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RECEPTOR
| STRUCTURE
| SIGNAL PROTEIN
| AUXILIARY PROTEIN
| STRUCTURE LIGAND
| PHYSIOLOGICAL LIGAND
| SODIUM ION SITE
| REFERENCE
| ANNOTATED
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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 | |||||
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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 | - | 87 | 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 | 8XGU | - | 3.0 | A | Active | 100 | 72 | Gi/o | αi1 | - | 60 | - | scFv16 |
TAK448
|
peptide | Agonist | kisspeptin-10, kisspeptin-54, kisspeptin-52, kisspeptin-14, kisspeptin-13 | 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-10, kisspeptin-54, kisspeptin-52, kisspeptin-14, kisspeptin-13 | 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 | 8XGS | - | 3.0 | A | Active | 100 | 74 | Gq/11 | αq | - | 64 | - | scFv16 |
Kisspeptin-10
|
peptide | Agonist | kisspeptin-10, kisspeptin-54, kisspeptin-52, kisspeptin-14, kisspeptin-13 | 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 | 8WVU | - | 3.6 | A | Inactive | 2 | 77 | - | - | - | - | - | - |
R-spondin-1
|
protein | Agonist | R-spondin-2, R-spondin-3, R-spondin-1, R-spondin-4 | peptide | No | No | - | - | 2024-10-30 | Yes | |
LGR4 | LGR4 | A orphans | A | Human | Cryo-EM | 8WVX | - | 3.3 | A | Inactive | 33 | 76 | - | - | - | - | - | - |
Norrin
|
peptide | Agonist | R-spondin-2, R-spondin-3, R-spondin-1, R-spondin-4 | peptide | No | No | - | - | 2024-10-30 | Yes | |
LGR4 | LGR4 | A orphans | A | Human | Cryo-EM | 8WVV | - | 3.4 | A | Inactive | 2 | 75 | - | - | - | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | R-spondin-2, R-spondin-3, R-spondin-1, R-spondin-4 | peptide | No | No | - | - | 2024-10-30 | Yes | |
LGR4 | LGR4 | A orphans | A | Human | Cryo-EM | 8WVW | - | 3.5 | A | Inactive | 2 | 76 | - | - | - | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | R-spondin-2, R-spondin-3, R-spondin-1, R-spondin-4 | peptide | No | No | - | - | 2024-10-30 | Yes | |
LGR4 | LGR4 | A orphans | A | Human | Cryo-EM | 8WVY | - | 3.3 | A | Inactive | 2 | 77 | - | - | - | - | - | - |
Norrin
|
peptide | Agonist | R-spondin-2, R-spondin-3, R-spondin-1, R-spondin-4 | 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 | 9EPP | - | 4.1 | R | Active | 100 | 87 | Gi/o | αi1 | - | 63 | - | - |
11,20-Ethanoretinal
|
small-molecule | Agonist | - | - | No | No | - | - | 2024-10-23 | 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 | |
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 | |
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 | |
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 | |
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 | |
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 | octopamine, β-phenylethylamine, CHEMBL1160703, tyramine, (+)-Octopamine, 3-iodothyronamine, dopamine | 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 | cholic acid, deoxycholic acid, chenodeoxycholic acid, lithocholic 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 | 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 | |
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 | |
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 | 8YNA | - | 2.6 | R | Active | 100 | 71 | Gi/o | αi1 | - | 63 | - | scFv16 |
