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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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ENDOGENOUS LIGAND
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SODIUM ION SITE
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REFERENCE
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ANNOTATED
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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
|
peptide | Agonist | pancreatic polypeptide, neuropeptide Y-(3-36), PYY-(3-36), neuropeptide Y, peptide YY | peptide | No | No | Tang T, Tan Q, Han S, Diemar A, Lobner K, Wang H, Schuss C, Behr V, Morl K, Wang M, Chu X, Yi C, Keller M, Kofoed J, Reedtz-Runge S, Kaiser A, Beck-Sickinger AG, Zhao Q, Wu B | 10.1126/SCIADV.ABM1232 | 2022-05-18 | Yes | |
5HT7R | 5-HT7 | 5-Hydroxytryptamine | A | Human | Cryo-EM | 7XTC | 7XTC_refined | 3.2 | R | Active | 100 | 57 | Gs | αs | - | 61 | BRIL | Nanobody-35 |
5-CT
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | No | No | Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE | 10.1016/J.MOLCEL.2022.05.031 | 2022-07-27 | Yes | |
SSR2 | SST2 | Somatostatin | A | Human | Cryo-EM | 7XAT | 7XAT_refined | 2.9 | A | Active | 100 | 78 | Gi/o | αi1 | - | 63 | - | scFv16 |
SOMATOSTATIN
|
protein | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | No | No | Bo Q, Yang F, Li Y, Meng X, Zhang H, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C | 10.1038/S41421-022-00405-2 | 2022-08-31 | Yes | |
AGRG2 | ADGRG2 | ADGRG | B2 | Mouse | Cryo-EM | 7XKE | - | 2.9 | R | Active | 100 | 25 | Gs | αs | Mini-Gs | 60 | - | Nanobody-35 |
PRASTERONE
|
small-molecule | Agonist | - | - | No | No | Lin H, Xiao P, Bu RQ, Guo S, Yang Z, Yuan D, Zhu ZL, Zhang CX, He QT, Zhang C, Ping YQ, Zhao RJ, Ma CS, Liu CH, Zhang XN, Jiang D, Huang S, Xi YT, Zhang DL, Xue CY, Yang BS, Li JY, Lin HC, Zeng XH, Zhao H, Xu WM, Yi F, Liu Z, Sun JP, Yu X | 10.1038/S41589-022-01084-6 | 2022-08-10 | Yes | |
V2R | V2 | Vasopressin and oxytocin | A | Human | Cryo-EM | 7R0C | - | 4.7 | A | Active | 100 | 76 | Beta | Beta-arrestin-1 | - | 84 | - | scFv30 |
vasopressin
|
peptide | Agonist | vasopressin, oxytocin | peptide | No | No | Bous J, Fouillen A, Orcel H, Trapani S, Cong X, Fontanel S, Saint-Paul J, Lai-Kee-Him J, Urbach S, Sibille N, Sounier R, Granier S, Mouillac B, Bron P | 10.1126/SCIADV.ABO7761 | 2022-09-14 | Yes | |
GP119 | GPR119 | GPR18, GPR55 and GPR119 | A | Human | Cryo-EM | 7WCN | 7WCN_refined | 2.9 | R | Active | 100 | 86 | Gs | αs | - | 60 | - | Nanobody-35 |
AR231453
|
small-molecule | Agonist | N-oleoylethanolamide, anandamide, N-palmitoylethanolamine, SEA | small-molecule | No | No | Qian Y, Wang J, Yang L, Liu Y, Wang L, Liu W, Lin Y, Yang H, Ma L, Ye S, Wu S, Qiao A | 10.1038/S41467-022-34696-6 | 2022-12-21 | Yes | |
SSR2 | SST2 | Somatostatin | A | Human | Cryo-EM | 7Y26 | 7Y26_refined | 3.3 | E | Active | 100 | 73 | Gq/11 | αq | Mini-Gq | 60 | - | scFv16 |
Octreotide
|
peptide | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | No | No | Chen S, Teng X, Zheng S | 10.1038/S41589-022-01130-3 | 2022-10-19 | Yes | |
ACM3 | M3 | Acetylcholine (muscarinic) | A | Human | Cryo-EM | 8EA0 | 8EA0_refined | 2.6 | A | Active | 99 | 48 | - | - | - | - | - | - |
iperoxo
|
small-molecule | Agonist | acetylcholine | small-molecule | No | No | Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL | 10.1038/S41586-022-05489-0 | 2022-11-30 | Yes | |
RL3R2 | RXFP4 | Relaxin family peptide | A | Human | Cryo-EM | 7YJ4 | - | 3.2 | R | Active | 100 | 76 | Gi/o | αi2 | - | 58 | - | scFv16 |
Insulin-like peptide INSL5 B chain
Insulin-like peptide INSL5 A chain |
peptide peptide |
Agonist | INSL5, relaxin-3 (B chain), relaxin-3 | peptide | No | No | Chen Y, Zhou Q, Wang J, Xu Y, Wang Y, Yan J, Wang Y, Zhu Q, Zhao F, Li C, Chen CW, Cai X, Bathgate RAD, Shen C, Eric Xu H, Yang D, Liu H, Wang MW | 10.1038/S41467-023-36182-Z | 2023-03-01 | Yes | |
GPR21 | GPR21 | A orphans | A | Human | Cryo-EM | 8HIX | - | 3.1 | R | Active | 100 | 81 | Gs | αs | Mini-Gs | 61 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | 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 | |
ACM2 | M2 | Acetylcholine (muscarinic) | A | Human | Cryo-EM | 7T8X | 7T8X_refined | 3.2 | A | Active | 100 | 59 | Gi/o | αo | - | 62 | - | Antibody fragment |
acetylcholine
|
small-molecule | Agonist | acetylcholine | small-molecule | No | No | - | - | 2023-01-25 | Yes | |
OPRK | κ | Opioid | A | Human | Cryo-EM | 8DZP | - | 2.7 | A | Active | 100 | 74 | Gi/o | αi1 | - | 60 | - | scFv16 |
SALVINORIN B METHOXYMETHYL ETHER
|
small-molecule | Agonist | [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 | |
SSR2 | SST2 | Somatostatin | A | Human | Cryo-EM | 7YAC | 7YAC_refined | 3.2 | E | Active | 100 | 76 | Gi/o | αi1 | - | 64 | - | scFv16 |
PALTUSOTINE
|
small-molecule | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | No | No | Zhao J, Fu H, Yu J, Hong W, Tian X, Qi J, Sun S, Zhao C, Wu C, Xu Z, Cheng L, Chai R, Yan W, Wei X, Shao Z | 10.1038/S41467-023-36673-Z | 2023-04-19 | Yes | |
AGRE5 | ADGRE5 | ADGRE | B2 | Human | Cryo-EM | 7YDJ | - | 3.0 | R | Active | 100 | 33 | G12/13 | α12 | Mini-G12 | 55 | - | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | - | - | 2023-07-12 | Yes | |
PF2R | FP | Prostanoid | A | Human | Cryo-EM | 8IUK | - | 2.7 | R | Active | 100 | 82 | Gq/11 | αq | - | 60 | - | scFv16 Nanobody-35 |
PGF2α
|
small-molecule | Agonist | thromboxane A2, PGF2α, PGI2, PGD2, 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 | |
5HT6R | 5-HT6 | 5-Hydroxytryptamine | A | Human | Cryo-EM | 8JLZ | - | 3.1 | R | Active | 100 | 61 | Gs | αs | - | 58 | - | Nanobody-35 |
CHEMBL365751
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | No | No | Pei Y, Wen X, Guo SC, Yang ZS, Zhang R, Xiao P, Sun JP | 10.1016/J.BBRC.2023.05.126 | 2023-06-28 | Yes | |
ADA1A | α1A | Adrenoceptors | A | Human | Cryo-EM | 8THK | - | 2.6 | R | Active | 100 | 52 | Gq/11 | αq | - | 57 | T4-Lysozyme | scFv16 |
CHEMBL133451
|
small-molecule | Agonist | (-)-adrenaline, (-)-noradrenaline | small-molecule | No | No | Su M, Wang J, Xiang G, Do HN, Levitz J, Miao Y, Huang XY | 10.1038/S41467-023-40524-2 | 2023-08-16 | Yes | |
CRFR1 | CRF1 | Corticotropin-releasing factor | B1 | Human | X-ray | 8GTI | - | 2.2 | A | Inactive | 16 | 63 | - | - | - | - | Endolysin | - |
8-(4-bromo-2,6-dimethoxyphenyl)-N-butyl-N-(cyclopropylmethyl)-2,7-dimethylpyrazolo[1,5-a][1,3,5]triazin-4-amine
|
small-molecule | Antagonist | urocortin 1, corticotrophin-releasing hormone, 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, C5a, C5a des-Arg, 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 | |
TAAR1 | TA1 | Trace amine | A | Human | Cryo-EM | 8JLO | - | 3.5 | R | Active | 100 | 84 | Gs | αs | - | 61 | - | - |
ulotaront
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, 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 | |
GRM5 | mGlu5 | Metabotropic glutamate | C | Human | Cryo-EM | 8T6J | - | 3.5 | A | Inactive | - | 63 | - | - | - | - | - | - |
CDPPB
|
small-molecule | Agonist | L-glutamic acid | small-molecule | No | No | Kumar KK, Wang H, Habrian C, Latorraca NR, Xu J, O'Brien ES, Zhang C, Montabana E, Koehl A, Marqusee S, Isacoff EY, Kobilka BK | 10.1101/2023.08.29.555158 | 2023-10-11 | Yes | |
OPRK | κ | Opioid | A | Human | X-ray | 4DJH | 4DJH_refined | 2.9 | A | Inactive | 6 | 76 | - | - | - | - | T4-Lysozyme | - |
JDTic
|
small-molecule | Antagonist | [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 | Wu H, Wacker D, Mileni M, Katritch V, Han GW, Vardy E, Liu W, Thompson AA, Huang XP, Carroll FI, Mascarella SW, Westkaemper RB, Mosier PD, Roth BL, Cherezov V, Stevens RC | 10.1038/NATURE10939 | 2012-03-21 | Yes | |
OPRD | δ | Opioid | A | Human | X-ray | 4RWA | 4RWA_refined | 3.3 | A | Inactive | 6 | 77 | - | - | - | - | 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 | No | Fenalti G, Zatsepin NA, Betti C, Giguere P, Han GW, Ishchenko A, Liu W, Guillemyn K, Zhang H, James D, Wang D, Weierstall U, Spence JC, Boutet S, Messerschmidt M, Williams GJ, Gati C, Yefanov OM, White TA, Oberthuer D, Metz M, Yoon CH, Barty A, Chapman HN, Basu S, Coe J, Conrad CE, Fromme R, Fromme P, Tourwe D, Schiller PW, Roth BL, Ballet S, Katritch V, Stevens RC, Cherezov V | 10.1038/NSMB.2965 | 2015-01-14 | Yes | |
GLR | glucagon | Glucagon | B1 | Human | X-ray | 5EE7 | 5EE7_refined | 2.5 | A | Inactive | 0 | 54 | - | - | - | - | T4-Lysozyme | - |
Octaethylene glycol monoethyl ether
MK-0893 |
small-molecule small-molecule |
Antagonist NAM |
glucagon | peptide | No | No | Jazayeri A, Dore AS, Lamb D, Krishnamurthy H, Southall SM, Baig AH, Bortolato A, Koglin M, Robertson NJ, Errey JC, Andrews SP, Teobald I, Brown AJ, Cooke RM, Weir M, Marshall FH | 10.1038/NATURE17414 | 2016-04-20 | Yes | |
SMO | SMO | Frizzled | F | Human | X-ray | 5V57 | 5V57_refined | 3.0 | A | Inactive | 1 | 62 | - | - | - | - | Flavodoxin | - |
N-methyl-N-[1-[4-(2-methylpyrazol-3-yl)phthalazin-1-yl]piperidin-4-yl]-4-nitro-2-(trifluoromethyl)benzamide
|
small-molecule | Antagonist | - | - | No | No | Zhang X, Zhao F, Wu Y, Yang J, Han GW, Zhao S, Ishchenko A, Ye L, Lin X, Ding K, Dharmarajan V, Griffin PR, Gati C, Nelson G, Hunter MS, Hanson MA, Cherezov V, Stevens RC, Tan W, Tao H, Xu F | 10.1038/NCOMMS15383 | 2017-05-24 | Yes | |
5HT2C | 5-HT2C | 5-Hydroxytryptamine | A | Human | X-ray | 6BQG | 6BQG_refined | 3.0 | A | Active | 80 | 62 | - | - | - | - | BRIL | - |
ergotamine
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | No | No | Peng Y, McCorvy JD, Harpsoe K, Lansu K, Yuan S, Popov P, Qu L, Pu M, Che T, Nikolajsen LF, Huang XP, Wu Y, Shen L, Bjorn-Yoshimoto WE, Ding K, Wacker D, Han GW, Cheng J, Katritch V, Jensen AA, Hanson MA, Zhao S, Gloriam DE, Roth BL, Stevens RC, Liu ZJ | 10.1016/j.cell.2018.01.001 | 2018-02-14 | Yes | |
PTAFR | PAF | Platelet-activating factor | A | Human | X-ray | 5ZKP | 5ZKP_refined | 2.8 | A | Other | - | 85 | - | - | - | - | Flavodoxin | - |
foropafant
|
small-molecule | Antagonist | PAF | small-molecule | No | No | Cao C, Tan Q, Xu C, He L, Yang L, Zhou Y, Zhou Y, Qiao A, Lu M, Yi C, Han GW, Wang X, Li X, Yang H, Rao Z, Jiang H, Zhao Y, Liu J, Stevens RC, Zhao Q, Zhang XC, Wu B | 10.1038/S41594-018-0068-Y | 2018-06-20 | Yes | |
ACM2 | M2 | Acetylcholine (muscarinic) | A | Human | X-ray | 5ZKC | 5ZKC_refined | 2.3 | A | Inactive | 2 | 60 | - | - | - | - | BRIL | - |
N-methyl scopolamine
|
small-molecule | Antagonist | acetylcholine | small-molecule | No | No | Suno R, Lee S, Maeda S, Yasuda S, Yamashita K, Hirata K, Horita S, Tawaramoto MS, Tsujimoto H, Murata T, Kinoshita M, Yamamoto M, Kobilka BK, Vaidehi N, Iwata S, Kobayashi T | 10.1038/S41589-018-0152-Y | 2018-11-21 | Yes | |
NK1R | NK1 | Tachykinin | A | Human | X-ray | 6J20 | 6J20_refined | 2.7 | A | Inactive | 0 | 71 | - | - | - | - | T4-Lysozyme | - |
aprepitant
|
small-molecule | Antagonist | neuropeptide-γ, neurokinin A, neuropeptide K, neurokinin B, hemokinin 1, substance P | peptide | No | No | Chen S, Lu M, Liu D, Yang L, Yi C, Ma L, Zhang H, Liu Q, Frimurer TM, Wang MW, Schwartz TW, Stevens RC, Wu B, Wuthrich K, Zhao Q | 10.1038/S41467-019-08568-5 | 2019-03-06 | Yes | |
NTR1 | NTS1 | Neurotensin | A | Human | Cryo-EM | 6OS9 | 6OS9_refined | 3.0 | R | Active | 100 | 73 | Gi/o | αi1 | - | 62 | - | scFv16 |
JMV449
|
peptide | Agonist | large neurotensin, large neuromedin N, neurotensin, neuromedin N | peptide | No | No | Kato HE, Zhang Y, Hu H, Suomivuori CM, Kadji FMN, Aoki J, Krishna Kumar K, Fonseca R, Hilger D, Huang W, Latorraca NR, Inoue A, Dror RO, Kobilka BK, Skiniotis G | 10.1038/S41586-019-1337-6 | 2019-07-10 | Yes | |
OX1R | OX1 | Orexin | A | Human | X-ray | 6TOD | - | 2.1 | A | Inactive | 0 | 71 | - | - | - | - | - | - |
EMPA
|
small-molecule | Antagonist | orexin-A, orexin-B | peptide | No | No | Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA. | 10.1021/acs.jmedchem.9b01787 | 2020-01-01 | Yes | |
ACM4 | M4 | Acetylcholine (muscarinic) | A | Human | X-ray | 6KP6 | 6KP6_refined | 3.0 | A | Inactive | 2 | 59 | - | - | - | - | GlgA glycogen synthase | - |
Apo (no ligand)
|
none | Apo (no ligand) | acetylcholine | small-molecule | No | No | Wang J, Wu M, Wu L, Xu Y, Li F, Wu Y, Popov P, Wang L, Bai F, Zhao S, Liu ZJ, Hua T | 10.1107/S2052252520000597 | 2020-03-11 | Yes | |
CALRL | calcitonin-like | Calcitonin | B1 | Human | Cryo-EM | 6UVA | - | 2.3 | R | Active | 100 | 75 | Gs | αs | - | 48 | - | Nanobody-35 RAMP3 |
adrenomedullin 2/intermedin
|
peptide | Agonist | - | - | No | No | Liang YL, Belousoff MJ, Fletcher MM, Zhang X, Khoshouei M, Deganutti G, Koole C, Furness SGB, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Danev R, Wootten D, Sexton PM | 10.1021/ACSPTSCI.9B00080 | 2020-04-01 | Yes | |
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 | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 7LCJ | 7LCJ_refined | 2.8 | R | Active | 99 | 84 | - | - | - | - | - | - |
danuglipron
|
small-molecule | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | No | No | Zhang X, Johnson RM, Drulyte I, Yu L, Kotecha A, Danev R, Wootten D, Sexton PM, Belousoff MJ | 10.1016/J.STR.2021.04.008 | 2021-01-20 | Yes | |
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 | |
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 | 7MTB | 7MTB_refined | 4.0 | R | Active | 97 | 93 | - | - | - | - | - | Fab light chain Fab heavy 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 | 7EZK | - | 3.1 | D | Active | 100 | 69 | Gs | αs | - | 58 | - | - |
CCK-8
|
peptide | Agonist | desulfated cholecystokinin-8, CCK-58, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8 | peptide | No | No | Liu Q, Yang D, Zhuang Y, Croll TI, Cai X, Dai A, He X, Duan J, Yin W, Ye C, Zhou F, Wu B, Zhao Q, Xu HE, Wang MW, Jiang Y | 10.1038/S41589-021-00841-3 | 2021-08-25 | Yes | |
CCKAR | CCK1 | Cholecystokinin | A | Human | X-ray | 7F8U | 7F8U_refined | 2.8 | A | Inactive | 0 | 65 | - | - | - | - | T4-Lysozyme | - |
lintitript
|
small-molecule | Antagonist | desulfated cholecystokinin-8, CCK-58, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8 | peptide | No | No | Zhang X, He C, Wang M, Zhou Q, Yang D, Zhu Y, Feng W, Zhang H, Dai A, Chu X, Wang J, Yang Z, Jiang Y, Sensfuss U, Tan Q, Han S, Reedtz-Runge S, Xu HE, Zhao S, Wang MW, Wu B, Zhao Q | 10.1038/S41589-021-00866-8 | 2021-10-13 | Yes | |
GP158 | GPR158 | C Orphans | C | Human | Cryo-EM | 7SHF | 7SHF_refined | 3.4 | B | Inactive | - | 23 | - | - | - | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Patil DN, Singh S, Laboute T, Strutzenberg TS, Qiu X, Wu D, Novick SJ, Robinson CV, Griffin PR, Hunt JF, Izard T, Singh AK, Martemyanov KA | 10.1126/SCIENCE.ABL4732 | 2021-12-01 | Yes | |
S1PR1 | S1P1 | Lysophospholipid (S1P) | A | Human | Cryo-EM | 7EO4 | 7EO4_refined | 2.9 | A | Active | 100 | 74 | Gi/o | αi1 | - | 43 | - | scFv16 |
siponimod
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | No | No | Xu Z, Ikuta T, Kawakami K, Kise R, Qian Y, Xia R, Sun MX, Zhang A, Guo C, Cai XH, Huang Z, Inoue A, He Y | 10.1038/S41589-021-00930-3 | 2022-01-05 | Yes | |
OXYR | OT | Vasopressin and oxytocin | A | Human | Cryo-EM | 7RYC | - | 2.9 | O | Active | 100 | 73 | Gq/11 | αq | Gamma subunit fused to alpha subunit | 55 | - | scFv16 |
oxytocin
|
peptide | Agonist | vasopressin, oxytocin | peptide | No | No | Meyerowitz JG, Robertson MJ, Barros-Alvarez X, Panova O, Nwokonko RM, Gao Y, Skiniotis G | 10.1038/S41594-022-00728-4 | 2022-03-09 | Yes | |
CALCR | CT | Calcitonin | B1 | Human | Cryo-EM | 7TYH | - | 3.3 | R | Active | 100 | 78 | Gs | αs | - | 58 | - | Nanobody-35 |
Calcitonin human
|
peptide | Agonist | adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP | peptide | No | No | - | - | 2022-03-23 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 7EZC | 7EZC_refined | 3.8 | B | Active | 72 | 70 | - | - | - | - | BRIL | - |
UK-432,097
|
small-molecule | Agonist | adenosine | small-molecule | No | No | Cui M, Zhou Q, Xu Y, Weng Y, Yao D, Zhao S, Song G | 10.1107/S2052252522001907 | 2022-04-13 | Yes | |
AGRG2 | ADGRG2 | ADGRG | B2 | Mouse | Cryo-EM | 7WUQ | - | 2.9 | R | Active | 100 | 28 | Gs | αs | - | 55 | - | Nanobody-35 | - | - | - | - | - | No | No | Xiao P, Guo S, Wen X, He QT, Lin H, Huang SM, Gou L, Zhang C, Yang Z, Zhong YN, Yang CC, Li Y, Gong Z, Tao XN, Yang ZS, Lu Y, Li SL, He JY, Wang C, Zhang L, Kong L, Sun JP, Yu X | 10.1038/S41586-022-04590-8 | 2022-04-27 | Yes | |
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, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, 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 | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 7X8S | 7X8S_refined | 3.1 | R | Active | 100 | 65 | Gs | αs | - | 60 | - | Nanobody-35 |
WB4-24
|
small-molecule | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | No | No | Cong Z, Zhou Q, Li Y, Chen LN, Zhang ZC, Liang A, Liu Q, Wu X, Dai A, Xia T, Wu W, Zhang Y, Yang D, Wang MW | 10.1073/PNAS.2200155119 | 2022-06-29 | Yes | |
MRGRD | MRGPRD | A orphans | A | Human | Cryo-EM | 7Y13 | - | 3.1 | R | Intermediate | 49 | 82 | - | - | - | - | BRIL | - |
Apo (no ligand)
|
none | Apo (no ligand) | β-alanine | small-molecule | No | No | Suzuki S, Iida M, Hiroaki Y, Tanaka K, Kawamoto A, Kato T, Oshima A | 10.1038/S42003-022-03668-3 | 2022-07-20 | Yes | |
SSR2 | SST2 | Somatostatin | A | Human | Cryo-EM | 7XMR | 7XMR_refined | 3.1 | R | Active | 100 | 77 | Gi/o | αi1 | - | 63 | - | - |
SOMATOSTATIN
|
protein | 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 | 7YP7 | - | 3.1 | R | Active | 100 | 24 | Gs | αs | - | 59 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | - | - | 2022-08-24 | Yes | |
5HT2B | 5-HT2B | 5-Hydroxytryptamine | A | Human | Cryo-EM | 7SRS | - | 3.3 | R | Active | 100 | 60 | Beta | Beta-arrestin-1 | - | 85 | - | Fab light chain Fab heavy chain Fab30 heavy chain Fab30 light chain |
Lysergide
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | No | No | Cao C, Barros-Alvarez X, Zhang S, Kim K, Damgen MA, Panova O, Suomivuori CM, Fay JF, Zhong X, Krumm BE, Gumpper RH, Seven AB, Robertson MJ, Krogan NJ, Huttenhain R, Nichols DE, Dror RO, Skiniotis G, Roth BL | 10.1016/J.NEURON.2022.08.006 | 2022-09-21 | Yes | |
ADA2A | α2A | Adrenoceptors | A | Human | Cryo-EM | 7W7E | - | 3.4 | R | Active | 100 | 56 | Gi/o | αo | - | 59 | - | scFv16 |
5-(3-Bicyclo[4.2.0]octa-1,3,5-trienyl)-1,2,3,6-tetrahydropyridine
|
small-molecule | Agonist | (-)-adrenaline, (-)-noradrenaline | small-molecule | No | No | Fink EA, Xu J, Hubner H, Braz JM, Seemann P, Avet C, Craik V, Weikert D, Schmidt MF, Webb CM, Tolmachova NA, Moroz YS, Huang XP, Kalyanaraman C, Gahbauer S, Chen G, Liu Z, Jacobson MP, Irwin JJ, Bouvier M, Du Y, Shoichet BK, Basbaum AI, Gmeiner P | 10.1126/SCIENCE.ABN7065 | 2022-09-28 | Yes | |
5HT5A | 5-HT5A | 5-Hydroxytryptamine | A | Human | Cryo-EM | 7X5H | 7X5H_refined | 3.1 | R | Active | 100 | 77 | Gi/o | αi1 | - | 63 | BRIL | scFv16 |
5-CT
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | No | No | Tan Y, Xu P, Huang S, Yang G, Zhou F, He X, Ma H, Xu HE, Jiang Y | 10.1038/S41421-022-00412-3 | 2022-09-14 | Yes | |
OPRM | μ | Opioid | A | Human | Cryo-EM | 8F7Q | - | 3.2 | R | Active | 100 | 72 | Gi/o | αi1 | - | 64 | - | scFv16 |
β-endorphin
|
peptide | 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 | 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 | |
GPR35 | GPR35 | A orphans | A | Human | Cryo-EM | 8H8J | 8H8J_refined | 3.2 | C | Active | 100 | 92 | G12/13 | α13 | - | 60 | - | scFv16 |
lodoxamide
|
small-molecule | Agonist | 1-Lyso-2-oleoyl-phosphatidic acid, 2-Oleoyllysophosphatydic acid, kynurenic acid, 2-oleoyl-LPA | small-molecule | No | No | Duan J, Liu Q, Yuan Q, Ji Y, Zhu S, Tan Y, He X, Xu Y, Shi J, Cheng X, Jiang H, Eric Xu H, Jiang Y | 10.1038/S41421-022-00499-8 | 2023-02-08 | Yes | |
GRPR | BB2 | Bombesin | A | Human | Cryo-EM | 7W40 | 7W40_refined | 3.0 | A | Active | 100 | 78 | Gq/11 | αq | - | 79 | - | scFv16 |
Bombesin
|
peptide | Agonist | neuromedin B, gastrin releasing peptide(14-27) (human), GRP-(18-27), gastrin-releasing peptide, neuromedin C | peptide | No | No | Peng S, Zhan Y, Zhang D, Ren L, Chen A, Chen ZF, Zhang H | 10.1073/PNAS.2216230120 | 2023-02-22 | Yes | |
ACM4 | M4 | Acetylcholine (muscarinic) | A | Human | Cryo-EM | 7TRQ | - | 2.5 | R | Active | 100 | 57 | Gi/o | αi1 | - | 64 | - | scFv16 |
iperoxo
VU0467154 |
small-molecule small-molecule |
Agonist PAM |
acetylcholine | small-molecule | No | No | - | - | 2023-05-17 | Yes | |
DRD3 | D3 | Dopamine | A | Human | Cryo-EM | 8IRT | - | 2.7 | R | Active | 100 | 68 | Gi/o | αi1 | - | 63 | BRIL | scFv16 |
rotigotine
|
small-molecule | Agonist | dopamine | small-molecule | No | No | Xu P, Huang S, Krumm BE, Zhuang Y, Mao C, Zhang Y, Wang Y, Huang XP, Liu YF, He X, Li H, Yin W, Jiang Y, Zhang Y, Roth BL, Xu HE | 10.1038/S41422-023-00808-0 | 2023-06-07 | Yes | |
GPR52 | GPR52 | A orphans | A | Human | Cryo-EM | 8HMP | - | 2.8 | R | Active | 100 | 79 | Gs | αs | - | 61 | - | Nanobody-35 |
derivative 17 [Nakahata et al., 2018]
|
small-molecule | Agonist | - | - | No | No | Fan Y, Lin X, Pan B, Chen B, Liu D, Wuthrich K, Xu F | 10.1002/MCO2.260 | 2023-06-21 | Yes | |
GRM2 | mGlu2 | Metabotropic glutamate | C | Human | Cryo-EM | 8JCZ | - | 3.0 | 2 | Inactive | - | 87 | - | - | - | - | - | - |
LY341495
|
small-molecule | Antagonist | L-glutamic acid | small-molecule | No | No | Wang X, Wang M, Xu T, Feng Y, Shao Q, Han S, Chu X, Xu Y, Lin S, Zhao Q, Wu B | 10.1038/S41422-023-00830-2 | 2023-06-21 | Yes | |
ACM4 | M4 | Acetylcholine (muscarinic) | A | Human | Cryo-EM | 8FX5 | - | 2.5 | R | Active | 100 | 57 | Gi/o | αi1 | - | 64 | - | scFv16 |
xanomeline
|
small-molecule | Agonist | acetylcholine | small-molecule | No | No | Burger WAC, Pham V, Vuckovic Z, Powers AS, Mobbs JI, Laloudakis Y, Glukhova A, Wootten D, Tobin AB, Sexton PM, Paul SM, Felder CC, Danev R, Dror RO, Christopoulos A, Valant C, Thal DM | 10.1038/S41467-023-41199-5 | 2023-09-13 | Yes | |
O52E4 | Olfactory 52E4 | Olfactory | A | Human | Cryo-EM | 8HTI | - | 3.0 | R | Active | 100 | 97 | Gs | αs | - | 40 | - | Nanobody-35 |
OCTANOIC ACID
|
small-molecule | Agonist | - | - | No | No | Choi C, Bae J, Kim S, Lee S, Kang H, Kim J, Bang I, Kim K, Huh WK, Seok C, Park H, Im W, Choi HJ | 10.1038/S41467-023-43983-9 | 2023-12-20 | Yes | |
O52E4 | Olfactory 52E4 | Olfactory | A | Human | Cryo-EM | 8J46 | - | 3.7 | A | Intermediate | 49 | 83 | - | - | - | - | BRIL | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Choi C, Bae J, Kim S, Lee S, Kang H, Kim J, Bang I, Kim K, Huh WK, Seok C, Park H, Im W, Choi HJ | 10.1038/S41467-023-43983-9 | 2023-12-20 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | Cryo-EM | 8JJO | - | 3.4 | F | Inactive | 0 | 65 | - | - | - | - | BRIL | - |
CHEMBL1160734
|
small-molecule | Antagonist | L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline | small-molecule | 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 | |
HCAR2 | HCA2 | Hydroxycarboxylic acid | A | Human | Cryo-EM | 8K5C | - | 3.1 | A | Active | 100 | 80 | - | - | - | - | - | - |
5-Methyl-4-oxidanyl-pyrazin-4-ium-2-carboxylic acid
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | No | No | Park JH, Kawakami K, Ishimoto N, Ikuta T, Ohki M, Ekimoto T, Ikeguchi M, Lee DS, Lee YH, Tame JRH, Inoue A, Park SY | 10.1038/S41467-023-42764-8 | 2023-11-22 | Yes | |
GP101 | GPR101 | A orphans | A | Human | Cryo-EM | 8W8Q | 8W8Q_refined | 2.9 | C | Active | 100 | 56 | Gs | αs | - | 59 | BRIL | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Yang Z, Wang JY, Yang F, Zhu KK, Wang GP, Guan Y, Ning SL, Lu Y, Li Y, Zhang C, Zheng Y, Zhou SH, Wang XW, Wang MW, Xiao P, Yi F, Zhang C, Zhang PJ, Xu F, Liu BH, Zhang H, Yu X, Gao N, Sun JP | 10.1038/S41589-023-01456-6 | 2024-01-03 | Yes | |
GHRHR | GHRH | Glucagon | B1 | Human | Cryo-EM | 7V9L | - | 2.6 | R | Active | 100 | 61 | Gs | αs | - | 60 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | GHRH | peptide | No | No | Cong Z, Zhou F, Zhang C, Zou X, Zhang H, Wang Y, Zhou Q, Cai X, Liu Q, Li J, Shao L, Mao C, Wang X, Wu J, Xia T, Zhao LH, Jiang H, Zhang Y, Xu HE, Cheng X, Yang D, Wang MW | 10.1073/PNAS.2106606118 | 2022-04-06 | Yes | |
OPRM | μ | Opioid | A | Mouse | X-ray | 4DKL | 4DKL_refined | 2.8 | A | Inactive | 6 | 71 | - | - | - | - | T4-Lysozyme | - |
Methyl 4-[[(4R,4aS,7R,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl]amino]-4-oxobutanoate
|
small-molecule | Antagonist | - | - | No | No | Manglik A, Kruse AC, Kobilka TS, Thian FS, Mathiesen JM, Sunahara RK, Pardo L, Weis WI, Kobilka BK, Granier S | 10.1038/NATURE10954 | 2012-03-21 | Yes | |
NTR1 | NTS1 | Neurotensin | A | Rat | X-ray | 3ZEV | 3ZEV_refined | 3.0 | A | Inactive | 3 | 72 | - | - | - | - | - | - |
neurotensin
|
peptide | Agonist | neurotensin, neuromedin N | peptide | No | No | Egloff P, Hillenbrand M, Klenk C, Batyuk A, Heine P, Balada S, Schlinkmann KM, Scott DJ, Schutz M, Pluckthun A | 10.1073/PNAS.1317903111 | 2014-01-29 | Yes | |
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 | 5K2A | 5K2A_refined | 2.5 | 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 | |
GLP1R | GLP-1 | Glucagon | B1 | Human | X-ray | 5VEW | 5VEW_refined | 2.7 | A | Inactive | 0 | 57 | - | - | - | - | T4-Lysozyme | - |
PF-06372222
|
small-molecule | NAM | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | No | No | Song G, Yang D, Wang Y, de Graaf C, Zhou Q, Jiang S, Liu K, Cai X, Dai A, Lin G, Liu D, Wu F, Wu Y, Zhao S, Ye L, Han GW, Lau J, Wu B, Hanson MA, Liu ZJ, Wang MW, Stevens RC | 10.1038/NATURE22378 | 2017-05-24 | Yes | |
C5AR1 | C5a1 | Complement peptide | A | Human | X-ray | 5O9H | 5O9H_refined | 2.7 | A | Inactive | 8 | 84 | - | - | - | - | - | - |
NDT9513727
|
small-molecule | Antagonist | ribosomal protein S19, C5a, C5a des-Arg, C3a | peptide | No | No | Robertson N, Rappas M, Dore AS, Brown J, Bottegoni G, Koglin M, Cansfield J, Jazayeri A, Cooke RM, Marshall FH | 10.1038/NATURE25025 | 2018-01-10 | Yes | |
Q98SW5 | SMO | Frizzled | F | African clawed frog | X-ray | 6D32 | 6D32_refined | 3.8 | A | Active | 78 | 58 | - | - | - | - | BRIL | - |
cyclopamine
|
small-molecule | Agonist (partial) | - | - | No | No | - | - | 2018-05-23 | Yes | |
ACM2 | M2 | Acetylcholine (muscarinic) | A | Human | X-ray | 5ZK3 | 5ZK3_refined | 2.6 | A | Inactive | 2 | 59 | - | - | - | - | BRIL | - |
CHEMBL558910
|
small-molecule | Antagonist | acetylcholine | small-molecule | No | No | 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 | |
CALCR | CT | Calcitonin | B1 | Human | Cryo-EM | 6NIY | - | 3.3 | R | Active | 100 | 55 | Gs | αs | - | 43 | - | - |
calcitonin (salmon synthetic)
|
small-molecule | Agonist | adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), adrenomedullin 2/intermedin, β-CGRP | peptide | No | No | Dal Maso E, Glukhova A, Zhu Y, Garcia-Nafria J, Tate CG, Atanasio S, Reynolds CA, Ramirez-Aportela E, Carazo JM, Hick CA, Furness SGB, Hay DL, Liang YL, Miller LJ, Christopoulos A, Wang MW, Wootten D, Sexton PM | 10.1021/ACSPTSCI.8B00056 | 2019-01-23 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 6PS0 | 6PS0_refined | 3.4 | A | Inactive | 0 | 68 | - | - | - | - | T4-Lysozyme | - |
carazolol
|
small-molecule | Antagonist | L-NOREPINEPHRINE, noradrenaline, (-)-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 | |
OPRD | δ | Opioid | A | Human | X-ray | 6PT2 | 6PT2_refined | 2.8 | A | Active | 72 | 78 | - | - | - | - | BRIL | - |
KGCHM07
|
peptide | Agonist | [Leu]enkephalin, β-endorphin, dynorphin A, [Met]enkephalin, endomorphin-1, α-neoendorphin, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13) | peptide | No | No | - | - | 2019-12-11 | Yes | |
GPR52 | GPR52 | A orphans | A | Human | X-ray | 6LI0 | - | 2.2 | A | Intermediate | 40 | 81 | - | - | - | - | Flavodoxin | - |
derivative 17 [Nakahata et al., 2018]
|
small-molecule | Agonist | - | - | No | No | Lin X, Li M, Wang N, Wu Y, Luo Z, Guo S, Han GW, Li S, Yue Y, Wei X, Xie X, Chen Y, Zhao S, Wu J, Lei M, Xu F | 10.1038/S41586-020-2019-0 | 2020-02-26 | Yes | |
ADA2B | α2B | Adrenoceptors | A | Human | Cryo-EM | 6K41 | - | 2.9 | R | Active | 100 | 54 | Gi/o | αo | - | 60 | T4-Lysozyme | scFv |
dexmedetomidine
|
small-molecule | Agonist | (-)-adrenaline, (-)-noradrenaline | small-molecule | No | No | Yuan D, Liu Z, Kaindl J, Maeda S, Zhao J, Sun X, Xu J, Gmeiner P, Wang HW, Kobilka BK | 10.1038/S41589-020-0492-2 | 2020-04-15 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 6S0L | 6S0L_refined | 2.7 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
ZM-241385
|
small-molecule | Antagonist | adenosine | small-molecule | No | No | Nass K, Cheng R, Vera L, Mozzanica A, Redford S, Ozerov D, Basu S, James D, Knopp G, Cirelli C, Martiel I, Casadei C, Weinert T, Nogly P, Skopintsev P, Usov I, Leonarski F, Geng T, Rappas M, Dore AS, Cooke R, Nasrollahi Shirazi S, Dworkowski F, Sharpe M, Olieric N, Bacellar C, Bohinc R, Steinmetz MO, Schertler G, Abela R, Patthey L, Schmitt B, Hennig M, Standfuss J, Wang M, Milne CJ | 10.1107/S2052252520011379 | 2020-07-15 | Yes | |
VIPR1 | VPAC1 | VIP and PACAP | B1 | Human | Cryo-EM | 6VN7 | 6VN7_refined | 3.2 | R | Active | 100 | 58 | Gs | αs | - | 61 | - | Nanobody-35 |
[Ac-His1]PACAP-27
|
peptide | Agonist | VIP, PHI, PHM, secretin, PACAP-27, GHRH, PACAP-38 | peptide | No | No | Duan J, Shen DD, Zhou XE, Bi P, Liu QF, Tan YX, Zhuang YW, Zhang HB, Xu PY, Huang SJ, Ma SS, He XH, Melcher K, Zhang Y, Xu HE, Jiang Y | 10.1038/S41467-020-17933-8 | 2020-09-02 | Yes | |
NTR1 | NTS1 | Neurotensin | A | Rat | Cryo-EM | 7L0P | - | 4.1 | C | Active | 100 | 73 | Gi/o | αi1 | - | 63 | - | - |
neurotensin
|
peptide | Agonist | neurotensin, neuromedin N | 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 | |
CALRL | calcitonin-like | Calcitonin | B1 | Human | Cryo-EM | 7KNU | 7KNU_refined | 3.5 | R | Inactive | 9 | 74 | - | - | - | - | - | RAMP1 |
Calcitonin gene-related peptide 1
|
peptide | Agonist | - | - | No | No | Josephs TM, Belousoff MJ, Liang YL, Piper SJ, Cao J, Garama DJ, Leach K, Gregory KJ, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM | 10.1126/SCIENCE.ABF7258 | 2021-02-24 | Yes | |
CCKAR | CCK1 | Cholecystokinin | A | Human | Cryo-EM | 7MBX | - | 2.0 | R | Active | 100 | 68 | Gs | αs | - | 61 | - | Nanobody-35 |
CHEMBL216166
|
protein | Agonist | desulfated cholecystokinin-8, CCK-58, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8 | peptide | No | No | Mobbs JI, Belousoff MJ, Harikumar KG, Piper SJ, Xu X, Furness SGB, Venugopal H, Christopoulos A, Danev R, Wootten D, Thal DM, Miller LJ, Sexton PM | 10.1371/JOURNAL.PBIO.3001295 | 2021-05-26 | Yes | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 7DUQ | - | 2.5 | R | Active | 100 | 83 | Gs | αs | - | 61 | - | Nanobody-35 |
N-Tert-butyl-6,7-dichloroquinoxalin-2-amine
CHEMBL410972 |
small-molecule protein |
Ago-PAM Agonist |
glucagon-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 | 2021-07-14 | Yes | |
S1PR3 | S1P3 | Lysophospholipid (S1P) | A | Human | Cryo-EM | 7EW4 | 7EW4_refined | 3.2 | R | Active | 100 | 76 | Gi/o | αi1 | - | 64 | - | scFv16 |
CYM-5541
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | No | No | Zhao C, Cheng L, Wang W, Wang H, Luo Y, Feng Y, Wang X, Fu H, Cai Y, Yang S, Fu P, Yan W, Shao Z | 10.1038/S41422-021-00567-W | 2021-09-29 | Yes | |
GP158 | GPR158 | C Orphans | C | Human | Cryo-EM | 7EWP | 7EWP_refined | 4.3 | A | Inactive | - | 47 | - | - | - | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Jeong E, Kim Y, Jeong J, Cho Y | 10.1038/S41467-021-27147-1 | 2021-12-01 | Yes | |
ADA1B | α1B | Adrenoceptors | A | Human | X-ray | 7B6W | - | 2.9 | A | Inactive | 1 | 51 | - | - | - | - | DARPin D12 | - |
(+)-cyclazosin
|
small-molecule | Inverse agonist | (-)-adrenaline, (-)-noradrenaline | small-molecule | No | No | Deluigi M, Morstein L, Schuster M, Klenk C, Merklinger L, Cridge RR, de Zhang LA, Klipp A, Vacca S, Vaid TM, Mittl PRE, Egloff P, Eberle SA, Zerbe O, Chalmers DK, Scott DJ, Pluckthun A | 10.1038/s41467-021-27911-3 | 2022-01-12 | Yes | |
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, neuropeptide Y, pancreatic polypeptide | peptide | No | No | Park C, Kim J, Ko SB, Choi YK, Jeong H, Woo H, Kang H, Bang I, Kim SA, Yoon TY, Seok C, Im W, Choi HJ | 10.1038/S41467-022-28510-6 | 2022-02-23 | Yes | |
GIPR | GIP | Glucagon | B1 | Human | Cryo-EM | 7VAB | 7VAB_refined | 3.2 | R | Active | 100 | 58 | Gs | αs | Mini-Gs | 60 | - | Nanobody-35 |
tirzepatide
|
peptide | Agonist | gastric inhibitory polypeptide | peptide | No | No | Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW | 10.1038/S41467-022-28683-0 | 2022-03-02 | Yes | |
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 | |
OPRD | δ | Opioid | A | Mouse | X-ray | 4EJ4 | 4EJ4_refined | 3.4 | A | Inactive | 6 | 76 | - | - | - | - | T4-Lysozyme | - |
naltrindole
|
small-molecule | Antagonist | [Leu]enkephalin, α-neoendorphin, [Met]enkephalin | peptide | No | No | Granier S, Manglik A, Kruse AC, Kobilka TS, Thian FS, Weis WI, Kobilka BK | 10.1038/NATURE11111 | 2012-05-16 | Yes | |
NTR1 | NTS1 | Neurotensin | A | Rat | X-ray | 4BUO | 4BUO_refined | 2.8 | A | Inactive | 3 | 72 | - | - | - | - | - | - |
neurotensin
|
peptide | Agonist | neurotensin, neuromedin N | peptide | No | No | - | - | 2014-01-29 | Yes | |
OPRX | NOP | Opioid | A | Human | X-ray | 5DHH | 5DHH_refined | 3.0 | A | Inactive | 6 | 76 | - | - | - | - | BRIL | - |
SB 612111
|
small-molecule | Antagonist | nociceptin/orphanin FQ | peptide | No | No | Miller RL, Thompson AA, Trapella C, Guerrini R, Malfacini D, Patel N, Han GW, Cherezov V, Calo G, Katritch V, Stevens RC | 10.1016/J.STR.2015.07.024 | 2015-10-21 | Yes | |
CNR1 | CB1 | Cannabinoid | A | Human | X-ray | 5TGZ | 5TGZ_refined | 2.8 | A | Inactive | 13 | 61 | - | - | - | - | Flavodoxin | - |
AM6538
|
small-molecule | Antagonist | 2-arachidonoylglycerol, anandamide | small-molecule | No | No | Hua T, Vemuri K, Pu M, Qu L, Han GW, Wu Y, Zhao S, Shui W, Li S, Korde A, Laprairie RB, Stahl EL, Ho JH, Zvonok N, Zhou H, Kufareva I, Wu B, Zhao Q, Hanson MA, Bohn LM, Makriyannis A, Stevens RC, Liu ZJ | 10.1016/J.CELL.2016.10.004 | 2016-11-02 | Yes | |
CNR1 | CB1 | Cannabinoid | A | Human | X-ray | 5XR8 | 5XR8_refined | 3.0 | A | Active | 96 | 60 | - | - | - | - | Flavodoxin | - |
AM841
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | No | No | Hua T, Vemuri K, Nikas SP, Laprairie RB, Wu Y, Qu L, Pu M, Korde A, Jiang S, Ho JH, Han GW, Ding K, Li X, Liu H, Hanson MA, Zhao S, Bohn LM, Makriyannis A, Stevens RC, Liu ZJ | 10.1038/NATURE23272 | 2017-07-12 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5OLG | 5OLG_refined | 1.9 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
ZM-241385
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | Rucktooa P, Cheng RKY, Segala E, Geng T, Errey JC, Brown GA, Cooke RM, Marshall FH, Dore AS | 10.1038/S41598-017-18570-W | 2018-01-17 | Yes | |
NPY1R | Y1 | Neuropeptide Y | A | Human | X-ray | 5ZBH | 5ZBH_refined | 3.0 | A | Inactive | 0 | 78 | - | - | - | - | T4-Lysozyme | - |
CHEMBL2046866
|
small-molecule | Antagonist | peptide YY, neuropeptide Y, pancreatic polypeptide | peptide | No | No | Yang Z, Han S, Keller M, Kaiser A, Bender BJ, Bosse M, Burkert K, Kogler LM, Wifling D, Bernhardt G, Plank N, Littmann T, Schmidt P, Yi C, Li B, Ye S, Zhang R, Xu B, Larhammar D, Stevens RC, Huster D, Meiler J, Zhao Q, Beck-Sickinger AG, Buschauer A, Wu B | 10.1038/S41586-018-0046-X | 2018-04-25 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 6MXT | 6MXT_refined | 3.0 | A | Active | 99 | 69 | - | - | - | - | T4-Lysozyme | Nanobody-71 |
salmeterol
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline | small-molecule | No | No | Masureel M, Zou Y, Picard LP, van der Westhuizen E, Mahoney JP, Rodrigues JPGLM, Mildorf TJ, Dror RO, Shaw DE, Bouvier M, Pardon E, Steyaert J, Sunahara RK, Weis WI, Zhang C, Kobilka BK | 10.1038/s41589-018-0145-x | 2018-11-14 | Yes | |
NK1R | NK1 | Tachykinin | A | Human | X-ray | 6J21 | 6J21_refined | 3.2 | A | Inactive | 0 | 71 | - | - | - | - | T4-Lysozyme | - |
aprepitant
|
small-molecule | Antagonist | neuropeptide-γ, neurokinin A, neuropeptide K, neurokinin B, hemokinin 1, substance P | peptide | No | No | - | - | 2019-03-06 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 6GT3 | 6GT3_refined | 2.0 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
imaradenant
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | - | - | 2019-06-26 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 6PS1 | 6PS1_refined | 3.2 | A | Inactive | 0 | 68 | - | - | - | - | T4-Lysozyme | - |
timolol
|
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 | |
OX1R | OX1 | Orexin | A | Human | X-ray | 6TP6 | 6TP6_refined | 2.3 | B | Inactive | 0 | 71 | - | - | - | - | - | - |
filorexant
|
small-molecule | Antagonist | orexin-A, orexin-B | peptide | No | No | Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA. | 10.1021/acs.jmedchem.9b01787 | 2020-01-01 | Yes | |
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 neurotensin, large neuromedin N, neurotensin, neuromedin N | peptide | No | No | Huang W, Masureel M, Qu Q, Janetzko J, Inoue A, Kato HE, Robertson MJ, Nguyen KC, Glenn JS, Skiniotis G, Kobilka BK | 10.1038/S41586-020-1953-1 | 2020-02-26 | Yes | |
MC4R | MC4 | Melanocortin | A | Human | X-ray | 6W25 | - | 2.8 | A | Intermediate | 44 | 79 | - | - | - | - | GlgA glycogen synthase | - |
SHU9119
Calcium |
peptide small-molecule |
Antagonist Cofactor |
β-MSH, α-MSH, agouti-related protein, γ-MSH, ACTH | peptide | No | No | Yu J, Gimenez LE, Hernandez CC, Wu Y, Wein AH, Han GW, McClary K, Mittal SR, Burdsall K, Stauch B, Wu L, Stevens SN, Peisley A, Williams SY, Chen V, Millhauser GL, Zhao S, Cone RD, Stevens RC | 10.1126/SCIENCE.AAZ8995 | 2020-04-29 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 6S0Q | 6S0Q_refined | 2.7 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
ZM-241385
|
small-molecule | Antagonist | adenosine | small-molecule | No | No | Nass K, Cheng R, Vera L, Mozzanica A, Redford S, Ozerov D, Basu S, James D, Knopp G, Cirelli C, Martiel I, Casadei C, Weinert T, Nogly P, Skopintsev P, Usov I, Leonarski F, Geng T, Rappas M, Dore AS, Cooke R, Nasrollahi Shirazi S, Dworkowski F, Sharpe M, Olieric N, Bacellar C, Bohinc R, Steinmetz MO, Schertler G, Abela R, Patthey L, Schmitt B, Hennig M, Standfuss J, Wang M, Milne CJ | 10.1107/S2052252520011379 | 2020-07-15 | Yes | |
ADRB1 | β1 | Adrenoceptors | A | Wild turkey | Cryo-EM | 7JJO | - | 2.6 | R | Active | 100 | 58 | Gs | αs | - | 51 | - | Nanobody-35 |
LEVISOPRENALINE
|
small-molecule | Agonist | - | - | No | No | Su M, Zhu L, Zhang Y, Paknejad N, Dey R, Huang J, Lee MY, Williams D, Jordan KD, Eng ET, Ernst OP, Meyerson JR, Hite RK, Walz T, Liu W, Huang XY | 10.1016/J.MOLCEL.2020.08.001 | 2020-09-02 | Yes | |
ADRB1 | β1 | Adrenoceptors | A | Human | X-ray | 7BVQ | 7BVQ_refined | 2.5 | A | Inactive | 0 | 60 | - | - | - | - | T4-Lysozyme | - |
Carazolol
|
small-molecule | Inverse 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 | |
NTR1 | NTS1 | Neurotensin | A | Rat | X-ray | 6ZA8 | 6ZA8_refined | 2.7 | A | Intermediate | 17 | 78 | - | - | - | - | DARPin D12 | - |
CHEMBL508044
|
small-molecule | Agonist (partial) | 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 | 7E2Z | - | 3.1 | R | Active | 100 | 66 | Gi/o | αi1 | - | 62 | - | - |
aripiprazole
|
small-molecule | Agonist (partial) | 5-hydroxytryptamine | small-molecule | No | No | Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen DD, Yen HY, Robinson CV, Harpsoe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE | 10.1038/S41586-021-03376-8 | 2021-04-14 | Yes | |
Q3KSP2 | BILF1 | Unclassified | A | strain GD1 | Cryo-EM | 7JHJ | - | 3.2 | R | Active | 100 | 89 | Gi/o | αi1 | - | 62 | - | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Tsutsumi N, Qu Q, Mavri M, Baggesen MS, Maeda S, Waghray D, Berg C, Kobilka BK, Rosenkilde MM, Skiniotis G, Garcia KC | 10.1016/J.IMMUNI.2021.06.001 | 2021-07-07 | Yes | |
MTR1A | MT1 | Melatonin | A | Human | Cryo-EM | 7DB6 | 7DB6_refined | 3.3 | D | Active | 100 | 79 | Gi/o | αi1 | - | 62 | - | scFv16 |
ramelteon
|
small-molecule | Agonist | melatonin | small-molecule | No | No | Okamoto HH, Miyauchi H, Inoue A, Raimondi F, Tsujimoto H, Kusakizako T, Shihoya W, Yamashita K, Suno R, Nomura N, Kobayashi T, Iwata S, Nishizawa T, Nureki O | 10.1038/S41594-021-00634-1 | 2021-08-18 | Yes | |
S1PR3 | S1P3 | Lysophospholipid (S1P) | A | Human | Cryo-EM | 7EW3 | - | 3.1 | R | Active | 100 | 77 | Gi/o | αi1 | - | 64 | - | scFv16 |
Sphingosine 1-phosphate
|
lipid | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | No | No | 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 | |
MRGX4 | MRGPRX4 | A orphans | A | Human | Cryo-EM | 7S8P | 7S8P_refined | 2.6 | R | Active | 100 | 77 | Gq/11 | αq | Gq-Gs chimera | 57 | BRIL | scFv16 |
N-[(1r,3R,5S,7R)-3,5-dimethyltricyclo[3.3.1.1~3,7~]decane-1-carbonyl]-D-phenylalanine
|
small-molecule | Agonist | - | - | No | No | Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL | 10.1038/S41586-021-04126-6 | 2021-11-17 | Yes | |
MRGX2 | MRGPRX2 | A orphans | A | Human | Cryo-EM | 7VV6 | 7VV6_refined | 3.3 | R | Active | 98 | 82 | - | - | - | - | - | - |
compound 48/80
|
small-molecule | Agonist | PAMP-20 | peptide | No | No | Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP | 10.1038/S41586-021-04077-Y | 2021-12-01 | Yes | |
5HT2A | 5-HT2A | 5-Hydroxytryptamine | A | Human | X-ray | 7WC6 | 7WC6_refined | 2.6 | A | Inactive | 1 | 58 | - | - | - | - | BRIL | - |
Lysergide
|
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 | 7F4D | - | 3.0 | R | Active | 100 | 83 | Gs | αs | - | 59 | - | Nanobody-35 |
INTERMEDINE
|
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 | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 7PYR | 7PYR_refined | 2.6 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
Preladenant conjugate PSB-2115
|
small-molecule | Antagonist | adenosine | small-molecule | No | No | Claff T, Klapschinski TA, Tiruttani Subhramanyam UK, Vaassen VJ, Schlegel JG, Vielmuth C, Voss JH, Labahn J, Muller CE | 10.1002/ANIE.202115545 | 2022-03-02 | Yes | |
GRM3 | mGlu3 | Metabotropic glutamate | C | Human | Cryo-EM | 7WI6 | 7WI6_refined | 3.7 | A | Inactive | - | 82 | - | - | - | - | - | - |
LY341495
|
small-molecule | Antagonist | NAAG, L-glutamic acid | small-molecule | No | No | Fang W, Yang F, Xu C, Ling S, Lin L, Zhou Y, Sun W, Wang X, Liu P, Rondard P, Shi P, Pin JP, Tian C, Liu J | 10.1038/S41422-022-00623-Z | 2022-03-16 | Yes | |
GALR1 | GAL1 | Galanin | A | Human | Cryo-EM | 7WQ3 | 7WQ3_refined | 2.7 | R | Active | 100 | 83 | Gi/o | αi1 | - | 64 | - | scFv16 |
galanin
|
peptide | Agonist | galanin-like peptide, galanin | peptide | No | No | - | - | 2022-04-20 | Yes | |
BKRB2 | B2 | Bradykinin | A | Human | Cryo-EM | 7F6I | 7F6I_refined | 2.8 | A | Active | 100 | 78 | Gq/11 | αq | - | 63 | - | - |
kallidin
|
peptide | Agonist | [des-Arg10]kallidin, Lys-[Hyp3]-bradykinin, kallidin, [des-Arg9]bradykinin, [Hyp3]bradykinin, T-kinin, bradykinin | peptide | No | No | Shen J, Zhang D, Fu Y, Chen A, Yang X, Zhang H | 10.1038/S41467-022-28399-1 | 2022-01-05 | Yes | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 7X8R | - | 2.6 | R | Active | 100 | 64 | Gs | αs | - | 59 | - | Nanobody-35 |
CHEMBL2158411
|
small-molecule | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | No | No | Cong Z, Zhou Q, Li Y, Chen LN, Zhang ZC, Liang A, Liu Q, Wu X, Dai A, Xia T, Wu W, Zhang Y, Yang D, Wang MW | 10.1073/PNAS.2200155119 | 2022-06-29 | Yes | |
ACKR3 | ACKR3 | Chemokine | A | Human | Cryo-EM | 7SK6 | 7SK6_refined | 4.0 | A | Active | 97 | 83 | - | - | - | - | - | CID24 Fab light chain CID24 Fab heavy chain |
Stromal cell-derived factor 1
|
peptide | Agonist | CXCL11, CXCL12α | peptide | No | No | Yen YC, Schafer CT, Gustavsson M, Eberle SA, Dominik PK, Deneka D, Zhang P, Schall TJ, Kossiakoff AA, Tesmer JJG, Handel TM | 10.1126/SCIADV.ABN8063 | 2022-07-27 | Yes | |
AGRL3 | ADGRL3 | ADGRL | B2 | Mouse | Cryo-EM | 7WY5 | - | 2.8 | R | Active | 100 | 17 | Gq/11 | αq | Mini-Gq | 59 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Qian Y, Ma Z, Liu C, Li X, Zhu X, Wang N, Xu Z, Xia R, Liang J, Duan Y, Yin H, Xiong Y, Zhang A, Guo C, Chen Z, Huang Z, He Y | 10.1016/J.MOLCEL.2022.10.009 | 2022-10-26 | Yes | |
LPAR1 | LPA1 | Lysophospholipid (LPA) | A | Human | Cryo-EM | 7YU3 | 7YU3_refined | 3.4 | R | Active | 100 | 80 | Gi/o | αi1 | - | 63 | - | scFv16 |
[(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate
|
small-molecule | Agonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | No | No | Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O | 10.1038/S41467-022-33121-2 | 2022-10-05 | Yes | |
OPRM | μ | Opioid | A | Human | Cryo-EM | 8EFQ | - | 3.3 | R | Active | 100 | 71 | Gi/o | αi1 | - | 61 | - | - |
DAMGO
|
peptide | 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 | |
5HT6R | 5-HT6 | 5-Hydroxytryptamine | A | Human | Cryo-EM | 7YS6 | 7YS6_refined | 3.0 | A | Active | 100 | 61 | Gs | αs | - | 59 | - | scFv16 |
5-hydroxytryptamine
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | No | No | - | - | 2023-03-29 | Yes | |
ACTHR | MC2 | Melanocortin | A | Human | Cryo-EM | 8GY7 | - | 3.3 | R | Active | 100 | 92 | Gs | αs | - | 59 | BRIL | - |
ACTH
|
peptide | Agonist | ACTH | peptide | No | No | Luo P, Feng W, Ma S, Dai A, Wu K, Chen X, Yuan Q, Cai X, Yang D, Wang MW, Eric Xu H, Jiang Y | 10.1038/S41422-022-00751-6 | 2023-01-11 | Yes | |
