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For information on state identification and Δ distance (Å) please refer to the documentation


Select all Receptor Rec family Class Species PDB code Resolution Pre. chain State Δ distance (Å) G-protein Arrestin Fusion Antibodies Endo. ligand Ligand type X-ray ligand X-ray lig. function X-ray lig. type Method Reference Date Annotated Refined Na+ binding GPCR Na+ in xtal
GLP-1 receptor Glucagon receptor family Class B1 (Secretin) Human 5NX2 3.7 A Intermediate 4.86 - - - - - truncated protein agonist
Agonist
Peptide
vapour diffusion 10.1038/NATURE22800 2017-06-14 Yes 5NX2_refined No No
US28 Unclassified Class A (Rhodopsin) strain AD169 5WB1 3.5 A Active - - - Nanobody 7 - N/A N/A N/A in meso/LCP 2018-06-13 Yes 5WB1_refined Yes No
SMO Frizzled Class F (Frizzled) Human 5L7D 3.2 B Inactive -1.98 - - BRIL
- constitutive
Constitutive N/A N/A N/A in meso/LCP 10.1038/NATURE18934 2016-07-20 Yes 5L7D_refined No No
ETB receptor Endothelin receptors Class A (Rhodopsin) Human 5X93 2.2 A Inactive -0.68 - - Endolysin
- - K-8794 pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NSMB.3450 2017-08-16 Yes 5X93_refined Yes No
β2-adrenoceptor Adrenoceptors Class A (Rhodopsin) Human 3SN6 3.2 R Active 9.96 Gs
- T4-Lysozyme
Antibody (-)-adrenaline
(-)-noradrenaline
small molecule BI-167107 pubchem
Agonist
small molecule
sponge mesophase 10.1038/NATURE10361 2011-07-20 Yes 3SN6_refined Yes No
CB1 receptor Cannabinoid receptors Class A (Rhodopsin) Human 5XRA 2.8 A Active 7.95 - - Flavodoxin
- 2-arachidonoylglycerol
Endocannabinoid CHEMBL1683648 pubchem
Agonist
small molecule
in meso/LCP 10.1038/NATURE23272 2017-07-12 Yes 5XRA_refined Yes No
P2Y1 receptor P2Y receptors Class A (Rhodopsin) Human 4XNW 2.7 A Intermediate 5.20 - - Rubredoxin
- ADP
small molecule MRS2500 pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE14287 2015-04-01 Yes 4XNW_refined Yes No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5G53 3.4 A Active 9.79 Engineered G protein
- - - - NECA pubchem
Agonist
small molecule
vapour diffusion 10.1038/NATURE18966 2016-08-03 Yes 5G53_refined Yes No
5-HT1B receptor 5-Hydroxytryptamine receptors Class A (Rhodopsin) Human 6G79 3.8 S Active 8.90 Go
- - - - Donitriptan pubchem
Agonist
small molecule
Cryo-EM 10.1038/S41586-018-0241-9 2018-06-20 Yes - Yes No
β2-adrenoceptor Adrenoceptors Class A (Rhodopsin) Human 5JQH 3.2 A Inactive -1.07 - - T4-Lysozyme
Nanobody (-)-adrenaline
(-)-noradrenaline
small molecule Carazolol pubchem
Inverse agonist
small molecule
in meso/LCP 10.1038/NATURE18636 2016-07-13 Yes 5JQH_refined Yes No
PAR1 Proteinase-activated receptors Class A (Rhodopsin) Human 3VW7 2.2 A Intermediate 6.18 - - T4-Lysozyme
- thrombin
Peptide Vorapaxar pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE11701 2012-12-12 Yes 3VW7_refined Yes No
GLP-1 receptor Glucagon receptor family Class B1 (Secretin) Human 5VEW 2.7 A Inactive -5.10 - - Endolysin
- - 97Y pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE22378 2017-05-24 Yes 5VEW_refined No No
OX2 receptor Orexin receptors Class A (Rhodopsin) Human 5WS3 2.3 A Inactive -1.13 - - Glycogen synthase
- - EMPA pubchem chembl_ligand
Antagonist
small molecule
in meso/LCP 2017-12-13 Yes - Yes No
CB1 receptor Cannabinoid receptors Class A (Rhodopsin) Human 5TGZ 2.8 A Inactive -0.85 - - Flavodoxin
- 2-arachidonoylglycerol
Endocannabinoid SCHEMBL662960 pubchem
Antagonist
small molecule
in meso/LCP 10.1016/J.CELL.2016.10.004 2016-11-02 Yes 5TGZ_refined Yes No
NTS1 receptor Neurotensin receptors Class A (Rhodopsin) Rat 5T04 3.3 A Active 8.26 - - T4-Lysozyme
- Neurotensin
neurotensin
Peptide CHEMBL342252 pubchem
Agonist
Peptide
in meso/LCP 10.1038/SREP38564 2016-12-21 Yes 5T04_refined Yes No
M1 receptor Acetylcholine receptors (muscarinic) Class A (Rhodopsin) Human 5CXV 2.7 A Inactive 0.64 - - Endolysin
- acetylcholine
small molecule CHEMBL258622 pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE17188 2016-03-09 Yes 5CXV_refined Yes No
δ receptor Opioid receptors Class A (Rhodopsin) Human 4N6H 1.8 A Inactive -1.54 - - BRIL
- β-endorphin
dynorphin A
dynorphin B
endomorphin-1
[Leu]enkephalin
[Met]enkephalin
Peptide Naltrindole pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE12944 2013-12-25 Yes 4N6H_refined Yes Yes
BLT1 receptor Leukotriene receptors Class A (Rhodopsin) Guinea pig 5X33 3.7 A Inactive -1.53 - - Endolysin
- - BIIL-260 pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NCHEMBIO.2547 2018-01-03 Yes 5X33_refined Yes No
mGlu5 receptor Metabotropic glutamate receptors Class C (Glutamate) Human 4OO9 2.6 A Inactive 3.98 - - T4-Lysozyme
- L-glutamic acid
small molecule Mavoglurant pubchem
NAM
small molecule
in meso/LCP 10.1038/NATURE13396 2014-07-02 Yes - No No
μ receptor Opioid receptors Class A (Rhodopsin) Mouse 5C1M 2.1 A Active 10.99 - - - Antibody β-endorphin
dynorphin A
dynorphin B
endomorphin-1
[Leu]enkephalin
[Met]enkephalin
Peptide BU72 pubchem
Agonist
small molecule
in meso/LCP 10.1038/NATURE14886 2015-08-05 Yes 5C1M_refined Yes No
LPA6 receptor Lysophospholipid (LPA) receptors Class A (Rhodopsin) Zebrafish 5XSZ 3.2 A Active 9.96 - - Endolysin
- - N/A N/A N/A in meso/LCP 10.1038/NATURE23448 2017-08-16 Yes 5XSZ_refined Yes No
5-HT2C receptor 5-Hydroxytryptamine receptors Class A (Rhodopsin) Human 6BQH 2.7 A Inactive 0.08 - - Soluble cytochrome b562
- - Ritanserin pubchem
Inverse agonist
small molecule
in meso/LCP 10.1016/J.CELL.2018.01.001 2018-02-14 Yes - Yes No
M2 receptor Acetylcholine receptors (muscarinic) Class A (Rhodopsin) Human 4MQT 3.7 A Active 8.74 - - - Nanobody acetylcholine
small molecule LY2119620 pubchem
iperoxo pubchem
PAM
Agonist
small molecule
small molecule
in meso/LCP 10.1038/NATURE12735 2013-11-27 Yes 4MQT_refined Yes No
FFA1 receptor Free fatty acid receptors Class A (Rhodopsin) Human 5TZY 3.2 A Intermediate 3.21 - - Endolysin
- long chain carboxylic acids
Lipid (2s,3r)-3-Cyclopropyl-3-[(2r)-2-(1-{(1s)-1-[5-Fluoro-2-(Trifluoromethoxy)phenyl]ethyl}piperidin-4-Yl)-3,4-Dihydro-2h-1-Benzopyran-7-Yl]-2-Methylpropanoic Acid pubchem
UNII-11612L5SPI pubchem
Agonist
Agonist
small molecule
small molecule
in meso/LCP 10.1038/NSMB.3417 2017-06-07 Yes 5TZY_refined No No
Y1 receptor Neuropeptide Y receptors Class A (Rhodopsin) Human 5ZBH 3.0 A Inactive -0.68 - - T4-Lysozyme
- - BMS-193885 pubchem
Antagonist
small molecule
N/A 10.1038/S41586-018-0046-X 2018-04-25 Yes 5ZBH_refined Yes No
M2 receptor Acetylcholine receptors (muscarinic) Class A (Rhodopsin) Human 3UON 3.0 A Inactive -1.50 - - T4-Lysozyme
- acetylcholine
small molecule 62869-69-6 pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE10753 2012-02-01 Yes 3UON_refined Yes No
D2 receptor Dopamine receptors Class A (Rhodopsin) Human 6CM4 2.9 A Inactive -1.80 - - Endolysin
- - Risperidone pubchem chembl_ligand
Inverse agonist
small molecule
in meso/LCP 10.1038/NATURE25758 2018-03-14 Yes 6CM4_refined Yes No
AT2 receptor Angiotensin receptors Class A (Rhodopsin) Human 5UNG 2.8 B Active 8.46 - - BRIL
- - CHEMBL289472 pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE22035 2017-04-05 Yes - Yes No
M4 receptor Acetylcholine receptors (muscarinic) Class A (Rhodopsin) Human 5DSG 2.6 B Inactive 0.28 - - T4-Lysozyme
- acetylcholine
small molecule Tiotropium pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE17188 2016-03-16 Yes 5DSG_refined Yes No
κ receptor Opioid receptors Class A (Rhodopsin) Human 4DJH 2.9 A Inactive -1.29 - - T4-Lysozyme
- dynorphin A
Peptide JDTic pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE10939 2012-03-21 Yes 4DJH_refined Yes No
PAF receptor Platelet-activating factor receptors Class A (Rhodopsin) Human 5ZKP 2.8 A Active 15.31 - - Flavodoxin
- - Foropafant pubchem
Antagonist
small molecule
N/A 10.1038/S41594-018-0068-Y 2018-06-20 Yes 5ZKP_refined Yes No
H1 receptor Histamine receptors Class A (Rhodopsin) Human 3RZE 3.1 A Inactive 0.45 - - T4-Lysozyme
