Loading...
RECEPTOR
| STRUCTURE
| SIGNAL PROTEIN
| AUXILIARY PROTEIN
| STRUCTURE LIGAND
| PHYSIOLOGICAL LIGAND
| SODIUM ION SITE
| REFERENCE
| ANNOTATED
| ||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
UniProt
| IUPHAR | Receptor family | Cl. | Species | Method | PDB
| Resolution | Preferred chain | % of Seq | Family | Subtype | Note | % of Seq | Fusion | Antibodies | Name | Type | Modality | Name | Type | D2x50 S3x39 | Sodium in structure | Authors | Reference | PDB Date | |||||
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| ||||||||||||
| CCR8 | CCR8 | Chemokine | A | Human | Cryo-EM | 8XML | - | 2.6 | R | Active | 100 | 63 | Gi/o | αi1 | - | 62 | BRIL | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | CCL8, CCL1 | peptide | No | No | - | - | 2025-01-01 | Yes | |
| GPR55 | GPR55 | GPR18, GPR55 and GPR119 | A | Human | Cryo-EM | 9IY8 | 9IY8_refined | 3.0 | R | Active | 100 | 92 | G12/13 | α13 | - | 57 | - | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | anandamide, 2-arachidonoylglycerol, N-palmitoylethanolamine, lysophosphatidylinositol, 2-arachidonoylglycerolphosphoinositol | small-molecule | No | No | Chang H, Li X, Shen L, Ge X, Hao S, Wu L, Liu S, Liu J, Cherezov V, Hua T | 10.1038/S41422-024-01046-8 | 2025-01-01 | Yes | |
| GPR55 | GPR55 | GPR18, GPR55 and GPR119 | A | Human | Cryo-EM | 9IYA | - | 3.0 | A | Active | 56 | 86 | - | - | - | - | BRIL | anti-BRIL Fab heavy chain anti-BRIL Fab light chain anti-BRIL Fab Nanobody |
4-(3-Bromo-5-ethoxy-4-hydroxyphenyl)-N-(2-methoxyphenyl)-2-methyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxamide
|
small-molecule | Antagonist | anandamide, 2-arachidonoylglycerol, N-palmitoylethanolamine, lysophosphatidylinositol, 2-arachidonoylglycerolphosphoinositol | small-molecule | No | No | - | - | 2025-01-01 | Yes | |
| LPAR1 | LPA1 | Lysophospholipid (LPA) | A | Human | Cryo-EM | 9IZH | - | 3.0 | R | Active | 100 | 82 | G12/13 | α13 | G13-Gi2 chimera | 56 | BRIL | scFv16 |
lysophosphatidic acid
|
small-molecule | Agonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | No | No | Suzuki S, Tanaka K, Kamegawa A, Nishikawa K, Suzuki H, Oshima A, Fujiyoshi Y | 10.1016/J.JSB.2024.108164 | 2025-01-01 | Yes | |
| LPAR1 | LPA1 | Lysophospholipid (LPA) | A | Human | Cryo-EM | 9IZF | - | 3.1 | R | Active | 100 | 80 | Gi/o | αi1 | - | 61 | BRIL | scFv16 |
lysophosphatidic acid
|
small-molecule | Agonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | No | No | - | - | 2025-01-01 | Yes | |
| LPAR1 | LPA1 | Lysophospholipid (LPA) | A | Human | Cryo-EM | 9IZG | - | 3.0 | R | Active | 100 | 82 | Gq/11 | αq | Gq-Gs chimera | 57 | BRIL | scFv16 |
lysophosphatidic acid
|
small-molecule | Agonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | No | No | - | - | 2025-01-01 | Yes | |
| AA2AR | A2A | Adenosine | A | Human | X-ray | 8UGW | - | 3.9 | A | Active | 69 | 67 | - | - | - | - | T4-Lysozyme | - |
CGS 21680
|
small-molecule | Agonist | adenosine | small-molecule | No | No | - | - | 2024-12-18 | Yes | |
| HCAR3 | HCA3 | Hydroxycarboxylic acid | A | Human | Cryo-EM | 8JEF | 8JEF_refined | 3.0 | A | Active | 100 | 73 | Gi/o | αi1 | - | 61 | - | scFv16 |
3-hydroxyoctanoic acid
|
small-molecule | Agonist | 3-hydroxyoctanoic acid | small-molecule | No | No | Ye F, Pan X, Zhang Z, Xiang X, Li X, Zhang B, Ning P, Liu A, Wang Q, Gong K, Li J, Zhu L, Qian C, Chen G, Du Y | 10.1016/J.CELREP.2024.114895 | 2024-12-18 | Yes | |
| MCHR1 | MCH1 | Melanin-concentrating hormone | A | Human | Cryo-EM | 8YNT | - | 3.4 | R | Inactive | 8 | 69 | - | - | - | - | BRIL | Fab 1B3 heavy chain Fab 1B3 light chain |
CHEMBL242004
|
small-molecule | Antagonist | melanin-concentrating hormone | peptide | No | No | - | - | 2024-12-18 | Yes | |
| MCHR1 | MCH1 | Melanin-concentrating hormone | A | Human | Cryo-EM | 8YNS | - | 3.3 | R | Inactive | 8 | 65 | - | - | - | - | BRIL | Fab 1B3 heavy chain Fab 1B3 light chain |
CHEMBL242004
|
small-molecule | Antagonist | melanin-concentrating hormone | peptide | No | No | - | - | 2024-12-18 | Yes | |
| FFAR1 | FFA1 | Free fatty acid | A | Human | Cryo-EM | 9K1C | 9K1C_refined | 3.2 | R | Active | 100 | 93 | Gi/o | αi1 | - | 62 | - | - |
docosahexaenoic acid
|
small-molecule | Agonist | docosahexaenoic acid, α-linolenic acid, oleic acid, myristic acid | small-molecule | No | No | Ke Y, Huang Y, Yi C, Ma L, Chu X, Wu B, Zhao Q, Han S | 10.1016/J.CELREP.2024.115024 | 2024-12-11 | Yes | |
| FFAR2 | FFA2 | Free fatty acid | A | Human | Cryo-EM | 9K1D | - | 3.3 | R | Active | 100 | 81 | Gi/o | αi1 | - | 62 | - | - |
