5'-guanidinonaltrindole [Ligand Id: 1669] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL485832 (5`-Guanidinonaltrindole, 5'-Guanidinonaltrindole, 5'-Guanidinylnaltrindole, C5'-Guanidinyl Naltrindole, Guanidinonaltrindole)
  • 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/Kappa opioid receptor in Rat [ChEMBL: CHEMBL3614] [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]
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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 Antagonistic activity against human cloned Opioid receptor delta 1 using DPDPE in [35S]GTP-gamma-S, assay F 7.81 pKd 15.49 nM Kd J Med Chem (2003) 46: 3127-3137 [PMID:12825951]
δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
ChEMBL Displacement of [3H]- diprenorphine from delta receptor expressed in HEK 293 cells B 7.34 pKi 46.2 nM Ki J Med Chem (2001) 44: 857-862 [PMID:11300867]
ChEMBL Binding affinity towards mouse delta-opioid receptor was determined using [3H]diprenorphine as radioligand B 7.61 pKi 24.8 nM Ki J Med Chem (2001) 44: 2073-2079 [PMID:11405645]
ChEMBL Displacement of [3H]- diprenorphine from delta-W284E-receptor expressed in HEK 293 cells B 8.96 pKi 1.1 nM Ki J Med Chem (2001) 44: 857-862 [PMID:11300867]
δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
ChEMBL Inhibition of [3H]-DADLE binding to Opioid receptor delta 1 of rat brain tissue B 7.15 pKi 70 nM Ki J Med Chem (2003) 46: 3127-3137 [PMID:12825951]
ChEMBL Binding affinity on HEK293 cells transiently transfected with plasmids encoding the rat Opioid receptor delta 1 B 7.34 pKi 46.2 nM Ki J Med Chem (2000) 43: 2759-2769 [PMID:10893314]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Antagonistic activity against human cloned kOpioid receptor kappa 1 using U69,593 in [35S]GTP-gamma-S, assay F 10.4 pKd 0.04 nM Kd J Med Chem (2003) 46: 3127-3137 [PMID:12825951]
ChEMBL Displacement of [125I]-IBNalA from KOR-1 expressed in CHO cells B 9.72 pKi 0.19 nM Ki Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410]
ChEMBL Displacement of [125I]-IBNtxA from KOR-1 expressed in CHO cells B 9.82 pKi 0.15 nM Ki Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410]
GtoPdb - - 9.9 pKi - - - Binding and activity of opioid ligands at the cloned human delta, mu and kappa receptors.. The Delta Receptor (2003);
Eur J Pharmacol (2000) 396: 49-52 [PMID:10822054];
J Med Chem (2000) 43: 2759-69 [PMID:10893314]
κ receptor/Kappa opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975]
ChEMBL Mutant factor of the compound against kappa[E297K] with Opioid receptor kappa 1 for binding affinity. B 7.89 pKi 12.9 nM Ki J Med Chem (1998) 41: 4911-4914 [PMID:9836606]
ChEMBL Effect on binding to kappa(Glu297Ala) opioid receptor, using [3H]diprenorphine in transiently expressed rat HEK293 cells B 8.41 pKi 3.93 nM Ki J Med Chem (2001) 44: 2073-2079 [PMID:11405645]
ChEMBL Displacement of [3H]diprenorphine from k-E297A-receptor expressed in HEK 293 cells B 8.41 pKi 3.9 nM Ki J Med Chem (2001) 44: 857-862 [PMID:11300867]
ChEMBL Effect on binding to wild-type opioid receptor kappa 1 using [3H]diprenorphine in transiently expressed rat HEK293 cells B 9.68 pKi 0.21 nM Ki J Med Chem (2001) 44: 2073-2079 [PMID:11405645]
ChEMBL Binding affinity on HEK293 cells transiently transfected with plasmids encoding the rat Opioid receptor kappa 1 B 9.74 pKi 0.18 nM Ki J Med Chem (2000) 43: 2759-2769 [PMID:10893314]
ChEMBL Displacement of [3H]diprenorphine from opioid receptor kappa 1 expressed in HEK 293 cells B 9.74 pKi 0.18 nM Ki J Med Chem (2001) 44: 857-862 [PMID:11300867]
ChEMBL Binding affinity towards rat opioid receptor kappa 1 was determined using [3H]diprenorphine radioligand B 9.85 pKi 0.14 nM Ki J Med Chem (2001) 44: 2073-2079 [PMID:11405645]
ChEMBL Effect on binding affinity of mutational exchange of Glu297 in the Opioid receptor kappa 1 in transiently expressed rat cos-7 cells activity expressed as binding affinity. B 10.05 pKi 0.09 nM Ki J Med Chem (1998) 41: 4911-4914 [PMID:9836606]
ChEMBL Mutant factor of the compound against mu-[K303E] with Opioid receptor kappa 1 for binding affinity B 10.22 pKi 0.06 nM Ki J Med Chem (1998) 41: 4911-4914 [PMID:9836606]
ChEMBL Displacement of [3H]diprenorphine from k-Y312A-receptor expressed in HEK 293 cells B 10.52 pKi 0.03 nM Ki J Med Chem (2001) 44: 857-862 [PMID:11300867]
Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
ChEMBL Inhibition of [3H]U-69593 binding to Opioid receptor kappa 1 of guinea pig brain B 9.74 pKi 0.18 nM Ki J Med Chem (2003) 46: 3127-3137 [PMID:12825951]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Antagonistic activity against human cloned Opioid receptor mu 1 using DPDPE in [35S]GTP-gamma-S, assay F 8.49 pKd 3.24 nM Kd J Med Chem (2003) 46: 3127-3137 [PMID:12825951]
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
ChEMBL Binding affinity towards rat mu-opioid receptor was determined using [3H]diprenorphine as radioligand B 7 pKi 99.7 nM Ki J Med Chem (2001) 44: 2073-2079 [PMID:11405645]
ChEMBL Inhibition of [3H]DAMGO binding to Opioid receptor mu 1 of rat brain tissue B 7.43 pKi 36.9 nM Ki J Med Chem (2003) 46: 3127-3137 [PMID:12825951]
ChEMBL Displacement of [3H]- diprenorphine from mu-receptor expressed in HEK 293 cells B 7.65 pKi 22.5 nM Ki J Med Chem (2001) 44: 857-862 [PMID:11300867]
ChEMBL Binding affinity on HEK293 cells transiently transfected with plasmids encoding the rat Opioid receptor mu 1 B 7.65 pKi 22.5 nM Ki J Med Chem (2000) 43: 2759-2769 [PMID:10893314]
ChEMBL Effect on binding affinity of mutational exchange of Lys303 in the Opioid receptor mu 1 in transiently expressed rat cos-7 cells activity expressed as binding affinity. B 8.03 pKi 9.23 nM Ki J Med Chem (1998) 41: 4911-4914 [PMID:9836606]
ChEMBL Displacement of [3H]- diprenorphine from mu-W318A-receptor expressed in HEK 293 cells B 9.3 pKi 0.5 nM Ki J Med Chem (2001) 44: 857-862 [PMID:11300867]
ChEMBL Displacement of [3H]- diprenorphine from mu-K303E-receptor expressed in HEK 293 cells B 10.05 pKi 0.09 nM Ki J Med Chem (2001) 44: 857-862 [PMID:11300867]

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]