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RECEPTOR EXPRESSION SOLUBILIZATION PURIFICATION STRUCTURE DETERMINATION
PDB pH Temp Resolution Reference Date
7VUI GP139 GPR139 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A JNJ-63533054 pubchem gtoplig chembl_ligand
Agonist 3.3 Active 10.1038/S41422-021-00591-W 2021-12-29
5IU4 AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusTni PRO (Trichoplusia ni) cell linesInsect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 5.5-5.5 20 ZM-241385 pubchem gtoplig chembl_ligand drugbank
Antagonist 1.7 Inactive 10.1021/acs.jmedchem.6b00653 2016-06-29
7C2E GLP1R GLP-1 Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 2-[[4-[6-[(4-cyano-2... pubchem
Agonist 4.2 Active 10.1038/S41422-020-0384-8 2020-08-26
4IB4 5HT2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 7 chems 8.0-8.5 20°C ergotamine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.7 Intermediate 10.1126/science.1232808 2013-03-13
7TYL CALCR CT Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A amylin peptide
Agonist 3.3 Active 10.1126/SCIENCE.ABM9609 2022-03-23
3OE9 CXCR4 CXCR4 Chemokine A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 6.0-6.0 20°C isothiourea-1t pubchem gtoplig chembl_ligand
Antagonist 3.1 Inactive 10.1126/SCIENCE.1194396 2010-10-27
4EJ4 OPRD δ Opioid A (Rhodopsin) Mouse BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 7.5-7.5 20°C naltrindole pubchem gtoplig chembl_ligand gtoplig
Antagonist 3.4 Inactive 10.1038/NATURE11111 2012-05-16
5K2D AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 5.0-5.0 20°C ZM-241385 pubchem gtoplig chembl_ligand drugbank
Antagonist 1.9 Inactive 10.1126/SCIADV.1600292 2016-09-21
6PB1 CRFR2 CRF2 Corticotropin-releasing factor B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL427807 chembl_ligand pubchem
Agonist 2.8 Active 10.1016/J.MOLCEL.2020.01.013 2020-02-12
6AKY CCR5 CCR5 Chemokine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CCR5 antagonist 34 pubchem gtoplig chembl_ligand
Antagonist 2.8 Inactive 10.1021/ACS.JMEDCHEM.8B01077 2018-10-24
7FIM GLP1R GLP-1 Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Tirzepatide pubchem
Agonist 3.4 Active 10.1038/S41467-022-28683-0 2022-03-02
6YVR NTR1 NTS1 Neurotensin A (Rhodopsin) Rat N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A JMV431 gtoplig chembl_ligand pubchem
Agonist 2.5 Inactive 10.1126/sciadv.abe5504 2021-02-10
7BB7 V2R V2 Vasopressin and oxytocin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A vasopressin pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 4.4 Active 10.1126/SCIADV.ABG5628 2021-06-02
6OSA NTR1 NTS1 Neurotensin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A JMV449 pubchem gtoplig chembl_ligand
Agonist 3.0 Active 10.1038/S41586-019-1337-6 2019-07-10
3EML AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 6.5-6.5 20°C ZM-241385 pubchem gtoplig chembl_ligand drugbank
Antagonist 2.6 Inactive 10.1126/SCIENCE.1164772 2008-10-14
5VEW GLP1R GLP-1 Glucagon B1 (Secretin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 6.2-6.6 20°C PF-06372222 pubchem
NAM 2.7 Inactive 10.1038/NATURE22378 2017-05-24
7WC8 5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A LUMATEPERONE chembl_ligand chembl_ligand pubchem
Agonist 2.5 Inactive 10.1126/SCIENCE.ABL8615 2022-01-26
4IAQ 5HT1B 5-HT1B 5-Hydroxytryptamine A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 8.7-8.7 20°C dihydroergotamine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.8 Inactive 10.1126/SCIENCE.1232807 2013-03-13
4OO9 GRM5 mGlu5 Metabotropic glutamate C (Glutamate) Human BaculovirusSf21Insect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 4 chems 6.8-6.8 20°C MAVOGLURANT chembl_ligand pubchem
NAM 2.6 Inactive 10.1038/NATURE13396 2014-07-02
7M8W PD2R2 DP2 Prostanoid A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 15(<i>R</i>)-15-meth... pubchem gtoplig
Antagonist 2.6 Inactive 10.1073/PNAS.2102813118 2021-08-25
6J21 NK1R NK1 Tachykinin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A aprepitant pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Antagonist 3.2 Inactive 10.1038/S41467-019-08568-5 2019-03-06
1F88 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 2 chemicals 2 steps vapour diffusionHanging drop 7 chems 6.0-6.0 4°C Retinal (11-cis) pubchem
Inverse agonist 2.8 Inactive 10.1126/SCIENCE.289.5480.739 2000-08-04
4BUO NTR1 NTS1 Neurotensin A (Rhodopsin) Rat NAE. coli BL21(DE3)Bacteria 6 chemicals 6 steps vapour diffusionSitting drop 5 chems 9.4-9.4 4°C neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
Agonist 2.8 Inactive 10.1073/PNAS.1317903111 2014-01-29
6RZ5 CLTR1 CysLT1 Leukotriene A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A zafirlukast pubchem gtoplig chembl_ligand drugbank drug_central
Antagonist 2.5 Intermediate 10.1126/SCIADV.AAX2518 2019-10-30
6IQL DRD4 D4 Dopamine A (Rhodopsin) Mouse N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A L745870 pubchem gtoplig chembl_ligand
Antagonist 3.5 Inactive 10.7554/ELIFE.48822 2019-12-04
4U15 ACM3 M3 Acetylcholine (muscarinic) A (Rhodopsin) Rat BaculovirusSf9Insect 9 chemicals 9 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 7.5-7.5 298 K tiotropium pubchem gtoplig chembl_ligand drugbank gtoplig
Antagonist 2.8 Inactive 10.1016/J.STR.2014.08.022 2014-11-26
7KNT CALRL calcitonin-like Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.2 Inactive 10.1126/SCIENCE.ABF7258 2021-02-24
7RMI NK1R NK1 Tachykinin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A substance P pubchem gtoplig chembl_ligand gtoplig gtoplig
Agonist 3.2 Active 10.1038/S41589-021-00890-8 2021-11-03
5VEX GLP1R GLP-1 Glucagon B1 (Secretin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 5.0-5.8 20°C NNC0640 pubchem gtoplig
NAM 3.0 Inactive 10.1038/NATURE22378 2017-05-17
6TOD OX1R OX1 Orexin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A EMPA pubchem gtoplig chembl_ligand
Antagonist 2.1 Inactive 10.1021/ACS.JMEDCHEM.9B01787 2020-01-01
7WIH GRM3 mGlu3 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL4081453 chembl_ligand pubchem
Agonist 3.7 Inactive 10.1038/S41422-022-00623-Z 2022-03-16
6FK9 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine BaculovirusHEK293S(TetR)-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 4.5-4.5 20°C (2~{S})-3-methyl-2-p... pubchem
Agonist 2.6 Active 10.1073/PNAS.1718084115 2018-04-04
4LDO ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)7.7 MAG 5 chems 6.5-6.5 20°C (-)-adrenaline pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Agonist 3.2 Active 10.1038/NATURE12572 2013-09-25
5ZKB ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A AF-DX 384 pubchem
Antagonist 3.0 Inactive 10.1038/S41589-018-0152-Y 2018-11-21
7JHJ Q3KSP2 BILF1 Unclassified A (Rhodopsin) strain GD1 N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.2 Active 10.1016/J.IMMUNI.2021.06.001 2021-07-07
5TGZ CNR1 CB1 Cannabinoid A (Rhodopsin) Human Transient_transfectionHEK293FMammalian 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 7.0-7.4 20°C AM6538 pubchem gtoplig
Antagonist 2.8 Inactive 10.1016/J.CELL.2016.10.004 2016-11-02
2RH1 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 6.8-6.8 21-23°C Carazolol pubchem
Inverse agonist 2.4 Inactive 10.1126/SCIENCE.1150577 2007-10-30
7EW3 S1PR3 S1P3 Lysophospholipid (S1P) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Sphingosine 1-phosph... pubchem
Agonist 3.1 Active 10.1038/S41422-021-00567-W 2021-09-29
7DD6 CASR CaS Calcium-sensing C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Calcium pubchem
L-tryptophan pubchem gtoplig chembl_ligand drugbank drug_central pubchem
AgonistPAM 3.2 Active 10.1126/SCIADV.ABG1483 2021-06-16
5EN0 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine Stable_cellsHEK293S(TetR)GnTI-Mammalian 1 chemicals 1 steps vapour diffusionSitting drop 4 chems 5.0-5.0 4°C Retinal (all-trans) pubchem
Agonist 2.8 Active 10.15252/EMBR.201642671 2016-08-10
7KI0 GLP1R GLP-1 Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A semaglutide pubchem gtoplig chembl_ligand drugbank pubchem
Agonist 2.5 Active 10.1016/J.CELREP.2021.109374 2021-08-04
6N51 GRM5 mGlu5 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A quisqualate pubchem gtoplig chembl_ligand drugbank gtoplig pubchem
Agonist 4.0 Intermediate 10.1038/S41586-019-0881-4 2019-01-23
7WI8 GRM3 mGlu3 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A LY341495 pubchem gtoplig chembl_ligand gtoplig
