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RECEPTOR
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STRUCTURE
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SIGNAL PROTEIN
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AUXILIARY PROTEIN
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STRUCTURE LIGAND
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PHYSIOLOGICAL LIGAND
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SODIUM ION SITE
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REFERENCE
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ANNOTATED
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UniProt
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IUPHAR | Receptor family | Cl. | Species | Method |
PDB
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Refined structure |
Resolution | Preferred chain |
State |
Degree active (%) |
% of Seq | Family | Subtype | Note | % of Seq | Fusion | Antibodies | Name | Type | Modality | Name | Type | D2x50 S3x39 |
Sodium in structure |
Authors | Reference | PDB Date | ||
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 1U19 | 1U19_refined | 2.2 | A | Inactive | 22 | 100 | - | - | - | - | - | - |
Retinal (11-cis)
|
small-molecule | Inverse agonist | - | - | No | No | Okada T, Sugihara M, Bondar AN, Elstner M, Entel P, Buss V | 10.1016/J.JMB.2004.07.044 | 2004-10-12 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 2I35 | - | 3.8 | A | Inactive | 22 | 94 | - | - | - | - | - | - |
Retinal (11-cis)
|
small-molecule | Inverse agonist | - | - | No | No | - | 10.1073/PNAS.0608022103 | 2006-10-17 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 1HZX | - | 2.8 | A | Inactive | 22 | 98 | - | - | - | - | - | - |
Retinal (11-cis)
|
small-molecule | Inverse agonist | - | - | No | No | Teller DC, Okada T, Behnke CA, Palczewski K, Stenkamp RE | 10.1021/BI0155091 | 2001-07-04 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 1GZM | 1GZM_refined | 2.7 | A | Inactive | 22 | 94 | - | - | - | - | - | - |
Retinal (11-cis)
|
small-molecule | Inverse agonist | - | - | No | No | Li J, Edwards PC, Burghammer M, Villa C, Schertler GF | 10.1016/J.JMB.2004.08.090 | 2003-11-20 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 2RH1 | - | 2.4 | A | Inactive | 0 | 68 | - | - | - | - | T4-Lysozyme | - |
Carazolol
|
small-molecule | Inverse agonist | (-)-noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, Zn2+, noradrenaline | small-molecule | No | No | - | 10.1126/SCIENCE.1150577 | 2007-10-30 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 1F88 | 1F88_refined | 2.8 | A | Inactive | 22 | 97 | - | - | - | - | - | - |
Retinal (11-cis)
|
small-molecule | Inverse agonist | - | - | No | No | Palczewski K, Kumasaka T, Hori T, Behnke CA, Motoshima H, Fox BA, Le Trong I, Teller DC, Okada T, Stenkamp RE, Yamamoto M, Miyano M | 10.1126/SCIENCE.289.5480.739 | 2000-08-04 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 2HPY | - | 2.8 | B | Inactive | 22 | 100 | - | - | - | - | - | - |
Retinal (all-trans)
|
small-molecule | Agonist | - | - | No | No | Nakamichi H, Okada T | 10.1073/PNAS.0601765103 | 2006-08-22 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 3REY | 3REY_refined | 3.3 | A | Inactive | 0 | 71 | - | - | - | - | - | - |
xanthine amine congener
|
small-molecule | Antagonist | adenosine | small-molecule | No | No | Dore AS, Robertson N, Errey JC, Ng I, Hollenstein K, Tehan B, Hurrell E, Bennett K, Congreve M, Magnani F, Tate CG, Weir M, Marshall FH | 10.1016/J.STR.2011.06.014 | 2011-09-07 | Yes | |
5HT1B | 5-HT1B | 5-Hydroxytryptamine | A | Human | X-ray | 4IAR | 4IAR_refined | 2.7 | A | Inactive | 17 | 70 | - | - | - | - | BRIL | - |
ergotamine
|
small-molecule | Agonist | 5-hydroxytryptamine, tryptamine, 5-HT-moduline | small-molecule | No | No | Wang C, Jiang Y, Ma J, Wu H, Wacker D, Katritch V, Han GW, Liu W, Huang XP, Vardy E, McCorvy JD, Gao X, Zhou XE, Melcher K, Zhang C, Bai F, Yang H, Yang L, Jiang H, Roth BL, Cherezov V, Stevens RC, Xu HE | 10.1126/SCIENCE.1232807 | 2013-03-13 | Yes | |
P2Y12 | P2Y12 | P2Y | A | Human | X-ray | 4PY0 | 4PY0_refined | 3.1 | A | Active | 56 | 83 | - | - | - | - | BRIL | - |
2MeSATP
|
small-molecule | Agonist (partial) | ADP, ATP | small-molecule | No | No | Zhang J, Zhang K, Gao ZG, Paoletta S, Zhang D, Han GW, Li T, Ma L, Zhang W, Muller CE, Yang H, Jiang H, Cherezov V, Katritch V, Jacobson KA, Stevens RC, Wu B, Zhao Q | 10.1038/NATURE13288 | 2014-04-30 | Yes | |
AGTR1 | AT1 | Angiotensin | A | Human | X-ray | 4ZUD | 4ZUD_refined | 2.8 | A | Inactive | 10 | 75 | - | - | - | - | BRIL | - |
OLMESARTAN
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small-molecule | Inverse agonist | angiotensin A, angiotensin II, angiotensin III, angiotensin IV | peptide | No | No | Zhang H, Unal H, Desnoyer R, Han GW, Patel N, Katritch V, Karnik SS, Cherezov V, Stevens RC | 10.1074/JBC.M115.689000 | 2015-10-07 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5K2B | 5K2B_refined | 2.5 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
ZM-241385
|
small-molecule | Antagonist | adenosine | small-molecule | No | No | Batyuk A, Galli L, Ishchenko A, Han GW, Gati C, Popov PA, Lee MY, Stauch B, White TA, Barty A, Aquila A, Hunter MS, Liang M, Boutet S, Pu M, Liu ZJ, Nelson G, James D, Li C, Zhao Y, Spence JC, Liu W, Fromme P, Katritch V, Weierstall U, Stevens RC, Cherezov V | 10.1126/SCIADV.1600292 | 2016-09-21 | Yes | |
SMO | SMO | Frizzled | F | Human | X-ray | 5V57 | 5V57_refined | 3.0 | A | Inactive | 0 | 62 | - | - | - | - | Flavodoxin | - |
N-methyl-N-[1-[4-(2-methylpyrazol-3-yl)phthalazin-1-yl]piperidin-4-yl]-4-nitro-2-(trifluoromethyl)benzamide
|
small-molecule | Antagonist | - | - | No | No | Zhang X, Zhao F, Wu Y, Yang J, Han GW, Zhao S, Ishchenko A, Ye L, Lin X, Ding K, Dharmarajan V, Griffin PR, Gati C, Nelson G, Hunter MS, Hanson MA, Cherezov V, Stevens RC, Tan W, Tao H, Xu F | 10.1038/NCOMMS15383 | 2017-05-24 | Yes | |
5HT2C | 5-HT2C | 5-Hydroxytryptamine | A | Human | X-ray | 6BQH | 6BQH_refined | 2.7 | A | Inactive | 1 | 63 | - | - | - | - | BRIL | - |
ritanserin
|
small-molecule | Inverse agonist | 5-hydroxytryptamine | small-molecule | No | No | Peng Y, McCorvy JD, Harpsoe K, Lansu K, Yuan S, Popov P, Qu L, Pu M, Che T, Nikolajsen LF, Huang XP, Wu Y, Shen L, Bjorn-Yoshimoto WE, Ding K, Wacker D, Han GW, Cheng J, Katritch V, Jensen AA, Hanson MA, Zhao S, Gloriam DE, Roth BL, Stevens RC, Liu ZJ | 10.1016/j.cell.2018.01.001 | 2018-02-14 | Yes | |
PTAFR | PAF | Platelet-activating factor | A | Human | X-ray | 5ZKQ | 5ZKQ_refined | 2.9 | B | Active | 56 | 83 | - | - | - | - | T4-Lysozyme | - |
ABT-491
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small-molecule | Inverse agonist | PAF | small-molecule | No | No | Cao C, Tan Q, Xu C, He L, Yang L, Zhou Y, Zhou Y, Qiao A, Lu M, Yi C, Han GW, Wang X, Li X, Yang H, Rao Z, Jiang H, Zhao Y, Liu J, Stevens RC, Zhao Q, Zhang XC, Wu B | 10.1038/S41594-018-0068-Y | 2018-06-20 | Yes | |
PE2R3 | EP3 | Prostanoid | A | Human | X-ray | 6AK3 | 6AK3_refined | 2.9 | B | Active | 87 | 69 | - | - | - | - | BRIL | - |
PGE2
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small-molecule | Agonist | PGD2, PGF2α, PGE2, thromboxane A2, PGE1, PGI2 | small-molecule | No | No | Morimoto K, Suno R, Hotta Y, Yamashita K, Hirata K, Yamamoto M, Narumiya S, Iwata S, Kobayashi T | 10.1038/S41589-018-0171-8 | 2018-12-05 | Yes | |
MTR1B | MT2 | Melatonin | A | Human | X-ray | 6ME9 | 6ME9_refined | 3.3 | B | Inactive | 1 | 79 | - | - | - | - | Rubredoxin | - |
ramelteon
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small-molecule | Agonist | melatonin | small-molecule | No | No | Johansson LC, Stauch B, McCorvy JD, Han GW, Patel N, Huang XP, Batyuk A, Gati C, Slocum ST, Li C, Grandner JM, Hao S, Olsen RHJ, Tribo AR, Zaare S, Zhu L, Zatsepin NA, Weierstall U, Yous S, Stevens RC, Liu W, Roth BL, Katritch V, Cherezov V | 10.1038/S41586-019-1144-0 | 2019-04-24 | Yes | |
CLTR1 | CysLT1 | Leukotriene | A | Human | X-ray | 6RZ4 | 6RZ4_refined | 2.7 | A | Active | 56 | 85 | - | - | - | - | BRIL | - |
pranlukast
|
small-molecule | Antagonist | LTE4, LTC4, LTD4 | small-molecule | No | No | Luginina A, Gusach A, Marin E, Mishin A, Brouillette R, Popov P, Shiriaeva A, Besserer-Offroy E, Longpre JM, Lyapina E, Ishchenko A, Patel N, Polovinkin V, Safronova N, Bogorodskiy A, Edelweiss E, Hu H, Weierstall U, Liu W, Batyuk A, Gordeliy V, Han GW, Sarret P, Katritch V, Borshchevskiy V, Cherezov V | 10.1126/SCIADV.AAX2518 | 2019-10-30 | Yes | |
OPRD | δ | Opioid | A | Human | X-ray | 6PT2 | 6PT2_refined | 2.8 | A | Active | 72 | 78 | - | - | - | - | BRIL | - |
KGCHM07
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peptide | Agonist | dynorphin A, α-neoendorphin, [Leu]enkephalin, endomorphin-1, [Met]enkephalin, dynorphin B, β-endorphin, dynorphin A-(1-13), dynorphin A-(1-8) | peptide | No | No | Claff T, Yu J, Blais V, Patel N, Martin C, Wu L, Han GW, Holleran BJ, Van der Poorten O, White KL, Hanson MA, Sarret P, Gendron L, Cherezov V, Katritch V, Ballet S, Liu ZJ, Muller CE, Stevens RC | 10.1126/SCIADV.AAX9115 | 2019-12-11 | Yes | |
CNR2 | CB2 | Cannabinoid | A | Human | Cryo-EM | 6PT0 | 6PT0_refined | 3.2 | R | Active | 100 | 83 | Gi/o | αi1 | - | 100 | - | scFv16 |
WIN55212-2
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small-molecule | Agonist | anandamide, 2-arachidonoylglycerol | small-molecule | No | No | Xing C, Zhuang Y, Xu TH, Feng Z, Zhou XE, Chen M, Wang L, Meng X, Xue Y, Wang J, Liu H, McGuire TF, Zhao G, Melcher K, Zhang C, Xu HE, Xie XQ | 10.1016/J.CELL.2020.01.007 | 2020-02-12 | Yes | |
CCR6 | CCR6 | Chemokine | A | Human | Cryo-EM | 6WWZ | 6WWZ_refined | 3.3 | R | Active | 100 | 83 | Gi/o | αo | - | 59 | - | scFv16 |
CCL20
|
peptide | Agonist | beta-defensin 4A, CCL20 | peptide | No | No | Wasilko DJ, Johnson ZL, Ammirati M, Che Y, Griffor MC, Han S, Wu H | 10.1038/S41467-020-16820-6 | 2020-06-24 | Yes | |
STE2 | STE2 | STE2 | D1 | strain ATCC 204508 / S288c | Cryo-EM | 7AD3 | - | 3.5 | A | Active | - | 69 | GPa1 family | αPa1 | Two alpha subunits bound to STE2 dimer | 46 | - | - |
Alpha-factor mating pheromone
