The Ligandable Human Proteome

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G protein-coupled receptor, rhodopsin-like

IndexGene Name PrimaryProtein NameUniprot IDGene Name SynonymLigand NameStructurePDB Codeligand desolvationLigand StructureCompound Affinity nM
15HT1B5-hydroxytryptamine receptor 1BP28222HTR1DBermCrystal structure of the chimeric protein of 5-HT1B-BRIL in complex with ergotamine (PSI Community Target)4iar89.47no data
25HT1B5-hydroxytryptamine receptor 1BP28222HTR1DB2gmCrystal structure of the chimeric protein of 5-HT1B-BRIL in complex with dihydroergotamine (PSI Community Target)4iaq89.36no data
35HT2A5-hydroxytryptamine receptor 2AP28223HTR2zotCrystal structure of 5-HT2AR in complex with zotepine6a9495.5no data
45HT2A5-hydroxytryptamine receptor 2AP28223HTR2clrCrystal structure of 5-HT2AR in complex with risperidone6a9355.24no data
55HT2A5-hydroxytryptamine receptor 2AP28223HTR2clrCrystal structure of 5-HT2AR in complex with zotepine6a9458.58no data
65HT2B5-hydroxytryptamine receptor 2BP41595ermCrystal structure of the chimeric protein of 5-HT2B-BRIL in complex with ergotamine4ib492.68no data
75HT2B5-hydroxytryptamine receptor 2BP41595ermStructural Insights into the Extracellular Recognition of the Human Serotonin 2B Receptor by an Antibody5tud92.97no data
85HT2B5-hydroxytryptamine receptor 2BP41595ermCrystal structure of the 5-HT2B receptor solved using serial femtosecond crystallography in lipidic cubic phase.4nc391.63no data
95HT2B5-hydroxytryptamine receptor 2BP415957ldCrystal structure of the LSD-bound 5-HT2B receptor5tvn92.590.91
105HT2B5-hydroxytryptamine receptor 2BP41595h8dStructural Determinants of Activation and Biased Agonism at the 5-HT2B Receptor6dry94.2no data
115HT2C5-hydroxytryptamine receptor 2CP28335HTR1CermCrystal structure of 5-HT2C in complex with ergotamine6bqg90.98no data
125HT2C5-hydroxytryptamine receptor 2CP28335HTR1Ce2jCrystal structure of 5-HT2C in complex with ritanserin6bqh90.18no data
13AA2ARAdenosine receptor A2aP29274ADORA2zmaStructure of human A2A adenosine receptor in complex with ZM241385 obtained from SFX experiments under atmospheric pressure6jzh81.79no data
14AA2ARAdenosine receptor A2aP29274ADORA2clrA2A Adenosine receptor room-temperature structure determined by serial millisecond crystallography5nlx71.91no data
15AA2ARAdenosine receptor A2aP29274ADORA2t4eStructure of the A2A-StaR2-bRIL562-Compound 4e complex at 1.86A obtained from in meso soaking experiments (24 hour soak).5om496.38no data
16AA2ARAdenosine receptor A2aP29274ADORA2t4eStructure of the A2A-StaR2-bRIL562-Compound 4e complex at 2.1A obtained from in meso soaking experiments (1 hour soak).5om196.13no data
17AA2ARAdenosine receptor A2aP29274ADORA2t4eStructure of the A2A-StaR2-bRIL562-Compound 4e complex at 1.9A obtained from bespoke co-crystallisation experiments.5olz96.22no data
18AA2ARAdenosine receptor A2aP29274ADORA2adnThermostabilised HUMAN A2a Receptor with adenosine bound2ydo92.7430.9
19AA2ARAdenosine receptor A2aP29274ADORA26dyCrystal structure of stabilized A2A adenosine receptor A2AR-StaR2-bRIL in complex with compound 12c at 1.9A resolution5iu775.811.1
20AA2ARAdenosine receptor A2aP29274ADORA26dzCrystal structure of stabilized A2A adenosine receptor A2AR-StaR2-bRIL in complex with compound 12f at 2.0A resolution5iu878.5618.
