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RECEPTOR
STRUCTURE
SIGNAL PROTEIN
AUXILIARY PROTEIN
STRUCTURE LIGAND
ENDOGENOUS 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 Function Name Type D2x50
S3x39
Sodium in
structure
Authors Reference PDB Date
OPSD Rhodopsin Opsins A Bovine X-ray 2I35 - 3.8 A Inactive 22 94 - - - - - - Retinal (11-cis)
small-molecule Inverse agonist - - No No - - 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 - 10.1021/BI0155091 2001-07-04 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 - 10.1126/SCIENCE.289.5480.739 2000-08-04 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 1L9H - 2.6 A Inactive 22 98 - - - - - - Retinal (11-cis)
small-molecule Inverse agonist - - No No - 10.1073/PNAS.082666399 2002-05-15 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 2RH1 - 2.4 A Inactive 0 68 - - - - T4-Lysozyme - Carazolol
small-molecule Inverse agonist L-NOREPINEPHRINE, (-)-noradrenaline, Zn2+, noradrenaline, (-)-adrenaline small-molecule No No - 10.1126/SCIENCE.1150577 2007-10-30 Yes
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 - 10.1016/J.JMB.2004.07.044 2004-10-12 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 2HPY - 2.8 B Inactive 22 100 - - - - - - Retinal (all-trans)
small-molecule Agonist - - No No - 10.1073/PNAS.0601765103 2006-08-22 Yes
OPSD Rhodopsin Opsins A Japanese flying squid X-ray 2ZIY - 3.7 A Inactive 17 83 - - - - - - Retinal (11-cis)
small-molecule Inverse agonist - - No No - 10.1074/JBC.C800040200 2008-05-06 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 3C9M - 3.4 A Inactive 22 94 - - - - - - Retinal (11-cis)
small-molecule Inverse agonist - - No No - 10.1107/S0907444908017162 2008-08-05 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 - 10.1016/J.JMB.2004.08.090 2003-11-20 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 2PED - 3.0 B Inactive 22 100 - - - - - - Retinal (9-cis)
small-molecule Inverse agonist - - No No - 10.1529/BIOPHYSJ.107.108225 2007-10-30 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 2I37 2I37_refined 4.2 A Inactive 22 91 - - - - - - Apo (no ligand)
none Apo (no ligand) - - No No - 10.1073/PNAS.0608022103 2006-10-17 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 2I36 - 4.1 A Inactive 22 94 - - - - - - Apo (no ligand)
none Apo (no ligand) - - No No - - 2006-10-17 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 2J4Y - 3.4 B Inactive 22 94 - - - - - - Retinal (11-cis)
small-molecule Inverse agonist - - No No - 10.1016/J.JMB.2007.03.007 2007-09-25 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 2G87 2G87_refined 2.6 A Inactive 22 100 - - - - - - Retinal (all-trans)
small-molecule Agonist - - No No - 10.1002/ANIE.200600595 2006-09-02 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 2R4R 2R4R_refined 3.4 A Inactive 1 52 - - - - - Antibody - - - L-NOREPINEPHRINE, (-)-noradrenaline, Zn2+, noradrenaline, (-)-adrenaline small-molecule No No - 10.1038/NATURE06325 2007-11-06 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 3C9L 3C9L_refined 2.7 A Inactive 22 94 - - - - - - Retinal (11-cis)
small-molecule Inverse agonist - - No No - - 2008-08-05 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 2R4S 2R4S_refined 3.4 A Inactive 1 52 - - - - - Antibody - - - L-NOREPINEPHRINE, (-)-noradrenaline, Zn2+, noradrenaline, (-)-adrenaline small-molecule No No - - 2007-11-06 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 2Y02 2Y02_refined 2.6 B Inactive 0 62 - - - - - - CARMOTEROL
small-molecule Agonist - - No No - - 2011-01-12 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 2Y04 2Y04_refined 3.1 B Inactive 0 62 - - - - - - levosalbutamol
small-molecule Agonist (partial) - - No No - - 2011-01-12 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 3PDS 3PDS_refined 3.5 A Inactive 0 68 - - - - T4-Lysozyme - FAUC50
small-molecule Agonist L-NOREPINEPHRINE, (-)-noradrenaline, Zn2+, noradrenaline, (-)-adrenaline small-molecule No No - 10.1038/NATURE09665 2011-01-12 Yes
AA2AR A2A Adenosine A Human X-ray 3RFM 3RFM_refined 3.6 A Inactive 1 71 - - - - - - caffeine
small-molecule Antagonist adenosine small-molecule No No - - 2011-09-07 Yes
AA2AR A2A Adenosine A Human X-ray 3UZC 3UZC_refined 3.3 A Inactive 1 71 - - - - - - CHEMBL2024114
small-molecule Antagonist adenosine small-molecule No No Congreve M, Andrews SP, Doré AS, Hollenstein K, Hurrell E, Langmead CJ, Mason JS, Ng IW, Tehan B, Zhukov A, Weir M, Marshall FH. 10.1021/jm201376w 2012-03-21 Yes
OPRM μ Opioid A Mouse X-ray 4DKL 4DKL_refined 2.8 A Inactive 4 71 - - - - T4-Lysozyme - Methyl 4-[[(4R,4aS,7R,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl]amino]-4-oxobutanoate
small-molecule Antagonist - - No No Manglik A, Kruse AC, Kobilka TS, Thian FS, Mathiesen JM, Sunahara RK, Pardo L, Weis WI, Kobilka BK, Granier S 10.1038/NATURE10954 2012-03-21 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 4AMI 4AMI_refined 3.2 A Inactive 0 58 - - - - - - Bucindolol
small-molecule Agonist - - No No Warne T, Edwards PC, Leslie AG, Tate CG 10.1016/J.STR.2012.03.014 2012-05-23 Yes
5HT1B 5-HT1B 5-Hydroxytryptamine A Human X-ray 4IAR 4IAR_refined 2.7 A Inactive 15 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
OPSD Rhodopsin Opsins A Bovine X-ray 4BEZ 4BEZ_refined 3.3 A Active 98 94 - - - - - - Apo (no ligand)
none Apo (no ligand) - - No No Singhal A, Ostermaier MK, Vishnivetskiy SA, Panneels V, Homan KT, Tesmer JJ, Veprintsev D, Deupi X, Gurevich VV, Schertler GF, Standfuss J 10.1038/EMBOR.2013.44 2013-04-24 Yes
5HT2B 5-HT2B 5-Hydroxytryptamine A Human X-ray 4NC3 4NC3_refined 2.8 A Intermediate 44 60 - - - - BRIL - ergotamine
small-molecule Agonist 5-hydroxytryptamine small-molecule No No Liu W, Wacker D, Gati C, Han GW, James D, Wang D, Nelson G, Weierstall U, Katritch V, Barty A, Zatsepin NA, Li D, Messerschmidt M, Boutet S, Williams GJ, Koglin JE, Seibert MM, Wang C, Shah ST, Basu S, Fromme R, Kupitz C, Rendek KN, Grotjohann I, Fromme P, Kirian RA, Beyerlein KR, White TA, Chapman HN, Caffrey M, Spence JC, Stevens RC, Cherezov V 10.1126/SCIENCE.1244142 2013-12-18 Yes
OPRD δ Opioid A Human X-ray 4N6H 4N6H_refined 1.8 A Inactive 4 81 - - - - BRIL - naltrindole
small-molecule Antagonist dynorphin A-(1-13), dynorphin A, dynorphin B, α-neoendorphin, endomorphin-1, [Met]enkephalin, dynorphin A-(1-8), [Leu]enkephalin, β-endorphin peptide No Yes Fenalti G, Giguere PM, Katritch V, Huang XP, Thompson AA, Cherezov V, Roth BL, Stevens RC 10.1038/NATURE12944 2013-12-25 Yes
P2Y12 P2Y12 P2Y A Human X-ray 4NTJ 4NTJ_refined 2.6 A Intermediate 44 78 - - - - BRIL - AZD1283
small-molecule Antagonist ADP, ATP small-molecule No No Zhang K, Zhang J, Gao ZG, Zhang D, Zhu L, Han GW, Moss SM, Paoletta S, Kiselev E, Lu W, Fenalti G, Zhang W, Muller CE, Yang H, Jiang H, Cherezov V, Katritch V, Jacobson KA, Stevens RC, Wu B, Zhao Q 10.1038/NATURE13083 2014-03-26 Yes
ACM3 M3 Acetylcholine (muscarinic) A Rat X-ray 4U14 4U14_refined 3.6 A Inactive 2 47 - - - - T4-Lysozyme - tiotropium
small-molecule Antagonist acetylcholine small-molecule No No Thorsen TS, Matt R, Weis WI, Kobilka BK 10.1016/J.STR.2014.08.022 2014-11-26 Yes
P2RY1 P2Y1 P2Y A Human X-ray 4XNW 4XNW_refined 2.7 A Intermediate 44 78 - - - - Rubredoxin - MRS2500
small-molecule Antagonist ADP, ATP small-molecule No No Zhang D, Gao ZG, Zhang K, Kiselev E, Crane S, Wang J, Paoletta S, Yi C, Ma L, Zhang W, Han GW, Liu H, Cherezov V, Katritch V, Jiang H, Stevens RC, Jacobson KA, Zhao Q, Wu B 10.1038/NATURE14287 2015-04-01 Yes
AA2AR A2A Adenosine A Human X-ray 4UHR 4UHR_refined 2.6 A Active 65 75 - - - - - - CGS 21680
small-molecule Agonist adenosine small-molecule No No Lebon G, Edwards PC, Leslie AG, Tate CG 10.1124/mol.114.097360 2015-04-08 Yes
