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RECEPTOR EXPRESSION SOLUBILIZATION PURIFICATION STRUCTURE DETERMINATION
PDB pH Temp Resolution Reference Date
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 pubchem
Antagonist 2.2 Active 10.1038/NATURE11701 2012-12-12
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 lysophosphatidic aci... pubchem
Agonist 3.0 Active 10.1016/J.JSB.2024.108164 2025-01-01
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 pubchem
Antagonist 3.1 Intermediate 10.1038/s41594-018-0116-7 2018-08-29
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
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
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
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
Agonist 3.4 Active 10.1038/S41467-023-36673-Z 2023-04-19
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 pubchem
Agonist 3.6 Active 10.1126/SCIADV.ABL5442 2022-01-26
8IW9 TAAR9 TAAR9 A orphans 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
Agonist 3.1 Active 10.1038/S41586-023-06106-4 2023-05-31
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 pubchem
Agonist 2.9 Active 10.1038/S41589-020-0492-2 2020-04-15
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
7VBI GLP1R GLP-1 Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A tirzepatide pubchem gtoplig
Agonist 3.0 Active 10.1038/S41467-022-28683-0 2022-03-02
2G87 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 6.5-7.5 283 K Retinal (all-trans) pubchem
Agonist 2.6 Inactive 10.1002/ANIE.200600595 2006-09-02
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 (5S)-5-methyl-4-oxo-... pubchem
Agonist 3.2 Active 10.1038/S41467-023-41650-7 2023-08-30
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
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
7LLY GLP1R GLP-1 Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Pro-glucagon pubchem
Agonist 3.3 Active 10.1038/S41467-021-27760-0 2022-01-12
7EVM GLP1R GLP-1 Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N-Tert-butyl-6,7-dic... pubchem
Ago-PAM 2.5 Active 10.1038/S41467-021-24058-Z 2021-08-11
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
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 pubchem
Agonist 2.7 Active 2022-12-28
3C9M OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANANA 1 chemicals 1 steps NANANA 1 chems 0.0-0.0 NA Retinal (11-cis) pubchem
Inverse agonist 3.4 Inactive 10.1107/S0907444908017162 2008-08-05
8IRJ GP179 GPR179 C Orphans C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.5 Inactive 2024-09-18
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
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
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 pubchem
Antagonist 3.4 Inactive 10.1038/S41467-023-44477-4 2024-01-17
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 drugbank pubchem
Antagonist 3.2 Inactive 2024-08-28
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 Carazolol pubchem
Inverse agonist 2.8 Active 10.1002/CPLU.202400288 2024-08-21
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
7RYC OXYR OT Vasopressin and oxytocin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A oxytocin pubchem gtoplig chembl_ligand drugbank drug_central gtoplig pubchem
Agonist 2.9 Active 10.1038/S41594-022-00728-4 2022-03-09
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
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 gtoplig pubchem
Agonist 3.4 Active 10.1038/S41467-024-46096-Z 2024-03-06
8JHC FZD3 FZD3 Frizzled F (Frizzled) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.3 Active 10.1038/S41421-023-00627-Y 2024-01-17
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
Agonist 3.1 Active 10.1126/SCIADV.ADJ2384 2024-01-24
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
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 Glycoprotein alpha gtoplig
Choriogonadotropin b... gtoplig
AgonistAgonist 4.3 Active 10.1038/S41586-021-03924-2 2021-09-29
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 chembl_ligand pubchem
Agonist 2.8 Active 10.7554/ELIFE.85821 2023-08-16
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 chembl_ligand pubchem
Agonist 3.2 Active 2024-04-03
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
Agonist 2.4 Active 10.1038/S41589-022-01084-6 2022-08-10
8YY8 FZD7 FZD7 Frizzled F (Frizzled) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.2 Active 10.1038/S41422-021-00525-6 2024-04-24
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 10.1038/S41467-017-00630-4 2017-09-27
7EWR GP158 GPR158 C Orphans C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 4.7 Inactive 10.1038/S41467-021-27147-1 2021-12-01
7BVQ ADRB1 β1 Adrenoceptors A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Carazolol pubchem
Inverse agonist 2.5 Inactive 10.1038/S41422-020-00424-2 2020-12-02
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
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
Agonist 2.8 Active 2024-12-04
7CUM GABR2 GABAB2 GABAB C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CGP 54626A pubchem gtoplig chembl_ligand gtoplig
Unknown ligand
NAMNAM 3.5 Inactive 10.1016/J.JMB.2020.09.023 2020-11-11
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
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
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 pubchem
Agonist 2.8 Intermediate 10.1126/SCIENCE.1244142 2013-12-18
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 5-Methyl-4-oxidanyl-... pubchem
Agonist 3.2 Active 10.1038/S41421-023-00610-7 2024-01-03
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)
Apo (no ligand) 3.1 Active 10.1016/J.CHEMBIOL.2023.08.003 2023-07-12
6XBL SMO SMO Frizzled F (Frizzled) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A SAG1.3 pubchem gtoplig chembl_ligand
Cholesterol pubchem
PAMAgonist 3.9 Active 10.1038/S41589-020-0646-2 2020-09-30
2VT4 ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 2 chemicals 2 steps vapour diffusionhanging drop 4 chems 6.9-7.3 18°C (S)-Cyanopindolol pubchem
Antagonist 2.7 Inactive 10.1038/NATURE07101 2008-06-24
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
7T6V FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A synthetic peptide
Agonist 3.1 Active 10.1038/S41467-022-28586-0 2022-03-30
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
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 Dual-agonist peptide...
Agonist 2.5 Active 10.1073/PNAS.2303696120 2023-11-08
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
Agonist 2.9 Active 10.1038/S41422-023-00779-2 2023-03-01
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
8XFT LGR4 LGR4 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A R-spondin-2
Agonist 3.2 Inactive 2024-12-04
6FK9 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine BaculovirusHEK293S(TetR)-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 4.5-4.5 20°C (2~{S})-3-methyl-2-p... pubchem
Agonist 2.6 Active 10.1073/PNAS.1718084115 2018-04-04
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 CHEMBL404594 chembl_ligand pubchem
Agonist 2.9 Active 10.1016/J.CELL.2018.12.006 2019-01-30
6KNM APJ apelin Apelin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Single domain antibo...
Agonist 3.2 Inactive 10.1126/SCIADV.AAX7379 2020-01-29
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.8 Active 10.1038/S41586-024-07153-1 2024-03-06
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
Antagonist 3.6 Inactive 10.1038/S41594-023-01175-5 2023-11-29
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)
Apo (no ligand) 3.4 Active 2024-11-13
7WI8 GRM3 mGlu3 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A LY341495 pubchem gtoplig chembl_ligand gtoplig
Antagonist 4.2 Inactive 10.1038/S41422-022-00623-Z 2022-03-16
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.7 Active 10.1038/S41586-024-07153-1 2024-03-06
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
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 CXCL12α gtoplig
Agonist 3.8 Active 10.1126/SCIADV.ABN8063 2022-07-27
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)
Apo (no ligand) 3.1 Active 10.1073/PNAS.2306145120 2023-10-18
7D3S SCTR secretin Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A SECRETIN chembl_ligand pubchem drugbank pubchem
Agonist 2.9 Active 10.1016/J.BBRC.2020.08.042 2020-11-04
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 CX3CL1 gtoplig
Agonist (partial) 3.8 Active 2015-03-04
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 Cyclomethyltryptopha... pubchem
tecalcet pubchem gtoplig chembl_ligand
AgonistPAM 3.6 Active 2024-04-17
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 gtoplig pubchem
Antagonist 3.2 Inactive 10.1038/S41467-023-44477-4 2024-01-17
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
8UY0 OR2T2 OR2T2 Odorant family 2 O2 (tetrapod specific odorant) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (5S)-2-methyl-5-(pro... pubchem
Agonist 3.2 Active 10.1038/S41586-024-08126-0 2024-10-30
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
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
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 CHEMBL1160787 chembl_ligand pubchem
mevidalen pubchem gtoplig chembl_ligand pubchem
AgonistPAM 3.0 Active 10.1038/S41422-021-00482-0 2021-03-03
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
Inverse agonist 2.4 Inactive 10.1124/MOL.115.101030 2015-09-30
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 chembl_ligand
Agonist 3.3 Active 10.1016/J.CELL.2022.09.041 2022-11-09
7TUY GP183 GPR183 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 8-[(2E)-3-(4-chlorop... pubchem
Inverse agonist 3.0 Active 10.1016/J.STR.2022.04.006 2022-04-13
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 gtoplig pubchem
Agonist 3.3 Active 2023-01-25
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 gtoplig pubchem
Agonist 3.5 Active 10.1073/PNAS.2216329120 2024-01-10
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 pubchem
Antagonist 2.1 Inactive 10.1038/S42004-023-00894-6 2023-05-31
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 (5R,6R)-6-(methylami... pubchem
Agonist 4.0 Active 10.1038/S41586-024-07153-1 2024-03-06
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 pubchem gtoplig chembl_ligand gtoplig gtoplig
Agonist 3.6 Inactive 10.1073/PNAS.1317903111 2014-01-29
7S8N MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (R)-ZINC-3573 pubchem gtoplig chembl_ligand
Agonist 2.9 Active 10.1038/S41586-021-04126-6 2021-11-17
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
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
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 AT118-L Nanobody
Antagonist 3.3 Inactive 10.1038/S41589-024-01620-6 2024-05-22
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 pubchem pubchem
Agonist 3.1 Active 10.1038/S41467-023-40524-2 2023-08-16
7L0Q NTR1 NTS1 Neurotensin A (Rhodopsin) Rat N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
Agonist 4.3 Active 10.1038/S41594-020-00554-6 2021-01-06
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 β-D-hydroxybuty... pubchem gtoplig chembl_ligand
Agonist 2.6 Active 10.1038/S41467-023-43537-Z 2023-12-06
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 pubchem
Agonist 2.8 Active 10.1126/SCIENCE.ADN6354 2024-05-29
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)
Apo (no ligand) 3.1 Inactive 10.1038/S41594-022-00859-8 2022-06-29
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 gtoplig pubchem
Agonist 3.0 Active 2023-10-11
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
7S8M MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Cortistatin 14 pubchem
Agonist 2.5 Active 10.1038/S41586-021-04126-6 2021-11-17
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 pubchem
Agonist 2.7 Active 10.1038/S41422-023-00808-0 2023-06-07
5TE5 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drop 4 chems 5.2-6.6 4°C 10,20-Methanoretinal pubchem
Agonist 4.0 Inactive 10.1073/PNAS.1617446114 2017-03-15
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
Agonist 3.3 Active 10.1038/S41421-024-00700-0 2024-09-18
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 pubchem
Agonist 3.3 Inactive 10.1038/S41586-019-1144-0 2019-04-24
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
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 pubchem
Antagonist 2.7 Active 10.1126/SCIADV.AAX2518 2019-10-30
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 pubchem
Agonist 3.2 Active 10.1038/S41594-024-01397-1 2024-03-13
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
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)
Apo (no ligand) 3.1 Active 10.1038/S41421-022-00403-4 2022-08-24
7MTB OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Retinal (all-trans) pubchem
Agonist 4.0 Active 10.1038/S41586-021-03721-X 2021-07-07
6N51 GRM5 mGlu5 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A quisqualate pubchem gtoplig chembl_ligand drugbank gtoplig pubchem
Agonist 4.0 Intermediate 10.1038/S41586-019-0881-4 2019-01-23
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
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
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 C-C motif chemokine ...
Agonist 3.7 Intermediate 10.1016/J.CELL.2024.07.005 2024-07-31
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 N-ethyl-3-fluoro-3-[... pubchem
Antagonist 2.6 Inactive 10.1038/S41467-022-33880-Y 2022-10-26
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 gtoplig pubchem
Agonist 3.2 Active 2023-01-25
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 pubchem gtoplig chembl_ligand drugbank drug_central gtoplig pubchem
Agonist 3.3 Active 10.1038/S41467-022-31325-0 2022-08-10
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
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
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 gtoplig pubchem
Agonist 4.1 Active 10.1038/S41467-024-55439-9 2024-11-06
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
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 acetylcholine pubchem gtoplig chembl_ligand drugbank drug_central gtoplig pubchem
LY2119620 pubchem gtoplig chembl_ligand
AgonistPAM 3.2 Active 2023-01-25
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 (5S)-5-methyl-4-oxo-... pubchem
Agonist 3.1 Active 10.1038/S41467-023-41650-7 2023-08-30
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 (2E)-N-[(2S)-2-(dime... pubchem
Agonist 3.0 Active 10.1002/ANIE.202200269 2022-04-20
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 N-methyl scopolamine pubchem gtoplig drugbank gtoplig chembl_ligand chembl_ligand chembl_ligand pubchem pubchem
Antagonist 2.3 Inactive 10.1038/S41589-018-0152-Y 2018-11-21
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
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)
Apo (no ligand) 2.9 Active 10.1038/S41422-024-00963-Y 2024-04-10
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... pubchem
Agonist 3.2 Active 10.7554/ELIFE.88204 2023-04-19
7CRH DRD1 D1 Dopamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL1416789 chembl_ligand pubchem
Agonist 3.3 Active 10.1016/J.CELL.2021.01.028 2021-03-03
5EN0 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine Stable_cellsHEK293S(TetR)GnTI-Mammalian 1 chemicals 1 steps vapour diffusionSitting drop 4 chems 5.0-5.0 4°C Retinal (all-trans) pubchem
Agonist 2.8 Active 10.15252/EMBR.201642671 2016-08-10
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 2-[4-(3-Fluorophenyl... pubchem
Agonist 3.1 Active 10.1016/J.CELL.2023.10.014 2023-12-27
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
Agonist 2.8 Active 10.1038/S41422-022-00669-Z 2022-06-01
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 chembl_ligand pubchem
Agonist 3.1 Active 10.1038/S41421-022-00420-3 2022-07-20
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
Agonist 6.0 Active 10.1038/S41467-024-54744-7 2024-11-27
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
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 Apo (no ligand)
Apo (no ligand) 3.1 Active 10.1038/S41467-022-33173-4 2022-09-28
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 gtoplig
Agonist 4.1 Active 10.7554/ELIFE.35946 2018-05-16
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 004-DTR-LYS-TY5-PHE-...
Agonist 3.3 Active 2024-07-03
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
8WVY LGR4 LGR4 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Norrin
Agonist 3.3 Inactive 2024-10-30
1U19 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 6.5-7.5 283 K Retinal (11-cis) pubchem
Inverse agonist 2.2 Inactive 10.1016/J.JMB.2004.07.044 2004-10-12
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 C5a
Agonist 3.2 Active 10.1038/S41422-023-00779-2 2023-03-01
8WVX LGR4 LGR4 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Norrin
Agonist 3.3 Inactive 2024-10-30
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 NNC0640 pubchem gtoplig
NAM 3.0 Inactive 10.1038/NATURE22363 2017-05-24
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 2024-04-03
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 CHEMBL1160787 chembl_ligand pubchem
Agonist 3.0 Active 10.1016/J.CELL.2021.01.027 2021-02-24
6UO9 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 CHEMBL112710 chembl_ligand pubchem pubchem
Agonist 4.8 Intermediate 10.1038/S41586-020-2408-4 2020-06-10
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 pubchem
Antagonist 3.6 Inactive 10.1016/J.STR.2011.06.014 2011-09-07
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.0 Active 10.1038/S41586-024-07153-1 2024-03-06
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 gtoplig
Antagonist 3.0 Inactive 10.1038/S41422-023-00830-2 2023-06-21
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
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 ligand
Agonist 3.6 Active 10.1016/J.CELL.2023.09.020 2023-10-18
5N2S AA1R A1 Adenosine A (Rhodopsin) Human BaculovirusTni PRO (Trichoplusia ni) cell linesInsect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 4 chems 7.5-7.5 20°C PSB36 pubchem
Agonist 3.3 Inactive 10.1016/j.str.2017.06.012 2017-07-26
3C9L OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANANA 1 chemicals 1 steps NANANA 1 chems 0.0-0.0 NA Retinal (11-cis) pubchem
Inverse agonist 2.7 Inactive 10.1107/S0907444908017162 2008-08-05
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 Parathyroid hormone pubchem
Agonist 2.8 Active 2023-07-05
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 pubchem
Agonist 4.1 Active 2020-04-15
6E3Y CALRL calcitonin-like Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Calcitonin gene-rela... pubchem
Agonist 3.3 Active 10.1038/S41586-018-0535-Y 2018-09-19
6UO8 GABR2 GABAB2 GABAB C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL112710 chembl_ligand pubchem pubchem
GS39783 pubchem gtoplig chembl_ligand
AgonistPAM 3.6 Active 10.1038/S41586-020-2408-4 2020-06-10
8GTI CRFR1 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 8-(4-bromo-2,6-dimet... pubchem
Antagonist 2.2 Inactive 10.1038/S12276-023-01082-1 2023-09-13
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 pubchem
Inverse agonist 2.8 Inactive 10.1016/J.STR.2008.05.001 2008-06-17
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06
3PWH AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusSf9Insect 1 chemicals 1 steps vapour diffusionsitting drop 6 chems 8.0-8.8 4°C ZM-241385 pubchem gtoplig chembl_ligand drugbank
Antagonist 3.3 Inactive 10.1016/J.STR.2011.06.014 2011-09-07
7EJX GPR88 GPR88 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A compound 2 [PMID: 24... pubchem gtoplig chembl_ligand
Allosteric agonist 2.4 Active 10.1038/S41467-022-30081-5 2022-04-13
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 pubchem
Antagonist 2.8 Inactive 10.1016/j.str.2017.06.012 2017-07-26
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
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 pro-MCH
Agonist 3.0 Active 10.1038/S41421-024-00679-8 2024-06-19
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
Agonist 3.3 Active 10.1126/SCIADV.ADK4855 2024-05-01
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 chembl_ligand pubchem
Antagonist 2.5 Inactive 10.1038/S41589-021-00866-8 2021-10-13
8G05 GPR84 GPR84 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 6-Octylimino-1,3-dia... pubchem
Agonist 3.0 Active 10.1038/S41467-023-41201-0 2023-11-01
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
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 pubchem gtoplig chembl_ligand gtoplig gtoplig pubchem pubchem pubchem
Agonist 3.3 Active 2024-07-31
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 Apo (no ligand)
Apo (no ligand) 2.9 Active 10.1038/S41586-022-04575-7 2022-04-27
7VUZ MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A PAMP-12 pubchem
Agonist 2.9 Active 10.1038/S41586-021-04077-Y 2021-12-01
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
Agonist 2.7 Active 10.1126/SCIENCE.AAY9813 2020-02-19
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 pubchem chembl_ligand drugbank chembl_ligand pubchem pubchem pubchem
Agonist 2.7 Active 10.1038/S41467-023-43922-8 2024-01-31
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 5-Methyl-4-oxidanyl-... pubchem
Agonist 3.1 Active 10.1038/S41467-023-42764-8 2023-11-22
7ZBC OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Retinal (11-cis) pubchem
Inverse agonist 1.8 Inactive 10.1038/S41586-023-05863-6 2023-03-29
5L7D SMO SMO Frizzled 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 Apo (no ligand)
Apo (no ligand) 3.2 Inactive 10.1038/NATURE18934 2016-07-20
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 gtoplig pubchem
Agonist 3.4 Active 10.1038/S41467-023-42764-8 2023-11-22
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
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 Zevaquenabant pubchem
Inverse agonist 3.3 Inactive 2024-11-20
5WB2 Q80KM9 US28 Unclassified A (Rhodopsin) strain AD169 BaculovirusHEK293S(TetR)-GnTI-Mammalian 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 7 chems 6.0-6.0 16-20°C CX3CL1 gtoplig
Agonist 3.5 Active 10.7554/ELIFE.35850 2018-06-13
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 CHEMBL404594 chembl_ligand pubchem
Agonist 3.4 Active 10.1038/S41598-020-68355-X 2020-07-29
7E6U CASR CaS Calcium-sensing C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 6.0 Inactive 10.7554/ELIFE.68578 2021-09-22
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
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
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 Envelope glycoprotei...
Antagonist 4.5 Inactive 10.1038/S41586-018-0804-9 2018-12-12
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 (5R,6R)-6-(methylami... pubchem
Agonist 4.0 Active 10.1038/S41586-024-07153-1 2024-03-06
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 gtoplig pubchem
CDPPB pubchem gtoplig chembl_ligand
AgonistAgonist 2.9 Active 10.1101/2023.08.29.555158 2023-10-11
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 [(2~{R})-2-[5-(2-hex... pubchem
Agonist 3.5 Active 10.1038/S41467-022-33121-2 2022-10-05
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 (1~{S},3~{R})-3-(1-a... pubchem
Agonist 3.0 Active 10.1038/S41586-023-06804-Z 2023-11-15
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
2YCX ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 2 chemicals 2 steps vapour diffusionNA 3 chems 6.9-7.3 NA (S)-Cyanopindolol pubchem
Antagonist 3.3 Inactive 2011-06-01
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 ICI 118551 pubchem gtoplig chembl_ligand chembl_ligand pubchem
Inverse agonist 2.8 Inactive 10.1021/JA105108Q 2010-08-11
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 Carazolol pubchem
Inverse agonist 4.0 Inactive 10.1371/JOURNAL.PONE.0046039 2012-10-24
8KGK GPR61 GPR61 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.2 Active 10.1038/S41467-023-41654-3 2023-10-11
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 pubchem
Agonist 2.9 Active 10.1073/PNAS.2117716119 2022-09-28
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
8K4S MRGX4 MRGPRX4 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A DCA-3P pubchem
Agonist 2.9 Active 10.1016/J.CELL.2024.10.001 2024-11-06
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 [(2~{R})-2-[5-(2-hex... pubchem
Agonist 3.4 Active 10.1038/S41467-022-33121-2 2022-10-05
8HMV GPR21 GPR21 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 2.9 Active 10.1002/MCO2.205 2023-03-01
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 (5R,6R)-6-(methylami... pubchem
Agonist 4.2 Active 10.1038/S41586-024-07153-1 2024-03-06
5NX2 GLP1R GLP-1 Glucagon B1 (Secretin) Human BaculovirusSf9Insect 2 chemicals 2 steps vapour diffusionSitting drop 4 chems 8.0-9.0 10°C Truncated protein ag...
