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PDB Refined structure Resolution
Q80KM9 US28 Unclassified A (Rhodopsin) strain AD169 5WB2_refined Active - - - CX3CL1
Agonist
peptide
in meso/LCP Yes No Garcia KC 10.7554/ELIFE.35850 2018-06-13 Yes
Q80KM9 US28 Unclassified A (Rhodopsin) strain AD169 5WB1_refined Active - - - N/A N/A N/A in meso/LCP Yes No Garcia KC 10.7554/ELIFE.35850 2018-06-13 Yes
EDNRB ETB Endothelin A (Rhodopsin) Human 5XPR_refined Inactive - - - N/A N/A N/A in meso/LCP Yes No Nureki O 10.1038/NSMB.3450 2017-08-16 Yes
EDNRB ETB Endothelin A (Rhodopsin) Human 5X93_refined Inactive - Endolysin - K-8794 pubchem
Antagonist
small molecule
in meso/LCP Yes No Nureki O 10.1038/NSMB.3450 2017-08-16 Yes
GLP1R GLP-1 Glucagon B1 (Secretin) Human 5NX2_refined Intermediate - - - truncated protein ag...
Agonist
peptide
vapour diffusion No No Marshall FH 10.1038/NATURE22800 2017-06-14 Yes
ACM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human 5DSG_refined Inactive - T4-Lysozyme acetylcholine
small molecule Tiotropium pubchem
Antagonist
small molecule
in meso/LCP Yes No Christopoulos A 10.1038/NATURE17188 2016-03-16 Yes
ACM1 M1 Acetylcholine (muscarinic) A (Rhodopsin) Human 5CXV_refined Inactive - Endolysin acetylcholine
small molecule CHEMBL258622 pubchem
Antagonist
small molecule
in meso/LCP Yes No Christopoulos A 10.1038/NATURE17188 2016-03-09 Yes
OX2R OX2 Orexin A (Rhodopsin) Human 5WS3_refined Inactive - 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
OX2R OX2 Orexin A (Rhodopsin) Human - Inactive - 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
AA2AR A2A Adenosine A (Rhodopsin) Human 5G53_refined Active Engineered G protein - - NECA pubchem
Agonist
small molecule
vapour diffusion Yes No Tate CG 10.1038/NATURE18966 2016-08-03 Yes
OPRD δ Opioid A (Rhodopsin) Human 4N6H_refined Inactive - 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
PE2R3 EP3 Prostanoid A (Rhodopsin) Human 6M9T_refined Intermediate - Endolysin chimera - misoprostol-FA pubchem
Antagonist
small molecule
N/A Yes No Stevens RC 10.1038/S41589-018-0160-Y 2018-12-05 Yes
NTR1 NTS1 Neurotensin A (Rhodopsin) Rat 5T04_refined Active - T4-Lysozyme neurotensin
peptide CHEMBL342252 pubchem
Agonist
peptide
in meso/LCP Yes No Grisshammer R 10.1038/SREP38564 2016-12-21 Yes
PAR1 PAR1 Proteinase-activated A (Rhodopsin) Human 3VW7_refined Intermediate - T4-Lysozyme thrombin
peptide Vorapaxar pubchem
Antagonist
small molecule
in meso/LCP Yes No Kobilka BK 10.1038/NATURE11701 2012-12-12 Yes
P2RY1 P2Y1 P2Y A (Rhodopsin) Human 4XNW_refined Intermediate - Rubredoxin ADP
small molecule MRS2500 pubchem
Antagonist
small molecule
in meso/LCP Yes No Wu B 10.1038/NATURE14287 2015-04-01 Yes
P2RY1 P2Y1 P2Y A (Rhodopsin) Human 4XNV_refined Intermediate - Rubredoxin ADP
small molecule BPTU pubchem
Antagonist
small molecule
in meso/LCP Yes No Wu B 10.1038/NATURE14287 2015-04-01 Yes
CALRL calcitonin-like Calcitonin B1 (Secretin) Human 6E3Y_refined Active Gs RAMP1 - Calcitonin gene-rela... pubchem
Agonist
peptide
N/A No No Sexton PM 10.1038/S41586-018-0535-Y 2018-09-19 Yes
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human 5JQH_refined Inactive - T4-Lysozyme (-)-adrenaline
(-)-noradrenaline
small molecule Carazolol pubchem
Inverse agonist
small molecule
in meso/LCP Yes No Lefkowitz RJ 10.1038/NATURE18636 2016-07-13 Yes
SMO SMO Frizzled F (Frizzled) Human 5L7D_refined Inactive - 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 F (Frizzled) Human 5L7I_refined Inactive - BRIL constitutive
Constitutive Vismodegib pubchem
Antagonist
small molecule
in meso/LCP No No Siebold C 10.1038/NATURE18934 2016-07-20 Yes
CNR1 CB1 Cannabinoid A (Rhodopsin) Human 5TGZ_refined Inactive - 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
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human 3SN6_refined Active Gs T4-Lysozyme (-)-adrenaline
(-)-noradrenaline
small molecule BI-167107 pubchem
Agonist
small molecule
sponge mesophase Yes No Kobilka BK 10.1038/NATURE10361 2011-07-20 Yes
5HT1B 5-HT1B 5-Hydroxytryptamine A (Rhodopsin) Human - Active Go - - Donitriptan pubchem
Agonist
small molecule
