A, Keller AN, Gregory KJ, Leach K, Christopoulos A, Danev R, Reynolds CA, Zhao P, Sexton PM, Wootten D | 10.1038/S41467-021-27760-0 | 2022-01-12 | 53739 | |
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 | 12R-HETE, LTB4, 20-hydroxy-LTB4 | small-molecule | Wang N, He X, Zhao J, Jiang H, Cheng X, Xia Y, Eric Xu H, He Y | 10.1038/S41467-022-28820-9 | 2022-03-09 | 53741 | |
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-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW | 10.1038/S41467-022-28683-0 | 2022-03-02 | 53756 | |
Gs | αs | Bovine | Gi1-Gs chimera | 56 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7S0G | - | 3.9 | ADRB1 | β1 | Adrenoceptors | A (Rhodopsin) | Wild turkey | - | - | - |
LEVISOPRENALINE
chembl_ligand
chembl_ligand
pubchem
|
small-molecule | Agonist | - | - | Alegre KO, Paknejad N, Su M, Lou JS, Huang J, Jordan KD, Eng ET, Meyerson JR, Hite RK, Huang XY | 10.1038/S41594-021-00679-2 | 2021-11-17 | 53756 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7F1Z | - | 3.5 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | - | - |
dopamine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | Teng X, Chen S, Wang Q, Chen Z, Wang X, Huang N, Zheng S | 10.1126/SCIADV.ABO4158 | 2022-06-15 | 53739 | |
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 | 53741 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7U2K | - | 3.3 | OPRM | μ | Opioid | A (Rhodopsin) | Mouse | - | - | - |
CHEMBL147044
chembl_ligand
pubchem
|
small-molecule | Agonist | - | - | Faouzi A, Wang H, Zaidi SA, DiBerto JF, Che T, Qu Q, Robertson MJ, Madasu MK, El Daibani A, Varga BR, Zhang T, Ruiz C, Liu S, Xu J, Appourchaux K, Slocum ST, Eans SO, Cameron MD, Al-Hasani R, Pan YX, Roth BL, McLaughlin JP, Skiniotis G, Katritch V, Kobilka BK, Majumdar S | 10.1038/S41586-022-05588-Y | 2022-12-07 | 53741 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7WZ4 | - | 3.0 | GPR88 | GPR88 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Chen G, Xu J, Inoue A, Schmidt MF, Bai C, Lu Q, Gmeiner P, Liu Z, Du Y | 10.1038/S41467-022-30081-5 | 2022-10-26 | 53741 | |
Gi/o | αi1 | Human | - | 63 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7YU7 | - | 3.8 | LPAR1 | LPA1 | Lysophospholipid (LPA) | A (Rhodopsin) | Human | - | scFv16 | - |
[(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate
pubchem
|
small-molecule | Agonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O | 10.1038/S41467-022-33121-2 | 2022-10-05 | 53741 | |
Gq/11 | αq | Human | - | 97 | β1 | Human | γ2 | Human | Cryo-EM | 7F6G | 7F6G_refined | 2.9 | AGTR1 | AT1 | Angiotensin | A (Rhodopsin) | Human | - | - | - |
SAR1-AngII
|
peptide | Agonist | angiotensin IV, angiotensin II, angiotensin III, angiotensin A | peptide | - | - | 2023-03-29 | 53749 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8HBD | 8HBD_refined | 3.0 | EDNRB | ETB | Endothelin | A (Rhodopsin) | Human | - | scFv16 | - |
sovateltide
pubchem
gtoplig
chembl_ligand
gtoplig
pubchem
pubchem
|
peptide | Agonist | endothelin-1, endothelin-2, endothelin-3 | peptide | - | - | 2023-03-22 | 53741 | |
Gs | αolf | Human | Golf-Gi chimera | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8IW1 | - | 3.4 | TAAR9 | TAAR9 | A orphans | A (Rhodopsin) | Mouse | - | scFv16 | - |
2-Phenylethanaminium
pubchem
|
small-molecule | Agonist | - | - | Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP | 10.1038/S41586-023-06106-4 | 2023-05-31 | 53740 | |
Gi/o | αo | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7XJJ | 7XJJ_refined | 3.3 | GALR1 | GAL1 | Galanin | A (Rhodopsin) | Human | - | scFv16 | - |
galanin
pubchem
gtoplig
chembl_ligand
gtoplig
pubchem
pubchem
pubchem
pubchem
|
peptide | Agonist | galanin-like peptide, galanin | peptide | - | - | 2023-05-03 | 53747 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8FLT | - | 3.0 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
M-PTH(1-14)
|
peptide | Agonist | TIP39, PTHrP-(1-36), PTHrP, PTH | peptide | Cary BP, Gerrard EJ, Belousoff MJ, Fletcher MM, Jiang Y, Russell IC, Piper SJ, Wootten D, Sexton PM | 10.1016/J.STR.2023.04.002 | 2023-04-26 | 53739 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8F2B | - | 2.0 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - |
Nanobody-35 RAMP3 |
- |
Pramlintide analogue San45
|
peptide | Agonist | adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP | peptide | Cao J, Belousoff MJ, Gerrard E, Danev R, Fletcher MM, Dal Maso E, Schreuder H, Lorenz K, Evers A, Tiwari G, Besenius M, Li Z, Johnson RM, Wootten D, Sexton PM | 10.1038/S41589-023-01393-4 | 2023-08-02 | 53739 | |
Gq/11 | αq | Human | GRK2 bound | 88 | - | - | - | - | Cryo-EM | 8JPC | - | 3.1 | NTR1 | NTS1 | Neurotensin | A (Rhodopsin) | Human | - | GRK2 | GRK2 |
JMV431
gtoplig
chembl_ligand
pubchem
CHEMBL4576388 chembl_ligand pubchem |
peptide small-molecule |
Agonist PAM |
large neurotensin, large neuromedin N, neurotensin, neuromedin N | peptide | Duan J, Liu H, Zhao F, Yuan Q, Ji Y, Cai X, He X, Li X, Li J, Wu K, Gao T, Zhu S, Lin S, Wang MW, Cheng X, Yin W, Jiang Y, Yang D, Xu HE | 10.1038/S41586-023-06395-9 | 2023-08-09 | 53749 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8HN8 | - | 3.0 | HRH4 | H4 | Histamine | A (Rhodopsin) | Human | - | scFv16 | - |
histamine
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
gtoplig
|
small-molecule | Agonist | histamine, CCL16 | small-molecule | - | - | 2023-12-20 | 53741 | |
Gi/o | αi1 | Human | - | 62 | β1 | Mouse | γ2 | Mouse | Cryo-EM | 8IHJ | 8IHJ_refined | 3.1 | HCAR3 | HCA3 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | BRIL | scFv16 | - |
(5S)-5-methyl-4-oxo-5-phenylfuran-2-carboxylic acid
pubchem
|
small-molecule | Agonist | 3-hydroxyoctanoic acid | small-molecule | Suzuki S, Tanaka K, Nishikawa K, Suzuki H, Oshima A, Fujiyoshi Y | 10.1038/S41467-023-41650-7 | 2023-08-30 | 53741 | |
Gs | αs | Human | - | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8JIS | 8JIS_refined | 2.5 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
Dual-agonist peptide P15
|
peptide | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Li Y, Zhou Q, Dai A, Zhao F, Chang R, Ying T, Wu B, Yang D, Wang MW, Cong Z | 10.1073/PNAS.2303696120 | 2023-11-08 | 53739 | |
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, PTHrP-(1-36), PTHrP, PTH | peptide | Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y | 10.1126/SCIENCE.AAV7942 | 2019-04-17 | 53756 | |
Gs | αs | Human | - | 49 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7DHR | 7DHR_refined | 3.8 | ADRB2 | β2 | Adrenoceptors | A (Rhodopsin) | Human | - | Nanobody-35 | - |
LEVISOPRENALINE
chembl_ligand
chembl_ligand
pubchem
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline | small-molecule | Si G, Du Y, Tang P, Ma G, Jia Z, Zhou X, Mu D, Shen Y, Lu Y, Mao Y, Chen C, Li Y, Gu N | 10.1093/NSR/NWAA284 | 2020-12-16 | 53739 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7JV5 | - | 3.0 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
CHEMBL1160787
chembl_ligand
pubchem
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP, Shen DD, Xu T, Liu YF, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE | 10.1016/J.CELL.2021.01.027 | 2021-02-24 | 53739 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7CX3 | - | 2.8 | PE2R2 | EP2 | Prostanoid | A (Rhodopsin) | Human | - | Nanobody-35 | - |
taprenepag
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | thromboxane A2, PGF2α, PGI2, PGD2, PGE1, PGE2 | small-molecule | Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y | 10.1126/SCIADV.ABF1268 | 2021-05-05 | 53739 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7EZH | - | 3.2 | CCKAR | CCK1 | Cholecystokinin | A (Rhodopsin) | Human | - | scFv16 | - |
CCK-8
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
peptide | Agonist | desulfated cholecystokinin-8, CCK-58, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8 | peptide | Liu Q, Yang D, Zhuang Y, Croll TI, Cai X, Dai A, He X, Duan J, Yin W, Ye C, Zhou F, Wu B, Zhao Q, Xu HE, Wang MW, Jiang Y | 10.1038/S41589-021-00841-3 | 2021-08-25 | 53741 | |
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 | desulfated gastrin-14, desulfated cholecystokinin-8, gastrin-34, gastrin-14, CCK-58, desulfated gastrin-17, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8, desulfated gastrin-34, gastrin-71, desulfated gastrin-71 | peptide | Zhang X, He C, Wang M, Zhou Q, Yang D, Zhu Y, Feng W, Zhang H, Dai A, Chu X, Wang J, Yang Z, Jiang Y, Sensfuss U, Tan Q, Han S, Reedtz-Runge S, Xu HE, Zhao S, Wang MW, Wu B, Zhao Q | 10.1038/S41589-021-00866-8 | 2021-10-13 | 53749 | |
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 | 53741 | |
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 | 53750 | |
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 | 53756 | |
Gs | αs | Human | Mini-Gs | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7WUI | - | 3.1 | AGRG2 | ADGRG2 | ADGRG | B2 (Adhesion) | Mouse | - | - | - |
IP15
|
peptide | Agonist | - | - | Xiao P, Guo S, Wen X, He QT, Lin H, Huang SM, Gou L, Zhang C, Yang Z, Zhong YN, Yang CC, Li Y, Gong Z, Tao XN, Yang ZS, Lu Y, Li SL, He JY, Wang C, Zhang L, Kong L, Sun JP, Yu X | 10.1038/S41586-022-04590-8 | 2022-04-27 | 53739 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7F23 | - | 3.6 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
dopamine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | Teng X, Chen S, Wang Q, Chen Z, Wang X, Huang N, Zheng S | 10.1126/SCIADV.ABO4158 | 2022-06-15 | 53739 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7XT9 | - | 3.2 | 5HT4R | 5-HT4 | 5-Hydroxytryptamine | A (Rhodopsin) | Human | BRIL | - | - |
5-hydroxytryptamine
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE | 10.1016/J.MOLCEL.2022.05.031 | 2022-07-27 | 53739 | |
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 | 53756 | |
Gs | αs | Human | - | 59 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7VVJ | 7VVJ_refined | 3.2 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
PTHrP[1-36]
|
peptide | Agonist | TIP39, PTHrP-(1-36), PTHrP, PTH | peptide | Kobayashi K, Kawakami K, Kusakizako T, Miyauchi H, Tomita A, Kobayashi K, Shihoya W, Yamashita K, Nishizawa T, Kato HE, Inoue A, Nureki O | 10.1016/J.MOLCEL.2022.07.003 | 2022-08-03 | 53739 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7VIG | 7VIG_refined | 2.9 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
icanbelimod
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | Yu L, He L, Gan B, Ti R, Xiao Q, Hu H, Zhu L, Wang S, Ren R | 10.1073/PNAS.2117716119 | 2022-09-28 | 53741 | |
Gi/o | αi1 | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7Y89 | - | 3.0 | GPR17 | GPR17 | A orphans | A (Rhodopsin) | Human | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | UDP, UDP-glucose, UDP-galactose, LTC4, LTD4, LTE4, ATP | small-molecule | Ye F, Wong TS, Chen G, Zhang Z, Zhang B, Gan S, Gao W, Li J, Wu Z, Pan X, Du Y | 10.1002/MCO2.159 | 2022-10-12 | 53741 | |
Gi/o | αi1 | Human | - | 64 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8EFL | 8EFL_refined | 3.2 | OPRM | μ | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
CHEMBL4452384
chembl_ligand
pubchem
|
small-molecule | Agonist | [Leu]enkephalin, β-endorphin, dynorphin A, [Met]enkephalin, endomorphin-1, endomorphin-2, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13) | peptide | Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, Rao Q, Yang J, Liu J, Zhou Q, Wang X, Liu M, Liu W, Jiang X, Yang D, Jiang H, Shen J, Melcher K, Chen H, Jiang Y, Cheng X, Wang MW, Xie X, Xu HE | 10.1016/J.CELL.2022.09.041 | 2022-11-09 | 53741 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7Y67 | 7Y67_refined | 2.8 | C5AR1 | C5a1 | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
C089
|
peptide | Agonist | ribosomal protein S19, C5a, C5a des-Arg, C3a | peptide | Feng Y, Zhao C, Deng Y, Wang H, Ma L, Liu S, Tian X, Wang B, Bin Y, Chen P, Yan W, Fu P, Shao Z | 10.1038/S41422-023-00779-2 | 2023-03-01 | 53741 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8HSC | - | 3.2 | GPR20 | GPR20 | A orphans | A (Rhodopsin) | Human | BRIL |
Antibody fab fragment light chain Antibody fab fragment heavy chain scFv16 |
- |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Lin X, Jiang S, Wu Y, Wei X, Han GW, Wu L, Liu J, Chen B, Zhang Z, Zhao S, Cherezov V, Xu F | 10.1038/S41421-023-00520-8 | 2023-03-08 | 53741 | |
Gs | αs | Human | Mini-Gs | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8IW9 | - | 3.1 | TAAR9 | TAAR9 | A orphans | A (Rhodopsin) | Mouse | - |
scFv16 Nanobody-35 |
- |
Cadaverine
pubchem
|
small-molecule | Agonist | - | - | Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP | 10.1038/S41586-023-06106-4 | 2023-05-31 | 53739 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8GUQ | 8GUQ_refined | 3.1 | CNR2 | CB2 | Cannabinoid | A (Rhodopsin) | Human | - | scFv16 | - |
olorinab
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | Li X, Chang H, Bouma J, de Paus LV, Mukhopadhyay P, Paloczi J, Mustafa M, van der Horst C, Kumar SS, Wu L, Yu Y, van den Berg RJBHN, Janssen APA, Lichtman A, Liu ZJ, Pacher P, van der Stelt M, Heitman LH, Hua T | 10.1038/S41467-023-37112-9 | 2023-05-10 | 53741 | |
Gq/11 | αq | Human | Mini-Gq | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7YDM | - | 2.9 | AGRE5 | ADGRE5 | ADGRE | B2 (Adhesion) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Wang N, Qian Y, Xia R, Zhu X, Xiong Y, Zhang A, Guo C, He Y | 10.1016/J.CHEMBIOL.2023.08.003 | 2023-07-12 | 53749 | |
Gq/11 | αq | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8IUM | - | 3.1 | PF2R | FP | Prostanoid | A (Rhodopsin) | Human | - |
scFv16 Nanobody-35 |
- |
tafluprost acid
pubchem
gtoplig
|
small-molecule | Agonist | thromboxane A2, PGF2α, PGI2, PGD2, PGE2 | small-molecule | Wu C, Xu Y, He Q, Li D, Duan J, Li C, You C, Chen H, Fan W, Jiang Y, Eric Xu H | 10.1038/S41467-023-38411-X | 2023-07-12 | 53749 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 8JD5 | - | 3.6 | GRM2 | mGlu2 | Metabotropic glutamate | C (Glutamate) | Human | - | scFv16 | - |
L-glutamic acid
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
pubchem
ADX88178 pubchem gtoplig chembl_ligand JNJ-40411813 pubchem gtoplig chembl_ligand drugbank |
small-molecule small-molecule small-molecule |
Agonist | L-glutamic acid | small-molecule | Wang X, Wang M, Xu T, Feng Y, Shao Q, Han S, Chu X, Xu Y, Lin S, Zhao Q, Wu B | 10.1038/S41422-023-00830-2 | 2023-06-21 | 53741 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8IJ3 | 8IJ3_refined | 3.3 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | β-D-hydroxybutyric acid, butyric acid | small-molecule | Pan X, Ye F, Ning P, Zhang Z, Li X, Zhang B, Wang Q, Chen G, Gao W, Qiu C, Wu Z, Li J, Zhu L, Xia J, Gong K, Du Y | 10.1038/S41421-023-00610-7 | 2024-01-03 | 53741 | |
Gs | αs | Human | - | 62 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8JIP | 8JIP_refined | 2.9 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
MEDI0382
|