Agonist 3.7 Intermediate 10.1038/NATURE22800 2017-06-14
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) pubchem gtoplig
Agonist 3.3 Active 10.1038/S41401-022-01032-Z 2022-12-21
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 (5S)-5-[(3R)-4,4-dif... pubchem
Agonist 3.5 Active 10.1073/PNAS.2216329120 2024-01-03
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
7VUG GP139 GPR139 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A JNJ-63533054 pubchem gtoplig chembl_ligand
Agonist 3.2 Active 10.1038/S41422-021-00591-W 2021-12-29
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 5-Methyl-4-oxidanyl-... pubchem
Agonist 3.5 Active 10.1038/S41467-024-46239-2 2024-03-06
6WZG SCTR secretin Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A SECRETIN chembl_ligand pubchem drugbank pubchem
Agonist 2.3 Active 10.1038/S41467-020-17791-4 2020-08-12
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 pubchem gtoplig chembl_ligand gtoplig gtoplig pubchem pubchem pubchem
Agonist 3.4 Active 10.1126/SCIADV.ABM1232 2022-05-18
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 lysophosphatidic aci... pubchem
Agonist 3.1 Active 10.1038/S41467-022-28417-2 2022-02-09
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
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 pubchem
Agonist 4.0 Active 10.1126/SCIADV.ABL5442 2022-01-26
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
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)
Apo (no ligand) 2.6 Active 2025-01-01
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 Carazolol pubchem
Inverse agonist 2.5 Inactive 10.1107/S2059798315021683 2016-01-13
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
Agonist 2.9 Active 2024-06-12
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)
Apo (no ligand) 3.2 Active 10.1073/PNAS.2116506119 2022-04-13
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
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
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
7F54 MC4R MC4 Melanocortin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A afamelanotide pubchem gtoplig chembl_ligand drugbank pubchem pubchem pubchem pubchem pubchem
Agonist 3.0 Active 2021-11-03
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 JDTic pubchem gtoplig chembl_ligand
Antagonist 3.3 Inactive 10.1038/S41467-020-14889-7 2020-03-18
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
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 [Ac-His<sup>1</sup>]... gtoplig chembl_ligand pubchem
Agonist 3.9 Active 10.1038/S41594-020-0386-8 2020-03-11
6UUN CALRL calcitonin-like Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Adrenomedullin pubchem
Agonist 3.0 Active 10.1021/ACSPTSCI.9B00080 2020-03-25
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 4-{(3R)-1-[(1R)-1-(p... pubchem
Agonist 3.0 Active 10.1126/SCIENCE.ADN6354 2024-05-29
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 bremelanotide pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Agonist 3.1 Active 10.1038/S41422-021-00557-Y 2021-09-08
7MTR GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem
2-methoxy-6-propyl-N... pubchem
AgonistAgo-PAM 3.3 Active 10.1038/S41586-021-03680-3 2021-07-07
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 [3H]NEMONAPRIDE chembl_ligand pubchem
Antagonist 2.0 Inactive 10.1126/SCIENCE.AAN5468 2017-10-18
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 gtoplig chembl_ligand drugbank drug_central pubchem pubchem pubchem pubchem pubchem pubchem pubchem
Agonist 3.8 Active 10.1038/S41401-022-01032-Z 2022-12-21
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
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 Lysergide pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.9 Active 10.1016/J.NEURON.2022.08.006 2022-09-21
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 pubchem
Antagonist 2.1 Inactive 10.1016/j.str.2017.06.012 2017-07-26
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 Lysergide pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.9 Intermediate 10.1016/J.CELL.2016.12.033 2017-02-01
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
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 gtoplig pubchem
Agonist 3.3 Active 10.1016/J.STR.2020.11.007 2020-11-18
9EPO FZD7 FZD7 Frizzled F (Frizzled) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 1.9 Inactive 2024-10-02
8W77 O52E4 OR52E4 Odorant family 52 O1 (fish-like odorant) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.6 Inactive 10.1038/S41467-023-43983-9 2023-12-20
6FKC OPSD Rhodopsin Opsins A (Rhodopsin) Bovine BaculovirusHEK293S(TetR)-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 4.5-4.5 20°C 3-[1'-[(2~{S})-2-(4-... pubchem
Agonist 2.5 Active 10.1073/PNAS.1718084115 2018-04-04
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 (1R)-4-[7-(3-carboxy... pubchem
Agonist (partial) 3.7 Active 10.1126/SCIADV.ABN8063 2022-07-27
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
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 gtoplig pubchem
Agonist 2.8 Active 2023-05-17
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 pubchem
Agonist 2.8 Active 10.1038/S41594-022-00796-6 2022-07-20
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 Apo (no ligand)
Apo (no ligand) 3.1 Active 10.1038/S41586-022-04580-W 2022-04-27
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 CHEMBL5430997 chembl_ligand pubchem
Agonist 2.5 Active 2024-05-29
8J1A GPR84 GPR84 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.2 Active 10.1038/S41467-023-38985-6 2023-06-21
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 gtoplig pubchem
Agonist 3.1 Active 10.1038/S41467-024-46840-5 2024-03-20
4A4M OPSD Rhodopsin Opsins A (Rhodopsin) Bovine Stable_cellsHEK293TMammalian 1 chemicals 1 steps vapour diffusionsitting drop 3 chems 4.5-4.5 4°C Retinal (all-trans) pubchem
Agonist 3.3 Active 10.1073/PNAS.1114089108 2012-01-25
5WKT OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drop 4 chems 5.5-5.5 7-10°C B-Octylglucoside pubchem
unknown 3.2 Active 10.1038/NPROT.2017.135 2017-12-13
5WIV DRD4 D4 Dopamine A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 5.9-6.2 20°C [3H]NEMONAPRIDE chembl_ligand pubchem
Antagonist 2.1 Inactive 10.1126/SCIENCE.AAN5468 2017-10-18
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
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 gtoplig pubchem
Agonist 2.7 Active 10.1002/ADVS.202310120 2024-06-05
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
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
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 teriparatide pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem pubchem pubchem pubchem pubchem pubchem
Agonist 2.6 Active 10.1038/S41401-022-01032-Z 2022-12-21
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
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
8HMP GPR52 GPR52 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A derivative 17 [Nakah... pubchem gtoplig chembl_ligand
Agonist 2.8 Active 10.1002/MCO2.260 2023-06-21
7WC8 5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A LUMATEPERONE chembl_ligand chembl_ligand pubchem drugbank pubchem
Agonist 2.5 Inactive 10.1126/SCIENCE.ABL8615 2022-01-26
7Y89 GPR17 GPR17 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.0 Active 10.1002/MCO2.159 2022-10-12
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)
Apo (no ligand) 2.5 Inactive 10.1038/nature19319 2016-09-07
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)
Apo (no ligand) 3.0 Inactive 10.1107/S2052252520000597 2020-03-11
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
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 pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Agonist 4.7 Active 10.1126/SCIADV.ABO7761 2022-09-14
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 CHEMBL58362 chembl_ligand pubchem
Agonist 2.5 Active 10.1038/S41589-022-01208-Y 2022-12-07
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
7T6S FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N-(4-chlorophenyl)-N... pubchem
Agonist 3.0 Active 2022-03-30
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 cinacalcet pubchem gtoplig chembl_ligand drugbank drug_central pubchem
L-tryptophan pubchem gtoplig chembl_ligand drugbank drug_central pubchem
PAMAgonist 3.6 Active 10.1038/S41586-024-07055-2 2024-02-07
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 CCL5 gtoplig
Agonist 3.0 Active 2021-07-14
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 (2S,3S,4R,5R)-5-(6-a... pubchem
Agonist 3.3 Active 10.1016/J.BBRC.2023.149393 2024-01-17
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 [(2~{R})-2-[5-(2-hex... pubchem
Agonist 3.3 Active 10.1038/S41467-022-33121-2 2022-10-05
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
5ZK3 ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL558910 chembl_ligand pubchem
Antagonist 2.6 Inactive 10.1038/S41589-018-0152-Y 2018-11-21
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 H2 relaxin pubchem chembl_ligand pubchem
Agonist 3.2 Active 2023-02-15
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 2-Phenylethanaminium pubchem
Agonist 3.0 Active 10.1038/S41586-023-06775-1 2023-11-22
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 light chain
CS-17 heavy chain
Inverse agonistInverse agonist 3.1 Inactive 10.1038/S41586-022-05159-1 2022-08-10
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.2 Active 10.1038/S41586-024-07153-1 2024-03-06
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 gtoplig pubchem
Agonist 3.0 Active 10.1126/SCIADV.ABJ5347 2022-04-13
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 pubchem gtoplig chembl_ligand drugbank gtoplig chembl_ligand chembl_ligand pubchem
Inverse agonist 2.5 Inactive 10.1073/PNAS.1914446116 2019-12-11
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
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)
Agonist 2.7 Active 10.1038/S41589-021-00918-Z 2022-03-23
6A94 5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A zotepine pubchem gtoplig chembl_ligand drug_central drugbank
Antagonist 2.9 Inactive 10.1038/S41594-018-0180-Z 2019-02-13
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 gtoplig chembl_ligand drugbank drug_central pubchem pubchem
Antagonist 3.0 Inactive 10.1038/S41594-022-00859-8 2022-06-29
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
Agonist 2.9 Active 10.1038/S41422-022-00679-X 2022-08-03
8HVI GP132 GPR132 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A NOX-6-7 pubchem gtoplig
Agonist 3.0 Active 10.1038/S42255-023-00899-4 2023-10-11
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 [(2~{R})-2-[5-(2-hex... pubchem
Agonist 4.5 Active 10.1038/S41467-022-33121-2 2022-10-05
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 ONO-AE3-208 pubchem
Antagonist 3.2 Inactive 10.1038/S41589-018-0131-3 2018-12-05
7MTA OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Retinal (all-trans) pubchem
Agonist 4.1 Active 10.1038/S41586-021-03721-X 2021-07-07
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
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06
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
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 chembl_ligand pubchem
Agonist 3.1 Active 10.1038/S41586-023-06804-Z 2023-11-15
7MT8 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Retinal (all-trans) pubchem
Agonist 5.8 Active 10.1038/S41586-021-03721-X 2021-07-07
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 C5a gtoplig
Agonist 3.2 Active 10.1016/J.CELL.2023.09.020 2023-10-18
8XBH GPR34 GPR34 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL4758243 chembl_ligand pubchem
Agonist 2.8 Active 2023-12-27
7XOX 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 pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.1 Active 10.1038/S41421-022-00420-3 2022-07-20
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 acetylcholine pubchem gtoplig chembl_ligand drugbank drug_central gtoplig pubchem
LY2119620 pubchem gtoplig chembl_ligand
AgonistPAM 3.2 Active 2023-01-25
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
4BVN ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 4 chems 7.0-7.0 22°C (S)-Cyanopindolol pubchem
Antagonist 2.1 Inactive 10.1371/JOURNAL.PONE.0092727 2014-04-02
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 oxymetazoline pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Agonist 2.9 Active 10.1038/S41467-023-39310-X 2023-07-05
6PEL OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Citronellol pubchem
unknown 3.2 Active 2020-06-24
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 CHEMBL3894759 chembl_ligand pubchem
L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem
NAMAgonist 3.3 Inactive 10.1038/S41422-023-00830-2 2023-06-21
5L7I SMO SMO Frizzled 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 pubchem
Antagonist 3.3 Inactive 10.1038/NATURE18934 2016-07-20
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
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
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)
Apo (no ligand) 3.3 Active 10.1038/S41421-023-00610-7 2024-01-03
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 2017-05-03
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 6-methyl-3-[(1S)-2-n... pubchem
CP55940 pubchem gtoplig chembl_ligand gtoplig
PAMAgonist 3.4 Active 10.1038/S41589-022-01038-Y 2022-06-15
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 lysophosphatidic aci... pubchem
Agonist 3.1 Active 2025-01-01
8JGG MRGX1 MRGPRX1 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A bovine adrenal medul... pubchem gtoplig chembl_ligand pubchem
Agonist 3.0 Active 10.1038/S41467-023-40705-Z 2024-01-10
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
Agonist 3.5 Active 10.1038/S41589-022-01130-3 2022-10-19
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)
Apo (no ligand) 3.5 Inactive 10.1038/NSMB.2504 2013-02-27
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
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
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 pubchem
Agonist 2.8 Active 10.1073/PNAS.2219569120 2023-05-24
6XBM SMO SMO Frizzled F (Frizzled) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 24,25-Epoxy-choleste... pubchem
24,25-Epoxy-choleste... pubchem
PAMAgonist 3.2 Active 10.1038/S41589-020-0646-2 2020-09-30
6WW2 FZD5 FZD5 Frizzled F (Frizzled) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.7 Inactive 10.7554/ELIFE.58464 2020-08-19
6DRY 5HT2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A methylergonovine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Agonist 2.9 Intermediate 10.1038/s41594-018-0116-7 2018-08-29
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
8J9N FZD1 FZD1 Frizzled F (Frizzled) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.5 Active 10.1038/S41421-023-00627-Y 2024-01-17
7VUJ GP139 GPR139 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A JNJ-63533054 pubchem gtoplig chembl_ligand
Agonist 3.8 Active 10.1038/S41422-021-00591-W 2021-12-29
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... pubchem
Agonist 3.0 Active 2023-02-22
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
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 PTH
Agonist 2.8 Active 10.1016/J.STR.2023.04.002 2023-04-26
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 rotigotine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Agonist 3.2 Active 10.1038/S41422-023-00808-0 2023-06-21
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 Inactive 2024-07-24
8P12 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.2 Active 2024-11-20
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 pubchem
Agonist 3.2 Active 10.1016/J.CELREP.2024.115024 2024-12-11
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
Antagonist 2.8 Inactive 10.1021/acs.jmedchem.8b01077 2018-10-24
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
6FKB OPSD Rhodopsin Opsins A (Rhodopsin) Bovine BaculovirusHEK293S(TetR)-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 4.5-4.5 20°C 2-(4-Chlorophenyl)-1... pubchem
Agonist 3.0 Active 10.1073/PNAS.1718084115 2018-04-04
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 gtoplig pubchem
Agonist 2.6 Active 10.1038/S41467-024-52585-Y 2024-10-09
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
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
Antagonist 3.2 Inactive 10.1101/2023.12.06.570395 2023-12-27
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
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 2018-06-20
8WVV LGR4 LGR4 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.4 Inactive 2024-10-30
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 2010-10-27
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 s... pubchem chembl_ligand pubchem pubchem
Agonist 2.6 Active 10.1126/SCIENCE.ABM9609 2022-03-30
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
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
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
Agonist 3.0 Active 10.1016/J.CELREP.2024.114381 2024-09-11
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 pubchem
Agonist 3.1 Active 10.1073/PNAS.2014879117 2020-11-18
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
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 drugbank
Agonist 2.7 Active 10.1038/S41467-023-38411-X 2023-07-12
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
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 N-[[3-(hydroxymethyl... pubchem
Agonist 3.3 Active 2024-09-11
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 pubchem
Agonist 3.6 Active 10.1038/S41586-018-0236-6 2018-06-20
8WM9 FZD4 FZD4 Frizzled F (Frizzled) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.5 Active 10.1038/S41467-024-52174-Z 2024-09-11
5DYS OPSD Rhodopsin Opsins A (Rhodopsin) Bovine Stable_cellsHEK293S-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionSitting drop 4 chems 4.5-4.5 20°C Retinal (all-trans) pubchem
Agonist 2.3 Active 2016-08-10
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 chembl_ligand chembl_ligand chembl_ligand pubchem drugbank drugbank pubchem
Agonist (partial) 3.2 Active 10.1038/S41589-023-01389-0 2023-09-06
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, Human pubchem
Agonist 3.3 Active 10.1073/PNAS.2121465119 2022-06-29
4BEZ OPSD Rhodopsin Opsins A (Rhodopsin) Bovine Stable_cellsHEK293S-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionsitting drop 4 chems 4.5-4.5 20°C Apo (no ligand)
Apo (no ligand) 3.3 Active 10.1038/EMBOR.2013.44 2013-04-24
8XFP LGR4 LGR4 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A R-spondin-2
Agonist 3.2 Inactive 2024-12-04
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 pubchem
Agonist 2.8 Active 2024-10-16
8IU2 OPSR OPN1LW Opsins A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Retinal (11-cis) pubchem
Agonist 3.4 Active 2024-03-27
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 pubchem
Antagonist 2.7 Inactive 10.1107/S2052252519013137 2019-11-13
8FCZ OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Retinal (11-cis) pubchem
Inverse agonist 3.7 Inactive 10.1038/S41467-023-40911-9 2023-08-30
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
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 VU-29 pubchem gtoplig chembl_ligand
quisqualate pubchem gtoplig chembl_ligand drugbank gtoplig pubchem
PAMAgonist 3.3 Active 10.1038/S41467-024-55439-9 2024-11-06
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
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 pubchem
Agonist 3.1 Active 10.1126/SCIADV.ABO4158 2022-06-15
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
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
5W0P OPSD Rhodopsin Opsins 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)
Apo (no ligand) 3.0 Active 10.1016/J.CELL.2017.07.002 2017-08-09
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 pubchem
L-tryptophan pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Calcium pubchem
PAMPAMAgonist 2.8 Active 10.1038/S41586-021-03691-0 2021-06-30
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
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 pubchem
Agonist 2.9 Active 10.1038/S41589-021-00930-3 2022-01-05
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 CHEMBL407070 chembl_ligand pubchem pubchem
Agonist 2.7 Active 10.1038/S41422-021-00557-Y 2021-09-08
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
Inverse agonist 2.8 Inactive 10.1074/JBC.M115.689000 2015-10-07
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
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 pubchem
Agonist 3.2 Active 10.1016/J.CELL.2023.09.020 2023-10-18
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)
Apo (no ligand) 3.2 Inactive 10.1016/J.MOLCEL.2023.12.020 2024-02-14
8ITF TAAR9 TAAR9 A orphans 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
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
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
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)
Apo (no ligand) 2.7 Active 10.1038/S41467-023-37177-6 2023-04-12
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
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
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 (1R)-1-(2H-1,3-benzo... pubchem
PAM 2.8 Inactive 2024-10-02
7L1U OX2R OX2 Orexin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Orexin-A pubchem
Agonist 3.2 Active 10.1038/S41467-021-21087-6 2021-02-10
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 pubchem
Agonist 3.0 Active 2011-05-18
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 pubchem
N-Tert-butyl-6,7-dic... pubchem
AgonistAgo-PAM 2.9 Active 10.1038/S41467-021-24058-Z 2021-07-07
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 (2r)-1-(Heptadecanoy... pubchem
BEFIRADOL chembl_ligand pubchem pubchem
PAMAgonist 2.9 Active 2024-05-29
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 4-[6-(2-naphthalen-1... pubchem
Antagonist 2.2 Inactive 10.1038/S41467-022-32447-1 2022-08-10
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 methyl (2R,3S)-3-[(m... pubchem
Agonist 3.3 Active 10.1038/S41467-022-30601-3 2022-06-08
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
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 gtoplig
NAM 2.2 Inactive 2018-03-07
8GTG CRFR1 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 8-(4-bromo-2,6-dimet... pubchem
Antagonist 2.8 Inactive 10.1038/S12276-023-01082-1 2023-09-13
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
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
Agonist 2.8 Active 10.1126/SCIENCE.AAY9813 2020-02-19
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
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 gtoplig
Agonist 2.6 Inactive 10.1016/J.STR.2017.04.008 2017-05-31
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 cinacalcet pubchem gtoplig chembl_ligand drugbank drug_central pubchem
L-tryptophan pubchem gtoplig chembl_ligand drugbank drug_central pubchem
PAMAgonist 3.1 Active 10.1038/S41586-024-07055-2 2024-02-07
8HJ1 GPR21 GPR21 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.3 Active 10.1038/S41467-023-35882-W 2023-12-27
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
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 CCL1
Agonist 3.1 Active 2023-12-20
7LLL GLP1R GLP-1 Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A exendin-4 pubchem gtoplig pubchem
Agonist 3.7 Active 10.1038/S41467-021-27760-0 2022-01-12
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 FME-LEU-PHE
Agonist 3.3 Active 10.1038/S41467-022-29361-X 2022-04-13
6LPK AA2AR A2A Adenosine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ZM-241385 pubchem gtoplig chembl_ligand drugbank
Antagonist 1.8 Inactive 2020-11-25
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 N-(2-aminoethyl)-5-(...
Antagonist 2.9 Intermediate 10.1021/ACS.JMEDCHEM.3C01822 2024-08-07
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
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 2014-04-30
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 4-[[3,4-Dioxo-2-[[(1... pubchem
1-(4-chlorophenyl)-N... pubchem
NAMAntagonist 3.3 Inactive 2024-09-11
6LFO CXCR2 CXCR2 Chemokine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Interleukin-8 pubchem
Agonist 3.4 Active 10.1038/S41586-020-2492-5 2020-09-02
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 pubchem
Agonist 2.6 Active 10.1038/S41586-024-07403-2 2024-05-15
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 2-(Furan-2-yl)-5-N-[... pubchem
Antagonist 2.2 Inactive 10.1021/acs.jmedchem.6b00653 2016-06-29
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... pubchem
Agonist 3.0 Active 10.1126/SCIADV.ABM1232 2022-05-18
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)
Apo (no ligand) 4.5 Inactive 10.1038/S41422-021-00474-0 2021-03-10
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) pubchem gtoplig chembl_ligand pubchem pubchem
Agonist 3.2 Active 10.1016/J.CELL.2022.12.026 2022-12-14
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
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
Agonist 2.9 Active 10.1038/S41589-022-01084-6 2022-08-10
9DQJ MRGRD MRGPRD A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 2-[[1-[1-(4-methoxyp... pubchem
Agonist 2.9 Active 2024-12-11
6KUW ADA2C α2C Adrenoceptors A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (8Ar,12aS,13aR)-12-e... pubchem
Antagonist 2.8 Inactive 2019-12-04
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 pubchem
mevidalen pubchem gtoplig chembl_ligand pubchem
AgonistPAM 3.0 Active 10.1038/S41467-022-30929-W 2022-06-15
6I9K B1B1U5 Rhodopsin Opsins A (Rhodopsin) Hasarius adansoni N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Retinal (11-cis) pubchem
Inverse agonist 2.2 Inactive 10.1073/PNAS.1902192116 2019-07-03
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 Lysergide pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.6 Active 10.1016/J.NEURON.2024.07.003 2024-09-04
6O3C SMO SMO Frizzled 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 SAG21k pubchem
Agonist 2.8 Active 10.1038/S41586-019-1355-4 2019-07-03
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)
Apo (no ligand) 6.0 Inactive 10.1038/S41467-023-36170-3 2023-03-22
3AYN OPSD Rhodopsin Opsins A (Rhodopsin) Japanese flying squid NANativeSquid 1 chemicals 1 steps vapour diffusionsitting drop 5 chems 6.0-6.0 4°C Retinal (9-cis) pubchem
Inverse agonist 2.7 Inactive 10.1016/J.JMB.2011.08.044 2011-08-17
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 CHEMBL216166 chembl_ligand pubchem
Agonist 2.5 Active 10.1371/JOURNAL.PBIO.3002673 2024-05-22
8UXV O51G2 OR51G2 Odorant family 51 O1 (fish-like odorant) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.2 Active 10.1038/S41586-024-08126-0 2024-10-30
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 heavy c...
Agonist 3.1 Inactive 10.1038/S41594-024-01397-1 2024-03-13
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 pubchem
Agonist 3.2 Active 10.1038/S12276-024-01296-X 2024-09-11
8KEX MRGX4 MRGPRX4 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A DCA-3P pubchem
Agonist 3.2 Active 10.1016/J.CELL.2024.10.001 2024-11-06
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)
Apo (no ligand) 3.3 Active 10.1016/J.CELL.2023.09.020 2023-10-18
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 chembl_ligand drugbank pubchem
Agonist 3.0 Active 10.1126/SCIENCE.ABF7958 2021-04-28
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
Inverse agonist 3.1 Inactive 2024-11-20
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
NAM 2.2 Active 10.1038/NATURE14287 2015-04-01
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
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 pubchem
Agonist 3.4 Active 10.1126/SCIADV.ADJ2384 2024-01-24
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
7Y13 MRGRD MRGPRD A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.1 Intermediate 10.1038/S42003-022-03668-3 2022-07-20
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 HYDROCORTISONE chembl_ligand pubchem
Agonist 2.9 Active 10.1038/S41586-020-03083-W 2021-02-03
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...