Cryo-EM Yes No Tate CG 10.1038/S41586-018-0241-9 2018-06-20 Yes
5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human 6A93_refined Inactive - Soluble cytochrome b562 - Risperidone pubchem chembl_ligand
Antagonist
small molecule
N/A No No Shimamura T 10.1038/S41594-018-0180-Z 2019-02-13 Yes
5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human 6A94_refined Inactive - Soluble cytochrome b562 - Zotepine pubchem chembl_ligand
Antagonist
small molecule
N/A No No Shimamura T 10.1038/S41594-018-0180-Z 2019-02-13 Yes
Q9WTK1 BLT1 Leukotriene A (Rhodopsin) Guinea pig - Inactive - 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 C (Glutamate) Human 4OO9_refined Inactive - 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 A (Rhodopsin) Mouse 5C1M_refined Active - - 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) A (Rhodopsin) Zebrafish 5XSZ_refined Active - 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) A (Rhodopsin) Human 4MQT_refined Active - - 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
ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human 4MQS_refined Active - - acetylcholine
small molecule iperoxo pubchem
Agonist
small molecule
in meso/LCP Yes No Kobilka BK 10.1038/NATURE12735 2013-11-27 Yes
5HT2C 5-HT2C 5-Hydroxytryptamine A (Rhodopsin) Human - Inactive - 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
5HT2C 5-HT2C 5-Hydroxytryptamine A (Rhodopsin) Human - Active - 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
NK1R NK1 Tachykinin A (Rhodopsin) Human 6HLO_refined Inactive - 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 A (Rhodopsin) Human 6HLP_refined Inactive - 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
NK1R NK1 Tachykinin A (Rhodopsin) Human 6HLL_refined Inactive - 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
FFAR1 FFA1 Free fatty acid A (Rhodopsin) Human 5TZY_refined Intermediate - 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
FFAR1 FFA1 Free fatty acid A (Rhodopsin) Human 5TZR_refined Intermediate - 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
NPY1R Y1 Neuropeptide Y A (Rhodopsin) Human 5ZBQ_refined Inactive - 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 A (Rhodopsin) Human 5ZBH_refined Inactive - T4-Lysozyme - BMS-193885 pubchem
Antagonist
small molecule
N/A Yes No Wu B 10.1038/S41586-018-0046-X 2018-04-25 Yes
DRD2 D2 Dopamine A (Rhodopsin) Human 6CM4_refined Inactive - Endolysin - Risperidone pubchem chembl_ligand
Inverse agonist
small molecule
in meso/LCP Yes No Roth BL 10.1038/NATURE25758 2018-03-14 Yes
CNR2 CB2 Cannabinoid A (Rhodopsin) Human 5ZTY_refined Inactive - Endolysin - AM10257 pubchem
Antagonist
small molecule
N/A Yes No Liu Z 10.1016/J.CELL.2018.12.011 2019-01-30 Yes
AGTR2 AT2 Angiotensin A (Rhodopsin) Human 5UNG_refined Active - BRIL - CHEMBL289472 pubchem
Antagonist
small molecule
in meso/LCP Yes No Cherezov V 10.1038/NATURE22035 2017-04-05 Yes
AGTR2 AT2 Angiotensin A (Rhodopsin) Human 5UNH_refined Active - BRIL - 8EM pubchem
Antagonist
small molecule
in meso/LCP Yes No Cherezov V 10.1038/NATURE22035 2017-04-05 Yes
AGTR2 AT2 Angiotensin A (Rhodopsin) Human 5UNF_refined Active - BRIL - CHEMBL289472 pubchem
Antagonist
small molecule
in meso/LCP Yes No Cherezov V 10.1038/NATURE22035 2017-04-05 Yes
TA2R TP Prostanoid A (Rhodopsin) Human 6IIV_refined Inactive - 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
TA2R TP Prostanoid A (Rhodopsin) Human 6IIU_refined Inactive - 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
OPRK κ Opioid A (Rhodopsin) Human 4DJH_refined Inactive - 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 A (Rhodopsin) Human - Intermediate - 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
PTAFR PAF Platelet-activating factor A (Rhodopsin) Human 5ZKP_refined Active - Flavodoxin - Foropafant pubchem
Antagonist
small molecule
N/A Yes No Wu B 10.1038/S41594-018-0068-Y 2018-06-20 Yes
