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RECEPTOR EXPRESSION SOLUBILIZATION PURIFICATION STRUCTURE DETERMINATION
PDB pH Temp Resolution Reference Date
8X63 HRH1 H1 Histamine 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 mepyramine pubchem gtoplig chembl_ligand drugbank drug_central
Inverse agonist 3.2 Inactive 10.1038/S41467-023-44477-4 2024-01-17
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
Inverse agonist 3.3 Inactive 10.1016/J.STR.2011.06.014 2011-09-07
8XZF 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 WN561
Agonist 3.0 Active 10.1016/J.CELL.2024.02.004 2024-03-20
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
8W8R GP101 GPR101 Orphan 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 AA-14 pubchem
Allosteric agonist 3.3 Active 10.1038/S41589-023-01456-6 2024-01-03
8DPI 5HT2C 5-HT2C 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 lorcaserin pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.4 Active 10.1016/J.CELREP.2022.111211 2022-08-24
4ZWJ OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Human Transient_transfectionHEK293S(TetR)-GnTI-Mammalian 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monopalmitolein (9.7 MAG) 5 chems 5.0-5.0 20°C Apo (no ligand)
3.3 Active 10.1038/NATURE14656 2015-07-29
9IIW T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A compound 28.1 [PMID:... pubchem gtoplig chembl_ligand
compound 28.1 [PMID:... pubchem gtoplig chembl_ligand
Allosteric agonistAgonist 3.2 Active 2024-07-24
8Y53 BRS3 BB3 Bombesin 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-5046 pubchem gtoplig chembl_ligand
Agonist 2.9 Active 2024-09-11
6PB1 CRHR2 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
Cholesterol pubchem drugbank
AgonistPAM 2.8 Active 10.1016/J.MOLCEL.2020.01.013 2020-02-12
6NWE OPSD Rhodopsin Opsin (sight) 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)
2.7 Active 2020-02-12
7V68 ACM4 M4 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
iperoxo pubchem gtoplig chembl_ligand
PAMAgonist 3.4 Active 10.1038/S41467-022-30595-Y 2022-05-11
7WUI AGRG2 ADGRG2 ADGRG B2 (Adhesion) Mouse N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A IP15
Agonist 3.1 Active 10.1038/S41586-022-04590-8 2022-04-27
7XW5 TSHR TSH 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 Thyrotropin (TSH) (c...
Thyrotropin (TSH) (c...
ML-109 pubchem
AgonistAgonistAllosteric agonist 3.0 Active 10.1038/S41586-022-05173-3 2022-08-24
8JD0 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 chembl_ligand pubchem pubchem drugbank
CHEMBL3894759 chembl_ligand pubchem
AgonistNAM 3.3 Intermediate 10.1038/S41422-023-00830-2 2023-06-21
8IKL AGRE5 ADGRE5 ADGRE 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 N/A N/A 2.3 Active 10.1016/J.MOLCEL.2023.12.020 2024-01-24
8IC0 CXCR1 CXCR1 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
Agonist 3.4 Active 10.1038/S41467-023-39799-2 2023-07-19
8TAO 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
CDPPB pubchem gtoplig chembl_ligand
Nanobody 43
AgonistAgo-PAMPAM 2.9 Active 10.1101/2023.08.29.555158 2023-10-11
8UNQ 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 c-Epi pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06
6D32 SMOS smo.S Unclassified 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 cyclopamine pubchem gtoplig chembl_ligand
cyclopamine pubchem gtoplig chembl_ligand
AgonistAntagonist 3.8 Active 10.1016/J.CELL.2018.04.029 2018-05-23
9PA5 OPRM μ 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 ESKETAMINE chembl_ligand pubchem drugbank
Agonist (partial) 2.9 Active 10.1038/S41594-026-01839-Y 2026-07-01
9AS0 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 2-bromo-LSD pubchem gtoplig chembl_ligand
Agonist (partial) 3.4 Active 2025-04-02
9M1R OXGR1 oxoglutarate Oxoglutarate 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-ketoglutaric... pubchem gtoplig chembl_ligand drugbank
Agonist 2.7 Active 10.1038/S44318-026-00823-Y 2026-06-17
9L42 HRH4 H4 Histamine 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 histamine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 2.9 Active 10.3390/PH18030292 2025-10-22
9RKH 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 CHEMBL4633760 chembl_ligand pubchem
Inverse agonist 2.5 Inactive 2026-04-22
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
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 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 3.0 Active 10.1038/S41589-021-00890-8 2021-11-03
7EWP MGLYR MGLYR Metabotropic glycine 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 Regulator of G-prote...
NAM 4.3 Inactive 10.1038/S41467-021-27147-1 2021-12-01
8HOC HRH4 H4 Histamine 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 imetit pubchem gtoplig chembl_ligand pubchem
Agonist 3.0 Active 2023-12-20
9UWL V1AR V1A 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 CHEMBL395817 chembl_ligand pubchem
Antagonist 2.6 Inactive 2026-02-04
8ZH8 QRFPR QRFP QRFP 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 QRFP26
Agonist 3.2 Active 10.1038/S41467-024-49030-5 2024-07-03
9UAZ 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 CHEMBL1379091 chembl_ligand pubchem chembl_ligand pubchem chembl_ligand pubchem
Antagonist 3.3 Inactive 2025-10-29
8U4T CXCR4 CXCR4 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 REGN7663 Fab (chain ...
REGN7663 Fab (chain ...
Inverse agonistInverse agonist 3.4 Inactive 2024-03-13
8HS3 GPR20 GPR20 Orphan 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)
3.1 Active 10.1038/S41421-023-00520-8 2023-03-08
6OYA OPSD Rhodopsin Opsin (sight) 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 all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 3.3 Active 10.1016/J.MOLCEL.2019.06.007 2019-07-24
9IJR GPR52 GPR52 Orphan 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 derivative 17 [Nakah... pubchem gtoplig chembl_ligand
Agonist 3.9 Active 10.1038/S41422-025-01165-W 2025-09-03
6RZ9 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-2770372 pubchem
Antagonist 2.7 Active 10.1038/S41467-019-13348-2 2019-12-11
9L3Y CML2 chemerin 2 Chemerin receptor 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 Chemerin
Agonist 3.6 Active 10.1093/PROCEL/PWAE073 2025-03-12
7XTA 5HT4R 5-HT4 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 Active 10.1016/J.MOLCEL.2022.05.031 2022-07-27
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... pubchem
Agonist 3.5 Active 10.1126/SCIENCE.AAV7942 2019-04-17
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
7IPC 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 FU336-61 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 1.9 Inactive 2026-05-20
9WEY UL33 UL33 Unclassified A (Rhodopsin) strain AD169 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 3.3 Active 10.1038/S42003-026-09660-5 2026-02-25
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
9XC6 OPRM μ 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 (-)-methadone pubchem gtoplig chembl_ligand drugbank drug_central pubchem gtoplig chembl_ligand drug_central drugbank
BMS-986187 pubchem gtoplig chembl_ligand
AgonistAgo-PAM 3.0 Active 2026-07-08
8IY6 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-1 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 3.1 Active 10.7554/ELIFE.85821 2023-08-16
8P12 OPSD Rhodopsin Opsin (sight) 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)
3.2 Active 2024-11-20
8XQI 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 Apo (no ligand)
3.3 Inactive 10.1038/S41467-024-55555-6 2025-01-22
9CHU 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 (-)-noradrenaline pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Agonist 3.5 Inactive 10.1073/PNAS.2414544121 2024-11-13
9P89 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 NTS8–13 pubchem
Agonist 3.9 Active 10.1038/S41586-026-10120-7 2026-03-25
8HNN CXCR3 CXCR3 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 CHEMBL1921858 chembl_ligand pubchem
Allosteric antagonist 3.6 Inactive 10.1038/S41594-023-01175-5 2023-11-29
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
AgonistAgonist 3.0 Active 10.7554/ELIFE.68578 2021-09-22
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
8ZPL CXCR4 CXCR4 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 CHEMBL5172755 chembl_ligand pubchem
Antagonist 3.0 Inactive 2025-02-26
4LDL 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 hydroxybenzylisoprot... pubchem
Agonist 3.1 Active 10.1038/NATURE12572 2013-09-25
7TYO 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 gtoplig chembl_ligand uniprot drug_central pubchem
Agonist 2.7 Active 10.1126/SCIENCE.ABM9609 2022-03-23
7XP5 T2R46 TAS2R46 Taste 2 T2 (Taste 2) 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)
3.1 Active 2022-10-12
20ZH 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
Agonist 2.4 Active 10.1038/S41586-026-10228-W 2026-06-03
8IKJ AGRE5 ADGRE5 ADGRE 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 Apo (no ligand)
3.2 Inactive 10.1016/J.MOLCEL.2023.12.020 2024-02-14
9JKS HCAR3 HCA3 Hydroxycarboxylic 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 compound 6o [PMID: 1... pubchem gtoplig chembl_ligand
Agonist 3.3 Active 2025-10-29
8IOC MC3R MC3 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 γ-MSH (Human) pubchem gtoplig uniprot uniprot uniprot pubchem
Calcium pubchem
AgonistCofactor 2.9 Active 10.1107/S0907444909042073 2023-09-20
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
2VT4 ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 2 chemicals 2 steps vapour diffusionhanging drop 4 chems 6.9-7.3 18°C 4-{[(2S)-3-(tert-but... pubchem drugbank
Antagonist 2.7 Inactive 10.1038/NATURE07101 2008-06-24
8JLP TAAR1 TA1 Trace amine 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 ralmitaront pubchem gtoplig chembl_ligand
Agonist 3.2 Active 10.1038/S41586-023-06804-Z 2023-11-15
8YKX SUCR1 succinate Succinate 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 maleic acid pubchem gtoplig chembl_ligand drugbank
Agonist 2.7 Active 10.1038/S41422-024-00984-7 2024-05-29
7F23 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 dopamine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.6 Active 10.1126/SCIADV.ABO4158 2022-06-15
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 bosentan pubchem gtoplig chembl_ligand drugbank drug_central
Antagonist 3.6 Inactive 10.1038/NSMB.3450 2017-08-16
8HTI O52E4 OR52E4 Olfactory family 52 O1 (Olfactory/extra-nasal 1) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A OCTANOIC ACID chembl_ligand pubchem pubchem drugbank drug_central
Agonist 3.0 Active 10.1038/S41467-023-43983-9 2023-12-20
9PXY OPRM μ 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 naloxone pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem
Agonist (partial) 3.0 Active 2025-11-12
8GDB 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 PGE2 pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.1 Active 10.1073/PNAS.2216329120 2024-01-10
8K5D HCAR2 HCA2 Hydroxycarboxylic 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 GSK256073 pubchem gtoplig
Agonist 3.7 Active 10.1038/S41467-023-42764-8 2023-11-22
7IOY 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
FU210-12 pubchem
AntagonistUnknown 2.0 Inactive 2026-05-20
9EBQ 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 Peptide 2 (GLP-1 (AC...
Agonist 3.2 Active 10.1073/PNAS.2407574122 2025-03-26
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 pubchem drugbank drugbank chembl_ligand
Antagonist 2.0 Inactive 10.1016/j.str.2017.06.012 2017-07-26
8Z5H GPR68 GPR68 Proton 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)
3.3 Active 2025-04-23
8XUM LGR4 LGR4 Orphan 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-spondin-2
Agonist 2.9 Inactive 2025-01-15
7VOE 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 aripiprazole pubchem gtoplig chembl_ligand drugbank drug_central
Agonist (partial) 2.9 Inactive 10.1038/S41593-021-00971-W 2021-12-22
9ARY 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 3.3 Active 10.1038/S41467-025-57956-7 2025-04-02
8ZFD GPR4 GPR4 Proton 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 Apo (no ligand)
2.6 Active 10.1016/J.CELL.2024.12.001 2025-02-26
8YNF ACKR1 ACKR1 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 CXCL8 (IL-8)
Agonist 3.7 Intermediate 2025-09-17
7XJH ADRB3 β3 Adrenoceptors A (Rhodopsin) Dog N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A LEVISOPRENALINE chembl_ligand pubchem drug_central
Agonist 3.3 Active 10.1016/J.MOLCEL.2021.06.024 2022-05-04
6ZA8 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 CHEMBL463227 chembl_ligand pubchem chembl_ligand pubchem
Agonist (partial) 2.7 Intermediate 10.1126/sciadv.abe5504 2021-02-10
7QVM 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 (Human) pubchem gtoplig chembl_ligand drugbank drug_central uniprot uniprot uniprot
Agonist 3.3 Active 10.1038/S41467-022-31325-0 2022-08-10
9LRS MRGX4 MRGPRX4 Orphan 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 PSB-18061 pubchem
Agonist 2.8 Active 2026-02-04
8I9A C3AR C3a Complement peptide 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 EP54
Agonist 3.6 Active 10.1016/J.CELL.2023.09.020 2023-10-18
9OPX TS1R2 TAS1R2 Taste 1 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)
3.6 Inactive 10.1038/S41422-025-01156-X 2025-09-03
9CGJ 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 C6-Quino pubchem
Agonist (partial) 2.8 Active 2025-04-02
8IQ4 PF2R FP 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 Carboprost trometham... pubchem pubchem drugbank pubchem chembl_ligand chembl_ligand
Agonist 2.7 Active 10.1038/S41467-023-43922-8 2024-01-31
8YK0 GP156 GPR156 Orphan 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)
2.4 Active 10.1038/S41467-024-54681-5 2025-02-05
8PJK 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 ST171 pubchem
Phosphatidylinositol...
Agonist (partial)PAM 2.4 Active 2024-05-29
9IVM 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 LSN3318839 pubchem gtoplig chembl_ligand chembl_ligand pubchem
glucagon-like peptid... pubchem
PAMAgonist (partial) 3.2 Active 2024-11-13
8ID3 FFAR4 FFA4 Free fatty 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 9-Hydroxyoctadecanoi... pubchem
Agonist 3.1 Active 10.1126/SCIENCE.ADD6220 2023-03-15
8UWL 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 lisuride pubchem gtoplig chembl_ligand drugbank drug_central
Agonist (partial) 2.8 Active 10.1126/SCIENCE.ADN6354 2024-05-29
7F1Z 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 dopamine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.5 Active 10.1126/SCIADV.ABO4158 2022-06-15
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 (S)-carazolol pubchem drugbank
Inverse agonist 2.5 Inactive 10.1038/S41422-020-00424-2 2020-12-02
8XFP LGR4 LGR4 Orphan 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 Zinc ring finger 3
R-spondin-2
UnknownAgonist 3.2 Inactive 2024-12-04
7VIE 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
Agonist 2.9 Active 10.1073/PNAS.2117716119 2022-09-28
7XP4 T2R46 TAS2R46 Taste 2 T2 (Taste 2) 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)
3.0 Active 10.1126/SCIENCE.ABO1633 2022-10-12
8YN2 HRH1 H1 Histamine 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 histamine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 2.7 Active 10.1038/S41467-024-52585-Y 2024-10-09
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 (Human) pubchem gtoplig chembl_ligand drugbank drug_central uniprot uniprot uniprot pubchem
Agonist 4.2 Active 10.1126/SCIADV.ABG5628 2021-06-02
7BU7 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 CHEMBL1615159 chembl_ligand pubchem
Agonist 2.6 Active 10.1038/S41422-020-00424-2 2020-12-02
8HCQ EDNRA ETA 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-1 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 3.0 Active 2023-03-22
9MXU 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 Glucagon pubchem
Agonist 2.5 Active 2026-04-22
8IA7 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 CCK-8 (Human) pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank pubchem
Agonist 3.1 Active 10.1038/S41421-022-00420-3 2023-12-06
7RAN 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 CHEMBL5399968 chembl_ligand pubchem pubchem
Agonist (partial) 3.5 Active 10.1038/S41586-022-05258-Z 2022-07-06
8J46 O52E4 OR52E4 Olfactory family 52 O1 (Olfactory/extra-nasal 1) 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)
3.7 Inactive 10.1038/S41467-023-43983-9 2023-12-20
7XK8 NMUR2 NMU2 Neuromedin U 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 CHEMBL3315349 chembl_ligand pubchem
Agonist 3.3 Active 10.1038/S41467-022-34814-4 2023-02-22
8ITL 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 Apo (no ligand)
3.2 Active 10.1073/PNAS.2306145120 2023-10-18
8F7R OPRM μ 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 endomorphin-1 (Human... pubchem gtoplig chembl_ligand
Agonist 3.3 Active 10.1016/J.CELL.2022.12.026 2022-12-14
8X0G 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
Agonist 3.0 Active 10.1038/S41467-024-55439-9 2024-11-06
8HDO AA2BR A2B 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 BAY 60-6583 pubchem gtoplig chembl_ligand
Agonist 2.9 Active 10.1038/S41421-022-00503-1 2023-01-18
9X3Z MAS MAS1 Orphan 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 neuropeptide FF (Hum... pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 2.5 Active 10.1038/S44318-026-00764-6 2026-04-15
9ODE OPRM μ Opioid 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 LOFENTANIL chembl_ligand pubchem drugbank
Agonist 2.5 Active 10.1038/S41586-025-10056-4 2026-03-04
9O36 OPRM μ Opioid 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 Fluornitrazene pubchem
Agonist 2.3 Active 2026-04-01
7PP1 P2Y12 P2Y12 P2Y 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 selatogrel pubchem pubchem gtoplig chembl_ligand drugbank
Inverse agonist 2.8 Active 10.1016/j.bcp.2022.115291 2022-11-02
9L0H C3AR C3a Complement peptide 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 JR14a pubchem gtoplig chembl_ligand
Agonist 3.6 Active 2025-11-26
9QD4 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 cp30a pubchem
Agonist 3.1 Inactive 2026-02-11
9AS6 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 mescaline pubchem gtoplig chembl_ligand
Agonist 3.1 Active 2025-04-02
8Y62 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 C16:0 ceramide pubchem
Agonist (partial) 3.2 Active 10.1126/SCIENCE.ADO4188 2025-02-05
9UWV OPRK κ 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 salvinorin A pubchem gtoplig chembl_ligand chembl_ligand pubchem chembl_ligand pubchem chembl_ligand pubchem drugbank
Agonist 3.3 Active 2026-05-27
9BLC 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 Cagrilintide backbon...
Agonist 3.3 Active 10.1038/S41467-025-58680-Y 2025-04-16
9VNF 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 (-)-pindolol pubchem gtoplig chembl_ligand
Agonist (partial) 2.7 Active 2025-11-12
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 Non-acylated tirzepa...
Agonist 3.0 Active 10.1038/S41467-022-28683-0 2022-03-02
8GG7 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 c-Epi pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06
6KPC CNR2 CB2 Cannabinoid 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 AM12033 pubchem
Agonist 3.2 Inactive 10.1016/J.CELL.2020.01.008 2020-02-12
9KDF 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 RES-701-3
Inverse agonist 3.3 Inactive 10.1038/S41467-025-57960-X 2025-05-07
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
8K2W CXCR3 CXCR3 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 CHEMBL397983 chembl_ligand pubchem
Antagonist 3.0 Inactive 10.1038/S41421-023-00617-0 2023-11-29
8IED GP156 GPR156 Orphan 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 PC 34:1 pubchem
Agonist 3.3 Active 2024-02-14
9X41 MAS MAS1 Orphan 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 AR234958 pubchem
Agonist 3.3 Intermediate 2026-05-20
9V82 MRGX4 MRGPRX4 Orphan 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 HEP-50768 gtoplig pubchem
Inverse agonist 2.6 Active 2026-05-06
9BUE 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 cagrilintide pubchem gtoplig drugbank
Agonist 3.6 Active 10.1038/S41467-025-58680-Y 2025-04-16
7IO5 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 FU12-45 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 1.8 Inactive 2026-05-20
6TP4 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 ACT-462206 pubchem gtoplig chembl_ligand chembl_ligand pubchem
Antagonist 3.0 Inactive 10.1021/acs.jmedchem.9b01787 2020-01-01
8J6L HCAR2 HCA2 Hydroxycarboxylic 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 nicotinic acid pubchem gtoplig chembl_ligand drugbank drug_central drugbank drugbank
Agonist 3.1 Active 10.1016/J.CELREP.2023.113406 2024-04-03
8E3X 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 PACAP-27 (Human) pubchem gtoplig uniprot uniprot uniprot uniprot pubchem
Agonist 2.3 Active 10.1038/S41467-022-34629-3 2022-11-23
8X79 PI2R IP 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 MRE-269 pubchem gtoplig chembl_ligand
Agonist 2.4 Active 2024-03-06
8FLQ 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 PTH pubchem
Agonist 2.6 Active 10.1016/J.STR.2023.04.002 2023-04-26
9R41 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 buspirone pubchem gtoplig chembl_ligand drugbank drug_central
Agonist (partial) 3.8 Active 2026-05-20
9N1P 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 SRB103H
Agonist 2.9 Active 2026-04-22
9BLW 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 Cagrilintide backbon...
Agonist 3.2 Active 10.1038/S41467-025-58680-Y 2025-04-16
9MM5 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 dC2_049
Unknown 3.3 Inactive 10.1038/S41586-026-10656-8 2026-01-28
9XQN GPR75 GPR75 Orphan 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)
3.9 Active 10.1038/S41401-025-01720-6 2026-02-04
9CLW FFAR2 FFA2 Free fatty 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 CHEMBL4176503 chembl_ligand pubchem
AMG7703 pubchem gtoplig chembl_ligand chembl_ligand pubchem
AgonistAgo-PAM 3.2 Active 2025-06-25
9U4J GPR4 GPR4 Proton 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)
3.4 Active 2026-03-25
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
8GGX 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 c-Epi pubchem
Agonist 3.6 Active 10.1038/S41586-024-07153-1 2024-03-06
7SK5 ACKR3 ACKR3 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 CXCL12
Agonist 4.0 Active 10.1126/SCIADV.ABN8063 2022-07-27
9M42 GP139 GPR139 Orphan 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 1.1(S) pubchem
Agonist 3.2 Active 2026-01-21
6PS5 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 (-)-propranolol pubchem gtoplig chembl_ligand drugbank pubchem gtoplig chembl_ligand drug_central
Inverse agonist 2.9 Inactive 10.1107/S2052252519013137 2019-11-13
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 LEVISOPRENALINE chembl_ligand pubchem drug_central
Agonist 2.8 Active 10.1126/SCIENCE.AAU5595 2018-10-17
8X5Y HRH1 H1 Histamine 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 astemizole pubchem gtoplig chembl_ligand drugbank drug_central
Inverse agonist 3.0 Inactive 10.1038/S41467-023-44477-4 2024-01-17
8GAG CNR1 CB1 Cannabinoid 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 methyl (2R)-2-({(1M)... pubchem
Agonist 3.3 Active 2024-02-28
9J5V 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 CpY pubchem gtoplig
Agonist 2.9 Active 2024-11-27
8X3L CNR2 CB2 Cannabinoid 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 CHEMBL5422946 chembl_ligand pubchem
Agonist 3.1 Active 10.1073/PNAS.2401091121 2024-11-20
7VL9 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 CCL15(26-92)
Agonist 2.6 Active 10.1038/S41589-021-00918-Z 2022-03-23
9U80 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 conivaptan pubchem gtoplig chembl_ligand drugbank drug_central
Antagonist 2.9 Inactive 2025-12-10
5NX2 GLP1R GLP-1 Glucagon B1 (Secretin) Human BaculovirusSf9Insect 2 chemicals 2 steps vapour diffusionSitting drop 4 chems 8.0-9.0 10°C Peptide 5
Agonist 3.7 Intermediate 10.1038/NATURE22800 2017-06-14
8X9T AGRD1 ADGRD1 ADGRD 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 AP503 pubchem
Agonist 2.8 Active 10.1016/J.CELL.2025.01.006 2025-02-12
9BUY 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 LM189 pubchem
compound-6FA pubchem
AgonistPAM 2.9 Active 2025-05-28
4ZJC OX1R OX1 Orexin A (Rhodopsin) Human BaculovirusSf9Insect 6 chemicals 6 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 5.6-5.6 20°C SB-674042 pubchem gtoplig chembl_ligand
Antagonist 2.8 Inactive 10.1038/NSMB.3183 2016-03-09
8K8J CNR1 CB1 Cannabinoid 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 FENOFIBRATE chembl_ligand pubchem drugbank drug_central
Agonist (partial) 2.9 Active 10.1002/ADVS.202306311 2024-02-14
7YIT OPRK κ 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 nalfurafine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.3 Active 10.1038/S41467-023-37041-7 2023-04-12
9W33 SSR5 SST5 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 S5A1 pubchem gtoplig
Antagonist 2.7 Inactive 2026-01-21
9IK8 SSR1 SST1 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 pasireotide pubchem gtoplig drugbank chembl_ligand drug_central
Agonist 2.8 Active 2025-04-30
9V0U AGRD1 ADGRD1 ADGRD 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 N/A N/A 3.5 Active 10.1016/J.BBRC.2025.152165 2025-07-30
7F1O 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 dopamine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.1 Active 10.1126/SCIADV.ABO4158 2022-06-15
9GYO 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 CHEMBL2331646 chembl_ligand pubchem
Agonist 2.5 Active 2024-10-09
7VOD 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 cariprazine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist (partial) 3.3 Inactive 10.1038/S41593-021-00971-W 2021-12-22
8XOH GPER1 GPER Estrogen (G protein-coupled) 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)
3.2 Active 10.1038/S41422-024-00963-Y 2024-04-10
9IQR 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 muscarinic toxin 3 gtoplig uniprot
Antagonist 3.4 Inactive 10.1038/S41467-025-61695-0 2025-07-23
7EWL MGLYR MGLYR Metabotropic glycine 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)
3.5 Inactive 10.1038/S41467-021-27147-1 2021-12-01
6PB0 CRHR1 CRF1 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
Cholesterol pubchem drugbank
AgonistCofactor 3.0 Active 10.1016/J.MOLCEL.2020.01.013 2020-02-12
9M40 Q5QNP8 taar13e Unclassified A (Rhodopsin) Zebrafish N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Agmatine pubchem drugbank
Agonist 2.7 Active 2026-03-11
9ODL OPRM μ Opioid 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 Mitragynine pseudoin...
Agonist (partial) 3.6 Active 10.1038/S41586-025-10056-4 2026-01-07
9EBO 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 (ACPC18)
Agonist 3.1 Active 10.1073/PNAS.2407574122 2025-03-26
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 chembl_ligand pubchem
Antagonist 2.8 Inactive 10.1126/SCIENCE.1215904 2012-02-15
9K3K 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 Apo (no ligand)
3.1 Active 10.1016/J.STR.2025.03.004 2025-08-06
7UL2 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 meclinertant pubchem gtoplig chembl_ligand drugbank
Na+ pubchem
Inverse agonistNAM 2.4 Intermediate 10.1038/S41594-022-00859-8 2022-06-29
8TRC GRM3 mGlu3 Metabotropic glutamate C (Glutamate) Rat 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
Antagonist 3.3 Inactive 10.1101/2023.08.13.552748 2024-07-31
6PS8 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 CHEMBL15060 chembl_ligand pubchem
Agonist 3.3 Inactive 10.1107/S2052252519013137 2019-11-13
8A6C OPSD Rhodopsin Opsin (sight) 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 all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 1.8 Inactive 10.1038/S41586-023-05863-6 2023-03-29
9PU5 OPRM μ 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 DAMGO pubchem gtoplig chembl_ligand pubchem
BMS-986187 pubchem gtoplig chembl_ligand
AgonistPAM 3.5 Active 2026-05-27
9K3H MC5R MC5 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 Apo (no ligand)
2.9 Active 10.1016/J.STR.2025.03.004 2025-08-06
9DYE 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 PtdIns4P pubchem
buspirone pubchem gtoplig chembl_ligand drugbank drug_central
PAMAgonist 2.9 Active 10.1126/SCIADV.ADU9851 2025-08-13
8XQF 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 apelin-13 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 3.1 Active 10.1038/S41467-024-55555-6 2025-01-22
8IYH HCAR2 HCA2 Hydroxycarboxylic 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 MK 6892 pubchem gtoplig chembl_ligand pubchem
Agonist 3.3 Active 10.1038/S41467-024-46239-2 2024-03-06
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 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot drugbank
Agonist 2.9 Active 10.1038/S41594-021-00645-Y 2021-10-13
9VAY 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
Agonist 3.7 Active 10.1038/S41586-026-10228-W 2026-06-03
9IQV ADA1A α1A 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 muscarinic toxin 3 gtoplig uniprot
Antagonist 3.3 Inactive 10.1038/S41467-025-61695-0 2025-07-23
9LL8 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 2.6 Active 10.1038/S41586-025-10061-7 2026-01-14
9NOX TS1R2 TAS1R2 Taste 1 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)
3.0 Active 10.1016/J.CELL.2025.04.021 2025-05-14
7CA3 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 rac-BHFF pubchem
PAM 4.5 Active 10.1016/J.JMB.2020.09.023 2020-11-11
9ISI C3AR C3a Complement peptide 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)
3.6 Inactive 10.1038/S44318-025-00429-W 2025-04-23
9N04 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 Peptide 15
Agonist 2.3 Active 2026-04-22
9BQ3 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 cagrilintide pubchem gtoplig drugbank
Agonist 2.8 Active 2025-04-23
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 CHEMBL1615159 chembl_ligand pubchem
Agonist 3.2 Active 10.1038/NATURE10361 2011-07-20
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 METHSCOPOLAMINE chembl_ligand pubchem pubchem drugbank drugbank drug_central chembl_ligand
Inverse agonist 2.5 Inactive 10.1038/S41589-018-0152-Y 2018-11-21
7XT9 5HT4R 5-HT4 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 Active 10.1016/J.MOLCEL.2022.05.031 2022-07-27
9UMJ C3AR C3a Complement peptide 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 EP54
Agonist 3.4 Active 10.1101/2025.05.26.656101 2025-11-26
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)
3.2 Intermediate 10.1126/sciadv.abe5504 2021-02-10
9P86 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 NTS8–13 pubchem
Agonist 2.9 Active 10.1038/S41586-026-10120-7 2026-03-25
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-1 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 2.8 Inactive 10.1038/nature19319 2016-09-07
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 SKF-83959 pubchem gtoplig chembl_ligand chembl_ligand pubchem pubchem
Agonist 3.3 Active 10.1016/J.CELL.2021.01.028 2021-03-03
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 Active 10.1038/NATURE22309 2017-05-03
6HLP 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 netupitant pubchem gtoplig chembl_ligand drug_central drugbank
Antagonist 2.2 Inactive 10.1038/S41467-018-07939-8 2019-01-16
7WXW AGRF1 ADGRF1 ADGRF 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 Apo (no ligand)
2.8 Active 10.1038/S41467-022-33173-4 2022-09-28
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 CHEMBL407774 chembl_ligand
Agonist 3.5 Inactive 10.1126/SCIENCE.ABF7258 2021-02-24
9UYN CML2 chemerin 2 Chemerin receptor 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 Palmitoleic Acid pubchem drugbank
Allosteric agonist 2.9 Active 10.1126/SCIENCE.ADT8794 2025-11-19
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 gtoplig chembl_ligand
Agonist 3.1 Active 10.1038/S41422-021-00567-W 2021-09-29
9PPY 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 Met-enkephalin
Agonist 3.1 Active 10.1126/SCIADV.AEB6737 2026-03-04
7U2K OPRM μ Opioid 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 CHEMBL147044 chembl_ligand pubchem
Agonist 3.3 Active 10.1038/S41586-022-05588-Y 2022-12-07
8W88 TAAR1 TA1 Trace amine 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 ulotaront pubchem gtoplig chembl_ligand drugbank
Agonist 2.6 Active 10.1038/S41586-023-06775-1 2023-11-22
7M3G 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 etelcalcetide pubchem gtoplig chembl_ligand drugbank drug_central
evocalcet pubchem gtoplig drug_central chembl_ligand drugbank
Calcium pubchem
D-tryptophan pubchem gtoplig chembl_ligand drugbank pubchem gtoplig chembl_ligand drugbank drug_central
PAMPAMAgonistPAM 2.5 Active 10.1038/S41586-021-03691-0 2021-06-30
8JWZ 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 AB928 pubchem gtoplig chembl_ligand
Antagonist 2.4 Inactive 2023-08-16
8IA2 C5AR1 C5a1 Complement peptide 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 [<sup>125</sup>I]C5a... gtoplig
Agonist 3.2 Active 10.1016/J.CELL.2023.09.020 2023-10-18
8WWL MCHR1 MCH1 Melanin-concentrating 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 melanin-concentratin... pubchem gtoplig uniprot uniprot uniprot
Agonist 2.8 Active 10.1038/S41421-024-00754-0 2024-11-13
7YDP AGRE5 ADGRE5 ADGRE 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 N/A N/A 3.1 Active 10.1016/J.CHEMBIOL.2023.08.003 2023-07-12
8ID6 FFAR4 FFA4 Free fatty 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 oleic acid pubchem gtoplig chembl_ligand drug_central pubchem drugbank
Agonist 2.8 Active 10.1126/SCIENCE.ADD6220 2023-03-15
9UAP 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 Apo (no ligand)
3.6 Active 10.1073/PNAS.2508879122 2025-10-29
9IBW OPSB OPN1SW Opsin (sight) 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 all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Inverse agonist 3.2 Inactive 10.1126/SCIENCE.ADZ3624 2026-06-24
7TS0 CRHR2 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 10.1038/S41467-022-33851-3 2022-11-09
7IN7 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 Apo (no ligand)
2.4 Inactive 10.1038/S42004-026-02059-7 2026-05-20
9U4Y Q90WJ2 GnRH1 Gonadotrophin-releasing hormone A (Rhodopsin) African clawed frog N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL266314 chembl_ligand pubchem pubchem drugbank pubchem chembl_ligand
Agonist 2.7 Active 10.1073/PNAS.2500112122 2025-06-11
2YDV AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusHi5Insect 4 chemicals 4 steps vapour diffusionsitting drop 5 chems 6.4-6.4 4°C NECA pubchem gtoplig chembl_ligand
Agonist 2.6 Active 10.1038/NATURE10136 2011-05-18
9PQ0 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 ADL5859 pubchem gtoplig chembl_ligand
Agonist 3.1 Active 2026-03-04
4X1H OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionsitting drop 3 chems 5.0-6.5 4°C Apo (no ligand)
2.3 Active 10.1016/J.STR.2015.09.015 2015-11-04
8DPH 5HT2C 5-HT2C 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 lorcaserin pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.2 Active 10.1016/J.CELREP.2022.111211 2022-08-24
9YFU GPR61 GPR61 Orphan 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 GPR61 inverse agonis... gtoplig pubchem
Inverse agonist 3.1 Active 2026-03-25
3QAK AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 5.0-5.5 20°C UK-432,097 pubchem gtoplig chembl_ligand drugbank
Agonist 2.7 Active 10.1126/SCIENCE.1202793 2011-03-09
7UM6 5HT5A 5-HT5A 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
Agonist (partial) 2.8 Active 10.1038/S41594-022-00796-6 2022-07-20
8GD9 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 Rivenprost pubchem
Agonist 3.2 Active 10.1073/PNAS.2216329120 2024-01-10
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
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 (S)-carazolol pubchem drugbank
Nanobody 60
Inverse agonistNAM 3.2 Inactive 10.1038/NATURE18636 2016-07-13
8K2X CXCR3 CXCR3 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 C-X-C motif chemokin...
Agonist 3.2 Active 10.1038/S41421-023-00617-0 2023-11-29
9ECJ P2RY8 P2RY8 Orphan 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-geranylgeranyl-L-g... pubchem
Agonist 2.9 Active 2025-11-05
9BS9 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 (+)-LSD pubchem gtoplig pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.3 Active 10.1016/J.NEURON.2025.06.012 2025-09-17
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 chembl_ligand
Agonist 3.0 Active 10.1038/S41467-021-21087-6 2021-02-10
7INN 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 N-(4-chlorophenyl)th... pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.3 Inactive 2026-05-20
9LZ0 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... pubchem
Agonist 3.8 Active 2026-03-18
8J20 FFAR3 FFA3 Free fatty 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 pentanoic acid pubchem gtoplig chembl_ligand drugbank chembl_ligand pubchem
AR420626 pubchem
AgonistPAM 3.2 Active 10.1038/S41422-023-00914-Z 2024-01-24
8TH4 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 losartan pubchem gtoplig chembl_ligand drugbank drug_central
AT118-L Nanobody
AntagonistAntagonist 3.3 Inactive 10.1038/S41589-024-01620-6 2024-05-22
7INY 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
FU2-59 pubchem
AntagonistUnknown 2.4 Inactive 2026-05-20
7Y65 C5AR1 C5a1 Complement peptide 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 C5aPEP
Agonist 3.2 Active 10.1038/S41422-023-00779-2 2023-03-01
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...
Antagonist 3.2 Inactive 10.1126/SCIADV.AAX7379 2020-01-29
8EA0 ACM3 M3 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
Agonist 2.6 Active 10.1038/S41586-022-05489-0 2022-11-30
8WCC TAAR1 TA1 Trace amine 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 Cyclohexylammonium I... pubchem drugbank pubchem drugbank
Agonist 3.0 Active 10.1016/J.CELL.2023.10.014 2023-12-27
4AMJ ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 2 chemicals 2 steps vapour diffusionsitting drops 3 chems 9.0-9.0 4°C CHEMBL3799125 chembl_ligand pubchem
Inverse agonist 2.3 Inactive 10.1016/J.STR.2012.03.014 2012-05-23
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 Apo (no ligand)
3.3 Inactive 10.1038/nature12393 2013-07-24
9C2F 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 D-tryptophan pubchem gtoplig chembl_ligand drugbank pubchem gtoplig chembl_ligand drugbank drug_central
'54149 pubchem
Calcium pubchem
AgonistPAMAgonist 2.8 Active 2024-10-02
9B65 CNR1 CB1 Cannabinoid 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 MDMB-Fubinaca pubchem gtoplig
Agonist 3.0 Active 10.1038/S41586-025-08618-7 2025-03-05
8JR9 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 PCO371 pubchem gtoplig chembl_ligand drugbank
Agonist 2.6 Active 10.1038/S41586-023-06467-W 2023-08-02
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 LPA pubchem
Agonist 2.8 Active 10.1038/S41467-022-28417-2 2022-02-09
8XVJ EDNRA ETA 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 macitentan pubchem gtoplig chembl_ligand drugbank drug_central
Antagonist 3.3 Inactive 2024-08-28
7INB 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 4-methoxybenzamide pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.1 Inactive 10.1038/S42004-026-02059-7 2026-05-20
9JVG GPR4 GPR4 Proton 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 Apo (no ligand)
2.8 Active 10.1016/J.CELL.2024.12.001 2025-02-26
8JIP 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-hexadecanoyl-L-glu... pubchem
COTADUTIDE chembl_ligand drugbank pubchem
AgonistAgonist 2.9 Active 10.1073/PNAS.2303696120 2023-09-06
3PQR OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drops 3 chems 5.6-5.6 4°C all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 2.9 Active 10.1038/NATURE09789 2011-03-09
8YW4 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 retatrutide pubchem gtoplig
Agonist 3.3 Active 10.1038/S41421-024-00700-0 2024-09-18
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 Chorionic gonadotrop...
Chorionic gonadotrop...
AgonistAgonist 4.3 Active 10.1038/S41586-021-03924-2 2021-09-29
9J8Z HCAR1 HCA1 Hydroxycarboxylic 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 Apo (no ligand)
3.4 Active 10.1371/JOURNAL.PBIO.3003126 2025-04-02
8IA8 C3AR C3a Complement peptide 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 E7 pubchem gtoplig gtoplig
Agonist 2.9 Active 2023-05-24
7F8U 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 lintitript pubchem gtoplig chembl_ligand drugbank
Antagonist 2.8 Inactive 10.1038/S41589-021-00866-8 2021-10-13
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)
3.2 Inactive 10.1126/SCIENCE.ABF7258 2021-02-24
4J4Q OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drop 3 chems 5.2-6.0 4°C Apo (no ligand)
2.7 Active 10.1002/ANIE.201302374 2013-10-30
8EFL OPRM μ 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 CHEMBL4452384 chembl_ligand pubchem
Agonist (partial) 3.2 Active 10.1016/J.CELL.2022.09.041 2022-11-09
9KX6 C5AR1 C5a1 Complement peptide 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 C5a des-Arg (Human) gtoplig
Agonist 3.1 Active 10.1101/2025.05.26.656101 2025-11-26
9UYQ GRM6 mGlu6 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
Agonist 3.3 Active 2026-03-18
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
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 23H
Agonist 3.9 Active 10.1038/S41392-020-00262-Z 2020-09-02
6ME9 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 3.3 Inactive 10.1038/S41586-019-1144-0 2019-04-24
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 HTL-9936 chembl_ligand pubchem
Agonist (partial) 2.3 Inactive 10.1016/J.CELL.2021.11.001 2021-10-06
8GEG 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 c-Epi pubchem
Agonist 3.8 Active 10.1038/S41586-024-07153-1 2024-03-06
8YN8 HRH3 H3 Histamine 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 proxyfan pubchem gtoplig chembl_ligand
Agonist 2.8 Active 2024-10-16
8U4P CXCR4 CXCR4 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 plerixafor pubchem gtoplig chembl_ligand drugbank drug_central
Agonist (partial) 3.2 Active 10.1038/S41594-024-01397-1 2024-03-13
9PXV OPRM μ 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 naloxone pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem
Agonist (partial) 3.0 Active 2025-11-12
7INX 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 FU2-57 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.3 Inactive 2026-05-20
20ZI 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
Agonist 2.7 Active 10.1038/S41586-026-10228-W 2026-06-03
7XOV 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 SR146131 pubchem gtoplig chembl_ligand
Agonist 3.0 Active 10.1038/S41421-022-00420-3 2022-07-20
8JCW 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
Antagonist 3.0 Inactive 10.1038/S41422-023-00830-2 2023-06-21
8XJN 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 cloprostenol pubchem gtoplig chembl_ligand drugbank
Agonist 3.1 Active 2024-02-28
8JGB MRGX1 MRGPRX1 Orphan 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 Conorfamide-Tx2
Agonist 2.8 Active 10.1038/S41467-023-40705-Z 2024-01-10
8XZH 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 MM07 pubchem gtoplig chembl_ligand
Agonist 2.6 Active 10.1016/J.CELL.2024.02.004 2024-03-20
7SK3 ACKR3 ACKR3 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 [<sup>125</sup>I]CXC... gtoplig
Agonist 3.8 Active 10.1126/SCIADV.ABN8063 2022-07-27
4BEY OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine Stable_cellsHEK293S(TetR)GnTI-Mammalian 1 chemicals 1 steps vapour diffusionsitting drop 4 chems 4.5-4.5 20°C Apo (no ligand)
2.9 Active 10.1038/EMBOR.2013.44 2013-05-08
8XX7 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 CXCL5
Agonist 3.3 Active 10.1016/J.MOLCEL.2025.01.024 2025-01-15
9K0K P2RY4 P2Y4 P2Y 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 UTP pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.1 Active 10.1038/S41421-025-00797-X 2025-06-11
7Y1F OPRK κ 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 Dynorphin A13 pubchem
Agonist 3.3 Active 10.1093/PROCEL/PWAC033 2023-05-24
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 (partial) 2.5 Active 10.1101/436212 2018-10-17
6XBJ SMO SMO Oxysterol 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 drugbank
Agonist 3.9 Active 10.1038/S41589-020-0646-2 2020-09-30
9AS1 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 dimethyltryptamine pubchem gtoplig chembl_ligand drugbank
Agonist 3.4 Active 2025-04-02
7MT8 OPSD Rhodopsin Opsin (sight) 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 all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 5.8 Active 10.1038/S41586-021-03721-X 2021-07-07
9X40 MAS MAS1 Orphan 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 AR234958 pubchem
Agonist 3.1 Active 2026-05-20
20ZK 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
Agonist 2.7 Active 10.1038/S41586-026-10228-W 2026-06-03
7XA3 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 C-C motif chemokine ...
Agonist 2.9 Active 10.1038/S41421-022-00403-4 2022-08-24
7IOZ 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 FU223-7 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 1.9 Inactive 2026-05-20
8A6E OPSD Rhodopsin Opsin (sight) 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 all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 1.8 Inactive 10.1038/S41586-023-05863-6 2023-03-29
8GW8 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 PCO371 pubchem gtoplig chembl_ligand drugbank
Agonist 2.9 Active 10.1038/S41586-023-06169-3 2023-06-14
8UNL 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 c-Epi pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06
5TE3 OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drop 4 chems 5.2-6.6 4°C Apo (no ligand)
2.7 Active 10.1073/PNAS.1617446114 2017-03-15
8YN5 HRH3 H3 Histamine 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 histamine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 2.7 Active 10.1038/S41467-024-52585-Y 2024-10-09
8YFS A0A9L0JPP9 MRGPRE Orphan A (Rhodopsin) Donkey N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (E)-3-(2-methoxyphen... pubchem
Agonist 2.8 Active 2025-03-05
7WC7 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 lisuride pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.6 Inactive 10.1126/SCIENCE.ABL8615 2022-01-26
7X9Y CCR3 CCR3 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)
3.1 Active 10.1038/S41421-022-00403-4 2022-08-24
6FUF OPSD Rhodopsin Opsin (sight) 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 all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 3.1 Active 10.1126/SCIADV.AAT7052 2018-10-03
7YU7 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 ONO-0740556 pubchem
Agonist 3.8 Active 10.1038/S41467-022-33121-2 2022-10-05
7XKA 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 c-Epi pubchem
Agonist 3.1 Active 2023-04-26
8Y52 BRS3 BB3 Bombesin 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 BA1
Agonist 2.9 Active 10.1016/J.CELREP.2024.114511 2024-09-11
8WG8 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 Unknown peptide (Cha...
