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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 noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ 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 - - - noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ 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 - - - noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ 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 noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ 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, 5-HT-moduline, tryptamine 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-(1-8), [Met]enkephalin, endomorphin-1, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin B, α-neoendorphin 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-(1-7), angiotensin II, angiotensin III 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, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide 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-1, endothelin-2, endothelin-3 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, PGD3, PGF2α, thromboxane A2, PGJ2, PGI2, 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, PGD3, PGF2α, thromboxane A2, PGJ2, PGI2, 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, PGF2α, thromboxane A2, PGI2, PGE1, 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 CCL2, CCL8, CCL11, CCL13, CCL14, CCL7, CCL5, CCL4, CCL16, CCL3 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 PTH, PTHrP-(1-36), TIP39, PTHrP 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 noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ 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 (-)-adrenaline, (-)-noradrenaline 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 LTE4, LTD4, LTC4 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-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
EDNRB ETB Endothelin A Human X-ray 6LRY 6LRY_refined 3.0 A Inactive 15 70 - - - - T4-Lysozyme - sarafotoxin S6b
peptide Agonist endothelin-1, endothelin-2, endothelin-3 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 (-)-adrenaline, (-)-noradrenaline 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 CCL20, beta-defensin 4A 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 noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ 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 CXCL3, CXCL1, CXCL6, CXCL2, CXCL7, CXCL5, 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 noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, (-)-noradrenaline 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, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide 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 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
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 noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, 5-hydroxytryptamine, dopamine 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 agouti-related protein, β-MSH, α-MSH, γ-MSH, ACTH 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 desulfated cholecystokinin-8, CCK-33, CCK-8, CCK-58, CCK-4, CCK-39, gastrin-17 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) CCL2, CCL8, CCL11, CCL13, CCL14, CCL7, CCL5, CCL4, CCL16, CCL3 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 desulfated cholecystokinin-8, CCK-33, CCK-8, CCK-58, CCK-4, CCK-39, gastrin-17 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 cholecystokinin-8, desulfated gastrin-17, CCK-33, CCK-8, CCK-58, desulfated gastrin-71, desulfated gastrin-14, CCK-4, desulfated gastrin-34, gastrin-34, gastrin-14, CCK-39, gastrin-17, gastrin-71 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 desulfated cholecystokinin-8, CCK-33, CCK-8, CCK-58, CCK-4, CCK-39, gastrin-17 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 agouti-related protein, β-MSH, α-MSH, γ-MSH, ACTH 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 sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate 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 resolvin D1, serum amyloid A, 15-deoxy-LXA4, LTC4, LL-37, humanin, LTD4, aspirin triggered lipoxin A4, annexin I, aspirin-triggered resolvin D1, fMet-Leu-Phe, PrP106-126, LXA4 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-14, CST-17, cortistatin-14, SRIF-28 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 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
CALCR CT Calcitonin B1 Human Cryo-EM 7TYL - 3.3 R Active 100 78 Gs αs - 58 - Nanobody-35 Amylin rat
peptide Agonist β-CGRP, α-CGRP, calcitonin, calcitonin (salmon), amylin, adrenomedullin, 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
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 β-CGRP, α-CGRP, calcitonin, calcitonin (salmon), amylin, adrenomedullin, 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
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 7α,25-dihydroxycholesterol, 7α,27-dihydroxycholesterol, 7β, 27-dihydroxycholesterol, 7β, 25-dihydroxycholesterol, 7α-hydroxycholesterol, 25-hydroxycholesterol, 27-hydroxycholesterol, 7β-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, PACAP-27, secretin, PHI, GHRH, PACAP-38 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 [Hyp3]bradykinin, [des-Arg10]kallidin, bradykinin, Lys-[Hyp3]-bradykinin, kallidin, [des-Arg9]bradykinin, T-kinin 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 galanin-like peptide, spexin-1, 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, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide 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 sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate 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 PTH, PTHrP-(1-36), TIP39, PTHrP 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 2, corticotrophin-releasing hormone, urocortin 3, 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-(1-8), [Met]enkephalin, endomorphin-1, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin B, α-neoendorphin 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 relaxin-3, INSL5, 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, neuropeptide Y-(3-36), peptide YY, pancreatic polypeptide, 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		 neuromedin N, neurotensin 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 neuromedin N, neurotensin 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 neuromedin N, neurotensin 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 noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ 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		 oleic acid, docosahexaenoic acid, α-linolenic acid, myristic 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-(1-8), β-neoendorphin, big dynorphin, [Met]enkephalin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin B, α-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, PGF2α, thromboxane A2, PGI2, PGE1, 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 CCL2, CCL8, CCL11, CCL13, CCL24, CCL7, CCL26, CCL16 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 noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ 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 neuromedin N, large neurotensin, neurotensin, large neuromedin N 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-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
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 (-)-adrenaline, (-)-noradrenaline 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 secretin, VIP 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, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide 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-B, orexin-A 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		 spermine, L-tryptophan, Ca2+, Mg2+ 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		 spermine, L-tryptophan, Ca2+, Mg2+ 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, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide 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 sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate 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 spermine, L-tryptophan, Ca2+, Mg2+ 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 γ-MSH, ACTH, 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
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 β-CGRP, α-CGRP, calcitonin, calcitonin (salmon), amylin, adrenomedullin, 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 2022-03-30 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 resolvin D1, serum amyloid A, 15-deoxy-LXA4, LTC4, LL-37, humanin, LTD4, aspirin triggered lipoxin A4, annexin I, aspirin-triggered resolvin D1, fMet-Leu-Phe, PrP106-126, LXA4 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 resolvin D1, serum amyloid A, 15-deoxy-LXA4, LTC4, LL-37, humanin, LTD4, aspirin triggered lipoxin A4, annexin I, aspirin-triggered resolvin D1, fMet-Leu-Phe, PrP106-126, LXA4 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 noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, 5-hydroxytryptamine, dopamine 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 noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, 5-hydroxytryptamine, dopamine 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, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide 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 deoxycholic acid, chenodeoxycholic acid, lithocholic acid, cholic 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 oxytocin, vasopressin 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 oxytocin, vasopressin 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, PACAP-27, secretin, PHI, PHM, GHRH, PACAP-38 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-14, CST-17, cortistatin-14, SRIF-28 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 PTH, PTHrP-(1-36), TIP39, PTHrP 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, PGF2α, thromboxane A2, PGI2, 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 noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ 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 noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ 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 noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ 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 noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ 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 CXCL12γ, CXCL12ε, CXCL12, CXCL12δ, CXCL12β, CXCL12φ, CXCL12α 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 CXCL12γ, CXCL12ε, CXCL12, CXCL12δ, CXCL12β, CXCL12φ, CXCL12α 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 - - - noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ 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 CXCL12γ, CXCL12ε, CXCL12, CXCL12δ, CXCL12β, CXCL12φ, CXCL12α 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 CXCL12γ, CXCL12ε, CXCL12, CXCL12δ, CXCL12β, CXCL12φ, CXCL12α 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 noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ 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
HRH1 H1 Histamine A Human X-ray 3RZE 3RZE_refined 3.1 A Inactive 2 55 - - - - T4-Lysozyme - doxepin
small-molecule Antagonist histamine small-molecule No No - 10.1038/NATURE10236 2011-06-15 Yes
AA2AR A2A Adenosine A Human X-ray 3REY 3REY_refined 3.3 A Inactive 1 71 - - - - - - xanthine amine congener
small-molecule Antagonist adenosine small-molecule No No - - 2011-09-07 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 3SN6 - 3.2 R Active 100 69 Gs αs - 89 T4-Lysozyme Antibody CHEMBL1615159
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ small-molecule No No - 10.1038/NATURE10361 2011-07-20 Yes
ACM2 M2 Acetylcholine (muscarinic) A Human X-ray 3UON 3UON_refined 3.0 A Inactive 2 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
AA2AR A2A Adenosine A Human X-ray 3VG9 3VG9_refined 2.7 A Inactive 1 72 - - - - - Antibody fab fragment light chain
Antibody fab fragment heavy chain		 ZM-241385
small-molecule Antagonist adenosine small-molecule No No Hino T, Arakawa T, Iwanari H, Yurugi-Kobayashi T, Ikeda-Suno C, Nakada-Nakura Y, Kusano-Arai O, Weyand S, Shimamura T, Nomura N, Cameron AD, Kobayashi T, Hamakubo T, Iwata S, Murata T 10.1038/NATURE10750 2012-02-01 Yes
AA2AR A2A Adenosine A Human X-ray 3VGA - 3.1 A Inactive 1 72 - - - - - - ZM-241385
small-molecule Antagonist adenosine small-molecule No No - - 2012-02-01 Yes
S1PR1 S1P1 Lysophospholipid (S1P) A Human X-ray 3V2Y 3V2Y_refined 2.8 A Inactive 1 76 - - - - T4-Lysozyme - W146
small-molecule Antagonist sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate small-molecule No No - - 2012-02-15 Yes
OPRD δ Opioid A Mouse X-ray 4EJ4 4EJ4_refined 3.4 A Inactive 4 76 - - - - T4-Lysozyme - naltrindole
small-molecule Antagonist [Leu]enkephalin, α-neoendorphin, [Met]enkephalin peptide No No Granier S, Manglik A, Kruse AC, Kobilka TS, Thian FS, Weis WI, Kobilka BK 10.1038/NATURE11111 2012-05-16 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 4AMJ 4AMJ_refined 2.3 B Inactive 0 62 - - - - - - CHEMBL3799125
small-molecule Inverse agonist - - No No Warne T, Edwards PC, Leslie AG, Tate CG 10.1016/J.STR.2012.03.014 2012-05-23 Yes
AA2AR A2A Adenosine A Human X-ray 4EIY 4EIY_refined 1.8 A Inactive 1 72 - - - - BRIL - ZM-241385
small-molecule Antagonist adenosine small-molecule No Yes Liu W, Chun E, Thompson AA, Chubukov P, Xu F, Katritch V, Han GW, Roth CB, Heitman LH, IJzerman AP, Cherezov V, Stevens RC 10.1126/SCIENCE.1219218 2012-07-25 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 4GBR 4GBR_refined 4.0 A Inactive 0 69 - - - - T4-Lysozyme - Carazolol
small-molecule Inverse agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ small-molecule No No Zou Y, Weis WI, Kobilka BK 10.1371/JOURNAL.PONE.0046039 2012-10-24 Yes
5HT1B 5-HT1B 5-Hydroxytryptamine A Human X-ray 4IAQ 4IAQ_refined 2.8 A Inactive 15 70 - - - - BRIL - dihydroergotamine
small-molecule Agonist 5-hydroxytryptamine, 5-HT-moduline, tryptamine small-molecule No No - - 2013-03-13 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 3ZPQ 3ZPQ_refined 2.8 B Inactive 0 62 - - - - - - CHEMBL200234
small-molecule Antagonist - - No Yes 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
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 3ZPR 3ZPR_refined 2.7 B Inactive 0 61 - - - - - - CHEMBL1559535
small-molecule Antagonist - - No Yes 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
CRFR1 CRF1 Corticotropin-releasing factor B1 Human X-ray 4K5Y - 3.0 C Inactive 17 60 - - - - T4-Lysozyme - CP 376,395
small-molecule Antagonist urocortin 2, corticotrophin-releasing hormone, urocortin 1 peptide No No Hollenstein K, Kean J, Bortolato A, Cheng RK, Dore AS, Jazayeri A, Cooke RM, Weir M, Marshall FH 10.1038/NATURE12357 2013-07-17 Yes
CCR5 CCR5 Chemokine A Human X-ray 4MBS 4MBS_refined 2.7 A Inactive 16 83 - - - - Rubredoxin - maraviroc
small-molecule Antagonist CCL2, CCL8, CCL11, CCL13, CCL14, CCL7, CCL5, CCL4, CCL16, CCL3 peptide No No Tan Q, Zhu Y, Li J, Chen Z, Han GW, Kufareva I, Li T, Ma L, Fenalti G, Li J, Zhang W, Xie X, Yang H, Jiang H, Cherezov V, Liu H, Stevens RC, Zhao Q, Wu B 10.1126/SCIENCE.1241475 2013-09-11 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 4J4Q 4J4Q_refined 2.7 A Active 100 94 Gi/o αt1 Only H5 3 - - B-Octylglucoside
small-molecule unknown - - No No Park JH, Morizumi T, Li Y, Hong JE, Pai EF, Hofmann KP, Choe HW, Ernst OP 10.1002/ANIE.201302374 2013-10-30 Yes
ACM2 M2 Acetylcholine (muscarinic) A Human X-ray 4MQS 4MQS_refined 3.5 A Active 99 59 - - - - - Nanobody iperoxo
small-molecule Agonist acetylcholine small-molecule No No Kruse AC, Ring AM, Manglik A, Hu J, Hu K, Eitel K, Hubner H, Pardon E, Valant C, Sexton PM, Christopoulos A, Felder CC, Gmeiner P, Steyaert J, Weis WI, Garcia KC, Wess J, Kobilka BK 10.1038/NATURE12735 2013-11-27 Yes
ACM2 M2 Acetylcholine (muscarinic) A Human X-ray 4MQT 4MQT_refined 3.7 A Active 99 59 - - - - - Nanobody iperoxo
LY2119620
small-molecule
small-molecule		 Agonist
PAM		 acetylcholine small-molecule No No Kruse AC, Ring AM, Manglik A, Hu J, Hu K, Eitel K, Hubner H, Pardon E, Valant C, Sexton PM, Christopoulos A, Felder CC, Gmeiner P, Steyaert J, Weis WI, Garcia KC, Wess J, Kobilka BK 10.1038/NATURE12735 2013-11-27 Yes
SMO SMO Frizzled F Human X-ray 4N4W 4N4W_refined 2.8 A Inactive 0 44 - - - - BRIL - SANT-1
small-molecule Antagonist - - No No Wang C, Wu H, Evron T, Vardy E, Han GW, Huang XP, Hufeisen SJ, Mangano TJ, Urban DJ, Katritch V, Cherezov V, Caron MG, Roth BL, Stevens RC 10.1038/NCOMMS5355 2014-01-22 Yes
NTR1 NTS1 Neurotensin A Rat X-ray 4BUO 4BUO_refined 2.8 A Inactive 3 72 - - - - - - neurotensin
peptide Agonist neuromedin N, neurotensin peptide No No - - 2014-01-29 Yes
NTR1 NTS1 Neurotensin A Rat X-ray 4BV0 4BV0_refined 3.1 A Inactive 3 70 - - - - - - neurotensin
peptide Agonist neuromedin N, neurotensin 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
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 4BVN 4BVN_refined 2.1 A Inactive 0 60 - - - - - - (S)-Cyanopindolol
small-molecule Antagonist - - No Yes Miller-Gallacher JL, Nehme R, Warne T, Edwards PC, Schertler GF, Leslie AG, Tate CG 10.1371/JOURNAL.PONE.0092727 2014-04-02 Yes
GRM5 mGlu5 Metabotropic glutamate C Human X-ray 4OO9 4OO9_refined 2.6 A Inactive - 20 - - - - T4-Lysozyme - MAVOGLURANT
small-molecule NAM L-glutamic acid small-molecule No No Dore AS, Okrasa K, Patel JC, Serrano-Vega M, Bennett K, Cooke RM, Errey JC, Jazayeri A, Khan S, Tehan B, Weir M, Wiggin GR, Marshall FH 10.1038/NATURE13396 2014-07-02 Yes
FFAR1 FFA1 Free fatty acid A Human X-ray 4PHU 4PHU_refined 2.3 A Intermediate 44 90 - - - - T4-Lysozyme - fasiglifam
small-molecule Allosteric agonist oleic acid, docosahexaenoic acid, α-linolenic acid, myristic 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
SMO SMO Frizzled F Human X-ray 4QIM 4QIM_refined 2.6 A Inactive 7 45 - - - - BRIL - ANTA XV
small-molecule Antagonist - - No No Wang C, Wu H, Evron T, Vardy E, Han GW, Huang XP, Hufeisen SJ, Mangano TJ, Urban DJ, Katritch V, Cherezov V, Caron MG, Roth BL, Stevens RC 10.1038/NCOMMS5355 2014-07-23 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
ACM3 M3 Acetylcholine (muscarinic) A Rat X-ray 4U15 4U15_refined 2.8 B 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
OPRD δ Opioid A Human X-ray 4RWA 4RWA_refined 3.3 A Inactive 4 77 - - - - BRIL - DIPP-NH2
peptide Antagonist dynorphin A-(1-8), [Met]enkephalin, endomorphin-1, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin B, α-neoendorphin peptide No No Fenalti G, Zatsepin NA, Betti C, Giguere P, Han GW, Ishchenko A, Liu W, Guillemyn K, Zhang H, James D, Wang D, Weierstall U, Spence JC, Boutet S, Messerschmidt M, Williams GJ, Gati C, Yefanov OM, White TA, Oberthuer D, Metz M, Yoon CH, Barty A, Chapman HN, Basu S, Coe J, Conrad CE, Fromme R, Fromme P, Tourwe D, Schiller PW, Roth BL, Ballet S, Katritch V, Stevens RC, Cherezov V 10.1038/NSMB.2965 2015-01-14 Yes
OPRD δ Opioid A Human X-ray 4RWD 4RWD_refined 2.7 A Inactive 4 79 - - - - BRIL - DIPP-NH2
peptide Antagonist dynorphin A-(1-8), [Met]enkephalin, endomorphin-1, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin B, α-neoendorphin peptide No Yes Fenalti G, Zatsepin NA, Betti C, Giguere P, Han GW, Ishchenko A, Liu W, Guillemyn K, Zhang H, James D, Wang D, Weierstall U, Spence JC, Boutet S, Messerschmidt M, Williams GJ, Gati C, Yefanov OM, White TA, Oberthuer D, Metz M, Yoon CH, Barty A, Chapman HN, Basu S, Coe J, Conrad CE, Fromme R, Fromme P, Tourwe D, Schiller PW, Roth BL, Ballet S, Katritch V, Stevens RC, Cherezov V 10.1038/NSMB.2965 2015-01-14 Yes
P2RY1 P2Y1 P2Y A Human X-ray 4XNV - 2.2 A Intermediate 44 78 - - - - Rubredoxin - BMS compound 16 [PMID:23368907]
small-molecule NAM 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 4UG2 4UG2_refined 2.6 A Active 65 71 - - - - - - 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
AGTR1 AT1 Angiotensin A Human X-ray 4YAY 4YAY_refined 2.9 A Inactive 5 79 - - - - BRIL - ZD-7155
small-molecule Antagonist angiotensin A, angiotensin III, angiotensin IV, angiotensin II peptide No No Zhang H, Unal H, Gati C, Han GW, Liu W, Zatsepin NA, James D, Wang D, Nelson G, Weierstall U, Sawaya MR, Xu Q, Messerschmidt M, Williams GJ, Boutet S, Yefanov OM, White TA, Wang C, Ishchenko A, Tirupula KC, Desnoyer R, Coe J, Conrad CE, Fromme P, Stevens RC, Katritch V, Karnik SS, Cherezov V 10.1016/J.CELL.2015.04.011 2015-04-22 Yes
LPAR1 LPA1 Lysophospholipid (LPA) A Human X-ray 4Z34 4Z34_refined 3.0 A Inactive 1 80 - - - - BRIL - ONO-9780307
small-molecule Antagonist 1-O-Oleoyl-D-glycerol 3-phosphoric acid small-molecule No No Chrencik JE, Roth CB, Terakado M, Kurata H, Omi R, Kihara Y, Warshaviak D, Nakade S, Asmar-Rovira G, Mileni M, Mizuno H, Griffith MT, Rodgers C, Han GW, Velasquez J, Chun J, Stevens RC, Hanson MA 10.1016/J.CELL.2015.06.002 2015-06-03 Yes
LPAR1 LPA1 Lysophospholipid (LPA) A Human X-ray 4Z35 4Z35_refined 2.9 A Inactive 1 80 - - - - BRIL - ONO-9910539
small-molecule Antagonist 1-O-Oleoyl-D-glycerol 3-phosphoric acid small-molecule No No Chrencik JE, Roth CB, Terakado M, Kurata H, Omi R, Kihara Y, Warshaviak D, Nakade S, Asmar-Rovira G, Mileni M, Mizuno H, Griffith MT, Rodgers C, Han GW, Velasquez J, Chun J, Stevens RC, Hanson MA 10.1016/J.CELL.2015.06.002 2015-06-03 Yes
OPSD Rhodopsin Opsins A Japanese flying squid X-ray 4WW3 4WW3_refined 2.8 A Inactive 16 78 - - - - - - Retinal (all-trans)
small-molecule Agonist - - No No Murakami M, Kouyama T 10.1371/JOURNAL.PONE.0126970 2015-06-17 Yes
NTR1 NTS1 Neurotensin A Rat X-ray 4XEE 4XEE_refined 2.9 A Active 79 71 - - - - T4-Lysozyme - neurotensin
peptide Agonist neuromedin N, neurotensin peptide No No Krumm BE, White JF, Shah P, Grisshammer R 10.1038/NCOMMS8895 2015-07-29 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
AGTR1 AT1 Angiotensin A Human X-ray 4ZUD 4ZUD_refined 2.8 A Inactive 5 75 - - - - BRIL - OLMESARTAN
small-molecule Inverse agonist angiotensin A, angiotensin III, angiotensin IV, angiotensin II 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
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 5F8U 5F8U_refined 3.4 A Inactive 0 57 - - - - - - (S)-Cyanopindolol
small-molecule Antagonist - - No No Leslie AG, Warne T, Tate CG 10.1038/NSMB.3130 2015-12-23 Yes
OX1R OX1 Orexin A Human X-ray 4ZJ8 4ZJ8_refined 2.8 A Inactive 1 72 - - - - GlgA glycogen synthase - suvorexant
small-molecule Antagonist orexin-B, orexin-A peptide No No Yin J, Babaoglu K, Brautigam CA, Clark L, Shao Z, Scheuermann TH, Harrell CM, Gotter AL, Roecker AJ, Winrow CJ, Renger JJ, Coleman PJ, Rosenbaum DM 10.1038/NSMB.3183 2016-03-09 Yes
OX1R OX1 Orexin A Human X-ray 4ZJC 4ZJC_refined 2.8 A Inactive 1 72 - - - - GlgA glycogen synthase - SB-674042
small-molecule Antagonist orexin-B, orexin-A peptide No No - - 2016-03-09 Yes
OPSD Rhodopsin Opsins A Human X-ray 5DGY 5DGY_refined 7.7 A Active 100 94 Visual S-arrestin - 86 T4-Lysozyme - Apo (no ligand)
none Apo (no ligand) - - No No Zhou XE, Gao X, Barty A, Kang Y, He Y, Liu W, Ishchenko A, White TA, Yefanov O, Han GW, Xu Q, de Waal PW, Suino-Powell KM, Boutet S, Williams GJ, Wang M, Li D, Caffrey M, Chapman HN, Spence JC, Fromme P, Weierstall U, Stevens RC, Cherezov V, Melcher K, Xu HE 10.1038/SDATA.2016.21 2016-03-23 Yes
GLR glucagon Glucagon B1 Human X-ray 5EE7 5EE7_refined 2.5 A Inactive 0 54 - - - - T4-Lysozyme - Octaethylene glycol monoethyl ether
MK-0893
small-molecule
small-molecule		 Antagonist
NAM		 glucagon peptide No No Jazayeri A, Dore AS, Lamb D, Krishnamurthy H, Southall SM, Baig AH, Bortolato A, Koglin M, Robertson NJ, Errey JC, Andrews SP, Teobald I, Brown AJ, Cooke RM, Weir M, Marshall FH 10.1038/NATURE17414 2016-04-20 Yes
CRFR1 CRF1 Corticotropin-releasing factor B1 Human X-ray 4Z9G - 3.2 A Inactive 17 63 - - - - T4-Lysozyme - CP 376,395
small-molecule Antagonist urocortin 2, corticotrophin-releasing hormone, urocortin 1 peptide No No Dore AS, Bortolato A, Hollenstein K, Cheng RKY, Read RJ, Marshall FH 10.2174/1874467210666170110114727 2016-06-29 Yes
AA2AR A2A Adenosine A Human X-ray 5IU7 5IU7_refined 1.9 A Inactive 1 72 - - - - BRIL - 2-(Furan-2-yl)-5-N-[2-(4-phenylpiperidin-1-yl)ethyl]-1H-[1,2,4]triazolo[1,5-a][1,3,5]triazin-8-ium-5,7-diamine
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 5IUA 5IUA_refined 2.2 A Inactive 1 72 - - - - BRIL - 2-(Furan-2-yl)-5-N-[3-(4-phenylpiperazin-1-yl)propyl]-1H-[1,2,4]triazolo[1,5-a][1,3,5]triazin-8-ium-5,7-diamine
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
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, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ 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
AA2AR A2A Adenosine A Human X-ray 5G53 5G53_refined 3.4 A Active 100 68 Gs αs Engineered G protein 50 - - NECA
small-molecule Agonist adenosine small-molecule No No Carpenter B, Nehme R, Warne T, Leslie AG, Tate CG 10.1038/NATURE18966 2016-08-03 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
ADRB2 β2 Adrenoceptors A Human X-ray 5D6L 5D6L_refined 3.2 A Inactive 0 68 - - - - T4-Lysozyme - Carazolol
small-molecule Inverse agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ 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
EDNRB ETB Endothelin A Human X-ray 5GLI 5GLI_refined 2.5 A Inactive 4 71 - - - - T4-Lysozyme - Apo (no ligand)
none Apo (no ligand) endothelin-1, endothelin-2, endothelin-3 peptide No No - 10.1038/nature19319 2016-09-07 Yes
AA2AR A2A Adenosine A Human X-ray 5K2A 5K2A_refined 2.5 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
AA2AR A2A Adenosine A Human X-ray 5K2B 5K2B_refined 2.5 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
CCR2 CCR2 Chemokine A Human X-ray 5T1A 5T1A_refined 2.8 A Inactive 16 76 - - - - T4-Lysozyme - CCR2-RA-[R]
BMS-681
small-molecule
small-molecule		 Allosteric antagonist
Antagonist		 CCL2, CCL8, CCL11, CCL13, CCL24, CCL7, CCL26, CCL16 peptide No No Zheng Y, Qin L, Zacarias NV, de Vries H, Han GW, Gustavsson M, Dabros M, Zhao C, Cherney RJ, Carter P, Stamos D, Abagyan R, Cherezov V, Stevens RC, IJzerman AP, Heitman LH, Tebben A, Kufareva I, Handel TM 10.1038/NATURE20605 2016-12-14 Yes
5HT2B 5-HT2B 5-Hydroxytryptamine A Human X-ray 5TVN 5TVN_refined 2.9 A Intermediate 44 61 - - - - BRIL - Lysergide
small-molecule Agonist 5-hydroxytryptamine small-molecule No No Wacker D, Wang S, McCorvy JD, Betz RM, Venkatakrishnan AJ, Levit A, Lansu K, Schools ZL, Che T, Nichols DE, Shoichet BK, Dror RO, Roth BL 10.1016/J.CELL.2016.12.033 2017-02-01 Yes
AGTR2 AT2 Angiotensin A Human X-ray 5UNH 5UNH_refined 2.9 B Active 99 75 - - - - BRIL - compound 2 [PMID: 28379944]
small-molecule Antagonist angiotensin-(1-7), angiotensin II, angiotensin III peptide No No Zhang H, Han GW, Batyuk A, Ishchenko A, White KL, Patel N, Sadybekov A, Zamlynny B, Rudd MT, Hollenstein K, Tolstikova A, White TA, Hunter MS, Weierstall U, Liu W, Babaoglu K, Moore EL, Katz RD, Shipman JM, Garcia-Calvo M, Sharma S, Sheth P, Soisson SM, Stevens RC, Katritch V, Cherezov V 10.1038/NATURE22035 2017-04-05 Yes
PAR2 PAR2 Proteinase-activated A Human X-ray 5NDZ 5NDZ_refined 3.6 A Intermediate 44 74 - - - - BRIL - AZ3451
small-molecule Allosteric antagonist - - No Yes 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
PAR2 PAR2 Proteinase-activated A Human X-ray 5NJ6 5NJ6_refined 4.0 A Intermediate 44 74 - - - - BRIL Fab3949 - - - - - 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
CALCR CT Calcitonin B1 Human Cryo-EM 5UZ7 - 4.1 R Active 100 56 Gs αs - 47 - - calcitonin (salmon synthetic)
small-molecule Agonist β-CGRP, α-CGRP, calcitonin, calcitonin (salmon), amylin, adrenomedullin, adrenomedullin 2/intermedin peptide No No Liang YL, Khoshouei M, Radjainia M, Zhang Y, Glukhova A, Tarrasch J, Thal DM, Furness SGB, Christopoulos G, Coudrat T, Danev R, Baumeister W, Miller LJ, Christopoulos A, Kobilka BK, Wootten D, Skiniotis G, Sexton PM 10.1038/NATURE22327 2017-05-03 Yes
AA2AR A2A Adenosine A Human X-ray 5UVI 5UVI_refined 3.2 A Inactive 1 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
SMO SMO Frizzled F Human X-ray 5V56 5V56_refined 2.9 B Inactive 1 61 - - - - 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 - - 2017-05-24 Yes
SMO SMO Frizzled F Human X-ray 5V57 5V57_refined 3.0 A Inactive 1 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
G1SGD4 GLP-1 Glucagon B1 Rabbit Cryo-EM 5VAI - 4.1 R Active 100 84 Gs αs - 59 - - CHEMBL410972
protein Agonist - - No No Zhang Y, Sun B, Feng D, Hu H, Chu M, Qu Q, Tarrasch JT, Li S, Sun Kobilka T, Kobilka BK, Skiniotis G 10.1038/NATURE22394 2017-05-24 Yes
GLR glucagon Glucagon B1 Human X-ray 5XEZ 5XEZ_refined 3.0 B Inactive 0 82 - - - - 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
AA2AR A2A Adenosine A Human X-ray 5JTB 5JTB_refined 2.8 A Inactive 1 72 - - - - BRIL - ZM-241385
small-molecule Antagonist adenosine small-molecule No No Melnikov I, Polovinkin V, Kovalev K, Gushchin I, Shevtsov M, Shevchenko V, Mishin A, Alekseev A, Rodriguez-Valera F, Borshchevskiy V, Cherezov V, Leonard GA, Gordeliy V, Popov A 10.1126/SCIADV.1602952 2017-05-31 Yes
APJ apelin Apelin A Human X-ray 5VBL - 2.6 B Inactive 4 79 - - - - Rubredoxin - AMG3054
peptide Agonist apelin-13, apelin-17, apelin-36, Elabela/Toddler-21, [Pyr1]apelin-13, Elabela/Toddler-11, apelin receptor early endogenous ligand, Elabela/Toddler-32 peptide No No Ma Y, Yue Y, Ma Y, Zhang Q, Zhou Q, Song Y, Shen Y, Li X, Ma X, Li C, Hanson MA, Han GW, Sickmier EA, Swaminath G, Zhao S, Stevens RC, Hu LA, Zhong W, Zhang M, Xu F 10.1016/J.STR.2017.04.008 2017-05-31 Yes
AA2AR A2A Adenosine A Human X-ray 5MZP 5MZP_refined 2.1 A Inactive 1 71 - - - - BRIL - caffeine
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
5HT2B 5-HT2B 5-Hydroxytryptamine A Human X-ray 5TUD 5TUD_refined 3.0 D Active 87 58 - - - - BRIL Antibody ergotamine
small-molecule Agonist 5-hydroxytryptamine small-molecule No No Ishchenko A, Wacker D, Kapoor M, Zhang A, Han GW, Basu S, Patel N, Messerschmidt M, Weierstall U, Liu W, Katritch V, Roth BL, Stevens RC, Cherezov V 10.1073/PNAS.1700891114 2017-07-26 Yes
Q08BG4 LPA6 Lysophospholipid (LPA) A Zebrafish X-ray 5XSZ 5XSZ_refined 3.2 A Active 65 78 - - - - T4-Lysozyme - Apo (no ligand)