HRH1 H1 Histamine A (Rhodopsin) Human 3RZE_refined Inactive - 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 A (Rhodopsin) Human 5DHH_refined Inactive - 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 A (Rhodopsin) Human 5DHG_refined Inactive - 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) A (Rhodopsin) Human 5ZKC_refined Inactive - 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) A (Rhodopsin) Human 5YC8_refined Inactive - 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) A (Rhodopsin) Human - Inactive - 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) A (Rhodopsin) Human 5ZK8_refined Inactive - 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
ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human 5ZK3_refined Inactive - 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
5HT2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human 5TUD_refined Active - BRIL 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 A (Rhodopsin) Human 5NDZ_refined Intermediate - T4-Lysozyme
BRIL
- AZ3451 pubchem
Antagonist
small molecule
in meso/LCP Yes Yes Dekker N 10.1038/NATURE22309 2017-05-03 Yes
PAR2 PAR2 Proteinase-activated A (Rhodopsin) Human 5NDD_refined Intermediate - 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 A (Rhodopsin) Human - Intermediate - BRIL
Fab3949
- N/A N/A N/A in meso/LCP Yes No Dekker N 10.1038/NATURE22309 2017-05-03 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human - Intermediate - - - 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 A (Rhodopsin) Human 4UHR_refined Intermediate - - - 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 A (Rhodopsin) Human - Inactive - 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
ACM3 M3 Acetylcholine (muscarinic) A (Rhodopsin) Rat - Inactive - 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) A (Rhodopsin) Rat 4U15_refined Inactive - 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) A (Rhodopsin) Rat 4U16_refined Inactive - 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 A (Rhodopsin) Human 6B73_refined Active - Soluble cytochrome b562 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 A (Rhodopsin) Japanese flying squid 2Z73_refined Inactive - - retinal
small molecule retinal gtoplig
Inverse agonist
small molecule
vapour diffusion Yes No Kouyama T 10.1038/NATURE06925 2008-05-13 Yes
Q98SW5 SMO Frizzled F (Frizzled) African clawed frog 6D32_refined Inactive - 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
Q98SW5 SMO Frizzled F (Frizzled) African clawed frog 6D35_refined Inactive - 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
PE2R3 EP3 Prostanoid A (Rhodopsin) Human 6AK3_refined Active - Soluble cytochrome b562 - Prostaglandin E2 pubchem chembl_ligand
Agonist
small molecule
N/A Yes No Kobayashi T 10.1038/S41589-018-0171-8 2018-12-05 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine 5EN0_refined Active 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 A (Rhodopsin) Bovine 5DYS_refined Active - - 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 B1 (Secretin) Human 5VEX_refined Inactive - 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 B1 (Secretin) Human - Inactive - Endolysin - 97Y pubchem
Antagonist
small molecule
in meso/LCP No No Stevens RC 10.1038/NATURE22378 2017-05-24 Yes
PE2R4 EP4 Prostanoid A (Rhodopsin) Human 5YWY_refined Inactive - Fab - ONO-AE3-208 pubchem
Antagonist
small molecule
N/A No No Kobayashi T 10.1038/S41589-018-0131-3 2018-12-05 Yes
PE2R4 EP4 Prostanoid A (Rhodopsin) Human 5YHL_refined Inactive - Fab - ONO-AE3-208-Br
Antagonist
small molecule
N/A No No Kobayashi T 10.1038/S41589-018-0131-3 2018-12-05 Yes
AA1R A1 Adenosine A (Rhodopsin) Human 5UEN_refined Inactive - 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) A (Rhodopsin) Human 4Z34_refined Inactive - 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) A (Rhodopsin) Human 4Z36_refined Inactive - 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
LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human 4Z35_refined Inactive - 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
CXCR4 CXCR4 Chemokine A (Rhodopsin) Human 3ODU_refined Inactive - 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 A (Rhodopsin) Human - Inactive - 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 A (Rhodopsin) Human - Inactive - 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 A (Rhodopsin) Human - Inactive - 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 A (Rhodopsin) Human 3OE0_refined Inactive - 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 A (Rhodopsin) Human - Inactive - - - NDT 9513727 pubchem