Agonist 2.0 Active 10.1038/S41589-023-01393-4 2023-08-02
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 chembl_ligand pubchem
Agonist 3.3 Active 10.1016/J.CELL.2023.10.014 2023-12-27
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 pubchem
Antagonist 3.2 Inactive 10.1124/MOLPHARM.122.000633 2023-03-22
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
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
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 pubchem gtoplig chembl_ligand drugbank gtoplig
Agonist 2.9 Active 10.1038/S41467-022-28399-1 2022-01-05
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 chembl_ligand chembl_ligand chembl_ligand pubchem drugbank drugbank pubchem
Agonist 3.8 Active 10.1038/S41421-020-0176-9 2020-08-05
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
Agonist 3.5 Intermediate 10.1073/PNAS.2414544121 2024-11-13
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 pubchem
Agonist 2.8 Active 10.1126/SCIENCE.AAU5595 2018-10-17
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)
Apo (no ligand) 2.8 Active 10.1038/S41467-021-24438-5 2021-07-14
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 2-Phenylethanaminium pubchem
Agonist 3.5 Active 10.1016/J.CELL.2023.10.014 2023-12-27
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
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 gtoplig
Agonist 3.3 Active 10.1126/SCIADV.ADD3709 2023-05-03
6OSA NTR1 NTS1 Neurotensin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A JMV449 pubchem gtoplig chembl_ligand
Agonist 3.0 Active 10.1038/S41586-019-1337-6 2019-07-10
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 pubchem
Agonist 3.6 Active 10.1126/SCIADV.ABJ5347 2022-04-13
7CX2 PE2R2 EP2 Prostanoid A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A PGE2 pubchem gtoplig chembl_ligand drugbank drug_central gtoplig pubchem
Agonist 2.8 Active 10.1126/SCIADV.ABF1268 2021-05-05
4Z9G CRFR1 CRF1 Corticotropin-releasing factor B1 (Secretin) Human BaculovirusHi5Insect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 4 chems 5.5-5.5 23°C CP 376,395 pubchem gtoplig chembl_ligand
Antagonist 3.2 Inactive 10.2174/1874467210666170110114727 2016-06-29
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 gtoplig pubchem
Agonist 3.0 Active 10.1038/S41467-024-55439-9 2024-11-06
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
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
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 pubchem
Agonist 3.0 Active 10.1016/J.MOLCEL.2021.01.003 2021-03-10
2Y00 ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 1 chemicals 1 steps vapour diffusionsitting drops 6 chems 8.5-8.5 4°C Dobutamine pubchem
Agonist (partial) 2.5 Inactive 10.1038/NATURE09746 2011-01-12
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 chembl_ligand
Agonist 2.9 Active 10.1038/S41467-023-41650-7 2023-09-13
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 salmeterol pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Agonist 3.0 Active 10.1038/s41589-018-0145-x 2018-11-14
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
Agonist 2.9 Active 2024-04-03
8TB7 GPR61 GPR61 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A compound 1 [PMID: 37... pubchem gtoplig
Inverse agonist 2.9 Active 10.1038/S41467-023-41646-3 2023-10-04
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 2-methoxy-6-propyl-N... pubchem
L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem
Ago-PAMAgonist 3.2 Active 10.1038/S41586-021-03680-3 2021-07-07
7T6U FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A synthetic peptide
Agonist 2.9 Active 10.1038/S41467-022-28586-0 2022-03-30
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
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 drugbank chembl_ligand pubchem
Agonist 2.6 Active 10.1038/S41586-023-06775-1 2023-11-22
8HQE GP132 GPR132 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.0 Active 10.1038/S42255-023-00899-4 2023-10-11
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 pro-MCH
Agonist 2.4 Active 10.1038/S41421-024-00679-8 2024-06-19
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 pubchem
mevidalen pubchem gtoplig chembl_ligand pubchem
AgonistPAM 3.1 Active 10.1016/J.CELL.2021.01.028 2021-03-03
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 pubchem
Agonist 2.1 Active 10.1038/NATURE14886 2015-08-05
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
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
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 [(2~{R})-1-hexadecan...
PAM 2.5 Active 2024-12-04
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
Agonist 3.0 Active 10.1038/s41586-019-1902-z 2020-01-08
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 Cyclomethyltryptopha... pubchem
Agonist 2.7 Active 10.1073/PNAS.2115849118 2022-01-19
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 chembl_ligand chembl_ligand chembl_ligand pubchem drugbank drugbank pubchem
Agonist 3.3 Active 10.1038/S41586-020-2419-1 2020-06-17
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 Dual-agonist peptide...
Agonist 3.4 Active 2023-09-13
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 pubchem gtoplig chembl_ligand gtoplig gtoplig
Agonist 3.1 Active 10.1038/S41589-021-00890-8 2021-11-03
7DDZ NPY2R Y2 Neuropeptide Y A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL1823578 chembl_ligand pubchem
Antagonist 2.8 Inactive 10.1038/S41467-021-21030-9 2021-01-27
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
7VL8 CCR1 CCR1 Chemokine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 2.9 Active 10.1038/S41589-021-00918-Z 2022-03-23
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
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
7TRY CRFR2 CRF2 Corticotropin-releasing factor B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Urocortin pubchem
Agonist 3.7 Active 10.1038/S41467-022-33851-3 2022-11-09
8JD1 GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem
Agonist 3.7 Inactive 10.1038/S41422-023-00830-2 2023-06-21
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
Antagonist 1.8 Inactive 10.1126/SCIENCE.1219218 2012-07-25
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.0 Active 10.1038/S41586-024-07153-1 2024-03-06
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 drugbank chembl_ligand pubchem
Agonist 3.2 Active 10.1038/S41586-023-06804-Z 2023-11-15
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 pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem
Agonist 3.3 Active 10.1038/S41422-022-00751-6 2023-01-11
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 CHEMBL5197819 chembl_ligand pubchem
glucagon-like peptid... pubchem gtoplig chembl_ligand gtoplig pubchem pubchem
PAMAgonist 3.3 Active 10.1038/S41589-020-0589-7 2020-07-22
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 pubchem
Antagonist 2.8 Inactive 10.1038/NSMB.3183 2016-03-09
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 3.0 Active 2024-07-24
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 Apelin receptor earl...
Agonist 3.8 Active 10.1038/S41594-022-00797-5 2022-07-27
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 N-[(2S)-2-(dimethyla... pubchem
Agonist 2.9 Active 10.1002/ANIE.202200269 2022-04-20
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 gtoplig pubchem
Agonist 3.3 Active 10.1038/S41467-021-22427-2 2021-03-31
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 s... pubchem chembl_ligand pubchem pubchem
Agonist 3.0 Active 10.1126/SCIENCE.ABM9609 2022-03-23
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 gtoplig pubchem
Agonist 2.6 Active 10.1038/S41467-023-43537-Z 2023-12-06
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
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 pubchem
Agonist 3.1 Active 10.1126/SCIADV.ABO4158 2022-06-15
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)
Apo (no ligand) 3.3 Inactive 10.1038/S41589-023-01389-0 2023-09-06
7XV3 GP174 GPR174 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (2~{S})-2-$l^{4}-aza... pubchem
Agonist 2.8 Active 10.1038/S41467-023-36575-0 2023-02-15
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
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 CX3CL1 gtoplig
Agonist (partial) 2.9 Active 10.1126/SCIENCE.AAA5026 2015-03-04
8F76 O51E2 OR51E2 Odorant family 51 O1 (fish-like odorant) 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
Agonist 3.1 Active 10.1038/S41586-023-05798-Y 2023-03-22
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 Apo (no ligand)
Apo (no ligand) 3.0 Active 10.1038/S41586-022-04619-Y 2022-05-11
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
8IW1 TAAR9 TAAR9 A orphans 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 2-Phenylethanaminium pubchem
Agonist 3.4 Active 10.1038/S41586-023-06106-4 2023-05-31
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 gtoplig
Antagonist 3.0 Inactive 10.1038/S41422-023-00830-2 2023-06-21
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
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 CHEMBL4576388 chembl_ligand pubchem
JMV431 gtoplig chembl_ligand pubchem
PAMAgonist 3.1 Active 10.1038/S41586-023-06395-9 2023-08-09
8K4N GPR34 GPR34 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (2R)-2-azanyl-3-[oxi... pubchem
Agonist 2.8 Active 2023-10-25
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 pubchem
Agonist 3.2 Active 10.1126/SCIADV.ABN0067 2022-04-06
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 pubchem gtoplig chembl_ligand gtoplig pubchem pubchem pubchem pubchem
Agonist 2.6 Active 10.1038/S41467-022-29072-3 2022-04-20
8FD0 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.7 Inactive 10.1038/S41467-023-40911-9 2023-08-30
6FK6 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine BaculovirusHEK293S(TetR)-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 4.5-4.5 20°C COMPOUND SUMMARY pubchem
Agonist 2.4 Active 10.1073/PNAS.1718084115 2018-04-04
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 pubchem
Agonist 3.3 Active 10.1093/NSR/NWAA284 2020-12-16
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 ACE-TYR-ALA-DTY-THR-...
Agonist 2.5 Active 10.1038/s41467-023-43718-w 2023-12-06
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 pubchem
mevidalen pubchem gtoplig chembl_ligand pubchem
AgonistPAM 3.2 Active 2021-03-03
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
Agonist 2.8 Active 10.1038/S41586-023-06775-1 2023-11-22
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06
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...
Agonist 2.8 Active 10.1038/S41421-024-00754-0 2024-11-13
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 pubchem
Agonist 3.1 Active 10.1126/SCIADV.ADJ2384 2024-01-24
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...
Agonist 4.0 Active 10.1126/SCIENCE.AAV7942 2019-04-17
8XBG GPR34 GPR34 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL4782438 chembl_ligand pubchem
Agonist 3.4 Active 10.1038/S41467-024-45046-Z 2024-05-15
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
Agonist 2.7 Active 10.1038/S41421-024-00700-0 2024-09-18
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 carazolol pubchem gtoplig chembl_ligand drug_central
Antagonist 3.4 Inactive 10.1107/S2052252519013137 2019-11-13
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
Antagonist 2.8 Inactive 10.1016/J.CELL.2018.12.011 2019-01-30
7MT9 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Retinal (all-trans) pubchem
Agonist 7.0 Active 10.1038/S41586-021-03721-X 2021-07-07
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 chembl_ligand pubchem chembl_ligand pubchem
Agonist 3.2 Active 10.1038/S41467-023-36673-Z 2023-04-19
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 Peptide Agonist fMLF
Agonist 2.9 Active 10.1038/S41467-022-32822-Y 2022-05-25
4DAJ ACM3 M3 Acetylcholine (muscarinic) A (Rhodopsin) Rat BaculovirusSf9Insect 6 chemicals 6 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 7.5-7.5 22°C tiotropium pubchem gtoplig chembl_ligand drugbank gtoplig chembl_ligand chembl_ligand pubchem
Antagonist 3.4 Inactive 10.1038/NATURE10867 2012-02-22
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 CHEMBL407070 chembl_ligand pubchem pubchem
Agonist 2.9 Active 10.1038/S41422-021-00557-Y 2021-09-08
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 L-tryptophan pubchem gtoplig chembl_ligand drugbank drug_central pubchem
cinacalcet pubchem gtoplig chembl_ligand drugbank drug_central pubchem
AgonistPAM 2.8 Active 10.1038/S41586-024-07055-2 2024-02-07
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
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 humanin pubchem gtoplig chembl_ligand pubchem
Agonist 2.8 Active 10.1038/S41467-022-29361-X 2022-04-13
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 chembl_ligand
Agonist 2.8 Active 10.1016/J.CELREP.2023.113406 2024-01-10
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 pubchem
Antagonist 3.6 Inactive 10.1038/NSMB.3450 2017-08-16
6M9T PE2R3 EP3 Prostanoid A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Misoprostol-FA pubchem
Agonist 2.5 Active 10.1038/S41589-018-0160-Y 2018-12-05
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 pubchem gtoplig chembl_ligand gtoplig pubchem pubchem
Agonist 3.2 Active 10.1126/SCIADV.ADE9020 2023-04-12
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.0 Active 10.1038/S41586-024-07153-1 2024-03-06
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
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
6D32 Q98SW5 SMO Frizzled F (Frizzled) African clawed frog BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 6.0-6.5 20°C cyclopamine pubchem gtoplig chembl_ligand
Agonist (partial) 3.8 Active 10.1016/J.CELL.2018.04.029 2018-05-23
9DQH MRGRD MRGPRD A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 2-[[1-[2-(4-chloroph... pubchem
Agonist 2.9 Active 2024-12-11
7DFP DRD2 D2 Dopamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A spiperone pubchem gtoplig chembl_ligand drug_central gtoplig
Antagonist 3.1 Inactive 10.1038/S41467-020-20221-0 2020-12-30
6ME4 MTR1A MT1 Melatonin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 2-iodo-melatonin pubchem gtoplig chembl_ligand drugbank
Agonist 3.2 Inactive 10.1038/S41586-019-1141-3 2019-04-24
5O9H C5AR1 C5a1 Complement peptide A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 5 chems 5.5-6.0 22.5°C NDT9513727 pubchem gtoplig chembl_ligand
Antagonist 2.7 Inactive 10.1038/NATURE25025 2018-01-10
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 pubchem
Agonist 3.8 Active 10.1038/S41586-020-2379-5 2020-06-17
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
Allosteric agonist 2.3 Active 10.1038/NATURE13494 2014-07-16
6WGT 5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Lysergide pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.4 Inactive 10.1016/J.CELL.2020.08.024 2020-09-23
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 chembl_ligand pubchem
Agonist 3.2 Active 10.1038/S42003-024-06905-Z 2024-10-02
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 pubchem gtoplig chembl_ligand gtoplig gtoplig pubchem pubchem pubchem
Agonist 3.2 Active 10.1038/S41467-022-28510-6 2022-02-23
7DD5 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 L-tryptophan pubchem gtoplig chembl_ligand drugbank drug_central pubchem
NPS 2143 pubchem gtoplig chembl_ligand drugbank
Calcium pubchem
PAMNAMAgonist 3.2 Inactive 10.1126/SCIADV.ABG1483 2021-06-16
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 pubchem
Inverse agonist 2.9 Inactive 10.1038/NATURE25758 2018-03-14
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
8A6E OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Retinal (11-cis) pubchem
Agonist 1.8 Inactive 10.1038/S41586-023-05863-6 2023-03-29
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 chembl_ligand
Antagonist 3.4 Inactive 10.1073/PNAS.1812717115 2018-12-12
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 10.1126/SCIADV.ADK5184 2024-03-06
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 A-(1-8) pubchem gtoplig chembl_ligand pubchem pubchem
Agonist 3.3 Active 10.1093/PROCEL/PWAC033 2023-05-24
5IU7 AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusTni PRO (Trichoplusia ni) cell linesInsect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 5.3-5.4 20°C 2-(Furan-2-yl)-5-N-[... pubchem
Antagonist 1.9 Inactive 10.1021/acs.jmedchem.6b00653 2016-06-29
4N4W SMO SMO Frizzled 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
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
Allosteric agonist 2.2 Active 10.1038/NSMB.3417 2017-06-07
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 L-tryptophan pubchem gtoplig chembl_ligand drugbank drug_central pubchem
PAM 4.4 Intermediate 10.1038/S41422-021-00474-0 2021-03-10
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
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
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
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 Cyclomethyltryptopha... pubchem
tecalcet pubchem gtoplig chembl_ligand
AgonistAgonist 2.7 Active 10.1073/PNAS.2115849118 2022-01-19
2ZIY OPSD Rhodopsin Opsins A (Rhodopsin) Japanese flying squid NANativeSquid 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 7.0-7.0 20°C Retinal (11-cis) pubchem
Inverse agonist 3.7 Inactive 10.1074/JBC.C800040200 2008-05-06
6GPS CCR2 CCR2 Chemokine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A MK-0812 pubchem
Antagonist 3.3 Inactive 10.1016/J.STR.2018.10.027 2019-01-02
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 pubchem
Agonist 3.1 Active 10.1038/S41422-023-00835-X 2023-06-21
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
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 gtoplig chembl_ligand gtoplig gtoplig
Agonist 3.1 Inactive 10.1073/PNAS.1317903111 2014-01-29
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 pubchem
Antagonist 3.1 Inactive 10.1038/S41467-020-14884-Y 2020-03-04
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 Apo (no ligand)
Apo (no ligand) 2.8 Active 10.1016/J.MOLCEL.2022.10.009 2022-10-26
7RMG NK1R NK1 Tachykinin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A substance P pubchem gtoplig chembl_ligand gtoplig gtoplig
Agonist 3.0 Active 10.1038/S41589-021-00890-8 2021-11-03
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 JNJ-40411813 pubchem gtoplig chembl_ligand drugbank
L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem
ADX88178 pubchem gtoplig chembl_ligand
PAMAgonistAgonist 3.6 Active 10.1038/S41422-023-00830-2 2023-06-21
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... pubchem
Agonist 2.4 Active 10.1021/ACS.BIOCHEM.4C00114 2024-04-24
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 CHEMBL3354065 chembl_ligand pubchem
Agonist 3.0 Active 10.1016/J.MOLCEL.2023.07.030 2023-09-06
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 chembl_ligand pubchem
Agonist 3.1 Active 10.7554/ELIFE.85821 2023-08-16
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 lysophosphatidic aci... pubchem
Agonist 3.0 Active 2025-01-01
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 CHEMBL216166 chembl_ligand pubchem
Agonist 2.4 Active 10.1371/JOURNAL.PBIO.3001295 2021-05-26
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 chembl_ligand pubchem
Agonist 2.6 Active 10.1016/J.MOLCEL.2020.08.001 2020-09-02
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
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 gtoplig chembl_ligand drugbank drug_central gtoplig pubchem pubchem pubchem pubchem pubchem
Agonist 3.7 Active 10.1126/SCIENCE.AAZ5346 2020-04-01
5V57 SMO SMO Frizzled F (Frizzled) Human Transient_transfectionHEK293FMammalian 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 5.0-5.0 20°C N-methyl-N-[1-[4-(2-... pubchem
Antagonist 3.0 Inactive 10.1038/NCOMMS15383 2017-05-24
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 pubchem gtoplig chembl_ligand drugbank drug_central gtoplig pubchem pubchem pubchem pubchem pubchem
Agonist 3.0 Active 10.1038/S41422-020-00442-0 2020-12-16
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06
6H7N ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (S)-Xamoterol pubchem
Agonist 2.5 Active 10.1101/436212 2018-10-17
8T1W GPR6 GPR6 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CVN424 pubchem gtoplig chembl_ligand chembl_ligand drugbank pubchem
Inverse agonist 3.5 Inactive 10.1126/SCISIGNAL.ADO8741 2024-12-04
7TYL CALCR CT Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Amylin rat pubchem
Agonist 3.3 Active 10.1126/SCIENCE.ABM9609 2022-03-23
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 gtoplig pubchem
Agonist 2.9 Active 10.1016/J.JMB.2024.168795 2024-10-02
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
Agonist 3.8 Active 10.1038/S41586-018-0241-9 2018-06-20
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 pubchem pubchem
Agonist 2.8 Active 10.1038/S12276-024-01296-X 2024-09-11
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 naloxone pubchem gtoplig chembl_ligand drugbank drug_central gtoplig pubchem
(2S)-3-(3-methoxy-4-... pubchem
AntagonistNAM 3.3 Inactive 2024-07-17
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
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 gtoplig
Agonist 3.9 Active 2024-12-18
6LI1 GPR52 GPR52 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 2.9 Inactive 10.1038/S41586-020-2019-0 2020-02-26
6LPL AA2AR A2A Adenosine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ZM-241385 pubchem gtoplig chembl_ligand drugbank
Antagonist 2.0 Inactive 10.1038/S41598-020-76277-X 2020-11-25
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)
Apo (no ligand) 2.8 Active 2024-11-13
7VDM MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A substance P pubchem gtoplig chembl_ligand gtoplig gtoplig
Agonist 3.0 Active 10.1038/S41586-021-04077-Y 2021-12-01
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 pubchem
Agonist 3.1 Active 2024-07-03
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
7PIU MC4R MC4 Melanocortin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A setmelanotide pubchem gtoplig drug_central chembl_ligand drugbank pubchem
Agonist 2.6 Active 10.1038/S41422-021-00569-8 2021-11-17
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 PGE2 pubchem gtoplig chembl_ligand drugbank drug_central gtoplig pubchem
Agonist 3.2 Active 10.1038/S41422-024-00963-Y 2024-04-10
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
Agonist 2.7 Active 10.1021/ACS.JMEDCHEM.4C01961 2024-10-16
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 chembl_ligand pubchem
Agonist 3.5 Active 2023-03-22
8Y69 LGR4 LGR4 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A R-spondin-2
Agonist 3.4 Inactive 2024-12-04
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 N1-(7-Chloroquinolin... pubchem
Agonist 2.6 Active 2024-04-10
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 3.1 Active 10.1038/S41467-023-41650-7 2023-08-30
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 Apo (no ligand)
Apo (no ligand) 3.3 Active 10.1038/S41586-022-04590-8 2022-04-27
8TRC GRM3 mGlu3 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A LY341495 pubchem gtoplig chembl_ligand gtoplig
Antagonist 3.3 Inactive 10.1101/2023.08.13.552748 2024-07-31
6H7L ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Dobutamine pubchem
Agonist 2.7 Active 10.1126/SCIENCE.AAU5595 2018-10-17
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 3.1 Active 2024-07-24
7JHJ Q3KSP2 BILF1 Unclassified A (Rhodopsin) strain GD1 N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.2 Active 10.1016/J.IMMUNI.2021.06.001 2021-07-07
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 Neuromedin U-25 (hum... pubchem
Agonist 3.3 Active 10.1038/S41467-022-34814-4 2023-02-22
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 gtoplig
Agonist 2.9 Active 10.1016/J.CELREP.2024.114422 2024-11-13
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
8KH4 GP161 GPR161 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.1 Active 10.1038/S41467-023-41654-3 2023-10-11
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 chembl_ligand pubchem drugbank pubchem
Agonist 4.3 Active 10.1038/S41467-020-17791-4 2020-08-12
6D35 Q98SW5 SMO Frizzled F (Frizzled) African clawed frog BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 6.0-6.5 20°C Cholesterol pubchem
Agonist 3.9 Active 10.1016/J.CELL.2018.04.029 2018-05-23
5XRA CNR1 CB1 Cannabinoid A (Rhodopsin) Human Transient_transfectionHEK293TMammalian 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 6.4-6.4 20°C AM11542 pubchem gtoplig chembl_ligand
Agonist 2.8 Active 2017-07-12
8TR2 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 (1S,4R,5R,6S)-4-amin... pubchem
Agonist 3.5 Active 10.1101/2023.08.13.552748 2024-07-31
8W8R GP101 GPR101 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 1-(4-Methylpyridin-2... pubchem
Agonist 3.3 Active 10.1038/S41589-023-01456-6 2024-01-03
8HSC GPR20 GPR20 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.2 Active 10.1038/S41421-023-00520-8 2023-03-08
6IQL DRD4 D4 Dopamine A (Rhodopsin) Mouse N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A L745870 pubchem gtoplig chembl_ligand
Antagonist 3.5 Inactive 10.7554/ELIFE.48822 2019-12-04
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
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
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
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
Cholesterol pubchem
Allosteric agonistAgonist 3.1 Inactive 2024-07-24
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
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
8HJ2 GPR21 GPR21 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.8 Active 10.1038/S41467-023-35882-W 2023-03-15
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 (5S)-5-methyl-4-oxo-... pubchem
Agonist 3.1 Active 10.1038/S41467-023-41650-7 2023-08-30
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 VU0364770 pubchem gtoplig chembl_ligand
Agonist 3.4 Active 10.1038/S41422-023-00830-2 2023-06-21
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 gtoplig pubchem pubchem pubchem drugbank
Agonist (partial) 2.7 Inactive 10.1038/S41467-018-07094-0 2018-11-21
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 1-(4-fluorophenyl)-4... pubchem
Agonist 3.0 Active 10.1016/J.CELL.2024.02.034 2024-02-28
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
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 4-(3-Bromo-5-ethoxy-... pubchem
Antagonist 3.0 Active 2025-01-01
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 JMV431 gtoplig chembl_ligand pubchem
Agonist 2.8 Active 10.1038/NATURE11558 2012-10-17
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 N-(tert-butylsulfony... pubchem
Antagonist 2.9 Inactive 10.1038/S41467-021-23149-1 2021-02-17
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 pubchem
Agonist 2.9 Active 2023-07-05
6FKD OPSD Rhodopsin Opsins A (Rhodopsin) Bovine BaculovirusHEK293S(TetR)-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 4.5-4.5 20°C 5-chloro-2-(2-oxo-2-... pubchem
Agonist 2.5 Active 10.1073/PNAS.1718084115 2018-04-04
8ZFJ E7FEL0 GPR4 A orphans 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)
Apo (no ligand) 3.1 Active 2024-08-07
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
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 pubchem
Antagonist 3.3 Inactive 2024-08-28
6BD4 FZD4 FZD4 Frizzled F (Frizzled) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 2.4 Inactive 10.1038/S41586-018-0447-X 2018-08-22
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 avacopan pubchem gtoplig chembl_ligand drugbank pubchem
PMX53 pubchem gtoplig chembl_ligand
NAMAntagonist 2.2 Inactive 10.1038/S41594-018-0067-Z 2018-05-30
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
8KGG P2Y10 P2RY10 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (2~{S})-2-$l^{4}-aza...