butyric acid
|
small-molecule | Agonist | acetic acid, propanoic acid, trans-2-methylcrotonic acid, butyric acid | small-molecule | No | No | Ke Y, Huang Y, Yi C, Ma L, Chu X, Wu B, Zhao Q, Han S | 10.1016/J.CELREP.2024.115024 | 2024-12-11 | Yes | |
| MRGRD | MRGPRD | A orphans | A | Human | Cryo-EM | 9DQH | 9DQH_refined | 2.9 | A | Active | 100 | 79 | Gq/11 | αq | Gq-Gs-Gi chimera | 57 | - | scFv16 |
2-[[1-[2-(4-chlorophenyl)-2-methylpropanoyl]piperidin-4-yl]amino]-5,6,7,8-tetrahydro-3H-quinazolin-4-one
|
small-molecule | Agonist | β-alanine | small-molecule | No | No | - | - | 2024-12-11 | Yes | |
| MRGRD | MRGPRD | A orphans | A | Human | Cryo-EM | 9DQJ | 9DQJ_refined | 2.9 | A | Active | 100 | 79 | Gq/11 | αq | Gq-Gs-Gi chimera | 57 | - | scFv16 |
2-[[1-[1-(4-methoxyphenyl)cyclopropanecarbonyl]piperidin-4-yl]amino]-3H-quinazolin-4-one
|
small-molecule | Agonist | β-alanine | small-molecule | No | No | - | - | 2024-12-11 | Yes | |
| S1PR1 | S1P1 | Lysophospholipid (S1P) | A | Human | Cryo-EM | 8YIC | 8YIC_refined | 3.5 | R | Active | 100 | 78 | Gi/o | αi1 | - | 64 | T4-Lysozyme | - |
SAR247799
|
small-molecule | Agonist | sphingosine 1-phosphate, sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate | small-molecule | No | No | - | - | 2024-12-11 | Yes | |
| XCR1 | XCR1 | Chemokine | A | Human | Cryo-EM | 9AST | 9AST_refined | 3.1 | R | Active | 100 | 85 | Gi/o | αi1 | - | 62 | - | scFv16 |
Lymphotactin
|
protein | Agonist | XCL2, XCL1 | peptide | No | No | Zhang X, Schlimgen RR, Singh S, Tomani MP, Volkman BF, Zhang C | 10.1073/PNAS.2405732121 | 2024-12-11 | Yes | |
| APJ | apelin | Apelin | A | Human | X-ray | 8S4D | - | 2.6 | A | Inactive | 16 | 73 | - | - | - | - | BRIL | - |
CMF-019
|
small-molecule | Agonist | [Pyr1]apelin-13, Elabela/Toddler-21, Elabela/Toddler-32, apelin receptor early endogenous ligand, apelin-36, Elabela/Toddler-11, apelin-17, apelin-13 | peptide | No | No | - | - | 2024-12-04 | Yes | |
| GPR6 | GPR6 | A orphans | A | Human | X-ray | 8T1W | - | 3.5 | A | Inactive | 1 | 73 | - | - | - | - | BRIL | - |
CVN424
|
small-molecule | Inverse agonist | sphingosine 1-phosphate | small-molecule | No | No | Barekatain M, Johansson LC, Lam JH, Chang H, Sadybekov AV, Han GW, Russo J, Bliesath J, Brice NL, Carlton MBL, Saikatendu KS, Sun H, Murphy ST, Monenschein H, Schiffer HH, Popov P, Lutomski CA, Robinson CV, Liu ZJ, Hua T, Katritch V, Cherezov V | 10.1126/SCISIGNAL.ADO8741 | 2024-12-04 | Yes | |
| GPR6 | GPR6 | A orphans | A | Human | Cryo-EM | 8TYW | 8TYW_refined | 3.4 | A | Active | 100 | 73 | Gs | αs | - | 60 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | sphingosine 1-phosphate | small-molecule | No | No | Barekatain M, Johansson LC, Lam JH, Chang H, Sadybekov AV, Han GW, Russo J, Bliesath J, Brice NL, Carlton MBL, Saikatendu KS, Sun H, Murphy ST, Monenschein H, Schiffer HH, Popov P, Lutomski CA, Robinson CV, Liu ZJ, Hua T, Katritch V, Cherezov V | 10.1126/SCISIGNAL.ADO8741 | 2024-12-04 | Yes | |
| GPR6 | GPR6 | A orphans | A | Human | X-ray | 8T1V | - | 2.6 | A | Inactive | 1 | 73 | - | - | - | - | BRIL | - |
CHEMBL4763822
|
small-molecule | Inverse agonist | sphingosine 1-phosphate | small-molecule | No | No | Barekatain M, Johansson LC, Lam JH, Chang H, Sadybekov AV, Han GW, Russo J, Bliesath J, Brice NL, Carlton MBL, Saikatendu KS, Sun H, Murphy ST, Monenschein H, Schiffer HH, Popov P, Lutomski CA, Robinson CV, Liu ZJ, Hua T, Katritch V, Cherezov V | 10.1126/SCISIGNAL.ADO8741 | 2024-12-04 | Yes | |
| GPR6 | GPR6 | A orphans | A | Human | X-ray | 8TF5 | - | 2.1 | A | Active | 99 | 73 | - | - | - | - | BRIL | - |
oleic acid
|
small-molecule | Inverse agonist | sphingosine 1-phosphate | small-molecule | No | No | Barekatain M, Johansson LC, Lam JH, Chang H, Sadybekov AV, Han GW, Russo J, Bliesath J, Brice NL, Carlton MBL, Saikatendu KS, Sun H, Murphy ST, Monenschein H, Schiffer HH, Popov P, Lutomski CA, Robinson CV, Liu ZJ, Hua T, Katritch V, Cherezov V | 10.1126/SCISIGNAL.ADO8741 | 2024-12-04 | Yes | |
| LGR4 | LGR4 | A orphans | A | Human | Cryo-EM | 8XFT | - | 3.2 | A | Inactive | 8 | 77 | - | - | - | - | - | Nanobody-52 |
R-spondin-2
|
protein | Agonist | R-spondin-2, R-spondin-1, R-spondin-4, R-spondin-3 | peptide | No | No | - | - | 2024-12-04 | Yes | |
| LGR4 | LGR4 | A orphans | A | Human | Cryo-EM | 8XFP | - | 3.2 | A | Inactive | 8 | 77 | - | - | - | - | - | Nanobody-52 |
R-spondin-2
|
