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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 Modality Name Type D2x50
S3x39		 Sodium in
structure		 Authors Reference PDB Date
OPSD Rhodopsin Opsins A Bovine X-ray 2I35 - 3.8 A Inactive 24 94 - - - - - - Retinal (11-cis)
small-molecule Inverse agonist - - No No - - 2006-10-17 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 1U19 1U19_refined 2.2 A Inactive 24 100 - - - - - - Retinal (11-cis)
small-molecule Inverse agonist - - No No Okada T, Sugihara M, Bondar AN, Elstner M, Entel P, Buss V 10.1016/J.JMB.2004.07.044 2004-10-12 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 1HZX - 2.8 A Inactive 24 98 - - - - - - Retinal (11-cis)
small-molecule Inverse agonist - - No No Teller DC, Okada T, Behnke CA, Palczewski K, Stenkamp RE 10.1021/BI0155091 2001-07-04 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 1F88 - 2.8 A Inactive 24 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 2G87 2G87_refined 2.6 A Inactive 24 100 - - - - - - Retinal (all-trans)
small-molecule Agonist - - No No - 10.1002/ANIE.200600595 2006-09-02 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 1L9H - 2.6 A Inactive 24 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 1GZM 1GZM_refined 2.7 A Inactive 24 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, noradrenaline, (-)-adrenaline, 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 Japanese flying squid X-ray 2ZIY - 3.7 A Inactive 9 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 2HPY - 2.8 B Inactive 24 100 - - - - - - Retinal (all-trans)
small-molecule Agonist - - No No - 10.1073/PNAS.0601765103 2006-08-22 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 2J4Y - 3.4 B Inactive 24 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 2I36 - 4.1 A Inactive 24 94 - - - - - - Apo (no ligand)
none Apo (no ligand) - - No No - 10.1073/PNAS.0608022103 2006-10-17 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 2PED - 3.0 B Inactive 24 100 - - - - - - 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 2R4R 2R4R_refined 3.4 A Inactive 1 52 - - - - - Antibody Carazolol
small-molecule Inverse agonist L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline small-molecule No No - - 2007-11-06 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, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline small-molecule No No - 10.1038/NATURE06325 2007-11-06 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 2I37 2I37_refined 4.2 A Inactive 24 91 - - - - - - Apo (no ligand)
none Apo (no ligand) - - No No - - 2006-10-17 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 3DQB - 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
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 - 10.1126/SCIENCE.1164772 2008-10-14 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 3C9L 3C9L_refined 2.7 A Inactive 24 94 - - - - - - Retinal (11-cis)
small-molecule Inverse agonist - - No No - - 2008-08-05 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 3CAP - 2.9 A Active 97 94 - - - - - - Apo (no ligand)
none Apo (no ligand) - - No No - 10.1038/NATURE07063 2008-06-24 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 3D4S 3D4S_refined 2.8 A Inactive 0 67 - - - - T4-Lysozyme - timolol
small-molecule Inverse agonist L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline small-molecule No No - 10.1016/J.STR.2008.05.001 2008-06-17 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 3NYA 3NYA_refined 3.2 A Inactive 0 67 - - - - T4-Lysozyme - CHEMBL1160734
small-molecule Antagonist L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline small-molecule No No - - 2010-08-11 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 3C9M - 3.4 A Inactive 24 94 - - - - - - Retinal (11-cis)
small-molecule Inverse agonist - - No No - 10.1107/S0907444908017162 2008-08-05 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 3NY9 3NY9_refined 2.8 A Inactive 0 67 - - - - T4-Lysozyme - CHEMBL1233771
small-molecule Inverse agonist L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline small-molecule No No - 10.1021/JA105108Q 2010-08-11 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 3NY8 3NY8_refined 2.8 A Inactive 0 67 - - - - T4-Lysozyme - ICI 118551
small-molecule Inverse agonist L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline small-molecule No No - - 2010-08-11 Yes
OPSD Rhodopsin Opsins A Japanese flying squid X-ray 2Z73 2Z73_refined 2.5 A Inactive 9 78 - - - - - - Retinal (11-cis)
small-molecule Inverse agonist - - No No - 10.1038/NATURE06925 2008-05-13 Yes
CXCR4 CXCR4 Chemokine A Human X-ray 3OE6 3OE6_refined 3.2 A Inactive 6 77 - - - - T4-Lysozyme - isothiourea-1t
