4UHR
 
 | | Thermostabilised HUMAN A2a Receptor with CGS21680 bound | | Descriptor: | 2-[P-(2-CARBOXYETHYL)PHENYLETHYL-AMINO]-5'-N-ETHYLCARBOXAMIDO ADENOSINE, THERMOSTABILISED HUMAN A2A RECEPTOR | | Authors: | Lebon, G, Edwards, P.C, Leslie, A.G.W, Tate, C.G. | | Deposit date: | 2015-03-25 | | Release date: | 2015-04-08 | | Last modified: | 2024-11-13 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Molecular Determinants of Cgs21680 Binding to the Human Adenosine A2A Receptor.
Mol.Pharmacol., 87, 2015
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6Z10
 | | Crystal structure of a humanized (K18E, K269N) rat succinate receptor SUCNR1 (GPR91) in complex with a nanobody and antagonist | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 2-[2-[[3-[4-chloranyl-2-fluoranyl-5-[(3~{R})-piperidin-3-yl]oxy-phenyl]-2-fluoranyl-phenyl]carbonylamino]-5-fluoranyl-phenyl]ethanoic acid, CHLORIDE ION, ... | | Authors: | Haffke, M, Villard, F. | | Deposit date: | 2020-05-11 | | Release date: | 2020-09-16 | | Last modified: | 2024-11-20 | | Method: | X-RAY DIFFRACTION (2.269 Å) | | Cite: | Discovery and Optimization of Novel SUCNR1 Inhibitors: Design of Zwitterionic Derivatives with a Salt Bridge for the Improvement of Oral Exposure.
J.Med.Chem., 63, 2020
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4UG2
 | | Thermostabilised HUMAN A2a Receptor with CGS21680 bound | | Descriptor: | (2S)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 2-[P-(2-CARBOXYETHYL)PHENYLETHYL-AMINO]-5'-N-ETHYLCARBOXAMIDO ADENOSINE, THERMOSTABILISED HUMAN A2A RECEPTOR | | Authors: | Lebon, G, Edwards, P.C, Leslie, A.G.W, Tate, C.G. | | Deposit date: | 2015-03-21 | | Release date: | 2015-04-08 | | Last modified: | 2024-11-13 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Molecular Determinants of Cgs21680 Binding to the Human Adenosine A2A Receptor.
Mol.Pharmacol., 87, 2015
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3KJ6
 | | Crystal structure of a Methylated beta2 Adrenergic Receptor-Fab complex | | Descriptor: | Beta-2 adrenergic receptor, Fab heavy chain, Fab light chain, ... | | Authors: | Bokoch, M.P, Zou, Y, Rasmussen, S.G.F, Liu, C.W, Nygaard, R, Rosenbaum, D.M, Fung, J.J, Choi, H.-J, Thian, F.S, Kobilka, T.S, Puglisi, J.D, Weis, W.I, Pardo, L, Prosser, S, Mueller, L, Kobilka, B.K. | | Deposit date: | 2009-11-02 | | Release date: | 2010-02-16 | | Last modified: | 2024-11-06 | | Method: | X-RAY DIFFRACTION (3.4 Å) | | Cite: | Ligand-specific regulation of the extracellular surface of a G-protein-coupled receptor.
Nature, 463, 2010
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2R4S
 | | Crystal structure of the human beta2 adrenoceptor | | Descriptor: | Beta-2 adrenergic receptor, antibody for beta2 adrenoceptor, heavy chain, ... | | Authors: | Rasmussen, S.G.F, Choi, H.J, Rosenbaum, D.M, Kobilka, T.S, Thian, F.S, Edwards, P.C, Burghammer, M, Ratnala, V.R, Sanishvili, R, Fischetti, R.F, Schertler, G.F, Weis, W.I, Kobilka, B.K. | | Deposit date: | 2007-08-31 | | Release date: | 2007-11-06 | | Last modified: | 2024-10-16 | | Method: | X-RAY DIFFRACTION (3.4 Å) | | Cite: | Crystal structure of the human beta2 adrenergic G-protein-coupled receptor.
Nature, 450, 2007
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2R4R
 | | Crystal structure of the human beta2 adrenoceptor | | Descriptor: | Beta-2 adrenergic receptor, antibody for beta2 adrenoceptor, heavy chain, ... | | Authors: | Rasmussen, S.G.F, Choi, H.J, Rosenbaum, D.M, Kobilka, T.S, Thian, F.S, Edwards, P.C, Burghammer, M, Ratnala, V.R, Sanishvili, R, Fischetti, R.F, Schertler, G.F, Weis, W.I, Kobilka, B.K. | | Deposit date: | 2007-08-31 | | Release date: | 2007-11-06 | | Last modified: | 2024-11-06 | | Method: | X-RAY DIFFRACTION (3.4 Å) | | Cite: | Crystal structure of the human beta2 adrenergic G-protein-coupled receptor.
