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. 2018 Jul;16(6):786–848. doi: 10.2174/1570159X16666180308161642

Table 1.

Three-dimensional structures of GPCRs retrieved from the Research Collaboratory for Structural Bioinformatics Protein Data Bank (RCSB PDB) until February 2018.

Rhodopsin-like or Class A GPCRs
PDBid GPCR Main Ligand(s) / Binding Partner(s) Resolution / [Å] Release Date Refs.
4IAQ 5-HT1BR Dihydroergotamine (agonist) 2.80 2013 [232]
4IAR 5-HT1BR Ergotamine (agonist) 2.70 2013 [232]
5V54 5-HT1BR Methiothepin (inverse agonist) 3.90 2018 [233]
4IB4 5-HT2BR Ergotamine (agonist) 2.70 2013 [234]
4NC3 5-HT2BR Ergotamine (agonist) 2.80 2013 [235]
5TUD 5-HT2BR Ergotamine (agonist) and anti-5-HT2B (antibody) 3.00 2017 [236]
5TVN 5-HT2BR Lysergic acid diethylamide (agonist) 2.90 2017 [237]
6BQG 5-HT2CR Ergotamine (agonist) 3.00 2018 [238]
6BQH 5-HT2CR Ritanserin (inverse agonist) 2.70 2018 [238]
5UEN A1AR DU172 (antagonist) 3.20 2017 [239]
2YDO A2AAR Adenosine (agonist) 3.00 2011 [240]
2YDV A2AAR 5′-(N-Ethylcarboxamido)adenosine (agonist) 2.60 2011 [240]
3EML A2AAR ZM241385 (antagonist) 2.60 2008 [44]
3PWH A2AAR ZM241385 (antagonist) 3.30 2011 [241]
3QAK A2AAR UK-432097 (agonist) 2.71 2011 [43]
3REY A2AAR Xanthine amine congener (antagonist) 3.31 2011 [241]
3RFM A2AAR Caffeine (antagonist) 3.60 2011 [241]
3VG9 A2AAR ZM241385 (antagonist) and Fab2838 (inverse agonist) 2.70 2012 [242]
3VGA A2AAR ZM241385 (antagonist) and Fab2838 (inverse agonist) 3.10 2012 [242]
3UZA A2AAR 6-(2,6-Dimethylpyridin-4-yl)-5-phenyl-1,2,4-triazin-3-amine (antagonist) 3.27 2012 [243]
3UZC A2AAR 4-(3-Amino-5-phenyl-1,2,4-triazin-6-yl)-2-chlorophenol (antagonist) 3.34 2012 [243]
4EIY A2AAR ZM241385 (antagonist) 1.80 2012 [244]
4UG2 A2AAR CGS21680 (agonist) 2.60 2015 [245]
4UHR A2AAR CGS21680 (agonist) 2.60 2015 [245]
5G53 A2AAR 5′-(N-Ethylcarboxamido)adenosine (agonist) and Gs proteins 3.40 2016 [246]
5IU4 A2AAR ZM241385 (antagonist) 1.72 2016 [247]
5IU7 A2AAR 2-(Furan-2-yl)-N5-(2-(4-phenylpiperidin-1-yl)ethyl)-1,2-dihydro-[1,2,4]triazolo[1,5-a][1,3,5]triazine-5,7-diamine (antagonist) 1.90 2016 [247]
5IU8 A2AAR 2-(Furan-2-yl)-N5-(2-(4-methylpiperazin-1-yl)ethyl)-1,2-dihydro-[1,2,4]triazolo[1,5-a][1,3,5]triazine-5,7-diamine (antagonist) 2.00 2016 [247]
5IUA A2AAR 2-(Furan-2-yl)-N5-(3-(4-phenylpiperazin-1-yl)propyl)-1,2-dihydro-[1,2,4]triazolo[1,5-a][1,3,5]triazine-5,7-diamine (antagonist) 2.20 2016 [247]
5IUB A2AAR N5-(2-(4-(2,4-Difluorophenyl)piperazin-1-yl)ethyl)-2-(furan-2-yl)-1,2-dihydro-[1,2,4]triazolo[1,5-a][1,3,5]triazine-5,7-diamine (antagonist) 2.10 2016 [247]
5JTB A2AAR ZM241385 (antagonist) 2.80 2017 [248]
5K2A A2AAR ZM241385 (antagonist) 2.50 2016 [249]
Rhodopsin-like or Class A GPCRs
PDBid GPCR Main Ligand(s) / Binding Partner(s) Resolution / [Å] Release Date Refs.
