endomorphin-1 [Ligand Id: 1623] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL316446 (Endomorphin 1)
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
  • δ receptor/Delta opioid receptor in Mouse [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
  • δ receptor/Delta opioid receptor in Rat [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
  • κ receptor/Kappa opioid receptor in Rat [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975]
  • Kappa opioid receptor in Guinea pig [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
  • μ receptor/Mu opioid receptor in Mouse [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866]
  • μ receptor/Mu opioid receptor in Rat [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
  • Mu opioid receptor in Guinea pig [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL Displacement of [3H]DPDPE from Myc-tagged delta opioid receptor expressed in HEK293 cells after 60 mins by liquid scintillation counter B 5.22 pKi 6080 nM Ki J. Med. Chem. (2012) 55: 6224-6236 [PMID:22724433]
ChEMBL Displacement of [3H]-DPDPE from delta opioid receptor (unknown origin) transfected in HEK293 cells B 5.22 pKi 6080 nM Ki Bioorg. Med. Chem. Lett. (2015) 25: 5393-5397 [PMID:26403932]
ChEMBL Displacement of [3H]DPDPE from human delta opioid receptor expressed in mouse HN9.10 cell membranes B 5.29 pKi 5100 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 3434-3437 [PMID:23623418]
ChEMBL Displacement of [3H]DPDPE from delta-opioid receptor expressed in CHOK1 cells after overnight incubation by scintillation proximity assay B 5.56 pKi 2765 nM Ki J. Med. Chem. (2012) 55: 5859-5867 [PMID:22680612]
ChEMBL Displacement of [3H]DPDPE from DOP receptor expressed in CHO-K1 cells after overnight incubation by beta counting method B 5.56 pKi 2765 nM Ki Bioorg. Med. Chem. (2012) 20: 6335-6343 [PMID:23022277]
GtoPdb - - 6.1 pKi - - - FEBS Lett (1998) 439: 152-6 [PMID:9849897]
ChEMBL Activity at delta opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay F 6.03 pEC50 932 nM EC50 J. Med. Chem. (2007) 50: 512-520 [PMID:17266203]
δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
ChEMBL Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically evoked muscle contractions F 6.55 pIC50 283 nM IC50 Bioorg. Med. Chem. (2007) 15: 1237-1251 [PMID:17142049]
ChEMBL Agonist activity at delta opioid receptor in Kunming mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction F 7.52 pIC50 30.4 nM IC50 J. Med. Chem. (2012) 55: 6224-6236 [PMID:22724433]
ChEMBL Agonist activity at delta opioid receptor by inhibition of electrically evoked muscle contraction in isolated mouse vas deferens F 7.58 pIC50 26.3 nM IC50 J. Med. Chem. (2007) 50: 512-520 [PMID:17266203]
ChEMBL Inhibition of delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction B 7.59 pIC50 26 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 3434-3437 [PMID:23623418]
δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
ChEMBL Displacement of [3H]Ile5,6-deltorphin II from opioid receptor delta 1 of rat brain membranes B 5.19 pKi 6390 nM Ki J. Med. Chem. (2004) 47: 735-743 [PMID:14736254]
ChEMBL Displacement of [3H]DPDPE from delta-opioid receptor in Wistar rat brain membrane after 3 hrs by microbeta scintillation counting method B 5.24 pKi 5775 nM Ki Bioorg Med Chem Lett (2017) 27: 2119-2123 [PMID:28377055]