Antagonist
small molecule
in meso/LCP Yes No Marshall FH 10.1038/NATURE25025 2018-01-10 Yes
CCR9 CCR9 Chemokine A (Rhodopsin) Human - Inactive - - - Vercirnon pubchem
Antagonist
small molecule
in meso/LCP No No Marshall FH 10.1038/NATURE20606 2016-12-07 Yes
DRD3 D3 Dopamine A (Rhodopsin) Human 3PBL_refined Inactive - 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 B1 (Secretin) Human 5XF1_refined Inactive - T4-Lysozyme - 4-{[(4-Cyclohexylphe... pubchem
Antagonist
small molecule
in meso/LCP No No Wu B 10.1038/NATURE22363 2017-05-24 Yes
GLR glucagon Glucagon B1 (Secretin) Human 5XEZ_refined Inactive - T4-Lysozyme - 4-{[(4-Cyclohexylphe... pubchem
Antagonist
small molecule
in meso/LCP No No Wu B 10.1038/NATURE22363 2017-05-24 Yes
APJ apelin Apelin A (Rhodopsin) Human 5VBL_refined Inactive - 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 A (Rhodopsin) Human 5WIV_refined Inactive - BRIL - Nemonapride pubchem
Antagonist
small molecule
in meso/LCP Yes Yes Roth BL 10.1126/SCIENCE.AAN5468 2017-10-18 Yes
DRD4 D4 Dopamine A (Rhodopsin) Human 5WIU_refined Inactive - - - Nemonapride pubchem
Antagonist
small molecule
in meso/LCP Yes No Roth BL 10.1126/SCIENCE.AAN5468 2017-10-18 Yes
CNR1 CB1 Cannabinoid A (Rhodopsin) Human 6N4B_refined Active Gi scFv16 2-arachidonoylglycerol
Endocannabinoid Fub-mdmb pubchem
Agonist
small molecule
N/A Yes No Skiniotis G 10.1016/J.CELL.2018.11.040 2019-01-30 Yes
AA1R A1 Adenosine A (Rhodopsin) Human 6D9H_refined Active 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 B1 (Secretin) Rabbit 5VAI_refined Active 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 B1 (Secretin) Human 6B3J_refined Active Gs - - Exendin-P5
Agonist
peptide
Cryo-EM No No Wootten D 10.1038/NATURE25773 2018-02-21 Yes
CRFR1 CRF1 Corticotropin-releasing factor B1 (Secretin) Human 4Z9G_refined Inactive - 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 A (Rhodopsin) Human 4NTJ_refined Intermediate - BRIL - AZD1283 pubchem
Antagonist
small molecule
in meso/LCP Yes No Zhao Q 10.1038/NATURE13083 2014-03-26 Yes
OX1R OX1 Orexin A (Rhodopsin) Human 4ZJC_refined Inactive - - 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 A (Rhodopsin) Human 4ZJ8_refined Inactive - - 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 B1 (Secretin) Human 6FJ3_refined Inactive - 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 A (Rhodopsin) Rat 4XEE_refined Intermediate - T4-Lysozyme neurotensin
peptide CHEMBL342252 pubchem
Agonist
peptide
in meso/LCP Yes No Grisshammer R 10.1038/NCOMMS8895 2015-07-29 Yes
NTR1 NTS1 Neurotensin A (Rhodopsin) Rat 4XES_refined Intermediate - T4-Lysozyme neurotensin
peptide CHEMBL342252 pubchem
Agonist
peptide
in meso/LCP Yes No Grisshammer R 10.1038/NCOMMS8895 2015-07-29 Yes
FZD4 FZD4 Frizzled F (Frizzled) Human 6BD4_refined Inactive - Rubredoxin - N/A N/A N/A N/A No No Xu F 10.1038/S41586-018-0447-X 2018-08-22 Yes
AGTR1 AT1 Angiotensin A (Rhodopsin) Human - Inactive - 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 A (Rhodopsin) Rat - Inactive - - neurotensin
peptide CHEMBL342252 pubchem
Agonist
peptide
vapour diffusion Yes No Plückthun A 10.1073/PNAS.1317903111 2014-01-29 No
NTR1 NTS1 Neurotensin A (Rhodopsin) Rat - Inactive - - neurotensin
peptide CHEMBL342252 pubchem
Agonist
peptide
vapour diffusion Yes No Plückthun A 10.1073/PNAS.1317903111 2014-01-29 Yes
NTR1 NTS1 Neurotensin A (Rhodopsin) Rat - Inactive - - neurotensin
peptide CHEMBL342252 pubchem
Agonist
peptide
vapour diffusion Yes No Plückthun A 10.1073/PNAS.1317903111 2014-01-29 No
NTR1 NTS1 Neurotensin A (Rhodopsin) Rat - Inactive - - neurotensin
peptide CHEMBL342252 pubchem
Agonist
peptide
vapour diffusion Yes No Plückthun A 10.1073/PNAS.1317903111 2014-01-29 No
OPRD δ Opioid A (Rhodopsin) Mouse 4EJ4_refined Inactive - 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 A (Rhodopsin) Human 5UIW_refined Inactive - 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