5K2B A2AAR ZM241385 (antagonist) 2.50 2016 [249]
5K2C A2AAR ZM241385 (antagonist) 1.90 2016 [249]
5K2D A2AAR ZM241385 (antagonist) 1.90 2016 [249]
5NLX A2AAR ZM241385 (antagonist) 2.14 2017 [250]
5NM2 A2AAR ZM241385 (antagonist) 1.95 2017 [250]
5OLG A2AAR ZM241385 (antagonist) 1.87 2018 [251]
5OLH A2AAR Vipadenant (antagonist) 2.60 2018 [251]
5OLO A2AAR Tozadenant (antagonist) 3.10 2018 [251]
5OLV A2AAR LUAA47070 (antagonist) 2.00 2018 [251]
5OLZ A2AAR 4-(3-Amino-5-phenyl-1,2,4-triazin-6-yl)-2-chlorophenol (antagonist) 1.90 2018 [251]
5OM1 A2AAR 4-(3-Amino-5-phenyl-1,2,4-triazin-6-yl)-2-chlorophenol (antagonist) 2.10 2018 [251]
5OM4 A2AAR 4-(3-Amino-5-phenyl-1,2,4-triazin-6-yl)-2-chlorophenol (antagonist) 2.00 2018 [251]
5UIG A2AAR 5-Amino-N-[(2-methoxyphenyl)methyl]-2-(3-methylphenyl)-2H-1,2,3-triazole-4-carboximidamide (antagonist) 3.50 2017 [252]
5UVI A2AAR ZM241385 (antagonist) 3.20 2017 [253]
5VRA A2AAR ZM241385 (antagonist) 2.35 2017 [254]
5WF5 A2AAR UK432097 (antagonist) 2.60 2018 [255]
5WF6 A2AAR UK432097 (antagonist) 2.90 2018 [255]
6AQF A2AAR ZM241385 (antagonist) 2.51 2018 [256]
5VBL APJR AMG3054 (agonist) 2.60 2017 [257]
4YAY AT1R ZD7155 (antagonist) 2.90 2015 [258]
4ZUD AT2R Olmesartan (inverse agonist) 2.80 2015 [259]
5UNF AT2R L-161,638 (antagonist) 2.80 2017 [260]
5UNG AT2R L-161,638 (antagonist) 2.80 2017 [260]
5UNH AT2R (N-[(Furan-2-yl)methyl]-N-(4-oxo-2-propyl-3-{[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl}-3,4-dihydroquinazolin-6-yl)benzamide) (antagonist) 2.90 2017 [260]
6F3Y B1R Des-Arg10-kallidin (agonist) NMR 2018 [261]
6F3V B2R Bradykinin (agonist) NMR 2018 [261]
2VT4 β1AR Cyanopindolol (antagonist) 2.70 2008 [262]
2Y00 β1AR Dobutamine (partial agonist) 2.50 2011 [263]
2Y01 β1AR Dobutamine (partial agonist) 2.60 2011 [263]
2Y02 β1AR Carmoterol (agonist) 2.60 2011 [263]
2Y03 β1AR Isoprenaline (agonist) 2.85 2011 [263]
2Y04 β1AR Salbutamol (partial agonist) 3.05 2011 [263]
2YCY β1AR Cyanopindolol (antagonist) 3.15 2011 [264]
2YCW β1AR Carazolol (antagonist) 3.10 2011 [264]
2YCX β1AR Cyanopindolol (antagonist) 3.25 2011 [264]
2YCZ β1AR Iodocyanopindolol (antagonist) 3.65 2011 [264]
3ZPQ β1AR 4-(Piperazin-1-yl)-1H-indole (antagonist) 2.80 2013 [265]
Rhodopsin-like or Class A GPCRs
PDBid GPCR Main Ligand(s) / Binding Partner(s) Resolution / [Å] Release Date Refs.
