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RECEPTOR
STRUCTURE
SIGNALING PROTEIN
AUXILIARY PROTEIN
LIGAND
SODIUM ION SITE
REFERENCE
ANNOTATED
PDB code Refined structure Resolution Δ distance (Å) PDB Date
GLP1R GLP-1 Glucagon Class B1 (Secretin) Human 5NX2 - 3.7 A Intermediate 4.86 - - - - - truncated protein ag...
Agonist
 peptide
 vapour diffusion No No Marshall FH 10.1038/NATURE22800 2017-06-14 Yes
CNR1 CB1 Cannabinoid Class A (Rhodopsin) Human 5XR8 - 3.0 A Active 7.90 - - Flavodoxin - 2-arachidonoylglycerol
 Endocannabinoid 8D0
Agonist
 small molecule
 in meso/LCP Yes No Liu Z 10.1038/NATURE23272 2017-07-12 Yes
CNR1 CB1 Cannabinoid Class A (Rhodopsin) Human 5XRA - 2.8 A Active 7.95 - - Flavodoxin - 2-arachidonoylglycerol
 Endocannabinoid CHEMBL1683648 pubchem
Agonist
 small molecule
 in meso/LCP Yes No Liu Z 10.1038/NATURE23272 2017-07-12 Yes
PAR1 PAR1 Proteinase-activated Class A (Rhodopsin) Human 3VW7 - 2.2 A Intermediate 6.18 - - T4-Lysozyme - thrombin
 peptide Vorapaxar pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Kobilka BK 10.1038/NATURE11701 2012-12-12 Yes
OPRD δ Opioid 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 Yes Yes Stevens RC 10.1038/NATURE12944 2013-12-25 Yes
ACM1 M1 Acetylcholine (muscarinic) Class A (Rhodopsin) Human 5CXV - 2.7 A Inactive 0.64 - - Endolysin - acetylcholine
 small molecule CHEMBL258622 pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Christopoulos A 10.1038/NATURE17188 2016-03-09 Yes
ACM4 M4 Acetylcholine (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 Yes No Christopoulos A 10.1038/NATURE17188 2016-03-16 Yes
CNR1 CB1 Cannabinoid Class A (Rhodopsin) Human 5TGZ - 2.8 A Inactive -0.85 - - Flavodoxin - 2-arachidonoylglycerol
 Endocannabinoid SCHEMBL662960 pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Liu Z 10.1016/J.CELL.2016.10.004 2016-11-02 Yes
EDNRB ETB Endothelin Class A (Rhodopsin) Human 5XPR - 3.6 A Inactive 0.09 - - - - - N/A N/A N/A in meso/LCP Yes No Nureki O 10.1038/NSMB.3450 2017-08-16 Yes
EDNRB ETB Endothelin Class A (Rhodopsin) Human 5X93 - 2.2 A Inactive -0.68 - - Endolysin - - K-8794 pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Nureki O 10.1038/NSMB.3450 2017-08-16 Yes
OX2R OX2 Orexin Class A (Rhodopsin) Human 5WQC - 2.0 A Inactive -0.99 - - Glycogen synthase - - EMPA pubchem chembl_ligand
Antagonist
 small molecule
 in meso/LCP Yes No Kobayashi T 10.1016/J.STR.2017.11.005 2017-11-29 Yes
OX2R OX2 Orexin Class A (Rhodopsin) Human 5WS3 - 2.3 A Inactive -1.13 - - Glycogen synthase - - EMPA pubchem chembl_ligand
Antagonist
 small molecule
 in meso/LCP Yes No Kobayashi T 10.1016/J.STR.2017.11.005 2017-12-13 Yes
CALRL calcitonin-like Calcitonin Class B1 (Secretin) Human 6E3Y - 3.3 R Active 6.86 Gs - RAMP1 Nanobody 35 - Calcitonin gene-rela... pubchem
Agonist
 peptide
 N/A No No Sexton PM 10.1038/S41586-018-0535-Y 2018-09-19 Yes
Q80KM9 US28 Unclassified Class A (Rhodopsin) strain AD169 5WB1 - 3.5 A Active - - - Nanobody - N/A N/A N/A in meso/LCP Yes No Garcia KC 10.7554/ELIFE.35850 2018-06-13 Yes
ADRB2 β2 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 No No Lefkowitz RJ 10.1038/NATURE18636 2016-07-13 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 5G53 - 3.4 A Active 9.79 Engineered G protein - - - - NECA pubchem
Agonist
 small molecule
 vapour diffusion Yes No Tate CG 10.1038/NATURE18966 2016-08-03 Yes
SMO 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 No No Siebold C 10.1038/NATURE18934 2016-07-20 Yes
SMO SMO Frizzled Class F (Frizzled) Human 5L7I - 3.3 B Inactive -2.33 - - BRIL - constitutive
 Constitutive Vismodegib pubchem
Antagonist
 small molecule
 in meso/LCP No No Siebold C 10.1038/NATURE18934 2016-07-20 Yes
ADRB2 β2 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 Yes No Kobilka BK 10.1038/NATURE10361 2011-07-20 Yes
NTR1 NTS1 Neurotensin Class A (Rhodopsin) Rat 5T04 - 3.3 A Active 8.26 - - T4-Lysozyme - Neurotensin
neurotensin
 peptide CHEMBL342252 pubchem
Agonist
 peptide
 in meso/LCP Yes No Grisshammer R 10.1038/SREP38564 2016-12-21 Yes
P2RY1 P2Y1 P2Y Class A (Rhodopsin) Human 4XNV - 2.2 A Intermediate 5.58 - - Rubredoxin - ADP
 small molecule BPTU pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Wu B 10.1038/NATURE14287 2015-04-01 Yes
P2RY1 P2Y1 P2Y Class A (Rhodopsin) Human 4XNW - 2.7 A Intermediate 5.20 - - Rubredoxin - ADP
 small molecule MRS2500 pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Wu B 10.1038/NATURE14287 2015-04-01 Yes
5HT1B 5-HT1B 5-Hydroxytryptamine Class A (Rhodopsin) Human 6G79 - 3.8 S Active 8.90 Go - - - - Donitriptan pubchem
Agonist
 small molecule
 Cryo-EM Yes No Tate CG 10.1038/S41586-018-0241-9 2018-06-20 Yes
Q9WTK1 BLT1 Leukotriene Class A (Rhodopsin) Guinea pig 5X33 - 3.7 A Inactive -1.53 - - Endolysin - - BIIL-260 pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Yokoyama S 10.1038/NCHEMBIO.2547 2018-01-03 Yes
GRM5 mGlu5 Metabotropic glutamate 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 No No Marshall FH 10.1038/NATURE13396 2014-07-02 Yes
OPRM μ Opioid 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 Yes No Kobilka BK 10.1038/NATURE14886 2015-08-05 Yes
Q08BG4 LPA6 Lysophospholipid (LPA) Class A (Rhodopsin) Zebrafish 5XSZ - 3.2 A Active 9.96 - - Endolysin - - N/A N/A N/A in meso/LCP Yes No Nureki O 10.1038/NATURE23448 2017-08-16 Yes
ACM2 M2 Acetylcholine (muscarinic) Class A (Rhodopsin) Human 4MQS - 3.5 A Active 9.14 - - - Nanobody acetylcholine
 small molecule iperoxo pubchem
Agonist
 small molecule
 in meso/LCP Yes No Kobilka BK 10.1038/NATURE12735 2013-11-27 Yes
ACM2 M2 Acetylcholine (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 Yes No Kobilka BK 10.1038/NATURE12735 2013-11-27 Yes
5HT2C 5-HT2C 5-Hydroxytryptamine Class A (Rhodopsin) Human 6BQG - 3.0 A Active 7.92 - - Soluble cytochrome b562 - - Ergotamine pubchem
Agonist
 small molecule
 in meso/LCP Yes No Liu Z 10.1016/J.CELL.2018.01.001 2018-02-14 Yes
5HT2C 5-HT2C 5-Hydroxytryptamine Class A (Rhodopsin) Human 6BQH - 2.7 A Inactive 0.08 - - Soluble cytochrome b562 - - Ritanserin pubchem
Inverse agonist
 small molecule
 in meso/LCP Yes No Liu Z 10.1016/J.CELL.2018.01.001 2018-02-14 Yes
FFAR1 FFA1 Free fatty acid 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 No No Soisson SM 10.1038/NSMB.3417 2017-06-07 Yes