small-molecule Antagonist CXCL12γ, CXCL12β, CXCL12, CXCL12α, CXCL12δ, CXCL12φ, CXCL12ε peptide No No - 10.1126/SCIENCE.1194396 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
CXCR4 CXCR4 Chemokine A Human X-ray 3OE0 - 2.9 A Inactive 6 78 - - - - T4-Lysozyme - CVX15
peptide Antagonist CXCL12γ, CXCL12β, CXCL12, CXCL12α, CXCL12δ, CXCL12φ, CXCL12ε peptide No No - - 2010-10-27 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 3KJ6 - 3.4 A Inactive 1 54 - - - - - Antibody Carazolol
small-molecule Inverse agonist L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, 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 6 83 - - - - T4-Lysozyme - isothiourea-1t
small-molecule Antagonist CXCL12γ, CXCL12β, CXCL12, CXCL12α, CXCL12δ, CXCL12φ, CXCL12ε peptide No No - - 2010-10-27 Yes
CXCR4 CXCR4 Chemokine A Human X-ray 3OE8 3OE8_refined 3.1 A Inactive 6 76 - - - - T4-Lysozyme - isothiourea-1t
small-molecule Antagonist CXCL12γ, CXCL12β, CXCL12, CXCL12α, CXCL12δ, CXCL12φ, CXCL12ε peptide No No - - 2010-10-27 Yes
CXCR4 CXCR4 Chemokine A Human X-ray 3OE9 3OE9_refined 3.1 A Inactive 6 74 - - - - T4-Lysozyme - isothiourea-1t
small-molecule Antagonist CXCL12γ, CXCL12β, CXCL12, CXCL12α, CXCL12δ, CXCL12φ, CXCL12ε peptide No No - 10.1126/SCIENCE.1194396 2010-10-27 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 2Y00 2Y00_refined 2.5 B Inactive 0 62 - - - - - - Dobutamine
small-molecule Agonist (partial) - - No No Warne T, Moukhametzianov R, Baker JG, Nehme R, Edwards PC, Leslie AG, Schertler GF, Tate CG 10.1038/NATURE09746 2011-01-12 Yes
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 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, noradrenaline, (-)-adrenaline, 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 24 100 - - - - - - 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, noradrenaline, (-)-adrenaline, 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 - - 2011-03-09 Yes
AA2AR A2A Adenosine A Human X-ray 3QAK 3QAK_refined 2.7 A Active 72 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 3PXO - 3.0 A Active 97 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
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 72 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 72 75 - - - - - - NECA
small-molecule Agonist adenosine small-molecule No No - - 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 - - 2011-06-01 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
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
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
ADRB2 β2 Adrenoceptors A Human X-ray 3SN6 - 3.2 R Active 100 69 Gs αs - 89 T4-Lysozyme Antibody CHEMBL1615159
small-molecule Agonist L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline small-molecule No No Rasmussen SG, DeVree BT, Zou Y, Kruse AC, Chung KY, Kobilka TS, Thian FS, Chae PS, Pardon E, Calinski D, Mathiesen JM, Shah ST, Lyons JA, Caffrey M, Gellman SH, Steyaert J, Skiniotis G, Weis WI, Sunahara RK, Kobilka BK 10.1038/NATURE10361 2011-07-20 Yes
OPSD Rhodopsin Opsins A Japanese flying squid X-ray 3AYM - 2.8 B Inactive 9 77 - - - - - - Retinal (all-trans)
small-molecule Agonist - - No No Murakami M, Kouyama T 10.1016/J.JMB.2011.08.044 2011-08-17 Yes
OPSD Rhodopsin Opsins A Japanese flying squid X-ray 3AYN - 2.7 B Inactive 9 77 - - - - - - Retinal (9-cis)
small-molecule Inverse agonist - - No No Murakami M, Kouyama T 10.1016/J.JMB.2011.08.044 2011-08-17 Yes
AA2AR A2A Adenosine A Human X-ray 3PWH 3PWH_refined 3.3 A Inactive 0 71 - - - - - - ZM-241385
small-molecule Antagonist adenosine small-molecule No No Dore AS, Robertson N, Errey JC, Ng I, Hollenstein K, Tehan B, Hurrell E, Bennett K, Congreve M, Magnani F, Tate CG, Weir M, Marshall FH 10.1016/J.STR.2011.06.014 2011-09-07 Yes
AA2AR A2A Adenosine A Human X-ray 3REY 3REY_refined 3.3 A Inactive 0 71 - - - - - - xanthine amine congener
small-molecule Antagonist adenosine small-molecule No No - - 2011-09-07 Yes
AA2AR A2A Adenosine A Human X-ray 3RFM 3RFM_refined 3.6 A Inactive 0 71 - - - - - - caffeine
small-molecule Antagonist adenosine small-molecule No No - - 2011-09-07 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 Deupi X, Edwards P, Singhal A, Nickle B, Oprian D, Schertler G, Standfuss J 10.1073/PNAS.1114089108 2012-01-25 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 0 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 0 72 - - - - - - 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
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
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 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
5HT2B 5-HT2B 5-Hydroxytryptamine A Human X-ray 4NC3 - 2.8 A Active 59 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
CXCR4 CXCR4 Chemokine A Human X-ray 4RWS 4RWS_refined 3.1 A Inactive 6 78 - - - - T4-Lysozyme - vMIP-II