- histamine
small molecule doxepin pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE10236 2011-06-15 Yes 3RZE_refined Yes No
NOP receptor Opioid receptors Class A (Rhodopsin) Human 5DHG 3.0 A Inactive -1.28 - - BRIL
- nociceptin/orphanin FQ
Peptide N/A N/A N/A in meso/LCP 10.1016/J.STR.2015.07.024 2015-10-21 Yes 5DHG_refined Yes No
5-HT2B receptor 5-Hydroxytryptamine receptors Class A (Rhodopsin) Human 5TUD 3.0 D Active 8.66 - - BRIL
Antibody Fab fragment 5-hydroxytryptamine
small molecule Ergotamine pubchem
Agonist
small molecule
in meso/LCP 10.1073/PNAS.1700891114 2017-07-26 Yes 5TUD_refined Yes No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 4UHR 2.6 A Intermediate 6.28 - - - - - Cgs 21680 pubchem
Agonist
small molecule
in meso/LCP 10.1124/MOL.114.097360 2015-04-08 Yes 4UHR_refined Yes No
PAR2 Proteinase-activated receptors Class A (Rhodopsin) Human 5NDD 2.8 A Intermediate 7.07 - - BRIL
T4-Lysozyme
- - GTPL9585 pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE22309 2017-05-03 Yes 5NDD_refined Yes Yes
M3 receptor Acetylcholine receptors (muscarinic) Class A (Rhodopsin) Rat 4U15 2.8 B Inactive 0.50 - - T4-Lysozyme
- acetylcholine
small molecule Tiotropium pubchem
Antagonist
small molecule
in meso/LCP 10.1016/J.STR.2014.08.022 2014-11-26 Yes 4U15_refined Yes No
CCR2 Chemokine receptors Class A (Rhodopsin) Human 5T1A 2.8 A Inactive 1.66 - - T4-Lysozyme
- - CCR2-RA-[R] pubchem
CHEMBL3577945 pubchem
Antagonist
Antagonist
small molecule
small molecule
in meso/LCP 10.1038/NATURE20605 2016-12-14 Yes 5T1A_refined No No
κ receptor Opioid receptors Class A (Rhodopsin) Human 6B73 3.1 A Active 9.71 - - Soluble cytochrome b562
Nanobody dynorphin A
Peptide MP1104 pubchem
Agonist
small molecule
in meso/LCP 10.1016/J.CELL.2017.12.011 2018-01-17 Yes 6B73_refined Yes No
Rhodopsin Opsins Class A (Rhodopsin) Japanese flying squid 2Z73 2.5 A Inactive -0.27 - - - - retinal
small molecule retinal gtoplig
Inverse agonist
small molecule
vapour diffusion 10.1038/NATURE06925 2008-05-13 Yes 2Z73_refined Yes No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 5DYS 2.3 A Active 7.70 - - - - retinal
small molecule retinal gtoplig
Inverse agonist
small molecule
vapour diffusion 10.15252/EMBR.201642671 2016-08-10 Yes 5DYS_refined No No
A1 receptor Adenosine receptors Class A (Rhodopsin) Human 5UEN 3.2 B Inactive -1.06 - - BRIL
- - CHEMBL144360 pubchem
Antagonist
small molecule
in meso/LCP 10.1016/J.CELL.2017.01.042 2017-03-01 Yes 5UEN_refined Yes No
LPA1 receptor Lysophospholipid (LPA) receptors Class A (Rhodopsin) Human 4Z35 2.9 A Inactive -1.30 - - BRIL
- LPA
Lipid ONO-9910539 pubchem
Antagonist
small molecule
in meso/LCP 10.1016/J.CELL.2015.06.002 2015-06-03 Yes 4Z35_refined Yes No
CXCR4 Chemokine receptors Class A (Rhodopsin) Human 3ODU 2.5 A Inactive -1.34 - - T4-Lysozyme
- CXCL12α
CXCL12β
Peptide IT1t pubchem
Antagonist
small molecule
in meso/LCP 10.1126/SCIENCE.1194396 2010-10-27 Yes 3ODU_refined Yes No
C5a1 receptor Complement peptide receptors Class A (Rhodopsin) Human 5O9H 2.7 A Inactive -1.46 - - - - - NDT 9513727 pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE25025 2018-01-10 Yes 5O9H_refined Yes No
CCR9 Chemokine receptors Class A (Rhodopsin) Human 5LWE 2.8 B Inactive 0.09 - - - - - Vercirnon pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE20606 2016-12-07 Yes - No No
D3 receptor Dopamine receptors Class A (Rhodopsin) Human 3PBL 2.9 A Inactive -0.43 - - T4-Lysozyme
- dopamine
small molecule Eticlopride pubchem
Antagonist
small molecule
in meso/LCP 10.1126/SCIENCE.1197410 2010-11-03 Yes 3PBL_refined Yes No
glucagon receptor Glucagon receptor family Class B1 (Secretin) Human 5XEZ 3.0 B Inactive -4.53 - - T4-Lysozyme
mAb1 - 4-{[(4-Cyclohexylphenyl){[3-(Methylsulfonyl)phenyl]carbamoyl}amino]methyl}-N-(1h-Tetrazol-5-Yl)benzamide pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE22363 2017-05-24 Yes 5XEZ_refined No No
apelin receptor Apelin receptors Class A (Rhodopsin) Human 5VBL 2.6 B Inactive -0.37 - - Rubredoxin
- apelin-13
apelin receptor early endogenous ligand
Peptide AMG3054
Agonist
Peptide
in meso/LCP 10.1016/J.STR.2017.04.008 2017-05-31 Yes 5VBL_refined Yes No
δ receptor Opioid receptors Class A (Rhodopsin) Mouse 4EJ4 3.4 A Inactive -1.23 - - T4-Lysozyme
- β-endorphin
dynorphin A
dynorphin B
endomorphin-1
[Leu]enkephalin
[Met]enkephalin
Peptide Naltrindole pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE11111 2012-05-16 Yes 4EJ4_refined Yes No
D4 receptor Dopamine receptors Class A (Rhodopsin) Human 5WIV 2.1 A Inactive -0.93 - - BRIL
- - Nemonapride pubchem
Antagonist
small molecule
in meso/LCP 10.1126/SCIENCE.AAN5468 2017-10-18 Yes 5WIV_refined Yes Yes
A1 receptor Adenosine receptors Class A (Rhodopsin) Human 6D9H 3.6 R Active 9.23 Gi2
- - - - Adenosine pubchem
Agonist
small molecule
Cryo-EM 10.1038/S41586-018-0236-6 2018-06-20 Yes 6D9H_refined Yes No
GLP-1 receptor Glucagon receptor family Class B1 (Secretin) Rabbit 5VAI 4.1 R Active 6.89 Gs
- - - glucagon-like peptide 1
Peptide GLP-1 pubchem
Agonist
Peptide
Cryo-EM 10.1038/NATURE22394 2017-05-24 Yes 5VAI_refined No No
GLP-1 receptor Glucagon receptor family Class B1 (Secretin) Human 6B3J 3.3 R Active 6.78 Gs
- - - - Exendin-P5
Agonist
Peptide
Cryo-EM 10.1038/NATURE25773 2018-02-21 Yes 6B3J_refined No No
CRF1 receptor Corticotropin-releasing factor receptors Class B1 (Secretin) Human 4Z9G 3.2 A Inactive -0.98 - - T4-Lysozyme
- corticotrophin-releasing hormone
Peptide CP-376395 pubchem
Antagonist
small molecule
in meso/LCP 10.2174/1874467210666170110114727 2016-06-29 Yes 4Z9G_refined No No
P2Y12 receptor P2Y receptors Class A (Rhodopsin) Human 4NTJ 2.6 A Intermediate 4.74 - - BRIL
- - AZD1283 pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE13083 2014-03-26 Yes - Yes No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 1GZM 2.7 A Inactive 0.06 - - - - retinal
small molecule retinal gtoplig
Inverse agonist
small molecule
vapour diffusion 10.1016/J.JMB.2004.08.090 2003-11-20 Yes - No No
AT1 receptor Angiotensin receptors Class A (Rhodopsin) Human 4ZUD 2.8 A Inactive -0.93 - - BRIL
- - OLM
Inverse agonist
small molecule
in meso/LCP 10.1074/JBC.M115.689000 2015-10-07 Yes 4ZUD_refined Yes No
NTS1 receptor Neurotensin receptors Class A (Rhodopsin) Rat 4XES 2.6 A Intermediate 6.03 - - T4-Lysozyme
- Neurotensin
neurotensin
Peptide CHEMBL342252 pubchem
Agonist
Peptide
in meso/LCP 10.1038/NCOMMS8895 2015-07-29 Yes 4XES_refined Yes No
OX1 receptor Orexin receptors Class A (Rhodopsin) Human 4ZJ8 2.8 A Inactive -0.47 - - - - noradrenaline
small molecule retinal gtoplig
Inverse agonist
small molecule
in meso/LCP 10.1038/NSMB.3183 2016-03-09 Yes 4ZJ8_refined No No
NTS1 receptor Neurotensin receptors Class A (Rhodopsin) Rat 4BUO 2.8 A Inactive 0.57 - - - - Neurotensin
neurotensin
Peptide CHEMBL342252 pubchem
Agonist
Peptide
vapour diffusion 10.1073/PNAS.1317903111 2014-01-29 Yes - Yes No
CCR5 Chemokine receptors Class A (Rhodopsin) Human 5UIW 2.2 A Inactive 1.02 - - Rubredoxin
- CCL11
CCL14
CCL16
CCL2
CCL3
CCL4
CCL5
CCL7
CCL8
Peptide 5P7-CCL5
Antagonist
Peptide
in meso/LCP 10.1016/J.IMMUNI.2017.05.002 2017-06-28 Yes 5UIW_refined No No
US28 Unclassified Class A (Rhodopsin) strain AD169 4XT1 2.9 A Active 9.02 - - - SignProtMimic_Nanobody CX3CL1
Peptide CX3CL1
Agonist
Peptide
in meso/LCP 10.1126/SCIENCE.AAA5026 2015-03-04 Yes 4XT1_refined Yes No
CT receptor Calcitonin receptors Class B1 (Secretin) Human 5UZ7 4.1 R Active 7.80 Gs
- - - - N/A N/A N/A Cryo-EM 10.1038/NATURE22327 2017-05-03 Yes 5UZ7_refined No No
PAF receptor Platelet-activating factor receptors Class A (Rhodopsin) Human 5ZKQ 2.9 B Intermediate 4.76 - - Endolysin
- - ABT-491 pubchem chembl_ligand
Inverse agonist
small molecule
N/A 10.1038/S41594-018-0068-Y 2018-06-20 Yes - Yes No
S1P1 receptor Lysophospholipid (S1P) receptors Class A (Rhodopsin) Human 3V2Y 2.8 A Inactive -0.61 - - T4-Lysozyme
