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RECEPTOR
STRUCTURE
SIGNAL PROTEIN
AUXILIARY PROTEIN
STRUCTURE LIGAND
PHYSIOLOGICAL LIGAND
SODIUM ION SITE
REFERENCE
ANNOTATED
UniProt
 IUPHAR Receptor family Cl. Species Method
PDB
 Refined
structure
 Resolution Preferred
chain		 State
 Degree
active (%)
 % of Seq Family Subtype Note % of Seq Fusion Antibodies Name Type Modality Name Type D2x50
S3x39		 Sodium in
structure		 Authors Reference PDB Date
OPSD Rhodopsin Opsins A Bovine X-ray 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 1F88 1F88_refined 2.8 A Inactive 22 97 - - - - - - Retinal (11-cis)
small-molecule Inverse agonist - - No No Palczewski K, Kumasaka T, Hori T, Behnke CA, Motoshima H, Fox BA, Le Trong I, Teller DC, Okada T, Stenkamp RE, Yamamoto M, Miyano M 10.1126/SCIENCE.289.5480.739 2000-08-04 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 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 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 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
ADRB2 β2 Adrenoceptors A Human X-ray 2RH1 - 2.4 A Inactive 0 68 - - - - T4-Lysozyme - Carazolol
small-molecule Inverse agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule No No Cherezov V, Rosenbaum DM, Hanson MA, Rasmussen SG, Thian FS, Kobilka TS, Choi HJ, Kuhn P, Weis WI, Kobilka BK, Stevens RC 10.1126/SCIENCE.1150577 2007-10-30 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 2J4Y - 3.4 B Inactive 22 94 - - - - - - Retinal (11-cis)
small-molecule Inverse agonist - - No No Standfuss J, Xie G, Edwards PC, Burghammer M, Oprian DD, Schertler GF 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
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
OPSD Rhodopsin Opsins A Japanese flying squid X-ray 2ZIY - 3.7 A Inactive 11 83 - - - - - - Retinal (11-cis)
small-molecule Inverse agonist - - No No Shimamura T, Hiraki K, Takahashi N, Hori T, Ago H, Masuda K, Takio K, Ishiguro M, Miyano M 10.1074/JBC.C800040200 2008-05-06 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 2R4S 2R4S_refined 3.4 A Inactive 1 52 - - - - - Antibody Carazolol
small-molecule Inverse agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule No No Rasmussen SG, Choi HJ, Rosenbaum DM, Kobilka TS, Thian FS, Edwards PC, Burghammer M, Ratnala VR, Sanishvili R, Fischetti RF, Schertler GF, Weis WI, Kobilka BK 10.1038/NATURE06325 2007-11-06 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 2HPY - 2.8 B Inactive 22 100 - - - - - - Retinal (all-trans)
small-molecule Agonist - - No No Nakamichi H, Okada T 10.1073/PNAS.0601765103 2006-08-22 Yes
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
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 Salom D, Lodowski DT, Stenkamp RE, Le Trong I, Golczak M, Jastrzebska B, Harris T, Ballesteros JA, Palczewski K 10.1073/PNAS.0608022103 2006-10-17 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
ADRB2 β2 Adrenoceptors A Human X-ray 2R4R 2R4R_refined 3.4 A Inactive 1 52 - - - - - Antibody Carazolol
small-molecule Inverse agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule No No - - 2007-11-06 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 3DQB 3DQB_refined 3.2 A Active 100 94 Gi/o αt1 Only H5 3 - - Apo (no ligand)
none Apo (no ligand) - - No No Scheerer P, Park JH, Hildebrand PW, Kim YJ, Krauss N, Choe HW, Hofmann KP, Ernst OP 10.1038/NATURE07330 2008-09-23 Yes
AA2AR A2A Adenosine A Human X-ray 3EML - 2.6 A Inactive 0 70 - - - - T4-Lysozyme - ZM-241385
small-molecule Antagonist adenosine small-molecule No No Jaakola VP, Griffith MT, Hanson MA, Cherezov V, Chien EY, Lane JR, Ijzerman AP, Stevens RC 10.1126/SCIENCE.1164772 2008-10-14 Yes
OPSD Rhodopsin Opsins A Japanese flying squid X-ray 2Z73 2Z73_refined 2.5 A Inactive 11 78 - - - - - - Retinal (11-cis)
small-molecule Inverse agonist - - No No - 10.1038/NATURE06925 2008-05-13 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 3NY8 3NY8_refined 2.8 A Inactive 0 67 - - - - T4-Lysozyme - ICI 118551
small-molecule Inverse agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule No No - - 2010-08-11 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 3NY9 3NY9_refined 2.8 A Inactive 0 67 - - - - T4-Lysozyme - CHEMBL1233771
small-molecule Inverse agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule No No Wacker D, Fenalti G, Brown MA, Katritch V, Abagyan R, Cherezov V, Stevens RC 10.1021/JA105108Q 2010-08-11 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 3D4S 3D4S_refined 2.8 A Inactive 0 67 - - - - T4-Lysozyme - timolol
small-molecule Inverse agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule No No Hanson MA, Cherezov V, Griffith MT, Roth CB, Jaakola VP, Chien EY, Velasquez J, Kuhn P, Stevens RC 10.1016/J.STR.2008.05.001 2008-06-17 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
ADRB2 β2 Adrenoceptors A Human X-ray 3NYA 3NYA_refined 3.2 A Inactive 0 67 - - - - T4-Lysozyme - CHEMBL1160734
small-molecule Antagonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline 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 Park JH, Scheerer P, Hofmann KP, Choe HW, Ernst OP 10.1038/NATURE07063 2008-06-24 Yes
CXCR4 CXCR4 Chemokine A Human X-ray 3OE0 - 2.9 A Inactive 10 78 - - - - T4-Lysozyme - CVX15
peptide Antagonist CXCL12α, CXCL12, CXCL12γ, CXCL12φ, CXCL12β, CXCL12δ, CXCL12ε peptide No No - - 2010-10-27 Yes
CXCR4 CXCR4 Chemokine A Human X-ray 3OE6 3OE6_refined 3.2 A Inactive 10 77 - - - - T4-Lysozyme - isothiourea-1t