peptide Antagonist CXCL12γ, CXCL12β, CXCL12, CXCL12α, CXCL12δ, CXCL12φ, CXCL12ε peptide No No Qin L, Kufareva I, Holden LG, Wang C, Zheng Y, Zhao C, Fenalti G, Wu H, Han GW, Cherezov V, Abagyan R, Stevens RC, Handel TM 10.1126/SCIENCE.1261064 2015-02-11 Yes
AA2AR A2A Adenosine A Human X-ray 5UVI 5UVI_refined 3.2 A Inactive 0 72 - - - - BRIL - ZM-241385
small-molecule Antagonist adenosine small-molecule No No Martin-Garcia JM, Conrad CE, Nelson G, Stander N, Zatsepin NA, Zook J, Zhu L, Geiger J, Chun E, Kissick D, Hilgart MC, Ogata C, Ishchenko A, Nagaratnam N, Roy-Chowdhury S, Coe J, Subramanian G, Schaffer A, James D, Ketwala G, Venugopalan N, Xu S, Corcoran S, Ferguson D, Weierstall U, Spence JCH, Cherezov V, Fromme P, Fischetti RF, Liu W 10.1107/S205225251700570X 2017-05-24 Yes
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
AA2AR A2A Adenosine A Human X-ray 5WF5 5WF5_refined 2.6 A Active 72 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
OPSD Rhodopsin Opsins A Bovine X-ray 6FUF - 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
PE2R4 EP4 Prostanoid A Human X-ray 5YWY 5YWY_refined 3.2 A Inactive 11 57 - - - - - Fab ONO-AE3-208
small-molecule Antagonist thromboxane A2, PGF2α, PGI2, PGD2, PGE1, PGE2 small-molecule No No Toyoda Y, Morimoto K, Suno R, Horita S, Yamashita K, Hirata K, Sekiguchi Y, Yasuda S, Shiroishi M, Shimizu T, Urushibata Y, Kajiwara Y, Inazumi T, Hotta Y, Asada H, Nakane T, Shiimura Y, Nakagita T, Tsuge K, Yoshida S, Kuribara T, Hosoya T, Sugimoto Y, Nomura N, Sato M, Hirokawa T, Kinoshita M, Murata T, Takayama K, Yamamoto M, Narumiya S, Iwata S, Kobayashi T 10.1038/S41589-018-0131-3 2018-12-05 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 Stauch B, Johansson LC, McCorvy JD, Patel N, Han GW, Huang XP, Gati C, Batyuk A, Slocum ST, Ishchenko A, Brehm W, White TA, Michaelian N, Madsen C, Zhu L, Grant TD, Grandner JM, Shiriaeva A, Olsen RHJ, Tribo AR, Yous S, Stevens RC, Weierstall U, Katritch V, Roth BL, Liu W, Cherezov V 10.1038/S41586-019-1141-3 2019-04-24 Yes
CCR7 CCR7 Chemokine A Human X-ray 6QZH 6QZH_refined 2.1 A Inactive 6 71 - - - - Sialidase NanA - SCHEMBL13407377
small-molecule Allosteric antagonist CCL21, CCL19 peptide No No Jaeger K, Bruenle S, Weinert T, Guba W, Muehle J, Miyazaki T, Weber M, Furrer A, Haenggi N, Tetaz T, Huang CY, Mattle D, Vonach JM, Gast A, Kuglstatter A, Rudolph MG, Nogly P, Benz J, Dawson RJP, Standfuss J 10.1016/J.CELL.2019.07.028 2019-09-04 Yes
DRD4 D4 Dopamine A Mouse X-ray 6IQL 6IQL_refined 3.5 A Inactive 17 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
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, PHI, PHM, PHV, PACAP-27, PACAP-38 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 6PH7 - 2.9 A Active 100 94 Gi/o αt2 Only H5 3 - - Nerol
small-molecule unknown - - No No - - 2020-07-01 Yes
ADRB2 β2 Adrenoceptors A Human Cryo-EM 7BZ2 7BZ2_refined 3.8 R Active 100 69 Gs αs - 50 - Nanobody-35 ARFORMOTEROL
small-molecule Agonist L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline 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
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 tryptamine, 5-hydroxytryptamine 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 7BTS 7BTS_refined 3.1 A Active 99 58 - - - - T4-Lysozyme Camelid antibody fragment Nb6B9 (-)-adrenaline
small-molecule Agonist (-)-adrenaline, (-)-noradrenaline, 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 7D77 - 2.9 R Active 100 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
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		 L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine small-molecule No No - - 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 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
GRM1 mGlu1 Metabotropic glutamate C Human Cryo-EM 7DGE 7DGE_refined 3.7 A Intermediate - 66 - - - - - Nanobody-43 quisqualate
small-molecule Agonist L-glutamic acid small-molecule No No Zhang J, Qu L, Wu L, Tang X, Luo F, Xu W, Xu Y, Liu ZJ, Hua T 10.1007/S13238-020-00808-5 2021-09-22 Yes
GP158 GPR158 C Orphans C Human Cryo-EM 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
FPR1 FPR1 Formylpeptide A Human Cryo-EM 7T6T 7T6T_refined 3.2 R Active 100 85 Gi/o αi1 - 61 - - synthetic peptide
peptide Agonist fMet-Leu-Phe, cathepsin G, annexin I, spinorphin 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 7TYF - 2.2 R Active 100 77 Gs αs - 58 - Nanobody-35
RAMP1		 amylin peptide
peptide Agonist adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), 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
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-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) 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