- sphingosine 1-phosphate
Lipid 909725-61-7 pubchem
Antagonist
small molecule
in meso/LCP 10.1126/SCIENCE.1215904 2012-02-15 Yes 3V2Y_refined Yes No
5-HT2B receptor 5-Hydroxytryptamine receptors Class A (Rhodopsin) Human 4IB4 2.7 A Intermediate 3.08 - - BRIL
- 5-hydroxytryptamine
small molecule ERGOTAMINE pubchem
Agonist
small molecule
in meso/LCP 10.1126/SCIENCE.1232808 2013-03-13 Yes 4IB4_refined Yes No
mGlu1 receptor Metabotropic glutamate receptors Class C (Glutamate) Human 4OR2 2.8 A,B Inactive 4.00 - - BRIL
- L-glutamic acid
small molecule FITM pubchem
NAM
small molecule
in meso/LCP 10.1126/SCIENCE.1249489 2014-03-19 Yes - No No
5-HT1B receptor 5-Hydroxytryptamine receptors Class A (Rhodopsin) Human 4IAQ 2.8 A Intermediate 2.79 - - BRIL
- - dihydroergotamine pubchem
Agonist
small molecule
in meso/LCP 10.1126/SCIENCE.1232807 2013-03-13 Yes 4IAQ_refined Yes No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 3VG9 2.7 A Inactive -1.20 - - - - - 139180-30-6 pubchem
Antagonist
small molecule
vapour diffusion 10.1038/NATURE10750 2012-02-01 Yes 3VG9_refined Yes No
Rhodopsin Opsins Class A (Rhodopsin) Human 4ZWJ 3.3 A Active 8.61 - S-arrestin
T4-Lysozyme
- retinal
small molecule N/A N/A N/A in meso/LCP 10.1038/NATURE14656 2015-07-29 Yes 4ZWJ_refined No No
μ receptor Opioid receptors Class A (Rhodopsin) Mouse 4DKL 2.8 A Inactive -1.44 - - T4-Lysozyme
- β-endorphin
dynorphin A
dynorphin B
endomorphin-1
[Leu]enkephalin
[Met]enkephalin
Peptide BF0
Antagonist
small molecule
in meso/LCP 10.1038/NATURE10954 2012-03-21 Yes 4DKL_refined Yes No
β1-adrenoceptor Adrenoceptors Class A (Rhodopsin) Common turkey 4AMJ 2.3 B Inactive -1.01 - - - - - (S)-Carvedilol pubchem
Inverse agonist
small molecule
vapour diffusion 10.1016/J.STR.2012.03.014 2012-05-23 Yes - Yes No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 1HZX 2.8 A,B Inactive -0.02 - - - - retinal
small molecule retinal gtoplig
Inverse agonist
small molecule
vapour diffusion 10.1021/BI0155091 2001-07-04 No - No No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 1L9H 2.6 A Inactive -0.45 - - - - retinal
small molecule retinal gtoplig
Inverse agonist
small molecule
vapour diffusion 10.1073/PNAS.082666399 2002-05-15 No - No No
β2-adrenoceptor Adrenoceptors Class A (Rhodopsin) Human 2RH1 2.4 A Inactive -0.82 - - T4-Lysozyme
- (-)-adrenaline
(-)-noradrenaline
small molecule Carazolol pubchem
Inverse agonist
small molecule
in meso/LCP 10.1126/SCIENCE.1150577 2007-10-30 Yes 2RH1_refined Yes No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5IU8 2.0 A Inactive -0.82 - - BRIL
- - CHEMBL3934661 pubchem
Agonist
small molecule
in meso/LCP 2016-06-29 Yes 5IU8_refined Yes Yes
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 3UZC 3.3 A Inactive -0.50 - - - - - T4E
Antagonist
small molecule
vapour diffusion 10.1021/JM201376W 2012-03-21 Yes - Yes No
β1-adrenoceptor Adrenoceptors Class A (Rhodopsin) Common turkey 2Y00 2.5 B Inactive -1.22 - - - - - Dobutamine pubchem
Agonist (partial)
small molecule
vapour diffusion 2011-01-12 Yes 2Y00_refined Yes No
β2-adrenoceptor Adrenoceptors Class A (Rhodopsin) Human 3PDS 3.5 A Inactive -0.96 - - T4-Lysozyme
- (-)-adrenaline
(-)-noradrenaline
small molecule FAUC50 pubchem
Agonist
small molecule
in meso/LCP 10.1038/NATURE09665 2011-01-12 Yes 3PDS_refined Yes No
β2-adrenoceptor Adrenoceptors Class A (Rhodopsin) Human 3NY8 2.8 A Inactive -1.26 - - T4-Lysozyme
- (-)-adrenaline
(-)-noradrenaline
small molecule AC1NSK5N pubchem
Inverse agonist
small molecule
in meso/LCP 10.1021/JA105108Q 2010-08-11 Yes 3NY8_refined Yes No
β1-adrenoceptor Adrenoceptors Class A (Rhodopsin) Common turkey 2Y04 3.1 B Inactive -1.14 - - - - - Levalbuterol pubchem
Agonist (partial)
small molecule
vapour diffusion 10.1038/NATURE09746 2011-01-12 Yes 2Y04_refined Yes No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5IUB 2.1 A Inactive -0.87 - - BRIL
- - CHEMBL184061 pubchem
Agonist
small molecule
in meso/LCP 10.1021/ACS.JMEDCHEM.6B00653 2016-06-29 Yes 5IUB_refined Yes Yes
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5K2C 1.9 A Inactive -0.67 - - BRIL
- - 139180-30-6 pubchem
Antagonist
small molecule
in meso/LCP 10.1126/SCIADV.1600292 2016-09-21 Yes - Yes Yes
Rhodopsin Opsins Class A (Rhodopsin) Bovine 4J4Q 2.7 A Active 8.54 Gt
- - - retinal
small molecule N/A N/A N/A vapour diffusion 10.1002/ANIE.201302374 2013-10-30 Yes 4J4Q_refined No No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5N2R 2.8 A Inactive -0.73 - - BRIL
- - PSB36 pubchem
Antagonist
small molecule
in meso/LCP 10.1016/J.STR.2017.06.012 2017-07-26 Yes 5N2R_refined Yes Yes
Rhodopsin Opsins Class A (Rhodopsin) Japanese flying squid 3AYM 2.8 A,B Inactive -0.22 - - - - retinal
small molecule retinal gtoplig
Agonist
small molecule
vapour diffusion 10.1016/J.JMB.2011.08.044 2011-08-17 No - Yes No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 2PED 3.0 A,B Inactive 0.24 - - - - retinal
small molecule retinal gtoplig
Inverse agonist
small molecule
vapour diffusion 10.1529/BIOPHYSJ.107.108225 2007-10-30 No - No No
OX2 receptor Orexin receptors Class A (Rhodopsin) Human 5WQC 2.0 A Inactive -0.99 - - Glycogen synthase
- - EMPA pubchem chembl_ligand
Antagonist
small molecule
in meso/LCP 10.1016/J.STR.2017.11.005 2017-11-29 Yes 5WQC_refined Yes No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5OLO 3.1 A Inactive -0.69 - - Soluble cytochrome b562
- - Tozadenant pubchem chembl_ligand
Antagonist
small molecule
in meso/LCP 10.1038/S41598-017-18570-W 2018-01-17 Yes 5OLO_refined Yes No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5VRA 2.4 A Inactive -0.39 - - BRIL
- - ZM 241385 pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NPROT.2017.135 2017-12-13 Yes 5VRA_refined Yes Yes
δ receptor Opioid receptors Class A (Rhodopsin) Human 4RWD 2.7 A,B Inactive -0.83 - - BRIL
- β-endorphin
dynorphin A
dynorphin B
endomorphin-1
[Leu]enkephalin
[Met]enkephalin
Peptide DIPP-NH2
Antagonist
peptide-like
in meso/LCP 10.1038/NSMB.2965 2015-01-14 Yes 4RWD_refined Yes Yes
SMO Frizzled Class F (Frizzled) Human 5L7I 3.3 B Inactive -2.33 - - BRIL
- constitutive
Constitutive Vismodegib pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE18934 2016-07-20 Yes 5L7I_refined No No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 5TE3 2.7 A Active 7.98 - - - - retinal
small molecule N/A N/A N/A vapour diffusion 10.1073/PNAS.1617446114 2017-03-15 Yes 5TE3_refined No No
β2-adrenoceptor Adrenoceptors Class A (Rhodopsin) Human 5D5A 2.5 A Inactive -1.14 - - T4-Lysozyme
- (-)-adrenaline
(-)-noradrenaline
small molecule Carazolol pubchem
Inverse agonist
small molecule
in meso/LCP 10.1107/S2059798315021683 2016-01-13 No - Yes No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 4EIY 1.8 A Inactive -0.55 - - BRIL
- - 139180-30-6 pubchem
Antagonist
small molecule
in meso/LCP 10.1126/SCIENCE.1219218 2012-07-25 Yes 4EIY_refined Yes Yes
β1-adrenoceptor Adrenoceptors Class A (Rhodopsin) Common turkey 2Y03 2.9 B Inactive -1.20 - - - - - LEVISOPRENALINE pubchem
Agonist
small molecule
vapour diffusion 10.1038/NATURE09746 2011-01-12 Yes 2Y03_refined Yes No
SMO Frizzled Class F (Frizzled) Human 5V56 2.9 B Inactive -1.89 - - Flavodoxin
- constitutive
Constitutive N-methyl-N-[1-[4-(2-methylpyrazol-3-yl)phthalazin-1-yl]piperidin-4-yl]-4-nitro-2-(trifluoromethyl)benzamide pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NCOMMS15383 2017-05-24 Yes - No No
β1-adrenoceptor Adrenoceptors Class A (Rhodopsin) Common turkey 2YCX 3.3 A Inactive -1.64 - - - - - (S)-Cyanopindolol pubchem
Antagonist
small molecule
vapour diffusion 10.1073/PNAS.1100185108 2011-06-01 No - Yes No
CRF1 receptor Corticotropin-releasing factor receptors Class B1 (Secretin) Human 4K5Y 3.0 C Inactive -2.02 - - T4-Lysozyme
- corticotrophin-releasing hormone