Agonist 3.1 Active 10.1016/J.CHEMBIOL.2024.08.005 2024-07-31
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 pubchem
Agonist 2.6 Active 10.1038/S41467-022-28417-2 2022-02-09
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 pubchem pubchem
Agonist 2.3 Active 10.1002/CPLU.202400288 2024-08-21
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)
Apo (no ligand) 3.2 Active 10.1073/PNAS.2306145120 2023-10-18
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 Cyclomethyltryptopha... pubchem
tecalcet pubchem gtoplig chembl_ligand
AgonistPAM 3.5 Active 10.1038/S41586-024-07331-1 2024-04-17
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 Sipagladenant pubchem
Inverse agonist 2.3 Inactive 10.1124/MOLPHARM.122.000633 2023-03-22
6VJM GABR2 GABAB2 GABAB C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 4.0 Inactive 10.1038/S41586-020-2408-4 2020-06-10
2Z73 OPSD Rhodopsin Opsins A (Rhodopsin) Japanese flying squid NANativeSquid 1 chemicals 1 steps vapour diffusionsitting drops 5 chems 6.4-6.4 4°C Retinal (11-cis) pubchem
Inverse agonist 2.5 Inactive 10.1038/NATURE06925 2008-05-13
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
NAM 3.2 Inactive 2017-05-24
7EPF GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (8~{R})-4-[2,4-Bis(f... pubchem
NAM 2.7 Inactive 10.1038/S41586-021-03641-W 2021-06-23
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 pubchem
Agonist 3.1 Active 10.1038/S41422-021-00566-X 2021-09-29
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
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
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
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 VU0467154 pubchem gtoplig chembl_ligand
iperoxo pubchem gtoplig chembl_ligand
PAMAgonist 2.5 Active 2023-05-17
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
Agonist 3.1 Active 10.1038/S41422-022-00679-X 2022-08-03
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
2YCW ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 2 chemicals 2 steps vapour diffusionNA 3 chems 8.1-8.1 NA Carazolol pubchem
Antagonist 3.0 Inactive 10.1073/PNAS.1100185108 2011-06-01
6OY9 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Retinal (all-trans) pubchem
Agonist 3.9 Active 10.1016/J.MOLCEL.2019.06.007 2019-07-24
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
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 SAR425899
Agonist 2.6 Active 10.1073/PNAS.2303696120 2023-09-06
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)
Apo (no ligand) 2.1 Active 10.1038/S41586-019-1663-8 2019-08-14
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
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
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
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 Cyanopindolol pubchem
Antagonist 2.5 Active 10.1038/S41467-022-31823-1 2022-07-27
8W8S GP101 GPR101 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 1-(4-Methylpyridin-2... pubchem
Agonist 3.3 Active 10.1038/S41589-023-01456-6 2024-01-03
6CMO OPSD Rhodopsin Opsins 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 Apo (no ligand)
Apo (no ligand) 4.5 Active 10.1038/S41586-018-0215-Y 2018-06-20
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 JMV431 gtoplig chembl_ligand pubchem
Agonist 2.6 Intermediate 10.1126/sciadv.abe5504 2021-02-10
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 (1R,2S)-N-[4-(2,6-di... pubchem
Agonist 3.7 Active 10.1038/S41594-022-00797-5 2022-07-27
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)
Apo (no ligand) 4.0 Active 10.1038/NATURE22309 2017-05-03
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
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
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)
Apo (no ligand) 2.8 Active 10.1038/S41467-022-33173-4 2022-09-28
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 pubchem gtoplig chembl_ligand gtoplig pubchem pubchem pubchem pubchem
Agonist 3.3 Active 2023-05-03
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
tecalcet pubchem gtoplig chembl_ligand
AgonistPAM 3.8 Active 2024-04-17
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 chembl_ligand pubchem
Agonist 4.6 Active 10.1038/S42003-024-06905-Z 2024-10-02
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
7JNI AGTR2 AT2 Angiotensin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A olodanrigan pubchem gtoplig chembl_ligand drugbank
Antagonist 3.0 Active 10.1073/PNAS.2116289119 2022-02-09
7VV0 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A PAMP-12 pubchem
Agonist 3.5 Active 10.1038/S41586-021-04077-Y 2021-12-01
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 pubchem
Agonist 3.4 Active 10.1038/S41422-021-00566-X 2021-09-29
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 pubchem
Antagonist 2.1 Inactive 10.1038/S42004-023-00894-6 2023-07-12
7VUY MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A PAMP-12 pubchem
Agonist 2.8 Active 10.1038/S41586-021-04077-Y 2021-12-01
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.6 Active 10.1038/S41586-024-07153-1 2024-03-06
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 chembl_ligand pubchem
Agonist 2.7 Active 10.1016/J.MOLCEL.2021.01.003 2021-03-10
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 M22 antibody heavy c...
M22 antibody light c...
N-[4-[[5-[(2S)-3-ben... pubchem
AgonistAgonistPAM 2.8 Active 10.1038/S41586-022-05173-3 2022-08-17
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 CCL3 gtoplig
Agonist 2.9 Active 2021-07-14
4PXF OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionsitting drop 3 chems 6.0-6.0 4°C B-Octylglucoside pubchem
unknown 2.8 Active 10.1038/NCOMMS5801 2014-09-17
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 gtoplig pubchem
Agonist 3.0 Intermediate 10.1101/2023.08.29.555158 2023-10-11
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 gtoplig chembl_ligand drugbank drug_central gtoplig pubchem pubchem pubchem pubchem pubchem
Agonist 3.9 Active 10.1126/SCIENCE.AAZ5346 2020-04-01
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)
Apo (no ligand) 2.9 Active 10.1038/S41586-022-04590-8 2022-04-27
8WGB 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 VU0155041 pubchem gtoplig chembl_ligand
Agonist 3.7 Active 10.1038/S41467-024-54744-7 2024-10-30
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 butyric acid pubchem gtoplig chembl_ligand drugbank
Agonist 3.3 Active 10.1016/J.CELREP.2024.115024 2024-12-11
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 C5a
Agonist 3.4 Active HTTPS://DOI.ORG/10.1016/J.CELL.2023.09.020 2023-10-18
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 NDT9513727 pubchem gtoplig chembl_ligand
PMX53 pubchem gtoplig chembl_ligand
NAMAntagonist 2.9 Inactive 10.1038/S41594-018-0067-Z 2018-05-30
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)
Apo (no ligand) 3.1 Active 2022-08-24
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 (3~{S})-3-cyclopropy... pubchem
Allosteric agonist 2.8 Active 10.1038/S41467-017-01240-W 2018-05-02
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
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 pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.2 Active 10.1038/S41589-021-00841-3 2021-08-25
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 neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
Agonist 2.8 Inactive 10.1073/PNAS.1317903111 2014-01-29
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 2019-11-13
8TYW GPR6 GPR6 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.4 Active 10.1126/SCISIGNAL.ADO8741 2024-12-04
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
7WC6 5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Lysergide pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.6 Inactive 10.1126/SCIENCE.ABL8615 2022-01-26
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 Glucagon model
Agonist 3.3 Inactive 10.1038/nature12393 2013-07-24
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 neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
Agonist 4.5 Active 10.1038/S41594-020-00554-6 2021-01-06
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 pubchem
Antagonist 2.2 Inactive 10.1021/acs.jmedchem.9b01787 2020-01-15
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 gtoplig
Agonist 2.5 Active 10.1038/NATURE13288 2014-04-30
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 pubchem
Agonist 3.3 Active 10.1016/J.CELL.2022.09.041 2022-11-09
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
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.1 Active 10.1038/S41586-024-07153-1 2024-03-06
7VV5 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A compound 48/80 pubchem gtoplig
Agonist 2.8 Active 10.1038/S41586-021-04077-Y 2021-12-01
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 drugbank
Agonist 2.8 Active 10.1016/J.CELREP.2024.113893 2024-02-28
6PB1 CRFR2 CRF2 Corticotropin-releasing factor B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Urocortin pubchem
Agonist 2.8 Active 10.1016/J.MOLCEL.2020.01.013 2020-02-12
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 pubchem
Antagonist 3.0 Inactive 10.1038/S41594-018-0180-Z 2019-02-13
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 Lysergide pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.6 Active 10.1038/S41586-024-07403-2 2024-05-15
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 Stromal cell-derived...
(1R)-4-[7-(3-carboxy... pubchem
AgonistAgonist (partial) 3.3 Active 10.1126/SCIADV.ABN8063 2022-07-27
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 [Ac-His<sup>1</sup>]... gtoplig chembl_ligand pubchem
Agonist 2.3 Active 10.1038/S41467-022-34629-3 2022-11-23
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 Apo (no ligand)
Apo (no ligand) 2.9 Active 10.1038/S41467-022-33173-4 2022-09-28
7VDH MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A compound 48/80 pubchem gtoplig
Agonist 2.9 Active 10.1038/S41586-021-04077-Y 2021-12-01
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
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
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
6AK3 PE2R3 EP3 Prostanoid A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A PGE2 pubchem gtoplig chembl_ligand drugbank drug_central gtoplig pubchem
Agonist 2.9 Active 10.1038/S41589-018-0171-8 2018-12-05
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 Apo (no ligand)
Apo (no ligand) 3.0 Active 10.1038/S41586-022-04580-W 2022-04-27
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 7-fluoro-5-methyl-3-... pubchem
Agonist 2.5 Inactive 10.1016/J.CELL.2021.11.001 2021-10-06
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
7CZ5 GHRHR GHRH Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Somatoliberin pubchem
Agonist 2.6 Active 10.1038/S41467-020-18945-0 2020-11-18
6OT0 SMO SMO Frizzled F (Frizzled) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 24,25-Epoxy-choleste... pubchem
Agonist 3.9 Active 10.1038/S41586-019-1286-0 2019-06-12
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 chembl_ligand
Agonist 3.4 Active 10.1038/S41467-023-42764-8 2024-02-07
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 Pramlintide analogue...
Agonist 2.0 Active 10.1038/S41589-023-01393-4 2023-08-02
6W2X GABR2 GABAB2 GABAB C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CGP55845 pubchem
1-Stearoyl-2-oleoyl-... pubchem
Inverse agonistNAM 3.6 Inactive 2020-07-01
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 gtoplig pubchem
Agonist 3.1 Active 10.1016/J.CELREP.2023.113406 2024-04-03
7ZBE OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Retinal (11-cis) pubchem
Inverse agonist 1.8 Inactive 10.1038/S41586-023-05863-6 2023-03-29
6XBJ SMO SMO Frizzled F (Frizzled) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Cholesterol pubchem
Agonist 3.9 Active 2020-09-30
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
7P02 NK1R NK1 Tachykinin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A substance P pubchem gtoplig chembl_ligand gtoplig gtoplig
Agonist 2.9 Active 10.1126/SCIADV.ABK2872 2021-12-15
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
8TF5 GPR6 GPR6 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A oleic acid pubchem gtoplig chembl_ligand drug_central
Inverse agonist 2.1 Active 10.1126/SCISIGNAL.ADO8741 2024-12-04
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
Agonist 3.7 Active 10.7554/ELIFE.76823 2022-07-13
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
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 cinacalcet pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Calcium pubchem
AgonistAgonist 2.7 Inactive 10.1038/S41422-023-00892-2 2023-11-22
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 1-(4-fluorophenyl)-4... pubchem
Agonist 2.7 Inactive 10.1016/J.CELL.2024.02.034 2024-02-28
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 Prolactin-releasing ...
Agonist 3.0 Active 10.1038/S41421-024-00724-6 2024-09-25
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 iperoxo pubchem gtoplig chembl_ligand
LY2119620 pubchem gtoplig chembl_ligand
AgonistPAM 3.4 Active 10.1038/S41467-022-30595-Y 2022-05-11
3DQB OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionhanging drops 5 chems 5.9-6.1 10°C Apo (no ligand)
Apo (no ligand) 3.2 Active 10.1038/NATURE07330 2008-09-23
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 NIT-FC0-NLE-A1D5B
Agonist 2.7 Active 2024-07-03
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
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 CHEMBL552527 chembl_ligand pubchem
Agonist 2.8 Active 10.1038/S41467-020-15009-1 2020-03-25
2J4Y OPSD Rhodopsin Opsins A (Rhodopsin) Bovine Transient_transfectionCOS1Mammalian 1 chemicals 1 steps vapour diffusionsitting drops 3 chems 7.5-7.5 4°C Retinal (11-cis) pubchem
Inverse agonist 3.4 Inactive 10.1016/J.JMB.2007.03.007 2007-09-25
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 3.1 Active 10.1038/S41467-024-46840-5 2024-03-20
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
Antagonist 3.5 Inactive 10.1107/S1600576723006428 2023-08-30
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 [N-(3-{bis[2-(pyridi...
Antagonist 3.3 Intermediate 10.1021/ACS.JMEDCHEM.3C01822 2024-08-07
5CGD GRM5 mGlu5 Metabotropic glutamate C (Glutamate) Human BaculovirusSf21Insect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 4 chems 5.5-6.8 20°C CHEMBL3603923 chembl_ligand pubchem
NAM 2.6 Inactive 10.1021/acs.jmedchem.5b00892 2015-08-12
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 Stromal cell-derived...
Agonist 4.0 Active 10.1126/SCIADV.ABN8063 2022-07-27
7VV6 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A compound 48/80 pubchem gtoplig
Agonist 3.3 Active 10.1038/S41586-021-04077-Y 2021-12-01
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
AgonistPAM 3.7 Active 2013-11-27
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 WB4-24 pubchem gtoplig chembl_ligand
Agonist 3.1 Active 10.1073/PNAS.2200155119 2022-06-29
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 2010-08-11
6P9X CRFR1 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 Corticoliberin pubchem
Agonist 2.9 Active 10.1016/J.MOLCEL.2020.01.012 2020-02-05
4UG2 AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusHi5Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 3 chems 7.0-7.0 22°C CGS 21680 pubchem gtoplig chembl_ligand gtoplig
Agonist 2.6 Active 10.1124/mol.114.097360 2015-04-08
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 5-Methyl-4-oxidanyl-... pubchem
Agonist 2.8 Active 10.1038/S41467-023-42764-8 2024-02-07
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 pubchem
Agonist 3.2 Active 10.1016/J.STR.2021.04.008 2021-01-20
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 drugbank gtoplig pubchem pubchem pubchem
NAM 2.7 Inactive 10.1021/ACS.JMEDCHEM.7B01722 2018-03-07
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...
Agonist 2.7 Active 10.1038/S41421-024-00754-0 2024-11-13
4EJ4 OPRD δ Opioid A (Rhodopsin) Mouse BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 7.5-7.5 20°C naltrindole pubchem gtoplig chembl_ligand gtoplig
Antagonist 3.4 Inactive 10.1038/NATURE11111 2012-05-16
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
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
Agonist 2.6 Active 10.1038/S41422-023-00914-Z 2024-01-24
6DDF OPRM μ Opioid A (Rhodopsin) Mouse BaculovirusSf9Insect 4 chemicals 4 steps Cryo-EMGatan K2 Summit direct electron camera , 300kV 5 chems 7.5-7.5 4°C DAMGO pubchem gtoplig chembl_ligand chembl_ligand
Agonist 3.5 Active 10.1038/S41586-018-0219-7 2018-06-13
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 2010-10-27
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)
Apo (no ligand) 2.6 Active 10.1073/PNAS.2106606118 2022-04-06
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 pubchem gtoplig
Agonist 2.0 Inactive 10.1038/S41467-018-07094-0 2018-11-21
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 pubchem
Agonist 3.0 Active 10.1073/PNAS.1700891114 2017-07-26
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
4BEY OPSD Rhodopsin Opsins 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)
Apo (no ligand) 2.9 Active 10.1038/EMBOR.2013.44 2013-05-08
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 [(2R)-3-[(E)-hexadec... pubchem
Agonist 2.8 Active 2024-10-16
7EZM CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CCK-8 pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 2.9 Active 10.1038/S41589-021-00841-3 2021-08-25
8A6D OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Retinal (11-cis) pubchem
Agonist 1.8 Inactive 10.1038/S41586-023-05863-6 2023-03-29
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
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 pubchem
Agonist 3.4 Active 10.1126/SCIADV.ABJ5347 2022-04-13
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
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
Antagonist 2.5 Inactive 10.1107/S2052252519013137 2019-11-13
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 L-tryptophan pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Calcium pubchem
PAMAgonist 3.5 Active 10.1038/S41422-021-00474-0 2021-03-10
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 gtoplig pubchem
Agonist 3.0 Active 10.1038/S41467-024-52585-Y 2024-10-09
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
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
Agonist 3.5 Active 10.1038/S41467-023-39310-X 2023-07-05
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 chembl_ligand pubchem
Agonist 3.9 Active 10.1038/S41594-021-00679-2 2021-11-17
8P15 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 5.9 Active 2024-11-20
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
Agonist 2.7 Active 10.1038/S41467-021-26735-5 2021-12-15
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 pubchem
Agonist 3.2 Active 10.1038/S41422-023-00808-0 2023-06-21
7T6T FPR1 FPR1 Formylpeptide A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A synthetic peptide
Agonist 3.2 Active 10.1038/S41467-022-28586-0 2022-03-30
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 gtoplig
Agonist 2.9 Active 10.1038/S41467-021-25364-2 2021-08-18
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
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 Insulin-like peptide... pubchem
Insulin-like peptide... pubchem
AgonistAgonist 3.2 Active 10.1038/S41467-023-36182-Z 2023-03-01
6IIU TA2R TP Prostanoid A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ramatroban pubchem gtoplig chembl_ligand drug_central drugbank gtoplig pubchem
Antagonist 2.5 Inactive 10.1038/S41589-018-0170-9 2018-12-19
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
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 BHFF pubchem
PAM 4.5 Active 10.1016/J.JMB.2020.09.023 2020-11-11
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 tiotropium pubchem gtoplig chembl_ligand drugbank gtoplig chembl_ligand chembl_ligand pubchem
Antagonist 2.6 Inactive 10.1038/NATURE17188 2016-03-16
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
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 pubchem
Antagonist 3.4 Inactive 10.1038/S41467-023-39310-X 2023-07-05
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
7TYI CALCR CT Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Amylin rat pubchem
Agonist 3.3 Active 10.1126/SCIENCE.ABM9609 2022-03-30
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
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.6 Active 10.1038/S41586-024-07153-1 2024-03-06
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 gtoplig chembl_ligand drugbank drug_central gtoplig pubchem pubchem pubchem pubchem pubchem
Agonist 3.3 Active 10.1038/S41586-023-06420-X 2023-08-16
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)
Apo (no ligand) 3.1 Active 10.1126/SCIENCE.ABO1633 2022-10-12
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 2019-04-24
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 3.2 Inactive 2012-05-23
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 chembl_ligand
Agonist 3.5 Active 10.1038/S41586-018-0219-7 2018-06-13
4U14 ACM3 M3 Acetylcholine (muscarinic) A (Rhodopsin) Rat BaculovirusSf9Insect 9 chemicals 9 steps sponge mesophaselipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 8.1-8.1 298 K tiotropium pubchem gtoplig chembl_ligand drugbank gtoplig chembl_ligand chembl_ligand pubchem
Antagonist 3.6 Inactive 10.1016/J.STR.2014.08.022 2014-11-26
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 Octaethylene glycol ... pubchem
MK-0893 pubchem gtoplig chembl_ligand drugbank
AntagonistNAM 2.5 Inactive 10.1038/NATURE17414 2016-04-20
8IZ4 GPR34 GPR34 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Lysergide pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.9 Active 2024-04-10
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 pubchem
Agonist 2.5 Active 10.1016/J.MOLCEL.2020.09.020 2020-09-09
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
Inverse agonist 2.4 Inactive 10.1038/S41594-022-00859-8 2022-06-29
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 chembl_ligand pubchem
Agonist 3.3 Active 10.1016/J.MOLCEL.2021.06.024 2022-05-04
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 pubchem
Agonist 3.2 Inactive 10.1038/S41589-023-01389-0 2023-09-06
1GZM OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionsitting drops 3 chems 8.5-8.5 18°C Retinal (11-cis) pubchem
Inverse agonist 2.7 Inactive 10.1016/J.JMB.2004.08.090 2003-11-20
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 pubchem
Agonist 3.5 Active 10.1038/S41467-022-28111-3 2022-03-02
8WMA FZD4 FZD4 Frizzled F (Frizzled) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.5 Active 10.1038/S41467-024-52174-Z 2024-09-11
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.6 Active 10.1038/S41586-024-07153-1 2024-03-06
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 (2S,5R)-5-[(1E,3S)-4... pubchem
Agonist 3.3 Active 10.1073/PNAS.2216329120 2024-01-10
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
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
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
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 Apo (no ligand)
Apo (no ligand) 2.9 Active 10.1016/J.CHEMBIOL.2023.08.003 2023-07-12
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 (3S)-N-[(2S)-5-carba... pubchem
Agonist 3.0 Active 10.1038/S41594-023-01175-5 2023-11-29
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 CP55940 pubchem gtoplig chembl_ligand gtoplig
6-methyl-3-[(1S)-2-n... pubchem
AgonistPAM 2.7 Inactive 10.1038/S41589-022-01038-Y 2022-06-15
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
1L9H OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 6.0-6.0 4°C Retinal (11-cis) pubchem
Inverse agonist 2.6 Inactive 10.1073/PNAS.082666399 2002-05-15
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 pubchem gtoplig drugbank
Agonist 2.9 Active 10.1038/S41421-022-00405-2 2022-08-31
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 N-Tert-butyl-6,7-dic... pubchem
CHEMBL410972 chembl_ligand pubchem pubchem
Ago-PAMAgonist 2.5 Active 10.1038/S41467-021-24058-Z 2021-07-14
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 pubchem gtoplig chembl_ligand gtoplig gtoplig pubchem pubchem pubchem
Agonist 3.2 Active 2024-07-31
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
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
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 Neuromedin U-25 (hum... pubchem
Agonist 2.8 Active 10.1038/S41467-022-29683-W 2022-04-20
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 (1R,2S)-N-[4-(2,6-di... pubchem
Agonist 3.6 Active 10.1038/S41594-022-00797-5 2022-07-27
6FK7 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine BaculovirusHEK293S(TetR)-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 4.5-4.5 20°C (2~{S})-2-(4-chlorop... pubchem
Agonist 2.6 Active 2018-04-04
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 gtoplig
Agonist 3.3 Active 10.1016/J.CELL.2023.09.020 2023-10-18
2I35 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 2 chemicals 2 steps vapour diffusionsitting drops 5 chems 7.0-8.0 5°C Retinal (11-cis) pubchem
Inverse agonist 3.8 Inactive 2006-10-17
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
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
5V56 SMO SMO Frizzled F (Frizzled) Human Transient_transfectionHEK293FMammalian 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 5.0-5.0 20°C N-methyl-N-[1-[4-(2-... pubchem
Antagonist 2.9 Inactive 10.1038/NCOMMS15383 2017-05-24
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 Apo (no ligand)
Apo (no ligand) 2.3 Active 10.1016/J.MOLCEL.2023.12.020 2024-01-24
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 pubchem pubchem
Agonist 2.9 Active 10.1038/S41422-023-00830-2 2023-06-21
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 N-pyridin-4-ylisoqui... pubchem
Agonist 3.5 Active 10.1126/SCIENCE.ABN7065 2022-09-28
8J46 O52E4 OR52E4 Odorant family 52 O1 (fish-like odorant) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.7 Active 10.1038/S41467-023-43983-9 2023-12-20
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 teriparatide pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem pubchem pubchem pubchem pubchem pubchem
Agonist 3.8 Active 10.1016/J.MOLCEL.2022.07.003 2022-08-03
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
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
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 gtoplig pubchem pubchem pubchem drugbank
Agonist 3.0 Active 2023-03-22
6NBH PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Long-acting parathyr...