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - Inactive - - 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
US28 US28 Unclassified A (Rhodopsin) strain AD169 4XT3_refined Active - - CX3CL1
peptide Fractalkine
Agonist
peptide
in meso/LCP Yes No Garcia KC 10.1126/SCIENCE.AAA5026 2015-03-04 Yes
US28 US28 Unclassified A (Rhodopsin) strain AD169 4XT1_refined Active - - CX3CL1
peptide CX3CL1
Agonist
peptide
in meso/LCP Yes No Garcia KC 10.1126/SCIENCE.AAA5026 2015-03-04 Yes
S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human 3V2Y_refined Inactive - 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) A (Rhodopsin) Human - Inactive - 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 A (Rhodopsin) Human 4IB4_refined Intermediate - BRIL 5-hydroxytryptamine
small molecule ERGOTAMINE pubchem
Agonist
small molecule
in meso/LCP Yes No 10.1126/SCIENCE.1232808 2013-03-13 Yes
GRM1 mGlu1 Metabotropic glutamate C (Glutamate) Human 4OR2_refined Inactive - 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
AA2AR A2A Adenosine A (Rhodopsin) Human - Inactive - - - ZM241385 pubchem
Antagonist
small molecule
vapour diffusion Yes No Murata T 10.1038/NATURE10750 2012-02-01 No
AA2AR A2A Adenosine A (Rhodopsin) Human 3VG9_refined Inactive - - - ZM241385 pubchem
Antagonist
small molecule
vapour diffusion Yes No Murata T 10.1038/NATURE10750 2012-02-01 Yes
OPRM μ Opioid A (Rhodopsin) Mouse 4DKL_refined Inactive - 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
OPSD Rhodopsin Opsins A (Rhodopsin) Human 4ZWJ_refined Active - 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
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey - Active - Thioredoxin 1 - ISOPRENALINE pubchem
Agonist
small molecule
N/A Yes No Tate CG 10.1101/436212 2018-10-17 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey 6H7O_refined Active - Thioredoxin 1 - 4-{[(2S)-3-(tert-but... pubchem
Agonist
small molecule
N/A Yes No Tate CG 10.1101/436212 2018-10-17 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey 6H7N_refined Active - Thioredoxin 1 - Xamoterol pubchem
Agonist
small molecule
N/A Yes No Tate CG 10.1101/436212 2018-10-17 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey 6H7L_refined Active - Thioredoxin 1 - DOBUTAMINE pubchem
Agonist
small molecule
N/A Yes No Tate CG 10.1101/436212 2018-10-17 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey 6H7M_refined Active - Thioredoxin 1 - SALBUTAMOL pubchem
Agonist
small molecule
N/A Yes No Tate CG 10.1101/436212 2018-10-17 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey - Inactive - - - 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 A (Rhodopsin) Common turkey - Inactive - - - (S)-Carvedilol pubchem
Inverse agonist
small molecule
vapour diffusion Yes No Tate CG 10.1016/J.STR.2012.03.014 2012-05-23 Yes
5HT1B 5-HT1B 5-Hydroxytryptamine A (Rhodopsin) Human 4IAQ_refined Intermediate - BRIL - dihydroergotamine pubchem
Agonist
small molecule
in meso/LCP Yes No 10.1126/SCIENCE.1232807 2013-03-13 Yes
5HT1B 5-HT1B 5-Hydroxytryptamine A (Rhodopsin) Human 4IAR_refined Intermediate - BRIL - ERGOTAMINE pubchem
Agonist
small molecule
in meso/LCP Yes No 10.1126/SCIENCE.1232807 2013-03-13 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey - Inactive - - - Carmoterol pubchem
Agonist
small molecule
vapour diffusion Yes No Tate CG 10.1038/NATURE09746 2011-01-12 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey 2Y00_refined Inactive - - - Dobutamine pubchem
Agonist (partial)
small molecule
vapour diffusion Yes No Tate CG 10.1038/NATURE09746 2011-01-12 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey 2Y03_refined Inactive - - - LEVISOPRENALINE pubchem
Agonist
small molecule
vapour diffusion Yes No Tate CG 10.1038/NATURE09746 2011-01-12 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey - Inactive - - - Dobutamine pubchem
Agonist (partial)
small molecule
vapour diffusion Yes No Tate CG 10.1038/NATURE09746 2011-03-30 No
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey 2Y04_refined Inactive - - - Levalbuterol pubchem
Agonist (partial)
small molecule
vapour diffusion Yes No Tate CG 10.1038/NATURE09746 2011-01-12 Yes