small-molecule Antagonist CXCL12α, CXCL12, CXCL12γ, CXCL12φ, CXCL12β, CXCL12δ, CXCL12ε 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 Carazolol
small-molecule Inverse agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline 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 10 83 - - - - T4-Lysozyme - isothiourea-1t
small-molecule Antagonist CXCL12α, CXCL12, CXCL12γ, CXCL12φ, CXCL12β, CXCL12δ, CXCL12ε peptide No No - 10.1126/SCIENCE.1194396 2010-10-27 Yes
CXCR4 CXCR4 Chemokine A Human X-ray 3OE8 3OE8_refined 3.1 A Inactive 10 76 - - - - T4-Lysozyme - isothiourea-1t
small-molecule Antagonist CXCL12α, CXCL12, CXCL12γ, CXCL12φ, CXCL12β, CXCL12δ, CXCL12ε peptide No No - - 2010-10-27 Yes
CXCR4 CXCR4 Chemokine A Human X-ray 3OE9 3OE9_refined 3.1 A Inactive 10 74 - - - - T4-Lysozyme - isothiourea-1t
small-molecule Antagonist CXCL12α, CXCL12, CXCL12γ, CXCL12φ, CXCL12β, CXCL12δ, CXCL12ε peptide No No - 10.1126/SCIENCE.1194396 2010-10-27 Yes
DRD3 D3 Dopamine A Human X-ray 3PBL 3PBL_refined 2.9 A Inactive 0 68 - - - - T4-Lysozyme - eticlopride
small-molecule Antagonist dopamine small-molecule No No Chien EY, Liu W, Zhao Q, Katritch V, Han GW, Hanson MA, Shi L, Newman AH, Javitch JA, Cherezov V, Stevens RC 10.1126/SCIENCE.1197410 2010-11-03 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 - - 2011-01-12 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 2Y02 2Y02_refined 2.6 B Inactive 0 62 - - - - - - CARMOTEROL
small-molecule Agonist - - No No Warne T, Moukhametzianov R, Baker JG, Nehme R, Edwards PC, Leslie AG, Schertler GF, Tate CG 10.1038/NATURE09746 2011-01-12 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 2Y03 2Y03_refined 2.9 B Inactive 0 62 - - - - - - LEVISOPRENALINE
small-molecule Agonist - - No No Warne T, Moukhametzianov R, Baker JG, Nehme R, Edwards PC, Leslie AG, Schertler GF, Tate CG 10.1038/NATURE09746 2011-01-12 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 2Y04 2Y04_refined 3.1 B Inactive 0 62 - - - - - - levosalbutamol
small-molecule Agonist (partial) - - No No Warne T, Moukhametzianov R, Baker JG, Nehme R, Edwards PC, Leslie AG, Schertler GF, Tate CG 10.1038/NATURE09746 2011-01-12 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 3PDS 3PDS_refined 3.5 A Inactive 0 68 - - - - T4-Lysozyme - FAUC50
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule No No Rosenbaum DM, Zhang C, Lyons JA, Holl R, Aragao D, Arlow DH, Rasmussen SG, Choi HJ, Devree BT, Sunahara RK, Chae PS, Gellman SH, Dror RO, Shaw DE, Weis WI, Caffrey M, Gmeiner P, Kobilka BK 10.1038/NATURE09665 2011-01-12 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 3OAX - 2.6 A Inactive 22 100 - - - - - - Retinal (11-cis)
small-molecule Inverse agonist - - No No Makino CL, Riley CK, Looney J, Crouch RK, Okada T 10.1016/J.BPJ.2010.08.003 2011-01-19 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 3P0G 3P0G_refined 3.5 A Active 99 69 - - - - T4-Lysozyme Nanobody CHEMBL1615159
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule No No Rasmussen SG, Choi HJ, Fung JJ, Pardon E, Casarosa P, Chae PS, Devree BT, Rosenbaum DM, Thian FS, Kobilka TS, Schnapp A, Konetzki I, Sunahara RK, Gellman SH, Pautsch A, Steyaert J, Weis WI, Kobilka BK 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 Choe HW, Kim YJ, Park JH, Morizumi T, Pai EF, Krauss N, Hofmann KP, Scheerer P, Ernst OP 10.1038/NATURE09789 2011-03-09 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 3PXO - 3.0 A Active 98 94 - - - - - - Retinal (all-trans)
small-molecule Agonist - - No No Choe HW, Kim YJ, Park JH, Morizumi T, Pai EF, Krauss N, Hofmann KP, Scheerer P, Ernst OP 10.1038/NATURE09789 2011-03-09 Yes
AA2AR A2A Adenosine A Human X-ray 3QAK 3QAK_refined 2.7 A Active 75 69 - - - - T4-Lysozyme - UK-432,097
small-molecule Agonist adenosine small-molecule No No Xu F, Wu H, Katritch V, Han GW, Jacobson KA, Gao ZG, Cherezov V, Stevens RC 10.1126/SCIENCE.1202793 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 Standfuss J, Edwards PC, D'Antona A, Fransen M, Xie G, Oprian DD, Schertler GF 10.1038/NATURE09795 2011-03-16 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 2Y01 - 2.6 A Inactive 0 59 - - - - - - Dobutamine
small-molecule Agonist (partial) - - No No Warne T, Moukhametzianov R, Baker JG, Nehme R, Edwards PC, Leslie AG, Schertler GF, Tate CG 10.1038/NATURE09746 2011-03-30 Yes
AA2AR A2A Adenosine A Human X-ray 2YDO 2YDO_refined 3.0 A Active 75 73 - - - - - - adenosine
small-molecule Agonist adenosine small-molecule No No Lebon G, Warne T, Edwards PC, Bennett K, Langmead CJ, Leslie AG, Tate CG 10.1038/NATURE10136 2011-05-18 Yes
AA2AR A2A Adenosine A Human X-ray 2YDV 2YDV_refined 2.6 A Active 75 75 - - - - - - NECA
small-molecule Agonist adenosine small-molecule No No Lebon G, Warne T, Edwards PC, Bennett K, Langmead CJ, Leslie AG, Tate CG 10.1038/NATURE10136 2011-05-18 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 2YCW 2YCW_refined 3.0 A Inactive 0 61 - - - - - - Carazolol
small-molecule Antagonist - - No No Moukhametzianov R, Warne T, Edwards PC, Serrano-Vega MJ, Leslie AG, Tate CG, Schertler GF 10.1073/PNAS.1100185108 2011-06-01 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 2YCX - 3.3 A Inactive 0 59 - - - - - - (S)-Cyanopindolol
small-molecule Antagonist - - No No Moukhametzianov R, Warne T, Edwards PC, Serrano-Vega MJ, Leslie AG, Tate CG, Schertler GF 10.1073/PNAS.1100185108 2011-06-01 Yes