OPSD Rhodopsin Opsins A Human X-ray 4ZWJ 4ZWJ_refined 3.3 A Active 100 94 Visual S-arrestin - 86 T4-Lysozyme - Apo (no ligand)
none Apo (no ligand) - - No No Kang Y, Zhou XE, Gao X, He Y, Liu W, Ishchenko A, Barty A, White TA, Yefanov O, Han GW, Xu Q, de Waal PW, Ke J, Tan MH, Zhang C, Moeller A, West GM, Pascal BD, Van Eps N, Caro LN, Vishnivetskiy SA, Lee RJ, Suino-Powell KM, Gu X, Pal K, Ma J, Zhi X, Boutet S, Williams GJ, Messerschmidt M, Gati C, Zatsepin NA, Wang D, James D, Basu S, Roy-Chowdhury S, Conrad CE, Coe J, Liu H, Lisova S, Kupitz C, Grotjohann I, Fromme R, Jiang Y, Tan M, Yang H, Li J, Wang M, Zheng Z, Li D, Howe N, Zhao Y, Standfuss J, Diederichs K, Dong Y, Potter CS, Carragher B, Caffrey M, Jiang H, Chapman HN, Spence JC, Fromme P, Weierstall U, Ernst OP, Katritch V, Gurevich VV, Griffin PR, Hubbell WL, Stevens RC, Cherezov V, Melcher K, Xu HE 10.1038/NATURE14656 2015-07-29 Yes
OPRX NOP Opioid A Human X-ray 5DHH 5DHH_refined 3.0 A Inactive 4 76 - - - - BRIL - SB 612111
small-molecule Antagonist nociceptin/orphanin FQ peptide No No Miller RL, Thompson AA, Trapella C, Guerrini R, Malfacini D, Patel N, Han GW, Cherezov V, Calo G, Katritch V, Stevens RC 10.1016/J.STR.2015.07.024 2015-10-21 Yes
AA2AR A2A Adenosine A Human X-ray 5IU4 5IU4_refined 1.7 A Inactive 1 71 - - - - BRIL - ZM-241385
small-molecule Antagonist adenosine small-molecule No Yes Segala E, Guo D, Cheng RK, Bortolato A, Deflorian F, Doré AS, Errey JC, Heitman LH, IJzerman AP, Marshall FH, Cooke RM. 10.1021/acs.jmedchem.6b00653 2016-06-29 Yes
AA2AR A2A Adenosine A Human X-ray 5IU8 5IU8_refined 2.0 A Inactive 1 71 - - - - BRIL - CHEMBL3934661
small-molecule Antagonist adenosine small-molecule No Yes Segala E, Guo D, Cheng RK, Bortolato A, Deflorian F, Doré AS, Errey JC, Heitman LH, IJzerman AP, Marshall FH, Cooke RM. 10.1021/acs.jmedchem.6b00653 2016-06-29 Yes
CNR1 CB1 Cannabinoid A Human X-ray 5U09 5U09_refined 2.6 A Inactive 11 60 - - - - Glycogen synthase - taranabant
small-molecule Inverse agonist 2-arachidonoylglycerol, anandamide small-molecule No No Shao Z, Yin J, Chapman K, Grzemska M, Clark L, Wang J, Rosenbaum DM 10.1038/NATURE20613 2016-12-07 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 5TE5 5TE5_refined 4.0 A Inactive 22 100 - - - - - - 10,20-Methanoretinal
small-molecule Agonist - - No No Gulati S, Jastrzebska B, Banerjee S, Placeres AL, Miszta P, Gao S, Gunderson K, Tochtrop GP, Filipek S, Katayama K, Kiser PD, Mogi M, Stewart PL, Palczewski K 10.1073/PNAS.1617446114 2017-03-15 Yes
AGTR2 AT2 Angiotensin A Human X-ray 5UNG 5UNG_refined 2.8 B Active 99 83 - - - - BRIL - compound 1 [PMID: 28379944]
small-molecule Antagonist angiotensin III, angiotensin-(1-7), angiotensin II peptide No No - - 2017-04-05 Yes
GLP1R GLP-1 Glucagon B1 Human X-ray 5NX2 - 3.7 A Intermediate 29 84 - - - - - - Truncated protein agonist
peptide Agonist glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon peptide No No Jazayeri A, Rappas M, Brown AJH, Kean J, Errey JC, Robertson NJ, Fiez-Vandal C, Andrews SP, Congreve M, Bortolato A, Mason JS, Baig AH, Teobald I, Dore AS, Weir M, Cooke RM, Marshall FH 10.1038/NATURE22800 2017-06-14 Yes
AA2AR A2A Adenosine A Human X-ray 5N2R 5N2R_refined 2.8 A Inactive 1 71 - - - - BRIL - PSB36
small-molecule Antagonist adenosine small-molecule No Yes Cheng RKY, Segala E, Robertson N, Deflorian F, Dore AS, Errey JC, Fiez-Vandal C, Marshall FH, Cooke RM 10.1016/j.str.2017.06.012 2017-07-26 Yes
OPSD Rhodopsin Opsins A Human X-ray 5W0P 5W0P_refined 3.0 D Active 100 93 Visual S-arrestin - 90 T4-Lysozyme - Apo (no ligand)
none Apo (no ligand) - - No No Zhou XE, He Y, de Waal PW, Gao X, Kang Y, Van Eps N, Yin Y, Pal K, Goswami D, White TA, Barty A, Latorraca NR, Chapman HN, Hubbell WL, Dror RO, Stevens RC, Cherezov V, Gurevich VV, Griffin PR, Ernst OP, Melcher K, Xu HE 10.1016/J.CELL.2017.07.002 2017-08-09 Yes
EDNRB ETB Endothelin A Human X-ray 5X93 5X93_refined 2.2 A Inactive 4 71 - - - - T4-Lysozyme - K-8794
small-molecule Antagonist endothelin-3, endothelin-1, endothelin-2 peptide No No Shihoya W, Nishizawa T, Yamashita K, Inoue A, Hirata K, Kadji FMN, Okuta A, Tani K, Aoki J, Fujiyoshi Y, Doi T, Nureki O 10.1038/NSMB.3450 2017-08-16 Yes
AA2AR A2A Adenosine A Human X-ray 5OLZ 5OLZ_refined 1.9 A Inactive 1 72 - - - - BRIL - CHEMBL2024114
small-molecule Antagonist adenosine small-molecule No Yes 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
AA2AR A2A Adenosine A Human X-ray 5OM1 5OM1_refined 2.1 A Inactive 1 72 - - - - BRIL - CHEMBL2024114
small-molecule Antagonist adenosine small-molecule No Yes 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
AA2AR A2A Adenosine A Human X-ray 5WF5 5WF5_refined 2.6 A Active 65 69 - - - - T4-Lysozyme - UK-432,097
small-molecule Agonist adenosine small-molecule No No White KL, Eddy MT, Gao ZG, Han GW, Lian T, Deary A, Patel N, Jacobson KA, Katritch V, Stevens RC 10.1016/J.STR.2017.12.013 2018-02-21 Yes
Q98SW5 SMO Frizzled F African clawed frog X-ray 6D35 6D35_refined 3.9 A Active 78 58 - - - - BRIL - Cholesterol
small-molecule Agonist - - No No - - 2018-05-23 Yes
Q80KM9 US28 Unclassified A strain AD169 X-ray 5WB2 5WB2_refined 3.5 A Active 100 82 - - - - - Nanobody CX3CL1
peptide Agonist - - No No Miles TF, Spiess K, Jude KM, Tsutsumi N, Burg JS, Ingram JR, Waghray D, Hjorto GM, Larsen O, Ploegh HL, Rosenkilde MM, Garcia KC 10.7554/ELIFE.35850 2018-06-13 Yes
PD2R2 DP2 Prostanoid A Human X-ray 6D26 6D26_refined 2.8 A Inactive 25 82 - - - - T4-Lysozyme - fevipiprant
small-molecule Antagonist PGE2, PGF, PGJ2, PGD3, PGI2, thromboxane A2, PGD2 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
PD2R2 DP2 Prostanoid A Human X-ray 6D27 6D27_refined 2.7 A Inactive 25 81 - - - - T4-Lysozyme - CHEMBL179036
small-molecule Antagonist PGE2, PGF, PGJ2, PGD3, PGI2, thromboxane A2, PGD2 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
ACM2 M2 Acetylcholine (muscarinic) A Human X-ray 5ZK3 5ZK3_refined 2.6 A Inactive 2 59 - - - - BRIL - CHEMBL558910
small-molecule Antagonist acetylcholine small-molecule No No - - 2018-11-21 Yes
PE2R3 EP3 Prostanoid A Human X-ray 6AK3 6AK3_refined 2.9 B Active 91 69 - - - - BRIL - PGE2
small-molecule Agonist PGE2, PGF, PGE1, PGI2, thromboxane A2, PGD2 small-molecule No No - 10.1038/S41589-018-0171-8 2018-12-05 Yes
CCR5 CCR5 Chemokine A Human Cryo-EM 6MEO 6MEO_refined 3.9 B Inactive 16 89 - - - - - T-cell surface glycoprotein CD4 Envelope glycoprotein gp160
protein Antagonist CCL11, CCL13, CCL4, CCL7, CCL14, CCL3, CCL8, CCL16, CCL5, CCL2 peptide No No - 10.1038/S41586-018-0804-9 2018-12-12 Yes
CNR2 CB2 Cannabinoid A Human X-ray 5ZTY 5ZTY_refined 2.8 A Inactive 11 80 - - - - T4-Lysozyme - AM10257
small-molecule Antagonist 2-arachidonoylglycerol, anandamide small-molecule No No - 10.1016/J.CELL.2018.12.011 2019-01-30 Yes
PTH1R PTH1 Parathyroid hormone B1 Human Cryo-EM 6NBH - 3.5 R Active 100 64 Gs αs - 57 - Nanobody-35 Long-acting parathyroid hormone analog
peptide Agonist PTHrP, PTH, PTHrP-(1-36), TIP39 peptide No No - - 2019-04-17 Yes
ACM1 M1 Acetylcholine (muscarinic) A Human Cryo-EM 6OIJ 6OIJ_refined 3.3 R Active 100 64 Gq/11 α11 - 63 - Antibody fragment iperoxo
small-molecule Agonist acetylcholine small-molecule No No - 10.1126/SCIENCE.AAW5188 2019-05-08 Yes
SMO SMO Frizzled F Human Cryo-EM 6OT0 - 3.9 R Active 100 46 Gi/o αi1 - 100 - Fab light chain
Fab heavy chain
24,25-Epoxy-cholesterol
small-molecule Agonist - - No No - 10.1038/S41586-019-1286-0 2019-06-12 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 6PS5 6PS5_refined 2.9 A Inactive 0 68 - - - - T4-Lysozyme - propranolol
small-molecule Antagonist L-NOREPINEPHRINE, (-)-noradrenaline, Zn2+, noradrenaline, (-)-adrenaline small-molecule No No - 10.1107/S2052252519013137 2019-11-13 Yes