Antagonist 4.2 Inactive 10.1038/S41422-022-00623-Z 2022-03-16
5NDD PAR2 PAR2 Proteinase-activated A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 5.5-6.2 20°C AZ8838 pubchem gtoplig chembl_ligand
Antagonist 2.8 Intermediate 10.1038/NATURE22309 2017-05-03
6QNO OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Retinal (all-trans) pubchem
Agonist 4.4 Active 10.7554/ELIFE.46041 2019-07-10
2G87 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 6.5-7.5 283 K Retinal (all-trans) pubchem
Agonist 2.6 Inactive 10.1002/ANIE.200600595 2006-09-02
6Z66 NTR1 NTS1 Neurotensin A (Rhodopsin) Rat N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.2 Intermediate 10.1126/sciadv.abe5504 2021-02-10
7FIG LSHR LH Glycoprotein hormone A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Choriogonadotropin b... gtoplig
Glycoprotein alpha gtoplig
AgonistAgonist 3.9 Active 10.1038/S41586-021-03924-2 2021-09-29
7VUZ MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A PAMP-12 pubchem
Agonist 2.9 Active 2021-12-01
6UUN CALRL calcitonin-like Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Adrenomedullin pubchem
Agonist 3.0 Active 10.1021/ACSPTSCI.9B00080 2020-03-25
7TYF CALCR CT Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A amylin peptide
Agonist 2.2 Active 10.1126/SCIENCE.ABM9609 2022-03-23
5XRA CNR1 CB1 Cannabinoid A (Rhodopsin) Human Transient_transfectionHEK293TMammalian 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 6.4-6.4 20°C AM11542 pubchem gtoplig chembl_ligand
Agonist 2.8 Active 10.1038/NATURE23272 2017-07-12
7JV5 DRD1 D1 Dopamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A SKF81297 pubchem chembl_ligand
Agonist 3.0 Active 10.1016/J.CELL.2021.01.027 2021-02-24
7WC4 5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 5-hydroxytryptamine pubchem gtoplig chembl_ligand drugbank
Agonist 3.2 Inactive 10.1126/SCIENCE.ABL8615 2022-01-26
4Z36 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 5.5-5.5 20°C ONO-3080573 pubchem gtoplig
Antagonist 2.9 Inactive 10.1016/J.CELL.2015.06.002 2015-06-03
3PBL DRD3 D3 Dopamine A (Rhodopsin) Human BaculovirusSf9Insect 6 chemicals 6 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 7.5-7.5 20°C eticlopride pubchem gtoplig chembl_ligand drugbank
Antagonist 2.9 Inactive 10.1126/SCIENCE.1197410 2010-11-03
3D4S ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 7.0-7.0 20°C timolol pubchem gtoplig chembl_ligand drugbank drug_central
Inverse agonist 2.8 Inactive 10.1016/J.STR.2008.05.001 2008-06-17
6XBK SMO SMO Frizzled F (Frizzled) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Cholesterol pubchem
Agonist 3.2 Active 10.1038/S41589-020-0646-2 2020-09-30
5UEN AA1R A1 Adenosine A (Rhodopsin) Human BaculovirusSf9Insect 6 chemicals 6 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 7.0-8.0 20°C DU172 pubchem gtoplig chembl_ligand
Antagonist 3.2 Inactive 10.1016/j.cell.2017.01.042 2017-03-01
5XJM AGTR2 AT2 Angiotensin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A SI pubchem chembl_ligand
Agonist 3.2 Active 10.1038/S41594-018-0079-8 2018-07-11
7L1U OX2R OX2 Orexin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Orexin-A pubchem
Agonist 3.2 Active 10.1038/S41467-021-21087-6 2021-02-10
4RWA OPRD δ Opioid A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 6.0-6.0 20°C DIPP-NH2
Antagonist 3.3 Inactive 10.1038/NSMB.2965 2015-01-14
6KUW ADA2C α2C Adrenoceptors A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (8Ar,12aS,13aR)-12-e... pubchem
Antagonist 2.8 Inactive 2019-12-04
7VV5 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A compound 48/80 pubchem gtoplig
Agonist 2.8 Active 2021-12-01
7EPA GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.6 Inactive 10.1038/S41586-021-03641-W 2021-06-23
7TYY CALCR CT Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Calcitonin salmon pubchem
Agonist 3.0 Active 10.1126/SCIENCE.ABM9609 2022-03-23
7WF7 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A sphingosine 1-phosph... pubchem gtoplig chembl_ligand pubchem
Agonist 3.4 Active 10.1038/S41589-021-00930-3 2022-01-05
7DFP DRD2 D2 Dopamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A spiperone pubchem gtoplig chembl_ligand drug_central gtoplig
Antagonist 3.1 Inactive 10.1038/S41467-020-20221-0 2020-12-30
7E6U CASR CaS Calcium-sensing C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 6.0 Inactive 10.7554/ELIFE.68578 2021-09-22
6LI1 GPR52 GPR52 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 2.9 Intermediate 10.1038/S41586-020-2019-0 2020-02-26
7V9M GHRHR GHRH Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Somatoliberin pubchem
Agonist 3.3 Active 2021-10-20
3SN6 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps sponge mesophaselipidic cubic phase (LCP)7.7 MAG 6 chems 6.5-6.5 20°C BI-167107 pubchem
Agonist 3.2 Active 10.1038/NATURE10361 2011-07-20
7CMU DRD3 D3 Dopamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A pramipexole pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.0 Active 10.1016/J.MOLCEL.2021.01.003 2021-03-10
6OS9 NTR1 NTS1 Neurotensin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A JMV449 pubchem gtoplig chembl_ligand
Agonist 3.0 Active 10.1038/S41586-019-1337-6 2019-07-10
3REY AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusSf9Insect 1 chemicals 1 steps vapour diffusionSitting drop 6 chems 8.0-8.8 4°C xanthine amine conge... pubchem gtoplig chembl_ligand gtoplig
Antagonist 3.3 Inactive 10.1016/J.STR.2011.06.014 2011-09-07
7EO2 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (S)-FTY720-phosphate pubchem gtoplig chembl_ligand
Agonist 2.9 Active 10.1038/S41589-021-00930-3 2022-01-05
6FKA OPSD Rhodopsin Opsins A (Rhodopsin) Bovine BaculovirusHEK293S(TetR)-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 4.5-4.5 20°C (2~{S})-2-(3,4-dichl... pubchem
Agonist 2.7 Active 10.1073/PNAS.1718084115 2018-04-04
7RMG NK1R NK1 Tachykinin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A substance P pubchem gtoplig chembl_ligand gtoplig gtoplig
Agonist 3.0 Active 10.1038/S41589-021-00890-8 2021-11-03
2Y03 ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 1 chemicals 1 steps vapour diffusionsitting drops 6 chems 8.5-8.5 4°C (R)-Isoproterenol pubchem chembl_ligand
Agonist 2.9 Inactive 10.1038/NATURE09746 2011-01-12
5JQH ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)7.7 MAG 5 chems 7.5-7.5 23°C Carazolol pubchem
Inverse agonist 3.2 Inactive 10.1038/NATURE18636 2016-07-13
7BB6 V2R V2 Vasopressin and oxytocin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A vasopressin pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 4.2 Active 10.1126/SCIADV.ABG5628 2021-06-02
2I36 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 2 chemicals 2 steps vapour diffusionsitting drops 5 chems 7.0-8.0 5°C Apo (no ligand)
Apo (no ligand) 4.1 Inactive 10.1073/PNAS.0608022103 2006-10-17
7S8L MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Cortistatin 14 pubchem
Agonist 2.5 Active 10.1038/S41586-021-04126-6 2021-11-17
3UZC AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusSf9Insect 1 chemicals 1 steps vapour diffusionsitting drop 6 chems 8.0-8.0 4°C CHEMBL2024114 chembl_ligand pubchem
Antagonist 3.3 Inactive 10.1021/JM201376W 2012-03-21
6TOT OX1R OX1 Orexin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A lemborexant pubchem gtoplig chembl_ligand drug_central drugbank
Antagonist 2.2 Inactive 10.1021/ACS.JMEDCHEM.9B01787 2020-01-15
6PWC NTR1 NTS1 Neurotensin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Neurotensin pubchem
Agonist 4.9 Active 10.1038/S41422-019-0256-2 2019-12-04
7FII LSHR LH Glycoprotein hormone A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Choriogonadotropin b... gtoplig
Glycoprotein alpha gtoplig
AgonistAgonist 4.3 Active 10.1038/S41586-021-03924-2 2021-09-29
7PIV MC4R MC4 Melanocortin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A afamelanotide pubchem gtoplig chembl_ligand drugbank pubchem pubchem pubchem pubchem
Agonist 2.9 Active 10.1038/S41422-021-00569-8 2021-11-17
6UUS CALRL calcitonin-like Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Adrenomedullin pubchem
Agonist 2.4 Active 10.1021/ACSPTSCI.9B00080 2020-04-01
7D76 AGRG3 ADGRG3 ADGRG B2 (Adhesion) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Beclomethasone pubchem
Agonist 3.1 Active 10.1038/S41586-020-03083-W 2021-02-03
6TKO ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A arformoterol pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.3 Active 10.1038/S41586-020-2419-1 2020-06-17