Agonist 3.5 Active 10.1126/SCIENCE.AAV7942 2019-04-17
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 pubchem
Agonist 3.0 Active 10.1038/S41422-023-00808-0 2023-06-07
4QIN SMO SMO Frizzled 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 pubchem
Agonist 2.6 Inactive 10.1038/NCOMMS5355 2014-07-23
8JGF MRGX1 MRGPRX1 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A bovine adrenal medul... pubchem gtoplig chembl_ligand pubchem
Agonist 2.7 Active 10.1038/S41467-023-40705-Z 2024-01-10
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 chembl_ligand
Agonist 3.5 Active 10.1038/S41467-024-46239-2 2024-03-06
3REY AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusSf9Insect 1 chemicals 1 steps vapour diffusionSitting drop 6 chems 8.0-8.8 4°C xanthine amine conge... pubchem gtoplig chembl_ligand gtoplig
Antagonist 3.3 Inactive 10.1016/J.STR.2011.06.014 2011-09-07
8JGB MRGX1 MRGPRX1 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Conorfamide-Tx2
Agonist 2.8 Active 10.1038/S41467-023-40705-Z 2024-01-10
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
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
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 2-Phenylethanaminium pubchem
Agonist 3.2 Active 10.1016/J.CELL.2023.10.014 2023-12-27
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
7SHF GP158 GPR158 C Orphans C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.4 Inactive 10.1126/SCIENCE.ABL4732 2021-12-01
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 pubchem
Agonist 2.8 Inactive 10.1126/SCIENCE.1232807 2013-03-13
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
7C4S S1PR3 S1P3 Lysophospholipid (S1P) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A sphingosine 1-phosph... pubchem gtoplig chembl_ligand pubchem
Agonist 3.2 Active 10.1126/SCIADV.ABF5325 2021-06-09
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 gtoplig pubchem pubchem
Agonist 3.3 Active 10.1016/J.CELL.2022.12.026 2022-12-14
7BB7 V2R V2 Vasopressin and oxytocin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A vasopressin pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Agonist 4.4 Active 10.1126/SCIADV.ABG5628 2021-06-02
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 pubchem
Antagonist 3.2 Inactive 2024-08-28
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 [Ac-His<sup>1</sup>]... gtoplig chembl_ligand pubchem
Agonist 3.5 Active 10.1038/S41422-020-0280-2 2020-03-11
7VUI GP139 GPR139 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A JNJ-63533054 pubchem gtoplig chembl_ligand
Agonist 3.3 Active 10.1038/S41422-021-00591-W 2021-12-29
8XBI GPR34 GPR34 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL4758243 chembl_ligand pubchem
Agonist 3.1 Active 2023-12-27
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 CHEMBL216166 chembl_ligand pubchem
Agonist 2.6 Active 10.1371/JOURNAL.PBIO.3002673 2024-05-22
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 gtoplig
Antagonist 2.8 Inactive 10.1038/S41422-023-00830-2 2023-06-21
5YC8 ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N-methyl scopolamine pubchem gtoplig drugbank gtoplig chembl_ligand chembl_ligand chembl_ligand pubchem pubchem
Antagonist 2.5 Inactive 10.1038/S41589-018-0152-Y 2018-11-21
5GLH EDNRB ETB Endothelin A (Rhodopsin) Human BaculovirusSF+Insect 6 chemicals 6 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 6.0-6.0 20°C ENDOTHELIN chembl_ligand pubchem
Agonist 2.8 Inactive 10.1038/nature19319 2016-09-07
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
7TYF CALCR CT Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A amylin peptide
Agonist 2.2 Active 10.1126/SCIENCE.ABM9609 2022-03-23
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 teriparatide pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem pubchem pubchem pubchem pubchem pubchem
Agonist 3.3 Active 10.1016/J.MOLCEL.2022.07.003 2022-08-03
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 pubchem gtoplig chembl_ligand gtoplig gtoplig pubchem pubchem pubchem
Agonist 3.2 Active 10.1126/SCIADV.ABM1232 2022-05-18
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
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 pubchem
Antagonist 2.9 Inactive 2023-12-20
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 pubchem
Agonist 2.9 Active 10.1038/S41589-023-01339-W 2023-05-10
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...
Agonist 2.8 Active 10.1038/S41421-024-00754-0 2024-11-13
8WZ2 QRFPR QRFP Peptide P518 A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Orexigenic neuropept...
Agonist 2.7 Active 10.1038/S41421-024-00670-3 2024-06-19
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 (5R)-N-[2-(1,2-benzo... pubchem
PAM 2.8 Inactive 2024-10-02
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 pubchem
Antagonist 3.2 Inactive 10.1107/S2052252519013137 2019-11-13
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 Stromal cell-derived...
Agonist 2.8 Active 2024-07-17
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 (5R,6R)-6-(methylami... pubchem
Agonist 4.0 Active 10.1038/S41586-024-07153-1 2024-03-06
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 neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
Agonist 2.9 Active 10.1038/NCOMMS8895 2015-07-29
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)
Apo (no ligand) 4.0 Intermediate 10.1073/PNAS.2414544121 2024-11-13
7C7Q 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 gtoplig pubchem pubchem
BHFF pubchem
AgonistPAM 3.0 Active 2020-07-01
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
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
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 pubchem
Agonist 3.4 Active 10.1038/S41422-021-00566-X 2021-09-29
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 pubchem
Agonist 2.9 Active 2021-01-20
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
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 chembl_ligand pubchem
Agonist 3.0 Active 2023-03-22
7EPA GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.6 Intermediate 10.1038/S41586-021-03641-W 2021-06-23
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 gtoplig pubchem
Agonist 3.0 Active 10.1038/S41467-023-42260-Z 2023-10-25
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 pubchem
Agonist 3.5 Active 10.1126/SCIADV.ABL5442 2022-01-26
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
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 39YLC3L0ZU pubchem
Agonist 2.9 Active 10.1016/J.CELL.2021.01.027 2021-02-24
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 (2S)-1-[(3-{1-[4-(4-...
Antagonist 3.0 Inactive 2024-07-17
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
3PQR OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drops 3 chems 5.6-5.6 4°C Retinal (all-trans) pubchem
Agonist 2.9 Active 10.1038/NATURE09789 2011-03-09
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 ligand
Agonist 2.9 Active 10.1016/J.CELL.2023.09.020 2023-10-18
8IEI GP156 GPR156 C Orphans C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A [(2R)-3-[(E)-hexadec... pubchem
Agonist 2.6 Inactive 2024-02-14
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
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
4QIM SMO SMO Frizzled F (Frizzled) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 5 chems 7.2-7.2 20°C ANTA XV pubchem gtoplig chembl_ligand
Antagonist 2.6 Inactive 10.1038/NCOMMS5355 2014-07-23
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 pubchem
Agonist 3.0 Active 10.1038/S41467-022-28417-2 2022-02-09
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
1F88 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 2 chemicals 2 steps vapour diffusionHanging drop 7 chems 6.0-6.0 4°C Retinal (11-cis) pubchem
Inverse agonist 2.8 Inactive 10.1126/SCIENCE.289.5480.739 2000-08-04
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 Apo (no ligand)
Apo (no ligand) 2.8 Active 10.1016/J.MOLCEL.2022.10.009 2022-10-26
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 pubchem gtoplig drugbank chembl_ligand gtoplig chembl_ligand chembl_ligand pubchem
Antagonist 2.7 Inactive 10.1126/SCIENCE.1241475 2013-09-11
7Y3G GPR12 GPR12 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 2.8 Active 10.1016/J.SCIB.2022.12.023 2023-06-07
6U1N ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A LY2119620 pubchem gtoplig chembl_ligand
Agonist 4.0 Active 10.1038/S41586-020-1954-0 2020-02-26
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)
Apo (no ligand) 3.5 Inactive 10.1038/S41467-023-44477-4 2024-01-17
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 5-(3-Bicyclo[4.2.0]o... pubchem
Agonist 3.4 Active 10.1126/SCIENCE.ABN7065 2022-09-28
6WIV 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 [(2R)-3-[(Z)-icos-11... pubchem
(2R)-3-{[(S)-(2-amin... pubchem
NAMNAM 3.3 Inactive 10.1038/S41586-020-2452-0 2020-07-01
7MTQ GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A LY341495 pubchem gtoplig chembl_ligand gtoplig
Antagonist 3.7 Inactive 10.1038/S41586-021-03680-3 2021-07-07
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06
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 Parathyroid hormone
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
8J19 GPR84 GPR84 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 6-nonylpyridine-2,4-... pubchem gtoplig chembl_ligand
Agonist 3.2 Active 10.1038/S41467-023-38985-6 2023-06-21
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 Amyloid beta-Peptide... pubchem
Agonist 3.0 Active 10.1038/S41467-022-29361-X 2022-04-13
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
4-[[3,4-Dioxo-2-[[(1... pubchem
AntagonistAllosteric antagonist 3.0 Inactive 2024-09-11
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
Agonist 2.7 Active 10.1038/S41594-022-00727-5 2022-03-09
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 pubchem
Agonist 3.0 Active 10.1038/S41422-021-00566-X 2021-09-29
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)
Apo (no ligand) 4.0 Inactive 10.1038/S41586-019-0881-4 2019-01-23
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
Agonist 3.0 Active 2024-07-10
8JH7 FZD6 FZD6 Frizzled F (Frizzled) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.2 Active 10.1038/S41421-023-00627-Y 2024-01-17
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 neuropeptide Y pubchem gtoplig chembl_ligand gtoplig gtoplig pubchem pubchem pubchem
Agonist 3.3 Active 2024-07-31
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 CHEMBL4576388 chembl_ligand pubchem
JMV431 gtoplig chembl_ligand pubchem
PAMAgonist 3.1 Active 10.1038/S41586-023-06395-9 2023-08-09
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 L-tryptophan pubchem gtoplig chembl_ligand drugbank drug_central pubchem
L-tryptophan pubchem gtoplig chembl_ligand drugbank drug_central pubchem
PAMAgonist 3.5 Active 10.1038/S41586-024-07055-2 2024-02-07
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 pubchem gtoplig
Agonist 2.8 Active 10.1038/S41467-022-28399-1 2022-01-05
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
Antagonist 2.9 Inactive 10.1038/S41467-023-43601-8 2023-12-20
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
Agonist 3.3 Active 10.1038/S41422-022-00646-6 2022-08-31
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
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 pubchem
Agonist 2.9 Active 10.1038/S41586-024-07403-2 2024-05-15
3RZE HRH1 H1 Histamine A (Rhodopsin) Human Pichia PastorisP. pastoris SMD1163Yeast 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 4.5-4.5 20-22°C doxepin pubchem gtoplig chembl_ligand drugbank gtoplig pubchem
Antagonist 3.1 Inactive 10.1038/NATURE10236 2011-06-15
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 Tethered agonist
Agonist 3.2 Active 2024-09-18
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
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
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06
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 pubchem
Agonist 3.3 Active 10.1038/S41594-021-00634-1 2021-08-18
7L0R NTR1 NTS1 Neurotensin A (Rhodopsin) Rat N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
Agonist 4.2 Active 10.1038/S41594-020-00554-6 2021-01-06
6UVA CALRL calcitonin-like Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A adrenomedullin 2/int... gtoplig
Agonist 2.3 Active 10.1021/ACSPTSCI.9B00080 2020-04-01
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
Cholesterol pubchem
Allosteric agonistAgonist 2.7 Active 2024-07-24
5D5B ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 6.5-7.0 20°C Carazolol pubchem
Inverse agonist 3.8 Inactive 2016-01-13
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
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
6UOA GABR2 GABAB2 GABAB C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 6.3 Intermediate 10.1038/S41586-020-2408-4 2020-06-10
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 pubchem gtoplig pubchem
Agonist 3.4 Active 10.1038/S41467-022-30041-Z 2022-05-18
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
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
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 Lymphotactin
Agonist 3.1 Active 10.1073/PNAS.2405732121 2024-12-11
7KH0 V2R V2 Vasopressin and oxytocin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A vasopressin pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Agonist 2.8 Active 10.1038/S41422-021-00483-Z 2021-05-26
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 Peptide agonist fMet... pubchem
Agonist 2.8 Active 10.1038/S41467-022-32822-Y 2022-09-21
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
Agonist 3.3 Active 2024-06-19
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.2 Active 10.1038/S41586-024-07153-1 2024-03-06
8JHI FZD3 FZD3 Frizzled F (Frizzled) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.2 Active 2024-01-17
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 Lysergide pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.7 Intermediate 10.1016/J.NEURON.2022.08.006 2022-09-21
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
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 pubchem
Agonist (partial) 3.1 Inactive 10.1038/NATURE09746 2011-01-12
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 gtoplig pubchem
Agonist 3.1 Active 10.1073/PNAS.2216329120 2024-01-10
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 2020-02-12
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 gtoplig
Antagonist 3.4 Inactive 10.1038/S41422-023-00830-2 2023-06-21
8IWM TAAR9 TAAR9 A orphans 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 2-Phenylethanaminium pubchem
Agonist 3.2 Active 10.1038/S41586-023-06106-4 2023-05-31
5X33 Q9WTK1 BLT1 Leukotriene A (Rhodopsin) Guinea pig Pichia PastorisP. pastoris SMD1163Yeast 4 chemicals 4 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 7 chems 8.5-9.0 4°C BIIL 260 pubchem gtoplig
Antagonist 3.7 Inactive 10.1038/NCHEMBIO.2547 2018-01-03
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
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 Tethered agonist
Agonist 3.0 Active 2024-09-18
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 JNJ-40411813 pubchem gtoplig chembl_ligand drugbank
L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem
PAMAgonist 3.3 Active 10.1038/S41422-023-00830-2 2023-06-21
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 evocalcet pubchem gtoplig drug_central chembl_ligand drugbank pubchem
L-tryptophan pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Calcium pubchem
PAMPAMAgonist 2.5 Active 10.1038/S41586-021-03691-0 2021-06-30
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
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 gtoplig
Agonist 3.1 Active 10.1016/J.CELREP.2024.113893 2024-02-28
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 gtoplig pubchem
Agonist 3.8 Active 10.1016/J.CELREP.2021.109648 2021-09-08
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
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 gtoplig pubchem
VU0424465 pubchem gtoplig chembl_ligand
AgonistPAM 3.2 Active 10.1038/S41467-024-55439-9 2024-11-06
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
Agonist 2.8 Active 10.1038/S41422-024-00984-7 2024-05-29
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 chembl_ligand pubchem
Agonist 3.0 Active 10.1016/J.CELL.2022.12.026 2022-12-14
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
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 pubchem
Agonist 3.5 Active 10.1126/SCIADV.ABO4158 2022-06-15
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
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.6 Active 10.1038/S41586-024-07153-1 2024-03-06
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 gtoplig pubchem
Agonist 3.4 Active 10.1038/S41467-024-46239-2 2024-03-06
3AYM OPSD Rhodopsin Opsins A (Rhodopsin) Japanese flying squid NANativeSquid 1 chemicals 1 steps vapour diffusionsitting drop 5 chems 6.6-6.6 4°C Retinal (all-trans) pubchem
Agonist 2.8 Inactive 10.1016/J.JMB.2011.08.044 2011-08-17
8HS3 GPR20 GPR20 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.1 Active 10.1038/S41421-023-00520-8 2023-03-08
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 C5a gtoplig
Agonist 3.0 Active 10.1038/S41589-023-01339-W 2023-05-10
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
8IWE TAAR9 TAAR9 A orphans 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
Agonist 3.4 Active 10.1038/S41586-023-06106-4 2023-05-31
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)
Apo (no ligand) 4.0 Inactive 10.1038/S41586-021-03641-W 2021-06-23
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 2010-10-27
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
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 FME-TYR-PHE-ILE-ASN-...
Agonist 3.1 Active 10.1038/S41467-022-29361-X 2022-04-13
7PIV MC4R MC4 Melanocortin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A afamelanotide pubchem gtoplig chembl_ligand drugbank pubchem pubchem pubchem pubchem pubchem
Agonist 2.9 Active 10.1038/S41422-021-00569-8 2021-11-17
7V9M GHRHR GHRH Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Somatoliberin pubchem
Agonist 3.3 Active 10.1073/PNAS.2106606118 2021-10-20
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 pubchem gtoplig chembl_ligand gtoplig gtoplig
Agonist 3.2 Active 10.1038/S41589-021-00890-8 2021-11-03
6PGS OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Geraniol pubchem
unknown 2.9 Active 2020-07-01
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 chembl_ligand
Agonist 3.0 Active 10.1038/S41467-024-47792-6 2024-05-29
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.9 Active 10.1038/S41586-024-07153-1 2024-03-06
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
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 chembl_ligand pubchem
Agonist 3.1 Active 10.1038/S41589-021-00866-8 2021-10-13
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
8HQN GP132 GPR132 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 9-hydroxyoctadecadie... pubchem gtoplig chembl_ligand drugbank
Agonist 3.0 Active 10.1038/S42255-023-00899-4 2023-10-11
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 chembl_ligand pubchem
Agonist (partial) 3.3 Inactive 10.1038/S41593-021-00971-W 2021-12-22
8TRD GRM3 mGlu3 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A LY341495 pubchem gtoplig chembl_ligand gtoplig
Antagonist 3.4 Inactive 10.1038/S41467-024-50548-X 2024-07-31
6WWZ CCR6 CCR6 Chemokine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CCL20 gtoplig
Agonist 3.3 Active 10.1038/S41467-020-16820-6 2020-06-24
6NWE OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A B-Octylglucoside pubchem
unknown 2.7 Active 2020-02-12
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
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 pubchem
Agonist 2.8 Active 10.1016/J.CELL.2021.01.027 2021-02-24
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
Agonist 3.2 Active 10.1038/S41422-024-00968-7 2024-05-22
8HIX GPR21 GPR21 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.1 Active 10.1038/S41467-023-35882-W 2023-03-15
3KJ6 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 3 chemicals 3 steps vapour diffusionbicelles 5 chems 7.5-7.5 298K Carazolol pubchem
Inverse agonist 3.4 Inactive 10.1038/NATURE08650 2010-02-16
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
Antagonist 2.0 Inactive 10.1016/j.str.2017.06.012 2017-07-26
7EW3 S1PR3 S1P3 Lysophospholipid (S1P) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Sphingosine 1-phosph... pubchem
Agonist 3.1 Active 10.1038/S41422-021-00567-W 2021-09-29
6QNO OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Retinal (all-trans) pubchem
Agonist 4.4 Active 10.7554/ELIFE.46041 2019-07-10
7CA5 GABR2 GABAB2 GABAB C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 7.6 Inactive 10.1016/J.JMB.2020.09.023 2020-11-11
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
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.8 Active 10.1038/S41586-024-07153-1 2024-03-06
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 pubchem
Antagonist 2.2 Inactive 10.1038/S41467-018-07939-8 2019-01-16
6Z66 NTR1 NTS1 Neurotensin A (Rhodopsin) Rat N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.2 Intermediate 10.1126/sciadv.abe5504 2021-02-10
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 3.0 Active 10.1126/SCIADV.ADD3709 2023-05-03
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
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 [Pyr<sup>1</sup>]ape... gtoplig pubchem
Agonist 3.2 Active 10.1016/J.CELL.2024.02.004 2024-03-27
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
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 pubchem
Agonist (partial) 3.1 Active 10.1038/S41586-021-03376-8 2021-04-14
6FK8 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine BaculovirusHEK293S(TetR)-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 4.5-4.5 20°C (2~{R},3~{S})-3-azan... pubchem
Agonist 2.9 Active 10.1073/PNAS.1718084115 2018-04-04
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
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)
Apo (no ligand) 3.3 Active 10.1126/SCIADV.ADJ7500 2024-02-07
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 pubchem
NAM 2.6 Inactive 10.1038/NATURE13396 2014-07-02
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
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)
Apo (no ligand) 3.0 Active 2023-07-12
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.9 Active 10.1038/S41586-024-07153-1 2024-03-06
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 pubchem
Agonist 3.0 Active 10.1038/S41422-022-00641-X 2022-06-15
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 N-Tert-butyl-6,7-dic... pubchem
Ago-PAM 3.3 Active 10.1038/S41467-021-24058-Z 2021-08-11
8TR0 GRM3 mGlu3 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A LY341495 pubchem gtoplig chembl_ligand gtoplig
Antagonist 3.2 Inactive 10.1101/2023.08.13.552748 2024-07-31
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 pubchem
Agonist 3.2 Active 10.1038/S41421-022-00503-1 2023-01-18
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 chembl_ligand chembl_ligand chembl_ligand pubchem drugbank drugbank pubchem
Agonist 2.7 Active 10.1038/S41586-020-2419-1 2019-01-09
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 5-Amino-N-(1,1-dimet... pubchem
Glycoprotein alpha gtoplig
Choriogonadotropin b... gtoplig
Allosteric agonistAgonistAgonist 3.2 Active 10.1038/S41586-021-03924-2 2021-09-29
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 pubchem
Agonist 3.2 Active 2022-08-31
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)
Apo (no ligand) 3.2 Active 10.1038/NATURE23448 2017-08-16
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
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 pubchem
Agonist (partial) 2.9 Inactive 10.1038/S41593-021-00971-W 2021-12-22
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
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 CHEMBL2046866 chembl_ligand pubchem
Antagonist 3.0 Inactive 10.1038/S41586-018-0046-X 2018-04-25
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
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
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)
Apo (no ligand) 2.9 Active 10.1038/S41421-024-00649-0 2024-03-06
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 3.0 Active 10.1073/PNAS.2219569120 2023-05-24
7E9H GRM4 mGlu4 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A L-serine-O-phosphate pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Agonist 4.0 Intermediate 10.1038/S41586-021-03495-2 2021-06-23
7KI0 GLP1R GLP-1 Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A semaglutide pubchem gtoplig chembl_ligand drugbank pubchem chembl_ligand pubchem
Agonist 2.5 Active 10.1016/J.CELREP.2021.109374 2021-08-04
4ZWJ OPSD Rhodopsin Opsins 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)
Apo (no ligand) 3.3 Active 10.1038/NATURE14656 2015-07-29
8YRG MRGX4 MRGPRX4 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Fospropofol pubchem
Agonist 3.1 Active 2024-05-22
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 chembl_ligand pubchem
Agonist 3.3 Active 10.1038/S41421-024-00705-9 2024-08-28
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 pubchem
Agonist 2.6 Active 10.1107/S0907444909042073 2023-09-20
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
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 pubchem
Agonist 3.3 Active 10.1038/S41467-022-30929-W 2022-06-15
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 CXC12
Agonist 3.3 Active 10.1038/S41594-024-01397-1 2024-03-13
5YHL PE2R4 EP4 Prostanoid A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ONO-AE3-208-Br pubchem
Antagonist 4.2 Inactive 10.1038/S41589-018-0131-3 2018-12-05
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
Agonist 2.7 Active 10.1038/S41422-020-00424-2 2020-12-02
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 pubchem pubchem
Antagonist 2.8 Inactive 10.1038/S41594-022-00859-8 2022-06-29
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 Stromal cell-derived...