5HT1B 5-HT1B 5-Hydroxytryptamine A Human X-ray 4IAQ 4IAQ_refined 2.8 A Inactive 17 70 - - - - BRIL - dihydroergotamine
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
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
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
AA2AR A2A Adenosine A Human X-ray 5K2B 5K2B_refined 2.5 A Inactive 0 72 - - - - BRIL - ZM-241385
small-molecule Antagonist adenosine small-molecule No No - - 2016-09-21 Yes
APJ apelin Apelin A Human X-ray 5VBL - 2.6 B Inactive 9 79 - - - - Rubredoxin - AMG3054
peptide Agonist apelin-36, apelin-17, apelin-13, Elabela/Toddler-21, Elabela/Toddler-32, Elabela/Toddler-11, [Pyr1]apelin-13, apelin receptor early endogenous ligand 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
Q9WTK1 BLT1 Leukotriene A Guinea pig X-ray 5X33 5X33_refined 3.7 A Inactive 10 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
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 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 55 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 6IGL - 2.7 A Inactive 3 70 - - - - T4-Lysozyme - sovateltide
peptide Agonist (partial) endothelin-2, endothelin-3, endothelin-1 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
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 Johansson LC, Stauch B, McCorvy JD, Han GW, Patel N, Huang XP, Batyuk A, Gati C, Slocum ST, Li C, Grandner JM, Hao S, Olsen RHJ, Tribo AR, Zaare S, Zhu L, Zatsepin NA, Weierstall U, Yous S, Stevens RC, Liu W, Roth BL, Katritch V, Cherezov V 10.1038/S41586-019-1144-0 2019-04-24 Yes
AA2AR A2A Adenosine A Human X-ray 6JZH 6JZH_refined 2.3 A Inactive 0 72 - - - - BRIL - ZM-241385
small-molecule Antagonist adenosine small-molecule No No Shimazu Y, Tono K, Tanaka T, Yamanaka Y, Nakane T, Mori C, Terakado Kimura K, Fujiwara T, Sugahara M, Tanaka R, Doak RB, Shimamura T, Iwata S, Nango E, Yabashi M 10.1107/S1600576719012846 2019-10-30 Yes
OPRD δ Opioid A Human X-ray 6PT3 6PT3_refined 3.3 A Active 75 78 - - - - BRIL - DPI-287
small-molecule Agonist endomorphin-1, α-neoendorphin, β-endorphin, dynorphin A, dynorphin A-(1-8), [Leu]enkephalin, dynorphin A-(1-13), dynorphin B, [Met]enkephalin 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
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 PHM, PHV, VIP, PACAP-27, PHI, 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
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 III, angiotensin II, angiotensin-(1-7) 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
GPBAR GPBA Bile acid A Human Cryo-EM 7CFM - 3.0 R Active 100 83 Gs αs - 58 - Nanobody-35 CHEMBL2331646
small-molecule Agonist cholic acid, deoxycholic acid, chenodeoxycholic acid, lithocholic acid small-molecule No No - - 2020-09-09 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
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
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 Chen Q, Plasencia M, Li Z, Mukherjee S, Patra D, Chen CL, Klose T, Yao XQ, Kossiakoff AA, Chang L, Andrews PC, Tesmer JJG 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 CCK-8, desulfated cholecystokinin-8, CCK-39, CCK-58, CCK-33, CCK-4, 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
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 neuropeptide-γ, hemokinin 1, neurokinin A, neuropeptide K, neurokinin B, substance P 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
CCKAR CCK1 Cholecystokinin A Human X-ray 7F8X 7F8X_refined 3.0 A Inactive 0 66 - - - - T4-Lysozyme - NN9056
peptide Agonist CCK-8, desulfated cholecystokinin-8, CCK-39, CCK-58, CCK-33, CCK-4, 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 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 7EJ0 - 3.2 R Active 100 56 Gi/o αo - 61 - scFv16 (-)-noradrenaline
small-molecule Agonist (-)-noradrenaline, (-)-adrenaline small-molecule No No Xu J, Cao S, Hubner H, Weikert D, Chen G, Lu Q, Yuan D, Gmeiner P, Liu Z, Du Y 10.1126/SCIADV.ABJ5347 2022-04-13 Yes
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
PAR1 PAR1 Proteinase-activated A Human Cryo-EM 8XOR 8XOR_refined 3.0 R Active 100 70 Gq/11 αq - 60 - scFv16 Tethered agonist
peptide Agonist thrombin peptide No No - - 2024-09-18 Yes
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 8YW3 8YW3_refined 2.7 R Active 100 83 Gs αs - 57 - Nanobody-35 Retatrutide
peptide Agonist glucagon-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide peptide No No Li W, Zhou Q, Cong Z, Yuan Q, Li W, Zhao F, Xu HE, Zhao LH, Yang D, Wang MW 10.1038/S41421-024-00700-0 2024-09-18 Yes
GP179 GPR179 C Orphans C Human Cryo-EM 8IRJ - 3.5 A Inactive - 22 - - - - - - Apo (no ligand)
none Apo (no ligand) - - No No - - 2024-09-18 Yes
EDNRB ETB Endothelin A Human Cryo-EM 8ZRT - 3.6 R Active 82 64 - - - - - - ENDOTHELIN
protein Agonist endothelin-2, endothelin-3, endothelin-1 peptide No No Tani K, Maki-Yonekura S, Kanno R, Negami T, Hamaguchi T, Hall M, Mizoguchi A, Humbel BM, Terada T, Yonekura K, Doi T 10.1038/S42003-024-06905-Z 2024-10-02 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 2YCY - 3.2 A Inactive 0 60 - - - - - - (S)-Cyanopindolol
small-molecule Antagonist - - No No Moukhametzianov R, Warne T, Edwards PC, Serrano-Vega MJ, Leslie AG, Tate CG, Schertler GF 10.1073/PNAS.1100185108 2011-06-08 Yes
5HT2B 5-HT2B 5-Hydroxytryptamine A Human X-ray 4IB4 4IB4_refined 2.7 A Intermediate 55 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
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
