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RECEPTOR
STRUCTURE
SIGNAL PROTEIN
AUXILIARY PROTEIN
STRUCTURE LIGAND
ENDOGENOUS LIGAND
SODIUM ION SITE
REFERENCE
ANNOTATED
UniProt
 IUPHAR Receptor family Cl. Species Method
PDB
 Refined
structure
 Resolution Preferred
chain		 State
 Degree
active (%)
 % of Seq Family Subtype Note % of Seq Fusion Antibodies Name Type Function Name Type D2x50
S3x39		 Sodium in
structure		 Authors Reference PDB Date
OPSD Rhodopsin Opsins A Bovine X-ray 1F88 1F88_refined 2.8 A Inactive 22 97 - - - - - - Retinal (11-cis) PubChem
small-molecule Inverse agonist - - No No Palczewski K, Kumasaka T, Hori T, Behnke CA, Motoshima H, Fox BA, Le Trong I, Teller DC, Okada T, Stenkamp RE, Yamamoto M, Miyano M 10.1126/SCIENCE.289.5480.739 2000-08-04 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 1HZX - 2.8 A Inactive 22 98 - - - - - - Retinal (11-cis) PubChem
small-molecule Inverse agonist - - No No Teller DC, Okada T, Behnke CA, Palczewski K, Stenkamp RE 10.1021/BI0155091 2001-07-04 No
OPSD Rhodopsin Opsins A Bovine X-ray 1L9H - 2.6 A Inactive 22 98 - - - - - - Retinal (11-cis) PubChem
small-molecule Inverse agonist - - No No Okada T, Fujiyoshi Y, Silow M, Navarro J, Landau EM, Shichida Y 10.1073/PNAS.082666399 2002-05-15 No
OPSD Rhodopsin Opsins A Bovine X-ray 1GZM 1GZM_refined 2.7 A Inactive 22 94 - - - - - - Retinal (11-cis) PubChem
small-molecule Inverse agonist - - No No - 10.1016/J.JMB.2004.08.090 2003-11-20 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 1U19 1U19_refined 2.2 A Inactive 22 100 - - - - - - Retinal (11-cis) PubChem
small-molecule Inverse agonist - - No No Okada T, Sugihara M, Bondar AN, Elstner M, Entel P, Buss V 10.1016/J.JMB.2004.07.044 2004-10-12 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 2HPY - 2.8 B Inactive 22 100 - - - - - - Retinal (all-trans) PubChem
small-molecule Agonist - - No No Nakamichi H, Okada T 10.1073/PNAS.0601765103 2006-08-22 No
OPSD Rhodopsin Opsins A Bovine X-ray 2G87 - 2.6 A Inactive 22 100 - - - - - - Retinal (all-trans) PubChem
small-molecule Agonist - - No No Nakamichi H, Okada T 10.1002/ANIE.200600595 2006-09-02 No
OPSD Rhodopsin Opsins A Bovine X-ray 2I35 - 3.8 A Inactive 22 94 - - - - - - Retinal (11-cis) PubChem
small-molecule Inverse agonist - - No No Salom D, Lodowski DT, Stenkamp RE, Le Trong I, Golczak M, Jastrzebska B, Harris T, Ballesteros JA, Palczewski K 10.1073/PNAS.0608022103 2006-10-17 No
OPSD Rhodopsin Opsins A Bovine X-ray 2I36 - 4.1 A Inactive 22 94 - - - - - - Apo (no ligand)
none Apo (no ligand) - - No No Salom D, Lodowski DT, Stenkamp RE, Le Trong I, Golczak M, Jastrzebska B, Harris T, Ballesteros JA, Palczewski K 10.1073/PNAS.0608022103 2006-10-17 No
OPSD Rhodopsin Opsins A Bovine X-ray 2I37 - 4.2 A Inactive 22 91 - - - - - - Apo (no ligand)
none Apo (no ligand) - - No No Salom D, Lodowski DT, Stenkamp RE, Le Trong I, Golczak M, Jastrzebska B, Harris T, Ballesteros JA, Palczewski K 10.1073/PNAS.0608022103 2006-10-17 No
OPSD Rhodopsin Opsins A Bovine X-ray 2J4Y - 3.4 B Inactive 22 94 - - - - - - Retinal (11-cis) PubChem
small-molecule Inverse agonist - - No No Standfuss J, Xie G, Edwards PC, Burghammer M, Oprian DD, Schertler GF 10.1016/J.JMB.2007.03.007 2007-09-25 No
OPSD Rhodopsin Opsins A Bovine X-ray 2PED - 3.0 B Inactive 22 100 - - - - - - Retinal (9-cis) PubChem
small-molecule Inverse agonist - - No No Nakamichi H, Buss V, Okada T 10.1529/BIOPHYSJ.107.108225 2007-10-30 No
ADRB2 β2 Adrenoceptors A Human X-ray 2RH1 2RH1_refined 2.4 A Inactive 0 68 - - - - T4-Lysozyme - Carazolol PubChem
small-molecule Inverse agonist noradrenaline, L-NOREPINEPHRINE, Zn2+, (-)-adrenaline, (-)-noradrenaline small-molecule Yes No Cherezov V, Rosenbaum DM, Hanson MA, Rasmussen SG, Thian FS, Kobilka TS, Choi HJ, Kuhn P, Weis WI, Kobilka BK, Stevens RC 10.1126/SCIENCE.1150577 2007-10-30 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 2R4R - 3.4 A Inactive 1 52 - - - - - Antibody - - - noradrenaline, L-NOREPINEPHRINE, Zn2+, (-)-adrenaline, (-)-noradrenaline small-molecule Yes No Rasmussen SG, Choi HJ, Rosenbaum DM, Kobilka TS, Thian FS, Edwards PC, Burghammer M, Ratnala VR, Sanishvili R, Fischetti RF, Schertler GF, Weis WI, Kobilka BK 10.1038/NATURE06325 2007-11-06 No
ADRB2 β2 Adrenoceptors A Human X-ray 2R4S - 3.4 A Inactive 1 52 - - - - - Antibody - - - noradrenaline, L-NOREPINEPHRINE, Zn2+, (-)-adrenaline, (-)-noradrenaline small-molecule Yes No Rasmussen SG, Choi HJ, Rosenbaum DM, Kobilka TS, Thian FS, Edwards PC, Burghammer M, Ratnala VR, Sanishvili R, Fischetti RF, Schertler GF, Weis WI, Kobilka BK 10.1038/NATURE06325 2007-11-06 No
OPSD Rhodopsin Opsins A Japanese flying squid X-ray 2ZIY - 3.7 A Inactive 13 83 - - - - - - Retinal (11-cis) PubChem
small-molecule Inverse agonist - - Yes No Shimamura T, Hiraki K, Takahashi N, Hori T, Ago H, Masuda K, Takio K, Ishiguro M, Miyano M 10.1074/JBC.C800040200 2008-05-06 No
OPSD Rhodopsin Opsins A Japanese flying squid X-ray 2Z73 2Z73_refined 2.5 A Inactive 13 78 - - - - - - Retinal (11-cis) PubChem
small-molecule Inverse agonist - - Yes No Murakami M, Kouyama T 10.1038/NATURE06925 2008-05-13 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 3D4S 3D4S_refined 2.8 A Inactive 0 67 - - - - T4-Lysozyme - timolol PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank Drug Central
small-molecule Inverse agonist noradrenaline, L-NOREPINEPHRINE, Zn2+, (-)-adrenaline, (-)-noradrenaline small-molecule Yes No Hanson MA, Cherezov V, Griffith MT, Roth CB, Jaakola VP, Chien EY, Velasquez J, Kuhn P, Stevens RC 10.1016/J.STR.2008.05.001 2008-06-17 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 2VT4 - 2.7 B Inactive 0 57 - - - - - - (S)-Cyanopindolol PubChem
small-molecule Antagonist - - Yes No Warne T, Serrano-Vega MJ, Baker JG, Moukhametzianov R, Edwards PC, Henderson R, Leslie AG, Tate CG, Schertler GF 10.1038/NATURE07101 2008-06-24 No
OPSD Rhodopsin Opsins A Bovine X-ray 3CAP - 2.9 A Active 99 94 - - - - - - Apo (no ligand)
none Apo (no ligand) - - No No Park JH, Scheerer P, Hofmann KP, Choe HW, Ernst OP 10.1038/NATURE07063 2008-06-24 No
OPSD Rhodopsin Opsins A Bovine X-ray 3C9L 3C9L_refined 2.7 A Inactive 22 94 - - - - - - Retinal (11-cis) PubChem
small-molecule Inverse agonist - - No No Stenkamp RE 10.1107/S0907444908017162 2008-08-05 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 3C9M 3C9M_refined 3.4 A Inactive 22 94 - - - - - - Retinal (11-cis) PubChem
small-molecule Inverse agonist - - No No Stenkamp RE 10.1107/S0907444908017162 2008-08-05 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 3KJ6 - 3.4 A Inactive 1 54 - - - - - Antibody - - - noradrenaline, L-NOREPINEPHRINE, Zn2+, (-)-adrenaline, (-)-noradrenaline small-molecule Yes No Bokoch MP, Zou Y, Rasmussen SG, Liu CW, Nygaard R, Rosenbaum DM, Fung JJ, Choi HJ, Thian FS, Kobilka TS, Puglisi JD, Weis WI, Pardo L, Prosser RS, Mueller L, Kobilka BK 10.1038/NATURE08650 2010-02-16 No
CXCR4 CXCR4 Chemokine A Human X-ray 3ODU 3ODU_refined 2.5 A Inactive 5 83 - - - - T4-Lysozyme - isothiourea-1t PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Antagonist CXCL12β, CXCL12φ, CXCL12, CXCL12γ, CXCL12δ, CXCL12ε, CXCL12α peptide Yes No Wu B, Chien EY, Mol CD, Fenalti G, Liu W, Katritch V, Abagyan R, Brooun A, Wells P, Bi FC, Hamel DJ, Kuhn P, Handel TM, Cherezov V, Stevens RC 10.1126/SCIENCE.1194396 2010-10-27 Yes
DRD3 D3 Dopamine A Human X-ray 3PBL 3PBL_refined 2.9 A Inactive 1 68 - - - - T4-Lysozyme - eticlopride PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank
small-molecule Antagonist dopamine small-molecule Yes No Chien EY, Liu W, Zhao Q, Katritch V, Han GW, Hanson MA, Shi L, Newman AH, Javitch JA, Cherezov V, Stevens RC 10.1126/SCIENCE.1197410 2010-11-03 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 3PDS 3PDS_refined 3.5 A Inactive 0 68 - - - - T4-Lysozyme - FAUC50 PubChem
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, Zn2+, (-)-adrenaline, (-)-noradrenaline small-molecule Yes No Rosenbaum DM, Zhang C, Lyons JA, Holl R, Aragao D, Arlow DH, Rasmussen SG, Choi HJ, Devree BT, Sunahara RK, Chae PS, Gellman SH, Dror RO, Shaw DE, Weis WI, Caffrey M, Gmeiner P, Kobilka BK 10.1038/NATURE09665 2011-01-12 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 3PXO - 3.0 A Active 99 94 - - - - - - Retinal (all-trans) PubChem
small-molecule Agonist - - No No Choe HW, Kim YJ, Park JH, Morizumi T, Pai EF, Krauss N, Hofmann KP, Scheerer P, Ernst OP 10.1038/NATURE09789 2011-03-09 No
AA2AR A2A Adenosine A Human X-ray 2YDO 2YDO_refined 3.0 A Active 73 73 - - - - - - adenosine PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank Drug Central
small-molecule Agonist adenosine small-molecule Yes No Lebon G, Warne T, Edwards PC, Bennett K, Langmead CJ, Leslie AG, Tate CG 10.1038/NATURE10136 2011-05-18 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 2YCW 2YCW_refined 3.0 A Inactive 0 61 - - - - - - Carazolol PubChem
small-molecule Antagonist - - Yes No Moukhametzianov R, Warne T, Edwards PC, Serrano-Vega MJ, Leslie AG, Tate CG, Schertler GF 10.1073/PNAS.1100185108 2011-06-01 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 3SN6 3SN6_refined 3.2 R Active 100 69 Gs αs - 89 T4-Lysozyme Antibody BI-167107 PubChem
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, Zn2+, (-)-adrenaline, (-)-noradrenaline small-molecule Yes No Rasmussen SG, DeVree BT, Zou Y, Kruse AC, Chung KY, Kobilka TS, Thian FS, Chae PS, Pardon E, Calinski D, Mathiesen JM, Shah ST, Lyons JA, Caffrey M, Gellman SH, Steyaert J, Skiniotis G, Weis WI, Sunahara RK, Kobilka BK 10.1038/NATURE10361 2011-07-20 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 4A4M 4A4M_refined 3.3 A Active 100 94 Gi/o αt1 Only H5 3 - - Retinal (all-trans) PubChem
small-molecule Agonist - - No No Deupi X, Edwards P, Singhal A, Nickle B, Oprian D, Schertler G, Standfuss J 10.1073/PNAS.1114089108 2012-01-25 Yes
S1PR1 S1P1 Lysophospholipid (S1P) A Human X-ray 3V2W - 3.4 A Inactive 1 68 - - - - T4-Lysozyme - W146 PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Antagonist dihydrosphingosine 1-phosphate, sphingosine 1-phosphate, sphingosylphosphorylcholine small-molecule Yes No Hanson MA, Roth CB, Jo E, Griffith MT, Scott FL, Reinhart G, Desale H, Clemons B, Cahalan SM, Schuerer SC, Sanna MG, Han GW, Kuhn P, Rosen H, Stevens RC 10.1126/SCIENCE.1215904 2012-02-15 No
AA2AR A2A Adenosine A Human X-ray 3UZC 3UZC_refined 3.3 A Inactive 1 71 - - - - - - CHEMBL2024114 ChEMBL_compound_ids PubChem
small-molecule Antagonist adenosine small-molecule Yes No Congreve M, Andrews SP, Dore AS, Hollenstein K, Hurrell E, Langmead CJ, Mason JS, Ng IW, Tehan B, Zhukov A, Weir M, Marshall FH 10.1021/JM201376W 2012-03-21 Yes
OPRX NOP Opioid A Human X-ray 4EA3 4EA3_refined 3.0 A Inactive 5 75 - - - - BRIL - compound 24 [PMID: 16451050] PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Antagonist nociceptin/orphanin FQ peptide Yes No Thompson AA, Liu W, Chun E, Katritch V, Wu H, Vardy E, Huang XP, Trapella C, Guerrini R, Calo G, Roth BL, Cherezov V, Stevens RC 10.1038/NATURE11085 2012-04-25 Yes