immepip
|
small-molecule | Agonist | CCL16, histamine | small-molecule | No | No | - | - | 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 | CCL16, 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 | |
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 | Ca2+, spermine, Mg2+, L-tryptophan | small-molecule | No | No | - | - | 2024-10-02 | 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 | Ca2+, spermine, Mg2+, L-tryptophan | small-molecule | No | No | - | - | 2024-10-02 | Yes | |
EDNRB | ETB | Endothelin | A | Human | Cryo-EM | 8ZRT | - | 3.6 | R | Active | 82 | 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 | 8XWQ | - | 4.6 | 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 | |
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 | |
FZD7 | FZD7 | Frizzled | F | Human | Cryo-EM | 9EPO | - | 1.9 | D | Inactive | 19 | 60 | - | - | - | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | - | - | 2024-10-02 | Yes | |
FZD7 | FZD7 | Frizzled | F | Human | Cryo-EM | 9EW2 | - | 3.2 | R | Active | 100 | 59 | Gs | αs | - | 59 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | - | - | 2024-10-02 | Yes | |
HCAR2 | HCA2 | Hydroxycarboxylic acid | A | Human | Cryo-EM | 9IQT | 9IQT_refined | 2.9 | R | Active | 100 | 80 | Gi/o | αi1 | - | 64 | - | scFv16 |
nicotinic acid
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | No | No | Liu Y, Zhou Z, Guan F, Han Z, Zhu C, Ye S, Yu X, Qiao A | 10.1016/J.JMB.2024.168795 | 2024-10-02 | Yes | |
P2RY1 | P2Y1 | P2Y | A | Human | Cryo-EM | 8WJX | - | 3.2 | R | Active | 100 | 80 | Gs | αs | - | 61 | BRIL | Nanobody-35 |
ADP
|
small-molecule | Agonist | ATP, ADP | small-molecule | No | No | - | - | 2024-10-02 | Yes | |
MC4R | MC4 | Melanocortin | A | Human | Cryo-EM | 8QJ2 | 8QJ2_refined | 3.4 | A | Active | 100 | 74 | Gs | αs | - | 56 | - | Nanobody-35 |
pN162
|
protein | Apo (no ligand) | γ-MSH, agouti-related protein, β-MSH, α-MSH, ACTH | peptide | No | No | - | - | 2024-09-25 | Yes | |
PRLHR | PrRP | Prolactin-releasing peptide | A | Human | Cryo-EM | 8ZPS | 8ZPS_refined | 3.0 | R | Active | 100 | 78 | Gi/o | αi1 | - | 57 | - | scFv16 |
Prolactin-releasing peptide PrRP20
|
peptide | Agonist | PrRP-20, neuropeptide Y, PrRP-31, PTHrP | peptide | No | No | Li Y, Yuan Q, He X, Zhang Y, You C, Wu C, Li J, Xu HE, Zhao LH | 10.1038/S41421-024-00724-6 | 2024-09-25 | Yes | |
PRLHR | PrRP | Prolactin-releasing peptide | A | Human | Cryo-EM | 8ZPT | 8ZPT_refined | 3.0 | R | Active | 100 | 79 | Gq/11 | αq | - | 59 | - | scFv16 |
Prolactin-releasing peptide PrRP20
|
peptide | Agonist | PrRP-20, neuropeptide Y, PrRP-31, PTHrP | peptide | No | No | Li Y, Yuan Q, He X, Zhang Y, You C, Wu C, Li J, Xu HE, Zhao LH | 10.1038/S41421-024-00724-6 | 2024-09-25 | Yes | |
DRD3 | D3 | Dopamine | A | Human | Cryo-EM | 9F33 | - | 3.1 | R | Active | 100 | 68 | Gi/o | αo | - | 61 | - | scFv16 |
CHEMBL4551160
|
small-molecule | Agonist | dopamine | small-molecule | No | No | - | - | 2024-09-18 | Yes | |
DRD3 | D3 | Dopamine | A | Human | Cryo-EM | 9F34 | - | 3.1 | R | Active | 100 | 68 | Gi/o | αo | - | 61 | - | scFv16 |
CHEMBL4551160
|
small-molecule | Agonist | dopamine | small-molecule | No | No | - | - | 2024-09-18 | Yes | |
GIPR | GIP | Glucagon | B1 | Human | Cryo-EM | 8YW4 | 8YW4_refined | 3.3 | R | Active | 100 | 63 | Gs | αs | - | 60 | - | Nanobody-35 |
