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RECEPTOR EXPRESSION SOLUBILIZATION PURIFICATION STRUCTURE DETERMINATION
PDB pH Temp Resolution Reference Date
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 2022-06-29
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 2021-01-06
6NIY CALCR CT Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Calcitonin salmon pubchem
Agonist 3.3 Active 10.1021/ACSPTSCI.8B00056 2019-01-23
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 Calcium pubchem
L-tryptophan pubchem gtoplig chembl_ligand drugbank drug_central pubchem
cinacalcet pubchem gtoplig chembl_ligand drugbank drug_central
AgonistPAMPAM 2.8 Active 10.1038/S41586-021-03691-0 2021-06-30
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 2021-08-25
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
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
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
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
5A8E ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey BaculovirusHi5Insect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 4 chems 7.0-7.0 20°C 7-methylcyanopindolo... pubchem
Inverse agonist 2.4 Inactive 10.1124/MOL.115.101030 2015-09-30
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
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
7TD0 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A (2r)-2-Hydroxy-3-(Ph... pubchem
Agonist 2.8 Active 10.1038/S41467-022-28417-2 2022-02-09
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
4ZJC OX1R OX1 Orexin A (Rhodopsin) Human BaculovirusSf9Insect 6 chemicals 6 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 5.6-5.6 20°C SB-674042 pubchem gtoplig chembl_ligand
Antagonist 2.8 Inactive 10.1038/NSMB.3183 2016-03-09
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
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... pubchem
Agonist 3.2 Active 10.1038/S41594-022-00797-5 2022-07-27
2R4S ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps vapour diffusionhanging drop 5 chems 6.5-7.5 22°C N/A N/A 3.4 Inactive 10.1038/NATURE06325 2007-11-06
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
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
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
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
7LD3 AA1R A1 Adenosine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A adenosine pubchem gtoplig chembl_ligand drugbank drug_central
{2-Amino-4-[3,5-bis(... pubchem
AgonistPAM 3.2 Active 2021-09-08
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
Antagonist 2.8 Intermediate 10.1016/j.bcp.2022.115291 2022-11-02
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
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
7WV9 CNR1 CB1 Cannabinoid A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A CP55940 pubchem gtoplig chembl_ligand gtoplig
6-methyl-3-[(1S)-2-n... pubchem
AgonistPAM 3.4 Active 10.1038/S41589-022-01038-Y 2022-06-15
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
5NDD PAR2 PAR2 Proteinase-activated A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 5.5-6.2 20°C AZ8838 pubchem gtoplig chembl_ligand
Antagonist 2.8 Intermediate 10.1038/NATURE22309 2017-05-03
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
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... pubchem
Agonist 4.2 Active 10.1038/S41594-022-00797-5 2022-07-27
3OE0 CXCR4 CXCR4 Chemokine A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 6.0-6.0 20°C CVX15
Antagonist 2.9 Inactive 10.1126/SCIENCE.1194396 2010-10-27
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
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 2022-07-20
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
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
7EW0 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ozanimod pubchem gtoplig drug_central chembl_ligand drugbank
Agonist 3.4 Active 10.1038/S41422-021-00566-X 2021-09-29
6VCB GLP1R GLP-1 Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A glucagon-like peptid... pubchem gtoplig chembl_ligand gtoplig pubchem pubchem
LSN3160440 pubchem
AgonistPAM 3.3 Active 10.1038/S41589-020-0589-7 2020-07-22
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
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
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
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
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
6K41 ADA2B α2B Adrenoceptors A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A dexmedetomidine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.9 Active 10.1038/S41589-020-0492-2 2020-04-15
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
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
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
6TO7 OX1R OX1 Orexin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A suvorexant pubchem gtoplig chembl_ligand drug_central drugbank
Antagonist 2.3 Inactive 10.1021/acs.jmedchem.9b01787 2020-01-01
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
Agonist 3.3 Active 2022-08-03
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
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
7T6T FPR1 FPR1 Formylpeptide A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A synthetic peptide
Agonist 3.2 Active 2022-03-30
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
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
7F1O DRD1 D1 Dopamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A dopamine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.1 Active 2022-06-15
6WGT 5HT2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Lysergide pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.4 Inactive 10.1016/J.CELL.2020.08.024 2020-09-23
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
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 L-tryptophan pubchem gtoplig chembl_ligand drugbank drug_central pubchem
evocalcet pubchem gtoplig drug_central chembl_ligand drugbank
Calcium pubchem
PAMPAMAgonist 3.2 Active 10.1126/SCIADV.ABG1483 2021-06-16
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
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
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 2021-12-01
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
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
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
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 34793198 2021-12-01
5ZBH NPY1R Y1 Neuropeptide Y A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A BMS-193885 pubchem
Antagonist 3.0 Inactive 10.1038/S41586-018-0046-X 2018-04-25