Unknown 2.7 Active 10.1038/S41421-024-00649-0 2024-03-06
8F2A 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 San385
Agonist 2.2 Active 10.1038/S41589-023-01393-4 2023-08-02
9LYD GPR3 GPR3 Orphan 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)
3.7 Active 10.1016/J.CELREP.2025.115478 2025-04-09
7IOC 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
FU18-82 pubchem
AntagonistUnknown 2.1 Inactive 2026-05-20
7IOF 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 FU99-31 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 1.9 Inactive 2026-05-20
8XXZ CXCR3 CXCR3 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)
3.3 Active 10.1038/S41467-025-58264-W 2025-02-26
8GGW 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 c-Epi pubchem
Agonist 3.6 Active 10.1038/S41586-024-07153-1 2024-03-06
7VDM MRGX2 MRGPRX2 Orphan 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 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 3.0 Active 10.1038/S41586-021-04077-Y 2021-12-01
8RWI 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 StilSwitch2 pubchem
Antagonist 2.8 Inactive 2025-01-08
7EJK 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 oxymetazoline pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.4 Active 10.1126/SCIADV.ABJ5347 2022-04-13
8FCZ OPSD Rhodopsin Opsin (sight) 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 all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Nanobody Nb2
Inverse agonistAllosteric antagonist 3.7 Inactive 10.1038/S41467-023-40911-9 2023-08-30
8DWH MRGX1 MRGPRX1 Orphan 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 16 [PMID: 3... pubchem gtoplig chembl_ligand
Agonist 3.3 Active 10.1038/S41589-022-01173-6 2022-11-02
7EPD 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)
3.9 Inactive 10.1038/S41586-021-03641-W 2021-06-23
7YU3 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 ONO-0740556 pubchem
Agonist 3.4 Active 10.1038/S41467-022-33121-2 2022-10-05
9LQZ 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 azelaprag pubchem gtoplig chembl_ligand chembl_ligand pubchem
Agonist 2.6 Inactive 2026-02-04
7T2H OPRM μ Opioid 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 LOFENTANIL chembl_ligand pubchem drugbank
Agonist 3.2 Active 10.1038/S41589-022-01208-Y 2022-12-07
9UAN 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 LTD4 pubchem gtoplig chembl_ligand chembl_ligand pubchem drugbank
Agonist 3.5 Active 2026-03-18
9LFD 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 WIN 64338 pubchem gtoplig chembl_ligand chembl_ligand chembl_ligand pubchem pubchem pubchem
Antagonist 3.6 Inactive 2026-05-27
7SK4 ACKR3 ACKR3 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 CXCL12_LRHQ
Agonist 3.3 Active 10.1126/SCIADV.ABN8063 2022-07-27
9W49 OPRK κ 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 U50488 pubchem gtoplig chembl_ligand
Agonist 2.9 Active 2025-11-19
11TL CCR4 CCR4 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 GSK2239633A pubchem gtoplig chembl_ligand
Antagonist 3.9 Inactive 2026-04-01
8UNN 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 c-Epi pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
8HQE GP132 GPR132 Proton 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)
3.0 Active 10.1038/S42255-023-00899-4 2023-10-11
8JBG NK3R NK3 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 neurokinin B (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot uniprot
Agonist 2.8 Active 2024-02-07
9M3Q TA13C taar13c Orphan A (Rhodopsin) Zebrafish N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A SPERMIDINE chembl_ligand pubchem drugbank
Agonist 2.7 Active 2026-03-11
8JHC FZD3 FZD3 WNT 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)
3.3 Active 10.1038/S41421-023-00627-Y 2024-01-17
8CU7 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 LJ-4517 pubchem gtoplig chembl_ligand
Antagonist 2.1 Inactive 10.1021/acs.jmedchem.2c00462 2022-08-31
9WIK GPR84 GPR84 Orphan 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 DL-175 pubchem gtoplig chembl_ligand
Agonist 3.3 Active 2026-07-01
9EE8 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 adenosine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.6 Active 10.1038/S41467-025-56434-4 2025-04-09
7FEE CNR1 CB1 Cannabinoid 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 ZCZ011 pubchem
CP55940 pubchem gtoplig chembl_ligand
Ago-PAMAgonist 2.7 Inactive 10.1038/S41589-022-01038-Y 2022-06-15
7WY8 AGRL3 ADGRL3 ADGRL B2 (Adhesion) Mouse 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 Active 10.1016/J.MOLCEL.2022.10.009 2022-10-26
9LLE 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 dopamine pubchem gtoplig chembl_ligand drugbank drug_central
GEM targeting TM1/2/...
AgonistAllosteric agonist 2.9 Active 2026-03-04
6FK8 OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine BaculovirusHEK293S(TetR)-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 4.5-4.5 20°C RS08 pubchem
Agonist 2.9 Active 10.1073/PNAS.1718084115 2018-04-04
7VUG GP139 GPR139 Orphan 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
8YRQ PAR4 PAR4 Proteinase-activated 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 Active 2026-06-10
8FY8 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 5-MeO-DMT pubchem gtoplig chembl_ligand drugbank
Agonist 2.8 Active 10.1038/S41586-024-07403-2 2024-05-15
7L0S 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 NTS8–13 pubchem
Agonist 4.5 Active 10.1038/S41594-020-00554-6 2021-01-06
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 iperoxo pubchem gtoplig chembl_ligand
LY2119620 pubchem gtoplig chembl_ligand
AgonistPAM 4.0 Active 10.1038/S41586-020-1954-0 2020-02-26
8J24 FFAR2 FFA2 Free fatty 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 acetic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank pubchem drugbank pubchem drugbank pubchem drugbank drugbank drugbank drugbank drugbank drugbank drugbank pubchem
Agonist 2.6 Active 10.1038/S41422-023-00914-Z 2024-01-24
9P80 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 NTS8–13 pubchem
Agonist 2.3 Active 10.1038/S41586-026-10120-7 2026-03-25
7XZ5 GP119 GPR119 GPR18, GPR55 and GPR119 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 Lysophosphatidylchol... pubchem
Agonist 3.1 Active 10.1038/S41594-022-00816-5 2022-08-24
8ID9 FFAR4 FFA4 Free fatty 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 EPA pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.0 Active 10.1126/SCIENCE.ADD6220 2023-03-15
8ZFB GPR4 GPR4 Proton A (Rhodopsin) Western clawed frog 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)
3.8 Active 10.1016/J.CELL.2024.12.001 2025-02-26
8IRJ GP179 GPR179 Orphan 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)
3.5 Inactive 2024-09-18
8GCM 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 L902688 pubchem
Agonist 3.5 Active 10.1073/PNAS.2216329120 2024-01-03
3OE8 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
7SHF MGLYR MGLYR Metabotropic glycine 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)
3.4 Inactive 10.1126/SCIENCE.ABL4732 2021-12-01
24XZ P2Y14 P2Y14 P2Y 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 UDP pubchem gtoplig chembl_ligand drugbank
Agonist 2.9 Active 10.1016/J.BBRC.2026.153976 2026-06-10
8YN6 HRH3 H3 Histamine 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 imetit pubchem gtoplig chembl_ligand pubchem
Agonist 2.8 Active 10.1038/S41467-024-52585-Y 2024-10-09
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 pubchem
Antagonist 3.5 Inactive 10.7554/ELIFE.48822 2019-12-04
8JSO TAAR1 TA1 Trace amine 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 dexamfetamine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.4 Active 10.1038/S41586-023-06804-Z 2023-11-15
7DGD GRM1 mGlu1 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)
4.0 Inactive 10.1007/S13238-020-00808-5 2021-09-22
9EPR B1B1U5 Rhodopsin Opsin (sight) 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 all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 4.9 Active 10.1038/S41467-024-53208-2 2024-10-30
4A4M OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine Stable_cellsHEK293TMammalian 1 chemicals 1 steps vapour diffusionsitting drop 3 chems 4.5-4.5 4°C all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 3.3 Active 10.1073/PNAS.1114089108 2012-01-25
9VB3 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
Agonist 3.0 Active 10.1038/S41586-026-10228-W 2026-06-03
9M0X Q5QNQ1 taar13d Unclassified A (Rhodopsin) Zebrafish N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Agmatine pubchem drugbank
Agmatine pubchem drugbank
UnknownAgonist 2.7 Active 2026-03-04
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
9VB7 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
Agonist 3.0 Active 10.1038/S41586-026-10228-W 2026-06-03
8JXW HRH4 H4 Histamine 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 CHEMBL213912 chembl_ligand pubchem
Agonist 3.0 Active 10.1038/S41467-024-46840-5 2024-03-20
8JD5 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 chembl_ligand pubchem pubchem drugbank
JNJ-40411813 pubchem gtoplig chembl_ligand drugbank
ADX88178 pubchem gtoplig chembl_ligand
AgonistPAMPAM 3.6 Active 10.1038/S41422-023-00830-2 2023-06-21
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
Antagonist 3.4 Inactive 10.1038/NATURE11111 2012-05-16
7TRK ACM4 M4 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
Agonist 2.8 Active 2023-05-17
9NYX OPSD Rhodopsin Opsin (sight) 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 all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Megabody 7
Inverse agonistNAM 3.1 Inactive 10.1073/PNAS.2532336123 2026-02-04
8IW7 TAAR9 TAAR9 Orphan 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 &beta;-phenylethylam... pubchem gtoplig chembl_ligand drugbank pubchem
Agonist 3.0 Active 10.1038/S41586-023-06106-4 2023-05-31
9XDR OPRK κ 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 BMS-986187 pubchem gtoplig chembl_ligand
asimadoline pubchem gtoplig chembl_ligand drugbank
Ago-PAMAgonist 2.6 Active 2026-07-08
5IUA 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 CHEMBL187810 chembl_ligand pubchem
Antagonist 2.2 Inactive 10.1021/acs.jmedchem.6b00653 2016-06-29
8Y45 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 ADL5859 pubchem gtoplig chembl_ligand
Agonist 3.5 Active 2024-11-27
9YDQ 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 MIPS3614 pubchem
DADLE pubchem gtoplig chembl_ligand drugbank pubchem
PAMAgonist 1.9 Active 2025-12-10
9LLG 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 flupentixol pubchem gtoplig chembl_ligand drugbank
negative allosteric ...
AntagonistNAM 2.8 Inactive 2026-03-04
7WY0 AGRF1 ADGRF1 ADGRF 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 N/A N/A 2.8 Active 10.1038/S41467-022-33173-4 2022-09-28
9JR0 Q9BML6 GABA-B-R2 Unclassified C (Glutamate) Fruit fly N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A GABA pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.1 Active 2025-10-22
9LQX 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 Apo (no ligand)
2.7 Inactive 2026-02-04
7YMH ADA1A α1A 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 (-)-noradrenaline pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Nb29
AgonistPAM 3.5 Active 10.1038/S41467-023-39310-X 2023-07-05
8JIT 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 N-hexadecanoyl-L-glu... pubchem
COTADUTIDE chembl_ligand drugbank pubchem
AgonistAgonist 2.9 Active 10.1073/PNAS.2303696120 2023-09-06
7IO6 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 FU12-86 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.4 Inactive 2026-05-20
7X9A 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 NEUROPEPTIDE-Y chembl_ligand pubchem
Agonist 3.2 Active 10.1126/SCIADV.ABM1232 2022-05-18
9XQB 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 Fab antibody fragmen...
Fab antibody fragmen...
Inverse agonistInverse agonist 3.5 Intermediate 10.1021/ACSOMEGA.5C11109 2026-01-07
7W0M 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 CHEMBL5812344 chembl_ligand pubchem
Agonist 3.7 Active 10.1038/S41594-022-00797-5 2022-07-27
6A93 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 risperidone pubchem gtoplig chembl_ligand drugbank drug_central
Inverse agonist 3.0 Inactive 10.1038/S41594-018-0180-Z 2019-02-13
8JD1 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 L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem pubchem drugbank
Agonist 3.7 Intermediate 10.1038/S41422-023-00830-2 2023-06-21
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
Agonist 3.4 Active 10.1038/NATURE18966 2016-08-03
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 Active 10.1038/S41467-019-13348-2 2019-12-11
7EB2 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 (-)-baclofen pubchem gtoplig chembl_ligand drugbank drugbank
rac-BHFF pubchem
AgonistPAM 3.5 Active 10.1038/S41586-021-03507-1 2021-05-05
8FD1 OPSD Rhodopsin Opsin (sight) 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 Nanobody Nb2
Allosteric antagonist 4.3 Inactive 10.1038/S41467-023-40911-9 2023-08-30
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 CHEMBL1615159 chembl_ligand pubchem
Agonist 3.8 Active 10.1038/S41594-019-0330-Y 2019-11-20
8XX6 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 CXCL8
Agonist 3.0 Active 10.1016/J.MOLCEL.2025.01.024 2025-01-15
6FKA OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine BaculovirusHEK293S(TetR)-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 4.5-4.5 20°C RS11 pubchem
Agonist 2.7 Active 10.1073/PNAS.1718084115 2018-04-04
8H0Q GRPR BB2 Bombesin 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 GRP(14-27) pubchem
Agonist 3.3 Active 10.1038/S41422-022-00743-6 2023-08-09
7F58 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 THIQ pubchem gtoplig chembl_ligand chembl_ligand pubchem chembl_ligand chembl_ligand pubchem pubchem
Agonist 3.1 Active 10.1038/S41422-021-00552-3 2021-11-03
8UNM 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 c-Epi pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
6OBA 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
AS408 pubchem gtoplig chembl_ligand
AntagonistNAM 3.1 Inactive 10.1038/S41589-020-0549-2 2020-03-25
8ZJG CML1 chemerin Chemerin receptor 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 Chemerin
Agonist 3.2 Active 10.1038/S42003-024-07228-9 2025-01-22
8A2O 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
Antagonist 3.5 Inactive 10.1107/S1600576723006428 2023-08-30
8XYI CXCR3 CXCR3 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 CHEMBL2181467 chembl_ligand pubchem chembl_ligand pubchem
Agonist 3.2 Active 2025-02-26
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
20ZX LPAR5 LPA5 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 LYSOPHOSPHATIDIC ACI... chembl_ligand pubchem
Agonist 3.0 Active 10.1073/PNAS.2537482123 2026-06-17
7F24 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 dopamine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 4.2 Active 10.1126/SCIADV.ABO4158 2022-06-15
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
8CIC 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 AB928 pubchem gtoplig chembl_ligand
Antagonist 2.1 Inactive 10.1038/S42004-023-00894-6 2023-05-31
8ZFE GPR4 GPR4 Proton 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 Apo (no ligand)
2.6 Active 10.1016/J.CELL.2024.12.001 2025-02-26
7TD3 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
Agonist 3.0 Active 10.1038/S41467-022-28417-2 2022-02-09
8WC6 TAAR1 TA1 Trace amine 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 &beta;-phenylethylam... pubchem gtoplig chembl_ligand drugbank pubchem
Agonist 3.2 Active 10.1016/J.CELL.2023.10.014 2023-12-27
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 LY2119620 pubchem gtoplig chembl_ligand
iperoxo pubchem gtoplig chembl_ligand
PAMAgonist 3.6 Active 10.1126/SCIENCE.AAW5188 2019-05-08
8JD6 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
VU0364770 pubchem gtoplig chembl_ligand
AgonistPAM 3.4 Active 10.1038/S41422-023-00830-2 2023-06-21
8UNP 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 c-Epi pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06
8H4K FFAR4 FFA4 Free fatty 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 GW9508 pubchem gtoplig chembl_ligand
Agonist 3.1 Active 10.1038/S41422-023-00835-X 2023-06-21
4GPO ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 3.6-4.0 18°C Apo (no ligand)
3.5 Inactive 10.1038/NSMB.2504 2013-02-27
8W8X MC3R MC3 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 Beta-MSH pubchem pubchem
Calcium pubchem
AgonistPAM 2.9 Active 2025-03-19
8ID4 FFAR4 FFA4 Free fatty 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 linoleic acid pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.1 Active 10.1126/SCIENCE.ADD6220 2023-03-15
6O3C SMO SMO Oxysterol F (Frizzled) Mouse N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Cholesterol pubchem drugbank
SAG21k
AgonistAgonist 2.8 Active 10.1038/S41586-019-1355-4 2019-07-03
8Y01 OPSG OPN1MW Opsin (sight) 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 all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 2.5 Active 2025-02-12
9K6L T2R16 TAS2R16 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A salicin pubchem gtoplig
Agonist 2.8 Active 10.1016/J.CELREP.2025.115604 2025-04-02
9LR3 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 azelaprag pubchem gtoplig chembl_ligand chembl_ligand pubchem
Agonist 2.8 Active 2026-02-04
7R0C 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 (Human) pubchem gtoplig chembl_ligand drugbank drug_central uniprot uniprot uniprot pubchem
Agonist 4.7 Active 10.1126/SCIADV.ABO7761 2022-09-14
8DCR 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 (partial) 2.6 Active 10.1038/S41467-022-31823-1 2022-07-27
5NM2 AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusSf9Insect 1 chemicals 1 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 2.0 Inactive 2017-09-27
9M4T ADA1A α1A 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 silodosin pubchem gtoplig chembl_ligand drugbank drug_central
Antagonist 3.2 Inactive 2025-07-02
9EK0 ACM5 M5 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
Agonist 2.8 Active 10.1038/S41467-025-62212-Z 2025-10-08
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 NTS8–13 pubchem
Agonist 4.3 Active 10.1038/S41594-020-00554-6 2021-01-06
7TD1 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 LPA pubchem
Agonist 3.1 Active 10.1038/S41467-022-28417-2 2022-02-09
9ITB LPAR6 LPA6 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 LPA pubchem
Agonist 2.9 Active 10.1073/PNAS.2415426122 2025-01-15
8UNO 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 c-Epi pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06
9FUP 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 istradefylline pubchem gtoplig chembl_ligand drug_central drugbank
Antagonist 2.5 Inactive 10.1038/S42004-024-01404-Y 2025-01-22
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 gtoplig
Agonist (partial) 2.4 Inactive 10.1124/MOL.115.101030 2015-09-30
8X0B 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 VU0424465 pubchem gtoplig chembl_ligand
quisqualate pubchem gtoplig chembl_ligand drugbank
Ago-PAMAgonist 3.1 Active 10.1038/S41467-024-55439-9 2024-11-06
9VIF NPFF1 NPFF1 Neuropeptide FF/neuropeptide AF 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 neuropeptide FF (Hum... pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 3.2 Active 10.1093/PROCEL/PWAF090 2025-12-03
8XQE 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 apelin-13 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 3.5 Active 10.1038/S41467-024-55555-6 2025-01-22
9VAX 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
Agonist 3.5 Active 10.1038/S41586-026-10228-W 2026-06-03
9BKK 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 (Human) pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank pubchem
Agonist 2.5 Active 10.1371/JOURNAL.PBIO.3002673 2024-05-22
8XWQ 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-1 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 4.6 Active 10.1038/S42003-024-06905-Z 2024-10-02
9MBC GRM8 mGlu8 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 (S)-3,4-DCPG pubchem gtoplig chembl_ligand
AZ12216052 pubchem
AgonistAgo-PAM 3.0 Active 2025-10-01
5TUD 5HT2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human BaculovirusSf21Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monopalmitolein (9.7 MAG) 6 chems 7.7-7.7 20°C ergotamine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.0 Active 10.1073/PNAS.1700891114 2017-07-26
7UL5 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 Apo (no ligand)
3.1 Intermediate 10.1038/S41594-022-00859-8 2022-06-29
8INR MC5R MC5 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 Alpha-MSH pubchem
Calcium pubchem
AgonistAgonist 2.7 Active 10.1107/S0907444909042073 2023-09-20
9KO4 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 CCL21
Agonist 3.3 Active 2025-11-26
8FYL 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 vilazodone pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.9 Active 10.1038/S41586-024-07403-2 2024-05-15
8YH2 AA3R A3 Adenosine A (Rhodopsin) Sheep 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/S41467-024-53473-1 2024-11-06
7F8Y 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 devazepide pubchem gtoplig chembl_ligand chembl_ligand pubchem chembl_ligand pubchem
Antagonist 2.5 Inactive 10.1038/S41589-021-00866-8 2021-10-13
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 pubchem gtoplig chembl_ligand drugbank
Agonist 2.5 Active 10.1016/J.MOLCEL.2020.09.020 2020-09-09
7SK8 ACKR3 ACKR3 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 CXCL12
CCX662 pubchem
AgonistAgonist (partial) 3.3 Active 10.1126/SCIADV.ABN8063 2022-07-27
8E9Z ACM3 M3 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
Agonist 2.7 Active 10.1038/S41586-022-05489-0 2022-11-30
9WP9 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
Agonist 3.3 Active 10.1073/PNAS.2507421122 2025-11-26
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
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
Agonist 2.8 Active 10.1038/NATURE23272 2017-07-12
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 Islet amyloid polype... pubchem
Agonist 3.3 Active 10.1126/SCIENCE.ABM9609 2022-03-30
6LMK 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 Glucagon pubchem
Agonist 3.7 Active 10.1126/SCIENCE.AAZ5346 2020-04-01
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
Cholesterol pubchem drugbank
AntagonistPAM 3.2 Inactive 10.1126/SCIADV.ABB5419 2020-08-05
8FLT 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 M-PTH(1-14)
Agonist 3.0 Active 10.1016/J.STR.2023.04.002 2023-04-26
9W0P T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHLORHEXIDINE chembl_ligand pubchem pubchem pubchem pubchem pubchem drugbank
Agonist 3.6 Active 10.1038/S41594-026-01786-8 2026-04-22
7TD4 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 2.6 Active 10.1038/S41467-022-28417-2 2022-02-09
8IUL PF2R FP 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 latanoprost (free ac... pubchem gtoplig chembl_ligand
Agonist 2.8 Active 10.1038/S41467-023-38411-X 2023-07-12
7XAT 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 drugbank drug_central pubchem
Agonist 2.9 Active 2022-08-31
8UTD HCAR2 HCA2 Hydroxycarboxylic 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 CHEMBL2057618 chembl_ligand pubchem
Agonist 3.2 Active 10.1016/J.CELL.2024.11.001 2025-02-26
7INI 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 F135 pubchem
Antagonist 2.6 Inactive 2026-05-20
9KO6 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 CCL19
Agonist 3.3 Active 2025-11-26
23IV CNR1 CB1 Cannabinoid 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 LZD503 pubchem
Agonist 2.4 Active 2026-05-20
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
Agonist 4.0 Active 10.1038/S41586-021-03495-2 2021-06-23
8GTM CRHR1 CRF1 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 BMK-C203
Allosteric antagonist 2.6 Inactive 10.1038/S12276-023-01082-1 2023-09-13
9JF4 NMBR BB1 Bombesin 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 PD 168368 pubchem gtoplig chembl_ligand
Antagonist 3.6 Inactive 2025-07-09
8GED 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 c-Epi pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
8WG9 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 D-AP4 pubchem gtoplig chembl_ligand pubchem gtoplig chembl_ligand chembl_ligand pubchem
Agonist 4.5 Intermediate 2024-11-27
8GGO 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 c-Epi pubchem
Agonist 3.2 Active 10.1038/S41586-024-07153-1 2024-03-06
9KUX 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 cmpd644 pubchem
Agonist 3.6 Active 2025-09-17
8EIT FFAR1 FFA1 Free fatty 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 docosahexaenoic acid pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 2.8 Active 10.1073/PNAS.2219569120 2023-05-24
4NTJ P2Y12 P2Y12 P2Y A (Rhodopsin) Human BaculovirusSf9Insect 6 chemicals 6 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 6.0-6.5 20°C AZD1283 pubchem gtoplig chembl_ligand
Antagonist 2.6 Active 10.1038/NATURE13083 2014-03-26
9LDZ O6C76 OR6C76 Olfactory family 6 O2 (Olfactory/extra-nasal 2) 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 drugbank
ethyl (2R,3S)-3-meth... pubchem
PAMAgonist 3.2 Active 2026-01-28
7INL 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 5-methyl-1,2-oxazole... pubchem
Antagonist 2.2 Inactive 2026-05-20
8IRR 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 rotigotine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.2 Active 10.1038/S41422-023-00808-0 2023-06-21
8Z65 GPR4 GPR4 Proton 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)
3.0 Active 2025-04-23
8CXO SMO SMO Oxysterol F (Frizzled) Mouse 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)
3.7 Inactive 10.1038/S41467-022-32125-2 2022-08-03
9S38 LGR4 LGR4 Orphan 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)
3.9 Inactive 2025-09-03
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 chembl_ligand pubchem drugbank drug_central drugbank
Agonist 2.7 Active 10.1038/S41586-020-2419-1 2019-01-09
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
7WBJ VIPR2 VPAC2 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 PACAP-27 (Human) pubchem gtoplig uniprot uniprot uniprot uniprot pubchem
Agonist 3.4 Active 10.1038/S41467-022-30041-Z 2022-05-18
9WQN GRM1 mGlu1 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 chembl_ligand pubchem pubchem drugbank
Ro0711401 pubchem gtoplig chembl_ligand
AgonistPAM 3.7 Active 2026-05-27
9KV8 C3AR C3a Complement peptide 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 TLQP-21 (Human) pubchem gtoplig uniprot
Agonist 3.2 Active 10.1101/2025.05.26.656101 2025-11-26
6GPX 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 gtoplig chembl_ligand pubchem
Antagonist 2.7 Inactive 10.1016/J.STR.2018.10.027 2019-01-02
8GGF 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 c-Epi pubchem
Agonist 3.6 Active 10.1038/S41586-024-07153-1 2024-03-06
2YDO AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusHi5Insect 4 chemicals 4 steps vapour diffusionsitting drop 5 chems 7.6-7.6 4°C adenosine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.0 Active 10.1038/NATURE10136 2011-05-18
9UST A0A9L0JPP9 MRGPRE Orphan A (Rhodopsin) Donkey N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (E)-3-(2-methoxyphen... pubchem
Agonist 3.0 Active 2025-07-02
8W8Y MC3R MC3 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 γ-MSH (Human) pubchem gtoplig uniprot uniprot uniprot pubchem
Agonist 2.9 Active 2025-03-19
8YJP GP156 GPR156 Orphan 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)
3.1 Active 10.1038/S41467-024-54681-5 2025-02-05
7ZBE OPSD Rhodopsin Opsin (sight) 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 all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Inverse agonist 1.8 Inactive 10.1038/S41586-023-05863-6 2023-03-29
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 CHEMBL124345 chembl_ligand pubchem
Agonist (partial) 3.1 Inactive 10.1021/acs.jmedchem.0c01856 2021-04-07
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 10.1038/S41467-022-28111-3 2022-03-02
8ZF9 GPR4 GPR4 Proton 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 Apo (no ligand)
2.6 Active 10.1016/J.CELL.2024.12.001 2025-02-26
7X9C NPY4R Y4 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 PANCREATIC POLYPEPTI... chembl_ligand pubchem
Agonist 3.0 Active 10.1126/SCIADV.ABM1232 2022-05-18
7MTB OPSD Rhodopsin Opsin (sight) 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 all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 4.0 Active 10.1038/S41586-021-03721-X 2021-07-07
9T9P 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 3.0 Inactive 10.1107/S2059798326003785 2026-05-27
8XZI 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 CMF-019 pubchem gtoplig chembl_ligand
Agonist 2.7 Active 2024-03-20
8XWF 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 CXCL3
Agonist 3.7 Active 10.1016/J.MOLCEL.2025.01.024 2025-01-15
9P84 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 NTS8–13 pubchem
Agonist 2.7 Active 10.1038/S41586-026-10120-7 2026-03-25
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 NTS8–13 pubchem
Agonist 2.8 Inactive 10.1073/PNAS.1317903111 2014-01-29
9K1C FFAR1 FFA1 Free fatty 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 docosahexaenoic acid pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.2 Active 10.1016/J.CELREP.2024.115024 2024-12-11
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 PACAP-38 pubchem
Agonist 3.0 Active 10.1016/J.MOLCEL.2020.01.012 2020-02-05
6CM4 DRD2 D2 Dopamine A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 6 chems 7.8-7.8 20°C risperidone pubchem gtoplig chembl_ligand drugbank drug_central
Inverse agonist 2.9 Inactive 10.1038/NATURE25758 2018-03-14
7WU3 AGRF1 ADGRF1 ADGRF 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 LPC 16:0
PAM 3.1 Active 10.1038/S41586-022-04580-W 2022-04-27
9KHH LGR4 LGR4 Orphan 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 Norrin
Agonist 3.7 Inactive 2025-07-16
8ZCJ SSR5 SST5 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 pasireotide pubchem gtoplig drugbank chembl_ligand drug_central
Agonist 3.1 Active 10.1038/S41401-024-01314-8 2024-07-10
7IP4 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 FU273-77 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.0 Inactive 2026-05-20
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 10.1107/S2052252520011379 2020-07-15
9II2 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 L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem pubchem drugbank
Agonist 3.7 Inactive 10.1038/S41589-025-01858-8 2025-03-05
6PH7 OPSD Rhodopsin Opsin (sight) 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
Agonist 2.9 Active 2020-07-01
22EM OPRK κ 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 beta01
Agonist 2.9 Active 2026-05-06
9KVS C3AR C3a Complement peptide 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 SB290157 pubchem gtoplig chembl_ligand
Antagonist 2.8 Active 2026-06-10
7DTU 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 D-tryptophan pubchem gtoplig chembl_ligand drugbank pubchem gtoplig chembl_ligand drugbank drug_central
PAM 4.4 Intermediate 10.1038/S41422-021-00474-0 2021-03-10
7EWR MGLYR MGLYR Metabotropic glycine 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 Regulator of G-prote...
Allosteric antagonist 4.7 Intermediate 10.1038/S41467-021-27147-1 2021-12-01
9L8L 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 CHEMBL1615159 chembl_ligand pubchem
ATAZANAVIR chembl_ligand pubchem drugbank
AgonistAgo-PAM 3.2 Active 10.1016/J.CELL.2025.12.023 2025-12-31
9LMP GPR4 GPR4 Proton 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 NE 52-QQ57 pubchem gtoplig chembl_ligand
Antagonist 2.7 Active 2025-07-02
9VJ6 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 NLX-101 pubchem gtoplig chembl_ligand
Agonist 2.6 Active 2025-11-12
7IOJ 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 CHEMBL1572253 chembl_ligand pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.3 Inactive 2026-05-20
8ZME PAR2 PAR2 Proteinase-activated 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 3.2 Active 10.1038/S41421-025-00851-8 2025-05-28
6PS0 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 (S)-carazolol pubchem drugbank
Inverse agonist 3.4 Inactive 10.1107/S2052252519013137 2019-11-13
9LLF 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 dopamine pubchem gtoplig chembl_ligand drugbank drug_central
De novo designed GPC...
AgonistPAM 2.6 Active 2026-03-04
8YW3 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 retatrutide pubchem gtoplig
Agonist 2.7 Active 10.1038/S41421-024-00700-0 2024-09-18
7INK 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
methyl 1H-indole-6-c... pubchem
AntagonistUnknown 2.2 Inactive 2026-05-20
25IF C5AR2 C5a2 Complement peptide 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 mC5a-desArg
Agonist 3.4 Active 10.1016/J.MOLCEL.2026.06.002 2026-07-01
8JPP SUCR1 succinate Succinate 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 succinic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank
Agonist 3.2 Active 10.1038/S41422-024-00968-7 2024-05-22
8E9Y ACM3 M3 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 Clozapine N-oxide pubchem
Agonist 2.8 Active 10.1038/S41586-022-05489-0 2022-11-30
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 drugbank
NAM 2.6 Inactive 10.1038/NATURE13396 2014-07-02
7RTB 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 Peptide-19
Agonist 2.1 Active 10.1016/J.BBRC.2021.09.016 2021-10-06
8UNX 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 c-Epi pubchem
Agonist 3.6 Active 10.1038/S41586-024-07153-1 2024-03-06
25IK MAS MAS1 Orphan 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)
3.0 Active 2026-05-20
7WVW 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 fM9
Agonist 3.1 Active 10.1038/S41467-022-29361-X 2022-04-13
8GFW 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 c-Epi pubchem
Agonist 3.0 Active 10.1038/S41586-024-07153-1 2024-03-06
8WC7 TAAR1 TA1 Trace amine 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 CHEMBL4301324 chembl_ligand pubchem
Agonist 3.1 Active 10.1016/J.CELL.2023.10.014 2023-12-27
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
Agonist 3.0 Active 10.1038/S41586-019-1337-6 2019-07-10
9UT8 TS1R2 TAS1R2 Taste 1 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)
3.4 Inactive 10.1038/S41586-025-09302-6 2025-07-16
8UO4 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 c-Epi pubchem
Agonist 4.0 Active 10.1038/S41586-024-07153-1 2024-03-06
9KVP C3AR C3a Complement peptide 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 SB290157 pubchem gtoplig chembl_ligand
Agonist 2.8 Active 2025-11-26
9R42 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 quinpirole pubchem gtoplig chembl_ligand
Agonist 3.2 Active 2026-05-20
8HK2 C3AR C3a Complement peptide 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 C3a anaphylatoxin
Agonist 2.9 Active 10.1038/S41589-023-01339-W 2023-05-10
5F8U ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 1 chemicals 1 steps vapour diffusionHanging drops 1 chems 3.6-4.0 18°C 4-{[(2S)-3-(tert-but... pubchem drugbank
Antagonist 3.4 Inactive 10.1038/NSMB.3130 2015-12-23
9J1P 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 g1:Ox
Agonist 3.0 Active 10.1021/JACS.4C12808 2025-02-26
8RWD 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 StilSwitch3 pubchem
Antagonist 2.1 Inactive 2025-01-08
8HAF 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 PTHrP-(1-36) (Human) pubchem gtoplig uniprot
Agonist 3.3 Active 10.1038/S41401-022-01032-Z 2022-12-21
9JH5 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 C16:0 ceramide pubchem
Agonist 2.8 Active 10.1038/S41586-025-08792-8 2025-04-23
7IOD 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 FU35-78 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.4 Inactive 2026-05-20
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 (Human) pubchem gtoplig chembl_ligand drugbank drug_central uniprot uniprot uniprot
Mg2+ pubchem gtoplig drugbank
AgonistCofactor 2.9 Active 10.1038/S41594-022-00728-4 2022-03-09
7WVU 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 fMet-Leu-Phe pubchem gtoplig chembl_ligand
Agonist 3.3 Active 10.1038/S41467-022-29361-X 2022-04-13
8GTG CRHR1 CRF1 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 BMK-I-152 pubchem
Antagonist 2.8 Inactive 10.1038/S12276-023-01082-1 2023-09-13
9KPF T2R16 TAS2R16 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A salicin pubchem gtoplig
Agonist 3.2 Active 10.1016/J.CELREP.2025.115604 2025-04-02
8GEF 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 c-Epi pubchem
Agonist 3.8 Active 10.1038/S41586-024-07153-1 2024-03-06
5NLX 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 2.1 Inactive 10.1038/S41467-017-00630-4 2017-09-27
7YJ4 RL3R2 RXFP4 Relaxin family peptide 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 INSL5 (chain A)
INSL5 (chain B)
AgonistAgonist 3.2 Active 10.1038/S41467-023-36182-Z 2023-03-01
7WQ3 GALR1 GAL1 Galanin 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 galanin(1-13)amide gtoplig pubchem
Agonist 2.7 Active 10.1038/S41467-022-29072-3 2022-04-20
9K27 PRLHR PrRP Prolactin-releasing peptide 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 PrRP31 pubchem
Agonist 2.7 Active 2025-01-29
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
8IRU DRD4 D4 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 Cholesterol pubchem drugbank
rotigotine pubchem gtoplig chembl_ligand drugbank drug_central
PAMAgonist 3.2 Active 10.1038/S41422-023-00808-0 2023-06-21
9M88 GPR3 GPR3 Orphan 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 AF64394 pubchem
N-oleoylethanolamide pubchem gtoplig chembl_ligand drugbank
NAMAgonist 3.1 Active 2025-09-24
8YZK GPC5D GPRC5D Orphan 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)
3.4 Inactive 10.1038/S41467-024-49625-Y 2024-07-03
8IJA HCAR2 HCA2 Hydroxycarboxylic 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 nicotinic acid pubchem gtoplig chembl_ligand drugbank drug_central drugbank drugbank
Agonist 2.7 Active 10.1038/S41421-023-00610-7 2024-01-03
7VVM 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 Parathyroid hormone
Agonist 3.2 Active 10.1016/J.MOLCEL.2022.07.003 2022-08-03
5TZR FFAR1 FFA1 Free fatty acid A (Rhodopsin) Human BaculovirusSf21Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 7.7-8.3 20°C MK-8666 chembl_ligand pubchem drugbank
Agonist (partial) 2.2 Active 10.1038/NSMB.3417 2017-06-07
9IV2 AGRD1 ADGRD1 ADGRD 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 dihydrotestosterone pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.5 Active 10.1016/J.CELL.2025.01.006 2025-02-12
9YDA OPSG OPN1MW Opsin (sight) 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 all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 2.9 Active 10.1073/PNAS.2516318122 2025-12-24
6LUQ 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 haloperidol pubchem gtoplig chembl_ligand drugbank drug_central
Antagonist 3.1 Inactive 10.1038/S41467-020-14884-Y 2020-03-04
7X2F 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 dopamine pubchem gtoplig chembl_ligand drugbank drug_central
mevidalen pubchem gtoplig chembl_ligand
AgonistPAM 3.0 Active 10.1038/S41467-022-30929-W 2022-06-15
8HQM GP132 GPR132 Proton 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-hexadecanoylglycin... pubchem drugbank
Agonist (partial) 3.0 Active 10.1038/S42255-023-00899-4 2023-10-11
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)
3.6 Inactive 10.1038/S41586-021-03641-W 2021-06-23
5DSG ACM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 5.5-8.0 20°C Pentaglyme pubchem drugbank
TIOTROPIUM chembl_ligand pubchem drugbank pubchem pubchem
NAMInverse agonist 2.6 Inactive 10.1038/NATURE17188 2016-03-16
7IOX 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 FU163-109 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.2 Inactive 2026-05-20
7XY6 AA2BR A2B 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 BAY 60-6583 pubchem gtoplig chembl_ligand
Agonist (partial) 3.0 Active 10.1126/SCIADV.ADD3709 2023-05-03
9S37 LGR4 LGR4 Orphan 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 NB21
Antagonist 3.9 Inactive 10.1038/S41467-025-63410-5 2025-07-30
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 E33 pubchem
Antagonist 2.8 Inactive 2019-12-04
4BEZ OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine Stable_cellsHEK293S-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionsitting drop 4 chems 4.5-4.5 20°C Apo (no ligand)
3.3 Active 10.1038/EMBOR.2013.44 2013-04-24
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 6o (BS46)
Antagonist 3.1 Inactive 10.1073/PNAS.1813988115 2018-11-28
7P00 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 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 2.7 Active 10.1126/SCIADV.ABK2872 2021-12-15
8Z9P GPR4 GPR4 Proton 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)
2.5 Active 10.1016/J.MOLCEL.2025.02.030 2025-07-09
8X17 AA3R A3 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 Cl-IB-MECA pubchem gtoplig chembl_ligand drugbank
Agonist 3.2 Active 10.1038/S41467-024-47207-6 2024-04-24
9LZ2 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... pubchem
Agonist 3.0 Active 2026-03-11
7INH 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 F132 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.3 Inactive 2026-05-20
8YN3 HRH2 H2 Histamine 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 histamine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 2.6 Active 10.1038/S41467-024-52585-Y 2024-10-09
9M1H PE2R1 EP1 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
Agonist 2.6 Active 10.1073/PNAS.2423840122 2025-04-30
9VJF 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 buspirone pubchem gtoplig chembl_ligand drugbank drug_central
Agonist (partial) 2.7 Active 10.1016/J.CELL.2025.10.022 2025-11-12
6BD4 FZD4 FZD4 WNT 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)
2.4 Inactive 10.1038/S41586-018-0447-X 2018-08-22
7CX3 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 taprenepag pubchem gtoplig chembl_ligand drugbank
Agonist 2.8 Active 10.1126/SCIADV.ABF1268 2021-05-05
6RZ7 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-2570366 pubchem gtoplig
Antagonist 2.4 Active 10.1038/S41467-019-13348-2 2019-12-11
6I9K B1B1U5 Rhodopsin Opsin (sight) 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 all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Inverse agonist 2.2 Inactive 10.1073/PNAS.1902192116 2019-07-03
8K6O 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 [Leu31, Pro34]-NPY pubchem
Agonist 3.3 Active 2024-07-31
8JIS 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 Peptide 15 (P15)
Agonist 2.5 Active 10.1073/PNAS.2303696120 2023-11-08
9K07 BRS3 BB3 Bombesin 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 DSO-5a
Agonist 2.8 Active 2025-08-27
9MQL OPRK κ 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 #020_E1 pubchem
Inverse agonist 3.0 Inactive 2025-02-12
8ZPM CXCR4 CXCR4 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 mavorixafor pubchem gtoplig chembl_ligand drugbank
Antagonist 3.2 Inactive 2025-02-26
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 chembl_ligand pubchem drugbank drug_central
Agonist 3.0 Active 10.1038/S41422-021-00552-3 2021-11-03
8E9X ACM4 M4 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 CHEMBL73538 chembl_ligand pubchem
Agonist 2.7 Active 10.1038/S41586-022-05489-0 2022-11-30
7SCG OPRM μ Opioid 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 FH210 pubchem
Agonist 3.0 Active 10.1002/ANIE.202200269 2022-04-20
6OY9 OPSD Rhodopsin Opsin (sight) 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 all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 3.9 Active 10.1016/J.MOLCEL.2019.06.007 2019-07-24
9ODG OPRM μ Opioid 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 Apo (no ligand)
4.3 Active 10.1038/S41586-025-10056-4 2026-03-04
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 drugbank drug_central pubchem
Agonist 2.5 Active 10.1038/S41594-022-00727-5 2022-03-09
8FYX 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 buspirone pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.6 Active 10.1038/S41586-024-07403-2 2024-05-15
7W0N 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 Elabela/Toddler-32 (... pubchem gtoplig uniprot
Agonist 4.2 Active 10.1038/S41594-022-00797-5 2022-07-27
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
Inverse agonist 2.7 Inactive 10.1107/S2052252519013137 2019-11-13
6K41 ADA2B α2B 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 dexmedetomidine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.9 Active 10.1038/S41589-020-0492-2 2020-04-15
7WV9 CNR1 CB1 Cannabinoid 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 CP55940 pubchem gtoplig chembl_ligand
ZCZ011 pubchem
AgonistPAM 3.4 Active 10.1038/S41589-022-01038-Y 2022-06-15
9BKJ 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 (Human) pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank pubchem
AMINO GROUP pubchem
AgonistAgonist 2.6 Active 10.1371/JOURNAL.PBIO.3002673 2024-05-22
9BQJ OPRM μ Opioid 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 RO-76 pubchem
Agonist (partial) 3.3 Active 2024-09-11
7IOO 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 FU132,428-27 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.0 Inactive 2026-05-20
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 2011-01-12
8ZF4 GPR4 GPR4 Proton A (Rhodopsin) Western clawed frog 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)
3.1 Active 10.1016/J.CELL.2024.12.001 2025-02-26
8IWM TAAR9 TAAR9 Orphan 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 &beta;-phenylethylam... pubchem gtoplig chembl_ligand drugbank pubchem
Agonist 3.2 Active 10.1038/S41586-023-06106-4 2023-05-31
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 RS79948 pubchem gtoplig chembl_ligand
Antagonist 2.7 Inactive 2019-12-04
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
Antagonist 3.7 Inactive 10.1038/S41586-021-03680-3 2021-07-07
9C1P 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
'6218 pubchem
D-tryptophan pubchem gtoplig chembl_ligand drugbank pubchem gtoplig chembl_ligand drugbank drug_central
AgonistPAMAgonist 2.8 Active 2024-10-02
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
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
4Z35 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-9910539 pubchem gtoplig
Antagonist 2.9 Inactive 2015-06-03
6NIY 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 chembl_ligand drug_central pubchem
Agonist 3.3 Active 10.1021/ACSPTSCI.8B00056 2019-01-23
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
7CKW 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 fenoldopam pubchem gtoplig chembl_ligand drugbank drug_central pubchem gtoplig chembl_ligand pubchem gtoplig
Agonist 3.2 Active 10.1016/J.CELL.2021.01.028 2021-03-03
7XBW CX3C1 CX3CR1 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 Cholesterol pubchem drugbank
PAM 2.8 Active 10.1126/SCIADV.ABN8048 2022-07-13
7VVJ 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 PTHrP[1-36]
Agonist 3.2 Active 10.1016/J.MOLCEL.2022.07.003 2022-08-03
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 CGEN-855A
Agonist 2.9 Active 10.1038/S41467-022-28586-0 2022-03-30
8XQS T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A flufenamic acid pubchem gtoplig chembl_ligand drugbank drug_central
Cholesterol pubchem drugbank
Allosteric agonistAgonist 3.3 Active 10.1038/S41586-024-07569-9 2024-07-10
8K5B HCAR2 HCA2 Hydroxycarboxylic 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 nicotinic acid pubchem gtoplig chembl_ligand drugbank drug_central drugbank drugbank
Agonist 3.4 Active 10.1038/S41467-023-42764-8 2023-11-22
8XXR 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 Apo (no ligand)
3.2 Active 10.1016/J.MOLCEL.2025.01.024 2025-01-15
7D77 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 cortisol pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.9 Active 10.1038/S41586-020-03083-W 2021-02-03
8I7V HCAR2 HCA2 Hydroxycarboxylic 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 Acipimox pubchem
Agonist 2.8 Active 10.1038/S41467-023-42764-8 2024-02-07
8YH5 AA3R A3 Adenosine A (Rhodopsin) Sheep N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Riboprine pubchem drugbank
Agonist 3.7 Active 10.1038/S41467-024-53473-1 2024-11-06
9P0M CXCR3 CXCR3 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 CXCL11
Agonist 3.0 Active 10.1126/SCIADV.ADZ3767 2026-04-29
8IZB GP174 GPR174 Orphan 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 L-serine pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank pubchem drugbank
LYSOPHOSPHATIDIC ACI... chembl_ligand pubchem
AgonistAgonist 3.1 Active 10.1371/JOURNAL.PBIO.3002387 2023-11-01
7SK6 ACKR3 ACKR3 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 CXCL12_LRHQ
Agonist 4.0 Active 10.1126/SCIADV.ABN8063 2022-07-27
9BP3 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 cagrilintide pubchem gtoplig drugbank
Agonist 2.2 Active 2025-04-23
8TR0 GRM3 mGlu3 Metabotropic glutamate C (Glutamate) Rat 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
Antagonist 3.2 Inactive 10.1101/2023.08.13.552748 2024-07-31
8ZJE KISSR kisspeptin Kisspeptin 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 TAK-448 pubchem gtoplig chembl_ligand drugbank
Agonist 3.1 Active 2024-07-03
9M3S Q5QNP9 taar13a Unclassified A (Rhodopsin) Zebrafish N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A histamine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 2.8 Active 2026-03-11
12IY CNR2 CB2 Cannabinoid 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 '5249 pubchem
Agonist 2.9 Active 2026-07-15
9JQZ 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 grapiprant pubchem gtoplig chembl_ligand drugbank
Antagonist 2.7 Inactive 2025-10-22
8KH5 GP174 GPR174 Orphan 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 Lysophosphotidylseri... pubchem drugbank
Agonist 2.8 Active 10.1038/S41467-023-41654-3 2023-10-18
7VQX VIPR2 VPAC2 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 PACAP-27 (Human) pubchem gtoplig uniprot uniprot uniprot uniprot pubchem
Agonist 2.7 Active 10.1038/S41467-022-30041-Z 2022-05-18
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 CHEMBL1823342 chembl_ligand chembl_ligand chembl_ligand pubchem pubchem pubchem
Antagonist 2.8 Inactive 10.1038/S41467-021-21030-9 2021-01-27
8YW5 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 retatrutide pubchem gtoplig
Agonist 2.8 Active 10.1038/S41421-024-00700-0 2024-08-07
8Z9O GPR4 GPR4 Proton 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)
2.4 Active 10.1016/J.MOLCEL.2025.02.030 2025-07-16
8HS2 GPR20 GPR20 Orphan 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)
3.1 Active 10.1038/S41421-023-00520-8 2023-03-08
8GEA 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 c-Epi pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
7X1T TRFR TRH1 Thyrotropin-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 taltirelin pubchem gtoplig chembl_ligand drug_central
Agonist 3.3 Active 10.1038/S41422-022-00646-6 2022-08-31
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 NTS8–13 pubchem
Agonist 4.9 Active 10.1038/S41422-019-0256-2 2019-12-04
5UZ7 CALCR CT Calcitonin B1 (Secretin) Human BaculovirusHi5Insect 2 chemicals 2 steps Cryo-EMVolta phase plate (FEI) 6 chems 7.4-7.4 cryoTemp(liquid Nitrogen) CALCITONIN SALMON pubchem chembl_ligand drug_central pubchem
Agonist 4.1 Active 10.1038/NATURE22327 2017-05-03
8X7A PI2R IP 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 treprostinil pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.6 Active 10.1126/SCIADV.ADK5184 2024-03-06
8EF5 OPRM μ 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 fentanyl pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.3 Active 10.1016/J.CELL.2022.09.041 2022-11-09
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 chembl_ligand pubchem drugbank drug_central drugbank
Agonist 3.3 Active 10.1038/S41586-020-2419-1 2020-06-17
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 CHEMBL6177228 chembl_ligand pubchem
Allosteric antagonist 3.2 Inactive 10.1038/S41586-020-2492-5 2020-09-02
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 dopamine pubchem gtoplig chembl_ligand drugbank drug_central
mevidalen pubchem gtoplig chembl_ligand
AgonistAgo-PAM 3.2 Active 10.1038/S41422-021-00482-0 2021-03-03
8JZZ C5AR1 C5a1 Complement peptide 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 C5a des-Arg (Human) gtoplig
Agonist (partial) 3.3 Active 10.1016/J.CELL.2023.09.020 2023-10-18
8XWP 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-1 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 3.2 Active 10.1038/S42003-024-06905-Z 2024-10-02
6RNK SUCR1 succinate Succinate 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 NF-56-EJ40 pubchem gtoplig chembl_ligand
Antagonist 1.9 Active 10.1038/S41586-019-1663-8 2019-08-14
7DHI 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 levosalbutamol pubchem gtoplig chembl_ligand drug_central drugbank
Agonist (partial) 3.3 Active 10.1093/NSR/NWAA284 2020-12-16
7VVN 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 PTH pubchem
Agonist 3.8 Active 10.1016/J.MOLCEL.2022.07.003 2022-08-03
9K0X P2RY2 P2Y2 P2Y 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 ATP pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.8 Active 10.1038/S41421-025-00797-X 2025-06-11
7ION 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 FU132-90 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.1 Inactive 2026-05-20
7INW 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 F428 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.6 Inactive 2026-05-20
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 PSB-2115 pubchem
Antagonist 2.6 Inactive 10.1002/ANIE.202115545 2022-03-02
8EJK FFAR1 FFA1 Free fatty 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 fasiglifam pubchem gtoplig chembl_ligand drugbank
Agonist (partial) 3.4 Active 10.1073/PNAS.2219569120 2023-05-24
4XEE 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 7.0-8.0 20°C NTS8–13 pubchem
Agonist 2.9 Active 10.1038/NCOMMS8895 2015-07-29
7W0L 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 CHEMBL5812344 chembl_ligand pubchem
Agonist 3.6 Active 10.1038/S41594-022-00797-5 2022-07-27
7IP8 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
FU300-24 pubchem
AntagonistUnknown 2.3 Inactive 2026-05-20
7XK2 HCAR2 HCA2 Hydroxycarboxylic 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 MK 6892 pubchem gtoplig chembl_ligand pubchem
Agonist 3.1 Active 10.1038/S41467-023-37177-6 2023-02-22
5XR8 CNR1 CB1 Cannabinoid A (Rhodopsin) Human Transient_transfectionHEK293TMammalian 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 6.2-6.2 20°C AM841 pubchem gtoplig chembl_ligand
Agonist 3.0 Active 10.1038/NATURE23272 2017-07-12
8GH1 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 c-Epi pubchem
Agonist 4.1 Active 10.1038/S41586-024-07153-1 2024-03-06
8W1V 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 Ligand 4
Antagonist 3.0 Inactive 2024-07-17
9YDP 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 DADLE pubchem gtoplig chembl_ligand drugbank pubchem
Agonist 2.0 Active 10.1101/2025.10.16.682975 2025-12-10
6CMO OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps Cryo-EMFEI TITAN Krios microscope,Gatan K2 Summit direct electron camera,GIF-quantum energy filter (Gatan) 4 chems 7.2-7.2 4°C all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 4.5 Active 10.1038/S41586-018-0215-Y 2018-06-20
9IK9 SSR1 SST1 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 LANREOTIDE chembl_ligand pubchem drugbank
Agonist 3.4 Active 10.1016/J.APSB.2025.03.043 2025-04-30
2R4R ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps vapour diffusionhanging drop 5 chems 6.5-7.5 22°C Apo (no ligand)
3.4 Inactive 10.1038/NATURE06325 2007-11-06
9J87 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-MeOT pubchem gtoplig chembl_ligand
Agonist 2.8 Active 2026-02-25
7IOL 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 FU132-3 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.8 Inactive 2026-05-20
9N1Q 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 SRB103H
Agonist 3.0 Active 2026-04-22
9U9V 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 METHAMPHETAMINE chembl_ligand pubchem drugbank drug_central
Agonist 2.9 Active 2025-09-03
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 (Human) pubchem gtoplig chembl_ligand drugbank drug_central uniprot uniprot uniprot pubchem
Agonist 4.4 Active 10.1126/SCIADV.ABG5628 2021-06-02
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 uniprot chembl_ligand pubchem
Agonist 3.3 Active 10.1038/S41589-021-00866-8 2021-10-13
9V35 C5AR2 C5a2 Complement peptide 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)
3.0 Inactive 10.1016/J.MOLCEL.2026.06.002 2026-07-01
8RW0 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 istradefylline pubchem gtoplig chembl_ligand drug_central drugbank
Antagonist 1.9 Inactive 10.1038/S41467-024-55109-W 2025-01-08
2YCW ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 2 chemicals 2 steps vapour diffusionNA 3 chems 8.1-8.1 NA (S)-carazolol pubchem drugbank
Antagonist 3.0 Inactive 10.1073/PNAS.1100185108 2011-06-01
9K3P 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 Apo (no ligand)
3.0 Active 10.1016/J.STR.2025.03.004 2025-08-06
5L7D SMO SMO Oxysterol F (Frizzled) Human Transient_transfectionHEK293S(TetR)-GnTI-Mammalian 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 7 chems 4.0-4.0 20°C Cholesterol pubchem drugbank
Agonist 3.2 Inactive 10.1038/NATURE18934 2016-07-20
6PS3 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 CHEMBL3799125 chembl_ligand pubchem
Agonist 2.5 Inactive 10.1107/S2052252519013137 2019-11-13
9VAZ 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
Agonist 3.4 Active 10.1038/S41586-026-10228-W 2026-06-03
9JEA 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 CHEMBL1379091 chembl_ligand pubchem chembl_ligand pubchem chembl_ligand pubchem
Antagonist 3.4 Inactive 2025-07-09
9JR2 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 Parathyroid hormone
Agonist 2.8 Active 2024-10-16
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
6FFH 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 fenobam pubchem gtoplig chembl_ligand pubchem drugbank pubchem
NAM 2.7 Inactive 10.1021/ACS.JMEDCHEM.7B01722 2018-03-07
7S8N MRGX2 MRGPRX2 Orphan 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)-ZINC-3573 pubchem gtoplig chembl_ligand
Agonist 2.9 Active 10.1038/S41586-021-04126-6 2021-11-17
8JXT HRH4 H4 Histamine 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 histamine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.1 Active 10.1038/S41467-024-46840-5 2024-03-20
1HZX OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine NANativeBovine 2 chemicals 2 steps vapour diffusionHanging drops 7 chems 6.0-6.0 4°C all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Inverse agonist 2.8 Inactive 10.1021/BI0155091 2001-07-04
8F76 O51E2 OR51E2 Olfactory family 51 O1 (Olfactory/extra-nasal 1) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A propanoic acid pubchem gtoplig chembl_ligand drugbank chembl_ligand pubchem
Agonist 3.1 Active 10.1038/S41586-023-05798-Y 2023-03-22
7E2Y 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 5-hydroxytryptamine pubchem gtoplig chembl_ligand drugbank
PtdIns4P pubchem
AgonistPAM 3.0 Active 10.1038/S41586-021-03376-8 2021-04-14
8Y69 LGR4 LGR4 Orphan 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-spondin-2
Agonist 3.4 Inactive 2024-12-04
8JHN HCAR2 HCA2 Hydroxycarboxylic 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 monomethyl fumarate pubchem gtoplig chembl_ligand drugbank pubchem
Agonist 3.8 Active 10.1038/S41467-024-46239-2 2024-03-06
7IND 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
4-fluorobenzene-1-ca... pubchem
AntagonistUnknown 2.7 Inactive 2026-05-20
8XWS 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 CXCL5
Agonist 3.1 Active 10.1016/J.MOLCEL.2025.01.024 2025-01-15
9JHJ 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 C18 Ceramide pubchem
Agonist 3.2 Active 10.1126/SCIENCE.ADO4188 2025-03-19
8GH0 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 c-Epi pubchem
Agonist 4.0 Active 10.1038/S41586-024-07153-1 2024-03-06
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 Compound 2 pubchem
Ago-PAM 2.5 Active 10.1038/S41467-021-24058-Z 2021-08-11
9V6O OPRK κ 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 nalfurafine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 2.8 Active 10.1038/S41467-025-64882-1 2025-11-19
8J21 FFAR3 FFA3 Free fatty 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 butyric acid pubchem gtoplig chembl_ligand drugbank chembl_ligand pubchem chembl_ligand pubchem
Agonist 3.3 Active 10.1038/S41422-023-00914-Z 2024-01-24
9GE3 GPR55 GPR55 GPR18, GPR55 and GPR119 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 1-palmitoyl-2-lysoph...