NTR1 NTS1 Neurotensin A Rat X-ray 4GRV 4GRV_refined 2.8 A Active 83 69 - - - - T4-Lysozyme - JMV431 Guide To Pharmacology ChEMBL_compound_ids PubChem
peptide Agonist neurotensin, neuromedin N peptide Yes No White JF, Noinaj N, Shibata Y, Love J, Kloss B, Xu F, Gvozdenovic-Jeremic J, Shah P, Shiloach J, Tate CG, Grisshammer R 10.1038/NATURE11558 2012-10-17 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 4GPO 4GPO_refined 3.5 B Inactive 0 58 - - - - - - - - - - - Yes No Huang J, Chen S, Zhang JJ, Huang XY 10.1038/NSMB.2504 2013-02-27 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 3ZPQ 3ZPQ_refined 2.8 B Inactive 0 62 - - - - - - CHEMBL200234 ChEMBL_compound_ids PubChem
small-molecule Antagonist - - Yes Yes Christopher JA, Brown J, Dore AS, Errey JC, Koglin M, Marshall FH, Myszka DG, Rich RL, Tate CG, Tehan B, Warne T, Congreve M 10.1021/JM400140Q 2013-04-03 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 4BEY 4BEY_refined 2.9 A Active 100 94 Gi/o αt1 Only H5 3 - - Apo (no ligand)
none Apo (no ligand) - - No No Singhal A, Ostermaier MK, Vishnivetskiy SA, Panneels V, Homan KT, Tesmer JJ, Veprintsev D, Deupi X, Gurevich VV, Schertler GF, Standfuss J 10.1038/EMBOR.2013.44 2013-05-08 Yes
CCR5 CCR5 Chemokine A Human X-ray 4MBS 4MBS_refined 2.7 A Inactive 12 83 - - - - Rubredoxin - maraviroc PubChem Guide To Pharmacology DrugBank ChEMBL_compound_ids Guide To Pharmacology
small-molecule Antagonist CCL2, CCL4, CCL11, CCL7, CCL8, CCL5, CCL14, CCL16, CCL3, CCL13 peptide No No Tan Q, Zhu Y, Li J, Chen Z, Han GW, Kufareva I, Li T, Ma L, Fenalti G, Li J, Zhang W, Xie X, Yang H, Jiang H, Cherezov V, Liu H, Stevens RC, Zhao Q, Wu B 10.1126/SCIENCE.1241475 2013-09-11 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 4J4Q 4J4Q_refined 2.7 A Active 100 94 Gi/o αt1 Only H5 3 - - B-Octylglucoside PubChem
small-molecule unknown - - No No Park JH, Morizumi T, Li Y, Hong JE, Pai EF, Hofmann KP, Choe HW, Ernst OP 10.1002/ANIE.201302374 2013-10-30 Yes
OPRD δ Opioid A Human X-ray 4N6H 4N6H_refined 1.8 A Inactive 5 81 - - - - BRIL - naltrindole PubChem Guide To Pharmacology ChEMBL_compound_ids Guide To Pharmacology
small-molecule Antagonist [Leu]enkephalin, dynorphin A, dynorphin A-(1-8), dynorphin A-(1-13), endomorphin-1, dynorphin B, β-endorphin peptide Yes Yes Fenalti G, Giguere PM, Katritch V, Huang XP, Thompson AA, Cherezov V, Roth BL, Stevens RC 10.1038/NATURE12944 2013-12-25 Yes
NTR1 NTS1 Neurotensin A Rat X-ray 4BV0 - 3.1 A Inactive 2 70 - - - - - - neurotensin PubChem Guide To Pharmacology ChEMBL_compound_ids Guide To Pharmacology Guide To Pharmacology
peptide Agonist neurotensin, neuromedin N peptide Yes No Egloff P, Hillenbrand M, Klenk C, Batyuk A, Heine P, Balada S, Schlinkmann KM, Scott DJ, Schutz M, Pluckthun A 10.1073/PNAS.1317903111 2014-01-29 No
P2Y12 P2Y12 P2Y A Human X-ray 4NTJ 4NTJ_refined 2.6 A Intermediate 36 78 - - - - BRIL - AZD1283 PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Antagonist ATP, ADP small-molecule Yes No Zhang K, Zhang J, Gao ZG, Zhang D, Zhu L, Han GW, Moss SM, Paoletta S, Kiselev E, Lu W, Fenalti G, Zhang W, Muller CE, Yang H, Jiang H, Cherezov V, Katritch V, Jacobson KA, Stevens RC, Wu B, Zhao Q 10.1038/NATURE13083 2014-03-26 Yes
FFAR1 FFA1 Free fatty acid A Human X-ray 4PHU 4PHU_refined 2.3 A Intermediate 46 90 - - - - T4-Lysozyme - fasiglifam PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank
small-molecule Agonist oleic acid, α-linolenic acid, docosahexaenoic acid, myristic acid small-molecule No No Srivastava A, Yano J, Hirozane Y, Kefala G, Gruswitz F, Snell G, Lane W, Ivetac A, Aertgeerts K, Nguyen J, Jennings A, Okada K 10.1038/NATURE13494 2014-07-16 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 4PXF 4PXF_refined 2.8 A Active 100 93 Visual S-arrestin Fragment 2 - - B-Octylglucoside PubChem
small-molecule unknown - - No No Szczepek M, Beyriere F, Hofmann KP, Elgeti M, Kazmin R, Rose A, Bartl FJ, von Stetten D, Heck M, Sommer ME, Hildebrand PW, Scheerer P 10.1038/NCOMMS5801 2014-09-17 Yes
ACM3 M3 Acetylcholine (muscarinic) A Rat X-ray 4U16 4U16_refined 3.7 B Inactive 3 47 - - - - T4-Lysozyme - N-methyl scopolamine PubChem Guide To Pharmacology DrugBank Guide To Pharmacology
small-molecule Antagonist acetylcholine small-molecule Yes No Thorsen TS, Matt R, Weis WI, Kobilka BK 10.1016/J.STR.2014.08.022 2014-11-26 Yes
CXCR4 CXCR4 Chemokine A Human X-ray 4RWS 4RWS_refined 3.1 A Inactive 5 78 - - - - T4-Lysozyme - viral macrophage inflammatory protein-II PubChem Guide To Pharmacology
peptide Antagonist CXCL12β, CXCL12φ, CXCL12, CXCL12γ, CXCL12δ, CXCL12ε, CXCL12α peptide Yes No Qin L, Kufareva I, Holden LG, Wang C, Zheng Y, Zhao C, Fenalti G, Wu H, Han GW, Cherezov V, Abagyan R, Stevens RC, Handel TM 10.1126/SCIENCE.1261064 2015-02-11 Yes
AGTR1 AT1 Angiotensin A Human X-ray 4YAY 4YAY_refined 2.9 A Inactive 5 79 - - - - BRIL - ZD-7155 PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Antagonist angiotensin III, angiotensin IV, angiotensin II, angiotensin A peptide Yes No Zhang H, Unal H, Gati C, Han GW, Liu W, Zatsepin NA, James D, Wang D, Nelson G, Weierstall U, Sawaya MR, Xu Q, Messerschmidt M, Williams GJ, Boutet S, Yefanov OM, White TA, Wang C, Ishchenko A, Tirupula KC, Desnoyer R, Coe J, Conrad CE, Fromme P, Stevens RC, Katritch V, Karnik SS, Cherezov V 10.1016/J.CELL.2015.04.011 2015-04-22 Yes
OPSD Rhodopsin Opsins A Japanese flying squid X-ray 4WW3 4WW3_refined 2.8 A Inactive 13 78 - - - - - - Retinal (all-trans) PubChem
small-molecule Agonist - - Yes No Murakami M, Kouyama T 10.1371/JOURNAL.PONE.0126970 2015-06-17 Yes
OPRM μ Opioid A Mouse X-ray 5C1M 5C1M_refined 2.1 A Active 100 74 - - - - - Antibody BU72 Guide To Pharmacology PubChem
small-molecule Agonist - - Yes No Huang W, Manglik A, Venkatakrishnan AJ, Laeremans T, Feinberg EN, Sanborn AL, Kato HE, Livingston KE, Thorsen TS, Kling RC, Granier S, Gmeiner P, Husbands SM, Traynor JR, Weis WI, Steyaert J, Dror RO, Kobilka BK 10.1038/NATURE14886 2015-08-05 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 5A8E 5A8E_refined 2.4 A Inactive 0 59 - - - - - - 7-methylcyanopindolol PubChem
small-molecule Inverse agonist - - Yes Yes Sato T, Baker J, Warne T, Brown GA, Leslie AG, Congreve M, Tate CG 10.1124/MOL.115.101030 2015-09-30 Yes
OPRX NOP Opioid A Human X-ray 5DHG 5DHG_refined 3.0 A Inactive 5 76 - - - - BRIL - CHEMBL1783826 ChEMBL_compound_ids PubChem
small-molecule Antagonist nociceptin/orphanin FQ peptide Yes No Miller RL, Thompson AA, Trapella C, Guerrini R, Malfacini D, Patel N, Han GW, Cherezov V, Calo G, Katritch V, Stevens RC 10.1016/J.STR.2015.07.024 2015-10-21 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 5D5A 5D5A_refined 2.5 A Inactive 0 68 - - - - T4-Lysozyme - Carazolol PubChem
small-molecule Inverse agonist noradrenaline, L-NOREPINEPHRINE, Zn2+, (-)-adrenaline, (-)-noradrenaline small-molecule Yes No Huang CY, Olieric V, Ma P, Howe N, Vogeley L, Liu X, Warshamanage R, Weinert T, Panepucci E, Kobilka B, Diederichs K, Wang M, Caffrey M 10.1107/S2059798315021683 2016-01-13 Yes
ACM4 M4 Acetylcholine (muscarinic) A Human X-ray 5DSG 5DSG_refined 2.6 B Inactive 3 60 - - - - T4-Lysozyme - tiotropium PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank Guide To Pharmacology
small-molecule Antagonist acetylcholine small-molecule Yes No - - 2016-03-16 Yes
AA2AR A2A Adenosine A Human X-ray 5IU4 5IU4_refined 1.7 A Inactive 1 71 - - - - BRIL - ZM-241385 PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank
small-molecule Antagonist adenosine small-molecule Yes Yes Segala E, Guo D, Cheng RK, Bortolato A, Deflorian F, Dore AS, Errey JC, Heitman LH, IJzerman AP, Marshall FH, Cooke RM 10.1021/acs.jmedchem.6b00653 2016-06-29 Yes
AA2AR A2A Adenosine A Human X-ray 5IUA 5IUA_refined 2.2 A Inactive 1 72 - - - - BRIL - 2-(Furan-2-yl)-5-N-[3-(4-phenylpiperazin-1-yl)propyl]-1H-[1,2,4]triazolo[1,5-a][1,3,5]triazin-8-ium-5,7-diamine PubChem
small-molecule Antagonist adenosine small-molecule Yes Yes Segala E, Guo D, Cheng RK, Bortolato A, Deflorian F, Dore AS, Errey JC, Heitman LH, IJzerman AP, Marshall FH, Cooke RM 10.1021/acs.jmedchem.6b00653 2016-06-29 Yes
SMO SMO Frizzled F Human X-ray 5L7I 5L7I_refined 3.3 B Inactive 4 59 - - - - BRIL - vismodegib PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank Drug Central
small-molecule Antagonist - - No No Byrne EFX, Sircar R, Miller PS, Hedger G, Luchetti G, Nachtergaele S, Tully MD, Mydock-McGrane L, Covey DF, Rambo RP, Sansom MSP, Newstead S, Rohatgi R, Siebold C 10.1038/NATURE18934 2016-07-20 Yes
EDNRB ETB Endothelin A Human X-ray 5GLH 5GLH_refined 2.8 A Inactive 13 66 - - - - T4-Lysozyme - ENDOTHELIN ChEMBL_compound_ids PubChem
protein Agonist endothelin-2, endothelin-3, endothelin-1 peptide Yes No Shihoya W, Nishizawa T, Okuta A, Tani K, Dohmae N, Fujiyoshi Y, Nureki O, Doi T 10.1038/nature19319 2016-09-07 Yes
AA2AR A2A Adenosine A Human X-ray 5K2D 5K2D_refined 1.9 A Inactive 1 72 - - - - BRIL - ZM-241385 PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank
small-molecule Antagonist adenosine small-molecule Yes Yes Batyuk A, Galli L, Ishchenko A, Han GW, Gati C, Popov PA, Lee MY, Stauch B, White TA, Barty A, Aquila A, Hunter MS, Liang M, Boutet S, Pu M, Liu ZJ, Nelson G, James D, Li C, Zhao Y, Spence JC, Liu W, Fromme P, Katritch V, Weierstall U, Stevens RC, Cherezov V 10.1126/SCIADV.1600292 2016-09-21 Yes
CCR2 CCR2 Chemokine A Human X-ray 5T1A 5T1A_refined 2.8 A Inactive 13 76 - - - - T4-Lysozyme - CCR2-RA-[R] PubChem Guide To Pharmacology ChEMBL_compound_ids
BMS-681 PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule
small-molecule		 Allosteric antagonist
Antagonist		 CCL11, CCL2, CCL7, CCL8, CCL16, CCL24, CCL13, CCL26 peptide No No Zheng Y, Qin L, Zacarias NV, de Vries H, Han GW, Gustavsson M, Dabros M, Zhao C, Cherney RJ, Carter P, Stamos D, Abagyan R, Cherezov V, Stevens RC, IJzerman AP, Heitman LH, Tebben A, Kufareva I, Handel TM 10.1038/NATURE20605 2016-12-14 Yes
AA1R A1 Adenosine A Human X-ray 5UEN 5UEN_refined 3.2 B Inactive 1 91 - - - - BRIL - DU172 PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Antagonist adenosine small-molecule Yes No Glukhova A, Thal DM, Nguyen AT, Vecchio EA, Jorg M, Scammells PJ, May LT, Sexton PM, Christopoulos A 10.1016/j.cell.2017.01.042 2017-03-01 Yes
AGTR2 AT2 Angiotensin A Human X-ray 5UNH 5UNH_refined 2.9 B Active 99 75 - - - - BRIL - compound 2 [PMID: 28379944] PubChem Guide To Pharmacology
small-molecule Antagonist angiotensin III, angiotensin II, angiotensin-(1-7) peptide Yes No Zhang H, Han GW, Batyuk A, Ishchenko A, White KL, Patel N, Sadybekov A, Zamlynny B, Rudd MT, Hollenstein K, Tolstikova A, White TA, Hunter MS, Weierstall U, Liu W, Babaoglu K, Moore EL, Katz RD, Shipman JM, Garcia-Calvo M, Sharma S, Sheth P, Soisson SM, Stevens RC, Katritch V, Cherezov V 10.1038/NATURE22035 2017-04-05 Yes
GLP1R GLP-1 Glucagon B1 Human X-ray 5VEX 5VEX_refined 3.0 B Inactive 0 57 - - - - T4-Lysozyme - NNC0640 PubChem Guide To Pharmacology
