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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
STE2 STE2 STE2 D1 (Ste2-like fungal pheromone) strain ATCC 204508 / S288c cryo-EM 7AD3 - 3.5 A Active - 69 GPa1 family αPa1 Two alpha subunits bound to STE2 dimer 46 - - Alpha-factor mating pheromone pubchem
peptide Agonist - - No No Velazhahan V, Ma N, Pándy-Szekeres G, Kooistra AJ, Lee Y, Gloriam DE, Vaidehi N, Tate CG 10.1038/S41586-020-2994-1 2020-12-09 Yes
OPRM μ Opioid A (Rhodopsin) Mouse X-ray 4DKL 4DKL_refined 2.8 A Inactive 7 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 [Leu]enkephalin, [Met]enkephalin, dynorphin A-(1-13), dynorphin A, dynorphin A-(1-8), dynorphin B, endomorphin-1, β-endorphin, endomorphin-2 peptide 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
OXYR OT Vasopressin and oxytocin A (Rhodopsin) Human X-ray 6TPK - 3.2 A Inactive 24 68 - - - - GIgA glycogen synthase - Retosiban pubchem
small molecule Antagonist vasopressin, oxytocin peptide Yes No Waltenspühl Y, Schöppe J, Ehrenmann J, Kummer L, Plückthun A 10.1126/SCIADV.ABB5419 2020-08-05 Yes
CCR2 CCR2 Chemokine A (Rhodopsin) Human X-ray 5T1A 5T1A_refined 2.8 A Inactive 30 76 - - - - T4-Lysozyme - GTPL9431 pubchem
BMS-681 pubchem
small molecule
small molecule		 Allosteric antagonist
Antagonist		 CCL16, CCL7, CCL13, CCL8, CCL24, CCL2, CCL11, CCL26 protein No No Zheng Y, Qin L, Zacarías NVO, 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
CNR2 CB2 Cannabinoid A (Rhodopsin) Human X-ray 5ZTY 5ZTY_refined 2.8 A Inactive 6 80 - - - - T4-Lysozyme - AM10257 pubchem
small molecule Antagonist 2-arachidonoylglycerol, anandamide small molecule Yes No Li X, Hua T, Vemuri K, Ho J, Wu Y, Wu L, Popov P, Benchama O, Zvonok N, Locke K, Qu L, Han GW, Iyer MR, Cinar R, Coffey NJ, Wang J, Wu M, Katritch V, Zhao S, Kunos G, Bohn LM, Makriyannis A, Stevens RC, Liu Z 10.1016/J.CELL.2018.12.011 2019-01-30 Yes
PE2R3 EP3 Prostanoid A (Rhodopsin) Human X-ray 6AK3 6AK3_refined 2.9 B Active 83 69 - - - - BRIL - Prostaglandin E2 pubchem chembl_ligand
small molecule Agonist PGE1, PGD2, PGE2, PGF2α, PGI2 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
5HT1B 5-HT1B 5-Hydroxytryptamine A (Rhodopsin) Human cryo-EM 6G79 6G79_refined 3.8 S Active 100 67 Gi/o αo - 59 - - Donitriptan pubchem
small molecule Agonist 5-hydroxytryptamine, tryptamine, 5-HT-moduline small molecule Yes No García-Nafría J, Nehmé R, Edwards PC, Tate CG 10.1038/S41586-018-0241-9 2018-06-20 Yes
OPRD δ Opioid A (Rhodopsin) Human X-ray 4N6H 4N6H_refined 1.8 A Inactive 7 81 - - - - BRIL - Naltrindole pubchem
small molecule Antagonist α-neoendorphin, [Leu]enkephalin, [Met]enkephalin, dynorphin A-(1-13), dynorphin A, dynorphin A-(1-8), dynorphin B, endomorphin-1, β-endorphin peptide Yes Yes Fenalti G, Giguere PM, Katritch V, Huang X, Thompson AA, Cherezov V, Roth BL, Stevens RC 10.1038/NATURE12944 2013-12-25 Yes
PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human cryo-EM 6NBI 6NBI_refined 4.0 R Active 100 62 Gs αs - 56 - Nanobody-35 Long-acting parathyroid hormone analog
peptide Agonist PTHrP, TIP39, PTH, PTHrP-(1-36) protein No No Zhao L, Ma S, Sutkeviciute I, Shen D, Zhou XE, de Waal PW, Li C, 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 M, Vilardaga J, Xu HE, Zhang Y 10.1126/SCIENCE.AAV7942 2019-04-17 Yes
PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human cryo-EM 6NBF - 3.0 R Active 100 62 Gs αs - 58 - Nanobody-35 Long-acting parathyroid hormone analog
peptide Agonist PTHrP, TIP39, PTH, PTHrP-(1-36) protein No No Zhao L, Ma S, Sutkeviciute I, Shen D, Zhou XE, de Waal PW, Li C, 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 M, Vilardaga J, Xu HE, Zhang Y 10.1126/SCIENCE.AAV7942 2019-04-17 Yes
PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human cryo-EM 6NBH - 3.5 R Active 100 64 Gs αs - 57 - Nanobody-35 Long-acting parathyroid hormone analog
peptide Agonist PTHrP, TIP39, PTH, PTHrP-(1-36) protein No No Zhao L, Ma S, Sutkeviciute I, Shen D, Zhou XE, de Waal PW, Li C, 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 M, Vilardaga J, Xu HE, Zhang Y 10.1126/SCIENCE.AAV7942 2019-04-17 Yes
GRM5 mGlu5 Metabotropic glutamate C (Glutamate) Human X-ray 4OO9 4OO9_refined 2.6 A Inactive 0 20 - - - - T4-Lysozyme - Mavoglurant pubchem
small molecule NAM L-glutamic acid small molecule No No Doré AS, Okrasa K, Patel JC, Serrano-Vega M, Bennett K, Cooke RM, Errey JC, Jazayeri A, Khan S, Tehan B, Weir M, Wiggin GR, Marshall FH 10.1038/NATURE13396 2014-07-02 Yes
Q08BG4 LPA6 Lysophospholipid (LPA) A (Rhodopsin) Zebrafish X-ray 5XSZ 5XSZ_refined 3.2 A Intermediate 41 78 - - - - T4-Lysozyme - - - - LPA small molecule 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
PAR2 PAR2 Proteinase-activated A (Rhodopsin) Human X-ray 5NDD 5NDD_refined 2.8 A Intermediate 41 74 - - - - T4-Lysozyme - AZ8838 pubchem
small molecule Antagonist thrombin protein Yes Yes Cheng RKY, Fiez-Vandal C, Schlenker O, Edman K, Aggeler B, Brown DG, Brown GA, Cooke RM, Dumelin CE, Doré AS, Geschwindner S, Grebner C, Hermansson N, Jazayeri A, Johansson P, Leong L, Prihandoko R, Rappas M, Soutter H, Snijder A, Sundström L, Tehan B, Thornton P, Troast D, Wiggin G, Zhukov A, Marshall FH, Dekker N 10.1038/NATURE22309 2017-05-03 Yes
PAR2 PAR2 Proteinase-activated A (Rhodopsin) Human X-ray 5NJ6 5NJ6_refined 4.0 A Intermediate 41 74 - - - - BRIL Fab3949 - - - thrombin protein Yes No Cheng RKY, Fiez-Vandal C, Schlenker O, Edman K, Aggeler B, Brown DG, Brown GA, Cooke RM, Dumelin CE, Doré AS, Geschwindner S, Grebner C, Hermansson N, Jazayeri A, Johansson P, Leong L, Prihandoko R, Rappas M, Soutter H, Snijder A, Sundström L, Tehan B, Thornton P, Troast D, Wiggin G, Zhukov A, Marshall FH, Dekker N 10.1038/NATURE22309 2017-05-03 Yes
PAR2 PAR2 Proteinase-activated A (Rhodopsin) Human X-ray 5NDZ 5NDZ_refined 3.6 A Intermediate 41 74 - - - - T4-Lysozyme - AZ3451 pubchem
small molecule Allosteric antagonist thrombin protein Yes Yes Cheng RKY, Fiez-Vandal C, Schlenker O, Edman K, Aggeler B, Brown DG, Brown GA, Cooke RM, Dumelin CE, Doré AS, Geschwindner S, Grebner C, Hermansson N, Jazayeri A, Johansson P, Leong L, Prihandoko R, Rappas M, Soutter H, Snijder A, Sundström L, Tehan B, Thornton P, Troast D, Wiggin G, Zhukov A, Marshall FH, Dekker N 10.1038/NATURE22309 2017-05-03 Yes
C5AR1 C5a1 Complement peptide A (Rhodopsin) Human X-ray 5O9H 5O9H_refined 2.7 A Inactive 10 84 - - - - - - NDT 9513727 pubchem
small molecule Antagonist C5a, C3a, C5a des-Arg, ribosomal protein S19 protein Yes No Robertson N, Rappas M, Doré AS, Brown J, Bottegoni G, Koglin M, Cansfield J, Jazayeri A, Cooke RM, Marshall FH 10.1038/NATURE25025 2018-01-10 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 1GZM 1GZM_refined 2.7 A Inactive 36 94 - - - - - - Retinal (11-cis) pubchem
small molecule Inverse agonist Retinal small molecule No No Li J, Edwards PC, Burghammer M, Villa C, Schertler GF 10.1016/J.JMB.2004.08.090 2003-11-20 Yes
CALRL calcitonin-like Calcitonin B1 (Secretin) Human cryo-EM 7KNU 7KNU_refined 3.5 R Inactive 10 74 - - - - - RAMP1 Calcitonin gene-related peptide 1 pubchem
peptide Agonist adrenomedullin, α-CGRP, β-CGRP, adrenomedullin 2/intermedin, α-CGRP-(8-37) (rat) peptide No No Josephs TM, Belousoff MJ, Liang Y, Piper SJ, Cao J, Garama DJ, Leach K, Gregory KJ, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM 10.1126/SCIENCE.ABF7258 2021-02-24 Yes
DRD1 D1 Dopamine A (Rhodopsin) Human cryo-EM 7JVP 7JVP_refined 2.9 R Active 100 63 Gs αs - 60 - Nanobody-35 39YLC3L0ZU pubchem
small molecule Agonist dopamine, noradrenaline, 5-hydroxytryptamine small molecule Yes No Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang X, Shen D, Xu T, Liu Y, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE 10.1016/J.CELL.2021.01.027 2021-02-24 Yes
DRD2 D2 Dopamine A (Rhodopsin) Human cryo-EM 7JVR 7JVR_refined 2.8 R Active 100 61 Gi/o αi1 - 63 - scFv16 Bromocriptine pubchem
small molecule Agonist dopamine small molecule Yes No Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang X, Shen D, Xu T, Liu Y, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE 10.1016/J.CELL.2021.01.027 2021-02-24 Yes
DRD1 D1 Dopamine A (Rhodopsin) Human cryo-EM 7JVQ 7JVQ_refined 3.0 R Active 100 64 Gs αs Engineered G alpha 60 - Nanobody-35 Apomorphine pubchem chembl_ligand
small molecule Agonist dopamine, noradrenaline, 5-hydroxytryptamine small molecule Yes No Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang X, Shen D, Xu T, Liu Y, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE 10.1016/J.CELL.2021.01.027 2021-02-24 Yes
DRD1 D1 Dopamine A (Rhodopsin) Human cryo-EM 7JV5 - 3.0 R Active 100 63 Gs αs - 60 - Nanobody-35 743408-71-1 pubchem chembl_ligand
small molecule Agonist dopamine, noradrenaline, 5-hydroxytryptamine small molecule Yes No Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang X, Shen D, Xu T, Liu Y, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE 10.1016/J.CELL.2021.01.027 2021-02-24 Yes
ADA2B α2B Adrenoceptors A (Rhodopsin) Human cryo-EM 6K42 - 4.1 R Active 100 60 Gi/o αi1 - 62 T4-Lysozyme scFv Dexmedetomidine pubchem
small molecule Agonist (-)-adrenaline, (-)-noradrenaline small molecule Yes No Yuan D, Liu Z, Kaindl J, Maeda S, Zhao J, Sun X, Xu J, Gmeiner P, Wang H, Kobilka BK 10.1038/S41589-020-0492-2 2020-04-15 Yes
ADA2B α2B Adrenoceptors A (Rhodopsin) Human cryo-EM 6K41 - 2.9 R Active 100 54 Gi/o αo - 60 T4-Lysozyme scFv Dexmedetomidine pubchem
small molecule Agonist (-)-adrenaline, (-)-noradrenaline small molecule Yes No Yuan D, Liu Z, Kaindl J, Maeda S, Zhao J, Sun X, Xu J, Gmeiner P, Wang H, Kobilka BK 10.1038/S41589-020-0492-2 2020-04-15 Yes
NTR1 NTS1 Neurotensin A (Rhodopsin) Human cryo-EM 6OS9 6OS9_refined 3.0 R Active 100 73 Gi/o αi1 - 62 - scFv16 JMV449 pubchem
peptide Agonist neurotensin, large neurotensin, neuromedin N, large neuromedin N peptide Yes No Kato HE, Zhang Y, Hu H, Suomivuori C, Kadji FMN, Aoki J, Krishna Kumar K, Fonseca R, Hilger D, Huang W, Latorraca NR, Inoue A, Dror RO, Kobilka BK, Skiniotis G 10.1038/S41586-019-1337-6 2019-07-10 Yes
NTR1 NTS1 Neurotensin A (Rhodopsin) Human cryo-EM 6OSA 6OSA_refined 3.0 R Active 100 77 Gi/o αi1 Non-canonical conformation 62 - - JMV449 pubchem
