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ChEMBL ligand: CHEMBL485832 (5'-Guanidinonaltrindole, 5`-Guanidinonaltrindole, 5'-Guanidinylnaltrindole, C5'-Guanidinyl Naltrindole, Guanidinonaltrindole) |
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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 | 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 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]