none Apo (no ligand) - - No No Taniguchi R, Inoue A, Sayama M, Uwamizu A, Yamashita K, Hirata K, Yoshida M, Tanaka Y, Kato HE, Nakada-Nakura Y, Otani Y, Nishizawa T, Doi T, Ohwada T, Ishitani R, Aoki J, Nureki O 10.1038/NATURE23448 2017-08-16 Yes
AA2AR A2A Adenosine A Human X-ray 5NLX - 2.1 A Inactive 1 73 - - - - 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
AA2AR A2A Adenosine A Human X-ray 5NM2 5NM2_refined 2.0 A Inactive 1 72 - - - - BRIL - ZM-241385
small-molecule Antagonist adenosine small-molecule No Yes 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
DRD4 D4 Dopamine A Human X-ray 5WIU - 2.0 A Inactive 1 64 - - - - 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
DRD4 D4 Dopamine A Human X-ray 5WIV - 2.1 A Inactive 1 65 - - - - BRIL - [3H]NEMONAPRIDE
small-molecule Antagonist dopamine small-molecule No Yes 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
OX2R OX2 Orexin A Human X-ray 5WQC 5WQC_refined 2.0 A Inactive 1 68 - - - - 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 2017-11-29 Yes
CXCR4 CXCR4 Chemokine A Human X-ray 3OE9 3OE9_refined 3.1 A Inactive 4 74 - - - - T4-Lysozyme - isothiourea-1t
small-molecule Antagonist CXCL12γ, CXCL12ε, CXCL12, CXCL12δ, CXCL12β, CXCL12φ, CXCL12α peptide No No - 10.1126/SCIENCE.1194396 2010-10-27 Yes
S1PR1 S1P1 Lysophospholipid (S1P) A Human X-ray 3V2W 3V2W_refined 3.4 A Inactive 1 68 - - - - T4-Lysozyme - W146
small-molecule Antagonist sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate small-molecule No No Hanson MA, Roth CB, Jo E, Griffith MT, Scott FL, Reinhart G, Desale H, Clemons B, Cahalan SM, Schuerer SC, Sanna MG, Han GW, Kuhn P, Rosen H, Stevens RC 10.1126/SCIENCE.1215904 2012-02-15 Yes
NTR1 NTS1 Neurotensin A Rat X-ray 3ZEV 3ZEV_refined 3.0 A Inactive 3 72 - - - - - - neurotensin
peptide Agonist neuromedin N, neurotensin 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
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 5A8E 5A8E_refined 2.4 A Inactive 0 59 - - - - - - 7-methylcyanopindolol
small-molecule Inverse agonist - - No Yes Sato T, Baker J, Warne T, Brown GA, Leslie AG, Congreve M, Tate CG 10.1124/MOL.115.101030 2015-09-30 Yes
AA2AR A2A Adenosine A Human X-ray 5IUB 5IUB_refined 2.1 A Inactive 1 71 - - - - BRIL - CHEMBL184061
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
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
OPSD Rhodopsin Opsins A Bovine X-ray 5WKT 5WKT_refined 3.2 A Active 100 94 Gi/o αt1 Only H5 3 - - B-Octylglucoside
small-molecule unknown - - No No Broecker J, Morizumi T, Ou WL, Klingel V, Kuo A, Kissick DJ, Ishchenko A, Lee MY, Xu S, Makarov O, Cherezov V, Ogata CM, Ernst OP 10.1038/NPROT.2017.135 2017-12-13 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 6FK6 6FK6_refined 2.4 A Active 98 94 - - - - - - COMPOUND SUMMARY
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
AGTR2 AT2 Angiotensin A Human X-ray 5XJM 5XJM_refined 3.2 A Active 100 78 - - - - BRIL Fab CHEMBL404594
protein Agonist angiotensin-(1-7), angiotensin II, angiotensin III peptide No No Asada H, Horita S, Hirata K, Shiroishi M, Shiimura Y, Iwanari H, Hamakubo T, Shimamura T, Nomura N, Kusano-Arai O, Uemura T, Suno C, Kobayashi T, Iwata S 10.1038/S41594-018-0079-8 2018-07-11 Yes
CCR5 CCR5 Chemokine A Human Cryo-EM 6MET 6MET_refined 4.5 B Inactive 16 89 - - - - - T-cell surface glycoprotein CD4 Envelope glycoprotein gp160
protein Antagonist CCL2, CCL8, CCL11, CCL13, CCL14, CCL7, CCL5, CCL4, CCL16, CCL3 peptide No No - - 2018-12-12 Yes
DRD3 D3 Dopamine A Human X-ray 3PBL 3PBL_refined 2.9 A Inactive 1 68 - - - - T4-Lysozyme - eticlopride
small-molecule Antagonist dopamine small-molecule No No - 10.1126/SCIENCE.1197410 2010-11-03 Yes
OPRK κ Opioid A Human X-ray 4DJH 4DJH_refined 2.9 A Inactive 4 76 - - - - T4-Lysozyme - JDTic
small-molecule Antagonist dynorphin A-(1-8), β-neoendorphin, big dynorphin, [Met]enkephalin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin B, α-neoendorphin peptide No No Wu H, Wacker D, Mileni M, Katritch V, Han GW, Vardy E, Liu W, Thompson AA, Huang XP, Carroll FI, Mascarella SW, Westkaemper RB, Mosier PD, Roth BL, Cherezov V, Stevens RC 10.1038/NATURE10939 2012-03-21 Yes
P2Y12 P2Y12 P2Y A Human X-ray 4PXZ 4PXZ_refined 2.5 A Intermediate 44 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
OPRX NOP Opioid A Human X-ray 5DHG 5DHG_refined 3.0 A Inactive 4 76 - - - - BRIL - CHEMBL1783826
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 5K2D 5K2D_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
FFAR1 FFA1 Free fatty acid A Human X-ray 5TZR 5TZR_refined 2.2 A Intermediate 44 91 - - - - T4-Lysozyme - MK-8666
small-molecule Allosteric agonist oleic acid, docosahexaenoic acid, α-linolenic acid, myristic 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
OX2R OX2 Orexin A Human X-ray 5WS3 5WS3_refined 2.3 A Inactive 1 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 6FKA 6FKA_refined 2.7 A Active 98 94 - - - - - - (2~{S})-2-(3,4-dichlorophenyl)-3-methyl-1-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-yl-butan-1-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
5HT2B 5-HT2B 5-Hydroxytryptamine A Human X-ray 6DS0 6DS0_refined 3.2 A Intermediate 44 59 - - - - BRIL - LY266097
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
ACM3 M3 Acetylcholine (muscarinic) A Rat X-ray 5ZHP 5ZHP_refined 3.1 B Inactive 2 47 - - - - T4-Lysozyme - (1R,2R,4S,5S,7s)-7-({[4-fluoro-2-(thiophen-2-yl)phenyl]carbamoyl}oxy)-9,9-dimethyl-3-oxa-9-azatricyclo[3.3.1.0~2,4~]nonan-9-ium
small-molecule Antagonist acetylcholine small-molecule No No - 10.1073/PNAS.1813988115 2018-11-28 Yes
MTR1B MT2 Melatonin A Human X-ray 6ME8 6ME8_refined 3.1 B Inactive 1 78 - - - - Rubredoxin - CHEMBL15060
small-molecule Agonist melatonin small-molecule No No - - 2019-04-24 Yes
GLP1R GLP-1 Glucagon B1 Human X-ray 6KK7 6KK7_refined 3.1 B Inactive 0 56 - - - - T4-Lysozyme - PF-06372222
small-molecule NAM glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide peptide No No - - 2019-11-13 Yes
OX1R OX1 Orexin A Human X-ray 6TOT 6TOT_refined 2.2 B Inactive 1 71 - - - - - - lemborexant
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 2020-01-15 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, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ 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
AA2AR A2A Adenosine A Human X-ray 6ZDV 6ZDV_refined 2.1 A Inactive 1 72 - - - - BRIL - 2-Methyl-3-(4-methylthiazol-2-yl)-4-oxo-6-propyl-4H-chromen-7-yl acetate
small-molecule Antagonist adenosine small-molecule No Yes Jespers W, Verdon G, Azuaje J, Majellaro M, Keranen H, Garcia-Mera X, Congreve M, Deflorian F, de Graaf C, Zhukov A, Dore AS, Mason JS, Aqvist J, Cooke RM, Sotelo E, Gutierrez-de-Teran H 10.1002/ANIE.202003788 2020-09-16 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 7JVP - 2.9 R Active 100 63 Gs αs - 60 - Nanobody-35 39YLC3L0ZU
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, 5-hydroxytryptamine, dopamine small-molecule No No - - 2021-02-24 Yes
V2R V2 Vasopressin and oxytocin A Human Cryo-EM 7KH0 - 2.8 R Active 100 74 Gs αs - 58 - scFv16
Nanobody-35		 vasopressin
peptide Agonist oxytocin, vasopressin peptide No No Wang L, Xu J, Cao S, Sun D, Liu H, Lu Q, Liu Z, Du Y, Zhang C 10.1038/S41422-021-00483-Z 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 CCL2, CCL8, CCL11, CCL13, CCL14, CCL7, CCL5, CCL4, CCL16, CCL3 peptide No No - - 2021-07-14 Yes
GHSR ghrelin Ghrelin A Human Cryo-EM 7F9Z 7F9Z_refined 3.2 R Active 100 77 Gq/11 αq Engineered G alpha 59 - Nanobody-35
scFv16		 GHRP-6
peptide Agonist [des-Gln14]ghrelin, ghrelin peptide No No - - 2021-08-18 Yes
ACM1 M1 Acetylcholine (muscarinic) A Human X-ray 6ZFZ 6ZFZ_refined 2.2 A Inactive 2 62 - - - - T4-Lysozyme - CHEMBL3354065
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
CNR1 CB1 Cannabinoid A Human X-ray 7V3Z 7V3Z_refined 3.3 A Active 91 60 - - - - Flavodoxin - CP55940
small-molecule Agonist 2-arachidonoylglycerol, anandamide small-molecule No No Wang X, Liu D, Shen L, Li F, Li Y, Yang L, Xu T, Tao H, Yao D, Wu L, Hirata K, Bohn LM, Makriyannis A, Liu X, Hua T, Liu ZJ, Wang J 10.1021/JACS.1C06847 2021-11-24 Yes
NK1R NK1 Tachykinin A Human Cryo-EM 7P02 - 2.9 R Active 100 71 Gs αs Gs-Gi1 chimera 57 - scFv16 substance P
peptide Agonist neurokinin B, neuropeptide-γ, hemokinin 1, substance P, neurokinin A, neuropeptide K peptide No No Thom C, Ehrenmann J, Vacca S, Waltenspuhl Y, Schoppe J, Medalia O, Pluckthun A 10.1126/SCIADV.ABK2872 2021-12-15 Yes
S1PR1 S1P1 Lysophospholipid (S1P) A Human Cryo-EM 7EVY - 3.0 D Active 100 71 Gi/o αi1 - 64 - scFv16 siponimod
small-molecule Agonist sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate 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
AA2AR A2A Adenosine A Human X-ray 7PX4 7PX4_refined 2.3 A Inactive 1 72 - - - - BRIL - Preladenant conjugate PSB-2113
small-molecule Antagonist adenosine small-molecule No No Claff T, Klapschinski TA, Tiruttani Subhramanyam UK, Vaassen VJ, Schlegel JG, Vielmuth C, Voss JH, Labahn J, Muller CE 10.1002/ANIE.202115545 2022-03-02 Yes
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 7VBI - 3.0 R Active 100 83 Gs αs Mini-Gs 58 - - tirzepatide
peptide Agonist glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide 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 7S0F - 3.0 R Active 100 56 Gi/o αi1 - 63 - - 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 7F1Z - 3.5 F Active 100 62 Gs αs - 60 - - dopamine
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, 5-hydroxytryptamine, dopamine 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
5HT2A 5-HT2A 5-Hydroxytryptamine A Human Cryo-EM 7RAN - 3.5 A Active 100 57 Gq/11 αq Gi2-mini-Gq chimera 60 - scFv16 3-[(3R)-3-methyl-1,2,3,6-tetrahydropyridin-1-ium-5-yl]-1H-pyrrolo[2,3-b]pyridine
small-molecule Agonist 5-hydroxytryptamine, tryptamine small-molecule No No Kaplan AL, Confair DN, Kim K, Barros-Alvarez X, Rodriguiz RM, Yang Y, Kweon OS, Che T, McCorvy JD, Kamber DN, Phelan JP, Martins LC, Pogorelov VM, DiBerto JF, Slocum ST, Huang XP, Kumar JM, Robertson MJ, Panova O, Seven AB, Wetsel AQ, Wetsel WC, Irwin JJ, Skiniotis G, Shoichet BK, Roth BL, Ellman JA 10.1038/S41586-022-05258-Z 2022-07-06 Yes
CX3C1 CX3CR1 Chemokine A Human Cryo-EM 7XBX - 3.4 R Active 16 81 Gi/o αi1 - 61 - - CX3CL1
peptide Agonist CX3CL1 peptide No No - - 2022-07-13 Yes
S1PR1 S1P1 Lysophospholipid (S1P) A Human Cryo-EM 7VIE 7VIE_refined 2.9 F Active 100 73 Gi/o αi1 - 64 - scFv16 sphingosine 1-phosphate
small-molecule Agonist sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate 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
T2R46 TAS2R46 Taste 2 T Human Cryo-EM 7XP6 - 3.0 R Active - 92 Gi/o αgust - 63 - Nanobody-35 strychnine
small-molecule Agonist - - 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
OPRM μ Opioid A Human Cryo-EM 8EF5 - 3.3 R Active 100 72 Gi/o αi1 - 64 - scFv16 fentanyl
small-molecule Agonist dynorphin A-(1-8), [Met]enkephalin, endomorphin-1, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin B, endomorphin-2 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
OPSD Rhodopsin Opsins A Bovine X-ray 7ZBC - 1.8 A Inactive 22 87 - - - - - - Retinal (11-cis)
small-molecule Inverse 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
AA2AR A2A Adenosine A Human X-ray 8GNG 8GNG_refined 3.2 X Inactive 1 69 - - - - - Antibody fab fragment light chain
Antibody fab fragment heavy chain		 istradefylline
small-molecule Antagonist adenosine small-molecule No No - - 2023-03-22 Yes
FFAR4 FFA4 Free fatty acid A Human Cryo-EM 8ID9 8ID9_refined 3.0 R Active 100 78 Gi/o αi1 - 56 - scFv16 EPA
small-molecule Agonist linoleic acid, oleic acid, α-linolenic acid, myristic acid small-molecule No No - 10.1126/SCIENCE.ADD6220 2023-03-15 Yes
CNR2 CB2 Cannabinoid A Human Cryo-EM 8GUS - 3.0 R Active 100 81 Gi/o αi1 - 62 - scFv16 CHEMBL2179724
small-molecule Agonist 2-arachidonoylglycerol, anandamide 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
SSR2 SST2 Somatostatin A Human Cryo-EM 7YAC 7YAC_refined 3.2 E Active 100 76 Gi/o αi1 - 64 - scFv16 Paltusotine
small-molecule Agonist SRIF-14, CST-17, cortistatin-14, SRIF-28 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
AGRE5 ADGRE5 ADGRE B2 Human Cryo-EM 7YDJ - 3.0 R Active - 33 G12/13 α12 Mini-G12 55 - scFv16 Apo (no ligand)
none Apo (no ligand) - - No No - - 2023-07-12 Yes
CALCR CT Calcitonin B1 Human Cryo-EM 8F0J - 2.0 R Active 100 78 Gs αs - 58 - Nanobody-35 Pramlintide analogue San45
peptide Agonist β-CGRP, α-CGRP, calcitonin, calcitonin (salmon), amylin, adrenomedullin, adrenomedullin 2/intermedin peptide No No Cao J, Belousoff MJ, Gerrard E, Danev R, Fletcher MM, Dal Maso E, Schreuder H, Lorenz K, Evers A, Tiwari G, Besenius M, Li Z, Johnson RM, Wootten D, Sexton PM 10.1038/S41589-023-01393-4 2023-08-02 Yes
GRM2 mGlu2 Metabotropic glutamate C Human Cryo-EM 8JD3 - 3.3 2 Active - 89 Gi/o αi1 - 62 - - L-glutamic acid
JNJ-40411813
small-molecule
small-molecule		 Agonist
PAM		 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
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 2Y00 2Y00_refined 2.5 B Inactive 0 62 - - - - - - Dobutamine
small-molecule Agonist (partial) - - No No - 10.1038/NATURE09746 2011-01-12 Yes
ACM3 M3 Acetylcholine (muscarinic) A Rat X-ray 4DAJ - 3.4 A Inactive 2 46 - - - - T4-Lysozyme - tiotropium
small-molecule Antagonist acetylcholine small-molecule No No Kruse AC, Hu J, Pan AC, Arlow DH, Rosenbaum DM, Rosemond E, Green HF, Liu T, Chae PS, Dror RO, Shaw DE, Weis WI, Wess J, Kobilka BK 10.1038/NATURE10867 2012-02-22 Yes
CXCR4 CXCR4 Chemokine A Human X-ray 4RWS 4RWS_refined 3.1 A Inactive 4 78 - - - - T4-Lysozyme - vMIP-II
peptide Antagonist CXCL12γ, CXCL12ε, CXCL12, CXCL12δ, CXCL12β, CXCL12φ, 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
AGTR2 AT2 Angiotensin A Human X-ray 5UNF 5UNF_refined 2.8 A Active 99 79 - - - - BRIL - compound 1 [PMID: 28379944]
small-molecule Antagonist angiotensin-(1-7), angiotensin II, angiotensin III peptide No No Zhang H, Han GW, Batyuk A, Ishchenko A, White KL, Patel N, Sadybekov A, Zamlynny B, Rudd MT, Hollenstein K, Tolstikova A, White TA, Hunter MS, Weierstall U, Liu W, Babaoglu K, Moore EL, Katz RD, Shipman JM, Garcia-Calvo M, Sharma S, Sheth P, Soisson SM, Stevens RC, Katritch V, Cherezov V 10.1038/NATURE22035 2017-04-05 Yes
AA2AR A2A Adenosine A Human X-ray 5VRA 5VRA_refined 2.4 A Inactive 1 72 - - - - BRIL - ZM-241385
small-molecule Antagonist adenosine small-molecule No Yes - - 2017-12-13 Yes
NPY1R Y1 Neuropeptide Y A Human X-ray 5ZBQ 5ZBQ_refined 2.7 A Inactive 1 80 - - - - T4-Lysozyme - CHEMBL3747822
small-molecule Antagonist pancreatic polypeptide, neuropeptide Y, peptide YY peptide No No Yang Z, Han S, Keller M, Kaiser A, Bender BJ, Bosse M, Burkert K, Kogler LM, Wifling D, Bernhardt G, Plank N, Littmann T, Schmidt P, Yi C, Li B, Ye S, Zhang R, Xu B, Larhammar D, Stevens RC, Huster D, Meiler J, Zhao Q, Beck-Sickinger AG, Buschauer A, Wu B 10.1038/S41586-018-0046-X 2018-04-25 Yes
ACM2 M2 Acetylcholine (muscarinic) A Human X-ray 5YC8 5YC8_refined 2.5 A Inactive 2 60 - - - - BRIL - N-methyl scopolamine
small-molecule Antagonist acetylcholine small-molecule No No Suno R, Lee S, Maeda S, Yasuda S, Yamashita K, Hirata K, Horita S, Tawaramoto MS, Tsujimoto H, Murata T, Kinoshita M, Yamamoto M, Kobilka BK, Vaidehi N, Iwata S, Kobayashi T 10.1038/S41589-018-0152-Y 2018-11-21 Yes
GRM5 mGlu5 Metabotropic glutamate C Human Cryo-EM 6N52 6N52_refined 4.0 A Inactive - 64 - - - - - Nanobody-43 - - - L-glutamic acid small-molecule No No - - 2019-01-23 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
OPRD δ Opioid A Human X-ray 6PT2 6PT2_refined 2.8 A Active 65 78 - - - - BRIL - KGCHM07
peptide Agonist dynorphin A-(1-8), [Met]enkephalin, endomorphin-1, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin B, α-neoendorphin peptide No No - - 2019-12-11 Yes
GPR52 GPR52 A orphans A Human Cryo-EM 6LI3 - 3.3 R Active 100 79 Gs αs Mini-Gs 61 - Nanobody-35 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
GABR2 GABAB2 GABAB C Human Cryo-EM 6UO9 - 4.8 B Intermediate - 73 - - - - - - CHEMBL112710
small-molecule Agonist - - No No - - 2020-06-10 Yes
FZD5 FZD5 Frizzled F Human Cryo-EM 6WW2 6WW2_refined 3.7 R Inactive 22 55 - - - - BRIL anti-BRIL Fab heavy chain
anti-BRIL Fab light chain
anti-Fab Nanobody		 Apo (no ligand)
none Apo (no ligand) - - No No Tsutsumi N, Mukherjee S, Waghray D, Janda CY, Jude KM, Miao Y, Burg JS, Aduri NG, Kossiakoff AA, Gati C, Garcia KC 10.7554/ELIFE.58464 2020-08-19 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
NTR1 NTS1 Neurotensin A Rat X-ray 6Z4V - 2.6 A Intermediate 15 79 - - - - DARPin D12 - JMV431
peptide 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
PE2R2 EP2 Prostanoid A Human Cryo-EM 7CX2 - 2.8 R Active 100 74 Gs αs - 58 - Nanobody-35 PGE2
small-molecule Agonist PGE2, PGF2α, thromboxane A2, PGI2, PGE1, PGD2 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 7M3E 7M3E_refined 3.2 B Inactive - 75 - - - - - - Calcium
NPS 2143
L-tryptophan
small-molecule
small-molecule
small-molecule		 Agonist
NAM
PAM		 spermine, L-tryptophan, Ca2+, Mg2+ small-molecule No No - 10.1038/S41586-021-03691-0 2021-06-30 Yes
AA2AR A2A Adenosine A Human MicroED 7RM5 7RM5_refined 2.8 A Inactive 1 72 - - - - BRIL - ZM-241385
small-molecule Antagonist adenosine small-molecule No Yes Martynowycz MW, Shiriaeva A, Ge X, Hattne J, Nannenga BL, Cherezov V, Gonen T 10.1073/PNAS.2106041118 2021-09-08 Yes
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 7RTB 7RTB_refined 2.1 R Active 100 83 Gs αs - 60 - Nanobody-35 Peptide-19
peptide Agonist glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide peptide No No Johnson RM, Zhang X, Piper SJ, Nettleton TJ, Vandekolk TH, Langmead CJ, Danev R, Sexton PM, Wootten D 10.1016/J.BBRC.2021.09.016 2021-10-06 Yes
5HT2A 5-HT2A 5-Hydroxytryptamine A Human X-ray 7VOE 7VOE_refined 2.9 A Inactive 1 58 - - - - BRIL - aripiprazole
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
LPAR1 LPA1 Lysophospholipid (LPA) A Human Cryo-EM 7TD0 - 2.8 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
FPR1 FPR1 Formylpeptide A Human Cryo-EM 7WVU 7WVU_refined 3.3 R Active 100 85 Gi/o αi1 - 62 - - FME-LEU-PHE
peptide Agonist cathepsin G, spinorphin, annexin I, fMet-Leu-Phe 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
AGRF1 ADGRF1 ADGRF B2 Human Cryo-EM 7WU5 - 3.0 R Active - 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
ADRB3 β3 Adrenoceptors A Dog Cryo-EM 7XJI - 3.9 R Active 100 68 Gs αs - 59 - Nanobody-35 3-[3-[2-[[(2~{S})-2-(3-chlorophenyl)-2-oxidanyl-ethyl]amino]ethylamino]phenyl]benzoic acid
small-molecule Agonist - - No No Nureki I, Kobayashi K, Tanaka T, Demura K, Inoue A, Shihoya W, Nureki O 10.1016/J.BBRC.2022.04.065 2022-05-04 Yes
SSR2 SST2 Somatostatin A Human Cryo-EM 7UL5 7UL5_refined 3.1 A Inactive 4 77 - - - - - Nanobody-6 Apo (no ligand)
none Apo (no ligand) SRIF-14, CST-17, cortistatin-14, SRIF-28 peptide 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
5HT5A 5-HT5A 5-Hydroxytryptamine A Human Cryo-EM 7UM7 7UM7_refined 2.8 A Active 100 72 Gi/o αo Mini-Go 60 - scFv16 methylergonovine
small-molecule Agonist 5-hydroxytryptamine small-molecule No No Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL 10.1038/S41594-022-00796-6 2022-07-20 Yes
ACKR3 ACKR3 Chemokine A Human Cryo-EM 7SK4 7SK4_refined 3.3 A Active 95 84 - - - - - CID25 Fab light chain
CID25 Fab heavy chain
CID24 Fab light chain
CID24 Fab heavy chain		 Stromal cell-derived factor 1
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
OPRM μ Opioid A Human Cryo-EM 8EFQ - 3.3 R Active 100 71 Gi/o αi1 - 61 - - DAMGO
peptide Agonist dynorphin A-(1-8), [Met]enkephalin, endomorphin-1, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin B, endomorphin-2 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
5HT6R 5-HT6 5-Hydroxytryptamine A Human Cryo-EM 7YS6 7YS6_refined 3.0 A Active 100 61 Gs αs - 59 - scFv16 5-hydroxytryptamine
small-molecule Agonist 5-hydroxytryptamine small-molecule No No - - 2023-03-29 Yes
ACTHR MC2 Melanocortin A Human Cryo-EM 8GY7 - 3.3 R Active 100 92 Gs αs - 59 BRIL - ACTH
peptide Agonist ACTH peptide No No - 10.1038/S41422-022-00751-6 2023-01-11 Yes
TAAR9 TAAR9 A orphans A Mouse Cryo-EM 8IW4 - 3.5 R Active 100 85 Gs αs - 45 - scFv16 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
OPRK κ Opioid A Human Cryo-EM 7Y1F 7Y1F_refined 3.3 R Active 100 75 Gi/o αi1 - 61 - scFv16 dynorphin A-(1-8)
peptide Agonist dynorphin A-(1-8), β-neoendorphin, big dynorphin, [Met]enkephalin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin B, α-neoendorphin peptide No No Chen Y, Chen B, Wu T, Zhou F, Xu F 10.1093/PROCEL/PWAC033 2023-05-24 Yes
PTH1R PTH1 Parathyroid hormone B1 Human Cryo-EM 8FLU - 2.8 R Active 100 61 Gs αs - 58 - Nanobody-35 PTH
peptide Agonist PTH, PTHrP-(1-36), TIP39, PTHrP 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
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 8JCY - 2.9 2 Inactive - 87 - - - - - - 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
AA2AR A2A Adenosine A Human X-ray 3QAK 3QAK_refined 2.7 A Active 65 69 - - - - T4-Lysozyme - UK-432,097
small-molecule Agonist adenosine small-molecule No No - 10.1126/SCIENCE.1202793 2011-03-09 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 4LDO 4LDO_refined 3.2 A Active 99 69 - - - - T4-Lysozyme Nanobody (-)-adrenaline
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ 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
OX2R OX2 Orexin A Human X-ray 4S0V 4S0V_refined 2.5 A Inactive 1 64 - - - - Glycogen synthase - suvorexant
small-molecule Antagonist orexin-B, orexin-A peptide No No Yin J, Mobarec JC, Kolb P, Rosenbaum DM 10.1038/NATURE14035 2015-01-14 Yes
ACM4 M4 Acetylcholine (muscarinic) A Human X-ray 5DSG 5DSG_refined 2.6 B Inactive 2 60 - - - - T4-Lysozyme - tiotropium
small-molecule Antagonist acetylcholine small-molecule No No Thal DM, Sun B, Feng D, Nawaratne V, Leach K, Felder CC, Bures MG, Evans DA, Weis WI, Bachhawat P, Kobilka TS, Sexton PM, Kobilka BK, Christopoulos A 10.1038/NATURE17188 2016-03-16 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 5TE3 5TE3_refined 2.7 A Active 98 94 - - - - - - B-Octylglucoside
small-molecule unknown - - 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
AA1R A1 Adenosine A Human X-ray 5N2S 5N2S_refined 3.3 A Inactive 1 86 - - - - BRIL - PSB36
small-molecule Agonist adenosine small-molecule No No 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
AA2AR A2A Adenosine A Human X-ray 5OLO 5OLO_refined 3.1 A Inactive 1 72 - - - - BRIL - tozadenant
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
OPRM μ Opioid A Mouse Cryo-EM 6DDE - 3.5 R Active 100 71 Gi/o αi1 - 61 - Antibody DAMGO
peptide Agonist - - No No Koehl A, Hu H, Maeda S, Zhang Y, Qu Q, Paggi JM, Latorraca NR, Hilger D, Dawson R, Matile H, Schertler GFX, Granier S, Weis WI, Dror RO, Manglik A, Skiniotis G, Kobilka BK 10.1038/S41586-018-0219-7 2018-06-13 Yes
NK1R NK1 Tachykinin A Human X-ray 6HLO 6HLO_refined 2.4 A Inactive 1 70 - - - - GlgA glycogen synthase - aprepitant
small-molecule Antagonist neurokinin B, neuropeptide-γ, hemokinin 1, substance P, neurokinin A, neuropeptide K peptide No No - - 2019-01-16 Yes
B1B1U5 Rhodopsin Opsins A Hasarius adansoni X-ray 6I9K - 2.2 A Inactive 17 83 - - - - - - Retinal (11-cis)
small-molecule Inverse agonist - - No No - 10.1073/PNAS.1902192116 2019-07-03 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 6PS1 6PS1_refined 3.2 A Inactive 0 68 - - - - T4-Lysozyme - timolol
small-molecule Antagonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ small-molecule No No - - 2019-11-13 Yes
OX2R OX2 Orexin A Human X-ray 6TPG 6TPG_refined 2.7 A Inactive 1 69 - - - - GlgA glycogen synthase - EMPA
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
GPR52 GPR52 A orphans A Human X-ray 6LI0 6LI0_refined 2.2 A Intermediate 40 81 - - - - Flavodoxin - derivative 17 [Nakahata et al., 2018]
small-molecule Agonist - - 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
CALRL calcitonin-like Calcitonin B1 Human Cryo-EM 6UVA - 2.3 R Active 100 75 Gs αs - 48 - Nanobody-35
RAMP3		 adrenomedullin 2/intermedin
peptide Agonist - - No No Liang YL, Belousoff MJ, Fletcher MM, Zhang X, Khoshouei M, Deganutti G, Koole C, Furness SGB, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Danev R, Wootten D, Sexton PM 10.1021/ACSPTSCI.9B00080 2020-04-01 Yes
5HT2A 5-HT2A 5-Hydroxytryptamine A Human X-ray 6WGT 6WGT_refined 3.4 B Inactive 1 59 - - - - BRIL - Lysergide
small-molecule Agonist 5-hydroxytryptamine, tryptamine small-molecule No No Kim K, Che T, Panova O, DiBerto JF, Lyu J, Krumm BE, Wacker D, Robertson MJ, Seven AB, Nichols DE, Shoichet BK, Skiniotis G, Roth BL 10.1016/J.CELL.2020.08.024 2020-09-23 Yes
AA2AR A2A Adenosine A Human X-ray 6LPL 6LPL_refined 2.0 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
NTR1 NTS1 Neurotensin A Rat X-ray 6Z8N 6Z8N_refined 2.8 A Intermediate 15 80 - - - - DARPin D12 - (2~{S})-4-methyl-2-[(1-quinolin-8-ylsulfonylindol-3-yl)carbonylamino]pentanoic acid
small-molecule 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
AA2AR A2A Adenosine A Human X-ray 7ARO 7ARO_refined 3.1 A Inactive 1 72 - - - - BRIL - CHEMBL124345
small-molecule Agonist (partial) adenosine small-molecule No Yes Amelia T, van Veldhoven JPD, Falsini M, Liu R, Heitman LH, van Westen GJP, Segala E, Verdon G, Cheng RKY, Cooke RM, van der Es D, IJzerman AP. 10.1021/acs.jmedchem.0c01856 2021-04-07 Yes
CASR CaS Calcium-sensing C Human Cryo-EM 7DD5 - 3.2 A Inactive - 74 - - - - - - Calcium
NPS 2143
L-tryptophan
small-molecule
small-molecule
small-molecule		 Agonist
NAM
PAM		 spermine, L-tryptophan, Ca2+, Mg2+ small-molecule No No Wen T, Wang Z, Chen X, Ren Y, Lu X, Xing Y, Lu J, Chang S, Zhang X, Shen Y, Yang X 10.1126/SCIADV.ABG1483 2021-06-16 Yes
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 7EVM - 2.5 R Active 100 61 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 - 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 sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate 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
MRGX2 MRGPRX2 A orphans A Human Cryo-EM 7S8M - 2.5 R Active 100 77 Gi/o αi1 - 62 BRIL scFv16 Cortistatin 14
peptide 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
CCKAR CCK1 Cholecystokinin A Human X-ray 7F8X 7F8X_refined 3.0 A Inactive 1 66 - - - - T4-Lysozyme - NN9056
peptide Agonist desulfated cholecystokinin-8, CCK-33, CCK-8, CCK-58, CCK-4, CCK-39, gastrin-17 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 2021-12-29 Yes
US28 US28 Unclassified A strain AD169 Cryo-EM 7RKM - 3.5 R Active 100 83 Gi/o αi1 - 61 - scFv16 Fractalkine
peptide Agonist - - No No Tsutsumi N, Maeda S, Qu Q, Vogele M, Jude KM, Suomivuori CM, Panova O, Waghray D, Kato HE, Velasco A, Dror RO, Skiniotis G, Kobilka BK, Garcia KC 10.1126/SCIADV.ABL5442 2022-01-26 Yes
ADA2A α2A Adrenoceptors A Human Cryo-EM 7EJA - 3.6 R Active 100 58 Gi/o αo - 59 - scFv16 dexmedetomidine
small-molecule Agonist (-)-adrenaline, (-)-noradrenaline 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
S1PR2 S1P2 Lysophospholipid (S1P) A Human Cryo-EM 7T6B 7T6B_refined 3.2 R Active 100 75 G12/13 α13 - 60 - scFv16 sphingosine 1-phosphate
small-molecule Agonist sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate small-molecule No No Chen H, Chen K, Huang W, Staudt LM, Cyster JG, Li X 10.1126/SCIADV.ABN0067 2022-04-06 Yes
OX2R OX2 Orexin A Human Cryo-EM 7SQO - 3.2 R Active 100 61 Gi/o αi1 - 61 - scFv16 methyl (2R,3S)-3-[(methanesulfonyl)amino]-2-({[(1s,4S)-4-phenylcyclohexyl]oxy}methyl)piperidine-1-carboxylate
small-molecule Agonist orexin-B, orexin-A peptide No No Yin J, Kang Y, McGrath AP, Chapman K, Sjodt M, Kimura E, Okabe A, Koike T, Miyanohana Y, Shimizu Y, Rallabandi R, Lian P, Bai X, Flinspach M, De Brabander JK, Rosenbaum DM 10.1038/S41467-022-30601-3 2022-05-25 Yes
OPRM μ Opioid A Mouse Cryo-EM 7UL4 7UL4_refined 2.8 A Inactive 4 72 - - - - - Megabody-6 alvimopan
small-molecule Antagonist - - 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
APJ apelin Apelin A Human Cryo-EM 7W0O 7W0O_refined 3.8 R Active 100 77 Gi/o αi1 - 64 BRIL scFv16 apelin receptor early endogenous ligand
peptide Agonist apelin-13, apelin-17, apelin-36, Elabela/Toddler-21, [Pyr1]apelin-13, Elabela/Toddler-11, apelin receptor early endogenous ligand, Elabela/Toddler-32 peptide No No Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F 10.1038/S41594-022-00797-5 2022-07-27 Yes
SSR2 SST2 Somatostatin A Human X-ray 7XNA - 2.7 A Inactive 4 78 - - - - - - CYN 154806
peptide Antagonist SRIF-14, CST-17, cortistatin-14, SRIF-28 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
AA2AR A2A Adenosine A Human X-ray 8CU7 8CU7_refined 2.1 A Inactive 1 72 - - - - BRIL - LJ-4517
small-molecule Antagonist adenosine small-molecule No Yes Shiriaeva A, Park D, Kim G, Lee Y, Hou X, Jarhad DB, Kim G, Yu J, Hyun YE, Kim W, Gao ZG, Jacobson KA, Han GW, Stevens RC, Jeong LS, Choi S, Cherezov V. 10.1021/acs.jmedchem.2c00462 2022-08-31 Yes
TSHR TSH Glycoprotein hormone A Human Cryo-EM 7UTZ - 2.4 R Active 100 79 Gs αs Mini-Gs 56 - Nanobody-35 Thyrotropin subunit beta
Glycoprotein hormones alpha chain analog TR1402
protein
protein		 Agonist TSH peptide No No Faust B, Billesbolle CB, Suomivuori CM, Singh I, Zhang K, Hoppe N, Pinto AFM, Diedrich JK, Muftuoglu Y, Szkudlinski MW, Saghatelian A, Dror RO, Cheng Y, Manglik A 10.1038/S41586-022-05159-1 2022-08-03 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 2Y01 - 2.6 A Inactive 0 59 - - - - - - Dobutamine
small-molecule Agonist (partial) - - No No - - 2011-03-30 Yes
PAR1 PAR1 Proteinase-activated A Human X-ray 3VW7 3VW7_refined 2.2 A Intermediate 44 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
SMO SMO Frizzled F Human X-ray 4QIN 4QIN_refined 2.6 A Inactive 11 43 - - - - BRIL - SAG1.5
small-molecule Agonist - - No No Wang C, Wu H, Evron T, Vardy E, Han GW, Huang XP, Hufeisen SJ, Mangano TJ, Urban DJ, Katritch V, Cherezov V, Caron MG, Roth BL, Stevens RC 10.1038/NCOMMS5355 2014-07-23 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 5D5A 5D5A_refined 2.5 A Inactive 0 68 - - - - T4-Lysozyme - Carazolol
small-molecule Inverse agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ 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
CCR9 CCR9 Chemokine A Human X-ray 5LWE - 2.8 B Inactive 55 67 - - - - - - vercirnon
small-molecule Allosteric antagonist CCL25 peptide No No Oswald C, Rappas M, Kean J, Dore AS, Errey JC, Bennett K, Deflorian F, Christopher JA, Jazayeri A, Mason JS, Congreve M, Cooke RM, Marshall FH 10.1038/NATURE20606 2016-12-07 Yes