ADA2C α2C Adrenoceptors A Human X-ray 6KUW 6KUW_refined 2.8 A Inactive 1 60 - - - - GlgA glycogen synthase - (8Ar,12aS,13aR)-12-ethylsulfonyl-3-methoxy-5,6,8,8a,9,10,11,12a,13,13a-decahydroisoquinolino[2,1-g][1,6]naphthyridine
small-molecule Antagonist (-)-noradrenaline, (-)-adrenaline small-molecule No No - - 2019-12-04 Yes
CLTR2 CysLT2 Leukotriene A Human X-ray 6RZ6 6RZ6_refined 2.4 A Intermediate 44 82 - - - - BRIL - ONO-2570366
small-molecule Antagonist LTC4, LTE4, LTD4 small-molecule No No Gusach A, Luginina A, Marin E, Brouillette RL, Besserer-Offroy E, Longpre JM, Ishchenko A, Popov P, Patel N, Fujimoto T, Maruyama T, Stauch B, Ergasheva M, Romanovskaia D, Stepko A, Kovalev K, Shevtsov M, Gordeliy V, Han GW, Katritch V, Borshchevskiy V, Sarret P, Mishin A, Cherezov V 10.1038/S41467-019-13348-2 2019-12-11 Yes
OX2R OX2 Orexin A Human X-ray 6TPN 6TPN_refined 2.6 A Inactive 1 71 - - - - GlgA glycogen synthase - HTL6641
small-molecule Antagonist orexin-A, orexin-B 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
EDNRB ETB Endothelin A Human X-ray 6LRY 6LRY_refined 3.0 A Inactive 15 70 - - - - T4-Lysozyme - sarafotoxin S6b
peptide Agonist endothelin-3, endothelin-1, endothelin-2 peptide No No Izume T, Miyauchi H, Shihoya W, Nureki O 10.1016/J.BBRC.2019.12.091 2020-02-12 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 2-arachidonoylglycerol, anandamide 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
GPR52 GPR52 A orphans A Human X-ray 6LI2 6LI2_refined 2.8 A Intermediate 40 80 - - - - Rubredoxin - Apo (no ligand)
none Apo (no ligand) - - No No Lin X, Li M, Wang N, Wu Y, Luo Z, Guo S, Han GW, Li S, Yue Y, Wei X, Xie X, Chen Y, Zhao S, Wu J, Lei M, Xu F 10.1038/S41586-020-2019-0 2020-02-26 Yes
GLR glucagon Glucagon B1 Human Cryo-EM 6LMK 6LMK_refined 3.7 R Active 100 83 Gs αs - 59 - Nanobody-35 glucagon
peptide Agonist glucagon peptide No No - - 2020-04-01 Yes
ADA2B α2B Adrenoceptors A Human Cryo-EM 6K42 - 4.1 R Active 100 60 Gi/o αi1 - 62 T4-Lysozyme scFv dexmedetomidine
small-molecule Agonist (-)-noradrenaline, (-)-adrenaline small-molecule No No Yuan D, Liu Z, Kaindl J, Maeda S, Zhao J, Sun X, Xu J, Gmeiner P, Wang HW, Kobilka BK 10.1038/S41589-020-0492-2 2020-04-15 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
ADRB2 β2 Adrenoceptors A Human Cryo-EM 7BZ2 7BZ2_refined 3.8 R Active 100 69 Gs αs - 50 - Nanobody-35 arformoterol
small-molecule Agonist L-NOREPINEPHRINE, (-)-noradrenaline, Zn2+, noradrenaline, (-)-adrenaline small-molecule No No Zhang Y, Yang F, Ling S, Lv P, Zhou Y, Fang W, Sun W, Zhang L, Shi P, Tian C 10.1038/S41421-020-0176-9 2020-08-05 Yes
CXCR2 CXCR2 Chemokine A Human Cryo-EM 6LFO 6LFO_refined 3.4 R Active 100 85 Gi/o αi1 - 65 - scFv16 Interleukin-8
protein Agonist CXCL6, CXCL2, CXCL1, CXCL5, CXCL7, CXCL3, CXCL8 peptide No No Liu K, Wu L, Yuan S, Wu M, Xu Y, Sun Q, Li S, Zhao S, Hua T, Liu ZJ 10.1038/S41586-020-2492-5 2020-09-02 Yes
SMO SMO Frizzled F Human Cryo-EM 6XBM - 3.2 R Active 100 42 Gi/o αi1 - 61 - scFv16 24,25-Epoxy-cholesterol
24,25-Epoxy-cholesterol
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
ADRB1 β1 Adrenoceptors A Human X-ray 7BVQ 7BVQ_refined 2.5 A Inactive 0 60 - - - - T4-Lysozyme - Carazolol
small-molecule Inverse agonist L-NOREPINEPHRINE, (-)-noradrenaline, noradrenaline, (-)-adrenaline small-molecule No No Xu X, Kaindl J, Clark MJ, Hubner H, Hirata K, Sunahara RK, Gmeiner P, Kobilka BK, Liu X 10.1038/S41422-020-00424-2 2020-12-02 Yes
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 7LCK 7LCK_refined 3.2 R Active 98 84 - - - - - - danuglipron
small-molecule Agonist glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon peptide No No Zhang X, Johnson RM, Drulyte I, Yu L, Kotecha A, Danev R, Wootten D, Sexton PM, Belousoff MJ 10.1016/J.STR.2021.04.008 2021-01-20 Yes
NTR1 NTS1 Neurotensin A Rat X-ray 6ZIN - 2.6 A Inactive 32 76 - - - - DARPin D12 - meclinertant
small-molecule Inverse agonist neurotensin, neuromedin N 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
CALRL calcitonin-like Calcitonin B1 Human Cryo-EM 7KNT 7KNT_refined 3.2 R Inactive 10 74 - - - - - RAMP1 Apo (no ligand)
none Apo (no ligand) - - No No Josephs TM, Belousoff MJ, Liang YL, Piper SJ, Cao J, Garama DJ, Leach K, Gregory KJ, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM 10.1126/SCIENCE.ABF7258 2021-02-24 Yes
DRD1 D1 Dopamine A Human Cryo-EM 7CKW 7CKW_refined 3.2 R Active 100 61 Gs αs - 60 - Nanobody-35 fenoldopam
small-molecule Agonist L-NOREPINEPHRINE, (-)-noradrenaline, 5-hydroxytryptamine, dopamine, 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
5HT1D 5-HT1D 5-Hydroxytryptamine A Human Cryo-EM 7E32 - 2.9 R Active 100 76 Gi/o αi1 - 62 - scFv16 5-hydroxytryptamine
small-molecule Agonist 5-hydroxytryptamine, 5-HT-moduline 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 2021-04-21 Yes
MC4R MC4 Melanocortin A Human Cryo-EM 7AUE 7AUE_refined 3.0 R Active 100 79 Gs αs - 59 - scFv16 setmelanotide
peptide Agonist β-MSH, α-MSH, ACTH, agouti-related protein, γ-MSH peptide No No Israeli H, Degtjarik O, Fierro F, Chunilal V, Gill AK, Roth NJ, Botta J, Prabahar V, Peleg Y, Chan LF, Ben-Zvi D, McCormick PJ, Niv MY, Shalev-Benami M 10.1126/SCIENCE.ABF7958 2021-04-28 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-58, CCK-39, CCK-8, CCK-4, gastrin-17, CCK-33, desulfated cholecystokinin-8 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
OPSD Rhodopsin Opsins A Bovine Cryo-EM 7MTA 7MTA_refined 4.1 R Active 98 93 - - - - - Fab heavy chain
Fab light chain
GRK1
Retinal (all-trans)
small-molecule Agonist - - No No - - 2021-07-07 Yes
GRM2 mGlu2 Metabotropic glutamate C Human Cryo-EM 7MTQ - 3.7 B Inactive - 85 - - - - - - LY341495
small-molecule Antagonist L-glutamic acid small-molecule No No - 10.1038/S41586-021-03680-3 2021-07-07 Yes
CCR5 CCR5 Chemokine A Human Cryo-EM 7F1S 7F1S_refined 2.8 R Active 100 78 Gi/o αi1 - 61 - - Apo (no ligand)
none Apo (no ligand) CCL11, CCL13, CCL4, CCL7, CCL14, CCL3, CCL8, CCL16, CCL5, CCL2 peptide No No - 10.1038/S41467-021-24438-5 2021-07-14 Yes
CCKAR CCK1 Cholecystokinin A Human Cryo-EM 7EZM - 2.9 D Active 100 71 Gq/11 αq - 63 - scFv16 CCK-8
peptide Agonist CCK-58, CCK-39, CCK-8, CCK-4, gastrin-17, CCK-33, desulfated cholecystokinin-8 peptide No No Liu Q, Yang D, Zhuang Y, Croll TI, Cai X, Dai A, He X, Duan J, Yin W, Ye C, Zhou F, Wu B, Zhao Q, Xu HE, Wang MW, Jiang Y 10.1038/S41589-021-00841-3 2021-08-25 Yes
GRM5 mGlu5 Metabotropic glutamate C Human Cryo-EM 7FD8 7FD8_refined 3.8 A Active - 63 - - - - - - quisqualate
small-molecule Agonist L-glutamic acid small-molecule No No Nasrallah C, Cannone G, Briot J, Rottier K, Berizzi AE, Huang CY, Quast RB, Hoh F, Baneres JL, Malhaire F, Berto L, Dumazer A, Font-Ingles J, Gomez-Santacana X, Catena J, Kniazeff J, Goudet C, Llebaria A, Pin JP, Vinothkumar KR, Lebon G 10.1016/J.CELREP.2021.109648 2021-09-08 Yes
AA1R A1 Adenosine A Human Cryo-EM 7LD3 - 3.2 R Active 100 88 Gi/o αi2 - 59 - - {2-Amino-4-[3,5-bis(trifluoromethyl)phenyl]thiophen-3-yl}(4-chlorophenyl)methanone
adenosine
small-molecule
small-molecule
Ago-PAM
Agonist
adenosine small-molecule No No - - 2021-09-08 Yes
GASR CCK2 Cholecystokinin A Human Cryo-EM 7F8W 7F8W_refined 3.1 R Active 100 62 Gq/11 αq Gq-Gi1 chimera 62 - scFv16 desulfated gastrin-17
peptide Agonist desulfated gastrin-17, CCK-58, gastrin-71, CCK-39, desulfated gastrin-34, CCK-8, CCK-4, desulfated gastrin-71, gastrin-17, gastrin-14, CCK-33, desulfated gastrin-14, desulfated cholecystokinin-8, gastrin-34 peptide No No Zhang X, He C, Wang M, Zhou Q, Yang D, Zhu Y, Feng W, Zhang H, Dai A, Chu X, Wang J, Yang Z, Jiang Y, Sensfuss U, Tan Q, Han S, Reedtz-Runge S, Xu HE, Zhao S, Wang MW, Wu B, Zhao Q 10.1038/S41589-021-00866-8 2021-10-13 Yes