ChEMBL Displacement of [3H]-DPDPE from delta opioid receptor in Wistar rat brain membranes preincubated for 3 hrs measured after 1 hr by scintillation counting method B 5.29 pKi 5093 nM Ki Bioorg Med Chem Lett (2017) 27: 1557-1560 [PMID:28256374]
ChEMBL Displacement of [3H][Ile5,6]deltorphin2 from delta opioid receptor in rat brain membrane homogenate by liquid scintillation counting B 5.38 pKi 4169 nM Ki J. Med. Chem. (2011) 54: 1462-1472 [PMID:21287991]
ChEMBL Displacement of [3H]Ile5,6deltorphin-2 from delta opioid receptor in Wistar rat brain B 5.72 pKi 1909 nM Ki J. Med. Chem. (2008) 51: 4270-4279 [PMID:18572932]
ChEMBL Displacement of [3H]deltorphin 2 from delta opioid receptor in rat brain P2 synaptosome B 5.76 pKi 1750 nM Ki Bioorg. Med. Chem. (2007) 15: 1237-1251 [PMID:17142049]
ChEMBL Displacement of [3H]DAMGO from delta opioid receptor in rat brain membrane B 5.89 pKi 1280 nM Ki Bioorg. Med. Chem. (2008) 16: 6286-6296 [PMID:18468445]
ChEMBL Displacement of [3H]DPDPE from rat cortex delta opioid receptor after 2.5 hrs by liquid scintillation counting analysis B 6.14 pKi 729 nM Ki Eur. J. Med. Chem. (2015) 92: 270-281 [PMID:25559207]
ChEMBL Displacement of [3H]DPDPE from rat cortical DOR after 2.5 hrs by liquid scintillation counting method B 6.24 pKi 575 nM Ki J. Med. Chem. (2016) 59: 1239-1245 [PMID:26789491]
ChEMBL Displacement of [3H]deltorphin2 from delta opioid receptor in rat brain membrane B 5.45 pIC50 3580 nM IC50 Bioorg. Med. Chem. (2007) 15: 3883-3888 [PMID:17395470]
ChEMBL Displacement of [3H][Ile5,6]deltorphin-2 from delta opioid receptor in Wistar rat brain membrane B 6 pIC50 >1000 nM IC50 Bioorg. Med. Chem. (2009) 17: 3789-3794 [PMID:19435668]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Displacement of [3H]diprenorphine from kappa-opioid receptor expressed in CHOK1 cells after overnight incubation by scintillation proximity assay B 5.69 pKi 2048 nM Ki J. Med. Chem. (2012) 55: 5859-5867 [PMID:22680612]
κ receptor/Kappa opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975]
ChEMBL Displacement of [3H]dynorphin A from Opioid receptor kappa 1 of rat brain membranes (DAMGO/DADLE quenching of mu/delta receptor binding) B 7.28 pKi 52.7 nM Ki J. Med. Chem. (2004) 47: 735-743 [PMID:14736254]
Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
ChEMBL Displacement of [3H]U69,593 from guinea pig KOR after 2 hrs by liquid scintillation counting method B 5.3 pKi 5069 nM Ki J. Med. Chem. (2016) 59: 1239-1245 [PMID:26789491]
ChEMBL Displacement of [3H]U69,593 from guinea pig cortex/cerebella kappa opioid receptor after 2 hrs by liquid scintillation counting analysis B 5.63 pKi 2354 nM Ki Eur. J. Med. Chem. (2015) 92: 270-281 [PMID:25559207]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
GtoPdb - - 8.3 pKi 5.01 nM Ki FEBS Lett (1998) 439: 152-6 [PMID:9849897];
Nature (1997) 386: 499-502 [PMID:9087409]
ChEMBL Binding affinity to human mu opioid receptor B 8.34 pKi 4.55 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 5387-5391 [PMID:19679474]
ChEMBL Displacement of [3H]-DAMGO from mu opioid receptor (unknown origin) transfected in HEK293 cells B 8.59 pKi 2.6 nM Ki Bioorg. Med. Chem. Lett. (2015) 25: 5393-5397 [PMID:26403932]
ChEMBL Displacement of [3H]DAMGO from FLAG-tagged mu opioid receptor expressed in HEK293 cells after 60 mins by liquid scintillation counter B 8.59 pKi 2.6 nM Ki J. Med. Chem. (2012) 55: 6224-6236 [PMID:22724433]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in human SH-SY5Y cells B 8.84 pKi 1.45 nM Ki Bioorg. Med. Chem. (2008) 16: 4341-4346 [PMID:18329886]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in human SHSY5Y cells B 8.95 pKi 1.11 nM Ki Bioorg. Med. Chem. (2008) 16: 6286-6296 [PMID:18468445]
