Table

The Costanzi Research Group

Experimentally solved GPCR structures
(Updated May 22, 2019)

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Row Family Receptor Organism PDB ID Res. (Ang.) Ligand Ligand chemical class Ligand type More on ligand type Putative State Signaling Partner Fusion protein Method Notes Year References
1FrizzledSmoothenedHuman4JKV2.45LY2940680small moleculeantagonistNAinactiveNABRIL-NTX-RAYNA2013Wang et al. 2013
2FrizzledSmoothenedHuman4N4W2.8SANT-1small moleculeantagonistNAinactiveNABRIL-NTX-RAYNA2014Wang et al. 2014
3FrizzledSmoothenedHuman4O9R3.2Cyclopaminesmall moleculeantagonistNAinactiveNABRIL-NTX-RAYNA2014Weierstall et al. 2014
4FrizzledSmoothenedHuman4QIM2.61ANTA XVsmall moleculeantagonistNAinactiveNABRIL-IL3X-RAYNA2014Wang et al. 2014
5FrizzledSmoothenedHuman4QIN2.6SAG1.5small moleculeagonistNAinactive or minimally activatedNABRIL-IL3X-RAYNA2014Wang et al. 2014
6FrizzledSmoothenedHuman5L7D3.2Cholesterolsmall moleculeallosteric ligandbound to extracellular cysteine-rich domain (CRO) inactiveNATBDX-RAYTBD2016Byrne et al. 2016
7FrizzledSmoothenedHuman5L7I3.3Vismodegibsmall moleculeantagonistNAinactiveNATBDX-RAYTBD2016Byrne et al. 2016
8SecretinCRF1 corticotropin-releasing factor receptorHuman4K5Y2.98CP-376395small moleculeantagonistnegative allosteric modulatorinactiveNANAX-RAYc2013Hollenstein et al. 2013
9SecretinGlucagon receptorHuman4L6R3.3unligandedunligandedunligandedNAinactiveNABRIL-NTX-RAYNA2013Siu et al. 2013
10SecretinCRF1 corticotropin-releasing factor receptorHuman4Z9G3.18CP-376395small moleculeallosteric antagonistallostericinactiveNATBDX-RAYTBD2016Dore et al. 2016
11SecretinGlucagon receptorHuman5EE72.5MK-0893small moleculeantagonistAllostericinactiveNATBDX-RAYNA2016Jazayeri et al. 2016
12RhodopsinRhodopsinBovine1F882.811-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NANAX-RAYNA2000Palczewski et al. 2000
13RhodopsinRhodopsinBovine1GZM2.6511-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NANAX-RAYNA2003Li et al. 2003
14RhodopsinRhodopsinBovine1HZX2.811-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NANAX-RAYNA2001Teller et al. 2001
15RhodopsinRhodopsinBovine1L9H2.611-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NANAX-RAYNA2002Okada et al. 2002
16RhodopsinRhodopsinBovine1U192.211-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NANAX-RAYNA2004Okada et al. 2004
17RhodopsinRhodopsinBovine2G872.6all-trans-retinal (distorted)small moleculeagonistNAinactive or minimally activated (bathorhodopsin)NANAX-RAYNA2006Nakamichi et al. 2006
18RhodopsinRhodopsinBovine2HPY2.8all-trans-retinalsmall moleculeagonistNAinactive or minimally activated (lumirhodopsin)NANAX-RAYNA2006Nakamichi et al. 2006
19RhodopsinRhodopsinBovine2I353.811-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NANAX-RAYNA2006Salom et al. 2006
20RhodopsinRhodopsinBovine2I364.111-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NANAX-RAYNA2006Salom et al. 2006
21RhodopsinRhodopsinBovine2I374.15all-trans-retinalsmall moleculeagonistNAinactive or minimally activated (early photoactivation intermediate)NANAX-RAYa b2006Salom et al. 2006
22RhodopsinRhodopsinBovine2J4Y3.411-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NANAX-RAYc2007Standfuss et al. 2007
23RhodopsinRhodopsinBovine2PED2.959-cis-retinalsmall moleculeinverse agonistNAinactive (isorhodopsin)NANAX-RAYNA2007Nakamichi et al. 2007
24Rhodopsinbeta2 adrenergic receptorHuman2R4R3.4carazololsmall moleculeinverse agonistNAinactiveNANAX-RAYa o2007Rasmussen et al. 2007
25Rhodopsinbeta2 adrenergic receptorHuman2R4S3.4carazololsmall moleculeinverse agonistNAinactiveNANAX-RAYa o2007Rasmussen et al. 2007
26Rhodopsinbeta2 adrenergic receptorHuman2RH12.4carazololsmall moleculeinverse agonistNAinactiveNAT4L-IL3X-RAYb2007Cherezov et al. 2007
27Rhodopsinbeta1 adrenergic receptorTurkey2VT42.7cyanopindololsmall moleculeantagonistNAinactiveNANAX-RAYc2008Warne et al. 2008
28RhodopsinRhodopsinBovine2X723.0all-trans-retinalsmall moleculeagonistNAactivated (metarhodopsin II)NAC-terminal peptide Galpha-tX-RAYg2011Standfuss et al. 2011
29Rhodopsinbeta1 adrenergic receptorTurkey2Y002.5dobutaminesmall moleculeagonistpartial agonistinactive or minimally activatedNANAX-RAYc2011Warne et al. 2011
30Rhodopsinbeta1 adrenergic receptorTurkey2Y012.6dobutaminesmall moleculeagonistpartial agonistinactive or minimally activatedNANAX-RAYc2011Warne et al. 2011
31Rhodopsinbeta1 adrenergic receptorTurkey2Y022.6carmoterolsmall moleculeagonistNAinactive or minimally activatedNANAX-RAYc2011Warne et al. 2011
32Rhodopsinbeta1 adrenergic receptorTurkey2Y032.85isoprenalinesmall moleculeagonistNAinactive or minimally activatedNANAX-RAYc2011Warne et al. 2011
33Rhodopsinbeta1 adrenergic receptorTurkey2Y043.05salbutamolsmall moleculeagonistpartial agonistinactive or minimally activatedNANAX-RAYc2011Warne et al. 2011
34Rhodopsinbeta1 adrenergic receptorTurkey2YCW3.0carazololsmall moleculeantagonistNAinactiveNANAX-RAYc f2011Moukhametzianov et al. 2011
35Rhodopsinbeta1 adrenergic receptorTurkey2YCX3.25cyanopindololsmall moleculeantagonistNAinactiveNANAX-RAYc f2011Moukhametzianov et al. 2011
36Rhodopsinbeta1 adrenergic receptorTurkey2YCY3.15cyanopindololsmall moleculeantagonistNAinactiveNANAX-RAYc2011Moukhametzianov et al. 2011
37Rhodopsinbeta1 adrenergic receptorTurkey2YCZ3.65iodocyanopindololsmall moleculeantagonistNAinactiveNANAX-RAYc2011Moukhametzianov et al. 2011
38RhodopsinA2A adenosine receptorHuman2YDO3.0adenosinesmall moleculeagonistNAinactive or minimally activatedNANAX-RAYc2011Lebon et al. 2011
39RhodopsinA2A adenosine receptorHuman2YDV2.6NECAsmall moleculeagonistNAinactive or minimally activatedNANAX-RAYc2011Lebon et al. 2011