21AA2ARAdenosine receptor A2aP29274ADORA26dxCrystal structure of stabilized A2A adenosine receptor A2AR-StaR2-bRIL in complex with compound 12b at 2.2A resolution5iua77.391.5
22AA2ARAdenosine receptor A2aP29274ADORA26dvCrystal structure of stabilized A2A adenosine receptor A2AR-StaR2-bRIL in complex with compound 12x at 2.1A resolution5iub75.830.35
23AA2ARAdenosine receptor A2aP29274ADORA29y2Structure of the A2A-StaR2-bRIL562-LUAA47070 complex at 2.0A obtained from in meso soaking experiments.5olv88.76no data
24AA2ARAdenosine receptor A2aP29274ADORA2zmaCrystal structure of human adenosine A2A receptor with an allosteric inverse-agonist antibody at 2.7 A resolution3vg976.28no data
25AA2ARAdenosine receptor A2aP29274ADORA2zmaCrystal structure of the chimeric protein of A2aAR-BRIL in complex with ZM241385 at 1.8A resolution4eiy81.12no data
26AA2ARAdenosine receptor A2aP29274ADORA2zmaCrystal structure of the chimeric protein of A2aAR-BRIL with bound iodide ions5jtb81.22no data
27AA2ARAdenosine receptor A2aP29274ADORA2zma1.9A angstrom A2a adenosine receptor structure with MR phasing using XFEL data5k2d80.34no data
28AA2ARAdenosine receptor A2aP29274ADORA2zmaThe 2.6 A Crystal Structure of a Human A2A Adenosine Receptor bound to ZM241385.3eml81.931.8
29AA2ARAdenosine receptor A2aP29274ADORA2zma2.5 angstrom A2a adenosine receptor structure with sulfur SAD phasing using XFEL data5k2a82no data
30AA2ARAdenosine receptor A2aP29274ADORA2zma1.9 angstrom A2a adenosine receptor structure with sulfur SAD phasing and phase extension using XFEL data5k2c80.07no data
31AA2ARAdenosine receptor A2aP29274ADORA2zma2.5 angstrom A2a adenosine receptor structure with MR phasing using XFEL data5k2b81.54no data
32AA2ARAdenosine receptor A2aP29274ADORA2zmaCrystal structure of A2AAR-BRIL in complex with the antagonist ZM241385 produced from Pichia pastoris6aqf81.85no data
33AA2ARAdenosine receptor A2aP29274ADORA2zmaA2A Adenosine receptor cryo structure5nm282.79no data
34AA2ARAdenosine receptor A2aP29274ADORA2zmaCrystal structure of stabilized A2A adenosine receptor A2AR-StaR2-bRIL in complex with ZM241385 at 1.7A resolution5iu483.760.53
35AA2ARAdenosine receptor A2aP29274ADORA2zmaStructure of the A2A-StaR2-bRIL562-ZM241385 complex at 1.86A obtained from in meso soaking experiments.5olg81.56no data
36AA2ARAdenosine receptor A2aP29274ADORA2zma2.35-Angstrom In situ Mylar structure of human A2A adenosine receptor at 100 K5vra80.8no data
37AA2ARAdenosine receptor A2aP29274ADORA2necThermostabilised HUMAN A2a Receptor with NECA bound2ydv94.6413.8
38AA2ARAdenosine receptor A2aP29274ADORA28jnCrystal structure of stabilized A2A adenosine receptor A2AR-StaR2-bRIL in complex with PSB36 at 2.8A resolution5n2r92.7no data
39ACM1Muscarinic acetylcholine receptor M1P11229y01Structure of the human M1 muscarinic acetylcholine receptor bound to antagonist Tiotropium5cxv53.14no data
40ACM1Muscarinic acetylcholine receptor M1P112290hkStructure of the human M1 muscarinic acetylcholine receptor bound to antagonist Tiotropium5cxv99.39no data
41ACM2Muscarinic acetylcholine receptor M2P08172qnbCrystal structure of rationally thermostabilized M2 muscarinic acetylcholine receptor bound with QNB5zk399.58no data