ChEMBL Displacement of [3H]DAMGO from MOP receptor expressed in CHO-K1 cells after overnight incubation by beta counting method B 9.12 pKi 0.76 nM Ki Bioorg. Med. Chem. (2012) 20: 6335-6343 [PMID:23022277]
ChEMBL Displacement of [3H]DAMGO from mu-opioid receptor expressed in CHOK1 cells after overnight incubation by scintillation proximity assay B 9.54 pKi 0.29 nM Ki J. Med. Chem. (2012) 55: 5859-5867 [PMID:22680612]
ChEMBL Agonist activity at mu-opioid receptor in human SH-SY5Y cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by immunoassay F 7.18 pIC50 65.4 nM IC50 J. Med. Chem. (2012) 55: 5859-5867 [PMID:22680612]
ChEMBL Agonist activity at mu opioid receptor in human SHSY5Y cells assessed as inhibition of forskolin-stimulated cAMP production F 7.85 pIC50 14 nM IC50 Bioorg. Med. Chem. (2008) 16: 6286-6296 [PMID:18468445]
ChEMBL Agonist activity at MOP receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins F 8.49 pIC50 3.2 nM IC50 Bioorg. Med. Chem. (2012) 20: 6335-6343 [PMID:23022277]
ChEMBL Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter F 7.84 pEC50 14.4 nM EC50 J. Med. Chem. (2012) 55: 6224-6236 [PMID:22724433]
ChEMBL Agonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production B 7.84 pEC50 14.4 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 5393-5397 [PMID:26403932]
μ receptor/Mu opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866]
ChEMBL Inhibition of Mu opioid receptor of mouse vas deferens B 7.44 pIC50 36.3 nM IC50 J. Med. Chem. (2004) 47: 735-743 [PMID:14736254]
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
ChEMBL Binding affinity towards Opioid receptor mu 1 B 7.95 pKi 11.1 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 2755-2758 [PMID:11133084]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane by liquid scintillation counting B 7.97 pKi 10.7 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 4115-4118 [PMID:19560919]
ChEMBL Displacement of [3H]DAMGO from mu-opioid receptor in Wistar rat brain membrane after 1 hr by microbeta scintillation counting method B 8.21 pKi 6.19 nM Ki Bioorg Med Chem Lett (2017) 27: 2119-2123 [PMID:28377055]
ChEMBL Displacement of [3H]DAMGO from rat mu opioid receptor expressed in mouse HN9.10 cell membranes B 8.34 pKi 4.6 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 3434-3437 [PMID:23623418]
ChEMBL Displacement of [3H]-DAMGO from mu opioid receptor in Wistar rat brain membranes preincubated for 1 hr measured after 1hr by scintillation counting method B 8.34 pKi 4.53 nM Ki Bioorg Med Chem Lett (2017) 27: 1557-1560 [PMID:28256374]
ChEMBL Displacement of [3H]DAMGO from Opioid receptor mu 1 of rat brain membranes B 8.38 pKi 4.21 nM Ki J. Med. Chem. (2004) 47: 735-743 [PMID:14736254]
ChEMBL Displacement of [3H]DAMGO from rat cortex mu opioid receptor after 30 mins by liquid scintillation counting analysis B 8.4 pKi 4 nM Ki Eur. J. Med. Chem. (2015) 92: 270-281 [PMID:25559207]
ChEMBL Displacement of [3H]endomorphin-2 from mu opioid receptor in Wistar rat brain B 8.68 pKi 2.1 nM Ki J. Med. Chem. (2008) 51: 4270-4279 [PMID:18572932]