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
CALCR CT Calcitonin B1 Human Cryo-EM 5UZ7 - 4.1 R Active 100 56 Gs αs - 47 - - calcitonin (salmon synthetic)
small-molecule Agonist calcitonin, adrenomedullin, amylin, α-CGRP, adrenomedullin 2/intermedin, β-CGRP 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
5HT2C 5-HT2C 5-Hydroxytryptamine A Human X-ray 6BQG 6BQG_refined 3.0 A Active 84 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
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 6IIV 6IIV_refined 3.0 A Inactive 33 87 - - - - Rubredoxin - daltroban
small-molecule Antagonist PGF2α, PGH2, PGI2, PGD2, thromboxane A2, PGE2 small-molecule No No Fan H, Chen S, Yuan X, Han S, Zhang H, Xia W, Xu Y, Zhao Q, Wu B 10.1038/S41589-018-0170-9 2018-12-19 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 Johansson LC, Stauch B, McCorvy JD, Han GW, Patel N, Huang XP, Batyuk A, Gati C, Slocum ST, Li C, Grandner JM, Hao S, Olsen RHJ, Tribo AR, Zaare S, Zhu L, Zatsepin NA, Weierstall U, Yous S, Stevens RC, Liu W, Roth BL, Katritch V, Cherezov V 10.1038/S41586-019-1144-0 2019-04-24 Yes
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-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide peptide No No Xu Y, Wang Y, Wang Y, Liu K, Peng Y, Yao D, Tao H, Liu H, Song G 10.1107/S2052252519013496 2019-11-13 Yes
OX1R OX1 Orexin A Human X-ray 6TP3 6TP3_refined 3.0 A Inactive 0 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
NTR1 NTS1 Neurotensin A Human Cryo-EM 6UP7 6UP7_refined 4.2 R Active 100 77 Beta Beta-arrestin-1 - 83 - - JMV431
peptide Agonist large neuromedin N, neuromedin N, neurotensin, large neurotensin 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 6VJM - 4.0 B Inactive - 73 - - - - - - Apo (no ligand)
none Apo (no ligand) - - 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
SCTR secretin Glucagon B1 Human Cryo-EM 6WZG 6WZG_refined 2.3 R Active 100 86 Gs αs - 61 - Nanobody-35 SECRETIN
protein Agonist VIP, secretin peptide No No Dong M, Deganutti G, Piper SJ, Liang YL, Khoshouei M, Belousoff MJ, Harikumar KG, Reynolds CA, Glukhova A, Furness SGB, Christopoulos A, Danev R, Wootten D, Sexton PM, Miller LJ 10.1038/S41467-020-17791-4 2020-08-12 Yes
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 X-ray 7JOZ 7JOZ_refined 3.8 R Active 100 64 Gs αs - 86 - Nanobody-35 CHEMBL4453318
small-molecule Agonist L-NOREPINEPHRINE, noradrenaline, (-)-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
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		 Ca2+, spermine, Mg2+, L-tryptophan small-molecule No No Gao Y, Robertson MJ, Rahman SN, Seven AB, Zhang C, Meyerowitz JG, Panova O, Hannan FM, Thakker RV, Brauner-Osborne H, Mathiesen JM, Skiniotis G 10.1038/S41586-021-03691-0 2021-06-30 Yes
PD2R2 DP2 Prostanoid A Human X-ray 7M8W 7M8W_refined 2.6 A Inactive 24 83 - - - - T4-Lysozyme - 15(R)-15-methyl-PGD2
small-molecule Antagonist PGF2α, PGI2, PGJ2, PGD2, thromboxane A2, PGE2, PGD3 small-molecule No No 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
S1PR3 S1P3 Lysophospholipid (S1P) A Human Cryo-EM 7EW2 - 3.1 R Active 100 77 Gi/o αi1 - 64 - scFv16 (S)-FTY720-phosphate
small-molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine small-molecule No No Zhao C, Cheng L, Wang W, Wang H, Luo Y, Feng Y, Wang X, Fu H, Cai Y, Yang S, Fu P, Yan W, Shao Z 10.1038/S41422-021-00567-W 2021-09-29 Yes
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
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
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 peptide YY, pancreatic polypeptide, neuropeptide Y 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
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 7FIM - 3.4 R Active 100 83 Gs αs - 57 - Nanobody-35 tirzepatide
peptide Agonist glucagon-like peptide 1-(7-37), glucagon, 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
AGRL3 ADGRL3 ADGRL B2 Human Cryo-EM 7SF7 - 2.9 A Active 100 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
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
CNR1 CB1 Cannabinoid A Human X-ray 7FEE 7FEE_refined 2.7 A Inactive 10 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		 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
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 cortistatin-14, SRIF-14, CST-17, 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 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
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
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
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, α-linolenic acid, myristic acid, docosahexaenoic acid small-molecule No No Kumari P, Inoue A, Chapman K, Lian P, Rosenbaum DM 10.1073/PNAS.2219569120 2023-05-24 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 ATP, ADP small-molecule No No - - 2023-06-07 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 calcitonin, adrenomedullin, amylin, α-CGRP, adrenomedullin 2/intermedin, β-CGRP 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 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
PE2R4 EP4 Prostanoid A Human Cryo-EM 8GDA 8GDA_refined 3.3 R Active 100 58 Gs αs - 58 - - (2S,5R)-5-[(1E,3S)-4,4-difluoro-3-hydroxy-4-phenylbut-1-en-1-yl]-1-[6-(1H-tetrazol-5-yl)hexyl]pyrrolidin-2-ol
