nor-binaltorphimine [Ligand Id: 1642] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL573214 (Nor-Binaltorphamine, (-)-Norbinaltorphimine, Norbinaltorphimine, Nor-Binaltorphimine, nor-BNI, norBNI)
  • 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 Mouse [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534]
  • 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]
  • Mu opioid receptor in Guinea pig [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
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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 Displacement of [3H]diprenorphine from human delta opioid receptor expressed in CHO cells after 1 hr by liquid scintillation counting B 7.19 pKi 65.2 nM Ki J Med Chem (2011) 54: 5868-5877 [PMID:21744827]
ChEMBL Binding affinity for delta opioid receptor was determined using radioligand [3H]DPDPE in Guinea pig brain membranes. B 7.37 pKi 43 nM Ki J Med Chem (1993) 36: 179-180 [PMID:8380614]
ChEMBL The binding affinity on delta-opioid receptor using [3H]- DPDPE as radioligand B 7.37 pKi 43 nM Ki J Med Chem (1994) 37: 1495-1500 [PMID:8182708]
ChEMBL Binding affinity determined on Opioid receptor delta 1 in Guinea pig brain membranes using radioligand [3H]DADLE B 7.37 pKi 42.9 nM Ki J Med Chem (1998) 41: 5188-5197 [PMID:9857089]
ChEMBL Binding affinity against Opioid receptor delta 1 was measured in the guinea pig brain membranes using [3H]DADLE in the presence of 1 uM unlabeled DAMGO as radioligand B 7.41 pKi 39 nM Ki J Med Chem (1991) 34: 1292-1296 [PMID:1849995]
ChEMBL Displacement of [3H]Naltrindole form human delta opioid receptor expressed in CHO cells B 7.62 pKi 24 nM Ki Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293]
ChEMBL In vitro binding affinity to human Opioid receptor delta 1 on CHO cell membranes using [3H]diprenorphine displacement. B 7.71 pKi 19.5 nM Ki J Med Chem (2003) 46: 2104-2109 [PMID:12747782]
ChEMBL Binding affinity towards cloned human Opioid receptor delta 1 in CHO cell membranes. B 7.72 pKi 19 nM Ki J Med Chem (2000) 43: 2698-2702 [PMID:10893307]
ChEMBL Antagonist activity on agonist (SNC-80) stimulated [35S]GTP-gamma-S, binding in cloned delta opioid receptors F 7.92 pKi 12.1 nM Ki J Med Chem (2001) 44: 2687-2690 [PMID:11495579]
ChEMBL Antagonist activity on agonist stimulated [35S]GTP-gamma-S, binding in guinea pig caudate membranes (10 uM SNC-80 as the agonist ligand for delta-receptor) F 7.99 pKi 10.2 nM Ki Bioorg Med Chem Lett (2003) 13: 529-532 [PMID:12565965]
ChEMBL Inhibition of stimulation of [35S]GTP-gamma-S, binding produced by the selective agonist (SNC-80, delta-receptor), in guinea pig caudate membranes F 7.99 pKi 10.2 nM Ki J Med Chem (2001) 44: 2687-2690 [PMID:11495579]
ChEMBL Inhibition of [35S]GTP-gamma-S, binding from Opioid receptor delta 1 in Guinea pig Caudate stimulated by SNC80 F 7.99 pKi 10.14 nM Ki J Med Chem (1998) 41: 5188-5197 [PMID:9857089]
ChEMBL Displacement of [3H]diprenorphine from human opioid delta receptor expressed in HEK293 cells after 120 mins by scintillation counting B 8.18 pKi 6.56 nM Ki J Med Chem (2011) 54: 8000-8012 [PMID:21958337]
GtoPdb - - 8.2 pKi - - - NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]