peptide Agonist neurotensin, large neurotensin, neuromedin N, large neuromedin N peptide Yes No Kato HE, Zhang Y, Hu H, Suomivuori C, Kadji FMN, Aoki J, Krishna Kumar K, Fonseca R, Hilger D, Huang W, Latorraca NR, Inoue A, Dror RO, Kobilka BK, Skiniotis G 10.1038/S41586-019-1337-6 2019-07-10 Yes
CCR6 CCR6 Chemokine A (Rhodopsin) Human cryo-EM 6WWZ 6WWZ_refined 3.3 R Active 100 83 Gi/o αo - 59 - scFv16 CCL20
protein Agonist CCL20, beta-defensin 4A protein No No Wasilko DJ, Johnson ZL, Ammirati M, Che Y, Griffor MC, Han S, Wu H 10.1038/S41467-020-16820-6 2020-06-24 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 3VGA - 3.1 A Inactive 1 72 - - - - - - ZM241385 pubchem
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 (Rhodopsin) Human X-ray 3VG9 3VG9_refined 2.7 A Inactive 1 72 - - - - - Antibody fab fragment light chain
Antibody fab fragment heavy chain		 ZM241385 pubchem
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 Yes
CASR CaS Calcium-sensing C (Glutamate) Human cryo-EM 7DTT 7DTT_refined 3.8 A Inactive 7 72 - - - - - - Calcium ion pubchem
ion Agonist L-tryptophan, spermine, Ca2+, Mg2+ amino acid No No Ling S, Shi P, Liu S, Meng X, Zhou Y, Sun W, Chang S, Zhang X, Zhang L, Shi C, Sun D, Liu L, Tian C 10.1038/S41422-021-00474-0 2021-03-10 Yes
CASR CaS Calcium-sensing C (Glutamate) Human cryo-EM 7DTU 7DTU_refined 4.4 A Inactive 7 72 - - - - - - Tryptophan pubchem chembl_ligand
amino acid PAM L-tryptophan, spermine, Ca2+, Mg2+ amino acid No No Ling S, Shi P, Liu S, Meng X, Zhou Y, Sun W, Chang S, Zhang X, Zhang L, Shi C, Sun D, Liu L, Tian C 10.1038/S41422-021-00474-0 2021-03-10 Yes
CASR CaS Calcium-sensing C (Glutamate) Human cryo-EM 7DTV 7DTV_refined 3.5 A Inactive 7 72 - - - - - - Calcium ion pubchem
Tryptophan pubchem chembl_ligand
ion
amino acid		 Agonist
PAM		 L-tryptophan, spermine, Ca2+, Mg2+ amino acid No No Ling S, Shi P, Liu S, Meng X, Zhou Y, Sun W, Chang S, Zhang X, Zhang L, Shi C, Sun D, Liu L, Tian C 10.1038/S41422-021-00474-0 2021-03-10 Yes
CASR CaS Calcium-sensing C (Glutamate) Human cryo-EM 7DTW 7DTW_refined 4.5 A Inactive 7 72 - - - - - - Apo (no ligand)
none Apo (no ligand) L-tryptophan, spermine, Ca2+, Mg2+ amino acid No No Ling S, Shi P, Liu S, Meng X, Zhou Y, Sun W, Chang S, Zhang X, Zhang L, Shi C, Sun D, Liu L, Tian C 10.1038/S41422-021-00474-0 2021-03-10 Yes
CXCR2 CXCR2 Chemokine A (Rhodopsin) Human cryo-EM 6LFO 6LFO_refined 3.4 R Active 100 85 Gi/o αi1 - 65 - scFv16 Interleukin-8 pubchem
protein Agonist CXCL6, CXCL8, CXCL1, CXCL2, CXCL3, CXCL5, CXCL7 protein No No Liu K, Wu L, Yuan S, Wu M, Xu Y, Sun Q, Li S, Zhao S, Hua T, Liu Z 10.1038/S41586-020-2492-5 2020-09-02 Yes
CXCR2 CXCR2 Chemokine A (Rhodopsin) Human cryo-EM 6LFM 6LFM_refined 3.5 R Active 100 85 Gi/o αi1 - 65 - scFv16 Interleukin-8 pubchem
protein Agonist CXCL6, CXCL8, CXCL1, CXCL2, CXCL3, CXCL5, CXCL7 protein No No Liu K, Wu L, Yuan S, Wu M, Xu Y, Sun Q, Li S, Zhao S, Hua T, Liu Z 10.1038/S41586-020-2492-5 2020-09-02 Yes
CXCR2 CXCR2 Chemokine A (Rhodopsin) Human X-ray 6LFL 6LFL_refined 3.2 A Inactive 8 76 - - - - GIgA glycogen synthase - 4-[[3,4-Dioxo-2-[[(1R)-1-(4-propan-2-ylfuran-2-yl)propyl]amino]cyclobuten-1-yl]amino]-3-hydroxy-N,N-dimethylpyridine-2-carboxamide pubchem
small molecule Allosteric antagonist CXCL6, CXCL8, CXCL1, CXCL2, CXCL3, CXCL5, CXCL7 protein No No Liu K, Wu L, Yuan S, Wu M, Xu Y, Sun Q, Li S, Zhao S, Hua T, Liu Z 10.1038/S41586-020-2492-5 2020-09-02 Yes
ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human X-ray 5ZKC 5ZKC_refined 2.3 A Inactive 5 60 - - - - - - N-methyl scopolamine 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
ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human X-ray 5ZK8 5ZK8_refined 3.0 A Inactive 5 59 - - - - - - N-methyl scopolamine pubchem
small molecule Antagonist acetylcholine small molecule Yes 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 (Rhodopsin) Human X-ray 5YC8 5YC8_refined 2.5 A Inactive 5 60 - - - - - - N-methyl scopolamine 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
ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human X-ray 5ZKB 5ZKB_refined 3.0 A Inactive 5 60 - - - - - - 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
ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human X-ray 5ZK3 5ZK3_refined 2.6 A Inactive 5 59 - - - - - - QNB 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
DRD2 D2 Dopamine A (Rhodopsin) Human X-ray 6CM4 6CM4_refined 2.9 A Inactive 1 59 - - - - T4-Lysozyme - Risperidone pubchem chembl_ligand
small molecule Inverse agonist dopamine small molecule Yes No Wang S, Che T, Levit A, Shoichet BK, Wacker D, Roth BL 10.1038/NATURE25758 2018-03-14 Yes
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human X-ray 5JQH 5JQH_refined 3.2 A Inactive 0 70 - - - - T4-Lysozyme Nanobody Carazolol pubchem
small molecule Inverse agonist noradrenaline, (-)-adrenaline, (-)-noradrenaline, Zn2+ 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
SUCR1 succinate Succinate A (Rhodopsin) Rat X-ray 6RNK 6RNK_refined 1.9 A Intermediate 41 90 - - - - - Nanobody6 NF-56-EJ40 pubchem
small molecule Antagonist succinic acid small molecule 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 V 10.1038/S41586-019-1663-8 2019-08-14 Yes
SUCR1 succinate Succinate A (Rhodopsin) Rat X-ray 6IBB 6IBB_refined 2.1 A Intermediate 41 93 - - - - - Nanobody6 - - - succinic acid small molecule 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 V 10.1038/S41586-019-1663-8 2019-08-14 Yes
ACM3 M3 Acetylcholine (muscarinic) A (Rhodopsin) Rat X-ray 5ZHP 5ZHP_refined 3.1 B Inactive 5 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, Hübner 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
5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 6A93 6A93_refined 3.0 A Inactive 1 60 - - - - BRIL - Risperidone pubchem chembl_ligand
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
5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 6A94 6A94_refined 2.9 A Inactive 1 60 - - - - BRIL - Zotepine pubchem chembl_ligand
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
PE2R2 EP2 Prostanoid A (Rhodopsin) Human cryo-EM 7CX4 7CX4_refined 2.9 R Active 100 74 Gs αs - 58 - Nanobody-35 Evatanepag pubchem chembl_ligand
small molecule Agonist PGE1, PGD2, PGE2, PGF2α, PGI2 small molecule Yes No Qu C, Mao C, Xiao P, Shen Q, Zhong Y, Yang F, Shen D, Tao X, Zhang H, Yan X, Zhao R, He J, Guan Y, Zhang C, Hou G, Zhang P, Hou G, Li Z, Yu X, Chai R, Guan Y, Sun J, Zhang Y 10.1126/SCIADV.ABF1268 2021-05-05 Yes
PE2R2 EP2 Prostanoid A (Rhodopsin) Human cryo-EM 7CX2 7CX2_refined 2.8 R Active 100 74 Gs αs - 58 - Nanobody-35 Prostaglandin E2 pubchem chembl_ligand
small molecule Agonist PGE1, PGD2, PGE2, PGF2α, PGI2 small molecule Yes No Qu C, Mao C, Xiao P, Shen Q, Zhong Y, Yang F, Shen D, Tao X, Zhang H, Yan X, Zhao R, He J, Guan Y, Zhang C, Hou G, Zhang P, Hou G, Li Z, Yu X, Chai R, Guan Y, Sun J, Zhang Y 10.1126/SCIADV.ABF1268 2021-05-05 Yes
PE2R2 EP2 Prostanoid A (Rhodopsin) Human cryo-EM 7CX3 7CX3_refined 2.8 R Active 100 74 Gs αs - 58 - Nanobody-35 Taprenepag pubchem chembl_ligand
small molecule Agonist PGE1, PGD2, PGE2, PGF2α, PGI2 small molecule Yes No Qu C, Mao C, Xiao P, Shen Q, Zhong Y, Yang F, Shen D, Tao X, Zhang H, Yan X, Zhao R, He J, Guan Y, Zhang C, Hou G, Zhang P, Hou G, Li Z, Yu X, Chai R, Guan Y, Sun J, Zhang Y 10.1126/SCIADV.ABF1268 2021-05-05 Yes
CNR1 CB1 Cannabinoid A (Rhodopsin) Human X-ray 5TGZ 5TGZ_refined 2.8 A Inactive 12 61 - - - - Flavodoxin - AM-6538 pubchem
small molecule Antagonist 2-arachidonoylglycerol, anandamide small molecule Yes No Hua T, Vemuri K, Pu M, Qu L, Han GW, Wu Y, Zhao S, Shui W, Li S, Korde A, Laprairie RB, Stahl EL, Ho J, Zvonok N, Zhou H, Kufareva I, Wu B, Zhao Q, Hanson MA, Bohn LM, Makriyannis A, Stevens RC, Liu Z 10.1016/J.CELL.2016.10.004 2016-11-02 Yes
CRFR2 CRF2 Corticotropin-releasing factor B1 (Secretin) Human cryo-EM 6PB1 6PB1_refined 2.8 P Active 100 68 Gs αs - 58 - Nanobody-35 Urocortin pubchem chembl_ligand
peptide Agonist urocortin 2, corticotrophin-releasing hormone, urocortin 1, urocortin 3 peptide No No Ma S, Shen Q, Zhao L, Mao C, Zhou XE, Shen D, de Waal PW, Bi P, Li C, Jiang Y, Wang M, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE 10.1016/J.MOLCEL.2020.01.013 2020-02-12 Yes
CRFR1 CRF1 Corticotropin-releasing factor B1 (Secretin) Human cryo-EM 6PB0 6PB0_refined 3.0 R Active 100 68 Gs αs Gs-Gi1 chimera 58 - Nanobody-35 Urocortin pubchem chembl_ligand
peptide Agonist urocortin 2, corticotrophin-releasing hormone, urocortin 1 peptide No No Ma S, Shen Q, Zhao L, Mao C, Zhou XE, Shen D, de Waal PW, Bi P, Li C, Jiang Y, Wang M, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE 10.1016/J.MOLCEL.2020.01.013 2020-02-12 Yes
CXCR4 CXCR4 Chemokine A (Rhodopsin) Human X-ray 3OE0 3OE0_refined 2.9 A Inactive 7 78 - - - - T4-Lysozyme - CVX15
peptide Antagonist CXCL12α, CXCL12γ, CXCL12δ, CXCL12ε, CXCL12φ, CXCL12β, CXCL12 protein Yes No Wu B, Chien EYT, 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
CXCR4 CXCR4 Chemokine A (Rhodopsin) Human X-ray 3OE6 - 3.2 A Inactive 7 77 - - - - T4-Lysozyme - IT1t pubchem
small molecule Antagonist CXCL12α, CXCL12γ, CXCL12δ, CXCL12ε, CXCL12φ, CXCL12β, CXCL12 protein Yes No Wu B, Chien EYT, 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 (Rhodopsin) Human X-ray 3OE9 - 3.1 A Inactive 7 74 - - - - T4-Lysozyme - IT1t pubchem
small molecule Antagonist CXCL12α, CXCL12γ, CXCL12δ, CXCL12ε, CXCL12φ, CXCL12β, CXCL12 protein Yes No Wu B, Chien EYT, 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 (Rhodopsin) Human X-ray 3OE8 - 3.1 A Inactive 7 76 - - - - T4-Lysozyme - IT1t pubchem
small molecule Antagonist CXCL12α, CXCL12γ, CXCL12δ, CXCL12ε, CXCL12φ, CXCL12β, CXCL12 protein Yes No Wu B, Chien EYT, 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 (Rhodopsin) Human X-ray 3ODU 3ODU_refined 2.5 A Inactive 7 83 - - - - T4-Lysozyme - IT1t pubchem
small molecule Antagonist CXCL12α, CXCL12γ, CXCL12δ, CXCL12ε, CXCL12φ, CXCL12β, CXCL12 protein Yes No Wu B, Chien EYT, 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
OPRM μ Opioid A (Rhodopsin) Mouse X-ray 5C1M 5C1M_refined 2.1 A Active 94 74 - - - - - Antibody GTPL9363 pubchem
small molecule Agonist [Leu]enkephalin, [Met]enkephalin, dynorphin A-(1-13), dynorphin A, dynorphin A-(1-8), dynorphin B, endomorphin-1, β-endorphin, endomorphin-2 peptide 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
ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human X-ray 4MQT 4MQT_refined 3.7 A Active 98 59 - - - - - Nanobody Iperoxo pubchem
2CU pubchem
small molecule
small molecule		 Agonist
PAM		 acetylcholine small molecule Yes No Kruse AC, Ring AM, Manglik A, Hu J, Hu K, Eitel K, Hübner 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
ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human X-ray 4MQS 4MQS_refined 3.5 A Active 98 59 - - - - - Nanobody Iperoxo pubchem
small molecule Agonist acetylcholine small molecule Yes No Kruse AC, Ring AM, Manglik A, Hu J, Hu K, Eitel K, Hübner 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
P2RY1 P2Y1 P2Y A (Rhodopsin) Human X-ray 4XNW 4XNW_refined 2.7 A Intermediate 41 78 - - - - Rubredoxin - MRS2500 pubchem
small molecule Antagonist ADP, ATP small molecule Yes No Zhang D, Gao Z, Zhang K, Kiselev E, Crane S, Wang J, Paoletta S, Yi C, Ma L, Zhang W, Han GW, Liu H, Cherezov V, Katritch V, Jiang H, Stevens RC, Jacobson KA, Zhao Q, Wu B 10.1038/NATURE14287 2015-04-01 Yes
P2RY1 P2Y1 P2Y A (Rhodopsin) Human X-ray 4XNV 4XNV_refined 2.2 A Intermediate 41 78 - - - - Rubredoxin - BPTU pubchem
small molecule NAM ADP, ATP small molecule Yes No Zhang D, Gao Z, Zhang K, Kiselev E, Crane S, Wang J, Paoletta S, Yi C, Ma L, Zhang W, Han GW, Liu H, Cherezov V, Katritch V, Jiang H, Stevens RC, Jacobson KA, Zhao Q, Wu B 10.1038/NATURE14287 2015-04-01 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 4UG2 4UG2_refined 2.6 A Active 76 71 - - - - - - CGS-21680 pubchem
small molecule Agonist adenosine small molecule Yes No Lebon G, Edwards PC, Leslie AGW, Tate CG 10.1124/MOL.114.097360 2015-04-08 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 4UHR 4UHR_refined 2.6 A Active 76 75 - - - - - - CGS-21680 pubchem
small molecule Agonist adenosine small molecule Yes No Lebon G, Edwards PC, Leslie AGW, Tate CG 10.1124/MOL.114.097360 2015-04-08 Yes
ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human cryo-EM 6U1N 6U1N_refined 4.0 R Active 91 57 Beta Beta-arrestin-1 - 96 - Fab30 light chain
Fab30 heavy chain		 2CU pubchem
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
MTR1A MT1 Melatonin A (Rhodopsin) Human X-ray 6ME3 6ME3_refined 2.9 A Inactive 1 82 - - - - GIgA glycogen synthase - 2-phenylmelatonin pubchem
small molecule Agonist melatonin small molecule No No Stauch B, Johansson LC, McCorvy JD, Patel N, Han GW, Huang X, 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
MTR1A MT1 Melatonin A (Rhodopsin) Human X-ray 6ME2 6ME2_refined 2.8 A Inactive 1 83 - - - - GIgA glycogen synthase - Ramelteon pubchem chembl_ligand
small molecule Agonist melatonin small molecule No No Stauch B, Johansson LC, McCorvy JD, Patel N, Han GW, Huang X, 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
MTR1A MT1 Melatonin A (Rhodopsin) Human X-ray 6ME4 6ME4_refined 3.2 A Inactive 1 83 - - - - GlgA glycogen synthase - 2-Iodomelatonin pubchem chembl_ligand
small molecule Agonist melatonin small molecule No No Stauch B, Johansson LC, McCorvy JD, Patel N, Han GW, Huang X, 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
MTR1A MT1 Melatonin A (Rhodopsin) Human X-ray 6ME5 6ME5_refined 3.2 A Inactive 1 83 - - - - GlgA glycogen synthase - Agomelatine pubchem chembl_ligand
small molecule Agonist melatonin small molecule No No Stauch B, Johansson LC, McCorvy JD, Patel N, Han GW, Huang X, 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
ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey X-ray 4AMI 4AMI_refined 3.2 A Inactive 0 58 - - - - - - Bucindolol pubchem
small molecule Agonist noradrenaline, (-)-adrenaline, (-)-noradrenaline small molecule Yes No Warne T, Edwards PC, Leslie AG, Tate CG 10.1016/J.STR.2012.03.014 2012-05-23 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey X-ray 4AMJ 4AMJ_refined 2.3 B Inactive 0 62 - - - - - - (S)-Carvedilol pubchem
small molecule Inverse agonist noradrenaline, (-)-adrenaline, (-)-noradrenaline small molecule Yes No Warne T, Edwards PC, Leslie AG, Tate CG 10.1016/J.STR.2012.03.014 2012-05-23 Yes
GABR2 GABAB2 GABAB C (Glutamate) Human cryo-EM 6W2X - 3.6 B Active 53 71 - - - - - - CGP55845 pubchem
1-Stearoyl-2-oleoyl-sn-glycero-3-phosphoethanolamine pubchem
small molecule
small molecule		 Inverse agonist
NAM		 GABA small molecule No No Papasergi-Scott MM, Robertson MJ, Seven AB, Panova O, Mathiesen JM, Skiniotis G 10.1038/S41586-020-2469-4 2020-07-01 Yes
GABR1 GABAB1 GABAB C (Glutamate) Human cryo-EM 6W2Y - 3.2 B Active 52 69 - - - - - - CGP55845 pubchem
1-Stearoyl-2-oleoyl-sn-glycero-3-phosphoethanolamine pubchem
small molecule
small molecule		 Inverse agonist
NAM		 GABA small molecule No No Papasergi-Scott MM, Robertson MJ, Seven AB, Panova O, Mathiesen JM, Skiniotis G 10.1038/S41586-020-2469-4 2020-07-01 Yes
OX2R OX2 Orexin A (Rhodopsin) Human X-ray 5WS3 5WS3_refined 2.3 A Inactive 1 70 - - - - Glycogen synthase - EMPA pubchem chembl_ligand
small molecule Antagonist orexin-A, orexin-B 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 2017-12-13 Yes
OX2R OX2 Orexin A (Rhodopsin) Human X-ray 5WQC 5WQC_refined 2.0 A Inactive 1 68 - - - - Glycogen synthase - EMPA pubchem chembl_ligand
small molecule Antagonist orexin-A, orexin-B 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
CLTR2 CysLT2 Leukotriene A (Rhodopsin) Human X-ray 6RZ8 6RZ8_refined 2.7 A Intermediate 41 78 - - - - BRIL - ONO-2080365 pubchem
small molecule Antagonist LTE4, LTD4, LTC4 small molecule No No Gusach A, Luginina A, Marin E, Brouillette RL, Besserer-Offroy É, Longpré J, 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
CLTR2 CysLT2 Leukotriene A (Rhodopsin) Human X-ray 6RZ7 6RZ7_refined 2.4 A Intermediate 41 79 - - - - BRIL - ONO-2570366 (C2221 space group) pubchem
small molecule Antagonist LTE4, LTD4, LTC4 small molecule No No Gusach A, Luginina A, Marin E, Brouillette RL, Besserer-Offroy É, Longpré J, 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
CLTR2 CysLT2 Leukotriene A (Rhodopsin) Human X-ray 6RZ9 6RZ9_refined 2.7 A Intermediate 41 81 - - - - BRIL - ONO-2770372 pubchem
small molecule Antagonist LTE4, LTD4, LTC4 small molecule No No Gusach A, Luginina A, Marin E, Brouillette RL, Besserer-Offroy É, Longpré J, 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
CLTR2 CysLT2 Leukotriene A (Rhodopsin) Human X-ray 6RZ6 6RZ6_refined 2.4 A Intermediate 41 82 - - - - BRIL - ONO-2570366 (C2221 space group) pubchem
small molecule Antagonist LTE4, LTD4, LTC4 small molecule No No Gusach A, Luginina A, Marin E, Brouillette RL, Besserer-Offroy É, Longpré J, 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
CCR7 CCR7 Chemokine A (Rhodopsin) Human X-ray 6QZH 6QZH_refined 2.1 A Inactive 8 71 - - - - Sialidase NanA - SCHEMBL13407377 pubchem
small molecule Allosteric antagonist Ccl21a, Ccl21b, CCL19, CCL21 protein No No Jaeger K, Bruenle S, Weinert T, Guba W, Muehle J, Miyazaki T, Weber M, Furrer A, Haenggi N, Tetaz T, Huang C, Mattle D, Vonach J, Gast A, Kuglstatter A, Rudolph MG, Nogly P, Benz J, Dawson RJ, Standfuss J 10.1016/J.CELL.2019.07.028 2019-09-04 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine cryo-EM 6OFJ 6OFJ_refined 4.5 A Inactive 36 93 - - - - - - Apo (no ligand)
none Apo (no ligand) Retinal small molecule No No Zhao DY, Pöge 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
AGRG3 ADGRG3 ADGRG B2 (Adhesion) Human cryo-EM 7D77 7D77_refined 2.9 R Active - 48 Gi/o αo - 61 - scFv16 Hydrocortisone pubchem
small molecule Agonist - - No No Ping Y, Mao C, Xiao P, Zhao R, Jiang Y, Yang Z, An W, Shen D, Yang F, Zhang H, Qu C, Shen Q, Tian C, Li Z, Li S, Wang G, Tao X, Wen X, Zhong Y, Yang J, Yi F, Yu X, Xu HE, Zhang Y, Sun J 10.1038/S41586-020-03083-W 2021-02-03 Yes
AGRG3 ADGRG3 ADGRG B2 (Adhesion) Human cryo-EM 7D76 - 3.1 R Active - 48 Gi/o αo - 59 - - Beclomethasone pubchem
small molecule Agonist - - No No Ping Y, Mao C, Xiao P, Zhao R, Jiang Y, Yang Z, An W, Shen D, Yang F, Zhang H, Qu C, Shen Q, Tian C, Li Z, Li S, Wang G, Tao X, Wen X, Zhong Y, Yang J, Yi F, Yu X, Xu HE, Zhang Y, Sun J 10.1038/S41586-020-03083-W 2021-02-03 Yes
NTR1 NTS1 Neurotensin A (Rhodopsin) Human cryo-EM 6PWC 6PWC_refined 4.9 R Active 83 77 Beta Beta-arrestin-1 - 94 - Fab30 heavy chain
Fab30 light chain		 neurotensin pubchem chembl_ligand
peptide Agonist neurotensin, large neurotensin, neuromedin N, large neuromedin N peptide Yes No Yin W, Li Z, Jin M, Yin Y, de Waal PW, Pal K, Yin Y, Gao X, He Y, Gao J, Wang X, Zhang Y, Zhou H, Melcher K, Jiang Y, Cong Y, Edward Zhou X, Yu X, Eric Xu H 10.1038/S41422-019-0256-2 2019-12-04 Yes
GLR glucagon Glucagon B1 (Secretin) Human X-ray 5XF1 5XF1_refined 3.2 B Inactive 0 81 - - - - T4-Lysozyme Antibody NNC0640 pubchem
small molecule NAM glucagon peptide No No Zhang H, Qiao A, Yang D, Yang L, Dai A, de Graaf C, Reedtz-Runge S, Dharmarajan V, Zhang H, Han GW, Grant TD, Sierra RG, Weierstall U, Nelson G, Liu W, Wu Y, Ma L, Cai X, Lin G, Wu X, Geng Z, Dong Y, Song G, Griffin PR, Lau J, Cherezov V, Yang H, Hanson MA, Stevens RC, Zhao Q, Jiang H, Wang M, Wu B 10.1038/NATURE22363 2017-05-24 Yes
GLR glucagon Glucagon B1 (Secretin) Human X-ray 5XEZ 5XEZ_refined 3.0 B Inactive 0 82 - - - - T4-Lysozyme Antibody NNC0640 pubchem
small molecule NAM glucagon peptide No No Zhang H, Qiao A, Yang D, Yang L, Dai A, de Graaf C, Reedtz-Runge S, Dharmarajan V, Zhang H, Han GW, Grant TD, Sierra RG, Weierstall U, Nelson G, Liu W, Wu Y, Ma L, Cai X, Lin G, Wu X, Geng Z, Dong Y, Song G, Griffin PR, Lau J, Cherezov V, Yang H, Hanson MA, Stevens RC, Zhao Q, Jiang H, Wang M, Wu B 10.1038/NATURE22363 2017-05-24 Yes
GHRHR GHRH Glucagon B1 (Secretin) Human cryo-EM 7CZ5 7CZ5_refined 2.6 R Active 100 64 Gs αs - 58 - Nanobody-35 Somatoliberin pubchem
peptide Agonist GHRH peptide No No Zhou F, Zhang H, Cong Z, Zhao L, Zhou Q, Mao C, Cheng X, Shen D, Cai X, Ma C, Wang Y, Dai A, Zhou Y, Sun W, Zhao F, Zhao S, Jiang H, Jiang Y, Yang D, Eric Xu H, Zhang Y, Wang M 10.1038/S41467-020-18945-0 2020-11-18 Yes
LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human X-ray 4Z35 4Z35_refined 2.9 A Inactive 1 80 - - - - BRIL - ONO-9910539 pubchem
small molecule Antagonist LPA 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
LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human X-ray 4Z34 4Z34_refined 3.0 A Inactive 1 80 - - - - BRIL - ONO-9780307 pubchem
small molecule Antagonist LPA 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
LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human X-ray 4Z36 4Z36_refined 2.9 A Inactive 1 79 - - - - BRIL - ONO-3080573 pubchem
small molecule Antagonist LPA 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
CRFR1 CRF1 Corticotropin-releasing factor B1 (Secretin) Human X-ray 4Z9G - 3.2 A Inactive 20 63 - - - - T4-Lysozyme - CP-376395 pubchem
small molecule Antagonist urocortin 2, corticotrophin-releasing hormone, urocortin 1 peptide No No Dore AS, Bortolato A, Hollenstein K, Cheng RK, Read RJ, Marshall FH 10.2174/1874467210666170110114727 2016-06-29 Yes
DRD4 D4 Dopamine A (Rhodopsin) Human X-ray 5WIV 5WIV_refined 2.1 A Inactive 1 58 - - - - BRIL - Nemonapride pubchem
small molecule Antagonist dopamine small molecule Yes Yes Wang S, Wacker D, Levit A, Che T, Betz RM, McCorvy JD, Venkatakrishnan AJ, Huang X, Dror RO, Shoichet BK, Roth BL 10.1126/SCIENCE.AAN5468 2017-10-18 Yes
DRD4 D4 Dopamine A (Rhodopsin) Human X-ray 5WIU 5WIU_refined 2.0 A Inactive 1 58 - - - - BRIL - Nemonapride pubchem
small molecule Antagonist dopamine small molecule Yes No Wang S, Wacker D, Levit A, Che T, Betz RM, McCorvy JD, Venkatakrishnan AJ, Huang X, Dror RO, Shoichet BK, Roth BL 10.1126/SCIENCE.AAN5468 2017-10-18 Yes
GLP1R GLP-1 Glucagon B1 (Secretin) Human X-ray 5VEX 5VEX_refined 3.0 B Inactive 0 57 - - - - T4-Lysozyme - NNC0640 pubchem
small molecule NAM glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) 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 Z, Wang M, Stevens RC 10.1038/NATURE22378 2017-05-17 Yes
GLP1R GLP-1 Glucagon B1 (Secretin) Human X-ray 5VEW 5VEW_refined 2.7 A Inactive 0 57 - - - - T4-Lysozyme - PF-06372222 pubchem
small molecule NAM glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) 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 Z, Wang M, Stevens RC 10.1038/NATURE22378 2017-05-24 Yes
ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human cryo-EM 6OIK 6OIK_refined 3.6 R Active 100 60 Gi/o αo - 61 - - Iperoxo pubchem
2CU pubchem
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
ACM1 M1 Acetylcholine (muscarinic) A (Rhodopsin) Human cryo-EM 6OIJ 6OIJ_refined 3.3 R Active 100 64 Gq/11 α11 - 63 - Antibody fragment Iperoxo pubchem
small molecule Agonist acetylcholine small molecule Yes No Maeda S, Qu Q, Robertson MJ, Skiniotis G, Kobilka BK 10.1126/SCIENCE.AAW5188 2019-05-08 Yes
5HT1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human cryo-EM 7E2X 7E2X_refined 3.0 R Active 100 66 Gi/o αi1 - 62 - - Apo (no ligand)
none Apo (no ligand) 5-hydroxytryptamine small molecule Yes No Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen D, Yen H, Robinson CV, Harpsøe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE 10.1038/S41586-021-03376-8 2021-04-14 Yes
5HT1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human cryo-EM 7E2Z 7E2Z_refined 3.1 R Active 100 66 Gi/o αi1 - 62 - - Aripiprazole pubchem
small molecule Agonist (partial) 5-hydroxytryptamine small molecule Yes No Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen D, Yen H, Robinson CV, Harpsøe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE 10.1038/S41586-021-03376-8 2021-04-14 Yes
5HT1E 5-ht1E 5-Hydroxytryptamine A (Rhodopsin) Human cryo-EM 7E33 7E33_refined 2.9 R Active 100 70 Gi/o αi1 - 61 - scFv16 3-(1-Methylpiperidin-4-yl)-1H-indol-5-ol pubchem
small molecule Agonist 5-hydroxytryptamine, tryptamine small molecule Yes No Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen D, Yen H, Robinson CV, Harpsøe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE 10.1038/S41586-021-03376-8 2021-04-14 Yes
5HT1D 5-HT1D 5-Hydroxytryptamine A (Rhodopsin) Human cryo-EM 7E32 7E32_refined 2.9 R Active 100 76 Gi/o αi1 - 62 - scFv16 Serotonin pubchem
small molecule Agonist 5-hydroxytryptamine, 5-HT-moduline small molecule Yes No Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen D, Yen H, Robinson CV, Harpsøe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE 10.1038/S41586-021-03376-8 2021-04-21 Yes
5HT1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human cryo-EM 7E2Y 7E2Y_refined 3.0 R Active 100 65 Gi/o αi1 - 62 - - Serotonin pubchem
small molecule Agonist 5-hydroxytryptamine small molecule Yes No Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen D, Yen H, Robinson CV, Harpsøe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE 10.1038/S41586-021-03376-8 2021-04-14 Yes
SMO SMO Frizzled F (Frizzled) Human X-ray 5L7I 5L7I_refined 3.3 B Inactive 5 59 - - - - BRIL - Vismodegib pubchem
small molecule Antagonist constitutive constitutive 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
SMO SMO Frizzled F (Frizzled) Human X-ray 5L7D 5L7D_refined 3.2 B Inactive 5 59 - - - - BRIL - - - - constitutive constitutive 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
DRD3 D3 Dopamine A (Rhodopsin) Human X-ray 3PBL 3PBL_refined 2.9 A Inactive 1 68 - - - - T4-Lysozyme - Eticlopride pubchem
small molecule Antagonist dopamine small molecule Yes No Chien EYT, Liu W, Zhao Q, Katritch V, Won Han G, Hanson MA, Shi L, Newman AH, Javitch JA, Cherezov V, Stevens RC 10.1126/SCIENCE.1197410 2010-11-03 Yes
HRH1 H1 Histamine A (Rhodopsin) Human X-ray 3RZE 3RZE_refined 3.1 A Inactive 5 55 - - - - T4-Lysozyme - Doxepin pubchem
small molecule Antagonist histamine small molecule Yes No Shimamura T, Shiroishi M, Weyand S, Tsujimoto H, Winter G, Katritch V, Abagyan R, Cherezov V, Liu W, Han GW, Kobayashi T, Stevens RC, Iwata S 10.1038/NATURE10236 2011-06-15 Yes
OPRK κ Opioid A (Rhodopsin) Human X-ray 6B73 6B73_refined 3.1 A Active 94 73 - - - - BRIL Nanobody MP1104 pubchem
small molecule Agonist α-neoendorphin, [Leu]enkephalin, [Met]enkephalin, dynorphin A-(1-13), dynorphin A, dynorphin A-(1-8), dynorphin B, β-endorphin, β-neoendorphin, big dynorphin peptide Yes No Che T, Majumdar S, Zaidi SA, Ondachi P, McCorvy JD, Wang S, Mosier PD, Uprety R, Vardy E, Krumm BE, Han GW, Lee M, Pardon E, Steyaert J, Huang X, Strachan RT, Tribo AR, Pasternak GW, Carroll FI, Stevens RC, Cherezov V, Katritch V, Wacker D, Roth BL 10.1016/J.CELL.2017.12.011 2018-01-17 Yes
GABR2 GABAB2 GABAB C (Glutamate) Human cryo-EM 6VJM 6VJM_refined 4.0 B Active 56 73 - - - - - - Apo (no ligand)
none Apo (no ligand) GABA small molecule No No Shaye H, Ishchenko A, Lam JH, Han GW, Xue L, Rondard P, Pin J, Katritch V, Gati C, Cherezov V 10.1038/S41586-020-2408-4 2020-06-10 Yes
GABR2 GABAB2 GABAB C (Glutamate) Human cryo-EM 6UO8 6UO8_refined 3.6 B Active 99 74 - - - - - - (R)-(3-aminopropyl)methylphosphinic acid pubchem chembl_ligand
N~4~,N~6~-dicyclopentyl-2-(methylsulfanyl)-5-nitropyrimidine-4,6-diamine pubchem
small molecule
small molecule		 Agonist
PAM		 GABA small molecule No No Shaye H, Ishchenko A, Lam JH, Han GW, Xue L, Rondard P, Pin J, Katritch V, Gati C, Cherezov V 10.1038/S41586-020-2408-4 2020-06-10 Yes
GABR2 GABAB2 GABAB C (Glutamate) Human cryo-EM 6UOA 6UOA_refined 6.3 B Active 56 71 - - - - - - (R)-(3-aminopropyl)methylphosphinic acid pubchem chembl_ligand
small molecule Agonist GABA small molecule No No Shaye H, Ishchenko A, Lam JH, Han GW, Xue L, Rondard P, Pin J, Katritch V, Gati C, Cherezov V 10.1038/S41586-020-2408-4 2020-06-10 Yes
GABR2 GABAB2 GABAB C (Glutamate) Human cryo-EM 6UO9 6UO9_refined 4.8 B Active 61 73 - - - - - - (R)-(3-aminopropyl)methylphosphinic acid pubchem chembl_ligand
small molecule Agonist GABA small molecule No No Shaye H, Ishchenko A, Lam JH, Han GW, Xue L, Rondard P, Pin J, Katritch V, Gati C, Cherezov V 10.1038/S41586-020-2408-4 2020-06-10 Yes
PAR1 PAR1 Proteinase-activated A (Rhodopsin) Human X-ray 3VW7 3VW7_refined 2.2 A Intermediate 41 66 - - - - T4-Lysozyme - Vorapaxar pubchem
small molecule Antagonist thrombin protein 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
GPR52 GPR52 A orphans A (Rhodopsin) Human cryo-EM 6LI3 6LI3_refined 3.3 R Active 100 79 Gs αs Mini-Gs 61 - Nanobody-35 Apo (no ligand)
none Apo (no ligand) - - Yes No Lin X, Li M, Wang N, Wu Y, Luo Z, Guo S, Han G, 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
GPR52 GPR52 A orphans A (Rhodopsin) Human X-ray 6LI1 6LI1_refined 2.9 A Intermediate 48 81 - - - - Flavodoxin - - - - - - Yes No Lin X, Li M, Wang N, Wu Y, Luo Z, Guo S, Han G, 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
GPR52 GPR52 A orphans A (Rhodopsin) Human X-ray 6LI2 6LI2_refined 2.8 A Intermediate 48 80 - - - - Rubredoxin - - - - - - Yes No Lin X, Li M, Wang N, Wu Y, Luo Z, Guo S, Han G, 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
GPR52 GPR52 A orphans A (Rhodopsin) Human X-ray 6LI0 6LI0_refined 2.2 A Intermediate 48 81 - - - - Flavodoxin - c17 pubchem
small molecule Agonist - - Yes No Lin X, Li M, Wang N, Wu Y, Luo Z, Guo S, Han G, 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
MC4R MC4 Melanocortin A (Rhodopsin) Human X-ray 6W25 6W25_refined 2.8 A Intermediate 56 79 - - - - GlgA glycogen synthase - SHU9119
Calcium ion pubchem
peptide
ion		 Antagonist
Cofactor		 agouti, α-MSH, ACTH, γ-MSH, β-MSH, agouti-related protein protein Yes No Yu J, Gimenez LE, Hernandez CC, Wu Y, Wein AH, Han GW, McClary K, Mittal SR, Burdsall K, Stauch B, Wu L, Stevens SN, Peisley A, Williams SY, Chen V, Millhauser GL, Zhao S, Cone RD, Stevens RC 10.1126/SCIENCE.AAZ8995 2020-04-29 Yes
PTAFR PAF Platelet-activating factor A (Rhodopsin) Human X-ray 5ZKQ 5ZKQ_refined 2.9 B Intermediate 41 83 - - - - T4-Lysozyme - ABT-491 pubchem chembl_ligand
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
PTAFR PAF Platelet-activating factor A (Rhodopsin) Human X-ray 5ZKP - 2.8 A Other - 85 - - - - Flavodoxin - Foropafant pubchem
small molecule Antagonist 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
5HT1B 5-HT1B 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 4IAQ 4IAQ_refined 2.8 A Inactive 24 70 - - - - BRIL - Dihydroergotamine pubchem
small molecule Agonist 5-hydroxytryptamine, tryptamine, 5-HT-moduline small molecule Yes No Wang C, Jiang Y, Ma J, Wu H, Wacker D, Katritch V, Han GW, Liu W, Huang X, Vardy E, McCorvy JD, Gao X, Zhou XE, Melcher K, Zhang C, Bai F, Yang H, Yang L, Jiang H, Roth BL, Cherezov V, Stevens RC, Xu HE 10.1126/SCIENCE.1232807 2013-03-13 Yes
5HT1B 5-HT1B 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 4IAR 4IAR_refined 2.7 A Inactive 24 70 - - - - BRIL - Ergotamine pubchem