protein | Agonist | R-spondin-2, R-spondin-1, R-spondin-4, R-spondin-3 | peptide | No | No | - | - | 2024-12-04 | Yes | |
| LGR4 | LGR4 | A orphans | A | Human | Cryo-EM | 8Y69 | - | 3.4 | D | Inactive | 8 | 77 | - | - | - | - | - | Nanobody-52 |
R-spondin-2
|
protein | Agonist | R-spondin-2, R-spondin-1, R-spondin-4, R-spondin-3 | peptide | No | No | - | - | 2024-12-04 | Yes | |
| LGR4 | LGR4 | A orphans | A | Human | Cryo-EM | 8XFS | - | 3.2 | A | Inactive | 8 | 77 | - | - | - | - | - | Nanobody-52 |
R-spondin-2
|
protein | Agonist | R-spondin-2, R-spondin-1, R-spondin-4, R-spondin-3 | peptide | No | No | - | - | 2024-12-04 | Yes | |
| PD2R2 | DP2 | Prostanoid | A | Human | Cryo-EM | 9IYB | - | 2.8 | A | Active | 100 | 76 | Gi/o | αi1 | - | 64 | - | scFv16 |
PGD2
|
lipid | Agonist | PGD2, thromboxane A2, PGD3, PGI2, PGF2α, PGE2, PGJ2 | small-molecule | No | No | - | - | 2024-12-04 | Yes | |
| PD2R2 | DP2 | Prostanoid | A | Human | Cryo-EM | 8XXV | - | 2.3 | A | Active | 100 | 76 | Gi/o | αi1 | - | 64 | - | scFv16 |
[(2~{R})-1-hexadecanoyloxy-3-[oxidanyl-[(2~{S},3~{R},5~{R},6~{S})-2,3,4,5,6-pentakis(oxidanyl)cyclohexyl]oxy-phosphoryl]oxy-propan-2-yl] (~{Z})-octadec-9-enoate
|
lipid | PAM | PGD2, thromboxane A2, PGD3, PGI2, PGF2α, PGE2, PGJ2 | small-molecule | No | No | - | - | 2024-12-04 | Yes | |
| PD2R2 | DP2 | Prostanoid | A | Human | Cryo-EM | 8XXU | - | 2.5 | A | Active | 100 | 80 | Gi/o | αi1 | - | 64 | - | scFv16 |
[(2~{R})-1-hexadecanoyloxy-3-[oxidanyl-[(2~{S},3~{R},5~{R},6~{S})-2,3,4,5,6-pentakis(oxidanyl)cyclohexyl]oxy-phosphoryl]oxy-propan-2-yl] (~{Z})-octadec-9-enoate
|
lipid | PAM | PGD2, thromboxane A2, PGD3, PGI2, PGF2α, PGE2, PGJ2 | small-molecule | No | No | - | - | 2024-12-04 | Yes | |
| GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 9IVG | 9IVG_refined | 3.0 | R | Active | 100 | 83 | Gs | αs | Gs-Gi chimera | 62 | - | Nanobody-35 |
CHEMBL410972
|
protein | Agonist | glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide | peptide | No | No | Li J, Li G, Mai Y, Liu X, Yang D, Zhou Q, Wang MW | 10.1016/J.APSB.2024.09.002 | 2024-11-27 | Yes | |
| GRM2 | mGlu2 | Metabotropic glutamate | C | Human | Cryo-EM | 8WGC | - | 6.0 | D | Active | - | 87 | - | - | - | - | - | - |
LY379268
|
small-molecule | Agonist | L-glutamic acid | small-molecule | No | No | Huang W, Jin N, Guo J, Shen C, Xu C, Xi K, Bonhomme L, Quast RB, Shen DD, Qin J, Liu YR, Song Y, Gao Y, Margeat E, Rondard P, Pin JP, Zhang Y, Liu J | 10.1038/S41467-024-54744-7 | 2024-11-27 | Yes | |
| GRM4 | mGlu4 | Metabotropic glutamate | C | Human | Cryo-EM | 8WGD | - | 4.5 | B | Inactive | - | 82 | - | - | - | - | - | - |
(2S)-2-azanyl-2-cyclopropyl-2-(4-phosphonophenyl)ethanoic acid
|
small-molecule | Antagonist | L-glutamic acid, L-serine-O-phosphate | small-molecule | No | No | - | - | 2024-11-27 | Yes | |
| GRM4 | mGlu4 | Metabotropic glutamate | C | Human | Cryo-EM | 8WG9 | - | 4.5 | B | Active | - | 85 | - | - | - | - | - | - |
L-AP4
|
small-molecule | Agonist | L-glutamic acid, L-serine-O-phosphate | small-molecule | No | No | - | - | 2024-11-27 | Yes | |
| LPAR1 | LPA1 | Lysophospholipid (LPA) | A | Human | Cryo-EM | 9J5V | - | 2.9 | R | Active | 100 | 80 | Gi/o | αi1 | - | 63 | - | scFv16 |
CpY
|
small-molecule | Agonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | No | No | - | - | 2024-11-27 | Yes | |
| OPRD | δ | Opioid | A | Human | Cryo-EM | 8Y45 | 8Y45_refined | 3.5 | A | Active | 100 | 77 | Gi/o | αi2 | - | 63 | - | scFv16 |
ADL5859
|
small-molecule | Agonist | dynorphin B, dynorphin A-(1-13), dynorphin A-(1-8), β-endorphin, [Met]enkephalin, [Leu]enkephalin, endomorphin-1, α-neoendorphin, dynorphin A | peptide | No | No | - | - | 2024-11-27 | Yes | |
| T2R14 | TAS2R14 | Taste 2 | T2 | Human | Cryo-EM | 8RQL | - | 3.0 | R | Active | 100 | 88 | Gi/o | αgust | - | 61 | - | scFv16 |
flufenamic acid
|
small-molecule | Agonist | - | - | No | No | Peri L, Matzov D, Huxley DR, Rainish A, Fierro F, Sapir L, Pfeiffer T, Waterloo L, Hubner H, Peleg Y, Gmeiner P, McCormick PJ, Weikert D, Niv MY, Shalev-Benami M | 10.1038/S41467-024-54157-6 | 2024-11-27 | Yes | |
| CNR1 | CB1 | Cannabinoid | A | Human | Cryo-EM | 9BA0 | - | 3.1 | R | Inactive | 7 | 60 | - | - | - | - | Glycogen synthase | Nanobody-36 |
Monlunabant
|
small-molecule | Inverse agonist | anandamide, 2-arachidonoylglycerol | small-molecule | No | No | - | - | 2024-11-20 | Yes | |
| CNR1 | CB1 | Cannabinoid | A | Human | Cryo-EM | 9B9Y | - | 3.5 | R | Inactive | 7 | 60 | - | - | - | - | Glycogen synthase | Nanobody-36 |
taranabant