|
peptide | Agonist | - | - | No | No | Velazhahan V, Ma N, Pandy-Szekeres G, Kooistra AJ, Lee Y, Gloriam DE, Vaidehi N, Tate CG | 10.1038/S41586-020-2994-1 | 2020-12-09 | Yes | |
DRD1 | D1 | Dopamine | A | Human | Cryo-EM | 7CKX | - | 3.5 | R | Active | 100 | 61 | Gs | αs | - | 60 | - | Nanobody-35 |
A77636
|
small-molecule | Agonist | (-)-noradrenaline, L-NOREPINEPHRINE, dopamine, 5-hydroxytryptamine, noradrenaline | small-molecule | No | No | 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 | Yes | |
CCKAR | CCK1 | Cholecystokinin | A | Human | Cryo-EM | 7MBY | - | 2.4 | R | Active | 100 | 66 | Gq/11 | αq | Gq-Gs-Gi1 chimera | 55 | - | - |
CHEMBL216166
|
protein | Agonist | CCK-4, CCK-39, desulfated cholecystokinin-8, CCK-33, gastrin-17, CCK-8, CCK-58 | peptide | No | No | 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 | Yes | |
CCR5 | CCR5 | Chemokine | A | Human | Cryo-EM | 7F1Q | - | 2.9 | R | Active | 100 | 85 | Gi/o | αi1 | - | 61 | - | - |
CCL3
|
peptide | Agonist | CCL3, CCL5, CCL16, CCL4, CCL8, CCL7, CCL11, CCL2, CCL14, CCL13 | peptide | No | No | - | - | 2021-07-14 | Yes | |
MC4R | MC4 | Melanocortin | A | Human | Cryo-EM | 7PIV | 7PIV_refined | 2.9 | R | Active | 100 | 78 | Gs | αs | - | 46 | - | Nanobody-35 |
afamelanotide
|
peptide | Agonist | β-MSH, ACTH, γ-MSH, α-MSH, agouti-related protein | peptide | No | No | - | - | 2021-11-17 | Yes | |
GP139 | GPR139 | A orphans | A | Human | Cryo-EM | 7VUJ | 7VUJ_refined | 3.8 | R | Active | 100 | 79 | Gs | αs | - | 59 | - | Nanobody-35 |
JNJ-63533054
|
small-molecule | Agonist | L-tryptophan, L-phenylalanine | small-molecule | No | No | 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 | Yes | |
S1PR1 | S1P1 | Lysophospholipid (S1P) | A | Human | Cryo-EM | 7EVZ | - | 3.1 | D | Active | 100 | 71 | Gi/o | αi1 | - | 64 | - | scFv16 |
cenerimod
|
small-molecule | Agonist | sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine | small-molecule | No | No | 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 | Yes | |
MTR1A | MT1 | Melatonin | A | Human | Cryo-EM | 7VGZ | 7VGZ_refined | 3.3 | B | Active | 100 | 81 | Gi/o | αi1 | - | 62 | - | scFv16 |
ramelteon
|
small-molecule | Agonist | melatonin | small-molecule | No | No | Wang Q, Lu Q, Guo Q, Teng M, Gong Q, Li X, Du Y, Liu Z, Tao Y | 10.1038/S41467-022-28111-3 | 2022-03-02 | Yes | |
ADA2A | α2A | Adrenoceptors | A | Human | Cryo-EM | 7EJ0 | - | 3.2 | R | Active | 100 | 56 | Gi/o | αo | - | 61 | - | scFv16 |
(-)-noradrenaline
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline | small-molecule | No | No | Xu J, Cao S, Hubner H, Weikert D, Chen G, Lu Q, Yuan D, Gmeiner P, Liu Z, Du Y | 10.1126/SCIADV.ABJ5347 | 2022-04-13 | Yes | |
FPR2 | FPR2/ALX | Formylpeptide | A | Human | Cryo-EM | 7WVX | - | 2.8 | R | Active | 100 | 85 | Gi/o | αi2 | - | 61 | BRIL | - |
humanin
|
peptide | Agonist | resolvin D1, humanin, aspirin triggered lipoxin A4, serum amyloid A, LL-37, aspirin-triggered resolvin D1, PrP106-126, LXA4, annexin I | peptide | No | No | 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 | Yes | |
ACM4 | M4 | Acetylcholine (muscarinic) | A | Human | Cryo-EM | 7V6A | - | 3.6 | R | Active | 100 | 58 | Gi/o | αi1 | - | 62 | - | scFv16 |
methyl 4-[4-(3-methyl-2-oxidanylidene-benzimidazol-1-yl)piperidin-1-yl]piperidine-1-carboxylate
|
small-molecule | Allosteric agonist | acetylcholine | small-molecule | No | No | Wang J, Wu M, Chen Z, Wu L, Wang T, Cao D, Wang H, Liu S, Xu Y, Li F, Liu J, Chen N, Zhao S, Cheng J, Wang S, Hua T | 10.1038/S41467-022-30595-Y | 2022-05-11 | Yes | |
HRH2 | H2 | Histamine | A | Human | Cryo-EM | 7UL3 | 7UL3_refined | 3.0 | A | Inactive | 9 | 75 | - | - | - | - | - | Nanobody-6M NabFab HC NabFab LC |
famotidine
|
small-molecule | Antagonist | histamine | small-molecule | No | No | Robertson MJ, Papasergi-Scott MM, He F, Seven AB, Meyerowitz JG, Panova O, Peroto MC, Che T, Skiniotis G | 10.1038/S41594-022-00859-8 | 2022-06-29 | Yes | |
5HT6R | 5-HT6 | 5-Hydroxytryptamine | A | Human | Cryo-EM | 7XTB | 7XTB_refined | 3.3 | R | Active | 100 | 63 | Gs | αs | - | 60 | BRIL | Nanobody-35 |
5-hydroxytryptamine
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | No | No | 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 | Yes | |
MRGRD | MRGPRD | A orphans | A | Human | Cryo-EM | 7Y15 | 7Y15_refined | 2.9 | R | Active | 100 | 82 | Gi/o | αi1 | - | 62 | BRIL | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | β-alanine | small-molecule | No | No | Suzuki S, Iida M, Hiroaki Y, Tanaka K, Kawamoto A, Kato T, Oshima A | 10.1038/S42003-022-03668-3 | 2022-07-20 | Yes | |
TSHR | TSH | Glycoprotein hormone | A | Human | Cryo-EM | 7XW5 | - | 3.0 | R | Active | 100 | 75 | Gs | αs | - | 60 | - | Nanobody-35 |
Glycoprotein hormones alpha chain
Thyrotropin subunit beta N-[4-[[5-[(2S)-3-benzyl-5-hydroxy-4-oxo-1,2-dihydroquinazolin-2-yl]-2-methoxyphenyl]methoxy]phenyl]acetamide |
protein protein small-molecule |
Agonist | TSH | peptide | No | No | 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 | Yes | |
TAAR9 | TAAR9 | A orphans | A | Mouse | Cryo-EM | 8IW7 | - | 3.0 | R | Active | 100 | 78 | Gs | αs | - | 59 | - | scFv16 |
2-Phenylethanaminium
|
small-molecule | Agonist | - | - | No | No | 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 | Yes | |
PTH1R | PTH1 | Parathyroid hormone | B1 | Human | Cryo-EM | 8FLS | - | 3.1 | R | Active | 100 | 61 | Gs | αs | - | 59 | - | Nanobody-35 |
abaloparatide
|
small-molecule | Agonist | PTH, PTHrP, PTHrP-(1-36), TIP39 | peptide | No | No | 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 | Yes | |
PTH1R | PTH1 | Parathyroid hormone | B1 | Human | Cryo-EM | 7Y35 | - | 2.9 | R | Active | 100 | 63 | Gs | αs | - | 57 | - | Nanobody-35 |
abaloparatide
|
small-molecule | Agonist | PTH, PTHrP, PTHrP-(1-36), TIP39 | peptide | No | No | - | - | 2023-07-05 | Yes | |
GPR84 | GPR84 | A orphans | A | Human | Cryo-EM | 8J1A | - | 3.2 | R | Active | 100 | 73 | Gi/o | αi1 | - | 62 | - | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | 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 | Yes | |
GLR | glucagon | Glucagon | B1 | Human | Cryo-EM | 8JRV | - | 3.3 | R | Active | 100 | 64 | Beta | Beta-arrestin-1 | - | 85 | - | scFv30 Nanobody-32 |
glucagon
|
peptide | Agonist | glucagon | peptide | No | No | Chen K, Zhang C, Lin S, Yan X, Cai H, Yi C, Ma L, Chu X, Liu Y, Zhu Y, Han S, Zhao Q, Wu B | 10.1038/S41586-023-06420-X | 2023-08-16 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 8A2O | - | 3.5 | A | Inactive | 0 | 71 | - | - | - | - | BRIL | - |
theophylline
|
small-molecule | Antagonist | adenosine | small-molecule | No | No | Birch J, Kwan TOC, Judge PJ, Axford D, Aller P, Butryn A, Reis RI, Bada Juarez JF, Vinals J, Owen RL, Nango E, Tanaka R, Tono K, Joti Y, Tanaka T, Owada S, Sugahara M, Iwata S, Orville AM, Watts A, Moraes I | 10.1107/S1600576723006428 | 2023-08-30 | Yes | |
HRH4 | H4 | Histamine | A | Human | Cryo-EM | 8HN8 | - | 3.0 | R | Active | 100 | 71 | Gi/o | αi1 | - | 62 | - | scFv16 |
histamine
|
small-molecule | Agonist | histamine, CCL16 | small-molecule | No | No | - | - | 2023-12-20 | Yes | |
HCAR2 | HCA2 | Hydroxycarboxylic acid | A | Human | Cryo-EM | 8IHI | - | 3.1 | R | Active | 100 | 80 | Gi/o | αi1 | - | 62 | BRIL | scFv16 |
(5S)-5-methyl-4-oxo-5-phenylfuran-2-carboxylic acid
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | No | No | Suzuki S, Tanaka K, Nishikawa K, Suzuki H, Oshima A, Fujiyoshi Y | 10.1038/S41467-023-41650-7 | 2023-08-30 | Yes | |
GLR | glucagon | Glucagon | B1 | Human | Cryo-EM | 8JIT | - | 2.9 | R | Active | 100 | 83 | Gs | αs | - | 58 | - | Nanobody-35 |
MEDI0382
|
peptide | Agonist | glucagon | peptide | No | No | 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 | Yes | |
GP101 | GPR101 | A orphans | A | Human | Cryo-EM | 8W8S | - | 3.3 | R | Active | 89 | 55 | - | - | - | - | - | - |
1-(4-Methylpyridin-2-yl)-3-[3-(trifluoromethyl)phenyl]thiourea
|
small-molecule | Agonist | - | - | No | No | 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 | Yes | |
GPR34 | GPR34 | A orphans | A | Human | Cryo-EM | 8WRB | - | 2.9 | R | Active | 100 | 74 | Gi/o | αi1 | - | 63 | - | scFv16 |
LYSOPHOSPHATIDIC ACID
|
small-molecule | Agonist | lysophosphatidylserine | small-molecule | No | No | Liu G, Li X, Wang Y, Zhang X, Gong W | 10.1371/JOURNAL.PBIO.3002387 | 2023-11-08 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | Cryo-EM | 8GEI | - | 4.1 | R | Active | 100 | 68 | Gs | αs | - | 70 | - | - |
(5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, Zn2+, noradrenaline | small-molecule | No | No | Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G | 10.1038/S41586-024-07153-1 | 2024-03-06 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | Cryo-EM | 8GGO | - | 3.2 | R | Active | 97 | 68 | - | - | - | - | - | - |
(5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, Zn2+, noradrenaline | small-molecule | No | No | Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G | 10.1038/S41586-024-07153-1 | 2024-03-06 | Yes | |
HCAR2 | HCA2 | Hydroxycarboxylic acid | A | Human | Cryo-EM | 8IYH | 8IYH_refined | 3.3 | D | Active | 100 | 79 | Gi/o | αo | - | 58 | - | scFv16 |
MK 6892
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | No | No | Yadav MK, Sarma P, Maharana J, Ganguly M, Mishra S, Zaidi N, Dalal A, Singh V, Saha S, Mahajan G, Sharma S, Chami M, Banerjee R, Shukla AK | 10.1038/S41467-024-46239-2 | 2024-03-06 | Yes | |
OPRM | μ | Opioid | A | Human | Cryo-EM | 8K9K | - | 3.0 | R | Active | 100 | 70 | Gi/o | αi3 | - | 63 | BRIL | scFv16 |
DAMGO
|
peptide | Agonist | dynorphin A, endomorphin-2, [Leu]enkephalin, endomorphin-1, [Met]enkephalin, dynorphin B, β-endorphin, dynorphin A-(1-13), dynorphin A-(1-8) | peptide | No | No | Kaneko S, Imai S, Uchikubo-Kamo T, Hisano T, Asao N, Shirouzu M, Shimada I | 10.1038/S41467-024-47792-6 | 2024-05-29 | 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 | |
FZD4 | FZD4 | Frizzled | F | Human | Cryo-EM | 8WMA | - | 3.5 | A | Active | 98 | 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 | |
SSR3 | SST3 | Somatostatin | A | Human | Cryo-EM | 8XIQ | - | 2.7 | A | Active | 100 | 69 | Gi/o | αi1 | - | 62 | - | Nanobody-35 |