small-molecule Agonist PGF2α, PGI2, PGD2, thromboxane A2, PGE1, PGE2 small-molecule No No Huang SM, Xiong MY, Liu L, Mu J, Wang MW, Jia YL, Cai K, Tie L, Zhang C, Cao S, Wen X, Wang JL, Guo SC, Li Y, Qu CX, He QT, Cai BY, Xue C, Gan S, Xie Y, Cong X, Yang Z, Kong W, Li S, Li Z, Xiao P, Yang F, Yu X, Guan YF, Zhang X, Liu Z, Yang BX, Du Y, Sun JP 10.1073/PNAS.2216329120 2024-01-10 Yes
C3AR C3a Complement peptide A Human Cryo-EM 8I9L - 3.2 C Active 100 57 Gi/o αo - 59 - scFv16 C3a anaphylatoxin
peptide Agonist C5a, C3a peptide No No Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C 10.1016/J.CELL.2023.09.020 2023-10-18 Yes
CCR8 CCR8 Chemokine A Human Cryo-EM 8KFY 8KFY_refined 3.1 R Active 100 81 Gi/o αi1 - 64 - scFv16 ZK 756326
small-molecule Agonist CCL8, CCL1 peptide No No Jiang S, Lin X, Wu L, Wang L, Wu Y, Xu Z, Xu F 10.1126/SCIADV.ADJ7500 2024-02-07 Yes
CXCR4 CXCR4 Chemokine A Human Cryo-EM 8U4Q - 3.4 R Active 100 84 Gi/o αi1 - 62 - REGN7663 Fab light chain REGN7663 Fab heavy chain
protein Agonist CXCL12α, CXCL12, CXCL12γ, CXCL12φ, CXCL12β, CXCL12δ, CXCL12ε peptide No No Saotome K, McGoldrick LL, Ho JH, Ramlall TF, Shah S, Moore MJ, Kim JH, Leidich R, Olson WC, Franklin MC 10.1038/S41594-024-01397-1 2024-03-13 Yes
KISSR kisspeptin Kisspeptin A Human Cryo-EM 8ZJD - 3.1 R Active 100 72 Gq/11 αq - 63 - scFv16 Kisspeptin-10
peptide Agonist kisspeptin-10, kisspeptin-54, kisspeptin-52, kisspeptin-14, kisspeptin-13 peptide No No - - 2024-07-03 Yes
T2R14 TAS2R14 Taste 2 T2 Human Cryo-EM 9IJ9 - 2.7 R Active 100 90 Gi/o αi1 - 62 - - Cholesterol
compound 28.1 [PMID: 36847646]
small-molecule
small-molecule		 Agonist
Allosteric agonist		 - - No No - - 2024-07-24 Yes
EDNRB ETB Endothelin A Human Cryo-EM 8XWQ - 4.6 R Active 100 68 Gi/o αi1 - 62 - scFv16 ENDOTHELIN
protein Agonist endothelin-2, endothelin-3, endothelin-1 peptide No No Tani K, Maki-Yonekura S, Kanno R, Negami T, Hamaguchi T, Hall M, Mizoguchi A, Humbel BM, Terada T, Yonekura K, Doi T 10.1038/S42003-024-06905-Z 2024-10-02 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 2YCZ 2YCZ_refined 3.7 B Inactive 0 60 - - - - - - Iodocyanopindolol
small-molecule Antagonist - - No No Moukhametzianov R, Warne T, Edwards PC, Serrano-Vega MJ, Leslie AG, Tate CG, Schertler GF 10.1073/PNAS.1100185108 2011-06-01 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
AGTR1 AT1 Angiotensin A Human X-ray 4YAY 4YAY_refined 2.9 A Inactive 10 79 - - - - BRIL - ZD-7155
small-molecule Antagonist angiotensin IV, angiotensin A, angiotensin III, 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
ADRB2 β2 Adrenoceptors A Human X-ray 5D6L 5D6L_refined 3.2 A Inactive 0 68 - - - - T4-Lysozyme - Carazolol
small-molecule Inverse agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule No No Ma P, Weichert D, Aleksandrov LA, Jensen TJ, Riordan JR, Liu X, Kobilka BK, Caffrey M 10.1038/NPROT.2017.057 2016-08-17 Yes
SMO SMO Frizzled F Human X-ray 5V57 5V57_refined 3.0 A Inactive 0 62 - - - - Flavodoxin - N-methyl-N-[1-[4-(2-methylpyrazol-3-yl)phthalazin-1-yl]piperidin-4-yl]-4-nitro-2-(trifluoromethyl)benzamide
small-molecule Antagonist - - No No Zhang X, Zhao F, Wu Y, Yang J, Han GW, Zhao S, Ishchenko A, Ye L, Lin X, Ding K, Dharmarajan V, Griffin PR, Gati C, Nelson G, Hunter MS, Hanson MA, Cherezov V, Stevens RC, Tan W, Tao H, Xu F 10.1038/NCOMMS15383 2017-05-24 Yes
AA2AR A2A Adenosine A Human X-ray 5OM1 5OM1_refined 2.1 A Inactive 0 72 - - - - BRIL - CHEMBL2024114
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
Q98SW5 SMO Frizzled F African clawed frog X-ray 6D35 6D35_refined 3.9 A Active 65 58 - - - - BRIL - Cholesterol
small-molecule Agonist - - No No - - 2018-05-23 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
AGTR1 AT1 Angiotensin A Human X-ray 6DO1 6DO1_refined 2.9 A Active 92 85 - - - - BRIL Nanobody-Nb.AT110i1 CHEMBL404594
protein Agonist angiotensin IV, angiotensin A, angiotensin III, angiotensin II peptide No No Wingler LM, McMahon C, Staus DP, Lefkowitz RJ, Kruse AC 10.1016/J.CELL.2018.12.006 2019-01-30 Yes
CLTR1 CysLT1 Leukotriene A Human X-ray 6RZ5 6RZ5_refined 2.5 B Active 55 84 - - - - BRIL - zafirlukast
small-molecule Antagonist LTE4, LTC4, LTD4 small-molecule No No Luginina A, Gusach A, Marin E, Mishin A, Brouillette R, Popov P, Shiriaeva A, Besserer-Offroy E, Longpre JM, Lyapina E, Ishchenko A, Patel N, Polovinkin V, Safronova N, Bogorodskiy A, Edelweiss E, Hu H, Weierstall U, Liu W, Batyuk A, Gordeliy V, Han GW, Sarret P, Katritch V, Borshchevskiy V, Cherezov V 10.1126/SCIADV.AAX2518 2019-10-30 Yes
OX1R OX1 Orexin A Human X-ray 6TP6 6TP6_refined 2.3 B Inactive 0 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
GPR52 GPR52 A orphans A Human X-ray 6LI1 6LI1_refined 2.9 A Inactive 37 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
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 - - 2020-09-23 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 7CKY - 3.2 R Active 100 62 Gs αs - 60 - Nanobody-35 CHEMBL3697578
small-molecule Agonist L-NOREPINEPHRINE, noradrenaline, (-)-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 7DD7 - 3.2 B Active - 73 - - - - - - Calcium
L-tryptophan
evocalcet
small-molecule
small-molecule
small-molecule		 Agonist
PAM
PAM		 Ca2+, spermine, Mg2+, L-tryptophan 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-like peptide 1-(7-37), glucagon, glucagon-like peptide 1-(7-36) amide peptide No No Cong Z, Chen LN, Ma H, Zhou Q, Zou X, Ye C, Dai A, Liu Q, Huang W, Sun X, Wang X, Xu P, Zhao L, Xia T, Zhong W, Yang D, Eric Xu H, Zhang Y, Wang MW 10.1038/S41467-021-24058-Z 2021-08-11 Yes