40RhodopsinRhodopsinSquid2Z732.511-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NANAX-RAYNA2008Murakami et al. 2008
41RhodopsinRhodopsinSquid2ZIY3.711-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NANAX-RAYNA2008Shimamura et al. 2008
42RhodopsinRhodopsinSquid3AYM2.8all-trans-retinalsmall moleculeagonistNAinactive or minimally activated (bathorhodopsin)NANAX-RAYNA2011Murakami et al. 2011
43RhodopsinRhodopsinSquid3AYN2.79-cis-retinalsmall moleculeinverse agonistNAinactive (isorhodopsin)NANAX-RAYNA2011Murakami et al. 2011
44RhodopsinRhodopsinBovine3C9L2.6511-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NANAX-RAYd2008Stenkamp et al. 2008
45RhodopsinRhodopsinBovine3C9M3.411-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NANAX-RAYe2008Stenkamp et al. 2008
46RhodopsinRhodopsinBovine3CAP2.9unligandedunligandedunligandedNAactivated opsinNANAX-RAYb2008Park et al. 2008
47Rhodopsinbeta2 adrenergic receptorHuman3D4S2.8timololsmall moleculeinverse agonistNAinactiveNAT4L-IL3X-RAYNA2008Hanson et al. 2008
48RhodopsinRhodopsinBovine3DQB3.2unligandedunligandedunligandedNAactivated opsinNAC-terminal peptide Galpha-tX-RAYNA2008Scheerer et al. 2008
49RhodopsinA2A adenosine receptorHuman3EML2.6ZM-241385small moleculeantagonistNAinactiveNAT4L-IL3X-RAYNA2008Jaakola et al. 2008
50Rhodopsinbeta2 adrenergic receptorHuman3KJ63.4carazololsmall moleculeinverse agonistNAinactiveNANAX-RAYa o2010Bokoch et al. 2010
51Rhodopsinbeta2 adrenergic receptorHuman3NY82.84ICI 118551small moleculeinverse agonistNAinactiveNAT4L-IL3X-RAYNA2010Wacker et al. 2010
52Rhodopsinbeta2 adrenergic receptorHuman3NY92.84recent comp.small moleculeinverse agonistNAinactiveNAT4L-IL3X-RAYNA2010Wacker et al. 2010
53Rhodopsinbeta2 adrenergic receptorHuman3NYA3.16alprenololsmall moleculeantagonistNAinactiveNAT4L-IL3X-RAYNA2010Wacker et al. 2010
54RhodopsinRhodopsinBovine3OAX2.611-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NANAX-RAYNA2011Makino et al. 2011
55RhodopsinCXCR4 chemokine receptorHuman3ODU2.5IT1tsmall moleculeantagonistNAinactiveNAT4L-IL3X-RAYb2010Wu et al. 2010
56RhodopsinCXCR4 chemokine receptorHuman3OE02.9CVX15peptideantagonistNAinactiveNAT4L-IL3X-RAYb2010Wu et al. 2010
57RhodopsinCXCR4 chemokine receptorHuman3OE63.2IT1tsmall moleculeantagonistNAinactiveNAT4L-IL3X-RAYb2010Wu et al. 2010
58RhodopsinCXCR4 chemokine receptorHuman3OE83.1IT1tsmall moleculeantagonistNAinactiveNAT4L-IL3X-RAYb2010Wu et al. 2010
59RhodopsinCXCR4 chemokine receptorHuman3OE93.1IT1tsmall moleculeantagonistNAinactiveNAT4L-IL3X-RAYb2010Wu et al. 2010
60Rhodopsinbeta2 adrenergic receptorHuman3P0G3.5BI-167107small moleculeagonistNAactivatedNAT4L-NTX-RAYp2011Rasmussen et al. 2011
61RhodopsinD3 dopamine receptorHuman3PBL2.89Eticlopridesmall moleculeantagonistNAinactiveNAT4L-IL3X-RAYNA2010Chien et al. 2010
62Rhodopsinbeta2 adrenergic receptorHuman3PDS3.5FAUC50small moleculeagonistirreversibleinactive or minimally activatedNAT4L-IL3X-RAYNA2011Rosenbaum et al. 2011
63RhodopsinRhodopsinBovine3PQR2.85all-trans-retinalsmall moleculeagonistNAactivated (metarhodopsin II)NAC-terminal peptide Galpha-tX-RAYNA2011Choe et al. 2011
64RhodopsinA2A adenosine receptorHuman3PWH3.3ZM-241385small moleculeantagonistNAinactiveNANAX-RAYc2011Dore et al. 2011
65RhodopsinRhodopsinBovine3PXO3.0all-trans-retinalsmall moleculeagonistNAactivated (metarhodopsin II)NANAX-RAYNA2011Choe et al. 2011
66RhodopsinA2A adenosine receptorHuman3QAK2.71UK-432097small moleculeagonistNAinactive or minimally activatedNAT4L-IL3X-RAYh2011Xu et al. 2011
67RhodopsinA2A adenosine receptorHuman3REY3.31XACsmall moleculeantagonistNAinactiveNANAX-RAYc2011Dore et al. 2011
68RhodopsinA2A adenosine receptorHuman3RFM3.6caffeinesmall moleculeantagonistNAinactiveNANAX-RAYc2011Dore et al. 2011
69RhodopsinH1 histamine receptorHuman3RZE3.1Doxepinsmall moleculeantagonistNAinactiveNAT4L-IL3X-RAYNA2011Shimamura et al. 2011
70RhodopsinA2A adenosine receptorHuman3UZA3.271 2 4-triazine 4gsmall moleculeantagonistNAinactiveNANAX-RAYc2012Congreve et al. 2012
71RhodopsinA2A adenosine receptorHuman3UZC3.341 2 4-triazine 4gsmall moleculeantagonistNAinactiveNANAX-RAYc2012Congreve et al. 2012
72RhodopsinS1P1 sphingosine 1-phosphate receptorHuman3V2W3.35ML056small moleculeantagonistNAinactiveNAT4L-IL3X-RAYNA2012Hanson et al. 2012
73RhodopsinS1P1 sphingosine 1-phosphate receptorHuman3V2Y2.8ML056small moleculeantagonistNAinactiveNAT4L-IL3X-RAYk2012Hanson et al. 2012
74RhodopsinA2A adenosine receptorHuman3VG92.7ZM-241385small moleculeantagonistNAinactiveNANAX-RAYh o2012Hino et al. 2012
75RhodopsinA2A adenosine receptorHuman3VGA3.1ZM-241385small moleculeantagonistNAinactiveNANAX-RAYo2012Hino et al. 2012
76RhodopsinPAR1 proteinase-activated receptorHuman3VW72.2Vorapaxarsmall moleculeantagonistNAinactiveNAT4L-IL3X-RAYNA2012Zhang et al. 2012
77RhodopsinNTS1 neurotensin receptorRat3ZEV3.0Neurotensin (8-13)peptideagonistNAinactive or minimally activatedNANAX-RAYc2014Egloff et al. 2014
78Rhodopsinbeta1 adrenergic receptorTurkey3ZPQ2.84-(piperazin-1-yl)-1H-indolesmall moleculeantagonistNAinactiveNANAX-RAYc2013Christopher et al. 2013
79Rhodopsinbeta1 adrenergic receptorTurkey3ZPR2.74-methyl-2-(piperazin-1-yl)quinolinesmall moleculeantagonistNAinactiveNANAX-RAYc2013Christopher et al. 2013
80RhodopsinRhodopsinBovine4A4M3.3all-trans-retinalsmall moleculeagonistNAactivated (metarhodopsin II)NANAX-RAYg2012Deupi et al. 2012
81Rhodopsinbeta1 adrenergic receptorTurkey4AMI3.2bucindololsmall moleculeagonistbiased agonist (beta-arrestin)inactive or minimally activatedNANAX-RAYc2012Warne et al. 2012
82Rhodopsinbeta1 adrenergic receptorTurkey4AMJ2.3carvedilolsmall moleculeagonistbiased agonist (beta-arrestin)inactive or minimally activatedNANAX-RAYc2012Warne et al. 2012