Agonist 4.0 Active 10.1126/SCIADV.ABN8063 2022-07-27
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 CX3CL1
Agonist 3.4 Active 2022-07-13
8J18 GPR84 GPR84 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (3R)-3-HYDROXYDODECA... pubchem
Agonist 2.9 Active 10.1038/S41467-023-38985-6 2023-06-21
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 pubchem
Agonist 2.8 Inactive 10.1038/S41586-019-1141-3 2019-04-24
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 pubchem gtoplig chembl_ligand
Agonist 3.3 Active 10.1016/J.CELL.2022.12.026 2022-12-14
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
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
7TYX CALCR CT Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Amylin rat pubchem
Agonist 2.6 Active 10.1126/SCIENCE.ABM9609 2022-03-30
8YZK GPC5D GPRC5D C Orphans C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.4 Inactive 10.1038/S41467-024-49625-Y 2024-07-03
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 Bombesin
Agonist 2.9 Active 10.1016/J.CELREP.2024.114511 2024-09-11
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
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 methyl (2R,3S)-3-[(m... pubchem
Agonist 3.2 Active 10.1038/S41467-022-30601-3 2022-05-25
7EVW FZD7 FZD7 Frizzled F (Frizzled) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.2 Active 10.1038/S41422-021-00525-6 2021-08-04
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
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 fulvestrant pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.2 Active 10.1038/S41422-024-00963-Y 2024-04-10
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 pubchem
Agonist 3.3 Active 10.1038/S41467-022-28111-3 2022-03-02
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 pubchem
Antagonist 2.5 Active 10.1126/SCIADV.AAX2518 2019-10-30
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 teriparatide pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem pubchem pubchem pubchem pubchem pubchem
Agonist 2.8 Active 10.1016/J.MOLCEL.2022.07.003 2022-08-03
7BW0 GPBAR GPBA Bile acid A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 3.9 Active 10.1038/S41392-020-00262-Z 2020-09-02
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
8PM2 TAA7F TAAR7F A orphans 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
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 CHEMBL216166 chembl_ligand pubchem
Agonist 3.1 Active 10.1038/S41421-022-00420-3 2023-12-06
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
5G53 AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusTni PRO (Trichoplusia ni) cell linesInsect 1 chemicals 1 steps vapour diffusionSitting drop 6 chems 5.7-5.7 4°C NECA pubchem gtoplig chembl_ligand gtoplig
Agonist 3.4 Active 10.1038/NATURE18966 2016-08-03
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
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 pubchem
Antagonist 3.0 Inactive 10.1021/acs.jmedchem.9b01787 2020-01-01
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)
Apo (no ligand) 3.4 Active 10.1016/J.CELREP.2022.111323 2022-08-17
8WVW LGR4 LGR4 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.5 Inactive 2024-10-30
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
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
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 N/A N/A 3.1 Active 10.1038/S41422-024-00963-Y 2024-04-10
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 neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
Agonist 2.9 Active 10.1021/ACS.BIOCHEM.3C00029 2023-03-29
3V2Y S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 7.8-7.8 20°C W146 pubchem gtoplig chembl_ligand
Antagonist 2.8 Inactive 2012-02-15
5ZBQ NPY1R Y1 Neuropeptide Y A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 4 chems 7.4-8.0 19–22 °C CHEMBL3747822 chembl_ligand chembl_ligand chembl_ligand pubchem
Antagonist 2.7 Inactive 10.1038/S41586-018-0046-X 2018-04-25
7DD6 CASR CaS Calcium-sensing C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A L-tryptophan pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Calcium pubchem
PAMAgonist 3.2 Active 10.1126/SCIADV.ABG1483 2021-06-16
5UNH AGTR2 AT2 Angiotensin A (Rhodopsin) Human BaculovirusSf21Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 7 chems 8.0-8.0 20°C compound 2 [PMID: 28... pubchem gtoplig
Antagonist 2.9 Active 10.1038/NATURE22035 2017-04-05
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 CHEMBL410972 chembl_ligand pubchem pubchem
Agonist 4.1 Active 10.1038/NATURE22394 2017-05-24
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 pubchem gtoplig chembl_ligand pubchem pubchem
Agonist 2.8 Active 10.1038/S41586-023-06804-Z 2023-11-15
8ZH8 QRFPR QRFP Peptide P518 A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A QRF-amide
Agonist 3.2 Active 10.1038/S41467-024-49030-5 2024-07-03
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 pubchem gtoplig chembl_ligand gtoplig pubchem pubchem pubchem pubchem
Agonist 2.7 Active 10.1038/S41467-022-29072-3 2022-04-20
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 gtoplig
Agonist 2.9 Active 2023-06-07
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 ALA-SER-LYS-LEU-GLY-...
Agonist 2.9 Active 2023-05-24
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 2020-02-12
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 Envelope glycoprotei...
Antagonist 3.9 Inactive 10.1038/S41586-018-0804-9 2018-12-12
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
8DWH MRGX1 MRGPRX1 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A compound 16 [PMID: 3... pubchem gtoplig chembl_ligand
Agonist 3.3 Active 10.1038/S41589-022-01173-6 2022-11-02
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 pubchem
Agonist 3.2 Active 10.1038/S41467-024-47207-6 2024-04-24
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 (1R,2R,4S,5S,7s)-7-(... pubchem
Antagonist 3.1 Inactive 10.1073/PNAS.1813988115 2018-11-28
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 pubchem
Agonist 2.6 Active 10.1126/SCIADV.ADK5184 2024-03-06
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 gtoplig
Agonist 2.8 Active 10.1038/S41467-023-37112-9 2023-05-10
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
Agonist 3.3 Active 10.1038/S41422-023-00914-Z 2024-01-24
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 chembl_ligand pubchem
Agonist 3.6 Active 10.1038/S42003-024-06905-Z 2024-10-02
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
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
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)
Apo (no ligand) 2.7 Active 10.1038/S41594-024-01397-1 2024-03-13
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
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
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
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 gtoplig
Agonist 3.3 Active 10.1021/JACS.1C06847 2021-11-24
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
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
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 pubchem
Agonist 3.2 Active 10.1016/J.CELL.2022.09.041 2022-11-09
7EPB GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A eglumegad pubchem gtoplig chembl_ligand gtoplig
Agonist 3.1 Active 10.1038/S41586-021-03641-W 2021-06-23
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 pubchem gtoplig chembl_ligand gtoplig gtoplig pubchem pubchem pubchem
Agonist 3.1 Active 10.1016/J.STR.2022.11.010 2023-03-22
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 neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
Agonist 4.1 Active 10.1038/S41594-020-00554-6 2021-01-06
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 Pramlintide analogue...
Agonist 2.2 Active 10.1038/S41589-023-01393-4 2023-08-02
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 1-[(4-Fluorophenyl)m... pubchem
Inverse agonist 3.6 Inactive 2024-08-28
6PH7 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Nerol pubchem
unknown 2.9 Active 2020-07-01
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 AT118-H Nanobody
Antagonist 3.0 Inactive 10.1038/S41589-024-01620-6 2024-05-22
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 s... pubchem chembl_ligand pubchem pubchem
Agonist 4.1 Active 10.1038/NATURE22327 2017-05-03
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
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 Prolactin-releasing ...
Agonist 3.0 Active 10.1038/S41421-024-00724-6 2024-09-25
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 (4R)-N-[2,5-bis(chlo... pubchem
pentanoic acid pubchem gtoplig chembl_ligand drugbank
PAMAgonist 3.2 Active 10.1038/S41422-023-00914-Z 2024-01-24
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 chembl_ligand pubchem
Agonist 3.2 Active 10.1038/S41586-023-06804-Z 2023-11-15
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 pubchem
Agonist 2.8 Active 10.1038/S41594-022-00796-6 2022-07-20
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 SAR1-AngII
Agonist 2.9 Active 2023-03-29
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 chembl_ligand pubchem
Agonist 3.0 Active 10.1038/S41594-021-00679-2 2021-11-17
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 4-carbamoyl-N-[(2R)-... pubchem
Carazolol pubchem
Allosteric antagonistAntagonist 2.7 Inactive 10.1038/NATURE23652 2017-08-16
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 drugbank chembl_ligand pubchem
Agonist 3.0 Active 10.1016/J.CELL.2023.10.014 2023-12-27
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 pubchem
Agonist 3.5 Active 10.1038/S41586-020-2492-5 2020-09-02
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 lysophosphatidic aci... pubchem
Agonist 3.1 Active 10.1038/S41467-022-28417-2 2022-02-09
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 heavy c...
Agonist 3.4 Active 10.1038/S41594-024-01397-1 2024-03-13
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 (5R,6R)-6-(methylami... pubchem
Agonist 2.9 Active 10.1038/S41586-024-07153-1 2024-03-06
5DHG OPRX NOP Opioid A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 6.4-6.4 20°C CHEMBL1783826 chembl_ligand pubchem
Antagonist 3.0 Inactive 10.1016/J.STR.2015.07.024 2015-10-21
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
Agonist 3.1 Active 10.1038/S41422-021-00552-3 2021-11-03
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 [1-Myristoyl-glycero... pubchem
Agonist 3.4 Active 10.1038/S41467-023-38083-7 2023-05-10
7Y15 MRGRD MRGPRD A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 2.9 Active 10.1038/S42003-022-03668-3 2022-07-20
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.6 Active 10.1038/S41586-024-07153-1 2024-03-06
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
Agonist 3.0 Active 10.1038/S41421-023-00564-W 2024-02-28
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 L-AP4 pubchem gtoplig chembl_ligand gtoplig pubchem
Agonist 4.5 Active 2024-11-27
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
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
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 pubchem
Agonist 3.2 Active 10.1038/S41467-024-46840-5 2024-03-20
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
Agonist 2.4 Active 10.1038/S41589-022-01084-6 2022-08-10
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
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 HYOSCYAMINE chembl_ligand pubchem
muscarinic toxin 7 gtoplig
AntagonistNAM 2.6 Inactive 10.1126/SCIENCE.AAX2517 2020-07-08
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 gtoplig pubchem
Agonist 3.4 Active 10.1038/S41467-024-55439-9 2024-11-06
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
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 Apo (no ligand)
Apo (no ligand) 2.7 Active 10.1038/S41421-024-00649-0 2024-03-06
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 pubchem
Agonist 4.2 Active 10.1126/SCIADV.ABO4158 2022-06-15
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 pubchem gtoplig pubchem
Agonist 2.9 Active 10.1107/S0907444909042073 2023-09-20
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
7S8L MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Cortistatin 14 pubchem
Agonist 2.5 Active 10.1038/S41586-021-04126-6 2021-11-17
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 gtoplig
Antagonist 1.8 Inactive 10.1038/NATURE12944 2013-12-25
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 pubchem
Antagonist 2.3 Inactive 10.1021/acs.jmedchem.9b01787 2020-01-01
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 heavy c...
Agonist 3.4 Inactive 2024-03-13
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
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
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
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
8HTI O52E4 OR52E4 Odorant family 52 O1 (fish-like odorant) 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
Agonist 3.0 Active 10.1038/S41467-023-43983-9 2023-12-20
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 heavy c...
Agonist 3.4 Active 10.1038/S41594-024-01397-1 2024-03-13
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)
Apo (no ligand) 2.8 Active 10.1038/S41586-022-04580-W 2022-04-27
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 gtoplig
Agonist 2.6 Active 10.1038/NATURE10136 2011-05-18
2Y02 ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 1 chemicals 1 steps vapour diffusionsitting drops 6 chems 9.0-9.0 4°C CARMOTEROL chembl_ligand pubchem pubchem
Agonist 2.6 Inactive 2011-01-12
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
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 cinacalcet pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Calcium pubchem
AgonistAgonist 3.1 Active 10.1038/S41422-023-00892-2 2023-11-22
8IEB GP156 GPR156 C Orphans C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A [(2R)-3-[(E)-hexadec... pubchem
Agonist 3.0 Inactive 2024-02-14
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 Peptide YY
Agonist 3.0 Active 10.1016/J.STR.2022.11.010 2023-03-22
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 [(2~{R})-2-[5-(2-hex... pubchem
Agonist 3.3 Active 10.1038/S41467-022-33121-2 2022-10-05
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
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 Cyclomethyltryptopha... pubchem
tecalcet pubchem gtoplig chembl_ligand
AgonistPAM 3.6 Active 10.1038/S41586-024-07331-1 2024-04-17
8IW4 TAAR9 TAAR9 A orphans 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
Agonist 3.5 Active 10.1038/S41586-023-06106-4 2023-05-31
6AKY CCR5 CCR5 Chemokine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CCR5 antagonist 34 pubchem gtoplig chembl_ligand
Antagonist 2.8 Inactive 10.1021/acs.jmedchem.8b01077 2018-10-24
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
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 (5R,6R)-6-(methylami... pubchem
Agonist 4.1 Active 10.1038/S41586-024-07153-1 2024-03-06
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 Apelin receptor earl...
Agonist 4.2 Active 10.1038/S41594-022-00797-5 2022-07-27
6UUS CALRL calcitonin-like Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Adrenomedullin pubchem
Agonist 2.4 Active 10.1021/ACSPTSCI.9B00080 2020-04-01
6FUF OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Retinal (all-trans) pubchem
Agonist 3.1 Active 10.1126/SCIADV.AAT7052 2018-10-03
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
Ago-PAMAgonist 3.6 Active 10.1126/SCIENCE.AAW5188 2019-05-08
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 pubchem
Agonist 3.0 Active 10.1016/J.CELL.2021.01.027 2021-02-24
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 pubchem gtoplig chembl_ligand
Agonist 2.8 Active 2024-02-07
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 BQ3020
Agonist 3.0 Active 10.1038/S41421-024-00705-9 2024-08-28
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 (2S,3R)-3-Cyclopropy... pubchem
MK-8666 chembl_ligand pubchem
PAMAgonist 3.2 Active 10.1038/NSMB.3417 2017-06-07
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
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
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 pubchem gtoplig chembl_ligand pubchem pubchem
Agonist 3.2 Active 10.1016/J.CELL.2021.01.028 2021-03-03
8X2K GPR3 GPR3 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N-oleoylethanolamide pubchem gtoplig chembl_ligand
Agonist 3.0 Active 10.1038/S41422-023-00919-8 2024-04-03
4O9R SMO SMO Frizzled 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
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
9EPQ B1B1U5 Rhodopsin Opsins A (Rhodopsin) Hasarius adansoni N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 11,20-Ethanoretinal pubchem
Agonist 4.2 Active 2024-10-23
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
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 chembl_ligand pubchem
Agonist 2.9 Inactive 10.1038/NATURE09746 2011-01-12
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
Agonist 3.5 Inactive 10.1101/2023.08.29.555158 2023-10-11
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
Antagonist 2.4 Inactive 10.1038/S42004-023-01014-0 2023-10-25
4DJH OPRK κ Opioid A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 6.0-6.0 20°C JDTic pubchem gtoplig chembl_ligand
Antagonist 2.9 Inactive 10.1038/NATURE10939 2012-03-21
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 pubchem
Antagonist 2.7 Inactive 10.1021/acs.jmedchem.9b01787 2020-01-01
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
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)
Apo (no ligand) 3.0 Active 10.1126/SCIENCE.ABO1633 2022-10-12
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 [(2~{R})-1-hexadecan...
PAM 2.3 Active 2024-12-04
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 SALVINORIN B METHOXY... chembl_ligand pubchem
Agonist 2.7 Active 10.1038/S41586-023-06030-7 2023-05-03
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
9IMA GPC5D GPRC5D C Orphans C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Talquetamab Fab ligh...
Talquetamab Fab heav...
AntagonistAntagonist 2.7 Inactive 10.1016/J.JMB.2024.168748 2024-09-11
5F8U ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 1 chemicals 1 steps vapour diffusionHanging drops 1 chems 3.6-4.0 18°C (S)-Cyanopindolol pubchem
Antagonist 3.4 Inactive 10.1038/NSMB.3130 2015-12-23
8UYQ OR4D5 OR4D5 Odorant family 4 O2 (tetrapod specific odorant) 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-methyl-1,3-th... pubchem
Agonist 3.5 Active 10.1038/S41586-024-08126-0 2024-10-30
8HJ0 GPR21 GPR21 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.1 Active 10.1038/S41467-023-35882-W 2023-03-15
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 N-methyl scopolamine pubchem gtoplig drugbank gtoplig chembl_ligand chembl_ligand chembl_ligand pubchem pubchem
Antagonist 3.7 Inactive 10.1016/J.STR.2014.08.022 2014-11-26
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 gtoplig
Agonist 2.6 Active 10.1124/mol.114.097360 2015-04-08
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.6 Active 10.1038/S41586-024-07153-1 2024-03-06
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 pubchem
Agonist 3.1 Active 2021-11-03
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
Agonist 3.3 Active 10.1038/S41586-024-07569-9 2024-07-10
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 INT-777 pubchem
INT-777 pubchem
PAMAgonist 3.0 Active 10.1038/S41586-020-2569-1 2020-09-09
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)
Apo (no ligand) 3.0 Active 10.1038/S41422-024-01046-8 2025-01-01
6WHC GLR glucagon Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Dual-agonist peptide...
Agonist 3.4 Active 10.1074/JBC.RA120.013793 2020-05-27
7VDL MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Cortistatin 14 pubchem
Agonist 3.2 Active 10.1038/S41586-021-04077-Y 2021-12-01
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 gtoplig pubchem
Agonist 2.7 Active 10.1038/S41467-024-52585-Y 2024-10-09
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 Q27453560 pubchem
Agonist 3.3 Active 10.1073/PNAS.1410415111 2014-07-23
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
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 gtoplig pubchem
Agonist 2.3 Active 10.1038/S41467-024-52585-Y 2024-10-09
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
Agonist 2.8 Active 10.1073/PNAS.2303696120 2023-09-13
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
7PYR AA2AR A2A Adenosine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Preladenant conjugat...
Antagonist 2.6 Inactive 10.1002/ANIE.202115545 2022-03-02
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 quisqualate pubchem gtoplig chembl_ligand drugbank gtoplig pubchem
VU0424465 pubchem gtoplig chembl_ligand
AgonistPAM 3.1 Active 10.1038/S41467-024-55439-9 2024-11-06
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 chembl_ligand drugbank pubchem
Antagonist 2.8 Active 10.1016/j.bcp.2022.115291 2022-11-02
1HZX OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 2 chemicals 2 steps vapour diffusionHanging drops 7 chems 6.0-6.0 4°C Retinal (11-cis) pubchem
Inverse agonist 2.8 Inactive 10.1021/BI0155091 2001-07-04
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
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 pubchem
Agonist 3.3 Active 10.1038/S41586-021-03897-2 2021-09-08
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 CHEMBL48981 chembl_ligand pubchem
Agonist 4.9 Active 10.1038/S41422-019-0256-2 2019-12-04
7DD7 CASR CaS Calcium-sensing C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Calcium pubchem
evocalcet pubchem gtoplig drug_central chembl_ligand drugbank pubchem
L-tryptophan pubchem gtoplig chembl_ligand drugbank drug_central pubchem
AgonistPAMPAM 3.2 Active 10.1126/SCIADV.ABG1483 2021-06-16
8K4P Q76SF8 ORF74 Unclassified A (Rhodopsin) HHV-8 N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 2.8 Active 2024-07-24
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 Stromal cell-derived...
Agonist 3.3 Active 10.1126/SCIADV.ABN8063 2022-07-27
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 gtoplig pubchem
Agonist 3.0 Active 2023-12-20
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 pubchem gtoplig chembl_ligand pubchem pubchem
Agonist 3.2 Active 10.1038/S41467-022-30929-W 2022-06-29
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
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
7E2X 5HT1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.0 Active 10.1038/S41586-021-03376-8 2021-04-14
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 MEDI0382
Agonist 2.9 Active 10.1073/PNAS.2303696120 2023-09-06
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 gtoplig
Antagonist 2.9 Inactive 10.1038/S41422-023-00830-2 2023-06-21
7EWL GP158 GPR158 C Orphans C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.5 Inactive 10.1038/S41467-021-27147-1 2021-12-01
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 Apo (no ligand)
Apo (no ligand) 3.0 Active 10.1016/J.MOLCEL.2022.10.009 2022-10-26
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 pubchem
Agonist 3.1 Active 10.1016/J.STR.2023.04.002 2023-04-26
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
Agonist 2.8 Active 2024-06-19
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
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 EP141 peptide agonis...
Agonist 3.1 Active 10.1016/J.CELL.2023.09.020 2023-10-18
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
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
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
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 FSHR agonist 1 pubchem
Follitropin subunit ...
Glycoprotein alpha
Allosteric agonistAgonistAgonist 2.8 Active 10.1038/S41467-023-36170-3 2023-03-29
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
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 Lysergide pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.3 Active 10.1016/J.NEURON.2022.08.006 2022-09-21
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
Antagonist 2.9 Inactive 10.1107/S2052252519013137 2019-11-13
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
Agonist 3.0 Active 10.1016/J.CELL.2023.10.014 2023-12-27
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.0 Active 10.1038/S41586-024-07153-1 2024-03-06
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
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
Agonist 2.8 Active 10.1126/SCIENCE.ADD6220 2023-03-15
8KH5 GP174 GPR174 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Lysophosphotidylseri... pubchem
Agonist 2.8 Active 10.1038/S41467-023-41654-3 2023-10-18
7KNT CALRL calcitonin-like Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.2 Inactive 10.1126/SCIENCE.ABF7258 2021-02-24
8CXO SMO SMO Frizzled 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
Agonist 3.7 Inactive 10.1038/S41467-022-32125-2 2022-08-03
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
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
Agonist 3.2 Active 10.1038/S41589-022-01208-Y 2022-12-07
7M8W PD2R2 DP2 Prostanoid A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 15(<i>R</i>)-15-meth... pubchem gtoplig
Antagonist 2.6 Inactive 10.1073/PNAS.2102813118 2021-08-25
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
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 ZM-241385 pubchem gtoplig chembl_ligand drugbank
Antagonist 3.1 Inactive 10.1038/NATURE10750 2012-02-01
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
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 Apo (no ligand)
Apo (no ligand) 2.9 Active 10.1016/J.MOLCEL.2022.10.009 2022-11-09
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 drugbank chembl_ligand pubchem
Agonist 3.7 Active 10.1038/S41586-023-06804-Z 2023-11-15
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 6-[3-[2-(2-methoxyph... pubchem
(2r)-1-(Heptadecanoy... pubchem
AgonistPAM 2.4 Active 2024-05-29
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
6PB0 CRFR1 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 Urocortin pubchem
Agonist 3.0 Active 10.1016/J.MOLCEL.2020.01.013 2020-02-12
8XBE GPR34 GPR34 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL4782438 chembl_ligand pubchem
Agonist 3.4 Active 10.1038/S41467-024-45046-Z 2024-05-15
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 pubchem
Agonist 3.2 Active 10.1016/J.CELL.2022.09.041 2022-11-09
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 N-[4-[[5-[(2S)-3-ben... pubchem
Thyrotropin subunit ...
