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RECEPTOR STRUCTURE SIGNAL PROTEIN AUXILIARY PROTEIN STRUCTURE LIGAND ENDOGENOUS LIGAND SODIUM ION SITE REFERENCE ANNOTATED
PDB Refined
structure
Resolution Preferred
chain
7TM Open IC (Å) % of Seq PDB Date
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5G53 5G53_refined 3.4 A Active 9.8 Gs Gs Engineered G protein 50 - - NECA pubchem
small molecule Agonist - Yes No Tate CG 10.1038/NATURE18966 2016-08-03 Yes
CNR1 CB1 Cannabinoid A (Rhodopsin) Human X-ray 5TGZ 5TGZ_refined 2.8 A Inactive -0.9 - - - - Flavodoxin - SCHEMBL662960 pubchem
small molecule Antagonist 2-arachidonoylglycer... Endocannabinoid Yes No Liu Z 10.1016/J.CELL.2016.10.004 2016-11-02 Yes
ACM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human X-ray 5DSG 5DSG_refined 2.6 B Inactive 0.3 - - - - T4-Lysozyme - Tiotropium pubchem
small molecule Antagonist acetylcholine small molecule Yes No Christopoulos A 10.1038/NATURE17188 2016-03-16 Yes
ACM1 M1 Acetylcholine (muscarinic) A (Rhodopsin) Human X-ray 5CXV 5CXV_refined 2.7 A Inactive 0.6 - - - - Endolysin - CHEMBL258622 pubchem
small molecule Antagonist acetylcholine small molecule Yes No Christopoulos A 10.1038/NATURE17188 2016-03-09 Yes
OX2R OX2 Orexin A (Rhodopsin) Human X-ray 5WQC 5WQC_refined 2.0 A Inactive -1.0 - - - - Glycogen synthase - EMPA pubchem chembl_ligand
small molecule Antagonist - Yes No Kobayashi T 10.1016/J.STR.2017.11.005 2017-11-29 Yes
OX2R OX2 Orexin A (Rhodopsin) Human X-ray 5WS3 - 2.3 A Inactive -1.1 - - - - Glycogen synthase - EMPA pubchem chembl_ligand
small molecule Antagonist - Yes No Kobayashi T 10.1016/J.STR.2017.11.005 2017-12-13 Yes
NTR1 NTS1 Neurotensin A (Rhodopsin) Human cryo-EM 6OSA 6OSA_refined 3.0 R Intermediate 6.2 Gi/o Gi1 Non-canonical confor... 62 - - JMV449 pubchem
Peptide Agonist - Yes No Skiniotis G 10.1038/S41586-019-1337-6 2019-07-10 Yes
NTR1 NTS1 Neurotensin A (Rhodopsin) Human cryo-EM 6OS9 6OS9_refined 3.0 R Intermediate 7.0 Gi/o Gi1 - 62 scFv16 - JMV449 pubchem
Peptide Agonist - Yes No Skiniotis G 10.1038/S41586-019-1337-6 2019-07-10 Yes
PAR1 PAR1 Proteinase-activated A (Rhodopsin) Human X-ray 3VW7 3VW7_refined 2.2 A Intermediate 6.2 - - - - T4-Lysozyme - Vorapaxar pubchem
small molecule Antagonist Thrombin Peptide Yes No Kobilka BK 10.1038/NATURE11701 2012-12-12 Yes
NTR1 NTS1 Neurotensin A (Rhodopsin) Rat X-ray 5T04 5T04_refined 3.3 A Active 8.3 - - - - T4-Lysozyme - CHEMBL342252 pubchem
Peptide Agonist neurotensin Peptide Yes No Grisshammer R 10.1038/SREP38564 2016-12-21 Yes
CALRL calcitonin-like Calcitonin B1 (Secretin) Human cryo-EM 6E3Y 6E3Y_refined 3.3 R Active 6.9 - - - - Receptor activity-modifying protein 1 Nanobody 35 Calcitonin gene-rela... pubchem
Peptide Agonist - No No Sexton PM 10.1038/S41586-018-0535-Y 2018-09-19 Yes
OPRD δ Opioid A (Rhodopsin) Human X-ray 4N6H 4N6H_refined 1.8 A Inactive -1.5 - - - - BRIL - Naltrindole pubchem
small molecule Antagonist β-endorphin, dy... Peptide Yes Yes Stevens RC 10.1038/NATURE12944 2013-12-25 Yes
Q80KM9 US28 Unclassified A (Rhodopsin) strain AD169 X-ray 5WB2 5WB2_refined 3.5 A Active 8.9 - - - - - Nanobody CX3CL1
Peptide Agonist - Yes No Garcia KC 10.7554/ELIFE.35850 2018-06-13 Yes
Q80KM9 US28 Unclassified A (Rhodopsin) strain AD169 X-ray 5WB1 5WB1_refined 3.5 A Active 9.1 - - - - - Nanobody N/A N/A N/A - Yes No Garcia KC 10.7554/ELIFE.35850 2018-06-13 Yes
EDNRB ETB Endothelin A (Rhodopsin) Human X-ray 5X93 5X93_refined 2.2 A Inactive -0.7 - - - - Endolysin - K-8794 pubchem
small molecule Antagonist - Yes No Nureki O 10.1038/NSMB.3450 2017-08-16 Yes
EDNRB ETB Endothelin A (Rhodopsin) Human X-ray 5XPR 5XPR_refined 3.6 A Inactive 0.1 - - - - - - N/A N/A N/A - Yes No Nureki O 10.1038/NSMB.3450 2017-08-16 Yes
PE2R3 EP3 Prostanoid A (Rhodopsin) Human X-ray 6M9T 6M9T_refined 2.5 A Intermediate 7.1 - - - - Endolysin chimera - misoprostol-FA pubchem
small molecule Antagonist - Yes No Stevens RC 10.1038/S41589-018-0160-Y 2018-12-05 Yes
GLP1R GLP-1 Glucagon B1 (Secretin) Human X-ray 5NX2 5NX2_refined 3.7 A Intermediate 4.9 - - - - - - truncated protein ag...
Peptide Agonist - No No Marshall FH 10.1038/NATURE22800 2017-06-14 Yes
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human X-ray 5JQH 5JQH_refined 3.2 A Inactive -1.1 - - - - T4-Lysozyme Nanobody Carazolol pubchem
small molecule Inverse agonist (-)-adrenaline, (-)-... small molecule Yes No Lefkowitz RJ 10.1038/NATURE18636 2016-07-13 Yes
SMO SMO Frizzled F (Frizzled) Human X-ray 5L7D 5L7D_refined 3.2 B Inactive -2.0 - - - - BRIL - N/A N/A N/A constitutive Constitutive No No Siebold C 10.1038/NATURE18934 2016-07-20 Yes
SMO SMO Frizzled F (Frizzled) Human X-ray 5L7I 5L7I_refined 3.3 B Inactive -2.3 - - - - BRIL - Vismodegib pubchem
small molecule Antagonist constitutive Constitutive No No Siebold C 10.1038/NATURE18934 2016-07-20 Yes
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human X-ray 3SN6 3SN6_refined 3.2 R Active 10.0 Gs Gs - 89 T4-Lysozyme Antibody BI-167107 pubchem
small molecule Agonist (-)-adrenaline, (-)-... small molecule Yes No Kobilka BK 10.1038/NATURE10361 2011-07-20 Yes
P2RY1 P2Y1 P2Y A (Rhodopsin) Human X-ray 4XNW 4XNW_refined 2.7 A Intermediate 5.2 - - - - Rubredoxin - MRS2500 pubchem
small molecule Antagonist ADP small molecule Yes No Wu B 10.1038/NATURE14287 2015-04-01 Yes
P2RY1 P2Y1 P2Y A (Rhodopsin) Human X-ray 4XNV 4XNV_refined 2.2 A Intermediate 5.6 - - - - Rubredoxin - BPTU pubchem
small molecule Antagonist ADP small molecule Yes No Wu B 10.1038/NATURE14287 2015-04-01 Yes
5HT1B 5-HT1B 5-Hydroxytryptamine A (Rhodopsin) Human cryo-EM 6G79 - 3.8 S Active 8.9 Gi/o Go - 59 - - Donitriptan pubchem
small molecule Agonist - Yes No Tate CG 10.1038/S41586-018-0241-9 2018-06-20 Yes
5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 6A93 6A93_refined 3.0 A Inactive -0.5 - - - - Soluble cytochrome b562 - Risperidone pubchem chembl_ligand
small molecule Antagonist - No No Shimamura T 10.1038/S41594-018-0180-Z 2019-02-13 Yes
5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 6A94 6A94_refined 2.9 A Inactive -0.8 - - - - Soluble cytochrome b562 - Zotepine pubchem chembl_ligand
small molecule Antagonist - No No Shimamura T 10.1038/S41594-018-0180-Z 2019-02-13 Yes
ACM1 M1 Acetylcholine (muscarinic) A (Rhodopsin) Human cryo-EM 6OIJ 6OIJ_refined 3.3 R Active 9.5 Gq/11 G11 - 63 - Antibody fragment Iperoxo pubchem
small molecule Agonist acetylcholine small molecule Yes No Kobilka BK 10.1126/SCIENCE.AAW5188 2019-05-08 Yes
ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human cryo-EM 6OIK 6OIK_refined 3.6 R Active 8.5 Gi/o Go - 61 - - LY2119620 pubchem
Iperoxo pubchem
small molecule
small molecule
Agonist acetylcholine small molecule Yes No Kobilka BK 10.1126/SCIENCE.AAW5188 2019-05-08 Yes
Q9WTK1 BLT1 Leukotriene A (Rhodopsin) Guinea pig X-ray 5X33 5X33_refined 3.7 A Inactive -1.5 - - - - Endolysin - BIIL-260 pubchem
small molecule Antagonist - Yes No Yokoyama S 10.1038/NCHEMBIO.2547 2018-01-03 Yes
GRM5 mGlu5 Metabotropic glutamate C (Glutamate) Human X-ray 4OO9 4OO9_refined 2.6 A Inactive 4.0 - - - - T4-Lysozyme - Mavoglurant pubchem
small molecule NAM L-glutamic acid small molecule No No Marshall FH 10.1038/NATURE13396 2014-07-02 Yes
OPRM μ Opioid A (Rhodopsin) Mouse X-ray 5C1M 5C1M_refined 2.1 A Active 11.0 - - - - - Antibody BU72 pubchem
small molecule Agonist β-endorphin, dy... Peptide Yes No Kobilka BK 10.1038/NATURE14886 2015-08-05 Yes
SMO SMO Frizzled F (Frizzled) Human cryo-EM 6OT0 6OT0_refined 3.9 R Active 5.1 Gi/o Gi1 - 100 Fab light chain
Fab heavy chain
- 24,25-Epoxy-choleste... pubchem
