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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, Pandy-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 5 71 - - - - T4-Lysozyme - Methyl 4-[[(4R,4aS,7R,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl]amino]-4-oxobutanoate pubchem
small molecule Antagonist [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
CNR2 CB2 Cannabinoid A (Rhodopsin) Human X-ray 5ZTY 5ZTY_refined 2.8 A Inactive 5 80 - - - - T4-Lysozyme - AM10257 pubchem
small molecule Antagonist 2-arachidonoylglycerol, anandamide small molecule Yes No Li X, Hua T, Vemuri K, Ho JH, 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 ZJ 10.1016/J.CELL.2018.12.011 2019-01-30 Yes
CCR2 CCR2 Chemokine A (Rhodopsin) Human X-ray 5T1A 5T1A_refined 2.8 A Inactive 24 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, Zacarias NV, de Vries H, Han GW, Gustavsson M, Dabros M, Zhao C, Cherney RJ, Carter P, Stamos D, Abagyan R, Cherezov V, Stevens RC, IJzerman AP, Heitman LH, Tebben A, Kufareva I, Handel TM 10.1038/NATURE20605 2016-12-14 Yes
CASR CaS Calcium-sensing C (Glutamate) Human cryo-EM 7DTT 7DTT_refined 3.8 A Inactive 39 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 7DTW 7DTW_refined 4.5 A Inactive 39 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
CASR CaS Calcium-sensing C (Glutamate) Human cryo-EM 7DTU 7DTU_refined 4.4 A Inactive 39 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 39 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
OXYR OT Vasopressin and oxytocin A (Rhodopsin) Human X-ray 6TPK - 3.2 A Inactive 18 68 - - - - GlgA glycogen synthase - Retosiban pubchem
small molecule Antagonist vasopressin, oxytocin peptide Yes No - 10.1126/SCIADV.ABB5419 2020-08-05 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 - 10.1038/S41586-018-0241-9 2018-06-20 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 HW, Kobilka BK 10.1038/S41589-020-0492-2 2020-04-15 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 HW, Kobilka BK 10.1038/S41589-020-0492-2 2020-04-15 Yes
CALRL calcitonin-like Calcitonin B1 (Secretin) Human cryo-EM 7KNT 7KNT_refined 3.2 R Inactive 10 74 - - - - - RAMP1 Apo (no ligand)
none Apo (no ligand) adrenomedullin, α-CGRP, β-CGRP, adrenomedullin 2/intermedin, α-CGRP-(8-37) (rat) peptide No No Josephs TM, Belousoff MJ, Liang YL, 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
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 YL, 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
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, PGF, 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
OPSD Rhodopsin Opsins A (Rhodopsin) Bovine X-ray 1GZM 1GZM_refined 2.7 A Inactive 28 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
CXCR2 CXCR2 Chemokine A (Rhodopsin) Human X-ray 6LFL 6LFL_refined 3.2 A Inactive 6 76 - - - - GlgA 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 ZJ 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 ZJ 10.1038/S41586-020-2492-5 2020-09-02 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 ZJ 10.1038/S41586-020-2492-5 2020-09-02 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 CM, 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 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 CM, 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
MTR1A MT1 Melatonin A (Rhodopsin) Human cryo-EM 7DB6 7DB6_refined 3.3 D Active 100 79 Gi/o αi1 - 62 - scFv16 Ramelteon pubchem chembl_ligand
small molecule Agonist melatonin small molecule Yes No Okamoto HH, Miyauchi H, Inoue A, Raimondi F, Tsujimoto H, Kusakizako T, Shihoya W, Yamashita K, Suno R, Nomura N, Kobayashi T, Iwata S, Nishizawa T, Nureki O 10.1038/S41594-021-00634-1 2021-08-18 Yes
CASR CaS Calcium-sensing C (Glutamate) Human cryo-EM 7DD5 - 3.2 A Inactive 73 74 - - - - - - Calcium ion pubchem
NPS-2143 pubchem
Tryptophan pubchem chembl_ligand
ion
small molecule
amino acid
Agonist
NAM
PAM
L-tryptophan, spermine, Ca2+, Mg2+ amino acid No No Wen T, Wang Z, Chen X, Ren Y, Lu X, Xing Y, Lu J, Chang S, Zhang X, Shen Y, Yang X 10.1126/SCIADV.ABG1483 2021-06-16 Yes
CASR CaS Calcium-sensing C (Glutamate) Human cryo-EM 7DD6 7DD6_refined 3.2 B Active 73 73 - - - - - - Calcium ion pubchem
Tryptophan pubchem chembl_ligand
ion
amino acid
Agonist
PAM
L-tryptophan, spermine, Ca2+, Mg2+ amino acid No No Wen T, Wang Z, Chen X, Ren Y, Lu X, Xing Y, Lu J, Chang S, Zhang X, Shen Y, Yang X 10.1126/SCIADV.ABG1483 2021-06-16 Yes
CASR CaS Calcium-sensing C (Glutamate) Human cryo-EM 7DD7 7DD7_refined 3.2 B Active 73 73 - - - - - - Calcium ion pubchem
Tryptophan pubchem chembl_ligand
Evocalcet pubchem
ion
amino acid
small molecule
Agonist
PAM
PAM
L-tryptophan, spermine, Ca2+, Mg2+ amino acid No No Wen T, Wang Z, Chen X, Ren Y, Lu X, Xing Y, Lu J, Chang S, Zhang X, Shen Y, Yang X 10.1126/SCIADV.ABG1483 2021-06-16 Yes
OPRD δ Opioid A (Rhodopsin) Human X-ray 4N6H 4N6H_refined 1.8 A Inactive 5 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 XP, Thompson AA, Cherezov V, Roth BL, Stevens RC 10.1038/NATURE12944 2013-12-25 Yes
Q08BG4 LPA6 Lysophospholipid (LPA) A (Rhodopsin) Zebrafish X-ray 5XSZ 5XSZ_refined 3.2 A Intermediate 32 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 32 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, Dore AS, Geschwindner S, Grebner C, Hermansson NO, Jazayeri A, Johansson P, Leong L, Prihandoko R, Rappas M, Soutter H, Snijder A, Sundstrom L, Tehan B, Thornton P, Troast D, Wiggin G, Zhukov A, Marshall FH, Dekker N 10.1038/NATURE22309 2017-05-03 Yes
PAR2 PAR2 Proteinase-activated A (Rhodopsin) Human X-ray 5NDZ 5NDZ_refined 3.6 A Intermediate 32 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, Dore AS, Geschwindner S, Grebner C, Hermansson NO, Jazayeri A, Johansson P, Leong L, Prihandoko R, Rappas M, Soutter H, Snijder A, Sundstrom L, Tehan B, Thornton P, Troast D, Wiggin G, Zhukov A, Marshall FH, Dekker N 10.1038/NATURE22309 2017-05-03 Yes
PAR2 PAR2 Proteinase-activated A (Rhodopsin) Human X-ray 5NJ6 5NJ6_refined 4.0 A Intermediate 32 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, Dore AS, Geschwindner S, Grebner C, Hermansson NO, Jazayeri A, Johansson P, Leong L, Prihandoko R, Rappas M, Soutter H, Snijder A, Sundstrom L, Tehan B, Thornton P, Troast D, Wiggin G, Zhukov A, Marshall FH, Dekker N 10.1038/NATURE22309 2017-05-03 Yes
GRM5 mGlu5 Metabotropic glutamate C (Glutamate) Human X-ray 4OO9 4OO9_refined 2.6 A Inactive 1 20 - - - - T4-Lysozyme - Mavoglurant pubchem
small molecule NAM L-glutamic acid amino acid No No Dore 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
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