Retatrutide
|
peptide | Agonist | gastric inhibitory polypeptide | peptide | No | No | Li W, Zhou Q, Cong Z, Yuan Q, Li W, Zhao F, Xu HE, Zhao LH, Yang D, Wang MW | 10.1038/S41421-024-00700-0 | 2024-09-18 | Yes | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 8YW3 | 8YW3_refined | 2.7 | R | Active | 100 | 83 | Gs | αs | - | 57 | - | Nanobody-35 |
Retatrutide
|
peptide | Agonist | glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide | peptide | No | No | Li W, Zhou Q, Cong Z, Yuan Q, Li W, Zhao F, Xu HE, Zhao LH, Yang D, Wang MW | 10.1038/S41421-024-00700-0 | 2024-09-18 | Yes | |
GP179 | GPR179 | C Orphans | C | Human | Cryo-EM | 8IRJ | - | 3.5 | A | Inactive | - | 22 | - | - | - | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | - | - | 2024-09-18 | Yes | |
PAR1 | PAR1 | Proteinase-activated | A | Human | Cryo-EM | 8XOR | 8XOR_refined | 3.0 | R | Active | 100 | 70 | Gq/11 | αq | - | 60 | - | scFv16 |
Tethered agonist
|
peptide | Agonist | thrombin | peptide | No | No | - | - | 2024-09-18 | Yes | |
PAR1 | PAR1 | Proteinase-activated | A | Human | Cryo-EM | 8XOS | - | 3.2 | R | Active | 100 | 68 | Gi/o | αi1 | - | 61 | - | scFv16 |
Tethered agonist
|
peptide | Agonist | thrombin | peptide | No | No | - | - | 2024-09-18 | Yes | |
ADA2A | α2A | Adrenoceptors | A | Human | Cryo-EM | 9CBM | - | 3.2 | R | Active | 100 | 55 | Gi/o | αi1 | - | 60 | T4-Lysozyme | - |
dexmedetomidine
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline | small-molecule | No | No | Lou JS, Su M, Wang J, Do HN, Miao Y, Huang XY | 10.1038/S12276-024-01296-X | 2024-09-11 | Yes | |
ADA2A | α2A | Adrenoceptors | A | Human | Cryo-EM | 9CBL | - | 2.8 | R | Active | 100 | 55 | Gi/o | αi1 | - | 60 | T4-Lysozyme | - |
(-)-adrenaline
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline | small-molecule | No | No | Lou JS, Su M, Wang J, Do HN, Miao Y, Huang XY | 10.1038/S12276-024-01296-X | 2024-09-11 | Yes | |
BRS3 | BB3 | Bombesin | A | Human | Cryo-EM | 8Y52 | 8Y52_refined | 2.9 | R | Active | 100 | 75 | Gq/11 | αq | - | 60 | - | - |
Bombesin
|
peptide | Agonist | - | - | No | No | Li C, Xu Y, Su W, He X, Li J, Li X, Xu HE, Yin W | 10.1016/J.CELREP.2024.114511 | 2024-09-11 | Yes | |
BRS3 | BB3 | Bombesin | A | Human | Cryo-EM | 8Y53 | 8Y53_refined | 2.9 | R | Active | 100 | 75 | Gq/11 | αq | - | 60 | - | scFv16 Nanobody-35 |
MK-5046
|
small-molecule | Agonist | - | - | No | No | - | - | 2024-09-11 | Yes | |
CCR6 | CCR6 | Chemokine | A | Human | Cryo-EM | 9D3G | - | 3.3 | A | Inactive | 6 | 72 | - | - | - | - | BRIL | Fab heavy chain Fab light chain anti-BRIL Fab Nanobody |
1-(4-chlorophenyl)-N-[[(2R)-4-(2,3-dihydro-1H-inden-2-yl)-5-oxomorpholin-2-yl]methyl]cyclopropane-1-carboxamide
4-[[3,4-Dioxo-2-[[(1R)-1-(4-propan-2-ylfuran-2-yl)propyl]amino]cyclobuten-1-yl]amino]-3-hydroxy-N,N-dimethylpyridine-2-carboxamide |
small-molecule small-molecule |
Antagonist NAM |
CCL20, beta-defensin 4A | peptide | No | No | - | - | 2024-09-11 | Yes | |
CCR6 | CCR6 | Chemokine | A | Human | Cryo-EM | 9D3E | - | 3.0 | A | Inactive | 6 | 66 | - | - | - | - | BRIL | anti-BRIL Fab heavy chain anti-BRIL Fab Nanobody anti-BRIL Fab light chain |
4-[[3,4-Dioxo-2-[[(1R)-1-(4-propan-2-ylfuran-2-yl)propyl]amino]cyclobuten-1-yl]amino]-3-hydroxy-N,N-dimethylpyridine-2-carboxamide