Nature, 450, 2007
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2LNL
 | | Structure of human CXCR1 in phospholipid bilayers | | Descriptor: | C-X-C chemokine receptor type 1 | | Authors: | Park, S, Das, B.B, Casagrande, F, Nothnagel, H, Chu, M, Kiefer, H, Maier, K, De Angelis, A, Marassi, F.M, Opella, S.J. | | Deposit date: | 2011-12-31 | | Release date: | 2012-10-17 | | Last modified: | 2024-11-06 | | Method: | SOLID-STATE NMR | | Cite: | Structure of the chemokine receptor CXCR1 in phospholipid bilayers.
Nature, 491, 2012
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4MQS
 | | Structure of active human M2 muscarinic acetylcholine receptor bound to the agonist iperoxo | | Descriptor: | 4-(4,5-dihydro-1,2-oxazol-3-yloxy)-N,N,N-trimethylbut-2-yn-1-aminium, Muscarinic acetylcholine receptor M2, Nanobody 9-8 | | Authors: | Kruse, A.C, Ring, A.M, Manglik, A, Hu, J, Hu, K, Eitel, K, Huebner, H, Pardon, E, Valant, C, Sexton, P.M, Christopoulos, A, Felder, C.C, Gmeiner, P, Steyaert, J, Weis, W.I, Garcia, K.C, Wess, J, Kobilka, B.K. | | Deposit date: | 2013-09-16 | | Release date: | 2013-11-27 | | Last modified: | 2024-10-09 | | Method: | X-RAY DIFFRACTION (3.5 Å) | | Cite: | Activation and allosteric modulation of a muscarinic acetylcholine receptor.
Nature, 504, 2013
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5LWE
 | | Crystal structure of the human CC chemokine receptor type 9 (CCR9) in complex with vercirnon | | Descriptor: | C-C chemokine receptor type 9, CHOLESTEROL, MALONATE ION, ... | | Authors: | Oswald, C, Rappas, M, Kean, J, Dore, A.S, Errey, J.C, Bennett, K, Deflorian, F, Christopher, J.A, Jazayeri, A, Mason, J.S, Congreve, M, Cooke, R.M, Marshall, F.H. | | Deposit date: | 2016-09-16 | | Release date: | 2016-12-07 | | Last modified: | 2024-11-20 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Intracellular allosteric antagonism of the CCR9 receptor.
Nature, 540, 2016
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4MQT
 | | Structure of active human M2 muscarinic acetylcholine receptor bound to the agonist iperoxo and allosteric modulator LY2119620 | | Descriptor: | 3-amino-5-chloro-N-cyclopropyl-4-methyl-6-[2-(4-methylpiperazin-1-yl)-2-oxoethoxy]thieno[2,3-b]pyridine-2-carboxamide, 4-(4,5-dihydro-1,2-oxazol-3-yloxy)-N,N,N-trimethylbut-2-yn-1-aminium, Muscarinic acetylcholine receptor M2, ... | | Authors: | Kruse, A.C, Ring, A.M, Manglik, A, Hu, J, Hu, K, Eitel, K, Huebner, H, Pardon, E, Valant, C, Sexton, P.M, Christopoulos, A, Felder, C.C, Gmeiner, P, Steyaert, J, Weis, W.I, Garcia, K.C, Wess, J, Kobilka, B.K. | | Deposit date: | 2013-09-16 | | Release date: | 2013-11-27 | | Last modified: | 2024-11-06 | | Method: | X-RAY DIFFRACTION (3.7 Å) | | Cite: | Activation and allosteric modulation of a muscarinic acetylcholine receptor.
Nature, 504, 2013
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7F83
 | | Crystal Structure of a receptor in Complex with inverse agonist | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 2-(2-methylimidazo[2,1-b][1,3]thiazol-6-yl)-1-[2-[(1R)-5-(6-methylpyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]-2,7-diazaspiro[3.5]nonan-7-yl]ethanone, Growth hormone secretagogue receptor type 1,Soluble cytochrome b562 | | Authors: | Xu, Z, Shao, Z. | | Deposit date: | 2021-07-01 | | Release date: | 2022-01-19 | | Last modified: | 2024-11-13 | | Method: | X-RAY DIFFRACTION (2.94 Å) | | Cite: | Molecular mechanism of agonism and inverse agonism in ghrelin receptor.