ChEMBL Binding affinity towards human cloned Opioid receptor delta 1 using [3H]Cl-DPDPE B 8.24 pKi 5.7 nM Ki J Med Chem (2003) 46: 3127-3137 [PMID:12825951]
ChEMBL Ability to displace [3H]DPDPE from human recombinant Opioid receptor delta 1 in CHO cells B 8.24 pKi 5.7 nM Ki J Med Chem (2003) 46: 314-317 [PMID:12519069]
ChEMBL Binding affinity against cloned human Opioid receptor delta 1 transfected into chinese hamster ovary cells using [3H]Cl-DPDPE as radioligand B 8.24 pKi 5.7 nM Ki J Med Chem (2003) 46: 5505-5511 [PMID:14640558]
ChEMBL Displacement of [3H]C1-DPDPE from human recombinant Opioid receptor delta 1 on CHO cell membranes. B 8.24 pKi 5.7 nM Ki J Med Chem (2003) 46: 1563-1566 [PMID:12672258]
ChEMBL Compound was evaluated for its binding affinity to CHO cells expressing cloned human Opioid receptor delta 1 by displacement of [3H]Cl-DPDPE B 8.24 pKi 5.7 nM Ki Bioorg Med Chem Lett (2000) 10: 2259-2261 [PMID:11055333]
ChEMBL Inhibition of [3H]C1-DPDPE binding to human delta opioid receptor expressed in CHO cells B 8.24 pKi 5.7 nM Ki J Med Chem (2004) 47: 5069-5075 [PMID:15456250]
ChEMBL Displacement of [3H]Cl-DPDPE from human recombinant delta opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method B 8.29 pKi 5.07 nM Ki Bioorg Med Chem (2014) 22: 4067-4072 [PMID:24973818]
ChEMBL Compound was evaluated for functional opioid activity by stimulation of [35S]GTP-gamma-S, in cloned human Opioid receptor delta 1 transfected into CHO cells F 8.35 pKi 4.42 nM Ki Bioorg Med Chem Lett (2000) 10: 2259-2261 [PMID:11055333]
ChEMBL Displacement of [3H]DPDPE from delta opioid receptor expressed in HEK293 cells by visible spectrophotometry B 9.1 pKi 0.8 nM Ki Bioorg Med Chem (2009) 17: 6671-6681 [PMID:19683449]
ChEMBL Antagonist activity at delta opioid receptor expressed in HEK293 cells assessed as inhibition of compound 14-induced [35S]GTPgammaS binding F 9.52 pKi 0.3 nM Ki Bioorg Med Chem (2009) 17: 6671-6681 [PMID:19683449]
ChEMBL Antagonist activity at human delta opioid receptor expressed in HEK cells assessed as inhibition of SNC-80-induced [35S]GTPgammaS binding F 7.62 pIC50 24 nM IC50 Bioorg Med Chem Lett (2010) 20: 5405-5410 [PMID:20719509]
ChEMBL Antagonist activity at human delta opioid receptor assessed as inhibition of SNC80-stimulated [35S]GTPgammaS binding F 7.62 pIC50 24 nM IC50 Bioorg Med Chem Lett (2010) 20: 5847-5852 [PMID:20727752]
ChEMBL Inhibition of Opioid receptor delta 1 by displacing 1 nM [3H]DPDPE in guinea pig brain membrane B 7.66 pIC50 22 nM IC50 J Med Chem (1992) 35: 4589-4594 [PMID:1335078]
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 Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
ChEMBL Displacement of [3H]- diprenorphine from mu-K303E-receptor expressed in HEK 293 cells B 7.38 pKi 41.5 nM Ki J Med Chem (2001) 44: 857-862 [PMID:11300867]
ChEMBL Binding affinity was measured on delta opioid receptor B 7.75 pKi 17.7 nM Ki J Med Chem (2001) 44: 3048-3053 [PMID:11543672]
ChEMBL Displacement of [3H]- diprenorphine from delta-receptor expressed in HEK 293 cells B 8.28 pKi 5.2 nM Ki J Med Chem (2001) 44: 857-862 [PMID:11300867]
GtoPdb - - 6.7 pIC50 - - - Proc Natl Acad Sci USA (1993) 90: 6736-40 [PMID:8393575]