3ZPR β1AR 4-Methyl-2-(piperazin-1-yl)quinoline (antagonist) 2.70 2013 [265]
4AMI β1AR Bucindolol (agonist) 3.20 2012 [266]
4AMJ β1AR Carvedilol (agonist) 2.30 2012 [266]
4BVN β1AR Cyanopindolol (antagonist) 2.10 2014 [267]
4GPO β1AR - 3.50 2013 [268]
5A8E β1AR 7-Methylcyanopindolol (inverse agonist) 2.40 2015 [269]
5F8U β1AR Cyanopindolol (antagonist) 3.35 2015 [270]
2R4R β2AR Fab5 (antibody) and carazolol (inverse agonist) 3.40 2007 [271]
2R4S β2AR Fab5 (antibody) and carazolol (inverse agonist) 3.40 2007 [271]
2RH1 β2AR Carazolol (inverse agonist) 2.40 2007 [272]
3D4S β2AR Timolol (partial inverse agonist) 2.80 2008 [273]
3KJ6 β2AR Fab5 (antibody) 3.40 2010 [274]
3NY8 β2AR ICI-118,551 (inverse agonist) 2.84 2010 [275]
3NY9 β2AR Ethyl 4-({(2S)-2-hydroxy-3-[(1-methylethyl)amino]propyl}oxy)-3-methyl-1-benzofuran-2-carboxylate (inverse agonist) 2.84 2010 [275]
3NYA β2AR Alprenolol (antagonist) 3.16 2010 [275]
3P0G β2AR Nb80 (nanobody) and BI-167107 (agonist) 3.50 2011 [276]
3PDS β2AR FAUC50 (agonist) 3.50 2011 [42]
3SN6 β2AR Gs proteins 3.20 2011 [277]
4GBR β2AR Carazolol (inverse agonist) 3.99 2012 [278]
5D5A β2AR Carazolol (inverse agonist) 2.48 2016 [279]
5D5B β2AR Carazolol (inverse agonist) 3.80 2016 [279]
5JQH β2AR Nb60 (nanobody) and carazolol (inverse agonist) 3.20 2016 [280]
5X7D β2AR Carazolol (inverse agonist) and 4-carbamoyl-N-[(2R)-2-cyclohexyl-2-phenylacetyl)]-L-phenylalanyl-3-bromo-N-methyl-L-phenylalaninamide (NAM) 2.70 2017 [281]
5O9H C5aR1 NDT9513727 (inverse agonist) 2.70 2018 [282]
5U09 CB1R Taranabant (inverse agonist) 2.60 2016 [283]
5TGZ CB1R AM6538 (antagonist) 2.80 2016 [284]
5T1A CCR2 BMS-681 (orthosteric antagonist) and CCR-RA-[R] (NAM) 2.81 2016 [285]
2RRS CCR5 - NMR 2012 [286]
4MBS CCR5 Maraviroc (antagonist) 2.71 2013 [287]
5LWE CCR9 Vercirnon (NAM) 2.60 2016 [288]
2LNL CXCR1 - NMR 2012 [289]
3ODU CXCR4 IT1t (antagonist) 2.50 2010 [290]
3OE0 CXCR4 CVX15 (antagonist) 2.90 2010 [290]
3OE6 CXCR4 IT1t (antagonist) 3.20 2010 [290]
3OE8 CXCR4 IT1t (antagonist) 3.10 2010 [290]
3OE9 CXCR4 IT1t (antagonist) 3.10 2010 [290]
4RWS CXCR4 vMIP-II complex (antagonist) 3.10 2015 [291]
2N55 CXCR5 CXCL12 (agonist) NMR 2016 [292]
Rhodopsin-like or Class A GPCRs
PDBid GPCR Main Ligand(s) / Binding Partner(s) Resolution / [Å] Release Date Refs.