OXM2 |
small-molecule small-molecule |
Allosteric antagonist | CCL20, beta-defensin 4A | peptide | No | No | - | - | 2024-09-11 | Yes | |
FZD4 | FZD4 | Frizzled | F | Human | Cryo-EM | 8WMA | - | 3.5 | A | Active | 78 | 60 | - | - | - | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Qian Y, Ma Z, Xu Z, Duan Y, Xiong Y, Xia R, Zhu X, Zhang Z, Tian X, Yin H, Liu J, Song J, Lu Y, Zhang A, Guo C, Jin L, Kim WJ, Ke J, Xu F, Huang Z, He Y | 10.1038/S41467-024-52174-Z | 2024-09-11 | Yes | |
FZD4 | FZD4 | Frizzled | F | Human | Cryo-EM | 8WM9 | - | 3.5 | A | Active | 78 | 60 | - | - | - | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Qian Y, Ma Z, Xu Z, Duan Y, Xiong Y, Xia R, Zhu X, Zhang Z, Tian X, Yin H, Liu J, Song J, Lu Y, Zhang A, Guo C, Jin L, Kim WJ, Ke J, Xu F, Huang Z, He Y | 10.1038/S41467-024-52174-Z | 2024-09-11 | Yes | |
GPC5D | GPRC5D | C Orphans | C | Human | Cryo-EM | 9IMA | - | 2.7 | A | Inactive | - | 72 | - | - | - | - | - | - |
Talquetamab Fab heavy chain
Talquetamab Fab light chain |
protein protein |
Antagonist | - | - | No | No | Jeong J, Park J, Young Mo G, Shin J, Cho Y | 10.1016/J.JMB.2024.168748 | 2024-09-11 | Yes | |
OPRM | μ | Opioid | A | Mouse | Cryo-EM | 9BQJ | - | 3.3 | D | Active | 100 | 71 | Gi/o | αi1 | - | 61 | - | scFv16 |
N-[[3-(hydroxymethyl)phenyl]methyl]-N-[1-(2-phenylethyl)piperidin-4-yl]propanamide
|
small-molecule | Agonist | - | - | No | No | - | - | 2024-09-11 | Yes | |
SUCR1 | succinate | Succinate | A | Human | Cryo-EM | 8WOG | - | 3.0 | A | Active | 100 | 93 | Gi/o | αi1 | - | 64 | - | - |
succinic acid
|
small-molecule | Agonist | succinic acid | small-molecule | No | No | Liu A, Liu Y, Zhang W, Ye RD | 10.1016/J.CELREP.2024.114381 | 2024-09-11 | Yes | |
SUCR1 | succinate | Succinate | A | Human | Cryo-EM | 8WP1 | - | 3.2 | A | Active | 100 | 91 | Gi/o | αi1 | - | 64 | - | - |
cis-epoxysuccinic acid
|
small-molecule | Agonist | succinic acid | small-molecule | No | No | Liu A, Liu Y, Zhang W, Ye RD | 10.1016/J.CELREP.2024.114381 | 2024-09-11 | Yes | |
DRD1 | D1 | Dopamine | A | Human | Cryo-EM | 8JXS | - | 3.0 | A | Active | 99 | 61 | - | - | - | - | - | Nanobody-3 Fab 8D3 heavy chain Fab 8D3 light chain |
CHEMBL4277264
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, (-)-noradrenaline, 5-hydroxytryptamine, dopamine | small-molecule | No | No | Fan L, Zhuang Y, Wu H, Li H, Xu Y, Wang Y, He L, Wang S, Chen Z, Cheng J, Xu HE, Wang S | 10.1016/J.NEURON.2024.07.003 | 2024-09-04 | Yes | |
DRD1 | D1 | Dopamine | A | Human | Cryo-EM | 8JXR | - | 3.6 | A | Active | 99 | 61 | - | - | - | - | - | Nanobody-3 Fab 8D3 heavy chain Fab 8D3 light chain |
Lysergide
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, (-)-noradrenaline, 5-hydroxytryptamine, dopamine | small-molecule | No | No | Fan L, Zhuang Y, Wu H, Li H, Xu Y, Wang Y, He L, Wang S, Chen Z, Cheng J, Xu HE, Wang S | 10.1016/J.NEURON.2024.07.003 | 2024-09-04 | Yes | |
FZD3 | FZD3 | Frizzled | F | Human | Cryo-EM | 8QW4 | - | 2.9 | A | Active | 99 | 48 | - | - | - | - | - | Nanobody-9 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Hillier J, Zhao Y, Carrique L, Malinauskas T, Ruza RR, Chang TH, Yi G, Duyvesteyn HME, Yu J, Lu W, Pardon E, Steyaert J, Zhu Y, Ni T, Jones EY | 10.1038/S41467-024-51451-1 | 2024-09-04 | Yes | |