FFAR1 FFA1 Free fatty acid Class A (Rhodopsin) Human 5TZY - 3.2 A Intermediate 3.21 - - Endolysin - long chain carboxylic acids
 Lipid (2s,3r)-3-Cyclopropy... pubchem
UNII-11612L5SPI pubchem
Agonist
Agonist
 small molecule
small molecule
 in meso/LCP No No Soisson SM 10.1038/NSMB.3417 2017-06-07 Yes
NPY1R Y1 Neuropeptide Y Class A (Rhodopsin) Human 5ZBQ - 2.7 A Inactive -1.31 - - T4-Lysozyme - - UR-MK299 pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Wu B 10.1038/S41586-018-0046-X 2018-04-25 Yes
NPY1R Y1 Neuropeptide Y Class A (Rhodopsin) Human 5ZBH - 3.0 A Inactive -0.68 - - T4-Lysozyme - - BMS-193885 pubchem
Antagonist
 small molecule
 N/A Yes No Wu B 10.1038/S41586-018-0046-X 2018-04-25 Yes
NK1R NK1 Tachykinin Class A (Rhodopsin) Human 6HLL - 3.3 A Inactive 1.05 - - GIgA glycogen synthase - - CP-99,994 pubchem chembl_ligand
Antagonist
 small molecule
 N/A Yes No Plückthun A 10.1038/S41467-018-07939-8 2019-01-16 Yes
NK1R NK1 Tachykinin Class A (Rhodopsin) Human 6HLO - 2.4 A Inactive 0.68 - - GIgA glycogen synthase - - Aprepitant pubchem chembl_ligand
Antagonist
 small molecule
 N/A Yes No Plückthun A 10.1038/S41467-018-07939-8 2019-01-16 Yes
NK1R NK1 Tachykinin Class A (Rhodopsin) Human 6HLP - 2.2 A Inactive 0.80 - - GIgA glycogen synthase - - Netupitant pubchem chembl_ligand
Antagonist
 small molecule
 N/A Yes No Plückthun A 10.1038/S41467-018-07939-8 2019-01-16 Yes
DRD2 D2 Dopamine Class A (Rhodopsin) Human 6CM4 - 2.9 A Inactive -1.80 - - Endolysin - - Risperidone pubchem chembl_ligand
Inverse agonist
 small molecule
 in meso/LCP Yes No Roth BL 10.1038/NATURE25758 2018-03-14 Yes
AGTR2 AT2 Angiotensin Class A (Rhodopsin) Human 5UNG - 2.8 B Active 8.46 - - BRIL - - CHEMBL289472 pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Cherezov V 10.1038/NATURE22035 2017-04-05 Yes
AGTR2 AT2 Angiotensin Class A (Rhodopsin) Human 5UNH - 2.9 B Active 9.17 - - BRIL - - 8EM pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Cherezov V 10.1038/NATURE22035 2017-04-05 Yes
AGTR2 AT2 Angiotensin Class A (Rhodopsin) Human 5UNF - 2.8 A Active 8.94 - - BRIL - - CHEMBL289472 pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Cherezov V 10.1038/NATURE22035 2017-04-05 Yes
TA2R TP Prostanoid Class A (Rhodopsin) Human 6IIU - 2.5 A Inactive 1.01 - - Soluble cytochrome b562
Rubredoxin 		- - Ramatroban pubchem chembl_ligand
Antagonist
 small molecule
 N/A No No Wu B 10.1038/S41589-018-0170-9 2018-12-19 Yes
TA2R TP Prostanoid Class A (Rhodopsin) Human 6IIV - 3.0 A Inactive 1.00 - - Soluble cytochrome b562
Rubredoxin 		- - Daltroban pubchem chembl_ligand
Antagonist
 small molecule
 N/A No No Wu B 10.1038/S41589-018-0170-9 2018-12-19 Yes
OPRK κ Opioid Class A (Rhodopsin) Human 4DJH - 2.9 A Inactive -1.29 - - T4-Lysozyme - dynorphin A
 peptide JDTic pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Stevens RC 10.1038/NATURE10939 2012-03-21 Yes
PTAFR PAF Platelet-activating factor Class A (Rhodopsin) Human 5ZKP - 2.8 A Active 15.31 - - Flavodoxin - - Foropafant pubchem
Antagonist
 small molecule
 N/A Yes No Wu B 10.1038/S41594-018-0068-Y 2018-06-20 Yes
PTAFR PAF Platelet-activating factor Class A (Rhodopsin) Human 5ZKQ - 2.9 B Intermediate 4.76 - - Endolysin - - ABT-491 pubchem chembl_ligand
Inverse agonist
 small molecule
 N/A Yes No Wu B 10.1038/S41594-018-0068-Y 2018-06-20 Yes
HRH1 H1 Histamine Class A (Rhodopsin) Human 3RZE - 3.1 A Inactive 0.45 - - T4-Lysozyme - histamine
 small molecule doxepin pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Iwata S 10.1038/NATURE10236 2011-06-15 Yes
OPRX NOP Opioid 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 Yes No Stevens RC 10.1016/J.STR.2015.07.024 2015-10-21 Yes
OPRX NOP Opioid 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 Yes No Stevens RC 10.1016/J.STR.2015.07.024 2015-10-21 Yes
ACM2 M2 Acetylcholine (muscarinic) Class A (Rhodopsin) Human 5YC8 - 2.5 A Inactive 1.05 - - Redesigned apo-cytochrome b562 - acetylcholine
 small molecule N-methyl scopolamine pubchem
Antagonist
 small molecule
 N/A No No Kobayashi T 10.1038/S41589-018-0152-Y 2018-11-21 Yes
ACM2 M2 Acetylcholine (muscarinic) Class A (Rhodopsin) Human 5ZK3 - 2.6 A Inactive 0.58 - - Apo-cytochrome b562 - acetylcholine
 small molecule Quinuclidinyl benzil... pubchem
Antagonist
 small molecule
 N/A No No Kobayashi T 10.1038/S41589-018-0152-Y 2018-11-21 Yes
ACM2 M2 Acetylcholine (muscarinic) Class A (Rhodopsin) Human 5ZKB - 3.0 A Inactive 0.97 - - Apo-cytochrome b562 - acetylcholine
 small molecule AF-DX 384 pubchem
Antagonist
 small molecule
 N/A No No Kobayashi T 10.1038/S41589-018-0152-Y 2018-11-21 Yes
ACM2 M2 Acetylcholine (muscarinic) Class A (Rhodopsin) Human 5ZKC - 2.3 A Inactive 0.83 - - Apo-cytochrome b562 - acetylcholine
 small molecule N-methyl scopolamine pubchem
Antagonist
 small molecule
 N/A No No Kobayashi T 10.1038/S41589-018-0152-Y 2018-11-21 Yes
ACM2 M2 Acetylcholine (muscarinic) Class A (Rhodopsin) Human 5ZK8 - 3.0 A Inactive 1.00 - - Redesigned apo-cytochrome b562 - acetylcholine
 small molecule N-methyl scopolamine pubchem
Antagonist
 small molecule
 N/A Yes No Kobayashi T 10.1038/S41589-018-0152-Y 2018-11-21 Yes
5HT2B 5-HT2B 5-Hydroxytryptamine Class A (Rhodopsin) Human 5TUD - 3.0 D Active 8.66 - - BRIL Antibody 5-hydroxytryptamine
 small molecule Ergotamine pubchem
Agonist
 small molecule
 in meso/LCP Yes No Cherezov V 10.1073/PNAS.1700891114 2017-07-26 Yes
PAR2 PAR2 Proteinase-activated Class A (Rhodopsin) Human 5NJ6 - 4.0 A Intermediate 7.10 - - BRIL
Fab3949 		- - N/A N/A N/A in meso/LCP Yes No Dekker N 10.1038/NATURE22309 2017-05-03 Yes
PAR2 PAR2 Proteinase-activated Class A (Rhodopsin) Human 5NDD - 2.8 A Intermediate 7.07 - - T4-Lysozyme
BRIL 		- - GTPL9585 pubchem
Antagonist
 small molecule
 in meso/LCP Yes Yes Dekker N 10.1038/NATURE22309 2017-05-03 Yes
PAR2 PAR2 Proteinase-activated Class A (Rhodopsin) Human 5NDZ - 3.6 A Intermediate 6.87 - - T4-Lysozyme
BRIL 		- - AZ3451 pubchem
Antagonist
 small molecule
 in meso/LCP Yes Yes Dekker N 10.1038/NATURE22309 2017-05-03 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 4UG2 - 2.6 A,B Intermediate 5.86 - - - - - Cgs 21680 pubchem
Agonist
 small molecule
 in meso/LCP Yes No Tate CG 10.1124/MOL.114.097360 2015-04-08 No
AA2AR A2A Adenosine Class A (Rhodopsin) Human 4UHR - 2.6 A Intermediate 6.28 - - - - - Cgs 21680 pubchem
Agonist
 small molecule
