[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 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]