Peptide CP-376395 pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE12357 2013-07-17 Yes 4K5Y_refined No No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 6AQF 2.5 A Inactive -0.44 - - Soluble cytochrome b562
- - ZM 241385 pubchem
Antagonist
small molecule
in meso/LCP 10.1016/J.CELL.2017.12.004 2018-01-10 Yes 6AQF_refined Yes No
NTS1 receptor Neurotensin receptors Class A (Rhodopsin) Rat 3ZEV 3.0 A Inactive 0.45 - - - - Neurotensin
neurotensin
Peptide CHEMBL342252 pubchem
Agonist
Peptide
vapour diffusion 10.1073/PNAS.1317903111 2014-01-29 No - Yes No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 6FK7 2.6 A Active 7.68 - - - - retinal
small molecule (2~{R},3~{R})-2-(4-chlorophenyl)-3-oxidanyl-1-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-yl-butan-1-one
Agonist
small molecule
N/A 10.1073/PNAS.1718084115 2018-04-04 Yes 6FK7_refined No No
5-HT2C receptor 5-Hydroxytryptamine receptors Class A (Rhodopsin) Human 6BQG 3.0 A Active 7.92 - - Soluble cytochrome b562
- - Ergotamine pubchem
Agonist
small molecule
in meso/LCP 10.1016/J.CELL.2018.01.001 2018-02-14 Yes - Yes No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5OLH 2.6 A Inactive -0.70 - - Soluble cytochrome b562
- - Vipadenant
Antagonist
small molecule
in meso/LCP 10.1038/S41598-017-18570-W 2018-01-17 Yes 5OLH_refined Yes Yes
β1-adrenoceptor Adrenoceptors Class A (Rhodopsin) Common turkey 5F8U 3.4 A Inactive -0.51 - - - - - (S)-Cyanopindolol pubchem
Antagonist
small molecule
vapour diffusion 10.1038/NSMB.3130 2015-12-23 Yes 5F8U_refined Yes No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 6FK6 2.4 A Active 7.85 - - - - retinal
small molecule (2~{S})-2-(4-chlorophenyl)-3-methyl-1-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-yl-butan-1-one
Agonist
small molecule
N/A 10.1073/PNAS.1718084115 2018-04-04 Yes 6FK6_refined No No
CB1 receptor Cannabinoid receptors Class A (Rhodopsin) Human 5XR8 3.0 A Active 7.90 - - Flavodoxin
- 2-arachidonoylglycerol
Endocannabinoid 8D0
Agonist
small molecule
in meso/LCP 10.1038/NATURE23272 2017-07-12 Yes - Yes No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 2YDV 2.6 A Intermediate 6.21 - - - - - NECA pubchem
Agonist
small molecule
vapour diffusion 10.1038/NATURE10136 2011-05-18 Yes 2YDV_refined Yes No
β1-adrenoceptor Adrenoceptors Class A (Rhodopsin) Common turkey 2VT4 2.7 B Inactive -1.55 - - - - - (S)-Cyanopindolol pubchem
Antagonist
small molecule
vapour diffusion 10.1038/NATURE07101 2008-06-24 No - Yes No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 3REY 3.3 A Inactive -0.38 - - - - - Xanthine amine congener pubchem
Antagonist
small molecule
vapour diffusion 10.1016/J.STR.2011.06.014 2011-09-07 Yes 3REY_refined Yes No
β1-adrenoceptor Adrenoceptors Class A (Rhodopsin) Common turkey 4AMI 3.2 A Inactive -1.16 - - - - - bucindolol pubchem
Agonist
small molecule
vapour diffusion 10.1016/J.STR.2012.03.014 2012-05-23 Yes 4AMI_refined Yes No
P2Y12 receptor P2Y receptors Class A (Rhodopsin) Human 4PY0 3.1 A Intermediate 3.81 - - BRIL
- - 2-Mesatp pubchem
Agonist (partial)
small molecule
in meso/LCP 10.1038/NATURE13288 2014-04-30 Yes 4PY0_refined Yes No
CXCR4 Chemokine receptors Class A (Rhodopsin) Human 3OE9 3.1 A Inactive -0.65 - - T4-Lysozyme
- CXCL12α
CXCL12β
Peptide IT1t pubchem
Antagonist
small molecule
in meso/LCP 10.1126/SCIENCE.1194396 2010-10-27 No - Yes No
β2-adrenoceptor Adrenoceptors Class A (Rhodopsin) Human 2R4R 3.4 A Inactive -2.80 - - - Antibody (-)-adrenaline
(-)-noradrenaline
small molecule N/A N/A N/A vapour diffusion 10.1038/NATURE06325 2007-11-06 No - Yes No
β2-adrenoceptor Adrenoceptors Class A (Rhodopsin) Human 4LDE 2.8 A Active 9.40 - - T4-Lysozyme
SignProtMimic_Nanobody (-)-adrenaline
(-)-noradrenaline
small molecule BI167107 pubchem
Agonist
small molecule
in meso/LCP 10.1038/NATURE12572 2013-09-25 Yes - Yes No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 4PXF 2.8 A Active 8.58 - Arrestin fragment
- - retinal
small molecule N/A N/A N/A vapour diffusion 10.1038/NCOMMS5801 2014-09-17 No - No No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5MZJ 2.0 A Inactive -0.54 - - - - - Theophylline pubchem
Antagonist
small molecule
in meso/LCP 10.1016/J.STR.2017.06.012 2017-07-26 Yes - Yes Yes
glucagon receptor Glucagon receptor family Class B1 (Secretin) Human 4L6R 3.3 A Inactive -4.62 - - BRIL
- - N/A N/A N/A in meso/LCP 10.1038/NATURE12393 2013-07-24 Yes 4L6R_refined No No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5MZP 2.1 A Inactive -0.75 - - - - - Caffeine pubchem
Antagonist
small molecule
in meso/LCP 10.1016/J.STR.2017.06.012 2017-07-26 Yes 5MZP_refined Yes Yes
Rhodopsin Opsins Class A (Rhodopsin) Bovine 3OAX 2.6 A Inactive 0.02 - - - - retinal
small molecule retinal gtoplig
Inverse agonist
small molecule
vapour diffusion 10.1016/J.BPJ.2010.08.003 2011-01-19 No - No No
μ receptor Opioid receptors Class A (Rhodopsin) Mouse 6DDF 3.5 R Active 7.85 Gi
- - - β-endorphin
dynorphin A
dynorphin B
endomorphin-1
[Leu]enkephalin
[Met]enkephalin
Peptide DAMGO pubchem chembl_ligand
Agonist
peptide-like
Cryo-EM 10.1038/S41586-018-0219-7 2018-06-13 Yes 6DDF_refined Yes No
Rhodopsin Opsins Class A (Rhodopsin) Japanese flying squid 4WW3 2.8 A, B Inactive 0.10 - - - - retinal
small molecule retinal gtoplig
Inverse agonist
small molecule
vapour diffusion 10.1371/JOURNAL.PONE.0126970 2015-06-17 No - Yes No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 2YDO 3.0 A Intermediate 6.28 - - - - - adenosine pubchem
Agonist
small molecule
vapour diffusion 10.1038/NATURE10136 2011-05-18 Yes 2YDO_refined Yes No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5JTB 2.8 A Inactive -0.46 - - BRIL
- - 139180-30-6 pubchem
Antagonist
small molecule
in meso/LCP 10.1126/SCIADV.1602952 2017-05-31 Yes 5JTB_refined Yes No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 3PQR 2.9 A Active 8.57 Gt
- - - retinal
small molecule retinal gtoplig
Agonist
small molecule
vapour diffusion 10.1038/NATURE09789 2011-03-09 Yes 3PQR_refined No No
glucagon receptor Glucagon receptor family Class B1 (Secretin) Human 5YQZ 3.0 R Inactive -4.97 - - T4-Lysoyzme
- - NNC1702
Partial agonist
Peptide
in meso/LCP 10.1038/NATURE25153 2018-01-17 Yes 5YQZ_refined No No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 4BEZ 3.3 A Active 8.33 - - - - retinal
small molecule N/A N/A N/A vapour diffusion 10.1038/EMBOR.2013.44 2013-04-24 No - No No
β2-adrenoceptor Adrenoceptors Class A (Rhodopsin) Human 3NYA 3.2 A Inactive -1.28 - - T4-Lysozyme
- (-)-adrenaline
(-)-noradrenaline
small molecule (-)-Alprenolol pubchem
Antagonist
small molecule
in meso/LCP 10.1021/JA105108Q 2010-08-11 Yes 3NYA_refined Yes No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 2I35 3.8 A Inactive -0.33 - - - - retinal
small molecule retinal gtoplig
Inverse agonist
small molecule
vapour diffusion 10.1073/PNAS.0608022103 2006-10-17 No - No No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5IUA 2.2 A Inactive -0.68 - - BRIL
- - 2-(Furan-2-Yl)-N~5~-[3-(4-Phenylpiperazin-1-Yl)propyl][1,2,4]triazolo[1,5-A][1,3,5]triazine-5,7-Diamine pubchem
Agonist
small molecule
in meso/LCP 10.1021/ACS.JMEDCHEM.6B00653 2016-06-29 Yes 5IUA_refined Yes Yes
M2 receptor Acetylcholine receptors (muscarinic) Class A (Rhodopsin) Human 4MQS 3.5 A Active 9.14 - - - Nanobody acetylcholine
small molecule iperoxo pubchem
Agonist
small molecule
in meso/LCP 10.1038/NATURE12735 2013-11-27 Yes 4MQS_refined Yes No
M3 receptor Acetylcholine receptors (muscarinic) Class A (Rhodopsin) Rat 4U14 3.6 A Inactive 0.52 - - T4-Lysozyme
- acetylcholine
small molecule Tiotropium pubchem
Antagonist
small molecule
sponge mesophase 10.1016/J.STR.2014.08.022 2014-11-26 No - Yes No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 3VGA 3.1 A Inactive -1.40 - - - - - 139180-30-6 pubchem
Antagonist
small molecule
vapour diffusion 10.1038/NATURE10750 2012-02-01 No - Yes No
β2-adrenoceptor Adrenoceptors Class A (Rhodopsin) Human 4QKX 3.3 A Active 9.44 - - T4-Lysozyme
