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ChEMBL ligand: CHEMBL415247 (Jdtic, Rti-jdtic) |
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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 | Displacement of [3H]diprenorphine from human opioid delta receptor expressed in HEK293 cells after 120 mins by scintillation counting | B | 6.73 | pKi | 188 | nM | Ki | J Med Chem (2011) 54: 8000-8012 [PMID:21958337] |
ChEMBL | Displacement of [3H]DADLE from human recombinant delta opioid receptor expressed in HEK cells after 60 mins | B | 7.44 | pKi | 36.11 | nM | Ki | Eur J Med Chem (2015) 90: 742-750 [PMID:25513968] |
ChEMBL | Binding affinity towards human cloned Opioid receptor delta 1 using [3H]Cl-DPDPE | B | 7.53 | pKi | 29.6 | nM | Ki | J Med Chem (2003) 46: 3127-3137 [PMID:12825951] |
ChEMBL | Agonist activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | F | 6.42 | pEC50 | 380 | nM | EC50 | J Med Chem (2010) 53: 5290-5301 [PMID:20568781] |
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 | 6.52 | pKi | 301 | nM | Ki | J Med Chem (2003) 46: 3127-3137 [PMID:12825951] |
ChEMBL | Binding affinity of compound for opioid receptor delta 1 was determined using [3H]DADLE as radioligand from rat brain tissue | B | 6.52 | pKi | 301 | nM | Ki | J Med Chem (2004) 47: 1070-1073 [PMID:14761209] |
ChEMBL | Displacement of [3H]DADLE from delta-opioid receptor in rat brain membranes after 2 hrs | B | 6.52 | pKi | >300 | nM | Ki | Eur J Med Chem (2017) 141: 632-647 [PMID:29107424] |
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Displacement of [3H]-astemizole from human ERG | B | 5.05 | pKi | 8820 | nM | Ki | Bioorg Med Chem (2015) 23: 6379-6388 [PMID:26342544] |
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
ChEMBL | Antagonist activity at human KOR assessed as inhibition of U69593-stimulated [35S]GTPgammaS binding | F | 10.46 | pKd | 0.03 | nM | Kd | J Med Chem (2013) 56: 2178-2195 [PMID:23360448] |
ChEMBL | Binding affinity towards human cloned Opioid receptor kappa 1 using [3H]U-69593 | B | 9.39 | pKi | 0.41 | nM | Ki | J Med Chem (2003) 46: 3127-3137 [PMID:12825951] |
GtoPdb | - | - | 9.4 | pKi | 0.4 | nM | Ki |
ACS Chem Neurosci (2015) 6: 646-57 [PMID:25635572]; J Med Chem (2001) 44: 2687-90 [PMID:11495579]; PLoS ONE (2013) 8: e70701 [PMID:23976952] |
ChEMBL | Displacement of [3H]diprenorphine from human opioid kappa receptor expressed in CHO cells after 120 mins by scintillation counting | B | 10.23 | pKi | 0.06 | nM | Ki | J Med Chem (2011) 54: 8000-8012 [PMID:21958337] |
ChEMBL | Antagonist activity at kappa opioid receptor (unknown origin) | B | 10.52 | pKi | 0.03 | nM | Ki | Eur J Med Chem (2015) 90: 742-750 [PMID:25513968] |
ChEMBL | Antagonist activity at kappa opioid receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS | F | 11 | pKi | 0.01 | nM | Ki | Eur J Med Chem (2017) 141: 632-647 [PMID:29107424] |
GtoPdb | Measuring antagonism of U50,488-induced [35S]GTPγS binding | - | 11.22 | pKi | 0.01 | nM | Ki | J Med Chem (2001) 44: 2687-90 [PMID:11495579] |
ChEMBL | Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | F | 8.22 | pEC50 | 6 | nM | EC50 | J Med Chem (2010) 53: 5290-5301 [PMID:20568781] |
κ receptor/Kappa opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975] | ||||||||
ChEMBL | Displacement of [3H]U69593 from rat recombinant kappa opioid receptor expressed in CHO cells after 60 mins | B | 9.49 | pKi | 0.32 | nM | Ki | Eur J Med Chem (2015) 90: 742-750 [PMID:25513968] |
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 | 9.49 | pKi | 0.32 | nM | Ki | J Med Chem (2003) 46: 3127-3137 [PMID:12825951] |
ChEMBL | Binding affinity of compound for Opioid receptor kappa 1 was determined using [3H]U-69593 as radioligand from guinea pig caudate | B | 9.49 | pKi | 0.32 | nM | Ki | J Med Chem (2004) 47: 1070-1073 [PMID:14761209] |
ChEMBL | Antagonist activity at kappa opioid receptor in guinea pig caudate assessed as inhibition of U69593-stimulated [35S]-GTP[gammaS] binding | F | 10.7 | pKi | 0.02 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 2021-2032 [PMID:24690494] |
ChEMBL | Displacement of [3H]U69,593 from kappa opioid receptor in guinea pig brain membranes after 2 hrs | B | 10.7 | pKi | 0.02 | nM | Ki | Eur J Med Chem (2017) 141: 632-647 [PMID:29107424] |
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
ChEMBL | Displacement of [3H]diprenorphine from human opioid mu receptor expressed in CHO cells after 120 mins by scintillation counting | B | 7.94 | pKi | 11.5 | nM | Ki | J Med Chem (2011) 54: 8000-8012 [PMID:21958337] |
ChEMBL | Displacement of [3H]diprenorphine from human recombinant mu opioid receptor expressed in HEK cells after 60 mins | B | 8.4 | pKi | 4 | nM | Ki | Eur J Med Chem (2015) 90: 742-750 [PMID:25513968] |
ChEMBL | Binding affinity towards human cloned Opioid receptor mu 1 using [3H]DAMGO | B | 9.02 | pKi | 0.96 | nM | Ki | J Med Chem (2003) 46: 3127-3137 [PMID:12825951] |
ChEMBL | Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | F | 6.92 | pEC50 | 120 | nM | EC50 | J Med Chem (2010) 53: 5290-5301 [PMID:20568781] |
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
ChEMBL | Inhibition of [3H]DAMGO binding to Opioid receptor mu 1 of rat brain tissue | B | 8.43 | pKi | 3.73 | nM | Ki | J Med Chem (2003) 46: 3127-3137 [PMID:12825951] |
ChEMBL | Binding affinity of compound for Opioid receptor mu 1 was determined using [3H]DAMGO as radioligand from rat brain tissue | B | 8.43 | pKi | 3.73 | nM | Ki | J Med Chem (2004) 47: 1070-1073 [PMID:14761209] |
ChEMBL | Displacement of [3H]DAMGO from mu-opioid receptor in rat brain membranes after 2 hrs | B | 8.67 | pKi | 2.16 | nM | Ki | Eur J Med Chem (2017) 141: 632-647 [PMID:29107424] |
Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266] | ||||||||
ChEMBL | Antagonist activity at mu opioid receptor in guinea pig caudate assessed as inhibition of DAMGO-stimulated [35S]-GTP[gammaS] binding | F | 8.67 | pKi | 2.16 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 2021-2032 [PMID:24690494] |
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]