Glycoprotein hormone...
PAMAgonistAgonist 3.0 Active 10.1038/S41586-022-05173-3 2022-08-24
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
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
Antagonist 3.0 Inactive 10.1021/acs.jmedchem.9b01787 2020-01-01
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 3-[3-[2-[[(2~{S})-2-... pubchem
Agonist 3.9 Active 10.1016/J.BBRC.2022.04.065 2022-05-04
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 ACY-DTY-HYP-ASN-THR-...
Agonist 3.1 Active 2024-07-03
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
Apo (no ligand) 3.4 Active 2024-09-25
7VUH GP139 GPR139 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A JNJ-63533054 pubchem gtoplig chembl_ligand
Agonist 3.2 Active 2021-12-29
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
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 pubchem
Agonist 3.3 Active 10.1038/S41467-024-50964-Z 2024-08-21
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 neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
Agonist 2.6 Active 10.1021/ACS.BIOCHEM.3C00029 2023-03-29
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 pubchem
Agonist 3.2 Active 10.1038/S41467-024-50964-Z 2024-08-21
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 3-[(1S)-1-(furan-2-y... pubchem
Agonist 3.4 Active 10.1073/PNAS.2321532121 2024-06-05
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
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 gtoplig chembl_ligand pubchem
Calcium pubchem
AntagonistCofactor 2.8 Intermediate 10.1126/SCIENCE.AAZ8995 2020-04-29
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
Antagonist 3.5 Inactive 10.1073/PNAS.2002704117 2020-07-15
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
6FKA OPSD Rhodopsin Opsins A (Rhodopsin) Bovine BaculovirusHEK293S(TetR)-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 4.5-4.5 20°C (2~{S})-2-(3,4-dichl... pubchem
Agonist 2.7 Active 10.1073/PNAS.1718084115 2018-04-04
5WB1 Q80KM9 US28 Unclassified A (Rhodopsin) strain AD169 BaculovirusHEK293S(TetR)-GnTI-Mammalian 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 6.0-6.0 16-20°C Apo (no ligand)
Apo (no ligand) 3.5 Active 10.7554/ELIFE.35850 2018-06-13
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 pubchem
Agonist 2.5 Active 10.1038/S41467-023-41199-5 2023-09-13
8W8Q GP101 GPR101 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 2.9 Active 10.1038/S41589-023-01456-6 2024-01-03
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 INTERMEDINE chembl_ligand pubchem pubchem pubchem
Agonist 2.7 Active 10.1107/S0907444909042073 2023-09-20
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 pubchem gtoplig chembl_ligand gtoplig gtoplig
Agonist 2.5 Active 10.1038/S41592-023-02082-9 2023-11-15
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
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 gtoplig pubchem
VU0424465 pubchem gtoplig chembl_ligand
AgonistPAM 3.5 Active 10.1038/S41467-024-55439-9 2024-11-06
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.2 Active 10.1038/S41586-024-07153-1 2024-03-06
2I36 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 2 chemicals 2 steps vapour diffusionsitting drops 5 chems 7.0-8.0 5°C Apo (no ligand)
Apo (no ligand) 4.1 Inactive 2006-10-17
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)
Apo (no ligand) 4.0 Inactive 10.1007/S13238-020-00808-5 2021-09-22
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 lysophosphatidic aci... pubchem
Agonist 2.8 Active 10.1038/S41467-022-28417-2 2022-02-09
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
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
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 LPI
Agonist 2.9 Active 2024-11-13
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 Apo (no ligand)
Apo (no ligand) 3.3 Active 10.1038/S41586-022-04619-Y 2022-05-11
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 pubchem
Agonist 3.6 Active 10.1126/SCIADV.ABO4158 2022-06-15
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 synthetic peptide
Agonist 2.9 Active 10.1038/S41467-022-29361-X 2022-04-13
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
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 gtoplig
Agonist 3.0 Active 2023-06-07
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 3.2 Active 10.1016/J.CELL.2022.09.041 2022-11-09
8ZQE GPR15 GPR15 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A GPR15LG
Agonist 2.9 Active 10.1038/S41421-024-00698-5 2024-07-10
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
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 pubchem gtoplig chembl_ligand drug_central drugbank pubchem pubchem pubchem
Agonist 2.9 Active 10.1126/SCIENCE.AAY9813 2020-02-19
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
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 MEDI0382
Agonist 2.9 Active 10.1073/PNAS.2303696120 2023-09-06
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
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 (2~{S})-4-fluoranyl-... pubchem
Agonist (partial) 3.2 Inactive 2019-12-04
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
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 (2S)-N-[(4S)-6-amino... pubchem
Agonist 2.7 Active 2024-07-03
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 Stromal cell-derived...
(1R)-4-[7-(3-carboxy... pubchem
AgonistAgonist (partial) 3.3 Active 10.1126/SCIADV.ABN8063 2022-07-27
7F16 PTH2R PTH2 Parathyroid hormone B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A TIP39 gtoplig
Agonist 2.8 Active 10.1073/PNAS.2101279118 2021-08-18
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 β-endorphin pubchem gtoplig chembl_ligand pubchem
Agonist 3.2 Active 10.1016/J.CELL.2022.12.026 2022-12-14
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 exendin-4 pubchem gtoplig pubchem
Agonist 2.4 Active 10.1038/S41589-021-00945-W 2022-01-05
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
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
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 s... pubchem chembl_ligand pubchem pubchem
Agonist 3.0 Active 10.1126/SCIENCE.ABM9609 2022-03-23
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 gtoplig pubchem pubchem
BHFF pubchem
AgonistPAM 3.5 Active 10.1038/S41586-021-03507-1 2021-05-05
7SHE GP158 GPR158 C Orphans C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.4 Inactive 10.1126/SCIENCE.ABL4732 2021-12-01
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 {2-Amino-4-[3,5-bis(... pubchem
adenosine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Ago-PAMAgonist 3.2 Active 10.1038/S41586-021-03897-2 2021-09-08
8J9O FZD1 FZD1 Frizzled F (Frizzled) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.4 Active 10.1038/S41421-023-00627-Y 2024-01-17
6LI0 GPR52 GPR52 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A derivative 17 [Nakah... pubchem gtoplig chembl_ligand
Agonist 2.2 Inactive 10.1038/S41586-020-2019-0 2020-02-26
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
Agonist 3.4 Active 10.1016/J.CELL.2020.08.024 2020-09-23
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
Agonist 3.1 Active 10.1038/S41467-022-28111-3 2022-03-02
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...
Agonist 3.0 Active 10.1126/SCIENCE.AAV7942 2019-04-17
8P13 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 5.2 Active 2024-11-20
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
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
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
7S8P MRGX4 MRGPRX4 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N-[(1r,3R,5S,7R)-3,5... pubchem
Agonist 2.6 Active 10.1038/S41586-021-04126-6 2021-11-17
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.2 Active 10.1038/S41586-024-07153-1 2024-03-06
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)
Apo (no ligand) 2.7 Active 10.1038/S41467-023-37177-6 2023-04-12
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.0 Active 10.1038/S41586-024-07153-1 2024-03-06
2YCY ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 2 chemicals 2 steps vapour diffusionNA 3 chems 6.9-7.3 NA (S)-Cyanopindolol pubchem
Antagonist 3.2 Inactive 10.1073/PNAS.1100185108 2011-06-08
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 Lysergide pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.1 Active 10.1016/J.CELREP.2024.114505 2024-07-24
8H8J GPR35 GPR35 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A lodoxamide pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.2 Active 10.1038/S41421-022-00499-8 2023-02-08
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 (2~{S})-2-(3-bromany... pubchem
DAMGO pubchem gtoplig chembl_ligand chembl_ligand
PAMAgonist 3.1 Active 10.1038/S41467-024-47792-6 2024-05-29
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 gtoplig pubchem
Agonist 2.7 Active 10.1038/S41421-023-00610-7 2024-01-03
8IED GP156 GPR156 C Orphans C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A [(2R)-3-[(E)-hexadec... pubchem
Agonist 3.3 Active 2024-02-14
7VV3 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Cortistatin 14 pubchem
Agonist 3.0 Active 10.1038/S41586-021-04077-Y 2021-12-01
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 Apo (no ligand)
Apo (no ligand) 3.1 Active 10.1016/J.CHEMBIOL.2023.08.003 2023-07-12
9EPR B1B1U5 Rhodopsin Opsins A (Rhodopsin) Hasarius adansoni N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Retinal (11-cis) pubchem
Agonist 4.9 Active 10.1038/S41467-024-53208-2 2024-10-30
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 drugbank chembl_ligand pubchem
Agonist 3.0 Active 10.1038/S41586-023-06775-1 2023-11-22
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
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
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 gtoplig
JNJ-40411813 pubchem gtoplig chembl_ligand drugbank
AgonistPAM 3.5 Intermediate 10.1038/S41586-021-03495-2 2021-06-23
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 C5a gtoplig
Agonist 3.9 Active HTTPS://DOI.ORG/10.1016/J.CELL.2023.09.020 2023-10-18
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 2-fluoro-4-[(1R)-6-m... pubchem
tirzepatide pubchem gtoplig
PAMAgonist 3.1 Active 10.1073/PNAS.2116506119 2022-04-13
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
8TQB 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 LY379268 pubchem gtoplig chembl_ligand
Agonist 3.3 Active 10.1101/2023.08.13.552748 2024-07-31
7WI6 GRM3 mGlu3 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A LY341495 pubchem gtoplig chembl_ligand gtoplig
Antagonist 3.7 Inactive 10.1038/S41422-022-00623-Z 2022-03-16
7T10 SSR2 SST2 Somatostatin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A SOMATOSTATIN chembl_ligand pubchem
Agonist 2.5 Active 10.1038/S41594-022-00727-5 2022-03-09
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...
Agonist 2.6 Active 10.1038/S41421-024-00754-0 2024-11-13
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 004-DTR-LYS-TYR-PHA-...
Agonist 3.1 Active 10.1038/S41401-024-01314-8 2024-07-10
8A6C OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Retinal (11-cis) pubchem
Agonist 1.8 Inactive 10.1038/S41586-023-05863-6 2023-03-29
2RH1 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 6.8-6.8 21-23°C Carazolol pubchem
Inverse agonist 2.4 Inactive 10.1126/SCIENCE.1150577 2007-10-30
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
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 CHEMBL410972 chembl_ligand pubchem pubchem
Agonist 2.1 Active 10.1016/J.MOLCEL.2020.09.020 2020-09-09
8SMV GP161 GPR161 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 2.7 Active 10.1101/2023.05.23.540554 2024-02-21
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 pubchem gtoplig pubchem
Agonist 2.7 Active 10.1038/S41467-022-30041-Z 2022-05-18
5DGY OPSD Rhodopsin Opsins 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)
Apo (no ligand) 7.7 Active 10.1038/SDATA.2016.21 2016-03-23
6OFJ OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 4.5 Inactive 10.1074/JBC.RA119.010089 2019-08-21
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
Antagonist 2.7 Inactive 10.1016/J.STR.2018.10.027 2019-01-02
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
Antagonist 3.4 Inactive 10.1126/SCIENCE.1215904 2012-02-15
7TZF CALCR CT Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A amylin peptide
Agonist 2.4 Active 10.1126/SCIENCE.ABM9609 2022-03-23
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 pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.1 Active 10.1038/S41589-021-00841-3 2021-08-25
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 pubchem
Agonist 2.7 Intermediate 10.1126/science.1232808 2013-03-13
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 gtoplig
Antagonist 3.0 Inactive 10.1038/S41422-023-00830-2 2023-06-21
8IW7 TAAR9 TAAR9 A orphans 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 2-Phenylethanaminium pubchem
Agonist 3.0 Active 10.1038/S41586-023-06106-4 2023-05-31
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 chembl_ligand pubchem
Agonist 3.8 Active 2020-12-16
8WGD 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 (2S)-2-azanyl-2-cycl... pubchem
Antagonist 4.5 Inactive 2024-11-27
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
Agonist 3.2 Active 10.1038/S41586-024-07569-9 2024-07-10
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 aristolochic acid pubchem gtoplig chembl_ligand
Agonist 3.0 Active 10.1038/S41586-024-07569-9 2024-07-10
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.2 Active 10.1038/S41586-024-07153-1 2024-03-06
5CXV ACM1 M1 Acetylcholine (muscarinic) A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 8.0-8.0 20°C 0HK pubchem
Antagonist 2.7 Inactive 10.1038/NATURE17188 2016-03-09
8QW4 FZD3 FZD3 Frizzled F (Frizzled) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 2.9 Active 10.1038/S41467-024-51451-1 2024-09-04
2R4S ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps vapour diffusionhanging drop 5 chems 6.5-7.5 22°C Carazolol pubchem
Inverse agonist 3.4 Inactive 10.1038/NATURE06325 2007-11-06
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
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 pubchem gtoplig pubchem
Agonist 2.1 Active 10.1186/S12915-023-01689-W 2023-10-18
8HS2 GPR20 GPR20 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.1 Active 10.1038/S41421-023-00520-8 2023-03-08
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.1 Active 2023-04-26
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 ICI 118551 pubchem gtoplig chembl_ligand chembl_ligand pubchem
Antagonist 2.6 Inactive 10.1107/S2052252519013137 2019-11-13
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 Apo (no ligand)
Apo (no ligand) 2.8 Active 10.1038/S41467-022-33173-4 2022-09-28
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 quisqualate pubchem gtoplig chembl_ligand drugbank gtoplig pubchem
Agonist 3.3 Intermediate 10.1101/2023.08.29.555158 2023-10-11
6ZDV AA2AR A2A Adenosine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 2-Methyl-3-(4-methyl... pubchem
Antagonist 2.1 Inactive 10.1002/ANIE.202003788 2020-09-16
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 CHEMBL410972 chembl_ligand pubchem pubchem
Agonist 3.0 Active 10.1016/J.APSB.2024.09.002 2024-11-27
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
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
8UXY OR1F1 OR1F1 Odorant family 1 O2 (tetrapod specific odorant) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A l-Menthol pubchem
Agonist 3.3 Active 10.1038/S41586-024-08126-0 2024-10-30
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
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 gtoplig
Org27569 pubchem gtoplig chembl_ligand
AgonistNAM 3.3 Inactive 10.1038/S41589-019-0387-2 2019-10-23
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
Agonist 3.0 Inactive 10.1038/S41421-023-00617-0 2023-11-29
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06
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 (5R,6R)-6-(methylami... pubchem
Agonist 4.1 Active 10.1038/S41586-024-07153-1 2024-03-06
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
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
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
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
L-tryptophan pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Calcium pubchem
NAMPAMAgonist 3.2 Inactive 10.1038/S41586-021-03691-0 2021-06-30
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 CHEMBL4576388 chembl_ligand pubchem
JMV431 gtoplig chembl_ligand pubchem
PAMAgonist 3.0 Active 10.1038/S41586-023-06395-9 2023-08-09
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)
Apo (no ligand) 3.2 Active 10.1016/J.CELL.2023.09.020 2023-10-18
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
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
3CAP OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drop 4 chems 5.6-5.6 4°C Apo (no ligand)
Apo (no ligand) 2.9 Active 10.1038/NATURE07063 2008-06-24
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 pubchem
Agonist 3.2 Active 10.1016/J.MOLCEL.2021.06.024 2021-08-04
7F2O BKRB2 B2 Bradykinin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A bradykinin pubchem gtoplig chembl_ligand drugbank gtoplig
Agonist 2.9 Active 10.1038/S41594-021-00645-Y 2021-10-13
7EIB BKRB1 B1 Bradykinin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A [des-Arg<sup>10</sup... pubchem gtoplig chembl_ligand gtoplig
Agonist 3.0 Active 10.1038/S41594-021-00645-Y 2021-10-13
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 2016-03-09
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
Agonist 2.9 Active 10.1038/S41421-022-00405-2 2022-08-31
7F8V GASR CCK2 Cholecystokinin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A desulfated gastrin-1... pubchem gtoplig chembl_ligand pubchem
Agonist 3.3 Active 10.1038/S41589-021-00866-8 2021-10-13
4K5Y CRFR1 CRF1 Corticotropin-releasing factor B1 (Secretin) Human BaculovirusHi5Insect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 4 chems 5.5-5.5 22.5°C CP 376,395 pubchem gtoplig chembl_ligand
Antagonist 3.0 Inactive 10.1038/NATURE12357 2013-07-17
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 pubchem
Agonist 2.8 Active 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
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
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
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
7TS0 CRFR2 CRF2 Corticotropin-releasing factor B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Urocortin pubchem
Agonist 2.8 Active 10.1038/S41467-022-33851-3 2022-11-09
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, Human pubchem
Agonist 3.1 Active 10.1371/JOURNAL.PBIO.3001714 2022-07-13
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.8 Active 10.1038/S41586-024-07153-1 2024-03-06
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 neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
Agonist 2.6 Active 10.1038/NCOMMS8895 2015-07-29
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 2.3 Inactive 2021-10-06
8XFS LGR4 LGR4 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A R-spondin-2
Agonist 3.2 Inactive 2024-12-04
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 s... pubchem chembl_ligand pubchem pubchem
Agonist 3.3 Active 10.1021/ACSPTSCI.8B00056 2019-01-23
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 Apo (no ligand)
Apo (no ligand) 2.8 Active 10.1038/S41467-022-33173-4 2022-09-28
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 quisqualate pubchem gtoplig chembl_ligand drugbank gtoplig pubchem
Agonist 3.7 Intermediate 10.1007/S13238-020-00808-5 2021-09-22
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 chembl_ligand
Agonist 3.7 Active 10.1038/S41467-023-42764-8 2023-11-22
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 Thyrotropin subunit ...
Glycoprotein hormone...
AgonistAgonist 2.4 Active 10.1038/S41586-022-05159-1 2022-08-03
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
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
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 light cha...
K1-70 scFv heavy cha...
AntagonistAntagonist 5.5 Inactive 10.1038/S41586-022-05173-3 2022-08-17
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 pubchem gtoplig
Antagonist 3.1 Inactive 10.1126/SCIENCE.1261064 2015-02-11
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.0 Active 10.1038/S41586-024-07153-1 2024-03-06
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 CHEMBL410972 chembl_ligand pubchem pubchem
LSN3318839 pubchem gtoplig chembl_ligand
AgonistPAM 3.2 Active 2024-11-13
7Y14 MRGRD MRGPRD A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A β-alanine pubchem gtoplig chembl_ligand drugbank pubchem
Agonist 3.2 Intermediate 10.1038/S42003-022-03668-3 2022-07-20
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
Antagonist 3.2 Intermediate 10.1038/s41594-018-0116-7 2018-08-29
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 CCL3 gtoplig
Agonist 2.6 Inactive 2021-07-14
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
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)
Apo (no ligand) 3.8 Inactive 10.1038/S41586-021-03924-2 2021-09-29
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
4J4Q OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drop 3 chems 5.2-6.0 4°C B-Octylglucoside pubchem
unknown 2.7 Active 10.1002/ANIE.201302374 2013-10-30
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
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 AM841 pubchem gtoplig chembl_ligand
Agonist 3.6 Active 10.1093/PROCEL/PWAD055 2024-02-28
8DWG MRGX1 MRGPRX1 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL5177388 chembl_ligand pubchem
Proenkephalin-A
PAMAgonist 2.7 Active 10.1038/S41589-022-01173-6 2022-11-02
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.6 Active 10.1038/S41586-024-07153-1 2024-03-06
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 exendin-4 pubchem gtoplig pubchem
Agonist 2.5 Active 10.1038/S41589-021-00945-W 2022-01-05
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 (2~{S})-4-methyl-2-[... pubchem
Agonist 2.8 Intermediate 10.1126/sciadv.abe5504 2021-02-10
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 ZM-241385 pubchem gtoplig chembl_ligand drugbank
Antagonist 2.7 Inactive 10.1038/NATURE10750 2012-02-01
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 3-[(3R)-3-methyl-1,2... pubchem
Agonist 3.5 Active 10.1038/S41586-022-05258-Z 2022-07-06
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 [(2~{R})-2-[5-(2-hex... pubchem
Agonist 3.8 Active 10.1038/S41467-022-33121-2 2022-10-05
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 pubchem
Antagonist 2.5 Inactive 10.1038/NATURE14035 2015-01-14
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 3.4 Active 10.1073/PNAS.2219569120 2023-05-24
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
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)
Apo (no ligand) 3.2 Active 10.1038/S41589-023-01339-W 2023-05-10
8DWC MRGX1 MRGPRX1 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Proenkephalin-A
Agonist 2.9 Active 10.1038/S41589-022-01173-6 2022-11-02
7TYH CALCR CT Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Calcitonin human pubchem
Agonist 3.3 Active 10.1126/SCIENCE.ABM9609 2022-03-23
6JOD AGTR2 AT2 Angiotensin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A angiotensin II pubchem gtoplig chembl_ligand drug_central drugbank pubchem pubchem pubchem
Agonist 3.2 Active 10.1016/J.STR.2019.12.003 2020-01-15
2PED OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drop 5 chems 6.4-6.4 283 K Retinal (9-cis) pubchem
Inverse agonist 3.0 Inactive 10.1529/BIOPHYSJ.107.108225 2007-10-30
7KNU CALRL calcitonin-like Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Calcitonin gene-rela... pubchem
Agonist 3.5 Inactive 10.1126/SCIENCE.ABF7258 2021-02-24
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
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
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 Carazolol pubchem
Inverse agonist 3.5 Intermediate 10.1073/PNAS.2414544121 2024-11-13
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 gtoplig pubchem
Agonist 3.5 Active 10.1016/J.MOLCEL.2023.07.030 2023-09-06
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
5ZK8 ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N-methyl scopolamine pubchem gtoplig drugbank gtoplig chembl_ligand chembl_ligand chembl_ligand pubchem pubchem
Antagonist 3.0 Inactive 10.1038/S41589-018-0152-Y 2018-11-21
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 pubchem pubchem
Agonist 2.8 Active 10.1038/S41422-023-00830-2 2023-06-21
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)
Apo (no ligand) 3.9 Inactive 10.1038/S41586-021-03641-W 2021-06-23
6LPJ AA2AR A2A Adenosine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ZM-241385 pubchem gtoplig chembl_ligand drugbank
Antagonist 1.8 Inactive 10.1038/S41598-020-76277-X 2020-11-25
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 pubchem
Antagonist 3.0 Inactive 10.1038/S41598-020-68355-X 2020-07-29
7C7S GABR2 GABAB2 GABAB C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CGP 54626A pubchem gtoplig chembl_ligand gtoplig
Antagonist 2.9 Inactive 10.1038/S41422-020-0350-5 2020-07-01
8JHB FZD6 FZD6 Frizzled F (Frizzled) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.3 Active 10.1038/S41421-023-00627-Y 2024-01-17
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 CXCL11 gtoplig
Agonist 3.0 Active 10.1038/S41594-023-01175-5 2023-11-29
4WW3 OPSD Rhodopsin Opsins A (Rhodopsin) Japanese flying squid NANativeSquid 1 chemicals 1 steps vapour diffusionsitting drop 4 chems 6.4-6.4 100-170 K Retinal (all-trans) pubchem
Agonist 2.8 Inactive 10.1371/JOURNAL.PONE.0126970 2015-06-17
8T1V GPR6 GPR6 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL4763822 chembl_ligand pubchem
Inverse agonist 2.6 Inactive 10.1126/SCISIGNAL.ADO8741 2024-12-04
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
Agonist 3.2 Active 10.1038/S41401-024-01314-8 2024-07-10
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)
Apo (no ligand) 3.5 Active 10.1038/S41586-023-06420-X 2023-08-16
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
6LI2 GPR52 GPR52 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 2.8 Inactive 10.1038/S41586-020-2019-0 2020-02-26
6W2Y GABR1 GABAB1 GABAB C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CGP55845 pubchem
1-Stearoyl-2-oleoyl-... pubchem
Inverse agonistNAM 3.2 Inactive 10.1038/S41586-020-2469-4 2020-07-01
9EW2 FZD7 FZD7 Frizzled F (Frizzled) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.2 Active 2024-10-02
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 CHEMBL4576388 chembl_ligand pubchem
neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
PAMAgonist 2.9 Active 10.1021/ACS.BIOCHEM.3C00029 2023-03-29
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 pubchem
Agonist 2.7 Inactive 10.1126/SCIENCE.1232807 2013-03-13
3PXO OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drops 3 chems 5.0-5.8 4°C Retinal (all-trans) pubchem
Agonist 3.0 Active 10.1038/NATURE09789 2011-03-09
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 (1R,2S)-N-[4-(2,6-di... pubchem
Agonist 2.7 Inactive 10.1038/S41594-022-00797-5 2022-07-27
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
Agonist 3.3 Active 10.1038/S41589-022-01130-3 2022-10-19
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 pubchem
Antagonist 2.8 Inactive 10.1038/S41467-020-19109-W 2020-10-07
5T04 NTR1 NTS1 Neurotensin A (Rhodopsin) Rat BaculovirusTni PRO (Trichoplusia ni) cell linesInsect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 8.5-9.0 20°C neurotensin pubchem gtoplig chembl_ligand gtoplig gtoplig
Agonist 3.3 Active 10.1038/SREP38564 2016-12-21
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 Protachykinin-1
Agonist 2.9 Active 2024-02-07
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
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
Antagonist 3.0 Inactive 10.1038/S41467-023-44477-4 2024-01-17
2HPY OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 5.9-6.1 283 K Retinal (all-trans) pubchem
Agonist 2.8 Inactive 10.1073/PNAS.0601765103 2006-08-22
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
5UIG AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps vapour diffusionSitting drop 6 chems 7.0-7.0 20°C 5-Amino-N-[(2-Methox... pubchem
Antagonist 3.5 Inactive 10.1073/PNAS.1621423114 2017-02-08
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 HIS-LYS-THR-ASP-SER-...