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 L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine small-molecule No No - - 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-58, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8 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 0 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 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, anandamide, N-palmitoylethanolamine, 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
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
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
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
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 pancreatic polypeptide, neuropeptide Y-(3-36), PYY-(3-36), neuropeptide Y, peptide YY peptide No No Kang H, Park C, Choi YK, Bae J, Kwon S, Kim J, Choi C, Seok C, Im W, Choi HJ 10.1016/J.STR.2022.11.010 2023-03-22 Yes
GPR20 GPR20 A orphans A Human Cryo-EM 8HS2 - 3.1 R Active 59 80 - - - - BRIL Antibody fab fragment heavy chain
Antibody fab fragment light chain		 Apo (no ligand)
none Apo (no ligand) - - No No Lin X, Jiang S, Wu Y, Wei X, Han GW, Wu L, Liu J, Chen B, Zhang Z, Zhao S, Cherezov V, Xu F 10.1038/S41421-023-00520-8 2023-03-08 Yes
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 7ZL9 - 2.7 A Active 59 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
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, C5a, C5a des-Arg, C3a 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
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 L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, 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
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
PE2R3 EP3 Prostanoid A Human Cryo-EM 8GDC 8GDC_refined 3.5 R Active 100 66 Gi/o αi1 - 58 - - PGE2
small-molecule Agonist thromboxane A2, PGF2α, PGI2, PGD2, 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
GASR CCK2 Cholecystokinin A Human Cryo-EM 8IA7 8IA7_refined 3.1 R Active 100 62 Gq/11 αq - 61 - - CHEMBL216166
protein Agonist desulfated gastrin-14, desulfated cholecystokinin-8, gastrin-34, gastrin-14, CCK-58, desulfated gastrin-17, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8, desulfated gastrin-34, gastrin-71, desulfated 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 2023-12-06 Yes
GLR glucagon Glucagon B1 Human Cryo-EM 8JIT - 2.9 R Active 100 83 Gs αs - 58 - Nanobody-35 MEDI0382
peptide Agonist glucagon peptide No No Li Y, Zhou Q, Dai A, Zhao F, Chang R, Ying T, Wu B, Yang D, Wang MW, Cong Z 10.1073/PNAS.2303696120 2023-09-06 Yes
TAAR1 TA1 Trace amine A Mouse Cryo-EM 8WC5 - 3.3 R Active 100 78 Gs αs - 58 - scFv16 Tetramethylammonium
small-molecule Agonist β-phenylethylamine, 3-iodothyronamine, 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
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
OX2R OX2 Orexin A Human X-ray 4S0V 4S0V_refined 2.5 A Inactive 0 64 - - - - Glycogen synthase - suvorexant
small-molecule Antagonist orexin-A, orexin-B 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 97 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
AA2AR A2A Adenosine A Human X-ray 5MZJ 5MZJ_refined 2.0 A Inactive 0 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 5OLO 5OLO_refined 3.1 A Inactive 0 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
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 89 70 - - - - T4-Lysozyme - Misoprostol-FA
small-molecule Agonist thromboxane A2, PGF2α, PGI2, PGD2, PGE1, PGE2 small-molecule No No Audet M, White KL, Breton B, Zarzycka B, Han GW, Lu Y, Gati C, Batyuk A, Popov P, Velasquez J, Manahan D, Hu H, Weierstall U, Liu W, Shui W, Katritch V, Cherezov V, Hanson MA, Stevens RC 10.1038/S41589-018-0160-Y 2018-12-05 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 Stauch B, Johansson LC, McCorvy JD, Patel N, Han GW, Huang XP, Gati C, Batyuk A, Slocum ST, Ishchenko A, Brehm W, White TA, Michaelian N, Madsen C, Zhu L, Grant TD, Grandner JM, Shiriaeva A, Olsen RHJ, Tribo AR, Yous S, Stevens RC, Weierstall U, Katritch V, Roth BL, Liu W, Cherezov V 10.1038/S41586-019-1141-3 2019-04-24 Yes
OPSD Rhodopsin Opsins A Bovine Cryo-EM 6OFJ 6OFJ_refined 4.5 A Inactive 24 93 - - - - - - Apo (no ligand)
none Apo (no ligand) - - No No Zhao DY, Poge M, Morizumi T, Gulati S, Van Eps N, Zhang J, Miszta P, Filipek S, Mahamid J, Plitzko JM, Baumeister W, Ernst OP, Palczewski K 10.1074/JBC.RA119.010089 2019-08-21 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 Ishchenko A, Stauch B, Han GW, Batyuk A, Shiriaeva A, Li C, Zatsepin N, Weierstall U, Liu W, Nango E, Nakane T, Tanaka R, Tono K, Joti Y, Iwata S, Moraes I, Gati C, Cherezov V 10.1107/S2052252519013137 2019-11-13 Yes