small-molecule NAM glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon peptide No No Song G, Yang D, Wang Y, de Graaf C, Zhou Q, Jiang S, Liu K, Cai X, Dai A, Lin G, Liu D, Wu F, Wu Y, Zhao S, Ye L, Han GW, Lau J, Wu B, Hanson MA, Liu ZJ, Wang MW, Stevens RC 10.1038/NATURE22378 2017-05-17 Yes
G1SGD4 GLP-1 Glucagon B1 Rabbit cryo-EM 5VAI 5VAI_refined 4.1 R Active 100 84 Gs αs - 59 - - GLP-1 PubChem PubChem ChEMBL_compound_ids
small-molecule Agonist - - No No Zhang Y, Sun B, Feng D, Hu H, Chu M, Qu Q, Tarrasch JT, Li S, Sun Kobilka T, Kobilka BK, Skiniotis G 10.1038/NATURE22394 2017-05-24 Yes
APJ apelin Apelin A Human X-ray 5VBL 5VBL_refined 2.6 B Inactive 5 79 - - - - Rubredoxin - AMG3054 Guide To Pharmacology
peptide Agonist apelin receptor early endogenous ligand, Elabela/Toddler-11, Elabela/Toddler-21, apelin-17, [Pyr1]apelin-13, apelin-13, apelin-36, Elabela/Toddler-32 peptide Yes No Ma Y, Yue Y, Ma Y, Zhang Q, Zhou Q, Song Y, Shen Y, Li X, Ma X, Li C, Hanson MA, Han GW, Sickmier EA, Swaminath G, Zhao S, Stevens RC, Hu LA, Zhong W, Zhang M, Xu F 10.1016/J.STR.2017.04.008 2017-05-31 Yes
CCR5 CCR5 Chemokine A Human X-ray 5UIW 5UIW_refined 2.2 A Inactive 12 85 - - - - Rubredoxin - 5P7-CCL5
protein Antagonist CCL2, CCL4, CCL11, CCL7, CCL8, CCL5, CCL14, CCL16, CCL3, CCL13 peptide No No Zheng Y, Han GW, Abagyan R, Wu B, Stevens RC, Cherezov V, Kufareva I, Handel TM 10.1016/J.IMMUNI.2017.05.002 2017-06-28 Yes
5HT2B 5-HT2B 5-Hydroxytryptamine A Human X-ray 5TUD 5TUD_refined 3.0 D Active 92 58 - - - - BRIL Antibody ergotamine PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank Drug Central
small-molecule Agonist 5-hydroxytryptamine small-molecule Yes No Ishchenko A, Wacker D, Kapoor M, Zhang A, Han GW, Basu S, Patel N, Messerschmidt M, Weierstall U, Liu W, Katritch V, Roth BL, Stevens RC, Cherezov V 10.1073/PNAS.1700891114 2017-07-26 Yes
EDNRB ETB Endothelin A Human X-ray 5XPR 5XPR_refined 3.6 A Inactive 4 69 - - - - T4-Lysozyme - - - - endothelin-2, endothelin-3, endothelin-1 peptide Yes No Shihoya W, Nishizawa T, Yamashita K, Inoue A, Hirata K, Kadji FMN, Okuta A, Tani K, Aoki J, Fujiyoshi Y, Doi T, Nureki O 10.1038/NSMB.3450 2017-08-16 Yes
AA2AR A2A Adenosine A Human X-ray 5NM2 5NM2_refined 2.0 A Inactive 1 72 - - - - BRIL - ZM-241385 PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank
small-molecule Antagonist adenosine small-molecule Yes Yes Weinert T, Olieric N, Cheng R, Brunle S, James D, Ozerov D, Gashi D, Vera L, Marsh M, Jaeger K, Dworkowski F, Panepucci E, Basu S, Skopintsev P, Dore AS, Geng T, Cooke RM, Liang M, Prota AE, Panneels V, Nogly P, Ermler U, Schertler G, Hennig M, Steinmetz MO, Wang M, Standfuss J 10.1038/S41467-017-00630-4 2017-09-27 Yes
OX2R OX2 Orexin A Human X-ray 5WQC 5WQC_refined 2.0 A Inactive 1 68 - - - - Glycogen synthase - EMPA PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Antagonist orexin-B, orexin-A peptide Yes No Suno R, Kimura KT, Nakane T, Yamashita K, Wang J, Fujiwara T, Yamanaka Y, Im D, Horita S, Tsujimoto H, Tawaramoto MS, Hirokawa T, Nango E, Tono K, Kameshima T, Hatsui T, Joti Y, Yabashi M, Shimamoto K, Yamamoto M, Rosenbaum DM, Iwata S, Shimamura T, Kobayashi T 10.1016/J.STR.2017.11.005 2017-11-29 Yes
C5AR1 C5a1 Complement peptide A Human X-ray 5O9H 5O9H_refined 2.7 A Inactive 6 84 - - - - - - NDT9513727 PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Antagonist C3a, C5a des-Arg, ribosomal protein S19, C5a peptide Yes No Robertson N, Rappas M, Dore AS, Brown J, Bottegoni G, Koglin M, Cansfield J, Jazayeri A, Cooke RM, Marshall FH 10.1038/NATURE25025 2018-01-10 Yes
AA2AR A2A Adenosine A Human X-ray 5OLO 5OLO_refined 3.1 A Inactive 1 72 - - - - BRIL - tozadenant PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank
small-molecule Antagonist adenosine small-molecule Yes No Rucktooa P, Cheng RKY, Segala E, Geng T, Errey JC, Brown GA, Cooke RM, Marshall FH, Dore AS 10.1038/S41598-017-18570-W 2018-01-17 Yes
AA2AR A2A Adenosine A Human X-ray 5OM4 5OM4_refined 2.0 A Inactive 1 72 - - - - BRIL - CHEMBL2024114 ChEMBL_compound_ids PubChem
small-molecule Antagonist adenosine small-molecule Yes Yes Rucktooa P, Cheng RKY, Segala E, Geng T, Errey JC, Brown GA, Cooke RM, Marshall FH, Dore AS 10.1038/S41598-017-18570-W 2018-01-17 Yes
5HT2C 5-HT2C 5-Hydroxytryptamine A Human X-ray 6BQG 6BQG_refined 3.0 A Active 92 62 - - - - BRIL - ergotamine PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank Drug Central
small-molecule Agonist 5-hydroxytryptamine small-molecule Yes No Peng Y, McCorvy JD, Harpsoe K, Lansu K, Yuan S, Popov P, Qu L, Pu M, Che T, Nikolajsen LF, Huang XP, Wu Y, Shen L, Bjorn-Yoshimoto WE, Ding K, Wacker D, Han GW, Cheng J, Katritch V, Jensen AA, Hanson MA, Zhao S, Gloriam DE, Roth BL, Stevens RC, Liu ZJ 10.1016/j.cell.2018.01.001 2018-02-14 Yes
GLP1R GLP-1 Glucagon B1 Human cryo-EM 6B3J 6B3J_refined 3.3 R Active 100 82 Gs αs - 49 - - Exendin-P5
peptide Agonist glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon peptide No No Liang YL, Khoshouei M, Glukhova A, Furness SGB, Zhao P, Clydesdale L, Koole C, Truong TT, Thal DM, Lei S, Radjainia M, Danev R, Baumeister W, Wang MW, Miller LJ, Christopoulos A, Sexton PM, Wootten D 10.1038/NATURE25773 2018-02-21 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 6FKA 6FKA_refined 2.7 A Active 99 94 - - - - - - (2~{S})-2-(3,4-dichlorophenyl)-3-methyl-1-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-yl-butan-1-one PubChem
small-molecule Agonist - - No No Mattle D, Kuhn B, Aebi J, Bedoucha M, Kekilli D, Grozinger N, Alker A, Rudolph MG, Schmid G, Schertler GFX, Hennig M, Standfuss J, Dawson RJP 10.1073/PNAS.1718084115 2018-04-04 Yes
NPY1R Y1 Neuropeptide Y A Human X-ray 5ZBH 5ZBH_refined 3.0 A Inactive 1 78 - - - - T4-Lysozyme - BMS-193885 PubChem
small-molecule Antagonist neuropeptide Y, pancreatic polypeptide, peptide YY peptide Yes No Yang Z, Han S, Keller M, Kaiser A, Bender BJ, Bosse M, Burkert K, Kogler LM, Wifling D, Bernhardt G, Plank N, Littmann T, Schmidt P, Yi C, Li B, Ye S, Zhang R, Xu B, Larhammar D, Stevens RC, Huster D, Meiler J, Zhao Q, Beck-Sickinger AG, Buschauer A, Wu B 10.1038/S41586-018-0046-X 2018-04-25 Yes
Q98SW5 SMO Frizzled F African clawed frog X-ray 6D32 6D32_refined 3.8 A Active 87 58 - - - - BRIL - cyclopamine PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Agonist (partial) - - No No Huang P, Zheng S, Wierbowski BM, Kim Y, Nedelcu D, Aravena L, Liu J, Kruse AC, Salic A 10.1016/J.CELL.2018.04.029 2018-05-23 Yes
Q80KM9 US28 Unclassified A strain AD169 X-ray 5WB1 5WB1_refined 3.5 A Active 100 82 - - - - - Nanobody - - - - - Yes No Miles TF, Spiess K, Jude KM, Tsutsumi N, Burg JS, Ingram JR, Waghray D, Hjorto GM, Larsen O, Ploegh HL, Rosenkilde MM, Garcia KC 10.7554/ELIFE.35850 2018-06-13 Yes
OPRM μ Opioid A Mouse cryo-EM 6DDF 6DDF_refined 3.5 R Active 100 71 Gi/o αi1 - 61 - - DAMGO PubChem Guide To Pharmacology ChEMBL_compound_ids ChEMBL_compound_ids
peptide Agonist - - Yes No Koehl A, Hu H, Maeda S, Zhang Y, Qu Q, Paggi JM, Latorraca NR, Hilger D, Dawson R, Matile H, Schertler GFX, Granier S, Weis WI, Dror RO, Manglik A, Skiniotis G, Kobilka BK 10.1038/S41586-018-0219-7 2018-06-13 Yes
5HT1B 5-HT1B 5-Hydroxytryptamine A Human cryo-EM 6G79 6G79_refined 3.8 S Active 100 67 Gi/o αo - 59 - - donitriptan PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Agonist 5-hydroxytryptamine, 5-HT-moduline, tryptamine small-molecule Yes No Garcia-Nafria J, Nehme R, Edwards PC, Tate CG 10.1038/S41586-018-0241-9 2018-06-20 Yes
5HT2B 5-HT2B 5-Hydroxytryptamine A Human X-ray 6DRY 6DRY_refined 2.9 A Intermediate 36 60 - - - - BRIL - methylergonovine PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank Drug Central
small-molecule Agonist 5-hydroxytryptamine small-molecule Yes No McCorvy JD, Wacker D, Wang S, Agegnehu B, Liu J, Lansu K, Tribo AR, Olsen RHJ, Che T, Jin J, Roth BL 10.1038/s41594-018-0116-7 2018-08-29 Yes
PD2R2 DP2 Prostanoid A Human X-ray 6D26 6D26_refined 2.8 A Inactive 19 82 - - - - T4-Lysozyme - fevipiprant PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank
small-molecule Antagonist PGI2, PGD2, PGE2, PGJ2, thromboxane A2, PGF2α, PGD3 small-molecule Yes No Wang L, Yao D, Deepak RNVK, Liu H, Xiao Q, Fan H, Gong W, Wei Z, Zhang C 10.1016/J.MOLCEL.2018.08.009 2018-10-03 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 6H7J 6H7J_refined 2.8 A Active 100 60 - - - - Thioredoxin 1 Camelid antibody fragment Nb80 (R)-Isoproterenol PubChem ChEMBL_compound_ids
small-molecule Agonist - - Yes No Warne T, Edwards PC, Dore AS, Leslie AGW, Tate CG 10.1126/SCIENCE.AAU5595 2018-10-17 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 6H7N 6H7N_refined 2.5 A Active 100 60 - - - - Thioredoxin 1 Camelid antibody fragment Nb6B9 (S)-Xamoterol PubChem
small-molecule Agonist - - Yes No - 10.1101/436212 2018-10-17 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 6MXT 6MXT_refined 3.0 A Active 100 69 - - - - T4-Lysozyme Nanobody-71 salmeterol PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank Drug Central
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, Zn2+, (-)-adrenaline, (-)-noradrenaline small-molecule Yes No Masureel M, Zou Y, Picard LP, van der Westhuizen E, Mahoney JP, Rodrigues JPGLM, Mildorf TJ, Dror RO, Shaw DE, Bouvier M, Pardon E, Steyaert J, Sunahara RK, Weis WI, Zhang C, Kobilka BK 10.1038/s41589-018-0145-x 2018-11-14 Yes
ACM2 M2 Acetylcholine (muscarinic) A Human X-ray 5ZKC 5ZKC_refined 2.3 A Inactive 3 60 - - - - BRIL - N-methyl scopolamine PubChem Guide To Pharmacology DrugBank Guide To Pharmacology
small-molecule Antagonist acetylcholine small-molecule No No Suno R, Lee S, Maeda S, Yasuda S, Yamashita K, Hirata K, Horita S, Tawaramoto MS, Tsujimoto H, Murata T, Kinoshita M, Yamamoto M, Kobilka BK, Vaidehi N, Iwata S, Kobayashi T 10.1038/S41589-018-0152-Y 2018-11-21 Yes
EDNRB ETB Endothelin A Human X-ray 6IGL 6IGL_refined 2.7 A Inactive 4 70 - - - - T4-Lysozyme - IRL 1620 PubChem Guide To Pharmacology ChEMBL_compound_ids Guide To Pharmacology PubChem PubChem
peptide Agonist (partial) endothelin-2, endothelin-3, endothelin-1 peptide Yes No Shihoya W, Izume T, Inoue A, Yamashita K, Kadji FMN, Hirata K, Aoki J, Nishizawa T, Nureki O 10.1038/S41467-018-07094-0 2018-11-21 Yes
PE2R3 EP3 Prostanoid A Human X-ray 6AK3 6AK3_refined 2.9 B Active 83 69 - - - - BRIL - PGE2 PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank Drug Central Guide To Pharmacology
small-molecule Agonist PGI2, PGE1, PGD2, PGE2, thromboxane A2, PGF2α small-molecule Yes No Morimoto K, Suno R, Hotta Y, Yamashita K, Hirata K, Yamamoto M, Narumiya S, Iwata S, Kobayashi T 10.1038/S41589-018-0171-8 2018-12-05 Yes
TA2R TP Prostanoid A Human X-ray 6IIU 6IIU_refined 2.5 A Intermediate 46 87 - - - - Rubredoxin - ramatroban PubChem Guide To Pharmacology ChEMBL_compound_ids Drug Central DrugBank Guide To Pharmacology
small-molecule Antagonist PGI2, PGD2, PGE2, PGH2, thromboxane A2, PGF2α small-molecule No No Fan H, Chen S, Yuan X, Han S, Zhang H, Xia W, Xu Y, Zhao Q, Wu B 10.1038/S41589-018-0170-9 2018-12-19 Yes
CCR2 CCR2 Chemokine A Human X-ray 6GPS 6GPS_refined 3.3 A Inactive 12 74 - - - - Rubredoxin - MK-0812 PubChem