EDNRB ETB Endothelin A (Rhodopsin) Human 6IGK_refined Intermediate - 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 A (Rhodopsin) Human 6IGL_refined Inactive - Endolysin - IRL1620 pubchem
Partial agonist
peptide
N/A Yes No Nureki O 10.1038/S41467-018-07094-0 2018-11-21 Yes
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human 3PDS_refined Inactive - 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
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human 3NY8_refined Inactive - 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 A (Rhodopsin) Human - Inactive - 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
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - Inactive - 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
AA2AR A2A Adenosine A (Rhodopsin) Human 5IU4_refined Inactive - 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 A (Rhodopsin) Human 5IU7_refined Inactive - 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 A (Rhodopsin) Human 5IUB_refined Inactive - BRIL - CHEMBL184061 pubchem
Agonist
small molecule
in meso/LCP Yes Yes Cooke RM 10.1021/ACS.JMEDCHEM.6B00653 2016-06-29 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human - Inactive - 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
CCR5 CCR5 Chemokine A (Rhodopsin) Human 6AKY_refined Inactive - 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
CCR5 CCR5 Chemokine A (Rhodopsin) Human 6AKX_refined Inactive - 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
AA2AR A2A Adenosine A (Rhodopsin) Human 5OLV_refined Inactive - 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 A (Rhodopsin) Human 5OM1_refined Inactive - 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 A (Rhodopsin) Human 5OLH_refined Inactive - Soluble cytochrome b562 - Vipadenant
Antagonist
small molecule
in meso/LCP Yes Yes Doré AS 10.1038/S41598-017-18570-W 2018-01-17 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human 5OLZ_refined Inactive - 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 A (Rhodopsin) Human - Inactive - 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 A (Rhodopsin) Human - Inactive - Soluble cytochrome b562 - ZM241385 pubchem
Antagonist
small molecule
in meso/LCP Yes Yes Doré AS 10.1038/S41598-017-18570-W 2018-01-17 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human 5OLO_refined Inactive - 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
CNR1 CB1 Cannabinoid A (Rhodopsin) Human 5XR8_refined Active - 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 A (Rhodopsin) Human 5XRA_refined Active - Flavodoxin 2-arachidonoylglycerol
Endocannabinoid CHEMBL1683648 pubchem
Agonist
small molecule
in meso/LCP Yes No Liu Z 10.1038/NATURE23272 2017-07-12 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human 5VRA_refined Inactive - Soluble cytochrome b562 - ZM241385 pubchem
Antagonist
small molecule
in meso/LCP Yes Yes Ernst OP 10.1038/NPROT.2017.135 2017-12-13 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine 5WKT_refined Active 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
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - Inactive - - 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 A (Rhodopsin) Bovine - Inactive - - 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 A (Rhodopsin) Bovine - Inactive - - retinal
small molecule retinal gtoplig
Inverse agonist
small molecule
vapour diffusion No No Okada T 10.1529/BIOPHYSJ.107.108225 2007-10-30 No
OPRD δ Opioid A (Rhodopsin) Human - Inactive - 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
OPRD δ Opioid A (Rhodopsin) Human 4RWD_refined Inactive - 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
CCR2 CCR2 Chemokine A (Rhodopsin) Human 6GPX_refined Inactive - 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 A (Rhodopsin) Human 6GPS_refined Inactive - Rubredoxin - MK-0812 pubchem
Antagonist
small molecule
N/A No No Schnapp G 10.1016/J.STR.2018.10.027 2019-01-02 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human - Inactive - BRIL - ZM241385 pubchem
Antagonist
small molecule
in meso/LCP Yes Yes Cherezov V 10.1126/SCIADV.1600292 2016-09-21 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human 5K2A_refined Inactive - BRIL - ZM241385 pubchem