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
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 TIP39, PTHrP, PTH, PTHrP-(1-36) peptide No No Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y 10.1126/SCIENCE.AAV7942 2019-04-17 Yes
PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human cryo-EM 6NBH - 3.5 R Active 100 64 Gs αs - 57 - Nanobody-35 Long-acting parathyroid hormone analog
peptide Agonist TIP39, PTHrP, PTH, PTHrP-(1-36) peptide No No Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y 10.1126/SCIENCE.AAV7942 2019-04-17 Yes
PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human cryo-EM 6NBF - 3.0 R Active 100 62 Gs αs - 58 - Nanobody-35 Long-acting parathyroid hormone analog
peptide Agonist TIP39, PTHrP, PTH, PTHrP-(1-36) peptide No No Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y 10.1126/SCIENCE.AAV7942 2019-04-17 Yes
GIPR GIP Glucagon B1 (Secretin) Human cryo-EM 7DTY 7DTY_refined 3.0 R Active 100 79 Gs αs - 59 - Nanobody-35 GIP pubchem
peptide Agonist gastric inhibitory polypeptide peptide No No Zhao F, Zhang C, Zhou Q, Hang K, Zou X, Chen Y, Wu F, Rao Q, Dai A, Yin W, Shen DD, Zhang Y, Xia T, Stevens RC, Xu HE, Yang D, Zhao L, Wang MW 10.7554/ELIFE.68719 2021-08-04 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
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
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 3VGA - 3.1 A Inactive 0 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 0 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
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, PGF, PGI2 small molecule Yes No Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, 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, PGF, PGI2 small molecule Yes No Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y 10.1126/SCIADV.ABF1268 2021-05-05 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, PGF, PGI2 small molecule Yes No Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y 10.1126/SCIADV.ABF1268 2021-05-05 Yes
GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human cryo-EM 7MTR 7MTR_refined 3.3 A Active 100 88 - - - - - - 2-methoxy-6-propyl-N-(2-{4-[(1H-tetrazol-5-yl)methoxy]phenyl}ethyl)thieno[2,3-d]pyrimidin-4-amine pubchem
Glutamic acid pubchem
small molecule
amino acid
Ago-PAM
Agonist
L-glutamic acid amino acid No No Seven AB, Barros-Alvarez X, de Lapeyriere M, Papasergi-Scott MM, Robertson MJ, Zhang C, Nwokonko RM, Gao Y, Meyerowitz JG, Rocher JP, Schelshorn D, Kobilka BK, Mathiesen JM, Skiniotis G 10.1038/S41586-021-03680-3 2021-07-07 Yes
GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human cryo-EM 7MTQ 7MTQ_refined 3.7 B Inactive 20 85 - - - - - - 2-[(1s,2s)-2-Carboxycyclopropyl]-3-(9h-Xanthen-9-Yl)-D-Alanine pubchem chembl_ligand
small molecule Antagonist L-glutamic acid amino acid No No Seven AB, Barros-Alvarez X, de Lapeyriere M, Papasergi-Scott MM, Robertson MJ, Zhang C, Nwokonko RM, Gao Y, Meyerowitz JG, Rocher JP, Schelshorn D, Kobilka BK, Mathiesen JM, Skiniotis G 10.1038/S41586-021-03680-3 2021-07-07 Yes
GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human cryo-EM 7MTS 7MTS_refined 3.2 A Active 100 90 Gi/o αi1 - 58 - - 2-methoxy-6-propyl-N-(2-{4-[(1H-tetrazol-5-yl)methoxy]phenyl}ethyl)thieno[2,3-d]pyrimidin-4-amine pubchem
Glutamic acid pubchem
small molecule
amino acid
Ago-PAM
Agonist
L-glutamic acid amino acid No No Seven AB, Barros-Alvarez X, de Lapeyriere M, Papasergi-Scott MM, Robertson MJ, Zhang C, Nwokonko RM, Gao Y, Meyerowitz JG, Rocher JP, Schelshorn D, Kobilka BK, Mathiesen JM, Skiniotis G 10.1038/S41586-021-03680-3 2021-07-07 Yes
C5AR1 C5a1 Complement peptide A (Rhodopsin) Human X-ray 5O9H 5O9H_refined 2.7 A Inactive 8 84 - - - - - - NDT 9513727 pubchem
small molecule Antagonist C5a, C3a, C5a des-Arg, ribosomal protein S19 protein Yes No Robertson N, Rappas M, Dore AS, Brown J, Bottegoni G, Koglin M, Cansfield J, Jazayeri A, Cooke RM, Marshall FH 10.1038/NATURE25025 2018-01-10 Yes
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
ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human X-ray 5ZK3 5ZK3_refined 2.6 A Inactive 4 59 - - - - BRIL - 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
ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human X-ray 5ZKB 5ZKB_refined 3.0 A Inactive 4 60 - - - - BRIL - AF-DX 384 pubchem
small molecule Antagonist acetylcholine small molecule No No Suno R, Lee S, Maeda S, Yasuda S, Yamashita K, Hirata K, Horita S, Tawaramoto MS, Tsujimoto H, Murata T, Kinoshita M, Yamamoto M, Kobilka BK, Vaidehi N, Iwata S, Kobayashi T 10.1038/S41589-018-0152-Y 2018-11-21 Yes
ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human X-ray 5YC8 5YC8_refined 2.5 A Inactive 4 60 - - - - BRIL - 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 5ZKC 5ZKC_refined 2.3 A Inactive 4 60 - - - - BRIL - 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 4 59 - - - - BRIL - 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
Q3KSP2 BILF1 Unclassified A (Rhodopsin) strain GD1 cryo-EM 7JHJ 7JHJ_refined 3.2 R Active 100 89 Gi/o αi1 - 62 - scFv16 Apo (no ligand)
none Apo (no ligand) - - No No Tsutsumi N, Qu Q, Mavri M, Baggesen MS, Maeda S, Waghray D, Berg C, Kobilka BK, Rosenkilde MM, Skiniotis G, Garcia KC 10.1016/J.IMMUNI.2021.06.001 2021-07-07 Yes
DRD1 D1 Dopamine A (Rhodopsin) Human cryo-EM 7JV5 7JV5_refined 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 XP, Shen DD, Xu T, Liu YF, 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 XP, Shen DD, Xu T, Liu YF, 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 XP, Shen DD, Xu T, Liu YF, 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 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 XP, Shen DD, Xu T, Liu YF, 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
SUCR1 succinate Succinate A (Rhodopsin) Rat X-ray 6RNK 6RNK_refined 1.9 A Intermediate 32 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 VP 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 32 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 VP 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 4 47 - - - - T4-Lysozyme - (1R,2R,4S,5S,7s)-7-({[4-fluoro-2-(thiophen-2-yl)phenyl]carbamoyl}oxy)-9,9-dimethyl-3-oxa-9-azatricyclo[3.3.1.0~2,4~]nonan-9-ium pubchem
small molecule Antagonist acetylcholine small molecule No No Liu H, Hofmann J, Fish I, Schaake B, Eitel K, Bartuschat A, Kaindl J, Rampp H, Banerjee A, Hubner H, Clark MJ, Vincent SG, Fisher JT, Heinrich MR, Hirata K, Liu X, Sunahara RK, Shoichet BK, Kobilka BK, Gmeiner P 10.1073/PNAS.1813988115 2018-11-28 Yes