ChEMBL Inhibitory activity against delta-opioid receptor in mouse vas deferens preparation using DADLE B 7.98 pIC50 10.4 nM IC50 J Med Chem (1993) 36: 2412-2415 [PMID:8360887]
δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
ChEMBL Binding affinity of compound for opioid receptor delta 1 was determined using [3H]DADLE as radioligand from rat brain tissue B 6.96 pKi 110.8 nM Ki J Med Chem (2004) 47: 1070-1073 [PMID:14761209]
ChEMBL Inhibition of [3H]-DADLE binding to Opioid receptor delta 1 of rat brain tissue B 7.07 pKi 86 nM Ki J Med Chem (2003) 46: 3127-3137 [PMID:12825951]
ChEMBL Ability to displace [3H]DADLE from Opioid receptor delta 1 of rat brain B 7.07 pKi 86 nM Ki J Med Chem (2002) 45: 3524-3530 [PMID:12139463]
ChEMBL Binding affinity of compound for opioid receptor delta 1 was determined using [3H]DADLE as radioligand from rat brain tissue B 7.07 pKi 86 nM Ki J Med Chem (2004) 47: 1070-1073 [PMID:14761209]
ChEMBL Binding affinity to delta-opioid receptor of rat brain using [3H]DADLE as radioligand B 7.07 pKi 86 nM Ki J Med Chem (2001) 44: 2687-2690 [PMID:11495579]
ChEMBL Binding affinity on HEK293 cells transiently transfected with plasmids encoding the rat Opioid receptor delta 1 B 7.38 pKi 41.5 nM Ki J Med Chem (2000) 43: 2759-2769 [PMID:10893314]
ChEMBL Inhibition of [3H]diprenorphine binding to rat Opioid receptor delta 1 expressed in C6 cells B 8.24 pKi 5.8 nM Ki J Med Chem (2005) 48: 1676-1679 [PMID:15743210]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Binding affinity using [3H]diprenorphine as the radioligand against E297K mutant Opioid receptor kappa 1 in COS-7 cells B 7.89 pKi 12.9 nM Ki J Med Chem (2000) 43: 1573-1576 [PMID:10780914]
ChEMBL Binding affinity using [3H]diprenorphine as the radioligand against E297A mutant Opioid receptor kappa 1 in COS-7 cells B 7.89 pKi 12.8 nM Ki J Med Chem (2000) 43: 1573-1576 [PMID:10780914]
ChEMBL Binding affinity to kappa opioid receptor B 9.05 pKi 0.9 nM Ki Bioorg Med Chem Lett (2010) 20: 5847-5852 [PMID:20727752]
ChEMBL Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in CHO cells after 1 hr by liquid scintillation counting B 9.07 pKi 0.85 nM Ki J Med Chem (2011) 54: 5868-5877 [PMID:21744827]
ChEMBL Inhibition of [3H]diprenorphine binding to human opioid receptor kappa 1 expressed in CHO cells B 9.4 pKi 0.4 nM Ki J Med Chem (2005) 48: 1676-1679 [PMID:15743210]
ChEMBL In vitro binding affinity towards human Opioid receptor kappa 1 on CHO cell membranes using [3H]diprenorphine displacement. B 9.43 pKi 0.37 nM Ki J Med Chem (2003) 46: 2104-2109 [PMID:12747782]
ChEMBL Binding affinity towards cloned human Opioid receptor kappa 1 in CHO cell membranes. B 9.44 pKi 0.36 nM Ki J Med Chem (2000) 43: 2698-2702 [PMID:10893307]
ChEMBL Displacement of [3H]Cl977 from human kappa opioid receptor expressed in HEK293 cells B 9.47 pKi 0.34 nM Ki J Med Chem (2010) 53: 4212-4222 [PMID:20441176]
ChEMBL Displacement of [125I]-IBNtxA from KOR-1 expressed in CHO cells B 9.64 pKi 0.23 nM Ki Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410]
ChEMBL Inhibition of [3H]U-69593 binding to human kappa opioid receptor expressed in CHO cells B 9.7 pKi 0.2 nM Ki J Med Chem (2004) 47: 5069-5075 [PMID:15456250]