peptide | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Li Y, Zhou Q, Dai A, Zhao F, Chang R, Ying T, Wu B, Yang D, Wang MW, Cong Z | 10.1073/PNAS.2303696120 | 2023-09-06 | 53739 | |
Gs | αs | Human | - | 55 | β1 | Human | γ2 | Human | Cryo-EM | 8U26 | 8U26_refined | 2.5 | NK1R | NK1 | Tachykinin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
substance P
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
|
peptide | Agonist | neuropeptide-γ, neurokinin A, neuropeptide K, neurokinin B, hemokinin 1, substance P | peptide | Chen M, Schmid MF, Chiu W | 10.1038/S41592-023-02082-9 | 2023-11-15 | 53739 | |
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 | 53851 | |
Gi/o | αt1 | Bovine | Only H5 | 3 | - | - | - | - | X-ray | 6NWE | - | 2.7 | OPSD | Rhodopsin | Opsins | A (Rhodopsin) | Bovine | - | - | - |
B-Octylglucoside
pubchem
|
small-molecule | unknown | - | - | - | - | 2020-02-12 | 53851 | |
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 | 53739 | |
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-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, Senel P, Stewart GD, Liang YL, Glukhova A, Venugopal H, Christopoulos A, Furness SGB, Miller LJ, Reedtz-Runge S, Langmead CJ, Gloriam DE, Danev R, Sexton PM, Wootten D | 10.1016/J.MOLCEL.2020.09.020 | 2020-09-09 | 53739 | |
Gs | αs | Human | Engineered G alpha | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7L1U | - | 3.2 | OX2R | OX2 | Orexin | A (Rhodopsin) | Human | - | scFv16 | - |
Orexin-A
pubchem
|
peptide | Agonist | orexin-A, orexin-B | peptide | Hong C, Byrne NJ, Zamlynny B, Tummala S, Xiao L, Shipman JM, Partridge AT, Minnick C, Breslin MJ, Rudd MT, Stachel SJ, Rada VL, Kern JC, Armacost KA, Hollingsworth SA, O'Brien JA, Hall DL, McDonald TP, Strickland C, Brooun A, Soisson SM, Hollenstein K | 10.1038/S41467-021-21087-6 | 2021-02-10 | 53739 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7AUE | 7AUE_refined | 3.0 | MC4R | MC4 | Melanocortin | A (Rhodopsin) | Human | - | scFv16 | - |
setmelanotide
pubchem
gtoplig
drug_central
chembl_ligand
drugbank
|
peptide | Agonist | β-MSH, α-MSH, agouti-related protein, γ-MSH, ACTH | peptide | Israeli H, Degtjarik O, Fierro F, Chunilal V, Gill AK, Roth NJ, Botta J, Prabahar V, Peleg Y, Chan LF, Ben-Zvi D, McCormick PJ, Niv MY, Shalev-Benami M | 10.1126/SCIENCE.ABF7958 | 2021-04-28 | 53739 | |
Gs | αs | Human | - | 58 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7F16 | - | 2.8 | PTH2R | PTH2 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
TIP39
gtoplig
|
peptide | Agonist | PTHrP, PTHrP-(1-36), PTH, PTHrP-(1-34) (human), TIP39 | peptide | Wang X, Cheng X, Zhao L, Wang Y, Ye C, Zou X, Dai A, Cong Z, Chen J, Zhou Q, Xia T, Jiang H, Xu HE, Yang D, Wang MW | 10.1073/PNAS.2101279118 | 2021-08-18 | 53739 | |
Gs | αs | Human | - | 48 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7PIU | - | 2.6 | MC4R | MC4 | Melanocortin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
setmelanotide
pubchem
gtoplig
drug_central
chembl_ligand
drugbank
|
peptide | Agonist | β-MSH, α-MSH, agouti-related protein, γ-MSH, ACTH | peptide | Heyder NA, Kleinau G, Speck D, Schmidt A, Paisdzior S, Szczepek M, Bauer B, Koch A, Gallandi M, Kwiatkowski D, Burger J, Mielke T, Beck-Sickinger AG, Hildebrand PW, Spahn CMT, Hilger D, Schacherl M, Biebermann H, Hilal T, Kuhnen P, Kobilka BK, Scheerer P | 10.1038/S41422-021-00569-8 | 2021-11-17 | 53739 | |
Gi/o | αo | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7W2Z | 7W2Z_refined | 2.8 | GHSR | ghrelin | Ghrelin | A (Rhodopsin) | Human | - | scFv16 | - |
Ghrelin
pubchem
|
peptide | Agonist | [des-Gln14]ghrelin, ghrelin | peptide | Qin J, Cai Y, Xu Z, Ming Q, Ji SY, Wu C, Zhang H, Mao C, Shen DD, Hirata K, Ma Y, Yan W, Zhang Y, Shao Z | 10.1038/S41467-022-27975-9 | 2022-01-19 | 53747 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7VL9 | - | 2.6 | CCR1 | CCR1 | Chemokine | A (Rhodopsin) | Human | - | scFv16 | - |
CCL15(26-92)
|
peptide | Agonist | CCL14, CCL8, CCL13, CCL15, CCL4, CCL23, CCL7, CCL5, CCL3, CCL16 | peptide | Shao Z, Shen Q, Yao B, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Ma H, Chen ZH, Xu HE, Ying S, Zhang Y, Shen H | 10.1038/S41589-021-00918-Z | 2022-03-23 | 53741 | |
G12/13 | α13 | Human | Gi2-mini-G13 chimera | 56 | β1 | Human | γ2 | Human | Cryo-EM | 7SF8 | - | 2.7 | AGRG1 | ADGRG1 | ADGRG | B2 (Adhesion) | Human | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Barros-Alvarez X, Nwokonko RM, Vizurraga A, Matzov D, He F, Papasergi-Scott MM, Robertson MJ, Panova O, Yardeni EH, Seven AB, Kwarcinski FE, Su H, Peroto MC, Meyerowitz JG, Shalev-Benami M, Tall GG, Skiniotis G | 10.1038/S41586-022-04575-7 | 2022-04-27 | 53754 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7V6A | - | 3.6 | ACM4 | M4 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | scFv16 | - |
methyl 4-[4-(3-methyl-2-oxidanylidene-benzimidazol-1-yl)piperidin-1-yl]piperidine-1-carboxylate
pubchem
|
small-molecule | Allosteric agonist | acetylcholine | small-molecule | Wang J, Wu M, Chen Z, Wu L, Wang T, Cao D, Wang H, Liu S, Xu Y, Li F, Liu J, Chen N, Zhao S, Cheng J, Wang S, Hua T | 10.1038/S41467-022-30595-Y | 2022-05-11 | 53741 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7XBX | - | 3.4 | CX3C1 | CX3CR1 | Chemokine | A (Rhodopsin) | Human | - | - | - |
CX3CL1
|
peptide | Agonist | CX3CL1 | peptide | - | - | 2022-07-13 | 53741 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7VFX | 7VFX_refined | 2.8 | FPR1 | FPR1 | Formylpeptide | A (Rhodopsin) | Human | - | scFv16 | - |
Peptide agonist fMet-Ile-Phe-Leu
pubchem
|
peptide | Agonist | fMet-Leu-Phe, cathepsin G, annexin I, spinorphin | peptide | Chen G, Wang X, Liao Q, Ge Y, Jiao H, Chen Q, Liu Y, Lyu W, Zhu L, van Zundert GCP, Robertson MJ, Skiniotis G, Du Y, Hu H, Ye RD | 10.1038/S41467-022-32822-Y | 2022-09-21 | 53741 | |
Gq/11 | αq | Human | Gs-mini-Gq chimera | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8DWH | 8DWH_refined | 3.3 | MRGX1 | MRGPRX1 | A orphans | A (Rhodopsin) | Human | - | - | - |
compound 16 [PMID: 31498617]
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | bovine adrenal medulla peptide 8-22 | peptide | Liu Y, Cao C, Huang XP, Gumpper RH, Rachman MM, Shih SL, Krumm BE, Zhang S, Shoichet BK, Fay JF, Roth BL | 10.1038/S41589-022-01173-6 | 2022-11-02 | 53749 | |
Gi/o | αi1 | Human | - | 62 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8F7X | 8F7X_refined | 3.3 | OPRX | NOP | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
nociceptin/orphanin FQ
pubchem
gtoplig
chembl_ligand
gtoplig
pubchem
pubchem
|
peptide | Agonist | nociceptin/orphanin FQ | peptide | Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y, Roth BL, Xu HE | 10.1016/J.CELL.2022.12.026 | 2022-12-14 | 53741 | |
Gi/o | αo | Human | Mini-Go | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8FN0 | - | 2.9 | NTR1 | NTS1 | Neurotensin | A (Rhodopsin) | Rat | - | scFv16 | - |
neurotensin
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
CHEMBL4576388 chembl_ligand pubchem |
peptide small-molecule |
Agonist PAM |
neurotensin, neuromedin N | peptide | Krumm BE, DiBerto JF, Olsen RHJ, Kang HJ, Slocum ST, Zhang S, Strachan RT, Huang XP, Slosky LM, Pinkerton AB, Barak LS, Caron MG, Kenakin T, Fay JF, Roth BL | 10.1021/ACS.BIOCHEM.3C00029 | 2023-03-29 | 53747 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 8ID6 | - | 2.8 | FFAR4 | FFA4 | Free fatty acid | A (Rhodopsin) | Human | - | scFv16 | - |
oleic acid
pubchem
gtoplig
chembl_ligand
drug_central
|
small-molecule | Agonist | myristic acid, linoleic acid, α-linolenic acid, oleic acid | small-molecule | Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP | 10.1126/SCIENCE.ADD6220 | 2023-03-15 | 53741 | |
Gq/11 | αq | Human | - | 59 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7XWO | 7XWO_refined | 2.7 | NK2R | NK2 | Tachykinin | A (Rhodopsin) | Human | BRIL | scFv16 | - |
HIS-LYS-THR-ASP-SER-PHE-VAL-GLY-LEU-MET-NH2
|
peptide | Agonist | neurokinin A, neuropeptide K, neurokinin B, neuropeptide γ, hemokinin 1, substance P | peptide | - | - | 2023-05-31 | 53749 | |
Gi/o | αi1 | Human | - | 64 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8HK2 | - | 2.9 | C3AR | C3a | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
C3a anaphylatoxin
pubchem
|
peptide | Agonist | C5a, C3a | peptide | Wang Y, Liu W, Xu Y, He X, Yuan Q, Luo P, Fan W, Zhu J, Zhang X, Cheng X, Jiang Y, Xu HE, Zhuang Y | 10.1038/S41589-023-01339-W | 2023-05-10 | 53741 | |
Gi/o | αi1 | Human | - | 65 | β1 | Human | γ2 | Human | Cryo-EM | 8IC0 | - | 3.4 | CXCR1 | CXCR1 | Chemokine | A (Rhodopsin) | Human | - | scFv16 | - |
Interleukin-8
pubchem
|
protein | Agonist | cytokine domain of tyrosyl tRNA synthetase, CXCL8, CXCL6 | peptide | Ishimoto N, Park JH, Kawakami K, Tajiri M, Mizutani K, Akashi S, Tame JRH, Inoue A, Park SY | 10.1038/S41467-023-39799-2 | 2023-07-19 | 53741 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8PM2 | - | 2.9 | TAA7F | TAAR7F | A orphans | A (Rhodopsin) | Mouse | - | Nanobody-35 | - |
N,N-Dimethylcyclohexylamine
pubchem
|
small-molecule | Agonist | - | - | Gusach A, Lee Y, Khoshgrudi AN, Mukhaleva E, Ma N, Koers EJ, Chen Q, Edwards PC, Huang F, Kim J, Mancia F, Verprintsev DB, Vaidehi N, Weyand SN, Tate CG | 10.1101/2023.07.07.547762 | 2023-08-09 | 53739 | |
Gs | αs | Human | - | 54 | β1 | Human | γ2 | Human | Cryo-EM | 8GD9 | - | 3.2 | PE2R4 | EP4 | Prostanoid | A (Rhodopsin) | Human | - | - | - |
4-({2-[(1R,2R,3R,5S)-3,5-dihydroxy-2-{(3S)-3-hydroxy-4-[3-(methoxymethyl)phenyl]butyl}cyclopentyl]ethyl}sulfanyl)butanoic acid
pubchem
|
small-molecule | Agonist | thromboxane A2, PGF2α, PGI2, PGD2, PGE1, PGE2 | small-molecule | Huang SM, Xiong MY, Liu L, Mu J, Wang MW, Jia YL, Cai K, Tie L, Zhang C, Cao S, Wen X, Wang JL, Guo SC, Li Y, Qu CX, He QT, Cai BY, Xue C, Gan S, Xie Y, Cong X, Yang Z, Kong W, Li S, Li Z, Xiao P, Yang F, Yu X, Guan YF, Zhang X, Liu Z, Yang BX, Du Y, Sun JP | 10.1073/PNAS.2216329120 | 2024-01-10 | 53739 | |
Gi/o | αo | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8I95 | - | 2.9 | C3AR | C3a | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
EP54 ligand
|
peptide | Agonist | C5a, C3a | peptide | Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C | 10.1016/J.CELL.2023.09.020 | 2023-10-18 | 53747 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 8JHY | - | 2.9 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | - | scFv16 | - |
compound 9n [PMID: 18752940]
pubchem
gtoplig
chembl_ligand
|
small-molecule | PAM | β-D-hydroxybutyric acid, butyric acid | small-molecule | Zhao C, Wang H, Liu Y, Cheng L, Wang B, Tian X, Fu H, Wu C, Li Z, Shen C, Yu J, Yang S, Hu H, Fu P, Ma L, Wang C, Yan W, Shao Z | 10.1016/J.MOLCEL.2023.07.030 | 2023-09-06 | 53741 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 8JZ7 | 8JZ7_refined | 2.6 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | - | scFv16 | - |
MK 6892
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | Cheng L, Sun S, Wang H, Zhao C, Tian X, Liu Y, Fu P, Shao Z, Chai R, Yan W | 10.1038/S41392-023-01625-Y | 2023-10-04 | 53741 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8WC3 | - | 3.0 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Mouse | - | scFv16 | - |
ulotaront
pubchem
gtoplig
drugbank
chembl_ligand
|
small-molecule | Agonist | β-phenylethylamine, 3-iodothyronamine, tyramine | small-molecule | Shang P, Rong N, Jiang JJ, Cheng J, Zhang MH, Kang D, Qi L, Guo L, Yang GM, Liu Q, Zhou Z, Li XB, Zhu KK, Meng QB, Han X, Yan W, Kong Y, Yang L, Wang X, Lei D, Feng X, Liu X, Yu X, Wang Y, Li Q, Shao ZH, Yang F, Sun JP | 10.1016/J.CELL.2023.10.014 | 2023-12-27 | 53739 | |
Gi/o | αt1 | Bovine | Only H5 | 3 | - | - | - | - | X-ray | 4BEY | - | 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 | 53851 | |
Gi/o | αt1 | Bovine | Only H5 | 3 | - | - | - | - | X-ray | 5WKT | - | 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 | 53851 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 6KPG | 6KPG_refined | 3.0 | CNR1 | CB1 | Cannabinoid | A (Rhodopsin) | Human | - | scFv16 | - |
AM841
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | Hua T, Li X, Wu L, Iliopoulos-Tsoutsouvas C, Wang Y, Wu M, Shen L, Brust CA, Nikas SP, Song F, Song X, Yuan S, Sun Q, Wu Y, Jiang S, Grim TW, Benchama O, Stahl EL, Zvonok N, Zhao S, Bohn LM, Makriyannis A, Liu ZJ | 10.1016/J.CELL.2020.01.008 | 2020-02-12 | 53741 | |
Gi/o | αt1 | Bovine | Only H5 | 3 | - | - | - | - | X-ray | 6PEL | - | 3.2 | OPSD | Rhodopsin | Opsins | A (Rhodopsin) | Bovine | - | - | - |
Citronellol
pubchem
|
small-molecule | unknown | - | - | - | - | 2020-06-24 | 53851 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7KH0 | - | 2.8 | V2R | V2 | Vasopressin and oxytocin | A (Rhodopsin) | Human | - |
scFv16 Nanobody-35 |
- |
vasopressin
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
peptide | Agonist | vasopressin, oxytocin | peptide | Wang L, Xu J, Cao S, Sun D, Liu H, Lu Q, Liu Z, Du Y, Zhang C | 10.1038/S41422-021-00483-Z | 2021-05-26 | 53739 | |
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 | 53749 | |
Gi/o | αi1 | Human | - | 40 | β1 | Human | γ2 | Human | Cryo-EM | 7WF7 | 7WF7_refined | 3.4 | S1PR1 | S1P1 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
sphingosine 1-phosphate
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | Xu Z, Ikuta T, Kawakami K, Kise R, Qian Y, Xia R, Sun MX, Zhang A, Guo C, Cai XH, Huang Z, Inoue A, He Y | 10.1038/S41589-021-00930-3 | 2022-01-05 | 53741 | |
Gi/o | αi3 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7T11 | 7T11_refined | 2.7 | SSR2 | SST2 | Somatostatin | A (Rhodopsin) | Human | - | scFv16 | - |
Octreotide
|
peptide | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | Robertson MJ, Meyerowitz JG, Panova O, Borrelli K, Skiniotis G | 10.1038/S41594-022-00727-5 | 2022-03-09 | 53743 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7TYL | - | 3.3 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - | Nanobody-35 | - |
Amylin rat
pubchem
|
peptide | Agonist | adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP | peptide | Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM | 10.1126/SCIENCE.ABM9609 | 2022-03-23 | 53739 | |
G12/13 | α13 | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7T6B | 7T6B_refined | 3.2 | S1PR2 | S1P2 | Lysophospholipid (S1P) | A (Rhodopsin) | Human | - | scFv16 | - |
sphingosine 1-phosphate
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | Chen H, Chen K, Huang W, Staudt LM, Cyster JG, Li X | 10.1126/SCIADV.ABN0067 | 2022-04-06 | 53754 | |
Gq/11 | αq | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7W57 | - | 3.2 | NMUR2 | NMU2 | Neuromedin U | A (Rhodopsin) | Human | - | scFv16 | - |
Neuromedin-S
|
peptide | Agonist | neuromedin U-23, neuromedin S-36, neuromedin S-33, neuromedin U-25 | peptide | You C, Zhang Y, Xu P, Huang S, Yin W, Eric Xu H, Jiang Y | 10.1038/S41467-022-29683-W | 2022-04-20 | 53749 | |