CNR1 CB1 Cannabinoid A (Rhodopsin) Human X-ray 5TGZ 5TGZ_refined 2.8 A Inactive 10 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 JH, Zvonok N, Zhou H, Kufareva I, Wu B, Zhao Q, Hanson MA, Bohn LM, Makriyannis A, Stevens RC, Liu ZJ 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 LH, Mao C, Zhou XE, Shen DD, de Waal PW, Bi P, Li C, Jiang Y, Wang MW, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE 10.1016/J.MOLCEL.2020.01.013 2020-02-12 Yes
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 LH, Mao C, Zhou XE, Shen DD, de Waal PW, Bi P, Li C, Jiang Y, Wang MW, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE 10.1016/J.MOLCEL.2020.01.013 2020-02-12 Yes
CXCR4 CXCR4 Chemokine A (Rhodopsin) Human X-ray 3ODU 3ODU_refined 2.5 A Inactive 5 83 - - - - T4-Lysozyme - IT1t pubchem
small molecule Antagonist CXCL12α, CXCL12γ, CXCL12δ, CXCL12ε, CXCL12φ, CXCL12β, CXCL12 protein Yes No Wu B, Chien EY, Mol CD, Fenalti G, Liu W, Katritch V, Abagyan R, Brooun A, Wells P, Bi FC, Hamel DJ, Kuhn P, Handel TM, Cherezov V, Stevens RC 10.1126/SCIENCE.1194396 2010-10-27 Yes
CXCR4 CXCR4 Chemokine A (Rhodopsin) Human X-ray 3OE0 3OE0_refined 2.9 A Inactive 5 78 - - - - T4-Lysozyme - CVX15
peptide Antagonist CXCL12α, CXCL12γ, CXCL12δ, CXCL12ε, CXCL12φ, CXCL12β, CXCL12 protein Yes No Wu B, Chien EY, Mol CD, Fenalti G, Liu W, Katritch V, Abagyan R, Brooun A, Wells P, Bi FC, Hamel DJ, Kuhn P, Handel TM, Cherezov V, Stevens RC 10.1126/SCIENCE.1194396 2010-10-27 Yes
CXCR4 CXCR4 Chemokine A (Rhodopsin) Human X-ray 3OE9 - 3.1 A Inactive 5 74 - - - - T4-Lysozyme - IT1t pubchem
small molecule Antagonist CXCL12α, CXCL12γ, CXCL12δ, CXCL12ε, CXCL12φ, CXCL12β, CXCL12 protein Yes No Wu B, Chien EY, Mol CD, Fenalti G, Liu W, Katritch V, Abagyan R, Brooun A, Wells P, Bi FC, Hamel DJ, Kuhn P, Handel TM, Cherezov V, Stevens RC 10.1126/SCIENCE.1194396 2010-10-27 No
CXCR4 CXCR4 Chemokine A (Rhodopsin) Human X-ray 3OE8 - 3.1 A Inactive 5 76 - - - - T4-Lysozyme - IT1t pubchem
small molecule Antagonist CXCL12α, CXCL12γ, CXCL12δ, CXCL12ε, CXCL12φ, CXCL12β, CXCL12 protein Yes No Wu B, Chien EY, Mol CD, Fenalti G, Liu W, Katritch V, Abagyan R, Brooun A, Wells P, Bi FC, Hamel DJ, Kuhn P, Handel TM, Cherezov V, Stevens RC 10.1126/SCIENCE.1194396 2010-10-27 No
CXCR4 CXCR4 Chemokine A (Rhodopsin) Human X-ray 3OE6 - 3.2 A Inactive 5 77 - - - - T4-Lysozyme - IT1t pubchem
small molecule Antagonist CXCL12α, CXCL12γ, CXCL12δ, CXCL12ε, CXCL12φ, CXCL12β, CXCL12 protein Yes No Wu B, Chien EY, Mol CD, Fenalti G, Liu W, Katritch V, Abagyan R, Brooun A, Wells P, Bi FC, Hamel DJ, Kuhn P, Handel TM, Cherezov V, Stevens RC 10.1126/SCIENCE.1194396 2010-10-27 No
LSHR LH Glycoprotein hormone A (Rhodopsin) Human cryo-EM 7FII - 4.3 R Active 100 82 Gs αs - 71 - - Glycoprotein alpha
Choriogonadotropin beta
protein
protein
Agonist LH, hCG protein Yes No Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE 10.1038/S41586-021-03924-2 2021-09-29 Yes
LSHR LH Glycoprotein hormone A (Rhodopsin) Human cryo-EM 7FIJ 7FIJ_refined 3.8 R Inactive 12 80 - - - - - - Apo (no ligand)
none Apo (no ligand) LH, hCG protein Yes No Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE 10.1038/S41586-021-03924-2 2021-09-29 Yes
LSHR LH Glycoprotein hormone A (Rhodopsin) Human cryo-EM 7FIG - 3.9 R Active 100 79 Gs αs - 71 - Nanobody-35 Glycoprotein alpha
Choriogonadotropin beta
protein
protein
Agonist LH, hCG protein Yes No Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE 10.1038/S41586-021-03924-2 2021-09-29 Yes
LSHR LH Glycoprotein hormone A (Rhodopsin) Human cryo-EM 7FIH - 3.2 R Active 100 79 Gs αs - 56 - - Glycoprotein alpha
Choriogonadotropin beta
5-Amino-N-(1,1-dimethylethyl)-2-(methylthio)-4-[3-[[2-(4-morpholinyl)acetyl]amino]phenyl]thieno[2,3-d]pyrimidine-6-carboxamide pubchem
protein
protein
small molecule
Agonist LH, hCG protein Yes No Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE 10.1038/S41586-021-03924-2 2021-09-29 Yes
OPRM μ Opioid A (Rhodopsin) Mouse X-ray 5C1M 5C1M_refined 2.1 A Active 96 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 4MQS 4MQS_refined 3.5 A Active 99 59 - - - - - Nanobody Iperoxo pubchem
small molecule Agonist acetylcholine small molecule Yes No Kruse AC, Ring AM, Manglik A, Hu J, Hu K, Eitel K, Hubner H, Pardon E, Valant C, Sexton PM, Christopoulos A, Felder CC, Gmeiner P, Steyaert J, Weis WI, Garcia KC, Wess J, Kobilka BK 10.1038/NATURE12735 2013-11-27 Yes
ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human X-ray 4MQT 4MQT_refined 3.7 A Active 99 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, Hubner H, Pardon E, Valant C, Sexton PM, Christopoulos A, Felder CC, Gmeiner P, Steyaert J, Weis WI, Garcia KC, Wess J, Kobilka BK 10.1038/NATURE12735 2013-11-27 Yes
P2RY1 P2Y1 P2Y A (Rhodopsin) Human X-ray 4XNW 4XNW_refined 2.7 A Intermediate 32 78 - - - - Rubredoxin - MRS2500 pubchem
small molecule Antagonist ADP, ATP small molecule Yes No Zhang D, Gao ZG, 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 32 78 - - - - Rubredoxin - BPTU pubchem
small molecule NAM ADP, ATP small molecule Yes No Zhang D, Gao ZG, 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 4UHR 4UHR_refined 2.6 A Active 69 75 - - - - - - CGS-21680 pubchem
small molecule Agonist adenosine small molecule Yes No Lebon G, Edwards PC, Leslie AG, Tate CG 10.1124/MOL.114.097360 2015-04-08 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 4UG2 4UG2_refined 2.6 A Active 69 71 - - - - - - CGS-21680 pubchem
small molecule Agonist adenosine small molecule Yes No Lebon G, Edwards PC, Leslie AG, Tate CG 10.1124/MOL.114.097360 2015-04-08 Yes
ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human cryo-EM 6U1N 6U1N_refined 4.0 R Active 90 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
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
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
MTR1A MT1 Melatonin A (Rhodopsin) Human X-ray 6ME2 6ME2_refined 2.8 A Inactive 1 83 - - - - GlgA 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 XP, Gati C, Batyuk A, Slocum ST, Ishchenko A, Brehm W, White TA, Michaelian N, Madsen C, Zhu L, Grant TD, Grandner JM, Shiriaeva A, Olsen RHJ, Tribo AR, Yous S, Stevens RC, Weierstall U, Katritch V, Roth BL, Liu W, Cherezov V 10.1038/S41586-019-1141-3 2019-04-24 Yes
MTR1A MT1 Melatonin A (Rhodopsin) Human X-ray 6ME3 6ME3_refined 2.9 A Inactive 1 82 - - - - GlgA glycogen synthase - 2-phenylmelatonin pubchem
small molecule Agonist melatonin small molecule No No Stauch B, Johansson LC, McCorvy JD, Patel N, Han GW, Huang XP, Gati C, Batyuk A, Slocum ST, Ishchenko A, Brehm W, White TA, Michaelian N, Madsen C, Zhu L, Grant TD, Grandner JM, Shiriaeva A, Olsen RHJ, Tribo AR, Yous S, Stevens RC, Weierstall U, Katritch V, Roth BL, Liu W, Cherezov V 10.1038/S41586-019-1141-3 2019-04-24 Yes