TAAR9 | TAAR9 | A orphans | A | Mouse | Cryo-EM | 8IWE | - | 3.4 | R | Active | 98 | 85 | - | - | - | - | - | - |
SPERMIDINE
|
small-molecule | Agonist | - | - | No | No | Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP | 10.1038/S41586-023-06106-4 | 2023-05-31 | Yes | |
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 | myristic acid, oleic acid, α-linolenic 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 | |
CML1 | chemerin | Chemerin receptor | A | Human | Cryo-EM | 7YKD | - | 2.8 | A | Active | 100 | 76 | Gi/o | αi1 | - | 61 | - | scFv16 |
chemerin C-terminal peptide
|
peptide | Agonist | 18R-HEPE, chemerin C-terminal peptide, EPA, resolvin E1, chemerin | peptide | No | No | Wang J, Chen G, Liao Q, Lyu W, Liu A, Zhu L, Du Y, Ye RD | 10.1073/PNAS.2214324120 | 2023-04-19 | Yes | |
EDNRB | ETB | Endothelin | A | Human | Cryo-EM | 8IY6 | - | 3.1 | R | Active | 82 | 66 | - | - | - | - | - | - |
ENDOTHELIN
|
protein | Agonist | endothelin-1, endothelin-2, endothelin-3 | peptide | No | No | Sano FK, Akasaka H, Shihoya W, Nureki O | 10.7554/ELIFE.85821 | 2023-08-16 | Yes | |
NTR1 | NTS1 | Neurotensin | A | Human | Cryo-EM | 8JPF | - | 3.0 | R | Active | 82 | 71 | - | - | - | - | - | - |
JMV431
CHEMBL4576388 |
peptide small-molecule |
Agonist PAM |
large neurotensin, large neuromedin N, neurotensin, neuromedin N | peptide | No | No | Duan J, Liu H, Zhao F, Yuan Q, Ji Y, Cai X, He X, Li X, Li J, Wu K, Gao T, Zhu S, Lin S, Wang MW, Cheng X, Yin W, Jiang Y, Yang D, Xu HE | 10.1038/S41586-023-06395-9 | 2023-08-09 | Yes | |
HRH4 | H4 | Histamine | A | Human | Cryo-EM | 7YFD | - | 3.1 | R | Active | 100 | 67 | Gq/11 | αq | - | 62 | - | scFv16 Nanobody-35 |
imetit
|
small-molecule | Agonist | histamine, CCL16 | small-molecule | No | No | Im D, Kishikawa JI, Shiimura Y, Hisano H, Ito A, Fujita-Fujiharu Y, Sugita Y, Noda T, Kato T, Asada H, Iwata S | 10.1038/S41467-023-42260-Z | 2023-10-25 | Yes | |
CXCR3 | CXCR3 | Chemokine | A | Human | Cryo-EM | 8HNK | - | 3.0 | R | Active | 100 | 81 | Gi/o | αi1 | - | 62 | - | scFv16 |
CXCL11
|
peptide | Agonist | 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 | |
GLR | glucagon | Glucagon | B1 | Human | Cryo-EM | 8JIQ | 8JIQ_refined | 3.4 | R | Active | 100 | 79 | Gs | αs | - | 56 | - | Nanobody-35 |
Dual-agonist peptide P15
|
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 | 2023-09-13 | Yes | |
GRM5 | mGlu5 | Metabotropic glutamate | C | Human | Cryo-EM | 8T8M | - | 3.0 | A | Intermediate | - | 62 | - | - | - | - | - | Nanobody-43 |
quisqualate
|
small-molecule | Agonist | L-glutamic acid | small-molecule | No | No | Kumar KK, Wang H, Habrian C, Latorraca NR, Xu J, O'Brien ES, Zhang C, Montabana E, Koehl A, Marqusee S, Isacoff EY, Kobilka BK | 10.1101/2023.08.29.555158 | 2023-10-11 | Yes | |
OPRX | NOP | Opioid | A | Human | X-ray | 4EA3 | 4EA3_refined | 3.0 | A | Inactive | 6 | 75 | - | - | - | - | BRIL | - |
compound 24 [PMID: 16451050]
|
small-molecule | Antagonist | nociceptin/orphanin FQ | peptide | No | No | Thompson AA, Liu W, Chun E, Katritch V, Wu H, Vardy E, Huang XP, Trapella C, Guerrini R, Calo G, Roth BL, Cherezov V, Stevens RC | 10.1038/NATURE11085 | 2012-04-25 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 4QKX | 4QKX_refined | 3.3 | A | Active | 99 | 69 | - | - | - | - | T4-Lysozyme | Nanobody |
Q27453560
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline | small-molecule | No | No | Weichert D, Kruse AC, Manglik A, Hiller C, Zhang C, Hubner H, Kobilka BK, Gmeiner P | 10.1073/PNAS.1410415111 | 2014-07-23 | Yes | |
ACM1 | M1 | Acetylcholine (muscarinic) | A | Human | X-ray | 5CXV | 5CXV_refined | 2.7 | A | Inactive | 2 | 62 | - | - | - | - | T4-Lysozyme | - |
0HK
|
small-molecule | Antagonist | acetylcholine | small-molecule | No | No | Thal DM, Sun B, Feng D, Nawaratne V, Leach K, Felder CC, Bures MG, Evans DA, Weis WI, Bachhawat P, Kobilka TS, Sexton PM, Kobilka BK, Christopoulos A | 10.1038/NATURE17188 | 2016-03-09 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5UIG | 5UIG_refined | 3.5 | A | Inactive | 21 | 70 | - | - | - | - | BRIL | - |
5-Amino-N-[(2-Methoxyphenyl)methyl]-2-(3-Methylphenyl)-2h-1,2,3-Triazole-4-Carboximidamide
|
small-molecule | Antagonist | adenosine | small-molecule | No | No | Sun B, Bachhawat P, Chu ML, Wood M, Ceska T, Sands ZA, Mercier J, Lebon F, Kobilka TS, Kobilka BK | 10.1073/PNAS.1621423114 | 2017-02-08 | Yes | |
CCR5 | CCR5 | Chemokine | A | Human | X-ray | 5UIW | - | 2.2 | A | Inactive | 19 | 85 | - | - | - | - | Rubredoxin | - |
5P7-CCL5
|
protein | Antagonist | CCL14, CCL8, CCL13, CCL4, CCL7, CCL2, CCL5, CCL11, CCL3, CCL16 | peptide | No | No | Zheng Y, Han GW, Abagyan R, Wu B, Stevens RC, Cherezov V, Kufareva I, Handel TM | 10.1016/J.IMMUNI.2017.05.002 | 2017-06-28 | Yes | |
OPRM | μ | Opioid | A | Mouse | Cryo-EM | 6DDF | - | 3.5 | R | Active | 100 | 71 | Gi/o | αi1 | - | 61 | - | - |
DAMGO
|
peptide | Agonist | - | - | No | No | Koehl A, Hu H, Maeda S, Zhang Y, Qu Q, Paggi JM, Latorraca NR, Hilger D, Dawson R, Matile H, Schertler GFX, Granier S, Weis WI, Dror RO, Manglik A, Skiniotis G, Kobilka BK | 10.1038/S41586-018-0219-7 | 2018-06-13 | Yes | |
ADRB1 | β1 | Adrenoceptors | A | Wild turkey | X-ray | 6IBL | 6IBL_refined | 2.7 | A | Active | 99 | 60 | - | - | - | - | Thioredoxin 1 | Camelid antibody fragment Nb80 |
ARFORMOTEROL
|
small-molecule | Agonist | - | - | No | No | Lee Y, Warne T, Nehme R, Pandey S, Dwivedi-Agnihotri H, Chaturvedi M, Edwards PC, Garcia-Nafria J, Leslie AGW, Shukla AK, Tate CG | 10.1038/S41586-020-2419-1 | 2019-01-09 | Yes | |
SMO | SMO | Frizzled | F | Human | Cryo-EM | 6OT0 | - | 3.9 | R | Active | 100 | 46 | Gi/o | αi1 | - | 100 | - | Fab light chain Fab heavy chain |
24,25-Epoxy-cholesterol
|
small-molecule | Agonist | - | - | No | No | Qi X, Liu H, Thompson B, McDonald J, Zhang C, Li X | 10.1038/S41586-019-1286-0 | 2019-06-12 | Yes | |
CLTR2 | CysLT2 | Leukotriene | A | Human | X-ray | 6RZ6 | - | 2.4 | A | Active | 59 | 82 | - | - | - | - | BRIL | - |
ONO-2570366
|
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 | |
CRFR1 | CRF1 | Corticotropin-releasing factor | B1 | Human | Cryo-EM | 6PB0 | - | 3.0 | R | Active | 100 | 68 | Gs | αs | Gs-Gi1 chimera | 58 | - | Nanobody-35 |
Urocortin
|
peptide | Agonist | urocortin 1, corticotrophin-releasing hormone, urocortin 2 | peptide | No | No | Ma S, Shen Q, Zhao LH, Mao C, Zhou XE, Shen DD, de Waal PW, Bi P, Li C, Jiang Y, Wang MW, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE | 10.1016/J.MOLCEL.2020.01.013 | 2020-02-12 | Yes | |
5HT1B | 5-HT1B | 5-Hydroxytryptamine | A | Human | X-ray | 7C61 | 7C61_refined | 3.0 | A | Inactive | 17 | 68 | - | - | - | - | BRIL | IgG heavy chain IgG light chain |
ergotamine
|
small-molecule | Antagonist | tryptamine, 5-hydroxytryptamine, 5-HT-moduline | small-molecule | 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 | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 6X1A | - | 2.5 | R | Active | 100 | 84 | Gs | αs | - | 89 | - | Nanobody-35 |
danuglipron
|
small-molecule | Agonist | glucagon-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 | |
GLP2R | GLP-2 | Glucagon | B1 | Human | Cryo-EM | 7D68 | - | 3.0 | R | Active | 100 | 53 | Gs | αs | - | 57 | - | Nanobody-35 |
glucagon
|
peptide | Agonist | glucagon-like peptide 2-(3-33), glucagon-like peptide 2 | peptide | No | No | Sun W, Chen LN, Zhou Q, Zhao LH, Yang D, Zhang H, Cong Z, Shen DD, Zhao F, Zhou F, Cai X, Chen Y, Zhou Y, Gadgaard S, van der Velden WJC, Zhao S, Jiang Y, Rosenkilde MM, Xu HE, Zhang Y, Wang MW | 10.1038/S41422-020-00442-0 | 2020-12-16 | Yes | |
CASR | CaS | Calcium-sensing | C | Human | Cryo-EM | 7DTW | 7DTW_refined | 4.5 | A | Inactive | - | 72 | - | - | - | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | 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 | |
GRM2 | mGlu2 | Metabotropic glutamate | C | Human | Cryo-EM | 7MTQ | - | 3.7 | B | Inactive | - | 85 | - | - | - | - | - | - |
LY341495
|
small-molecule | Antagonist | L-glutamic acid | small-molecule | No | No | Seven AB, Barros-Alvarez X, de Lapeyriere M, Papasergi-Scott MM, Robertson MJ, Zhang C, Nwokonko RM, Gao Y, Meyerowitz JG, Rocher JP, Schelshorn D, Kobilka BK, Mathiesen JM, Skiniotis G | 10.1038/S41586-021-03680-3 | 2021-07-07 | Yes | |
GRM5 | mGlu5 | Metabotropic glutamate | C | Human | Cryo-EM | 7FD8 | 7FD8_refined | 3.8 | A | Active | - | 63 | - | - | - | - | - | - |
quisqualate
|
small-molecule | Agonist | L-glutamic acid | small-molecule | No | No | Nasrallah C, Cannone G, Briot J, Rottier K, Berizzi AE, Huang CY, Quast RB, Hoh F, Baneres JL, Malhaire F, Berto L, Dumazer A, Font-Ingles J, Gomez-Santacana X, Catena J, Kniazeff J, Goudet C, Llebaria A, Pin JP, Vinothkumar KR, Lebon G | 10.1016/J.CELREP.2021.109648 | 2021-09-08 | Yes | |
GASR | CCK2 | Cholecystokinin | A | Human | Cryo-EM | 7F8V | - | 3.3 | R | Active | 100 | 62 | Gi/o | αi2 | - | 61 | - | - |
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 | Zhang X, He C, Wang M, Zhou Q, Yang D, Zhu Y, Feng W, Zhang H, Dai A, Chu X, Wang J, Yang Z, Jiang Y, Sensfuss U, Tan Q, Han S, Reedtz-Runge S, Xu HE, Zhao S, Wang MW, Wu B, Zhao Q | 10.1038/S41589-021-00866-8 | 2021-10-13 | Yes | |
MRGX2 | MRGPRX2 | A orphans | A | Human | Cryo-EM | 7VUZ | 7VUZ_refined | 2.9 | R | Active | 100 | 76 | Gi/o | αi1 | - | 62 | - | scFv16 |
PAMP-12
|
peptide | Agonist | PAMP-20 | peptide | No | No | Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP | 10.1038/S41586-021-04077-Y | 2021-12-01 | Yes | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 7LLY | 7LLY_refined | 3.3 | R | Active | 100 | 77 | Gs | αs | - | 50 | - | Nanobody-35 |
Pro-glucagon
|
peptide | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | No | No | Deganutti G, Liang YL, Zhang X, Khoshouei M, Clydesdale L, Belousoff MJ, Venugopal H, Truong TT, Glukhova A, Keller AN, Gregory KJ, Leach K, Christopoulos A, Danev R, Reynolds CA, Zhao P, Sexton PM, Wootten D | 10.1038/S41467-021-27760-0 | 2022-01-12 | Yes | |
LPAR1 | LPA1 | Lysophospholipid (LPA) | A | Human | Cryo-EM | 7TD0 | - | 2.8 | R | Active | 100 | 80 | Gi/o | αi1 | - | 62 | - | - |
lysophosphatidic acid
|
small-molecule | Agonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | No | No | Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY | 10.1038/S41467-022-28417-2 | 2022-02-09 | Yes | |
FPR2 | FPR2/ALX | Formylpeptide | A | Human | Cryo-EM | 7WVV | 7WVV_refined | 2.9 | R | Active | 100 | 85 | Gi/o | αi2 | - | 63 | BRIL | - |
synthetic peptide
|
peptide | Agonist | 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 | Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B | 10.1038/S41467-022-29361-X | 2022-04-13 | Yes | |
AGRF1 | ADGRF1 | ADGRF | B2 | Human | Cryo-EM | 7WU5 | - | 3.0 | R | Active | 100 | 31 | Gi/o | αi1 | Mini-Gi1 | 58 | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Qu X, Qiu N, Wang M, Zhang B, Du J, Zhong Z, Xu W, Chu X, Ma L, Yi C, Han S, Shui W, Zhao Q, Wu B | 10.1038/S41586-022-04580-W | 2022-04-27 | Yes | |
ADRB3 | β3 | Adrenoceptors | A | Dog | Cryo-EM | 7XJH | - | 3.3 | R | Active | 100 | 68 | Gs | αs | - | 59 | - | Nanobody-35 |
LEVISOPRENALINE
|
small-molecule | Agonist | - | - | No | No | Nagiri C, Kobayashi K, Tomita A, Kato M, Kobayashi K, Yamashita K, Nishizawa T, Inoue A, Shihoya W, Nureki O | 10.1016/J.MOLCEL.2021.06.024 | 2022-05-04 | Yes | |
DRD1 | D1 | Dopamine | A | Human | Cryo-EM | 7X2F | 7X2F_refined | 3.0 | F | Active | 100 | 63 | Gs | αs | - | 58 | - | Nanobody-35 |
dopamine
mevidalen |
small-molecule small-molecule |
Agonist PAM |
L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | No | No | Teng X, Chen S, Nie Y, Xiao P, Yu X, Shao Z, Zheng S | 10.1038/S41467-022-30929-W | 2022-06-15 | Yes | |
GASR | CCK2 | Cholecystokinin | A | Human | Cryo-EM | 7XOX | 7XOX_refined | 3.1 | R | Active | 100 | 62 | Gq/11 | αq | - | 61 | - | scFv16 |
CCK-8
|
peptide | Agonist | desulfated 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 | |
OXYR | OT | Vasopressin and oxytocin | A | Human | Cryo-EM | 7QVM | - | 3.3 | R | Active | 100 | 64 | Gi/o | αo | - | 59 | - | scFv16 |
oxytocin
|
peptide | Agonist | vasopressin, oxytocin | peptide | No | No | Waltenspuhl Y, Ehrenmann J, Vacca S, Thom C, Medalia O, Pluckthun A | 10.1038/S41467-022-31325-0 | 2022-08-10 | Yes | |
AGRG2 | ADGRG2 | ADGRG | B2 | Mouse | Cryo-EM | 7XKD | - | 2.4 | R | Active | 100 | 26 | Gs | αs | - | 57 | - | Nanobody-35 |
PRASTERONE
|
small-molecule | Agonist | - | - | No | No | - | - | 2022-08-10 | Yes | |
P2Y12 | P2Y12 | P2Y | A | Human | X-ray | 7PP1 | - | 2.8 | A | Active | 59 | 78 | - | - | - | - | BRIL | - |
selatogrel
|
small-molecule | Antagonist | ADP, ATP | small-molecule | No | No | Pons V, Garcia C, Tidten-Luksch N, Mac Sweeney A, Caroff E, Gales C, Riederer MA | 10.1016/j.bcp.2022.115291 | 2022-11-02 | Yes | |
S1PR1 | S1P1 | Lysophospholipid (S1P) | A | Human | Cryo-EM | 7VIH | 7VIH_refined | 3.0 | F | Active | 100 | 73 | Gi/o | αi1 | - | 64 | - | scFv16 |
icanbelimod
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | No | No | Yu L, He L, Gan B, Ti R, Xiao Q, Hu H, Zhu L, Wang S, Ren R | 10.1073/PNAS.2117716119 | 2022-09-28 | Yes | |
SSR2 | SST2 | Somatostatin | A | Human | Cryo-EM | 7Y24 | - | 3.3 | E | Active | 100 | 77 | Gi/o | αo | - | 60 | - | scFv16 |
Octreotide
|
peptide | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | No | No | Chen S, Teng X, Zheng S | 10.1038/S41589-022-01130-3 | 2022-10-19 | Yes | |
OPRM | μ | Opioid | A | Human | Cryo-EM | 8EFO | - | 2.8 | R | Active | 100 | 72 | Gi/o | αi1 | - | 64 | - | scFv16 |
PZM21
|
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 | |
O51E2 | Olfactory 51E2 | Olfactory | A | Human | Cryo-EM | 8F76 | 8F76_refined | 3.1 | A | Active | 100 | 94 | Gs | αs | Mini-Gs | 55 | - | Nanobody-35 |
propanoic acid
|
small-molecule | Agonist | - | - | No | No | Billesbolle CB, de March CA, van der Velden WJC, Ma N, Tewari J, Del Torrent CL, Li L, Faust B, Vaidehi N, Matsunami H, Manglik A | 10.1038/S41586-023-05798-Y | 2023-03-22 | Yes | |
GPR21 | GPR21 | A orphans | A | Human | Cryo-EM | 8HMV | 8HMV_refined | 2.9 | A | Active | 100 | 79 | Gs | αs | - | 58 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Wong TS, Gao W, Chen G, Qiu C, He G, Ye F, Wu Z, Zeng Z, Du Y | 10.1002/MCO2.205 | 2023-03-01 | Yes | |
HCAR2 | HCA2 | Hydroxycarboxylic acid | A | Human | Cryo-EM | 7XK2 | 7XK2_refined | 3.1 | R | Active | 100 | 78 | Gi/o | αi1 | - | 63 | - | scFv16 |
MK 6892
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | No | No | Yang Y, Kang HJ, Gao R, Wang J, Han GW, DiBerto JF, Wu L, Tong J, Qu L, Wu Y, Pileski R, Li X, Zhang XC, Zhao S, Kenakin T, Wang Q, Stevens RC, Peng W, Roth BL, Rao Z, Liu ZJ | 10.1038/S41467-023-37177-6 | 2023-02-22 | Yes | |
OPRK | κ | Opioid | A | Human | Cryo-EM | 7Y1F | 7Y1F_refined | 3.3 | R | Active | 100 | 75 | Gi/o | αi1 | - | 61 | - | scFv16 |
dynorphin A-(1-8)
|
peptide | Agonist | [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 | Chen Y, Chen B, Wu T, Zhou F, Xu F | 10.1093/PROCEL/PWAC033 | 2023-05-24 | Yes | |
CNR2 | CB2 | Cannabinoid | A | Human | Cryo-EM | 8GUR | 8GUR_refined | 2.8 | R | Active | 100 | 78 | Gi/o | αi1 | - | 64 | - | scFv16 |
CP55940
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | No | No | Li X, Chang H, Bouma J, de Paus LV, Mukhopadhyay P, Paloczi J, Mustafa M, van der Horst C, Kumar SS, Wu L, Yu Y, van den Berg RJBHN, Janssen APA, Lichtman A, Liu ZJ, Pacher P, van der Stelt M, Heitman LH, Hua T | 10.1038/S41467-023-37112-9 | 2023-05-10 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 8C9W | - | 2.1 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
AB928
|
small-molecule | Antagonist | adenosine | small-molecule | No | No | Claff T, Schlegel JG, Voss JH, Vaassen VJ, Weisse RH, Cheng RKY, Markovic-Mueller S, Bucher D, Strater N, Muller CE | 10.1038/S42004-023-00894-6 | 2023-07-12 | Yes | |
GPR84 | GPR84 | A orphans | A | Human | Cryo-EM | 8J18 | - | 2.9 | R | Active | 100 | 73 | Gi/o | αi1 | - | 62 | - | scFv16 |
(3R)-3-HYDROXYDODECANOIC ACID
|
small-molecule | Agonist | - | - | No | No | Liu H, Zhang Q, He X, Jiang M, Wang S, Yan X, Cheng X, Liu Y, Nan FJ, Xu HE, Xie X, Yin W | 10.1038/S41467-023-38985-6 | 2023-06-21 | Yes | |
PTH1R | PTH1 | Parathyroid hormone | B1 | Human | Cryo-EM | 8JR9 | - | 2.6 | R | Active | 100 | 43 | Gs | αs | - | 59 | - | Nanobody-35 |
PCO371
|
small-molecule | Agonist | TIP39, PTHrP-(1-36), PTHrP, PTH | peptide | No | No | Zhao LH, He Q, Yuan Q, Gu Y, He X, Shan H, Li J, Wang K, Li Y, Hu W, Wu K, Shen J, Xu HE | 10.1038/S41586-023-06467-W | 2023-08-02 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 8FD0 | - | 3.7 | A | Inactive | 24 | 89 | - | - | - | - | - | Nanobody-2 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | 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 | |
ADA1A | α1A | Adrenoceptors | A | Human | Cryo-EM | 8HN1 | - | 2.9 | A | Inactive | 2 | 57 | - | - | - | - | - | Nanobody-6 |
ρ-Da1a
|
peptide | Antagonist | (-)-adrenaline, (-)-noradrenaline | small-molecule | No | No | - | - | 2023-12-20 | Yes | |
MC5R | MC5 | Melanocortin | A | Human | Cryo-EM | 8INR | - | 2.7 | R | Active | 100 | 83 | Gs | αs | Gi1-Gs chimera | 60 | - | - |
INTERMEDINE
|
protein | Agonist | β-MSH, α-MSH, agouti-related protein, γ-MSH, ACTH | peptide | No | No | Chen VB, Arendall WB 3rd, Headd JJ, Keedy DA, Immormino RM, Kapral GJ, Murray LW, Richardson JS, Richardson DC | 10.1107/S0907444909042073 | 2023-09-20 | Yes | |
TAAR1 | TA1 | Trace amine | A | Human | Cryo-EM | 8JLP | - | 3.2 | R | Active | 100 | 84 | Gs | αs | - | 61 | - | - |
ralmitaront
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, 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 | |
GPR61 | GPR61 | A orphans | A | Human | Cryo-EM | 8TB7 | - | 2.9 | R | Active | 85 | 47 | - | - | - | - | BRIL | Fab24 BAK5 heavy chain Fab hinge-binding nanobody Fab24 BAK5 light chain |
compound 1 [PMID: 37741852]
|
small-molecule | Inverse agonist | - | - | No | No | Lees JA, Dias JM, Rajamohan F, Fortin JP, O'Connor R, Kong JX, Hughes EAG, Fisher EL, Tuttle JB, Lovett G, Kormos BL, Unwalla RJ, Zhang L, Dechert Schmitt AM, Zhou D, Moran M, Stevens KA, Fennell KF, Varghese AE, Maxwell A, Cote EE, Zhang Y, Han S | 10.1038/S41467-023-41646-3 | 2023-10-04 | Yes | |
ADRB1 | β1 | Adrenoceptors | A | Wild turkey | X-ray | 4AMI | 4AMI_refined | 3.2 | A | Inactive | 0 | 58 | - | - | - | - | - | - |
Bucindolol
|
small-molecule | Agonist | - | - | No | No | Warne T, Edwards PC, Leslie AG, Tate CG | 10.1016/J.STR.2012.03.014 | 2012-05-23 | Yes | |
SMO | SMO | Frizzled | F | Human | X-ray | 4N4W | 4N4W_refined | 2.8 | A | Inactive | 0 | 44 | - | - | - | - | BRIL | - |
SANT-1
|
small-molecule | Antagonist | - | - | No | No | Wang C, Wu H, Evron T, Vardy E, Han GW, Huang XP, Hufeisen SJ, Mangano TJ, Urban DJ, Katritch V, Cherezov V, Caron MG, Roth BL, Stevens RC | 10.1038/NCOMMS5355 | 2014-01-22 | Yes | |
LPAR1 | LPA1 | Lysophospholipid (LPA) | A | Human | X-ray | 4Z36 | 4Z36_refined | 2.9 | A | Inactive | 1 | 79 | - | - | - | - | BRIL | - |
ONO-3080573
|
small-molecule | Antagonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | No | No | Chrencik JE, Roth CB, Terakado M, Kurata H, Omi R, Kihara Y, Warshaviak D, Nakade S, Asmar-Rovira G, Mileni M, Mizuno H, Griffith MT, Rodgers C, Han GW, Velasquez J, Chun J, Stevens RC, Hanson MA | 10.1016/J.CELL.2015.06.002 | 2015-06-03 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 5JQH | 5JQH_refined | 3.2 | A | Inactive | 0 | 70 | - | - | - | - | T4-Lysozyme | Nanobody |
Carazolol
|
small-molecule | Inverse agonist | L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline | small-molecule | No | No | Staus DP, Strachan RT, Manglik A, Pani B, Kahsai AW, Kim TH, Wingler LM, Ahn S, Chatterjee A, Masoudi A, Kruse AC, Pardon E, Steyaert J, Weis WI, Prosser RS, Kobilka BK, Costa T, Lefkowitz RJ | 10.1038/NATURE18636 | 2016-07-13 | Yes | |
FFAR1 | FFA1 | Free fatty acid | A | Human | X-ray | 5TZR | - | 2.2 | A | Active | 59 | 91 | - | - | - | - | T4-Lysozyme | - |
MK-8666
|
small-molecule | Allosteric agonist | myristic acid, oleic acid, α-linolenic acid, docosahexaenoic acid | small-molecule | No | No | Lu J, Byrne N, Wang J, Bricogne G, Brown FK, Chobanian HR, Colletti SL, Di Salvo J, Thomas-Fowlkes B, Guo Y, Hall DL, Hadix J, Hastings NB, Hermes JD, Ho T, Howard AD, Josien H, Kornienko M, Lumb KJ, Miller MW, Patel SB, Pio B, Plummer CW, Sherborne BS, Sheth P, Souza S, Tummala S, Vonrhein C, Webb M, Allen SJ, Johnston JM, Weinglass AB, Sharma S, Soisson SM | 10.1038/NSMB.3417 | 2017-06-07 | Yes | |
OX2R | OX2 | Orexin | A | Human | X-ray | 5WS3 | 5WS3_refined | 2.3 | A | Inactive | 0 | 70 | - | - | - | - | Glycogen synthase | - |
EMPA
|
small-molecule | Antagonist | orexin-A, orexin-B | peptide | No | No | Suno R, Kimura KT, Nakane T, Yamashita K, Wang J, Fujiwara T, Yamanaka Y, Im D, Horita S, Tsujimoto H, Tawaramoto MS, Hirokawa T, Nango E, Tono K, Kameshima T, Hatsui T, Joti Y, Yabashi M, Shimamoto K, Yamamoto M, Rosenbaum DM, Iwata S, Shimamura T, Kobayashi T | 10.1016/J.STR.2017.11.005 | 2017-12-13 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 6FKA | 6FKA_refined | 2.7 | A | Active | 97 | 94 | - | - | - | - | - | - |
(2~{S})-2-(3,4-dichlorophenyl)-3-methyl-1-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-yl-butan-1-one
|
small-molecule | Agonist | - | - | No | No | Mattle D, Kuhn B, Aebi J, Bedoucha M, Kekilli D, Grozinger N, Alker A, Rudolph MG, Schmid G, Schertler GFX, Hennig M, Standfuss J, Dawson RJP | 10.1073/PNAS.1718084115 | 2018-04-04 | Yes | |
CALRL | calcitonin-like | Calcitonin | B1 | Human | Cryo-EM | 6E3Y | 6E3Y_refined | 3.3 | R | Active | 100 | 75 | Gs | αs | - | 48 | - | Nanobody-35 RAMP1 |
Calcitonin gene-related peptide 1
|
peptide | Agonist | - | - | No | No | Liang YL, Khoshouei M, Deganutti G, Glukhova A, Koole C, Peat TS, Radjainia M, Plitzko JM, Baumeister W, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Wootten D, Sexton PM | 10.1038/S41586-018-0535-Y | 2018-09-19 | Yes | |
B1B1U5 | Rhodopsin | Opsins | A | Hasarius adansoni | X-ray | 6I9K | - | 2.2 | A | Inactive | 9 | 83 | - | - | - | - | - | - |
Retinal (11-cis)
|
small-molecule | Inverse agonist | - | - | No | No | Varma N, Mutt E, Muhle J, Panneels V, Terakita A, Deupi X, Nogly P, Schertler GFX, Lesca E | 10.1073/PNAS.1902192116 | 2019-07-03 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 6PRZ | 6PRZ_refined | 2.8 | A | Inactive | 0 | 68 | - | - | - | - | T4-Lysozyme | - |
CHEMBL1160734
|
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 | |
OX1R | OX1 | Orexin | A | Human | X-ray | 6TP4 | - | 3.0 | A | Inactive | 0 | 70 | - | - | - | - | - | - |
ACT-462206
|
small-molecule | Antagonist | orexin-A, orexin-B | peptide | No | No | Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA. | 10.1021/acs.jmedchem.9b01787 | 2020-01-01 | Yes | |
GPR52 | GPR52 | A orphans | A | Human | Cryo-EM | 6LI3 | - | 3.3 | R | Active | 100 | 79 | Gs | αs | Mini-Gs | 61 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Lin X, Li M, Wang N, Wu Y, Luo Z, Guo S, Han GW, Li S, Yue Y, Wei X, Xie X, Chen Y, Zhao S, Wu J, Lei M, Xu F | 10.1038/S41586-020-2019-0 | 2020-02-26 | Yes | |
GABR2 | GABAB2 | GABAB | C | Human | Cryo-EM | 6UO9 | - | 4.8 | B | Intermediate | - | 73 | - | - | - | - | - | - |
CHEMBL112710
|
small-molecule | Agonist | - | - | No | No | 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 | |
DRD2 | D2 | Dopamine | A | Human | X-ray | 7DFP | 7DFP_refined | 3.1 | A | Inactive | 0 | 57 | - | - | - | - | BRIL | Fab heavy chain Fab light chain |
spiperone
|
small-molecule | Antagonist | dopamine | small-molecule | No | No | Im D, Inoue A, Fujiwara T, Nakane T, Yamanaka Y, Uemura T, Mori C, Shiimura Y, Kimura KT, Asada H, Nomura N, Tanaka T, Yamashita A, Nango E, Tono K, Kadji FMN, Aoki J, Iwata S, Shimamura T | 10.1038/S41467-020-20221-0 | 2020-12-30 | Yes | |
NTR1 | NTS1 | Neurotensin | A | Rat | X-ray | 6ZIN | - | 2.6 | A | Inactive | 33 | 76 | - | - | - | - | DARPin D12 | - |
meclinertant
|
small-molecule | Inverse agonist | neurotensin, neuromedin N | peptide | No | No | Deluigi M, Klipp A, Klenk C, Merklinger L, Eberle SA, Morstein L, Heine P, Mittl PRE, Ernst P, Kamenecka TM, He Y, Vacca S, Egloff P, Honegger A, Pluckthun A | 10.1126/sciadv.abe5504 | 2021-02-10 | Yes | |
5HT1E | 5-HT1E | 5-Hydroxytryptamine | A | Human | Cryo-EM | 7E33 | 7E33_refined | 2.9 | R | Active | 100 | 70 | Gi/o | αi1 | - | 61 | - | scFv16 |
BRL-54443
|
small-molecule | Agonist | tryptamine, 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 | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 7E14 | - | 2.9 | R | Active | 100 | 81 | Gs | αs | - | 49 | - | Nanobody-35 |
N-Tert-butyl-6,7-dichloroquinoxalin-2-amine
orforglipron |
small-molecule small-molecule |
Ago-PAM Agonist |
glucagon-like peptide 1-(7-36) 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 | 2021-07-07 | Yes | |
CCKAR | CCK1 | Cholecystokinin | A | Human | Cryo-EM | 7EZM | - | 2.9 | D | Active | 100 | 71 | Gq/11 | αq | - | 63 | - | scFv16 |
CCK-8
|
peptide | Agonist | desulfated cholecystokinin-8, CCK-58, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8 | peptide | No | No | Liu Q, Yang D, Zhuang Y, Croll TI, Cai X, Dai A, He X, Duan J, Yin W, Ye C, Zhou F, Wu B, Zhao Q, Xu HE, Wang MW, Jiang Y | 10.1038/S41589-021-00841-3 | 2021-08-25 | Yes | |
MC4R | MC4 | Melanocortin | A | Human | Cryo-EM | 7F53 | - | 3.0 | R | Active | 100 | 82 | Gs | αs | - | 58 | - | Nanobody-35 |
α-MSH
|
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 | |
NK1R | NK1 | Tachykinin | A | Human | Cryo-EM | 7P02 | - | 2.9 | R | Active | 100 | 71 | Gs | αs | Gs-Gi1 chimera | 57 | - | scFv16 |
substance P
|
peptide | Agonist | neuropeptide-γ, neurokinin A, neuropeptide K, neurokinin B, hemokinin 1, substance P | peptide | No | No | Thom C, Ehrenmann J, Vacca S, Waltenspuhl Y, Schoppe J, Medalia O, Pluckthun A | 10.1126/SCIADV.ABK2872 | 2021-12-15 | Yes | |
GHRHR | GHRH | Glucagon | B1 | Human | Cryo-EM | 7V9M | 7V9M_refined | 3.3 | R | Active | 100 | 63 | Gs | αs | - | 57 | - | Nanobody-35 |
Somatoliberin
|
peptide | Agonist | GHRH | peptide | No | No | Cong Z, Zhou F, Zhang C, Zou X, Zhang H, Wang Y, Zhou Q, Cai X, Liu Q, Li J, Shao L, Mao C, Wang X, Wu J, Xia T, Zhao LH, Jiang H, Zhang Y, Xu HE, Cheng X, Yang D, Wang MW | 10.1073/PNAS.2106606118 | 2021-10-20 | Yes | |
LPAR1 | LPA1 | Lysophospholipid (LPA) | A | Human | Cryo-EM | 7TD1 | - | 3.1 | R | Active | 100 | 80 | Gi/o | αi1 | - | 62 | - | - |
lysophosphatidic acid
|
small-molecule | Agonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | No | No | Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY | 10.1038/S41467-022-28417-2 | 2022-02-09 | Yes | |
FPR2 | FPR2/ALX | Formylpeptide | A | Human | Cryo-EM | 7WVW | - | 3.1 | R | Active | 100 | 85 | Gi/o | αi2 | - | 63 | BRIL | - |
FME-TYR-PHE-ILE-ASN-ILE-LEU-THE-LEU
|
peptide | 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 | Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B | 10.1038/S41467-022-29361-X | 2022-04-13 | Yes | |
GPR88 | GPR88 | A orphans | A | Human | Cryo-EM | 7EJX | - | 2.4 | R | Active | 100 | 60 | Gi/o | αi1 | - | 61 | - | scFv16 |
compound 2 [PMID: 24793972]
|
small-molecule | Allosteric agonist | - | - | No | No | Chen G, Xu J, Inoue A, Schmidt MF, Bai C, Lu Q, Gmeiner P, Liu Z, Du Y | 10.1038/S41467-022-30081-5 | 2022-04-13 | Yes | |
OX2R | OX2 | Orexin | A | Human | Cryo-EM | 7SR8 | - | 3.3 | R | Active | 100 | 64 | Gq/11 | αq | - | 58 | - | scFv16 |
methyl (2R,3S)-3-[(methanesulfonyl)amino]-2-({[(1s,4S)-4-phenylcyclohexyl]oxy}methyl)piperidine-1-carboxylate
|
small-molecule | Agonist | orexin-A, orexin-B | peptide | No | No | Yin J, Kang Y, McGrath AP, Chapman K, Sjodt M, Kimura E, Okabe A, Koike T, Miyanohana Y, Shimizu Y, Rallabandi R, Lian P, Bai X, Flinspach M, De Brabander JK, Rosenbaum DM | 10.1038/S41467-022-30601-3 | 2022-06-08 | Yes | |
SSR2 | SST2 | Somatostatin | A | Human | Cryo-EM | 7UL5 | 7UL5_refined | 3.1 | A | Inactive | 6 | 77 | - | - | - | - | - | Nanobody-6 |
Apo (no ligand)
|
none | Apo (no ligand) | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | No | No | Robertson MJ, Papasergi-Scott MM, He F, Seven AB, Meyerowitz JG, Panova O, Peroto MC, Che T, Skiniotis G | 10.1038/S41594-022-00859-8 | 2022-06-29 | Yes | |
5HT6R | 5-HT6 | 5-Hydroxytryptamine | A | Human | Cryo-EM | 7XTB | 7XTB_refined | 3.3 | R | Active | 100 | 63 | Gs | αs | - | 60 | BRIL | Nanobody-35 |
5-hydroxytryptamine
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | No | No | Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE | 10.1016/J.MOLCEL.2022.05.031 | 2022-07-27 | Yes | |
MRGRD | MRGPRD | A orphans | A | Human | Cryo-EM | 7Y14 | - | 3.2 | R | Intermediate | 49 | 82 | - | - | - | - | BRIL | - |
β-alanine
|
small-molecule | Agonist | β-alanine | small-molecule | No | No | Suzuki S, Iida M, Hiroaki Y, Tanaka K, Kawamoto A, Kato T, Oshima A | 10.1038/S42003-022-03668-3 | 2022-07-20 | Yes | |
SSR2 | SST2 | Somatostatin | A | Human | X-ray | 7XNA | - | 2.7 | A | Inactive | 6 | 78 | - | - | - | - | - | - |
CYN 154806
|
peptide | Antagonist | 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 | |
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 | Yes | Shiriaeva A, Park D, Kim G, Lee Y, Hou X, Jarhad DB, Kim G, Yu J, Hyun YE, Kim W, Gao ZG, Jacobson KA, Han GW, Stevens RC, Jeong LS, Choi S, Cherezov V. | 10.1021/acs.jmedchem.2c00462 | 2022-08-31 | Yes | |
TSHR | TSH | Glycoprotein hormone | A | Human | Cryo-EM | 7T9N | - | 2.9 | R | Active | 100 | 73 | Gs | αs | Mini-Gs | 56 | - | M22 Fab light chain M22 Fab heavy chain Nanobody-35 |
M22 antibody heavy chain
M22 antibody light chain |
protein protein |
Agonist | TSH | peptide | No | No | Faust B, Billesbolle CB, Suomivuori CM, Singh I, Zhang K, Hoppe N, Pinto AFM, Diedrich JK, Muftuoglu Y, Szkudlinski MW, Saghatelian A, Dror RO, Cheng Y, Manglik A | 10.1038/S41586-022-05159-1 | 2022-08-03 | Yes | |
ADRB1 | β1 | Adrenoceptors | A | Wild turkey | X-ray | 4AMJ | 4AMJ_refined | 2.3 | B | Inactive | 0 | 62 | - | - | - | - | - | - |
CHEMBL3799125
|
small-molecule | Inverse agonist | - | - | No | No | Warne T, Edwards PC, Leslie AG, Tate CG | 10.1016/J.STR.2012.03.014 | 2012-05-23 | Yes | |
NTR1 | NTS1 | Neurotensin | A | Rat | X-ray | 4BWB | - | 3.6 | A | Inactive | 3 | 72 | - | - | - | - | - | - |
neurotensin
|
peptide | Agonist | neurotensin, neuromedin N | peptide | No | No | Egloff P, Hillenbrand M, Klenk C, Batyuk A, Heine P, Balada S, Schlinkmann KM, Scott DJ, Schutz M, Pluckthun A | 10.1073/PNAS.1317903111 | 2014-01-29 | Yes | |
GRM5 | mGlu5 | Metabotropic glutamate | C | Human | X-ray | 5CGD | 5CGD_refined | 2.6 | A | Inactive | - | 20 | - | - | - | - | T4-Lysozyme | - |
CHEMBL3603923
|
small-molecule | NAM | L-glutamic acid | small-molecule | No | No | Christopher JA, Aves SJ, Bennett KA, Doré AS, Errey JC, Jazayeri A, Marshall FH, Okrasa K, Serrano-Vega MJ, Tehan BG, Wiggin GR, Congreve M. | 10.1021/acs.jmedchem.5b00892 | 2015-08-12 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5G53 | - | 3.4 | A | Active | 100 | 68 | Gs | αs | Engineered G protein | 50 | - | - |
NECA
|
small-molecule | Agonist | adenosine | small-molecule | No | No | Carpenter B, Nehme R, Warne T, Leslie AG, Tate CG | 10.1038/NATURE18966 | 2016-08-03 | Yes | |
GLP1R | GLP-1 | Glucagon | B1 | Human | X-ray | 5NX2 | - | 3.7 | A | Intermediate | 56 | 84 | - | - | - | - | - | - |
Truncated protein agonist
|
peptide | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | No | No | Jazayeri A, Rappas M, Brown AJH, Kean J, Errey JC, Robertson NJ, Fiez-Vandal C, Andrews SP, Congreve M, Bortolato A, Mason JS, Baig AH, Teobald I, Dore AS, Weir M, Cooke RM, Marshall FH | 10.1038/NATURE22800 | 2017-06-14 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5OM1 | 5OM1_refined | 2.1 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
CHEMBL2024114
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | Rucktooa P, Cheng RKY, Segala E, Geng T, Errey JC, Brown GA, Cooke RM, Marshall FH, Dore AS | 10.1038/S41598-017-18570-W | 2018-01-17 | Yes | |
OPRM | μ | Opioid | A | Mouse | Cryo-EM | 6DDE | - | 3.5 | R | Active | 100 | 71 | Gi/o | αi1 | - | 61 | - | Antibody |
DAMGO
|
peptide | Agonist | - | - | No | No | Koehl A, Hu H, Maeda S, Zhang Y, Qu Q, Paggi JM, Latorraca NR, Hilger D, Dawson R, Matile H, Schertler GFX, Granier S, Weis WI, Dror RO, Manglik A, Skiniotis G, Kobilka BK | 10.1038/S41586-018-0219-7 | 2018-06-13 | Yes | |
NK1R | NK1 | Tachykinin | A | Human | X-ray | 6HLP | 6HLP_refined | 2.2 | A | Inactive | 0 | 71 | - | - | - | - | GlgA glycogen synthase | - |
netupitant
|
small-molecule | Antagonist | neuropeptide-γ, neurokinin A, neuropeptide K, neurokinin B, hemokinin 1, 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 | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 6E67 | - | 3.7 | B | Active | 100 | 72 | Gs | αs | Fused partial Gs | 44 | T4-Lysozyme | - |
CHEMBL1615159
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline | small-molecule | No | No | Liu X, Xu X, Hilger D, Aschauer P, Tiemann JKS, Du Y, Liu H, Hirata K, Sun X, Guixa-Gonzalez R, Mathiesen JM, Hildebrand PW, Kobilka BK | 10.1016/J.CELL.2019.04.021 | 2019-06-05 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 6PS3 | 6PS3_refined | 2.5 | A | Inactive | 0 | 68 | - | - | - | - | T4-Lysozyme | - |
CHEMBL3799125
|
small-molecule | Antagonist | 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 | |
OX1R | OX1 | Orexin | A | Human | X-ray | 6TQ6 | 6TQ6_refined | 2.6 | B | Inactive | 0 | 71 | - | - | - | - | - | - |
CHEMBL4592653
|
small-molecule | Antagonist | orexin-A, orexin-B | peptide | No | No | Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA. | 10.1021/acs.jmedchem.9b01787 | 2020-01-01 | Yes | |
GPR52 | GPR52 | A orphans | A | Human | X-ray | 6LI2 | - | 2.8 | A | Intermediate | 40 | 80 | - | - | - | - | Rubredoxin | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Lin X, Li M, Wang N, Wu Y, Luo Z, Guo S, Han GW, Li S, Yue Y, Wei X, Xie X, Chen Y, Zhao S, Wu J, Lei M, Xu F | 10.1038/S41586-020-2019-0 | 2020-02-26 | Yes | |
CALRL | calcitonin-like | Calcitonin | B1 | Human | Cryo-EM | 6UUS | 6UUS_refined | 2.4 | R | Active | 100 | 74 | Gs | αs | - | 48 | - | Nanobody-35 RAMP3 |
Adrenomedullin
|
peptide | Agonist | - | - | No | No | Liang YL, Belousoff MJ, Fletcher MM, Zhang X, Khoshouei M, Deganutti G, Koole C, Furness SGB, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Danev R, Wootten D, Sexton PM | 10.1021/ACSPTSCI.9B00080 | 2020-04-01 | Yes | |
GPBAR | GPBA | Bile acid | A | Human | Cryo-EM | 7CFN | 7CFN_refined | 3.0 | R | Active | 100 | 83 | Gs | αs | - | 59 | - | Nanobody-35 |
INT-777
INT-777 |
small-molecule small-molecule |
Agonist PAM |
deoxycholic acid, cholic acid, chenodeoxycholic acid, lithocholic acid | small-molecule | No | No | - | - | 2020-09-09 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 6LPK | 6LPK_refined | 1.8 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
ZM-241385
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | Ihara K, Hato M, Nakane T, Yamashita K, Kimura-Someya T, Hosaka T, Ishizuka-Katsura Y, Tanaka R, Tanaka T, Sugahara M, Hirata K, Yamamoto M, Nureki O, Tono K, Nango E, Iwata S, Shirouzu M | 10.1038/S41598-020-76277-X | 2020-11-25 | Yes | |
AGRG3 | ADGRG3 | ADGRG | B2 | Human | Cryo-EM | 7D76 | - | 3.1 | R | Active | 100 | 48 | Gi/o | αo | - | 61 | - | - |
Beclomethasone
|
small-molecule | Agonist | - | - | No | No | Ping YQ, Mao C, Xiao P, Zhao RJ, Jiang Y, Yang Z, An WT, Shen DD, Yang F, Zhang H, Qu C, Shen Q, Tian C, Li ZJ, Li S, Wang GY, Tao X, Wen X, Zhong YN, Yang J, Yi F, Yu X, Xu HE, Zhang Y, Sun JP | 10.1038/S41586-020-03083-W | 2021-02-03 | Yes | |
DRD1 | D1 | Dopamine | A | Human | Cryo-EM | 7CRH | 7CRH_refined | 3.3 | R | Active | 100 | 61 | Gs | αs | - | 60 | - | Nanobody-35 |
CHEMBL1416789
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | No | No | Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z | 10.1016/J.CELL.2021.01.028 | 2021-03-03 | Yes | |
V2R | V2 | Vasopressin and oxytocin | A | Human | Cryo-EM | 7BB6 | - | 4.2 | A | Active | 100 | 73 | Gs | αs | - | 54 | - | Nanobody-35 |
vasopressin
|
peptide | Agonist | vasopressin, oxytocin | peptide | No | No | Bous J, Orcel H, Floquet N, Leyrat C, Lai-Kee-Him J, Gaibelet G, Ancelin A, Saint-Paul J, Trapani S, Louet M, Sounier R, Demene H, Granier S, Bron P, Mouillac B | 10.1126/SCIADV.ABG5628 | 2021-06-02 | Yes | |
CCR5 | CCR5 | Chemokine | A | Human | Cryo-EM | 7F1S | 7F1S_refined | 2.8 | R | Active | 100 | 78 | Gi/o | αi1 | - | 61 | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | CCL14, CCL8, CCL13, CCL4, CCL7, CCL2, CCL5, CCL11, CCL3, CCL16 | peptide | No | No | Zhang H, Chen K, Tan Q, Shao Q, Han S, Zhang C, Yi C, Chu X, Zhu Y, Xu Y, Zhao Q, Wu B | 10.1038/S41467-021-24438-5 | 2021-07-14 | Yes | |
GRM5 | mGlu5 | Metabotropic glutamate | C | Human | Cryo-EM | 7FD9 | 7FD9_refined | 4.0 | A | Inactive | - | 63 | - | - | - | - | - | - |
LY341495
|
small-molecule | Antagonist | L-glutamic acid | small-molecule | No | No | Nasrallah C, Cannone G, Briot J, Rottier K, Berizzi AE, Huang CY, Quast RB, Hoh F, Baneres JL, Malhaire F, Berto L, Dumazer A, Font-Ingles J, Gomez-Santacana X, Catena J, Kniazeff J, Goudet C, Llebaria A, Pin JP, Vinothkumar KR, Lebon G | 10.1016/J.CELREP.2021.109648 | 2021-09-08 | Yes | |
CCKAR | CCK1 | Cholecystokinin | A | Human | X-ray | 7F8Y | 7F8Y_refined | 2.5 | A | Inactive | 0 | 65 | - | - | - | - | T4-Lysozyme | - |
DEVAZEPIDE
|
small-molecule | Antagonist | desulfated cholecystokinin-8, CCK-58, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8 | peptide | No | No | Zhang X, He C, Wang M, Zhou Q, Yang D, Zhu Y, Feng W, Zhang H, Dai A, Chu X, Wang J, Yang Z, Jiang Y, Sensfuss U, Tan Q, Han S, Reedtz-Runge S, Xu HE, Zhao S, Wang MW, Wu B, Zhao Q | 10.1038/S41589-021-00866-8 | 2021-10-13 | Yes | |
MRGX2 | MRGPRX2 | A orphans | A | Human | Cryo-EM | 7VDH | - | 2.9 | R | Active | 100 | 81 | Gi/o | αi1 | - | 62 | - | scFv16 |
compound 48/80
|
small-molecule | Agonist | PAMP-20 | peptide | No | No | Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP | 10.1038/S41586-021-04077-Y | 2021-12-01 | Yes | |
5HT2A | 5-HT2A | 5-Hydroxytryptamine | A | Human | X-ray | 7WC4 | 7WC4_refined | 3.2 | A | Inactive | 1 | 61 | - | - | - | - | BRIL | - |
5-hydroxytryptamine
|
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 | |
S1PR1 | S1P1 | Lysophospholipid (S1P) | A | Human | Cryo-EM | 7EW7 | - | 3.3 | D | Active | 100 | 75 | Gi/o | αi1 | - | 64 | - | scFv16 |
SEW2871
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | No | No | Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z | 10.1038/S41422-021-00566-X | 2021-09-29 | Yes | |
S1PR1 | S1P1 | Lysophospholipid (S1P) | A | Human | Cryo-EM | 7TD3 | - | 3.0 | R | Active | 100 | 76 | Gi/o | αi1 | - | 63 | - | - |
sphingosine 1-phosphate
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | No | No | Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY | 10.1038/S41467-022-28417-2 | 2022-02-09 | Yes | |
GLR | glucagon | Glucagon | B1 | Human | Cryo-EM | 7V35 | 7V35_refined | 3.4 | R | Active | 100 | 82 | Gs | αs | - | 53 | - | Nanobody-35 |
Peptide-20
|
peptide | Agonist | glucagon | peptide | No | No | Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW | 10.1038/S41467-022-28683-0 | 2022-03-02 | Yes | |
NMUR1 | NMU1 | Neuromedin U | A | Human | Cryo-EM | 7W53 | - | 3.2 | R | Active | 100 | 62 | Gq/11 | αq | - | 54 | - | scFv16 |
Neuromedin U-25 (human)
|
peptide | Agonist | neuromedin U-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 | |
5HT5A | 5-HT5A | 5-Hydroxytryptamine | A | Human | Cryo-EM | 7UM7 | 7UM7_refined | 2.8 | A | Active | 100 | 72 | Gi/o | αo | Mini-Go | 60 | - | scFv16 |
methylergonovine
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | No | No | Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL | 10.1038/S41594-022-00796-6 | 2022-07-20 | Yes | |
ACKR3 | ACKR3 | Chemokine | A | Human | Cryo-EM | 7SK9 | 7SK9_refined | 3.7 | A | Active | 97 | 78 | - | - | - | - | - | CID24 Fab heavy chain CID24 Fab light chain |
(1R)-4-[7-(3-carboxypropoxy)-6-methylquinolin-8-yl]-1-{[2-(4-hydroxypiperidin-1-yl)-1,3-thiazol-4-yl]methyl}-1,4-diazepan-1-ium
|
small-molecule | Agonist (partial) | CXCL11, CXCL12α | peptide | No | No | Yen YC, Schafer CT, Gustavsson M, Eberle SA, Dominik PK, Deneka D, Zhang P, Schall TJ, Kossiakoff AA, Tesmer JJG, Handel TM | 10.1126/SCIADV.ABN8063 | 2022-07-27 | Yes | |
TSHR | TSH | Glycoprotein hormone | A | Human | Cryo-EM | 7XW5 | - | 3.0 | R | Active | 100 | 75 | Gs | αs | - | 60 | - | Nanobody-35 |
Thyrotropin subunit beta
Glycoprotein hormones alpha chain N-[4-[[5-[(2S)-3-benzyl-5-hydroxy-4-oxo-1,2-dihydroquinazolin-2-yl]-2-methoxyphenyl]methoxy]phenyl]acetamide |
protein protein small-molecule |
Agonist | TSH | peptide | No | No | Duan J, Xu P, Luan X, Ji Y, He X, Song N, Yuan Q, Jin Y, Cheng X, Jiang H, Zheng J, Zhang S, Jiang Y, Xu HE | 10.1038/S41586-022-05173-3 | 2022-08-24 | Yes | |
TAAR9 | TAAR9 | A orphans | A | Mouse | Cryo-EM | 8IWM | - | 3.2 | R | Active | 98 | 78 | - | - | - | - | - | - |
2-Phenylethanaminium
|
small-molecule | Agonist | - | - | No | No | Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP | 10.1038/S41586-023-06106-4 | 2023-05-31 | Yes | |
P2Y12 | P2Y12 | P2Y | A | Human | Cryo-EM | 7XXI | 7XXI_refined | 3.0 | A | Active | 100 | 86 | Gi/o | αi2 | - | 61 | - | - |
2MeSADP
|
small-molecule | Agonist | ADP, ATP | small-molecule | No | No | - | - | 2023-06-07 | Yes | |
FFAR1 | FFA1 | Free fatty acid | A | Human | Cryo-EM | 8EJC | - | 3.0 | R | Active | 100 | 90 | Gq/11 | αq | - | 60 | - | scFv16 |
fasiglifam
|
small-molecule | Agonist | myristic acid, oleic acid, α-linolenic 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 | |
PTH1R | PTH1 | Parathyroid hormone | B1 | Human | Cryo-EM | 8FLU | - | 2.8 | R | Active | 100 | 61 | Gs | αs | - | 58 | - | Nanobody-35 |
PTH
|
peptide | 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 | |
DRD4 | D4 | Dopamine | A | Human | Cryo-EM | 8IRU | - | 3.2 | R | Active | 100 | 64 | Gi/o | αi1 | - | 60 | - | scFv16 |
rotigotine
|
small-molecule | Agonist | dopamine | small-molecule | No | No | Xu P, Huang S, Krumm BE, Zhuang Y, Mao C, Zhang Y, Wang Y, Huang XP, Liu YF, He X, Li H, Yin W, Jiang Y, Zhang Y, Roth BL, Xu HE | 10.1038/S41422-023-00808-0 | 2023-06-21 | Yes | |
NTR1 | NTS1 | Neurotensin | A | Human | Cryo-EM | 8JPB | - | 3.1 | R | Active | 100 | 71 | Gq/11 | αq | GRK2 bound | 88 | - | GRK2 |
JMV431
CHEMBL4576388 |
peptide small-molecule |
Agonist PAM |
large neurotensin, large neuromedin N, neurotensin, neuromedin N | peptide | No | No | Duan J, Liu H, Zhao F, Yuan Q, Ji Y, Cai X, He X, Li X, Li J, Wu K, Gao T, Zhu S, Lin S, Wang MW, Cheng X, Yin W, Jiang Y, Yang D, Xu HE | 10.1038/S41586-023-06395-9 | 2023-08-09 | Yes | |
OPRM | μ | Opioid | A | Mouse | X-ray | 8E0G | - | 2.1 | A | Active | 100 | 74 | - | - | - | - | - | Nanobody-39 |
BU72
|
small-molecule | Agonist | - | - | No | No | Munro TA | 10.1186/S12915-023-01689-W | 2023-10-18 | Yes | |
C5AR1 | C5a1 | Complement peptide | A | Mouse | Cryo-EM | 8HPT | - | 3.4 | A | Active | 100 | 73 | Gi/o | αo | - | 58 | - | scFv16 |
C5a
|
peptide | Agonist | - | - | No | No | - | HTTPS://DOI.ORG/10.1016/J.CELL.2023.09.020 | 2023-10-18 | Yes | |
HCAR2 | HCA2 | Hydroxycarboxylic acid | A | Human | Cryo-EM | 8IJB | 8IJB_refined | 3.2 | A | Active | 100 | 81 | Gi/o | αi1 | - | 61 | - | scFv16 |
5-Methyl-4-oxidanyl-pyrazin-4-ium-2-carboxylic 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 | |
ADRB2 | β2 | Adrenoceptors | A | Human | Cryo-EM | 8JJL | - | 3.2 | A | Inactive | 0 | 68 | - | - | - | - | BRIL | - |
olodaterol
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline | small-molecule | 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 | |
GPR61 | GPR61 | A orphans | A | Human | Cryo-EM | 8KGK | 8KGK_refined | 3.2 | A | Active | 100 | 57 | Gs | αs | - | 58 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | 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 | 2023-10-11 | Yes | |
5HT1A | 5-HT1A | 5-Hydroxytryptamine | A | Human | Cryo-EM | 8W8B | - | 3.0 | R | Active | 100 | 66 | Gi/o | αi1 | - | 61 | BRIL | scFv16 |
ulotaront
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | No | No | Liu H, Zheng Y, Wang Y, Wang Y, He X, Xu P, Huang S, Yuan Q, Zhang X, Wang L, Jiang K, Chen H, Li Z, Liu W, Wang S, Xu HE, Xu F | 10.1038/S41586-023-06775-1 | 2023-11-22 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 4EIY | 4EIY_refined | 1.8 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
ZM-241385
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | Liu W, Chun E, Thompson AA, Chubukov P, Xu F, Katritch V, Han GW, Roth CB, Heitman LH, IJzerman AP, Cherezov V, Stevens RC | 10.1126/SCIENCE.1219218 | 2012-07-25 | Yes | |
SMO | SMO | Frizzled | F | Human | X-ray | 4O9R | 4O9R_refined | 3.2 | A | Inactive | 11 | 42 | - | - | - | - | BRIL | - |
cyclopamine
|
small-molecule | Antagonist | - | - | No | No | Weierstall U, James D, Wang C, White TA, Wang D, Liu W, Spence JC, Bruce Doak R, Nelson G, Fromme P, Fromme R, Grotjohann I, Kupitz C, Zatsepin NA, Liu H, Basu S, Wacker D, Han GW, Katritch V, Boutet S, Messerschmidt M, Williams GJ, Koglin JE, Marvin Seibert M, Klinker M, Gati C, Shoeman RL, Barty A, Chapman HN, Kirian RA, Beyerlein KR, Stevens RC, Li D, Shah ST, Howe N, Caffrey M, Cherezov V | 10.1038/NCOMMS4309 | 2014-03-05 | Yes | |