5HT2A | 5-HT2A | 5-Hydroxytryptamine | A | Human | X-ray | 8ZMG | - | 3.4 | A | Inactive | 1 | 59 | - | - | - | - | BRIL | - |
pimavanserin
|
small-molecule | Inverse agonist | 5-hydroxytryptamine, tryptamine | small-molecule | No | No | - | - | 2024-08-28 | Yes | |
5HT2C | 5-HT2C | 5-Hydroxytryptamine | A | Human | X-ray | 8ZMF | - | 3.6 | A | Inactive | 1 | 62 | - | - | - | - | BRIL | - |
1-[(4-Fluorophenyl)methyl]-1-(5-methyl-5-azaspiro[2.5]octan-8-yl)-3-[[4-(2-methylpropoxy)phenyl]methyl]urea
|
small-molecule | Inverse agonist | 5-hydroxytryptamine | small-molecule | No | No | - | - | 2024-08-28 | Yes | |
EDNRA | ETA | Endothelin | A | Human | Cryo-EM | 8XVJ | - | 3.3 | R | Inactive | 10 | 68 | - | - | - | - | BRIL | Fab heavy chain Fab light chain anti-Fab Nanobody |
macitentan
|
small-molecule | Antagonist | endothelin-2, endothelin-3, endothelin-1 | peptide | No | No | - | - | 2024-08-28 | Yes | |
EDNRA | ETA | Endothelin | A | Human | Cryo-EM | 8XVI | 8XVI_refined | 3.3 | R | Active | 100 | 72 | Gs | αs | - | 59 | - | Nanobody-35 |
ENDOTHELIN
|
protein | Agonist | endothelin-2, endothelin-3, endothelin-1 | peptide | No | No | Hou J, Liu S, Zhang X, Tu G, Wu L, Zhang Y, Yang H, Li X, Liu J, Jiang L, Tan Q, Bai F, Liu Z, Miao C, Hua T, Luo Z | 10.1038/S41421-024-00705-9 | 2024-08-28 | Yes | |
EDNRA | ETA | Endothelin | A | Human | Cryo-EM | 8XVK | - | 3.2 | R | Inactive | 10 | 67 | - | - | - | - | BRIL | Fab heavy chain Fab light chain anti-Fab Nanobody |
ambrisentan
|
small-molecule | Antagonist | endothelin-2, endothelin-3, endothelin-1 | peptide | No | No | - | - | 2024-08-28 | Yes | |
EDNRA | ETA | Endothelin | A | Human | Cryo-EM | 8XVL | - | 3.2 | R | Inactive | 10 | 66 | - | - | - | - | BRIL | Fab heavy chain Fab light chain anti-Fab Nanobody |
zibotentan
|
small-molecule | Antagonist | endothelin-2, endothelin-3, endothelin-1 | peptide | No | No | - | - | 2024-08-28 | Yes | |
EDNRB | ETB | Endothelin | A | Human | Cryo-EM | 8XVE | 8XVE_refined | 3.0 | R | Active | 100 | 70 | Gs | αs | - | 59 | - | Nanobody-35 |
BQ3020
|
peptide | Agonist | endothelin-2, endothelin-3, endothelin-1 | peptide | No | No | Hou J, Liu S, Zhang X, Tu G, Wu L, Zhang Y, Yang H, Li X, Liu J, Jiang L, Tan Q, Bai F, Liu Z, Miao C, Hua T, Luo Z | 10.1038/S41421-024-00705-9 | 2024-08-28 | Yes | |
EDNRB | ETB | Endothelin | A | Human | Cryo-EM | 8XVH | 8XVH_refined | 3.3 | R | Active | 100 | 69 | Gs | αs | - | 59 | - | Nanobody-35 |
ENDOTHELIN
|
protein | Agonist | endothelin-2, endothelin-3, endothelin-1 | peptide | No | No | Hou J, Liu S, Zhang X, Tu G, Wu L, Zhang Y, Yang H, Li X, Liu J, Jiang L, Tan Q, Bai F, Liu Z, Miao C, Hua T, Luo Z | 10.1038/S41421-024-00705-9 | 2024-08-28 | Yes | |
ADRB3 | β3 | Adrenoceptors | A | Human | Cryo-EM | 9IJE | 9IJE_refined | 2.3 | R | Active | 100 | 62 | Gs | αs | - | 57 | - | scFv16 Camelid antibody VHH fragment |
(-)-adrenaline
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline, (±)-adrenaline, (+)-adrenaline | small-molecule | No | No | - | - | 2024-08-21 | Yes | |
ADRB3 | β3 | Adrenoceptors | A | Human | Cryo-EM | 9IJD | - | 2.8 | R | Active | 100 | 62 | Gs | αs | - | 57 | - | Camelid antibody VHH fragment |
Carazolol
|