83RhodopsinRhodopsinBovine4BEY2.9unligandedunligandedunligandedNAactivated opsinNAC-terminal peptide Galpha-tX-RAYNA2013Singhal et al. 2013
84RhodopsinRhodopsinBovine4BEZ3.3unligandedunligandedunligandedNAactivated opsinNANAX-RAYb2013Singhal et al. 2013
85RhodopsinNTS1 neurotensin receptorRat4BUO2.75Neurotensin (8-13)peptideagonistNAinactive or minimally activatedNANAX-RAYc2014Egloff et al. 2014
86RhodopsinNTS1 neurotensin receptorRat4BV03.1Neurotensin (8-13)peptideagonistNAinactive or minimally activatedNANAX-RAYc2014Egloff et al. 2014
87Rhodopsinbeta1 adrenergic receptorTurkey4BVN2.1cyanopindololsmall moleculeantagonistNAinactiveNANAX-RAYc2014Miller-Gallacher et al. 2014
88RhodopsinNTS1 neurotensin receptorRat4BWB3.57Neurotensin (8-13)peptideagonistNAinactive or minimally activatedNANAX-RAYc2014Egloff et al. 2014
89RhodopsinM3 muscarinic receptorRat4DAJ3.4Tiotropiumsmall moleculeinverse agonistNAinactiveNAT4L-IL3X-RAYNA2012Kruse et al. 2012
90Rhodopsinkappa opioid receptorHuman4DJH2.9JDTicsmall moleculeantagonistNAinactiveNAT4L-IL3X-RAYf p2012Wu et al. 2012
91Rhodopsinmu opioid receptorMouse4DKL2.8funaltrexaminesmall moleculeantagonistirreversibleinactiveNAT4L-IL3X-RAYb2012Manglik et al. 2012
92RhodopsinNociception-orphanin FQ (NOP) receptorHuman4EA33.01Peptide mimetic c-24small moleculeantagonistNAinactiveNABRIL-NTX-RAYNA2012Thompson et al. 2012
93RhodopsinA2A adenosine receptorHuman4EIY1.8ZM-241385small moleculeantagonistNAinactiveNABRIL-IL3X-RAYNA2012Liu et al. 2012
94Rhodopsindelta opioid receptorMouse4EJ43.4Naltrindolesmall moleculeantagonistNAinactiveNAT4L-IL3X-RAYb2012Granier et al. 2012
95Rhodopsinbeta2 adrenergic receptorHuman4GBR3.99carazololsmall moleculeinverse agonistNAinactiveNAT4L-NTX-RAYNA2012Zou et al. 2012
96Rhodopsinbeta1 adrenergic receptorTurkey4GPO3.5unligandedunligandedunligandedNAinactiveNANAX-RAYl2013Huang et al. 2013
97RhodopsinNTS1 neurotensin receptorRat4GRV2.8Neurotensin (8-13)peptideagonistNAactivated (partially)NAT4L-IL3X-RAYc2012White et al. 2012
98Rhodopsin5-HT1B serotonin receptorHuman4IAQ2.8Dihydroergotaminesmall moleculeagonistNAinactive or minimally activatedNABRIL-IL3X-RAYNA2013Wang et al. 2013
99Rhodopsin5-HT1B serotonin receptorHuman4IAR2.7Ergotaminesmall moleculeagonistNAinactive or minimally activatedNABRIL-IL3X-RAYNA2013Wang et al. 2013
100Rhodopsin5-HT2B serotonin receptorHuman4IB42.7Ergotaminesmall moleculeagonistbiased agonist (beta-arrestin)inactive or minimally activatedNABRIL-IL3X-RAYNA2013Wacker et al. 2013
101RhodopsinRhodopsinBovine4J4Q2.65unligandedunligandedunligandedNAactivated opsinNAC-terminal peptide Galpha-tX-RAYNA2013Park et al. 2013
102Rhodopsinbeta2 adrenergic receptorHuman4LDE2.79BI-167107small moleculeagonistNAactivatedNAT4L-NTX-RAYp2013Ring et al. 2013
103Rhodopsinbeta2 adrenergic receptorHuman4LDL3.1Hydroxybenzylisoproterenolsmall moleculeagonistNAactivatedNAT4L-NTX-RAYp2013Ring et al. 2013
104Rhodopsinbeta2 adrenergic receptorHuman4LDO3.2Adrenalinesmall moleculeagonistNAactivatedNAT4L-NTX-RAYp2013Ring et al. 2013
105RhodopsinCCR5 chemokine receptorHuman4MBS2.71Maravirocsmall moleculeinverse agonistNAinactiveNARubredoxin-IL3X-RAYNA2013Tan et al. 2013
106RhodopsinM2 muscarinic receptorHuman4MQS3.5iperoxosmall moleculeagonistNAactivatedNANAX-RAYp2013Kruse et al. 2013
107RhodopsinM2 muscarinic receptorHuman4MQT3.7iperoxo + LY2119620small moleculeagonist + positive allosteric modulatorstructure includes positive allosteric modulator as a second ligandactivatedNANAX-RAYp2013Kruse et al. 2013
108Rhodopsindelta opioid receptorHuman4N6H1.8Naltrindolesmall moleculeantagonistNAinactiveNABRIL-NTX-RAYi2013Fenalti et al. 2013
109Rhodopsin5-HT2B serotonin receptorHuman4NC32.8Ergotaminesmall moleculeagonistbiased agonist (beta-arrestin)inactive or minimally activatedNABRIL-IL3X-RAYj2013Liu et al. 2013
110RhodopsinP2Y12 receptorHuman4NTJ2.62AZD1283small moleculeantagonistNAInactiveNABRIL-IL3X-RAYNA2014Zhang et al. 2014
111RhodopsinFFA1 receptor (GPR40)Human4PHU2.33TAK-875 or fasiglifamsmall moleculeantagonistNAinactiveNAT4L-IL3X-RAYc2014Srivastava et al. 2014
112RhodopsinRhodopsinBovine4PXF2.75unligandedunligandedunligandedNAactivated opsinNAArrestin-1 peptideX-RAYNA2014Szczepek et al. 2014
113RhodopsinP2Y12 receptorHuman4PXZ2.52-MeSADPsmall moleculeagonistNAinactive or minimally activatedNABRIL-IL3X-RAYNA2014Zhang et al. 2014
114RhodopsinP2Y12 receptorHuman4PY03.12-MeSADPsmall moleculeagonistNAinactive or minimally activatedNABRIL-IL3X-RAYNA2014Zhang et al. 2014
115Rhodopsinbeta2 adrenergic receptorHuman4QKX3.3Covalently-bound analog of noradrenalinesmall moleculeagonistirreversibleactivatedNAT4L-NTX-RAYp2014Weichert et al. 2014
116Rhodopsindelta opioid receptorHuman4RWA3.28H-Dmt-Tic-Phe-Phe-NH2 (DIPP-NH2)peptideantagonistdual functioninactiveNABRIL-NTX-RAYNA2015Fenalti et al. 2015
117Rhodopsindelta opioid receptorHuman4RWD2.7H-Dmt-Tic-Phe-Phe-NH2 (DIPP-NH2)peptideantagonistdual functioninactiveNABRIL-NTX-RAYi2015Fenalti et al. 2015
118RhodopsinCXCR4 chemokine receptorHuman4RWS3.1Viral chemokinepeptideantagonistNAinactiveNAT4L-IL3X-RAYNA2015Qin et al. 2015
119RhodopsinOX2 orexin receptorHuman4S0V2.5Suvorexantsmall moleculeantagonistNAinactiveNAGlycogen synthase-IL3X-RAYNA2015Yin et al. 2015
120RhodopsinM3 muscarinic receptorRat4U143.57Tiotropiumsmall moleculeinverse agonistNAinactiveNAdsT4L-IL3X-RAYNA2014Thorsen et al. 2014
121RhodopsinM3 muscarinic receptorRat4U152.8Tiotropiumsmall moleculeinverse agonistNAinactiveNAdsT4L-IL3X-RAYNA2014Thorsen et al. 2014
122RhodopsinM3 muscarinic receptorRat4U163.7N-methyl scopolaminesmall moleculeantagonistNAinactiveNAdsT4L-IL3X-RAYNA2014Thorsen et al. 2014
123RhodopsinA2A adenosine receptorHuman4UG22.6CGS21680small moleculeagonistNAinactive or minimally activatedNANAX-RAYc2015Lebon et al. 2015