5WB1 Q80KM9 US28 Unclassified A (Rhodopsin) strain AD169 BaculovirusHEK293S(TetR)-GnTI-Mammalian 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 6.0-6.0 16-20°C N/A N/A 3.5 Active 10.7554/ELIFE.35850 2018-06-13
6TQ4 OX1R OX1 Orexin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL4590386 chembl_ligand pubchem
Antagonist 2.3 Inactive 10.1021/ACS.JMEDCHEM.9B01787 2020-01-01
2PED OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drop 5 chems 6.4-6.4 283 K Retinal (9-cis) pubchem
Inverse agonist 3.0 Inactive 10.1529/BIOPHYSJ.107.108225 2007-10-30
5IU7 AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusTni PRO (Trichoplusia ni) cell linesInsect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 5.3-5.4 20°C 2-(Furan-2-yl)-5-N-[... pubchem
Antagonist 1.9 Inactive 10.1021/acs.jmedchem.6b00653 2016-06-29
7RYC OXYR OT Vasopressin and oxytocin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A oxytocin pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
Agonist 2.9 Active 10.1038/S41594-022-00728-4 2022-03-09
7TD0 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (2r)-2-Hydroxy-3-(Ph... pubchem
Agonist 2.8 Active 10.1038/S41467-022-28417-2 2022-02-09
7CRH DRD1 D1 Dopamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL1416789 chembl_ligand pubchem
Agonist 3.3 Active 10.1016/J.CELL.2021.01.028 2021-03-03
6OS0 AGTR1 AT1 Angiotensin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Angiotensinogen pubchem
Agonist 2.9 Active 10.1126/SCIENCE.AAY9813 2020-02-19
7VL8 CCR1 CCR1 Chemokine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 2.9 Active 10.1038/S41589-021-00918-Z 2022-03-23
7FIN GIPR GIP Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Peptide-20
Agonist 3.1 Active 10.1038/S41467-022-28683-0 2022-02-23
4K5Y CRFR1 CRF1 Corticotropin-releasing factor B1 (Secretin) Human BaculovirusHi5Insect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 4 chems 5.5-5.5 22.5°C CP 376,395 pubchem gtoplig chembl_ligand
Antagonist 3.0 Inactive 10.1038/NATURE12357 2013-07-17
7T10 SSR2 SST2 Somatostatin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A SOMATOSTATIN chembl_ligand pubchem
Agonist 2.5 Active 10.1038/S41594-022-00727-5 2022-03-09
6DDF OPRM μ Opioid A (Rhodopsin) Mouse BaculovirusSf9Insect 4 chemicals 4 steps Cryo-EMGatan K2 Summit direct electron camera , 300kV 5 chems 7.5-7.5 4°C DAMGO pubchem gtoplig chembl_ligand chembl_ligand
Agonist 3.5 Active 10.1038/S41586-018-0219-7 2018-06-13
6WGT 5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Lysergide pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.4 Inactive 10.1016/J.CELL.2020.08.024 2020-09-23
7BR3 GNRHR GnRH1 Gonadotrophin-releasing hormone A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A elagolix pubchem gtoplig chembl_ligand drug_central drugbank
Antagonist 2.8 Inactive 2020-10-07
6H7N ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (S)-Xamoterol pubchem
Agonist 2.5 Active 10.1101/436212 2018-10-17
2Y01 ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 1 chemicals 1 steps vapour diffusionsitting drops 6 chems 9.0-9.0 4°C Dobutamine pubchem
Agonist (partial) 2.6 Inactive 10.1038/NATURE09746 2011-03-30
7KH0 V2R V2 Vasopressin and oxytocin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A vasopressin pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.8 Active 10.1038/S41422-021-00483-Z 2021-05-26
7TYX CALCR CT Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A amylin peptide
Agonist 2.6 Active 10.1126/SCIENCE.ABM9609 2022-03-30
4L6R GLR glucagon Glucagon B1 (Secretin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 7.0-7.0 20°C N/A N/A 3.3 Inactive 10.1038/nature12393 2013-07-24
5VRA AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 7 chems 4.6-5.0 20°C ZM-241385 pubchem gtoplig chembl_ligand drugbank
Antagonist 2.4 Inactive 10.1038/NPROT.2017.135 2017-12-13
6D9H AA1R A1 Adenosine A (Rhodopsin) Human BaculovirusHi5Insect 2 chemicals 2 steps Cryo-EMVolta phase plate(FEI), FEI Titan Krios@300kV, Gatan K2 Summit direct electron camera , Gatan Quantum energy filter 6 chems 7.4-7.4 4°C adenosine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.6 Active 10.1038/S41586-018-0236-6 2018-06-20
7C7S GABR2 GABAB2 GABAB C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CGP 54626A pubchem gtoplig chembl_ligand gtoplig
Antagonist 2.9 Inactive 10.1038/S41422-020-0350-5 2020-07-01
7ARO AA2AR A2A Adenosine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A LUF5833 pubchem chembl_ligand
Agonist (partial) 3.1 Inactive 10.1021/ACS.JMEDCHEM.0C01856 2021-04-07
6PH7 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Nerol pubchem
unknown 2.9 Active 2020-07-01
5MZJ AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusTni PRO (Trichoplusia ni) cell linesInsect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 5.3-5.4 20 theophylline pubchem gtoplig chembl_ligand drugbank drug_central
Antagonist 2.0 Inactive 10.1016/j.str.2017.06.012 2017-07-26
6OS1 AGTR1 AT1 Angiotensin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A TRV023 pubchem gtoplig chembl_ligand
Agonist 2.8 Active 10.1126/SCIENCE.AAY9813 2020-02-19
6JOD AGTR2 AT2 Angiotensin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A angiotensin II pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Agonist 3.2 Active 10.1016/J.STR.2019.12.003 2020-01-15
7JVQ DRD1 D1 Dopamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A apomorphine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.0 Active 10.1016/J.CELL.2021.01.027 2021-02-24
4DAJ ACM3 M3 Acetylcholine (muscarinic) A (Rhodopsin) Rat BaculovirusSf9Insect 6 chemicals 6 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 7.5-7.5 22°C tiotropium pubchem gtoplig chembl_ligand drugbank gtoplig
Antagonist 3.4 Inactive 10.1038/NATURE10867 2012-02-22
3UZA AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusSf9Insect 1 chemicals 1 steps vapour diffusionsitting drop 6 chems 8.0-8.0 4°C compound 4g [PMID: 2... pubchem gtoplig chembl_ligand
Antagonist 3.3 Inactive 10.1021/JM201376W 2012-03-21
5DYS OPSD Rhodopsin Opsins A (Rhodopsin) Bovine Stable_cellsHEK293S-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionSitting drop 4 chems 4.5-4.5 20°C Retinal (all-trans) pubchem
Agonist 2.3 Active 10.15252/EMBR.201642671 2016-08-10
6KUX ADA2A α2A Adrenoceptors A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A RSC pubchem
Antagonist 2.7 Inactive 2019-12-04
6IIU TA2R TP Prostanoid A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ramatroban pubchem gtoplig chembl_ligand drug_central drugbank gtoplig
Antagonist 2.5 Intermediate 10.1038/S41589-018-0170-9 2018-12-19
6DRY 5HT2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A methylergonovine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.9 Intermediate 10.1038/s41594-018-0116-7 2018-08-29
6FKD OPSD Rhodopsin Opsins A (Rhodopsin) Bovine BaculovirusHEK293S(TetR)-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 4.5-4.5 20°C 5-chloro-2-(2-oxo-2-... pubchem
Agonist 2.5 Active 10.1073/PNAS.1718084115 2018-04-04
7W2Z GHSR ghrelin Ghrelin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Ghrelin pubchem
Agonist 2.8 Active 10.1038/S41467-022-27975-9 2022-01-19
6S0Q AA2AR A2A Adenosine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ZM-241385 pubchem gtoplig chembl_ligand drugbank
Antagonist 2.7 Inactive 2020-07-15
4U14 ACM3 M3 Acetylcholine (muscarinic) A (Rhodopsin) Rat BaculovirusSf9Insect 9 chemicals 9 steps sponge mesophaselipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 8.1-8.1 298 K tiotropium pubchem gtoplig chembl_ligand drugbank gtoplig
Antagonist 3.6 Inactive 10.1016/J.STR.2014.08.022 2014-11-26
7C4S S1PR3 S1P3 Lysophospholipid (S1P) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A sphingosine 1-phosph... pubchem gtoplig chembl_ligand pubchem
Agonist 3.2 Active 10.1126/SCIADV.ABF5325 2021-06-09
7DDZ NPY2R Y2 Neuropeptide Y A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL1823578 chembl_ligand pubchem
Antagonist 2.8 Inactive 2021-01-27
7LJD DRD1 D1 Dopamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A LY3154207 pubchem gtoplig chembl_ligand
dopamine pubchem gtoplig chembl_ligand drugbank drug_central
PAMAgonist 3.2 Active 10.1101/2021.02.07.430101 2021-03-03
6JZH AA2AR A2A Adenosine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ZM-241385 pubchem gtoplig chembl_ligand drugbank
Antagonist 2.3 Inactive 10.1107/S1600576719012846 2019-10-30