small molecule Agonist 5-hydroxytryptamine, tryptamine, 5-HT-moduline small molecule Yes No Wang C, Jiang Y, Ma J, Wu H, Wacker D, Katritch V, Han GW, Liu W, Huang X, Vardy E, McCorvy JD, Gao X, Zhou XE, Melcher K, Zhang C, Bai F, Yang H, Yang L, Jiang H, Roth BL, Cherezov V, Stevens RC, Xu HE 10.1126/SCIENCE.1232807 2013-03-13 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Human X-ray 4ZWJ 4ZWJ_refined 3.3 A Active 93 94 Visual S-arrestin - 86 T4-Lysozyme - Apo (no ligand)
none Apo (no ligand) Retinal small molecule 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 MHE, 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 JCH, 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
ACM5 M5 Acetylcholine (muscarinic) A (Rhodopsin) Human X-ray 6OL9 6OL9_refined 2.5 A Inactive 5 53 - - - - T4-Lysozyme - Tiotropium pubchem
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
S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human X-ray 3V2W - 3.4 A Inactive 1 68 - - - - T4-Lysozyme - (R)-3-Amino-4-(3-hexylphenylamino)-4-oxobutylphosphonic acid pubchem
small molecule Antagonist LPA, 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
S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human X-ray 3V2Y 3V2Y_refined 2.8 A Inactive 1 76 - - - - T4-Lysozyme - (R)-3-Amino-4-(3-hexylphenylamino)-4-oxobutylphosphonic acid pubchem
small molecule Antagonist LPA, 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 Yes
EDNRB ETB Endothelin A (Rhodopsin) Human X-ray 5X93 5X93_refined 2.2 A Inactive 15 71 - - - - T4-Lysozyme - K-8794 pubchem
small molecule Antagonist endothelin-3, Big endothelin-1, endothelin-2 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
EDNRB ETB Endothelin A (Rhodopsin) Human X-ray 5XPR 5XPR_refined 3.6 A Inactive 15 69 - - - - T4-Lysozyme - - - - endothelin-3, Big endothelin-1, endothelin-2 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
CNR2 CB2 Cannabinoid A (Rhodopsin) Human cryo-EM 6PT0 6PT0_refined 3.2 R Active 100 83 Gi/o αi1 - 100 - scFv16 Win 55212-2 pubchem chembl_ligand
small molecule Agonist 2-arachidonoylglycerol, anandamide small molecule Yes No Xing C, Zhuang Y, Xu T, Feng Z, Zhou XE, Chen M, Wang L, Meng X, Xue Y, Wang J, Liu H, McGuire TF, Zhao G, Melcher K, Zhang C, Xu HE, Xie X 10.1016/J.CELL.2020.01.007 2020-02-12 Yes
NK1R NK1 Tachykinin A (Rhodopsin) Human X-ray 6HLP 6HLP_refined 2.2 A Inactive 1 71 - - - - GIgA glycogen synthase - Netupitant pubchem chembl_ligand
small molecule Antagonist hemokinin 1, neuropeptide K, neuropeptide-γ, neurokinin A, neurokinin B, substance P peptide Yes No Schöppe J, Ehrenmann J, Klenk C, Rucktooa P, Schütz M, Doré AS, Plückthun A 10.1038/S41467-018-07939-8 2019-01-16 Yes
NK1R NK1 Tachykinin A (Rhodopsin) Human X-ray 6HLL 6HLL_refined 3.3 A Inactive 1 67 - - - - GIgA glycogen synthase - CP-99,994 pubchem chembl_ligand
small molecule Antagonist hemokinin 1, neuropeptide K, neuropeptide-γ, neurokinin A, neurokinin B, substance P peptide Yes No Schöppe J, Ehrenmann J, Klenk C, Rucktooa P, Schütz M, Doré AS, Plückthun A 10.1038/S41467-018-07939-8 2019-01-16 Yes
NK1R NK1 Tachykinin A (Rhodopsin) Human X-ray 6HLO 6HLO_refined 2.4 A Inactive 1 70 - - - - GIgA glycogen synthase - Aprepitant pubchem pubchem chembl_ligand
small molecule Antagonist hemokinin 1, neuropeptide K, neuropeptide-γ, neurokinin A, neurokinin B, substance P peptide Yes No Schöppe J, Ehrenmann J, Klenk C, Rucktooa P, Schütz M, Doré AS, Plückthun A 10.1038/S41467-018-07939-8 2019-01-16 Yes
CLTR1 CysLT1 Leukotriene A (Rhodopsin) Human X-ray 6RZ4 6RZ4_refined 2.7 A Intermediate 41 85 - - - - BRIL - Pranlukast pubchem chembl_ligand
small molecule Antagonist LTE4, LTD4, LTC4 small molecule Yes Yes Luginina A, Gusach A, Marin E, Mishin A, Brouillette R, Popov P, Shiriaeva A, Besserer-Offroy É, Longpré J, 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
CLTR1 CysLT1 Leukotriene A (Rhodopsin) Human X-ray 6RZ5 6RZ5_refined 2.5 B Intermediate 41 84 - - - - BRIL - Zafirlukast pubchem chembl_ligand
small molecule Antagonist LTE4, LTD4, LTC4 small molecule Yes Yes Luginina A, Gusach A, Marin E, Mishin A, Brouillette R, Popov P, Shiriaeva A, Besserer-Offroy É, Longpré J, 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
DRD3 D3 Dopamine A (Rhodopsin) Human cryo-EM 7CMU 7CMU_refined 3.0 R Active 100 68 Gi/o αi1 - 64 BRIL scFv16 Pramipexole pubchem
small molecule Agonist dopamine small molecule Yes No Xu P, Huang S, Mao C, Krumm BE, Zhou XE, Tan Y, Huang X, Liu Y, Shen D, Jiang Y, Yu X, Jiang H, Melcher K, Roth BL, Cheng X, Zhang Y, Xu HE 10.1016/J.MOLCEL.2021.01.003 2021-03-10 Yes
DRD3 D3 Dopamine A (Rhodopsin) Human cryo-EM 7CMV 7CMV_refined 2.7 R Active 100 68 Gi/o αi1 - 64 BRIL scFv16 (4Ar,10bR)-rel-4-Propyl-2,3,4,4a,5,10b-hexahydrochromeno[4,3-b][1,4]oxazin-9-ol pubchem chembl_ligand
small molecule Agonist dopamine small molecule Yes No Xu P, Huang S, Mao C, Krumm BE, Zhou XE, Tan Y, Huang X, Liu Y, Shen D, Jiang Y, Yu X, Jiang H, Melcher K, Roth BL, Cheng X, Zhang Y, Xu HE 10.1016/J.MOLCEL.2021.01.003 2021-03-10 Yes
NTR1 NTS1 Neurotensin A (Rhodopsin) Rat X-ray 4BWB - 3.6 A Inactive 3 72 - - - - - - neurotensin pubchem chembl_ligand
peptide Agonist neurotensin, large neurotensin, neuromedin N, large neuromedin N peptide Yes No Egloff P, Hillenbrand M, Klenk C, Batyuk A, Heine P, Balada S, Schlinkmann KM, Scott DJ, Schütz M, Plückthun A 10.1073/PNAS.1317903111 2014-01-29 No
NTR1 NTS1 Neurotensin A (Rhodopsin) Rat X-ray 3ZEV - 3.0 A Inactive 3 72 - - - - - - neurotensin pubchem chembl_ligand
peptide Agonist neurotensin, large neurotensin, neuromedin N, large neuromedin N peptide Yes No Egloff P, Hillenbrand M, Klenk C, Batyuk A, Heine P, Balada S, Schlinkmann KM, Scott DJ, Schütz M, Plückthun A 10.1073/PNAS.1317903111 2014-01-29 No
NTR1 NTS1 Neurotensin A (Rhodopsin) Rat X-ray 4BV0 - 3.1 A Inactive 3 70 - - - - - - neurotensin pubchem chembl_ligand
peptide Agonist neurotensin, large neurotensin, neuromedin N, large neuromedin N peptide Yes No Egloff P, Hillenbrand M, Klenk C, Batyuk A, Heine P, Balada S, Schlinkmann KM, Scott DJ, Schütz M, Plückthun A 10.1073/PNAS.1317903111 2014-01-29 No
NTR1 NTS1 Neurotensin A (Rhodopsin) Rat X-ray 4BUO 4BUO_refined 2.8 A Inactive 3 72 - - - - - - neurotensin pubchem chembl_ligand
peptide Agonist neurotensin, large neurotensin, neuromedin N, large neuromedin N peptide Yes No Egloff P, Hillenbrand M, Klenk C, Batyuk A, Heine P, Balada S, Schlinkmann KM, Scott DJ, Schütz M, Plückthun A 10.1073/PNAS.1317903111 2014-01-29 Yes
PE2R4 EP4 Prostanoid A (Rhodopsin) Human X-ray 5YWY 5YWY_refined 3.2 A Inactive 18 57 - - - - - Fab ONO-AE3-208 pubchem
small molecule Antagonist PGE1, PGD2, PGE2, PGF2α, PGI2 small molecule No No Toyoda Y, Morimoto K, Suno R, Horita S, Yamashita K, Hirata K, Sekiguchi Y, Yasuda S, Shiroishi M, Shimizu T, Urushibata Y, Kajiwara Y, Inazumi T, Hotta Y, Asada H, Nakane T, Shiimura Y, Nakagita T, Tsuge K, Yoshida S, Kuribara T, Hosoya T, Sugimoto Y, Nomura N, Sato M, Hirokawa T, Kinoshita M, Murata T, Takayama K, Yamamoto M, Narumiya S, Iwata S, Kobayashi T 10.1038/S41589-018-0131-3 2018-12-05 Yes
PE2R4 EP4 Prostanoid A (Rhodopsin) Human X-ray 5YHL 5YHL_refined 4.2 A Inactive 18 57 - - - - - Fab ONO-AE3-208-Br pubchem
small molecule Antagonist PGE1, PGD2, PGE2, PGF2α, PGI2 small molecule No No Toyoda Y, Morimoto K, Suno R, Horita S, Yamashita K, Hirata K, Sekiguchi Y, Yasuda S, Shiroishi M, Shimizu T, Urushibata Y, Kajiwara Y, Inazumi T, Hotta Y, Asada H, Nakane T, Shiimura Y, Nakagita T, Tsuge K, Yoshida S, Kuribara T, Hosoya T, Sugimoto Y, Nomura N, Sato M, Hirokawa T, Kinoshita M, Murata T, Takayama K, Yamamoto M, Narumiya S, Iwata S, Kobayashi T 10.1038/S41589-018-0131-3 2018-12-05 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey X-ray 6IBL 6IBL_refined 2.7 A Active 99 60 - - - - Thioredoxin 1 Carmelid antibody fragment Nb80 Formoterol pubchem chembl_ligand
small molecule Agonist noradrenaline, (-)-adrenaline, (-)-noradrenaline small molecule Yes No Warne T, Edwards PC, Doré AS, Leslie AGW, Tate CG 10.1101/436212 2019-01-09 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey X-ray 6H7N 6H7N_refined 2.5 A Active 99 60 - - - - Thioredoxin 1 Camelid antibody fragment Nb6B9 Xamoterol pubchem
small molecule Agonist noradrenaline, (-)-adrenaline, (-)-noradrenaline small molecule Yes No Warne T, Edwards PC, Doré AS, Leslie AGW, Tate CG 10.1101/436212 2018-10-17 Yes
AGTR1 AT1 Angiotensin A (Rhodopsin) Human X-ray 4ZUD 4ZUD_refined 2.8 A Inactive 7 75 - - - - BRIL - Olmesartan
small molecule Inverse agonist angiotensin II, angiotensin IV, angiotensin A, angiotensin III peptide Yes No Zhang H, Unal H, Desnoyer R, Han GW, Patel N, Katritch V, Karnik SS, Cherezov V, Stevens RC 10.1074/JBC.M115.689000 2015-10-07 Yes
AGTR2 AT2 Angiotensin A (Rhodopsin) Human X-ray 6JOD 6JOD_refined 3.2 A Active 93 84 - - - - BRIL Heavy chain of 4A03Fab
Light chain of 4A03Fab		 angiotensin II pubchem chembl_ligand
peptide Agonist angiotensin II, angiotensin III, angiotensin-(1-7) peptide Yes No Asada H, Inoue A, Ngako Kadji FM, Hirata K, Shiimura Y, Im D, Shimamura T, Nomura N, Iwanari H, Hamakubo T, Kusano-Arai O, Hisano H, Uemura T, Suno C, Aoki J, Iwata S 10.1016/J.STR.2019.12.003 2020-01-15 Yes
CCR9 CCR9 Chemokine A (Rhodopsin) Human X-ray 5LWE - 2.8 B Inactive 67 67 - - - - - - Vercirnon pubchem
small molecule Allosteric antagonist CCL25 protein No No Oswald C, Rappas M, Kean J, Doré AS, Errey JC, Bennett K, Deflorian F, Christopher JA, Jazayeri A, Mason JS, Congreve M, Cooke RM, Marshall FH 10.1038/NATURE20606 2016-12-07 Yes
FZD4 FZD4 Frizzled F (Frizzled) Human X-ray 6BD4 6BD4_refined 2.4 A Inactive 21 61 - - - - Rubredoxin - - - - norrin protein No No Yang S, Wu Y, Xu T, de Waal PW, He Y, Pu M, Chen Y, DeBruine ZJ, Zhang B, Zaidi SA, Popov P, Guo Y, Han GW, Lu Y, Suino-Powell K, Dong S, Harikumar KG, Miller LJ, Katritch V, Xu HE, Shui W, Stevens RC, Melcher K, Zhao S, Xu F 10.1038/S41586-018-0447-X 2018-08-22 Yes
5HT2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 4IB4 4IB4_refined 2.7 A Intermediate 41 59 - - - - BRIL - Ergotamine pubchem
small molecule Agonist 5-hydroxytryptamine small molecule Yes No Wacker D, Wang C, Katritch V, Han GW, Huang X, 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
GPBAR GPBA Bile acid A (Rhodopsin) Human cryo-EM 7CFM 7CFM_refined 3.0 R Active 100 83 Gs αs - 58 - Nanobody-35 P395 pubchem chembl_ligand