SignProtMimic_Nanobody (-)-adrenaline
(-)-noradrenaline
small molecule 35V pubchem
Agonist
small molecule
in meso/LCP 10.1073/PNAS.1410415111 2014-07-23 Yes 4QKX_refined Yes No
D4 receptor Dopamine receptors Class A (Rhodopsin) Human 5WIU 2.0 A Inactive -0.97 - - - - - Nemonapride pubchem
Antagonist
small molecule
in meso/LCP 10.1126/SCIENCE.AAN5468 2017-10-18 Yes 5WIU_refined Yes No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 2G87 2.6 A,B Inactive -0.18 - - - - retinal
small molecule retinal gtoplig
Agonist
small molecule
vapour diffusion 10.1002/ANIE.200600595 2006-09-02 No - No No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 3EML 2.6 A Inactive -1.16 - - T4-Lysozyme
- - 139180-30-6 pubchem
Antagonist
small molecule
in meso/LCP 10.1126/SCIENCE.1164772 2008-10-14 No - Yes No
NTS1 receptor Neurotensin receptors Class A (Rhodopsin) Rat 4GRV 2.8 A Intermediate 7.34 - - T4-Lysozyme
- Neurotensin
neurotensin
Peptide CHEMBL342252 pubchem
Agonist
Peptide
in meso/LCP 10.1038/NATURE11558 2012-10-17 Yes 4GRV_refined Yes No
US28 Unclassified Class A (Rhodopsin) strain AD169 4XT3 3.8 A Active 8.85 - - - - CX3CL1
Peptide Fractalkine
Agonist
Peptide
in meso/LCP 10.1126/SCIENCE.AAA5026 2015-03-04 Yes 4XT3_refined Yes No
C5a1 receptor Complement peptide receptors Class A (Rhodopsin) Human 6C1R 2.2 B Inactive -1.37 - - Soluble cytochrome b562
- - PMX53 pubchem chembl_ligand
Avacopan pubchem
Antagonist
Antagonist
Peptide
small molecule
N/A 10.1038/S41594-018-0067-Z 2018-05-30 Yes - Yes No
β2-adrenoceptor Adrenoceptors Class A (Rhodopsin) Human 3D4S 2.8 A Inactive -1.53 - - T4-Lysozyme
- (-)-adrenaline
(-)-noradrenaline
small molecule timolol pubchem
Inverse agonist
small molecule
in meso/LCP 10.1016/J.STR.2008.05.001 2008-06-17 Yes 3D4S_refined Yes No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5K2B 2.5 A Inactive -0.63 - - BRIL
- - 139180-30-6 pubchem
Antagonist
small molecule
in meso/LCP 10.1126/SCIADV.1600292 2016-09-21 Yes 5K2B_refined Yes Yes
Rhodopsin Opsins Class A (Rhodopsin) Human 5W0P 3.0 D Active 8.63 - S-arrestin
Endolysin
- retinal
small molecule N/A N/A N/A in meso/LCP 10.1016/J.CELL.2017.07.002 2017-08-09 Yes - No No
δ receptor Opioid receptors Class A (Rhodopsin) Human 4RWA 3.3 A,B Inactive -1.20 - - BRIL
- β-endorphin
dynorphin A
dynorphin B
endomorphin-1
[Leu]enkephalin
[Met]enkephalin
Peptide DIPP-NH2
Antagonist
peptide-like
in meso/LCP 10.1038/NSMB.2965 2015-01-14 No - Yes No
LPA1 receptor Lysophospholipid (LPA) receptors Class A (Rhodopsin) Human 4Z34 3.0 A Inactive -1.30 - - BRIL
- LPA
Lipid ONO-9780307 pubchem
Antagonist
small molecule
in meso/LCP 10.1016/J.CELL.2015.06.002 2015-06-03 Yes 4Z34_refined Yes No
P2Y1 receptor P2Y receptors Class A (Rhodopsin) Human 4XNV 2.2 A Intermediate 5.58 - - Rubredoxin
- ADP
small molecule BPTU pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE14287 2015-04-01 Yes 4XNV_refined Yes No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 4BEY 2.9 A Active 8.38 Gt
- - - retinal
small molecule N/A N/A N/A vapour diffusion 10.1038/EMBOR.2013.44 2013-05-08 No - No No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 3UZA 3.3 A Inactive -0.56 - - - - - CHEMBL2024115 pubchem
Antagonist
small molecule
vapour diffusion 10.1021/JM201376W 2012-03-21 Yes - Yes No
ETB receptor Endothelin receptors Class A (Rhodopsin) Human 5GLH 2.8 A Inactive -0.17 - - - - - Et 1 pubchem
Agonist
Peptide
in meso/LCP 10.1038/NATURE19319 2016-09-07 Yes 5GLH_refined Yes No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 6GDG 4.1 A Active 10.41 Gs
- TrxA
Nanobody Nb35 - NECA pubchem
Agonist
small molecule
Cryo-EM 10.7554/ELIFE.35946 2018-05-16 Yes 6GDG_refined Yes No
Rhodopsin Opsins Class A (Rhodopsin) Japanese flying squid 2ZIY 3.7 A Inactive -0.28 - - - - retinal
small molecule retinal gtoplig
Inverse agonist
small molecule
vapour diffusion 10.1074/JBC.C800040200 2008-05-06 No - Yes No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 2HPY 2.8 A,B Inactive 0.33 - - - - retinal
small molecule retinal gtoplig
Agonist
small molecule
vapour diffusion 10.1073/PNAS.0601765103 2006-08-22 No - No No
S1P1 receptor Lysophospholipid (S1P) receptors Class A (Rhodopsin) Human 3V2W 3.4 A Inactive -1.48 - - T4-Lysozyme
- sphingosine 1-phosphate
Lipid 909725-61-7 pubchem
Antagonist
small molecule
in meso/LCP 10.1126/SCIENCE.1215904 2012-02-15 No - Yes No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 2J4Y 3.4 A,B Inactive -0.41 - - - - retinal
small molecule retinal gtoplig
Inverse agonist
small molecule
vapour diffusion 10.1016/J.JMB.2007.03.007 2007-09-25 No - No No
FFA1 receptor Free fatty acid receptors Class A (Rhodopsin) Human 4PHU 2.3 A Intermediate 3.58 - - T4-Lysozyme
- long chain carboxylic acids
Lipid TAK-875 pubchem
Agonist
small molecule
in meso/LCP 10.1038/NATURE13494 2014-07-16 Yes 4PHU_refined No No
CCR5 Chemokine receptors Class A (Rhodopsin) Human 4MBS 2.7 A Inactive 0.46 - - Rubredoxin
- CCL11
CCL14
CCL16
CCL2
CCL3
CCL4
CCL5
CCL7
CCL8
Peptide Maraviroc pubchem
Antagonist
small molecule
in meso/LCP 10.1126/SCIENCE.1241475 2013-09-11 Yes 4MBS_refined No No
PAR2 Proteinase-activated receptors Class A (Rhodopsin) Human 5NJ6 4.0 A Intermediate 7.10 - - BRIL
T4-Lysozyme
- - N/A N/A N/A in meso/LCP 10.1038/NATURE22309 2017-05-03 Yes 5NJ6_refined Yes No
Rhodopsin Opsins Class A (Rhodopsin) Human 6CMO 4.5 R Active 9.40 Gi
- Fab
- retinal
small molecule N/A N/A N/A Cryo-EM 2018-06-20 Yes 6CMO_refined No No
LPA1 receptor Lysophospholipid (LPA) receptors Class A (Rhodopsin) Human 4Z36 2.9 A Inactive -1.22 - - BRIL
- LPA
Lipid ONO-3080573 pubchem
Antagonist
small molecule
in meso/LCP 10.1016/J.CELL.2015.06.002 2015-06-03 Yes 4Z36_refined Yes No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5IU4 1.7 A Inactive -0.76 - - BRIL
- - 139180-30-6 pubchem
Antagonist
small molecule
in meso/LCP 10.1021/ACS.JMEDCHEM.6B00653 2016-06-29 Yes 5IU4_refined Yes Yes
β1-adrenoceptor Adrenoceptors Class A (Rhodopsin) Common turkey 2YCY 3.2 A Inactive -1.62 - - - - - (S)-Cyanopindolol pubchem
Antagonist
small molecule
vapour diffusion 10.1073/PNAS.1100185108 2011-06-08 No - Yes No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 1F88 2.8 A,B Inactive -0.50 - - - - retinal
small molecule retinal gtoplig
Inverse agonist
small molecule
vapour diffusion 10.1126/SCIENCE.289.5480.739 2000-08-04 No - No No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5WF5 2.6 A Intermediate 5.91 - - Endolysin
- - UK-432,097 pubchem
Agonist
small molecule
in meso/LCP 10.1016/J.STR.2017.12.013 2018-02-21 Yes 5WF5_refined No No
mGlu5 receptor Metabotropic glutamate receptors Class C (Glutamate) Human 5CGC 3.1 A Inactive 4.25 - - T4-Lysozyme
- L-glutamic acid
small molecule CHEMBL3603915 pubchem
NAM
small molecule
in meso/LCP 10.1021/ACS.JMEDCHEM.5B00892 2015-08-12 Yes - No No
FFA1 receptor Free fatty acid receptors Class A (Rhodopsin) Human 5TZR 2.2 A Intermediate 3.69 - - Endolysin
- long chain carboxylic acids
Lipid UNII-11612L5SPI pubchem
Agonist
small molecule
in meso/LCP 10.1038/NSMB.3417 2017-06-07 Yes - No No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 3QAK 2.7 A Intermediate 6.12 - - T4-Lysozyme
- - UK-432097 pubchem
Agonist
small molecule
in meso/LCP 10.1126/SCIENCE.1202793 2011-03-09 Yes 3QAK_refined Yes No
US28 Unclassified Class A (Rhodopsin) strain AD169 5WB2 3.5 A Active - - - Nanobody 7 Nanobody B1 - CX3CL1
Agonist
Peptide
in meso/LCP 2018-06-13 Yes - Yes No
β2-adrenoceptor Adrenoceptors Class A (Rhodopsin) Human 5D6L 3.2 A Inactive -0.99 - - T4-Lysozyme
- (-)-adrenaline
(-)-noradrenaline
small molecule Carazolol pubchem
Inverse agonist
small molecule
in meso/LCP 10.1038/NPROT.2017.057 2016-08-17 Yes 5D6L_refined Yes No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5OLV 2.0 A Inactive -0.56 - - Soluble cytochrome b562
- - CHEMBL1671936 pubchem chembl_ligand