small molecule Agonist constitutive Constitutive No No Li X 10.1038/S41586-019-1286-0 2019-06-12 Yes
Q08BG4 LPA6 Lysophospholipid (LPA) A (Rhodopsin) Zebrafish X-ray 5XSZ 5XSZ_refined 3.2 A Active 10.0 - - - - Endolysin - N/A N/A N/A - Yes No Nureki O 10.1038/NATURE23448 2017-08-16 Yes
ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human X-ray 4MQT 4MQT_refined 3.7 A Active 8.7 - - - - - Nanobody LY2119620 pubchem
Iperoxo pubchem
small molecule
small molecule
PAM
Agonist
acetylcholine small molecule Yes No Kobilka BK 10.1038/NATURE12735 2013-11-27 Yes
ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human X-ray 4MQS 4MQS_refined 3.5 A Active 9.1 - - - - - Nanobody Iperoxo pubchem
small molecule Agonist acetylcholine small molecule Yes No Kobilka BK 10.1038/NATURE12735 2013-11-27 Yes
5HT2C 5-HT2C 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 6BQG - 3.0 A Active 7.9 - - - - Soluble cytochrome b562 - Ergotamine pubchem
small molecule Agonist - Yes No Liu Z 10.1016/J.CELL.2018.01.001 2018-02-14 Yes
5HT2C 5-HT2C 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 6BQH - 2.7 A Inactive 0.1 - - - - Soluble cytochrome b562 - Ritanserin pubchem
small molecule Inverse agonist - Yes No Liu Z 10.1016/J.CELL.2018.01.001 2018-02-14 Yes
NK1R NK1 Tachykinin A (Rhodopsin) Human X-ray 6HLP - 2.2 A Inactive 0.8 - - - - GIgA glycogen synthase - Netupitant pubchem chembl_ligand
small molecule Antagonist - Yes No Plückthun A 10.1038/S41467-018-07939-8 2019-01-16 Yes
NK1R NK1 Tachykinin A (Rhodopsin) Human X-ray 6HLL 6HLL_refined 3.3 A Inactive 1.1 - - - - GIgA glycogen synthase - CP-99,994 pubchem chembl_ligand
small molecule Antagonist - Yes No Plückthun A 10.1038/S41467-018-07939-8 2019-01-16 Yes
NK1R NK1 Tachykinin A (Rhodopsin) Human X-ray 6HLO 6HLO_refined 2.4 A Inactive 0.7 - - - - GIgA glycogen synthase - Aprepitant pubchem pubchem chembl_ligand
small molecule Antagonist - Yes No Plückthun A 10.1038/S41467-018-07939-8 2019-01-16 Yes
FFAR1 FFA1 Free fatty acid A (Rhodopsin) Human X-ray 5TZR 5TZR_refined 2.2 A Intermediate 3.7 - - - - Endolysin - UNII-11612L5SPI pubchem
small molecule Agonist long chain carboxyli... Lipid No No Soisson SM 10.1038/NSMB.3417 2017-06-07 Yes
FFAR1 FFA1 Free fatty acid A (Rhodopsin) Human X-ray 5TZY 5TZY_refined 3.2 A Intermediate 3.2 - - - - Endolysin - (2s,3r)-3-Cyclopropy... pubchem
UNII-11612L5SPI pubchem
small molecule
small molecule
Agonist long chain carboxyli... Lipid No No Soisson SM 10.1038/NSMB.3417 2017-06-07 Yes
NPY1R Y1 Neuropeptide Y A (Rhodopsin) Human X-ray 5ZBQ 5ZBQ_refined 2.7 A Inactive -1.3 - - - - T4-Lysozyme - UR-MK299 pubchem
small molecule Antagonist - Yes No Wu B 10.1038/S41586-018-0046-X 2018-04-25 Yes
NPY1R Y1 Neuropeptide Y A (Rhodopsin) Human X-ray 5ZBH 5ZBH_refined 3.0 A Inactive -0.7 - - - - T4-Lysozyme - BMS-193885 pubchem
small molecule Antagonist - Yes No Wu B 10.1038/S41586-018-0046-X 2018-04-25 Yes
DRD2 D2 Dopamine A (Rhodopsin) Human X-ray 6CM4 6CM4_refined 2.9 A Inactive -1.8 - - - - Endolysin - Risperidone pubchem chembl_ligand
small molecule Inverse agonist - Yes No Roth BL 10.1038/NATURE25758 2018-03-14 Yes
CNR2 CB2 Cannabinoid A (Rhodopsin) Human X-ray 5ZTY 5ZTY_refined 2.8 A Inactive -0.5 - - - - Endolysin - AM10257 pubchem
small molecule Antagonist - Yes No Liu Z 10.1016/J.CELL.2018.12.011 2019-01-30 Yes
AGTR2 AT2 Angiotensin A (Rhodopsin) Human X-ray 5UNH 5UNH_refined 2.9 B Active 9.2 - - - - BRIL - N-[(Furan-2-Yl)methy... pubchem
small molecule Antagonist - Yes No Cherezov V 10.1038/NATURE22035 2017-04-05 Yes
AGTR2 AT2 Angiotensin A (Rhodopsin) Human X-ray 5UNG - 2.8 B Active 8.5 - - - - BRIL - CHEMBL289472 pubchem
small molecule Antagonist - Yes No Cherezov V 10.1038/NATURE22035 2017-04-05 Yes
AGTR2 AT2 Angiotensin A (Rhodopsin) Human X-ray 5UNF 5UNF_refined 2.8 A Active 8.9 - - - - BRIL - CHEMBL289472 pubchem
small molecule Antagonist - Yes No Cherezov V 10.1038/NATURE22035 2017-04-05 Yes
TA2R TP Prostanoid A (Rhodopsin) Human X-ray 6IIV 6IIV_refined 3.0 A Inactive 1.0 - - - - Soluble cytochrome b562
Rubredoxin
- Daltroban pubchem chembl_ligand
small molecule Antagonist - No No Wu B 10.1038/S41589-018-0170-9 2018-12-19 Yes
TA2R TP Prostanoid A (Rhodopsin) Human X-ray 6IIU 6IIU_refined 2.5 A Inactive 1.0 - - - - Soluble cytochrome b562
Rubredoxin
- Ramatroban pubchem chembl_ligand
small molecule Antagonist - No No Wu B 10.1038/S41589-018-0170-9 2018-12-19 Yes
OPRK κ Opioid A (Rhodopsin) Human X-ray 4DJH 4DJH_refined 2.9 A Inactive -1.3 - - - - T4-Lysozyme - JDTic pubchem
small molecule Antagonist dynorphin A Peptide Yes No Stevens RC 10.1038/NATURE10939 2012-03-21 Yes
PTAFR PAF Platelet-activating factor A (Rhodopsin) Human X-ray 5ZKP 5ZKP_refined 2.8 A Active 15.3 - - - - Flavodoxin - Foropafant pubchem
small molecule Antagonist - Yes No Wu B 10.1038/S41594-018-0068-Y 2018-06-20 Yes
PTAFR PAF Platelet-activating factor A (Rhodopsin) Human X-ray 5ZKQ 5ZKQ_refined 2.9 B Intermediate 4.8 - - - - Endolysin - ABT-491 pubchem chembl_ligand
small molecule Inverse agonist - Yes No Wu B 10.1038/S41594-018-0068-Y 2018-06-20 Yes
HRH1 H1 Histamine A (Rhodopsin) Human X-ray 3RZE 3RZE_refined 3.1 A Inactive 0.5 - - - - T4-Lysozyme - doxepin pubchem
small molecule Antagonist histamine small molecule Yes No Iwata S 10.1038/NATURE10236 2011-06-15 Yes
OPRX NOP Opioid A (Rhodopsin) Human X-ray 5DHG 5DHG_refined 3.0 A Inactive -1.3 - - - - BRIL - N/A N/A N/A nociceptin/orphanin ... Peptide Yes No Stevens RC 10.1016/J.STR.2015.07.024 2015-10-21 Yes
OPRX NOP Opioid A (Rhodopsin) Human X-ray 5DHH 5DHH_refined 3.0 A Inactive -1.1 - - - - BRIL - N/A N/A N/A nociceptin/orphanin ... Peptide Yes No Stevens RC 10.1016/J.STR.2015.07.024 2015-10-21 Yes
ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human X-ray 5YC8 5YC8_refined 2.5 A Inactive 1.1 - - - - Redesigned apo-cytochrome b562 - N-methyl scopolamine pubchem
small molecule Antagonist acetylcholine small molecule No No Kobayashi T 10.1038/S41589-018-0152-Y 2018-11-21 Yes
ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human X-ray 5ZK3 5ZK3_refined 2.6 A Inactive 0.6 - - - - Apo-cytochrome b562 - Quinuclidinyl benzil... pubchem
small molecule Antagonist acetylcholine small molecule No No Kobayashi T 10.1038/S41589-018-0152-Y 2018-11-21 Yes
ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human X-ray 5ZK8 5ZK8_refined 3.0 A Inactive 1.0 - - - - Redesigned apo-cytochrome b562 - N-methyl scopolamine pubchem
small molecule Antagonist acetylcholine small molecule Yes No Kobayashi T 10.1038/S41589-018-0152-Y 2018-11-21 Yes
ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human X-ray 5ZKB 5ZKB_refined 3.0 A Inactive 1.0 - - - - Apo-cytochrome b562 - AF-DX 384 pubchem
small molecule Antagonist acetylcholine small molecule No No Kobayashi T 10.1038/S41589-018-0152-Y 2018-11-21 Yes
ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human X-ray 5ZKC 5ZKC_refined 2.3 A Inactive 0.8 - - - - Apo-cytochrome b562 - N-methyl scopolamine pubchem
small molecule Antagonist acetylcholine small molecule No No Kobayashi T 10.1038/S41589-018-0152-Y 2018-11-21 Yes
5HT2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 5TUD 5TUD_refined 3.0 D Active 8.7 - - - - BRIL Antibody Ergotamine pubchem
small molecule Agonist 5-hydroxytryptamine small molecule Yes No Cherezov V 10.1073/PNAS.1700891114 2017-07-26 Yes
PAR2 PAR2 Proteinase-activated A (Rhodopsin) Human X-ray 5NDZ 5NDZ_refined 3.6 A Intermediate 6.9 - - - - T4-Lysozyme
BRIL
- AZ3451 pubchem
small molecule Antagonist - Yes Yes Dekker N 10.1038/NATURE22309 2017-05-03 Yes
PAR2 PAR2 Proteinase-activated A (Rhodopsin) Human X-ray 5NJ6 5NJ6_refined 4.0 A Intermediate 7.1 - - - - BRIL
Fab3949