|
small-molecule | Inverse agonist | anandamide, 2-arachidonoylglycerol | small-molecule | No | No | Kumari P, Dvoracsko S, Enos MD, Ramesh K, Lim D, Hassan SA, Kunos G, Cinar R, Iyer MR, Rosenbaum DM | 10.1038/S41467-024-54206-0 | 2024-11-20 | Yes | |
| CNR1 | CB1 | Cannabinoid | A | Human | Cryo-EM | 9B9Z | - | 3.3 | R | Inactive | 7 | 60 | - | - | - | - | Glycogen synthase | Nanobody-36 |
Zevaquenabant
|
small-molecule | Inverse agonist | anandamide, 2-arachidonoylglycerol | small-molecule | No | No | - | - | 2024-11-20 | Yes | |
| CNR2 | CB2 | Cannabinoid | A | Human | Cryo-EM | 8X3L | 8X3L_refined | 3.1 | R | Active | 100 | 80 | Gi/o | αi1 | - | 62 | - | scFv16 |
CHEMBL5422946
|
small-molecule | Agonist | anandamide, 2-arachidonoylglycerol | small-molecule | No | No | Yang X, Zhou P, Shen S, Hu Q, Tian C, Xia A, Wang Y, Yang Z, Nan J, Zhou Y, Chen S, Tian X, Wu C, Lin G, Zhang L, Wang K, Zheng T, Zou J, Yan W, Shao Z, Yang S | 10.1073/PNAS.2401091121 | 2024-11-20 | Yes | |
| HCAR3 | HCA3 | Hydroxycarboxylic acid | A | Human | Cryo-EM | 8JEI | - | 2.7 | A | Active | 100 | 74 | Gi/o | αi1 | - | 61 | - | scFv16 |
4-(n-propyl)amino-3-nitrobenzoic acid
|
small-molecule | Agonist | 3-hydroxyoctanoic acid | small-molecule | No | No | Ye F, Pan X, Zhang Z, Xiang X, Li X, Zhang B, Ning P, Liu A, Wang Q, Gong K, Li J, Zhu L, Qian C, Chen G, Du Y | 10.1016/J.CELREP.2024.114895 | 2024-11-20 | Yes | |
| OPSD | Rhodopsin | Opsins | A | Bovine | Cryo-EM | 8P13 | - | 5.2 | R | Active | 100 | 91 | Gi/o | αi1 | - | 94 | - | Fab heavy chain Fab light chain scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | - | - | 2024-11-20 | Yes | |
| OPSD | Rhodopsin | Opsins | A | Bovine | Cryo-EM | 8P12 | - | 3.2 | R | Active | 100 | 91 | Gi/o | αi1 | - | 59 | - | Fab heavy chain Fab light chain |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | - | - | 2024-11-20 | Yes | |
| OPSD | Rhodopsin | Opsins | A | Bovine | Cryo-EM | 8P15 | - | 5.9 | R | Active | 100 | 92 | Gi/o | αi1 | - | 96 | - | Fab heavy chain Fab light chain scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | - | - | 2024-11-20 | Yes | |
| ADRB2 | β2 | Adrenoceptors | A | Human | Cryo-EM | 9CHV | - | 4.0 | A | Intermediate | 47 | 63 | - | - | - | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | (-)-noradrenaline, (-)-adrenaline, Zn2+, noradrenaline, L-NOREPINEPHRINE | small-molecule | No | No | Xu J, Chen G, Wang H, Cao S, Heng J, Deupi X, Du Y, Kobilka BK | 10.1073/PNAS.2414544121 | 2024-11-13 | Yes | |
| ADRB2 | β2 | Adrenoceptors | A | Human | Cryo-EM | 9CHU | - | 3.5 | A | Intermediate | 47 | 66 | - | - | - | - | - | - |
Noradrenaline
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline, Zn2+, noradrenaline, L-NOREPINEPHRINE | small-molecule | No | No | Xu J, Chen G, Wang H, Cao S, Heng J, Deupi X, Du Y, Kobilka BK | 10.1073/PNAS.2414544121 | 2024-11-13 | Yes | |
| ADRB2 | β2 | Adrenoceptors | A | Human | Cryo-EM | 9CHX | - | 3.5 | A | Intermediate | 47 | 67 | - | - | - | - | - | - |
Carazolol
|
small-molecule | Inverse agonist | (-)-noradrenaline, (-)-adrenaline, Zn2+, noradrenaline, L-NOREPINEPHRINE | small-molecule | No | No | Xu J, Chen G, Wang H, Cao S, Heng J, Deupi X, Du Y, Kobilka BK | 10.1073/PNAS.2414544121 | 2024-11-13 | Yes | |
| GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 9IVM | - | 3.2 | R | Active | 100 | 83 | Gs | αs | Gs-Gi chimera | 62 | - | Nanobody-35 |
CHEMBL410972
LSN3318839 |
protein small-molecule |
Agonist PAM |
glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide | peptide | No | No | - | - | 2024-11-13 | Yes | |
| GPR55 | GPR55 | GPR18, GPR55 and GPR119 | A | Human | Cryo-EM | 8ZX5 | - | 3.0 | R | Active | 100 | 88 | G12/13 | α13 | - | 56 | - | - |
AM251
|
small-molecule | Agonist | anandamide, 2-arachidonoylglycerol, N-palmitoylethanolamine, lysophosphatidylinositol, 2-arachidonoylglycerolphosphoinositol | small-molecule | No | No | - | - | 2024-11-13 | Yes | |
| GPR55 | GPR55 | GPR18, GPR55 and GPR119 | A | Human | Cryo-EM | 8ZX4 | - | 2.9 | R | Active | 100 | 90 | G12/13 | α13 | - | 56 | - | - |
LPI
|
small-molecule | Agonist | anandamide, 2-arachidonoylglycerol, N-palmitoylethanolamine, lysophosphatidylinositol, 2-arachidonoylglycerolphosphoinositol | small-molecule | No | No | - | - | 2024-11-13 | Yes | |
| MCHR1 | MCH1 | Melanin-concentrating hormone | A | Human | Cryo-EM | 8WWI | 8WWI_refined | 3.4 | R | Active | 100 | 68 | Gi/o | αi1 | - | 63 | - | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | melanin-concentrating hormone | peptide | No | No | - | - | 2024-11-13 | Yes | |
