Table

The Costanzi Research Group

Experimentally solved GPCR structures
(Updated November 8, 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 Method Year References
1FrizzledSmoothenedHuman4JKV2.45LY2940680small moleculeantagonistNAinactiveNAX-RAY2013Wang et al. 2013
2FrizzledSmoothenedHuman4N4W2.8SANT-1small moleculeantagonistNAinactiveNAX-RAY2014Wang et al. 2014
3FrizzledSmoothenedHuman4O9R3.2Cyclopaminesmall moleculeantagonistNAinactiveNAX-RAY2014Weierstall et al. 2014
4FrizzledSmoothenedHuman4QIM2.61ANTA XVsmall moleculeantagonistNAinactiveNAX-RAY2014Wang et al. 2014
5FrizzledSmoothenedHuman4QIN2.6SAG1.5small moleculeagonistNAinactive or minimally activatedNAX-RAY2014Wang et al. 2014
6FrizzledSmoothenedHuman5L7D3.2Cholesterolsmall moleculeallosteric ligandbound to extracellular cysteine-rich domain (CRO) inactiveNAX-RAY2016Byrne et al. 2016
7FrizzledSmoothenedHuman5L7I3.3Vismodegibsmall moleculeantagonistNAinactiveNAX-RAY2016Byrne et al. 2016
8SecretinCRF1 corticotropin-releasing factor receptorHuman4K5Y2.98CP-376395small moleculeantagonistnegative allosteric modulatorinactiveNAX-RAY2013Hollenstein et al. 2013
9SecretinGlucagon receptorHuman4L6R3.3unligandedunligandedunligandedNAinactiveNAX-RAY2013Siu et al. 2013
10SecretinCRF1 corticotropin-releasing factor receptorHuman4Z9G3.18CP-376395small moleculeantagonistallosteric antagonistinactiveNAX-RAY2016Dore et al. 2016
11SecretinGlucagon receptorHuman5EE72.5MK-0893small moleculeantagonistallosteric antagonistinactiveNAX-RAY2016Jazayeri et al. 2016
12RhodopsinRhodopsinBovine1F882.811-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NAX-RAY2000Palczewski et al. 2000
13RhodopsinRhodopsinBovine1GZM2.6511-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NAX-RAY2003Li et al. 2003
14RhodopsinRhodopsinBovine1HZX2.811-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NAX-RAY2001Teller et al. 2001
15RhodopsinRhodopsinBovine1L9H2.611-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NAX-RAY2002Okada et al. 2002
16RhodopsinRhodopsinBovine1U192.211-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NAX-RAY2004Okada et al. 2004
17RhodopsinRhodopsinBovine2G872.6all-trans-retinal (distorted)small moleculeagonistNAinactive or minimally activated (bathorhodopsin)NAX-RAY2006Nakamichi et al. 2006
18RhodopsinRhodopsinBovine2HPY2.8all-trans-retinalsmall moleculeagonistNAinactive or minimally activated (lumirhodopsin)NAX-RAY2006Nakamichi et al. 2006
19RhodopsinRhodopsinBovine2I353.811-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NAX-RAY2006Salom et al. 2006
20RhodopsinRhodopsinBovine2I364.111-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NAX-RAY2006Salom et al. 2006
21RhodopsinRhodopsinBovine2I374.15all-trans-retinalsmall moleculeagonistNAinactive or minimally activated (early photoactivation intermediate)NAX-RAY2006Salom et al. 2006
22RhodopsinRhodopsinBovine2J4Y3.411-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NAX-RAY2007Standfuss et al. 2007
23RhodopsinRhodopsinBovine2PED2.959-cis-retinalsmall moleculeinverse agonistNAinactive (isorhodopsin)NAX-RAY2007Nakamichi et al. 2007
24Rhodopsinbeta2 adrenergic receptorHuman2R4R3.4carazololsmall moleculeinverse agonistNAinactiveNAX-RAY2007Rasmussen et al. 2007
25Rhodopsinbeta2 adrenergic receptorHuman2R4S3.4carazololsmall moleculeinverse agonistNAinactiveNAX-RAY2007Rasmussen et al. 2007
26Rhodopsinbeta2 adrenergic receptorHuman2RH12.4carazololsmall moleculeinverse agonistNAinactiveNAX-RAY2007Cherezov et al. 2007
27Rhodopsinbeta1 adrenergic receptorTurkey2VT42.7cyanopindololsmall moleculeantagonistNAinactiveNAX-RAY2008Warne et al. 2008
28RhodopsinRhodopsinBovine2X723.0all-trans-retinalsmall moleculeagonistNAactivated (metarhodopsin II)NAX-RAY2011Standfuss et al. 2011
29Rhodopsinbeta1 adrenergic receptorTurkey2Y002.5dobutaminesmall moleculepartial agonistNAinactive or minimally activatedNAX-RAY2011Warne et al. 2011
30Rhodopsinbeta1 adrenergic receptorTurkey2Y012.6dobutaminesmall moleculepartial agonistNAinactive or minimally activatedNAX-RAY2011Warne et al. 2011
31Rhodopsinbeta1 adrenergic receptorTurkey2Y022.6carmoterolsmall moleculeagonistNAinactive or minimally activatedNAX-RAY2011Warne et al. 2011
32Rhodopsinbeta1 adrenergic receptorTurkey2Y032.85isoprenalinesmall moleculeagonistNAinactive or minimally activatedNAX-RAY2011Warne et al. 2011
33Rhodopsinbeta1 adrenergic receptorTurkey2Y043.05salbutamolsmall moleculepartial agonistNAinactive or minimally activatedNAX-RAY2011Warne et al. 2011
34Rhodopsinbeta1 adrenergic receptorTurkey2YCW3.0carazololsmall moleculeantagonistNAinactiveNAX-RAY2011Moukhametzianov et al. 2011
35Rhodopsinbeta1 adrenergic receptorTurkey2YCX3.25cyanopindololsmall moleculeantagonistNAinactiveNAX-RAY2011Moukhametzianov et al. 2011
36Rhodopsinbeta1 adrenergic receptorTurkey2YCY3.15cyanopindololsmall moleculeantagonistNAinactiveNAX-RAY2011Moukhametzianov et al. 2011
37Rhodopsinbeta1 adrenergic receptorTurkey2YCZ3.65iodocyanopindololsmall moleculeantagonistNAinactiveNAX-RAY2011Moukhametzianov et al. 2011
38RhodopsinA2A adenosine receptorHuman2YDO3.0adenosinesmall moleculeagonistNAinactive or minimally activatedNAX-RAY2011Lebon et al. 2011
39RhodopsinA2A adenosine receptorHuman2YDV2.6NECAsmall moleculeagonistNAinactive or minimally activatedNAX-RAY2011Lebon et al. 2011
40RhodopsinRhodopsinSquid2Z732.511-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NAX-RAY2008Murakami et al. 2008