 in meso/LCP Yes No Tate CG 10.1124/MOL.114.097360 2015-04-08 Yes
CCR2 CCR2 Chemokine 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 No No Handel TM 10.1038/NATURE20605 2016-12-14 Yes
Q98SW5 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 in meso/LCP No No Salic A 10.1016/J.CELL.2018.04.029 2018-05-23 Yes
Q98SW5 SMO Frizzled Class F (Frizzled) African clawed frog 6D32 - 3.8 A Inactive -2.20 - - Cytochrome b562 - constitutive
 Constitutive Cyclopamine pubchem
Antagonist
 small molecule
 in meso/LCP No No Salic A 10.1016/J.CELL.2018.04.029 2018-05-23 Yes
ACM3 M3 Acetylcholine (muscarinic) Class A (Rhodopsin) Rat 4U14 - 3.6 A Inactive 0.52 - - T4-Lysozyme - acetylcholine
 small molecule Tiotropium pubchem
Antagonist
 small molecule
 sponge mesophase Yes No Kobilka BK 10.1016/J.STR.2014.08.022 2014-11-26 No
ACM3 M3 Acetylcholine (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 Yes No Kobilka BK 10.1016/J.STR.2014.08.022 2014-11-26 Yes
ACM3 M3 Acetylcholine (muscarinic) Class A (Rhodopsin) Rat 4U16 - 3.7 B Inactive 0.20 - - T4-Lysozyme - acetylcholine
 small molecule methscopolamine pubchem
Antagonist
 small molecule
 sponge mesophase Yes No Kobilka BK 10.1016/J.STR.2014.08.022 2014-11-26 Yes
OPRK κ Opioid 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 Yes No Roth BL 10.1016/J.CELL.2017.12.011 2018-01-17 Yes
OPSD 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 Yes No Kouyama T 10.1038/NATURE06925 2008-05-13 Yes
PE2R4 EP4 Prostanoid Class A (Rhodopsin) Human 5YHL - 4.2 A Inactive -0.94 - - Fab - - ONO-AE3-208-Br
Antagonist
 small molecule
 N/A No No Kobayashi T 10.1038/S41589-018-0131-3 2018-12-05 Yes
PE2R4 EP4 Prostanoid Class A (Rhodopsin) Human 5YWY - 3.2 A Inactive -0.97 - - Fab - - ONO-AE3-208 pubchem
Antagonist
 small molecule
 N/A No No Kobayashi T 10.1038/S41589-018-0131-3 2018-12-05 Yes
PE2R3 EP3 Prostanoid Class A (Rhodopsin) Human 6AK3 - 2.9 B Active 7.57 - - Soluble cytochrome b562 - - Prostaglandin E2 pubchem chembl_ligand
Agonist
 small molecule
 N/A Yes No Kobayashi T 10.1038/S41589-018-0131-3 2018-12-05 Yes
OPSD 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 No No Standfuss J 10.15252/EMBR.201642671 2016-08-10 Yes
OPSD Rhodopsin Opsins Class A (Rhodopsin) Bovine 5DYS - 2.3 A Active 7.70 - - - - retinal
 small molecule retinal gtoplig
Inverse agonist
 small molecule
 vapour diffusion No No Standfuss J 10.15252/EMBR.201642671 2016-08-10 Yes
GLP1R GLP-1 Glucagon Class B1 (Secretin) Human 5VEX - 3.0 B Inactive -5.05 - - Endolysin - - 4-{[(4-Cyclohexylphe... pubchem
Antagonist
 small molecule
 in meso/LCP No No Stevens RC 10.1038/NATURE22378 2017-05-17 Yes
GLP1R GLP-1 Glucagon Class B1 (Secretin) Human 5VEW - 2.7 A Inactive -5.10 - - Endolysin - - 97Y pubchem
Antagonist
 small molecule
 in meso/LCP No No Stevens RC 10.1038/NATURE22378 2017-05-24 Yes
AA1R A1 Adenosine Class A (Rhodopsin) Human 5UEN - 3.2 B Inactive -1.06 - - BRIL - - CHEMBL144360 pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Christopoulos A 10.1016/J.CELL.2017.01.042 2017-03-01 Yes
LPAR1 LPA1 Lysophospholipid (LPA) Class A (Rhodopsin) Human 4Z35 - 2.9 A Inactive -1.30 - - BRIL - LPA
 Lipid ONO-9910539 pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Hanson MA 10.1016/J.CELL.2015.06.002 2015-06-03 Yes
LPAR1 LPA1 Lysophospholipid (LPA) Class A (Rhodopsin) Human 4Z34 - 3.0 A Inactive -1.30 - - BRIL - LPA
 Lipid ONO-9780307 pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Hanson MA 10.1016/J.CELL.2015.06.002 2015-06-03 Yes
LPAR1 LPA1 Lysophospholipid (LPA) Class A (Rhodopsin) Human 4Z36 - 2.9 A Inactive -1.22 - - BRIL - LPA
 Lipid ONO-3080573 pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Hanson MA 10.1016/J.CELL.2015.06.002 2015-06-03 Yes
CXCR4 CXCR4 Chemokine Class A (Rhodopsin) Human 3OE8 - 3.1 A Inactive -1.28 - - T4-Lysozyme - CXCL12α
CXCL12β
 peptide IT1t pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Stevens RC 10.1126/SCIENCE.1194396 2010-10-27 No
CXCR4 CXCR4 Chemokine Class A (Rhodopsin) Human 3OE6 - 3.2 A Inactive -1.33 - - T4-Lysozyme - CXCL12α
CXCL12β
 peptide IT1t pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Stevens RC 10.1126/SCIENCE.1194396 2010-10-27 No
CXCR4 CXCR4 Chemokine Class A (Rhodopsin) Human 3OE9 - 3.1 A Inactive -0.65 - - T4-Lysozyme - CXCL12α
CXCL12β
 peptide IT1t pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Stevens RC 10.1126/SCIENCE.1194396 2010-10-27 No
CXCR4 CXCR4 Chemokine Class A (Rhodopsin) Human 3ODU - 2.5 A Inactive -1.34 - - T4-Lysozyme - CXCL12α
CXCL12β
 peptide IT1t pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Stevens RC 10.1126/SCIENCE.1194396 2010-10-27 Yes
CXCR4 CXCR4 Chemokine Class A (Rhodopsin) Human 3OE0 - 2.9 A Inactive -1.45 - - T4-Lysozyme - CXCL12α
CXCL12β
 peptide CVX15
Antagonist
 peptide
 in meso/LCP Yes No Stevens RC 10.1126/SCIENCE.1194396 2010-10-27 Yes
C5AR1 C5a1 Complement peptide Class A (Rhodopsin) Human 5O9H - 2.7 A Inactive -1.46 - - - - - NDT 9513727 pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Marshall FH 10.1038/NATURE25025 2018-01-10 Yes
CCR9 CCR9 Chemokine Class A (Rhodopsin) Human 5LWE - 2.8 B Inactive 0.09 - - - - - Vercirnon pubchem
Antagonist
 small molecule
 in meso/LCP No No Marshall FH 10.1038/NATURE20606 2016-12-07 Yes
DRD3 D3 Dopamine Class A (Rhodopsin) Human 3PBL - 2.9 A Inactive -0.43 - - T4-Lysozyme - dopamine
 small molecule Eticlopride pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Stevens RC 10.1126/SCIENCE.1197410 2010-11-03 Yes
GLR glucagon Glucagon Class B1 (Secretin) Human 5XF1 - 3.2 B Inactive -4.75 - - T4-Lysozyme Antibody - 4-{[(4-Cyclohexylphe... pubchem
Antagonist
 small molecule
 in meso/LCP No No Wu B 10.1038/NATURE22363 2017-05-24 Yes
GLR glucagon Glucagon Class B1 (Secretin) Human 5XEZ - 3.0 B Inactive -4.53 - - T4-Lysozyme Antibody - 4-{[(4-Cyclohexylphe... pubchem
Antagonist
 small molecule
 in meso/LCP No No Wu B 10.1038/NATURE22363 2017-05-24 Yes
APJ apelin Apelin 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 Yes No Xu F 10.1016/J.STR.2017.04.008 2017-05-31 Yes
DRD4 D4 Dopamine Class A (Rhodopsin) Human 5WIV - 2.1 A Inactive -0.93 - - BRIL - - Nemonapride pubchem
Antagonist
 small molecule
 in meso/LCP Yes Yes Roth BL 10.1126/SCIENCE.AAN5468 2017-10-18 Yes