CCKAR CCK1 Cholecystokinin A Human X-ray 7F8Y 7F8Y_refined 2.5 A Inactive 1 65 - - - - T4-Lysozyme - DEVAZEPIDE
small-molecule Antagonist CCK-58, CCK-39, CCK-8, CCK-4, gastrin-17, CCK-33, desulfated cholecystokinin-8 peptide No No Zhang X, He C, Wang M, Zhou Q, Yang D, Zhu Y, Feng W, Zhang H, Dai A, Chu X, Wang J, Yang Z, Jiang Y, Sensfuss U, Tan Q, Han S, Reedtz-Runge S, Xu HE, Zhao S, Wang MW, Wu B, Zhao Q 10.1038/S41589-021-00866-8 2021-10-13 Yes
MC4R MC4 Melanocortin A Human Cryo-EM 7F58 7F58_refined 3.1 R Active 100 82 Gs αs - 58 - Nanobody-35 THIQ
small-molecule Agonist β-MSH, α-MSH, ACTH, agouti-related protein, γ-MSH 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
MRGX2 MRGPRX2 A orphans A Human Cryo-EM 7VDH - 2.9 R Active 100 81 Gi/o αi1 - 62 - scFv16 compound 48/80
small-molecule Agonist PAMP-20 peptide No No Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP 10.1038/S41586-021-04077-Y 2021-12-01 Yes
MRGX2 MRGPRX2 A orphans A Human Cryo-EM 7VV4 7VV4_refined 3.0 R Active 97 80 - - - - - - Cortistatin 14
peptide Agonist PAMP-20 peptide No No Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP 10.1038/S41586-021-04077-Y 2021-12-01 Yes
MRGX2 MRGPRX2 A orphans A Human Cryo-EM 7VV5 7VV5_refined 2.8 R Active 100 81 Gi/o αi1 - 64 - scFv16 compound 48/80
small-molecule Agonist PAMP-20 peptide No No Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP 10.1038/S41586-021-04077-Y 2021-12-01 Yes
S1PR1 S1P1 Lysophospholipid (S1P) A Human Cryo-EM 7WF7 7WF7_refined 3.4 A Active 100 71 Gi/o αi1 - 40 - scFv16 sphingosine 1-phosphate
small-molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine small-molecule No No Xu Z, Ikuta T, Kawakami K, Kise R, Qian Y, Xia R, Sun MX, Zhang A, Guo C, Cai XH, Huang Z, Inoue A, He Y 10.1038/S41589-021-00930-3 2022-01-05 Yes
5HT2A 5-HT2A 5-Hydroxytryptamine A Human X-ray 7WC9 7WC9_refined 2.5 A Inactive 1 59 - - - - BRIL - IHCH-7086
small-molecule Agonist 5-hydroxytryptamine, tryptamine small-molecule No No Cao D, Yu J, Wang H, Luo Z, Liu X, He L, Qi J, Fan L, Tang L, Chen Z, Li J, Cheng J, Wang S 10.1126/SCIENCE.ABL8615 2022-01-26 Yes
GHRHR GHRH Glucagon B1 Human Cryo-EM 7V9M 7V9M_refined 3.3 R Active 100 63 Gs αs - 57 - Nanobody-35 Somatoliberin
peptide Agonist 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 2021-10-20 Yes
FPR2 FPR2/ALX Formylpeptide A Human Cryo-EM 7T6V 7T6V_refined 3.1 R Active 100 85 Gi/o αi1 - 61 - scFv16 synthetic peptide
peptide Agonist aspirin triggered lipoxin A4, LXA4, LTC4, serum amyloid A, aspirin-triggered resolvin D1, annexin I, LL-37, PrP106-126, fMet-Leu-Phe, 15-deoxy-LXA4, resolvin D1, humanin, LTD4 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
SSR2 SST2 Somatostatin A Human Cryo-EM 7T11 7T11_refined 2.7 R Active 100 77 Gi/o αi3 - 62 - scFv16 Octreotide
peptide Agonist SRIF-28, SRIF-14, cortistatin-14, CST-17 peptide No No Robertson MJ, Meyerowitz JG, Panova O, Borrelli K, Skiniotis G 10.1038/S41594-022-00727-5 2022-03-09 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 20-hydroxy-LTB4, 12R-HETE, 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
CALCR CT Calcitonin B1 Human Cryo-EM 7TYL - 3.3 R Active 100 78 Gs αs - 58 - Nanobody-35 Amylin rat
peptide Agonist adrenomedullin, α-CGRP, amylin, calcitonin, adrenomedullin 2/intermedin, calcitonin (salmon), β-CGRP 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
CALCR CT Calcitonin B1 Human Cryo-EM 7TYW - 3.0 R Active 100 78 Gs αs - 58 - Nanobody-35 calcitonin (salmon synthetic)
small-molecule Agonist adrenomedullin, α-CGRP, amylin, calcitonin, adrenomedullin 2/intermedin, calcitonin (salmon), β-CGRP 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
GIPR GIP Glucagon B1 Human Cryo-EM 7VAB 7VAB_refined 3.2 R Active 100 58 Gs αs Mini-Gs 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
GALR1 GAL1 Galanin A Human Cryo-EM 7WQ3 7WQ3_refined 2.7 R Active 100 83 Gi/o αi1 - 64 - scFv16 galanin
peptide Agonist galanin-like peptide, galanin peptide No No Duan J, Shen DD, Zhao T, Guo S, He X, Yin W, Xu P, Ji Y, Chen LN, Liu J, Zhang H, Liu Q, Shi Y, Cheng X, Jiang H, Eric Xu H, Zhang Y, Xie X, Jiang Y 10.1038/S41467-022-29072-3 2022-04-20 Yes
GP183 GPR183 A orphans A Human Cryo-EM 7TUZ 7TUZ_refined 3.1 R Active 100 79 Gi/o αi1 - 64 - scFv16 (2S,4aS,4bS,7R,8S,8aS,9R,10aR)-7-[(2R,3R)-7-hydroxy-3,7-dimethyloctan-2-yl]-4a,7,8-trimethyltetradecahydrophenanthrene-2,9-diol
small-molecule Agonist 7β, 25-dihydroxycholesterol, 7β-hydroxycholesterol, 7α,27-dihydroxycholesterol, 7α,25-dihydroxycholesterol, 27-hydroxycholesterol, 7β, 27-dihydroxycholesterol, 7α-hydroxycholesterol, 25-hydroxycholesterol small-molecule No No Chen H, Huang W, Li X 10.1016/J.STR.2022.04.006 2022-04-13 Yes
GIPR GIP Glucagon B1 Human Cryo-EM 7RBT 7RBT_refined 3.1 R Active 100 81 Gs αs - 56 - scFv16
Nanobody-35
tirzepatide
2-fluoro-4-[(1R)-6-methoxy-1-methyl-2-{(1S)-1-[4-(propan-2-yl)phenyl]ethyl}-1,2,3,4-tetrahydroisoquinolin-5-yl]-6-[(2-methylpropyl)amino]phenol
peptide
small-molecule
Agonist
PAM
gastric inhibitory polypeptide peptide No No Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW 10.1073/PNAS.2116506119 2022-04-13 Yes
VIPR2 VPAC2 VIP and PACAP B1 Human Cryo-EM 7WBJ - 3.4 R Active 100 82 Gs αs - 60 - Nanobody-35 PACAP-27
peptide Agonist VIP, secretin, PACAP-38, PHI, GHRH, PACAP-27 peptide No No Xu Y, Feng W, Zhou Q, Liang A, Li J, Dai A, Zhao F, Yan J, Chen CW, Li H, Zhao LH, Xia T, Jiang Y, Xu HE, Yang D, Wang MW 10.1038/S41467-022-30041-Z 2022-05-18 Yes
BKRB2 B2 Bradykinin A Human Cryo-EM 7F6I 7F6I_refined 2.8 A Active 100 78 Gq/11 αq - 63 - - kallidin
peptide Agonist T-kinin, kallidin, [Hyp3]bradykinin, [des-Arg9]bradykinin, bradykinin, [des-Arg10]kallidin, Lys-[Hyp3]-bradykinin 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
GALR2 GAL2 Galanin A Human Cryo-EM 7XJK 7XJK_refined 3.3 F Active 100 72 Gq/11 αq - 58 - scFv16 Galanin, Human
peptide Agonist spexin-1, galanin-like peptide, galanin peptide No No - - 2022-06-29 Yes
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 7X8R - 2.6 R Active 100 64 Gs αs - 59 - Nanobody-35 CHEMBL2158411
small-molecule Agonist glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon peptide No No Cong Z, Zhou Q, Li Y, Chen LN, Zhang ZC, Liang A, Liu Q, Wu X, Dai A, Xia T, Wu W, Zhang Y, Yang D, Wang MW 10.1073/PNAS.2200155119 2022-06-29 Yes
5HT4R 5-HT4 5-Hydroxytryptamine A Human Cryo-EM 7XT8 - 3.1 R Active 100 76 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
CX3C1 CX3CR1 Chemokine A Human Cryo-EM 7XBW 7XBW_refined 2.8 R Active 16 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
ACKR3 ACKR3 Chemokine A Human Cryo-EM 7SK3 7SK3_refined 3.8 A Active 95 84 - - - - - CID25 Fab light chain
CID25 Fab heavy chain
CID24 Fab light chain
CID24 Fab heavy chain
CXCL12α
peptide Agonist CXCL12α, CXCL11 peptide No No Yen YC, Schafer CT, Gustavsson M, Eberle SA, Dominik PK, Deneka D, Zhang P, Schall TJ, Kossiakoff AA, Tesmer JJG, Handel TM 10.1126/SCIADV.ABN8063 2022-07-27 Yes
5HT2C 5-HT2C 5-Hydroxytryptamine A Human Cryo-EM 8DPF - 2.8 A Active 100 58 Gq/11 αq Gi2-mini-Gq chimera 57 - scFv16 lorcaserin
small-molecule Agonist 5-hydroxytryptamine small-molecule No No Gumpper RH, Fay JF, Roth BL 10.1016/J.CELREP.2022.111211 2022-08-24 Yes
TRFR TRH1 Thyrotropin-releasing hormone A Human Cryo-EM 7X1T - 3.3 A Active 100 68 Gq/11 αq - 57 - scFv16 taltirelin
small-molecule Agonist TRH peptide No No Yang F, Zhang H, Meng X, Li Y, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C 10.1038/S41422-022-00646-6 2022-08-31 Yes