42ACM2Muscarinic acetylcholine receptor M2P0817282fCrystal structure of rationally thermostabilized M2 muscarinic acetylcholine receptor bound with AF-DX 3845zkb92.69no data
43ACM2Muscarinic acetylcholine receptor M2P081723c0Crystal structure of rationally thermostabilized M2 muscarinic acetylcholine receptor bound with NMS (Hg-derivative)5yc897.91no data
44ACM2Muscarinic acetylcholine receptor M2P081723c0Crystal structure of M2 muscarinic acetylcholine receptor bound with NMS5zk898.22no data
45ACM2Muscarinic acetylcholine receptor M2P081723c0Crystal structure of rationally thermostabilized M2 muscarinic acetylcholine receptor bound with NMS5zkc98.04no data
46ACM2Muscarinic acetylcholine receptor M2P08172qnbStructure of the human M2 muscarinic acetylcholine receptor bound to an antagonist3uon99.18no data
47ACM3Muscarinic acetylcholine receptor M3P203090hkM3-mT4L receptor bound to tiotropium4u1599.09no data
48ACM4Muscarinic acetylcholine receptor M4P081730hkStructure of the M4 muscarinic acetylcholine receptor (M4-mT4L) bound to tiotropium5dsg99.49no data
49ADRB2Beta-2 adrenergic receptorP07550ADRB2R B2ARk5yCrystal structure of human beta2 adrenergic receptor bound to salmeterol and Nb716mxt93.06no data
50ADRB2Beta-2 adrenergic receptorP07550ADRB2R B2AR8vsStructure of beta2 adrenoceptor bound to carazolol and an intracellular allosteric antagonist5x7d80.85no data
51ADRB2Beta-2 adrenergic receptorP07550ADRB2R B2ARtimCholesterol bound form of human beta2 adrenergic receptor.3d4s95.98no data
52ADRB2Beta-2 adrenergic receptorP07550ADRB2R B2ARjrzCrystal structure of the human beta2 adrenergic receptor in complex with the inverse agonist ICI 118,5513ny892.79no data
53ADRB2Beta-2 adrenergic receptorP07550ADRB2R B2ARjszCrystal structure of the human beta2 adrenergic receptor in complex with a novel inverse agonist3ny992.67no data
54ADRB2Beta-2 adrenergic receptorP07550ADRB2R B2ARp0gStructure of beta2 adrenoceptor bound to BI167107 and an engineered nanobody4lde95.57no data
55ADRB2Beta-2 adrenergic receptorP07550ADRB2R B2ARcauIn meso in situ serial X-ray crystallography structure of the Beta2-adrenergic receptor at 100 K5d5a90.88no data
56ADRB2Beta-2 adrenergic receptorP07550ADRB2R B2ARcauHigh resolution crystal structure of human B2-adrenergic G protein-coupled receptor.2rh190.76no data
57ADRB2Beta-2 adrenergic receptorP07550ADRB2R B2ARcauStructure of beta2 adrenoceptor bound to carazolol and an intracellular allosteric antagonist5x7d92.88no data
58AGTR1Type-1 angiotensin II receptorP30556AGTR1A AGTR1B AT2R1 AT2R1Bzd7XFEL structure of human Angiotensin Receptor4yay80.692.9
59AGTR1Type-1 angiotensin II receptorP30556AGTR1A AGTR1B AT2R1 AT2R1BolmCrystal Structure of Human Angiotensin Receptor in Complex with Inverse Agonist Olmesartan at 2.8A resolution.4zud81.256.9
60C5AR1C5a anaphylatoxin chemotactic receptor 1P21730C5AR C5R1efdCrystal structure of human C5a receptor in complex with an orthosteric antagonist PMX53 and an allosteric antagonist avacopan6c1r83.82no data
61CCR5C-C chemokine receptor type 5P51681CMKBR5mrvCrystal Structure of the CCR5 Chemokine Receptor4mbs80.82no data
62CCR5C-C chemokine receptor type 5P51681CMKBR5a4xThe Crystal structure of Human Chemokine Receptor CCR5 in complex with compound 346aky82.34no data