Agonist 2.9 Active 2025-03-05
8GFY 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 c-Epi pubchem
Agonist 3.0 Active 10.1038/S41586-024-07153-1 2024-03-06
6MXT 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 CHEMBL230056 chembl_ligand pubchem
Agonist (partial) 3.0 Active 10.1038/s41589-018-0145-x 2018-11-14
9P82 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 NTS8–13 pubchem
Agonist 2.4 Active 10.1038/S41586-026-10120-7 2026-03-25
5V56 SMO SMO Oxysterol 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 TC114 pubchem
Antagonist 2.9 Inactive 10.1038/NCOMMS15383 2017-05-24
5WS3 OX2R OX2 Orexin A (Rhodopsin) Human BaculovirusSf9Insect 9 chemicals 9 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 4 chems 5.8-6.2 20°C EMPA pubchem gtoplig chembl_ligand
Antagonist 2.3 Inactive 10.1016/J.STR.2017.11.005 2017-12-13
7YXA S1PR5 S1P5 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 CHEMBL6059624 chembl_ligand pubchem pubchem
Inverse agonist 2.2 Inactive 10.1038/S41467-022-32447-1 2022-08-10
9JCP GPR4 GPR4 Proton 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 Lysophosphatidylchol... pubchem
PAM 2.6 Active 2025-07-09
8H4I FFAR4 FFA4 Free fatty 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 docosahexaenoic acid pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.1 Active 10.1038/S41422-023-00835-X 2023-06-21
7DW9 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 (Human) pubchem gtoplig chembl_ligand drugbank drug_central uniprot uniprot uniprot pubchem
Agonist 2.6 Active 10.1038/S41422-021-00480-2 2021-07-21
22ES OPRK κ 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 difelikefalin pubchem gtoplig chembl_ligand drugbank
Agonist 2.4 Active 2026-05-06
8WWH MCHR1 MCH1 Melanin-concentrating 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 Apo (no ligand)
2.8 Active 2024-11-13
8IRS 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 rotigotine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.0 Active 10.1038/S41422-023-00808-0 2023-06-07
8YN4 HRH2 H2 Histamine 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 histamine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.0 Active 10.1038/S41467-024-52585-Y 2024-10-09
7IP2 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 (4-(trifluoromethoxy... drugbank pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.1 Inactive 2026-05-20
8Z3M GPR4 GPR4 Proton 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)
2.9 Active 2025-04-23
8XJM PF2R FP 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 latanoprost (free ac... pubchem gtoplig chembl_ligand
Agonist 2.9 Active 10.1016/J.CELREP.2024.113893 2024-02-28
3AYM OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Japanese flying squid NANativeSquid 1 chemicals 1 steps vapour diffusionsitting drop 5 chems 6.6-6.6 4°C all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 2.8 Inactive 10.1016/J.JMB.2011.08.044 2011-08-17
9K25 P2RY2 P2Y2 P2Y 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)
3.3 Active 10.1038/S41421-025-00797-X 2025-06-11
9K1D FFAR2 FFA2 Free fatty 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 Cholesterol pubchem drugbank
butyric acid pubchem gtoplig chembl_ligand drugbank chembl_ligand pubchem chembl_ligand pubchem
PAMAgonist 3.3 Active 10.1016/J.CELREP.2024.115024 2024-12-11
7D7M 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 PGE2 pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.3 Active 10.1016/J.STR.2020.11.007 2020-11-18
9EBH AA3R A3 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 3.6 Active 10.1038/S41467-025-62872-X 2025-08-20
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 angiotensin II (Huma... pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank
Agonist 2.9 Active 10.1126/SCIENCE.AAY9813 2020-02-19
7YOO 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 NEUROPEPTIDE-Y chembl_ligand pubchem
Agonist 3.1 Active 10.1016/J.STR.2022.11.010 2023-03-22
8WGB 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-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem pubchem drugbank
VU0155041 pubchem gtoplig chembl_ligand
AgonistPAM 3.7 Active 10.1038/S41467-024-54744-7 2024-10-30
9QC1 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 cp28a pubchem
Agonist 3.1 Inactive 2026-02-11
9W1J NK2R NK2 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 neurokinin A (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 3.0 Active 2026-06-17
9UPU CXCR4 CXCR4 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 SDV1a
Agonist 2.8 Active 10.1101/2025.07.08.663251 2026-04-29
8A2P 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 CHEMBL1671936 chembl_ligand pubchem
Antagonist 3.5 Inactive 10.1107/S1600576723006428 2023-08-30
8IUK PF2R FP 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 PGF<sub>2&alpha;</su... pubchem gtoplig chembl_ligand drug_central pubchem drugbank drugbank
Agonist 2.7 Active 10.1038/S41467-023-38411-X 2023-07-12
9ODK OPRM μ Opioid 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 Apo (no ligand)
3.9 Active 10.1038/S41586-025-10056-4 2026-01-07
2Y04 ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 1 chemicals 1 steps vapour diffusionsitting drops 6 chems 9.0-9.0 4°C levosalbutamol pubchem gtoplig chembl_ligand drug_central drugbank
Agonist (partial) 3.1 Inactive 2011-01-12
6TPN 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 HTL6641 pubchem gtoplig chembl_ligand
Antagonist 2.6 Inactive 10.1021/acs.jmedchem.9b01787 2020-01-01
8Y6Y FFAR2 FFA2 Free fatty 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 GLPG0974 pubchem gtoplig chembl_ligand drugbank
Allosteric antagonist 3.4 Active 2025-04-02
9EGO CNR1 CB1 Cannabinoid 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 methyl (2R)-2-({(1M)... pubchem
Agonist 3.2 Active 10.1038/S41467-025-57136-7 2025-04-30
9J05 P2Y14 P2Y14 P2Y 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)
3.2 Active 2025-08-06
9M1P Q5QNQ1 taar13d Unclassified A (Rhodopsin) Zebrafish N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A histamine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 2.8 Active 2026-03-04
8JHI FZD3 FZD3 WNT 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)
3.2 Active 2024-01-17
9GL2 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 Befiradol pubchem chembl_ligand
Phosphatidylinositol...
AgonistPAM 3.2 Active 10.1126/SCIADV.ADV9267 2025-07-02
8GGM 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 c-Epi pubchem
Agonist 3.2 Active 10.1038/S41586-024-07153-1 2024-03-06
9JMC MTLR motilin Motilin 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 DS-3801b free base pubchem gtoplig chembl_ligand
Agonist 2.6 Active 2025-05-28
9JIC HCAR3 HCA3 Hydroxycarboxylic 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 Apo (no ligand)
3.4 Active 10.1016/J.CELREP.2024.114895 2025-12-17
8TF5 GPR6 GPR6 Orphan 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 oleic acid pubchem gtoplig chembl_ligand drug_central pubchem drugbank
Agonist 2.1 Active 10.1126/SCISIGNAL.ADO8741 2024-12-04
11TK CCR4 CCR4 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 AZD2098 pubchem gtoplig chembl_ligand
Antagonist 3.5 Inactive 2026-04-01
8ZCE GPR4 GPR4 Proton 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)
3.1 Active 10.1038/S41422-025-01092-W 2025-04-23
4U16 ACM3 M3 Acetylcholine (muscarinic) A (Rhodopsin) Rat BaculovirusSf9Insect 9 chemicals 9 steps sponge mesophaselipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 7.5-7.5 298 K METHSCOPOLAMINE chembl_ligand pubchem pubchem drugbank drugbank drug_central chembl_ligand
Antagonist 3.7 Inactive 10.1016/J.STR.2014.08.022 2014-11-26
7Y36 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 PTH pubchem
Agonist 2.8 Active 2023-07-05
9GE2 GPR55 GPR55 GPR18, GPR55 and GPR119 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 CID2440433 pubchem gtoplig chembl_ligand
Agonist 2.5 Active 2025-03-05
6W25 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 SHU9119 pubchem
Antagonist 2.8 Inactive 10.1126/SCIENCE.AAZ8995 2020-04-29
8GGK 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 c-Epi pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06
7LD3 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
MIPS521 pubchem gtoplig chembl_ligand
AgonistPAM 3.2 Active 10.1038/S41586-021-03897-2 2021-09-08
7JHJ Q3KSP2 BILF1 Unclassified A (Rhodopsin) HHV-4 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)
3.2 Active 10.1016/J.IMMUNI.2021.06.001 2021-07-07
7O7F 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 [6P4]CCL5
Agonist 3.2 Active 10.1126/SCIADV.ABG8685 2021-06-30
4DKL OPRM μ Opioid A (Rhodopsin) Mouse BaculovirusSf9Insect 12 chemicals 12 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 7.0-7.0 20°C beta-funaltrexamine pubchem
Antagonist 2.8 Inactive 10.1038/NATURE10954 2012-03-21
5WKT OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drop 4 chems 5.5-5.5 7-10°C Apo (no ligand)
3.2 Active 10.1038/NPROT.2017.135 2017-12-13
4MBS CCR5 CCR5 Chemokine 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 MARAVIROC chembl_ligand pubchem drugbank
Inverse agonist 2.7 Inactive 10.1126/SCIENCE.1241475 2013-09-11
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
7W56 NMUR1 NMU1 Neuromedin U 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 Neuromedin-S
Agonist 2.9 Active 10.1038/S41467-022-29683-W 2022-04-20
8ZVZ PD2R DP1 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 CHEMBL1591294 chembl_ligand pubchem pubchem
Agonist 2.4 Active 2025-05-28
7IPB 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
FU336-34 pubchem
AntagonistUnknown 2.1 Inactive 2026-05-20
9MET CXCR4 CXCR4 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 HIV-2/gp120
T-cell surface glyco...
AgonistAgonist 5.7 Inactive 2025-09-10
9BLB 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 Cagrilintide backbon...
Agonist 3.2 Active 10.1038/S41467-025-58680-Y 2025-04-16
7ZBC OPSD Rhodopsin Opsin (sight) 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 all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Inverse agonist 1.8 Inactive 10.1038/S41586-023-05863-6 2023-03-29
6LFM 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
Agonist 3.5 Active 10.1038/S41586-020-2492-5 2020-09-02
8W8B 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 ulotaront pubchem gtoplig chembl_ligand drugbank
Agonist 3.0 Active 10.1038/S41586-023-06775-1 2023-11-22
7VGY 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 pubchem
Agonist 3.1 Active 10.1038/S41467-022-28111-3 2022-03-02
7SIL 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 tecalcet pubchem gtoplig chembl_ligand
CYCLOMETHYLTRYPTOPHA... pubchem
Calcium pubchem
PAMAgonistAgonist 2.7 Active 10.1073/PNAS.2115849118 2022-01-19
8YNT MCHR1 MCH1 Melanin-concentrating 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 CHEMBL242004 chembl_ligand pubchem
Antagonist 3.4 Inactive 2024-12-18
8XIQ SSR3 SST3 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 L-796,778 pubchem gtoplig chembl_ligand pubchem
Agonist 2.7 Active 2024-07-03
9UWM 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 cagrilintide pubchem gtoplig drugbank
Agonist 3.1 Active 10.1038/S41401-025-01635-2 2026-05-27
8XGO KISSR kisspeptin Kisspeptin 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 TAK448
Agonist 2.7 Active 10.1126/SCIADV.ADN7771 2024-10-30
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 Active 10.1038/NATURE22309 2017-05-03
6DDE 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 pubchem
Agonist 3.5 Active 10.1038/S41586-018-0219-7 2018-06-13
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 Muscarinic toxin 7
CHEMBL1379091 chembl_ligand pubchem chembl_ligand pubchem chembl_ligand pubchem
NAMAntagonist 2.6 Inactive 10.1126/SCIENCE.AAX2517 2020-07-08
3PDS ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 3 chemicals 3 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 6.7-6.7 20°C FAUC50 pubchem
Agonist 3.5 Inactive 10.1038/NATURE09665 2011-01-12
9WST OPRM μ Opioid 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 DAMGO pubchem gtoplig chembl_ligand pubchem
Agonist 2.8 Active 10.1038/S41422-025-01191-8 2025-11-26
8JCV 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
Antagonist 3.4 Inactive 10.1038/S41422-023-00830-2 2023-06-21
4QKX ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)7.7 MAG 5 chems 7.8-8.4 20°C Compound 2 (covalent... pubchem
Agonist 3.3 Active 10.1073/PNAS.1410415111 2014-07-23
9E82 ACKR3 ACKR3 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 SDF-1-beta(3-72)
Agonist 3.4 Active 10.1038/S41586-025-09024-9 2025-04-02
8XBG GPR34 GPR34 Orphan 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 CHEMBL4782438 chembl_ligand pubchem
Agonist 3.4 Active 10.1038/S41467-024-45046-Z 2024-05-15
8JT6 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 (R)-IHCH-7179 pubchem
Agonist 3.0 Active 10.1016/J.CELL.2024.02.034 2024-02-28
3KJ6 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 3 chemicals 3 steps vapour diffusionbicelles 5 chems 7.5-7.5 298K Apo (no ligand)
3.4 Inactive 10.1038/NATURE08650 2010-02-16
8IHI HCAR2 HCA2 Hydroxycarboxylic 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 Acifran pubchem
Agonist 3.1 Active 10.1038/S41467-023-41650-7 2023-08-30
9LLZ GRM6 mGlu6 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
Agonist 3.2 Active 2026-03-18
9X3Y MAS MAS1 Orphan 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 neuropeptide FF (Hum... pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 2.8 Intermediate 10.1038/S44318-026-00764-6 2026-04-15
8XVH 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-1 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 3.3 Active 10.1038/S41421-024-00705-9 2024-08-28
7EUO 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 fMet-Leu-Phe pubchem gtoplig chembl_ligand
Agonist 2.9 Active 10.1038/S41467-022-32822-Y 2022-05-25
9HC3 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 Apo (no ligand)
2.9 Inactive 10.1002/PRO.70104 2025-06-25
7IOA 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
FU35-5 (N-phenyl-1H-... pubchem
AntagonistUnknown 2.1 Inactive 2026-05-20
9RHG FZD7 FZD7 WNT 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 C407 pubchem
NAM 2.5 Inactive 2025-12-24
8JD3 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 chembl_ligand pubchem pubchem drugbank
JNJ-40411813 pubchem gtoplig chembl_ligand drugbank
AgonistPAM 3.3 Active 10.1038/S41422-023-00830-2 2023-06-21
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 ICI118551 pubchem gtoplig chembl_ligand
Inverse agonist 2.8 Inactive 10.1021/JA105108Q 2010-08-11
8YKV SUCR1 succinate Succinate 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 31 [PMID: 2... pubchem gtoplig chembl_ligand pubchem
Agonist 2.5 Active 2024-05-29
8FLU 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... pubchem
Agonist 2.8 Active 10.1016/J.STR.2023.04.002 2023-04-26
7X1U TRFR TRH1 Thyrotropin-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 TRH (Human) pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank pubchem
Agonist 3.2 Active 10.1038/S41422-022-00646-6 2022-08-31
8V6U 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 Z7757 pubchem
Agonist 3.0 Active 10.1126/SCIENCE.ADN6354 2024-05-29
9WQL 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 L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem pubchem drugbank
CDPPB pubchem gtoplig chembl_ligand
AgonistPAM 3.2 Active 10.1126/SCIADV.AEE0044 2026-05-27
9UPV CXCR4 CXCR4 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 SDV1a
Agonist 2.7 Active 10.1101/2025.07.08.663251 2026-04-29
8Y72 OPRM μ 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 BMS-986122 pubchem
DAMGO pubchem gtoplig chembl_ligand pubchem
PAMAgonist 2.7 Active 10.1126/SCIADV.AEA9832 2025-08-06
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
9LRB HRH1 H1 Histamine 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 histamine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 2.8 Active 10.1038/S42003-025-08363-7 2025-06-11
9KUW 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 cmpd644 pubchem
Agonist 3.5 Active 2025-09-17
9UMR C5AR1 C5a1 Complement peptide 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 C5a-pep
Agonist 3.2 Active 10.1101/2025.05.26.656101 2025-11-26
8W87 TAAR1 TA1 Trace amine 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 METHAMPHETAMINE chembl_ligand pubchem drugbank drug_central
Agonist 2.8 Active 10.1038/S41586-023-06775-1 2023-11-22
7VDL MRGX2 MRGPRX2 Orphan 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 chembl_ligand pubchem
Agonist 3.2 Active 10.1038/S41586-021-04077-Y 2021-12-01
7VV5 MRGX2 MRGPRX2 Orphan 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 10.1038/S41586-021-04077-Y 2021-12-01
8QJ2 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 pN162
Agonist 3.4 Active 2024-09-25
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)
2.9 Active 10.1038/S41589-021-00918-Z 2022-03-23
27XK 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 Glucagon-like peptid... pubchem
Agonist 2.6 Active 2026-07-01
8JT8 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 (R)-IHCH-7179 pubchem
Antagonist 2.7 Inactive 10.1016/J.CELL.2024.02.034 2024-02-28
7DTY 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 Gastric inhibitory p... pubchem
Agonist 3.0 Active 10.7554/ELIFE.68719 2021-08-04
5V54 5HT1B 5-HT1B 5-Hydroxytryptamine A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 7 chems 7.0-7.0 20°C CHEMBL428892 chembl_ligand pubchem
Antagonist 3.9 Inactive 2018-02-07
9BTW 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 cagrilintide pubchem gtoplig drugbank
Agonist 3.0 Active 10.1038/S41467-025-58680-Y 2025-04-16
8GG0 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 c-Epi pubchem
Agonist 2.9 Active 10.1038/S41586-024-07153-1 2024-03-06
4ZUD AGTR1 AT1 Angiotensin A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 5.0-5.0 20°C OLMESARTAN chembl_ligand pubchem drugbank
Inverse agonist 2.8 Inactive 10.1074/JBC.M115.689000 2015-10-07
8XXU 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 Apo (no ligand)
2.5 Active 2024-12-04
9UVU 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 N/A N/A 3.7 Inactive 2026-05-06
8TR2 GRM3 mGlu3 Metabotropic glutamate C (Glutamate) Rat N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A LY379268 pubchem
Agonist 3.5 Active 10.1101/2023.08.13.552748 2024-07-31
9UMX C5AR1 C5a1 Complement peptide 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 EP54
Agonist 3.2 Active 10.1101/2025.05.26.656101 2025-11-26
9E7R PAR2 PAR2 Proteinase-activated 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 GB88 pubchem
Agonist (partial) 3.2 Active 2025-05-07
4XNW P2RY1 P2Y1 P2Y 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 MRS2500 pubchem gtoplig chembl_ligand
Antagonist 2.7 Active 10.1038/NATURE14287 2015-04-01
9W0W T2R46 TAS2R46 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A strychnine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.2 Active 10.1038/S41594-026-01786-8 2026-04-22
9LW5 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 dopamine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.9 Active 2026-02-18
8ZWF C3AR C3a Complement peptide 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 JR14a pubchem gtoplig chembl_ligand
Agonist 3.0 Active 2025-05-14
8IYS FFAR4 FFA4 Free fatty 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 TUG-891 pubchem gtoplig chembl_ligand
Agonist 3.0 Active 10.1038/S41422-023-00835-X 2023-06-21
6G79 5HT1B 5-HT1B 5-Hydroxytryptamine A (Rhodopsin) Human BaculovirusTni PRO (Trichoplusia ni) cell linesInsect 1 chemicals 1 steps Cryo-EMVolta phase plate, Falcon III detector (FEI Titan Krios, 300kV) 5 chems 7.5-7.5 4°C donitriptan pubchem gtoplig chembl_ligand pubchem
Agonist 3.8 Active 10.1038/S41586-018-0241-9 2018-06-20
8WJX P2RY1 P2Y1 P2Y 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 ADP pubchem gtoplig chembl_ligand
Agonist 3.2 Active 2024-10-02
9W3F 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 BERBERINE chembl_ligand pubchem drugbank
Antagonist 3.0 Inactive 10.1038/S41421-026-00892-7 2026-06-10
7IN2 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 Apo (no ligand)
2.4 Inactive 10.1038/S42004-026-02059-7 2026-05-20
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
Antagonist 3.1 Inactive 10.1038/S41467-020-20221-0 2020-12-30
8YRG MRGX4 MRGPRX4 Orphan 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 Fospropofol pubchem drugbank
Agonist 3.1 Active 2024-05-22
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 orforglipron pubchem gtoplig chembl_ligand drugbank
Compound 2 pubchem
AgonistAgo-PAM 2.9 Active 10.1038/S41467-021-24058-Z 2021-07-07
7SBF OPRM μ Opioid 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 PZM21 pubchem gtoplig chembl_ligand drugbank
Agonist (partial) 2.9 Active 10.1002/ANIE.202200269 2022-04-20
8XQR T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A flufenamic acid pubchem gtoplig chembl_ligand drugbank drug_central
Allosteric agonist 3.2 Active 10.1038/S41586-024-07569-9 2024-07-10
7YDJ AGRE5 ADGRE5 ADGRE 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 Apo (no ligand)
3.0 Active 2023-07-12
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 PtdIns4P pubchem
Cholesterol pubchem drugbank
PAMPAM 3.0 Active 10.1038/S41586-021-03376-8 2021-04-14
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
Antagonist 2.5 Inactive 10.1038/S41589-018-0170-9 2018-12-19
8XQJ 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...
Antagonist 3.0 Inactive 10.1038/S41467-024-55555-6 2025-01-22
9WSV OPRM μ Opioid 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 DAMGO pubchem gtoplig chembl_ligand pubchem
Agonist 2.8 Active 10.1038/S41422-025-01191-8 2025-11-26
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
Inverse agonist 3.3 Inactive 10.1016/J.STR.2011.06.014 2011-09-07
8FYT 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 (+)-LSD pubchem gtoplig pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.6 Active 10.1038/S41586-024-07403-2 2024-05-15
9KO2 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 CCL19
Agonist 3.0 Active 2025-11-26
8WC9 TAAR1 TA1 Trace amine 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 CHEMBL476516 chembl_ligand pubchem
Agonist 3.2 Active 10.1016/J.CELL.2023.10.014 2023-12-27
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
Agonist 2.9 Active 10.1038/S41589-018-0171-8 2018-12-05
8DU3 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 CHEMBL5206530 chembl_ligand pubchem
Antagonist 2.5 Inactive 10.1016/j.ejmech.2022.114620 2022-08-10
8JWY 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 CHEMBL5440290 chembl_ligand pubchem
Antagonist 2.3 Inactive 2023-08-16
9AS2 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 dimethyltryptamine pubchem gtoplig chembl_ligand drugbank
Agonist 3.2 Active 2025-04-02
8JLN TAAR1 TA1 Trace amine 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 CHEMBL1182312 chembl_ligand pubchem
Agonist 3.2 Active 10.1038/S41586-023-06804-Z 2023-11-15
7W0P 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 Elabela/Toddler-32 (... pubchem gtoplig uniprot
Agonist 3.2 Active 10.1038/S41594-022-00797-5 2022-07-27
2I36 OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine NANativeBovine 2 chemicals 2 steps vapour diffusionsitting drops 5 chems 7.0-8.0 5°C Apo (no ligand)
4.1 Inactive 2006-10-17
8GFX 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 c-Epi pubchem
Agonist 3.0 Active 10.1038/S41586-024-07153-1 2024-03-06
8XWA 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 CXCL1
Agonist 3.5 Active 10.1016/J.MOLCEL.2025.01.024 2025-01-15
2J4Y OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine Transient_transfectionCOS1Mammalian 1 chemicals 1 steps vapour diffusionsitting drops 3 chems 7.5-7.5 4°C all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Inverse agonist 3.4 Inactive 10.1016/J.JMB.2007.03.007 2007-09-25
5X93 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 K-8794 pubchem gtoplig
Antagonist 2.2 Inactive 10.1038/NSMB.3450 2017-08-16
9LZ1 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... pubchem
Agonist 3.2 Active 2026-03-11
9IJD ADRB3 β3 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 (S)-carazolol pubchem drugbank
Agonist 2.8 Active 10.1002/CPLU.202400288 2024-08-21
8QOT OPRM μ Opioid 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 Nanobody E (NbE)
Antagonist 3.2 Inactive 10.1101/2023.12.06.570395 2023-12-27
8XOS PAR1 PAR1 Proteinase-activated 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 3.2 Active 2024-09-18
9HYI 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 DP81 pubchem
Agonist 2.3 Active 2026-01-21
5V57 SMO SMO Oxysterol 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 TC114 pubchem
Antagonist 3.0 Inactive 10.1038/NCOMMS15383 2017-05-24
9MNI 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 dC2_050
Antagonist 4.1 Inactive 10.1101/2025.03.23.644666 2025-10-22
7IPE 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 FU428-8
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 1.8 Inactive 2026-05-20
5DYS OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine Stable_cellsHEK293S-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionSitting drop 4 chems 4.5-4.5 20°C all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 2.3 Active 10.15252/EMBR.201642671 2016-08-10
9UGL 5HT2C 5-HT2C 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 SB 242084 pubchem gtoplig chembl_ligand
Antagonist 2.7 Inactive 2026-04-15
8GE2 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 c-Epi pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06
6FK7 OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine BaculovirusHEK293S(TetR)-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 4.5-4.5 20°C RS06 pubchem
Agonist 2.6 Active 10.1073/PNAS.1718084115 2018-04-04
9KB8 LGR4 LGR4 Orphan 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 ZNRF3
R-spondin-2
UnknownAgonist 3.3 Inactive 10.1038/S41467-025-64129-Z 2025-10-15
8XXH 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 CXCL2
Agonist 2.8 Active 10.1016/J.MOLCEL.2025.01.024 2025-01-15
6AKX 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 CHEMBL4238063 chembl_ligand pubchem
Allosteric antagonist 2.8 Inactive 10.1021/acs.jmedchem.8b01077 2018-10-24
7W6P 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 CHEMBL5542553 chembl_ligand pubchem
Agonist (partial) 3.5 Active 10.1126/SCIENCE.ABN7065 2022-09-28
9LWC 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 (-)-adrenaline pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.9 Active 2026-02-18
7IOW 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 FU163-106 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.2 Inactive 2026-05-20
9VMY 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 TMU4142 pubchem
Agonist 2.9 Active 2025-11-12
9VAW 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
Agonist 2.2 Active 10.1038/S41586-026-10228-W 2026-06-03
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
5W0P OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Human Transient_transfectionHEK293S(TetR- GnTI-Mammalian 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monopalmitolein (9.7 MAG) 5 chems 5.0-5.0 20°C Apo (no ligand)
3.0 Active 10.1016/J.CELL.2017.07.002 2017-08-09
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 CHEMBL3937413 chembl_ligand pubchem
Antagonist 1.9 Inactive 10.1021/acs.jmedchem.6b00653 2016-06-29
7WUQ AGRG2 ADGRG2 ADGRG B2 (Adhesion) Mouse 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)
2.9 Active 10.1038/S41586-022-04590-8 2022-04-27
4Z9G CRHR1 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 23°C CP 376,395 pubchem gtoplig chembl_ligand
Antagonist 3.2 Inactive 10.2174/1874467210666170110114727 2016-06-29
9OXB T2R43 TAS2R43 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A aristolochic acid pubchem gtoplig chembl_ligand
Agonist 3.0 Active 10.1038/S41594-026-01776-W 2026-04-22
9BHM GPR68 GPR68 Proton 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)
2.9 Active 10.1016/J.CELL.2024.11.036 2025-01-22
2I35 OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine NANativeBovine 2 chemicals 2 steps vapour diffusionsitting drops 5 chems 7.0-8.0 5°C all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Inverse agonist 3.8 Inactive 10.1073/PNAS.0608022103 2006-10-17
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 gtoplig drugbank
Agonist 2.5 Active 10.1016/J.CELREP.2021.109374 2021-08-04
8IKG CNR1 CB1 Cannabinoid 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 CB-02 pubchem
Allosteric agonist 3.4 Active 10.1073/PNAS.2321532121 2024-06-05
7T9I TSHR TSH 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 Thyrotropin subunit ...
Glycoprotein hormone...
AgonistAgonist 2.9 Active 10.1038/S41586-022-05159-1 2022-08-03
9KGK LGR4 LGR4 Orphan 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)
2.6 Inactive 2025-07-16
6ME5 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 agomelatine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.2 Inactive 10.1038/S41586-019-1141-3 2019-04-24
7XKD AGRG2 ADGRG2 ADGRG B2 (Adhesion) Mouse N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A PRASTERONE chembl_ligand pubchem drugbank
Agonist (partial) 2.4 Active 10.1038/S41589-022-01084-6 2022-08-10
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... uniprot
Agonist 3.3 Active 10.1038/S41586-018-0535-Y 2018-09-19
4WW3 OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Japanese flying squid NANativeSquid 1 chemicals 1 steps vapour diffusionsitting drop 4 chems 6.4-6.4 100-170 K all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 2.8 Inactive 10.1371/JOURNAL.PONE.0126970 2015-06-17
9JVH GPR4 GPR4 Proton 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 Apo (no ligand)
2.8 Active 10.1016/J.CELL.2024.12.001 2025-02-26
9W32 SSR5 SST5 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 CHEMBL4063587 chembl_ligand pubchem
Antagonist 2.6 Inactive 2026-01-21
8WWK MCHR1 MCH1 Melanin-concentrating 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 melanin-concentratin... pubchem gtoplig uniprot uniprot uniprot
Agonist 2.6 Active 10.1038/S41421-024-00754-0 2024-11-13
20ZJ 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
Agonist 2.9 Active 10.1038/S41586-026-10228-W 2026-06-03
8T3Q FFAR4 FFA4 Free fatty 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 docosahexaenoic acid pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.1 Active 10.1126/SCIADV.ADJ2384 2024-01-24
8YYX OXGR1 oxoglutarate Oxoglutarate 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 LTE4 pubchem gtoplig chembl_ligand
Allosteric agonist 2.8 Active 2025-04-09
9DQJ MRGRD MRGPRD Orphan 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 EP-3945 pubchem
Agonist 2.9 Active 2024-12-11
8UO0 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 c-Epi pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
7T32 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 3.4 Inactive 10.1038/S41467-022-32125-2 2022-08-10
7W3Z GRPR BB2 Bombesin 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 Gastrin Releasing Pe...
Agonist 3.0 Active 10.1073/PNAS.2216230120 2023-02-22
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 CHEMBL3697578 chembl_ligand pubchem
Agonist 3.2 Active 10.1016/J.CELL.2021.01.028 2021-03-03
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
Agonist 3.0 Active 10.1038/S41586-019-1337-6 2019-07-10
7WVX 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 fhumanin
Agonist 2.8 Active 10.1038/S41467-022-29361-X 2022-04-13
8J23 FFAR2 FFA2 Free fatty 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 Apo (no ligand)
3.2 Active 2024-04-17
4MQT ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 7.2-7.9 20°C iperoxo pubchem gtoplig chembl_ligand
LY2119620 pubchem gtoplig chembl_ligand
AgonistAgo-PAM 3.7 Active 10.1038/NATURE12735 2013-11-27
7FIY 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 tirzepatide pubchem gtoplig
Agonist 3.4 Active 10.1038/S41467-022-28683-0 2022-03-02
9DYD 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 (3aS,12bR)-asenapine pubchem
PtdIns4P pubchem
Agonist (partial)PAM 3.0 Active 2025-08-13
8XX3 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 CXCL3
Agonist 3.4 Active 10.1016/J.MOLCEL.2025.01.024 2025-01-15
9YDU P2Y14 P2Y14 P2Y 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 UDP-glucose pubchem gtoplig chembl_ligand drugbank
Agonist 3.2 Active 10.1038/S42003-025-09174-6 2025-11-19
8WVW LGR4 LGR4 Orphan 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)
3.5 Inactive 2024-10-30
7XTB 5HT6R 5-HT6 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 3.3 Active 10.1016/J.MOLCEL.2022.05.031 2022-07-27
8IHK HCAR3 HCA3 Hydroxycarboxylic 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 Acifran pubchem
Agonist 3.2 Active 10.1038/S41467-023-41650-7 2023-08-30
9H2X 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 Compound 7 pubchem
Inverse agonist 1.8 Inactive 2025-06-18
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
8ZMF 5HT2C 5-HT2C 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 CHEMBL5575992 chembl_ligand pubchem pubchem
Inverse agonist 3.6 Inactive 2024-08-28
6PEL OPSD Rhodopsin Opsin (sight) 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 Citronellol pubchem
Agonist 3.2 Active 2020-06-24
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 Glycoprotein hormone...
Choriogonadotropin s...
AgonistAgonist 3.9 Active 10.1038/S41586-021-03924-2 2021-09-29
9AS3 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 (+)-LSD pubchem gtoplig pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.2 Active 10.1038/S41467-025-57956-7 2025-04-02
9UTB TS1R2 TAS1R2 Taste 1 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 Sucralose drugbank pubchem
Agonist 3.6 Active 10.1038/S41586-025-09302-6 2025-07-16
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 Tuberoinfundibular p...