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 | 53741 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7X9Y | 7X9Y_refined | 3.1 | CCR3 | CCR3 | Chemokine | A (Rhodopsin) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | CCL28, CCL8, CXCL11, CCL13, CCL15, CXCL9, CXCL10, CCL7, CCL2, CCL5, CCL11, CCL24, CCL26 | peptide | Shao Z, Tan Y, Shen Q, Hou L, Yao B, Qin J, Xu P, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Chen ZH, Jiang Y, Xu HE, Ying S, Ma H, Zhang Y, Shen H | 10.1038/S41421-022-00403-4 | 2022-08-24 | 53741 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7XZ6 | - | 2.8 | GP119 | GPR119 | GPR18, GPR55 and GPR119 | A (Rhodopsin) | Human | BRIL | Nanobody-35 | - |
APD668
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | N-oleoylethanolamide, anandamide, N-palmitoylethanolamine, SEA | small-molecule | Xu P, Huang S, Guo S, Yun Y, Cheng X, He X, Cai P, Lan Y, Zhou H, Jiang H, Jiang Y, Xie X, Xu HE | 10.1038/S41594-022-00816-5 | 2022-08-24 | 53739 | |
Gq/11 | αq | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7WXU | - | 2.9 | AGRF1 | ADGRF1 | ADGRF | B2 (Adhesion) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y | 10.1038/S41467-022-33173-4 | 2022-09-28 | 53749 | |
Gi/o | αgust | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7XP4 | - | 3.0 | T2R46 | TAS2R46 | Taste 2 | T (Taste 2) | Human | - | Nanobody-35 | Endoglucanase H |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Xu W, Wu L, Liu S, Liu X, Cao X, Zhou C, Zhang J, Fu Y, Guo Y, Wu Y, Tan Q, Wang L, Liu J, Jiang L, Fan Z, Pei Y, Yu J, Cheng J, Zhao S, Hao X, Liu ZJ, Hua T | 10.1126/SCIENCE.ABO1633 | 2022-10-12 | 53746 | |
Gs | αs | Human | - | 55 | β1 | Human | γ2 | Human | Cryo-EM | 8E3Z | 8E3Z_refined | 2.7 | VIPR1 | VPAC1 | VIP and PACAP | B1 (Secretin) | Human | - | Nanobody-35 | - |
Vasoactive intestinal polypeptide
pubchem
|
small-molecule | Agonist | VIP, PHI, PHM, secretin, PACAP-27, GHRH, PACAP-38 | peptide | Piper SJ, Deganutti G, Lu J, Zhao P, Liang YL, Lu Y, Fletcher MM, Hossain MA, Christopoulos A, Reynolds CA, Danev R, Sexton PM, Wootten D | 10.1038/S41467-022-34629-3 | 2022-11-23 | 53739 | |
Gs | αs | Human | Mini-Gs | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8HDP | - | 3.2 | AA2BR | A2B | Adenosine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
adenosine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | adenosine | small-molecule | Cai H, Xu Y, Guo S, He X, Sun J, Li X, Li C, Yin W, Cheng X, Jiang H, Xu HE, Xie X, Jiang Y | 10.1038/S41421-022-00503-1 | 2023-01-18 | 53739 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7XK8 | 7XK8_refined | 3.3 | NMUR2 | NMU2 | Neuromedin U | A (Rhodopsin) | Human | - | - | - |
Neuromedin U-25 (human)
pubchem
|
peptide | Agonist | neuromedin U-23, neuromedin S-36, neuromedin S-33, neuromedin U-25 | peptide | Zhao W, Zhang W, Wang M, Lu M, Chen S, Tang T, Schnapp G, Wagner H, Brennauer A, Yi C, Chu X, Han S, Wu B, Zhao Q | 10.1038/S41467-022-34814-4 | 2023-02-22 | 53741 | |
Gs | αs | Human | Mini-Gs | 57 | β1 | Human | γ2 | Human | Cryo-EM | 7XY7 | - | 3.3 | AA2BR | A2B | Adenosine | A (Rhodopsin) | Human | BRIL | - | - |
NECA
pubchem
gtoplig
chembl_ligand
gtoplig
|
small-molecule | Agonist | adenosine | small-molecule | Chen Y, Zhang J, Weng Y, Xu Y, Lu W, Liu W, Liu M, Hua T, Song G | 10.1126/SCIADV.ADD3709 | 2023-05-03 | 53739 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8ITF | - | 3.5 | TAAR9 | TAAR9 | A orphans | A (Rhodopsin) | Mouse | - |
scFv16 Nanobody-35 |
- |
N,N-Dimethylcyclohexylamine
pubchem
|
small-molecule | Agonist | - | - | Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP | 10.1038/S41586-023-06106-4 | 2023-05-31 | 53739 | |
Gq/11 | αq | Human | Mini-Gq | 51 | - | - | - | - | Cryo-EM | 7YMH | 7YMH_refined | 3.5 | ADA1A | α1A | Adrenoceptors | A (Rhodopsin) | Human | - | Nanobody-29 | - |
Noradrenaline
pubchem
|
small-molecule | Agonist | (-)-adrenaline, (-)-noradrenaline | small-molecule | Toyoda Y, Zhu A, Kong F, Shan S, Zhao J, Wang N, Sun X, Zhang L, Yan C, Kobilka BK, Liu X | 10.1038/S41467-023-39310-X | 2023-07-05 | 53749 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8F0K | - | 1.9 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - |
Nanobody-35 RAMP3 |
- |
San385
|
peptide | Agonist | adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP | peptide | Cao J, Belousoff MJ, Gerrard E, Danev R, Fletcher MM, Dal Maso E, Schreuder H, Lorenz K, Evers A, Tiwari G, Besenius M, Li Z, Johnson RM, Wootten D, Sexton PM | 10.1038/S41589-023-01393-4 | 2023-08-02 | 53739 | |
Gi/o | αi1 | Human | - | 62 | β1 | Mouse | γ2 | Mouse | Cryo-EM | 8IHB | - | 2.9 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | BRIL | - | - |
GSK256073
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | Suzuki S, Tanaka K, Nishikawa K, Suzuki H, Oshima A, Fujiyoshi Y | 10.1038/S41467-023-41650-7 | 2023-09-13 | 53741 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 8JIL | - | 3.5 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | - | scFv16 | - |
nicotinic acid
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
pubchem
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | Zhao C, Wang H, Liu Y, Cheng L, Wang B, Tian X, Fu H, Wu C, Li Z, Shen C, Yu J, Yang S, Hu H, Fu P, Ma L, Wang C, Yan W, Shao Z | 10.1016/J.MOLCEL.2023.07.030 | 2023-09-06 | 53741 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8K4N | 8K4N_refined | 2.8 | GPR34 | GPR34 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
(2R)-2-azanyl-3-[oxidanyl-[(2R)-2-oxidanyl-3-tetradec-9-enoyloxy-propoxy]phosphoryl]oxy-propanoic acid
pubchem
|
small-molecule | Agonist | lysophosphatidylserine | small-molecule | - | - | 2023-10-25 | 53741 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8WC7 | - | 3.1 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Mouse | - | scFv16 | - |
2-[4-(3-Fluorophenyl)phenyl]ethan-1-amine
pubchem
|
small-molecule | Agonist | β-phenylethylamine, 3-iodothyronamine, tyramine | small-molecule | Shang P, Rong N, Jiang JJ, Cheng J, Zhang MH, Kang D, Qi L, Guo L, Yang GM, Liu Q, Zhou Z, Li XB, Zhu KK, Meng QB, Han X, Yan W, Kong Y, Yang L, Wang X, Lei D, Feng X, Liu X, Yu X, Wang Y, Li Q, Shao ZH, Yang F, Sun JP | 10.1016/J.CELL.2023.10.014 | 2023-12-27 | 53739 | |
Gs | αs | Human | - | 57 | β1 | Human | γ2 | Human | Cryo-EM | 6VCB | - | 3.3 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
glucagon-like peptide 1-(7-37)
pubchem
gtoplig
chembl_ligand
gtoplig
pubchem
pubchem
CHEMBL5197819 chembl_ligand pubchem |
peptide small-molecule |
Agonist PAM |
glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Bueno AB, Sun B, Willard FS, Feng D, Ho JD, Wainscott DB, Showalter AD, Vieth M, Chen Q, Stutsman C, Chau B, Ficorilli J, Agejas FJ, Cumming GR, Jimenez A, Rojo I, Kobilka TS, Kobilka BK, Sloop KW | 10.1038/S41589-020-0589-7 | 2020-07-22 | 53739 | |
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 | 53755 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7CKX | - | 3.5 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
A77636
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | - | - | 2021-03-03 | 53739 | |
Gs | αs | Human | - | 55 | β1 | Human | γ2 | Human | Cryo-EM | 7BB7 | - | 4.4 | V2R | V2 | Vasopressin and oxytocin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
vasopressin
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
peptide | Agonist | vasopressin, oxytocin | peptide | Bous J, Orcel H, Floquet N, Leyrat C, Lai-Kee-Him J, Gaibelet G, Ancelin A, Saint-Paul J, Trapani S, Louet M, Sounier R, Demene H, Granier S, Bron P, Mouillac B | 10.1126/SCIADV.ABG5628 | 2021-06-02 | 53739 | |
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 | 53739 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7VLA | 7VLA_refined | 2.7 | CCR1 | CCR1 | Chemokine | A (Rhodopsin) | Human | - | scFv16 | - |
CCL15(27-92)
|
peptide | Agonist | CCL14, CCL8, CCL13, CCL15, CCL4, CCL23, CCL7, CCL5, CCL3, CCL16 | peptide | Shao Z, Shen Q, Yao B, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Ma H, Chen ZH, Xu HE, Ying S, Zhang Y, Shen H | 10.1038/S41589-021-00918-Z | 2022-03-23 | 53741 | |
Gs | αs | Human | - | 56 | β1 | Human | γ2 | Human | Cryo-EM | 7RG9 | 7RG9_refined | 3.2 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - |
scFv16 Nanobody-35 |
- |
Apo (no ligand)
|
none | Apo (no ligand) | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW | 10.1073/PNAS.2116506119 | 2022-04-13 | 53739 | |
Gs | αs | Bovine | - | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7VQX | - | 2.7 | VIPR2 | VPAC2 | VIP and PACAP | B1 (Secretin) | Human | - | Nanobody-35 | - |
PACAP-27
pubchem
gtoplig
pubchem
|
peptide | Agonist | VIP, PHI, secretin, PACAP-27, GHRH, PACAP-38 | peptide | Xu Y, Feng W, Zhou Q, Liang A, Li J, Dai A, Zhao F, Yan J, Chen CW, Li H, Zhao LH, Xia T, Jiang Y, Xu HE, Yang D, Wang MW | 10.1038/S41467-022-30041-Z | 2022-05-18 | 53756 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7XTA | 7XTA_refined | 3.2 | 5HT4R | 5-HT4 | 5-Hydroxytryptamine | A (Rhodopsin) | Human | BRIL | scFv16 | - |
5-hydroxytryptamine
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE | 10.1016/J.MOLCEL.2022.05.031 | 2022-07-27 | 53741 | |
Gq/11 | αq | Human | Gi2-mini-Gq chimera | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8DPH | - | 3.2 | 5HT2C | 5-HT2C | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | scFv16 | - |
lorcaserin
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Gumpper RH, Fay JF, Roth BL | 10.1016/J.CELREP.2022.111211 | 2022-08-24 | 53749 | |
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 | 53739 | |
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 | 53750 | |
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, PHI, PHM, PHV, PACAP-27, 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 | 53739 | |
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 | 53739 | |
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 | 53741 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7CMV | - | 2.7 | DRD3 | D3 | Dopamine | A (Rhodopsin) | Human | BRIL | scFv16 | - |
CHEMBL70565
chembl_ligand
chembl_ligand
pubchem
|
small-molecule | Agonist | dopamine | small-molecule | 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 | 53741 | |
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 | 53756 | |
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-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Johnson RM, Zhang X, Piper SJ, Nettleton TJ, Vandekolk TH, Langmead CJ, Danev R, Sexton PM, Wootten D | 10.1016/J.BBRC.2021.09.016 | 2021-10-06 | 53739 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7VUI | 7VUI_refined | 3.3 | GP139 | GPR139 | A orphans | A (Rhodopsin) | Human | - | Nanobody-35 | Xylanase |
JNJ-63533054
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | L-phenylalanine, L-tryptophan | small-molecule | Zhou Y, Daver H, Trapkov B, Wu L, Wu M, Harpsoe K, Gentry PR, Liu K, Larionova M, Liu J, Chen N, Brauner-Osborne H, Gloriam DE, Hua T, Liu ZJ | 10.1038/S41422-021-00591-W | 2021-12-29 | 53739 | |
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 | 53741 | |
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 | 53747 | |
Gi/o | αi2 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7WVX | - | 2.8 | FPR2 | FPR2/ALX | Formylpeptide | A (Rhodopsin) | Human | BRIL | - | - |
humanin
pubchem
gtoplig
chembl_ligand
pubchem
|
peptide | Agonist | humanin, aspirin-triggered resolvin D1, LXA4, resolvin D1, serum amyloid A, PrP106-126, 15-deoxy-LXA4, aspirin triggered lipoxin A4, LL-37, LTC4, annexin I, fMet-Leu-Phe, LTD4 | peptide | Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B | 10.1038/S41467-022-29361-X | 2022-04-13 | 53742 | |
Gs | αs | Bovine | - | 60 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7WBJ | - | 3.4 | VIPR2 | VPAC2 | VIP and PACAP | B1 (Secretin) | Human | - | Nanobody-35 | - |
PACAP-27
pubchem
gtoplig
pubchem
|
peptide | Agonist | VIP, PHI, secretin, PACAP-27, GHRH, PACAP-38 | peptide | Xu Y, Feng W, Zhou Q, Liang A, Li J, Dai A, Zhao F, Yan J, Chen CW, Li H, Zhao LH, Xia T, Jiang Y, Xu HE, Yang D, Wang MW | 10.1038/S41467-022-30041-Z | 2022-05-18 | 53756 | |
Gi/o | αo | Human | Mini-Go | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7UM5 | 7UM5_refined | 2.7 | 5HT5A | 5-HT5A | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | scFv16 | - |
5-CT
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL | 10.1038/S41594-022-00796-6 | 2022-07-20 | 53747 | |
Gq/11 | αq | Human | Mini-Gq | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7Y27 | 7Y27_refined | 3.5 | SSR2 | SST2 | Somatostatin | A (Rhodopsin) | Human | - | scFv16 | - |
SOMATOSTATIN
chembl_ligand
pubchem
|
protein | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | Chen S, Teng X, Zheng S | 10.1038/S41589-022-01130-3 | 2022-10-19 | 53749 | |
Gi/o | αi1 | Human | - | 63 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8F7R | - | 3.3 | OPRM | μ | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
endomorphin-1
pubchem
gtoplig
chembl_ligand
|
peptide | Agonist | [Leu]enkephalin, β-endorphin, dynorphin A, [Met]enkephalin, endomorphin-1, endomorphin-2, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13) | peptide | Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y, Roth BL, Xu HE | 10.1016/J.CELL.2022.12.026 | 2022-12-14 | 53741 | |
Gq/11 | αq | Human | Mini-Gq | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8FMZ | - | 2.6 | NTR1 | NTS1 | Neurotensin | A (Rhodopsin) | Rat | - | scFv16 | - |
neurotensin
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
|
peptide | Agonist | neurotensin, neuromedin N | peptide | Krumm BE, DiBerto JF, Olsen RHJ, Kang HJ, Slocum ST, Zhang S, Strachan RT, Huang XP, Slosky LM, Pinkerton AB, Barak LS, Caron MG, Kenakin T, Fay JF, Roth BL | 10.1021/ACS.BIOCHEM.3C00029 | 2023-03-29 | 53749 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 8ID4 | - | 3.1 | FFAR4 | FFA4 | Free fatty acid | A (Rhodopsin) | Human | - | scFv16 | - |
linoleic acid
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
|
small-molecule | Agonist | myristic acid, linoleic acid, α-linolenic acid, oleic acid | small-molecule | Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP | 10.1126/SCIENCE.ADD6220 | 2023-03-15 | 53741 | |
Gs | αs | Human | - | 45 | β1 | Human | γ2 | Human | Cryo-EM | 8IW4 | - | 3.5 | TAAR9 | TAAR9 | A orphans | A (Rhodopsin) | Mouse | - | scFv16 | - |
SPERMIDINE
chembl_ligand
pubchem
|
small-molecule | Agonist | - | - | Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP | 10.1038/S41586-023-06106-4 | 2023-05-31 | 53739 | |
Gs | αs | Human | - | 56 | β1 | Human | γ2 | Human | Cryo-EM | 7Y3G | 7Y3G_refined | 2.8 | GPR12 | GPR12 | A orphans | A (Rhodopsin) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | sphingosine 1-phosphate | small-molecule | Li H, Zhang J, Yu Y, Luo F, Wu L, Liu J, Chen N, Liu Z, Hua T | 10.1016/J.SCIB.2022.12.023 | 2023-06-07 | 53739 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8IA8 | - | 2.9 | C3AR | C3a | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
ALA-SER-LYS-LEU-GLY-LEU-ALA-ARG
|
peptide | Agonist | C5a, C3a | peptide | - | - | 2023-05-24 | 53741 | |
Gq/11 | αq | Human | - | 56 | β1 | Human | γ2 | Human | Cryo-EM | 8H0Q | - | 3.3 | GRPR | BB2 | Bombesin | A (Rhodopsin) | Human | - | - | - |