AGTR2 AT2 Angiotensin A Human X-ray 6JOD 6JOD_refined 3.2 A Active 100 84 - - - - BRIL Heavy chain of 4A03Fab
Light chain of 4A03Fab		 angiotensin II
peptide Agonist angiotensin-(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
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 CXCL8, CXCL1, CXCL5, CXCL2, CXCL7, CXCL6, CXCL3 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
CASR CaS Calcium-sensing C Human Cryo-EM 7DTU 7DTU_refined 4.4 A Intermediate - 72 - - - - - - L-tryptophan
small-molecule PAM Mg2+, L-tryptophan, spermine, Ca2+ 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 7M3J 7M3J_refined 4.1 A Inactive - 72 - - - - - - NPS 2143
small-molecule NAM Mg2+, L-tryptophan, spermine, Ca2+ 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 27 83 - - - - T4-Lysozyme - 15(R)-15-methyl-PGD2
small-molecule Antagonist thromboxane A2, PGF2α, PGI2, PGJ2, PGD3, PGD2, PGE2 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 7FIH - 3.2 R Active 100 79 Gs αs - 60 - - Glycoprotein alpha
Choriogonadotropin beta
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
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
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
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
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
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-28, cortistatin-14, CST-17, SRIF-14 peptide No No Zhao W, Han S, Qiu N, Feng W, Lu M, Zhang W, Wang M, Zhou Q, Chen S, Xu W, Du J, Chu X, Yi C, Dai A, Hu L, Shen MY, Sun Y, Zhang Q, Ma Y, Zhong W, Yang D, Wang MW, Wu B, Zhao Q 10.1038/S41422-022-00679-X 2022-08-03 Yes
AGRG2 ADGRG2 ADGRG B2 Mouse Cryo-EM 7XKF - 2.4 R Active 100 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 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 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 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
AGRF1 ADGRF1 ADGRF B2 Human Cryo-EM 7WZ7 - 2.8 R Active 100 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 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
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 TIP39, PTHrP-(1-36), PTHrP, PTH 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 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 Lin X, Chen B, Wu Y, Han Y, Qi A, Wang J, Yang Z, Wei X, Zhao T, Wu L, Xie X, Sun J, Zheng J, Zhao S, Xu F 10.1038/S41467-023-35882-W 2023-03-15 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, relaxin-1, relaxin-3 peptide No No - - 2023-02-15 Yes
OPRK κ Opioid A Human Cryo-EM 8DZR - 2.6 A Active 100 68 Gi/o αgust - 58 - scFv16 CHEMBL277863
small-molecule Agonist [Leu]enkephalin, β-neoendorphin, β-endorphin, dynorphin A, [Met]enkephalin, α-neoendorphin, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13), big dynorphin 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
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 100 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
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 myristic acid, linoleic acid, α-linolenic acid, oleic 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
GPR84 GPR84 A orphans A Human Cryo-EM 8J1A - 3.2 R Active 100 73 Gi/o αi1 - 62 - scFv16 Apo (no ligand)
none Apo (no ligand) - - No No Liu H, Zhang Q, He X, Jiang M, Wang S, Yan X, Cheng X, Liu Y, Nan FJ, Xu HE, Xie X, Yin W 10.1038/S41467-023-38985-6 2023-06-21 Yes
GLR glucagon Glucagon B1 Human Cryo-EM 8JRV - 3.3 R Active 100 64 Beta Beta-arrestin-1 - 85 - scFv30
Nanobody-32		 glucagon
peptide Agonist glucagon peptide No No Chen K, Zhang C, Lin S, Yan X, Cai H, Yi C, Ma L, Chu X, Liu Y, Zhu Y, Han S, Zhao Q, Wu B 10.1038/S41586-023-06420-X 2023-08-16 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 8FCZ - 3.7 A Inactive 24 89 - - - - - Nanobody-2 Retinal (11-cis)
small-molecule Inverse agonist - - No No Wu A, Salom D, Hong JD, Tworak A, Watanabe K, Pardon E, Steyaert J, Kandori H, Katayama K, Kiser PD, Palczewski K 10.1038/S41467-023-40911-9 2023-08-30 Yes
CXCR3 CXCR3 Chemokine A Human Cryo-EM 8HNN - 3.6 R Inactive 6 70 - - - - - Nanobody-6 CHEMBL1921858
small-molecule Antagonist CCL19, CXCL11, CCL13, CXCL9, CXCL10, CCL7, CCL5, CCL11, CXCL12α, CCL20 peptide No No Jiao H, Pang B, Liu A, Chen Q, Pan Q, Wang X, Xu Y, Chiang YC, Ren R, Hu H 10.1038/S41594-023-01175-5 2023-11-29 Yes
HCAR2 HCA2 Hydroxycarboxylic acid A Human Cryo-EM 8IHI - 3.1 R Active 100 80 Gi/o αi1 - 62 BRIL scFv16 (5S)-5-methyl-4-oxo-5-phenylfuran-2-carboxylic acid
small-molecule Agonist β-D-hydroxybutyric acid, butyric acid small-molecule No No Suzuki S, Tanaka K, Nishikawa K, Suzuki H, Oshima A, Fujiyoshi Y 10.1038/S41467-023-41650-7 2023-08-30 Yes