DRD4 D4 Dopamine Class A (Rhodopsin) Human 5WIU - 2.0 A Inactive -0.97 - - - - - Nemonapride pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Roth BL 10.1126/SCIENCE.AAN5468 2017-10-18 Yes
AA1R A1 Adenosine Class A (Rhodopsin) Human 6D9H - 3.6 R Active 9.23 Gi2 - - - - Adenosine pubchem
Agonist
 small molecule
 Cryo-EM Yes No Christopoulos A 10.1038/S41586-018-0236-6 2018-06-20 Yes
G1SGD4 GLP-1 Glucagon Class B1 (Secretin) Rabbit 5VAI - 4.1 R Active 6.89 Gs - - - glucagon-like peptide 1
 peptide GLP-1 pubchem
Agonist
 peptide
 Cryo-EM No No Skiniotis G 10.1038/NATURE22394 2017-05-24 Yes
GLP1R GLP-1 Glucagon Class B1 (Secretin) Human 6B3J - 3.3 R Active 6.78 Gs - - - - Exendin-P5
Agonist
 peptide
 Cryo-EM No No Wootten D 10.1038/NATURE25773 2018-02-21 Yes
CRFR1 CRF1 Corticotropin-releasing factor 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 No No Marshall FH 10.2174/1874467210666170110114727 2016-06-29 Yes
P2Y12 P2Y12 P2Y Class A (Rhodopsin) Human 4NTJ - 2.6 A Intermediate 4.74 - - BRIL - - AZD1283 pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Zhao Q 10.1038/NATURE13083 2014-03-26 Yes
OPSD Rhodopsin Opsins Class A (Rhodopsin) Bovine 1GZM - 2.7 A Inactive 0.06 - - - - retinal
 small molecule retinal gtoplig
Inverse agonist
 small molecule
 vapour diffusion No No Schertler GF 10.1016/J.JMB.2004.08.090 2003-11-20 Yes
AGTR1 AT1 Angiotensin Class A (Rhodopsin) Human 4ZUD - 2.8 A Inactive -0.93 - - BRIL - - OLM
Inverse agonist
 small molecule
 in meso/LCP Yes No Stevens RC 10.1074/JBC.M115.689000 2015-10-07 Yes
NTR1 NTS1 Neurotensin Class A (Rhodopsin) Rat 4XEE - 2.9 A Intermediate 6.49 - - T4-Lysozyme - Neurotensin
neurotensin
 peptide CHEMBL342252 pubchem
Agonist
 peptide
 in meso/LCP Yes No Grisshammer R 10.1038/NCOMMS8895 2015-07-29 Yes
NTR1 NTS1 Neurotensin Class A (Rhodopsin) Rat 4XES - 2.6 A Intermediate 6.03 - - T4-Lysozyme - Neurotensin
neurotensin
 peptide CHEMBL342252 pubchem
Agonist
 peptide
 in meso/LCP Yes No Grisshammer R 10.1038/NCOMMS8895 2015-07-29 Yes
OX1R OX1 Orexin Class A (Rhodopsin) Human 4ZJC - 2.8 A Inactive -0.54 - - - - noradrenaline
 small molecule SB-674042 pubchem
Antagonist
 small molecule
 in meso/LCP No No Rosenbaum DM 10.1038/NSMB.3183 2016-03-09 Yes
OX1R OX1 Orexin Class A (Rhodopsin) Human 4ZJ8 - 2.8 A Inactive -0.47 - - - - noradrenaline
 small molecule Suvorexant pubchem
Antagonist
 small molecule
 in meso/LCP No No Rosenbaum DM 10.1038/NSMB.3183 2016-03-09 Yes
PTH1R PTH1 Parathyroid hormone Class B1 (Secretin) Human 6FJ3 - 2.5 A Inactive -19.28 - - GlgA glycogen synthase - - ePTH
Agonist
 peptide
 N/A No No Plückthun A 10.1038/S41594-018-0151-4 2018-11-21 Yes
NTR1 NTS1 Neurotensin Class A (Rhodopsin) Rat 4BV0 - 3.1 A Inactive 0.95 - - - - Neurotensin
neurotensin
 peptide CHEMBL342252 pubchem
Agonist
 peptide
 vapour diffusion Yes No Plückthun A 10.1073/PNAS.1317903111 2014-01-29 No
NTR1 NTS1 Neurotensin Class A (Rhodopsin) Rat 3ZEV - 3.0 A Inactive 0.45 - - - - Neurotensin
neurotensin
 peptide CHEMBL342252 pubchem
Agonist
 peptide
 vapour diffusion Yes No Plückthun A 10.1073/PNAS.1317903111 2014-01-29 No
NTR1 NTS1 Neurotensin Class A (Rhodopsin) Rat 4BWB - 3.6 A Inactive 1.53 - - - - Neurotensin
neurotensin
 peptide CHEMBL342252 pubchem
Agonist
 peptide
 vapour diffusion Yes No Plückthun A 10.1073/PNAS.1317903111 2014-01-29 No
NTR1 NTS1 Neurotensin Class A (Rhodopsin) Rat 4BUO - 2.8 A Inactive 0.57 - - - - Neurotensin
neurotensin
 peptide CHEMBL342252 pubchem
Agonist
 peptide
 vapour diffusion Yes No Plückthun A 10.1073/PNAS.1317903111 2014-01-29 Yes
OPRD δ Opioid 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 Yes No Kobilka BK 10.1038/NATURE11111 2012-05-16 Yes
CCR5 CCR5 Chemokine 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 No No Handel TM 10.1016/J.IMMUNI.2017.05.002 2017-06-28 Yes
US28 US28 Unclassified Class A (Rhodopsin) strain AD169 4XT1 - 2.9 A Active 9.02 - - - Nanobody CX3CL1
 peptide CX3CL1
Agonist
 peptide
 in meso/LCP Yes No Garcia KC 10.1126/SCIENCE.AAA5026 2015-03-04 Yes
US28 US28 Unclassified Class A (Rhodopsin) strain AD169 4XT3 - 3.8 A Active 8.85 - - - - CX3CL1
 peptide Fractalkine
Agonist
 peptide
 in meso/LCP Yes No Garcia KC 10.1126/SCIENCE.AAA5026 2015-03-04 Yes
CALCR CT Calcitonin Class B1 (Secretin) Human 5UZ7 - 4.1 R Active 7.80 Gs - - - - N/A N/A N/A Cryo-EM No No Sexton PM 10.1038/NATURE22327 2017-05-03 Yes
S1PR1 S1P1 Lysophospholipid (S1P) Class A (Rhodopsin) Human 3V2Y - 2.8 A Inactive -0.61 - - T4-Lysozyme - sphingosine 1-phosphate
 Lipid W146 pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Stevens RC 10.1126/SCIENCE.1215904 2012-02-15 Yes
S1PR1 S1P1 Lysophospholipid (S1P) Class A (Rhodopsin) Human 3V2W - 3.4 A Inactive -1.48 - - T4-Lysozyme - sphingosine 1-phosphate
 Lipid W146 pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Stevens RC 10.1126/SCIENCE.1215904 2012-02-15 No
5HT2B 5-HT2B 5-Hydroxytryptamine Class A (Rhodopsin) Human 4IB4 - 2.7 A Intermediate 3.08 - - BRIL - 5-hydroxytryptamine
 small molecule ERGOTAMINE pubchem
Agonist
 small molecule
 in meso/LCP Yes No Stevens RC 10.1126/SCIENCE.1232808 2013-03-13 Yes
GRM1 mGlu1 Metabotropic glutamate 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 No No Stevens RC 10.1126/SCIENCE.1249489 2014-03-19 Yes
5HT1B 5-HT1B 5-Hydroxytryptamine Class A (Rhodopsin) Human 4IAR - 2.7 A Intermediate 4.22 - - BRIL - - ERGOTAMINE pubchem
Agonist
 small molecule
 in meso/LCP Yes No Xu HE 10.1126/SCIENCE.1232807 2013-03-13 Yes
5HT1B 5-HT1B 5-Hydroxytryptamine Class A (Rhodopsin) Human 4IAQ - 2.8 A Intermediate 2.79 - - BRIL - - dihydroergotamine pubchem
Agonist
 small molecule
 in meso/LCP Yes No Xu HE 10.1126/SCIENCE.1232807 2013-03-13 Yes
ADRB1 β1 Adrenoceptors Class A (Rhodopsin) Common turkey 6H7O - 2.8 A Active 9.29 - - Thioredoxin 1 Camelid antibody fragment Nb6B9 - 4-{[(2S)-3-(tert-but... pubchem
Agonist
 small molecule
 N/A No No Tate CG 10.1101/436212 2018-10-17 Yes
ADRB1 β1 Adrenoceptors Class A (Rhodopsin) Common turkey 6H7N - 2.5 A Active 9.29 - - Thioredoxin 1 Camelid antibody fragment Nb6B9 - Xamoterol pubchem
Agonist
 small molecule
 N/A No No Tate CG 10.1101/436212 2018-10-17 Yes
ADRB1 β1 Adrenoceptors Class A (Rhodopsin) Common turkey 6H7L - 2.7 A Active 9.24 - - Thioredoxin 1 Camelid antibody fragment Nb6B9 - DOBUTAMINE pubchem
Agonist
 small molecule
 N/A No No Tate CG 10.1101/436212 2018-10-17 Yes