NIT-FC0-NLE-A1D5B
|
peptide | Agonist | SRIF-14, CST-17, SRIF-28, cortistatin-14 | peptide | No | No | - | - | 2024-07-03 | Yes | |
HRH2 | H2 | Histamine | A | Human | Cryo-EM | 8YUT | - | 2.7 | R | Active | 100 | 82 | Gs | αs | - | 58 | - | Nanobody-35 |
amthamine
|
small-molecule | Agonist | histamine | small-molecule | No | No | - | - | 2024-06-05 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 2YDV | 2YDV_refined | 2.6 | A | Active | 72 | 75 | - | - | - | - | - | - |
NECA
|
small-molecule | Agonist | adenosine | small-molecule | No | No | Lebon G, Warne T, Edwards PC, Bennett K, Langmead CJ, Leslie AG, Tate CG | 10.1038/NATURE10136 | 2011-05-18 | Yes | |
PAR1 | PAR1 | Proteinase-activated | A | Human | X-ray | 3VW7 | 3VW7_refined | 2.2 | A | Active | 56 | 66 | - | - | - | - | T4-Lysozyme | - |
vorapaxar
|
small-molecule | Antagonist | thrombin | peptide | No | No | Zhang C, Srinivasan Y, Arlow DH, Fung JJ, Palmer D, Zheng Y, Green HF, Pandey A, Dror RO, Shaw DE, Weis WI, Coughlin SR, Kobilka BK | 10.1038/NATURE11701 | 2012-12-12 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 4PXF | 4PXF_refined | 2.8 | A | Active | 100 | 93 | Visual | S-arrestin | Fragment | 2 | - | - |
B-Octylglucoside
|
small-molecule | unknown | - | - | No | No | Szczepek M, Beyriere F, Hofmann KP, Elgeti M, Kazmin R, Rose A, Bartl FJ, von Stetten D, Heck M, Sommer ME, Hildebrand PW, Scheerer P | 10.1038/NCOMMS5801 | 2014-09-17 | Yes | |
GRM5 | mGlu5 | Metabotropic glutamate | C | Human | X-ray | 5CGD | 5CGD_refined | 2.6 | A | Inactive | - | 20 | - | - | - | - | T4-Lysozyme | - |
CHEMBL3603923
|
small-molecule | NAM | L-glutamic acid | small-molecule | No | No | Christopher JA, Aves SJ, Bennett KA, Doré AS, Errey JC, Jazayeri A, Marshall FH, Okrasa K, Serrano-Vega MJ, Tehan BG, Wiggin GR, Congreve M. | 10.1021/acs.jmedchem.5b00892 | 2015-08-12 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 5JQH | 5JQH_refined | 3.2 | A | Inactive | 0 | 70 | - | - | - | - | T4-Lysozyme | Nanobody |
Carazolol
|
small-molecule | Inverse agonist | (-)-noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, Zn2+, noradrenaline | small-molecule | No | No | Staus DP, Strachan RT, Manglik A, Pani B, Kahsai AW, Kim TH, Wingler LM, Ahn S, Chatterjee A, Masoudi A, Kruse AC, Pardon E, Steyaert J, Weis WI, Prosser RS, Kobilka BK, Costa T, Lefkowitz RJ | 10.1038/NATURE18636 | 2016-07-13 | Yes | |
CNR1 | CB1 | Cannabinoid | A | Human | X-ray | 5XR8 | 5XR8_refined | 3.0 | A | Active | 91 | 60 | - | - | - | - | Flavodoxin | - |
AM841
|
small-molecule | Agonist | anandamide, 2-arachidonoylglycerol | small-molecule | No | No | Hua T, Vemuri K, Nikas SP, Laprairie RB, Wu Y, Qu L, Pu M, Korde A, Jiang S, Ho JH, Han GW, Ding K, Li X, Liu H, Hanson MA, Zhao S, Bohn LM, Makriyannis A, Stevens RC, Liu ZJ | 10.1038/NATURE23272 | 2017-07-12 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5OLH | 5OLH_refined | 2.6 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
vipadenant
|
small-molecule | Antagonist | adenosine | small-molecule | No | No | Rucktooa P, Cheng RKY, Segala E, Geng T, Errey JC, Brown GA, Cooke RM, Marshall FH, Dore AS | 10.1038/S41598-017-18570-W | 2018-01-17 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 6FKD | 6FKD_refined | 2.5 | A | Active | 98 | 94 | - | - | - | - | - | - |
5-chloro-2-(2-oxo-2-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-ylethyl)-3H-pyridin-6-one
|
small-molecule | Agonist | - | - | No | No | Mattle D, Kuhn B, Aebi J, Bedoucha M, Kekilli D, Grozinger N, Alker A, Rudolph MG, Schmid G, Schertler GFX, Hennig M, Standfuss J, Dawson RJP | 10.1073/PNAS.1718084115 | 2018-04-04 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 6FUF | 6FUF_refined | 3.1 | A | Active | 100 | 91 | Gi/o | αo | Mini-Go | 51 | - | - |
Retinal (all-trans)
|
small-molecule | Agonist | - | - | No | No | 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 | Yes | |
CCR5 | CCR5 | Chemokine | A | Human | Cryo-EM | 6MEO | 6MEO_refined | 3.9 | B | Inactive | 10 | 89 | - | - | - | - | - | T-cell surface glycoprotein CD4 |
Envelope glycoprotein gp160
|
protein | Antagonist | CCL3, CCL5, CCL16, CCL4, CCL8, CCL7, CCL11, CCL2, CCL14, CCL13 | peptide | No | No | Shaik MM, Peng H, Lu J, Rits-Volloch S, Xu C, Liao M, Chen B | 10.1038/S41586-018-0804-9 | 2018-12-12 | Yes | |
HCAR2 | HCA2 | Hydroxycarboxylic acid | A | Human | Cryo-EM | 8J6P | - | 2.6 | R | Active | 100 | 81 | Gi/o | αi1 | - | 64 | - | scFv16 |
nicotinic acid
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | No | No | 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 | Yes | |
HCAR2 | HCA2 | Hydroxycarboxylic acid | A | Human | Cryo-EM | 8JZ7 | 8JZ7_refined | 2.6 | A | Active | 100 | 80 | Gi/o | αi1 | - | 64 | - | scFv16 |
MK 6892
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | No | No | Cheng L, Sun S, Wang H, Zhao C, Tian X, Liu Y, Fu P, Shao Z, Chai R, Yan W | 10.1038/S41392-023-01625-Y | 2023-10-04 | Yes | |
TAAR1 | TA1 | Trace amine | A | Human | Cryo-EM | 8W87 | - | 2.8 | R | Active | 100 | 85 | Gs | αs | - | 59 | - | Nanobody-35 |
METHAMPHETAMINE
|
small-molecule | Agonist | octopamine, 3-iodothyronamine, β-phenylethylamine, CHEMBL1160703, dopamine, tyramine, (+)-Octopamine | small-molecule | No | No | 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 | Yes | |
GHRHR | GHRH | Glucagon | B1 | Human | Cryo-EM | 7V9L | - | 2.6 | R | Active | 100 | 61 | Gs | αs | - | 60 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | GHRH | peptide | No | No | 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 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | Cryo-EM | 8GEE | 8GEE_refined | 3.7 | R | Active | 100 | 68 | Gs | αs | - | 69 | - | - |
(5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, Zn2+, noradrenaline | small-molecule | No | No | Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G | 10.1038/S41586-024-07153-1 | 2024-03-06 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | Cryo-EM | 8GGJ | - | 3.5 | R | Active | 97 | 69 | - | - | - | - | - | - |
(5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, Zn2+, noradrenaline | small-molecule | No | No | Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G | 10.1038/S41586-024-07153-1 | 2024-03-06 | Yes | |
PF2R | FP | Prostanoid | A | Human | Cryo-EM | 8IQ6 | 8IQ6_refined | 3.4 | R | Active | 100 | 76 | Gs | αs | - | 51 | - | Nanobody-35 |
latanoprost (free acid form)
|
small-molecule | Agonist | PGD2, PGF2α, PGE2, thromboxane A2, PGI2 | small-molecule | No | No | Lv X, Gao K, Nie J, Zhang X, Zhang S, Ren Y, Sun X, Li Q, Huang J, Liu L, Zhang X, Zhang W, Liu X | 10.1038/S41467-023-43922-8 | 2024-01-31 | Yes | |
SUCR1 | succinate | Succinate | A | Human | Cryo-EM | 8JPN | - | 2.9 | R | Active | 100 | 89 | Gi/o | αi1 | - | 64 | BRIL | scFv16 |
cis-epoxysuccinic acid
|
small-molecule | Agonist | succinic acid | small-molecule | No | No | Wang T, Tang W, Zhu X, Lv Z, Chen J, Li Y, Sun X, Lv H, Gu Q, Li F, Wang J | 10.1038/S41422-024-00968-7 | 2024-05-22 | Yes | |
AGTR1 | AT1 | Angiotensin | A | Human | Cryo-EM | 8TH4 | - | 3.3 | A | Inactive | 10 | 78 | - | - | - | - | BRIL | BAG2 Anti-BRIL Fab Heavy chain BAG2 Anti-BRIL Fab Light chain |
AT118-L Nanobody
|
protein | Antagonist | angiotensin A, angiotensin II, angiotensin III, angiotensin IV | peptide | No | No | Skiba MA, Sterling SM, Rawson S, Zhang S, Xu H, Jiang H, Nemeth GR, Gilman MSA, Hurley JD, Shen P, Staus DP, Kim J, McMahon C, Lehtinen MK, Rockman HA, Barth P, Wingler LM, Kruse AC | 10.1038/S41589-024-01620-6 | 2024-05-22 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | Cryo-EM | 8UO1 | 8UO1_refined | 3.6 | R | Active | 100 | 68 | Gs | αs | GTP bound, Class Q | 85 | - | - |
(5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, Zn2+, noradrenaline | small-molecule | No | No | Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G | 10.1038/S41586-024-07153-1 | 2024-03-06 | Yes | |
HRH1 | H1 | Histamine | A | Human | Cryo-EM | 8X5X | - | 3.5 | B | Inactive | 3 | 52 | - | - | - | - | BRIL | - |
Apo (no ligand)
|
none | Apo (no ligand) | histamine | small-molecule | No | No | Wang D, Guo Q, Wu Z, Li M, He B, Du Y, Zhang K, Tao Y | 10.1038/S41467-023-44477-4 | 2024-01-17 | Yes | |
GPER1 | GPER | Estrogen (G protein-coupled) | A | Human | Cryo-EM | 8XOI | 8XOI_refined | 3.2 | R | Active | 100 | 70 | Gq/11 | αq | - | 59 | - | scFv16 |
fulvestrant
|
small-molecule | Agonist | 17β-estradiol | small-molecule | No | No | Liu H, Guo S, Dai A, Xu P, Li X, Huang S, He X, Wu K, Zhang X, Yang D, Xie X, Xu HE | 10.1038/S41422-024-00963-Y | 2024-04-10 | Yes | |
APJ | apelin | Apelin | A | Human | Cryo-EM | 8XZF | 8XZF_refined | 3.0 | R | Active | 100 | 80 | Gi/o | αi1 | - | 61 | - | scFv16 |
WN561
|
peptide | Agonist | apelin-13, apelin receptor early endogenous ligand, apelin-36, [Pyr1]apelin-13, Elabela/Toddler-11, Elabela/Toddler-32, Elabela/Toddler-21, apelin-17 | peptide | No | No | Wang WW, Ji SY, Zhang W, Zhang J, Cai C, Hu R, Zang SK, Miao L, Xu H, Chen LN, Yang Z, Guo J, Qin J, Shen DD, Liang P, Zhang Y, Zhang Y | 10.1016/J.CELL.2024.02.004 | 2024-03-20 | Yes | |
ADRB1 | β1 | Adrenoceptors | A | Wild turkey | X-ray | 2Y00 | 2Y00_refined | 2.5 | B | Inactive | 0 | 62 | - | - | - | - | - | - |
Dobutamine
|
small-molecule | Agonist (partial) | - | - | No | No | Warne T, Moukhametzianov R, Baker JG, Nehme R, Edwards PC, Leslie AG, Schertler GF, Tate CG | 10.1038/NATURE09746 | 2011-01-12 | Yes | |
ACM2 | M2 | Acetylcholine (muscarinic) | A | Human | X-ray | 3UON | 3UON_refined | 3.0 | A | Inactive | 3 | 60 | - | - | - | - | T4-Lysozyme | - |
CHEMBL558910
|
small-molecule | Antagonist | acetylcholine | small-molecule | No | No | Haga K, Kruse AC, Asada H, Yurugi-Kobayashi T, Shiroishi M, Zhang C, Weis WI, Okada T, Kobilka BK, Haga T, Kobayashi T | 10.1038/NATURE10753 | 2012-02-01 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 4LDO | 4LDO_refined | 3.2 | A | Active | 98 | 69 | - | - | - | - | T4-Lysozyme | Nanobody |
(-)-adrenaline
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, Zn2+, noradrenaline | small-molecule | No | No | Ring AM, Manglik A, Kruse AC, Enos MD, Weis WI, Garcia KC, Kobilka BK | 10.1038/NATURE12572 | 2013-09-25 | Yes | |