Antagonist
small molecule
in meso/LCP Yes Yes Cherezov V 10.1126/SCIADV.1600292 2016-09-21 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human 5K2C_refined Inactive - BRIL - ZM241385 pubchem
Antagonist
small molecule
in meso/LCP Yes Yes Cherezov V 10.1126/SCIADV.1600292 2016-09-21 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human 5K2D_refined Inactive - BRIL - ZM241385 pubchem
Antagonist
small molecule
in meso/LCP Yes Yes Cherezov V 10.1126/SCIADV.1600292 2016-09-21 Yes
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human 2RH1_refined Inactive - 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 A (Rhodopsin) Human 6MXT_refined Active - Endolysin (-)-adrenaline
(-)-noradrenaline
small molecule Salmeterol pubchem
Agonist
small molecule
N/A Yes No Kobilka BK 10.1038/S41589-018-0145-X 2018-11-14 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human - Inactive - - - T4E
Antagonist
small molecule
vapour diffusion Yes No Marshall FH 10.1021/JM201376W 2012-03-21 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human - Inactive - - - CHEMBL2024115 pubchem
Antagonist
small molecule
vapour diffusion Yes No Marshall FH 10.1021/JM201376W 2012-03-21 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine 4J4Q_refined Active 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 A (Rhodopsin) Human 5N2R_refined Inactive - BRIL - PSB36 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 A (Rhodopsin) Human 5N2S_refined Inactive - - - PSB36 pubchem
Agonist
small molecule
in meso/LCP Yes No Cooke RM 10.1016/J.STR.2017.06.012 2017-07-26 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human 5MZJ_refined Inactive - - - 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 A (Rhodopsin) Human 5MZP_refined Inactive - - - Caffeine 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 A (Rhodopsin) Bovine - Inactive - - retinal
small molecule 10,20-Methanoretinal pubchem
Agonist
small molecule
vapour diffusion No No Palczewski K 10.1073/PNAS.1617446114 2017-03-15 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine 5TE3_refined Active - - retinal
small molecule N/A N/A N/A vapour diffusion No No Palczewski K 10.1073/PNAS.1617446114 2017-03-15 Yes
NK1R NK1 Tachykinin A (Rhodopsin) Human - Inactive - Endolysin - Aprepitant pubchem chembl_ligand
Antagonist
small molecule
N/A Yes No Zhao Q 10.1038/S41467-019-08568-5 2019-03-06 Yes
NK1R NK1 Tachykinin A (Rhodopsin) Human 6J20_refined Inactive - Endolysin - Aprepitant pubchem chembl_ligand
Antagonist
small molecule
N/A No No Zhao Q 10.1038/S41467-019-08568-5 2019-03-06 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human 4EIY_refined Inactive - BRIL - ZM241385 pubchem
Antagonist
small molecule
in meso/LCP Yes Yes Stevens RC 10.1126/SCIENCE.1219218 2012-07-25 Yes
SMO SMO Frizzled F (Frizzled) Human 5V57_refined Inactive - 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 F (Frizzled) Human 5V56_refined Inactive - 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 A (Rhodopsin) Japanese flying squid - Inactive - - 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 A (Rhodopsin) Japanese flying squid - Inactive - - 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 A (Rhodopsin) Common turkey - Inactive - - - (S)-Cyanopindolol pubchem
Antagonist
small molecule
vapour diffusion Yes No Schertler GFX 10.1073/PNAS.1100185108 2011-06-01 No
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey - Inactive - - - (S)-Cyanopindolol pubchem
Antagonist
small molecule
vapour diffusion Yes No Schertler GFX 10.1073/PNAS.1100185108 2011-06-08 No
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey - Inactive - - - timolol pubchem
Antagonist
small molecule
vapour diffusion Yes No Schertler GFX 10.1073/PNAS.1100185108 2011-06-01 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey 2YCW_refined Inactive - - - timolol pubchem
Inverse agonist
small molecule
vapour diffusion Yes No Schertler GFX 10.1073/PNAS.1100185108 2011-06-01 Yes