GRM5 | mGlu5 | Metabotropic glutamate | C | Human | X-ray | 5CGC | 5CGC_refined | 3.1 | A | Inactive | - | 20 | - | - | - | - | T4-Lysozyme | - |
CHEMBL3603915
|
small-molecule | NAM | L-glutamic acid | small-molecule | No | No | Christopher JA, Aves SJ, Bennett KA, Doré AS, Errey JC, Jazayeri A, Marshall FH, Okrasa K, Serrano-Vega MJ, Tehan BG, Wiggin GR, Congreve M. | 10.1021/acs.jmedchem.5b00892 | 2015-08-12 | Yes | |
SMO | SMO | Frizzled | F | Human | X-ray | 5L7I | 5L7I_refined | 3.3 | B | Inactive | 4 | 59 | - | - | - | - | BRIL | - |
vismodegib
|
small-molecule | Antagonist | - | - | No | No | - | - | 2016-07-20 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 5X7D | 5X7D_refined | 2.7 | A | Inactive | 0 | 68 | - | - | - | - | T4-Lysozyme | - |
4-carbamoyl-N-[(2R)-2-cyclohexyl-2-phenylacetyl]-L-phenylalanyl-3-bromo-N-methyl-L-phenylalaninamide
Carazolol |
small-molecule small-molecule |
Allosteric antagonist Antagonist |
L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline | small-molecule | No | No | Liu X, Ahn S, Kahsai AW, Meng KC, Latorraca NR, Pani B, Venkatakrishnan AJ, Masoudi A, Weis WI, Dror RO, Chen X, Lefkowitz RJ, Kobilka BK | 10.1038/NATURE23652 | 2017-08-16 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 6FK7 | 6FK7_refined | 2.6 | A | Active | 97 | 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 | |
FZD4 | FZD4 | Frizzled | F | Human | X-ray | 6BD4 | 6BD4_refined | 2.4 | A | Inactive | 22 | 61 | - | - | - | - | Rubredoxin | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Yang S, Wu Y, Xu TH, de Waal PW, He Y, Pu M, Chen Y, DeBruine ZJ, Zhang B, Zaidi SA, Popov P, Guo Y, Han GW, Lu Y, Suino-Powell K, Dong S, Harikumar KG, Miller LJ, Katritch V, Xu HE, Shui W, Stevens RC, Melcher K, Zhao S, Xu F | 10.1038/S41586-018-0447-X | 2018-08-22 | Yes | |
ACM2 | M2 | Acetylcholine (muscarinic) | A | Human | X-ray | 5ZKB | 5ZKB_refined | 3.0 | A | Inactive | 2 | 60 | - | - | - | - | BRIL | - |
AF-DX 384
|
small-molecule | Antagonist | acetylcholine | small-molecule | No | No | Suno R, Lee S, Maeda S, Yasuda S, Yamashita K, Hirata K, Horita S, Tawaramoto MS, Tsujimoto H, Murata T, Kinoshita M, Yamamoto M, Kobilka BK, Vaidehi N, Iwata S, Kobayashi T | 10.1038/S41589-018-0152-Y | 2018-11-21 | Yes | |
PTH1R | PTH1 | Parathyroid hormone | B1 | Human | Cryo-EM | 6NBF | - | 3.0 | R | Active | 100 | 62 | Gs | αs | - | 58 | - | Nanobody-35 |
Long-acting parathyroid hormone analog
|
peptide | Agonist | 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 | 6RZ7 | - | 2.4 | A | Active | 59 | 79 | - | - | - | - | BRIL | - |
ONO-2570366
|
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 | |
EDNRB | ETB | Endothelin | A | Human | X-ray | 6LRY | 6LRY_refined | 3.0 | A | Inactive | 17 | 70 | - | - | - | - | T4-Lysozyme | - |
sarafotoxin S6b
|
peptide | Agonist | endothelin-1, endothelin-2, endothelin-3 | peptide | No | No | Izume T, Miyauchi H, Shihoya W, Nureki O | 10.1016/J.BBRC.2019.12.091 | 2020-02-12 | Yes | |
DRD2 | D2 | Dopamine | A | Human | Cryo-EM | 6VMS | - | 3.8 | R | Active | 100 | 63 | Gi/o | αi1 | - | 64 | T4-Lysozyme | scFv16 |
bromocriptine
|
small-molecule | Agonist | dopamine | small-molecule | No | No | Yin J, Chen KM, Clark MJ, Hijazi M, Kumari P, Bai XC, Sunahara RK, Barth P, Rosenbaum DM | 10.1038/S41586-020-2379-5 | 2020-06-17 | Yes | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 7C2E | - | 4.2 | R | Active | 100 | 82 | Gs | αs | - | 49 | - | Nanobody-35 |
2-[[4-[6-[(4-cyano-2-fluoranyl-phenyl)methoxy]pyridin-2-yl]-3,6-dihydro-2~{H}-pyridin-1-yl]methyl]-3-[[(2~{S})-oxetan-2-yl]methyl]imidazo[4,5-b]pyridine-5-carboxylic acid
|
small-molecule | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | No | No | Ma H, Huang W, Wang X, Zhao L, Jiang Y, Liu F, Guo W, Sun X, Zhong W, Yuan D, Xu HE | 10.1038/S41422-020-0384-8 | 2020-08-26 | Yes | |
GABR2 | GABAB2 | GABAB | C | Human | Cryo-EM | 7CA3 | - | 4.5 | B | Active | - | 72 | - | - | - | - | - | - |
BHFF
|
small-molecule | PAM | - | - | No | No | Kim Y, Jeong E, Jeong JH, Kim Y, Cho Y | 10.1016/J.JMB.2020.09.023 | 2020-11-11 | Yes | |
OX2R | OX2 | Orexin | A | Human | Cryo-EM | 7L1V | - | 3.0 | R | Active | 100 | 64 | Gs | αs | Engineered G alpha | 58 | - | scFv16 Nanobody-51 |
compound 1 [PMID: 33547286]
|
small-molecule | Agonist | orexin-A, orexin-B | peptide | No | No | Hong C, Byrne NJ, Zamlynny B, Tummala S, Xiao L, Shipman JM, Partridge AT, Minnick C, Breslin MJ, Rudd MT, Stachel SJ, Rada VL, Kern JC, Armacost KA, Hollingsworth SA, O'Brien JA, Hall DL, McDonald TP, Strickland C, Brooun A, Soisson SM, Hollenstein K | 10.1038/S41467-021-21087-6 | 2021-02-10 | Yes | |
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, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | No | No | Sun B, Feng D, Chu ML, Fish I, Lovera S, Sands ZA, Kelm S, Valade A, Wood M, Ceska T, Kobilka TS, Lebon F, Kobilka BK | 10.1038/S41467-021-23519-9 | 2021-04-14 | Yes | |
GRM2 | mGlu2 | Metabotropic glutamate | C | Human | X-ray | 7EPE | 7EPE_refined | 2.5 | A | Inactive | - | 28 | - | - | - | - | Flavodoxin | - |
CHEMBL3894759
|
small-molecule | NAM | L-glutamic acid | small-molecule | No | No | Du J, Wang D, Fan H, Xu C, Tai L, Lin S, Han S, Tan Q, Wang X, Xu T, Zhang H, Chu X, Yi C, Liu P, Wang X, Zhou Y, Pin JP, Rondard P, Liu H, Liu J, Sun F, Wu B, Zhao Q | 10.1038/S41586-021-03641-W | 2021-06-23 | Yes | |
GRM2 | mGlu2 | Metabotropic glutamate | C | Human | Cryo-EM | 7MTS | - | 3.2 | A | Active | - | 90 | Gi/o | αi1 | - | 58 | - | - |
2-methoxy-6-propyl-N-(2-{4-[(1H-tetrazol-5-yl)methoxy]phenyl}ethyl)thieno[2,3-d]pyrimidin-4-amine
L-glutamic acid |
small-molecule small-molecule |
Ago-PAM Agonist |
L-glutamic acid | small-molecule | No | No | Seven AB, Barros-Alvarez X, de Lapeyriere M, Papasergi-Scott MM, Robertson MJ, Zhang C, Nwokonko RM, Gao Y, Meyerowitz JG, Rocher JP, Schelshorn D, Kobilka BK, Mathiesen JM, Skiniotis G | 10.1038/S41586-021-03680-3 | 2021-07-07 | Yes | |
ACM1 | M1 | Acetylcholine (muscarinic) | A | Human | X-ray | 6ZFZ | 6ZFZ_refined | 2.2 | A | Inactive | 2 | 62 | - | - | - | - | T4-Lysozyme | - |
CHEMBL3354065
|
small-molecule | Agonist | acetylcholine | small-molecule | No | No | Brown AJH, Bradley SJ, Marshall FH, Brown GA, Bennett KA, Brown J, Cansfield JE, Cross DM, de Graaf C, Hudson BD, Dwomoh L, Dias JM, Errey JC, Hurrell E, Liptrot J, Mattedi G, Molloy C, Nathan PJ, Okrasa K, Osborne G, Patel JC, Pickworth M, Robertson N, Shahabi S, Bundgaard C, Phillips K, Broad LM, Goonawardena AV, Morairty SR, Browning M, Perini F, Dawson GR, Deakin JFW, Smith RT, Sexton PM, Warneck J, Vinson M, Tasker T, Tehan BG, Teobald B, Christopoulos A, Langmead CJ, Jazayeri A, Cooke RM, Rucktooa P, Congreve MS, Weir M, Tobin AB | 10.1016/J.CELL.2021.11.001 | 2021-10-06 | Yes | |
MRGX2 | MRGPRX2 | A orphans | A | Human | Cryo-EM | 7S8O | - | 2.6 | R | Active | 100 | 78 | Gi/o | αi1 | - | 62 | BRIL | scFv16 |
(R)-ZINC-3573
|
small-molecule | Agonist | PAMP-20 | peptide | No | No | Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL | 10.1038/S41586-021-04126-6 | 2021-11-17 | Yes | |
GP139 | GPR139 | A orphans | A | Human | Cryo-EM | 7VUG | 7VUG_refined | 3.2 | R | Active | 100 | 80 | Gi/o | αi1 | - | 62 | - | scFv16 |
JNJ-63533054
|
small-molecule | Agonist | L-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 | |
MSHR | MC1 | Melanocortin | A | Human | Cryo-EM | 7F4H | - | 2.7 | R | Active | 100 | 84 | Gs | αs | - | 59 | - | Nanobody-35 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 | 7TYW | - | 3.0 | R | Active | 100 | 78 | Gs | αs | - | 58 | - | Nanobody-35 |
calcitonin (salmon synthetic)
|
small-molecule | 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 | |
AGRF1 | ADGRF1 | ADGRF | B2 | Human | Cryo-EM | 7WU3 | - | 3.1 | R | Active | 100 | 31 | Gs | αs | Mini-Gs | 54 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Qu X, Qiu N, Wang M, Zhang B, Du J, Zhong Z, Xu W, Chu X, Ma L, Yi C, Han S, Shui W, Zhao Q, Wu B | 10.1038/S41586-022-04580-W | 2022-04-27 | Yes | |
FPR1 | FPR1 | Formylpeptide | A | Human | Cryo-EM | 7EUO | 7EUO_refined | 2.9 | R | Active | 100 | 84 | Gi/o | αi1 | - | 62 | - | scFv16 |
Peptide Agonist fMLF
|
peptide | Agonist | fMet-Leu-Phe, cathepsin G, annexin I, spinorphin | peptide | No | No | Chen G, Wang X, Liao Q, Ge Y, Jiao H, Chen Q, Liu Y, Lyu W, Zhu L, van Zundert GCP, Robertson MJ, Skiniotis G, Du Y, Hu H, Ye RD | 10.1038/S41467-022-32822-Y | 2022-05-25 | Yes | |
HRH2 | H2 | Histamine | A | Human | Cryo-EM | 7UL3 | 7UL3_refined | 3.0 | A | Inactive | 6 | 75 | - | - | - | - | - | Nanobody-6M NabFab HC NabFab LC |
famotidine
|
small-molecule | Antagonist | histamine | small-molecule | No | No | Robertson MJ, Papasergi-Scott MM, He F, Seven AB, Meyerowitz JG, Panova O, Peroto MC, Che T, Skiniotis G | 10.1038/S41594-022-00859-8 | 2022-06-29 | Yes | |
5HT5A | 5-HT5A | 5-Hydroxytryptamine | A | Human | Cryo-EM | 7UM6 | - | 2.8 | A | Active | 100 | 72 | Gi/o | αo | Mini-Go | 60 | - | scFv16 |
lisuride
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | No | No | Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL | 10.1038/S41594-022-00796-6 | 2022-07-20 | Yes | |
ACKR3 | ACKR3 | Chemokine | A | Human | Cryo-EM | 7SK7 | - | 3.3 | A | Active | 97 | 74 | - | - | - | - | - | CID25 Fab light chain CID25 Fab heavy chain anti-Fab Nanobody |
Stromal cell-derived factor 1
(1R)-4-[7-(3-carboxypropoxy)-6-methylquinolin-8-yl]-1-{[2-(4-hydroxypiperidin-1-yl)-1,3-thiazol-4-yl]methyl}-1,4-diazepan-1-ium |
peptide small-molecule |
Agonist Agonist (partial) |
CXCL11, CXCL12α | peptide | No | No | Yen YC, Schafer CT, Gustavsson M, Eberle SA, Dominik PK, Deneka D, Zhang P, Schall TJ, Kossiakoff AA, Tesmer JJG, Handel TM | 10.1126/SCIADV.ABN8063 | 2022-07-27 | Yes | |
ACM3 | M3 | Acetylcholine (muscarinic) | A | Human | Cryo-EM | 8E9Z | - | 2.7 | A | Active | 100 | 47 | Gq/11 | αq | Mini-Gq | 57 | - | scFv16 |
iperoxo
|
small-molecule | Agonist | acetylcholine | small-molecule | No | No | Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL | 10.1038/S41586-022-05489-0 | 2022-11-30 | Yes | |
RL3R2 | RXFP4 | Relaxin family peptide | A | Human | Cryo-EM | 7YK6 | 7YK6_refined | 3.0 | R | Active | 100 | 76 | Gi/o | αi2 | - | 59 | - | scFv16 |
CHEMBL4522365
|
small-molecule | Agonist | INSL5, relaxin-3 (B chain), relaxin-3 | peptide | No | No | Chen Y, Zhou Q, Wang J, Xu Y, Wang Y, Yan J, Wang Y, Zhu Q, Zhao F, Li C, Chen CW, Cai X, Bathgate RAD, Shen C, Eric Xu H, Yang D, Liu H, Wang MW | 10.1038/S41467-023-36182-Z | 2023-03-01 | Yes | |
AA2AR | A2A | Adenosine | A | Human | MicroED | 8FYN | 8FYN_refined | 2.0 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
ZM-241385
|
small-molecule | Antagonist | adenosine | small-molecule | No | No | Martynowycz MW, Shiriaeva A, Clabbers MTB, Nicolas WJ, Weaver SJ, Hattne J, Gonen T | 10.1038/S41467-023-36733-4 | 2023-03-08 | Yes | |
FFAR4 | FFA4 | Free fatty acid | A | Human | Cryo-EM | 8ID8 | - | 3.0 | R | Active | 100 | 81 | Gi/o | αi1 | - | 64 | - | scFv16 |
TUG-891
|
small-molecule | Agonist | 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 | |
AGRF1 | ADGRF1 | ADGRF | B2 | Human | Cryo-EM | 8G2Y | - | 3.4 | R | Active | 100 | 28 | Gq/11 | αq | Gs-mini-Gq chimera | 52 | - | Nanobody-35 |
[1-Myristoyl-glycerol-3-YL]phosphonylcholine
|
small-molecule | Agonist | - | - | No | No | Jones DTD, Dates AN, Rawson SD, Burruss MM, Lipper CH, Blacklow SC | 10.1038/S41467-023-38083-7 | 2023-05-10 | Yes | |
SSR2 | SST2 | Somatostatin | A | Human | Cryo-EM | 7YAE | 7YAE_refined | 3.4 | E | Active | 100 | 76 | Gi/o | αi1 | - | 64 | - | scFv16 |
Octreotide
|
peptide | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | No | No | Zhao J, Fu H, Yu J, Hong W, Tian X, Qi J, Sun S, Zhao C, Wu C, Xu Z, Cheng L, Chai R, Yan W, Wei X, Shao Z | 10.1038/S41467-023-36673-Z | 2023-04-19 | Yes | |
P2RY1 | P2Y1 | P2Y | A | Human | Cryo-EM | 7XXH | 7XXH_refined | 2.9 | R | Active | 100 | 81 | Gq/11 | α11 | - | 63 | - | scFv16 |
2MeSADP
|
small-molecule | Agonist | ADP, ATP | small-molecule | No | No | - | - | 2023-06-07 | Yes | |
CALCR | CT | Calcitonin | B1 | Human | Cryo-EM | 8F0J | - | 2.0 | R | Active | 100 | 78 | Gs | αs | - | 58 | - | Nanobody-35 |
Pramlintide analogue San45
|
peptide | Agonist | adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), 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 | 8JD2 | - | 2.8 | 2 | Active | - | 86 | - | - | - | - | - | - |
L-glutamic acid
|
small-molecule | Agonist | L-glutamic acid | small-molecule | No | No | Wang X, Wang M, Xu T, Feng Y, Shao Q, Han S, Chu X, Xu Y, Lin S, Zhao Q, Wu B | 10.1038/S41422-023-00830-2 | 2023-06-21 | Yes | |
PE2R4 | EP4 | Prostanoid | A | Human | Cryo-EM | 8GDB | 8GDB_refined | 3.1 | R | Active | 100 | 58 | Gs | αs | - | 59 | - | - |
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 | |
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 | |
NTR1 | NTS1 | Neurotensin | A | Rat | X-ray | 4GRV | 4GRV_refined | 2.8 | A | Active | 82 | 69 | - | - | - | - | T4-Lysozyme | - |
JMV431
|
peptide | Agonist | neurotensin, neuromedin N | peptide | No | No | White JF, Noinaj N, Shibata Y, Love J, Kloss B, Xu F, Gvozdenovic-Jeremic J, Shah P, Shiloach J, Tate CG, Grisshammer R | 10.1038/NATURE11558 | 2012-10-17 | Yes | |
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 | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 5D5A | 5D5A_refined | 2.5 | A | Inactive | 0 | 68 | - | - | - | - | T4-Lysozyme | - |
Carazolol
|
small-molecule | Inverse agonist | L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline | small-molecule | No | No | Huang CY, Olieric V, Ma P, Howe N, Vogeley L, Liu X, Warshamanage R, Weinert T, Panepucci E, Kobilka B, Diederichs K, Wang M, Caffrey M | 10.1107/S2059798315021683 | 2016-01-13 | Yes | |
CCR2 | CCR2 | Chemokine | A | Human | X-ray | 5T1A | 5T1A_refined | 2.8 | A | Inactive | 19 | 76 | - | - | - | - | T4-Lysozyme | - |
CCR2-RA-[R]
BMS-681 |
small-molecule small-molecule |
Allosteric antagonist Antagonist |
CCL8, CCL13, CCL7, CCL2, CCL11, CCL24, CCL16, CCL26 | peptide | No | No | Zheng Y, Qin L, Zacarias NV, de Vries H, Han GW, Gustavsson M, Dabros M, Zhao C, Cherney RJ, Carter P, Stamos D, Abagyan R, Cherezov V, Stevens RC, IJzerman AP, Heitman LH, Tebben A, Kufareva I, Handel TM | 10.1038/NATURE20605 | 2016-12-14 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5MZP | 5MZP_refined | 2.1 | A | Inactive | 0 | 71 | - | - | - | - | BRIL | - |
caffeine
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | Cheng RKY, Segala E, Robertson N, Deflorian F, Dore AS, Errey JC, Fiez-Vandal C, Marshall FH, Cooke RM | 10.1016/j.str.2017.06.012 | 2017-07-26 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5OLV | 5OLV_refined | 2.0 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
CHEMBL1671936
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | Rucktooa P, Cheng RKY, Segala E, Geng T, Errey JC, Brown GA, Cooke RM, Marshall FH, Dore AS | 10.1038/S41598-017-18570-W | 2018-01-17 | Yes | |
C5AR1 | C5a1 | Complement peptide | A | Human | X-ray | 6C1R | 6C1R_refined | 2.2 | B | Inactive | 8 | 83 | - | - | - | - | BRIL | - |
PMX53
avacopan |
peptide small-molecule |
Antagonist NAM |
ribosomal protein S19, C5a, C5a des-Arg, C3a | peptide | No | No | - | - | 2018-05-30 | Yes | |
PTH1R | PTH1 | Parathyroid hormone | B1 | Human | X-ray | 6FJ3 | - | 2.5 | A | Inactive | 0 | 62 | - | - | - | - | GlgA glycogen synthase | - |
ePTH
|
peptide | Agonist (partial) | TIP39, PTHrP-(1-36), PTHrP, PTH | peptide | No | No | Ehrenmann J, Schoppe J, Klenk C, Rappas M, Kummer L, Dore AS, Pluckthun A | 10.1038/S41594-018-0151-4 | 2018-11-21 | Yes | |
SMO | SMO | Frizzled | F | Mouse | X-ray | 6O3C | 6O3C_refined | 2.8 | A | Active | 95 | 61 | - | - | - | - | - | Nanobody-Smo8 |
SAG21k
|
small-molecule | Agonist | - | - | No | No | Deshpande I, Liang J, Hedeen D, Roberts KJ, Zhang Y, Ha B, Latorraca NR, Faust B, Dror RO, Beachy PA, Myers BR, Manglik A | 10.1038/S41586-019-1355-4 | 2019-07-03 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 6PS6 | 6PS6_refined | 2.7 | A | Inactive | 0 | 68 | - | - | - | - | T4-Lysozyme | - |
timolol
|
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 | |
APJ | apelin | Apelin | A | Human | X-ray | 6KNM | 6KNM_refined | 3.2 | B | Inactive | 6 | 78 | - | - | - | - | Rubredoxin | - |
Single domain antibody JN241
|
protein | Agonist | Elabela/Toddler-21, apelin-17, [Pyr1]apelin-13, Elabela/Toddler-11, Elabela/Toddler-32, apelin-13, apelin-36, apelin receptor early endogenous ligand | peptide | No | No | Ma Y, Ding Y, Song X, Ma X, Li X, Zhang N, Song Y, Sun Y, Shen Y, Zhong W, Hu LA, Ma Y, Zhang MY | 10.1126/SCIADV.AAX7379 | 2020-01-29 | Yes | |
CXCR2 | CXCR2 | Chemokine | A | Human | Cryo-EM | 6LFO | 6LFO_refined | 3.4 | R | Active | 100 | 85 | Gi/o | αi1 | - | 65 | - | scFv16 |
Interleukin-8
|
protein | Agonist | 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 | 7DTT | 7DTT_refined | 3.8 | A | Active | - | 72 | - | - | - | - | - | - |
Calcium
|
small-molecule | Agonist | 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 | 7M3G | 7M3G_refined | 2.5 | A | Active | - | 76 | - | - | - | - | - | - |
Calcium
evocalcet L-tryptophan |
small-molecule small-molecule small-molecule |
Agonist PAM 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 | |
CASR | CaS | Calcium-sensing | C | Human | Cryo-EM | 7E6T | 7E6T_refined | 3.0 | A | Active | - | 74 | - | - | - | - | - | - |
Calcium
Cyclomethyltryptophan |
small-molecule small-molecule |
Agonist PAM |
Mg2+, L-tryptophan, spermine, Ca2+ | small-molecule | No | No | Chen X, Wang L, Cui Q, Ding Z, Han L, Kou Y, Zhang W, Wang H, Jia X, Dai M, Shi Z, Li Y, Li X, Geng Y | 10.7554/ELIFE.68578 | 2021-09-22 | Yes | |
CNR1 | CB1 | Cannabinoid | A | Human | X-ray | 7V3Z | 7V3Z_refined | 3.3 | A | Active | 96 | 60 | - | - | - | - | Flavodoxin | - |
CP55940
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | No | No | Wang X, Liu D, Shen L, Li F, Li Y, Yang L, Xu T, Tao H, Yao D, Wu L, Hirata K, Bohn LM, Makriyannis A, Liu X, Hua T, Liu ZJ, Wang J | 10.1021/JACS.1C06847 | 2021-11-24 | Yes | |
NK1R | NK1 | Tachykinin | A | Human | Cryo-EM | 7P00 | - | 2.7 | R | Active | 100 | 71 | Gq/11 | αq | Gq-Gs-Gi1 chimera | 59 | - | scFv16 |
substance P
|
peptide | Agonist | neuropeptide-γ, neurokinin A, neuropeptide K, neurokinin B, hemokinin 1, substance P | peptide | No | No | Thom C, Ehrenmann J, Vacca S, Waltenspuhl Y, Schoppe J, Medalia O, Pluckthun A | 10.1126/SCIADV.ABK2872 | 2021-12-15 | Yes | |
S1PR1 | S1P1 | Lysophospholipid (S1P) | A | Human | Cryo-EM | 7EW0 | 7EW0_refined | 3.4 | D | Active | 100 | 71 | Gi/o | αi1 | - | 64 | - | scFv16 |
ozanimod
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | No | No | Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z | 10.1038/S41422-021-00566-X | 2021-09-29 | Yes | |
S1PR1 | S1P1 | Lysophospholipid (S1P) | A | Human | Cryo-EM | 7TD4 | - | 2.6 | R | Active | 100 | 76 | Gi/o | αi1 | - | 63 | - | - |
siponimod
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | No | No | Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY | 10.1038/S41467-022-28417-2 | 2022-02-09 | Yes | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 7VBI | - | 3.0 | R | Active | 100 | 83 | Gs | αs | Mini-Gs | 58 | - | - |
tirzepatide
|
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 | 2022-03-02 | Yes | |
ADRB1 | β1 | Adrenoceptors | A | Wild turkey | Cryo-EM | 7S0F | - | 3.0 | R | Active | 100 | 56 | Gi/o | αi1 | - | 63 | - | - |
LEVISOPRENALINE
|
small-molecule | Agonist | - | - | No | No | Alegre KO, Paknejad N, Su M, Lou JS, Huang J, Jordan KD, Eng ET, Meyerson JR, Hite RK, Huang XY | 10.1038/S41594-021-00679-2 | 2021-11-17 | Yes | |
DRD1 | D1 | Dopamine | A | Human | Cryo-EM | 7F1O | - | 3.1 | F | Active | 100 | 62 | Gs | αs | - | 60 | - | Nanobody-35 |
dopamine
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, 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 | tryptamine, 5-hydroxytryptamine | small-molecule | No | No | Kaplan AL, Confair DN, Kim K, Barros-Alvarez X, Rodriguiz RM, Yang Y, Kweon OS, Che T, McCorvy JD, Kamber DN, Phelan JP, Martins LC, Pogorelov VM, DiBerto JF, Slocum ST, Huang XP, Kumar JM, Robertson MJ, Panova O, Seven AB, Wetsel AQ, Wetsel WC, Irwin JJ, Skiniotis G, Shoichet BK, Roth BL, Ellman JA | 10.1038/S41586-022-05258-Z | 2022-07-06 | Yes | |
CX3C1 | CX3CR1 | Chemokine | A | Human | Cryo-EM | 7XBW | 7XBW_refined | 2.8 | R | Active | 19 | 81 | Gi/o | αi1 | - | 61 | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | CX3CL1 | peptide | No | No | Lu M, Zhao W, Han S, Lin X, Xu T, Tan Q, Wang M, Yi C, Chu X, Yang W, Zhu Y, Wu B, Zhao Q | 10.1126/SCIADV.ABN8048 | 2022-07-13 | Yes | |
SSR4 | SST4 | Somatostatin | A | Human | Cryo-EM | 7XMS | - | 2.9 | R | Active | 100 | 71 | Gi/o | αi1 | - | 63 | - | scFv16 |
SOMATOSTATIN
|
protein | 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 | |
SMO | SMO | Frizzled | F | Mouse | Cryo-EM | 8CXO | 8CXO_refined | 3.7 | A | Inactive | 15 | 43 | - | - | - | - | GlgA glycogen synthase | - |
Cholesterol
|
small-molecule | Agonist | - | - | No | No | Zhang K, Wu H, Hoppe N, Manglik A, Cheng Y | 10.1038/S41467-022-32125-2 | 2022-08-03 | Yes | |
OPRM | μ | Opioid | A | Mouse | Cryo-EM | 7T2G | - | 2.5 | R | Active | 100 | 70 | Gi/o | αi1 | - | 62 | BRIL | - |
CHEMBL58362
|
small-molecule | Agonist | - | - | No | No | Qu Q, Huang W, Aydin D, Paggi JM, Seven AB, Wang H, Chakraborty S, Che T, DiBerto JF, Robertson MJ, Inoue A, Suomivuori CM, Roth BL, Majumdar S, Dror RO, Kobilka BK, Skiniotis G | 10.1038/S41589-022-01208-Y | 2022-12-07 | Yes | |
AGRL3 | ADGRL3 | ADGRL | B2 | Mouse | Cryo-EM | 7WY8 | - | 2.8 | R | Active | 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 | |
LPAR1 | LPA1 | Lysophospholipid (LPA) | A | Human | Cryo-EM | 7YU6 | 7YU6_refined | 3.5 | R | Active | 100 | 80 | Gi/o | αi1 | - | 63 | - | scFv16 |
[(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate
|
small-molecule | Agonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | No | No | Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O | 10.1038/S41467-022-33121-2 | 2022-10-05 | Yes | |
OPRK | κ | Opioid | A | Human | Cryo-EM | 8F7W | 8F7W_refined | 3.2 | R | Active | 100 | 75 | Gi/o | αi1 | - | 64 | - | scFv16 |
dynorphin A-(1-8)
|
peptide | Agonist | [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 | Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y, Roth BL, Xu HE | 10.1016/J.CELL.2022.12.026 | 2022-12-14 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 8A6C | 8A6C_refined | 1.8 | A | Inactive | 24 | 87 | - | - | - | - | - | - |
Retinal (11-cis)
|
small-molecule | Agonist | - | - | No | No | Gruhl T, Weinert T, Rodrigues MJ, Milne CJ, Ortolani G, Nass K, Nango E, Sen S, Johnson PJM, Cirelli C, Furrer A, Mous S, Skopintsev P, James D, Dworkowski F, Bath P, Kekilli D, Ozerov D, Tanaka R, Glover H, Bacellar C, Brunle S, Casadei CM, Diethelm AD, Gashi D, Gotthard G, Guixa-Gonzalez R, Joti Y, Kabanova V, Knopp G, Lesca E, Ma P, Martiel I, Muhle J, Owada S, Pamula F, Sarabi D, Tejero O, Tsai CJ, Varma N, Wach A, Boutet S, Tono K, Nogly P, Deupi X, Iwata S, Neutze R, Standfuss J, Schertler G, Panneels V | 10.1038/S41586-023-05863-6 | 2023-03-29 | Yes | |
AA2BR | A2B | Adenosine | A | Human | Cryo-EM | 8HDO | - | 2.9 | R | Active | 100 | 83 | Gs | αs | Mini-Gs | 59 | - | Nanobody-35 |
BAY 60-6583
|
small-molecule | Agonist | adenosine | small-molecule | No | No | Cai H, Xu Y, Guo S, He X, Sun J, Li X, Li C, Yin W, Cheng X, Jiang H, Xu HE, Xie X, Jiang Y | 10.1038/S41421-022-00503-1 | 2023-01-18 | Yes | |
GRPR | BB2 | Bombesin | A | Human | X-ray | 7W41 | 7W41_refined | 3.0 | A | Inactive | 6 | 75 | - | - | - | - | GlgA glycogen synthase | - |
PD 176252
|
small-molecule | Antagonist | neuromedin B, gastrin releasing peptide(14-27) (human), GRP-(18-27), gastrin-releasing peptide, neuromedin C | peptide | No | No | Peng S, Zhan Y, Zhang D, Ren L, Chen A, Chen ZF, Zhang H | 10.1073/PNAS.2216230120 | 2023-02-22 | Yes | |
GP174 | GPR174 | A orphans | A | Human | Cryo-EM | 7XV3 | 7XV3_refined | 2.8 | R | Active | 100 | 87 | Gs | αs | - | 59 | - | - |
(2~{S})-2-$l^{4}-azanyl-3-[[(2~{R})-3-octadecanoyloxy-2-oxidanyl-propoxy]-oxidanyl-oxidanylidene-$l^{6}-phosphanyl]oxy-propanoic acid
|
small-molecule | Agonist | lysophosphatidylserine | small-molecule | No | No | Liang J, Inoue A, Ikuta T, Xia R, Wang N, Kawakami K, Xu Z, Qian Y, Zhu X, Zhang A, Guo C, Huang Z, He Y | 10.1038/S41467-023-36575-0 | 2023-02-15 | Yes | |
OPRK | κ | Opioid | A | Human | Cryo-EM | 8DZS | - | 2.7 | A | Active | 100 | 71 | Gi/o | αz | - | 59 | - | 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 | |
ACM4 | M4 | Acetylcholine (muscarinic) | A | Human | Cryo-EM | 7TRP | - | 2.4 | R | Active | 100 | 56 | Gi/o | αi1 | - | 64 | - | scFv16 |
iperoxo
LY2033298 |
small-molecule small-molecule |
Agonist PAM |
acetylcholine | small-molecule | No | No | - | - | 2023-05-17 | Yes | |
NMBR | BB1 | Bombesin | A | Human | Cryo-EM | 8H0P | - | 3.2 | R | Active | 100 | 75 | Gq/11 | αq | - | 57 | - | scFv16 |
NMB30
|
peptide | Agonist | neuromedin B, gastrin releasing peptide(14-27) (human), GRP-(18-27), gastrin-releasing peptide | peptide | No | No | Li C, Xu Y, Liu H, Cai H, Jiang Y, Xu HE, Yin W | 10.1038/S41422-022-00743-6 | 2023-08-09 | Yes | |
GRM2 | mGlu2 | Metabotropic glutamate | C | Human | Cryo-EM | 8JCV | - | 3.4 | 2 | Inactive | - | 88 | - | - | - | - | - | - |
LY341495
|
small-molecule | Antagonist | L-glutamic acid | small-molecule | No | No | Wang X, Wang M, Xu T, Feng Y, Shao Q, Han S, Chu X, Xu Y, Lin S, Zhao Q, Wu B | 10.1038/S41422-023-00830-2 | 2023-06-21 | Yes | |
HRH4 | H4 | Histamine | A | Human | Cryo-EM | 7YFC | - | 3.0 | R | Active | 100 | 67 | Gq/11 | αq | - | 62 | - | scFv16 Nanobody-35 |
histamine
|
small-molecule | Agonist | histamine, CCL16 | small-molecule | No | No | Im D, Kishikawa JI, Shiimura Y, Hisano H, Ito A, Fujita-Fujiharu Y, Sugita Y, Noda T, Kato T, Asada H, Iwata S | 10.1038/S41467-023-42260-Z | 2023-10-25 | Yes | |
GPR21 | GPR21 | A orphans | A | Human | Cryo-EM | 8HJ1 | 8HJ1_refined | 3.3 | R | Active | 100 | 81 | Gs | αs | - | 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 | 2023-12-27 | Yes | |
C3AR | C3a | Complement peptide | A | Human | Cryo-EM | 8I9S | 8I9S_refined | 3.3 | C | Active | 100 | 57 | Gi/o | αo | - | 59 | - | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | 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 | |
C3AR | C3a | Complement peptide | A | Human | Cryo-EM | 8J6D | 8J6D_refined | 3.1 | C | Active | 100 | 58 | Gi/o | αo | - | 59 | - | scFv16 |
EP141 peptide agonist
|
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 | |
5HT1A | 5-HT1A | 5-Hydroxytryptamine | A | Human | Cryo-EM | 8JSP | - | 3.7 | R | Active | 100 | 68 | Gi/o | αi1 | - | 61 | - | scFv16 |
ulotaront
|
small-molecule | Agonist | 5-hydroxytryptamine | 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 | |
TAAR1 | TA1 | Trace amine | A | Human | Cryo-EM | 8W89 | - | 3.0 | R | Active | 100 | 84 | Gs | αs | - | 60 | - | Nanobody-35 |
2-Phenylethanaminium
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, dopamine | small-molecule | No | No | Liu H, Zheng Y, Wang Y, Wang Y, He X, Xu P, Huang S, Yuan Q, Zhang X, Wang L, Jiang K, Chen H, Li Z, Liu W, Wang S, Xu HE, Xu F | 10.1038/S41586-023-06775-1 | 2023-11-22 | Yes | |
GPR34 | GPR34 | A orphans | A | Human | Cryo-EM | 8XBH | 8XBH_refined | 2.8 | R | Active | 100 | 78 | Gi/o | αi1 | - | 62 | - | scFv16 |
CHEMBL4758243
|
small-molecule | Agonist | lysophosphatidylserine | small-molecule | No | No | - | - | 2023-12-27 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 4GBR | 4GBR_refined | 4.0 | A | Inactive | 0 | 69 | - | - | - | - | T4-Lysozyme | - |
Carazolol
|
small-molecule | Inverse agonist | L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline | small-molecule | No | No | Zou Y, Weis WI, Kobilka BK | 10.1371/JOURNAL.PONE.0046039 | 2012-10-24 | Yes | |
FFAR1 | FFA1 | Free fatty acid | A | Human | X-ray | 4PHU | - | 2.3 | A | Active | 59 | 90 | - | - | - | - | T4-Lysozyme | - |
fasiglifam
|
small-molecule | Allosteric agonist | myristic acid, oleic acid, α-linolenic acid, docosahexaenoic acid | small-molecule | No | No | Srivastava A, Yano J, Hirozane Y, Kefala G, Gruswitz F, Snell G, Lane W, Ivetac A, Aertgeerts K, Nguyen J, Jennings A, Okada K | 10.1038/NATURE13494 | 2014-07-16 | Yes | |
OPRX | NOP | Opioid | A | Human | X-ray | 5DHG | 5DHG_refined | 3.0 | A | Inactive | 6 | 76 | - | - | - | - | BRIL | - |
CHEMBL1783826
|
small-molecule | Antagonist | nociceptin/orphanin FQ | peptide | No | No | Miller RL, Thompson AA, Trapella C, Guerrini R, Malfacini D, Patel N, Han GW, Cherezov V, Calo G, Katritch V, Stevens RC | 10.1016/J.STR.2015.07.024 | 2015-10-21 | Yes | |
CNR1 | CB1 | Cannabinoid | A | Human | X-ray | 5U09 | 5U09_refined | 2.6 | A | Inactive | 13 | 60 | - | - | - | - | Glycogen synthase | - |
taranabant
|
small-molecule | Inverse agonist | 2-arachidonoylglycerol, anandamide | small-molecule | No | No | Shao Z, Yin J, Chapman K, Grzemska M, Clark L, Wang J, Rosenbaum DM | 10.1038/NATURE20613 | 2016-12-07 | Yes | |
FFAR1 | FFA1 | Free fatty acid | A | Human | X-ray | 5TZY | - | 3.2 | A | Active | 59 | 91 | - | - | - | - | T4-Lysozyme | - |
MK-8666
(2S,3R)-3-Cyclopropyl-3-[(2R)-2-[1-[(1S)-1-[5-fluoro-2-(trifluoromethoxy)phenyl]ethyl]piperidin-4-yl]-3,4-dihydro-2H-chromen-7-yl]-2-methylpropanoic acid |
small-molecule small-molecule |
Agonist PAM |
myristic acid, oleic acid, α-linolenic acid, docosahexaenoic acid | small-molecule | No | No | Lu J, Byrne N, Wang J, Bricogne G, Brown FK, Chobanian HR, Colletti SL, Di Salvo J, Thomas-Fowlkes B, Guo Y, Hall DL, Hadix J, Hastings NB, Hermes JD, Ho T, Howard AD, Josien H, Kornienko M, Lumb KJ, Miller MW, Patel SB, Pio B, Plummer CW, Sherborne BS, Sheth P, Souza S, Tummala S, Vonrhein C, Webb M, Allen SJ, Johnston JM, Weinglass AB, Sharma S, Soisson SM | 10.1038/NSMB.3417 | 2017-06-07 | Yes | |
OPRK | κ | Opioid | A | Human | X-ray | 6B73 | 6B73_refined | 3.1 | A | Active | 100 | 73 | - | - | - | - | BRIL | Nanobody |
MP1104
|
small-molecule | Agonist | [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 | Che T, Majumdar S, Zaidi SA, Ondachi P, McCorvy JD, Wang S, Mosier PD, Uprety R, Vardy E, Krumm BE, Han GW, Lee MY, Pardon E, Steyaert J, Huang XP, Strachan RT, Tribo AR, Pasternak GW, Carroll FI, Stevens RC, Cherezov V, Katritch V, Wacker D, Roth BL | 10.1016/J.CELL.2017.12.011 | 2018-01-17 | Yes | |
5HT2B | 5-HT2B | 5-Hydroxytryptamine | A | Human | X-ray | 6DRX | - | 3.1 | A | Active | 59 | 59 | - | - | - | - | BRIL | - |
lisuride
|
small-molecule | Antagonist | 5-hydroxytryptamine | small-molecule | No | No | McCorvy JD, Wacker D, Wang S, Agegnehu B, Liu J, Lansu K, Tribo AR, Olsen RHJ, Che T, Jin J, Roth BL | 10.1038/s41594-018-0116-7 | 2018-08-29 | Yes | |
EDNRB | ETB | Endothelin | A | Human | X-ray | 6IGK | 6IGK_refined | 2.0 | A | Inactive | 4 | 70 | - | - | - | - | T4-Lysozyme | - |
endothelin-3
|
peptide | Agonist | endothelin-1, endothelin-2, endothelin-3 | peptide | No | No | Shihoya W, Izume T, Inoue A, Yamashita K, Kadji FMN, Hirata K, Aoki J, Nishizawa T, Nureki O | 10.1038/S41467-018-07094-0 | 2018-11-21 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 6N48 | 6N48_refined | 3.2 | A | Active | 99 | 70 | - | - | - | - | T4-Lysozyme | Camelid Antibody Fragment |
CHEMBL1615159
2-[[(3R)-4-(4-Tert-butylphenyl)-3-[[2-(4-methoxyphenyl)sulfanyl-5-[methyl(propan-2-yl)sulfamoyl]benzoyl]amino]butanoyl]amino]acetic acid |
small-molecule small-molecule |
Agonist PAM |
L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline | small-molecule | No | No | Liu X, Masoudi A, Kahsai AW, Huang LY, Pani B, Staus DP, Shim PJ, Hirata K, Simhal RK, Schwalb AM, Rambarat PK, Ahn S, Lefkowitz RJ, Kobilka B | 10.1126/SCIENCE.AAW8981 | 2019-06-26 | Yes | |
ADA2C | α2C | Adrenoceptors | A | Human | X-ray | 6KUW | 6KUW_refined | 2.8 | A | Inactive | 1 | 60 | - | - | - | - | GlgA glycogen synthase | - |
(8Ar,12aS,13aR)-12-ethylsulfonyl-3-methoxy-5,6,8,8a,9,10,11,12a,13,13a-decahydroisoquinolino[2,1-g][1,6]naphthyridine
|
small-molecule | Antagonist | (-)-adrenaline, (-)-noradrenaline | small-molecule | No | No | - | - | 2019-12-04 | Yes | |
CNR2 | CB2 | Cannabinoid | A | Human | Cryo-EM | 6KPF | 6KPF_refined | 2.9 | R | Active | 100 | 81 | Gi/o | αi1 | - | 62 | - | scFv16 |
AM12033
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | No | No | Hua T, Li X, Wu L, Iliopoulos-Tsoutsouvas C, Wang Y, Wu M, Shen L, Brust CA, Nikas SP, Song F, Song X, Yuan S, Sun Q, Wu Y, Jiang S, Grim TW, Benchama O, Stahl EL, Zvonok N, Zhao S, Bohn LM, Makriyannis A, Liu ZJ | 10.1016/J.CELL.2020.01.008 | 2020-02-12 | Yes | |
GABR2 | GABAB2 | GABAB | C | Human | Cryo-EM | 6UOA | - | 6.3 | B | Intermediate | - | 71 | - | - | - | - | - | - |
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 | 6WI9 | 6WI9_refined | 4.3 | R | Active | 100 | 84 | Gs | αs | - | 49 | - | Nanobody-35 |
SECRETIN
|
protein | Agonist | VIP, secretin | peptide | No | No | Dong M, Deganutti G, Piper SJ, Liang YL, Khoshouei M, Belousoff MJ, Harikumar KG, Reynolds CA, Glukhova A, Furness SGB, Christopoulos A, Danev R, Wootten D, Sexton PM, Miller LJ | 10.1038/S41467-020-17791-4 | 2020-08-12 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 6LPJ | 6LPJ_refined | 1.8 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
ZM-241385
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | Ihara K, Hato M, Nakane T, Yamashita K, Kimura-Someya T, Hosaka T, Ishizuka-Katsura Y, Tanaka R, Tanaka T, Sugahara M, Hirata K, Yamamoto M, Nureki O, Tono K, Nango E, Iwata S, Shirouzu M | 10.1038/S41598-020-76277-X | 2020-11-25 | Yes | |
NPY2R | Y2 | Neuropeptide Y | A | Human | X-ray | 7DDZ | 7DDZ_refined | 2.8 | A | Inactive | 0 | 76 | - | - | - | - | Flavodoxin | - |
CHEMBL1823578
|
small-molecule | Antagonist | pancreatic polypeptide, neuropeptide Y-(3-36), PYY-(3-36), neuropeptide Y, peptide YY | peptide | No | No | Tang T, Hartig C, Chen Q, Zhao W, Kaiser A, Zhang X, Zhang H, Qu H, Yi C, Ma L, Han S, Zhao Q, Beck-Sickinger AG, Wu B | 10.1038/S41467-021-21030-9 | 2021-01-27 | Yes | |
DRD3 | D3 | Dopamine | A | Human | Cryo-EM | 7CMU | - | 3.0 | R | Active | 100 | 68 | Gi/o | αi1 | - | 64 | BRIL | scFv16 |
pramipexole
|
small-molecule | Agonist | dopamine | small-molecule | No | No | Xu P, Huang S, Mao C, Krumm BE, Zhou XE, Tan Y, Huang XP, Liu Y, Shen DD, Jiang Y, Yu X, Jiang H, Melcher K, Roth BL, Cheng X, Zhang Y, Xu HE | 10.1016/J.MOLCEL.2021.01.003 | 2021-03-10 | Yes | |
CASR | CaS | Calcium-sensing | C | Human | Cryo-EM | 7DD7 | - | 3.2 | B | Active | - | 73 | - | - | - | - | - | - |
Calcium
evocalcet L-tryptophan |
small-molecule small-molecule small-molecule |
Agonist PAM PAM |
Mg2+, L-tryptophan, spermine, Ca2+ | small-molecule | No | No | Wen T, Wang Z, Chen X, Ren Y, Lu X, Xing Y, Lu J, Chang S, Zhang X, Shen Y, Yang X | 10.1126/SCIADV.ABG1483 | 2021-06-16 | Yes | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 7EVM | - | 2.5 | R | Active | 100 | 61 | Gs | αs | - | 60 | - | Nanobody-35 |
N-Tert-butyl-6,7-dichloroquinoxalin-2-amine
|
small-molecule | Ago-PAM | glucagon-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 | |
S1PR5 | S1P5 | Lysophospholipid (S1P) | A | Human | Cryo-EM | 7EW1 | 7EW1_refined | 3.4 | A | Active | 100 | 68 | Gi/o | αi1 | - | 64 | - | scFv16 |
siponimod
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | No | No | Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z | 10.1038/S41422-021-00566-X | 2021-09-29 | Yes | |
MC4R | MC4 | Melanocortin | A | Human | Cryo-EM | 7PIV | 7PIV_refined | 2.9 | R | Active | 100 | 78 | Gs | αs | - | 46 | - | Nanobody-35 |
afamelanotide
|
peptide | Agonist | β-MSH, α-MSH, agouti-related protein, γ-MSH, ACTH | peptide | No | No | Heyder NA, Kleinau G, Speck D, Schmidt A, Paisdzior S, Szczepek M, Bauer B, Koch A, Gallandi M, Kwiatkowski D, Burger J, Mielke T, Beck-Sickinger AG, Hildebrand PW, Spahn CMT, Hilger D, Schacherl M, Biebermann H, Hilal T, Kuhnen P, Kobilka BK, Scheerer P | 10.1038/S41422-021-00569-8 | 2021-11-17 | Yes | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 7S3I | - | 2.5 | R | Active | 100 | 57 | Gs | αs | - | 59 | - | Nanobody-35 |
exendin-4
|
peptide | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | No | No | Cary BP, Deganutti G, Zhao P, Truong TT, Piper SJ, Liu X, Belousoff MJ, Danev R, Sexton PM, Wootten D, Gellman SH | 10.1038/S41589-021-00945-W | 2022-01-05 | Yes | |
S1PR1 | S1P1 | Lysophospholipid (S1P) | A | Human | Cryo-EM | 7EVY | - | 3.0 | D | Active | 100 | 71 | Gi/o | αi1 | - | 64 | - | scFv16 |
siponimod
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | No | No | Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z | 10.1038/S41422-021-00566-X | 2021-09-29 | Yes | |
LPAR1 | LPA1 | Lysophospholipid (LPA) | A | Human | Cryo-EM | 7TD2 | - | 3.1 | R | Active | 100 | 80 | Gi/o | αi1 | - | 62 | - | - |
lysophosphatidic acid
|
small-molecule | Agonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | No | No | Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY | 10.1038/S41467-022-28417-2 | 2022-02-09 | Yes | |
FPR1 | FPR1 | Formylpeptide | A | Human | Cryo-EM | 7WVU | 7WVU_refined | 3.3 | R | Active | 100 | 85 | Gi/o | αi1 | - | 62 | - | - |
FME-LEU-PHE
|
peptide | Agonist | fMet-Leu-Phe, cathepsin G, annexin I, spinorphin | peptide | No | No | Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B | 10.1038/S41467-022-29361-X | 2022-04-13 | Yes | |
AGRG4 | ADGRG4 | ADGRG | B2 | Human | Cryo-EM | 7WUJ | - | 3.3 | E | Active | 100 | 9 | Gs | αs | Mini-Gs | 59 | - | scFv16 Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | - | - | 2022-04-27 | Yes | |
NPY4R | Y4 | Neuropeptide Y | A | Human | Cryo-EM | 7X9C | 7X9C_refined | 3.0 | R | Active | 100 | 81 | Gi/o | αi1 | - | 61 | - | - |
Pancreatic polypeptide
|
peptide | Agonist | peptide YY, neuropeptide Y, PYY-(3-36), pancreatic polypeptide | peptide | No | No | Tang T, Tan Q, Han S, Diemar A, Lobner K, Wang H, Schuss C, Behr V, Morl K, Wang M, Chu X, Yi C, Keller M, Kofoed J, Reedtz-Runge S, Kaiser A, Beck-Sickinger AG, Zhao Q, Wu B | 10.1126/SCIADV.ABM1232 | 2022-05-18 | Yes | |
APJ | apelin | Apelin | A | Human | Cryo-EM | 7W0L | 7W0L_refined | 3.6 | R | Active | 100 | 78 | Gi/o | αi1 | - | 64 | BRIL | scFv16 |
(1R,2S)-N-[4-(2,6-dimethoxyphenyl)-5-(6-methylpyridin-2-yl)-1,2,4-triazol-3-yl]-1-(5-methylpyrimidin-2-yl)-1-oxidanyl-propane-2-sulfonamide
|
small-molecule | Agonist | Elabela/Toddler-21, apelin-17, [Pyr1]apelin-13, Elabela/Toddler-11, Elabela/Toddler-32, apelin-13, apelin-36, 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 | |
ADRB1 | β1 | Adrenoceptors | A | Wild turkey | Cryo-EM | 8DCR | - | 2.6 | R | Active | 100 | 57 | Gs | αs | - | 51 | T4-Lysozyme | Nanobody-35 |
Dobutamine
|
small-molecule | Agonist | - | - | No | No | Su M, Paknejad N, Zhu L, Wang J, Do HN, Miao Y, Liu W, Hite RK, Huang XY | 10.1038/S41467-022-31823-1 | 2022-07-27 | Yes | |
PTH1R | PTH1 | Parathyroid hormone | B1 | Human | Cryo-EM | 7VVL | 7VVL_refined | 2.8 | R | Active | 100 | 58 | 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 | |
GP119 | GPR119 | GPR18, GPR55 and GPR119 | A | Human | Cryo-EM | 7WCM | 7WCM_refined | 2.3 | R | Active | 100 | 86 | Gs | αs | - | 60 | - | Nanobody-35 |
MBX-2982
|
small-molecule | Agonist | N-oleoylethanolamide, anandamide, N-palmitoylethanolamine, SEA | small-molecule | No | No | Qian Y, Wang J, Yang L, Liu Y, Wang L, Liu W, Lin Y, Yang H, Ma L, Ye S, Wu S, Qiao A | 10.1038/S41467-022-34696-6 | 2022-12-21 | Yes | |
T2R46 | TAS2R46 | Taste 2 | T | Human | Cryo-EM | 7XP5 | - | 3.1 | R | Active | - | 97 | Gi/o | αgust | - | 63 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Xu W, Wu L, Liu S, Liu X, Cao X, Zhou C, Zhang J, Fu Y, Guo Y, Wu Y, Tan Q, Wang L, Liu J, Jiang L, Fan Z, Pei Y, Yu J, Cheng J, Zhao S, Hao X, Liu ZJ, Hua T | 10.1126/SCIENCE.ABO1633 | 2022-10-12 | Yes | |
ACM3 | M3 | Acetylcholine (muscarinic) | A | Human | Cryo-EM | 8E9W | - | 2.7 | A | Active | 100 | 47 | Gq/11 | αq | Mini-Gq | 57 | - | scFv16 |
CHEMBL73538
|
small-molecule | Agonist | acetylcholine | small-molecule | No | No | Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL | 10.1038/S41586-022-05489-0 | 2022-11-30 | Yes | |
RL3R2 | RXFP4 | Relaxin family peptide | A | Human | Cryo-EM | 7YK7 | 7YK7_refined | 2.8 | R | Active | 100 | 75 | Gi/o | αi2 | - | 61 | - | scFv16 |
DC591053
|
small-molecule | Agonist | INSL5, relaxin-3 (B chain), relaxin-3 | peptide | No | No | Chen Y, Zhou Q, Wang J, Xu Y, Wang Y, Yan J, Wang Y, Zhu Q, Zhao F, Li C, Chen CW, Cai X, Bathgate RAD, Shen C, Eric Xu H, Yang D, Liu H, Wang MW | 10.1038/S41467-023-36182-Z | 2023-03-01 | Yes | |
FFAR4 | FFA4 | Free fatty acid | A | Human | Cryo-EM | 8G59 | 8G59_refined | 2.6 | R | Active | 100 | 78 | Gq/11 | αq | - | 61 | - | - |
TUG-891
|
small-molecule | Agonist | 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 | 2023-03-08 | Yes | |
ACM2 | M2 | Acetylcholine (muscarinic) | A | Human | Cryo-EM | 7T90 | 7T90_refined | 3.3 | A | Active | 100 | 59 | Gi/o | αo | - | 62 | - | scFv16 |
acetylcholine
|
small-molecule | Agonist | acetylcholine | small-molecule | No | No | - | - | 2023-01-25 | Yes | |
MRGX1 | MRGPRX1 | A orphans | A | Human | Cryo-EM | 8HJ5 | 8HJ5_refined | 3.0 | F | Active | 100 | 78 | Gq/11 | αq | - | 60 | BRIL | scFv16 Nanobody-35 |
compound 16 [PMID: 31498617]
|
small-molecule | Agonist | bovine adrenal medulla peptide 8-22 | peptide | No | No | - | - | 2023-05-31 | Yes | |
DRD5 | D5 | Dopamine | A | Human | Cryo-EM | 8IRV | 8IRV_refined | 3.1 | R | Active | 100 | 58 | Gs | αs | - | 60 | BRIL | - |
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 | 2023-06-07 | Yes | |
AGRE5 | ADGRE5 | ADGRE | B2 | Human | Cryo-EM | 7YDP | - | 3.1 | R | Active | 100 | 32 | Gs | αs | Mini-Gs | 59 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Wang N, Qian Y, Xia R, Zhu X, Xiong Y, Zhang A, Guo C, He Y | 10.1016/J.CHEMBIOL.2023.08.003 | 2023-07-12 | Yes | |
EDNRB | ETB | Endothelin | A | Human | Cryo-EM | 8IY5 | - | 2.8 | R | Active | 100 | 71 | Gi/o | αi1 | - | 62 | - | scFv16 |
ENDOTHELIN
|
protein | Agonist | endothelin-1, endothelin-2, endothelin-3 | peptide | No | No | Sano FK, Akasaka H, Shihoya W, Nureki O | 10.7554/ELIFE.85821 | 2023-08-16 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 8JWZ | - | 2.4 | A | Inactive | 0 | 71 | - | - | - | - | T4-Lysozyme | - |
AB928
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | - | - | 2023-08-16 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 8FD1 | - | 4.3 | A | Inactive | 24 | 88 | - | - | - | - | - | Nanobody-2 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | 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 | 8HNM | - | 2.9 | R | Active | 100 | 75 | Gi/o | αi1 | - | 62 | - | scFv16 |
CHEMBL2220409
|
small-molecule | Agonist | 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 | 8IJD | - | 3.3 | A | Active | 100 | 81 | Gi/o | αi1 | - | 61 | - | scFv16 |
MK 6892
|
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 | Human | Cryo-EM | 8JLN | - | 3.2 | R | Active | 100 | 84 | Gs | αs | - | 61 | BRIL | scFv16 |
CHEMBL1182312
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, 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 | |
CML1 | chemerin | Chemerin receptor | A | Human | Cryo-EM | 8SG1 | - | 2.9 | R | Active | 100 | 75 | Gi/o | αi1 | - | 61 | - | scFv16 |
chemerin C-terminal peptide
|
peptide | Agonist | 18R-HEPE, chemerin C-terminal peptide, EPA, resolvin E1, chemerin | peptide | No | No | Zhang X, Weiss T, Cheng MH, Chen S, Ambrosius CK, Czerniak AS, Li K, Feng M, Bahar I, Beck-Sickinger AG, Zhang C | 10.1371/JOURNAL.PBIO.3002188 | 2023-11-01 | Yes | |
CASR | CaS | Calcium-sensing | C | Human | Cryo-EM | 8WPU | - | 3.1 | A | Active | - | 74 | Gq/11 | αq | Gi2-mini-Gq chimera | 58 | - | scFv16 |
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 | |
PAR1 | PAR1 | Proteinase-activated | A | Human | X-ray | 3VW7 | - | 2.2 | A | Active | 59 | 66 | - | - | - | - | T4-Lysozyme | - |
vorapaxar
|
small-molecule | Antagonist | thrombin | peptide | No | No | Zhang C, Srinivasan Y, Arlow DH, Fung JJ, Palmer D, Zheng Y, Green HF, Pandey A, Dror RO, Shaw DE, Weis WI, Coughlin SR, Kobilka BK | 10.1038/NATURE11701 | 2012-12-12 | Yes | |
ADRB1 | β1 | Adrenoceptors | A | Wild turkey | X-ray | 4BVN | 4BVN_refined | 2.1 | A | Inactive | 0 | 60 | - | - | - | - | - | - |
(S)-Cyanopindolol
|
small-molecule | Antagonist | - | - | No | Yes | Miller-Gallacher JL, Nehme R, Warne T, Edwards PC, Schertler GF, Leslie AG, Tate CG | 10.1371/JOURNAL.PONE.0092727 | 2014-04-02 | Yes | |
LPAR1 | LPA1 | Lysophospholipid (LPA) | A | Human | X-ray | 4Z35 | 4Z35_refined | 2.9 | A | Inactive | 1 | 80 | - | - | - | - | BRIL | - |
ONO-9910539
|
small-molecule | Antagonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | No | No | Chrencik JE, Roth CB, Terakado M, Kurata H, Omi R, Kihara Y, Warshaviak D, Nakade S, Asmar-Rovira G, Mileni M, Mizuno H, Griffith MT, Rodgers C, Han GW, Velasquez J, Chun J, Stevens RC, Hanson MA | 10.1016/J.CELL.2015.06.002 | 2015-06-03 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5IUA | 5IUA_refined | 2.2 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
2-(Furan-2-yl)-5-N-[3-(4-phenylpiperazin-1-yl)propyl]-1H-[1,2,4]triazolo[1,5-a][1,3,5]triazin-8-ium-5,7-diamine