- N/A N/A N/A - Yes No Dekker N 10.1038/NATURE22309 2017-05-03 Yes
PAR2 PAR2 Proteinase-activated A (Rhodopsin) Human X-ray 5NDD 5NDD_refined 2.8 A Intermediate 7.1 - - - - T4-Lysozyme
BRIL
- (~{s})-(4-Fluoranyl-... pubchem
small molecule Antagonist - Yes Yes Dekker N 10.1038/NATURE22309 2017-05-03 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 4UG2 - 2.6 B Intermediate 5.9 - - - - - - Cgs 21680 pubchem
small molecule Agonist - Yes No Tate CG 10.1124/MOL.114.097360 2015-04-08 No
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 4UHR 4UHR_refined 2.6 A Intermediate 6.3 - - - - - - Cgs 21680 pubchem
small molecule Agonist - Yes No Tate CG 10.1124/MOL.114.097360 2015-04-08 Yes
CCR2 CCR2 Chemokine A (Rhodopsin) Human X-ray 5T1A 5T1A_refined 2.8 A Inactive 1.7 - - - - T4-Lysozyme - CCR2-RA-[R] pubchem
CHEMBL3577945 pubchem
small molecule
small molecule
Antagonist - No No Handel TM 10.1038/NATURE20605 2016-12-14 Yes
Q98SW5 SMO Frizzled F (Frizzled) African clawed frog X-ray 6D32 6D32_refined 3.8 A Inactive -2.2 - - - - Cytochrome b562 - Cyclopamine pubchem
small molecule Antagonist constitutive Constitutive No No Salic A 10.1016/J.CELL.2018.04.029 2018-05-23 Yes
Q98SW5 SMO Frizzled F (Frizzled) African clawed frog X-ray 6D35 6D35_refined 3.9 A Inactive -2.2 - - - - Cytochrome b562 - N/A N/A N/A constitutive Constitutive No No Salic A 10.1016/J.CELL.2018.04.029 2018-05-23 Yes
MTR1A MT1 Melatonin A (Rhodopsin) Human X-ray 6ME5 6ME5_refined 3.2 A Inactive -0.8 - - - - GlgA glycogen synthase - Agomelatine pubchem chembl_ligand
small molecule Agonist - No No Cherezov V 10.1038/S41586-019-1141-3 2019-04-24 Yes
MTR1A MT1 Melatonin A (Rhodopsin) Human X-ray 6ME3 6ME3_refined 2.9 A Inactive -0.7 - - - - GIgA glycogen synthase - 2-Phenylmelatonin pubchem
small molecule Agonist - No No Cherezov V 10.1038/S41586-019-1141-3 2019-04-24 Yes
MTR1A MT1 Melatonin A (Rhodopsin) Human X-ray 6ME2 6ME2_refined 2.8 A Inactive -0.6 - - - - GIgA glycogen synthase - Ramelteon pubchem chembl_ligand
small molecule Agonist - No No Cherezov V 10.1038/S41586-019-1141-3 2019-04-24 Yes
MTR1A MT1 Melatonin A (Rhodopsin) Human X-ray 6ME4 6ME4_refined 3.2 A Inactive -1.3 - - - - GlgA glycogen synthase - 2-Iodomelatonin pubchem chembl_ligand
small molecule Agonist - No No Cherezov V 10.1038/S41586-019-1141-3 2019-04-24 Yes
OPRK κ Opioid A (Rhodopsin) Human X-ray 6B73 6B73_refined 3.1 A Active 9.7 - - - - Soluble cytochrome b562 Nanobody MP1104 pubchem
small molecule Agonist dynorphin A Peptide Yes No Roth BL 10.1016/J.CELL.2017.12.011 2018-01-17 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Japanese flying squid X-ray 2Z73 2Z73_refined 2.5 A Inactive -0.3 - - - - - - retinal gtoplig
small molecule Inverse agonist retinal small molecule Yes No Kouyama T 10.1038/NATURE06925 2008-05-13 Yes
PE2R3 EP3 Prostanoid A (Rhodopsin) Human X-ray 6AK3 6AK3_refined 2.9 B Active 7.6 - - - - Soluble cytochrome b562 - Prostaglandin E2 pubchem chembl_ligand
small molecule Agonist - Yes No Kobayashi T 10.1038/S41589-018-0171-8 2018-12-05 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 5EN0 5EN0_refined 2.8 A Active 8.4 Gi/o Gt3 Only H5 3 - - retinal gtoplig
small molecule Inverse agonist retinal small molecule No No Standfuss J 10.15252/EMBR.201642671 2016-08-10 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 5DYS 5DYS_refined 2.3 A Active 7.7 - - - - - - retinal gtoplig
small molecule Inverse agonist retinal small molecule No No Standfuss J 10.15252/EMBR.201642671 2016-08-10 Yes
GLP1R GLP-1 Glucagon B1 (Secretin) Human X-ray 5VEW 5VEW_refined 2.7 A Inactive -5.1 - - - - Endolysin - N-{4-[(R)-(3,3-Dimet... pubchem
small molecule Antagonist - No No Stevens RC 10.1038/NATURE22378 2017-05-24 Yes
GLP1R GLP-1 Glucagon B1 (Secretin) Human X-ray 5VEX 5VEX_refined 3.0 B Inactive -5.1 - - - - Endolysin - 4-{[(4-Cyclohexylphe... pubchem
small molecule Antagonist - No No Stevens RC 10.1038/NATURE22378 2017-05-17 Yes
PE2R4 EP4 Prostanoid A (Rhodopsin) Human X-ray 5YWY 5YWY_refined 3.2 A Inactive -1.0 - - - - Fab - ONO-AE3-208 pubchem
small molecule Antagonist - No No Kobayashi T 10.1038/S41589-018-0131-3 2018-12-05 Yes
PE2R4 EP4 Prostanoid A (Rhodopsin) Human X-ray 5YHL 5YHL_refined 4.2 A Inactive -0.9 - - - - Fab - ONO-AE3-208-Br
small molecule Antagonist - No No Kobayashi T 10.1038/S41589-018-0131-3 2018-12-05 Yes
AA1R A1 Adenosine A (Rhodopsin) Human X-ray 5UEN 5UEN_refined 3.2 B Inactive -1.1 - - - - BRIL - CHEMBL144360 pubchem
small molecule Antagonist - Yes No Christopoulos A 10.1016/J.CELL.2017.01.042 2017-03-01 Yes
LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human X-ray 4Z35 4Z35_refined 2.9 A Inactive -1.3 - - - - BRIL - ONO-9910539 pubchem
small molecule Antagonist LPA Lipid Yes No Hanson MA 10.1016/J.CELL.2015.06.002 2015-06-03 Yes
LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human X-ray 4Z34 4Z34_refined 3.0 A Inactive -1.3 - - - - BRIL - ONO-9780307 pubchem
small molecule Antagonist LPA Lipid Yes No Hanson MA 10.1016/J.CELL.2015.06.002 2015-06-03 Yes
LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human X-ray 4Z36 4Z36_refined 2.9 A Inactive -1.2 - - - - BRIL - ONO-3080573 pubchem
small molecule Antagonist LPA Lipid Yes No Hanson MA 10.1016/J.CELL.2015.06.002 2015-06-03 Yes
CXCR4 CXCR4 Chemokine A (Rhodopsin) Human X-ray 3OE8 - 3.1 A Inactive -1.3 - - - - T4-Lysozyme - IT1t pubchem
small molecule Antagonist CXCL12α, CXCL1... Peptide Yes No Stevens RC 10.1126/SCIENCE.1194396 2010-10-27 No
CXCR4 CXCR4 Chemokine A (Rhodopsin) Human X-ray 3OE9 - 3.1 A Inactive -0.7 - - - - T4-Lysozyme - IT1t pubchem
small molecule Antagonist CXCL12α, CXCL1... Peptide Yes No Stevens RC 10.1126/SCIENCE.1194396 2010-10-27 No
CXCR4 CXCR4 Chemokine A (Rhodopsin) Human X-ray 3OE6 - 3.2 A Inactive -1.3 - - - - T4-Lysozyme - IT1t pubchem
small molecule Antagonist CXCL12α, CXCL1... Peptide Yes No Stevens RC 10.1126/SCIENCE.1194396 2010-10-27 No
CXCR4 CXCR4 Chemokine A (Rhodopsin) Human X-ray 3ODU 3ODU_refined 2.5 A Inactive -1.3 - - - - T4-Lysozyme - IT1t pubchem
small molecule Antagonist CXCL12α, CXCL1... Peptide Yes No Stevens RC 10.1126/SCIENCE.1194396 2010-10-27 Yes
CXCR4 CXCR4 Chemokine A (Rhodopsin) Human X-ray 3OE0 3OE0_refined 2.9 A Inactive -1.5 - - - - T4-Lysozyme - CVX15
Peptide Antagonist CXCL12α, CXCL1... Peptide Yes No Stevens RC 10.1126/SCIENCE.1194396 2010-10-27 Yes
C5AR1 C5a1 Complement peptide A (Rhodopsin) Human X-ray 5O9H 5O9H_refined 2.7 A Inactive -1.5 - - - - - - NDT 9513727 pubchem
small molecule Antagonist - Yes No Marshall FH 10.1038/NATURE25025 2018-01-10 Yes
CCR9 CCR9 Chemokine A (Rhodopsin) Human X-ray 5LWE - 2.8 B Inactive 0.1 - - - - - - Vercirnon pubchem
small molecule Antagonist - No No Marshall FH 10.1038/NATURE20606 2016-12-07 Yes
DRD3 D3 Dopamine A (Rhodopsin) Human X-ray 3PBL 3PBL_refined 2.9 A Inactive -0.4 - - - - T4-Lysozyme - Eticlopride pubchem
small molecule Antagonist dopamine small molecule Yes No Stevens RC 10.1126/SCIENCE.1197410 2010-11-03 Yes
GLR glucagon Glucagon B1 (Secretin) Human X-ray 5XEZ 5XEZ_refined 3.0 B Inactive -4.5 - - - - T4-Lysozyme Antibody 4-{[(4-Cyclohexylphe... pubchem
small molecule Antagonist - No No Wu B 10.1038/NATURE22363 2017-05-24 Yes
GLR glucagon Glucagon B1 (Secretin) Human X-ray 5XF1 - 3.2 B Inactive -4.8 - - - - T4-Lysozyme Antibody 4-{[(4-Cyclohexylphe... pubchem
small molecule Antagonist - No No Wu B 10.1038/NATURE22363 2017-05-24 Yes
APJ apelin Apelin A (Rhodopsin) Human X-ray 5VBL 5VBL_refined 2.6 B Inactive -0.4 - - - - Rubredoxin - AMG3054
Peptide Agonist apelin-13, apelin re... Peptide Yes No Xu F 10.1016/J.STR.2017.04.008 2017-05-31 Yes