Agonist 2.8 Active 10.1073/PNAS.2101279118 2021-08-18
8YN7 HRH3 H3 Histamine 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 immethridine pubchem gtoplig chembl_ligand
Agonist 2.8 Active 2024-10-16
8GE6 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 c-Epi pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
9UVY 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 CHEMBL4303142 chembl_ligand pubchem drugbank chembl_ligand
Antagonist 3.0 Inactive 2026-05-06
9K3F MC3R MC3 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 Apo (no ligand)
2.8 Active 10.1016/J.STR.2025.03.004 2025-08-06
7WU4 AGRF1 ADGRF1 ADGRF 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 LPC 16:0
PAM 3.4 Active 10.1038/S41586-022-04580-W 2022-04-27
9FTE AGRV1 ADGRV1 ADGRV B2 (Adhesion) Mouse 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)
3.8 Inactive 2026-01-14
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 rat amylin pubchem
Agonist 2.6 Active 10.1126/SCIENCE.ABM9609 2022-03-30
6PGS OPSD Rhodopsin Opsin (sight) 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 drugbank pubchem
Agonist 2.9 Active 2020-07-01
9PA1 OPRK κ 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 PHENCYCLIDINE chembl_ligand pubchem drugbank pubchem drug_central
Agonist (partial) 2.6 Active 10.1038/S41594-026-01839-Y 2026-07-01
7XN9 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 L-054,522 pubchem gtoplig chembl_ligand
Agonist 2.6 Inactive 10.1038/S41422-022-00679-X 2022-08-03
8WVY LGR4 LGR4 Orphan 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 Norrin
Agonist 3.3 Inactive 2024-10-30
8THL ADA1A α1A 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 (-)-adrenaline pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.1 Active 10.1038/S41467-023-40524-2 2023-08-16
3DQB OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionhanging drops 5 chems 5.9-6.1 10°C Apo (no ligand)
3.2 Active 10.1038/NATURE07330 2008-09-23
9U81 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 Tolvaptan pubchem
Antagonist 3.1 Inactive 2025-12-10
5U09 CNR1 CB1 Cannabinoid A (Rhodopsin) Human BaculovirusSf21Insect 9 chemicals 9 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 5.5-5.5 20°C taranabant pubchem gtoplig chembl_ligand drugbank
Inverse agonist 2.6 Inactive 10.1038/NATURE20613 2016-12-07
8XVI EDNRA ETA 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-1 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 3.3 Active 10.1038/S41421-024-00705-9 2024-08-28
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
9UCP 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 iperoxo pubchem gtoplig chembl_ligand
Nanobody Nb1B4
AgonistAllosteric agonist 2.9 Active 10.1073/PNAS.2508879122 2025-10-29
8HJ2 GPR21 GPR21 Orphan 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)
3.8 Active 10.1038/S41467-023-35882-W 2023-03-15
2X72 OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine Stable_cellsHEK293S-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionsitting drop 3 chems 4.5-4.5 4°C all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 3.0 Active 10.1038/NATURE09795 2011-03-16
7XJK GALR2 GAL2 Galanin 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 galanin(1-13)amide gtoplig pubchem
Agonist 3.3 Active 10.1073/PNAS.2121465119 2022-06-29
5OLZ 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 1.9 Inactive 10.1038/S41598-017-18570-W 2018-01-17
9OXA T2R43 TAS2R43 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A aristolochic acid pubchem gtoplig chembl_ligand
Agonist 2.9 Active 10.1038/S41594-026-01776-W 2026-04-22
9JFY NPFF2 NPFF2 Neuropeptide FF/neuropeptide AF 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 Neuropeptide SF pubchem
Agonist 3.2 Active 10.1038/S44319-025-00428-2 2025-04-09
7DB6 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 10.1038/S41594-021-00634-1 2021-08-18
7EZH 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 (Human) pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank pubchem
Agonist 3.2 Active 10.1038/S41589-021-00841-3 2021-08-25
7TUY GP183 GPR183 Orphan 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 GSK682753A pubchem gtoplig
Inverse agonist 3.0 Active 10.1016/J.STR.2022.04.006 2022-04-13
9LQU 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 Apo (no ligand)
2.7 Inactive 2026-02-04
7XZ6 GP119 GPR119 GPR18, GPR55 and GPR119 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 APD668 pubchem gtoplig chembl_ligand
Agonist 2.8 Active 10.1038/S41594-022-00816-5 2022-08-24
9UYI CML2 chemerin 2 Chemerin receptor 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 Chemerin
Agonist 3.2 Active 10.1126/SCIENCE.ADT8794 2025-11-19
9W2G NK2R NK2 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 EB1001
Agonist 3.4 Active 2026-06-17
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
9LLA 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 Ariadne pubchem
Agonist 3.3 Active 2026-01-14
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
Antagonist 3.7 Inactive 10.1038/S41422-022-00623-Z 2022-03-16
8GUQ CNR2 CB2 Cannabinoid 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 olorinab pubchem gtoplig chembl_ligand drugbank
Agonist 3.1 Active 10.1038/S41467-023-37112-9 2023-05-10
8HK5 C5AR1 C5a1 Complement peptide 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 [<sup>125</sup>I]C5a... gtoplig
Agonist 3.0 Active 10.1038/S41589-023-01339-W 2023-05-10
7TRQ ACM4 M4 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
VU0467154 pubchem gtoplig chembl_ligand
AgonistPAM 2.5 Active 2023-05-17
8T1V GPR6 GPR6 Orphan 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 CHEMBL4763822 chembl_ligand pubchem
Inverse agonist 2.6 Inactive 10.1126/SCISIGNAL.ADO8741 2024-12-04
7XAU 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 octreotide pubchem gtoplig chembl_ligand drugbank pubchem pubchem
Agonist 3.0 Active 10.1038/S41421-022-00405-2 2022-08-31
9LXR 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... pubchem
Agonist 3.1 Active 2025-09-10
7WU2 AGRD1 ADGRD1 ADGRD 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 Apo (no ligand)
2.8 Active 10.1038/S41586-022-04580-W 2022-04-27
7IOU 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 FU163-75 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.2 Inactive 2026-05-20
8UUJ HCAR2 HCA2 Hydroxycarboxylic acid 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 compound (+)17a [PMI... pubchem gtoplig chembl_ligand chembl_ligand pubchem pubchem
Agonist 2.6 Active 10.1016/J.CELL.2024.11.001 2025-02-26
9IJS GPR52 GPR52 Orphan 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)
3.6 Active 10.1038/S41422-025-01165-W 2025-09-03
8UYQ OR4D5 OR4D5 Olfactory family 4 O2 (Olfactory/extra-nasal 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 2-methylthiazoline pubchem
Agonist 3.5 Active 10.1038/S41586-024-08126-0 2024-10-30
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
8H8J GPR35 GPR35 Orphan 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 lodoxamide pubchem gtoplig chembl_ligand drug_central drugbank
Calcium pubchem
AgonistPAM 3.2 Active 10.1038/S41421-022-00499-8 2023-02-08
25NV 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 SPT
Agonist 3.2 Active 2026-06-03
8IBV MTLR motilin Motilin 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 motilin (Human) pubchem gtoplig chembl_ligand uniprot uniprot
Agonist 3.2 Active 10.1126/SCIADV.ADE9020 2023-04-12
7VIH 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 icanbelimod pubchem gtoplig chembl_ligand
Agonist 3.0 Active 10.1073/PNAS.2117716119 2022-09-28
8JSP 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 ulotaront pubchem gtoplig chembl_ligand drugbank
Agonist 3.7 Active 10.1038/S41586-023-06804-Z 2023-11-15
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 gtoplig chembl_ligand uniprot drug_central pubchem
Agonist 3.3 Active 10.1126/SCIENCE.ABM9609 2022-03-23
8GGR 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 c-Epi pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
9I3T OPSG OPN1MW Opsin (sight) 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 all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Inverse agonist 3.7 Inactive 10.1126/SCIENCE.ADZ3624 2026-06-24
6DS0 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 LY266097 pubchem
Agonist (partial) 3.2 Active 10.1038/s41594-018-0116-7 2018-08-29
7VIG 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 icanbelimod pubchem gtoplig chembl_ligand
Agonist 2.9 Active 10.1073/PNAS.2117716119 2022-09-28
9P93 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 Vasoactive intestina... pubchem
Agonist 3.2 Active 10.1073/PNAS.2521157122 2025-11-19
9JLC MAS MAS1 Orphan 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 AVE 0991 pubchem gtoplig chembl_ligand
Agonist 3.0 Active 2025-09-24
8Z3Q GPR4 GPR4 Proton 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)
2.8 Active 2025-04-23
8J6D C3AR C3a Complement peptide 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 E7 pubchem gtoplig gtoplig
Agonist 3.1 Active 10.1016/J.CELL.2023.09.020 2023-10-18
6Z4Q 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 SR142948A pubchem gtoplig chembl_ligand
Inverse agonist 2.9 Inactive 10.1126/sciadv.abe5504 2021-02-10
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 Inactive 10.1038/S41589-018-0170-9 2018-12-19
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
7V69 ACM4 M4 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 Apo (no ligand)
3.4 Active 10.1038/S41467-022-30595-Y 2022-05-11
9W0H 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 SPM-242 pubchem
Cpd-32
AntagonistAllosteric antagonist 3.0 Inactive 2026-06-03
7EW1 S1PR5 S1P5 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 3.4 Active 10.1038/S41422-021-00566-X 2021-09-29
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 (+)-LSD pubchem gtoplig pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.6 Inactive 10.1126/SCIENCE.ABL8615 2022-01-26
9MD1 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 PtdIns4P pubchem
buspirone pubchem gtoplig chembl_ligand drugbank drug_central
PAMAgonist 3.0 Active 10.1126/SCIADV.ADU9851 2025-08-13
8IEQ GP156 GPR156 Orphan 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 PC 34:1 pubchem
Agonist 2.7 Active 2024-02-14
9JFZ GPR4 GPR4 Proton 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)
2.9 Active 10.1038/S41422-025-01092-W 2025-04-23
9IYA GPR55 GPR55 GPR18, GPR55 and GPR119 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-9710531 pubchem
Inverse agonist 3.0 Active 2025-01-01
5ZTY CNR2 CB2 Cannabinoid 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 AM10257 pubchem gtoplig chembl_ligand
Inverse agonist 2.8 Inactive 10.1016/J.CELL.2018.12.011 2019-01-30
6IBB SUCR1 succinate Succinate 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)
2.1 Active 10.1038/S41586-019-1663-8 2019-08-14
7EJX GPR88 GPR88 Orphan 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 2 [PMID: 24... pubchem gtoplig chembl_ligand
Allosteric agonist 2.4 Active 10.1038/S41467-022-30081-5 2022-04-13
9B9Y CNR1 CB1 Cannabinoid 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 taranabant pubchem gtoplig chembl_ligand drugbank
Inverse agonist 3.5 Inactive 10.1038/S41467-024-54206-0 2024-11-20
8JIQ 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 Peptide 15 (P15)
Agonist 3.4 Active 10.1073/PNAS.2303696120 2023-09-13
9VB1 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
Agonist 3.3 Active 10.1038/S41586-026-10228-W 2026-06-03
8P15 OPSD Rhodopsin Opsin (sight) 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)
5.9 Active 2024-11-20
8XQN T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A aristolochic acid pubchem gtoplig chembl_ligand
Cholesterol pubchem drugbank
Allosteric agonistAgonist 3.1 Active 10.1038/S41586-024-07569-9 2024-07-10
8ZF7 GPR4 GPR4 Proton A (Rhodopsin) Western clawed frog 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)
3.2 Active 10.1016/J.CELL.2024.12.001 2025-02-26
8JLQ TAAR1 TA1 Trace amine 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 fenoldopam pubchem gtoplig chembl_ligand drugbank drug_central pubchem gtoplig chembl_ligand pubchem gtoplig
Agonist 2.8 Active 10.1038/S41586-023-06804-Z 2023-11-15
9PLN 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 N-(5-methylnaphthale... pubchem
Agonist 2.8 Active 2025-08-20
7WU5 AGRF1 ADGRF1 ADGRF 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 LPC 16:0
Allosteric agonist 3.0 Active 10.1038/S41586-022-04580-W 2022-04-27
8HMP GPR52 GPR52 Orphan 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 derivative 17 [Nakah... pubchem gtoplig chembl_ligand
Allosteric agonist 2.8 Active 10.1002/MCO2.260 2023-06-21
8ZSV TAAR1 TA1 Trace amine 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 RO5256390 pubchem gtoplig chembl_ligand
Agonist (partial) 3.0 Active 2024-07-24
9VMN OXGR1 oxoglutarate Oxoglutarate 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 &alpha;-ketoglutaric... pubchem gtoplig chembl_ligand drugbank
Agonist 2.6 Active 10.1016/J.CELL.2026.01.036 2026-03-18
8XQO T2R14 TAS2R14 Taste 2 T2 (Taste 2) 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 drugbank
aristolochic acid pubchem gtoplig chembl_ligand
AgonistAllosteric agonist 2.8 Active 10.1038/S41586-024-07569-9 2024-07-10
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
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
9JKT HCAR3 HCA3 Hydroxycarboxylic 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 D-phenyllactic acid pubchem gtoplig drugbank pubchem
Agonist 3.1 Active 10.1371/JOURNAL.PBIO.3003480 2025-10-29
7IOG 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
FU99-89 pubchem
AntagonistUnknown 2.0 Inactive 2026-05-20
9JKX HCAR3 HCA3 Hydroxycarboxylic 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 Acifran pubchem
Agonist 3.2 Active 10.1371/JOURNAL.PBIO.3003480 2025-10-29
9LLB 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 DOI-NBOMe pubchem
Agonist 3.0 Active 2026-01-14
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
9UXX OPRK κ 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 salvinorin A pubchem gtoplig chembl_ligand chembl_ligand pubchem chembl_ligand pubchem chembl_ligand pubchem drugbank
Agonist 3.6 Active 2026-05-27
24TB 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 Apo (no ligand)
3.0 Active 10.1093/PROCEL/PWAG016 2026-07-08
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 pubchem
Agonist 3.5 Active 10.1038/S41586-018-0219-7 2018-06-13
9I54 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 Compound 24 pubchem
Agonist 2.7 Active 2025-07-16
9P1T 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 3.2 Inactive 10.1038/S42004-025-01825-3 2025-12-24
9AS9 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 RS130-180 pubchem
Agonist 3.5 Active 2025-04-02
8XGS KISSR kisspeptin Kisspeptin 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 Metastin (KP54) pubchem
Agonist 3.0 Active 10.1126/SCIADV.ADN7771 2024-10-30
7XOU 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 (Human) pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank pubchem
Agonist 3.2 Active 10.1038/S41421-022-00420-3 2022-07-20
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
8X9S AGRD1 ADGRD1 ADGRD 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 dihydrotestosterone pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.5 Active 10.1016/J.CELL.2025.01.006 2025-02-12
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 PACAP-27 (Human) pubchem gtoplig uniprot uniprot uniprot uniprot pubchem
Agonist 3.2 Active 10.1038/S41467-020-17933-8 2020-09-02
9MQH OPRM μ 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 Apo (no ligand)
3.9 Inactive 10.1101/2025.01.09.632033 2025-02-12
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
Agonist 3.4 Active 10.1038/S41586-020-2492-5 2020-09-02
9PXU OPRM μ 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 naloxone pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem
Agonist (partial) 3.4 Inactive 2025-11-12
8X0D 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
VU0424465 pubchem gtoplig chembl_ligand
AgonistAgo-PAM 3.5 Active 10.1038/S41467-024-55439-9 2024-11-06
8UO1 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 c-Epi pubchem
Agonist 3.6 Active 10.1038/S41586-024-07153-1 2024-03-06
9AXF 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
tecalcet pubchem gtoplig chembl_ligand
CYCLOMETHYLTRYPTOPHA... pubchem
AgonistPAMAgonist 3.5 Active 10.1038/S41586-024-07331-1 2024-04-17
6WPW 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 Glucagon derivative ...
Agonist 3.1 Active 10.1126/SCIENCE.ABA3373 2020-08-12
8IHB HCAR2 HCA2 Hydroxycarboxylic 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 GSK256073 pubchem gtoplig
Agonist 2.9 Active 10.1038/S41467-023-41650-7 2023-09-13
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 drugbank
Agonist 2.6 Inactive 10.1038/NATURE09746 2011-01-12
9XF4 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 [Leu]enkephalin (Hum... pubchem gtoplig chembl_ligand uniprot uniprot uniprot pubchem
BMS-986187 pubchem gtoplig chembl_ligand
AgonistAgo-PAM 3.1 Active 2026-07-08
9L3W CML1 chemerin Chemerin receptor 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 Chemerin
Agonist 3.5 Active 10.1093/PROCEL/PWAE073 2025-03-12
9VBA 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
Agonist 3.4 Active 10.1038/S41586-026-10228-W 2026-06-03
8T3O FFAR4 FFA4 Free fatty 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 TUG-891 pubchem gtoplig chembl_ligand
Agonist 3.1 Active 10.1126/SCIADV.ADJ2384 2024-01-17
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 (Human) pubchem gtoplig chembl_ligand drugbank drug_central uniprot uniprot uniprot pubchem
Agonist 2.8 Active 10.1038/S41422-021-00483-Z 2021-05-26
6WQA 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 10.1107/S2052252520012701 2020-11-18
7Y67 C5AR1 C5a1 Complement peptide 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 C089
Agonist 2.8 Active 10.1038/S41422-023-00779-2 2023-03-01
8JPS ACKR1 ACKR1 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 CCL7
Agonist 3.7 Intermediate 10.1016/J.CELL.2024.07.005 2024-07-31
9JGK 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 balovaptan pubchem gtoplig chembl_ligand drugbank
Antagonist 3.6 Inactive 2025-07-16
9EJC VGPCR ORF74 Unclassified A (Rhodopsin) isolate GK18 N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CXCL1
Agonist 3.0 Active 10.1038/S41467-025-63457-4 2025-09-03
8DWC MRGX1 MRGPRX1 Orphan 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 bovine adrenal medul... pubchem gtoplig chembl_ligand uniprot
Agonist 2.9 Active 2022-11-02
7XJJ GALR1 GAL1 Galanin 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 galanin(1-13)amide gtoplig pubchem
Agonist 3.3 Active 2023-05-03
8GFV 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 c-Epi pubchem
Agonist 3.1 Active 10.1038/S41586-024-07153-1 2024-03-06
9P85 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 NTS8–13 pubchem
Agonist 3.0 Active 10.1038/S41586-026-10120-7 2026-03-25
6TQ7 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-334867 pubchem gtoplig chembl_ligand
Antagonist 2.7 Inactive 10.1021/acs.jmedchem.9b01787 2020-01-01
7JJO 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 LEVISOPRENALINE chembl_ligand pubchem drug_central
Agonist 2.6 Active 10.1016/J.MOLCEL.2020.08.001 2020-09-02
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
3P0G ADRB2 β2 Adrenoceptors 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 CHEMBL1615159 chembl_ligand pubchem
Agonist 3.5 Active 10.1038/NATURE09648 2011-01-19
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
7XRR 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 lemborexant pubchem gtoplig chembl_ligand drug_central drugbank
Antagonist 2.9 Inactive 10.1016/J.STR.2022.11.001 2022-11-23
9IZH 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 LPA pubchem
Agonist 3.0 Active 10.1016/J.JSB.2024.108164 2025-01-01
8U4R CXCR4 CXCR4 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 REGN7663 Fab (chain ...
REGN7663 Fab (chain ...
Inverse agonistInverse agonist 3.1 Inactive 10.1038/S41594-024-01397-1 2024-03-13
8FN1 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 NTS8–13 pubchem
Agonist 2.9 Active 10.1021/ACS.BIOCHEM.3C00029 2023-03-29
8E0G OPRM μ Opioid 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 BU72, modelled as co...
Agonist 2.1 Active 2023-10-18
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 CHEMBL5433301 chembl_ligand pubchem
Allosteric antagonist 2.1 Inactive 10.1016/J.CELL.2019.07.028 2019-09-04
9LRE HRH4 H4 Histamine 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 histamine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 2.8 Active 10.1038/S42003-025-08363-7 2025-06-11
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 (S)-carazolol pubchem drugbank
Inverse agonist 3.2 Inactive 10.1038/NPROT.2017.057 2016-08-17
6LI0 GPR52 GPR52 Orphan 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 derivative 17 [Nakah... pubchem gtoplig chembl_ligand
Allosteric agonist 2.2 Inactive 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 rat amylin pubchem
Agonist 2.4 Active 10.1126/SCIENCE.ABM9609 2022-03-23
8X5X HRH1 H1 Histamine 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)
3.5 Inactive 10.1038/S41467-023-44477-4 2024-01-17
9UWI V1AR V1A 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 N/A N/A 2.8 Inactive 2026-01-28
7V9L 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 Apo (no ligand)
2.6 Active 10.1073/PNAS.2106606118 2022-04-06
8GEH 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 c-Epi pubchem
Agonist 4.0 Active 10.1038/S41586-024-07153-1 2024-03-06
7INE 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
3,4-dihydro-1H-quino... pubchem
AntagonistUnknown 2.3 Inactive 10.1038/S42004-026-02059-7 2026-05-20
9H37 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 Compound 9 pubchem
Inverse agonist 1.7 Inactive 2025-06-18
7VDH MRGX2 MRGPRX2 Orphan 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 2.9 Active 10.1038/S41586-021-04077-Y 2021-12-01
9JKY HCAR2 HCA2 Hydroxycarboxylic 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 Acifran pubchem
Agonist 2.7 Active 10.1371/JOURNAL.PBIO.3003480 2025-10-29
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 Fab4A03 (chain H)
SI pubchem
Fab4A03 (chain L)
PAMAgonistPAM 3.2 Active 10.1038/S41594-018-0079-8 2018-07-11
27TM GRM1 mGlu1 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 chembl_ligand pubchem pubchem drugbank
Ro0711401 pubchem gtoplig chembl_ligand
AgonistPAM 3.2 Active 2026-06-24
9JED HRH4 H4 Histamine 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 histamine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 2.6 Active 10.1038/S41401-025-01633-4 2025-09-10
8RQL T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A flufenamic acid pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.0 Active 10.1038/S41467-024-54157-6 2024-11-27
8WPG 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 D-tryptophan pubchem gtoplig chembl_ligand drugbank pubchem gtoplig chembl_ligand drugbank drug_central
Calcium pubchem
cinacalcet pubchem gtoplig chembl_ligand drugbank drug_central
AgonistAgonistPAM 2.7 Active 10.1038/S41422-023-00892-2 2023-11-22
7V35 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 Peptide 20
Agonist 3.4 Active 10.1038/S41467-022-28683-0 2022-03-02
7Y13 MRGRD MRGPRD Orphan 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)
3.1 Intermediate 10.1038/S42003-022-03668-3 2022-07-20
9UWJ V1AR V1A 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 balovaptan pubchem gtoplig chembl_ligand drugbank
Antagonist 3.0 Inactive 2026-02-04
9M0J BRS3 BB3 Bombesin 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 oridonin pubchem
Agonist 2.9 Active 2026-03-04
7IP1 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 FU235-66 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.3 Inactive 2026-05-20
7IN9 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 CHEMBL2164538 chembl_ligand pubchem
Antagonist 2.5 Inactive 2026-05-20
9JG0 NPFF2 NPFF2 Neuropeptide FF/neuropeptide AF 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)
2.9 Inactive 10.1038/S44319-025-00428-2 2025-04-09
8K3Z CXCR4 CXCR4 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 CXCL12
Agonist 2.8 Active 2024-07-17
7INP 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
2-[(5-CHLORO-2-PYRID... pubchem
AntagonistUnknown 2.2 Inactive 10.1038/S42004-026-02059-7 2026-05-20
8ZFC GPR4 GPR4 Proton 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 Apo (no ligand)
2.7 Active 10.1016/J.CELL.2024.12.001 2025-02-26
9VPM 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 N/A N/A 4.0 Active 2026-07-08
8UNV 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 c-Epi pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06
8ZW0 PD2R DP1 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 PGD2 pubchem gtoplig chembl_ligand drugbank
Agonist 2.7 Active 10.1073/PNAS.2501902122 2025-05-28
7RGP 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 gtoplig
Agonist 2.9 Active 10.1073/PNAS.2116506119 2022-04-13
6OIJ 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 iperoxo pubchem gtoplig chembl_ligand
Agonist 3.3 Active 10.1126/SCIENCE.AAW5188 2019-05-08
9VMP OXGR1 oxoglutarate Oxoglutarate 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 A-1 pubchem
Agonist 2.5 Active 2026-03-18
7XBD GALR2 GAL2 Galanin 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 galanin(1-13)amide gtoplig pubchem
Agonist 3.1 Active 10.1371/JOURNAL.PBIO.3001714 2022-07-13
5WIU DRD4 D4 Dopamine A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 5 chems 5.8-6.2 20°C nemonapride drug_central pubchem
Antagonist 2.0 Inactive 10.1126/science.aan5468 2017-10-18
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
Inverse agonist 2.0 Inactive 10.1038/S41598-020-76277-X 2020-11-25
7DGE GRM1 mGlu1 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 Nanobody 43
quisqualate pubchem gtoplig chembl_ligand drugbank
PAMAgonist 3.7 Intermediate 10.1007/S13238-020-00808-5 2021-09-22
8XBI GPR34 GPR34 Orphan 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 CHEMBL4758243 chembl_ligand pubchem
Agonist 3.1 Active 2023-12-27
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
Nanobody DN13
AgonistPAM 3.1 Active 10.1038/S41586-021-03641-W 2021-06-23
3VGA AA2AR A2A Adenosine A (Rhodopsin) Human P.pastorisP. pastoris SMD1163Yeast 2 chemicals 2 steps vapour diffusionhanging drop 4 chems 6.5-6.5 20°C Fab2838 (chain C)
Fab2838 (chain B)
ZM-241385 pubchem gtoplig chembl_ligand drugbank
Inverse agonistInverse agonistAntagonist 3.1 Inactive 10.1038/NATURE10750 2012-02-01
7XV3 GP174 GPR174 Orphan 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 LysoPS(18:0)
Agonist 2.8 Active 10.1038/S41467-023-36575-0 2023-02-15
8JRV 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 Glucagon pubchem
Agonist 3.3 Active 10.1038/S41586-023-06420-X 2023-08-16
7RM5 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 2.8 Inactive 10.1073/PNAS.2106041118 2021-09-08
7WIC 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 drugbank drug_central pubchem
Agonist 2.8 Active 10.1038/S41422-022-00669-Z 2022-06-01
9UYP GRM6 mGlu6 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
Agonist 3.5 Active 2026-03-18
9IJ9 T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A compound 28.1 [PMID:... pubchem gtoplig chembl_ligand
Allosteric agonist 2.7 Active 2024-07-24
10TL OPRM μ 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 DAMGO pubchem gtoplig chembl_ligand pubchem
BMS-986187 pubchem gtoplig chembl_ligand
AgonistPAM 3.5 Active 2026-05-27
6C1R C5AR1 C5a1 Complement peptide A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 6.5-6.5 10°C PMX53 pubchem gtoplig chembl_ligand
avacopan pubchem gtoplig drugbank chembl_ligand
AntagonistAllosteric antagonist 2.2 Inactive 10.1038/S41594-018-0067-Z 2018-05-30
9IPY C3AR C3a Complement peptide 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 JR14a pubchem gtoplig chembl_ligand
Agonist 3.5 Inactive 2025-04-23
12IZ CNR2 CB2 Cannabinoid 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 '5249 pubchem
Agonist 2.7 Active 2026-07-15
11TD CCR4 CCR4 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)
3.7 Inactive 2026-04-01
7IP9 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 FU336-22 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.1 Inactive 2026-05-20
9LQW 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 Apo (no ligand)
2.7 Inactive 2026-02-04
6HLO 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 2.4 Inactive 10.1038/S41467-018-07939-8 2019-01-16
9DYF 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 PtdIns4P pubchem
(3aS,12bR)-asenapine pubchem
PAMAgonist (partial) 2.7 Active 2025-08-13
8DPG 5HT2C 5-HT2C 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 (partial) 3.6 Active 10.1016/J.CELREP.2022.111211 2022-08-24
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
Allosteric antagonist 2.8 Inactive 10.1021/acs.jmedchem.8b01077 2018-10-24
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 chembl_ligand pubchem chembl_ligand pubchem drugbank
Antagonist 3.0 Active 10.1073/PNAS.2116289119 2022-02-09
9V3C C5AR2 C5a2 Complement peptide 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 [<sup>125</sup>I]C5a... gtoplig
Agonist 3.8 Active 10.1016/J.MOLCEL.2026.06.002 2026-07-01
7S8M MRGX2 MRGPRX2 Orphan 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 chembl_ligand pubchem
Agonist 2.5 Active 10.1038/S41586-021-04126-6 2021-11-17
8JZ7 HCAR2 HCA2 Hydroxycarboxylic 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 MK 6892 pubchem gtoplig chembl_ligand pubchem
Agonist 2.6 Active 10.1038/S41392-023-01625-Y 2023-10-04
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 LEVISOPRENALINE chembl_ligand pubchem drug_central
Agonist 3.8 Active 10.1093/NSR/NWAA284 2020-12-16
6ZDR 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 CHEMBL2030687 chembl_ligand pubchem
Antagonist 1.9 Inactive 10.1002/ANIE.202003788 2020-09-16
8Y71 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 BMS-986187 pubchem gtoplig chembl_ligand
SNC80 pubchem
PAMAgonist 3.0 Active 2026-01-07
7C61 5HT1B 5-HT1B 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 ergotamine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.0 Inactive 10.1038/S41598-020-68355-X 2020-07-29
8K4O VGPCR ORF74 Unclassified A (Rhodopsin) isolate GK18 N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CXCL1
Agonist 3.0 Active 2024-07-24
9IYB 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 PGD2 pubchem gtoplig chembl_ligand drugbank
Agonist 2.8 Active 2024-12-04
7VVK 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 PTH pubchem
Agonist 3.3 Active 10.1016/J.MOLCEL.2022.07.003 2022-08-03
6XBM SMO SMO Oxysterol 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 24(S),25-Epoxycholes... pubchem
Agonist 3.2 Active 10.1038/S41589-020-0646-2 2020-09-30
8J22 FFAR2 FFA2 Free fatty 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 CHEMBL4176503 chembl_ligand pubchem
Agonist 3.2 Active 10.1038/S41422-023-00914-Z 2024-01-24
7DD5 A0A8I3AZV5 CaS Calcium-sensing C (Glutamate) Chicken 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
D-tryptophan pubchem gtoplig chembl_ligand drugbank pubchem gtoplig chembl_ligand drugbank drug_central
Calcium pubchem
NAMAgonistAgonist 3.2 Inactive 10.1126/SCIADV.ABG1483 2021-06-16
8ZD1 GPR4 GPR4 Proton A (Rhodopsin) Western clawed frog 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)
2.6 Active 10.1016/J.CELL.2024.12.001 2025-02-26
8I9L C3AR C3a Complement peptide 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 C3a anaphylatoxin
Agonist 3.2 Active 10.1016/J.CELL.2023.09.020 2023-10-18
7Y3G GPR12 GPR12 Orphan 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)
2.8 Active 10.1016/J.SCIB.2022.12.023 2023-06-07
8K4P VGPCR ORF74 Unclassified A (Rhodopsin) isolate GK18 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)
2.8 Active 2024-07-24
8WVX LGR4 LGR4 Orphan 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 Norrin
Agonist 3.3 Inactive 2024-10-30
9QXL AGRL4 ADGRL4 ADGRL 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 Apo (no ligand)
3.1 Active 10.1038/S41467-025-67629-0 2026-01-14
9LM0 GRM6 mGlu6 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)
3.8 Inactive 2026-03-18
8GDC 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
Agonist 3.5 Active 10.1073/PNAS.2216329120 2024-01-10
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 chembl_ligand pubchem pubchem drugbank
ADX55164 pubchem
AgonistAgo-PAM 3.3 Active 10.1038/S41586-021-03680-3 2021-07-07
9LE1 OR6A2 OR6A2 Olfactory family 6 O2 (Olfactory/extra-nasal 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (E)-dec-2-enal pubchem
Agonist 3.3 Active 2026-01-28
8UNR 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 c-Epi pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
8IW4 TAAR9 TAAR9 Orphan 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 SPERMIDINE chembl_ligand pubchem drugbank
Agonist 3.5 Active 10.1038/S41586-023-06106-4 2023-05-31
9XHH 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 C-C motif chemokine ...
Agonist 3.0 Active 10.1073/PNAS.2533975123 2026-04-22
7SQO 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 danavorexton pubchem gtoplig chembl_ligand drugbank
Agonist 3.2 Active 10.1038/S41467-022-30601-3 2022-05-25
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
Inverse agonist 3.7 Inactive 10.1038/NCHEMBIO.2547 2018-01-03
7INA 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-{[5-(trifluorometh... pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.2 Inactive 2026-05-20
6BQG 5HT2C 5-HT2C 5-Hydroxytryptamine A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 5 chems 6.0-6.0 20°C ergotamine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.0 Active 10.1016/j.cell.2018.01.001 2018-02-14
9PY4 OPRM μ 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 loperamide pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.8 Active 2025-11-12
7Y26 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 octreotide pubchem gtoplig chembl_ligand drugbank pubchem pubchem
Agonist 3.3 Active 10.1038/S41589-022-01130-3 2022-10-19
7XTC 5HT7R 5-HT7 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-CT pubchem gtoplig chembl_ligand
Agonist 3.2 Active 10.1016/J.MOLCEL.2022.05.031 2022-07-27
8JXS 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 CHEMBL4277264 chembl_ligand pubchem
Agonist 3.0 Active 10.1016/J.NEURON.2024.07.003 2024-09-04
7RKF US28 US28 Unclassified A (Rhodopsin) strain AD169 N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Fractalkine
Agonist 4.0 Active 10.1126/SCIADV.ABL5442 2022-01-26
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
7DFL HRH1 H1 Histamine 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 histamine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.3 Active 10.1038/S41467-021-22427-2 2021-03-31
7EXD 5HT1F 5-HT1F 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 lasmiditan pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.4 Active 10.1038/S41422-021-00527-4 2021-08-04
8J6Q HCAR2 HCA2 Hydroxycarboxylic 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 &beta;-D-hydroxybuty... pubchem gtoplig chembl_ligand
compound 9n [PMID: 1... pubchem gtoplig chembl_ligand
AgonistAgo-PAM 2.6 Active 10.1038/S41467-023-43537-Z 2023-12-06
6LPB 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 PACAP-38 pubchem
Agonist 3.9 Active 10.1038/S41594-020-0386-8 2020-03-11
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 nemonapride drug_central pubchem
Na+ pubchem
AntagonistNAM 2.1 Inactive 10.1126/science.aan5468 2017-10-18
6B73 OPRK κ Opioid A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 7 chems 6.5-7.0 20°C CHEMBL5431513 chembl_ligand pubchem
Agonist 3.1 Active 10.1016/J.CELL.2017.12.011 2018-01-17
9D4Z PAR1 PAR1 Proteinase-activated 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 2.7 Active 10.1038/S41467-025-59138-X 2025-05-07
8GGI 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 c-Epi pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
8VHF GP119 GPR119 GPR18, GPR55 and GPR119 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 MBX-2982 pubchem gtoplig chembl_ligand drugbank
Agonist 3.5 Active 2024-10-30
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 GHRH (Human) pubchem gtoplig uniprot
Agonist 3.3 Active 10.1073/PNAS.2106606118 2021-10-20
7C7S 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 CGP 54626A pubchem gtoplig chembl_ligand
Antagonist 2.9 Inactive 10.1038/S41422-020-0350-5 2020-07-01
9EAJ 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 Nanobody AT206
PAM 3.2 Inactive 10.1073/PNAS.2423931122 2025-03-05
6VI4 OPRK κ 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 Nanobody 6
JDTic pubchem gtoplig chembl_ligand chembl_ligand pubchem chembl_ligand pubchem
NAMInverse agonist 3.3 Inactive 10.1038/S41467-020-14889-7 2020-03-18
4PXZ P2Y12 P2Y12 P2Y A (Rhodopsin) Human BaculovirusSf9Insect 6 chemicals 6 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 5.0-6.0 20°C 2MeSADP pubchem gtoplig chembl_ligand
Agonist 2.5 Active 10.1038/NATURE13288 2014-04-30
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 chembl_ligand drug_central pubchem
Agonist 2.6 Active 10.1126/SCIENCE.ABM9609 2022-03-30
23IW CNR1 CB1 Cannabinoid 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 LZD503 pubchem
Agonist 2.4 Active 2026-05-20
7W53 NMUR1 NMU1 Neuromedin U 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 CHEMBL3315349 chembl_ligand pubchem
Agonist 3.2 Active 10.1038/S41467-022-29683-W 2022-04-20
8WKY 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 PG-934
Antagonist 2.9 Inactive 10.1021/acs.jmedchem.3c01822 2024-08-07
8JIR 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-hexadecanoyl-L-glu... pubchem
SAR425899 pubchem
AgonistAgonist 2.6 Active 10.1073/PNAS.2303696120 2023-09-06
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
5UIW CCR5 CCR5 Chemokine A (Rhodopsin) Human BaculovirusSf21Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 6.3-6.3 20°C [5P7]CCL5
Antagonist 2.2 Inactive 10.1016/J.IMMUNI.2017.05.002 2017-06-28
7VUJ GP139 GPR139 Orphan 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 3.8 Active 10.1038/S41422-021-00591-W 2021-12-29
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 chembl_ligand pubchem drugbank pubchem pubchem
Antagonist 2.8 Inactive 10.1016/J.STR.2014.08.022 2014-11-26
8G94 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 Early activation ant...
Allosteric agonist 3.2 Active 10.7554/ELIFE.88204 2023-04-19
9P83 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 NTS8–13 pubchem
Agonist 3.2 Active 10.1038/S41586-026-10120-7 2026-03-25
8XZG 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 apelin-13 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 3.2 Active 10.1016/J.CELL.2024.02.004 2024-03-27
8JHB FZD6 FZD6 WNT 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)
3.3 Active 10.1038/S41421-023-00627-Y 2024-01-17
8YFO 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 Ac-LA-PTH
Agonist 2.7 Active 2025-09-03
8XZJ 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 WN353
Agonist 3.0 Active 10.1016/J.CELL.2024.02.004 2024-03-20
6E59 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 L760735 pubchem gtoplig
Antagonist 3.4 Inactive 10.1073/PNAS.1812717115 2018-12-12
3NY9 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 CHEMBL1233771 chembl_ligand pubchem
Inverse agonist 2.8 Inactive 10.1021/JA105108Q 2010-08-11
8JLO TAAR1 TA1 Trace amine 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 ulotaront pubchem gtoplig chembl_ligand drugbank
Agonist 3.5 Active 10.1038/S41586-023-06804-Z 2023-11-15
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 chembl_ligand pubchem
Agonist 2.6 Active 10.1124/mol.114.097360 2015-04-08
6K42 ADA2B α2B 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 dexmedetomidine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 4.1 Active 10.1038/S41589-020-0492-2 2020-04-15
6E67 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 CHEMBL1615159 chembl_ligand pubchem
Agonist 3.7 Active 10.1016/J.CELL.2019.04.021 2019-06-05
7UTZ TSHR TSH 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 TR1402 (chain B)
DPPC pubchem
TR1402 (chain A)
AgonistPAMAgonist 2.4 Active 10.1038/S41586-022-05159-1 2022-08-03
9WXM GPR15 GPR15 Orphan 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 GPR15LG
Agonist 3.3 Active 10.1016/J.ISCI.2025.113935 2025-11-19
7M3F 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 cinacalcet pubchem gtoplig chembl_ligand drugbank drug_central
D-tryptophan pubchem gtoplig chembl_ligand drugbank pubchem gtoplig chembl_ligand drugbank drug_central
Calcium pubchem
PAMPAMAgonist 2.8 Active 10.1038/S41586-021-03691-0 2021-06-30
9L74 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 d16:1 S1P pubchem
Agonist 3.7 Active 2025-11-26
7C6A 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
Agonist (partial) 3.4 Active 10.1038/S41598-020-68355-X 2020-07-29
7XKE AGRG2 ADGRG2 ADGRG B2 (Adhesion) Mouse N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A PRASTERONE chembl_ligand pubchem drugbank
Agonist 2.9 Active 10.1038/S41589-022-01084-6 2022-08-10
8XGR 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-1 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 3.2 Active 2024-04-03
9MZF 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 Peptide 15
Agonist 2.5 Active 2026-04-22
9UVZ LPAR2 LPA2 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 Ki16425 pubchem
Antagonist 3.0 Inactive 2026-05-06
25IL MAS MAS1 Orphan 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)
3.2 Active 10.1016/J.JMB.2026.169844 2026-05-20
10TM OPRM μ 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 DAMGO pubchem gtoplig chembl_ligand pubchem
Agonist 3.0 Active 2026-05-27
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
6KPF CNR2 CB2 Cannabinoid 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 AM12033 pubchem
Agonist 2.9 Active 10.1016/J.CELL.2020.01.008 2020-02-12
8WPU 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 D-tryptophan pubchem gtoplig chembl_ligand drugbank pubchem gtoplig chembl_ligand drugbank drug_central
cinacalcet pubchem gtoplig chembl_ligand drugbank drug_central
Calcium pubchem
AgonistPAMAgonist 3.1 Active 10.1038/S41422-023-00892-2 2023-11-22
4UHR AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusHi5Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 4 chems 4.8-4.8 22°C CGS 21680 pubchem gtoplig chembl_ligand chembl_ligand pubchem
Agonist 2.6 Active 10.1124/mol.114.097360 2015-04-08
9P7Z 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 NTS8–13 pubchem
Agonist 2.1 Active 10.1038/S41586-026-10120-7 2026-03-25
7WUJ AGRG4 ADGRG4 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 N/A N/A 3.3 Active 10.1038/S41586-022-04590-8 2022-04-27
8I7W HCAR2 HCA2 Hydroxycarboxylic 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 GSK256073 pubchem gtoplig
Agonist 3.4 Active 10.1038/S41467-023-42764-8 2024-02-07
7IP5 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 FU293-69 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.0 Inactive 2026-05-20
5ZKC 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 METHSCOPOLAMINE chembl_ligand pubchem pubchem drugbank drugbank drug_central chembl_ligand
Inverse agonist 2.3 Inactive 10.1038/S41589-018-0152-Y 2018-11-21
9XDQ 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 BMS-986187 pubchem gtoplig chembl_ligand
Ago-PAM 2.8 Active 2026-07-08
7ZI0 SMO SMO Oxysterol 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 SAG1.3 pubchem gtoplig chembl_ligand
Cholesterol pubchem drugbank
Allosteric agonistAgonist 3.0 Inactive 10.1126/SCIADV.ABM5563 2022-06-15
9IQS ACM4 M4 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 muscarinic toxin 3 gtoplig uniprot
Antagonist 3.6 Inactive 10.1038/S41467-025-61695-0 2025-07-23
8J19 GPR84 GPR84 Orphan 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 6-nonylpyridine-2,4-... pubchem gtoplig chembl_ligand
Agonist 3.2 Active 10.1038/S41467-023-38985-6 2023-06-21
8GGP 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 c-Epi pubchem
Agonist 3.2 Active 10.1038/S41586-024-07153-1 2024-03-06
8GGY 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 c-Epi pubchem
Agonist 3.9 Active 10.1038/S41586-024-07153-1 2024-03-06
8K6M 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 NEUROPEPTIDE-Y chembl_ligand pubchem
Agonist 3.3 Active 2024-07-31
8JCX 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
Antagonist 3.0 Inactive 10.1038/S41422-023-00830-2 2023-06-21
9MQI OPRM μ 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 #020_E1 pubchem
Antagonist 3.3 Inactive 2025-02-12
8GG4 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 c-Epi pubchem
Agonist 3.2 Active 10.1038/S41586-024-07153-1 2024-03-06
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 NAM597 pubchem
NAM 2.7 Inactive 10.1038/S41586-021-03641-W 2021-06-23
9KZ8 C3AR C3a Complement peptide 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 EP67
Agonist 3.3 Active 10.1073/PNAS.2614459123 2025-11-26
7TD2 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 LPA pubchem
Agonist 3.1 Active 10.1038/S41467-022-28417-2 2022-02-09
8RWH 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 StilSwitch2 pubchem
Antagonist 2.5 Inactive 2025-01-08
8IJD HCAR2 HCA2 Hydroxycarboxylic 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 MK 6892 pubchem gtoplig chembl_ligand pubchem
Agonist 3.3 Active 10.1038/S41421-023-00610-7 2024-01-03
9W0M S1PR2 S1P2 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 Apo (no ligand)
3.8 Active 10.1093/PROCEL/PWAF068 2026-06-03
7F1T 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 N/A N/A 2.6 Inactive 2021-07-14
9IZC HCAR2 HCA2 Hydroxycarboxylic 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 CHEMBL2057618 chembl_ligand pubchem
Agonist 2.7 Active 10.1371/JOURNAL.PBIO.3003126 2025-04-02
8W8W MC3R MC3 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 Alpha-MSH pubchem
Agonist 2.9 Active 2025-03-19
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
Allosteric antagonist 2.5 Inactive 10.1038/NATURE17414 2016-04-20
7YM8 ADA1A α1A 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 Nanobody 29 (Nb29)
oxymetazoline pubchem gtoplig chembl_ligand drugbank drug_central
PAMAgonist (partial) 2.9 Active 10.1038/S41467-023-39310-X 2023-07-05
9L16 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 CCL21
Agonist 3.5 Active 2025-12-17
9W3L GP151 GPR151 Orphan 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)
2.8 Inactive 10.1073/PNAS.2534234123 2026-05-06
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
7FIJ 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 Apo (no ligand)
3.8 Inactive 10.1038/S41586-021-03924-2 2021-09-29
5YQZ GLR glucagon Glucagon B1 (Secretin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)MAG 7.8 5 chems 8.0-8.0 20°C NNC1702 gtoplig
Agonist (partial) 3.0 Inactive 10.1038/NATURE25153 2018-01-17
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
Agonist 3.2 Active 10.1038/NATURE12572 2013-09-25
8ZPT PRLHR PrRP Prolactin-releasing peptide 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 PrRP20 pubchem
Agonist 3.0 Active 10.1038/S41421-024-00724-6 2024-09-25
9P87 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 NTS8–13 pubchem
Agonist 2.8 Active 10.1038/S41586-026-10120-7 2026-03-25
9IMA GPC5D GPRC5D Orphan 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)
2.7 Inactive 10.1016/J.JMB.2024.168748 2024-09-11
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
Inverse agonist 3.2 Active 10.1038/S41586-020-2469-4 2020-07-01
7SRR 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 (+)-LSD pubchem gtoplig pubchem gtoplig chembl_ligand drugbank drug_central
Agonist (partial) 2.9 Active 10.1016/J.NEURON.2022.08.006 2022-09-21
8ZRT 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-1 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 3.6 Active 10.1038/S42003-024-06905-Z 2024-10-02
8XVK EDNRA ETA 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 ambrisentan pubchem gtoplig chembl_ligand drug_central chembl_ligand pubchem drugbank
Antagonist 3.2 Inactive 2024-08-28
6J20 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 2.7 Inactive 10.1038/S41467-019-08568-5 2019-03-06
8U4O CXCR4 CXCR4 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 Stromal cell-derived...