6CM4 D2R Risperidone (inverse agonist) 2.87 2018 [293]
3PBL D3R Eticlopride (antagonist) 2.89 2010 [294]
5WIU D4R Nemonapride (antagonist) 1.96 2017 [295]
5WIV D4R Nemonapride (antagonist) 2.14 2017 [295]
4N6H DOR Naltrindole (antagonist) 1.80 2013 [296]
4RWA DOR DIPP-NH2 (antagonist) 3.28 2015 [297]
4RWD DOR DIPP-NH2 (antagonist) 2.70 2015 [297]
5GLH ETBR Endothelin-1 (agonist) 2.80 2016 [298]
5GLI ETBR - 2.50 2016 [298]
4PHU FFAR1 TAK-875 (PAM) 2.33 2014 [299]
5TZR FFAR1 MK-8666 (partial agonist) 2.20 2017 [300]
5TZY FFAR1 AP8 (ago-PAM) and MK-8666 (partial agonist) 3.22 2017 [300]
4AY9 FSHR FSH (agonist) 2.50 2012 [301]
4MQW FSHR FSH (agonist) 2.90 2014 [302]
3RZE H1R Doxepin (antagonist) 3.10 2011 [303]
4DJH KOR JDTic (antagonist) 2.90 2012 [304]
6B73 KOR Nb39 (nanobody) and MP1104 (agonist) 3.10 2018 [305]
4Z34 LPAR1 ONO9780307 (antagonist) 3.00 2015 [306]
4Z35 LPAR1 ONO9910539 (antagonist) 2.90 2015 [306]
4Z36 LPAR1 ONO3080573 (antagonist) 2.90 2015 [306]
5CXV mAChR1 Tiotropium (inverse agonist) 2.70 2016 [307]
3UON mAChR2 R-(-)-Quinuclidinyl benzilate (inverse agonist) 3.00 2012 [308]
4MQS mAChR2 Iperoxo (agonist) 3.50 2013 [309]
4MQT mAChR2 Iperoxo (agonist) and LY2119620 (PAM) 3.70 2013 [309]
4DAJ mAChR3 Tiotropium (inverse agonist) 3.40 2012 [310]
4U14 mAChR3 Tiotropium (inverse agonist) 3.57 2014 [311]
4U15 mAChR3 Tiotropium (inverse agonist) 2.80 2014 [311]
4U16 mAChR3 N-Methylscopolamine (antagonist) 3.70 2014 [311]
5DSG mAChR3 Tiotropium (inverse agonist) 2.60 2016 [307]
4DKL MOR β-Funaltrexamine (antagonist) 2.80 2012 [312]
5C1M MOR BU72 (agonist) 2.10 2015 [313]
4EJ4 N/OFQR Naltrindole (antagonist) 3.40 2012 [314]
4GRV N/OFQR Neurotensin 8-13 (agonist) 2.80 2012 [315]
5DHG N/OFQR C35 (antagonist) 3.00 2015 [316]
5DHH N/OFQR SB612111 (antagonist) 3.00 2015 [316]
3ZEV NTSR1 TM86V-∆IC3A 3.00 2014 [317]
4BUO NTSR1 TM86V-∆IC3B 2.75 2014 [317]
4BV0 NTSR1 OGG7V-∆IC3A 3.10 2014 [317]
4BWB NTSR1 HTGH4-∆IC3 3.57 2014 [317]
4XEE NTSR1 Neurotensin/Neuromedin N (agonist) 2.90 2015 [318]
4XES NTSR1 Neurotensin/Neuromedin N (agonist) 2.60 2015 [318]
Rhodopsin-like or Class A GPCRs
PDBid GPCR Main Ligand(s) / Binding Partner(s) Resolution / [Å] Release Date Refs.
