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 nM Ki Bioorg Med Chem Lett (2010) 20: 5035-5038 [PMID:20685120]
ChEMBL Inhibition of [35S]GTP-gamma-S, binding from Opioid receptor mu 1 in Guinea pig Caudate stimulated by DAMGO F 7.78 pKi 16.75 nM Ki J Med Chem (1998) 41: 5188-5197 [PMID:9857089]
ChEMBL inhibition of stimulation of [35S]GTP-gamma-S, binding produced by the selective agonist (DAMGO, mu-receptor), in guinea pig caudate membranes F 7.78 pKi 16.7 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 DAMGO as the agonist ligand for mu-receptor) F 7.83 pKi 14.8 nM Ki Bioorg Med Chem Lett (2003) 13: 529-532 [PMID:12565965]
ChEMBL Inhibition of opioid receptor mu by displacing 1 nM [3H]DAGO in guinea pig brain membrane B 7.74 pIC50 18 nM IC50 J Med Chem (1992) 35: 4589-4594 [PMID:1335078]
ChEMBL Inhibitory activity against mu-opioid receptor in guinea pig ileum longitudinal muscle using morphine B 8.08 pIC50 8.3 nM IC50 J Med Chem (1993) 36: 2412-2415 [PMID:8360887]

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]