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RECEPTOR
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STRUCTURE
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SIGNAL PROTEIN
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AUXILIARY PROTEIN
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STRUCTURE LIGAND
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PHYSIOLOGICAL LIGAND
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SODIUM ION SITE
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REFERENCE
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ANNOTATED
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UniProt
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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 |