HCAR2 HCA2 Hydroxycarboxylic acid A Human Cryo-EM 8JII - 3.2 A Active 100 80 Gi/o αi1 - 64 - scFv16 nicotinic acid
compound 9n [PMID: 18752940]
small-molecule
small-molecule		 Agonist
PAM		 β-D-hydroxybutyric acid, butyric acid small-molecule No No Zhao C, Wang H, Liu Y, Cheng L, Wang B, Tian X, Fu H, Wu C, Li Z, Shen C, Yu J, Yang S, Hu H, Fu P, Ma L, Wang C, Yan W, Shao Z 10.1016/J.MOLCEL.2023.07.030 2023-09-06 Yes
GP174 GPR174 A orphans A Human Cryo-EM 8KH5 - 2.8 A Active 100 84 Gs αs - 58 - Nanobody-35 Lysophosphotidylserine
small-molecule Agonist lysophosphatidylserine small-molecule No No Nie Y, Qiu Z, Chen S, Chen Z, Song X, Ma Y, Huang N, Cyster JG, Zheng S 10.1038/S41467-023-41654-3 2023-10-18 Yes
TAAR1 TA1 Trace amine A Mouse Cryo-EM 8WCC - 3.0 R Active 98 81 - - - - - - Cyclohexylammonium ion
small-molecule Agonist β-phenylethylamine, 3-iodothyronamine, 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
AA2AR A2A Adenosine A Human X-ray 3UZA 3UZA_refined 3.3 A Inactive 0 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
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
OPRD δ Opioid A Human X-ray 4RWD 4RWD_refined 2.7 A Inactive 6 79 - - - - BRIL - DIPP-NH2
peptide Antagonist [Leu]enkephalin, β-endorphin, dynorphin A, [Met]enkephalin, endomorphin-1, α-neoendorphin, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13) 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
CRFR1 CRF1 Corticotropin-releasing factor B1 Human X-ray 4Z9G - 3.2 A Inactive 16 63 - - - - T4-Lysozyme - CP 376,395
small-molecule Antagonist urocortin 1, corticotrophin-releasing hormone, urocortin 2 peptide No No Dore AS, Bortolato A, Hollenstein K, Cheng RKY, Read RJ, Marshall FH 10.2174/1874467210666170110114727 2016-06-29 Yes
CALCR CT Calcitonin B1 Human Cryo-EM 5UZ7 - 4.1 R Active 100 56 Gs αs - 47 - - calcitonin (salmon synthetic)
small-molecule Agonist adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), 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
Q9WTK1 BLT1 Leukotriene A Guinea pig X-ray 5X33 5X33_refined 3.7 A Inactive 6 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 6FKB 6FKB_refined 3.0 A Active 97 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
5HT2B 5-HT2B 5-Hydroxytryptamine A Human X-ray 6DRZ - 3.1 A Active 59 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
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 Liu H, Hofmann J, Fish I, Schaake B, Eitel K, Bartuschat A, Kaindl J, Rampp H, Banerjee A, Hubner H, Clark MJ, Vincent SG, Fisher JT, Heinrich MR, Hirata K, Liu X, Sunahara RK, Shoichet BK, Kobilka BK, Gmeiner P 10.1073/PNAS.1813988115 2018-11-28 Yes
MTR1A MT1 Melatonin A Human X-ray 6ME4 6ME4_refined 3.2 A Inactive 1 83 - - - - GlgA glycogen synthase - 2-iodo-melatonin
small-molecule Agonist melatonin small-molecule No No Stauch B, Johansson LC, McCorvy JD, Patel N, Han GW, Huang XP, Gati C, Batyuk A, Slocum ST, Ishchenko A, Brehm W, White TA, Michaelian N, Madsen C, Zhu L, Grant TD, Grandner JM, Shiriaeva A, Olsen RHJ, Tribo AR, Yous S, Stevens RC, Weierstall U, Katritch V, Roth BL, Liu W, Cherezov V 10.1038/S41586-019-1141-3 2019-04-24 Yes
SUCR1 succinate Succinate A Rat X-ray 6RNK - 1.9 A Active 59 90 - - - - - Nanobody-6 NF-56-EJ40
small-molecule Antagonist - - No No - - 2019-08-14 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, noradrenaline, (-)-adrenaline, 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
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-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) 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 humanin, aspirin-triggered resolvin D1, LXA4, resolvin D1, serum amyloid A, PrP106-126, 15-deoxy-LXA4, aspirin triggered lipoxin A4, LL-37, LTC4, annexin I, fMet-Leu-Phe, LTD4 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 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
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 thromboxane A2, PGF2α, PGI2, PGD2, PGE1, PGE2 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 6Z8N 6Z8N_refined 2.8 A Intermediate 17 80 - - - - DARPin D12 - (2~{S})-4-methyl-2-[(1-quinolin-8-ylsulfonylindol-3-yl)carbonylamino]pentanoic acid
small-molecule Agonist neurotensin, neuromedin N peptide No No Deluigi M, Klipp A, Klenk C, Merklinger L, Eberle SA, Morstein L, Heine P, Mittl PRE, Ernst P, Kamenecka TM, He Y, Vacca S, Egloff P, Honegger A, Pluckthun A 10.1126/sciadv.abe5504 2021-02-10 Yes
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
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		 Mg2+, L-tryptophan, spermine, Ca2+ 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
AA2AR A2A Adenosine A Human MicroED 7RM5 7RM5_refined 2.8 A Inactive 0 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