5T04 NTSR1 Neurotensin 8-13 (Arg-Arg-Pro-Tyr-Ile-Leu; agonist) 3.30 2016 [319]
4ZJ8 OX1R Suvorexant (antagonist) 2.75 2016 [320]
4ZJC OX1R SB-674042 (antagonist) 2.83 2016 [320]
4S0V OX2R Suvorexant (antagonist) 2.50 2015 [321]
4XNV P2Y1R BPTU (antagonist) 2.20 2015 [322]
4XNW P2Y1R MRS2500 (antagonist) 2.70 2015 [322]
4NTJ P2Y12R AZD1283 (agonist) 2.62 2014 [323]
4PXZ P2Y12R 2MeSADP (agonist) 2.50 2014 [324]
4PY0 P2Y12R 2MeSATP (partial agonist) 3.10 2014 [324]
3VW7 PAR1 Vorapaxar (antagonist) 2.20 2012 [325]
5NDD PAR2 AZ8838 (antagonist) 2.80 2017 [326]
5NDZ PAR2 AZ3451 (antagonist) 3.60 2017 [326]
5NJ6 PAR2 Fab3949 (antibody) and AZ7188 (antagonist) 4.00 2017 [326]
1F88 RHO 11-cis-Retinal (agonist) 2.80 2000 [231]
1GZM RHO 11-cis-Retinal (agonist) 2.65 2003 [327]
1HZX RHO 11-cis-Retinal (agonist) 2.80 2001 [328]
1JFP RHO 11-cis-Retinal (agonist) NMR 2001 [329]
1L9H RHO 11-cis-Retinal (agonist) 2.60 2002 [330]
1LN6 RHO 11-cis-Retinal (agonist) NMR 2002 [331]
1U19 RHO 11-cis-Retinal (agonist) 2.20 2004 [332]
2G87 RHO 11-cis-Retinal (agonist) 2.60 2006 [333]
2HPY RHO 11-cis-Retinal (agonist) 2.80 2006 [334]
2I35 RHO 11-cis-Retinal (agonist) 3.80 2006 [335]
2I36 RHO - 4.10 2006 [335]
2I37 RHO - 4.15 2006 [335]
2J4Y RHO 11-cis-Retinal (agonist) 3.40 2007 [336]
2PED RHO 11-cis-Retinal (agonist) 2.95 2007 [337]
2X72 RHO Gαt1 and 11-cis-retinal (agonist) 3.00 2011 [338]
2Z73 RHO 11-cis-Retinal (agonist) 2.50 2008 [339]
2ZIY RHO 11-cis-Retinal (agonist) 3.70 2008 [340]
3AYM RHO 11-cis-Retinal (agonist) 2.80 2011 [341]
3AYN RHO 11-cis-Retinal (agonist) 2.70 2011 [341]
3C9L RHO 11-cis-Retinal (agonist) 2.65 2008 [342]
3C9M RHO 11-cis-Retinal (agonist) 3.40 2008 [342]
3CAP RHO - 2.90 2008 [343]
3DQB RHO Gαt1 3.20 2008 [344]
3PQR RHO Gαt1 and 11-cis-retinal (agonist) 2.85 2011 [345]
3PXO RHO 11-cis-Retinal (agonist) 3.00 2011 [345]
3OAX RHO β-Ionone and 11-cis-retinal (agonist) 2.60 2011 [346]
4A4M RHO Gαt3 and 11-cis-retinal (agonist) 3.30 2012 [347]
4BEY RHO Gαt2 2.90 2013 [348]
Rhodopsin-like or Class B GPCRs
PDBid GPCR Ligand(s) / Binding Partner(s) Resolution / [Å] Release Date Refs.
4BEZ RHO - 3.30 2013 [348]
4J4Q RHO Gαt1 2.65 2013 [349]
4PXF RHO Arrestin-1 2.75 2014 [350]
4X1H RHO Gαt1 2.29 2015 [351]
4ZWJ RHO - 3.30 2015 [352]
5DGY RHO Visual arrestin-1 7.70 2016 [353]
5DYS RHO 11-cis-Retinal (agonist) 2.30 2016 [354]
5EN0 RHO Gαt3 and 11-cis-retinal (agonist) 2.81 2016 [354]
5TE3 RHO - 2.70 2017 [355]
5TE5 RHO (2E)-{(4E)-4-[(3E)-4-(2,6,6-Trimethylcyclohex-1-en-1-yl)but-3-en-2-ylidene]cyclohex-2-en-1-ylidene}acetaldehyde 4.01 2017 [355]
5W0P RHO Visual arrestin-1 3.01 2017 [356]
5WKT RHO Transducin Gα peptide (GαCT2) 3.20 2017 [254]
3V2W S1PR1 ML056 (antagonist) 3.35 2012 [357]
3V2Y S1PR1 CYM-5442 (agonist) 2.80 2012 [357]
2XWT TSHR K1-70 (antagonist) 1.90 2011 [358]
3G04 TSHR Thyroid-stimulating human monoclonal autoantibody (M22) 2.55 2009 [359]
4XT1 US28 CX3CL1 (agonist) 2.89 2015 [360]
4XT3 US28 CX3CL1 (agonist) 3.80 2015 [360]
4JQI V2R Arrestin-2 2.60 2013 [361]
Secretin-like or Class B GPCRs
PDBid GPCR Ligand(s) / Binding Partner(s) Resolution / [Å] Release Date Refs.