small-molecule Antagonist CCL11, CCL2, CCL7, CCL8, CCL16, CCL24, CCL13, CCL26 peptide No No Apel AK, Cheng RKY, Tautermann CS, Brauchle M, Huang CY, Pautsch A, Hennig M, Nar H, Schnapp G 10.1016/J.STR.2018.10.027 2019-01-02 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 6IBL 6IBL_refined 2.7 A Active 100 60 - - - - Thioredoxin 1 Camelid antibody fragment Nb80 arformoterol PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank Drug Central
small-molecule Agonist - - Yes No - 10.1101/436212 2019-01-09 Yes
NK1R NK1 Tachykinin A Human X-ray 6HLP 6HLP_refined 2.2 A Inactive 1 71 - - - - GlgA glycogen synthase - netupitant PubChem Guide To Pharmacology ChEMBL_compound_ids Drug Central DrugBank
small-molecule Antagonist hemokinin 1, neurokinin A, neurokinin B, substance P, neuropeptide-γ, neuropeptide K peptide Yes No Schoppe J, Ehrenmann J, Klenk C, Rucktooa P, Schutz M, Dore AS, Pluckthun A 10.1038/S41467-018-07939-8 2019-01-16 Yes
GRM5 mGlu5 Metabotropic glutamate C Human cryo-EM 6N52 6N52_refined 4.0 A Inactive 29 64 - - - - - Nanobody-43 - - - L-glutamic acid small-molecule No No - - 2019-01-23 Yes
CALCR CT Calcitonin B1 Human cryo-EM 6NIY 6NIY_refined 3.3 R Active 100 55 Gs αs - 43 - - Calcitonin salmon PubChem
peptide Agonist calcitonin (salmon), adrenomedullin, calcitonin, adrenomedullin 2/intermedin, β-CGRP, α-CGRP, amylin peptide No No Dal Maso E, Glukhova A, Zhu Y, Garcia-Nafria J, Tate CG, Atanasio S, Reynolds CA, Ramirez-Aportela E, Carazo JM, Hick CA, Furness SGB, Hay DL, Liang YL, Miller LJ, Christopoulos A, Wang MW, Wootten D, Sexton PM 10.1021/ACSPTSCI.8B00056 2019-01-23 Yes
CNR1 CB1 Cannabinoid A Human cryo-EM 6N4B 6N4B_refined 3.0 R Active 100 58 Gi/o αi1 - 62 - scFv16 MDMB-Fubinaca PubChem Guide To Pharmacology
small-molecule Agonist 2-arachidonoylglycerol, anandamide small-molecule Yes No Krishna Kumar K, Shalev-Benami M, Robertson MJ, Hu H, Banister SD, Hollingsworth SA, Latorraca NR, Kato HE, Hilger D, Maeda S, Weis WI, Farrens DL, Dror RO, Malhotra SV, Kobilka BK, Skiniotis G 10.1016/J.CELL.2018.11.040 2019-01-30 Yes
5HT2A 5-HT2A 5-Hydroxytryptamine A Human X-ray 6A94 6A94_refined 2.9 A Inactive 1 60 - - - - BRIL - zotepine PubChem Guide To Pharmacology ChEMBL_compound_ids Drug Central DrugBank
small-molecule Antagonist 5-hydroxytryptamine, tryptamine small-molecule No No Kimura KT, Asada H, Inoue A, Kadji FMN, Im D, Mori C, Arakawa T, Hirata K, Nomura Y, Nomura N, Aoki J, Iwata S, Shimamura T 10.1038/S41594-018-0180-Z 2019-02-13 Yes
PTH1R PTH1 Parathyroid hormone B1 Human cryo-EM 6NBF 6NBF_refined 3.0 R Active 100 62 Gs αs - 58 - Nanobody-35 Long-acting parathyroid hormone analog
peptide Agonist PTH, PTHrP-(1-36), PTHrP, TIP39 peptide No No Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y 10.1126/SCIENCE.AAV7942 2019-04-17 Yes
PTH1R PTH1 Parathyroid hormone B1 Human cryo-EM 6NBI 6NBI_refined 4.0 R Active 100 62 Gs αs - 56 - Nanobody-35 Long-acting parathyroid hormone analog
peptide Agonist PTH, PTHrP-(1-36), PTHrP, TIP39 peptide No No Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y 10.1126/SCIENCE.AAV7942 2019-04-17 Yes
MTR1A MT1 Melatonin A Human X-ray 6ME4 6ME4_refined 3.2 A Inactive 1 83 - - - - GlgA glycogen synthase - 2-iodo-melatonin PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank
small-molecule Agonist melatonin small-molecule No No Stauch B, Johansson LC, McCorvy JD, Patel N, Han GW, Huang XP, Gati C, Batyuk A, Slocum ST, Ishchenko A, Brehm W, White TA, Michaelian N, Madsen C, Zhu L, Grant TD, Grandner JM, Shiriaeva A, Olsen RHJ, Tribo AR, Yous S, Stevens RC, Weierstall U, Katritch V, Roth BL, Liu W, Cherezov V 10.1038/S41586-019-1141-3 2019-04-24 Yes
MTR1B MT2 Melatonin A Human X-ray 6ME6 6ME6_refined 2.8 B Inactive 1 78 - - - - Rubredoxin - 2-phenylmelatonin PubChem
small-molecule Agonist melatonin small-molecule No No Johansson LC, Stauch B, McCorvy JD, Han GW, Patel N, Huang XP, Batyuk A, Gati C, Slocum ST, Li C, Grandner JM, Hao S, Olsen RHJ, Tribo AR, Zaare S, Zhu L, Zatsepin NA, Weierstall U, Yous S, Stevens RC, Liu W, Roth BL, Katritch V, Cherezov V 10.1038/S41586-019-1144-0 2019-04-24 Yes
MTR1B MT2 Melatonin A Human X-ray 6ME8 6ME8_refined 3.1 B Inactive 1 78 - - - - Rubredoxin - 2-phenylmelatonin PubChem
small-molecule Agonist melatonin small-molecule Yes No Johansson LC, Stauch B, McCorvy JD, Han GW, Patel N, Huang XP, Batyuk A, Gati C, Slocum ST, Li C, Grandner JM, Hao S, Olsen RHJ, Tribo AR, Zaare S, Zhu L, Zatsepin NA, Weierstall U, Yous S, Stevens RC, Liu W, Roth BL, Katritch V, Cherezov V 10.1038/S41586-019-1144-0 2019-04-24 Yes
AA2AR A2A Adenosine A Human X-ray 6MH8 6MH8_refined 4.2 A Inactive 1 72 - - - - BRIL - ZM-241385 PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank
small-molecule Antagonist adenosine small-molecule Yes No Martin-Garcia JM, Zhu L, Mendez D, Lee MY, Chun E, Li C, Hu H, Subramanian G, Kissick D, Ogata C, Henning R, Ishchenko A, Dobson Z, Zhang S, Weierstall U, Spence JCH, Fromme P, Zatsepin NA, Fischetti RF, Cherezov V, Liu W 10.1107/S205225251900263X 2019-04-24 Yes
ACM2 M2 Acetylcholine (muscarinic) A Human cryo-EM 6OIK 6OIK_refined 3.6 R Active 100 60 Gi/o αo - 61 - - iperoxo PubChem Guide To Pharmacology ChEMBL_compound_ids
LY2119620 PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule
small-molecule		 Agonist
PAM		 acetylcholine small-molecule Yes No Maeda S, Qu Q, Robertson MJ, Skiniotis G, Kobilka BK 10.1126/SCIENCE.AAW5188 2019-05-08 Yes
SMO SMO Frizzled F Human cryo-EM 6OT0 - 3.9 R Active 100 46 Gi/o αi1 - 100 - Fab light chain
Fab heavy chain		 24,25-Epoxy-cholesterol PubChem
small-molecule Agonist - - No No Qi X, Liu H, Thompson B, McDonald J, Zhang C, Li X 10.1038/S41586-019-1286-0 2019-06-12 Yes
SMO SMO Frizzled F Mouse X-ray 6O3C 6O3C_refined 2.8 A Active 94 61 - - - - - Nanobody-Smo8 SAG21k PubChem
small-molecule Agonist - - No No Deshpande I, Liang J, Hedeen D, Roberts KJ, Zhang Y, Ha B, Latorraca NR, Faust B, Dror RO, Beachy PA, Myers BR, Manglik A 10.1038/S41586-019-1355-4 2019-07-03 Yes
OPSD Rhodopsin Opsins A Bovine cryo-EM 6QNO 6QNO_refined 4.4 R Active 100 96 Gi/o αi1 - 60 - Fab antibody fragment light chain
Fab antibody fragment heavy chain		 Retinal (all-trans) PubChem
small-molecule Agonist - - No No Tsai CJ, Marino J, Adaixo R, Pamula F, Muehle J, Maeda S, Flock T, Taylor NM, Mohammed I, Matile H, Dawson RJ, Deupi X, Stahlberg H, Schertler G 10.7554/ELIFE.46041 2019-07-10 Yes
SUCR1 succinate Succinate A Rat X-ray 6RNK 6RNK_refined 1.9 A Intermediate 36 90 - - - - - Nanobody-6 NF-56-EJ40 PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Antagonist - - Yes No Haffke M, Fehlmann D, Rummel G, Boivineau J, Duckely M, Gommermann N, Cotesta S, Sirockin F, Freuler F, Littlewood-Evans A, Kaupmann K, Jaakola VP 10.1038/S41586-019-1663-8 2019-08-14 Yes
AA2AR A2A Adenosine A Human X-ray 6JZH 6JZH_refined 2.3 A Inactive 1 72 - - - - BRIL - ZM-241385 PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank
small-molecule Antagonist adenosine small-molecule Yes Yes Shimazu Y, Tono K, Tanaka T, Yamanaka Y, Nakane T, Mori C, Terakado Kimura K, Fujiwara T, Sugahara M, Tanaka R, Doak RB, Shimamura T, Iwata S, Nango E, Yabashi M 10.1107/S1600576719012846 2019-10-30 Yes
GLP1R GLP-1 Glucagon B1 Human X-ray 6KK1 6KK1_refined 2.8 B Inactive 0 57 - - - - T4-Lysozyme - PF-06372222 PubChem
small-molecule NAM glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon peptide No No Xu Y, Wang Y, Wang Y, Liu K, Peng Y, Yao D, Tao H, Liu H, Song G 10.1107/S2052252519013496 2019-11-13 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 6PS1 6PS1_refined 3.2 A Inactive 0 68 - - - - T4-Lysozyme - timolol PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank Drug Central
small-molecule Antagonist noradrenaline, L-NOREPINEPHRINE, Zn2+, (-)-adrenaline, (-)-noradrenaline small-molecule Yes No Ishchenko A, Stauch B, Han GW, Batyuk A, Shiriaeva A, Li C, Zatsepin N, Weierstall U, Liu W, Nango E, Nakane T, Tanaka R, Tono K, Joti Y, Iwata S, Moraes I, Gati C, Cherezov V 10.1107/S2052252519013137 2019-11-13 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 6PS5 6PS5_refined 2.9 A Inactive 0 68 - - - - T4-Lysozyme - (-)-propranolol PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank
small-molecule Antagonist noradrenaline, L-NOREPINEPHRINE, Zn2+, (-)-adrenaline, (-)-noradrenaline small-molecule Yes No Ishchenko A, Stauch B, Han GW, Batyuk A, Shiriaeva A, Li C, Zatsepin N, Weierstall U, Liu W, Nango E, Nakane T, Tanaka R, Tono K, Joti Y, Iwata S, Moraes I, Gati C, Cherezov V 10.1107/S2052252519013137 2019-11-13 Yes
ADRB2 β2 Adrenoceptors A Human cryo-EM 6NI3 6NI3_refined 3.8 R Active 100 69 Gs αs - 59 - Nanobody-35 BI-167107 PubChem
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, Zn2+, (-)-adrenaline, (-)-noradrenaline small-molecule Yes No Nguyen AH, Thomsen ARB, Cahill TJ 3rd, Huang R, Huang LY, Marcink T, Clarke OB, Heissel S, Masoudi A, Ben-Hail D, Samaan F, Dandey VP, Tan YZ, Hong C, Mahoney JP, Triest S, Little J 4th, Chen X, Sunahara R, Steyaert J, Molina H, Yu Z, des Georges A, Lefkowitz RJ 10.1038/S41594-019-0330-Y 2019-11-20 Yes
ACM5 M5 Acetylcholine (muscarinic) A Human X-ray 6OL9 6OL9_refined 2.5 A Inactive 3 53 - - - - T4-Lysozyme - tiotropium PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank Guide To Pharmacology
small-molecule Inverse agonist acetylcholine small-molecule No No Vuckovic Z, Gentry PR, Berizzi AE, Hirata K, Varghese S, Thompson G, van der Westhuizen ET, Burger WAC, Rahmani R, Valant C, Langmead CJ, Lindsley CW, Baell JB, Tobin AB, Sexton PM, Christopoulos A, Thal DM 10.1073/PNAS.1914446116 2019-12-11 Yes
CLTR2 CysLT2 Leukotriene A Human X-ray 6RZ7 6RZ7_refined 2.4 A Intermediate 36 79 - - - - BRIL - ONO-2570366 Guide To Pharmacology PubChem
small-molecule Antagonist LTC4, LTD4, LTE4 small-molecule No No Gusach A, Luginina A, Marin E, Brouillette RL, Besserer-Offroy E, Longpre JM, Ishchenko A, Popov P, Patel N, Fujimoto T, Maruyama T, Stauch B, Ergasheva M, Romanovskaia D, Stepko A, Kovalev K, Shevtsov M, Gordeliy V, Han GW, Katritch V, Borshchevskiy V, Sarret P, Mishin A, Cherezov V 10.1038/S41467-019-13348-2 2019-12-11 Yes
OX1R OX1 Orexin A Human X-ray 6TOD 6TOD_refined 2.1 A Inactive 1 71 - - - - - - EMPA PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Antagonist orexin-B, orexin-A peptide No No Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Dore AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA 10.1021/ACS.JMEDCHEM.9B01787 2020-01-01 Yes
OX2R OX2 Orexin A Human X-ray 6TPG 6TPG_refined 2.7 A Inactive 1 69 - - - - GlgA glycogen synthase - EMPA PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Antagonist orexin-B, orexin-A peptide No No Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Dore AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA 10.1021/ACS.JMEDCHEM.9B01787 2020-01-01 Yes
OX1R OX1 Orexin A Human X-ray 6TQ4 6TQ4_refined 2.3 B Inactive 1 70 - - - - - - CHEMBL4590386 ChEMBL_compound_ids PubChem
small-molecule Antagonist orexin-B, orexin-A peptide No No Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Dore AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA 10.1021/ACS.JMEDCHEM.9B01787 2020-01-01 Yes