ADRB1 β1 Adrenoceptors Class A (Rhodopsin) Common turkey 6H7J - 2.8 A Active 9.27 - - Thioredoxin 1 Camelid antibody fragment Nb80 - ISOPRENALINE pubchem
Agonist
 small molecule
 N/A No No Tate CG 10.1101/436212 2018-10-17 Yes
ADRB1 β1 Adrenoceptors Class A (Rhodopsin) Common turkey 6H7M - 2.8 A Active 9.30 - - Thioredoxin 1 Camelid antibody fragment Nb6B9 - SALBUTAMOL pubchem
Agonist
 small molecule
 N/A No No Tate CG 10.1101/436212 2018-10-17 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 3VGA - 3.1 A Inactive -1.40 - - - - - ZM241385 pubchem
Antagonist
 small molecule
 vapour diffusion Yes No Murata T 10.1038/NATURE10750 2012-02-01 No
AA2AR A2A Adenosine Class A (Rhodopsin) Human 3VG9 - 2.7 A Inactive -1.20 - - - - - ZM241385 pubchem
Antagonist
 small molecule
 vapour diffusion Yes No Murata T 10.1038/NATURE10750 2012-02-01 Yes
OPSD 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 No No Xu HE 10.1038/NATURE14656 2015-07-29 Yes
OPRM μ Opioid 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 Yes No Granier S 10.1038/NATURE10954 2012-03-21 Yes
ADRB1 β1 Adrenoceptors Class A (Rhodopsin) Common turkey 4AMI - 3.2 A Inactive -1.16 - - - - - bucindolol pubchem
Agonist
 small molecule
 vapour diffusion Yes No Tate CG 10.1016/J.STR.2012.03.014 2012-05-23 Yes
ADRB1 β1 Adrenoceptors Class A (Rhodopsin) Common turkey 4AMJ - 2.3 B Inactive -1.01 - - - - - (S)-Carvedilol pubchem
Inverse agonist
 small molecule
 vapour diffusion Yes No Tate CG 10.1016/J.STR.2012.03.014 2012-05-23 Yes
ADRB2 β2 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 Yes No Kobilka BK 10.1038/NATURE09665 2011-01-12 Yes
ADRB1 β1 Adrenoceptors Class A (Rhodopsin) Common turkey 2Y00 - 2.5 B Inactive -1.22 - - - - - Dobutamine pubchem
Agonist (partial)
 small molecule
 vapour diffusion Yes No Tate CG 10.1038/NATURE09746 2011-01-12 Yes
ADRB1 β1 Adrenoceptors Class A (Rhodopsin) Common turkey 2Y02 - 2.6 B Inactive -1.15 - - - - - Carmoterol pubchem
Agonist
 small molecule
 vapour diffusion Yes No Tate CG 10.1038/NATURE09746 2011-01-12 Yes
ADRB1 β1 Adrenoceptors Class A (Rhodopsin) Common turkey 2Y04 - 3.1 B Inactive -1.14 - - - - - Levalbuterol pubchem
Agonist (partial)
 small molecule
 vapour diffusion Yes No Tate CG 10.1038/NATURE09746 2011-01-12 Yes
ADRB1 β1 Adrenoceptors Class A (Rhodopsin) Common turkey 2Y03 - 2.9 B Inactive -1.20 - - - - - LEVISOPRENALINE pubchem
Agonist
 small molecule
 vapour diffusion Yes No Tate CG 10.1038/NATURE09746 2011-01-12 Yes
ADRB1 β1 Adrenoceptors Class A (Rhodopsin) Common turkey 2Y01 - 2.6 A Inactive -1.07 - - - - - Dobutamine pubchem
Agonist (partial)
 small molecule
 vapour diffusion Yes No Tate CG 10.1038/NATURE09746 2011-03-30 No
OPSD Rhodopsin Opsins Class A (Rhodopsin) Bovine 1L9H - 2.6 A Inactive -0.45 - - - - retinal
 small molecule retinal gtoplig
Inverse agonist
 small molecule
 vapour diffusion No No Shichida Y 10.1073/PNAS.082666399 2002-05-15 No
OPSD 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 No No Okada T 10.1529/BIOPHYSJ.107.108225 2007-10-30 No
AA2AR A2A Adenosine Class A (Rhodopsin) Human 5IUA - 2.2 A Inactive -0.68 - - BRIL - - 2-(Furan-2-Yl)-N~5~-... pubchem
Agonist
 small molecule
 in meso/LCP Yes Yes Cooke RM 10.1021/ACS.JMEDCHEM.6B00653 2016-06-29 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 5IU8 - 2.0 A Inactive -0.82 - - BRIL - - CHEMBL3934661 pubchem
Agonist
 small molecule
 in meso/LCP Yes Yes Cooke RM 10.1021/ACS.JMEDCHEM.6B00653 2016-06-29 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 5IU4 - 1.7 A Inactive -0.76 - - BRIL - - ZM241385 pubchem
Antagonist
 small molecule
 in meso/LCP Yes Yes Cooke RM 10.1021/ACS.JMEDCHEM.6B00653 2016-06-29 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 5IU7 - 1.9 A Inactive -0.68 - - BRIL - - 2-(Furan-2-Yl)-N~5~-... pubchem
Agonist
 small molecule
 in meso/LCP Yes Yes Cooke RM 10.1021/ACS.JMEDCHEM.6B00653 2016-06-29 Yes
ADRB2 β2 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 Yes No Stevens RC 10.1021/JA105108Q 2010-08-11 Yes
ADRB2 β2 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 Yes No Stevens RC 10.1021/JA105108Q 2010-08-11 Yes
ADRB2 β2 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 Yes No Stevens RC 10.1021/JA105108Q 2010-08-11 Yes
OPSD 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 No No Stenkamp RE 10.1021/BI0155091 2001-07-04 No
OPSD 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 No No Ernst OP 10.1038/NPROT.2017.135 2017-12-13 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 5VRA - 2.4 A Inactive -0.39 - - BRIL - - ZM 241385 pubchem
Antagonist
 small molecule
 in meso/LCP Yes Yes Ernst OP 10.1038/NPROT.2017.135 2017-12-13 Yes
OPRD δ Opioid 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 Yes Yes Cherezov V 10.1038/NSMB.2965 2015-01-14 Yes
OPRD δ Opioid 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 Yes No Cherezov V 10.1038/NSMB.2965 2015-01-14 No
AA2AR A2A Adenosine Class A (Rhodopsin) Human 5K2A - 2.5 A Inactive -0.71 - - BRIL - - ZM241385 pubchem
Antagonist
 small molecule
 in meso/LCP Yes Yes Cherezov V 10.1126/SCIADV.1600292 2016-09-21 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 5K2B - 2.5 A Inactive -0.63 - - BRIL - - ZM241385 pubchem
Antagonist
 small molecule
 in meso/LCP Yes Yes Cherezov V 10.1126/SCIADV.1600292 2016-09-21 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 5K2C - 1.9 A Inactive -0.67 - - BRIL - - ZM241385 pubchem
Antagonist
 small molecule
 in meso/LCP Yes Yes Cherezov V 10.1126/SCIADV.1600292 2016-09-21 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 5K2D - 1.9 A Inactive -0.71 - - BRIL - - ZM241385 pubchem
Antagonist
 small molecule
 in meso/LCP Yes Yes Cherezov V 10.1126/SCIADV.1600292 2016-09-21 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 5OLV - 2.0 A Inactive -0.56 - - Soluble cytochrome b562 - - CHEMBL1671936 pubchem chembl_ligand
Antagonist
 small molecule
 in meso/LCP Yes Yes Doré AS 10.1038/S41598-017-18570-W 2018-01-17 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 5OLG - 1.9 A Inactive -0.73 - - Soluble cytochrome b562 - - ZM 241385
Antagonist
 small molecule
 in meso/LCP Yes Yes Doré AS 10.1038/S41598-017-18570-W 2018-01-17 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 5OLZ - 1.9 A Inactive -0.75 - - Soluble cytochrome b562 - - 4-(3-amino-5-phenyl-...