41RhodopsinRhodopsinSquid2ZIY3.711-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NAX-RAY2008Shimamura et al. 2008
42RhodopsinRhodopsinSquid3AYM2.8all-trans-retinalsmall moleculeagonistNAinactive or minimally activated (bathorhodopsin)NAX-RAY2011Murakami et al. 2011
43RhodopsinRhodopsinSquid3AYN2.79-cis-retinalsmall moleculeinverse agonistNAinactive (isorhodopsin)NAX-RAY2011Murakami et al. 2011
44RhodopsinRhodopsinBovine3C9L2.6511-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NAX-RAY2008Stenkamp et al. 2008
45RhodopsinRhodopsinBovine3C9M3.411-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NAX-RAY2008Stenkamp et al. 2008
46RhodopsinRhodopsinBovine3CAP2.9unligandedunligandedunligandedNAactivated opsinNAX-RAY2008Park et al. 2008
47Rhodopsinbeta2 adrenergic receptorHuman3D4S2.8timololsmall moleculeinverse agonistNAinactiveNAX-RAY2008Hanson et al. 2008
48RhodopsinRhodopsinBovine3DQB3.2unligandedunligandedunligandedNAactivated opsinNAX-RAY2008Scheerer et al. 2008
49RhodopsinA2A adenosine receptorHuman3EML2.6ZM-241385small moleculeantagonistNAinactiveNAX-RAY2008Jaakola et al. 2008
50Rhodopsinbeta2 adrenergic receptorHuman3KJ63.4carazololsmall moleculeinverse agonistNAinactiveNAX-RAY2010Bokoch et al. 2010
51Rhodopsinbeta2 adrenergic receptorHuman3NY82.84ICI 118551small moleculeinverse agonistNAinactiveNAX-RAY2010Wacker et al. 2010
52Rhodopsinbeta2 adrenergic receptorHuman3NY92.84recent comp.small moleculeinverse agonistNAinactiveNAX-RAY2010Wacker et al. 2010
53Rhodopsinbeta2 adrenergic receptorHuman3NYA3.16alprenololsmall moleculeantagonistNAinactiveNAX-RAY2010Wacker et al. 2010
54RhodopsinRhodopsinBovine3OAX2.611-cis-retinalsmall moleculeinverse agonistNAinactive (ground state)NAX-RAY2011Makino et al. 2011
55RhodopsinCXCR4 chemokine receptorHuman3ODU2.5IT1tsmall moleculeantagonistNAinactiveNAX-RAY2010Wu et al. 2010
56RhodopsinCXCR4 chemokine receptorHuman3OE02.9CVX15peptideantagonistNAinactiveNAX-RAY2010Wu et al. 2010
57RhodopsinCXCR4 chemokine receptorHuman3OE63.2IT1tsmall moleculeantagonistNAinactiveNAX-RAY2010Wu et al. 2010
58RhodopsinCXCR4 chemokine receptorHuman3OE83.1IT1tsmall moleculeantagonistNAinactiveNAX-RAY2010Wu et al. 2010
59RhodopsinCXCR4 chemokine receptorHuman3OE93.1IT1tsmall moleculeantagonistNAinactiveNAX-RAY2010Wu et al. 2010
60Rhodopsinbeta2 adrenergic receptorHuman3P0G3.5BI-167107small moleculeagonistNAactivatedNAX-RAY2011Rasmussen et al. 2011
61RhodopsinD3 dopamine receptorHuman3PBL2.89Eticlopridesmall moleculeantagonistNAinactiveNAX-RAY2010Chien et al. 2010
62Rhodopsinbeta2 adrenergic receptorHuman3PDS3.5FAUC50small moleculeagonistirreversibleinactive or minimally activatedNAX-RAY2011Rosenbaum et al. 2011
63RhodopsinRhodopsinBovine3PQR2.85all-trans-retinalsmall moleculeagonistNAactivated (metarhodopsin II)NAX-RAY2011Choe et al. 2011
64RhodopsinA2A adenosine receptorHuman3PWH3.3ZM-241385small moleculeantagonistNAinactiveNAX-RAY2011Dore et al. 2011
65RhodopsinRhodopsinBovine3PXO3.0all-trans-retinalsmall moleculeagonistNAactivated (metarhodopsin II)NAX-RAY2011Choe et al. 2011
66RhodopsinA2A adenosine receptorHuman3QAK2.71UK-432097small moleculeagonistNAinactive or minimally activatedNAX-RAY2011Xu et al. 2011
67RhodopsinA2A adenosine receptorHuman3REY3.31XACsmall moleculeantagonistNAinactiveNAX-RAY2011Dore et al. 2011
68RhodopsinA2A adenosine receptorHuman3RFM3.6caffeinesmall moleculeantagonistNAinactiveNAX-RAY2011Dore et al. 2011
69RhodopsinH1 histamine receptorHuman3RZE3.1Doxepinsmall moleculeantagonistNAinactiveNAX-RAY2011Shimamura et al. 2011
70RhodopsinA2A adenosine receptorHuman3UZA3.271 2 4-triazine 4gsmall moleculeantagonistNAinactiveNAX-RAY2012Congreve et al. 2012
71RhodopsinA2A adenosine receptorHuman3UZC3.341 2 4-triazine 4gsmall moleculeantagonistNAinactiveNAX-RAY2012Congreve et al. 2012
72RhodopsinS1P1 sphingosine 1-phosphate receptorHuman3V2W3.35ML056small moleculeantagonistNAinactiveNAX-RAY2012Hanson et al. 2012
73RhodopsinS1P1 sphingosine 1-phosphate receptorHuman3V2Y2.8ML056small moleculeantagonistNAinactiveNAX-RAY2012Hanson et al. 2012
74RhodopsinA2A adenosine receptorHuman3VG92.7ZM-241385small moleculeantagonistNAinactiveNAX-RAY2012Hino et al. 2012
75RhodopsinA2A adenosine receptorHuman3VGA3.1ZM-241385small moleculeantagonistNAinactiveNAX-RAY2012Hino et al. 2012
76RhodopsinPAR1 proteinase-activated receptorHuman3VW72.2Vorapaxarsmall moleculeantagonistNAinactiveNAX-RAY2012Zhang et al. 2012
77RhodopsinNTS1 neurotensin receptorRat3ZEV3.0Neurotensin (8-13)peptideagonistNAinactive or minimally activatedNAX-RAY2014Egloff et al. 2014
78Rhodopsinbeta1 adrenergic receptorTurkey3ZPQ2.84-(piperazin-1-yl)-1H-indolesmall moleculeantagonistNAinactiveNAX-RAY2013Christopher et al. 2013
79Rhodopsinbeta1 adrenergic receptorTurkey3ZPR2.74-methyl-2-(piperazin-1-yl)quinolinesmall moleculeantagonistNAinactiveNAX-RAY2013Christopher et al. 2013
80RhodopsinRhodopsinBovine4A4M3.3all-trans-retinalsmall moleculeagonistNAactivated (metarhodopsin II)NAX-RAY2012Deupi et al. 2012
81Rhodopsinbeta1 adrenergic receptorTurkey4AMI3.2bucindololsmall moleculeagonistbiased agonist (beta-arrestin)inactive or minimally activatedNAX-RAY2012Warne et al. 2012
82Rhodopsinbeta1 adrenergic receptorTurkey4AMJ2.3carvedilolsmall moleculeagonistbiased agonist (beta-arrestin)inactive or minimally activatedNAX-RAY2012Warne et al. 2012
83RhodopsinRhodopsinBovine4BEY2.9unligandedunligandedunligandedNAactivated opsinNAX-RAY2013Singhal et al. 2013