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
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 CCK-8, desulfated cholecystokinin-8, gastrin-14, CCK-58, desulfated gastrin-17, CCK-39, CCK-33, desulfated gastrin-34, gastrin-34, gastrin-71, desulfated gastrin-71, CCK-4, desulfated gastrin-14, 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
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
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
MSHR MC1 Melanocortin A Human Cryo-EM 7F4F - 2.9 R Active 100 85 Gs αs - 59 - scFv16 CHEMBL407070
protein Agonist γ-MSH, β-MSH, α-MSH, ACTH 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 7TYN - 2.6 R Active 100 79 Gs αs - 58 - Nanobody-35 calcitonin (salmon synthetic)
small-molecule Agonist calcitonin, adrenomedullin, amylin, α-CGRP, adrenomedullin 2/intermedin, β-CGRP peptide No No Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM 10.1126/SCIENCE.ABM9609 2022-03-30 Yes
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
DRD1 D1 Dopamine A Human Cryo-EM 7F0T - 3.1 F Active 100 63 Gs αs - 58 - Nanobody-35 dopamine
small-molecule Agonist L-NOREPINEPHRINE, noradrenaline, (-)-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
MRGRD MRGPRD A orphans A Human Cryo-EM 7Y13 7Y13_refined 3.1 R Intermediate 47 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
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
AA2AR A2A Adenosine A Human X-ray 8CU7 8CU7_refined 2.1 A Inactive 0 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
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-palmitoylethanolamine, anandamide, N-oleoylethanolamide, SEA 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
AGRL3 ADGRL3 ADGRL B2 Mouse Cryo-EM 7WY8 - 2.8 R Active 100 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
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
PTH1R PTH1 Parathyroid hormone B1 Human Cryo-EM 8HA0 - 2.6 R Active 100 61 Gs αs - 60 - Nanobody-35 teriparatide
peptide Agonist PTHrP-(1-36), PTHrP, PTH, TIP39 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
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-2, endothelin-3, endothelin-1 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
C5AR1 C5a1 Complement peptide A Human Cryo-EM 7Y64 - 2.9 D Active 100 84 Gi/o αi1 - 63 - scFv16 C5a anaphylatoxin
peptide Agonist ribosomal protein S19, C3a, C5a, 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
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 8JWZ - 2.4 A Inactive 0 71 - - - - T4-Lysozyme - AB928
small-molecule Antagonist adenosine small-molecule No No - - 2023-08-16 Yes
CRFR1 CRF1 Corticotropin-releasing factor B1 Human X-ray 8GTG - 2.8 A Inactive 16 63 - - - - Endolysin - 8-(4-bromo-2,6-dimethoxyphenyl)-N,N-bis(2-methoxyethyl)-2,7-dimethylpyrazolo[1,5-a][1,3,5]triazin-4-amine
small-molecule Antagonist corticotrophin-releasing hormone, urocortin 1, urocortin 2 peptide No No Kim H, Lim T, Ha GE, Lee JY, Kim JW, Chang N, Kim SH, Kim KH, Lee J, Cho Y, Kim BW, Abrahamsson A, Kim SH, Kim HJ, Park S, Lee SJ, Park J, Cheong E, Kim BM, Cho HS 10.1038/S12276-023-01082-1 2023-09-13 Yes
C5AR1 C5a1 Complement peptide A Human Cryo-EM 8IA2 8IA2_refined 3.2 A Active 100 84 Gi/o αo - 59 - scFv16 C5a
peptide Agonist ribosomal protein S19, C3a, C5a, C5a des-Arg peptide No No Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C 10.1016/J.CELL.2023.09.020 2023-10-18 Yes
TAAR1 TA1 Trace amine A Human Cryo-EM 8JLQ - 2.8 R Active 100 83 Gs αs - 58 BRIL scFv16 fenoldopam
small-molecule Agonist octopamine, β-phenylethylamine, CHEMBL1160703, tyramine, (+)-Octopamine, 3-iodothyronamine, dopamine small-molecule No No Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z 10.1038/S41586-023-06804-Z 2023-11-15 Yes
CCR8 CCR8 Chemokine A Human Cryo-EM 8TLM - 2.9 C Inactive 10 75 - - - - - Fab heavy chain
Fab light chain		 mAb1
protein Antagonist CCL8, CCL1 peptide No No Sun D, Sun Y, Janezic E, Zhou T, Johnson M, Azumaya C, Noreng S, Chiu C, Seki A, Arenzana TL, Nicoludis JM, Shi Y, Wang B, Ho H, Joshi P, Tam C, Payandeh J, Comps-Agrar L, Wang J, Rutz S, Koerber JT, Masureel M 10.1038/S41467-023-43601-8 2023-12-20 Yes
TAAR1 TA1 Trace amine A Mouse Cryo-EM 8WCB - 3.1 R Active 100 75 Gq/11 αq - 57 - scFv16 Cyclohexylammonium ion
small-molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine small-molecule No No Shang P, Rong N, Jiang JJ, Cheng J, Zhang MH, Kang D, Qi L, Guo L, Yang GM, Liu Q, Zhou Z, Li XB, Zhu KK, Meng QB, Han X, Yan W, Kong Y, Yang L, Wang X, Lei D, Feng X, Liu X, Yu X, Wang Y, Li Q, Shao ZH, Yang F, Sun JP 10.1016/J.CELL.2023.10.014 2023-12-27 Yes
ADRB2 β2 Adrenoceptors A Human Cryo-EM 8GE7 8GE7_refined 3.4 R Active 100 68 Gs αs - 58 - - (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule No No Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06 Yes
ADRB2 β2 Adrenoceptors A Human Cryo-EM 8GGB 8GGB_refined 3.5 R Active 100 64 Gs αs - 79 - - (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule No No Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06 Yes
GP156 GPR156 C Orphans C Human Cryo-EM 8IEI - 2.6 A Inactive - 34 - - - - - - [(2R)-3-[(E)-hexadec-9-enoyl]oxy-2-octadecanoyloxypropyl] 2-(trimethylazaniumyl)ethyl phosphate
lipid Agonist - - No No - - 2024-02-14 Yes
NK3R NK3 Tachykinin A Human Cryo-EM 8JBG 8JBG_refined 2.8 B Active 100 60 Gq/11 αq - 59 - scFv16 neurokinin B
peptide Agonist neurokinin A, substance P, neurokinin B peptide No No - - 2024-02-07 Yes
