[Met]enkephalin [Ligand Id: 1614] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL13786 (Met-Enkephalin)
  • 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 in Rat [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 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]diprenorphine from human cloned delta opioid receptor B 8.7 pKi 2 nM Ki Bioorg Med Chem Lett (2007) 17: 2656-2660 [PMID:17350835]
ChEMBL Displacement of radiolabeled DPDPE-Cl from delta opioid receptor in Hartley guinea pig brain B 8.96 pKi 1.1 nM Ki Bioorg Med Chem Lett (2006) 16: 4291-4295 [PMID:16777416]
ChEMBL Agonist activity at delta receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation by bioluminescent assay F 8.19 pIC50 6.4 nM IC50 J Med Chem (2015) 58: 8573-8583 [PMID:26465170]
ChEMBL Agonist activity at human cloned delta opioid receptor assessed as stimulation of [35S]GTP-gamma-S binding F 7.33 pEC50 47 nM EC50 Bioorg Med Chem Lett (2007) 17: 2656-2660 [PMID:17350835]
ChEMBL Agonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assay F 8.99 pEC50 1.03 nM EC50 Bioorg Med Chem Lett (2009) 19: 2792-2795 [PMID:19362480]
ChEMBL Agonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assay F 8.99 pEC50 1.03 nM EC50 Bioorg Med Chem (2012) 20: 949-961 [PMID:22197670]
δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
GtoPdb - - 7.4 pIC50 - - - Proc Natl Acad Sci USA (1993) 90: 6736-40 [PMID:8393575]
ChEMBL Inhibitory potency against delta Opioid receptor delta 1 in longitudinal muscle preparation of mouse vas deferens B 7.89 pIC50 13 nM IC50 J Med Chem (1981) 24: 1119-1124 [PMID:6276540]
δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
ChEMBL Inhibition of [3H]DTLET binding torat brain membrane Opioid receptor delta 1 B 8.14 pKi 7.3 nM Ki J Med Chem (1988) 31: 1891-1897 [PMID:2845081]
ChEMBL Compound was evaluated for its binding affinity against enkephalin delta receptor using [3H]DPDPE as ligand in rat cerebrum in vitro B 9 pIC50 1 nM IC50 Bioorg Med Chem Lett (1992) 2: 219-222
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Displacement of [3H]diprenorphine from human cloned kappa opioid receptor B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2007) 17: 2656-2660 [PMID:17350835]
κ receptor in Rat [GtoPdb: 318] [UniProtKB: P34975]
GtoPdb - - 6 pKi - - - Proc Natl Acad Sci USA (1993) 90: 9954-8 [PMID:8234341]
Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
ChEMBL Displacement of radiolabeled U69593 from kappa1 opioid receptor in Hartley guinea pig brain B 5.35 pKi 4467 nM Ki Bioorg Med Chem Lett (2006) 16: 4291-4295 [PMID:16777416]
ChEMBL Compound was evaluated for its binding affinity against enkephalin kappa receptor using [3H]U-69593 as ligand in guinea pig cerebrum in vitro B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (1992) 2: 219-222
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Displacement of [3H]diprenorphine from human cloned mu opioid receptor B 7.72 pKi 19 nM Ki Bioorg Med Chem Lett (2007) 17: 2656-2660 [PMID:17350835]
ChEMBL Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation by bioluminescent assay F 7.89 pIC50 13 nM IC50 J Med Chem (2015) 58: 8573-8583 [PMID:26465170]
ChEMBL Agonist activity at human cloned mu opioid receptor assessed as stimulation of [35S]GTPgammaS binding F 6.21 pEC50 620 nM EC50 Bioorg Med Chem Lett (2007) 17: 2656-2660 [PMID:17350835]
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
ChEMBL Inhibition of [3H]DAGO binding to rat brain membrane Opioid receptor mu 1 B 7.56 pKi 27.5 nM Ki J Med Chem (1988) 31: 1891-1897 [PMID:2845081]
ChEMBL Compound was evaluated for binding affinity towards mu-specific opiate receptor from combinatorial peptoid library B 7.7 pKi 20 nM Ki J Med Chem (1994) 37: 2678-2685 [PMID:8064796]
GtoPdb - - 9.2 pKi - - - Mol Pharmacol (1994) 45: 330-4 [PMID:8114680]
ChEMBL Compound was evaluated for its binding affinity against enkephalin mu receptor using [3H]PL-017 as ligand in rat cerebrum in vitro B 8.7 pIC50 2 nM IC50 Bioorg Med Chem Lett (1992) 2: 219-222
ChEMBL Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP F 6.51 pEC50 309.03 nM EC50 J Med Chem (2013) 56: 5964-5973 [PMID:23822516]
ChEMBL Agonist activity at mu opioid receptor in rat brain membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins in presence of GDP F 6.52 pEC50 304 nM EC50 J Med Chem (2013) 56: 5964-5973 [PMID:23822516]
Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
ChEMBL Displacement of radiolabeled DAMGO from mu opioid receptor in Hartley guinea pig brain B 8.16 pKi 6.9 nM Ki Bioorg Med Chem Lett (2006) 16: 4291-4295 [PMID:16777416]
ChEMBL Inhibitory potency against Opioid receptor mu 1 in longitudinal muscle preparation of guinea pig ileum B 6.7 pIC50 200 nM IC50 J Med Chem (1981) 24: 1119-1124 [PMID:6276540]
Mu opioid receptor-like OR2 in Danio rerio (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3611961] [UniProtKB: Q98UH1]
ChEMBL Displacement of [3H]DPN from zebrafish mu opioid receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method B 6.16 pKi 684 nM Ki Bioorg Med Chem (2017) 25: 2260-2265 [PMID:28284867]
Nociceptin receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5492] [UniProtKB: P47748]
ChEMBL Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain B 6.56 pKi 277 nM Ki Bioorg Med Chem Lett (2006) 16: 4291-4295 [PMID:16777416]
Opioid receptor, delta 1b in Danio rerio (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105711] [UniProtKB: B3DH72]
ChEMBL Displacement of [3H]DPN from zebrafish delta 1b opioid receptor expressed in HEK293 cell membranes after 4 hrs by scintillation counting method B 7.35 pKi 45 nM Ki Bioorg Med Chem (2017) 25: 2260-2265 [PMID:28284867]

ChEMBL data shown on this page come from version 32:

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]