84RhodopsinRhodopsinBovine4BEZ3.3unligandedunligandedunligandedNAactivated opsinNAX-RAY2013Singhal et al. 2013
85RhodopsinNTS1 neurotensin receptorRat4BUO2.75Neurotensin (8-13)peptideagonistNAinactive or minimally activatedNAX-RAY2014Egloff et al. 2014
86RhodopsinNTS1 neurotensin receptorRat4BV03.1Neurotensin (8-13)peptideagonistNAinactive or minimally activatedNAX-RAY2014Egloff et al. 2014
87Rhodopsinbeta1 adrenergic receptorTurkey4BVN2.1cyanopindololsmall moleculeantagonistNAinactiveNAX-RAY2014Miller-Gallacher et al. 2014
88RhodopsinNTS1 neurotensin receptorRat4BWB3.57Neurotensin (8-13)peptideagonistNAinactive or minimally activatedNAX-RAY2014Egloff et al. 2014
89RhodopsinM3 muscarinic receptorRat4DAJ3.4Tiotropiumsmall moleculeinverse agonistNAinactiveNAX-RAY2012Kruse et al. 2012
90Rhodopsinkappa opioid receptorHuman4DJH2.9JDTicsmall moleculeantagonistNAinactiveNAX-RAY2012Wu et al. 2012
91Rhodopsinmu opioid receptorMouse4DKL2.8funaltrexaminesmall moleculeantagonistirreversibleinactiveNAX-RAY2012Manglik et al. 2012
92RhodopsinNociception-orphanin FQ (NOP) receptorHuman4EA33.01Peptide mimetic c-24small moleculeantagonistNAinactiveNAX-RAY2012Thompson et al. 2012
93RhodopsinA2A adenosine receptorHuman4EIY1.8ZM-241385small moleculeantagonistNAinactiveNAX-RAY2012Liu et al. 2012
94Rhodopsindelta opioid receptorMouse4EJ43.4Naltrindolesmall moleculeantagonistNAinactiveNAX-RAY2012Granier et al. 2012
95Rhodopsinbeta2 adrenergic receptorHuman4GBR3.99carazololsmall moleculeinverse agonistNAinactiveNAX-RAY2012Zou et al. 2012
96Rhodopsinbeta1 adrenergic receptorTurkey4GPO3.5unligandedunligandedunligandedNAinactiveNAX-RAY2013Huang et al. 2013
97RhodopsinNTS1 neurotensin receptorRat4GRV2.8Neurotensin (8-13)peptideagonistNAactivated (partially)NAX-RAY2012White et al. 2012
98Rhodopsin5-HT1B serotonin receptorHuman4IAQ2.8Dihydroergotaminesmall moleculeagonistNAinactive or minimally activatedNAX-RAY2013Wang et al. 2013
99Rhodopsin5-HT1B serotonin receptorHuman4IAR2.7Ergotaminesmall moleculeagonistNAinactive or minimally activatedNAX-RAY2013Wang et al. 2013
100Rhodopsin5-HT2B serotonin receptorHuman4IB42.7Ergotaminesmall moleculeagonistbiased agonist (beta-arrestin)inactive or minimally activatedNAX-RAY2013Wacker et al. 2013
101RhodopsinRhodopsinBovine4J4Q2.65unligandedunligandedunligandedNAactivated opsinNAX-RAY2013Park et al. 2013
102Rhodopsinbeta2 adrenergic receptorHuman4LDE2.79BI-167107small moleculeagonistNAactivatedNAX-RAY2013Ring et al. 2013
103Rhodopsinbeta2 adrenergic receptorHuman4LDL3.1Hydroxybenzylisoproterenolsmall moleculeagonistNAactivatedNAX-RAY2013Ring et al. 2013
104Rhodopsinbeta2 adrenergic receptorHuman4LDO3.2Adrenalinesmall moleculeagonistNAactivatedNAX-RAY2013Ring et al. 2013
105RhodopsinCCR5 chemokine receptorHuman4MBS2.71Maravirocsmall moleculeinverse agonistNAinactiveNAX-RAY2013Tan et al. 2013
106RhodopsinM2 muscarinic receptorHuman4MQS3.5iperoxosmall moleculeagonistNAactivatedNAX-RAY2013Kruse et al. 2013
107RhodopsinM2 muscarinic receptorHuman4MQT3.7iperoxo + LY2119620small moleculeagonist + positive allosteric modulatorstructure includes positive allosteric modulator as a second ligandactivatedNAX-RAY2013Kruse et al. 2013
108Rhodopsindelta opioid receptorHuman4N6H1.8Naltrindolesmall moleculeantagonistNAinactiveNAX-RAY2013Fenalti et al. 2013
109Rhodopsin5-HT2B serotonin receptorHuman4NC32.8Ergotaminesmall moleculeagonistbiased agonist (beta-arrestin)inactive or minimally activatedNAX-RAY2013Liu et al. 2013
110RhodopsinP2Y12 receptorHuman4NTJ2.62AZD1283small moleculeantagonistNAinactiveNAX-RAY2014Zhang et al. 2014
111RhodopsinFFA1 receptor (GPR40)Human4PHU2.33TAK-875 or fasiglifamsmall moleculeantagonistNAinactiveNAX-RAY2014Srivastava et al. 2014
112RhodopsinRhodopsinBovine4PXF2.75unligandedunligandedunligandedNAactivated opsinNAX-RAY2014Szczepek et al. 2014
113RhodopsinP2Y12 receptorHuman4PXZ2.52-MeSADPsmall moleculeagonistNAinactive or minimally activatedNAX-RAY2014Zhang et al. 2014
114RhodopsinP2Y12 receptorHuman4PY03.12-MeSADPsmall moleculeagonistNAinactive or minimally activatedNAX-RAY2014Zhang et al. 2014
115Rhodopsinbeta2 adrenergic receptorHuman4QKX3.3Covalently-bound analog of noradrenalinesmall moleculeagonistirreversibleactivatedNAX-RAY2014Weichert et al. 2014
116Rhodopsindelta opioid receptorHuman4RWA3.28H-Dmt-Tic-Phe-Phe-NH2 (DIPP-NH2)peptideantagonistdual functioninactiveNAX-RAY2015Fenalti et al. 2015
117Rhodopsindelta opioid receptorHuman4RWD2.7H-Dmt-Tic-Phe-Phe-NH2 (DIPP-NH2)peptideantagonistdual functioninactiveNAX-RAY2015Fenalti et al. 2015
118RhodopsinCXCR4 chemokine receptorHuman4RWS3.1Viral chemokinepeptideantagonistNAinactiveNAX-RAY2015Qin et al. 2015
119RhodopsinOX2 orexin receptorHuman4S0V2.5Suvorexantsmall moleculeantagonistNAinactiveNAX-RAY2015Yin et al. 2015
120RhodopsinM3 muscarinic receptorRat4U143.57Tiotropiumsmall moleculeinverse agonistNAinactiveNAX-RAY2014Thorsen et al. 2014
121RhodopsinM3 muscarinic receptorRat4U152.8Tiotropiumsmall moleculeinverse agonistNAinactiveNAX-RAY2014Thorsen et al. 2014
122RhodopsinM3 muscarinic receptorRat4U163.7N-methyl scopolaminesmall moleculeantagonistNAinactiveNAX-RAY2014Thorsen et al. 2014
123RhodopsinA2A adenosine receptorHuman4UG22.6CGS21680small moleculeagonistNAinactive or minimally activatedNAX-RAY2015Lebon et al. 2015
124RhodopsinA2A adenosine receptorHuman4UHR2.6CGS21680small moleculeagonistNAinactive or minimally activatedNAX-RAY2015Lebon et al. 2015