Gastrin-releasing peptide
pubchem
|
peptide | Agonist | neuromedin B, gastrin releasing peptide(14-27) (human), GRP-(18-27), gastrin-releasing peptide, neuromedin C | peptide | Li C, Xu Y, Liu H, Cai H, Jiang Y, Xu HE, Yin W | 10.1038/S41422-022-00743-6 | 2023-08-09 | 53749 | |
Gs | αs | Human | Gi1-Gs chimera | 59 | β1 | Human | γ2 | Bovine | Cryo-EM | 8IOD | - | 2.6 | MC5R | MC5 | Melanocortin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
PG-901
pubchem
|
peptide | Agonist | β-MSH, α-MSH, agouti-related protein, γ-MSH, ACTH | peptide | Chen VB, Arendall WB 3rd, Headd JJ, Keedy DA, Immormino RM, Kapral GJ, Murray LW, Richardson JS, Richardson DC | 10.1107/S0907444909042073 | 2023-09-20 | 53739 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8JLQ | - | 2.8 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Human | BRIL | scFv16 | - |
fenoldopam
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
gtoplig
chembl_ligand
pubchem
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, dopamine | small-molecule | Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z | 10.1038/S41586-023-06804-Z | 2023-11-15 | 53739 | |
Gq/11 | αq | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8WC9 | - | 3.2 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Mouse | - | scFv16 | - |
CHEMBL476516
chembl_ligand
pubchem
|
small-molecule | Agonist | β-phenylethylamine, 3-iodothyronamine, tyramine | small-molecule | Shang P, Rong N, Jiang JJ, Cheng J, Zhang MH, Kang D, Qi L, Guo L, Yang GM, Liu Q, Zhou Z, Li XB, Zhu KK, Meng QB, Han X, Yan W, Kong Y, Yang L, Wang X, Lei D, Feng X, Liu X, Yu X, Wang Y, Li Q, Shao ZH, Yang F, Sun JP | 10.1016/J.CELL.2023.10.014 | 2023-12-27 | 53749 | |
Gi/o | αi1 | Human | - | 100 | β1 | Human | γ2 | Human | Cryo-EM | 6PT0 | 6PT0_refined | 3.2 | CNR2 | CB2 | Cannabinoid | A (Rhodopsin) | Human | - | scFv16 | - |
WIN55212-2
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | Xing C, Zhuang Y, Xu TH, Feng Z, Zhou XE, Chen M, Wang L, Meng X, Xue Y, Wang J, Liu H, McGuire TF, Zhao G, Melcher K, Zhang C, Xu HE, Xie XQ | 10.1016/J.CELL.2020.01.007 | 2020-02-12 | 53741 | |
Gs | αs | Human | - | 56 | β1 | Human | γ2 | Human | Cryo-EM | 6XOX | - | 3.1 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - |
scFv16 Nanobody-35 |
- |
orforglipron
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Kawai T, Sun B, Yoshino H, Feng D, Suzuki Y, Fukazawa M, Nagao S, Wainscott DB, Showalter AD, Droz BA, Kobilka TS, Coghlan MP, Willard FS, Kawabe Y, Kobilka BK, Sloop KW | 10.1073/PNAS.2014879117 | 2020-11-18 | 53739 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7JVP | - | 2.9 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
39YLC3L0ZU
pubchem
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | - | - | 2021-02-24 | 53739 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7CX4 | 7CX4_refined | 2.9 | PE2R2 | EP2 | Prostanoid | A (Rhodopsin) | Human | - | Nanobody-35 | - |
evatanepag
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | thromboxane A2, PGF2α, PGI2, PGD2, PGE1, PGE2 | small-molecule | Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y | 10.1126/SCIADV.ABF1268 | 2021-05-05 | 53739 | |
Gq/11 | αq | Human | Engineered G alpha | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7F9Y | - | 2.9 | GHSR | ghrelin | Ghrelin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
ghrelin
gtoplig
|
peptide | Agonist | [des-Gln14]ghrelin, ghrelin | peptide | Wang Y, Guo S, Zhuang Y, Yun Y, Xu P, He X, Guo J, Yin W, Xu HE, Xie X, Jiang Y | 10.1038/S41467-021-25364-2 | 2021-08-18 | 53749 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7S1M | 7S1M_refined | 2.4 | GLP1R | GLP-1 | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
exendin-4
pubchem
gtoplig
pubchem
|
peptide | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | Cary BP, Deganutti G, Zhao P, Truong TT, Piper SJ, Liu X, Belousoff MJ, Danev R, Sexton PM, Wootten D, Gellman SH | 10.1038/S41589-021-00945-W | 2022-01-05 | 53739 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7VL8 | 7VL8_refined | 2.9 | CCR1 | CCR1 | Chemokine | A (Rhodopsin) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | CCL14, CCL8, CCL13, CCL15, CCL4, CCL23, CCL7, CCL5, CCL3, CCL16 | peptide | Shao Z, Shen Q, Yao B, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Ma H, Chen ZH, Xu HE, Ying S, Zhang Y, Shen H | 10.1038/S41589-021-00918-Z | 2022-03-23 | 53741 | |
Gs | αs | Bovine | - | 59 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7FIN | - | 3.1 | GIPR | GIP | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
Peptide-20
|
peptide | Agonist | gastric inhibitory polypeptide | peptide | Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW | 10.1038/S41467-022-28683-0 | 2022-02-23 | 53756 | |
Gs | αs | Human | Mini-Gs | 53 | β1 | Human | γ2 | Human | Cryo-EM | 7WU2 | - | 2.8 | AGRD1 | ADGRD1 | ADGRD | B2 (Adhesion) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | - | - | 2022-04-27 | 53739 | |
Gi/o | αi1 | Human | - | 61 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7SQO | - | 3.2 | OX2R | OX2 | Orexin | A (Rhodopsin) | Human | - | scFv16 | - |
methyl (2R,3S)-3-[(methanesulfonyl)amino]-2-({[(1s,4S)-4-phenylcyclohexyl]oxy}methyl)piperidine-1-carboxylate
pubchem
|
small-molecule | Agonist | orexin-A, orexin-B | peptide | Yin J, Kang Y, McGrath AP, Chapman K, Sjodt M, Kimura E, Okabe A, Koike T, Miyanohana Y, Shimizu Y, Rallabandi R, Lian P, Bai X, Flinspach M, De Brabander JK, Rosenbaum DM | 10.1038/S41467-022-30601-3 | 2022-05-25 | 53741 | |
Gq/11 | αq | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7WKD | - | 3.0 | TRFR | TRH1 | Thyrotropin-releasing hormone | A (Rhodopsin) | Human | - | scFv16 | - |
TRH
pubchem
|
peptide | Agonist | TRH | peptide | Xu Y, Cai H, You C, He X, Yuan Q, Jiang H, Cheng X, Jiang Y, Xu HE | 10.1038/S41422-022-00641-X | 2022-06-15 | 53749 | |
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 | deoxycholic acid, cholic acid, chenodeoxycholic acid, lithocholic 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 | 53739 | |
Gq/11 | αq | Human | - | 57 | β1 | Bovine | γ2 | Bovine | Cryo-EM | 7X1U | 7X1U_refined | 3.2 | TRFR | TRH1 | Thyrotropin-releasing hormone | A (Rhodopsin) | Human | - | scFv16 | - |
TRH
pubchem
|
peptide | Agonist | TRH | peptide | - | - | 2022-08-31 | 53749 | |
Gs | αs | Human | - | 58 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7VVO | 7VVO_refined | 4.1 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
Parathyroid hormone
|
peptide | Agonist | TIP39, PTHrP-(1-36), PTHrP, PTH | peptide | Kobayashi K, Kawakami K, Kusakizako T, Miyauchi H, Tomita A, Kobayashi K, Shihoya W, Yamashita K, Nishizawa T, Kato HE, Inoue A, Nureki O | 10.1016/J.MOLCEL.2022.07.003 | 2022-08-03 | 53739 | |
Gi/o | αo | Human | - | 63 | β1 | Rat | γ2 | Mouse | Cryo-EM | 7TS0 | 7TS0_refined | 2.8 | CRFR2 | CRF2 | Corticotropin-releasing factor | B1 (Secretin) | Human | - | scFv16 | - |
Urocortin
pubchem
|
peptide | Agonist | urocortin 1, corticotrophin-releasing hormone, urocortin 2, urocortin 3 | peptide | Zhao LH, Lin J, Ji SY, Zhou XE, Mao C, Shen DD, He X, Xiao P, Sun J, Melcher K, Zhang Y, Yu X, Xu HE | 10.1038/S41467-022-33851-3 | 2022-11-09 | 53747 | |
Gi/o | αi1 | Human | - | 63 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7YU5 | 7YU5_refined | 3.3 | LPAR1 | LPA1 | Lysophospholipid (LPA) | A (Rhodopsin) | Human | - | scFv16 | - |
[(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate
pubchem
|
small-molecule | Agonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O | 10.1038/S41467-022-33121-2 | 2022-10-05 | 53741 | |
Gi/o | αi1 | Human | - | 62 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8F7S | 8F7S_refined | 3.0 | OPRD | δ | Opioid | A (Rhodopsin) | Human | - | - | - |
DELTORPHIN II
chembl_ligand
pubchem
|
protein | Agonist | [Leu]enkephalin, β-endorphin, dynorphin A, [Met]enkephalin, endomorphin-1, α-neoendorphin, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13) | peptide | Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y, Roth BL, Xu HE | 10.1016/J.CELL.2022.12.026 | 2022-12-14 | 53741 | |
Gi/o | αo | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8FN1 | - | 2.9 | NTR1 | NTS1 | Neurotensin | A (Rhodopsin) | Rat | - | scFv16 | - |
neurotensin
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
|
peptide | Agonist | neurotensin, neuromedin N | peptide | Krumm BE, DiBerto JF, Olsen RHJ, Kang HJ, Slocum ST, Zhang S, Strachan RT, Huang XP, Slosky LM, Pinkerton AB, Barak LS, Caron MG, Kenakin T, Fay JF, Roth BL | 10.1021/ACS.BIOCHEM.3C00029 | 2023-03-29 | 53747 | |
Gs | αs | Human | fused Gs | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8I2G | - | 2.8 | FSHR | FSH | Glycoprotein hormone | A (Rhodopsin) | Human | - | Nanobody-35 | - |
Follitropin subunit beta
Glycoprotein alpha FSHR agonist 1 pubchem |
peptide peptide small-molecule |
Agonist | FSH | peptide | Duan J, Xu P, Zhang H, Luan X, Yang J, He X, Mao C, Shen DD, Ji Y, Cheng X, Jiang H, Jiang Y, Zhang S, Zhang Y, Xu HE | 10.1038/S41467-023-36170-3 | 2023-03-29 | 53739 | |
Gi/o | αo | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8JZZ | 8JZZ_refined | 3.3 | C5AR1 | C5a1 | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
C5a des-Arg
gtoplig
|
peptide | Agonist | ribosomal protein S19, C5a, C5a des-Arg, C3a | peptide | Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C | 10.1016/J.CELL.2023.09.020 | 2023-10-18 | 53747 | |
Gs | αs | Human | - | 56 | β1 | Human | γ2 | Human | Cryo-EM | 8WC8 | - | 2.9 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Human | - | scFv16 | - |
CHEMBL476516
chembl_ligand
pubchem
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, dopamine | small-molecule | Shang P, Rong N, Jiang JJ, Cheng J, Zhang MH, Kang D, Qi L, Guo L, Yang GM, Liu Q, Zhou Z, Li XB, Zhu KK, Meng QB, Han X, Yan W, Kong Y, Yang L, Wang X, Lei D, Feng X, Liu X, Yu X, Wang Y, Li Q, Shao ZH, Yang F, Sun JP | 10.1016/J.CELL.2023.10.014 | 2023-12-27 | 53739 | |
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 | 53741 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7CKY | - | 3.2 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
CHEMBL3697578
chembl_ligand
pubchem
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z | 10.1016/J.CELL.2021.01.028 | 2021-03-03 | 53739 | |
Gq/11 | αq | Human | Gq-Gs-Gi1 chimera | 55 | β1 | Rat | γ2 | Human | Cryo-EM | 7MBY | - | 2.4 | CCKAR | CCK1 | Cholecystokinin | A (Rhodopsin) | Human | - | - | - |
CHEMBL216166
chembl_ligand
pubchem
|
protein | Agonist | desulfated cholecystokinin-8, CCK-58, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8 | peptide | Mobbs JI, Belousoff MJ, Harikumar KG, Piper SJ, Xu X, Furness SGB, Venugopal H, Christopoulos A, Danev R, Wootten D, Thal DM, Miller LJ, Sexton PM | 10.1371/JOURNAL.PBIO.3001295 | 2021-05-26 | 53749 | |
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 | 53739 | |
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 | 53742 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7F58 | 7F58_refined | 3.1 | MC4R | MC4 | Melanocortin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
THIQ
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | β-MSH, α-MSH, agouti-related protein, γ-MSH, ACTH | peptide | Zhang H, Chen LN, Yang D, Mao C, Shen Q, Feng W, Shen DD, Dai A, Xie S, Zhou Y, Qin J, Sun JP, Scharf DH, Hou T, Zhou T, Wang MW, Zhang Y | 10.1038/S41422-021-00552-3 | 2021-11-03 | 53739 | |
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 | 53741 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7RKM | - | 3.5 | US28 | US28 | Unclassified | A (Rhodopsin) | strain AD169 | - | scFv16 | - |
Fractalkine
pubchem
|
peptide | Agonist | - | - | Tsutsumi N, Maeda S, Qu Q, Vogele M, Jude KM, Suomivuori CM, Panova O, Waghray D, Kato HE, Velasco A, Dror RO, Skiniotis G, Kobilka BK, Garcia KC | 10.1126/SCIADV.ABL5442 | 2022-01-26 | 53741 | |
Gi/o | αo | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7EJK | - | 3.4 | ADA2A | α2A | Adrenoceptors | A (Rhodopsin) | Human | - | scFv16 | - |
oxymetazoline
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | (-)-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 | 53747 | |
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 | - | - | - | - | 2022-04-20 | 53741 | |
Gq/11 | αq | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7F6H | 7F6H_refined | 2.9 | BKRB2 | B2 | Bradykinin | A (Rhodopsin) | Human | - | - | - |
bradykinin
pubchem
gtoplig
chembl_ligand
drugbank
gtoplig
|
peptide | Agonist | [des-Arg10]kallidin, Lys-[Hyp3]-bradykinin, kallidin, [des-Arg9]bradykinin, [Hyp3]bradykinin, T-kinin, bradykinin | peptide | Shen J, Zhang D, Fu Y, Chen A, Yang X, Zhang H | 10.1038/S41467-022-28399-1 | 2022-01-05 | 53749 | |
Gi/o | αi2 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7WV9 | - | 3.4 | CNR1 | CB1 | Cannabinoid | A (Rhodopsin) | Human | - | scFv16 | - |
CP55940
pubchem
gtoplig
chembl_ligand
gtoplig
6-methyl-3-[(1S)-2-nitro-1-thiophen-2-yl-ethyl]-2-phenyl-1H-indole pubchem |
small-molecule small-molecule |
Agonist PAM |
2-arachidonoylglycerol, anandamide | small-molecule | Yang X, Wang X, Xu Z, Wu C, Zhou Y, Wang Y, Lin G, Li K, Wu M, Xia A, Liu J, Cheng L, Zou J, Yan W, Shao Z, Yang S | 10.1038/S41589-022-01038-Y | 2022-06-15 | 53742 | |
Gi/o | αi1 | Human | - | 64 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8EFB | 8EFB_refined | 3.2 | OPRM | μ | Opioid | A (Rhodopsin) | Human | - | scFv16 | - |
OLICERIDINE
chembl_ligand
pubchem
|
small-molecule | Agonist | [Leu]enkephalin, β-endorphin, dynorphin A, [Met]enkephalin, endomorphin-1, endomorphin-2, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13) | peptide | Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, Rao Q, Yang J, Liu J, Zhou Q, Wang X, Liu M, Liu W, Jiang X, Yang D, Jiang H, Shen J, Melcher K, Chen H, Jiang Y, Cheng X, Wang MW, Xie X, Xu HE | 10.1016/J.CELL.2022.09.041 | 2022-11-09 | 53741 | |
Gi/o | αi1 | Human | - | 56 | β1 | Human | γ2 | Human | Cryo-EM | 8ID9 | 8ID9_refined | 3.0 | FFAR4 | FFA4 | Free fatty acid | A (Rhodopsin) | Human | - | scFv16 | - |
EPA
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | myristic acid, linoleic acid, α-linolenic acid, oleic acid | small-molecule | Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP | 10.1126/SCIENCE.ADD6220 | 2023-03-15 | 53741 | |
Gq/11 | αq | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8IBV | 8IBV_refined | 3.2 | MTLR | motilin | Motilin | A (Rhodopsin) | Human | BRIL | scFv16 | - |
motilin
pubchem
gtoplig
chembl_ligand
gtoplig
pubchem
pubchem
|
peptide | Agonist | motilin | peptide | You C, Zhang Y, Xu Y, Xu P, Li Z, Li H, Huang S, Chen Z, Li J, Xu HE, Jiang Y | 10.1126/SCIADV.ADE9020 | 2023-04-12 | 53749 | |
Gs | αs | Human | - | 57 | β1 | Human | γ2 | Human | Cryo-EM | 7XY6 | - | 3.0 | AA2BR | A2B | Adenosine | A (Rhodopsin) | Human | BRIL | - | - |
BAY 60-6583
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | adenosine | small-molecule | Chen Y, Zhang J, Weng Y, Xu Y, Lu W, Liu W, Liu M, Hua T, Song G | 10.1126/SCIADV.ADD3709 | 2023-05-03 | 53739 | |