ChEMBL Ability to displace [3H]U-69593 from human recombinant Opioid receptor kappa 1 in CHO cells B 9.7 pKi 0.2 nM Ki J Med Chem (2003) 46: 314-317 [PMID:12519069]
ChEMBL Binding affinity against cloned human Opioid receptor kappa 1 transfected into chinese hamster ovary cells using [3H]U-69593 as radioligand B 9.7 pKi 0.2 nM Ki J Med Chem (2003) 46: 5505-5511 [PMID:14640558]
ChEMBL Displacement of [3H]U-69593 from human recombinant Opioid receptor kappa 1 on CHO cell membranes. B 9.7 pKi 0.2 nM Ki J Med Chem (2003) 46: 1563-1566 [PMID:12672258]
ChEMBL Binding affinity towards human cloned Opioid receptor kappa 1 using [3H]U-69593 B 9.7 pKi 0.2 nM Ki J Med Chem (2003) 46: 3127-3137 [PMID:12825951]
ChEMBL Compound was evaluated for its binding affinity to CHO cells expressing cloned human Opioid receptor kappa 1 by displacing [3H]U-69593 B 9.7 pKi 0.2 nM Ki Bioorg Med Chem Lett (2000) 10: 2259-2261 [PMID:11055333]
ChEMBL Displacement of [3H]U69593 from human recombinant kappa opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method B 9.7 pKi 0.2 nM Ki Bioorg Med Chem (2014) 22: 4067-4072 [PMID:24973818]
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 [3H]diprenorphine from human opioid kappa receptor expressed in CHO cells after 120 mins by scintillation counting B 9.82 pKi 0.15 nM Ki J Med Chem (2011) 54: 8000-8012 [PMID:21958337]
ChEMBL Antagonist activity at kappa opioid receptor (unknown origin) B 9.82 pKi 0.15 nM Ki Eur J Med Chem (2015) 90: 742-750 [PMID:25513968]
ChEMBL Binding affinity using [3H]diprenorphine as the radioligand against wild-type Opioid receptor kappa 1 in COS-7 cells B 9.89 pKi 0.13 nM Ki J Med Chem (2000) 43: 1573-1576 [PMID:10780914]
ChEMBL Displacement of [3H]diprenorphine from human recombinant kappa opioid receptor expressed in in CHO cells B 9.9 pKi 0.13 nM Ki Bioorg Med Chem (2007) 15: 4434-4443 [PMID:17490886]
ChEMBL Antagonist activity on agonist (U50,488) stimulated [35S]GTP-gamma-S, binding in cloned opioid receptor kappa 1 F 10.15 pKi 0.07 nM Ki J Med Chem (2001) 44: 2687-2690 [PMID:11495579]
ChEMBL Compound was evaluated for its binding affinity by displacing [3H]U-69593 to human cloned Kappa opioid receptor transfected into CHO cells using [35S]GTP-gamma-S, assay F 10.41 pKi 0.04 nM Ki Bioorg Med Chem Lett (2000) 10: 2259-2261 [PMID:11055333]
ChEMBL Displacement of [3H]U69593 form human kappa opioid receptor expressed in CHO cells B 10.57 pKi 0.03 nM Ki Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293]
GtoPdb - - 11 pKi - - - NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407];
Binding and activity of opioid ligands at the cloned human delta, mu and kappa receptors.. The Delta Receptor (2003);
Life Sci (1995) 56: PL201-PL207 [PMID:7869844];
Proc Natl Acad Sci USA (1995) 92: 7006-10 [PMID:7624359];
J Pharmacol Exp Ther (1997) 282: 676-84 [PMID:9262330];
J Med Chem (1987) 30: 1991-4 [PMID:2444704]
ChEMBL Antagonist activity at human KOR expressed in CHO cell membranes assessed as inhibition of U50488-induced [35S]-GTPgammaS binding preincubated for 5 mins followed by U50488 and [35S]-GTPgammaS addition measured after 80 mins F 8.03 pIC50 9.3 nM IC50 J Med Chem (2018) 61: 6075-6086 [PMID:29939746]