7FII LSHR LH Glycoprotein hormone A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Choriogonadotropin b... gtoplig
Glycoprotein alpha gtoplig
AgonistAgonist 4.3 Active 10.1038/S41586-021-03924-2 2021-09-29
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 2-phenylmelatonin pubchem
Agonist 2.9 Inactive 10.1038/S41586-019-1141-3 2019-04-24
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
Agonist 3.1 Active 10.1038/S41422-020-00424-2 2020-12-02
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
Agonist 2.6 Active 10.1038/S41401-022-01032-Z 2022-12-21
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
PAM 2.4 Active 2022-04-13
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
7FIG LSHR LH Glycoprotein hormone A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Choriogonadotropin b... gtoplig
Glycoprotein alpha gtoplig
AgonistAgonist 3.9 Active 10.1038/S41586-021-03924-2 2021-09-29
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
Antagonist 2.3 Inactive 10.1038/S41589-018-0152-Y 2018-11-21
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
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
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
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
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
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
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 2022-01-05
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
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
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
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 2022-03-23
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
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
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
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
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
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 Proenkephalin-A
2-(Cyclopropanesulfo... pubchem
AgonistPAM 2.7 Active 10.1038/S41589-022-01173-6 2022-11-02
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
Agonist 3.3 Active 10.1038/S41589-022-01130-3 2022-10-19
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
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
Antagonist 2.7 Inactive 10.1126/SCIENCE.1241475 2013-09-11
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
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
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
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
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
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
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 2022-06-29
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
3D4S ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 5 chems 7.0-7.0 20°C timolol pubchem gtoplig chembl_ligand drugbank drug_central
Inverse agonist 2.8 Inactive 10.1016/J.STR.2008.05.001 2008-06-17
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
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
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 Intermediate 10.1038/NATURE13288 2014-04-30
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
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
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 Calcium pubchem
NPS 2143 pubchem gtoplig chembl_ligand drugbank
L-tryptophan pubchem gtoplig chembl_ligand drugbank drug_central pubchem
AgonistNAMPAM 3.2 Inactive 10.1126/SCIADV.ABG1483 2021-06-16
7EVY S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A siponimod pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.0 Active 10.1038/S41422-021-00566-X 2021-09-29
7DHI ADRB2 β2 Adrenoceptors A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A levosalbutamol pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 3.3 Active 10.1093/NSR/NWAA284 2020-12-16
7BZ2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A arformoterol pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.8 Active 10.1038/S41421-020-0176-9 2020-08-05
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
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
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 2021-12-01
7DD6 CASR CaS Calcium-sensing C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Calcium pubchem
L-tryptophan pubchem gtoplig chembl_ligand drugbank drug_central pubchem
AgonistPAM 3.2 Active 10.1126/SCIADV.ABG1483 2021-06-16
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
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
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 Unknown ligand
CGP 54626A pubchem gtoplig chembl_ligand gtoplig
NAMAntagonist 3.5 Inactive 10.1016/J.JMB.2020.09.023 2020-11-11
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
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 2021-10-13
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
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
Antagonist 2.8 Inactive 2022-06-29
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
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
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
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
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 Intermediate 10.1021/acs.jmedchem.0c01020 2020-09-16
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
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
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 2,4-bis(3-methoxy-4-... pubchem
Agonist 3.1 Active 10.1073/PNAS.2200155119 2022-06-29
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
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
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 (2r)-2-Hydroxy-3-(Ph... pubchem
Agonist 3.1 Active 10.1038/S41467-022-28417-2 2022-02-09
7F58 MC4R MC4 Melanocortin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A THIQ pubchem gtoplig chembl_ligand
Agonist 3.1 Active 2021-11-03
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 2.6 Active 10.1038/S41467-022-31823-1 2022-07-27
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
7CX2 PE2R2 EP2 Prostanoid A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A PGE2 pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
Agonist 2.8 Active 10.1126/SCIADV.ABF1268 2021-05-05
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 N/A N/A 4.7 Active 10.1126/SCIADV.ABO7761 2022-09-14
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
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 Active 2022-07-20
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