3EHS CRFR1 - 2.76 2008 [362]
3EHT CRFR1 CRF (agonist) 3.40 2008 [362]
3EHU CRFR1 CRF (agonist) 1.96 2008 [362]
4K5Y CRFR1 CP-376395 (antagonist) 2.98 2013 [363]
4Z9G CRFR1 CP-376395 (antagonist) 3.18 2016 [364]
3AQF CRLR RAMP2 2.60 2011 [365]
3N7P CRLR RAMP1 2.80 2010 [366]
3N7R CRLR RAMP1 and telcagepant (antagonist) 2.90 2010 [366]
3N7S CRLR RAMP1 and olcegepant (antagonist) 2.10 2010 [366]
5UZ7 CRLR Gs proteins 4.10 2017 [367]
5V6Y CRLR RAMP1 and adrenomedullin variant (antagonist) 2.80 2018 [368]
4ERS GLP1R mAb1 (antagonist) 2.64 2012 [369]
4L6R GLP1R Glucagon (agonist) 3.30 2013 [370]
5EE7 GLP1R MK-0893 (antagonist) 2.50 2016 [371]
5NX2 GLP1R Peptide 5 (agonist) 3.70 2017 [372]
5VAI GLP1R Gs proteins 4.10 2017 [373]
5VEW GLP1R PF-06372222 (NAM) 2.70 2017 [374]
5VEX GLP1R NNC0640 (NAM) 3.00 2017 [374]
3H3G PTH1R PTHrP 1.94 2009 [375]
Glutamate-like or Class C GPCRs
PDBid GPCR Ligand(s) / Binding Partner(s) Resolution / [Å] Release Date Refs.
4MQE GABABR - 2.35 2013 [376]
4MQF GABABR 2-Hydroxysaclofen (antagonist) 2.22 2013 [376]
4MR7 GABABR CGP54626 (antagonist) 2.15 2013 [376]
4MR8 GABABR CGP35348 (antagonist) 2.15 2013 [376]
4MR9 GABABR SCH50911 (antagonist) 2.35 2013 [376]
4MRM GABABR Phaclofen (antagonist) 2.86 2013 [376]
4MS1 GABABR CGP46381 (antagonist) 2.25 2013 [376]
4MS3 GABABR γ-Aminobutyric acid (agonist) 2.50 2013 [376]
4MS4 GABABR Baclofen (agonist) 1.90 2013 [376]
4OR2 mGluR1 FITM (NAM) 2.80 2014 [377]
1EWK mGluR1 Glutamate (agonist) 2.20 2000 [378]
1EWT mGluR1 - 3.70 2000 [378]
1EWV mGluR1 - 4.00 2000 [378]
5CNI mGluR2 Glutamate (agonist) 2.69 2015 [379]
5CNJ mGluR2 LY2812223 (agonist) 2.65 2015 [379]
2E4U mGluR3 Glutamate (agonist) 2.35 2007 [380]
2E4V mGluR3 DCG-IV (agonist) 2.40 2007 [380]
2E4W mGluR3 1S,3S-ACPD (agonist) 2.40 2007 [380]
2E4X mGluR3 1S,3R-ACPD (agonist) 2.75 2007 [380]
2E4Y mGluR3 2R,4R-APDC (agonist) 3.40 2007 [380]
5CNK mGluR3 Glutamate (agonist) 3.15 2015 [379]
5CNM mGluR3 LY2812223 (agonist) 2.84 2015 [379]
4OO9 mGluR5 Mavoglurant (NAM) 2.60 2014 [381]
5CGC mGluR5 3-Chloro-4-fluoro-5-[6-(1H-pyrazol-1-yl)pyrimidin-4-yl]benzonitrile (NAM) 3.10 2015 [382]
5CGD mGluR5 HTL14242 (NAM) 2.60 2015 [382]
6FFH mGluR5 Fenobam (NAM) 2.65 2018 [383]
6FF1 mGluR5 MMPEP (NAM) 2.20 2018 [383]
2E4Z mGluR7 - 3.30 2007 [380]
Frizzled/taste2-like or Class F GPCRs
PDBid GPCR Ligand(s) / Binding Partner(s) Resolution / [Å] Release Date Reference
4JKV Smo LY2940680 (antagonist) 2.45 2013 [384]
4N4W Smo SANT-1 (antagonist) 2.80 2014 [385]
4O9R Smo Cyclopamine (antagonist) 3.20 2014 [386]