125RhodopsinRhodopsinSquid4WW32.8all-trans-retinalsmall moleculeagonistNAinactive or minimally activated (lumirhodopsin)NAX-RAY2015Murakami et al. 2015
126RhodopsinRhodopsinBovine4X1H2.29unligandedunligandedunligandedNAactivated opsinNAX-RAY2015Blankenship et al. 2015
127RhodopsinNTS1 neurotensin receptorRat4XEE2.9Neurotensin (8-13)peptideagonistNAactivated (partially)NAX-RAY2015Krumm et al. 2015
128RhodopsinNTS1 neurotensin receptorRat4XES2.6Neurotensin (8-13)peptideagonistNAactivated (partially)NAX-RAY2015Krumm et al. 2015
129RhodopsinP2Y1 receptorHuman4XNV2.2BPTUsmall moleculeantagonistNAinactiveNAX-RAY2015Zhang et al. 2015
130RhodopsinP2Y1 receptorHuman4XNW2.7MRS2500small moleculeantagonistNAinactiveNAX-RAY2015Zhang et al. 2015
131RhodopsinViral US28 receptorVirus4XT12.89Human CX3CL1peptideagonistNAactivatedNAX-RAY2015Burg et al. 2015
132RhodopsinViral US28 receptorVirus4XT33.8Human CX3CL1peptideagonistNAactivatedNAX-RAY2015Burg et al. 2015
133RhodopsinAT1R angiotensin II type 1 receptorHuman4YAY2.9ZD7155small moleculeantagonistNAinactiveNAX-RAY2015Zhang et al. 2015
134RhodopsinLPA1 receptorHuman4Z343.0ONO-9780307small moleculeantagonistNAinactiveNAX-RAY2015Chrencik et al. 2015
135RhodopsinLPA1 receptorHuman4Z352.9ONO-9780307small moleculeantagonistNAinactiveNAX-RAY2015Chrencik et al. 2015
136RhodopsinLPA1 receptorHuman4Z362.9ONO-3080573small moleculeantagonistNAinactiveNAX-RAY2015Chrencik et al. 2015
137RhodopsinOX1 orexin receptorHuman4ZJ82.75Suvorexantsmall moleculeantagonistNAinactiveNAX-RAY2016Yin et al. 2016
138RhodopsinOX1 orexin receptorHuman4ZJC2.83SB-674042small moleculeantagonistNAinactiveNAX-RAY2016Yin et al. 2016
139RhodopsinAT1R angiotensin II type 1 receptorHuman4ZUD2.8Olmesartansmall moleculeantagonistNAinactiveNAX-RAY2015Zhang et al. 2015
140RhodopsinRhodopsinHuman4ZWJ3.3all-trans-retinalsmall moleculeagonistNAactivatedVisual arrestin (fused)X-RAY2015Kang et al. 2015
141Rhodopsinbeta1 adrenergic receptorTurkey5A8E2.47-Methylcyanopindololsmall moleculeinverse agonistNAinactiveNAX-RAY2015Sato et al. 2015
142Rhodopsinmu opioid receptorMouse5C1M2.1BU75small moleculeagonistNAactivatedNAX-RAY2015Huang et al. 2015
143RhodopsinM1 muscarinic receptorHuman5CXV2.7Tiotropiumsmall moleculeantagonistNAinactiveNAX-RAY2016Thal et al. 2016
144Rhodopsinbeta2 adrenergic receptorHuman5D5A2.48carazololsmall moleculeinverse agonistNAinactiveNAX-RAY2016Huang et al. 2016
145Rhodopsinbeta2 adrenergic receptorHuman5D5B3.8carazololsmall moleculeinverse agonistNAinactiveNAX-RAY2016Huang et al. 2016
146Rhodopsinbeta2 adrenergic receptorHuman5D6L3.2Carazololsmall moleculeinverse agonistNAinactiveNAX-RAY2016Ma et al. 2016
147RhodopsinRhodopsinHuman5DGY7.7all-trans-retinalsmall moleculeagonistNAactivatedVisual arrestin (fused)X-RAY2016Zhou et al. 2016
148RhodopsinNociception-orphanin FQ (NOP) receptorHuman5DHG3.0C-35small moleculeantagonistNAinactiveNAX-RAY2015Miller et al. 2015
149RhodopsinNociception-orphanin FQ (NOP) receptorHuman5DHH3.0SB-612111small moleculeantagonistNAinactiveNAX-RAY2015Miller et al. 2015
150RhodopsinM4 muscarinic receptorHuman5DSG2.6Tiotropiumsmall moleculeantagonistNAinactiveNAX-RAY2016Thal et al. 2016
151RhodopsinRhodopsinBovine5DYS2.3all-trans-retinalsmall moleculeagonistNAactivated (metarhodopsin II)NAX-RAY2016Singhal et al. 2016
152RhodopsinRhodopsinBovine5EN02.81all-trans-retinalsmall moleculeagonistNAactivated (metarhodopsin II)NAX-RAY2016Singhal et al. 2016
153Rhodopsinbeta1 adrenergic receptorTurkey5F8U3.35cyanopindololsmall moleculeantagonistNAinactiveNAX-RAY2015Leslie et al. 2015
154RhodopsinA2A adenosine receptorHuman5G533.4NECAsmall moleculeagonistNAactivatedmini-GsX-RAY2016Carpenter et al. 2016
155RhodopsinA2A adenosine receptorHuman5IU41.72ZM-241385small moleculeantagonistNAinactiveNAX-RAY2016Segala et al. 2016
156RhodopsinA2A adenosine receptorHuman5IU71.912csmall moleculeantagonistNAinactiveNAX-RAY2016Segala et al. 2016
157RhodopsinA2A adenosine receptorHuman5IU82.012fsmall moleculeantagonistNAinactiveNAX-RAY2016Segala et al. 2016
158RhodopsinA2A adenosine receptorHuman5IUA2.212bsmall moleculeantagonistNAinactiveNAX-RAY2016Segala et al. 2016
159RhodopsinA2A adenosine receptorHuman5IUB2.112xsmall moleculeantagonistNAinactiveNAX-RAY2016Segala et al. 2016
160Rhodopsinbeta2 adrenergic receptorHuman5JQH3.2Carazololsmall moleculeinverse agonistNAinactiveNAX-RAY2016Staus et al. 2016
161Rhodopsinbeta2 adrenergic receptorHuman3SN63.2BI-167107small moleculeagonistNAactivatedGs heterotrimerX-RAY2011Rasmussen et al. 2011b
162RhodopsinM2 muscarinic receptorHuman3UON3.03-quinuclidinyl-benzilatesmall moleculeantagonistNAinactiveNAX-RAY2012Haga et al. 2012
163GlutamatemGlu5 receptorHuman4OO92.6Mavoglurantsmall moleculeantagonistnegative allosteric modulatorinactiveNAX-RAY2014Dore et al. 2014
164GlutamatemGlu1 receptorHuman4OR22.8FITMsmall moleculeantagonistnegative allosteric modulatorinactiveNAX-RAY2014Wu et al. 2014
165GlutamatemGlu5 receptorHuman5CGC3.1Comp. 14small moleculeantagonistnegative allosteric modulatorinactiveNAX-RAY2015Christopher et al. 2015
166GlutamatemGlu5 receptorHuman5CGD2.6Comp. 25small moleculeantagonistnegative allosteric modulatorinactiveNAX-RAY2015Christopher et al. 2015
167RhodopsinETB endothelin receptorHuman5GLH2.8endothelin-1peptideagonistNAactivatedNAX-RAY2016Shihoya et al. 2016
168RhodopsinETB endothelin receptorHuman5GLI2.5unligandedunligandedunligandedNAinactiveNAX-RAY2016Shihoya et al. 2016