Antagonist
 small molecule
 in meso/LCP Yes Yes Doré AS 10.1038/S41598-017-18570-W 2018-01-17 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 5OM4 - 2.0 A Inactive -0.66 - - Soluble cytochrome b562 - - 4-(3-amino-5-phenyl-...
Antagonist
 small molecule
 in meso/LCP Yes Yes Doré AS 10.1038/S41598-017-18570-W 2018-01-17 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 5OM1 - 2.1 A Inactive -0.69 - - Soluble cytochrome b562 - - 4-(3-amino-5-phenyl-...
Antagonist
 small molecule
 in meso/LCP Yes Yes Doré AS 10.1038/S41598-017-18570-W 2018-01-17 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 5OLO - 3.1 A Inactive -0.69 - - Soluble cytochrome b562 - - Tozadenant pubchem chembl_ligand
Antagonist
 small molecule
 in meso/LCP Yes No Doré AS 10.1038/S41598-017-18570-W 2018-01-17 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 5OLH - 2.6 A Inactive -0.70 - - Soluble cytochrome b562 - - Vipadenant
Antagonist
 small molecule
 in meso/LCP Yes Yes Doré AS 10.1038/S41598-017-18570-W 2018-01-17 Yes
EDNRB ETB Endothelin Class A (Rhodopsin) Human 6IGK - 2.0 A Intermediate 2.18 - - Endolysin - - Endothelin-3 pubchem
Agonist
 peptide
 N/A Yes No Nureki O 10.1038/S41467-018-07094-0 2018-11-21 Yes
EDNRB ETB Endothelin Class A (Rhodopsin) Human 6IGL - 2.7 A Inactive 0.16 - - Endolysin - - IRL1620 pubchem
Partial agonist
 peptide
 N/A Yes No Nureki O 10.1038/S41467-018-07094-0 2018-11-21 Yes
CCR5 CCR5 Chemokine Class A (Rhodopsin) Human 6AKX - 2.8 B Inactive 0.71 - - Rubredoxin - CCL11
CCL14
CCL16
CCL2
CCL3
CCL4
CCL5
CCL7
CCL8
 peptide N-[(1S)-3-{(3-exo)-3...
Antagonist
 small molecule
 N/A No No Liu H 10.1021/ACS.JMEDCHEM.8B01077 2018-10-24 Yes
CCR5 CCR5 Chemokine Class A (Rhodopsin) Human 6AKY - 2.8 A Inactive 0.40 - - Rubredoxin - CCL11
CCL14
CCL16
CCL2
CCL3
CCL4
CCL5
CCL7
CCL8
 peptide 4,4-difluoro-N-[(1S)...
Antagonist
 small molecule
 N/A No No Liu H 10.1021/ACS.JMEDCHEM.8B01077 2018-10-24 Yes
CCR2 CCR2 Chemokine Class A (Rhodopsin) Human 6GPX - 2.7 B Inactive 0.58 - - Rubredoxin - - MK-0812 pubchem
Antagonist
 small molecule
 N/A No No Schnapp G 10.1016/J.STR.2018.10.027 2019-01-02 Yes
CCR2 CCR2 Chemokine Class A (Rhodopsin) Human 6GPS - 3.3 A Inactive 0.82 - - Rubredoxin - - MK-0812 pubchem
Antagonist
 small molecule
 N/A No No Schnapp G 10.1016/J.STR.2018.10.027 2019-01-02 Yes
ADRB2 β2 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 Yes No Stevens RC 10.1126/SCIENCE.1150577 2007-10-30 Yes
ADRB2 β2 Adrenoceptors Class A (Rhodopsin) Human 6MXT - 3.0 A Active 8.22 - - Endolysin Nanobody 71 (-)-adrenaline
(-)-noradrenaline
 small molecule Salmeterol pubchem
Agonist
 small molecule
 N/A No No Kobilka BK 10.1038/S41589-018-0145-X 2018-11-14 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 3UZA - 3.3 A Inactive -0.56 - - - - - CHEMBL2024115 pubchem
Antagonist
 small molecule
 vapour diffusion Yes No Marshall FH 10.1021/JM201376W 2012-03-21 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 3UZC - 3.3 A Inactive -0.50 - - - - - T4E
Antagonist
 small molecule
 vapour diffusion Yes No Marshall FH 10.1021/JM201376W 2012-03-21 Yes
OPSD 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 No No Ernst OP 10.1002/ANIE.201302374 2013-10-30 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 5MZJ - 2.0 A Inactive -0.54 - - - - - Theophylline pubchem
Antagonist
 small molecule
 in meso/LCP Yes Yes Cooke RM 10.1016/J.STR.2017.06.012 2017-07-26 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 5MZP - 2.1 A Inactive -0.75 - - - - - Caffeine pubchem
Antagonist
 small molecule
 in meso/LCP Yes Yes Cooke RM 10.1016/J.STR.2017.06.012 2017-07-26 Yes
AA1R A1 Adenosine Class A (Rhodopsin) Human 5N2S - 3.3 A Inactive -0.47 - - - - - PSB36 pubchem
Agonist
 small molecule
 in meso/LCP No No Cooke RM 10.1016/J.STR.2017.06.012 2017-07-26 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 5N2R - 2.8 A Inactive -0.73 - - BRIL - - PSB36 pubchem
Antagonist
 small molecule
 in meso/LCP Yes Yes Cooke RM 10.1016/J.STR.2017.06.012 2017-07-26 Yes
OPSD Rhodopsin Opsins Class A (Rhodopsin) Bovine 5TE3 - 2.7 A Active 7.98 - - - - retinal
 small molecule N/A N/A N/A vapour diffusion No No Palczewski K 10.1073/PNAS.1617446114 2017-03-15 Yes
OPSD 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 No No Palczewski K 10.1073/PNAS.1617446114 2017-03-15 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 4EIY - 1.8 A Inactive -0.55 - - BRIL - - ZM241385 pubchem
Antagonist
 small molecule
 in meso/LCP Yes Yes Stevens RC 10.1126/SCIENCE.1219218 2012-07-25 Yes
SMO SMO Frizzled Class F (Frizzled) Human 5V57 - 3.0 A Inactive -1.67 - - Flavodoxin - constitutive
 Constitutive N-methyl-N-[1-[4-(2-... pubchem
Antagonist
 small molecule
 in meso/LCP No No Xu F 10.1038/NCOMMS15383 2017-05-24 Yes
SMO SMO Frizzled Class F (Frizzled) Human 5V56 - 2.9 B Inactive -1.89 - - Flavodoxin - constitutive
 Constitutive N-methyl-N-[1-[4-(2-... pubchem
Antagonist
 small molecule
 in meso/LCP No No Xu F 10.1038/NCOMMS15383 2017-05-24 Yes
OPSD 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 Yes No Kouyama T 10.1016/J.JMB.2011.08.044 2011-08-17 No
OPSD 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 Yes No Kouyama T 10.1016/J.JMB.2011.08.044 2011-08-17 No
ADRB1 β1 Adrenoceptors Class A (Rhodopsin) Common turkey 2YCZ - 3.7 B Inactive -1.72 - - - - - timolol pubchem
Antagonist
 small molecule
 vapour diffusion Yes No Schertler GFX 10.1073/PNAS.1100185108 2011-06-01 Yes