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 XP, Gati C, Batyuk A, Slocum ST, Ishchenko A, Brehm W, White TA, Michaelian N, Madsen C, Zhu L, Grant TD, Grandner JM, Shiriaeva A, Olsen RHJ, Tribo AR, Yous S, Stevens RC, Weierstall U, Katritch V, Roth BL, Liu W, Cherezov V 10.1038/S41586-019-1141-3 2019-04-24 Yes
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 XP, Gati C, Batyuk A, Slocum ST, Ishchenko A, Brehm W, White TA, Michaelian N, Madsen C, Zhu L, Grant TD, Grandner JM, Shiriaeva A, Olsen RHJ, Tribo AR, Yous S, Stevens RC, Weierstall U, Katritch V, Roth BL, Liu W, Cherezov V 10.1038/S41586-019-1141-3 2019-04-24 Yes
GABR1 GABAB1 GABAB C (Glutamate) Human cryo-EM 6W2Y 6W2Y_refined 3.2 B Inactive 26 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
GABR2 GABAB2 GABAB C (Glutamate) Human cryo-EM 6W2X - 3.6 B Inactive 26 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
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
CCR7 CCR7 Chemokine A (Rhodopsin) Human X-ray 6QZH 6QZH_refined 2.1 A Inactive 6 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 CY, Mattle D, Vonach JM, Gast A, Kuglstatter A, Rudolph MG, Nogly P, Benz J, Dawson RJP, 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 28 93 - - - - - - Apo (no ligand)
none Apo (no ligand) Retinal small molecule No No Zhao DY, Poge M, Morizumi T, Gulati S, Van Eps N, Zhang J, Miszta P, Filipek S, Mahamid J, Plitzko JM, Baumeister W, Ernst OP, Palczewski K 10.1074/JBC.RA119.010089 2019-08-21 Yes
CLTR2 CysLT2 Leukotriene A (Rhodopsin) Human X-ray 6RZ8 6RZ8_refined 2.7 A Intermediate 32 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 E, Longpre JM, Ishchenko A, Popov P, Patel N, Fujimoto T, Maruyama T, Stauch B, Ergasheva M, Romanovskaia D, Stepko A, Kovalev K, Shevtsov M, Gordeliy V, Han GW, Katritch V, Borshchevskiy V, Sarret P, Mishin A, Cherezov V 10.1038/S41467-019-13348-2 2019-12-11 Yes
CLTR2 CysLT2 Leukotriene A (Rhodopsin) Human X-ray 6RZ6 6RZ6_refined 2.4 A Intermediate 32 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 E, Longpre JM, Ishchenko A, Popov P, Patel N, Fujimoto T, Maruyama T, Stauch B, Ergasheva M, Romanovskaia D, Stepko A, Kovalev K, Shevtsov M, Gordeliy V, Han GW, Katritch V, Borshchevskiy V, Sarret P, Mishin A, Cherezov V 10.1038/S41467-019-13348-2 2019-12-11 Yes
CLTR2 CysLT2 Leukotriene A (Rhodopsin) Human X-ray 6RZ9 6RZ9_refined 2.7 A Intermediate 32 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 E, Longpre JM, Ishchenko A, Popov P, Patel N, Fujimoto T, Maruyama T, Stauch B, Ergasheva M, Romanovskaia D, Stepko A, Kovalev K, Shevtsov M, Gordeliy V, Han GW, Katritch V, Borshchevskiy V, Sarret P, Mishin A, Cherezov V 10.1038/S41467-019-13348-2 2019-12-11 Yes
CLTR2 CysLT2 Leukotriene A (Rhodopsin) Human X-ray 6RZ7 6RZ7_refined 2.4 A Intermediate 32 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 E, Longpre JM, Ishchenko A, Popov P, Patel N, Fujimoto T, Maruyama T, Stauch B, Ergasheva M, Romanovskaia D, Stepko A, Kovalev K, Shevtsov M, Gordeliy V, Han GW, Katritch V, Borshchevskiy V, Sarret P, Mishin A, Cherezov V 10.1038/S41467-019-13348-2 2019-12-11 Yes
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 YQ, Mao C, Xiao P, Zhao RJ, Jiang Y, Yang Z, An WT, Shen DD, Yang F, Zhang H, Qu C, Shen Q, Tian C, Li ZJ, Li S, Wang GY, Tao X, Wen X, Zhong YN, Yang J, Yi F, Yu X, Xu HE, Zhang Y, Sun JP 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 YQ, Mao C, Xiao P, Zhao RJ, Jiang Y, Yang Z, An WT, Shen DD, Yang F, Zhang H, Qu C, Shen Q, Tian C, Li ZJ, Li S, Wang GY, Tao X, Wen X, Zhong YN, Yang J, Yi F, Yu X, Xu HE, Zhang Y, Sun JP 10.1038/S41586-020-03083-W 2021-02-03 Yes
SMO SMO Frizzled F (Frizzled) Human X-ray 5L7I 5L7I_refined 3.3 B Inactive 4 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 4 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
NTR1 NTS1 Neurotensin A (Rhodopsin) Human cryo-EM 6PWC 6PWC_refined 4.9 R Active 84 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 YL, 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 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 MW, Wu B 10.1038/NATURE22363 2017-05-24 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 MW, Wu B 10.1038/NATURE22363 2017-05-24 Yes
HRH1 H1 Histamine A (Rhodopsin) Human X-ray 3RZE 3RZE_refined 3.1 A Inactive 4 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
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 ZJ, Wang MW, 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 ZJ, Wang MW, 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
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 LH, Zhou Q, Mao C, Cheng X, Shen DD, 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 MW 10.1038/S41467-020-18945-0 2020-11-18 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
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
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 RKY, 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 XP, 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 XP, Dror RO, Shoichet BK, Roth BL 10.1126/SCIENCE.AAN5468 2017-10-18 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 DD, Yen HY, Robinson CV, Harpsoe 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 DD, Yen HY, Robinson CV, Harpsoe 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 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 DD, Yen HY, Robinson CV, Harpsoe 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 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 DD, Yen HY, Robinson CV, Harpsoe 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 DD, Yen HY, Robinson CV, Harpsoe 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
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 EY, Liu W, Zhao Q, Katritch V, Han GW, Hanson MA, Shi L, Newman AH, Javitch JA, Cherezov V, Stevens RC 10.1126/SCIENCE.1197410 2010-11-03 Yes
OPRK κ Opioid A (Rhodopsin) Human X-ray 6B73 6B73_refined 3.1 A Active 96 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 MY, Pardon E, Steyaert J, Huang XP, 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
ADRB3 β3 Adrenoceptors A (Rhodopsin) Dog cryo-EM 7DH5 7DH5_refined 3.2 R Active 100 68 Gs αs - 59 - Nanobody-35 Mirabegron pubchem
small molecule Agonist (-)-adrenaline, (-)-noradrenaline, (±)-adrenaline small molecule Yes No Nagiri C, Kobayashi K, Tomita A, Kato M, Kobayashi K, Yamashita K, Nishizawa T, Inoue A, Shihoya W, Nureki O 10.1016/J.MOLCEL.2021.06.024 2021-08-04 Yes
PAR1 PAR1 Proteinase-activated A (Rhodopsin) Human X-ray 3VW7 3VW7_refined 2.2 A Intermediate 32 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
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