169RhodopsinA2A adenosine receptorHuman5K2A2.5ZM-241385small moleculeantagonistNAinactiveNAX-RAY2016Batyuk et al. 2016
170RhodopsinA2A adenosine receptorHuman5K2B2.5ZM-241385small moleculeantagonistNAinactiveNAX-RAY2016Batyuk et al. 2016
171RhodopsinA2A adenosine receptorHuman5K2C1.9ZM-241385small moleculeantagonistNAinactiveNAX-RAY2016Batyuk et al. 2016
172RhodopsinA2A adenosine receptorHuman5K2D1.9ZM-241385small moleculeantagonistNAinactiveNAX-RAY2016Batyuk et al. 2016
173RhodopsinCB1 cannabinoid receptorHuman5TGZ2.8AM6538small moleculeantagonistNAinactiveNAX-RAY2016Hua et al. 2016
174FrizzledSmoothenedHuman5V562.9TC114small moleculeantagonistNAinactiveNAX-RAY2017Zhang et al. 2017
175FrizzledSmoothenedHuman5V573.0TC114small moleculeantagonistNAinactiveNAX-RAY2017Zhang et al. 2017
176SecretinGLP1 glucagon-like peptide receptorHuman5VEW2.7PF-06372222small moleculeantagonistnegative allosteric modulatorinactiveNAX-RAY2017Song et al. 2017
177SecretinGLP1 glucagon-like peptide receptorHuman5VEX3.0NNC0640small moleculeantagonistnegative allosteric modulatorinactiveNAX-RAY2017Song et al. 2017
178SecretinGlucagon receptorHuman5XEZ3.0NNC0640small moleculeantagonistnegative allosteric modulatorinactiveNAX-RAY2017Zhang et al. 2017
179SecretinGlucagon receptorHuman5XF13.19NNC0640small moleculeantagonistnegative allosteric modulatorinactiveNAX-RAY2017Zhang et al. 2017
180RhodopsinCCR9 chemokine receptorHuman5LWE2.8Vercirnonsmall moleculeantagonistallosteric antagonistinactiveNAX-RAY2016Oswald et al. 2016
181RhodopsinPAR2 proteinase-activated receptorHuman5NDD2.8AZ8838small moleculeantagonistNAinactiveNAX-RAY2017Cheng et al. 2017
182RhodopsinPAR2 proteinase-activated receptorHuman5NDZ3.6AZ3451small moleculeantagonistallosteric antagonistinactiveNAX-RAY2017Cheng et al. 2017
183RhodopsinPAR2 proteinase-activated receptorHuman5NJ64.0AZ7188small moleculeantagonistNAinactiveNAX-RAY2017Cheng et al. 2017
184RhodopsinNTS1 neurotensin receptorRat5T043.3Neurotensin (8-13)peptideagonistNAactivated (partially)NAX-RAY2016Krumm 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 bundleinactiveNAX-RAY2016Zheng et al. 2016
186RhodopsinRhodopsinBovine5TE32.7unligandedunligandedunligandedNAactivated opsinNAX-RAY2017Gulati et al. 2017
187RhodopsinRhodopsinBovine5TE54.016mrsix-carbon ring retinal chromophoreinverse agonistNAinactiveNAX-RAY2017Gulati et al. 2017
188Rhodopsin5-HT2B serotonin receptorHuman5TVN2.9LSDsmall moleculeagonistbiased agonist (beta-arrestin)inactive or minimally activatedNAX-RAY2017Wacker et al. 2017
189RhodopsinCB1 cannabinoid receptorHuman5U092.6Taranabantsmall moleculeinverse agonistNAinactiveNAX-RAY2016Shao et al. 2016
190RhodopsinA1 adenosine receptorHuman5UEN3.2DU172small moleculeantagonistNAinactiveNAX-RAY2017Glukhova et al. 2017
191RhodopsinA2A adenosine receptorHuman5UIG3.5Comp. 1small moleculeantagonistdual antagonist - second target: NR2BinactiveNAX-RAY2017Sun et al. 2017
192RhodopsinAT2R angiotensin II type 2 receptorHuman5UNF2.8Comp. 1small moleculeligandNAactive-likeNAX-RAY2017Zhang et al. 2017
193RhodopsinAT2R angiotensin II type 2 receptorHuman5UNG2.8Comp. 1small moleculeligandNAactive-likeNAX-RAY2017Zhang et al. 2017
194RhodopsinAT2R angiotensin II type 2 receptorHuman5UNH2.9Comp. 2small moleculeligandNAactive-likeNAX-RAY2017Zhang et al. 2017
195RhodopsinA2A adenosine receptorHuman5UVI3.2ZM-241385small moleculeantagonistTBDinactiveNAX-RAY2017Martin-Garcia et al. 2017
196RhodopsinA2A adenosine receptorHuman5JTB2.8ZM-241385small moleculeantagonistNAinactiveNAX-RAY2017Melnikov et al. 2017
197RhodopsinFFA1 receptor (GPR40)Human5TZR2.2MK-8666small moleculepartial agonistNAinactive or minimally activatedNAX-RAY2017Lu et al. 2017
198RhodopsinFFA1 receptor (GPR40)Human5TZY3.22MK-8666 + AP8small moleculepartial agonist + full allosteric agonistfull allosteric agonistinactive or minimally activatedNAX-RAY2017Lu et al. 2017
199SecretinGLP1 glucagon-like peptide receptorHuman5NX23.7Peptide 5peptideagonistNAactivatedNAX-RAY2017Rappas et al. 2017
200RhodopsinFFA1 receptor (GPR40)Human5KW22.76TBDTBDTBDTBDTBDTBDX-RAY2018Ho et al. 2018
201RhodopsinA2A adenosine receptorHuman5MZJ2.0Theophyllinesmall moleculeantagonistNAinactiveNAX-RAY2017Cheng et al. 2017
202RhodopsinA2A adenosine receptorHuman5MZP2.1Caffeinesmall moleculeantagonistNAinactiveNAX-RAY2017Cheng et al. 2017
203RhodopsinA2A adenosine receptorHuman5N2R2.8PSB36small moleculeantagonistNAinactiveNAX-RAY2017Cheng et al. 2017
204RhodopsinA1 adenosine receptorHuman5N2S3.3PSB36small moleculeantagonistNAinactiveNAX-RAY2017Cheng et al. 2017
205RhodopsinA2A adenosine receptorHuman5NLX2.14ZM241385small moleculeantagonistNAinactiveNAX-RAY2017Weinert et al. 2017
206RhodopsinA2A adenosine receptorHuman5NM21.95ZM241385small moleculeantagonistNAinactiveNAX-RAY2017Weinert et al. 2017
207RhodopsinA2A adenosine receptorHuman5NM41.7ZM241385small moleculeantagonistNAinactiveNAX-RAY2017Weinert et al. 2017
208RhodopsinC5a1 complement peptide receptorHuman5O9H2.7TBDTBDTBDTBDTBDTBDX-RAY2018Robertson et al. 2018
209RhodopsinA2A adenosine receptorHuman5OLG1.87TBDTBDTBDTBDTBDTBDX-RAY2018Rucktooa et al. 2018
210RhodopsinA2A adenosine receptorHuman5OLH2.6TBDTBDTBDTBDTBDTBDX-RAY2018Rucktooa et al. 2018
211RhodopsinA2A adenosine receptorHuman5OLO3.1TBDTBDTBDTBDTBDTBDX-RAY2018Rucktooa et al. 2018
212RhodopsinA2A adenosine receptorHuman5OLV2.0TBDTBDTBDTBDTBDTBDX-RAY2018Rucktooa et al. 2018