| MCHR1 | MCH1 | Melanin-concentrating hormone | A | Human | Cryo-EM | 8WWM | 8WWM_refined | 2.8 | R | Active | 100 | 68 | Gi/o | αi1 | - | 63 | - | scFv16 |
Melanin-concentrating hormone
|
peptide | Agonist | melanin-concentrating hormone | peptide | No | No | Ye X, Liu G, Li X, He B, Tao Y, Guan J, Mu Y, Liu H, Gong W | 10.1038/S41421-024-00754-0 | 2024-11-13 | Yes | |
| MCHR1 | MCH1 | Melanin-concentrating hormone | A | Human | Cryo-EM | 8WWK | 8WWK_refined | 2.6 | R | Active | 100 | 68 | Gi/o | αi1 | - | 63 | - | scFv16 |
Melanin-concentrating hormone
|
peptide | Agonist | melanin-concentrating hormone | peptide | No | No | Ye X, Liu G, Li X, He B, Tao Y, Guan J, Mu Y, Liu H, Gong W | 10.1038/S41421-024-00754-0 | 2024-11-13 | Yes | |
| MCHR1 | MCH1 | Melanin-concentrating hormone | A | Human | Cryo-EM | 8WWN | 8WWN_refined | 2.7 | R | Active | 100 | 68 | Gi/o | αi1 | - | 63 | - | scFv16 |
Melanin-concentrating hormone
|
peptide | Agonist | melanin-concentrating hormone | peptide | No | No | Ye X, Liu G, Li X, He B, Tao Y, Guan J, Mu Y, Liu H, Gong W | 10.1038/S41421-024-00754-0 | 2024-11-13 | Yes | |
| MCHR1 | MCH1 | Melanin-concentrating hormone | A | Human | Cryo-EM | 8WWJ | - | 3.0 | R | Active | 100 | 68 | Gi/o | αi1 | - | 63 | - | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | melanin-concentrating hormone | peptide | No | No | - | - | 2024-11-13 | Yes | |
| MCHR1 | MCH1 | Melanin-concentrating hormone | A | Human | Cryo-EM | 8WWL | 8WWL_refined | 2.8 | R | Active | 100 | 68 | Gi/o | αi1 | - | 63 | - | scFv16 |
Melanin-concentrating hormone
|
peptide | Agonist | melanin-concentrating hormone | peptide | No | No | Ye X, Liu G, Li X, He B, Tao Y, Guan J, Mu Y, Liu H, Gong W | 10.1038/S41421-024-00754-0 | 2024-11-13 | Yes | |
| MCHR1 | MCH1 | Melanin-concentrating hormone | A | Human | Cryo-EM | 8WWH | 8WWH_refined | 2.8 | R | Active | 100 | 68 | Gi/o | αi1 | - | 63 | - | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | melanin-concentrating hormone | peptide | No | No | - | - | 2024-11-13 | Yes | |
| PTAFR | PAF | Platelet-activating factor | A | Human | Cryo-EM | 8XYD | 8XYD_refined | 2.9 | A | Active | 100 | 89 | Gi/o | αi1 | - | 61 | - | scFv16 |
PAF
|
small-molecule | Agonist | PAF | small-molecule | No | No | Fan W, Xu Y, He X, Luo P, Zhu J, Li J, Wang R, Yuan Q, Wu K, Hu W, Zhao Y, Xu S, Cheng X, Wang Y, Xu HE, Zhuang Y | 10.1016/J.CELREP.2024.114422 | 2024-11-13 | Yes | |
| GRM5 | mGlu5 | Metabotropic glutamate | C | Human | Cryo-EM | 8X0C | - | 3.2 | A | Active | - | 63 | - | - | - | - | - | - |
quisqualate
VU0424465 |
small-molecule small-molecule |
Agonist PAM |
L-glutamic acid | small-molecule | No | No | Cannone G, Berto L, Malhaire F, Ferguson G, Fouillen A, Balor S, Font-Ingles J, Llebaria A, Goudet C, Kotecha A, K R V, Lebon G | 10.1038/S41467-024-55439-9 | 2024-11-06 | Yes | |
| GRM5 | mGlu5 | Metabotropic glutamate | C | Human | Cryo-EM | 8X0B | - | 3.1 | A | Active | - | 64 | - | - | - | - | - | - |
quisqualate
VU0424465 |
small-molecule small-molecule |
Agonist PAM |
L-glutamic acid | small-molecule | No | No | Cannone G, Berto L, Malhaire F, Ferguson G, Fouillen A, Balor S, Font-Ingles J, Llebaria A, Goudet C, Kotecha A, K R V, Lebon G | 10.1038/S41467-024-55439-9 | 2024-11-06 | Yes | |
| GRM5 | mGlu5 | Metabotropic glutamate | C | Human | Cryo-EM | 8X0D | - | 3.5 | A | Active | - | 63 | - | - | - | - | - | - |
quisqualate
VU0424465 |
small-molecule small-molecule |
Agonist PAM |
L-glutamic acid | small-molecule | No | No | Cannone G, Berto L, Malhaire F, Ferguson G, Fouillen A, Balor S, Font-Ingles J, Llebaria A, Goudet C, Kotecha A, K R V, Lebon G | 10.1038/S41467-024-55439-9 | 2024-11-06 | Yes | |
| GRM5 | mGlu5 | Metabotropic glutamate | C | Human | Cryo-EM | 8X0H | - | 4.1 | A | Active | - | 64 | - | - | - | - | - | - |
quisqualate
|
small-molecule | Agonist | L-glutamic acid | small-molecule | No | No | Cannone G, Berto L, Malhaire F, Ferguson G, Fouillen A, Balor S, Font-Ingles J, Llebaria A, Goudet C, Kotecha A, K R V, Lebon G | 10.1038/S41467-024-55439-9 | 2024-11-06 | Yes | |
| GRM5 | mGlu5 | Metabotropic glutamate | C | Human | Cryo-EM | 8X0G | - | 3.0 | A | Active | - | 63 | - | - | - | - | - | - |
quisqualate
|
small-molecule | Agonist | L-glutamic acid | small-molecule | No | No | Cannone G, Berto L, Malhaire F, Ferguson G, Fouillen A, Balor S, Font-Ingles J, Llebaria A, Goudet C, Kotecha A, K R V, Lebon G | 10.1038/S41467-024-55439-9 | 2024-11-06 | Yes | |