ChEMBL Antagonist activity against HA-tagged human recombinant kappa opioid receptor expressed in CHO cells assessed as inhibition of U69,593-induced ERK phosphorylation pre-incubated with compound before U69,593 stimulation for 10 mins B 8.34 pIC50 4.6 nM IC50 Bioorg Med Chem (2015) 23: 3948-3956 [PMID:25593096]
ChEMBL Antagonistic activity in the Opioid receptor kappa 1-mediated [35S]GTP-gamma-S, binding assay against 50 nM U-50,488 F 8.36 pIC50 4.37 nM IC50 J Med Chem (2003) 46: 2104-2109 [PMID:12747782]
ChEMBL Antagonist activity against human kappa opioid receptor expressed in human U2OS cells co-expressing beta-arrestin2 pre-treated for 15 mins before U69,593 stimulation for 90 mins by DiscoveRx beta-arrestin2 recruitment based PathHunter assay B 8.6 pIC50 2.5 nM IC50 Bioorg Med Chem (2015) 23: 3948-3956 [PMID:25593096]
ChEMBL Antagonist activity at human kappa opioid receptor expressed in HEK cells assessed as inhibition of dynorphin A-induced [35S]GTPgammaS binding F 8.68 pIC50 2.1 nM IC50 Bioorg Med Chem Lett (2010) 20: 5405-5410 [PMID:20719509]
ChEMBL Antagonist activity at human kappa opioid receptor assessed as inhibition of dynorphin A-induced [35S]GTPgammaS binding F 8.68 pIC50 2.1 nM IC50 Bioorg Med Chem Lett (2010) 20: 5847-5852 [PMID:20727752]
ChEMBL Antagonist activity against HA-tagged human recombinant kappa opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay F 9.55 pIC50 0.28 nM IC50 Bioorg Med Chem (2015) 23: 3948-3956 [PMID:25593096]
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 Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534]
ChEMBL Displacement of [3H]U69,593 from kappa opioid receptor in mouse brain tissue B 8.78 pKd 1.65 nM Kd J Biol Chem (2007) 282: 29803-29811 [PMID:17702750]
ChEMBL Antagonist activity at mouse kappa opioid receptor-1 expressed in CHO cell membranes assessed as inhibition of U50,488H-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis F 8.54 pIC50 2.9 nM IC50 J Med Chem (2016) 59: 8381-8397 [PMID:27556704]
GtoPdb - - 8.9 pIC50 - - - Proc Natl Acad Sci USA (1993) 90: 6736-40 [PMID:8393575]
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 7.9 pKi 12.5 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 8.86 pKi 1.39 nM Ki J Med Chem (2001) 44: 857-862 [PMID:11300867]
ChEMBL Mutant factor against mu-[K303E] with Opioid receptor kappa 1 for binding affinity B 9.11 pKi 0.77 nM Ki J Med Chem (1998) 41: 4911-4914 [PMID:9836606]
ChEMBL Binding affinity on HEK293 cells transiently transfected with plasmids encoding the rat Opioid receptor kappa 1 B 9.61 pKi 0.24 nM Ki J Med Chem (2000) 43: 2759-2769 [PMID:10893314]
ChEMBL Displacement of [3H]diprenorphine from delta-W284E-receptor expressed in HEK 293 cells B 9.62 pKi 0.24 nM Ki J Med Chem (2001) 44: 857-862 [PMID:11300867]
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 9.92 pKi 0.12 nM Ki J Med Chem (1998) 41: 4911-4914 [PMID:9836606]
ChEMBL Displacement of [3H]diprenorphine from opioid receptor kappa 1 expressed in HEK 293 cells B 10.15 pKi 0.07 nM Ki J Med Chem (2001) 44: 857-862 [PMID:11300867]
GtoPdb - - 10.7 pKi - - - Biochem J (1993) 295 ( Pt 3): 625-8 [PMID:8240267];