GLP1R GLP-1 Glucagon B1 Human X-ray 5VEW 5VEW_refined 2.7 A Inactive 0 57 - - - - T4-Lysozyme - PF-06372222
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 2017-05-24 Yes
AA2AR A2A Adenosine A Human X-ray 6AQF 6AQF_refined 2.5 A Inactive 1 72 - - - - BRIL - ZM-241385
small-molecule Antagonist adenosine small-molecule No No Eddy MT, Lee MY, Gao ZG, White KL, Didenko T, Horst R, Audet M, Stanczak P, McClary KM, Han GW, Jacobson KA, Stevens RC, Wuthrich K 10.1016/J.CELL.2017.12.004 2018-01-10 Yes
NPY1R Y1 Neuropeptide Y A Human X-ray 5ZBH 5ZBH_refined 3.0 A Inactive 1 78 - - - - T4-Lysozyme - BMS-193885
small-molecule Antagonist pancreatic polypeptide, neuropeptide Y, peptide YY peptide No No Yang Z, Han S, Keller M, Kaiser A, Bender BJ, Bosse M, Burkert K, Kogler LM, Wifling D, Bernhardt G, Plank N, Littmann T, Schmidt P, Yi C, Li B, Ye S, Zhang R, Xu B, Larhammar D, Stevens RC, Huster D, Meiler J, Zhao Q, Beck-Sickinger AG, Buschauer A, Wu B 10.1038/S41586-018-0046-X 2018-04-25 Yes
CCR5 CCR5 Chemokine A Human X-ray 6AKX 6AKX_refined 2.8 B Inactive 16 82 - - - - Rubredoxin - CHEMBL4238063
small-molecule Antagonist CCL2, CCL8, CCL11, CCL13, CCL14, CCL7, CCL5, CCL4, CCL16, CCL3 peptide No No Peng P, Chen H, Zhu Y, Wang Z, Li J, Luo RH, Wang J, Chen L, Yang LM, Jiang H, Xie X, Wu B, Zheng YT, Liu H. 10.1021/acs.jmedchem.8b01077 2018-10-24 Yes
CALCR CT Calcitonin B1 Human Cryo-EM 6NIY - 3.3 R Active 100 55 Gs αs - 43 - - calcitonin (salmon synthetic)
small-molecule Agonist β-CGRP, α-CGRP, calcitonin, calcitonin (salmon), amylin, adrenomedullin, adrenomedullin 2/intermedin peptide No No - 10.1021/ACSPTSCI.8B00056 2019-01-23 Yes
AA2AR A2A Adenosine A Human X-ray 6JZH 6JZH_refined 2.3 A Inactive 1 72 - - - - BRIL - ZM-241385
small-molecule Antagonist adenosine small-molecule No Yes - 10.1107/S1600576719012846 2019-10-30 Yes
OX1R OX1 Orexin A Human X-ray 6TQ9 6TQ9_refined 2.7 B Inactive 1 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
AGTR1 AT1 Angiotensin A Human X-ray 6OS2 - 2.7 A Active 95 85 - - - - BRIL Nanobody-Nb.AT110i1_le TRV026
peptide Agonist angiotensin A, angiotensin III, angiotensin IV, angiotensin II peptide No No Wingler LM, Skiba MA, McMahon C, Staus DP, Kleinhenz ALW, Suomivuori CM, Latorraca NR, Dror RO, Lefkowitz RJ, Kruse AC 10.1126/SCIENCE.AAY9813 2020-02-19 Yes
GABR2 GABAB2 GABAB C Human Cryo-EM 6VJM - 4.0 B Inactive - 73 - - - - - - Apo (no ligand)
none Apo (no ligand) - - No No - - 2020-06-10 Yes
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 7C2E - 4.2 R Active 100 82 Gs αs - 49 - Nanobody-35 2-[[4-[6-[(4-cyano-2-fluoranyl-phenyl)methoxy]pyridin-2-yl]-3,6-dihydro-2~{H}-pyridin-1-yl]methyl]-3-[[(2~{S})-oxetan-2-yl]methyl]imidazo[4,5-b]pyridine-5-carboxylic acid
small-molecule Agonist glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide peptide No No Ma H, Huang W, Wang X, Zhao L, Jiang Y, Liu F, Guo W, Sun X, Zhong W, Yuan D, Xu HE 10.1038/S41422-020-0384-8 2020-08-26 Yes
GABR2 GABAB2 GABAB C Human Cryo-EM 7CUM - 3.5 B Inactive - 72 - - - - - - CGP 54626A
Unknown ligand
small-molecule
none		 NAM - - No No Kim Y, Jeong E, Jeong JH, Kim Y, Cho Y 10.1016/J.JMB.2020.09.023 2020-11-11 Yes
CCKAR CCK1 Cholecystokinin A Human Cryo-EM 7MBX - 2.0 R Active 100 68 Gs αs - 61 - Nanobody-35 CHEMBL216166
protein Agonist desulfated cholecystokinin-8, CCK-33, CCK-8, CCK-58, CCK-4, CCK-39, gastrin-17 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
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 7DUQ - 2.5 R Active 100 83 Gs αs - 61 - Nanobody-35 N-Tert-butyl-6,7-dichloroquinoxalin-2-amine
CHEMBL410972
small-molecule
protein		 Ago-PAM
Agonist		 glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide peptide No No - 10.1038/S41467-021-24058-Z 2021-07-14 Yes
LSHR LH Glycoprotein hormone A Human Cryo-EM 7FII - 4.3 R Active 100 82 Gs αs - 91 - - Choriogonadotropin beta
Glycoprotein alpha
protein
protein		 Agonist hCG, LH peptide No No Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE 10.1038/S41586-021-03924-2 2021-09-29 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 sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate 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
S1PR1 S1P1 Lysophospholipid (S1P) A Human Cryo-EM 7TD3 - 3.0 R Active 100 76 Gi/o αi1 - 63 - - sphingosine 1-phosphate
small-molecule Agonist sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate 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
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 7FIM - 3.4 R Active 100 83 Gs αs - 57 - Nanobody-35 tirzepatide
peptide Agonist glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide 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
AGRG4 ADGRG4 ADGRG B2 Human Cryo-EM 7WUJ - 3.3 E Active - 9 Gs αs Mini-Gs 59 - scFv16
Nanobody-35		 Apo (no ligand)
none Apo (no ligand) - - No No Xiao P, Guo S, Wen X, He QT, Lin H, Huang SM, Gou L, Zhang C, Yang Z, Zhong YN, Yang CC, Li Y, Gong Z, Tao XN, Yang ZS, Lu Y, Li SL, He JY, Wang C, Zhang L, Kong L, Sun JP, Yu X 10.1038/S41586-022-04590-8 2022-04-27 Yes
ADRB3 β3 Adrenoceptors A Dog Cryo-EM 7XJH - 3.3 R Active 100 68 Gs αs - 59 - Nanobody-35 LEVISOPRENALINE
small-molecule Agonist - - No No Nagiri C, Kobayashi K, Tomita A, Kato M, Kobayashi K, Yamashita K, Nishizawa T, Inoue A, Shihoya W, Nureki O 10.1016/J.MOLCEL.2021.06.024 2022-05-04 Yes
DRD1 D1 Dopamine A Human Cryo-EM 7X2F 7X2F_refined 3.0 F Active 100 63 Gs αs - 58 - Nanobody-35 dopamine
mevidalen
small-molecule
small-molecule		 Agonist
PAM		 noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, 5-hydroxytryptamine, dopamine small-molecule No No Teng X, Chen S, Nie Y, Xiao P, Yu X, Shao Z, Zheng S 10.1038/S41467-022-30929-W 2022-06-15 Yes
GASR CCK2 Cholecystokinin A Human Cryo-EM 7XOX 7XOX_refined 3.1 R Active 100 62 Gq/11 αq - 61 - scFv16 CCK-8
peptide Agonist desulfated cholecystokinin-8, desulfated gastrin-17, CCK-33, CCK-8, CCK-58, desulfated gastrin-71, desulfated gastrin-14, CCK-4, desulfated gastrin-34, gastrin-34, gastrin-14, CCK-39, gastrin-17, gastrin-71 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 2022-07-20 Yes
SSR2 SST2 Somatostatin A Human Cryo-EM 7XAV 7XAV_refined 2.9 A Active 100 76 Gi/o αi1 - 63 - scFv16 lanreotide
peptide Agonist SRIF-14, CST-17, cortistatin-14, SRIF-28 peptide No No Bo Q, Yang F, Li Y, Meng X, Zhang H, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C 10.1038/S41421-022-00405-2 2022-08-31 Yes
PTH1R PTH1 Parathyroid hormone B1 Human Cryo-EM 7VVO 7VVO_refined 4.1 R Active 100 51 Gs αs - 58 - Nanobody-35 Parathyroid hormone
peptide Agonist PTH, PTHrP-(1-36), TIP39, PTHrP 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
5HT2B 5-HT2B 5-Hydroxytryptamine A Human Cryo-EM 7SRQ 7SRQ_refined 2.7 R Intermediate 44 53 - - - - - - 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
FPR1 FPR1 Formylpeptide A Human Cryo-EM 7VFX 7VFX_refined 2.8 R Active 100 84 Gi/o αi1 - 62 - scFv16 Peptide agonist fMet-Ile-Phe-Leu
peptide Agonist cathepsin G, spinorphin, annexin I, fMet-Leu-Phe peptide No No Chen G, Wang X, Liao Q, Ge Y, Jiao H, Chen Q, Liu Y, Lyu W, Zhu L, van Zundert GCP, Robertson MJ, Skiniotis G, Du Y, Hu H, Ye RD 10.1038/S41467-022-32822-Y 2022-09-21 Yes
5HT5A 5-HT5A 5-Hydroxytryptamine A Human Cryo-EM 7X5H 7X5H_refined 3.1 R Active 100 77 Gi/o αi1 - 63 BRIL scFv16 5-CT
small-molecule Agonist 5-hydroxytryptamine small-molecule No No Tan Y, Xu P, Huang S, Yang G, Zhou F, He X, Ma H, Xu HE, Jiang Y 10.1038/S41421-022-00412-3 2022-09-14 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-(1-8), [Met]enkephalin, endomorphin-1, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin B, endomorphin-2 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 C3a, C5a, ribosomal protein S19, C5a des-Arg 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 8HS3 - 3.1 R Active 100 78 Gi/o αi1 - 62 BRIL scFv16 Apo (no ligand)
none Apo (no ligand) - - No No - - 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
GALR1 GAL1 Galanin A Human Cryo-EM 7XJJ 7XJJ_refined 3.3 E Active 100 77 Gi/o αo - 61 - scFv16 galanin
peptide Agonist galanin-like peptide, galanin peptide No No - - 2023-05-03 Yes
TAAR9 TAAR9 A orphans A Mouse Cryo-EM 8ITF - 3.5 R Active 100 86 Gs αs - 59 - scFv16
Nanobody-35		 N,N-Dimethylcyclohexylamine
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
ADA1A α1A Adrenoceptors A Human Cryo-EM 7YMJ - 3.4 A Inactive 4 60 - - - - - Nanobody-6 tamsulosin
small-molecule Antagonist (-)-adrenaline, (-)-noradrenaline small-molecule No No Toyoda Y, Zhu A, Kong F, Shan S, Zhao J, Wang N, Sun X, Zhang L, Yan C, Kobilka BK, Liu X 10.1038/S41467-023-39310-X 2023-07-05 Yes
PF2R FP Prostanoid A Human Cryo-EM 8IUK - 2.7 R Active 100 82 Gq/11 αq - 60 - scFv16
Nanobody-35		 PGF2α
small-molecule Agonist PGE2, PGF2α, thromboxane A2, PGI2, 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 8JD1 - 3.7 2 Inactive - 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
AA2AR A2A Adenosine A Human X-ray 2YDO 2YDO_refined 3.0 A Active 65 73 - - - - - - adenosine
small-molecule Agonist adenosine small-molecule No No - 10.1038/NATURE10136 2011-05-18 Yes
NTR1 NTS1 Neurotensin A Rat X-ray 4GRV 4GRV_refined 2.8 A Active 79 69 - - - - T4-Lysozyme - JMV431
peptide Agonist neuromedin N, neurotensin peptide No No White JF, Noinaj N, Shibata Y, Love J, Kloss B, Xu F, Gvozdenovic-Jeremic J, Shah P, Shiloach J, Tate CG, Grisshammer R 10.1038/NATURE11558 2012-10-17 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 4QKX 4QKX_refined 3.3 A Active 99 69 - - - - T4-Lysozyme Nanobody Q27453560
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ small-molecule No No Weichert D, Kruse AC, Manglik A, Hiller C, Zhang C, Hubner H, Kobilka BK, Gmeiner P 10.1073/PNAS.1410415111 2014-07-23 Yes
ACM1 M1 Acetylcholine (muscarinic) A Human X-ray 5CXV 5CXV_refined 2.7 A Inactive 2 62 - - - - T4-Lysozyme - 0HK
small-molecule Antagonist acetylcholine small-molecule No No Thal DM, Sun B, Feng D, Nawaratne V, Leach K, Felder CC, Bures MG, Evans DA, Weis WI, Bachhawat P, Kobilka TS, Sexton PM, Kobilka BK, Christopoulos A 10.1038/NATURE17188 2016-03-09 Yes
AA2AR A2A Adenosine A Human X-ray 5UIG 5UIG_refined 3.5 A Inactive 19 70 - - - - BRIL - 5-Amino-N-[(2-Methoxyphenyl)methyl]-2-(3-Methylphenyl)-2h-1,2,3-Triazole-4-Carboximidamide
small-molecule Antagonist adenosine small-molecule No No Sun B, Bachhawat P, Chu ML, Wood M, Ceska T, Sands ZA, Mercier J, Lebon F, Kobilka TS, Kobilka BK 10.1073/PNAS.1621423114 2017-02-08 Yes
CCR5 CCR5 Chemokine A Human X-ray 5UIW - 2.2 A Inactive 16 85 - - - - Rubredoxin - 5P7-CCL5
protein Antagonist CCL2, CCL8, CCL11, CCL13, CCL14, CCL7, CCL5, CCL4, CCL16, CCL3 peptide No No Zheng Y, Han GW, Abagyan R, Wu B, Stevens RC, Cherezov V, Kufareva I, Handel TM 10.1016/J.IMMUNI.2017.05.002 2017-06-28 Yes
C5AR1 C5a1 Complement peptide A Human X-ray 6C1Q 6C1Q_refined 2.9 B Inactive 6 82 - - - - BRIL - PMX53
NDT9513727
peptide
small-molecule		 Antagonist
NAM		 C3a, C5a, ribosomal protein S19, C5a des-Arg peptide No No Liu H, Kim HR, Deepak RNVK, Wang L, Chung KY, Fan H, Wei Z, Zhang C 10.1038/S41594-018-0067-Z 2018-05-30 Yes
ACM2 M2 Acetylcholine (muscarinic) A Human X-ray 5ZKB 5ZKB_refined 3.0 A Inactive 2 60 - - - - BRIL - AF-DX 384
small-molecule Antagonist acetylcholine small-molecule No No Suno R, Lee S, Maeda S, Yasuda S, Yamashita K, Hirata K, Horita S, Tawaramoto MS, Tsujimoto H, Murata T, Kinoshita M, Yamamoto M, Kobilka BK, Vaidehi N, Iwata S, Kobayashi T 10.1038/S41589-018-0152-Y 2018-11-21 Yes
NK1R NK1 Tachykinin A Human X-ray 6J20 6J20_refined 2.7 A Inactive 1 71 - - - - T4-Lysozyme - aprepitant
small-molecule Antagonist neurokinin B, neuropeptide-γ, hemokinin 1, substance P, neurokinin A, neuropeptide K peptide No No - 10.1038/S41467-019-08568-5 2019-03-06 Yes
NTR1 NTS1 Neurotensin A Human Cryo-EM 6OSA - 3.0 R Active 100 77 Gi/o αi1 Non-canonical conformation 62 - - JMV449
peptide Agonist neuromedin N, large neurotensin, neurotensin, large neuromedin N peptide No No - - 2019-07-10 Yes
OX1R OX1 Orexin A Human X-ray 6TO7 - 2.3 A Inactive 1 71 - - - - - - suvorexant
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
AGTR1 AT1 Angiotensin A Human X-ray 6OS0 6OS0_refined 2.9 A Active 95 85 - - - - BRIL Nanobody-Nb.AT110i1 angiotensin II
peptide Agonist angiotensin A, angiotensin III, angiotensin IV, angiotensin II peptide No No Wingler LM, Skiba MA, McMahon C, Staus DP, Kleinhenz ALW, Suomivuori CM, Latorraca NR, Dror RO, Lefkowitz RJ, Kruse AC 10.1126/SCIENCE.AAY9813 2020-02-19 Yes
ADRB1 β1 Adrenoceptors A Wild turkey Cryo-EM 6TKO 6TKO_refined 3.3 A Active 100 58 Beta Beta-arrestin-1 - 82 - Fab30 heavy chain
Fab30 light chain		 arformoterol
small-molecule Agonist - - No No - 10.1038/S41586-020-2419-1 2020-06-17 Yes
GHSR ghrelin Ghrelin A Human X-ray 6KO5 6KO5_refined 3.3 A Inactive 1 80 - - - - BRIL Fab7881 heavy chain
Fab7881 light chain		 CHEMBL1956994
small-molecule Antagonist [des-Gln14]ghrelin, ghrelin peptide No No Shiimura Y, Horita S, Hamamoto A, Asada H, Hirata K, Tanaka M, Mori K, Uemura T, Kobayashi T, Iwata S, Kojima M 10.1038/S41467-020-17554-1 2020-08-12 Yes
5HT2A 5-HT2A 5-Hydroxytryptamine A Human X-ray 6WH4 6WH4_refined 3.4 C Inactive 1 59 - - - - BRIL - CHEMBL428892
small-molecule Inverse agonist 5-hydroxytryptamine, tryptamine small-molecule No No Kim K, Che T, Panova O, DiBerto JF, Lyu J, Krumm BE, Wacker D, Robertson MJ, Seven AB, Nichols DE, Shoichet BK, Skiniotis G, Roth BL 10.1016/J.CELL.2020.08.024 2020-09-23 Yes
ADRB2 β2 Adrenoceptors A Human Cryo-EM 7DHR 7DHR_refined 3.8 R Active 100 69 Gs αs - 49 - Nanobody-35 LEVISOPRENALINE
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ small-molecule No No Jin Y, Zhao Q, Zhu W, Feng Y, Xiao T, Zhang P, Jiang L, Hou Y, Guo C, Huang H, Chen Y, Tong X, Cao J, Li F, Zhu X, Qin J, Gao D, Liu XY, Zhang H, Chen L, Thomas RK, Wong KK, Zhang L, Wang Y, Hu L, Ji H 10.1093/NSR/NWAA284 2020-12-16 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, (-)-noradrenaline, 5-hydroxytryptamine, dopamine 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 PGE2, PGF2α, thromboxane A2, PGI2, PGE1, PGD2 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
Q3KSP2 BILF1 Unclassified A strain GD1 Cryo-EM 7JHJ - 3.2 R Active 100 89 Gi/o αi1 - 62 - scFv16 Apo (no ligand)
none Apo (no ligand) - - No No - 10.1016/J.IMMUNI.2021.06.001 2021-07-07 Yes
PTH2R PTH2 Parathyroid hormone B1 Human Cryo-EM 7F16 - 2.8 R Active 100 68 Gs αs - 58 - Nanobody-35 TIP39
peptide Agonist PTHrP-(1-34) (human), TIP39, PTHrP-(1-36), PTHrP, PTH peptide No No Wang X, Cheng X, Zhao L, Wang Y, Ye C, Zou X, Dai A, Cong Z, Chen J, Zhou Q, Xia T, Jiang H, Xu HE, Yang D, Wang MW 10.1073/PNAS.2101279118 2021-08-18 Yes
NK1R NK1 Tachykinin A Human Cryo-EM 7RMH 7RMH_refined 3.1 R Active 100 70 Gs αs - 55 - Nanobody-35 substance P
peptide Agonist neurokinin B, neuropeptide-γ, hemokinin 1, substance P, neurokinin A, neuropeptide K 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
GP139 GPR139 A orphans A Human Cryo-EM 7VUI 7VUI_refined 3.3 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
CASR CaS Calcium-sensing C Human Cryo-EM 7SIL 7SIL_refined 2.7 A Active - 72 - - - - - - tecalcet
Cyclomethyltryptophan
small-molecule
small-molecule		 Agonist spermine, L-tryptophan, Ca2+, Mg2+ 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
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 - - 2022-03-02 Yes
ADA2A α2A Adrenoceptors A Human Cryo-EM 7EJ8 - 3.0 R Active 100 57 Gi/o αo - 61 - scFv16 brimonidine
small-molecule Agonist (-)-adrenaline, (-)-noradrenaline 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
AA2AR A2A Adenosine A Human X-ray 7EZC 7EZC_refined 3.8 B Active 65 70 - - - - BRIL - UK-432,097
small-molecule Agonist adenosine small-molecule No No Cui M, Zhou Q, Xu Y, Weng Y, Yao D, Zhao S, Song G 10.1107/S2052252522001907 2022-04-13 Yes
NMUR2 NMU2 Neuromedin U A Human Cryo-EM 7W57 - 3.2 R Active 100 72 Gq/11 αq - 59 - scFv16 Neuromedin-S
peptide Agonist neuromedin U-25, neuromedin U-23, 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
MRGRD MRGPRD A orphans A Human Cryo-EM 7Y12 - 3.1 R Active 100 82 Gi/o αi1 - 62 BRIL scFv16 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
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 8IWM - 3.2 R Active 97 78 - - - - - - 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
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
HCAR2 HCA2 Hydroxycarboxylic acid A Human X-ray 7ZL9 - 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
OPRK κ Opioid A Human Cryo-EM 8DZS - 2.7 A Active 100 71 Gi/o αz - 59 - scFv16 CHEMBL277863
small-molecule Agonist dynorphin A-(1-8), β-neoendorphin, big dynorphin, [Met]enkephalin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin B, α-neoendorphin peptide No No Han J, Zhang J, Nazarova AL, Bernhard SM, Krumm BE, Zhao L, Lam JH, Rangari VA, Majumdar S, Nichols DE, Katritch V, Yuan P, Fay JF, Che T 10.1038/S41586-023-06030-7 2023-05-03 Yes
DRD3 D3 Dopamine A Human Cryo-EM 8IRT - 2.7 R Active 100 68 Gi/o αi1 - 63 BRIL scFv16 rotigotine
small-molecule Agonist dopamine small-molecule No No Xu P, Huang S, Krumm BE, Zhuang Y, Mao C, Zhang Y, Wang Y, Huang XP, Liu YF, He X, Li H, Yin W, Jiang Y, Zhang Y, Roth BL, Xu HE 10.1038/S41422-023-00808-0 2023-06-07 Yes
GPR84 GPR84 A orphans A Human Cryo-EM 8J18 - 2.9 R Active 100 73 Gi/o αi1 - 62 - scFv16 (3R)-3-HYDROXYDODECANOIC ACID
small-molecule Agonist - - 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
NTR1 NTS1 Neurotensin A Human Cryo-EM 8JPB - 3.1 R Active 100 71 Gq/11 αq GRK2 bound 88 - GRK2 JMV431
CHEMBL4576388
peptide
small-molecule		 Agonist
PAM		 neuromedin N, large neurotensin, neurotensin, large neuromedin N peptide No No Duan J, Liu H, Zhao F, Yuan Q, Ji Y, Cai X, He X, Li X, Li J, Wu K, Gao T, Zhu S, Lin S, Wang MW, Cheng X, Yin W, Jiang Y, Yang D, Xu HE 10.1038/S41586-023-06395-9 2023-08-09 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 2YCW 2YCW_refined 3.0 A Inactive 0 61 - - - - - - Carazolol
small-molecule Antagonist - - No No - 10.1073/PNAS.1100185108 2011-06-01 Yes
GLR glucagon Glucagon B1 Human X-ray 4L6R 4L6R_refined 3.3 A Inactive 7 61 - - - - BRIL - - - - glucagon peptide No No Siu FY, He M, de Graaf C, Han GW, Yang D, Zhang Z, Zhou C, Xu Q, Wacker D, Joseph JS, Liu W, Lau J, Cherezov V, Katritch V, Wang MW, Stevens RC 10.1038/nature12393 2013-07-24 Yes
GRM1 mGlu1 Metabotropic glutamate C Human X-ray 4OR2 4OR2_refined 2.8 B Inactive - 22 - - - - BRIL - FITM
small-molecule NAM L-glutamic acid small-molecule No No Wu H, Wang C, Gregory KJ, Han GW, Cho HP, Xia Y, Niswender CM, Katritch V, Meiler J, Cherezov V, Conn PJ, Stevens RC 10.1126/science.1249489 2014-03-19 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
SMO SMO Frizzled F Human X-ray 5L7I 5L7I_refined 3.3 B Inactive 4 59 - - - - BRIL - vismodegib
small-molecule Antagonist - - No No - - 2016-07-20 Yes
EDNRB ETB Endothelin A Human X-ray 5XPR 5XPR_refined 3.6 A Inactive 4 69 - - - - T4-Lysozyme - bosentan
small-molecule Antagonist endothelin-1, endothelin-2, endothelin-3 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
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 Intermediate 44 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
PE2R4 EP4 Prostanoid A Human X-ray 5YWY 5YWY_refined 3.2 A Inactive 9 57 - - - - - Fab ONO-AE3-208
small-molecule Antagonist PGE2, PGF2α, thromboxane A2, PGI2, PGE1, PGD2 small-molecule No No - - 2018-12-05 Yes
MTR1B MT2 Melatonin A Human X-ray 6ME6 6ME6_refined 2.8 B Inactive 1 78 - - - - Rubredoxin - CHEMBL15060
small-molecule Agonist melatonin small-molecule No No - 10.1038/S41586-019-1144-0 2019-04-24 Yes
GLP1R GLP-1 Glucagon B1 Human X-ray 6KK1 6KK1_refined 2.8 B Inactive 0 57 - - - - T4-Lysozyme - PF-06372222
small-molecule NAM glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide peptide No No - - 2019-11-13 Yes
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 6ORV 6ORV_refined 3.0 E Active 100 61 Gs αs - 49 - Nanobody-35 CHEMBL3950796
small-molecule Agonist glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide peptide No No Zhao P, Liang YL, Belousoff MJ, Deganutti G, Fletcher MM, Willard FS, Bell MG, Christe ME, Sloop KW, Inoue A, Truong TT, Clydesdale L, Furness SGB, Christopoulos A, Wang MW, Miller LJ, Reynolds CA, Danev R, Sexton PM, Wootten D 10.1038/s41586-019-1902-z 2020-01-08 Yes
FPR2 FPR2/ALX Formylpeptide A Human X-ray 6LW5 6LW5_refined 2.8 A Active 100 91 - - - - BRIL - CHEMBL552527
protein Agonist resolvin D1, serum amyloid A, 15-deoxy-LXA4, LTC4, LL-37, humanin, LTD4, aspirin triggered lipoxin A4, annexin I, aspirin-triggered resolvin D1, fMet-Leu-Phe, PrP106-126, LXA4 peptide No No Chen T, Xiong M, Zong X, Ge Y, Zhang H, Wang M, Won Han G, Yi C, Ma L, Ye RD, Xu Y, Zhao Q, Wu B 10.1038/S41467-020-15009-1 2020-03-25 Yes
GABR2 GABAB2 GABAB C Human Cryo-EM 7C7S - 2.9 B Inactive - 71 - - - - - - CGP 54626A
small-molecule Antagonist - - 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
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		 deoxycholic acid, chenodeoxycholic acid, lithocholic acid, cholic 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
ADRB1 β1 Adrenoceptors A Human X-ray 7BU6 7BU6_refined 2.7 A Active 99 58 - - - - T4-Lysozyme Camelid antibody fragment Nb6B9 Noradrenaline
small-molecule Agonist noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, (-)-noradrenaline 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
AGRG3 ADGRG3 ADGRG B2 Human Cryo-EM 7D76 - 3.1 R Active - 48 Gi/o αo - 61 - - Beclomethasone
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
CASR CaS Calcium-sensing C Human Cryo-EM 7DTU 7DTU_refined 4.4 A Intermediate - 72 - - - - - - L-tryptophan
small-molecule PAM spermine, L-tryptophan, Ca2+, Mg2+ small-molecule No No - - 2021-03-10 Yes
CCR5 CCR5 Chemokine A Human Cryo-EM 7O7F 7O7F_refined 3.2 C Active 100 85 Gi/o αi1 - 62 - Fab heavy chain
Fab light chain		 CCL5
peptide Agonist CCL2, CCL8, CCL11, CCL13, CCL14, CCL7, CCL5, CCL4, CCL16, CCL3 peptide No No - 10.1126/SCIADV.ABG8685 2021-06-30 Yes
MRGX2 MRGPRX2 A orphans A Human Cryo-EM 7S8N 7S8N_refined 2.9 R Active 100 76 Gq/11 αq Gq-Gs chimera 57 - 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
MRGX2 MRGPRX2 A orphans A Human Cryo-EM 7VV0 7VV0_refined 3.5 R Active 97 80 - - - - - - PAMP-12
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
5HT2A 5-HT2A 5-Hydroxytryptamine A Human X-ray 7WC5 7WC5_refined 3.2 A Inactive 1 60 - - - - BRIL - psilocin
small-molecule Agonist 5-hydroxytryptamine, tryptamine small-molecule No No - - 2022-01-26 Yes
MSHR MC1 Melanocortin A Human Cryo-EM 7F4I 7F4I_refined 3.1 R Active 100 84 Gs αs - 59 - Nanobody-35 bremelanotide
peptide Agonist γ-MSH, ACTH, 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
S1PR1 S1P1 Lysophospholipid (S1P) A Human Cryo-EM 7TD4 - 2.6 R Active 100 76 Gi/o αi1 - 63 - - siponimod
small-molecule Agonist sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate 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
GRM3 mGlu3 Metabotropic glutamate C Human Cryo-EM 7WI6 7WI6_refined 3.7 A Inactive - 82 - - - - - - LY341495
small-molecule Antagonist L-glutamic acid, NAAG small-molecule No No Fang W, Yang F, Xu C, Ling S, Lin L, Zhou Y, Sun W, Wang X, Liu P, Rondard P, Shi P, Pin JP, Tian C, Liu J 10.1038/S41422-022-00623-Z 2022-03-16 Yes
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 7RG9 7RG9_refined 3.2 R Active 100 58 Gs αs - 56 - scFv16
Nanobody-35		 Apo (no ligand)
none Apo (no ligand) glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide 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
ACM4 M4 Acetylcholine (muscarinic) A Human Cryo-EM 7V68 - 3.4 R Active 100 58 Gi/o αi1 - 62 - scFv16 iperoxo
LY2119620
small-molecule
small-molecule		 Agonist
PAM		 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
TRFR TRH1 Thyrotropin-releasing hormone A Human Cryo-EM 7WKD - 3.0 R Active 100 66 Gq/11 αq - 60 - scFv16 TRH
peptide Agonist TRH peptide No No Xu Y, Cai H, You C, He X, Yuan Q, Jiang H, Cheng X, Jiang Y, Xu HE 10.1038/S41422-022-00641-X 2022-06-15 Yes
MRGRD MRGPRD A orphans A Human Cryo-EM 7Y13 7Y13_refined 3.1 R Intermediate 55 82 - - - - BRIL - 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
SSR2 SST2 Somatostatin A Human X-ray 7XN9 7XN9_refined 2.6 A Inactive 4 79 - - - - - - L-054,522
small-molecule Antagonist SRIF-14, CST-17, cortistatin-14, SRIF-28 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
AA2AR A2A Adenosine A Human X-ray 8DU3 8DU3_refined 2.5 A Inactive 1 72 - - - - BRIL - CHEMBL5206530
small-molecule Antagonist adenosine small-molecule No No Bolteau R, Duroux R, Laversin A, Vreulz B, Shiriaeva A, Stauch B, Han GW, Cherezov V, Renault N, Barczyk A, Ravez S, Coevoet M, Melnyk P, Liberelle M, Yous S. 10.1016/j.ejmech.2022.114620 2022-08-10 Yes
TSHR TSH Glycoprotein hormone A Human Cryo-EM 7T9N - 2.9 R Active 100 73 Gs αs Mini-Gs 56 - M22 Fab light chain
M22 Fab heavy chain
Nanobody-35		 M22 antibody light chain
M22 antibody heavy chain
protein
protein		 Agonist TSH peptide No No Faust B, Billesbolle CB, Suomivuori CM, Singh I, Zhang K, Hoppe N, Pinto AFM, Diedrich JK, Muftuoglu Y, Szkudlinski MW, Saghatelian A, Dror RO, Cheng Y, Manglik A 10.1038/S41586-022-05159-1 2022-08-03 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 2YCX - 3.3 A Inactive 0 59 - - - - - - (S)-Cyanopindolol
small-molecule Antagonist - - No No - - 2011-06-01 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 4BEY 4BEY_refined 2.9 A Active 100 94 Gi/o αt1 Only H5 3 - - 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 2013-05-08 Yes
P2Y12 P2Y12 P2Y A Human X-ray 4PY0 4PY0_refined 3.1 A Intermediate 44 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
OPSD Rhodopsin Opsins A Bovine X-ray 4X1H 4X1H_refined 2.3 A Active 100 94 Gi/o αt1 Only H5 3 - - B-Nonylglucoside
small-molecule unknown - - No No Blankenship E, Vahedi-Faridi A, Lodowski DT 10.1016/J.STR.2015.09.015 2015-11-04 Yes
EDNRB ETB Endothelin A Human X-ray 5GLH 5GLH_refined 2.8 A Inactive 15 66 - - - - T4-Lysozyme - ENDOTHELIN
protein Agonist endothelin-1, endothelin-2, endothelin-3 peptide No No - 10.1038/nature19319 2016-09-07 Yes
CNR1 CB1 Cannabinoid A Human X-ray 5XR8 5XR8_refined 3.0 A Active 91 60 - - - - Flavodoxin - AM841
small-molecule Agonist 2-arachidonoylglycerol, anandamide 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 5OM4 5OM4_refined 2.0 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
C5AR1 C5a1 Complement peptide A Human X-ray 6C1R 6C1R_refined 2.2 B Inactive 6 83 - - - - BRIL - PMX53
avacopan
peptide
small-molecule		 Antagonist
NAM		 C3a, C5a, ribosomal protein S19, C5a des-Arg peptide No No - - 2018-05-30 Yes
ACM2 M2 Acetylcholine (muscarinic) A Human X-ray 5ZKC 5ZKC_refined 2.3 A Inactive 2 60 - - - - BRIL - N-methyl scopolamine
small-molecule Antagonist acetylcholine small-molecule No No Suno R, Lee S, Maeda S, Yasuda S, Yamashita K, Hirata K, Horita S, Tawaramoto MS, Tsujimoto H, Murata T, Kinoshita M, Yamamoto M, Kobilka BK, Vaidehi N, Iwata S, Kobayashi T 10.1038/S41589-018-0152-Y 2018-11-21 Yes
5HT2A 5-HT2A 5-Hydroxytryptamine A Human X-ray 6A94 6A94_refined 2.9 A Inactive 1 60 - - - - BRIL - zotepine
small-molecule Antagonist 5-hydroxytryptamine, tryptamine small-molecule No No - - 2019-02-13 Yes
SMO SMO Frizzled F Mouse X-ray 6O3C 6O3C_refined 2.8 A Active 95 61 - - - - - Nanobody-Smo8 SAG21k
small-molecule Agonist - - No No - 10.1038/S41586-019-1355-4 2019-07-03 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 6PS4 6PS4_refined 2.6 A Inactive 0 68 - - - - T4-Lysozyme - ICI 118551
small-molecule Antagonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ small-molecule No No - 10.1107/S2052252519013137 2019-11-13 Yes
OX1R OX1 Orexin A Human X-ray 6TQ4 6TQ4_refined 2.3 B Inactive 1 70 - - - - - - CHEMBL4590386
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
GPR52 GPR52 A orphans A Human X-ray 6LI1 6LI1_refined 2.9 A Intermediate 40 81 - - - - Flavodoxin - 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 6LML 6LML_refined 3.9 R Active 100 83 Gi/o αi1 - 63 - scFv16 glucagon
peptide Agonist glucagon peptide No No Qiao A, Han S, Li X, Li Z, Zhao P, Dai A, Chang R, Tai L, Tan Q, Chu X, Ma L, Thorsen TS, Reedtz-Runge S, Yang D, Wang MW, Sexton PM, Wootten D, Sun F, Zhao Q, Wu B 10.1126/SCIENCE.AAZ5346 2020-04-01 Yes
ADRB1 β1 Adrenoceptors A Wild turkey Cryo-EM 7JJO - 2.6 R Active 100 58 Gs αs - 51 - Nanobody-35 LEVISOPRENALINE
small-molecule Agonist - - No No Su M, Zhu L, Zhang Y, Paknejad N, Dey R, Huang J, Lee MY, Williams D, Jordan KD, Eng ET, Ernst OP, Meyerson JR, Hite RK, Walz T, Liu W, Huang XY 10.1016/J.MOLCEL.2020.08.001 2020-09-02 Yes
AA2AR A2A Adenosine A Human X-ray 6LPK 6LPK_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
NTR1 NTS1 Neurotensin A Rat X-ray 6Z4Q - 2.9 A Inactive 32 75 - - - - DARPin D12 - SR142948A
small-molecule Inverse agonist neuromedin N, neurotensin peptide No No - - 2021-02-10 Yes
5HT1A 5-HT1A 5-Hydroxytryptamine A Human Cryo-EM 7E2Y - 3.0 R Active 100 65 Gi/o αi1 - 62 - - 5-hydroxytryptamine
small-molecule Agonist 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
CASR CaS Calcium-sensing C Human Cryo-EM 7M3J 7M3J_refined 4.1 A Inactive - 72 - - - - - - NPS 2143
small-molecule NAM spermine, L-tryptophan, Ca2+, Mg2+ small-molecule No No - - 2021-06-30 Yes
GRM5 mGlu5 Metabotropic glutamate C Human Cryo-EM 7FD9 7FD9_refined 4.0 A Inactive - 63 - - - - - - LY341495
small-molecule Antagonist 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
GASR CCK2 Cholecystokinin A Human Cryo-EM 7F8V - 3.3 R Active 100 62 Gi/o αi2 - 61 - - desulfated gastrin-17
peptide Agonist desulfated cholecystokinin-8, desulfated gastrin-17, CCK-33, CCK-8, CCK-58, desulfated gastrin-71, desulfated gastrin-14, CCK-4, desulfated gastrin-34, gastrin-34, gastrin-14, CCK-39, gastrin-17, gastrin-71 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
MRGX2 MRGPRX2 A orphans A Human Cryo-EM 7VV3 - 3.0 R Active 100 79 Gi/o αi1 - 62 - scFv16 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
US28 US28 Unclassified A strain AD169 Cryo-EM 7RKF - 4.0 R Active 100 84 Gq/11 α11 - 97 - scFv16 Fractalkine
peptide Agonist - - No No Tsutsumi N, Maeda S, Qu Q, Vogele M, Jude KM, Suomivuori CM, Panova O, Waghray D, Kato HE, Velasco A, Dror RO, Skiniotis G, Kobilka BK, Garcia KC 10.1126/SCIADV.ABL5442 2022-01-26 Yes