ADRB1 β1 Adrenoceptors Class A (Rhodopsin) Common turkey 2YCW - 3.0 A Inactive -1.08 - - - - - timolol pubchem
Inverse agonist
 small molecule
 vapour diffusion Yes No Schertler GFX 10.1073/PNAS.1100185108 2011-06-01 Yes
ADRB1 β1 Adrenoceptors Class A (Rhodopsin) Common turkey 2YCY - 3.2 A Inactive -1.62 - - - - - (S)-Cyanopindolol pubchem
Antagonist
 small molecule
 vapour diffusion Yes No Schertler GFX 10.1073/PNAS.1100185108 2011-06-08 No
ADRB1 β1 Adrenoceptors Class A (Rhodopsin) Common turkey 2YCX - 3.3 A Inactive -1.64 - - - - - (S)-Cyanopindolol pubchem
Antagonist
 small molecule
 vapour diffusion Yes No Schertler GFX 10.1073/PNAS.1100185108 2011-06-01 No
CRFR1 CRF1 Corticotropin-releasing factor 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 No No Marshall FH 10.1038/NATURE12357 2013-07-17 Yes
ADRB2 β2 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 Yes No Caffrey M 10.1107/S2059798315021683 2016-01-13 No
ADRB2 β2 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 Yes No Caffrey M 10.1107/S2059798315021683 2016-01-13 No
AA2AR A2A Adenosine Class A (Rhodopsin) Human 6AQF - 2.5 A Inactive -0.44 - - Soluble cytochrome b562 - - ZM 241385 pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Wüthrich K 10.1016/J.CELL.2017.12.004 2018-01-10 Yes
OPSD Rhodopsin Opsins Class A (Rhodopsin) Bovine 6FK7 - 2.6 A Active 7.68 - - - - retinal
 small molecule (2~{R},3~{R})-2-(4-c...
Agonist
 small molecule
 vapour diffusion No No Dawson RJP 10.1073/PNAS.1718084115 2018-04-04 Yes
OPSD Rhodopsin Opsins Class A (Rhodopsin) Bovine 6FK8 - 2.9 A Active 7.94 - - - - retinal
 small molecule (2~{R},3~{S})-3-azan...
Agonist
 small molecule
 vapour diffusion No No Dawson RJP 10.1073/PNAS.1718084115 2018-04-04 Yes
OPSD Rhodopsin Opsins Class A (Rhodopsin) Bovine 6FKB - 3.0 A Active 7.93 - - - - retinal
 small molecule 2-(4-chlorophenyl)-1...
Agonist
 small molecule
 vapour diffusion No No Dawson RJP 10.1073/PNAS.1718084115 2018-04-04 Yes
OPSD Rhodopsin Opsins Class A (Rhodopsin) Bovine 6FK9 - 2.6 A Active 7.83 - - - - retinal
 small molecule (2~{S})-3-methyl-2-p...
Agonist
 small molecule
 vapour diffusion No No Dawson RJP 10.1073/PNAS.1718084115 2018-04-04 Yes
OPSD Rhodopsin Opsins Class A (Rhodopsin) Bovine 6FKD - 2.5 A Active 7.92 - - - - retinal
 small molecule 5-chloranyl-2-(2-oxi...
Agonist
 small molecule
 vapour diffusion No No Dawson RJP 10.1073/PNAS.1718084115 2018-04-04 Yes
OPSD Rhodopsin Opsins Class A (Rhodopsin) Bovine 6FKC - 2.5 A Active 7.84 - - - - retinal
 small molecule 3-[1'-[(2~{S})-2-(4-...
Agonist
 small molecule
 vapour diffusion No No Dawson RJP 10.1073/PNAS.1718084115 2018-04-04 Yes
OPSD Rhodopsin Opsins Class A (Rhodopsin) Bovine 6FKA - 2.7 A Active 7.99 - - - - retinal
 small molecule (2~{S})-2-(3,4-dichl...
Agonist
 small molecule
 vapour diffusion No No Dawson RJP 10.1073/PNAS.1718084115 2018-04-04 Yes
OPSD Rhodopsin Opsins Class A (Rhodopsin) Bovine 6FK6 - 2.4 A Active 7.85 - - - - retinal
 small molecule (2~{S})-2-(4-chlorop...
Agonist
 small molecule
 vapour diffusion No No Dawson RJP 10.1073/PNAS.1718084115 2018-04-04 Yes
ADRB1 β1 Adrenoceptors Class A (Rhodopsin) Common turkey 5F8U - 3.4 A Inactive -0.51 - - - - - (S)-Cyanopindolol pubchem
Antagonist
 small molecule
 vapour diffusion Yes No Tate CG 10.1038/NSMB.3130 2015-12-23 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 2YDO - 3.0 A Intermediate 6.28 - - - - - adenosine pubchem
Agonist
 small molecule
 vapour diffusion Yes No Tate CG 10.1038/NATURE10136 2011-05-18 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 2YDV - 2.6 A Intermediate 6.21 - - - - - NECA pubchem
Agonist
 small molecule
 vapour diffusion Yes No Tate CG 10.1038/NATURE10136 2011-05-18 Yes
5HT2B 5-HT2B 5-Hydroxytryptamine Class A (Rhodopsin) Human 6DS0 - 3.2 A Intermediate 3.21 - - Soluble cytochrome b562 - 5-hydroxytryptamine
 small molecule LY266097 pubchem
Antagonist
 small molecule
 N/A Yes No Roth BL 10.1038/S41594-018-0116-7 2018-08-29 Yes
5HT2B 5-HT2B 5-Hydroxytryptamine Class A (Rhodopsin) Human 6DRY - 2.9 A Intermediate 4.34 - - Soluble cytochrome b562 - 5-hydroxytryptamine
 small molecule Methylergonovine pubchem chembl_ligand
Agonist
 small molecule
 N/A Yes No Roth BL 10.1038/S41594-018-0116-7 2018-08-29 Yes
5HT2B 5-HT2B 5-Hydroxytryptamine Class A (Rhodopsin) Human 6DRZ - 3.1 A Intermediate 4.19 - - Soluble cytochrome b562 - 5-hydroxytryptamine
 small molecule Methysergide pubchem
Antagonist
 small molecule
 N/A Yes No Roth BL 10.1038/S41594-018-0116-7 2018-08-29 Yes
5HT2B 5-HT2B 5-Hydroxytryptamine Class A (Rhodopsin) Human 6DRX - 3.1 A Intermediate 2.67 - - Soluble cytochrome b562 - 5-hydroxytryptamine
 small molecule Lisuride pubchem
Antagonist
 small molecule
 N/A Yes No Roth BL 10.1038/S41594-018-0116-7 2018-08-29 Yes
ADRB1 β1 Adrenoceptors Class A (Rhodopsin) Common turkey 2VT4 - 2.7 B Inactive -1.55 - - - - - (S)-Cyanopindolol pubchem
Antagonist
 small molecule
 vapour diffusion Yes No Schertler GFX 10.1038/NATURE07101 2008-06-24 No
AA2AR A2A Adenosine Class A (Rhodopsin) Human 3REY - 3.3 A Inactive -0.38 - - - - - Xanthine amine conge... pubchem
Antagonist
 small molecule
 vapour diffusion Yes No Marshall FH 10.1016/J.STR.2011.06.014 2011-09-07 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 3RFM - 3.6 A Inactive -0.48 - - - - - caffeine pubchem
Antagonist
 small molecule
 vapour diffusion Yes No Marshall FH 10.1016/J.STR.2011.06.014 2011-09-07 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 3PWH - 3.3 A Inactive -0.67 - - - - - ZM241385 pubchem