DRD4 D4 Dopamine A (Rhodopsin) Human X-ray 5WIU 5WIU_refined 2.0 A Inactive -1.0 - - - - - - Nemonapride pubchem
small molecule Antagonist - Yes No Roth BL 10.1126/SCIENCE.AAN5468 2017-10-18 Yes
DRD4 D4 Dopamine A (Rhodopsin) Human X-ray 5WIV 5WIV_refined 2.1 A Inactive -0.9 - - - - BRIL - Nemonapride pubchem
small molecule Antagonist - Yes Yes Roth BL 10.1126/SCIENCE.AAN5468 2017-10-18 Yes
CNR1 CB1 Cannabinoid A (Rhodopsin) Human cryo-EM 6N4B 6N4B_refined 3.0 R Active 8.3 Gi/o Gi1 - 62 scFv16 - Fub-mdmb pubchem
small molecule Agonist 2-arachidonoylglycer... Endocannabinoid Yes No Skiniotis G 10.1016/J.CELL.2018.11.040 2019-01-30 Yes
AA1R A1 Adenosine A (Rhodopsin) Human cryo-EM 6D9H 6D9H_refined 3.6 R Active 9.2 Gi/o Gi2 - 59 - - Adenosine pubchem
small molecule Agonist - Yes No Christopoulos A 10.1038/S41586-018-0236-6 2018-06-20 Yes
G1SGD4 GLP-1 Glucagon B1 (Secretin) Rabbit cryo-EM 5VAI 5VAI_refined 4.1 R Active 6.9 Gs Gs - 59 - - GLP-1 pubchem
Peptide Agonist glucagon-like peptid... Peptide No No Skiniotis G 10.1038/NATURE22394 2017-05-24 Yes
GLP1R GLP-1 Glucagon B1 (Secretin) Human cryo-EM 6B3J 6B3J_refined 3.3 R Active 6.8 Gs Gs - 49 - - Exendin-P5
Peptide Agonist - No No Wootten D 10.1038/NATURE25773 2018-02-21 Yes
CRFR1 CRF1 Corticotropin-releasing factor B1 (Secretin) Human X-ray 4Z9G 4Z9G_refined 3.2 A Inactive -1.0 - - - - T4-Lysozyme - CP-376395 pubchem
small molecule Antagonist corticotrophin-relea... Peptide No No Marshall FH 10.2174/1874467210666170110114727 2016-06-29 Yes
P2Y12 P2Y12 P2Y A (Rhodopsin) Human X-ray 4NTJ 4NTJ_refined 2.6 A Intermediate 4.7 - - - - BRIL - AZD1283 pubchem
small molecule Antagonist - Yes No Zhao Q 10.1038/NATURE13083 2014-03-26 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 1GZM - 2.7 A Inactive 0.1 - - - - - - retinal gtoplig
small molecule Inverse agonist retinal small molecule No No Schertler GF 10.1016/J.JMB.2004.08.090 2003-11-20 Yes
AGTR1 AT1 Angiotensin A (Rhodopsin) Human X-ray 4ZUD 4ZUD_refined 2.8 A Inactive -0.9 - - - - BRIL - OLM
small molecule Inverse agonist - Yes No Stevens RC 10.1074/JBC.M115.689000 2015-10-07 Yes
FZD4 FZD4 Frizzled F (Frizzled) Human X-ray 6BD4 6BD4_refined 2.4 A Inactive -4.3 - - - - Rubredoxin - N/A N/A N/A - No No Xu F 10.1038/S41586-018-0447-X 2018-08-22 Yes
NTR1 NTS1 Neurotensin A (Rhodopsin) Rat X-ray 4XEE 4XEE_refined 2.9 A Intermediate 6.5 - - - - T4-Lysozyme - CHEMBL342252 pubchem
Peptide Agonist neurotensin Peptide Yes No Grisshammer R 10.1038/NCOMMS8895 2015-07-29 Yes
NTR1 NTS1 Neurotensin A (Rhodopsin) Rat X-ray 4XES 4XES_refined 2.6 A Intermediate 6.0 - - - - T4-Lysozyme - CHEMBL342252 pubchem
Peptide Agonist neurotensin Peptide Yes No Grisshammer R 10.1038/NCOMMS8895 2015-07-29 Yes
OX1R OX1 Orexin A (Rhodopsin) Human X-ray 4ZJC 4ZJC_refined 2.8 A Inactive -0.5 - - - - - - SB-674042 pubchem
small molecule Antagonist noradrenaline small molecule No No Rosenbaum DM 10.1038/NSMB.3183 2016-03-09 Yes
OX1R OX1 Orexin A (Rhodopsin) Human X-ray 4ZJ8 4ZJ8_refined 2.8 A Inactive -0.5 - - - - - - Suvorexant pubchem
small molecule Antagonist noradrenaline small molecule No No Rosenbaum DM 10.1038/NSMB.3183 2016-03-09 Yes
PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human X-ray 6FJ3 6FJ3_refined 2.5 A Inactive -19.3 - - - - GlgA glycogen synthase - ePTH
Peptide Agonist - No No Plückthun A 10.1038/S41594-018-0151-4 2018-11-21 Yes
NTR1 NTS1 Neurotensin A (Rhodopsin) Rat X-ray 4BUO - 2.8 A Inactive 0.6 - - - - - - CHEMBL342252 pubchem
Peptide Agonist neurotensin Peptide Yes No Plückthun A 10.1073/PNAS.1317903111 2014-01-29 Yes
NTR1 NTS1 Neurotensin A (Rhodopsin) Rat X-ray 4BWB - 3.6 A Inactive 1.5 - - - - - - CHEMBL342252 pubchem
Peptide Agonist neurotensin Peptide Yes No Plückthun A 10.1073/PNAS.1317903111 2014-01-29 No
NTR1 NTS1 Neurotensin A (Rhodopsin) Rat X-ray 3ZEV - 3.0 A Inactive 0.5 - - - - - - CHEMBL342252 pubchem
Peptide Agonist neurotensin Peptide Yes No Plückthun A 10.1073/PNAS.1317903111 2014-01-29 No
NTR1 NTS1 Neurotensin A (Rhodopsin) Rat X-ray 4BV0 - 3.1 A Inactive 1.0 - - - - - - CHEMBL342252 pubchem
Peptide Agonist neurotensin Peptide Yes No Plückthun A 10.1073/PNAS.1317903111 2014-01-29 No
OPRD δ Opioid A (Rhodopsin) Mouse X-ray 4EJ4 4EJ4_refined 3.4 A Inactive -1.2 - - - - T4-Lysozyme - Naltrindole pubchem
small molecule Antagonist β-endorphin, dy... Peptide Yes No Kobilka BK 10.1038/NATURE11111 2012-05-16 Yes
CCR5 CCR5 Chemokine A (Rhodopsin) Human X-ray 5UIW 5UIW_refined 2.2 A Inactive 1.0 - - - - Rubredoxin - 5P7-CCL5
Peptide Antagonist CCL11, CCL14, CCL16,... Peptide No No Handel TM 10.1016/J.IMMUNI.2017.05.002 2017-06-28 Yes
ACM3 M3 Acetylcholine (muscarinic) A (Rhodopsin) Rat X-ray 5ZHP 5ZHP_refined 3.1 B Inactive 0.9 - - - - Endolysin - (1R,2R,4S,5S,7s)-7-(... pubchem
small molecule Antagonist acetylcholine small molecule No No Gmeiner P 10.1073/PNAS.1813988115 2018-11-28 Yes
US28 US28 Unclassified A (Rhodopsin) strain AD169 X-ray 4XT1 - 2.9 A Active 9.0 - - - - - Nanobody CX3CL1
Peptide Agonist CX<sub>3</sub>CL1 Peptide Yes No Garcia KC 10.1126/SCIENCE.AAA5026 2015-03-04 Yes
US28 US28 Unclassified A (Rhodopsin) strain AD169 X-ray 4XT3 4XT3_refined 3.8 A Active 8.9 - - - - - - Fractalkine
Peptide Agonist CX<sub>3</sub>CL1 Peptide Yes No Garcia KC 10.1126/SCIENCE.AAA5026 2015-03-04 Yes
S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human X-ray 3V2Y 3V2Y_refined 2.8 A Inactive -0.6 - - - - T4-Lysozyme - 909725-61-7 pubchem
small molecule Antagonist sphingosine 1-phosph... Lipid Yes No Stevens RC 10.1126/SCIENCE.1215904 2012-02-15 Yes
S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human X-ray 3V2W - 3.4 A Inactive -1.5 - - - - T4-Lysozyme - 909725-61-7 pubchem
small molecule Antagonist sphingosine 1-phosph... Lipid Yes No Stevens RC 10.1126/SCIENCE.1215904 2012-02-15 No
5HT2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 4IB4 4IB4_refined 2.7 A Intermediate 3.1 - - - - Soluble cytochrome b562 - Ergotamine pubchem
small molecule Agonist 5-hydroxytryptamine small molecule Yes No Stevens RC 10.1126/SCIENCE.1232808 2013-03-13 Yes
GRM1 mGlu1 Metabotropic glutamate C (Glutamate) Human X-ray 4OR2 4OR2_refined 2.8 B Inactive 4.0 - - - - BRIL - FITM pubchem
small molecule NAM L-glutamic acid small molecule No No Stevens RC 10.1126/SCIENCE.1249489 2014-03-19 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey X-ray 6H7N 6H7N_refined 2.5 A Active 9.3 - - - - Thioredoxin 1 Camelid antibody fragment Nb6B9 Xamoterol pubchem
small molecule Agonist - Yes No Tate CG 10.1101/436212 2018-10-17 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey X-ray 6H7O 6H7O_refined 2.8 A Active 9.3 - - - - Thioredoxin 1 Camelid antibody fragment Nb6B9 4-{[(2S)-3-(tert-but... pubchem
small molecule Agonist - Yes No Tate CG 10.1101/436212 2018-10-17 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey X-ray 6H7L - 2.7 A Active 9.2 - - - - Thioredoxin 1 Camelid antibody fragment Nb6B9 DOBUTAMINE pubchem
small molecule Agonist - Yes No Tate CG 10.1101/436212 2018-10-17 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey X-ray 6H7J 6H7J_refined 2.8 A Active 9.3 - - - - Thioredoxin 1 Camelid antibody fragment Nb80 ISOPRENALINE pubchem
small molecule Agonist - Yes No Tate CG 10.1101/436212 2018-10-17 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey X-ray 6H7M 6H7M_refined 2.8 A Active 9.3 - - - - Thioredoxin 1 Camelid antibody fragment Nb6B9 SALBUTAMOL pubchem
small molecule Agonist - Yes No Tate CG 10.1101/436212 2018-10-17 Yes
PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human cryo-EM 6NBH 6NBH_refined 3.5 R Active 6.5 Gs Gs - 57 - Nanobody-35 Long-acting parathyr...