PTAFR PAF Platelet-activating factor A (Rhodopsin) Human X-ray 5ZKQ 5ZKQ_refined 2.9 B Intermediate 32 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
5HT1B 5-HT1B 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 4IAQ 4IAQ_refined 2.8 A Inactive 18 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 XP, 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 18 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 XP, 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
MC4R MC4 Melanocortin A (Rhodopsin) Human X-ray 6W25 6W25_refined 2.8 A Intermediate 45 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
GABR2 GABAB2 GABAB C (Glutamate) Human cryo-EM 6VJM 6VJM_refined 4.0 B Inactive 30 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 JP, 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 Inactive 30 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 JP, 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 Inactive 36 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 JP, 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 97 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 JP, Katritch V, Gati C, Cherezov V 10.1038/S41586-020-2408-4 2020-06-10 Yes
GPR52 GPR52 A orphans A (Rhodopsin) Human X-ray 6LI1 6LI1_refined 2.9 A Intermediate 38 81 - - - - Flavodoxin - - - - - - Yes No Lin X, Li M, Wang N, Wu Y, Luo Z, Guo S, Han GW, Li S, Yue Y, Wei X, Xie X, Chen Y, Zhao S, Wu J, Lei M, Xu F 10.1038/S41586-020-2019-0 2020-02-26 Yes
GPR52 GPR52 A orphans A (Rhodopsin) Human X-ray 6LI2 6LI2_refined 2.8 A Intermediate 38 80 - - - - Rubredoxin - - - - - - Yes No Lin X, Li M, Wang N, Wu Y, Luo Z, Guo S, Han GW, Li S, Yue Y, Wei X, Xie X, Chen Y, Zhao S, Wu J, Lei M, Xu F 10.1038/S41586-020-2019-0 2020-02-26 Yes
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 GW, Li S, Yue Y, Wei X, Xie X, Chen Y, Zhao S, Wu J, Lei M, Xu F 10.1038/S41586-020-2019-0 2020-02-26 Yes
GPR52 GPR52 A orphans A (Rhodopsin) Human X-ray 6LI0 6LI0_refined 2.2 A Intermediate 38 81 - - - - Flavodoxin - c17 pubchem
small molecule Agonist - - Yes No Lin X, Li M, Wang N, Wu Y, Luo Z, Guo S, Han GW, Li S, Yue Y, Wei X, Xie X, Chen Y, Zhao S, Wu J, Lei M, Xu F 10.1038/S41586-020-2019-0 2020-02-26 Yes
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 - 10.1101/436212 2018-10-17 Yes
ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey X-ray 6IBL 6IBL_refined 2.7 A Active 99 60 - - - - Thioredoxin 1 Camelid antibody fragment Nb80 Formoterol pubchem chembl_ligand
small molecule Agonist noradrenaline, (-)-adrenaline, (-)-noradrenaline small molecule Yes No - 10.1101/436212 2019-01-09 Yes
OPSD Rhodopsin Opsins A (Rhodopsin) Human X-ray 4ZWJ 4ZWJ_refined 3.3 A Active 95 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 MH, Zhang C, Moeller A, West GM, Pascal BD, Van Eps N, Caro LN, Vishnivetskiy SA, Lee RJ, Suino-Powell KM, Gu X, Pal K, Ma J, Zhi X, Boutet S, Williams GJ, Messerschmidt M, Gati C, Zatsepin NA, Wang D, James D, Basu S, Roy-Chowdhury S, Conrad CE, Coe J, Liu H, Lisova S, Kupitz C, Grotjohann I, Fromme R, Jiang Y, Tan M, Yang H, Li J, Wang M, Zheng Z, Li D, Howe N, Zhao Y, Standfuss J, Diederichs K, Dong Y, Potter CS, Carragher B, Caffrey M, Jiang H, Chapman HN, Spence JC, Fromme P, Weierstall U, Ernst OP, Katritch V, Gurevich VV, Griffin PR, Hubbell WL, Stevens RC, Cherezov V, Melcher K, Xu HE 10.1038/NATURE14656 2015-07-29 Yes
S1PR3 S1P3 Lysophospholipid (S1P) A (Rhodopsin) Human cryo-EM 7EW2 7EW2_refined 3.1 R Active 100 77 Gi/o αi1 - 64 - scFv16 S-fingolimod phosphate ester pubchem chembl_ligand
lipid Agonist sphingosine 1-phosphate, sphingosylphosphorylcholine small molecule Yes No Zhao C, Cheng L, Wang W, Wang H, Luo Y, Feng Y, Wang X, Fu H, Cai Y, Yang S, Fu P, Yan W, Shao Z 10.1038/S41422-021-00567-W 2021-09-29 Yes
S1PR3 S1P3 Lysophospholipid (S1P) A (Rhodopsin) Human cryo-EM 7EW3 - 3.1 R Active 100 77 Gi/o αi1 - 64 - scFv16 sphingosine 1-phosphate pubchem chembl_ligand pubchem
small molecule Agonist sphingosine 1-phosphate, sphingosylphosphorylcholine small molecule Yes No Zhao C, Cheng L, Wang W, Wang H, Luo Y, Feng Y, Wang X, Fu H, Cai Y, Yang S, Fu P, Yan W, Shao Z 10.1038/S41422-021-00567-W 2021-09-29 Yes
S1PR3 S1P3 Lysophospholipid (S1P) A (Rhodopsin) Human cryo-EM 7EW4 - 3.2 R Active 100 76 Gi/o αi1 - 64 - scFv16 N,N-Dicyclohexyl-5-cyclopropyl-1,2-oxazole-3-carboxamide pubchem chembl_ligand
small molecule Agonist sphingosine 1-phosphate, sphingosylphosphorylcholine small molecule Yes No Zhao C, Cheng L, Wang W, Wang H, Luo Y, Feng Y, Wang X, Fu H, Cai Y, Yang S, Fu P, Yan W, Shao Z 10.1038/S41422-021-00567-W 2021-09-29 Yes
ACM5 M5 Acetylcholine (muscarinic) A (Rhodopsin) Human X-ray 6OL9 6OL9_refined 2.5 A Inactive 4 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
EDNRB ETB Endothelin A (Rhodopsin) Human X-ray 5XPR 5XPR_refined 3.6 A Inactive 14 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
EDNRB ETB Endothelin A (Rhodopsin) Human X-ray 5X93 5X93_refined 2.2 A Inactive 14 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
AGTR1 AT1 Angiotensin A (Rhodopsin) Human X-ray 4ZUD 4ZUD_refined 2.8 A Inactive 6 75 - - - - BRIL - Olmesartan pubchem
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
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 sphingosine 1-phosphate, LPA, 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
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 sphingosine 1-phosphate, LPA, 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
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 TH, 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 XQ 10.1016/J.CELL.2020.01.007 2020-02-12 Yes
CASR CaS Calcium-sensing C (Glutamate) Human cryo-EM 7M3J 7M3J_refined 4.1 A Inactive 73 72 - - - - - - NPS-2143 pubchem
small molecule NAM L-tryptophan, spermine, Ca2+, Mg2+ amino acid No No Gao Y, Robertson MJ, Rahman SN, Seven AB, Zhang C, Meyerowitz JG, Panova O, Hannan FM, Thakker RV, Brauner-Osborne H, Mathiesen JM, Skiniotis G 10.1038/S41586-021-03691-0 2021-06-30 Yes
CASR CaS Calcium-sensing C (Glutamate) Human cryo-EM 7M3E 7M3E_refined 3.2 B Inactive 73 75 - - - - - - Calcium ion pubchem
NPS-2143 pubchem
Tryptophan pubchem chembl_ligand
ion
small molecule
amino acid
Agonist
NAM
PAM
L-tryptophan, spermine, Ca2+, Mg2+ amino acid No No Gao Y, Robertson MJ, Rahman SN, Seven AB, Zhang C, Meyerowitz JG, Panova O, Hannan FM, Thakker RV, Brauner-Osborne H, Mathiesen JM, Skiniotis G 10.1038/S41586-021-03691-0 2021-06-30 Yes
CASR CaS Calcium-sensing C (Glutamate) Human cryo-EM 7M3G 7M3G_refined 2.5 A Active 73 76 - - - - - - Calcium ion pubchem
Evocalcet pubchem