| GRM5 | mGlu5 | Metabotropic glutamate | C | Human | Cryo-EM | 8X0F | - | 3.3 | A | Active | - | 63 | - | - | - | - | - | - |
quisqualate
VU-29 |
small-molecule small-molecule |
Agonist PAM |
L-glutamic acid | small-molecule | No | No | Cannone G, Berto L, Malhaire F, Ferguson G, Fouillen A, Balor S, Font-Ingles J, Llebaria A, Goudet C, Kotecha A, K R V, Lebon G | 10.1038/S41467-024-55439-9 | 2024-11-06 | Yes | |
| GRM5 | mGlu5 | Metabotropic glutamate | C | Human | Cryo-EM | 8X0E | - | 3.4 | A | Active | - | 63 | - | - | - | - | - | - |
quisqualate
|
small-molecule | Agonist | L-glutamic acid | small-molecule | No | No | Cannone G, Berto L, Malhaire F, Ferguson G, Fouillen A, Balor S, Font-Ingles J, Llebaria A, Goudet C, Kotecha A, K R V, Lebon G | 10.1038/S41467-024-55439-9 | 2024-11-06 | Yes | |
| MRGX4 | MRGPRX4 | A orphans | A | Human | Cryo-EM | 8KEX | - | 3.2 | E | Active | 98 | 79 | - | - | - | - | BRIL | - |
DCA-3P
|
small-molecule | Agonist | - | - | No | No | Yang J, Zhao T, Fan J, Zou H, Lan G, Guo F, Shi Y, Ke H, Yu H, Yue Z, Wang X, Bai Y, Li S, Liu Y, Wang X, Chen Y, Li Y, Lei X | 10.1016/J.CELL.2024.10.001 | 2024-11-06 | Yes | |
| MRGX4 | MRGPRX4 | A orphans | A | Human | Cryo-EM | 8K4S | 8K4S_refined | 2.9 | E | Active | 100 | 79 | Gq/11 | αq | Gq-Gs chimera | 57 | BRIL | scFv16 |
DCA-3P
|
small-molecule | Agonist | - | - | No | No | Yang J, Zhao T, Fan J, Zou H, Lan G, Guo F, Shi Y, Ke H, Yu H, Yue Z, Wang X, Bai Y, Li S, Liu Y, Wang X, Chen Y, Li Y, Lei X | 10.1016/J.CELL.2024.10.001 | 2024-11-06 | Yes | |
| B1B1U5 | Rhodopsin | Opsins | A | Hasarius adansoni | Cryo-EM | 9EPR | - | 4.9 | R | Active | 100 | 89 | Gi/o | αi1 | - | 60 | - | - |
Retinal (11-cis)
|
small-molecule | Agonist | - | - | No | No | Tejero O, Pamula F, Koyanagi M, Nagata T, Afanasyev P, Das I, Deupi X, Sheves M, Terakita A, Schertler GFX, Rodrigues MJ, Tsai CJ | 10.1038/S41467-024-53208-2 | 2024-10-30 | Yes | |
| GP119 | GPR119 | GPR18, GPR55 and GPR119 | A | Human | Cryo-EM | 8VHF | 8VHF_refined | 3.5 | R | Active | 100 | 88 | Gs | αs | - | 60 | BRIL | Nanobody-35 |
MBX-2982
|
small-molecule | Agonist | N-palmitoylethanolamine, anandamide, N-oleoylethanolamide, SEA | small-molecule | No | No | - | - | 2024-10-30 | Yes | |
| GRM2 | mGlu2 | Metabotropic glutamate | C | Human | Cryo-EM | 8WGB | - | 3.7 | B | Active | - | 83 | Gi/o | αi3 | - | 63 | - | - |
VU0155041
|
small-molecule | Agonist | L-glutamic acid | small-molecule | No | No | Huang W, Jin N, Guo J, Shen C, Xu C, Xi K, Bonhomme L, Quast RB, Shen DD, Qin J, Liu YR, Song Y, Gao Y, Margeat E, Rondard P, Pin JP, Zhang Y, Liu J | 10.1038/S41467-024-54744-7 | 2024-10-30 | Yes | |
| KISSR | kisspeptin | Kisspeptin | A | Human | Cryo-EM | 8XGS | - | 3.0 | A | Active | 100 | 74 | Gq/11 | αq | - | 64 | - | scFv16 |
Kisspeptin-10
|
peptide | Agonist | kisspeptin-13, kisspeptin-14, kisspeptin-54, kisspeptin-52, kisspeptin-10 | peptide | No | No | Wu Z, Chen G, Qiu C, Yan X, Xu L, Jiang S, Xu J, Han R, Shi T, Liu Y, Gao W, Wang Q, Li J, Ye F, Pan X, Zhang Z, Ning P, Zhang B, Chen J, Du Y | 10.1126/SCIADV.ADN7771 | 2024-10-30 | Yes | |
| KISSR | kisspeptin | Kisspeptin | A | Human | Cryo-EM | 8XGO | - | 2.7 | A | Active | 100 | 75 | Gq/11 | αq | - | 64 | - | scFv16 |
TAK448
|
peptide | Agonist | kisspeptin-13, kisspeptin-14, kisspeptin-54, kisspeptin-52, kisspeptin-10 | peptide | No | No | Wu Z, Chen G, Qiu C, Yan X, Xu L, Jiang S, Xu J, Han R, Shi T, Liu Y, Gao W, Wang Q, Li J, Ye F, Pan X, Zhang Z, Ning P, Zhang B, Chen J, Du Y | 10.1126/SCIADV.ADN7771 | 2024-10-30 | Yes | |
| KISSR | kisspeptin | Kisspeptin | A | Human | Cryo-EM | 8XGU | - | 3.0 | A | Active | 100 | 72 | Gi/o | αi1 | - | 60 | - | scFv16 |
ACY-DTY-HYP-ASN-THR-PHE-XZA-LEU-NMM-TRP-NH2
|
peptide | Agonist | kisspeptin-13, kisspeptin-14, kisspeptin-54, kisspeptin-52, kisspeptin-10 | peptide | No | No | Wu Z, Chen G, Qiu C, Yan X, Xu L, Jiang S, Xu J, Han R, Shi T, Liu Y, Gao W, Wang Q, Li J, Ye F, Pan X, Zhang Z, Ning P, Zhang B, Chen J, Du Y | 10.1126/SCIADV.ADN7771 | 2024-10-30 | Yes | |
| LGR4 | LGR4 | A orphans | A | Human | Cryo-EM | 8WVW | - | 3.5 | A | Inactive | 8 | 76 | - | - | - | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | R-spondin-2, R-spondin-1, R-spondin-4, R-spondin-3 | peptide | No | No | - | - | 2024-10-30 | Yes | |
| LGR4 | LGR4 | A orphans | A | Human | Cryo-EM | 8WVU | - | 3.6 | A | Inactive | 8 | 77 | - | - | - | - | - | - |
R-spondin-1
|