Peptide Agonist - No No Zhang Y 10.1126/SCIENCE.AAV7942 2019-04-17 Yes
PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human cryo-EM 6NBF 6NBF_refined 3.0 R Active 7.0 Gs Gs - 58 - Nanobody-35 Long-acting parathyr...
Peptide Agonist - No No Zhang Y 10.1126/SCIENCE.AAV7942 2019-04-17 Yes
PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human cryo-EM 6NBI 6NBI_refined 4.0 R Active 6.6 Gs Gs - 56 - Nanobody-35 Long-acting parathyr...
Peptide Agonist - No No Zhang Y 10.1126/SCIENCE.AAV7942 2019-04-17 Yes
5HT1B 5-HT1B 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 4IAR 4IAR_refined 2.7 A Intermediate 4.2 - - - - BRIL - ERGOTAMINE pubchem
small molecule Agonist - Yes No Xu HE 10.1126/SCIENCE.1232807 2013-03-13 Yes
5HT1B 5-HT1B 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 4IAQ 4IAQ_refined 2.8 A Intermediate 2.8 - - - - BRIL - dihydroergotamine pubchem
small molecule Agonist - Yes No Xu HE 10.1126/SCIENCE.1232807 2013-03-13 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 3VG9 3VG9_refined 2.7 A Inactive -1.2 - - - - - - ZM241385 pubchem
small molecule Antagonist - Yes No Murata T 10.1038/NATURE10750 2012-02-01 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 3VGA - 3.1 A Inactive -1.4 - - - - - - ZM241385 pubchem
small molecule Antagonist - Yes No Murata T 10.1038/NATURE10750 2012-02-01 No
OPSD Rhodopsin Opsins A (Rhodopsin) Human X-ray 4ZWJ 4ZWJ_refined 3.3 A Active 8.6 Arrestin S-arrestin - 86 T4-Lysozyme - N/A N/A N/A retinal small molecule No No Xu HE 10.1038/NATURE14656 2015-07-29 Yes
OPRM μ Opioid A (Rhodopsin) Mouse X-ray 4DKL 4DKL_refined 2.8 A Inactive -1.4 - - - - T4-Lysozyme - BF0
small molecule Antagonist &beta;-endorphin, dy... Peptide Yes No Granier S 10.1038/NATURE10954 2012-03-21 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey X-ray 4AMI - 3.2 A Inactive -1.2 - - - - - - bucindolol pubchem
small molecule Agonist - Yes No Tate CG 10.1016/J.STR.2012.03.014 2012-05-23 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey X-ray 4AMJ 4AMJ_refined 2.3 B Inactive -1.0 - - - - - - (S)-Carvedilol pubchem
small molecule Inverse agonist - Yes No Tate CG 10.1016/J.STR.2012.03.014 2012-05-23 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5IUA 5IUA_refined 2.2 A Inactive -0.7 - - - - BRIL - 6DX pubchem
small molecule Agonist - Yes Yes Cooke RM 10.1021/ACS.JMEDCHEM.6B00653 2016-06-29 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5IU7 5IU7_refined 1.9 A Inactive -0.7 - - - - BRIL - 6DY pubchem
small molecule Agonist - Yes Yes Cooke RM 10.1021/ACS.JMEDCHEM.6B00653 2016-06-29 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5IUB 5IUB_refined 2.1 A Inactive -0.9 - - - - BRIL - CHEMBL184061 pubchem
small molecule Agonist - Yes Yes Cooke RM 10.1021/ACS.JMEDCHEM.6B00653 2016-06-29 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5IU4 - 1.7 A Inactive -0.8 - - - - BRIL - ZM241385 pubchem
small molecule Antagonist - Yes Yes Cooke RM 10.1021/ACS.JMEDCHEM.6B00653 2016-06-29 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 1L9H - 2.6 A Inactive -0.5 - - - - - - retinal gtoplig
small molecule Inverse agonist retinal small molecule No No Shichida Y 10.1073/PNAS.082666399 2002-05-15 No
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human X-ray 3NY9 3NY9_refined 2.8 A Inactive -1.5 - - - - T4-Lysozyme - CHEMBL1233771 pubchem
small molecule Inverse agonist (-)-adrenaline, (-)-... small molecule Yes No Stevens RC 10.1021/JA105108Q 2010-08-11 Yes
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human X-ray 3NYA 3NYA_refined 3.2 A Inactive -1.3 - - - - T4-Lysozyme - UNII-3J532ZIY9K pubchem
small molecule Antagonist (-)-adrenaline, (-)-... small molecule Yes No Stevens RC 10.1021/JA105108Q 2010-08-11 Yes
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human X-ray 3NY8 3NY8_refined 2.8 A Inactive -1.3 - - - - T4-Lysozyme - (2S,3S)-1-[(7-methyl... pubchem
small molecule Inverse agonist (-)-adrenaline, (-)-... small molecule Yes No Stevens RC 10.1021/JA105108Q 2010-08-11 Yes
CCR5 CCR5 Chemokine A (Rhodopsin) Human X-ray 6AKX - 2.8 B Inactive 0.7 - - - - Rubredoxin - N-[(1S)-3-{(3-exo)-3...
small molecule Antagonist CCL11, CCL14, CCL16,... Peptide No No Liu H 10.1021/ACS.JMEDCHEM.8B01077 2018-10-24 Yes
CCR5 CCR5 Chemokine A (Rhodopsin) Human X-ray 6AKY 6AKY_refined 2.8 A Inactive 0.4 - - - - Rubredoxin - 4,4-difluoro-N-[(1S)...