CXCR4 | CXCR4 | Chemokine | A | Human | X-ray | 4RWS | 4RWS_refined | 3.1 | A | Inactive | 9 | 78 | - | - | - | - | T4-Lysozyme | - |
vMIP-II
|
peptide | Antagonist | CXCL12γ, CXCL12β, CXCL12ε, CXCL12φ, CXCL12δ, CXCL12, CXCL12α | peptide | No | No | Qin L, Kufareva I, Holden LG, Wang C, Zheng Y, Zhao C, Fenalti G, Wu H, Han GW, Cherezov V, Abagyan R, Stevens RC, Handel TM | 10.1126/SCIENCE.1261064 | 2015-02-11 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5UVI | 5UVI_refined | 3.2 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
ZM-241385
|
small-molecule | Antagonist | adenosine | small-molecule | No | No | Martin-Garcia JM, Conrad CE, Nelson G, Stander N, Zatsepin NA, Zook J, Zhu L, Geiger J, Chun E, Kissick D, Hilgart MC, Ogata C, Ishchenko A, Nagaratnam N, Roy-Chowdhury S, Coe J, Subramanian G, Schaffer A, James D, Ketwala G, Venugopalan N, Xu S, Corcoran S, Ferguson D, Weierstall U, Spence JCH, Cherezov V, Fromme P, Fischetti RF, Liu W | 10.1107/S205225251700570X | 2017-05-24 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5NM2 | 5NM2_refined | 2.0 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
ZM-241385
|
small-molecule | Antagonist | adenosine | small-molecule | No | No | Weinert T, Olieric N, Cheng R, Brunle S, James D, Ozerov D, Gashi D, Vera L, Marsh M, Jaeger K, Dworkowski F, Panepucci E, Basu S, Skopintsev P, Dore AS, Geng T, Cooke RM, Liang M, Prota AE, Panneels V, Nogly P, Ermler U, Schertler G, Hennig M, Steinmetz MO, Wang M, Standfuss J | 10.1038/S41467-017-00630-4 | 2017-09-27 | Yes | |
Q98SW5 | SMO | Frizzled | F | African clawed frog | X-ray | 6D35 | 6D35_refined | 3.9 | A | Active | 66 | 58 | - | - | - | - | BRIL | - |
Cholesterol
|
small-molecule | Agonist | - | - | No | No | Huang P, Zheng S, Wierbowski BM, Kim Y, Nedelcu D, Aravena L, Liu J, Kruse AC, Salic A | 10.1016/J.CELL.2018.04.029 | 2018-05-23 | Yes | |
ADRB1 | β1 | Adrenoceptors | A | Wild turkey | X-ray | 6H7O | 6H7O_refined | 2.8 | A | Active | 98 | 60 | - | - | - | - | Thioredoxin 1 | Camelid antibody fragment Nb6B9 |
(S)-Cyanopindolol
|
small-molecule | Agonist | - | - | No | No | Warne T, Edwards PC, Dore AS, Leslie AGW, Tate CG | 10.1126/SCIENCE.AAU5595 | 2018-10-17 | Yes | |
GRM5 | mGlu5 | Metabotropic glutamate | C | Human | Cryo-EM | 6N52 | 6N52_refined | 4.0 | A | Inactive | - | 64 | - | - | - | - | - | Nanobody-43 |
Apo (no ligand)
|
none | Apo (no ligand) | L-glutamic acid | small-molecule | No | No | Koehl A, Hu H, Feng D, Sun B, Zhang Y, Robertson MJ, Chu M, Kobilka TS, Laeremans T, Steyaert J, Tarrasch J, Dutta S, Fonseca R, Weis WI, Mathiesen JM, Skiniotis G, Kobilka BK | 10.1038/S41586-019-0881-4 | 2019-01-23 | Yes | |
SUCR1 | succinate | Succinate | A | Rat | X-ray | 6RNK | 6RNK_refined | 1.9 | A | Active | 56 | 90 | - | - | - | - | - | Nanobody-6 |
NF-56-EJ40
|
small-molecule | Antagonist | - | - | No | No | Haffke M, Fehlmann D, Rummel G, Boivineau J, Duckely M, Gommermann N, Cotesta S, Sirockin F, Freuler F, Littlewood-Evans A, Kaupmann K, Jaakola VP | 10.1038/S41586-019-1663-8 | 2019-08-14 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 6PS6 | 6PS6_refined | 2.7 | A | Inactive | 0 | 68 | - | - | - | - | T4-Lysozyme | - |
timolol
|
small-molecule | Antagonist | (-)-noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, Zn2+, noradrenaline | small-molecule | No | No | Ishchenko A, Stauch B, Han GW, Batyuk A, Shiriaeva A, Li C, Zatsepin N, Weierstall U, Liu W, Nango E, Nakane T, Tanaka R, Tono K, Joti Y, Iwata S, Moraes I, Gati C, Cherezov V | 10.1107/S2052252519013137 | 2019-11-13 | Yes | |
AGTR2 | AT2 | Angiotensin | A | Human | X-ray | 6JOD | 6JOD_refined | 3.2 | A | Active | 100 | 84 | - | - | - | - | BRIL | Heavy chain of 4A03Fab Light chain of 4A03Fab |
angiotensin II
|
peptide | Agonist | angiotensin II, angiotensin-(1-7), angiotensin III | peptide | No | No | Asada H, Inoue A, Ngako Kadji FM, Hirata K, Shiimura Y, Im D, Shimamura T, Nomura N, Iwanari H, Hamakubo T, Kusano-Arai O, Hisano H, Uemura T, Suno C, Aoki J, Iwata S | 10.1016/J.STR.2019.12.003 | 2020-01-15 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 6OBA | 6OBA_refined | 3.1 | A | Inactive | 0 | 68 | - | - | - | - | T4-Lysozyme | - |
CHEMBL1160734
AS408 |
small-molecule small-molecule |
Antagonist NAM |
(-)-noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, Zn2+, noradrenaline | small-molecule | No | No | Liu X, Kaindl J, Korczynska M, Stossel A, Dengler D, Stanek M, Hubner H, Clark MJ, Mahoney J, Matt RA, Xu X, Hirata K, Shoichet BK, Sunahara RK, Kobilka BK, Gmeiner P | 10.1038/S41589-020-0549-2 | 2020-03-25 | Yes | |
GABR2 | GABAB2 | GABAB | C | Human | Cryo-EM | 7C7Q | - | 3.0 | B | Active | - | 71 | - | - | - | - | - | - |
(-)-baclofen
BHFF |
small-molecule small-molecule |
Agonist PAM |
- | - | No | No | Mao C, Shen C, Li C, Shen DD, Xu C, Zhang S, Zhou R, Shen Q, Chen LN, Jiang Z, Liu J, Zhang Y | 10.1038/S41422-020-0350-5 | 2020-07-01 | Yes | |
SMO | SMO | Frizzled | F | Human | Cryo-EM | 6XBL | - | 3.9 | R | Active | 100 | 59 | Gi/o | αi1 | - | 61 | - | scFv16 |
Cholesterol
SAG1.3 |
small-molecule small-molecule |
Agonist PAM |
- | - | No | No | Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X | 10.1038/S41589-020-0646-2 | 2020-09-30 | Yes | |
DRD1 | D1 | Dopamine | A | Human | Cryo-EM | 7JV5 | - | 3.0 | R | Active | 100 | 63 | Gs | αs | - | 60 | - | Nanobody-35 |
CHEMBL1160787
|
small-molecule | Agonist | (-)-noradrenaline, L-NOREPINEPHRINE, dopamine, 5-hydroxytryptamine, noradrenaline | small-molecule | No | No | 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 | Yes | |
PE2R2 | EP2 | Prostanoid | A | Human | Cryo-EM | 7CX3 | - | 2.8 | R | Active | 100 | 74 | Gs | αs | - | 58 | - | Nanobody-35 |
taprenepag
|
small-molecule | Agonist | PGD2, PGF2α, PGE2, thromboxane A2, PGE1, PGI2 | small-molecule | No | No | Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y | 10.1126/SCIADV.ABF1268 | 2021-05-05 | Yes | |
CASR | CaS | Calcium-sensing | C | Human | Cryo-EM | 7M3G | 7M3G_refined | 2.5 | A | Active | - | 76 | - | - | - | - | - | - |
Calcium
L-tryptophan evocalcet |
small-molecule small-molecule small-molecule |
Agonist PAM PAM |
L-tryptophan, spermine, Ca2+, Mg2+ | small-molecule | No | No | Gao Y, Robertson MJ, Rahman SN, Seven AB, Zhang C, Meyerowitz JG, Panova O, Hannan FM, Thakker RV, Brauner-Osborne H, Mathiesen JM, Skiniotis G | 10.1038/S41586-021-03691-0 | 2021-06-30 | Yes | |
S1PR3 | S1P3 | Lysophospholipid (S1P) | A | Human | Cryo-EM | 7EW2 | - | 3.1 | R | Active | 100 | 77 | Gi/o | αi1 | - | 64 | - | scFv16 |
(S)-FTY720-phosphate
|
small-molecule | Agonist | sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine | small-molecule | No | No | 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 | Yes | |
NK1R | NK1 | Tachykinin | A | Human | Cryo-EM | 7RMG | - | 3.0 | R | Active | 100 | 71 | Gq/11 | αq | Gs-Gq chimera | 52 | - | Nanobody-35 |
substance P
|
peptide | Agonist | neuropeptide-γ, neurokinin B, neuropeptide K, substance P, hemokinin 1, neurokinin A | peptide | No | No | Harris JA, Faust B, Gondin AB, Damgen MA, Suomivuori CM, Veldhuis NA, Cheng Y, Dror RO, Thal DM, Manglik A | 10.1038/S41589-021-00890-8 | 2021-11-03 | Yes | |
5HT2A | 5-HT2A | 5-Hydroxytryptamine | A | Human | X-ray | 7VOD | 7VOD_refined | 3.3 | A | Inactive | 1 | 58 | - | - | - | - | BRIL | - |
cariprazine
|
small-molecule | Agonist (partial) | 5-hydroxytryptamine, tryptamine | small-molecule | No | No | Chen Z, Fan L, Wang H, Yu J, Lu D, Qi J, Nie F, Luo Z, Liu Z, Cheng J, Wang S | 10.1038/S41593-021-00971-W | 2021-12-22 | Yes | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 7LLL | - | 3.7 | R | Active | 100 | 79 | Gs | αs | - | 59 | - | Nanobody-35 |
exendin-4
|
peptide | Agonist | glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide | peptide | No | No | 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 | Yes | |
LT4R1 | BLT1 | Leukotriene | A | Human | Cryo-EM | 7VKT | 7VKT_refined | 2.9 | A | Active | 100 | 82 | Gi/o | αi1 | - | 64 | - | scFv16 |
LTB4
|
small-molecule | Agonist | 12R-HETE, LTB4, 20-hydroxy-LTB4 | small-molecule | No | No | Wang N, He X, Zhao J, Jiang H, Cheng X, Xia Y, Eric Xu H, He Y | 10.1038/S41467-022-28820-9 | 2022-03-09 | Yes | |
GIPR | GIP | Glucagon | B1 | Human | Cryo-EM | 7FIY | - | 3.4 | R | Active | 100 | 77 | Gs | αs | - | 60 | - | Nanobody-35 |
tirzepatide
|
peptide | Agonist | gastric inhibitory polypeptide | peptide | No | No | 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 | Yes | |
ADRB1 | β1 | Adrenoceptors | A | Wild turkey | Cryo-EM | 7S0G | - | 3.9 | R | Active | 100 | 57 | Gs | αs | Gi1-Gs chimera | 56 | - | - |
LEVISOPRENALINE
|
small-molecule | Agonist | - | - | No | No | Alegre KO, Paknejad N, Su M, Lou JS, Huang J, Jordan KD, Eng ET, Meyerson JR, Hite RK, Huang XY | 10.1038/S41594-021-00679-2 | 2021-11-17 | Yes | |
DRD1 | D1 | Dopamine | A | Human | Cryo-EM | 7F1O | - | 3.1 | F | Active | 100 | 62 | Gs | αs | - | 60 | - | Nanobody-35 |
dopamine
|
small-molecule | Agonist | (-)-noradrenaline, L-NOREPINEPHRINE, dopamine, 5-hydroxytryptamine, noradrenaline | small-molecule | No | No | Teng X, Chen S, Wang Q, Chen Z, Wang X, Huang N, Zheng S | 10.1126/SCIADV.ABO4158 | 2022-06-15 | Yes | |
SMO | SMO | Frizzled | F | Human | X-ray | 7ZI0 | 7ZI0_refined | 3.0 | A | Inactive | 4 | 61 | - | - | - | - | BRIL | - |
3-chloro-N-[trans-4-(methylamino)cyclohexyl]-N-{[3-(pyridin-4-yl)phenyl]methyl}-1-benzothiophene-2-carboxamide
|
small-molecule | Antagonist | - | - | No | No | Kinnebrew M, Woolley RE, Ansell TB, Byrne EFX, Frigui S, Luchetti G, Sircar R, Nachtergaele S, Mydock-McGrane L, Krishnan K, Newstead S, Sansom MSP, Covey DF, Siebold C, Rohatgi R | 10.1126/SCIADV.ABM5563 | 2022-06-15 | Yes | |
MRGRD | MRGPRD | A orphans | A | Human | Cryo-EM | 7Y14 | 7Y14_refined | 3.2 | R | Intermediate | 47 | 82 | - | - | - | - | BRIL | - |
β-alanine
|
small-molecule | Agonist | β-alanine | small-molecule | No | No | Suzuki S, Iida M, Hiroaki Y, Tanaka K, Kawamoto A, Kato T, Oshima A | 10.1038/S42003-022-03668-3 | 2022-07-20 | Yes | |