S1PR5 S1P5 Lysophospholipid (S1P) A Human X-ray 7YXA 7YXA_refined 2.2 A Inactive 1 72 - - - - BRIL - 4-[6-(2-naphthalen-1-ylethoxy)-2,3,4,5-tetrahydro-1H-3-benzazepin-3-ium-3-yl]butanoic acid
small-molecule Antagonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine small-molecule No No Lyapina E, Marin E, Gusach A, Orekhov P, Gerasimov A, Luginina A, Vakhrameev D, Ergasheva M, Kovaleva M, Khusainov G, Khorn P, Shevtsov M, Kovalev K, Bukhdruker S, Okhrimenko I, Popov P, Hu H, Weierstall U, Liu W, Cho Y, Gushchin I, Rogachev A, Bourenkov G, Park S, Park G, Hyun HJ, Park J, Gordeliy V, Borshchevskiy V, Mishin A, Cherezov V 10.1038/S41467-022-32447-1 2022-08-10 Yes
PTH1R PTH1 Parathyroid hormone B1 Human Cryo-EM 7VVM 7VVM_refined 3.2 R Active 100 60 Gs αs - 58 - Nanobody-35 Parathyroid hormone
peptide Agonist PTHrP, PTH, PTHrP-(1-36), TIP39 peptide No No Kobayashi K, Kawakami K, Kusakizako T, Miyauchi H, Tomita A, Kobayashi K, Shihoya W, Yamashita K, Nishizawa T, Kato HE, Inoue A, Nureki O 10.1016/J.MOLCEL.2022.07.003 2022-08-03 Yes
HRH3 H3 Histamine A Human X-ray 7F61 7F61_refined 2.6 A Inactive 8 68 - - - - BRIL - N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]cyclobutane-1-carboxamide
small-molecule Antagonist histamine small-molecule No No Peng X, Yang L, Liu Z, Lou S, Mei S, Li M, Chen Z, Zhang H 10.1038/S41467-022-33880-Y 2022-10-26 Yes
CRFR2 CRF2 Corticotropin-releasing factor B1 Human Cryo-EM 7TS0 7TS0_refined 2.8 P Active 100 72 Gi/o αo - 63 - scFv16 Urocortin
peptide Agonist urocortin 3, urocortin 2, corticotrophin-releasing hormone, urocortin 1 peptide No No Zhao LH, Lin J, Ji SY, Zhou XE, Mao C, Shen DD, He X, Xiao P, Sun J, Melcher K, Zhang Y, Yu X, Xu HE 10.1038/S41467-022-33851-3 2022-11-09 Yes
OPRM μ Opioid A Mouse Cryo-EM 7U2K - 3.3 D Active 100 71 Gi/o αi1 - 61 - - CHEMBL147044
small-molecule Agonist - - No No Faouzi A, Wang H, Zaidi SA, DiBerto JF, Che T, Qu Q, Robertson MJ, Madasu MK, El Daibani A, Varga BR, Zhang T, Ruiz C, Liu S, Xu J, Appourchaux K, Slocum ST, Eans SO, Cameron MD, Al-Hasani R, Pan YX, Roth BL, McLaughlin JP, Skiniotis G, Katritch V, Kobilka BK, Majumdar S 10.1038/S41586-022-05588-Y 2022-12-07 Yes
AGRF1 ADGRF1 ADGRF B2 Human Cryo-EM 7WZ7 - 2.8 R Active - 30 G12/13 α12 Mini-G12 55 - scFv16 Apo (no ligand)
none Apo (no ligand) - - No No Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y 10.1038/S41467-022-33173-4 2022-09-28 Yes
LPAR1 LPA1 Lysophospholipid (LPA) A Human Cryo-EM 7YU5 7YU5_refined 3.3 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
LPAR1 LPA1 Lysophospholipid (LPA) A Human Cryo-EM 7YU8 - 4.5 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
ACM4 M4 Acetylcholine (muscarinic) A Human Cryo-EM 8E9X - 2.7 A Active 100 57 Gi/o αo Mini-Go 61 - scFv16 CHEMBL73538
small-molecule Agonist acetylcholine small-molecule No No - - 2022-11-30 Yes
OPRD δ Opioid A Human Cryo-EM 8F7S 8F7S_refined 3.0 R Active 100 78 Gi/o αi1 - 62 - - DELTORPHIN II
protein Agonist dynorphin A-(1-13), dynorphin A, dynorphin B, α-neoendorphin, endomorphin-1, [Met]enkephalin, dynorphin A-(1-8), [Leu]enkephalin, β-endorphin peptide No No Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y, Roth BL, Xu HE 10.1016/J.CELL.2022.12.026 2022-12-14 Yes
RL3R2 RXFP4 Relaxin family peptide A Human Cryo-EM 7YJ4 - 3.2 R Active 100 76 Gi/o αi2 - 58 - scFv16 Insulin-like peptide INSL5 A chain
Insulin-like peptide INSL5 B chain
peptide
peptide
Agonist INSL5, relaxin-3, relaxin-3 (B chain) peptide No No - - 2023-03-01 Yes
NPY2R Y2 Neuropeptide Y A Human Cryo-EM 7YON 7YON_refined 3.0 R Active 100 79 Gi/o αi1 - 62 - scFv16 Peptide YY
peptide Agonist neuropeptide Y, pancreatic polypeptide, neuropeptide Y-(3-36), peptide YY, PYY-(3-36) 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
NTR1 NTS1 Neurotensin A Rat Cryo-EM 8FN0 - 2.9 A Active 100 67 Gi/o αo Mini-Go 60 - scFv16 neurotensin
CHEMBL4576388
peptide
small-molecule
Agonist
PAM
neurotensin, neuromedin N peptide No No - - 2023-03-29 Yes
AA2BR A2B Adenosine A Human Cryo-EM 8HDO - 2.9 R Active 100 83 Gs αs Mini-Gs 59 - Nanobody-35 BAY 60-6583
small-molecule Agonist adenosine small-molecule No No - 10.1038/S41421-022-00503-1 2023-01-18 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 3DQB 3DQB_refined 3.2 A Active 100 94 Gi/o αt1 Only H5 3 - - Apo (no ligand)
none Apo (no ligand) - - No No - 10.1038/NATURE07330 2008-09-23 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 2Y03 2Y03_refined 2.9 B Inactive 0 62 - - - - - - LEVISOPRENALINE
small-molecule Agonist - - No No - - 2011-01-12 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 3PXO - 3.0 A Active 98 94 - - - - - - Retinal (all-trans)
small-molecule Agonist - - No No - - 2011-03-09 Yes
AA2AR A2A Adenosine A Human X-ray 3UZA 3UZA_refined 3.3 A Inactive 1 71 - - - - - - compound 4g [PMID: 22220592]
small-molecule Antagonist adenosine small-molecule No No Congreve M, Andrews SP, Doré AS, Hollenstein K, Hurrell E, Langmead CJ, Mason JS, Ng IW, Tehan B, Zhukov A, Weir M, Marshall FH. 10.1021/jm201376w 2012-03-21 Yes
OPRX NOP Opioid A Human X-ray 4EA3 4EA3_refined 3.0 A Inactive 4 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
5HT2B 5-HT2B 5-Hydroxytryptamine A Human X-ray 4IB4 4IB4_refined 2.7 A Intermediate 44 59 - - - - BRIL - ergotamine
small-molecule Agonist 5-hydroxytryptamine small-molecule No No Wacker D, Wang C, Katritch V, Han GW, Huang XP, Vardy E, McCorvy JD, Jiang Y, Chu M, Siu FY, Liu W, Xu HE, Cherezov V, Roth BL, Stevens RC 10.1126/science.1232808 2013-03-13 Yes
NTR1 NTS1 Neurotensin A Rat X-ray 4BWB - 3.6 A Inactive 3 72 - - - - - - neurotensin
peptide Agonist neurotensin, neuromedin N peptide No No Egloff P, Hillenbrand M, Klenk C, Batyuk A, Heine P, Balada S, Schlinkmann KM, Scott DJ, Schutz M, Pluckthun A 10.1073/PNAS.1317903111 2014-01-29 Yes
ACM3 M3 Acetylcholine (muscarinic) A Rat X-ray 4U16 4U16_refined 3.7 B Inactive 2 47 - - - - T4-Lysozyme - N-methyl scopolamine
small-molecule Antagonist acetylcholine small-molecule No No Thorsen TS, Matt R, Weis WI, Kobilka BK 10.1016/J.STR.2014.08.022 2014-11-26 Yes
NTR1 NTS1 Neurotensin A Rat X-ray 4XES 4XES_refined 2.6 A Active 79 72 - - - - T4-Lysozyme - neurotensin
peptide Agonist neurotensin, neuromedin N peptide No No Krumm BE, White JF, Shah P, Grisshammer R 10.1038/NCOMMS8895 2015-07-29 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 5D5B 5D5B_refined 3.8 A Inactive 0 68 - - - - T4-Lysozyme - Carazolol
small-molecule Inverse agonist L-NOREPINEPHRINE, (-)-noradrenaline, Zn2+, noradrenaline, (-)-adrenaline small-molecule No No Huang CY, Olieric V, Ma P, Howe N, Vogeley L, Liu X, Warshamanage R, Weinert T, Panepucci E, Kobilka B, Diederichs K, Wang M, Caffrey M 10.1107/S2059798315021683 2016-01-13 Yes
AA2AR A2A Adenosine A Human X-ray 5K2C 5K2C_refined 1.9 A Inactive 1 72 - - - - BRIL - ZM-241385
small-molecule Antagonist adenosine small-molecule No Yes 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
CNR1 CB1 Cannabinoid A Human X-ray 5TGZ 5TGZ_refined 2.8 A Inactive 11 61 - - - - Flavodoxin - AM6538
small-molecule Antagonist 2-arachidonoylglycerol, anandamide small-molecule No No Hua T, Vemuri K, Pu M, Qu L, Han GW, Wu Y, Zhao S, Shui W, Li S, Korde A, Laprairie RB, Stahl EL, Ho JH, Zvonok N, Zhou H, Kufareva I, Wu B, Zhao Q, Hanson MA, Bohn LM, Makriyannis A, Stevens RC, Liu ZJ 10.1016/J.CELL.2016.10.004 2016-11-02 Yes
GLR glucagon Glucagon B1 Human X-ray 5XF1 5XF1_refined 3.2 B Inactive 0 81 - - - - T4-Lysozyme Antibody NNC0640
small-molecule NAM glucagon peptide No No Zhang H, Qiao A, Yang D, Yang L, Dai A, de Graaf C, Reedtz-Runge S, Dharmarajan V, Zhang H, Han GW, Grant TD, Sierra RG, Weierstall U, Nelson G, Liu W, Wu Y, Ma L, Cai X, Lin G, Wu X, Geng Z, Dong Y, Song G, Griffin PR, Lau J, Cherezov V, Yang H, Hanson MA, Stevens RC, Zhao Q, Jiang H, Wang MW, Wu B 10.1038/NATURE22363 2017-05-24 Yes