small-molecule | Inverse agonist | (-)-noradrenaline, (-)-adrenaline, (±)-adrenaline, (+)-adrenaline | small-molecule | No | No | Zheng S, Zhang S, Dai S, Chen K, Gao K, Sun X, Lin B, Liu X | 10.1002/CPLU.202400288 | 2024-08-21 | Yes | |
CML2 | chemerin 2 | Chemerin receptor | A | Human | Cryo-EM | 8XGM | - | 3.3 | A | Active | 100 | 86 | Gi/o | αi1 | - | 66 | - | scFv16 |
Retinoic acid receptor responder protein 2
|
protein | Agonist | chemerin | peptide | No | No | - | - | 2024-08-21 | Yes | |
CML2 | chemerin 2 | Chemerin receptor | A | Human | Cryo-EM | 8JJP | - | 2.9 | A | Active | 100 | 82 | Gi/o | αi1 | - | 66 | - | scFv16 |
chemerin C-terminal peptide
|
peptide | Agonist | chemerin | peptide | No | No | - | - | 2024-08-21 | Yes | |
DRD2 | D2 | Dopamine | A | Human | Cryo-EM | 8TZQ | 8TZQ_refined | 3.2 | R | Active | 100 | 61 | Gi/o | αo | - | 62 | - | scFv16 |
dopamine
|
small-molecule | Agonist | dopamine | small-molecule | No | No | Knight KM, Krumm BE, Kapolka NJ, Ludlam WG, Cui M, Mani S, Prytkova I, Obarow EG, Lefevre TJ, Wei W, Ma N, Huang XP, Fay JF, Vaidehi N, Smrcka AV, Slesinger PA, Logothetis DE, Martemyanov KA, Roth BL, Dohlman HG | 10.1038/S41467-024-50964-Z | 2024-08-21 | Yes | |
DRD2 | D2 | Dopamine | A | Human | Cryo-EM | 8U02 | 8U02_refined | 3.3 | R | Active | 100 | 61 | Gi/o | αo | - | 97 | - | - |
dopamine
|
small-molecule | Agonist | dopamine | small-molecule | No | No | Knight KM, Krumm BE, Kapolka NJ, Ludlam WG, Cui M, Mani S, Prytkova I, Obarow EG, Lefevre TJ, Wei W, Ma N, Huang XP, Fay JF, Vaidehi N, Smrcka AV, Slesinger PA, Logothetis DE, Martemyanov KA, Roth BL, Dohlman HG | 10.1038/S41467-024-50964-Z | 2024-08-21 | Yes | |
E7FEL0 | GPR4 | A orphans | A | Zebrafish | Cryo-EM | 8ZFJ | - | 3.1 | R | Active | 100 | 72 | Gs | αs | - | 60 | BRIL | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | - | - | 2024-08-07 | Yes | |
GLR | glucagon | Glucagon | B1 | Human | Cryo-EM | 8YW5 | 8YW5_refined | 2.8 | R | Active | 100 | 79 | Gs | αs | - | 57 | - | Nanobody-35 |
Retatrutide
|
peptide | Agonist | glucagon | peptide | No | No | Li W, Zhou Q, Cong Z, Yuan Q, Li W, Zhao F, Xu HE, Zhao LH, Yang D, Wang MW | 10.1038/S41421-024-00700-0 | 2024-08-07 | Yes | |
MC4R | MC4 | Melanocortin | A | Human | X-ray | 8WKZ | - | 3.3 | A | Intermediate | 41 | 79 | - | - | - | - | GlgA glycogen synthase | - |
[N-(3-{bis[2-(pyridin-2-yl-kappaN)ethyl]amino-kappaN}propyl)-5-(2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanamide](azido)(hydroxy)copper
|
peptide | Antagonist | γ-MSH, agouti-related protein, β-MSH, α-MSH, ACTH | peptide | No | No | Gimenez LE, Martin C, Yu J, Hollanders C, Hernandez CC, Wu Y, Yao D, Han GW, Dahir NS, Wu L, Van der Poorten O, Lamouroux A, Mannes M, Zhao S, Tourwe D, Stevens RC, Cone RD, Ballet S | 10.1021/ACS.JMEDCHEM.3C01822 | 2024-08-07 | Yes | |
MC4R | MC4 | Melanocortin | A | Human | X-ray | 8WKY | - | 2.9 | A | Intermediate | 41 | 79 | - | - | - | - | GlgA glycogen synthase | - |
N-(2-aminoethyl)-5-(2-{[4-(morpholin-4-yl)pyridin-2-yl]amino}-1,3-thiazol-5-yl)pyridine-3-carboxamide
|
peptide | Antagonist | γ-MSH, agouti-related protein, β-MSH, α-MSH, ACTH | peptide | No | No | Gimenez LE, Martin C, Yu J, Hollanders C, Hernandez CC, Wu Y, Yao D, Han GW, Dahir NS, Wu L, Van der Poorten O, Lamouroux A, Mannes M, Zhao S, Tourwe D, Stevens RC, Cone RD, Ballet S | 10.1021/ACS.JMEDCHEM.3C01822 | 2024-08-07 | Yes | |