7E32 5HT1D 5-HT1D 5-Hydroxytryptamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 5-hydroxytryptamine pubchem gtoplig chembl_ligand drugbank
Agonist 2.9 Active 10.1038/S41586-021-03376-8 2021-04-21
6AK3 PE2R3 EP3 Prostanoid A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A PGE2 pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
Agonist 2.9 Active 10.1038/S41589-018-0171-8 2018-12-05
7F4D MSHR MC1 Melanocortin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A αMSH pubchem chembl_ligand pubchem pubchem
Agonist 3.0 Active 10.1038/S41422-021-00557-Y 2021-09-08
6UO8 GABR2 GABAB2 GABAB C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A GS39783 pubchem gtoplig chembl_ligand
CHEMBL112710 chembl_ligand pubchem pubchem
PAMAgonist 3.6 Active 10.1038/S41586-020-2408-4 2020-06-10
5CXV ACM1 M1 Acetylcholine (muscarinic) A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 8.0-8.0 20°C 0HK pubchem
Antagonist 2.7 Inactive 10.1038/NATURE17188 2016-03-09
7EPB GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A eglumegad pubchem gtoplig chembl_ligand gtoplig
Agonist 3.1 Inactive 10.1038/S41586-021-03641-W 2021-06-23
5EE7 GLR glucagon Glucagon B1 (Secretin) Human Transient_transfectionSf21Insect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 4 chems 5.5-6.5 20°C MK-0893 pubchem gtoplig chembl_ligand drugbank
Octaethylene glycol ... pubchem
NAMAntagonist 2.5 Inactive 10.1038/NATURE17414 2016-04-20
6OIK ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A iperoxo pubchem gtoplig chembl_ligand
LY2119620 pubchem gtoplig chembl_ligand
AgonistPAM 3.6 Active 10.1126/SCIENCE.AAW5188 2019-05-08
5K2B AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 5.0-5.0 20°C ZM-241385 pubchem gtoplig chembl_ligand drugbank
Antagonist 2.5 Inactive 10.1126/SCIADV.1600292 2016-09-21
4PXF OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionsitting drop 3 chems 6.0-6.0 4°C B-Octylglucoside pubchem
unknown 2.8 Active 10.1038/NCOMMS5801 2014-09-17
6WZG SCTR secretin Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A SECRETIN chembl_ligand pubchem
Agonist 2.3 Active 10.1038/S41467-020-17791-4 2020-08-12
6IGL EDNRB ETB Endothelin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A IRL 1620 pubchem gtoplig chembl_ligand gtoplig pubchem pubchem
Agonist (partial) 2.7 Inactive 10.1038/S41467-018-07094-0 2018-11-21
6TPG OX2R OX2 Orexin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A EMPA pubchem gtoplig chembl_ligand
Antagonist 2.7 Inactive 10.1021/ACS.JMEDCHEM.9B01787 2020-01-01
7JVR DRD2 D2 Dopamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A bromocriptine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.8 Active 10.1016/J.CELL.2021.01.027 2021-02-24
6M9T PE2R3 EP3 Prostanoid A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Misoprostol-FA pubchem
Agonist 2.5 Active 10.1038/S41589-018-0160-Y 2018-12-05
2Y00 ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 1 chemicals 1 steps vapour diffusionsitting drops 6 chems 8.5-8.5 4°C Dobutamine pubchem
Agonist (partial) 2.5 Inactive 10.1038/NATURE09746 2011-01-12
7F8X CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A NN9056
Agonist 3.0 Inactive 10.1038/S41589-021-00866-8 2021-12-29
5DHH OPRX NOP Opioid A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 6.4-6.4 20°C SB 612111 pubchem gtoplig chembl_ligand
Antagonist 3.0 Inactive 2015-10-21
6ZG4 ACM1 M1 Acetylcholine (muscarinic) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Ethyl (4S)-4-[4-[(1-... pubchem
Agonist 2.3 Inactive 10.1016/J.CELL.2021.11.001 2021-10-06
6FKC OPSD Rhodopsin Opsins A (Rhodopsin) Bovine BaculovirusHEK293S(TetR)-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 4.5-4.5 20°C 3-[1'-[(2~{S})-2-(4-... pubchem
Agonist 2.5 Active 10.1073/PNAS.1718084115 2018-04-04
7EPE GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL3894759 chembl_ligand pubchem
NAM 2.5 Inactive 10.1038/S41586-021-03641-W 2021-06-23
5ZBH NPY1R Y1 Neuropeptide Y A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A BMS-193885 pubchem
Antagonist 3.0 Inactive 10.1038/S41586-018-0046-X 2018-04-25
6FKB OPSD Rhodopsin Opsins A (Rhodopsin) Bovine BaculovirusHEK293S(TetR)-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 4.5-4.5 20°C 2-(4-Chlorophenyl)-1... pubchem
Agonist 3.0 Active 10.1073/PNAS.1718084115 2018-04-04
7DTT CASR CaS Calcium-sensing C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Calcium pubchem
Agonist 3.8 Inactive 10.1038/S41422-021-00474-0 2021-03-10
7EVZ S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A cenerimod pubchem gtoplig chembl_ligand drugbank
Agonist 3.1 Active 10.1038/S41422-021-00566-X 2021-09-29
3CAP OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drop 4 chems 5.6-5.6 4°C Apo (no ligand)
Apo (no ligand) 2.9 Active 10.1038/NATURE07063 2008-06-24
6K1Q EDNRB ETB Endothelin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A IRL 2500 pubchem gtoplig chembl_ligand
Inverse agonist 2.7 Inactive 10.1038/S42003-019-0482-7 2019-07-17
6D35 Q98SW5 SMO Frizzled F (Frizzled) African clawed frog BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 6.0-6.5 20°C Cholesterol pubchem
Agonist 3.9 Active 10.1016/J.CELL.2018.04.029 2018-05-23
7WC6 5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Lysergide pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.6 Inactive 10.1126/SCIENCE.ABL8615 2022-01-26
7EPF GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (8~{R})-4-[2,4-Bis(f... pubchem
NAM 2.7 Inactive 10.1038/S41586-021-03641-W 2021-06-23
5GLH EDNRB ETB Endothelin A (Rhodopsin) Human BaculovirusSF+Insect 6 chemicals 6 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 6.0-6.0 20°C ENDOTHELIN chembl_ligand pubchem
Agonist 2.8 Inactive 10.1038/nature19319 2016-09-07
6LFO CXCR2 CXCR2 Chemokine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Interleukin-8 pubchem
Agonist 3.4 Active 10.1038/S41586-020-2492-5 2020-09-02
3OE0 CXCR4 CXCR4 Chemokine A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 6.0-6.0 20°C CVX15
Antagonist 2.9 Inactive 10.1126/SCIENCE.1194396 2010-10-27
6MH8 AA2AR A2A Adenosine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ZM-241385 pubchem gtoplig chembl_ligand drugbank
Antagonist 4.2 Inactive 10.1107/S205225251900263X 2019-04-24
7T6S FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N-(4-chlorophenyl)-N... pubchem
Agonist 3.0 Active 2022-03-30
6KJV GLP1R GLP-1 Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A PF-06372222 pubchem
NAM 2.8 Inactive 10.1107/S2052252519013496 2019-11-13
4Z34 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 5.5-5.5 20°C ONO-9780307 pubchem gtoplig
Antagonist 3.0 Inactive 10.1016/J.CELL.2015.06.002 2015-06-03
7DUQ GLP1R GLP-1 Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A GLP-1 pubchem pubchem chembl_ligand
N-Tert-butyl-6,7-dic... pubchem
AgonistAgo-PAM 2.5 Active 10.1038/S41467-021-24058-Z 2021-07-14
5OLO AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusTni PRO (Trichoplusia ni) cell linesInsect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 5.3-5.4 20°C tozadenant pubchem gtoplig chembl_ligand drugbank
Antagonist 3.1 Inactive 10.1038/S41598-017-18570-W 2018-01-17
3RZE HRH1 H1 Histamine A (Rhodopsin) Human Pichia PastorisP. pastoris SMD1163Yeast 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 4.5-4.5 20-22°C doxepin pubchem gtoplig chembl_ligand drugbank gtoplig
Antagonist 3.1 Inactive 10.1038/NATURE10236 2011-06-15
7PIU MC4R MC4 Melanocortin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A setmelanotide pubchem gtoplig drug_central chembl_ligand drugbank
Agonist 2.6 Active 10.1038/S41422-021-00569-8 2021-11-17
3C9M OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANANA 1 chemicals 1 steps NANANA 1 chems 0.0-0.0 NA Retinal (11-cis) pubchem
Inverse agonist 3.4 Inactive 10.1107/S0907444908017162 2008-08-05
6ZDV AA2AR A2A Adenosine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 2-Methyl-3-(4-methyl... pubchem
Antagonist 2.1 Inactive 10.1002/ANIE.202003788 2020-09-16
5WQC OX2R OX2 Orexin A (Rhodopsin) Human BaculovirusSf9Insect 9 chemicals 9 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 4 chems 5.8-6.2 20°C EMPA pubchem gtoplig chembl_ligand
Antagonist 2.0 Inactive 10.1016/J.STR.2017.11.005 2017-11-29
7EVM GLP1R GLP-1 Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N-Tert-butyl-6,7-dic... pubchem
Ago-PAM 2.5 Active 10.1038/S41467-021-24058-Z 2021-08-11
6ZIN NTR1 NTS1 Neurotensin A (Rhodopsin) Rat N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A meclinertant pubchem gtoplig chembl_ligand drugbank