Tryptophan pubchem chembl_ligand
ion
small molecule
amino acid
Agonist
PAM
PAM
L-tryptophan, spermine, Ca2+, Mg2+ amino acid No No Gao Y, Robertson MJ, Rahman SN, Seven AB, Zhang C, Meyerowitz JG, Panova O, Hannan FM, Thakker RV, Brauner-Osborne H, Mathiesen JM, Skiniotis G 10.1038/S41586-021-03691-0 2021-06-30 Yes
CASR CaS Calcium-sensing C (Glutamate) Human cryo-EM 7M3F 7M3F_refined 2.8 B Active 73 75 - - - - - - Calcium ion pubchem
Cinacalcet pubchem
Tryptophan pubchem chembl_ligand
ion
small molecule
amino acid
Agonist
PAM
PAM
L-tryptophan, spermine, Ca2+, Mg2+ amino acid No No Gao Y, Robertson MJ, Rahman SN, Seven AB, Zhang C, Meyerowitz JG, Panova O, Hannan FM, Thakker RV, Brauner-Osborne H, Mathiesen JM, Skiniotis G 10.1038/S41586-021-03691-0 2021-06-30 Yes
NK1R NK1 Tachykinin A (Rhodopsin) Human X-ray 6HLL 6HLL_refined 3.3 A Inactive 1 67 - - - - GlgA 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 Schoppe J, Ehrenmann J, Klenk C, Rucktooa P, Schutz M, Dore AS, Pluckthun A 10.1038/S41467-018-07939-8 2019-01-16 Yes
NK1R NK1 Tachykinin A (Rhodopsin) Human X-ray 6HLP 6HLP_refined 2.2 A Inactive 1 71 - - - - GlgA glycogen synthase - Netupitant pubchem chembl_ligand
small molecule Antagonist hemokinin 1, neuropeptide K, neuropeptide-γ, neurokinin A, neurokinin B, substance P peptide Yes No Schoppe J, Ehrenmann J, Klenk C, Rucktooa P, Schutz M, Dore AS, Pluckthun A 10.1038/S41467-018-07939-8 2019-01-16 Yes
NK1R NK1 Tachykinin A (Rhodopsin) Human X-ray 6HLO 6HLO_refined 2.4 A Inactive 1 70 - - - - GlgA 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 Schoppe J, Ehrenmann J, Klenk C, Rucktooa P, Schutz M, Dore AS, Pluckthun A 10.1038/S41467-018-07939-8 2019-01-16 Yes
5HT1F 5-HT1F 5-Hydroxytryptamine A (Rhodopsin) Human cryo-EM 7EXD 7EXD_refined 3.4 R Active 100 74 Gi/o αi1 - 62 BRIL scFv16 Lasmiditan pubchem
small molecule Agonist 5-hydroxytryptamine small molecule Yes No Huang S, Xu P, Tan Y, You C, Zhang Y, Jiang Y, Xu HE 10.1038/S41422-021-00527-4 2021-08-04 Yes
FZD4 FZD4 Frizzled F (Frizzled) Human X-ray 6BD4 6BD4_refined 2.4 A Inactive 17 61 - - - - Rubredoxin - - - - norrin protein No No Yang S, Wu Y, Xu TH, 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
CLTR1 CysLT1 Leukotriene A (Rhodopsin) Human X-ray 6RZ4 6RZ4_refined 2.7 A Intermediate 32 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 E, Longpre JM, Lyapina E, Ishchenko A, Patel N, Polovinkin V, Safronova N, Bogorodskiy A, Edelweiss E, Hu H, Weierstall U, Liu W, Batyuk A, Gordeliy V, Han GW, Sarret P, Katritch V, Borshchevskiy V, Cherezov V 10.1126/SCIADV.AAX2518 2019-10-30 Yes
CLTR1 CysLT1 Leukotriene A (Rhodopsin) Human X-ray 6RZ5 6RZ5_refined 2.5 B Intermediate 32 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 E, Longpre JM, Lyapina E, Ishchenko A, Patel N, Polovinkin V, Safronova N, Bogorodskiy A, Edelweiss E, Hu H, Weierstall U, Liu W, Batyuk A, Gordeliy V, Han GW, Sarret P, Katritch V, Borshchevskiy V, Cherezov V 10.1126/SCIADV.AAX2518 2019-10-30 Yes
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, Schutz M, Pluckthun 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, Schutz M, Pluckthun 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, Schutz M, Pluckthun A 10.1073/PNAS.1317903111 2014-01-29 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, Schutz M, Pluckthun A 10.1073/PNAS.1317903111 2014-01-29 No
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 XP, Liu Y, Shen DD, 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 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 XP, Liu Y, Shen DD, 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
PE2R4 EP4 Prostanoid A (Rhodopsin) Human X-ray 5YHL 5YHL_refined 4.2 A Inactive 12 57 - - - - - Fab ONO-AE3-208-Br pubchem
small molecule Antagonist PGE1, PGD2, PGE2, PGF, 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 5YWY 5YWY_refined 3.2 A Inactive 12 57 - - - - - Fab ONO-AE3-208 pubchem
small molecule Antagonist PGE1, PGD2, PGE2, PGF, 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
5HT2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 4IB4 4IB4_refined 2.7 A Intermediate 32 59 - - - - BRIL - Ergotamine pubchem
small molecule Agonist 5-hydroxytryptamine small molecule Yes No Wacker D, Wang C, Katritch V, Han GW, Huang XP, Vardy E, McCorvy JD, Jiang Y, Chu M, Siu FY, Liu W, Xu HE, Cherezov V, Roth BL, Stevens RC 10.1126/SCIENCE.1232808 2013-03-13 Yes
AGTR2 AT2 Angiotensin A (Rhodopsin) Human X-ray 6JOD 6JOD_refined 3.2 A Active 95 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
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 DD, 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 JP, 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 DD, 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 JP, 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
GRM1 mGlu1 Metabotropic glutamate C (Glutamate) Human cryo-EM 7DGE 7DGE_refined 3.7 A Inactive 47 66 - - - - - Nanobody-43 Quisqualic acid pubchem
small molecule Agonist L-glutamic acid amino acid No No Zhang J, Qu L, Wu L, Tang X, Luo F, Xu W, Xu Y, Liu ZJ, Hua T 10.1007/S13238-020-00808-5 2021-09-22 Yes
GRM1 mGlu1 Metabotropic glutamate C (Glutamate) Human cryo-EM 7DGD 7DGD_refined 4.0 A Inactive 47 66 - - - - - - Apo (no ligand)
none Apo (no ligand) L-glutamic acid amino acid No No Zhang J, Qu L, Wu L, Tang X, Luo F, Xu W, Xu Y, Liu ZJ, Hua T 10.1007/S13238-020-00808-5 2021-09-22 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
CCR9 CCR9 Chemokine A (Rhodopsin) Human X-ray 5LWE - 2.8 B Inactive 53 67 - - - - - - Vercirnon pubchem
small molecule Allosteric antagonist CCL25 protein No No Oswald C, Rappas M, Kean J, Dore 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
APJ apelin Apelin A (Rhodopsin) Human X-ray 5VBL 5VBL_refined 2.6 B Inactive 5 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
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
PD2R2 DP2 Prostanoid A (Rhodopsin) Human X-ray 7M8W 7M8W_refined 2.6 A Inactive 24 83 - - - - T4-Lysozyme - 15R-methyl-prostaglandin D2 pubchem
small molecule Antagonist PGD2, PGE2, PGF, PGJ2, PGI2, PGD3 small molecule Yes Yes Liu H, Deepak RNVK, Shiriaeva A, Gati C, Batyuk A, Hu H, Weierstall U, Liu W, Wang L, Cherezov V, Fan H, Zhang C 10.1073/PNAS.2102813118 2021-08-25 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, Dore AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA 10.1021/ACS.JMEDCHEM.9B01787 2020-01-01 Yes
OX1R OX1 Orexin A (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, Dore AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA 10.1021/ACS.JMEDCHEM.9B01787 2020-01-15 Yes