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | Segala E, Guo D, Cheng RK, Bortolato A, Deflorian F, Doré AS, Errey JC, Heitman LH, IJzerman AP, Marshall FH, Cooke RM. | 10.1021/acs.jmedchem.6b00653 | 2016-06-29 | Yes | |
AGTR2 | AT2 | Angiotensin | A | Human | X-ray | 5UNF | 5UNF_refined | 2.8 | A | Active | 99 | 79 | - | - | - | - | BRIL | - |
compound 1 [PMID: 28379944]
|
small-molecule | Antagonist | angiotensin-(1-7), angiotensin II, angiotensin III | peptide | No | No | Zhang H, Han GW, Batyuk A, Ishchenko A, White KL, Patel N, Sadybekov A, Zamlynny B, Rudd MT, Hollenstein K, Tolstikova A, White TA, Hunter MS, Weierstall U, Liu W, Babaoglu K, Moore EL, Katz RD, Shipman JM, Garcia-Calvo M, Sharma S, Sheth P, Soisson SM, Stevens RC, Katritch V, Cherezov V | 10.1038/NATURE22035 | 2017-04-05 | Yes | |
DRD4 | D4 | Dopamine | A | Human | X-ray | 5WIV | - | 2.1 | A | Inactive | 1 | 65 | - | - | - | - | BRIL | - |
[3H]NEMONAPRIDE
|
small-molecule | Antagonist | dopamine | small-molecule | No | Yes | Wang S, Wacker D, Levit A, Che T, Betz RM, McCorvy JD, Venkatakrishnan AJ, Huang XP, Dror RO, Shoichet BK, Roth BL | 10.1126/SCIENCE.AAN5468 | 2017-10-18 | Yes | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 6B3J | - | 3.3 | R | Active | 100 | 82 | Gs | αs | - | 49 | - | - |
Exendin-P5
|
peptide | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | No | No | Liang YL, Khoshouei M, Glukhova A, Furness SGB, Zhao P, Clydesdale L, Koole C, Truong TT, Thal DM, Lei S, Radjainia M, Danev R, Baumeister W, Wang MW, Miller LJ, Christopoulos A, Sexton PM, Wootten D | 10.1038/NATURE25773 | 2018-02-21 | Yes | |
5HT2A | 5-HT2A | 5-Hydroxytryptamine | A | Human | X-ray | 6A93 | 6A93_refined | 3.0 | A | Inactive | 1 | 60 | - | - | - | - | BRIL | - |
risperidone
|
small-molecule | Antagonist | tryptamine, 5-hydroxytryptamine | small-molecule | No | No | Kimura KT, Asada H, Inoue A, Kadji FMN, Im D, Mori C, Arakawa T, Hirata K, Nomura Y, Nomura N, Aoki J, Iwata S, Shimamura T | 10.1038/S41594-018-0180-Z | 2019-02-13 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | Cryo-EM | 6QNO | - | 4.4 | R | Active | 100 | 96 | Gi/o | αi1 | - | 60 | - | Fab antibody fragment light chain Fab antibody fragment heavy chain |
Retinal (all-trans)
|
small-molecule | Agonist | - | - | No | No | Tsai CJ, Marino J, Adaixo R, Pamula F, Muehle J, Maeda S, Flock T, Taylor NM, Mohammed I, Matile H, Dawson RJ, Deupi X, Stahlberg H, Schertler G | 10.7554/ELIFE.46041 | 2019-07-10 | Yes | |
OX1R | OX1 | Orexin | A | Human | X-ray | 6TQ9 | 6TQ9_refined | 2.7 | B | Inactive | 0 | 71 | - | - | - | - | - | - |
SB-408124
|
small-molecule | Antagonist | orexin-A, orexin-B | peptide | No | No | Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA. | 10.1021/acs.jmedchem.9b01787 | 2020-01-01 | Yes | |
PACR | PAC1 | VIP and PACAP | B1 | Human | Cryo-EM | 6M1H | - | 3.6 | A | Active | 100 | 73 | Gs | αs | - | 55 | - | Nanobody-35 |
maxadilan
|
peptide | Agonist | VIP, PHI, PHM, PHV, PACAP-27, 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 | |
GPBAR | GPBA | Bile acid | A | Human | Cryo-EM | 7CFM | - | 3.0 | R | Active | 100 | 83 | Gs | αs | - | 58 | - | Nanobody-35 |
CHEMBL2331646
|
small-molecule | Agonist | deoxycholic acid, cholic acid, chenodeoxycholic acid, lithocholic acid | small-molecule | No | No | Yang F, Mao C, Guo L, Lin J, Ming Q, Xiao P, Wu X, Shen Q, Guo S, Shen DD, Lu R, Zhang L, Huang S, Ping Y, Zhang C, Ma C, Zhang K, Liang X, Shen Y, Nan F, Yi F, Luca VC, Zhou J, Jiang C, Sun JP, Xie X, Yu X, Zhang Y | 10.1038/S41586-020-2569-1 | 2020-09-09 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 6LPL | 6LPL_refined | 2.0 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
ZM-241385
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | Ihara K, Hato M, Nakane T, Yamashita K, Kimura-Someya T, Hosaka T, Ishizuka-Katsura Y, Tanaka R, Tanaka T, Sugahara M, Hirata K, Yamamoto M, Nureki O, Tono K, Nango E, Iwata S, Shirouzu M | 10.1038/S41598-020-76277-X | 2020-11-25 | Yes | |
NTR1 | NTS1 | Neurotensin | A | Rat | X-ray | 6Z4Q | - | 2.9 | A | Inactive | 33 | 75 | - | - | - | - | DARPin D12 | - |
SR142948A
|
small-molecule | Inverse agonist | neurotensin, neuromedin N | peptide | No | No | Deluigi M, Klipp A, Klenk C, Merklinger L, Eberle SA, Morstein L, Heine P, Mittl PRE, Ernst P, Kamenecka TM, He Y, Vacca S, Egloff P, Honegger A, Pluckthun A | 10.1126/sciadv.abe5504 | 2021-02-10 | Yes | |
5HT1A | 5-HT1A | 5-Hydroxytryptamine | A | Human | Cryo-EM | 7E2Y | - | 3.0 | R | Active | 100 | 65 | Gi/o | αi1 | - | 62 | - | - |
5-hydroxytryptamine
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | No | No | Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen DD, Yen HY, Robinson CV, Harpsoe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE | 10.1038/S41586-021-03376-8 | 2021-04-14 | Yes | |
GRM2 | mGlu2 | Metabotropic glutamate | C | Human | X-ray | 7EPF | 7EPF_refined | 2.7 | A | Inactive | - | 28 | - | - | - | - | Flavodoxin | - |
(8~{R})-4-[2,4-Bis(fluoranyl)phenyl]-8-methyl-7-[(2-methylpyrazol-3-yl)methyl]-6,8-dihydro-5~{H}-1,7-naphthyridine-2-carboxamide
|
small-molecule | NAM | L-glutamic acid | small-molecule | No | No | Du J, Wang D, Fan H, Xu C, Tai L, Lin S, Han S, Tan Q, Wang X, Xu T, Zhang H, Chu X, Yi C, Liu P, Wang X, Zhou Y, Pin JP, Rondard P, Liu H, Liu J, Sun F, Wu B, Zhao Q | 10.1038/S41586-021-03641-W | 2021-06-23 | Yes | |
CCR5 | CCR5 | Chemokine | A | Human | Cryo-EM | 7F1R | - | 3.0 | R | Active | 100 | 79 | Gi/o | αi1 | - | 61 | - | - |
CCL5
|
peptide | Agonist | CCL14, CCL8, CCL13, CCL4, CCL7, CCL2, CCL5, CCL11, CCL3, CCL16 | peptide | No | No | - | - | 2021-07-14 | Yes | |
LSHR | LH | Glycoprotein hormone | A | Human | Cryo-EM | 7FIJ | 7FIJ_refined | 3.8 | R | Inactive | 6 | 80 | - | - | - | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | hCG, LH | peptide | No | No | Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE | 10.1038/S41586-021-03924-2 | 2021-09-29 | Yes | |
MRGX2 | MRGPRX2 | A orphans | A | Human | Cryo-EM | 7S8M | - | 2.5 | R | Active | 100 | 77 | Gi/o | αi1 | - | 62 | BRIL | scFv16 |
Cortistatin 14
|
peptide | Agonist | PAMP-20 | peptide | No | No | Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL | 10.1038/S41586-021-04126-6 | 2021-11-17 | Yes | |
GP139 | GPR139 | A orphans | A | Human | Cryo-EM | 7VUH | 7VUH_refined | 3.2 | R | Active | 100 | 80 | Gs | αs | - | 61 | - | Nanobody-35 |
JNJ-63533054
|
small-molecule | Agonist | L-phenylalanine, L-tryptophan | small-molecule | No | No | - | - | 2021-12-29 | Yes | |
CASR | CaS | Calcium-sensing | C | Human | Cryo-EM | 7SIM | 7SIM_refined | 2.7 | A | Active | - | 72 | - | - | - | - | - | - |
Cyclomethyltryptophan
|
small-molecule | Agonist | Mg2+, L-tryptophan, spermine, Ca2+ | small-molecule | No | No | Park J, Zuo H, Frangaj A, Fu Z, Yen LY, Zhang Z, Mosyak L, Slavkovich VN, Liu J, Ray KM, Cao B, Vallese F, Geng Y, Chen S, Grassucci R, Dandey VP, Tan YZ, Eng E, Lee Y, Kloss B, Liu Z, Hendrickson WA, Potter CS, Carragher B, Graziano J, Conigrave AD, Frank J, Clarke OB, Fan QR | 10.1073/PNAS.2115849118 | 2022-01-19 | Yes | |
MTR1B | MT2 | Melatonin | A | Human | Cryo-EM | 7VH0 | 7VH0_refined | 3.5 | A | Active | 100 | 75 | Gi/o | αi1 | - | 61 | - | scFv16 |
ramelteon
|
small-molecule | Agonist | melatonin | small-molecule | No | No | Wang Q, Lu Q, Guo Q, Teng M, Gong Q, Li X, Du Y, Liu Z, Tao Y | 10.1038/S41467-022-28111-3 | 2022-03-02 | Yes | |
GRM3 | mGlu3 | Metabotropic glutamate | C | Human | Cryo-EM | 7WIH | 7WIH_refined | 3.7 | A | Active | - | 84 | - | - | - | - | - | - |
CHEMBL4081453
|
small-molecule | Agonist | NAAG, L-glutamic acid | small-molecule | No | No | Fang W, Yang F, Xu C, Ling S, Lin L, Zhou Y, Sun W, Wang X, Liu P, Rondard P, Shi P, Pin JP, Tian C, Liu J | 10.1038/S41422-022-00623-Z | 2022-03-16 | Yes | |
GIPR | GIP | Glucagon | B1 | Human | Cryo-EM | 7RBT | 7RBT_refined | 3.1 | R | Active | 100 | 81 | Gs | αs | - | 56 | - | scFv16 Nanobody-35 |
tirzepatide
2-fluoro-4-[(1R)-6-methoxy-1-methyl-2-{(1S)-1-[4-(propan-2-yl)phenyl]ethyl}-1,2,3,4-tetrahydroisoquinolin-5-yl]-6-[(2-methylpropyl)amino]phenol |
peptide small-molecule |
Agonist PAM |
gastric inhibitory polypeptide | peptide | No | No | Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW | 10.1073/PNAS.2116506119 | 2022-04-13 | Yes | |
OPRM | μ | Opioid | A | Mouse | Cryo-EM | 7UL4 | 7UL4_refined | 2.8 | A | Inactive | 6 | 72 | - | - | - | - | - | Megabody-6 |
alvimopan
|
small-molecule | Antagonist | - | - | No | No | Robertson MJ, Papasergi-Scott MM, He F, Seven AB, Meyerowitz JG, Panova O, Peroto MC, Che T, Skiniotis G | 10.1038/S41594-022-00859-8 | 2022-06-29 | Yes | |
APJ | apelin | Apelin | A | Human | Cryo-EM | 7W0O | 7W0O_refined | 3.8 | R | Active | 100 | 77 | Gi/o | αi1 | - | 64 | BRIL | scFv16 |
apelin receptor early endogenous ligand
|
peptide | Agonist | Elabela/Toddler-21, apelin-17, [Pyr1]apelin-13, Elabela/Toddler-11, Elabela/Toddler-32, apelin-13, apelin-36, 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 | |
SSR2 | SST2 | Somatostatin | A | Human | X-ray | 7XN9 | 7XN9_refined | 2.6 | A | Inactive | 6 | 79 | - | - | - | - | - | - |
L-054,522
|
small-molecule | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | No | No | - | - | 2022-08-03 | Yes | |
PTH1R | PTH1 | Parathyroid hormone | B1 | Human | Cryo-EM | 7VVM | 7VVM_refined | 3.2 | R | Active | 100 | 60 | Gs | αs | - | 58 | - | Nanobody-35 |
Parathyroid hormone
|
peptide | Agonist | 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 | 7VIE | 7VIE_refined | 2.9 | F | Active | 100 | 73 | Gi/o | αi1 | - | 64 | - | scFv16 |
sphingosine 1-phosphate
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | No | No | Yu L, He L, Gan B, Ti R, Xiao Q, Hu H, Zhu L, Wang S, Ren R | 10.1073/PNAS.2117716119 | 2022-09-28 | Yes | |
AGRL3 | ADGRL3 | ADGRL | B2 | Mouse | Cryo-EM | 7X10 | - | 2.9 | R | Active | 100 | 17 | G12/13 | α12 | - | 55 | - | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Qian Y, Ma Z, Liu C, Li X, Zhu X, Wang N, Xu Z, Xia R, Liang J, Duan Y, Yin H, Xiong Y, Zhang A, Guo C, Chen Z, Huang Z, He Y | 10.1016/J.MOLCEL.2022.10.009 | 2022-11-09 | Yes | |
MRGX1 | MRGPRX1 | A orphans | A | Human | Cryo-EM | 8DWC | - | 2.9 | R | Active | 100 | 78 | Gq/11 | αq | Gs-mini-Gq chimera | 57 | - | scFv16 |
Proenkephalin-A
|
peptide | Agonist | bovine adrenal medulla peptide 8-22 | peptide | No | No | 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 | 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 | 8HJ0 | - | 3.1 | 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 | |
ACM2 | M2 | Acetylcholine (muscarinic) | A | Human | Cryo-EM | 7T94 | - | 3.2 | A | Active | 100 | 57 | Gi/o | αo | - | 62 | - | Antibody fragment |
acetylcholine
LY2119620 |
small-molecule small-molecule |
Agonist PAM |
acetylcholine | small-molecule | No | No | - | - | 2023-01-25 | Yes | |
HCAR2 | HCA2 | Hydroxycarboxylic acid | A | Human | X-ray | 7ZLY | - | 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 | |
OPRK | κ | Opioid | A | Human | Cryo-EM | 8DZQ | 8DZQ_refined | 2.8 | A | Active | 100 | 72 | Gi/o | αo | - | 61 | - | scFv16 |
SALVINORIN B METHOXYMETHYL ETHER
|
small-molecule | Agonist | [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 | |
CNR1 | CB1 | Cannabinoid | A | Human | Cryo-EM | 8GHV | 8GHV_refined | 2.8 | D | Active | 100 | 59 | Gi/o | αi1 | - | 62 | - | scFv16 |
CHEMBL4208628
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | No | No | Krishna Kumar K, Robertson MJ, Thadhani E, Wang H, Suomivuori CM, Powers AS, Ji L, Nikas SP, Dror RO, Inoue A, Makriyannis A, Skiniotis G, Kobilka B | 10.1038/S41467-023-37864-4 | 2023-05-24 | Yes | |
PTH1R | PTH1 | Parathyroid hormone | B1 | Human | Cryo-EM | 8GW8 | - | 2.9 | R | Active | 100 | 37 | Gs | αs | - | 58 | - | Nanobody-35 |
PCO371
|
small-molecule | Agonist | TIP39, PTHrP-(1-36), PTHrP, PTH | peptide | No | No | Kobayashi K, Kawakami K, Kusakizako T, Tomita A, Nishimura M, Sawada K, Okamoto HH, Hiratsuka S, Nakamura G, Kuwabara R, Noda H, Muramatsu H, Shimizu M, Taguchi T, Inoue A, Murata T, Nureki O | 10.1038/S41586-023-06169-3 | 2023-06-14 | Yes | |
FFAR4 | FFA4 | Free fatty acid | A | Human | Cryo-EM | 8IYS | - | 3.0 | R | Active | 100 | 82 | Gq/11 | αq | - | 99 | - | scFv16 |
TUG-891
|
small-molecule | Agonist | 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 | |
GLR | glucagon | Glucagon | B1 | Human | Cryo-EM | 8JRU | - | 3.5 | R | Active | 100 | 53 | Beta | Beta-arrestin-1 | - | 83 | - | scFv30 Nanobody-32 |
Apo (no ligand)
|
none | Apo (no ligand) | glucagon | peptide | No | No | Chen K, Zhang C, Lin S, Yan X, Cai H, Yi C, Ma L, Chu X, Liu Y, Zhu Y, Han S, Zhao Q, Wu B | 10.1038/S41586-023-06420-X | 2023-08-16 | Yes | |
ADA1A | α1A | Adrenoceptors | A | Human | Cryo-EM | 8THL | - | 3.1 | R | Active | 100 | 52 | Gq/11 | αq | - | 57 | T4-Lysozyme | scFv16 |
(-)-adrenaline
|
small-molecule | Agonist | (-)-adrenaline, (-)-noradrenaline | small-molecule | No | No | Su M, Wang J, Xiang G, Do HN, Levitz J, Miao Y, Huang XY | 10.1038/S41467-023-40524-2 | 2023-08-16 | Yes | |
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 | urocortin 1, corticotrophin-releasing hormone, 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 | |
HCAR2 | HCA2 | Hydroxycarboxylic acid | A | Human | Cryo-EM | 8IHH | - | 3.1 | R | Active | 100 | 80 | Gi/o | αi1 | - | 62 | BRIL | scFv16 |
5-butyl-1H-pyrazole-3-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 | 8JIM | - | 3.0 | E | Active | 100 | 80 | Gi/o | αi1 | - | 64 | - | scFv16 |
CHEMBL3354065
|
small-molecule | Agonist | 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 | |
HCAR2 | HCA2 | Hydroxycarboxylic acid | A | Human | Cryo-EM | 8K5B | - | 3.4 | A | Active | 100 | 80 | - | - | - | - | - | - |
nicotinic acid
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | No | No | Park JH, Kawakami K, Ishimoto N, Ikuta T, Ohki M, Ekimoto T, Ikeguchi M, Lee DS, Lee YH, Tame JRH, Inoue A, Park SY | 10.1038/S41467-023-42764-8 | 2023-11-22 | Yes | |
TAAR1 | TA1 | Trace amine | A | Human | Cryo-EM | 8W88 | - | 2.6 | R | Active | 100 | 83 | Gs | αs | - | 60 | - | Nanobody-35 |
ulotaront
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, dopamine | small-molecule | No | No | Liu H, Zheng Y, Wang Y, Wang Y, He X, Xu P, Huang S, Yuan Q, Zhang X, Wang L, Jiang K, Chen H, Li Z, Liu W, Wang S, Xu HE, Xu F | 10.1038/S41586-023-06775-1 | 2023-11-22 | Yes | |
GPR34 | GPR34 | A orphans | A | Human | Cryo-EM | 8XBI | - | 3.1 | R | Active | 63 | 78 | - | - | - | - | - | - |
CHEMBL4758243
|
small-molecule | Agonist | lysophosphatidylserine | small-molecule | No | No | - | - | 2023-12-27 | Yes | |
ADRB1 | β1 | Adrenoceptors | A | Wild turkey | X-ray | 4GPO | 4GPO_refined | 3.5 | B | Inactive | 0 | 58 | - | - | - | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Huang J, Chen S, Zhang JJ, Huang XY | 10.1038/NSMB.2504 | 2013-02-27 | Yes | |
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 | |
NTR1 | NTS1 | Neurotensin | A | Rat | X-ray | 4XES | 4XES_refined | 2.6 | A | Active | 82 | 72 | - | - | - | - | T4-Lysozyme | - |
neurotensin
|
peptide | Agonist | neurotensin, neuromedin N | peptide | No | No | Krumm BE, White JF, Shah P, Grisshammer R | 10.1038/NCOMMS8895 | 2015-07-29 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5K2C | 5K2C_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 | 5XEZ | 5XEZ_refined | 3.0 | B | Inactive | 0 | 82 | - | - | - | - | T4-Lysozyme | Antibody |
NNC0640
|
small-molecule | NAM | glucagon | peptide | No | No | Zhang H, Qiao A, Yang D, Yang L, Dai A, de Graaf C, Reedtz-Runge S, Dharmarajan V, Zhang H, Han GW, Grant TD, Sierra RG, Weierstall U, Nelson G, Liu W, Wu Y, Ma L, Cai X, Lin G, Wu X, Geng Z, Dong Y, Song G, Griffin PR, Lau J, Cherezov V, Yang H, Hanson MA, Stevens RC, Zhao Q, Jiang H, Wang MW, Wu B | 10.1038/NATURE22363 | 2017-05-24 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5WF6 | 5WF6_refined | 2.9 | A | Active | 72 | 68 | - | - | - | - | T4-Lysozyme | - |
UK-432,097
|
small-molecule | Agonist | adenosine | small-molecule | No | No | White KL, Eddy MT, Gao ZG, Han GW, Lian T, Deary A, Patel N, Jacobson KA, Katritch V, Stevens RC | 10.1016/J.STR.2017.12.013 | 2018-02-21 | Yes | |
PD2R2 | DP2 | Prostanoid | A | Human | X-ray | 6D27 | 6D27_refined | 2.7 | A | Inactive | 27 | 81 | - | - | - | - | T4-Lysozyme | - |
CHEMBL179036
|
small-molecule | Antagonist | thromboxane A2, PGF2α, PGI2, PGJ2, PGD3, PGD2, PGE2 | small-molecule | No | No | Wang L, Yao D, Deepak RNVK, Liu H, Xiao Q, Fan H, Gong W, Wei Z, Zhang C | 10.1016/J.MOLCEL.2018.08.009 | 2018-10-03 | Yes | |
NK1R | NK1 | Tachykinin | A | Human | X-ray | 6E59 | 6E59_refined | 3.4 | A | Inactive | 0 | 70 | - | - | - | - | GlgA glycogen synthase | - |
L760735
|
small-molecule | Antagonist | neuropeptide-γ, neurokinin A, neuropeptide K, neurokinin B, hemokinin 1, substance P | peptide | No | No | Yin J, Chapman K, Clark LD, Shao Z, Borek D, Xu Q, Wang J, Rosenbaum DM | 10.1073/PNAS.1812717115 | 2018-12-12 | Yes | |
MTR1A | MT1 | Melatonin | A | Human | X-ray | 6ME2 | 6ME2_refined | 2.8 | A | Inactive | 1 | 83 | - | - | - | - | GlgA glycogen synthase | - |
ramelteon
|
small-molecule | Agonist | melatonin | small-molecule | No | No | 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 | |
EDNRB | ETB | Endothelin | A | Human | X-ray | 6K1Q | 6K1Q_refined | 2.7 | A | Inactive | 4 | 68 | - | - | - | - | T4-Lysozyme | - |
IRL 2500
|
peptide | Inverse agonist | endothelin-1, endothelin-2, endothelin-3 | peptide | No | No | Nagiri C, Shihoya W, Inoue A, Kadji FMN, Aoki J, Nureki O | 10.1038/S42003-019-0482-7 | 2019-07-17 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | Cryo-EM | 6NI3 | 6NI3_refined | 3.8 | R | Active | 100 | 69 | Gs | αs | - | 59 | - | Nanobody-35 |
CHEMBL1615159
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline | small-molecule | No | No | Nguyen AH, Thomsen ARB, Cahill TJ 3rd, Huang R, Huang LY, Marcink T, Clarke OB, Heissel S, Masoudi A, Ben-Hail D, Samaan F, Dandey VP, Tan YZ, Hong C, Mahoney JP, Triest S, Little J 4th, Chen X, Sunahara R, Steyaert J, Molina H, Yu Z, des Georges A, Lefkowitz RJ | 10.1038/S41594-019-0330-Y | 2019-11-20 | Yes | |
GPR52 | GPR52 | A orphans | A | Human | X-ray | 6LI1 | - | 2.9 | A | Intermediate | 40 | 81 | - | - | - | - | Flavodoxin | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Lin X, Li M, Wang N, Wu Y, Luo Z, Guo S, Han GW, Li S, Yue Y, Wei X, Xie X, Chen Y, Zhao S, Wu J, Lei M, Xu F | 10.1038/S41586-020-2019-0 | 2020-02-26 | Yes | |
GLR | glucagon | Glucagon | B1 | Human | Cryo-EM | 6LML | 6LML_refined | 3.9 | R | Active | 100 | 83 | Gi/o | αi1 | - | 63 | - | scFv16 |
glucagon
|
peptide | Agonist | glucagon | peptide | No | No | Qiao A, Han S, Li X, Li Z, Zhao P, Dai A, Chang R, Tai L, Tan Q, Chu X, Ma L, Thorsen TS, Reedtz-Runge S, Yang D, Wang MW, Sexton PM, Wootten D, Sun F, Zhao Q, Wu B | 10.1126/SCIENCE.AAZ5346 | 2020-04-01 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 6ZDV | 6ZDV_refined | 2.1 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
2-Methyl-3-(4-methylthiazol-2-yl)-4-oxo-6-propyl-4H-chromen-7-yl acetate
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | Jespers W, Verdon G, Azuaje J, Majellaro M, Keranen H, Garcia-Mera X, Congreve M, Deflorian F, de Graaf C, Zhukov A, Dore AS, Mason JS, Aqvist J, Cooke RM, Sotelo E, Gutierrez-de-Teran H | 10.1002/ANIE.202003788 | 2020-09-16 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 6WQA | 6WQA_refined | 2.0 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
ZM-241385
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | Lee MY, Geiger J, Ishchenko A, Han GW, Barty A, White TA, Gati C, Batyuk A, Hunter MS, Aquila A, Boutet S, Weierstall U, Cherezov V, Liu W | 10.1107/S2052252520012701 | 2020-11-18 | Yes | |
NTR1 | NTS1 | Neurotensin | A | Rat | Cryo-EM | 7L0R | - | 4.2 | C | Active | 100 | 73 | Gi/o | αi1 | Non-canonical conformation | 63 | - | - |
neurotensin
|
peptide | Agonist | neurotensin, neuromedin N | peptide | No | No | Zhang M, Gui M, Wang ZF, Gorgulla C, Yu JJ, Wu H, Sun ZJ, Klenk C, Merklinger L, Morstein L, Hagn F, Pluckthun A, Brown A, Nasr ML, Wagner G | 10.1038/S41594-020-00554-6 | 2021-01-06 | Yes | |
CASR | CaS | Calcium-sensing | C | Human | Cryo-EM | 7DTV | 7DTV_refined | 3.5 | A | Active | - | 72 | - | - | - | - | - | - |
Calcium
L-tryptophan |
small-molecule small-molecule |
Agonist 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 | |
CCR5 | CCR5 | Chemokine | A | Human | Cryo-EM | 7O7F | 7O7F_refined | 3.2 | C | Active | 100 | 85 | Gi/o | αi1 | - | 62 | - | Fab heavy chain Fab light chain |
CCL5
|
peptide | Agonist | CCL14, CCL8, CCL13, CCL4, CCL7, CCL2, CCL5, CCL11, CCL3, CCL16 | peptide | No | No | Isaikina P, Tsai CJ, Dietz N, Pamula F, Grahl A, Goldie KN, Guixa-Gonzalez R, Branco C, Paolini-Bertrand M, Calo N, Cerini F, Schertler GFX, Hartley O, Stahlberg H, Maier T, Deupi X, Grzesiek S | 10.1126/SCIADV.ABG8685 | 2021-06-30 | Yes | |
MRGX2 | MRGPRX2 | A orphans | A | Human | Cryo-EM | 7S8L | - | 2.5 | R | Active | 100 | 76 | Gq/11 | αq | Gq-Gs chimera | 57 | - | scFv16 |
Cortistatin 14
|
peptide | Agonist | PAMP-20 | peptide | No | No | Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL | 10.1038/S41586-021-04126-6 | 2021-11-17 | Yes | |
GHSR | ghrelin | Ghrelin | A | Human | Cryo-EM | 7NA7 | 7NA7_refined | 2.7 | R | Active | 100 | 80 | Gi/o | αi1 | - | 61 | - | Antibody fragment |
Ghrelin-27
|
peptide | Agonist | [des-Gln14]ghrelin, ghrelin | peptide | No | No | Liu H, Sun D, Myasnikov A, Damian M, Baneres JL, Sun J, Zhang C | 10.1038/S41467-021-26735-5 | 2021-12-15 | Yes | |
FPR2 | FPR2/ALX | Formylpeptide | A | Human | Cryo-EM | 7T6V | 7T6V_refined | 3.1 | R | Active | 100 | 85 | Gi/o | αi1 | - | 61 | - | scFv16 |
synthetic peptide
|
peptide | 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 | 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 | 7TYN | - | 2.6 | R | Active | 100 | 79 | Gs | αs | - | 58 | - | Nanobody-35 |
calcitonin (salmon synthetic)
|
small-molecule | 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 | |
GP183 | GPR183 | A orphans | A | Human | Cryo-EM | 7TUZ | 7TUZ_refined | 3.1 | R | Active | 100 | 79 | Gi/o | αi1 | - | 64 | - | scFv16 |
(2S,4aS,4bS,7R,8S,8aS,9R,10aR)-7-[(2R,3R)-7-hydroxy-3,7-dimethyloctan-2-yl]-4a,7,8-trimethyltetradecahydrophenanthrene-2,9-diol
|
small-molecule | Agonist | 7α,25-dihydroxycholesterol, 7α,27-dihydroxycholesterol, 25-hydroxycholesterol, 7α-hydroxycholesterol, 27-hydroxycholesterol, 7β-hydroxycholesterol, 7β, 25-dihydroxycholesterol, 7β, 27-dihydroxycholesterol | small-molecule | No | No | Chen H, Huang W, Li X | 10.1016/J.STR.2022.04.006 | 2022-04-13 | Yes | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 7S15 | 7S15_refined | 3.8 | R | Active | 93 | 83 | - | - | - | - | - | - |
CHEMBL5191519
|
small-molecule | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | No | No | Griffith DA, Edmonds DJ, Fortin JP, Kalgutkar AS, Kuzmiski JB, Loria PM, Saxena AR, Bagley SW, Buckeridge C, Curto JM, Derksen DR, Dias JM, Griffor MC, Han S, Jackson VM, Landis MS, Lettiere D, Limberakis C, Liu Y, Mathiowetz AM, Patel JC, Piotrowski DW, Price DA, Ruggeri RB, Tess DA. | 10.1021/acs.jmedchem.1c01856 | 2022-06-08 | Yes | |
DRD1 | D1 | Dopamine | A | Human | Cryo-EM | 7F24 | - | 4.2 | F | Active | 100 | 62 | Gs | αs | - | 57 | - | - |
dopamine
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, 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 | |
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 | Elabela/Toddler-21, apelin-17, [Pyr1]apelin-13, Elabela/Toddler-11, Elabela/Toddler-32, apelin-13, apelin-36, 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 | |
SSR2 | SST2 | Somatostatin | A | Human | Cryo-EM | 7XAV | 7XAV_refined | 2.9 | A | Active | 100 | 76 | Gi/o | αi1 | - | 63 | - | scFv16 |
lanreotide
|
peptide | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | No | No | Bo Q, Yang F, Li Y, Meng X, Zhang H, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C | 10.1038/S41421-022-00405-2 | 2022-08-31 | Yes | |
PTH1R | PTH1 | Parathyroid hormone | B1 | Human | Cryo-EM | 7VVN | 7VVN_refined | 3.8 | R | Active | 100 | 51 | Gs | αs | - | 58 | - | Nanobody-35 |
teriparatide
|
peptide | Agonist | 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 | |
CRFR2 | CRF2 | Corticotropin-releasing factor | B1 | Human | Cryo-EM | 7TRY | - | 3.7 | P | Active | 100 | 79 | Gq/11 | α11 | - | 62 | - | - |
Urocortin
|
peptide | Agonist | urocortin 1, corticotrophin-releasing hormone, urocortin 2, urocortin 3 | peptide | No | No | Zhao LH, Lin J, Ji SY, Zhou XE, Mao C, Shen DD, He X, Xiao P, Sun J, Melcher K, Zhang Y, Yu X, Xu HE | 10.1038/S41467-022-33851-3 | 2022-11-09 | Yes | |
AGRF1 | ADGRF1 | ADGRF | B2 | Human | Cryo-EM | 7X2V | - | 3.1 | R | Active | 100 | 30 | Gi/o | αi1 | - | 62 | - | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y | 10.1038/S41467-022-33173-4 | 2022-09-28 | Yes | |
OPRM | μ | Opioid | A | Human | Cryo-EM | 8EF6 | 8EF6_refined | 3.2 | R | Active | 100 | 72 | Gi/o | αi1 | - | 64 | - | scFv16 |
morphine
|
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 | 7ZBC | - | 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 | 8GNE | - | 2.3 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
Sipagladenant
|
small-molecule | Inverse agonist | adenosine | small-molecule | No | Yes | 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 | |
FSHR | FSH | Glycoprotein hormone | A | Human | Cryo-EM | 8I2H | 8I2H_refined | 6.0 | A | Inactive | 17 | 82 | - | - | - | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | FSH | peptide | No | No | Duan J, Xu P, Zhang H, Luan X, Yang J, He X, Mao C, Shen DD, Ji Y, Cheng X, Jiang H, Jiang Y, Zhang S, Zhang Y, Xu HE | 10.1038/S41467-023-36170-3 | 2023-03-22 | Yes | |
OPRK | κ | Opioid | A | Human | X-ray | 7YIT | - | 3.3 | A | Active | 100 | 74 | - | - | - | - | BRIL | Nanobody-39 |
nalfurafine
|
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 | El Daibani A, Paggi JM, Kim K, Laloudakis YD, Popov P, Bernhard SM, Krumm BE, Olsen RHJ, Diberto J, Carroll FI, Katritch V, Wunsch B, Dror RO, Che T | 10.1038/S41467-023-37041-7 | 2023-04-12 | Yes | |
CNR2 | CB2 | Cannabinoid | A | Human | Cryo-EM | 8GUS | - | 3.0 | R | Active | 100 | 81 | Gi/o | αi1 | - | 62 | - | scFv16 |
CHEMBL2179724
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | No | No | Li X, Chang H, Bouma J, de Paus LV, Mukhopadhyay P, Paloczi J, Mustafa M, van der Horst C, Kumar SS, Wu L, Yu Y, van den Berg RJBHN, Janssen APA, Lichtman A, Liu ZJ, Pacher P, van der Stelt M, Heitman LH, Hua T | 10.1038/S41467-023-37112-9 | 2023-05-10 | Yes | |
MTLR | motilin | Motilin | A | Human | Cryo-EM | 8IBU | 8IBU_refined | 3.5 | R | Active | 100 | 66 | Gq/11 | αq | - | 60 | BRIL | scFv16 |
erythromycin
|
small-molecule | Agonist | motilin | peptide | No | No | You C, Zhang Y, Xu Y, Xu P, Li Z, Li H, Huang S, Chen Z, Li J, Xu HE, Jiang Y | 10.1126/SCIADV.ADE9020 | 2023-04-12 | Yes | |
ADA1A | α1A | Adrenoceptors | A | Human | Cryo-EM | 7YM8 | 7YM8_refined | 2.9 | A | Active | 100 | 58 | Gq/11 | αq | Mini-Gq | 46 | - | Nanobody-29 |
oxymetazoline
|
small-molecule | Agonist | (-)-adrenaline, (-)-noradrenaline | small-molecule | No | No | Toyoda Y, Zhu A, Kong F, Shan S, Zhao J, Wang N, Sun X, Zhang L, Yan C, Kobilka BK, Liu X | 10.1038/S41467-023-39310-X | 2023-07-05 | Yes | |
CALCR | CT | Calcitonin | B1 | Human | Cryo-EM | 8F2A | - | 2.2 | R | Active | 100 | 78 | Gs | αs | - | 59 | - | Nanobody-35 |
Pramlintide analogue San385
|
peptide | Agonist | adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), 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 | 8JD3 | - | 3.3 | 2 | Active | - | 89 | Gi/o | αi1 | - | 62 | - | - |
L-glutamic acid
JNJ-40411813 |
small-molecule small-molecule |
Agonist PAM |
L-glutamic acid | small-molecule | No | No | Wang X, Wang M, Xu T, Feng Y, Shao Q, Han S, Chu X, Xu Y, Lin S, Zhao Q, Wu B | 10.1038/S41422-023-00830-2 | 2023-06-21 | Yes | |
GP132 | GPR132 | A orphans | A | Human | Cryo-EM | 8HQM | 8HQM_refined | 3.0 | R | Active | 100 | 81 | Gi/o | αi1 | - | 60 | BRIL | scFv16 |
CHEMBL3354065
|
small-molecule | Agonist | 9-hydroxyoctadecadienoic acid | small-molecule | No | No | Wang JL, Dou XD, Cheng J, Gao MX, Xu GF, Ding W, Ding JH, Li Y, Wang SH, Ji ZW, Zhao XY, Huo TY, Zhang CF, Liu YM, Sha XY, Gao JR, Zhang WH, Hao Y, Zhang C, Sun JP, Jiao N, Yu X | 10.1038/S42255-023-00899-4 | 2023-10-11 | Yes | |
GIPR | GIP | Glucagon | B1 | Human | Cryo-EM | 8ITM | - | 3.1 | R | Active | 100 | 60 | Gs | αs | - | 59 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | gastric inhibitory polypeptide | peptide | No | No | Zhao F, Hang K, Zhou Q, Shao L, Li H, Li W, Lin S, Dai A, Cai X, Liu Y, Xu Y, Feng W, Yang D, Wang MW | 10.1073/PNAS.2306145120 | 2023-10-18 | 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 | β-phenylethylamine, 3-iodothyronamine, 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 | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 8PWN | - | 2.4 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
theophylline
|
small-molecule | Antagonist | adenosine | small-molecule | No | No | El Omari K, Duman R, Mykhaylyk V, Orr CM, Latimer-Smith M, Winter G, Grama V, Qu F, Bountra K, Kwong HS, Romano M, Reis RI, Vogeley L, Vecchia L, Owen CD, Wittmann S, Renner M, Senda M, Matsugaki N, Kawano Y, Bowden TA, Moraes I, Grimes JM, Mancini EJ, Walsh MA, Guzzo CR, Owens RJ, Jones EY, Brown DG, Stuart DI, Beis K, Wagner A | 10.1038/S42004-023-01014-0 | 2023-10-25 | Yes | |
TAAR1 | TA1 | Trace amine | A | Mouse | Cryo-EM | 8WC6 | - | 3.2 | R | Active | 100 | 80 | Gs | αs | - | 58 | - | scFv16 Nanobody-35 |
2-Phenylethanaminium
|
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 | |
5HT1B | 5-HT1B | 5-Hydroxytryptamine | A | Human | X-ray | 4IAQ | 4IAQ_refined | 2.8 | A | Inactive | 17 | 70 | - | - | - | - | BRIL | - |
dihydroergotamine
|
small-molecule | Agonist | tryptamine, 5-hydroxytryptamine, 5-HT-moduline | small-molecule | No | No | Wang C, Jiang Y, Ma J, Wu H, Wacker D, Katritch V, Han GW, Liu W, Huang XP, Vardy E, McCorvy JD, Gao X, Zhou XE, Melcher K, Zhang C, Bai F, Yang H, Yang L, Jiang H, Roth BL, Cherezov V, Stevens RC, Xu HE | 10.1126/SCIENCE.1232807 | 2013-03-13 | Yes | |
P2Y12 | P2Y12 | P2Y | A | Human | X-ray | 4PXZ | - | 2.5 | A | Active | 59 | 84 | - | - | - | - | BRIL | - |
2MeSADP
|
small-molecule | Agonist | ADP, ATP | small-molecule | No | No | Zhang J, Zhang K, Gao ZG, Paoletta S, Zhang D, Han GW, Li T, Ma L, Zhang W, Muller CE, Yang H, Jiang H, Cherezov V, Katritch V, Jacobson KA, Stevens RC, Wu B, Zhao Q | 10.1038/NATURE13288 | 2014-04-30 | Yes | |
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 | |
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, noradrenaline, (-)-adrenaline, 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 | 5V56 | 5V56_refined | 2.9 | B | Inactive | 1 | 61 | - | - | - | - | Flavodoxin | - |
N-methyl-N-[1-[4-(2-methylpyrazol-3-yl)phthalazin-1-yl]piperidin-4-yl]-4-nitro-2-(trifluoromethyl)benzamide
|
small-molecule | Antagonist | - | - | No | No | 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 | |
GLR | glucagon | Glucagon | B1 | Human | X-ray | 5YQZ | 5YQZ_refined | 3.0 | R | Inactive | 2 | 83 | - | - | - | - | T4-Lysozyme | - |
NNC1702
|
peptide | Agonist (partial) | glucagon | peptide | No | No | Zhang H, Qiao A, Yang L, Van Eps N, Frederiksen KS, Yang D, Dai A, Cai X, Zhang H, Yi C, Cao C, He L, Yang H, Lau J, Ernst OP, Hanson MA, Stevens RC, Wang MW, Reedtz-Runge S, Jiang H, Zhao Q, Wu B | 10.1038/NATURE25153 | 2018-01-17 | Yes | |
ADRB1 | β1 | Adrenoceptors | A | Wild turkey | X-ray | 6H7O | 6H7O_refined | 2.8 | A | Active | 99 | 60 | - | - | - | - | Thioredoxin 1 | Camelid antibody fragment Nb6B9 |
(S)-Cyanopindolol
|
small-molecule | Agonist | - | - | No | No | Warne T, Edwards PC, Dore AS, Leslie AGW, Tate CG | 10.1126/SCIENCE.AAU5595 | 2018-10-17 | Yes | |
CNR2 | CB2 | Cannabinoid | A | Human | X-ray | 5ZTY | 5ZTY_refined | 2.8 | A | Inactive | 5 | 80 | - | - | - | - | T4-Lysozyme | - |
AM10257
|
small-molecule | Antagonist | 2-arachidonoylglycerol, anandamide | small-molecule | No | No | Li X, Hua T, Vemuri K, Ho JH, Wu Y, Wu L, Popov P, Benchama O, Zvonok N, Locke K, Qu L, Han GW, Iyer MR, Cinar R, Coffey NJ, Wang J, Wu M, Katritch V, Zhao S, Kunos G, Bohn LM, Makriyannis A, Stevens RC, Liu ZJ | 10.1016/J.CELL.2018.12.011 | 2019-01-30 | Yes | |
ACM2 | M2 | Acetylcholine (muscarinic) | A | Human | Cryo-EM | 6OIK | 6OIK_refined | 3.6 | R | Active | 100 | 60 | Gi/o | αo | - | 61 | - | - |
LY2119620
iperoxo |
small-molecule small-molecule |
Ago-PAM Agonist |
acetylcholine | small-molecule | No | No | Maeda S, Qu Q, Robertson MJ, Skiniotis G, Kobilka BK | 10.1126/SCIENCE.AAW5188 | 2019-05-08 | Yes | |
ADA2A | α2A | Adrenoceptors | A | Human | X-ray | 6KUX | 6KUX_refined | 2.7 | A | Inactive | 1 | 57 | - | - | - | - | BRIL | - |
RS79948
|
small-molecule | Antagonist | (-)-adrenaline, (-)-noradrenaline | small-molecule | No | No | - | - | 2019-12-04 | Yes | |
CRFR1 | CRF1 | Corticotropin-releasing factor | B1 | Human | Cryo-EM | 6P9X | - | 2.9 | R | Active | 100 | 65 | Gs | αs | - | 49 | - | Nanobody-35 |
Corticoliberin
|
peptide | Agonist | urocortin 1, corticotrophin-releasing hormone, urocortin 2 | peptide | No | No | Liang YL, Belousoff MJ, Zhao P, Koole C, Fletcher MM, Truong TT, Julita V, Christopoulos G, Xu HE, Zhang Y, Khoshouei M, Christopoulos A, Danev R, Sexton PM, Wootten D | 10.1016/J.MOLCEL.2020.01.012 | 2020-02-05 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 6PGS | - | 2.9 | A | Active | 100 | 94 | Gi/o | αt2 | Only H5 | 3 | - | - |
Geraniol
|
small-molecule | unknown | - | - | No | No | - | - | 2020-07-01 | Yes | |
GHSR | ghrelin | Ghrelin | A | Human | X-ray | 6KO5 | 6KO5_refined | 3.3 | A | Inactive | 0 | 80 | - | - | - | - | BRIL | Fab7881 heavy chain Fab7881 light chain |
CHEMBL1956994
|
small-molecule | Antagonist | [des-Gln14]ghrelin, ghrelin | peptide | No | No | Shiimura Y, Horita S, Hamamoto A, Asada H, Hirata K, Tanaka M, Mori K, Uemura T, Kobayashi T, Iwata S, Kojima M | 10.1038/S41467-020-17554-1 | 2020-08-12 | Yes | |
5HT2A | 5-HT2A | 5-Hydroxytryptamine | A | Human | X-ray | 6WGT | 6WGT_refined | 3.4 | B | Inactive | 1 | 59 | - | - | - | - | BRIL | - |
Lysergide
|
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 | 7BU7 | 7BU7_refined | 2.6 | A | Active | 99 | 58 | - | - | - | - | T4-Lysozyme | Camelid antibody fragment Nb6B9 |
CHEMBL1615159
|
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 | |
NTR1 | NTS1 | Neurotensin | A | Rat | X-ray | 6Z4V | - | 2.6 | A | Intermediate | 17 | 79 | - | - | - | - | DARPin D12 | - |
JMV431
|
peptide | 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 | |
PE2R2 | EP2 | Prostanoid | A | Human | Cryo-EM | 7CX2 | - | 2.8 | R | Active | 100 | 74 | Gs | αs | - | 58 | - | Nanobody-35 |
PGE2
|
small-molecule | Agonist | thromboxane A2, PGF2α, PGI2, PGD2, PGE1, PGE2 | small-molecule | No | No | Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y | 10.1126/SCIADV.ABF1268 | 2021-05-05 | Yes | |
CASR | CaS | Calcium-sensing | C | Human | Cryo-EM | 7M3F | 7M3F_refined | 2.8 | B | Active | - | 75 | - | - | - | - | - | - |
Calcium
cinacalcet L-tryptophan |
small-molecule small-molecule small-molecule |
Agonist PAM 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 | |
AA1R | A1 | Adenosine | A | Human | Cryo-EM | 7LD4 | 7LD4_refined | 3.3 | R | Active | 100 | 88 | Gi/o | αi2 | - | 59 | - | - |
adenosine
|
small-molecule | Agonist | adenosine | small-molecule | No | No | Draper-Joyce CJ, Bhola R, Wang J, Bhattarai A, Nguyen ATN, Cowie-Kent I, O'Sullivan K, Chia LY, Venugopal H, Valant C, Thal DM, Wootten D, Panel N, Carlsson J, Christie MJ, White PJ, Scammells P, May LT, Sexton PM, Danev R, Miao Y, Glukhova A, Imlach WL, Christopoulos A | 10.1038/S41586-021-03897-2 | 2021-09-08 | Yes | |
BKRB2 | B2 | Bradykinin | A | Human | Cryo-EM | 7F2O | - | 2.9 | R | Active | 100 | 73 | Gq/11 | αq | Gq-Gi1 chimera | 60 | - | scFv16 |
bradykinin
|
peptide | Agonist | [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 | 7VDM | 7VDM_refined | 3.0 | R | Active | 100 | 77 | Gi/o | αi1 | - | 61 | - | scFv16 |
substance P
|
peptide | Agonist | PAMP-20 | peptide | No | No | Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP | 10.1038/S41586-021-04077-Y | 2021-12-01 | Yes | |
5HT2A | 5-HT2A | 5-Hydroxytryptamine | A | Human | X-ray | 7WC8 | 7WC8_refined | 2.5 | A | Inactive | 1 | 59 | - | - | - | - | BRIL | - |
LUMATEPERONE
|
small-molecule | Agonist | 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 | |
FPR2 | FPR2/ALX | Formylpeptide | A | Human | Cryo-EM | 7T6S | 7T6S_refined | 3.0 | R | Active | 100 | 85 | Gi/o | αi1 | - | 61 | - | scFv16 |
N-(4-chlorophenyl)-N'-[1-methyl-3-oxo-2-phenyl-5-(propan-2-yl)-2,3-dihydro-1H-pyrazol-4-yl]urea
|
small-molecule | Agonist | 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 | 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 | 7TYI | - | 3.3 | R | Active | 100 | 77 | Gs | αs | - | 58 | - | 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 | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 7RGP | - | 2.9 | R | Active | 100 | 82 | Gs | αs | Engineered G alpha | 55 | - | scFv16 Nanobody-35 |
tirzepatide
|
peptide | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | 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 | |
GALR2 | GAL2 | Galanin | A | Human | Cryo-EM | 7XJK | 7XJK_refined | 3.3 | F | Active | 100 | 72 | Gq/11 | αq | - | 58 | - | scFv16 |
Galanin, Human
|
peptide | Agonist | galanin-like peptide, spexin-1, galanin | peptide | No | No | Jiang W, Zheng S | 10.1073/PNAS.2121465119 | 2022-06-29 | Yes | |
SSR2 | SST2 | Somatostatin | A | Human | Cryo-EM | 7WJ5 | 7WJ5_refined | 3.7 | R | Active | 100 | 76 | Gi/o | αi1 | - | 60 | BRIL | scFv16 |
SOMATOSTATIN
|
protein | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | No | No | Heo Y, Yoon E, Jeon YE, Yun JH, Ishimoto N, Woo H, Park SY, Song JJ, Lee W | 10.7554/ELIFE.76823 | 2022-07-13 | Yes | |
TSHR | TSH | Glycoprotein hormone | A | Human | Cryo-EM | 7XW7 | 7XW7_refined | 5.5 | R | Inactive | 17 | 74 | - | - | - | - | - | - |
K1-70 scFv light chain
K1-70 scFv heavy chain |
protein protein |
Antagonist | TSH | peptide | No | No | Duan J, Xu P, Luan X, Ji Y, He X, Song N, Yuan Q, Jin Y, Cheng X, Jiang H, Zheng J, Zhang S, Jiang Y, Xu HE | 10.1038/S41586-022-05173-3 | 2022-08-17 | Yes | |
OPRM | μ | Opioid | A | Mouse | Cryo-EM | 7T2H | - | 3.2 | D | Active | 100 | 71 | Gi/o | αi1 | - | 61 | - | scFv16 |
LOFENTANIL
|
small-molecule | Agonist | - | - | No | No | Qu Q, Huang W, Aydin D, Paggi JM, Seven AB, Wang H, Chakraborty S, Che T, DiBerto JF, Robertson MJ, Inoue A, Suomivuori CM, Roth BL, Majumdar S, Dror RO, Kobilka BK, Skiniotis G | 10.1038/S41589-022-01208-Y | 2022-12-07 | Yes | |
AGRL3 | ADGRL3 | ADGRL | B2 | Mouse | Cryo-EM | 7WYB | - | 3.0 | R | Active | 100 | 17 | Gi/o | αi1 | - | 64 | - | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Qian Y, Ma Z, Liu C, Li X, Zhu X, Wang N, Xu Z, Xia R, Liang J, Duan Y, Yin H, Xiong Y, Zhang A, Guo C, Chen Z, Huang Z, He Y | 10.1016/J.MOLCEL.2022.10.009 | 2022-10-26 | Yes | |
MRGX1 | MRGPRX1 | A orphans | A | Human | Cryo-EM | 8DWG | - | 2.7 | R | Active | 100 | 77 | Gq/11 | αq | Gs-mini-Gq chimera | 57 | - | scFv16 |
Proenkephalin-A
CHEMBL5177388 |
peptide small-molecule |
Agonist PAM |
bovine adrenal medulla peptide 8-22 | peptide | No | No | 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 | 8HAO | - | 3.8 | R | Active | 100 | 61 | Gs | αs | - | 60 | - | Nanobody-35 |
teriparatide
|
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 | |
GRPR | BB2 | Bombesin | A | Human | Cryo-EM | 7W3Z | - | 3.0 | A | Active | 100 | 78 | Gq/11 | αq | - | 98 | - | scFv16 |
Gastrin-releasing peptide
|
peptide | Agonist | neuromedin B, gastrin releasing peptide(14-27) (human), GRP-(18-27), gastrin-releasing peptide, neuromedin C | peptide | No | No | Peng S, Zhan Y, Zhang D, Ren L, Chen A, Chen ZF, Zhang H | 10.1073/PNAS.2216230120 | 2023-02-22 | Yes | |
S1PR1 | S1P1 | Lysophospholipid (S1P) | A | Human | Cryo-EM | 8G94 | 8G94_refined | 3.2 | A | Active | 100 | 75 | Gi/o | αi1 | - | 62 | - | scFv16 |
Early activation antigen CD69
|
peptide | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | No | No | Chen H, Qin Y, Chou M, Cyster JG, Li X | 10.7554/ELIFE.88204 | 2023-04-19 | Yes | |
PTH1R | PTH1 | Parathyroid hormone | B1 | Human | Cryo-EM | 8FLR | - | 2.9 | R | Active | 100 | 61 | Gs | αs | - | 59 | - | Nanobody-35 |
PTHrP[1-36]
|
peptide | Agonist | 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 | |
GRM2 | mGlu2 | Metabotropic glutamate | C | Human | Cryo-EM | 8JCY | - | 2.9 | 2 | Inactive | - | 87 | - | - | - | - | - | - |
LY341495
|
small-molecule | Antagonist | L-glutamic acid | small-molecule | No | No | Wang X, Wang M, Xu T, Feng Y, Shao Q, Han S, Chu X, Xu Y, Lin S, Zhao Q, Wu B | 10.1038/S41422-023-00830-2 | 2023-06-21 | Yes | |
PE2R4 | EP4 | Prostanoid | A | Human | Cryo-EM | 8GCP | 8GCP_refined | 3.1 | R | Active | 100 | 56 | Gi/o | αi1 | - | 61 | - | scFv16 |
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 | 2024-01-03 | Yes | |
GP132 | GPR132 | A orphans | A | Human | Cryo-EM | 8HVI | 8HVI_refined | 3.0 | R | Active | 100 | 81 | Gi/o | αi1 | - | 60 | BRIL | scFv16 |
NOX-6-7
|
small-molecule | Agonist | 9-hydroxyoctadecadienoic acid | small-molecule | No | No | Wang JL, Dou XD, Cheng J, Gao MX, Xu GF, Ding W, Ding JH, Li Y, Wang SH, Ji ZW, Zhao XY, Huo TY, Zhang CF, Liu YM, Sha XY, Gao JR, Zhang WH, Hao Y, Zhang C, Sun JP, Jiao N, Yu X | 10.1038/S42255-023-00899-4 | 2023-10-11 | Yes | |
HCAR2 | HCA2 | Hydroxycarboxylic acid | A | Human | Cryo-EM | 8J6Q | - | 2.6 | R | Active | 100 | 81 | Gi/o | αi1 | - | 64 | - | scFv16 |
β-D-hydroxybutyric 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 | |
TAAR1 | TA1 | Trace amine | A | Human | Cryo-EM | 8JSO | 8JSO_refined | 3.4 | R | Active | 100 | 83 | Gs | αs | - | 59 | BRIL | scFv16 |
dexamfetamine
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, 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 | 19 | 75 | - | - | - | - | - | Fab heavy chain Fab light chain |
mAb1
|
protein | Antagonist | 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 | 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 | |
5HT1B | 5-HT1B | 5-Hydroxytryptamine | A | Human | X-ray | 4IAR | 4IAR_refined | 2.7 | A | Inactive | 17 | 70 | - | - | - | - | BRIL | - |
ergotamine
|
small-molecule | Agonist | tryptamine, 5-hydroxytryptamine, 5-HT-moduline | small-molecule | No | No | - | - | 2013-03-13 | Yes | |
ACM3 | M3 | Acetylcholine (muscarinic) | A | Rat | X-ray | 4U14 | 4U14_refined | 3.6 | A | Inactive | 2 | 47 | - | - | - | - | T4-Lysozyme | - |
tiotropium
|
small-molecule | Antagonist | acetylcholine | small-molecule | No | No | Thorsen TS, Matt R, Weis WI, Kobilka BK | 10.1016/J.STR.2014.08.022 | 2014-11-26 | Yes | |
ADRB1 | β1 | Adrenoceptors | A | Wild turkey | X-ray | 5A8E | 5A8E_refined | 2.4 | A | Inactive | 0 | 59 | - | - | - | - | - | - |
7-methylcyanopindolol
|
small-molecule | Inverse agonist | - | - | No | Yes | Sato T, Baker J, Warne T, Brown GA, Leslie AG, Congreve M, Tate CG | 10.1124/MOL.115.101030 | 2015-09-30 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 5DYS | 5DYS_refined | 2.3 | A | Active | 97 | 94 | - | - | - | - | - | - |
Retinal (all-trans)
|
small-molecule | Agonist | - | - | No | No | Singhal A, Guo Y, Matkovic M, Schertler G, Deupi X, Yan EC, Standfuss J | 10.15252/EMBR.201642671 | 2016-08-10 | Yes | |
AGTR2 | AT2 | Angiotensin | A | Human | X-ray | 5UNG | 5UNG_refined | 2.8 | B | Active | 99 | 83 | - | - | - | - | BRIL | - |
compound 1 [PMID: 28379944]
|
small-molecule | Antagonist | angiotensin-(1-7), angiotensin II, angiotensin III | peptide | No | No | Zhang H, Han GW, Batyuk A, Ishchenko A, White KL, Patel N, Sadybekov A, Zamlynny B, Rudd MT, Hollenstein K, Tolstikova A, White TA, Hunter MS, Weierstall U, Liu W, Babaoglu K, Moore EL, Katz RD, Shipman JM, Garcia-Calvo M, Sharma S, Sheth P, Soisson SM, Stevens RC, Katritch V, Cherezov V | 10.1038/NATURE22035 | 2017-04-05 | Yes | |
Q08BG4 | LPA6 | Lysophospholipid (LPA) | A | Zebrafish | X-ray | 5XSZ | - | 3.2 | A | Active | 59 | 78 | - | - | - | - | T4-Lysozyme | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Taniguchi R, Inoue A, Sayama M, Uwamizu A, Yamashita K, Hirata K, Yoshida M, Tanaka Y, Kato HE, Nakada-Nakura Y, Otani Y, Nishizawa T, Doi T, Ohwada T, Ishitani R, Aoki J, Nureki O | 10.1038/NATURE23448 | 2017-08-16 | Yes | |
5HT1B | 5-HT1B | 5-Hydroxytryptamine | A | Human | X-ray | 5V54 | 5V54_refined | 3.9 | A | Inactive | 17 | 71 | - | - | - | - | BRIL | - |
CHEMBL428892
|
small-molecule | Antagonist | tryptamine, 5-hydroxytryptamine, 5-HT-moduline | small-molecule | No | No | - | - | 2018-02-07 | Yes | |
AA1R | A1 | Adenosine | A | Human | Cryo-EM | 6D9H | 6D9H_refined | 3.6 | R | Active | 100 | 88 | Gi/o | αi2 | - | 59 | - | - |
adenosine
|
small-molecule | Agonist | adenosine | small-molecule | No | No | Draper-Joyce CJ, Khoshouei M, Thal DM, Liang YL, Nguyen ATN, Furness SGB, Venugopal H, Baltos JA, Plitzko JM, Danev R, Baumeister W, May LT, Wootten D, Sexton PM, Glukhova A, Christopoulos A | 10.1038/S41586-018-0236-6 | 2018-06-20 | Yes | |
CCR2 | CCR2 | Chemokine | A | Human | X-ray | 6GPS | 6GPS_refined | 3.3 | A | Inactive | 19 | 74 | - | - | - | - | Rubredoxin | - |
MK-0812
|