Gq/11 | αq | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8H4L | - | 3.1 | FFAR4 | FFA4 | Free fatty acid | A (Rhodopsin) | Human | - | Nanobody-35 | - |
docosahexaenoic acid
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
pubchem
|
small-molecule | Agonist | myristic acid, linoleic acid, α-linolenic acid, oleic acid | small-molecule | Yin H, Inoue A, Ma Z, Zhu X, Xia R, Xu Z, Wang N, Duan Y, Zhang A, Guo C, He Y | 10.1038/S41422-023-00835-X | 2023-06-21 | 53749 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8GDA | - | 3.3 | PE2R4 | EP4 | Prostanoid | A (Rhodopsin) | Human | - | - | - |
(2S,5R)-5-[(1E,3S)-4,4-difluoro-3-hydroxy-4-phenylbut-1-en-1-yl]-1-[6-(1H-tetrazol-5-yl)hexyl]pyrrolidin-2-ol
pubchem
|
small-molecule | Agonist | thromboxane A2, PGF2α, PGI2, PGD2, PGE1, PGE2 | small-molecule | Huang SM, Xiong MY, Liu L, Mu J, Wang MW, Jia YL, Cai K, Tie L, Zhang C, Cao S, Wen X, Wang JL, Guo SC, Li Y, Qu CX, He QT, Cai BY, Xue C, Gan S, Xie Y, Cong X, Yang Z, Kong W, Li S, Li Z, Xiao P, Yang F, Yu X, Guan YF, Zhang X, Liu Z, Yang BX, Du Y, Sun JP | 10.1073/PNAS.2216329120 | 2024-01-10 | 53739 | |
Gi/o | αo | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8I97 | 8I97_refined | 3.2 | C3AR | C3a | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | C5a, C3a | peptide | Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C | 10.1016/J.CELL.2023.09.020 | 2023-10-18 | 53747 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8IZB | - | 3.1 | GP174 | GPR174 | A orphans | A (Rhodopsin) | Human | - | Nanobody-35 | - |
L-serine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
LYSOPHOSPHATIDIC ACID chembl_ligand pubchem |
small-molecule small-molecule |
Agonist | lysophosphatidylserine | small-molecule | Liu G, Li X, Wang Y, Zhang X, Gong W | 10.1371/JOURNAL.PBIO.3002387 | 2023-11-01 | 53739 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8K2X | 8K2X_refined | 3.2 | CXCR3 | CXCR3 | Chemokine | A (Rhodopsin) | Human | BRIL | scFv16 | - |
C-X-C motif chemokine 10
|
small-molecule | Agonist | CCL19, CXCL11, CCL13, CXCL9, CXCL10, CCL7, CCL5, CCL11, CXCL12α, CCL20 | peptide | Jiao H, Pang B, Chiang YC, Chen Q, Pan Q, Ren R, Hu H | 10.1038/S41421-023-00617-0 | 2023-11-29 | 53741 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8WC4 | - | 3.1 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Mouse | - | scFv16 | - |
CHEMBL476516
chembl_ligand
pubchem
|
small-molecule | Agonist | β-phenylethylamine, 3-iodothyronamine, tyramine | small-molecule | Shang P, Rong N, Jiang JJ, Cheng J, Zhang MH, Kang D, Qi L, Guo L, Yang GM, Liu Q, Zhou Z, Li XB, Zhu KK, Meng QB, Han X, Yan W, Kong Y, Yang L, Wang X, Lei D, Feng X, Liu X, Yu X, Wang Y, Li Q, Shao ZH, Yang F, Sun JP | 10.1016/J.CELL.2023.10.014 | 2023-12-27 | 53739 | |
Gi/o | αi1 | Human | - | 100 | β1 | Rat | γ2 | Bovine | Cryo-EM | 6CMO | - | 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 | 53741 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 6N4B | 6N4B_refined | 3.0 | CNR1 | CB1 | Cannabinoid | A (Rhodopsin) | Human | - | scFv16 | - |
MDMB-Fubinaca
pubchem
gtoplig
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | Krishna Kumar K, Shalev-Benami M, Robertson MJ, Hu H, Banister SD, Hollingsworth SA, Latorraca NR, Kato HE, Hilger D, Maeda S, Weis WI, Farrens DL, Dror RO, Malhotra SV, Kobilka BK, Skiniotis G | 10.1016/J.CELL.2018.11.040 | 2019-01-30 | 53741 | |
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 | 53741 | |
Gq/11 | αq | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7DFL | - | 3.3 | HRH1 | H1 | Histamine | A (Rhodopsin) | Human | - | scFv16 | - |
histamine
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
gtoplig
|
small-molecule | Agonist | histamine | small-molecule | Xia R, Wang N, Xu Z, Lu Y, Song J, Zhang A, Guo C, He Y | 10.1038/S41467-021-22427-2 | 2021-03-31 | 53749 | |
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 | 53743 | |
Gq/11 | αq | Human | Engineered G alpha | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7F9Z | 7F9Z_refined | 3.2 | GHSR | ghrelin | Ghrelin | A (Rhodopsin) | Human | - |
Nanobody-35 scFv16 |
- |
GHRP-6
pubchem
gtoplig
|
peptide | Agonist | [des-Gln14]ghrelin, ghrelin | peptide | Wang Y, Guo S, Zhuang Y, Yun Y, Xu P, He X, Guo J, Yin W, Xu HE, Xie X, Jiang Y | 10.1038/S41467-021-25364-2 | 2021-08-18 | 53749 | |
Gs | αs | Bovine | - | 91 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7FII | - | 4.3 | LSHR | LH | Glycoprotein hormone | A (Rhodopsin) | Human | - | - | - |
Glycoprotein alpha
gtoplig
Choriogonadotropin beta gtoplig |
protein protein |
Agonist | hCG, LH | peptide | Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE | 10.1038/S41586-021-03924-2 | 2021-09-29 | 53756 | |
Gi/o | αi1 | Human | - | 62 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7T6U | - | 2.9 | FPR2 | FPR2/ALX | Formylpeptide | A (Rhodopsin) | Human | - | - | - |
synthetic peptide
|
peptide | Agonist | humanin, aspirin-triggered resolvin D1, LXA4, resolvin D1, serum amyloid A, PrP106-126, 15-deoxy-LXA4, aspirin triggered lipoxin A4, LL-37, LTC4, annexin I, fMet-Leu-Phe, LTD4 | peptide | 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 | 53741 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7TYY | - | 3.0 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - | Nanobody-35 | - |
calcitonin (salmon synthetic)
pubchem
|
small-molecule | Agonist | adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP | peptide | Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM | 10.1126/SCIENCE.ABM9609 | 2022-03-23 | 53739 | |
G12/13 | α13 | Human | Gi2-mini-G13 chimera | 56 | β1 | Human | γ2 | Human | Cryo-EM | 7SF7 | - | 2.9 | AGRL3 | ADGRL3 | ADGRL | B2 (Adhesion) | Human | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Barros-Alvarez X, Nwokonko RM, Vizurraga A, Matzov D, He F, Papasergi-Scott MM, Robertson MJ, Panova O, Yardeni EH, Seven AB, Kwarcinski FE, Su H, Peroto MC, Meyerowitz JG, Shalev-Benami M, Tall GG, Skiniotis G | 10.1038/S41586-022-04575-7 | 2022-04-27 | 53754 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7V68 | - | 3.4 | ACM4 | M4 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | scFv16 | - |
iperoxo
pubchem
gtoplig
chembl_ligand
LY2119620 pubchem gtoplig chembl_ligand |
small-molecule small-molecule |
Agonist PAM |
acetylcholine | small-molecule | Wang J, Wu M, Chen Z, Wu L, Wang T, Cao D, Wang H, Liu S, Xu Y, Li F, Liu J, Chen N, Zhao S, Cheng J, Wang S, Hua T | 10.1038/S41467-022-30595-Y | 2022-05-11 | 53741 | |
Gi/o | αo | Human | Mini-Go | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8E9X | - | 2.7 | ACM4 | M4 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | scFv16 | - |
CHEMBL73538
chembl_ligand
pubchem
|
small-molecule | Agonist | acetylcholine | small-molecule | Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL | 10.1038/S41586-022-05489-0 | 2022-11-30 | 53747 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7Y65 | - | 3.2 | C5AR1 | C5a1 | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
C5a
|
peptide | Agonist | ribosomal protein S19, C5a, C5a des-Arg, C3a | peptide | Feng Y, Zhao C, Deng Y, Wang H, Ma L, Liu S, Tian X, Wang B, Bin Y, Chen P, Yan W, Fu P, Shao Z | 10.1038/S41422-023-00779-2 | 2023-03-01 | 53741 | |
Gq/11 | αq | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8HCX | 8HCX_refined | 3.5 | EDNRB | ETB | Endothelin | A (Rhodopsin) | Human | - | scFv16 | - |
ENDOTHELIN
chembl_ligand
pubchem
|
protein | Agonist | endothelin-1, endothelin-2, endothelin-3 | peptide | - | - | 2023-03-22 | 53749 | |
Gq/11 | αq | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8EIT | - | 2.8 | FFAR1 | FFA1 | Free fatty acid | A (Rhodopsin) | Human | - | scFv16 | - |
docosahexaenoic acid
pubchem
gtoplig
chembl_ligand
drug_central
drugbank
pubchem
|
small-molecule | Agonist | myristic acid, oleic acid, α-linolenic acid, docosahexaenoic acid | small-molecule | Kumari P, Inoue A, Chapman K, Lian P, Rosenbaum DM | 10.1073/PNAS.2219569120 | 2023-05-24 | 53749 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 7TRK | - | 2.8 | ACM4 | M4 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | scFv16 | - |
iperoxo
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | acetylcholine | small-molecule | - | - | 2023-05-17 | 53741 | |
Gs | αs | Human | - | 57 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7Y36 | - | 2.8 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
teriparatide
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
pubchem
pubchem
pubchem
pubchem
pubchem
|
peptide | Agonist | TIP39, PTHrP-(1-36), PTHrP, PTH | peptide | - | - | 2023-07-05 | 53739 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 8G05 | - | 3.0 | GPR84 | GPR84 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
6-Octylimino-1,3-diazinane-2,4-dione
pubchem
|
lipid | Agonist | - | - | Zhang X, Wang Y, Supekar S, Cao X, Zhou J, Dang J, Chen S, Jenkins L, Marsango S, Li X, Liu G, Milligan G, Feng M, Fan H, Gong W, Zhang C | 10.1038/S41467-023-41201-0 | 2023-11-01 | 53741 | |
Gi/o | αi1 | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8HQE | 8HQE_refined | 3.0 | GP132 | GPR132 | A orphans | A (Rhodopsin) | Human | BRIL | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | 9-hydroxyoctadecadienoic acid | small-molecule | Wang JL, Dou XD, Cheng J, Gao MX, Xu GF, Ding W, Ding JH, Li Y, Wang SH, Ji ZW, Zhao XY, Huo TY, Zhang CF, Liu YM, Sha XY, Gao JR, Zhang WH, Hao Y, Zhang C, Sun JP, Jiao N, Yu X | 10.1038/S42255-023-00899-4 | 2023-10-11 | 53741 | |
Gs | αs | Human | Gi1-Gs chimera | 60 | β1 | Human | γ2 | Bovine | Cryo-EM | 8IOC | - | 2.9 | MC3R | MC3 | Melanocortin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
γ-MSH
pubchem
gtoplig
pubchem
|
peptide | Agonist | β-MSH, α-MSH, agouti-related protein, γ-MSH, ACTH | peptide | Chen VB, Arendall WB 3rd, Headd JJ, Keedy DA, Immormino RM, Kapral GJ, Murray LW, Richardson JS, Richardson DC | 10.1107/S0907444909042073 | 2023-09-20 | 53739 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8JLR | - | 3.0 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Human | BRIL | scFv16 | - |
(1~{S},3~{R})-3-(1-adamantyl)-1-(aminomethyl)-3,4-dihydro-1~{H}-isochromene-5,6-diol
pubchem
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, dopamine | small-molecule | Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z | 10.1038/S41586-023-06804-Z | 2023-11-15 | 53739 | |
Gi/o | αi1 | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8U1U | - | 3.1 | CCR8 | CCR8 | Chemokine | A (Rhodopsin) | Human | - | scFv16 | - |
CCL1
|
protein | Agonist | CCL1 | peptide | - | - | 2023-12-20 | 53741 | |
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 | 53851 | |
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 | 53741 | |
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 | 53741 | |
Gs | αs | Bovine | - | 91 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7FIG | - | 3.9 | LSHR | LH | Glycoprotein hormone | A (Rhodopsin) | Human | - | Nanobody-35 | - |
Glycoprotein alpha
gtoplig
Choriogonadotropin beta gtoplig |
protein protein |
Agonist | hCG, LH | peptide | Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE | 10.1038/S41586-021-03924-2 | 2021-09-29 | 53756 | |
Gs | αs | Human | - | 54 | β1 | Human | γ2 | Human | Cryo-EM | 7EPT | - | 3.0 | AGRD1 | ADGRD1 | ADGRD | B2 (Adhesion) | Human | - | Nanobody-35 | - | - | - | - | - | - | Ping YQ, Xiao P, Yang F, Zhao RJ, Guo SC, Yan X, Wu X, Zhang C, Lu Y, Zhao F, Zhou F, Xi YT, Yin W, Liu FZ, He DF, Zhang DL, Zhu ZL, Jiang Y, Du L, Feng SQ, Schoneberg T, Liebscher I, Xu HE, Sun JP | 10.1038/S41586-022-04619-Y | 2022-05-11 | 53739 | |
Gi/o | αi1 | Human | - | 64 | β1 | Rat | γ2 | Bovine | Cryo-EM | 7WIG | 7WIG_refined | 2.7 | SSR2 | SST2 | Somatostatin | A (Rhodopsin) | Human | - | scFv16 | - |
~{N}-[(2~{R})-1-[[(1~{R},3~{S})-3-(aminomethyl)cyclohexyl]methylamino]-3-(1~{H}-indol-3-yl)-1-oxidanylidene-propan-2-yl]spiro[indene-1,4'-piperidine]-1'-carboxamide
pubchem
|
small-molecule | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | Chen LN, Wang WW, Dong YJ, Shen DD, Guo J, Yu X, Qin J, Ji SY, Zhang H, Shen Q, He Q, Yang B, Zhang Y, Li Q, Mao C | 10.1038/S41422-022-00669-Z | 2022-06-01 | 53741 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7XT8 | - | 3.1 | 5HT4R | 5-HT4 | 5-Hydroxytryptamine | A (Rhodopsin) | Human | BRIL | Nanobody-35 | - |
5-hydroxytryptamine
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE | 10.1016/J.MOLCEL.2022.05.031 | 2022-07-27 | 53739 | |
Gq/11 | αq | Human | Gi2-mini-Gq chimera | 57 | β1 | Human | γ2 | Human | Cryo-EM | 8DPG | - | 3.6 | 5HT2C | 5-HT2C | 5-Hydroxytryptamine | A (Rhodopsin) | Human | - | scFv16 | - |
psilocin
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | Gumpper RH, Fay JF, Roth BL | 10.1016/J.CELREP.2022.111211 | 2022-08-24 | 53749 | |
Gi/o | αi1 | Human | - | 38 | β1 | Human | γ2 | Human | Cryo-EM | 7WU9 | 7WU9_refined | 3.4 | PE2R3 | EP3 | Prostanoid | A (Rhodopsin) | Human | - | scFv16 | - | - | - | - | thromboxane A2, PGF2α, PGI2, PGD2, PGE1, PGE2 | small-molecule | Suno R, Sugita Y, Morimoto K, Takazaki H, Tsujimoto H, Hirose M, Suno-Ikeda C, Nomura N, Hino T, Inoue A, Iwasaki K, Kato T, Iwata S, Kobayashi T | 10.1016/J.CELREP.2022.111323 | 2022-08-17 | 53741 | |
Gs | αs | Human | Mini-Gs | 56 | β1 | Human | γ2 | Human | Cryo-EM | 7T9I | - | 2.9 | TSHR | TSH | Glycoprotein hormone | A (Rhodopsin) | Human | - | Nanobody-35 | - |
Thyrotropin subunit beta
Glycoprotein hormones alpha chain |
protein protein |
Agonist | TSH | peptide | Faust B, Billesbolle CB, Suomivuori CM, Singh I, Zhang K, Hoppe N, Pinto AFM, Diedrich JK, Muftuoglu Y, Szkudlinski MW, Saghatelian A, Dror RO, Cheng Y, Manglik A | 10.1038/S41586-022-05159-1 | 2022-08-03 | 53739 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 8HOC | - | 3.0 | HRH4 | H4 | Histamine | A (Rhodopsin) | Human | - | scFv16 | - |
imetit
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | histamine, CCL16 | small-molecule | - | - | 2023-12-20 | 53741 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 8IJA | - | 2.7 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | - | scFv16 | - |
nicotinic acid
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
gtoplig
pubchem
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | Pan X, Ye F, Ning P, Zhang Z, Li X, Zhang B, Wang Q, Chen G, Gao W, Qiu C, Wu Z, Li J, Zhu L, Xia J, Gong K, Du Y | 10.1038/S41421-023-00610-7 | 2024-01-03 | 53741 | |
Gs | αs | Human | - | 59 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8JIU | 8JIU_refined | 2.8 | GLR | glucagon | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
SAR425899
|
peptide | Agonist | glucagon | peptide | Li Y, Zhou Q, Dai A, Zhao F, Chang R, Ying T, Wu B, Yang D, Wang MW, Cong Z | 10.1073/PNAS.2303696120 | 2023-09-13 | 53739 | |
Gi/o | αi2 | Human | - | 0 | β1 | Human | γ2 | Human | Cryo-EM | 8W8A | - | 2.8 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
CHEMBL3684869
chembl_ligand
pubchem