SSR2 | SST2 | Somatostatin | A | Human | Cryo-EM | 7XMR | 7XMR_refined | 3.1 | R | Active | 100 | 77 | Gi/o | αi1 | - | 63 | - | - |
SOMATOSTATIN
|
protein | Agonist | SRIF-14, CST-17, SRIF-28, cortistatin-14 | peptide | No | No | 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 | Yes | |
AGRG2 | ADGRG2 | ADGRG | B2 | Mouse | Cryo-EM | 7YP7 | - | 3.1 | R | Active | 100 | 24 | Gs | αs | - | 59 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | - | - | 2022-08-24 | Yes | |
OPRM | μ | Opioid | A | Mouse | Cryo-EM | 7T2G | - | 2.5 | R | Active | 100 | 70 | Gi/o | αi1 | - | 62 | BRIL | - |
CHEMBL58362
|
small-molecule | Agonist | - | - | No | No | Qu Q, Huang W, Aydin D, Paggi JM, Seven AB, Wang H, Chakraborty S, Che T, DiBerto JF, Robertson MJ, Inoue A, Suomivuori CM, Roth BL, Majumdar S, Dror RO, Kobilka BK, Skiniotis G | 10.1038/S41589-022-01208-Y | 2022-12-07 | Yes | |
AGRL3 | ADGRL3 | ADGRL | B2 | Mouse | Cryo-EM | 7WY5 | - | 2.8 | R | Active | 100 | 17 | Gq/11 | αq | Mini-Gq | 59 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | 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 | Yes | |
LPAR1 | LPA1 | Lysophospholipid (LPA) | A | Human | Cryo-EM | 7YU3 | 7YU3_refined | 3.4 | R | Active | 100 | 80 | Gi/o | αi1 | - | 63 | - | scFv16 |
[(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate
|
small-molecule | Agonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | No | No | Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O | 10.1038/S41467-022-33121-2 | 2022-10-05 | Yes | |
OPRM | μ | Opioid | A | Human | Cryo-EM | 8EFO | - | 2.8 | R | Active | 100 | 72 | Gi/o | αi1 | - | 64 | - | scFv16 |
PZM21
|
small-molecule | Agonist | dynorphin A, endomorphin-2, [Leu]enkephalin, endomorphin-1, [Met]enkephalin, dynorphin B, β-endorphin, dynorphin A-(1-13), dynorphin A-(1-8) | peptide | No | No | 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 | Yes | |
C5AR1 | C5a1 | Complement peptide | A | Human | Cryo-EM | 7Y67 | 7Y67_refined | 2.8 | D | Active | 100 | 79 | Gi/o | αi1 | - | 63 | - | scFv16 |
C089
|
peptide | Agonist | C5a des-Arg, C3a, C5a, ribosomal protein S19 | peptide | No | No | 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 | Yes | |
FFAR4 | FFA4 | Free fatty acid | A | Human | Cryo-EM | 8ID4 | - | 3.1 | R | Active | 100 | 79 | Gi/o | αi1 | - | 64 | - | scFv16 |
linoleic acid
|
small-molecule | Agonist | linoleic acid, myristic acid, α-linolenic acid, oleic acid | small-molecule | No | No | 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 | Yes | |
TAAR9 | TAAR9 | A orphans | A | Mouse | Cryo-EM | 8IW9 | - | 3.1 | R | Active | 100 | 89 | Gs | αs | Mini-Gs | 59 | - | scFv16 Nanobody-35 |
Cadaverine
|
small-molecule | Agonist | - | - | No | No | 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 | Yes | |
NK2R | NK2 | Tachykinin | A | Human | Cryo-EM | 7XWO | 7XWO_refined | 2.7 | B | Active | 100 | 68 | Gq/11 | αq | - | 59 | BRIL | scFv16 |
HIS-LYS-THR-ASP-SER-PHE-VAL-GLY-LEU-MET-NH2
|
peptide | Agonist | neurokinin B, substance P, neuropeptide K, hemokinin 1, neuropeptide γ, neurokinin A | peptide | No | No | - | - | 2023-05-31 | Yes | |
C3AR | C3a | Complement peptide | A | Human | Cryo-EM | 8HK2 | - | 2.9 | A | Active | 100 | 59 | Gi/o | αi1 | - | 64 | - | scFv16 |
C3a anaphylatoxin
|
peptide | Agonist | C3a, C5a | peptide | No | No | Wang Y, Liu W, Xu Y, He X, Yuan Q, Luo P, Fan W, Zhu J, Zhang X, Cheng X, Jiang Y, Xu HE, Zhuang Y | 10.1038/S41589-023-01339-W | 2023-05-10 | Yes | |
GPR52 | GPR52 | A orphans | A | Human | Cryo-EM | 8HMP | - | 2.8 | R | Active | 100 | 79 | Gs | αs | - | 61 | - | Nanobody-35 |
derivative 17 [Nakahata et al., 2018]
|
small-molecule | Agonist | - | - | No | No | Fan Y, Lin X, Pan B, Chen B, Liu D, Wuthrich K, Xu F | 10.1002/MCO2.260 | 2023-06-21 | Yes | |
GRM2 | mGlu2 | Metabotropic glutamate | C | Human | Cryo-EM | 8JCV | - | 3.4 | 2 | Inactive | - | 88 | - | - | - | - | - | - |
LY341495
|
small-molecule | Antagonist | L-glutamic acid | small-molecule | No | No | Wang X, Wang M, Xu T, Feng Y, Shao Q, Han S, Chu X, Xu Y, Lin S, Zhao Q, Wu B | 10.1038/S41422-023-00830-2 | 2023-06-21 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 8FD1 | - | 4.3 | A | Inactive | 22 | 88 | - | - | - | - | - | Nanobody-2 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Wu A, Salom D, Hong JD, Tworak A, Watanabe K, Pardon E, Steyaert J, Kandori H, Katayama K, Kiser PD, Palczewski K | 10.1038/S41467-023-40911-9 | 2023-08-30 | Yes | |
CXCR3 | CXCR3 | Chemokine | A | Human | Cryo-EM | 8HNL | - | 3.0 | R | Active | 100 | 80 | - | - | - | - | - | - |
(3S)-N-[(2S)-5-carbamimidamido-1-(cyclohexylmethylamino)-1-oxidanylidene-pentan-2-yl]-2-(4-oxidanylidene-4-phenyl-butanoyl)-3,4-dihydro-1H-isoquinoline-3-carboxamide
|
small-molecule | Agonist | CCL5, CCL20, CXCL9, CXCL10, CCL19, CXCL11, CCL7, CCL11, CCL13, CXCL12α | peptide | No | No | 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 | Yes | |
MC5R | MC5 | Melanocortin | A | Human | Cryo-EM | 8INR | - | 2.7 | R | Active | 100 | 83 | Gs | αs | Gi1-Gs chimera | 60 | - | - |
INTERMEDINE
|
protein | Agonist | β-MSH, ACTH, γ-MSH, α-MSH, agouti-related protein | peptide | No | No | 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 | Yes | |
AGRL3 | ADGRL3 | ADGRL | B2 | Human | Cryo-EM | 8JMT | - | 3.3 | A | Inactive | 0 | 16 | - | - | - | - | BRIL | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Guo Q, He B, Zhong Y, Jiao H, Ren Y, Wang Q, Ge Q, Gao Y, Liu X, Du Y, Hu H, Tao Y | 10.1038/S41589-023-01389-0 | 2023-09-06 | Yes | |
CML1 | chemerin | Chemerin receptor | A | Human | Cryo-EM | 8SG1 | - | 2.9 | R | Active | 100 | 75 | Gi/o | αi1 | - | 61 | - | scFv16 |
chemerin C-terminal peptide
|
peptide | Agonist | resolvin E1, chemerin C-terminal peptide, EPA, 18R-HEPE, chemerin | peptide | No | No | Zhang X, Weiss T, Cheng MH, Chen S, Ambrosius CK, Czerniak AS, Li K, Feng M, Bahar I, Beck-Sickinger AG, Zhang C | 10.1371/JOURNAL.PBIO.3002188 | 2023-11-01 | Yes | |
CASR | CaS | Calcium-sensing | C | Human | Cryo-EM | 8WPU | - | 3.1 | A | Active | - | 74 | Gq/11 | αq | Gi2-mini-Gq chimera | 58 | - | scFv16 |
Calcium
cinacalcet |
small-molecule small-molecule |
Agonist | L-tryptophan, spermine, Ca2+, Mg2+ | small-molecule | No | No | Ling S, Meng X, Zhang Y, Xia Z, Zhou Y, Yang F, Shi P, Shi C, Tian C | 10.1038/S41422-023-00892-2 | 2023-11-22 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | Cryo-EM | 8GGL | - | 3.2 | R | Active | 97 | 69 | - | - | - | - | - | - |
(5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, Zn2+, noradrenaline | small-molecule | No | No | Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G | 10.1038/S41586-024-07153-1 | 2024-03-06 | Yes | |
HCAR2 | HCA2 | Hydroxycarboxylic acid | A | Human | Cryo-EM | 8IY9 | 8IY9_refined | 3.4 | R | Active | 100 | 82 | Gi/o | αo | - | 59 | - | scFv16 |
nicotinic acid
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | No | No | Yadav MK, Sarma P, Maharana J, Ganguly M, Mishra S, Zaidi N, Dalal A, Singh V, Saha S, Mahajan G, Sharma S, Chami M, Banerjee R, Shukla AK | 10.1038/S41467-024-46239-2 | 2024-03-06 | Yes | |
SUCR1 | succinate | Succinate | A | Human | Cryo-EM | 8JPP | - | 3.2 | R | Active | 100 | 91 | Gs | αs | - | 60 | BRIL | - |
succinic acid
|
small-molecule | Agonist | succinic acid | small-molecule | No | No | Wang T, Tang W, Zhu X, Lv Z, Chen J, Li Y, Sun X, Lv H, Gu Q, Li F, Wang J | 10.1038/S41422-024-00968-7 | 2024-05-22 | Yes | |
FFAR1 | FFA1 | Free fatty acid | A | Human | Cryo-EM | 8T3V | - | 3.4 | R | Active | 100 | 92 | Gq/11 | αq | - | 59 | - | scFv16 |
docosahexaenoic acid
|
small-molecule | Agonist | oleic acid, myristic acid, α-linolenic acid, docosahexaenoic acid | small-molecule | No | No | Zhang X, Guseinov AA, Jenkins L, Li K, Tikhonova IG, Milligan G, Zhang C | 10.1126/SCIADV.ADJ2384 | 2024-01-24 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | Cryo-EM | 8UNN | - | 3.4 | R | Active | 100 | 69 | Gs | αs | GTP bound, Class C | 59 | - | - |
(5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, Zn2+, noradrenaline | small-molecule | No | No | Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G | 10.1038/S41586-024-07153-1 | 2024-03-06 | Yes | |
5HT2A | 5-HT2A | 5-Hydroxytryptamine | A | Human | Cryo-EM | 8UWL | - | 2.8 | A | Active | 100 | 59 | Gq/11 | αq | Gi2-mini-Gq chimera | 58 | - | scFv16 |
lisuride
|
small-molecule | Agonist | 5-hydroxytryptamine, tryptamine | small-molecule | No | No | Lyu J, Kapolka N, Gumpper R, Alon A, Wang L, Jain MK, Barros-Alvarez X, Sakamoto K, Kim Y, DiBerto J, Kim K, Glenn IS, Tummino TA, Huang S, Irwin JJ, Tarkhanova OO, Moroz Y, Skiniotis G, Kruse AC, Shoichet BK, Roth BL | 10.1126/SCIENCE.ADN6354 | 2024-05-29 | Yes | |
EDNRB | ETB | Endothelin | A | Human | Cryo-EM | 8XGR | - | 3.2 | R | Active | 100 | 69 | Gi/o | αt1 | - | 59 | - | Camelid antibody VHH fragment |
ENDOTHELIN
|
protein | Agonist | endothelin-2, endothelin-3, endothelin-1 | peptide | No | No | - | - | 2024-04-03 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 3OAX | - | 2.6 | A | Inactive | 22 | 100 | - | - | - | - | - | - |
Retinal (11-cis)
|
small-molecule | Inverse agonist | - | - | No | No | Makino CL, Riley CK, Looney J, Crouch RK, Okada T | 10.1016/J.BPJ.2010.08.003 | 2011-01-19 | Yes | |
ADRB1 | β1 | Adrenoceptors | A | Wild turkey | X-ray | 3ZPR | 3ZPR_refined | 2.7 | B | Inactive | 0 | 61 | - | - | - | - | - | - |
CHEMBL1559535
|
small-molecule | Antagonist | - | - | No | No | Christopher JA, Brown J, Doré AS, Errey JC, Koglin M, Marshall FH, Myszka DG, Rich RL, Tate CG, Tehan B, Warne T, Congreve M. | 10.1021/jm400140q | 2013-04-03 | Yes | |
P2Y12 | P2Y12 | P2Y | A | Human | X-ray | 4PXZ | 4PXZ_refined | 2.5 | A | Active | 56 | 84 | - | - | - | - | BRIL | - |
2MeSADP
|
small-molecule | Agonist | ADP, ATP | small-molecule | No | No | Zhang J, Zhang K, Gao ZG, Paoletta S, Zhang D, Han GW, Li T, Ma L, Zhang W, Muller CE, Yang H, Jiang H, Cherezov V, Katritch V, Jacobson KA, Stevens RC, Wu B, Zhao Q | 10.1038/NATURE13288 | 2014-04-30 | Yes | |
OPRM | μ | Opioid | A | Mouse | X-ray | 5C1M | 5C1M_refined | 2.1 | A | Active | 100 | 74 | - | - | - | - | - | Antibody |
BU72
|