Nat Commun, 13, 2022
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8QOT
 | | Structure of the mu opioid receptor bound to the antagonist nanobody NbE | | Descriptor: | Anti-Fab Nanobody, Mu-type opioid receptor, NabFab HC, ... | | Authors: | Yu, J, Kumar, A, Zhang, X, Martin, C, Raia, P, Manglik, A, Ballet, S, Boland, A, Stoeber, M. | | Deposit date: | 2023-09-29 | | Release date: | 2023-12-27 | | Last modified: | 2025-01-29 | | Method: | ELECTRON MICROSCOPY (3.2 Å) | | Cite: | Structural basis of mu-opioid receptor targeting by a nanobody antagonist.
Nat Commun, 15, 2024
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3VG9
 | | Crystal structure of human adenosine A2A receptor with an allosteric inverse-agonist antibody at 2.7 A resolution | | Descriptor: | 4-{2-[(7-amino-2-furan-2-yl[1,2,4]triazolo[1,5-a][1,3,5]triazin-5-yl)amino]ethyl}phenol, Adenosine receptor A2a, DODECYL-BETA-D-MALTOSIDE, ... | | Authors: | Hino, T, Arakawa, T, Iwanari, H, Yurugi-Kobayashi, T, Ikeda-Suno, C, Nakada-Nakura, Y, Kusano-Arai, O, Weyand, S, Shimamura, T, Nomura, N, Cameron, A.D, Kobayashi, T, Hamakubo, T, Iwata, S, Murata, T. | | Deposit date: | 2011-08-04 | | Release date: | 2012-02-01 | | Last modified: | 2024-11-06 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | G-protein-coupled receptor inactivation by an allosteric inverse-agonist antibody
Nature, 482, 2012
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3UZC
 | | Thermostabilised Adenosine A2A receptor in complex with 4-(3-amino-5-phenyl-1,2,4-triazin-6-yl)-2-chlorophenol | | Descriptor: | 4-(3-amino-5-phenyl-1,2,4-triazin-6-yl)-2-chlorophenol, Adenosine A2A Receptor | | Authors: | Congreve, M, Andrews, S.P, Dore, A.S, Hollenstein, K, Hurrell, E, Langmead, C.J, Mason, J.S, Ng, I.W, Zhukov, A, Weir, M, Marshall, F.H. | | Deposit date: | 2011-12-07 | | Release date: | 2012-03-21 | | Last modified: | 2024-10-30 | | Method: | X-RAY DIFFRACTION (3.341 Å) | | Cite: | Discovery of 1,2,4-Triazine Derivatives as Adenosine A(2A) Antagonists using Structure Based Drug Design
J.Med.Chem., 55, 2012
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3UZA
 | | Thermostabilised Adenosine A2A receptor in complex with 6-(2,6-Dimethylpyridin-4-yl)-5-phenyl-1,2,4-triazin-3-amine | | Descriptor: | 6-(2,6-dimethylpyridin-4-yl)-5-phenyl-1,2,4-triazin-3-amine, Adenosine receptor A2a | | Authors: | Congreve, M, Andrews, S.P, Dore, A.S, Hollenstein, K, Hurrell, E, Langmead, C.J, Mason, J.S, Ng, I.W, Tehan, B, Zhukov, A, Weir, M, Marshall, F.H. | | Deposit date: | 2011-12-07 | | Release date: | 2012-03-21 | | Last modified: | 2024-10-30 | | Method: | X-RAY DIFFRACTION (3.273 Å) | | Cite: | Discovery of 1,2,4-Triazine Derivatives as Adenosine A(2A) Antagonists using Structure Based Drug Design
J.Med.Chem., 55, 2012
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6VI4
 | | Nanobody-Enabled Monitoring of Kappa Opioid Receptor States | | Descriptor: | (3R)-7-hydroxy-N-{(2S)-1-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]-3-methylbutan-2-yl}-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, CHOLESTEROL, Kappa opioid receptor, ... | | Authors: | Che, T, Roth, B.L. | | Deposit date: | 2020-01-11 | | Release date: | 2020-03-18 | | Last modified: | 2024-11-13 | | Method: | X-RAY DIFFRACTION (3.3 Å) | | Cite: | Nanobody-enabled monitoring of kappa opioid receptor states.
