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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 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]