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ChEMBL ligand: CHEMBL316446 (Endomorphin 1) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]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 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 (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] |
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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]