small molecule Agonist chenodeoxycholic acid, cholic acid, deoxycholic acid, lithocholic acid small molecule No No Yang F, Mao C, Guo L, Lin J, Ming Q, Xiao P, Wu X, Shen Q, Guo S, Shen D, Lu R, Zhang L, Huang S, Ping Y, Zhang C, Ma C, Zhang K, Liang X, Shen Y, Nan F, Yi F, Luca VC, Zhou J, Jiang C, Sun J, Xie X, Yu X, Zhang Y 10.1038/S41586-020-2569-1 2020-09-09 Yes
GPBAR GPBA Bile acid A (Rhodopsin) Human cryo-EM 7CFN 7CFN_refined 3.0 R Active 100 83 Gs αs - 59 - Nanobody-35 INT-777 pubchem
INT-777 pubchem
small molecule
small molecule		 Agonist
PAM		 chenodeoxycholic acid, cholic acid, deoxycholic acid, lithocholic acid small molecule No No Yang F, Mao C, Guo L, Lin J, Ming Q, Xiao P, Wu X, Shen Q, Guo S, Shen D, Lu R, Zhang L, Huang S, Ping Y, Zhang C, Ma C, Zhang K, Liang X, Shen Y, Nan F, Yi F, Luca VC, Zhou J, Jiang C, Sun J, Xie X, Yu X, Zhang Y 10.1038/S41586-020-2569-1 2020-09-09 Yes
GLR glucagon Glucagon B1 (Secretin) Human cryo-EM 6WPW 6WPW_refined 3.1 R Active 100 83 Gs αs - 56 - Nanobody-35 Glucagon derivative ZP3780
peptide Agonist glucagon peptide No No Hilger D, Kumar KK, Hu H, Pedersen MF, O’Brien ES, Giehm L, Jennings C, Eskici G, Inoue A, Lerch M, Mathiesen JM, Skiniotis G, Kobilka BK 10.1126/SCIENCE.ABA3373 2020-08-12 Yes
MC4R MC4 Melanocortin A (Rhodopsin) Human cryo-EM 7AUE 7AUE_refined 3.0 R Active 100 79 Gs αs - 59 - scFv16 Aminoserine
peptide Agonist agouti, α-MSH, ACTH, γ-MSH, β-MSH, agouti-related protein protein Yes No Israeli H, Degtjarik O, Fierro F, Chunilal V, Gill AK, Roth NJ, Botta J, Prabahar V, Peleg Y, Chan LF, Ben-Zvi D, McCormick PJ, Niv MY, Shalev-Benami M 10.1126/SCIENCE.ABF7958 2021-04-28 Yes
APJ apelin Apelin A (Rhodopsin) Human X-ray 5VBL 5VBL_refined 2.6 B Inactive 7 79 - - - - Rubredoxin - AMG3054
peptide Agonist Elabela/Toddler-32, Elabela/Toddler-21, Elabela/Toddler-11, [Pyr1]apelin-13, apelin-13, apelin-36, apelin-17, apelin receptor early endogenous ligand 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
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5G53 - 3.4 A Active 100 68 Gs αs Engineered G protein 50 - - NECA pubchem
small molecule Agonist adenosine small molecule Yes No Carpenter B, Nehmé R, Warne T, Leslie AGW, Tate CG 10.1038/NATURE18966 2016-08-03 Yes
CNR1 CB1 Cannabinoid A (Rhodopsin) Human cryo-EM 6N4B 6N4B_refined 3.0 R Active 100 58 Gi/o αi1 - 62 - scFv16 Fub-mdmb pubchem
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
OX1R OX1 Orexin A (Rhodopsin) Human X-ray 6TP4 6TP4_refined 3.0 A Inactive 1 70 - - - - - - ACT-462206 pubchem chembl_ligand
small molecule Antagonist orexin-A, orexin-B peptide No No Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré 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 (Rhodopsin) Human X-ray 6TQ7 6TQ7_refined 2.7 A Inactive 1 71 - - - - - - SB-334867 pubchem chembl_ligand
small molecule Antagonist orexin-A, orexin-B peptide No No Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré 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 (Rhodopsin) Human X-ray 6TO7 6TO7_refined 2.3 A Inactive 1 71 - - - - - - Suvorexant pubchem
small molecule Antagonist orexin-A, orexin-B peptide No No Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré 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 (Rhodopsin) Human X-ray 6TPJ 6TPJ_refined 2.7 A Inactive 1 68 - - - - GlgA glycogen synthase - Suvorexant pubchem
small molecule Antagonist orexin-A, orexin-B peptide No No Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré 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 (Rhodopsin) Human X-ray 6TOS 6TOS_refined 2.1 B Inactive 1 72 - - - - - - GSK1059865 pubchem chembl_ligand
small molecule Antagonist orexin-A, orexin-B peptide No No Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré 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
OX1R OX1 Orexin A (Rhodopsin) Human X-ray 6TOD 6TOD_refined 2.1 A Inactive 1 71 - - - - - - EMPA pubchem chembl_ligand
small molecule Antagonist orexin-A, orexin-B peptide No No Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré 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 (Rhodopsin) Human X-ray 6TPN 6TPN_refined 2.6 A Inactive 1 71 - - - - GlgA glycogen synthase - HTL6641 pubchem chembl_ligand
small molecule Antagonist orexin-A, orexin-B peptide No No Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré 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 (Rhodopsin) Human X-ray 6TQ4 6TQ4_refined 2.3 B Inactive 1 70 - - - - - - 2-[1-(phenylsulfonyl)-1,8-diazaspiro[4.5]decan-8-yl]-1,3-benzoxazole pubchem
small molecule Antagonist orexin-A, orexin-B peptide No No Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré 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 (Rhodopsin) Human X-ray 6TQ6 6TQ6_refined 2.6 B Inactive 1 71 - - - - - - 2-(5-methylsulfonylpyridin-3-yl)-1,1-bis(oxidanylidene)-4-[[2,4,6-tris(fluoranyl)phenyl]methyl]pyrido[2,3-e][1,2,4]thiadiazin-3-one pubchem
small molecule Antagonist orexin-A, orexin-B peptide No No Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré 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 (Rhodopsin) Human X-ray 6TOT 6TOT_refined 2.2 B Inactive 1 71 - - - - - - Lemborexant pubchem chembl_ligand
small molecule Antagonist orexin-A, orexin-B peptide No No Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré 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
OX1R OX1 Orexin A (Rhodopsin) Human X-ray 6TQ9 6TQ9_refined 2.7 B Inactive 1 71 - - - - - - SB-408124 pubchem chembl_ligand
small molecule Antagonist orexin-A, orexin-B peptide No No Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré 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 (Rhodopsin) Human X-ray 6TPG 6TPG_refined 2.7 A Inactive 1 69 - - - - GlgA glycogen synthase - EMPA pubchem chembl_ligand
small molecule Antagonist orexin-A, orexin-B peptide No No Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré 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 (Rhodopsin) Human X-ray 6TP3 6TP3_refined 3.0 A Inactive 1 74 - - - - - - Nemorexant pubchem
small molecule Antagonist orexin-A, orexin-B peptide No No Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré 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 (Rhodopsin) Human X-ray 6TP6 6TP6_refined 2.3 B Inactive 1 71 - - - - - - Filorexant pubchem chembl_ligand
small molecule Antagonist orexin-A, orexin-B peptide No No Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré 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
SCTR secretin Glucagon B1 (Secretin) Human cryo-EM 6WI9 6WI9_refined 4.3 R Active 100 84 Gs αs - 49 - Nanobody-35 secretin
peptide Agonist secretin, VIP peptide No No Dong M, Deganutti G, Piper SJ, Liang Y, Khoshouei M, Belousoff MJ, Harikumar KG, Reynolds CA, Glukhova A, Furness SGB, Christopoulos A, Danev R, Wootten D, Sexton PM, Miller LJ 10.1038/S41467-020-17791-4 2020-08-12 Yes
SCTR secretin Glucagon B1 (Secretin) Human cryo-EM 6WZG 6WZG_refined 2.3 R Active 100 86 Gs αs - 61 - Nanobody-35 secretin
peptide Agonist secretin, VIP peptide No No Dong M, Deganutti G, Piper SJ, Liang Y, Khoshouei M, Belousoff MJ, Harikumar KG, Reynolds CA, Glukhova A, Furness SGB, Christopoulos A, Danev R, Wootten D, Sexton PM, Miller LJ 10.1038/S41467-020-17791-4 2020-08-12 Yes
V2R V2 Vasopressin and oxytocin A (Rhodopsin) Human cryo-EM 7KH0 7KH0_refined 2.8 R Active 100 74 Gs αs - 58 - scFv16
Nanobody-35		 Argipressin pubchem chembl_ligand
peptide Agonist vasopressin, oxytocin peptide Yes No Wang L, Xu J, Cao S, Sun D, Liu H, Lu Q, Liu Z, Du Y, Zhang C 10.1038/S41422-021-00483-Z 2021-05-26 Yes
AA1R A1 Adenosine A (Rhodopsin) Human X-ray 5UEN 5UEN_refined 3.2 B Inactive 1 91 - - - - BRIL - DU172 pubchem
small molecule Antagonist adenosine small molecule Yes No Glukhova A, Thal DM, Nguyen AT, Vecchio EA, Jörg M, Scammells PJ, May LT, Sexton PM, Christopoulos A 10.1016/J.CELL.2017.01.042 2017-03-01 Yes
5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human cryo-EM 6WHA 6WHA_refined 3.4 A Active 100 52 Gq/11 αq Gq-Gi2-Gs chimera 59 BRIL scFv16 25-CN-NBOH pubchem
small molecule Agonist 5-hydroxytryptamine, tryptamine small molecule Yes No Kim K, Che T, Panova O, DiBerto JF, Lyu J, Krumm BE, Wacker D, Robertson MJ, Seven AB, Nichols DE, Shoichet BK, Skiniotis G, Roth BL 10.1016/J.CELL.2020.08.024 2020-09-23 Yes
5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 6WH4 6WH4_refined 3.4 C Inactive 1 59 - - - - BRIL - CHEMBL428892 pubchem chembl_ligand
small molecule Inverse agonist 5-hydroxytryptamine, tryptamine small molecule Yes No Kim K, Che T, Panova O, DiBerto JF, Lyu J, Krumm BE, Wacker D, Robertson MJ, Seven AB, Nichols DE, Shoichet BK, Skiniotis G, Roth BL 10.1016/J.CELL.2020.08.024 2020-09-23 Yes
5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 6WGT 6WGT_refined 3.4 B Inactive 1 59 - - - - BRIL - Lysergide pubchem
small molecule Agonist 5-hydroxytryptamine, tryptamine small molecule Yes No Kim K, Che T, Panova O, DiBerto JF, Lyu J, Krumm BE, Wacker D, Robertson MJ, Seven AB, Nichols DE, Shoichet BK, Skiniotis G, Roth BL 10.1016/J.CELL.2020.08.024 2020-09-23 Yes
OPRX NOP Opioid A (Rhodopsin) Human X-ray 5DHG 5DHG_refined 3.0 A Inactive 7 76 - - - - BRIL - C-35 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, Caló G, Katritch V, Stevens RC 10.1016/J.STR.2015.07.024 2015-10-21 Yes
OPRX NOP Opioid A (Rhodopsin) Human X-ray 5DHH 5DHH_refined 3.0 A Inactive 7 76 - - - - BRIL - SB-612111 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, Caló G, Katritch V, Stevens RC 10.1016/J.STR.2015.07.024 2015-10-21 Yes
5HT2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 5TUD 5TUD_refined 3.0 D Active 80 58 - - - - BRIL Antibody Ergotamine pubchem
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
PE2R3 EP3 Prostanoid A (Rhodopsin) Human X-ray 6M9T 6M9T_refined 2.5 A Active 83 70 - - - - T4-Lysozyme - Misoprostol-FA pubchem
small molecule Agonist PGE1, PGD2, PGE2, PGF2α, PGI2 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
OPRK κ Opioid A (Rhodopsin) Human X-ray 6VI4 6VI4_refined 3.3 B Inactive 7 73 - - - - - Nanobody 6 JDTic pubchem
small molecule Antagonist α-neoendorphin, [Leu]enkephalin, [Met]enkephalin, dynorphin A-(1-13), dynorphin A, dynorphin A-(1-8), dynorphin B, β-endorphin, β-neoendorphin, big dynorphin 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