CASR CaS Calcium-sensing C Human Cryo-EM 8SZG - 3.6 A Active - 48 Gq/11 αq - 61 - - L-tryptophan
cinacalcet
small-molecule
small-molecule		 Agonist
PAM		 Ca2+, spermine, Mg2+, L-tryptophan small-molecule No No He F, Wu CG, Gao Y, Rahman SN, Zaoralova M, Papasergi-Scott MM, Gu TJ, Robertson MJ, Seven AB, Li L, Mathiesen JM, Skiniotis G 10.1038/S41586-024-07055-2 2024-02-07 Yes
ADRB2 β2 Adrenoceptors A Human Cryo-EM 8UNY - 3.6 R Active 100 69 Gs αs GTP bound, Class N 60 - - (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule No No Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06 Yes
HRH1 H1 Histamine A Human Cryo-EM 8X5X - 3.5 B Inactive 2 52 - - - - BRIL - Apo (no ligand)
none Apo (no ligand) histamine small-molecule No No Wang D, Guo Q, Wu Z, Li M, He B, Du Y, Zhang K, Tao Y 10.1038/S41467-023-44477-4 2024-01-17 Yes
GPER1 GPER Estrogen (G protein-coupled) A Human Cryo-EM 8XOI 8XOI_refined 3.2 R Active 100 70 Gq/11 αq - 59 - scFv16 fulvestrant
small-molecule Agonist 17β-estradiol small-molecule No No Liu H, Guo S, Dai A, Xu P, Li X, Huang S, He X, Wu K, Zhang X, Yang D, Xie X, Xu HE 10.1038/S41422-024-00963-Y 2024-04-10 Yes
APJ apelin Apelin A Human Cryo-EM 8XZJ 8XZJ_refined 3.0 R Active 100 80 Gi/o αi1 - 62 - scFv16 WN353
peptide Agonist apelin-36, apelin-17, apelin-13, Elabela/Toddler-21, Elabela/Toddler-32, Elabela/Toddler-11, [Pyr1]apelin-13, apelin receptor early endogenous ligand peptide No No Wang WW, Ji SY, Zhang W, Zhang J, Cai C, Hu R, Zang SK, Miao L, Xu H, Chen LN, Yang Z, Guo J, Qin J, Shen DD, Liang P, Zhang Y, Zhang Y 10.1016/J.CELL.2024.02.004 2024-03-20 Yes
OPRM μ Opioid A Mouse Cryo-EM 9BQJ - 3.3 D Active 100 71 Gi/o αi1 - 61 - scFv16 N-[[3-(hydroxymethyl)phenyl]methyl]-N-[1-(2-phenylethyl)piperidin-4-yl]propanamide
small-molecule Agonist - - No No - - 2024-09-11 Yes
NPY1R Y1 Neuropeptide Y A Human Cryo-EM 8K6O 8K6O_refined 3.3 D Active 100 78 Gi/o αi2 - 63 - scFv16 neuropeptide Y
peptide Agonist peptide YY, pancreatic polypeptide, neuropeptide Y peptide No No - - 2024-07-31 Yes
B1B1U5 Rhodopsin Opsins A Hasarius adansoni Cryo-EM 9EPP - 4.1 R Active 100 87 Gi/o αi1 - 63 - - 11,20-Ethanoretinal
small-molecule Agonist - - No No - - 2024-10-23 Yes
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 Shimamura T, Shiroishi M, Weyand S, Tsujimoto H, Winter G, Katritch V, Abagyan R, Cherezov V, Liu W, Han GW, Kobayashi T, Stevens RC, Iwata S 10.1038/NATURE10236 2011-06-15 Yes
GLR glucagon Glucagon B1 Human X-ray 4L6R 4L6R_refined 3.3 A Inactive 6 61 - - - - BRIL - Glucagon model
peptide Agonist 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
P2Y12 P2Y12 P2Y A Human X-ray 4PY0 4PY0_refined 3.1 A Active 55 83 - - - - BRIL - 2MeSATP
small-molecule Agonist (partial) ATP, ADP small-molecule No No Zhang J, Zhang K, Gao ZG, Paoletta S, Zhang D, Han GW, Li T, Ma L, Zhang W, Muller CE, Yang H, Jiang H, Cherezov V, Katritch V, Jacobson KA, Stevens RC, Wu B, Zhao Q 10.1038/NATURE13288 2014-04-30 Yes
OPRM μ Opioid A Mouse X-ray 5C1M 5C1M_refined 2.1 A Active 100 74 - - - - - Antibody BU72
small-molecule Agonist - - No No Huang W, Manglik A, Venkatakrishnan AJ, Laeremans T, Feinberg EN, Sanborn AL, Kato HE, Livingston KE, Thorsen TS, Kling RC, Granier S, Gmeiner P, Husbands SM, Traynor JR, Weis WI, Steyaert J, Dror RO, Kobilka BK 10.1038/NATURE14886 2015-08-05 Yes
SMO SMO Frizzled F Human X-ray 5L7I 5L7I_refined 3.3 B Inactive 4 59 - - - - BRIL - vismodegib
small-molecule Antagonist - - 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
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
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 Pfitzer E, Bitomsky L, Nissen M, Kausch C, Kowatsch T 10.1101/436212 2018-10-17 Yes
NK1R NK1 Tachykinin A Human X-ray 6HLO 6HLO_refined 2.4 A Inactive 0 70 - - - - GlgA glycogen synthase - aprepitant
small-molecule Antagonist neuropeptide-γ, hemokinin 1, neurokinin A, neuropeptide K, neurokinin B, substance P peptide No No Schoppe J, Ehrenmann J, Klenk C, Rucktooa P, Schutz M, Dore AS, Pluckthun A 10.1038/S41467-018-07939-8 2019-01-16 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 Maeda S, Qu Q, Robertson MJ, Skiniotis G, Kobilka BK 10.1126/SCIENCE.AAW5188 2019-05-08 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 6PS4 6PS4_refined 2.6 A Inactive 0 68 - - - - T4-Lysozyme - ICI 118551
small-molecule Antagonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule No No Ishchenko A, Stauch B, Han GW, Batyuk A, Shiriaeva A, Li C, Zatsepin N, Weierstall U, Liu W, Nango E, Nakane T, Tanaka R, Tono K, Joti Y, Iwata S, Moraes I, Gati C, Cherezov V 10.1107/S2052252519013137 2019-11-13 Yes
OX1R OX1 Orexin A Human X-ray 6TOS 6TOS_refined 2.1 B Inactive 0 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
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 PHM, PHV, VIP, PACAP-27, PHI, 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
CXCR2 CXCR2 Chemokine A Human X-ray 6LFL 6LFL_refined 3.2 A Inactive 6 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, CXCL8, CXCL7, CXCL2, CXCL1, CXCL6, CXCL5 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
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 7KNT 7KNT_refined 3.2 R Inactive 9 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
CASR CaS Calcium-sensing C Human Cryo-EM 7DTW 7DTW_refined 4.5 A Inactive - 72 - - - - - - Apo (no ligand)
none Apo (no ligand) Ca2+, spermine, Mg2+, L-tryptophan 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
