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) |
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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 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]