Agonist 3.3 Active 10.1038/S41594-024-01397-1 2024-03-13
7WJ5 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 drugbank drug_central pubchem
Agonist 3.7 Active 10.7554/ELIFE.76823 2022-07-13
8JIU 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 SAR425899 pubchem
Agonist 2.8 Active 10.1073/PNAS.2303696120 2023-09-13
21DU AGRG6 ADGRG6 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 apomorphine pubchem gtoplig chembl_ligand drugbank drug_central
PAM 2.9 Active 10.1038/S41421-025-00866-1 2026-02-11
8ZWG C3AR C3a Complement peptide 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 JR14a pubchem gtoplig chembl_ligand
Agonist 2.9 Active 2025-05-14
7IOQ 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
FU163-51 pubchem
AntagonistUnknown 2.3 Inactive 2026-05-20
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
8GGZ 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 c-Epi pubchem
Agonist 3.9 Active 10.1038/S41586-024-07153-1 2024-03-06
21AG 5HT1F 5-HT1F 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 LY334370 pubchem gtoplig chembl_ligand
Agonist 3.1 Active 2026-04-08
9EPO FZD7 FZD7 WNT 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)
1.9 Inactive 2024-10-02
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 acid pubchem
Agonist 2.5 Active 10.1038/S41589-018-0160-Y 2018-12-05
8EFO OPRM μ 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 PZM21 pubchem gtoplig chembl_ligand drugbank
Agonist 2.8 Active 10.1016/J.CELL.2022.09.041 2022-11-09
5OLV 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 CHEMBL1671936 chembl_ligand pubchem
Antagonist 2.0 Inactive 10.1038/S41598-017-18570-W 2018-01-17
9PPZ 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 SNC80 pubchem gtoplig chembl_ligand
Agonist 3.2 Active 2026-03-04
8W8S GP101 GPR101 Orphan 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 AA-14 pubchem
Allosteric agonist 3.3 Active 10.1038/S41589-023-01456-6 2024-01-03
6KQI CNR1 CB1 Cannabinoid 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 CP55940 pubchem gtoplig chembl_ligand
Org27569 pubchem gtoplig chembl_ligand
AgonistNAM 3.3 Inactive 10.1038/S41589-019-0387-2 2019-10-23
9W2H NK2R NK2 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 EB1002 pubchem
Agonist 3.1 Active 2026-06-17
6KP6 ACM4 M4 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 Apo (no ligand)
3.0 Inactive 10.1107/S2052252520000597 2020-03-11
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 NPS 2143 pubchem gtoplig chembl_ligand drugbank
D-tryptophan pubchem gtoplig chembl_ligand drugbank pubchem gtoplig chembl_ligand drugbank drug_central
Calcium pubchem
NAMAgonistAgonist 3.2 Inactive 10.1038/S41586-021-03691-0 2021-06-30
8Z7J 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 JN241-9
Agonist 3.1 Active 10.1038/S41467-024-55555-6 2025-01-22
7INC 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 (1R)-1-(1H-1,3-benzi... pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.2 Inactive 2026-05-20
9UYH CML2 chemerin 2 Chemerin receptor 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 Chemerin
Agonist 3.3 Active 10.1126/SCIENCE.ADT8794 2025-11-19
7F1R 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 N/A N/A 3.0 Active 2021-07-14
8JD4 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 chembl_ligand pubchem pubchem drugbank
Agonist 2.9 Active 10.1038/S41422-023-00830-2 2023-06-21
24TI 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 PCO371 pubchem gtoplig chembl_ligand drugbank
Allosteric agonist 2.9 Active 10.1093/PROCEL/PWAG016 2026-07-08
9KFI RL3R1 RXFP3 Relaxin family peptide 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 Relaxin-3 (chain A)
Relaxin-3 (chain B)
AgonistAgonist 2.9 Active 10.1038/S42003-025-08220-7 2025-08-13
9NOS TS1R2 TAS1R2 Taste 1 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)
3.5 Active 10.1016/J.CELL.2025.04.021 2025-05-14
9XXT GP174 GPR174 Orphan 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 lysophosphatidylseri... pubchem gtoplig chembl_ligand
Agonist 2.0 Active 2026-04-15
9KT6 HCAR3 HCA3 Hydroxycarboxylic 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 Acifran pubchem
Agonist 3.0 Active 10.1021/ACS.JMEDCHEM.4C02567 2025-12-10
7DUR 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 Compound 2 pubchem
Ago-PAM 3.3 Active 10.1038/S41467-021-24058-Z 2021-08-11
8XJK PF2R FP 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 cloprostenol pubchem gtoplig chembl_ligand drugbank
Agonist 2.6 Active 2024-02-28
9CM7 FFAR2 FFA2 Free fatty 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 CHEMBL4176503 chembl_ligand pubchem
AZ-1729 pubchem
AgonistAgo-PAM 3.3 Active 2025-06-25
8UXV O51G2 OR51G2 Olfactory family 51 O1 (Olfactory/extra-nasal 1) 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)
3.2 Active 10.1038/S41586-024-08126-0 2024-10-30
5GLI EDNRB ETB Endothelin A (Rhodopsin) Human BaculovirusSf9Insect 6 chemicals 6 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 6.3-6.3 20°C Apo (no ligand)
2.5 Inactive 10.1038/nature19319 2016-09-07
7ZL9 HCAR2 HCA2 Hydroxycarboxylic 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 Apo (no ligand)
2.7 Active 10.1038/S41467-023-37177-6 2023-04-12
7XMS SSR4 SST4 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 drugbank drug_central pubchem
Agonist 2.9 Active 10.1038/S41422-022-00679-X 2022-08-03
3C9M OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine NANANA 1 chemicals 1 steps NANANA 1 chems 0.0-0.0 NA all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Inverse agonist 3.4 Inactive 10.1107/S0907444908017162 2008-08-05
9LFC 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 CHEMBL410363 chembl_ligand pubchem
Antagonist 3.6 Inactive 2026-05-27
7INF 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 2,4-difluorobenzene-... pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.3 Inactive 2026-05-20
9W0Q T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A TANGERETIN chembl_ligand pubchem
Agonist 3.2 Active 2026-04-22
8FLR 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 PTHrP[1-36]
Agonist 2.9 Active 10.1016/J.STR.2023.04.002 2023-04-26
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
9VAU 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
Agonist 3.0 Active 10.1038/S41586-026-10228-W 2026-06-03
7X8S 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 CHEMBL2158488 chembl_ligand pubchem
Agonist 3.1 Active 10.1073/PNAS.2200155119 2022-06-29
6PS2 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 2.4 Inactive 10.1107/S2052252519013137 2019-11-13
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 (S)-carazolol pubchem drugbank
Inverse agonist 3.8 Inactive 10.1107/S2059798315021683 2016-01-13
9ASB 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
tecalcet pubchem gtoplig chembl_ligand
CYCLOMETHYLTRYPTOPHA... pubchem
AgonistPAMAgonist 3.4 Active 2024-04-17
8IZ4 GPR34 GPR34 Orphan 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-oxidanyl-3-p... pubchem
L-serine pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank pubchem drugbank
AgonistAgonist 2.9 Active 2024-04-10
9XQC GPR75 GPR75 Orphan 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)
3.0 Active 10.1038/S41401-025-01720-6 2026-02-04
1F88 OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine NANativeBovine 2 chemicals 2 steps vapour diffusionHanging drop 7 chems 6.0-6.0 4°C all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Inverse agonist 2.8 Inactive 10.1126/SCIENCE.289.5480.739 2000-08-04
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
Agonist 2.8 Active 10.1126/SCIADV.ABF1268 2021-05-05
8UNW 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 c-Epi pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
8WST MCHR2 MCH2 Melanin-concentrating 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 melanin-concentratin... pubchem gtoplig uniprot uniprot uniprot
Agonist 2.4 Active 10.1038/S41421-024-00679-8 2024-06-19
6S0L 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 10.1107/S2052252520011379 2020-07-15
8HQC C5AR1 C5a1 Complement peptide 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 [<sup>125</sup>I]C5a... gtoplig
Agonist 3.9 Active HTTPS://DOI.ORG/10.1016/J.CELL.2023.09.020 2023-10-18
4N4W SMO SMO Oxysterol F (Frizzled) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 7 chems 6.9-6.9 20°C SANT-1 pubchem gtoplig chembl_ligand
Antagonist 2.8 Inactive 10.1038/NCOMMS5355 2014-01-22
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
Nanobody 43
AgonistPAM 4.0 Active 10.1038/S41586-019-0881-4 2019-01-23
8GGE 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 c-Epi pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
8IOD MC5R MC5 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 PG-901
Agonist 2.6 Active 10.1107/S0907444909042073 2023-09-20
23OI OPRX NOP 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 cebranopadol pubchem gtoplig chembl_ligand chembl_ligand chembl_ligand drugbank
Agonist 2.7 Active 2026-07-01
8Z67 GPR4 GPR4 Proton 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)
3.2 Active 2025-04-23
8GGU 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 c-Epi pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
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 chembl_ligand pubchem drugbank pubchem pubchem
Antagonist 3.6 Inactive 10.1016/J.STR.2014.08.022 2014-11-26
8XOR PAR1 PAR1 Proteinase-activated 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 3.0 Active 2024-09-18
9VI9 NPFF1 NPFF1 Neuropeptide FF/neuropeptide AF 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 RFRP-3
Agonist 3.0 Active 10.1093/PROCEL/PWAF090 2025-12-03
7UM5 5HT5A 5-HT5A 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-CT pubchem gtoplig chembl_ligand
Agonist 2.7 Active 10.1038/S41594-022-00796-6 2022-07-20
9IPV C3AR C3a Complement peptide 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 JR14a pubchem gtoplig chembl_ligand
Agonist 2.5 Active 2025-04-23
8JCZ 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
Antagonist 3.0 Inactive 10.1038/S41422-023-00830-2 2023-06-21
9J0I P2Y14 P2Y14 P2Y 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 UDP-glucuronic acid pubchem gtoplig chembl_ligand drugbank
Agonist 2.8 Active 10.1038/S41421-025-00799-9 2025-06-04
8FMZ 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 NTS8–13 pubchem
Agonist 2.6 Active 10.1021/ACS.BIOCHEM.3C00029 2023-03-29
4XT1 US28 US28 Unclassified A (Rhodopsin) strain AD169 BaculovirusHEK293S(TetR)-GnTI-Mammalian 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 7 chems 6.3-7.0 20°C Fractalkine (CX3CL1)
Agonist 2.9 Active 10.1126/SCIENCE.AAA5026 2015-03-04
4MQS ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 7.2-7.9 20°C iperoxo pubchem gtoplig chembl_ligand
Agonist 3.5 Active 10.1038/NATURE12735 2013-11-27
9BUB 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 cagrilintide pubchem gtoplig drugbank
Agonist 2.3 Active 2025-04-23
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
9LL7 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 (R)-DOI pubchem gtoplig chembl_ligand
Agonist 2.8 Active 2026-01-14
8F7Q OPRM μ 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 Beta-endorphin pubchem
Agonist 3.2 Active 10.1016/J.CELL.2022.12.026 2022-12-14
6TP3 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 daridorexant pubchem gtoplig chembl_ligand drugbank
Antagonist 3.0 Inactive 10.1021/acs.jmedchem.9b01787 2020-01-01
9UVV 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 CHEMBL4303142 chembl_ligand pubchem drugbank chembl_ligand
Antagonist 3.0 Inactive 2026-05-06
6OT0 SMO SMO Oxysterol 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 24(S),25-Epoxycholes... pubchem
Agonist 3.9 Active 10.1038/S41586-019-1286-0 2019-06-12
8TB0 GPR61 GPR61 Orphan 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)
3.5 Active 2023-10-04
4GRV 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 7.0-7.0 20°C NTS8–13 pubchem
Agonist 2.8 Active 10.1038/NATURE11558 2012-10-17
8XGM CML2 chemerin 2 Chemerin receptor 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 Chemerin
Agonist 3.3 Active 2024-08-21
6TOS 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 CHEMBL2413522 chembl_ligand pubchem
Antagonist 2.1 Inactive 10.1021/acs.jmedchem.9b01787 2020-01-15
4PXF OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionsitting drop 3 chems 6.0-6.0 4°C Apo (no ligand)
2.8 Active 10.1038/NCOMMS5801 2014-09-17
8VVE OPRK κ 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 nor-binaltorphimine pubchem gtoplig chembl_ligand
Inverse agonist 3.3 Active 2025-01-15
9XJW GP119 GPR119 GPR18, GPR55 and GPR119 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 AS1269574 pubchem gtoplig chembl_ligand
Agonist (partial) 2.5 Active 2026-05-27
7CFM 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 CHEMBL2331646 chembl_ligand pubchem
Agonist 3.0 Active 10.1038/S41586-020-2569-1 2020-09-09
9VJE 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 buspirone pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.5 Active 10.1016/J.CELL.2025.10.022 2025-11-12
8JGG MRGX1 MRGPRX1 Orphan 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 bovine adrenal medul... pubchem gtoplig chembl_ligand uniprot
Agonist 3.0 Active 10.1038/S41467-023-40705-Z 2024-01-10
9MZE 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 Oxyntomodulin pubchem pubchem
Agonist 2.2 Active 2026-04-22
7IO8 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 FU18-82 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.3 Inactive 2026-05-20
8IJ3 HCAR2 HCA2 Hydroxycarboxylic 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 Apo (no ligand)
3.3 Active 10.1038/S41421-023-00610-7 2024-01-03
7XY7 AA2BR A2B 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 NECA pubchem gtoplig chembl_ligand
Agonist 3.3 Active 10.1126/SCIADV.ADD3709 2023-05-03
7INO 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 F223 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.1 Inactive 2026-05-20
8VY9 T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A compound 28.1 [PMID:... pubchem gtoplig chembl_ligand
Cholesterol pubchem drugbank
Ago-PAMAgonist 2.9 Active 2024-04-03
7Y27 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 drugbank drug_central pubchem
Agonist 3.5 Active 10.1038/S41589-022-01130-3 2022-10-19
9J0B P2Y14 P2Y14 P2Y 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 UDP-glucose pubchem gtoplig chembl_ligand drugbank
Agonist 2.9 Active 10.1038/S41421-025-00799-9 2025-06-04
9PUD OPRM μ 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 DAMGO pubchem gtoplig chembl_ligand pubchem
Agonist 3.0 Active 2026-05-27
8P13 OPSD Rhodopsin Opsin (sight) 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)
5.2 Active 2024-11-20
7SK7 ACKR3 ACKR3 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 CXCL12
CCX662 pubchem
AgonistAgonist (partial) 3.3 Active 10.1126/SCIADV.ABN8063 2022-07-27
24XY P2Y13 P2Y13 P2Y 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 ADP pubchem gtoplig chembl_ligand
Agonist 3.0 Active 10.1016/J.BBRC.2026.153976 2026-06-10
8WGC 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 LY379268 pubchem gtoplig chembl_ligand pubchem
Agonist 6.0 Intermediate 10.1038/S41467-024-54744-7 2024-11-27
9VJ5 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 GEPIRONE chembl_ligand pubchem drugbank drug_central
Agonist 2.7 Active 2025-11-12
9EPP B1B1U5 Rhodopsin Opsin (sight) 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 11,20-Ethanoretinal pubchem
Agonist 4.1 Active 2024-10-23
8ZSJ TAAR1 TA1 Trace amine 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)
2.8 Active 10.1016/J.CELREP.2024.114505 2024-07-24
8GE3 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 c-Epi pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06
8FN0 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 SBI-553 pubchem gtoplig chembl_ligand
NTS8–13 pubchem
Ago-PAMAgonist 2.9 Active 10.1021/ACS.BIOCHEM.3C00029 2023-03-29
8JPN SUCR1 succinate Succinate 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 <i>cis</i>-epoxysucc... pubchem gtoplig chembl_ligand
Agonist 2.9 Active 10.1038/S41422-024-00968-7 2024-05-22
4IAR 5HT1B 5-HT1B 5-Hydroxytryptamine A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 7.5-7.5 20°C ergotamine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.7 Inactive 10.1126/SCIENCE.1232807 2013-03-13
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
9KUV 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 cmpd644 pubchem
Agonist 3.2 Active 2025-09-17
8Z8B HCAR1 HCA1 Hydroxycarboxylic 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 Apo (no ligand)
2.7 Active 10.1126/SCISIGNAL.ADW1483 2025-10-29
8G59 FFAR4 FFA4 Free fatty 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 TUG-891 pubchem gtoplig chembl_ligand
Agonist 2.6 Active 10.1126/SCIENCE.ADD6220 2023-03-08
8JPC 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 NTS8–13 pubchem
SBI-553 pubchem gtoplig chembl_ligand
AgonistAgo-PAM 3.1 Active 10.1038/S41586-023-06395-9 2023-08-09
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)
7.6 Inactive 10.1016/J.JMB.2020.09.023 2020-11-11
8XWV 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 CXCL1
Agonist 3.1 Active 10.1016/J.MOLCEL.2025.01.024 2025-01-22
7MTA OPSD Rhodopsin Opsin (sight) 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 all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 4.1 Active 10.1038/S41586-021-03721-X 2021-07-07
8J6I HCAR2 HCA2 Hydroxycarboxylic 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 MK 6892 pubchem gtoplig chembl_ligand pubchem
Agonist 2.9 Active 10.1016/J.CELREP.2023.113406 2024-04-03
6OL9 ACM5 M5 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 TIOTROPIUM chembl_ligand pubchem drugbank pubchem pubchem
Inverse agonist 2.5 Inactive 10.1073/PNAS.1914446116 2019-12-11
8IEP GP156 GPR156 Orphan 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 PC 34:1 pubchem
Agonist 2.6 Active 2024-02-14
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 Chromone 5d pubchem
Antagonist 2.1 Inactive 10.1002/ANIE.202003788 2020-09-16
7VIF 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 2.8 Active 10.1073/PNAS.2117716119 2022-09-28
8WZ2 QRFPR QRFP QRFP 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 26RFa pubchem
Agonist 2.7 Active 10.1038/S41421-024-00670-3 2024-06-19
7IOV 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 FU163-104 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.3 Inactive 2026-05-20
7IO9 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 FU35-2 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 1.9 Inactive 2026-05-20
9ITE LPAR6 LPA6 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 LPA pubchem
Agonist 3.1 Active 10.1073/PNAS.2415426122 2025-01-15
8U1U CCR8 CCR8 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 N/A N/A 3.1 Active 2023-12-20
8RWE 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 CHEMBL2381766 chembl_ligand pubchem
Antagonist 2.2 Inactive 2025-01-08
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 glucagon-like peptid... pubchem gtoplig uniprot uniprot uniprot chembl_ligand pubchem
Compound 2 pubchem
AgonistAgo-PAM 2.5 Active 10.1038/S41467-021-24058-Z 2021-07-14
7IOM 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 FU18-82 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.1 Inactive 2026-05-20
8HVI GP132 GPR132 Proton 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 NOX-6-7 pubchem gtoplig
Agonist 3.0 Active 10.1038/S42255-023-00899-4 2023-10-11
7S8P MRGX4 MRGPRX4 Orphan 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 MS47134
Agonist 2.6 Active 10.1038/S41586-021-04126-6 2021-11-17
9GGG 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 I-BOP pubchem gtoplig chembl_ligand
Agonist 3.3 Active 2025-08-27
9UYO GRM6 mGlu6 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
Agonist 3.4 Active 2026-03-18
7IOE 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 FU44-18 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.1 Inactive 2026-05-20
2G87 OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 6.5-7.5 283 K all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 2.6 Inactive 10.1002/ANIE.200600595 2006-09-02
9MEN CXCR4 CXCR4 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 Surface protein gp12...
Agonist 3.6 Inactive 10.1038/S41467-025-63815-2 2025-09-10
8SZI 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
D-tryptophan pubchem gtoplig chembl_ligand drugbank pubchem gtoplig chembl_ligand drugbank drug_central
D-tryptophan pubchem gtoplig chembl_ligand drugbank pubchem gtoplig chembl_ligand drugbank drug_central
AgonistAgonistPAM 3.5 Active 10.1038/S41586-024-07055-2 2024-02-07
7XMR 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 drugbank drug_central pubchem
Agonist 3.1 Active 10.1038/S41422-022-00679-X 2022-08-03
9AS8 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 2.5 Active 10.1038/S41467-025-57956-7 2025-04-02
9W0T T2R46 TAS2R46 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A denatonium pubchem gtoplig chembl_ligand
Agonist 3.3 Active 10.1038/S41594-026-01786-8 2026-04-22
7CX4 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 evatanepag pubchem gtoplig chembl_ligand drugbank
Agonist 2.9 Active 10.1126/SCIADV.ABF1268 2021-05-05
8TB7 GPR61 GPR61 Orphan 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: 37... pubchem gtoplig
Inverse agonist 2.9 Active 10.1038/S41467-023-41646-3 2023-10-04
2ZIY OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Japanese flying squid NANativeSquid 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 7.0-7.0 20°C all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Inverse agonist 3.7 Inactive 10.1074/JBC.C800040200 2008-05-06
4AMI ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 2 chemicals 2 steps vapour diffusionsitting drops 3 chems 9.0-9.0 4°C Bucindolol pubchem
Agonist (partial) 3.2 Inactive 10.1016/J.STR.2012.03.014 2012-05-23
6C1Q C5AR1 C5a1 Complement peptide A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 6.5-6.5 10°C PMX53 pubchem gtoplig chembl_ligand
NDT9513727 pubchem gtoplig
AntagonistAllosteric antagonist 2.9 Inactive 10.1038/S41594-018-0067-Z 2018-05-30
8JJ8 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 chembl_ligand pubchem drugbank drug_central drugbank
Agonist (partial) 3.2 Active 10.1038/S41589-023-01389-0 2023-09-06
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
9KPD T2R16 TAS2R16 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A salicin pubchem gtoplig
Agonist 2.8 Active 10.1016/J.CELREP.2025.115604 2025-04-02
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 (Human) pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank pubchem
Agonist 2.9 Active 10.1038/S41589-021-00841-3 2021-08-25
8GHV CNR1 CB1 Cannabinoid 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 CHEMBL4208628 chembl_ligand pubchem
Agonist 2.8 Active 10.1038/S41467-023-37864-4 2023-05-24
8UO3 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 c-Epi pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
6KPG CNR1 CB1 Cannabinoid 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 AM841 pubchem gtoplig chembl_ligand
Agonist 3.0 Active 10.1016/J.CELL.2020.01.008 2020-02-12
8YH0 AA3R A3 Adenosine A (Rhodopsin) Sheep N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A NECA pubchem gtoplig chembl_ligand
Agonist 2.9 Active 10.1038/S41467-024-53473-1 2024-11-06
8YU7 CXCR4 CXCR4 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)
3.0 Inactive 10.1016/J.CELREP.2025.115255 2025-03-05
9WSW OPRM μ Opioid 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 endomorphin-1 (Human... pubchem gtoplig chembl_ligand
Agonist 2.8 Active 10.1038/S41422-025-01191-8 2025-11-26
6RZ4 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 pranlukast pubchem gtoplig chembl_ligand drugbank drug_central
Na+ pubchem
AntagonistNAM 2.7 Active 10.1126/SCIADV.AAX2518 2019-10-30
8IW9 TAAR9 TAAR9 Orphan 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 Cadaverine pubchem drugbank
Agonist 3.1 Active 10.1038/S41586-023-06106-4 2023-05-31
9WQK 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 L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem pubchem drugbank
CDPPB pubchem gtoplig chembl_ligand
AgonistPAM 3.7 Active 10.1126/SCIADV.AEE0044 2026-05-27
7IN8 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 Apo (no ligand)
2.5 Inactive 10.1038/S42004-026-02059-7 2026-05-20
9V3Y C5AR2 C5a2 Complement peptide 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 C5a-pep
Agonist 3.1 Active 10.1016/J.MOLCEL.2026.06.002 2026-07-01
3ZPQ ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 1 chemicals 1 steps vapour diffusionsitting drops 3 chems 9.0-9.0 4°C CHEMBL200234 chembl_ligand pubchem
Antagonist 2.8 Inactive 10.1021/jm400140q 2013-04-03
9VOR MGLYR MGLYR Metabotropic glycine 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 Nb20
Antagonist 3.5 Inactive 10.1038/S41467-026-68339-X 2025-12-31
2YCY ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 2 chemicals 2 steps vapour diffusionNA 3 chems 6.9-7.3 NA 4-{[(2S)-3-(tert-but... pubchem drugbank
Antagonist 3.2 Inactive 10.1073/PNAS.1100185108 2011-06-08
6PT2 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 CHEMBL3408735 chembl_ligand pubchem pubchem
Agonist 2.8 Active 2019-12-11
8U4N CXCR4 CXCR4 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)
2.7 Active 10.1038/S41594-024-01397-1 2024-03-13
9UXQ OXGR1 oxoglutarate Oxoglutarate 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 &alpha;-ketoglutaric... pubchem gtoplig chembl_ligand drugbank
Agonist 2.9 Active 10.1038/S44318-026-00823-Y 2026-05-27
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 NTS8–13 pubchem
Agonist 3.3 Active 10.1038/SREP38564 2016-12-21
7YK7 RL3R2 RXFP4 Relaxin family peptide 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 DC591053 pubchem gtoplig
Agonist 2.8 Active 10.1038/S41467-023-36182-Z 2023-03-01
9CHX 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 (S)-carazolol pubchem drugbank
Inverse agonist 3.5 Inactive 10.1073/PNAS.2414544121 2024-11-13
9QP4 OPSB OPN1SW Opsin (sight) 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 all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Inverse agonist 3.1 Inactive 10.1126/SCIENCE.ADZ3624 2026-06-24
7XNA 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 CYN 154806 pubchem
Antagonist 2.7 Inactive 10.1038/S41422-022-00679-X 2022-08-03
9BYO 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-asp3
Agonist 2.3 Active 2025-06-11
7YDH AGRE5 ADGRE5 ADGRE 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 Apo (no ligand)
3.1 Active 10.1016/J.CHEMBIOL.2023.08.003 2023-07-12
9UAM 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 LTC4 pubchem gtoplig chembl_ligand drugbank
Agonist 3.3 Active 2026-03-18
9HC0 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 alloswitch-1 pubchem gtoplig
NAM 2.3 Inactive 10.1002/PRO.70104 2025-06-25
9BIP GPR4 GPR4 Proton 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)
2.8 Active 10.1016/J.CELL.2024.11.036 2025-01-15
9U4W GNRHR GnRH1 Gonadotrophin-releasing hormone A (Rhodopsin) Pig N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL266314 chembl_ligand pubchem pubchem drugbank pubchem chembl_ligand
Agonist 3.2 Active 10.1073/PNAS.2500112122 2025-06-11
9KWX C5AR1 C5a1 Complement peptide 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 C5a-desArg
Agonist 3.1 Active 10.1101/2025.05.26.656101 2025-11-26
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 pubchem
Agonist 3.2 Inactive 10.1038/S41586-019-1141-3 2019-04-24
9ZZO OPRK κ 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 CHEMBL5431513 chembl_ligand pubchem
Agonist 2.6 Active 10.1038/S41467-026-73968-3 2026-06-17
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 chembl_ligand pubchem drugbank drug_central
Agonist 2.9 Active 10.1038/S41422-021-00569-8 2021-11-17
9VPN 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 Apo (no ligand)
4.0 Active 2026-07-08
2R4S ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps vapour diffusionhanging drop 5 chems 6.5-7.5 22°C Apo (no ligand)
3.4 Inactive 10.1038/NATURE06325 2007-11-06
9LKB A2RT31 OR5V1 Olfactory family 5 O2 (Olfactory/extra-nasal 2) Mouse N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A PL45 pubchem
Agonist 3.7 Active 2026-01-21
7JOZ 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 CHEMBL4453318 chembl_ligand pubchem
Agonist 3.8 Active 10.1038/S41467-021-23519-9 2021-04-14
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 chembl_ligand drug_central pubchem
Agonist 3.0 Active 10.1126/SCIENCE.ABM9609 2022-03-23
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
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 Active 10.1038/s41594-018-0116-7 2018-08-29
8HQN GP132 GPR132 Proton 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 9-hydroxyoctadecadie... pubchem gtoplig chembl_ligand drugbank
Agonist 3.0 Active 10.1038/S42255-023-00899-4 2023-10-11
7CMV 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 CHEMBL70565 chembl_ligand pubchem
Agonist 2.7 Active 10.1016/J.MOLCEL.2021.01.003 2021-03-10
7F8W 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 uniprot chembl_ligand pubchem
Agonist 3.1 Active 10.1038/S41589-021-00866-8 2021-10-13
8WC8 TAAR1 TA1 Trace amine 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 CHEMBL476516 chembl_ligand pubchem
Agonist 2.9 Active 10.1016/J.CELL.2023.10.014 2023-12-27
8T1W GPR6 GPR6 Orphan 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 solengepras pubchem gtoplig chembl_ligand chembl_ligand drugbank
Inverse agonist 3.5 Inactive 10.1126/SCISIGNAL.ADO8741 2024-12-04
9KZK C3AR C3a Complement peptide 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 mouse C3a anaphylato...
Agonist 3.5 Active 10.1101/2025.05.26.656101 2025-11-26
8IRV DRD5 D5 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 rotigotine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.1 Active 10.1038/S41422-023-00808-0 2023-06-07
8T8M 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
Nanobody 43
AgonistPAM 3.0 Active 10.1101/2023.08.29.555158 2023-10-11
8GEE 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 c-Epi pubchem
Agonist 3.7 Active 10.1038/S41586-024-07153-1 2024-03-06
8TH3 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 N/A N/A 3.0 Inactive 10.1038/S41589-024-01620-6 2024-05-22
3UON ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 7.5-7.5 19.85°C CHEMBL558910 chembl_ligand pubchem
Inverse agonist 3.0 Inactive 10.1038/NATURE10753 2012-02-01
8YH6 AA3R A3 Adenosine A (Rhodopsin) Sheep N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Cl-IB-MECA pubchem gtoplig chembl_ligand drugbank
Agonist 3.6 Active 10.1038/S41467-024-53473-1 2024-11-06
5TVN 5HT2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human BaculovirusSf21Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 7.5-8.0 20°C (+)-LSD pubchem gtoplig pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.9 Active 10.1016/J.CELL.2016.12.033 2017-02-01
8WVU LGR4 LGR4 Orphan 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-spondin-1
E3 ubiquitin-protein...
AgonistAllosteric agonist 3.6 Inactive 2024-10-30
8F7W OPRK κ 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 dynorphin A-(1-8) (H... pubchem gtoplig uniprot uniprot uniprot chembl_ligand
Agonist 3.2 Active 10.1016/J.CELL.2022.12.026 2022-12-14
9CBL 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 (-)-adrenaline pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.8 Active 10.1038/S12276-024-01296-X 2024-09-11
9UK2 OXGR1 oxoglutarate Oxoglutarate 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)
2.9 Active 2026-04-22
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
Agonist 3.4 Active 10.1038/S41589-021-00930-3 2022-01-05
9CGK 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 C5-Quino pubchem
Agonist 2.6 Active 2025-04-02
8KGG P2Y10 P2RY10 Orphan 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 LysoPS(18:0)
Agonist 3.1 Active 10.1016/J.CHEMBIOL.2024.08.005 2024-07-31
8ID8 FFAR4 FFA4 Free fatty 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 TUG-891 pubchem gtoplig chembl_ligand
Agonist 3.0 Active 10.1126/SCIENCE.ADD6220 2023-03-15
8GDA 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 L902688 pubchem
Agonist 3.3 Active 10.1073/PNAS.2216329120 2024-01-10
9OMO GRM7 mGlu7 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)
4.1 Inactive 10.1073/PNAS.2507112122 2025-07-09
5C1M OPRM μ Opioid A (Rhodopsin) Mouse BaculovirusSf9Insect 6 chemicals 6 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 7 chems 7.5-7.5 20°C BU72 pubchem gtoplig
Agonist 2.1 Active 10.1038/NATURE14886 2015-08-05
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
Inverse agonist 1.8 Inactive 10.1038/S41598-020-76277-X 2020-11-25
9WPM O5B21 OR5B21 Olfactory family 5 O2 (Olfactory/extra-nasal 2) 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)
2.6 Active 10.1016/J.CELL.2025.12.018 2026-01-28
7IO4 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 FU12-19 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.1 Inactive 2026-05-20
8DCS 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 4-{[(2S)-3-(tert-but... pubchem drugbank
Agonist (partial) 2.5 Active 10.1038/S41467-022-31823-1 2022-07-27
8UNY 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 c-Epi pubchem
Agonist 3.6 Active 10.1038/S41586-024-07153-1 2024-03-06
9IIX T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A compound 28.1 [PMID:... pubchem gtoplig chembl_ligand
compound 28.1 [PMID:... pubchem gtoplig chembl_ligand
AgonistAllosteric agonist 2.9 Active 2024-07-24
25NX 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 Peptide 2 (PTHrP ana...
Agonist 2.9 Active 10.1021/JACS.6C02192 2026-06-03
9EI5 PD2R DP1 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 Apo (no ligand)
2.8 Intermediate 10.1038/S41467-025-64002-Z 2025-09-03
9BHL GPR65 GPR65 Proton 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)
2.8 Active 10.1016/J.CELL.2024.11.036 2025-01-22
7DD7 A0A8I3AZV5 CaS Calcium-sensing C (Glutamate) Chicken N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Calcium pubchem
evocalcet pubchem gtoplig drug_central chembl_ligand drugbank
D-tryptophan pubchem gtoplig chembl_ligand drugbank pubchem gtoplig chembl_ligand drugbank drug_central
AgonistPAMAgonist 3.2 Active 10.1126/SCIADV.ABG1483 2021-06-16
7RKN US28 US28 Unclassified A (Rhodopsin) strain AD169 N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Fractalkine
Agonist (partial) 3.6 Active 10.1126/SCIADV.ABL5442 2022-01-26
7VV3 MRGX2 MRGPRX2 Orphan 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)
3.0 Active 10.1038/S41586-021-04077-Y 2021-12-01
8X0H 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
Agonist 4.1 Intermediate 10.1038/S41467-024-55439-9 2024-11-06
7SHE MGLYR MGLYR Metabotropic glycine 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)
3.4 Inactive 10.1126/SCIENCE.ABL4732 2021-12-01
9VMO OXGR1 oxoglutarate Oxoglutarate 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 Itaconic acid pubchem
Agonist 2.4 Active 10.1016/J.CELL.2026.01.036 2026-03-18
5XF1 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 NNC0640 pubchem gtoplig
Antibody mAb1 (chain...
Antibody mAb1 (chain...
NAMAntagonistAntagonist 3.2 Inactive 10.1038/NATURE22363 2017-05-24
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 uniprot pubchem
Agonist 3.0 Active 10.1021/ACSPTSCI.9B00080 2020-03-25
9PA4 OPRK κ 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 ESKETAMINE chembl_ligand pubchem drugbank
Agonist (partial) 2.5 Active 10.1038/S41594-026-01839-Y 2026-07-01
8X64 HRH1 H1 Histamine 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 desloratadine pubchem gtoplig chembl_ligand drugbank drug_central
Inverse agonist 3.4 Inactive 10.1038/S41467-023-44477-4 2024-01-17
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
Inverse agonist 2.9 Inactive 10.1038/S41594-018-0180-Z 2019-02-13
8WRZ CNR1 CB1 Cannabinoid 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 V2Rpp (phosphorylate...
AM841 pubchem gtoplig chembl_ligand
AgonistAgonist 3.6 Active 10.1093/PROCEL/PWAD055 2024-02-28
1U19 OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 6.5-7.5 283 K all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Inverse agonist 2.2 Inactive 10.1016/J.JMB.2004.07.044 2004-10-12
8HJ5 MRGX1 MRGPRX1 Orphan 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 16 [PMID: 3... pubchem gtoplig chembl_ligand
Agonist 3.0 Active 2023-05-31
8IEB GP156 GPR156 Orphan 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 PC 34:1 pubchem
Agonist 3.0 Active 2024-02-14
9LRC HRH4 H4 Histamine 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 histamine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 2.8 Active 10.1038/S42003-025-08363-7 2025-06-11
8UGY 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 CHEMBL252719 chembl_ligand pubchem
Agonist 3.3 Active 10.1126/SCIADV.ADK4855 2024-05-01
5XSZ Q08BG4 LPA6 Lysophospholipid (LPA) A (Rhodopsin) Zebrafish BaculovirusSf9Insect 8 chemicals 8 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 6 chems 6.0-6.0 20°C Apo (no ligand)
3.2 Active 10.1038/NATURE23448 2017-08-16
9N05 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 SRB103Q
Agonist 2.2 Active 2026-04-22
8ZPS PRLHR PrRP Prolactin-releasing peptide 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 PrRP20 pubchem
Agonist 3.0 Active 10.1038/S41421-024-00724-6 2024-09-25
2YCZ ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 2 chemicals 2 steps vapour diffusionNA 3 chems 6.9-7.3 NA Iodocyanopindolol pubchem
Antagonist 3.7 Inactive 10.1073/PNAS.1100185108 2011-06-01
9L3Z CML1 chemerin Chemerin receptor 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 LRH7-C2
Antagonist 3.9 Inactive 10.1093/PROCEL/PWAE073 2025-03-12
5N2R 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 PSB36
Antagonist 2.8 Inactive 10.1016/j.str.2017.06.012 2017-07-26
7VKT LT4R1 BLT1 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 LTB4 pubchem gtoplig chembl_ligand drugbank
Agonist 2.9 Active 10.1038/S41467-022-28820-9 2022-03-09
9RKG 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 CHEMBL4633760 chembl_ligand pubchem
Antagonist 2.5 Inactive 2026-04-22
8GE5 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 c-Epi pubchem
Agonist 3.2 Active 10.1038/S41586-024-07153-1 2024-03-06
7VLA 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 CCL15(27-92) (CCL15M...
Agonist 2.7 Active 10.1038/S41589-021-00918-Z 2022-03-23
6ME6 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 CHEMBL15060 chembl_ligand pubchem
Agonist 2.8 Inactive 10.1038/S41586-019-1144-0 2019-04-24
5WB2 US28 US28 Unclassified A (Rhodopsin) strain AD169 BaculovirusHEK293S(TetR)-GnTI-Mammalian 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 7 chems 6.0-6.0 16-20°C CX3CL1.35
Agonist 3.5 Active 10.7554/ELIFE.35850 2018-06-13
7XJL GALR2 GAL2 Galanin 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 Spexin pubchem
Agonist 3.5 Active 10.1073/PNAS.2121465119 2022-06-29
8W8A TAAR1 TA1 Trace amine 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 CHEMBL3684869 chembl_ligand pubchem
Agonist 2.8 Active 10.1038/S41586-023-06775-1 2023-11-22
8IW1 TAAR9 TAAR9 Orphan 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 N/A N/A 3.4 Active 10.1038/S41586-023-06106-4 2023-05-31
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
8HN1 ADA1A α1A 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 ρ-Da1a gtoplig uniprot
Antagonist 2.9 Inactive 2023-12-20
8ZSP TAAR1 TA1 Trace amine 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 (+)-LSD pubchem gtoplig pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.1 Active 10.1016/J.CELREP.2024.114505 2024-07-24
22XC CXCR4 CXCR4 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 dCX1_001
Antagonist 3.3 Inactive 10.1038/S41586-026-10656-8 2026-04-22
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
Antagonist 3.3 Inactive 10.1016/j.str.2017.06.012 2017-07-26
9LYC GPR3 GPR3 Orphan 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)
3.1 Active 10.1016/J.CELREP.2025.115478 2025-04-09
7K15 LT4R1 BLT1 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 CHEMBL6030437 chembl_ligand pubchem
Antagonist 2.9 Inactive 10.1038/S41467-021-23149-1 2021-02-17
8GE1 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 c-Epi pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
6H7O 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 4-{[(2S)-3-(tert-but... pubchem drugbank
Agonist (partial) 2.8 Active 2018-10-17
7VGX 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 NEUROPEPTIDE-Y chembl_ligand pubchem
Agonist 3.2 Active 10.1038/S41467-022-28510-6 2022-02-23
8YYW OXGR1 oxoglutarate Oxoglutarate 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 &alpha;-ketoglutaric... pubchem gtoplig chembl_ligand drugbank
Agonist 3.2 Active 10.1038/S41467-025-67101-Z 2025-04-09
7XOW 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 uniprot chembl_ligand pubchem
Agonist 3.1 Active 10.1038/S41421-022-00420-3 2022-07-20
9P1S 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 3.3 Inactive 10.1038/S42004-025-01825-3 2025-12-24
8IU2 OPSR OPN1LW Opsin (sight) 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 all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 3.4 Active 2024-03-27
9VAV 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
Agonist 3.0 Active 10.1038/S41586-026-10228-W 2026-06-03
5XEZ 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 Antibody mAb1 (chain...
Antibody mAb1 (chain...
NNC0640 pubchem gtoplig
AntagonistAntagonistNAM 3.0 Inactive 10.1038/NATURE22363 2017-05-24
7IO1 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 FU7-1 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.3 Inactive 2026-05-20
9LYB GPR3 GPR3 Orphan 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)
3.2 Active 10.1016/J.CELREP.2025.115478 2025-04-09
8YG4 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 LA-PTH-R1
Agonist 2.6 Active 2025-09-03
7F6G 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 CHEMBL216061 chembl_ligand pubchem
Agonist 2.9 Active 2023-03-29
9B54 CNR1 CB1 Cannabinoid 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 VIP36 pubchem gtoplig
Agonist 2.9 Active 2025-03-05
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 chembl_ligand pubchem
Agonist (partial) 3.1 Active 10.1038/s41594-018-0116-7 2018-08-29
8I2H FSHR FSH 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 Apo (no ligand)
6.0 Inactive 10.1038/S41467-023-36170-3 2023-03-22
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
9W3K GP151 GPR151 Orphan 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)
3.1 Inactive 10.1073/PNAS.2534234123 2026-05-06
3VG9 AA2AR A2A Adenosine A (Rhodopsin) Human P.pastorisP. pastoris SMD1163Yeast 2 chemicals 2 steps vapour diffusionhanging drop 4 chems 6.5-6.5 20°C Fab2838 (chain B)
Fab2838 (chain C)
ZM-241385 pubchem gtoplig chembl_ligand drugbank
Inverse agonistInverse agonistAntagonist 2.7 Inactive 10.1038/NATURE10750 2012-02-01
8E3Z 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 Vasoactive intestina... pubchem
Agonist 2.7 Active 10.1038/S41467-022-34629-3 2022-11-23
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 SKF-81297 pubchem gtoplig chembl_ligand chembl_ligand pubchem chembl_ligand pubchem
Agonist 3.0 Active 10.1016/J.CELL.2021.01.027 2021-02-24
8W1Z G5EG04 fshr-1 Unclassified A (Rhodopsin) Caenorhabditis elegans 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)
3.8 Active 10.1038/S41467-025-66676-X 2025-12-24
8IYX GPR34 GPR34 Orphan 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 YL-365 pubchem gtoplig
Antagonist 3.3 Active 10.1073/PNAS.2308435120 2024-03-20
8IJB HCAR2 HCA2 Hydroxycarboxylic 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 Acipimox pubchem
Agonist 3.2 Active 10.1038/S41421-023-00610-7 2024-01-03
7XW9 TRFR TRH1 Thyrotropin-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 TRH (Human) pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank pubchem
Agonist 2.7 Active 2022-12-28
8HSC GPR20 GPR20 Orphan 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)
3.2 Active 10.1038/S41421-023-00520-8 2023-03-08
8UNZ 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 c-Epi pubchem
Agonist 3.8 Active 10.1038/S41586-024-07153-1 2024-03-06
8CU6 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 LJ-4517 pubchem gtoplig chembl_ligand
Antagonist 2.8 Inactive 10.1021/acs.jmedchem.2c00462 2022-08-31
8Y63 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 Cer(d18:0/20:0) pubchem
Agonist 3.2 Active 2025-02-05
6PT0 CNR2 CB2 Cannabinoid 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 WIN55212-2 pubchem gtoplig chembl_ligand drugbank
Agonist 3.2 Active 10.1016/J.CELL.2020.01.007 2020-02-12
9CHV 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 Apo (no ligand)
4.0 Inactive 10.1073/PNAS.2414544121 2024-11-13
9X20 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 Glucagon-like peptid... pubchem
Agonist 3.2 Active 10.1016/J.APSB.2026.01.023 2026-05-06
9OQ0 TS1R2 TAS1R2 Taste 1 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)
3.7 Intermediate 10.1038/S41422-025-01156-X 2025-08-27
4QIM SMO SMO Oxysterol 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
9HAP 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 CHEMBL4303142 chembl_ligand pubchem drugbank chembl_ligand
Inverse agonist 2.5 Inactive 2025-06-04
8GEJ 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 c-Epi pubchem
Agonist 4.2 Active 10.1038/S41586-024-07153-1 2024-03-06
8J6P HCAR2 HCA2 Hydroxycarboxylic 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 nicotinic acid pubchem gtoplig chembl_ligand drugbank drug_central drugbank drugbank
compound 9n [PMID: 1... pubchem gtoplig chembl_ligand
AgonistAgo-PAM 2.6 Active 10.1038/S41467-023-43537-Z 2023-12-06
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 Active 10.1038/S41422-022-00623-Z 2022-03-16
6ZFZ 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 CHEMBL3354065 chembl_ligand pubchem
Agonist 2.2 Inactive 10.1016/J.CELL.2021.11.001 2021-10-06
9UXO OXGR1 oxoglutarate Oxoglutarate 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 maleic acid pubchem gtoplig chembl_ligand drugbank
Agonist 3.0 Active 10.1038/S44318-026-00823-Y 2026-05-27
8T7H 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 Nanobody 43
quisqualate pubchem gtoplig chembl_ligand drugbank
PAMAgonist 3.3 Intermediate 10.1101/2023.08.29.555158 2023-10-11
9LRD HRH1 H1 Histamine 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 histamine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.2 Active 10.1038/S42003-025-08363-7 2025-06-11
6XBL SMO SMO Oxysterol 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 SAG1.3 pubchem gtoplig chembl_ligand
Cholesterol pubchem drugbank
AgonistAgonist 3.9 Active 10.1038/S41589-020-0646-2 2020-09-30
8YKW SUCR1 succinate Succinate 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 succinic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank
Agonist 2.8 Active 10.1038/S41422-024-00984-7 2024-05-29
7W41 GRPR BB2 Bombesin 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 PD 176252 pubchem gtoplig chembl_ligand
Antagonist 3.0 Inactive 10.1073/PNAS.2216230120 2023-02-22
7T90 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 acetylcholine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.3 Active 2023-01-25
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 pubchem chembl_ligand drug_central pubchem drugbank
Agonist 2.9 Active 10.1016/J.BBRC.2020.08.042 2020-11-04
9WIJ GPR84 GPR84 Orphan 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 GLPG1205 pubchem gtoplig chembl_ligand drugbank
NAM 3.1 Inactive 2026-07-01
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
8Z3O GPR68 GPR68 Proton 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)
3.3 Active 2025-04-23
3NYA ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 7.0-7.0 21-23°C CHEMBL1160734 chembl_ligand pubchem
Antagonist 3.2 Inactive 10.1021/JA105108Q 2010-08-11
8ZPN CXCR4 CXCR4 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 plerixafor pubchem gtoplig chembl_ligand drugbank drug_central
Antagonist 3.3 Inactive 10.1073/PNAS.2425795122 2025-02-26
8PWN 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
Antagonist 2.4 Inactive 10.1038/S42004-023-01014-0 2023-10-25
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 CIDOXEPIN chembl_ligand pubchem chembl_ligand pubchem drugbank drugbank drug_central
doxepin pubchem gtoplig chembl_ligand drugbank
Inverse agonistInverse agonist 3.1 Inactive 10.1038/NATURE10236 2011-06-15
9LR1 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 JN241-9
Agonist 2.5 Active 2026-02-04
7LJC 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 SKF-81297 pubchem gtoplig chembl_ligand chembl_ligand pubchem chembl_ligand pubchem
mevidalen pubchem gtoplig chembl_ligand
AgonistAgo-PAM 3.0 Active 10.1038/S41422-021-00482-0 2021-03-03
8I9S C3AR C3a Complement peptide 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)
3.3 Active 10.1016/J.CELL.2023.09.020 2023-10-18
7EPT AGRD1 ADGRD1 ADGRD 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 N/A N/A 3.0 Active 10.1038/S41586-022-04619-Y 2022-05-11
7X2D 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 tavapadon pubchem gtoplig chembl_ligand drugbank
Agonist 3.3 Active 10.1038/S41467-022-30929-W 2022-06-15
7Y66 C5AR1 C5a1 Complement peptide 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 BM213 pubchem
Agonist 2.9 Active 10.1038/S41422-023-00779-2 2023-03-01
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 drugbank
Agonist 2.6 Active 10.1038/S41422-021-00569-8 2021-11-17
6UOA 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 Apo (no ligand)
6.3 Intermediate 2020-06-10
8GGL 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 c-Epi pubchem
Agonist 3.2 Active 10.1038/S41586-024-07153-1 2024-03-06
7WZ4 GPR88 GPR88 Orphan 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)
3.0 Active 10.1038/S41467-022-30081-5 2022-10-26
7IOT 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
FU163-67 pubchem
AntagonistUnknown 2.3 Inactive 2026-05-20
7T96 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
acetylcholine pubchem gtoplig chembl_ligand drugbank drug_central
PAMAgonist 3.2 Active 2023-01-25
8XFT LGR4 LGR4 Orphan 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 E3 ubiquitin-protein...
R-spondin-2
UnknownAgonist 3.2 Inactive 2024-12-04
7F0T 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 dopamine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.1 Active 10.1126/SCIADV.ABO4158 2022-06-15
9VB5 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
Agonist 3.1 Active 10.1038/S41586-026-10228-W 2026-06-03
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 CHEMBL5184791 chembl_ligand pubchem drugbank
Agonist 3.4 Active 10.1016/J.CELL.2020.08.024 2020-09-23
7EZK 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 (Human) pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank pubchem
Agonist 3.1 Active 10.1038/S41589-021-00841-3 2021-08-25
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 neurotensin NTS8-13
Agonist 2.5 Inactive 10.1126/sciadv.abe5504 2021-02-10
7F6H 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 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot drugbank
Agonist 2.9 Active 10.1038/S41467-022-28399-1 2022-01-05
9JRT 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 TG6-129 pubchem
Antagonist 3.3 Intermediate 2025-10-22
8JLR TAAR1 TA1 Trace amine 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
Agonist 3.0 Active 10.1038/S41586-023-06804-Z 2023-11-15
9M0D 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 Apo (no ligand)
3.4 Active 2025-04-09
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 (Huma... pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank
Agonist 3.2 Active 10.1016/J.STR.2019.12.003 2020-01-15
9F33 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 CHEMBL4551160 chembl_ligand pubchem
Agonist 3.1 Active 2024-09-18
7RBT 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 tirzepatide pubchem gtoplig
LSN3556672 pubchem
AgonistPAM 3.1 Active 10.1073/PNAS.2116506119 2022-04-13
7WY5 AGRL3 ADGRL3 ADGRL B2 (Adhesion) Mouse 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 Active 10.1016/J.MOLCEL.2022.10.009 2022-10-26
7VAB 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 Non-acylated tirzepa...
Agonist 3.2 Active 10.1038/S41467-022-28683-0 2022-03-02
7ING 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
6-chloro-1,3-dihydro... pubchem
AntagonistUnknown 2.2 Inactive 10.1038/S42004-026-02059-7 2026-05-20
8JLZ 5HT6R 5-HT6 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 CHEMBL365751 chembl_ligand pubchem
Agonist 3.1 Active 10.1016/J.BBRC.2023.05.126 2023-06-28
8WC3 TAAR1 TA1 Trace amine 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 ulotaront pubchem gtoplig chembl_ligand drugbank
Agonist 3.0 Active 10.1016/J.CELL.2023.10.014 2023-12-27
9LR2 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 JN241-9
Agonist 3.1 Active 2026-02-04
9MDU CXCR4 CXCR4 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)
2.9 Inactive 2025-09-10
8QW4 FZD3 FZD3 WNT 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)
2.9 Active 10.1038/S41467-024-51451-1 2024-09-04
9VNY 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 CYM5442 pubchem
Agonist 3.7 Active 2026-01-28
8GG3 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 c-Epi pubchem
Agonist 3.1 Active 10.1038/S41586-024-07153-1 2024-03-06
9KT8 HCAR2 HCA2 Hydroxycarboxylic 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 Acifran pubchem
Agonist 2.7 Active 10.1021/ACS.JMEDCHEM.4C02567 2025-12-10
9UXU OPRK κ 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 salvinorin A pubchem gtoplig chembl_ligand chembl_ligand pubchem chembl_ligand pubchem chembl_ligand pubchem drugbank
Agonist 3.6 Active 2026-05-27
7IN5 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 Apo (no ligand)
2.5 Inactive 10.1038/S42004-026-02059-7 2026-05-20
7INR 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
4-(trifluoromethyl)b... pubchem
AntagonistUnknown 2.1 Inactive 10.1038/S42004-026-02059-7 2026-05-20
9O38 TS1R2 TAS1R2 Taste 1 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)
3.0 Active 10.1016/J.CELL.2025.04.021 2025-05-14
8ZR5 GP119 GPR119 GPR18, GPR55 and GPR119 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 DS-8500a pubchem gtoplig chembl_ligand
Agonist 3.3 Active 2024-06-19
8JXV HRH4 H4 Histamine 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 clozapine pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem
Agonist 3.2 Active 10.1038/S41467-024-46840-5 2024-03-20
4BV0 NTR1 NTS1 Neurotensin A (Rhodopsin) Rat NAE. coli BL21(DE3)Bacteria 3 chemicals 3 steps vapour diffusionsitting drops 5 chems 9.4-9.4 4°C Neurotensin pubchem
Agonist 3.1 Inactive 10.1073/PNAS.1317903111 2014-01-29
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
9JEQ HRH3 H3 Histamine 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 histamine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.1 Active 10.1038/S41401-025-01633-4 2025-09-24
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
7IOB 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
FU35-42 pubchem
AntagonistUnknown 2.1 Inactive 2026-05-20
9XHI 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 C-C motif chemokine ...