4QIM Smo Anta XV (antagonist) 2.61 2014 [385]
4QIN Smo SAG1.5 (agonist) 2.60 2014 [385]
5KZV Smo 20(S)-Hydroxycholesterol (agonist) 1.62 2016 [387]
5KZY Smo Cyclopamine (antagonist) 2.48 2016 [387]
5KZZ Smo - 1.33 2016 [387]
5L7D Smo Cholesterol (agonist) 3.20 2016 [388]
5L7I Smo Vismodegib (antagonist) 3.30 2016 [388]
Frizzled/taste2-like or Class F GPCRs
PDBid GPCR Ligand(s) / Binding Partner(s) Resolution / [Å] Release Date Reference
5V56 Smo TC114 (antagonist) 2.90 2017 [389]
5V57 Smo TC114 (antagonist) 3.00 2017 [389]
Adhesion GPCRs
PDBid GPCR Ligand(s) / Binding Partner(s) Resolution / [Å] Release date Reference
5KVM ADGRG1 FN3 monobody 2.45 2016 [390]
4RMK ADGRL3 - 1.61 2015 [391]
4RML ADGRL3 - 1.60 2015 [391]
5FTT ADGRL3 Unc5D and FLRT2 3.40 2016 [392]
5FTU ADGRL3 Unc5D and FLRT2 6.01 2016 [392]

Abbrevations: (5-HTR - 5-HydroxyTryptamine receptor; ADGRG1 - Adhesion G-protein coupled Receptor G1; ADGRL3 - Adhesion G-protein coupled Receptor L3; AR - Adenosine Receptor; APJR - Apelin Receptor; ATR - Angiotensin II Receptor; BR – Bradykinin Receptor; βAR: - β-Adrenergic Receptor; C5aR – C5a anaphylatoxin chemotactic Receptor; CBR - Cannabinoid Receptor; CCR - CC Chemokine Receptor; CRF - Corticotropin Releasing Factor; CRFR - Corticotropin Releasing Factor Receptor; CRLR - Calcitonin Receptor-Like Receptor; CXCR - CXC Chemokine Receptor; DOR - δ-Opioid Receptor; DR - Dopamine Receptor; ETR - Endothelin Receptor; FFAR - Free Fatty Acid Receptor; FLRT2 - Fibronectin Leucin-Rich Transmembrane protein 2; FN3 - FibroNectin type III domain; FSH - Follicle-Stimulating Hormone; FSHR - Follicle-Stimulating Hormone Receptor; GABAR - γ-AminoButyric Acid Receptor; GLPR - Glucagon-Like Peptide Receptor; HR - Histamine Receptor; KOR - κ-Opioid Receptor; LPAR - LysoPhosphatidic Acid Receptor; mAChR - muscarinic AcetylCholine Receptor; mGluR - metabotropic Glutamate Receptor; MOR - μ-Opioid Receptor; N/OFQR - Nociceptin/Orphanin FQ Receptor; NTSR - Neurotensin Receptor; OXR - Orexin Receptor; P2YR - Purinergic P2Y Receptor; PAR - Protease-Activated Receptor; PTHR - ParaThyroid Hormone-related peptide Receptor; PTHrP - ParaThyroid Hormone-related Peptide; RAMP - Receptor-Activity Modifying Protein; RHO - Rhodopsin; S1PR - Sphingosine-1-Phosphate Receptor; Smo - Smoothened Receptor; TSHR - Thyroid-Stimulating Hormone Receptor; Unc5D - Unc5D guidance receptor; US28 - Cytomegalovirus-encoded chemokine Receptor; VIPR - Vasoactive Intestinal Peptide Receptor; VR - Vasopressin Receptor).