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
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 10.1038/S41589-020-0646-2 2020-09-30
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
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
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 gtoplig pubchem
Antagonist 2.8 Inactive 10.1021/ACS.JMEDCHEM.2C00462 2022-08-31
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 2021-04-14
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 Apo (no ligand)
Apo (no ligand) 3.6 Inactive 10.1038/NSMB.3450 2017-08-16
7T6V FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A synthetic peptide
Agonist 3.1 Active 2022-03-30
6AK3 PE2R3 EP3 Prostanoid A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A PGE2 pubchem gtoplig chembl_ligand drugbank drug_central gtoplig
Agonist 2.9 Active 10.1038/S41589-018-0171-8 2018-12-05
7DB6 MTR1A MT1 Melatonin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ramelteon pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.3 Active 10.1038/S41594-021-00634-1 2021-08-18
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
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
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 2021-08-18
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
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 2021-12-01
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
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
Agonist 3.8 Active 2022-08-03
3PBL DRD3 D3 Dopamine A (Rhodopsin) Human BaculovirusSf9Insect 6 chemicals 6 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 7.5-7.5 20°C eticlopride pubchem gtoplig chembl_ligand drugbank
Antagonist 2.9 Inactive 10.1126/SCIENCE.1197410 2010-11-03
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 Org27569 pubchem gtoplig chembl_ligand
CP55940 pubchem gtoplig chembl_ligand gtoplig
NAMAgonist 3.3 Inactive 10.1038/S41589-019-0387-2 2019-10-23
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
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
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
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 2021-05-26
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
AgonistPAM 3.0 Active 10.1038/S41586-020-2569-1 2020-09-09
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
BHFF pubchem
AgonistPAM 3.0 Active 10.1038/S41422-020-0350-5 2020-07-01
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
6D9H AA1R A1 Adenosine A (Rhodopsin) Human BaculovirusHi5Insect 2 chemicals 2 steps Cryo-EMVolta phase plate(FEI), FEI Titan Krios@300kV, Gatan K2 Summit direct electron camera , Gatan Quantum energy filter 6 chems 7.4-7.4 4°C adenosine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.6 Active 10.1038/S41586-018-0236-6 2018-06-20
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
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
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
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
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 Calcium pubchem
L-tryptophan pubchem gtoplig chembl_ligand drugbank drug_central pubchem
evocalcet pubchem gtoplig drug_central chembl_ligand drugbank
AgonistPAMPAM 2.5 Active 10.1038/S41586-021-03691-0 2021-06-30
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
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
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
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
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
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
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
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
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
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
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 2022-08-10
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
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
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
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 2021-02-17
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
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 10.1021/ACS.JMEDCHEM.7B01722 2018-03-07
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 10.1038/NATURE12735 2013-11-27
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
7F9Z GHSR ghrelin Ghrelin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A GHRP-6 pubchem gtoplig
Agonist 3.2 Active 2021-08-18
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
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
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
Agonist 3.0 Active 10.1038/S41422-020-00442-0 2020-12-16
6VMS DRD2 D2 Dopamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A bromocriptine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.8 Active 10.1038/S41586-020-2379-5 2020-06-17
5DYS OPSD Rhodopsin Opsins A (Rhodopsin) Bovine Stable_cellsHEK293S-GnTI-Mammalian 1 chemicals 1 steps vapour diffusionSitting drop 4 chems 4.5-4.5 20°C Retinal (all-trans) pubchem
Agonist 2.3 Active 10.15252/EMBR.201642671 2016-08-10
8DCS ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 4-{[(2S)-3-(tert-but... pubchem
Agonist 2.5 Active 10.1038/S41467-022-31823-1 2022-07-27
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
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 10.1038/NATURE22363 2017-05-24
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
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
Agonist 3.0 Active 10.1038/s41589-018-0145-x 2018-11-14
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
LY3154207 pubchem gtoplig chembl_ligand
AgonistAgonist 3.0 Active 10.1038/S41467-022-30929-W 2022-06-15
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
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
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 2021-11-17
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
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
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
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
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 JNJ-40411813 pubchem gtoplig chembl_ligand drugbank
eglumegad pubchem gtoplig chembl_ligand gtoplig
PAMAgonist 3.5 Intermediate 10.1038/S41586-021-03495-2 2021-06-23
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
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 2021-12-01
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
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
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
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