small-molecule | Antagonist | CCL8, CCL13, CCL7, CCL2, CCL11, CCL24, CCL16, CCL26 | peptide | No | No | Apel AK, Cheng RKY, Tautermann CS, Brauchle M, Huang CY, Pautsch A, Hennig M, Nar H, Schnapp G | 10.1016/J.STR.2018.10.027 | 2019-01-02 | Yes | |
NTR1 | NTS1 | Neurotensin | A | Human | Cryo-EM | 6OSA | - | 3.0 | R | Active | 100 | 77 | Gi/o | αi1 | Non-canonical conformation | 62 | - | - |
JMV449
|
peptide | Agonist | large neurotensin, large neuromedin N, neurotensin, neuromedin N | peptide | No | No | Kato HE, Zhang Y, Hu H, Suomivuori CM, Kadji FMN, Aoki J, Krishna Kumar K, Fonseca R, Hilger D, Huang W, Latorraca NR, Inoue A, Dror RO, Kobilka BK, Skiniotis G | 10.1038/S41586-019-1337-6 | 2019-07-10 | Yes | |
OX1R | OX1 | Orexin | A | Human | X-ray | 6TQ7 | 6TQ7_refined | 2.7 | A | Inactive | 0 | 71 | - | - | - | - | - | - |
SB-334867
|
small-molecule | Antagonist | orexin-A, orexin-B | peptide | No | No | Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA. | 10.1021/acs.jmedchem.9b01787 | 2020-01-01 | Yes | |
PACR | PAC1 | VIP and PACAP | B1 | Human | Cryo-EM | 6LPB | 6LPB_refined | 3.9 | R | Active | 100 | 71 | Gs | αs | - | 57 | - | Nanobody-35 |
[Ac-His1]PACAP-27
|
peptide | Agonist | VIP, PHI, PHM, PHV, PACAP-27, 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 | |
OX1R | OX1 | Orexin | A | Human | X-ray | 6V9S | 6V9S_refined | 3.5 | A | Inactive | 0 | 72 | - | - | - | - | GlgA glycogen synthase | - |
JH112
|
small-molecule | Antagonist | orexin-A, orexin-B | peptide | No | No | Hellmann J, Drabek M, Yin J, Gunera J, Proll T, Kraus F, Langmead CJ, Hubner H, Weikert D, Kolb P, Rosenbaum DM, Gmeiner P | 10.1073/PNAS.2002704117 | 2020-07-15 | Yes | |
GPBAR | GPBA | Bile acid | A | Human | Cryo-EM | 7BW0 | 7BW0_refined | 3.9 | R | Active | 100 | 85 | Gs | αs | - | 57 | BRIL | Nanobody-35 | - | - | - | deoxycholic acid, cholic acid, chenodeoxycholic acid, lithocholic acid | small-molecule | No | No | Chen G, Wang X, Ge Y, Ma L, Chen Q, Liu H, Du Y, Ye RD, Hu H, Ren R | 10.1038/S41392-020-00262-Z | 2020-09-02 | Yes | |
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 | |
DRD2 | D2 | Dopamine | A | Human | Cryo-EM | 7JVR | - | 2.8 | R | Active | 100 | 61 | Gi/o | αi1 | - | 63 | - | scFv16 |
bromocriptine
|
small-molecule | Agonist | dopamine | small-molecule | No | No | Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP, Shen DD, Xu T, Liu YF, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE | 10.1016/J.CELL.2021.01.027 | 2021-02-24 | Yes | |
CASR | CaS | Calcium-sensing | C | Human | Cryo-EM | 7DD6 | - | 3.2 | B | Active | - | 73 | - | - | - | - | - | - |
Calcium
L-tryptophan |
small-molecule small-molecule |
Agonist PAM |
Mg2+, L-tryptophan, spermine, Ca2+ | 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 | |
CCR5 | CCR5 | Chemokine | A | Human | X-ray | 7F1T | - | 2.6 | A | Inactive | 19 | 86 | - | - | - | - | Rubredoxin | - |
CCL3
|
peptide | Agonist | CCL14, CCL8, CCL13, CCL4, CCL7, CCL2, CCL5, CCL11, CCL3, CCL16 | peptide | No | No | - | - | 2021-07-14 | Yes | |
MRGX2 | MRGPRX2 | A orphans | A | Human | Cryo-EM | 7VUY | - | 2.8 | R | Active | 100 | 78 | Gi/o | αi1 | - | 64 | - | scFv16 |
PAMP-12
|
peptide | Agonist | PAMP-20 | peptide | No | No | Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP | 10.1038/S41586-021-04077-Y | 2021-12-01 | Yes | |
5HT2A | 5-HT2A | 5-Hydroxytryptamine | A | Human | X-ray | 7WC7 | 7WC7_refined | 2.6 | A | Inactive | 1 | 59 | - | - | - | - | BRIL | - |
lisuride
|
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 | 7F4I | 7F4I_refined | 3.1 | R | Active | 100 | 84 | Gs | αs | - | 59 | - | Nanobody-35 |
bremelanotide
|
peptide | 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 | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 7PX4 | 7PX4_refined | 2.3 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
Preladenant conjugate PSB-2113
|
small-molecule | Antagonist | adenosine | small-molecule | No | No | Claff T, Klapschinski TA, Tiruttani Subhramanyam UK, Vaassen VJ, Schlegel JG, Vielmuth C, Voss JH, Labahn J, Muller CE | 10.1002/ANIE.202115545 | 2022-03-02 | Yes | |
GRM3 | mGlu3 | Metabotropic glutamate | C | Human | Cryo-EM | 7WI8 | 7WI8_refined | 4.2 | A | Inactive | - | 82 | - | - | - | - | - | - |
LY341495
|
small-molecule | Antagonist | NAAG, L-glutamic acid | small-molecule | No | No | Fang W, Yang F, Xu C, Ling S, Lin L, Zhou Y, Sun W, Wang X, Liu P, Rondard P, Shi P, Pin JP, Tian C, Liu J | 10.1038/S41422-022-00623-Z | 2022-03-16 | Yes | |
GALR2 | GAL2 | Galanin | A | Human | Cryo-EM | 7WQ4 | 7WQ4_refined | 2.6 | R | Active | 100 | 73 | Gq/11 | αq | - | 60 | - | Nanobody-35 |
galanin
|
peptide | Agonist | galanin-like peptide, spexin-1, galanin | peptide | No | No | Duan J, Shen DD, Zhao T, Guo S, He X, Yin W, Xu P, Ji Y, Chen LN, Liu J, Zhang H, Liu Q, Shi Y, Cheng X, Jiang H, Eric Xu H, Zhang Y, Xie X, Jiang Y | 10.1038/S41467-022-29072-3 | 2022-04-20 | Yes | |
AGRG5 | ADGRG5 | ADGRG | B2 | Human | Cryo-EM | 7EQ1 | - | 3.3 | R | Active | 100 | 54 | Gs | αs | - | 60 | - | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Ping YQ, Xiao P, Yang F, Zhao RJ, Guo SC, Yan X, Wu X, Zhang C, Lu Y, Zhao F, Zhou F, Xi YT, Yin W, Liu FZ, He DF, Zhang DL, Zhu ZL, Jiang Y, Du L, Feng SQ, Schoneberg T, Liebscher I, Xu HE, Sun JP | 10.1038/S41586-022-04619-Y | 2022-05-11 | Yes | |
SSR2 | SST2 | Somatostatin | A | Human | Cryo-EM | 7WIC | - | 2.8 | R | Active | 100 | 78 | Gi/o | αi1 | - | 64 | - | scFv16 |
SOMATOSTATIN
|
protein | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | No | No | Chen LN, Wang WW, Dong YJ, Shen DD, Guo J, Yu X, Qin J, Ji SY, Zhang H, Shen Q, He Q, Yang B, Zhang Y, Li Q, Mao C | 10.1038/S41422-022-00669-Z | 2022-06-01 | Yes | |
APJ | apelin | Apelin | A | Human | Cryo-EM | 7W0M | 7W0M_refined | 3.7 | R | Active | 100 | 76 | Gi/o | αi1 | - | 62 | BRIL | scFv16 |
(1R,2S)-N-[4-(2,6-dimethoxyphenyl)-5-(6-methylpyridin-2-yl)-1,2,4-triazol-3-yl]-1-(5-methylpyrimidin-2-yl)-1-oxidanyl-propane-2-sulfonamide
|
small-molecule | Agonist | Elabela/Toddler-21, apelin-17, [Pyr1]apelin-13, Elabela/Toddler-11, Elabela/Toddler-32, apelin-13, apelin-36, 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 | |
5HT2C | 5-HT2C | 5-Hydroxytryptamine | A | Human | Cryo-EM | 8DPF | - | 2.8 | A | Active | 100 | 58 | Gq/11 | αq | Gi2-mini-Gq chimera | 57 | - | scFv16 |
lorcaserin
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | No | No | Gumpper RH, Fay JF, Roth BL | 10.1016/J.CELREP.2022.111211 | 2022-08-24 | Yes | |
TSHR | TSH | Glycoprotein hormone | A | Human | Cryo-EM | 7XW6 | - | 2.8 | R | Active | 100 | 74 | Gs | αs | - | 59 | - | Nanobody-35 |
M22 antibody heavy chain
M22 antibody light chain N-[4-[[5-[(2S)-3-benzyl-5-hydroxy-4-oxo-1,2-dihydroquinazolin-2-yl]-2-methoxyphenyl]methoxy]phenyl]acetamide |
protein protein small-molecule |
Agonist | TSH | peptide | No | No | Duan J, Xu P, Luan X, Ji Y, He X, Song N, Yuan Q, Jin Y, Cheng X, Jiang H, Zheng J, Zhang S, Jiang Y, Xu HE | 10.1038/S41586-022-05173-3 | 2022-08-17 | Yes | |
HCAR3 | HCA3 | Hydroxycarboxylic acid | A | Human | Cryo-EM | 8IHK | - | 3.2 | R | Active | 100 | 73 | - | - | - | - | BRIL | - |
(5S)-5-methyl-4-oxo-5-phenylfuran-2-carboxylic acid
|
small-molecule | Agonist | 3-hydroxyoctanoic 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 | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 8JIR | 8JIR_refined | 2.6 | R | Active | 100 | 83 | Gs | αs | - | 58 | - | Nanobody-35 |
SAR425899
|
peptide | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | 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 | |
GPR61 | GPR61 | A orphans | A | Human | Cryo-EM | 8TB0 | 8TB0_refined | 3.5 | R | Active | 100 | 56 | Gs | αs | - | 56 | - | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | - | - | 2023-10-04 | Yes | |
TAAR1 | TA1 | Trace amine | A | Human | Cryo-EM | 8WCA | - | 3.5 | R | Active | 100 | 81 | Gs | αs | - | 59 | - | scFv16 |
2-Phenylethanaminium
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, dopamine | 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 | |
5HT2B | 5-HT2B | 5-Hydroxytryptamine | A | Human | X-ray | 4IB4 | - | 2.7 | A | Active | 59 | 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 | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 4PXF | 4PXF_refined | 2.8 | A | Active | 100 | 93 | Visual | S-arrestin | Fragment | 2 | - | - |
B-Octylglucoside
|
small-molecule | unknown | - | - | No | No | Szczepek M, Beyriere F, Hofmann KP, Elgeti M, Kazmin R, Rose A, Bartl FJ, von Stetten D, Heck M, Sommer ME, Hildebrand PW, Scheerer P | 10.1038/NCOMMS5801 | 2014-09-17 | Yes | |
OPSD | Rhodopsin | Opsins | A | Human | X-ray | 4ZWJ | 4ZWJ_refined | 3.3 | A | Active | 100 | 94 | Visual | S-arrestin | - | 86 | T4-Lysozyme | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Kang Y, Zhou XE, Gao X, He Y, Liu W, Ishchenko A, Barty A, White TA, Yefanov O, Han GW, Xu Q, de Waal PW, Ke J, Tan MH, Zhang C, Moeller A, West GM, Pascal BD, Van Eps N, Caro LN, Vishnivetskiy SA, Lee RJ, Suino-Powell KM, Gu X, Pal K, Ma J, Zhi X, Boutet S, Williams GJ, Messerschmidt M, Gati C, Zatsepin NA, Wang D, James D, Basu S, Roy-Chowdhury S, Conrad CE, Coe J, Liu H, Lisova S, Kupitz C, Grotjohann I, Fromme R, Jiang Y, Tan M, Yang H, Li J, Wang M, Zheng Z, Li D, Howe N, Zhao Y, Standfuss J, Diederichs K, Dong Y, Potter CS, Carragher B, Caffrey M, Jiang H, Chapman HN, Spence JC, Fromme P, Weierstall U, Ernst OP, Katritch V, Gurevich VV, Griffin PR, Hubbell WL, Stevens RC, Cherezov V, Melcher K, Xu HE | 10.1038/NATURE14656 | 2015-07-29 | Yes | |
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 | Mannervik M | 10.1101/436212 | 2018-10-17 | Yes | |
GRM5 | mGlu5 | Metabotropic glutamate | C | Human | Cryo-EM | 6N51 | 6N51_refined | 4.0 | B | Intermediate | - | 65 | - | - | - | - | - | Nanobody-43 |
quisqualate
|
small-molecule | Agonist | L-glutamic acid | small-molecule | No | No | Koehl A, Hu H, Feng D, Sun B, Zhang Y, Robertson MJ, Chu M, Kobilka TS, Laeremans T, Steyaert J, Tarrasch J, Dutta S, Fonseca R, Weis WI, Mathiesen JM, Skiniotis G, Kobilka BK | 10.1038/S41586-019-0881-4 | 2019-01-23 | Yes | |
CNR1 | CB1 | Cannabinoid | A | Human | X-ray | 6KQI | 6KQI_refined | 3.3 | A | Inactive | 13 | 60 | - | - | - | - | GlgA glycogen synthase | - |
CP55940
Org27569 |
small-molecule small-molecule |
Agonist NAM |
2-arachidonoylglycerol, anandamide | small-molecule | No | No | Shao Z, Yan W, Chapman K, Ramesh K, Ferrell AJ, Yin J, Wang X, Xu Q, Rosenbaum DM | 10.1038/S41589-019-0387-2 | 2019-10-23 | Yes | |
OX1R | OX1 | Orexin | A | Human | X-ray | 6TQ4 | 6TQ4_refined | 2.3 | B | Inactive | 0 | 70 | - | - | - | - | - | - |
CHEMBL4590386
|
small-molecule | Antagonist | orexin-A, orexin-B | peptide | No | No | Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA. | 10.1021/acs.jmedchem.9b01787 | 2020-01-01 | Yes | |
FPR2 | FPR2/ALX | Formylpeptide | A | Human | Cryo-EM | 6OMM | 6OMM_refined | 3.2 | R | Active | 100 | 85 | Gi/o | αi1 | - | 61 | - | - |
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 | Zhuang Y, Liu H, Edward Zhou X, Kumar Verma R, de Waal PW, Jang W, Xu TH, Wang L, Meng X, Zhao G, Kang Y, Melcher K, Fan H, Lambert NA, Eric Xu H, Zhang C | 10.1038/S41467-020-14728-9 | 2020-02-26 | Yes | |
GABR2 | GABAB2 | GABAB | C | Human | Cryo-EM | 7C7S | - | 2.9 | B | Inactive | - | 71 | - | - | - | - | - | - |
CGP 54626A
|
small-molecule | Antagonist | - | - | No | No | - | - | 2020-07-01 | Yes | |
SMO | SMO | Frizzled | F | Human | Cryo-EM | 6XBJ | - | 3.9 | R | Active | 100 | 59 | Gi/o | αi1 | - | 61 | - | scFv16 |
Cholesterol
|
small-molecule | Agonist | - | - | No | No | Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X | 10.1038/S41589-020-0646-2 | 2020-09-30 | Yes | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 7LCI | 7LCI_refined | 2.9 | R | Active | 100 | 85 | Gs | αs | - | 62 | - | - |
danuglipron
|
small-molecule | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | No | No | Zhang X, Johnson RM, Drulyte I, Yu L, Kotecha A, Danev R, Wootten D, Sexton PM, Belousoff MJ | 10.1016/J.STR.2021.04.008 | 2021-01-20 | Yes | |
DRD1 | D1 | Dopamine | A | Human | Cryo-EM | 7LJC | - | 3.0 | R | Active | 100 | 63 | Gs | αs | Engineered G alpha | 60 | - | Nanobody-35 |
CHEMBL1160787
mevidalen |
small-molecule small-molecule |
Agonist PAM |
L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | No | No | Zhuang Y, Krumm B, Zhang H, Zhou XE, Wang Y, Huang XP, Liu Y, Cheng X, Jiang Y, Jiang H, Zhang C, Yi W, Roth BL, Zhang Y, Xu HE | 10.1038/S41422-021-00482-0 | 2021-03-03 | Yes | |
GRM2 | mGlu2 | Metabotropic glutamate | C | Human | Cryo-EM | 7EPB | 7EPB_refined | 3.1 | B | Active | - | 89 | - | - | - | - | - | Anti-RON nanobody |
eglumegad
|
small-molecule | Agonist | L-glutamic acid | small-molecule | No | No | Du J, Wang D, Fan H, Xu C, Tai L, Lin S, Han S, Tan Q, Wang X, Xu T, Zhang H, Chu X, Yi C, Liu P, Wang X, Zhou Y, Pin JP, Rondard P, Liu H, Liu J, Sun F, Wu B, Zhao Q | 10.1038/S41586-021-03641-W | 2021-06-23 | Yes | |
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-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | No | No | Zhang X, Belousoff MJ, Liang YL, Danev R, Sexton PM, Wootten D | 10.1016/J.CELREP.2021.109374 | 2021-08-04 | Yes | |
NK1R | NK1 | Tachykinin | A | Human | Cryo-EM | 7RMI | - | 3.2 | R | Active | 100 | 70 | Gq/11 | αq | Gs-Gq chimera | 52 | - | Nanobody-35 |
substance P
|
peptide | Agonist | neuropeptide-γ, neurokinin A, neuropeptide K, neurokinin B, hemokinin 1, 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 | |
GHSR | ghrelin | Ghrelin | A | Human | Cryo-EM | 7NA8 | - | 2.7 | R | Active | 100 | 78 | Gi/o | αi1 | - | 61 | - | Antibody fragment |
ibutamoren
|
small-molecule | Agonist | [des-Gln14]ghrelin, ghrelin | peptide | No | No | Liu H, Sun D, Myasnikov A, Damian M, Baneres JL, Sun J, Zhang C | 10.1038/S41467-021-26735-5 | 2021-12-15 | Yes | |
S1PR1 | S1P1 | Lysophospholipid (S1P) | A | Human | Cryo-EM | 7EVZ | - | 3.1 | D | Active | 100 | 71 | Gi/o | αi1 | - | 64 | - | scFv16 |
cenerimod
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | No | No | Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z | 10.1038/S41422-021-00566-X | 2021-09-29 | Yes | |
MTR1A | MT1 | Melatonin | A | Human | Cryo-EM | 7VGZ | 7VGZ_refined | 3.3 | B | Active | 100 | 81 | Gi/o | αi1 | - | 62 | - | scFv16 |
ramelteon
|
small-molecule | Agonist | melatonin | small-molecule | No | No | Wang Q, Lu Q, Guo Q, Teng M, Gong Q, Li X, Du Y, Liu Z, Tao Y | 10.1038/S41467-022-28111-3 | 2022-03-02 | Yes | |
ADA2A | α2A | Adrenoceptors | A | Human | Cryo-EM | 7EJ8 | - | 3.0 | R | Active | 100 | 57 | Gi/o | αo | - | 61 | - | scFv16 |
brimonidine (UK14304)
|
small-molecule | Agonist | (-)-adrenaline, (-)-noradrenaline | small-molecule | No | No | Xu J, Cao S, Hubner H, Weikert D, Chen G, Lu Q, Yuan D, Gmeiner P, Liu Z, Du Y | 10.1126/SCIADV.ABJ5347 | 2022-04-13 | Yes | |
OPRM | μ | Opioid | A | Mouse | Cryo-EM | 7SBF | - | 2.9 | R | Active | 100 | 71 | Gi/o | αi1 | - | 61 | BRIL | scFv16 |
N-[(2S)-2-(dimethylamino)-3-(4-hydroxyphenyl)propyl]-N'-[(2S)-1-(thiophen-3-yl)propan-2-yl]urea
|
small-molecule | Agonist | - | - | No | No | Wang H, Hetzer F, Huang W, Qu Q, Meyerowitz J, Kaindl J, Hubner H, Skiniotis G, Kobilka BK, Gmeiner P | 10.1002/ANIE.202200269 | 2022-04-20 | Yes | |
NPY1R | Y1 | Neuropeptide Y | A | Human | Cryo-EM | 7X9A | 7X9A_refined | 3.2 | R | Active | 100 | 80 | Gi/o | αi1 | - | 61 | - | - |
neuropeptide Y
|
peptide | Agonist | peptide YY, neuropeptide Y, pancreatic polypeptide | peptide | No | No | Tang T, Tan Q, Han S, Diemar A, Lobner K, Wang H, Schuss C, Behr V, Morl K, Wang M, Chu X, Yi C, Keller M, Kofoed J, Reedtz-Runge S, Kaiser A, Beck-Sickinger AG, Zhao Q, Wu B | 10.1126/SCIADV.ABM1232 | 2022-05-18 | Yes | |
APJ | apelin | Apelin | A | Human | Cryo-EM | 7W0N | - | 4.2 | R | Active | 100 | 78 | Gi/o | αi1 | - | 64 | BRIL | scFv16 |
apelin receptor early endogenous ligand
|
peptide | Agonist | Elabela/Toddler-21, apelin-17, [Pyr1]apelin-13, Elabela/Toddler-11, Elabela/Toddler-32, apelin-13, apelin-36, 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 | CCL8, CCL13, CCL7, CCL2, CCL11, CCL24, CCL16, 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 | 7WY0 | - | 2.8 | R | Active | 100 | 30 | G12/13 | α13 | - | 55 | - | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y | 10.1038/S41467-022-33173-4 | 2022-09-28 | Yes | |
LPAR1 | LPA1 | Lysophospholipid (LPA) | A | Human | Cryo-EM | 7YU4 | 7YU4_refined | 3.3 | A | Active | 99 | 73 | - | - | - | - | - | - |
[(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate
|
small-molecule | Agonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | No | No | - | - | 2022-10-05 | Yes | |
VIPR1 | VPAC1 | VIP and PACAP | B1 | Human | Cryo-EM | 8E3Y | - | 2.3 | R | Active | 100 | 81 | Gs | αs | - | 56 | - | Nanobody-35 |
[Ac-His1]PACAP-27
|
peptide | Agonist | VIP, PHI, PHM, secretin, PACAP-27, GHRH, PACAP-38 | peptide | No | No | Piper SJ, Deganutti G, Lu J, Zhao P, Liang YL, Lu Y, Fletcher MM, Hossain MA, Christopoulos A, Reynolds CA, Danev R, Sexton PM, Wootten D | 10.1038/S41467-022-34629-3 | 2022-11-23 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 8A6D | 8A6D_refined | 1.8 | A | Inactive | 24 | 87 | - | - | - | - | - | - |
Retinal (11-cis)
|
small-molecule | Agonist | - | - | No | No | Gruhl T, Weinert T, Rodrigues MJ, Milne CJ, Ortolani G, Nass K, Nango E, Sen S, Johnson PJM, Cirelli C, Furrer A, Mous S, Skopintsev P, James D, Dworkowski F, Bath P, Kekilli D, Ozerov D, Tanaka R, Glover H, Bacellar C, Brunle S, Casadei CM, Diethelm AD, Gashi D, Gotthard G, Guixa-Gonzalez R, Joti Y, Kabanova V, Knopp G, Lesca E, Ma P, Martiel I, Muhle J, Owada S, Pamula F, Sarabi D, Tejero O, Tsai CJ, Varma N, Wach A, Boutet S, Tono K, Nogly P, Deupi X, Iwata S, Neutze R, Standfuss J, Schertler G, Panneels V | 10.1038/S41586-023-05863-6 | 2023-03-29 | Yes | |
EDNRA | ETA | Endothelin | A | Human | Cryo-EM | 8HCQ | 8HCQ_refined | 3.0 | R | Active | 100 | 71 | Gq/11 | αq | - | 57 | - | scFv16 |
ENDOTHELIN
|
protein | Agonist | endothelin-1, endothelin-2, endothelin-3 | peptide | No | No | - | - | 2023-03-22 | Yes | |
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 | |
C3AR | C3a | Complement peptide | A | Human | Cryo-EM | 8HK3 | 8HK3_refined | 3.2 | C | Active | 100 | 59 | Gi/o | αi1 | - | 63 | - | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | C5a, C3a | peptide | No | No | Wang Y, Liu W, Xu Y, He X, Yuan Q, Luo P, Fan W, Zhu J, Zhang X, Cheng X, Jiang Y, Xu HE, Zhuang Y | 10.1038/S41589-023-01339-W | 2023-05-10 | Yes | |
C5AR1 | C5a1 | Complement peptide | A | Human | Cryo-EM | 8HK5 | 8HK5_refined | 3.0 | A | Active | 100 | 84 | Gi/o | αi1 | - | 63 | - | - |
C5a
|
peptide | Agonist | ribosomal protein S19, C5a, C5a des-Arg, C3a | peptide | No | No | Wang Y, Liu W, Xu Y, He X, Yuan Q, Luo P, Fan W, Zhu J, Zhang X, Cheng X, Jiang Y, Xu HE, Zhuang Y | 10.1038/S41589-023-01339-W | 2023-05-10 | Yes | |
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 | thromboxane A2, PGF2α, PGI2, PGD2, 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 | |
GRM4 | mGlu4 | Metabotropic glutamate | C | Human | Cryo-EM | 8JD6 | - | 3.4 | S | Active | - | 83 | Gi/o | αi3 | - | 63 | - | scFv16 |
VU0364770
|
small-molecule | Agonist | L-serine-O-phosphate, 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 | 8H2G | 8H2G_refined | 3.0 | A | Active | 100 | 80 | Gi/o | αi1 | - | 63 | - | scFv16 |
nicotinic acid
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | No | No | - | - | 2023-10-11 | Yes | |
HCAR2 | HCA2 | Hydroxycarboxylic acid | A | Human | Cryo-EM | 8IHF | - | 3.0 | R | Active | 100 | 80 | Gi/o | αi1 | - | 62 | BRIL | scFv16 |
MK 6892
|
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 | |
ADRB2 | β2 | Adrenoceptors | A | Human | Cryo-EM | 8JJ8 | - | 3.2 | F | Active | 99 | 68 | - | - | - | - | BRIL | - |
ARFORMOTEROL
|
small-molecule | Agonist (partial) | L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline | small-molecule | 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 | |
HCAR2 | HCA2 | Hydroxycarboxylic acid | A | Human | Cryo-EM | 8K5D | - | 3.7 | A | Active | 100 | 80 | - | - | - | - | - | - |
GSK256073
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | No | No | Park JH, Kawakami K, Ishimoto N, Ikuta T, Ohki M, Ekimoto T, Ikeguchi M, Lee DS, Lee YH, Tame JRH, Inoue A, Park SY | 10.1038/S41467-023-42764-8 | 2023-11-22 | Yes | |
GP101 | GPR101 | A orphans | A | Human | Cryo-EM | 8W8R | - | 3.3 | R | Active | 100 | 55 | Gs | αs | - | 60 | - | scFv16 |
1-(4-Methylpyridin-2-yl)-3-[3-(trifluoromethyl)phenyl]thiourea
|
small-molecule | Agonist | - | - | No | No | Yang Z, Wang JY, Yang F, Zhu KK, Wang GP, Guan Y, Ning SL, Lu Y, Li Y, Zhang C, Zheng Y, Zhou SH, Wang XW, Wang MW, Xiao P, Yi F, Zhang C, Zhang PJ, Xu F, Liu BH, Zhang H, Yu X, Gao N, Sun JP | 10.1038/S41589-023-01456-6 | 2024-01-03 | Yes | |
ADRB1 | β1 | Adrenoceptors | A | Wild turkey | X-ray | 3ZPQ | 3ZPQ_refined | 2.8 | B | Inactive | 0 | 62 | - | - | - | - | - | - |
CHEMBL200234
|
small-molecule | Antagonist | - | - | No | Yes | Christopher JA, Brown J, Doré AS, Errey JC, Koglin M, Marshall FH, Myszka DG, Rich RL, Tate CG, Tehan B, Warne T, Congreve M. | 10.1021/jm400140q | 2013-04-03 | Yes | |
P2Y12 | P2Y12 | P2Y | A | Human | X-ray | 4NTJ | - | 2.6 | A | Active | 59 | 78 | - | - | - | - | BRIL | - |
AZD1283
|
small-molecule | Antagonist | ADP, ATP | small-molecule | No | No | Zhang K, Zhang J, Gao ZG, Zhang D, Zhu L, Han GW, Moss SM, Paoletta S, Kiselev E, Lu W, Fenalti G, Zhang W, Muller CE, Yang H, Jiang H, Cherezov V, Katritch V, Jacobson KA, Stevens RC, Wu B, Zhao Q | 10.1038/NATURE13083 | 2014-03-26 | Yes | |
OPSD | Rhodopsin | Opsins | A | Japanese flying squid | X-ray | 4WW3 | 4WW3_refined | 2.8 | A | Inactive | 9 | 78 | - | - | - | - | - | - |
Retinal (all-trans)
|
small-molecule | Agonist | - | - | No | No | Murakami M, Kouyama T | 10.1371/JOURNAL.PONE.0126970 | 2015-06-17 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 5EN0 | - | 2.8 | A | Active | 100 | 94 | Gi/o | αgust | Only H5 | 3 | - | - |
Retinal (all-trans)
|
small-molecule | Agonist | - | - | No | No | Singhal A, Guo Y, Matkovic M, Schertler G, Deupi X, Yan EC, Standfuss J | 10.15252/EMBR.201642671 | 2016-08-10 | Yes | |
PAR2 | PAR2 | Proteinase-activated | A | Human | X-ray | 5NJ6 | - | 4.0 | A | Active | 59 | 74 | - | - | - | - | BRIL | Fab3949 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Cheng RKY, Fiez-Vandal C, Schlenker O, Edman K, Aggeler B, Brown DG, Brown GA, Cooke RM, Dumelin CE, Dore AS, Geschwindner S, Grebner C, Hermansson NO, Jazayeri A, Johansson P, Leong L, Prihandoko R, Rappas M, Soutter H, Snijder A, Sundstrom L, Tehan B, Thornton P, Troast D, Wiggin G, Zhukov A, Marshall FH, Dekker N | 10.1038/NATURE22309 | 2017-05-03 | Yes | |
EDNRB | ETB | Endothelin | A | Human | X-ray | 5XPR | 5XPR_refined | 3.6 | A | Inactive | 4 | 69 | - | - | - | - | T4-Lysozyme | - |
bosentan
|
small-molecule | Antagonist | endothelin-1, endothelin-2, endothelin-3 | peptide | No | No | Shihoya W, Nishizawa T, Yamashita K, Inoue A, Hirata K, Kadji FMN, Okuta A, Tani K, Aoki J, Fujiyoshi Y, Doi T, Nureki O | 10.1038/NSMB.3450 | 2017-08-16 | Yes | |
5HT2C | 5-HT2C | 5-Hydroxytryptamine | A | Human | X-ray | 6BQH | 6BQH_refined | 2.7 | A | Inactive | 1 | 63 | - | - | - | - | BRIL | - |
ritanserin
|
small-molecule | Inverse agonist | 5-hydroxytryptamine | small-molecule | No | No | Peng Y, McCorvy JD, Harpsoe K, Lansu K, Yuan S, Popov P, Qu L, Pu M, Che T, Nikolajsen LF, Huang XP, Wu Y, Shen L, Bjorn-Yoshimoto WE, Ding K, Wacker D, Han GW, Cheng J, Katritch V, Jensen AA, Hanson MA, Zhao S, Gloriam DE, Roth BL, Stevens RC, Liu ZJ | 10.1016/j.cell.2018.01.001 | 2018-02-14 | Yes | |
5HT1B | 5-HT1B | 5-Hydroxytryptamine | A | Human | Cryo-EM | 6G79 | - | 3.8 | S | Active | 100 | 67 | Gi/o | αo | - | 59 | - | - |
donitriptan
|
small-molecule | Agonist | tryptamine, 5-hydroxytryptamine, 5-HT-moduline | small-molecule | No | No | Garcia-Nafria J, Nehme R, Edwards PC, Tate CG | 10.1038/S41586-018-0241-9 | 2018-06-20 | Yes | |
CCR5 | CCR5 | Chemokine | A | Human | Cryo-EM | 6MET | 6MET_refined | 4.5 | B | Inactive | 19 | 89 | - | - | - | - | - | T-cell surface glycoprotein CD4 |
Envelope glycoprotein gp160
|
protein | Antagonist | CCL14, CCL8, CCL13, CCL4, CCL7, CCL2, CCL5, CCL11, CCL3, CCL16 | peptide | No | No | Shaik MM, Peng H, Lu J, Rits-Volloch S, Xu C, Liao M, Chen B | 10.1038/S41586-018-0804-9 | 2018-12-12 | Yes | |
GRM5 | mGlu5 | Metabotropic glutamate | C | Human | Cryo-EM | 8T7H | - | 3.3 | A | Intermediate | - | 64 | - | - | - | - | - | Nanobody-43 |
quisqualate
|
small-molecule | Agonist | L-glutamic acid | small-molecule | No | No | - | - | 2023-10-11 | Yes | |
ADRB1 | β1 | Adrenoceptors | A | Wild turkey | X-ray | 3ZPR | 3ZPR_refined | 2.7 | B | Inactive | 0 | 61 | - | - | - | - | - | - |
CHEMBL1559535
|
small-molecule | Antagonist | - | - | No | Yes | Christopher JA, Brown J, Doré AS, Errey JC, Koglin M, Marshall FH, Myszka DG, Rich RL, Tate CG, Tehan B, Warne T, Congreve M. | 10.1021/jm400140q | 2013-04-03 | Yes | |
SMO | SMO | Frizzled | F | Human | X-ray | 4QIM | 4QIM_refined | 2.6 | A | Inactive | 7 | 45 | - | - | - | - | BRIL | - |
ANTA XV
|
small-molecule | Antagonist | - | - | No | No | Wang C, Wu H, Evron T, Vardy E, Han GW, Huang XP, Hufeisen SJ, Mangano TJ, Urban DJ, Katritch V, Cherezov V, Caron MG, Roth BL, Stevens RC | 10.1038/NCOMMS5355 | 2014-07-23 | Yes | |
OX1R | OX1 | Orexin | A | Human | X-ray | 4ZJ8 | 4ZJ8_refined | 2.8 | A | Inactive | 0 | 72 | - | - | - | - | GlgA glycogen synthase | - |
suvorexant
|
small-molecule | Antagonist | orexin-A, orexin-B | peptide | No | No | Yin J, Babaoglu K, Brautigam CA, Clark L, Shao Z, Scheuermann TH, Harrell CM, Gotter AL, Roecker AJ, Winrow CJ, Renger JJ, Coleman PJ, Rosenbaum DM | 10.1038/NSMB.3183 | 2016-03-09 | Yes | |
5HT2B | 5-HT2B | 5-Hydroxytryptamine | A | Human | X-ray | 5TVN | - | 2.9 | A | Active | 59 | 61 | - | - | - | - | BRIL | - |
Lysergide
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | No | No | Wacker D, Wang S, McCorvy JD, Betz RM, Venkatakrishnan AJ, Levit A, Lansu K, Schools ZL, Che T, Nichols DE, Shoichet BK, Dror RO, Roth BL | 10.1016/J.CELL.2016.12.033 | 2017-02-01 | Yes | |
APJ | apelin | Apelin | A | Human | X-ray | 5VBL | - | 2.6 | B | Inactive | 6 | 79 | - | - | - | - | Rubredoxin | - |
AMG3054
|
peptide | Agonist | Elabela/Toddler-21, apelin-17, [Pyr1]apelin-13, Elabela/Toddler-11, Elabela/Toddler-32, apelin-13, apelin-36, 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 | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 6AQF | 6AQF_refined | 2.5 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
ZM-241385
|
small-molecule | Antagonist | adenosine | small-molecule | No | No | Eddy MT, Lee MY, Gao ZG, White KL, Didenko T, Horst R, Audet M, Stanczak P, McClary KM, Han GW, Jacobson KA, Stevens RC, Wuthrich K | 10.1016/J.CELL.2017.12.004 | 2018-01-10 | Yes | |
NPY1R | Y1 | Neuropeptide Y | A | Human | X-ray | 5ZBQ | 5ZBQ_refined | 2.7 | A | Inactive | 1 | 80 | - | - | - | - | T4-Lysozyme | - |
CHEMBL3747822
|
small-molecule | Antagonist | peptide YY, neuropeptide Y, pancreatic polypeptide | peptide | No | No | Yang Z, Han S, Keller M, Kaiser A, Bender BJ, Bosse M, Burkert K, Kogler LM, Wifling D, Bernhardt G, Plank N, Littmann T, Schmidt P, Yi C, Li B, Ye S, Zhang R, Xu B, Larhammar D, Stevens RC, Huster D, Meiler J, Zhao Q, Beck-Sickinger AG, Buschauer A, Wu B | 10.1038/S41586-018-0046-X | 2018-04-25 | Yes | |
CCR5 | CCR5 | Chemokine | A | Human | X-ray | 6AKY | 6AKY_refined | 2.8 | A | Inactive | 19 | 81 | - | - | - | - | Rubredoxin | - |
CCR5 antagonist 34
|
small-molecule | Antagonist | CCL14, CCL8, CCL13, CCL4, CCL7, CCL2, CCL5, CCL11, CCL3, CCL16 | peptide | No | No | Peng P, Chen H, Zhu Y, Wang Z, Li J, Luo RH, Wang J, Chen L, Yang LM, Jiang H, Xie X, Wu B, Zheng YT, Liu H. | 10.1021/acs.jmedchem.8b01077 | 2018-10-24 | Yes | |
CCR2 | CCR2 | Chemokine | A | Human | X-ray | 6GPX | 6GPX_refined | 2.7 | B | Inactive | 19 | 70 | - | - | - | - | Rubredoxin | - |
MK-0812
|
small-molecule | Antagonist | CCL8, CCL13, CCL7, CCL2, CCL11, CCL24, CCL16, CCL26 | peptide | No | No | Apel AK, Cheng RKY, Tautermann CS, Brauchle M, Huang CY, Pautsch A, Hennig M, Nar H, Schnapp G | 10.1016/J.STR.2018.10.027 | 2019-01-02 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | Cryo-EM | 6OY9 | - | 3.9 | R | Active | 100 | 94 | Gi/o | αt1 | - | 64 | - | - |
Retinal (all-trans)
|
small-molecule | Agonist | - | - | No | No | Gao Y, Hu H, Ramachandran S, Erickson JW, Cerione RA, Skiniotis G | 10.1016/J.MOLCEL.2019.06.007 | 2019-07-24 | Yes | |
ADA2A | α2A | Adrenoceptors | A | Human | X-ray | 6KUY | 6KUY_refined | 3.2 | A | Inactive | 1 | 56 | - | - | - | - | BRIL | - |
(2~{S})-4-fluoranyl-2-(1~{H}-imidazol-5-yl)-1-propan-2-yl-2,3-dihydroindole
|
small-molecule | Agonist (partial) | (-)-adrenaline, (-)-noradrenaline | small-molecule | No | No | - | - | 2019-12-04 | Yes | |
CNR2 | CB2 | Cannabinoid | A | Human | X-ray | 6KPC | 6KPC_refined | 3.2 | A | Inactive | 5 | 79 | - | - | - | - | T4-Lysozyme | - |
AM12033
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | No | No | Hua T, Li X, Wu L, Iliopoulos-Tsoutsouvas C, Wang Y, Wu M, Shen L, Brust CA, Nikas SP, Song F, Song X, Yuan S, Sun Q, Wu Y, Jiang S, Grim TW, Benchama O, Stahl EL, Zvonok N, Zhao S, Bohn LM, Makriyannis A, Liu ZJ | 10.1016/J.CELL.2020.01.008 | 2020-02-12 | Yes | |
OPRK | κ | Opioid | A | Human | X-ray | 6VI4 | 6VI4_refined | 3.3 | B | Inactive | 6 | 73 | - | - | - | - | - | Nanobody-6 |
JDTic
|
small-molecule | Antagonist | [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 | Che T, English J, Krumm BE, Kim K, Pardon E, Olsen RHJ, Wang S, Zhang S, Diberto JF, Sciaky N, Carroll FI, Steyaert J, Wacker D, Roth BL | 10.1038/S41467-020-14889-7 | 2020-03-18 | Yes | |
GABR1 | GABAB1 | GABAB | C | Human | Cryo-EM | 6W2Y | - | 3.2 | B | Inactive | - | 69 | - | - | - | - | - | - |
CGP55845
1-Stearoyl-2-oleoyl-sn-glycero-3-phosphoethanolamine |
small-molecule small-molecule |
Inverse agonist NAM |
GABA | small-molecule | No | No | Papasergi-Scott MM, Robertson MJ, Seven AB, Panova O, Mathiesen JM, Skiniotis G | 10.1038/S41586-020-2469-4 | 2020-07-01 | Yes | |
SCTR | secretin | Glucagon | B1 | Human | Cryo-EM | 7D3S | 7D3S_refined | 2.9 | R | Active | 100 | 60 | Gs | αs | - | 58 | - | Nanobody-35 |
SECRETIN
|
protein | Agonist | VIP, secretin | peptide | No | No | Fukuhara S, Kobayashi K, Kusakizako T, Iida W, Kato M, Shihoya W, Nureki O | 10.1016/J.BBRC.2020.08.042 | 2020-11-04 | Yes | |
NTR1 | NTS1 | Neurotensin | A | Rat | X-ray | 6Z66 | 6Z66_refined | 3.2 | A | Intermediate | 17 | 80 | - | - | - | - | DARPin D12 | - |
Apo (no ligand)
|
none | Apo (no ligand) | 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 | |
DRD1 | D1 | Dopamine | A | Human | Cryo-EM | 7CKZ | - | 3.1 | R | Active | 100 | 62 | Gs | αs | - | 60 | - | Nanobody-35 |
dopamine
mevidalen |
small-molecule small-molecule |
Agonist PAM |
L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, 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 | |
GRM7 | mGlu7 | Metabotropic glutamate | C | Human | Cryo-EM | 7EPC | 7EPC_refined | 4.0 | B | Inactive | - | 85 | - | - | - | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | L-serine-O-phosphate, 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 | |
FZD7 | FZD7 | Frizzled | F | Human | Cryo-EM | 7EVW | - | 3.2 | R | Active | 100 | 59 | Gs | αs | - | 59 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Xu L, Chen B, Schihada H, Wright SC, Turku A, Wu Y, Han GW, Kowalski-Jahn M, Kozielewicz P, Bowin CF, Zhang X, Li C, Bouvier M, Schulte G, Xu F | 10.1038/S41422-021-00525-6 | 2021-08-04 | Yes | |
GRM1 | mGlu1 | Metabotropic glutamate | C | Human | Cryo-EM | 7DGD | 7DGD_refined | 4.0 | A | Inactive | - | 66 | - | - | - | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | L-glutamic acid | small-molecule | No | No | Zhang J, Qu L, Wu L, Tang X, Luo F, Xu W, Xu Y, Liu ZJ, Hua T | 10.1007/S13238-020-00808-5 | 2021-09-22 | Yes | |
MC4R | MC4 | Melanocortin | A | Human | Cryo-EM | 7F54 | - | 3.0 | R | Active | 100 | 82 | Gs | αs | - | 58 | - | Nanobody-35 |
afamelanotide
|
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 | |
5HT2A | 5-HT2A | 5-Hydroxytryptamine | A | Human | X-ray | 7VOD | 7VOD_refined | 3.3 | A | Inactive | 1 | 58 | - | - | - | - | BRIL | - |
cariprazine
|
small-molecule | Agonist (partial) | tryptamine, 5-hydroxytryptamine | small-molecule | No | No | Chen Z, Fan L, Wang H, Yu J, Lu D, Qi J, Nie F, Luo Z, Liu Z, Cheng J, Wang S | 10.1038/S41593-021-00971-W | 2021-12-22 | Yes | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 7LLL | - | 3.7 | R | Active | 100 | 79 | Gs | αs | - | 59 | - | Nanobody-35 |
exendin-4
|
peptide | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | No | No | Deganutti G, Liang YL, Zhang X, Khoshouei M, Clydesdale L, Belousoff MJ, Venugopal H, Truong TT, Glukhova A, Keller AN, Gregory KJ, Leach K, Christopoulos A, Danev R, Reynolds CA, Zhao P, Sexton PM, Wootten D | 10.1038/S41467-021-27760-0 | 2022-01-12 | Yes | |
LT4R1 | BLT1 | Leukotriene | A | Human | Cryo-EM | 7VKT | 7VKT_refined | 2.9 | A | Active | 100 | 82 | Gi/o | αi1 | - | 64 | - | scFv16 |
LTB4
|
small-molecule | Agonist | 12R-HETE, LTB4, 20-hydroxy-LTB4 | small-molecule | No | No | Wang N, He X, Zhao J, Jiang H, Cheng X, Xia Y, Eric Xu H, He Y | 10.1038/S41467-022-28820-9 | 2022-03-09 | Yes | |
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-(7-36) 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 | 2022-03-02 | Yes | |
ADRB1 | β1 | Adrenoceptors | A | Wild turkey | Cryo-EM | 7S0G | - | 3.9 | R | Active | 100 | 57 | Gs | αs | Gi1-Gs chimera | 56 | - | - |
LEVISOPRENALINE
|
small-molecule | Agonist | - | - | No | No | Alegre KO, Paknejad N, Su M, Lou JS, Huang J, Jordan KD, Eng ET, Meyerson JR, Hite RK, Huang XY | 10.1038/S41594-021-00679-2 | 2021-11-17 | Yes | |
DRD1 | D1 | Dopamine | A | Human | Cryo-EM | 7F1Z | - | 3.5 | F | Active | 100 | 62 | Gs | αs | - | 60 | - | - |
dopamine
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | No | No | Teng X, Chen S, Wang Q, Chen Z, Wang X, Huang N, Zheng S | 10.1126/SCIADV.ABO4158 | 2022-06-15 | Yes | |
SMO | SMO | Frizzled | F | Human | X-ray | 7ZI0 | 7ZI0_refined | 3.0 | A | Inactive | 4 | 61 | - | - | - | - | BRIL | - |
3-chloro-N-[trans-4-(methylamino)cyclohexyl]-N-{[3-(pyridin-4-yl)phenyl]methyl}-1-benzothiophene-2-carboxamide
|
small-molecule | Antagonist | - | - | No | No | Kinnebrew M, Woolley RE, Ansell TB, Byrne EFX, Frigui S, Luchetti G, Sircar R, Nachtergaele S, Mydock-McGrane L, Krishnan K, Newstead S, Sansom MSP, Covey DF, Siebold C, Rohatgi R | 10.1126/SCIADV.ABM5563 | 2022-06-15 | Yes | |
MRGRD | MRGPRD | A orphans | A | Human | Cryo-EM | 7Y15 | 7Y15_refined | 2.9 | R | Active | 100 | 82 | Gi/o | αi1 | - | 62 | BRIL | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | β-alanine | small-molecule | No | No | Suzuki S, Iida M, Hiroaki Y, Tanaka K, Kawamoto A, Kato T, Oshima A | 10.1038/S42003-022-03668-3 | 2022-07-20 | Yes | |
S1PR5 | S1P5 | Lysophospholipid (S1P) | A | Human | X-ray | 7YXA | 7YXA_refined | 2.2 | A | Inactive | 1 | 72 | - | - | - | - | BRIL | - |
4-[6-(2-naphthalen-1-ylethoxy)-2,3,4,5-tetrahydro-1H-3-benzazepin-3-ium-3-yl]butanoic acid
|
small-molecule | Antagonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | No | No | Lyapina E, Marin E, Gusach A, Orekhov P, Gerasimov A, Luginina A, Vakhrameev D, Ergasheva M, Kovaleva M, Khusainov G, Khorn P, Shevtsov M, Kovalev K, Bukhdruker S, Okhrimenko I, Popov P, Hu H, Weierstall U, Liu W, Cho Y, Gushchin I, Rogachev A, Bourenkov G, Park S, Park G, Hyun HJ, Park J, Gordeliy V, Borshchevskiy V, Mishin A, Cherezov V | 10.1038/S41467-022-32447-1 | 2022-08-10 | Yes | |
HRH3 | H3 | Histamine | A | Human | X-ray | 7F61 | 7F61_refined | 2.6 | A | Inactive | 6 | 68 | - | - | - | - | BRIL | - |
N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]cyclobutane-1-carboxamide
|
small-molecule | Antagonist | histamine | small-molecule | No | No | Peng X, Yang L, Liu Z, Lou S, Mei S, Li M, Chen Z, Zhang H | 10.1038/S41467-022-33880-Y | 2022-10-26 | Yes | |
OPRM | μ | Opioid | A | Mouse | Cryo-EM | 7U2K | - | 3.3 | D | Active | 100 | 71 | Gi/o | αi1 | - | 61 | - | - |
CHEMBL147044
|
small-molecule | Agonist | - | - | No | No | Faouzi A, Wang H, Zaidi SA, DiBerto JF, Che T, Qu Q, Robertson MJ, Madasu MK, El Daibani A, Varga BR, Zhang T, Ruiz C, Liu S, Xu J, Appourchaux K, Slocum ST, Eans SO, Cameron MD, Al-Hasani R, Pan YX, Roth BL, McLaughlin JP, Skiniotis G, Katritch V, Kobilka BK, Majumdar S | 10.1038/S41586-022-05588-Y | 2022-12-07 | Yes | |
GPR88 | GPR88 | A orphans | A | Human | Cryo-EM | 7WZ4 | - | 3.0 | R | Active | 100 | 61 | Gi/o | αi1 | - | 61 | - | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Chen G, Xu J, Inoue A, Schmidt MF, Bai C, Lu Q, Gmeiner P, Liu Z, Du Y | 10.1038/S41467-022-30081-5 | 2022-10-26 | Yes | |
LPAR1 | LPA1 | Lysophospholipid (LPA) | A | Human | Cryo-EM | 7YU7 | - | 3.8 | R | Active | 100 | 80 | Gi/o | αi1 | - | 63 | - | scFv16 |
[(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate
|
small-molecule | Agonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | No | No | Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O | 10.1038/S41467-022-33121-2 | 2022-10-05 | Yes | |
AGTR1 | AT1 | Angiotensin | A | Human | Cryo-EM | 7F6G | 7F6G_refined | 2.9 | A | Active | 100 | 86 | Gq/11 | αq | - | 97 | - | - |
SAR1-AngII
|
peptide | Agonist | angiotensin IV, angiotensin II, angiotensin III, angiotensin A | peptide | No | No | - | - | 2023-03-29 | Yes | |
EDNRB | ETB | Endothelin | A | Human | Cryo-EM | 8HBD | 8HBD_refined | 3.0 | R | Active | 100 | 68 | Gi/o | αi1 | - | 61 | - | scFv16 |
sovateltide
|
peptide | Agonist | endothelin-1, endothelin-2, endothelin-3 | peptide | No | No | - | - | 2023-03-22 | Yes | |
TAAR9 | TAAR9 | A orphans | A | Mouse | Cryo-EM | 8IW1 | - | 3.4 | R | Active | 100 | 78 | Gs | αolf | Golf-Gi chimera | 59 | - | scFv16 |
2-Phenylethanaminium
|
small-molecule | Agonist | - | - | No | No | Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP | 10.1038/S41586-023-06106-4 | 2023-05-31 | Yes | |
GALR1 | GAL1 | Galanin | A | Human | Cryo-EM | 7XJJ | 7XJJ_refined | 3.3 | E | Active | 100 | 77 | Gi/o | αo | - | 61 | - | scFv16 |
galanin
|
peptide | Agonist | galanin-like peptide, galanin | peptide | No | No | - | - | 2023-05-03 | Yes | |
PTH1R | PTH1 | Parathyroid hormone | B1 | Human | Cryo-EM | 8FLT | - | 3.0 | R | Active | 100 | 45 | Gs | αs | - | 59 | - | Nanobody-35 |
M-PTH(1-14)
|
peptide | Agonist | 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 | |
CALCR | CT | Calcitonin | B1 | Human | Cryo-EM | 8F2B | - | 2.0 | R | Active | 100 | 78 | Gs | αs | - | 58 | - | Nanobody-35 RAMP3 |
Pramlintide analogue San45
|
peptide | Agonist | adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), 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 | |
NTR1 | NTS1 | Neurotensin | A | Human | Cryo-EM | 8JPC | - | 3.1 | R | Active | 100 | 71 | Gq/11 | αq | GRK2 bound | 88 | - | GRK2 |
JMV431
CHEMBL4576388 |
peptide small-molecule |
Agonist PAM |
large neurotensin, large neuromedin N, neurotensin, neuromedin N | peptide | No | No | Duan J, Liu H, Zhao F, Yuan Q, Ji Y, Cai X, He X, Li X, Li J, Wu K, Gao T, Zhu S, Lin S, Wang MW, Cheng X, Yin W, Jiang Y, Yang D, Xu HE | 10.1038/S41586-023-06395-9 | 2023-08-09 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 8A2O | - | 3.5 | A | Inactive | 0 | 71 | - | - | - | - | BRIL | - |
theophylline
|
small-molecule | Antagonist | adenosine | small-molecule | No | No | Birch J, Kwan TOC, Judge PJ, Axford D, Aller P, Butryn A, Reis RI, Bada Juarez JF, Vinals J, Owen RL, Nango E, Tanaka R, Tono K, Joti Y, Tanaka T, Owada S, Sugahara M, Iwata S, Orville AM, Watts A, Moraes I | 10.1107/S1600576723006428 | 2023-08-30 | Yes | |
HRH4 | H4 | Histamine | A | Human | Cryo-EM | 8HN8 | - | 3.0 | R | Active | 100 | 71 | Gi/o | αi1 | - | 62 | - | scFv16 |
histamine
|
small-molecule | Agonist | histamine, CCL16 | small-molecule | No | No | - | - | 2023-12-20 | Yes | |
HCAR3 | HCA3 | Hydroxycarboxylic acid | A | Human | Cryo-EM | 8IHJ | 8IHJ_refined | 3.1 | R | Active | 100 | 73 | Gi/o | αi1 | - | 62 | BRIL | scFv16 |
(5S)-5-methyl-4-oxo-5-phenylfuran-2-carboxylic acid
|
small-molecule | Agonist | 3-hydroxyoctanoic 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 | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 8JIS | 8JIS_refined | 2.5 | R | Active | 100 | 83 | Gs | αs | - | 60 | - | Nanobody-35 |
Dual-agonist peptide P15
|
peptide | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | 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 | 2023-11-08 | Yes | |
GRM5 | mGlu5 | Metabotropic glutamate | C | Human | Cryo-EM | 8TAO | - | 2.9 | A | Active | - | 64 | - | - | - | - | - | Nanobody-43 |
quisqualate
CDPPB |
small-molecule small-molecule |
Agonist | L-glutamic acid | small-molecule | No | No | Kumar KK, Wang H, Habrian C, Latorraca NR, Xu J, O'Brien ES, Zhang C, Montabana E, Koehl A, Marqusee S, Isacoff EY, Kobilka BK | 10.1101/2023.08.29.555158 | 2023-10-11 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 4BEZ | 4BEZ_refined | 3.3 | A | Active | 97 | 94 | - | - | - | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Singhal A, Ostermaier MK, Vishnivetskiy SA, Panneels V, Homan KT, Tesmer JJ, Veprintsev D, Deupi X, Gurevich VV, Schertler GF, Standfuss J | 10.1038/EMBOR.2013.44 | 2013-04-24 | Yes | |
NTR1 | NTS1 | Neurotensin | A | Rat | X-ray | 4BV0 | 4BV0_refined | 3.1 | A | Inactive | 3 | 70 | - | - | - | - | - | - |
neurotensin
|
peptide | Agonist | neurotensin, neuromedin N | peptide | No | No | Egloff P, Hillenbrand M, Klenk C, Batyuk A, Heine P, Balada S, Schlinkmann KM, Scott DJ, Schutz M, Pluckthun A | 10.1073/PNAS.1317903111 | 2014-01-29 | Yes | |
ADRB1 | β1 | Adrenoceptors | A | Wild turkey | X-ray | 5F8U | 5F8U_refined | 3.4 | A | Inactive | 0 | 57 | - | - | - | - | - | - |
(S)-Cyanopindolol
|
small-molecule | Antagonist | - | - | No | No | Leslie AG, Warne T, Tate CG | 10.1038/NSMB.3130 | 2015-12-23 | Yes | |
EDNRB | ETB | Endothelin | A | Human | X-ray | 5GLH | 5GLH_refined | 2.8 | A | Inactive | 17 | 66 | - | - | - | - | T4-Lysozyme | - |
ENDOTHELIN
|
protein | Agonist | endothelin-1, endothelin-2, endothelin-3 | peptide | No | No | Shihoya W, Nishizawa T, Okuta A, Tani K, Dohmae N, Fujiyoshi Y, Nureki O, Doi T | 10.1038/nature19319 | 2016-09-07 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5N2R | 5N2R_refined | 2.8 | A | Inactive | 0 | 71 | - | - | - | - | BRIL | - |
PSB36
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | Cheng RKY, Segala E, Robertson N, Deflorian F, Dore AS, Errey JC, Fiez-Vandal C, Marshall FH, Cooke RM | 10.1016/j.str.2017.06.012 | 2017-07-26 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5OM4 | 5OM4_refined | 2.0 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
CHEMBL2024114
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | Rucktooa P, Cheng RKY, Segala E, Geng T, Errey JC, Brown GA, Cooke RM, Marshall FH, Dore AS | 10.1038/S41598-017-18570-W | 2018-01-17 | Yes | |
Q80KM9 | US28 | Unclassified | A | strain AD169 | X-ray | 5WB2 | 5WB2_refined | 3.5 | A | Active | 100 | 82 | - | - | - | - | - | Nanobody |
CX3CL1
|
peptide | Agonist | - | - | No | No | - | - | 2018-06-13 | Yes | |
PTH1R | PTH1 | Parathyroid hormone | B1 | Human | Cryo-EM | 6NBH | - | 3.5 | R | Active | 100 | 64 | Gs | αs | - | 57 | - | Nanobody-35 |
Long-acting parathyroid hormone analog
|
peptide | Agonist | 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 | |
OX2R | OX2 | Orexin | A | Human | X-ray | 6TPJ | 6TPJ_refined | 2.7 | A | Inactive | 0 | 68 | - | - | - | - | GlgA glycogen synthase | - |
suvorexant
|
small-molecule | Antagonist | orexin-A, orexin-B | peptide | No | No | Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA. | 10.1021/acs.jmedchem.9b01787 | 2020-01-01 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 6OBA | 6OBA_refined | 3.1 | A | Inactive | 0 | 68 | - | - | - | - | T4-Lysozyme | - |
CHEMBL1160734
AS408 |
small-molecule small-molecule |
Antagonist NAM |
L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline | small-molecule | No | No | Liu X, Kaindl J, Korczynska M, Stossel A, Dengler D, Stanek M, Hubner H, Clark MJ, Mahoney J, Matt RA, Xu X, Hirata K, Shoichet BK, Sunahara RK, Kobilka BK, Gmeiner P | 10.1038/S41589-020-0549-2 | 2020-03-25 | Yes | |
GABR2 | GABAB2 | GABAB | C | Human | Cryo-EM | 7C7Q | - | 3.0 | B | Active | - | 71 | - | - | - | - | - | - |
(-)-baclofen
BHFF |
small-molecule small-molecule |
Agonist PAM |
- | - | No | No | Mao C, Shen C, Li C, Shen DD, Xu C, Zhang S, Zhou R, Shen Q, Chen LN, Jiang Z, Liu J, Zhang Y | 10.1038/S41422-020-0350-5 | 2020-07-01 | Yes | |
GNRHR | GnRH1 | Gonadotrophin-releasing hormone | A | Human | X-ray | 7BR3 | 7BR3_refined | 2.8 | A | Inactive | 36 | 84 | - | - | - | - | GlgA glycogen synthase | - |
elagolix
|
small-molecule | Antagonist | GnRH I, GnRH II | peptide | No | No | Yan W, Cheng L, Wang W, Wu C, Yang X, Du X, Ma L, Qi S, Wei Y, Lu Z, Yang S, Shao Z | 10.1038/S41467-020-19109-W | 2020-10-07 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | Cryo-EM | 7DHR | 7DHR_refined | 3.8 | R | Active | 100 | 69 | Gs | αs | - | 49 | - | Nanobody-35 |
LEVISOPRENALINE
|
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 | 7JV5 | - | 3.0 | R | Active | 100 | 63 | Gs | αs | - | 60 | - | Nanobody-35 |
CHEMBL1160787
|
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 | |