124RhodopsinA2A adenosine receptorHuman4UHR2.6CGS21680small moleculeagonistNAinactive or minimally activatedNANAX-RAYc2015Lebon et al. 2015
125RhodopsinRhodopsinSquid4WW32.8all-trans-retinalsmall moleculeagonistNAinactive or minimally activated (lumirhodopsin)NANAX-RAYNA2015Murakami et al. 2015
126RhodopsinRhodopsinBovine4X1H2.29unligandedunligandedunligandedNAactivated opsinNANAX-RAYb2015Blankenship et al. 2015
127RhodopsinNTS1 neurotensin receptorRat4XEE2.9Neurotensin (8-13)peptideagonistNAactivated (partially)NAT4L-IL3X-RAYc2015Krumm et al. 2015
128RhodopsinNTS1 neurotensin receptorRat4XES2.6Neurotensin (8-13)peptideagonistNAactivated (partially)NAT4L-IL3X-RAYc2015Krumm et al. 2015
129RhodopsinP2Y1 receptorHuman4XNV2.2BPTUsmall moleculeantagonistNAinactiveNAT4L-NT and Rubredoxin-IL3X-RAYNA2015Zhang et al. 2015
130RhodopsinP2Y1 receptorHuman4XNW2.7MRS2500small moleculeantagonistNAinactiveNAT4L-NT and Rubredoxin-IL3X-RAYNA2015Zhang et al. 2015
131RhodopsinViral US28 receptorVirus4XT12.89Human CX3CL1peptideagonistNAactivatedNANAX-RAYNA2015Burg et al. 2015
132RhodopsinViral US28 receptorVirus4XT33.8Human CX3CL1peptideagonistNAactivatedNANAX-RAYp2015Burg et al. 2015
133RhodopsinAT1R angiotensin II type 1 receptorHuman4YAY2.9ZD7155small moleculeantagonistNAInactiveNABRIL-NTX-RAYNA2015Zhang et al. 2015
134RhodopsinLPA1 receptorHuman4Z343.0ONO-9780307small moleculeantagonistNAInactiveNABRIL-IL3X-RAYNA2015Chrencik et al. 2015
135RhodopsinLPA1 receptorHuman4Z352.9ONO-9780307small moleculeantagonistNAInactiveNABRIL-IL3X-RAYNA2015Chrencik et al. 2015
136RhodopsinLPA1 receptorHuman4Z362.9ONO-3080573small moleculeantagonistNAInactiveNABRIL-IL3X-RAYNA2015Chrencik et al. 2015
137RhodopsinOX1 orexin receptorHuman4ZJ82.75Suvorexantsmall moleculeantagonistNAinactiveNAGlycogen synthase-IL3X-RAYNA2016Yin et al. 2016
138RhodopsinOX1 orexin receptorHuman4ZJC2.83SB-674042small moleculeantagonistNAinactiveNAGlycogen synthase-IL3X-RAYNA2016Yin et al. 2016
139RhodopsinAT1R angiotensin II type 1 receptorHuman4ZUD2.8Olmesartansmall moleculeantagonistNAInactiveNABRIL-NTX-RAYNA2015Zhang et al. 2015
140RhodopsinRhodopsinHuman4ZWJ3.3all-trans-retinalsmall moleculeagonistNAactivatedVisual arrestin (fusion)T4L-NTX-RAYa g2015Kang et al. 2015
141Rhodopsinbeta1 adrenergic receptorTurkey5A8E2.47-Methylcyanopindololsmall moleculeinverse agonistNAinactiveNANAX-RAYc2015Sato et al. 2015
142Rhodopsinmu opioid receptorMouse5C1M2.1BU75small moleculeagonistNAactivatedNANAX-RAYb p2015Huang et al. 2015
143RhodopsinM1 muscarinic receptorHuman5CXV2.7Tiotropiumsmall moleculeantagonistNAInactiveNAT4L-IL3X-RAYNA2016Thal et al. 2016
144Rhodopsinbeta2 adrenergic receptorHuman5D5A2.48carazololsmall moleculeinverse agonistNAinactiveNAT4L-IL3X-RAYNA2016Huang et al. 2016
145Rhodopsinbeta2 adrenergic receptorHuman5D5B3.8carazololsmall moleculeinverse agonistNAinactiveNAT4L-IL3X-RAYNA2016Huang et al. 2016
146Rhodopsinbeta2 adrenergic receptorHuman5D6L3.2Carazololsmall moleculeinverse agonistNAinactiveNATBDX-RAYTBD2016Ma et al. 2016
147RhodopsinRhodopsinHuman5DGY7.7all-trans-retinalsmall moleculeagonistNAactivatedVisual arrestin (fusion protein)T4L-NTX-RAYa m2016Zhou et al. 2016
148RhodopsinNociception-orphanin FQ (NOP) receptorHuman5DHG3.0C-35small moleculeantagonistNAinactiveNABRIL-NTX-RAYNA2015Miller et al. 2015
149RhodopsinNociception-orphanin FQ (NOP) receptorHuman5DHH3.0SB-612111small moleculeantagonistNAinactiveNABRIL-NTX-RAYNA2015Miller et al. 2015
150RhodopsinM4 muscarinic receptorHuman5DSG2.6Tiotropiumsmall moleculeantagonistNAInactiveNAT4L-IL3X-RAYNA2016Thal et al. 2016
151RhodopsinRhodopsinBovine5DYS2.3all-trans-retinalsmall moleculeagonistNAactivated (metarhodopsin II)NANAX-RAYg2016Singhal et al. 2016
152RhodopsinRhodopsinBovine5EN02.81all-trans-retinalsmall moleculeagonistNAactivated (metarhodopsin II)NANAX-RAYg2016Singhal et al. 2016
153Rhodopsinbeta1 adrenergic receptorTurkey5F8U3.35cyanopindololsmall moleculeantagonistNAinactiveNANAX-RAYl2015Leslie et al. 2015
154RhodopsinA2A adenosine receptorHuman5G533.4NECAsmall moleculeagonistNAactivemini-GsTBDX-RAYTBD2016Carpenter et al. 2016
155RhodopsinA2A adenosine receptorHuman5IU41.72ZM-241385small moleculeantagonistNAinactiveNABRIL-IL3X-RAYTBD2016Segala et al. 2016
156RhodopsinA2A adenosine receptorHuman5IU71.912csmall moleculeantagonistNAinactiveNABRIL-IL3X-RAYTBD2016Segala et al. 2016
157RhodopsinA2A adenosine receptorHuman5IU82.012fsmall moleculeantagonistNAinactiveNABRIL-IL3X-RAYTBD2016Segala et al. 2016
158RhodopsinA2A adenosine receptorHuman5IUA2.212bsmall moleculeantagonistNAinactiveNABRIL-IL3X-RAYTBD2016Segala et al. 2016
159RhodopsinA2A adenosine receptorHuman5IUB2.112xsmall moleculeantagonistNAinactiveNABRIL-IL3X-RAYTBD2016Segala et al. 2016
160Rhodopsinbeta2 adrenergic receptorHuman5JQH3.2Carazololsmall moleculeinverse agonistNAinactiveNAT4-IL3X-RAYTBD2016Staus et al. 2016
161Rhodopsinbeta2 adrenergic receptorHuman3SN63.2BI-167107small moleculeagonistNAactivatedGs heterotrimerT4L-NTX-RAYp2011Rasmussen et al. 2011b
162RhodopsinM2 muscarinic receptorHuman3UON3.03-quinuclidinyl-benzilatesmall moleculeantagonistNAinactiveNAT4L-IL3X-RAYNA2012Haga et al. 2012
163GlutamatemGlu5 receptorHuman4OO92.6Mavoglurantsmall moleculeantagonistnegative allosteric modulatorinactiveNAT4L-IL2X-RAYc2014Dore et al. 2014
164GlutamatemGlu1 receptorHuman4OR22.8FITMsmall moleculeantagonistnegative allosteric modulatorinactiveNABRIL-NTX-RAYNA2014Wu et al. 2014
165GlutamatemGlu5 receptorHuman5CGC3.1Comp. 14small moleculeantagonistnegative allosteric modulatorinactiveNANAX-RAYc2015Christopher et al. 2015
166GlutamatemGlu5 receptorHuman5CGD2.6Comp. 25small moleculeantagonistnegative allosteric modulatorinactiveNANAX-RAYc2015Christopher et al. 2015
