Loading...
G PROTEIN
|
STRUCTURE
|
RECEPTOR
|
OTHER PROTEINS
|
STRUCTURE LIGAND
|
ENDOGENOUS LIGAND
|
REFERENCE
|
||||||||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Fam. | α | Species | Note | % of Seq | β | Species | γ | Species | Method |
PDB
|
Refined structure |
Resolution |
UniProt
|
IUPHAR | Receptor family | Class | Species | Receptor fusion | Antibodies | Other | Name | Type | Function | Name | Type | Authors | Reference | PDB Date | ||
Gi/o | αt1 | Bovine | Only H5 | 3 | - | - | - | - | X-ray | 3DQB | - | 3.2 | OPSD | Rhodopsin | Opsins | A (Rhodopsin) | Bovine | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | None | 10.1038/NATURE07330 | 2008-09-23 | 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 |