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, dopamine | small-molecule | Liu H, Zheng Y, Wang Y, Wang Y, He X, Xu P, Huang S, Yuan Q, Zhang X, Wang L, Jiang K, Chen H, Li Z, Liu W, Wang S, Xu HE, Xu F | 10.1038/S41586-023-06775-1 | 2023-11-22 | 53742 | |
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 | 53747 | |
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 | 53741 | |
Gs | αs | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 7CKW | 7CKW_refined | 3.2 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
fenoldopam
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
gtoplig
chembl_ligand
pubchem
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z | 10.1016/J.CELL.2021.01.028 | 2021-03-03 | 53739 | |
Gi/o | αi1 | Human | - | 61 | β1 | Human | γ2 | Human | Cryo-EM | 7F1Q | - | 2.9 | CCR5 | CCR5 | Chemokine | A (Rhodopsin) | Human | - | - | - |
CCL3
gtoplig
|
peptide | Agonist | CCL14, CCL8, CCL13, CCL4, CCL7, CCL2, CCL5, CCL11, CCL3, CCL16 | peptide | - | - | 2021-07-14 | 53741 | |
Gs | αs | Human | - | 55 | β1 | Human | γ2 | Human | Cryo-EM | 7RMH | 7RMH_refined | 3.1 | NK1R | NK1 | Tachykinin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
substance P
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
|
peptide | Agonist | neuropeptide-γ, neurokinin A, neuropeptide K, neurokinin B, hemokinin 1, substance P | peptide | Harris JA, Faust B, Gondin AB, Damgen MA, Suomivuori CM, Veldhuis NA, Cheng Y, Dror RO, Thal DM, Manglik A | 10.1038/S41589-021-00890-8 | 2021-11-03 | 53739 | |
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 | 53741 | |
Gi/o | αo | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7EJA | - | 3.6 | ADA2A | α2A | Adrenoceptors | A (Rhodopsin) | Human | - | scFv16 | - |
dexmedetomidine
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
|
small-molecule | Agonist | (-)-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 | 53747 | |
Gi/o | αi2 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7WVY | 7WVY_refined | 3.0 | FPR2 | FPR2/ALX | Formylpeptide | A (Rhodopsin) | Human | BRIL | - | - |
Amyloid beta-Peptide (1-42)
pubchem
|
peptide | Agonist | humanin, aspirin-triggered resolvin D1, LXA4, resolvin D1, serum amyloid A, PrP106-126, 15-deoxy-LXA4, aspirin triggered lipoxin A4, LL-37, LTC4, annexin I, fMet-Leu-Phe, LTD4 | peptide | Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B | 10.1038/S41467-022-29361-X | 2022-04-13 | 53742 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 7V69 | - | 3.4 | ACM4 | M4 | Acetylcholine (muscarinic) | A (Rhodopsin) | Human | - | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | acetylcholine | small-molecule | Wang J, Wu M, Chen Z, Wu L, Wang T, Cao D, Wang H, Liu S, Xu Y, Li F, Liu J, Chen N, Zhao S, Cheng J, Wang S, Hua T | 10.1038/S41467-022-30595-Y | 2022-05-11 | 53741 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7X2C | 7X2C_refined | 3.2 | DRD1 | D1 | Dopamine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
fenoldopam
pubchem
gtoplig
chembl_ligand
drugbank
drug_central
pubchem
gtoplig
chembl_ligand
pubchem
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | Teng X, Chen S, Nie Y, Xiao P, Yu X, Shao Z, Zheng S | 10.1038/S41467-022-30929-W | 2022-06-29 | 53739 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8E3X | 8E3X_refined | 2.3 | PACR | PAC1 | VIP and PACAP | B1 (Secretin) | Human | - | Nanobody-35 | - |
[Ac-His1]PACAP-27
gtoplig
chembl_ligand
pubchem
|
peptide | Agonist | VIP, PHI, PHM, PHV, PACAP-27, PACAP-38 | peptide | Piper SJ, Deganutti G, Lu J, Zhao P, Liang YL, Lu Y, Fletcher MM, Hossain MA, Christopoulos A, Reynolds CA, Danev R, Sexton PM, Wootten D | 10.1038/S41467-022-34629-3 | 2022-11-23 | 53739 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 7Y66 | - | 2.9 | C5AR1 | C5a1 | Complement peptide | A (Rhodopsin) | Human | - | scFv16 | - |
BM213
|
peptide | Agonist | ribosomal protein S19, C5a, C5a des-Arg, C3a | peptide | Feng Y, Zhao C, Deng Y, Wang H, Ma L, Liu S, Tian X, Wang B, Bin Y, Chen P, Yan W, Fu P, Shao Z | 10.1038/S41422-023-00779-2 | 2023-03-01 | 53741 | |
Gi/o | αi1 | Human | - | 62 | β1 | Human | γ2 | Human | Cryo-EM | 8HS3 | - | 3.1 | GPR20 | GPR20 | A orphans | A (Rhodopsin) | Human | BRIL | scFv16 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Lin X, Jiang S, Wu Y, Wei X, Han GW, Wu L, Liu J, Chen B, Zhang Z, Zhao S, Cherezov V, Xu F | 10.1038/S41421-023-00520-8 | 2023-03-08 | 53741 | |
Gs | αs | Human | - | 54 | β1 | Human | γ2 | Human | Cryo-EM | 8FU6 | 8FU6_refined | 2.9 | GLR | glucagon | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
Glucagon derivative ZP3780
|
peptide | Agonist | glucagon | peptide | Krishna Kumar K, O'Brien ES, Habrian CH, Latorraca NR, Wang H, Tuneew I, Montabana E, Marqusee S, Hilger D, Isacoff EY, Mathiesen JM, Kobilka BK | 10.1016/J.CELL.2023.02.028 | 2023-04-12 | 53739 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8FLQ | - | 2.6 | PTH1R | PTH1 | Parathyroid hormone | B1 (Secretin) | Human | - | Nanobody-35 | - |
Parathyroid hormone
|
peptide | Agonist | TIP39, PTHrP-(1-36), PTHrP, PTH | peptide | Cary BP, Gerrard EJ, Belousoff MJ, Fletcher MM, Jiang Y, Russell IC, Piper SJ, Wootten D, Sexton PM | 10.1016/J.STR.2023.04.002 | 2023-04-26 | 53739 | |
Gq/11 | αq | Human | Mini-Gq | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8H4K | - | 3.1 | FFAR4 | FFA4 | Free fatty acid | A (Rhodopsin) | Human | - | Nanobody-35 | - |
GW9508
pubchem
gtoplig
chembl_ligand
|
small-molecule | Agonist | myristic acid, linoleic acid, α-linolenic acid, oleic acid | small-molecule | Yin H, Inoue A, Ma Z, Zhu X, Xia R, Xu Z, Wang N, Duan Y, Zhang A, Guo C, He Y | 10.1038/S41422-023-00835-X | 2023-06-21 | 53749 | |
Gi/o | αi1 | Human | - | 56 | β1 | Human | γ2 | Human | Cryo-EM | 8GCM | - | 3.5 | PE2R4 | EP4 | Prostanoid | A (Rhodopsin) | Human | - | scFv16 | - |
(5S)-5-[(3R)-4,4-difluoro-3-hydroxy-4-phenylbutyl]-1-[6-(1H-tetrazol-5-yl)hexyl]pyrrolidin-2-one
pubchem
|
lipid | Agonist | thromboxane A2, PGF2α, PGI2, PGD2, PGE1, PGE2 | small-molecule | Huang SM, Xiong MY, Liu L, Mu J, Wang MW, Jia YL, Cai K, Tie L, Zhang C, Cao S, Wen X, Wang JL, Guo SC, Li Y, Qu CX, He QT, Cai BY, Xue C, Gan S, Xie Y, Cong X, Yang Z, Kong W, Li S, Li Z, Xiao P, Yang F, Yu X, Guan YF, Zhang X, Liu Z, Yang BX, Du Y, Sun JP | 10.1073/PNAS.2216329120 | 2024-01-03 | 53741 | |
Gi/o | αo | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8HQC | - | 3.9 | C5AR1 | C5a1 | Complement peptide | A (Rhodopsin) | Mouse | - | - | fragment |
C5a
gtoplig
|
peptide | Agonist | - | - | None | HTTPS://DOI.ORG/10.1016/J.CELL.2023.09.020 | 2023-10-18 | 53747 | |
Gi/o | αi1 | Human | - | 64 | β1 | Human | γ2 | Human | Cryo-EM | 8J6R | - | 2.8 | HCAR2 | HCA2 | Hydroxycarboxylic acid | A (Rhodopsin) | Human | - | scFv16 | - |
MK 6892
pubchem
gtoplig
chembl_ligand
pubchem
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | Mao C, Gao M, Zang SK, Zhu Y, Shen DD, Chen LN, Yang L, Wang Z, Zhang H, Wang WW, Shen Q, Lu Y, Ma X, Zhang Y | 10.1038/S41467-023-43537-Z | 2023-12-06 | 53741 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8W87 | - | 2.8 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Human | - | Nanobody-35 | - |
METHAMPHETAMINE
chembl_ligand
pubchem
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, dopamine | small-molecule | Liu H, Zheng Y, Wang Y, Wang Y, He X, Xu P, Huang S, Yuan Q, Zhang X, Wang L, Jiang K, Chen H, Li Z, Liu W, Wang S, Xu HE, Xu F | 10.1038/S41586-023-06775-1 | 2023-11-22 | 53739 | |
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 | 53739 | |
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-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | - | - | 2021-08-04 | 53739 | |
Gq/11 | αq | Human | Gs-Gq chimera | 52 | β1 | Human | γ2 | Human | Cryo-EM | 7RMG | - | 3.0 | NK1R | NK1 | Tachykinin | A (Rhodopsin) | Human | - | Nanobody-35 | - |
substance P
pubchem
gtoplig
chembl_ligand
gtoplig
gtoplig
|
peptide | Agonist | neuropeptide-γ, neurokinin A, neuropeptide K, neurokinin B, hemokinin 1, substance P | peptide | Harris JA, Faust B, Gondin AB, Damgen MA, Suomivuori CM, Veldhuis NA, Cheng Y, Dror RO, Thal DM, Manglik A | 10.1038/S41589-021-00890-8 | 2021-11-03 | 53749 | |
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 | 53739 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 7TYO | - | 2.7 | CALCR | CT | Calcitonin | B1 (Secretin) | Human | - | Nanobody-35 | - |
Calcitonin human
pubchem
|
peptide | Agonist | adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP | peptide | Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM | 10.1126/SCIENCE.ABM9609 | 2022-03-23 | 53739 | |
Gq/11 | αq | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 7W56 | - | 2.9 | NMUR1 | NMU1 | Neuromedin U | A (Rhodopsin) | Human | - | scFv16 | - |
Neuromedin-S
|
peptide | Agonist | neuromedin U-23, neuromedin S-36, neuromedin S-33, neuromedin U-25 | peptide | You C, Zhang Y, Xu P, Huang S, Yin W, Eric Xu H, Jiang Y | 10.1038/S41467-022-29683-W | 2022-04-20 | 53749 | |
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 | desulfated cholecystokinin-8, CCK-58, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8 | peptide | Ding Y, Zhang H, Liao YY, Chen LN, Ji SY, Qin J, Mao C, Shen DD, Lin L, Wang H, Zhang Y, Li XM | 10.1038/S41421-022-00420-3 | 2022-07-20 | 53739 | |
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-28, cortistatin-14, CST-17, SRIF-14 | peptide | Bo Q, Yang F, Li Y, Meng X, Zhang H, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C | 10.1038/S41421-022-00405-2 | 2022-08-31 | 53741 | |
Gs | αs | Human | Mini-Gs | 56 | β1 | Human | γ2 | Human | Cryo-EM | 7UTZ | - | 2.4 | TSHR | TSH | Glycoprotein hormone | A (Rhodopsin) | Human | - | Nanobody-35 | - |
Thyrotropin subunit beta
Glycoprotein hormones alpha chain analog TR1402 |
protein protein |
Agonist | TSH | peptide | Faust B, Billesbolle CB, Suomivuori CM, Singh I, Zhang K, Hoppe N, Pinto AFM, Diedrich JK, Muftuoglu Y, Szkudlinski MW, Saghatelian A, Dror RO, Cheng Y, Manglik A | 10.1038/S41586-022-05159-1 | 2022-08-03 | 53739 | |
Gi/o | αi1 | Human | - | 60 | β1 | Human | γ2 | Human | Cryo-EM | 8HQN | 8HQN_refined | 3.0 | GP132 | GPR132 | A orphans | A (Rhodopsin) | Human | BRIL | scFv16 | - |
9-hydroxyoctadecadienoic acid
pubchem
gtoplig
chembl_ligand
drugbank
|
small-molecule | Agonist | 9-hydroxyoctadecadienoic acid | small-molecule | Wang JL, Dou XD, Cheng J, Gao MX, Xu GF, Ding W, Ding JH, Li Y, Wang SH, Ji ZW, Zhao XY, Huo TY, Zhang CF, Liu YM, Sha XY, Gao JR, Zhang WH, Hao Y, Zhang C, Sun JP, Jiao N, Yu X | 10.1038/S42255-023-00899-4 | 2023-10-11 | 53741 | |
Gs | αs | Bovine | - | 59 | β1 | Rat | γ2 | Bovine | Cryo-EM | 8ITL | - | 3.2 | GIPR | GIP | Glucagon | B1 (Secretin) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | gastric inhibitory polypeptide | peptide | Zhao F, Hang K, Zhou Q, Shao L, Li H, Li W, Lin S, Dai A, Cai X, Liu Y, Xu Y, Feng W, Yang D, Wang MW | 10.1073/PNAS.2306145120 | 2023-10-18 | 53756 | |
Gs | αs | Human | - | 59 | β1 | Human | γ2 | Human | Cryo-EM | 8JLK | - | 3.2 | TAAR1 | TA1 | Trace amine | A (Rhodopsin) | Mouse | - | scFv16 | - |
ulotaront
pubchem
gtoplig
drugbank
chembl_ligand
|
small-molecule | Agonist | β-phenylethylamine, 3-iodothyronamine, tyramine | small-molecule | Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z | 10.1038/S41586-023-06804-Z | 2023-11-15 | 53739 | |
Gs | αs | Human | - | 58 | β1 | Human | γ2 | Human | Cryo-EM | 8KH4 | 8KH4_refined | 3.1 | GP161 | GPR161 | A orphans | A (Rhodopsin) | Human | - | Nanobody-35 | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | Nie Y, Qiu Z, Chen S, Chen Z, Song X, Ma Y, Huang N, Cyster JG, Zheng S | 10.1038/S41467-023-41654-3 | 2023-10-11 | 53739 | |
Gi/o | αi1 | Human | - | 63 | β1 | Human | γ2 | Human | Cryo-EM | 8WRB | - | 2.9 | GPR34 | GPR34 | A orphans | A (Rhodopsin) | Human | - | scFv16 | - |
LYSOPHOSPHATIDIC ACID
chembl_ligand
pubchem
|
small-molecule | Agonist | lysophosphatidylserine | small-molecule | Liu G, Li X, Wang Y, Zhang X, Gong W | 10.1371/JOURNAL.PBIO.3002387 | 2023-11-08 | 53741 | |
Gs | αs2 | Human | - | 96 | - | - | - | - | X-ray | 6AU6 | - | 1.7 | - | - | - | - | - | - | - | - | - | - | - | - | - | Hu Q, Shokat KM | 29628140 | 2018-05-09 | 53739 | |
Gs | αs2 | Human | - | 97 | β1 | Human | γ2 | Human | X-ray | 6EG8 | - | 2.8 | - | - | - | - | - | - | - | - | - | - | - | - | - | Liu X, Xu X, Hilger D, Aschauer P, Tiemann JKS, Du Y, Liu H, Hirata K, Sun X, Guixa-Gonzalez R, Mathiesen JM, Hildebrand PW, Kobilka BK | 31080070 | 2019-06-05 | 53739 | |
Gs | αs2 | Human | - | 96 | - | - | - | - | X-ray | 7BPH | - | 1.6 | - | - | - | - | - | - | - | GN13 | - | - | - | - | - | Dai SA, Hu Q, Gao R, Blythe EE, Touhara KK, Peacock H, Zhang Z, von Zastrow M, Suga H, Shokat KM | 36170854 | 2021-03-31 | 53739 | |
Gs | αs2 | Human | - | 88 | - | - | - | - | X-ray | 7E5E | - | 2.0 | - | - | - | - | - | - | - | GD20 | - | - | - | - | - | Dai SA, Hu Q, Gao R, Blythe EE, Touhara KK, Peacock H, Zhang Z, von Zastrow M, Suga H, Shokat KM | 36170854 | 2022-03-02 | 53739 | |
Gs | αs2 | Human | - | 96 | - | - | - | - | Cryo-EM | 8EL7 | - | 2.8 | - | - | - | - | - | - | - | Isoform 1 of Synembryn-B | - | - | - | - | - | Papasergi-Scott MM, Kwarcinski FE, Yu M, Panova O, Ovrutsky AM, Skiniotis G, Tall GG | 36931277 | 2023-03-01 | 53739 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 1AZS | - | 2.3 | - | - | - | - | - | - | - |
VC1 IIC2 |
- | - | - | - | - | Tesmer JJ, Sunahara RK, Gilman AG, Sprang SR | 9417641 | 1998-02-25 | 53756 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 1AZT | - | 2.3 | - | - | - | - | - | - | - | - | - | - | - | - | - | Sunahara RK, Tesmer JJ, Gilman AG, Sprang SR | 9395396 | 1998-02-25 | 53756 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 1CJK | - | 3.0 | - | - | - | - | - | - | - |
Adenylate cyclase type V ADENYLATE CYCLASE TYPE II |
- | - | - | - | - | Tesmer JJ, Sunahara RK, Johnson RA, Gosselin G, Gilman AG, Sprang SR | 10427002 | 1999-08-31 | 53756 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 1CJT | - | 2.8 | - | - | - | - | - | - | - |
Adenylate cyclase type V ADENYLATE CYCLASE TYPE II |
- | - | - | - | - | Tesmer JJ, Sunahara RK, Johnson RA, Gosselin G, Gilman AG, Sprang SR | 10427002 | 1999-08-31 | 53756 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 1CJU | - | 2.8 | - | - | - | - | - | - | - |
Adenylate cyclase type V ADENYLATE CYCLASE TYPE II |
- | - | - | - | - | Tesmer JJ, Sunahara RK, Johnson RA, Gosselin G, Gilman AG, Sprang SR | 10427002 | 1999-08-31 | 53756 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 1CJV | - | 3.0 | - | - | - | - | - | - | - |
Adenylate cyclase type V ADENYLATE CYCLASE TYPE II |
- | - | - | - | - | Tesmer JJ, Sunahara RK, Johnson RA, Gosselin G, Gilman AG, Sprang SR | 10427002 | 1999-08-31 | 53756 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 1CS4 | - | 2.5 | - | - | - | - | - | - | - |
TYPE V ADENYLATE CYCLASE TYPE II ADENYLATE CYCLASE |
- | - | - | - | - | Tesmer JJ, Dessauer CW, Sunahara RK, Murray LD, Johnson RA, Gilman AG, Sprang SR | 11087399 | 2001-01-10 | 53756 | |
