[Met]enkephalin [Ligand Id: 1614] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL13786 (Met-Enkephalin) |
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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 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]