small-molecule | Agonist | - | - | No | No | Huang W, Manglik A, Venkatakrishnan AJ, Laeremans T, Feinberg EN, Sanborn AL, Kato HE, Livingston KE, Thorsen TS, Kling RC, Granier S, Gmeiner P, Husbands SM, Traynor JR, Weis WI, Steyaert J, Dror RO, Kobilka BK | 10.1038/NATURE14886 | 2015-08-05 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 5D6L | 5D6L_refined | 3.2 | A | Inactive | 0 | 68 | - | - | - | - | T4-Lysozyme | - |
Carazolol
|
small-molecule | Inverse agonist | (-)-noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, Zn2+, noradrenaline | small-molecule | No | No | Ma P, Weichert D, Aleksandrov LA, Jensen TJ, Riordan JR, Liu X, Kobilka BK, Caffrey M | 10.1038/NPROT.2017.057 | 2016-08-17 | Yes | |
GLP1R | GLP-1 | Glucagon | B1 | Human | X-ray | 5VEX | 5VEX_refined | 3.0 | B | Inactive | 0 | 57 | - | - | - | - | T4-Lysozyme | - |
NNC0640
|
small-molecule | NAM | glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide | peptide | No | No | Song G, Yang D, Wang Y, de Graaf C, Zhou Q, Jiang S, Liu K, Cai X, Dai A, Lin G, Liu D, Wu F, Wu Y, Zhao S, Ye L, Han GW, Lau J, Wu B, Hanson MA, Liu ZJ, Wang MW, Stevens RC | 10.1038/NATURE22378 | 2017-05-17 | Yes | |
OX2R | OX2 | Orexin | A | Human | X-ray | 5WS3 | 5WS3_refined | 2.3 | A | Inactive | 0 | 70 | - | - | - | - | Glycogen synthase | - |
EMPA
|
small-molecule | Antagonist | orexin-B, orexin-A | peptide | No | No | Suno R, Kimura KT, Nakane T, Yamashita K, Wang J, Fujiwara T, Yamanaka Y, Im D, Horita S, Tsujimoto H, Tawaramoto MS, Hirokawa T, Nango E, Tono K, Kameshima T, Hatsui T, Joti Y, Yabashi M, Shimamoto K, Yamamoto M, Rosenbaum DM, Iwata S, Shimamura T, Kobayashi T | 10.1016/J.STR.2017.11.005 | 2017-12-13 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 6FKC | 6FKC_refined | 2.5 | A | Active | 98 | 94 | - | - | - | - | - | - |
3-[1'-[(2~{S})-2-(4-chlorophenyl)-3-methyl-butanoyl]spiro[1,3-benzodioxole-2,4'-piperidine]-5-yl]propanoic acid
|
small-molecule | Agonist | - | - | No | No | Mattle D, Kuhn B, Aebi J, Bedoucha M, Kekilli D, Grozinger N, Alker A, Rudolph MG, Schmid G, Schertler GFX, Hennig M, Standfuss J, Dawson RJP | 10.1073/PNAS.1718084115 | 2018-04-04 | Yes | |
PD2R2 | DP2 | Prostanoid | A | Human | X-ray | 6D27 | 6D27_refined | 2.7 | A | Inactive | 24 | 81 | - | - | - | - | T4-Lysozyme | - |
CHEMBL179036
|
small-molecule | Antagonist | PGD2, PGF2α, PGD3, PGE2, PGJ2, thromboxane A2, PGI2 | small-molecule | No | No | Wang L, Yao D, Deepak RNVK, Liu H, Xiao Q, Fan H, Gong W, Wei Z, Zhang C | 10.1016/J.MOLCEL.2018.08.009 | 2018-10-03 | Yes | |
NK1R | NK1 | Tachykinin | A | Human | X-ray | 6E59 | 6E59_refined | 3.4 | A | Inactive | 0 | 70 | - | - | - | - | GlgA glycogen synthase | - |
L760735
|
small-molecule | Antagonist | neuropeptide-γ, neurokinin B, neuropeptide K, substance P, hemokinin 1, neurokinin A | peptide | No | No | Yin J, Chapman K, Clark LD, Shao Z, Borek D, Xu Q, Wang J, Rosenbaum DM | 10.1073/PNAS.1812717115 | 2018-12-12 | Yes | |
MTR1A | MT1 | Melatonin | A | Human | X-ray | 6ME4 | 6ME4_refined | 3.2 | A | Inactive | 1 | 83 | - | - | - | - | GlgA glycogen synthase | - |
2-iodo-melatonin
|
small-molecule | Agonist | melatonin | small-molecule | No | No | Stauch B, Johansson LC, McCorvy JD, Patel N, Han GW, Huang XP, Gati C, Batyuk A, Slocum ST, Ishchenko A, Brehm W, White TA, Michaelian N, Madsen C, Zhu L, Grant TD, Grandner JM, Shiriaeva A, Olsen RHJ, Tribo AR, Yous S, Stevens RC, Weierstall U, Katritch V, Roth BL, Liu W, Cherezov V | 10.1038/S41586-019-1141-3 | 2019-04-24 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | Cryo-EM | 6OYA | - | 3.3 | R | Active | 100 | 94 | Gi/o | αt1 | - | 59 | - | Camelid antibody VHH fragment |
Retinal (all-trans)
|
small-molecule | Agonist | - | - | No | No | - | - | 2019-07-24 | Yes | |
ACM5 | M5 | Acetylcholine (muscarinic) | A | Human | X-ray | 6OL9 | 6OL9_refined | 2.5 | A | Inactive | 3 | 53 | - | - | - | - | T4-Lysozyme | - |
tiotropium
|
small-molecule | Inverse agonist | acetylcholine | small-molecule | No | No | Vuckovic Z, Gentry PR, Berizzi AE, Hirata K, Varghese S, Thompson G, van der Westhuizen ET, Burger WAC, Rahmani R, Valant C, Langmead CJ, Lindsley CW, Baell JB, Tobin AB, Sexton PM, Christopoulos A, Thal DM | 10.1073/PNAS.1914446116 | 2019-12-11 | Yes | |
CNR1 | CB1 | Cannabinoid | A | Human | Cryo-EM | 6KPG | 6KPG_refined | 3.0 | R | Active | 100 | 60 | Gi/o | αi1 | - | 64 | - | scFv16 |
AM841
|
small-molecule | Agonist | anandamide, 2-arachidonoylglycerol | small-molecule | No | No | Hua T, Li X, Wu L, Iliopoulos-Tsoutsouvas C, Wang Y, Wu M, Shen L, Brust CA, Nikas SP, Song F, Song X, Yuan S, Sun Q, Wu Y, Jiang S, Grim TW, Benchama O, Stahl EL, Zvonok N, Zhao S, Bohn LM, Makriyannis A, Liu ZJ | 10.1016/J.CELL.2020.01.008 | 2020-02-12 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 6PEL | 6PEL_refined | 3.2 | A | Active | 100 | 93 | Gi/o | αt1 | Only H5 | 3 | - | - |
Citronellol
|
small-molecule | unknown | - | - | No | No | - | - | 2020-06-24 | Yes | |
ACM1 | M1 | Acetylcholine (muscarinic) | A | Human | X-ray | 6WJC | - | 2.6 | A | Inactive | 3 | 62 | - | - | - | - | T4-Lysozyme | - |
HYOSCYAMINE
muscarinic toxin 7 |
small-molecule peptide |
Antagonist NAM |
acetylcholine | small-molecule | No | No | Maeda S, Xu J, N Kadji FM, Clark MJ, Zhao J, Tsutsumi N, Aoki J, Sunahara RK, Inoue A, Garcia KC, Kobilka BK | 10.1126/SCIENCE.AAX2517 | 2020-07-08 | Yes | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 6XOX | - | 3.1 | R | Active | 100 | 82 | Gs | αs | - | 56 | - | scFv16 Nanobody-35 |
orforglipron
|
small-molecule | Agonist | glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide | peptide | No | No | Kawai T, Sun B, Yoshino H, Feng D, Suzuki Y, Fukazawa M, Nagao S, Wainscott DB, Showalter AD, Droz BA, Kobilka TS, Coghlan MP, Willard FS, Kawabe Y, Kobilka BK, Sloop KW | 10.1073/PNAS.2014879117 | 2020-11-18 | Yes | |
DRD1 | D1 | Dopamine | A | Human | Cryo-EM | 7JVQ | 7JVQ_refined | 3.0 | R | Active | 100 | 64 | Gs | αs | Engineered G alpha | 60 | - | Nanobody-35 |
apomorphine
|
small-molecule | Agonist | (-)-noradrenaline, L-NOREPINEPHRINE, dopamine, 5-hydroxytryptamine, noradrenaline | small-molecule | No | No | 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 | Yes | |
GABR2 | GABAB2 | GABAB | C | Human | Cryo-EM | 7EB2 | - | 3.5 | D | Active | - | 72 | Gi/o | αi1 | - | 99 | - | scFv16 |
(-)-baclofen
BHFF |
small-molecule small-molecule |
Agonist PAM |
- | - | No | No | 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 | Yes | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 7DUR | - | 3.3 | R | Active | 100 | 80 | Gs | αs | - | 60 | - | Nanobody-35 |
N-Tert-butyl-6,7-dichloroquinoxalin-2-amine
|
small-molecule | Ago-PAM | glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide | peptide | No | No | 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 | Yes | |
S1PR5 | S1P5 | Lysophospholipid (S1P) | A | Human | Cryo-EM | 7EW1 | 7EW1_refined | 3.4 | A | Active | 100 | 68 | Gi/o | αi1 | - | 64 | - | scFv16 |
siponimod
|
small-molecule | Agonist | sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine | small-molecule | No | No | 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 | Yes | |
MC4R | MC4 | Melanocortin | A | Human | Cryo-EM | 7F54 | - | 3.0 | R | Active | 100 | 82 | Gs | αs | - | 58 | - | Nanobody-35 |
afamelanotide
|
peptide | Agonist | β-MSH, ACTH, γ-MSH, α-MSH, agouti-related protein | peptide | No | No | 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 | Yes | |
GP139 | GPR139 | A orphans | A | Human | Cryo-EM | 7VUG | 7VUG_refined | 3.2 | R | Active | 100 | 80 | Gi/o | αi1 | - | 62 | - | scFv16 |
JNJ-63533054
|
small-molecule | Agonist | L-tryptophan, L-phenylalanine | small-molecule | No | No | 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 | Yes | |
MSHR | MC1 | Melanocortin | A | Human | Cryo-EM | 7F4F | - | 2.9 | R | Active | 100 | 85 | Gs | αs | - | 59 | - | scFv16 |
CHEMBL407070
|
protein | Agonist | ACTH, γ-MSH, β-MSH, α-MSH | peptide | No | No | 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 | Yes | |
CALCR | CT | Calcitonin | B1 | Human | Cryo-EM | 7TZF | - | 2.4 | R | Active | 100 | 77 | Gs | αs | - | 59 | - | Nanobody-35 RAMP3 |
amylin peptide
|
peptide | Agonist | adrenomedullin, amylin, β-CGRP, calcitonin, α-CGRP, adrenomedullin 2/intermedin | peptide | No | No | 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 | Yes | |
NMUR2 | NMU2 | Neuromedin U | A | Human | Cryo-EM | 7W55 | - | 2.8 | R | Active | 100 | 73 | Gq/11 | αq | - | 60 | - | scFv16 |
Neuromedin U-25 (human)
|
peptide | Agonist | neuromedin U-23, neuromedin U-25, neuromedin S-33, neuromedin S-36 | peptide | No | No | You C, Zhang Y, Xu P, Huang S, Yin W, Eric Xu H, Jiang Y | 10.1038/S41467-022-29683-W | 2022-04-20 | Yes | |
CX3C1 | CX3CR1 | Chemokine | A | Human | Cryo-EM | 7XBW | 7XBW_refined | 2.8 | R | Active | 10 | 81 | Gi/o | αi1 | - | 61 | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | CX3CL1 | peptide | No | No | Lu M, Zhao W, Han S, Lin X, Xu T, Tan Q, Wang M, Yi C, Chu X, Yang W, Zhu Y, Wu B, Zhao Q | 10.1126/SCIADV.ABN8048 | 2022-07-13 | Yes | |
SSR4 | SST4 | Somatostatin | A | Human | Cryo-EM | 7XMS | - | 2.9 | R | Active | 100 | 71 | Gi/o | αi1 | - | 63 | - | scFv16 |
SOMATOSTATIN
|
protein | Agonist | SRIF-14, CST-17, SRIF-28, cortistatin-14 | peptide | No | No | 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 | Yes | |
SMO | SMO | Frizzled | F | Mouse | Cryo-EM | 8CXO | 8CXO_refined | 3.7 | A | Inactive | 13 | 43 | - | - | - | - | GlgA glycogen synthase | - |
Cholesterol
|
small-molecule | Agonist | - | - | No | No | Zhang K, Wu H, Hoppe N, Manglik A, Cheng Y | 10.1038/S41467-022-32125-2 | 2022-08-03 | Yes | |
5HT2B | 5-HT2B | 5-Hydroxytryptamine | A | Human | Cryo-EM | 7SRS | - | 3.3 | R | Active | 100 | 60 | Beta | Beta-arrestin-1 | - | 85 | - | Fab light chain Fab heavy chain Fab30 heavy chain Fab30 light chain |
Lysergide
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | No | No | 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 | Yes | |
S1PR1 | S1P1 | Lysophospholipid (S1P) | A | Human | Cryo-EM | 7VIH | 7VIH_refined | 3.0 | F | Active | 100 | 73 | Gi/o | αi1 | - | 64 | - | scFv16 |