FFAR1 FFA1 Free fatty acid A Human X-ray 5TZY 5TZY_refined 3.2 A Intermediate 44 91 - - - - T4-Lysozyme - MK-8666
(2S,3R)-3-Cyclopropyl-3-[(2R)-2-[1-[(1S)-1-[5-fluoro-2-(trifluoromethoxy)phenyl]ethyl]piperidin-4-yl]-3,4-dihydro-2H-chromen-7-yl]-2-methylpropanoic acid
small-molecule
small-molecule
Agonist
PAM
docosahexaenoic acid, oleic acid, myristic acid, α-linolenic acid small-molecule No No Lu J, Byrne N, Wang J, Bricogne G, Brown FK, Chobanian HR, Colletti SL, Di Salvo J, Thomas-Fowlkes B, Guo Y, Hall DL, Hadix J, Hastings NB, Hermes JD, Ho T, Howard AD, Josien H, Kornienko M, Lumb KJ, Miller MW, Patel SB, Pio B, Plummer CW, Sherborne BS, Sheth P, Souza S, Tummala S, Vonrhein C, Webb M, Allen SJ, Johnston JM, Weinglass AB, Sharma S, Soisson SM 10.1038/NSMB.3417 2017-06-07 Yes
OPRK κ Opioid A Human X-ray 6B73 6B73_refined 3.1 A Active 100 73 - - - - BRIL Nanobody MP1104
small-molecule Agonist dynorphin A-(1-13), dynorphin A, dynorphin B, α-neoendorphin, [Met]enkephalin, dynorphin A-(1-8), [Leu]enkephalin, big dynorphin, β-endorphin, β-neoendorphin peptide No No Che T, Majumdar S, Zaidi SA, Ondachi P, McCorvy JD, Wang S, Mosier PD, Uprety R, Vardy E, Krumm BE, Han GW, Lee MY, Pardon E, Steyaert J, Huang XP, Strachan RT, Tribo AR, Pasternak GW, Carroll FI, Stevens RC, Cherezov V, Katritch V, Wacker D, Roth BL 10.1016/J.CELL.2017.12.011 2018-01-17 Yes
AA2AR A2A Adenosine A Human X-ray 5WF6 5WF6_refined 2.9 A Active 65 68 - - - - T4-Lysozyme - UK-432,097
small-molecule Agonist adenosine small-molecule No No White KL, Eddy MT, Gao ZG, Han GW, Lian T, Deary A, Patel N, Jacobson KA, Katritch V, Stevens RC 10.1016/J.STR.2017.12.013 2018-02-21 Yes
OPSD Rhodopsin Opsins A Human Cryo-EM 6CMO 6CMO_refined 4.5 R Active 81 92 Gi/o αi1 - 100 BRIL Fab Apo (no ligand)
none Apo (no ligand) - - No No Kang Y, Kuybeda O, de Waal PW, Mukherjee S, Van Eps N, Dutka P, Zhou XE, Bartesaghi A, Erramilli S, Morizumi T, Gu X, Yin Y, Liu P, Jiang Y, Meng X, Zhao G, Melcher K, Ernst OP, Kossiakoff AA, Subramaniam S, Xu HE 10.1038/S41586-018-0215-Y 2018-06-20 Yes
5HT2B 5-HT2B 5-Hydroxytryptamine A Human X-ray 6DRX 6DRX_refined 3.1 A Intermediate 44 59 - - - - BRIL - lisuride
small-molecule Antagonist 5-hydroxytryptamine small-molecule No No McCorvy JD, Wacker D, Wang S, Agegnehu B, Liu J, Lansu K, Tribo AR, Olsen RHJ, Che T, Jin J, Roth BL 10.1038/s41594-018-0116-7 2018-08-29 Yes
PE2R4 EP4 Prostanoid A Human X-ray 5YHL 5YHL_refined 4.2 A Inactive 9 57 - - - - - Fab ONO-AE3-208-Br
small-molecule Antagonist PGE2, PGF, PGE1, PGI2, thromboxane A2, PGD2 small-molecule No No - 10.1038/S41589-018-0131-3 2018-12-05 Yes
CCR2 CCR2 Chemokine A Human X-ray 6GPX 6GPX_refined 2.7 B Inactive 16 70 - - - - Rubredoxin - MK-0812
small-molecule Antagonist CCL11, CCL13, CCL26, CCL8, CCL7, CCL24, CCL16, CCL2 peptide No No - - 2019-01-02 Yes
MTR1B MT2 Melatonin A Human X-ray 6ME7 6ME7_refined 3.2 A Inactive 1 79 - - - - Rubredoxin - CHEMBL15060
small-molecule Agonist melatonin small-molecule No No - - 2019-04-24 Yes
SUCR1 succinate Succinate A Rat X-ray 6RNK 6RNK_refined 1.9 A Active 65 90 - - - - - Nanobody-6 NF-56-EJ40
small-molecule Antagonist - - No No - - 2019-08-14 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 6PS0 6PS0_refined 3.4 A Inactive 0 68 - - - - T4-Lysozyme - carazolol
small-molecule Antagonist L-NOREPINEPHRINE, (-)-noradrenaline, Zn2+, noradrenaline, (-)-adrenaline small-molecule No No - - 2019-11-13 Yes
NTR1 NTS1 Neurotensin A Human Cryo-EM 6PWC 6PWC_refined 4.9 R Active 100 77 Beta Beta-arrestin-1 - 84 - Fab30 heavy chain
Fab30 light chain
CHEMBL48981
protein Agonist large neurotensin, large neuromedin N, neuromedin N, neurotensin peptide No No Yin W, Li Z, Jin M, Yin YL, de Waal PW, Pal K, Yin Y, Gao X, He Y, Gao J, Wang X, Zhang Y, Zhou H, Melcher K, Jiang Y, Cong Y, Edward Zhou X, Yu X, Eric Xu H 10.1038/S41422-019-0256-2 2019-12-04 Yes
OX1R OX1 Orexin A Human X-ray 6TP4 - 3.0 A Inactive 1 70 - - - - - - ACT-462206
small-molecule Antagonist orexin-A, orexin-B 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
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 2-arachidonoylglycerol, anandamide 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
ACM4 M4 Acetylcholine (muscarinic) A Human X-ray 6KP6 6KP6_refined 3.0 A Inactive 2 59 - - - - GlgA glycogen synthase - Apo (no ligand)
none Apo (no ligand) acetylcholine small-molecule No No Wang J, Wu M, Wu L, Xu Y, Li F, Wu Y, Popov P, Wang L, Bai F, Zhao S, Liu ZJ, Hua T 10.1107/S2052252520000597 2020-03-11 Yes
ADA2B α2B Adrenoceptors A Human Cryo-EM 6K41 - 2.9 R Active 100 54 Gi/o αo - 60 T4-Lysozyme scFv dexmedetomidine
small-molecule Agonist (-)-noradrenaline, (-)-adrenaline small-molecule No No Yuan D, Liu Z, Kaindl J, Maeda S, Zhao J, Sun X, Xu J, Gmeiner P, Wang HW, Kobilka BK 10.1038/S41589-020-0492-2 2020-04-15 Yes
DRD2 D2 Dopamine A Human Cryo-EM 6VMS - 3.8 R Active 100 63 Gi/o αi1 - 64 T4-Lysozyme scFv16 bromocriptine
small-molecule Agonist dopamine small-molecule No No Yin J, Chen KM, Clark MJ, Hijazi M, Kumari P, Bai XC, Sunahara RK, Barth P, Rosenbaum DM 10.1038/S41586-020-2379-5 2020-06-17 Yes
AA2AR A2A Adenosine A Human X-ray 6S0Q 6S0Q_refined 2.7 A Inactive 1 72 - - - - BRIL - ZM-241385
small-molecule Antagonist adenosine small-molecule No No - 10.1107/S2052252520011379 2020-07-15 Yes
SCTR secretin Glucagon B1 Human Cryo-EM 6WI9 6WI9_refined 4.3 R Active 100 84 Gs αs - 49 - Nanobody-35 SECRETIN
protein Agonist VIP, secretin peptide No No Dong M, Deganutti G, Piper SJ, Liang YL, Khoshouei M, Belousoff MJ, Harikumar KG, Reynolds CA, Glukhova A, Furness SGB, Christopoulos A, Danev R, Wootten D, Sexton PM, Miller LJ 10.1038/S41467-020-17791-4 2020-08-12 Yes
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 6X19 - 2.1 R Active 100 84 Gs αs - 89 - Nanobody-35 CHU-128
small-molecule Agonist glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon peptide No No Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, Senel P, Stewart GD, Liang YL, Glukhova A, Venugopal H, Christopoulos A, Furness SGB, Miller LJ, Reedtz-Runge S, Langmead CJ, Gloriam DE, Danev R, Sexton PM, Wootten D 10.1016/J.MOLCEL.2020.09.020 2020-09-09 Yes
AA2AR A2A Adenosine A Human X-ray 6LPJ 6LPJ_refined 1.8 A Inactive 1 72 - - - - BRIL - ZM-241385
small-molecule Antagonist adenosine small-molecule No Yes 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
DRD2 D2 Dopamine A Human X-ray 7DFP 7DFP_refined 3.1 A Inactive 1 57 - - - - BRIL Fab heavy chain
Fab light chain
spiperone
small-molecule Antagonist dopamine small-molecule No No Im D, Inoue A, Fujiwara T, Nakane T, Yamanaka Y, Uemura T, Mori C, Shiimura Y, Kimura KT, Asada H, Nomura N, Tanaka T, Yamashita A, Nango E, Tono K, Kadji FMN, Aoki J, Iwata S, Shimamura T 10.1038/S41467-020-20221-0 2020-12-30 Yes
AGRG3 ADGRG3 ADGRG B2 Human Cryo-EM 7D77 - 2.9 R Active - 48 Gi/o αo - 61 - scFv16 HYDROCORTISONE
small-molecule Agonist - - No No Ping YQ, Mao C, Xiao P, Zhao RJ, Jiang Y, Yang Z, An WT, Shen DD, Yang F, Zhang H, Qu C, Shen Q, Tian C, Li ZJ, Li S, Wang GY, Tao X, Wen X, Zhong YN, Yang J, Yi F, Yu X, Xu HE, Zhang Y, Sun JP 10.1038/S41586-020-03083-W 2021-02-03 Yes
OX2R OX2 Orexin A Human Cryo-EM 7L1V - 3.0 R Active 100 64 Gs αs Engineered G alpha 58 - scFv16
Nanobody-51
compound 1 [PMID: 33547286]
small-molecule Agonist orexin-A, orexin-B peptide No No Hong C, Byrne NJ, Zamlynny B, Tummala S, Xiao L, Shipman JM, Partridge AT, Minnick C, Breslin MJ, Rudd MT, Stachel SJ, Rada VL, Kern JC, Armacost KA, Hollingsworth SA, O'Brien JA, Hall DL, McDonald TP, Strickland C, Brooun A, Soisson SM, Hollenstein K 10.1038/S41467-021-21087-6 2021-02-10 Yes