Agonist 3.2 Active 10.1073/PNAS.2533975123 2026-04-22
5TE5 OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drop 4 chems 5.2-6.6 4°C 10,20-Methanoretinal pubchem
Inverse agonist 4.0 Inactive 10.1073/PNAS.1617446114 2017-03-15
8WU1 CNR1 CB1 Cannabinoid 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 MDMB-Fubinaca pubchem gtoplig
Agonist 3.2 Active 10.1016/J.CELL.2023.11.017 2024-03-20
9M54 NPFF2 NPFF2 Neuropeptide FF/neuropeptide AF 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 Neuropeptide VF pubchem
Agonist 3.2 Active 10.1016/J.CELREP.2025.116160 2025-07-23
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-9990614 pubchem
Antagonist 4.2 Inactive 10.1038/S41589-018-0131-3 2018-12-05
8ZSS TAAR1 TA1 Trace amine 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 RO5256390 pubchem gtoplig chembl_ligand
Agonist (partial) 3.1 Active 2024-07-24
7V6A ACM4 M4 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 CHEMBL6164470 chembl_ligand pubchem
Allosteric agonist 3.6 Active 10.1038/S41467-022-30595-Y 2022-05-11
6UO8 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 CHEMBL112710 chembl_ligand pubchem pubchem
GS39783 pubchem gtoplig chembl_ligand
AgonistAgo-PAM 3.6 Active 10.1038/S41586-020-2408-4 2020-06-10
9JQY 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 TG6-129 pubchem
Antagonist 2.9 Inactive 2025-10-22
9LGM GPR4 GPR4 Proton 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)
2.8 Active 10.1038/S41422-025-01092-W 2025-04-23
7DTW 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)
4.5 Inactive 10.1038/S41422-021-00474-0 2021-03-10
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 chembl_ligand pubchem drugbank pubchem pubchem
Inverse agonist 3.4 Inactive 10.1038/NATURE10867 2012-02-22
8WOG SUCR1 succinate Succinate 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 succinic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank
Agonist 3.0 Active 10.1016/J.CELREP.2024.114381 2024-09-11
7INU 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
F336 pubchem
AntagonistUnknown 2.5 Inactive 2026-05-20
9GG5 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 U46619 pubchem gtoplig chembl_ligand
Cholesterol pubchem drugbank
AgonistPAM 3.3 Active 10.1038/S41467-026-69844-9 2025-08-27
9UXN OXGR1 oxoglutarate Oxoglutarate 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 succinic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank
Agonist 2.7 Active 10.1038/S44318-026-00823-Y 2026-05-27
8GE8 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 c-Epi pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
8Y51 BRS3 BB3 Bombesin 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)
3.3 Active 2025-02-12
8WC5 TAAR1 TA1 Trace amine 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 Tetramethylammonium pubchem drugbank
Agonist 3.3 Active 10.1016/J.CELL.2023.10.014 2023-12-27
9JFV GPR4 GPR4 Proton 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)
2.7 Active 10.1038/S41422-025-01092-W 2025-04-23
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 pubchem
Antagonist 2.7 Inactive 10.1038/S41586-018-0046-X 2018-04-25
9B5Y 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... pubchem
Agonist 3.5 Active 10.1073/PNAS.2426178122 2025-03-19
8E3Y 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 PACAP-27 (Human) pubchem gtoplig uniprot uniprot uniprot uniprot pubchem
Agonist 2.3 Active 10.1038/S41467-022-34629-3 2022-11-23
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)
6.0 Inactive 10.7554/ELIFE.68578 2021-09-22
7WQ4 GALR2 GAL2 Galanin 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 galanin(1-13)amide gtoplig pubchem
Agonist 2.6 Active 10.1038/S41467-022-29072-3 2022-04-20
8XXX 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 CXCL6
Agonist 3.2 Active 10.1016/J.MOLCEL.2025.01.024 2025-01-15
8H4L FFAR4 FFA4 Free fatty 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 docosahexaenoic acid pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.1 Active 10.1038/S41422-023-00835-X 2023-06-21
6H7M 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 levosalbutamol pubchem gtoplig chembl_ligand drug_central drugbank
Agonist (partial) 2.8 Active 10.1126/SCIENCE.AAU5595 2018-10-17
4K5Y CRHR1 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
Inverse agonist 3.0 Inactive 10.1038/NATURE12357 2013-07-17
9P0K CXCR3 CXCR3 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 CXCL9
Agonist (partial) 3.5 Active 10.1126/SCIADV.ADZ3767 2026-04-29
9JVM GPR4 GPR4 Proton A (Rhodopsin) Western clawed frog 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)
2.4 Active 10.1016/J.CELL.2024.12.001 2025-02-26
7EW7 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 SEW2871 pubchem gtoplig chembl_ligand
Agonist 3.3 Active 10.1038/S41422-021-00566-X 2021-09-29
7TRP ACM4 M4 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 LY2033298 pubchem gtoplig chembl_ligand
iperoxo pubchem gtoplig chembl_ligand
PAMAgonist 2.4 Active 2023-05-17
7UL4 OPRM μ Opioid 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 alvimopan pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem
Inverse agonist 2.8 Inactive 10.1038/S41594-022-00859-8 2022-06-29
8JEI HCAR3 HCA3 Hydroxycarboxylic 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 4-(<i>n</i>-propyl)a... pubchem gtoplig chembl_ligand
Agonist 2.7 Active 10.1016/J.CELREP.2024.114895 2024-11-20
7WVY 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 Aβ42 pubchem
Agonist 3.0 Active 10.1038/S41467-022-29361-X 2022-04-13
6D26 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 fevipiprant pubchem gtoplig chembl_ligand drugbank
Antagonist 2.8 Inactive 10.1016/J.MOLCEL.2018.08.009 2018-10-03
9ODM OPRM μ Opioid 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 DAMGO pubchem gtoplig chembl_ligand pubchem
Agonist 2.8 Active 2026-03-04
9KVH 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 Cinobufotenine
PtdIns4P pubchem
AgonistPAM 2.6 Active 2025-12-03
6ME3 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 CHEMBL15060 chembl_ligand pubchem
Agonist 2.9 Inactive 10.1038/S41586-019-1141-3 2019-04-24
9KVG 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 5-MeO-DMT pubchem gtoplig chembl_ligand drugbank
PtdIns4P pubchem
AgonistPAM 2.6 Active 10.34133/RESEARCH.0987 2025-12-03
7WXU AGRF1 ADGRF1 ADGRF 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 N/A N/A 2.9 Active 10.1038/S41467-022-33173-4 2022-09-28
9LDX O6C76 OR6C76 Olfactory family 6 O2 (Olfactory/extra-nasal 2) 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 drugbank
Benzophenone pubchem drugbank
PAMAgonist 2.8 Active 10.1016/J.CELL.2025.12.017 2026-01-28
4O9R SMO SMO Oxysterol F (Frizzled) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 5 chems 7.4-7.4 20°C cyclopamine pubchem gtoplig chembl_ligand
Antagonist 3.2 Inactive 10.1038/NCOMMS4309 2014-03-05
8JMT AGRL3 ADGRL3 ADGRL 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 Apo (no ligand)
3.3 Inactive 10.1038/S41589-023-01389-0 2023-09-06
7IP6 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 FU293-80 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.1 Inactive 10.1038/S42004-026-02059-7 2026-05-20
7YU5 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 ONO-0740556 pubchem
Agonist 3.3 Active 10.1038/S41467-022-33121-2 2022-10-05
3ODU 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 2.5 Inactive 10.1126/SCIENCE.1194396 2010-10-27
7YU6 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 ONO-0740556 pubchem
Agonist 3.5 Active 10.1038/S41467-022-33121-2 2022-10-05
2YCX ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 2 chemicals 2 steps vapour diffusionNA 3 chems 6.9-7.3 NA 4-{[(2S)-3-(tert-but... pubchem drugbank
Antagonist 3.3 Inactive 10.1073/PNAS.1100185108 2011-06-01
8UY0 OR2T2 OR2T2 Olfactory family 2 O2 (Olfactory/extra-nasal 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A S-carvone pubchem
Agonist 3.2 Active 10.1038/S41586-024-08126-0 2024-10-30
7EJ0 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 (-)-noradrenaline pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Agonist 3.2 Active 10.1126/SCIADV.ABJ5347 2022-04-13
7F4I 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 SHU9119 pubchem
Calcium pubchem
Agonist (partial)PAM 3.1 Active 10.1038/S41422-021-00557-Y 2021-09-08
7YP7 AGRG2 ADGRG2 ADGRG B2 (Adhesion) Mouse 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)
3.1 Active 2022-08-24
5WF6 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 2.9 Active 10.1016/J.STR.2017.12.013 2018-02-21
8YNA HRH4 H4 Histamine 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 immepip pubchem gtoplig chembl_ligand
Agonist 2.6 Active 2024-10-09
7IPF 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 FU428-16
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 1.9 Inactive 2026-05-20
9NOZ OPSD Rhodopsin Opsin (sight) 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 Megabody 7 (Mb7)
NAM 3.5 Inactive 10.1073/PNAS.2532336123 2026-02-18
7INV 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 5-chloropyridin-3-ol pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.6 Inactive 10.1038/S42004-026-02059-7 2026-05-20
8SG1 CML1 chemerin Chemerin receptor 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 chemerin C-terminal ... pubchem gtoplig chembl_ligand pubchem
Agonist 2.9 Active 10.1371/JOURNAL.PBIO.3002188 2023-11-01
6ZG9 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 GSK1034702 pubchem
Agonist 2.5 Inactive 10.1016/J.CELL.2021.11.001 2021-10-06
9VV6 OXGR1 oxoglutarate Oxoglutarate 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 Itaconic acid pubchem
Agonist 2.6 Active 2026-07-15
9ODF OPRM μ Opioid 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 LOFENTANIL chembl_ligand pubchem drugbank
Agonist 2.4 Active 10.1038/S41586-025-10056-4 2026-03-04
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
Na+ pubchem
AntagonistNAM 2.5 Active 10.1126/SCIADV.AAX2518 2019-10-30
7CKZ 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 dopamine pubchem gtoplig chembl_ligand drugbank drug_central
mevidalen pubchem gtoplig chembl_ligand
AgonistPAM 3.1 Active 10.1016/J.CELL.2021.01.028 2021-03-03
9JFT GPR65 GPR65 Proton 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)
3.3 Active 10.1038/S41422-025-01092-W 2025-08-13
7RKM US28 US28 Unclassified A (Rhodopsin) strain AD169 N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Fractalkine
Agonist (partial) 3.5 Active 10.1126/SCIADV.ABL5442 2022-01-26
7EW4 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 CYM-5541 pubchem gtoplig chembl_ligand
Agonist 3.2 Active 10.1038/S41422-021-00567-W 2021-09-29
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 ADM pubchem
Agonist 2.4 Active 10.1021/ACSPTSCI.9B00080 2020-04-01
8ZX5 GPR55 GPR55 GPR18, GPR55 and GPR119 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 AM251 pubchem gtoplig chembl_ligand
Agonist 3.0 Active 2024-11-13
9D3G 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 CHEMBL6177228 chembl_ligand pubchem
OXM1 pubchem
Allosteric antagonistAllosteric antagonist 3.3 Inactive 2024-09-11
3VW7 PAR1 PAR1 Proteinase-activated A (Rhodopsin) Human BaculovirusSf9Insect 6 chemicals 6 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 6.0-6.5 20°C vorapaxar pubchem gtoplig chembl_ligand drug_central drugbank
Antagonist 2.2 Active 10.1038/NATURE11701 2012-12-12
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 glucagon-like peptid... pubchem gtoplig uniprot uniprot uniprot chembl_ligand pubchem
Agonist 4.1 Active 10.1038/NATURE22394 2017-05-24
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
5YWY 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 Fab001 (chain H)
ONO-AE3-208 pubchem gtoplig pubchem
Fab001 (chain L)
Allosteric antagonistAntagonistAllosteric antagonist 3.2 Inactive 10.1038/S41589-018-0131-3 2018-12-05
7T9M TSHR TSH 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 CS-17 Fab (chain L)
CS-17 Fab (chain H)
Inverse agonistInverse agonist 3.1 Inactive 10.1038/S41586-022-05159-1 2022-08-10
7YS6 5HT6R 5-HT6 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 3.0 Active 2023-03-29
7V3Z CNR1 CB1 Cannabinoid 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 CP55940 pubchem gtoplig chembl_ligand
Agonist 3.3 Active 10.1021/JACS.1C06847 2021-11-24
8DWG MRGX1 MRGPRX1 Orphan 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 bovine adrenal medul... pubchem gtoplig chembl_ligand uniprot
CHEMBL5177388 chembl_ligand pubchem
AgonistPAM 2.7 Active 10.1038/S41589-022-01173-6 2022-11-02
8E9W ACM3 M3 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 CHEMBL73538 chembl_ligand pubchem
Agonist 2.7 Active 10.1038/S41586-022-05489-0 2022-11-30
8IHJ HCAR3 HCA3 Hydroxycarboxylic 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 Acifran pubchem
Agonist 3.1 Active 10.1038/S41467-023-41650-7 2023-08-30
8H0P NMBR BB1 Bombesin 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 NMB30
Agonist 3.2 Active 10.1038/S41422-022-00743-6 2023-08-09
9UXP OXGR1 oxoglutarate Oxoglutarate 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 Itaconic acid pubchem
Agonist 2.9 Active 10.1038/S44318-026-00823-Y 2026-05-27
9BJK OPRM μ Opioid 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 Compound 368 pubchem
naloxone pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem
NAMAntagonist 3.3 Inactive 2024-07-17
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 rat amylin pubchem
Agonist 2.2 Active 10.1126/SCIENCE.ABM9609 2022-03-23
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 2011-03-30
8ZFA GPR4 GPR4 Proton A (Rhodopsin) Western clawed frog 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)
3.0 Active 10.1016/J.CELL.2024.12.001 2025-02-26
9NS9 FFAR2 FFA2 Free fatty 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 CHEMBL5965059 chembl_ligand pubchem
CHEMBL4176503 chembl_ligand pubchem
Ago-PAMAgonist 3.3 Active 2025-06-25
7W40 GRPR BB2 Bombesin 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 Bombesin (6-14) [D-P...
Agonist 3.0 Active 2023-02-22
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
Agonist 3.7 Active 10.1038/S41467-021-27760-0 2022-01-12
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
NAM 5.9 Inactive 10.1073/PNAS.2115849118 2022-01-19
9CIB HCAR2 HCA2 Hydroxycarboxylic acid 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 compound (+)17a [PMI... pubchem gtoplig chembl_ligand chembl_ligand pubchem pubchem
Agonist 2.6 Active 10.1016/J.CELL.2024.11.001 2025-05-14
8HMV GPR21 GPR21 Orphan 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)
2.9 Active 10.1002/MCO2.205 2023-03-01
8S2T 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 LEVISOPRENALINE chembl_ligand pubchem drug_central
Agonist 3.3 Active 10.1016/J.STR.2025.07.020 2025-05-21
8DPF 5HT2C 5-HT2C 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 lorcaserin pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.8 Active 10.1016/J.CELREP.2022.111211 2022-08-24
9LQY 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 azelaprag pubchem gtoplig chembl_ligand chembl_ligand pubchem
Agonist 2.4 Inactive 2026-02-04
9IV1 AGRD1 ADGRD1 ADGRD 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 dihydrotestosterone pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.0 Active 10.1016/J.CELL.2025.01.006 2025-02-12
9KB7 LGR4 LGR4 Orphan 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-spondin-2
Agonist 4.0 Inactive 10.1038/S41467-025-64129-Z 2025-10-15
9EBI AA3R A3 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 piclidenoson pubchem gtoplig chembl_ligand chembl_ligand pubchem drugbank
Agonist 3.6 Active 10.1038/S41467-025-62872-X 2025-08-20
9HB3 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 Mambaquaretin-1 K39A
Inverse agonist 2.5 Inactive 10.1038/S41467-025-59114-5 2025-06-04
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 TMP-301 pubchem gtoplig chembl_ligand
NAM 2.6 Inactive 10.1021/acs.jmedchem.5b00892 2015-08-12
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 ICI118551 pubchem gtoplig chembl_ligand
Inverse agonist 2.6 Inactive 10.1107/S2052252519013137 2019-11-13
8GGS 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 c-Epi pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
7XBX CX3C1 CX3CR1 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 Cholesterol pubchem drugbank
PAM 3.4 Active 2022-07-13
5EN0 OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine Stable_cellsHEK293S(TetR)GnTI-Mammalian 1 chemicals 1 steps vapour diffusionSitting drop 4 chems 5.0-5.0 4°C all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 2.8 Active 10.15252/EMBR.201642671 2016-08-10
7AUE 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 drugbank
Calcium pubchem
AgonistCofactor 3.0 Active 10.1126/SCIENCE.ABF7958 2021-04-28
2Z73 OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Japanese flying squid NANativeSquid 1 chemicals 1 steps vapour diffusionsitting drops 5 chems 6.4-6.4 4°C all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Inverse agonist 2.5 Inactive 10.1038/NATURE06925 2008-05-13
8F0J 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 San45
N-hexadecanoyl-L-glu... pubchem
AgonistAgonist 2.0 Active 10.1038/S41589-023-01393-4 2023-08-02
9JR3 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 Parathyroid hormone
Agonist 2.8 Active 2024-10-16
9AS7 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 2.7 Active 10.1038/S41467-025-57956-7 2025-04-02
8ZBJ SSR5 SST5 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 drugbank drug_central pubchem
Agonist 2.9 Active 2025-04-30
6V9S 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 JH112 pubchem gtoplig chembl_ligand
Antagonist 3.5 Inactive 10.1073/PNAS.2002704117 2020-07-15
8KFX CCR8 CCR8 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 CHEMBL5268017 chembl_ligand pubchem
Agonist 3.0 Active 10.1126/SCIADV.ADJ7500 2024-02-07
8X8N SSR5 SST5 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 octreotide pubchem gtoplig chembl_ligand drugbank pubchem pubchem
Agonist 2.9 Active 2024-06-12
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 Alpha-MSH pubchem
Calcium pubchem
AgonistPAM 3.0 Active 10.1038/S41422-021-00557-Y 2021-09-08
8T6J 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 CDPPB pubchem gtoplig chembl_ligand
Ago-PAM 3.5 Inactive 10.1101/2023.08.29.555158 2023-10-11
8ZBI SSR3 SST3 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 drugbank drug_central pubchem
Agonist 2.8 Active 2025-04-30
9UY3 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 Anamorelin pubchem
Agonist 2.5 Active 2025-07-02
9PEE 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 OXM2
PF-07054894 pubchem gtoplig chembl_ligand
Allosteric antagonistAllosteric antagonist 3.4 Inactive 2025-10-01
8HNM CXCR3 CXCR3 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 CHEMBL2220409 chembl_ligand pubchem
Agonist 2.9 Active 10.1038/S41594-023-01175-5 2023-11-29
9KT9 HCAR1 HCA1 Hydroxycarboxylic 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 3,5-dihydroxybenzoic... pubchem gtoplig chembl_ligand
Agonist 2.7 Active 10.1021/ACS.JMEDCHEM.4C02567 2025-12-10
9K20 P2RY2 P2Y2 P2Y 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 ATP pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.7 Active 10.1038/S41421-025-00797-X 2025-06-11
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
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
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 sovateltide pubchem gtoplig chembl_ligand pubchem drugbank
Agonist (partial) 2.7 Inactive 10.1038/S41467-018-07094-0 2018-11-21
8YKD AGRG2 ADGRG2 ADGRG B2 (Adhesion) Mouse N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A PRASTERONE chembl_ligand pubchem drugbank
Agonist 2.9 Active 10.1038/S41589-025-01896-2 2025-08-13
8Z3Y GPR4 GPR4 Proton 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)
3.2 Active 10.1016/J.MOLCEL.2025.03.018 2025-06-04
8UHB TAAR1 TA1 Trace amine 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 CHEMBL3684869 chembl_ligand pubchem
Agonist 3.4 Active 10.1038/S41467-023-44601-4 2024-01-10
9V2N 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 macimorelin pubchem gtoplig chembl_ligand drugbank
Agonist 2.6 Active 2025-07-02
9KFK RL3R2 RXFP4 Relaxin family peptide 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 Relaxin-3 (chain A)
Relaxin-3 (chain B)
AgonistAgonist 3.0 Active 10.1038/S42003-025-08220-7 2025-08-13
7SK9 ACKR3 ACKR3 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 CCX662 pubchem
Agonist (partial) 3.7 Active 10.1126/SCIADV.ABN8063 2022-07-27
8U8F GPR3 GPR3 Orphan 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 palmitic acid pubchem gtoplig chembl_ligand drugbank
Agonist 3.5 Active 10.1021/ACS.BIOCHEM.3C00647 2024-03-06
8WG7 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 Apo (no ligand)
2.5 Active 10.1038/S41421-024-00649-0 2024-03-06
8F7X OPRX NOP 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 nociceptin/orphanin ... pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 3.3 Active 10.1016/J.CELL.2022.12.026 2022-12-14
5TZY FFAR1 FFA1 Free fatty acid A (Rhodopsin) Human BaculovirusSf21Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 6.3-6.8 20°C MK-8666 chembl_ligand pubchem drugbank
AP8 pubchem
Agonist (partial)Ago-PAM 3.2 Active 2017-06-07
7XXI P2Y12 P2Y12 P2Y 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 2MeSADP pubchem gtoplig chembl_ligand
Agonist 3.0 Active 2023-06-07
5ZKP 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 foropafant pubchem gtoplig chembl_ligand
Antagonist 2.8 Other 10.1038/S41594-018-0068-Y 2018-06-20
6FK9 OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine BaculovirusHEK293S(TetR)-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 4.5-4.5 20°C RS09 pubchem
Agonist 2.6 Active 10.1073/PNAS.1718084115 2018-04-04
8TQB GRM3 mGlu3 Metabotropic glutamate C (Glutamate) Rat N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A LY379268 pubchem gtoplig chembl_ligand pubchem
Agonist 3.3 Active 2024-07-31
7LCI 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 pubchem gtoplig chembl_ligand drugbank
Agonist 2.9 Active 10.1016/J.STR.2021.04.008 2021-01-20
9W0O 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 Apo (no ligand)
3.0 Active 10.1093/PROCEL/PWAF068 2026-06-03
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 RGT1383 pubchem
Agonist 4.2 Active 10.1038/S41422-020-0384-8 2020-08-26
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 uniprot
Agonist 3.0 Active 10.1038/S41594-021-00645-Y 2021-10-13
12JA CNR2 CB2 Cannabinoid 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 '1029
Agonist 2.9 Active 2026-07-15
8Y0H CXCR3 CXCR3 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 CHEMBL2221034 chembl_ligand pubchem
Agonist 3.5 Active 2025-02-26
8KEX MRGX4 MRGPRX4 Orphan 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 DCA-3P pubchem
Agonist 3.2 Active 10.1016/J.CELL.2024.10.001 2024-11-06
5X7D ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 3 chemicals 3 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 7 chems 7.5-7.5 20°C CHEMBL4225747 chembl_ligand pubchem pubchem
(S)-carazolol pubchem drugbank
NAMInverse agonist 2.7 Inactive 10.1038/NATURE23652 2017-08-16
7IOP 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
FU163-33 pubchem
AntagonistUnknown 1.9 Inactive 2026-05-20
8GGT 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 c-Epi pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
9ME1 CXCR4 CXCR4 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 Stromal cell-derived...
Agonist 3.4 Inactive 10.1038/S41467-025-63815-2 2025-09-10
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
9UPM Q9XSX4 OPN1LW Opsin (sight) A (Rhodopsin) Crab-eating macaque N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Inverse agonist 3.2 Inactive 10.1126/SCIENCE.ADZ3996 2026-06-24
8J9N FZD1 FZD1 WNT 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)
3.5 Active 10.1038/S41421-023-00627-Y 2024-01-17
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 (partial) 2.7 Active 10.1126/SCIENCE.AAU5595 2018-10-17
5IUB 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°C CHEMBL184061 chembl_ligand pubchem
Antagonist 2.1 Inactive 10.1021/acs.jmedchem.6b00653 2016-06-29
5L7I SMO SMO Oxysterol F (Frizzled) Human Transient_transfectionHEK293S(TetR)-GnTI-Mammalian 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 8 chems 6.0-6.0 20°C vismodegib pubchem gtoplig chembl_ligand drugbank drug_central
Antagonist 3.3 Inactive 10.1038/NATURE18934 2016-07-20
8ZBW 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 Quin-C1 pubchem
Agonist 2.6 Active 2025-09-10
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 pubchem chembl_ligand drug_central pubchem drugbank
Agonist 2.3 Active 10.1038/S41467-020-17791-4 2020-08-12
6FKB OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine BaculovirusHEK293S(TetR)-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 4.5-4.5 20°C RS13 pubchem
Agonist 3.0 Active 10.1073/PNAS.1718084115 2018-04-04
7S1M 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 Ex4-D-Ala
Agonist 2.4 Active 10.1038/S41589-021-00945-W 2022-01-05
8YUV HRH3 H3 Histamine 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 immepip pubchem gtoplig chembl_ligand
Agonist 3.0 Active 2024-06-05
8XIP SSR1 SST1 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 pasireotide pubchem gtoplig drugbank chembl_ligand drug_central
Agonist 3.3 Active 2024-07-03
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 ADM2 (Adrenomedullin...
Agonist 2.3 Active 10.1021/ACSPTSCI.9B00080 2020-04-01
7IP3 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 FU273-23 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.1 Inactive 2026-05-20
2HPY OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 5.9-6.1 283 K all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 2.8 Inactive 10.1073/PNAS.0601765103 2006-08-22
3PXO OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drops 3 chems 5.0-5.8 4°C all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 3.0 Active 10.1038/NATURE09789 2011-03-09
9UYL CML2 chemerin 2 Chemerin receptor 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 Chemerin
Agonist 3.3 Active 10.1126/SCIENCE.ADT8794 2025-11-19
7INT 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 F293 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.3 Inactive 2026-05-20
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
7EW0 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 ozanimod pubchem gtoplig drug_central chembl_ligand drugbank
Agonist 3.4 Active 10.1038/S41422-021-00566-X 2021-09-29
8T3S FFAR2 FFA2 Free fatty 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 butyric acid pubchem gtoplig chembl_ligand drugbank chembl_ligand pubchem chembl_ligand pubchem
Agonist 3.1 Active 10.1126/SCIADV.ADJ2384 2024-01-24
7Y35 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 abaloparatide drug_central pubchem
Agonist 2.9 Active 2023-07-05
4JKV SMO SMO Oxysterol 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
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 chembl_ligand pubchem pubchem
Antagonist 3.0 Inactive 10.1016/J.STR.2015.07.024 2015-10-21
7AD3 STE2 STE2 STE2 D1 (Ste2-like fungal pheromone) strain ATCC 204508 / S288c N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Alpha-factor mating ... pubchem
Agonist 3.5 Active 10.1038/S41586-020-2994-1 2020-12-09
20YC GP174 GPR174 Orphan 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)
3.4 Active 2026-04-15
9P0L CXCR3 CXCR3 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 CXCL10
Agonist (partial) 3.1 Active 10.1126/SCIADV.ADZ3767 2026-04-29
8ZF6 GPR4 GPR4 Proton A (Rhodopsin) Western clawed frog 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)
3.0 Active 10.1016/J.CELL.2024.12.001 2025-02-26
9LWP BRS3 BB3 Bombesin 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)
2.9 Active 10.1016/J.APSB.2025.06.025 2025-07-16
7T8X 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 acetylcholine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.2 Active 2023-01-25
6KK1 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
7MBY 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 (Human) pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank pubchem
Agonist 2.4 Active 10.1371/JOURNAL.PBIO.3001295 2021-05-26
7IPG 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
FU428-36 (3S-diaster... pubchem pubchem
AntagonistUnknown 2.1 Inactive 2026-05-20
7RA3 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 Gastric inhibitory p... pubchem
Agonist 3.2 Active 10.1073/PNAS.2116506119 2022-04-13
6LML 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 Glucagon pubchem
Agonist 3.9 Active 10.1126/SCIENCE.AAZ5346 2020-04-01
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 METHSCOPOLAMINE chembl_ligand pubchem pubchem drugbank drugbank drug_central chembl_ligand
Inverse agonist 3.0 Inactive 10.1038/S41589-018-0152-Y 2018-11-21
8ZBE SSR5 SST5 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 octreotide pubchem gtoplig chembl_ligand drugbank pubchem pubchem
Agonist 3.2 Active 10.1038/S41401-024-01314-8 2024-07-10
7WIG 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 CHEMBL69303 chembl_ligand pubchem pubchem
Agonist 2.7 Active 10.1038/S41422-022-00669-Z 2022-06-01
7DD6 A0A8I3AZV5 CaS Calcium-sensing C (Glutamate) Chicken N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A D-tryptophan pubchem gtoplig chembl_ligand drugbank pubchem gtoplig chembl_ligand drugbank drug_central
Calcium pubchem
AgonistAgonist 3.2 Active 10.1126/SCIADV.ABG1483 2021-06-16
7E2Z 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 aripiprazole pubchem gtoplig chembl_ligand drugbank drug_central
PtdIns4P pubchem
Agonist (partial)PAM 3.1 Active 10.1038/S41586-021-03376-8 2021-04-14
7C7Q 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 rac-BHFF pubchem
(-)-baclofen pubchem gtoplig chembl_ligand drugbank drugbank
Ago-PAMAgonist 3.0 Active 10.1038/S41422-020-0350-5 2020-07-01
7W55 NMUR2 NMU2 Neuromedin U 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 CHEMBL3315349 chembl_ligand pubchem
Agonist 2.8 Active 10.1038/S41467-022-29683-W 2022-04-20
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
9JQX Q9BML7 GABA-B-R1 Unclassified C (Glutamate) Fruit fly 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
Antagonist 3.6 Inactive 2025-10-01
9L60 OPRK κ 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 MPAM-15 pubchem
Dynorphin A13 pubchem
PAMAgonist 2.9 Active 2025-12-31
6UO9 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 CHEMBL112710 chembl_ligand pubchem pubchem
Agonist 4.8 Intermediate 10.1038/S41586-020-2408-4 2020-06-10
8XYD 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 PAF pubchem gtoplig chembl_ligand drugbank
Agonist 2.9 Active 10.1016/J.CELREP.2024.114422 2024-11-13
7IOK 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
FU113-99 pubchem
AntagonistUnknown 2.3 Inactive 2026-05-20
9JRO 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 PF-04418948 pubchem gtoplig chembl_ligand drugbank
Antagonist 3.5 Intermediate 2025-10-22
9NNZ OPSD Rhodopsin Opsin (sight) 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)
3.9 Inactive 10.1073/PNAS.2532336123 2026-02-18
7WVV 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-formyl-MLFII (fM5)
Agonist 2.9 Active 10.1038/S41467-022-29361-X 2022-04-13
9PPW 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 naltrindole pubchem gtoplig chembl_ligand
Antagonist 3.3 Active 10.1126/SCIADV.AEB6737 2026-03-04
9LL9 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 (R)-DOI pubchem gtoplig chembl_ligand
Agonist 2.8 Active 2026-01-14
11TH CCR4 CCR4 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 FLX475 pubchem gtoplig chembl_ligand drugbank
Antagonist 3.5 Inactive 2026-04-01
8Y6W FFAR2 FFA2 Free fatty 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 CHEMBL4176503 chembl_ligand pubchem
AMG7703 pubchem gtoplig chembl_ligand chembl_ligand pubchem
AgonistAgo-PAM 3.2 Active 2025-04-02
8X8L SSR5 SST5 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 Cortistatin
Agonist 2.7 Active 2024-06-12
9KV6 C3AR C3a Complement peptide 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 TLQP-21 (Human) pubchem gtoplig uniprot
Agonist 2.9 Active 10.1101/2025.05.26.656101 2025-11-26
7T6B S1PR2 S1P2 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
Agonist 3.2 Active 10.1126/SCIADV.ABN0067 2022-04-06
8Y0N CXCR3 CXCR3 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 CHEMBL2221034 chembl_ligand pubchem
Agonist 3.1 Active 2025-02-26
9K26 PRLHR PrRP Prolactin-releasing peptide 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 PrRP31 pubchem
Agonist 3.0 Active 2025-01-29
6NBI 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... pubchem
Agonist 4.0 Active 10.1126/SCIENCE.AAV7942 2019-04-17
8IBU MTLR motilin Motilin 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 erythromycin pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.5 Active 10.1126/SCIADV.ADE9020 2023-04-12
8WA3 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 Apo (no ligand)
2.9 Active 10.1038/S41421-024-00649-0 2024-03-06
8JCU 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
Antagonist 2.8 Inactive 10.1038/S41422-023-00830-2 2023-06-21
9I52 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 19B
Agonist 2.8 Active 2025-07-16
8RW4 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 AzoSwitch2
Antagonist 2.2 Inactive 2025-01-08
8G2Y AGRF1 ADGRF1 ADGRF 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 Apo (no ligand)
3.4 Active 10.1038/S41467-023-38083-7 2023-05-10
9M4Q ADA1A α1A 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 doxazosin pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem pubchem
Antagonist 3.0 Inactive 2025-07-02
7S8O MRGX2 MRGPRX2 Orphan 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)-ZINC-3573 pubchem gtoplig chembl_ligand
Agonist 2.6 Active 10.1038/S41586-021-04126-6 2021-11-17
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 chembl_ligand pubchem pubchem drugbank
ADX55164 pubchem
AgonistAgo-PAM 3.2 Active 10.1038/S41586-021-03680-3 2021-07-07
6VMS 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 3.8 Active 10.1038/S41586-020-2379-5 2020-06-17
6TP6 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 filorexant pubchem gtoplig chembl_ligand drugbank
Antagonist 2.3 Inactive 10.1021/acs.jmedchem.9b01787 2020-01-01
8FU6 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 Glucagon derivative ...
Agonist 2.9 Active 10.1016/J.CELL.2023.02.028 2023-04-12
8EJC FFAR1 FFA1 Free fatty 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 fasiglifam pubchem gtoplig chembl_ligand drugbank
Agonist (partial) 3.0 Active 10.1073/PNAS.2219569120 2023-05-24
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
Agonist 2.6 Inactive 10.1073/PNAS.2102813118 2021-08-25
7X9B 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 NEUROPEPTIDE-Y chembl_ligand pubchem
Agonist 3.4 Active 10.1126/SCIADV.ABM1232 2022-05-18
8FX5 ACM4 M4 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 xanomeline pubchem gtoplig chembl_ligand drug_central drugbank
xanomeline pubchem gtoplig chembl_ligand drug_central drugbank
PAMAgonist 2.5 Active 10.1038/S41467-023-41199-5 2023-09-13
9V1H NPFF2 NPFF2 Neuropeptide FF/neuropeptide AF 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 GUB08248
Agonist 2.9 Active 10.1038/S41401-025-01741-1 2026-02-04
6WW2 FZD5 FZD5 WNT 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)
3.7 Inactive 10.7554/ELIFE.58464 2020-08-19
9UWD PD2R DP1 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 Apo (no ligand)
3.4 Intermediate 10.1073/PNAS.2501902122 2025-05-28
7YAC 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 paltusotine pubchem gtoplig chembl_ligand drugbank chembl_ligand
Agonist 3.2 Active 10.1038/S41467-023-36673-Z 2023-04-19
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 rat amylin pubchem
Agonist 3.3 Active 10.1126/SCIENCE.ABM9609 2022-03-23
8DZS OPRK κ 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 CHEMBL277863 chembl_ligand pubchem
Agonist 2.7 Active 10.1038/S41586-023-06030-7 2023-05-03
6P9X CRHR1 CRF1 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 corticorelin drug_central pubchem
Agonist 2.9 Active 10.1016/J.MOLCEL.2020.01.012 2020-02-05
9MB9 GRM8 mGlu8 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 (S)-3,4-DCPG pubchem gtoplig chembl_ligand
VU0422288 pubchem gtoplig chembl_ligand
AgonistAgo-PAM 3.0 Active 2025-10-01
8IKH CNR1 CB1 Cannabinoid 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 CB-05 pubchem
Allosteric agonist 3.3 Active 10.1073/PNAS.2321532121 2024-06-05
8JH7 FZD6 FZD6 WNT 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)
3.2 Active 10.1038/S41421-023-00627-Y 2024-01-17
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
8JPB 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 SBI-553 pubchem gtoplig chembl_ligand
NTS8–13 pubchem
Ago-PAMAgonist 3.1 Active 10.1038/S41586-023-06395-9 2023-08-09
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
9W6W 5HT5A 5-HT5A 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-CT pubchem gtoplig chembl_ligand
Agonist 3.1 Active 10.1186/S43556-025-00359-3 2025-11-26
7EQ1 AGRG5 ADGRG5 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 N/A N/A 3.3 Active 10.1038/S41586-022-04619-Y 2022-05-11
5KW2 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 8.5-8.5 20°C Compound 1 pubchem
Agonist 2.8 Active 10.1038/S41467-017-01240-W 2018-05-02
7BU6 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 (-)-noradrenaline pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Agonist 2.7 Active 10.1038/S41422-020-00424-2 2020-12-02
9PPX 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 naltrexone pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem
Antagonist 3.0 Active 2026-03-04
7X5H 5HT5A 5-HT5A 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-CT pubchem gtoplig chembl_ligand
Agonist 3.1 Active 10.1038/S41421-022-00412-3 2022-09-14
9M1U OXGR1 oxoglutarate Oxoglutarate 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 succinic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank
Agonist 2.6 Active 10.1038/S44318-026-00823-Y 2026-06-17
9IQT HCAR2 HCA2 Hydroxycarboxylic 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 nicotinic acid pubchem gtoplig chembl_ligand drugbank drug_central drugbank drugbank
Agonist 2.9 Active 10.1016/J.JMB.2024.168795 2024-10-02
9V38 C5AR2 C5a2 Complement peptide 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 EP54
Agonist 3.3 Active 10.1016/J.MOLCEL.2026.06.002 2026-07-01
8DZP OPRK κ 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 CHEMBL180126 chembl_ligand pubchem chembl_ligand pubchem
Agonist 2.7 Active 10.1038/S41586-023-06030-7 2023-05-03
7F1Q 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 N/A N/A 2.9 Active 2021-07-14
9EEA 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 adenosine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.4 Active 10.1038/S41467-025-56434-4 2025-04-09
7IPD 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 7-chloroquinolin-2(1... pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.2 Inactive 2026-05-20
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 Active 10.1038/S41594-018-0068-Y 2018-06-20
8JIM HCAR2 HCA2 Hydroxycarboxylic 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 monomethyl fumarate pubchem gtoplig chembl_ligand drugbank pubchem
Agonist 3.0 Active 10.1016/J.MOLCEL.2023.07.030 2023-09-06
2Y03 ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 1 chemicals 1 steps vapour diffusionsitting drops 6 chems 8.5-8.5 4°C LEVISOPRENALINE chembl_ligand pubchem drug_central
Agonist 2.9 Inactive 2011-01-12
8SZH 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 spermine pubchem gtoplig chembl_ligand drugbank
Calcium pubchem
D-tryptophan pubchem gtoplig chembl_ligand drugbank pubchem gtoplig chembl_ligand drugbank drug_central
cinacalcet pubchem gtoplig chembl_ligand drugbank drug_central
Ago-PAMAgonistAgonistPAM 3.1 Active 10.1038/S41586-024-07055-2 2024-02-07
9OPY TS1R2 TAS1R2 Taste 1 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)
3.5 Inactive 10.1038/S41422-025-01156-X 2025-09-03
9EAI 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 losartan pubchem gtoplig chembl_ligand drugbank drug_central
Nanobody AT206
AntagonistPAM 3.1 Inactive 10.1073/PNAS.2423931122 2025-03-05
9VB6 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
Agonist 3.4 Active 10.1038/S41586-026-10228-W 2026-06-03
8XVE 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 BQ 3020 pubchem gtoplig
Agonist 3.0 Active 10.1038/S41421-024-00705-9 2024-08-28
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 gtoplig
Agonist 3.4 Active 10.1038/S41467-022-28683-0 2022-03-02
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 chembl_ligand pubchem
Antagonist 3.4 Inactive 10.1126/SCIENCE.1215904 2012-02-15
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 (+)-LSD pubchem gtoplig pubchem gtoplig chembl_ligand drugbank drug_central
Agonist (partial) 3.4 Inactive 10.1016/J.CELL.2020.08.024 2020-09-23
8GE9 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 c-Epi pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
8U4S CXCR4 CXCR4 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 REGN7663 Fab (chain ...
REGN7663 Fab (chain ...
Inverse agonistInverse agonist 3.4 Active 10.1038/S41594-024-01397-1 2024-03-13
8UNS 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 c-Epi pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
6TO7 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 suvorexant pubchem gtoplig chembl_ligand drug_central drugbank
Antagonist 2.3 Inactive 10.1021/acs.jmedchem.9b01787 2020-01-01
8XT9 LGR4 LGR4 Orphan 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)
3.1 Inactive 2025-01-15
7YON 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 CHEMBL439904 chembl_ligand pubchem
Agonist 3.0 Active 10.1016/J.STR.2022.11.010 2023-03-22
9JKV HCAR3 HCA3 Hydroxycarboxylic 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 IBC 293 pubchem gtoplig chembl_ligand
Agonist 3.3 Active 2025-10-29
9JFK UR2R UT Urotensin 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 P5U
Agonist 3.2 Active 10.1016/J.JBC.2025.110794 2025-12-03
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 10.1038/S41467-021-25364-2 2021-08-18
8K9L OPRM μ 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 DAMGO pubchem gtoplig chembl_ligand pubchem
BMS-986122 pubchem
AgonistPAM 3.1 Active 10.1038/S41467-024-47792-6 2024-05-29
8VY7 T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A compound 28.1 [PMID:... pubchem gtoplig chembl_ligand
Cholesterol pubchem drugbank
Ago-PAMAgonist 2.7 Active 2024-04-03
8FD0 OPSD Rhodopsin Opsin (sight) 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 Nanobody Nb2
Allosteric antagonist 3.7 Inactive 10.1038/S41467-023-40911-9 2023-08-30
5VBL APJ apelin Apelin A (Rhodopsin) Human BaculovirusSf21Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 7 chems 6.1-6.1 20-22°C AMG3054
Agonist 2.6 Inactive 10.1016/J.STR.2017.04.008 2017-05-31
6GDG AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusTni PRO (Trichoplusia ni) cell linesInsect 1 chemicals 1 steps Cryo-EMFalcon III detector , 300kV, FEI TITAN Krios microscope, Volta PhasePlate, GIF-quantum energy filter (Gatan) 4 chems 7.5-7.5 4°C NECA pubchem gtoplig chembl_ligand
Agonist 4.1 Active 10.7554/ELIFE.35946 2018-05-16
9M8P GPR3 GPR3 Orphan 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 AF64394 pubchem
N-oleoylethanolamide pubchem gtoplig chembl_ligand drugbank
NAMAgonist 3.4 Active 2025-09-24
9JCO GPR4 GPR4 Proton 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 Lysophosphatidylchol... pubchem
PAM 2.4 Active 2025-07-09
8RWC 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 StilSwitch2 pubchem
Antagonist 2.3 Inactive 2025-01-08
9VB0 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
Agonist 3.2 Active 10.1038/S41586-026-10228-W 2026-06-03
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
7T94 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
acetylcholine pubchem gtoplig chembl_ligand drugbank drug_central
PAMAgonist 3.2 Active 2023-01-25
7T9N TSHR TSH 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 M22 Fab (chain H)
M22 Fab (chain L)
AgonistAgonist 2.9 Active 10.1038/S41586-022-05159-1 2022-08-03
5LWE CCR9 CCR9 Chemokine A (Rhodopsin) Human BaculovirusSf21Insect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 7.9-8.0 20°C vercirnon pubchem gtoplig chembl_ligand drugbank
Allosteric antagonist 2.8 Inactive 10.1038/NATURE20606 2016-12-07
6WI9 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 pubchem chembl_ligand drug_central pubchem drugbank
Agonist 4.3 Active 10.1038/S41467-020-17791-4 2020-08-12
8GEB 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 c-Epi pubchem
Agonist 3.6 Active 10.1038/S41586-024-07153-1 2024-03-06
8XOI GPER1 GPER Estrogen (G protein-coupled) 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)
3.2 Active 10.1038/S41422-024-00963-Y 2024-04-10
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
8IRT 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 rotigotine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.7 Active 10.1038/S41422-023-00808-0 2023-06-07
6FFI 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 methoxy-MPEP pubchem gtoplig chembl_ligand
NAM 2.2 Inactive 10.1021/ACS.JMEDCHEM.7B01722 2018-03-07
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 pubchem drugbank drug_central
Antagonist 2.5 Inactive 10.1126/SCIENCE.ABL8615 2022-01-26
9IZG 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 LPA pubchem
Agonist 3.0 Active 2025-01-01
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
8GUS CNR2 CB2 Cannabinoid 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 CHEMBL2179724 chembl_ligand pubchem
Agonist 3.0 Active 10.1038/S41467-023-37112-9 2023-05-10
6RZ6 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-2570366 pubchem gtoplig
Antagonist 2.4 Active 10.1038/S41467-019-13348-2 2019-12-11
9YDR 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 MIPS3983
DADLE pubchem gtoplig chembl_ligand drugbank pubchem
PAMAgonist 2.1 Active 2025-12-10
9VJG 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 CHEMBL26998 chembl_ligand pubchem
Agonist 2.7 Active 2025-11-12
9W0R T2R46 TAS2R46 Taste 2 T2 (Taste 2) 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)
2.7 Active 10.1038/S41594-026-01786-8 2026-04-22
8SMV GP161 GPR161 Orphan 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 Cholesterol pubchem drugbank
Allosteric agonist 2.7 Active 10.1101/2023.05.23.540554 2024-02-21
8JXR 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 (+)-LSD pubchem gtoplig pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.6 Active 10.1016/J.NEURON.2024.07.003 2024-09-04
8U4Q CXCR4 CXCR4 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 REGN7663 Fab (chain ...
REGN7663 Fab (chain ...
Inverse agonistInverse agonist 3.4 Active 10.1038/S41594-024-01397-1 2024-03-13
7IN4 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 Apo (no ligand)
2.7 Inactive 10.1038/S42004-026-02059-7 2026-05-20
8GGC 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 c-Epi pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
7Y12 MRGRD MRGPRD Orphan 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 β-alanine pubchem gtoplig chembl_ligand drugbank
Agonist 3.1 Active 10.1038/S42003-022-03668-3 2022-07-20
8YH3 AA3R A3 Adenosine A (Rhodopsin) Sheep N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL383144 chembl_ligand pubchem
Agonist 3.4 Active 10.1038/S41467-024-53473-1 2024-11-06
8GE4 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 c-Epi pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06
8I2G FSHR FSH 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 Follitropin (FSH) (c...
Follitropin (FSH) (c...