167RhodopsinETB endothelin receptorHuman5GLH2.8endothelin-1peptideagonistNAactiveNAT4L-IL3X-RAYNA2016Shihoya et al. 2016
168RhodopsinETB endothelin receptorHuman5GLI2.5unligandedunligandedunligandedNAinactiveNAT4L-IL3X-RAYNA2016Shihoya et al. 2016
169RhodopsinA2A adenosine receptorHuman5K2A2.5ZM-241385small moleculeantagonistNAinactiveNABRIL-IL3X-RAYTBD2016Batyuk et al. 2016
170RhodopsinA2A adenosine receptorHuman5K2B2.5ZM-241385small moleculeantagonistNAinactiveNABRIL-IL3X-RAYTBD2016Batyuk et al. 2016
171RhodopsinA2A adenosine receptorHuman5K2C1.9ZM-241385small moleculeantagonistNAinactiveNABRIL-IL3X-RAYTBD2016Batyuk et al. 2016
172RhodopsinA2A adenosine receptorHuman5K2D1.9ZM-241385small moleculeantagonistNAinactiveNABRIL-IL3X-RAYTBD2016Batyuk et al. 2016
173RhodopsinCB1 cannabinoid receptorHuman5TGZ2.8AM6538small moleculeantagonistNAinactiveNAFlavodoxin-IL3X-RAYNA2016Hua et al. 2016
174FrizzledSmoothenedHuman5V562.9TBDTBDTBDTBDinactiveTBDTBDX-RAYTBD2017Zhang et al. 2017
175FrizzledSmoothenedHuman5V573.0TBDTBDTBDTBDinactiveTBDTBDX-RAYTBD2017Zhang et al. 2017
176SecretinGLP1 glucagon-like peptide receptorHuman5VEW2.7TBDTBDTBDTBDinactiveTBDTBDX-RAYNA2017Song et al. 2017
177SecretinGLP1 glucagon-like peptide receptorHuman5VEX3.0TBDTBDTBDTBDinactiveTBDTBDX-RAYNA2017Song et al. 2017
178SecretinGlucagon receptorHuman5XEZ3.0TBDTBDTBDTBDinactiveTBDTBDX-RAYNA2017Zhang et al. 2017
179SecretinGlucagon receptorHuman5XF13.19TBDTBDTBDTBDinactiveTBDTBDX-RAYNA2017Zhang et al. 2017
180RhodopsinCCR9 chemokine receptorHuman5LWE2.8Vercirnonsmall moleculeallosteric antagonistallostericinactiveNANAX-RAYTBD2016Oswald et al. 2016
181RhodopsinPAR2 proteinase-activated receptorHuman5NDD2.8AZ8838small moleculeantagonistNAinactiveNABRIL-IL3X-RAYTBD2017Cheng et al. 2017
182RhodopsinPAR2 proteinase-activated receptorHuman5NDZ3.6AZ3451small moleculeantagonistallostericinactiveNABRIL-IL3X-RAYTBD2017Cheng et al. 2017
183RhodopsinPAR2 proteinase-activated receptorHuman5NJ64.0AZ7188small moleculeantagonistNAinactiveNABRIL-IL3X-RAYa o2017Cheng et al. 2017
184RhodopsinNTS1 neurotensin receptorRat5T043.3Neurotensin (8-13)peptideagonistNAactivated (partially)NAT4L-IL3X-RAYc2016Krumm et al. 2016
185RhodopsinCCR2 chemokine receptorHuman5T1A2.81BMS-681 + CCR2-RA-[R]small moleculeantagonist + allosteric antagonistthe allosteric antagonist CCR2-RA-[R] binds at the intracellular opening of the helical bundleinactiveNAT4L-IL3X-RAYNA2016Zheng et al. 2016
186RhodopsinRhodopsinBovine5TE32.7unligandedunligandedunligandedNAactivated opsinNANAX-RAYNA2017Gulati et al. 2017
187RhodopsinRhodopsinBovine5TE54.016mrsix-carbon ring retinal chromophoreinverse agonistNAinactiveNANAX-RAYNA2017Gulati et al. 2017
188Rhodopsin5-HT2B serotonin receptorHuman5TVN2.9LSDsmall moleculeagonistbiased agonist (beta-arrestin)inactive or minimally activatedNABRIL-IL3X-RAYNA2017Wacker et al. 2017
189RhodopsinCB1 cannabinoid receptorHuman5U092.6Taranabantsmall moleculeinverse agonistNAinactiveNAPGS-IL3X-RAYNA2016Shao et al. 2016
190RhodopsinA1 adenosine receptorHuman5UEN3.2DU172small moleculeantagonistNAinactiveNABRIL-IL3X-RAYNA2017Glukhova et al. 2017
191RhodopsinA2A adenosine receptorHuman5UIG3.5Comp. 1small moleculeantagonistdual antagonist - second target: NR2BinactiveNABRIL-IL3X-RAYNA2017Sun et al. 2017
192RhodopsinAT2R angiotensin II type 2 receptorHuman5UNF2.8Comp. 1small moleculeligandNAactive-likeNABRIL-NTX-RAYn2017Zhang et al. 2017
193RhodopsinAT2R angiotensin II type 2 receptorHuman5UNG2.8Comp. 1small moleculeligandNAactive-likeNABRIL-NTX-RAYn2017Zhang et al. 2017
194RhodopsinAT2R angiotensin II type 2 receptorHuman5UNH2.9Comp. 2small moleculeligandNAactive-likeNABRIL-NTX-RAYn2017Zhang et al. 2017
195RhodopsinA2A adenosine receptorHuman5UVI3.2TBDTBDTBDTBDinactiveTBDTBDX-RAYTBD2017Martin-Garcia et al. 2017
196RhodopsinA2A adenosine receptorHuman5JTB2.8ZM-241385small moleculeantagonistNAinactiveNATBDX-RAYTBD2017Melnikov et al. 2017
197RhodopsinFFA1 receptor (GPR40)Human5TZR2.2MK-8666small moleculeagonistpartial agonistinactive or minimally activatedNAT4L-IL3X-RAYNA2017Lu et al. 2017
198RhodopsinFFA1 receptor (GPR40)Human5TZY3.22MK-8666 + AP8small moleculeagonist + full allosteric agonistpartial agonist + full allosteric agonist (AgoPAM) bound to a second pocketinactive or minimally activatedNAT4L-IL3X-RAYNA2017Lu et al. 2017
199SecretinGLP1 glucagon-like peptide receptorHuman5NX23.7TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2017Rappas et al. 2017
200RhodopsinFFA1 receptor (GPR40)Human5KW22.76TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Ho et al. 2018
201RhodopsinA2A adenosine receptorHuman5MZJ2.0TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2017Cheng et al. 2017
202RhodopsinA2A adenosine receptorHuman5MZP2.1TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2017Cheng et al. 2017
203RhodopsinA2A adenosine receptorHuman5N2R2.8TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2017Cheng et al. 2017
204RhodopsinA1 adenosine receptorHuman5N2S3.3TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2017Cheng et al. 2017
205RhodopsinA2A adenosine receptorHuman5NLX2.14TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2017Weinert et al. 2017
206RhodopsinA2A adenosine receptorHuman5NM21.95TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2017Weinert et al. 2017
207RhodopsinA2A adenosine receptorHuman5NM41.7TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2017Weinert et al. 2017
208RhodopsinC5a1 complement peptide receptorHuman5O9H2.7TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Robertson et al. 2018
209RhodopsinA2A adenosine receptorHuman5OLG1.87TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Rucktooa et al. 2018