small molecule Antagonist CCL11, CCL14, CCL16,... Peptide No No Liu H 10.1021/ACS.JMEDCHEM.8B01077 2018-10-24 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 2PED - 3.0 B Inactive 0.2 - - - - - - retinal gtoplig
small molecule Inverse agonist retinal small molecule No No Okada T 10.1529/BIOPHYSJ.107.108225 2007-10-30 No
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey X-ray 2Y00 2Y00_refined 2.5 B Inactive -1.2 - - - - - - Dobutamine pubchem
small molecule Agonist (partial) - Yes No Tate CG 10.1038/NATURE09746 2011-01-12 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey X-ray 2Y04 2Y04_refined 3.1 B Inactive -1.1 - - - - - - Levalbuterol pubchem
small molecule Agonist (partial) - Yes No Tate CG 10.1038/NATURE09746 2011-01-12 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey X-ray 2Y01 - 2.6 A Inactive -1.1 - - - - - - Dobutamine pubchem
small molecule Agonist (partial) - Yes No Tate CG 10.1038/NATURE09746 2011-03-30 No
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey X-ray 2Y02 2Y02_refined 2.6 B Inactive -1.2 - - - - - - Carmoterol pubchem
small molecule Agonist - Yes No Tate CG 10.1038/NATURE09746 2011-01-12 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey X-ray 2Y03 - 2.9 B Inactive -1.2 - - - - - - LEVISOPRENALINE pubchem
small molecule Agonist - Yes No Tate CG 10.1038/NATURE09746 2011-01-12 Yes
EDNRB ETB Endothelin A (Rhodopsin) Human X-ray 6IGK 6IGK_refined 2.0 A Intermediate 2.2 - - - - Endolysin - Endothelin-3 pubchem
Peptide Agonist - Yes No Nureki O 10.1038/S41467-018-07094-0 2018-11-21 Yes
EDNRB ETB Endothelin A (Rhodopsin) Human X-ray 6IGL 6IGL_refined 2.7 A Inactive 0.2 - - - - Endolysin - IRL1620 pubchem
Peptide Partial agonist - Yes No Nureki O 10.1038/S41467-018-07094-0 2018-11-21 Yes
CNR1 CB1 Cannabinoid A (Rhodopsin) Human X-ray 5XRA 5XRA_refined 2.8 A Active 8.0 - - - - Flavodoxin - CHEMBL1683648 pubchem
small molecule Agonist 2-arachidonoylglycer... Endocannabinoid Yes No Liu Z 10.1038/NATURE23272 2017-07-12 Yes
CNR1 CB1 Cannabinoid A (Rhodopsin) Human X-ray 5XR8 5XR8_refined 3.0 A Active 7.9 - - - - Flavodoxin - 8D0
small molecule Agonist 2-arachidonoylglycer... Endocannabinoid Yes No Liu Z 10.1038/NATURE23272 2017-07-12 Yes
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human X-ray 3PDS 3PDS_refined 3.5 A Inactive -1.0 - - - - T4-Lysozyme - FAUC50 pubchem
small molecule Agonist (-)-adrenaline, (-)-... small molecule Yes No Kobilka BK 10.1038/NATURE09665 2011-01-12 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5OLO 5OLO_refined 3.1 A Inactive -0.7 - - - - Soluble cytochrome b562 - Tozadenant pubchem chembl_ligand
small molecule Antagonist - Yes No Doré AS 10.1038/S41598-017-18570-W 2018-01-17 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5OLH - 2.6 A Inactive -0.7 - - - - Soluble cytochrome b562 - Vipadenant
small molecule Antagonist - Yes Yes Doré AS 10.1038/S41598-017-18570-W 2018-01-17 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5OM1 5OM1_refined 2.1 A Inactive -0.7 - - - - Soluble cytochrome b562 - 4-(3-amino-5-phenyl-...
small molecule Antagonist - Yes Yes Doré AS 10.1038/S41598-017-18570-W 2018-01-17 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5OLV 5OLV_refined 2.0 A Inactive -0.6 - - - - Soluble cytochrome b562 - CHEMBL1671936 pubchem chembl_ligand
small molecule Antagonist - Yes Yes Doré AS 10.1038/S41598-017-18570-W 2018-01-17 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5OM4 5OM4_refined 2.0 A Inactive -0.7 - - - - Soluble cytochrome b562 - 4-(3-amino-5-phenyl-...
small molecule Antagonist - Yes Yes Doré AS 10.1038/S41598-017-18570-W 2018-01-17 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5OLG - 1.9 A Inactive -0.7 - - - - Soluble cytochrome b562 - ZM241385 pubchem
small molecule Antagonist - Yes Yes Doré AS 10.1038/S41598-017-18570-W 2018-01-17 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5OLZ 5OLZ_refined 1.9 A Inactive -0.8 - - - - Soluble cytochrome b562 - 4-(3-amino-5-phenyl-...
small molecule Antagonist - Yes Yes Doré AS 10.1038/S41598-017-18570-W 2018-01-17 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5VRA 5VRA_refined 2.4 A Inactive -0.4 - - - - Soluble cytochrome b562 - ZM241385 pubchem
small molecule Antagonist - Yes Yes Ernst OP 10.1038/NPROT.2017.135 2017-12-13 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 5WKT 5WKT_refined 3.2 A Active 8.0 Gi/o Gt1 Only H5 3 - - N/A N/A N/A retinal small molecule No No Ernst OP 10.1038/NPROT.2017.135 2017-12-13 Yes
OPRD δ Opioid A (Rhodopsin) Human X-ray 4RWA - 3.3 A Inactive -1.2 - - - - BRIL - DIPP-NH2
peptide-like Antagonist &beta;-endorphin, dy... Peptide Yes No Cherezov V 10.1038/NSMB.2965 2015-01-14 No
OPRD δ Opioid A (Rhodopsin) Human X-ray 4RWD 4RWD_refined 2.7 A Inactive -0.8 - - - - BRIL - DIPP-NH2
peptide-like Antagonist &beta;-endorphin, dy... Peptide Yes Yes Cherezov V 10.1038/NSMB.2965 2015-01-14 Yes
MTR1B MT2 Melatonin A (Rhodopsin) Human X-ray 6ME6 6ME6_refined 2.8 B Inactive -0.8 - - - - Soluble cytochrome b562
Rubredoxin
- 2-Phenylmelatonin pubchem
small molecule Agonist - No No Cherezov V 10.1038/S41586-019-1144-0 2019-04-24 Yes
MTR1B MT2 Melatonin A (Rhodopsin) Human X-ray 6ME9 6ME9_refined 3.3 B Inactive -0.5 - - - - Soluble cytochrome b562
Rubredoxin
- Ramelteon pubchem chembl_ligand
small molecule Agonist - No No Cherezov V 10.1038/S41586-019-1144-0 2019-04-24 Yes
MTR1B MT2 Melatonin A (Rhodopsin) Human X-ray 6ME8 6ME8_refined 3.1 B Inactive -0.7 - - - - Soluble cytochrome b562
Rubredoxin
- 2-Phenylmelatonin pubchem
small molecule Agonist - Yes No Cherezov V 10.1038/S41586-019-1144-0 2019-04-24 Yes
MTR1B MT2 Melatonin A (Rhodopsin) Human X-ray 6ME7 - 3.2 A Inactive -1.0 - - - - Soluble cytochrome b562
Rubredoxin
- 2-Phenylmelatonin pubchem
small molecule Agonist - No No Cherezov V 10.1038/S41586-019-1144-0 2019-04-24 Yes
CCR2 CCR2 Chemokine A (Rhodopsin) Human X-ray 6GPS 6GPS_refined 3.3 A Inactive 0.8 - - - - Rubredoxin - MK-0812 pubchem
small molecule Antagonist - No No Schnapp G 10.1016/J.STR.2018.10.027 2019-01-02 Yes
CCR2 CCR2 Chemokine A (Rhodopsin) Human X-ray 6GPX 6GPX_refined 2.7 B Inactive 0.6 - - - - Rubredoxin - MK-0812 pubchem
small molecule Antagonist - No No Schnapp G 10.1016/J.STR.2018.10.027 2019-01-02 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 1HZX - 2.8 A Inactive -0.0 - - - - - - retinal gtoplig
small molecule Inverse agonist retinal small molecule No No Stenkamp RE 10.1021/BI0155091 2001-07-04 No
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5K2B 5K2B_refined 2.5 A Inactive -0.6 - - - - BRIL - 139180-30-6 pubchem
small molecule Antagonist - Yes Yes Cherezov V 10.1126/SCIADV.1600292 2016-09-21 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5K2C 5K2C_refined 1.9 A Inactive -0.7 - - - - BRIL - ZM241385 pubchem
small molecule Antagonist - Yes Yes Cherezov V 10.1126/SCIADV.1600292 2016-09-21 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5K2A 5K2A_refined 2.5 A Inactive -0.7 - - - - BRIL - ZM241385 pubchem
small molecule Antagonist - Yes Yes Cherezov V 10.1126/SCIADV.1600292 2016-09-21 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5K2D 5K2D_refined 1.9 A Inactive -0.7 - - - - BRIL - ZM241385 pubchem
small molecule Antagonist - Yes Yes Cherezov V 10.1126/SCIADV.1600292 2016-09-21 Yes
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human X-ray 2RH1 2RH1_refined 2.4 A Inactive -0.8 - - - - T4-Lysozyme - Carazolol pubchem
small molecule Inverse agonist (-)-adrenaline, (-)-... small molecule Yes No Stevens RC 10.1126/SCIENCE.1150577 2007-10-30 Yes
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human X-ray 6MXT 6MXT_refined 3.0 A Active 8.2 - - - - Endolysin Nanobody 71 Salmeterol pubchem
small molecule Agonist (-)-adrenaline, (-)-... small molecule Yes No Kobilka BK 10.1038/S41589-018-0145-X 2018-11-14 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 3UZA - 3.3 A Inactive -0.6 - - - - - - CHEMBL2024115 pubchem
small molecule Antagonist - Yes No Marshall FH 10.1021/JM201376W 2012-03-21 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 3UZC - 3.3 A Inactive -0.5 - - - - - - T4E
small molecule Antagonist - Yes No Marshall FH 10.1021/JM201376W 2012-03-21 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 4J4Q 4J4Q_refined 2.7 A Active 8.5 Gi/o Gt1 Only H5 3 - - N/A N/A N/A retinal small molecule No No Ernst OP 10.1002/ANIE.201302374 2013-10-30 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5MZP - 2.1 A Inactive -0.8 - - - - - - Caffeine pubchem
small molecule Antagonist - Yes Yes Cooke RM 10.1016/J.STR.2017.06.012 2017-07-26 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5N2R - 2.8 A Inactive -0.7 - - - - BRIL - PSB36 pubchem