GLP1R GLP-1 Glucagon B1 Human cryo-EM 6ORV - 3.0 E Active 100 61 Gs αs - 48 - Nanobody-35 CHEMBL3950796 ChEMBL_compound_ids PubChem
small-molecule Agonist glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon peptide No No Zhao P, Liang YL, Belousoff MJ, Deganutti G, Fletcher MM, Willard FS, Bell MG, Christe ME, Sloop KW, Inoue A, Truong TT, Clydesdale L, Furness SGB, Christopoulos A, Wang MW, Miller LJ, Reynolds CA, Danev R, Sexton PM, Wootten D 10.1038/s41586-019-1902-z 2020-01-08 Yes
APJ apelin Apelin A Human X-ray 6KNM 6KNM_refined 3.2 B Inactive 5 78 - - - - Rubredoxin - Single domain antibody JN241
protein Agonist apelin receptor early endogenous ligand, Elabela/Toddler-11, Elabela/Toddler-21, apelin-17, [Pyr1]apelin-13, apelin-13, apelin-36, Elabela/Toddler-32 peptide Yes No Ma Y, Ding Y, Song X, Ma X, Li X, Zhang N, Song Y, Sun Y, Shen Y, Zhong W, Hu LA, Ma Y, Zhang MY 10.1126/SCIADV.AAX7379 2020-01-29 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 6NWE 6NWE_refined 2.7 A Active 100 94 Gi/o αt1 Only H5 3 - - B-Octylglucoside PubChem
small-molecule unknown - - No No - - 2020-02-12 Yes
CRFR2 CRF2 Corticotropin-releasing factor B1 Human cryo-EM 6PB1 6PB1_refined 2.8 P Active 100 68 Gs αs - 58 - Nanobody-35 CHEMBL427807 ChEMBL_compound_ids PubChem
protein Agonist urocortin 2, urocortin 1, corticotrophin-releasing hormone, urocortin 3 peptide No No Ma S, Shen Q, Zhao LH, Mao C, Zhou XE, Shen DD, de Waal PW, Bi P, Li C, Jiang Y, Wang MW, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE 10.1016/J.MOLCEL.2020.01.013 2020-02-12 Yes
GPR52 GPR52 A orphans A Human X-ray 6LI1 6LI1_refined 2.9 A Inactive 32 81 - - - - Flavodoxin - - - - - - Yes No Lin X, Li M, Wang N, Wu Y, Luo Z, Guo S, Han GW, Li S, Yue Y, Wei X, Xie X, Chen Y, Zhao S, Wu J, Lei M, Xu F 10.1038/S41586-020-2019-0 2020-02-26 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 3DQB 3DQB_refined 3.2 A Active 100 94 Gi/o αt1 Only H5 3 - - Apo (no ligand)
none Apo (no ligand) - - No No Scheerer P, Park JH, Hildebrand PW, Kim YJ, Krauss N, Choe HW, Hofmann KP, Ernst OP 10.1038/NATURE07330 2008-09-23 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 3NY9 3NY9_refined 2.8 A Inactive 0 67 - - - - T4-Lysozyme - CHEMBL1233771 ChEMBL_compound_ids PubChem
small-molecule Inverse agonist noradrenaline, L-NOREPINEPHRINE, Zn2+, (-)-adrenaline, (-)-noradrenaline small-molecule Yes No Wacker D, Fenalti G, Brown MA, Katritch V, Abagyan R, Cherezov V, Stevens RC 10.1021/JA105108Q 2010-08-11 Yes
CXCR4 CXCR4 Chemokine A Human X-ray 3OE6 - 3.2 A Inactive 5 77 - - - - T4-Lysozyme - isothiourea-1t PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Antagonist CXCL12β, CXCL12φ, CXCL12, CXCL12γ, CXCL12δ, CXCL12ε, CXCL12α peptide Yes No Wu B, Chien EY, Mol CD, Fenalti G, Liu W, Katritch V, Abagyan R, Brooun A, Wells P, Bi FC, Hamel DJ, Kuhn P, Handel TM, Cherezov V, Stevens RC 10.1126/SCIENCE.1194396 2010-10-27 No
CXCR4 CXCR4 Chemokine A Human X-ray 3OE9 - 3.1 A Inactive 5 74 - - - - T4-Lysozyme - isothiourea-1t PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Antagonist CXCL12β, CXCL12φ, CXCL12, CXCL12γ, CXCL12δ, CXCL12ε, CXCL12α peptide Yes No Wu B, Chien EY, Mol CD, Fenalti G, Liu W, Katritch V, Abagyan R, Brooun A, Wells P, Bi FC, Hamel DJ, Kuhn P, Handel TM, Cherezov V, Stevens RC 10.1126/SCIENCE.1194396 2010-10-27 No
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 2Y04 2Y04_refined 3.1 B Inactive 0 62 - - - - - - levosalbutamol PubChem Guide To Pharmacology ChEMBL_compound_ids Drug Central DrugBank
small-molecule Agonist (partial) - - Yes No Warne T, Moukhametzianov R, Baker JG, Nehme R, Edwards PC, Leslie AG, Schertler GF, Tate CG 10.1038/NATURE09746 2011-01-12 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 3PQR 3PQR_refined 2.9 A Active 100 94 Gi/o αt1 Only H5 3 - - Retinal (all-trans) PubChem
small-molecule Agonist - - No No Choe HW, Kim YJ, Park JH, Morizumi T, Pai EF, Krauss N, Hofmann KP, Scheerer P, Ernst OP 10.1038/NATURE09789 2011-03-09 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 2X72 2X72_refined 3.0 A Active 100 94 Gi/o αt1 Only H5 3 - - Retinal (all-trans) PubChem
small-molecule Agonist - - No No Standfuss J, Edwards PC, D'Antona A, Fransen M, Xie G, Oprian DD, Schertler GF 10.1038/NATURE09795 2011-03-16 Yes
AA2AR A2A Adenosine A Human X-ray 2YDV 2YDV_refined 2.6 A Active 73 75 - - - - - - NECA PubChem Guide To Pharmacology ChEMBL_compound_ids Guide To Pharmacology
small-molecule Agonist adenosine small-molecule Yes No Lebon G, Warne T, Edwards PC, Bennett K, Langmead CJ, Leslie AG, Tate CG 10.1038/NATURE10136 2011-05-18 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 2YCY - 3.2 A Inactive 0 60 - - - - - - (S)-Cyanopindolol PubChem
small-molecule Antagonist - - Yes No Moukhametzianov R, Warne T, Edwards PC, Serrano-Vega MJ, Leslie AG, Tate CG, Schertler GF 10.1073/PNAS.1100185108 2011-06-08 No
OPSD Rhodopsin Opsins A Japanese flying squid X-ray 3AYN - 2.7 B Inactive 13 77 - - - - - - Retinal (9-cis) PubChem
small-molecule Inverse agonist - - Yes No Murakami M, Kouyama T 10.1016/J.JMB.2011.08.044 2011-08-17 No
AA2AR A2A Adenosine A Human X-ray 3RFM 3RFM_refined 3.6 A Inactive 1 71 - - - - - - caffeine PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank Drug Central
small-molecule Antagonist adenosine small-molecule Yes No Dore AS, Robertson N, Errey JC, Ng I, Hollenstein K, Tehan B, Hurrell E, Bennett K, Congreve M, Magnani F, Tate CG, Weir M, Marshall FH 10.1016/J.STR.2011.06.014 2011-09-07 Yes
AA2AR A2A Adenosine A Human X-ray 3VGA - 3.1 A Inactive 1 72 - - - - - - ZM-241385 PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank
small-molecule Antagonist adenosine small-molecule Yes No 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 AD, Kobayashi T, Hamakubo T, Iwata S, Murata T 10.1038/NATURE10750 2012-02-01 No
AA2AR A2A Adenosine A Human X-ray 3UZA 3UZA_refined 3.3 A Inactive 1 71 - - - - - - compound 4g [PMID: 22220592] PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Antagonist adenosine small-molecule Yes No Congreve M, Andrews SP, Dore AS, Hollenstein K, Hurrell E, Langmead CJ, Mason JS, Ng IW, Tehan B, Zhukov A, Weir M, Marshall FH 10.1021/JM201376W 2012-03-21 Yes
OPRM μ Opioid A Mouse X-ray 4DKL 4DKL_refined 2.8 A Inactive 5 71 - - - - T4-Lysozyme - Methyl 4-[[(4R,4aS,7R,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl]amino]-4-oxobutanoate PubChem
small-molecule Antagonist - - Yes No Manglik A, Kruse AC, Kobilka TS, Thian FS, Mathiesen JM, Sunahara RK, Pardo L, Weis WI, Kobilka BK, Granier S 10.1038/NATURE10954 2012-03-21 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 4AMJ 4AMJ_refined 2.3 B Inactive 0 62 - - - - - - (S)-Carvedilol PubChem ChEMBL_compound_ids
small-molecule Inverse agonist - - Yes No Warne T, Edwards PC, Leslie AG, Tate CG 10.1016/J.STR.2012.03.014 2012-05-23 Yes
PAR1 PAR1 Proteinase-activated A Human X-ray 3VW7 3VW7_refined 2.2 A Intermediate 36 66 - - - - T4-Lysozyme - vorapaxar PubChem Guide To Pharmacology ChEMBL_compound_ids Drug Central DrugBank
small-molecule Antagonist thrombin peptide Yes No Zhang C, Srinivasan Y, Arlow DH, Fung JJ, Palmer D, Zheng Y, Green HF, Pandey A, Dror RO, Shaw DE, Weis WI, Coughlin SR, Kobilka BK 10.1038/NATURE11701 2012-12-12 Yes
5HT2B 5-HT2B 5-Hydroxytryptamine A Human X-ray 4IB4 4IB4_refined 2.7 A Intermediate 36 59 - - - - BRIL - ergotamine PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank Drug Central
small-molecule Agonist 5-hydroxytryptamine small-molecule Yes No Wacker D, Wang C, Katritch V, Han GW, Huang XP, Vardy E, McCorvy JD, Jiang Y, Chu M, Siu FY, Liu W, Xu HE, Cherezov V, Roth BL, Stevens RC 10.1126/science.1232808 2013-03-13 Yes
SMO SMO Frizzled F Human X-ray 4JKV 4JKV_refined 2.5 A Inactive 0 44 - - - - BRIL - taladegib PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank
small-molecule Antagonist - - No No Wang C, Wu H, Katritch V, Han GW, Huang XP, Liu W, Siu FY, Roth BL, Cherezov V, Stevens RC 10.1038/NATURE12167 2013-04-24 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 4LDL 4LDL_refined 3.1 A Active 100 69 - - - - T4-Lysozyme Nanobody hydroxybenzylisoproterenol PubChem
small-molecule Agonist noradrenaline, L-NOREPINEPHRINE, Zn2+, (-)-adrenaline, (-)-noradrenaline small-molecule Yes No Ring AM, Manglik A, Kruse AC, Enos MD, Weis WI, Garcia KC, Kobilka BK 10.1038/NATURE12572 2013-09-25 Yes
ACM2 M2 Acetylcholine (muscarinic) A Human X-ray 4MQT 4MQT_refined 3.7 A Active 100 59 - - - - - Nanobody iperoxo PubChem Guide To Pharmacology ChEMBL_compound_ids
LY2119620 PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule
small-molecule		 Agonist
PAM		 acetylcholine small-molecule Yes No Kruse AC, Ring AM, Manglik A, Hu J, Hu K, Eitel K, Hubner H, Pardon E, Valant C, Sexton PM, Christopoulos A, Felder CC, Gmeiner P, Steyaert J, Weis WI, Garcia KC, Wess J, Kobilka BK 10.1038/NATURE12735 2013-11-27 Yes
NTR1 NTS1 Neurotensin A Rat X-ray 3ZEV - 3.0 A Inactive 2 72 - - - - - - neurotensin PubChem Guide To Pharmacology ChEMBL_compound_ids Guide To Pharmacology Guide To Pharmacology
peptide Agonist neurotensin, neuromedin N peptide Yes No Egloff P, Hillenbrand M, Klenk C, Batyuk A, Heine P, Balada S, Schlinkmann KM, Scott DJ, Schutz M, Pluckthun A 10.1073/PNAS.1317903111 2014-01-29 No
SMO SMO Frizzled F Human X-ray 4O9R 4O9R_refined 3.2 A Inactive 12 42 - - - - BRIL - cyclopamine PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Antagonist - - No No Weierstall U, James D, Wang C, White TA, Wang D, Liu W, Spence JC, Bruce Doak R, Nelson G, Fromme P, Fromme R, Grotjohann I, Kupitz C, Zatsepin NA, Liu H, Basu S, Wacker D, Han GW, Katritch V, Boutet S, Messerschmidt M, Williams GJ, Koglin JE, Marvin Seibert M, Klinker M, Gati C, Shoeman RL, Barty A, Chapman HN, Kirian RA, Beyerlein KR, Stevens RC, Li D, Shah ST, Howe N, Caffrey M, Cherezov V 10.1038/NCOMMS4309 2014-03-05 Yes
P2Y12 P2Y12 P2Y A Human X-ray 4PXZ 4PXZ_refined 2.5 A Intermediate 36 84 - - - - BRIL - 2MeSADP PubChem Guide To Pharmacology ChEMBL_compound_ids Guide To Pharmacology
small-molecule Agonist ATP, ADP small-molecule Yes No Zhang J, Zhang K, Gao ZG, Paoletta S, Zhang D, Han GW, Li T, Ma L, Zhang W, Muller CE, Yang H, Jiang H, Cherezov V, Katritch V, Jacobson KA, Stevens RC, Wu B, Zhao Q 10.1038/NATURE13288 2014-04-30 Yes
SMO SMO Frizzled F Human X-ray 4QIM 4QIM_refined 2.6 A Inactive 8 45 - - - - BRIL - ANTA XV PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Antagonist - - No No Wang C, Wu H, Evron T, Vardy E, Han GW, Huang XP, Hufeisen SJ, Mangano TJ, Urban DJ, Katritch V, Cherezov V, Caron MG, Roth BL, Stevens RC 10.1038/NCOMMS5355 2014-07-23 Yes
ACM3 M3 Acetylcholine (muscarinic) A Rat X-ray 4U14 4U14_refined 3.6 A Inactive 3 47 - - - - T4-Lysozyme - tiotropium PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank Guide To Pharmacology
small-molecule Antagonist acetylcholine small-molecule Yes No Thorsen TS, Matt R, Weis WI, Kobilka BK 10.1016/J.STR.2014.08.022 2014-11-26 Yes