GABR2 GABAB2 GABAB C (Glutamate) Human cryo-EM 7C7S 7C7S_refined 2.9 B Active 52 71 - - - - - - CGP54626 pubchem
small molecule Antagonist GABA small molecule No No Mao C, Shen C, Li C, Shen D, Xu C, Zhang S, Zhou R, Shen Q, Chen L, Jiang Z, Liu J, Zhang Y 10.1038/S41422-020-0350-5 2020-07-01 Yes
GABR2 GABAB2 GABAB C (Glutamate) Human cryo-EM 7C7Q 7C7Q_refined 3.0 B Active 100 71 - - - - - - Baclofen pubchem
BHFF pubchem
small molecule
small molecule		 Agonist
PAM		 GABA small molecule No No Mao C, Shen C, Li C, Shen D, Xu C, Zhang S, Zhou R, Shen Q, Chen L, Jiang Z, Liu J, Zhang Y 10.1038/S41422-020-0350-5 2020-07-01 Yes
GLP1R GLP-1 Glucagon B1 (Secretin) Human X-ray 5NX2 5NX2_refined 3.7 A Intermediate 73 84 - - - - - - Truncated protein agonist
peptide Agonist glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) peptide No No Jazayeri A, Rappas M, Brown AJH, Kean J, Errey JC, Robertson NJ, Fiez-Vandal C, Andrews SP, Congreve M, Bortolato A, Mason JS, Baig AH, Teobald I, Doré AS, Weir M, Cooke RM, Marshall FH 10.1038/NATURE22800 2017-06-14 Yes
P2Y12 P2Y12 P2Y A (Rhodopsin) Human X-ray 4NTJ 4NTJ_refined 2.6 A Intermediate 41 78 - - - - BRIL - AZD1283 pubchem
small molecule Antagonist ADP small molecule Yes No Zhang K, Zhang J, Gao Z, Zhang D, Zhu L, Han GW, Moss SM, Paoletta S, Kiselev E, Lu W, Fenalti G, Zhang W, Müller CE, Yang H, Jiang H, Cherezov V, Katritch V, Jacobson KA, Stevens RC, Wu B, Zhao Q 10.1038/NATURE13083 2014-03-26 Yes
CRFR1 CRF1 Corticotropin-releasing factor B1 (Secretin) Human cryo-EM 6P9X 6P9X_refined 2.9 R Active 100 65 Gs αs - 49 - Nanobody-35 Corticoliberin pubchem
peptide Agonist urocortin 2, corticotrophin-releasing hormone, urocortin 1 peptide No No Liang Y, Belousoff MJ, Zhao P, Koole C, Fletcher MM, Truong TT, Julita V, Christopoulos G, Xu HE, Zhang Y, Khoshouei M, Christopoulos A, Danev R, Sexton PM, Wootten D 10.1016/J.MOLCEL.2020.01.012 2020-02-05 Yes
PACR PAC1 VIP and PACAP B1 (Secretin) Human cryo-EM 6P9Y 6P9Y_refined 3.0 R Active 100 55 Gs αs - 49 - Nanobody-35 PACAP pubchem
peptide Agonist VIP, PACAP-27, PACAP-38, PHM, PHV, PHI peptide No No Liang Y, Belousoff MJ, Zhao P, Koole C, Fletcher MM, Truong TT, Julita V, Christopoulos G, Xu HE, Zhang Y, Khoshouei M, Christopoulos A, Danev R, Sexton PM, Wootten D 10.1016/J.MOLCEL.2020.01.012 2020-02-05 Yes
CCR5 CCR5 Chemokine A (Rhodopsin) Human X-ray 5UIW 5UIW_refined 2.2 A Inactive 30 85 - - - - Rubredoxin - 5P7-CCL5
protein Antagonist CCL16, CCL14, CCL3, CCL5, CCL7, CCL13, CCL8, CCL4, CCL2, CCL11 protein 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
VIPR1 VPAC1 VIP and PACAP B1 (Secretin) Human cryo-EM 6VN7 6VN7_refined 3.2 R Active 100 58 Gs αs - 61 - Nanobody-35 PACAP pubchem
peptide Agonist secretin, GHRH, VIP, PACAP-27, PACAP-38, PHM, PHV, PHI peptide No No Duan J, Shen D, Zhou XE, Bi P, Liu Q, Tan Y, Zhuang Y, Zhang H, Xu P, Huang S, Ma S, He X, Melcher K, Zhang Y, Xu HE, Jiang Y 10.1038/S41467-020-17933-8 2020-09-02 Yes
GLP1R GLP-1 Glucagon B1 (Secretin) Human cryo-EM 6X1A 6X1A_refined 2.5 R Active 100 84 Gs αs - 89 - Nanobody-35 PF-06882961 pubchem
small molecule Agonist glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) peptide No No Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, Šenel P, Stewart GD, Liang Y, Glukhova A, Venugopal H, Christopoulos A, Furness SGB, Miller LJ, Reedtz-Runge S, Langmead CJ, Gloriam DE, Danev R, Sexton PM, Wootten D 10.1101/2020.08.16.252585 2020-09-09 Yes
GLP1R GLP-1 Glucagon B1 (Secretin) Human cryo-EM 6X19 - 2.1 R Active 100 84 Gs αs - 89 - Nanobody-35 CHU-128 pubchem
small molecule Agonist glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) peptide No No Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, Šenel P, Stewart GD, Liang Y, Glukhova A, Venugopal H, Christopoulos A, Furness SGB, Miller LJ, Reedtz-Runge S, Langmead CJ, Gloriam DE, Danev R, Sexton PM, Wootten D 10.1101/2020.08.16.252585 2020-09-09 Yes
GLP1R GLP-1 Glucagon B1 (Secretin) Human cryo-EM 6X18 6X18_refined 2.1 R Active 100 83 Gs αs - 90 - Nanobody-35 GLP-1
peptide Agonist glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) peptide No No Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, Šenel P, Stewart GD, Liang Y, Glukhova A, Venugopal H, Christopoulos A, Furness SGB, Miller LJ, Reedtz-Runge S, Langmead CJ, Gloriam DE, Danev R, Sexton PM, Wootten D 10.1101/2020.08.16.252585 2020-09-09 Yes
TA2R TP Prostanoid A (Rhodopsin) Human X-ray 6IIV 6IIV_refined 3.0 A Intermediate 41 87 - - - - BRIL - Daltroban pubchem chembl_ligand
small molecule Antagonist PGD2, PGE2, PGF2α, PGI2, thromboxane A2 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
TA2R TP Prostanoid A (Rhodopsin) Human X-ray 6IIU 6IIU_refined 2.5 A Intermediate 41 87 - - - - BRIL - Ramatroban pubchem chembl_ligand
small molecule Antagonist PGD2, PGE2, PGF2α, PGI2, thromboxane A2 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
GRM1 mGlu1 Metabotropic glutamate C (Glutamate) Human X-ray 4OR2 4OR2_refined 2.8 B Inactive 1 22 - - - - BRIL - FITM pubchem
small molecule NAM L-glutamic acid small molecule No No Wu H, Wang C, Gregory KJ, Han GW, Cho HP, Xia Y, Niswender CM, Katritch V, Meiler J, Cherezov V, Conn PJ, Stevens RC 10.1126/SCIENCE.1249489 2014-03-19 Yes
GLP2R GLP-2 Glucagon B1 (Secretin) Human cryo-EM 7D68 7D68_refined 3.0 R Active 100 53 Gs αs - 57 - Nanobody-35 glucagon pubchem
peptide Agonist glucagon-like peptide 2-(2-33), glucagon-like peptide 2, glucagon-like peptide 2-(3-33) peptide No No Sun W, Chen L, Zhou Q, Zhao L, Yang D, Zhang H, Cong Z, Shen D, Zhao F, Zhou F, Cai X, Chen Y, Zhou Y, Gadgaard S, van der Velden WJC, Zhao S, Jiang Y, Rosenkilde MM, Xu HE, Zhang Y, Wang M 10.1038/S41422-020-00442-0 2020-12-16 Yes
OX2R OX2 Orexin A (Rhodopsin) Human cryo-EM 7L1V 7L1V_refined 3.0 R Active 100 64 Gs αs Engineered G alpha 58 - scFv16 4'-Methoxy-N,N-dimethyl-3'-{[3-(2-{[2-(2H-1,2,3-triazol-2-yl)benzene-1-carbonyl]amino}ethyl)phenyl]sulfamoyl}[1,1'-biphenyl]-3-carboxamide pubchem
small molecule Agonist orexin-A, orexin-B peptide Yes No Hong C, Byrne NJ, Zamlynny B, Tummala S, Xiao L, Shipman JM, Partridge AT, Minnick C, Breslin MJ, Rudd MT, Stachel SJ, Rada VL, Kern JC, Armacost KA, Hollingsworth SA, O’Brien JA, Hall DL, McDonald TP, Strickland C, Brooun A, Soisson SM, Hollenstein K 10.1038/S41467-021-21087-6 2021-02-10 Yes
OX2R OX2 Orexin A (Rhodopsin) Human cryo-EM 7L1U 7L1U_refined 3.2 R Active 100 63 Gs αs Engineered G alpha 58 - scFv16 orexin-A
peptide Agonist orexin-A, orexin-B peptide Yes No Hong C, Byrne NJ, Zamlynny B, Tummala S, Xiao L, Shipman JM, Partridge AT, Minnick C, Breslin MJ, Rudd MT, Stachel SJ, Rada VL, Kern JC, Armacost KA, Hollingsworth SA, O’Brien JA, Hall DL, McDonald TP, Strickland C, Brooun A, Soisson SM, Hollenstein K 10.1038/S41467-021-21087-6 2021-02-10 Yes
FFAR1 FFA1 Free fatty acid A (Rhodopsin) Human X-ray 5TZR 5TZR_refined 2.2 A Intermediate 41 91 - - - - T4-Lysozyme - MK-8666 pubchem
small molecule Agonist α-linolenic acid, docosahexaenoic acid, oleic 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
FFAR1 FFA1 Free fatty acid A (Rhodopsin) Human X-ray 5TZY 5TZY_refined 3.2 A Intermediate 41 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		 α-linolenic acid, docosahexaenoic acid, oleic 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
AA1R A1 Adenosine A (Rhodopsin) Human cryo-EM 6D9H 6D9H_refined 3.6 R Active 100 88 Gi/o αi2 - 59 - - adenosine pubchem
small molecule Agonist adenosine small molecule Yes No Draper-Joyce CJ, Khoshouei M, Thal DM, Liang Y, Nguyen ATN, Furness SGB, Venugopal H, Baltos J, Plitzko JM, Danev R, Baumeister W, May LT, Wootten D, Sexton PM, Glukhova A, Christopoulos A 10.1038/S41586-018-0236-6 2018-06-20 Yes
CALCR CT Calcitonin B1 (Secretin) Human cryo-EM 6NIY 6NIY_refined 3.3 R Active 100 55 Gs αs - 43 - - calcitonin
peptide Agonist calcitonin, adrenomedullin, amylin, α-CGRP, β-CGRP, adrenomedullin 2/intermedin peptide No No dal Maso E, Glukhova A, Zhu Y, Garcia-Nafria J, Tate CG, Atanasio S, Reynolds CA, Ramírez-Aportela E, Carazo J, Hick CA, Furness SGB, Hay DL, Liang Y, Miller LJ, Christopoulos A, Wang M, Wootten D, Sexton PM 10.1021/ACSPTSCI.8B00056 2019-01-23 Yes
5HT2C 5-HT2C 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 6BQG 6BQG_refined 3.0 A Active 80 62 - - - - BRIL - Ergotamine pubchem
small molecule Agonist 5-hydroxytryptamine small molecule Yes No Peng Y, McCorvy JD, Harpsøe K, Lansu K, Yuan S, Popov P, Qu L, Pu M, Che T, Nikolajsen LF, Huang X, Wu Y, Shen L, Bjørn-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 Z 10.1016/J.CELL.2018.01.001 2018-02-14 Yes
5HT2C 5-HT2C 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 6BQH 6BQH_refined 2.7 A Inactive 1 63 - - - - BRIL - Ritanserin pubchem
small molecule Inverse agonist 5-hydroxytryptamine small molecule Yes No Peng Y, McCorvy JD, Harpsøe K, Lansu K, Yuan S, Popov P, Qu L, Pu M, Che T, Nikolajsen LF, Huang X, Wu Y, Shen L, Bjørn-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 Z 10.1016/J.CELL.2018.01.001 2018-02-14 Yes
CALRL calcitonin-like Calcitonin B1 (Secretin) Human cryo-EM 6UUS 6UUS_refined 2.4 R Active 100 74 Gs αs - 48 - Nanobody-35
RAMP3		 adrenomedullin
peptide Agonist adrenomedullin, α-CGRP, β-CGRP, adrenomedullin 2/intermedin, α-CGRP-(8-37) (rat) peptide No No Liang Y, 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
CALRL calcitonin-like Calcitonin B1 (Secretin) Human cryo-EM 6UVA 6UVA_refined 2.3 R Active 100 75 Gs αs - 48 - Nanobody-35
RAMP3		 Adrenomedullin-2
peptide Agonist adrenomedullin, α-CGRP, β-CGRP, adrenomedullin 2/intermedin, α-CGRP-(8-37) (rat) peptide No No Liang Y, 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
CALRL calcitonin-like Calcitonin B1 (Secretin) Human cryo-EM 6UUN 6UUN_refined 3.0 R Active 100 77 Gs αs - 48 - Nanobody-35
RAMP2		 adrenomedullin
peptide Agonist adrenomedullin, α-CGRP, β-CGRP, adrenomedullin 2/intermedin, α-CGRP-(8-37) (rat) peptide No No Liang Y, 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
SMO SMO Frizzled F (Frizzled) Human cryo-EM 6XBL 6XBL_refined 3.9 R Active 100 59 Gi/o αi1 - 61 - scFv16 Cholesterol pubchem
SAG pubchem
N/A
small molecule		 Agonist
PAM		 constitutive constitutive No No Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X 10.1038/S41589-020-0646-2 2020-09-30 Yes