icanbelimod
|
small-molecule | Agonist | sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine | small-molecule | No | No | 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 | Yes | |
SSR2 | SST2 | Somatostatin | A | Human | Cryo-EM | 7Y27 | 7Y27_refined | 3.5 | E | Active | 100 | 74 | Gq/11 | αq | Mini-Gq | 60 | - | scFv16 |
SOMATOSTATIN
|
protein | Agonist | SRIF-14, CST-17, SRIF-28, cortistatin-14 | peptide | No | No | Chen S, Teng X, Zheng S | 10.1038/S41589-022-01130-3 | 2022-10-19 | Yes | |
OPRM | μ | Opioid | A | Human | Cryo-EM | 8EFL | 8EFL_refined | 3.2 | R | Active | 100 | 72 | Gi/o | αi1 | - | 64 | - | scFv16 |
CHEMBL4452384
|
small-molecule | Agonist | dynorphin A, endomorphin-2, [Leu]enkephalin, endomorphin-1, [Met]enkephalin, dynorphin B, β-endorphin, dynorphin A-(1-13), dynorphin A-(1-8) | peptide | No | No | 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 | Yes | |
C5AR1 | C5a1 | Complement peptide | A | Human | Cryo-EM | 7Y66 | - | 2.9 | D | Active | 100 | 80 | Gi/o | αi1 | - | 63 | - | scFv16 |
BM213
|
peptide | Agonist | C5a des-Arg, C3a, C5a, ribosomal protein S19 | peptide | No | No | 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 | Yes | |
GPR20 | GPR20 | A orphans | A | Human | Cryo-EM | 8HSC | - | 3.2 | R | Active | 100 | 76 | Gi/o | αi1 | - | 62 | BRIL | Antibody fab fragment light chain Antibody fab fragment heavy chain scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Lin X, Jiang S, Wu Y, Wei X, Han GW, Wu L, Liu J, Chen B, Zhang Z, Zhao S, Cherezov V, Xu F | 10.1038/S41421-023-00520-8 | 2023-03-08 | Yes | |
TAAR9 | TAAR9 | A orphans | A | Mouse | Cryo-EM | 8IW1 | - | 3.4 | R | Active | 100 | 78 | Gs | αolf | Golf-Gi chimera | 59 | - | scFv16 |
2-Phenylethanaminium
|
small-molecule | Agonist | - | - | No | No | 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 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 8CIC | - | 2.1 | A | Inactive | 0 | 71 | - | - | - | - | BRIL | - |
AB928
|
small-molecule | Antagonist | adenosine | small-molecule | No | No | Claff T, Schlegel JG, Voss JH, Vaassen VJ, Weisse RH, Cheng RKY, Markovic-Mueller S, Bucher D, Strater N, Muller CE | 10.1038/S42004-023-00894-6 | 2023-05-31 | Yes | |
CNR2 | CB2 | Cannabinoid | A | Human | Cryo-EM | 8GUQ | 8GUQ_refined | 3.1 | R | Active | 100 | 81 | Gi/o | αi1 | - | 62 | - | scFv16 |
olorinab
|
small-molecule | Agonist | anandamide, 2-arachidonoylglycerol | small-molecule | No | No | 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 | Yes | |
AGRE5 | ADGRE5 | ADGRE | B2 | Human | Cryo-EM | 7YDP | - | 3.1 | R | Active | 100 | 32 | Gs | αs | Mini-Gs | 59 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | 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 | Yes | |
PF2R | FP | Prostanoid | A | Human | Cryo-EM | 8IUL | - | 2.8 | R | Active | 100 | 82 | Gq/11 | αq | - | 60 | - | scFv16 |
latanoprost (free acid form)
|
small-molecule | Agonist | PGD2, PGF2α, PGE2, thromboxane A2, PGI2 | small-molecule | No | No | 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 | Yes | |
GRM2 | mGlu2 | Metabotropic glutamate | C | Human | Cryo-EM | 8JD2 | - | 2.8 | 2 | Active | - | 86 | - | - | - | - | - | - |
L-glutamic acid
|
small-molecule | Agonist | L-glutamic acid | small-molecule | No | No | Wang X, Wang M, Xu T, Feng Y, Shao Q, Han S, Chu X, Xu Y, Lin S, Zhao Q, Wu B | 10.1038/S41422-023-00830-2 | 2023-06-21 | Yes | |
CRFR1 | CRF1 | Corticotropin-releasing factor | B1 | Human | X-ray | 8GTI | - | 2.2 | A | Inactive | 16 | 63 | - | - | - | - | Endolysin | - |
8-(4-bromo-2,6-dimethoxyphenyl)-N-butyl-N-(cyclopropylmethyl)-2,7-dimethylpyrazolo[1,5-a][1,3,5]triazin-4-amine
|
small-molecule | Antagonist | urocortin 2, urocortin 1, corticotrophin-releasing hormone | peptide | No | No | Kim H, Lim T, Ha GE, Lee JY, Kim JW, Chang N, Kim SH, Kim KH, Lee J, Cho Y, Kim BW, Abrahamsson A, Kim SH, Kim HJ, Park S, Lee SJ, Park J, Cheong E, Kim BM, Cho HS | 10.1038/S12276-023-01082-1 | 2023-09-13 | Yes | |
GASR | CCK2 | Cholecystokinin | A | Human | Cryo-EM | 8IA7 | 8IA7_refined | 3.1 | R | Active | 100 | 62 | Gq/11 | αq | - | 61 | - | - |
CHEMBL216166
|
protein | Agonist | gastrin-71, desulfated gastrin-14, CCK-4, desulfated gastrin-17, gastrin-14, CCK-39, desulfated gastrin-34, desulfated gastrin-71, gastrin-34, CCK-33, desulfated cholecystokinin-8, gastrin-17, CCK-8, CCK-58 | peptide | No | No | 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 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | Cryo-EM | 8JJ8 | - | 3.2 | F | Active | 98 | 68 | - | - | - | - | BRIL | - |
ARFORMOTEROL
|
small-molecule | Agonist (partial) | (-)-noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, Zn2+, noradrenaline | small-molecule | No | No | Guo Q, He B, Zhong Y, Jiao H, Ren Y, Wang Q, Ge Q, Gao Y, Liu X, Du Y, Hu H, Tao Y | 10.1038/S41589-023-01389-0 | 2023-09-06 | Yes | |
GP161 | GPR161 | A orphans | A | Human | Cryo-EM | 8KH4 | 8KH4_refined | 3.1 | A | Active | 100 | 50 | Gs | αs | - | 58 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | 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 | Yes | |
GP101 | GPR101 | A orphans | A | Human | Cryo-EM | 8W8R | - | 3.3 | R | Active | 100 | 55 | Gs | αs | - | 60 | - | scFv16 |
1-(4-Methylpyridin-2-yl)-3-[3-(trifluoromethyl)phenyl]thiourea
|
small-molecule | Agonist | - | - | No | No | 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 | Yes | |
5HT1A | 5-HT1A | 5-Hydroxytryptamine | A | Human | Cryo-EM | 8FYX | - | 2.6 | R | Active | 100 | 68 | Gi/o | αi1 | - | 66 | BRIL | - |
buspirone
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | No | No | Warren AL, Lankri D, Cunningham MJ, Serrano IC, Parise LF, Kruegel AC, Duggan P, Zilberg G, Capper MJ, Havel V, Russo SJ, Sames D, Wacker D | 10.1038/S41586-024-07403-2 | 2024-05-15 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | Cryo-EM | 8GG1 | - | 3.0 | R | Active | 100 | 68 | Gs | αs | - | 59 | - | - |
(5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, Zn2+, noradrenaline | small-molecule | No | No | Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G | 10.1038/S41586-024-07153-1 | 2024-03-06 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | Cryo-EM | 8GGZ | - | 3.9 | R | Active | 97 | 68 | - | - | - | - | - | - |
(5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, Zn2+, noradrenaline | small-molecule | No | No | Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G | 10.1038/S41586-024-07153-1 | 2024-03-06 | Yes | |
HCAR2 | HCA2 | Hydroxycarboxylic acid | A | Human | Cryo-EM | 8J6J | 8J6J_refined | 2.8 | R | Active | 100 | 85 | Gi/o | αi1 | - | 61 | - | scFv16 |
GSK256073
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | No | No | Zhu S, Yuan Q, Li X, He X, Shen S, Wang D, Li J, Cheng X, Duan X, Xu HE, Duan J | 10.1016/J.CELREP.2023.113406 | 2024-01-10 | Yes | |
FZD3 | FZD3 | Frizzled | F | Human | Cryo-EM | 8QW4 | - | 2.9 | A | Active | 98 | 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 | |
CXCR4 | CXCR4 | Chemokine | A | Human | Cryo-EM | 8U4Q | - | 3.4 | R | Active | 100 | 84 | Gi/o | αi1 | - | 62 | - | REGN7663 Fab light chain |
REGN7663 Fab heavy chain
|
protein | Agonist | CXCL12γ, CXCL12β, CXCL12ε, CXCL12φ, CXCL12δ, CXCL12, CXCL12α | peptide | No | No | Saotome K, McGoldrick LL, Ho JH, Ramlall TF, Shah S, Moore MJ, Kim JH, Leidich R, Olson WC, Franklin MC | 10.1038/S41594-024-01397-1 | 2024-03-13 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 2X72 | 2X72_refined | 3.0 | A | Active | 100 | 94 | Gi/o | αt1 | Only H5 | 3 | - | - |
Retinal (all-trans)
|
small-molecule | Agonist | - | - | No | No | Standfuss J, Edwards PC, D'Antona A, Fransen M, Xie G, Oprian DD, Schertler GF | 10.1038/NATURE09795 | 2011-03-16 | Yes | |
OPRX | NOP | Opioid | A | Human | X-ray | 4EA3 | 4EA3_refined | 3.0 | A | Inactive | 9 | 75 | - | - | - | - | BRIL | - |
compound 24 [PMID: 16451050]
|
small-molecule | Antagonist | nociceptin/orphanin FQ | peptide | No | No | Thompson AA, Liu W, Chun E, Katritch V, Wu H, Vardy E, Huang XP, Trapella C, Guerrini R, Calo G, Roth BL, Cherezov V, Stevens RC | 10.1038/NATURE11085 | 2012-04-25 | Yes | |
FFAR1 | FFA1 | Free fatty acid | A | Human | X-ray | 4PHU | 4PHU_refined | 2.3 | A | Active | 56 | 90 | - | - | - | - | T4-Lysozyme | - |
fasiglifam
|
small-molecule | Allosteric agonist | oleic acid, myristic acid, α-linolenic acid, docosahexaenoic acid | small-molecule | No | No | Srivastava A, Yano J, Hirozane Y, Kefala G, Gruswitz F, Snell G, Lane W, Ivetac A, Aertgeerts K, Nguyen J, Jennings A, Okada K | 10.1038/NATURE13494 | 2014-07-16 | Yes | |
GRM5 | mGlu5 | Metabotropic glutamate | C | Human | X-ray | 5CGC | 5CGC_refined | 3.1 | A | Inactive | - | 20 | - | - | - | - | T4-Lysozyme | - |
CHEMBL3603915
|
small-molecule | NAM | L-glutamic acid | small-molecule | No | No | Christopher JA, Aves SJ, Bennett KA, Doré AS, Errey JC, Jazayeri A, Marshall FH, Okrasa K, Serrano-Vega MJ, Tehan BG, Wiggin GR, Congreve M. | 10.1021/acs.jmedchem.5b00892 | 2015-08-12 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 5DYS | 5DYS_refined | 2.3 | A | Active | 98 | 94 | - | - | - | - | - | - |
Retinal (all-trans)
|
small-molecule | Agonist | - | - | No | No | Singhal A, Guo Y, Matkovic M, Schertler G, Deupi X, Yan EC, Standfuss J | 10.15252/EMBR.201642671 | 2016-08-10 | Yes | |
PAR2 | PAR2 | Proteinase-activated | A | Human | X-ray | 5NDZ | 5NDZ_refined | 3.6 | A | Active | 56 | 74 | - | - | - | - | BRIL | - |
AZ3451
|
small-molecule | Allosteric antagonist | - | - | No | No | Cheng RKY, Fiez-Vandal C, Schlenker O, Edman K, Aggeler B, Brown DG, Brown GA, Cooke RM, Dumelin CE, Dore AS, Geschwindner S, Grebner C, Hermansson NO, Jazayeri A, Johansson P, Leong L, Prihandoko R, Rappas M, Soutter H, Snijder A, Sundstrom L, Tehan B, Thornton P, Troast D, Wiggin G, Zhukov A, Marshall FH, Dekker N | 10.1038/NATURE22309 | 2017-05-03 | Yes | |
DRD4 | D4 | Dopamine | A | Human | X-ray | 5WIV | - | 2.1 | A | Inactive | 1 | 65 | - | - | - | - | BRIL | - |
[3H]NEMONAPRIDE
|
small-molecule | Antagonist | dopamine | small-molecule | No | No | Wang S, Wacker D, Levit A, Che T, Betz RM, McCorvy JD, Venkatakrishnan AJ, Huang XP, Dror RO, Shoichet BK, Roth BL | 10.1126/SCIENCE.AAN5468 | 2017-10-18 | Yes | |