Antagonist
 small molecule
 vapour diffusion Yes No Marshall FH 10.1016/J.STR.2011.06.014 2011-09-07 No
P2Y12 P2Y12 P2Y Class A (Rhodopsin) Human 4PXZ - 2.5 A Intermediate 3.91 - - BRIL - - 2-MeSADP pubchem
Agonist
 small molecule
 in meso/LCP Yes No Zhao Q 10.1038/NATURE13288 2014-04-30 Yes
P2Y12 P2Y12 P2Y Class A (Rhodopsin) Human 4PY0 - 3.1 A Intermediate 3.81 - - BRIL - - 2-Mesatp pubchem
Agonist (partial)
 small molecule
 in meso/LCP Yes No Zhao Q 10.1038/NATURE13288 2014-04-30 Yes
ADRB2 β2 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 Yes No Kobilka BK 10.1038/NATURE06325 2007-11-06 No
ADRB2 β2 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 Yes No Kobilka BK 10.1038/NATURE06325 2007-11-06 No
ADRB2 β2 Adrenoceptors Class A (Rhodopsin) Human 4LDE - 2.8 A Active 9.40 - - T4-Lysozyme Nanobody (-)-adrenaline
(-)-noradrenaline
 small molecule BI167107 pubchem
Agonist
 small molecule
 in meso/LCP No No Kobilka BK 10.1038/NATURE12572 2013-09-25 Yes
ADRB2 β2 Adrenoceptors Class A (Rhodopsin) Human 4LDL - 3.1 A Active 9.26 - - T4-Lysozyme Nanobody (-)-adrenaline
(-)-noradrenaline
 small molecule hydroxybenzylisoprot... pubchem
Agonist
 small molecule
 in meso/LCP No No Kobilka BK 10.1038/NATURE12572 2013-09-25 Yes
ADRB2 β2 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 No No Kobilka BK 10.1038/NATURE12572 2013-09-25 Yes
OPSD 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 No No Scheerer P 10.1038/NCOMMS5801 2014-09-17 No
GLR glucagon Glucagon Class B1 (Secretin) Human 4L6R - 3.3 A Inactive -4.62 - - BRIL - - N/A N/A N/A in meso/LCP No No Stevens RC 10.1038/NATURE12393 2013-07-24 Yes
OPSD Rhodopsin Opsins Class A (Rhodopsin) Bovine 3OAX - 2.6 A Inactive 0.02 - - - - retinal
 small molecule retinal gtoplig
Inverse agonist
 small molecule
 vapour diffusion No No Okada T 10.1016/J.BPJ.2010.08.003 2011-01-19 No
OPRM μ Opioid 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 Yes No Kobilka BK 10.1038/S41586-018-0219-7 2018-06-13 Yes
OPRM μ Opioid Class A (Rhodopsin) Mouse 6DDE - 3.5 R Active 7.19 Gi - - Antibody β-endorphin
dynorphin A
dynorphin B
endomorphin-1
[Leu]enkephalin
[Met]enkephalin
 peptide DAMGO pubchem chembl_ligand
Agonist
 peptide-like
 Cryo-EM Yes No Kobilka BK 10.1038/S41586-018-0219-7 2018-06-13 Yes
OPSD 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 Yes No Kouyama T 10.1371/JOURNAL.PONE.0126970 2015-06-17 No
ACM2 M2 Acetylcholine (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 Yes No Kobayashi T 10.1038/NATURE10753 2012-02-01 Yes
AA2AR A2A Adenosine Class A (Rhodopsin) Human 5JTB - 2.8 A Inactive -0.46 - - BRIL - - ZM241385 pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Popov A 10.1126/SCIADV.1602952 2017-05-31 Yes
OPSD Rhodopsin Opsins Class A (Rhodopsin) Bovine 3PXO - 3.0 A Active 7.94 - - - - retinal
 small molecule retinal gtoplig
Agonist
 small molecule
 vapour diffusion No No Ernst OP 10.1038/NATURE09789 2011-03-09 No
OPSD Rhodopsin Opsins Class A (Rhodopsin) Bovine 3PQR - 2.9 A Active 8.57 Gt - - - retinal
 small molecule retinal gtoplig
Agonist
 small molecule
 vapour diffusion No No Ernst OP 10.1038/NATURE09789 2011-03-09 Yes
OPSD Rhodopsin Opsins Class A (Rhodopsin) Bovine 4BEZ - 3.3 A Active 8.33 - - - - retinal
 small molecule N/A N/A N/A vapour diffusion No No Standfuss J 10.1038/EMBOR.2013.44 2013-04-24 No
OPSD 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 No No Standfuss J 10.1038/EMBOR.2013.44 2013-05-08 No
OPSD Rhodopsin Opsins Class A (Rhodopsin) Bovine 2I36 - 4.1 A,B,C Inactive -0.36 - - - - retinal
 small molecule N/A N/A N/A vapour diffusion No No Palczewski K 10.1073/PNAS.0608022103 2006-10-17 No
OPSD Rhodopsin Opsins Class A (Rhodopsin) Bovine 2I35 - 3.8 A Inactive -0.33 - - - - retinal
 small molecule retinal gtoplig
Inverse agonist
 small molecule
 vapour diffusion No No Palczewski K 10.1073/PNAS.0608022103 2006-10-17 No
OPSD Rhodopsin Opsins Class A (Rhodopsin) Bovine 2I37 - 4.2 A Inactive -1.63 - - - - retinal
 small molecule N/A N/A N/A vapour diffusion No No Palczewski K 10.1073/PNAS.0608022103 2006-10-17 No
ADRB2 β2 Adrenoceptors Class A (Rhodopsin) Human 4QKX - 3.3 A Active 9.44 - - T4-Lysozyme Nanobody (-)-adrenaline
(-)-noradrenaline
 small molecule 35V pubchem
Agonist
 small molecule
 in meso/LCP No No Gmeiner P 10.1073/PNAS.1410415111 2014-07-23 Yes
OPSD Rhodopsin Opsins Class A (Rhodopsin) Bovine 2G87 - 2.6 A,B Inactive -0.18 - - - - retinal
 small molecule retinal gtoplig
Agonist
 small molecule
 vapour diffusion No No Okada T 10.1002/ANIE.200600595 2006-09-02 No
AA2AR A2A Adenosine Class A (Rhodopsin) Human 3EML - 2.6 A Inactive -1.16 - - T4-Lysozyme - - ZM241385 pubchem
Antagonist
 small molecule
 in meso/LCP Yes No Stevens RC 10.1126/SCIENCE.1164772 2008-10-14 No
NTR1 NTS1 Neurotensin Class A (Rhodopsin) Rat 4GRV - 2.8 A Intermediate 7.34 - - T4-Lysozyme - Neurotensin
neurotensin
 peptide Neurotensin(8-13) pubchem
Agonist
 peptide
 in meso/LCP Yes No Grisshammer R 10.1038/NATURE11558 2012-10-17 Yes
OPSD Rhodopsin Opsins Class A (Rhodopsin) Bovine 6FUF - 3.1 A Active 8.28 - - - - retinal
 small molecule Retinal pubchem
Inverse agonist
 small molecule
 N/A No No Schertler GFX 10.1126/SCIADV.AAT7052 2018-10-03 Yes
C5AR1 C5a1 Complement peptide Class A (Rhodopsin) Human 6C1R - 2.2 B Inactive -1.37 - - Soluble cytochrome b562 - - PMX53 pubchem chembl_ligand