Biochem J (1993) 295 ( Pt 3): 629-33 [PMID:8240268];
Proc Natl Acad Sci USA (1993) 90: 9954-8 [PMID:8234341]
Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
ChEMBL Binding affinity to opioid receptor kappa 1 of guinea pig brain, using [3H]U-69593 as radioligand B 6.96 pKi 109 nM Ki J Med Chem (2001) 44: 2687-2690 [PMID:11495579]
ChEMBL Binding affinity of compound for Opioid receptor kappa 1 was determined using [3H]U-69593 as radioligand from guinea pig caudate B 8.88 pKi 1.33 nM Ki J Med Chem (2004) 47: 1070-1073 [PMID:14761209]
ChEMBL Inhibition of [3H]U-69593 binding to Opioid receptor kappa 1 of guinea pig brain B 8.96 pKi 1.09 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 8.96 pKi 1.09 nM Ki J Med Chem (2004) 47: 1070-1073 [PMID:14761209]
ChEMBL Ability to displace [3H]U-69593 from Opioid receptor kappa 1 of guinea pig brain B 8.96 pKi 1.09 nM Ki J Med Chem (2002) 45: 3524-3530 [PMID:12139463]
ChEMBL Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum B 9.06 pKi 0.86 nM Ki Bioorg Med Chem (2011) 19: 1205-1221 [PMID:21256034]
ChEMBL Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum B 9.06 pKi 0.86 nM Ki Bioorg Med Chem Lett (2010) 20: 5035-5038 [PMID:20685120]
ChEMBL Binding affinity was measured on opioid receptor kappa 1 B 9.09 pKi 0.81 nM Ki J Med Chem (2001) 44: 3048-3053 [PMID:11543672]
ChEMBL Binding affinity determined on Opioid receptor kappa 1 in Guinea pig brain membranes using radioligand [3H]U-69593 B 9.55 pKi 0.28 nM Ki J Med Chem (1998) 41: 5188-5197 [PMID:9857089]
ChEMBL Binding affinity for k opioid receptor was determined using [3H]U-69593 radioligand in Guinea pig brain membranes B 9.55 pKi 0.28 nM Ki J Med Chem (1993) 36: 179-180 [PMID:8380614]
ChEMBL The binding affinity on kappa-opioid receptor using [3H]- U-69,593 as radioligand B 9.55 pKi 0.28 nM Ki J Med Chem (1994) 37: 1495-1500 [PMID:8182708]
ChEMBL Binding affinity of compound was measured against Opioid receptor kappa 1 on electrically stimulated guinea pig ileal longitudinal muscle myenteric plexus (GPI) at 100 nM preparation using U-50,488H as agonist B 9.59 pKi 0.26 nM Ki J Med Chem (1991) 34: 1292-1296 [PMID:1849995]
ChEMBL Antagonist activity on agonist stimulated [35S]GTP-gamma-S, binding in guinea pig caudate membranes (10 uM U69,593 as the agonist ligand for kappa-receptor) F 9.92 pKi 0.12 nM Ki Bioorg Med Chem Lett (2003) 13: 529-532 [PMID:12565965]
ChEMBL Inhibition of stimulation of [35S]GTP-gamma-S, binding produced by the selective agonist (U69593, kappa-receptor), in guinea pig caudate membranes F 10.42 pKi 0.04 nM Ki J Med Chem (2001) 44: 2687-2690 [PMID:11495579]
ChEMBL Inhibition of [35S]GTP-gamma-S, binding from Opioid receptor kappa 1 in Guinea pig Caudate stimulated by U69,593 F 10.42 pKi 0.04 nM Ki J Med Chem (1998) 41: 5188-5197 [PMID:9857089]
ChEMBL Inhibitory activity against kappa-opioid receptor in guinea pig ileum longitudinal muscle using ethylketazocine B 6.74 pIC50 181 nM IC50 J Med Chem (1993) 36: 2412-2415 [PMID:8360887]
