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]-DPDPE from Wistar rat delta opioid receptor incubated for 3 hrs by liquid scintillation counting method B 5 pKi >10000 nM Ki Bioorg Med Chem (2020) 28: 115438-115438 [PMID:32199689]
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 DOR in Wistar rat brain membranes measured after 3 hrs by scintillation counting method B 5.21 pKi 6105 nM Ki J Med Chem (2021) 64: 16801-16819 [PMID:34781680]
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]U69593 from KOP (unknown origin) stably expressed in HEK293 cells by liquid scintillation counter analysis B 5 pKi >10000 nM Ki J Med Chem (2022) 65: 1612-1661 [PMID:34995453]
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]-U69,593 from Wistar rat kappa opioid receptor incubated for 1.5 hrs by liquid scintillation counting method B 5 pKi >10000 nM Ki Bioorg Med Chem (2020) 28: 115438-115438 [PMID:32199689]
ChEMBL Displacement of [3H]-U69593 from KOR in Wistar rat brain membranes measured after 1 hr by scintillation counting method B 5 pKi >10000 nM Ki J Med Chem (2021) 64: 16801-16819 [PMID:34781680]
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 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 human cloned mu-opioid receptor by radioligand binding assay B 8.59 pKi 2.6 nM Ki J Med Chem (2022) 65: 13483-13504 [PMID:36206553]
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 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 (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method F 7.21 pEC50 61 nM EC50 Bioorg Med Chem (2020) 28: 115438-115438 [PMID:32199689]
ChEMBL Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISA F 7.68 pEC50 21.1 nM EC50 J Med Chem (2021) 64: 16801-16819 [PMID:34781680]
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 F 7.84 pEC50 14.4 nM EC50 Bioorg Med Chem Lett (2015) 25: 5393-5397 [PMID:26403932]
ChEMBL Agonist activity at human MOP assessed as forskolin stimulated cAMP accumulation F 7.85 pEC50 14 nM EC50 J Med Chem (2022) 65: 1612-1661 [PMID:34995453]
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 Displacement of [3H]-DAMGO from Wistar rat mu opioid receptor incubated for 1 hr by liquid scintillation counting method B 7.75 pKi 17.8 nM Ki Bioorg Med Chem (2020) 28: 115438-115438 [PMID:32199689]
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 MOR in Wistar rat brain membranes measured after 1 hr by scintillation counting method B 8.33 pKi 4.63 nM Ki J Med Chem (2021) 64: 16801-16819 [PMID:34781680]
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 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 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 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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]