213RhodopsinA2A adenosine receptorHuman5OLZ1.9TBDTBDTBDTBDTBDTBDX-RAY2018Rucktooa et al. 2018
214RhodopsinA2A adenosine receptorHuman5OM12.1TBDTBDTBDTBDTBDTBDX-RAY2018Rucktooa et al. 2018
215RhodopsinA2A adenosine receptorHuman5OM42.0TBDTBDTBDTBDTBDTBDX-RAY2018Rucktooa et al. 2018
216Rhodopsin5-HT2B serotonin receptorHuman5TUD3.0TBDTBDTBDTBDTBDTBDX-RAY2017Ishchenko et al. 2017
217RhodopsinCCR5 chemokine receptorHuman5UIW2.2TBDTBDTBDTBDTBDTBDX-RAY2017Zheng et al. 2017
218Rhodopsin5-HT1B serotonin receptorHuman5V543.9TBDTBDTBDTBDTBDTBDX-RAY2018Yin et al. 2018
219RhodopsinRhodopsinHuman5W0P3.01unligandedNANANAactivatedVisual arrestinX-RAY2017Zhou et al. 2017
220RhodopsinD4 dopamine receptorHuman5WF62.9TBDTBDTBDTBDTBDTBDX-RAY2018White et al. 2018
221RhodopsinD4 dopamine receptorHuman5WIU1.96TBDTBDTBDTBDTBDTBDX-RAY2017Wacker et al. 2017
222RhodopsinD4 dopamine receptorHuman5WIV2.14TBDTBDTBDTBDTBDTBDX-RAY2017Wacker et al. 2017
223RhodopsinRhodopsinBovine5WKT3.2TBDTBDTBDTBDTBDTBDX-RAY2017Broecker et al. 2017
224RhodopsinOX2 orexin receptorHuman5WQC1.96TBDTBDTBDTBDTBDTBDX-RAY2017Suno et al. 2017
225RhodopsinOX2 orexin receptorHuman5WS32.3TBDTBDTBDTBDTBDTBDX-RAY2017Suno et al. 2017
226Rhodopsinbeta2 adrenergic receptorHuman5X7D2.7TBDTBDTBDTBDTBDTBDX-RAY2017Liu et al. 2017
227RhodopsinETB endothelin receptorHuman5X932.2TBDTBDTBDTBDTBDTBDX-RAY2017Shihoya et al. 2017
228RhodopsinETB endothelin receptorHuman5XPR3.6TBDTBDTBDTBDTBDTBDX-RAY2017Shihoya et al. 2017
229RhodopsinCB1 cannabinoid receptorHuman5XR82.95TBDTBDTBDTBDTBDTBDX-RAY2017Hua et al. 2017
230RhodopsinCB1 cannabinoid receptorHuman5XRA2.8TBDTBDTBDTBDTBDTBDX-RAY2017Hua et al. 2017
231RhodopsinLPA6 receptor Zebrafish5XSZ3.2TBDTBDTBDTBDTBDTBDX-RAY2017Taniguchi et al. 2017
232RhodopsinY1 neuropeptide receptorHuman5ZBH3.0TBDTBDTBDTBDTBDTBDX-RAY2018Yang et al. 2018
233RhodopsinY1 neuropeptide receptorHuman5ZBQ2.7TBDTBDTBDTBDTBDTBDX-RAY2018Yang et al. 2018
234RhodopsinA2A adenosine receptorHuman6AQF2.51TBDTBDTBDTBDTBDTBDX-RAY2018Eddy et al. 2018
235Rhodopsinkappa opioid receptorHuman6B733.1TBDTBDTBDTBDTBDTBDX-RAY2018Che et al. 2018
236Rhodopsin5-HT2C serotonin receptorHuman6BQG3.0TBDTBDTBDTBDTBDTBDX-RAY2018Peng et al. 2018
237Rhodopsin5-HT2C serotonin receptorHuman6BQH2.7TBDTBDTBDTBDTBDTBDX-RAY2018Peng et al. 2018
238RhodopsinD2 dopamine receptorHuman6CM42.87TBDTBDTBDTBDTBDTBDX-RAY2018Wang et al. 2018
239RhodopsinRhodopsinBovine6FK62.36RS01small moleculeagonistNAactivatedNAX-RAY2018Mattle et al. 2018
240RhodopsinRhodopsinBovine6FK72.62RS06small moleculeagonistNAactivatedNAX-RAY2018Mattle et al. 2018
241RhodopsinRhodopsinBovine6FK82.87RS08small moleculeagonistNAactivatedNAX-RAY2018Mattle et al. 2018
242RhodopsinRhodopsinBovine6FK92.63RS09small moleculeagonistNAactivatedNAX-RAY2018Mattle et al. 2018
243RhodopsinRhodopsinBovine6FKA2.7RS11small moleculeagonistNAactivatedNAX-RAY2018Mattle et al. 2018
244RhodopsinRhodopsinBovine6FKB3.03RS13small moleculeagonistNAactivatedNAX-RAY2018Mattle et al. 2018
245RhodopsinRhodopsinBovine6FKC2.46RS15small moleculeagonistNAactivatedNAX-RAY2018Mattle et al. 2018
246RhodopsinRhodopsinBovine6FKD2.49RS16small moleculeagonistNAactivatedNAX-RAY2018Mattle et al. 2018
247GlutamatemGlu5 receptorHuman6FFH2.65fenobamsmall moleculeantagonist + allosteric antagonistnegative allosteric modulatorinactiveNAX-RAY2018Christopher et al. 2018
248GlutamatemGlu5 receptorHuman6FFI2.2M-MPEPsmall moleculeantagonist + allosteric antagonistnegative allosteric modulatorinactiveNAX-RAY2018Christopher et al. 2018
249FrizzledSmoothenedXenopus6D323.75TBDTBDTBDTBDTBDTBDX-RAY2018Huang et al. 2018
250FrizzledSmoothenedXenopus6D353.9TBDTBDTBDTBDTBDTBDX-RAY2018Huang et al. 2018
251RhodopsinViral US28 receptorVirus5WB23.5TBDTBDTBDTBDTBDTBDX-RAY2018Jude et al. 2018
252RhodopsinA2A adenosine receptorHuman5WF52.6TBDTBDTBDTBDTBDTBDX-RAY2018White et al. 2018
253RhodopsinAT2R angiotensin II type 2 receptorHuman5XJM3.2TBDTBDTBDTBDTBDTBDX-RAY2018Asada et al. 2018
254FrizzledFZD4 frizzled receptorHuman6BD42.4TBDTBDTBDTBDTBDTBDX-RAY2018Yang et al. 2018
255Rhodopsin5-HT2B serotonin receptorHuman6DRX3.1lisuridesmall moleculeantagonistNainactive or minimally activatedTBDX-RAY2018McCorvy et al. 2018
256Rhodopsin5-HT2B serotonin receptorHuman6DRY2.92methylergonovinesmall moleculeagonistNAinactive or minimally activatedTBDX-RAY2018McCorvy et al. 2018
257Rhodopsin5-HT2B serotonin receptorHuman6DRZ3.1methysergidesmall moleculepartial agonistantagonist for wild type receptorinactive or minimally activatedTBDX-RAY2018McCorvy et al. 2018
258Rhodopsin5-HT2B serotonin receptorHuman6DS03.19LY266097small moleculepartial agonistbiased (Gq)inactive or minimally activatedTBDX-RAY2018McCorvy et al. 2018
259RhodopsinRhodopsinBovine6FUF3.12all-trans retinolsmall moleculeagonistNAactivatedmini-GoX-RAY2018Tsai et al. 2018
260SecretinPTH1 parathyroid hormone receptorHuman6FJ32.5TBDTBDTBDTBDTBDTBDX-RAY2018Ehrenmann et al. 2018
261RhodopsinM2 muscarinic receptorHuman5YC82.5TBDTBDTBDTBDTBDTBDX-RAY2018Suno et al. 2018
262RhodopsinM3 muscarinic receptorRat5ZHP3.1TBDTBDTBDTBDTBDTBDX-RAY2018Liu et al. 2018
263RhodopsinM2 muscarinic receptorHuman5ZK32.6TBDTBDTBDTBDTBDTBDX-RAY2018Suno et al. 2018
264RhodopsinM2 muscarinic receptorHuman5ZK83.0TBDTBDTBDTBDTBDTBDX-RAY2018Suno et al. 2018
265RhodopsinM2 muscarinic receptorHuman5ZKB2.95TBDTBDTBDTBDTBDTBDX-RAY2018Suno et al. 2018