PE2R2 | EP2 | Prostanoid | A | Human | Cryo-EM | 7CX3 | - | 2.8 | R | Active | 100 | 74 | Gs | αs | - | 58 | - | Nanobody-35 |
taprenepag
|
small-molecule | Agonist | thromboxane A2, PGF2α, PGI2, PGD2, PGE1, PGE2 | small-molecule | No | No | Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y | 10.1126/SCIADV.ABF1268 | 2021-05-05 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | Cryo-EM | 7MTA | 7MTA_refined | 4.1 | R | Active | 97 | 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 | desulfated cholecystokinin-8, CCK-58, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8 | peptide | No | No | Liu Q, Yang D, Zhuang Y, Croll TI, Cai X, Dai A, He X, Duan J, Yin W, Ye C, Zhou F, Wu B, Zhao Q, Xu HE, Wang MW, Jiang Y | 10.1038/S41589-021-00841-3 | 2021-08-25 | Yes | |
GASR | CCK2 | Cholecystokinin | A | Human | Cryo-EM | 7F8W | 7F8W_refined | 3.1 | R | Active | 100 | 62 | Gq/11 | αq | Gq-Gi1 chimera | 62 | - | scFv16 |
desulfated gastrin-17
|
peptide | Agonist | desulfated gastrin-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 | Zhang X, He C, Wang M, Zhou Q, Yang D, Zhu Y, Feng W, Zhang H, Dai A, Chu X, Wang J, Yang Z, Jiang Y, Sensfuss U, Tan Q, Han S, Reedtz-Runge S, Xu HE, Zhao S, Wang MW, Wu B, Zhao Q | 10.1038/S41589-021-00866-8 | 2021-10-13 | Yes | |
MRGX2 | MRGPRX2 | A orphans | A | Human | Cryo-EM | 7VV3 | - | 3.0 | R | Active | 100 | 79 | Gi/o | αi1 | - | 62 | - | scFv16 |
Cortistatin 14
|
peptide | Agonist | PAMP-20 | peptide | No | No | Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP | 10.1038/S41586-021-04077-Y | 2021-12-01 | Yes | |
US28 | US28 | Unclassified | A | strain AD169 | Cryo-EM | 7RKF | - | 4.0 | R | Active | 100 | 84 | Gq/11 | α11 | - | 97 | - | scFv16 |
Fractalkine
|
peptide | Agonist | - | - | No | No | Tsutsumi N, Maeda S, Qu Q, Vogele M, Jude KM, Suomivuori CM, Panova O, Waghray D, Kato HE, Velasco A, Dror RO, Skiniotis G, Kobilka BK, Garcia KC | 10.1126/SCIADV.ABL5442 | 2022-01-26 | Yes | |
GIPR | GIP | Glucagon | B1 | Human | Cryo-EM | 7FIY | - | 3.4 | R | Active | 100 | 77 | Gs | αs | - | 60 | - | Nanobody-35 |
tirzepatide
|
peptide | Agonist | gastric inhibitory polypeptide | peptide | No | No | Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW | 10.1038/S41467-022-28683-0 | 2022-03-02 | Yes | |
AGRG2 | ADGRG2 | ADGRG | B2 | Mouse | Cryo-EM | 7WUI | - | 3.1 | R | Active | 100 | 24 | Gs | αs | Mini-Gs | 58 | - | - |
IP15
|
peptide | Agonist | - | - | No | No | Xiao P, Guo S, Wen X, He QT, Lin H, Huang SM, Gou L, Zhang C, Yang Z, Zhong YN, Yang CC, Li Y, Gong Z, Tao XN, Yang ZS, Lu Y, Li SL, He JY, Wang C, Zhang L, Kong L, Sun JP, Yu X | 10.1038/S41586-022-04590-8 | 2022-04-27 | Yes | |
DRD1 | D1 | Dopamine | A | Human | Cryo-EM | 7F23 | - | 3.6 | F | Active | 100 | 62 | Gs | αs | - | 60 | - | Nanobody-35 |
dopamine
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | No | No | Teng X, Chen S, Wang Q, Chen Z, Wang X, Huang N, Zheng S | 10.1126/SCIADV.ABO4158 | 2022-06-15 | Yes | |
5HT4R | 5-HT4 | 5-Hydroxytryptamine | A | Human | Cryo-EM | 7XT9 | - | 3.2 | R | Active | 100 | 76 | Gs | αs | - | 60 | BRIL | - |
5-hydroxytryptamine
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | No | No | Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE | 10.1016/J.MOLCEL.2022.05.031 | 2022-07-27 | Yes | |
ADRB1 | β1 | Adrenoceptors | A | Wild turkey | Cryo-EM | 8DCS | - | 2.5 | R | Active | 100 | 57 | Gs | αs | - | 51 | T4-Lysozyme | Nanobody-35 |
4-{[(2S)-3-(tert-butylamino)-2-hydroxypropyl]oxy}-3H-indole-2-carbonitrile
|
small-molecule | Agonist | - | - | No | No | Su M, Paknejad N, Zhu L, Wang J, Do HN, Miao Y, Liu W, Hite RK, Huang XY | 10.1038/S41467-022-31823-1 | 2022-07-27 | Yes | |
PTH1R | PTH1 | Parathyroid hormone | B1 | Human | Cryo-EM | 7VVJ | 7VVJ_refined | 3.2 | R | Active | 100 | 62 | Gs | αs | - | 59 | - | Nanobody-35 |
PTHrP[1-36]
|
peptide | Agonist | 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 | 7VIG | 7VIG_refined | 2.9 | F | Active | 100 | 73 | Gi/o | αi1 | - | 63 | - | scFv16 |
icanbelimod
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | No | No | Yu L, He L, Gan B, Ti R, Xiao Q, Hu H, Zhu L, Wang S, Ren R | 10.1073/PNAS.2117716119 | 2022-09-28 | Yes | |
GPR17 | GPR17 | A orphans | A | Human | Cryo-EM | 7Y89 | - | 3.0 | A | Active | 100 | 78 | Gi/o | αi1 | - | 58 | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | UDP, UDP-glucose, UDP-galactose, LTC4, LTD4, LTE4, ATP | small-molecule | No | No | Ye F, Wong TS, Chen G, Zhang Z, Zhang B, Gan S, Gao W, Li J, Wu Z, Pan X, Du Y | 10.1002/MCO2.159 | 2022-10-12 | Yes | |
OPRM | μ | Opioid | A | Human | Cryo-EM | 8EFL | 8EFL_refined | 3.2 | R | Active | 100 | 72 | Gi/o | αi1 | - | 64 | - | scFv16 |
CHEMBL4452384
|
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 | |
C5AR1 | C5a1 | Complement peptide | A | Human | Cryo-EM | 7Y67 | 7Y67_refined | 2.8 | D | Active | 100 | 79 | Gi/o | αi1 | - | 63 | - | scFv16 |
C089
|
peptide | Agonist | 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 | |
GPR20 | GPR20 | A orphans | A | Human | Cryo-EM | 8HSC | - | 3.2 | R | Active | 100 | 76 | Gi/o | αi1 | - | 62 | BRIL | Antibody fab fragment light chain Antibody fab fragment heavy chain scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | 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 | |
TAAR9 | TAAR9 | A orphans | A | Mouse | Cryo-EM | 8IW9 | - | 3.1 | R | Active | 100 | 89 | Gs | αs | Mini-Gs | 59 | - | scFv16 Nanobody-35 |
Cadaverine
|
small-molecule | Agonist | - | - | No | No | Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP | 10.1038/S41586-023-06106-4 | 2023-05-31 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 8CIC | - | 2.1 | A | Inactive | 0 | 71 | - | - | - | - | BRIL | - |
AB928
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | Claff T, Schlegel JG, Voss JH, Vaassen VJ, Weisse RH, Cheng RKY, Markovic-Mueller S, Bucher D, Strater N, Muller CE | 10.1038/S42004-023-00894-6 | 2023-05-31 | Yes | |
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 | 8IUM | - | 3.1 | R | Active | 100 | 82 | Gq/11 | αq | - | 60 | - | scFv16 Nanobody-35 |
tafluprost acid
|
small-molecule | Agonist | thromboxane A2, PGF2α, PGI2, PGD2, 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 |
L-glutamic acid
ADX88178 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 | 8IJ3 | 8IJ3_refined | 3.3 | A | Active | 100 | 80 | Gi/o | αi1 | - | 61 | - | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | 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 | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 8JIP | 8JIP_refined | 2.9 | R | Active | 100 | 83 | Gs | αs | - | 62 | - | Nanobody-35 |
MEDI0382
|
peptide | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | 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 | |
NK1R | NK1 | Tachykinin | A | Human | Cryo-EM | 8U26 | 8U26_refined | 2.5 | R | Active | 100 | 70 | Gs | αs | - | 55 | - | Nanobody-35 |
substance P
|
peptide | Agonist | neuropeptide-γ, neurokinin A, neuropeptide K, neurokinin B, hemokinin 1, substance P | peptide | No | No | Chen M, Schmid MF, Chiu W | 10.1038/S41592-023-02082-9 | 2023-11-15 | Yes | |
SMO | SMO | Frizzled | F | Human | X-ray | 4JKV | 4JKV_refined | 2.5 | A | Inactive | 0 | 44 | - | - | - | - | BRIL | - |
taladegib
|
small-molecule | Antagonist | - | - | No | No | Wang C, Wu H, Katritch V, Han GW, Huang XP, Liu W, Siu FY, Roth BL, Cherezov V, Stevens RC | 10.1038/NATURE12167 | 2013-04-24 | Yes | |
LPAR1 | LPA1 | Lysophospholipid (LPA) | A | Human | X-ray | 4Z34 | 4Z34_refined | 3.0 | A | Inactive | 1 | 80 | - | - | - | - | BRIL | - |
ONO-9780307
|
small-molecule | Antagonist | 1-O-Oleoyl-D-glycerol 3-phosphoric acid | small-molecule | No | No | Chrencik JE, Roth CB, Terakado M, Kurata H, Omi R, Kihara Y, Warshaviak D, Nakade S, Asmar-Rovira G, Mileni M, Mizuno H, Griffith MT, Rodgers C, Han GW, Velasquez J, Chun J, Stevens RC, Hanson MA | 10.1016/J.CELL.2015.06.002 | 2015-06-03 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5IUB | 5IUB_refined | 2.1 | A | Inactive | 0 | 71 | - | - | - | - | BRIL | - |
CHEMBL184061
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | Segala E, Guo D, Cheng RK, Bortolato A, Deflorian F, Doré AS, Errey JC, Heitman LH, IJzerman AP, Marshall FH, Cooke RM. | 10.1021/acs.jmedchem.6b00653 | 2016-06-29 | Yes | |
PAR2 | PAR2 | Proteinase-activated | A | Human | X-ray | 5NDZ | - | 3.6 | A | Active | 59 | 74 | - | - | - | - | BRIL | - |
AZ3451
|
small-molecule | Allosteric antagonist | - | - | No | Yes | - | - | 2017-05-03 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5NM2 | 5NM2_refined | 2.0 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
ZM-241385
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | Weinert T, Olieric N, Cheng R, Brunle S, James D, Ozerov D, Gashi D, Vera L, Marsh M, Jaeger K, Dworkowski F, Panepucci E, Basu S, Skopintsev P, Dore AS, Geng T, Cooke RM, Liang M, Prota AE, Panneels V, Nogly P, Ermler U, Schertler G, Hennig M, Steinmetz MO, Wang M, Standfuss J | 10.1038/S41467-017-00630-4 | 2017-09-27 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 6FKD | 6FKD_refined | 2.5 | A | Active | 97 | 94 | - | - | - | - | - | - |
5-chloro-2-(2-oxo-2-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-ylethyl)-3H-pyridin-6-one
|
small-molecule | Agonist | - | - | No | No | Mattle D, Kuhn B, Aebi J, Bedoucha M, Kekilli D, Grozinger N, Alker A, Rudolph MG, Schmid G, Schertler GFX, Hennig M, Standfuss J, Dawson RJP | 10.1073/PNAS.1718084115 | 2018-04-04 | Yes | |
ADRB1 | β1 | Adrenoceptors | A | Wild turkey | X-ray | 6H7L | 6H7L_refined | 2.7 | A | Active | 99 | 60 | - | - | - | - | Thioredoxin 1 | Camelid antibody fragment Nb6B9 |
Dobutamine
|
small-molecule | Agonist | - | - | No | No | Warne T, Edwards PC, Dore AS, Leslie AGW, Tate CG | 10.1126/SCIENCE.AAU5595 | 2018-10-17 | Yes | |
GRM5 | mGlu5 | Metabotropic glutamate | C | Human | Cryo-EM | 6N52 | 6N52_refined | 4.0 | A | Inactive | - | 64 | - | - | - | - | - | Nanobody-43 |
Apo (no ligand)
|
none | Apo (no ligand) | L-glutamic acid | small-molecule | No | No | Koehl A, Hu H, Feng D, Sun B, Zhang Y, Robertson MJ, Chu M, Kobilka TS, Laeremans T, Steyaert J, Tarrasch J, Dutta S, Fonseca R, Weis WI, Mathiesen JM, Skiniotis G, Kobilka BK | 10.1038/S41586-019-0881-4 | 2019-01-23 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | Cryo-EM | 6OYA | - | 3.3 | R | Active | 100 | 94 | Gi/o | αt1 | - | 59 | - | Camelid antibody VHH fragment |
Retinal (all-trans)
|
small-molecule | Agonist | - | - | No | No | Gao Y, Hu H, Ramachandran S, Erickson JW, Cerione RA, Skiniotis G | 10.1016/J.MOLCEL.2019.06.007 | 2019-07-24 | Yes | |
NTR1 | NTS1 | Neurotensin | A | Human | Cryo-EM | 6PWC | 6PWC_refined | 4.9 | R | Active | 100 | 77 | Beta | Beta-arrestin-1 | - | 84 | - | Fab30 heavy chain Fab30 light chain |
CHEMBL48981
|
protein | Agonist | large neurotensin, large neuromedin N, neurotensin, neuromedin N | peptide | No | No | Yin W, Li Z, Jin M, Yin YL, de Waal PW, Pal K, Yin Y, Gao X, He Y, Gao J, Wang X, Zhang Y, Zhou H, Melcher K, Jiang Y, Cong Y, Edward Zhou X, Yu X, Eric Xu H | 10.1038/S41422-019-0256-2 | 2019-12-04 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 6NWE | - | 2.7 | A | Active | 100 | 94 | Gi/o | αt1 | Only H5 | 3 | - | - |
B-Octylglucoside
|
small-molecule | unknown | - | - | No | No | - | - | 2020-02-12 | Yes | |
GLR | glucagon | Glucagon | B1 | Human | Cryo-EM | 6LMK | 6LMK_refined | 3.7 | R | Active | 100 | 83 | Gs | αs | - | 59 | - | Nanobody-35 |
glucagon
|
peptide | Agonist | glucagon | peptide | No | No | 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 | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 6X18 | - | 2.1 | R | Active | 100 | 83 | Gs | αs | - | 90 | - | Nanobody-35 |
CHEMBL410972
|
protein | 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 | |
OX2R | OX2 | Orexin | A | Human | Cryo-EM | 7L1U | - | 3.2 | R | Active | 100 | 63 | Gs | αs | Engineered G alpha | 58 | - | scFv16 |
Orexin-A
|
peptide | Agonist | orexin-A, orexin-B | peptide | No | No | Hong C, Byrne NJ, Zamlynny B, Tummala S, Xiao L, Shipman JM, Partridge AT, Minnick C, Breslin MJ, Rudd MT, Stachel SJ, Rada VL, Kern JC, Armacost KA, Hollingsworth SA, O'Brien JA, Hall DL, McDonald TP, Strickland C, Brooun A, Soisson SM, Hollenstein K | 10.1038/S41467-021-21087-6 | 2021-02-10 | Yes | |
MC4R | MC4 | Melanocortin | A | Human | Cryo-EM | 7AUE | 7AUE_refined | 3.0 | R | Active | 100 | 79 | Gs | αs | - | 59 | - | scFv16 |
setmelanotide
|
peptide | Agonist | β-MSH, α-MSH, agouti-related protein, γ-MSH, ACTH | peptide | No | No | Israeli H, Degtjarik O, Fierro F, Chunilal V, Gill AK, Roth NJ, Botta J, Prabahar V, Peleg Y, Chan LF, Ben-Zvi D, McCormick PJ, Niv MY, Shalev-Benami M | 10.1126/SCIENCE.ABF7958 | 2021-04-28 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | Cryo-EM | 7MT9 | 7MT9_refined | 7.0 | R | Active | 97 | 93 | - | - | - | - | - | 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 | |
PTH2R | PTH2 | Parathyroid hormone | B1 | Human | Cryo-EM | 7F16 | - | 2.8 | R | Active | 100 | 68 | Gs | αs | - | 58 | - | Nanobody-35 |
TIP39
|
peptide | Agonist | PTHrP, PTHrP-(1-36), PTH, PTHrP-(1-34) (human), TIP39 | peptide | No | No | Wang X, Cheng X, Zhao L, Wang Y, Ye C, Zou X, Dai A, Cong Z, Chen J, Zhou Q, Xia T, Jiang H, Xu HE, Yang D, Wang MW | 10.1073/PNAS.2101279118 | 2021-08-18 | Yes | |
MC4R | MC4 | Melanocortin | A | Human | Cryo-EM | 7PIU | - | 2.6 | R | Active | 100 | 78 | Gs | αs | - | 48 | - | Nanobody-35 |
setmelanotide
|
peptide | Agonist | β-MSH, α-MSH, agouti-related protein, γ-MSH, ACTH | peptide | No | No | Heyder NA, Kleinau G, Speck D, Schmidt A, Paisdzior S, Szczepek M, Bauer B, Koch A, Gallandi M, Kwiatkowski D, Burger J, Mielke T, Beck-Sickinger AG, Hildebrand PW, Spahn CMT, Hilger D, Schacherl M, Biebermann H, Hilal T, Kuhnen P, Kobilka BK, Scheerer P | 10.1038/S41422-021-00569-8 | 2021-11-17 | Yes | |
5HT2A | 5-HT2A | 5-Hydroxytryptamine | A | Human | X-ray | 7VOE | 7VOE_refined | 2.9 | A | Inactive | 1 | 58 | - | - | - | - | BRIL | - |
aripiprazole
|
small-molecule | Agonist (partial) | tryptamine, 5-hydroxytryptamine | small-molecule | No | No | - | - | 2021-12-22 | Yes | |
GHSR | ghrelin | Ghrelin | A | Human | Cryo-EM | 7W2Z | 7W2Z_refined | 2.8 | R | Active | 100 | 82 | Gi/o | αo | - | 60 | - | scFv16 |
Ghrelin
|
peptide | Agonist | [des-Gln14]ghrelin, ghrelin | peptide | No | No | 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 | |
CCR1 | CCR1 | Chemokine | A | Human | Cryo-EM | 7VL9 | - | 2.6 | R | Active | 100 | 85 | Gi/o | αi1 | - | 62 | - | scFv16 |
CCL15(26-92)
|
peptide | Agonist | CCL14, CCL8, CCL13, CCL15, CCL4, CCL23, CCL7, CCL5, CCL3, CCL16 | peptide | No | No | Shao Z, Shen Q, Yao B, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Ma H, Chen ZH, Xu HE, Ying S, Zhang Y, Shen H | 10.1038/S41589-021-00918-Z | 2022-03-23 | Yes | |
AGRG1 | ADGRG1 | ADGRG | B2 | Human | Cryo-EM | 7SF8 | - | 2.7 | A | Active | 100 | 37 | 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 | 7V6A | - | 3.6 | R | Active | 100 | 58 | Gi/o | αi1 | - | 62 | - | scFv16 |
methyl 4-[4-(3-methyl-2-oxidanylidene-benzimidazol-1-yl)piperidin-1-yl]piperidine-1-carboxylate
|
small-molecule | Allosteric agonist | acetylcholine | small-molecule | No | No | Wang J, Wu M, Chen Z, Wu L, Wang T, Cao D, Wang H, Liu S, Xu Y, Li F, Liu J, Chen N, Zhao S, Cheng J, Wang S, Hua T | 10.1038/S41467-022-30595-Y | 2022-05-11 | Yes | |
NTR1 | NTS1 | Neurotensin | A | Human | Cryo-EM | 7UL2 | 7UL2_refined | 2.4 | R | Inactive | 6 | 69 | - | - | - | - | - | Nanobody-6 |
meclinertant
|
small-molecule | Inverse agonist | large neurotensin, large neuromedin N, neurotensin, neuromedin N | peptide | No | No | Robertson MJ, Papasergi-Scott MM, He F, Seven AB, Meyerowitz JG, Panova O, Peroto MC, Che T, Skiniotis G | 10.1038/S41594-022-00859-8 | 2022-06-29 | Yes | |
5HT5A | 5-HT5A | 5-Hydroxytryptamine | A | Human | X-ray | 7UM4 | 7UM4_refined | 2.8 | A | Inactive | 36 | 71 | - | - | - | - | PGS | - |
CHEMBL3654198
|
small-molecule | Antagonist | 5-hydroxytryptamine | small-molecule | No | No | Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL | 10.1038/S41594-022-00796-6 | 2022-07-20 | Yes | |
CX3C1 | CX3CR1 | Chemokine | A | Human | Cryo-EM | 7XBX | - | 3.4 | R | Active | 19 | 81 | Gi/o | αi1 | - | 61 | - | - |
CX3CL1
|
peptide | Agonist | CX3CL1 | peptide | No | No | - | - | 2022-07-13 | Yes | |
FPR1 | FPR1 | Formylpeptide | A | Human | Cryo-EM | 7VFX | 7VFX_refined | 2.8 | R | Active | 100 | 84 | Gi/o | αi1 | - | 62 | - | scFv16 |
Peptide agonist fMet-Ile-Phe-Leu
|
peptide | Agonist | fMet-Leu-Phe, cathepsin G, annexin I, spinorphin | peptide | No | No | Chen G, Wang X, Liao Q, Ge Y, Jiao H, Chen Q, Liu Y, Lyu W, Zhu L, van Zundert GCP, Robertson MJ, Skiniotis G, Du Y, Hu H, Ye RD | 10.1038/S41467-022-32822-Y | 2022-09-21 | Yes | |
OX2R | OX2 | Orexin | A | Human | X-ray | 7XRR | 7XRR_refined | 2.9 | A | Inactive | 0 | 70 | - | - | - | - | - | - |
lemborexant
|
small-molecule | Antagonist | orexin-A, orexin-B | peptide | No | No | Asada H, Im D, Hotta Y, Yasuda S, Murata T, Suno R, Iwata S | 10.1016/J.STR.2022.11.001 | 2022-11-23 | Yes | |
MRGX1 | MRGPRX1 | A orphans | A | Human | Cryo-EM | 8DWH | 8DWH_refined | 3.3 | R | Active | 100 | 77 | Gq/11 | αq | Gs-mini-Gq chimera | 57 | - | - |
compound 16 [PMID: 31498617]
|
small-molecule | Agonist | bovine adrenal medulla peptide 8-22 | peptide | No | No | Liu Y, Cao C, Huang XP, Gumpper RH, Rachman MM, Shih SL, Krumm BE, Zhang S, Shoichet BK, Fay JF, Roth BL | 10.1038/S41589-022-01173-6 | 2022-11-02 | Yes | |
OPRX | NOP | Opioid | A | Human | Cryo-EM | 8F7X | 8F7X_refined | 3.3 | R | Active | 100 | 77 | Gi/o | αi1 | - | 62 | - | scFv16 |
nociceptin/orphanin FQ
|
peptide | Agonist | nociceptin/orphanin FQ | peptide | No | No | Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y, Roth BL, Xu HE | 10.1016/J.CELL.2022.12.026 | 2022-12-14 | Yes | |
NTR1 | NTS1 | Neurotensin | A | Rat | Cryo-EM | 8FN0 | - | 2.9 | A | Active | 100 | 67 | Gi/o | αo | Mini-Go | 60 | - | scFv16 |
neurotensin
CHEMBL4576388 |
peptide small-molecule |
Agonist PAM |
neurotensin, neuromedin N | peptide | No | No | Krumm BE, DiBerto JF, Olsen RHJ, Kang HJ, Slocum ST, Zhang S, Strachan RT, Huang XP, Slosky LM, Pinkerton AB, Barak LS, Caron MG, Kenakin T, Fay JF, Roth BL | 10.1021/ACS.BIOCHEM.3C00029 | 2023-03-29 | Yes | |
FFAR4 | FFA4 | Free fatty acid | A | Human | Cryo-EM | 8ID6 | - | 2.8 | R | Active | 100 | 80 | Gi/o | αi1 | - | 64 | - | scFv16 |
oleic acid
|
small-molecule | Agonist | 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 | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 7XKA | - | 3.1 | A | Active | 99 | 69 | - | - | - | - | T4-Lysozyme | Antibody fragment |
(5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline | small-molecule | No | No | - | - | 2023-04-26 | Yes | |
NK2R | NK2 | Tachykinin | A | Human | Cryo-EM | 7XWO | 7XWO_refined | 2.7 | B | Active | 100 | 68 | Gq/11 | αq | - | 59 | BRIL | scFv16 |
HIS-LYS-THR-ASP-SER-PHE-VAL-GLY-LEU-MET-NH2
|
peptide | Agonist | neurokinin A, neuropeptide K, neurokinin B, neuropeptide γ, hemokinin 1, substance P | peptide | No | No | - | - | 2023-05-31 | Yes | |
C3AR | C3a | Complement peptide | A | Human | Cryo-EM | 8HK2 | - | 2.9 | A | Active | 100 | 59 | Gi/o | αi1 | - | 64 | - | scFv16 |
C3a anaphylatoxin
|
peptide | Agonist | C5a, C3a | peptide | No | No | Wang Y, Liu W, Xu Y, He X, Yuan Q, Luo P, Fan W, Zhu J, Zhang X, Cheng X, Jiang Y, Xu HE, Zhuang Y | 10.1038/S41589-023-01339-W | 2023-05-10 | Yes | |
CXCR1 | CXCR1 | Chemokine | A | Human | Cryo-EM | 8IC0 | - | 3.4 | A | Active | 100 | 86 | Gi/o | αi1 | - | 65 | - | scFv16 |
Interleukin-8
|
protein | Agonist | cytokine domain of tyrosyl tRNA synthetase, CXCL8, 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 | |
TAA7F | TAAR7F | A orphans | A | Mouse | Cryo-EM | 8PM2 | - | 2.9 | R | Active | 100 | 73 | Gs | αs | - | 58 | - | Nanobody-35 |
N,N-Dimethylcyclohexylamine
|
small-molecule | Agonist | - | - | No | No | Gusach A, Lee Y, Khoshgrudi AN, Mukhaleva E, Ma N, Koers EJ, Chen Q, Edwards PC, Huang F, Kim J, Mancia F, Verprintsev DB, Vaidehi N, Weyand SN, Tate CG | 10.1101/2023.07.07.547762 | 2023-08-09 | Yes | |
PE2R4 | EP4 | Prostanoid | A | Human | Cryo-EM | 8GD9 | - | 3.2 | R | Active | 100 | 57 | Gs | αs | - | 54 | - | - |
4-({2-[(1R,2R,3R,5S)-3,5-dihydroxy-2-{(3S)-3-hydroxy-4-[3-(methoxymethyl)phenyl]butyl}cyclopentyl]ethyl}sulfanyl)butanoic acid
|
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 | |
C3AR | C3a | Complement peptide | A | Human | Cryo-EM | 8I95 | - | 2.9 | C | Active | 100 | 58 | Gi/o | αo | - | 59 | - | 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 | 8JHY | - | 2.9 | A | Active | 100 | 80 | Gi/o | αi1 | - | 64 | - | scFv16 |
compound 9n [PMID: 18752940]
|
small-molecule | 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 | |
HCAR2 | HCA2 | Hydroxycarboxylic acid | A | Human | Cryo-EM | 8JZ7 | 8JZ7_refined | 2.6 | A | Active | 100 | 80 | Gi/o | αi1 | - | 64 | - | scFv16 |
MK 6892
|
small-molecule | Agonist | β-D-hydroxybutyric acid, butyric acid | small-molecule | No | No | Cheng L, Sun S, Wang H, Zhao C, Tian X, Liu Y, Fu P, Shao Z, Chai R, Yan W | 10.1038/S41392-023-01625-Y | 2023-10-04 | Yes | |
TAAR1 | TA1 | Trace amine | A | Mouse | Cryo-EM | 8WC3 | - | 3.0 | R | Active | 100 | 80 | Gs | αs | - | 59 | - | scFv16 |
ulotaront
|
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 | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 4BEY | - | 2.9 | A | Active | 100 | 94 | Gi/o | αt1 | Only H5 | 3 | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Singhal A, Ostermaier MK, Vishnivetskiy SA, Panneels V, Homan KT, Tesmer JJ, Veprintsev D, Deupi X, Gurevich VV, Schertler GF, Standfuss J | 10.1038/EMBOR.2013.44 | 2013-05-08 | Yes | |
P2Y12 | P2Y12 | P2Y | A | Human | X-ray | 4PY0 | - | 3.1 | A | Active | 59 | 83 | - | - | - | - | BRIL | - |
2MeSATP
|
small-molecule | Agonist (partial) | ADP, ATP | small-molecule | No | No | Zhang J, Zhang K, Gao ZG, Paoletta S, Zhang D, Han GW, Li T, Ma L, Zhang W, Muller CE, Yang H, Jiang H, Cherezov V, Katritch V, Jacobson KA, Stevens RC, Wu B, Zhao Q | 10.1038/NATURE13288 | 2014-04-30 | Yes | |
AGTR1 | AT1 | Angiotensin | A | Human | X-ray | 4ZUD | 4ZUD_refined | 2.8 | A | Inactive | 6 | 75 | - | - | - | - | BRIL | - |
OLMESARTAN
|
small-molecule | Inverse agonist | angiotensin IV, angiotensin II, angiotensin III, angiotensin A | peptide | No | No | Zhang H, Unal H, Desnoyer R, Han GW, Patel N, Katritch V, Karnik SS, Cherezov V, Stevens RC | 10.1074/JBC.M115.689000 | 2015-10-07 | Yes | |
EDNRB | ETB | Endothelin | A | Human | X-ray | 5GLI | 5GLI_refined | 2.5 | A | Inactive | 4 | 71 | - | - | - | - | T4-Lysozyme | - |
Apo (no ligand)
|
none | Apo (no ligand) | endothelin-1, endothelin-2, endothelin-3 | peptide | No | No | Shihoya W, Nishizawa T, Okuta A, Tani K, Dohmae N, Fujiyoshi Y, Nureki O, Doi T | 10.1038/nature19319 | 2016-09-07 | Yes | |
GLP1R | GLP-1 | Glucagon | B1 | Human | X-ray | 5VEX | 5VEX_refined | 3.0 | B | Inactive | 0 | 57 | - | - | - | - | T4-Lysozyme | - |
NNC0640
|
small-molecule | NAM | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | No | No | Song G, Yang D, Wang Y, de Graaf C, Zhou Q, Jiang S, Liu K, Cai X, Dai A, Lin G, Liu D, Wu F, Wu Y, Zhao S, Ye L, Han GW, Lau J, Wu B, Hanson MA, Liu ZJ, Wang MW, Stevens RC | 10.1038/NATURE22378 | 2017-05-17 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 5WKT | - | 3.2 | A | Active | 100 | 94 | Gi/o | αt1 | Only H5 | 3 | - | - |
B-Octylglucoside
|
small-molecule | unknown | - | - | No | No | Broecker J, Morizumi T, Ou WL, Klingel V, Kuo A, Kissick DJ, Ishchenko A, Lee MY, Xu S, Makarov O, Cherezov V, Ogata CM, Ernst OP | 10.1038/NPROT.2017.135 | 2017-12-13 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 6FK6 | 6FK6_refined | 2.4 | A | Active | 97 | 94 | - | - | - | - | - | - |
COMPOUND SUMMARY
|
small-molecule | Agonist | - | - | No | No | Mattle D, Kuhn B, Aebi J, Bedoucha M, Kekilli D, Grozinger N, Alker A, Rudolph MG, Schmid G, Schertler GFX, Hennig M, Standfuss J, Dawson RJP | 10.1073/PNAS.1718084115 | 2018-04-04 | Yes | |
AGTR2 | AT2 | Angiotensin | A | Human | X-ray | 5XJM | 5XJM_refined | 3.2 | A | Active | 100 | 78 | - | - | - | - | BRIL | Fab |
CHEMBL404594
|
protein | Agonist | angiotensin-(1-7), angiotensin II, angiotensin III | peptide | No | No | Asada H, Horita S, Hirata K, Shiroishi M, Shiimura Y, Iwanari H, Hamakubo T, Shimamura T, Nomura N, Kusano-Arai O, Uemura T, Suno C, Kobayashi T, Iwata S | 10.1038/S41594-018-0079-8 | 2018-07-11 | Yes | |
TA2R | TP | Prostanoid | A | Human | X-ray | 6IIV | - | 3.0 | A | Inactive | 36 | 87 | - | - | - | - | Rubredoxin | - |
daltroban
|
small-molecule | Antagonist | thromboxane A2, PGF2α, PGI2, PGH2, PGD2, 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 | 6ME9 | 6ME9_refined | 3.3 | B | Inactive | 1 | 79 | - | - | - | - | Rubredoxin | - |
ramelteon
|
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 | |
CLTR1 | CysLT1 | Leukotriene | A | Human | X-ray | 6RZ5 | - | 2.5 | B | Active | 59 | 84 | - | - | - | - | BRIL | - |
zafirlukast
|
small-molecule | Antagonist | LTD4, LTC4, LTE4 | small-molecule | No | Yes | 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 | |
ACM5 | M5 | Acetylcholine (muscarinic) | A | Human | X-ray | 6OL9 | 6OL9_refined | 2.5 | A | Inactive | 2 | 53 | - | - | - | - | T4-Lysozyme | - |
tiotropium
|
small-molecule | Inverse agonist | acetylcholine | small-molecule | No | No | Vuckovic Z, Gentry PR, Berizzi AE, Hirata K, Varghese S, Thompson G, van der Westhuizen ET, Burger WAC, Rahmani R, Valant C, Langmead CJ, Lindsley CW, Baell JB, Tobin AB, Sexton PM, Christopoulos A, Thal DM | 10.1073/PNAS.1914446116 | 2019-12-11 | Yes | |
CNR1 | CB1 | Cannabinoid | A | Human | Cryo-EM | 6KPG | 6KPG_refined | 3.0 | R | Active | 100 | 60 | Gi/o | αi1 | - | 64 | - | scFv16 |
AM841
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | No | No | Hua T, Li X, Wu L, Iliopoulos-Tsoutsouvas C, Wang Y, Wu M, Shen L, Brust CA, Nikas SP, Song F, Song X, Yuan S, Sun Q, Wu Y, Jiang S, Grim TW, Benchama O, Stahl EL, Zvonok N, Zhao S, Bohn LM, Makriyannis A, Liu ZJ | 10.1016/J.CELL.2020.01.008 | 2020-02-12 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 6PEL | - | 3.2 | A | Active | 100 | 93 | Gi/o | αt1 | Only H5 | 3 | - | - |
Citronellol
|
small-molecule | unknown | - | - | No | No | - | - | 2020-06-24 | Yes | |
ACM1 | M1 | Acetylcholine (muscarinic) | A | Human | X-ray | 6WJC | - | 2.6 | A | Inactive | 2 | 62 | - | - | - | - | T4-Lysozyme | - |
HYOSCYAMINE
muscarinic toxin 7 |
small-molecule peptide |
Antagonist NAM |
acetylcholine | small-molecule | No | No | Maeda S, Xu J, N Kadji FM, Clark MJ, Zhao J, Tsutsumi N, Aoki J, Sunahara RK, Inoue A, Garcia KC, Kobilka BK | 10.1126/SCIENCE.AAX2517 | 2020-07-08 | Yes | |
GABR2 | GABAB2 | GABAB | C | Human | Cryo-EM | 7CUM | - | 3.5 | B | Inactive | - | 72 | - | - | - | - | - | - |
CGP 54626A
Unknown ligand |
small-molecule none |
NAM | - | - | No | No | Kim Y, Jeong E, Jeong JH, Kim Y, Cho Y | 10.1016/J.JMB.2020.09.023 | 2020-11-11 | Yes | |
V2R | V2 | Vasopressin and oxytocin | A | Human | Cryo-EM | 7KH0 | - | 2.8 | R | Active | 100 | 74 | Gs | αs | - | 58 | - | scFv16 Nanobody-35 |
vasopressin
|
peptide | Agonist | vasopressin, oxytocin | peptide | No | No | Wang L, Xu J, Cao S, Sun D, Liu H, Lu Q, Liu Z, Du Y, Zhang C | 10.1038/S41422-021-00483-Z | 2021-05-26 | Yes | |
GRM2 | mGlu2 | Metabotropic glutamate | C | Human | Cryo-EM | 7MTR | 7MTR_refined | 3.3 | A | Active | - | 88 | - | - | - | - | - | - |
2-methoxy-6-propyl-N-(2-{4-[(1H-tetrazol-5-yl)methoxy]phenyl}ethyl)thieno[2,3-d]pyrimidin-4-amine
L-glutamic acid |
small-molecule small-molecule |
Ago-PAM Agonist |
L-glutamic acid | small-molecule | No | No | Seven AB, Barros-Alvarez X, de Lapeyriere M, Papasergi-Scott MM, Robertson MJ, Zhang C, Nwokonko RM, Gao Y, Meyerowitz JG, Rocher JP, Schelshorn D, Kobilka BK, Mathiesen JM, Skiniotis G | 10.1038/S41586-021-03680-3 | 2021-07-07 | Yes | |
GRM5 | mGlu5 | Metabotropic glutamate | C | Human | X-ray | 7P2L | 7P2L_refined | 2.5 | A | Inactive | - | 21 | - | - | - | - | T4-Lysozyme | - |
alloswitch-1
|
small-molecule | NAM | L-glutamic acid | small-molecule | No | No | Nasrallah C, Cannone G, Briot J, Rottier K, Berizzi AE, Huang CY, Quast RB, Hoh F, Baneres JL, Malhaire F, Berto L, Dumazer A, Font-Ingles J, Gomez-Santacana X, Catena J, Kniazeff J, Goudet C, Llebaria A, Pin JP, Vinothkumar KR, Lebon G | 10.1016/J.CELREP.2021.109648 | 2021-09-08 | Yes | |
ACM1 | M1 | Acetylcholine (muscarinic) | A | Human | X-ray | 6ZG4 | 6ZG4_refined | 2.3 | A | Inactive | 2 | 62 | - | - | - | - | T4-Lysozyme | - |
Ethyl (4S)-4-[4-[(1-methylcyclobutyl)carbamoyl]piperidin-1-yl]azepane-1-carboxylate
|
small-molecule | Agonist | acetylcholine | small-molecule | No | No | Brown AJH, Bradley SJ, Marshall FH, Brown GA, Bennett KA, Brown J, Cansfield JE, Cross DM, de Graaf C, Hudson BD, Dwomoh L, Dias JM, Errey JC, Hurrell E, Liptrot J, Mattedi G, Molloy C, Nathan PJ, Okrasa K, Osborne G, Patel JC, Pickworth M, Robertson N, Shahabi S, Bundgaard C, Phillips K, Broad LM, Goonawardena AV, Morairty SR, Browning M, Perini F, Dawson GR, Deakin JFW, Smith RT, Sexton PM, Warneck J, Vinson M, Tasker T, Tehan BG, Teobald B, Christopoulos A, Langmead CJ, Jazayeri A, Cooke RM, Rucktooa P, Congreve MS, Weir M, Tobin AB | 10.1016/J.CELL.2021.11.001 | 2021-10-06 | Yes | |
MRGX2 | MRGPRX2 | A orphans | A | Human | Cryo-EM | 7S8N | 7S8N_refined | 2.9 | R | Active | 100 | 76 | Gq/11 | αq | Gq-Gs chimera | 57 | - | scFv16 |
(R)-ZINC-3573
|
small-molecule | Agonist | PAMP-20 | peptide | No | No | Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL | 10.1038/S41586-021-04126-6 | 2021-11-17 | Yes | |
MRGX2 | MRGPRX2 | A orphans | A | Human | Cryo-EM | 7VV0 | 7VV0_refined | 3.5 | R | Active | 98 | 80 | - | - | - | - | - | - |
PAMP-12
|
peptide | Agonist | PAMP-20 | peptide | No | No | Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP | 10.1038/S41586-021-04077-Y | 2021-12-01 | Yes | |
S1PR1 | S1P1 | Lysophospholipid (S1P) | A | Human | Cryo-EM | 7WF7 | 7WF7_refined | 3.4 | A | Active | 100 | 71 | Gi/o | αi1 | - | 40 | - | scFv16 |
sphingosine 1-phosphate
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | No | No | Xu Z, Ikuta T, Kawakami K, Kise R, Qian Y, Xia R, Sun MX, Zhang A, Guo C, Cai XH, Huang Z, Inoue A, He Y | 10.1038/S41589-021-00930-3 | 2022-01-05 | Yes | |
SSR2 | SST2 | Somatostatin | A | Human | Cryo-EM | 7T11 | 7T11_refined | 2.7 | R | Active | 100 | 77 | Gi/o | αi3 | - | 62 | - | scFv16 |
Octreotide
|
peptide | Agonist | SRIF-28, 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 | 7TYL | - | 3.3 | R | Active | 100 | 78 | Gs | αs | - | 58 | - | 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 | 2022-03-23 | Yes | |
S1PR2 | S1P2 | Lysophospholipid (S1P) | A | Human | Cryo-EM | 7T6B | 7T6B_refined | 3.2 | R | Active | 100 | 75 | G12/13 | α13 | - | 60 | - | scFv16 |
sphingosine 1-phosphate
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | No | No | Chen H, Chen K, Huang W, Staudt LM, Cyster JG, Li X | 10.1126/SCIADV.ABN0067 | 2022-04-06 | Yes | |
NMUR2 | NMU2 | Neuromedin U | A | Human | Cryo-EM | 7W57 | - | 3.2 | R | Active | 100 | 72 | Gq/11 | αq | - | 59 | - | scFv16 |
Neuromedin-S
|
peptide | Agonist | neuromedin U-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 | |
MRGRD | MRGPRD | A orphans | A | Human | Cryo-EM | 7Y12 | - | 3.1 | R | Active | 100 | 82 | Gi/o | αi1 | - | 62 | BRIL | scFv16 |
β-alanine
|
small-molecule | Agonist | β-alanine | small-molecule | No | No | Suzuki S, Iida M, Hiroaki Y, Tanaka K, Kawamoto A, Kato T, Oshima A | 10.1038/S42003-022-03668-3 | 2022-07-20 | Yes | |
CCR3 | CCR3 | Chemokine | A | Human | Cryo-EM | 7X9Y | 7X9Y_refined | 3.1 | R | Active | 100 | 83 | Gi/o | αi1 | - | 62 | - | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | CCL28, CCL8, CXCL11, CCL13, CCL15, CXCL9, CXCL10, CCL7, CCL2, CCL5, CCL11, CCL24, 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 | |
GP119 | GPR119 | GPR18, GPR55 and GPR119 | A | Human | Cryo-EM | 7XZ6 | - | 2.8 | R | Active | 100 | 87 | Gs | αs | - | 60 | BRIL | Nanobody-35 |
APD668
|
small-molecule | Agonist | N-oleoylethanolamide, 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 | 7WXU | - | 2.9 | R | Active | 100 | 30 | Gq/11 | αq | - | 60 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y | 10.1038/S41467-022-33173-4 | 2022-09-28 | Yes | |
T2R46 | TAS2R46 | Taste 2 | T | Human | Cryo-EM | 7XP4 | - | 3.0 | R | Active | - | 97 | Gi/o | αgust | - | 63 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Xu W, Wu L, Liu S, Liu X, Cao X, Zhou C, Zhang J, Fu Y, Guo Y, Wu Y, Tan Q, Wang L, Liu J, Jiang L, Fan Z, Pei Y, Yu J, Cheng J, Zhao S, Hao X, Liu ZJ, Hua T | 10.1126/SCIENCE.ABO1633 | 2022-10-12 | Yes | |
VIPR1 | VPAC1 | VIP and PACAP | B1 | Human | Cryo-EM | 8E3Z | 8E3Z_refined | 2.7 | R | Active | 100 | 81 | Gs | αs | - | 55 | - | Nanobody-35 |
Vasoactive intestinal polypeptide
|
small-molecule | Agonist | VIP, PHI, PHM, secretin, PACAP-27, GHRH, PACAP-38 | peptide | No | No | Piper SJ, Deganutti G, Lu J, Zhao P, Liang YL, Lu Y, Fletcher MM, Hossain MA, Christopoulos A, Reynolds CA, Danev R, Sexton PM, Wootten D | 10.1038/S41467-022-34629-3 | 2022-11-23 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 8A6E | 8A6E_refined | 1.8 | A | Inactive | 24 | 87 | - | - | - | - | - | - |
Retinal (11-cis)
|
small-molecule | Agonist | - | - | No | No | Gruhl T, Weinert T, Rodrigues MJ, Milne CJ, Ortolani G, Nass K, Nango E, Sen S, Johnson PJM, Cirelli C, Furrer A, Mous S, Skopintsev P, James D, Dworkowski F, Bath P, Kekilli D, Ozerov D, Tanaka R, Glover H, Bacellar C, Brunle S, Casadei CM, Diethelm AD, Gashi D, Gotthard G, Guixa-Gonzalez R, Joti Y, Kabanova V, Knopp G, Lesca E, Ma P, Martiel I, Muhle J, Owada S, Pamula F, Sarabi D, Tejero O, Tsai CJ, Varma N, Wach A, Boutet S, Tono K, Nogly P, Deupi X, Iwata S, Neutze R, Standfuss J, Schertler G, Panneels V | 10.1038/S41586-023-05863-6 | 2023-03-29 | Yes | |
AA2BR | A2B | Adenosine | A | Human | Cryo-EM | 8HDP | - | 3.2 | R | Active | 100 | 84 | Gs | αs | Mini-Gs | 60 | - | Nanobody-35 |
adenosine
|
small-molecule | Agonist | adenosine | small-molecule | No | No | Cai H, Xu Y, Guo S, He X, Sun J, Li X, Li C, Yin W, Cheng X, Jiang H, Xu HE, Xie X, Jiang Y | 10.1038/S41421-022-00503-1 | 2023-01-18 | Yes | |
NMUR2 | NMU2 | Neuromedin U | A | Human | Cryo-EM | 7XK8 | 7XK8_refined | 3.3 | R | Active | 100 | 68 | Gi/o | αi1 | - | 64 | - | - |
Neuromedin U-25 (human)
|
peptide | Agonist | neuromedin U-23, neuromedin S-36, neuromedin S-33, neuromedin U-25 | peptide | No | No | Zhao W, Zhang W, Wang M, Lu M, Chen S, Tang T, Schnapp G, Wagner H, Brennauer A, Yi C, Chu X, Han S, Wu B, Zhao Q | 10.1038/S41467-022-34814-4 | 2023-02-22 | Yes | |
AA2BR | A2B | Adenosine | A | Human | Cryo-EM | 7XY7 | - | 3.3 | R | Active | 100 | 85 | Gs | αs | Mini-Gs | 57 | BRIL | - |
NECA
|
small-molecule | Agonist | adenosine | small-molecule | No | No | Chen Y, Zhang J, Weng Y, Xu Y, Lu W, Liu W, Liu M, Hua T, Song G | 10.1126/SCIADV.ADD3709 | 2023-05-03 | Yes | |
TAAR9 | TAAR9 | A orphans | A | Mouse | Cryo-EM | 8ITF | - | 3.5 | R | Active | 100 | 86 | Gs | αs | - | 59 | - | scFv16 Nanobody-35 |
N,N-Dimethylcyclohexylamine
|
small-molecule | Agonist | - | - | No | No | Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP | 10.1038/S41586-023-06106-4 | 2023-05-31 | Yes | |
ADA1A | α1A | Adrenoceptors | A | Human | Cryo-EM | 7YMH | 7YMH_refined | 3.5 | A | Active | 100 | 58 | Gq/11 | αq | Mini-Gq | 51 | - | Nanobody-29 |
Noradrenaline
|
small-molecule | Agonist | (-)-adrenaline, (-)-noradrenaline | small-molecule | No | No | Toyoda Y, Zhu A, Kong F, Shan S, Zhao J, Wang N, Sun X, Zhang L, Yan C, Kobilka BK, Liu X | 10.1038/S41467-023-39310-X | 2023-07-05 | Yes | |
CALCR | CT | Calcitonin | B1 | Human | Cryo-EM | 8F0K | - | 1.9 | R | Active | 100 | 78 | Gs | αs | - | 58 | - | Nanobody-35 RAMP3 |
San385
|
peptide | Agonist | adrenomedullin, α-CGRP, calcitonin, amylin, calcitonin (salmon), 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 | 8JD0 | - | 3.3 | 2 | Inactive | - | 88 | - | - | - | - | - | - |
L-glutamic acid
CHEMBL3894759 |
small-molecule small-molecule |
Agonist NAM |
L-glutamic acid | small-molecule | No | No | Wang X, Wang M, Xu T, Feng Y, Shao Q, Han S, Chu X, Xu Y, Lin S, Zhao Q, Wu B | 10.1038/S41422-023-00830-2 | 2023-06-21 | Yes | |
CRFR1 | CRF1 | Corticotropin-releasing factor | B1 | Human | X-ray | 8GTM | - | 2.6 | A | Inactive | 16 | 63 | - | - | - | - | Endolysin | - |
7-(4-bromanyl-2,6-dimethoxy-phenyl)-4,8-dimethyl-~{N},~{N}-bis[4,4,4-tris(fluoranyl)butyl]-1$l^{4},3,5,9-tetrazabicyclo[4.3.0]nona-1(6),2,4,8-tetraen-2-amine
|
small-molecule | Antagonist | urocortin 1, corticotrophin-releasing hormone, 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 | |
HCAR2 | HCA2 | Hydroxycarboxylic acid | A | Human | Cryo-EM | 8IHB | - | 2.9 | R | Active | 100 | 80 | Gi/o | αi1 | - | 62 | BRIL | - |
GSK256073
|
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 | 2023-09-13 | Yes | |
HCAR2 | HCA2 | Hydroxycarboxylic acid | A | Human | Cryo-EM | 8JIL | - | 3.5 | A | Active | 100 | 79 | Gi/o | αi1 | - | 63 | - | scFv16 |
nicotinic acid
|
small-molecule | Agonist | 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 | |
GPR34 | GPR34 | A orphans | A | Human | Cryo-EM | 8K4N | 8K4N_refined | 2.8 | D | Active | 100 | 73 | Gi/o | αi1 | - | 61 | - | scFv16 |
(2R)-2-azanyl-3-[oxidanyl-[(2R)-2-oxidanyl-3-tetradec-9-enoyloxy-propoxy]phosphoryl]oxy-propanoic acid
|
small-molecule | Agonist | lysophosphatidylserine | small-molecule | No | No | - | - | 2023-10-25 | Yes | |
TAAR1 | TA1 | Trace amine | A | Mouse | Cryo-EM | 8WC7 | - | 3.1 | R | Active | 100 | 81 | Gs | αs | - | 58 | - | scFv16 |
2-[4-(3-Fluorophenyl)phenyl]ethan-1-amine
|
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 | |
CRFR1 | CRF1 | Corticotropin-releasing factor | B1 | Human | X-ray | 4K5Y | - | 3.0 | C | Inactive | 16 | 60 | - | - | - | - | T4-Lysozyme | - |
CP 376,395
|
small-molecule | Antagonist | urocortin 1, corticotrophin-releasing hormone, urocortin 2 | peptide | No | No | Hollenstein K, Kean J, Bortolato A, Cheng RK, Dore AS, Jazayeri A, Cooke RM, Weir M, Marshall FH | 10.1038/NATURE12357 | 2013-07-17 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 4UHR | 4UHR_refined | 2.6 | A | Active | 72 | 75 | - | - | - | - | - | - |
CGS 21680
|
small-molecule | Agonist | adenosine | small-molecule | No | No | Lebon G, Edwards PC, Leslie AG, Tate CG | 10.1124/mol.114.097360 | 2015-04-08 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5IU4 | 5IU4_refined | 1.7 | A | Inactive | 0 | 71 | - | - | - | - | BRIL | - |
ZM-241385
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | Segala E, Guo D, Cheng RK, Bortolato A, Deflorian F, Doré AS, Errey JC, Heitman LH, IJzerman AP, Marshall FH, Cooke RM. | 10.1021/acs.jmedchem.6b00653 | 2016-06-29 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 5TE5 | 5TE5_refined | 4.0 | A | Inactive | 24 | 100 | - | - | - | - | - | - |
10,20-Methanoretinal
|
small-molecule | Agonist | - | - | No | No | Gulati S, Jastrzebska B, Banerjee S, Placeres AL, Miszta P, Gao S, Gunderson K, Tochtrop GP, Filipek S, Katayama K, Kiser PD, Mogi M, Stewart PL, Palczewski K | 10.1073/PNAS.1617446114 | 2017-03-15 | Yes | |
5HT2B | 5-HT2B | 5-Hydroxytryptamine | A | Human | X-ray | 5TUD | 5TUD_refined | 3.0 | D | Active | 80 | 58 | - | - | - | - | BRIL | Antibody |
ergotamine
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | No | No | Ishchenko A, Wacker D, Kapoor M, Zhang A, Han GW, Basu S, Patel N, Messerschmidt M, Weierstall U, Liu W, Katritch V, Roth BL, Stevens RC, Cherezov V | 10.1073/PNAS.1700891114 | 2017-07-26 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 6FKC | 6FKC_refined | 2.5 | A | Active | 97 | 94 | - | - | - | - | - | - |
3-[1'-[(2~{S})-2-(4-chlorophenyl)-3-methyl-butanoyl]spiro[1,3-benzodioxole-2,4'-piperidine]-5-yl]propanoic acid
|
small-molecule | Agonist | - | - | No | No | Mattle D, Kuhn B, Aebi J, Bedoucha M, Kekilli D, Grozinger N, Alker A, Rudolph MG, Schmid G, Schertler GFX, Hennig M, Standfuss J, Dawson RJP | 10.1073/PNAS.1718084115 | 2018-04-04 | Yes | |
ADRB1 | β1 | Adrenoceptors | A | Wild turkey | X-ray | 6H7J | 6H7J_refined | 2.8 | A | Active | 99 | 60 | - | - | - | - | Thioredoxin 1 | Camelid antibody fragment Nb80 |
LEVISOPRENALINE
|
small-molecule | Agonist | - | - | No | No | Warne T, Edwards PC, Dore AS, Leslie AGW, Tate CG | 10.1126/SCIENCE.AAU5595 | 2018-10-17 | Yes | |
TA2R | TP | Prostanoid | A | Human | X-ray | 6IIU | - | 2.5 | A | Inactive | 36 | 87 | - | - | - | - | Rubredoxin | - |
ramatroban
|
small-molecule | Antagonist | thromboxane A2, PGF2α, PGI2, PGH2, PGD2, 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 | 6ME8 | 6ME8_refined | 3.1 | 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 | |
GLP1R | GLP-1 | Glucagon | B1 | Human | X-ray | 6KJV | 6KJV_refined | 2.8 | B | Inactive | 0 | 57 | - | - | - | - | T4-Lysozyme | - |
PF-06372222
|
small-molecule | NAM | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | 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 | |
OX2R | OX2 | Orexin | A | Human | X-ray | 6TPN | 6TPN_refined | 2.6 | A | Inactive | 0 | 71 | - | - | - | - | GlgA glycogen synthase | - |
HTL6641
|
small-molecule | Antagonist | orexin-A, orexin-B | peptide | No | No | Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA. | 10.1021/acs.jmedchem.9b01787 | 2020-01-01 | Yes | |
AGTR1 | AT1 | Angiotensin | A | Human | X-ray | 6OS2 | - | 2.7 | A | Active | 93 | 85 | - | - | - | - | BRIL | Nanobody-Nb.AT110i1_le |
TRV026
|
peptide | Agonist | angiotensin IV, angiotensin II, angiotensin III, angiotensin A | peptide | No | No | Wingler LM, Skiba MA, McMahon C, Staus DP, Kleinhenz ALW, Suomivuori CM, Latorraca NR, Dror RO, Lefkowitz RJ, Kruse AC | 10.1126/SCIENCE.AAY9813 | 2020-02-19 | Yes | |
ADRB1 | β1 | Adrenoceptors | A | Wild turkey | Cryo-EM | 6TKO | 6TKO_refined | 3.3 | A | Active | 100 | 58 | Beta | Beta-arrestin-1 | - | 82 | - | Fab30 heavy chain Fab30 light chain |
ARFORMOTEROL
|
small-molecule | Agonist | - | - | No | No | Lee Y, Warne T, Nehme R, Pandey S, Dwivedi-Agnihotri H, Chaturvedi M, Edwards PC, Garcia-Nafria J, Leslie AGW, Shukla AK, Tate CG | 10.1038/S41586-020-2419-1 | 2020-06-17 | Yes | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 6VCB | - | 3.3 | R | Active | 100 | 82 | Gs | αs | - | 57 | - | Nanobody-35 |
glucagon-like peptide 1-(7-37)
CHEMBL5197819 |
peptide small-molecule |
Agonist PAM |
glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | No | No | Bueno AB, Sun B, Willard FS, Feng D, Ho JD, Wainscott DB, Showalter AD, Vieth M, Chen Q, Stutsman C, Chau B, Ficorilli J, Agejas FJ, Cumming GR, Jimenez A, Rojo I, Kobilka TS, Kobilka BK, Sloop KW | 10.1038/S41589-020-0589-7 | 2020-07-22 | Yes | |
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 | 7CKX | - | 3.5 | R | Active | 100 | 61 | Gs | αs | - | 60 | - | Nanobody-35 |
A77636
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | No | No | - | - | 2021-03-03 | Yes | |
V2R | V2 | Vasopressin and oxytocin | A | Human | Cryo-EM | 7BB7 | - | 4.4 | A | Active | 100 | 72 | Gs | αs | - | 55 | - | Nanobody-35 |
vasopressin
|
peptide | Agonist | vasopressin, oxytocin | peptide | No | No | Bous J, Orcel H, Floquet N, Leyrat C, Lai-Kee-Him J, Gaibelet G, Ancelin A, Saint-Paul J, Trapani S, Louet M, Sounier R, Demene H, Granier S, Bron P, Mouillac B | 10.1126/SCIADV.ABG5628 | 2021-06-02 | Yes | |
V2R | V2 | Vasopressin and oxytocin | A | Human | Cryo-EM | 7DW9 | - | 2.6 | R | Active | 100 | 75 | Gs | αs | - | 60 | - | Nanobody-35 scFv16 |
vasopressin
|
peptide | Agonist | vasopressin, oxytocin | peptide | No | No | Zhou F, Ye C, Ma X, Yin W, Croll TI, Zhou Q, He X, Zhang X, Yang D, Wang P, Xu HE, Wang MW, Jiang Y | 10.1038/S41422-021-00480-2 | 2021-07-21 | Yes | |
CASR | CaS | Calcium-sensing | C | Human | Cryo-EM | 7E6U | 7E6U_refined | 6.0 | A | Inactive | - | 72 | - | - | - | - | - | Nanobody-2D11 |
Apo (no ligand)
|
none | Apo (no ligand) | Mg2+, L-tryptophan, spermine, Ca2+ | small-molecule | No | No | Chen X, Wang L, Cui Q, Ding Z, Han L, Kou Y, Zhang W, Wang H, Jia X, Dai M, Shi Z, Li Y, Li X, Geng Y | 10.7554/ELIFE.68578 | 2021-09-22 | Yes | |
GP158 | GPR158 | C Orphans | C | Human | Cryo-EM | 7EWR | 7EWR_refined | 4.7 | A | Inactive | - | 47 | - | - | - | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Jeong E, Kim Y, Jeong J, Cho Y | 10.1038/S41467-021-27147-1 | 2021-12-01 | Yes | |
5HT2A | 5-HT2A | 5-Hydroxytryptamine | A | Human | X-ray | 7WC9 | 7WC9_refined | 2.5 | A | Inactive | 1 | 59 | - | - | - | - | BRIL | - |
IHCH-7086
|
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 | |
AGTR2 | AT2 | Angiotensin | A | Human | X-ray | 7JNI | 7JNI_refined | 3.0 | A | Active | 99 | 82 | - | - | - | - | BRIL | - |
olodanrigan
|
small-molecule | Antagonist | angiotensin-(1-7), angiotensin II, angiotensin III | peptide | No | No | Perryman R, Renziehausen A, Shaye H, Kostagianni AD, Tsiailanis AD, Thorne T, Chatziathanasiadou MV, Sivolapenko GB, El Mubarak MA, Han GW, Zarzycka B, Katritch V, Lebon G, Lo Nigro C, Lattanzio L, Morse SV, Choi JJ, O'Neill K, Kanaki Z, Klinakis A, Crook T, Cherezov V, Tzakos AG, Syed N | 10.1073/PNAS.2116289119 | 2022-02-09 | Yes | |
CCR1 | CCR1 | Chemokine | A | Human | Cryo-EM | 7VLA | 7VLA_refined | 2.7 | R | Active | 100 | 85 | Gi/o | αi1 | - | 64 | - | scFv16 |