Gs | αs2 | Bovine | - | 96 | - | - | - | - | X-ray | 1CUL | - | 2.4 | - | - | - | - | - | - | - |
TYPE V ADENYLYL CYCLASE TYPE II ADENYLYL CYCLASE |
- | - | - | - | - | Tesmer JJ, Dessauer CW, Sunahara RK, Murray LD, Johnson RA, Gilman AG, Sprang SR | 11087399 | 2001-01-10 | 53756 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 1TL7 | - | 2.8 | - | - | - | - | - | - | - |
Adenylate cyclase type V Adenylate cyclase type II |
- | - | - | - | - | Mou TC, Gille A, Fancy DA, Seifert R, Sprang SR | 15591060 | 2004-12-14 | 53756 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 1U0H | - | 2.9 | - | - | - | - | - | - | - |
Adenylate cyclase type V Adenylate cyclase type II |
- | - | - | - | - | Mou TC, Gille A, Fancy DA, Seifert R, Sprang SR | 15591060 | 2004-12-14 | 53756 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 2GVD | - | 2.9 | - | - | - | - | - | - | - |
Adenylate cyclase type 5 Adenylate cyclase type 2 |
- | - | - | - | - | Mou TC, Gille A, Suryanarayana S, Richter M, Seifert R, Sprang SR | 16766715 | 2006-07-04 | 53756 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 2GVZ | - | 3.3 | - | - | - | - | - | - | - |
Adenylate cyclase type 5 Adenylate cyclase type 2 |
- | - | - | - | - | Mou TC, Gille A, Suryanarayana S, Richter M, Seifert R, Sprang SR | 16766715 | 2006-07-04 | 53756 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 3C14 | - | 2.7 | - | - | - | - | - | - | - |
Adenylate cyclase type 5 Adenylate cyclase type 2 |
- | - | - | - | - | Mou TC, Masada N, Cooper DM, Sprang SR | 19243146 | 2009-02-03 | 53756 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 3C15 | - | 2.8 | - | - | - | - | - | - | - |
Adenylate cyclase type 5 Adenylate cyclase type 2 |
- | - | - | - | - | Mou TC, Masada N, Cooper DM, Sprang SR | 19243146 | 2009-02-03 | 53756 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 3C16 | - | 2.9 | - | - | - | - | - | - | - |
Adenylate cyclase type 5 Adenylate cyclase type 2 |
- | - | - | - | - | Mou TC, Masada N, Cooper DM, Sprang SR | 19243146 | 2009-02-03 | 53756 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 3G82 | - | 3.1 | - | - | - | - | - | - | - |
Adenylate cyclase type 5 Adenylate cyclase type 2 |
- | - | - | - | - | - | - | 2010-02-16 | 53756 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | X-ray | 3MAA | - | 3.0 | - | - | - | - | - | - | - |
Adenylate cyclase type 5 Adenylate cyclase type 2 |
- | - | - | - | - | Mou TC, Masada N, Cooper DM, Sprang SR | 19243146 | 2010-04-07 | 53756 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | Cryo-EM | 6R3Q | - | 3.4 | - | - | - | - | - | - | - | Adenylate cyclase 9 | - | - | - | - | - | Qi C, Sorrentino S, Medalia O, Korkhov VM | 31023924 | 2019-05-08 | 53756 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | Cryo-EM | 6R4O | - | 4.2 | - | - | - | - | - | - | - | Adenylate cyclase 9 | - | - | - | - | - | Qi C, Sorrentino S, Medalia O, Korkhov VM | 31023924 | 2019-05-08 | 53756 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | Cryo-EM | 6R4P | - | 3.1 | - | - | - | - | - | - | - | Adenylate cyclase 9 | - | - | - | - | - | Qi C, Sorrentino S, Medalia O, Korkhov VM | 31023924 | 2019-05-08 | 53756 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | Cryo-EM | 7PDE | - | 4.5 | - | - | - | - | - | - | - | Adenylate cyclase 9 | - | - | - | - | - | Qi C, Lavriha P, Mehta V, Khanppnavar B, Mohammed I, Li Y, Lazaratos M, Schaefer JV, Dreier B, Pluckthun A, Bondar AN, Dessauer CW, Korkhov VM | 35210418 | 2022-01-19 | 53756 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | Cryo-EM | 7PDF | - | 3.8 | - | - | - | - | - | - | - | Adenylate cyclase 9 | - | - | - | - | - | Qi C, Lavriha P, Mehta V, Khanppnavar B, Mohammed I, Li Y, Lazaratos M, Schaefer JV, Dreier B, Pluckthun A, Bondar AN, Dessauer CW, Korkhov VM | 35210418 | 2022-01-26 | 53756 | |
Gs | αs2 | Bovine | - | 100 | - | - | - | - | Cryo-EM | 8BUZ | - | 3.5 | - | - | - | - | - | - | - | Adenylate cyclase type 8 | - | - | - | - | - | Khanppnavar B, Schuster D, Lavriha P, Uliana F, Ozel M, Mehta V, Leitner A, Picotti P, Korkhov VM | 38351373 | 2023-12-13 | 53756 | |
Gs | αs2 | Rat | - | 100 | β1 | Human | γ2 | Human | Cryo-EM | 8UHB | - | 3.4 | - | - | - | - | - | - | Nanobody-35 | - | - | - | - | - | - | Zilberg G, Parpounas AK, Warren AL, Yang S, Wacker D | 38168118 | 2024-01-10 | 53758 | |
Gs | αl | Human | - | 100 | - | - | - | - | Cryo-EM | 8EL8 | - | 3.2 | - | - | - | - | - | - | - | Isoform 1 of Synembryn-B | - | - | - | - | - | Papasergi-Scott MM, Kwarcinski FE, Yu M, Panova O, Ovrutsky AM, Skiniotis G, Tall GG | 36931277 | 2023-03-01 | 53740 | |
Gs | αl | Mouse | - | 100 | - | - | - | - | X-ray | 8HTG | - | 2.9 | - | - | - | - | - | - | - | - | - | - | - | - | - | Choi C, Bae J, Kim S, Lee S, Kang H, Kim J, Bang I, Kim K, Huh WK, Seok C, Park H, Im W, Choi HJ | 38062020 | 2023-12-20 | 53774 | |
Gi/o | αi1 | Human | - | 92 | - | - | - | - | X-ray | 1KJY | - | 2.7 | - | - | - | - | - | - | - | Regulator of G-protein signaling 14 | - | - | - | - | - | Kimple RJ, Kimple ME, Betts L, Sondek J, Siderovski DP | 11976690 | 2002-05-08 | 53741 | |
Gi/o | αi1 | Human | - | 93 | - | - | - | - | X-ray | 1Y3A | - | 2.5 | - | - | - | - | - | - | - | KB752 peptide | - | - | - | - | - | Johnston CA, Willard FS, Jezyk MR, Fredericks Z, Bodor ET, Jones MB, Blaesius R, Watts VJ, Harden TK, Sondek J, Ramer JK, Siderovski DP | 16004878 | 2005-07-12 | 53741 | |
Gi/o | αi1 | Human | - | 88 | - | - | - | - | X-ray | 2G83 | - | 2.8 | - | - | - | - | - | - | - | KB-1753 phage display peptide | - | - | - | - | - | Johnston CA, Lobanova ES, Shavkunov AS, Low J, Ramer JK, Blaesius R, Fredericks Z, Willard FS, Kuhlman B, Arshavsky VY, Siderovski DP | 16981699 | 2006-10-10 | 53741 | |
Gi/o | αi1 | Human | - | 91 | - | - | - | - | X-ray | 2GTP | - | 2.6 | - | - | - | - | - | - | - | Regulator of G-protein signaling 1 | - | - | - | - | - | Soundararajan M, Willard FS, Kimple AJ, Turnbull AP, Ball LJ, Schoch GA, Gileadi C, Fedorov OY, Dowler EF, Higman VA, Hutsell SQ, Sundstrom M, Doyle DA, Siderovski DP | 18434541 | 2006-05-23 | 53741 | |
Gi/o | αi1 | Human | - | 92 | - | - | - | - | X-ray | 2IK8 | - | 2.7 | - | - | - | - | - | - | - | Regulator of G-protein signaling 16 | - | - | - | - | - | Soundararajan M, Willard FS, Kimple AJ, Turnbull AP, Ball LJ, Schoch GA, Gileadi C, Fedorov OY, Dowler EF, Higman VA, Hutsell SQ, Sundstrom M, Doyle DA, Siderovski DP | 18434541 | 2006-11-21 | 53741 | |
Gi/o | αi1 | Human | - | 92 | - | - | - | - | X-ray | 2OM2 | - | 2.2 | - | - | - | - | - | - | - | Regulator of G-protein signalling 14 GoLoco motif peptide | - | - | - | - | - | Sammond DW, Eletr ZM, Purbeck C, Kimple RJ, Siderovski DP, Kuhlman B | 17603074 | 2007-07-10 | 53741 | |
Gi/o | αi1 | Human | - | 92 | - | - | - | - | X-ray | 2XNS | - | 3.4 | - | - | - | - | - | - | - | Regulator of G-protein signaling 14 | - | - | - | - | - | Sammond DW, Bosch DE, Butterfoss GL, Purbeck C, Machius M, Siderovski DP, Kuhlman B | 21388199 | 2011-06-08 | 53741 | |
Gi/o | αi1 | Human | - | 93 | - | - | - | - | X-ray | 3ONW | - | 2.4 | - | - | - | - | - | - | - | Regulator of G-protein signaling 14 | - | - | - | - | - | Bosch DE, Kimple AJ, Sammond DW, Muller RE, Miley MJ, Machius M, Kuhlman B, Willard FS, Siderovski DP | 21115486 | 2010-11-24 | 53741 | |
Gi/o | αi1 | Human | - | 92 | - | - | - | - | X-ray | 3QE0 | - | 3.0 | - | - | - | - | - | - | - | KB752 peptide | - | - | - | - | - | Bosch DE, Willard FS, Ramanujam R, Kimple AJ, Willard MD, Naqvi NI, Siderovski DP | 22383884 | 2012-01-25 | 53741 | |
Gi/o | αi1 | Human | - | 93 | - | - | - | - | X-ray | 3QI2 | - | 2.8 | - | - | - | - | - | - | - | Regulator of G-protein signaling 14 | - | - | - | - | - | Bosch DE, Willard FS, Ramanujam R, Kimple AJ, Willard MD, Naqvi NI, Siderovski DP | 22383884 | 2012-02-01 | 53741 | |
Gi/o | αi1 | Human | - | 100 | - | - | - | - | X-ray | 3UMR | - | 2.0 | - | - | - | - | - | - | - | - | - | - | - | - | - | - | - | 2012-10-24 | 53741 | |
Gi/o | αi1 | Human | - | 100 | - | - | - | - | X-ray | 3UMS | - | 2.3 | - | - | - | - | - | - | - | - | - | - | - | - | - | - | - | 2012-02-08 | 53741 | |
Gi/o | αi1 | Human | - | 93 | - | - | - | - | X-ray | 4G5Q | - | 2.9 | - | - | - | - | - | - | - | G-protein-signaling modulator 2 | - | - | - | - | - | - | - | 2012-09-05 | 53741 | |
Gi/o | αi1 | Human | - | 100 | β1 | Rat | γ2 | Bovine | X-ray | 5TDH | - | 3.0 | - | - | - | - | - | - | - | - | - | - | - | - | - | Liu P, Jia MZ, Zhou XE, De Waal PW, Dickson BM, Liu B, Hou L, Yin YT, Kang YY, Shi Y, Melcher K, Xu HE, Jiang Y | 27498775 | 2016-11-09 | 53741 | |
Gi/o | αi1 | Human | - | 100 | β1 | Human | γ2 | Human | X-ray | 6CRK | - | 2.0 | - | - | - | - | - | - | single-chain Fv | - | - | - | - | - | - | Maeda S, Koehl A, Matile H, Hu H, Hilger D, Schertler GFX, Manglik A, Skiniotis G, Dawson RJP, Kobilka BK | 30213947 | 2018-10-24 | 53741 | |
Gi/o | αi1 | Human | - | 100 | - | - | - | - | Cryo-EM | 6VU8 | - | 4.1 | - | - | - | - | - | - | - | Resistance to inhibitors of cholinesterase 8 homolog A (C. elegans) | - | - | - | - | - | Seven AB, Hilger D, Papasergi-Scott MM, Zhang L, Qu Q, Kobilka BK, Tall GG, Skiniotis G | 32126208 | 2020-03-18 | 53741 | |
Gi/o | αi1 | Human | - | 100 | β1 | Human | γ2 | Human | Cryo-EM | 7RKX | - | 3.1 | - | - | - | - | - | - | Antibody fragment scFv16 | G-protein coupled receptor homolog US27 | - | - | - | - | - | - | - | 2022-01-26 | 53741 | |
Gi/o | αi1 | Human | - | 100 | β1 | Human | γ2 | Human | Cryo-EM | 7RKY | - | 3.8 | - | - | - | - | - | - | Antibody fragment scFv16 | G-protein coupled receptor homolog US27 | - | - | - | - | - | - | - | 2022-01-26 | 53741 | |
Gi/o | αi1 | Human | - | 100 | β1 | Human | γ2 | Human | Cryo-EM | 7YOO | - | 3.1 | - | - | - | - | - | - | single-chain antibody Fv fragment (scFv16) |
Neuropeptide Y Neuropeptide Y receptor type 2 |
- | - | - | - | - | Kang H, Park C, Choi YK, Bae J, Kwon S, Kim J, Choi C, Seok C, Im W, Choi HJ | 36525977 | 2023-03-22 | 53741 | |
Gi/o | αi1 | Human | - | 100 | β1 | Human | γ2 | Human | Cryo-EM | 8HNL | - | 3.0 | - | - | - | - | - | - | single-chain variable fragment scFv16 | - | - | - | - | - | - | Jiao H, Pang B, Liu A, Chen Q, Pan Q, Wang X, Xu Y, Chiang YC, Ren R, Hu H | 38177682 | 2023-11-29 | 53741 | |
Gi/o | αi1 | Human | - | 100 | β1 | Human | γ2 | Human | Cryo-EM | 8J6J | - | 2.8 | - | - | - | - | - | - | - |
Scfv16 Hydroxycarboxylic acid receptor 2 hydroxycarboxylic acid receptor 2 |
- | - | - | - | - | Zhu S, Yuan Q, Li X, He X, Shen S, Wang D, Li J, Cheng X, Duan X, Xu HE, Duan J | 37952153 | 2024-01-10 | 53741 | |
Gi/o | αi1 | Human | - | 100 | β1 | Human | γ2 | Human | Cryo-EM | 8JGB | - | 2.8 | - | - | - | - | - | - | scFv16 |
Conorfamide-Tx2 Mas-related G-protein coupled receptor member X1 |
- | - | - | - | - | Guo L, Zhang Y, Fang G, Tie L, Zhuang Y, Xue C, Liu Q, Zhang M, Zhu K, You C, Xu P, Yuan Q, Zhang C, Liu L, Rong N, Peng S, Liu Y, Wang C, Luo X, Lv Z, Kang D, Yu X, Zhang C, Jiang Y, Dong X, Zhou J, Liu Z, Yang F, Eric Xu H, Sun JP | 37591889 | 2024-01-10 | 53741 | |
Gi/o | αi1 | Human | - | 100 | β1 | Human | γ2 | Human | Cryo-EM | 8JGG | - | 3.0 | - | - | - | - | - | - | - |
BAM8-22 Single-Chain Fragment Variable 16 Mas-related G-protein coupled receptor member X1 |
- | - | - | - | - | Guo L, Zhang Y, Fang G, Tie L, Zhuang Y, Xue C, Liu Q, Zhang M, Zhu K, You C, Xu P, Yuan Q, Zhang C, Liu L, Rong N, Peng S, Liu Y, Wang C, Luo X, Lv Z, Kang D, Yu X, Zhang C, Jiang Y, Dong X, Zhou J, Liu Z, Yang F, Eric Xu H, Sun JP | 37591889 | 2024-01-10 | 53741 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1AGR | - | 2.8 | - | - | - | - | - | - | - | RGS4 | - | - | - | - | - | Tesmer JJ, Berman DM, Gilman AG, Sprang SR | 9108480 | 1997-06-16 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1AS0 | - | 2.0 | - | - | - | - | - | - | - | - | - | - | - | - | - | Raw AS, Coleman DE, Gilman AG, Sprang SR | 9398294 | 1997-11-12 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1AS2 | - | 2.8 | - | - | - | - | - | - | - | - | - | - | - | - | - | Raw AS, Coleman DE, Gilman AG, Sprang SR | 9398294 | 1997-11-12 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1AS3 | - | 2.4 | - | - | - | - | - | - | - | - | - | - | - | - | - | Raw AS, Coleman DE, Gilman AG, Sprang SR | 9398294 | 1997-11-12 | 53801 | |
Gi/o | αi1 | Rat | - | 89 | - | - | - | - | X-ray | 1BH2 | - | 2.1 | - | - | - | - | - | - | - | - | - | - | - | - | - | Posner BA, Mixon MB, Wall MA, Sprang SR, Gilman AG | 9705312 | 1998-11-04 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1BOF | - | 2.2 | - | - | - | - | - | - | - | - | - | - | - | - | - | Coleman DE, Sprang SR | 9772163 | 1999-01-06 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1CIP | - | 1.5 | - | - | - | - | - | - | - | - | - | - | - | - | - | Coleman DE, Sprang SR | 10358003 | 1999-04-09 | 53801 | |
Gi/o | αi1 | Rat | - | 92 | - | - | - | - | X-ray | 1FQJ | - | 2.0 | - | - | - | - | - | - | - | Regulator of G-protein signaling 9 | - | - | - | - | - | Slep KC, Kercher MA, He W, Cowan CW, Wensel TG, Sigler PB | 11234020 | 2001-02-28 | 53801 | |
Gi/o | αi1 | Rat | - | 92 | - | - | - | - | X-ray | 1FQK | - | 2.3 | - | - | - | - | - | - | - | Regulator of G-protein signaling 9 | - | - | - | - | - | Slep KC, Kercher MA, He W, Cowan CW, Wensel TG, Sigler PB | 11234020 | 2001-02-28 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1GDD | - | 2.2 | - | - | - | - | - | - | - | - | - | - | - | - | - | Mixon MB, Lee E, Coleman DE, Berghuis AM, Gilman AG, Sprang SR | 7481799 | 1995-11-27 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1GFI | - | 2.2 | - | - | - | - | - | - | - | - | - | - | - | - | - | Coleman DE, Berghuis AM, Lee E, Linder ME, Gilman AG, Sprang SR | 8073283 | 1995-03-31 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | β1 | Bovine | γ2 | Bovine | X-ray | 1GG2 | - | 2.4 | - | - | - | - | - | - | - | - | - | - | - | - | - | Wall MA, Coleman DE, Lee E, Iniguez-Lluhi JA, Posner BA, Gilman AG, Sprang SR | 8521505 | 1997-02-12 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1GIA | - | 2.0 | - | - | - | - | - | - | - | - | - | - | - | - | - | Coleman DE, Berghuis AM, Lee E, Linder ME, Gilman AG, Sprang SR | 8073283 | 1994-09-30 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1GIL | - | 2.3 | - | - | - | - | - | - | - | - | - | - | - | - | - | Coleman DE, Berghuis AM, Lee E, Linder ME, Gilman AG, Sprang SR | 8073283 | 1995-02-14 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1GIT | - | 2.6 | - | - | - | - | - | - | - | - | - | - | - | - | - | Berghuis AM, Lee E, Raw AS, Gilman AG, Sprang SR | 8939752 | 1997-02-12 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | β1 | Bovine | γ2 | Bovine | X-ray | 1GP2 | - | 2.3 | - | - | - | - | - | - | - | - | - | - | - | - | - | Wall MA, Coleman DE, Lee E, Iniguez-Lluhi JA, Posner BA, Gilman AG, Sprang SR | 8521505 | 1997-02-12 | 53801 | |
Gi/o | αi1 | Rat | - | 96 | - | - | - | - | X-ray | 1SHZ | - | 2.9 | - | - | - | - | - | - | - |
Guanine Nucleotide-Binding Protein Galpha(13):Galpha(i1) Chimera Rho guanine nucleotide exchange factor 1 |