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - Inactive - 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 A (Rhodopsin) Human - Inactive - 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 A (Rhodopsin) Human 6AQF_refined Inactive - Soluble cytochrome b562 - ZM241385 pubchem
Antagonist
small molecule
in meso/LCP Yes No Wüthrich K 10.1016/J.CELL.2017.12.004 2018-01-10 Yes
CRFR1 CRF1 Corticotropin-releasing factor B1 (Secretin) Human 4K5Y_refined Inactive - 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
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey 5F8U_refined Inactive - - - (S)-Cyanopindolol pubchem
Antagonist
small molecule
vapour diffusion Yes No Tate CG 10.1038/NSMB.3130 2015-12-23 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human 2YDV_refined Intermediate - - - NECA pubchem
Agonist
small molecule
vapour diffusion Yes No Tate CG 10.1038/NATURE10136 2011-05-18 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human 2YDO_refined Intermediate - - - adenosine pubchem
Agonist
small molecule
vapour diffusion Yes No Tate CG 10.1038/NATURE10136 2011-05-18 Yes
5HT2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human 6DRZ_refined Intermediate - 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 A (Rhodopsin) Human 6DS0_refined Intermediate - 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 A (Rhodopsin) Human 6DRY_refined Intermediate - 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 A (Rhodopsin) Human 6DRX_refined Intermediate - 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
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine 6FKB_refined Active - - 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 A (Rhodopsin) Bovine 6FK9_refined Active - - 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 A (Rhodopsin) Bovine 6FKD_refined Active - - 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 A (Rhodopsin) Bovine 6FK7_refined Active - - 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 A (Rhodopsin) Bovine - Active - - 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 A (Rhodopsin) Bovine 6FK8_refined Active - - 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 A (Rhodopsin) Bovine 6FKA_refined Active - - 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
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey - Inactive - - - (S)-Cyanopindolol pubchem
Antagonist
small molecule
vapour diffusion Yes No Schertler GFX 10.1038/NATURE07101 2008-06-24 No
AA2AR A2A Adenosine A (Rhodopsin) Human - Inactive - - - 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 A (Rhodopsin) Human 3REY_refined Inactive - - - 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 A (Rhodopsin) Human - Inactive - - - 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 A (Rhodopsin) Human - Intermediate - BRIL - 2-MeSADP pubchem
Agonist
small molecule
in meso/LCP Yes No Zhao Q 10.1038/NATURE13288 2014-04-30 Yes
P2Y12 P2Y12 P2Y A (Rhodopsin) Human 4PY0_refined Intermediate - 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 A (Rhodopsin) Human - Inactive - - (-)-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 A (Rhodopsin) Human - Inactive - - (-)-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 A (Rhodopsin) Human - Active - T4-Lysozyme (-)-adrenaline
(-)-noradrenaline
small molecule hydroxybenzylisoprot... pubchem
Agonist
small molecule
in meso/LCP Yes No Kobilka BK 10.1038/NATURE12572 2013-09-25 Yes
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human 4LDE_refined Active - T4-Lysozyme (-)-adrenaline
(-)-noradrenaline
small molecule BI167107 pubchem
Agonist
small molecule
in meso/LCP Yes No Kobilka BK 10.1038/NATURE12572 2013-09-25 Yes
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human 4LDO_refined Active - T4-Lysozyme (-)-adrenaline
(-)-noradrenaline
small molecule epinephrine pubchem
Agonist
small molecule
in meso/LCP Yes No Kobilka BK 10.1038/NATURE12572 2013-09-25 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - Active - - 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 B1 (Secretin) Human 4L6R_refined Inactive - BRIL - N/A N/A N/A in meso/LCP No No Stevens RC 10.1038/NATURE12393 2013-07-24 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine - Inactive - - retinal
small molecule retinal