CASR CaS Calcium-sensing C Human Cryo-EM 7DTV 7DTV_refined 3.5 A Active - 72 - - - - - - Calcium
L-tryptophan
small-molecule
small-molecule
Agonist
PAM
Ca2+, Mg2+, L-tryptophan, spermine small-molecule No No Ling S, Shi P, Liu S, Meng X, Zhou Y, Sun W, Chang S, Zhang X, Zhang L, Shi C, Sun D, Liu L, Tian C 10.1038/S41422-021-00474-0 2021-03-10 Yes
5HT1E 5-HT1E 5-Hydroxytryptamine A Human Cryo-EM 7E33 7E33_refined 2.9 R Active 100 70 Gi/o αi1 - 61 - scFv16 BRL-54443
small-molecule Agonist 5-hydroxytryptamine, tryptamine 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
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
Ca2+, Mg2+, L-tryptophan, spermine small-molecule No No - - 2021-06-30 Yes
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 7E14 - 2.9 R Active 100 81 Gs αs - 49 - Nanobody-35 N-Tert-butyl-6,7-dichloroquinoxalin-2-amine
orforglipron
small-molecule
small-molecule
Ago-PAM
Agonist
glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon peptide No No - 10.1038/S41467-021-24058-Z 2021-07-07 Yes
GRM5 mGlu5 Metabotropic glutamate C Human X-ray 7P2L 7P2L_refined 2.5 A Inactive - 21 - - - - T4-Lysozyme - alloswitch-1
small-molecule NAM L-glutamic acid small-molecule No No Nasrallah C, Cannone G, Briot J, Rottier K, Berizzi AE, Huang CY, Quast RB, Hoh F, Baneres JL, Malhaire F, Berto L, Dumazer A, Font-Ingles J, Gomez-Santacana X, Catena J, Kniazeff J, Goudet C, Llebaria A, Pin JP, Vinothkumar KR, Lebon G 10.1016/J.CELREP.2021.109648 2021-09-08 Yes
S1PR3 S1P3 Lysophospholipid (S1P) A Human Cryo-EM 7EW4 7EW4_refined 3.2 R Active 100 76 Gi/o αi1 - 64 - scFv16 CYM-5541
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
ACM1 M1 Acetylcholine (muscarinic) A Human X-ray 6ZG9 6ZG9_refined 2.5 A Inactive 2 62 - - - - T4-Lysozyme - 7-fluoro-5-methyl-3-[1-(oxan-4-yl)piperidin-4-yl]-1H-benzimidazol-2-one
small-molecule Agonist acetylcholine small-molecule No No Brown AJH, Bradley SJ, Marshall FH, Brown GA, Bennett KA, Brown J, Cansfield JE, Cross DM, de Graaf C, Hudson BD, Dwomoh L, Dias JM, Errey JC, Hurrell E, Liptrot J, Mattedi G, Molloy C, Nathan PJ, Okrasa K, Osborne G, Patel JC, Pickworth M, Robertson N, Shahabi S, Bundgaard C, Phillips K, Broad LM, Goonawardena AV, Morairty SR, Browning M, Perini F, Dawson GR, Deakin JFW, Smith RT, Sexton PM, Warneck J, Vinson M, Tasker T, Tehan BG, Teobald B, Christopoulos A, Langmead CJ, Jazayeri A, Cooke RM, Rucktooa P, Congreve MS, Weir M, Tobin AB 10.1016/J.CELL.2021.11.001 2021-10-06 Yes
MRGX2 MRGPRX2 A orphans A Human Cryo-EM 7S8O - 2.6 R Active 100 78 Gi/o αi1 - 62 BRIL scFv16 (R)-ZINC-3573
small-molecule Agonist PAMP-20 peptide No No Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL 10.1038/S41586-021-04126-6 2021-11-17 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
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
5HT2A 5-HT2A 5-Hydroxytryptamine A Human X-ray 7WC4 7WC4_refined 3.2 A Inactive 1 61 - - - - BRIL - 5-hydroxytryptamine
small-molecule Agonist 5-hydroxytryptamine, tryptamine small-molecule No No Cao D, Yu J, Wang H, Luo Z, Liu X, He L, Qi J, Fan L, Tang L, Chen Z, Li J, Cheng J, Wang S 10.1126/SCIENCE.ABL8615 2022-01-26 Yes
CASR CaS Calcium-sensing C Human Cryo-EM 7SIM 7SIM_refined 2.7 A Active - 72 - - - - - - Cyclomethyltryptophan
small-molecule Agonist Ca2+, Mg2+, L-tryptophan, spermine small-molecule No No Park J, Zuo H, Frangaj A, Fu Z, Yen LY, Zhang Z, Mosyak L, Slavkovich VN, Liu J, Ray KM, Cao B, Vallese F, Geng Y, Chen S, Grassucci R, Dandey VP, Tan YZ, Eng E, Lee Y, Kloss B, Liu Z, Hendrickson WA, Potter CS, Carragher B, Graziano J, Conigrave AD, Frank J, Clarke OB, Fan QR 10.1073/PNAS.2115849118 2022-01-19 Yes
MSHR MC1 Melanocortin A Human Cryo-EM 7F4D - 3.0 R Active 100 83 Gs αs - 59 - Nanobody-35 INTERMEDINE
protein Agonist β-MSH, α-MSH, ACTH, γ-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
LPAR1 LPA1 Lysophospholipid (LPA) A Human Cryo-EM 7TD2 - 3.1 R Active 100 80 Gi/o αi1 - 62 - - lysophosphatidic acid
small-molecule Agonist 1-O-Oleoyl-D-glycerol 3-phosphoric acid small-molecule No No Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY 10.1038/S41467-022-28417-2 2022-02-09 Yes
CALCR CT Calcitonin B1 Human Cryo-EM 7TYN - 2.6 R Active 100 79 Gs αs - 58 - Nanobody-35 calcitonin (salmon synthetic)
small-molecule Agonist adrenomedullin, α-CGRP, amylin, calcitonin, adrenomedullin 2/intermedin, calcitonin (salmon), β-CGRP 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 2022-03-30 Yes
FPR2 FPR2/ALX Formylpeptide A Human Cryo-EM 7WVW - 3.1 R Active 100 85 Gi/o αi2 - 63 BRIL - FME-TYR-PHE-ILE-ASN-ILE-LEU-THE-LEU
peptide Agonist aspirin triggered lipoxin A4, LXA4, LTC4, serum amyloid A, aspirin-triggered resolvin D1, annexin I, LL-37, PrP106-126, fMet-Leu-Phe, 15-deoxy-LXA4, resolvin D1, humanin, LTD4 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
FPR2 FPR2/ALX Formylpeptide A Human Cryo-EM 7WVX - 2.8 R Active 100 85 Gi/o αi2 - 61 BRIL - humanin
peptide Agonist aspirin triggered lipoxin A4, LXA4, LTC4, serum amyloid A, aspirin-triggered resolvin D1, annexin I, LL-37, PrP106-126, fMet-Leu-Phe, 15-deoxy-LXA4, resolvin D1, humanin, LTD4 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
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
ACM4 M4 Acetylcholine (muscarinic) A Human Cryo-EM 7V69 - 3.4 R Active 100 58 Gi/o αi1 - 62 - scFv16 Apo (no ligand)
none Apo (no ligand) 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
DRD1 D1 Dopamine A Human Cryo-EM 7F1O - 3.1 F Active 100 62 Gs αs - 60 - Nanobody-35 dopamine
small-molecule Agonist L-NOREPINEPHRINE, (-)-noradrenaline, 5-hydroxytryptamine, dopamine, 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
DRD1 D1 Dopamine A Human Cryo-EM 7X2C 7X2C_refined 3.2 F Active 100 63 Gs αs - 58 - Nanobody-35 fenoldopam
small-molecule Agonist L-NOREPINEPHRINE, (-)-noradrenaline, 5-hydroxytryptamine, dopamine, noradrenaline small-molecule No No Teng X, Chen S, Nie Y, Xiao P, Yu X, Shao Z, Zheng S 10.1038/S41467-022-30929-W 2022-06-29 Yes
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 7X8S 7X8S_refined 3.1 R Active 100 65 Gs αs - 60 - Nanobody-35 WB4-24
small-molecule Agonist glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon peptide No No Cong Z, Zhou Q, Li Y, Chen LN, Zhang ZC, Liang A, Liu Q, Wu X, Dai A, Xia T, Wu W, Zhang Y, Yang D, Wang MW 10.1073/PNAS.2200155119 2022-06-29 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
GPBAR GPBA Bile acid A Human Cryo-EM 7XTQ 7XTQ_refined 3.2 R Active 100 83 Gs αs - 58 - Nanobody-35 CHEMBL2181246
small-molecule Agonist cholic acid, deoxycholic acid, lithocholic acid, chenodeoxycholic acid small-molecule No No Ma L, Yang F, Wu X, Mao C, Guo L, Miao T, Zang SK, Jiang X, Shen DD, Wei T, Zhou H, Wei Q, Li S, Shu Q, Feng S, Jiang C, Chu B, Du L, Sun JP, Yu X, Zhang Y, Zhang P 10.1073/PNAS.2117054119 2022-07-06 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
OXYR OT Vasopressin and oxytocin A Human Cryo-EM 7QVM - 3.3 R Active 100 64 Gi/o αo - 59 - scFv16 oxytocin
peptide Agonist vasopressin, oxytocin peptide No No Waltenspuhl Y, Ehrenmann J, Vacca S, Thom C, Medalia O, Pluckthun A 10.1038/S41467-022-31325-0 2022-08-10 Yes
TSHR TSH Glycoprotein hormone A Human Cryo-EM 7XW6 - 2.8 R Active 100 74 Gs αs - 59 - Nanobody-35 M22 antibody light chain
M22 antibody heavy chain
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 2022-08-17 Yes
AGRG2 ADGRG2 ADGRG B2 Mouse Cryo-EM 7XKF - 2.4 R Active - 26 Gs αs - 57 - Nanobody-35 PRASTERONE
small-molecule Agonist - - No No Lin H, Xiao P, Bu RQ, Guo S, Yang Z, Yuan D, Zhu ZL, Zhang CX, He QT, Zhang C, Ping YQ, Zhao RJ, Ma CS, Liu CH, Zhang XN, Jiang D, Huang S, Xi YT, Zhang DL, Xue CY, Yang BS, Li JY, Lin HC, Zeng XH, Zhao H, Xu WM, Yi F, Liu Z, Sun JP, Yu X 10.1038/S41589-022-01084-6 2022-08-10 Yes