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, Dore AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA 10.1021/ACS.JMEDCHEM.9B01787 2020-01-01 Yes
OX1R OX1 Orexin A (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, Dore AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA 10.1021/ACS.JMEDCHEM.9B01787 2020-01-01 Yes
OX1R OX1 Orexin A (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, Dore AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA 10.1021/ACS.JMEDCHEM.9B01787 2020-01-01 Yes
OX1R OX1 Orexin A (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, Dore AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA 10.1021/ACS.JMEDCHEM.9B01787 2020-01-01 Yes
OX1R OX1 Orexin A (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, Dore AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA 10.1021/ACS.JMEDCHEM.9B01787 2020-01-15 Yes
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, Dore AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA 10.1021/ACS.JMEDCHEM.9B01787 2020-01-01 Yes
OX2R OX2 Orexin A (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, Dore AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA 10.1021/ACS.JMEDCHEM.9B01787 2020-01-01 Yes
OX2R OX2 Orexin A (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, Dore AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA 10.1021/ACS.JMEDCHEM.9B01787 2020-01-01 Yes
OX1R OX1 Orexin A (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, Dore AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA 10.1021/ACS.JMEDCHEM.9B01787 2020-01-01 Yes
OX1R OX1 Orexin A (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, Dore AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA 10.1021/ACS.JMEDCHEM.9B01787 2020-01-01 Yes
OX1R OX1 Orexin A (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, Dore AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA 10.1021/ACS.JMEDCHEM.9B01787 2020-01-01 Yes
OX1R OX1 Orexin A (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, Dore AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA 10.1021/ACS.JMEDCHEM.9B01787 2020-01-01 Yes
AA2AR A2A Adenosine A (Rhodopsin) Human X-ray 5G53 5G53_refined 3.4 A Active 100 68 Gs αs Engineered G protein 50 - - NECA pubchem
small molecule Agonist adenosine small molecule Yes No Carpenter B, Nehme R, Warne T, Leslie AG, Tate CG 10.1038/NATURE18966 2016-08-03 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
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 YL, 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 YL, 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
AA1R A1 Adenosine A (Rhodopsin) Human X-ray 5UEN 5UEN_refined 3.2 B Inactive 0 91 - - - - BRIL - DU172 pubchem
small molecule Antagonist adenosine small molecule Yes No Glukhova A, Thal DM, Nguyen AT, Vecchio EA, Jorg M, Scammells PJ, May LT, Sexton PM, Christopoulos A 10.1016/J.CELL.2017.01.042 2017-03-01 Yes
PTH2R PTH2 Parathyroid hormone B1 (Secretin) Human cryo-EM 7F16 7F16_refined 2.8 R Active 100 68 Gs αs - 58 - Nanobody-35 TIP39
peptide Agonist TIP39, PTH, PTHrP-(1-36), PTHrP-(1-34) (human) peptide No No Wang X, Cheng X, Zhao L, Wang Y, Ye C, Zou X, Dai A, Cong Z, Chen J, Zhou Q, Xia T, Jiang H, Xu HE, Yang D, Wang MW 10.1073/PNAS.2101279118 2021-08-18 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
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, PGF, 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
OPRX NOP Opioid A (Rhodopsin) Human X-ray 5DHG 5DHG_refined 3.0 A Inactive 5 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, Calo 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 5 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, Calo G, Katritch V, Stevens RC 10.1016/J.STR.2015.07.024 2015-10-21 Yes
GLP1R GLP-1 Glucagon B1 (Secretin) Human X-ray 5NX2 5NX2_refined 3.7 A Intermediate 74 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, Dore AS, Weir M, Cooke RM, Marshall FH 10.1038/NATURE22800 2017-06-14 Yes
5HT2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 5TUD 5TUD_refined 3.0 D Active 81 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
CCR5 CCR5 Chemokine A (Rhodopsin) Human X-ray 5UIW 5UIW_refined 2.2 A Inactive 24 85 - - - - Rubredoxin - 5P7-CCL5
protein Antagonist CCL5, CCL3, CCL16, CCL14, 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
AA1R A1 Adenosine A (Rhodopsin) Human cryo-EM 7LD4 7LD4_refined 3.3 R Active 100 88 Gi/o αi2 - 59 - - adenosine pubchem
small molecule Agonist adenosine small molecule Yes No Draper-Joyce CJ, Bhola R, Wang J, Bhattarai A, Nguyen ATN, Cowie-Kent I, O'Sullivan K, Chia LY, Venugopal H, Valant C, Thal DM, Wootten D, Panel N, Carlsson J, Christie MJ, White PJ, Scammells P, May LT, Sexton PM, Danev R, Miao Y, Glukhova A, Imlach WL, Christopoulos A 10.1038/S41586-021-03897-2 2021-09-08 Yes
AA1R A1 Adenosine A (Rhodopsin) Human cryo-EM 7LD3 7LD3_refined 3.2 R Active 100 88 Gi/o αi2 - 59 - - adenosine pubchem
{2-Amino-4-[3,5-bis(trifluoromethyl)phenyl]thiophen-3-yl}(4-chlorophenyl)methanone pubchem
small molecule
none
Agonist
PAM
adenosine small molecule Yes No Draper-Joyce CJ, Bhola R, Wang J, Bhattarai A, Nguyen ATN, Cowie-Kent I, O'Sullivan K, Chia LY, Venugopal H, Valant C, Thal DM, Wootten D, Panel N, Carlsson J, Christie MJ, White PJ, Scammells P, May LT, Sexton PM, Danev R, Miao Y, Glukhova A, Imlach WL, Christopoulos A 10.1038/S41586-021-03897-2 2021-09-08 Yes
OPRK κ Opioid A (Rhodopsin) Human X-ray 6VI4 6VI4_refined 3.3 B Inactive 5 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 Inactive 25 71 - - - - - - CGP54626 pubchem
small molecule Antagonist GABA small molecule No No Mao C, Shen C, Li C, Shen DD, Xu C, Zhang S, Zhou R, Shen Q, Chen LN, 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 DD, Xu C, Zhang S, Zhou R, Shen Q, Chen LN, Jiang Z, Liu J, Zhang Y 10.1038/S41422-020-0350-5 2020-07-01 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 YL, 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
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 YL, 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
P2Y12 P2Y12 P2Y A (Rhodopsin) Human X-ray 4NTJ 4NTJ_refined 2.6 A Intermediate 32 78 - - - - BRIL - AZD1283 pubchem
small molecule Antagonist ADP small molecule Yes No Zhang K, Zhang J, Gao ZG, Zhang D, Zhu L, Han GW, Moss SM, Paoletta S, Kiselev E, Lu W, Fenalti G, Zhang W, Muller CE, Yang H, Jiang H, Cherezov V, Katritch V, Jacobson KA, Stevens RC, Wu B, Zhao Q 10.1038/NATURE13083 2014-03-26 Yes
TA2R TP Prostanoid A (Rhodopsin) Human X-ray 6IIU 6IIU_refined 2.5 A Intermediate 32 87 - - - - BRIL - Ramatroban pubchem chembl_ligand
small molecule Antagonist PGD2, PGE2, PGF, 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 6IIV 6IIV_refined 3.0 A Intermediate 32 87 - - - - BRIL - Daltroban pubchem chembl_ligand