CCL15(27-92)
|
peptide | Agonist | CCL14, CCL8, CCL13, CCL15, CCL4, CCL23, CCL7, CCL5, CCL3, CCL16 | peptide | No | No | Shao Z, Shen Q, Yao B, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Ma H, Chen ZH, Xu HE, Ying S, Zhang Y, Shen H | 10.1038/S41589-021-00918-Z | 2022-03-23 | Yes | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 7RG9 | 7RG9_refined | 3.2 | R | Active | 100 | 58 | Gs | αs | - | 56 | - | scFv16 Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | No | No | Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW | 10.1073/PNAS.2116506119 | 2022-04-13 | Yes | |
VIPR2 | VPAC2 | VIP and PACAP | B1 | Human | Cryo-EM | 7VQX | - | 2.7 | R | Active | 100 | 82 | Gs | αs | - | 60 | - | Nanobody-35 |
PACAP-27
|
peptide | Agonist | VIP, PHI, secretin, PACAP-27, GHRH, PACAP-38 | peptide | No | No | Xu Y, Feng W, Zhou Q, Liang A, Li J, Dai A, Zhao F, Yan J, Chen CW, Li H, Zhao LH, Xia T, Jiang Y, Xu HE, Yang D, Wang MW | 10.1038/S41467-022-30041-Z | 2022-05-18 | Yes | |
5HT4R | 5-HT4 | 5-Hydroxytryptamine | A | Human | Cryo-EM | 7XTA | 7XTA_refined | 3.2 | R | Active | 100 | 73 | Gi/o | αi1 | - | 62 | BRIL | scFv16 |
5-hydroxytryptamine
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | No | No | Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE | 10.1016/J.MOLCEL.2022.05.031 | 2022-07-27 | Yes | |
5HT2C | 5-HT2C | 5-Hydroxytryptamine | A | Human | Cryo-EM | 8DPH | - | 3.2 | A | Active | 100 | 58 | Gq/11 | αq | Gi2-mini-Gq chimera | 57 | - | scFv16 |
lorcaserin
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | No | No | Gumpper RH, Fay JF, Roth BL | 10.1016/J.CELREP.2022.111211 | 2022-08-24 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 8CU6 | 8CU6_refined | 2.8 | 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 | |
TSHR | TSH | Glycoprotein hormone | A | Human | Cryo-EM | 7T9M | - | 3.1 | R | Inactive | 30 | 74 | - | - | - | - | - | - |
CS-17 light chain
CS-17 heavy chain |
protein protein |
Inverse agonist | TSH | peptide | No | No | Faust B, Billesbolle CB, Suomivuori CM, Singh I, Zhang K, Hoppe N, Pinto AFM, Diedrich JK, Muftuoglu Y, Szkudlinski MW, Saghatelian A, Dror RO, Cheng Y, Manglik A | 10.1038/S41586-022-05159-1 | 2022-08-10 | Yes | |
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 | |
GRM5 | mGlu5 | Metabotropic glutamate | C | Human | X-ray | 4OO9 | 4OO9_refined | 2.6 | A | Inactive | - | 20 | - | - | - | - | T4-Lysozyme | - |
MAVOGLURANT
|
small-molecule | NAM | L-glutamic acid | small-molecule | No | No | Dore AS, Okrasa K, Patel JC, Serrano-Vega M, Bennett K, Cooke RM, Errey JC, Jazayeri A, Khan S, Tehan B, Weir M, Wiggin GR, Marshall FH | 10.1038/NATURE13396 | 2014-07-02 | Yes | |
NTR1 | NTS1 | Neurotensin | A | Rat | X-ray | 4XEE | 4XEE_refined | 2.9 | A | Active | 82 | 71 | - | - | - | - | T4-Lysozyme | - |
neurotensin
|
peptide | Agonist | neurotensin, neuromedin N | peptide | No | No | Krumm BE, White JF, Shah P, Grisshammer R | 10.1038/NCOMMS8895 | 2015-07-29 | Yes | |
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 | 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 | |
G1SGD4 | GLP-1 | Glucagon | B1 | Rabbit | Cryo-EM | 5VAI | - | 4.1 | R | Active | 100 | 84 | Gs | αs | - | 59 | - | - |
CHEMBL410972
|
protein | Agonist | - | - | No | No | Zhang Y, Sun B, Feng D, Hu H, Chu M, Qu Q, Tarrasch JT, Li S, Sun Kobilka T, Kobilka BK, Skiniotis G | 10.1038/NATURE22394 | 2017-05-24 | Yes | |
Q80KM9 | US28 | Unclassified | A | strain AD169 | X-ray | 5WB1 | 5WB1_refined | 3.5 | A | Active | 100 | 82 | - | - | - | - | - | Nanobody |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Miles TF, Spiess K, Jude KM, Tsutsumi N, Burg JS, Ingram JR, Waghray D, Hjorto GM, Larsen O, Ploegh HL, Rosenkilde MM, Garcia KC | 10.7554/ELIFE.35850 | 2018-06-13 | Yes | |
ADRB1 | β1 | Adrenoceptors | A | Wild turkey | X-ray | 6H7M | 6H7M_refined | 2.8 | A | Active | 99 | 60 | - | - | - | - | Thioredoxin 1 | Camelid antibody fragment Nb6B9 |
levosalbutamol
|
small-molecule | Agonist | - | - | No | No | Warne T, Edwards PC, Dore AS, Leslie AGW, Tate CG | 10.1126/SCIENCE.AAU5595 | 2018-10-17 | Yes | |
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, neurokinin A, neuropeptide K, neurokinin B, hemokinin 1, 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 | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 6PS7 | 6PS7_refined | 1.9 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
ZM-241385
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | 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-A, orexin-B | peptide | No | No | Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA. | 10.1021/acs.jmedchem.9b01787 | 2020-01-15 | 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 | VIP, PHI, PHM, PHV, PACAP-27, 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 | |
GLR | glucagon | Glucagon | B1 | Human | Cryo-EM | 6WPW | 6WPW_refined | 3.1 | R | Active | 100 | 83 | Gs | αs | - | 56 | - | Nanobody-35 |
Glucagon derivative ZP3780
|
peptide | Agonist | glucagon | peptide | No | No | Hilger D, Kumar KK, Hu H, Pedersen MF, O'Brien ES, Giehm L, Jennings C, Eskici G, Inoue A, Lerch M, Mathiesen JM, Skiniotis G, Kobilka BK | 10.1126/SCIENCE.ABA3373 | 2020-08-12 | Yes | |
NTR1 | NTS1 | Neurotensin | A | Rat | Cryo-EM | 7L0S | - | 4.5 | C | Active | 100 | 73 | Gi/o | αi1 | Non-canonical conformation | 95 | - | - |
neurotensin
|
peptide | Agonist | neurotensin, neuromedin N | 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 | |
DRD3 | D3 | Dopamine | A | Human | Cryo-EM | 7CMV | - | 2.7 | R | Active | 100 | 68 | Gi/o | αi1 | - | 64 | BRIL | scFv16 |
CHEMBL70565
|
small-molecule | Agonist | dopamine | small-molecule | No | No | Xu P, Huang S, Mao C, Krumm BE, Zhou XE, Tan Y, Huang XP, Liu Y, Shen DD, Jiang Y, Yu X, Jiang H, Melcher K, Roth BL, Cheng X, Zhang Y, Xu HE | 10.1016/J.MOLCEL.2021.01.003 | 2021-03-10 | Yes | |
GRM2 | mGlu2 | Metabotropic glutamate | C | Human | Cryo-EM | 7EPA | 7EPA_refined | 3.6 | A | Intermediate | - | 90 | - | - | - | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | L-glutamic acid | small-molecule | No | No | Du J, Wang D, Fan H, Xu C, Tai L, Lin S, Han S, Tan Q, Wang X, Xu T, Zhang H, Chu X, Yi C, Liu P, Wang X, Zhou Y, Pin JP, Rondard P, Liu H, Liu J, Sun F, Wu B, Zhao Q | 10.1038/S41586-021-03641-W | 2021-06-23 | Yes | |
GIPR | GIP | Glucagon | B1 | Human | Cryo-EM | 7DTY | - | 3.0 | R | Active | 100 | 79 | Gs | αs | - | 59 | - | Nanobody-35 |
GIP
|
small-molecule | Agonist | gastric inhibitory polypeptide | peptide | No | No | Zhao F, Zhang C, Zhou Q, Hang K, Zou X, Chen Y, Wu F, Rao Q, Dai A, Yin W, Shen DD, Zhang Y, Xia T, Stevens RC, Xu HE, Yang D, Zhao L, Wang MW | 10.7554/ELIFE.68719 | 2021-08-04 | Yes | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 7RTB | 7RTB_refined | 2.1 | R | Active | 100 | 83 | Gs | αs | - | 60 | - | Nanobody-35 |
Peptide-19
|
peptide | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | No | No | Johnson RM, Zhang X, Piper SJ, Nettleton TJ, Vandekolk TH, Langmead CJ, Danev R, Sexton PM, Wootten D | 10.1016/J.BBRC.2021.09.016 | 2021-10-06 | Yes | |
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 | |
CASR | CaS | Calcium-sensing | C | Human | Cryo-EM | 7SIN | 7SIN_refined | 5.9 | A | Inactive | - | 74 | - | - | - | - | - | - |
NPS 2143
|
small-molecule | Antagonist | Mg2+, L-tryptophan, spermine, Ca2+ | small-molecule | No | No | Park J, Zuo H, Frangaj A, Fu Z, Yen LY, Zhang Z, Mosyak L, Slavkovich VN, Liu J, Ray KM, Cao B, Vallese F, Geng Y, Chen S, Grassucci R, Dandey VP, Tan YZ, Eng E, Lee Y, Kloss B, Liu Z, Hendrickson WA, Potter CS, Carragher B, Graziano J, Conigrave AD, Frank J, Clarke OB, Fan QR | 10.1073/PNAS.2115849118 | 2022-01-19 | Yes | |
MTR1A | MT1 | Melatonin | A | Human | Cryo-EM | 7VGY | - | 3.1 | A | Active | 100 | 80 | Gi/o | αi1 | - | 62 | - | scFv16 |
2-iodo-melatonin
|
small-molecule | Agonist | melatonin | small-molecule | No | No | Wang Q, Lu Q, Guo Q, Teng M, Gong Q, Li X, Du Y, Liu Z, Tao Y | 10.1038/S41467-022-28111-3 | 2022-03-02 | Yes | |
ADA2A | α2A | Adrenoceptors | A | Human | Cryo-EM | 7EJ0 | - | 3.2 | R | Active | 100 | 56 | Gi/o | αo | - | 61 | - | scFv16 |
(-)-noradrenaline
|
small-molecule | Agonist | (-)-adrenaline, (-)-noradrenaline | small-molecule | No | No | Xu J, Cao S, Hubner H, Weikert D, Chen G, Lu Q, Yuan D, Gmeiner P, Liu Z, Du Y | 10.1126/SCIADV.ABJ5347 | 2022-04-13 | Yes | |
FPR2 | FPR2/ALX | Formylpeptide | A | Human | Cryo-EM | 7WVX | - | 2.8 | R | Active | 100 | 85 | Gi/o | αi2 | - | 61 | BRIL | - |
humanin
|
peptide | 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 | Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B | 10.1038/S41467-022-29361-X | 2022-04-13 | Yes | |
VIPR2 | VPAC2 | VIP and PACAP | B1 | Human | Cryo-EM | 7WBJ | - | 3.4 | R | Active | 100 | 82 | Gs | αs | - | 60 | - | Nanobody-35 |
PACAP-27
|
peptide | Agonist | VIP, PHI, secretin, PACAP-27, GHRH, PACAP-38 | peptide | No | No | Xu Y, Feng W, Zhou Q, Liang A, Li J, Dai A, Zhao F, Yan J, Chen CW, Li H, Zhao LH, Xia T, Jiang Y, Xu HE, Yang D, Wang MW | 10.1038/S41467-022-30041-Z | 2022-05-18 | Yes | |
5HT5A | 5-HT5A | 5-Hydroxytryptamine | A | Human | Cryo-EM | 7UM5 | 7UM5_refined | 2.7 | A | Active | 100 | 75 | Gi/o | αo | Mini-Go | 60 | - | scFv16 |
5-CT
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | No | No | Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL | 10.1038/S41594-022-00796-6 | 2022-07-20 | Yes | |
ACKR3 | ACKR3 | Chemokine | A | Human | Cryo-EM | 7SK5 | 7SK5_refined | 4.0 | A | Active | 97 | 83 | - | - | - | - | - | CID24 Fab heavy chain CID24 Fab light chain anti-Fab Nanobody |
Stromal cell-derived factor 1
|
peptide | Agonist | CXCL11, CXCL12α | peptide | No | No | Yen YC, Schafer CT, Gustavsson M, Eberle SA, Dominik PK, Deneka D, Zhang P, Schall TJ, Kossiakoff AA, Tesmer JJG, Handel TM | 10.1126/SCIADV.ABN8063 | 2022-07-27 | Yes | |
SSR2 | SST2 | Somatostatin | A | Human | Cryo-EM | 7Y27 | 7Y27_refined | 3.5 | E | Active | 100 | 74 | Gq/11 | αq | Mini-Gq | 60 | - | scFv16 |
SOMATOSTATIN
|
protein | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | No | No | Chen S, Teng X, Zheng S | 10.1038/S41589-022-01130-3 | 2022-10-19 | Yes | |
OPRM | μ | Opioid | A | Human | Cryo-EM | 8F7R | - | 3.3 | R | Active | 100 | 72 | Gi/o | αi1 | - | 63 | - | scFv16 |
endomorphin-1
|
peptide | 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 | Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y, Roth BL, Xu HE | 10.1016/J.CELL.2022.12.026 | 2022-12-14 | Yes | |
NTR1 | NTS1 | Neurotensin | A | Rat | Cryo-EM | 8FMZ | - | 2.6 | A | Active | 100 | 66 | Gq/11 | αq | Mini-Gq | 57 | - | scFv16 |
neurotensin
|
peptide | Agonist | neurotensin, neuromedin N | peptide | No | No | Krumm BE, DiBerto JF, Olsen RHJ, Kang HJ, Slocum ST, Zhang S, Strachan RT, Huang XP, Slosky LM, Pinkerton AB, Barak LS, Caron MG, Kenakin T, Fay JF, Roth BL | 10.1021/ACS.BIOCHEM.3C00029 | 2023-03-29 | Yes | |
FFAR4 | FFA4 | Free fatty acid | A | Human | Cryo-EM | 8ID4 | - | 3.1 | R | Active | 100 | 79 | Gi/o | αi1 | - | 64 | - | scFv16 |
linoleic acid
|
small-molecule | Agonist | 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 | 8IW4 | - | 3.5 | R | Active | 100 | 85 | Gs | αs | - | 45 | - | scFv16 |
SPERMIDINE
|
small-molecule | Agonist | - | - | No | No | Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP | 10.1038/S41586-023-06106-4 | 2023-05-31 | Yes | |
GPR12 | GPR12 | A orphans | A | Human | Cryo-EM | 7Y3G | 7Y3G_refined | 2.8 | R | Active | 100 | 78 | Gs | αs | - | 56 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | sphingosine 1-phosphate | small-molecule | No | No | Li H, Zhang J, Yu Y, Luo F, Wu L, Liu J, Chen N, Liu Z, Hua T | 10.1016/J.SCIB.2022.12.023 | 2023-06-07 | Yes | |
C3AR | C3a | Complement peptide | A | Human | Cryo-EM | 8IA8 | - | 2.9 | A | Active | 100 | 59 | Gi/o | αi1 | - | 61 | - | scFv16 |
ALA-SER-LYS-LEU-GLY-LEU-ALA-ARG
|
peptide | Agonist | C5a, C3a | peptide | No | No | - | - | 2023-05-24 | Yes | |
ADA1A | α1A | Adrenoceptors | A | Human | Cryo-EM | 7YMJ | - | 3.4 | A | Inactive | 6 | 60 | - | - | - | - | - | Nanobody-6 |
tamsulosin
|
small-molecule | Antagonist | (-)-adrenaline, (-)-noradrenaline | small-molecule | No | No | Toyoda Y, Zhu A, Kong F, Shan S, Zhao J, Wang N, Sun X, Zhang L, Yan C, Kobilka BK, Liu X | 10.1038/S41467-023-39310-X | 2023-07-05 | Yes | |
GRPR | BB2 | Bombesin | A | Human | Cryo-EM | 8H0Q | - | 3.3 | R | Active | 100 | 77 | Gq/11 | αq | - | 56 | - | - |
Gastrin-releasing peptide
|
peptide | Agonist | neuromedin B, gastrin releasing peptide(14-27) (human), GRP-(18-27), gastrin-releasing peptide, neuromedin C | peptide | No | No | Li C, Xu Y, Liu H, Cai H, Jiang Y, Xu HE, Yin W | 10.1038/S41422-022-00743-6 | 2023-08-09 | Yes | |
GRM2 | mGlu2 | Metabotropic glutamate | C | Human | Cryo-EM | 8JCU | - | 2.8 | 2 | Inactive | - | 87 | - | - | - | - | - | - |
LY341495
|
small-molecule | Antagonist | L-glutamic acid | small-molecule | No | No | Wang X, Wang M, Xu T, Feng Y, Shao Q, Han S, Chu X, Xu Y, Lin S, Zhao Q, Wu B | 10.1038/S41422-023-00830-2 | 2023-06-21 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 8A2P | - | 3.5 | A | Inactive | 0 | 71 | - | - | - | - | BRIL | - |
CHEMBL1671936
|
small-molecule | Antagonist | adenosine | small-molecule | No | No | Birch J, Kwan TOC, Judge PJ, Axford D, Aller P, Butryn A, Reis RI, Bada Juarez JF, Vinals J, Owen RL, Nango E, Tanaka R, Tono K, Joti Y, Tanaka T, Owada S, Sugahara M, Iwata S, Orville AM, Watts A, Moraes I | 10.1107/S1600576723006428 | 2023-08-30 | Yes | |
CXCR3 | CXCR3 | Chemokine | A | Human | Cryo-EM | 8HNL | - | 3.0 | R | Active | 100 | 80 | - | - | - | - | - | - |
(3S)-N-[(2S)-5-carbamimidamido-1-(cyclohexylmethylamino)-1-oxidanylidene-pentan-2-yl]-2-(4-oxidanylidene-4-phenyl-butanoyl)-3,4-dihydro-1H-isoquinoline-3-carboxamide
|
small-molecule | Agonist | 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 | |
MC5R | MC5 | Melanocortin | A | Human | Cryo-EM | 8IOD | - | 2.6 | R | Active | 100 | 83 | Gs | αs | Gi1-Gs chimera | 59 | - | Nanobody-35 |
PG-901
|
peptide | Agonist | β-MSH, α-MSH, agouti-related protein, γ-MSH, ACTH | peptide | No | No | Chen VB, Arendall WB 3rd, Headd JJ, Keedy DA, Immormino RM, Kapral GJ, Murray LW, Richardson JS, Richardson DC | 10.1107/S0907444909042073 | 2023-09-20 | 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 | β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, 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 | |
O52E4 | Olfactory 52E4 | Olfactory | A | Human | Cryo-EM | 8W77 | - | 3.6 | A | Intermediate | 49 | 83 | - | - | - | - | BRIL | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Choi C, Bae J, Kim S, Lee S, Kang H, Kim J, Bang I, Kim K, Huh WK, Seok C, Park H, Im W, Choi HJ | 10.1038/S41467-023-43983-9 | 2023-12-20 | Yes | |
TAAR1 | TA1 | Trace amine | A | Mouse | Cryo-EM | 8WC9 | - | 3.2 | R | Active | 100 | 79 | Gq/11 | αq | - | 58 | - | scFv16 |
CHEMBL476516
|
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 | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 4LDE | 4LDE_refined | 2.8 | A | Active | 99 | 69 | - | - | - | - | T4-Lysozyme | Nanobody |
CHEMBL1615159
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline | small-molecule | No | No | Ring AM, Manglik A, Kruse AC, Enos MD, Weis WI, Garcia KC, Kobilka BK | 10.1038/NATURE12572 | 2013-09-25 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 4UG2 | 4UG2_refined | 2.6 | A | Active | 72 | 71 | - | - | - | - | - | - |
CGS 21680
|
small-molecule | Agonist | adenosine | small-molecule | No | No | Lebon G, Edwards PC, Leslie AG, Tate CG | 10.1124/mol.114.097360 | 2015-04-08 | Yes | |
SMO | SMO | Frizzled | F | Human | X-ray | 5L7D | 5L7D_refined | 3.2 | B | Inactive | 4 | 59 | - | - | - | - | BRIL | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | 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 | |
AA1R | A1 | Adenosine | A | Human | X-ray | 5N2S | 5N2S_refined | 3.3 | A | Inactive | 0 | 86 | - | - | - | - | BRIL | - |
PSB36
|
small-molecule | Agonist | adenosine | small-molecule | No | No | Cheng RKY, Segala E, Robertson N, Deflorian F, Dore AS, Errey JC, Fiez-Vandal C, Marshall FH, Cooke RM | 10.1016/j.str.2017.06.012 | 2017-07-26 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5OLZ | 5OLZ_refined | 1.9 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
CHEMBL2024114
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | Rucktooa P, Cheng RKY, Segala E, Geng T, Errey JC, Brown GA, Cooke RM, Marshall FH, Dore AS | 10.1038/S41598-017-18570-W | 2018-01-17 | Yes | |
Q98SW5 | SMO | Frizzled | F | African clawed frog | X-ray | 6D35 | 6D35_refined | 3.9 | A | Active | 78 | 58 | - | - | - | - | BRIL | - |
Cholesterol
|
small-molecule | Agonist | - | - | No | No | Huang P, Zheng S, Wierbowski BM, Kim Y, Nedelcu D, Aravena L, Liu J, Kruse AC, Salic A | 10.1016/J.CELL.2018.04.029 | 2018-05-23 | Yes | |
ACM2 | M2 | Acetylcholine (muscarinic) | A | Human | X-ray | 5YC8 | 5YC8_refined | 2.5 | A | Inactive | 2 | 60 | - | - | - | - | BRIL | - |
N-methyl scopolamine
|
small-molecule | Antagonist | acetylcholine | small-molecule | No | No | Suno R, Lee S, Maeda S, Yasuda S, Yamashita K, Hirata K, Horita S, Tawaramoto MS, Tsujimoto H, Murata T, Kinoshita M, Yamamoto M, Kobilka BK, Vaidehi N, Iwata S, Kobayashi T | 10.1038/S41589-018-0152-Y | 2018-11-21 | Yes | |
AGTR1 | AT1 | Angiotensin | A | Human | X-ray | 6DO1 | 6DO1_refined | 2.9 | A | Active | 93 | 85 | - | - | - | - | BRIL | Nanobody-Nb.AT110i1 |
CHEMBL404594
|
protein | Agonist | angiotensin IV, angiotensin II, angiotensin III, angiotensin A | 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 | 6RZ4 | - | 2.7 | A | Active | 59 | 85 | - | - | - | - | BRIL | - |
pranlukast
|
small-molecule | Antagonist | LTD4, LTC4, LTE4 | small-molecule | No | Yes | 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 | |
OPRD | δ | Opioid | A | Human | X-ray | 6PT3 | 6PT3_refined | 3.3 | A | Active | 72 | 78 | - | - | - | - | BRIL | - |
DPI-287
|
small-molecule | Agonist | [Leu]enkephalin, β-endorphin, dynorphin A, [Met]enkephalin, endomorphin-1, α-neoendorphin, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13) | 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 | |
CNR2 | CB2 | Cannabinoid | A | Human | Cryo-EM | 6PT0 | 6PT0_refined | 3.2 | R | Active | 100 | 83 | Gi/o | αi1 | - | 100 | - | scFv16 |
WIN55212-2
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | No | No | Xing C, Zhuang Y, Xu TH, Feng Z, Zhou XE, Chen M, Wang L, Meng X, Xue Y, Wang J, Liu H, McGuire TF, Zhao G, Melcher K, Zhang C, Xu HE, Xie XQ | 10.1016/J.CELL.2020.01.007 | 2020-02-12 | Yes | |
GABR2 | GABAB2 | GABAB | C | Human | Cryo-EM | 6W2X | - | 3.6 | B | Inactive | - | 71 | - | - | - | - | - | - |
CGP55845
1-Stearoyl-2-oleoyl-sn-glycero-3-phosphoethanolamine |
small-molecule small-molecule |
Inverse agonist NAM |
- | - | No | No | Papasergi-Scott MM, Robertson MJ, Seven AB, Panova O, Mathiesen JM, Skiniotis G | 10.1038/S41586-020-2469-4 | 2020-07-01 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 6ZDR | 6ZDR_refined | 1.9 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
CHEMBL2030687
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | Jespers W, Verdon G, Azuaje J, Majellaro M, Keranen H, Garcia-Mera X, Congreve M, Deflorian F, de Graaf C, Zhukov A, Dore AS, Mason JS, Aqvist J, Cooke RM, Sotelo E, Gutierrez-de-Teran H | 10.1002/ANIE.202003788 | 2020-09-16 | Yes | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 6XOX | - | 3.1 | R | Active | 100 | 82 | Gs | αs | - | 56 | - | scFv16 Nanobody-35 |
orforglipron
|
small-molecule | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | No | No | Kawai T, Sun B, Yoshino H, Feng D, Suzuki Y, Fukazawa M, Nagao S, Wainscott DB, Showalter AD, Droz BA, Kobilka TS, Coghlan MP, Willard FS, Kawabe Y, Kobilka BK, Sloop KW | 10.1073/PNAS.2014879117 | 2020-11-18 | Yes | |
DRD1 | D1 | Dopamine | A | Human | Cryo-EM | 7JVP | - | 2.9 | R | Active | 100 | 63 | Gs | αs | - | 60 | - | Nanobody-35 |
39YLC3L0ZU
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | No | No | - | - | 2021-02-24 | Yes | |
PE2R2 | EP2 | Prostanoid | A | Human | Cryo-EM | 7CX4 | 7CX4_refined | 2.9 | R | Active | 100 | 74 | Gs | αs | - | 58 | - | Nanobody-35 |
evatanepag
|
small-molecule | Agonist | thromboxane A2, PGF2α, PGI2, PGD2, PGE1, PGE2 | small-molecule | No | No | Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y | 10.1126/SCIADV.ABF1268 | 2021-05-05 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | Cryo-EM | 7MT8 | 7MT8_refined | 5.8 | R | Active | 97 | 93 | - | - | - | - | - | 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 | |
GHSR | ghrelin | Ghrelin | A | Human | Cryo-EM | 7F9Y | - | 2.9 | R | Active | 100 | 78 | Gq/11 | αq | Engineered G alpha | 59 | - | Nanobody-35 |
ghrelin
|
peptide | Agonist | [des-Gln14]ghrelin, ghrelin | peptide | No | No | Wang Y, Guo S, Zhuang Y, Yun Y, Xu P, He X, Guo J, Yin W, Xu HE, Xie X, Jiang Y | 10.1038/S41467-021-25364-2 | 2021-08-18 | Yes | |
ACM1 | M1 | Acetylcholine (muscarinic) | A | Human | X-ray | 6ZG9 | 6ZG9_refined | 2.5 | A | Inactive | 2 | 62 | - | - | - | - | T4-Lysozyme | - |
7-fluoro-5-methyl-3-[1-(oxan-4-yl)piperidin-4-yl]-1H-benzimidazol-2-one
|
small-molecule | Agonist | acetylcholine | small-molecule | No | No | Brown AJH, Bradley SJ, Marshall FH, Brown GA, Bennett KA, Brown J, Cansfield JE, Cross DM, de Graaf C, Hudson BD, Dwomoh L, Dias JM, Errey JC, Hurrell E, Liptrot J, Mattedi G, Molloy C, Nathan PJ, Okrasa K, Osborne G, Patel JC, Pickworth M, Robertson N, Shahabi S, Bundgaard C, Phillips K, Broad LM, Goonawardena AV, Morairty SR, Browning M, Perini F, Dawson GR, Deakin JFW, Smith RT, Sexton PM, Warneck J, Vinson M, Tasker T, Tehan BG, Teobald B, Christopoulos A, Langmead CJ, Jazayeri A, Cooke RM, Rucktooa P, Congreve MS, Weir M, Tobin AB | 10.1016/J.CELL.2021.11.001 | 2021-10-06 | Yes | |
GP158 | GPR158 | C Orphans | C | Human | Cryo-EM | 7EWL | 7EWL_refined | 3.5 | A | Inactive | - | 41 | - | - | - | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Jeong E, Kim Y, Jeong J, Cho Y | 10.1038/S41467-021-27147-1 | 2021-12-01 | Yes | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 7S1M | 7S1M_refined | 2.4 | R | Active | 100 | 82 | Gs | αs | - | 59 | - | Nanobody-35 |
exendin-4
|
peptide | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | No | No | Cary BP, Deganutti G, Zhao P, Truong TT, Piper SJ, Liu X, Belousoff MJ, Danev R, Sexton PM, Wootten D, Gellman SH | 10.1038/S41589-021-00945-W | 2022-01-05 | Yes | |
CCR1 | CCR1 | Chemokine | A | Human | Cryo-EM | 7VL8 | 7VL8_refined | 2.9 | R | Active | 100 | 80 | Gi/o | αi1 | - | 62 | - | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | CCL14, CCL8, CCL13, CCL15, CCL4, CCL23, CCL7, CCL5, CCL3, CCL16 | peptide | No | No | Shao Z, Shen Q, Yao B, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Ma H, Chen ZH, Xu HE, Ying S, Zhang Y, Shen H | 10.1038/S41589-021-00918-Z | 2022-03-23 | Yes | |
GIPR | GIP | Glucagon | B1 | Human | Cryo-EM | 7FIN | - | 3.1 | R | Active | 100 | 82 | Gs | αs | - | 59 | - | Nanobody-35 |
Peptide-20
|
peptide | Agonist | gastric inhibitory polypeptide | peptide | No | No | Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW | 10.1038/S41467-022-28683-0 | 2022-02-23 | Yes | |
AGRD1 | ADGRD1 | ADGRD | B2 | Human | Cryo-EM | 7WU2 | - | 2.8 | R | Active | 100 | 32 | Gs | αs | Mini-Gs | 53 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | - | - | 2022-04-27 | Yes | |
OX2R | OX2 | Orexin | A | Human | Cryo-EM | 7SQO | - | 3.2 | R | Active | 100 | 61 | Gi/o | αi1 | - | 61 | - | scFv16 |
methyl (2R,3S)-3-[(methanesulfonyl)amino]-2-({[(1s,4S)-4-phenylcyclohexyl]oxy}methyl)piperidine-1-carboxylate
|
small-molecule | Agonist | orexin-A, orexin-B | peptide | No | No | Yin J, Kang Y, McGrath AP, Chapman K, Sjodt M, Kimura E, Okabe A, Koike T, Miyanohana Y, Shimizu Y, Rallabandi R, Lian P, Bai X, Flinspach M, De Brabander JK, Rosenbaum DM | 10.1038/S41467-022-30601-3 | 2022-05-25 | Yes | |
TRFR | TRH1 | Thyrotropin-releasing hormone | A | Human | Cryo-EM | 7WKD | - | 3.0 | R | Active | 100 | 66 | Gq/11 | αq | - | 60 | - | scFv16 |
TRH
|
peptide | Agonist | TRH | peptide | No | No | Xu Y, Cai H, You C, He X, Yuan Q, Jiang H, Cheng X, Jiang Y, Xu HE | 10.1038/S41422-022-00641-X | 2022-06-15 | Yes | |
GPBAR | GPBA | Bile acid | A | Human | Cryo-EM | 7XTQ | 7XTQ_refined | 3.2 | R | Active | 100 | 83 | Gs | αs | - | 58 | - | Nanobody-35 |
CHEMBL2181246
|
small-molecule | Agonist | deoxycholic acid, cholic acid, chenodeoxycholic acid, lithocholic acid | small-molecule | No | No | Ma L, Yang F, Wu X, Mao C, Guo L, Miao T, Zang SK, Jiang X, Shen DD, Wei T, Zhou H, Wei Q, Li S, Shu Q, Feng S, Jiang C, Chu B, Du L, Sun JP, Yu X, Zhang Y, Zhang P | 10.1073/PNAS.2117054119 | 2022-07-06 | Yes | |
TRFR | TRH1 | Thyrotropin-releasing hormone | A | Human | Cryo-EM | 7X1U | 7X1U_refined | 3.2 | A | Active | 100 | 68 | Gq/11 | αq | - | 57 | - | scFv16 |
TRH
|
peptide | Agonist | TRH | peptide | No | No | - | - | 2022-08-31 | Yes | |
PTH1R | PTH1 | Parathyroid hormone | B1 | Human | Cryo-EM | 7VVO | 7VVO_refined | 4.1 | R | Active | 100 | 51 | Gs | αs | - | 58 | - | Nanobody-35 |
Parathyroid hormone
|
peptide | Agonist | 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 | |
5HT2B | 5-HT2B | 5-Hydroxytryptamine | A | Human | Cryo-EM | 7SRQ | - | 2.7 | R | Active | 59 | 53 | - | - | - | - | - | - |
Lysergide
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | No | No | Cao C, Barros-Alvarez X, Zhang S, Kim K, Damgen MA, Panova O, Suomivuori CM, Fay JF, Zhong X, Krumm BE, Gumpper RH, Seven AB, Robertson MJ, Krogan NJ, Huttenhain R, Nichols DE, Dror RO, Skiniotis G, Roth BL | 10.1016/J.NEURON.2022.08.006 | 2022-09-21 | Yes | |
CRFR2 | CRF2 | Corticotropin-releasing factor | B1 | Human | Cryo-EM | 7TS0 | 7TS0_refined | 2.8 | P | Active | 100 | 72 | Gi/o | αo | - | 63 | - | scFv16 |
Urocortin
|
peptide | Agonist | urocortin 1, corticotrophin-releasing hormone, urocortin 2, urocortin 3 | peptide | No | No | Zhao LH, Lin J, Ji SY, Zhou XE, Mao C, Shen DD, He X, Xiao P, Sun J, Melcher K, Zhang Y, Yu X, Xu HE | 10.1038/S41467-022-33851-3 | 2022-11-09 | Yes | |
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 | |
OPRD | δ | Opioid | A | Human | Cryo-EM | 8F7S | 8F7S_refined | 3.0 | R | Active | 100 | 78 | Gi/o | αi1 | - | 62 | - | - |
DELTORPHIN II
|
protein | Agonist | [Leu]enkephalin, β-endorphin, dynorphin A, [Met]enkephalin, endomorphin-1, α-neoendorphin, dynorphin A-(1-8), dynorphin B, dynorphin A-(1-13) | peptide | No | No | Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y, Roth BL, Xu HE | 10.1016/J.CELL.2022.12.026 | 2022-12-14 | Yes | |
NTR1 | NTS1 | Neurotensin | A | Rat | Cryo-EM | 8FN1 | - | 2.9 | A | Active | 100 | 66 | Gi/o | αo | - | 60 | - | scFv16 |
neurotensin
|
peptide | Agonist | neurotensin, neuromedin N | peptide | No | No | Krumm BE, DiBerto JF, Olsen RHJ, Kang HJ, Slocum ST, Zhang S, Strachan RT, Huang XP, Slosky LM, Pinkerton AB, Barak LS, Caron MG, Kenakin T, Fay JF, Roth BL | 10.1021/ACS.BIOCHEM.3C00029 | 2023-03-29 | Yes | |
FSHR | FSH | Glycoprotein hormone | A | Human | Cryo-EM | 8I2G | - | 2.8 | R | Active | 100 | 86 | Gs | αs | fused Gs | 58 | - | Nanobody-35 |
Follitropin subunit beta
Glycoprotein alpha FSHR agonist 1 |
peptide peptide small-molecule |
Agonist | FSH | peptide | No | No | Duan J, Xu P, Zhang H, Luan X, Yang J, He X, Mao C, Shen DD, Ji Y, Cheng X, Jiang H, Jiang Y, Zhang S, Zhang Y, Xu HE | 10.1038/S41467-023-36170-3 | 2023-03-29 | Yes | |
C5AR1 | C5a1 | Complement peptide | A | Human | Cryo-EM | 8JZZ | 8JZZ_refined | 3.3 | A | Active | 100 | 84 | Gi/o | αo | - | 59 | - | scFv16 |
C5a des-Arg
|
peptide | Agonist | ribosomal protein S19, C5a, C5a des-Arg, 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 | |
TAAR1 | TA1 | Trace amine | A | Human | Cryo-EM | 8WC8 | - | 2.9 | R | Active | 100 | 81 | Gs | αs | - | 56 | - | scFv16 |
CHEMBL476516
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, dopamine | 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 | |
CCR5 | CCR5 | Chemokine | A | Human | X-ray | 4MBS | 4MBS_refined | 2.7 | A | Inactive | 19 | 83 | - | - | - | - | Rubredoxin | - |
maraviroc
|
small-molecule | Antagonist | CCL14, CCL8, CCL13, CCL4, CCL7, CCL2, CCL5, CCL11, CCL3, CCL16 | peptide | No | No | Tan Q, Zhu Y, Li J, Chen Z, Han GW, Kufareva I, Li T, Ma L, Fenalti G, Li J, Zhang W, Xie X, Yang H, Jiang H, Cherezov V, Liu H, Stevens RC, Zhao Q, Wu B | 10.1126/SCIENCE.1241475 | 2013-09-11 | Yes | |
AGTR1 | AT1 | Angiotensin | A | Human | X-ray | 4YAY | 4YAY_refined | 2.9 | A | Inactive | 6 | 79 | - | - | - | - | BRIL | - |
ZD-7155
|
small-molecule | Antagonist | angiotensin IV, angiotensin II, angiotensin III, angiotensin A | 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 | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5IU7 | 5IU7_refined | 1.9 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
2-(Furan-2-yl)-5-N-[2-(4-phenylpiperidin-1-yl)ethyl]-1H-[1,2,4]triazolo[1,5-a][1,3,5]triazin-8-ium-5,7-diamine
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | Segala E, Guo D, Cheng RK, Bortolato A, Deflorian F, Doré AS, Errey JC, Heitman LH, IJzerman AP, Marshall FH, Cooke RM. | 10.1021/acs.jmedchem.6b00653 | 2016-06-29 | Yes | |
AGTR2 | AT2 | Angiotensin | A | Human | X-ray | 5UNH | 5UNH_refined | 2.9 | B | Active | 99 | 75 | - | - | - | - | BRIL | - |
compound 2 [PMID: 28379944]
|
small-molecule | Antagonist | angiotensin-(1-7), angiotensin II, angiotensin III | peptide | No | No | Zhang H, Han GW, Batyuk A, Ishchenko A, White KL, Patel N, Sadybekov A, Zamlynny B, Rudd MT, Hollenstein K, Tolstikova A, White TA, Hunter MS, Weierstall U, Liu W, Babaoglu K, Moore EL, Katz RD, Shipman JM, Garcia-Calvo M, Sharma S, Sheth P, Soisson SM, Stevens RC, Katritch V, Cherezov V | 10.1038/NATURE22035 | 2017-04-05 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5NM4 | - | 1.7 | A | Inactive | 0 | 73 | - | - | - | - | BRIL | - |
ZM-241385
|
small-molecule | Antagonist | adenosine | small-molecule | No | No | - | - | 2017-09-27 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 6FK8 | 6FK8_refined | 2.9 | A | Active | 97 | 94 | - | - | - | - | - | - |
(2~{R},3~{S})-3-azanyl-2-(4-chlorophenyl)-1-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-yl-butan-1-one
|
small-molecule | Agonist | - | - | No | No | Mattle D, Kuhn B, Aebi J, Bedoucha M, Kekilli D, Grozinger N, Alker A, Rudolph MG, Schmid G, Schertler GFX, Hennig M, Standfuss J, Dawson RJP | 10.1073/PNAS.1718084115 | 2018-04-04 | Yes | |
5HT2B | 5-HT2B | 5-Hydroxytryptamine | A | Human | X-ray | 6DS0 | - | 3.2 | A | Active | 59 | 59 | - | - | - | - | BRIL | - |
LY266097
|
small-molecule | Antagonist | 5-hydroxytryptamine | small-molecule | No | No | McCorvy JD, Wacker D, Wang S, Agegnehu B, Liu J, Lansu K, Tribo AR, Olsen RHJ, Che T, Jin J, Roth BL | 10.1038/s41594-018-0116-7 | 2018-08-29 | Yes | |
EDNRB | ETB | Endothelin | A | Human | X-ray | 6IGL | - | 2.7 | A | Inactive | 4 | 70 | - | - | - | - | T4-Lysozyme | - |
sovateltide
|
peptide | Agonist (partial) | endothelin-1, endothelin-2, endothelin-3 | peptide | No | No | 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 | Yes | 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 | |
OX1R | OX1 | Orexin | A | Human | X-ray | 6TP3 | 6TP3_refined | 3.0 | A | Inactive | 0 | 74 | - | - | - | - | - | - |
daridorexant
|
small-molecule | Antagonist | orexin-A, orexin-B | peptide | No | No | Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA. | 10.1021/acs.jmedchem.9b01787 | 2020-01-01 | Yes | |
DRD2 | D2 | Dopamine | A | Human | X-ray | 6LUQ | 6LUQ_refined | 3.1 | A | Inactive | 0 | 59 | - | - | - | - | T4-Lysozyme | - |
haloperidol
|
small-molecule | Antagonist | dopamine | small-molecule | No | No | Fan L, Tan L, Chen Z, Qi J, Nie F, Luo Z, Cheng J, Wang S | 10.1038/S41467-020-14884-Y | 2020-03-04 | Yes | |
GABR2 | GABAB2 | GABAB | C | Human | Cryo-EM | 6UO8 | - | 3.6 | B | Active | - | 74 | - | - | - | - | - | - |
CHEMBL112710
GS39783 |
small-molecule small-molecule |
Agonist PAM |
- | - | No | No | Shaye H, Ishchenko A, Lam JH, Han GW, Xue L, Rondard P, Pin JP, Katritch V, Gati C, Cherezov V | 10.1038/S41586-020-2408-4 | 2020-06-10 | Yes | |
FZD5 | FZD5 | Frizzled | F | Human | Cryo-EM | 6WW2 | 6WW2_refined | 3.7 | R | Inactive | 22 | 55 | - | - | - | - | BRIL | anti-BRIL Fab heavy chain anti-BRIL Fab light chain anti-Fab Nanobody |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Tsutsumi N, Mukherjee S, Waghray D, Janda CY, Jude KM, Miao Y, Burg JS, Aduri NG, Kossiakoff AA, Gati C, Garcia KC | 10.7554/ELIFE.58464 | 2020-08-19 | Yes | |
SMO | SMO | Frizzled | F | Human | Cryo-EM | 6XBK | - | 3.2 | R | Active | 100 | 59 | Gi/o | αi1 | - | 61 | - | scFv16 |
Cholesterol
|
small-molecule | Agonist | - | - | No | No | Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X | 10.1038/S41589-020-0646-2 | 2020-09-30 | Yes | |
GLP1R | GLP-1 | Glucagon | B1 | Human | Cryo-EM | 7LCK | 7LCK_refined | 3.2 | R | Active | 99 | 84 | - | - | - | - | - | - |
danuglipron
|
small-molecule | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | No | No | Zhang X, Johnson RM, Drulyte I, Yu L, Kotecha A, Danev R, Wootten D, Sexton PM, Belousoff MJ | 10.1016/J.STR.2021.04.008 | 2021-01-20 | Yes | |
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, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, 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 | |
CCKAR | CCK1 | Cholecystokinin | A | Human | Cryo-EM | 7MBY | - | 2.4 | R | Active | 100 | 66 | Gq/11 | αq | Gq-Gs-Gi1 chimera | 55 | - | - |
CHEMBL216166
|
protein | Agonist | desulfated cholecystokinin-8, CCK-58, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8 | peptide | No | No | Mobbs JI, Belousoff MJ, Harikumar KG, Piper SJ, Xu X, Furness SGB, Venugopal H, Christopoulos A, Danev R, Wootten D, Thal DM, Miller LJ, Sexton PM | 10.1371/JOURNAL.PBIO.3001295 | 2021-05-26 | Yes | |
ADRB3 | β3 | Adrenoceptors | A | Dog | Cryo-EM | 7DH5 | - | 3.2 | R | Active | 100 | 68 | Gs | αs | - | 59 | - | Nanobody-35 |
mirabegron
|
small-molecule | Agonist | - | - | No | No | Nagiri C, Kobayashi K, Tomita A, Kato M, Kobayashi K, Yamashita K, Nishizawa T, Inoue A, Shihoya W, Nureki O | 10.1016/J.MOLCEL.2021.06.024 | 2021-08-04 | Yes | |
AA1R | A1 | Adenosine | A | Human | Cryo-EM | 7LD3 | - | 3.2 | R | Active | 100 | 88 | Gi/o | αi2 | - | 59 | - | - |
{2-Amino-4-[3,5-bis(trifluoromethyl)phenyl]thiophen-3-yl}(4-chlorophenyl)methanone
adenosine |
small-molecule small-molecule |
Ago-PAM Agonist |
adenosine | small-molecule | No | No | Draper-Joyce CJ, Bhola R, Wang J, Bhattarai A, Nguyen ATN, Cowie-Kent I, O'Sullivan K, Chia LY, Venugopal H, Valant C, Thal DM, Wootten D, Panel N, Carlsson J, Christie MJ, White PJ, Scammells P, May LT, Sexton PM, Danev R, Miao Y, Glukhova A, Imlach WL, Christopoulos A | 10.1038/S41586-021-03897-2 | 2021-09-08 | Yes | |
MC4R | MC4 | Melanocortin | A | Human | Cryo-EM | 7F58 | 7F58_refined | 3.1 | R | Active | 100 | 82 | Gs | αs | - | 58 | - | Nanobody-35 |
THIQ
|
small-molecule | Agonist | β-MSH, α-MSH, 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 | 7VV5 | 7VV5_refined | 2.8 | R | Active | 100 | 81 | Gi/o | αi1 | - | 64 | - | scFv16 |
compound 48/80
|
small-molecule | Agonist | PAMP-20 | peptide | No | No | Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP | 10.1038/S41586-021-04077-Y | 2021-12-01 | Yes | |
US28 | US28 | Unclassified | A | strain AD169 | Cryo-EM | 7RKM | - | 3.5 | R | Active | 100 | 83 | Gi/o | αi1 | - | 61 | - | scFv16 |
Fractalkine
|
peptide | Agonist | - | - | No | No | Tsutsumi N, Maeda S, Qu Q, Vogele M, Jude KM, Suomivuori CM, Panova O, Waghray D, Kato HE, Velasco A, Dror RO, Skiniotis G, Kobilka BK, Garcia KC | 10.1126/SCIADV.ABL5442 | 2022-01-26 | Yes | |
ADA2A | α2A | Adrenoceptors | A | Human | Cryo-EM | 7EJK | - | 3.4 | R | Active | 100 | 55 | Gi/o | αo | - | 61 | - | scFv16 |
oxymetazoline
|
small-molecule | Agonist | (-)-adrenaline, (-)-noradrenaline | small-molecule | No | No | Xu J, Cao S, Hubner H, Weikert D, Chen G, Lu Q, Yuan D, Gmeiner P, Liu Z, Du Y | 10.1126/SCIADV.ABJ5347 | 2022-04-13 | Yes | |
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 | - | - | 2022-04-20 | Yes | |
BKRB2 | B2 | Bradykinin | A | Human | Cryo-EM | 7F6H | 7F6H_refined | 2.9 | A | Active | 100 | 78 | Gq/11 | αq | - | 63 | - | - |
bradykinin
|
peptide | Agonist | [des-Arg10]kallidin, Lys-[Hyp3]-bradykinin, kallidin, [des-Arg9]bradykinin, [Hyp3]bradykinin, T-kinin, bradykinin | peptide | No | No | Shen J, Zhang D, Fu Y, Chen A, Yang X, Zhang H | 10.1038/S41467-022-28399-1 | 2022-01-05 | Yes | |
CNR1 | CB1 | Cannabinoid | A | Human | Cryo-EM | 7WV9 | - | 3.4 | R | Active | 100 | 61 | Gi/o | αi2 | - | 63 | - | scFv16 |
CP55940
6-methyl-3-[(1S)-2-nitro-1-thiophen-2-yl-ethyl]-2-phenyl-1H-indole |
small-molecule small-molecule |
Agonist PAM |
2-arachidonoylglycerol, anandamide | small-molecule | No | No | Yang X, Wang X, Xu Z, Wu C, Zhou Y, Wang Y, Lin G, Li K, Wu M, Xia A, Liu J, Cheng L, Zou J, Yan W, Shao Z, Yang S | 10.1038/S41589-022-01038-Y | 2022-06-15 | Yes | |
ACKR3 | ACKR3 | Chemokine | A | Human | Cryo-EM | 7SK4 | 7SK4_refined | 3.3 | A | Active | 97 | 84 | - | - | - | - | - | CID25 Fab light chain CID25 Fab heavy chain CID24 Fab light chain CID24 Fab heavy chain |
Stromal cell-derived factor 1
|
peptide | Agonist | CXCL11, CXCL12α | peptide | No | No | Yen YC, Schafer CT, Gustavsson M, Eberle SA, Dominik PK, Deneka D, Zhang P, Schall TJ, Kossiakoff AA, Tesmer JJG, Handel TM | 10.1126/SCIADV.ABN8063 | 2022-07-27 | Yes | |
OPRM | μ | Opioid | A | Human | Cryo-EM | 8EFB | 8EFB_refined | 3.2 | R | Active | 100 | 71 | Gi/o | αi1 | - | 64 | - | scFv16 |
OLICERIDINE
|
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 | |
NPY2R | Y2 | Neuropeptide Y | A | Human | Cryo-EM | 7YOO | 7YOO_refined | 3.1 | R | Active | 98 | 79 | - | - | - | - | - | - |
neuropeptide Y
|
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 | |
FFAR4 | FFA4 | Free fatty acid | A | Human | Cryo-EM | 8ID9 | 8ID9_refined | 3.0 | R | Active | 100 | 78 | Gi/o | αi1 | - | 56 | - | scFv16 |
EPA
|
small-molecule | Agonist | 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 | |
MTLR | motilin | Motilin | A | Human | Cryo-EM | 8IBV | 8IBV_refined | 3.2 | R | Active | 100 | 68 | Gq/11 | αq | - | 60 | BRIL | scFv16 |
motilin
|
peptide | Agonist | motilin | peptide | No | No | You C, Zhang Y, Xu Y, Xu P, Li Z, Li H, Huang S, Chen Z, Li J, Xu HE, Jiang Y | 10.1126/SCIADV.ADE9020 | 2023-04-12 | Yes | |
AA2BR | A2B | Adenosine | A | Human | Cryo-EM | 7XY6 | - | 3.0 | R | Active | 100 | 86 | Gs | αs | - | 57 | BRIL | - |
BAY 60-6583
|
small-molecule | Agonist | adenosine | small-molecule | No | No | Chen Y, Zhang J, Weng Y, Xu Y, Lu W, Liu W, Liu M, Hua T, Song G | 10.1126/SCIADV.ADD3709 | 2023-05-03 | Yes | |
FFAR4 | FFA4 | Free fatty acid | A | Human | Cryo-EM | 8H4L | - | 3.1 | R | Active | 100 | 84 | Gq/11 | αq | - | 60 | - | 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 | |
GRM2 | mGlu2 | Metabotropic glutamate | C | Human | Cryo-EM | 8JD1 | - | 3.7 | 2 | Inactive | - | 86 | - | - | - | - | - | - |
L-glutamic acid
|
small-molecule | Agonist | L-glutamic acid | small-molecule | No | No | Wang X, Wang M, Xu T, Feng Y, Shao Q, Han S, Chu X, Xu Y, Lin S, Zhao Q, Wu B | 10.1038/S41422-023-00830-2 | 2023-06-21 | Yes | |
PE2R4 | EP4 | Prostanoid | A | Human | Cryo-EM | 8GDA | - | 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 | 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 | |
C3AR | C3a | Complement peptide | A | Human | Cryo-EM | 8I97 | 8I97_refined | 3.2 | C | Active | 100 | 57 | Gi/o | αo | - | 59 | - | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | 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 | |
GP174 | GPR174 | A orphans | A | Human | Cryo-EM | 8IZB | - | 3.1 | R | Active | 100 | 85 | Gs | αs | - | 60 | - | Nanobody-35 |
L-serine
LYSOPHOSPHATIDIC ACID |
small-molecule small-molecule |
Agonist | lysophosphatidylserine | small-molecule | No | No | Liu G, Li X, Wang Y, Zhang X, Gong W | 10.1371/JOURNAL.PBIO.3002387 | 2023-11-01 | Yes | |
CXCR3 | CXCR3 | Chemokine | A | Human | Cryo-EM | 8K2X | 8K2X_refined | 3.2 | R | Active | 100 | 79 | Gi/o | αi1 | - | 62 | BRIL | scFv16 |
C-X-C motif chemokine 10
|
small-molecule | Agonist | CCL19, CXCL11, CCL13, CXCL9, CXCL10, CCL7, CCL5, CCL11, CXCL12α, CCL20 | peptide | No | No | Jiao H, Pang B, Chiang YC, Chen Q, Pan Q, Ren R, Hu H | 10.1038/S41421-023-00617-0 | 2023-11-29 | Yes | |
TAAR1 | TA1 | Trace amine | A | Mouse | Cryo-EM | 8WC4 | - | 3.1 | R | Active | 100 | 82 | Gs | αs | - | 59 | - | scFv16 |
CHEMBL476516
|
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 | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 4LDL | 4LDL_refined | 3.1 | A | Active | 99 | 69 | - | - | - | - | T4-Lysozyme | Nanobody |
hydroxybenzylisoproterenol
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline | small-molecule | No | No | Ring AM, Manglik A, Kruse AC, Enos MD, Weis WI, Garcia KC, Kobilka BK | 10.1038/NATURE12572 | 2013-09-25 | Yes | |
US28 | US28 | Unclassified | A | strain AD169 | X-ray | 4XT1 | - | 2.9 | A | Active | 100 | 82 | - | - | - | - | - | Nanobody |
CX3CL1
|
peptide | Agonist (partial) | - | - | No | No | Burg JS, Ingram JR, Venkatakrishnan AJ, Jude KM, Dukkipati A, Feinberg EN, Angelini A, Waghray D, Dror RO, Ploegh HL, Garcia KC | 10.1126/SCIENCE.AAA5026 | 2015-03-04 | Yes | |
AA1R | A1 | Adenosine | A | Human | X-ray | 5UEN | 5UEN_refined | 3.2 | B | Inactive | 0 | 91 | - | - | - | - | BRIL | - |
DU172
|
small-molecule | Antagonist | adenosine | small-molecule | No | No | Glukhova A, Thal DM, Nguyen AT, Vecchio EA, Jorg M, Scammells PJ, May LT, Sexton PM, Christopoulos A | 10.1016/j.cell.2017.01.042 | 2017-03-01 | Yes | |
EDNRB | ETB | Endothelin | A | Human | X-ray | 5X93 | 5X93_refined | 2.2 | A | Inactive | 4 | 71 | - | - | - | - | T4-Lysozyme | - |
K-8794
|
small-molecule | Antagonist | endothelin-1, endothelin-2, endothelin-3 | peptide | No | No | Shihoya W, Nishizawa T, Yamashita K, Inoue A, Hirata K, Kadji FMN, Okuta A, Tani K, Aoki J, Fujiyoshi Y, Doi T, Nureki O | 10.1038/NSMB.3450 | 2017-08-16 | Yes | |
GRM5 | mGlu5 | Metabotropic glutamate | C | Human | X-ray | 6FFI | 6FFI_refined | 2.2 | A | Inactive | - | 20 | - | - | - | - | T4-Lysozyme | - |
methoxy-MPEP
|
small-molecule | NAM | L-glutamic acid | small-molecule | No | No | - | - | 2018-03-07 | Yes | |
OPSD | Rhodopsin | Opsins | A | Human | Cryo-EM | 6CMO | - | 4.5 | R | Active | 75 | 92 | Gi/o | αi1 | - | 100 | BRIL | Fab |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Kang Y, Kuybeda O, de Waal PW, Mukherjee S, Van Eps N, Dutka P, Zhou XE, Bartesaghi A, Erramilli S, Morizumi T, Gu X, Yin Y, Liu P, Jiang Y, Meng X, Zhao G, Melcher K, Ernst OP, Kossiakoff AA, Subramaniam S, Xu HE | 10.1038/S41586-018-0215-Y | 2018-06-20 | Yes | |
CNR1 | CB1 | Cannabinoid | A | Human | Cryo-EM | 6N4B | 6N4B_refined | 3.0 | R | Active | 100 | 58 | Gi/o | αi1 | - | 62 | - | scFv16 |
MDMB-Fubinaca
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | No | No | Krishna Kumar K, Shalev-Benami M, Robertson MJ, Hu H, Banister SD, Hollingsworth SA, Latorraca NR, Kato HE, Hilger D, Maeda S, Weis WI, Farrens DL, Dror RO, Malhotra SV, Kobilka BK, Skiniotis G | 10.1016/J.CELL.2018.11.040 | 2019-01-30 | 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-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | 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 | |
OX2R | OX2 | Orexin | A | Human | X-ray | 6TPG | 6TPG_refined | 2.7 | A | Inactive | 0 | 69 | - | - | - | - | GlgA glycogen synthase | - |
EMPA
|
small-molecule | Antagonist | orexin-A, orexin-B | peptide | No | No | Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA. | 10.1021/acs.jmedchem.9b01787 | 2020-01-01 | Yes | |
ACM2 | M2 | Acetylcholine (muscarinic) | A | Human | Cryo-EM | 6U1N | 6U1N_refined | 4.0 | R | Active | 100 | 57 | Beta | Beta-arrestin-1 | - | 86 | - | Fab30 light chain Fab30 heavy chain |
LY2119620
|
small-molecule | Agonist | acetylcholine | small-molecule | No | No | Staus DP, Hu H, Robertson MJ, Kleinhenz ALW, Wingler LM, Capel WD, Latorraca NR, Lefkowitz RJ, Skiniotis G | 10.1038/S41586-020-1954-0 | 2020-02-26 | Yes | |
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 | |
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 | 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 | |
SMO | SMO | Frizzled | F | Human | Cryo-EM | 6XBL | - | 3.9 | R | Active | 100 | 59 | Gi/o | αi1 | - | 61 | - | scFv16 |
Cholesterol
SAG1.3 |
small-molecule small-molecule |
Agonist PAM |
- | - | No | No | Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X | 10.1038/S41589-020-0646-2 | 2020-09-30 | Yes | |
LT4R1 | BLT1 | Leukotriene | A | Human | X-ray | 7K15 | 7K15_refined | 2.9 | A | Inactive | 6 | 85 | - | - | - | - | Flavodoxin | - |
N-(tert-butylsulfonyl)-4-fluoro-2-{(3S,4R)-4-hydroxy-3-[(pyridin-2-yl)methyl]-3,4-dihydro-2H-1-benzopyran-7-yl}benzamide
|
small-molecule | Antagonist | 12R-HETE, LTB4, 20-hydroxy-LTB4 | small-molecule | No | Yes | Michaelian N, Sadybekov A, Besserer-Offroy E, Han GW, Krishnamurthy H, Zamlynny BA, Fradera X, Siliphaivanh P, Presland J, Spencer KB, Soisson SM, Popov P, Sarret P, Katritch V, Cherezov V | 10.1038/S41467-021-23149-1 | 2021-02-17 | Yes | |
HRH1 | H1 | Histamine | A | Human | Cryo-EM | 7DFL | - | 3.3 | R | Active | 100 | 56 | Gq/11 | αq | - | 63 | - | scFv16 |