Antagonist
small molecule
in meso/LCP 10.1038/S41598-017-18570-W 2018-01-17 Yes 5OLV_refined Yes Yes
μ receptor Opioid receptors Class A (Rhodopsin) Mouse 6DDE 3.5 R Intermediate 7.19 Gi
- scFv16
- β-endorphin
dynorphin A
dynorphin B
endomorphin-1
[Leu]enkephalin
[Met]enkephalin
Peptide DAMGO pubchem chembl_ligand
Agonist
peptide-like
Cryo-EM 10.1038/S41586-018-0219-7 2018-06-13 Yes 6DDE_refined Yes No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 3PWH 3.3 A Inactive -0.67 - - - - - 139180-30-6 pubchem
Antagonist
small molecule
vapour diffusion 10.1016/J.STR.2011.06.014 2011-09-07 No - Yes No
mGlu5 receptor Metabotropic glutamate receptors Class C (Glutamate) Human 6FFI 2.2 A Inactive 4.49 - - Endolysin
Endolysin
- L-glutamic acid
small molecule 2-[2-(3-methoxyphenyl)ethynyl]-6-methyl-pyridine pubchem
NAM
small molecule
in meso/LCP 10.1021/ACS.JMEDCHEM.7B01722 2018-03-07 Yes - No No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5NLX 2.1 A Inactive -0.71 - - BRIL
- - N/A N/A N/A in meso/LCP 10.1038/S41467-017-00630-4 2017-09-27 No - Yes No
SMO Frizzled Class F (Frizzled) Human 4JKV 2.5 A Inactive -2.20 - - BRIL
- constitutive
Constitutive LY2940680 pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE12167 2013-04-24 Yes 4JKV_refined No No
AT2 receptor Angiotensin receptors Class A (Rhodopsin) Human 5UNF 2.8 A Active 8.94 - - BRIL
- - CHEMBL289472 pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE22035 2017-04-05 Yes 5UNF_refined Yes No
β2-adrenoceptor Adrenoceptors Class A (Rhodopsin) Human 3P0G 3.5 A Active 9.03 - - T4-Lysozyme
SignProtMimic_Nanobody (-)-adrenaline
(-)-noradrenaline
small molecule BI-167107 pubchem
Agonist
small molecule
in meso/LCP 10.1038/NATURE09648 2011-01-19 Yes 3P0G_refined Yes No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5OM1 2.1 A Inactive -0.69 - - Soluble cytochrome b562
- - 4-(3-amino-5-phenyl-1,2,4-triazin-6-yl)-2-chlorophenol
Antagonist
small molecule
in meso/LCP 10.1038/S41598-017-18570-W 2018-01-17 Yes 5OM1_refined Yes Yes
glucagon receptor Glucagon receptor family Class B1 (Secretin) Human 5XF1 3.2 B Inactive -4.75 - - T4-Lysozyme
mAb1 - 4-{[(4-Cyclohexylphenyl){[3-(Methylsulfonyl)phenyl]carbamoyl}amino]methyl}-N-(1h-Tetrazol-5-Yl)benzamide pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE22363 2017-05-24 Yes 5XF1_refined No No
β1-adrenoceptor Adrenoceptors Class A (Rhodopsin) Common turkey 2Y02 2.6 B Inactive -1.15 - - - - - Carmoterol pubchem
Agonist
small molecule
vapour diffusion 10.1038/NATURE09746 2011-01-12 Yes 2Y02_refined Yes No
β2-adrenoceptor Adrenoceptors Class A (Rhodopsin) Human 5D5B 3.8 A Inactive -1.06 - - T4-Lysozyme
- (-)-adrenaline
(-)-noradrenaline
small molecule Carazolol pubchem
Inverse agonist
small molecule
in meso/LCP 10.1107/S2059798315021683 2016-01-13 No - Yes No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 5WKT 3.2 A Active 7.98 Gt
- - - retinal
small molecule N/A N/A N/A vapour diffusion 10.1038/NPROT.2017.135 2017-12-13 Yes 5WKT_refined No No
C5a1 receptor Complement peptide receptors Class A (Rhodopsin) Human 6C1Q 2.9 B Inactive -1.37 - - Soluble cytochrome b562
- - H94Wrl71FP pubchem
PMX53 pubchem chembl_ligand
Antagonist
Antagonist
small molecule
Peptide
N/A 10.1038/S41594-018-0067-Z 2018-05-30 Yes - Yes No
mGlu5 receptor Metabotropic glutamate receptors Class C (Glutamate) Human 6FFH 2.7 A Inactive 4.08 - - Endolysin
- L-glutamic acid
small molecule Fenobam pubchem
NAM
small molecule
in meso/LCP 10.1021/ACS.JMEDCHEM.7B01722 2018-03-07 Yes - No No
Rhodopsin Opsins Class A (Rhodopsin) Human 5DGY 7.7 A Active 8.61 - S-arrestin
T4-Lysozyme
- retinal
small molecule N/A N/A N/A in meso/LCP 10.1038/SDATA.2016.21 2016-03-23 Yes 5DGY_refined No No
5-HT2B receptor 5-Hydroxytryptamine receptors Class A (Rhodopsin) Human 4NC3 2.8 A Intermediate 3.09 - - BRIL
- 5-hydroxytryptamine
small molecule ERGOTAMINE pubchem
Agonist
small molecule
in meso/LCP 10.1126/SCIENCE.1244142 2013-12-18 Yes 4NC3_refined Yes No
mGlu5 receptor Metabotropic glutamate receptors Class C (Glutamate) Human 5CGD 2.6 A Inactive 4.13 - - T4-Lysozyme
- L-glutamic acid
small molecule CHEMBL3603923 pubchem
NAM
small molecule
in meso/LCP 10.1021/ACS.JMEDCHEM.5B00892 2015-08-12 Yes - No No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5WF6 2.9 A Intermediate 5.83 - - Endolysin
- - UK-432,097 pubchem
Agonist
small molecule
in meso/LCP 10.1016/J.STR.2017.12.013 2018-02-21 Yes 5WF6_refined No No
CXCR4 Chemokine receptors Class A (Rhodopsin) Human 3OE0 2.9 A Inactive -1.45 - - T4-Lysozyme
- CXCL12α
CXCL12β
Peptide CVX15
Antagonist
Peptide
in meso/LCP 10.1126/SCIENCE.1194396 2010-10-27 Yes 3OE0_refined Yes No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5K2A 2.5 A Inactive -0.71 - - BRIL
- - 139180-30-6 pubchem
Antagonist
small molecule
in meso/LCP 10.1126/SCIADV.1600292 2016-09-21 Yes 5K2A_refined Yes Yes
Rhodopsin Opsins Class A (Rhodopsin) Bovine 6FK8 2.9 A Active 7.94 - - - - retinal
small molecule (2~{R},3~{S})-3-azanyl-2-(4-chlorophenyl)-1-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-yl-butan-1-one
Agonist
small molecule
N/A 10.1073/PNAS.1718084115 2018-04-04 Yes 6FK8_refined No No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 2I37 4.2 A Inactive -1.63 - - - - retinal
small molecule retinal gtoplig
Inverse agonist
small molecule
vapour diffusion 10.1073/PNAS.0608022103 2006-10-17 No - No No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5OLG 1.9 A Inactive -0.73 - - Soluble cytochrome b562
- - ZM 241385
Antagonist
small molecule
in meso/LCP 10.1038/S41598-017-18570-W 2018-01-17 Yes 5OLG_refined Yes Yes
PAR2 Proteinase-activated receptors Class A (Rhodopsin) Human 5NDZ 3.6 A Intermediate 6.87 - - BRIL
T4-Lysozyme
- - 2-(6-Bromanyl-1,3-Benzodioxol-5-Yl)-~{n}-(4-Cyanophenyl)-1-[(1~{s})-1-Cyclohexylethyl]benzimidazole-5-Carboxamide pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE22309 2017-05-03 Yes 5NDZ_refined Yes Yes
CXCR4 Chemokine receptors Class A (Rhodopsin) Human 3OE8 3.1 A Inactive -1.28 - - T4-Lysozyme
- CXCL12α
CXCL12β
Peptide IT1t pubchem
Antagonist
small molecule
in meso/LCP 10.1126/SCIENCE.1194396 2010-10-27 No - Yes No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 4X1H 2.3 A Active 8.24 Gt
- - - retinal
small molecule 69984-73-2 pubchem
Inverse agonist
N/A
vapour diffusion 10.1016/J.STR.2015.09.015 2015-11-04 No - No No
NTS1 receptor Neurotensin receptors Class A (Rhodopsin) Rat 4BWB 3.6 A Inactive 1.53 - - - - Neurotensin
neurotensin
Peptide CHEMBL342252 pubchem
Agonist
Peptide
vapour diffusion 10.1073/PNAS.1317903111 2014-01-29 No - Yes No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 6FKB 3.0 A Active 7.93 - - - - retinal
small molecule 2-(4-chlorophenyl)-1-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-yl-ethanone
Agonist
small molecule
N/A 10.1073/PNAS.1718084115 2018-04-04 Yes - No No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 5TE5 4.0 A Inactive -0.47 - - - - retinal
small molecule 10,20-Methanoretinal pubchem
Agonist
small molecule
vapour diffusion 10.1073/PNAS.1617446114 2017-03-15 Yes 5TE5_refined No No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 6FKA 2.7 A Active 7.99 - - - - retinal
small molecule (2~{S})-2-(3,4-dichlorophenyl)-3-methyl-1-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-yl-butan-1-one
Agonist
small molecule
N/A 10.1073/PNAS.1718084115 2018-04-04 Yes 6FKA_refined No No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 2X72 3.0 A Active 8.34 Gt
- - - retinal
small molecule retinal gtoplig
Agonist
small molecule
vapour diffusion 10.1038/NATURE09795 2011-03-16 Yes 2X72_refined No No
β1-adrenoceptor Adrenoceptors Class A (Rhodopsin) Common turkey 2YCW 3.0 A Inactive -1.08 - - - - - timolol pubchem
Inverse agonist
small molecule
vapour diffusion 10.1073/PNAS.1100185108 2011-06-01 Yes 2YCW_refined Yes No