Inverse agonist 2.6 Inactive 10.1126/sciadv.abe5504 2021-02-10
6PS7 AA2AR A2A Adenosine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ZM-241385 pubchem gtoplig chembl_ligand drugbank
Antagonist 1.9 Inactive 10.1107/S2052252519013137 2019-11-13
7DHR ADRB2 β2 Adrenoceptors A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (R)-Isoproterenol pubchem chembl_ligand
Agonist 3.8 Active 10.1093/NSR/NWAA284 2020-12-16
5TE3 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drop 4 chems 5.2-6.6 4°C B-Octylglucoside pubchem
unknown 2.7 Active 10.1073/PNAS.1617446114 2017-03-15
4A4M OPSD Rhodopsin Opsins A (Rhodopsin) Bovine Stable_cellsHEK293TMammalian 1 chemicals 1 steps vapour diffusionsitting drop 3 chems 4.5-4.5 4°C Retinal (all-trans) pubchem
Agonist 3.3 Active 10.1073/PNAS.1114089108 2012-01-25
6WWZ CCR6 CCR6 Chemokine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CCL20 gtoplig
Agonist 3.3 Active 10.1038/S41467-020-16820-6 2020-06-24
7VH0 MTR1B MT2 Melatonin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ramelteon pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.5 Active 2022-03-02
3PWH AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusSf9Insect 1 chemicals 1 steps vapour diffusionsitting drop 6 chems 8.0-8.8 4°C ZM-241385 pubchem gtoplig chembl_ligand drugbank
Antagonist 3.3 Inactive 10.1016/J.STR.2011.06.014 2011-09-07
7FD9 GRM5 mGlu5 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A LY341495 pubchem gtoplig chembl_ligand gtoplig
Antagonist 4.0 Inactive 10.1016/J.CELREP.2021.109648 2021-09-08
4X1H OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionsitting drop 3 chems 5.0-6.5 4°C B-Nonylglucoside pubchem
unknown 2.3 Active 10.1016/J.STR.2015.09.015 2015-11-04
7F83 GHSR ghrelin Ghrelin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A PF-05190457 pubchem gtoplig chembl_ligand drugbank
Inverse agonist 2.9 Inactive 10.1038/S41467-022-27975-9 2022-01-19
7E33 5HT1E 5-HT1E 5-Hydroxytryptamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A BRL-54443 pubchem gtoplig chembl_ligand
Agonist 2.9 Active 10.1038/S41586-021-03376-8 2021-04-14
6ME4 MTR1A MT1 Melatonin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 2-iodo-melatonin pubchem gtoplig chembl_ligand drugbank
Agonist 3.2 Inactive 10.1038/S41586-019-1141-3 2019-04-24
6PS1 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A timolol pubchem gtoplig chembl_ligand drugbank drug_central
Antagonist 3.2 Inactive 10.1107/S2052252519013137 2019-11-13
7CX2 PE2R2 EP2 Prostanoid A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A PGE2 pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
Agonist 2.8 Active 10.1126/SCIADV.ABF1268 2021-05-05
3OE6 CXCR4 CXCR4 Chemokine A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 5.5-5.5 20°C isothiourea-1t pubchem gtoplig chembl_ligand
Antagonist 3.2 Inactive 10.1126/SCIENCE.1194396 2010-10-27
6QZH CCR7 CCR7 Chemokine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A SCHEMBL13407377 pubchem
Allosteric antagonist 2.1 Inactive 10.1016/J.CELL.2019.07.028 2019-09-04
5T04 NTR1 NTS1 Neurotensin A (Rhodopsin) Rat BaculovirusTni PRO (Trichoplusia ni) cell linesInsect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 8.5-9.0 20°C neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
Agonist 3.3 Active 10.1038/SREP38564 2016-12-21
5ZBQ NPY1R Y1 Neuropeptide Y A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 4 chems 7.4-8.0 19–22 °C CHEMBL3747822 chembl_ligand chembl_ligand chembl_ligand pubchem
Antagonist 2.7 Inactive 10.1038/S41586-018-0046-X 2018-04-25
7F4F MSHR MC1 Melanocortin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A [Nle4,D-Phe7]-αMSH pubchem chembl_ligand
Agonist 2.9 Active 10.1038/S41422-021-00557-Y 2021-09-08
7T6V FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A synthetic peptide
Agonist 3.1 Active 2022-03-30
6W2Y GABR1 GABAB1 GABAB C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CGP55845 pubchem
1-Stearoyl-2-oleoyl-... pubchem
Inverse agonistNAM 3.2 Inactive 10.1038/S41586-020-2469-4 2020-07-01
4NC3 5HT2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 8.0-8.0 20°C ergotamine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.8 Intermediate 10.1126/SCIENCE.1244142 2013-12-18
7MTS GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem
2-methoxy-6-propyl-N... pubchem
AgonistAgo-PAM 3.2 Active 10.1038/S41586-021-03680-3 2021-07-07
7KI1 GLP1R GLP-1 Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Taspoglutide pubchem
Agonist 2.5 Active 10.1016/J.CELREP.2021.109374 2021-08-04
5ZHP ACM3 M3 Acetylcholine (muscarinic) A (Rhodopsin) Rat N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (1R,2R,4S,5S,7s)-7-(... pubchem
Antagonist 3.1 Inactive 10.1073/PNAS.1813988115 2018-11-28
5G53 AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusTni PRO (Trichoplusia ni) cell linesInsect 1 chemicals 1 steps vapour diffusionSitting drop 6 chems 5.7-5.7 4°C NECA pubchem gtoplig chembl_ligand gtoplig
Agonist 3.4 Active 10.1038/NATURE18966 2016-08-03
6PGS OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Geraniol pubchem
unknown 2.9 Active 2020-07-01
1U19 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 6.5-7.5 283 K Retinal (11-cis) pubchem
Inverse agonist 2.2 Inactive 10.1016/J.JMB.2004.07.044 2004-10-12
5WF5 AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 5.0-5.0 20°C UK-432,097 pubchem gtoplig chembl_ligand drugbank
Agonist 2.6 Active 10.1016/J.STR.2017.12.013 2018-02-21
2X72 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine Stable_cellsHEK293S-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionsitting drop 3 chems 4.5-4.5 4°C Retinal (all-trans) pubchem
Agonist 3.0 Active 10.1038/NATURE09795 2011-03-16
6M1I PACR PAC1 VIP and PACAP B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL524658 chembl_ligand pubchem
Agonist 3.5 Active 10.1038/S41422-020-0280-2 2020-03-11
6W2X GABR2 GABAB2 GABAB C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CGP55845 pubchem
1-Stearoyl-2-oleoyl-... pubchem
Inverse agonistNAM 3.6 Inactive 10.1038/S41586-020-2469-4 2020-07-01
6HLL NK1R NK1 Tachykinin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CP 99994 pubchem gtoplig chembl_ligand
Antagonist 3.3 Inactive 10.1038/S41467-018-07939-8 2019-01-16
7L0R NTR1 NTS1 Neurotensin A (Rhodopsin) Rat N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
Agonist 4.2 Active 2021-01-06
6IIV TA2R TP Prostanoid A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A daltroban pubchem gtoplig chembl_ligand
Antagonist 3.0 Intermediate 10.1038/S41589-018-0170-9 2018-12-19
4RWD OPRD δ Opioid A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 6.0-6.0 20°C DIPP-NH2
Antagonist 2.7 Inactive 10.1038/NSMB.2965 2015-01-14
5ZK3 ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL558910 chembl_ligand pubchem
Antagonist 2.6 Inactive 10.1038/S41589-018-0152-Y 2018-11-21
5NM4 AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusSf9Insect 1 chemicals 1 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 5 chems 5.0-5.0 20°C ZM-241385 pubchem gtoplig chembl_ligand drugbank
Antagonist 1.7 Inactive 10.1038/S41467-017-00630-4 2017-09-27
6AQF AA2AR A2A Adenosine A (Rhodopsin) Human Pichia PastorisP. pastoris SMD1163Yeast 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 5.0-5.0 20°C ZM-241385 pubchem gtoplig chembl_ligand drugbank
Antagonist 2.5 Inactive 10.1016/J.CELL.2017.12.004 2018-01-10
6IBL ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A arformoterol pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.7 Active 10.1101/436212 2019-01-09
7JNI AGTR2 AT2 Angiotensin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A olodanrigan pubchem gtoplig chembl_ligand drugbank
Antagonist 3.0 Active 2022-02-09
5WIV DRD4 D4 Dopamine A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 5.9-6.2 20°C [3H]NEMONAPRIDE chembl_ligand pubchem
Antagonist 2.1 Inactive 10.1126/SCIENCE.AAN5468 2017-10-18
7CA5 GABR2 GABAB2 GABAB C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 7.6 Intermediate 10.1016/J.JMB.2020.09.023 2020-11-11
7EW2 S1PR3 S1P3 Lysophospholipid (S1P) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (S)-FTY720-phosphate pubchem gtoplig chembl_ligand
Agonist 3.1 Active 10.1038/S41422-021-00567-W 2021-09-29
7EIB BKRB1 B1 Bradykinin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A [des-Arg<sup>10</sup... pubchem gtoplig chembl_ligand gtoplig
Agonist 3.0 Active 10.1038/S41594-021-00645-Y 2021-10-13