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
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
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 chembl_ligand pubchem
Agonist 3.3 Active 10.1038/S41467-022-30929-W 2022-06-15
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 2-phenylmelatonin pubchem
Agonist 3.3 Inactive 10.1107/S2052252519013137 2019-11-13
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
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
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
7DH5 ADRB3 β3 Adrenoceptors A (Rhodopsin) Dog N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A mirabegron pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.2 Active 10.1016/J.MOLCEL.2021.06.024 2021-08-04
6DRX 5HT2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A lisuride pubchem gtoplig chembl_ligand drugbank drug_central
Antagonist 3.1 Intermediate 10.1038/s41594-018-0116-7 2018-08-29
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
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
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
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
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 2022-03-23
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
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) gtoplig
Agonist 3.3 Active 10.1038/S41401-022-01032-Z 2022-12-21
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
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
Antagonist 2.6 Inactive 10.1038/S41422-022-00679-X 2022-08-03
6C1R C5AR1 C5a1 Complement peptide A (Rhodopsin) Human BaculovirusSf9Insect 4 chemicals 4 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 6.5-6.5 10°C PMX53 pubchem gtoplig chembl_ligand
avacopan pubchem gtoplig chembl_ligand drugbank
AntagonistNAM 2.2 Inactive 10.1038/S41594-018-0067-Z 2018-05-30
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
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
7TYN CALCR CT Calcitonin B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Calcitonin salmon pubchem
Agonist 2.6 Active 2022-03-30
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
Agonist 3.2 Active 10.1038/S41467-022-30929-W 2022-06-29
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
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
8EF5 OPRM μ Opioid A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A fentanyl pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.3 Active 10.1016/J.CELL.2022.09.041 2022-11-09
7VGZ MTR1A MT1 Melatonin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ramelteon pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.3 Active 2022-03-02
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 2022-08-03
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
6BQG 5HT2C 5-HT2C 5-Hydroxytryptamine A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phasemonoolein (9.9 MAG) 5 chems 6.0-6.0 20°C ergotamine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.0 Active 10.1016/j.cell.2018.01.001 2018-02-14
7V68 ACM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A LY2119620 pubchem gtoplig chembl_ligand
iperoxo pubchem gtoplig chembl_ligand
PAMAgonist 3.4 Active 2022-05-11
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 34793198 2021-12-01
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
7MTS GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem
2-methoxy-6-propyl-N... pubchem
AgonistAgo-PAM 3.2 Active 10.1038/S41586-021-03680-3 2021-07-07
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 N-[(1S)-3-{(3-exo)-3... pubchem
Antagonist 2.8 Inactive 10.1021/acs.jmedchem.8b01077 2018-10-24
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
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
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 CHEMBL410972 chembl_ligand pubchem pubchem
N-Tert-butyl-6,7-dic... pubchem
AgonistAgo-PAM 2.5 Active 10.1038/S41467-021-24058-Z 2021-07-14
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
7UM6 5HT5A 5-HT5A 5-Hydroxytryptamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A lisuride pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.8 Active 10.1038/S41594-022-00796-6 2022-07-20
7KI0 GLP1R GLP-1 Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A semaglutide pubchem gtoplig chembl_ligand drugbank pubchem
Agonist 2.5 Active 10.1016/J.CELREP.2021.109374 2021-08-04
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
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 2-methoxy-6-propyl-N... pubchem
L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem
Ago-PAMAgonist 3.3 Active 10.1038/S41586-021-03680-3 2021-07-07
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 10.1038/S41467-021-24438-5 2021-07-14
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
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
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 gtoplig pubchem
Antagonist 2.8 Inactive 10.1016/J.CELL.2018.12.011 2019-01-30
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
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
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
7D3S SCTR secretin Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A SECRETIN chembl_ligand pubchem
Agonist 2.9 Active 10.1016/J.BBRC.2020.08.042 2020-11-04
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
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
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
Agonist 3.2 Active 10.1016/J.CELL.2022.09.041 2022-11-09
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
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
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
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
7XRR OX2R OX2 Orexin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A lemborexant pubchem gtoplig chembl_ligand drug_central drugbank
Antagonist 2.9 Inactive 10.1016/J.STR.2022.11.001 2022-11-23
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
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 2022-03-02
3NY9 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human BaculovirusSf9Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 6 chems 7.5-8.0 20°C CHEMBL1233771 chembl_ligand pubchem
Inverse agonist 2.8 Inactive 10.1021/JA105108Q 2010-08-11
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
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
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
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 2021-12-01
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
Agonist 2.8 Active 2021-01-20
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