GLR glucagon Glucagon B1 Human Cryo-EM 7V35 7V35_refined 3.4 R Active 100 82 Gs αs - 53 - Nanobody-35 Peptide-20
peptide Agonist glucagon 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
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-25, neuromedin U-23, 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
GASR CCK2 Cholecystokinin A Human Cryo-EM 7XOW 7XOW_refined 3.1 R Active 100 62 Gq/11 αq - 61 - scFv16 desulfated gastrin-17
peptide Agonist desulfated cholecystokinin-8, desulfated gastrin-17, CCK-33, CCK-8, CCK-58, desulfated gastrin-71, desulfated gastrin-14, CCK-4, desulfated gastrin-34, gastrin-34, gastrin-14, CCK-39, gastrin-17, gastrin-71 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 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, cortistatin-14, SRIF-28 peptide No No - - 2022-08-03 Yes
AGRG2 ADGRG2 ADGRG B2 Mouse Cryo-EM 7YP7 - 3.1 R Active - 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 7WY8 - 2.8 R Active - 17 Gs αs Mini-Gs 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 7YU6 7YU6_refined 3.5 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
OPRX NOP Opioid A Human Cryo-EM 8F7X 8F7X_refined 3.3 R Active 100 77 Gi/o αi1 - 62 - scFv16 nociceptin/orphanin FQ
peptide Agonist nociceptin/orphanin FQ 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
NTR1 NTS1 Neurotensin A Rat Cryo-EM 8FN1 - 2.9 A Active 100 66 Gi/o αo - 60 - scFv16 neurotensin
peptide Agonist neuromedin N, neurotensin peptide No No - - 2023-03-29 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, oleic acid, α-linolenic acid, myristic acid small-molecule No No - 10.1126/SCIENCE.ADD6220 2023-03-15 Yes
AGRF1 ADGRF1 ADGRF B2 Human Cryo-EM 8G2Y - 3.4 R Active - 28 Gq/11 αq Gs-mini-Gq chimera 52 - Nanobody-35 [1-Myristoyl-glycerol-3-YL]phosphonylcholine
small-molecule Agonist - - No No Jones DTD, Dates AN, Rawson SD, Burruss MM, Lipper CH, Blacklow SC 10.1038/S41467-023-38083-7 2023-05-10 Yes
ACM4 M4 Acetylcholine (muscarinic) A Human Cryo-EM 7TRQ - 2.5 R Active 100 57 Gi/o αi1 - 64 - scFv16 iperoxo
VU0467154
small-molecule
small-molecule		 Agonist
PAM		 acetylcholine small-molecule No No - - 2023-05-17 Yes
P2RY1 P2Y1 P2Y A Human Cryo-EM 7XXH 7XXH_refined 2.9 R Active 100 81 Gq/11 α11 - 63 - scFv16 2MeSADP
small-molecule Agonist ADP, ATP small-molecule No No - - 2023-06-07 Yes
NMBR BB1 Bombesin A Human Cryo-EM 8H0P - 3.2 R Active 100 75 Gq/11 αq - 56 - scFv16 NMB30
peptide Agonist gastrin-releasing peptide, neuromedin B, gastrin releasing peptide(14-27) (human), GRP-(18-27) peptide No No Li C, Xu Y, Liu H, Cai H, Jiang Y, Xu HE, Yin W 10.1038/S41422-022-00743-6 2023-08-09 Yes
GRM2 mGlu2 Metabotropic glutamate C Human Cryo-EM 8JCW - 3.0 2 Inactive - 87 - - - - - - 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 Japanese flying squid X-ray 3AYM - 2.8 B Inactive 17 77 - - - - - - Retinal (all-trans)
small-molecule Agonist - - No No - 10.1016/J.JMB.2011.08.044 2011-08-17 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 4LDE 4LDE_refined 2.8 A Active 99 69 - - - - T4-Lysozyme Nanobody CHEMBL1615159
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ 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
US28 US28 Unclassified A strain AD169 X-ray 4XT3 4XT3_refined 3.8 A Active 100 81 - - - - - - CX3CL1
peptide Agonist (partial) - - No No Burg JS, Ingram JR, Venkatakrishnan AJ, Jude KM, Dukkipati A, Feinberg EN, Angelini A, Waghray D, Dror RO, Ploegh HL, Garcia KC 10.1126/SCIENCE.AAA5026 2015-03-04 Yes
NTR1 NTS1 Neurotensin A Rat X-ray 5T04 5T04_refined 3.3 A Active 79 69 - - - - T4-Lysozyme - neurotensin
peptide Agonist neuromedin N, neurotensin peptide No No Krumm BE, Lee S, Bhattacharya S, Botos I, White CF, Du H, Vaidehi N, Grisshammer R 10.1038/SREP38564 2016-12-21 Yes
CNR1 CB1 Cannabinoid A Human X-ray 5XRA 5XRA_refined 2.8 A Active 91 60 - - - - Flavodoxin - AM11542
small-molecule Agonist 2-arachidonoylglycerol, anandamide 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 5OLV 5OLV_refined 2.0 A Inactive 1 72 - - - - BRIL - CHEMBL1671936
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
Q80KM9 US28 Unclassified A strain AD169 X-ray 5WB1 5WB1_refined 3.5 A Active 100 82 - - - - - Nanobody - - - - - 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
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 6H7O 6H7O_refined 2.8 A Active 99 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
AGTR1 AT1 Angiotensin A Human X-ray 6DO1 6DO1_refined 2.9 A Active 95 85 - - - - BRIL Nanobody-Nb.AT110i1 CHEMBL404594
protein Agonist angiotensin A, angiotensin III, angiotensin IV, angiotensin II peptide No No - 10.1016/J.CELL.2018.12.006 2019-01-30 Yes
CNR1 CB1 Cannabinoid A Human X-ray 6KQI 6KQI_refined 3.3 A Inactive 11 60 - - - - GlgA glycogen synthase - CP55940
Org27569
small-molecule
small-molecule		 Agonist
NAM		 2-arachidonoylglycerol, anandamide small-molecule No No - 10.1038/S41589-019-0387-2 2019-10-23 Yes
OX1R OX1 Orexin A Human X-ray 6TP6 6TP6_refined 2.3 B Inactive 1 71 - - - - - - filorexant
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
DRD2 D2 Dopamine A Human X-ray 6LUQ 6LUQ_refined 3.1 A Inactive 1 59 - - - - T4-Lysozyme - haloperidol
small-molecule Antagonist dopamine small-molecule No No Fan L, Tan L, Chen Z, Qi J, Nie F, Luo Z, Cheng J, Wang S 10.1038/S41467-020-14884-Y 2020-03-04 Yes
MC4R MC4 Melanocortin A Human X-ray 6W25 - 2.8 A Intermediate 49 79 - - - - GlgA glycogen synthase - SHU9119
Calcium
peptide
small-molecule		 Antagonist
Cofactor		 agouti-related protein, β-MSH, α-MSH, γ-MSH, ACTH peptide No No Yu J, Gimenez LE, Hernandez CC, Wu Y, Wein AH, Han GW, McClary K, Mittal SR, Burdsall K, Stauch B, Wu L, Stevens SN, Peisley A, Williams SY, Chen V, Millhauser GL, Zhao S, Cone RD, Stevens RC 10.1126/SCIENCE.AAZ8995 2020-04-29 Yes
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 6VCB - 3.3 R Active 100 82 Gs αs - 57 - Nanobody-35 glucagon-like peptide 1-(7-37)
CHEMBL5197819
peptide
small-molecule		 Agonist
PAM		 glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide peptide No No Bueno AB, Sun B, Willard FS, Feng D, Ho JD, Wainscott DB, Showalter AD, Vieth M, Chen Q, Stutsman C, Chau B, Ficorilli J, Agejas FJ, Cumming GR, Jimenez A, Rojo I, Kobilka TS, Kobilka BK, Sloop KW 10.1038/S41589-020-0589-7 2020-07-22 Yes
NTR1 NTS1 Neurotensin A Rat Cryo-EM 7L0P - 4.1 C Active 100 73 Gi/o αi1 - 63 - - neurotensin
peptide Agonist neuromedin N, neurotensin peptide No No Zhang M, Gui M, Wang ZF, Gorgulla C, Yu JJ, Wu H, Sun ZJ, Klenk C, Merklinger L, Morstein L, Hagn F, Pluckthun A, Brown A, Nasr ML, Wagner G 10.1038/S41594-020-00554-6 2021-01-06 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, (-)-noradrenaline, 5-hydroxytryptamine, dopamine 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
V2R V2 Vasopressin and oxytocin A Human Cryo-EM 7BB6 - 4.2 A Active 100 73 Gs αs - 54 - Nanobody-35 vasopressin
peptide Agonist oxytocin, vasopressin peptide No No Bous J, Orcel H, Floquet N, Leyrat C, Lai-Kee-Him J, Gaibelet G, Ancelin A, Saint-Paul J, Trapani S, Louet M, Sounier R, Demene H, Granier S, Bron P, Mouillac B 10.1126/SCIADV.ABG5628 2021-06-02 Yes
GRM2 mGlu2 Metabotropic glutamate C Human Cryo-EM 7MTR 7MTR_refined 3.3 A Active - 88 - - - - - - 2-methoxy-6-propyl-N-(2-{4-[(1H-tetrazol-5-yl)methoxy]phenyl}ethyl)thieno[2,3-d]pyrimidin-4-amine
L-glutamic acid
small-molecule
small-molecule		 Ago-PAM
Agonist		 L-glutamic acid small-molecule No No - - 2021-07-07 Yes
CASR CaS Calcium-sensing C Human Cryo-EM 7E6U 7E6U_refined 6.0 A Inactive - 72 - - - - - Nanobody-2D11 Apo (no ligand)
none Apo (no ligand) spermine, L-tryptophan, Ca2+, Mg2+ small-molecule No No - - 2021-09-22 Yes
GP158 GPR158 C Orphans C Human Cryo-EM 7EWR 7EWR_refined 4.7 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
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 7LLY 7LLY_refined 3.3 R Active 100 77 Gs αs - 50 - Nanobody-35 Pro-glucagon
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
LPAR1 LPA1 Lysophospholipid (LPA) A Human Cryo-EM 7TD1 - 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
FPR2 FPR2/ALX Formylpeptide A Human Cryo-EM 7WVV 7WVV_refined 2.9 R Active 100 85 Gi/o αi2 - 63 BRIL - synthetic peptide
peptide Agonist resolvin D1, serum amyloid A, 15-deoxy-LXA4, LTC4, LL-37, humanin, LTD4, aspirin triggered lipoxin A4, annexin I, aspirin-triggered resolvin D1, fMet-Leu-Phe, PrP106-126, LXA4 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
GPR88 GPR88 A orphans A Human Cryo-EM 7EJX - 2.4 R Active 100 60 Gi/o αi1 - 61 - scFv16 compound 2 [PMID: 24793972]
small-molecule Allosteric agonist - - No No Chen G, Xu J, Inoue A, Schmidt MF, Bai C, Lu Q, Gmeiner P, Liu Z, Du Y 10.1038/S41467-022-30081-5 2022-04-13 Yes
OX2R OX2 Orexin A Human Cryo-EM 7SR8 - 3.3 R Active 100 64 Gq/11 αq - 58 - scFv16 methyl (2R,3S)-3-[(methanesulfonyl)amino]-2-({[(1s,4S)-4-phenylcyclohexyl]oxy}methyl)piperidine-1-carboxylate
small-molecule Agonist orexin-B, orexin-A peptide No No Yin J, Kang Y, McGrath AP, Chapman K, Sjodt M, Kimura E, Okabe A, Koike T, Miyanohana Y, Shimizu Y, Rallabandi R, Lian P, Bai X, Flinspach M, De Brabander JK, Rosenbaum DM 10.1038/S41467-022-30601-3 2022-06-08 Yes
CNR1 CB1 Cannabinoid A Human X-ray 7FEE 7FEE_refined 2.7 A Inactive 11 61 - - - - GlgA glycogen synthase - CP55940
6-methyl-3-[(1S)-2-nitro-1-thiophen-2-yl-ethyl]-2-phenyl-1H-indole
small-molecule
small-molecule		 Agonist
PAM		 2-arachidonoylglycerol, anandamide 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 7SK7 - 3.3 A Active 95 74 - - - - - CID25 Fab light chain
CID25 Fab heavy chain
anti-Fab Nanobody		 Stromal cell-derived factor 1
(1R)-4-[7-(3-carboxypropoxy)-6-methylquinolin-8-yl]-1-{[2-(4-hydroxypiperidin-1-yl)-1,3-thiazol-4-yl]methyl}-1,4-diazepan-1-ium
peptide
small-molecule		 Agonist
Agonist (partial)		 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
ACM3 M3 Acetylcholine (muscarinic) A Human Cryo-EM 8E9W - 2.7 A Active 100 47 Gq/11 αq Mini-Gq 57 - scFv16 CHEMBL73538
small-molecule Agonist acetylcholine small-molecule No No - - 2022-11-30 Yes
PTH1R PTH1 Parathyroid hormone B1 Human Cryo-EM 8HAO - 3.8 R Active 100 61 Gs αs - 60 - Nanobody-35 teriparatide
peptide Agonist PTH, PTHrP-(1-36), TIP39, PTHrP peptide No No Zhao LH, Yuan QN, Dai AT, He XH, Chen CW, Zhang C, Xu YW, Zhou Y, Wang MW, Yang DH, Xu HE 10.1038/S41401-022-01032-Z 2022-12-21 Yes
ACM2 M2 Acetylcholine (muscarinic) A Human Cryo-EM 7T8X 7T8X_refined 3.2 A Active 100 59 Gi/o αo - 62 - Antibody fragment acetylcholine
small-molecule Agonist acetylcholine small-molecule No No - - 2023-01-25 Yes
GP174 GPR174 A orphans A Human Cryo-EM 7XV3 7XV3_refined 2.8 R Active 100 87 Gs αs - 59 - - (2~{S})-2-$l^{4}-azanyl-3-[[(2~{R})-3-octadecanoyloxy-2-oxidanyl-propoxy]-oxidanyl-oxidanylidene-$l^{6}-phosphanyl]oxy-propanoic acid
small-molecule Agonist lysophosphatidylserine small-molecule No No Liang J, Inoue A, Ikuta T, Xia R, Wang N, Kawakami K, Xu Z, Qian Y, Zhu X, Zhang A, Guo C, Huang Z, He Y 10.1038/S41467-023-36575-0 2023-02-15 Yes
MTLR motilin Motilin A Human Cryo-EM 8IBU 8IBU_refined 3.5 R Active 100 66 Gq/11 αq - 60 BRIL scFv16 erythromycin
small-molecule Agonist motilin peptide No No You C, Zhang Y, Xu Y, Xu P, Li Z, Li H, Huang S, Chen Z, Li J, Xu HE, Jiang Y 10.1126/SCIADV.ADE9020 2023-04-12 Yes
CML1 chemerin Chemerin receptor A Human Cryo-EM 7YKD - 2.8 A Active 100 76 Gi/o αi1 - 61 - scFv16 chemerin C-terminal peptide
peptide Agonist chemerin C-terminal peptide, chemerin, 18R-HEPE, resolvin E1, EPA peptide No No Wang J, Chen G, Liao Q, Lyu W, Liu A, Zhu L, Du Y, Ye RD 10.1073/PNAS.2214324120 2023-04-19 Yes
FFAR4 FFA4 Free fatty acid A Human Cryo-EM 8IYS - 3.0 R Active 100 82 Gq/11 αq - 99 - scFv16 TUG-891
small-molecule Agonist linoleic acid, oleic acid, α-linolenic acid, myristic acid small-molecule No No Yin H, Inoue A, Ma Z, Zhu X, Xia R, Xu Z, Wang N, Duan Y, Zhang A, Guo C, He Y 10.1038/S41422-023-00835-X 2023-06-21 Yes
NTR1 NTS1 Neurotensin A Human Cryo-EM 8JPF - 3.0 R Active 79 71 - - - - - - JMV431
CHEMBL4576388
peptide
small-molecule		 Agonist
PAM		 neuromedin N, large neurotensin, neurotensin, large neuromedin N peptide No No Duan J, Liu H, Zhao F, Yuan Q, Ji Y, Cai X, He X, Li X, Li J, Wu K, Gao T, Zhu S, Lin S, Wang MW, Cheng X, Yin W, Jiang Y, Yang D, Xu HE 10.1038/S41586-023-06395-9 2023-08-09 Yes
OPSD Rhodopsin Opsins A Japanese flying squid X-ray 3AYN - 2.7 B Inactive 17 77 - - - - - - Retinal (9-cis)
small-molecule Inverse agonist - - No No - - 2011-08-17 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 4LDL 4LDL_refined 3.1 A Active 99 69 - - - - T4-Lysozyme Nanobody hydroxybenzylisoproterenol
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ small-molecule No No - - 2013-09-25 Yes
US28 US28 Unclassified A strain AD169 X-ray 4XT1 - 2.9 A Active 100 82 - - - - - Nanobody CX3CL1
peptide Agonist (partial) - - No No Burg JS, Ingram JR, Venkatakrishnan AJ, Jude KM, Dukkipati A, Feinberg EN, Angelini A, Waghray D, Dror RO, Ploegh HL, Garcia KC 10.1126/SCIENCE.AAA5026 2015-03-04 Yes
AA1R A1 Adenosine A Human X-ray 5UEN 5UEN_refined 3.2 B Inactive 1 91 - - - - BRIL - DU172
small-molecule Antagonist adenosine small-molecule No No Glukhova A, Thal DM, Nguyen AT, Vecchio EA, Jorg M, Scammells PJ, May LT, Sexton PM, Christopoulos A 10.1016/j.cell.2017.01.042 2017-03-01 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 5X7D 5X7D_refined 2.7 A Inactive 0 68 - - - - T4-Lysozyme - 4-carbamoyl-N-[(2R)-2-cyclohexyl-2-phenylacetyl]-L-phenylalanyl-3-bromo-N-methyl-L-phenylalaninamide
Carazolol
small-molecule
small-molecule		 Allosteric antagonist
Antagonist		 noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ small-molecule No No Liu X, Ahn S, Kahsai AW, Meng KC, Latorraca NR, Pani B, Venkatakrishnan AJ, Masoudi A, Weis WI, Dror RO, Chen X, Lefkowitz RJ, Kobilka BK 10.1038/NATURE23652 2017-08-16 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 6FK9 6FK9_refined 2.6 A Active 98 94 - - - - - - (2~{S})-3-methyl-2-phenyl-1-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-yl-butan-1-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
5HT2B 5-HT2B 5-Hydroxytryptamine A Human X-ray 6DRZ 6DRZ_refined 3.1 A Intermediate 44 61 - - - - BRIL - methysergide
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
EDNRB ETB Endothelin A Human X-ray 6IGK 6IGK_refined 2.0 A Inactive 4 70 - - - - T4-Lysozyme - endothelin-3
peptide Agonist endothelin-1, endothelin-2, endothelin-3 peptide No No Shihoya W, Izume T, Inoue A, Yamashita K, Kadji FMN, Hirata K, Aoki J, Nishizawa T, Nureki O 10.1038/S41467-018-07094-0 2018-11-21 Yes
MTR1A MT1 Melatonin A Human X-ray 6ME2 6ME2_refined 2.8 A Inactive 1 83 - - - - GlgA glycogen synthase - ramelteon
small-molecule Agonist melatonin small-molecule No No - 10.1038/S41586-019-1141-3 2019-04-24 Yes
OPSD Rhodopsin Opsins A Bovine Cryo-EM 6OY9 - 3.9 R Active 100 94 Gi/o αt1 - 64 - - Retinal (all-trans)
small-molecule Agonist - - No No - 10.1016/J.MOLCEL.2019.06.007 2019-07-24 Yes
ACM5 M5 Acetylcholine (muscarinic) A Human X-ray 6OL9 6OL9_refined 2.5 A Inactive 2 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
CNR2 CB2 Cannabinoid A Human X-ray 6KPC 6KPC_refined 3.2 A Inactive 11 79 - - - - T4-Lysozyme - AM12033
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
GLP1R GLP-1 Glucagon B1 Human X-ray 6LN2 6LN2_refined 3.2 A Inactive 0 83 - - - - - Fab7F38 light chain
Fab7F38 heavy chain		 PF-06372222
small-molecule NAM glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide peptide No No Wu F, Yang L, Hang K, Laursen M, Wu L, Han GW, Ren Q, Roed NK, Lin G, Hanson MA, Jiang H, Wang MW, Reedtz-Runge S, Song G, Stevens RC 10.1038/S41467-020-14934-5 2020-03-18 Yes
GABR1 GABAB1 GABAB C Human Cryo-EM 6W2Y - 3.2 B Inactive - 69 - - - - - - CGP55845
1-Stearoyl-2-oleoyl-sn-glycero-3-phosphoethanolamine
small-molecule
small-molecule		 Inverse agonist
NAM		 GABA small-molecule No No - - 2020-07-01 Yes
GNRHR GnRH1 Gonadotrophin-releasing hormone A Human X-ray 7BR3 7BR3_refined 2.8 A Inactive 35 84 - - - - GlgA glycogen synthase - elagolix
small-molecule Antagonist GnRH II, GnRH I peptide No No Yan W, Cheng L, Wang W, Wu C, Yang X, Du X, Ma L, Qi S, Wei Y, Lu Z, Yang S, Shao Z 10.1038/S41467-020-19109-W 2020-10-07 Yes
ADRB2 β2 Adrenoceptors A Human Cryo-EM 7DHI - 3.3 R Active 100 70 Gs αs - 55 - Nanobody-35 levosalbutamol
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ small-molecule No No - - 2020-12-16 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, (-)-noradrenaline, 5-hydroxytryptamine, dopamine 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 7CX4 7CX4_refined 2.9 R Active 100 74 Gs αs - 58 - Nanobody-35 evatanepag
small-molecule Agonist PGE2, PGF2α, thromboxane A2, PGI2, PGE1, PGD2 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
OPSD Rhodopsin Opsins A Bovine Cryo-EM 7MTB 7MTB_refined 4.0 R Active 98 93 - - - - - Fab light chain
Fab heavy chain
GRK1		 Retinal (all-trans)
small-molecule Agonist - - No No - - 2021-07-07 Yes
AA1R A1 Adenosine A Human Cryo-EM 7LD4 7LD4_refined 3.3 R Active 100 88 Gi/o αi2 - 59 - - adenosine
small-molecule Agonist adenosine small-molecule No No Draper-Joyce CJ, Bhola R, Wang J, Bhattarai A, Nguyen ATN, Cowie-Kent I, O'Sullivan K, Chia LY, Venugopal H, Valant C, Thal DM, Wootten D, Panel N, Carlsson J, Christie MJ, White PJ, Scammells P, May LT, Sexton PM, Danev R, Miao Y, Glukhova A, Imlach WL, Christopoulos A 10.1038/S41586-021-03897-2 2021-09-08 Yes
CCKAR CCK1 Cholecystokinin A Human X-ray 7F8U 7F8U_refined 2.8 A Inactive 1 65 - - - - T4-Lysozyme - lintitript
small-molecule Antagonist desulfated cholecystokinin-8, CCK-33, CCK-8, CCK-58, CCK-4, CCK-39, gastrin-17 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
GP158 GPR158 C Orphans C Human Cryo-EM 7SHF 7SHF_refined 3.4 B Inactive - 23 - - - - - - Apo (no ligand)
none Apo (no ligand) - - No No Patil DN, Singh S, Laboute T, Strutzenberg TS, Qiu X, Wu D, Novick SJ, Robinson CV, Griffin PR, Hunt JF, Izard T, Singh AK, Martemyanov KA 10.1126/SCIENCE.ABL4732 2021-12-01 Yes
S1PR1 S1P1 Lysophospholipid (S1P) A Human Cryo-EM 7EO4 7EO4_refined 2.9 A Active 100 74 Gi/o αi1 - 43 - scFv16 siponimod
small-molecule Agonist sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate 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
NPY1R Y1 Neuropeptide Y A Human Cryo-EM 7VGX 7VGX_refined 3.2 R Active 100 73 Gi/o αi1 - 63 - scFv16 neuropeptide Y
peptide Agonist pancreatic polypeptide, neuropeptide Y, peptide YY peptide No No Park C, Kim J, Ko SB, Choi YK, Jeong H, Woo H, Kang H, Bang I, Kim SA, Yoon TY, Seok C, Im W, Choi HJ 10.1038/S41467-022-28510-6 2022-02-23 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
AGRG1 ADGRG1 ADGRG B2 Human Cryo-EM 7SF8 - 2.7 A Active - 37 G12/13 α13 Gi2-mini-G13 chimera 56 - - Apo (no ligand)
none Apo (no ligand) - - No No - - 2022-04-27 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
GALR2 GAL2 Galanin A Human Cryo-EM 7XJL 7XJL_refined 3.5 F Active 100 72 Gq/11 αq - 58 - scFv16 Spexin
small-molecule Agonist galanin-like peptide, spexin-1, galanin peptide No No Jiang W, Zheng S 10.1073/PNAS.2121465119 2022-06-29 Yes
SSR2 SST2 Somatostatin A Human Cryo-EM 7WJ5 7WJ5_refined 3.7 R Active 100 76 Gi/o αi1 - 60 BRIL scFv16 SOMATOSTATIN
protein Agonist SRIF-14, CST-17, cortistatin-14, SRIF-28 peptide No No Heo Y, Yoon E, Jeon YE, Yun JH, Ishimoto N, Woo H, Park SY, Song JJ, Lee W 10.7554/ELIFE.76823 2022-07-13 Yes
TSHR TSH Glycoprotein hormone A Human Cryo-EM 7XW7 7XW7_refined 5.5 R Inactive 15 74 - - - - - - K1-70 scFv heavy chain
K1-70 scFv light chain
protein
protein		 Antagonist 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
CRFR2 CRF2 Corticotropin-releasing factor B1 Human Cryo-EM 7TRY - 3.7 P Active 100 79 Gq/11 α11 - 62 - - Urocortin
peptide Agonist urocortin 2, corticotrophin-releasing hormone, urocortin 3, 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
GPR88 GPR88 A orphans A Human Cryo-EM 7WZ4 - 3.0 R Active 100 61 Gi/o αi1 - 61 - scFv16 Apo (no ligand)
none Apo (no ligand) - - No No Chen G, Xu J, Inoue A, Schmidt MF, Bai C, Lu Q, Gmeiner P, Liu Z, Du Y 10.1038/S41467-022-30081-5 2022-10-26 Yes
MRGX1 MRGPRX1 A orphans A Human Cryo-EM 8DWG - 2.7 R Active 100 77 Gq/11 αq Gs-mini-Gq chimera 57 - scFv16 Proenkephalin-A
CHEMBL5177388
peptide
small-molecule		 Agonist
PAM		 bovine adrenal medulla peptide 8-22 peptide No No - - 2022-11-02 Yes
RL3R2 RXFP4 Relaxin family peptide A Human Cryo-EM 7YK7 7YK7_refined 2.8 R Active 100 75 Gi/o αi2 - 61 - scFv16 DC591053
small-molecule Agonist relaxin-3, INSL5, relaxin-3 (B chain) peptide No No Chen Y, Zhou Q, Wang J, Xu Y, Wang Y, Yan J, Wang Y, Zhu Q, Zhao F, Li C, Chen CW, Cai X, Bathgate RAD, Shen C, Eric Xu H, Yang D, Liu H, Wang MW 10.1038/S41467-023-36182-Z 2023-03-01 Yes
AA2AR A2A Adenosine A Human MicroED 8FYN 8FYN_refined 2.0 A Inactive 1 72 - - - - BRIL - ZM-241385
small-molecule Antagonist adenosine small-molecule No No - 10.1038/S41467-023-36733-4 2023-03-08 Yes
FFAR4 FFA4 Free fatty acid A Human Cryo-EM 8ID6 - 2.8 R Active 100 80 Gi/o αi1 - 64 - scFv16 oleic acid
small-molecule Agonist linoleic acid, oleic acid, α-linolenic acid, myristic acid small-molecule No No - 10.1126/SCIENCE.ADD6220 2023-03-15 Yes
MTLR motilin Motilin A Human Cryo-EM 8IBV 8IBV_refined 3.2 R Active 100 68 Gq/11 αq - 60 BRIL scFv16 motilin
peptide Agonist motilin peptide No No You C, Zhang Y, Xu Y, Xu P, Li Z, Li H, Huang S, Chen Z, Li J, Xu HE, Jiang Y 10.1126/SCIADV.ADE9020 2023-04-12 Yes
AGRE5 ADGRE5 ADGRE B2 Human Cryo-EM 7YDM - 2.9 R Active - 33 Gq/11 αq Mini-Gq 60 - Nanobody-35 Apo (no ligand)
none Apo (no ligand) - - No No - - 2023-07-12 Yes
CALCR CT Calcitonin B1 Human Cryo-EM 8F2B - 2.0 R Active 100 78 Gs αs - 58 - Nanobody-35
RAMP3		 Pramlintide analogue San45
peptide Agonist β-CGRP, α-CGRP, calcitonin, calcitonin (salmon), amylin, adrenomedullin, adrenomedullin 2/intermedin peptide No No Cao J, Belousoff MJ, Gerrard E, Danev R, Fletcher MM, Dal Maso E, Schreuder H, Lorenz K, Evers A, Tiwari G, Besenius M, Li Z, Johnson RM, Wootten D, Sexton PM 10.1038/S41589-023-01393-4 2023-08-02 Yes
TAA7F TAAR7F A orphans A Mouse Cryo-EM 8PM2 - 2.9 R Active 100 73 Gs αs - 58 - Nanobody-35 N,N-Dimethylcyclohexylamine
small-molecule Agonist - - No No Gusach A, Lee Y, Khoshgrudi AN, Mukhaleva E, Ma N, Koers EJ, Chen Q, Edwards PC, Huang F, Kim J, Mancia F, Verprintsev DB, Vaidehi N, Weyand SN, Tate CG 10.1101/2023.07.07.547762 2023-08-09 Yes
AA2AR A2A Adenosine A Human X-ray 3PWH 3PWH_refined 3.3 A Inactive 1 71 - - - - - - ZM-241385
small-molecule Antagonist adenosine small-molecule No No - 10.1016/J.STR.2011.06.014 2011-09-07 Yes
SMO SMO Frizzled F Human X-ray 4JKV 4JKV_refined 2.5 A Inactive 0 44 - - - - BRIL - taladegib
small-molecule Antagonist - - No No Wang C, Wu H, Katritch V, Han GW, Huang XP, Liu W, Siu FY, Roth BL, Cherezov V, Stevens RC 10.1038/NATURE12167 2013-04-24 Yes
LPAR1 LPA1 Lysophospholipid (LPA) A Human X-ray 4Z36 4Z36_refined 2.9 A Inactive 1 79 - - - - BRIL - ONO-3080573
small-molecule Antagonist 1-O-Oleoyl-D-glycerol 3-phosphoric acid small-molecule No No Chrencik JE, Roth CB, Terakado M, Kurata H, Omi R, Kihara Y, Warshaviak D, Nakade S, Asmar-Rovira G, Mileni M, Mizuno H, Griffith MT, Rodgers C, Han GW, Velasquez J, Chun J, Stevens RC, Hanson MA 10.1016/J.CELL.2015.06.002 2015-06-03 Yes
SMO SMO Frizzled F Human X-ray 5L7D 5L7D_refined 3.2 B Inactive 4 59 - - - - BRIL - - - - - - No No Byrne EFX, Sircar R, Miller PS, Hedger G, Luchetti G, Nachtergaele S, Tully MD, Mydock-McGrane L, Covey DF, Rambo RP, Sansom MSP, Newstead S, Rohatgi R, Siebold C 10.1038/NATURE18934 2016-07-20 Yes
AA2AR A2A Adenosine A Human X-ray 5MZJ 5MZJ_refined 2.0 A Inactive 1 71 - - - - BRIL - theophylline
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
AA2AR A2A Adenosine A Human X-ray 5OLG 5OLG_refined 1.9 A Inactive 1 72 - - - - BRIL - ZM-241385
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
FFAR1 FFA1 Free fatty acid A Human X-ray 5KW2 5KW2_refined 2.8 A Intermediate 44 82 - - - - T4-Lysozyme - (3~{S})-3-cyclopropyl-3-[2-[1-[2-[2,2-dimethylpropyl-(6-methylpyridin-2-yl)carbamoyl]-5-methoxy-phenyl]piperidin-4-yl]-1-benzofuran-6-yl]propanoic acid
small-molecule Allosteric agonist oleic acid, docosahexaenoic acid, α-linolenic acid, myristic acid small-molecule No No Ho JD, Chau B, Rodgers L, Lu F, Wilbur KL, Otto KA, Chen Y, Song M, Riley JP, Yang HC, Reynolds NA, Kahl SD, Lewis AP, Groshong C, Madsen RE, Conners K, Lineswala JP, Gheyi T, Saflor MD, Lee MR, Benach J, Baker KA, Montrose-Rafizadeh C, Genin MJ, Miller AR, Hamdouchi C 10.1038/S41467-017-01240-W 2018-05-02 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 6MXT 6MXT_refined 3.0 A Active 98 69 - - - - T4-Lysozyme Nanobody-71 salmeterol
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ small-molecule No No Masureel M, Zou Y, Picard LP, van der Westhuizen E, Mahoney JP, Rodrigues JPGLM, Mildorf TJ, Dror RO, Shaw DE, Bouvier M, Pardon E, Steyaert J, Sunahara RK, Weis WI, Zhang C, Kobilka BK 10.1038/s41589-018-0145-x 2018-11-14 Yes
5HT2A 5-HT2A 5-Hydroxytryptamine A Human X-ray 6A93 6A93_refined 3.0 A Inactive 1 60 - - - - BRIL - risperidone
small-molecule Antagonist 5-hydroxytryptamine, tryptamine small-molecule No No - 10.1038/S41594-018-0180-Z 2019-02-13 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 neuromedin N, large neurotensin, neurotensin, large neuromedin N peptide No No - 10.1038/S41586-019-1337-6 2019-07-10 Yes
OX1R OX1 Orexin A Human X-ray 6TOD - 2.1 A Inactive 1 71 - - - - - - EMPA
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
FPR2 FPR2/ALX Formylpeptide A Human Cryo-EM 6OMM 6OMM_refined 3.2 R Active 100 85 Gi/o αi1 - 61 - - CHEMBL552527
protein Agonist resolvin D1, serum amyloid A, 15-deoxy-LXA4, LTC4, LL-37, humanin, LTD4, aspirin triggered lipoxin A4, annexin I, aspirin-triggered resolvin D1, fMet-Leu-Phe, PrP106-126, LXA4 peptide No No Zhuang Y, Liu H, Edward Zhou X, Kumar Verma R, de Waal PW, Jang W, Xu TH, Wang L, Meng X, Zhao G, Kang Y, Melcher K, Fan H, Lambert NA, Eric Xu H, Zhang C 10.1038/S41467-020-14728-9 2020-02-26 Yes
GABR2 GABAB2 GABAB C Human Cryo-EM 6WIV - 3.3 B Inactive - 71 - - - - - - [(2R)-3-[(Z)-icos-11-enoyl]oxy-2-[(Z)-octadec-9-enoyl]oxypropyl] 2-(trimethylazaniumyl)ethylphosphate
(2R)-3-{[(S)-(2-aminoethoxy)(hydroxy)phosphoryl]oxy}-2-{[(9Z)-octadec-9-enoyl]oxy}propyl(5Z,8Z,11Z,14Z)-icosa-5,8,11,14-tetraenoate
small-molecule
small-molecule		 NAM - - No No Park J, Fu Z, Frangaj A, Liu J, Mosyak L, Shen T, Slavkovich VN, Ray KM, Taura J, Cao B, Geng Y, Zuo H, Kou Y, Grassucci R, Chen S, Liu Z, Lin X, Williams JP, Rice WJ, Eng ET, Huang RK, Soni RK, Kloss B, Yu Z, Javitch JA, Hendrickson WA, Slesinger PA, Quick M, Graziano J, Yu H, Fiehn O, Clarke OB, Frank J, Fan QR 10.1038/S41586-020-2452-0 2020-07-01 Yes
GABR2 GABAB2 GABAB C Human Cryo-EM 7CA5 - 7.6 B Inactive - 70 - - - - - - Apo (no ligand)
none Apo (no ligand) - - No No Kim Y, Jeong E, Jeong JH, Kim Y, Cho Y 10.1016/J.JMB.2020.09.023 2020-11-11 Yes
NTR1 NTS1 Neurotensin A Rat X-ray 6Z4S - 2.7 A Inactive 3 77 - - - - DARPin D12 - meclinertant
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 Cryo-EM 7EPD 7EPD_refined 3.9 A Inactive - 89 - - - - - - Apo (no ligand)
none Apo (no ligand) 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
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 7KI0 - 2.5 R Active 100 83 Gs αs - 53 - Nanobody-35 semaglutide
peptide Agonist glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide peptide No No Zhang X, Belousoff MJ, Liang YL, Danev R, Sexton PM, Wootten D 10.1016/J.CELREP.2021.109374 2021-08-04 Yes
MC4R MC4 Melanocortin A Human Cryo-EM 7F54 - 3.0 R Active 100 82 Gs αs - 58 - Nanobody-35 afamelanotide
peptide Agonist agouti-related protein, β-MSH, α-MSH, γ-MSH, ACTH 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
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 7S1M 7S1M_refined 2.4 R Active 100 82 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 Cary BP, Deganutti G, Zhao P, Truong TT, Piper SJ, Liu X, Belousoff MJ, Danev R, Sexton PM, Wootten D, Gellman SH 10.1038/S41589-021-00945-W 2022-01-05 Yes
CCR1 CCR1 Chemokine A Human Cryo-EM 7VL8 7VL8_refined 2.9 R Active 100 80 Gi/o αi1 - 62 - scFv16 Apo (no ligand)
none Apo (no ligand) CCL8, CCL13, CCL14, CCL16, CCL5, CCL7, CCL4, CCL23, CCL15, CCL3 peptide No No Shao Z, Shen Q, Yao B, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Ma H, Chen ZH, Xu HE, Ying S, Zhang Y, Shen H 10.1038/S41589-021-00918-Z 2022-03-23 Yes
GIPR GIP Glucagon B1 Human Cryo-EM 7FIN - 3.1 R Active 100 82 Gs αs - 59 - Nanobody-35 Peptide-20
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 2022-02-23 Yes
AGRD1 ADGRD1 ADGRD B2 Human Cryo-EM 7WU2 - 2.8 R Active - 32 Gs αs Mini-Gs 53 - Nanobody-35 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
AGRD1 ADGRD1 ADGRD B2 Human Cryo-EM 7EPT - 3.0 R Active - 31 Gs αs - 54 - Nanobody-35 - - - - - No No Ping YQ, Xiao P, Yang F, Zhao RJ, Guo SC, Yan X, Wu X, Zhang C, Lu Y, Zhao F, Zhou F, Xi YT, Yin W, Liu FZ, He DF, Zhang DL, Zhu ZL, Jiang Y, Du L, Feng SQ, Schoneberg T, Liebscher I, Xu HE, Sun JP 10.1038/S41586-022-04619-Y 2022-05-11 Yes
DRD1 D1 Dopamine A Human Cryo-EM 7F0T - 3.1 F Active 100 63 Gs αs - 58 - Nanobody-35 dopamine
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, 5-hydroxytryptamine, dopamine 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 55 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
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, cortistatin-14, SRIF-28 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 15 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 7SRR - 2.9 R Active 100 57 Gq/11 αq Gi2-mini-Gq chimera 58 - scFv16 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
ADA2A α2A Adrenoceptors A Human Cryo-EM 7W7E - 3.4 R Active 100 56 Gi/o αo - 59 - scFv16 5-(3-Bicyclo[4.2.0]octa-1,3,5-trienyl)-1,2,3,6-tetrahydropyridine
small-molecule Agonist (-)-adrenaline, (-)-noradrenaline small-molecule No No Fink EA, Xu J, Hubner H, Braz JM, Seemann P, Avet C, Craik V, Weikert D, Schmidt MF, Webb CM, Tolmachova NA, Moroz YS, Huang XP, Kalyanaraman C, Gahbauer S, Chen G, Liu Z, Jacobson MP, Irwin JJ, Bouvier M, Du Y, Shoichet BK, Basbaum AI, Gmeiner P 10.1126/SCIENCE.ABN7065 2022-09-28 Yes