ACKR1 | ACKR1 | Chemokine | A | Human | Cryo-EM | 8JPS | - | 3.7 | A | Intermediate | 47 | 76 | - | - | - | - | - | - |
C-C motif chemokine 7
|
peptide | Agonist | CCL11, CCL14, CCL2, CXCL8, CXCL11, CCL5, CXCL6, CCL7, CXCL5, CCL17 | peptide | No | No | Saha S, Khanppnavar B, Maharana J, Kim H, Carino CMC, Daly C, Houston S, Sharma S, Zaidi N, Dalal A, Mishra S, Ganguly M, Tiwari D, Kumari P, Jhingan GD, Yadav PN, Plouffe B, Inoue A, Chung KY, Banerjee R, Korkhov VM, Shukla AK | 10.1016/J.CELL.2024.07.005 | 2024-07-31 | Yes | |
GRM3 | mGlu3 | Metabotropic glutamate | C | Human | Cryo-EM | 8TRD | - | 3.4 | A | Inactive | - | 84 | - | - | - | - | - | - |
LY341495
|
small-molecule | Antagonist | L-glutamic acid, NAAG | small-molecule | No | No | Strauss A, Gonzalez-Hernandez AJ, Lee J, Abreu N, Selvakumar P, Salas-Estrada L, Kristt M, Arefin A, Huynh K, Marx DC, Gilliland K, Melancon BJ, Filizola M, Meyerson J, Levitz J | 10.1038/S41467-024-50548-X | 2024-07-31 | Yes | |
GRM3 | mGlu3 | Metabotropic glutamate | C | Human | Cryo-EM | 8TQB | - | 3.3 | A | Active | - | 85 | - | - | - | - | - | - |
LY379268
|
small-molecule | Agonist | L-glutamic acid, NAAG | small-molecule | No | No | Strauss A, Gonzalez-Hernandez AJ, Lee J, Abreu N, Selvakumar P, Salas-Estrada L, Kristt M, Marx DC, Gilliland K, Melancon BJ, Filizola M, Meyerson J, Levitz J | 10.1101/2023.08.13.552748 | 2024-07-31 | Yes | |
GRM3 | mGlu3 | Metabotropic glutamate | C | Human | Cryo-EM | 8TR2 | - | 3.5 | A | Active | - | 85 | - | - | - | - | - | - |
(1S,4R,5R,6S)-4-amino-2-oxabicyclo[3.1.0]hexane-4,6-dicarboxylic acid
|
small-molecule | Agonist | L-glutamic acid, NAAG | small-molecule | No | No | Strauss A, Gonzalez-Hernandez AJ, Lee J, Abreu N, Selvakumar P, Salas-Estrada L, Kristt M, Marx DC, Gilliland K, Melancon BJ, Filizola M, Meyerson J, Levitz J | 10.1101/2023.08.13.552748 | 2024-07-31 | Yes | |
GRM3 | mGlu3 | Metabotropic glutamate | C | Human | Cryo-EM | 8TRC | - | 3.3 | A | Inactive | - | 84 | - | - | - | - | - | - |
LY341495
|
small-molecule | Antagonist | L-glutamic acid, NAAG | small-molecule | No | No | Strauss A, Gonzalez-Hernandez AJ, Lee J, Abreu N, Selvakumar P, Salas-Estrada L, Kristt M, Marx DC, Gilliland K, Melancon BJ, Filizola M, Meyerson J, Levitz J | 10.1101/2023.08.13.552748 | 2024-07-31 | Yes | |
GRM3 | mGlu3 | Metabotropic glutamate | C | Human | Cryo-EM | 8TR0 | - | 3.2 | A | Inactive | - | 85 | - | - | - | - | - | - |
LY341495
|
small-molecule | Antagonist | L-glutamic acid, NAAG | small-molecule | No | No | Strauss A, Gonzalez-Hernandez AJ, Lee J, Abreu N, Selvakumar P, Salas-Estrada L, Kristt M, Marx DC, Gilliland K, Melancon BJ, Filizola M, Meyerson J, Levitz J | 10.1101/2023.08.13.552748 | 2024-07-31 | Yes | |
NPY1R | Y1 | Neuropeptide Y | A | Human | Cryo-EM | 8K6O | 8K6O_refined | 3.3 | D | Active | 100 | 78 | Gi/o | αi2 | - | 63 | - | scFv16 |
neuropeptide Y
|
peptide | Agonist | peptide YY, pancreatic polypeptide, neuropeptide Y | peptide | No | No | - | - | 2024-07-31 | Yes | |
NPY1R | Y1 | Neuropeptide Y | A | Human | Cryo-EM | 8K6M | 8K6M_refined | 3.3 | D | Active | 100 | 78 | Gi/o | αi2 | - | 63 | - | scFv16 |
neuropeptide Y
|
peptide | Agonist | peptide YY, pancreatic polypeptide, neuropeptide Y | peptide | No | No | - | - | 2024-07-31 | Yes | |