OPRD δ Opioid A Human X-ray 4RWD 4RWD_refined 2.7 A Inactive 5 79 - - - - BRIL - DIPP-NH2
peptide Antagonist [Leu]enkephalin, dynorphin A, dynorphin A-(1-8), dynorphin A-(1-13), endomorphin-1, dynorphin B, β-endorphin peptide Yes Yes Fenalti G, Zatsepin NA, Betti C, Giguere P, Han GW, Ishchenko A, Liu W, Guillemyn K, Zhang H, James D, Wang D, Weierstall U, Spence JC, Boutet S, Messerschmidt M, Williams GJ, Gati C, Yefanov OM, White TA, Oberthuer D, Metz M, Yoon CH, Barty A, Chapman HN, Basu S, Coe J, Conrad CE, Fromme R, Fromme P, Tourwe D, Schiller PW, Roth BL, Ballet S, Katritch V, Stevens RC, Cherezov V 10.1038/NSMB.2965 2015-01-14 Yes
US28 US28 Unclassified A strain AD169 X-ray 4XT3 4XT3_refined 3.8 A Active 100 81 - - - - - - CX3CL1 Guide To Pharmacology
peptide Agonist (partial) - - Yes No Burg JS, Ingram JR, Venkatakrishnan AJ, Jude KM, Dukkipati A, Feinberg EN, Angelini A, Waghray D, Dror RO, Ploegh HL, Garcia KC 10.1126/SCIENCE.AAA5026 2015-03-04 Yes
AA2AR A2A Adenosine A Human X-ray 4UG2 4UG2_refined 2.6 A Active 73 71 - - - - - - CGS 21680 PubChem Guide To Pharmacology ChEMBL_compound_ids Guide To Pharmacology
small-molecule Agonist adenosine small-molecule Yes No Lebon G, Edwards PC, Leslie AG, Tate CG 10.1124/mol.114.097360 2015-04-08 Yes
LPAR1 LPA1 Lysophospholipid (LPA) A Human X-ray 4Z36 4Z36_refined 2.9 A Inactive 1 79 - - - - BRIL - ONO-3080573 PubChem Guide To Pharmacology
small-molecule Antagonist 1-O-Oleoyl-D-glycerol 3-phosphoric acid small-molecule Yes No Chrencik JE, Roth CB, Terakado M, Kurata H, Omi R, Kihara Y, Warshaviak D, Nakade S, Asmar-Rovira G, Mileni M, Mizuno H, Griffith MT, Rodgers C, Han GW, Velasquez J, Chun J, Stevens RC, Hanson MA 10.1016/J.CELL.2015.06.002 2015-06-03 Yes
OPSD Rhodopsin Opsins A Human X-ray 4ZWJ 4ZWJ_refined 3.3 A Active 100 94 Visual S-arrestin - 86 T4-Lysozyme - Apo (no ligand)
none Apo (no ligand) - - No No Kang Y, Zhou XE, Gao X, He Y, Liu W, Ishchenko A, Barty A, White TA, Yefanov O, Han GW, Xu Q, de Waal PW, Ke J, Tan MH, Zhang C, Moeller A, West GM, Pascal BD, Van Eps N, Caro LN, Vishnivetskiy SA, Lee RJ, Suino-Powell KM, Gu X, Pal K, Ma J, Zhi X, Boutet S, Williams GJ, Messerschmidt M, Gati C, Zatsepin NA, Wang D, James D, Basu S, Roy-Chowdhury S, Conrad CE, Coe J, Liu H, Lisova S, Kupitz C, Grotjohann I, Fromme R, Jiang Y, Tan M, Yang H, Li J, Wang M, Zheng Z, Li D, Howe N, Zhao Y, Standfuss J, Diederichs K, Dong Y, Potter CS, Carragher B, Caffrey M, Jiang H, Chapman HN, Spence JC, Fromme P, Weierstall U, Ernst OP, Katritch V, Gurevich VV, Griffin PR, Hubbell WL, Stevens RC, Cherezov V, Melcher K, Xu HE 10.1038/NATURE14656 2015-07-29 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 4X1H 4X1H_refined 2.3 A Active 100 94 Gi/o αt1 Only H5 3 - - B-Nonylglucoside PubChem
small-molecule unknown - - No No Blankenship E, Vahedi-Faridi A, Lodowski DT 10.1016/J.STR.2015.09.015 2015-11-04 Yes
OX1R OX1 Orexin A Human X-ray 4ZJ8 4ZJ8_refined 2.8 A Inactive 1 72 - - - - GlgA glycogen synthase - suvorexant PubChem Guide To Pharmacology ChEMBL_compound_ids Drug Central DrugBank
small-molecule Antagonist orexin-B, orexin-A peptide No No Yin J, Babaoglu K, Brautigam CA, Clark L, Shao Z, Scheuermann TH, Harrell CM, Gotter AL, Roecker AJ, Winrow CJ, Renger JJ, Coleman PJ, Rosenbaum DM 10.1038/NSMB.3183 2016-03-09 Yes
OPSD Rhodopsin Opsins A Human X-ray 5DGY 5DGY_refined 7.7 A Active 100 94 Visual S-arrestin - 86 T4-Lysozyme - Apo (no ligand)
none Apo (no ligand) - - No No Zhou XE, Gao X, Barty A, Kang Y, He Y, Liu W, Ishchenko A, White TA, Yefanov O, Han GW, Xu Q, de Waal PW, Suino-Powell KM, Boutet S, Williams GJ, Wang M, Li D, Caffrey M, Chapman HN, Spence JC, Fromme P, Weierstall U, Stevens RC, Cherezov V, Melcher K, Xu HE 10.1038/SDATA.2016.21 2016-03-23 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 5JQH 5JQH_refined 3.2 A Inactive 0 70 - - - - T4-Lysozyme Nanobody Carazolol PubChem
small-molecule Inverse agonist noradrenaline, L-NOREPINEPHRINE, Zn2+, (-)-adrenaline, (-)-noradrenaline small-molecule Yes No Staus DP, Strachan RT, Manglik A, Pani B, Kahsai AW, Kim TH, Wingler LM, Ahn S, Chatterjee A, Masoudi A, Kruse AC, Pardon E, Steyaert J, Weis WI, Prosser RS, Kobilka BK, Costa T, Lefkowitz RJ 10.1038/NATURE18636 2016-07-13 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 5DYS 5DYS_refined 2.3 A Active 99 94 - - - - - - Retinal (all-trans) PubChem
small-molecule Agonist - - No No Singhal A, Guo Y, Matkovic M, Schertler G, Deupi X, Yan EC, Standfuss J 10.15252/EMBR.201642671 2016-08-10 Yes
EDNRB ETB Endothelin A Human X-ray 5GLI 5GLI_refined 2.5 A Inactive 4 71 - - - - T4-Lysozyme - Apo (no ligand)
none Apo (no ligand) endothelin-2, endothelin-3, endothelin-1 peptide Yes No Shihoya W, Nishizawa T, Okuta A, Tani K, Dohmae N, Fujiyoshi Y, Nureki O, Doi T 10.1038/nature19319 2016-09-07 Yes
AA2AR A2A Adenosine A Human X-ray 5K2C 5K2C_refined 1.9 A Inactive 1 72 - - - - BRIL - ZM-241385 PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank
small-molecule Antagonist adenosine small-molecule Yes Yes Batyuk A, Galli L, Ishchenko A, Han GW, Gati C, Popov PA, Lee MY, Stauch B, White TA, Barty A, Aquila A, Hunter MS, Liang M, Boutet S, Pu M, Liu ZJ, Nelson G, James D, Li C, Zhao Y, Spence JC, Liu W, Fromme P, Katritch V, Weierstall U, Stevens RC, Cherezov V 10.1126/SCIADV.1600292 2016-09-21 Yes
CNR1 CB1 Cannabinoid A Human X-ray 5U09 5U09_refined 2.6 A Inactive 8 60 - - - - Glycogen synthase - taranabant PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank
small-molecule Inverse agonist 2-arachidonoylglycerol, anandamide small-molecule Yes No Shao Z, Yin J, Chapman K, Grzemska M, Clark L, Wang J, Rosenbaum DM 10.1038/NATURE20613 2016-12-07 Yes
AA2AR A2A Adenosine A Human X-ray 5UIG 5UIG_refined 3.5 A Inactive 16 70 - - - - BRIL - 5-Amino-N-[(2-Methoxyphenyl)methyl]-2-(3-Methylphenyl)-2h-1,2,3-Triazole-4-Carboximidamide PubChem
small-molecule Antagonist adenosine small-molecule Yes No Sun B, Bachhawat P, Chu ML, Wood M, Ceska T, Sands ZA, Mercier J, Lebon F, Kobilka TS, Kobilka BK 10.1073/PNAS.1621423114 2017-02-08 Yes
AGTR2 AT2 Angiotensin A Human X-ray 5UNF 5UNF_refined 2.8 A Active 99 79 - - - - BRIL - compound 1 [PMID: 28379944] PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Antagonist angiotensin III, angiotensin II, angiotensin-(1-7) peptide Yes No Zhang H, Han GW, Batyuk A, Ishchenko A, White KL, Patel N, Sadybekov A, Zamlynny B, Rudd MT, Hollenstein K, Tolstikova A, White TA, Hunter MS, Weierstall U, Liu W, Babaoglu K, Moore EL, Katz RD, Shipman JM, Garcia-Calvo M, Sharma S, Sheth P, Soisson SM, Stevens RC, Katritch V, Cherezov V 10.1038/NATURE22035 2017-04-05 Yes
PAR2 PAR2 Proteinase-activated A Human X-ray 5NDZ 5NDZ_refined 3.6 A Intermediate 36 74 - - - - BRIL - AZ3451 PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Allosteric antagonist - - Yes Yes Cheng RKY, Fiez-Vandal C, Schlenker O, Edman K, Aggeler B, Brown DG, Brown GA, Cooke RM, Dumelin CE, Dore AS, Geschwindner S, Grebner C, Hermansson NO, Jazayeri A, Johansson P, Leong L, Prihandoko R, Rappas M, Soutter H, Snijder A, Sundstrom L, Tehan B, Thornton P, Troast D, Wiggin G, Zhukov A, Marshall FH, Dekker N 10.1038/NATURE22309 2017-05-03 Yes
AA2AR A2A Adenosine A Human X-ray 5UVI 5UVI_refined 3.2 A Inactive 1 72 - - - - BRIL - ZM-241385 PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank
small-molecule Antagonist adenosine small-molecule Yes No Martin-Garcia JM, Conrad CE, Nelson G, Stander N, Zatsepin NA, Zook J, Zhu L, Geiger J, Chun E, Kissick D, Hilgart MC, Ogata C, Ishchenko A, Nagaratnam N, Roy-Chowdhury S, Coe J, Subramanian G, Schaffer A, James D, Ketwala G, Venugopalan N, Xu S, Corcoran S, Ferguson D, Weierstall U, Spence JCH, Cherezov V, Fromme P, Fischetti RF, Liu W 10.1107/S205225251700570X 2017-05-24 Yes
SMO SMO Frizzled F Human X-ray 5V57 5V57_refined 3.0 A Inactive 1 62 - - - - Flavodoxin - N-methyl-N-[1-[4-(2-methylpyrazol-3-yl)phthalazin-1-yl]piperidin-4-yl]-4-nitro-2-(trifluoromethyl)benzamide PubChem
small-molecule Antagonist - - No No Zhang X, Zhao F, Wu Y, Yang J, Han GW, Zhao S, Ishchenko A, Ye L, Lin X, Ding K, Dharmarajan V, Griffin PR, Gati C, Nelson G, Hunter MS, Hanson MA, Cherezov V, Stevens RC, Tan W, Tao H, Xu F 10.1038/NCOMMS15383 2017-05-24 Yes
AA2AR A2A Adenosine A Human X-ray 5JTB 5JTB_refined 2.8 A Inactive 1 72 - - - - BRIL - ZM-241385 PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank
small-molecule Antagonist adenosine small-molecule Yes No Melnikov I, Polovinkin V, Kovalev K, Gushchin I, Shevtsov M, Shevchenko V, Mishin A, Alekseev A, Rodriguez-Valera F, Borshchevskiy V, Cherezov V, Leonard GA, Gordeliy V, Popov A 10.1126/SCIADV.1602952 2017-05-31 Yes
FFAR1 FFA1 Free fatty acid A Human X-ray 5TZY 5TZY_refined 3.2 A Intermediate 46 91 - - - - T4-Lysozyme - MK-8666 PubChem
(2S,3R)-3-Cyclopropyl-3-[(2R)-2-[1-[(1S)-1-[5-fluoro-2-(trifluoromethoxy)phenyl]ethyl]piperidin-4-yl]-3,4-dihydro-2H-chromen-7-yl]-2-methylpropanoic acid PubChem
small-molecule
small-molecule		 Agonist
PAM		 oleic acid, α-linolenic acid, docosahexaenoic acid, myristic acid small-molecule No No Lu J, Byrne N, Wang J, Bricogne G, Brown FK, Chobanian HR, Colletti SL, Di Salvo J, Thomas-Fowlkes B, Guo Y, Hall DL, Hadix J, Hastings NB, Hermes JD, Ho T, Howard AD, Josien H, Kornienko M, Lumb KJ, Miller MW, Patel SB, Pio B, Plummer CW, Sherborne BS, Sheth P, Souza S, Tummala S, Vonrhein C, Webb M, Allen SJ, Johnston JM, Weinglass AB, Sharma S, Soisson SM 10.1038/NSMB.3417 2017-06-07 Yes
CNR1 CB1 Cannabinoid A Human X-ray 5XRA 5XRA_refined 2.8 A Active 97 60 - - - - Flavodoxin - AM11542 PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Agonist 2-arachidonoylglycerol, anandamide small-molecule Yes No Hua T, Vemuri K, Nikas SP, Laprairie RB, Wu Y, Qu L, Pu M, Korde A, Jiang S, Ho JH, Han GW, Ding K, Li X, Liu H, Hanson MA, Zhao S, Bohn LM, Makriyannis A, Stevens RC, Liu ZJ 10.1038/NATURE23272 2017-07-12 Yes
AA2AR A2A Adenosine A Human X-ray 5N2R 5N2R_refined 2.8 A Inactive 1 71 - - - - BRIL - PSB36 PubChem
small-molecule Antagonist adenosine small-molecule Yes Yes Cheng RKY, Segala E, Robertson N, Deflorian F, Dore AS, Errey JC, Fiez-Vandal C, Marshall FH, Cooke RM 10.1016/j.str.2017.06.012 2017-07-26 Yes
EDNRB ETB Endothelin A Human X-ray 5X93 5X93_refined 2.2 A Inactive 4 71 - - - - T4-Lysozyme - K-8794 PubChem Guide To Pharmacology
small-molecule Antagonist endothelin-2, endothelin-3, endothelin-1 peptide Yes No Shihoya W, Nishizawa T, Yamashita K, Inoue A, Hirata K, Kadji FMN, Okuta A, Tani K, Aoki J, Fujiyoshi Y, Doi T, Nureki O 10.1038/NSMB.3450 2017-08-16 Yes
Q08BG4 LPA6 Lysophospholipid (LPA) A Zebrafish X-ray 5XSZ 5XSZ_refined 3.2 A Intermediate 36 78 - - - - T4-Lysozyme - - - - - - Yes No Taniguchi R, Inoue A, Sayama M, Uwamizu A, Yamashita K, Hirata K, Yoshida M, Tanaka Y, Kato HE, Nakada-Nakura Y, Otani Y, Nishizawa T, Doi T, Ohwada T, Ishitani R, Aoki J, Nureki O 10.1038/NATURE23448 2017-08-16 Yes
AA2AR A2A Adenosine A Human X-ray 5NM4 5NM4_refined 1.7 A Inactive 1 73 - - - - BRIL - ZM-241385 PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank
small-molecule Antagonist adenosine small-molecule Yes No Weinert T, Olieric N, Cheng R, Brunle S, James D, Ozerov D, Gashi D, Vera L, Marsh M, Jaeger K, Dworkowski F, Panepucci E, Basu S, Skopintsev P, Dore AS, Geng T, Cooke RM, Liang M, Prota AE, Panneels V, Nogly P, Ermler U, Schertler G, Hennig M, Steinmetz MO, Wang M, Standfuss J 10.1038/S41467-017-00630-4 2017-09-27 Yes
AA2AR A2A Adenosine A Human X-ray 5VRA 5VRA_refined 2.4 A Inactive 1 72 - - - - BRIL - ZM-241385 PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank
small-molecule Antagonist adenosine small-molecule Yes Yes Broecker J, Morizumi T, Ou WL, Klingel V, Kuo A, Kissick DJ, Ishchenko A, Lee MY, Xu S, Makarov O, Cherezov V, Ogata CM, Ernst OP 10.1038/NPROT.2017.135 2017-12-13 Yes
AA2AR A2A Adenosine A Human X-ray 6AQF 6AQF_refined 2.5 A Inactive 1 72 - - - - BRIL - ZM-241385 PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank
small-molecule Antagonist adenosine small-molecule Yes No Eddy MT, Lee MY, Gao ZG, White KL, Didenko T, Horst R, Audet M, Stanczak P, McClary KM, Han GW, Jacobson KA, Stevens RC, Wuthrich K 10.1016/J.CELL.2017.12.004 2018-01-10 Yes
AA2AR A2A Adenosine A Human X-ray 5OLV 5OLV_refined 2.0 A Inactive 1 72 - - - - BRIL - CHEMBL1671936 ChEMBL_compound_ids PubChem
small-molecule Antagonist adenosine small-molecule Yes Yes Rucktooa P, Cheng RKY, Segala E, Geng T, Errey JC, Brown GA, Cooke RM, Marshall FH, Dore AS 10.1038/S41598-017-18570-W 2018-01-17 Yes
GLR glucagon Glucagon B1 Human X-ray 5YQZ 5YQZ_refined 3.0 R Inactive 3 83 - - - - T4-Lysozyme - NNC1702 Guide To Pharmacology
peptide Agonist (partial) glucagon peptide No No Zhang H, Qiao A, Yang L, Van Eps N, Frederiksen KS, Yang D, Dai A, Cai X, Zhang H, Yi C, Cao C, He L, Yang H, Lau J, Ernst OP, Hanson MA, Stevens RC, Wang MW, Reedtz-Runge S, Jiang H, Zhao Q, Wu B 10.1038/NATURE25153 2018-01-17 Yes
AA2AR A2A Adenosine A Human X-ray 5WF6 5WF6_refined 2.9 A Active 73 68 - - - - T4-Lysozyme - UK-432,097 PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank
small-molecule Agonist adenosine small-molecule No No White KL, Eddy MT, Gao ZG, Han GW, Lian T, Deary A, Patel N, Jacobson KA, Katritch V, Stevens RC 10.1016/J.STR.2017.12.013 2018-02-21 Yes
GRM5 mGlu5 Metabotropic glutamate C Human X-ray 6FFI - 2.2 A Inactive 20 20 - - - - T4-Lysozyme - methoxy-MPEP PubChem Guide To Pharmacology ChEMBL_compound_ids Guide To Pharmacology
small-molecule NAM L-glutamic acid small-molecule No No Christopher JA, Orgovan Z, Congreve M, Dore AS, Errey JC, Marshall FH, Mason JS, Okrasa K, Rucktooa P, Serrano-Vega MJ, Ferenczy GG, Keseru GM 10.1021/ACS.JMEDCHEM.7B01722 2018-03-07 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 6FK7 6FK7_refined 2.6 A Active 99 94 - - - - - - (2~{S})-2-(4-chlorophenyl)-3-methyl-1-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-yl-butan-1-one PubChem
small-molecule Agonist - - No No Mattle D, Kuhn B, Aebi J, Bedoucha M, Kekilli D, Grozinger N, Alker A, Rudolph MG, Schmid G, Schertler GFX, Hennig M, Standfuss J, Dawson RJP 10.1073/PNAS.1718084115 2018-04-04 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 6FKB 6FKB_refined 3.0 A Active 99 94 - - - - - - 2-(4-Chlorophenyl)-1-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-yl-ethanone PubChem
small-molecule Agonist - - No No Mattle D, Kuhn B, Aebi J, Bedoucha M, Kekilli D, Grozinger N, Alker A, Rudolph MG, Schmid G, Schertler GFX, Hennig M, Standfuss J, Dawson RJP 10.1073/PNAS.1718084115 2018-04-04 Yes
NPY1R Y1 Neuropeptide Y A Human X-ray 5ZBQ 5ZBQ_refined 2.7 A Inactive 1 80 - - - - T4-Lysozyme - CHEMBL3747822 ChEMBL_compound_ids ChEMBL_compound_ids ChEMBL_compound_ids PubChem
small-molecule Antagonist neuropeptide Y, pancreatic polypeptide, peptide YY peptide Yes No Yang Z, Han S, Keller M, Kaiser A, Bender BJ, Bosse M, Burkert K, Kogler LM, Wifling D, Bernhardt G, Plank N, Littmann T, Schmidt P, Yi C, Li B, Ye S, Zhang R, Xu B, Larhammar D, Stevens RC, Huster D, Meiler J, Zhao Q, Beck-Sickinger AG, Buschauer A, Wu B 10.1038/S41586-018-0046-X 2018-04-25 Yes
Q98SW5 SMO Frizzled F African clawed frog X-ray 6D35 6D35_refined 3.9 A Active 87 58 - - - - BRIL - Cholesterol PubChem
small-molecule Agonist - - No No Huang P, Zheng S, Wierbowski BM, Kim Y, Nedelcu D, Aravena L, Liu J, Kruse AC, Salic A 10.1016/J.CELL.2018.04.029 2018-05-23 Yes
OPRM μ Opioid A Mouse cryo-EM 6DDE 6DDE_refined 3.5 R Active 100 71 Gi/o αi1 - 61 - Antibody DAMGO PubChem Guide To Pharmacology ChEMBL_compound_ids ChEMBL_compound_ids
peptide Agonist - - Yes No Koehl A, Hu H, Maeda S, Zhang Y, Qu Q, Paggi JM, Latorraca NR, Hilger D, Dawson R, Matile H, Schertler GFX, Granier S, Weis WI, Dror RO, Manglik A, Skiniotis G, Kobilka BK 10.1038/S41586-018-0219-7 2018-06-13 Yes
PTAFR PAF Platelet-activating factor A Human X-ray 5ZKQ 5ZKQ_refined 2.9 B Intermediate 36 83 - - - - T4-Lysozyme - ABT-491 PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Inverse agonist PAF, methylcarbamyl PAF small-molecule Yes No Cao C, Tan Q, Xu C, He L, Yang L, Zhou Y, Zhou Y, Qiao A, Lu M, Yi C, Han GW, Wang X, Li X, Yang H, Rao Z, Jiang H, Zhao Y, Liu J, Stevens RC, Zhao Q, Zhang XC, Wu B 10.1038/S41594-018-0068-Y 2018-06-20 Yes
AGTR2 AT2 Angiotensin A Human X-ray 5XJM 5XJM_refined 3.2 A Active 99 78 - - - - BRIL Fab SI PubChem ChEMBL_compound_ids
small-molecule Agonist angiotensin III, angiotensin II, angiotensin-(1-7) peptide Yes No Asada H, Horita S, Hirata K, Shiroishi M, Shiimura Y, Iwanari H, Hamakubo T, Shimamura T, Nomura N, Kusano-Arai O, Uemura T, Suno C, Kobayashi T, Iwata S 10.1038/S41594-018-0079-8 2018-07-11 Yes
5HT2B 5-HT2B 5-Hydroxytryptamine A Human X-ray 6DS0 6DS0_refined 3.2 A Intermediate 36 59 - - - - BRIL - LY266097 PubChem
small-molecule Antagonist 5-hydroxytryptamine small-molecule Yes No McCorvy JD, Wacker D, Wang S, Agegnehu B, Liu J, Lansu K, Tribo AR, Olsen RHJ, Che T, Jin J, Roth BL 10.1038/s41594-018-0116-7 2018-08-29 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 6FUF 6FUF_refined 3.1 A Active 100 91 Gi/o αo Mini-Go 51 - - Retinal (all-trans) PubChem
small-molecule Agonist - - No No Tsai CJ, Pamula F, Nehme R, Muhle J, Weinert T, Flock T, Nogly P, Edwards PC, Carpenter B, Gruhl T, Ma P, Deupi X, Standfuss J, Tate CG, Schertler GFX 10.1126/SCIADV.AAT7052 2018-10-03 Yes
ADRB1 β1 Adrenoceptors A Wild turkey X-ray 6H7M 6H7M_refined 2.8 A Active 100 60 - - - - Thioredoxin 1 Camelid antibody fragment Nb6B9 levosalbutamol PubChem Guide To Pharmacology ChEMBL_compound_ids Drug Central DrugBank
small-molecule Agonist - - Yes No Warne T, Edwards PC, Dore AS, Leslie AGW, Tate CG 10.1126/SCIENCE.AAU5595 2018-10-17 Yes
CCR5 CCR5 Chemokine A Human X-ray 6AKY 6AKY_refined 2.8 A Inactive 12 81 - - - - Rubredoxin - CCR5 antagonist 34 PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Antagonist CCL2, CCL4, CCL11, CCL7, CCL8, CCL5, CCL14, CCL16, CCL3, CCL13 peptide No No Peng P, Chen H, Zhu Y, Wang Z, Li J, Luo RH, Wang J, Chen L, Yang LM, Jiang H, Xie X, Wu B, Zheng YT, Liu H 10.1021/ACS.JMEDCHEM.8B01077 2018-10-24 Yes
ACM2 M2 Acetylcholine (muscarinic) A Human X-ray 5YC8 5YC8_refined 2.5 A Inactive 3 60 - - - - BRIL - N-methyl scopolamine PubChem Guide To Pharmacology DrugBank Guide To Pharmacology
small-molecule Antagonist acetylcholine small-molecule No No Suno R, Lee S, Maeda S, Yasuda S, Yamashita K, Hirata K, Horita S, Tawaramoto MS, Tsujimoto H, Murata T, Kinoshita M, Yamamoto M, Kobilka BK, Vaidehi N, Iwata S, Kobayashi T 10.1038/S41589-018-0152-Y 2018-11-21 Yes
ACM2 M2 Acetylcholine (muscarinic) A Human X-ray 5ZKB 5ZKB_refined 3.0 A Inactive 3 60 - - - - BRIL - AF-DX 384 PubChem
small-molecule Antagonist acetylcholine small-molecule No No Suno R, Lee S, Maeda S, Yasuda S, Yamashita K, Hirata K, Horita S, Tawaramoto MS, Tsujimoto H, Murata T, Kinoshita M, Yamamoto M, Kobilka BK, Vaidehi N, Iwata S, Kobayashi T 10.1038/S41589-018-0152-Y 2018-11-21 Yes
ACM3 M3 Acetylcholine (muscarinic) A Rat X-ray 5ZHP 5ZHP_refined 3.1 B Inactive 3 47 - - - - T4-Lysozyme - (1R,2R,4S,5S,7s)-7-({[4-fluoro-2-(thiophen-2-yl)phenyl]carbamoyl}oxy)-9,9-dimethyl-3-oxa-9-azatricyclo[3.3.1.0~2,4~]nonan-9-ium PubChem
small-molecule Antagonist acetylcholine small-molecule No No Liu H, Hofmann J, Fish I, Schaake B, Eitel K, Bartuschat A, Kaindl J, Rampp H, Banerjee A, Hubner H, Clark MJ, Vincent SG, Fisher JT, Heinrich MR, Hirata K, Liu X, Sunahara RK, Shoichet BK, Kobilka BK, Gmeiner P 10.1073/PNAS.1813988115 2018-11-28 Yes
PE2R3 EP3 Prostanoid A Human X-ray 6M9T 6M9T_refined 2.5 A Active 83 70 - - - - T4-Lysozyme - Misoprostol-FA PubChem
small-molecule Agonist PGI2, PGE1, PGD2, PGE2, thromboxane A2, PGF2α small-molecule Yes No Audet M, White KL, Breton B, Zarzycka B, Han GW, Lu Y, Gati C, Batyuk A, Popov P, Velasquez J, Manahan D, Hu H, Weierstall U, Liu W, Shui W, Katritch V, Cherezov V, Hanson MA, Stevens RC 10.1038/S41589-018-0160-Y 2018-12-05 Yes
CCR5 CCR5 Chemokine A Human cryo-EM 6MET 6MET_refined 4.5 B Inactive 13 89 - - - - - T-cell surface glycoprotein CD4 Envelope glycoprotein gp160
protein Antagonist CCL2, CCL4, CCL11, CCL7, CCL8, CCL5, CCL14, CCL16, CCL3, CCL13 peptide No No Shaik MM, Peng H, Lu J, Rits-Volloch S, Xu C, Liao M, Chen B 10.1038/S41586-018-0804-9 2018-12-12 Yes
EDNRB ETB Endothelin A Human X-ray 6K1Q 6K1Q_refined 2.7 A Inactive 4 68 - - - - T4-Lysozyme - IRL 2500 PubChem Guide To Pharmacology ChEMBL_compound_ids
peptide Inverse agonist endothelin-2, endothelin-3, endothelin-1 peptide Yes No Nagiri C, Shihoya W, Inoue A, Kadji FMN, Aoki J, Nureki O 10.1038/S42003-019-0482-7 2019-07-17 Yes
SUCR1 succinate Succinate A Rat X-ray 6IBB 6IBB_refined 2.1 A Intermediate 36 93 - - - - - Nanobody-6 - - - - - Yes No Haffke M, Fehlmann D, Rummel G, Boivineau J, Duckely M, Gommermann N, Cotesta S, Sirockin F, Freuler F, Littlewood-Evans A, Kaupmann K, Jaakola VP 10.1038/S41586-019-1663-8 2019-08-14 Yes
OPSD Rhodopsin Opsins A Bovine cryo-EM 6OFJ 6OFJ_refined 4.5 A Inactive 22 93 - - - - - - Apo (no ligand)
none Apo (no ligand) - - No No Zhao DY, Poge M, Morizumi T, Gulati S, Van Eps N, Zhang J, Miszta P, Filipek S, Mahamid J, Plitzko JM, Baumeister W, Ernst OP, Palczewski K 10.1074/JBC.RA119.010089 2019-08-21 Yes
CLTR1 CysLT1 Leukotriene A Human X-ray 6RZ4 6RZ4_refined 2.7 A Intermediate 36 85 - - - - BRIL - pranlukast PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank Drug Central
small-molecule Antagonist LTC4, LTD4, LTE4 small-molecule Yes Yes Luginina A, Gusach A, Marin E, Mishin A, Brouillette R, Popov P, Shiriaeva A, Besserer-Offroy E, Longpre JM, Lyapina E, Ishchenko A, Patel N, Polovinkin V, Safronova N, Bogorodskiy A, Edelweiss E, Hu H, Weierstall U, Liu W, Batyuk A, Gordeliy V, Han GW, Sarret P, Katritch V, Borshchevskiy V, Cherezov V 10.1126/SCIADV.AAX2518 2019-10-30 Yes
GLP1R GLP-1 Glucagon B1 Human X-ray 6KK7 6KK7_refined 3.1 B Inactive 0 56 - - - - T4-Lysozyme - PF-06372222 PubChem
small-molecule NAM glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon peptide No No Xu Y, Wang Y, Wang Y, Liu K, Peng Y, Yao D, Tao H, Liu H, Song G 10.1107/S2052252519013496 2019-11-13 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 6PS2 6PS2_refined 2.4 A Inactive 0 68 - - - - T4-Lysozyme - CHEMBL1160734 ChEMBL_compound_ids PubChem