ChEMBL Displacement of [3H]endomorphin-2 from Opioid receptor mu 1 of rat brain membranes B 8.79 pKi 1.62 nM Ki J. Med. Chem. (2004) 47: 735-743 [PMID:14736254]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane homogenate by liquid scintillation counting B 8.8 pKi 1.6 nM Ki J. Med. Chem. (2011) 54: 1462-1472 [PMID:21287991]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane B 8.94 pKi 1.15 nM Ki Bioorg. Med. Chem. (2008) 16: 6286-6296 [PMID:18468445]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain B 9.13 pKi 0.74 nM Ki J. Med. Chem. (2008) 51: 4270-4279 [PMID:18572932]
ChEMBL Displacement of [3H]DAMGO from rat cortical MOR by liquid scintillation counting method B 9.15 pKi 0.7 nM Ki J. Med. Chem. (2016) 59: 1239-1245 [PMID:26789491]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in rat brain P2 synaptosome B 9.25 pKi 0.56 nM Ki Bioorg. Med. Chem. (2007) 15: 1237-1251 [PMID:17142049]
ChEMBL Inhibition of [3H]-DAMGO binding to Opioid receptor mu 1 of rat brain membranes B 9.8 pKi 0.16 nM Ki J. Med. Chem. (2004) 47: 5198-5203 [PMID:15456262]
ChEMBL Binding affinity towards Opioid receptor mu 1 by displacing [3H]DAMGO in rat brain membranes. B 9.8 pKi 0.16 nM Ki J. Med. Chem. (2002) 45: 2571-2578 [PMID:12036366]
ChEMBL Concentration required for inhibition of [3H]DAMGO binding to Opioid receptor mu 1 in rat brain membranes B 7.25 pIC50 56 nM IC50 Bioorg. Med. Chem. Lett. (2000) 10: 2755-2758 [PMID:11133084]
ChEMBL Displacement of [3H]DAGO from mu opioid receptor in rat brain membrane B 8.72 pIC50 1.89 nM IC50 Bioorg. Med. Chem. (2007) 15: 3883-3888 [PMID:17395470]
ChEMBL Inhibitory activity against [3H]DAMGO binding to Opioid receptor mu 1 in rat brain membranes B 9.3 pIC50 0.5 nM IC50 J. Med. Chem. (2002) 45: 2571-2578 [PMID:12036366]
ChEMBL Inhibition of [3H]DAMGO binding to Opioid receptor mu 1 of rat brain membranes B 9.3 pIC50 0.5 nM IC50 J. Med. Chem. (2004) 47: 5198-5203 [PMID:15456262]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membrane B 9.37 pIC50 0.43 nM IC50 Bioorg. Med. Chem. (2009) 17: 3789-3794 [PMID:19435668]
ChEMBL Agonist activity at mu opioid receptor in rat brain membrane by [35S]GTPgammaS binding assay F 6.78 pEC50 166 nM EC50 J. Med. Chem. (2011) 54: 1462-1472 [PMID:21287991]
ChEMBL Activity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS binding F 6.98 pEC50 104 nM EC50 J. Med. Chem. (2008) 51: 4270-4279 [PMID:18572932]
Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
ChEMBL Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated contraction F 4.55 pIC50 28000 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 4115-4118 [PMID:19560919]
ChEMBL Agonist activity at mu opioid receptor by inhibition of electrically evoked muscle contraction in guinea pig ileum F 7.76 pIC50 17.2 nM IC50 J. Med. Chem. (2007) 50: 512-520 [PMID:17266203]
ChEMBL Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction F 7.85 pIC50 14.1 nM IC50 J. Med. Chem. (2012) 55: 6224-6236 [PMID:22724433]
ChEMBL Inhibition of mu opioid receptor in guinea pig ileum/longitudinal muscle with myenteric plexus assessed as inhibition of electrically-stimulated muscle contraction B 7.96 pIC50 11 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 3434-3437 [PMID:23623418]
ChEMBL Inhibition of Opioid receptor mu 1 of guinea pig ileum B 8 pIC50 10.1 nM IC50 J. Med. Chem. (2004) 47: 735-743 [PMID:14736254]
ChEMBL Agonist activity at mu opioid receptor in Hartley guinea pig intestine assessed as inhibition of electrically evoked myenteric plexus longitudinal muscle contractions F 8.39 pIC50 4.03 nM IC50 Bioorg. Med. Chem. (2007) 15: 1237-1251 [PMID:17142049]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]