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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 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]