small-molecule Antagonist noradrenaline, L-NOREPINEPHRINE, Zn2+, (-)-adrenaline, (-)-noradrenaline small-molecule Yes No Ishchenko A, Stauch B, Han GW, Batyuk A, Shiriaeva A, Li C, Zatsepin N, Weierstall U, Liu W, Nango E, Nakane T, Tanaka R, Tono K, Joti Y, Iwata S, Moraes I, Gati C, Cherezov V 10.1107/S2052252519013137 2019-11-13 Yes
ADRB2 β2 Adrenoceptors A Human X-ray 6PS6 6PS6_refined 2.7 A Inactive 0 68 - - - - T4-Lysozyme - timolol PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank Drug Central
small-molecule Antagonist noradrenaline, L-NOREPINEPHRINE, Zn2+, (-)-adrenaline, (-)-noradrenaline small-molecule Yes No Ishchenko A, Stauch B, Han GW, Batyuk A, Shiriaeva A, Li C, Zatsepin N, Weierstall U, Liu W, Nango E, Nakane T, Tanaka R, Tono K, Joti Y, Iwata S, Moraes I, Gati C, Cherezov V 10.1107/S2052252519013137 2019-11-13 Yes
DRD4 D4 Dopamine A Mouse X-ray 6IQL 6IQL_refined 3.5 A Inactive 83 65 - - - - BRIL - L745870 PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Antagonist - - Yes No Zhou Y, Cao C, He L, Wang X, Zhang XC 10.7554/ELIFE.48822 2019-12-04 Yes
ADA2A α2A Adrenoceptors A Human X-ray 6KUY 6KUY_refined 3.2 A Inactive 1 56 - - - - BRIL - (2~{S})-4-fluoranyl-2-(1~{H}-imidazol-5-yl)-1-propan-2-yl-2,3-dihydroindole PubChem
small-molecule Agonist (partial) (-)-adrenaline, (-)-noradrenaline small-molecule Yes No - - 2019-12-04 Yes
OPRD δ Opioid A Human X-ray 6PT3 6PT3_refined 3.3 A Active 73 78 - - - - BRIL - DPI-287 PubChem
small-molecule Agonist [Leu]enkephalin, dynorphin A, dynorphin A-(1-8), dynorphin A-(1-13), endomorphin-1, dynorphin B, β-endorphin peptide No No Claff T, Yu J, Blais V, Patel N, Martin C, Wu L, Han GW, Holleran BJ, Van der Poorten O, White KL, Hanson MA, Sarret P, Gendron L, Cherezov V, Katritch V, Ballet S, Liu ZJ, Muller CE, Stevens RC 10.1126/SCIADV.AAX9115 2019-12-11 Yes
CLTR2 CysLT2 Leukotriene A Human X-ray 6RZ9 6RZ9_refined 2.7 A Intermediate 36 81 - - - - BRIL - ONO-2770372 PubChem
small-molecule Antagonist LTC4, LTD4, LTE4 small-molecule No No Gusach A, Luginina A, Marin E, Brouillette RL, Besserer-Offroy E, Longpre JM, Ishchenko A, Popov P, Patel N, Fujimoto T, Maruyama T, Stauch B, Ergasheva M, Romanovskaia D, Stepko A, Kovalev K, Shevtsov M, Gordeliy V, Han GW, Katritch V, Borshchevskiy V, Sarret P, Mishin A, Cherezov V 10.1038/S41467-019-13348-2 2019-12-11 Yes
OX1R OX1 Orexin A Human X-ray 6TP4 6TP4_refined 3.0 A Inactive 1 70 - - - - - - ACT-462206 PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Antagonist orexin-B, orexin-A peptide No No Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Dore AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA 10.1021/ACS.JMEDCHEM.9B01787 2020-01-01 Yes
OX2R OX2 Orexin A Human X-ray 6TPJ 6TPJ_refined 2.7 A Inactive 1 68 - - - - GlgA glycogen synthase - suvorexant PubChem Guide To Pharmacology ChEMBL_compound_ids Drug Central DrugBank
small-molecule Antagonist orexin-B, orexin-A peptide No No Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Dore AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA 10.1021/ACS.JMEDCHEM.9B01787 2020-01-01 Yes
OX1R OX1 Orexin A Human X-ray 6TQ9 6TQ9_refined 2.7 B Inactive 1 71 - - - - - - SB-408124 PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Antagonist orexin-B, orexin-A peptide No No Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Dore AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA 10.1021/ACS.JMEDCHEM.9B01787 2020-01-01 Yes
OX1R OX1 Orexin A Human X-ray 6TOT 6TOT_refined 2.2 B Inactive 1 71 - - - - - - lemborexant PubChem Guide To Pharmacology ChEMBL_compound_ids Drug Central DrugBank
small-molecule Antagonist orexin-B, orexin-A peptide No No Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Dore AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA 10.1021/ACS.JMEDCHEM.9B01787 2020-01-15 Yes
CNR2 CB2 Cannabinoid A Human X-ray 6KPC 6KPC_refined 3.2 A Inactive 8 79 - - - - T4-Lysozyme - AM841 PubChem Guide To Pharmacology
small-molecule Agonist 2-arachidonoylglycerol, anandamide small-molecule Yes No Hua T, Li X, Wu L, Iliopoulos-Tsoutsouvas C, Wang Y, Wu M, Shen L, Brust CA, Nikas SP, Song F, Song X, Yuan S, Sun Q, Wu Y, Jiang S, Grim TW, Benchama O, Stahl EL, Zvonok N, Zhao S, Bohn LM, Makriyannis A, Liu ZJ 10.1016/J.CELL.2020.01.008 2020-02-12 Yes
CNR2 CB2 Cannabinoid A Human cryo-EM 6KPF 6KPF_refined 2.9 R Active 100 81 Gi/o αi1 - 62 - scFv16 AM841 PubChem Guide To Pharmacology
small-molecule Agonist 2-arachidonoylglycerol, anandamide small-molecule Yes No Hua T, Li X, Wu L, Iliopoulos-Tsoutsouvas C, Wang Y, Wu M, Shen L, Brust CA, Nikas SP, Song F, Song X, Yuan S, Sun Q, Wu Y, Jiang S, Grim TW, Benchama O, Stahl EL, Zvonok N, Zhao S, Bohn LM, Makriyannis A, Liu ZJ 10.1016/J.CELL.2020.01.008 2020-02-12 Yes
CRFR1 CRF1 Corticotropin-releasing factor B1 Human cryo-EM 6PB0 6PB0_refined 3.0 R Active 100 68 Gs αs Gs-Gi1 chimera 58 - Nanobody-35 CHEMBL427807 ChEMBL_compound_ids PubChem
protein Agonist urocortin 2, corticotrophin-releasing hormone, urocortin 1 peptide No No Ma S, Shen Q, Zhao LH, Mao C, Zhou XE, Shen DD, de Waal PW, Bi P, Li C, Jiang Y, Wang MW, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE 10.1016/J.MOLCEL.2020.01.013 2020-02-12 Yes
AGTR1 AT1 Angiotensin A Human X-ray 6OS2 6OS2_refined 2.7 A Active 91 85 - - - - BRIL Nanobody-Nb.AT110i1_le TRV026 PubChem Guide To Pharmacology ChEMBL_compound_ids
peptide Agonist angiotensin III, angiotensin IV, angiotensin II, angiotensin A peptide Yes No Wingler LM, Skiba MA, McMahon C, Staus DP, Kleinhenz ALW, Suomivuori CM, Latorraca NR, Dror RO, Lefkowitz RJ, Kruse AC 10.1126/SCIENCE.AAY9813 2020-02-19 Yes
ACM2 M2 Acetylcholine (muscarinic) A Human cryo-EM 6U1N 6U1N_refined 4.0 R Active 100 57 Beta Beta-arrestin-1 - 86 - Fab30 light chain
Fab30 heavy chain		 LY2119620 PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Agonist acetylcholine small-molecule Yes No Staus DP, Hu H, Robertson MJ, Kleinhenz ALW, Wingler LM, Capel WD, Latorraca NR, Lefkowitz RJ, Skiniotis G 10.1038/S41586-020-1954-0 2020-02-26 Yes
ACM4 M4 Acetylcholine (muscarinic) A Human X-ray 6KP6 6KP6_refined 3.0 A Inactive 3 59 - - - - GlgA glycogen synthase - - - - acetylcholine small-molecule Yes No Wang J, Wu M, Wu L, Xu Y, Li F, Wu Y, Popov P, Wang L, Bai F, Zhao S, Liu ZJ, Hua T 10.1107/S2052252520000597 2020-03-11 Yes
GLP1R GLP-1 Glucagon B1 Human X-ray 6LN2 6LN2_refined 3.2 A Inactive 0 83 - - - - - Fab7F38 light chain
Fab7F38 heavy chain		 PF-06372222 PubChem
small-molecule NAM glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon peptide No No Wu F, Yang L, Hang K, Laursen M, Wu L, Han GW, Ren Q, Roed NK, Lin G, Hanson MA, Jiang H, Wang MW, Reedtz-Runge S, Song G, Stevens RC 10.1038/S41467-020-14934-5 2020-03-18 Yes
OPRK κ Opioid A Human X-ray 6VI4 6VI4_refined 3.3 B Inactive 5 73 - - - - - Nanobody-6 JDTic PubChem Guide To Pharmacology ChEMBL_compound_ids
small-molecule Antagonist dynorphin A, dynorphin A-(1-8), dynorphin A-(1-13), β-neoendorphin, big dynorphin, dynorphin B, α-neoendorphin, β-endorphin peptide Yes No Che T, English J, Krumm BE, Kim K, Pardon E, Olsen RHJ, Wang S, Zhang S, Diberto JF, Sciaky N, Carroll FI, Steyaert J, Wacker D, Roth BL 10.1038/S41467-020-14889-7 2020-03-18 Yes
CALRL calcitonin-like Calcitonin B1 Human cryo-EM 6UUN 6UUN_refined 3.0 R Active 100 77 Gs αs - 48 - Nanobody-35
RAMP2		 Adrenomedullin PubChem
peptide Agonist - - No No Liang YL, Belousoff MJ, Fletcher MM, Zhang X, Khoshouei M, Deganutti G, Koole C, Furness SGB, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Danev R, Wootten D, Sexton PM 10.1021/ACSPTSCI.9B00080 2020-03-25 Yes
CALRL calcitonin-like Calcitonin B1 Human cryo-EM 6UVA 6UVA_refined 2.3 R Active 100 75 Gs αs - 48 - Nanobody-35
RAMP3		 adrenomedullin 2/intermedin Guide To Pharmacology
peptide Agonist - - No No Liang YL, Belousoff MJ, Fletcher MM, Zhang X, Khoshouei M, Deganutti G, Koole C, Furness SGB, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Danev R, Wootten D, Sexton PM 10.1021/ACSPTSCI.9B00080 2020-04-01 Yes
GABR2 GABAB2 GABAB C Human cryo-EM 6UOA 6UOA_refined 6.3 B Inactive 3 71 - - - - - - CHEMBL112710 ChEMBL_compound_ids PubChem PubChem
small-molecule Agonist - - No No Shaye H, Ishchenko A, Lam JH, Han GW, Xue L, Rondard P, Pin JP, Katritch V, Gati C, Cherezov V 10.1038/S41586-020-2408-4 2020-06-10 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 6PEL 6PEL_refined 3.2 A Active 100 93 Gi/o αt1 Only H5 3 - - Citronellol PubChem
small-molecule unknown - - No No - - 2020-06-24 Yes
OPSD Rhodopsin Opsins A Bovine X-ray 6PH7 6PH7_refined 2.9 A Active 100 94 Gi/o αt2 Only H5 3 - - Nerol PubChem
small-molecule unknown - - No No - - 2020-07-01 Yes
GABR2 GABAB2 GABAB C Human cryo-EM 6WIV 6WIV_refined 3.3 B Inactive 0 71 - - - - - - [(2R)-3-[(Z)-icos-11-enoyl]oxy-2-[(Z)-octadec-9-enoyl]oxypropyl] 2-(trimethylazaniumyl)ethylphosphate PubChem
(2R)-3-{[(S)-(2-aminoethoxy)(hydroxy)phosphoryl]oxy}-2-{[(9Z)-octadec-9-enoyl]oxy}propyl(5Z,8Z,11Z,14Z)-icosa-5,8,11,14-tetraenoate PubChem
small-molecule
small-molecule		 NAM - - No No Park J, Fu Z, Frangaj A, Liu J, Mosyak L, Shen T, Slavkovich VN, Ray KM, Taura J, Cao B, Geng Y, Zuo H, Kou Y, Grassucci R, Chen S, Liu Z, Lin X, Williams JP, Rice WJ, Eng ET, Huang RK, Soni RK, Kloss B, Yu Z, Javitch JA, Hendrickson WA, Slesinger PA, Quick M, Graziano J, Yu H, Fiehn O, Clarke OB, Frank J, Fan QR 10.1038/S41586-020-2452-0 2020-07-01 Yes
AA2AR A2A Adenosine A Human X-ray 6S0L 6S0L_refined 2.7 A Inactive 1 72 - - - - BRIL - ZM-241385 PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank
small-molecule Antagonist adenosine small-molecule Yes No Nass K, Cheng R, Vera L, Mozzanica A, Redford S, Ozerov D, Basu S, James D, Knopp G, Cirelli C, Martiel I, Casadei C, Weinert T, Nogly P, Skopintsev P, Usov I, Leonarski F, Geng T, Rappas M, Dore AS, Cooke R, Nasrollahi Shirazi S, Dworkowski F, Sharpe M, Olieric N, Bacellar C, Bohinc R, Steinmetz MO, Schertler G, Abela R, Patthey L, Schmitt B, Hennig M, Standfuss J, Wang M, Milne CJ 10.1107/S2052252520011379 2020-07-15 Yes
OX1R OX1 Orexin A Human X-ray 6V9S 6V9S_refined 3.5 A Inactive 1 72 - - - - GlgA glycogen synthase - JH112 PubChem Guide To Pharmacology
small-molecule Antagonist orexin-B, orexin-A peptide No No Hellmann J, Drabek M, Yin J, Gunera J, Proll T, Kraus F, Langmead CJ, Hubner H, Weikert D, Kolb P, Rosenbaum DM, Gmeiner P 10.1073/PNAS.2002704117 2020-07-15 Yes
OXYR OT Vasopressin and oxytocin A Human X-ray 6TPK - 3.2 A Inactive 13 68 - - - - GlgA glycogen synthase - retosiban PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank
small-molecule Antagonist oxytocin, vasopressin peptide Yes No Waltenspuhl Y, Schoppe J, Ehrenmann J, Kummer L, Pluckthun A 10.1126/SCIADV.ABB5419 2020-08-05 Yes
GHSR ghrelin Ghrelin A Human X-ray 6KO5 6KO5_refined 3.3 A Inactive 1 80 - - - - BRIL Fab7881 heavy chain
Fab7881 light chain		 CHEMBL1956994 ChEMBL_compound_ids