Nat Commun, 11, 2020
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3VGA
 | | Crystal structure of human adenosine A2A receptor with an allosteric inverse-agonist antibody at 3.1 A resolution | | Descriptor: | 4-{2-[(7-amino-2-furan-2-yl[1,2,4]triazolo[1,5-a][1,3,5]triazin-5-yl)amino]ethyl}phenol, Adenosine receptor A2a, antibody fab fragment heavy chain, ... | | Authors: | Hino, T, Arakawa, T, Iwanari, H, Yurugi-Kobayashi, T, Ikeda-Suno, C, Nakada-Nakura, Y, Kusano-Arai, O, Weyand, S, Shimamura, T, Nomura, N, Cameron, A.D, Kobayashi, T, Hamakubo, T, Iwata, S, Murata, T. | | Deposit date: | 2011-08-04 | | Release date: | 2012-02-01 | | Last modified: | 2024-10-30 | | Method: | X-RAY DIFFRACTION (3.1 Å) | | Cite: | G-protein-coupled receptor inactivation by an allosteric inverse-agonist antibody
Nature, 482, 2012
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2ZIY
 | | Crystal structure of squid rhodopsin | | Descriptor: | PALMITIC ACID, RETINAL, Rhodopsin | | Authors: | Miyano, M, Shimamura, T. | | Deposit date: | 2008-02-27 | | Release date: | 2008-05-06 | | Last modified: | 2024-11-20 | | Method: | X-RAY DIFFRACTION (3.7 Å) | | Cite: | Crystal structure of squid rhodopsin with intracellularly extended cytoplasmic region
J.Biol.Chem., 283, 2008
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5A8E
 | | thermostabilised beta1-adrenoceptor with rationally designed inverse agonist 7-methylcyanopindolol bound | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (CARBAMOYLMETHYL-CARBOXYMETHYL-AMINO)-ACETIC ACID, 4-[(2S)-3-(tert-butylamino)-2-hydroxypropoxy]-7-methyl-1H-indole-2-carbonitrile, ... | | Authors: | Sato, T, Baker, J.G, Warne, T, Brown, G.A, Congreve, M, Leslie, A.G.W, Tate, C.G. | | Deposit date: | 2015-07-15 | | Release date: | 2015-09-30 | | Last modified: | 2024-10-23 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Pharmacological Analysis and Structure Determination of 7-Methylcyanopindolol-Bound Beta1-Adrenergic Receptor.
Mol.Pharmacol., 88, 2015
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2YCW
 | | TURKEY BETA1 ADRENERGIC RECEPTOR WITH STABILISING MUTATIONS AND BOUND ANTAGONIST CARAZOLOL | | Descriptor: | (2S)-1-(9H-Carbazol-4-yloxy)-3-(isopropylamino)propan-2-ol, BETA-1 ADRENERGIC RECEPTOR, HEGA-10, ... | | Authors: | Moukhametzianov, R, Warne, T, Edwards, P.C, Serrano-Vega, M.J, Leslie, A.G.W, Tate, C.G, Schertler, G.F.X. | | Deposit date: | 2011-03-17 | | Release date: | 2011-06-01 | | Last modified: | 2024-11-20 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Two Distinct Conformations of Helix 6 Observed in Antagonist-Bound Structures of a Beta-1- Adrenergic Receptor.
Proc.Natl.Acad.Sci.USA, 108, 2011
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5C1M
 | | Crystal structure of active mu-opioid receptor bound to the agonist BU72 | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2R,3S,3aR,5aR,6R,11bR,11cS)-3a-methoxy-3,14-dimethyl-2-phenyl-2,3,3a,6,7,11c-hexahydro-1H-6,11b-(epiminoethano)-3,5a-methanonaphtho[2,1-g]indol-10-ol, CHOLESTEROL, ... | | Authors: | Huang, W.J, Manglik, A, Venkatakrishnan, A.J, Laeremans, T, Feinberg, E.N, Sanborn, A.L, Kato, H.E, Livingston, K.E, Thorsen, T.S, Kling, R, Granier, S, Gmeiner, P, Husbands, S.M, Traynor, J.R, Weis, W.I, Steyaert, J, Dror, R.O, Kobilka, B.K. | | Deposit date: | 2015-06-15 | | Release date: | 2015-08-05 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2.07 Å) | | Cite: | Structural insights into mu-opioid receptor activation.
Nature, 524, 2015
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4WW3
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4GPO
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5F8U
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8ZWF
 | | cryoEM structure of JR14a bound C3aR-BRIL-BAG2 complex | | Descriptor: | (2~{S})-5-[bis(azanyl)methylideneamino]-2-[[5-[bis(4-chlorophenyl)methyl]-3-methyl-thiophen-2-yl]carbonylamino]pentanoic acid, Beta-2 adrenergic receptor,C3a anaphylatoxin chemotactic receptor,Soluble cytochrome b562, anti-BRIL Fab HC, ... | | Authors: | Luo, P, Xu, Y, Xu, H.E. | | Deposit date: | 2024-06-13 | | Release date: | 2025-05-14 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Structural insights into the agonist activity of the nonpeptide modulator JR14a on C3aR.
Cell Discov, 11, 2025
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