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 [des-Arg10]kallidin, Lys-[Hyp3]-bradykinin, kallidin, [des-Arg9]bradykinin, [Hyp3]bradykinin, T-kinin, bradykinin 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 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
GHSR ghrelin Ghrelin A Human X-ray 7F83 7F83_refined 2.9 A Inactive 15 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
SSR2 SST2 Somatostatin A Human Cryo-EM 7T10 - 2.5 R Active 100 78 Gi/o αi3 - 62 - scFv16 SOMATOSTATIN
protein Agonist SRIF-28, cortistatin-14, CST-17, SRIF-14 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 7TZF - 2.4 R Active 100 77 Gs αs - 59 - Nanobody-35
RAMP3		 amylin peptide
peptide Agonist adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), 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
NMUR2 NMU2 Neuromedin U A Human Cryo-EM 7W55 - 2.8 R Active 100 73 Gq/11 αq - 60 - scFv16 Neuromedin U-25 (human)
peptide Agonist neuromedin U-23, neuromedin S-36, neuromedin S-33, neuromedin U-25 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 gastrin-14, desulfated cholecystokinin-8, gastrin-34, gastrin-14, CCK-58, desulfated gastrin-17, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8, desulfated gastrin-34, gastrin-71, desulfated 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
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
PTH1R PTH1 Parathyroid hormone B1 Human Cryo-EM 7VVK - 3.3 R Active 100 56 Gs αs - 58 - Nanobody-35 teriparatide
peptide Agonist TIP39, PTHrP-(1-36), PTHrP, PTH 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 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
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
OPRM μ Opioid A Human Cryo-EM 8EF5 - 3.3 R Active 100 72 Gi/o αi1 - 64 - scFv16 fentanyl
small-molecule Agonist [Leu]enkephalin, β-endorphin, dynorphin A, [Met]enkephalin, endomorphin-1, endomorphin-2, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13) 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 24 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 0 69 - - - - - Antibody fab fragment light chain
Antibody fab fragment heavy chain		 istradefylline
small-molecule Antagonist adenosine small-molecule No No Ohno Y, Suzuki M, Asada H, Kanda T, Saki M, Miyagi H, Yasunaga M, Suno C, Iwata S, Saito JI, Uchida S 10.1124/MOLPHARM.122.000633 2023-03-22 Yes
FFAR4 FFA4 Free fatty acid A Human Cryo-EM 8ID3 8ID3_refined 3.1 R Active 100 81 Gi/o αi1 - 64 - scFv16 9-Hydroxyoctadecanoic acid
small-molecule Agonist myristic acid, linoleic acid, α-linolenic acid, oleic acid small-molecule No No Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP 10.1126/SCIENCE.ADD6220 2023-03-15 Yes
TAAR9 TAAR9 A orphans A Mouse Cryo-EM 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 TIP39, PTHrP-(1-36), PTHrP, PTH peptide No No Cary BP, Gerrard EJ, Belousoff MJ, Fletcher MM, Jiang Y, Russell IC, Piper SJ, Wootten D, Sexton PM 10.1016/J.STR.2023.04.002 2023-04-26 Yes
PTH1R PTH1 Parathyroid hormone B1 Human Cryo-EM 7Y35 - 2.9 R Active 100 63 Gs αs - 57 - Nanobody-35 abaloparatide
small-molecule Agonist TIP39, PTHrP-(1-36), PTHrP, PTH peptide No No - - 2023-07-05 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
AA2AR A2A Adenosine A Human X-ray 8JWY - 2.3 A Inactive 0 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
OPRK κ Opioid A Human Cryo-EM 8FEG - 2.5 B Active 100 73 Gi/o αi1 - 55 - scFv16 ACE-TYR-ALA-DTY-THR-THR-CYS-THR-DPN-XT9
peptide Agonist [Leu]enkephalin, β-neoendorphin, β-endorphin, dynorphin A, [Met]enkephalin, α-neoendorphin, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13), big dynorphin peptide No No Cheng Y, Prusoff WH 10.1016/0006-2952(73)90196-2 2023-12-06 Yes
C3AR C3a Complement peptide A Human Cryo-EM 8I9A - 3.6 C Active 100 56 Gq/11 αq - 58 - scFv16 EP54 ligand
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
HCAR2 HCA2 Hydroxycarboxylic acid A Human Cryo-EM 8J6P - 2.6 R Active 100 81 Gi/o αi1 - 64 - scFv16 nicotinic acid
small-molecule Agonist β-D-hydroxybutyric acid, butyric acid small-molecule No No Mao C, Gao M, Zang SK, Zhu Y, Shen DD, Chen LN, Yang L, Wang Z, Zhang H, Wang WW, Shen Q, Lu Y, Ma X, Zhang Y 10.1038/S41467-023-43537-Z 2023-12-06 Yes
AGRL3 ADGRL3 ADGRL B2 Human Cryo-EM 8JMT - 3.3 A Inactive 0 16 - - - - BRIL - Apo (no ligand)
none Apo (no ligand) - - No No Guo Q, He B, Zhong Y, Jiao H, Ren Y, Wang Q, Ge Q, Gao Y, Liu X, Du Y, Hu H, Tao Y 10.1038/S41589-023-01389-0 2023-09-06 Yes
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 Mg2+, L-tryptophan, spermine, Ca2+ 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
AA2AR A2A Adenosine A Human X-ray 3UZC 3UZC_refined 3.3 A Inactive 0 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