SMO SMO Frizzled F (Frizzled) Human cryo-EM 6XBM 6XBM_refined 3.2 R Active 100 42 Gi/o αi1 - 61 - scFv16 24,25-Epoxy-cholesterol pubchem
24,25-Epoxy-cholesterol pubchem
small molecule
small molecule		 Agonist
PAM		 constitutive constitutive No No Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X 10.1038/S41589-020-0646-2 2020-09-30 Yes
SMO SMO Frizzled F (Frizzled) Human cryo-EM 6XBJ 6XBJ_refined 3.9 R Active 100 59 Gi/o αi1 - 61 - scFv16 Cholesterol pubchem
N/A Agonist constitutive constitutive No No Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X 10.1038/S41589-020-0646-2 2020-09-30 Yes
SMO SMO Frizzled F (Frizzled) Human cryo-EM 6XBK 6XBK_refined 3.2 R Active 100 59 Gi/o αi1 - 61 - scFv16 Cholesterol pubchem
N/A Agonist constitutive constitutive No No Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X 10.1038/S41589-020-0646-2 2020-09-30 Yes
PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human X-ray 6FJ3 6FJ3_refined 2.5 A Inactive 0 62 - - - - GlgA glycogen synthase - ePTH
peptide Agonist (partial) PTHrP, TIP39, PTH, PTHrP-(1-36) protein No No Ehrenmann J, Schöppe J, Klenk C, Rappas M, Kummer L, Doré AS, Plückthun A 10.1038/S41594-018-0151-4 2018-11-21 Yes
ACM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human X-ray 6KP6 6KP6_refined 3.0 A Inactive 5 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 Z, Hua T 10.1107/S2052252520000597 2020-03-11 Yes
Q80KM9 US28 Unclassified A (Rhodopsin) strain AD169 X-ray 5WB1 5WB1_refined 3.5 A Active 94 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
Q80KM9 US28 Unclassified A (Rhodopsin) strain AD169 X-ray 5WB2 5WB2_refined 3.5 A Active 94 82 - - - - - Nanobody CX3CL1
peptide Agonist - - 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
OPRD δ Opioid A (Rhodopsin) Human X-ray 6PT3 6PT3_refined 3.3 A Active 76 78 - - - - BRIL - DPI-287 pubchem
small molecule Agonist α-neoendorphin, [Leu]enkephalin, [Met]enkephalin, dynorphin A-(1-13), dynorphin A, dynorphin A-(1-8), dynorphin B, endomorphin-1, 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 Z, Müller CE, Stevens RC 10.1126/SCIADV.AAX9115 2019-12-11 Yes
OPRD δ Opioid A (Rhodopsin) Human X-ray 6PT2 6PT2_refined 2.8 A Active 76 78 - - - - BRIL - KGCHM07
peptide Agonist α-neoendorphin, [Leu]enkephalin, [Met]enkephalin, dynorphin A-(1-13), dynorphin A, dynorphin A-(1-8), dynorphin B, endomorphin-1, 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 Z, Müller CE, Stevens RC 10.1126/SCIADV.AAX9115 2019-12-11 Yes
ACM1 M1 Acetylcholine (muscarinic) A (Rhodopsin) Human X-ray 6WJC 6WJC_refined 2.6 A Inactive 5 62 - - - - T4-Lysozyme - Hyoscyamine pubchem
Muscarinic toxin 7
small molecule
peptide		 Antagonist
NAM		 acetylcholine small molecule No No Maeda S, Xu J, N. Kadji FM, Clark MJ, Zhao J, Tsutsumi N, Aoki J, Sunahara RK, Inoue A, Garcia KC, Kobilka BK 10.1126/SCIENCE.AAX2517 2020-07-08 Yes
NPY1R Y1 Neuropeptide Y A (Rhodopsin) 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, Kögler 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
NPY1R Y1 Neuropeptide Y A (Rhodopsin) Human X-ray 5ZBQ 5ZBQ_refined 2.7 A Inactive 1 80 - - - - T4-Lysozyme - UR-MK299 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, Kögler 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
ADRB2 β2 Adrenoceptors A (Rhodopsin) 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, (-)-adrenaline, (-)-noradrenaline, Zn2+ small molecule Yes No Rasmussen SGF, DeVree BT, Zou Y, Kruse AC, Chung KY, Kobilka TS, Thian FS, Chae PS, Pardon E, Calinski D, Mathiesen JM, Shah STA, Lyons JA, Caffrey M, Gellman SH, Steyaert J, Skiniotis G, Weis WI, Sunahara RK, Kobilka BK 10.1038/NATURE10361 2011-07-20 Yes
EDNRB ETB Endothelin A (Rhodopsin) Human X-ray 5GLI 5GLI_refined 2.5 A Inactive 15 71 - - - - T4-Lysozyme - Apo (no ligand)
none Apo (no ligand) endothelin-3, Big endothelin-1, endothelin-2 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
EDNRB ETB Endothelin A (Rhodopsin) Human X-ray 5GLH 5GLH_refined 2.8 A Inactive 15 66 - - - - T4-Lysozyme - Endothelin-1 pubchem
peptide Agonist endothelin-3, Big endothelin-1, endothelin-2 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 (Rhodopsin) Human X-ray 2YDO 2YDO_refined 3.0 A Active 76 73 - - - - - - adenosine pubchem
small molecule Agonist adenosine small molecule Yes No Lebon G, Warne T, Edwards PC, Bennett K, Langmead CJ, Leslie AGW, Tate CG 10.1038/NATURE10136 2011-05-18 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 2YDV 2YDV_refined 2.6 A Active 76 75 - - - - - - NECA pubchem
small molecule Agonist adenosine small molecule Yes No Lebon G, Warne T, Edwards PC, Bennett K, Langmead CJ, Leslie AGW, Tate CG 10.1038/NATURE10136 2011-05-18 Yes
ADRB2 β2 Adrenoceptors A (Rhodopsin) Human X-ray 6PS1 6PS1_refined 3.2 A Inactive 0 68 - - - - T4-Lysozyme - Timolol pubchem
small molecule Antagonist noradrenaline, (-)-adrenaline, (-)-noradrenaline, Zn2+ 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 (Rhodopsin) Human X-ray 6PS5 6PS5_refined 2.9 A Inactive 0 68 - - - - T4-Lysozyme - (S)-Propranolol pubchem
small molecule Antagonist noradrenaline, (-)-adrenaline, (-)-noradrenaline, Zn2+ 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 (Rhodopsin) Human X-ray 6PS0 6PS0_refined 3.4 A Inactive 0 68 - - - - T4-Lysozyme - Carazolol pubchem
small molecule Antagonist noradrenaline, (-)-adrenaline, (-)-noradrenaline, Zn2+ 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
MTR1A MT1 Melatonin A (Rhodopsin) Human X-ray 6PS8 6PS8_refined 3.3 A Inactive 1 83 - - - - GIgA glycogen synthase - 2-phenylmelatonin pubchem
small molecule Agonist melatonin small molecule No 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 (Rhodopsin) Human X-ray 6PS6 6PS6_refined 2.7 A Inactive 0 68 - - - - T4-Lysozyme - Timolol pubchem
small molecule Antagonist noradrenaline, (-)-adrenaline, (-)-noradrenaline, Zn2+ 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
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 6PS7 6PS7_refined 1.9 A Inactive 0 72 - - - - BRIL - ZM241385 pubchem
small molecule Antagonist adenosine small molecule Yes Yes 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 (Rhodopsin) Human X-ray 6PS4 6PS4_refined 2.6 A Inactive 0 68 - - - - T4-Lysozyme - ICI-118551 pubchem
small molecule Antagonist noradrenaline, (-)-adrenaline, (-)-noradrenaline, Zn2+ 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 (Rhodopsin) Human X-ray 6PS2 6PS2_refined 2.4 A Inactive 0 68 - - - - T4-Lysozyme - (S)-Alprenolol pubchem
small molecule Antagonist noradrenaline, (-)-adrenaline, (-)-noradrenaline, Zn2+ 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 (Rhodopsin) Human X-ray 6PS3 6PS3_refined 2.5 A Inactive 0 68 - - - - T4-Lysozyme - (S)-Carvedilol pubchem
small molecule Antagonist noradrenaline, (-)-adrenaline, (-)-noradrenaline, Zn2+ 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
Q9WTK1 BLT1 Leukotriene A (Rhodopsin) Guinea pig X-ray 5X33 5X33_refined 3.7 A Inactive 7 78 - - - - T4-Lysozyme - BIIL-260 pubchem
small molecule Antagonist 20-hydroxy-LTB4, 12R-HETE, LTB4 small molecule Yes No Hori T, Okuno T, Hirata K, Yamashita K, Kawano Y, Yamamoto M, Hato M, Nakamura M, Shimizu T, Yokomizo T, Miyano M, Yokoyama S 10.1038/NCHEMBIO.2547 2018-01-03 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey cryo-EM 6TKO 6TKO_refined 3.3 A Active 99 58 Beta Beta-arrestin-1 - 78 - Fab30 heavy chain
Fab30 light chain		 Formoterol pubchem chembl_ligand
small molecule Agonist noradrenaline, (-)-adrenaline, (-)-noradrenaline small molecule Yes No Lee Y, Warne T, Nehmé R, Pandey S, Dwivedi-Agnihotri H, Chaturvedi M, Edwards PC, García-Nafría J, Leslie AGW, Shukla AK, Tate CG 10.1038/S41586-020-2419-1 2020-06-17 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 2X72 2X72_refined 3.0 A Active 93 94 Gi/o αt1 Only H5 3 - - Retinal (11-cis) pubchem
small molecule Agonist Retinal small molecule No No Standfuss J, Edwards PC, D’Antona A, Fransen M, Xie G, Oprian DD, Schertler GFX 10.1038/NATURE09795 2011-03-16 Yes
GPBAR GPBA Bile acid A (Rhodopsin) Human cryo-EM 7BW0 7BW0_refined 3.9 R Active 100 85 Gs αs - 56 BRIL Nanobody-35 - - - chenodeoxycholic acid, cholic acid, deoxycholic acid, lithocholic acid small molecule No No Chen G, Wang X, Ge Y, Ma L, Chen Q, Liu H, Du Y, Ye RD, Hu H, Ren R 10.1038/S41392-020-00262-Z 2020-09-02 Yes
GLP1R GLP-1 Glucagon B1 (Secretin) Human cryo-EM 6B3J 6B3J_refined 3.3 R Active 100 82 Gs αs - 49 - - Exendin-P5
peptide Agonist glucagon, glucagon-like peptide 1-(7-36) amide, glucagon-like peptide 1-(7-37) peptide No No Liang Y, 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 M, Miller LJ, Christopoulos A, Sexton PM, Wootten D 10.1038/NATURE25773 2018-02-21 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 2I37 - 4.2 A Inactive 36 91 - - - - - - Apo (no ligand)
none Apo (no ligand) Retinal small molecule No No Salom D, Lodowski DT, Stenkamp RE, Trong IL, Golczak M, Jastrzebska B, Harris T, Ballesteros JA, Palczewski K 10.1073/PNAS.0608022103 2006-10-17 No
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 2I36 - 4.1 A Inactive 36 94 - - - - - - Apo (no ligand)
none Apo (no ligand) Retinal small molecule No No Salom D, Lodowski DT, Stenkamp RE, Trong IL, Golczak M, Jastrzebska B, Harris T, Ballesteros JA, Palczewski K 10.1073/PNAS.0608022103 2006-10-17 No
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 2I35 - 3.8 A Inactive 36 94 - - - - - - Retinal (11-cis) pubchem
small molecule Inverse agonist Retinal small molecule No No Salom D, Lodowski DT, Stenkamp RE, Trong IL, Golczak M, Jastrzebska B, Harris T, Ballesteros JA, Palczewski K 10.1073/PNAS.0608022103 2006-10-17 No
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5OLH 5OLH_refined 2.6 A Inactive 0 72 - - - - BRIL - Vipadenant 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, Doré AS 10.1038/S41598-017-18570-W 2018-01-17 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5OLO 5OLO_refined 3.1 A Inactive 0 72 - - - - BRIL - Tozadenant pubchem chembl_ligand
small molecule Antagonist adenosine small molecule Yes No Rucktooa P, Cheng RKY, Segala E, Geng T, Errey JC, Brown GA, Cooke RM, Marshall FH, Doré AS 10.1038/S41598-017-18570-W 2018-01-17 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5OLG 5OLG_refined 1.9 A Inactive 0 72 - - - - BRIL - ZM241385 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, Doré AS 10.1038/S41598-017-18570-W 2018-01-17