3KJ6 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 3 chemicals 3 steps vapour diffusionbicelles 5 chems 7.5-7.5 298K N/A N/A 3.4 Inactive 10.1038/NATURE08650 2010-02-16
6LI3 GPR52 GPR52 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.3 Active 10.1038/S41586-020-2019-0 2020-02-26
7TZF CALCR CT Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A amylin peptide
Agonist 2.4 Active 10.1126/SCIENCE.ABM9609 2022-03-23
7MTR GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem
2-methoxy-6-propyl-N... pubchem
AgonistAgo-PAM 3.3 Active 10.1038/S41586-021-03680-3 2021-07-07
6LI2 GPR52 GPR52 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 2.8 Intermediate 10.1038/S41586-020-2019-0 2020-02-26
7KNU CALRL calcitonin-like Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Calcitonin gene-rela... pubchem
Agonist 3.5 Inactive 10.1126/SCIENCE.ABF7258 2021-02-24
7LD4 AA1R A1 Adenosine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A adenosine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.3 Active 10.1038/S41586-021-03897-2 2021-09-08
5O9H C5AR1 C5a1 Complement peptide A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 5 chems 5.5-6.0 22.5°C NDT9513727 pubchem gtoplig chembl_ligand
Antagonist 2.7 Inactive 10.1038/NATURE25025 2018-01-10
6ME2 MTR1A MT1 Melatonin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ramelteon pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.8 Inactive 10.1038/S41586-019-1141-3 2019-04-24
7EVY S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A siponimod pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.0 Active 10.1038/S41422-021-00566-X 2021-09-29
6P9Y PACR PAC1 VIP and PACAP B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL524658 chembl_ligand pubchem
Agonist 3.0 Active 10.1016/J.MOLCEL.2020.01.012 2020-02-05
6TQ6 OX1R OX1 Orexin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL4592653 chembl_ligand pubchem
Antagonist 2.6 Inactive 10.1021/ACS.JMEDCHEM.9B01787 2020-01-01
3V2Y S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 7.8-7.8 20°C W146 pubchem gtoplig chembl_ligand
Antagonist 2.8 Inactive 10.1126/SCIENCE.1215904 2012-02-15
7F53 MC4R MC4 Melanocortin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A α-MSH pubchem gtoplig
Agonist 3.0 Active 10.1038/S41422-021-00552-3 2021-11-03
7E14 GLP1R GLP-1 Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N-Tert-butyl-6,7-dic... pubchem
CHEMBL4446782 chembl_ligand pubchem
Ago-PAMAgonist 2.9 Active 10.1038/S41467-021-24058-Z 2021-07-07
7WI6 GRM3 mGlu3 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A LY341495 pubchem gtoplig chembl_ligand gtoplig
Antagonist 3.7 Inactive 10.1038/S41422-022-00623-Z 2022-03-16
3RFM AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusSf9Insect 1 chemicals 1 steps vapour diffusionsitting drop 6 chems 8.0-8.8 4°C caffeine pubchem gtoplig chembl_ligand drugbank drug_central
Antagonist 3.6 Inactive 10.1016/J.STR.2011.06.014 2011-09-07
7T6T FPR1 FPR1 Formylpeptide A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A synthetic peptide
Agonist 3.2 Active 2022-03-30
7TYW CALCR CT Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Calcitonin salmon pubchem
Agonist 3.0 Active 10.1126/SCIENCE.ABM9609 2022-03-23
6TPJ OX2R OX2 Orexin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A suvorexant pubchem gtoplig chembl_ligand drug_central drugbank
Antagonist 2.7 Inactive 10.1021/ACS.JMEDCHEM.9B01787 2020-01-01
7VUH GP139 GPR139 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A JNJ-63533054 pubchem gtoplig chembl_ligand
Agonist 3.2 Active 10.1038/S41422-021-00591-W 2021-12-29
7M3J CASR CaS Calcium-sensing C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A NPS 2143 pubchem gtoplig chembl_ligand drugbank
NAM 4.1 Inactive 10.1038/S41586-021-03691-0 2021-06-30
7SIN CASR CaS Calcium-sensing C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A NPS 2143 pubchem gtoplig chembl_ligand drugbank
Antagonist 5.9 Active 10.1073/PNAS.2115849118 2022-01-19
3C9L OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANANA 1 chemicals 1 steps NANANA 1 chems 0.0-0.0 NA Retinal (11-cis) pubchem
Inverse agonist 2.7 Inactive 10.1107/S0907444908017162 2008-08-05
6I9K B1B1U5 Rhodopsin Opsins A (Rhodopsin) Hasarius adansoni N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Retinal (11-cis) pubchem
Inverse agonist 2.2 Inactive 10.1073/PNAS.1902192116 2019-07-03
5ZK8 ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N-methyl scopolamine pubchem gtoplig drugbank gtoplig
Antagonist 3.0 Inactive 10.1038/S41589-018-0152-Y 2018-11-21
5NDZ PAR2 PAR2 Proteinase-activated A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 5.5-6.2 20°C AZ3451 pubchem gtoplig chembl_ligand
Allosteric antagonist 3.6 Intermediate 10.1038/NATURE22309 2017-05-03
4JKV SMO SMO Frizzled F (Frizzled) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 6 chems 7.4-7.4 20°C taladegib pubchem gtoplig chembl_ligand drugbank
Antagonist 2.5 Inactive 10.1038/NATURE12167 2013-04-24
7PYR AA2AR A2A Adenosine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Preladenant conjugat...
Antagonist 2.6 Inactive 10.1002/ANIE.202115545 2022-03-02
7TYN CALCR CT Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Calcitonin salmon pubchem
Agonist 2.6 Active 10.1126/SCIENCE.ABM9609 2022-03-30
5D5B ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 6.5-7.0 20°C Carazolol pubchem
Inverse agonist 3.8 Inactive 10.1107/S2059798315021683 2016-01-13
6PRZ ADRB2 β2 Adrenoceptors A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL1160734 chembl_ligand pubchem
Antagonist 2.8 Inactive 10.1107/S2052252519013137 2019-11-13
7VBI GLP1R GLP-1 Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Tirzepatide pubchem
Agonist 3.0 Active 10.1038/S41467-022-28683-0 2022-03-02
7MTB OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Retinal (all-trans) pubchem
Agonist 4.0 Active 10.1038/S41586-021-03721-X 2021-07-07
5A8E ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 4 chems 7.0-7.0 20°C 7-methylcyanopindolo... pubchem
Inverse agonist 2.4 Inactive 10.1124/MOL.115.101030 2015-09-30
7VGZ MTR1A MT1 Melatonin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ramelteon pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.3 Active 2022-03-02
6U1N ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A LY2119620 pubchem gtoplig chembl_ligand
Agonist 4.0 Active 10.1038/S41586-020-1954-0 2020-02-26
6PT3 OPRD δ Opioid A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A DPI-287 pubchem
Agonist 3.3 Active 10.1126/SCIADV.AAX9115 2019-12-11
5VAI G1SGD4 GLP-1 Glucagon B1 (Secretin) Rabbit BaculovirusSf9Insect 6 chemicals 6 steps Cryo-EMFEI, glow-discharged holey carbon grids 7 chems 7.5-7.5 20°C GLP-1 pubchem pubchem chembl_ligand
Agonist 4.1 Active 10.1038/NATURE22394 2017-05-24
5V56 SMO SMO Frizzled F (Frizzled) Human Transient_transfectionHEK293FMammalian 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 5.0-5.0 20°C N-methyl-N-[1-[4-(2-... pubchem
Antagonist 2.9 Inactive 10.1038/NCOMMS15383 2017-05-24
7E6T CASR CaS Calcium-sensing C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Calcium pubchem
Cyclomethyltryptopha... pubchem
AgonistPAM 3.0 Inactive 10.7554/ELIFE.68578 2021-09-22
7LLL GLP1R GLP-1 Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A exendin-4 pubchem gtoplig pubchem
Agonist 3.7 Active 10.1038/S41467-021-27760-0 2022-01-12
6DRX 5HT2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A lisuride pubchem gtoplig chembl_ligand drugbank drug_central
Antagonist 3.1 Intermediate 10.1038/s41594-018-0116-7 2018-08-29
7WC5 5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A psilocin pubchem gtoplig chembl_ligand
Agonist 3.2 Inactive 10.1126/SCIENCE.ABL8615 2022-01-26
6WJC ACM1 M1 Acetylcholine (muscarinic) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ENDO-ATROPINE chembl_ligand pubchem
muscarinic toxin 7 gtoplig
AntagonistNAM 2.6 Inactive 10.1126/SCIENCE.AAX2517 2020-07-08
6LPK AA2AR A2A Adenosine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ZM-241385 pubchem gtoplig chembl_ligand drugbank
Antagonist 1.8 Inactive 10.1038/S41598-020-76277-X 2020-11-25
5N2S AA1R A1 Adenosine A (Rhodopsin) Human BaculovirusTni PRO (Trichoplusia ni) cell linesInsect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 4 chems 7.5-7.5 20°C PSB36 pubchem
Agonist 3.3 Inactive 10.1016/j.str.2017.06.012 2017-07-26
3ZPR ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 1 chemicals 1 steps vapour diffusionsitting drops 3 chems 9.0-9.0 4°C CHEMBL1559535 chembl_ligand pubchem