266RhodopsinM2 muscarinic receptorHuman5ZKC2.3TBDTBDTBDTBDTBDTBDX-RAY2018Suno et al. 2018
267RhodopsinCB2 cannabinoid receptorHuman5ZTY2.8TBDTBDTBDTBDTBDTBDX-RAY2019Li et al. 2019
268Rhodopsin5-HT2A serotonin receptorHuman6A933.0TBDTBDTBDTBDTBDTBDX-RAY2019Kimura et al. 2019
269Rhodopsin5-HT2A serotonin receptorHuman6A942.9TBDTBDTBDTBDTBDTBDX-RAY2019Kimura et al. 2019
270RhodopsinCCR5 chemokine receptorHuman6AKX2.8TBDTBDTBDTBDTBDTBDX-RAY2018Zhu et al. 2018
271RhodopsinCCR5 chemokine receptorHuman6AKY2.8TBDTBDTBDTBDTBDTBDX-RAY2018Zhu et al. 2018
272RhodopsinAT1R angiotensin II type 1 receptorHuman6DO12.9TBDTBDTBDTBDTBDTBDX-RAY2019Wingler et al. 2019
273RhodopsinNK1 tachykinin receptor (substance-P receptor)Human6E593.4TBDTBDTBDTBDTBDTBDX-RAY2018Yin et al. 2018
274RhodopsinCCR2 chemokine receptorHuman6GPS3.3TBDTBDTBDTBDTBDTBDX-RAY2019Pautsch et al. 2019
275RhodopsinCCR2 chemokine receptorHuman6GPX2.7TBDTBDTBDTBDTBDTBDX-RAY2019Pautsch et al. 2019
276RhodopsinNK1 tachykinin receptor (substance-P receptor)Human6HLO2.4TBDTBDTBDTBDTBDTBDX-RAY2019Schoppe et al. 2019
277RhodopsinNK1 tachykinin receptor (substance-P receptor)Human6HLP2.2TBDTBDTBDTBDTBDTBDX-RAY2019Schoppe et al. 2019
278Rhodopsinbeta1 adrenergic receptorTurkey6IBL2.7TBDTBDTBDTBDTBDTBDX-RAY2019Warne et al. 2019
279RhodopsinETB endothelin receptorHuman6IGK2.0TBDTBDTBDTBDTBDTBDX-RAY2018Shihoya et al. 2018
280RhodopsinETB endothelin receptorHuman6IGL2.7TBDTBDTBDTBDTBDTBDX-RAY2018Shihoya et al. 2018
281RhodopsinNK1 tachykinin receptor (substance-P receptor)Human6J202.7TBDTBDTBDTBDTBDTBDX-RAY2019Chen et al. 2019
282RhodopsinNK1 tachykinin receptor (substance-P receptor)Human6J213.2TBDTBDTBDTBDTBDTBDX-RAY2019Chen et al. 2019
283RhodopsinMLT1A melatonin receptorHuman6ME22.8TBDTBDTBDTBDTBDTBDX-RAY2019Stauch et al. 2019
284RhodopsinMLT1A melatonin receptorHuman6ME32.9TBDTBDTBDTBDTBDTBDX-RAY2019Stauch et al. 2019
285RhodopsinMLT1A melatonin receptorHuman6ME43.2TBDTBDTBDTBDTBDTBDX-RAY2019Stauch et al. 2019
286RhodopsinMLT1A melatonin receptorHuman6ME53.2TBDTBDTBDTBDTBDTBDX-RAY2019Stauch et al. 2019
287RhodopsinMLT1B melatonin receptorHuman6ME62.8TBDTBDTBDTBDTBDTBDX-RAY2019Johansson et al. 2019
288RhodopsinMLT1B melatonin receptorHuman6ME73.2TBDTBDTBDTBDTBDTBDX-RAY2019Johansson et al. 2019
289RhodopsinMLT1B melatonin receptorHuman6ME83.1TBDTBDTBDTBDTBDTBDX-RAY2019Johansson et al. 2019
290RhodopsinMLT1B melatonin receptorHuman6ME93.3TBDTBDTBDTBDTBDTBDX-RAY2019Johansson et al. 2019
291RhodopsinA2A adenosine receptorHuman6MH84.2TBDTBDTBDTBDTBDTBDX-RAY2019Martin-Garcia et al. 2019
292Rhodopsinbeta2 adrenergic receptorHuman6MXT2.96TBDTBDTBDTBDTBDTBDX-RAY2018Masureel et al. 2018
293GlutamatemGlu5 receptorHuman6N4X4.0TBDTBDTBDTBDTBDTBDX-RAY2019Koehl et al. 2019
294RhodopsinViral US28 receptorVirus5WB13.51TBDTBDTBDTBDTBDTBDX-RAY2018Jude et al. 2018
295RhodopsinBLT1 leukotriene B4 receptorNA5X333.7TBDTBDTBDTBDTBDTBDX-RAY2018Hori et al. 2018
296RhodopsinEP3 prostanoid receptor (prostaglandin E receptor 3)Human6AK32.9TBDTBDTBDTBDTBDTBDX-RAY2018Morimoto et al. 2018
297RhodopsinDP2 prostanoid receptor (prostaglandin D2 receptor 2)Human6D262.8TBDTBDTBDTBDTBDTBDX-RAY2018Wang et al. 2018
298RhodopsinDP2 prostanoid receptor (prostaglandin D2 receptor 2)Human6D272.74TBDTBDTBDTBDTBDTBDX-RAY2018Wang et al. 2018
299RhodopsinTP prostanoid receptor (thromboxane A2 receptor)Human6IIU2.5TBDTBDTBDTBDTBDTBDX-RAY2018Fan et al. 2018
300RhodopsinTP prostanoid receptor (thromboxane A2 receptor)Human6IIV3.0TBDTBDTBDTBDTBDTBDX-RAY2018Fan et al. 2018
304RhodopsinPAF receptorHuman5ZKQ2.9TBDTBDTBDTBDTBDTBDX-RAY2018Cao et al. 2018
305RhodopsinPAF receptorHuman5ZKP2.81TBDTBDTBDTBDTBDTBDX-RAY2018Cao et al. 2018
314RhodopsinEP4 prostanoid receptor (prostaglandin E receptor 4)Human5YHL4.2TBDTBDTBDTBDTBDTBDX-RAY2018Toyoda et al. 2018
315RhodopsinEP4 prostanoid receptor (prostaglandin E receptor 4)Human5YWY3.2TBDTBDTBDTBDTBDTBDX-RAY2018Toyoda et al. 2018
316RhodopsinEP3 prostanoid receptor (prostaglandin E receptor 3)Human6M9T2.5TBDTBDTBDTBDTBDTBDX-RAY2018Audet et al. 2018
322RhodopsinRhodopsinBovine1JFP0.0TBDTBDTBDTBDTBDTBDNMR2001Yeagle et al. 2001
323RhodopsinRhodopsinBovine1LN60.0TBDTBDTBDTBDTBDTBDNMR2002Choi et al. 2002
327RhodopsinNK1 tachykinin receptor (substance-P receptor)Human2KS90.0TBDTBDTBDTBDTBDTBDNMR2010Gayen et al. 2010
328RhodopsinNK1 tachykinin receptor (substance-P receptor)Human2KSA0.0TBDTBDTBDTBDTBDTBDNMR2010Gayen et al. 2010
329RhodopsinNK1 tachykinin receptor (substance-P receptor)Human2KSB0.0TBDTBDTBDTBDTBDTBDNMR2010Gayen et al. 2010
330RhodopsinCXCR1 chemokine receptorHuman2LNL0.0TBDTBDTBDTBDTBDTBDNMR2012Park et al. 2012
331RhodopsinRhodopsinHuman6CMO4.5NANANANAactivatedGi heterotrimerElectron Microscopy2018Kang et al. 2018
334RhodopsinApelin receptorHuman5VBL2.6TBDTBDTBDTBDTBDTBDX-RAY2017Ma et al. 2017
335RhodopsinA2A adenosine receptorHuman5VRA2.35TBDTBDTBDTBDTBDTBDX-RAY2017Broecker et al. 2017
336RhodopsinA1 adenosine receptorHuman6D9H3.6Adenosinesmall moleculeagonistNAactivatedGi heterotrimerElectron Microscopy2018Draper-Joyce et al. 2018
337Rhodopsinmu opioid receptorHuman6DDE3.5DAMGOpeptideagonistNAactivatedGi heterotrimerElectron Microscopy2018Koehl et al. 2018
338Rhodopsinmu opioid receptorHuman6DDF3.5DAMGOpeptideagonistNAactivatedGi heterotrimerElectron Microscopy2018Koehl et al. 2018
339Rhodopsin5-HT1B serotonin receptorHuman6G793.78Donitriptansmall moleculeagonistNAactivatedGo heterotrimerElectron Microscopy2018Garcia-Nafria et al. 2018