OPRD δ Opioid A Human X-ray 4N6H 4N6H_refined 1.8 A Inactive 6 81 - - - - BRIL - naltrindole
small-molecule Antagonist [Leu]enkephalin, β-endorphin, dynorphin A, [Met]enkephalin, endomorphin-1, α-neoendorphin, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13) 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
US28 US28 Unclassified A strain AD169 X-ray 4XT3 4XT3_refined 3.8 A Active 100 81 - - - - - - CX3CL1
peptide Agonist (partial) - - No No - - 2015-03-04 Yes
AA2AR A2A Adenosine A Human X-ray 5K2D 5K2D_refined 1.9 A Inactive 0 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
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
DRD2 D2 Dopamine A Human X-ray 6CM4 6CM4_refined 2.9 A Inactive 0 59 - - - - T4-Lysozyme - risperidone
small-molecule Inverse agonist dopamine small-molecule No No Wang S, Che T, Levit A, Shoichet BK, Wacker D, Roth BL 10.1038/NATURE25758 2018-03-14 Yes
5HT2B 5-HT2B 5-Hydroxytryptamine A Human X-ray 6DRY - 2.9 A Active 59 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
PE2R4 EP4 Prostanoid A Human X-ray 5YHL 5YHL_refined 4.2 A Inactive 11 57 - - - - - Fab ONO-AE3-208-Br
small-molecule Antagonist thromboxane A2, PGF2α, PGI2, PGD2, PGE1, PGE2 small-molecule No No Toyoda Y, Morimoto K, Suno R, Horita S, Yamashita K, Hirata K, Sekiguchi Y, Yasuda S, Shiroishi M, Shimizu T, Urushibata Y, Kajiwara Y, Inazumi T, Hotta Y, Asada H, Nakane T, Shiimura Y, Nakagita T, Tsuge K, Yoshida S, Kuribara T, Hosoya T, Sugimoto Y, Nomura N, Sato M, Hirokawa T, Kinoshita M, Murata T, Takayama K, Yamamoto M, Narumiya S, Iwata S, Kobayashi T 10.1038/S41589-018-0131-3 2018-12-05 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 TIP39, PTHrP-(1-36), PTHrP, PTH peptide No No Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y 10.1126/SCIENCE.AAV7942 2019-04-17 Yes
CLTR2 CysLT2 Leukotriene A Human X-ray 6RZ8 - 2.7 A Active 59 78 - - - - BRIL - ONO-2080365
small-molecule Antagonist LTD4, LTC4, LTE4 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 1, corticotrophin-releasing hormone, urocortin 2, urocortin 3 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
OXYR OT Vasopressin and oxytocin A Human X-ray 6TPK 6TPK_refined 3.2 A Inactive 17 68 - - - - GlgA glycogen synthase - retosiban
small-molecule Antagonist vasopressin, oxytocin peptide No No Waltenspuhl Y, Schoppe J, Ehrenmann J, Kummer L, Pluckthun A 10.1126/SCIADV.ABB5419 2020-08-05 Yes
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 6X19 - 2.1 R Active 100 84 Gs αs - 89 - Nanobody-35 CHU-128
small-molecule Agonist glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) 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
ADRB2 β2 Adrenoceptors A Human Cryo-EM 7DHI - 3.3 R Active 100 70 Gs αs - 55 - Nanobody-35 levosalbutamol
small-molecule Agonist L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline small-molecule No No Si G, Du Y, Tang P, Ma G, Jia Z, Zhou X, Mu D, Shen Y, Lu Y, Mao Y, Chen C, Li Y, Gu N 10.1093/NSR/NWAA284 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 L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, 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
GABR2 GABAB2 GABAB C Human Cryo-EM 7EB2 - 3.5 D Active - 72 Gi/o αi1 - 99 - scFv16 (-)-baclofen
BHFF
small-molecule
small-molecule		 Agonist
PAM		 - - No No Shen C, Mao C, Xu C, Jin N, Zhang H, Shen DD, Shen Q, Wang X, Hou T, Chen Z, Rondard P, Pin JP, Zhang Y, Liu J 10.1038/S41586-021-03507-1 2021-05-05 Yes
GLP1R GLP-1 Glucagon B1 Human Cryo-EM 7DUR - 3.3 R Active 100 80 Gs αs - 60 - Nanobody-35 N-Tert-butyl-6,7-dichloroquinoxalin-2-amine
small-molecule Ago-PAM glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) 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
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 7F55 - 3.1 R Active 100 82 Gs αs - 58 - Nanobody-35 bremelanotide
peptide Agonist β-MSH, α-MSH, agouti-related protein, 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 7VV4 7VV4_refined 3.0 R Active 98 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
5HT2A 5-HT2A 5-Hydroxytryptamine A Human X-ray 7WC5 7WC5_refined 3.2 A Inactive 1 60 - - - - BRIL - psilocin
small-molecule Agonist tryptamine, 5-hydroxytryptamine 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 β-MSH, ACTH, γ-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 7TYX - 2.6 R Active 100 77 Gs αs - 59 - Nanobody-35 Amylin rat
peptide Agonist adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), 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
AGRF1 ADGRF1 ADGRF B2 Human Cryo-EM 7WU4 - 3.4 R Active 100 31 Gi/o αi1 Mini-Gi1 58 - - Apo (no ligand)
none Apo (no ligand) - - No No - - 2022-04-27 Yes
NPY2R Y2 Neuropeptide Y A Human Cryo-EM 7X9B 7X9B_refined 3.4 R Active 100 79 Gi/o αi1 - 62 - - neuropeptide Y