AGRL3 ADGRL3 ADGRL B2 Mouse Cryo-EM 7X10 - 2.9 R Active - 17 G12/13 α12 - 55 - scFv16 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 2022-11-09 Yes
VIPR1 VPAC1 VIP and PACAP B1 Human Cryo-EM 8E3Z 8E3Z_refined 2.7 R Active 100 81 Gs αs - 55 - Nanobody-35 Vasoactive intestinal polypeptide
small-molecule Agonist VIP, PACAP-27, secretin, PHI, PHM, GHRH, PACAP-38 peptide No No Piper SJ, Deganutti G, Lu J, Zhao P, Liang YL, Lu Y, Fletcher MM, Hossain MA, Christopoulos A, Reynolds CA, Danev R, Sexton PM, Wootten D 10.1038/S41467-022-34629-3 2022-11-23 Yes
C5AR1 C5a1 Complement peptide A Human Cryo-EM 7Y66 - 2.9 D Active 100 80 Gi/o αi1 - 63 - scFv16 BM213
peptide Agonist C3a, C5a, ribosomal protein S19, C5a des-Arg 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
GPR21 GPR21 A orphans A Human Cryo-EM 8HMV 8HMV_refined 2.9 A Active 100 79 Gs αs - 58 - Nanobody-35 Apo (no ligand)
none Apo (no ligand) - - No No - 10.1002/MCO2.205 2023-03-01 Yes
HCAR2 HCA2 Hydroxycarboxylic acid A Human Cryo-EM 7XK2 7XK2_refined 3.1 R Active 100 78 Gi/o αi1 - 63 - scFv16 MK 6892
small-molecule Agonist 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 2023-02-22 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, hemokinin 1, substance P, neurokinin A, neuropeptide γ, neuropeptide K 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
FFAR4 FFA4 Free fatty acid A Human Cryo-EM 8H4K - 3.1 R Active 100 83 Gq/11 αq Mini-Gq 60 - Nanobody-35 GW9508
small-molecule Agonist linoleic acid, oleic acid, α-linolenic acid, myristic acid small-molecule No No Yin H, Inoue A, Ma Z, Zhu X, Xia R, Xu Z, Wang N, Duan Y, Zhang A, Guo C, He Y 10.1038/S41422-023-00835-X 2023-06-21 Yes
GRM2 mGlu2 Metabotropic glutamate C Human Cryo-EM 8JCZ - 3.0 2 Inactive - 87 - - - - - - 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 4A4M 4A4M_refined 3.3 A Active 100 94 Gi/o αt1 Only H5 3 - - Retinal (all-trans)
small-molecule Agonist - - No No - 10.1073/PNAS.1114089108 2012-01-25 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 4GPO 4GPO_refined 3.5 B Inactive 0 58 - - - - - - Apo (no ligand)
none Apo (no ligand) - - No No Huang J, Chen S, Zhang JJ, Huang XY 10.1038/NSMB.2504 2013-02-27 Yes
SMO SMO Frizzled F Human X-ray 4O9R 4O9R_refined 3.2 A Inactive 11 42 - - - - BRIL - cyclopamine
small-molecule Antagonist - - No No Weierstall U, James D, Wang C, White TA, Wang D, Liu W, Spence JC, Bruce Doak R, Nelson G, Fromme P, Fromme R, Grotjohann I, Kupitz C, Zatsepin NA, Liu H, Basu S, Wacker D, Han GW, Katritch V, Boutet S, Messerschmidt M, Williams GJ, Koglin JE, Marvin Seibert M, Klinker M, Gati C, Shoeman RL, Barty A, Chapman HN, Kirian RA, Beyerlein KR, Stevens RC, Li D, Shah ST, Howe N, Caffrey M, Cherezov V 10.1038/NCOMMS4309 2014-03-05 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 5EN0 5EN0_refined 2.8 A Active 100 94 Gi/o αgust Only H5 3 - - Retinal (all-trans)
small-molecule Agonist - - No No - - 2016-08-10 Yes
PAR2 PAR2 Proteinase-activated A Human X-ray 5NDD 5NDD_refined 2.8 A Intermediate 44 74 - - - - BRIL - AZ8838
small-molecule Antagonist - - No Yes 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
AA2AR A2A Adenosine A Human X-ray 5NM4 - 1.7 A Inactive 1 73 - - - - 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
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
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 6H7M 6H7M_refined 2.8 A Active 99 60 - - - - Thioredoxin 1 Camelid antibody fragment Nb6B9 levosalbutamol
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 6N51 6N51_refined 4.0 B Intermediate - 65 - - - - - Nanobody-43 quisqualate
small-molecule Agonist L-glutamic acid small-molecule No No - 10.1038/S41586-019-0881-4 2019-01-23 Yes
CCR7 CCR7 Chemokine A Human X-ray 6QZH 6QZH_refined 2.1 A Inactive 5 71 - - - - Sialidase NanA - SCHEMBL13407377
small-molecule Allosteric antagonist CCL21, CCL19 peptide No No - 10.1016/J.CELL.2019.07.028 2019-09-04 Yes
OPRD δ Opioid A Human X-ray 6PT3 6PT3_refined 3.3 A Active 65 78 - - - - BRIL - DPI-287
small-molecule Agonist dynorphin A-(1-8), [Met]enkephalin, endomorphin-1, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin B, α-neoendorphin 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
OPSD Rhodopsin Opsins A Bovine X-ray 6NWE 6NWE_refined 2.7 A Active 100 94 Gi/o αt1 Only H5 3 - - B-Octylglucoside
small-molecule unknown - - No No - - 2020-02-12 Yes
CALRL calcitonin-like Calcitonin B1 Human Cryo-EM 6UUS 6UUS_refined 2.4 R Active 100 74 Gs αs - 48 - Nanobody-35
RAMP3		 Adrenomedullin
peptide Agonist - - No No Liang YL, Belousoff MJ, Fletcher MM, Zhang X, Khoshouei M, Deganutti G, Koole C, Furness SGB, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Danev R, Wootten D, Sexton PM 10.1021/ACSPTSCI.9B00080 2020-04-01 Yes
GPBAR GPBA Bile acid A Human Cryo-EM 7BW0 7BW0_refined 3.9 R Active 100 85 Gs αs - 57 BRIL Nanobody-35 - - - deoxycholic acid, chenodeoxycholic acid, lithocholic acid, cholic acid small-molecule No No Chen G, Wang X, Ge Y, Ma L, Chen Q, Liu H, Du Y, Ye RD, Hu H, Ren R 10.1038/S41392-020-00262-Z 2020-09-02 Yes
GABR2 GABAB2 GABAB C Human Cryo-EM 7CA3 - 4.5 B Active - 72 - - - - - - BHFF
small-molecule PAM - - No No Kim Y, Jeong E, Jeong JH, Kim Y, Cho Y 10.1016/J.JMB.2020.09.023 2020-11-11 Yes
OX2R OX2 Orexin A Human Cryo-EM 7L1U - 3.2 R Active 100 63 Gs αs Engineered G alpha 58 - scFv16 Orexin-A
peptide Agonist orexin-B, orexin-A 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
5HT1A 5-HT1A 5-Hydroxytryptamine A Human Cryo-EM 7E2Z - 3.1 R Active 100 66 Gi/o αi1 - 62 - - aripiprazole
small-molecule Agonist (partial) 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
OPSD Rhodopsin Opsins A Bovine Cryo-EM 7MT9 7MT9_refined 7.0 R Active 98 93 - - - - - GRK1 Retinal (all-trans)
small-molecule Agonist - - No No - - 2021-07-07 Yes
CCKAR CCK1 Cholecystokinin A Human Cryo-EM 7EZK - 3.1 D Active 100 69 Gs αs - 58 - - CCK-8
peptide Agonist desulfated cholecystokinin-8, CCK-33, CCK-8, CCK-58, CCK-4, CCK-39, gastrin-17 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
MC4R MC4 Melanocortin A Human Cryo-EM 7F53 - 3.0 R Active 100 82 Gs αs - 58 - Nanobody-35 α-MSH
peptide Agonist agouti-related protein, β-MSH, α-MSH, γ-MSH, ACTH 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
S1PR1 S1P1 Lysophospholipid (S1P) A Human Cryo-EM 7EW7 - 3.3 D Active 100 75 Gi/o αi1 - 64 - scFv16 SEW2871
small-molecule Agonist sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate 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
AA2AR A2A Adenosine A Human X-ray 7PYR 7PYR_refined 2.6 A Inactive 1 72 - - - - BRIL - Preladenant conjugate PSB-2115
small-molecule Antagonist adenosine small-molecule No No Claff T, Klapschinski TA, Tiruttani Subhramanyam UK, Vaassen VJ, Schlegel JG, Vielmuth C, Voss JH, Labahn J, Muller CE 10.1002/ANIE.202115545 2022-03-02 Yes
GRM3 mGlu3 Metabotropic glutamate C Human Cryo-EM 7WI8 7WI8_refined 4.2 A Inactive - 82 - - - - - - LY341495
small-molecule Antagonist L-glutamic acid, NAAG small-molecule No No - - 2022-03-16 Yes
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 7RGP - 2.9 R Active 100 82 Gs αs Engineered G alpha 55 - scFv16
Nanobody-35		 tirzepatide
peptide Agonist glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide 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
HRH2 H2 Histamine A Human Cryo-EM 7UL3 7UL3_refined 3.0 A Inactive 4 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
5HT4R 5-HT4 5-Hydroxytryptamine A Human Cryo-EM 7XT9 - 3.2 R Active 100 76 Gs αs - 60 BRIL - 5-hydroxytryptamine
small-molecule Agonist 5-hydroxytryptamine small-molecule No No - - 2022-07-27 Yes
ADRB1 β1 Adrenoceptors A Wild turkey Cryo-EM 8DCR - 2.6 R Active 100 57 Gs αs - 51 T4-Lysozyme Nanobody-35 Dobutamine
small-molecule Agonist - - No No Su M, Paknejad N, Zhu L, Wang J, Do HN, Miao Y, Liu W, Hite RK, Huang XY 10.1038/S41467-022-31823-1 2022-07-27 Yes
PTH1R PTH1 Parathyroid hormone B1 Human Cryo-EM 7VVK - 3.3 R Active 100 56 Gs αs - 58 - Nanobody-35 teriparatide
peptide Agonist PTH, PTHrP-(1-36), TIP39, PTHrP 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
S1PR1 S1P1 Lysophospholipid (S1P) A Human Cryo-EM 7VIG 7VIG_refined 2.9 F Active 100 73 Gi/o αi1 - 63 - scFv16 icanbelimod
small-molecule Agonist sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate 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 7Y26 7Y26_refined 3.3 E Active 100 73 Gq/11 αq Mini-Gq 60 - scFv16 Octreotide
peptide Agonist SRIF-14, CST-17, cortistatin-14, SRIF-28 peptide No No Chen S, Teng X, Zheng S 10.1038/S41589-022-01130-3 2022-10-19 Yes
ACM3 M3 Acetylcholine (muscarinic) A Human Cryo-EM 8EA0 8EA0_refined 2.6 A Active 99 48 - - - - - - iperoxo
small-molecule Agonist acetylcholine small-molecule No No Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL 10.1038/S41586-022-05489-0 2022-11-30 Yes
PTH1R PTH1 Parathyroid hormone B1 Human Cryo-EM 8HAF - 3.3 R Active 100 62 Gs αs - 60 - Nanobody-35 PTHrP-(1-36)
peptide Agonist PTH, PTHrP-(1-36), TIP39, PTHrP peptide No No Zhao LH, Yuan QN, Dai AT, He XH, Chen CW, Zhang C, Xu YW, Zhou Y, Wang MW, Yang DH, Xu HE 10.1038/S41401-022-01032-Z 2022-12-21 Yes
GPR21 GPR21 A orphans A Human Cryo-EM 8HIX - 3.1 R Active 100 81 Gs αs Mini-Gs 61 - Nanobody-35 Apo (no ligand)
none Apo (no ligand) - - No No - 10.1038/S41467-023-35882-W 2023-03-15 Yes
GRPR BB2 Bombesin A Human Cryo-EM 7W3Z - 3.0 A Active 100 78 Gq/11 αq - 98 - scFv16 Gastrin-releasing peptide
peptide Agonist neuromedin B, gastrin releasing peptide(14-27) (human), gastrin-releasing peptide, neuromedin C, GRP-(18-27) peptide No No Peng S, Zhan Y, Zhang D, Ren L, Chen A, Chen ZF, Zhang H 10.1073/PNAS.2216230120 2023-02-22 Yes
AA2BR A2B Adenosine A Human Cryo-EM 7XY7 - 3.3 R Active 100 85 Gs αs Mini-Gs 57 BRIL - NECA
small-molecule Agonist adenosine small-molecule No No Chen Y, Zhang J, Weng Y, Xu Y, Lu W, Liu W, Liu M, Hua T, Song G 10.1126/SCIADV.ADD3709 2023-05-03 Yes
PTH1R PTH1 Parathyroid hormone B1 Human Cryo-EM 8FLT - 3.0 R Active 100 45 Gs αs - 59 - Nanobody-35 M-PTH(1-14)
peptide Agonist PTH, PTHrP-(1-36), TIP39, PTHrP 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
CALCR CT Calcitonin B1 Human Cryo-EM 8F2A - 2.2 R Active 100 78 Gs αs - 59 - Nanobody-35 Pramlintide analogue San385
peptide Agonist β-CGRP, α-CGRP, calcitonin, calcitonin (salmon), amylin, adrenomedullin, adrenomedullin 2/intermedin peptide No No Cao J, Belousoff MJ, Gerrard E, Danev R, Fletcher MM, Dal Maso E, Schreuder H, Lorenz K, Evers A, Tiwari G, Besenius M, Li Z, Johnson RM, Wootten D, Sexton PM 10.1038/S41589-023-01393-4 2023-08-02 Yes
GLR glucagon Glucagon B1 Human Cryo-EM 8JRU - 3.5 R Active 100 53 Beta Beta-arrestin-1 - 83 - scFv30
Nanobody-32		 Apo (no ligand)
none Apo (no ligand) 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
ADA1A α1A Adrenoceptors A Human Cryo-EM 8THL - 3.1 R Active 100 52 Gq/11 αq - 55 T4-Lysozyme scFv16 (-)-adrenaline
small-molecule Agonist (-)-adrenaline, (-)-noradrenaline small-molecule No No Su M, Wang J, Xiang G, Do HN, Levitz J, Miao Y, Huang XY 10.1038/S41467-023-40524-2 2023-08-16 Yes
Q9WTK1 BLT1 Leukotriene A Guinea pig X-ray 5X33 5X33_refined 3.7 A Inactive 5 78 - - - - T4-Lysozyme - BIIL 260
small-molecule Antagonist - - No No Hori T, Okuno T, Hirata K, Yamashita K, Kawano Y, Yamamoto M, Hato M, Nakamura M, Shimizu T, Yokomizo T, Miyano M, Yokoyama S 10.1038/NCHEMBIO.2547 2018-01-03 Yes
DRD2 D2 Dopamine A Human X-ray 6CM4 6CM4_refined 2.9 A Inactive 1 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 22 61 - - - - Rubredoxin - - - - - - 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-(1-36), TIP39, PTHrP 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
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 - - 2019-04-24 Yes
OPSD Rhodopsin Opsins A Bovine Cryo-EM 6OFJ 6OFJ_refined 4.5 A Inactive 22 93 - - - - - - Apo (no ligand)
none Apo (no ligand) - - No No - 10.1074/JBC.RA119.010089 2019-08-21 Yes
ADA2A α2A Adrenoceptors A Human X-ray 6KUX 6KUX_refined 2.7 A Inactive 1 57 - - - - BRIL - RSC
small-molecule Antagonist (-)-adrenaline, (-)-noradrenaline small-molecule No No - - 2019-12-04 Yes
PACR PAC1 VIP and PACAP B1 Human Cryo-EM 6P9Y - 3.0 R Active 100 55 Gs αs - 49 - Nanobody-35 [Ac-His1]PACAP-27
peptide Agonist VIP, PHV, PACAP-27, PHI, PHM, PACAP-38 peptide No No - - 2020-02-05 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 6PH7 6PH7_refined 2.9 A Active 100 94 Gi/o αt2 Only H5 3 - - Nerol
small-molecule unknown - - No No - - 2020-07-01 Yes
AGTR2 AT2 Angiotensin A Human X-ray 7C6A 7C6A_refined 3.4 A Active 99 77 - - - - BRIL IgG heavy chain
IgG light chain		 CHEMBL404594
protein Agonist angiotensin-(1-7), angiotensin II, angiotensin III peptide No No Miyagi H, Asada H, Suzuki M, Takahashi Y, Yasunaga M, Suno C, Iwata S, Saito JI 10.1038/S41598-020-68355-X 2020-07-29 Yes
SMO SMO Frizzled F Human Cryo-EM 6XBJ - 3.9 R Active 100 59 Gi/o αi1 - 61 - scFv16 Cholesterol
small-molecule Agonist - - No No Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X 10.1038/S41589-020-0646-2 2020-09-30 Yes
NTR1 NTS1 Neurotensin A Rat Cryo-EM 7L0S - 4.5 C Active 100 73 Gi/o αi1 Non-canonical conformation 95 - - neurotensin
peptide Agonist neuromedin N, neurotensin peptide No No Zhang M, Gui M, Wang ZF, Gorgulla C, Yu JJ, Wu H, Sun ZJ, Klenk C, Merklinger L, Morstein L, Hagn F, Pluckthun A, Brown A, Nasr ML, Wagner G 10.1038/S41594-020-00554-6 2021-01-06 Yes
CASR CaS Calcium-sensing C Human Cryo-EM 7DTT 7DTT_refined 3.8 A Active - 72 - - - - - - Calcium
small-molecule Agonist spermine, L-tryptophan, Ca2+, Mg2+ 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
CASR CaS Calcium-sensing C Human Cryo-EM 7M3F 7M3F_refined 2.8 B Active - 75 - - - - - - Calcium
L-tryptophan
cinacalcet
small-molecule
small-molecule
small-molecule		 Agonist
PAM
PAM		 spermine, L-tryptophan, Ca2+, Mg2+ small-molecule No No - - 2021-06-30 Yes
S1PR3 S1P3 Lysophospholipid (S1P) A Human Cryo-EM 7EW3 - 3.1 R Active 100 77 Gi/o αi1 - 64 - scFv16 Sphingosine 1-phosphate
lipid Agonist sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate small-molecule No No - - 2021-09-29 Yes
NK1R NK1 Tachykinin A Human Cryo-EM 7RMI - 3.2 R Active 100 70 Gs αs Gs-Gq chimera 49 - Nanobody-35 substance P
peptide Agonist neurokinin B, neuropeptide-γ, hemokinin 1, substance P, neurokinin A, neuropeptide K 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
GHSR ghrelin Ghrelin A Human Cryo-EM 7NA8 - 2.7 R Active 100 78 Gi/o αi1 - 61 - Antibody fragment ibutamoren
small-molecule Agonist [des-Gln14]ghrelin, ghrelin peptide No No Liu H, Sun D, Myasnikov A, Damian M, Baneres JL, Sun J, Zhang C 10.1038/S41467-021-26735-5 2021-12-15 Yes
S1PR1 S1P1 Lysophospholipid (S1P) A Human Cryo-EM 7EW0 7EW0_refined 3.4 D Active 100 71 Gi/o αi1 - 64 - scFv16 ozanimod
small-molecule Agonist sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate 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
MTR1B MT2 Melatonin A Human Cryo-EM 7VH0 7VH0_refined 3.5 A Active 100 75 Gi/o αi1 - 61 - 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
GRM3 mGlu3 Metabotropic glutamate C Human Cryo-EM 7WIH 7WIH_refined 3.7 A Active - 84 - - - - - - CHEMBL4081453
small-molecule Agonist L-glutamic acid, NAAG small-molecule No No Fang W, Yang F, Xu C, Ling S, Lin L, Zhou Y, Sun W, Wang X, Liu P, Rondard P, Shi P, Pin JP, Tian C, Liu J 10.1038/S41422-022-00623-Z 2022-03-16 Yes
AGRF1 ADGRF1 ADGRF B2 Human Cryo-EM 7WU4 - 3.4 R Active - 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 [Hyp3]bradykinin, [des-Arg10]kallidin, bradykinin, Lys-[Hyp3]-bradykinin, kallidin, [des-Arg9]bradykinin, T-kinin 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		 2-arachidonoylglycerol, anandamide 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 7SK5 7SK5_refined 4.0 A Active 95 83 - - - - - CID24 Fab heavy chain
CID24 Fab light chain
anti-Fab Nanobody		 Stromal cell-derived factor 1
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
SSR2 SST2 Somatostatin A Human Cryo-EM 7Y24 - 3.3 E Active 100 77 Gi/o αo - 60 - scFv16 Octreotide
peptide Agonist SRIF-14, CST-17, cortistatin-14, SRIF-28 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 8EF6 8EF6_refined 3.2 R Active 100 72 Gi/o αi1 - 64 - scFv16 morphine
small-molecule Agonist dynorphin A-(1-8), [Met]enkephalin, endomorphin-1, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin B, endomorphin-2 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
OPSD Rhodopsin Opsins A Bovine X-ray 7ZBE 7ZBE_refined 1.8 A Inactive 22 87 - - - - - - Retinal (11-cis)
small-molecule Inverse 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
GPR35 GPR35 A orphans A Human Cryo-EM 8H8J 8H8J_refined 3.2 C Active 100 92 G12/13 α13 - 60 - scFv16 lodoxamide
small-molecule Agonist 1-Lyso-2-oleoyl-phosphatidic acid, kynurenic acid, 2-Oleoyllysophosphatydic acid, 2-oleoyl-LPA small-molecule No No - 10.1038/S41421-022-00499-8 2023-02-08 Yes
RXFP1 RXFP1 Relaxin family peptide A Human Cryo-EM 7TMW - 3.2 R Active 100 36 Gs αs Gs fused to receptor 57 - Nanobody-35 H2 relaxin
small-molecule Agonist relaxin-3, relaxin, relaxin-1 peptide No No - - 2023-02-15 Yes
MRGX1 MRGPRX1 A orphans A Human Cryo-EM 8HJ5 8HJ5_refined 3.0 F Active 100 78 Gq/11 αq - 60 BRIL scFv16
Nanobody-35		 compound 16 [PMID: 31498617]
small-molecule Agonist bovine adrenal medulla peptide 8-22 peptide No No - - 2023-05-31 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
C5AR1 C5a1 Complement peptide A Human Cryo-EM 8HK5 8HK5_refined 3.0 A Active 100 84 Gi/o αi1 - 63 - - C5a
peptide Agonist C3a, C5a, ribosomal protein S19, C5a des-Arg 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
EDNRB ETB Endothelin A Human Cryo-EM 8IY6 - 3.1 R Active 79 66 - - - - - - ENDOTHELIN
protein Agonist endothelin-1, endothelin-2, endothelin-3 peptide No No Sano FK, Akasaka H, Shihoya W, Nureki O 10.7554/ELIFE.85821 2023-08-16 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
C5AR1 C5a1 Complement peptide A Human X-ray 5O9H 5O9H_refined 2.7 A Inactive 6 84 - - - - - - NDT9513727
small-molecule Antagonist C3a, C5a, ribosomal protein S19, C5a des-Arg peptide No No Robertson N, Rappas M, Dore AS, Brown J, Bottegoni G, Koglin M, Cansfield J, Jazayeri A, Cooke RM, Marshall FH 10.1038/NATURE25025 2018-01-10 Yes
OPRM μ Opioid A Mouse Cryo-EM 6DDF - 3.5 R Active 100 71 Gi/o αi1 - 61 - - DAMGO
peptide Agonist - - No No - - 2018-06-13 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 6IBL 6IBL_refined 2.7 A Active 99 60 - - - - Thioredoxin 1 Camelid antibody fragment Nb80 arformoterol
small-molecule Agonist - - No No - 10.1038/S41586-020-2419-1 2019-01-09 Yes
OPSD Rhodopsin Opsins A Bovine Cryo-EM 6QNO - 4.4 R Active 100 96 Gi/o αi1 - 60 - Fab antibody fragment light chain
Fab antibody fragment heavy chain		 Retinal (all-trans)
small-molecule Agonist - - No No - 10.7554/ELIFE.46041 2019-07-10 Yes
CLTR2 CysLT2 Leukotriene A Human X-ray 6RZ8 6RZ8_refined 2.7 A Intermediate 44 78 - - - - BRIL - ONO-2080365
small-molecule Antagonist LTE4, LTD4, LTC4 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
CRFR1 CRF1 Corticotropin-releasing factor B1 Human Cryo-EM 6PB0 - 3.0 R Active 100 68 Gs αs Gs-Gi1 chimera 58 - Nanobody-35 Urocortin
peptide Agonist urocortin 2, corticotrophin-releasing hormone, urocortin 1 peptide No No Ma S, Shen Q, Zhao LH, Mao C, Zhou XE, Shen DD, de Waal PW, Bi P, Li C, Jiang Y, Wang MW, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE 10.1016/J.MOLCEL.2020.01.013 2020-02-12 Yes
5HT1B 5-HT1B 5-Hydroxytryptamine A Human X-ray 7C61 7C61_refined 3.0 A Inactive 15 68 - - - - BRIL IgG heavy chain
IgG light chain		 ergotamine
small-molecule Antagonist 5-hydroxytryptamine, 5-HT-moduline, tryptamine small-molecule No No - - 2020-07-29 Yes
AA2AR A2A Adenosine A Human X-ray 6ZDR 6ZDR_refined 1.9 A Inactive 1 72 - - - - BRIL - CHEMBL2030687
small-molecule Antagonist adenosine small-molecule No Yes - - 2020-09-16 Yes
AA2AR A2A Adenosine A Human X-ray 6WQA 6WQA_refined 2.0 A Inactive 1 72 - - - - BRIL - ZM-241385
small-molecule Antagonist adenosine small-molecule No Yes Lee MY, Geiger J, Ishchenko A, Han GW, Barty A, White TA, Gati C, Batyuk A, Hunter MS, Aquila A, Boutet S, Weierstall U, Cherezov V, Liu W 10.1107/S2052252520012701 2020-11-18 Yes
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 7LCJ 7LCJ_refined 2.8 R Active 98 84 - - - - - - danuglipron
small-molecule Agonist glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide 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
DRD2 D2 Dopamine A Human Cryo-EM 7JVR - 2.8 R Active 100 61 Gi/o αi1 - 63 - scFv16 bromocriptine
small-molecule Agonist dopamine 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
S1PR3 S1P3 Lysophospholipid (S1P) A Human X-ray 7C4S 7C4S_refined 3.2 A Active 73 75 - - - - - Fab light chain
Fab heavy chain		 sphingosine 1-phosphate
small-molecule Agonist sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate small-molecule No No Maeda S, Shiimura Y, Asada H, Hirata K, Luo F, Nango E, Tanaka N, Toyomoto M, Inoue A, Aoki J, Iwata S, Hagiwara M 10.1126/SCIADV.ABF5325 2021-06-09 Yes
GRM2 mGlu2 Metabotropic glutamate C Human Cryo-EM 7MTS - 3.2 A Active - 90 Gi/o αi1 - 58 - - 2-methoxy-6-propyl-N-(2-{4-[(1H-tetrazol-5-yl)methoxy]phenyl}ethyl)thieno[2,3-d]pyrimidin-4-amine
L-glutamic acid
small-molecule
small-molecule		 Ago-PAM
Agonist		 L-glutamic acid small-molecule No No - - 2021-07-07 Yes
ACM1 M1 Acetylcholine (muscarinic) A Human X-ray 6ZG4 6ZG4_refined 2.3 A Inactive 2 62 - - - - T4-Lysozyme - Ethyl (4S)-4-[4-[(1-methylcyclobutyl)carbamoyl]piperidin-1-yl]azepane-1-carboxylate
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
GP158 GPR158 C Orphans C Human Cryo-EM 7SHE 7SHE_refined 3.4 A Inactive - 45 - - - - - - Apo (no ligand)
none Apo (no ligand) - - No No Patil DN, Singh S, Laboute T, Strutzenberg TS, Qiu X, Wu D, Novick SJ, Robinson CV, Griffin PR, Hunt JF, Izard T, Singh AK, Martemyanov KA 10.1126/SCIENCE.ABL4732 2021-12-01 Yes
S1PR1 S1P1 Lysophospholipid (S1P) A Human Cryo-EM 7EO2 7EO2_refined 2.9 A Active 100 73 Gi/o αi1 - 62 - scFv16 (S)-FTY720-phosphate
small-molecule Agonist sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate 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
FPR2 FPR2/ALX Formylpeptide A Human Cryo-EM 7T6S 7T6S_refined 3.0 R Active 100 85 Gi/o αi1 - 61 - scFv16 N-(4-chlorophenyl)-N'-[1-methyl-3-oxo-2-phenyl-5-(propan-2-yl)-2,3-dihydro-1H-pyrazol-4-yl]urea
small-molecule Agonist resolvin D1, serum amyloid A, 15-deoxy-LXA4, LTC4, LL-37, humanin, LTD4, aspirin triggered lipoxin A4, annexin I, aspirin-triggered resolvin D1, fMet-Leu-Phe, PrP106-126, LXA4 peptide No No - - 2022-03-30 Yes
CALCR CT Calcitonin B1 Human Cryo-EM 7TYO - 2.7 R Active 100 76 Gs αs - 58 - Nanobody-35 Calcitonin human
peptide Agonist β-CGRP, α-CGRP, calcitonin, calcitonin (salmon), amylin, adrenomedullin, 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
OPRM μ Opioid A Mouse Cryo-EM 7U2L - 3.2 D Active 100 71 Gi/o αi1 - 61 - scFv16 N-(5-carbamimidamidopentyl)-N-[1-(2-phenylethyl)piperidin-4-yl]propanamide
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 2022-05-04 Yes
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 7S15 7S15_refined 3.8 R Active 94 83 - - - - - - CHEMBL5191519
small-molecule Agonist glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide peptide No No Griffith DA, Edmonds DJ, Fortin JP, Kalgutkar AS, Kuzmiski JB, Loria PM, Saxena AR, Bagley SW, Buckeridge C, Curto JM, Derksen DR, Dias JM, Griffor MC, Han S, Jackson VM, Landis MS, Lettiere D, Limberakis C, Liu Y, Mathiowetz AM, Patel JC, Piotrowski DW, Price DA, Ruggeri RB, Tess DA. 10.1021/acs.jmedchem.1c01856 2022-06-08 Yes
DRD1 D1 Dopamine A Human Cryo-EM 7F24 - 4.2 F Active 100 62 Gs αs - 57 - - dopamine
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, 5-hydroxytryptamine, dopamine 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
5HT7R 5-HT7 5-Hydroxytryptamine A Human Cryo-EM 7XTC 7XTC_refined 3.2 R Active 100 57 Gs αs - 61 BRIL Nanobody-35 5-CT
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
5HT2C 5-HT2C 5-Hydroxytryptamine A Human Cryo-EM 8DPH - 3.2 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
PE2R3 EP3 Prostanoid A Human Cryo-EM 7WU9 7WU9_refined 3.4 R Active 100 70 Gi/o αi1 - 38 - scFv16 - - - PGE2, PGF2α, thromboxane A2, PGI2, PGE1, PGD2 small-molecule No No Suno R, Sugita Y, Morimoto K, Takazaki H, Tsujimoto H, Hirose M, Suno-Ikeda C, Nomura N, Hino T, Inoue A, Iwasaki K, Kato T, Iwata S, Kobayashi T 10.1016/J.CELREP.2022.111323 2022-08-17 Yes
TSHR TSH Glycoprotein hormone A Human Cryo-EM 7T9I - 2.9 R Active 100 78 Gs αs Mini-Gs 56 - Nanobody-35 Thyrotropin subunit beta
Glycoprotein hormones alpha chain
protein
protein		 Agonist TSH peptide No No Faust B, Billesbolle CB, Suomivuori CM, Singh I, Zhang K, Hoppe N, Pinto AFM, Diedrich JK, Muftuoglu Y, Szkudlinski MW, Saghatelian A, Dror RO, Cheng Y, Manglik A 10.1038/S41586-022-05159-1 2022-08-03 Yes
AA2AR A2A Adenosine A Human X-ray 5OLH 5OLH_refined 2.6 A Inactive 1 72 - - - - BRIL - vipadenant
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
Q98SW5 SMO Frizzled F African clawed frog X-ray 6D32 6D32_refined 3.8 A Active 78 58 - - - - BRIL - cyclopamine
small-molecule Agonist (partial) - - 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
CCR5 CCR5 Chemokine A Human X-ray 6AKY 6AKY_refined 2.8 A Inactive 16 81 - - - - Rubredoxin - CCR5 antagonist 34
small-molecule Antagonist CCL2, CCL8, CCL11, CCL13, CCL14, CCL7, CCL5, CCL4, CCL16, CCL3 peptide No No Peng P, Chen H, Zhu Y, Wang Z, Li J, Luo RH, Wang J, Chen L, Yang LM, Jiang H, Xie X, Wu B, Zheng YT, Liu H. 10.1021/acs.jmedchem.8b01077 2018-10-24 Yes
NK1R NK1 Tachykinin A Human X-ray 6HLP 6HLP_refined 2.2 A Inactive 1 71 - - - - GlgA glycogen synthase - netupitant
small-molecule Antagonist neurokinin B, neuropeptide-γ, hemokinin 1, substance P, neurokinin A, neuropeptide K peptide No No - - 2019-01-16 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 6N48 6N48_refined 3.2 A Active 99 70 - - - - T4-Lysozyme Camelid Antibody Fragment CHEMBL1615159
2-[[(3R)-4-(4-Tert-butylphenyl)-3-[[2-(4-methoxyphenyl)sulfanyl-5-[methyl(propan-2-yl)sulfamoyl]benzoyl]amino]butanoyl]amino]acetic acid
small-molecule
small-molecule		 Agonist
PAM		 noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ small-molecule No No - 10.1126/SCIENCE.AAW8981 2019-06-26 Yes
AA2AR A2A Adenosine A Human X-ray 6PS7 6PS7_refined 1.9 A Inactive 1 72 - - - - BRIL - ZM-241385
small-molecule Antagonist adenosine small-molecule No Yes - 10.1107/S2052252519013137 2019-11-13 Yes
OX1R OX1 Orexin A Human X-ray 6TOS 6TOS_refined 2.1 B Inactive 1 72 - - - - - - CHEMBL2413522
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 2020-01-15 Yes
OPRK κ Opioid A Human X-ray 6VI4 6VI4_refined 3.3 B Inactive 4 73 - - - - - Nanobody-6 JDTic
small-molecule Antagonist dynorphin A-(1-8), β-neoendorphin, big dynorphin, [Met]enkephalin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin B, α-neoendorphin peptide No No Che T, English J, Krumm BE, Kim K, Pardon E, Olsen RHJ, Wang S, Zhang S, Diberto JF, Sciaky N, Carroll FI, Steyaert J, Wacker D, Roth BL 10.1038/S41467-020-14889-7 2020-03-18 Yes
GABR2 GABAB2 GABAB C Human Cryo-EM 6W2X - 3.6 B Inactive - 71 - - - - - - CGP55845
1-Stearoyl-2-oleoyl-sn-glycero-3-phosphoethanolamine
small-molecule
small-molecule		 Inverse agonist
NAM		 - - No No Papasergi-Scott MM, Robertson MJ, Seven AB, Panova O, Mathiesen JM, Skiniotis G 10.1038/S41586-020-2469-4 2020-07-01 Yes
SMO SMO Frizzled F Human Cryo-EM 6XBK - 3.2 R Active 100 59 Gi/o αi1 - 61 - scFv16 Cholesterol
small-molecule Agonist - - No No Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X 10.1038/S41589-020-0646-2 2020-09-30 Yes
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 7LCI 7LCI_refined 2.9 R Active 100 85 Gs αs - 62 - - danuglipron
small-molecule Agonist glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide 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
DRD3 D3 Dopamine A Human Cryo-EM 7CMU - 3.0 R Active 100 68 Gi/o αi1 - 64 BRIL scFv16 pramipexole
small-molecule Agonist dopamine small-molecule No No Xu P, Huang S, Mao C, Krumm BE, Zhou XE, Tan Y, Huang XP, Liu Y, Shen DD, Jiang Y, Yu X, Jiang H, Melcher K, Roth BL, Cheng X, Zhang Y, Xu HE 10.1016/J.MOLCEL.2021.01.003 2021-03-10 Yes
GRM2 mGlu2 Metabotropic glutamate C Human Cryo-EM 7EPB 7EPB_refined 3.1 B Active - 89 - - - - - Anti-RON nanobody eglumegad
small-molecule Agonist 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
5HT1F 5-HT1F 5-Hydroxytryptamine A Human Cryo-EM 7EXD 7EXD_refined 3.4 R Active 100 74 Gi/o αi1 - 62 BRIL scFv16 lasmiditan
small-molecule Agonist 5-hydroxytryptamine small-molecule No No Huang S, Xu P, Tan Y, You C, Zhang Y, Jiang Y, Xu HE 10.1038/S41422-021-00527-4 2021-08-04 Yes
LSHR LH Glycoprotein hormone A Human Cryo-EM 7FIG - 3.9 R Active 100 79 Gs αs - 91 - Nanobody-35 Choriogonadotropin beta
Glycoprotein alpha
protein
protein		 Agonist hCG, LH peptide No No Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE 10.1038/S41586-021-03924-2 2021-09-29 Yes
AGRG2 ADGRG2 ADGRG B2 Mouse Cryo-EM 7WUQ - 2.9 R Active - 28 Gs αs - 55 - Nanobody-35 - - - - - No No Xiao P, Guo S, Wen X, He QT, Lin H, Huang SM, Gou L, Zhang C, Yang Z, Zhong YN, Yang CC, Li Y, Gong Z, Tao XN, Yang ZS, Lu Y, Li SL, He JY, Wang C, Zhang L, Kong L, Sun JP, Yu X 10.1038/S41586-022-04590-8 2022-04-27 Yes
SSR2 SST2 Somatostatin A Human Cryo-EM 7WIG 7WIG_refined 2.7 R Active 100 77 Gi/o αi1 - 64 - scFv16 ~{N}-[(2~{R})-1-[[(1~{R},3~{S})-3-(aminomethyl)cyclohexyl]methylamino]-3-(1~{H}-indol-3-yl)-1-oxidanylidene-propan-2-yl]spiro[indene-1,4'-piperidine]-1'-carboxamide
small-molecule Agonist SRIF-14, CST-17, cortistatin-14, SRIF-28 peptide No No Chen LN, Wang WW, Dong YJ, Shen DD, Guo J, Yu X, Qin J, Ji SY, Zhang H, Shen Q, He Q, Yang B, Zhang Y, Li Q, Mao C 10.1038/S41422-022-00669-Z 2022-06-01 Yes
5HT5A 5-HT5A 5-Hydroxytryptamine A Human X-ray 7UM4 7UM4_refined 2.8 A Inactive 35 71 - - - - PGS - CHEMBL3654198
small-molecule Antagonist 5-hydroxytryptamine small-molecule No No Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL 10.1038/S41594-022-00796-6 2022-07-20 Yes
GALR2 GAL2 Galanin A Human Cryo-EM 7XBD 7XBD_refined 3.1 A Active 100 72 Gq/11 αq - 60 - scFv16 Galanin, Human
peptide Agonist galanin-like peptide, spexin-1, galanin peptide No No Heo Y, Ishimoto N, Jeon YE, Yun JH, Ohki M, Anraku Y, Sasaki M, Kita S, Fukuhara H, Ikuta T, Kawakami K, Inoue A, Maenaka K, Tame JRH, Lee W, Park SY 10.1371/JOURNAL.PBIO.3001714 2022-07-13 Yes