protein | Agonist | R-spondin-2, R-spondin-1, R-spondin-4, R-spondin-3 | peptide | No | No | - | - | 2024-10-30 | Yes | |
| LGR4 | LGR4 | A orphans | A | Human | Cryo-EM | 8WVV | - | 3.4 | A | Inactive | 8 | 75 | - | - | - | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | R-spondin-2, R-spondin-1, R-spondin-4, R-spondin-3 | peptide | No | No | - | - | 2024-10-30 | Yes | |
| LGR4 | LGR4 | A orphans | A | Human | Cryo-EM | 8WVX | - | 3.3 | A | Inactive | 8 | 76 | - | - | - | - | - | - |
Norrin
|
peptide | Agonist | R-spondin-2, R-spondin-1, R-spondin-4, R-spondin-3 | peptide | No | No | - | - | 2024-10-30 | Yes | |
| LGR4 | LGR4 | A orphans | A | Human | Cryo-EM | 8WVY | - | 3.3 | A | Inactive | 8 | 77 | - | - | - | - | - | - |
Norrin
|
peptide | Agonist | R-spondin-2, R-spondin-1, R-spondin-4, R-spondin-3 | peptide | No | No | - | - | 2024-10-30 | Yes | |
| O51G2 | OR51G2 | Odorant family 51 | O1 | Human | Cryo-EM | 8UXV | - | 3.2 | A | Active | - | 96 | Gs | αs | Mini-Gs | 56 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | de March CA, Ma N, Billesbolle CB, Tewari J, Llinas Del Torrent C, van der Velden WJC, Ojiro I, Takayama I, Faust B, Li L, Vaidehi N, Manglik A, Matsunami H | 10.1038/S41586-024-08126-0 | 2024-10-30 | Yes | |
| OR1F1 | OR1F1 | Odorant family 1 | O2 | Human | Cryo-EM | 8UXY | - | 3.3 | A | Active | - | 94 | Gs | αs | Mini-Gs | 56 | - | Nanobody-35 |
l-Menthol
|
small-molecule | Agonist | - | - | No | No | de March CA, Ma N, Billesbolle CB, Tewari J, Llinas Del Torrent C, van der Velden WJC, Ojiro I, Takayama I, Faust B, Li L, Vaidehi N, Manglik A, Matsunami H | 10.1038/S41586-024-08126-0 | 2024-10-30 | Yes | |
| OR2T2 | OR2T2 | Odorant family 2 | O2 | Human | Cryo-EM | 8UY0 | - | 3.2 | A | Active | - | 89 | Gs | αs | Mini-Gs | 55 | - | Nanobody-35 |
(5S)-2-methyl-5-(prop-1-en-2-yl)cyclohex-2-en-1-one
|
small-molecule | Agonist | - | - | No | No | de March CA, Ma N, Billesbolle CB, Tewari J, Llinas Del Torrent C, van der Velden WJC, Ojiro I, Takayama I, Faust B, Li L, Vaidehi N, Manglik A, Matsunami H | 10.1038/S41586-024-08126-0 | 2024-10-30 | Yes | |
| OR4D5 | OR4D5 | Odorant family 4 | O2 | Human | Cryo-EM | 8UYQ | - | 3.5 | A | Active | - | 93 | Gs | αs | Mini-Gs | 55 | - | Nanobody-35 |
(2R)-2-methyl-1,3-thiazolidine
|
small-molecule | Agonist | - | - | No | No | de March CA, Ma N, Billesbolle CB, Tewari J, Llinas Del Torrent C, van der Velden WJC, Ojiro I, Takayama I, Faust B, Li L, Vaidehi N, Manglik A, Matsunami H | 10.1038/S41586-024-08126-0 | 2024-10-30 | Yes | |
| B1B1U5 | Rhodopsin | Opsins | A | Hasarius adansoni | Cryo-EM | 9EPQ | - | 4.2 | R | Active | 100 | 86 | Gi/o | αi1 | - | 65 | - | - |
11,20-Ethanoretinal
|
small-molecule | Agonist | - | - | No | No | - | - | 2024-10-23 | Yes | |
| B1B1U5 | Rhodopsin | Opsins | A | Hasarius adansoni | Cryo-EM | 9EPP | - | 4.1 | R | Active | 100 | 87 | Gi/o | αi1 | - | 63 | - | - |
11,20-Ethanoretinal
|
small-molecule | Agonist | - | - | No | No | - | - | 2024-10-23 | Yes | |
| HRH3 | H3 | Histamine | A | Human | Cryo-EM | 8YN7 | - | 2.8 | R | Active | 100 | 64 | Gi/o | αo | Mini-Go | 61 | - | scFv16 |
[(2R)-3-[(E)-hexadec-9-enoyl]oxy-2-octadecanoyloxypropyl] 2-(trimethylazaniumyl)ethyl phosphate
|
lipid | Agonist | histamine | small-molecule | No | No | - | - | 2024-10-16 | Yes | |
| HRH3 | H3 | Histamine | A | Human | Cryo-EM | 8YN8 | - | 2.8 | R | Active | 100 | 64 | Gi/o | αo | Mini-Go | 61 | - | scFv16 |
proxyfan
|
small-molecule | Agonist | histamine | small-molecule | No | No | - | - | 2024-10-16 | Yes | |
| PTH1R | PTH1 | Parathyroid hormone | B1 | Human | Cryo-EM | 9JR3 | - | 2.8 | R | Active | 100 | 60 | Gq/11 | αq | Mini-Gq | 57 | - | scFv16 |
Parathyroid hormone
|
peptide | Agonist | PTHrP-(1-36), PTHrP, PTH, TIP39 | peptide | No | No | - | - | 2024-10-16 | Yes | |
| PTH1R | PTH1 | Parathyroid hormone | B1 | Human | Cryo-EM | 9JR2 | - | 2.8 | R | Active | 100 | 59 | Gq/11 | αq | Mini-Gq | 57 | - | scFv16 |
Parathyroid hormone
|
peptide | Agonist | PTHrP-(1-36), PTHrP, PTH, TIP39 | peptide | No | No | - | - | 2024-10-16 | Yes | |
| TAAR1 | TA1 | Trace amine | A | Human | Cryo-EM | 9JKQ | 9JKQ_refined | 2.7 | R | Active | 100 | 87 | Gs | αs | - | 60 | BRIL | Nanobody-35 |
METHAMPHETAMINE
|
small-molecule | Agonist | 3-iodothyronamine, dopamine, CHEMBL1160703, (+)-Octopamine, tyramine, octopamine, β-phenylethylamine | small-molecule | No | No | Lin Y, Wang J, Shi F, Yang L, Wu S, Qiao A, Ye S | 10.1021/ACS.JMEDCHEM.4C01961 | 2024-10-16 | Yes | |