small molecule Antagonist PGD2, PGE2, PGF, 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
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 DD, Zhou XE, Bi P, Liu QF, Tan YX, Zhuang YW, Zhang HB, Xu PY, Huang SJ, Ma SS, He XH, 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 - 10.1101/2020.08.16.252585 2020-09-09 Yes
GLP1R GLP-1 Glucagon B1 (Secretin) Human cryo-EM 6X19 6X19_refined 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 - 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 - 10.1101/2020.08.16.252585 2020-09-09 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 amino acid 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 LN, Zhou Q, Zhao LH, Yang D, Zhang H, Cong Z, Shen DD, 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 MW 10.1038/S41422-020-00442-0 2020-12-16 Yes
5HT2C 5-HT2C 5-Hydroxytryptamine A (Rhodopsin) Human X-ray 6BQG 6BQG_refined 3.0 A Active 81 62 - - - - BRIL - Ergotamine pubchem
small molecule Agonist 5-hydroxytryptamine small molecule Yes No Peng Y, McCorvy JD, Harpsoe K, Lansu K, Yuan S, Popov P, Qu L, Pu M, Che T, Nikolajsen LF, Huang XP, Wu Y, Shen L, Bjorn-Yoshimoto WE, Ding K, Wacker D, Han GW, Cheng J, Katritch V, Jensen AA, Hanson MA, Zhao S, Gloriam DE, Roth BL, Stevens RC, Liu ZJ 10.1016/J.CELL.2018.01.001 2018-02-14 Yes
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, Harpsoe K, Lansu K, Yuan S, Popov P, Qu L, Pu M, Che T, Nikolajsen LF, Huang XP, Wu Y, Shen L, Bjorn-Yoshimoto WE, Ding K, Wacker D, Han GW, Cheng J, Katritch V, Jensen AA, Hanson MA, Zhao S, Gloriam DE, Roth BL, Stevens RC, Liu ZJ 10.1016/J.CELL.2018.01.001 2018-02-14 Yes
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
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) TIP39, PTHrP, PTH, PTHrP-(1-36) peptide No No Ehrenmann J, Schoppe J, Klenk C, Rappas M, Kummer L, Dore AS, Pluckthun 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 4 59 - - - - GlgA glycogen synthase - - - - acetylcholine small molecule Yes No Wang J, Wu M, Wu L, Xu Y, Li F, Wu Y, Popov P, Wang L, Bai F, Zhao S, Liu ZJ, Hua T 10.1107/S2052252520000597 2020-03-11 Yes
GRM5 mGlu5 Metabotropic glutamate C (Glutamate) Human X-ray 7P2L 7P2L_refined 2.5 A Inactive 0 21 - - - - T4-Lysozyme - Alloswitch-1
small molecule NAM L-glutamic acid amino acid No No Nasrallah C, Cannone G, Briot J, Rottier K, Berizzi AE, Huang CY, Quast RB, Hoh F, Baneres JL, Malhaire F, Berto L, Dumazer A, Font-Ingles J, Gomez-Santacana X, Catena J, Kniazeff J, Goudet C, Llebaria A, Pin JP, Vinothkumar KR, Lebon G 10.1016/J.CELREP.2021.109648 2021-09-08 Yes
GRM5 mGlu5 Metabotropic glutamate C (Glutamate) Human cryo-EM 7FD9 7FD9_refined 4.0 A Inactive 33 63 - - - - - - 2-[(1s,2s)-2-Carboxycyclopropyl]-3-(9h-Xanthen-9-Yl)-D-Alanine pubchem chembl_ligand
small molecule Antagonist L-glutamic acid amino acid No No Nasrallah C, Cannone G, Briot J, Rottier K, Berizzi AE, Huang CY, Quast RB, Hoh F, Baneres JL, Malhaire F, Berto L, Dumazer A, Font-Ingles J, Gomez-Santacana X, Catena J, Kniazeff J, Goudet C, Llebaria A, Pin JP, Vinothkumar KR, Lebon G 10.1016/J.CELREP.2021.109648 2021-09-08 Yes
GRM5 mGlu5 Metabotropic glutamate C (Glutamate) Human cryo-EM 7FD8 7FD8_refined 3.8 A Inactive 8 63 - - - - - - Quisqualic acid pubchem
small molecule Agonist L-glutamic acid amino acid No No Nasrallah C, Cannone G, Briot J, Rottier K, Berizzi AE, Huang CY, Quast RB, Hoh F, Baneres JL, Malhaire F, Berto L, Dumazer A, Font-Ingles J, Gomez-Santacana X, Catena J, Kniazeff J, Goudet C, Llebaria A, Pin JP, Vinothkumar KR, Lebon G 10.1016/J.CELREP.2021.109648 2021-09-08 Yes
GRM7 mGlu7 Metabotropic glutamate C (Glutamate) Human cryo-EM 7EPC 7EPC_refined 4.0 B Inactive 47 85 - - - - - - Apo (no ligand)
none Apo (no ligand) L-glutamic acid, L-serine-O-phosphate amino acid No No Du J, Wang D, Fan H, Xu C, Tai L, Lin S, Han S, Tan Q, Wang X, Xu T, Zhang H, Chu X, Yi C, Liu P, Wang X, Zhou Y, Pin JP, Rondard P, Liu H, Liu J, Sun F, Wu B, Zhao Q 10.1038/S41586-021-03641-W 2021-06-23 Yes
GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human X-ray 7EPE 7EPE_refined 2.5 A Inactive 3 28 - - - - Flavodoxin - 4-(1-Methylpyrazol-4-yl)-7-[[(2~{S})-2-(trifluoromethyl)morpholin-4-yl]methyl]quinoline-2-carboxamide pubchem
small molecule NAM L-glutamic acid amino acid No No Du J, Wang D, Fan H, Xu C, Tai L, Lin S, Han S, Tan Q, Wang X, Xu T, Zhang H, Chu X, Yi C, Liu P, Wang X, Zhou Y, Pin JP, Rondard P, Liu H, Liu J, Sun F, Wu B, Zhao Q 10.1038/S41586-021-03641-W 2021-06-23 Yes
GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human cryo-EM 7EPD 7EPD_refined 3.9 A Inactive 43 89 - - - - - - Apo (no ligand)
none Apo (no ligand) L-glutamic acid amino acid No No Du J, Wang D, Fan H, Xu C, Tai L, Lin S, Han S, Tan Q, Wang X, Xu T, Zhang H, Chu X, Yi C, Liu P, Wang X, Zhou Y, Pin JP, Rondard P, Liu H, Liu J, Sun F, Wu B, Zhao Q 10.1038/S41586-021-03641-W 2021-06-23 Yes
GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human cryo-EM 7EPA 7EPA_refined 3.6 A Inactive 43 90 - - - - - - Apo (no ligand)
none Apo (no ligand) L-glutamic acid amino acid No No Du J, Wang D, Fan H, Xu C, Tai L, Lin S, Han S, Tan Q, Wang X, Xu T, Zhang H, Chu X, Yi C, Liu P, Wang X, Zhou Y, Pin JP, Rondard P, Liu H, Liu J, Sun F, Wu B, Zhao Q 10.1038/S41586-021-03641-W 2021-06-23 Yes
GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human X-ray 7EPF 7EPF_refined 2.7 A Inactive 3 28 - - - - Flavodoxin - (8~{R})-4-[2,4-Bis(fluoranyl)phenyl]-8-methyl-7-[(2-methylpyrazol-3-yl)methyl]-6,8-dihydro-5~{H}-1,7-naphthyridine-2-carboxamide pubchem
small molecule NAM L-glutamic acid amino acid No No Du J, Wang D, Fan H, Xu C, Tai L, Lin S, Han S, Tan Q, Wang X, Xu T, Zhang H, Chu X, Yi C, Liu P, Wang X, Zhou Y, Pin JP, Rondard P, Liu H, Liu J, Sun F, Wu B, Zhao Q 10.1038/S41586-021-03641-W 2021-06-23 Yes
GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human cryo-EM 7EPB 7EPB_refined 3.1 B Inactive 43 89 - - - - - Anti-RON nanobody Eglumetad pubchem
small molecule Agonist L-glutamic acid amino acid No No Du J, Wang D, Fan H, Xu C, Tai L, Lin S, Han S, Tan Q, Wang X, Xu T, Zhang H, Chu X, Yi C, Liu P, Wang X, Zhou Y, Pin JP, Rondard P, Liu H, Liu J, Sun F, Wu B, Zhao Q 10.1038/S41586-021-03641-W 2021-06-23 Yes
Q80KM9 US28 Unclassified A (Rhodopsin) strain AD169 X-ray 5WB1 5WB1_refined 3.5 A Active 96 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 96 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
ACM1 M1 Acetylcholine (muscarinic) A (Rhodopsin) Human X-ray 6WJC 6WJC_refined 2.6 A Inactive 4 62 - - - - T4-Lysozyme - Hyoscyamine