Cpd-21f pubchem
AgonistAgonistAllosteric agonist 2.8 Active 10.1038/S41467-023-36170-3 2023-03-29
1L9H OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 6.0-6.0 4°C all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Inverse agonist 2.6 Inactive 10.1073/PNAS.082666399 2002-05-15
9NOT TS1R2 TAS1R2 Taste 1 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)
3.8 Active 10.1016/J.CELL.2025.04.021 2025-05-14
9II3 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 L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem pubchem drugbank
Agonist 3.9 Inactive 10.1038/S41589-025-01858-8 2025-03-05
8DZQ OPRK κ 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 CHEMBL180126 chembl_ligand pubchem chembl_ligand pubchem
Agonist 2.8 Active 10.1038/S41586-023-06030-7 2023-05-03
8IY9 HCAR2 HCA2 Hydroxycarboxylic 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 nicotinic acid pubchem gtoplig chembl_ligand drugbank drug_central drugbank drugbank
Agonist 3.4 Active 10.1038/S41467-024-46239-2 2024-03-06
7T11 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 octreotide pubchem gtoplig chembl_ligand drugbank pubchem pubchem
Agonist 2.7 Active 10.1038/S41594-022-00727-5 2022-03-09
8IYW HCAR2 HCA2 Hydroxycarboxylic 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 GSK256073 pubchem gtoplig
Agonist 3.5 Active 10.1038/S41467-024-46239-2 2024-03-06
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
3ZEV NTR1 NTS1 Neurotensin A (Rhodopsin) Rat NAE. coli BL21(DE3)Bacteria 3 chemicals 3 steps vapour diffusionsitting drops 7 chems 9.4-9.4 4°C Neurotensin pubchem
Agonist 3.0 Inactive 10.1073/PNAS.1317903111 2014-01-29
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 afamelanotide pubchem gtoplig chembl_ligand chembl_ligand pubchem drugbank drug_central
Calcium pubchem
AgonistPAM 2.9 Active 10.1038/S41422-021-00557-Y 2021-09-08
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
Antagonist 4.0 Inactive 10.1016/J.CELREP.2021.109648 2021-09-08
6NBF 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... pubchem
Agonist 3.0 Active 10.1126/SCIENCE.AAV7942 2019-04-17
9M0Z Q5QNQ1 taar13d Unclassified A (Rhodopsin) Zebrafish N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Cadaverine pubchem drugbank
Agonist 2.7 Active 2026-03-04
5UIG AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps vapour diffusionSitting drop 6 chems 7.0-7.0 20°C Cmpd-1 pubchem
Antagonist 3.5 Inactive 10.1073/PNAS.1621423114 2017-02-08
9L84 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 ATAZANAVIR chembl_ligand pubchem drugbank
(-)-adrenaline pubchem gtoplig chembl_ligand drugbank drug_central
Ago-PAMAgonist 3.2 Active 10.1016/J.CELL.2025.12.023 2025-12-31
6LN2 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 3.2 Inactive 10.1038/S41467-020-14934-5 2020-03-18
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 chembl_ligand pubchem chembl_ligand pubchem
Antagonist 2.9 Inactive 10.1038/NATURE10939 2012-03-21
7FD8 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
Agonist 3.8 Intermediate 10.1016/J.CELREP.2021.109648 2021-09-08
20ZD 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
Agonist 2.8 Active 10.1038/S41586-026-10228-W 2026-06-03
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
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 GHRH (Human) pubchem gtoplig uniprot
Agonist 2.6 Active 10.1038/S41467-020-18945-0 2020-11-18
7YMJ ADA1A α1A 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 tamsulosin pubchem gtoplig chembl_ligand drugbank drug_central
Antagonist 3.4 Inactive 10.1038/S41467-023-39310-X 2023-07-05
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
7RG9 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 Apo (no ligand)
3.2 Active 10.1073/PNAS.2116506119 2022-04-13
8S4D 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 CMF-019 pubchem gtoplig chembl_ligand
Agonist 2.6 Inactive 2024-12-04
8XBH GPR34 GPR34 Orphan 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 CHEMBL4758243 chembl_ligand pubchem
Agonist 2.8 Active 2023-12-27
7S0F 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 LEVISOPRENALINE chembl_ligand pubchem drug_central
Agonist 3.0 Active 10.1038/S41594-021-00679-2 2021-11-17
9AVL 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 CYCLOMETHYLTRYPTOPHA... pubchem
Calcium pubchem
tecalcet pubchem gtoplig chembl_ligand
AgonistAgonistPAM 3.8 Active 2024-04-17
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 pubchem
Agonist 2.8 Active 10.1126/SCIENCE.AAY9813 2020-02-19
8GDZ 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 c-Epi pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
8JGF MRGX1 MRGPRX1 Orphan 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 bovine adrenal medul... pubchem gtoplig chembl_ligand uniprot
Agonist 2.7 Active 10.1038/S41467-023-40705-Z 2024-01-10
8GEC 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 c-Epi pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
6FKD OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine BaculovirusHEK293S(TetR)-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 4.5-4.5 20°C RS16 pubchem
Agonist 2.5 Active 10.1073/PNAS.1718084115 2018-04-04
9P88 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 NTS8–13 pubchem
Agonist 2.9 Active 10.1038/S41586-026-10120-7 2026-03-25
8FYE 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 CHEMBL352186 chembl_ligand pubchem
Agonist 2.9 Active 10.1038/S41586-024-07403-2 2024-05-15
9EE9 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 adenosine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.2 Active 10.1038/S41467-025-56434-4 2025-04-09
8VVG OPRK κ 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 GB18 pubchem
Inverse agonist 3.3 Active 2025-01-15
5MZP 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 caffeine pubchem gtoplig chembl_ligand drugbank drug_central
Antagonist 2.1 Inactive 10.1016/j.str.2017.06.012 2017-07-26
5JTB 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 2.8 Inactive 10.1126/SCIADV.1602952 2017-05-31
8W89 TAAR1 TA1 Trace amine 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 &beta;-phenylethylam... pubchem gtoplig chembl_ligand drugbank pubchem
Agonist 3.0 Active 10.1038/S41586-023-06775-1 2023-11-22
9V81 MRGX4 MRGPRX4 Orphan 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 HEP-50768 gtoplig pubchem
Inverse agonist 2.6 Active 2026-05-06
7YK6 RL3R2 RXFP4 Relaxin family peptide 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 CHEMBL4522365 chembl_ligand pubchem
Agonist 3.0 Active 10.1038/S41467-023-36182-Z 2023-03-01
8RW7 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 CHEMBL3736368 chembl_ligand pubchem
Antagonist 2.3 Inactive 2025-01-08
4XNV P2RY1 P2Y1 P2Y A (Rhodopsin) Human BaculovirusSf9Insect 6 chemicals 6 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 6.5-6.5 20°C BMS compound 16 [PMI... pubchem gtoplig chembl_ligand
Allosteric antagonist 2.2 Active 10.1038/NATURE14287 2015-04-01
9M2S TA13C taar13c Orphan A (Rhodopsin) Zebrafish N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Cadaverine pubchem drugbank
Agonist 2.8 Active 2026-03-04
8J6R HCAR2 HCA2 Hydroxycarboxylic 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 MK 6892 pubchem gtoplig chembl_ligand pubchem
Agonist 2.8 Active 10.1038/S41467-023-43537-Z 2023-12-06
8WVV LGR4 LGR4 Orphan 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)
3.4 Inactive 2024-10-30
8UGW 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 CGS 21680 pubchem gtoplig chembl_ligand chembl_ligand pubchem
Agonist 3.9 Active 2024-12-18
4S0V OX2R OX2 Orexin A (Rhodopsin) Human BaculovirusSf9Insect 9 chemicals 9 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 5.9-6.0 20°C suvorexant pubchem gtoplig chembl_ligand drug_central drugbank
Antagonist 2.5 Inactive 10.1038/NATURE14035 2015-01-14
8DZR OPRK κ 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 CHEMBL277863 chembl_ligand pubchem
Agonist 2.6 Active 10.1038/S41586-023-06030-7 2023-05-03
7IO7 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
FU18-60 pubchem
AntagonistUnknown 2.2 Inactive 2026-05-20
20ZC 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
Agonist 2.6 Active 10.1038/S41586-026-10228-W 2026-06-03
9V4D C5AR2 C5a2 Complement peptide 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 R8Y
Agonist 3.1 Active 10.1016/J.MOLCEL.2026.06.002 2026-07-01
7UL3 HRH2 H2 Histamine 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 famotidine pubchem
Antagonist 3.0 Intermediate 10.1038/S41594-022-00859-8 2022-06-29
8J18 GPR84 GPR84 Orphan 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 (3R)-3-HYDROXYDODECA... pubchem drugbank
Agonist 2.9 Active 10.1038/S41467-023-38985-6 2023-06-21
24XB FFAR4 FFA4 Free fatty 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 Apo (no ligand)
2.7 Active 2026-07-08
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
Ago-PAM 2.3 Active 10.1038/NATURE13494 2014-07-16
8WGD 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 CPPG pubchem
LY341495 pubchem
AntagonistAntagonist 4.5 Inactive 10.1038/S41467-024-54744-7 2024-11-27
4XES 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 7.0-7.4 20°C NTS8–13 pubchem
Agonist 2.6 Active 10.1038/NCOMMS8895 2015-07-29
9UPN Q9XSX2 OPN1MW3 Unclassified A (Rhodopsin) Crab-eating macaque N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Inverse agonist 3.4 Inactive 10.1126/SCIENCE.ADZ3996 2026-06-24
9UPO Q9XSX2 OPN1MW3 Unclassified A (Rhodopsin) Crab-eating macaque N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Inverse agonist 3.7 Inactive 10.1126/SCIENCE.ADZ3996 2026-06-24
7Y15 MRGRD MRGPRD Orphan 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)
2.9 Active 10.1038/S42003-022-03668-3 2022-07-20
4N6H OPRD δ Opioid A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 7 chems 6.1-6.2 20-23°C naltrindole pubchem gtoplig chembl_ligand
Na+ pubchem
AntagonistNAM 1.8 Inactive 10.1038/NATURE12944 2013-12-25
8WSS MCHR1 MCH1 Melanin-concentrating 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 melanin-concentratin... pubchem gtoplig uniprot uniprot uniprot
Agonist 3.0 Active 10.1038/S41421-024-00679-8 2024-06-19
8GUR CNR2 CB2 Cannabinoid 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 CP55940 pubchem gtoplig chembl_ligand
Agonist 2.8 Active 10.1038/S41467-023-37112-9 2023-05-10
7CUM 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 CGP 54626A pubchem gtoplig chembl_ligand
Antagonist 3.5 Inactive 10.1016/J.JMB.2020.09.023 2020-11-11
5D5A 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 (S)-carazolol pubchem drugbank
Inverse agonist 2.5 Inactive 10.1107/S2059798315021683 2016-01-13
9IZD HCAR1 HCA1 Hydroxycarboxylic 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 CHEMBL2146910 chembl_ligand pubchem
Agonist 3.2 Active 2025-04-02
9JG1 HRH4 H4 Histamine 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 adriforant pubchem gtoplig chembl_ligand drugbank
Antagonist 3.6 Inactive 2025-12-03
8JHY HCAR2 HCA2 Hydroxycarboxylic 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 compound 9n [PMID: 1... pubchem gtoplig chembl_ligand
Ago-PAM 2.9 Active 10.1016/J.MOLCEL.2023.07.030 2023-09-06
9EW2 FZD7 FZD7 WNT 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)
3.2 Active 2024-10-02
8UO2 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 c-Epi pubchem
Agonist 3.6 Active 10.1038/S41586-024-07153-1 2024-03-06
9KWG C5AR1 C5a1 Complement peptide 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 C5A pubchem
Agonist 3.2 Active 10.1101/2025.05.26.656101 2025-11-26
9YGZ OPSG OPN1MW Opsin (sight) 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 all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 3.0 Active 10.1016/J.BPJ.2026.03.029 2026-05-20
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 6-11 pubchem
Agonist 3.2 Active 10.1038/S41589-021-00890-8 2021-11-03
6KUY 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 (2S)-4-fluoro-2-(1H-... pubchem
Agonist (partial) 3.2 Inactive 2019-12-04
21CI 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 vornorexant pubchem gtoplig chembl_ligand
Antagonist 3.3 Inactive 2026-06-03
9PA3 OPRM μ 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 3-OH-PCP pubchem
Agonist (partial) 3.1 Active 2026-07-01
8JBH NK3R NK3 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 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 2.9 Active 2024-02-07
7TRY CRHR2 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 3.7 Active 10.1038/S41467-022-33851-3 2022-11-09
8XGU KISSR kisspeptin Kisspeptin 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 TAK448
Agonist 3.0 Active 10.1126/SCIADV.ADN7771 2024-10-30
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 Active 10.1126/science.1232808 2013-03-13
8ZJD KISSR kisspeptin Kisspeptin 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 kisspeptin-10 (Human... pubchem gtoplig chembl_ligand
Agonist 3.1 Active 2024-07-03
1GZM OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionsitting drops 3 chems 8.5-8.5 18°C all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Inverse agonist 2.7 Inactive 10.1016/J.JMB.2004.08.090 2003-11-20
8XIO SSR1 SST1 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 L-797591 pubchem
Agonist 2.7 Active 2024-07-03
9JKQ TAAR1 TA1 Trace amine 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 METHAMPHETAMINE chembl_ligand pubchem drugbank drug_central
Agonist 2.7 Active 10.1021/ACS.JMEDCHEM.4C01961 2024-10-16
6N52 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 Apo (no ligand)
4.0 Inactive 10.1038/S41586-019-0881-4 2019-01-23
7IOI 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 FU101-88 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.0 Inactive 2026-05-20
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
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 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 2.9 Active 10.1126/SCIADV.ABK2872 2021-12-15
7IO3 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 FU7-29 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.2 Inactive 2026-05-20
8SZF 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 D-tryptophan pubchem gtoplig chembl_ligand drugbank pubchem gtoplig chembl_ligand drugbank drug_central
Calcium pubchem
spermine pubchem gtoplig chembl_ligand drugbank
cinacalcet pubchem gtoplig chembl_ligand drugbank drug_central
AgonistAgonistAgonistPAM 2.8 Active 10.1038/S41586-024-07055-2 2024-02-07
9AUC 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 gene-rela...
Agonist 2.4 Active 10.1021/ACS.BIOCHEM.4C00114 2024-04-24
8K6N 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 NEUROPEPTIDE-Y chembl_ligand pubchem
Agonist 3.2 Active 2024-07-31
9M8V GPR3 GPR3 Orphan 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 AF64394 pubchem
NAM 3.8 Active 2025-09-24
9UVW 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 CHEMBL4303142 chembl_ligand pubchem drugbank chembl_ligand
Antagonist 2.9 Inactive 2026-05-06
9BUD 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 cagrilintide pubchem gtoplig drugbank
Agonist 2.5 Active 2025-04-23
8JBF NK3R NK3 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 senktide pubchem gtoplig chembl_ligand chembl_ligand pubchem pubchem
Agonist 3.0 Active 10.1038/S41421-023-00564-W 2024-02-28
8HNL CXCR3 CXCR3 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 PS372424 pubchem
Agonist 3.0 Active 10.1038/S41594-023-01175-5 2023-11-29
9WQO GRM1 mGlu1 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 chembl_ligand pubchem pubchem drugbank
Agonist 2.9 Active 10.1126/SCIADV.AEE0044 2026-05-27
8K4N GPR34 GPR34 Orphan 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-azanyl-3-[oxi...
Agonist 2.8 Active 2023-10-25
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 Oxyntomodulin pubchem pubchem
Agonist 3.3 Active 10.1038/S41467-021-27760-0 2022-01-12
9LDV O6C76 OR6C76 Olfactory family 6 O2 (Olfactory/extra-nasal 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ethyl (2R,3S)-3-meth... pubchem
Cholesterol pubchem drugbank
AgonistPAM 2.8 Active 2026-01-28
9XB1 V1AR V1A 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 Apo (no ligand)
2.8 Inactive 10.1038/S41467-026-68331-5 2026-02-04
9JH6 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 Cer(d18:0/20:0) pubchem
Agonist 2.9 Active 2025-04-30
7VUY MRGX2 MRGPRX2 Orphan 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 CHEMBL5665416 chembl_ligand pubchem pubchem
Agonist 2.8 Active 10.1038/S41586-021-04077-Y 2021-12-01
7IN3 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 Apo (no ligand)
2.7 Inactive 10.1038/S42004-026-02059-7 2026-05-20
7XW7 TSHR TSH 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 K1-70 scFv
Antagonist 5.5 Inactive 10.1038/S41586-022-05173-3 2022-08-17
7SUS 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 CHEMBL5812344 chembl_ligand pubchem
Agonist 2.7 Inactive 10.1038/S41594-022-00797-5 2022-07-27
6ORV 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 CHEMBL3950796 chembl_ligand pubchem
Allosteric agonist 3.0 Active 10.1038/s41586-019-1902-z 2020-01-08
9WQM GRM1 mGlu1 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 chembl_ligand pubchem pubchem drugbank
Ro0711401 pubchem gtoplig chembl_ligand
AgonistPAM 3.3 Active 2026-05-27
5WB1 US28 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 Apo (no ligand)
3.5 Active 10.7554/ELIFE.35850 2018-06-13
5OM1 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 2.1 Inactive 10.1038/S41598-017-18570-W 2018-01-17
8KFZ CCR8 CCR8 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)
3.3 Active 10.1126/SCIADV.ADJ7500 2024-02-07
8JJO 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 3.4 Inactive 10.1038/S41589-023-01389-0 2023-09-06
6WIV 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 Phosphatidylcholine ... pubchem
Calcium pubchem
NAMPAM 3.3 Inactive 10.1038/S41586-020-2452-0 2020-07-01
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
8GE7 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 c-Epi pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
9W0U T2R46 TAS2R46 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A TANGERETIN chembl_ligand pubchem
Agonist 2.9 Active 2026-04-22
25ST TA2R4 TAS2R4 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A L-Trp-Trp-Trp pubchem gtoplig chembl_ligand
Agonist 3.0 Active 2026-06-24
7Y64 C5AR1 C5a1 Complement peptide 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 C5a anaphylatoxin
Agonist 2.9 Active 10.1038/S41422-023-00779-2 2023-03-01
7XJI ADRB3 β3 Adrenoceptors A (Rhodopsin) Dog N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Solabegron pubchem
Agonist 3.9 Active 10.1016/J.BBRC.2022.04.065 2022-05-04
7XK9 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 CHEMBL6913 chembl_ligand pubchem
Agonist 3.4 Active 2023-04-26
9LFA 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 CHEMBL1254945 chembl_ligand pubchem
Antagonist 3.5 Inactive 2026-05-27
8J1A GPR84 GPR84 Orphan 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)
3.2 Active 10.1038/S41467-023-38985-6 2023-06-21
9JCL P2RY1 P2Y1 P2Y 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 ADP pubchem gtoplig chembl_ligand
Agonist 2.8 Active 2025-09-10
7YFC HRH4 H4 Histamine 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 histamine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.0 Active 10.1038/S41467-023-42260-Z 2023-10-25
9WDI C5AR2 C5a2 Complement peptide 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 mC5a-desArg
Agonist 3.3 Active 10.1016/J.MOLCEL.2026.06.002 2026-07-01
6Z8N 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 SRI-9829 pubchem
Agonist 2.8 Intermediate 10.1126/sciadv.abe5504 2021-02-10
7VV6 MRGX2 MRGPRX2 Orphan 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 3.3 Active 10.1038/S41586-021-04077-Y 2021-12-01
8YNS MCHR1 MCH1 Melanin-concentrating 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 CHEMBL242004 chembl_ligand pubchem
Antagonist 3.3 Inactive 2024-12-18
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
7IN6 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 Apo (no ligand)
2.5 Inactive 10.1038/S42004-026-02059-7 2026-05-20
9CBM 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 dexmedetomidine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.2 Active 10.1038/S12276-024-01296-X 2024-09-11
7D68 GLP2R GLP-2 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 glucagon-like peptid... pubchem gtoplig uniprot pubchem
Agonist 3.0 Active 10.1038/S41422-020-00442-0 2020-12-16
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-B (Human) pubchem gtoplig chembl_ligand uniprot
Agonist 3.2 Active 10.1038/S41467-021-21087-6 2021-02-10
7EJ8 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 brimonidine (UK14304... pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.0 Active 10.1126/SCIADV.ABJ5347 2022-04-13
7VFX 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 fMIFL pubchem
Agonist 2.8 Active 10.1038/S41467-022-32822-Y 2022-09-21
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
Agonist 3.3 Active 10.1038/S41467-020-16820-6 2020-06-24
6LI2 GPR52 GPR52 Orphan 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)
2.8 Inactive 10.1038/S41586-020-2019-0 2020-02-26
9W2I NK2R NK2 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 Peptide 336 (P336) s...
Agonist 2.9 Active 2026-06-17
7X10 AGRL3 ADGRL3 ADGRL B2 (Adhesion) Mouse 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 Active 10.1016/J.MOLCEL.2022.10.009 2022-11-09
8HA0 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 PTH pubchem
Agonist 2.6 Active 10.1038/S41401-022-01032-Z 2022-12-21
7F1S 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 Apo (no ligand)
2.8 Active 10.1038/S41467-021-24438-5 2021-07-14
5UNG 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
4RWS CXCR4 CXCR4 Chemokine A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 5.5-5.5 20°C vMIP-II
Antagonist 3.1 Inactive 10.1126/SCIENCE.1261064 2015-02-11
6N4B CNR1 CB1 Cannabinoid 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 MDMB-Fubinaca pubchem gtoplig
Agonist 3.0 Active 10.1016/J.CELL.2018.11.040 2019-01-30
9AS4 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 (+)-LSD pubchem gtoplig pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.1 Active 10.1038/S41467-025-57956-7 2025-04-02
7X2V AGRF1 ADGRF1 ADGRF 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 N/A N/A 3.1 Active 10.1038/S41467-022-33173-4 2022-09-28
7XW6 TSHR TSH 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 ML-109 pubchem
M22 antibody (chain ...
M22 antibody (chain ...
Allosteric agonistAgonistAgonist 2.8 Active 10.1038/S41586-022-05173-3 2022-08-17
8EF6 OPRM μ 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 morphine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.2 Active 10.1016/J.CELL.2022.09.041 2022-11-09
8XVL EDNRA ETA 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 zibotentan pubchem gtoplig chembl_ligand drugbank
Antagonist 3.2 Inactive 2024-08-28
9PA2 OPRM μ 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 PHENCYCLIDINE chembl_ligand pubchem drugbank pubchem drug_central
Agonist (partial) 2.9 Active 10.1038/S41594-026-01839-Y 2026-07-01
8XBE GPR34 GPR34 Orphan 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 CHEMBL4782438 chembl_ligand pubchem
Agonist 3.4 Active 10.1038/S41467-024-45046-Z 2024-05-15
7INJ 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
F148 pubchem
AntagonistUnknown 2.1 Inactive 2026-05-20
7E9G 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
JNJ-40411813 pubchem gtoplig chembl_ligand drugbank
DN13
AgonistPAMPAM 3.5 Active 10.1038/S41586-021-03495-2 2021-06-23
8HDP AA2BR A2B 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 3.2 Active 10.1038/S41421-022-00503-1 2023-01-18
6BQH 5HT2C 5-HT2C 5-Hydroxytryptamine A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 5 chems 6.0-6.0 20°C ritanserin pubchem gtoplig chembl_ligand drugbank
Inverse agonist 2.7 Inactive 10.1016/j.cell.2018.01.001 2018-02-14
8TZQ 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 dopamine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.2 Active 10.1038/S41467-024-50964-Z 2024-08-21
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
Unknown 2.9 Active 10.1038/NATURE22035 2017-04-05
9MBD GRM8 mGlu8 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)
3.3 Inactive 10.1016/J.MOLCEL.2025.08.019 2025-10-01
9UJM 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 pimavanserin pubchem gtoplig chembl_ligand drug_central drugbank
Inverse agonist 3.1 Inactive 2026-04-29
8GY7 ACTHR MC2 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 ACTH (Corticotropin)
Calcium pubchem
AgonistCofactor 3.3 Active 10.1038/S41422-022-00751-6 2023-01-11
8JLJ TAAR1 TA1 Trace amine 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 CHEMBL1182312 chembl_ligand pubchem
Agonist 3.1 Active 10.1038/S41586-023-06804-Z 2023-11-15
9F34 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 CHEMBL4551160 chembl_ligand pubchem
Agonist 3.1 Active 2024-09-18
9JHP GPR4 GPR4 Proton 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)
3.4 Active 10.1038/S41422-025-01092-W 2025-04-23
8GG2 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 c-Epi pubchem
Agonist 3.0 Active 10.1038/S41586-024-07153-1 2024-03-06
8XQP T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A aristolochic acid pubchem gtoplig chembl_ligand
Cholesterol pubchem drugbank
Allosteric agonistAgonist 3.3 Active 10.1038/S41586-024-07569-9 2024-07-10
9BI6 GPR68 GPR68 Proton 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)
2.9 Active 10.1016/J.CELL.2024.11.036 2025-01-15
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 compound 43 [PMID: 2... pubchem gtoplig chembl_ligand
Agonist 3.0 Active 10.1038/S41467-022-28586-0 2022-03-30
23SO OPRM μ 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 cebranopadol pubchem gtoplig chembl_ligand chembl_ligand chembl_ligand drugbank
Agonist 3.0 Active 2026-07-01
9E2A 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(7-36)NH2 pubchem
Agonist 3.3 Active 10.1126/SCIADV.ADW0899 2025-10-29
9NOR TS1R2 TAS1R2 Taste 1 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)
3.4 Active 10.1016/J.CELL.2025.04.021 2025-05-14
7F6I 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 kallidin (Human) pubchem gtoplig uniprot chembl_ligand
Agonist 2.8 Active 10.1038/S41467-022-28399-1 2022-01-05
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
Inverse agonist 2.7 Inactive 10.1038/NATURE25025 2018-01-10
6KO5 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 CHEMBL1956994 chembl_ligand pubchem
Antagonist 3.3 Inactive 10.1038/S41467-020-17554-1 2020-08-12
9B9Z CNR1 CB1 Cannabinoid 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 MRI-1867 pubchem
Inverse agonist 3.3 Inactive 2024-11-20
24QH FFAR4 FFA4 Free fatty 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 Apo (no ligand)
2.7 Active 2026-07-08
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
Antagonist 4.2 Inactive 10.1038/S41422-022-00623-Z 2022-03-16
8HN8 HRH4 H4 Histamine 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 histamine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.0 Active 2023-12-20
8ZQE GPR15 GPR15 Orphan 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 GPR15LC11
Agonist 2.9 Active 10.1038/S41421-024-00698-5 2024-07-10
7WYB AGRL3 ADGRL3 ADGRL B2 (Adhesion) Mouse 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 3.0 Active 10.1016/J.MOLCEL.2022.10.009 2022-10-26
9BSB 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 (+)-LSD pubchem gtoplig pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.3 Active 10.1016/J.NEURON.2025.06.012 2025-09-17
7YAE 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 octreotide pubchem gtoplig chembl_ligand drugbank pubchem pubchem
Agonist 3.4 Active 10.1038/S41467-023-36673-Z 2023-04-19
9N0E 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 Oxyntomodulin pubchem pubchem
Agonist 2.3 Active 2026-04-22
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 fMLFII
Agonist 3.1 Active 10.1038/S41467-022-28586-0 2022-03-30
8WC4 TAAR1 TA1 Trace amine 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 CHEMBL476516 chembl_ligand pubchem
Agonist 3.1 Active 10.1016/J.CELL.2023.10.014 2023-12-27
8G05 GPR84 GPR84 Orphan 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 6-n-octylaminouracil pubchem gtoplig chembl_ligand pubchem
Agonist 3.0 Active 10.1038/S41467-023-41201-0 2023-11-01
7IOS 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
CHEMBL1524252 chembl_ligand pubchem
AntagonistUnknown 2.4 Inactive 2026-05-20
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
9ODJ OPRM μ Opioid 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 Mitragynine pseudoin...
Agonist (partial) 3.0 Active 10.1038/S41586-025-10056-4 2026-01-07
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 PACAP-38 pubchem
Agonist 3.5 Active 10.1038/S41422-020-0280-2 2020-03-11
7XTQ 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 CHEMBL2181246 chembl_ligand pubchem
Agonist 3.2 Active 10.1073/PNAS.2117054119 2022-07-06
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 Calcium pubchem
Alpha-MSH pubchem
CofactorAgonist 3.0 Active 10.1038/S41422-021-00552-3 2021-11-03
5T1A CCR2 CCR2 Chemokine A (Rhodopsin) Human BaculovirusSf21Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 5 chems 6.5-6.5 20 °C. BMS-681 pubchem gtoplig chembl_ligand
CCR2-RA-[R] pubchem gtoplig chembl_ligand
AntagonistAllosteric antagonist 2.8 Inactive 10.1038/NATURE20605 2016-12-14
8GG8 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 c-Epi pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06
9AU0 PD2R DP1 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 CHEMBL1591294 chembl_ligand pubchem pubchem
Agonist 2.5 Active 2025-08-27
9CM3 FFAR2 FFA2 Free fatty 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 CHEMBL4176503 chembl_ligand pubchem
CHEMBL5965059 chembl_ligand pubchem
AgonistAgo-PAM 3.1 Active 2025-06-25
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
8XIR SSR3 SST3 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 pasireotide pubchem gtoplig drugbank chembl_ligand drug_central
Agonist 2.5 Active 2024-07-03
9UYJ CML2 chemerin 2 Chemerin receptor 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 Chemerin
Agonist 3.3 Active 10.1126/SCIENCE.ADT8794 2025-11-19
9LQT 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 Apo (no ligand)
2.6 Inactive 2026-02-04
7TRS ACM4 M4 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 acetylcholine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.8 Active 2023-05-17
9ARX 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 Active 10.1038/S41467-025-57956-7 2025-04-02
6MEO 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 T-cell surface glyco...
Envelope glycoprotei...
AntagonistAntagonist 3.9 Inactive 10.1038/S41586-018-0804-9 2018-12-12
7XT8 5HT4R 5-HT4 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 3.1 Active 10.1016/J.MOLCEL.2022.05.031 2022-07-27
8WWJ MCHR1 MCH1 Melanin-concentrating 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 Apo (no ligand)
3.0 Active 2024-11-13
9IZA HCAR2 HCA2 Hydroxycarboxylic 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 SCH 900271 pubchem gtoplig chembl_ligand drugbank
Agonist 3.1 Active 2025-04-02
8UXY OR1F1 OR1F1 Olfactory family 1 O2 (Olfactory/extra-nasal 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Levomenthol pubchem drugbank
Agonist 3.3 Active 10.1038/S41586-024-08126-0 2024-10-30
6LI1 GPR52 GPR52 Orphan 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)
2.9 Inactive 10.1038/S41586-020-2019-0 2020-02-26
5NJ6 PAR2 PAR2 Proteinase-activated A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 7 chems 5.5-6.2 20°C Apo (no ligand)
4.0 Active 10.1038/NATURE22309 2017-05-03
9IJE ADRB3 β3 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 (-)-adrenaline pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.3 Active 10.1002/CPLU.202400288 2024-08-21
8Y02 OPSB OPN1SW Opsin (sight) 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 all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 2.6 Active 10.1126/SCIENCE.ADZ8141 2025-06-11
7VV4 MRGX2 MRGPRX2 Orphan 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 linear cortistatin-1...
Agonist 3.0 Active 10.1038/S41586-021-04077-Y 2021-12-01
9PXW OPRM μ 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 naloxone pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem
Agonist (partial) 3.8 Active 2025-11-12
8WCB TAAR1 TA1 Trace amine 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 Cyclohexylammonium I... pubchem drugbank pubchem drugbank
Agonist 3.1 Active 10.1016/J.CELL.2023.10.014 2023-12-27
8GGJ 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 c-Epi pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
8W8Q GP101 GPR101 Orphan 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)
2.9 Active 10.1038/S41589-023-01456-6 2024-01-03
9N29 ACM4 M4 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 diphenhydramine pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem pubchem drugbank drugbank pubchem
Agonist 2.6 Active 10.1038/S41392-026-02865-4 2026-07-15
9KPE T2R16 TAS2R16 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A salicin pubchem gtoplig
Agonist 3.4 Active 10.1016/J.CELREP.2025.115604 2025-04-02
9PY2 OPRM μ 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 loperamide pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.2 Active 2025-11-12
7VUZ MRGX2 MRGPRX2 Orphan 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 CHEMBL5665416 chembl_ligand pubchem pubchem
Agonist 2.9 Active 10.1038/S41586-021-04077-Y 2021-12-01
8C9W 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 AB928 pubchem gtoplig chembl_ligand
Antagonist 2.1 Inactive 2023-07-12
7SF8 AGRG1 ADGRG1 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 N/A N/A 2.7 Active 10.1038/S41586-022-04575-7 2022-04-27
7YKD CML1 chemerin Chemerin receptor 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 chemerin C-terminal ... pubchem gtoplig chembl_ligand pubchem
Agonist 2.8 Active 10.1073/PNAS.2214324120 2023-04-19
8KGK GPR61 GPR61 Orphan 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)
3.2 Active 10.1038/S41467-023-41654-3 2023-10-11
9AYF 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 tecalcet pubchem gtoplig chembl_ligand
CYCLOMETHYLTRYPTOPHA... pubchem
Calcium pubchem
PAMAgonistAgonist 3.6 Active 10.1038/S41586-024-07331-1 2024-04-17
8UNT 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 c-Epi pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
9LKD A2RT31 OR5V1 Olfactory family 5 O2 (Olfactory/extra-nasal 2) Mouse N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A PL45 pubchem
Agonist 3.6 Active 2026-01-21
9EJZ ACM5 M5 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 acetylcholine pubchem gtoplig chembl_ligand drugbank drug_central
VU6007678 pubchem gtoplig
AgonistAgo-PAM 2.1 Active 2025-08-13
8THK ADA1A α1A 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 CHEMBL133451 chembl_ligand pubchem
Agonist 2.6 Active 10.1038/S41467-023-40524-2 2023-08-16
8J9O FZD1 FZD1 WNT 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)
3.4 Inactive 10.1038/S41421-023-00627-Y 2024-01-17
9EKH PD2R DP1 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 ONO3030297 pubchem
Inverse agonist 2.9 Intermediate 2025-09-03
8Z8A HCAR1 HCA1 Hydroxycarboxylic 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 D-lactic acid pubchem gtoplig chembl_ligand drugbank pubchem gtoplig chembl_ligand pubchem drugbank pubchem drugbank drugbank pubchem drugbank drugbank drugbank
Agonist 2.8 Active 10.1126/SCISIGNAL.ADW1483 2025-10-29
7T2G OPRM μ Opioid 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 Mitragynine pseudoin...
Agonist (partial) 2.5 Active 10.1038/S41589-022-01208-Y 2022-12-07
7CFN 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 S-EMCA pubchem gtoplig chembl_ligand chembl_ligand pubchem
S-EMCA pubchem gtoplig chembl_ligand chembl_ligand pubchem
Ago-PAMAgonist 3.0 Active 2020-09-09
8WWN MCHR1 MCH1 Melanin-concentrating 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 melanin-concentratin... pubchem gtoplig uniprot uniprot uniprot
Agonist 2.7 Active 10.1038/S41421-024-00754-0 2024-11-13
9LDW O6C76 OR6C76 Olfactory family 6 O2 (Olfactory/extra-nasal 2) 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 drugbank
alpha-Hexylcinnamald... pubchem
PAMAgonist 2.6 Active 2026-01-28
8XOG GPER1 GPER Estrogen (G protein-coupled) 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)
2.9 Active 10.1038/S41422-024-00963-Y 2024-04-10
8XJL PF2R FP 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 PGF<sub>2&alpha;</su... pubchem gtoplig chembl_ligand drug_central pubchem drugbank drugbank
Agonist 2.8 Active 10.1016/J.CELREP.2024.113893 2024-02-28
7JVP 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 SKF-83959 pubchem gtoplig chembl_ligand chembl_ligand pubchem pubchem
Agonist (partial) 2.9 Active 10.1016/J.CELL.2021.01.027 2021-02-24
20ZG 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
Agonist 2.4 Active 10.1038/S41586-026-10228-W 2026-06-03
6GT3 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 imaradenant pubchem gtoplig chembl_ligand drugbank
Antagonist 2.0 Inactive 2019-06-26
7DH5 ADRB3 β3 Adrenoceptors A (Rhodopsin) Dog N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A mirabegron pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.2 Active 10.1016/J.MOLCEL.2021.06.024 2021-08-04
3CAP OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drop 4 chems 5.6-5.6 4°C Apo (no ligand)
2.9 Active 10.1038/NATURE07063 2008-06-24
9KFJ RL3R1 RXFP3 Relaxin family peptide 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 CHEMBL4522365 chembl_ligand pubchem
Agonist 3.1 Active 10.1038/S42003-025-08220-7 2025-08-13
9KZ2 C3AR C3a Complement peptide 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 EP67
Agonist 3.4 Active 10.1073/PNAS.2614459123 2025-11-26
9KFT 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 fMLFC peptide
Agonist 3.1 Active 2025-11-12
8ITM 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 Apo (no ligand)
3.1 Active 10.1073/PNAS.2306145120 2023-10-18
8X2K GPR3 GPR3 Orphan 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-oleoylethanolamide pubchem gtoplig chembl_ligand drugbank
Agonist 3.0 Active 10.1038/S41422-023-00919-8 2024-04-03
8Z87 HCAR1 HCA1 Hydroxycarboxylic 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 CHEMBL2146910 chembl_ligand pubchem
Agonist 2.7 Active 2025-11-05
9IZF 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 LPA pubchem
Agonist 3.1 Active 2025-01-01
7ZLY HCAR2 HCA2 Hydroxycarboxylic 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 Apo (no ligand)
2.7 Active 10.1038/S41467-023-37177-6 2023-04-12
8X16 AA3R A3 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 piclidenoson pubchem gtoplig chembl_ligand chembl_ligand pubchem drugbank
Agonist 3.3 Active 10.1038/S41467-024-47207-6 2024-04-24
9PA6 OPRK κ 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 Apo (no ligand)
3.4 Active 10.1038/S41594-026-01839-Y 2026-07-01
7SR8 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 danavorexton pubchem gtoplig chembl_ligand drugbank
Agonist 3.3 Active 10.1038/S41467-022-30601-3 2022-06-08
8HK3 C3AR C3a Complement peptide 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)
3.2 Active 10.1038/S41589-023-01339-W 2023-05-10
9PLO 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 N-(5-methylnaphthale... pubchem
Agonist 2.8 Active 2025-07-30
7WZ7 AGRF1 ADGRF1 ADGRF 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 N/A N/A 2.8 Active 10.1038/S41467-022-33173-4 2022-09-28
7L0P 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 NTS8–13 pubchem
Agonist 4.1 Active 2021-01-06
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 chembl_ligand pubchem drugbank drug_central drugbank
Agonist 3.8 Active 10.1038/S41421-020-0176-9 2020-08-05
9LMO GPR4 GPR4 Proton 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)
3.2 Active 10.1016/J.MOLCEL.2025.02.030 2025-07-09
9BA0 CNR1 CB1 Cannabinoid 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 monlunabant pubchem gtoplig pubchem
Inverse agonist 3.1 Inactive 2024-11-20
8Y73 OPRM μ 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 MPAM-15 pubchem
DAMGO pubchem gtoplig chembl_ligand pubchem
PAMAgonist 2.8 Active 2025-08-06
8RQQ 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 2.4 Inactive 2024-04-03
11TF CCR4 CCR4 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 zelnecirnon pubchem gtoplig chembl_ligand
Antagonist 3.4 Inactive 2026-04-01
9J31 GPR4 GPR4 Proton A (Rhodopsin) Zebrafish 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)
3.1 Active 10.1038/S41467-025-55901-2 2025-01-22
9PY3 OPRM μ 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 loperamide pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.2 Active 2025-11-12
8ZYT 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 NTS8–13 pubchem
SBI-553 pubchem gtoplig chembl_ligand
AgonistAllosteric agonist 2.7 Active 2025-04-09
8K4S MRGX4 MRGPRX4 Orphan 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 DCA-3P pubchem
Agonist 2.9 Active 10.1016/J.CELL.2024.10.001 2024-11-06
9MEJ CXCR4 CXCR4 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 gp120
Agonist 4.0 Inactive 10.1038/S41467-025-63815-2 2025-09-10
8T3V FFAR1 FFA1 Free fatty 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 docosahexaenoic acid pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.4 Active 10.1126/SCIADV.ADJ2384 2024-01-24
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 chembl_ligand drug_central pubchem
Agonist 3.0 Active 10.1126/SCIENCE.ABM9609 2022-03-23
8XML CCR8 CCR8 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)
2.6 Active 2025-01-01
8UNU 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 c-Epi pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
8HJ0 GPR21 GPR21 Orphan 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)
3.1 Active 10.1038/S41467-023-35882-W 2023-03-15
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 (S)-carazolol pubchem drugbank
Inverse agonist 2.4 Inactive 10.1126/SCIENCE.1150577 2007-10-30
9D3E 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 OXM2
CHEMBL6177228 chembl_ligand pubchem
Allosteric antagonistAllosteric antagonist 3.0 Inactive 2024-09-11
8ZYU 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 NTS8–13 pubchem
SBI-553 pubchem gtoplig chembl_ligand
AgonistAllosteric agonist 2.7 Active 10.1038/S41422-025-01095-7 2025-04-16
9IXX 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 LTD4 pubchem gtoplig chembl_ligand chembl_ligand pubchem drugbank
Agonist 3.2 Active 10.1073/PNAS.2417148122 2025-04-02
7IP0 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 FU223-43 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.0 Inactive 2026-05-20
7Y24 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 octreotide pubchem gtoplig chembl_ligand drugbank pubchem pubchem
Agonist 3.3 Active 10.1038/S41589-022-01130-3 2022-10-19
8F0K 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 San385
Agonist 1.9 Active 10.1038/S41589-023-01393-4 2023-08-02
4PY0 P2Y12 P2Y12 P2Y A (Rhodopsin) Human BaculovirusSf9Insect 6 chemicals 6 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 5.0-6.0 20°C 2MeSATP pubchem gtoplig chembl_ligand
Agonist (partial) 3.1 Active 10.1038/NATURE13288 2014-04-30
8GGB 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 c-Epi pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
6XBK SMO SMO Oxysterol 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 drugbank
Agonist 3.2 Active 10.1038/S41589-020-0646-2 2020-09-30
6FKC OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine BaculovirusHEK293S(TetR)-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 4.5-4.5 20°C RS15 pubchem
Agonist 2.5 Active 10.1073/PNAS.1718084115 2018-04-04
8POK HRH2 H2 Histamine 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 histamine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.4 Active 10.1038/S41467-024-46096-Z 2024-03-06
6M1H 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 maxadilan gtoplig uniprot pubchem
Agonist 3.6 Active 10.1038/S41422-020-0280-2 2020-03-11
9KB9 LGR4 LGR4 Orphan 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-spondin-2
E3 ubiquitin-protein...
AgonistAgonist 3.6 Inactive 10.1038/S41467-025-64129-Z 2025-10-15
9P94 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 PACAP-27 (Human) pubchem gtoplig uniprot uniprot uniprot uniprot pubchem
Agonist 3.0 Active 10.1073/PNAS.2521157122 2025-11-19
7EZC 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 UK-432,097 pubchem gtoplig chembl_ligand drugbank
Agonist 3.8 Active 10.1107/S2052252522001907 2022-04-13
8GNE 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 KW-6356 pubchem
Inverse agonist 2.3 Inactive 10.1124/MOLPHARM.122.000633 2023-03-22
9BUC 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 cagrilintide pubchem gtoplig drugbank
Agonist 3.4 Active 2025-04-23
8JSR 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 anamorelin pubchem gtoplig chembl_ligand drugbank
Agonist 2.9 Active 10.1038/S41594-024-01481-6 2025-01-22
9VMG A0A678XLR1 A0A678XLR1 Orphan A (Rhodopsin) Sea lamprey N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A spermine pubchem gtoplig chembl_ligand drugbank
Agonist 2.8 Active 10.1038/S41421-025-00839-4 2026-05-13
9KVI 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 bufotenine pubchem gtoplig chembl_ligand drugbank
PtdIns4P pubchem
AgonistPAM 2.5 Active 2025-12-03
7DTV 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 D-tryptophan pubchem gtoplig chembl_ligand drugbank pubchem gtoplig chembl_ligand drugbank drug_central
Calcium pubchem
AgonistAgonist 3.5 Active 10.1038/S41422-021-00474-0 2021-03-10
8IY5 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-1 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 2.8 Active 10.7554/ELIFE.85821 2023-08-16
8X9U AGRD1 ADGRD1 ADGRD 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 Metenolone drugbank pubchem
Agonist (partial) 2.9 Active 2025-02-12
9LLJ 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 Agonist-positive all...
GEM targeting TM3/4/...