ChEMBL Inhibition of opioid receptor kappa by displacing 0.5 nM [3H]bremazocine in guinea pig brain membrane B 8.22 pIC50 6 nM IC50 J Med Chem (1992) 35: 4589-4594 [PMID:1335078]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Displacement of [3H]diprenorphine from human mu opioid receptor expressed in CHO cells after 1 hr by liquid scintillation counting B 7.1 pKi 79.9 nM Ki J Med Chem (2011) 54: 5868-5877 [PMID:21744827]
ChEMBL In vitro binding affinity to human Opioid receptor mu 1 on CHO cell membranes using [3H]diprenorphine displacement. B 7.1 pKi 79.4 nM Ki J Med Chem (2003) 46: 2104-2109 [PMID:12747782]
ChEMBL Binding affinity using [3H]diprenorphine as the radioligand against wild-type Opioid receptor mu 1 in COS-7 cells B 7.15 pKi 70 nM Ki J Med Chem (2000) 43: 1573-1576 [PMID:10780914]
ChEMBL Binding affinity towards cloned human Opioid receptor mu 1 in CHO cell membranes. B 7.25 pKi 56 nM Ki J Med Chem (2000) 43: 2698-2702 [PMID:10893307]
ChEMBL Displacement of [3H]diprenorphine from human opioid mu receptor expressed in CHO cells after 120 mins by scintillation counting B 7.49 pKi 32.4 nM Ki J Med Chem (2011) 54: 8000-8012 [PMID:21958337]
ChEMBL Compound was evaluated for its binding affinity to CHO cells expressing cloned human Opioid receptor mu 1 by displacing [3H]-DAMGO B 7.68 pKi 21 nM Ki Bioorg Med Chem Lett (2000) 10: 2259-2261 [PMID:11055333]
ChEMBL Inhibition of [3H]DAMGO binding to human Mu opioid receptor expressed in CHO cells B 7.68 pKi 21 nM Ki J Med Chem (2004) 47: 5069-5075 [PMID:15456250]
ChEMBL Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method B 7.68 pKi 21 nM Ki Bioorg Med Chem (2014) 22: 4067-4072 [PMID:24973818]
ChEMBL Ability to displace [3H]DAMGO from human recombinant Opioid receptor mu 1 in CHO cells B 7.68 pKi 21 nM Ki J Med Chem (2003) 46: 314-317 [PMID:12519069]
ChEMBL Binding affinity against cloned human Opioid receptor mu 1 transfected into chinese hamster ovary cells using [3H]DAMGO as radioligand B 7.68 pKi 21 nM Ki J Med Chem (2003) 46: 5505-5511 [PMID:14640558]
ChEMBL Displacement of [3H]DAMGO from human recombinant Opioid receptor mu 1 on CHO cell membranes. B 7.68 pKi 21 nM Ki J Med Chem (2003) 46: 1563-1566 [PMID:12672258]
ChEMBL Binding affinity towards human cloned Opioid receptor mu 1 using [3H]DAMGO B 7.68 pKi 21 nM Ki J Med Chem (2003) 46: 3127-3137 [PMID:12825951]
GtoPdb - - 7.7 pKi - - - NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]
ChEMBL Compound was evaluated for its binding affinity by displacing DAMGO to human cloned mu opioid receptor transfected into CHO cells using [35S]GTP-gamma-S, assay F 7.72 pKi 18.9 nM Ki Bioorg Med Chem Lett (2000) 10: 2259-2261 [PMID:11055333]
ChEMBL Displacement of [3H]DAMGO form human mu opioid receptor expressed in CHO cells B 8.57 pKi 2.7 nM Ki Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293]
ChEMBL Binding affinity using [3H]diprenorphine as the radioligand against K303E Opioid receptor mu 1 in COS-7 cells B 9.03 pKi 0.94 nM Ki J Med Chem (2000) 43: 1573-1576 [PMID:10780914]
ChEMBL Antagonist activity at human mu opioid receptor expressed in HEK cells assessed as inhibition of DAMGO-induced [35S]GTPgammaS binding F 6.67 pIC50 212 nM IC50 Bioorg Med Chem Lett (2010) 20: 5405-5410 [PMID:20719509]