210RhodopsinA2A adenosine receptorHuman5OLH2.6TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Rucktooa et al. 2018
211RhodopsinA2A adenosine receptorHuman5OLO3.1TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Rucktooa et al. 2018
212RhodopsinA2A adenosine receptorHuman5OLV2.0TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Rucktooa et al. 2018
213RhodopsinA2A adenosine receptorHuman5OLZ1.9TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Rucktooa et al. 2018
214RhodopsinA2A adenosine receptorHuman5OM12.1TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Rucktooa et al. 2018
215RhodopsinA2A adenosine receptorHuman5OM42.0TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Rucktooa et al. 2018
216Rhodopsin5-HT2B serotonin receptorHuman5TUD3.0TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2017Ishchenko et al. 2017
217RhodopsinCCR5 chemokine receptorHuman5UIW2.2TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2017Zheng et al. 2017
218Rhodopsin5-HT1B serotonin receptorHuman5V543.9TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Yin et al. 2018
219RhodopsinRhodopsinHuman5W0P3.01TBDTBDTBDTBDTBDVisual arrestinTBDX-RAYTBD2017Zhou et al. 2017
220RhodopsinD4 dopamine receptorHuman5WF62.9TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018White et al. 2018
221RhodopsinD4 dopamine receptorHuman5WIU1.96TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2017Wacker et al. 2017
222RhodopsinD4 dopamine receptorHuman5WIV2.14TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2017Wacker et al. 2017
223RhodopsinRhodopsinBovine5WKT3.2TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2017Broecker et al. 2017
224RhodopsinOX2 orexin receptorHuman5WQC1.96TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2017Suno et al. 2017
225RhodopsinOX2 orexin receptorHuman5WS32.3TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2017Suno et al. 2017
226Rhodopsinbeta2 adrenergic receptorHuman5X7D2.7TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2017Liu et al. 2017
227RhodopsinETB endothelin receptorHuman5X932.2TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2017Shihoya et al. 2017
228RhodopsinETB endothelin receptorHuman5XPR3.6TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2017Shihoya et al. 2017
229RhodopsinCB1 cannabinoid receptorHuman5XR82.95TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2017Hua et al. 2017
230RhodopsinCB1 cannabinoid receptorHuman5XRA2.8TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2017Hua et al. 2017
231RhodopsinLPA6 receptor Zebrafish5XSZ3.2TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2017Taniguchi et al. 2017
232RhodopsinY1 neuropeptide receptorHuman5ZBH3.0TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Yang et al. 2018
233RhodopsinY1 neuropeptide receptorHuman5ZBQ2.7TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Yang et al. 2018
234RhodopsinA2A adenosine receptorHuman6AQF2.51TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Eddy et al. 2018
235Rhodopsinkappa opioid receptorHuman6B733.1TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Che et al. 2018
236Rhodopsin5-HT2C serotonin receptorHuman6BQG3.0TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Peng et al. 2018
237Rhodopsin5-HT2C serotonin receptorHuman6BQH2.7TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Peng et al. 2018
238RhodopsinD2 dopamine receptorHuman6CM42.87TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Wang et al. 2018
239RhodopsinRhodopsinBovine6FK62.36TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Mattle et al. 2018
240RhodopsinRhodopsinBovine6FK72.62TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Mattle et al. 2018
241RhodopsinRhodopsinBovine6FK82.87TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Mattle et al. 2018
242RhodopsinRhodopsinBovine6FK92.63TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Mattle et al. 2018
243RhodopsinRhodopsinBovine6FKA2.7TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Mattle et al. 2018
244RhodopsinRhodopsinBovine6FKB3.03TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Mattle et al. 2018
245RhodopsinRhodopsinBovine6FKC2.46TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Mattle et al. 2018
246RhodopsinRhodopsinBovine6FKD2.49TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Mattle et al. 2018
247GlutamatemGlu5 receptorHuman6FFH2.65TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Christopher et al. 2018
248GlutamatemGlu5 receptorHuman6FFI2.2TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Christopher et al. 2018
249FrizzledSmoothenedXenopus6D323.75TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Huang et al. 2018
250FrizzledSmoothenedXenopus6D353.9TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Huang et al. 2018
251RhodopsinViral US28 receptorVirus5WB23.5TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Jude et al. 2018
252RhodopsinA2A adenosine receptorHuman5WF52.6TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018White et al. 2018
253RhodopsinAT2R angiotensin II type 2 receptorHuman5XJM3.2TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Asada et al. 2018
254FrizzledFZD4 frizzled receptorHuman6BD42.4TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Yang et al. 2018
255Rhodopsin5-HT2B serotonin receptorHuman6DRX3.1TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018McCorvy et al. 2018
256Rhodopsin5-HT2B serotonin receptorHuman6DRY2.92TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018McCorvy et al. 2018
257Rhodopsin5-HT2B serotonin receptorHuman6DRZ3.1TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018McCorvy et al. 2018
258Rhodopsin5-HT2B serotonin receptorHuman6DS03.19TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018McCorvy et al. 2018