CCR2 CCR2 Chemokine A Human Cryo-EM 7XA3 7XA3_refined 2.9 R Active 100 79 Gi/o αi1 - 65 - scFv16 C-C motif chemokine 2
peptide Agonist CCL2, CCL8, CCL11, CCL13, CCL24, CCL7, CCL26, CCL16 peptide No No Shao Z, Tan Y, Shen Q, Hou L, Yao B, Qin J, Xu P, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Chen ZH, Jiang Y, Xu HE, Ying S, Ma H, Zhang Y, Shen H 10.1038/S41421-022-00403-4 2022-08-24 Yes
GP119 GPR119 GPR18, GPR55 and GPR119 A Human Cryo-EM 7WCM 7WCM_refined 2.3 R Active 100 86 Gs αs - 60 - Nanobody-35 MBX-2982
small-molecule Agonist N-oleoylethanolamide, SEA, anandamide, N-palmitoylethanolamine small-molecule No No Qian Y, Wang J, Yang L, Liu Y, Wang L, Liu W, Lin Y, Yang H, Ma L, Ye S, Wu S, Qiao A 10.1038/S41467-022-34696-6 2022-12-21 Yes
T2R46 TAS2R46 Taste 2 T Human Cryo-EM 7XP5 - 3.1 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
PACR PAC1 VIP and PACAP B1 Human Cryo-EM 8E3X 8E3X_refined 2.3 R Active 100 77 Gs αs - 59 - Nanobody-35 [Ac-His1]PACAP-27
peptide Agonist VIP, PHV, PACAP-27, PHI, PHM, PACAP-38 peptide No No - - 2022-11-23 Yes
O51E2 Olfactory 51E2 Olfactory A Human Cryo-EM 8F76 8F76_refined 3.1 A Active 100 94 Gs αs Mini-Gs 55 - Nanobody-35 propanoic acid
small-molecule Agonist - - No No - 10.1038/S41586-023-05798-Y 2023-03-22 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 - - 2023-03-08 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
AA2AR A2A Adenosine A Human X-ray 8CIC - 2.1 A Inactive 1 71 - - - - BRIL - AB928
small-molecule Antagonist adenosine small-molecule No Yes 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
FFAR1 FFA1 Free fatty acid A Human Cryo-EM 8EJK - 3.4 R Active 100 89 Gq/11 αq - 60 - scFv16 fasiglifam
small-molecule Agonist oleic acid, docosahexaenoic acid, α-linolenic acid, myristic acid small-molecule No No Kumari P, Inoue A, Chapman K, Lian P, Rosenbaum DM 10.1073/PNAS.2219569120 2023-05-24 Yes
AA2BR A2B Adenosine A Human Cryo-EM 7XY6 - 3.0 R Active 100 86 Gs αs - 57 BRIL - BAY 60-6583
small-molecule Agonist adenosine small-molecule No No Chen Y, Zhang J, Weng Y, Xu Y, Lu W, Liu W, Liu M, Hua T, Song G 10.1126/SCIADV.ADD3709 2023-05-03 Yes
FFAR4 FFA4 Free fatty acid A Human Cryo-EM 8H4I - 3.1 R Active 100 78 Gs αs - 59 - Nanobody-35 docosahexaenoic acid
small-molecule Agonist linoleic acid, oleic acid, α-linolenic acid, myristic acid small-molecule No No Yin H, Inoue A, Ma Z, Zhu X, Xia R, Xu Z, Wang N, Duan Y, Zhang A, Guo C, He Y 10.1038/S41422-023-00835-X 2023-06-21 Yes
GRM2 mGlu2 Metabotropic glutamate C Human Cryo-EM 8JCX - 3.0 2 Inactive - 87 - - - - - - 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
GLR glucagon Glucagon B1 Human X-ray 5YQZ 5YQZ_refined 3.0 R Inactive 2 83 - - - - T4-Lysozyme - NNC1702
peptide Agonist (partial) glucagon peptide No No Zhang H, Qiao A, Yang L, Van Eps N, Frederiksen KS, Yang D, Dai A, Cai X, Zhang H, Yi C, Cao C, He L, Yang H, Lau J, Ernst OP, Hanson MA, Stevens RC, Wang MW, Reedtz-Runge S, Jiang H, Zhao Q, Wu B 10.1038/NATURE25153 2018-01-17 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 6H7N 6H7N_refined 2.5 A Active 99 60 - - - - Thioredoxin 1 Camelid antibody fragment Nb6B9 (S)-Xamoterol
small-molecule Agonist - - No No Miller RH, Bell EM, Russell Esposito E 10.1101/436212 2018-10-17 Yes
NK1R NK1 Tachykinin A Human X-ray 6J21 6J21_refined 3.2 A Inactive 1 71 - - - - T4-Lysozyme - aprepitant
small-molecule Antagonist neurokinin B, neuropeptide-γ, hemokinin 1, substance P, neurokinin A, neuropeptide K peptide No No - - 2019-03-06 Yes
AA2AR A2A Adenosine A Human X-ray 6GT3 6GT3_refined 2.0 A Inactive 1 72 - - - - BRIL - imaradenant
small-molecule Antagonist adenosine small-molecule No Yes - - 2019-06-26 Yes
CLTR1 CysLT1 Leukotriene A Human X-ray 6RZ4 6RZ4_refined 2.7 A Intermediate 44 85 - - - - BRIL - pranlukast
small-molecule Antagonist LTE4, LTD4, LTC4 small-molecule No Yes - 10.1126/SCIADV.AAX2518 2019-10-30 Yes
CLTR2 CysLT2 Leukotriene A Human X-ray 6RZ7 6RZ7_refined 2.4 A Intermediate 44 79 - - - - BRIL - ONO-2570366
small-molecule Antagonist LTE4, LTD4, LTC4 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
CRFR2 CRF2 Corticotropin-releasing factor B1 Human Cryo-EM 6PB1 6PB1_refined 2.8 P Active 100 68 Gs αs - 58 - Nanobody-35 Urocortin
peptide Agonist urocortin 2, corticotrophin-releasing hormone, urocortin 3, urocortin 1 peptide No No Ma S, Shen Q, Zhao LH, Mao C, Zhou XE, Shen DD, de Waal PW, Bi P, Li C, Jiang Y, Wang MW, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE 10.1016/J.MOLCEL.2020.01.013 2020-02-12 Yes
AA2AR A2A Adenosine A Human X-ray 6S0L 6S0L_refined 2.7 A Inactive 1 72 - - - - BRIL - ZM-241385
small-molecule Antagonist adenosine small-molecule No No - - 2020-07-15 Yes
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 6X1A - 2.5 R Active 100 84 Gs αs - 89 - Nanobody-35 danuglipron
small-molecule Agonist glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide 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
GLP2R GLP-2 Glucagon B1 Human Cryo-EM 7D68 - 3.0 R Active 100 53 Gs αs - 57 - Nanobody-35 glucagon
peptide Agonist glucagon-like peptide 2, glucagon-like peptide 2-(3-33) peptide No No Sun W, Chen LN, Zhou Q, Zhao LH, Yang D, Zhang H, Cong Z, Shen DD, Zhao F, Zhou F, Cai X, Chen Y, Zhou Y, Gadgaard S, van der Velden WJC, Zhao S, Jiang Y, Rosenkilde MM, Xu HE, Zhang Y, Wang MW 10.1038/S41422-020-00442-0 2020-12-16 Yes
HRH1 H1 Histamine A Human Cryo-EM 7DFL - 3.3 R Active 100 56 Gq/11 αq - 63 - scFv16 histamine
small-molecule Agonist histamine small-molecule No No Xia R, Wang N, Xu Z, Lu Y, Song J, Zhang A, Guo C, He Y 10.1038/S41467-021-22427-2 2021-03-31 Yes
GRM2 mGlu2 Metabotropic glutamate C Human Cryo-EM 7EPA 7EPA_refined 3.6 A Intermediate - 90 - - - - - - Apo (no ligand)
none Apo (no ligand) 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
GIPR GIP Glucagon B1 Human Cryo-EM 7DTY - 3.0 R Active 100 79 Gs αs - 59 - Nanobody-35 GIP
small-molecule Agonist gastric inhibitory polypeptide peptide No No Zhao F, Zhang C, Zhou Q, Hang K, Zou X, Chen Y, Wu F, Rao Q, Dai A, Yin W, Shen DD, Zhang Y, Xia T, Stevens RC, Xu HE, Yang D, Zhao L, Wang MW 10.7554/ELIFE.68719 2021-08-04 Yes
BKRB1 B1 Bradykinin A Human Cryo-EM 7EIB - 3.0 A Active 100 84 Gq/11 αq Gq-Gi1 chimera 61 - - [des-Arg10]kallidin
peptide Agonist [Hyp3]bradykinin, [des-Arg10]kallidin, bradykinin, Lys-[Hyp3]-bradykinin, kallidin, [des-Arg9]bradykinin, T-kinin peptide No No Yin YL, Ye C, Zhou F, Wang J, Yang D, Yin W, Wang MW, Xu HE, Jiang Y 10.1038/S41594-021-00645-Y 2021-10-13 Yes
MRGX2 MRGPRX2 A orphans A Human Cryo-EM 7VDM 7VDM_refined 3.0 R Active 100 77 Gi/o αi1 - 61 - scFv16 substance P
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
5HT2A 5-HT2A 5-Hydroxytryptamine A Human X-ray 7WC8 7WC8_refined 2.5 A Inactive 1 59 - - - - BRIL - LUMATEPERONE
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
FPR1 FPR1 Formylpeptide A Human Cryo-EM 7T6T 7T6T_refined 3.2 R Active 100 85 Gi/o αi1 - 61 - - synthetic peptide
peptide Agonist cathepsin G, spinorphin, annexin I, fMet-Leu-Phe 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 7TYH - 3.3 R Active 100 78 Gs αs - 58 - Nanobody-35 Calcitonin human
peptide Agonist β-CGRP, α-CGRP, calcitonin, calcitonin (salmon), amylin, adrenomedullin, 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
OPRM μ Opioid A Mouse Cryo-EM 7SBF - 2.9 R Active 100 71 Gi/o αi1 - 61 BRIL scFv16 N-[(2S)-2-(dimethylamino)-3-(4-hydroxyphenyl)propyl]-N'-[(2S)-1-(thiophen-3-yl)propan-2-yl]urea
small-molecule Agonist - - No No Wang H, Hetzer F, Huang W, Qu Q, Meyerowitz J, Kaindl J, Hubner H, Skiniotis G, Kobilka BK, Gmeiner P 10.1002/ANIE.202200269 2022-04-20 Yes
NPY2R Y2 Neuropeptide Y A Human Cryo-EM 7X9B 7X9B_refined 3.4 R Active 100 79 Gi/o αi1 - 62 - - neuropeptide Y
peptide Agonist neuropeptide Y, neuropeptide Y-(3-36), peptide YY, pancreatic polypeptide, PYY-(3-36) peptide No No Tang T, Tan Q, Han S, Diemar A, Lobner K, Wang H, Schuss C, Behr V, Morl K, Wang M, Chu X, Yi C, Keller M, Kofoed J, Reedtz-Runge S, Kaiser A, Beck-Sickinger AG, Zhao Q, Wu B 10.1126/SCIADV.ABM1232 2022-05-18 Yes
APJ apelin Apelin A Human Cryo-EM 7W0L 7W0L_refined 3.6 R Active 100 78 Gi/o αi1 - 64 BRIL scFv16 (1R,2S)-N-[4-(2,6-dimethoxyphenyl)-5-(6-methylpyridin-2-yl)-1,2,4-triazol-3-yl]-1-(5-methylpyrimidin-2-yl)-1-oxidanyl-propane-2-sulfonamide
small-molecule Agonist apelin-13, apelin-17, apelin-36, Elabela/Toddler-21, [Pyr1]apelin-13, Elabela/Toddler-11, apelin receptor early endogenous ligand, Elabela/Toddler-32 peptide No No Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F 10.1038/S41594-022-00797-5 2022-07-27 Yes
ADRB1 β1 Adrenoceptors A Wild turkey Cryo-EM 8DCS - 2.5 R Active 100 57 Gs αs - 51 T4-Lysozyme Nanobody-35 4-{[(2S)-3-(tert-butylamino)-2-hydroxypropyl]oxy}-3H-indole-2-carbonitrile
small-molecule Agonist - - No No Su M, Paknejad N, Zhu L, Wang J, Do HN, Miao Y, Liu W, Hite RK, Huang XY 10.1038/S41467-022-31823-1 2022-07-27 Yes
PTH1R PTH1 Parathyroid hormone B1 Human Cryo-EM 7VVJ 7VVJ_refined 3.2 R Active 100 62 Gs αs - 59 - Nanobody-35 PTHrP[1-36]
peptide Agonist PTH, PTHrP-(1-36), TIP39, PTHrP 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
ADA2A α2A Adrenoceptors A Human Cryo-EM 7W6P - 3.5 R Active 100 55 Gi/o αo - 58 - scFv16 N-pyridin-4-ylisoquinolin-4-amine
small-molecule Agonist (-)-adrenaline, (-)-noradrenaline small-molecule No No - - 2022-09-28 Yes
OX2R OX2 Orexin A Human X-ray 7XRR 7XRR_refined 2.9 A Inactive 1 70 - - - - - - lemborexant
small-molecule Antagonist orexin-B, orexin-A peptide No No Asada H, Im D, Hotta Y, Yasuda S, Murata T, Suno R, Iwata S 10.1016/J.STR.2022.11.001 2022-11-23 Yes
MRGX1 MRGPRX1 A orphans A Human Cryo-EM 8DWH 8DWH_refined 3.3 R Active 100 77 Gq/11 αq Gs-mini-Gq chimera 57 - - compound 16 [PMID: 31498617]
small-molecule Agonist bovine adrenal medulla peptide 8-22 peptide No No Liu Y, Cao C, Huang XP, Gumpper RH, Rachman MM, Shih SL, Krumm BE, Zhang S, Shoichet BK, Fay JF, Roth BL 10.1038/S41589-022-01173-6 2022-11-02 Yes
OPRK κ Opioid A Human Cryo-EM 8F7W 8F7W_refined 3.2 R Active 100 75 Gi/o αi1 - 64 - scFv16 dynorphin A-(1-8)
peptide Agonist dynorphin A-(1-8), β-neoendorphin, big dynorphin, [Met]enkephalin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin B, α-neoendorphin 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
OPSD Rhodopsin Opsins A Bovine X-ray 8A6D 8A6D_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 8HJ0 - 3.1 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 7T94 - 3.2 A Active 100 57 Gi/o αo - 62 - Antibody fragment acetylcholine
LY2119620
small-molecule
small-molecule		 Agonist
PAM		 acetylcholine small-molecule No No - - 2023-01-25 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 7XK9 - 3.4 A Active 99 69 - - - - T4-Lysozyme Camelid Antibody Fragment CHEMBL6913
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ small-molecule No No - - 2023-04-26 Yes
CNR2 CB2 Cannabinoid A Human Cryo-EM 8GUT 8GUT_refined 3.0 R Active 100 81 Gi/o αi1 - 62 - scFv16 1-[[4-[5-Fluoro-6-[(oxan-4-ylamino)methyl]pyridin-2-yl]phenyl]methyl]-3-(2-methylpropyl)imidazolidine-2,4-dione
small-molecule Agonist 2-arachidonoylglycerol, anandamide 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 7YDH - 3.1 R Active - 33 G12/13 α13 Gi2-mini-G13 chimera 57 - scFv16 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
CALCR CT Calcitonin B1 Human Cryo-EM 8F0K - 1.9 R Active 100 78 Gs αs - 58 - Nanobody-35
RAMP3		 San385
peptide Agonist β-CGRP, α-CGRP, calcitonin, calcitonin (salmon), amylin, adrenomedullin, adrenomedullin 2/intermedin peptide No No Cao J, Belousoff MJ, Gerrard E, Danev R, Fletcher MM, Dal Maso E, Schreuder H, Lorenz K, Evers A, Tiwari G, Besenius M, Li Z, Johnson RM, Wootten D, Sexton PM 10.1038/S41589-023-01393-4 2023-08-02 Yes
GRM4 mGlu4 Metabotropic glutamate C Human Cryo-EM 8JD6 - 3.4 S Active - 83 Gi/o αi3 - 63 - scFv16 VU0364770
small-molecule Agonist L-glutamic acid, L-serine-O-phosphate 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
5HT1B 5-HT1B 5-Hydroxytryptamine A Human X-ray 5V54 5V54_refined 3.9 A Inactive 15 71 - - - - BRIL - CHEMBL428892
small-molecule Antagonist 5-hydroxytryptamine, 5-HT-moduline, tryptamine small-molecule No No - - 2018-02-07 Yes
CALRL calcitonin-like Calcitonin B1 Human Cryo-EM 6E3Y 6E3Y_refined 3.3 R Active 100 75 Gs αs - 48 - Nanobody-35
RAMP1		 Calcitonin gene-related peptide 1
peptide Agonist - - No No Liang YL, Khoshouei M, Deganutti G, Glukhova A, Koole C, Peat TS, Radjainia M, Plitzko JM, Baumeister W, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Wootten D, Sexton PM 10.1038/S41586-018-0535-Y 2018-09-19 Yes
MTR1A MT1 Melatonin A Human X-ray 6ME5 6ME5_refined 3.2 A Inactive 1 83 - - - - GlgA glycogen synthase - agomelatine
small-molecule Agonist melatonin small-molecule No No - - 2019-04-24 Yes
CLTR1 CysLT1 Leukotriene A Human X-ray 6RZ5 6RZ5_refined 2.5 B Intermediate 44 84 - - - - BRIL - zafirlukast
small-molecule Antagonist LTE4, LTD4, LTC4 small-molecule No Yes - - 2019-10-30 Yes
OX2R OX2 Orexin A Human X-ray 6TPJ 6TPJ_refined 2.7 A Inactive 1 68 - - - - GlgA glycogen synthase - suvorexant
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
CALRL calcitonin-like Calcitonin B1 Human Cryo-EM 6UUN 6UUN_refined 3.0 R Active 100 77 Gs αs - 48 - Nanobody-35
RAMP2		 Adrenomedullin
peptide Agonist - - No No Liang YL, Belousoff MJ, Fletcher MM, Zhang X, Khoshouei M, Deganutti G, Koole C, Furness SGB, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Danev R, Wootten D, Sexton PM 10.1021/ACSPTSCI.9B00080 2020-03-25 Yes
CXCR2 CXCR2 Chemokine A Human Cryo-EM 6LFM 6LFM_refined 3.5 R Active 100 85 Gi/o αi1 - 65 - scFv16 Interleukin-8
protein Agonist CXCL3, CXCL1, CXCL6, CXCL2, CXCL7, CXCL5, 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
DRD1 D1 Dopamine A Human Cryo-EM 7LJD - 3.2 R Active 100 64 Gs αs Engineered G alpha 60 - Nanobody-35 dopamine
mevidalen
small-molecule
small-molecule		 Agonist
PAM		 noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, 5-hydroxytryptamine, dopamine small-molecule No No - - 2021-03-03 Yes
CASR CaS Calcium-sensing C Human Cryo-EM 7DD7 - 3.2 B Active - 73 - - - - - - Calcium
L-tryptophan
evocalcet
small-molecule
small-molecule
small-molecule		 Agonist
PAM
PAM		 spermine, L-tryptophan, Ca2+, Mg2+ small-molecule No No Wen T, Wang Z, Chen X, Ren Y, Lu X, Xing Y, Lu J, Chang S, Zhang X, Shen Y, Yang X 10.1126/SCIADV.ABG1483 2021-06-16 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 - 10.1038/S41467-021-24058-Z 2021-08-11 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 sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate 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
MC4R MC4 Melanocortin A Human Cryo-EM 7PIV 7PIV_refined 2.9 R Active 100 78 Gs αs - 46 - Nanobody-35 afamelanotide
peptide Agonist agouti-related protein, β-MSH, α-MSH, γ-MSH, ACTH peptide No No Heyder NA, Kleinau G, Speck D, Schmidt A, Paisdzior S, Szczepek M, Bauer B, Koch A, Gallandi M, Kwiatkowski D, Burger J, Mielke T, Beck-Sickinger AG, Hildebrand PW, Spahn CMT, Hilger D, Schacherl M, Biebermann H, Hilal T, Kuhnen P, Kobilka BK, Scheerer P 10.1038/S41422-021-00569-8 2021-11-17 Yes
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 7S3I - 2.5 R Active 100 57 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 - - 2022-01-05 Yes
CASR CaS Calcium-sensing C Human Cryo-EM 7SIN 7SIN_refined 5.9 A Inactive - 74 - - - - - - NPS 2143
small-molecule Antagonist spermine, L-tryptophan, Ca2+, Mg2+ 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
MTR1A MT1 Melatonin A Human Cryo-EM 7VGY - 3.1 A Active 100 80 Gi/o αi1 - 62 - scFv16 2-iodo-melatonin
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 (-)-adrenaline, (-)-noradrenaline 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 7WVY 7WVY_refined 3.0 R Active 100 85 Gi/o αi2 - 63 BRIL - Amyloid beta-Peptide (1-42)
peptide Agonist resolvin D1, serum amyloid A, 15-deoxy-LXA4, LTC4, LL-37, humanin, LTD4, aspirin triggered lipoxin A4, annexin I, aspirin-triggered resolvin D1, fMet-Leu-Phe, PrP106-126, LXA4 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
NPY1R Y1 Neuropeptide Y A Human Cryo-EM 7X9A 7X9A_refined 3.2 R Active 100 80 Gi/o αi1 - 61 - - neuropeptide Y
peptide Agonist pancreatic polypeptide, neuropeptide Y, peptide YY peptide No No Tang T, Tan Q, Han S, Diemar A, Lobner K, Wang H, Schuss C, Behr V, Morl K, Wang M, Chu X, Yi C, Keller M, Kofoed J, Reedtz-Runge S, Kaiser A, Beck-Sickinger AG, Zhao Q, Wu B 10.1126/SCIADV.ABM1232 2022-05-18 Yes
APJ apelin Apelin A Human Cryo-EM 7W0N - 4.2 R Active 100 78 Gi/o αi1 - 64 BRIL scFv16 apelin receptor early endogenous ligand
peptide Agonist apelin-13, apelin-17, apelin-36, Elabela/Toddler-21, [Pyr1]apelin-13, Elabela/Toddler-11, apelin receptor early endogenous ligand, Elabela/Toddler-32 peptide No No Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F 10.1038/S41594-022-00797-5 2022-07-27 Yes
TRFR TRH1 Thyrotropin-releasing hormone A Human Cryo-EM 7X1U 7X1U_refined 3.2 A Active 100 68 Gq/11 αq - 57 - scFv16 TRH
peptide 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
PTH1R PTH1 Parathyroid hormone B1 Human Cryo-EM 7VVL 7VVL_refined 2.8 R Active 100 58 Gs αs - 58 - Nanobody-35 teriparatide
peptide Agonist PTH, PTHrP-(1-36), TIP39, PTHrP 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
GP119 GPR119 GPR18, GPR55 and GPR119 A Human Cryo-EM 7WCN 7WCN_refined 2.9 R Active 100 86 Gs αs - 60 - Nanobody-35 AR231453
small-molecule Agonist N-oleoylethanolamide, SEA, anandamide, N-palmitoylethanolamine small-molecule No No Qian Y, Wang J, Yang L, Liu Y, Wang L, Liu W, Lin Y, Yang H, Ma L, Ye S, Wu S, Qiao A 10.1038/S41467-022-34696-6 2022-12-21 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, cortistatin-14, SRIF-28 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 8EFB 8EFB_refined 3.2 R Active 100 71 Gi/o αi1 - 64 - scFv16 OLICERIDINE
small-molecule Agonist dynorphin A-(1-8), [Met]enkephalin, endomorphin-1, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin B, endomorphin-2 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 98 79 - - - - - - neuropeptide Y
peptide Agonist neuropeptide Y, neuropeptide Y-(3-36), peptide YY, pancreatic polypeptide, 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
FSHR FSH Glycoprotein hormone A Human Cryo-EM 8I2H 8I2H_refined 6.0 A Inactive 15 82 - - - - - - Apo (no ligand)
none Apo (no ligand) FSH peptide No No - 10.1038/S41467-023-36170-3 2023-03-22 Yes
GLR glucagon Glucagon B1 Human Cryo-EM 8FU6 8FU6_refined 2.9 R Active 100 72 Gs αs - 54 - Nanobody-35 Glucagon derivative ZP3780
peptide Agonist glucagon peptide No No Krishna Kumar K, O'Brien ES, Habrian CH, Latorraca NR, Wang H, Tuneew I, Montabana E, Marqusee S, Hilger D, Isacoff EY, Mathiesen JM, Kobilka BK 10.1016/J.CELL.2023.02.028 2023-04-12 Yes
ACM4 M4 Acetylcholine (muscarinic) A Human Cryo-EM 7TRK - 2.8 R Active 100 57 Gi/o αi1 - 64 - scFv16 iperoxo
small-molecule Agonist acetylcholine small-molecule No No - - 2023-05-17 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-(1-36), TIP39, PTHrP peptide No No - - 2023-07-05 Yes
EDNRB ETB Endothelin A Human Cryo-EM 8IY5 - 2.8 R Active 100 71 Gi/o αi1 - 62 - scFv16 ENDOTHELIN
protein Agonist endothelin-1, endothelin-2, endothelin-3 peptide No No Sano FK, Akasaka H, Shihoya W, Nureki O 10.7554/ELIFE.85821 2023-08-16 Yes
AA2AR A2A Adenosine A Human X-ray 8JWZ - 2.4 A Inactive 1 71 - - - - T4-Lysozyme - AB928
small-molecule Antagonist adenosine small-molecule No Yes - - 2023-08-16 Yes
5HT2C 5-HT2C 5-Hydroxytryptamine A Human X-ray 6BQG 6BQG_refined 3.0 A Active 87 62 - - - - BRIL - ergotamine
small-molecule 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 5ZKP 5ZKP_refined 2.8 A Other - 85 - - - - Flavodoxin - foropafant
small-molecule Antagonist 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
ACM2 M2 Acetylcholine (muscarinic) A Human X-ray 5ZK8 5ZK8_refined 3.0 A Inactive 2 59 - - - - BRIL - N-methyl scopolamine
small-molecule Antagonist acetylcholine small-molecule No No Suno R, Lee S, Maeda S, Yasuda S, Yamashita K, Hirata K, Horita S, Tawaramoto MS, Tsujimoto H, Murata T, Kinoshita M, Yamamoto M, Kobilka BK, Vaidehi N, Iwata S, Kobayashi T 10.1038/S41589-018-0152-Y 2018-11-21 Yes
CNR1 CB1 Cannabinoid A Human Cryo-EM 6N4B 6N4B_refined 3.0 R Active 100 58 Gi/o αi1 - 62 - scFv16 MDMB-Fubinaca
small-molecule Agonist 2-arachidonoylglycerol, anandamide small-molecule No No - 10.1016/J.CELL.2018.11.040 2019-01-30 Yes
GLP1R GLP-1 Glucagon B1 Human X-ray 6KJV 6KJV_refined 2.8 B Inactive 0 57 - - - - T4-Lysozyme - PF-06372222
small-molecule NAM glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide peptide No No - 10.1107/S2052252519013496 2019-11-13 Yes
OX1R OX1 Orexin A Human X-ray 6TP3 6TP3_refined 3.0 A Inactive 1 74 - - - - - - daridorexant
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 6LPB 6LPB_refined 3.9 R Active 100 71 Gs αs - 57 - Nanobody-35 [Ac-His1]PACAP-27
peptide Agonist VIP, PHV, PACAP-27, PHI, PHM, PACAP-38 peptide No No Kobayashi K, Shihoya W, Nishizawa T, Kadji FMN, Aoki J, Inoue A, Nureki O 10.1038/S41594-020-0386-8 2020-03-11 Yes
ACM1 M1 Acetylcholine (muscarinic) A Human X-ray 6WJC - 2.6 A Inactive 2 62 - - - - T4-Lysozyme - ENDO-ATROPINE
muscarinic toxin 7
small-molecule
peptide		 Antagonist
NAM		 acetylcholine small-molecule No No - 10.1126/SCIENCE.AAX2517 2020-07-08 Yes
PE2R4 EP4 Prostanoid A Human Cryo-EM 7D7M 7D7M_refined 3.3 A Active 100 58 Gs αs - 58 - Nanobody-35 PGE2
small-molecule Agonist PGE2, PGF2α, thromboxane A2, PGI2, PGE1, PGD2 small-molecule No No Nojima S, Fujita Y, Kimura KT, Nomura N, Suno R, Morimoto K, Yamamoto M, Noda T, Iwata S, Shigematsu H, Kobayashi T 10.1016/J.STR.2020.11.007 2020-11-18 Yes
NTR1 NTS1 Neurotensin A Rat X-ray 6ZA8 6ZA8_refined 2.7 A Intermediate 15 78 - - - - DARPin D12 - CHEMBL508044
small-molecule Agonist (partial) 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
DRD1 D1 Dopamine A Human X-ray 7JOZ 7JOZ_refined 3.8 R Active 100 64 Gs αs - 86 - Nanobody-35 CHEMBL4453318
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, 5-hydroxytryptamine, dopamine small-molecule No No Sun B, Feng D, Chu ML, Fish I, Lovera S, Sands ZA, Kelm S, Valade A, Wood M, Ceska T, Kobilka TS, Lebon F, Kobilka BK 10.1038/S41467-021-23519-9 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
CASR CaS Calcium-sensing C Human Cryo-EM 7E6T 7E6T_refined 3.0 A Active - 74 - - - - - - Calcium
Cyclomethyltryptophan
small-molecule
small-molecule		 Agonist
PAM		 spermine, L-tryptophan, Ca2+, Mg2+ small-molecule No No Chen X, Wang L, Cui Q, Ding Z, Han L, Kou Y, Zhang W, Wang H, Jia X, Dai M, Shi Z, Li Y, Li X, Geng Y 10.7554/ELIFE.68578 2021-09-22 Yes
GP158 GPR158 C Orphans C Human Cryo-EM 7EWL 7EWL_refined 3.5 A Inactive - 41 - - - - - - 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
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
GHSR ghrelin Ghrelin A Human X-ray 7F83 7F83_refined 2.9 A Inactive 13 78 - - - - BRIL - PF-05190457
small-molecule Inverse agonist [des-Gln14]ghrelin, ghrelin peptide No No Qin J, Cai Y, Xu Z, Ming Q, Ji SY, Wu C, Zhang H, Mao C, Shen DD, Hirata K, Ma Y, Yan W, Zhang Y, Shao Z 10.1038/S41467-022-27975-9 2022-01-19 Yes
OXYR OT Vasopressin and oxytocin A Human Cryo-EM 7RYC - 2.9 O Active 100 73 Gq/11 αq Gamma subunit fused to alpha subunit 55 - scFv16 oxytocin
peptide Agonist oxytocin, vasopressin peptide No No Meyerowitz JG, Robertson MJ, Barros-Alvarez X, Panova O, Nwokonko RM, Gao Y, Skiniotis G 10.1038/S41594-022-00728-4 2022-03-09 Yes
CALCR CT Calcitonin B1 Human Cryo-EM 7TYI - 3.3 R Active 100 77 Gs αs - 58 - Nanobody-35 Amylin rat
peptide Agonist β-CGRP, α-CGRP, calcitonin, calcitonin (salmon), amylin, adrenomedullin, 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 2022-03-30 Yes
OPRM μ Opioid A Mouse Cryo-EM 7SCG - 3.0 D Active 100 71 Gi/o αi1 - 61 - scFv16 (2E)-N-[(2S)-2-(dimethylamino)-3-(4-hydroxyphenyl)propyl]-3-(naphthalen-1-yl)prop-2-enamide
small-molecule Agonist - - No No Wang H, Hetzer F, Huang W, Qu Q, Meyerowitz J, Kaindl J, Hubner H, Skiniotis G, Kobilka BK, Gmeiner P 10.1002/ANIE.202200269 2022-04-20 Yes
NPY4R Y4 Neuropeptide Y A Human Cryo-EM 7X9C 7X9C_refined 3.0 R Active 100 81 Gi/o αi1 - 61 - - Pancreatic polypeptide
peptide Agonist pancreatic polypeptide, neuropeptide Y, PYY-(3-36), peptide YY peptide No No Tang T, Tan Q, Han S, Diemar A, Lobner K, Wang H, Schuss C, Behr V, Morl K, Wang M, Chu X, Yi C, Keller M, Kofoed J, Reedtz-Runge S, Kaiser A, Beck-Sickinger AG, Zhao Q, Wu B 10.1126/SCIADV.ABM1232 2022-05-18 Yes
APJ apelin Apelin A Human Cryo-EM 7W0M 7W0M_refined 3.7 R Active 100 76 Gi/o αi1 - 62 BRIL scFv16 (1R,2S)-N-[4-(2,6-dimethoxyphenyl)-5-(6-methylpyridin-2-yl)-1,2,4-triazol-3-yl]-1-(5-methylpyrimidin-2-yl)-1-oxidanyl-propane-2-sulfonamide
small-molecule Agonist apelin-13, apelin-17, apelin-36, Elabela/Toddler-21, [Pyr1]apelin-13, Elabela/Toddler-11, apelin receptor early endogenous ligand, Elabela/Toddler-32 peptide No No Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F 10.1038/S41594-022-00797-5 2022-07-27 Yes
5HT2C 5-HT2C 5-Hydroxytryptamine A Human Cryo-EM 8DPG - 3.6 A Active 100 58 Gq/11 αq Gi2-mini-Gq chimera 57 - scFv16 psilocin
small-molecule Agonist 5-hydroxytryptamine small-molecule No No - - 2022-08-24 Yes
AA2AR A2A Adenosine A Human X-ray 8CU6 8CU6_refined 2.8 A Inactive 1 72 - - - - BRIL - LJ-4517
small-molecule Antagonist adenosine small-molecule No No Shiriaeva A, Park D, Kim G, Lee Y, Hou X, Jarhad DB, Kim G, Yu J, Hyun YE, Kim W, Gao ZG, Jacobson KA, Han GW, Stevens RC, Jeong LS, Choi S, Cherezov V. 10.1021/acs.jmedchem.2c00462 2022-08-31 Yes
TSHR TSH Glycoprotein hormone A Human Cryo-EM 7T9M - 3.1 R Inactive 28 74 - - - - - - CS-17 heavy chain
CS-17 light chain
protein
protein		 Inverse agonist TSH peptide No No Faust B, Billesbolle CB, Suomivuori CM, Singh I, Zhang K, Hoppe N, Pinto AFM, Diedrich JK, Muftuoglu Y, Szkudlinski MW, Saghatelian A, Dror RO, Cheng Y, Manglik A 10.1038/S41586-022-05159-1 2022-08-10 Yes
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 6B3J - 3.3 R Active 100 82 Gs αs - 49 - - Exendin-P5
peptide Agonist glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide peptide No No Liang YL, Khoshouei M, Glukhova A, Furness SGB, Zhao P, Clydesdale L, Koole C, Truong TT, Thal DM, Lei S, Radjainia M, Danev R, Baumeister W, Wang MW, Miller LJ, Christopoulos A, Sexton PM, Wootten D 10.1038/NATURE25773 2018-02-21 Yes
PTH1R PTH1 Parathyroid hormone B1 Human Cryo-EM 6NBF - 3.0 R Active 100 62 Gs αs - 58 - Nanobody-35 Long-acting parathyroid hormone analog
peptide Agonist PTH, PTHrP-(1-36), TIP39, PTHrP peptide No No - 10.1126/SCIENCE.AAV7942 2019-04-17 Yes
MTR1A MT1 Melatonin A Human X-ray 6PS8 6PS8_refined 3.3 A Inactive 1 83 - - - - GlgA glycogen synthase - CHEMBL15060
small-molecule Agonist melatonin small-molecule No No - 10.1107/S2052252519013137 2019-11-13 Yes
OX1R OX1 Orexin A Human X-ray 6TQ6 6TQ6_refined 2.6 B Inactive 1 71 - - - - - - CHEMBL4592653
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
ACM2 M2 Acetylcholine (muscarinic) A Human Cryo-EM 6U1N 6U1N_refined 4.0 R Active 100 57 Beta Beta-arrestin-1 - 86 - Fab30 light chain
Fab30 heavy chain		 LY2119620
small-molecule Agonist acetylcholine small-molecule No No Staus DP, Hu H, Robertson MJ, Kleinhenz ALW, Wingler LM, Capel WD, Latorraca NR, Lefkowitz RJ, Skiniotis G 10.1038/S41586-020-1954-0 2020-02-26 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
OX1R OX1 Orexin A Human X-ray 6V9S 6V9S_refined 3.5 A Inactive 1 72 - - - - GlgA glycogen synthase - JH112
small-molecule Antagonist orexin-B, orexin-A peptide No No Hellmann J, Drabek M, Yin J, Gunera J, Proll T, Kraus F, Langmead CJ, Hubner H, Weikert D, Kolb P, Rosenbaum DM, Gmeiner P 10.1073/PNAS.2002704117 2020-07-15 Yes
GPBAR GPBA Bile acid A Human Cryo-EM 7CFM - 3.0 R Active 100 83 Gs αs - 58 - Nanobody-35 CHEMBL2331646
small-molecule Agonist deoxycholic acid, chenodeoxycholic acid, lithocholic acid, cholic 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
ADRB1 β1 Adrenoceptors A Human X-ray 7BTS 7BTS_refined 3.1 A Active 99 58 - - - - T4-Lysozyme Camelid antibody fragment Nb6B9 (-)-adrenaline
small-molecule Agonist noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, (-)-noradrenaline small-molecule No No - - 2020-12-02 Yes
NPY2R Y2 Neuropeptide Y A Human X-ray 7DDZ 7DDZ_refined 2.8 A Inactive 1 76 - - - - Flavodoxin - CHEMBL1823578
small-molecule Antagonist neuropeptide Y, neuropeptide Y-(3-36), peptide YY, pancreatic polypeptide, PYY-(3-36) peptide No No Tang T, Hartig C, Chen Q, Zhao W, Kaiser A, Zhang X, Zhang H, Qu H, Yi C, Ma L, Han S, Zhao Q, Beck-Sickinger AG, Wu B 10.1038/S41467-021-21030-9 2021-01-27 Yes
DRD3 D3 Dopamine A Human Cryo-EM 7CMV - 2.7 R Active 100 68 Gi/o αi1 - 64 BRIL scFv16 CHEMBL70565
small-molecule Agonist dopamine small-molecule No No Xu P, Huang S, Mao C, Krumm BE, Zhou XE, Tan Y, Huang XP, Liu Y, Shen DD, Jiang Y, Yu X, Jiang H, Melcher K, Roth BL, Cheng X, Zhang Y, Xu HE 10.1016/J.MOLCEL.2021.01.003 2021-03-10 Yes
GRM7 mGlu7 Metabotropic glutamate C Human Cryo-EM 7EPC 7EPC_refined 4.0 B Inactive - 85 - - - - - - Apo (no ligand)
none Apo (no ligand) L-glutamic acid, L-serine-O-phosphate 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
FZD7 FZD7 Frizzled F Human Cryo-EM 7EVW - 3.2 R Active 100 59 Gs αs - 59 - Nanobody-35 Apo (no ligand)
none Apo (no ligand) - - No No Xu L, Chen B, Schihada H, Wright SC, Turku A, Wu Y, Han GW, Kowalski-Jahn M, Kozielewicz P, Bowin CF, Zhang X, Li C, Bouvier M, Schulte G, Xu F 10.1038/S41422-021-00525-6 2021-08-04 Yes
GRM1 mGlu1 Metabotropic glutamate C Human Cryo-EM 7DGD 7DGD_refined 4.0 A Inactive - 66 - - - - - - Apo (no ligand)
none Apo (no ligand) 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
MRGX2 MRGPRX2 A orphans A Human Cryo-EM 7S8L - 2.5 R Active 100 76 Gq/11 αq Gq-Gs chimera 57 - scFv16 Cortistatin 14
peptide 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
MRGX2 MRGPRX2 A orphans A Human Cryo-EM 7VUZ 7VUZ_refined 2.9 R Active 100 76 Gi/o αi1 - 62 - scFv16 PAMP-12
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
GHSR ghrelin Ghrelin A Human Cryo-EM 7W2Z 7W2Z_refined 2.8 R Active 100 82 Gi/o αo - 60 - scFv16 Ghrelin
peptide Agonist [des-Gln14]ghrelin, ghrelin peptide No No - - 2022-01-19 Yes