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
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
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 2021-10-06
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
6IGL EDNRB ETB Endothelin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A IRL 1620 pubchem gtoplig chembl_ligand gtoplig pubchem pubchem
Agonist (partial) 2.7 Inactive 10.1038/S41467-018-07094-0 2018-11-21
6H7M ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A levosalbutamol pubchem gtoplig chembl_ligand drug_central drugbank
Agonist 2.8 Active 10.1126/SCIENCE.AAU5595 2018-10-17
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
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
6TKO ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A arformoterol pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.3 Active 10.1038/S41586-020-2419-1 2020-06-17
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
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 Intermediate 10.1038/NATURE23448 2017-08-16
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 2021-11-03
6DRY 5HT2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A methylergonovine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 2.9 Intermediate 10.1038/s41594-018-0116-7 2018-08-29
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
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
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
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 2022-04-13
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
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
6TP3 OX1R OX1 Orexin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A daridorexant pubchem gtoplig chembl_ligand drugbank
Antagonist 3.0 Inactive 10.1021/acs.jmedchem.9b01787 2020-01-01
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
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
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
5TUD 5HT2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human BaculovirusSf21Insect 2 chemicals 2 steps in meso/LCPlipidic cubic phase (LCP)monopalmitolein (9.7 MAG) 6 chems 7.7-7.7 20°C ergotamine pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.0 Active 10.1073/PNAS.1700891114 2017-07-26
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
6ME7 MTR1B MT2 Melatonin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A 2-phenylmelatonin pubchem
Agonist 3.2 Inactive 10.1038/S41586-019-1144-0 2019-04-24
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
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
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
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
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
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
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
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
Antagonist 2.6 Inactive 10.1038/NATURE17188 2016-03-16
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
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 Intermediate 10.1038/NATURE13288 2014-04-30
6TPJ OX2R OX2 Orexin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A suvorexant pubchem gtoplig chembl_ligand drug_central drugbank
Antagonist 2.7 Inactive 10.1021/acs.jmedchem.9b01787 2020-01-01
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 Intermediate 2022-04-13
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
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
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
3RFM AA2AR A2A Adenosine A (Rhodopsin) Human BaculovirusSf9Insect 1 chemicals 1 steps vapour diffusionsitting drop 6 chems 8.0-8.8 4°C caffeine pubchem gtoplig chembl_ligand drugbank drug_central
Antagonist 3.6 Inactive 10.1016/J.STR.2011.06.014 2011-09-07
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
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
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 2020-04-01
7V9M GHRHR GHRH Glucagon B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Somatoliberin pubchem
Agonist 3.3 Active 2021-10-20
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 (4M)-6-bromo-4-(fura... pubchem
Antagonist 2.5 Inactive 10.1016/J.EJMECH.2022.114620 2022-08-10
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
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
7XP5 T2R46 TAS2R46 Taste 2 T (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
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
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
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
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
4OO9 GRM5 mGlu5 Metabotropic glutamate C (Glutamate) Human BaculovirusSf21Insect 1 chemicals 1 steps in meso/LCPlipidic cubic phase (LCP)monoolein (9.9 MAG) 4 chems 6.8-6.8 20°C MAVOGLURANT chembl_ligand pubchem
NAM 2.6 Inactive 10.1038/NATURE13396 2014-07-02
8E3Z VIPR1 VPAC1 VIP and PACAP B1 (Secretin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A Vasoactive intestina... pubchem
Agonist 2.7 Active 10.1038/S41467-022-34629-3 2022-11-23
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
6TOT OX1R OX1 Orexin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A lemborexant pubchem gtoplig chembl_ligand drug_central drugbank
Antagonist 2.2 Inactive 10.1021/acs.jmedchem.9b01787 2020-01-15
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
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
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
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
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
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
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 2022-05-04
7JNI AGTR2 AT2 Angiotensin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A olodanrigan pubchem gtoplig chembl_ligand drugbank
Antagonist 3.0 Active 2022-02-09
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
6OIK ACM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A iperoxo pubchem gtoplig chembl_ligand
LY2119620 pubchem gtoplig chembl_ligand
AgonistPAM 3.6 Active 10.1126/SCIENCE.AAW5188 2019-05-08
7PIU MC4R MC4 Melanocortin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A setmelanotide pubchem gtoplig drug_central chembl_ligand drugbank
Agonist 2.6 Active 10.1038/S41422-021-00569-8 2021-11-17
7VH0 MTR1B MT2 Melatonin A (Rhodopsin) Human N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A N/A ramelteon pubchem gtoplig chembl_ligand drugbank drug_central
Agonist 3.5 Active 2022-03-02
7FD8 GRM5 mGlu5 Metabotropic glutamate C (Glutamate) Human N/A