Agonist 2.7 Active 2023-05-31
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 methyl 4-[4-(3-methy... pubchem
Allosteric agonist 3.6 Active 10.1038/S41467-022-30595-Y 2022-05-11
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
7SIN CASR CaS Calcium-sensing C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A NPS 2143 pubchem gtoplig chembl_ligand drugbank
Antagonist 5.9 Inactive 10.1073/PNAS.2115849118 2022-01-19
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
8SAI GPR34 GPR34 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A O-[(S)-Hydroxy{[(2s)... pubchem
Agonist 3.3 Active 10.1073/PNAS.2308435120 2023-10-04
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 (4R,7R,18E)-4,7-dihy... pubchem
Agonist 3.1 Active 10.1038/S41594-022-00816-5 2022-08-24
8HJ5 MRGX1 MRGPRX1 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A compound 16 [PMID: 3... pubchem gtoplig chembl_ligand
Agonist 3.0 Active 2023-05-31
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 gtoplig pubchem
Agonist 3.1 Active 10.1073/PNAS.2216329120 2024-01-03
7BB6 V2R V2 Vasopressin and oxytocin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A vasopressin pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Agonist 4.2 Active 10.1126/SCIADV.ABG5628 2021-06-02
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 INTERMEDINE chembl_ligand pubchem pubchem pubchem
Agonist 3.0 Active 10.1038/S41422-021-00557-Y 2021-09-08
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
9EPP B1B1U5 Rhodopsin Opsins A (Rhodopsin) Hasarius adansoni N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 11,20-Ethanoretinal pubchem
Agonist 4.1 Active 2024-10-23
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
4JKV SMO SMO Frizzled F (Frizzled) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 6 chems 7.4-7.4 20°C taladegib pubchem gtoplig chembl_ligand drugbank pubchem
Antagonist 2.5 Inactive 10.1038/NATURE12167 2013-04-24
5TE3 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drop 4 chems 5.2-6.6 4°C B-Octylglucoside pubchem
unknown 2.7 Active 10.1073/PNAS.1617446114 2017-03-15
7Y12 MRGRD MRGPRD A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A β-alanine pubchem gtoplig chembl_ligand drugbank pubchem
Agonist 3.1 Active 10.1038/S42003-022-03668-3 2022-07-20
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 tirzepatide pubchem gtoplig
Agonist 3.2 Active 10.1038/S41467-022-28683-0 2022-03-02
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 [Ac-His<sup>1</sup>]... gtoplig chembl_ligand pubchem
Agonist 3.0 Active 10.1016/J.MOLCEL.2020.01.012 2020-02-05
7WZ4 GPR88 GPR88 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.0 Active 10.1038/S41467-022-30081-5 2022-10-26
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06
7S8O MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (R)-ZINC-3573 pubchem gtoplig chembl_ligand
Agonist 2.6 Active 10.1038/S41586-021-04126-6 2021-11-17
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.2 Active 10.1038/S41586-024-07153-1 2024-03-06
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
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
7WF7 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A sphingosine 1-phosph... pubchem gtoplig chembl_ligand pubchem
Agonist 3.4 Active 10.1038/S41589-021-00930-3 2022-01-05
8GTM CRFR1 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 7-(4-bromanyl-2,6-di... pubchem
Antagonist 2.6 Inactive 10.1038/S12276-023-01082-1 2023-09-13
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 pubchem
Antagonist 2.4 Inactive 2023-08-16
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 chembl_ligand pubchem
Agonist 3.3 Active 10.1038/S41421-024-00705-9 2024-08-28
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
Agonist 3.0 Active 10.1073/PNAS.2216230120 2023-02-22
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
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
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 pubchem gtoplig chembl_ligand gtoplig gtoplig
Agonist 2.7 Active 10.1126/SCIADV.ABK2872 2021-12-15
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
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
Agonist 3.1 Active 10.1038/S41586-024-07569-9 2024-07-10
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 gtoplig pubchem
Agonist 2.7 Active 10.1038/S41467-024-52585-Y 2024-10-09
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 pubchem pubchem
Agonist 3.1 Active 10.1038/S41422-020-00424-2 2020-12-02
4LDO ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)7.7 MAG 5 chems 6.5-6.5 20°C (-)-adrenaline pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem
Agonist 3.2 Active 10.1038/NATURE12572 2013-09-25
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 3.6 Active 10.1016/J.CELREP.2022.111211 2022-08-24
2I37 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 2 chemicals 2 steps vapour diffusionsitting drops 5 chems 7.0-8.0 5°C Apo (no ligand)
Apo (no ligand) 4.2 Inactive 10.1073/PNAS.0608022103 2006-10-17
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
Agonist 2.7 Active 2024-04-03
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 Methyl 4-[[(4R,4aS,7... pubchem
Antagonist 2.8 Inactive 10.1038/NATURE10954 2012-03-21
6Z4S NTR1 NTS1 Neurotensin A (Rhodopsin) Rat N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A meclinertant pubchem gtoplig chembl_ligand drugbank
Inverse agonist 2.7 Inactive 10.1126/sciadv.abe5504 2021-02-10
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
Antagonist 3.0 Inactive 10.1038/NATURE10753 2012-02-01
7FD9 GRM5 mGlu5 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A LY341495 pubchem gtoplig chembl_ligand gtoplig
Antagonist 4.0 Inactive 10.1016/J.CELREP.2021.109648 2021-09-08
3OAX OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionHanging drops 5 chems 6.0-6.0 283 K Retinal (11-cis) pubchem
Inverse agonist 2.6 Inactive 10.1016/J.BPJ.2010.08.003 2011-01-19
6OS9 NTR1 NTS1 Neurotensin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A JMV449 pubchem gtoplig chembl_ligand
Agonist 3.0 Active 10.1038/S41586-019-1337-6 2019-07-10
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
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 ACY-DTY-HYP-ASN-THR-...
Agonist 3.0 Active 10.1126/SCIADV.ADN7771 2024-10-30
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 GIP pubchem
Agonist 3.0 Active 10.7554/ELIFE.68719 2021-08-04
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 Gastrin-releasing pe... pubchem
Agonist 3.3 Active 10.1038/S41422-022-00743-6 2023-08-09
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
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)
Apo (no ligand) 2.8 Active 10.1016/J.CELREP.2024.114505 2024-07-24
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 gtoplig chembl_ligand gtoplig gtoplig
Agonist 3.0 Inactive 10.1073/PNAS.1317903111 2014-01-29
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
Agonist 2.8 Active 10.1038/S41421-024-00700-0 2024-08-07
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
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 (S)-Cyanopindolol pubchem
Agonist 2.8 Active 10.1126/SCIENCE.AAU5595 2018-10-17
8WVU LGR4 LGR4 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A R-spondin-1
Agonist 3.6 Inactive 2024-10-30
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
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 pubchem
Agonist 2.6 Inactive 10.1126/SCIENCE.ABL8615 2022-01-26
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
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 pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.2 Active 10.1038/S41421-022-00420-3 2022-07-20
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
8K4O Q76SF8 ORF74 Unclassified A (Rhodopsin) HHV-8 N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Growth-regulated alp...
Agonist 3.0 Active 2024-07-24
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
Agonist 3.3 Active 10.1038/S41586-024-07569-9 2024-07-10
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 004-DTR-LYS-TY5-PHE-...
Agonist 2.5 Active 2024-07-03
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 N-(5-carbamimidamido...
Agonist 3.2 Active 10.1038/S41586-022-05588-Y 2022-05-04
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 pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Agonist 2.6 Active 10.1038/S41422-021-00480-2 2021-07-21
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 Apo (no ligand)
Apo (no ligand) 3.4 Active 10.1038/S41586-022-04580-W 2022-04-27
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 CCL5 gtoplig
Agonist 3.2 Active 10.1126/SCIADV.ABG8685 2021-06-30
5D6L ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 7.0-7.0 20°C Carazolol pubchem
Inverse agonist 3.2 Inactive 10.1038/NPROT.2017.057 2016-08-17
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
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 1-[[4-[5-Fluoro-6-[(... pubchem
Agonist 3.0 Active 10.1038/S41467-023-37112-9 2023-05-10
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 [Ac-His<sup>1</sup>]... gtoplig chembl_ligand pubchem
Agonist 2.3 Active 10.1038/S41467-022-34629-3 2022-11-23
8HQM GP132 GPR132 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CHEMBL3354065 chembl_ligand pubchem
Agonist 3.0 Active 10.1038/S42255-023-00899-4 2023-10-11
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 chembl_ligand pubchem pubchem
Agonist 2.7 Active 10.1038/S41467-022-34629-3 2022-11-23
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
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
Agonist 2.7 Active 10.1126/SCIENCE.ABM9609 2022-03-23
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 JMV431 gtoplig chembl_ligand pubchem
Agonist 4.2 Active 10.1038/S41586-020-1953-1 2020-02-26
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
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
7F53 MC4R MC4 Melanocortin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A α-MSH pubchem gtoplig
Agonist 3.0 Active 2021-11-03
6LI3 GPR52 GPR52 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.3 Active 10.1038/S41586-020-2019-0 2020-02-26
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 2-[[(3R)-4-(4-Tert-b... pubchem
CHEMBL1615159 chembl_ligand pubchem
PAMAgonist 3.2 Active 10.1126/SCIENCE.AAW8981 2019-06-26
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06
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
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
7TUZ GP183 GPR183 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (2S,4aS,4bS,7R,8S,8a... pubchem
Agonist 3.1 Active 10.1016/J.STR.2022.04.006 2022-04-13
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 pubchem
Agonist 3.1 Active 10.1038/S41422-023-00835-X 2023-06-21
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 chembl_ligand pubchem
Agonist 2.9 Active 10.1038/S41594-023-01175-5 2023-11-29
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.6 Active 10.1038/S41586-024-07153-1 2024-03-06
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
Agonist 3.0 Active 10.1038/S41421-022-00405-2 2022-08-31
2Y01 ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 1 chemicals 1 steps vapour diffusionsitting drops 6 chems 9.0-9.0 4°C Dobutamine pubchem
Agonist (partial) 2.6 Inactive 10.1038/NATURE09746 2011-03-30
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 4-({2-[(1R,2R,3R,5S)... pubchem
Agonist 3.2 Active 10.1073/PNAS.2216329120 2024-01-10
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
8FD1 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 4.3 Inactive 10.1038/S41467-023-40911-9 2023-08-30
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 Apo (no ligand)
Apo (no ligand) 2.8 Active 10.1126/SCIADV.ABN8048 2022-07-13
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 drugbank chembl_ligand pubchem
Agonist 3.5 Active 10.1038/S41586-023-06804-Z 2023-11-15
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 3-[(1R)-1-(2-methoxy... pubchem
Agonist 3.3 Active 10.1073/PNAS.2321532121 2024-06-05
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)
Apo (no ligand) 2.5 Active 10.1038/S41421-024-00649-0 2024-03-06
8IEP GP156 GPR156 C Orphans C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A [(2R)-3-[(E)-hexadec... pubchem
Agonist 2.6 Inactive 2024-02-14
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 chembl_ligand pubchem
Agonist 2.8 Active 10.1126/SCIENCE.AAU5595 2018-10-17
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 CHEMBL508044 chembl_ligand pubchem
Agonist (partial) 2.7 Intermediate 10.1126/sciadv.abe5504 2021-02-10
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
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
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)
Apo (no ligand) 3.4 Active 2022-05-11
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 10.1016/J.CELL.2015.06.002 2015-06-03
8IYX GPR34 GPR34 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A YL-365 pubchem gtoplig
Antagonist 3.3 Active 10.1073/PNAS.2308435120 2024-03-20
7ZI0 SMO SMO Frizzled F (Frizzled) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 3-chloro-N-[trans-4-... pubchem
Antagonist 3.0 Inactive 10.1126/SCIADV.ABM5563 2022-06-15
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
Agonist 3.0 Active 10.1038/S41586-021-03376-8 2021-04-14
8TB0 GPR61 GPR61 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 3.5 Active 2023-10-04
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 CHEMBL216166 chembl_ligand pubchem
Agonist 2.0 Active 10.1371/JOURNAL.PBIO.3001295 2021-05-26
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
8WW2 GPR3 GPR3 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A oleic acid pubchem gtoplig chembl_ligand drug_central
Agonist 2.8 Active 10.1038/S41422-024-00932-5 2024-02-14
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
Agonist 3.1 Active 10.1016/J.CELL.2023.10.014 2023-12-27
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 Retinoic acid recept...
Agonist 3.3 Active 2024-08-21
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 pubchem
Antagonist 3.1 Intermediate 10.1038/s41594-018-0116-7 2018-08-29
7C2E GLP1R GLP-1 Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 2-[[4-[6-[(4-cyano-2... pubchem
Agonist 4.2 Active 10.1038/S41422-020-0384-8 2020-08-26
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
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 pubchem
Agonist 3.0 Active 10.1016/j.cell.2018.01.001 2018-02-14
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
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
Agonist 3.8 Active 10.1038/S41467-024-46239-2 2024-03-06
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 Neuromedin U-25 (hum... pubchem
Agonist 3.2 Active 10.1038/S41467-022-29683-W 2022-04-20
6RZ8 CLTR2 CysLT2 Leukotriene A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ONO-2080365 pubchem
Antagonist 2.7 Active 10.1038/S41467-019-13348-2 2019-12-11
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
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
Agonist 3.3 Active 10.1038/S41589-022-01130-3 2022-10-19
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
6TPK OXYR OT Vasopressin and oxytocin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A retosiban pubchem gtoplig chembl_ligand drugbank
Antagonist 3.2 Inactive 10.1126/SCIADV.ABB5419 2020-08-05
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.2 Active 10.1038/S41586-024-07153-1 2024-03-06
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 pubchem
Agonist 3.4 Active 10.1038/S41467-023-39799-2 2023-07-19
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
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
8IZB GP174 GPR174 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A LYSOPHOSPHATIDIC ACI... chembl_ligand pubchem
L-serine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
AgonistAgonist 3.1 Active 10.1371/JOURNAL.PBIO.3002387 2023-11-01
8WRB GPR34 GPR34 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A LYSOPHOSPHATIDIC ACI... chembl_ligand pubchem
Agonist 2.9 Active 10.1371/JOURNAL.PBIO.3002387 2023-11-08
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.1 Active 10.1038/S41586-024-07153-1 2024-03-06
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
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)
Apo (no ligand) 3.2 Active 2024-04-17
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 [Ac-His<sup>1</sup>]... gtoplig chembl_ligand pubchem
Agonist 3.2 Active 10.1038/S41467-020-17933-8 2020-09-02
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 chembl_ligand pubchem
Agonist 3.0 Inactive 10.1016/J.BBRC.2019.12.091 2020-02-12
2R4R ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps vapour diffusionhanging drop 5 chems 6.5-7.5 22°C Carazolol pubchem
Inverse agonist 3.4 Inactive 2007-11-06
6OYA OPSD Rhodopsin Opsins A (Rhodopsin) Bovine N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Retinal (all-trans) pubchem
Agonist 3.3 Active 10.1016/J.MOLCEL.2019.06.007 2019-07-24
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
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 SALVINORIN B METHOXY... chembl_ligand pubchem
Agonist 2.8 Active 10.1038/S41586-023-06030-7 2023-05-03
8IEQ GP156 GPR156 C Orphans C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A [(2R)-3-[(E)-hexadec... pubchem
Agonist 2.7 Inactive 2024-02-14
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
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 aristolochic acid pubchem gtoplig chembl_ligand
Agonist 2.8 Active 10.1038/S41586-024-07569-9 2024-07-10
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 drugbank
Agonist 3.3 Active 10.1038/S41467-024-47207-6 2024-04-24
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 antibody heavy c...
M22 antibody light c...
AgonistAgonist 2.9 Active 10.1038/S41586-022-05159-1 2022-08-03
5JQH ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)7.7 MAG 5 chems 7.5-7.5 23°C Carazolol pubchem
Inverse agonist 3.2 Inactive 10.1038/NATURE18636 2016-07-13
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
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
PAM 2.9 Active 10.1016/J.MOLCEL.2023.07.030 2023-09-06
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
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
6LFL CXCR2 CXCR2 Chemokine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 4-[[3,4-Dioxo-2-[[(1... pubchem
Allosteric antagonist 3.2 Inactive 10.1038/S41586-020-2492-5 2020-09-02
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 Cyclomethyltryptopha... pubchem
tecalcet pubchem gtoplig chembl_ligand
AgonistPAM 3.4 Active 2024-04-17
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 2024-05-22
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 pubchem
Agonist 3.2 Inactive 10.1038/S41586-019-1141-3 2019-04-24
7VV4 MRGX2 MRGPRX2 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Cortistatin 14 pubchem
Agonist 3.0 Active 10.1038/S41586-021-04077-Y 2021-12-01
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
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06
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 CHEMBL552527 chembl_ligand pubchem
Agonist 3.2 Active 10.1038/S41467-020-14728-9 2020-02-26
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
Allosteric agonistAgonist 2.9 Active 2024-07-24
6XBK SMO SMO Frizzled F (Frizzled) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Cholesterol pubchem
Agonist 3.2 Active 10.1038/S41589-020-0646-2 2020-09-30
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.5 Active 10.1038/S41586-024-07153-1 2024-03-06
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 gtoplig
Agonist 3.0 Active 10.1126/SCIENCE.ABO1633 2022-10-12
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
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 Apo (no ligand)
Apo (no ligand) 2.7 Active 10.1038/S41586-022-04575-7 2022-04-27
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 KGCHM07
Agonist 2.8 Active 10.1126/SCIADV.AAX9115 2019-12-11
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 Cyclomethyltryptopha... pubchem
Calcium pubchem
PAMAgonist 3.0 Active 10.7554/ELIFE.68578 2021-09-22
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 pubchem
Agonist 2.8 Active 2024-10-16
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
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
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
Agonist 2.9 Active 10.1002/ADVS.202306311 2024-02-14
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.4 Active 10.1038/S41586-024-07153-1 2024-03-06
7EWP GP158 GPR158 C Orphans C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Apo (no ligand)
Apo (no ligand) 4.3 Inactive 10.1038/S41467-021-27147-1 2021-12-01
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
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 pubchem
Antagonist 2.9 Inactive 10.1016/J.STR.2022.11.001 2022-11-23
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 alpha gtoplig
Choriogonadotropin b... gtoplig
AgonistAgonist 3.9 Active 10.1038/S41586-021-03924-2 2021-09-29
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
Agonist 2.9 Active 10.1038/S41586-024-07569-9 2024-07-10
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 pubchem
Agonist 3.6 Active 10.1038/S41422-020-0280-2 2020-03-11
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 Apelin receptor earl...
Agonist 3.2 Active 10.1038/S41594-022-00797-5 2022-07-27
2X72 OPSD Rhodopsin Opsins A (Rhodopsin) Bovine Stable_cellsHEK293S-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionsitting drop 3 chems 4.5-4.5 4°C Retinal (all-trans) pubchem
Agonist 3.0 Active 10.1038/NATURE09795 2011-03-16
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 pubchem
Agonist 3.1 Active 10.1038/S41422-023-00808-0 2023-06-07
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 Parathyroid hormone
Agonist 2.6 Active 10.1016/J.STR.2023.04.002 2023-04-26
8U8F GPR3 GPR3 A orphans A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A palmitic acid pubchem gtoplig chembl_ligand drugbank pubchem
Agonist 3.5 Active 10.1021/ACS.BIOCHEM.3C00647 2024-03-06
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
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 pubchem
Inverse agonist 3.4 Inactive 2024-08-28
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
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 ~{N}-[(2~{R})-1-[[(1... pubchem
Agonist 2.7 Active 10.1038/S41422-022-00669-Z 2022-06-01
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 pubchem
Agonist 3.4 Active 10.1038/S41422-021-00527-4 2021-08-04
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)
Apo (no ligand) 3.0 Active 2024-11-13
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 gtoplig pubchem
compound 9n [PMID: 1... pubchem gtoplig chembl_ligand
AgonistPAM 3.2 Active 10.1016/J.MOLCEL.2023.07.030 2023-09-06
6YVR NTR1 NTS1 Neurotensin A (Rhodopsin) Rat N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A JMV431 gtoplig chembl_ligand pubchem
Agonist 2.5 Inactive 10.1126/sciadv.abe5504 2021-02-10
4X1H OPSD Rhodopsin Opsins A (Rhodopsin) Bovine NANativeBovine 1 chemicals 1 steps vapour diffusionsitting drop 3 chems 5.0-6.5 4°C B-Nonylglucoside pubchem
unknown 2.3 Active 10.1016/J.STR.2015.09.015 2015-11-04
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 CHEMBL404594 chembl_ligand pubchem
Agonist 3.2 Active 10.1038/S41594-018-0079-8 2018-07-11
4U15 ACM3 M3 Acetylcholine (muscarinic) A (Rhodopsin) Rat BaculovirusSf9Insect 9 chemicals 9 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 7.5-7.5 298 K tiotropium pubchem gtoplig chembl_ligand drugbank gtoplig chembl_ligand chembl_ligand pubchem
Antagonist 2.8 Inactive 10.1016/J.STR.2014.08.022 2014-11-26
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 Kisspeptin-10 pubchem
Agonist 3.0 Active 10.1126/SCIADV.ADN7771 2024-10-30
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 (5R,6R)-6-(methylami... pubchem
Agonist 3.3 Active 10.1038/S41586-024-07153-1 2024-03-06