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-like peptide 1-(7-37), glucagon, 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
CCKAR CCK1 Cholecystokinin A Human X-ray 7F8Y 7F8Y_refined 2.5 A Inactive 0 65 - - - - T4-Lysozyme - DEVAZEPIDE
small-molecule Antagonist CCK-8, desulfated cholecystokinin-8, CCK-39, CCK-58, CCK-33, CCK-4, 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
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-phenylalanine, L-tryptophan 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 7EVY - 3.0 D Active 100 71 Gi/o αi1 - 64 - scFv16 siponimod
small-molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine small-molecule No No Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z 10.1038/S41422-021-00566-X 2021-09-29 Yes
CALCR CT Calcitonin B1 Human Cryo-EM 7TYH - 3.3 R Active 100 78 Gs αs - 58 - Nanobody-35 Calcitonin human
peptide Agonist calcitonin, adrenomedullin, amylin, α-CGRP, adrenomedullin 2/intermedin, β-CGRP peptide No No Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM 10.1126/SCIENCE.ABM9609 2022-03-23 Yes
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
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 peptide YY, PYY-(3-36), neuropeptide Y-(3-36), pancreatic polypeptide, neuropeptide Y peptide No No - - 2022-05-18 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-36, apelin-17, apelin-13, Elabela/Toddler-21, Elabela/Toddler-32, Elabela/Toddler-11, [Pyr1]apelin-13, apelin receptor early endogenous ligand 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
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 CCL11, CCL2, CCL8, CCL16, CCL24, CCL13, CCL7, CCL26 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
AGRF1 ADGRF1 ADGRF B2 Human Cryo-EM 7WXW - 2.8 R Active 100 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
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
OPRM μ Opioid A Human Cryo-EM 8F7Q - 3.2 R Active 100 72 Gi/o αi1 - 64 - scFv16 β-endorphin
peptide Agonist endomorphin-1, β-endorphin, dynorphin A, dynorphin A-(1-8), [Leu]enkephalin, dynorphin A-(1-13), dynorphin B, [Met]enkephalin, 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
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-2, endothelin-3, endothelin-1 peptide No No - - 2023-03-22 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
AA2AR A2A Adenosine A Human X-ray 8CIC - 2.1 A Inactive 0 71 - - - - BRIL - AB928
small-molecule Antagonist adenosine small-molecule No No Claff T, Schlegel JG, Voss JH, Vaassen VJ, Weisse RH, Cheng RKY, Markovic-Mueller S, Bucher D, Strater N, Muller CE 10.1038/S42004-023-00894-6 2023-05-31 Yes
CNR2 CB2 Cannabinoid A Human Cryo-EM 8GUQ 8GUQ_refined 3.1 R Active 100 81 Gi/o αi1 - 62 - scFv16 olorinab
small-molecule Agonist 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 7YDM - 2.9 R Active 100 33 Gq/11 αq Mini-Gq 60 - Nanobody-35 Apo (no ligand)
none Apo (no ligand) - - No No Wang N, Qian Y, Xia R, Zhu X, Xiong Y, Zhang A, Guo C, He Y 10.1016/J.CHEMBIOL.2023.08.003 2023-07-12 Yes
PF2R FP Prostanoid A Human Cryo-EM 8IUL - 2.8 R Active 100 82 Gq/11 αq - 60 - scFv16 latanoprost (free acid form)
small-molecule Agonist PGF2α, PGI2, PGD2, thromboxane A2, PGE2 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
HCAR2 HCA2 Hydroxycarboxylic acid A Human Cryo-EM 8IJA - 2.7 A Active 100 81 Gi/o αi1 - 61 - scFv16 nicotinic acid
small-molecule Agonist β-D-hydroxybutyric acid, butyric acid small-molecule No No Pan X, Ye F, Ning P, Zhang Z, Li X, Zhang B, Wang Q, Chen G, Gao W, Qiu C, Wu Z, Li J, Zhu L, Xia J, Gong K, Du Y 10.1038/S41421-023-00610-7 2024-01-03 Yes
TAAR1 TA1 Trace amine A Mouse Cryo-EM 8JLJ - 3.1 R Active 100 81 Gs αs - 59 BRIL scFv16 CHEMBL1182312
small-molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine small-molecule No No Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z 10.1038/S41586-023-06804-Z 2023-11-15 Yes
GPR34 GPR34 A orphans A Human Cryo-EM 8SAI 8SAI_refined 3.3 A Active 100 76 Gi/o αi1 - 64 - scFv16 O-[(S)-Hydroxy{[(2s)-2-Hydroxy-3-(Octadec-9-Enoyloxy)propyl]oxy}phosphoryl]-L-Serine
small-molecule Agonist lysophosphatidylserine small-molecule No No Xia A, Yong X, Zhang C, Lin G, Jia G, Zhao C, Wang X, Hao Y, Wang Y, Zhou P, Yang X, Deng Y, Wu C, Chen Y, Zhu J, Tang X, Liu J, Zhang S, Zhang J, Xu Z, Hu Q, Zhao J, Yue Y, Yan W, Su Z, Wei Y, Zhou R, Dong H, Shao Z, Yang S 10.1073/PNAS.2308435120 2023-10-04 Yes
CASR CaS Calcium-sensing C Human Cryo-EM 8WPG - 2.7 A Inactive - 74 - - - - - - cinacalcet
Calcium
small-molecule
small-molecule		 Agonist Ca2+, spermine, Mg2+, L-tryptophan small-molecule No No Ling S, Meng X, Zhang Y, Xia Z, Zhou Y, Yang F, Shi P, Shi C, Tian C 10.1038/S41422-023-00892-2 2023-11-22 Yes
ADRB2 β2 Adrenoceptors A Human Cryo-EM 8GGC - 3.4 R Active 100 60 Gs αs - 75 - - (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol
small-molecule Agonist L-NOREPINEPHRINE, (-)-adrenaline, noradrenaline, Zn2+, (-)-noradrenaline small-molecule No No Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06 Yes
GP156 GPR156 C Orphans C Human Cryo-EM 8IEB - 3.0 A Inactive - 33 - - - - - - [(2R)-3-[(E)-hexadec-9-enoyl]oxy-2-octadecanoyloxypropyl] 2-(trimethylazaniumyl)ethyl phosphate
lipid Agonist - - No No - - 2024-02-14 Yes
HCAR2 HCA2 Hydroxycarboxylic acid A Human Cryo-EM 8J6L 8J6L_refined 3.1 R Active 100 81 Gi/o αi1 - 61 - scFv16 nicotinic acid
small-molecule Agonist