340RhodopsinA2A adenosine receptorHuman6GDG4.11NECAsmall moleculeagonistNAactivatedMini GsElectron Microscopy2018Garcia-Nafria et al. 2018
341Rhodopsinbeta1 adrenergic receptorTurkey6H7J2.8Isoprenalinesmall moleculeagonistNAactivatedNAX-RAY2018Warne et al. 2018
342Rhodopsinbeta1 adrenergic receptorTurkey6H7L2.7Dobutaminesmall moleculeagonistNAactivatedNAX-RAY2018Warne et al. 2018
343Rhodopsinbeta1 adrenergic receptorTurkey6H7M2.76Salbutamolsmall moleculeagonistNAactivatedNAX-RAY2018Warne et al. 2018
344Rhodopsinbeta1 adrenergic receptorTurkey6H7N2.5Xamoterolsmall moleculeagonistNAactivatedNAX-RAY2018Warne et al. 2018
345Rhodopsinbeta1 adrenergic receptorTurkey6H7O2.8Cyanopindololsmall moleculeagonistNAactivatedNAX-RAY2018Warne et al. 2018
346RhodopsinNK1 tachykinin receptor (substance-P receptor)Human6HLL3.27CP-99,994small moleculeantagonistNAinactiveNAX-RAY2019Schoppe et al. 2019
347RhodopsinCCR5 chemokine receptorHuman6MEO3.9T-cell surface glycoprotein CD4proteinTBDTBDTBDTBDElectron Microscopy2018Shaik et al. 2018
348RhodopsinCCR5 chemokine receptorHuman6MET4.5T-cell surface glycoprotein CD4proteinTBDTBDTBDTBDElectron Microscopy2018Shaik et al. 2018
349RhodopsinCB1 cannabinoid receptorHuman6N4B3.0FUBsmall moleculeagonistNAactivatedGi heterotrimerElectron Microscopy2019Krishna Kumar et al. 2019
350RhodopsinM1 muscarinic receptorHuman6OIJ3.3Iperoxosmall moleculeagonistNAactivatedG11 heterotrimerElectron Microscopy2019Maeda et al. 2019
351RhodopsinM2 muscarinic receptorHuman6OIK3.6Iperoxosmall moleculeagonistNAactivatedGo heterotrimerElectron Microscopy2019Maeda et al. 2019
352GlutamatemGlu5 receptorHuman6N514.0Quisqualatesmall moleculeagonistNAactivatedNAElectron Microscopy2019Koehl et al. 2019
353GlutamatemGlu5 receptorHuman6N524.0unligandedNANANAinactiveNAElectron Microscopy2019Koehl et al. 2019
354SecretinCalcitonin receptorHuman6NIY3.34sCTpeptideagonistNAactivatedGs heterotrimerElectron Microscopy2019Dal Maso et al. 2019
355SecretinCalcitonin receptorHuman5UZ74.1sCTpeptideagonistNAactivatedGs heterotrimerElectron Microscopy2019Liang et al. 2017
356SecretinCalcitonin receptorHuman6E3Y3.34sCTpeptideagonistNAactivatedGs heterotrimerElectron Microscopy2019Liang et al. 2018
357SecretinGLP1 glucagon-like peptide receptorRabbit5VAI4.1GLP-1peptideagonistNAactivatedGs heterotrimerElectron Microscopy2017Zhang et al. 2017
358SecretinGLP1 glucagon-like peptide receptorHuman6B3J3.3Exendin-P5peptideagonistbiased agonist (G protein-biased)activatedGs heterotrimerElectron Microscopy2018Liang et al. 2018
359SecretinPTH1 parathyroid hormone receptorRat6NBF3.0LA-PTHpeptideagonistNAactivatedGs heterotrimerElectron Microscopy2019Zhao et al. 2019
360SecretinPTH1 parathyroid hormone receptorRat6NBH3.5LA-PTHpeptideagonistNAactivatedGs heterotrimerElectron Microscopy2019Zhao et al. 2019
361SecretinPTH1 parathyroid hormone receptorRat6NBI4.0LA-PTHpeptideagonistNAactivatedGs heterotrimerElectron Microscopy2019Zhao et al. 2019
362FrizzledSmoothenedMouse6O3C2.8TBDTBDTBDTBDactivatedTBDTBD2019Deshpande et al. 2019
363FrizzledSmoothenedHuman6OT03.84TBDTBDTBDTBDactivatedGi1 heterotrimerTBD2019Qi et al. 2019
366Rhodopsinbeta2 adrenergic receptorHuman6E673.7BI-167107small moleculeagonistNAactivatedGs peptide (fused)X-RAY2019Liu et al. 2019
367RhodopsinA2A adenosine receptorHuman6GT32.0AZD4635small moleculeantagonistNAinactiveNAX-RAY2019Borodovsky et al. 2019
368RhodopsinRhodopsin-1Jumping Spider6I9K2.14TBDTBDTBDTBDTBDTBDTBD2019Varma et al. 2019
369RhodopsinSuccinate receptor 1Rat6IBB2.12TBDTBDTBDTBDTBDTBDTBD2019Haffke et al. 2019
370RhodopsinETB endothelin receptorHuman6K1Q2.7TBDTBDTBDTBDTBDTBDTBD2019Nagiri et al. 2019
371RhodopsinCB1 cannabinoid receptorHuman6KQI3.24TBDTBDTBDTBDTBDTBDTBD2019Shao et al. 2019
372Rhodopsinbeta2 adrenergic receptorHuman6N483.2BI-167107 + positive allosteric modulatorsmall moleculeagonist + positive allosteric modulatorpositive allosteric modulator as second ligandactivatedTBDTBD2019Liu et al. 2019
373RhodopsinRhodopsinBovine6OFJ4.5TBDTBDTBDTBDTBDTBDTBD2019Zhao et al. 2019
374RhodopsinNTS1 neurotensin receptorHuman6OS93.0TBDTBDTBDTBDactivatedGi1 heterotrimerTBD2019Kato et al. 2019
375RhodopsinNTS1 neurotensin receptorHuman6OSA3.0TBDTBDTBDTBDactivatedGi1 heterotrimerTBD2019Kato et al. 2019
376RhodopsinRhodopsinBovine6OY93.9all-trans-retinalsmall moleculeagonistNAactivatedGt heterotrimerElectron Microscopy2019Gao et al. 2019
377RhodopsinRhodopsinBovine6OYA3.3all-trans-retinalsmall moleculeagonistNAactivatedGt heterotrimerElectron Microscopy2019Gao et al. 2019
378RhodopsinRhodopsinHuman6QNO4.38TBDTBDTBDTBDactivatedGi1 heterotrimerTBD2019Tsai et al. 2019
379RhodopsinCCR7 chemokine receptorHuman6QZH2.1Cmp2105small moleculeallosteric antagonistintracellular allosteric antagonistTBDNATBD2019Jaeger et al. 2019
380RhodopsinSuccinate receptor 1Human6RNK1.94TBDTBDTBDTBDTBDTBDTBD2019Haffke et al. 2019
381RhodopsinA2A adenosine receptorHuman6JZH2.25ZM241385small moleculeantagonistNATBDNAX-RAY2019Nango et al. 2019
382RhodopsinCysLT1 cysteinyl leukotriene receptorHuman6RZ42.7pranlukastsmall moleculeantagonistNATBDNAX-RAY2019Luginina et al. 2019
383RhodopsinCysLT1 cysteinyl leukotriene receptorHuman6RZ52.53zafirlukastsmall moleculeantagonistNATBDNAX-RAY2019Luginina 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 Method Year References



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