Antagonist 2.7 Inactive 10.1021/JM400140Q 2013-04-03
7F8V GASR CCK2 Cholecystokinin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A desulfated gastrin-1... pubchem gtoplig chembl_ligand pubchem
Agonist 3.3 Active 10.1038/S41589-021-00866-8 2021-10-13
5UNF AGTR2 AT2 Angiotensin A (Rhodopsin) Human BaculovirusSf21Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 7 chems 8.0-8.0 20°C compound 1 [PMID: 28... pubchem gtoplig chembl_ligand
Antagonist 2.8 Active 10.1038/NATURE22035 2017-04-05
5YC8 ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N-methyl scopolamine pubchem gtoplig drugbank gtoplig
Antagonist 2.5 Inactive 10.1038/S41589-018-0152-Y 2018-11-21
5TE5 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drop 4 chems 5.2-6.6 4°C 10,20-Methanoretinal pubchem
Agonist 4.0 Inactive 2017-03-15
6H7J ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (R)-Isoproterenol pubchem chembl_ligand
Agonist 2.8 Active 10.1126/SCIENCE.AAU5595 2018-10-17
7PX4 AA2AR A2A Adenosine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Preladenant conjugat... pubchem
Antagonist 2.3 Inactive 10.1002/ANIE.202115545 2022-03-02
5X33 Q9WTK1 BLT1 Leukotriene A (Rhodopsin) Guinea pig Pichia PastorisP. pastoris SMD1163Yeast 4 chemicals 4 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 7 chems 8.5-9.0 4°C BIIL 260 pubchem gtoplig
Antagonist 3.7 Inactive 10.1038/NCHEMBIO.2547 2018-01-03
5D6L ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 7.0-7.0 20°C Carazolol pubchem
Inverse agonist 3.2 Inactive 10.1038/NPROT.2017.057 2016-08-17
2Z73 OPSD Rhodopsin Opsins A (Rhodopsin) Japanese flying squid NANativeSquid 1 chemicals 1 steps vapour diffusionsitting drops 5 chems 6.4-6.4 4°C Retinal (11-cis) pubchem
Inverse agonist 2.5 Inactive 10.1038/NATURE06925 2008-05-13
7MT9 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Retinal (all-trans) pubchem
Agonist 7.0 Active 10.1038/S41586-021-03721-X 2021-07-07
7BW0 GPBAR GPBA Bile acid A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 3.9 Active 10.1038/S41392-020-00262-Z 2020-09-02
6WHA 5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 25-CN-NBOH pubchem
Agonist 3.4 Active 10.1016/J.CELL.2020.08.024 2020-09-23
7F54 MC4R MC4 Melanocortin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A afamelanotide pubchem gtoplig chembl_ligand drugbank pubchem pubchem pubchem pubchem
Agonist 3.0 Active 10.1038/S41422-021-00552-3 2021-11-03
7DD7 CASR CaS Calcium-sensing C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Calcium pubchem
L-tryptophan pubchem gtoplig chembl_ligand drugbank drug_central pubchem
evocalcet pubchem gtoplig drug_central chembl_ligand drugbank
AgonistPAMPAM 3.2 Active 10.1126/SCIADV.ABG1483 2021-06-16
6NI3 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A BI-167107 pubchem
Agonist 3.8 Active 10.1038/S41594-019-0330-Y 2019-11-20
6WH4 5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL428892 chembl_ligand pubchem
Inverse agonist 3.4 Inactive 10.1016/J.CELL.2020.08.024 2020-09-23
7EVW FZD7 FZD7 Frizzled F (Frizzled) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.2 Active 10.1038/S41422-021-00525-6 2021-08-04
6VN7 VIPR1 VPAC1 VIP and PACAP B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL524658 chembl_ligand pubchem
Agonist 3.2 Active 10.1038/S41467-020-17933-8 2020-09-02
5OLG AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusTni PRO (Trichoplusia ni) cell linesInsect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 5.3-5.4 20°C ZM-241385 pubchem gtoplig chembl_ligand drugbank
Antagonist 1.9 Inactive 10.1038/S41598-017-18570-W 2018-01-17
3V2W S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 7.8-7.8 20°C W146 pubchem gtoplig chembl_ligand
Antagonist 3.4 Inactive 10.1126/SCIENCE.1215904 2012-02-15
7L1V OX2R OX2 Orexin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A compound 1 [PMID: 33... pubchem gtoplig
Agonist 3.0 Active 10.1038/S41467-021-21087-6 2021-02-10
5OM4 AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusTni PRO (Trichoplusia ni) cell linesInsect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 5.3-5.4 20°C CHEMBL2024114 chembl_ligand pubchem
Antagonist 2.0 Inactive 10.1038/S41598-017-18570-W 2018-01-17
5UNH AGTR2 AT2 Angiotensin A (Rhodopsin) Human BaculovirusSf21Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 7 chems 8.0-8.0 20°C compound 2 [PMID: 28... pubchem gtoplig
Antagonist 2.9 Active 10.1038/NATURE22035 2017-04-05
6LPJ AA2AR A2A Adenosine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ZM-241385 pubchem gtoplig chembl_ligand drugbank
Antagonist 1.8 Inactive 10.1038/S41598-020-76277-X 2020-11-25
5CGC GRM5 mGlu5 Metabotropic glutamate C (Glutamate) Human BaculovirusSf21Insect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 4 chems 5.5-6.8 20°C CHEMBL3603915 chembl_ligand pubchem
NAM 3.1 Inactive 10.1021/ACS.JMEDCHEM.5B00892 2015-08-12
4PHU FFAR1 FFA1 Free fatty acid A (Rhodopsin) Human BaculovirusSf9Insect 6 chemicals 6 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 7.6-7.6 20°C fasiglifam pubchem gtoplig chembl_ligand drugbank
Agonist 2.3 Intermediate 10.1038/NATURE13494 2014-07-16
7EZM CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CCK-8 pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 2.9 Active 2021-08-25
5UVI AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 5.0-5.0 20°C ZM-241385 pubchem gtoplig chembl_ligand drugbank
Antagonist 3.2 Inactive 10.1107/S205225251700570X 2017-05-24
5XPR EDNRB ETB Endothelin A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 7.0-7.0 20°C N/A N/A 3.6 Inactive 10.1038/NSMB.3450 2017-08-16
1L9H OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 6.0-6.0 4°C Retinal (11-cis) pubchem
Inverse agonist 2.6 Inactive 10.1073/PNAS.082666399 2002-05-15
6B3J GLP1R GLP-1 Glucagon B1 (Secretin) Human BaculovirusTni PRO (Trichoplusia ni) cell linesInsect 2 chemicals 2 steps Cryo-EMVolta phase plate (FEI) 5 chems 7.4-7.4 4°C Exendin-P5
Agonist 3.3 Active 10.1038/NATURE25773 2018-02-21
7EO4 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A siponimod pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 2.9 Active 10.1038/S41589-021-00930-3 2022-01-05
7BVQ ADRB1 β1 Adrenoceptors A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Carazolol pubchem
Inverse agonist 2.5 Inactive 10.1038/S41422-020-00424-2 2020-12-02
7M3E CASR CaS Calcium-sensing C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Calcium pubchem
NPS 2143 pubchem gtoplig chembl_ligand drugbank
L-tryptophan pubchem gtoplig chembl_ligand drugbank drug_central pubchem
AgonistNAMPAM 3.2 Inactive 10.1038/S41586-021-03691-0 2021-06-30
6ME7 MTR1B MT2 Melatonin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 2-phenylmelatonin pubchem
Agonist 3.2 Inactive 10.1038/S41586-019-1144-0 2019-04-24
6H7L ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Dobutamine pubchem
Agonist 2.7 Active 10.1126/SCIENCE.AAU5595 2018-10-17
5CGD GRM5 mGlu5 Metabotropic glutamate C (Glutamate) Human BaculovirusSf21Insect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 4 chems 5.5-6.8 20°C CHEMBL3603923 chembl_ligand pubchem
NAM 2.6 Inactive 10.1021/ACS.JMEDCHEM.5B00892 2015-08-12
6PS6 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A timolol pubchem gtoplig chembl_ligand drugbank drug_central
Antagonist 2.7 Inactive 10.1107/S2052252519013137 2019-11-13
4ZJ8 OX1R OX1 Orexin A (Rhodopsin) Human BaculovirusSf9Insect 6 chemicals 6 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 5.4-5.4 20°C suvorexant pubchem gtoplig chembl_ligand drug_central drugbank
Antagonist 2.8 Inactive 10.1038/NSMB.3183 2016-03-09
7F2O BKRB2 B2 Bradykinin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A bradykinin pubchem gtoplig chembl_ligand drugbank gtoplig
Agonist 2.9 Active 10.1038/S41594-021-00645-Y 2021-10-13
6GPS CCR2 CCR2 Chemokine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A MK-0812 pubchem
Antagonist 3.3 Inactive 10.1016/J.STR.2018.10.027 2019-01-02
3NY8 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 7.5-8.0 20°C CHEMBL1233766 chembl_ligand pubchem
Inverse agonist 2.8 Inactive 10.1021/JA105108Q 2010-08-11
5ZKQ PTAFR PAF Platelet-activating factor A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ABT-491 pubchem gtoplig chembl_ligand
Inverse agonist 2.9 Intermediate 10.1038/S41594-018-0068-Y 2018-06-20
6NBH PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Long-acting parathyr...
