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ChEMBL ligand: CHEMBL982 (JF-1, JKB-121, Nalmefene, Nalmefene hydrochloride dihydrate, Nalmefene hydrochloride hydrate, Nalmetrene, ORF 1167, ORF-1167, ORF 11676, ORF-11676, Revex, Selincro, SRD-174, SRD174) |
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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 | Activity at human delta opioid receptor by [35S]GTPgammaS binding assay | F | 9.04 | pKd | 0.91 | nM | Kd | J Med Chem (2008) 51: 1913-1924 [PMID:18298057] |
ChEMBL | Displacement of [3H]naltrindole from human delta-opioid receptor expressed in CHO cell membranes after 3 hrs by scintillation counting | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2016) 59: 8712-8756 [PMID:27299736] |
ChEMBL | Displacement of [3H]DPDPE from human delta opioid receptor expressed in CHO cells | B | 7.88 | pKi | 13.26 | nM | Ki | J Med Chem (2008) 51: 1913-1924 [PMID:18298057] |
ChEMBL | Displacement of [3H]DPDPE from delta opioid receptor expressed in HEK293 cells by visible spectrophotometry | B | 7.88 | pKi | 13.26 | nM | Ki | Bioorg Med Chem (2009) 17: 6671-6681 [PMID:19683449] |
ChEMBL | Displacement of [3H]Naltrindole form human delta opioid receptor expressed in CHO cells | B | 8.03 | pKi | 9.3 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293] |
GtoPdb | - | - | 8.1 | pKi | - | - | - | NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407] |
δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533] | ||||||||
ChEMBL | Binding affinity towards delta-opioid receptor by displacement of [3H]DADL in rat brain homogenates | B | 8.47 | pKi | 3.4 | nM | Ki | J Med Chem (1993) 36: 2842-2850 [PMID:8410999] |
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
ChEMBL | Displacement of [3H]U69593 from human kappa opioid receptor expressed in CHO cells | B | 8.99 | pKi | 1.03 | nM | Ki | J Med Chem (2008) 51: 1913-1924 [PMID:18298057] |
ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor expressed in HEK293 cells by visible spectrophotometry | B | 8.99 | pKi | 1.03 | nM | Ki | Bioorg Med Chem (2009) 17: 6671-6681 [PMID:19683449] |
GtoPdb | - | - | 9.5 | pKi | - | - | - | NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407] |
ChEMBL | Displacement of [3H]U69593 form human kappa opioid receptor expressed in CHO cells | B | 9.92 | pKi | 0.12 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293] |
ChEMBL | Displacement of [3H]U69,593 from human kappa-opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting | B | 10.08 | pKi | 0.08 | nM | Ki | J Med Chem (2016) 59: 8712-8756 [PMID:27299736] |
Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
ChEMBL | Binding affinity towards kappa opioid receptor by displacement of [3H]EKC in guinea pig cortical tissue | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (1993) 36: 2842-2850 [PMID:8410999] |
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
ChEMBL | Activity at human mu opioid receptor by [35S]GTPgammaS binding assay | F | 9.53 | pKd | 0.3 | nM | Kd | J Med Chem (2008) 51: 1913-1924 [PMID:18298057] |
ChEMBL | Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells | B | 9.04 | pKi | 0.91 | nM | Ki | J Med Chem (2008) 51: 1913-1924 [PMID:18298057] |
ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor expressed in HEK293 cells by visible spectrophotometry | B | 9.04 | pKi | 0.91 | nM | Ki | Bioorg Med Chem (2009) 17: 6671-6681 [PMID:19683449] |
ChEMBL | Displacement of [3H]DAMGO form human mu opioid receptor expressed in CHO cells | B | 9.36 | pKi | 0.44 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293] |
GtoPdb | - | - | 9.5 | pKi | - | - | - | NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407] |
ChEMBL | Displacement of [3H]DAMGO from human mu-opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting | B | 9.62 | pKi | 0.24 | nM | Ki | J Med Chem (2016) 59: 8712-8756 [PMID:27299736] |
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
ChEMBL | Binding affinity towards mu-opioid receptor by the displacement of [3H]Nal in rat brain homogenates | B | 9.54 | pKi | 0.29 | nM | Ki | J Med Chem (1993) 36: 2842-2850 [PMID:8410999] |
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]