β1-adrenoceptor Adrenoceptors Class A (Rhodopsin) Common turkey 4BVN 2.1 A Inactive -2.09 - - - - - (S)-Cyanopindolol pubchem
Antagonist
small molecule
in meso/LCP 10.1371/JOURNAL.PONE.0092727 2014-04-02 Yes 4BVN_refined Yes Yes
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5UVI 3.2 A Inactive -0.58 - - BRIL
- - 139180-30-6 pubchem
Antagonist
small molecule
in meso/LCP 10.1107/S205225251700570X 2017-05-24 Yes 5UVI_refined Yes No
ETB receptor Endothelin receptors Class A (Rhodopsin) Human 5XPR 3.6 A Inactive 0.09 - - - - - N/A N/A N/A in meso/LCP 10.1038/NSMB.3450 2017-08-16 Yes 5XPR_refined Yes No
β1-adrenoceptor Adrenoceptors Class A (Rhodopsin) Common turkey 3ZPR 2.7 B Inactive -1.11 - - - - - 4-Methyl-2-piperazin-1-yl-quinoline pubchem
Antagonist
small molecule
vapour diffusion 10.1021/JM400140Q 2013-04-03 Yes 3ZPR_refined Yes Yes
A1 receptor Adenosine receptors Class A (Rhodopsin) Human 5N2S 3.3 A Inactive -0.47 - - - - - PSB36 pubchem
Agonist
small molecule
in meso/LCP 10.1016/J.STR.2017.06.012 2017-07-26 Yes - Yes No
5-HT2B receptor 5-Hydroxytryptamine receptors Class A (Rhodopsin) Human 5TVN 2.9 A Intermediate 4.46 - - BRIL
- 5-hydroxytryptamine
small molecule Lysergide pubchem
Agonist
small molecule
in meso/LCP 10.1016/J.CELL.2016.12.033 2017-02-01 Yes 5TVN_refined Yes No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5UIG 3.5 A Inactive 1.11 - - BRIL
- - J3.651.884G pubchem
Antagonist
small molecule
vapour diffusion 10.1073/PNAS.1621423114 2017-02-08 Yes 5UIG_refined Yes No
NOP receptor Opioid receptors Class A (Rhodopsin) Human 4EA3 3.0 A Inactive -1.21 - - BRIL
- nociceptin/orphanin FQ
Peptide C-24 pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE11085 2012-04-25 Yes 4EA3_refined Yes No
GLP-1 receptor Glucagon receptor family Class B1 (Secretin) Human 5VEX 3.0 B Inactive -5.05 - - Endolysin
- - 4-{[(4-Cyclohexylphenyl){[3-(Methylsulfonyl)phenyl]carbamoyl}amino]methyl}-N-(1h-Tetrazol-5-Yl)benzamide pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE22378 2017-05-17 Yes 5VEX_refined No No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 6FKD 2.5 A Active 7.92 - - - - retinal
small molecule 5-chloranyl-2-(2-oxidanylidene-2-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-yl-ethyl)-3~{H}-pyridin-6-one
Agonist
small molecule
N/A 10.1073/PNAS.1718084115 2018-04-04 Yes 6FKD_refined No No
glucagon receptor Glucagon receptor family Class B1 (Secretin) Human 5EE7 2.5 A Inactive -4.80 - - BRIL
- - 3,6,9,12,15,18,21,24-OCTAOXAHEXACOSAN-1-OL pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE17414 2016-04-20 Yes 5EE7_refined No No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 3RFM 3.6 A Inactive -0.48 - - - - - caffeine pubchem
Antagonist
small molecule
vapour diffusion 10.1016/J.STR.2011.06.014 2011-09-07 Yes - Yes No
β2-adrenoceptor Adrenoceptors Class A (Rhodopsin) Human 5X7D 2.7 A Inactive -1.08 - - T4-Lysozyme
- (-)-adrenaline
(-)-noradrenaline
small molecule Carazolol pubchem
4-carbamoyl-N-[(2R)-2-cyclohexyl-2-phenylacetyl]-L-phenylalanyl-3-bromo-N-methyl-L-phenylalaninamide pubchem
Antagonist
Antagonist
small molecule
small molecule
in meso/LCP 10.1038/NATURE23652 2017-08-16 Yes 5X7D_refined Yes No
SMO Frizzled Class F (Frizzled) Human 5V57 3.0 A Inactive -1.67 - - Flavodoxin
- constitutive
Constitutive N-methyl-N-[1-[4-(2-methylpyrazol-3-yl)phthalazin-1-yl]piperidin-4-yl]-4-nitro-2-(trifluoromethyl)benzamide pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NCOMMS15383 2017-05-24 Yes 5V57_refined No No
β2-adrenoceptor Adrenoceptors Class A (Rhodopsin) Human 3KJ6 3.4 A Inactive -2.18 - - - Antibody (-)-adrenaline
(-)-noradrenaline
small molecule N/A N/A N/A vapour diffusion 10.1038/NATURE08650 2010-02-16 No - Yes No
β2-adrenoceptor Adrenoceptors Class A (Rhodopsin) Human 4LDL 3.1 A Active 9.26 - - T4-Lysozyme
Nanobody (-)-adrenaline
(-)-noradrenaline
small molecule hydroxybenzylisoproterenol pubchem
Agonist
small molecule
in meso/LCP 10.1038/NATURE12572 2013-09-25 Yes 4LDL_refined Yes No
FFA1 receptor Free fatty acid receptors Class A (Rhodopsin) Human 5KW2 2.8 A Intermediate 4.17 - - T4-Lysozyme
- long chain carboxylic acids
Lipid (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
Antagonist
small molecule
N/A 10.1038/S41467-017-01240-W 2018-05-02 Yes - No No
NOP receptor Opioid receptors Class A (Rhodopsin) Human 5DHH 3.0 A Inactive -1.11 - - BRIL
- nociceptin/orphanin FQ
Peptide N/A N/A N/A in meso/LCP 10.1016/J.STR.2015.07.024 2015-10-21 Yes 5DHH_refined Yes No
5-HT1B receptor 5-Hydroxytryptamine receptors Class A (Rhodopsin) Human 5V54 3.9 A Intermediate 3.69 - - Soluble cytochrome b562
- - CHEMBL428892 pubchem chembl_ligand
Antagonist
small molecule
in meso/LCP 2018-02-07 Yes 5V54_refined Yes No
AT2 receptor Angiotensin receptors Class A (Rhodopsin) Human 5UNH 2.9 B Active 9.17 - - BRIL
- - 8EM pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE22035 2017-04-05 Yes 5UNH_refined Yes No
Rhodopsin Opsins Class A (Rhodopsin) Japanese flying squid 3AYN 2.7 A,B Inactive -0.22 - - - - retinal
small molecule retinal gtoplig
Inverse agonist
small molecule
vapour diffusion 10.1016/J.JMB.2011.08.044 2011-08-17 No - Yes No
M3 receptor Acetylcholine receptors (muscarinic) Class A (Rhodopsin) Rat 4DAJ 3.4 A Inactive 0.22 - - T4-Lysozyme
- acetylcholine
small molecule Tiotropium pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NATURE10867 2012-02-22 No - Yes No
β1-adrenoceptor Adrenoceptors Class A (Rhodopsin) Common turkey 2YCZ 3.7 B Inactive -1.72 - - - - - timolol pubchem
Antagonist
small molecule
vapour diffusion 10.1073/PNAS.1100185108 2011-06-01 Yes - Yes No
β1-adrenoceptor Adrenoceptors Class A (Rhodopsin) Common turkey 2Y01 2.6 A Inactive -1.07 - - - - - Dobutamine pubchem
Agonist (partial)
small molecule
vapour diffusion 10.1038/NATURE09746 2011-03-30 No - Yes No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 4A4M 3.3 A Active 8.20 Gt-alpha3
- - - retinal
small molecule retinal gtoplig
Agonist
small molecule
vapour diffusion 10.1073/PNAS.1114089108 2012-01-25 Yes 4A4M_refined No No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 3C9M 3.4 A Inactive -0.20 - - - - retinal
small molecule retinal gtoplig
Inverse agonist
small molecule
NA 10.1107/S0907444908017162 2008-08-05 No - No No
CXCR4 Chemokine receptors Class A (Rhodopsin) Human 3OE6 3.2 A Inactive -1.33 - - T4-Lysozyme
- CXCL12α
CXCL12β
Peptide IT1t pubchem
Antagonist
small molecule
in meso/LCP 10.1126/SCIENCE.1194396 2010-10-27 No - Yes No
β1-adrenoceptor Adrenoceptors Class A (Rhodopsin) Common turkey 4GPO 3.5 A,B Inactive -1.36 - - - - - N/A N/A N/A vapour diffusion 10.1038/NSMB.2504 2013-02-27 Yes 4GPO_refined Yes No
β2-adrenoceptor Adrenoceptors Class A (Rhodopsin) Human 2R4S 3.4 A Inactive -2.89 - - - Antibody (-)-adrenaline
(-)-noradrenaline
small molecule N/A N/A N/A vapour diffusion 10.1038/NATURE06325 2007-11-06 No - Yes No
β2-adrenoceptor Adrenoceptors Class A (Rhodopsin) Human 3NY9 2.8 A Inactive -1.49 - - T4-Lysozyme
- (-)-adrenaline
(-)-noradrenaline
small molecule CHEMBL1233771 pubchem
Inverse agonist
small molecule
in meso/LCP 10.1021/JA105108Q 2010-08-11 Yes - Yes No
β2-adrenoceptor Adrenoceptors Class A (Rhodopsin) Human 4GBR 4.0 A Inactive -0.55 - - T4-Lysozyme
- (-)-adrenaline
(-)-noradrenaline
small molecule timolol pubchem
Inverse agonist (partial)
small molecule
in meso/LCP 10.1371/JOURNAL.PONE.0046039 2012-10-24 No - Yes No
NTS1 receptor Neurotensin receptors Class A (Rhodopsin) Rat 4XEE 2.9 A Intermediate 6.49 - - T4-Lysozyme
- Neurotensin
neurotensin
Peptide CHEMBL342252 pubchem
Agonist
Peptide
in meso/LCP 10.1038/NCOMMS8895 2015-07-29 Yes 4XEE_refined Yes No
β1-adrenoceptor Adrenoceptors Class A (Rhodopsin) Common turkey 3ZPQ 2.8 B Inactive -1.18 - - - - - 4-(1-Piperazinyl)-1H-indole pubchem
Antagonist
small molecule
vapour diffusion 10.1021/JM400140Q 2013-04-03 Yes 3ZPQ_refined Yes Yes