CCR1 CCR1 Chemokine A Human Cryo-EM 7VLA 7VLA_refined 2.7 R Active 100 85 Gi/o αi1 - 64 - scFv16 CCL15(27-92)
peptide Agonist CCL8, CCL13, CCL14, CCL16, CCL5, CCL7, CCL4, CCL23, CCL15, CCL3 peptide No No Shao Z, Shen Q, Yao B, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Ma H, Chen ZH, Xu HE, Ying S, Zhang Y, Shen H 10.1038/S41589-021-00918-Z 2022-03-23 Yes
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 7VBH 7VBH_refined 3.0 R Active 100 83 Gs αs - 53 - Nanobody-35 Peptide 20
peptide Agonist glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide 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 2022-04-06 Yes
NTR1 NTS1 Neurotensin A Human Cryo-EM 7UL2 7UL2_refined 2.4 R Inactive 4 69 - - - - - Nanobody-6 meclinertant
small-molecule Inverse agonist neuromedin N, large neurotensin, neurotensin, large neuromedin N peptide No No - - 2022-06-29 Yes
5HT5A 5-HT5A 5-Hydroxytryptamine A Human Cryo-EM 7UM5 7UM5_refined 2.7 A Active 100 75 Gi/o αo Mini-Go 60 - scFv16 5-CT
small-molecule Agonist 5-hydroxytryptamine small-molecule No No Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL 10.1038/S41594-022-00796-6 2022-07-20 Yes
ACKR3 ACKR3 Chemokine A Human Cryo-EM 7SK8 7SK8_refined 3.3 A Active 95 85 - - - - - CID25 Fab light chain
CID25 Fab heavy chain
CID24 Fab light chain
CID24 Fab heavy chain		 Stromal cell-derived factor 1
(1R)-4-[7-(3-carboxypropoxy)-6-methylquinolin-8-yl]-1-{[2-(4-hydroxypiperidin-1-yl)-1,3-thiazol-4-yl]methyl}-1,4-diazepan-1-ium
peptide
small-molecule		 Agonist
Agonist (partial)		 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
MRGX1 MRGPRX1 A orphans A Human Cryo-EM 8DWC - 2.9 R Active 100 78 Gq/11 αq Gs-mini-Gq chimera 57 - scFv16 Proenkephalin-A
peptide Agonist bovine adrenal medulla peptide 8-22 peptide No No - - 2022-11-02 Yes
C5AR1 C5a1 Complement peptide A Human Cryo-EM 7Y65 - 3.2 D Active 100 81 Gi/o αi1 - 64 - scFv16 C5a
peptide Agonist C3a, C5a, ribosomal protein S19, C5a des-Arg 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
EDNRB ETB Endothelin A Human Cryo-EM 8HBD 8HBD_refined 3.0 R Active 100 68 Gi/o αi1 - 61 - scFv16 sovateltide
peptide Agonist endothelin-1, endothelin-2, endothelin-3 peptide No No - - 2023-03-22 Yes
FFAR1 FFA1 Free fatty acid A Human Cryo-EM 8EIT - 2.8 R Active 100 89 Gq/11 αq - 59 - scFv16 docosahexaenoic acid
small-molecule Agonist oleic acid, docosahexaenoic acid, α-linolenic acid, myristic acid small-molecule No No Kumari P, Inoue A, Chapman K, Lian P, Rosenbaum DM 10.1073/PNAS.2219569120 2023-05-24 Yes
ACM4 M4 Acetylcholine (muscarinic) A Human Cryo-EM 7TRS - 2.8 R Active 100 56 Gi/o αi1 - 63 - scFv16 acetylcholine
small-molecule Agonist acetylcholine small-molecule No No - - 2023-05-17 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 2-arachidonoylglycerol, anandamide 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 - 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
CXCR1 CXCR1 Chemokine A Human Cryo-EM 8IC0 - 3.4 A Active 100 86 Gi/o αi1 - 65 - scFv16 Interleukin-8
protein Agonist CXCL8, cytokine domain of tyrosyl tRNA synthetase, CXCL6 peptide No No Ishimoto N, Park JH, Kawakami K, Tajiri M, Mizutani K, Akashi S, Tame JRH, Inoue A, Park SY 10.1038/S41467-023-39799-2 2023-07-19 Yes
AA2AR A2A Adenosine A Human X-ray 8JWY - 2.3 A Inactive 1 70 - - - - T4-Lysozyme - 3-[2-Azanyl-6-[2-oxidanylidene-1-[[6-(2-oxidanylpropan-2-yl)pyridin-2-yl]methyl]pyridin-4-yl]pyrimidin-4-yl]-2-methyl-benzenecarbonitrile
small-molecule Antagonist adenosine small-molecule No Yes - - 2023-08-16 Yes
GRM5 mGlu5 Metabotropic glutamate C Human X-ray 6FFH 6FFH_refined 2.7 A Inactive - 21 - - - - T4-Lysozyme - fenobam
small-molecule NAM L-glutamic acid small-molecule No No Christopher JA, Orgovan Z, Congreve M, Dore AS, Errey JC, Marshall FH, Mason JS, Okrasa K, Rucktooa P, Serrano-Vega MJ, Ferenczy GG, Keseru GM 10.1021/ACS.JMEDCHEM.7B01722 2018-03-07 Yes
5HT1B 5-HT1B 5-Hydroxytryptamine A Human Cryo-EM 6G79 - 3.8 S Active 100 67 Gi/o αo - 59 - - donitriptan
small-molecule Agonist 5-hydroxytryptamine, 5-HT-moduline, tryptamine small-molecule No No Garcia-Nafria J, Nehme R, Edwards PC, Tate CG 10.1038/S41586-018-0241-9 2018-06-20 Yes
TA2R TP Prostanoid A Human X-ray 6IIU 6IIU_refined 2.5 A Inactive 35 87 - - - - Rubredoxin - ramatroban
small-molecule Antagonist PGE2, PGF2α, thromboxane A2, PGH2, PGI2, PGD2 small-molecule No No - 10.1038/S41589-018-0170-9 2018-12-19 Yes
AA2AR A2A Adenosine A Human X-ray 6MH8 6MH8_refined 4.2 A Inactive 1 72 - - - - BRIL - ZM-241385
small-molecule Antagonist adenosine small-molecule No No - 10.1107/S205225251900263X 2019-04-24 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 6PS2 6PS2_refined 2.4 A Inactive 0 68 - - - - T4-Lysozyme - CHEMBL1160734
small-molecule Antagonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ small-molecule No No - - 2019-11-13 Yes
OX1R OX1 Orexin A Human X-ray 6TQ7 6TQ7_refined 2.7 A Inactive 1 71 - - - - - - SB-334867
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
NTR1 NTS1 Neurotensin A Human Cryo-EM 6UP7 6UP7_refined 4.2 R Active 100 77 Beta Beta-arrestin-1 - 83 - - JMV431
peptide Agonist neuromedin N, large neurotensin, neurotensin, large neuromedin N peptide No No Huang W, Masureel M, Qu Q, Janetzko J, Inoue A, Kato HE, Robertson MJ, Nguyen KC, Glenn JS, Skiniotis G, Kobilka BK 10.1038/S41586-020-1953-1 2020-02-26 Yes
GABR2 GABAB2 GABAB C Human Cryo-EM 6UO8 - 3.6 B Active - 74 - - - - - - CHEMBL112710
GS39783
small-molecule
small-molecule		 Agonist
PAM		 - - No No Shaye H, Ishchenko A, Lam JH, Han GW, Xue L, Rondard P, Pin JP, Katritch V, Gati C, Cherezov V 10.1038/S41586-020-2408-4 2020-06-10 Yes
CXCR2 CXCR2 Chemokine A Human X-ray 6LFL 6LFL_refined 3.2 A Inactive 5 76 - - - - GlgA glycogen synthase - 4-[[3,4-Dioxo-2-[[(1R)-1-(4-propan-2-ylfuran-2-yl)propyl]amino]cyclobuten-1-yl]amino]-3-hydroxy-N,N-dimethylpyridine-2-carboxamide
small-molecule Allosteric antagonist CXCL3, CXCL1, CXCL6, CXCL2, CXCL7, CXCL5, 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
SCTR secretin Glucagon B1 Human Cryo-EM 7D3S 7D3S_refined 2.9 R Active 100 60 Gs αs - 58 - Nanobody-35 SECRETIN
protein Agonist secretin, VIP peptide No No Fukuhara S, Kobayashi K, Kusakizako T, Iida W, Kato M, Shihoya W, Nureki O 10.1016/J.BBRC.2020.08.042 2020-11-04 Yes
NTR1 NTS1 Neurotensin A Rat X-ray 6Z66 6Z66_refined 3.2 A Intermediate 15 80 - - - - DARPin D12 - Apo (no ligand)
none Apo (no ligand) 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
DRD1 D1 Dopamine A Human Cryo-EM 7CRH 7CRH_refined 3.3 R Active 100 61 Gs αs - 60 - Nanobody-35 CHEMBL1416789
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, 5-hydroxytryptamine, dopamine 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
CASR CaS Calcium-sensing C Human Cryo-EM 7DD6 - 3.2 B Active - 73 - - - - - - Calcium
L-tryptophan
small-molecule
small-molecule		 Agonist
PAM		 spermine, L-tryptophan, Ca2+, Mg2+ small-molecule No No - - 2021-06-16 Yes
ADRB3 β3 Adrenoceptors A Dog Cryo-EM 7DH5 - 3.2 R Active 100 68 Gs αs - 59 - Nanobody-35 mirabegron
small-molecule Agonist - - No No Nagiri C, Kobayashi K, Tomita A, Kato M, Kobayashi K, Yamashita K, Nishizawa T, Inoue A, Shihoya W, Nureki O 10.1016/J.MOLCEL.2021.06.024 2021-08-04 Yes
PD2R2 DP2 Prostanoid A Human X-ray 7M8W 7M8W_refined 2.6 A Inactive 25 83 - - - - T4-Lysozyme - 15(R)-15-methyl-PGD2
small-molecule Antagonist PGE2, PGD3, PGF2α, thromboxane A2, PGJ2, PGI2, PGD2 small-molecule No Yes Liu H, Deepak RNVK, Shiriaeva A, Gati C, Batyuk A, Hu H, Weierstall U, Liu W, Wang L, Cherezov V, Fan H, Zhang C 10.1073/PNAS.2102813118 2021-08-25 Yes
LSHR LH Glycoprotein hormone A Human Cryo-EM 7FIJ 7FIJ_refined 3.8 R Inactive 9 80 - - - - - - Apo (no ligand)
none Apo (no ligand) hCG, LH peptide No No Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE 10.1038/S41586-021-03924-2 2021-09-29 Yes
MC4R MC4 Melanocortin A Human Cryo-EM 7PIU - 2.6 R Active 100 78 Gs αs - 48 - Nanobody-35 setmelanotide
peptide Agonist agouti-related protein, β-MSH, α-MSH, γ-MSH, ACTH peptide No No Heyder NA, Kleinau G, Speck D, Schmidt A, Paisdzior S, Szczepek M, Bauer B, Koch A, Gallandi M, Kwiatkowski D, Burger J, Mielke T, Beck-Sickinger AG, Hildebrand PW, Spahn CMT, Hilger D, Schacherl M, Biebermann H, Hilal T, Kuhnen P, Kobilka BK, Scheerer P 10.1038/S41422-021-00569-8 2021-11-17 Yes
GHSR ghrelin Ghrelin A Human Cryo-EM 7NA7 7NA7_refined 2.7 R Active 100 80 Gi/o αi1 - 61 - Antibody fragment Ghrelin-27
peptide Agonist [des-Gln14]ghrelin, ghrelin peptide No No Liu H, Sun D, Myasnikov A, Damian M, Baneres JL, Sun J, Zhang C 10.1038/S41467-021-26735-5 2021-12-15 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, serum amyloid A, 15-deoxy-LXA4, LTC4, LL-37, humanin, LTD4, aspirin triggered lipoxin A4, annexin I, aspirin-triggered resolvin D1, fMet-Leu-Phe, PrP106-126, LXA4 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 7TYX - 2.6 R Active 100 77 Gs αs - 59 - Nanobody-35 Amylin rat
peptide Agonist β-CGRP, α-CGRP, calcitonin, calcitonin (salmon), amylin, adrenomedullin, 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 2022-03-30 Yes
AGRF1 ADGRF1 ADGRF B2 Human Cryo-EM 7WU3 - 3.1 R Active - 31 Gs αs Mini-Gs 54 - Nanobody-35 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
VIPR2 VPAC2 VIP and PACAP B1 Human Cryo-EM 7VQX - 2.7 R Active 100 82 Gs αs - 60 - Nanobody-35 PACAP-27
peptide Agonist VIP, PACAP-27, secretin, PHI, GHRH, PACAP-38 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
5HT5A 5-HT5A 5-Hydroxytryptamine A Human Cryo-EM 7UM6 - 2.8 A Active 100 72 Gi/o αo Mini-Go 60 - scFv16 lisuride
small-molecule Agonist 5-hydroxytryptamine small-molecule No No Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL 10.1038/S41594-022-00796-6 2022-07-20 Yes
ACKR3 ACKR3 Chemokine A Human Cryo-EM 7SK6 7SK6_refined 4.0 A Active 95 83 - - - - - CID24 Fab light chain
CID24 Fab heavy chain		 Stromal cell-derived factor 1
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
AGRL3 ADGRL3 ADGRL B2 Mouse Cryo-EM 7WY5 - 2.8 R Active - 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 7YU4 7YU4_refined 3.3 A Active 99 73 - - - - - - [(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
ACM3 M3 Acetylcholine (muscarinic) A Human Cryo-EM 8E9Z - 2.7 A Active 100 47 Gq/11 αq Mini-Gq 57 - scFv16 iperoxo
small-molecule Agonist acetylcholine small-molecule No No - - 2022-11-30 Yes
AGTR1 AT1 Angiotensin A Human Cryo-EM 7F6G 7F6G_refined 2.9 A Active 100 86 Gq/11 αq - 97 - - SAR1-AngII
peptide Agonist angiotensin A, angiotensin III, angiotensin IV, angiotensin II peptide No No - - 2023-03-29 Yes
EDNRA ETA Endothelin A Human Cryo-EM 8HCQ 8HCQ_refined 3.0 R Active 100 71 Gq/11 αq - 57 - scFv16 ENDOTHELIN
protein Agonist endothelin-1, endothelin-2, endothelin-3 peptide No No - - 2023-03-22 Yes
GRPR BB2 Bombesin A Human Cryo-EM 7W40 7W40_refined 3.0 A Active 100 78 Gq/11 αq - 79 - scFv16 Bombesin
peptide Agonist neuromedin B, gastrin releasing peptide(14-27) (human), gastrin-releasing peptide, neuromedin C, GRP-(18-27) peptide No No Peng S, Zhan Y, Zhang D, Ren L, Chen A, Chen ZF, Zhang H 10.1073/PNAS.2216230120 2023-02-22 Yes
S1PR1 S1P1 Lysophospholipid (S1P) A Human Cryo-EM 8G94 8G94_refined 3.2 A Active 100 75 Gi/o αi1 - 62 - scFv16 Early activation antigen CD69
peptide Agonist sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate small-molecule No No Chen H, Qin Y, Chou M, Cyster JG, Li X 10.7554/ELIFE.88204 2023-04-19 Yes
ACM4 M4 Acetylcholine (muscarinic) A Human Cryo-EM 7TRP - 2.4 R Active 100 56 Gi/o αi1 - 64 - scFv16 iperoxo
LY2033298
small-molecule
small-molecule		 Agonist
PAM		 acetylcholine small-molecule No No - - 2023-05-17 Yes
PF2R FP Prostanoid A Human Cryo-EM 8IUM - 3.1 R Active 100 82 Gq/11 αq - 60 - scFv16
Nanobody-35		 tafluprost acid
small-molecule Agonist PGE2, PGF2α, thromboxane A2, PGI2, 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 8JD5 - 3.6 2 Active - 90 Gi/o αi1 - 63 - scFv16 ADX88178
L-glutamic acid
JNJ-40411813
small-molecule
small-molecule
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
GRM5 mGlu5 Metabotropic glutamate C Human X-ray 6FFI 6FFI_refined 2.2 A Inactive - 20 - - - - T4-Lysozyme - methoxy-MPEP
small-molecule NAM L-glutamic acid small-molecule No No Christopher JA, Orgovan Z, Congreve M, Dore AS, Errey JC, Marshall FH, Mason JS, Okrasa K, Rucktooa P, Serrano-Vega MJ, Ferenczy GG, Keseru GM 10.1021/ACS.JMEDCHEM.7B01722 2018-03-07 Yes
AA1R A1 Adenosine A Human Cryo-EM 6D9H 6D9H_refined 3.6 R Active 100 88 Gi/o αi2 - 59 - - adenosine
small-molecule Agonist adenosine small-molecule No No Draper-Joyce CJ, Khoshouei M, Thal DM, Liang YL, Nguyen ATN, Furness SGB, Venugopal H, Baltos JA, Plitzko JM, Danev R, Baumeister W, May LT, Wootten D, Sexton PM, Glukhova A, Christopoulos A 10.1038/S41586-018-0236-6 2018-06-20 Yes
CCR2 CCR2 Chemokine A Human X-ray 6GPS 6GPS_refined 3.3 A Inactive 16 74 - - - - Rubredoxin - MK-0812
small-molecule Antagonist CCL2, CCL8, CCL11, CCL13, CCL24, CCL7, CCL26, CCL16 peptide No No - 10.1016/J.STR.2018.10.027 2019-01-02 Yes
EDNRB ETB Endothelin A Human X-ray 6K1Q 6K1Q_refined 2.7 A Inactive 4 68 - - - - T4-Lysozyme - IRL 2500
peptide Inverse agonist endothelin-1, endothelin-2, endothelin-3 peptide No No - 10.1038/S42003-019-0482-7 2019-07-17 Yes
ADRB2 β2 Adrenoceptors A Human Cryo-EM 6NI3 6NI3_refined 3.8 R Active 100 69 Gs αs - 59 - Nanobody-35 CHEMBL1615159
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ small-molecule No No Nguyen AH, Thomsen ARB, Cahill TJ 3rd, Huang R, Huang LY, Marcink T, Clarke OB, Heissel S, Masoudi A, Ben-Hail D, Samaan F, Dandey VP, Tan YZ, Hong C, Mahoney JP, Triest S, Little J 4th, Chen X, Sunahara R, Steyaert J, Molina H, Yu Z, des Georges A, Lefkowitz RJ 10.1038/S41594-019-0330-Y 2019-11-20 Yes
PACR PAC1 VIP and PACAP B1 Human Cryo-EM 6M1I - 3.5 A Active 100 75 Gs αs - 57 - Nanobody-35 [Ac-His1]PACAP-27
peptide Agonist VIP, PHV, PACAP-27, PHI, PHM, PACAP-38 peptide No No - - 2020-03-11 Yes
GLR glucagon Glucagon B1 Human Cryo-EM 6WPW 6WPW_refined 3.1 R Active 100 83 Gs αs - 56 - Nanobody-35 Glucagon derivative ZP3780
peptide Agonist glucagon peptide No No Hilger D, Kumar KK, Hu H, Pedersen MF, O'Brien ES, Giehm L, Jennings C, Eskici G, Inoue A, Lerch M, Mathiesen JM, Skiniotis G, Kobilka BK 10.1126/SCIENCE.ABA3373 2020-08-12 Yes
NTR1 NTS1 Neurotensin A Rat Cryo-EM 7L0R - 4.2 C Active 100 73 Gi/o αi1 Non-canonical conformation 63 - - neurotensin
peptide Agonist neuromedin N, neurotensin peptide No No Zhang M, Gui M, Wang ZF, Gorgulla C, Yu JJ, Wu H, Sun ZJ, Klenk C, Merklinger L, Morstein L, Hagn F, Pluckthun A, Brown A, Nasr ML, Wagner G 10.1038/S41594-020-00554-6 2021-01-06 Yes
DRD1 D1 Dopamine A Human Cryo-EM 7LJC - 3.0 R Active 100 63 Gs αs Engineered G alpha 60 - Nanobody-35 CHEMBL1160787
mevidalen
small-molecule
small-molecule		 Agonist
PAM		 noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, 5-hydroxytryptamine, dopamine small-molecule No No Zhuang Y, Krumm B, Zhang H, Zhou XE, Wang Y, Huang XP, Liu Y, Cheng X, Jiang Y, Jiang H, Zhang C, Yi W, Roth BL, Zhang Y, Xu HE 10.1038/S41422-021-00482-0 2021-03-03 Yes
GRM4 mGlu4 Metabotropic glutamate C Human Cryo-EM 7E9H - 4.0 R Intermediate - 84 Gi/o αi3 - 63 - scFv16 L-serine-O-phosphate
small-molecule Agonist L-glutamic acid, L-serine-O-phosphate small-molecule No No Lin S, Han S, Cai X, Tan Q, Zhou K, Wang D, Wang X, Du J, Yi C, Chu X, Dai A, Zhou Y, Chen Y, Zhou Y, Liu H, Liu J, Yang D, Wang MW, Zhao Q, Wu B 10.1038/S41586-021-03495-2 2021-06-23 Yes
MTR1A MT1 Melatonin A Human Cryo-EM 7DB6 7DB6_refined 3.3 D Active 100 79 Gi/o αi1 - 62 - scFv16 ramelteon
small-molecule Agonist melatonin small-molecule No No Okamoto HH, Miyauchi H, Inoue A, Raimondi F, Tsujimoto H, Kusakizako T, Shihoya W, Yamashita K, Suno R, Nomura N, Kobayashi T, Iwata S, Nishizawa T, Nureki O 10.1038/S41594-021-00634-1 2021-08-18 Yes
LSHR LH Glycoprotein hormone A Human Cryo-EM 7FIH - 3.2 R Active 100 79 Gs αs - 60 - - Choriogonadotropin beta
Glycoprotein alpha
5-Amino-N-(1,1-dimethylethyl)-2-(methylthio)-4-[3-[[2-(4-morpholinyl)acetyl]amino]phenyl]thieno[2,3-d]pyrimidine-6-carboxamide
protein
protein
small-molecule		 Agonist hCG, LH peptide No No Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE 10.1038/S41586-021-03924-2 2021-09-29 Yes
GP183 GPR183 A orphans A Human Cryo-EM 7TUY 7TUY_refined 3.0 R Active 65 73 - - - - BRIL anti-BRIL Fab heavy chain
anti-BRIL Fab light chain
anti-Fab Nanobody		 8-[(2E)-3-(4-chlorophenyl)prop-2-enoyl]-3-[(3,4-dichlorophenyl)methyl]-1-oxa-3,8-diazaspiro[4.5]decan-2-one
small-molecule Inverse agonist 7α,25-dihydroxycholesterol, 7α,27-dihydroxycholesterol, 7β, 27-dihydroxycholesterol, 7β, 25-dihydroxycholesterol, 7α-hydroxycholesterol, 25-hydroxycholesterol, 27-hydroxycholesterol, 7β-hydroxycholesterol small-molecule No No Chen H, Huang W, Li X 10.1016/J.STR.2022.04.006 2022-04-13 Yes
NMUR1 NMU1 Neuromedin U A Human Cryo-EM 7W56 - 2.9 R Active 100 65 Gq/11 αq - 59 - scFv16 Neuromedin-S
peptide Agonist neuromedin U-25, neuromedin U-23, 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
APJ apelin Apelin A Human Cryo-EM 7W0P 7W0P_refined 3.2 R Active 100 77 Gi/o αi1 - 64 BRIL scFv16 apelin receptor early endogenous ligand
peptide Agonist apelin-13, apelin-17, apelin-36, Elabela/Toddler-21, [Pyr1]apelin-13, Elabela/Toddler-11, apelin receptor early endogenous ligand, Elabela/Toddler-32 peptide No No Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F 10.1038/S41594-022-00797-5 2022-07-27 Yes
SSR4 SST4 Somatostatin A Human Cryo-EM 7XMT 7XMT_refined 2.8 R Active 100 68 Gi/o αi1 - 63 - scFv16 J-2156
small-molecule Agonist SRIF-14, CST-17, cortistatin-14, SRIF-28 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 7XKE - 2.9 R Active - 25 Gs αs Mini-Gs 60 - Nanobody-35 PRASTERONE
small-molecule Agonist - - No No - - 2022-08-10 Yes
P2Y12 P2Y12 P2Y A Human X-ray 7PP1 - 2.8 A Intermediate 44 78 - - - - BRIL - selatogrel
small-molecule Antagonist ADP, ATP small-molecule No No Pons V, Garcia C, Tidten-Luksch N, Mac Sweeney A, Caroff E, Gales C, Riederer MA 10.1016/j.bcp.2022.115291 2022-11-02 Yes
S1PR1 S1P1 Lysophospholipid (S1P) A Human Cryo-EM 7VIF 7VIF_refined 2.8 F Active 100 73 Gi/o αi1 - 64 - scFv16 (S)-FTY720-phosphate
small-molecule Agonist sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate 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
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 8F7R - 3.3 R Active 100 72 Gi/o αi1 - 63 - scFv16 endomorphin-1
peptide Agonist dynorphin A-(1-8), [Met]enkephalin, endomorphin-1, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin B, endomorphin-2 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
NTR1 NTS1 Neurotensin A Rat Cryo-EM 8FMZ - 2.6 A Active 100 66 Gq/11 αq Mini-Gq 57 - scFv16 neurotensin
peptide Agonist neuromedin N, neurotensin peptide No No - 10.1021/ACS.BIOCHEM.3C00029 2023-03-29 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, oleic acid, α-linolenic acid, myristic acid small-molecule No No - 10.1126/SCIENCE.ADD6220 2023-03-15 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-(1-36), TIP39, PTHrP 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 8FLR - 2.9 R Active 100 61 Gs αs - 59 - Nanobody-35 PTHrP[1-36]
peptide Agonist PTH, PTHrP-(1-36), TIP39, PTHrP 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
GRM2 mGlu2 Metabotropic glutamate C Human Cryo-EM 8JCU - 2.8 2 Inactive - 87 - - - - - - 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 6FK7 6FK7_refined 2.6 A Active 98 94 - - - - - - (2~{S})-2-(4-chlorophenyl)-3-methyl-1-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-yl-butan-1-one
small-molecule Agonist - - No No - - 2018-04-04 Yes
5HT2B 5-HT2B 5-Hydroxytryptamine A Human X-ray 6DRY 6DRY_refined 2.9 A Intermediate 44 60 - - - - BRIL - methylergonovine
small-molecule Agonist 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
EDNRB ETB Endothelin A Human X-ray 6IGL - 2.7 A Inactive 4 70 - - - - T4-Lysozyme - sovateltide
peptide Agonist (partial) endothelin-1, endothelin-2, endothelin-3 peptide No No - - 2018-11-21 Yes
PTH1R PTH1 Parathyroid hormone B1 Human Cryo-EM 6NBI - 4.0 R Active 100 62 Gs αs - 56 - Nanobody-35 Long-acting parathyroid hormone analog
peptide Agonist PTH, PTHrP-(1-36), TIP39, PTHrP peptide No No - - 2019-04-17 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 6PS6 6PS6_refined 2.7 A Inactive 0 68 - - - - T4-Lysozyme - timolol
small-molecule Antagonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ small-molecule No No - 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-(1-7), angiotensin II, 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
PACR PAC1 VIP and PACAP B1 Human Cryo-EM 6M1H - 3.6 A Active 100 73 Gs αs - 55 - Nanobody-35 maxadilan
peptide Agonist VIP, PHV, PACAP-27, PHI, PHM, PACAP-38 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
SUCR1 succinate Succinate A Rat X-ray 6Z10 6Z10_refined 2.3 A Active 65 90 - - - - - Nanobody-6 CHEMBL4751488
small-molecule Antagonist - - No No Velcicky J,Wilcken R,Cotesta S,Janser P,Schlapbach A,Wagner T,Piechon P,Villard F,Bouhelal R,Piller F,Harlfinger S,Stringer R,Fehlmann D,Kaupmann K,Littlewood-Evans A,Haffke M,Gommermann N 10.1021/acs.jmedchem.0c01020 2020-09-16 Yes
GHRHR GHRH Glucagon B1 Human Cryo-EM 7CZ5 7CZ5_refined 2.6 R Active 100 64 Gs αs - 58 - Nanobody-35 Somatoliberin
peptide Agonist GHRH peptide No No Zhou F, Zhang H, Cong Z, Zhao LH, Zhou Q, Mao C, Cheng X, Shen DD, Cai X, Ma C, Wang Y, Dai A, Zhou Y, Sun W, Zhao F, Zhao S, Jiang H, Jiang Y, Yang D, Eric Xu H, Zhang Y, Wang MW 10.1038/S41467-020-18945-0 2020-11-18 Yes
CALRL calcitonin-like Calcitonin B1 Human Cryo-EM 7KNU 7KNU_refined 3.5 R Inactive 10 74 - - - - - RAMP1 Calcitonin gene-related peptide 1
peptide Agonist - - 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
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 7KI1 - 2.5 R Active 100 83 Gs αs - 89 - Nanobody-35 Taspoglutide
peptide Agonist glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide peptide No No Zhang X, Belousoff MJ, Liang YL, Danev R, Sexton PM, Wootten D 10.1016/J.CELREP.2021.109374 2021-08-04 Yes
NK1R NK1 Tachykinin A Human Cryo-EM 7RMG - 3.0 R Active 100 71 Gs αs Gs-Gq chimera 49 - Nanobody-35 substance P
peptide Agonist neurokinin B, neuropeptide-γ, hemokinin 1, substance P, neurokinin A, neuropeptide K 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
GP139 GPR139 A orphans A Human Cryo-EM 7VUH 7VUH_refined 3.2 R Active 100 80 Gs αs - 61 - 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
US28 US28 Unclassified A strain AD169 Cryo-EM 7RKN - 3.6 R Active 100 83 Gi/o αi1 - 61 - scFv16 Fractalkine
peptide Agonist - - No No Tsutsumi N, Maeda S, Qu Q, Vogele M, Jude KM, Suomivuori CM, Panova O, Waghray D, Kato HE, Velasco A, Dror RO, Skiniotis G, Kobilka BK, Garcia KC 10.1126/SCIADV.ABL5442 2022-01-26 Yes
ADA2A α2A Adrenoceptors A Human Cryo-EM 7EJK - 3.4 R Active 100 55 Gi/o αo - 61 - scFv16 oxymetazoline
small-molecule Agonist (-)-adrenaline, (-)-noradrenaline 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
GALR2 GAL2 Galanin A Human Cryo-EM 7WQ4 7WQ4_refined 2.6 R Active 100 73 Gq/11 αq - 60 - Nanobody-35 galanin
peptide Agonist galanin-like peptide, spexin-1, galanin peptide No No - - 2022-04-20 Yes
AGRG5 ADGRG5 ADGRG B2 Human Cryo-EM 7EQ1 - 3.3 R Active - 54 Gs αs - 60 - scFv16 Apo (no ligand)
none Apo (no ligand) - - No No Ping YQ, Xiao P, Yang F, Zhao RJ, Guo SC, Yan X, Wu X, Zhang C, Lu Y, Zhao F, Zhou F, Xi YT, Yin W, Liu FZ, He DF, Zhang DL, Zhu ZL, Jiang Y, Du L, Feng SQ, Schoneberg T, Liebscher I, Xu HE, Sun JP 10.1038/S41586-022-04619-Y 2022-05-11 Yes
SSR2 SST2 Somatostatin A Human Cryo-EM 7WIC - 2.8 R Active 100 78 Gi/o αi1 - 64 - scFv16 SOMATOSTATIN
protein Agonist SRIF-14, CST-17, cortistatin-14, SRIF-28 peptide No No Chen LN, Wang WW, Dong YJ, Shen DD, Guo J, Yu X, Qin J, Ji SY, Zhang H, Shen Q, He Q, Yang B, Zhang Y, Li Q, Mao C 10.1038/S41422-022-00669-Z 2022-06-01 Yes
CCKAR CCK1 Cholecystokinin A Human Cryo-EM 7XOU - 3.2 R Active 100 67 Gs αs - 58 - Nanobody-35 CCK-8
peptide Agonist desulfated cholecystokinin-8, CCK-33, CCK-8, CCK-58, CCK-4, CCK-39, gastrin-17 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 2022-07-20 Yes
5HT2C 5-HT2C 5-Hydroxytryptamine A Human Cryo-EM 8DPI - 3.4 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
AA2AR A2A Adenosine A Human Cryo-EM 7T32 7T32_refined 3.4 A Inactive 1 69 - - - - BRIL - ZM-241385
small-molecule Antagonist adenosine small-molecule No No Zhang K, Wu H, Hoppe N, Manglik A, Cheng Y 10.1038/S41467-022-32125-2 2022-08-10 Yes
GP119 GPR119 GPR18, GPR55 and GPR119 A Human Cryo-EM 7XZ6 - 2.8 R Active 100 87 Gs αs - 60 BRIL Nanobody-35 APD668
small-molecule Agonist N-oleoylethanolamide, SEA, anandamide, N-palmitoylethanolamine small-molecule No No Xu P, Huang S, Guo S, Yun Y, Cheng X, He X, Cai P, Lan Y, Zhou H, Jiang H, Jiang Y, Xie X, Xu HE 10.1038/S41594-022-00816-5 2022-08-24 Yes
AGRF1 ADGRF1 ADGRF B2 Human Cryo-EM 7WXU - 2.9 R Active - 30 Gq/11 αq - 60 - 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
AGRF1 ADGRF1 ADGRF B2 Human Cryo-EM 7X2V - 3.1 R Active - 30 Gi/o αi1 - 62 - 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
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-(1-8), [Met]enkephalin, endomorphin-1, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin B, endomorphin-2 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
OPSD Rhodopsin Opsins A Bovine X-ray 8A6C 8A6C_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
EDNRB ETB Endothelin A Human Cryo-EM 8HCX 8HCX_refined 3.5 C Active 100 66 Gq/11 αq - 61 - scFv16 ENDOTHELIN
protein Agonist endothelin-1, endothelin-2, endothelin-3 peptide No No - - 2023-03-22 Yes
DRD2 D2 Dopamine A Human Cryo-EM 8IRS - 3.0 R Active 100 60 Gi/o αi1 - 63 BRIL scFv16 rotigotine
small-molecule Agonist dopamine small-molecule No No Xu P, Huang S, Krumm BE, Zhuang Y, Mao C, Zhang Y, Wang Y, Huang XP, Liu YF, He X, Li H, Yin W, Jiang Y, Zhang Y, Roth BL, Xu HE 10.1038/S41422-023-00808-0 2023-06-07 Yes
PTH1R PTH1 Parathyroid hormone B1 Human Cryo-EM 8FLQ - 2.6 R Active 100 61 Gs αs - 59 - Nanobody-35 Parathyroid hormone
peptide Agonist PTH, PTHrP-(1-36), TIP39, PTHrP 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
GRPR BB2 Bombesin A Human Cryo-EM 8H0Q - 3.3 R Active 100 77 Gq/11 αq - 56 - - Gastrin-releasing peptide
peptide Agonist neuromedin B, gastrin releasing peptide(14-27) (human), gastrin-releasing peptide, neuromedin C, GRP-(18-27) peptide No No Li C, Xu Y, Liu H, Cai H, Jiang Y, Xu HE, Yin W 10.1038/S41422-022-00743-6 2023-08-09 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 6FK8 6FK8_refined 2.9 A Active 98 94 - - - - - - (2~{R},3~{S})-3-azanyl-2-(4-chlorophenyl)-1-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-yl-butan-1-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
NK1R NK1 Tachykinin A Human X-ray 6E59 6E59_refined 3.4 A Inactive 1 70 - - - - GlgA glycogen synthase - L760735
small-molecule Antagonist neurokinin B, neuropeptide-γ, hemokinin 1, substance P, neurokinin A, neuropeptide K peptide No No - 10.1073/PNAS.1812717115 2018-12-12 Yes
MTR1A MT1 Melatonin A Human X-ray 6ME3 6ME3_refined 2.9 A Inactive 1 82 - - - - GlgA glycogen synthase - CHEMBL15060
small-molecule Agonist melatonin small-molecule No No - - 2019-04-24 Yes
SUCR1 succinate Succinate A Rat X-ray 6IBB 6IBB_refined 2.1 A Active 65 93 - - - - - Nanobody-6 - - - - - No No - 10.1038/S41586-019-1663-8 2019-08-14 Yes
ADA2A α2A Adrenoceptors A Human X-ray 6KUY 6KUY_refined 3.2 A Inactive 1 56 - - - - BRIL - (2~{S})-4-fluoranyl-2-(1~{H}-imidazol-5-yl)-1-propan-2-yl-2,3-dihydroindole
small-molecule Agonist (partial) (-)-adrenaline, (-)-noradrenaline small-molecule No No - - 2019-12-04 Yes
APJ apelin Apelin A Human X-ray 6KNM 6KNM_refined 3.2 B Inactive 4 78 - - - - Rubredoxin - Single domain antibody JN241
protein Agonist apelin-13, apelin-17, apelin-36, Elabela/Toddler-21, [Pyr1]apelin-13, Elabela/Toddler-11, apelin receptor early endogenous ligand, Elabela/Toddler-32 peptide No No Ma Y, Ding Y, Song X, Ma X, Li X, Zhang N, Song Y, Sun Y, Shen Y, Zhong W, Hu LA, Ma Y, Zhang MY 10.1126/SCIADV.AAX7379 2020-01-29 Yes
VIPR1 VPAC1 VIP and PACAP B1 Human Cryo-EM 6VN7 6VN7_refined 3.2 R Active 100 58 Gs αs - 61 - Nanobody-35 [Ac-His1]PACAP-27
peptide Agonist VIP, PACAP-27, secretin, PHI, PHM, GHRH, PACAP-38 peptide No No Duan J, Shen DD, Zhou XE, Bi P, Liu QF, Tan YX, Zhuang YW, Zhang HB, Xu PY, Huang SJ, Ma SS, He XH, Melcher K, Zhang Y, Xu HE, Jiang Y 10.1038/S41467-020-17933-8 2020-09-02 Yes
NTR1 NTS1 Neurotensin A Rat Cryo-EM 7L0Q - 4.3 C Active 100 73 Gi/o αi1 - 95 - - neurotensin
peptide Agonist neuromedin N, neurotensin peptide No No Zhang M, Gui M, Wang ZF, Gorgulla C, Yu JJ, Wu H, Sun ZJ, Klenk C, Merklinger L, Morstein L, Hagn F, Pluckthun A, Brown A, Nasr ML, Wagner G 10.1038/S41594-020-00554-6 2021-01-06 Yes
DRD1 D1 Dopamine A Human Cryo-EM 7CKY - 3.2 R Active 100 62 Gs αs - 60 - Nanobody-35 CHEMBL3697578
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, 5-hydroxytryptamine, dopamine 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
V2R V2 Vasopressin and oxytocin A Human Cryo-EM 7BB7 - 4.4 A Active 100 72 Gs αs - 55 - Nanobody-35 vasopressin
peptide Agonist oxytocin, vasopressin peptide No No Bous J, Orcel H, Floquet N, Leyrat C, Lai-Kee-Him J, Gaibelet G, Ancelin A, Saint-Paul J, Trapani S, Louet M, Sounier R, Demene H, Granier S, Bron P, Mouillac B 10.1126/SCIADV.ABG5628 2021-06-02 Yes
CCR5 CCR5 Chemokine A Human Cryo-EM 7F1R - 3.0 R Active 100 79 Gi/o αi1 - 61 - - CCL5
peptide Agonist CCL2, CCL8, CCL11, CCL13, CCL14, CCL7, CCL5, CCL4, CCL16, CCL3 peptide No No - - 2021-07-14 Yes
GHSR ghrelin Ghrelin A Human Cryo-EM 7F9Y - 2.9 R Active 100 78 Gq/11 αq Engineered G alpha 59 - Nanobody-35 ghrelin
peptide Agonist [des-Gln14]ghrelin, ghrelin peptide No No Wang Y, Guo S, Zhuang Y, Yun Y, Xu P, He X, Guo J, Yin W, Xu HE, Xie X, Jiang Y 10.1038/S41467-021-25364-2 2021-08-18 Yes
BKRB2 B2 Bradykinin A Human Cryo-EM 7F2O - 2.9 R Active 100 73 Gq/11 αq Gq-Gi1 chimera 60 - scFv16 bradykinin
peptide Agonist [Hyp3]bradykinin, [des-Arg10]kallidin, bradykinin, Lys-[Hyp3]-bradykinin, kallidin, [des-Arg9]bradykinin, T-kinin peptide No No Yin YL, Ye C, Zhou F, Wang J, Yang D, Yin W, Wang MW, Xu HE, Jiang Y 10.1038/S41594-021-00645-Y 2021-10-13 Yes
MRGX2 MRGPRX2 A orphans A Human Cryo-EM 7VUY - 2.8 R Active 100 78 Gi/o αi1 - 64 - scFv16 PAMP-12