small molecule Antagonist - Yes Yes Cooke RM 10.1016/J.STR.2017.06.012 2017-07-26 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5MZJ 5MZJ_refined 2.0 A Inactive -0.5 - - - - - - Theophylline pubchem
small molecule Antagonist - Yes Yes Cooke RM 10.1016/J.STR.2017.06.012 2017-07-26 Yes
AA1R A1 Adenosine A (Rhodopsin) Human X-ray 5N2S 5N2S_refined 3.3 A Inactive -0.5 - - - - - - PSB36 pubchem
small molecule Agonist - Yes No Cooke RM 10.1016/J.STR.2017.06.012 2017-07-26 Yes
NK1R NK1 Tachykinin A (Rhodopsin) Human X-ray 6J21 6J21_refined 3.2 A Inactive 0.4 - - - - Endolysin - Aprepitant pubchem pubchem chembl_ligand
small molecule Antagonist - Yes No Zhao Q 10.1038/S41467-019-08568-5 2019-03-06 Yes
NK1R NK1 Tachykinin A (Rhodopsin) Human X-ray 6J20 6J20_refined 2.7 A Inactive 0.2 - - - - Endolysin - Aprepitant pubchem pubchem chembl_ligand
small molecule Antagonist - No No Zhao Q 10.1038/S41467-019-08568-5 2019-03-06 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 5TE5 5TE5_refined 4.0 A Inactive -0.5 - - - - - - 10,20-Methanoretinal pubchem
small molecule Agonist retinal small molecule No No Palczewski K 10.1073/PNAS.1617446114 2017-03-15 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 5TE3 5TE3_refined 2.7 A Active 8.0 - - - - - - N/A N/A N/A retinal small molecule No No Palczewski K 10.1073/PNAS.1617446114 2017-03-15 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 4EIY 4EIY_refined 1.8 A Inactive -0.6 - - - - BRIL - ZM241385 pubchem
small molecule Antagonist - Yes Yes Stevens RC 10.1126/SCIENCE.1219218 2012-07-25 Yes
SMO SMO Frizzled F (Frizzled) Human X-ray 5V57 5V57_refined 3.0 A Inactive -1.7 - - - - Flavodoxin - N-methyl-N-[1-[4-(2-... pubchem
small molecule Antagonist constitutive Constitutive No No Xu F 10.1038/NCOMMS15383 2017-05-24 Yes
SMO SMO Frizzled F (Frizzled) Human X-ray 5V56 - 2.9 B Inactive -1.9 - - - - Flavodoxin - N-methyl-N-[1-[4-(2-... pubchem
small molecule Antagonist constitutive Constitutive No No Xu F 10.1038/NCOMMS15383 2017-05-24 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Japanese flying squid X-ray 3AYM - 2.8 B Inactive -0.2 - - - - - - retinal gtoplig
small molecule Agonist retinal small molecule Yes No Kouyama T 10.1016/J.JMB.2011.08.044 2011-08-17 No
OPSD Rhodopsin Opsins A (Rhodopsin) Japanese flying squid X-ray 3AYN - 2.7 B Inactive -0.2 - - - - - - retinal gtoplig
small molecule Inverse agonist retinal small molecule Yes No Kouyama T 10.1016/J.JMB.2011.08.044 2011-08-17 No
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey X-ray 2YCY - 3.2 A Inactive -1.6 - - - - - - (S)-Cyanopindolol pubchem
small molecule Antagonist - Yes No Schertler GFX 10.1073/PNAS.1100185108 2011-06-08 No
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey X-ray 2YCZ 2YCZ_refined 3.7 B Inactive -1.7 - - - - - - timolol pubchem
small molecule Antagonist - Yes No Schertler GFX 10.1073/PNAS.1100185108 2011-06-01 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey X-ray 2YCW 2YCW_refined 3.0 A Inactive -1.1 - - - - - - timolol pubchem
small molecule Inverse agonist - Yes No Schertler GFX 10.1073/PNAS.1100185108 2011-06-01 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey X-ray 2YCX - 3.3 A Inactive -1.6 - - - - - - (S)-Cyanopindolol pubchem
small molecule Antagonist - Yes No Schertler GFX 10.1073/PNAS.1100185108 2011-06-01 No
CRFR1 CRF1 Corticotropin-releasing factor B1 (Secretin) Human X-ray 4K5Y 4K5Y_refined 3.0 C Inactive -2.0 - - - - T4-Lysozyme - CP-376395 pubchem
small molecule Antagonist corticotrophin-relea... Peptide No No Marshall FH 10.1038/NATURE12357 2013-07-17 Yes
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human X-ray 5D5B - 3.8 A Inactive -1.1 - - - - T4-Lysozyme - Carazolol pubchem
small molecule Inverse agonist (-)-adrenaline, (-)-... small molecule Yes No Caffrey M 10.1107/S2059798315021683 2016-01-13 No
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human X-ray 5D5A - 2.5 A Inactive -1.1 - - - - T4-Lysozyme - Carazolol pubchem
small molecule Inverse agonist (-)-adrenaline, (-)-... small molecule Yes No Caffrey M 10.1107/S2059798315021683 2016-01-13 No
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 6AQF 6AQF_refined 2.5 A Inactive -0.4 - - - - Soluble cytochrome b562 - ZM241385 pubchem
small molecule Antagonist - Yes No Wüthrich K 10.1016/J.CELL.2017.12.004 2018-01-10 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 6FKB 6FKB_refined 3.0 A Active 7.9 - - - - - - 2-(4-chlorophenyl)-1...
small molecule Agonist retinal small molecule No No Dawson RJP 10.1073/PNAS.1718084115 2018-04-04 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 6FKC 6FKC_refined 2.5 A Active 7.8 - - - - - - 3-[1'-[(2~{S})-2-(4-...
small molecule Agonist retinal small molecule No No Dawson RJP 10.1073/PNAS.1718084115 2018-04-04 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 6FKA 6FKA_refined 2.7 A Active 8.0 - - - - - - (2~{S})-2-(3,4-dichl...
small molecule Agonist retinal small molecule No No Dawson RJP 10.1073/PNAS.1718084115 2018-04-04 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 6FK8 6FK8_refined 2.9 A Active 7.9 - - - - - - (2~{R},3~{S})-3-azan...
small molecule Agonist retinal small molecule No No Dawson RJP 10.1073/PNAS.1718084115 2018-04-04 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 6FK7 6FK7_refined 2.6 A Active 7.7 - - - - - - (2~{R},3~{R})-2-(4-c...
small molecule Agonist retinal small molecule No No Dawson RJP 10.1073/PNAS.1718084115 2018-04-04 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 6FK9 6FK9_refined 2.6 A Active 7.8 - - - - - - (2~{S})-3-methyl-2-p...
small molecule Agonist retinal small molecule No No Dawson RJP 10.1073/PNAS.1718084115 2018-04-04 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 6FKD 6FKD_refined 2.5 A Active 7.9 - - - - - - 5-chloranyl-2-(2-oxi...
small molecule Agonist retinal small molecule No No Dawson RJP 10.1073/PNAS.1718084115 2018-04-04 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 6FK6 6FK6_refined 2.4 A Active 7.9 - - - - - - (2~{S})-2-(4-chlorop...
small molecule Agonist retinal small molecule No No Dawson RJP 10.1073/PNAS.1718084115 2018-04-04 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey X-ray 5F8U 5F8U_refined 3.4 A Inactive -0.5 - - - - - - (S)-Cyanopindolol pubchem
small molecule Antagonist - Yes No Tate CG 10.1038/NSMB.3130 2015-12-23 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 2YDO 2YDO_refined 3.0 A Intermediate 6.3 - - - - - - adenosine pubchem
small molecule Agonist - Yes No Tate CG 10.1038/NATURE10136 2011-05-18 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 2YDV 2YDV_refined 2.6 A Intermediate 6.2 - - - - - - NECA pubchem
small molecule Agonist - Yes No Tate CG 10.1038/NATURE10136 2011-05-18 Yes
5HT2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 6DS0 6DS0_refined 3.2 A Intermediate 3.2 - - - - Soluble cytochrome b562 - LY266097 pubchem
small molecule Antagonist 5-hydroxytryptamine small molecule Yes No Roth BL 10.1038/S41594-018-0116-7 2018-08-29 Yes
5HT2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 6DRX - 3.1 A Intermediate 2.7 - - - - Soluble cytochrome b562 - Lisuride pubchem
small molecule Antagonist 5-hydroxytryptamine small molecule Yes No Roth BL 10.1038/S41594-018-0116-7 2018-08-29 Yes
5HT2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 6DRY 6DRY_refined 2.9 A Intermediate 4.3 - - - - Soluble cytochrome b562 - Methylergonovine pubchem chembl_ligand
small molecule Agonist 5-hydroxytryptamine small molecule Yes No Roth BL 10.1038/S41594-018-0116-7 2018-08-29 Yes
5HT2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 6DRZ 6DRZ_refined 3.1 A Intermediate 4.2 - - - - Soluble cytochrome b562 - Methysergide pubchem
small molecule Antagonist 5-hydroxytryptamine small molecule Yes No Roth BL 10.1038/S41594-018-0116-7 2018-08-29 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Common turkey X-ray 2VT4 - 2.7 B Inactive -1.6 - - - - - - (S)-Cyanopindolol pubchem
small molecule Antagonist - Yes No Schertler GFX 10.1038/NATURE07101 2008-06-24 No
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 3PWH - 3.3 A Inactive -0.7 - - - - - - ZM241385 pubchem
small molecule Antagonist - Yes No Marshall FH 10.1016/J.STR.2011.06.014 2011-09-07 No
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 3REY 3REY_refined 3.3 A Inactive -0.4 - - - - - - Xanthine amine conge... pubchem
small molecule Antagonist - Yes No Marshall FH 10.1016/J.STR.2011.06.014 2011-09-07 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 3RFM - 3.6 A Inactive -0.5 - - - - - - caffeine pubchem
small molecule Antagonist - Yes No Marshall FH 10.1016/J.STR.2011.06.014 2011-09-07 Yes
P2Y12 P2Y12 P2Y A (Rhodopsin) Human X-ray 4PY0 4PY0_refined 3.1 A Intermediate 3.8 - - - - BRIL - 2-Mesatp pubchem