Agonist 3.5 Active 10.1126/SCIENCE.AAV7942 2019-04-17
7MTQ GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A LY341495 pubchem gtoplig chembl_ligand gtoplig
Antagonist 3.7 Inactive 10.1038/S41586-021-03680-3 2021-07-07
6X1A GLP1R GLP-1 Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A DANUGLIPRON chembl_ligand pubchem
Agonist 2.5 Active 10.1101/2020.08.16.252585 2020-09-09
6TPK OXYR OT Vasopressin and oxytocin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A retosiban pubchem gtoplig chembl_ligand drugbank
Antagonist 3.2 Inactive 10.1126/SCIADV.ABB5419 2020-08-05
7TYI CALCR CT Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Amylin rat pubchem
Agonist 3.3 Active 10.1126/SCIENCE.ABM9609 2022-03-30
5YHL PE2R4 EP4 Prostanoid A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ONO-AE3-208-Br pubchem
Antagonist 4.2 Inactive 10.1038/S41589-018-0131-3 2018-12-05
7P02 NK1R NK1 Tachykinin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A substance P pubchem gtoplig chembl_ligand gtoplig gtoplig
Agonist 2.9 Active 10.1126/SCIADV.ABK2872 2021-12-15
7VDL MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Cortistatin 14 pubchem
Agonist 3.2 Active 2021-12-01
6KK7 GLP1R GLP-1 Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A PF-06372222 pubchem
NAM 3.1 Inactive 10.1107/S2052252519013496 2019-11-13
6KNM APJ apelin Apelin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Single domain antibo...
Agonist 3.2 Inactive 10.1126/SCIADV.AAX7379 2020-01-29
4OR2 GRM1 mGlu1 Metabotropic glutamate C (Glutamate) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 7.0-7.0 20°C FITM pubchem gtoplig chembl_ligand
NAM 2.8 Inactive 10.1126/science.1249489 2014-03-19
6WHC GLR glucagon Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Dual-agonist peptide...
Agonist 3.4 Active 10.1074/JBC.RA120.013793 2020-05-27
7F16 PTH2R PTH2 Parathyroid hormone B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A TIP39 gtoplig
Agonist 2.8 Active 10.1073/PNAS.2101279118 2021-08-18
2Y02 ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 1 chemicals 1 steps vapour diffusionsitting drops 6 chems 9.0-9.0 4°C CARMOTEROL chembl_ligand pubchem pubchem
Agonist 2.6 Inactive 10.1038/NATURE09746 2011-01-12
6LPL AA2AR A2A Adenosine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ZM-241385 pubchem gtoplig chembl_ligand drugbank
Antagonist 2.0 Inactive 10.1038/S41598-020-76277-X 2020-11-25
7LCK GLP1R GLP-1 Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A DANUGLIPRON chembl_ligand pubchem
Agonist 3.2 Active 2021-01-20
6RZ8 CLTR2 CysLT2 Leukotriene A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ONO-2080365 pubchem
Antagonist 2.7 Intermediate 10.1038/S41467-019-13348-2 2019-12-11
7LLY GLP1R GLP-1 Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Pro-glucagon pubchem
Agonist 3.3 Active 2022-01-12
6OFJ OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 4.5 Inactive 10.1074/JBC.RA119.010089 2019-08-21
6IGK EDNRB ETB Endothelin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A endothelin-3 pubchem gtoplig
Agonist 2.0 Inactive 10.1038/S41467-018-07094-0 2018-11-21
6Z4S NTR1 NTS1 Neurotensin A (Rhodopsin) Rat N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A meclinertant pubchem gtoplig chembl_ligand drugbank
Inverse agonist 2.7 Inactive 10.1126/sciadv.abe5504 2021-02-10
6D27 PD2R2 DP2 Prostanoid A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL179036 chembl_ligand pubchem
Antagonist 2.7 Inactive 10.1016/J.MOLCEL.2018.08.009 2018-10-03
4UG2 AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusHi5Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 3 chems 7.0-7.0 22°C CGS 21680 pubchem gtoplig chembl_ligand gtoplig
Agonist 2.6 Active 10.1124/mol.114.097360 2015-04-08
6TQ9 OX1R OX1 Orexin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A SB-408124 pubchem gtoplig chembl_ligand
Antagonist 2.7 Inactive 10.1021/ACS.JMEDCHEM.9B01787 2020-01-01
6A94 5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A zotepine pubchem gtoplig chembl_ligand drug_central drugbank
Antagonist 2.9 Inactive 10.1038/S41594-018-0180-Z 2019-02-13
7BZ2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A arformoterol pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.8 Active 10.1038/S41421-020-0176-9 2020-08-05
6DRZ 5HT2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A methysergide pubchem gtoplig chembl_ligand drugbank drug_central
Antagonist 3.1 Intermediate 10.1038/s41594-018-0116-7 2018-08-29
6LFL CXCR2 CXCR2 Chemokine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 4-[[3,4-Dioxo-2-[[(1... pubchem
Allosteric antagonist 3.2 Inactive 10.1038/S41586-020-2492-5 2020-09-02
7EWL GP158 GPR158 C Orphans C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.5 Inactive 10.1038/S41467-021-27147-1 2021-12-01
7TYH CALCR CT Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Calcitonin human pubchem
Agonist 3.3 Active 10.1126/SCIENCE.ABM9609 2022-03-23
7EWR GP158 GPR158 C Orphans C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 4.7 Inactive 10.1038/S41467-021-27147-1 2021-12-01
5K2C AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 5.0-5.0 20°C ZM-241385 pubchem gtoplig chembl_ligand drugbank
Antagonist 1.9 Inactive 10.1126/SCIADV.1600292 2016-09-21
7CZ5 GHRHR GHRH Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Somatoliberin pubchem
Agonist 2.6 Active 10.1038/S41467-020-18945-0 2020-11-18
7E2X 5HT1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.0 Active 10.1038/S41586-021-03376-8 2021-04-14
7D3S SCTR secretin Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A SECRETIN chembl_ligand pubchem
Agonist 2.9 Active 10.1016/J.BBRC.2020.08.042 2020-11-04
7T6U FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A synthetic peptide
Agonist 2.9 Active 2022-03-30
6UVA CALRL calcitonin-like Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A adrenomedullin 2/int... gtoplig
Agonist 2.3 Active 10.1021/ACSPTSCI.9B00080 2020-04-01
7F9Z GHSR ghrelin Ghrelin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A GHRP-6 pubchem gtoplig
Agonist 3.2 Active 2021-08-18
4QIM SMO SMO Frizzled F (Frizzled) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 5 chems 7.2-7.2 20°C ANTA XV pubchem gtoplig chembl_ligand
Antagonist 2.6 Inactive 10.1038/NCOMMS5355 2014-07-23
6PS4 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL1233766 chembl_ligand pubchem
Antagonist 2.6 Inactive 10.1107/S2052252519013137 2019-11-13
6BD4 FZD4 FZD4 Frizzled F (Frizzled) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 2.4 Inactive 10.1038/S41586-018-0447-X 2018-08-22
4BVN ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 4 chems 7.0-7.0 22°C (S)-Cyanopindolol pubchem
Antagonist 2.1 Inactive 10.1371/JOURNAL.PONE.0092727 2014-04-02
6OYA OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Retinal (all-trans) pubchem
Agonist 3.3 Active 10.1016/J.MOLCEL.2019.06.007 2019-07-24
7L0Q NTR1 NTS1 Neurotensin A (Rhodopsin) Rat N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
Agonist 4.3 Active 2021-01-06
4DJH OPRK κ Opioid A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 6.0-6.0 20°C JDTic pubchem gtoplig chembl_ligand
Antagonist 2.9 Inactive 10.1038/NATURE10939 2012-03-21
7CKY DRD1 D1 Dopamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A PW0464 (24) pubchem chembl_ligand
Agonist 3.2 Active 10.1016/J.CELL.2021.01.028 2021-03-03
7F4H MSHR MC1 Melanocortin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A [Nle4,D-Phe7]-αMSH pubchem chembl_ligand
Agonist 2.7 Active 10.1038/S41422-021-00557-Y 2021-09-08
6XOX GLP1R GLP-1 Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL4446782 chembl_ligand pubchem
Agonist 3.1 Active 10.1073/PNAS.2014879117 2020-11-18
6E3Y CALRL calcitonin-like Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Calcitonin gene-rela... pubchem
Agonist 3.3 Active 10.1038/S41586-018-0535-Y 2018-09-19
7E9H GRM4 mGlu4 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A L-serine-O-phosphate pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Agonist 4.0 Active 10.1038/S41586-021-03495-2 2021-06-23
5DHG OPRX NOP Opioid A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 6.4-6.4 20°C CHEMBL1783826 chembl_ligand pubchem
Antagonist 3.0 Inactive 10.1016/J.STR.2015.07.024 2015-10-21
7CKX DRD1 D1 Dopamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A A77636 pubchem gtoplig chembl_ligand
Agonist 3.5 Active 10.1016/J.CELL.2021.01.028 2021-03-03
5UIG AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps vapour diffusionSitting drop 6 chems 7.0-7.0 20°C 5-Amino-N-[(2-Methox... pubchem
Antagonist 3.5 Inactive 10.1073/PNAS.1621423114 2017-02-08