GEM targeting TM1/2/...
dopamine pubchem gtoplig chembl_ligand drugbank drug_central
Ago-PAMUnknownUnknownAgonist 2.6 Active 2026-03-04
9IJA T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A compound 28.1 [PMID:... pubchem gtoplig chembl_ligand
Allosteric agonist 3.1 Active 2024-07-24
8IHF HCAR2 HCA2 Hydroxycarboxylic 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 MK 6892 pubchem gtoplig chembl_ligand pubchem
Agonist 3.0 Active 10.1038/S41467-023-41650-7 2023-08-30
6DO1 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 S1I8
Agonist (partial) 2.9 Active 10.1016/J.CELL.2018.12.006 2019-01-30
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
Inverse agonist 3.6 Inactive 10.1016/J.STR.2011.06.014 2011-09-07
8GCP 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 PGE2 pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.1 Active 10.1073/PNAS.2216329120 2024-01-03
8YWF 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 retatrutide pubchem gtoplig
Agonist 2.7 Active 2025-04-16
8RLN 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 CHEMBL122622 chembl_ligand pubchem
Agonist (partial) 2.4 Inactive 2024-06-19
9W45 Q7TRW7 OR1D2 Olfactory family 1 O2 (Olfactory/extra-nasal 2) Mouse N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Methyl cinnamate pubchem
Agonist 3.2 Active 2026-03-04
8WWM MCHR1 MCH1 Melanin-concentrating 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 melanin-concentratin... pubchem gtoplig uniprot uniprot uniprot
Agonist 2.8 Active 10.1038/S41421-024-00754-0 2024-11-13
7VVL 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 PTH pubchem
Agonist 2.8 Active 10.1016/J.MOLCEL.2022.07.003 2022-08-03
5DGY OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Human Transient_transfectionHEK293SMammalian 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monopalmitolein (9.7 MAG) 5 chems 5.0-5.0 20°C Apo (no ligand)
7.7 Active 10.1038/SDATA.2016.21 2016-03-23
8YY8 FZD7 FZD7 WNT 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)
3.2 Active 10.1038/S41422-021-00525-6 2024-04-24
9UYM CML2 chemerin 2 Chemerin receptor 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 Chemerin
Agonist 3.5 Active 10.1126/SCIENCE.ADT8794 2025-11-19
7F9Y 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
OCTANOIC ACID chembl_ligand pubchem pubchem drugbank drug_central
AgonistAgonist 2.9 Active 10.1038/S41467-021-25364-2 2021-08-18
9X22 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 [<sup>125</sup>I]GLP... pubchem gtoplig pubchem
Agonist 2.9 Active 10.1016/J.APSB.2026.01.023 2026-03-25
8WWI MCHR1 MCH1 Melanin-concentrating 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 Apo (no ligand)
3.4 Active 2024-11-13
7S8L MRGX2 MRGPRX2 Orphan 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 chembl_ligand pubchem
Agonist 2.5 Active 10.1038/S41586-021-04126-6 2021-11-17
7W0O 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 Elabela/Toddler-32 (... pubchem gtoplig uniprot
Agonist 3.8 Active 10.1038/S41594-022-00797-5 2022-07-27
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
Agonist 3.2 Active 10.1126/SCIADV.ABF5325 2021-06-09
8XWM 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 CXCL6
Agonist 3.7 Active 10.1016/J.MOLCEL.2025.01.024 2025-01-15
5IU8 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°C CHEMBL3934661 chembl_ligand pubchem
Antagonist 2.0 Inactive 10.1021/acs.jmedchem.6b00653 2016-06-29
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 NTS8–13 pubchem
Agonist 4.2 Active 10.1038/S41594-020-00554-6 2021-01-06
8JII HCAR2 HCA2 Hydroxycarboxylic 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 nicotinic acid pubchem gtoplig chembl_ligand drugbank drug_central drugbank drugbank
compound 9n [PMID: 1... pubchem gtoplig chembl_ligand
AgonistAgo-PAM 3.2 Active 10.1016/J.MOLCEL.2023.07.030 2023-09-06
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 4-{[(2S)-3-(tert-but... pubchem drugbank
Agonist (partial) 2.1 Inactive 10.1371/JOURNAL.PONE.0092727 2014-04-02
9VO1 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 SAR247799 pubchem gtoplig chembl_ligand
Agonist 3.0 Active 2026-01-28
8JER HCAR2 HCA2 Hydroxycarboxylic 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 Acipimox pubchem
Agonist 3.5 Active 10.1038/S41467-024-46239-2 2024-03-06
7IO2 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 FU7-15 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.0 Inactive 2026-05-20
9VJT OPRM μ 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 (-)-methadone pubchem gtoplig chembl_ligand drugbank drug_central pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.0 Active 2026-06-24
9VB4 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
Agonist 2.9 Active 10.1038/S41586-026-10228-W 2026-06-03
8J6J HCAR2 HCA2 Hydroxycarboxylic 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 GSK256073 pubchem gtoplig
Agonist 2.8 Active 10.1016/J.CELREP.2023.113406 2024-01-10
8GGV 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 c-Epi pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
9LY3 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... pubchem
Agonist 3.4 Active 2026-03-04
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
9JFU GPR4 GPR4 Proton 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 NE 52-QQ57 pubchem gtoplig chembl_ligand
Antagonist 3.2 Active 2025-04-23
9DQH MRGRD MRGPRD Orphan 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 EP-2825 pubchem
Agonist 2.9 Active 2024-12-11
9IY8 GPR55 GPR55 GPR18, GPR55 and GPR119 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)
3.0 Active 10.1038/S41422-024-01046-8 2025-01-01
7Y14 MRGRD MRGPRD Orphan 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 β-alanine pubchem gtoplig chembl_ligand drugbank
Agonist 3.2 Intermediate 10.1038/S42003-022-03668-3 2022-07-20
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
8U02 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 dopamine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.3 Active 10.1038/S41467-024-50964-Z 2024-08-21
9KDG 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 Apo (no ligand)
3.3 Inactive 10.1038/S41467-025-57960-X 2025-05-07
9JH3 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 CMF-019 pubchem gtoplig chembl_ligand
Agonist (partial) 2.9 Active 2025-04-23
8XVU 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 CXCL2
Agonist 3.1 Active 10.1016/J.MOLCEL.2025.01.024 2025-01-15
7VUI GP139 GPR139 Orphan 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
7VV0 MRGX2 MRGPRX2 Orphan 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 CHEMBL5665416 chembl_ligand pubchem pubchem
Agonist 3.5 Active 10.1038/S41586-021-04077-Y 2021-12-01
6Z10 SUCR1 succinate Succinate 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 CHEMBL4751488 chembl_ligand pubchem
Antagonist 2.3 Active 10.1021/acs.jmedchem.0c01020 2020-09-16
9IV6 GPR4 GPR4 Proton 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)
2.7 Active 2025-07-30
8GGQ 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 c-Epi pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
9W0L 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 SPM-242 pubchem
CHEMBL5779183 chembl_ligand pubchem
AntagonistAllosteric antagonist 3.6 Inactive 2026-06-03
5OLH 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 vipadenant pubchem gtoplig chembl_ligand drugbank
Antagonist 2.6 Inactive 10.1038/S41598-017-18570-W 2018-01-17
8GGA 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 c-Epi pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
7Y89 GPR17 GPR17 Orphan 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)
3.0 Active 10.1002/MCO2.159 2022-10-12
7SIM 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
AgonistAgonist 2.7 Active 10.1073/PNAS.2115849118 2022-01-19
7WU9 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 Apo (no ligand)
3.4 Active 10.1016/J.CELREP.2022.111323 2022-08-17
8Z66 GPR4 GPR4 Proton 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)
3.1 Active 2025-04-23
8XOJ GPER1 GPER Estrogen (G protein-coupled) 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)
3.1 Active 10.1038/S41422-024-00963-Y 2024-04-10
9RKF 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 CHEMBL4633760 chembl_ligand pubchem
Inverse agonist 2.5 Inactive 2026-04-22
8Z68 GPR68 GPR68 Proton 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)
2.6 Active 2025-04-23
7YDM AGRE5 ADGRE5 ADGRE 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 N/A N/A 2.9 Active 10.1016/J.CHEMBIOL.2023.08.003 2023-07-12
8YIC 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 SAR247799 pubchem gtoplig chembl_ligand
Agonist 3.5 Active 2024-12-11
25SU TA2R4 TAS2R4 Taste 2 T2 (Taste 2) 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)
3.3 Active 2026-07-15
9EBN 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 Apo (no ligand)
3.4 Active 10.1073/PNAS.2407574122 2025-03-26
8GG1 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 c-Epi pubchem
Agonist 3.0 Active 10.1038/S41586-024-07153-1 2024-03-06
6OFJ OPSD Rhodopsin Opsin (sight) 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)
4.5 Inactive 10.1074/JBC.RA119.010089 2019-08-21
8XQT T2R14 TAS2R14 Taste 2 T2 (Taste 2) 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 drugbank
Agonist 2.9 Active 10.1038/S41586-024-07569-9 2024-07-10
9KUT C3AR C3a Complement peptide 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 JR14a pubchem gtoplig chembl_ligand
Agonist 3.3 Active 2025-11-26
8XWN 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 CXCL8
Agonist 3.3 Active 10.1016/J.MOLCEL.2025.01.024 2025-01-15
9M1O NPFF2 NPFF2 Neuropeptide FF/neuropeptide AF 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 neuropeptide FF (Hum... pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 2.5 Active 10.1016/J.CELREP.2025.116160 2025-07-23
8HJ1 GPR21 GPR21 Orphan 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)
3.3 Active 10.1038/S41467-023-35882-W 2023-12-27
7TMW RXFP1 RXFP1 Relaxin family peptide 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)
3.2 Active 2023-02-15
6VCB 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 glucagon-like peptid... pubchem gtoplig uniprot uniprot uniprot chembl_ligand pubchem
CHEMBL5197819 chembl_ligand pubchem
AgonistPAM 3.3 Active 10.1038/S41589-020-0589-7 2020-07-22
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 pubchem gtoplig chembl_ligand drugbank
Agonist 3.2 Active 10.1016/J.STR.2021.04.008 2021-01-20
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
7S3I 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 Apo (no ligand)
2.5 Active 10.1038/S41589-021-00945-W 2022-01-05
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 gtoplig chembl_ligand chembl_ligand
Antagonist 3.0 Inactive 10.1038/S41586-018-0046-X 2018-04-25
8JXX HRH4 H4 Histamine 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 clobenpropit pubchem gtoplig chembl_ligand
Agonist (partial) 3.1 Active 10.1038/S41467-024-46840-5 2024-03-20
9EPQ B1B1U5 Rhodopsin Opsin (sight) 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 11,20-Ethanoretinal pubchem
Agonist 4.2 Active 2024-10-23
8H2G HCAR2 HCA2 Hydroxycarboxylic 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 nicotinic acid pubchem gtoplig chembl_ligand drugbank drug_central drugbank drugbank
Agonist 3.0 Active 2023-10-11
2I37 OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine NANativeBovine 2 chemicals 2 steps vapour diffusionsitting drops 5 chems 7.0-8.0 5°C Apo (no ligand)
4.2 Inactive 10.1073/PNAS.0608022103 2006-10-17
6LRY 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 sarafotoxin S6b pubchem gtoplig chembl_ligand uniprot chembl_ligand pubchem
Agonist 3.0 Inactive 10.1016/J.BBRC.2019.12.091 2020-02-12
8JPF 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 SBI-553 pubchem gtoplig chembl_ligand
NTS8–13 pubchem
Ago-PAMAgonist 3.0 Active 10.1038/S41586-023-06395-9 2023-08-09
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
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 orforglipron pubchem gtoplig chembl_ligand drugbank
Agonist (partial) 3.1 Active 10.1073/PNAS.2014879117 2020-11-18
9WSX OPRM μ Opioid 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 endomorphin-1 (Human... pubchem gtoplig chembl_ligand
Agonist 2.8 Active 10.1038/S41422-025-01191-8 2025-11-26
8GG9 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 c-Epi pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
8K5C HCAR2 HCA2 Hydroxycarboxylic 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 Acipimox pubchem
Agonist 3.1 Active 10.1038/S41467-023-42764-8 2023-11-22
7IN1 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 Apo (no ligand)
2.5 Inactive 10.1038/S42004-026-02059-7 2026-05-20
6FK6 OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine BaculovirusHEK293S(TetR)-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 4.5-4.5 20°C S-RS1 pubchem
Agonist 2.4 Active 10.1073/PNAS.1718084115 2018-04-04
7XXH P2RY1 P2Y1 P2Y 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 2MeSADP pubchem gtoplig chembl_ligand
Agonist 2.9 Active 2023-06-07
8GNG 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 istradefylline pubchem gtoplig chembl_ligand drug_central drugbank
Antagonist 3.2 Inactive 10.1124/MOLPHARM.122.000633 2023-03-22
8HNK CXCR3 CXCR3 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 [<sup>125</sup>I]CXC... gtoplig
Agonist 3.0 Active 10.1038/S41594-023-01175-5 2023-11-29
9MQJ OPRM μ 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 #020_E1 pubchem
Antagonist 3.2 Inactive 2025-02-12
7XP6 T2R46 TAS2R46 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A strychnine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.0 Active 10.1126/SCIENCE.ABO1633 2022-10-12
7WKD TRFR TRH1 Thyrotropin-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 TRH (Human) pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank pubchem
Agonist 3.0 Active 10.1038/S41422-022-00641-X 2022-06-15
9M2O Q5QNQ1 taar13d Unclassified A (Rhodopsin) Zebrafish N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Putrescine pubchem drugbank
Agonist 2.6 Active 2026-03-04
7S0G 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 LEVISOPRENALINE chembl_ligand pubchem drug_central
Agonist 3.9 Active 10.1038/S41594-021-00679-2 2021-11-17
4BWB NTR1 NTS1 Neurotensin A (Rhodopsin) Rat NAE. coli BL21(DE3)Bacteria 3 chemicals 3 steps vapour diffusionsitting drops 7 chems 5.5-5.5 4°C Neurotensin
Agonist 3.6 Inactive 10.1073/PNAS.1317903111 2014-01-29
2PED OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drop 5 chems 6.4-6.4 283 K all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Inverse agonist 3.0 Inactive 10.1529/BIOPHYSJ.107.108225 2007-10-30
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
Inverse agonist 3.2 Inactive 10.1107/S2052252519013137 2019-11-13
8XOF GPER1 GPER Estrogen (G protein-coupled) 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 Lys05 pubchem
Agonist 2.6 Active 2024-04-10
6QNO OPSD Rhodopsin Opsin (sight) 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 all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 4.4 Active 10.7554/ELIFE.46041 2019-07-10
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 10.1038/S41467-020-19109-W 2020-10-07
6X18 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(7-36)NH2 pubchem
Agonist 2.1 Active 10.1016/J.MOLCEL.2020.09.020 2020-09-09
9E9S PD2R DP1 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 PGD2 pubchem gtoplig chembl_ligand drugbank
Agonist 2.7 Active 10.1038/S41467-025-64002-Z 2025-09-03
6D35 SMOS smo.S Unclassified 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 drugbank
Agonist 3.9 Active 10.1016/J.CELL.2018.04.029 2018-05-23
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 TIOTROPIUM chembl_ligand pubchem drugbank pubchem pubchem
Inverse agonist 2.7 Inactive 10.1038/NATURE17188 2016-03-09
7IOH 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 FU99-91 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.1 Inactive 2026-05-20
9VUS OXGR1 oxoglutarate Oxoglutarate 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 &alpha;-ketoglutaric... pubchem gtoplig chembl_ligand drugbank
Agonist 2.4 Active 2026-07-15
8GEI 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 c-Epi pubchem
Agonist 4.1 Active 10.1038/S41586-024-07153-1 2024-03-06
7SRQ 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 (+)-LSD pubchem gtoplig pubchem gtoplig chembl_ligand drugbank drug_central
Agonist (partial) 2.7 Active 10.1016/J.NEURON.2022.08.006 2022-09-21
7LCJ 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 pubchem gtoplig chembl_ligand drugbank
Agonist 2.8 Active 10.1016/J.STR.2021.04.008 2021-01-20
9JID HCAR3 HCA3 Hydroxycarboxylic 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 nicotinic acid pubchem gtoplig chembl_ligand drugbank drug_central drugbank drugbank
Agonist 2.8 Active 10.1016/J.CELREP.2024.114895 2025-12-17
8IQ6 PF2R FP 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 latanoprost (free ac... pubchem gtoplig chembl_ligand
Agonist 3.4 Active 10.1038/S41467-023-43922-8 2024-01-31
4EIY 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
Na+ pubchem
AntagonistNAM 1.8 Inactive 10.1126/SCIENCE.1219218 2012-07-25
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
8ZFZ GPR4 GPR4 Proton A (Rhodopsin) Zebrafish 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)
3.3 Active 10.1038/S41467-025-55901-2 2025-01-22
9JFX GPR4 GPR4 Proton 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)
2.9 Active 10.1038/S41422-025-01092-W 2025-04-23
9AST XCR1 XCR1 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 XCL1 CC3
Agonist 3.1 Active 10.1073/PNAS.2405732121 2024-12-11
9EE5 PD2R DP1 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 ONO2550289 pubchem
Inverse agonist 2.9 Intermediate 2025-09-03
8WDT 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 trans-photoNECA (blu...
Agonist 3.3 Active 10.1016/J.BBRC.2023.149393 2024-01-17
8F7S 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 deltorphin II pubchem gtoplig chembl_ligand pubchem
Agonist 3.0 Active 10.1016/J.CELL.2022.12.026 2022-12-14
8WRB GPR34 GPR34 Orphan 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 LYSOPHOSPHATIDIC ACI... chembl_ligand pubchem
L-serine pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank pubchem drugbank
AgonistAgonist 2.9 Active 10.1371/JOURNAL.PBIO.3002387 2023-11-08
7IP7 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
FU293-87 pubchem
AntagonistUnknown 2.3 Inactive 2026-05-20
9N09 ACM4 M4 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 CHEMBL6164470 chembl_ligand pubchem
Agonist 2.6 Active 2026-01-28
7B6W ADA1B α1B 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 (+)-cyclazosin pubchem gtoplig chembl_ligand
Inverse agonist 2.9 Inactive 10.1038/s41467-021-27911-3 2022-01-12
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 CHEMBL15060 chembl_ligand pubchem
Agonist 3.2 Inactive 10.1038/S41586-019-1144-0 2019-04-24
7F61 HRH3 H3 Histamine 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-03654746 pubchem gtoplig chembl_ligand drugbank
Antagonist 2.6 Inactive 10.1038/S41467-022-33880-Y 2022-10-26
7IPA 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 FU336-32 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.3 Inactive 2026-05-20
9D0A PAR2 PAR2 Proteinase-activated 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 3.1 Active 10.1038/S41467-025-59138-X 2025-05-07
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 gtoplig chembl_ligand pubchem
Antagonist 3.3 Inactive 10.1016/J.STR.2018.10.027 2019-01-02
7S15 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 CHEMBL5191519 chembl_ligand pubchem
Agonist 3.8 Active 10.1021/acs.jmedchem.1c01856 2022-06-08
9KT7 HCAR2 HCA2 Hydroxycarboxylic 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 MK 6892 pubchem gtoplig chembl_ligand pubchem
Agonist 2.8 Active 10.1021/ACS.JMEDCHEM.4C02567 2025-12-10
9M2F NPFF1 NPFF1 Neuropeptide FF/neuropeptide AF 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 neuropeptide FF
Agonist 2.9 Active 10.1016/J.CELREP.2025.116160 2025-07-23
8YUU HRH3 H3 Histamine 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 histamine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 2.7 Active 10.1002/ADVS.202310120 2024-06-05
9ASA 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 RS130-180 pubchem
Agonist 3.1 Active 2025-04-02
8YUT HRH2 H2 Histamine 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 amthamine pubchem gtoplig chembl_ligand
Agonist 2.7 Active 2024-06-05
9JMD MTLR motilin Motilin 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 azithromycin pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.7 Active 10.1016/J.CELREP.2025.115329 2025-05-28
6LW5 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 WKYMVM pubchem
Agonist 2.8 Active 10.1038/S41467-020-15009-1 2020-03-25
9C0K 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-phe1
Agonist 2.7 Active 2025-06-11
8KFY CCR8 CCR8 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 ZK 756326 pubchem gtoplig chembl_ligand
Agonist 3.1 Active 10.1126/SCIADV.ADJ7500 2024-02-07
7INQ 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 4-[(trifluoromethyl)... pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.2 Inactive 10.1038/S42004-026-02059-7 2026-05-20
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
8Z74 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 JN241-9
Agonist 3.0 Inactive 10.1038/S41467-024-55555-6 2025-01-22
9P92 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 Vasoactive intestina... pubchem
Agonist 3.8 Active 10.1073/PNAS.2521157122 2025-11-19
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
Inverse agonist 2.6 Inactive 10.1038/S41589-018-0152-Y 2018-11-21
8TLM CCR8 CCR8 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 mAb1 Fab fragment (c...
mAb1 Fab fragment (c...
AntagonistAntagonist 2.9 Inactive 10.1038/S41467-023-43601-8 2023-12-20
4LDE 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 CHEMBL1615159 chembl_ligand pubchem
Agonist 2.8 Active 10.1038/NATURE12572 2013-09-25
20ZL 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
Agonist 3.1 Active 10.1038/S41586-026-10228-W 2026-06-03
7XAV 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 LANREOTIDE chembl_ligand pubchem drugbank
Agonist 2.9 Active 10.1038/S41421-022-00405-2 2022-08-31
8FEG OPRK κ 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 DNCP-beta-NalA(1)
Agonist 2.5 Active 10.1038/s41467-023-43718-w 2023-12-06
9VO0 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 Ponesimod pubchem drugbank
Agonist 2.8 Active 2026-01-28
9MZG 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 Glucagon pubchem
Agonist 3.0 Active 2026-04-22
9AVG 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
tecalcet pubchem gtoplig chembl_ligand
AgonistAgonistPAM 3.6 Active 2024-04-17
8JCY 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
Antagonist 2.9 Inactive 10.1038/S41422-023-00830-2 2023-06-21
8GFZ 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 c-Epi pubchem
Agonist 3.0 Active 10.1038/S41586-024-07153-1 2024-03-06
9UWQ 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 cagrilintide pubchem gtoplig drugbank
Agonist 3.1 Active 10.1038/S41401-025-01635-2 2026-05-27
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
7WCM GP119 GPR119 GPR18, GPR55 and GPR119 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 MBX-2982 pubchem gtoplig chembl_ligand drugbank
Agonist 2.3 Active 10.1038/S41467-022-34696-6 2022-12-21
7UM4 5HT5A 5-HT5A 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 CHEMBL3654198 chembl_ligand pubchem
Antagonist 2.8 Inactive 10.1038/S41594-022-00796-6 2022-07-20
9L79 GP119 GPR119 GPR18, GPR55 and GPR119 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 AR231453 pubchem gtoplig chembl_ligand
Agonist 3.0 Active 2025-12-31
7YU8 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 ONO-0740556 pubchem
Agonist 4.5 Active 10.1038/S41467-022-33121-2 2022-10-05
9M1S OXGR1 oxoglutarate Oxoglutarate 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 Itaconic acid pubchem
Agonist 2.7 Active 10.1038/S44318-026-00823-Y 2026-06-17
7IO0 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 FU4-54
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.1 Inactive 2026-05-20
7MT9 OPSD Rhodopsin Opsin (sight) 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 all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 7.0 Active 10.1038/S41586-021-03721-X 2021-07-07
8WCA TAAR1 TA1 Trace amine 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 &beta;-phenylethylam... pubchem gtoplig chembl_ligand drugbank pubchem
Agonist 3.5 Active 10.1016/J.CELL.2023.10.014 2023-12-27
9IVG 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 glucagon-like peptid... pubchem
Agonist (partial) 3.0 Active 10.1016/J.APSB.2024.09.002 2024-11-27
8HAO 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 teriparatide pubchem pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem
Agonist 3.8 Active 10.1038/S41401-022-01032-Z 2022-12-21
6MET 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 T-cell surface glyco...
Envelope glycoprotei...
UnknownAntagonist 4.5 Inactive 10.1038/S41586-018-0804-9 2018-12-12
8TYW GPR6 GPR6 Orphan 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)
3.4 Active 10.1126/SCISIGNAL.ADO8741 2024-12-04
8XXV 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 Phosphatidylinositol...
indomethacin pubchem gtoplig chembl_ligand drugbank drug_central
PAMAgonist 2.3 Active 2024-12-04
8XQL T2R14 TAS2R14 Taste 2 T2 (Taste 2) 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 drugbank
aristolochic acid pubchem gtoplig chembl_ligand
AgonistAllosteric agonist 3.0 Active 10.1038/S41586-024-07569-9 2024-07-10
9UVX 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 OPC-51803 pubchem gtoplig chembl_ligand drugbank
Agonist (partial) 3.3 Inactive 2026-05-06
4GBR ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 4 chems 6.5-6.5 20°C (S)-carazolol pubchem drugbank
Inverse agonist 4.0 Inactive 10.1371/JOURNAL.PONE.0046039 2012-10-24
7MBX 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 (Human) pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank pubchem
Agonist 2.0 Active 10.1371/JOURNAL.PBIO.3001295 2021-05-26
9IXJ HRH2 H2 Histamine 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 histamine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 2.9 Active 2025-07-30
7VBH 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 Peptide 20
Agonist 3.0 Active 10.1038/S41467-022-28683-0 2022-04-06
9PPQ OPRM μ 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 0505 pubchem
Agonist 3.3 Active 2026-03-04
7P2L 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 alloswitch-1 pubchem gtoplig
NAM 2.5 Inactive 10.1016/J.CELREP.2021.109648 2021-09-08
6W2X 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
Inverse agonist 3.6 Inactive 10.1038/S41586-020-2469-4 2020-07-01
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 fMLFII
Agonist 3.2 Active 10.1038/S41467-022-28586-0 2022-03-30
9N2I 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 SRB103Q
Agonist 3.0 Active 2026-04-22
5K2A 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
8K9K OPRM μ 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 DAMGO pubchem gtoplig chembl_ligand pubchem
Agonist 3.0 Active 10.1038/S41467-024-47792-6 2024-05-29
9VAT 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
Agonist 3.4 Active 10.1038/S41586-026-10228-W 2026-06-03
9ODN OPRM μ Opioid 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 DAMGO pubchem gtoplig chembl_ligand pubchem
Agonist 2.4 Active 2026-03-04
7EPC GRM7 mGlu7 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)
4.0 Inactive 10.1038/S41586-021-03641-W 2021-06-23
8SZG 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 D-tryptophan pubchem gtoplig chembl_ligand drugbank pubchem gtoplig chembl_ligand drugbank drug_central
Calcium pubchem
cinacalcet pubchem gtoplig chembl_ligand drugbank drug_central
spermine pubchem gtoplig chembl_ligand drugbank
AgonistAgonistPAMAgo-PAM 3.6 Active 10.1038/S41586-024-07055-2 2024-02-07
8IEI GP156 GPR156 Orphan 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 PC 34:1 pubchem
Agonist 2.6 Active 2024-02-14
9KB6 LGR4 LGR4 Orphan 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)
3.5 Inactive 10.1038/S41467-025-64129-Z 2025-10-15
9LLI 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 flupentixol pubchem gtoplig chembl_ligand drugbank
GEM targeting TM5/6/...
GEM targeting TM3/4/...
GEM targeting TM1/2/...
AntagonistNAMUnknownUnknown 3.0 Inactive 2026-03-04
7NA7 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-27
Agonist 2.7 Active 10.1038/S41467-021-26735-5 2021-12-15
8JLK TAAR1 TA1 Trace amine 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 ulotaront pubchem gtoplig chembl_ligand drugbank
Agonist 3.2 Active 10.1038/S41586-023-06804-Z 2023-11-15
8KH4 GP161 GPR161 Orphan 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)
3.1 Active 10.1038/S41467-023-41654-3 2023-10-11
8EFB OPRM μ 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 OLICERIDINE chembl_ligand pubchem drugbank drug_central
Agonist (partial) 3.2 Active 10.1016/J.CELL.2022.09.041 2022-11-09
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
Inverse agonist 1.8 Inactive 10.1038/S41598-020-76277-X 2020-11-25
3AYN OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Japanese flying squid NANativeSquid 1 chemicals 1 steps vapour diffusionsitting drop 5 chems 6.0-6.0 4°C all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Inverse agonist 2.7 Inactive 10.1016/J.JMB.2011.08.044 2011-08-17
9LXP 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... pubchem
Agonist 3.2 Active 2026-03-04
9L9O MTR1L GPR50 Orphan 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)
3.0 Inactive 10.1016/J.MOCELL.2026.100331 2026-02-18
8PKM 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 Befiradol pubchem chembl_ligand
Phosphatidylinositol...
AgonistPAM 2.9 Active 2024-05-29
6UP7 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 NTS8–13 pubchem
PIO pubchem
AgonistPAM 4.2 Active 10.1038/S41586-020-1953-1 2020-02-26
8W77 O52E4 OR52E4 Olfactory family 52 O1 (Olfactory/extra-nasal 1) 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)
3.6 Inactive 10.1038/S41467-023-43983-9 2023-12-20
8JRU 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 Apo (no ligand)
3.5 Active 10.1038/S41586-023-06420-X 2023-08-16
7SF7 AGRL3 ADGRL3 ADGRL 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 N/A N/A 2.9 Active 10.1038/S41586-022-04575-7 2022-04-27
8GTI CRHR1 CRF1 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 BMK-C205 pubchem
Antagonist 2.2 Inactive 10.1038/S12276-023-01082-1 2023-09-13
8EFQ OPRM μ 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 DAMGO pubchem gtoplig chembl_ligand pubchem
MONOETHANOLAMINE chembl_ligand pubchem drugbank
AgonistAgonist 3.3 Active 10.1016/J.CELL.2022.09.041 2022-11-09
8X0C 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
VU0424465 pubchem gtoplig chembl_ligand
AgonistAgo-PAM 3.2 Active 10.1038/S41467-024-55439-9 2024-11-06
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 Active 10.1038/s41594-018-0116-7 2018-08-29
7RMH 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 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 3.1 Active 10.1038/S41589-021-00890-8 2021-11-03
9VNZ 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 HY-X-1011 pubchem
Agonist 2.8 Active 2026-01-28
21AH 5HT1F 5-HT1F 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 LY334370 pubchem gtoplig chembl_ligand
Agonist 3.2 Active 2026-04-08
9MBB GRM8 mGlu8 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
Antagonist 3.3 Inactive 10.1016/J.MOLCEL.2025.08.019 2025-10-01
7EJA 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 dexmedetomidine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.6 Active 10.1126/SCIADV.ABJ5347 2022-04-13
8XJO 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 U46619 pubchem gtoplig chembl_ligand
Agonist 3.1 Active 10.1016/J.CELREP.2024.113893 2024-02-28
4QIN SMO SMO Oxysterol F (Frizzled) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 6 chems 7.2-7.2 20°C SAG1.5
Agonist 2.6 Inactive 10.1038/NCOMMS5355 2014-07-23
9JCQ GPR4 GPR4 Proton 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 Lysophosphatidylchol... pubchem
PAM 2.6 Active 2025-07-09
7YU4 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 ONO-0740556 pubchem
Agonist 3.3 Active 10.1038/S41467-022-33121-2 2022-10-05
8IHH HCAR2 HCA2 Hydroxycarboxylic 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 5-butyl-1H-pyrazole-... pubchem gtoplig chembl_ligand
Agonist (partial) 3.1 Active 10.1038/S41467-023-41650-7 2023-08-30
8A6D OPSD Rhodopsin Opsin (sight) 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 all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Agonist 1.8 Inactive 10.1038/S41586-023-05863-6 2023-03-29
8ZMD PAR2 PAR2 Proteinase-activated 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 3.3 Active 10.1038/S41421-025-00851-8 2025-05-28
6ME8 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 CHEMBL15060 chembl_ligand pubchem
Agonist 3.1 Inactive 10.1038/S41586-019-1144-0 2019-04-24
9DGI CNR1 CB1 Cannabinoid 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 methyl (2R)-2-({(1M)... pubchem
Agonist 3.4 Active 10.1038/S41467-025-57136-7 2025-04-30
7UM7 5HT5A 5-HT5A 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 2.8 Active 10.1038/S41594-022-00796-6 2022-07-20
9LLH 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 dopamine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist-positive all...
AgonistAgo-PAM 2.7 Active 2026-03-04
7U2L OPRM μ Opioid 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 C5 guano pubchem
Agonist 3.2 Active 10.1038/S41586-022-05588-Y 2022-05-04
8ZYY 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 NTS8–13 pubchem
SBI-553 pubchem gtoplig chembl_ligand
AgonistAllosteric agonist 2.8 Active 2025-04-09
8I97 C3AR C3a Complement peptide 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)
3.2 Active 10.1016/J.CELL.2023.09.020 2023-10-18
7TUZ GP183 GPR183 Orphan 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 7&alpha;,25-dihydrox... pubchem gtoplig chembl_ligand
Agonist 3.1 Active 10.1016/J.STR.2022.04.006 2022-04-13
8FLS 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 abaloparatide drug_central pubchem
Agonist 3.1 Active 10.1016/J.STR.2023.04.002 2023-04-26
26XH OXGR1 oxoglutarate Oxoglutarate 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 maleic acid pubchem gtoplig chembl_ligand drugbank
Agonist 2.8 Active 10.1038/S44318-026-00823-Y 2026-06-17
4YAY AGTR1 AT1 Angiotensin A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 6 chems 5.0-6.0 20°C ZD-7155 pubchem gtoplig chembl_ligand
Antagonist 2.9 Inactive 10.1016/J.CELL.2015.04.011 2015-04-22
8XFS LGR4 LGR4 Orphan 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-spondin-2
E3 ubiquitin-protein...
AgonistUnknown 3.2 Inactive 2024-12-04
9RKI 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 CHEMBL4633760 chembl_ligand pubchem
Antagonist 2.6 Inactive 2026-04-22
8U26 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 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 2.5 Active 10.1038/S41592-023-02082-9 2023-11-15
7VUH GP139 GPR139 Orphan 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
7BTS 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 (-)-adrenaline pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.1 Active 10.1038/S41422-020-00424-2 2020-12-02
8JJP CML2 chemerin 2 Chemerin receptor 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 chemerin C-terminal ... pubchem gtoplig chembl_ligand pubchem
Agonist 2.9 Active 2024-08-21
9EHS AA3R A3 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 CHEMBL4439336 chembl_ligand pubchem
Antagonist 3.2 Inactive 2025-08-20
8X0F 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
VU-29 pubchem gtoplig chembl_ligand
AgonistPAM 3.3 Active 10.1038/S41467-024-55439-9 2024-11-06
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
9MBA GRM8 mGlu8 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 chembl_ligand pubchem pubchem drugbank
Agonist 3.1 Inactive 10.1016/J.MOLCEL.2025.08.019 2025-10-01
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 Active 10.1126/SCIENCE.1244142 2013-12-18
9MQK OPRK κ 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 #020_E1 pubchem
Inverse agonist 3.2 Inactive 2025-02-12
6Z4V 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 NTS8–13 pubchem
Agonist 2.6 Intermediate 10.1126/sciadv.abe5504 2021-02-10
7W7E 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 CHEMBL5517987 chembl_ligand pubchem
Agonist 3.4 Active 10.1126/SCIENCE.ABN7065 2022-09-28
8FYN 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/S41467-023-36733-4 2023-03-08
8GGN 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 c-Epi pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06
7W57 NMUR2 NMU2 Neuromedin U 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 Neuromedin-S
Agonist 3.2 Active 10.1038/S41467-022-29683-W 2022-04-20
9WG4 O52E8 OR52E8 Olfactory family 52 O1 (Olfactory/extra-nasal 1) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (3R)-3-Hydroxy-3-met... pubchem
Agonist 3.3 Active 2026-06-17
7INM 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 theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
5-(trifluoromethyl)p... pubchem
AntagonistUnknown 2.2 Inactive 10.1038/S42004-026-02059-7 2026-05-20
8W1A VGPCR ORF74 Unclassified A (Rhodopsin) isolate GK18 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)
2.9 Inactive 10.1038/S41467-025-63457-4 2025-08-27
6OMM 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 WKYMVM pubchem
Agonist 3.2 Active 10.1038/S41467-020-14728-9 2020-02-26
7IOR 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 FU163-53 pubchem
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 1.9 Inactive 2026-05-20
6VJM 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 Apo (no ligand)
4.0 Inactive 10.1038/S41586-020-2408-4 2020-06-10
8PM2 TAA7F TAAR7F Orphan 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 N,N-dimethylcyclohex... pubchem
Agonist 2.9 Active 10.1101/2023.07.07.547762 2023-08-09
9EAH 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 OLMESARTAN chembl_ligand pubchem drugbank
Antagonist 3.1 Inactive 10.1073/PNAS.2423931122 2025-03-05
9YDV P2Y14 P2Y14 P2Y 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 CHEMBL1198696 chembl_ligand pubchem
Agonist 3.1 Active 2025-11-19
9M0R NPFF1 NPFF1 Neuropeptide FF/neuropeptide AF 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 Neuropeptide VF pubchem
Agonist 2.5 Active 10.1016/J.CELREP.2025.116160 2025-07-23
6LI3 GPR52 GPR52 Orphan 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)
3.3 Active 10.1038/S41586-020-2019-0 2020-02-26
7WC9 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 IHCH-7086 pubchem
Agonist 2.5 Inactive 10.1126/SCIENCE.ABL8615 2022-01-26
8ZX4 GPR55 GPR55 GPR18, GPR55 and GPR119 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 L-alpha-lysophosphat...
Agonist 2.9 Active 2024-11-13
8I95 C3AR C3a Complement peptide 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 EP54
Agonist 2.9 Active 10.1016/J.CELL.2023.09.020 2023-10-18
10KT 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 Compound 50 pubchem
Antagonist 2.6 Inactive 2026-05-20
8IWE TAAR9 TAAR9 Orphan 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 SPERMIDINE chembl_ligand pubchem drugbank
Agonist 3.4 Active 10.1038/S41586-023-06106-4 2023-05-31
9ARZ 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 2-bromo-LSD pubchem gtoplig chembl_ligand
Agonist (partial) 3.4 Active 2025-04-02
9KUG C5AR1 C5a1 Complement peptide 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 EP67
Agonist 3.1 Active 10.1073/PNAS.2614459123 2025-11-26
8XYK CXCR3 CXCR3 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 CHEMBL2181467 chembl_ligand pubchem chembl_ligand pubchem
Agonist 3.0 Active 2025-02-26
8JEF HCAR3 HCA3 Hydroxycarboxylic 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 3-hydroxyoctanoic ac... pubchem gtoplig
Agonist 3.0 Active 10.1016/J.CELREP.2024.114895 2024-12-18
8ZCF GPR4 GPR4 Proton 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)
2.9 Active 10.1038/S41422-025-01092-W 2025-04-23
9VO2 OXGR1 oxoglutarate Oxoglutarate 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)
2.7 Active 10.1016/J.CELL.2026.01.036 2026-03-18
9V0X PRLHR PrRP Prolactin-releasing peptide 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 GUB08248
KUT [2-(2-[2-(2-[2-(... pubchem
AgonistAgonist 2.7 Active 10.1038/S41401-025-01741-1 2026-02-04
9L80 GP119 GPR119 GPR18, GPR55 and GPR119 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 ATAZANAVIR chembl_ligand pubchem drugbank
Ago-PAM 3.3 Active 10.1016/J.CELL.2025.12.023 2025-12-31
9W0S T2R46 TAS2R46 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Artemisinin pubchem drugbank
Agonist 3.3 Active 2026-04-22
7INZ 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 FU4-40
theophylline pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank chembl_ligand
UnknownAntagonist 2.4 Inactive 2026-05-20
8HCX 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-1 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 3.5 Active 2023-03-22
8JD2 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 chembl_ligand pubchem pubchem drugbank
Agonist 2.8 Active 10.1038/S41422-023-00830-2 2023-06-21
8YN9 HRH4 H4 Histamine 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 histamine pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 2.3 Active 10.1038/S41467-024-52585-Y 2024-10-09
9PXX OPRM μ 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 naloxone pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem
Agonist (partial) 3.1 Active 2025-11-12
9LY2 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... pubchem
Agonist 3.1 Active 2026-03-04
9OMP GRM7 mGlu7 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)
4.3 Inactive 10.1073/PNAS.2507112122 2025-07-09
8ITF TAAR9 TAAR9 Orphan 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 N,N-dimethylcyclohex... pubchem
Agonist 3.5 Active 10.1038/S41586-023-06106-4 2023-05-31
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 pubchem chembl_ligand drugbank chembl_ligand
Agonist 2.5 Active 10.1016/J.CELREP.2021.109374 2021-08-04
9P81 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 NTS8–13 pubchem
Agonist 2.6 Active 10.1038/S41586-026-10120-7 2026-03-25
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 10.1038/S41467-022-28111-3 2022-03-02
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 Active 10.1038/S41422-021-00474-0 2021-03-10
8HIX GPR21 GPR21 Orphan 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)
3.1 Active 10.1038/S41467-023-35882-W 2023-03-15
8IUM PF2R FP 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 tafluprost acid pubchem gtoplig
Agonist 3.1 Active 10.1038/S41467-023-38411-X 2023-07-12
9VB2 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
Agonist 3.1 Active 10.1038/S41586-026-10228-W 2026-06-03
9LE0 OR6A2 OR6A2 Olfactory family 6 O2 (Olfactory/extra-nasal 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Octanal pubchem
Agonist 2.5 Active 10.1016/J.CELL.2025.12.017 2026-01-28
7SRS 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 (+)-LSD pubchem gtoplig pubchem gtoplig chembl_ligand drugbank drug_central
Agonist (partial) 3.3 Active 10.1016/J.NEURON.2022.08.006 2022-09-21
8XXY CXCR3 CXCR3 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)
3.7 Active 10.1038/S41467-025-58264-W 2025-02-26
3OAX OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 6.0-6.0 283 K all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
beta-ionone pubchem
Inverse agonistAllosteric agonist 2.6 Inactive 10.1016/J.BPJ.2010.08.003 2011-01-19
9UVT 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 N/A N/A 3.3 Inactive 2026-05-06
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 afamelanotide pubchem gtoplig chembl_ligand chembl_ligand pubchem drugbank drug_central
Calcium pubchem
AgonistPAM 2.7 Active 10.1038/S41422-021-00557-Y 2021-09-08
9MEU CXCR4 CXCR4 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 Stromal cell-derived...
Agonist 3.5 Inactive 10.1038/S41467-025-63815-2 2025-09-10
3C9L OPSD Rhodopsin Opsin (sight) A (Rhodopsin) Bovine NANANA 1 chemicals 1 steps NANANA 1 chems 0.0-0.0 NA all-<i>trans</i>-ret... pubchem gtoplig chembl_ligand
Inverse agonist 2.7 Inactive 10.1107/S0907444908017162 2008-08-05
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
7F55 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 bremelanotide pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.1 Active 10.1038/S41422-021-00552-3 2021-11-03
9UCO AGRE1 ADGRE1 ADGRE B2 (Adhesion) Mouse N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Stalk peptide
Agonist 3.6 Active 2026-04-08
8JIL HCAR2 HCA2 Hydroxycarboxylic 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 nicotinic acid pubchem gtoplig chembl_ligand drugbank drug_central drugbank drugbank
Agonist 3.5 Active 10.1016/J.MOLCEL.2023.07.030 2023-09-06
8HPT C5AR1 C5a1 Complement peptide 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 C5apep
Agonist 3.4 Active HTTPS://DOI.ORG/10.1016/J.CELL.2023.09.020 2023-10-18
8WMA FZD4 FZD4 WNT 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 DEP domain of DVL2
Allosteric agonist 3.5 Active 10.1038/S41467-024-52174-Z 2024-09-11
8UH3 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 SETIPTILINE chembl_ligand pubchem drugbank
Agonist 3.3 Active 10.1126/SCIADV.ADK4855 2024-05-01
7X2C 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 fenoldopam pubchem gtoplig chembl_ligand drugbank drug_central pubchem gtoplig chembl_ligand pubchem gtoplig
Agonist 3.2 Active 10.1038/S41467-022-30929-W 2022-06-29
8JZP C5AR1 C5a1 Complement peptide 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 C5a anaphylatoxin
Agonist 3.5 Active 2025-01-15
4EA3 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 compound 24 [PMID: 1... pubchem gtoplig chembl_ligand
Antagonist 3.0 Inactive 10.1038/NATURE11085 2012-04-25
6X19 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 CHU-128 pubchem
Agonist 2.1 Active 10.1016/J.MOLCEL.2020.09.020 2020-09-09
9JFW GPR4 GPR4 Proton 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)
3.1 Active 10.1038/S41422-025-01092-W 2025-04-23
8VVF OPRK κ 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 JDTic pubchem gtoplig chembl_ligand chembl_ligand pubchem chembl_ligand pubchem
Inverse agonist 3.0 Active 10.1038/S41589-024-01812-0 2025-01-15
6N48 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 CHEMBL1615159 chembl_ligand pubchem
compound-6FA pubchem
Nanobody 6B9
AgonistPAMAllosteric agonist 3.2 Active 10.1126/SCIENCE.AAW8981 2019-06-26
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
7WCN GP119 GPR119 GPR18, GPR55 and GPR119 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 AR231453 pubchem gtoplig chembl_ligand
Agonist 2.9 Active 10.1038/S41467-022-34696-6 2022-12-21
8JJL 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 olodaterol pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.2 Inactive 10.1038/S41589-023-01389-0 2023-09-06
7NA8 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 ibutamoren pubchem gtoplig chembl_ligand
Cholesterol pubchem drugbank
AgonistPAM 2.7 Active 10.1038/S41467-021-26735-5 2021-12-15
8WW2 GPR3 GPR3 Orphan 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 oleic acid pubchem gtoplig chembl_ligand drug_central pubchem drugbank
Agonist 2.8 Active 10.1038/S41422-024-00932-5 2024-02-14
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
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
8WM9 FZD4 FZD4 WNT 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 Dishevelled-2 DEP do...
Allosteric agonist 3.5 Active 10.1038/S41467-024-52174-Z 2024-09-11
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 10.1016/J.STR.2015.07.024 2015-10-21
6FJ3 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 ePTH
Agonist (partial) 2.5 Inactive 10.1038/S41594-018-0151-4 2018-11-21
9J0F P2Y14 P2Y14 P2Y 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 NADH pubchem drugbank
Agonist 2.8 Active 10.1038/S41421-025-00799-9 2025-06-04
8TRD GRM3 mGlu3 Metabotropic glutamate C (Glutamate) Rat 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
Antagonist 3.4 Inactive 10.1038/S41467-024-50548-X 2024-07-31
8RVW 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 StilSwitch3 pubchem
Antagonist 2.7 Inactive 2025-01-08
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
9K3L ACTHR MC2 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 Apo (no ligand)
3.0 Active 10.1016/J.STR.2025.03.004 2025-08-06
9KXS C5AR1 C5a1 Complement peptide 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 EP67
Agonist 3.3 Active 10.1073/PNAS.2614459123 2025-11-26
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 Peptide 15 (P15)
Agonist 3.4 Active 10.1074/JBC.RA120.013793 2020-05-27
7X8R 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 CHEMBL2158411 chembl_ligand pubchem
Agonist 2.6 Active 10.1073/PNAS.2200155119 2022-06-29
8GUT CNR2 CB2 Cannabinoid 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 LEI-102 pubchem
Agonist (partial) 3.0 Active 10.1038/S41467-023-37112-9 2023-05-10
8KIG MC3R MC3 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 SHU9119 pubchem
Calcium pubchem
AntagonistAgonist 3.1 Inactive 2025-02-26
8GG6 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 c-Epi pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06
9W2J NK2R NK2 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 Peptide 383 (P383)
Agonist 2.8 Active 2026-06-17
8X0E 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
Agonist 3.4 Active 10.1038/S41467-024-55439-9 2024-11-06
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 (Human) pubchem gtoplig uniprot uniprot uniprot
Agonist 2.0 Inactive 10.1038/S41467-018-07094-0 2018-11-21
8SAI GPR34 GPR34 Orphan 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 LysoPS (18:1) pubchem
Agonist 3.3 Active 10.1073/PNAS.2308435120 2023-10-04
8YKY T2R14 TAS2R14 Taste 2 T2 (Taste 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A compound 28.1 [PMID:... pubchem gtoplig chembl_ligand
Cholesterol pubchem drugbank
Allosteric agonistAgonist 3.0 Active 2024-07-10
7XMT SSR4 SST4 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 J-2156 pubchem gtoplig chembl_ligand
Agonist 2.8 Active 10.1038/S41422-022-00679-X 2022-08-03
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
7VVO 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 PTH pubchem
Agonist 4.1 Active 10.1016/J.MOLCEL.2022.07.003 2022-08-03
9ERX CNR1 CB1 Cannabinoid 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 HU-210 pubchem gtoplig chembl_ligand
Agonist 2.9 Active 2024-06-26
8F2B 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 pramlintide analogue...
N-hexadecanoyl-L-glu... pubchem
AgonistAgonist 2.0 Active 10.1038/S41589-023-01393-4 2023-08-02
9D61 OPRK κ 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 JDTic pubchem gtoplig chembl_ligand chembl_ligand pubchem chembl_ligand pubchem
Inverse agonist 3.6 Active 10.1038/S41589-024-01812-0 2025-01-15
8ZRK GP119 GPR119 GPR18, GPR55 and GPR119 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 GSK-1292263 chembl_ligand pubchem drugbank
Agonist 2.8 Active 2024-06-19
9PQD 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 z7149 pubchem
Agonist 3.3 Active 2025-08-20
9AS5 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 mescaline pubchem gtoplig chembl_ligand
Agonist 3.3 Active 2025-04-02
8HBD 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 sovateltide pubchem gtoplig chembl_ligand pubchem drugbank
Agonist 3.0 Active 2023-03-22
8WKZ 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 SBL-MC-31
Antagonist 3.3 Inactive 10.1021/acs.jmedchem.3c01822 2024-08-07
9E51 AGRL2 ADGRL2 ADGRL 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 Apo (no ligand)
2.9 Active 10.1073/PNAS.2508436122 2025-11-12
7XWO NK2R NK2 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 neurokinin A (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Agonist 2.7 Active 2023-05-31
8WP1 SUCR1 succinate Succinate 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 <i>cis</i>-epoxysucc... pubchem gtoplig chembl_ligand
Agonist 3.2 Active 10.1016/J.CELREP.2024.114381 2024-09-11
8RWX 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 StilSwitch3 pubchem
Na+ pubchem
AntagonistNAM 3.1 Inactive 2025-01-08
9NOY TS1R2 TAS1R2 Taste 1 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)
3.7 Inactive 10.1016/J.CELL.2025.04.021 2025-05-21
7YFD HRH4 H4 Histamine 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 imetit pubchem gtoplig chembl_ligand pubchem
Agonist 3.1 Active 10.1038/S41467-023-42260-Z 2023-10-25
8ZMG 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 pimavanserin pubchem gtoplig chembl_ligand drug_central drugbank
Inverse agonist 3.4 Inactive 2024-08-28
6OS2 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 TRV026 pubchem gtoplig chembl_ligand
Agonist 2.7 Active 10.1126/SCIENCE.AAY9813 2020-02-19
8GG5 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 c-Epi pubchem
Agonist 3.2 Active 10.1038/S41586-024-07153-1 2024-03-06
9UTA TS1R2 TAS1R2 Taste 1 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)
3.8 Inactive 10.1038/S41586-025-09302-6 2025-07-16
7XKF AGRG2 ADGRG2 ADGRG B2 (Adhesion) Mouse N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A PRASTERONE chembl_ligand pubchem drugbank
Agonist 2.4 Active 10.1038/S41589-022-01084-6 2022-08-10
4XT3 US28 US28 Unclassified A (Rhodopsin) strain AD169 BaculovirusHEK293S(TetR)-GnTI-Mammalian 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monovaccenin(11.7 MAG) 6 chems 7.4-7.4 20°C Fractalkine
Agonist 3.8 Active 10.1126/SCIENCE.AAA5026 2015-03-04
7FIH 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 Chorionic gonadotrop...
Chorionic gonadotrop...
Org43553 pubchem
AgonistAgonistAllosteric agonist 3.2 Active 10.1038/S41586-021-03924-2 2021-09-29
9LE2 OR6A2 OR6A2 Olfactory family 6 O2 (Olfactory/extra-nasal 2) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (E)-dec-2-enal pubchem
Agonist 3.3 Active 2026-01-28