small molecule Agonist (partial) - Yes No Zhao Q 10.1038/NATURE13288 2014-04-30 Yes
P2Y12 P2Y12 P2Y A (Rhodopsin) Human X-ray 4PXZ 4PXZ_refined 2.5 A Intermediate 3.9 - - - - BRIL - 2-MeSADP pubchem
small molecule Agonist - Yes No Zhao Q 10.1038/NATURE13288 2014-04-30 Yes
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human X-ray 2R4S - 3.4 A Inactive -2.9 - - - - - Antibody N/A N/A N/A (-)-adrenaline, (-)-... small molecule Yes No Kobilka BK 10.1038/NATURE06325 2007-11-06 No
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human X-ray 2R4R - 3.4 A Inactive -2.8 - - - - - Antibody N/A N/A N/A (-)-adrenaline, (-)-... small molecule Yes No Kobilka BK 10.1038/NATURE06325 2007-11-06 No
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human X-ray 4LDO 4LDO_refined 3.2 A Active 9.2 - - - - T4-Lysozyme Nanobody epinephrine pubchem
small molecule Agonist (-)-adrenaline, (-)-... small molecule Yes No Kobilka BK 10.1038/NATURE12572 2013-09-25 Yes
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human X-ray 4LDE 4LDE_refined 2.8 A Active 9.4 - - - - T4-Lysozyme Nanobody BI167107 pubchem
small molecule Agonist (-)-adrenaline, (-)-... small molecule Yes No Kobilka BK 10.1038/NATURE12572 2013-09-25 Yes
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human X-ray 4LDL - 3.1 A Active 9.3 - - - - T4-Lysozyme Nanobody hydroxybenzylisoprot... pubchem
small molecule Agonist (-)-adrenaline, (-)-... small molecule Yes No Kobilka BK 10.1038/NATURE12572 2013-09-25 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 4PXF - 2.8 A Active 8.6 Arrestin S-arrestin Fragment 3 - - N/A N/A N/A retinal small molecule No No Scheerer P 10.1038/NCOMMS5801 2014-09-17 No
GLR glucagon Glucagon B1 (Secretin) Human X-ray 4L6R 4L6R_refined 3.3 A Inactive -4.6 - - - - BRIL - N/A N/A N/A - No No Stevens RC 10.1038/NATURE12393 2013-07-24 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 3OAX - 2.6 A Inactive 0.0 - - - - - - retinal gtoplig
small molecule Inverse agonist retinal small molecule No No Okada T 10.1016/J.BPJ.2010.08.003 2011-01-19 No
OPRM μ Opioid A (Rhodopsin) Mouse cryo-EM 6DDE 6DDE_refined 3.5 R Active 7.2 Gi/o Gi1 - 61 - Antibody DAMGO pubchem chembl_ligand
peptide-like Agonist &beta;-endorphin, dy... Peptide Yes No Kobilka BK 10.1038/S41586-018-0219-7 2018-06-13 Yes
OPRM μ Opioid A (Rhodopsin) Mouse cryo-EM 6DDF 6DDF_refined 3.5 R Active 7.9 Gi/o Gi1 - 61 - - DAMGO pubchem chembl_ligand
peptide-like Agonist &beta;-endorphin, dy... Peptide Yes No Kobilka BK 10.1038/S41586-018-0219-7 2018-06-13 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Japanese flying squid X-ray 4WW3 - 2.8 A Inactive 0.1 - - - - - - retinal gtoplig
small molecule Inverse agonist retinal small molecule Yes No Kouyama T 10.1371/JOURNAL.PONE.0126970 2015-06-17 No
ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human X-ray 3UON 3UON_refined 3.0 A Inactive -1.5 - - - - T4-Lysozyme - 62869-69-6 pubchem
small molecule Antagonist acetylcholine small molecule Yes No Kobayashi T 10.1038/NATURE10753 2012-02-01 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5JTB - 2.8 A Inactive -0.5 - - - - BRIL - ZM241385 pubchem
small molecule Antagonist - Yes No Popov A 10.1126/SCIADV.1602952 2017-05-31 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 3PXO - 3.0 A Active 7.9 - - - - - - retinal gtoplig
small molecule Agonist retinal small molecule No No Ernst OP 10.1038/NATURE09789 2011-03-09 No
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 3PQR 3PQR_refined 2.9 A Active 8.6 Gi/o Gt1 Only H5 3 - - retinal gtoplig
small molecule Agonist retinal small molecule No No Ernst OP 10.1038/NATURE09789 2011-03-09 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 4BEZ - 3.3 A Active 8.3 - - - - - - N/A N/A N/A retinal small molecule No No Standfuss J 10.1038/EMBOR.2013.44 2013-04-24 No
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 4BEY - 2.9 A Active 8.4 Gi/o Gt1 Only H5 3 - - N/A N/A N/A retinal small molecule No No Standfuss J 10.1038/EMBOR.2013.44 2013-05-08 No
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine cryo-EM 6OYA - 3.3 R Active 8.5 Gi/o Gt1 - 59 - Camelid antibody VHH fragment Retinal pubchem
small molecule Inverse agonist retinal small molecule No No Skiniotis G 10.1016/J.MOLCEL.2019.06.007 2019-07-24 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine cryo-EM 6OY9 6OY9_refined 3.9 R Active 8.7 Gi/o Gt1 - 64 - - Retinal pubchem
small molecule Inverse agonist retinal small molecule No No Skiniotis G 10.1016/J.MOLCEL.2019.06.007 2019-07-24 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 2I35 - 3.8 A Inactive -0.3 - - - - - - retinal gtoplig
small molecule Inverse agonist retinal small molecule No No Palczewski K 10.1073/PNAS.0608022103 2006-10-17 No
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 2I37 - 4.2 A Inactive -1.6 - - - - - - N/A N/A N/A retinal small molecule No No Palczewski K 10.1073/PNAS.0608022103 2006-10-17 No
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 2I36 - 4.1 A Inactive -0.4 - - - - - - N/A N/A N/A retinal small molecule No No Palczewski K 10.1073/PNAS.0608022103 2006-10-17 No
ACM3 M3 Acetylcholine (muscarinic) A (Rhodopsin) Rat X-ray 4U14 - 3.6 A Inactive 0.5 - - - - T4-Lysozyme - Tiotropium pubchem
small molecule Antagonist acetylcholine small molecule Yes No Kobilka BK 10.1016/J.STR.2014.08.022 2014-11-26 No
ACM3 M3 Acetylcholine (muscarinic) A (Rhodopsin) Rat X-ray 4U16 4U16_refined 3.7 B Inactive 0.2 - - - - T4-Lysozyme - methscopolamine pubchem
small molecule Antagonist acetylcholine small molecule Yes No Kobilka BK 10.1016/J.STR.2014.08.022 2014-11-26 Yes
ACM3 M3 Acetylcholine (muscarinic) A (Rhodopsin) Rat X-ray 4U15 4U15_refined 2.8 B Inactive 0.5 - - - - T4-Lysozyme - Tiotropium pubchem
small molecule Antagonist acetylcholine small molecule Yes No Kobilka BK 10.1016/J.STR.2014.08.022 2014-11-26 Yes
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human X-ray 4QKX 4QKX_refined 3.3 A Active 9.4 - - - - T4-Lysozyme Nanobody 4-[(1r)-1-Hydroxy-2-... pubchem
small molecule Agonist (-)-adrenaline, (-)-... small molecule Yes No Gmeiner P 10.1073/PNAS.1410415111 2014-07-23 Yes
GRM5 mGlu5 Metabotropic glutamate C (Glutamate) Human cryo-EM 6N52 - 4.0 A Inactive 4.1 - - - - - Nanobody 43 N/A N/A N/A L-glutamic acid small molecule No No Kobilka BK 10.1038/S41586-019-0881-4 2019-01-23 Yes
GRM5 mGlu5 Metabotropic glutamate C (Glutamate) Human cryo-EM 6N51 - 4.0 B Intermediate 5.5 - - - - - Nanobody 43 Quisqualic acid pubchem
small molecule Agonist L-glutamic acid small molecule No No Kobilka BK 10.1038/S41586-019-0881-4 2019-01-23 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 2G87 - 2.6 A Inactive -0.2 - - - - - - retinal gtoplig
small molecule Agonist retinal small molecule No No Okada T 10.1002/ANIE.200600595 2006-09-02 No
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 3EML - 2.6 A Inactive -1.2 - - - - T4-Lysozyme - ZM241385 pubchem
small molecule Antagonist - Yes No Stevens RC 10.1126/SCIENCE.1164772 2008-10-14 No
NTR1 NTS1 Neurotensin A (Rhodopsin) Rat X-ray 4GRV 4GRV_refined 2.8 A Intermediate 7.3 - - - - T4-Lysozyme - Neurotensin(8-13) pubchem
Peptide Agonist neurotensin Peptide Yes No Grisshammer R 10.1038/NATURE11558 2012-10-17 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 6FUF 6FUF_refined 3.1 A Active 8.3 Gi/o Go mini-Go 51 - - Retinal pubchem
small molecule Inverse agonist retinal small molecule No No Schertler GFX 10.1126/SCIADV.AAT7052 2018-10-03 Yes
C5AR1 C5a1 Complement peptide A (Rhodopsin) Human X-ray 6C1R 6C1R_refined 2.2 B Inactive -1.4 - - - - Soluble cytochrome b562 - PMX53 pubchem chembl_ligand
Avacopan pubchem
Peptide
small molecule
Antagonist - Yes No Zhang C 10.1038/S41594-018-0067-Z 2018-05-30 Yes
C5AR1 C5a1 Complement peptide A (Rhodopsin) Human X-ray 6C1Q 6C1Q_refined 2.9 B Inactive -1.4 - - - - Soluble cytochrome b562 - PMX53 pubchem chembl_ligand
H94Wrl71FP pubchem
Peptide
small molecule
Antagonist - Yes No Zhang C 10.1038/S41594-018-0067-Z 2018-05-30 Yes
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human X-ray 3D4S 3D4S_refined 2.8 A Inactive -1.5 - - - - T4-Lysozyme - timolol pubchem
small molecule Inverse agonist (-)-adrenaline, (-)-... small molecule Yes No Stevens RC 10.1016/J.STR.2008.05.001 2008-06-17 Yes
GLR glucagon Glucagon B1 (Secretin) Human X-ray 5YQZ 5YQZ_refined 3.0 R Inactive -5.0 - - - - T4-Lysozyme - NNC1702
Peptide Partial agonist - No No Wu B 10.1038/NATURE25153 2018-01-17 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Human X-ray 5W0P 5W0P_refined 3.0 D Active 8.6 Arrestin S-arrestin - 87 Endolysin - N/A N/A N/A retinal small molecule No No Xu HE 10.1016/J.CELL.2017.07.002