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
ADA1B α1B Adrenoceptors A Human X-ray 7B6W - 2.9 A Inactive 1 51 - - - - DARPin D12 - (+)-cyclazosin
small-molecule Inverse agonist (-)-adrenaline, (-)-noradrenaline 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
SSR2 SST2 Somatostatin A Human Cryo-EM 7T10 - 2.5 R Active 100 78 Gi/o αi3 - 62 - scFv16 SOMATOSTATIN
protein Agonist SRIF-14, CST-17, cortistatin-14, SRIF-28 peptide No No Robertson MJ, Meyerowitz JG, Panova O, Borrelli K, Skiniotis G 10.1038/S41594-022-00727-5 2022-03-09 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 β-CGRP, α-CGRP, calcitonin, calcitonin (salmon), amylin, adrenomedullin, 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
AGRL3 ADGRL3 ADGRL B2 Human Cryo-EM 7SF7 - 2.9 A Active - 19 G12/13 α13 Gi2-mini-G13 chimera 56 - - Apo (no ligand)
none Apo (no ligand) - - No No Barros-Alvarez X, Nwokonko RM, Vizurraga A, Matzov D, He F, Papasergi-Scott MM, Robertson MJ, Panova O, Yardeni EH, Seven AB, Kwarcinski FE, Su H, Peroto MC, Meyerowitz JG, Shalev-Benami M, Tall GG, Skiniotis G 10.1038/S41586-022-04575-7 2022-04-27 Yes
FPR1 FPR1 Formylpeptide A Human Cryo-EM 7EUO 7EUO_refined 2.9 R Active 100 84 Gi/o αi1 - 62 - scFv16 Peptide Agonist fMLF
peptide Agonist cathepsin G, spinorphin, annexin I, fMet-Leu-Phe peptide No No Chen G, Wang X, Liao Q, Ge Y, Jiao H, Chen Q, Liu Y, Lyu W, Zhu L, van Zundert GCP, Robertson MJ, Skiniotis G, Du Y, Hu H, Ye RD 10.1038/S41467-022-32822-Y 2022-05-25 Yes
DRD1 D1 Dopamine A Human Cryo-EM 7X2D 7X2D_refined 3.3 F Active 100 63 Gs αs - 58 - Nanobody-35 TAVAPADON
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, 5-hydroxytryptamine, dopamine small-molecule No No Teng X, Chen S, Nie Y, Xiao P, Yu X, Shao Z, Zheng S 10.1038/S41467-022-30929-W 2022-06-15 Yes
CCKAR CCK1 Cholecystokinin A Human Cryo-EM 7XOV - 3.0 R Active 100 67 Gs αs - 58 - Nanobody-35 SR146131
small-molecule Agonist desulfated cholecystokinin-8, CCK-33, CCK-8, CCK-58, CCK-4, CCK-39, gastrin-17 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 2022-07-20 Yes
SSR2 SST2 Somatostatin A Human Cryo-EM 7XAT 7XAT_refined 2.9 A Active 100 78 Gi/o αi1 - 63 - scFv16 SOMATOSTATIN
protein Agonist SRIF-14, CST-17, cortistatin-14, SRIF-28 peptide No No Bo Q, Yang F, Li Y, Meng X, Zhang H, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C 10.1038/S41421-022-00405-2 2022-08-31 Yes
AGRG2 ADGRG2 ADGRG B2 Mouse Cryo-EM 7XKD - 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
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 sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate 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
GPR17 GPR17 A orphans A Human Cryo-EM 7Y89 - 3.0 A Active 100 78 Gi/o αi1 - 58 - - Apo (no ligand)
none Apo (no ligand) LTE4, UDP-galactose, LTC4, ATP, LTD4, UDP-glucose, UDP small-molecule No No Ye F, Wong TS, Chen G, Zhang Z, Zhang B, Gan S, Gao W, Li J, Wu Z, Pan X, Du Y 10.1002/MCO2.159 2022-10-12 Yes
OPRM μ Opioid A Human Cryo-EM 8F7Q - 3.2 R Active 100 72 Gi/o αi1 - 64 - scFv16 β-endorphin
peptide Agonist dynorphin A-(1-8), [Met]enkephalin, endomorphin-1, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin B, endomorphin-2 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
AA2AR A2A Adenosine A Human X-ray 8GNE - 2.3 A Inactive 1 72 - - - - BRIL - Sipagladenant
small-molecule Inverse agonist adenosine small-molecule No Yes - 10.1124/MOLPHARM.122.000633 2023-03-22 Yes
FSHR FSH Glycoprotein hormone A Human Cryo-EM 8I2G - 2.8 R Active 100 86 Gs αs fused Gs 58 - Nanobody-35 Glycoprotein alpha
Follitropin subunit beta
FSHR agonist 1
peptide
peptide
small-molecule		 Agonist FSH peptide No No - - 2023-03-29 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 6FKB 6FKB_refined 3.0 A Active 98 94 - - - - - - 2-(4-Chlorophenyl)-1-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-yl-ethanone
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
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 6H7J 6H7J_refined 2.8 A Active 99 60 - - - - Thioredoxin 1 Camelid antibody fragment Nb80 LEVISOPRENALINE
small-molecule Agonist - - No No Warne T, Edwards PC, Dore AS, Leslie AGW, Tate CG 10.1126/SCIENCE.AAU5595 2018-10-17 Yes
TA2R TP Prostanoid A Human X-ray 6IIV 6IIV_refined 3.0 A Inactive 35 87 - - - - Rubredoxin - daltroban
small-molecule Antagonist PGE2, PGF2α, thromboxane A2, PGH2, PGI2, PGD2 small-molecule No No - - 2018-12-19 Yes
ACM2 M2 Acetylcholine (muscarinic) A Human Cryo-EM 6OIK 6OIK_refined 3.6 R Active 100 60 Gi/o αo - 61 - - LY2119620
iperoxo
small-molecule
small-molecule		 Ago-PAM
Agonist		 acetylcholine small-molecule No No - - 2019-05-08 Yes
DRD4 D4 Dopamine A Mouse X-ray 6IQL 6IQL_refined 3.5 A Inactive 15 65 - - - - BRIL - L745870
small-molecule Antagonist - - No No Zhou Y, Cao C, He L, Wang X, Zhang XC 10.7554/ELIFE.48822 2019-12-04 Yes
CNR2 CB2 Cannabinoid A Human Cryo-EM 6KPF 6KPF_refined 2.9 R Active 100 81 Gi/o αi1 - 62 - scFv16 AM12033
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
GLR glucagon Glucagon B1 Human Cryo-EM 6WHC 6WHC_refined 3.4 R Active 100 78 Gs αs - 56 - Nanobody-35 Dual-agonist peptide P15
peptide Agonist glucagon peptide No No Chang R, Zhang X, Qiao A, Dai A, Belousoff MJ, Tan Q, Shao L, Zhong L, Lin G, Liang YL, Ma L, Han S, Yang D, Danev R, Wang MW, Wootten D, Wu B, Sexton PM 10.1074/JBC.RA120.013793 2020-05-27 Yes
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 6X18 - 2.1 R Active 100 83 Gs αs - 90 - Nanobody-35 CHEMBL410972
protein Agonist glucagon, glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide 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
LT4R1 BLT1 Leukotriene A Human X-ray 7K15 7K15_refined 2.9 A Inactive 5 85 - - - - Flavodoxin - N-(tert-butylsulfonyl)-4-fluoro-2-{(3S,4R)-4-hydroxy-3-[(pyridin-2-yl)methyl]-3,4-dihydro-2H-1-benzopyran-7-yl}benzamide
small-molecule Antagonist 12R-HETE, LTB4, 20-hydroxy-LTB4 small-molecule No Yes Michaelian N, Sadybekov A, Besserer-Offroy E, Han GW, Krishnamurthy H, Zamlynny BA, Fradera X, Siliphaivanh P, Presland J, Spencer KB, Soisson SM, Popov P, Sarret P, Katritch V, Cherezov V 10.1038/S41467-021-23149-1 2021-02-17 Yes
CASR CaS Calcium-sensing C Human Cryo-EM 7DTW 7DTW_refined 4.5 A Inactive - 72 - - - - - - Apo (no ligand)
none Apo (no ligand) spermine, L-tryptophan, Ca2+, Mg2+ 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
OPSD Rhodopsin Opsins A Bovine Cryo-EM 7MT8 7MT8_refined 5.8 R Active 98 93 - - - - - GRK1 Retinal (all-trans)
small-molecule Agonist - - No No - 10.1038/S41586-021-03721-X 2021-07-07 Yes
CCKAR CCK1 Cholecystokinin A Human Cryo-EM 7EZH - 3.2 D Active 100 69 Gi/o αi1 - 61 - scFv16 CCK-8
peptide Agonist desulfated cholecystokinin-8, CCK-33, CCK-8, CCK-58, CCK-4, CCK-39, gastrin-17 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
MC4R MC4 Melanocortin A Human Cryo-EM 7F55 - 3.1 R Active 100 82 Gs αs - 58 - Nanobody-35 bremelanotide
peptide Agonist agouti-related protein, β-MSH, α-MSH, γ-MSH, ACTH 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
NK1R NK1 Tachykinin A Human Cryo-EM 7P00 - 2.7 R Active 100 71 Gq/11 αq Gq-Gs-Gi1 chimera 59 - scFv16 substance P
peptide Agonist neurokinin B, neuropeptide-γ, hemokinin 1, substance P, neurokinin A, neuropeptide K peptide No No - - 2021-12-15 Yes
MSHR MC1 Melanocortin A Human Cryo-EM 7F4F - 2.9 R Active 100 85 Gs αs - 59 - scFv16 CHEMBL407070
protein Agonist γ-MSH, ACTH, β-MSH, α-MSH peptide No No - - 2021-09-08 Yes
CALCR CT Calcitonin B1 Human Cryo-EM 7TYF - 2.2 R Active 100 77 Gs αs - 58 - Nanobody-35
RAMP1		 amylin peptide
peptide Agonist β-CGRP, α-CGRP, calcitonin, calcitonin (salmon), amylin, adrenomedullin, 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
GIPR GIP Glucagon B1 Human Cryo-EM 7RA3 - 3.2 R Active 100 80 Gs αs Engineered G alpha 56 - scFv16
Nanobody-35		 gastric inhibitory polypeptide (human) - Incretin
peptide Agonist 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
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
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 6H7L 6H7L_refined 2.7 A Active 99 60 - - - - Thioredoxin 1 Camelid antibody fragment Nb6B9 Dobutamine
small-molecule Agonist - - No No Warne T, Edwards PC, Dore AS, Leslie AGW, Tate CG 10.1126/SCIENCE.AAU5595 2018-10-17 Yes
NK1R NK1 Tachykinin A Human X-ray 6HLL 6HLL_refined 3.3 A Inactive 1 67 - - - - GlgA glycogen synthase - CP 99994
small-molecule Antagonist neurokinin B, neuropeptide-γ, hemokinin 1, substance P, neurokinin A, neuropeptide K peptide No No - 10.1038/S41467-018-07939-8 2019-01-16 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 6E67 6E67_refined 3.7 B Active 100 72 Gs αs Fused partial Gs 44 T4-Lysozyme - CHEMBL1615159
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ small-molecule No No - 10.1016/J.CELL.2019.04.021 2019-06-05 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 6PS3 6PS3_refined 2.5 A Inactive 0 68 - - - - T4-Lysozyme - CHEMBL3799125
small-molecule Antagonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ small-molecule No No - - 2019-11-13 Yes
CRFR1 CRF1 Corticotropin-releasing factor B1 Human Cryo-EM 6P9X - 2.9 R Active 100 65 Gs αs - 49 - Nanobody-35 Corticoliberin
peptide Agonist urocortin 2, corticotrophin-releasing hormone, urocortin 1 peptide No No Liang YL, Belousoff MJ, Zhao P, Koole C, Fletcher MM, Truong TT, Julita V, Christopoulos G, Xu HE, Zhang Y, Khoshouei M, Christopoulos A, Danev R, Sexton PM, Wootten D 10.1016/J.MOLCEL.2020.01.012 2020-02-05 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 6PGS 6PGS_refined 2.9 A Active 100 94 Gi/o αt2 Only H5 3 - - Geraniol
small-molecule unknown - - No No - - 2020-07-01 Yes
OXYR OT Vasopressin and oxytocin A Human X-ray 6TPK 6TPK_refined 3.2 A Inactive 15 68 - - - - GlgA glycogen synthase - retosiban
small-molecule Antagonist oxytocin, vasopressin peptide No No Waltenspuhl Y, Schoppe J, Ehrenmann J, Kummer L, Pluckthun A 10.1126/SCIADV.ABB5419 2020-08-05 Yes
5HT2A 5-HT2A 5-Hydroxytryptamine A Human Cryo-EM 6WHA - 3.4 A Active 100 52 Gq/11 αq Gq-Gi2-Gs chimera 57 BRIL scFv16 CHEMBL5184791
small-molecule Agonist 5-hydroxytryptamine, tryptamine small-molecule No No Kim K, Che T, Panova O, DiBerto JF, Lyu J, Krumm BE, Wacker D, Robertson MJ, Seven AB, Nichols DE, Shoichet BK, Skiniotis G, Roth BL 10.1016/J.CELL.2020.08.024 2020-09-23 Yes
ADRB1 β1 Adrenoceptors A Human X-ray 7BU7 7BU7_refined 2.6 A Active 99 58 - - - - T4-Lysozyme Camelid antibody fragment Nb6B9 CHEMBL1615159
small-molecule Agonist noradrenaline, (-)-adrenaline, L-NOREPINEPHRINE, (-)-noradrenaline 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
NTR1 NTS1 Neurotensin A Rat X-ray 6YVR - 2.5 B Inactive 3 83 - - - - DARPin D12 - JMV431
peptide 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
GRM2 mGlu2 Metabotropic glutamate C Human X-ray 7EPF 7EPF_refined 2.7 A Inactive - 28 - - - - Flavodoxin - (8~{R})-4-[2,4-Bis(fluoranyl)phenyl]-8-methyl-7-[(2-methylpyrazol-3-yl)methyl]-6,8-dihydro-5~{H}-1,7-naphthyridine-2-carboxamide
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
CCR5 CCR5 Chemokine A Human X-ray 7F1T - 2.6 A Inactive 16 86 - - - - Rubredoxin - CCL3
peptide Agonist CCL2, CCL8, CCL11, CCL13, CCL14, CCL7, CCL5, CCL4, CCL16, CCL3 peptide No No - - 2021-07-14 Yes
MRGX2 MRGPRX2 A orphans A Human Cryo-EM 7VDL - 3.2 R Active 100 78 Gi/o αi1 - 61 - scFv16 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
5HT2A 5-HT2A 5-Hydroxytryptamine A Human X-ray 7WC6 7WC6_refined 2.6 A Inactive 1 58 - - - - BRIL - Lysergide
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
AGTR2 AT2 Angiotensin A Human X-ray 7JNI 7JNI_refined 3.0 A Active 99 82 - - - - BRIL - olodanrigan
small-molecule Antagonist angiotensin-(1-7), angiotensin II, angiotensin III peptide No No Perryman R, Renziehausen A, Shaye H, Kostagianni AD, Tsiailanis AD, Thorne T, Chatziathanasiadou MV, Sivolapenko GB, El Mubarak MA, Han GW, Zarzycka B, Katritch V, Lebon G, Lo Nigro C, Lattanzio L, Morse SV, Choi JJ, O'Neill K, Kanaki Z, Klinakis A, Crook T, Cherezov V, Tzakos AG, Syed N 10.1073/PNAS.2116289119 2022-02-09 Yes
CCR1 CCR1 Chemokine A Human Cryo-EM 7VL9 - 2.6 R Active 100 85 Gi/o αi1 - 62 - scFv16 CCL15(26-92)
peptide Agonist CCL8, CCL13, CCL14, CCL16, CCL5, CCL7, CCL4, CCL23, CCL15, CCL3 peptide No No Shao Z, Shen Q, Yao B, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Ma H, Chen ZH, Xu HE, Ying S, Zhang Y, Shen H 10.1038/S41589-021-00918-Z 2022-03-23 Yes
AGRG2 ADGRG2 ADGRG B2 Mouse Cryo-EM 7WUI - 3.1 R Active - 24 Gs αs Mini-Gs 58 - - IP15
peptide Agonist - - No No Xiao P, Guo S, Wen X, He QT, Lin H, Huang SM, Gou L, Zhang C, Yang Z, Zhong YN, Yang CC, Li Y, Gong Z, Tao XN, Yang ZS, Lu Y, Li SL, He JY, Wang C, Zhang L, Kong L, Sun JP, Yu X 10.1038/S41586-022-04590-8 2022-04-27 Yes
DRD1 D1 Dopamine A Human Cryo-EM 7F23 - 3.6 F Active 100 62 Gs αs - 60 - Nanobody-35 dopamine
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, 5-hydroxytryptamine, dopamine 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
5HT4R 5-HT4 5-Hydroxytryptamine A Human Cryo-EM 7XTA 7XTA_refined 3.2 R Active 100 73 Gi/o αi1 - 62 BRIL scFv16 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
SSR2 SST2 Somatostatin A Human Cryo-EM 7XAU - 3.0 A Active 100 76 Gi/o αi1 - 63 - scFv16 Octreotide
peptide Agonist SRIF-14, CST-17, cortistatin-14, SRIF-28 peptide No No Bo Q, Yang F, Li Y, Meng X, Zhang H, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C 10.1038/S41421-022-00405-2 2022-08-31 Yes
PTH1R PTH1 Parathyroid hormone B1 Human Cryo-EM 7VVN 7VVN_refined 3.8 R Active 100 51 Gs αs - 58 - Nanobody-35 teriparatide
peptide Agonist PTH, PTHrP-(1-36), TIP39, PTHrP 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
OPRM μ Opioid A Mouse Cryo-EM 7T2H - 3.2 D Active 100 71 Gi/o αi1 - 61 - scFv16 LOFENTANIL
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 7WYB - 3.0 R Active - 17 Gi/o αi1 - 64 - scFv16 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 7YU7 - 3.8 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
PTH1R PTH1 Parathyroid hormone B1 Human Cryo-EM 8HA0 - 2.6 R Active 100 61 Gs αs - 60 - Nanobody-35 teriparatide
peptide Agonist PTH, PTHrP-(1-36), TIP39, PTHrP peptide No No Zhao LH, Yuan QN, Dai AT, He XH, Chen CW, Zhang C, Xu YW, Zhou Y, Wang MW, Yang DH, Xu HE 10.1038/S41401-022-01032-Z 2022-12-21 Yes
AA2BR A2B Adenosine A Human Cryo-EM 8HDP - 3.2 R Active 100 84 Gs αs Mini-Gs 60 - Nanobody-35 adenosine
small-molecule Agonist adenosine small-molecule No No - - 2023-01-18 Yes
NMUR2 NMU2 Neuromedin U A Human Cryo-EM 7XK8 7XK8_refined 3.3 R Active 100 68 Gi/o αi1 - 64 - - Neuromedin U-25 (human)
peptide Agonist neuromedin U-25, neuromedin U-23, neuromedin S-33, neuromedin S-36 peptide No No Zhao W, Zhang W, Wang M, Lu M, Chen S, Tang T, Schnapp G, Wagner H, Brennauer A, Yi C, Chu X, Han S, Wu B, Zhao Q 10.1038/S41467-022-34814-4 2023-02-22 Yes
OPRK κ Opioid A Human Cryo-EM 8DZQ 8DZQ_refined 2.8 A Active 100 72 Gi/o αo - 61 - scFv16 SALVINORIN B METHOXYMETHYL ETHER
small-molecule Agonist dynorphin A-(1-8), β-neoendorphin, big dynorphin, [Met]enkephalin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin B, α-neoendorphin peptide No No Han J, Zhang J, Nazarova AL, Bernhard SM, Krumm BE, Zhao L, Lam JH, Rangari VA, Majumdar S, Nichols DE, Katritch V, Yuan P, Fay JF, Che T 10.1038/S41586-023-06030-7 2023-05-03 Yes
CNR1 CB1 Cannabinoid A Human Cryo-EM 8GHV 8GHV_refined 2.8 D Active 100 59 Gi/o αi1 - 62 - scFv16 CHEMBL4208628
small-molecule Agonist 2-arachidonoylglycerol, anandamide small-molecule No No Krishna Kumar K, Robertson MJ, Thadhani E, Wang H, Suomivuori CM, Powers AS, Ji L, Nikas SP, Dror RO, Inoue A, Makriyannis A, Skiniotis G, Kobilka B 10.1038/S41467-023-37864-4 2023-05-24 Yes
PTH1R PTH1 Parathyroid hormone B1 Human Cryo-EM 8GW8 - 2.9 R Active 100 37 Gs αs - 58 - Nanobody-35 PCO371
small-molecule Agonist PTH, PTHrP-(1-36), TIP39, PTHrP peptide No No Kobayashi K, Kawakami K, Kusakizako T, Tomita A, Nishimura M, Sawada K, Okamoto HH, Hiratsuka S, Nakamura G, Kuwabara R, Noda H, Muramatsu H, Shimizu M, Taguchi T, Inoue A, Murata T, Nureki O 10.1038/S41586-023-06169-3 2023-06-14 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
GRM2 mGlu2 Metabotropic glutamate C Human Cryo-EM 8JD4 - 2.9 2 Active - 84 - - - - - - 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
AA2AR A2A Adenosine A Human Cryo-EM 6GDG 6GDG_refined 4.1 A Active 100 64 Gs αs - 57 TrxA Nanobody-35 NECA
small-molecule Agonist adenosine small-molecule No No Garcia-Nafria J, Lee Y, Bai X, Carpenter B, Tate CG 10.7554/ELIFE.35946 2018-05-16 Yes
PE2R3 EP3 Prostanoid A Human X-ray 6M9T 6M9T_refined 2.5 A Active 91 70 - - - - T4-Lysozyme - Misoprostol-FA
small-molecule Agonist PGE2, PGF2α, thromboxane A2, PGI2, PGE1, PGD2 small-molecule No No - 10.1038/S41589-018-0160-Y 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 - - 2019-04-24 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 6PRZ 6PRZ_refined 2.8 A Inactive 0 68 - - - - T4-Lysozyme - CHEMBL1160734
small-molecule Antagonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ small-molecule No No - 10.1107/S2052252519013137 2019-11-13 Yes
CLTR2 CysLT2 Leukotriene A Human X-ray 6RZ9 6RZ9_refined 2.7 A Intermediate 44 81 - - - - BRIL - ONO-2770372
small-molecule Antagonist LTE4, LTD4, LTC4 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
AGTR1 AT1 Angiotensin A Human X-ray 6OS1 - 2.8 A Active 95 85 - - - - BRIL Nanobody-Nb.AT110i1_le TRV023
peptide Agonist angiotensin A, angiotensin III, angiotensin IV, angiotensin II peptide No No Wingler LM, Skiba MA, McMahon C, Staus DP, Kleinhenz ALW, Suomivuori CM, Latorraca NR, Dror RO, Lefkowitz RJ, Kruse AC 10.1126/SCIENCE.AAY9813 2020-02-19 Yes
GABR2 GABAB2 GABAB C Human Cryo-EM 6UOA - 6.3 B Intermediate - 71 - - - - - - Apo (no ligand)
none Apo (no ligand) - - No No - - 2020-06-10 Yes
SCTR secretin Glucagon B1 Human Cryo-EM 6WZG 6WZG_refined 2.3 R Active 100 86 Gs αs - 61 - Nanobody-35 SECRETIN
protein Agonist secretin, VIP 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
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 7CKZ - 3.1 R Active 100 62 Gs αs - 60 - Nanobody-35 dopamine
mevidalen
small-molecule
small-molecule		 Agonist
PAM		 noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, 5-hydroxytryptamine, dopamine 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
GRM2 mGlu2 Metabotropic glutamate C Human Cryo-EM 7E9G - 3.5 R Intermediate - 88 Gi/o αi1 - 63 - scFv16 eglumegad
JNJ-40411813
small-molecule
small-molecule		 Agonist
PAM		 L-glutamic acid small-molecule No No - - 2021-06-23 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
MRGX4 MRGPRX4 A orphans A Human Cryo-EM 7S8P 7S8P_refined 2.6 R Active 100 77 Gq/11 αq Gq-Gs chimera 57 BRIL scFv16 N-[(1r,3R,5S,7R)-3,5-dimethyltricyclo[3.3.1.1~3,7~]decane-1-carbonyl]-D-phenylalanine
small-molecule Agonist - - 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
MRGX2 MRGPRX2 A orphans A Human Cryo-EM 7VV6 7VV6_refined 3.3 R Active 97 82 - - - - - - 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
5HT2A 5-HT2A 5-Hydroxytryptamine A Human X-ray 7WC7 7WC7_refined 2.6 A Inactive 1 59 - - - - BRIL - lisuride
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
MSHR MC1 Melanocortin A Human Cryo-EM 7F4H - 2.7 R Active 100 84 Gs αs - 59 - Nanobody-35
scFv16		 CHEMBL407070
protein Agonist γ-MSH, ACTH, 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 β-CGRP, α-CGRP, calcitonin, calcitonin (salmon), amylin, adrenomedullin, 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
NMUR1 NMU1 Neuromedin U A Human Cryo-EM 7W53 - 3.2 R Active 100 62 Gq/11 αq - 54 - scFv16 Neuromedin U-25 (human)
peptide Agonist neuromedin U-25, neuromedin U-23, 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
APJ apelin Apelin A Human X-ray 7SUS 7SUS_refined 2.7 A Inactive 4 76 - - - - Rubredoxin - (1R,2S)-N-[4-(2,6-dimethoxyphenyl)-5-(6-methylpyridin-2-yl)-1,2,4-triazol-3-yl]-1-(5-methylpyrimidin-2-yl)-1-oxidanyl-propane-2-sulfonamide
small-molecule Agonist apelin-13, apelin-17, apelin-36, Elabela/Toddler-21, [Pyr1]apelin-13, Elabela/Toddler-11, apelin receptor early endogenous ligand, Elabela/Toddler-32 peptide No No Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F 10.1038/S41594-022-00797-5 2022-07-27 Yes
ACKR3 ACKR3 Chemokine A Human Cryo-EM 7SK9 7SK9_refined 3.7 A Active 95 78 - - - - - CID24 Fab heavy chain
CID24 Fab light chain		 (1R)-4-[7-(3-carboxypropoxy)-6-methylquinolin-8-yl]-1-{[2-(4-hydroxypiperidin-1-yl)-1,3-thiazol-4-yl]methyl}-1,4-diazepan-1-ium
small-molecule Agonist (partial) 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
CCR3 CCR3 Chemokine A Human Cryo-EM 7X9Y 7X9Y_refined 3.1 R Active 100 83 Gi/o αi1 - 62 - scFv16 Apo (no ligand)
none Apo (no ligand) CCL2, CCL8, CCL11, CXCL9, CCL13, CCL24, CCL5, CCL7, CXCL10, CXCL11, CCL26, CCL15, CCL28 peptide No No Shao Z, Tan Y, Shen Q, Hou L, Yao B, Qin J, Xu P, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Chen ZH, Jiang Y, Xu HE, Ying S, Ma H, Zhang Y, Shen H 10.1038/S41421-022-00403-4 2022-08-24 Yes
GP119 GPR119 GPR18, GPR55 and GPR119 A Human Cryo-EM 7XZ5 - 3.1 R Active 100 87 Gs αs - 60 BRIL Nanobody-35 (4R,7R,18E)-4,7-dihydroxy-N,N,N-trimethyl-10-oxo-3,5,9-trioxa-4-phosphaheptacos-18-en-1-aminium 4-oxide
small-molecule Agonist N-oleoylethanolamide, SEA, anandamide, N-palmitoylethanolamine small-molecule No No Xu P, Huang S, Guo S, Yun Y, Cheng X, He X, Cai P, Lan Y, Zhou H, Jiang H, Jiang Y, Xie X, Xu HE 10.1038/S41594-022-00816-5 2022-08-24 Yes
AGRF1 ADGRF1 ADGRF B2 Human Cryo-EM 7WY0 - 2.8 R Active - 30 G12/13 α13 - 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
TRFR TRH1 Thyrotropin-releasing hormone A Human Cryo-EM 7XW9 - 2.7 R Active 100 72 Gq/11 αq - 58 - scFv16 TRH
peptide Agonist TRH peptide No No - - 2022-12-28 Yes
ACM3 M3 Acetylcholine (muscarinic) A Human Cryo-EM 8E9Y - 2.8 A Active 100 47 Gq/11 αq Mini-Gq 56 - scFv16 Clozapine N-oxide
small-molecule Agonist acetylcholine small-molecule No No Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL 10.1038/S41586-022-05489-0 2022-11-30 Yes
RL3R2 RXFP4 Relaxin family peptide A Human Cryo-EM 7YK6 7YK6_refined 3.0 R Active 100 76 Gi/o αi2 - 59 - scFv16 CHEMBL4522365
small-molecule Agonist relaxin-3, INSL5, relaxin-3 (B chain) peptide No No Chen Y, Zhou Q, Wang J, Xu Y, Wang Y, Yan J, Wang Y, Zhu Q, Zhao F, Li C, Chen CW, Cai X, Bathgate RAD, Shen C, Eric Xu H, Yang D, Liu H, Wang MW 10.1038/S41467-023-36182-Z 2023-03-01 Yes
FFAR4 FFA4 Free fatty acid A Human Cryo-EM 8G59 8G59_refined 2.6 R Active 100 78 Gq/11 αq - 61 - - TUG-891
small-molecule Agonist linoleic acid, oleic acid, α-linolenic acid, myristic acid small-molecule No No - 10.1126/SCIENCE.ADD6220 2023-03-08 Yes
ACM2 M2 Acetylcholine (muscarinic) A Human Cryo-EM 7T90 7T90_refined 3.3 A Active 100 59 Gi/o αo - 62 - scFv16 acetylcholine
small-molecule Agonist acetylcholine small-molecule No No - - 2023-01-25 Yes
OPRK κ Opioid A Human Cryo-EM 8DZR - 2.6 A Active 100 68 Gi/o αgust - 58 - scFv16 CHEMBL277863
small-molecule Agonist dynorphin A-(1-8), β-neoendorphin, big dynorphin, [Met]enkephalin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin B, α-neoendorphin peptide No No Han J, Zhang J, Nazarova AL, Bernhard SM, Krumm BE, Zhao L, Lam JH, Rangari VA, Majumdar S, Nichols DE, Katritch V, Yuan P, Fay JF, Che T 10.1038/S41586-023-06030-7 2023-05-03 Yes
C5AR1 C5a1 Complement peptide A Human Cryo-EM 7Y64 - 2.9 D Active 100 84 Gi/o αi1 - 63 - scFv16 C5a anaphylatoxin
peptide Agonist C3a, C5a, ribosomal protein S19, C5a des-Arg 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 8H4L - 3.1 R Active 100 84 Gq/11 αq - 60 - Nanobody-35 docosahexaenoic acid
small-molecule Agonist linoleic acid, oleic acid, α-linolenic acid, myristic acid small-molecule No No Yin H, Inoue A, Ma Z, Zhu X, Xia R, Xu Z, Wang N, Duan Y, Zhang A, Guo C, He Y 10.1038/S41422-023-00835-X 2023-06-21 Yes
GRM2 mGlu2 Metabotropic glutamate C Human Cryo-EM 8JD0 - 3.3 2 Inactive - 88 - - - - - - L-glutamic acid
CHEMBL3894759
small-molecule
small-molecule		 Agonist
NAM		 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
OPRK κ Opioid A Human X-ray 7YIT - 3.3 A Active 100 74 - - - - BRIL Nanobody-39 nalfurafine
small-molecule Agonist dynorphin A-(1-8), β-neoendorphin, big dynorphin, [Met]enkephalin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin B, α-neoendorphin peptide No No El Daibani A, Paggi JM, Kim K, Laloudakis YD, Popov P, Bernhard SM, Krumm BE, Olsen RHJ, Diberto J, Carroll FI, Katritch V, Wunsch B, Dror RO, Che T 10.1038/S41467-023-37041-7 2023-04-12 Yes
OPRK κ Opioid A Human Cryo-EM 8DZP - 2.7 A Active 100 74 Gi/o αi1 - 60 - scFv16 SALVINORIN B METHOXYMETHYL ETHER
small-molecule Agonist dynorphin A-(1-8), β-neoendorphin, big dynorphin, [Met]enkephalin, dynorphin A, [Leu]enkephalin, β-endorphin, dynorphin A-(1-13), dynorphin B, α-neoendorphin peptide No No - - 2023-05-03 Yes
DRD5 D5 Dopamine A Human Cryo-EM 8IRV 8IRV_refined 3.1 R Active 100 58 Gs αs - 60 BRIL - rotigotine
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, 5-hydroxytryptamine, dopamine small-molecule No No Xu P, Huang S, Krumm BE, Zhuang Y, Mao C, Zhang Y, Wang Y, Huang XP, Liu YF, He X, Li H, Yin W, Jiang Y, Zhang Y, Roth BL, Xu HE 10.1038/S41422-023-00808-0 2023-06-07 Yes
ADA1A α1A Adrenoceptors A Human Cryo-EM 7YMH 7YMH_refined 3.5 A Active 100 58 Gq/11 αq Mini-Gq 51 - Nanobody-29 Noradrenaline
small-molecule Agonist (-)-adrenaline, (-)-noradrenaline small-molecule No No - - 2023-07-05 Yes
DRD4 D4 Dopamine A Human Cryo-EM 8IRU - 3.2 R Active 100 64 Gi/o αi1 - 60 - scFv16 rotigotine
small-molecule Agonist dopamine small-molecule No No Xu P, Huang S, Krumm BE, Zhuang Y, Mao C, Zhang Y, Wang Y, Huang XP, Liu YF, He X, Li H, Yin W, Jiang Y, Zhang Y, Roth BL, Xu HE 10.1038/S41422-023-00808-0 2023-06-21 Yes
5HT6R 5-HT6 5-Hydroxytryptamine A Human Cryo-EM 8JLZ - 3.1 R Active 100 61 Gs αs - 58 - Nanobody-35 CHEMBL365751
small-molecule Agonist 5-hydroxytryptamine small-molecule No No Pei Y, Wen X, Guo SC, Yang ZS, Zhang R, Xiao P, Sun JP 10.1016/J.BBRC.2023.05.126 2023-06-28 Yes
ADA1A α1A Adrenoceptors A Human Cryo-EM 8THK - 2.6 R Active 100 52 Gq/11 αq - 55 T4-Lysozyme scFv16 CHEMBL133451
small-molecule Agonist (-)-adrenaline, (-)-noradrenaline small-molecule No No Su M, Wang J, Xiang G, Do HN, Levitz J, Miao Y, Huang XY 10.1038/S41467-023-40524-2 2023-08-16 Yes
GPR20 GPR20 A orphans A Human Cryo-EM 8HS2 8HS2_refined 3.1 R Active 65 80 - - - - BRIL Antibody fab fragment heavy chain
Antibody fab fragment light chain		 Apo (no ligand)
none Apo (no ligand) - - No No - 10.1038/S41421-023-00520-8 2023-03-08 Yes
GRPR BB2 Bombesin A Human X-ray 7W41 7W41_refined 3.0 A Inactive 4 75 - - - - GlgA glycogen synthase - PD 176252
small-molecule Antagonist neuromedin B, gastrin releasing peptide(14-27) (human), gastrin-releasing peptide, neuromedin C, GRP-(18-27) peptide No No Peng S, Zhan Y, Zhang D, Ren L, Chen A, Chen ZF, Zhang H 10.1073/PNAS.2216230120 2023-02-22 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 7XKA - 3.1 A Active 99 69 - - - - T4-Lysozyme Antibody fragment (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, (-)-adrenaline, Zn2+ small-molecule No No - - 2023-04-26 Yes
GPR12 GPR12 A orphans A Human Cryo-EM 7Y3G 7Y3G_refined 2.8 R Active 100 78 Gs αs - 56 - Nanobody-35 Apo (no ligand)
none Apo (no ligand) sphingosine 1-phosphate small-molecule No No Li H, Zhang J, Yu Y, Luo F, Wu L, Liu J, Chen N, Liu Z, Hua T 10.1016/J.SCIB.2022.12.023 2023-06-07 Yes
C3AR C3a Complement peptide A Human Cryo-EM 8IA8 - 2.9 A Active 100 59 Gi/o αi1 - 61 - scFv16 ALA-SER-LYS-LEU-GLY-LEU-ALA-ARG
peptide Agonist C3a, C5a peptide No No - - 2023-05-24 Yes
ADA1A α1A Adrenoceptors A Human Cryo-EM 7YM8 7YM8_refined 2.9 A Active 100 58 Gq/11 αq Mini-Gq 46 - Nanobody-29 oxymetazoline
small-molecule Agonist (-)-adrenaline, (-)-noradrenaline small-molecule No No Toyoda Y, Zhu A, Kong F, Shan S, Zhao J, Wang N, Sun X, Zhang L, Yan C, Kobilka BK, Liu X 10.1038/S41467-023-39310-X 2023-07-05 Yes
DRD1 D1 Dopamine A Human Cryo-EM 8IRR - 3.2 R Active 100 63 Gs αs Mini-Gs 57 - Nanobody-35 rotigotine
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, (-)-noradrenaline, 5-hydroxytryptamine, dopamine small-molecule No No Xu P, Huang S, Krumm BE, Zhuang Y, Mao C, Zhang Y, Wang Y, Huang XP, Liu YF, He X, Li H, Yin W, Jiang Y, Zhang Y, Roth BL, Xu HE 10.1038/S41422-023-00808-0 2023-06-21 Yes
PTH1R PTH1 Parathyroid hormone B1 Human Cryo-EM 8JR9 - 2.6 R Active 100 43 Gs αs - 59 - Nanobody-35 PCO371
small-molecule Agonist PTH, PTHrP-(1-36), TIP39, PTHrP peptide No No Zhao LH, He Q, Yuan Q, Gu Y, He X, Shan H, Li J, Wang K, Li Y, Hu W, Wu K, Shen J, Xu HE 10.1038/S41586-023-06467-W 2023-08-02 Yes
FFAR4 FFA4 Free fatty acid A Human Cryo-EM 8ID8 - 3.0 R Active 100 81 Gi/o αi1 - 64 - scFv16 TUG-891
small-molecule Agonist linoleic acid, oleic acid, α-linolenic acid, myristic acid small-molecule No No - 10.1126/SCIENCE.ADD6220 2023-03-15 Yes
P2Y12 P2Y12 P2Y A Human Cryo-EM 7XXI 7XXI_refined 3.0 A Active 100 86 Gi/o αi2 - 61 - - 2MeSADP
small-molecule Agonist ADP, ATP small-molecule No No - - 2023-06-07 Yes
FFAR1 FFA1 Free fatty acid A Human Cryo-EM 8EJC - 3.0 R Active 100 90 Gq/11 αq - 60 - scFv16 fasiglifam
small-molecule Agonist oleic acid, docosahexaenoic acid, α-linolenic acid, myristic acid small-molecule No No Kumari P, Inoue A, Chapman K, Lian P, Rosenbaum DM 10.1073/PNAS.2219569120 2023-05-24 Yes
CNR2 CB2 Cannabinoid A Human Cryo-EM 8GUR 8GUR_refined 2.8 R Active 100 78 Gi/o αi1 - 64 - scFv16 CP55940
small-molecule Agonist 2-arachidonoylglycerol, anandamide 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
AA2AR A2A Adenosine A Human X-ray 8C9W - 2.1 A Inactive 1 72 - - - - 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 2023-07-12 Yes
GPR84 GPR84 A orphans A Human Cryo-EM 8J19 - 3.2 R Active 100 71 Gi/o αi1 - 62 - scFv16 6-nonylpyridine-2,4-diol
small-molecule Agonist - - 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
NTR1 NTS1 Neurotensin A Human Cryo-EM 8JPC - 3.1 R Active 100 71 Gq/11 αq GRK2 bound 88 - GRK2 JMV431
CHEMBL4576388
peptide
small-molecule		 Agonist
PAM		 neuromedin N, large neurotensin, neurotensin, large neuromedin N peptide No No Duan J, Liu H, Zhao F, Yuan Q, Ji Y, Cai X, He X, Li X, Li J, Wu K, Gao T, Zhu S, Lin S, Wang MW, Cheng X, Yin W, Jiang Y, Yang D, Xu HE 10.1038/S41586-023-06395-9 2023-08-09 Yes