- | - | - | - | - | Chen Z, Singer WD, Sternweis PC, Sprang SR | 15665872 | 2005-01-18 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1SVK | - | 2.0 | - | - | - | - | - | - | - | - | - | - | - | - | - | Thomas CJ, Du X, Li P, Wang Y, Ross EM, Sprang SR | 15128951 | 2004-06-01 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 1SVS | - | 1.5 | - | - | - | - | - | - | - | - | - | - | - | - | - | Thomas CJ, Du X, Li P, Wang Y, Ross EM, Sprang SR | 15128951 | 2004-06-01 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | β1 | Bovine | γ2 | Bovine | X-ray | 2BCJ | - | 3.1 | - | - | - | - | - | - | - | G-protein-coupled receptor kinase 2 | - | - | - | - | - | Tesmer VM, Kawano T, Shankaranarayanan A, Kozasa T, Tesmer JJ | 16339447 | 2005-12-20 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 2RGN | - | 3.5 | - | - | - | - | - | - | - |
Rho guanine nucleotide exchange factor 25 Transforming protein RhoA |
- | - | - | - | - | Lutz S, Shankaranarayanan A, Coco C, Ridilla M, Nance MR, Vettel C, Baltus D, Evelyn CR, Neubig RR, Wieland T, Tesmer JJ | 18096806 | 2008-01-15 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 2ZJY | - | 2.8 | - | - | - | - | - | - | - | - | - | - | - | - | - | - | - | 2009-03-24 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 2ZJZ | - | 2.6 | - | - | - | - | - | - | - | - | - | - | - | - | - | - | - | 2009-03-24 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | β1 | Bovine | γ2 | Bovine | X-ray | 3AH8 | - | 2.9 | - | - | - | - | - | - | - | YM-254890 | - | - | - | - | - | Nishimura A, Kitano K, Takasaki J, Taniguchi M, Mizuno N, Tago K, Hakoshima T, Itoh H | 20639466 | 2010-07-21 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 3D7M | - | 2.9 | - | - | - | - | - | - | - | - | - | - | - | - | - | Preininger AM, Funk MA, Oldham WM, Meier SM, Johnston CA, Adhikary S, Kimple AJ, Siderovski DP, Hamm HE, Iverson TM | 19222191 | 2009-03-03 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 3FFA | - | 2.3 | - | - | - | - | - | - | - | - | - | - | - | - | - | Kapoor N, Menon ST, Chauhan R, Sachdev P, Sakmar TP | 19703466 | 2009-10-06 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 3FFB | - | 2.6 | - | - | - | - | - | - | - | - | - | - | - | - | - | Kapoor N, Menon ST, Chauhan R, Sachdev P, Sakmar TP | 19703466 | 2009-10-06 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 3V00 | - | 2.9 | - | - | - | - | - | - | - | - | - | - | - | - | - | Singh G, Ramachandran S, Cerione RA | 22448927 | 2012-04-18 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 4N0D | - | 1.6 | - | - | - | - | - | - | - | - | - | - | - | - | - | Thaker TM, Sarwar M, Preininger AM, Hamm HE, Iverson TM | 24596087 | 2014-03-12 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 4N0E | - | 2.1 | - | - | - | - | - | - | - | - | - | - | - | - | - | Thaker TM, Sarwar M, Preininger AM, Hamm HE, Iverson TM | 24596087 | 2014-03-12 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 4PAM | - | 2.1 | - | - | - | - | - | - | - | - | - | - | - | - | - | Kaya AI, Lokits AD, Gilbert JA, Iverson TM, Meiler J, Hamm HE | 25037222 | 2014-07-30 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 4PAN | - | 2.4 | - | - | - | - | - | - | - | - | - | - | - | - | - | Kaya AI, Lokits AD, Gilbert JA, Iverson TM, Meiler J, Hamm HE | 25037222 | 2014-07-30 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 4PAO | - | 2.0 | - | - | - | - | - | - | - | - | - | - | - | - | - | Kaya AI, Lokits AD, Gilbert JA, Iverson TM, Meiler J, Hamm HE | 25037222 | 2014-07-30 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 4PAQ | - | 2.0 | - | - | - | - | - | - | - | - | - | - | - | - | - | Kaya AI, Lokits AD, Gilbert JA, Iverson TM, Meiler J, Hamm HE | 25037222 | 2014-07-30 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 5KDL | - | 2.7 | - | - | - | - | - | - | - | - | - | - | - | - | - | Kaya AI, Lokits AD, Gilbert JA, Iverson TM, Meiler J, Hamm HE | 27462082 | 2016-08-03 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | β1 | Bovine | γT1 | Bovine | X-ray | 5KDO | - | 1.9 | - | - | - | - | - | - | - | - | - | - | - | - | - | Kaya AI, Lokits AD, Gilbert JA, Iverson TM, Meiler J, Hamm HE | 27462082 | 2016-08-03 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 6M8H | - | 2.1 | - | - | - | - | - | - | - | - | - | - | - | - | - | - | - | 2019-08-21 | 53801 | |
Gi/o | αi1 | Rat | - | 100 | - | - | - | - | X-ray | 6TYL | - | 3.3 | - | - | - | - | - | - |
Nanobody A Nanobody B Nanobody C |
Resistance to inhibitors of cholinesterase 8 homolog A (C. elegans) | - | - | - | - | - | McClelland LJ, Zhang K, Mou TC, Johnston J, Yates-Hansen C, Li S, Thomas CJ, Doukov TI, Triest S, Wohlkonig A, Tall GG, Steyaert J, Chiu W, Sprang SR | 32103024 | 2020-03-11 | 53801 | |
Gi/o | αi1 | Rat | - | 91 | - | - | - | - | Cryo-EM | 6UKT | - | 3.9 | - | - | - | - | - | - |
NB8109 NB8117 NB8119 NB9156 |
Resistance to inhibitors of cholinesterase 8 homolog A (C. elegans) | - | - | - | - | - | McClelland LJ, Zhang K, Mou TC, Johnston J, Yates-Hansen C, Li S, Thomas CJ, Doukov TI, Triest S, Wohlkonig A, Tall GG, Steyaert J, Chiu W, Sprang SR | 32103024 | 2020-03-11 | 53801 | |
Gi/o | αi3 | Human | - | 91 | - | - | - | - | X-ray | 2IHB | - | 2.7 | - | - | - | - | - | - | - | Regulator of G-protein signalling 10 | - | - | - | - | - | Soundararajan M, Willard FS, Kimple AJ, Turnbull AP, Ball LJ, Schoch GA, Gileadi C, Fedorov OY, Dowler EF, Higman VA, Hutsell SQ, Sundstrom M, Doyle DA, Siderovski DP | 18434541 | 2006-11-21 | 53743 | |
Gi/o | αi3 | Human | - | 99 | - | - | - | - | X-ray | 2ODE | - | 1.9 | - | - | - | - | - | - | - | Regulator of G-protein signaling 8 | - | - | - | - | - | Soundararajan M, Willard FS, Kimple AJ, Turnbull AP, Ball LJ, Schoch GA, Gileadi C, Fedorov OY, Dowler EF, Higman VA, Hutsell SQ, Sundstrom M, Doyle DA, Siderovski DP | 18434541 | 2007-02-06 | 53743 | |
Gi/o | αi3 | Human | - | 99 | - | - | - | - | X-ray | 2V4Z | - | 2.8 | - | - | - | - | - | - | - | REGULATOR OF G-PROTEIN SIGNALING 2 | - | - | - | - | - | Kimple AJ, Soundararajan M, Hutsell SQ, Roos AK, Urban DJ, Setola V, Temple BR, Roth BL, Knapp S, Willard FS, Siderovski DP | 19478087 | 2008-11-04 | 53743 | |
Gi/o | αi3 | Human | - | 93 | - | - | - | - | X-ray | 4G5O | - | 2.9 | - | - | - | - | - | - | - | G-protein-signaling modulator 2 | - | - | - | - | - | - | - | 2012-09-05 | 53743 | |
Gi/o | αi3 | Human | - | 93 | - | - | - | - | X-ray | 4G5R | - | 3.5 | - | - | - | - | - | - | - | G-protein-signaling modulator 2 | - | - | - | - | - | - | - | 2012-09-05 | 53743 | |
Gi/o | αi3 | Human | - | 93 | - | - | - | - | X-ray | 4G5S | - | 3.6 | - | - | - | - | - | - | - | G-protein-signaling modulator 2 | - | - | - | - | - | - | - | 2012-09-05 | 53743 | |
Gi/o | αi3 | Human | - | 100 | - | - | - | - | Cryo-EM | 7X6I | - | 3.9 | - | - | - | - | - | - | - | Short transient receptor potential channel 5 | - | - | - | - | - | Won J, Kim J, Jeong H, Kim J, Feng S, Jeong B, Kwak M, Ko J, Im W, So I, Lee HH | 37137991 | 2023-04-26 | 53743 | |
Gi/o | αi3 | Human | - | 100 | - | - | - | - | Cryo-EM | 8GVX | - | 3.9 | - | - | - | - | - | - | - | Short transient receptor potential channel 5 | - | - | - | - | - | Won J, Kim J, Jeong H, Kim J, Feng S, Jeong B, Kwak M, Ko J, Im W, So I, Lee HH | 37137991 | 2023-05-24 | 53743 | |
Gi/o | αi3 | Rat | - | 99 | - | - | - | - | X-ray | 6MHE | - | 2.2 | - | - | - | - | - | - | - | KB752 peptide | - | - | - | - | - | Kalogriopoulos NA, Rees SD, Ngo T, Kopcho NJ, Ilatovskiy AV, Sun N, Komives EA, Chang G, Ghosh P, Kufareva I | 31363053 | 2019-07-31 | 53848 | |
Gi/o | αi3 | Rat | - | 99 | - | - | - | - | X-ray | 6MHF | - | 2.0 | - | - | - | - | - | - | - | Girdin | - | - | - | - | - | Kalogriopoulos NA, Rees SD, Ngo T, Kopcho NJ, Ilatovskiy AV, Sun N, Komives EA, Chang G, Ghosh P, Kufareva I | 31363053 | 2019-07-31 | 53848 | |
Gi/o | αt1 | Human | - | 3 | - | - | - | - | X-ray | 3RBQ | - | 2.0 | - | - | - | - | - | - | - | Protein unc-119 homolog A | - | - | - | - | - | Zhang H, Constantine R, Vorobiev S, Chen Y, Seetharaman J, Huang YJ, Xiao R, Montelione GT, Gerstner CD, Davis MW, Inana G, Whitby FG, Jorgensen EM, Hill CP, Tong L, Baehr W | 21642972 | 2011-06-08 | 53744 | |
Gi/o | αt1 | Bovine | - | 100 | β1 | Bovine | γT1 | Bovine | X-ray | 1GOT | - | 2.0 | - | - | - | - | - | - | - | - | - | - | - | - | - | Lambright DG, Sondek J, Bohm A, Skiba NP, Hamm HE, Sigler PB | 8552184 | 1997-03-12 | 53851 | |
Gi/o | αt1 | Bovine | - | 93 | - | - | - | - | X-ray | 1TAD | - | 1.7 | - | - | - | - | - | - | - | - | - | - | - | - | - | Sondek J, Lambright DG, Noel JP, Hamm HE, Sigler PB | 7969474 | 1995-05-08 | 53851 | |
Gi/o | αt1 | Bovine | - | 93 | - | - | - | - | X-ray | 1TAG | - | 1.8 | - | - | - | - | - | - | - | - | - | - | - | - | - | Lambright DG, Noel JP, Hamm HE, Sigler PB | 8208289 | 1995-02-07 | 53851 | |
Gi/o | αt1 | Bovine | - | 93 | - | - | - | - | X-ray | 1TND | - | 2.2 | - | - | - | - | - | - | - | - | - | - | - | - | - | Noel JP, Hamm HE, Sigler PB | 8259210 | 1994-07-31 | 53851 | |
Gi/o | αt1 | Bovine | - | 100 | - | - | - | - | Cryo-EM | 7JSN | - | 3.2 | - | - | - | - | - | - | - |
Rod cGMP-specific 3' 5'-cyclic phosphodiesterase subunit alpha Rod cGMP-specific 3' 5'-cyclic phosphodiesterase subunit beta |
- | - | - | - | - | Gao Y, Eskici G, Ramachandran S, Poitevin F, Seven AB, Panova O, Skiniotis G, Cerione RA | 33007200 | 2020-10-21 | 53851 | |
Gi/o | αt2 | Human | - | 100 | - | - | - | - | X-ray | 6N84 | - | 1.8 | - | - | - | - | - | - | - | - | - | - | - | - | - | Srivastava D, Gakhar L, Artemyev NO | 31300652 | 2019-07-10 | 53745 | |
Gi/o | αt2 | Human | - | 100 | - | - | - | - | X-ray | 6N85 | - | 2.5 | - | - | - | - | - | - | - | Synembryn-A | - | - | - | - | - | Srivastava D, Gakhar L, Artemyev NO | 31300652 | 2019-07-10 | 53745 | |
Gi/o | αo | Mouse | - | 94 | - | - | - | - | X-ray | 3C7K | - | 2.9 | - | - | - | - | - | - | - | Regulator of G-protein signaling 16 | - | - | - | - | - | Slep KC, Kercher MA, Wieland T, Chen CK, Simon MI, Sigler PB | 18434540 | 2008-05-06 | 53926 | |
Gq/11 | αq | Human | - | 100 | - | - | - | - | Cryo-EM | 6VU5 | - | 3.5 | - | - | - | - | - | - | - | Resistance to inhibitors of cholinesterase-8A (Ric-8A) | - | - | - | - | - | Seven AB, Hilger D, Papasergi-Scott MM, Zhang L, Qu Q, Kobilka BK, Tall GG, Skiniotis G | 32126208 | 2020-03-18 | 53749 | |
Gq/11 | αq | Human | - | 98 | - | - | - | - | Cryo-EM | 8JPE | - | 2.9 | - | - | - | - | - | - | - | - | - | - | - | - | - | Duan J, Liu H, Zhao F, Yuan Q, Ji Y, Cai X, He X, Li X, Li J, Wu K, Gao T, Zhu S, Lin S, Wang MW, Cheng X, Yin W, Jiang Y, Yang D, Xu HE | 37532940 | 2023-08-09 | 53749 | |
Gq/11 | αq | Human | - | 99 | - | - | - | - | Cryo-EM | 8UQN | - | 3.4 | - | - | - | - | - | - | - |
1-phosphatidylinositol 4 5-bisphosphate phosphodiesterase beta-3 |
- | - | - | - | - | Falzone ME, MacKinnon R | 37991948 | 2023-12-06 | 53749 | |
Gq/11 | αq | Human | - | 99 | β1 | Human | γ2 | Human | Cryo-EM | 8UQO | - | 3.4 | - | - | - | - | - | - | - |
1-phosphatidylinositol 4 5-bisphosphate phosphodiesterase beta-3 |
- | - | - | - | - | Falzone ME, MacKinnon R | 37991948 | 2023-12-06 | 53749 | |
Gq/11 | αq | Mouse | - | 97 | - | - | - | - | X-ray | 4EKC | - | 7.4 | - | - | - | - | - | - | - | Regulator of G-protein signaling 2 | - | - | - | - | - | Nance MR, Kreutz B, Tesmer VM, Sterne-Marr R, Kozasa T, Tesmer JJ | 23434405 | 2013-01-30 | 53963 | |
Gq/11 | αq | Mouse | - | 97 | - | - | - | - | X-ray | 4EKD | - | 2.7 | - | - | - | - | - | - | - | Regulator of G-protein signaling 2 | - | - | - | - | - | Nance MR, Kreutz B, Tesmer VM, Sterne-Marr R, Kozasa T, Tesmer JJ | 23434405 | 2013-01-30 | 53963 | |
Gq/11 | αq | Mouse | - | 98 | - | - | - | - | X-ray | 4GNK | - | 4.0 | - | - | - | - | - | - | - |
1-phosphatidylinositol 4 5-bisphosphate phosphodiesterase beta-3 |
- | - | - | - | - | Lyon AM, Dutta S, Boguth CA, Skiniotis G, Tesmer JJ | 23377541 | 2013-02-06 | 53963 | |
Gq/11 | αq | Mouse | - | 100 | - | - | - | - | X-ray | 4QJ3 | - | 3.0 | - | - | - | - | - | - | - |
1-phosphatidylinositol 4 5-bisphosphate phosphodiesterase beta-3 |
- | - | - | - | - | Lyon AM, Begley JA, Manett TD, Tesmer JJG | 25435326 | 2014-10-22 | 53963 | |
Gq/11 | αq | Mouse | - | 100 | - | - | - | - | X-ray | 4QJ4 | - | 3.3 | - | - | - | - | - | - | - |
1-phosphatidylinositol 4 5-bisphosphate phosphodiesterase beta-3 |
- | - | - | - | - | Lyon AM, Begley JA, Manett TD, Tesmer JJG | 25435326 | 2014-10-22 | 53963 | |
Gq/11 | αq | Mouse | - | 100 | - | - | - | - | X-ray | 4QJ5 | - | 3.4 | - | - | - | - | - | - | - |
1-phosphatidylinositol 4 5-bisphosphate phosphodiesterase beta-3 |
- | - | - | - | - | Lyon AM, Begley JA, Manett TD, Tesmer JJG | 25435326 | 2014-10-22 | 53963 | |
Gq/11 | αq | Mouse | - | 87 | - | - | - | - | X-ray | 5DO9 | - | 2.6 | - | - | - | - | - | - | - | Regulator of G-protein signaling 8 | - | - | - | - | - | Taylor VG, Bommarito PA, Tesmer JJ | 26755720 | 2016-01-20 | 53963 | |
Gq/11 | αq | Mouse | - | 91 | - | - | - | - | X-ray | 7SQ2 | - | 2.6 | - | - | - | - | - | - | - |
1-phosphatidylinositol 4 5-bisphosphate phosphodiesterase beta-3 |
- | - | - | - | - | Waldo GL, Ricks TK, Hicks SN, Cheever ML, Kawano T, Tsuboi K, Wang X, Montell C, Kozasa T, Sondek J, Harden TK | 20966218 | 2021-11-17 | 53963 | |
G12/13 | α12 | Mouse | - | 95 | - | - | - | - | X-ray | 1ZCA | - | 2.9 | - | - | - | - | - | - | - | - | - | - | - | - | - | Kreutz B, Yau DM, Nance MR, Tanabe S, Tesmer JJ, Kozasa T | 16388592 | 2005-11-15 | 54027 | |
G12/13 | α13 | Mouse | - | 96 | - | - | - | - | X-ray | 1ZCB | - | 2.0 | - | - | - | - | - | - | - | - | - | - | - | - | - | Kreutz B, Yau DM, Nance MR, Tanabe S, Tesmer JJ, Kozasa T | 16388592 | 2005-11-15 | 54046 | |
G12/13 | α13 | Mouse | - | 96 | - | - | - | - | X-ray | 3AB3 | - | 2.4 | - | - | - | - | - | - | - | Rho guanine nucleotide exchange factor 1 | - | - | - | - | - | Hajicek N, Kukimoto-Niino M, Mishima-Tsumagari C, Chow CR, Shirouzu M, Terada T, Patel M, Yokoyama S, Kozasa T | 21507947 | 2010-12-29 | 54046 | |
G12/13 | α13 | Mouse | - | 90 | - | - | - | - | X-ray | 3CX6 | - | 2.5 | - | - | - | - | - | - | - | Rho guanine nucleotide exchange factor 11 | - | - | - | - | - | Chen Z, Singer WD, Danesh SM, Sternweis PC, Sprang SR | 18940608 | 2008-10-28 | 54046 | |
G12/13 | α13 | Mouse | - | 90 | - | - | - | - | X-ray | 3CX7 | - | 2.3 | - | - | - | - | - | - | - | Glutamate Transporter Associated Protein 48 | - | - | - | - | - | Chen Z, Singer WD, Danesh SM, Sternweis PC, Sprang SR | 18940608 | 2008-10-28 | 54046 | |
G12/13 | α13 | Mouse | - | 90 | - | - | - | - | X-ray | 3CX8 | - | 2.0 | - | - | - | - | - | - | - | Rho guanine nucleotide exchange factor 11 | - | - | - | - | - | Chen Z, Singer WD, Danesh SM, Sternweis PC, Sprang SR | 18940608 | 2008-10-28 | 54046 |
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G protein family | Subtype | PDB | UniProt | IUPHAR | Rec. family | Class | Species | PDB Date |
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