63CCR5C-C chemokine receptor type 5P51681CMKBR5a4rThe Crystal structure of Human Chemokine Receptor CCR5 in complex with compound 216akx79.75no data
64CCR7C-C chemokine receptor type 7P32248CMKBR7 EBI1 EVI1jlwStructure of the human CC Chemokine Receptor 7 in complex with the intracellular allosteric antagonist Cmp2105 and the insertion protein Sialidase NanA6qzh87.35no data
65CCR9C-C chemokine receptor type 9P51686GPR28clrCrystal structure of the human CC chemokine receptor type 9 (CCR9) in complex with vercirnon5lwe55.18no data
66CCR9C-C chemokine receptor type 9P51686GPR2879kCrystal structure of the human CC chemokine receptor type 9 (CCR9) in complex with vercirnon5lwe98.690.11
67CNR1Cannabinoid receptor 1P21554CNRzdgCrystal Structure of the Human Cannabinoid Receptor CB15tgz93.68no data
68CNR1Cannabinoid receptor 1P21554CNRkcaCannabinoid Receptor 1-G Protein Complex6n4b94.82no data
69CNR1Cannabinoid receptor 1P21554CNRclrCrystal structure of the human CB1 in complex with agonist AM115425xra66.02no data
70CNR1Cannabinoid receptor 1P21554CNRclrCrystal structure of the human CB1 in complex with agonist AM8415xr860.51no data
71CNR1Cannabinoid receptor 1P21554CNRclrCannabinoid Receptor 1-G Protein Complex6n4b47.72no data
72CNR1Cannabinoid receptor 1P21554CNR8d0Crystal structure of the human CB1 in complex with agonist AM8415xr896.72no data
73CNR1Cannabinoid receptor 1P21554CNR7dyHigh-resolution crystal structure of the human CB1 cannabinoid receptor5u0995.94no data
74CNR2Cannabinoid receptor 2P34972CB2A CB2B9juCrystal structure of human G protein coupled receptor5zty96.47no data
75CXCR4C-X-C chemokine receptor type 4P61073itdThe 2.5 A structure of the CXCR4 chemokine receptor in complex with small molecule antagonist IT1t3odu83.787.3
76DRD3D(3) dopamine receptorP35462etqStructure of the human dopamine D3 receptor in complex with eticlopride3pbl95.41no data
77DRD4D(4) dopamine receptorP21917aqdStructure of the human D4 Dopamine receptor in complex with Nemonapride5wiu94.76no data
78EDNRBEndothelin receptor type BP24530ETRBd2uHuman endothelin receptor type-B in complex with inverse agonist IRL25006k1q89.5no data
79LPAR1Lysophosphatidic acid receptor 1Q92633EDG2 LPA1on9Crystal Structure of Human Lysophosphatidic Acid Receptor 1 in complex with ONO-99105394z3596.82no data
80LPAR1Lysophosphatidic acid receptor 1Q92633EDG2 LPA1on7Crystal Structure of Human Lysophosphatidic Acid Receptor 1 in complex with ONO97803074z3496.17no data
81LPAR1Lysophosphatidic acid receptor 1Q92633EDG2 LPA1on3Crystal Structure of Human Lysophosphatidic Acid Receptor 1 in complex with ONO-30805734z3693.32no data
82MTR1AMelatonin receptor type 1AP48039jeyXFEL crystal structure of human melatonin receptor MT1 in complex with 2-phenylmelatonin6me397.5no data
83MTR1AMelatonin receptor type 1AP48039jevXFEL crystal structure of human melatonin receptor MT1 in complex with ramelteon6me296.51no data
84MTR1BMelatonin receptor type 1BP49286jeyXFEL crystal structure of human melatonin receptor MT2 in complex with 2-phenylmelatonin6me696.97no data
85NK1RSubstance-P receptorP25103NK1R TAC1RgbqCrystal structure of the human NK1 substance P receptor6j2090.8no data