259RhodopsinRhodopsinBovine6FUF3.12TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Tsai et al. 2018
260SecretinPTH1 parathyroid hormone receptorHuman6FJ32.5TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Ehrenmann et al. 2018
261RhodopsinM2 muscarinic receptorHuman5YC82.5TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Suno et al. 2018
262RhodopsinM3 muscarinic receptorRat5ZHP3.1TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Liu et al. 2018
263RhodopsinM2 muscarinic receptorHuman5ZK32.6TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Suno et al. 2018
264RhodopsinM2 muscarinic receptorHuman5ZK83.0TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Suno et al. 2018
265RhodopsinM2 muscarinic receptorHuman5ZKB2.95TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Suno et al. 2018
266RhodopsinM2 muscarinic receptorHuman5ZKC2.3TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Suno et al. 2018
267RhodopsinCB2 cannabinoid receptorHuman5ZTY2.8TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2019Li et al. 2019
268Rhodopsin5-HT2A serotonin receptorHuman6A933.0TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2019Kimura et al. 2019
269Rhodopsin5-HT2A serotonin receptorHuman6A942.9TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2019Kimura et al. 2019
270RhodopsinCCR5 chemokine receptorHuman6AKX2.8TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Zhu et al. 2018
271RhodopsinCCR5 chemokine receptorHuman6AKY2.8TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Zhu et al. 2018
272RhodopsinAT1R angiotensin II type 1 receptorHuman6DO12.9TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2019Wingler et al. 2019
273RhodopsinNK1 tachykinin receptor (substance-P receptor)Human6E593.4TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Yin et al. 2018
274RhodopsinCCR2 chemokine receptorHuman6GPS3.3TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2019Pautsch et al. 2019
275RhodopsinCCR2 chemokine receptorHuman6GPX2.7TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2019Pautsch et al. 2019
276RhodopsinNK1 tachykinin receptor (substance-P receptor)Human6HLO2.4TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2019Schoppe et al. 2019
277RhodopsinNK1 tachykinin receptor (substance-P receptor)Human6HLP2.2TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2019Schoppe et al. 2019
278Rhodopsinbeta1 adrenergic receptorTurkey6IBL2.7TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2019Warne et al. 2019
279RhodopsinETB endothelin receptorHuman6IGK2.0TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Shihoya et al. 2018
280RhodopsinETB endothelin receptorHuman6IGL2.7TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Shihoya et al. 2018
281RhodopsinNK1 tachykinin receptor (substance-P receptor)Human6J202.7TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2019Chen et al. 2019
282RhodopsinNK1 tachykinin receptor (substance-P receptor)Human6J213.2TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2019Chen et al. 2019
283RhodopsinMLT1A melatonin receptorHuman6ME22.8TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2019Stauch et al. 2019
284RhodopsinMLT1A melatonin receptorHuman6ME32.9TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2019Stauch et al. 2019
285RhodopsinMLT1A melatonin receptorHuman6ME43.2TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2019Stauch et al. 2019
286RhodopsinMLT1A melatonin receptorHuman6ME53.2TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2019Stauch et al. 2019
287RhodopsinMLT1B melatonin receptorHuman6ME62.8TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2019Johansson et al. 2019
288RhodopsinMLT1B melatonin receptorHuman6ME73.2TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2019Johansson et al. 2019
289RhodopsinMLT1B melatonin receptorHuman6ME83.1TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2019Johansson et al. 2019
290RhodopsinMLT1B melatonin receptorHuman6ME93.3TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2019Johansson et al. 2019
291RhodopsinA2A adenosine receptorHuman6MH84.2TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2019Martin-Garcia et al. 2019
292Rhodopsinbeta2 adrenergic receptorHuman6MXT2.96TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Masureel et al. 2018
293GlutamatemGlu5 receptorHuman6N4X4.0TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2019Koehl et al. 2019
294RhodopsinViral US28 receptorVirus5WB13.51TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Jude et al. 2018
295RhodopsinBLT1 leukotriene B4 receptorNA5X333.7TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Hori et al. 2018
296RhodopsinEP3 prostanoid receptor (prostaglandin E receptor 3)Human6AK32.9TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Morimoto et al. 2018
297RhodopsinDP2 prostanoid receptor (prostaglandin D2 receptor 2)Human6D262.8TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Wang et al. 2018
298RhodopsinDP2 prostanoid receptor (prostaglandin D2 receptor 2)Human6D272.74TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Wang et al. 2018
299RhodopsinTP prostanoid receptor (thromboxane A2 receptor)Human6IIU2.5TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Fan et al. 2018
300RhodopsinTP prostanoid receptor (thromboxane A2 receptor)Human6IIV3.0TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Fan et al. 2018
304RhodopsinPAF receptorHuman5ZKQ2.9TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Cao et al. 2018
305RhodopsinPAF receptorHuman5ZKP2.81TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Cao et al. 2018
314RhodopsinEP4 prostanoid receptor (prostaglandin E receptor 4)Human5YHL4.2TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Toyoda et al. 2018
