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RECEPTOR
STRUCTURE
SIGNAL PROTEIN
AUXILIARY PROTEIN
STRUCTURE LIGAND
PHYSIOLOGICAL LIGAND
SODIUM ION SITE
REFERENCE
ANNOTATED
UniProt
IUPHAR Receptor family Cl. Species Method
PDB
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
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
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
small-molecule Agonist PGD2, PGF, 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
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
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
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, PGF, 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, PGF, 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, PGF, 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, PGF, 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