86NK1RSubstance-P receptorP25103NK1R TAC1RgbqCrystal structure of the Neurokinin 1 receptor in complex with the small molecule antagonist Aprepitant6hlo90.38no data
87NK1RSubstance-P receptorP25103NK1R TAC1RgawCrystal structure of the Neurokinin 1 receptor in complex with the small molecule antagonist Netupitant6hlp80.09no data
88NPY1RNeuropeptide Y receptor type 1P25929NPYR NPYY19afThe Crystal Structure of Human Neuropeptide Y Y1 Receptor with BMS-1938855zbh87.07no data
89OPRKKappa-type opioid receptorP41145OPRKjdcStructure of the human kappa opioid receptor in complex with JDTic4djh90.430.32
90OPRMMu-type opioid receptorP35372MOR1clrCrystal structure of active mu-opioid receptor bound to the agonist BU725c1m66.64no data
91OPRMMu-type opioid receptorP35372MOR1clrCrystal structure of the mu-opioid receptor bound to a morphinan antagonist4dkl53.51no data
92OPRXNociceptin receptorP41146OOR ORL1dgvThe crystal structure of nociceptin/orphanin FQ peptide receptor (NOP) in complex with C-35 (PSI Community Target)5dhg85.750.72
93OX1ROrexin receptor type 1O436134otStructures of the human OX1 orexin receptor bound to selective and dual antagonists4zjc87.751.1
94P2RY1P2Y purinoceptor 1P47900clrThe human P2Y1 receptor in complex with BPTU4xnv52.23no data
95P2RY1P2Y purinoceptor 1P47900burThe human P2Y1 receptor in complex with BPTU4xnv70.54161.
96P2Y12P2Y purinoceptor 12Q9H244HORK3clrCrystal structure of P2Y12 receptor in complex with 2MeSADP4pxz61.84no data
97P2Y12P2Y purinoceptor 12Q9H244HORK3clrStructure of the human P2Y12 receptor in complex with an antithrombotic drug4ntj41.59no data
98P2Y12P2Y purinoceptor 12Q9H244HORK3azjStructure of the human P2Y12 receptor in complex with an antithrombotic drug4ntj85.8943.9
99PAR1Proteinase-activated receptor 1P25116CF2R PAR1 TRvpxCrystal structure of human protease-activated receptor 1 (PAR1) bound with antagonist vorapaxar at 2.2 angstrom3vw796.068.
100PAR2Proteinase-activated receptor 2P55085GPR11 PAR28tzCrystal structure of a thermostabilised human protease-activated receptor-2 (PAR2) in complex with AZ8838 at 2.8 angstrom resolution5ndd99.39344.
101PE2R3Prostaglandin E2 receptor EP3 subtypeP43115p2eCrystal structure of the human prostaglandin E receptor EP3 bound to prostaglandin E26ak399.52no data
102PE2R3Prostaglandin E2 receptor EP3 subtypeP43115j9pCrystal structure of EP3 receptor bound to misoprostol-FA6m9t98.38no data
103PTAFRPlatelet-activating factor receptorP25105PAFR9erCrystal structure of the human platelet-activating factor receptor in complex with SR 274175zkp94.61no data
104PTAFRPlatelet-activating factor receptorP25105PAFR9euCrystal structure of the human platelet-activating factor receptor in complex with ABT-4915zkq96.46no data
105TA2RThromboxane A2 receptorP21731clrCrystal structure of the human thromboxane A2 receptor bound to daltroban6iiv35.87no data
106TA2RThromboxane A2 receptorP21731clrCrystal structure of the human thromboxane A2 receptor bound to ramatroban6iiu42.78no data
107TA2RThromboxane A2 receptorP21731a90Crystal structure of the human thromboxane A2 receptor bound to daltroban6iiv95.03no data
108TA2RThromboxane A2 receptorP21731a8xCrystal structure of the human thromboxane A2 receptor bound to ramatroban6iiu98.06no data