NPY2R | Y2 | Neuropeptide Y | A | Human | Cryo-EM | 8K6N | 8K6N_refined | 3.2 | E | Active | 100 | 79 | Gi/o | αi2 | - | 63 | - | scFv16 |
neuropeptide Y
|
peptide | Agonist | peptide YY, PYY-(3-36), neuropeptide Y-(3-36), pancreatic polypeptide, neuropeptide Y | peptide | No | No | - | - | 2024-07-31 | Yes | |
P2Y10 | P2RY10 | A orphans | A | Human | Cryo-EM | 8KGG | - | 3.1 | R | Active | 100 | 86 | G12/13 | α13 | - | 56 | - | scFv16 |
(2~{S})-2-$l^{4}-azanyl-3-[[(2~{R})-3-octadecanoyloxy-2-oxidanyl-propoxy]-oxidanyl-oxidanylidene-$l^{6}-phosphanyl]oxy-propanoic acid
|
lipid | Agonist | LPA, sphingosine 1-phosphate, 1-O-Oleoyl-D-glycerol 3-phosphoric acid, LYSOPHOSPHATIDIC ACID | small-molecule | No | No | Yin H, Kamakura N, Qian Y, Tatsumi M, Ikuta T, Liang J, Xu Z, Xia R, Zhang A, Guo C, Inoue A, He Y | 10.1016/J.CHEMBIOL.2024.08.005 | 2024-07-31 | Yes | |
Q76SF8 | ORF74 | Unclassified | A | HHV-8 | Cryo-EM | 8K4O | - | 3.0 | E | Active | 100 | 97 | Gi/o | αi1 | - | 65 | - | - |
Growth-regulated alpha protein
|
protein | Agonist | - | - | No | No | - | - | 2024-07-24 | Yes | |
Q76SF8 | ORF74 | Unclassified | A | HHV-8 | Cryo-EM | 8K4P | - | 2.8 | A | Active | 100 | 86 | Gi/o | αi1 | - | 66 | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | - | - | 2024-07-24 | Yes | |
T2R14 | TAS2R14 | Taste 2 | T2 | Human | Cryo-EM | 9IJ9 | - | 2.7 | R | Active | 100 | 90 | Gi/o | αi1 | - | 62 | - | - |
Cholesterol
compound 28.1 [PMID: 36847646] |
small-molecule small-molecule |
Agonist Allosteric agonist |
- | - | No | No | - | - | 2024-07-24 | Yes | |
T2R14 | TAS2R14 | Taste 2 | T2 | Human | Cryo-EM | 9IJA | - | 3.1 | R | Inactive | 0 | 90 | - | - | - | - | - | - |
Cholesterol
compound 28.1 [PMID: 36847646] |
small-molecule small-molecule |
Agonist Allosteric agonist |
- | - | No | No | - | - | 2024-07-24 | Yes | |
T2R14 | TAS2R14 | Taste 2 | T2 | Human | Cryo-EM | 9IIX | - | 2.9 | R | Active | 100 | 90 | Gi/o | αgust | - | 64 | - | - |
compound 28.1 [PMID: 36847646]
compound 28.1 [PMID: 36847646] |
small-molecule small-molecule |
Agonist Allosteric agonist |
- | - | No | No | - | - | 2024-07-24 | Yes | |
T2R14 | TAS2R14 | Taste 2 | T2 | Human | Cryo-EM | 9IIW | - | 3.2 | R | Inactive | 0 | 90 | - | - | - | - | - | - |
compound 28.1 [PMID: 36847646]
compound 28.1 [PMID: 36847646] |
small-molecule small-molecule |
Agonist Allosteric agonist |
- | - | No | No | - | - | 2024-07-24 | Yes | |
TAAR1 | TA1 | Trace amine | A | Human | Cryo-EM | 8ZSJ | - | 2.8 | R | Active | 100 | 83 | Gs | αs | - | 58 | BRIL | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | octopamine, β-phenylethylamine, CHEMBL1160703, tyramine, (+)-Octopamine, 3-iodothyronamine, dopamine | small-molecule | No | No | Jiang K, Zheng Y, Zeng L, Wang L, Li F, Pu J, Lu Y, Zhao S, Xu F | 10.1016/J.CELREP.2024.114505 | 2024-07-24 | Yes | |
TAAR1 | TA1 | Trace amine | A | Human | Cryo-EM | 8ZSP | - | 3.1 | R | Active | 100 | 83 | Gs | αs | - | 58 | BRIL | Nanobody-35 |
Lysergide
|
small-molecule | Agonist | octopamine, β-phenylethylamine, CHEMBL1160703, tyramine, (+)-Octopamine, 3-iodothyronamine, dopamine | small-molecule | No | No | Jiang K, Zheng Y, Zeng L, Wang L, Li F, Pu J, Lu Y, Zhao S, Xu F | 10.1016/J.CELREP.2024.114505 | 2024-07-24 | Yes |
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