ChEMBL Antagonist activity at human mu opioid receptor assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding F 6.67 pIC50 212 nM IC50 Bioorg Med Chem Lett (2010) 20: 5847-5852 [PMID:20727752]
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 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 6.99 pKi 101.9 nM Ki J Med Chem (1998) 41: 4911-4914 [PMID:9836606]
ChEMBL Binding affinity to mu-opioid receptor of rat brain using [3H]DAMGO as radioligand B 7.19 pKi 65.06 nM Ki J Med Chem (2001) 44: 2687-2690 [PMID:11495579]
ChEMBL Ability to displace [3H]DAMGO from Opioid receptor mu 1 of rat brain B 7.19 pKi 65 nM Ki J Med Chem (2002) 45: 3524-3530 [PMID:12139463]
ChEMBL Binding affinity of compound for Opioid receptor mu 1 was determined using [3H]DAMGO as radioligand from rat brain tissue B 7.19 pKi 65 nM Ki J Med Chem (2004) 47: 1070-1073 [PMID:14761209]
ChEMBL Inhibition of [3H]DAMGO binding to Opioid receptor mu 1 of rat brain tissue B 7.19 pKi 65 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 7.25 pKi 56.6 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 7.3 pKi 49.7 nM Ki J Med Chem (2000) 43: 2759-2769 [PMID:10893314]
ChEMBL Antagonist activity on agonist (DAMGO) stimulated [35S]GTP-gamma-S, binding in cloned mu opioid receptors F 7.8 pKi 15.8 nM Ki J Med Chem (2001) 44: 2687-2690 [PMID:11495579]
ChEMBL Binding affinity of compound for Opioid receptor mu 1 was determined using [3H]DAMGO as radioligand from rat brain tissue B 8.08 pKi 8.3 nM Ki J Med Chem (2004) 47: 1070-1073 [PMID:14761209]
ChEMBL Inhibition of [3H]diprenorphine binding to rat Opioid receptor mu 1 expressed in C6 cells B 8.92 pKi 1.2 nM Ki J Med Chem (2005) 48: 1676-1679 [PMID:15743210]
ChEMBL Displacement of [3H]- diprenorphine from mu-W318A-receptor expressed in HEK 293 cells B 9.41 pKi 0.39 nM Ki J Med Chem (2001) 44: 857-862 [PMID:11300867]
ChEMBL Displacement of [3H]- diprenorphine from mu-W318A-receptor expressed in HEK 293 cells B 9.66 pKi 0.22 nM Ki J Med Chem (2001) 44: 857-862 [PMID:11300867]
Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
ChEMBL Binding affinity determined on Opioid receptor mu 1 in Guinea pig brain membranes using radioligand [3H]DAMGO B 7.33 pKi 47.2 nM Ki J Med Chem (1998) 41: 5188-5197 [PMID:9857089]
ChEMBL Binding affinity of compound was measured against Opioid receptor mu 1 on electrically stimulated guinea pig ileal longitudinal muscle myenteric plexus (GPI)at 100 nM preparation using DAMGO as agonist B 7.33 pKi 47 nM Ki J Med Chem (1991) 34: 1292-1296 [PMID:1849995]
ChEMBL The binding affinity against mu-opioid receptor using [3H]- DAMGO as radioligand B 7.33 pKi 47 nM Ki J Med Chem (1994) 37: 1495-1500 [PMID:8182708]
ChEMBL Binding affinity for mu opioid receptor was determined using radioligand [3H][D-Ala2,MePhe4,Gly-ol6]enkephalin (DAMGO) in Guinea pig brain membranes. B 7.33 pKi 47 nM Ki J Med Chem (1993) 36: 179-180 [PMID:8380614]
ChEMBL Binding affinity was measured on mu opioid receptor B 7.55 pKi 28.4 nM Ki J Med Chem (2001) 44: 3048-3053 [PMID:11543672]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in guinea pig forebrain B 7.55 pKi 28.2 nM Ki Bioorg Med Chem (2011) 19: 1205-1221 [PMID:21256034]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in guinea pig forebrain B 7.55 pKi 28.2