V2R V2 Vasopressin and oxytocin A Human Cryo-EM 7R0C - 4.7 A Active 100 76 Beta Beta-arrestin-1 - 84 - scFv30 vasopressin
peptide Agonist vasopressin, oxytocin peptide No No Bous J, Fouillen A, Orcel H, Trapani S, Cong X, Fontanel S, Saint-Paul J, Lai-Kee-Him J, Urbach S, Sibille N, Sounier R, Granier S, Mouillac B, Bron P 10.1126/SCIADV.ABO7761 2022-09-14 Yes
AGRF1 ADGRF1 ADGRF B2 Human Cryo-EM 7WXW - 2.8 R Active - 30 Gs αs Mini-Gs 59 - Nanobody-35 Apo (no ligand)
none Apo (no ligand) - - No No Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y 10.1038/S41467-022-33173-4 2022-09-28 Yes
T2R46 TAS2R46 Taste 2 T Human Cryo-EM 7XP4 - 3.0 R Active - 97 Gi/o αgust - 63 - Nanobody-35 Apo (no ligand)
none Apo (no ligand) - - No No Xu W, Wu L, Liu S, Liu X, Cao X, Zhou C, Zhang J, Fu Y, Guo Y, Wu Y, Tan Q, Wang L, Liu J, Jiang L, Fan Z, Pei Y, Yu J, Cheng J, Zhao S, Hao X, Liu ZJ, Hua T 10.1126/SCIENCE.ABO1633 2022-10-12 Yes
VIPR1 VPAC1 VIP and PACAP B1 Human Cryo-EM 8E3Y - 2.3 R Active 100 81 Gs αs - 56 - Nanobody-35 [Ac-His1]PACAP-27
peptide Agonist VIP, secretin, PACAP-38, PHI, GHRH, PACAP-27, PHM peptide No No - - 2022-11-23 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 8A6E 8A6E_refined 1.8 A Inactive 22 87 - - - - - - Retinal (11-cis)
small-molecule Agonist - - No No Gruhl T, Weinert T, Rodrigues MJ, Milne CJ, Ortolani G, Nass K, Nango E, Sen S, Johnson PJM, Cirelli C, Furrer A, Mous S, Skopintsev P, James D, Dworkowski F, Bath P, Kekilli D, Ozerov D, Tanaka R, Glover H, Bacellar C, Brunle S, Casadei CM, Diethelm AD, Gashi D, Gotthard G, Guixa-Gonzalez R, Joti Y, Kabanova V, Knopp G, Lesca E, Ma P, Martiel I, Muhle J, Owada S, Pamula F, Sarabi D, Tejero O, Tsai CJ, Varma N, Wach A, Boutet S, Tono K, Nogly P, Deupi X, Iwata S, Neutze R, Standfuss J, Schertler G, Panneels V 10.1038/S41586-023-05863-6 2023-03-29 Yes
GPR21 GPR21 A orphans A Human Cryo-EM 8HJ2 8HJ2_refined 3.8 R Active 100 81 Gs αs Mini-Gs 61 - Nanobody-35 Apo (no ligand)
none Apo (no ligand) - - No No - - 2023-03-15 Yes
ACM2 M2 Acetylcholine (muscarinic) A Human Cryo-EM 7T96 7T96_refined 3.2 A Active 100 59 Gi/o αo - 62 - scFv16 acetylcholine
LY2119620
small-molecule
small-molecule
Agonist
PAM
acetylcholine small-molecule No No - - 2023-01-25 Yes
HCAR2 HCA2 Hydroxycarboxylic acid A Human X-ray 7ZLY - 2.7 A Active 65 83 - - - - BRIL - Apo (no ligand)
none Apo (no ligand) β-D-hydroxybutyric acid, butyric acid small-molecule No No Yang Y, Kang HJ, Gao R, Wang J, Han GW, DiBerto JF, Wu L, Tong J, Qu L, Wu Y, Pileski R, Li X, Zhang XC, Zhao S, Kenakin T, Wang Q, Stevens RC, Peng W, Roth BL, Rao Z, Liu ZJ 10.1038/S41467-023-37177-6 2023-04-12 Yes
SSR2 SST2 Somatostatin A Human Cryo-EM 7YAE 7YAE_refined 3.4 E Active 100 76 Gi/o αi1 - 64 - scFv16 Octreotide
peptide Agonist SRIF-28, SRIF-14, cortistatin-14, CST-17 peptide No No Zhao J, Fu H, Yu J, Hong W, Tian X, Qi J, Sun S, Zhao C, Wu C, Xu Z, Cheng L, Chai R, Yan W, Wei X, Shao Z 10.1038/S41467-023-36673-Z 2023-04-19 Yes
PTH1R PTH1 Parathyroid hormone B1 Human Cryo-EM 7Y36 - 2.8 R Active 100 63 Gs αs - 57 - Nanobody-35 teriparatide
peptide Agonist PTHrP, PTH, PTHrP-(1-36), TIP39 peptide No No - - 2023-07-05 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 PGE2, PGF, PGI2, thromboxane A2, PGD2 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
OPSD Rhodopsin Opsins A Japanese flying squid X-ray 2Z73 2Z73_refined 2.5 A Inactive 16 78 - - - - - - Retinal (11-cis)
small-molecule Inverse agonist - - No No - 10.1038/NATURE06925 2008-05-13 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 3D4S 3D4S_refined 2.8 A Inactive 0 67 - - - - T4-Lysozyme - timolol
small-molecule Inverse agonist L-NOREPINEPHRINE, (-)-noradrenaline, Zn2+, noradrenaline, (-)-adrenaline small-molecule No No - 10.1016/J.STR.2008.05.001 2008-06-17 Yes
AA2AR A2A Adenosine A Human X-ray 3EML - 2.6 A Inactive 1 70 - - - - T4-Lysozyme - ZM-241385
small-molecule Antagonist adenosine small-molecule No No - 10.1126/SCIENCE.1164772 2008-10-14 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 3NY8 3NY8_refined 2.8 A Inactive 0 67 - - - - T4-Lysozyme - ICI 118551
small-molecule Inverse agonist L-NOREPINEPHRINE, (-)-noradrenaline, Zn2+, noradrenaline, (-)-adrenaline small-molecule No No - - 2010-08-11 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 3CAP - 2.9 A Active 98 94 - - - - - - Apo (no ligand)
none Apo (no ligand) - - No No - 10.1038/NATURE07063 2008-06-24 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 3NY9 3NY9_refined 2.8 A Inactive 0 67 - - - - T4-Lysozyme - CHEMBL1233771
small-molecule Inverse agonist L-NOREPINEPHRINE, (-)-noradrenaline, Zn2+, noradrenaline, (-)-adrenaline small-molecule No No - 10.1021/JA105108Q 2010-08-11 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 3NYA 3NYA_refined 3.2 A Inactive 0 67 - - - - T4-Lysozyme - CHEMBL1160734
small-molecule Antagonist L-NOREPINEPHRINE, (-)-noradrenaline, Zn2+, noradrenaline, (-)-adrenaline small-molecule No No - - 2010-08-11 Yes
CXCR4 CXCR4 Chemokine A Human X-ray 3OE0 - 2.9 A Inactive 4 78 - - - - T4-Lysozyme - CVX15
peptide Antagonist CXCL12ε, CXCL12α, CXCL12, CXCL12γ, CXCL12β, CXCL12φ, CXCL12δ peptide No No - - 2010-10-27 Yes
CXCR4 CXCR4 Chemokine A Human X-ray 3OE6 3OE6_refined 3.2 A Inactive 4 77 - - - - T4-Lysozyme - isothiourea-1t
small-molecule Antagonist CXCL12ε, CXCL12α, CXCL12, CXCL12γ, CXCL12β, CXCL12φ, CXCL12δ peptide No No - - 2010-10-27 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 2VT4 - 2.7 B Inactive 0 57 - - - - - - (S)-Cyanopindolol
small-molecule Antagonist - - No No - 10.1038/NATURE07101 2008-06-24 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 3KJ6 - 3.4 A Inactive 1 54 - - - - - Antibody - - - L-NOREPINEPHRINE, (-)-noradrenaline, Zn2+, noradrenaline, (-)-adrenaline small-molecule No No - 10.1038/NATURE08650 2010-02-16 Yes
CXCR4 CXCR4 Chemokine A Human X-ray 3ODU 3ODU_refined 2.5 A Inactive 4 83 - - - - T4-Lysozyme - isothiourea-1t
small-molecule Antagonist CXCL12ε, CXCL12α, CXCL12, CXCL12γ, CXCL12β, CXCL12φ, CXCL12δ peptide No No - - 2010-10-27 Yes
CXCR4 CXCR4 Chemokine A Human X-ray 3OE8 3OE8_refined 3.1 A Inactive 4 76 - - - - T4-Lysozyme - isothiourea-1t
small-molecule Antagonist CXCL12ε, CXCL12α, CXCL12, CXCL12γ, CXCL12β, CXCL12φ, CXCL12δ peptide No No - 10.1126/SCIENCE.1194396 2010-10-27 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 3OAX - 2.6 A Inactive 22 100 - - - - - - Retinal (11-cis)
small-molecule Inverse agonist - - No No - 10.1016/J.BPJ.2010.08.003 2011-01-19 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 3P0G 3P0G_refined 3.5 A Active 99 69 - - - - T4-Lysozyme Nanobody CHEMBL1615159
small-molecule Agonist L-NOREPINEPHRINE, (-)-noradrenaline, Zn2+, noradrenaline, (-)-adrenaline small-molecule No No - 10.1038/NATURE09648 2011-01-19 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 3PQR 3PQR_refined 2.9 A Active 100 94 Gi/o αt1 Only H5 3 - - Retinal (all-trans)
small-molecule Agonist - - No No - 10.1038/NATURE09789 2011-03-09 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 - 10.1038/NATURE09795 2011-03-16 Yes
AA2AR A2A Adenosine A Human X-ray 2YDV 2YDV_refined 2.6 A Active 65 75 - - - - - - NECA
small-molecule Agonist adenosine small-molecule No No - - 2011-05-18 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 2YCZ 2YCZ_refined 3.7 B Inactive 0 60 - - - - - - Iodocyanopindolol
small-molecule Antagonist - - No No - - 2011-06-01 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 2YCY - 3.2 A Inactive 0 60 - - - - - - (S)-Cyanopindolol
small-molecule Antagonist - - No No - - 2011-06-08 Yes