DRD2 | D2 | Dopamine | A | Human | X-ray | 6CM4 | 6CM4_refined | 2.9 | A | Inactive | 0 | 59 | - | - | - | - | T4-Lysozyme | - |
risperidone
|
small-molecule | Inverse agonist | dopamine | small-molecule | No | No | Wang S, Che T, Levit A, Shoichet BK, Wacker D, Roth BL | 10.1038/NATURE25758 | 2018-03-14 | Yes | |
FZD4 | FZD4 | Frizzled | F | Human | X-ray | 6BD4 | 6BD4_refined | 2.4 | A | Inactive | 19 | 61 | - | - | - | - | Rubredoxin | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Yang S, Wu Y, Xu TH, de Waal PW, He Y, Pu M, Chen Y, DeBruine ZJ, Zhang B, Zaidi SA, Popov P, Guo Y, Han GW, Lu Y, Suino-Powell K, Dong S, Harikumar KG, Miller LJ, Katritch V, Xu HE, Shui W, Stevens RC, Melcher K, Zhao S, Xu F | 10.1038/S41586-018-0447-X | 2018-08-22 | Yes | |
PTH1R | PTH1 | Parathyroid hormone | B1 | Human | X-ray | 6FJ3 | - | 2.5 | A | Inactive | 0 | 62 | - | - | - | - | GlgA glycogen synthase | - |
ePTH
|
peptide | Agonist (partial) | PTH, PTHrP, PTHrP-(1-36), TIP39 | peptide | No | No | Ehrenmann J, Schoppe J, Klenk C, Rappas M, Kummer L, Dore AS, Pluckthun A | 10.1038/S41594-018-0151-4 | 2018-11-21 | Yes | |
NTR1 | NTS1 | Neurotensin | A | Human | Cryo-EM | 6OS9 | 6OS9_refined | 3.0 | R | Active | 100 | 73 | Gi/o | αi1 | - | 62 | - | scFv16 |
JMV449
|
peptide | Agonist | neurotensin, large neurotensin, large neuromedin N, neuromedin N | peptide | No | No | 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 | Yes | |
OX1R | OX1 | Orexin | A | Human | X-ray | 6TQ9 | 6TQ9_refined | 2.7 | B | Inactive | 0 | 71 | - | - | - | - | - | - |
SB-408124
|
small-molecule | Antagonist | orexin-B, orexin-A | peptide | No | No | Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA. | 10.1021/acs.jmedchem.9b01787 | 2020-01-01 | Yes | |
PACR | PAC1 | VIP and PACAP | B1 | Human | Cryo-EM | 6M1H | - | 3.6 | A | Active | 100 | 73 | Gs | αs | - | 55 | - | Nanobody-35 |
maxadilan
|
peptide | Agonist | PHI, PHM, PHV, PACAP-38, VIP, PACAP-27 | peptide | No | No | Wang J, Song X, Zhang D, Chen X, Li X, Sun Y, Li C, Song Y, Ding Y, Ren R, Harrington EH, Hu LA, Zhong W, Xu C, Huang X, Wang HW, Ma Y | 10.1038/S41422-020-0280-2 | 2020-03-11 | Yes | |
GPBAR | GPBA | Bile acid | A | Human | Cryo-EM | 7CFN | 7CFN_refined | 3.0 | R | Active | 100 | 83 | Gs | αs | - | 59 | - | Nanobody-35 |
INT-777
INT-777 |
small-molecule small-molecule |
Agonist PAM |
chenodeoxycholic acid, cholic acid, deoxycholic acid, lithocholic acid | small-molecule | No | No | Yang F, Mao C, Guo L, Lin J, Ming Q, Xiao P, Wu X, Shen Q, Guo S, Shen DD, Lu R, Zhang L, Huang S, Ping Y, Zhang C, Ma C, Zhang K, Liang X, Shen Y, Nan F, Yi F, Luca VC, Zhou J, Jiang C, Sun JP, Xie X, Yu X, Zhang Y | 10.1038/S41586-020-2569-1 | 2020-09-09 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 6LPL | 6LPL_refined | 2.0 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
ZM-241385
|
small-molecule | Antagonist | adenosine | small-molecule | No | No | Ihara K, Hato M, Nakane T, Yamashita K, Kimura-Someya T, Hosaka T, Ishizuka-Katsura Y, Tanaka R, Tanaka T, Sugahara M, Hirata K, Yamamoto M, Nureki O, Tono K, Nango E, Iwata S, Shirouzu M | 10.1038/S41598-020-76277-X | 2020-11-25 | Yes | |
NTR1 | NTS1 | Neurotensin | A | Rat | X-ray | 6Z4Q | - | 2.9 | A | Inactive | 30 | 75 | - | - | - | - | DARPin D12 | - |
SR142948A
|
small-molecule | Inverse agonist | neuromedin N, neurotensin | peptide | No | No | Deluigi M, Klipp A, Klenk C, Merklinger L, Eberle SA, Morstein L, Heine P, Mittl PRE, Ernst P, Kamenecka TM, He Y, Vacca S, Egloff P, Honegger A, Pluckthun A | 10.1126/sciadv.abe5504 | 2021-02-10 | Yes | |
5HT1A | 5-HT1A | 5-Hydroxytryptamine | A | Human | Cryo-EM | 7E2X | - | 3.0 | R | Active | 100 | 66 | Gi/o | αi1 | - | 62 | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | 5-hydroxytryptamine | small-molecule | No | No | 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 | Yes | |
GRM2 | mGlu2 | Metabotropic glutamate | C | Human | X-ray | 7EPE | 7EPE_refined | 2.5 | A | Inactive | - | 28 | - | - | - | - | Flavodoxin | - |
CHEMBL3894759
|
small-molecule | NAM | L-glutamic acid | small-molecule | No | No | Du J, Wang D, Fan H, Xu C, Tai L, Lin S, Han S, Tan Q, Wang X, Xu T, Zhang H, Chu X, Yi C, Liu P, Wang X, Zhou Y, Pin JP, Rondard P, Liu H, Liu J, Sun F, Wu B, Zhao Q | 10.1038/S41586-021-03641-W | 2021-06-23 | Yes | |
V2R | V2 | Vasopressin and oxytocin | A | Human | Cryo-EM | 7DW9 | - | 2.6 | R | Active | 100 | 75 | Gs | αs | - | 60 | - | Nanobody-35 scFv16 |
vasopressin
|
peptide | Agonist | oxytocin, vasopressin | peptide | No | No | Zhou F, Ye C, Ma X, Yin W, Croll TI, Zhou Q, He X, Zhang X, Yang D, Wang P, Xu HE, Wang MW, Jiang Y | 10.1038/S41422-021-00480-2 | 2021-07-21 | Yes | |
GRM1 | mGlu1 | Metabotropic glutamate | C | Human | Cryo-EM | 7DGE | 7DGE_refined | 3.7 | A | Intermediate | - | 66 | - | - | - | - | - | Nanobody-43 |
quisqualate
|
small-molecule | Agonist | L-glutamic acid | small-molecule | No | No | Zhang J, Qu L, Wu L, Tang X, Luo F, Xu W, Xu Y, Liu ZJ, Hua T | 10.1007/S13238-020-00808-5 | 2021-09-22 | Yes | |
GP158 | GPR158 | C Orphans | C | Human | Cryo-EM | 7EWP | 7EWP_refined | 4.3 | A | Inactive | - | 47 | - | - | - | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Jeong E, Kim Y, Jeong J, Cho Y | 10.1038/S41467-021-27147-1 | 2021-12-01 | Yes | |
ADA1B | α1B | Adrenoceptors | A | Human | X-ray | 7B6W | - | 2.9 | A | Inactive | 1 | 51 | - | - | - | - | DARPin D12 | - |
(+)-cyclazosin
|
small-molecule | Inverse agonist | (-)-noradrenaline, (-)-adrenaline | small-molecule | No | No | Deluigi M, Morstein L, Schuster M, Klenk C, Merklinger L, Cridge RR, de Zhang LA, Klipp A, Vacca S, Vaid TM, Mittl PRE, Egloff P, Eberle SA, Zerbe O, Chalmers DK, Scott DJ, Pluckthun A | 10.1038/s41467-021-27911-3 | 2022-01-12 | Yes | |
FPR2 | FPR2/ALX | Formylpeptide | A | Human | Cryo-EM | 7T6U | - | 2.9 | R | Active | 100 | 85 | Gi/o | αi1 | - | 62 | - | - |
synthetic peptide
|
peptide | Agonist | resolvin D1, humanin, aspirin triggered lipoxin A4, serum amyloid A, LL-37, aspirin-triggered resolvin D1, PrP106-126, LXA4, annexin I | peptide | No | No | 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 | Yes | |
CALCR | CT | Calcitonin | B1 | Human | Cryo-EM | 7TYY | - | 3.0 | R | Active | 100 | 78 | Gs | αs | - | 58 | - | Nanobody-35 |
calcitonin (salmon synthetic)
|
small-molecule | Agonist | adrenomedullin, amylin, β-CGRP, calcitonin, α-CGRP, adrenomedullin 2/intermedin | peptide | No | No | 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 | Yes | |
AGRF1 | ADGRF1 | ADGRF | B2 | Human | Cryo-EM | 7WU5 | - | 3.0 | R | Active | 100 | 31 | Gi/o | αi1 | Mini-Gi1 | 58 | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | 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 | Yes | |
BKRB2 | B2 | Bradykinin | A | Human | Cryo-EM | 7F6H | 7F6H_refined | 2.9 | A | Active | 100 | 78 | Gq/11 | αq | - | 63 | - | - |
bradykinin
|
peptide | Agonist | [des-Arg10]kallidin, bradykinin, Lys-[Hyp3]-bradykinin, [Hyp3]bradykinin, [des-Arg9]bradykinin, T-kinin, kallidin | peptide | No | No | Shen J, Zhang D, Fu Y, Chen A, Yang X, Zhang H | 10.1038/S41467-022-28399-1 | 2022-01-05 | Yes | |
CNR1 | CB1 | Cannabinoid | A | Human | Cryo-EM | 7WV9 | - | 3.4 | R | Active | 100 | 61 | Gi/o | αi2 | - | 63 | - | scFv16 |
CP55940
6-methyl-3-[(1S)-2-nitro-1-thiophen-2-yl-ethyl]-2-phenyl-1H-indole |
small-molecule small-molecule |
Agonist PAM |
anandamide, 2-arachidonoylglycerol | small-molecule | No | No | Yang X, Wang X, Xu Z, Wu C, Zhou Y, Wang Y, Lin G, Li K, Wu M, Xia A, Liu J, Cheng L, Zou J, Yan W, Shao Z, Yang S | 10.1038/S41589-022-01038-Y | 2022-06-15 | Yes | |
ACKR3 | ACKR3 | Chemokine | A | Human | Cryo-EM | 7SK3 | 7SK3_refined | 3.8 | A | Active | 97 | 84 | - | - | - | - | - | CID25 Fab light chain CID25 Fab heavy chain CID24 Fab light chain CID24 Fab heavy chain |
CXCL12α
|
peptide | Agonist | CXCL11, CXCL12α | peptide | No | No | - | - | 2022-07-27 | Yes | |
OPRM | μ | Opioid | A | Human | Cryo-EM | 8EFB | 8EFB_refined | 3.2 | R | Active | 100 | 71 | Gi/o | αi1 | - | 64 | - | scFv16 |
OLICERIDINE
|
small-molecule | Agonist | dynorphin A, endomorphin-2, [Leu]enkephalin, endomorphin-1, [Met]enkephalin, dynorphin B, β-endorphin, dynorphin A-(1-13), dynorphin A-(1-8) | peptide | No | No | 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 | Yes | |
NPY2R | Y2 | Neuropeptide Y | A | Human | Cryo-EM | 7YOO | 7YOO_refined | 3.1 | R | Active | 96 | 79 | - | - | - | - | - | - |
neuropeptide Y
|
peptide | Agonist | PYY-(3-36), neuropeptide Y, pancreatic polypeptide, neuropeptide Y-(3-36), peptide YY | peptide | No | No | 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 | Yes | |
FFAR4 | FFA4 | Free fatty acid | A | Human | Cryo-EM | 8ID3 | 8ID3_refined | 3.1 | R | Active | 100 | 81 | Gi/o | αi1 | - | 64 | - | scFv16 |
9-Hydroxyoctadecanoic acid
|
small-molecule | Agonist | linoleic acid, myristic acid, α-linolenic acid, oleic acid | small-molecule | No | No | 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 | Yes | |
TAAR9 | TAAR9 | A orphans | A | Mouse | Cryo-EM | 8IWE | - | 3.4 | R | Active | 97 | 85 | - | - | - | - | - | - |
SPERMIDINE
|
small-molecule | Agonist | - | - | No | No | 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 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 7XK9 | - | 3.4 | A | Active | 98 | 69 | - | - | - | - | T4-Lysozyme | Camelid Antibody Fragment |
CHEMBL6913
|
small-molecule | Agonist | (-)-noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, Zn2+, noradrenaline | small-molecule | No | No | - | - | 2023-04-26 | Yes | |
C3AR | C3a | Complement peptide | A | Human | Cryo-EM | 8HK3 | 8HK3_refined | 3.2 | C | Active | 100 | 59 | Gi/o | αi1 | - | 63 | - | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | C3a, C5a | peptide | No | No | Wang Y, Liu W, Xu Y, He X, Yuan Q, Luo P, Fan W, Zhu J, Zhang X, Cheng X, Jiang Y, Xu HE, Zhuang Y | 10.1038/S41589-023-01339-W | 2023-05-10 | Yes | |
CNR2 | CB2 | Cannabinoid | A | Human | Cryo-EM | 8GUR | 8GUR_refined | 2.8 | R | Active | 100 | 78 | Gi/o | αi1 | - | 64 | - | scFv16 | CP55940 |