315RhodopsinEP4 prostanoid receptor (prostaglandin E receptor 4)Human5YWY3.2TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Toyoda et al. 2018
316RhodopsinEP3 prostanoid receptor (prostaglandin E receptor 3)Human6M9T2.5TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2018Audet et al. 2018
322RhodopsinRhodopsinBovine1JFP0.0TBDTBDTBDTBDTBDTBDTBDNMRTBD2001Yeagle et al. 2001
323RhodopsinRhodopsinBovine1LN60.0TBDTBDTBDTBDTBDTBDTBDNMRTBD2002Choi et al. 2002
327RhodopsinNK1 tachykinin receptor (substance-P receptor)Human2KS90.0TBDTBDTBDTBDTBDTBDTBDNMRTBD2010Gayen et al. 2010
328RhodopsinNK1 tachykinin receptor (substance-P receptor)Human2KSA0.0TBDTBDTBDTBDTBDTBDTBDNMRTBD2010Gayen et al. 2010
329RhodopsinNK1 tachykinin receptor (substance-P receptor)Human2KSB0.0TBDTBDTBDTBDTBDTBDTBDNMRTBD2010Gayen et al. 2010
330RhodopsinCXCR1 chemokine receptorHuman2LNL0.0TBDTBDTBDTBDTBDTBDTBDNMRTBD2012Park et al. 2012
331RhodopsinRhodopsinHuman6CMO4.5TBDTBDTBDTBDActivatedGiTBDElectron MicroscopyTBD2018Kang et al. 2018
334RhodopsinApelin receptorHuman5VBL2.6TBDTBDTBDTBDTBDTBDTBDX-RAYTBD2017Ma et al. 2017
335RhodopsinA2A adenosine receptorHuman5VRA2.35TBDTBDTBDTBDTBDTBDcytochrome b562X-RAYTBD2017Broecker et al. 2017
336RhodopsinA1 adenosine receptorHuman6D9H3.6Adenosinesmall moleculeagonistNAActivatedGiTBDElectron MicroscopyTBD2018Draper-Joyce et al. 2018
337Rhodopsinmu opioid receptorHuman6DDE3.5DAMGOpeptideagonistNAActivatedGiTBDElectron MicroscopyTBD2018Koehl et al. 2018
338Rhodopsinmu opioid receptorHuman6DDF3.5DAMGOpeptideagonistNAActivatedGiTBDElectron MicroscopyTBD2018Koehl et al. 2018
339Rhodopsin5-HT1B serotonin receptorHuman6G793.78Donitriptansmall moleculeagonistNAActivatedGoTBDElectron MicroscopyTBD2018Garcia-Nafria et al. 2018
340RhodopsinA2A adenosine receptorHuman6GDG4.11NECAsmall moleculeagonistNAActivatedMini GsTBDElectron MicroscopyTBD2018Garcia-Nafria et al. 2018
341Rhodopsinbeta1 adrenergic receptorTurkey6H7J2.8Isoprenalinesmall moleculeagonistNAActivatedNATBDX-RAYp2018Warne et al. 2018
342Rhodopsinbeta1 adrenergic receptorTurkey6H7L2.7Dobutaminesmall moleculeagonistNAActivatedNATBDX-RAYp2018Warne et al. 2018
343Rhodopsinbeta1 adrenergic receptorTurkey6H7M2.76Salbutamolsmall moleculeagonistNAActivatedNATBDX-RAYp2018Warne et al. 2018
344Rhodopsinbeta1 adrenergic receptorTurkey6H7N2.5Xamoterolsmall moleculeagonistNAActivatedNATBDX-RAYp2018Warne et al. 2018
345Rhodopsinbeta1 adrenergic receptorTurkey6H7O2.8Cyanopindololsmall moleculeagonistNAActivatedNATBDX-RAYTBD2018Warne et al. 2018
346RhodopsinNK1 tachykinin receptor (substance-P receptor)Human6HLL3.27CP-99,994small moleculeantagonistNAInactiveNATBDX-RAYTBD2019Schoppe et al. 2019
347RhodopsinCCR5 chemokine receptorHuman6MEO3.9T-cell surface glycoprotein CD4proteinTBDTBDTBDTBDTBDElectron MicroscopyTBD2018Shaik et al. 2018
348RhodopsinCCR5 chemokine receptorHuman6MET4.5T-cell surface glycoprotein CD4proteinTBDTBDTBDTBDTBDElectron MicroscopyTBD2018Shaik et al. 2018
349RhodopsinCB1 cannabinoid receptorHuman6N4B3.0FUBsmall moleculeagonistNAActivatedGiTBDElectron MicroscopyTBD2019Krishna Kumar et al. 2019
350RhodopsinM1 muscarinic receptorHuman6OIJ3.3Iperoxosmall moleculeagonistNAActivatedG11TBDElectron MicroscopyTBD2019Maeda et al. 2019
351RhodopsinM2 muscarinic receptorHuman6OIK3.6Iperoxosmall moleculeagonistNAActivatedGoTBDElectron MicroscopyTBD2019Maeda et al. 2019
352GlutamatemGlu5 receptorHuman6N514.0Quisqualatesmall moleculeagonistNAActivatedNATBDElectron Microscopyb p2019Koehl et al. 2019
353GlutamatemGlu5 receptorHuman6N524.0UnligandedNANANAInactiveNATBDElectron Microscopyb2019Koehl et al. 2019
354SecretinCalcitonin receptorHuman6NIY3.34TBDTBDTBDNAActivatedGsTBDElectron MicroscopyTBD2019Dal Maso et al. 2019
355SecretinCalcitonin receptorHuman5UZ74.1TBDTBDTBDNAActivatedGsTBDElectron MicroscopyTBD2019Liang et al. 2017
356SecretinCalcitonin receptorHuman6E3Y3.34TBDTBDTBDNAActivatedGsTBDElectron MicroscopyTBD2019Liang et al. 2018
357SecretinGLP1 glucagon-like peptide receptorRabbit5VAI4.1GLP-1peptideagonistNAActivatedGsTBDElectron MicroscopyTBD2017Zhang et al. 2017
358SecretinGLP1 glucagon-like peptide receptorHuman6B3J3.3Exendin-P5peptideagonistbiased agonist (G protein-biased)ActivatedGsTBDElectron Microscopyp2018Liang et al. 2018
359SecretinPTH1 parathyroid hormone receptorRat6NBF3.0LA-PTHpeptideagonistTBDActivatedGsTBDElectron Microscopyp2019Zhao et al. 2019
360SecretinPTH1 parathyroid hormone receptorRat6NBH3.5LA-PTHpeptideagonistTBDActivatedGsTBDElectron Microscopyp2019Zhao et al. 2019
361SecretinPTH1 parathyroid hormone receptorRat6NBI4.0LA-PTHpeptideagonistTBDActivatedGsTBDElectron Microscopyp2019Zhao et al. 2019
Visualized fields:
Column number Family Receptor Organism PDB ID Resolution Ligand Ligand chemical class Ligand type
More on ligand type Putative State Signaling partner Fusion protein Method Notes Year References


Notes
a Ligand not visible.
b Potentially biologically relevant dimer observed in the structure
c Thermally stable mutant receptor.
d Alternative model of 1GZM.
e Alternative model of 2J4Y.
f Showing an intact salt bridge linking the cytoplasmic ends of helices 3 and 6.
g Constitutively active mutant.
h Fab prevents agonist binding.
k Processed with a microdiffraction data assembly method.
i Intact IL3.
j Serial femtosecond crystallography.
l 5F8U is a re-analysis of 4GPO showing ligand occupancy.
m Synchrotron data structure for 4ZWJ.
n The ligands stabilize an active-like state, but with a conformation of Helix VIII that prevents binding of G proteins or arrestins.
o Solved with antibody FAB.
p Solved with nanobody.

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