| GPBAR | GPBA | Bile acid | A | Human | Cryo-EM | 9GYO | - | 2.5 | R | Active | 100 | 83 | Gs | αs | Mini-Gs | 59 | BRIL | Nanobody-35 |
CHEMBL2331646
|
small-molecule | Agonist | chenodeoxycholic acid, deoxycholic acid, lithocholic acid, cholic acid | small-molecule | No | No | - | - | 2024-10-09 | Yes | |
| HRH1 | H1 | Histamine | A | Human | Cryo-EM | 8YN2 | - | 2.7 | R | Active | 100 | 56 | Gq/11 | αq | Mini-Gq | 64 | - | scFv16 |
histamine
|
small-molecule | Agonist | histamine | small-molecule | No | No | Zhang X, Liu G, Zhong YN, Zhang R, Yang CC, Niu C, Pu X, Sun J, Zhang T, Yang L, Zhang C, Li X, Shen X, Xiao P, Sun JP, Gong W | 10.1038/S41467-024-52585-Y | 2024-10-09 | Yes | |
| HRH2 | H2 | Histamine | A | Human | Cryo-EM | 8YN4 | - | 3.0 | R | Active | 100 | 75 | Gq/11 | αq | Mini-Gq | 64 | - | scFv16 |
histamine
|
small-molecule | Agonist | histamine | small-molecule | No | No | Zhang X, Liu G, Zhong YN, Zhang R, Yang CC, Niu C, Pu X, Sun J, Zhang T, Yang L, Zhang C, Li X, Shen X, Xiao P, Sun JP, Gong W | 10.1038/S41467-024-52585-Y | 2024-10-09 | Yes | |
| HRH2 | H2 | Histamine | A | Human | Cryo-EM | 8YN3 | - | 2.6 | R | Active | 100 | 78 | Gs | αs | Mini-Gq | 60 | - | Nanobody-35 |
histamine
|
small-molecule | Agonist | histamine | small-molecule | No | No | Zhang X, Liu G, Zhong YN, Zhang R, Yang CC, Niu C, Pu X, Sun J, Zhang T, Yang L, Zhang C, Li X, Shen X, Xiao P, Sun JP, Gong W | 10.1038/S41467-024-52585-Y | 2024-10-09 | Yes | |
| HRH3 | H3 | Histamine | A | Human | Cryo-EM | 8YN6 | - | 2.8 | R | Active | 100 | 65 | Gi/o | αi1 | - | 63 | - | scFv16 |
imetit
|
small-molecule | Agonist | histamine | small-molecule | No | No | Zhang X, Liu G, Zhong YN, Zhang R, Yang CC, Niu C, Pu X, Sun J, Zhang T, Yang L, Zhang C, Li X, Shen X, Xiao P, Sun JP, Gong W | 10.1038/S41467-024-52585-Y | 2024-10-09 | Yes | |
| HRH3 | H3 | Histamine | A | Human | Cryo-EM | 8YN5 | - | 2.7 | R | Active | 100 | 65 | Gi/o | αi1 | - | 63 | - | scFv16 |
histamine
|
small-molecule | Agonist | histamine | small-molecule | No | No | Zhang X, Liu G, Zhong YN, Zhang R, Yang CC, Niu C, Pu X, Sun J, Zhang T, Yang L, Zhang C, Li X, Shen X, Xiao P, Sun JP, Gong W | 10.1038/S41467-024-52585-Y | 2024-10-09 | Yes | |
| HRH4 | H4 | Histamine | A | Human | Cryo-EM | 8YN9 | - | 2.3 | R | Active | 100 | 71 | Gi/o | αi1 | - | 63 | - | scFv16 |
histamine
|
small-molecule | Agonist | histamine, CCL16 | small-molecule | No | No | Zhang X, Liu G, Zhong YN, Zhang R, Yang CC, Niu C, Pu X, Sun J, Zhang T, Yang L, Zhang C, Li X, Shen X, Xiao P, Sun JP, Gong W | 10.1038/S41467-024-52585-Y | 2024-10-09 | Yes | |
| HRH4 | H4 | Histamine | A | Human | Cryo-EM | 8YNA | - | 2.6 | R | Active | 100 | 71 | Gi/o | αi1 | - | 63 | - | scFv16 |
immepip
|
small-molecule | Agonist | histamine, CCL16 | small-molecule | No | No | - | - | 2024-10-09 | Yes | |
| CASR | CaS | Calcium-sensing | C | Human | Cryo-EM | 9C1P | - | 2.8 | A | Inactive | - | 72 | - | - | - | - | - | - |
(5R)-N-[2-(1,2-benzothiazol-3-yl)ethyl]-1-methyl-2,3,4,5-tetrahydro-1H-1-benzazepin-5-amine
|
small-molecule | PAM | spermine, Mg2+, L-tryptophan, Ca2+ | small-molecule | No | No | - | - | 2024-10-02 | Yes | |
| CASR | CaS | Calcium-sensing | C | Human | Cryo-EM | 9C2F | - | 2.8 | A | Inactive | - | 71 | - | - | - | - | - | - |
(1R)-1-(2H-1,3-benzodioxol-4-yl)-N-[2-(1,2-benzothiazol-3-yl)ethyl]ethan-1-amine
|
small-molecule | PAM | spermine, Mg2+, L-tryptophan, Ca2+ | small-molecule | No | No | - | - | 2024-10-02 | Yes | |
| EDNRB | ETB | Endothelin | A | Human | Cryo-EM | 8ZRT | - | 3.6 | R | Active | 83 | 64 | - | - | - | - | - | - |
ENDOTHELIN
|
protein | Agonist | endothelin-2, endothelin-3, endothelin-1 | peptide | No | No | Tani K, Maki-Yonekura S, Kanno R, Negami T, Hamaguchi T, Hall M, Mizoguchi A, Humbel BM, Terada T, Yonekura K, Doi T | 10.1038/S42003-024-06905-Z | 2024-10-02 | Yes | |
| EDNRB | ETB | Endothelin | A | Human | Cryo-EM | 8XWP | 8XWP_refined | 3.2 | R | Active | 100 | 68 | Gi/o | αi1 | - | 62 | - | scFv16 |
ENDOTHELIN
|
protein | Agonist | endothelin-2, endothelin-3, endothelin-1 | peptide | No | No | Tani K, Maki-Yonekura S, Kanno R, Negami T, Hamaguchi T, Hall M, Mizoguchi A, Humbel BM, Terada T, Yonekura K, Doi T | 10.1038/S42003-024-06905-Z | 2024-10-02 | Yes | |
Showing 1 to 100 of 1,716 entries
Pick reference from selection
Superpositions structures selected in the browser to the reference checked in this table
| PDB | UniProt | IUPHAR | Rec. family | Class | Species | State | PDB Date |
|---|