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5NM2 2.0 A Inactive -0.83 - - BRIL
- - 139180-30-6 pubchem
Antagonist
small molecule
in meso/LCP 10.1038/S41467-017-00630-4 2017-09-27 Yes 5NM2_refined Yes Yes
SMO Frizzled Class F (Frizzled) Human 4QIM 2.6 A Inactive -2.23 - - BRIL
- constitutive
Constitutive AntaXV pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NCOMMS5355 2014-07-23 Yes 4QIM_refined No No
ETB receptor Endothelin receptors Class A (Rhodopsin) Human 5GLI 2.5 A Inactive -0.38 - - Endolysin
- - N/A N/A N/A in meso/LCP 10.1038/NATURE19319 2016-09-07 Yes 5GLI_refined Yes No
SMO Frizzled Class F (Frizzled) Human 4QIN 2.6 A Inactive -2.38 - - BRIL
- constitutive
Constitutive SAG1.5
Agonist
small molecule
in meso/LCP 10.1038/NCOMMS5355 2014-07-23 Yes 4QIN_refined No No
CB1 receptor Cannabinoid receptors Class A (Rhodopsin) Human 5U09 2.6 A Inactive -2.87 - - Glycogen synthase
- 2-arachidonoylglycerol
Endocannabinoid Taranabant pubchem
Inverse agonist
small molecule
in meso/LCP 10.1038/NATURE20613 2016-12-07 Yes 5U09_refined Yes No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 3PXO 3.0 A Active 7.94 - - - - retinal
small molecule retinal gtoplig
Agonist
small molecule
vapour diffusion 10.1038/NATURE09789 2011-03-09 No - No No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 3C9L 2.7 A Inactive 0.09 - - - - retinal
small molecule retinal gtoplig
Inverse agonist
small molecule
NA 10.1107/S0907444908017162 2008-08-05 No - No No
OX1 receptor Orexin receptors Class A (Rhodopsin) Human 4ZJC 2.8 A Inactive -0.54 - - - - noradrenaline
small molecule retinal gtoplig
Inverse agonist
small molecule
in meso/LCP 10.1038/NSMB.3183 2016-03-09 Yes 4ZJC_refined No No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 6FK9 2.6 A Active 7.83 - - - - retinal
small molecule (2~{S})-3-methyl-2-phenyl-1-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-yl-butan-1-one
Agonist
small molecule
N/A 10.1073/PNAS.1718084115 2018-04-04 Yes 6FK9_refined No No
SMO Frizzled Class F (Frizzled) Human 4N4W 2.8 A Inactive -1.76 - - BRIL
- constitutive
Constitutive SANT-1 pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NCOMMS5355 2014-01-22 Yes - No No
OX2 receptor Orexin receptors Class A (Rhodopsin) Human 4S0V 2.5 A Inactive -1.02 - - PGS
- - Suvorexant pubchem
Antagonist
N/A
in meso/LCP 10.1038/NATURE14035 2015-01-14 Yes 4S0V_refined Yes No
NTS1 receptor Neurotensin receptors Class A (Rhodopsin) Rat 4BV0 3.1 A Inactive 0.95 - - - - Neurotensin
neurotensin
Peptide CHEMBL342252 pubchem
Agonist
Peptide
vapour diffusion 10.1073/PNAS.1317903111 2014-01-29 No - Yes No
5-HT1B receptor 5-Hydroxytryptamine receptors Class A (Rhodopsin) Human 4IAR 2.7 A Intermediate 4.22 - - BRIL
- - ERGOTAMINE pubchem
Agonist
small molecule
in meso/LCP 10.1126/SCIENCE.1232807 2013-03-13 Yes 4IAR_refined Yes No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 2I36 4.1 A,B,C Inactive -0.36 - - - - retinal
small molecule retinal gtoplig
Inverse agonist
small molecule
vapour diffusion 10.1073/PNAS.0608022103 2006-10-17 No - No No
M3 receptor Acetylcholine receptors (muscarinic) Class A (Rhodopsin) Rat 4U16 3.7 B Inactive 0.20 - - T4-Lysozyme
- acetylcholine
small molecule methscopolamine pubchem
Antagonist
small molecule
sponge mesophase 10.1016/J.STR.2014.08.022 2014-11-26 Yes 4U16_refined Yes No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 6FKC 2.5 A Active 7.84 - - - - retinal
small molecule 3-[1'-[(2~{S})-2-(4-chlorophenyl)-3-methyl-butanoyl]spiro[1,3-benzodioxole-2,4'-piperidine]-5-yl]propanoic acid
Agonist
small molecule
N/A 10.1073/PNAS.1718084115 2018-04-04 Yes 6FKC_refined No No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 5EN0 2.8 A Active 8.40 Gt-alpha3
- - - retinal
small molecule retinal gtoplig
Inverse agonist
small molecule
vapour diffusion 10.15252/EMBR.201642671 2016-08-10 Yes 5EN0_refined No No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 4UG2 2.6 A,B Intermediate 5.86 - - - - - Cgs 21680 pubchem
Agonist
small molecule
in meso/LCP 10.1124/MOL.114.097360 2015-04-08 No - Yes No
SMO Frizzled Class F (Frizzled) Human 4O9R 3.2 A Inactive -2.77 - - BRIL
- constitutive
Constitutive Cyclopamine pubchem
Antagonist
small molecule
in meso/LCP 10.1038/NCOMMS4309 2014-03-05 Yes 4O9R_refined No No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 3DQB 3.2 A Active 8.59 Gt
- - - retinal
small molecule N/A N/A N/A vapour diffusion 10.1038/NATURE07330 2008-09-23 Yes 3DQB_refined No No
AT1 receptor Angiotensin receptors Class A (Rhodopsin) Human 4YAY 2.9 A Inactive -1.10 - - BRIL
- - ZD7155 pubchem
Antagonist
small molecule
in meso/LCP 10.1016/J.CELL.2015.04.011 2015-04-22 Yes 4YAY_refined Yes No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5OLZ 1.9 A Inactive -0.75 - - Soluble cytochrome b562
- - 4-(3-amino-5-phenyl-1,2,4-triazin-6-yl)-2-chlorophenol
Antagonist
small molecule
in meso/LCP 10.1038/S41598-017-18570-W 2018-01-17 Yes 5OLZ_refined Yes Yes
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5NM4 1.7 A Inactive -0.80 - - BRIL
- - 139180-30-6 pubchem
Antagonist
small molecule
in meso/LCP 10.1038/S41467-017-00630-4 2017-09-27 No - Yes No
P2Y12 receptor P2Y receptors Class A (Rhodopsin) Human 4PXZ 2.5 A Intermediate 3.91 - - BRIL
- - 2-MeSADP pubchem
Agonist
small molecule
in meso/LCP 10.1038/NATURE13288 2014-04-30 Yes 4PXZ_refined Yes No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 1U19 2.2 A Inactive -0.23 - - - - retinal
small molecule retinal gtoplig
Inverse agonist
small molecule
vapour diffusion 10.1016/J.JMB.2004.07.044 2004-10-12 Yes 1U19_refined No No
SMO Frizzled Class F (Frizzled) African clawed frog 6D35 3.9 A Inactive -2.20 - - Cytochrome b562
- constitutive
Constitutive N/A N/A N/A N/A 10.1016/J.CELL.2018.04.029 2018-05-23 Yes 6D35_refined No No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5OM4 2.0 A Inactive -0.66 - - Soluble cytochrome b562
- - 4-(3-amino-5-phenyl-1,2,4-triazin-6-yl)-2-chlorophenol
Antagonist
small molecule
in meso/LCP 10.1038/S41598-017-18570-W 2018-01-17 Yes 5OM4_refined Yes Yes
Y1 receptor Neuropeptide Y receptors Class A (Rhodopsin) Human 5ZBQ 2.7 A Inactive -1.31 - - T4-Lysozyme
- - UR-MK299 pubchem
Antagonist
small molecule
N/A 10.1038/S41586-018-0046-X 2018-04-25 Yes 5ZBQ_refined Yes No
β1-adrenoceptor Adrenoceptors Class A (Rhodopsin) Common turkey 5A8E 2.4 A Inactive -2.23 - - - - - 7-methylcyanopindolol
Inverse agonist
small molecule
in meso/LCP 10.1124/MOL.115.101030 2015-09-30 Yes 5A8E_refined Yes Yes
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5K2D 1.9 A Inactive -0.71 - - BRIL
- - 139180-30-6 pubchem
Antagonist
small molecule
in meso/LCP 10.1126/SCIADV.1600292 2016-09-21 Yes 5K2D_refined Yes Yes
β2-adrenoceptor Adrenoceptors Class A (Rhodopsin) Human 4LDO 3.2 A Active 9.16 - - T4-Lysozyme
Nanobody (-)-adrenaline
(-)-noradrenaline
small molecule epinephrine pubchem
Agonist
small molecule
in meso/LCP 10.1038/NATURE12572 2013-09-25 Yes 4LDO_refined Yes No
CXCR4 Chemokine receptors Class A (Rhodopsin) Human 4RWS 3.1 A Inactive -0.91 - - T4-Lysozyme
- CXCL12α
CXCL12β
Peptide vMIP-II
Antagonist
Peptide
in meso/LCP 10.1126/SCIENCE.1261064 2015-02-11 Yes 4RWS_refined Yes No
Rhodopsin Opsins Class A (Rhodopsin) Bovine 3CAP 2.9 A Active 7.91 - - - - retinal
small molecule N/A N/A N/A vapour diffusion 10.1038/NATURE07063 2008-06-24 No - No No
A2A receptor Adenosine receptors Class A (Rhodopsin) Human 5IU7 1.9 A Inactive -0.68 - - BRIL
- - 2-(Furan-2-Yl)-N~5~-[2-(4-Phenylpiperidin-1-Yl)ethyl][1,2,4]triazolo[1,5-A][1,3,5]triazine-5,7-Diamine pubchem
Agonist
small molecule
in meso/LCP 10.1021/ACS.JMEDCHEM.6B00653 2016-06-29 Yes 5IU7_refined Yes Yes
SMO Frizzled Class F (Frizzled) African clawed frog 6D32 3.8 A Inactive -2.20 - - Cytochrome b562
- constitutive
Constitutive Cyclopamine pubchem
Antagonist
small molecule
N/A 10.1016/J.CELL.2018.04.029 2018-05-23 Yes - No No