histamine
|
small-molecule | Agonist | histamine | small-molecule | No | No | Xia R, Wang N, Xu Z, Lu Y, Song J, Zhang A, Guo C, He Y | 10.1038/S41467-021-22427-2 | 2021-03-31 | Yes | |
GRM4 | mGlu4 | Metabotropic glutamate | C | Human | Cryo-EM | 7E9H | - | 4.0 | R | Intermediate | - | 84 | Gi/o | αi3 | - | 63 | - | scFv16 |
L-serine-O-phosphate
|
small-molecule | Agonist | L-serine-O-phosphate, 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 | |
GHSR | ghrelin | Ghrelin | A | Human | Cryo-EM | 7F9Z | 7F9Z_refined | 3.2 | R | Active | 100 | 77 | Gq/11 | αq | Engineered G alpha | 59 | - | Nanobody-35 scFv16 |
GHRP-6
|
peptide | Agonist | [des-Gln14]ghrelin, ghrelin | peptide | No | No | Wang Y, Guo S, Zhuang Y, Yun Y, Xu P, He X, Guo J, Yin W, Xu HE, Xie X, Jiang Y | 10.1038/S41467-021-25364-2 | 2021-08-18 | Yes | |
LSHR | LH | Glycoprotein hormone | A | Human | Cryo-EM | 7FII | - | 4.3 | R | Active | 100 | 82 | Gs | αs | - | 91 | - | - |
Glycoprotein alpha
Choriogonadotropin beta |
protein protein |
Agonist | hCG, LH | peptide | No | No | Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE | 10.1038/S41586-021-03924-2 | 2021-09-29 | Yes | |
FPR2 | FPR2/ALX | Formylpeptide | A | Human | Cryo-EM | 7T6U | - | 2.9 | R | Active | 100 | 85 | Gi/o | αi1 | - | 62 | - | - |
synthetic peptide
|
peptide | 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 | 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 | 7TYY | - | 3.0 | R | Active | 100 | 78 | Gs | αs | - | 58 | - | Nanobody-35 |
calcitonin (salmon synthetic)
|
small-molecule | 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 | |
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 | 13 | 61 | - | - | - | - | GlgA glycogen synthase | - |
CP55940
6-methyl-3-[(1S)-2-nitro-1-thiophen-2-yl-ethyl]-2-phenyl-1H-indole |
small-molecule small-molecule |
Agonist PAM |
2-arachidonoylglycerol, anandamide | small-molecule | No | No | Yang X, Wang X, Xu Z, Wu C, Zhou Y, Wang Y, Lin G, Li K, Wu M, Xia A, Liu J, Cheng L, Zou J, Yan W, Shao Z, Yang S | 10.1038/S41589-022-01038-Y | 2022-06-15 | Yes | |
ACKR3 | ACKR3 | Chemokine | A | Human | Cryo-EM | 7SK3 | 7SK3_refined | 3.8 | A | Active | 97 | 84 | - | - | - | - | - | CID25 Fab light chain CID25 Fab heavy chain CID24 Fab light chain CID24 Fab heavy chain |
CXCL12α
|
peptide | Agonist | CXCL11, CXCL12α | peptide | No | No | Yen YC, Schafer CT, Gustavsson M, Eberle SA, Dominik PK, Deneka D, Zhang P, Schall TJ, Kossiakoff AA, Tesmer JJG, Handel TM | 10.1126/SCIADV.ABN8063 | 2022-07-27 | Yes | |
ACM4 | M4 | Acetylcholine (muscarinic) | A | Human | Cryo-EM | 8E9X | - | 2.7 | A | Active | 100 | 57 | Gi/o | αo | Mini-Go | 61 | - | scFv16 |
CHEMBL73538
|
small-molecule | Agonist | acetylcholine | small-molecule | No | No | 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 | |
C5AR1 | C5a1 | Complement peptide | A | Human | Cryo-EM | 7Y65 | - | 3.2 | D | Active | 100 | 81 | Gi/o | αi1 | - | 64 | - | scFv16 |
C5a
|
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 | |
EDNRB | ETB | Endothelin | A | Human | Cryo-EM | 8HCX | 8HCX_refined | 3.5 | C | Active | 100 | 66 | Gq/11 | αq | - | 61 | - | scFv16 |
ENDOTHELIN
|
protein | Agonist | endothelin-1, endothelin-2, endothelin-3 | peptide | No | No | - | - | 2023-03-22 | Yes | |
FFAR1 | FFA1 | Free fatty acid | A | Human | Cryo-EM | 8EIT | - | 2.8 | R | Active | 100 | 89 | Gq/11 | αq | - | 59 | - | scFv16 |
docosahexaenoic acid
|
small-molecule | Agonist | myristic acid, oleic acid, α-linolenic 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 | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 7XK9 | - | 3.4 | A | Active | 99 | 69 | - | - | - | - | T4-Lysozyme | Camelid Antibody Fragment |
CHEMBL6913
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline | small-molecule | No | No | - | - | 2023-04-26 | Yes | |
ACM4 | M4 | Acetylcholine (muscarinic) | A | Human | Cryo-EM | 7TRK | - | 2.8 | R | Active | 100 | 57 | Gi/o | αi1 | - | 64 | - | scFv16 |
iperoxo
|
small-molecule | Agonist | acetylcholine | small-molecule | No | No | - | - | 2023-05-17 | Yes | |
PTH1R | PTH1 | Parathyroid hormone | B1 | Human | Cryo-EM | 7Y36 | - | 2.8 | R | Active | 100 | 63 | Gs | αs | - | 57 | - | Nanobody-35 |
teriparatide
|
peptide | Agonist | TIP39, PTHrP-(1-36), PTHrP, PTH | peptide | No | No | - | - | 2023-07-05 | Yes | |
GRM2 | mGlu2 | Metabotropic glutamate | C | Human | Cryo-EM | 8JCW | - | 3.0 | 2 | Inactive | - | 87 | - | - | - | - | - | - |
LY341495
|
small-molecule | Antagonist | L-glutamic acid | small-molecule | No | No | Wang X, Wang M, Xu T, Feng Y, Shao Q, Han S, Chu X, Xu Y, Lin S, Zhao Q, Wu B | 10.1038/S41422-023-00830-2 | 2023-06-21 | Yes | |
GPR84 | GPR84 | A orphans | A | Human | Cryo-EM | 8G05 | - | 3.0 | R | Active | 100 | 72 | Gi/o | αi1 | - | 63 | - | scFv16 |
6-Octylimino-1,3-diazinane-2,4-dione
|
lipid | Agonist | - | - | No | No | Zhang X, Wang Y, Supekar S, Cao X, Zhou J, Dang J, Chen S, Jenkins L, Marsango S, Li X, Liu G, Milligan G, Feng M, Fan H, Gong W, Zhang C | 10.1038/S41467-023-41201-0 | 2023-11-01 | Yes | |
GP132 | GPR132 | A orphans | A | Human | Cryo-EM | 8HQE | 8HQE_refined | 3.0 | R | Active | 100 | 81 | Gi/o | αi1 | - | 60 | BRIL | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | 9-hydroxyoctadecadienoic acid | small-molecule | No | No | Wang JL, Dou XD, Cheng J, Gao MX, Xu GF, Ding W, Ding JH, Li Y, Wang SH, Ji ZW, Zhao XY, Huo TY, Zhang CF, Liu YM, Sha XY, Gao JR, Zhang WH, Hao Y, Zhang C, Sun JP, Jiao N, Yu X | 10.1038/S42255-023-00899-4 | 2023-10-11 | Yes | |
MC3R | MC3 | Melanocortin | A | Human | Cryo-EM | 8IOC | - | 2.9 | R | Active | 100 | 84 | Gs | αs | Gi1-Gs chimera | 60 | - | Nanobody-35 |
γ-MSH
|
peptide | Agonist | β-MSH, α-MSH, agouti-related protein, γ-MSH, ACTH | peptide | No | No | Chen VB, Arendall WB 3rd, Headd JJ, Keedy DA, Immormino RM, Kapral GJ, Murray LW, Richardson JS, Richardson DC | 10.1107/S0907444909042073 | 2023-09-20 | Yes | |
TAAR1 | TA1 | Trace amine | A | Human | Cryo-EM | 8JLR | - | 3.0 | R | Active | 100 | 79 | Gs | αs | - | 59 | BRIL | scFv16 |
(1~{S},3~{R})-3-(1-adamantyl)-1-(aminomethyl)-3,4-dihydro-1~{H}-isochromene-5,6-diol
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, 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 | 8U1U | - | 3.1 | A | Active | 100 | 83 | Gi/o | αi1 | - | 60 | - | scFv16 |
CCL1
|
protein | Agonist | CCL1 | peptide | No | No | - | - | 2023-12-20 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 4LDO | 4LDO_refined | 3.2 | A | Active | 99 | 69 | - | - | - | - | T4-Lysozyme | Nanobody |
(-)-adrenaline
|
small-molecule | Agonist | L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline | small-molecule | No | No | Ring AM, Manglik A, Kruse AC, Enos MD, Weis WI, Garcia KC, Kobilka BK | 10.1038/NATURE12572 | 2013-09-25 | Yes | |
P2RY1 | P2Y1 | P2Y | A | Human | X-ray | 4XNW | - | 2.7 | A | Active | 59 | 78 | - | - | - | - | Rubredoxin | - |
MRS2500
|
small-molecule | Antagonist | ADP, ATP | small-molecule | No | No | - | - | 2015-04-01 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5IU8 | 5IU8_refined | 2.0 | A | Inactive | 0 | 71 | - | - | - | - | BRIL | - |
CHEMBL3934661
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | Segala E, Guo D, Cheng RK, Bortolato A, Deflorian F, Doré AS, Errey JC, Heitman LH, IJzerman AP, Marshall FH, Cooke RM. | 10.1021/acs.jmedchem.6b00653 | 2016-06-29 | Yes | |
PAR2 | PAR2 | Proteinase-activated | A | Human | X-ray | 5NDD | - | 2.8 | A | Active | 59 | 74 | - | - | - | - | BRIL | - |
AZ8838
|
small-molecule | Antagonist | - | - | No | Yes | Cheng RKY, Fiez-Vandal C, Schlenker O, Edman K, Aggeler B, Brown DG, Brown GA, Cooke RM, Dumelin CE, Dore AS, Geschwindner S, Grebner C, Hermansson NO, Jazayeri A, Johansson P, Leong L, Prihandoko R, Rappas M, Soutter H, Snijder A, Sundstrom L, Tehan B, Thornton P, Troast D, Wiggin G, Zhukov A, Marshall FH, Dekker N | 10.1038/NATURE22309 | 2017-05-03 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5NLX | - | 2.1 | A | Inactive | 0 | 73 | - | - | - | - | BRIL | - |
ZM-241385
|
small-molecule | Antagonist | adenosine | small-molecule | No | No | - | - | 2017-09-27 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 6FK9 | 6FK9_refined | 2.6 | A | Active | 97 | 94 | - | - | - | - | - | - |
(2~{S})-3-methyl-2-phenyl-1-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-yl-butan-1-one
|
small-molecule | Agonist | - | - | No | No | Mattle D, Kuhn B, Aebi J, Bedoucha M, Kekilli D, Grozinger N, Alker A, Rudolph MG, Schmid G, Schertler GFX, Hennig M, Standfuss J, Dawson RJP | 10.1073/PNAS.1718084115 | 2018-04-04 | Yes | |
PD2R2 | DP2 | Prostanoid | A | Human | X-ray | 6D26 | 6D26_refined | 2.8 | A | Inactive | 27 | 82 | - | - | - | - | T4-Lysozyme | - |
fevipiprant
|
small-molecule | Antagonist | thromboxane A2, PGF2α, PGI2, PGJ2, PGD3, PGD2, PGE2 | small-molecule | No | No | Wang L, Yao D, Deepak RNVK, Liu H, Xiao Q, Fan H, Gong W, Wei Z, Zhang C | 10.1016/J.MOLCEL.2018.08.009 | 2018-10-03 | Yes | |
CCR5 | CCR5 | Chemokine | A | Human | Cryo-EM | 6MEO | 6MEO_refined | 3.9 | B | Inactive | 19 | 89 | - | - | - | - | - | T-cell surface glycoprotein CD4 |
Envelope glycoprotein gp160
|
protein | Antagonist | CCL14, CCL8, CCL13, CCL4, CCL7, CCL2, CCL5, CCL11, CCL3, CCL16 | peptide | No | No | Shaik MM, Peng H, Lu J, Rits-Volloch S, Xu C, Liao M, Chen B | 10.1038/S41586-018-0804-9 | 2018-12-12 | Yes | |
OPRM | μ | Opioid | A | Mouse | Cryo-EM | 8QOT | - | 3.2 | A | Inactive | 6 | 72 | - | - | - | - | - | Nanobody-E NabFab HC NabFab LC anti-Fab Nanobody |
Nanobody-E
|
protein | Antagonist | - | - | No | No | Yu J, Kumar A, Zhang X, Martin C, Raia P, Koehl A, Laeremans T, Steyaert J, Manglik A, Ballet S, Boland A, Stoeber M | 10.1101/2023.12.06.570395 | 2023-12-27 | Yes | |
OPSD | Rhodopsin | Opsins | A | Bovine | X-ray | 4J4Q | 4J4Q_refined | 2.7 | A | Active | 100 | 94 | Gi/o | αt1 | Only H5 | 3 | - | - |
B-Octylglucoside
|
small-molecule | unknown | - | - | No | No | Park JH, Morizumi T, Li Y, Hong JE, Pai EF, Hofmann KP, Choe HW, Ernst OP | 10.1002/ANIE.201302374 | 2013-10-30 | Yes | |
ACM3 | M3 | Acetylcholine (muscarinic) | A | Rat | X-ray | 4U16 | 4U16_refined | 3.7 | B | Inactive | 2 | 47 | - | - | - | - | T4-Lysozyme | - |
N-methyl scopolamine
|
small-molecule | Antagonist | acetylcholine | small-molecule | No | No | Thorsen TS, Matt R, Weis WI, Kobilka BK | 10.1016/J.STR.2014.08.022 | 2014-11-26 | Yes | |
OX1R | OX1 | Orexin | A | Human | X-ray | 4ZJC | 4ZJC_refined | 2.8 | A | Inactive | 0 | 72 | - | - | - | - | GlgA glycogen synthase | - |
SB-674042
|
small-molecule | Antagonist | orexin-A, orexin-B | peptide | No | No | Yin J, Babaoglu K, Brautigam CA, Clark L, Shao Z, Scheuermann TH, Harrell CM, Gotter AL, Roecker AJ, Winrow CJ, Renger JJ, Coleman PJ, Rosenbaum DM | 10.1038/NSMB.3183 | 2016-03-09 | Yes | |
CCR9 | CCR9 | Chemokine | A | Human | X-ray | 5LWE | - | 2.8 | B | Inactive | 49 | 67 | - | - | - | - | - | - |
vercirnon
|
small-molecule | Allosteric antagonist | CCL25 | peptide | No | No | Oswald C, Rappas M, Kean J, Dore AS, Errey JC, Bennett K, Deflorian F, Christopher JA, Jazayeri A, Mason JS, Congreve M, Cooke RM, Marshall FH | 10.1038/NATURE20606 | 2016-12-07 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5JTB | 5JTB_refined | 2.8 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
ZM-241385
|
small-molecule | Antagonist | adenosine | small-molecule | No | No | Melnikov I, Polovinkin V, Kovalev K, Gushchin I, Shevtsov M, Shevchenko V, Mishin A, Alekseev A, Rodriguez-Valera F, Borshchevskiy V, Cherezov V, Leonard GA, Gordeliy V, Popov A | 10.1126/SCIADV.1602952 | 2017-05-31 | Yes | |
OX2R | OX2 | Orexin | A | Human | X-ray | 5WQC | 5WQC_refined | 2.0 | A | Inactive | 0 | 68 | - | - | - | - | Glycogen synthase | - |
EMPA
|
small-molecule | Antagonist | orexin-A, orexin-B | peptide | No | No | Suno R, Kimura KT, Nakane T, Yamashita K, Wang J, Fujiwara T, Yamanaka Y, Im D, Horita S, Tsujimoto H, Tawaramoto MS, Hirokawa T, Nango E, Tono K, Kameshima T, Hatsui T, Joti Y, Yabashi M, Shimamoto K, Yamamoto M, Rosenbaum DM, Iwata S, Shimamura T, Kobayashi T | 10.1016/J.STR.2017.11.005 | 2017-11-29 | Yes | |
GRM5 | mGlu5 | Metabotropic glutamate | C | Human | X-ray | 6FFH | 6FFH_refined | 2.7 | A | Inactive | - | 21 | - | - | - | - | T4-Lysozyme | - |
fenobam
|
small-molecule | NAM | L-glutamic acid | small-molecule | No | No | Christopher JA, Orgovan Z, Congreve M, Dore AS, Errey JC, Marshall FH, Mason JS, Okrasa K, Rucktooa P, Serrano-Vega MJ, Ferenczy GG, Keseru GM | 10.1021/ACS.JMEDCHEM.7B01722 | 2018-03-07 | Yes | |
PTAFR | PAF | Platelet-activating factor | A | Human | X-ray | 5ZKQ | - | 2.9 | B | Active | 59 | 83 | - | - | - | - | T4-Lysozyme | - |
ABT-491
|
small-molecule | Inverse agonist | PAF | small-molecule | No | No | Cao C, Tan Q, Xu C, He L, Yang L, Zhou Y, Zhou Y, Qiao A, Lu M, Yi C, Han GW, Wang X, Li X, Yang H, Rao Z, Jiang H, Zhao Y, Liu J, Stevens RC, Zhao Q, Zhang XC, Wu B | 10.1038/S41594-018-0068-Y | 2018-06-20 | Yes | |
PE2R3 | EP3 | Prostanoid | A | Human | X-ray | 6AK3 | 6AK3_refined | 2.9 | B | Active | 89 | 69 | - | - | - | - | BRIL | - |
PGE2
|
small-molecule | Agonist | thromboxane A2, PGF2α, PGI2, PGD2, PGE1, PGE2 | small-molecule | No | No | Morimoto K, Suno R, Hotta Y, Yamashita K, Hirata K, Yamamoto M, Narumiya S, Iwata S, Kobayashi T | 10.1038/S41589-018-0171-8 | 2018-12-05 | 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 | 6KK7 | 6KK7_refined | 3.1 | B | Inactive | 0 | 56 | - | - | - | - | T4-Lysozyme | - |
PF-06372222
|
small-molecule | NAM | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | 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 | 6TO7 | - | 2.3 | A | Inactive | 0 | 71 | - | - | - | - | - | - |
suvorexant
|
small-molecule | Antagonist | orexin-A, orexin-B | peptide | No | No | Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA. | 10.1021/acs.jmedchem.9b01787 | 2020-01-01 | Yes | |
AGTR1 | AT1 | Angiotensin | A | Human | X-ray | 6OS0 | 6OS0_refined | 2.9 | A | Active | 93 | 85 | - | - | - | - | BRIL | Nanobody-Nb.AT110i1 |
angiotensin II
|
peptide | Agonist | angiotensin IV, angiotensin II, angiotensin III, angiotensin A | peptide | No | No | Wingler LM, Skiba MA, McMahon C, Staus DP, Kleinhenz ALW, Suomivuori CM, Latorraca NR, Dror RO, Lefkowitz RJ, Kruse AC | 10.1126/SCIENCE.AAY9813 | 2020-02-19 | Yes | |
ADA2B | α2B | Adrenoceptors | A | Human | Cryo-EM | 6K42 | - | 4.1 | R | Active | 100 | 60 | Gi/o | αi1 | - | 62 | T4-Lysozyme | scFv |
dexmedetomidine
|
small-molecule | Agonist | (-)-adrenaline, (-)-noradrenaline | small-molecule | No | No | Yuan D, Liu Z, Kaindl J, Maeda S, Zhao J, Sun X, Xu J, Gmeiner P, Wang HW, Kobilka BK | 10.1038/S41589-020-0492-2 | 2020-04-15 | Yes | |
AGTR2 | AT2 | Angiotensin | A | Human | X-ray | 7C6A | 7C6A_refined | 3.4 | A | Active | 99 | 77 | - | - | - | - | BRIL | IgG heavy chain IgG light chain |
CHEMBL404594
|
protein | Agonist | angiotensin-(1-7), angiotensin II, angiotensin III | peptide | No | No | Miyagi H, Asada H, Suzuki M, Takahashi Y, Yasunaga M, Suno C, Iwata S, Saito JI | 10.1038/S41598-020-68355-X | 2020-07-29 | Yes | |
5HT2A | 5-HT2A | 5-Hydroxytryptamine | A | Human | X-ray | 6WH4 | 6WH4_refined | 3.4 | C | Inactive | 1 | 59 | - | - | - | - | BRIL | - |
CHEMBL428892
|
small-molecule | Inverse 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 | 7BU6 | 7BU6_refined | 2.7 | A | Active | 99 | 58 | - | - | - | - | T4-Lysozyme | Camelid antibody fragment Nb6B9 |
Noradrenaline
|
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 | |
NTR1 | NTS1 | Neurotensin | A | Rat | X-ray | 6YVR | - | 2.5 | B | Inactive | 3 | 83 | - | - | - | - | DARPin D12 | - |
JMV431
|
peptide | 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 | |
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 | |
5HT1F | 5-HT1F | 5-Hydroxytryptamine | A | Human | Cryo-EM | 7EXD | 7EXD_refined | 3.4 | R | Active | 100 | 74 | Gi/o | αi1 | - | 62 | BRIL | scFv16 |
lasmiditan
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | No | No | Huang S, Xu P, Tan Y, You C, Zhang Y, Jiang Y, Xu HE | 10.1038/S41422-021-00527-4 | 2021-08-04 | Yes | |
LSHR | LH | Glycoprotein hormone | A | Human | Cryo-EM | 7FIG | - | 3.9 | R | Active | 100 | 79 | Gs | αs | - | 91 | - | Nanobody-35 |
Glycoprotein alpha
Choriogonadotropin beta |
protein protein |
Agonist | hCG, LH | peptide | No | No | Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE | 10.1038/S41586-021-03924-2 | 2021-09-29 | Yes | |
AGRD1 | ADGRD1 | ADGRD | B2 | Human | Cryo-EM | 7EPT | - | 3.0 | R | Active | 100 | 31 | Gs | αs | - | 54 | - | Nanobody-35 | - | - | - | - | - | No | No | Ping YQ, Xiao P, Yang F, Zhao RJ, Guo SC, Yan X, Wu X, Zhang C, Lu Y, Zhao F, Zhou F, Xi YT, Yin W, Liu FZ, He DF, Zhang DL, Zhu ZL, Jiang Y, Du L, Feng SQ, Schoneberg T, Liebscher I, Xu HE, Sun JP | 10.1038/S41586-022-04619-Y | 2022-05-11 | Yes | |
SSR2 | SST2 | Somatostatin | A | Human | Cryo-EM | 7WIG | 7WIG_refined | 2.7 | R | Active | 100 | 77 | Gi/o | αi1 | - | 64 | - | scFv16 |
~{N}-[(2~{R})-1-[[(1~{R},3~{S})-3-(aminomethyl)cyclohexyl]methylamino]-3-(1~{H}-indol-3-yl)-1-oxidanylidene-propan-2-yl]spiro[indene-1,4'-piperidine]-1'-carboxamide
|
small-molecule | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | No | No | Chen LN, Wang WW, Dong YJ, Shen DD, Guo J, Yu X, Qin J, Ji SY, Zhang H, Shen Q, He Q, Yang B, Zhang Y, Li Q, Mao C | 10.1038/S41422-022-00669-Z | 2022-06-01 | Yes | |
5HT4R | 5-HT4 | 5-Hydroxytryptamine | A | Human | Cryo-EM | 7XT8 | - | 3.1 | R | Active | 100 | 76 | Gs | αs | - | 60 | BRIL | Nanobody-35 |
5-hydroxytryptamine
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | No | No | Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE | 10.1016/J.MOLCEL.2022.05.031 | 2022-07-27 | Yes | |
5HT2C | 5-HT2C | 5-Hydroxytryptamine | A | Human | Cryo-EM | 8DPG | - | 3.6 | A | Active | 100 | 58 | Gq/11 | αq | Gi2-mini-Gq chimera | 57 | - | scFv16 |
psilocin
|
small-molecule | Agonist | 5-hydroxytryptamine | small-molecule | No | No | Gumpper RH, Fay JF, Roth BL | 10.1016/J.CELREP.2022.111211 | 2022-08-24 | Yes | |
PE2R3 | EP3 | Prostanoid | A | Human | Cryo-EM | 7WU9 | 7WU9_refined | 3.4 | R | Active | 100 | 70 | Gi/o | αi1 | - | 38 | - | scFv16 | - | - | - | thromboxane A2, PGF2α, PGI2, PGD2, PGE1, PGE2 | small-molecule | No | No | Suno R, Sugita Y, Morimoto K, Takazaki H, Tsujimoto H, Hirose M, Suno-Ikeda C, Nomura N, Hino T, Inoue A, Iwasaki K, Kato T, Iwata S, Kobayashi T | 10.1016/J.CELREP.2022.111323 | 2022-08-17 | Yes | |
TSHR | TSH | Glycoprotein hormone | A | Human | Cryo-EM | 7T9I | - | 2.9 | R | Active | 100 | 78 | Gs | αs | Mini-Gs | 56 | - | Nanobody-35 |
Thyrotropin subunit beta
Glycoprotein hormones alpha chain |
protein protein |
Agonist | TSH | peptide | No | No | Faust B, Billesbolle CB, Suomivuori CM, Singh I, Zhang K, Hoppe N, Pinto AFM, Diedrich JK, Muftuoglu Y, Szkudlinski MW, Saghatelian A, Dror RO, Cheng Y, Manglik A | 10.1038/S41586-022-05159-1 | 2022-08-03 | Yes | |
HRH4 | H4 | Histamine | A | Human | Cryo-EM | 8HOC | - | 3.0 | R | Active | 100 | 71 | Gi/o | αi1 | - | 64 | - | scFv16 |
imetit
|
small-molecule | Agonist | histamine, CCL16 | small-molecule | No | No | - | - | 2023-12-20 | 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 | |
GLR | glucagon | Glucagon | B1 | Human | Cryo-EM | 8JIU | 8JIU_refined | 2.8 | R | Active | 100 | 83 | Gs | αs | - | 59 | - | Nanobody-35 |
SAR425899
|
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 | 2023-09-13 | Yes | |
TAAR1 | TA1 | Trace amine | A | Human | Cryo-EM | 8W8A | - | 2.8 | R | Active | 100 | 85 | Gi/o | αi2 | - | 0 | - | Nanobody-35 |
CHEMBL3684869
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, dopamine | small-molecule | No | No | Liu H, Zheng Y, Wang Y, Wang Y, He X, Xu P, Huang S, Yuan Q, Zhang X, Wang L, Jiang K, Chen H, Li Z, Liu W, Wang S, Xu HE, Xu F | 10.1038/S41586-023-06775-1 | 2023-11-22 | Yes | |
ACM2 | M2 | Acetylcholine (muscarinic) | A | Human | X-ray | 4MQT | 4MQT_refined | 3.7 | A | Active | 99 | 59 | - | - | - | - | - | Nanobody |
iperoxo
LY2119620 |
small-molecule small-molecule |
Agonist PAM |
acetylcholine | small-molecule | No | No | Kruse AC, Ring AM, Manglik A, Hu J, Hu K, Eitel K, Hubner H, Pardon E, Valant C, Sexton PM, Christopoulos A, Felder CC, Gmeiner P, Steyaert J, Weis WI, Garcia KC, Wess J, Kobilka BK | 10.1038/NATURE12735 | 2013-11-27 | Yes | |
P2RY1 | P2Y1 | P2Y | A | Human | X-ray | 4XNV | - | 2.2 | A | Active | 59 | 78 | - | - | - | - | Rubredoxin | - |
BMS compound 16 [PMID:23368907]
|
small-molecule | NAM | ADP, ATP | small-molecule | No | No | Zhang D, Gao ZG, Zhang K, Kiselev E, Crane S, Wang J, Paoletta S, Yi C, Ma L, Zhang W, Han GW, Liu H, Cherezov V, Katritch V, Jiang H, Stevens RC, Jacobson KA, Zhao Q, Wu B | 10.1038/NATURE14287 | 2015-04-01 | Yes | |
OPSD | Rhodopsin | Opsins | A | Human | X-ray | 5DGY | 5DGY_refined | 7.7 | A | Active | 100 | 94 | Visual | S-arrestin | - | 86 | T4-Lysozyme | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Zhou XE, Gao X, Barty A, Kang Y, He Y, Liu W, Ishchenko A, White TA, Yefanov O, Han GW, Xu Q, de Waal PW, Suino-Powell KM, Boutet S, Williams GJ, Wang M, Li D, Caffrey M, Chapman HN, Spence JC, Fromme P, Weierstall U, Stevens RC, Cherezov V, Melcher K, Xu HE | 10.1038/SDATA.2016.21 | 2016-03-23 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5VRA | 5VRA_refined | 2.4 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
ZM-241385
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | Broecker J, Morizumi T, Ou WL, Klingel V, Kuo A, Kissick DJ, Ishchenko A, Lee MY, Xu S, Makarov O, Cherezov V, Ogata CM, Ernst OP | 10.1038/NPROT.2017.135 | 2017-12-13 | Yes | |
C5AR1 | C5a1 | Complement peptide | A | Human | X-ray | 6C1Q | 6C1Q_refined | 2.9 | B | Inactive | 8 | 82 | - | - | - | - | BRIL | - |
PMX53
NDT9513727 |
peptide small-molecule |
Antagonist NAM |
ribosomal protein S19, C5a, C5a des-Arg, C3a | peptide | No | No | Liu H, Kim HR, Deepak RNVK, Wang L, Chung KY, Fan H, Wei Z, Zhang C | 10.1038/S41594-018-0067-Z | 2018-05-30 | Yes | |
ACM2 | M2 | Acetylcholine (muscarinic) | A | Human | X-ray | 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 | |
5HT2A | 5-HT2A | 5-Hydroxytryptamine | A | Human | X-ray | 6A94 | 6A94_refined | 2.9 | A | Inactive | 1 | 60 | - | - | - | - | BRIL | - |
zotepine
|
small-molecule | Antagonist | tryptamine, 5-hydroxytryptamine | small-molecule | No | No | Kimura KT, Asada H, Inoue A, Kadji FMN, Im D, Mori C, Arakawa T, Hirata K, Nomura Y, Nomura N, Aoki J, Iwata S, Shimamura T | 10.1038/S41594-018-0180-Z | 2019-02-13 | Yes | |
SUCR1 | succinate | Succinate | A | Rat | X-ray | 6IBB | - | 2.1 | A | Active | 59 | 93 | - | - | - | - | - | Nanobody-6 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Haffke M, Fehlmann D, Rummel G, Boivineau J, Duckely M, Gommermann N, Cotesta S, Sirockin F, Freuler F, Littlewood-Evans A, Kaupmann K, Jaakola VP | 10.1038/S41586-019-1663-8 | 2019-08-14 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 6PS5 | 6PS5_refined | 2.9 | A | Inactive | 0 | 68 | - | - | - | - | T4-Lysozyme | - |
propranolol
|
small-molecule | Antagonist | L-NOREPINEPHRINE, noradrenaline, (-)-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 | |
OX1R | OX1 | Orexin | A | Human | X-ray | 6TOT | 6TOT_refined | 2.2 | B | Inactive | 0 | 71 | - | - | - | - | - | - |
lemborexant
|
small-molecule | Antagonist | orexin-A, orexin-B | peptide | No | No | Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA. | 10.1021/acs.jmedchem.9b01787 | 2020-01-15 | Yes | |
GLP1R | GLP-1 | Glucagon | B1 | Human | X-ray | 6LN2 | 6LN2_refined | 3.2 | A | Inactive | 0 | 83 | - | - | - | - | - | Fab7F38 light chain Fab7F38 heavy chain |
PF-06372222
|
small-molecule | NAM | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | No | No | Wu F, Yang L, Hang K, Laursen M, Wu L, Han GW, Ren Q, Roed NK, Lin G, Hanson MA, Jiang H, Wang MW, Reedtz-Runge S, Song G, Stevens RC | 10.1038/S41467-020-14934-5 | 2020-03-18 | Yes | |
CCR6 | CCR6 | Chemokine | A | Human | Cryo-EM | 6WWZ | 6WWZ_refined | 3.3 | R | Active | 100 | 83 | Gi/o | αo | - | 59 | - | scFv16 |
CCL20
|
peptide | Agonist | beta-defensin 4A, CCL20 | peptide | No | No | Wasilko DJ, Johnson ZL, Ammirati M, Che Y, Griffor MC, Han S, Wu H | 10.1038/S41467-020-16820-6 | 2020-06-24 | Yes | |
NTR1 | NTS1 | Neurotensin | A | Rat | Cryo-EM | 7L0Q | - | 4.3 | C | Active | 100 | 73 | Gi/o | αi1 | - | 95 | - | - |
neurotensin
|
peptide | Agonist | neurotensin, neuromedin N | peptide | No | No | Zhang M, Gui M, Wang ZF, Gorgulla C, Yu JJ, Wu H, Sun ZJ, Klenk C, Merklinger L, Morstein L, Hagn F, Pluckthun A, Brown A, Nasr ML, Wagner G | 10.1038/S41594-020-00554-6 | 2021-01-06 | Yes | |
DRD1 | D1 | Dopamine | A | Human | Cryo-EM | 7CKW | 7CKW_refined | 3.2 | R | Active | 100 | 61 | Gs | αs | - | 60 | - | Nanobody-35 |
fenoldopam
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, 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 | |
S1PR3 | S1P3 | Lysophospholipid (S1P) | A | Human | X-ray | 7C4S | 7C4S_refined | 3.2 | A | Active | 63 | 75 | - | - | - | - | - | Fab light chain Fab heavy chain |
sphingosine 1-phosphate
|
small-molecule | Agonist | sphingosylphosphorylcholine, dihydrosphingosine 1-phosphate, sphingosine 1-phosphate | small-molecule | No | No | Maeda S, Shiimura Y, Asada H, Hirata K, Luo F, Nango E, Tanaka N, Toyomoto M, Inoue A, Aoki J, Iwata S, Hagiwara M | 10.1126/SCIADV.ABF5325 | 2021-06-09 | Yes | |
CCR5 | CCR5 | Chemokine | A | Human | Cryo-EM | 7F1Q | - | 2.9 | R | Active | 100 | 85 | Gi/o | αi1 | - | 61 | - | - |
CCL3
|
peptide | Agonist | CCL14, CCL8, CCL13, CCL4, CCL7, CCL2, CCL5, CCL11, CCL3, CCL16 | peptide | No | No | - | - | 2021-07-14 | Yes | |
NK1R | NK1 | Tachykinin | A | Human | Cryo-EM | 7RMH | 7RMH_refined | 3.1 | R | Active | 100 | 70 | Gs | αs | - | 55 | - | Nanobody-35 |
substance P
|
peptide | Agonist | neuropeptide-γ, neurokinin A, neuropeptide K, neurokinin B, hemokinin 1, 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 | desulfated cholecystokinin-8, CCK-58, CCK-33, CCK-4, gastrin-17, CCK-39, CCK-8 | peptide | No | No | Zhang X, He C, Wang M, Zhou Q, Yang D, Zhu Y, Feng W, Zhang H, Dai A, Chu X, Wang J, Yang Z, Jiang Y, Sensfuss U, Tan Q, Han S, Reedtz-Runge S, Xu HE, Zhao S, Wang MW, Wu B, Zhao Q | 10.1038/S41589-021-00866-8 | 2021-12-29 | 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 | 7EJA | - | 3.6 | R | Active | 100 | 58 | Gi/o | αo | - | 59 | - | scFv16 |
dexmedetomidine
|
small-molecule | Agonist | (-)-adrenaline, (-)-noradrenaline | small-molecule | No | No | Xu J, Cao S, Hubner H, Weikert D, Chen G, Lu Q, Yuan D, Gmeiner P, Liu Z, Du Y | 10.1126/SCIADV.ABJ5347 | 2022-04-13 | Yes | |
FPR2 | FPR2/ALX | Formylpeptide | A | Human | Cryo-EM | 7WVY | 7WVY_refined | 3.0 | R | Active | 100 | 85 | Gi/o | αi2 | - | 63 | BRIL | - |
Amyloid beta-Peptide (1-42)
|
peptide | Agonist | 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 | Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B | 10.1038/S41467-022-29361-X | 2022-04-13 | Yes | |
ACM4 | M4 | Acetylcholine (muscarinic) | A | Human | Cryo-EM | 7V69 | - | 3.4 | R | Active | 100 | 58 | Gi/o | αi1 | - | 62 | - | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | acetylcholine | small-molecule | No | No | Wang J, Wu M, Chen Z, Wu L, Wang T, Cao D, Wang H, Liu S, Xu Y, Li F, Liu J, Chen N, Zhao S, Cheng J, Wang S, Hua T | 10.1038/S41467-022-30595-Y | 2022-05-11 | Yes | |
DRD1 | D1 | Dopamine | A | Human | Cryo-EM | 7X2C | 7X2C_refined | 3.2 | F | Active | 100 | 63 | Gs | αs | - | 58 | - | Nanobody-35 |
fenoldopam
|
small-molecule | Agonist | L-NOREPINEPHRINE, 5-hydroxytryptamine, noradrenaline, (-)-noradrenaline, dopamine | small-molecule | No | No | Teng X, Chen S, Nie Y, Xiao P, Yu X, Shao Z, Zheng S | 10.1038/S41467-022-30929-W | 2022-06-29 | Yes | |
APJ | apelin | Apelin | A | Human | X-ray | 7SUS | 7SUS_refined | 2.7 | A | Inactive | 6 | 76 | - | - | - | - | Rubredoxin | - |
(1R,2S)-N-[4-(2,6-dimethoxyphenyl)-5-(6-methylpyridin-2-yl)-1,2,4-triazol-3-yl]-1-(5-methylpyrimidin-2-yl)-1-oxidanyl-propane-2-sulfonamide
|
small-molecule | Agonist | Elabela/Toddler-21, apelin-17, [Pyr1]apelin-13, Elabela/Toddler-11, Elabela/Toddler-32, apelin-13, apelin-36, 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 | |
ACKR3 | ACKR3 | Chemokine | A | Human | Cryo-EM | 7SK8 | 7SK8_refined | 3.3 | A | Active | 97 | 85 | - | - | - | - | - | CID25 Fab light chain CID25 Fab heavy chain CID24 Fab light chain CID24 Fab heavy chain |
Stromal cell-derived factor 1
(1R)-4-[7-(3-carboxypropoxy)-6-methylquinolin-8-yl]-1-{[2-(4-hydroxypiperidin-1-yl)-1,3-thiazol-4-yl]methyl}-1,4-diazepan-1-ium |
peptide small-molecule |
Agonist Agonist (partial) |
CXCL11, CXCL12α | peptide | No | No | Yen YC, Schafer CT, Gustavsson M, Eberle SA, Dominik PK, Deneka D, Zhang P, Schall TJ, Kossiakoff AA, Tesmer JJG, Handel TM | 10.1126/SCIADV.ABN8063 | 2022-07-27 | Yes | |
PACR | PAC1 | VIP and PACAP | B1 | Human | Cryo-EM | 8E3X | 8E3X_refined | 2.3 | R | Active | 100 | 77 | Gs | αs | - | 59 | - | Nanobody-35 |
[Ac-His1]PACAP-27
|
peptide | Agonist | VIP, PHI, PHM, PHV, PACAP-27, PACAP-38 | peptide | No | No | Piper SJ, Deganutti G, Lu J, Zhao P, Liang YL, Lu Y, Fletcher MM, Hossain MA, Christopoulos A, Reynolds CA, Danev R, Sexton PM, Wootten D | 10.1038/S41467-022-34629-3 | 2022-11-23 | Yes | |
C5AR1 | C5a1 | Complement peptide | A | Human | Cryo-EM | 7Y66 | - | 2.9 | D | Active | 100 | 80 | Gi/o | αi1 | - | 63 | - | scFv16 |
BM213
|
peptide | Agonist | 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 | |
GPR20 | GPR20 | A orphans | A | Human | Cryo-EM | 8HS3 | - | 3.1 | R | Active | 100 | 78 | Gi/o | αi1 | - | 62 | BRIL | scFv16 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | 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 | |
GLR | glucagon | Glucagon | B1 | Human | Cryo-EM | 8FU6 | 8FU6_refined | 2.9 | R | Active | 100 | 72 | Gs | αs | - | 54 | - | Nanobody-35 |
Glucagon derivative ZP3780
|
peptide | Agonist | glucagon | peptide | No | No | Krishna Kumar K, O'Brien ES, Habrian CH, Latorraca NR, Wang H, Tuneew I, Montabana E, Marqusee S, Hilger D, Isacoff EY, Mathiesen JM, Kobilka BK | 10.1016/J.CELL.2023.02.028 | 2023-04-12 | Yes | |
PTH1R | PTH1 | Parathyroid hormone | B1 | Human | Cryo-EM | 8FLQ | - | 2.6 | R | Active | 100 | 61 | Gs | αs | - | 59 | - | Nanobody-35 |
Parathyroid hormone
|
peptide | 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 | |
FFAR4 | FFA4 | Free fatty acid | A | Human | Cryo-EM | 8H4K | - | 3.1 | R | Active | 100 | 83 | Gq/11 | αq | Mini-Gq | 60 | - | Nanobody-35 |
GW9508
|
small-molecule | Agonist | 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 | |
GRM2 | mGlu2 | Metabotropic glutamate | C | Human | Cryo-EM | 8JCX | - | 3.0 | 2 | Inactive | - | 87 | - | - | - | - | - | - |
LY341495
|
small-molecule | Antagonist | L-glutamic acid | small-molecule | No | No | Wang X, Wang M, Xu T, Feng Y, Shao Q, Han S, Chu X, Xu Y, Lin S, Zhao Q, Wu B | 10.1038/S41422-023-00830-2 | 2023-06-21 | Yes | |
PE2R4 | EP4 | Prostanoid | A | Human | Cryo-EM | 8GCM | - | 3.5 | R | Active | 100 | 52 | Gi/o | αi1 | - | 56 | - | scFv16 |
(5S)-5-[(3R)-4,4-difluoro-3-hydroxy-4-phenylbutyl]-1-[6-(1H-tetrazol-5-yl)hexyl]pyrrolidin-2-one
|
lipid | 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 | 2024-01-03 | Yes | |
C5AR1 | C5a1 | Complement peptide | A | Mouse | Cryo-EM | 8HQC | - | 3.9 | A | Active | 100 | 78 | Gi/o | αo | - | 60 | - | - |
C5a
|
peptide | Agonist | - | - | No | No | - | HTTPS://DOI.ORG/10.1016/J.CELL.2023.09.020 | 2023-10-18 | Yes | |
HCAR2 | HCA2 | Hydroxycarboxylic acid | A | Human | Cryo-EM | 8J6R | - | 2.8 | R | Active | 100 | 81 | Gi/o | αi1 | - | 64 | - | scFv16 |
MK 6892
|
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 | |
CXCR3 | CXCR3 | Chemokine | A | Human | Cryo-EM | 8K2W | - | 3.0 | R | Inactive | 6 | 71 | - | - | - | - | BRIL | Nanobody-6 |
CHEMBL397983
|
small-molecule | Agonist | CCL19, CXCL11, CCL13, CXCL9, CXCL10, CCL7, CCL5, CCL11, CXCL12α, CCL20 | peptide | No | No | Jiao H, Pang B, Chiang YC, Chen Q, Pan Q, Ren R, Hu H | 10.1038/S41421-023-00617-0 | 2023-11-29 | Yes | |
TAAR1 | TA1 | Trace amine | A | Human | Cryo-EM | 8W87 | - | 2.8 | R | Active | 100 | 85 | Gs | αs | - | 59 | - | Nanobody-35 |
METHAMPHETAMINE
|
small-molecule | Agonist | β-phenylethylamine, tyramine, 3-iodothyronamine, (+)-Octopamine, CHEMBL1160703, octopamine, dopamine | small-molecule | No | No | Liu H, Zheng Y, Wang Y, Wang Y, He X, Xu P, Huang S, Yuan Q, Zhang X, Wang L, Jiang K, Chen H, Li Z, Liu W, Wang S, Xu HE, Xu F | 10.1038/S41586-023-06775-1 | 2023-11-22 | Yes | |
SMO | SMO | Frizzled | F | Human | X-ray | 4QIN | 4QIN_refined | 2.6 | A | Inactive | 11 | 43 | - | - | - | - | BRIL | - |
SAG1.5
|
small-molecule | Agonist | - | - | No | No | Wang C, Wu H, Evron T, Vardy E, Han GW, Huang XP, Hufeisen SJ, Mangano TJ, Urban DJ, Katritch V, Cherezov V, Caron MG, Roth BL, Stevens RC | 10.1038/NCOMMS5355 | 2014-07-23 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 5D5B | 5D5B_refined | 3.8 | A | Inactive | 0 | 68 | - | - | - | - | T4-Lysozyme | - |
Carazolol
|
small-molecule | Inverse agonist | L-NOREPINEPHRINE, noradrenaline, (-)-adrenaline, Zn2+, (-)-noradrenaline | small-molecule | No | No | Huang CY, Olieric V, Ma P, Howe N, Vogeley L, Liu X, Warshamanage R, Weinert T, Panepucci E, Kobilka B, Diederichs K, Wang M, Caffrey M | 10.1107/S2059798315021683 | 2016-01-13 | Yes | |
NTR1 | NTS1 | Neurotensin | A | Rat | X-ray | 5T04 | 5T04_refined | 3.3 | A | Active | 82 | 69 | - | - | - | - | T4-Lysozyme | - |
neurotensin
|
peptide | Agonist | neurotensin, neuromedin N | peptide | No | No | Krumm BE, Lee S, Bhattacharya S, Botos I, White CF, Du H, Vaidehi N, Grisshammer R | 10.1038/SREP38564 | 2016-12-21 | Yes | |
CNR1 | CB1 | Cannabinoid | A | Human | X-ray | 5XRA | 5XRA_refined | 2.8 | A | Active | 96 | 60 | - | - | - | - | Flavodoxin | - |
AM11542
|
small-molecule | Agonist | 2-arachidonoylglycerol, anandamide | small-molecule | No | No | Hua T, Vemuri K, Nikas SP, Laprairie RB, Wu Y, Qu L, Pu M, Korde A, Jiang S, Ho JH, Han GW, Ding K, Li X, Liu H, Hanson MA, Zhao S, Bohn LM, Makriyannis A, Stevens RC, Liu ZJ | 10.1038/NATURE23272 | 2017-07-12 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 5OLH | 5OLH_refined | 2.6 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
vipadenant
|
small-molecule | Antagonist | adenosine | small-molecule | No | Yes | - | - | 2018-01-17 | Yes | |
FFAR1 | FFA1 | Free fatty acid | A | Human | X-ray | 5KW2 | - | 2.8 | A | Active | 59 | 82 | - | - | - | - | T4-Lysozyme | - |
(3~{S})-3-cyclopropyl-3-[2-[1-[2-[2,2-dimethylpropyl-(6-methylpyridin-2-yl)carbamoyl]-5-methoxy-phenyl]piperidin-4-yl]-1-benzofuran-6-yl]propanoic acid
|
small-molecule | Allosteric agonist | myristic acid, oleic acid, α-linolenic acid, docosahexaenoic acid | small-molecule | No | No | Ho JD, Chau B, Rodgers L, Lu F, Wilbur KL, Otto KA, Chen Y, Song M, Riley JP, Yang HC, Reynolds NA, Kahl SD, Lewis AP, Groshong C, Madsen RE, Conners K, Lineswala JP, Gheyi T, Saflor MD, Lee MR, Benach J, Baker KA, Montrose-Rafizadeh C, Genin MJ, Miller AR, Hamdouchi C | 10.1038/S41467-017-01240-W | 2018-05-02 | Yes | |
CCR5 | CCR5 | Chemokine | A | Human | X-ray | 6AKX | 6AKX_refined | 2.8 | B | Inactive | 19 | 82 | - | - | - | - | Rubredoxin | - |
CHEMBL4238063
|
small-molecule | Antagonist | CCL14, CCL8, CCL13, CCL4, CCL7, CCL2, CCL5, CCL11, CCL3, CCL16 | peptide | No | No | Peng P, Chen H, Zhu Y, Wang Z, Li J, Luo RH, Wang J, Chen L, Yang LM, Jiang H, Xie X, Wu B, Zheng YT, Liu H. | 10.1021/acs.jmedchem.8b01077 | 2018-10-24 | Yes | |
NK1R | NK1 | Tachykinin | A | Human | X-ray | 6HLL | 6HLL_refined | 3.3 | A | Inactive | 0 | 67 | - | - | - | - | GlgA glycogen synthase | - |
CP 99994
|
small-molecule | Antagonist | neuropeptide-γ, neurokinin A, neuropeptide K, neurokinin B, hemokinin 1, 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 | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 6MH8 | 6MH8_refined | 4.2 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
ZM-241385
|
small-molecule | Antagonist | adenosine | small-molecule | No | No | Martin-Garcia JM, Zhu L, Mendez D, Lee MY, Chun E, Li C, Hu H, Subramanian G, Kissick D, Ogata C, Henning R, Ishchenko A, Dobson Z, Zhang S, Weierstall U, Spence JCH, Fromme P, Zatsepin NA, Fischetti RF, Cherezov V, Liu W | 10.1107/S205225251900263X | 2019-04-24 | Yes | |
ADRB2 | β2 | Adrenoceptors | A | Human | X-ray | 6PS2 | 6PS2_refined | 2.4 | A | Inactive | 0 | 68 | - | - | - | - | T4-Lysozyme | - |
CHEMBL1160734
|
small-molecule | Antagonist | 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 | |
CLTR2 | CysLT2 | Leukotriene | A | Human | X-ray | 6RZ9 | - | 2.7 | A | Active | 59 | 81 | - | - | - | - | BRIL | - |
ONO-2770372
|
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 | |
AGTR1 | AT1 | Angiotensin | A | Human | X-ray | 6OS1 | - | 2.8 | A | Active | 93 | 85 | - | - | - | - | BRIL | Nanobody-Nb.AT110i1_le |
TRV023
|
peptide | Agonist | angiotensin IV, angiotensin II, angiotensin III, angiotensin A | peptide | No | No | Wingler LM, Skiba MA, McMahon C, Staus DP, Kleinhenz ALW, Suomivuori CM, Latorraca NR, Dror RO, Lefkowitz RJ, Kruse AC | 10.1126/SCIENCE.AAY9813 | 2020-02-19 | Yes | |
GLR | glucagon | Glucagon | B1 | Human | Cryo-EM | 6WHC | 6WHC_refined | 3.4 | R | Active | 100 | 78 | Gs | αs | - | 56 | - | Nanobody-35 |
Dual-agonist peptide P15
|
peptide | Agonist | glucagon | peptide | No | No | Chang R, Zhang X, Qiao A, Dai A, Belousoff MJ, Tan Q, Shao L, Zhong L, Lin G, Liang YL, Ma L, Han S, Yang D, Danev R, Wang MW, Wootten D, Wu B, Sexton PM | 10.1074/JBC.RA120.013793 | 2020-05-27 | Yes | |
SUCR1 | succinate | Succinate | A | Rat | X-ray | 6Z10 | - | 2.3 | A | Active | 59 | 90 | - | - | - | - | - | Nanobody-6 |
CHEMBL4751488
|
small-molecule | Antagonist | - | - | No | No | Velcicky J,Wilcken R,Cotesta S,Janser P,Schlapbach A,Wagner T,Piechon P,Villard F,Bouhelal R,Piller F,Harlfinger S,Stringer R,Fehlmann D,Kaupmann K,Littlewood-Evans A,Haffke M,Gommermann N | 10.1021/acs.jmedchem.0c01020 | 2020-09-16 | Yes | |
GABR2 | GABAB2 | GABAB | C | Human | Cryo-EM | 7CA5 | - | 7.6 | B | Inactive | - | 70 | - | - | - | - | - | - |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | No | No | Kim Y, Jeong E, Jeong JH, Kim Y, Cho Y | 10.1016/J.JMB.2020.09.023 | 2020-11-11 | Yes | |
NTR1 | NTS1 | Neurotensin | A | Rat | X-ray | 6Z4S | - | 2.7 | A | Inactive | 3 | 77 | - | - | - | - | DARPin D12 | - |
meclinertant
|
small-molecule | Inverse agonist | 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 | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 7ARO | 7ARO_refined | 3.1 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
CHEMBL124345
|
small-molecule | Agonist (partial) | adenosine | small-molecule | No | Yes | Amelia T, van Veldhoven JPD, Falsini M, Liu R, Heitman LH, van Westen GJP, Segala E, Verdon G, Cheng RKY, Cooke RM, van der Es D, IJzerman AP. | 10.1021/acs.jmedchem.0c01856 | 2021-04-07 | Yes | |
CASR | CaS | Calcium-sensing | C | Human | Cryo-EM | 7DD5 | - | 3.2 | A | Inactive | - | 74 | - | - | - | - | - | - |
Calcium
NPS 2143 L-tryptophan |
small-molecule small-molecule small-molecule |
Agonist NAM PAM |
Mg2+, L-tryptophan, spermine, Ca2+ | 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 | 7KI1 | - | 2.5 | R | Active | 100 | 83 | Gs | αs | - | 89 | - | Nanobody-35 |
Taspoglutide
|
peptide | Agonist | glucagon-like peptide 1-(7-36) amide, glucagon, glucagon-like peptide 1-(7-37) | peptide | No | No | - | - | 2021-08-04 | Yes | |
NK1R | NK1 | Tachykinin | A | Human | Cryo-EM | 7RMG | - | 3.0 | R | Active | 100 | 71 | Gq/11 | αq | Gs-Gq chimera | 52 | - | Nanobody-35 |
substance P
|
peptide | Agonist | neuropeptide-γ, neurokinin A, neuropeptide K, neurokinin B, hemokinin 1, 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 | |
GP139 | GPR139 | A orphans | A | Human | Cryo-EM | 7VUJ | 7VUJ_refined | 3.8 | R | Active | 100 | 79 | Gs | αs | - | 59 | - | Nanobody-35 |
JNJ-63533054
|
small-molecule | Agonist | L-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 | |
CASR | CaS | Calcium-sensing | C | Human | Cryo-EM | 7SIL | 7SIL_refined | 2.7 | A | Active | - | 72 | - | - | - | - | - | - |
Cyclomethyltryptophan
tecalcet |
small-molecule small-molecule |
Agonist | Mg2+, L-tryptophan, spermine, Ca2+ | small-molecule | No | No | Park J, Zuo H, Frangaj A, Fu Z, Yen LY, Zhang Z, Mosyak L, Slavkovich VN, Liu J, Ray KM, Cao B, Vallese F, Geng Y, Chen S, Grassucci R, Dandey VP, Tan YZ, Eng E, Lee Y, Kloss B, Liu Z, Hendrickson WA, Potter CS, Carragher B, Graziano J, Conigrave AD, Frank J, Clarke OB, Fan QR | 10.1073/PNAS.2115849118 | 2022-01-19 | Yes | |
CALCR | CT | Calcitonin | B1 | Human | Cryo-EM | 7TYO | - | 2.7 | R | Active | 100 | 76 | Gs | αs | - | 58 | - | Nanobody-35 |
Calcitonin human
|
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 | |
GP183 | GPR183 | A orphans | A | Human | Cryo-EM | 7TUY | - | 3.0 | R | Active | 59 | 73 | - | - | - | - | BRIL | anti-BRIL Fab heavy chain anti-BRIL Fab light chain anti-Fab Nanobody |
8-[(2E)-3-(4-chlorophenyl)prop-2-enoyl]-3-[(3,4-dichlorophenyl)methyl]-1-oxa-3,8-diazaspiro[4.5]decan-2-one
|
small-molecule | Inverse agonist | 7α,25-dihydroxycholesterol, 7α,27-dihydroxycholesterol, 25-hydroxycholesterol, 7α-hydroxycholesterol, 27-hydroxycholesterol, 7β-hydroxycholesterol, 7β, 25-dihydroxycholesterol, 7β, 27-dihydroxycholesterol | small-molecule | No | No | Chen H, Huang W, Li X | 10.1016/J.STR.2022.04.006 | 2022-04-13 | Yes | |
NMUR1 | NMU1 | Neuromedin U | A | Human | Cryo-EM | 7W56 | - | 2.9 | R | Active | 100 | 65 | Gq/11 | αq | - | 59 | - | scFv16 |
Neuromedin-S
|
peptide | Agonist | neuromedin U-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 | |
CCKAR | CCK1 | Cholecystokinin | A | Human | Cryo-EM | 7XOU | - | 3.2 | R | Active | 100 | 67 | Gs | αs | - | 58 | - | Nanobody-35 |
CCK-8
|
peptide | Agonist | desulfated cholecystokinin-8, CCK-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 | |
SSR2 | SST2 | Somatostatin | A | Human | Cryo-EM | 7XAU | - | 3.0 | A | Active | 100 | 76 | Gi/o | αi1 | - | 63 | - | scFv16 |
Octreotide
|
peptide | Agonist | SRIF-28, cortistatin-14, CST-17, SRIF-14 | peptide | No | No | Bo Q, Yang F, Li Y, Meng X, Zhang H, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C | 10.1038/S41421-022-00405-2 | 2022-08-31 | Yes | |
AA2AR | A2A | Adenosine | A | Human | X-ray | 8DU3 | 8DU3_refined | 2.5 | A | Inactive | 0 | 72 | - | - | - | - | BRIL | - |
CHEMBL5206530
|
small-molecule | Antagonist | adenosine | small-molecule | No | No | Bolteau R, Duroux R, Laversin A, Vreulz B, Shiriaeva A, Stauch B, Han GW, Cherezov V, Renault N, Barczyk A, Ravez S, Coevoet M, Melnyk P, Liberelle M, Yous S. | 10.1016/j.ejmech.2022.114620 | 2022-08-10 | Yes | |
TSHR | TSH | Glycoprotein hormone | A | Human | Cryo-EM | 7UTZ | - | 2.4 | R | Active | 100 | 79 | Gs | αs | Mini-Gs | 56 | - | Nanobody-35 |
Thyrotropin subunit beta
Glycoprotein hormones alpha chain analog TR1402 |
protein protein |
Agonist | TSH | peptide | No | No | Faust B, Billesbolle CB, Suomivuori CM, Singh I, Zhang K, Hoppe N, Pinto AFM, Diedrich JK, Muftuoglu Y, Szkudlinski MW, Saghatelian A, Dror RO, Cheng Y, Manglik A | 10.1038/S41586-022-05159-1 | 2022-08-03 | Yes | |
GP132 | GPR132 | A orphans | A | Human | Cryo-EM | 8HQN | 8HQN_refined | 3.0 | R | Active | 100 | 82 | Gi/o | αi1 | - | 60 | BRIL | scFv16 |
9-hydroxyoctadecadienoic acid
|
small-molecule | Agonist | 9-hydroxyoctadecadienoic acid | small-molecule | No | No | Wang JL, Dou XD, Cheng J, Gao MX, Xu GF, Ding W, Ding JH, Li Y, Wang SH, Ji ZW, Zhao XY, Huo TY, Zhang CF, Liu YM, Sha XY, Gao JR, Zhang WH, Hao Y, Zhang C, Sun JP, Jiao N, Yu X | 10.1038/S42255-023-00899-4 | 2023-10-11 | Yes | |
GIPR | GIP | Glucagon | B1 | Human | Cryo-EM | 8ITL | - | 3.2 | R | Active | 100 | 60 | Gs | αs | - | 59 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | gastric inhibitory polypeptide | peptide | No | No | Zhao F, Hang K, Zhou Q, Shao L, Li H, Li W, Lin S, Dai A, Cai X, Liu Y, Xu Y, Feng W, Yang D, Wang MW | 10.1073/PNAS.2306145120 | 2023-10-18 | Yes | |
TAAR1 | TA1 | Trace amine | A | Mouse | Cryo-EM | 8JLK | - | 3.2 | R | Active | 100 | 81 | Gs | αs | - | 59 | - | scFv16 |
ulotaront
|
small-molecule | Agonist | β-phenylethylamine, 3-iodothyronamine, 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 | |
GP161 | GPR161 | A orphans | A | Human | Cryo-EM | 8KH4 | 8KH4_refined | 3.1 | A | Active | 100 | 50 | Gs | αs | - | 58 | - | Nanobody-35 |
Apo (no ligand)
|
none | Apo (no ligand) | - | - | 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 | 2023-10-11 | Yes | |
GP101 | GPR101 | A orphans | A | Human | Cryo-EM | 8W8S | - | 3.3 | R | Active | 85 | 55 | - | - | - | - | - | - |
1-(4-Methylpyridin-2-yl)-3-[3-(trifluoromethyl)phenyl]thiourea
|
small-molecule | Agonist | - | - | No | No | Yang Z, Wang JY, Yang F, Zhu KK, Wang GP, Guan Y, Ning SL, Lu Y, Li Y, Zhang C, Zheng Y, Zhou SH, Wang XW, Wang MW, Xiao P, Yi F, Zhang C, Zhang PJ, Xu F, Liu BH, Zhang H, Yu X, Gao N, Sun JP | 10.1038/S41589-023-01456-6 | 2024-01-03 | Yes | |
GPR34 | GPR34 | A orphans | A | Human | Cryo-EM | 8WRB | - | 2.9 | R | Active | 100 | 74 | Gi/o | αi1 | - | 63 | - | scFv16 |
LYSOPHOSPHATIDIC ACID
|
small-molecule | Agonist | lysophosphatidylserine | small-molecule | No | No | Liu G, Li X, Wang Y, Zhang X, Gong W | 10.1371/JOURNAL.PBIO.3002387 | 2023-11-08 | Yes |
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